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1.
Fitoterapia ; 140: 104443, 2020 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-31790767

RESUMO

Aucubin is an iridoid glycoside that is widely prevalent in traditional medicinal herbs, such as Eucommia ulmoides Oliv., Aucuba japonica Thunb. and Plantago asiatica L. This review aims to provide a comprehensive summary of the source, biological activity, pharmacokinetics and toxicology of aucubin with the ultimate objective of providing a guide for future drug development and potential clinical applications of aucubin. Aucubin is a highly active compound possessing extensive biological effects including antioxidant, anti-aging, anti-inflammatory, anti-fibrotic, anti-cancer, hepatoprotective, neuroprotective and osteoprotective properties. Although aucubin has been shown to have poor oral bioavailability in rats, aucubin is widely distributed in multiple organs including kidney, liver, heart, spleen and lung, and there is a sex difference in the absorption of aucubin. Tolerance of aucubin is good and no serious adverse reactions have been observed to date. In short, aucubin is a compound with abundant potential sources, good safety and numerous beneficial biological activities, which exhibits high potential value for use in health care products and pharmaceuticals. In order to accelerate the development and utilization of aucubin-related products, in-depth studies should be focused on the following questions of interest. First, it is necessary to introduce advanced separation and formulation technologies to improve the yield and stability of aucubin products. Second, studies should focus on the specific pharmacological activities of aucubin to determine the structure-activity relationship so as to improve the efficacy and reduce side effects. Finally, clinical studies are needed to confirm the efficacy of aucubin in specific diseases.


Assuntos
Glucosídeos Iridoides/farmacologia , Glucosídeos Iridoides/toxicidade , Animais , Humanos , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/toxicidade , Plantas Medicinais/química
2.
J Ethnopharmacol ; 246: 112206, 2020 Jan 10.
Artigo em Inglês | MEDLINE | ID: mdl-31494199

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Cedrela serrata Royle (C. serrata) is a medicinal plant not only used for constructions but also an important conventional medicine for the treatment of various diseases such as; diabetes, jaundice, liver diseases, diarrhea, fever, chronic infantile dysentery, intestinal worms, hypertension, skin and blood diseases. AIMS: This review article documents and critically assesses, for the first time; up to date categorized information about C. serrata including its reported pharmacological activities, cultural uses, active compounds, and botanical description. MATERIALS AND METHOD: s: All provided information about C. serrata was collected using the electronic databases (e.g. Google Scholar, Web of Science, Scopus, PubMed, Science Direct and Springer Link), books (e.g. Trees of Pakistan and Herbalism, Phytochemistry, and Ethnopharmacology) and thesis. RESULTS: Qualitative and quantitative phytochemical studies on C. serrata revealed the presence of important chemical constituents such as; flavonoids, phenolic acids, alkaloids, saponins, tannins, and cardiac glycosides. The phytochemicals showed various in vitro activities like antioxidant, anti-infective, antiglycation, cytotoxic activities. Major areas of research conducted on C. serrata are its antioxidant and anti-infective activities. Few historical uses of C. serrata are supported by modern in vitro pharmacological studies such as; antidiarrheal, antidiabetic, and leishmanicidal activity. CONCLUSION: There were convincing evidence in in vitro studies supporting C. serrata antioxidant, anti-infective, anti-diabetic, anti-glycating, and cytotoxic activities. Nevertheless, all reported pharmacological activities were carried out in vitro and a gap in research i.e. preclinical and clinical investigation still exists. The authors emphasize the need for future in-depth research and clinical trials to investigate C. serrata pharmacological activity, clinical efficacy and safety. The potential chemical compounds with suggestive classes may need to be isolated and pharmacological activities must be established for these compounds. The plant has very limited information about pharmacological activities and the data available for supportive cultural uses needs proper validation.


Assuntos
Cedrela , Fitoterapia , Animais , Etnobotânica , Etnofarmacologia , Humanos , Medicina Tradicional , Compostos Fitoquímicos/análise , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/uso terapêutico , Compostos Fitoquímicos/toxicidade , Preparações de Plantas/química , Preparações de Plantas/farmacologia , Preparações de Plantas/uso terapêutico , Preparações de Plantas/toxicidade
3.
Curr Top Med Chem ; 19(29): 2718-2738, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31721714

RESUMO

Widely advocated for their health benefits worldwide, herbal medicines (HMs) have evolved into a billion dollar generating industry. Much is known regarding their wellness inducing properties, prophylactic and therapeutic benefits for the relief of both minor to chronic ailment conditions given their long-standing use among various cultures worldwide. On the other hand, their equally meaningful chemistry, pharmacokinetic profile in humans, interaction and toxicity profile have been poorly researched and documented. Consequently, this review is an attempt to highlight the health benefits, pharmacokinetics, interaction, and toxicity profile of five globally famous HMs. A systematic literature search was conducted by browsing major scientific databases such as Bentham Science, SciFinder, ScienceDirect, PubMed, Google Scholar and EBSCO to include 196 articles. In general, ginsenosides, glycyrrhizin and curcumin demonstrate low bioavailability when orally administered. Ginkgo biloba L. induces both CYP3A4 and CYP2C9 and alters the AUC and Cmax of conventional medications including midazolam, tolbutamide, lopinavir and nifedipine. Ginsenosides Re stimulates CYP2C9, decreasing the anticoagulant activity of warfarin. Camellia sinensis (L.) Kuntze increases the bioavailability of buspirone and is rich in vitamin K thereby inhibiting the activity of anticoagulant agents. Glycyrrhiza glabra L. displaces serum bound cardiovascular drugs such as diltiazem, nifedipine and verapamil. Herbal medicine can directly affect hepatocytes leading to hepatoxicity based on both intrinsic and extrinsic factors. The potentiation of the activity of concurrently administered conventional agents is potentially lethal especially if the drugs bear dangerous side effects and have a low therapeutic window.


