RESUMEN
Bacterial multidrug resistance causes many therapeutic failures, making it more difficult to fight against bacterial diseases. This study aimed to investigate the antibacterial activity of extract, fractions, and phytochemicals from Plectranthus glandulosus (Lamiaceae) against multidrug-resistant (MDR) Gram-negative phenotypes expressing efflux pumps. The crude extract after extraction was subjected to column chromatography, and the structures of the isolated compounds were determined using spectrometric and spectroscopic techniques. Antibacterial assays of samples alone and in the presence of an efflux pump inhibitor (phenylalanine-arginine ß-naphthylamide, PAßN) were carried out using the broth microdilution method. The phytochemical study of P. glandulosus plant extract afforded seven major fractions (A-G) which lead to the isolation of seventeen known compounds. The ethanol extract of P. glandulosus was not active at up to 1024 µg/mL, whereas its fractions showed MICs varying from 32 to 512 µg/mL on the studied bacteria. Fraction C of P. glandulosus showed the lowest MIC (32 µg/mL) on E. coli ATCC8739 strain. Fraction D presented the highest activity spectrum by inhibiting the growth of 90% (9/10) of the studied bacteria. The presence of PAßN has improved the activity of extract and all fractions. Overall, the tested phytochemicals showed low activity against the studied bacteria. The overall results obtained in this study show that some fractions from P. glandulosus, mainly fractions C and D, should be investigated more for their possible use to fight against MDR bacteria.
Asunto(s)
Antibacterianos/farmacología , Bacterias Gramnegativas/efectos de los fármacos , Extractos Vegetales/farmacología , Plectranthus/química , Farmacorresistencia Bacteriana Múltiple/genética , Genes MDR , Bacterias Gramnegativas/genética , Pruebas de Sensibilidad MicrobianaRESUMEN
In order to contribute to the fight against infectious diseases, the in vitro antibacterial activity and the antibiotic-potentiating effects of Tristemma hirtum and five other Cameroonian edible plants have been evaluated against Gram-negative multidrug-resistant (MDR) phenotypes. The microdilution method was used to evaluate the bacterial susceptibility of the extracts and their combination to common antibiotics. The phytochemical screening of the extracts was carried out according to standard methods. Phytochemical analysis of the extracts revealed the presence of alkaloids, triterpenes, steroids, and polyphenols, including flavonoids in most of the tested extracts. The entire tested extracts showed moderate (512 µg/mL ≤ MIC ≤ 2048 µg/mL) to weak (MIC > 2048 µg/mL) antibacterial activities against the tested bacteria. Furthermore, extracts of leaf of Tristemma hirtum and pericarps of Raphia hookeri (at their MIC/2 and MIC/4) strongly potentiated the activities of all antibiotics used in the study, especially those of chloramphenicol (CHL), ciprofloxacin (CIP), kanamycin (KAN), and tetracycline (TET) against 70% (7/10) to 100% (10/10) of the tested MDR bacteria, with the modulating factors ranging from 2 to 128. The results of this study suggest that extracts from leaves of Tristemma hirtum and pericarps of Raphia hookeri can be sources of plant-derived products with antibiotic modifying activity.
Asunto(s)
Antiinfecciosos/farmacología , Farmacorresistencia Bacteriana Múltiple/efectos de los fármacos , Bacterias Gramnegativas/efectos de los fármacos , Melastomataceae/química , Extractos Vegetales/farmacología , Plantas Comestibles/química , Pruebas de Sensibilidad Microbiana , Fitoquímicos/químicaRESUMEN
This work was designed to investigate the antibacterial activities of methanol extracts from thirteen Cameroonian edible plants and their antibiotic-potentiating effects against Gram-negative multidrug-resistant (MDR) phenotypes. The broth microdilution method was used to evaluate the minimal inhibitory concentration (MIC) and minimal bactericidal concentration (MBC) of the extracts, as well as their antibiotic-potentiating activities. The phytochemical screening of the extracts was carried out according to the standard methods. The results of phytochemical tests revealed the presence of sterols, polyphenols, and tannins in most of the tested extracts, with the other classes of secondary metabolites being selectively distributed. Tested extracts showed variable antibacterial activities with MIC values ranging from 64 to 1024 µg/mL. However, some extracts were significantly active against certain bacterial strains: seeds extract of Theobroma cacao (64 µg/mL) against Escherichia coli AG100Atet and Klebsiella pneumoniae K24, and the bark extract of Uapaca guineensis against E. coli ATCC 8739. The leaves extract of T. cacao displayed the best MBC values (256 µg/mL) against E. aerogenes EA27. Some tested extracts included extracts from the leaves of T. cacao and P. vulgaris, and the seeds of D. edulis and barks A. indica has selectively improved (2- to 64-fold) the antibacterial activities of some of the tested antibiotics, chloramphenicol (CHL), tetracycline (TET), kanamycin (KAN), streptomycin (STR), and erythromycin (ERY), against more than 70% of tested MDR bacteria. The findings of this work showed that tested plant extracts and particularly those from T. cacao and Phaseolus vulgaris can be used alone or in combination with conventional antibiotics in the treatment of infections involving multiresistant bacteria.
