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1.
BMC Complement Med Ther ; 23(1): 341, 2023 Sep 27.
Artigo em Inglês | MEDLINE | ID: mdl-37752510

RESUMO

BACKGROUND: Bauhinia thonningii is a plant traditionally used against many human diseases such as gastric ulcers, fever, inflammations, coughs, dysentery, diarrhea, and malaria. In the present investigation, the cytotoxicity of methanol extract of Bauhinia thonningii leaves (BTL), fractions and the isolated phytoconstituents was determined in a panel of 9 human cancer cell lines including drug sensitive and multidrug-resistant (MDR) phenotypes. The acute and sub-chronic oral toxicity of BTL was investigated as well. METHODS: Compounds were isolated using chromatographic techniques while their chemical structures were determined using spectroscopic methods. The resazurin reduction assay (RRA) was used to evaluate the cytotoxicity of samples, propidium iodide (PI) for apoptosis, 5,5',6,6'-tetrachloro-1,1',3,3'-tetraethylbenzimidazolylcarbocyanine iodide (JC-1) staining for mitochondrial membrane potential (MMP) analysis, 2´,7´-dichlorodihydrofluoresceine diacetate (H2DCFH-DA) staining for the quantification of reactive oxygen species (ROS), whereas Caspase Glo assays were combined by means of flow cytometry. Furthermore, the toxicological investigations were performed as recommended by the Organization for Economic Cooperation and Development (OECD). RESULTS: The botanicals as well as 6-C-methylquercetin-3,7-dimethyl ether (2), quercetin-3-O-L-rhamnopyranoside (5), quercetin-3-O-ß-glucopyranoside (6), 6,8-C-dimethylkaempferol 3,7-dimethyl ether (7), and 6,8-C-dimethylkaempferol-3-methyl ether (8) had promising cytotoxic effects in the 9 tested cancer cell lines. The IC50 values below 20 µg/mL (botanicals) or 10 µM (compounds) on at least 1/9 tested cancer cell lines were considered. The best cytotoxic effects with IC50 values below 5 µM were achieved with compounds 7 against CEM/ADR5000 leukemia cells (2.86 µM) and MDA-MB-231-pcDNA breast adenocarcinoma cells (1.93 µM) as well as 8 against CCRF-CEM leukemia cells (3.03 µM), CEM/ADR5000 cells (2.42 µM), MDA-MB-231-pcDNA (2.34 µM), and HCT116 p53-/- cells (3.41 µM). BTL and compound 8 induced apoptotic cell death in CCRF-CEM cells through caspase activation, alteration of MMP, and increased ROS production. BTL did not cause any adverse effects in rats after a single administration at 5000 mg/kg or a repeated dose of 250 mg/kg body weight (b. w.). CONCLUSION: Bauhinia thonningii and its constituents are sources of cytotoxic drugs that deserve more in-depth studies to develop novel antiproliferative phytomedicine to fight cancer including resistant phenotypes.


Assuntos
Bauhinia , Fabaceae , Leucemia , Humanos , Animais , Ratos , Quercetina , Espécies Reativas de Oxigênio , Caspases
2.
BMC Complement Med Ther ; 23(1): 48, 2023 Feb 15.
Artigo em Inglês | MEDLINE | ID: mdl-36793009

