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1.
J Toxicol Environ Health A ; 87(14): 592-603, 2024 Jul 17.
Artículo en Inglés | MEDLINE | ID: mdl-38712866

RESUMEN

Punica granatum, popularly known as pomegranate, is a fruit tree with wide worldwide distribution, containing numerous phytochemicals of great medicinal value. The aim of the present study was to determine the phytochemical profile and antioxidant potential of a protein fraction (PF) derived from P. granatum sarcotesta which is rich in lectin. In addition, the acute oral toxicity, genotoxicity and antigenotoxicity of this protein fraction (PF) from P. granatum sarcotesta was measured. The phytochemical profile of PF was determined using HPLC. The in vitro antioxidant effect was assessed using the methods of total antioxidant capacity (TAC) and DPPH and ABTS+ radical scavenging. Acute oral toxicity was determined in female Swiss mice administered a single dose of 2000 mg/kg. This PF was examined for genotoxicity and antigenotoxicity at doses of 500, 1000 and 2000 mg/kg, utilizing mouse peripheral blood cells. Phytochemical characterization detected a high content of ellagic acid and antioxidant capacity similar to that of ascorbic acid (positive control). PF was not toxic (LD50 >2000 mg/kg) and did not exert a genotoxic effect in mice. PF protected the DNA of peripheral blood cells against damage induced by cyclophosphamide. In conclusion, this PF fraction exhibited significant antioxidant activity without initiating toxic or genotoxic responses in mice.


Asunto(s)
Antioxidantes , Extractos Vegetales , Granada (Fruta) , Animales , Ratones , Antioxidantes/farmacología , Femenino , Extractos Vegetales/toxicidad , Extractos Vegetales/química , Extractos Vegetales/farmacología , Granada (Fruta)/química , Lectinas/toxicidad , Pruebas de Mutagenicidad , Daño del ADN/efectos de los fármacos , Pruebas de Toxicidad Aguda
2.
J Toxicol Environ Health A ; 87(16): 662-673, 2024 Aug 17.
Artículo en Inglés | MEDLINE | ID: mdl-38808737

RESUMEN

Pseudobombax marginatum, popularly known as "embiratanha," is widely used by traditional communities as anti-inflammatory and analgesic agent. This study aimed to determine the phytochemical profile as well as cytotoxicity, acute oral toxicity, genotoxicity, and mutagenicity attributed to exposure to aqueous (AqEx) and ethanolic (EtEx) extracts of embiratanha bark. Phytochemical screening was conducted using thin-layer chromatography (TLC). Cell viability was analyzed using MTT assay with human mammary gland adenocarcinoma (MDA-MB-231) and macrophage (J774A.1) cell lines, exposed to concentrations of 12.5, 25, 50, or 100 µg/ml of either extract. For acute oral toxicity, comet assay and micronucleus (MN) tests, a single dose of 2,000 mg/kg of either extract was administered orally to Wistar rats. TLC analysis identified classes of metabolites in the extracts, including cinnamic acid derivatives, flavonoids, hydrolyzable tannins, condensed tannins, coumarins, and terpenes/steroids. In the cytotoxicity assay, the varying concentrations of extracts derived from embiratanha induced no significant alterations in the viability of MDA-MB-231 cells. The lowest concentration of EtEx significantly increased macrophage J774A.1 viability. However, the higher concentrations of AqEx markedly lowered macrophage J774A.1 viability. Animals exhibited no toxicity in the parameters analyzed in acute oral toxicity, comet assay, and MN tests. Further, EtEx promoted a significant reduction in DNA damage index and DNA damage frequency utilizing the comet assay, while the group treated with AqEx exhibited no marked differences. Thus, data demonstrated that AqEx or EtEx of embiratanha may be considered safe at a dose of 2,000 mg/kg orgally under our experimental conditions tested.


Asunto(s)
Extractos Vegetales , Ratas Wistar , Extractos Vegetales/toxicidad , Extractos Vegetales/química , Animales , Humanos , Ratas , Línea Celular Tumoral , Masculino , Ensayo Cometa , Pruebas de Micronúcleos , Femenino , Supervivencia Celular/efectos de los fármacos , Fitoquímicos/toxicidad , Fitoquímicos/análisis , Ratones , Corteza de la Planta/química , Mutágenos/toxicidad , Pruebas de Mutagenicidad , Etanol/química
3.
Inflammopharmacology ; 32(1): 595-602, 2024 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-37823930