Assuntos
Medicina Herbária , Compostos Fitoquímicos/farmacocinética , Compostos Fitoquímicos/toxicidade , Fitoterapia , Área Sob a Curva , Disponibilidade Biológica , Citocromo P-450 CYP2C9/biossíntese , Citocromo P-450 CYP3A/biossíntese , Indução Enzimática , História do Século XXI , Humanos
4.
SAR QSAR Environ Res ; 30(11): 801-824, 2019 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-31565973

RESUMO

Human malaria is the most widespread mosquito-borne life-threatening disease worldwide. In the absence of effective vaccines, prevention and treatment of malaria only depend on prophylaxis and drug-based therapy either in monotherapy or in combination. Unfortunately, the number of available antimalarial drugs presenting different mechanisms of action is rather limited. In addition, the appearance of drug-resistance in the parasite strains impacts the efficacy of the treatments. As a result, there is a crucial need to find new drugs to circumvent resistance problems. In the quest to identify new antimalarial agents a huge number of plant-derived compounds (PDCs) have been investigated. Surprisingly in the in silico PDC screening programs, toxicity filters are either never used or so simple that their interest is limited. In this context, the goal of this study was to show how to take advantage of validated toxicity QSAR models for refining the selection of PDCs. From an original data set of 507 PDCs collected from the literature, the use of toxicity filters for endocrine disruption, developmental toxicity, and hepatotoxicity in conjunction with classical pharmacokinetic filters allowed us to obtain a list of 31 compounds of potential interest. The pros and cons of such a strategy have been discussed.


Assuntos
Antimaláricos/toxicidade , Compostos Fitoquímicos/toxicidade , Testes de Toxicidade/métodos , Antimaláricos/química , Antimaláricos/farmacocinética , Antimaláricos/farmacologia , Simulação por Computador , Desenho de Drogas , Modelos Químicos , Compostos Fitoquímicos/química , Compostos Fitoquímicos/farmacocinética , Compostos Fitoquímicos/farmacologia , Plantas/química , Relação Quantitativa Estrutura-Atividade
5.
Molecules ; 24(16)2019 Aug 14.
Artigo em Inglês | MEDLINE | ID: mdl-31416129

RESUMO

The present work describes the chemical characterization and the phytotoxicity assessment of essential oils (EOs) obtained from spent materials or pruning waste of four plant species: Zingiber officinale Roscoe used in the juicing industry, Pistacia vera L. var. Bronte used in the food industry, discarded material of industrial hemp (Cannabis sativa L. var. Futura 75), and pruning waste from Cupressus sempervirens L. The phytochemical profile of the EOs was evaluated by gas chromatographic flame ionization detection (GC-FID) and GC-MS analyses, which highlighted the presence of several compounds with a wide range of biological activities. Among them, application possibilities in agriculture were evaluated by studying the phytotoxic activity in vitro against germination and initial radical growth of several seeds such as Raphanus sativus L., Lepidium sativum L., Lactuca sativa L., Solanum lycopersicum L., Lolium multiflorum Lam., and Portulaca oleracea L.


Assuntos
Óleos Voláteis/química , Óleos Voláteis/farmacologia , Óleos Vegetais/química , Óleos Vegetais/farmacologia , Antioxidantes/química , Antioxidantes/farmacologia , Antioxidantes/toxicidade , Cromatografia Gasosa-Espectrometria de Massas , Óleos Voláteis/toxicidade , Compostos Fitoquímicos/química , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/toxicidade , Óleos Vegetais/toxicidade , Plantas/química , Plantas/ultraestrutura , Portulaca/efeitos dos fármacos
6.
J Ethnopharmacol ; 245: 112147, 2019 Dec 05.
Artigo em Inglês | MEDLINE | ID: mdl-31401319