RESUMO

BACKGROUND: Cancer remains a global health concern and constitutes an important barrier to increasing life expectancy. Malignant cells rapidly develop drug resistance leading to many clinical therapeutic failures. The importance of medicinal plants as an alternative to classical drug discovery to fight cancer is well known. Brucea antidysenterica is an African medicinal plant traditionally used to treat cancer, dysentery, malaria, diarrhea, stomach aches, helminthic infections, fever, and asthma. The present work was designed to identify the cytotoxic constituents of Brucea antidysenterica on a broad range of cancer cell lines and to demonstrate the mode of induction of apoptosis of the most active samples. METHODS: Seven phytochemicals were isolated from the leaves (BAL) and stem (BAS) extract of Brucea antidysenterica by column chromatography and structurally elucidated using spectroscopic techniques. The antiproliferative effects of the crude extracts and compounds against 9 human cancer cell lines were evaluated by the resazurin reduction assay (RRA). The activity in cell lines was assessed by the Caspase-Glo assay. The cell cycle distribution, apoptosis via propidium iodide (PI) staining, mitochondrial membrane potential (MMP) through 5,5',6,6'-tetrachloro-1,1',3,3'-tetraethylbenzimidazolylcarbocyanine iodide (JC-1) staining, and the reactive oxygen species (ROS) via 2´,7´-dichlorodihydrofluoresceine diacetate (H2DCFH-DA) staining, were investigated by flow cytometry. RESULTS: Phytochemical studies of the botanicals (BAL and BAS) led to the isolation of seven compounds. BAL and its constituents 3, (3-(3-Methyl-1-oxo-2-butenyl))1H indole (1) and hydnocarpin (2), as well as the reference compound, doxorubicin, had antiproliferative activity against 9 cancer cell lines. The IC50 values varied from 17.42 µg/mL (against CCRF-CEM leukemia cells) to 38.70 µg/mL (against HCT116 p53-/- colon adenocarcinoma cells) for BAL, from 19.11 µM (against CCRF-CEM cells) to 47.50 µM (against MDA-MB-231-BCRP adenocarcinoma cells) for compound 1, and from 4.07 µM (against MDA-MB-231-pcDNA cells) to 11.44 µM (against HCT116 p53+/+ cells) for compound 2. Interestingly, hypersensitivity of resistant cancer cells to compound 2 was also observed. BAL and hydnocarpin induced apoptosis in CCRF-CEM cells mediated by caspase activation, the alteration of MMP, and increased ROS levels. CONCLUSION: BAL and its constituents, mostly compound 2, are potential antiproliferative products from Brucea antidysenterica. Other studies will be necessary in the perspective of the discovery of new antiproliferative agents to fight against resistance to anticancer drugs.


Assuntos
Adenocarcinoma , Antineoplásicos Fitogênicos , Brucea , Neoplasias do Colo , Simaroubaceae , Humanos , Extratos Vegetais/química , Metanol , Adenocarcinoma/tratamento farmacológico , Espécies Reativas de Oxigênio/metabolismo , Membro 2 da Subfamília G de Transportadores de Cassetes de Ligação de ATP , Proteína Supressora de Tumor p53 , Linhagem Celular Tumoral , Antineoplásicos Fitogênicos/química , Resistencia a Medicamentos Antineoplásicos , Neoplasias do Colo/tratamento farmacológico , Proteínas de Neoplasias/metabolismo , Proteínas de Neoplasias/farmacologia , Caspases/metabolismo
3.
J Ethnopharmacol ; 267: 113535, 2021 Mar 01.
Artigo em Inglês | MEDLINE | ID: mdl-33166626