RESUMEN

Wounds encompass physical, chemical, biological, induced damages to the skin or mucous membranes. In wound treatment, combating infections is a critical challenge due to their potential to impede recovery and inflict systemic harm on patients. Previously, the essential oil extracted from Psidium glaziovianum (PgEO) demonstrated antinociceptive and anti-inflammatory attributes, along with negligible oral toxicity. Hence, our study aimed to assess the effects of topically applying a gel formulation containing PgEO to excisional wounds in mice. Additionally, an in vitro antimicrobial assessment was conducted. The formulated gel underwent characterization and toxicological evaluation on erythrocytes, as well as a dermal irritation test. Its antimicrobial activity was tested against both gram-positive and gram-negative bacteria, as well as fungi. Subsequently, an assessment of its efficacy in excisional wound healing was conducted in mice. The findings of this investigation highlight the gel's efficacy against both gram-positive and gram-negative bacteria, as well as fungi. Moreover, this study underscores that the PgEO-gel treatment enhances skin wound healing, potentially due to its capacity to trigger antioxidant enzymes and suppress pro-inflammatory cytokines. Furthermore, the gel exhibited minimal toxicity to erythrocytes and skin irritation. These findings hold promise for prospective preclinical and clinical trials across diverse wound types. In conclusion, this study sheds light on the potential therapeutic applications of the gel formulation containing essential oil from P. glaziovianum in the context of wound healing.


Asunto(s)
Aceites Volátiles , Psidium , Humanos , Animales , Ratones , Antibacterianos , Estudios Prospectivos , Bacterias Gramnegativas , Bacterias Grampositivas , Cicatrización de Heridas , Aceites Volátiles/farmacología
4.
J Toxicol Environ Health A ; 86(16): 557-574, 2023 08 18.
Artículo en Inglés | MEDLINE | ID: mdl-37350297

RESUMEN

This study aimed to characterize the phytochemical profile of bark and leaves aqueous extract Commiphora leptophloeos, and conduct in vivo and in vitro assays to determine the presence of any toxicological consequences due to exposure. The phytochemical analysis was carried out using high-performance liquid chromatography (HPLC). The antioxidant activity was estimated utilizing DPPH free radical scavenging and phosphomolybdenum assays. Cell viability was measured by the MTT method on J774 and human adenocarcinoma cells, which were treated with concentrations of 12,5, 25, 50, 100 or 200 µg/ml of both extracts. Acute oral toxicity, genotoxicity, and mutagenicity assays were determined using a single oral dose of 2000 g/kg in male Swiss albino mice (Mus musculus). Biochemical analysis of the blood and histological analyses of the kidneys, liver, spleen, pylorus, duodenum and jejunum were undertaken. Genotoxicity and mutagenicity were determined utilizing blood samples. Gallic acid, catechin, and epicatechin were identified in the bark and chlorogenic acid in leaves. Data demonstrated a high content of phenolic compounds and flavonoids associated with significant antioxidant potential. No significant signs in damage or symptoms of toxicity were detected. No marked reduction in cell viability was found at lower concentrations tested. On histomorphometry, only the gastrointestinal organs exhibited significant difference. Renal hepatic and blood parameters were within the normal range. No apparent signs of toxicity, genotoxicity, mutagenicity or cytotoxicity were found in vivo and in vitro experiments.


Asunto(s)
Antioxidantes , Catequina , Ratones , Animales , Masculino , Humanos , Antioxidantes/química , Extractos Vegetales/toxicidad , Extractos Vegetales/química , Commiphora , Corteza de la Planta/química , Fitoquímicos/toxicidad , Hojas de la Planta/química
5.
Inflammopharmacology ; 31(6): 3143-3151, 2023 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-37498376

RESUMEN

Myrciaria floribunda is a plant that is distributed across different Brazilian biomes such as the Amazon, Caatinga, Cerrado, and Atlantic Forest, and it possesses antioxidant, antimicrobial, and anticancer properties. The antinociceptive and anti-inflammatory properties of the essential oil from M. floribunda leaves (MfEO) were examined in this study using mouse models. Gas chromatography-mass spectrometry was employed to describe the oil, and the results revealed that δ-cadinene, bicyclogermacrene, α-cadinol, and epi-α-muurolol predominated in the chemical profile. The oil stimulated a decrease in nociception in the chemical and thermal models used to evaluate acute antinociceptive activity. Findings from the use of pain pathway blockers to study the presumed underlying mechanism indicated opioid pathway activity. The anti-edematogenic effect, decreased cell migration, and generation of pro-inflammatory cytokines provided evidence of the anti-inflammatory potential of the essential oil from M. floribunda. According to this research, the essential oil from M. floribunda can effectively alleviate acute pain and inflammation.


