Your browser doesn't support javascript.
loading
Mostrar: 20 | 50 | 100
Resultados 1 - 20 de 34
Filtrar
Más filtros

Bases de datos
Tipo del documento
Intervalo de año de publicación
1.
An Acad Bras Cienc ; 95(suppl 1): e20220427, 2023.
Artículo en Inglés | MEDLINE | ID: mdl-37556712

RESUMEN

The antiulcer mechanisms of the dry extract of T. erecta flowers (DETe) were studied here. The acute ulcers induced by acidified ethanol or indomethacin were reproduced in mice pretreated with DETe (3 - 300 mg/kg). The antiulcer activity of DETe was also verified in mice pretreated with NEM, L-NAME, indomethacin, or yohimbine. The antisecretory effect of DETe was verified in rats, and its anti-Helicobacter pylori activity was determined in vitro. DETe (300 mg/kg, p.o) reduced the ethanol- or indomethacin-induced ulcer by 49 and 93%, respectively. The pre-treatment with L-NAME, NEM or yohimbine abolished the gastroprotective effect of DETe. However, DETe did not change the volume, acidity, or peptic activity in rats and did not affect H. pylori. This study expands knowledge about the antiulcerogenic potential of DETe, evidencing the role of nitric oxide, non-protein sulfhydryl groups, α2 adrenergic receptors, and prostaglandins, but not antisecretory or anti-H. pylori properties.


Asunto(s)
Extractos Vegetales , Tagetes , Ratas , Ratones , Animales , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico , Ratas Wistar , NG-Nitroarginina Metil Éster/farmacología , Mucosa Gástrica , Indometacina/farmacología , Yohimbina/farmacología , Etanol/farmacología , Flores
2.
J Ethnopharmacol ; 309: 116338, 2023 Jun 12.
Artículo en Inglés | MEDLINE | ID: mdl-36870462

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: Fridericia chica (Bonpl.) L.G. Lohmann (Bignoniaceae), is a climber native to Brazil, found in all Brazilian biomes. It is mostly known in Brazil as "carajiru," and home medicines made from the leaves have been used to cure disorders including stomach ulcers and other gastrointestinal disorders. AIM OF THE STUDY: The objective of the study was to investigate the F. chica hydroethanolic extract of leaves (HEFc) preventative and curative antiulcer gastrointestinal efficacy as well as the mechanisms of action using in vivo rodent models. MATERIALS AND METHODS: F. chica was collected in the municipality of Juína, Mato Grosso, and its leaves were used to prepare the extract by maceration technique (70% hydroethanol in the 1:10 ratio, w/v) to obtain the HEFc. The chromatographic analysis of HEFc was carried out by High Performance Liquid Chromatography-Photo Diode Array-Electrospray Ionization-Mass Spectrometry (HPLC-PDA-ESI-MS)- LCQ Fleet™ system. To determine the potential antiulcer potential of HEFc (1, 5 and 20 mg/kg, p.o.), the gastroprotective activity was assessed in various animal models of stomach ulcers caused by acidified ethanol, water constraint stress, indomethacin, (acute), and acid acetic (chronic). Additionally, the prokinetic properties of the HEFC were assessed in mice. The gastroprotective underlying mechanisms were evaluated by the histopathological analysis and determination of gastric secretion (volume, free and total acidity), gastric barrier mucus, activation of PGs, NO, K +ATP channels, α2-adrenoceptor, antioxidant activity (GSH, MPO and MDA), NO and mucosal cytokines (TNF-α, IL-1ß, and IL-10) levels. RESULTS: The chemical composition of HEFc was analyzed and apigenin, scutellarin, and carajurone were identified. HEFc (1, 5 and 20 mg/kg) showed effect against acute ulcers induced by HCl/EtOH with a reduction in the ulcerated area of 64.41% (p < 0.001), 54.23% (p < 0.01), 38.71% (p < 0.01), respectively. In the indomethacin experiment, there was no change in the doses tested, whereas in the water immersion restraint stress ulcer there was a reduction of lesions at doses of 1, 5, and 20 mg/kg by 80.34% (p < 0.001), 68.46% (p < 0.01) and 52.04% (p < 0.01). HEFc increased the mucus production at doses of 1 and 20 mg/kg in 28.14% (p < 0.05) and 38.36% (p < 0.01), respectively. In the pyloric ligation-induced model of gastric ulceration, the HEFc decreased the total acidity in all doses by 54.23%, 65.08%, and 44.40% (p < 0.05) and gastric secretory volume in 38.47% at dose of 1 mg/kg (p < 0,05) and increased the free acidity at the dose of 5 mg/kg by 11.86% (p < 0.05). The administration of EHFc (1 mg/kg) showed a gastroprotective effect possibly by stimulating the release of prostaglandins and activating K+ATP channels and α2-adrenoreceptors. Also, the gastroprotective effect of HEFc involved an increase in CAT and GSH activities, and a reduction in MPO activity and MDA levels. In the chronic gastric ulcer model, the HEFc (1, 5 and 20 mg/kg) decreased the ulcerated area significantly (p < 0.001) at all doses by 71.37%, 91.00%, and 93.46%, respectively. In the histological analysis, HEFc promoted the healing of gastric lesions by stimulating the formation of granulation tissue and consequently epithelialization. On the other hand, regarding the effect of HEFc on gastric emptying and intestinal transit, it was observed that the extract did not alter gastric emptying, but there was an increase in intestinal transit at the dose of 1 mg/kg (p < 0.01). CONCLUSION: These outcomes confirmed the advantages of Fridericia chica leaves for the treatment of stomach ulcers, which are well-known. HEFc was discovered to have antiulcer characteristics through multitarget pathways, which might be related to an increase in stomach defense mechanisms and a decrease in defensive factor. HEFc can be regarded as a potential new antiulcer herbal remedy because of its antiulcer properties, which may be attributed to the mixture of flavonoids, apigenin, scutellarin and carajurone.


Asunto(s)
Antiulcerosos , Bignoniaceae , Gastritis , Úlcera Gástrica , Ratas , Ratones , Animales , Apigenina/análisis , Úlcera/tratamiento farmacológico , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico , Extractos Vegetales/química , Úlcera Gástrica/inducido químicamente , Úlcera Gástrica/tratamiento farmacológico , Úlcera Gástrica/patología , Fitoterapia , Ratas Wistar , Antiulcerosos/farmacología , Antiulcerosos/uso terapéutico , Antiulcerosos/química , Indometacina/farmacología , Etanol/química , Gastritis/tratamiento farmacológico , Agua , Adenosina Trifosfato , Hojas de la Planta/química
3.
Pharmaceuticals (Basel) ; 16(3)2023 Mar 11.
Artículo en Inglés | MEDLINE | ID: mdl-36986529

RESUMEN

Piper glabratum Kunth is a plant traditionally used to treat pain and inflammation in the Mato Grosso do Sul, Brazil. Even pregnant women consume this plant. Toxicology studies of the ethanolic extract from the leaves of P. glabratum (EEPg) could establish the safety of popular use of P. glabratrum. Thus, the effects of the ethanolic extract of leaves of P. glabratum (EEPg) on the reproductive performance and embryofetal development of Swiss mice were evaluated. Pregnant female mice were treated with 100, 1000 and 2000 mg/kg throughout the gestational period by gavage (p.o). The control group received the EEPg vehicle (Tween 80-1%) in the proportion of 0.1 mL/10 g (p.o.). The results demonstrated that EEPg has low maternal toxic potential and does not alter the reproductive performance of females. However, it altered embryofetal development and caused fetal weight reduction (increasing the frequency of small-for-gestational-age fetuses) at the two highest doses. In addition, it interfered with placental weight, placental index and placental efficiency. The frequency of visceral malformations increased by 2.8 times for the lowest dose of EEPg, and skeletal malformations increased by 2.48, 1.89 and 2.11 times for doses of 100, 1000 and 2000 mg/kg of EEPg, respectively. It is noteworthy that 100% of the offspring treated with EEPg showed changes in the ossification process. Thus, it is considered that the EEPg has low maternal toxic potential; it does not alter the reproductive performance of females. However, it is teratogenic and interferes, mainly, in the ossification process, and therefore its use is contraindicated in the gestational period.