Asunto(s)
Antibacterianos/farmacología , Bacterias Gramnegativas/efectos de los fármacos , Fenotipo , Extractos Vegetales/farmacología , Plantas Medicinales , Antibacterianos/aislamiento & purificación , Camerún , Farmacorresistencia Bacteriana Múltiple , Sinergismo Farmacológico , Bacterias Gramnegativas/fisiología , Humanos , Pruebas de Sensibilidad Microbiana/métodos , Corteza de la Planta , Extractos Vegetales/aislamiento & purificación , Hojas de la PlantaRESUMEN
BACKGROUND: Bacterial resistance to antibiotics is becoming a serious problem worldwide. The discovery of new and effective antimicrobials and/or resistance modulators is necessary to tackle the spread of resistance or to reverse the multi-drug resistance. We investigated the antibacterial and antibiotic-resistance modifying activities of the methanol extracts from Allanblackia gabonensis, Gladiolus quartinianus and Combretum molle against 29 Gram-negative bacteria including multi-drug resistant (MDR) phenotypes. METHODS: The broth microdilution method was used to determine the minimal inhibitory concentrations (MIC) and minimal bactericidal concentrations (MBC) of the samples meanwhile the standard phytochemical methods were used for the preliminary phytochemical screening of the plant extracts. RESULTS: Phytochemical analysis showed the presence of alkaloids, flavonoids, phenols and tannins in all studied extracts. Other chemical classes of secondary metabolites were selectively presents. Extracts from A. gabonensis and C. molle displayed a broad spectrum of activity with MICs varying from 16 to 1024 µg/mL against about 72.41% of the tested bacteria. The extract from the fruits of A. gabonensis had the best activity, with MIC values below 100 µg/mL on 37.9% of tested bacteria. Percentages of antibiotic-modulating effects ranging from 67 to 100% were observed against tested MDR bacteria when combining the leaves extract from C. molle (at MIC/2 and MIC/4) with chloramphenicol, kanamycin, streptomycin and tetracycline. CONCLUSION: The overall results of the present study provide information for the possible use of the studied plant, especially Allanblackia gabonensis and Combretum molle in the control of Gram-negative bacterial infections including MDR species as antibacterials as well as resistance modulators.
Asunto(s)
Antibacterianos/farmacología , Clusiaceae/química , Combretum/química , Farmacorresistencia Bacteriana Múltiple/efectos de los fármacos , Bacterias Gramnegativas/efectos de los fármacos , Iridaceae/química , Extractos Vegetales/farmacología , Pruebas de Sensibilidad MicrobianaRESUMEN
BACKGROUND: The rapid spread of bacteria expressing multi-drug resistance propels the search for new antibacterial agents. The present study was designed to evaluate the antibacterial activities of the methanol extracts from Beilschmiedia obscura and six other Cameroonian plants against a panel of twenty nine Gram-negative bacteria including Multi-drug resistant (MDR) phenotypes. METHODS: The phytochemical investigations of the extracts were carried out according to the standard methods and the liquid micro-dilution assay was used for all antibacterial assays. RESULTS: Phytochemical analysis showed the presence of alkaloids in all studied extracts. Other chemical classes of secondary metabolites such as anthocyanines, anthraquinones flavonoids, saponins, tannins, sterols and triterpenes were selectively detected in the extracts. The extract from the fruits of Beilschmiedia obscura, Pachypodanthium staudtii leaves and Peperomia fernandopoiana (whole plant) displayed the best spectrum of activity with MIC values ranging from 16 to 1024 µg/mL against at least 65% and above of the tested bacteria. The extract from Beilschmiedia obscura was the most active with MIC values below 100 µg/mL against ten of the tested bacteria. This extract also showed MBC values below 1024 µg/mL against 55.17% of the studied microorganisms. Phenylalanine arginine ß-naphthylamide (PAßN) significantly modulated the activities of extracts from the leaves and fruits of Pachypodanthium staudtii and Beilschmiedia obscura respectively, by increasing their inhibitory activity against Klebsiella pneumoniae KP55 strain at least four fold. CONCLUSION: The overall results of the present investigation provide information for the possible use of the methanol extracts of the studied plant species, especially B. obscura to fight infectious diseases caused by Gram-negative bacteria including MDR phenotypes.