Asunto(s)
Antiinfecciosos , Aceites Volátiles , Ratones , Animales , Aceites Volátiles/farmacología , Antiinflamatorios/farmacología , Antiinflamatorios/química , Antioxidantes/farmacología , Antiinfecciosos/farmacología , Extractos Vegetales/química , Analgésicos/farmacología , Analgésicos/química , Hojas de la Planta/química
6.
Chem Biodivers ; 19(9): e202200034, 2022 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-35864035

RESUMEN

The purpose of this study was to analyses the influence of seasonal variation on the chemical composition and antimicrobial, antioxidant and cytotoxicity activities of the essential oil (EO) extracted from the leaves of Eugenia pohliana. Chemical characterization of the samples - by gas chromatography-mass spectrometry - found 35 and 38 components for summer and winter, respectively, of the EO from E. pohliana leaves, totaling 47 different compounds. Analysis of antioxidant capacity (DPPH, ABTS and TAC) revealed that the summer EO showed greater free radical scavenging capacity than the winter. Similarly, the summer EO exhibited superior antimicrobial potential (MIC=128-512 µg/mL and MMC=128-1024 µg/mL, compared to the winter EO (128-2048 µg/mL and 256-2048 µg/mL, respectively). Results showed that both oils had a low potential to cause hemolysis. This study provides new scientific evidence on the influence of seasonality on the pharmacological properties of E. pohliana leaves and its potential for the development of herbal medicines.


Asunto(s)
Antiinfecciosos , Eugenia , Aceites Volátiles , Antibacterianos/farmacología , Antiinfecciosos/farmacología , Antioxidantes/química , Radicales Libres , Pruebas de Sensibilidad Microbiana , Aceites Volátiles/química , Hojas de la Planta/química , Estaciones del Año
7.
Inflammopharmacology ; 30(2): 599-607, 2022 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-35257283

RESUMEN

Plants of the genus Psidium have been employed in "in natura" consumption and agroindustry, and owing to the diversity of phytochemicals, the development of new pharmaceutical forms has received remarkable research interest. In this study, the essential oil obtained from Psidium glaziovianum (PgEO) leaves were evaluated antinociceptive and anti-inflammatory activities were evaluated in mouse models. Initially, PgEO was characterized by gas chromatography-mass spectrometry and gas chromatography with flame ionization detection, and the profile was dominated by sesquiterpene compounds. In the evaluation of acute antinociceptive activity (abdominal contortions induced by acetic acid, formalin, tail immersion, and hot plate tests), PgEO promoted a reduction in nociception in the chemical and thermal models. Additionally, the potential underlying mechanism was investigated using pain pathway blockers, and the results revealed a combined action of opioidergic and muscarinic pathways. The anti-inflammatory potential was confirmed by anti-edematogenic action, reduced cell migration, pro-inflammatory cytokine production, and granuloma formation in chronic processes. This study provides evidence that PgEO can be effective for the treatment of pain and acute and chronic inflammation.


Asunto(s)
Aceites Volátiles , Psidium , Administración Oral , Analgésicos , Animales , Edema/inducido químicamente , Edema/tratamiento farmacológico , Inflamación/tratamiento farmacológico , Ratones , Aceites Volátiles/farmacología , Dolor/tratamiento farmacológico , Extractos Vegetales , Hojas de la Planta/química , Psidium/química
8.
Inflammopharmacology ; 30(6): 2273-2284, 2022 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-36094726

RESUMEN

Eugenia pohliana DC.(Myrtaceae) is used in folk medicine by communities in Brazil. However, there are no reports on its biological activity. This is the first study to identify the components of E. pohliana essential oil (EpEO) and evaluate their antinociceptive and anti-inflammatory activities in an in vivo model at doses of 25, 50, and 100 mg/kg. The essential oil (EO) was obtained by hydrodistillation, and the analysis was performed by gas chromatography coupled with mass spectrometry. Antinociceptive activity was evaluated by writhing tests, tail movement, and formalin (neurogenic and inflammatory pain); naloxone was used to determine the nociception mechanism. Anti-inflammatory activity was assessed by oedema and peritonitis tests. We found that (E)-ß-caryophyllene (BCP) (15.56%), δ-cadinene (11.24%) and α-cadinol (10.89%) were the major components. In the writhing test, there was a decrease in writing by 42.95-70.70%, in the tail movement, an increase in latency time by 69.12-86.63%, and in the formalin test, there was a reduction in pain neurogenic by 29.54-61.74%, and inflammatory pain by 37.42-64.87%. The antinociceptive effect of EpEO occurs through the activation of opioid receptors. In addition, a reduction in inflammation by 74.93‒81.41% was observed in the paw edema test and inhibition of the influx of leukocytes by 51.86‒70.38% and neutrophils by 37.74‒54.72% in the peritonitis test. It was concluded that EpEO has antinociceptive effect by the opioid pathway, as shown by the inhibitory effect of naloxone, and anti-inflammatory actions, and that its use does not cause hemolytic damage or behavioral change.