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Ilex pubescens (I. pubescens), which is well known in Chinese as Mao-Dong-Qing, is widely used in traditional Chinese medicine. This plant is distributed in the wild in southern China, and the roots and stems are used for clearing heat, detoxifying, activating blood circulation and dispelling stasis. Moreover, it is used for treating wind-heat cold, lung-heat asthma, swelling and pain of pharynxes and gingivae, thoracic obstruction and cardiodynia with pungent, stroke, hemiplegia, thromboangiitis obliterans, burn, scald and central retinitis. AIMS OF THE REVIEW: This paper aims to provide a critical summary of the current studies on I. pubescens. The progress in research on the botany, traditional uses, phytochemistry, pharmacology and toxicology of the plant is discussed. We mainly focus on the phytochemical and pharmacological investigations of I. pubescens. Furthermore, perspectives for possible future studies on I. pubescens are also discussed. MATERIALS AND METHODS: A systematic review was conducted on the studies of I. pubescens performed during the past 40 years with resources including the Chinese Pharmacopoeia and literature databases such as PubMed, Science Direct, Wiley, CNKI (China National Knowledge Infrastructure), SciFinder, Web of Science, Google Scholar and Baidu Scholar. RESULTS: To date, more than 200 compounds have been isolated and identified from the plant, a substantial proportion of which were reported to be triterpenes. Biological effects such as protective effects against cardio-cerebrovascular diseases, anti-thrombosis, anti-inflammatory and anti-tumour activities were also investigated in in vitro and in vivo research. Therapeutic effects are attributed to the bioactivities of the naturally occurring compounds in this herb. Furthermore, toxicological studies on I. pubescens are relatively scarce, and it is worthy of further research. CONCLUSIONS: This review summarizes the results from current studies of I. pubescens, which is one of the valuable medicinal sources from traditional herbs. Some conventional uses have been evaluated by pharmacological investigation. In addition, unresolved issues include molecular mechanisms underlying bioactivities, pharmacokinetics, toxicology and efficacy, which are still being studied and explored before achieving integration into clinical medicines.


Assuntos
Ilex , Animais , Etnobotânica , Etnofarmacologia , Humanos , Medicina Tradicional Chinesa , Compostos Fitoquímicos/análise , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/uso terapêutico , Compostos Fitoquímicos/toxicidade , Fitoterapia , Preparações de Plantas/química , Preparações de Plantas/farmacologia , Preparações de Plantas/uso terapêutico , Preparações de Plantas/toxicidade
7.
J Ethnopharmacol ; 245: 112169, 2019 Dec 05.
Artigo em Inglês | MEDLINE | ID: mdl-31425732

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Plinia cauliflora (Mart.) Kausel is widespread in alluvial plains and open forests in Brazil, Argentina, and Paraguay. The fruits of P. cauliflora are used as food, and almost all parts of this species have long been used as a traditional Brazilian medicine for the treatment of skin irritations, flu, diarrhea, labyrinthitis, genito-urinary problems, and asthma. THE AIM OF THE REVIEW: This review provides comprehensive and up-to-date information on P. cauliflora with regard to its ethnopharmacological uses, constituents, biological activities, and toxicology, all of which are useful for future research and the development of new drugs. MATERIALS AND METHODS: The information and data on P. cauliflora were collected from ethnobotanical textbooks and scientific databases, such as PubMed, Scopus, EBSCO, Science Direct, Google, and Google Scholar. RESULTS: The main chemical constituents in P. cauliflora preparations were depsides, flavonoids, and hydrolysable tannins. The main medicinal use of the species in Brazil is for the treatment of diarrhea. Although antimicrobial potential of this species has been demonstrated, data on gastrointestinal motility are still incipient and need further investigation. Studies that indicate the efficacy of its traditional use for sore throat, pelvic hemorrhage, uterine wounds, vaginal discharge, and flu are nonexistent. The scientific literature does not describe any toxic effects of its popular use. However, the available data do not allow us to conclude that the ethnomedicinal use of this species is safe, with a lack of well-designed preclinical tests and randomized clinical trials. CONCLUSION: This review summarizes research on the traditional use, phytochemistry, biological activities, and toxicology of P. cauliflora. Although P. cauliflora possesses significant biological activities, much of its ethnomedicinal use has not been scientifically evaluated. Well-designed pharmacological and toxicological assays and randomized clinical trials are still needed to validate its ethnopharmacological use as an herbal medicine.


Assuntos
Myrtaceae , Animais , Brasil , Etnofarmacologia , Humanos , Compostos Fitoquímicos/análise , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/uso terapêutico , Compostos Fitoquímicos/toxicidade , Fitoterapia , Preparações de Plantas/química , Preparações de Plantas/farmacologia , Preparações de Plantas/uso terapêutico , Preparações de Plantas/toxicidade
8.
Food Chem Toxicol ; 133: 110758, 2019 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-31412289

RESUMO

Various phytochemicals have been reported to protect against oxidative stress. However, the mechanism underlying has not been systematically evaluated, which limited their application in disease treatment. Nuclear factor erythroid 2-related factor 2 (Nrf2), a central transcription factor in oxidative stress response related to numerous diseases, is activated after dissociating from the cytoskeleton-anchored Kelch-like ECH-associated protein 1 (Keap1). The Keap1-Nrf2 protein-protein interaction has become an important drug target. This study was designed to clarify whether antioxidantive phytochemicals inhibit the Keap1-Nrf2 protein-protein interaction and activate the Nrf2-ARE signaling pathway efficiently. Molecular docking and 3D-QSAR were applied to evaluate the interaction effects between 178 antioxidant phytochemicals and the Nrf2 binding site in Keap1. The Nrf2 activation effect was tested on a H2O2-induced oxidative-injured cell model. Results showed that the 178 phytochemicals could be divided into high-, medium-, and low-total-score groups depending on their binding affinity with Keap1, and the high-total-score group consisted of 24 compounds with abundant oxygen or glycosides. Meanwhile, these compounds could bind with key amino acids in the structure of the Keap1-Nrf2 interface. Compounds from high-total-score group show effective activation effects on Nrf2. In conclusion, phytochemicals showed high binding affinity with Keap1 are promising new Nrf2 activators.