Asunto(s)
Antibacterianos/farmacología , Bacterias Gramnegativas/efectos de los fármacos , Extractos Vegetales/farmacología , Plantas Medicinales/química , Alcaloides/química , Alcaloides/farmacología , Antibacterianos/química , Camerún , Dipéptidos/farmacología , Flavonoides/química , Flavonoides/farmacología , Lauraceae/química , Pruebas de Sensibilidad Microbiana , Extractos Vegetales/químicaRESUMEN
BACKGROUND: The continuous spread of multidrug-resistant (MDR) bacteria, partially due to efflux pumps drastically reduced the efficacy of the antibiotic armory, increasing the frequency of therapeutic failure. The search for new compounds to potentiate the efficacy of commonly used antibiotics is therefore important. The present study was designed to evaluate the ability of the methanol extracts of four Cameroonian dietary plants (Capsicum frutescens L. var. facilulatum, Brassica oleacera L. var. italica, Brassica oleacera L. var. butyris and Basilicum polystachyon (L.) Moench.) to improve the activity of commonly used antibiotics against MDR Gram-negative bacteria expressing active efflux pumps. METHODS: The qualitative phytochemical screening of the plant extracts was performed using standard methods whilst the antibacterial activity was performed by broth micro-dilution method. RESULTS: All the studied plant extracts revealed the presence of alkaloids, phenols, flavonoids, triterpenes and sterols. The minimal inhibitory concentrations (MIC) of the studied extracts ranged from 256-1024 µg/mL. Capsicum frutescens var. facilulatum extract displayed the largest spectrum of activity (73%) against the tested bacterial strains whilst the lower MIC value (256 µg/mL) was recorded with Basilicum polystachyon against E. aerogenes ATCC 13048 and P. stuartii ATCC 29916. In the presence of PAßN, the spectrum of activity of Brassica oleacera var. italica extract against bacteria strains increased (75%). The extracts from Brassica oleacera var. butyris, Brassica oleacera var. italica, Capsicum frutescens var. facilulatum and Basilicum polystachyon showed synergistic effects (FIC ≤ 0.5) against the studied bacteria, with an average of 75.3% of the tested antibiotics. CONCLUSION: These results provide promising information for the potential use of the tested plants alone or in combination with some commonly used antibiotics in the fight against MDR Gram-negative bacteria.
Asunto(s)
Antibacterianos/farmacología , Brassica/química , Capsicum/química , Bacterias Gramnegativas/efectos de los fármacos , Extractos Vegetales/farmacología , Alcaloides/farmacología , Antibacterianos/química , Camerún , Farmacorresistencia Microbiana , Sinergismo Farmacológico , Flavonoides/farmacología , Pruebas de Sensibilidad Microbiana , Ocimum basilicum/química , Extractos Vegetales/químicaRESUMEN
BACKGROUND: The flora of Saudi Arabia is one of the richest biodiversity areas in the Arabian Peninsula and comprises very important genetic resources of crop and medicinal plants. The present study was designed to investigate the cytotoxicity and the antibacterial activities of the organic extracts from twenty six Saudi Arabian medicinal plants. The study was also extended to the investigation of the effects of the extracts from the four best plants, Ononis serrata (SY160), Haplophyllum tuberculatum (SY177), Pulicaria crispa (SY179), and Achillea beiberstenii (SY-200) on cell cycle distribution, apoptosis, caspases activities and mitochondrial function in leukemia CCRF-CEM cell line. METHODS: A resazurin assay was used to assess the cytotoxicity of the extracts on a panel of human cancer cell lines whilst the microbroth dilution was used to determine the minimal inhibitory concentration (MIC) of the samples against twelve bacterial strains belonging to four species, Escherichia coli, Enterobacter aerogenes, Klebsiella pneumoniae and Pseudomonas aeruginosa. RESULTS: The best activity on leukemia cell lines were recorded with SY177 (IC50 of 9.94 µg/mL) and SY179 (IC50 of 1.81 µg/mL) against CCRF-CEM as well as Ach-b (IC50 of 9.30 µg/mL) and SY160 (IC50 of 5.06 µg/mL) against HL60 cells. The extracts from SY177 and SY179 were also toxic against the seven solid cancer cell lines studied with the highest IC50 values of 31.64 µg/mL (SY177 against Hep-G2 cells). SY177 and Ach-b induced cell cycle arrest in G0/G1 and S phases whilst SY160 and SY179 induced arrest in G0/G1 phase. All the four plant extracts induced apoptosis in CCRF-CEM cells with the alteration of the mitochondrial membrane potential. In the antibacterial assays, only Ach-b displayed moderate antibacterial activities against E. coli and E. aerogenes ATCC strains (MIC of 256 µg/mL), AG100A(TeT) and K. pneumoniae ATCC strains (MIC of 128 µg/mL). CONCLUSIONS: Finally, the results of the present investigation provided supportive data for the possible use of some Saudi Arabian plants investigated herein, and mostly Haplophyllum tuberculatum, Pulicaria crispa, Ononis serrata and Achillea beiberstenii in the control of cancer diseases.