Asunto(s)
Eugenia , Myrtaceae , Aceites Volátiles , Peritonitis , Ratones , Animales , Eugenia/química , Aceites Volátiles/farmacología , Aceites Volátiles/uso terapéutico , Nocicepción , Analgésicos/uso terapéutico , Antiinflamatorios/uso terapéutico , Edema/inducido químicamente , Edema/tratamiento farmacológico , Dolor/tratamiento farmacológico , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico , Inflamación/tratamiento farmacológico , Peritonitis/tratamiento farmacológico , Naloxona/uso terapéutico
9.
Arch Microbiol ; 203(7): 4303-4311, 2021 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-34110480

RESUMEN

The aim of this study was to evaluate the antioxidant, antibacterial, and antibiofilm activities of nerolidol. The antioxidant activity of nerolidol was determined using the total antioxidant activity method. Antibacterial activity was performed using the microdilution method to determine the minimum inhibitory concentration (MIC) against seven standard strains of the ATCC and four bacterial clinical isolates with a resistance profile, following the Clinical and Laboratory Standards Institute (CLSI). The antibiofilm activity of nerolidol was performed using the crystal violet method. The results of the antioxidant test revealed a total antioxidant activity of 93.94%. Nerolidol inhibited the growth of Staphylococcus aureus (MIC = 1 mg/mL), Streptococcus mutans (MIC = 4 mg/mL), Pseudomonas aeruginosa (MIC = 0.5 mg/mL), and Klebsiella pneumoniae (MIC = 0.5 mg/mL). For clinical isolates, nerolidol showed an inhibitory potential against multidrug-resistant P. aeruginosa, K. pneumoniae carbapenemase (MIC = 0.5 mg/mL), methicillin-susceptible S. aureus (MIC = 2 mg/mL), and methicillin-resistant S. aureus (MIC = 2 mg/mL). Nerolidol showed similar antibacterial activity against ATCC strains and hospital clinical isolates with resistance profile, suggesting that even though these strains are resistant to antibiotics, they are still sensitive to nerolidol. Nerolidol exerted a dose-dependent effect on the inhibition of biofilm formation, even at subinhibitory concentrations. Nerolidol inhibited bacterial biofilms of ATCC strains at a rate ranging from 51 to 98%, at concentrations ranging from 0.5 to 4 mg/mL. For clinical bacterial isolates, biofilm inhibition ranged from 6 to 60%. Therefore, the present study showed the antioxidant, antibacterial, and antibiofilm properties of nerolidol.


Asunto(s)
Bacterias , Biopelículas , Sesquiterpenos , Antibacterianos/farmacología , Antioxidantes/farmacología , Bacterias/efectos de los fármacos , Biopelículas/efectos de los fármacos , Farmacorresistencia Bacteriana/efectos de los fármacos , Pruebas de Sensibilidad Microbiana , Sesquiterpenos/farmacología
10.
Pestic Biochem Physiol ; 177: 104901, 2021 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-34301362

RESUMEN

Lippia alba is an aromatic shrub known to produce a diversity of essential oils, which can be classified into chemotypes. This study reports on the insecticidal activity of essential oil from L. alba leaves collected at Caatinga and its major compound against termite Nasutitermes corniger and maize weevil Sitophilus zeamais. The chromatographic analysis revealed the presence of 19 compounds, with 1,8-cineole being the most common (70.01%). When ingested, the oil promoted the mortality of N. corniger (LC50: 18.25 and 8.4 nL/g for workers and soldiers, respectively). The compound 1,8-cineole was also termiticidal for workers (LC50: 13.7 nL/g). The oil inhibited the activity of N. corniger exoglucanase, xylanase, and proteases. Toxicity by ingestion to S. zeamais was detected for the oil (LC50: 0.297 µL/g) but not for 1,8-cineole; however, both the oil and 1,8-cineole showed anti-nutritional effects. Fumigant effects of the oil and 1,8-cineole against S. zeamais (LC50 of 78.0 and 13.64 µL/L in air, respectively) were detected. This is the first record of a chemotype VI oil from L. alba collected at Caatinga and the first report of the insecticidal activity of a chemotype VI oil. Our study demonstrates that essential oil from L. alba and 1,8 cineole have the potential for the development of natural insecticides.


Asunto(s)
Insecticidas , Isópteros , Lippia , Aceites Volátiles , Gorgojos , Animales , Eucaliptol , Insecticidas/farmacología , Aceites Volátiles/farmacología , Hojas de la Planta
11.
Chem Biodivers ; 17(10): e2000575, 2020 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-32894822

RESUMEN

The Croton argyrophyllus leaf essential oil has anti-inflammatory, antioxidant, cytotoxic among other activities. However, there are chemical composition variations in the literature. This work reports the first study of the intraspecific chemical variation of C. argyrophyllus population from Pernambuco state, Brazil. The essential oils of nine specimens (OCA1 to OCA9) were analyzed by GC/MS and NIR to identify the chemical compositions and to verify the similarities between the analyzed samples. These analyses resulted in the identification of bicyclogermacrene (mean 38.42 %), (Z)-caryophyllene (mean of 14.06 %), epi-longipinanol (mean of 9.78 %) and germacrene B (mean of 9.1 %) as the major constituents, as well as the same chemical markers for all oil samples. However, these are different to those that were previously registered in the literature for C. argyrophyllus essential oil. The data obtained from the analysis by NIR spectroscopy were treated by PCA and HCA and showed similarities in the chemical samples' profile. By statistical analyses three clusters were obtained: OCA1-6, OCA7-8 and OCA9. All these groups were potentially active against Staphylococcus aureus. However, the OCA7-8 group was the most active.