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Araliopsis soyauxii Engl. (Rutaceae) is a Cameroonian medicinal plant traditionally used to treat lung diseases, malaria, and gonorrhea. It has been demonstrated that infectious disease contribute to about 20% of all human tumours. AIMS OF THE STUDY: (1) To perform a phytochemical investigation of the dichloromethane-methanol 1:1 extracts of the bark (ASB), roots (ASR), and leaves (ASL) from Araliopsis soyauxii; (2) to evaluate the cytotoxicity of extracts and isolated compounds; (3) to determine the mode of induction of apoptosis of ASB and kihadanin B (12). MATERIALS AND METHODS: Fourteen constituents of the crude extracts were isolated by column chromatography, while spectroscopic techniques were used for structural elucidation. The resazurin reduction assay (RRA) was applied to determine the cytotoxicity of samples towards a panel of 9 cancer cell lines. For caspases activity, the Caspase-Glo assay was used; flow cytometry was applied to investigate the cell cycle distribution (PI staining), apoptosis (annexin V/PI staining), mitochondrial membrane potential (MMP; JC-1 staining), and the reactive oxygen species (ROS; H2DCFH-DA staining). RESULTS: Phytochemical investigations of botanicals (ASB, ASR, and ASL) led to the isolation of 14 compounds. Extract ASB, obacunone (11), kihadanin B (12) as well as doxorubicin (control drug) revealed cytotoxicity towards the 9 cancer cell lines tested. The IC50 values ranged from 11.11 µg/mL (against CCRF-CEM leukemia cells) to 28.18 µg/mL (against HCT116 p53+/+ colon adenocarcinoma cells) for ASB; from 28.25 µM (against MDA-MB-231-pcDNA breast adenocarcinoma cells) to 65.13 µM (against HepG2 hepatocarcinoma cells) for compound 11, and from 5.77 µM (against CCRF-CEM cells) to 43.56 µM (against U87.MGΔEGFR glioblastoma cells) for compound 12. ASB and compound 12 induced apoptosis in CCRF-CEM cells. ASB induced the apoptotic process mediated by MMP alteration and enhanced ROS production, while compound 12 induced apoptosis by caspases activation, MMP alteration, and enhanced ROS production. CONCLUSION: This study demonstrated that Araliopsis soyauxii is a potential source of cytotoxic phytochemicals such as kihadanin B and that ASB and compound 12. Extract and compounds will be explored further to develop anticancer drugs.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Apoptose/efeitos dos fármacos , Neoplasias/tratamento farmacológico , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/farmacologia , Rutaceae , Antineoplásicos Fitogênicos/isolamento & purificação , Proteínas Reguladoras de Apoptose/metabolismo , Benzoxepinas/farmacologia , Pontos de Checagem do Ciclo Celular/efeitos dos fármacos , Relação Dose-Resposta a Droga , Células HCT116 , Células Hep G2 , Humanos , Concentração Inibidora 50 , Limoninas/farmacologia , Potencial da Membrana Mitocondrial/efeitos dos fármacos , Mitocôndrias/efeitos dos fármacos , Mitocôndrias/metabolismo , Mitocôndrias/patologia , Neoplasias/patologia , Estresse Oxidativo/efeitos dos fármacos , Compostos Fitoquímicos/isolamento & purificação , Extratos Vegetais/isolamento & purificação , Espécies Reativas de Oxigênio/metabolismo , Rutaceae/química , Transdução de Sinais
4.
BMC Complement Med Ther ; 20(1): 342, 2020 Nov 12.
Artigo em Inglês | MEDLINE | ID: mdl-33183278

RESUMO

BACKGROUND: Multidrug-resistant (MDR) bacteria remain a major cause of morbidity and mortality globally. The present study was designed to investigate the in vitro antibacterial activities of crude methanol extract and constituents isolated by Column Chromatography (CC) from Cassia sieberiana bark (CSB) against ten MDR Gram-negative bacteria, as well as the mechanisms of action of the most active sample. METHODS: The antibacterial activity of the tested samples (extract, the fractions and their compounds isolated by CC and the structures obtained by exploiting 1H and 13C Nuclear magnetic resonance (NMR) spectra) in the presence and absence of an efflux pumps inhibitor, phenylalanine-arginine ß-naphthylamide (PAßN), was evaluated using the micro-dilution method. The effects of the most active sample were evaluated on the cell growth kinetic and on the bacterial H+-ATPase proton pumps. RESULTS: Phytochemical composition of the crude extract showed a rather selective distribution of secondary metabolites (presence of polyphenols, tannins, steroids, triterpenes, flavonoids, alkaloids, saponins and absence of anthocyanins, anthraquinones). The tested samples displayed different antibacterial activities with minimal inhibitory concentrations (MICs) ranging from 64 to 512 µg/mL. Crude extract (CS) and fraction CSc showed the highest inhibitory spectra, both inhibiting all of the studied bacteria except Enterobacter aerogenes EA27 strain. Fraction CSc exerted bactericidal effects on most bacteria meanwhile, crude extract (CS) and sub-fraction CSc2 exerted bacteriostatic effects. Compounds 1 (spectaline) and 2 (iso-6-cassine) inhibited the growth of 70% (Escherichia coli ATCC8739 and AG102, Klebsiella pneumoniae ATCC11296, Enterobacter aerogenes ATCC13048 and EA27, Providencia stuartii ATCC29916, Pseudomonas aeruginosa PA01) and 60% (Escherichia coli ATCC8739, Klebsiella pneumoniae ATCC11296 and KP55, Providencia stuartii ATCC29916, Pseudomonas aeruginosa PA01 and PA124) of bacteria respectively with MICs ranging from 128 to 512 µg/mL. In the presence of PAßN, the activities of crude extract CS, fraction CAc and sub-fraction CSc2 strongly increased on most bacteria strains as their MICs significantly decreased. Sub-fraction CSc2 inhibited the H+-ATPase proton pumps and altered growth kinetic of Escherichia coli ATCC8739. CONCLUSION: The overall results justify the traditional use of C. sieberiana for the treatment of bacterial infections.