Asunto(s)
Antibacterianos/farmacología , Extractos Vegetales/farmacología , Plantas Medicinales/química , Antibacterianos/química , Antineoplásicos/farmacología , Apoptosis/efectos de los fármacos , Caspasas/metabolismo , Ciclo Celular/efectos de los fármacos , Línea Celular Tumoral , Supervivencia Celular/efectos de los fármacos , Enterobacteriaceae/efectos de los fármacos , Humanos , Potencial de la Membrana Mitocondrial/efectos de los fármacos , Pruebas de Sensibilidad Microbiana , Extractos Vegetales/química , Pseudomonas/efectos de los fármacosRESUMEN
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.
Asunto(s)
Antibacterianos/farmacología , Bacterias Gramnegativas/efectos de los fármacos , Magnoliopsida , Extractos Vegetales/farmacología , Plantas Comestibles , Camerún , Dieta , Resistencia a Múltiples Medicamentos/efectos de los fármacos , Humanos , Pruebas de Sensibilidad MicrobianaRESUMEN
Medicinal plants have been used as a source of remedies since ancient times in Egypt. The present study was designed to investigate the antibacterial activity and the cytotoxicity of the organic extracts from 16 selected medicinal plants of Egypt. The study was also extended to the isolation of the antiproliferative compound jaeschkeanadiol p-hydroxybenzoate (FH-25) from Ferula hermonis. The microbroth dilution was used to determine the minimal inhibitory concentration (MIC) of the samples against twelve bacterial strains belonging to four species, Providencia stuartii, Pseudomonas aeruginosa, Klebsiella pneumoniae, and Escherichia coli, while a resazurin assay was used to assess the cytotoxicity of the extracts on the human pancreatic cancer cell line MiaPaCa-2, breast cancer cell line MCF-7, CCRF-CEM leukemia cells, and their multidrug resistant subline, CEM/ADR5000. The results of the MIC determination indicated that all the studied crude extracts were able to inhibit the growth of at least one of the tested bacterial species, the best activity being recorded with the crude extracts from F. hermonis and Vitis vinifera, whichwere active against 91.7% and 83.3% of the studied bacteria, respectively. The lowest MIC value of 128 µg/mL was recorded against P. stuartii ATCC 29916 and E. coli ATCC 10536 with the extract from V. vinifera and Commiphora molmol, respectively. In the cytotoxicity study, IC50 values below 20 µg/mL were recorded for the crude extract of F. hermonis on all four studied cancer cell lines. FH-25 also showed good cytotoxicity against MCF-7 cells (IC50: 2.47 µg/mL). Finally, the results of the present investigation provided supportive data for the possible use of the plant extracts investigated herein, mostly F. hermonis and V. vinifera in the treatment of bacterial infections and jaeschkeanadiol p-hydroxybenzoate in the control of cancer diseases.