Asunto(s)
Antibacterianos/farmacología , Croton/química , Aceites Volátiles/farmacología , Hojas de la Planta/química , Staphylococcus aureus/efectos de los fármacos , Antibacterianos/química , Antibacterianos/aislamiento & purificación , Brasil , Pruebas de Sensibilidad Microbiana , Aceites Volátiles/química , Aceites Volátiles/aislamiento & purificación
12.
Molecules ; 25(17)2020 Aug 23.
Artículo en Inglés | MEDLINE | ID: mdl-32842529

RESUMEN

Caesalpinia ferrea C. Mart., popularly known as "Jucá" or "Pau-ferro", belongs to the Fabaceae family, and is classified as a native and endemic species in Brazil. Numerous studies that portray its ethnobotany, chemical composition, and biological activities exist in the literature. The present study aimed to systematically review publications addressing the botanical aspects, uses in popular medicine, phytochemical composition, and bioactivities of C. ferrea. The searches focused on publications from 2015 to March 2020 using the Scopus, Periódicos Capes, PubMed, Google Scholar, and ScienceDirect databases. The leaves, fruits, seeds, and bark from C. ferrea are used in popular medicine to treat disorders affecting several systems, including the circulatory, immune, cardiovascular, digestive, respiratory, genitourinary, musculoskeletal, and conjunctive systems. The most commonly found chemical classes in phytochemical studies are flavonoids, polyphenols, terpenoids, tannins, saponins, steroids, and other phenolic compounds. The biological properties of the extracts and isolated compounds of C. ferrea most cited in the literature were antibacterial, antifungal, antioxidant, antiproliferative, anti-inflammatory, and healing potential. However, further studies are still needed to clarify a link between its traditional uses, the active compounds, and the reported pharmacological activities, as well as detailed research to determine the toxicological profile of C. ferrea.


Asunto(s)
Antiinfecciosos , Antiinflamatorios , Antioxidantes , Caesalpinia/química , Fitoquímicos , Extractos Vegetales , Animales , Antiinfecciosos/química , Antiinfecciosos/uso terapéutico , Antiinflamatorios/química , Antiinflamatorios/uso terapéutico , Antioxidantes/química , Antioxidantes/uso terapéutico , Etnobotánica , Etnofarmacología , Humanos , Fitoquímicos/química , Fitoquímicos/uso terapéutico , Fitoterapia , Extractos Vegetales/química , Extractos Vegetales/uso terapéutico
13.
Ecotoxicol Environ Saf ; 169: 669-677, 2019 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-30500736

RESUMEN

The increase in urbanization and industrialization has contributed to the contamination of different environments by means of xenobiotic compounds, such as heavy metals, causing changes in microbial communities. Among these metals, the Mercury (Hg2+) is one the most prevalent toxic metals for the environment The present study aimed to evaluate the effect of mercury on the formation of biofilm by environmental (collected from urban stream water) and clinical isolates of Klebsiella pneumoniae. In addition, antibiotic resistance, virulence factors, and genetic diversity were investigated. Taxonomic identity of eight isolates (one reference, two clinical, and five environmental isolates) was performed by MALDI-TOF-MS, while the antibiotic susceptibility profile was assessed by the disc diffusion method. The ability to form biofilms was evaluated by culture on Congo red agar and by crystal violet staining. Biofilm structure was analyzed by scanning electron microscopy. The hydrophobicity profile and the presence of the virulence genes cps, fimH, and mrkD was investigated. The presence of merA and its relationship with antimicrobial resistance were also assessed. The identity of all isolates was confirmed by MALDI-TOF-MS, and different profiles of resistance to mercury and antibiotics as well as of biofilm formation were identified for the clinical and environmental isolates. All isolates were hydrophilic and positive for the virulence genes cps, fimH, and mrkD; only the clinical isolate K36-A2 was positive for merA. The diversity of the isolates was confirmed by ERIC-PCR, which revealed high heterogeneity among the isolates. In conclusion, the data demonstrate that the investigated isolates present different responses to exposure to Hg2+ and correspond to distinct populations of K. pneumoniae disseminated in the investigated environment. The data obtained in this work will aid in understanding the mechanisms of survival of this pathogen under adverse conditions.