4.
J Ethnopharmacol ; 302(Pt B): 115921, 2023 Feb 10.
Artículo en Inglés | MEDLINE | ID: mdl-36403741

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: The traditional medical system plays a major role in healthcare in Kachin State, Myanmar, where long-term political instability persists and conventional healthcare facilities are inadequate. A knowledge of the traditional medicinal plants therefore benefits the Kachin people, yet documentation and records of the uses of these plants are rare. In this study, we attempt to answer the questions on what medicinal plants and how they are used by the Kachin people. AIM OF THE STUDY: We aimed to document knowledge of the traditional medicinal plants and to identify those most frequently used by the Kachin people. MATERIALS AND METHODS: Eighty-two informants from eight villages in three townships were interviewed, and their knowledge of medicinal plants was recorded. The reported ailments were classified to the standard categories of the International Classification of Primary Care-2 (ICPC-2) system. Use reports (UR) were employed to evaluate the knowledge consensus of the informants. RESULTS: We recorded a total of 117 species used as medicinal plants, of which 22 are newly recorded medicinal plant species for Myanmar. The plants belonged to 103 genera in 52 families, and were used to treat a total of 72 ailments from 17 ICPC-2 disease categories. Fabaceae and Lamiaceae were the most highly represented families of medicinal plants, with eleven and eight species used, respectively. The most cited species based on URs were Tinospora cordifolia (Willd.) Hook.f. & Thomson (URs = 39), Oroxylum indicum (L.) Kurz (URs = 28), Aquilaria malaccensis Lam. (URs = 26), Chromolaena odorata (L.) R.M.King & H.Rob. (URs = 24), and Chloranthus elatior Link. (URs = 22). Digestive system disorder was the most prevalent disease category, and was treated with 47 different medicinal plants (URs = 142). Leaves were the most commonly used plant part; decoction was the dominant method of preparation; and oral consumption was the most frequent method of administration. CONCLUSION: Our study documented a list of 117 medicinal plants and their uses in traditional medicine based on the local knowledge of the Kachin people. The study also identified the five most frequently cited species and found that the plants investigated are used to treat a total of 72 diseases. The 642 therapeutic reports we collected showcase a rich and diverse living knowledge of medicinal plant use by the Kachin people. Moreover, we present 22 new medicinal records, enriching the list of known medicinal plants in Myanmar. This exploratory study has enabled us to assemble the local knowledge of the Kachin people into solid dataset that will allow further scientific validation and will potentially contribute to better integration of medicinal plants into the healthcare provision for Kachin people in Myanmar.


Asunto(s)
Medicina Tradicional , Plantas Medicinales , Humanos , Bignoniaceae , Lamiaceae , Mianmar
5.
J Ethnopharmacol ; 300: 115742, 2023 Jan 10.
Artículo en Inglés | MEDLINE | ID: mdl-36152784

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: Despite widespread use of herbal remedies for treating arthritis and osteosarcoma, many plants are still not pharmacologically evaluated for their efficacy. Contrary to many non-steroidal, immunosuppressants, antibiotics, and antineoplastic drugs that have adverse effects, phytotherapeutic compounds have promising benefits with fewer complications. In this study the unexplored Northeastern India indigenous plant Trevesia palmata (Roxb. ex Lindl.) Vis. used in traditional medicine to cure bone fractures is chosen for studying anti-proliferative and anti-rheumatic properties. AIM OF THE STUDY: This study designed to explore the polyphenolic composition, antioxidant, anti-inflammatory and anti-arthritic potential of T. palmata leaf extracts. Further, the cellular activity was studied using MG 63 osteoblast cell lines and pharmacologically evaluated using Complete Freund's Adjuvant (CFA) induced arthritic rat model. MATERIALS AND METHODS: In vitro free radical scavenging activity, anti-inflammatory and anti-arthritic activities of extracts were analyzed using standardized methods. The polyphenolic profiling and apoptosis inducing ability of T. palmata ethyl acetate (TPEA) extract on MG 63 osteoblast cell lines were analyzed. The in vivo pharmacological studies were carried out with low dose 250 mg/kg and high dose of 500 mg/kg of T. palmata. The biochemical and haematological parameters and in vivo antioxidant activity were evaluated for the control and treated groups. Radiological and histological study were done to understand the impact and penetration of inflammatory arthritis from tissues to joint bones. RESULTS: TPEA showed highest free radical scavenging activity (DPPH - 4.72 IC50, ABTS - 242.33 ± 6.81 mM TE/g extract), anti-inflammatory (40.04% inhibition of RBC lysis) and anti-arthritic activity (32.4% inhibition of protein denaturation) with the presence of gallic acid, catechin, caffeic acid, rutin, quercetin and naringenin. The TPEA extract inhibited cell proliferation of MG 63 osteoblast cells and induced apoptosis by arresting cell cycle at different phases. After acute toxicity studies the doses 250 mg/kg and 500 mg/kg were fixed and showed better results in CFA-induced arthritic animals. Thus, the extract phytoconstituents may have immense potential against chronic inflammation, joint ailments, bone cancer and arthritis which serves as a phytomedicine contrary to synthetic medications. CONCLUSIONS: The potential treatment of polyphenolic compounds in the T. palmata extract on osteosarcoma and arthritis was demonstrated from this study. Thus, cellular inflammatory infiltrates are significantly reduced in bone and joint tissues as well.


Asunto(s)
Araliaceae , Artritis Experimental , Catequina , Osteosarcoma , Animales , Antibacterianos/uso terapéutico , Antiinflamatorios/farmacología , Antiinflamatorios/uso terapéutico , Antioxidantes/farmacología , Antioxidantes/uso terapéutico , Artritis Experimental/tratamiento farmacológico , Artritis Experimental/patología , Línea Celular , Radicales Libres , Adyuvante de Freund , Ácido Gálico/uso terapéutico , Inmunosupresores , Osteosarcoma/tratamiento farmacológico , Extractos Vegetales/química , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico , Quercetina/uso terapéutico , Ratas , Rutina
6.
J Ethnopharmacol ; 300: 115745, 2023 Jan 10.
Artículo en Inglés | MEDLINE | ID: mdl-36162548