Asunto(s)
Antibacterianos/farmacología , Antineoplásicos Fitogénicos/uso terapéutico , Ferula/química , Fitoterapia , Extractos Vegetales/uso terapéutico , Plantas Medicinales/química , Vitis/química , Antibacterianos/aislamiento & purificación , Antineoplásicos Fitogénicos/aislamiento & purificación , Antineoplásicos Fitogénicos/farmacología , Neoplasias de la Mama/tratamiento farmacológico , Línea Celular Tumoral , Resistencia a Antineoplásicos/efectos de los fármacos , Egipto , Escherichia coli/efectos de los fármacos , Femenino , Humanos , Concentración 50 Inhibidora , Klebsiella/efectos de los fármacos , Leucemia/tratamiento farmacológico , Magnoliopsida/química , Pruebas de Sensibilidad Microbiana , Extractos Vegetales/química , Extractos Vegetales/farmacología , Providencia/efectos de los fármacos , Pseudomonas/efectos de los fármacos , Sesquiterpenos/aislamiento & purificación , Sesquiterpenos/farmacología , Sesquiterpenos/uso terapéuticoRESUMEN
BACKGROUND: The emergence of multi-drug resistant (MDR) phenotypes is a major public health problem today in the treatment of bacterial infections. The present study was designed to evaluate the antibacterial activities of the methanol extracts of eleven Cameroonian spices on a panel of twenty nine Gram negative bacteria including MDR strains. METHODS: The phytochemical analysis of the extracts was carried out by standard tests meanwhile the liquid micro-broth dilution was used for all antimicrobial assays. RESULTS: Phytochemical analysis showed the presence of alkaloids, phenols and tannins in all plants extracts. The results of the antibacterial assays indicated that all tested extracts exert antibacterial activities, with the minimum inhibitory concentration (MIC) values varying from 32 to 1024 µg/ml. The extracts from Dichrostachys glomerata, Beilschmiedia cinnamomea, Aframomum citratum, Piper capense, Echinops giganteus, Fagara xanthoxyloïdes and Olax subscorpioïdea were the most active. In the presence of efflux pump inhibitor, PAßN, the activity of the extract from D. glomerata significantly increased on 69.2% of the tested MDR bacteria. At MIC/5, synergistic effects were noted with the extract of D. glomerata on 75% of the tested bacteria for chloramphenicol (CHL), tetracycline (TET) and norfloxacin (NOR). With B. cinnamomea synergy were observed on 62.5% of the studied MDR bacteria with CHL, cefepime (FEP), NOR and ciprofloxacin (CIP) and 75% with erythromycin (ERY). CONCLUSION: The overall results provide information for the possible use of the studied extracts of the spices in the control of bacterial infections involving MDR phenotypes.
Asunto(s)
Antibacterianos/farmacología , Farmacorresistencia Bacteriana Múltiple , Bacterias Gramnegativas/efectos de los fármacos , Extractos Vegetales/farmacología , Especias/análisis , Camerún , Interacciones Farmacológicas , Bacterias Gramnegativas/fisiología , Infecciones por Bacterias Gramnegativas/tratamiento farmacológico , Infecciones por Bacterias Gramnegativas/microbiología , Humanos , Pruebas de Sensibilidad Microbiana , Extractos Vegetales/análisis , Plantas Medicinales/químicaRESUMEN
ETHNOPHARMACOLOGICAL RELEVANCE: Infections due to multidrug-resistant (MDR) bacteria constitute a real problem in the public health worldwide. Hypericum roeperianum Schimp. ex A. Rich (Hypericaceae) is used traditionally for treatment of various ailments such as abdominal pains, constipation, diarrhea, indigestion, nausea, and bacterial diseases. AIM OF THE STUDY: This study was aimed at investigating the antibacterial and antibiotic-modifying activity of the crude methanol extracts (HRB), ethyl-acetate soluble fraction (HRBa), residual material (HRBb), and 11 compounds from the bark of Hypericum roeperianum against multi-drug resistant (MDR) bacteria expressing active efflux pumps. MATERIALS AND METHODS: The antibacterial activity, the efflux pump effect using the efflux pump inhibitor (EPI), phenylalanine-arginine-ß-naphthylamide (PAßN), as well as the antibiotic-modifying activity of samples were determined using the broth micro-dilution method. Spectrophotometric methods were used to evaluate the effects of HRB and 8,8-bis(dihydroconiferyl) diferulate (11) on bacterial growth, and bacterial membrane damage, whereas follow-up of the acidification of the bacterial culture was used to study their effects on bacteria proton-ATPase pumps. RESULTS: The crude extract (HRB), HRBa, and HRBb had selective antibacterial activity with MICs ranging from 16 to 512 µg/mL. Phytochemical 11 displayed the best antibacterial activity (0.5 ≤ MIC ≤ 2 µg/mL). The activity of HRB and 11 in the presence of EPI significantly increased on the tested bacteria strains (up to 32-fold). The activity of cloxacillin (CLO), doxycycline (DOX), and tetracycline (TET), was considerably improved (up to 64-fold) towards the multidrug-resistant Enterobacter aerogenes EA-CM64 strain. The crude extract (HRB) and 11 induced the leakage of bacterial intracellular components and inhibited the proton-ATPase pumps. CONCLUSIONS: The crude extract (HRB) and 8,8-bis(dihydroconiferyl)diferulate from the bark of Hypericum roeperianum are good antibacterial candidates that deserve further investigations to achieve antibacterial drugs to fight infections involving MDR bacteria.