Assuntos
Antibacterianos/farmacologia , Cassia/química , Dipeptídeos/farmacologia , Bactérias Gram-Negativas/efeitos dos fármacos , Extratos Vegetais/farmacologia , Antibacterianos/química , Antibacterianos/metabolismo , Proteínas de Bactérias/antagonistas & inibidores , Proteínas de Bactérias/metabolismo , Farmacorresistência Bacteriana Múltipla , Bactérias Gram-Negativas/crescimento & desenvolvimento , Testes de Sensibilidade Microbiana , Casca de Planta/química , Extratos Vegetais/química , ATPases Translocadoras de Prótons/antagonistas & inibidores , ATPases Translocadoras de Prótons/metabolismo
5.
J Ethnopharmacol ; 190: 100-5, 2016 Aug 22.
Artigo em Inglês | MEDLINE | ID: mdl-27267830

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Harungana madagascariensis Lam. ex Poir. (Hypericaceae) is used in folk medicine to treat a variety of human ailments, mainly antibacterial, antifungal, antiviral and viral infections. In the present study, the methanol extract from the leaves (HML) and bark (HMB) of this plant as well as fractions (HMBa-c), sub-fractions (HMBa1-5) and compounds isolated from HMBa and HMBb namely betulinic acid (1), madagascin (2), ferruginin A (3) and Kaempferol-3-O-ß-d-glucopyranoside (4) were tested for their antimicrobial activities against a panel of 28 g-negative bacteria including multidrug resistant (MDR) phenotypes. MATERIALS AND METHODS: The broth microdilution method was used to determine the minimal inhibitory concentration (MIC) and minimal bactericidal concentration (MBC) of the above samples; column chromatography was used for the fractionation and purification of the bark extract whilst the chemical structures of compounds were determined using spectroscopic techniques. RESULTS: Crude extract HMB together with fraction HMBa and sub-fraction HMBa3 were active on the 28 tested bacterial strains. HML as well as fractions HMBb, HMBc and sub-fractions HMBa1, HMBa2, HMBa4 and HMBa5 were selectively active. MIC values below or equal to 1024µg/mL were recorded with these samples on 92.9% (for HML and HMBa 4), 82.1% (for HMBb), 78.6% (for HMBa2), 50.0% (for HMBa5) and 42.9% (for HMBc) tested bacteria. For crude material, the lowest MIC value below 8µg/mL was obtained with HMB against Escherichia coli ATCC10536 and W3110 strains, and with sub-fraction HMBa3 against Klebsiella pneumoniae K2 strains. MIC values below 10µg/mL were recorded with compound 3 against E. coli ATCC10536, Enterobacter aerogenes ATCC13048 and EA294, Pseudomonas aeruginosa PA01, K. pneumoniae K2 and Kp55 and Enterobacter cloacae BM67. CONCLUSIONS: Harungana madagascariensis is a potential source of antimicrobial drugs to fight against MDR bacteria. The anthranol 3 is the main antibacterial constituents of the bark of the plant. HMB and compound 3 deserve further investigations to develop natural drug to combat Gram-negative bacteria and otherwise MDR phenotypes.