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: Anadenanthera colubrina (Vell.) Brenan is an endemic tree to South America and different parts of it are used by the population for the treatment of various diseases, as well as in indigenous rituals. This species has high pharmacological potential but may present toxic potential due to the presence of psychotropic compounds. AIM OF THE STUDY: To review published studies with the species A. colubrina regarding ethnobotanical, phytochemical, pharmacological and toxicological aspects, as well as discuss perspectives for new research and protection of this species. MATERIALS AND METHODS: A literature review was performed by accessing published articles on databases such as: PubMed, Science Direct, Scielo, Scopus, Taylor and Francis online, Springer Link, National Center for Biotechnology Information (NCBI), ACS Publications, Chemspider and Google Scholar. The keywords used were: "Anadenanthera colubrina" or "Mimosa colubrina" or "Piptadenia colubrina" or "Piptadenia macrocarpa" or "Piptadenia grata" or "Anadenanthera macrocarpa" and "medicinal plants" or "pharmacological" or "phytochemicals" or "traditional use" or "toxicological" or "ethnobotanical" or "pre-clinical trial" or "clinical". Articles found by database searches and search engines were screened at four stages: (i) title screening, (ii) locality screening, (iii) abstract screening, and (iv) full text. Other articles found through supplementary searches were screened in the full text whenever available. Each article was assessed by three reviewers at the title and abstract screening stages, except for those found in Portuguese databases that were assessed by the native reviewer. RESULTS: This robust tree has been popularly useful for agroeconomic, medicinal and as a hallucinogen in religious rituals. According to the published studies, the main parts of the plant are the bark and seeds that are mostly used for respiratory conditions and as entheogens, respectively. It is a rich traditional herbal medicine with many pharmacological properties such as anti-inflammatory, antinociceptive, antidiarrheal, wound healing, antimicrobial, antitumoral, antioxidant, antiaddictive, insecticide and allelopathic that were described in in vitro and in vivo assays, and approximately 56 compounds were identified, suggesting a therapeutic potential for this species. Although most relate to medicinal uses, these are preliminaries and do not show the mechanism of action. The phytochemical assays showed the presence of phenolic compounds, flavonoids, triterpenes, steroids and alkaloids. Some of the compounds are anadanthoflavone, which is exclusive to this species, and no pharmacological or toxicological studies have yet demonstrated this compound. Another important compound is bufotenine which was isolated from seeds and is related to hallucinogenic and antiviral activity. The extracts made from leaves, bark, gum, and fruits appear to be safe, according to both in vivo and in vitro toxicology testing, which all shown low toxicity. Due to the presence of bufotenine in the seeds, it can be toxic, however, it was not found in toxicological assays with the seed extracts. CONCLUSIONS: Therefore, part of the studies confirms the popular use of A. colubrina, however, more assays with isolated compounds and with the different extracts are necessary to corroborate other uses and the mechanism of action of their pharmacological effects needs to discuss in more detail. Therefore, the present review would be identified the gaps and suggests further studies oriented to validate the popular use. Thus, it must be noted that the use of this species must be controlled in order to minimize the environmental impact, as most of the pharmacological potential was shown with the bark and seeds. Due to its wide use in folk medicine, it is part of the Brazilian medicinal species with priority for conservation.


Asunto(s)
Alcaloides , Colubrina , Fabaceae , Alucinógenos , Insecticidas , Plantas Medicinales , Triterpenos , Analgésicos , Antiinflamatorios , Antidiarreicos , Antioxidantes , Antivirales , Brasil , Bufotenina , Etnofarmacología , Flavonoides , Fitoquímicos/uso terapéutico , Fitoquímicos/toxicidad , Fitoterapia , Extractos Vegetales/química , Extractos Vegetales/toxicidad
7.
Chem Biodivers ; 19(12): e202200322, 2022 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-36269048

RESUMEN

Preparations of Helicteres sacarolha (Malvaceae) leaves and roots are used in the form of decoction, infusion or maceration, to treat gastrointestinal disturbances, among others. Studies supporting some of its ethnomedicinal uses are still incipient. The present study aimed to investigate it potential effect on chronic ulcer, ulcerative colitis and possible prokinetic activities as part of its mechanism of action. The powdered leaves of Helicteres sacarolha (HEHs) was prepared by maceration in 70 % hydroethanolic solution. Its qualitative phytochemical constituents were investigated by direct flow injection analysis coupled to atmospheric pressure chemical ionization ion trap tandem mass spectrometry (FIA-APCI-IT-MSn ). The gastric ulcer healing effect was evaluated in acetic acid induced chronic ulcer in mice and the lesions were evaluated, including analysis of blood plasma cytokine levels. The prokinetic properties (gastric emptying and intestinal transit) were carried out in mice. Potential anti-ulcerative colitis activity was evaluated in rats using 2,4,6-trinitrobenzenesulfonic acid (5 % TNBS) -induced colitis. All animal experiments were carried out at the doses of 20, 50 and 250 mg/kg (p.o.). Eight compounds were putatively identified, specifically lariciresinol, and its derivatives, kaempferol derivatives and Tricin-O-Glc. The extract promoted increased gastric ulcer healing at all doses tested. Modulation of the cytokines involved inhibition of some key pro-inflammatory cytokines with maximum effect on IL-1ß (70 %, 50 mg/kg, p<0.05), TNF-α (79 %, 20 mg/kg, p<0.01), and in the anti-inflammatory cytokines, namely IL-10 (57 %, 50 mg/kg, p<0.05) and IL-17 (79 %, only at 50 mg/kg, p<0.05). Histological findings demonstrated a mitigated inflammatory activity, and tissues undergoing regeneration. HEHs treatment caused delayed gastric emptying, and increased intestinal transit, but had no effect in the experimentally induced ulcerative colitis. We report for the first time putatively the presence of Lariciresinol and tricin derivatives from the hydroethanolic leaves extract of H. sacarolha. Its possible mechanism of actions of gastric ulcer healing involves cytokines modulation, mitigation of inflammatory response and tissue regeneration and provoked opposing effect in the gastrointestinal system. The present study demonstrates the therapeutic potential of H. sacarolha leaves used in Brazilian ethnomedicine in the treatment of chronic gastric ulcer.


Asunto(s)
Antiulcerosos , Malvaceae , Úlcera Gástrica , Ratas , Ratones , Animales , Úlcera Gástrica/inducido químicamente , Úlcera Gástrica/tratamiento farmacológico , Úlcera Gástrica/patología , Citocinas , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico , Extractos Vegetales/química , Fitoterapia/métodos , Ratas Wistar , Antiulcerosos/farmacología , Antiulcerosos/uso terapéutico , Antiulcerosos/química , Malvaceae/química
8.
Artículo en Inglés | MEDLINE | ID: mdl-35646149

RESUMEN

Humans have been using herbs to prevent and cure various ailments since antiquity, and Ipomoea wightii is a significant medicinal plant known for its wide ethnobotanical uses. Although the plant is known to treat ulcers, there is no significant scientific validation. The present study aimed to assess the acute toxicity, subacute toxicity, and antiulcer properties of the leaf methanol extract of I. wightii (IWL). In the subacute study, the extracts were given orally at 100, 200, and 400 mg/kg doses for 28 days, and we analyzed the biochemical and histological parameters to evaluate the toxicity of IWL. Two different models were assessed to explore antiulcer properties, such as indomethacin- and ethanol-induced ulcer model. Ulcer areas and ulceration percentage histopathology of the stomach were used to study the efficacy of extracts. The acute toxicity study showed that IWL was safe to the maximum dose of 2000 mg/kg body weight. In a subacute toxicity study, the oral administration of IWL did not produce any mortality in the tested animals. The analysis of haematological, liver biochemical, kidney profile, lipid profile, and in vivo antioxidant parameters depicted that all the values were within the control limits after the experimental period and were considered nontoxic to animals. Additionally, the antiulcer study demonstrated a positive response of IWL in a dose-related manner (indomethacin- and ethanol-induced models). Macroscopic analysis showed that pretreatment with I. wightii leaf methanol extract significantly reduced the gastric lesion and decreased the ulceration area (14.52 mm2), demonstrating superior results to the positive control group (27.71 mm2). The histopathological analysis revealed that pretreatment with a high dose of 400 mg/kg of I. wightii leaf methanol extract and positive control group (omeprazole) markedly protected pathological effects, and the gastric mucosa appeared normal. In conclusion, I. wightii has solid nontoxic potential as a promising native herb for an integral therapy for the treatment of ulcers.