Asunto(s)
Antibacterianos/farmacología , Bacterias/efectos de los fármacos , Hypericum/química , Extractos Vegetales/farmacología , Antibacterianos/administración & dosificación , Antibacterianos/aislamiento & purificación , Farmacorresistencia Bacteriana Múltiple , Sinergismo Farmacológico , Proteínas de Transporte de Membrana/metabolismo , Pruebas de Sensibilidad Microbiana , Fitoquímicos/administración & dosificación , Fitoquímicos/aislamiento & purificación , Fitoquímicos/farmacología , Corteza de la Planta , Extractos Vegetales/administración & dosificaciónRESUMEN
Two new furoquinoline alkaloids, maculine B (1) and kokusaginine B (2) and one new dihydrooxazole alkaloid, veprisazole (3), along with four known compounds namely, N13-methyl-3-methoxyrutaecarpine (4), flindersiamine (5), skimmianine (6) and tilianin (7) were isolated from the methanol extract of the stem bark of Araliopsis soyauxii Engl. by various chromatographic methods. Their structures were determined using spectrometry and spectroscopic techniques including NMR and MS. The cytotoxicity of the new compounds compared to that of doxorubicin, the reference anticancer compound, was determined on a panel of nine cancer cell lines including sensitive and drug resistant phenotypes. The three previously undescribed alkaloids displayed selective activities. Maculine B (1), the most active one among the newly described compounds, exhibited IC50 below 30⯵M against CCRF-CEM leukemia and U87MG glioblastoma cells.
Asunto(s)
Alcaloides/farmacología , Antineoplásicos Fitogénicos/farmacología , Corteza de la Planta/química , Rutaceae/química , Alcaloides/aislamiento & purificación , Antineoplásicos Fitogénicos/aislamiento & purificación , Camerún , Línea Celular Tumoral , Dioxoles , Resistencia a Múltiples Medicamentos/efectos de los fármacos , Resistencia a Antineoplásicos/efectos de los fármacos , Flavonoides , Furanos , Glicósidos , Humanos , Estructura Molecular , Fitoquímicos/aislamiento & purificación , Fitoquímicos/farmacología , QuinolinasRESUMEN
Allanblackia genus, an endless source of bioactive compounds, was investigated for its antibacterial properties. The chemical study of the methanol extract from the fruits of Allanblackia gabonensis resulted in the isolation of the undescribed guttiferone BL (1) along with the known kaempferol (2), morelloflavone (3), morelloflavone 7â³-O-ß-D-glucopyranoside (4), ß-sitosterol 3-O-ß-D-glucopyranoside and ß-sitosterol. Their structures were determined using spectrometry and spectroscopic techniques. The antibacterial activity was evaluated against five Gram-negative and two Gram-positive strains using a broth micro-dilution method. Compounds displayed low to significant activity against the tested bacterial strains with MICs ranging from 8 to 512 µg/mL. Morelloflavone (3) presented significant activity against E. coli ATCC8739 (MIC = 8 µg/mL) while guttiferone BL (1) exhibited low activity (MICs = 256-512 µg/mL) against all the tested strains. The crude extract also had moderate to significant activity against the tested bacterial strains.
Asunto(s)
Antibacterianos/farmacología , Benzofenonas/farmacología , Clusiaceae/química , Antibacterianos/química , Benzofenonas/aislamiento & purificación , Biflavonoides/aislamiento & purificación , Biflavonoides/farmacología , Evaluación Preclínica de Medicamentos/métodos , Escherichia coli/efectos de los fármacos , Frutas/química , Bacterias Gramnegativas/efectos de los fármacos , Bacterias Grampositivas/efectos de los fármacos , Quempferoles/aislamiento & purificación , Quempferoles/farmacología , Metanol/química , Pruebas de Sensibilidad Microbiana , Estructura Molecular , Extractos Vegetales/químicaRESUMEN
BACKGROUND: Cancer cells rapidly acquire resistance leading to treatment failures. In the present study, we have evaluated the cytotoxicity of 17 methanol extracts from 11 Cameroonian medicinal plants against the sensitive leukemia CCRF-CEM cells and the best ones were further tested on a panel of 8 other human cancer cell lines, including various MDR phenotypes as well as against the normal AML12 hepatocytes. METHODS: The cytotoxicity of the extracts was determined using a resazurin reduction assay meanwhile flow cytometry was used to measure cell cycle, apoptosis, mitochondrial membrane potential (MMP), and reactive oxygen species. RESULTS: In an initial screening using leukemia CCRF-CEM cells, ten extracts from five plants namely Alchornea floribunda, Annona muricata, Euphorbia prostata, Pachypodanthium staudtii and Passiflora edulis displayed IC50 values below 20 µg/mL. They were further tested in 8 other cell lines as well as in normal AML12 hepatocytes. All selected extracts were active against leukemia CEM/ADR5000 cells with IC50 value below 40 µg/mL. IC50 values ranging from 10.13 µg/mL (towards CEM/ADR5000 cells) to 72.01 µg/mL [towards resistant colon carcinoma HCT116 (p53-/-) cells] for Pachypodanthium staudtii roots and from 0.11 µg/mL (towards CCRF-CEM cells) to 108 µg/mL (towards P-glycoprotein-over-expressing CEM/ADR5000 cells) for doxorubicin were obtained in the eight other cancer cell lines studied. Extracts from Annona muricata leaves (AML) and seeds (AMS), and Passiflora edulis fruit (PEF) had IC50 values below 1 µg/mL against CCRF-CEM cells and below 10 µg/mL against its MDR subline CEM/ADR5000 cells. AML, AMS and PEF induced MMP-loss-mediated apoptosis in CCRF-CEM cells. CONCLUSIONS: Results of the present study suggest that some of the tested plants namely Alchornea floribunda, Annona muricata, Euphorbia prostata, Pachypodanthium staudtii and Passiflora edulis represent a source of anticancer drugs. Annona muricata and Passiflora edulis are good cytotoxic plants that could be exploited to develop phytomedicine to fight mostly hematological cancers including MDR phenotypes.