Assuntos
Antibacterianos/farmacologia , Bactérias/efeitos dos fármacos , Clusiaceae/química , Metanol/química , Extratos Vegetais/farmacologia , Solventes/química , Antralina/isolamento & purificação , Antralina/farmacologia , Antraquinonas/isolamento & purificação , Antraquinonas/farmacologia , Antibacterianos/química , Antibacterianos/isolamento & purificação , Bactérias/crescimento & desenvolvimento , Farmacorresistência Bacteriana Múltipla , Hemiterpenos/isolamento & purificação , Hemiterpenos/farmacologia , Quempferóis/isolamento & purificação , Quempferóis/farmacologia , Testes de Sensibilidade Microbiana , Estrutura Molecular , Triterpenos Pentacíclicos , Fitoterapia , Casca de Planta , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Folhas de Planta , Plantas Medicinais , Triterpenos/isolamento & purificação , Triterpenos/farmacologia , Ácido Betulínico
6.
Fitoterapia ; 109: 206-11, 2016 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-26802608

RESUMO

A new dihydroflavonol-flavonol biflavonoid derivative, named ericoside was isolated from the ethanol extract of the whole plant of Erica mannii along with the known flavonoid, taxifolin 3-O-α-L-rhamnopyranoside; and two readily available sterols (sitosterol, sitosterol 3-O-ß-D-glucopyranoside). The isolation was performed using chromatographic methods and the structure of purified molecules were elucidated using spectroscopic techniques (e.g. MS, NMR) and by comparison with literature data. The crude ethanol extract, ericoside, and taxifolin 3-O-α-L-rhamnopyranoside were tested against ten Gram-negative bacteria including multidrug resistant clinical isolates using a broth microdilution method. The crude ethanol extract showed no noteworthy activity. Of the purified compounds, ericoside displayed moderate activity against the resistant Escherichia coli AG100 with a MIC of 64 µg/mL.


Assuntos
Antibacterianos/química , Biflavonoides/química , Ericaceae/química , Antibacterianos/isolamento & purificação , Biflavonoides/isolamento & purificação , Camarões , Escherichia coli/efeitos dos fármacos , Testes de Sensibilidade Microbiana , Estrutura Molecular , Extratos Vegetais/química
7.
BMC Complement Altern Med ; 15: 412, 2015 Nov 22.
Artigo em Inglês | MEDLINE | ID: mdl-26590804

RESUMO

BACKGROUND: The present study was designed to investigate the antibacterial activities of the methanol extracts from different parts of Beilschmedia acuta Kosterm (Lauraceae), Clausena anisata (Willd) Hook (Rutaceae), Newbouldia laevis Seem (Bignoniaceae) and Polyscias fulva (Hiern) Harms (Araliaceae) as well as their synergistic effects with antibiotics against a panel of Gram-negative bacteria, including multi-drug resistant (MDR) phenotypes expressing active efflux pumps. METHODS: Broth microdilution method was used to determine the minimum inhibitory concentrations (MICs) and the minimum bactericidal concentrations (MBCs) of the extracts, as well as those of antibiotics in association with the most active ones, B. acuta, N. laevis and P. fulva. RESULTS: MIC values obtained indicate that extracts from the bark of B. acuta were active on all the 26 tested Gram-negative bacteria, with MICs ranging from values below 8 to 256 µg/mL. Other samples displayed selective activities, their inhibitory effects being observed on 9 (34.62 %) of the 26 bacterial strains for N. laevis leaves extract, 6 (23.10 %) for both C. anisata leaves and roots extracts, 7 (26.9 %) and 4 (15.4 %) for leaves and roots extracts of P. fulva respectively. Extract from B. actua bark displayed the best antibacterial activity with MIC values below 100 µg/mL against 16 (61.5 %) of the 26 tested microorganisms. The lowest MIC values (below 8 µg/mL) were obtained with this extract against Escherichia coli W3110 and Klebsiella pneumoniae ATCC11296. The MIC values of this extract were lower than those of ciprofloxacin against E. coli W3110, Enterobacter aerogenes ATCC13048, CM64 and Providencia stuartii NAE16. At MIC/2, the best percentages of synergistic effects (100 %), were obtained with B. acuta bark extract and tetracycline (TET) as well as with P. fulva leaves extract and TET and kanamycin (KAN). CONCLUSION: The overall results of the present study provide information for the possible use of the studied plants and mostly Beilschmedia acuta in the control of bacterial infections including MDR phenotypes.