9.
Front Pharmacol ; 13: 874474, 2022.
Artículo en Inglés | MEDLINE | ID: mdl-35600869

RESUMEN

Diabetes mellitus is a prevalent metabolic and endocrine illness affecting people all over the world and is of serious health and financial concern. Antidiabetic medicine delivered through pharmacotherapy, including synthetic antidiabetic drugs, are known to have several negative effects. Fortunately, several natural polysaccharides have antidiabetic properties, and the use of these polysaccharides as adjuncts to conventional therapy is becoming more common, particularly in underdeveloped nations. Oxidative stress has a critical role in the development of diabetes mellitus (DM). The review of current literature presented here focusses, therefore, on the antioxidant properties of mushroom polysaccharides used in the management of diabetic complications, and discusses whether these antioxidant properties contribute to the deactivation of the oxidative stress-related signalling pathways, and to the amelioration of ß-cell dysfunction and insulin resistance. In this study, we conducted a systematic review of the relevant information concerning the antioxidant and antidiabetic effects of mushrooms from electronic databases, such as PubMed, Scopus or Google Scholar, for the period 1994 to 2021. In total, 104 different polysaccharides from mushrooms have been found to have antidiabetic effects. Most of the literature on mushroom polysaccharides has demonstrated the beneficial effects of these polysaccharides on reactive oxygen and nitrogen species (RONS) levels. This review discuss the effects of these polysaccharides on hyperglycemia and other alternative antioxidant therapies for diabetic complications through their applications and limits, in order to gain a better understanding of how they can be used to treat DM. Preclinical and phytochemical investigations have found that most of the active polysaccharides extracted from mushrooms have antioxidant activity, reducing oxidative stress and preventing the development of DM. Further research is necessary to confirm whether mushroom polysaccharides can effectively alleviate hyperglycemia, and the mechanisms by which they do this, and to investigate whether these polysaccharides might be utilized as a complementary therapy for the prevention and management of DM in the future.

10.
J Ethnopharmacol ; 293: 115258, 2022 Jul 15.
Artículo en Inglés | MEDLINE | ID: mdl-35378194

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: Tagetes erecta L. (Asteraceae), popularly known as Aztec Marigold, is used in South America to treat several ailments. Despite reports that T. erecta flowers are used in folk medicine to treat gastrointestinal diseases, there is no study regarding its gastric healing effects. AIM OF THE STUDY: The effect of dry extract of T. erecta L. (DETe) in gastric healing and gastric ulcer recurrence was evaluated, contributing to the validation of the antiulcer potential of this medicinal plant. METHODS: Rats were treated orally with vehicle (1 ml/kg), omeprazole (20 mg/kg), or DETe (3, 30 or 300 mg/kg) for 7 days, twice a day. The lesion area was evaluated, and the levels of reduced glutathione (GSH) and lipoperoxides (LOOH) and the activity of the superoxide dismutase (SOD), catalase (CAT), glutathione S-transferase (GST), and myeloperoxidase (MPO) were measured. The ulcer recurrence was evaluated in mice and induced by interleukin (IL)-1ß (1 µg/kg, i.p). The recurred area, gastric wall thickness, GSH and cytokines levels, MPO and N-acetylglucosaminidase (NAG) activities were measured. RESULTS: DETe accelerated the healing of gastric ulcers only at 300 mg/kg, reducing the ulcerated area by 66%. In parallel, DETe reduced LOOH levels, SOD, CAT and MPO activities, while increasing GST activity and mucin amount. In the recurrence model, DETe reduced the lesion area by 94%, and in parallel decreased the gastric wall thickness and TNF levels, while increasing IL-10 amount. CONCLUSIONS: Corroborating the popular use of T. erecta, DETe favors the antioxidant system and reduce gastric inflammation, accelerating the gastric healing process and reducing the ulcer recurrence.


Asunto(s)
Antiulcerosos , Extractos Vegetales , Úlcera Gástrica , Tagetes , Animales , Antiulcerosos/uso terapéutico , Mucosa Gástrica , Luteína/farmacología , Ratones , Fitoterapia , Extractos Vegetales/uso terapéutico , Plantas Medicinales/química , Ratas , Ratas Wistar , Roedores , Úlcera Gástrica/inducido químicamente , Úlcera Gástrica/tratamiento farmacológico , Superóxido Dismutasa , Tagetes/química , Úlcera/tratamiento farmacológico
11.
Artículo en Inglés | MEDLINE | ID: mdl-35295928

RESUMEN

The goal of this study was to identify new compounds from a methanol extract of a polyherbal combination of Aristolochia indica L. and Piper nigrum L. (MECAIPN), two traditional medicinal plants used to cure envenomation, as well as to assess their antioxidant and antivenom properties. MECAIPN yielded EA1 (an essential oil), AA2 (4-(2-oxo-propyl)-cyclopentane-1,3-dione), and W3 ((2,5-dioxo-imidazolidin-4-yl)-urea) (Allantoin). Although EA1 had stronger radical scavenging activity, AA2 had higher DPPH and ferric ion radical scavenging activity, and W3 had higher molybdenum ion radical scavenging activity due to being a single molecule, the binding investigation revealed that EA1 has a greater Stern-Volmer quenching constant (Ksv) than AA2 and W3. Synchronous measurements indicated that EA1, AA2, and W3 bind to tryptophan and tyrosine residues in venom, causing denaturation of the secondary structure of the residue. Finally, the current study concludes that EA1 has more therapeutic antivenom potential, which could be related to the synergism of chemicals found in it. When it came to single compounds, AA2 had stronger antioxidant and antivenom capabilities than W3. To understand the mechanism of action and manufacture the green antivenom medication, more testing of the EA1 and compounds remains required.

12.
J Ethnopharmacol ; 283: 114540, 2022 Jan 30.
Artículo en Inglés | MEDLINE | ID: mdl-34509604

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: Tinospora cordifolia (Willd.) Miers (Menispermaceae) is a Mediterranean herb, used in Ayurvedic, Siddha, Unani, and folk medicines. The herb is also used in conventional medicine to treat oxidative stress-related diseases and conditions, including inflammation, pain, diarrhea, asthma, respiratory infections, cancer, diabetes, and gastrointestinal disorders. AIM OF THE REVIEW: The taxonomy, botanical classification, geographical distribution, and ethnobotanical uses of T. cordifolia, as well as the phytochemical compounds found in the herb, the toxicology of and pharmacological and clinical studies on the effects of T. cordifolia are all covered in this study. MATERIALS AND METHODS: To gather information on T. cordifolia, we used a variety of scientific databases, including Scopus, Google Scholar, PubMed, and Science Direct. The information discussed focuses on biologically active compounds found in T. cordifolia, and common applications and pharmacological activity of the herb, as well as toxicological and clinical studies on its properties. RESULTS: The findings of this study reveal a connection between the use of T. cordifolia in conventional medicine and its antioxidant, anti-inflammatory, antihypertensive, antidiabetic, anticancer, immunomodulatory, and other biological effects. The entire plant, stem, leaves, root, and extracts of T. cordifolia have been shown to have a variety of biological activities, including antioxidant, antimicrobial, antiviral, antiparasitic, antidiabetic, anticancer, anti-inflammatory, analgesic and antipyretic, hepatoprotective, and cardioprotective impact. Toxicological testing demonstrated that this plant may have medicinal applications. T. cordifolia contains a variety of biologically active compounds from various chemical classes, including alkaloids, terpenoids, sitosterols, flavonoids, and phenolic acids. Based on the reports researched for this review, we believe that chemicals in T. cordifolia may activate Nrf2, which leads to the overexpression of antioxidant enzymes such as CAT, GPx, GST, and GR, and thereby induces the adaptive response to oxidative stress. T. cordifolia is also able to reduce NF-κB signalling by inhibiting PI3K/Akt, activating AMPK and sirtuins, and downregulating PI3K/Akt. CONCLUSIONS: Our findings indicate that the pharmacological properties displayed by T. cordifolia back up its conventional uses. Antimicrobial, antiviral, antioxidant, anticancer, anti-inflammatory, antimutagenic, antidiabetic, nephroprotective, gastroprotective, hepatoprotective, and cardioprotective activities were all demonstrated in T. cordifolia stem extracts. To validate pharmacodynamic targets, further research is needed to evaluate the molecular mechanisms of the known compounds against gastrointestinal diseases, inflammatory processes, and microbial infections, as immunostimulants, and in chemotherapy. The T. cordifolia safety profile was confirmed in a toxicological analysis, which prompted pharmacokinetic assessment testing to confirm its bioavailability.