Assuntos
Antioxidantes/farmacologia , Proteína 1 Associada a ECH Semelhante a Kelch/antagonistas & inibidores , Fator 2 Relacionado a NF-E2/agonistas , Compostos Fitoquímicos/farmacologia , Ligação Proteica/efeitos dos fármacos , Animais , Antioxidantes/metabolismo , Antioxidantes/toxicidade , Sítios de Ligação , Humanos , Proteína 1 Associada a ECH Semelhante a Kelch/metabolismo , Simulação de Acoplamento Molecular , Estrutura Molecular , Fator 2 Relacionado a NF-E2/metabolismo , Células PC12 , Compostos Fitoquímicos/metabolismo , Compostos Fitoquímicos/toxicidade , Relação Quantitativa Estrutura-Atividade , Ratos
9.
J Ethnopharmacol ; 242: 112052, 2019 Oct 05.
Artigo em Inglês | MEDLINE | ID: mdl-31265886

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Combretum aculeatum Vent was traditionally used in Sudan, Eretria and Ethiopia as anti-inflammatory in case of skin inflammation, catarrh, wounds, scorpion stings and snake bites. Nevertheless, there is no scientific information regarding this activity. AIM OF STUDY: The present study aimed to evaluate the phytochemical constituents and the scientific basis for the traditional use of Combretum aculeatum Vent through studying its anti-inflammatory properties for the first time to illustrate the putative mechanisms behind this bioactivity. MATERIALS AND METHODS: the ethanolic extract was partitioned by petroleum ether, methylene chloride, ethyl acetate, and n-butanol saturated with water. The petroleum ether fraction was saponified and the saponifiable and unsaponifiable fractions were analyzed on GC/MS. The different fractions were subjected to phytochemical investigation to isolate pure compounds. In-vivo anti-inflammatory activity of the ethanolic extract was evaluated using carrageenan induced rat paws edema method at doses of 200, 400 and 600 mg/kg and proved based on histopathological and biochemical parameters. RESULTS: Five known compounds were isolated for the first time from the aerial parts of Combretum aculeatum Vent: quercetin, vitexin, isorhamnetin 3-O-ß-glucoside, isovitexin and rutin, in addition to two previously isolated ones: ß-sitosterol and its glucoside. The ethanolic extract evidenced in-vivo anti-inflammatory activity by oral intake of 400 mg/kg of the ethanolic extract significantly (P ≥ 0.05) decreased the paw edema (only 32±1.9% increase in paw weight after 4 h) compared to indomethacin (28.6±2.5%). Moreover, it significantly suppressed the serum malondialdehyde (MDA) and nitric oxide (NO) and increased the GSH to be 11.76±0.85, 5.13±0.62 µmol/mL and 5.66±0.28 µM/mL, respectively. It diminished the serum cytokines TNF-α, IL-6 and IL-1ß levels to be 39.1±1.2, 32.6±1.1 and 37.5±1.2 pg/mL, respectively. Results are accompanied by histopathological examination. CONCLUSION: Overall, the results herein presented significant anti-inflammatory properties traditionally ascribed to Combretum aculeatum Vent. Moreover, the biochemical mechanisms associated to this action were highlighted, introducing new prospects for the development of effective anti-inflammatory herbal medicinal products.


Assuntos
Anti-Inflamatórios , Combretum , Edema/tratamento farmacológico , Compostos Fitoquímicos , Extratos Vegetais , Animais , Anti-Inflamatórios/química , Anti-Inflamatórios/uso terapêutico , Anti-Inflamatórios/toxicidade , Carragenina , Citocinas/imunologia , Edema/induzido quimicamente , Edema/imunologia , Edema/patologia , Dose Letal Mediana , Masculino , Camundongos , Compostos Fitoquímicos/análise , Compostos Fitoquímicos/uso terapêutico , Compostos Fitoquímicos/toxicidade , Componentes Aéreos da Planta , Extratos Vegetais/química , Extratos Vegetais/uso terapêutico , Extratos Vegetais/toxicidade , Ratos , Sudão
10.
Pak J Pharm Sci ; 32(3 (Supplementary)): 1145-1154, 2019 May.
Artigo em Inglês | MEDLINE | ID: mdl-31303583