Assuntos
Antibacterianos/farmacologia , Araliaceae/química , Bignoniaceae/química , Clausena/química , Bactérias Gram-Negativas/efeitos dos fármacos , Lauraceae/química , Extratos Vegetais/farmacologia , Rutaceae/química , Antibacterianos/química , Ciprofloxacina/farmacologia , Farmacorresistência Bacteriana Múltipla/efeitos dos fármacos , Sinergismo Farmacológico , Canamicina/farmacologia , Metanol , Testes de Sensibilidade Microbiana , Extratos Vegetais/química , Folhas de Planta/química , Tetraciclina/farmacologia
8.
J Ethnopharmacol ; 169: 275-9, 2015 Jul 01.
Artigo em Inglês | MEDLINE | ID: mdl-25937257

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Fagara tessmannii is a shrub of the African rainforests used to treat bacterial infections, cancers, swellings and inflammation. In the present study, the methanol extract from the leaves (FTL), bark (FTB), and roots (FTR) of this plant as well as fractions (FTR1-5) and compounds isolated from FTR namely ß-sitosterol-3-O-ß-d-glucopyranoside (1), nitidine chloride (2) and buesgenine (3), were tested for their antimicrobial activities against a panel of Gram-negative bacteria including multidrug resistant (MDR) phenotypes. MATERIALS AND METHODS: The broth microdilution method was used to determine the minimal inhibitory concentration (MIC) and minimal bactericidal concentration (MBC) of the above samples; Column chromatography was used for the fractionation and purification of the roots extract whilst the chemical structures of compounds were determined using spectroscopic techniques. RESULTS: Results of the MIC determinations indicated that the crude extracts from the roots as well as fraction FTRa4 were active on all the 26 tested bacterial strains. MIC values below 100µg/mL were obtained with roots, leaves and bark extract respectively against 30.8%, 15.4% and 11.5% tested bacteria. The lowest MIC value below of 8µg/mL was obtained with extract from the roots against Escherichia coli MC100 strain. The lowest MIC value of 4µg/mL was also obtained with compound 3 against E. coli AG102 and Klebsiella pneumoniae ATCC11296 CONCLUSIONS: The present study demonstrates that F. tessmannii is a potential source of antimicrobial drugs to fight against MDR bacteria. Benzophenanthrine alkaloids 2 and 3 are the main antibacterial consituents of the roots of the plant.


Assuntos
Antibacterianos/farmacologia , Metanol/química , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Zanthoxylum/química , Benzofenantridinas/isolamento & purificação , Benzofenantridinas/farmacologia , Glucosídeos/isolamento & purificação , Glucosídeos/farmacologia , Testes de Sensibilidade Microbiana , Fenantridinas/isolamento & purificação , Fenantridinas/farmacologia , Casca de Planta/química , Folhas de Planta/química , Raízes de Plantas/química , Sitosteroides/isolamento & purificação , Sitosteroides/farmacologia
9.
Nat Prod Res ; 29(10): 921-5, 2015.
Artigo em Inglês | MEDLINE | ID: mdl-25220189

RESUMO

A new unprecedented cinnamate derivative (1) was obtained from Erythrina excelsa (Leguminosae) and identified as nonadecyl para-hydroperoxycinnamate. This compound was isolated together with three known compounds, namely lupeol (2), mixture of sitosterol and stigmasterol (3), and isoneorautenol (4). Their structures were established on the basis of NMR and mass spectroscopic data in conjunction with those reported in the literature. Compound 1 was evaluated for its capability of inhibiting cancer cell lines and growth of a panel of microbial strains. It turned out that 1 is moderately to significantly cytotoxic against six cancer cell lines and shows weak to no antimicrobial activity.