RESUMEN
BACKGROUND: Medicinal plants are used worldwide for several human ailments including bacterial infections. The present work was designed to assess the in vitro antibacterial activities of some Cameroonian medicinal plants including Entada abyssinica, Entada africana, Pentaclethra macrophylla, Allexis cauliflora, Anthocleista leibrechtsiana, Carapa procera, Carica papaya and Persea americana against Gram-negative bacteria expressing multidrug resistant (MDR) phenotypes. METHODS: The microbroth dilution was used to determine the minimal inhibitory concentration (MIC) and minimal bactericidal concentration (MBC) of the samples against eight bacterial strains belonging to four species, Escherichia coli, Enterobacter aerogenes, Klebsiella pneumoniae and Providencia stuartii. RESULTS: The extracts displayed selective antibacterial activities with the minimal inhibitory concentrations (MIC) values ranges of 64 to 1024 µg/mL. The most active extract was that from Pentaclethra macrophylla (TPM) that showed inhibitory activities against five of the eight (62.5%) tested bacteria. The lowest MIC value (64 µg/mL) was recorded with the crude extract of Entada africana against E. coli AG100A whilst the best MBC (256 µg/mL) value was also obtained with methanol extract of Persea americana against this bacterial strain. CONCLUSION: The results of the present work provide baseline information on the possible use of Pentaclethra macrophylla, Entada africana and Entada abyssinica in the treatment of selected bacterial infections.
Asunto(s)
Antibacterianos/farmacología , Farmacorresistencia Bacteriana Múltiple , Bacterias Gramnegativas/efectos de los fármacos , Infecciones por Bacterias Gramnegativas/tratamiento farmacológico , Extractos Vegetales/farmacología , Plantas Medicinales/química , Antibacterianos/química , Camerún , Humanos , Pruebas de Sensibilidad Microbiana , Extractos Vegetales/químicaRESUMEN
Introduction. The present study aims at evaluating the cytotoxicity of twelve parts from six Cameroonian medicinal plants on sensitive and drug-resistant cancer cell lines. We also studied the mode of action of the most active plants, Gladiolus quartinianus, Vepris soyauxii, and Anonidium mannii. Methods. The cytotoxicity of the extracts was determined using a resazurin assay. Flow cytometry was used for cell-cycle analysis and detection of apoptosis, analysis of mitochondrial membrane potential (MMP), and measurement of reactive oxygen species (ROS). Results. At 40 g/mL, three extracts showed a growth of CCRF-CEM leukemia cells by less than 50%. This includes the extracts from G. quartinianus (GQW; 25.69%), Vepris soyauxii leaves (VSL; 29.82%), and Anonidium mannii leaves (AML; 31.58%). The lowest IC50 values below 30 µ g/mL were obtained with GQW, AML and VSL against 7/9, 8/9, and 9/9 tested cancer cell lines, respectively. The lowest IC50 values for each plant were 4.09 µ g/mL, and 9.14 µ g/mL (against U87MG.ΔEGFR cells), respectively, for VSL and AML and 10.57 µ g/mL (against CCRF-CEM cells) for GQW. GQW induced cell cycle arrest between G0/G1 and S phases, whilst VSL and AML induced arrest in G0/G1. All three extracts induced apoptosis in CCRF-CEM cells by loss of MMP, whilst AML also enhanced production of ROS. Conclusion. The three active plants may be a source for the development of new anticancer drugs.