RESUMO

Survivin (IAP proteins) is considered as a significant target for anticancer drug research owing to its upregulation in tumor cells to mediate resistance to apoptotic stimulus. The current study aimed to investigate phytochemicals as inhibitors of survivin with caspases to reactivate the functioning of caspases through molecular docking. The compounds namely 2(R), 4(R)-dihydroxypyrrolidine, 4-hydroxy-2-(4-methoxyphenyl)-1,1-dioxo-3,4-dihydrothieno[3,2-e]thiazine-6-sulfonamide, 2,3-Diketo-L-gulonic acid, (3-hydroxy-2-octadeca-9,12-dienoyloxypropyl) octadecanoate, 2-[[4-[[4-[(4-formamido-1-methylimidazole-2-carbonyl)amino]-1-methylimidazole-2-carbonyl]amino]-1-methylimidazole-2-carbonyl]amino]ethyl-dimethylazanium, Picolinic acid and (2-Hydroxy-5-nitrophenyl) dihydrogen phosphate successfully bind inside the pocket of survivin. ADMETsar was used to evaluate the anticancer potential of selected compounds. These compounds can be proposed as effective inhibitors, disrupting the survivin-caspases interaction and reactivating the caspases function of apoptosis. The study might facilitate the development of cost-effective and natural drugs against cancer. However, further validation is essential for confirmation of its drug efficacy and bio-compatibility.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Ensaios de Seleção de Medicamentos Antitumorais/métodos , Compostos Fitoquímicos/farmacologia , Survivina/antagonistas & inibidores , Survivina/química , Antineoplásicos Fitogênicos/farmacocinética , Antineoplásicos Fitogênicos/toxicidade , Caspases/metabolismo , Simulação por Computador , Humanos , Simulação de Acoplamento Molecular , Terapia de Alvo Molecular , Compostos Fitoquímicos/farmacocinética , Compostos Fitoquímicos/toxicidade , Conformação Proteica , Survivina/metabolismo , Distribuição Tecidual
11.
J Ethnopharmacol ; 243: 112086, 2019 Oct 28.
Artigo em Inglês | MEDLINE | ID: mdl-31310830

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Medicinal plants widely used by the population contain significant concentrations of biologically active compounds and, although they have proven pharmacological properties, can cause DNA damage and develop fatal diseases. AIM OF THE STUDY: The present study aimed to evaluate the genotoxic, cytotoxic potential and clastogenic effects of the aqueous extract from Mangifera indica leaves (EAMI) on rats submitted to experimental genotoxicity models and through the SMART test performed in Drosophila melanogaster. MATERIAL AND METHODS: The comet assay and the micronucleus test were performed on peripheral and bone marrow blood, respectively, of Wistar rats, orally treated with EAMI at doses of 125, 250, 500 and 1000 mg/kg/bw for 28 days. In the SMART test, the standard cross between three mutant D. melanogaster strains was used. Larvae were treated with EAMI at different concentrations, and the wings of adult flies were evaluated for the presence/frequency of mutant spots and compared to the negative control group. RESULTS: Phytochemical analysis of EAMI indicated high levels of flavonoids. The tests performed in rats showed that EAMI did not present significant genotoxic or clastogenic effects. The results showed a critical dose-dependent cytoprotective effect exerted by EAMI. This result was attributed to the high content of polyphenols and flavonoids. The biotransformation metabolites of EAMI did not present genotoxic activity, as demonstrated by the SMART test. CONCLUSIONS: These results are relevant since they provide safety information about a plant species of great therapeutic, economical, nutritious and ethnopharmacological value for the population.


Assuntos
Mangifera , Extratos Vegetais/toxicidade , Animais , Ensaio Cometa , Drosophila melanogaster/efeitos dos fármacos , Drosophila melanogaster/genética , Feminino , Flavonoides/análise , Flavonoides/toxicidade , Humanos , Masculino , Testes para Micronúcleos , Compostos Fitoquímicos/análise , Compostos Fitoquímicos/toxicidade , Extratos Vegetais/química , Folhas de Planta/classificação , Ratos Wistar , Medição de Risco
12.
BMC Complement Altern Med ; 19(1): 150, 2019 Jun 26.
Artigo em Inglês | MEDLINE | ID: mdl-31242939

RESUMO

BACKGROUND: Traditional medicine remedies are commonly used for treatment of diverse ailments including bacterial infections. The activity against resistant bacteria and safety of some remedies sold as anti-infective treatments in market places in Buea, Southwest Cameroon were investigated as potential alternative treatment to counter increasing antibiotic resistance. METHODS: Ten remedies were purchased, their components documented and microbial load estimated. Methanol extracts of the remedies were tested for antibacterial activity by disc diffusion and microdilution. Cytotoxicity was evaluated on monkey kidney epithelial cells (LLC-MK2) while acute oral toxicity was done in BALB/c mice for the bactericidal extract. Extracts were further analysed using phytochemical tests. RESULTS: All the remedies had microbial loads above the acceptable limit of 105 CFU/g. The highest activity was produced by extracts of four remedies (TP 1, 2, 4, 6a, 6b) against all clinical isolates among which three were active against four control strains. Zones of inhibition ranged from 8 to 27 mm. Two of the four extracts produced zones ≥20 mm against multidrug resistant clinical isolates of Citrobacter freundii and Escherichia coli but were less active compared to Gentamycin positive control (P < 0.0001-0.0014). The most active extracts also recorded minimum inhibitory concentrations of 1 to 4 mg/mL. One of them (TP2) was bactericidal against a clinical isolate of methicillin-resistant Staphylococcus aureus with a minimum bactericidal concentration of 8 mg/mL. Extracts of six remedies did not show cytotoxicity and no mortality or adverse effect was recorded in the acute oral toxicity test. Phytochemical screening showed the most active extracts contained relatively high amounts of alkaloids and flavonoids. CONCLUSION: Only four of the eight remedies tested showed activity against multidrug resistant bacteria suggesting some of these remedies may not be effective against bacterial infections. Production and handling methods should be improved and the product quality controlled to ensure biosecurity. The remedies which were both active and non-toxic should be further investigated including in vivo experiments to assess their efficacy.