Assuntos
Antibacterianos/química , Antineoplásicos Fitogênicos/química , Cinamatos/química , Erythrina/química , Antibacterianos/isolamento & purificação , Antineoplásicos Fitogênicos/isolamento & purificação , Linhagem Celular Tumoral , Cinamatos/isolamento & purificação , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Espectroscopia de Ressonância Magnética , Espectrometria de Massas , Estrutura Molecular , Casca de Planta/química , Extratos Vegetais/química
10.
Chin J Integr Med ; 20(7): 546-54, 2014 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-24972582

RESUMO

OBJECTIVE: To evaluate the in vitro antibacterial properties and the ability to potentiate some common antibiotics effects of the methanol extracts of 11 Cameroonian food plants on 29 Gram-negative bacteria expressing multidrug resistant (MDR) phenotypes. METHODS: The antimicrobial activity of the extracts was performed using the broth microdilution method. The phytochemical screening of these extracts was also performed using standard methods. RESULTS: Ocimum basilicum, Gnetum africanum and Eucalyptus robusta extracts possessed an antibacterial activity against all the 29 studied bacteria. The extracts from G. africanum and E. robusta were the most active with the lowest minimal inhibitory concentration of 64 µg/mL on Escherichia coli AG100A for both extracts and also against Klebsiella pneumoniae K24 for G. africanum. When tested in the presence of phenylalanine-arginine ß-Naphtylamide (PAßN), an efflux pump inhibitor, the extract of Thymus vulgaris and E. Robusta showed the best activities on most tested strains. E. Robusta extract showed good synergistic effects, improving the activity of commonly used antibiotics in about 85% of cases. CONCLUSION: The overall results obtained provide the baseline information for the use of the tested plants in the treatment of bacterial infections.


Assuntos
Antibacterianos/farmacologia , Resistência a Múltiplos Medicamentos/efeitos dos fármacos , Bactérias Gram-Negativas/efeitos dos fármacos , Infecções por Bactérias Gram-Negativas/tratamento farmacológico , Medicinas Tradicionais Africanas/métodos , Preparações de Plantas/farmacologia , Camarões , Eucalyptus/química , Gnetum/química , Infecções por Bactérias Gram-Negativas/microbiologia , Humanos , Testes de Sensibilidade Microbiana , Ocimum basilicum/química , Fitoterapia/métodos , Plantas Comestíveis/química
11.
J Ethnopharmacol ; 153(1): 207-19, 2014 Apr 11.
Artigo em Inglês | MEDLINE | ID: mdl-24583070

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Beilschmiedia acuta Kosterm, Clausena anisata (Willd) Hook, Fagara tessmannii Engl., Newbouldia laevis Seem., and Polyscias fulva (Hiern) Harms. are medicinal plants used in Cameroonian traditional medicine in the treatment of various types of cancers. The present study aims at investigating 11 methanolic extracts from the above Cameroonian medicinal plants on a panel of human cancer cell lines, including various drug-resistant phenotypes. Possible modes of action were analyzed for two extracts from Beilschmiedia acuta and Polyscia fulva and alpha-hederin, the representative constituent of Polyscia fulva. MATERIALS AND METHODS: Cytotoxicity was determined using a resazurin assay. Cell cycle, apoptosis, mitochondrial membrane potential (MMP), and reactive oxygen species (ROS) were measured by flow cytometry. Cellular response to alpha-hederin was investigated by a mRNA microarray approach. RESULTS: Prescreening of extracts (40µg/mL) showed that three of eleven plant extracts inhibited proliferation of CCRF-CEM cells by more than 50%, i.e. BAL (73.65%), the bark extract of Beilschmiedia acuta (78.67%) and PFR (68.72%). Subsequent investigations revealed IC50 values below or around 30µg/mL of BAL and PFR in 10 cell lines, including drug-resistant models, i.e. P-glycoprotein-overexpressing CEM/ADR5000, breast cancer resistance protein-transfected MDA-MB-231-BCRP, TP53 knockout cells (HCT116 p53(-/-)), and mutation-activated epidermal growth factor receptor-transfected U87MG.ΔEGFR cells. IC50 values below 5µg/mL of BAL were obtained for HCT116 (p53(-/-)) cells. IC50 values below 10µM of alpha-hederin were found for sensitive CCRF-CEM and multidrug-resistant CEM/ADR5000 cells. The BAL and PFR extracts induced cell cycle arrest between G0/G1 and S phases. PFR-induced apoptosis was associated with increased ROS generation and MMP breakdown. Microarray-based cluster analysis revealed a gene expression profile that predicted cellular response to alpha-hederin. CONCLUSION: BAL, PFL and alpha-hederin, an exemplarily taken constituent of Beilschmiedia acuta and Polyscia fulva extracts revealed cytotoxicity towards cancer cell lines. Hence, Beilschmiedia acuta and Polyscia fulva may be valuable to develop drugs against otherwise drug-resistant cancer cells.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Neoplasias/tratamento farmacológico , Extratos Vegetais/farmacologia , Plantas Medicinais/química , Antineoplásicos Fitogênicos/administração & dosagem , Apoptose/efeitos dos fármacos , Camarões , Pontos de Checagem do Ciclo Celular/efeitos dos fármacos , Linhagem Celular Tumoral , Resistencia a Medicamentos Antineoplásicos , Humanos , Concentração Inibidora 50 , Potencial da Membrana Mitocondrial/efeitos dos fármacos , Neoplasias/patologia , Extratos Vegetais/administração & dosagem
12.
BMC Complement Altern Med ; 13: 164, 2013 Jul 10.
Artigo em Inglês | MEDLINE | ID: mdl-23837916