Asunto(s)
Tratamiento Farmacológico de COVID-19 , Medicina Tradicional , Estrés Oxidativo/efectos de los fármacos , Plantas Medicinales , SARS-CoV-2 , Tinospora/química , Humanos , Fitoterapia
13.
ScientificWorldJournal ; 2021: 1424675, 2021.
Artículo en Inglés | MEDLINE | ID: mdl-34504407

RESUMEN

OBJECTIVES: To explore the effective and safe medicines for treating diabetes. METHODS: Hydroalcoholic extracts of 130 medicinal plants belonging to 66 families were evaluated using porcine pancreatic lipase (PPL) inhibition and glucose uptake methods together with a literature review. RESULTS: The extracts of 22 species showed the PPL inhibition activity; 18 extracts of 15 species stimulated glucose uptake in 3T3-L1 adipocytes. Among them, Mansonia gagei J.R. Drumm., Mesua ferrea L., and Centella asiatica (L.) Urb. exhibited both activities. The extracts of Caladium lindenii (André) Madison rhizomes and Azadirachta indica A. Juss. leaves presented the utmost lipase inhibitory activity with IC50 of 6.86 ± 0.25 and 11.46 ± 0.06 µg/mL, respectively. The extracts of Coptis teeta Wall. rhizomes and Croton tiglium L. seeds stimulated the maximum glucose uptake. Ten species are reported to have antidiabetic activity for the first time. Flavonoids and triterpenoids are the dominant antidiabetic compounds in selected medicinal plants from Myanmar. CONCLUSIONS: P. zeylanica, L. cubeba, H. crenulate, M. gagei, C. teeta, and M. ferrea are worthy to advance further study according to their strong antidiabetic activities and limited research on effects in in vivo animal studies, unclear chemical constitutes, and safety.


Asunto(s)
Azadirachta/química , Centella/química , Coptis/química , Croton/química , Hipoglucemiantes/farmacología , Malvaceae/química , Células 3T3-L1 , Animales , Transporte Biológico/efectos de los fármacos , Diabetes Mellitus/tratamiento farmacológico , Diabetes Mellitus/metabolismo , Flavonoides/clasificación , Flavonoides/aislamiento & purificación , Flavonoides/farmacología , Glucosa/metabolismo , Humanos , Hipoglucemiantes/química , Hipoglucemiantes/aislamiento & purificación , Lipasa/antagonistas & inhibidores , Lipasa/aislamiento & purificación , Lipasa/metabolismo , Ratones , Mianmar , Páncreas/química , Páncreas/enzimología , Fitoterapia/métodos , Extractos Vegetales/química , Hojas de la Planta/química , Plantas Medicinales , Rizoma/química , Porcinos , Triterpenos/clasificación , Triterpenos/aislamiento & purificación , Triterpenos/farmacología
14.
J Ethnopharmacol ; 270: 113778, 2021 Apr 24.
Artículo en Inglés | MEDLINE | ID: mdl-33421601

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: Cariniana rubra Gardner ex Miers (Lecythidaceae), is a native and endemic tree in Brazil, whose inner stem bark decoction preparation is used in folk medicine to treat various inflammatory disorders. Previous scientific reports confirmed its popular use as an anti-inflammatory, without, however, evaluating its action mechanisms. AIM: The objective of this study was to determine the cytotoxicity and anti-inflammatory mechanism of action of the methanolic extract of Cariniana rubra (MECr), using experimental models in vivo and in vitro, as well as to identify secondary metabolites present in the extract. MATERIAL AND METHODS: The MECr was prepared by maceration of inner stem bark powder in methanol (1:10 w/v). The in vitro cytotoxicity effect was evaluated in CHO-k1 cells. The Hippocratic screening test was conducted to evaluate the acute toxicity of MECr in mice. The actions of MECr on leukocyte migration, cytokine levels (IL-1ß and TNF-α) and annexin-A1 (AnxA1) expression, were carried out on lambda-type carrageenan air pouch inflammation model in Swiss mice. Additionally, the phytochemical analysis of MECr was carried out by thin-layer chromatography (TLC) and spectrometric mass analysis with electrospray ionization ESI(-)/MS and gas chromatography-mass spectrometry (GC-MS). RESULTS: Treatment of CHO-k1 cells for 24 h with MECr did not cause cytotoxicity (IC50 > 200 µg/mL), however, the MECr was shown to be cytotoxic after 72 h of cell exposure (IC50 = 19.90 ± 3.51 µg/mL). In the Hippocratic test, oral treatment of mice with 750, 1500, or 3000 mg/kg of MECr did not show any histopathological changes and mortality during the 14 days of observation. In the carrageenan air pouch inflammation model, MECr reduced (p < 0.001) polymorphonuclear migration (57.7% and 57.8%), leukocyte monocyte migration (74.5% and 61.8%) in the air pouch cavity and in the skin tissue, respectively. MECr also inhibited TNF-α concentration in the air cavity wash (3.2%, p < 0.01) and increased expression of the AnxA1 protein (26.9%, p < 0.01) in the skin tissue, particularly in neutrophils. ß-sitosterol (1.95%), gallic acid (1.24%), ß-amyrin (0.87%) and stigmasterol (0.66%) were identified as the major constituents in methanolic extract. CONCLUSION: MECr exhibits significant anti-inflammatory action at least by increasing AnxA1 expression and by inhibiting the release of TNF-α pro-inflammatory cytokine and leukocyte migration, which is probably linked to the presence of identified biologically active compounds, especially gallic acid and terpenes. We believe that the results of this study provide a pharmacological basis for the MECr to be considered as a potential therapeutic agent for the treatment of inflammatory diseases.


Asunto(s)
Antiinflamatorios/uso terapéutico , Movimiento Celular/efectos de los fármacos , Lecythidaceae/química , Leucocitos/efectos de los fármacos , Corteza de la Planta/química , Extractos Vegetales/uso terapéutico , Tallos de la Planta/química , Animales , Anexina A1/genética , Anexina A1/metabolismo , Antiinflamatorios/análisis , Antiinflamatorios/química , Brasil , Células CHO , Carragenina/toxicidad , Supervivencia Celular/efectos de los fármacos , Cricetulus , Regulación hacia Abajo/efectos de los fármacos , Inflamación/inducido químicamente , Inflamación/tratamiento farmacológico , Inflamación/metabolismo , Interleucina-1beta/metabolismo , Leucocitos/citología , Leucocitos/metabolismo , Masculino , Metanol/química , Ratones , Extractos Vegetales/análisis , Extractos Vegetales/química , Factor de Necrosis Tumoral alfa/genética , Factor de Necrosis Tumoral alfa/metabolismo , Regulación hacia Arriba/efectos de los fármacos
15.
Nat Prod Res ; 35(23): 5287-5293, 2021 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-32290696

RESUMEN

The hydroethanolic extract obtained from the dry leaves of Fridericia chica (HEFc) underwent several fractionations by different chromatographic techniques. The ethyl acetate and dichloromethane fraction were subjected to phytochemical analysis, resulting in the identification and isolation of scutellarein (1) and in a fraction rich in carajurone (2). They were tested for cytotoxicity in CHO-K1 and the antibacterial activity and mode of action by in vitro assays. The HEFc and scutellarein (1) presented no cytotoxicity. The results showed good antibacterial effect of HEFc against Streptococcus pyogenes and Staphylococcus aureus and moderate activity for Staphylococcus epidermidis, Pseudomonas aeruginosa and Salmonella typhimurium. The fraction containing the compound carajurone (2) showed good activity against Staphylococcus aureus and Staphylococcus epidermidis and moderate activity against Streptococcus pyogenes. Scutellarein (1) showed no activity against the bacteria tested. HEFc antibacterial mode of action appeared to be associated with changes in the permeability of bacterial membranes and nucleotide leakage.