Assuntos
Antibacterianos/farmacologia , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/farmacologia , Plantas Medicinais/química , Animais , Antibacterianos/química , Antibacterianos/isolamento & purificação , Antibacterianos/toxicidade , Bactérias/efeitos dos fármacos , Bactérias/genética , Bactérias/crescimento & desenvolvimento , Bactérias/isolamento & purificação , Infecções Bacterianas/tratamento farmacológico , Infecções Bacterianas/microbiologia , Camarões , Farmacorresistência Bacteriana Múltipla , Escherichia coli/efeitos dos fármacos , Escherichia coli/crescimento & desenvolvimento , Feminino , Humanos , Medicina Tradicional , Staphylococcus aureus Resistente à Meticilina/efeitos dos fármacos , Staphylococcus aureus Resistente à Meticilina/crescimento & desenvolvimento , Camundongos , Camundongos Endogâmicos BALB C , Testes de Sensibilidade Microbiana , Compostos Fitoquímicos/química , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/toxicidade , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/toxicidade , Plantas Medicinais/microbiologia
13.
Molecules ; 24(7)2019 Mar 29.
Artigo em Inglês | MEDLINE | ID: mdl-30934947

RESUMO

In this work, we explore the current knowledge about the phytochemistry and in vitro and in vivo evaluations of the extracts and, where appropriate, the main active components characterized and isolated from the Allamanda cathartica. Of the 15 Allamanda species, most phytochemical, pharmacological, and toxicological studies have focused on A. cathartica. These plants are used for the treatment of various health disorders. Numerous phytochemical investigations of plants from the A. cathartica have shown the presence of hydrocarbons, alcohols, esters, ethers, aldehydes, ketones, fatty acids, phospholipids, volatile compounds, phenolic compounds, flavonoids, alkaloids, steroids, terpenes, lactones, and carbohydrates. Various studies have confirmed that extracts and active substances isolated from the A. cathartica have multiple pharmacological activities. The species A. cathartica has emerged as a source of traditional medicine used for human health. Further studies on the phytochemical, pharmacological, and toxicological properties and their mechanisms of action, safety, and efficacy in the species of A. cathartica is recommended.


Assuntos
Apocynaceae/química , Compostos Fitoquímicos/química , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Biotecnologia/métodos , Etnofarmacologia/métodos , Medicina Tradicional , Estrutura Molecular , Compostos Fitoquímicos/toxicidade , Extratos Vegetais/toxicidade , Plantas Medicinais/química , Toxicologia/métodos
14.
Int J Mol Sci ; 20(7)2019 Apr 03.
Artigo em Inglês | MEDLINE | ID: mdl-30987173

RESUMO

Fritillariae Thunbergii Bulbus (FTB) has been widely used as an antitussive herb for thousands of years in China. However, FTB's traditional uses, chemical compounds and pharmacological activities have not been systematically reviewed. This study aimed to review its traditional uses, phytochemistry, pharmacodynamics, pharmacokinetics and toxicity. We searched the Encyclopedia of Traditional Chinese Medicine to explore the historical records which indicate that it acts to clear heat, resolve phlegm, relieve cough, remove toxicity and disperse abscesses and nodules. We searched 11 databases to identify potential phytochemical or pharmacological studies. Characteristics of its chemical constituents, pharmacological effects, pharmacokinetic and toxicity were descriptively summarized. A total of 9706 studies were identified and 83 of them were included. As a result, 134 chemical constituents were identified, including 26 alkaloids, 29 compounds found in essential oils, 13 diterpenoids, two carbohydrates, two sterols, 18 amino acids, six nucleosides, four nucleobases, four fatty acids, three lignans, and 27 elements. Thirteen pharmacological effects of FTB were identified, including anti-cancer, tracheobronchial relaxation, antitussive, expectorant, anti-muscarinic, anti-inflammation, anti-thyroid, regulation of blood rheology, antiulcer, anti-diarrhea, pain suppression, antioxidation and neuroprotection. These pharmacological activities may be mainly attributed to the alkaloids in FTB. Further phytochemical, pharmacological and network pharmacological studies are recommended.