Asunto(s)
Biopelículas/efectos de los fármacos , Contaminantes Ambientales/toxicidad , Klebsiella pneumoniae/efectos de los fármacos , Mercurio/toxicidad , Antibacterianos/farmacología , Biopelículas/crecimiento & desarrollo , Farmacorresistencia Bacteriana/efectos de los fármacos , Farmacorresistencia Bacteriana/genética , Hospitales , Humanos , Klebsiella pneumoniae/genética , Klebsiella pneumoniae/patogenicidad , Pruebas de Sensibilidad Microbiana , Factores de Virulencia/genética
14.
BMC Complement Altern Med ; 18(1): 284, 2018 Oct 19.
Artículo en Inglés | MEDLINE | ID: mdl-30340567

RESUMEN

BACKGROUND: Spondias tuberosa is a plant that produces a fruit crop with high economic relevance at Brazilian Caatinga. Its roots and leaves are used in folk medicine. METHODS: Chemical composition of a hexane extract from S. tuberosa leaves was evaluated by thin-layer chromatography (TLC), high-performance liquid chromatography (HPLC) and 1H nuclear magnetic resonance (NMR). Antioxidant potential was investigated by DPPH and ABTS assays. Antifungal action on Candida species was evaluated determining the minimal inhibitory concentration (MIC50) and putative mechanisms were determined by flow cytometry analysis. In addition, hemolytic activity on human erythrocytes was assessed and the concentration required to promote 50% hemolysis (EC50) was determined. RESULTS: Phytochemical analysis by TLC showed the presence of flavonoids, hydrolysable tannins, saponins and terpenes. The HPLC profile of the extract suggested the presence of gallic acid (0.28 ± 0.01 g%) and hyperoside (1.27 ± 0.01 g%). The representative 1H NMR spectrum showed saturated and unsaturated fatty acids among the main components. The extract showed weak and moderate antioxidant activity in DPPH (IC50: 234.00 µg/mL) and ABTS (IC50: 123.33 µg/mL) assays, respectively. It was able to inhibit the growth of C. albicans and C. glabrata with MIC50 of 2.0 and 0.078 mg/mL, respectively. The treatment of C. glabrata cells with the extract increased levels of mitochondrial superoxide anion, caused hyperpolarization of mitochondrial membrane, and compromised the lysosomal membrane. Weak hemolytic activity (EC50: 740.8 µg/mL) was detected. CONCLUSION: The results demonstrate the pharmacological potential of the extract as antioxidant and antifungal agent, aggregating biotechnological value to this plant and stimulating its conservation.


Asunto(s)
Anacardiaceae/química , Antifúngicos/farmacología , Antioxidantes/farmacología , Membranas Mitocondriales/efectos de los fármacos , Extractos Vegetales/farmacología , Candida/citología , Candida/efectos de los fármacos , Hexanos , Lisosomas/efectos de los fármacos
15.
Exp Parasitol ; 173: 18-28, 2017 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-27956086

RESUMEN

Tritrichomonas foetus infects the bovine urogenital tract, causing bovine trichomoniasis. Significant economic losses may occur due to infertility and abortion among cattle. Trichomonas vaginalis is the causative agent of trichomoniasis; the most common but overlooked non-viral sexually transmitted disease worldwide. Human and bovine trichomoniasis present treatment restrictions and efforts to identify new alternatives are essential. The present study evaluated the anti-trichomonads activities of seven fractions from northwest endemic plant Manilkara rufula. Flavonoids and condensed tannins were identified from these fractions by LC-DAD-MS/MS and MALDI-MS/MS. Altogether, the results demonstrated for the first time the structural description of tannins from leaves of M. rufula and the relation of these compounds with anti-T. vaginalis and anti-T. foetus activities. Overall, this report reveals the potential of M. rufula fractions against both parasites and shows new alternatives to treat the infection caused by trichomonads.


Asunto(s)
Antitricomonas/farmacología , Flavonoides/farmacología , Manilkara/química , Extractos Vegetales/farmacología , Taninos/farmacología , Trichomonas vaginalis/efectos de los fármacos , Tritrichomonas foetus/efectos de los fármacos , Antitricomonas/química , Antitricomonas/aislamiento & purificación , Brasil , Línea Celular , Supervivencia Celular , Cromatografía Liquida , Células Epiteliales/efectos de los fármacos , Flavonoides/química , Flavonoides/aislamiento & purificación , Células HeLa , Humanos , Estructura Molecular , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación , Hojas de la Planta/química , Espectrometría de Masa por Láser de Matriz Asistida de Ionización Desorción , Taninos/química , Taninos/aislamiento & purificación , Trichomonas vaginalis/fisiología , Tritrichomonas foetus/fisiología
16.
Bioorg Med Chem Lett ; 26(9): 2229-36, 2016 May 01.
Artículo en Inglés | MEDLINE | ID: mdl-27020521

RESUMEN

Trichomonas vaginalis causes trichomoniasis; the most common but overlooked non-viral sexually transmitted disease worldwide. The treatment is based at 5'-nitroimidazoles, however, failure are related to resistance of T. vaginalis to chemotherapy. Caatinga is a uniquely Brazilian region representing a biome with type desert vegetation and plants present diverse biological activity, however, with few studies. The aim of this study was to investigate the activity against T. vaginalis of different plants from Caatinga and identify the compounds responsible by the activity. A bioguided fractionation of Manilkara rufula was performed and four major compounds were identified: caproate of α-amyrin (1b), acetate of ß-amyrin (2a), caproate of ß-amyrin (2b), and acetate of lupeol (3a). In addition, six derivatives of α-amyrin (1), ß-amyrin (2) and lupeol (3) were synthesized and tested against the parasite. Ursolic acid (5) reduced about 98% of parasite viability after 2h of incubation and drastic ultrastructural alterations were observed by scanning electron microscopy. Moreover, 5 presented high cytotoxicity to HMVII and HeLa cell line and low cytotoxicity against Vero line at 50 µM (MIC against the parasite). Metronidazole effect against T. vaginalis resistant isolate was improved when in association with 5.