RESUMO

BACKGROUND: In response to the propagation of bacteria resistant to many antibiotics also called multi-drug resistant (MDR) bacteria, the discovery of new and more efficient antibacterial agents is primordial. The present study was aimed at evaluating the antibacterial activities of seven Cameroonian dietary plants (Adansonia digitata, Aframomum alboviolaceum, Aframomum polyanthum, Anonidium. mannii, Hibiscus sabdarifa, Ocimum gratissimum and Tamarindus indica). METHODS: The phytochemical screening of the studied extracts was performed using described methods whilst the liquid broth micro dilution was used for all antimicrobial assays against 27 Gram-negative bacteria. RESULTS: The results of the phytochemical tests indicate that all tested extracts contained phenols and triterpenes, other classes of chemicals being selectively present. The studied extracts displayed various degrees of antibacterial activities. The extracts of A. digitata, H. sabdarifa, A. polyanthum, A. alboviolaceum and O. gratissimum showed the best spectra of activity, their inhibitory effects being recorded against 81.48%, 66.66%, 62.96%, 55.55%, and 55.55% of the 27 tested bacteria respectively. The extract of A. polyanthum was very active against E. aerogenes EA294 with the lowest recorded minimal inhibitory concentration (MIC) of 32 µg/ml. CONCLUSION: The results of the present work provide useful baseline information for the potential use of the studied edible plants in the fight against both sensitive and MDR phenotypes.


Assuntos
Antibacterianos/farmacologia , Bactérias Gram-Negativas/efeitos dos fármacos , Magnoliopsida , Extratos Vegetais/farmacologia , Plantas Comestíveis , Camarões , Dieta , Resistência a Múltiplos Medicamentos/efeitos dos fármacos , Humanos , Testes de Sensibilidade Microbiana
13.
Artigo em Inglês | MEDLINE | ID: mdl-22474511

RESUMO

The present work was designed to assess the antibacterial properties of the methanol extracts of some Cameroonian medicinal plants and the effect of their associations with currently used antibiotics on multidrug resistant (MDR) Gram-negative bacteria overexpressing active efflux pumps. The antibacterial activities of twelve methanol extracts of medicinal plants were evaluated using broth microdilution. The results of this test showed that three extracts Garcinia lucida with the minimal inhibitory concentrations (MIC) varying from 128 to 512 µg/mL, Garcinia kola (MIC of 256 to 1024 µg/mL), and Picralima nitida (MIC of 128 to 1024 µg/mL) were active on all the twenty-nine studied bacteria including MDR phenotypes. The association of phenylalanine arginine ß-naphthylamide (PAßN or efflux pumps inhibitor) to different extracts did not modify their activities. At the concentration of MIC/2 and MIC/5, the extracts of P. nitida and G. kola improved the antibacterial activities of some commonly used antibiotics suggesting their synergistic effects with the tested antibiotics. The results of this study suggest that the tested plant extracts and mostly those from P. nitida, G. lucida and G. kola could be used alone or in association with common antibiotics in the fight of bacterial infections involving MDR strains.

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