Assuntos
Asteraceae/química , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/farmacocinética , Extratos Vegetais/farmacologia , Extratos Vegetais/farmacocinética , Testes de Toxicidade , Animais , Humanos , Compostos Fitoquímicos/química , Compostos Fitoquímicos/toxicidade , Extratos Vegetais/química , Extratos Vegetais/toxicidade
15.
Chin J Nat Med ; 17(3): 161-186, 2019 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-30910054

RESUMO

Chimonanthus plants widely distributed in southern area of China, which have a long history of edibles and medicine. Phytochemical investigations have shown that Chimonanthus produced 143 non-volatile constituents, including alkaloids, flavonoids, terpenoids, coumarins and others, which exhibit significant anti-oxidant, anti-bacterial, anti-cancer, anti-inflammatory, antihyperglycemic, antihyperlipidemic and other biological activities. On the basis of systematic reviewing of literatures, this article overviews the non-volatile constituents and pharmacology of Chimonanthus from domestic and foreign over the last 30 years (until June 2018), and may provide a useful reference for the further development of Chimonanthus.


Assuntos
Calycanthaceae/química , Medicamentos de Ervas Chinesas/química , Medicamentos de Ervas Chinesas/farmacologia , Compostos Fitoquímicos/química , Compostos Fitoquímicos/farmacologia , Animais , Medicamentos de Ervas Chinesas/uso terapêutico , Medicamentos de Ervas Chinesas/toxicidade , Humanos , Medicina Tradicional Chinesa , Compostos Fitoquímicos/uso terapêutico , Compostos Fitoquímicos/toxicidade , Fitoterapia
16.
J Mol Model ; 25(4): 88, 2019 Mar 08.
Artigo em Inglês | MEDLINE | ID: mdl-30847632

RESUMO

Alternative treatments from plant-derived small molecules for neutralizing the venom lethality in snake envenomation are prevalent now. Elephantopus scaber, a tropical plant species has been recognized for its various pharmacological activities and especially anti-snake venom property; however, the molecular basis for this property is not understood. It is reported that snake venom PLA2 is a toxic factor with pharmacological effects independent of their catalytic activity. Here we report the inhibition of catalytic property of Cobra and Viper (group I and group II) snake venom PLA2 by the phytocompounds from E. scaber through molecular docking and dynamics studies. Initially, Lipinski's rule, ADMET, and molecular docking studies were carried out. Our results show that among 124 phytocompounds, crepiside E (deacylcynaropicrin-3' beta-glucopyranoside) has shown interactions with the conserved catalytic active site residues, His 48 and Asp 49, in both the PLA2s. Further, molecular dynamic simulations for 60 ns confirmed the stability of crepiside E in the active site of PLA2s and were found to be stable throughout the simulation. In order to understand the drug-likeness of crepiside E, pIC50 and MMGBSA scores were correlated by performing a linear regression analysis. Crepiside E was found to have similar chemical features to that of doxycycline, a known PLA2 inhibitor as indicated by a similarity score of 64.15%. Hence, it is concluded that crepiside E beta glucopyranoside present in Elephantopus scaber contributes to neutralizing the snake venom.


Assuntos
Simulação de Acoplamento Molecular , Simulação de Dinâmica Molecular , Compostos Fitoquímicos/química , Venenos de Serpentes/química , Asteraceae/química , Sítios de Ligação , Domínio Catalítico , Concentração Inibidora 50 , Ligantes , Modelos Moleculares , Conformação Molecular , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/toxicidade , Venenos de Serpentes/antagonistas & inibidores , Relação Estrutura-Atividade
17.
Food Chem Toxicol ; 125: 361-369, 2019 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-30677443

RESUMO

A myriad of phytochemicals may have potential to lead toxicity and endocrine disruption effects by interfering with nuclear hormone receptors. In this examination, the toxicity and estrogen receptor-binding abilities of a set of 2826 phytochemicals were evaluated. The endpoints mutagenicity, carcinogenicity (both CAESAR and ISS models), developmental toxicity, skin sensitization and estrogen receptor relative binding affinity (ER_RBA) were studied using the VEGA QSAR modeling package. Alongside the predictions, models were providing possible information for applicability domains and most similar compounds as similarity sets from their training sets. This information was subjected to perform the clustering and classification of chemicals using Self-Organizing Maps. The identified clusters and their respective indicators were considered as potential hotspot structures for the specified data set analysis. Molecular screening interpretations of models were exhibited accurate predictions. Moreover, the indication sets were defined significant clusters and cluster indicators with probable prediction labels (precision). Accordingly, developed QSAR models showed good predictive abilities and robustness, which observed from applicability domains, representation spaces, clustering and classification schemes. Furthermore, the designed new path could be useful as a valuable approach to determine toxicity levels of phytochemicals and other environmental pollutants and protect the human health.