Asunto(s)
Extractos Vegetales/farmacología , Plantas Medicinales/química , Trichomonas vaginalis/efectos de los fármacos , Evaluación Preclínica de Medicamentos , Plantas Medicinales/clasificación
17.
Pharm Biol ; 53(3): 464-8, 2015 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-25472018

RESUMEN

CONTEXT: The local communities living in the Brazilian Caatinga biome have a significant body of traditional knowledge on a considerable number of medicinal plants used to heal several maladies. OBJECTIVE: Based on ethnopharmacological data, this study screened 23 aqueous plant extracts against two well-known models of biofilm-forming bacteria: Staphylococcus epidermidis and Pseudomonas aeruginosa. MATERIALS AND METHODS: Crystal violet assay and scanning electron microscopy (SEM) were used to evaluate the effect of extracts on biofilm formation and measurements of the absorbance at 600 nm to assess bacterial growth. Selected extracts were investigated regarding the cytotoxicity by MTT assay using mammal cells and the qualitative phytochemical fingerprint by thin layer chromatography. RESULTS: Harpochilus neesianus Mart. ex Nees. (Acanthaceae) leaves, Apuleia leiocarpa Vogel J. F. Macbr. (Fabaceae), and Poincianella microphylla Mart. ex G. Don L. P. Queiroz (Fabaceae) fruits showed non-biocidal antibiofilm action against S. epidermidis with activities of 69, 52, and 63%, respectively. SEM confirmed that biofilm structure was strongly prevented and that extracts promoted overproduction of the matrix and/or bacterial morphology modification. Poincianella microphylla demonstrated toxicity at 4.0 mg/mL and 2.0 mg/mL, A. leiocarpa presented toxicity only at 4.0 mg/mL, whereas H. neesianus presented the absence of toxicity against Vero cell line. Preliminary phytochemical analysis revealed the presence of flavonoids, terpenoids, steroids, amines, and polyphenols. DISCUSSION AND CONCLUSIONS: This work provides a scientific basis which may justify the ethnopharmacological use of the plants herein studied, indicating extracts that possess limited mammal cytotoxicity in vitro and a high potential as a source of antibiofilm drugs prototypes.


Asunto(s)
Antibacterianos/farmacología , Biopelículas/efectos de los fármacos , Extractos Vegetales/farmacología , Plantas Medicinales , Pseudomonas aeruginosa/efectos de los fármacos , Staphylococcus epidermidis/efectos de los fármacos , Animales , Antibacterianos/aislamiento & purificación , Biopelículas/crecimiento & desarrollo , Brasil , Chlorocebus aethiops , Extractos Vegetales/aislamiento & purificación , Pseudomonas aeruginosa/fisiología , Staphylococcus epidermidis/fisiología , Células Vero
18.
Parasitol Int ; 98: 102820, 2024 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-37884077

RESUMEN

Aedes aegypti, a mosquito, is responsible for the spread of many diseases, including dengue, zika, and chikungunya. However, due to this mosquito's developed resistance to conventional pesticides, effectively controlling it has proven to be challenging. This study aimed to evaluate the insecticidal potential of the essential oil from the leaves of Eugenia stipitata against Ae. aegypti, offering a natural and sustainable alternative for mosquito control. Tests were conducted using third-stage larvae to evaluate larvicidal activity and pupae collected up to 14 h after transformation to investigate pupicidal activity. Throughout the bioassays, the organisms were exposed to various essential oil concentrations. The findings demonstrated that the essential oil of E. stipitata exhibited larvicidal action, resulting in 100% larval mortality after 24 h and an LC50 value of 0.34 mg/mL. The effectiveness of essential oil as a pupicidal agent was also demonstrated by its LC50 value of 2.33 mg/mL and 100% larval mortality in 24 h. It can be concluded that the essential oil of E. stipitata holds promise as a natural pest control agent. Its use may reduce the reliance on conventional chemical pesticides, providing a more sustainable and effective strategy to combat diseases spread by mosquitoes.