Asunto(s)
Extractos Vegetales , Hojas de la Planta , Antibacterianos/farmacología , Apigenina , Pruebas de Sensibilidad Microbiana , Extractos Vegetales/farmacología
16.
J Ethnopharmacol ; 267: 113499, 2021 Mar 01.
Artículo en Inglés | MEDLINE | ID: mdl-33091486

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: Ethnobotanical studies show that the infusion of the leaves from Copaifera malmei Harms (Fabaceae) has been utilized in the Brazilian traditional medicine to treat provocative and gastrointestinal diseases, among others. Recently, our research team has shown that an infusion extract of the leaves of C. malmei has a strong antiulcer activity and its oral use gives no indications of toxicity. AIM OF THE STUDY: The aim of the study is to evaluate the anti-inflammatory intestinal effect of an infusion extract from the leaves of Copaifera malmei (IECm) in an animal model of ulcerative colitis induced by 2,4,6-trinitrobenzenesulfonic acid (TNBS). MATERIALS AND METHODS: Acute intestinal inflammation was induced in male Wistar rats by TNBS in 20% EtOH (0.25 mL). IECm was administered by oral gavage (for 72, 48, 24 and 2 h) preceding the induction of ulcerative colitis. The colon damage and degree of inflammation were evaluated by morphological observation scores and colon weight. The improved colonic mucosal injury, oxidative stress and inflammatory response were assessed by histopathological investigation and by estimating myeloperoxidase (MPO) activity, malondialdehyde (MDA) and glutathione (GSH) levels and tumor necrosis factor (TNF), interleukin 1ß (IL1-ß), IL-17 and IL-10 colon tissue concentrations. The histopathological changes were done on the colon tissues by hematoxylin and eosin and Periodic Acid-Schiff staining were utilized to measure the mucus. RESULTS: Pre-treatment (25, 100 and 400 mg/kg) with IECm altogether diminished the intestinal inflammation prompted by TNBS in rats by diminishing colonic score by 69.12% (p < 0.01), 19.87% (p < 0.05) and 67.60% (p < 0.01), individually. Improvement of colonic mucosal injury by treatment with IECm was shown by a decline in MPO activity at dosages 25 and 400 mg/kg by 67.98% and 59.68% (p < 0.001), MDA levels 64.80% and 80.00% (p < 0.01) and an expansion in GSH content at all portions (62.53%, 53.38% and 81.20% p < 0.05) compared with vehicle control group. IECm additionally prevention of intestinal inflammation as confirm by decreased cytokine levels, for example, TNF (31.26%, p < 0.05, 50.68% and 45.95%, p < 0.01), IL1-ß (56.41%, 58.83% and 56.65%, p < 0.001), IL-17 (51.66%, p < 0.001, 22.23%, p < 0.05 and 49.67%, p < 0.001) and increased the IL-10 levels at 25 and 400 mg/kg (57.13%, p < 0.01 and 35.83%, p < 0.05) respectively. Histopathological examination of the colon tissue displayed recovery of ulcerative colitis of IECm treated animals by reducing leukocyte infiltrate, epithelial, submucosal and muscular layer damages and maintaining mucus production. CONCLUSION: These findings revealed that IECm was effective and possess anti-colitic activities in a rodent model of UC and can be useful in inflammatory bowel diseases (IBD). The pre-treatment with IECm decreased intestinal inflammation by reducing macroscopical and microscopical colon injury. In addition, the present study demonstrated that IECm ameliorates TNBS-colitis by promoting antioxidant effect, modulation of cytokines release and restauration of mucus production. The study reinforces the traditional use of the Copaifera malmei leaves infusion to inflammatory gastrointestinal disorders and makes IECm a potential herbal medicine for the treatment of IBD.


Asunto(s)
Antiinflamatorios/farmacología , Antioxidantes/farmacología , Colitis Ulcerosa/prevención & control , Colon/efectos de los fármacos , Citocinas/metabolismo , Fabaceae , Mediadores de Inflamación/metabolismo , Moco/metabolismo , Estrés Oxidativo/efectos de los fármacos , Extractos Vegetales/farmacología , Hojas de la Planta , Animales , Antiinflamatorios/aislamiento & purificación , Antioxidantes/aislamiento & purificación , Biomarcadores/metabolismo , Colitis Ulcerosa/inducido químicamente , Colitis Ulcerosa/metabolismo , Colitis Ulcerosa/patología , Colon/metabolismo , Colon/patología , Modelos Animales de Enfermedad , Fabaceae/química , Masculino , Extractos Vegetales/aislamiento & purificación , Hojas de la Planta/química , Ratas Wistar , Transducción de Señal , Ácido Trinitrobencenosulfónico
17.
J Ethnopharmacol ; 269: 113735, 2021 Apr 06.
Artículo en Inglés | MEDLINE | ID: mdl-33359865

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: Dilodendron bipinnatum (Sapindaceae) stem bark decoction and macerate were used to treat uterine inflammation, pain in general, dermatitis and bone fractures. These homemade preparations also have diuretic, stimulant, expectorants and sedative effects and are effective in treating worm infections in the Brazilian Pantanal population. Our previous research confirmed the anti-inflammatory activity of the hydroethanolic extract of inner stem bark of D. bipinnatum (HEDb). AIM: This work aimed to investigate the efficacy of HEDb in ameliorating experimental colitis in rats and to elucidate the possible mechanisms involved in the anti-ulcerative colitis properties of HEDb in rats and Caco-2 cell line. MATERIALS AND METHODS: The effects on cell viability, IL-8 and TNF-α in human colon adenocarcinoma (Caco-2) were determined by flow cytometer and ELISA. Wistar rats (n = 6-7) were orally gavaged with, vehicle (0.9% saline), HEDb at doses of 20, 100 or 500 mg/kg, or mesalazine at a dose of 500 mg/kg, at 48, 24 and 1 h prior to the administration of trinitrobenzene sulfonic acid via rectal administration to induce colitis. The anti-inflammatory effects of HEDb were assessed macroscopically, by myeloperoxidase (MPO) activity and for glutathione (GSH) concentration in the colon. Additionally, colonic histopathological analyses of UC severity were conducted by different staining methods (H&E, PAS and toluidine blue). Pro-inflammatory cytokines TNF-α and IL-1ß were quantified in colonic tissue by ELISA and colonic expressions of COX-2 and IL-17 were analyzed by western blotting. RESULTS: HEDb was shown to be non-cytotoxic with mean viability of 80% in Caco-2 cells. HEDb pre-treatments of 1, 5 or 20 µg/mL significantly reduced TNF-α production in Caco-2 cells by 21.8% (p < 0.05), 60.5 and 82.1% (p < 0.001) respectively following LPS treatment compared to LPS alone. However, no change in IL-8 production was observed. HEDb pre-treatment of rats subjected to TNBS significantly (p < 0.001) reduced colonic lesion score. Higher doses (100 and 500 mg/kg) caused a sharp downregulation of haemorrhagic damage, leukocyte infiltration, edema and restoration of mucus production. Moreover, mast cell degranulation was inhibited. Colonic MPO activity was reduced following all doses of HEDb, reaching 51.1% ± 1.51 (p < 0.05) with the highest dose. GSH concentration was restored by 58% and 70% following 100 and 500 mg/kg of HEDb, respectively. The oral treatment of HEDb at doses 20, 100 and 500 mg/kg decreased the concentrations of TNF-α and IL-1ß at all doses in comparison to vehicle treated control. In addition, HEDb inhibited the COX-2 and IL-17 expressions with maximal effect at 500 mg/kg (60.3% and 65% respectively; p < 0.001). In all trials, the effect of HEDb at all doses being 20, 100 and 500 mg/kg was statistically comparable to mesalazine (500 mg/kg). CONCLUSIONS: HEDb reduces colonic damage in the TNBS colitis model and relieves oxidative and inflammatory events, at least in part, by increasing mucus production, reducing leukocyte migration and reducing TNF-α (in vivo and in vitro), IL-1ß, IL-17 and COX-2 expression. Therefore, HEDb requires further investigation as a candidate for treating IBD.