Assuntos
Compostos Fitoquímicos/química , Compostos Fitoquímicos/toxicidade , Receptores Estrogênicos/química , Algoritmos , Carcinógenos/química , Carcinógenos/toxicidade , Simulação por Computador , Disruptores Endócrinos/química , Disruptores Endócrinos/toxicidade , Mutagênicos/química , Mutagênicos/toxicidade , Relação Quantitativa Estrutura-Atividade
18.
Plant Foods Hum Nutr ; 74(1): 40-46, 2019 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-30324543

RESUMO

Plants, including most food and feed plants, produce a broad range of bioactive chemical compounds. Among these compounds, polyphenols are reported to provide beneficial effects as anti-carcinogenic, anti-atherogenic, anti-inflammatory, immune modulating, anti-microbial, vasodilatory and analgesic. Cocoa (Theobroma cacao), a major, economically important, international crop, has been related to several nutritional benefits, which have been associated with the phenolic fraction. The main subclass of flavonoids found in cocoa is flavanols, particularly (epi)catechins monomers, and their oligomers, also known as procyanidins. In this study, these compounds were isolated by different methodologies as solid phase extraction (SPE), semi-preparative high-performance liquid chromatography (HPLC) and membrane technologies to obtain different polyphenolic profiles by HPLC coupled to electrospray time-of-flight mass spectrometry (ESI-TOF-MS) and to test their cytotoxicity. Finally, different polyphenolic profiles were collected, where the combination of both semi-preparative HPLC and SPE technologies provided the most purified fractions. Filtration with membranes and SPE provide extracts with different composition depending on the pore size of membranes and on the solvent, respectively. In addition, the results of toxicity assay indicated low levels in all fractions.


Assuntos
Cacau/química , Flavonoides/isolamento & purificação , Compostos Fitoquímicos/isolamento & purificação , Extração em Fase Sólida/métodos , Cromatografia Líquida de Alta Pressão , Flavonoides/toxicidade , Inocuidade dos Alimentos , Análise de Perigos e Pontos Críticos de Controle , Humanos , Compostos Fitoquímicos/toxicidade , Polifenóis/isolamento & purificação , Polifenóis/toxicidade , Proantocianidinas/isolamento & purificação , Proantocianidinas/toxicidade , Espectrometria de Massas por Ionização por Electrospray
19.
J Ethnopharmacol ; 231: 197-204, 2019 Mar 01.
Artigo em Inglês | MEDLINE | ID: mdl-30453050

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Serjania marginata Casar. (Sapindaceae) is a species traditionally known to be used for the treatment of gastric pain and inflammatory symptoms. AIM OF THIS STUDY: Due to the therapeutic importance of this species, this study investigated the toxicological effects of S. marginata leaves (AESM), after a single and a repeated exposure in rats. MATERIALS AND METHODS: For the acute toxicity test, 2000 mg/kg of AESM was administered to male and female rats by gavage, whereas for subacute toxicity test, 30, 150, or 750 mg/kg of AESM were used. RESULTS: No evidence of toxicity was observed in the animals acutely exposed to the extract, indicating that the LD50 is higher than 2000 mg/kg. After the repeated administration of AESM the hematological and biochemical parameters were unaltered, except the erythrocytes number and albumin levels in the exposed animals. Moreover, daily administration of this extract caused alteration on kidney histology. AESM also induced an increase of abnormal sperm, however the other reproductive parameters analyzed, in both sexes, were not altered by the treatment. CONCLUSION: Although AESM was not toxic after a single exposure, its use after prolonged periods affected some analyzed parameters, indicating that precautions should be taken when it is given over longer periods.


Assuntos
Extratos Vegetais/toxicidade , Sapindaceae , Animais , Contagem de Eritrócitos , Feminino , Rim/efeitos dos fármacos , Rim/patologia , Dose Letal Mediana , Masculino , Compostos Fitoquímicos/análise , Compostos Fitoquímicos/toxicidade , Extratos Vegetais/química , Folhas de Planta/química , Ratos Wistar , Sapindaceae/química , Espermatozoides/efeitos dos fármacos , Testes de Toxicidade Aguda , Testes de Toxicidade Subaguda
20.
Braz J Biol ; 79(3): 452-459, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-30379200

RESUMO

The study aimed to evaluate the antimicrobial activity, antioxidant, toxicity and phytochemical screening of the Red Propolis Alagoas. Antimicrobial activity was evaluated by disk diffusion method. Determination of antioxidant activity was performed using the DPPH assay (1.1-diphenyl-2-picrylhydrazyl), FTC (ferric thiocyanate) and determination of phenolic compounds by Follin method. Toxicity was performed by the method of Artemia salina and cytotoxicity by MTT method. The phytochemical screening for the detection of allelochemicals was performed. The ethanol extract of propolis of Alagoas showed significant results for antimicrobial activity, and inhibitory activity for Staphylococcus aureus and Candida krusei. The antioxidant activity of the FTC method was 80% to 108.3% hydrogen peroxide kidnapping, the DPPH method showed an EC50 3.97 mg/mL, the content of total phenolic compounds was determined by calibration curve gallic acid, resulting from 0.0005 mg/100 g of gallic acid equivalent. The extract was non-toxic by A. salina method. The propolis extract showed high activity with a higher percentage than 75% inhibition of tumor cells OVCAR-8, SF-295 and HCT116. Chemical constituents were observed as flavonones, xanthones, flavonols, and Chalcones Auronas, Catechins and leucoanthocyanidins. It is concluded that the extract can be tested is considered a potential source of bioactive metabolites.


Assuntos
Antibacterianos/farmacologia , Antifúngicos/farmacologia , Antineoplásicos/farmacologia , Antioxidantes/farmacologia , Própole/química , Brasil , Compostos Fitoquímicos/química , Compostos Fitoquímicos/toxicidade , Própole/toxicidade
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