Asunto(s)
Aedes , Insecticidas , Aceites Volátiles , Infección por el Virus Zika , Virus Zika , Animales , Insecticidas/farmacología , Aceites Volátiles/farmacología , Aceites Volátiles/química , Hojas de la Planta/química , Larva , Extractos Vegetales/química
19.
J Ethnopharmacol ; 303: 115941, 2023 Mar 01.
Artículo en Inglés | MEDLINE | ID: mdl-36442761

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: Eugenia gracillima is widely used by the population in the manufacture of pulps and jellies, with popular reports of its use in the treatment of infections in the urinary system, respiratory and dermatological problems. A previous study reports that EO from E. gracillima leaves proved to be a promising antioxidant agent in combating the promastigote forms of protozoa. Despite this, this species has been little studied due to its pharmacological properties. STUDY OBJECTIVE: In this study, an essential oil extracted (EO) from Eugenia gracillima leaves was evaluated for its acute toxicity and anti-inflammatory, antinociceptive and behavioral effects in mice. METHODS: The EO was obtained by hydrodistillation, and the composition analysis was performed by gas chromatography coupled to mass spectrometry. Acute toxicity assessment was performed with observation of hematological parameters and histopathological evaluation, as well as tests to investigate antinociceptive, anti-inflammatory activities and behavioral effects. RESULTS: Chromatographic analysis showed D-germacrene (16.10%), γ-muurolene-g (15.60%) and bicyclogermacrene (8.53%) as the majority of compounds. In the toxicity evaluation, no death or physiological changes were observed in mice treated with a single oral dose of up to 5000 mg/kg, and it did not lyse erythrocytes in vitro. The hematological parameters evaluated were not changed after treatment; however, 5,000 mg/kg promoted an increase in transaminase levels. In the histopathological evaluation, only the animals that received the dose of 5000 mg/kg showed discrete leukocyte infiltration around the centrilobular vein in the liver. Antinociceptive activity was detected through tests of acetic acid-induced writhing, formalin, and tail flick, promoted in part by the opioid receptor pathway. In the evaluation of anti-inflammatory activity, a reduction in inflammation was observed in the paw edema test and a decrease in the migration of leukocytes and neutrophils in the peritonitis test. The open field and elevated plus maze tests showed that EO did not affect the animals' motor functions or exploratory activity. CONCLUSION: It was concluded that the essential oil of E. gracillima has potential for the development of pharmaceutical formulations with analgesic and anti-inflammatory actions in non-toxic concentrations.


Asunto(s)
Eugenia , Aceites Volátiles , Ratones , Animales , Aceites Volátiles/uso terapéutico , Aceites Volátiles/toxicidad , Eugenia/química , Cromatografía de Gases y Espectrometría de Masas , Dolor/inducido químicamente , Dolor/tratamiento farmacológico , Analgésicos/uso terapéutico , Analgésicos/toxicidad , Antiinflamatorios/uso terapéutico , Antiinflamatorios/toxicidad , Inflamación/inducido químicamente , Inflamación/tratamiento farmacológico , Extractos Vegetales/farmacología , Hojas de la Planta , Edema/inducido químicamente , Edema/tratamiento farmacológico
20.
Toxicol Res ; 39(2): 179-190, 2023 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-37008695

RESUMEN

The present study aimed to evaluate saline extracts from the leaves (LE) and stem (SE) of Portulaca elatior in relation to their phytochemical composition and photoprotective and antioxidant effects, as well as to evaluate the toxicity of the leaf extract. The extracts were characterized for protein concentration and phenol and flavonoid contents, as well as for thin layer chromatography (TLC) and high-performance liquid chromatography (HPLC) profiles. Total antioxidant capacity and DPPH and ABTS+ scavenging activities were determined. In the photoprotective activity assay, the sun protection factor (SPF) was calculated. The toxicity evaluation of LE included in vitro hemolytic assay and in vivo oral and dermal acute toxicity assays in Swiss mice. LE showed the highest protein, phenol, and flavonoid (8.79 mg/mL, 323.46 mg GAE/g, and 101.96 QE/g, respectively). TLC revealed the presence of flavonoids, reducing sugars, terpenes, and steroids in both extracts. In HPLC profiles, LE contained flavonoids, while SE contained flavonoids and ellagic tannins. The antioxidant activity assays showed the lowest IC50 values ​(34.15-413.3 µg/mL) for LE, which presented relevant SPF (> 6) at 50 and 100 µg/mL. LE demonstrated low hemolytic capacity, and no signs of intoxication were observed in mice treated orally or topically at 1000 mg/kg. However, at 2000 mg/kg, an increase in the mean corpuscular volume of erythrocytes and a reduction in lymphocytes were observed; animals treated topically with 2000 mg/kg displayed scratching behavior during the first hour of observation and showed edema and erythema that regressed after six days. In conclusion, LE did not present acute oral or dermal toxicity in Swiss mice at a dose of 1000 mg/kg and showed slight toxicity in animals treated with 2000 mg/kg. Supplementary Information: The online version contains supplementary material available at 10.1007/s43188-022-00160-2.

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