Asunto(s)
Antioxidantes/farmacología , Colitis Ulcerosa/prevención & control , Moco/metabolismo , Corteza de la Planta/química , Extractos Vegetales/farmacología , Sapindaceae/química , Animales , Antioxidantes/química , Antioxidantes/uso terapéutico , Brasil , Células CACO-2 , Supervivencia Celular/efectos de los fármacos , Colitis Ulcerosa/inducido químicamente , Colitis Ulcerosa/patología , Ciclooxigenasa 2/metabolismo , Modelos Animales de Enfermedad , Edema/inducido químicamente , Edema/prevención & control , Glutatión/metabolismo , Humanos , Interleucina-17/metabolismo , Interleucina-1beta/metabolismo , Interleucina-8/metabolismo , Lipopolisacáridos/toxicidad , Mastocitos/efectos de los fármacos , Peroxidasa/metabolismo , Extractos Vegetales/química , Extractos Vegetales/uso terapéutico , Ratas Wistar , Ácido Trinitrobencenosulfónico/toxicidad , Factor de Necrosis Tumoral alfa/metabolismo
18.
J Ethnopharmacol ; 254: 112707, 2020 May 23.
Artículo en Inglés | MEDLINE | ID: mdl-32112897

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: Piper umbellatum L. leaves, commonly found in the Amazon, Cerrado and Atlantic rain forest regions of Brazil, are widely used as a traditional medicine to treat gastrointestinal disorders and inflammation, among others diseases. Also, previous scientific studies demonstrated that P. umbellatum has gastroprotective and anti-inflammatory activity. AIM: To investigate the phytochemical profiles and the intestinal anti-inflammatory effect of the hydroethanolic extract of P. umbellatum (HEPu) leaf on ulcerative colitis in rats. MATERIALS AND METHODS: In this study, the chemical composition of HEPu was analyzed by gas chromatography-mass spectrometry (GC-MS) and liquid chromatography coupled to mass spectrometry (LC/MS). Also, this work studied the effects of HEPu on ulcerative colitis induced by 2,4,6-trinitrobenzene sulfonic acid (TNBS, 30 mg/mL in 20% ethanol) by intrarectal administration in rats. Simultaneously, animals were pre-treated orally with HEPu (30, 100 and 300 mg/kg), mesalazine (500 mg/kg), or vehicle. At the end of the experimental period, clinical signs of ulcerative colitis were evaluated by determination of weight loss, gross appearance, ulcer area and histological changes. Reduced glutathione (GSH), lipoperoxides (MDA) and nitric oxide (NO) levels, and superoxide dismutase (SOD), myeloperoxidase (MPO) and catalase (CAT) activities were determined in colon tissues. Also, pro-inflammatory mediators such as tumor necrosis factor alpha (TNF-α) and interleukin 1 beta (IL- 1ß) were quantified by immunoassay on the surface of fluorescent-coded magnetic beads (Luminex MagPix System). RESULTS: GC-MS analysis showed the presence of 17 different phytochemical compounds in the HEPu. LC/MS analyses revealed the presence of compounds in HEPu as protocatechuic acid, ferulic acid, kaempferol, rosmarinic acid, apigenin and ursolic acid. Treatment with HEPu significantly ameliorated weight loss, macroscopic damage, ulcerated area and histopathological changes such as sub-mucosal edema, cell infiltration, ulceration and necrosis (p < 0.001). Furthermore, HEPu (30, 100, and 300 mg/kg, p.o) inhibited the levels of oxidative parameters, such as MPO (49%, 53%, and 62%, p < 0.001), NO (20%, 19%, 22%, p < 0.01), and MDA (75%, 83%, 70%, p < 0.001), whereas increased the antioxidant activities such as SOD (208%, 192%, 64%, p < 0.001), GSH (94%, 75%, 49%, p < 0.01), and CAT (92%, 69%, 108%, p < 0.01). The extract also inhibited the pro-inflammatory cytokines TNF-α (81%, 85%, 85%, p < 0.001) and IL-1ß (95%, 79%, 89%, p < 0.001) levels. CONCLUSION: Together, these results revealed that P. umbellatum L. is a promising source of metabolites to be used in the treatment of inflammatory bowel disease.


Asunto(s)
Antiinflamatorios/uso terapéutico , Antioxidantes/uso terapéutico , Colitis Ulcerosa/tratamiento farmacológico , Piper , Extractos Vegetales/uso terapéutico , Animales , Antiinflamatorios/química , Antiinflamatorios/farmacología , Antioxidantes/química , Antioxidantes/farmacología , Catalasa/metabolismo , Colitis Ulcerosa/inducido químicamente , Colitis Ulcerosa/metabolismo , Colitis Ulcerosa/patología , Colon/efectos de los fármacos , Colon/metabolismo , Colon/patología , Citocinas/metabolismo , Femenino , Malondialdehído/metabolismo , Óxido Nítrico/metabolismo , Fitoquímicos/análisis , Fitoquímicos/farmacología , Fitoquímicos/uso terapéutico , Extractos Vegetales/química , Extractos Vegetales/farmacología , Hojas de la Planta , Ratas Wistar , Superóxido Dismutasa/metabolismo , Ácido Trinitrobencenosulfónico
19.
J Ethnopharmacol ; 248: 112307, 2020 Feb 10.
Artículo en Inglés | MEDLINE | ID: mdl-31629026