RESUMEN
The morbidity and mortality caused by bacterial infections significantly increased with resistance to commonly used antibiotics. This is partially due to the activation of efflux pumps in Gram-negative bacteria. The present work designed to assess the in vitro antibacterial activities of seven Cameroonian dietary plants (Sesamum indicum, Sesamum radiatum, Cinnamomum zeylanicum, Corchous olitorius, Cyperus esculentus, Adansonia digitata, Aframomum kayserianum), against multidrug resistant (MDR) Gram-negative bacteria over expressing active efflux pumps. The standard phytochemical methods were used to detect the main classes of secondary metabolites in the extracts. The antibacterial activities of the studied extracts in the absence or presence of an efflux pump inhibitor (PAßN) were evaluated using liquid microbroth dilution method. The results obtained indicated that apart from the extract of C. esculentus, all other samples contained alkaloids, phenols and polyphenols meanwhile other classes of chemicals were selectively present. The studied extracts displayed antibacterial activities with minimal inhibitory concentrations (MICs) values ranged from 64 to 1024 µg/mL on the majority of the 27 tested microbial strains. The extract of S. indicum was active against 77.77% of the tested microorganisms whilst the lowest MIC value (64 µg/mL) was recorded with that of A. kayserianum against E. aerogenes EA294. The results of the present work provide baseline information on the possible used of the tested Cameroonian dietary plants in the treatment of bacterial infections including multi-drug resistant phenotypes.
RESUMEN
BACKGROUND: The present work was designed to evaluate the antibacterial properties of the methanol extracts of eleven selected Cameroonian spices on multi-drug resistant bacteria (MDR), and their ability to potentiate the effect of some common antibiotics used in therapy. RESULTS: The extract of Cinnamomum zeylanicum against Escherichia coli ATCC 8739 and AG100 strains showed the best activities, with the lowest minimal inhibitory concentration (MIC) of 64 µg/ml. The extract of Dorstenia psilurus was the most active when tested in the presence of an efflux pump inhibitor, phenylalanine Arginine-ß- Naphtylamide (PAßN), a synergistic effect being observed in 56.25 % of the tested bacteria when it was combined with erythromycin (ERY). CONCLUSION: The present work evidently provides information on the role of some Cameroonian spices in the fight against multi-resistant bacteria.
Asunto(s)
Antibacterianos/farmacología , Bacterias/efectos de los fármacos , Metanol/química , Extractos Vegetales/farmacología , Solventes/química , Especias , Antibacterianos/química , Antibacterianos/aislamiento & purificación , Antibacterianos/metabolismo , Bacterias/crecimiento & desarrollo , Bacterias/metabolismo , Proteínas Bacterianas/metabolismo , Camerún , Farmacorresistencia Bacteriana Múltiple , Sinergismo Farmacológico , Pruebas de Sensibilidad Microbiana , Proteínas Asociadas a Resistencia a Múltiples Medicamentos/metabolismo , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación , Extractos Vegetales/metabolismo , Plantas MedicinalesRESUMEN
ETHNOPHARMACOLOGICAL RELEVANCE: Several medicinal plants and spices are used traditionally to treat cancers in Cameroon. AIM: Methanol extracts from thirty-four spices and plants, with related ethnobotanical use were investigated for their in vitro cytotoxicity on the human pancreatic cancer cell line MiaPaCa-2, leukemia CCRF-CEM cells and their multidrug resistant (MDR) subline CEM/ADR5000, and the normal human umbilical vein endothelial cells (HUVECs). In addition the anti-angiogenic properties of the most active extracts were investigated. MATERIAL AND METHODS: The MTS [3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium] assay was used for cytotoxic studies and the CAM-assay (chicken-chorioallantoic-membrane-assay) for anti-angiogenesis test. RESULTS: The results of the cytotoxicity tests indicated that, when tested at 20 µg/ml, extracts from Xylopia aethiopica, Echinops giganteus, Imperata cylindrica, Dorstenia psilirus and Piper capense were able to inhibit more that 50% the proliferation of the three tested cancer cells (MiaPaCa-2, CEM/ADR5000 CCRF-CEM). The lowest IC(50) values of 6.86 µg/ml on MiaPaCa-2 and 3.91 µg/ml on CCRF-CEM cells were obtained with X. aethiopica, while the corresponding value of 6.56 µg/ml was obtained with P. capense on CEM/ADR5000 cells. Against leukemia cells, no cross-resistance was observed with I. cylindrica, P. capense and Zinziber officinalis. Extracts from D. psilirus and E. giganteus were able to inhibit angiogenesis by more than 50% in quail embryo. CONCLUSION: The overall results of the present study provide supportive data on the use of some Cameroonian plants for cancer treatment.