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: Sorocea guilleminina Gaudich. is a tree or shrub endemic to Brazil. Its leaves are used in Brazilian folk medicine for the healing of wounds, stomach problems, inflammation and as diuretic. The present study evaluates the activity and action mechanisms of the healing properties of the aqueous extract of S. guilleminiana leaves (AESg), in experimental models in vivo and in vitro, as well as performs a phytochemical analysis of the extract. MATERIALS AND METHODS: The AESg was prepared by infusion: Ten g of dry leaves powder in 1 L hot water, soaked for 15 min, filtered, lyophilized, and stored at -30 °C. Phytochemical analyses were realized by colorimetry and HPLC/ESI/MS. Its' in vitro cytotoxicity was evaluated on fibroblastic N3T3 cells. The potential of the wound healing activity in vivo was evaluated using excision and incision wound rat models, by histopathology of the injured skin along with the determination of nitric oxide, cytokines (IL-1ß, IL-10, and TNF-α), and antioxidant parameters (GSH, MPO and CAT). In vitro wound healing activity was also demonstrated in scratched N3T3 cells, by measuring the proliferation/migration rate. RESULTS: The phytochemical analysis of the AESg revealed a strong presence of polar compounds, especially flavonoids (4 majoritarian), as well as terpenes and/or sterols (2 majoritarian). The AESg showed no toxicity in the N3T3 cell line (IC50 > 800 µg/mL). Topical treatment with the AESg showed an increase (p < 0.05) in wound contraction with 2 mg/g cream on days 5 and 9 (43.56% and 6.70% increase, respectively), and with 50 mg/g on days 7 and 9 (10.88% and 7.91%, respectively), compared to the vehicle (non-ionic neutral cream). Topical application of AESg (2 or 50 mg/g non-ionic cream) in incised wounds caused an increase in the force necessary for the rupture of the wound when compared to the vehicle group. No changes in cytokines (IL-1ß, IL-10, or TNF-α) or NO accumulation was found with up to 50 mg/g AESg treatment. For antioxidant activity on the incision wound, an increase in GSH levels was denoted with the AESg use, at the lowest and highest dose (2 and 50 mg/g) by 75.86% and 61.20% respectively, when compared to the vehicle. Also, the CAT activity was accentuated by AESg at the highest dose (50 mg/g) by 85.87%. Finally, the AESg at all doses attenuated MPO activity significantly in the incision wound by 71.35%, 73.21%, 78.08%, respectively. In the scratch test on N3T3 cells, the treatment with AESg resulted also in an increase in fibroblast proliferation/migration rate, compared to the vehicle. CONCLUSION: AESg is not cytotoxic. The results confirm the popular use of the leaf infusion of S. guilleminiana for the treatment of cutaneous wounds, possibly by stimulating the proliferation of fibroblasts with a consequent deposition of collagen, fastening rearrangement of collagen fibers, and greater transformation into myofibroblasts, essential in the healing process. Preliminary chemical analyzes of AESg revealed the presence mainly of phenolic compounds, being salicylic acid, gallic acid, pinocembrin and isoquercitrin the majoritarian ones.


Asunto(s)
Moraceae , Extractos Vegetales/farmacología , Hojas de la Planta , Piel/efectos de los fármacos , Cicatrización de Heridas/efectos de los fármacos , Heridas Penetrantes/tratamiento farmacológico , Animales , Movimiento Celular/efectos de los fármacos , Proliferación Celular/efectos de los fármacos , Citocinas/metabolismo , Modelos Animales de Enfermedad , Ratones , Moraceae/química , Células 3T3 NIH , Óxido Nítrico/metabolismo , Extractos Vegetales/aislamiento & purificación , Extractos Vegetales/toxicidad , Hojas de la Planta/química , Ratas Wistar , Repitelización/efectos de los fármacos , Piel/lesiones , Piel/metabolismo , Piel/patología , Heridas Penetrantes/metabolismo , Heridas Penetrantes/patología
20.
J Ethnopharmacol ; 233: 101-114, 2019 Apr 06.
Artículo en Inglés | MEDLINE | ID: mdl-30611907

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: Cochlospermum regium (Bixaceae) is a native shrub of Brazil and its xylopodium (infusion/decoction) is being used for the treatment of gastritis, ulcers, arthritis, intestinal infections, gynaecological infections, skin diseases, among others. The aim of the present study was to evaluate the gastroprotective/antiulcer activity and the mechanism of action of hydroethanolic extract of C. regium xylopodium (HECr), using in vitro and in vivo models. Additionally, phytochemical constituents were identified by high-performance liquid chromatography (HPLC). MATERIALS AND METHODS: C. regium xylopodium was macerated with ethanol/water to obtain the HECr. The phytochemical characterisation was carried out by HPLC. The antiulcer efficacy of HECr (25, 100 and 400 mg/kg, p.o.) was evaluated using acute acidified ethanol (HCl/EtOH), piroxicam and water immersion-induced experimental ulcer models. Chronic gastric ulcer healing activity of HECr was evaluated through acetic acid (99.8%) - induced model. Histological analysis and myeloperoxidase (MPO), glutathione (GSH), catalase (CAT) activities were also evaluated in chronic ulcer induced gastric tissues. The plausible mode of action of the HECr was assessed by estimation of gastric wall mucus production and the role of gastric secretion in pylorus ligature. The animals were also pre-treated with various inhibitors which includes indomethacin (10 mg/kg, p.o.) a selective inhibitor of cyclooxygenase, L-NAME (10 mg/kg, i.p.), an inhibitor of nitric oxide synthase, glibenclamide, a ATP-sensitive potassium channels (K+ATP) blocker (5 mg/kg, p.o.) or yohimbine (2 mg/kg, i.p.), an α2-adrenergic receptor antagonist. In vitro, Helicobacter pylori action was done by broth microdilution method. RESULTS: The HPLC analysis data revealed the presence of gallic acid, rutin, myricetin, morin and kaempferol. HECr promoted protective effect against acute ulcers induced by HCl/EtOH with inhibitions of 47.52% (p < 0.01) and 62.69% (p < 0.001) at 100 and 400 mg/kg, and in piroxicam by 34.11% (p < 0.05), 49.14% (p < 0.01) and 61.34% (p < 0.001), at 25, 100 or 400 mg/kg, respectively, and in water restraint stress by 78.26% inhibition, p < 0.001, at the dose of 400 mg/kg when compared to the vehicle control group respectively. In the chronic gastric ulcer model, HECr (25, 100 and 400 mg/kg p.o.) significantly (p < 0.001) decreased the injured area by 58.80%, 77.87% and 71.10% respectively. Histological examination indicated that oral treatment of HECr promoted healing of gastric lesions by regenerating gastric mucosa layer with less inflammatory cells. HECr augmented the GSH, CAT activities and reduced MPO level. The pre-treatment with HECr increased the gastric wall mucus production. It also significantly altered the gastric secretion parameters by causing the reduction in the gastric juice volume, elevated the pH level and reduced the total acidity at all doses tested when compared with the vehicle group. HECr at the most active dose (100 mg/kg) reversed completely the reduction of PGs, NO production, closure of K+ATP- channels and α2-adrenoreceptor blockage - induced damages. In microdilution assay, the HECr showed good anti-Helicobacter pylori effect with MIC = 100 µg/mL. CONCLUSION: The HECr presented preventive and curative effects in the experimental gastric ulcer models, besides good anti-Helicobacter pylori activity, which supports the traditional medicinal use of the xylopodium of this plant for gastrointestinal diseases. The underlying mechanisms of this antiulcerogenic/antiulcer action involve, at least, augmentation of mucus production, inhibition of gastric secretion, stimulation of PGs and NO synthesis. And that it involves activation of K+ATP channels and α-2-adrenergic receptors, in addition to an antioxidant activity, probably due to the presence of gallic acid and flavonoids in HECr.


Asunto(s)
Antiulcerosos/uso terapéutico , Bixaceae , Extractos Vegetales/uso terapéutico , Úlcera Gástrica/tratamiento farmacológico , Ácido Acético , Animales , Antiinflamatorios no Esteroideos , Antiulcerosos/farmacología , Modelos Animales de Enfermedad , Etanol , Femenino , Mucosa Gástrica/efectos de los fármacos , Mucosa Gástrica/metabolismo , Mucosa Gástrica/patología , Helicobacter pylori/efectos de los fármacos , Masculino , Ratones , Fitoterapia , Piroxicam , Extractos Vegetales/farmacología , Ratas Wistar , Úlcera Gástrica/inducido químicamente , Úlcera Gástrica/metabolismo , Úlcera Gástrica/patología , Estrés Fisiológico
SELECCIÓN DE REFERENCIAS
DETALLE DE LA BÚSQUEDA