RESUMEN

Difficulties encountered in treating drug-resistant pathogens have created a need for new therapies. Synergistic combinations of antibiotics are considered as ideal strategies in combating clinical and multidrug-resistant (MDR) infections. In this study, the antimicrobial activities of triterpenes and steroids from Ludwigia abyssinica A. Rich (Onagraceae) and their combined effects with antibiotics were assessed. The associations between plant constituents and antibiotics were evaluated by determining their fractional inhibitory concentrations (FICs). Sitost-5-en-3ß-ol formiate (1), 5α,6ß-dihydroxysitosterol (2), and maslinic acid (3) were isolated from the L. abyssinica ethyl acetate (EtOAc) extract. The EtOAc extract, compounds 1, 2, and 3 (MIC = 16-128 µg/mL) would be the best antibacterial and antifungal agents. The antimicrobial activities of amoxicillin were relatively weak against MDR Escherichia coli and Shigella flexneri and significant against Staphylococcus aureus ATCC 25923. However, when used in association with plant constituents, it displayed an interesting synergistic effect. Among plant components-antibiotic combinations, the EtOAc extract and compound 1 (steroid) showed a synergistic effect with amoxicillin/fluconazole against all the tested microorganisms whereas the association of compound 3 (triterpenoid) and amoxicillin/fluconazole displayed an additive effect against Shigella flexneri and Escherichia coli and a synergistic effect on Staphylococcus aureus, Cryptococcus neoformans, Candida tropicalis, and Candida albicans ATCC 10231. Overall, the results of the present study demonstrated antibacterial and antifungal activities of extracts and compounds isolated from L. abyssinica. The findings of the current study also showed that the potency of antibiotics was improved when screened in combination with L. abyssinica components, supporting the drug combination strategy to combat antimicrobial resistance.

RESUMEN

Phytochemicals present in medicinal plants (herbs, shrubs, and trees) are endowed with high antimicrobial and antioxidant properties. The aim of this work was to study the chemical composition, antioxidant, and antifungal activities of Tristemma mauritianum, Crassocephalum bougheyanum, and Lavigeria macrocarpa. Chemical composition of the plant extracts was determined using standard methods. The antioxidant activities were performed using 2,2-diphenyl-1-picrylhydrazyl (DPPH), ferric reducing antioxidant power (FRAP), nitric oxide (NO), and hydroxyl (OH) scavenging assays. The antifungal activity of plant extracts and their combinations with antifungals was evaluated against eleven Candida spp. using the broth microdilution method by determining the minimum inhibitory concentration (MIC) and minimum fungicidal concentration (MFC). The quantitative chemical analysis of the extracts of T. mauritianum, L. macrocarpa, and C. bougheyanum showed that they contain phenols, tannins, and flavonoids that vary according to the plant species and extracts. All the plant extracts presented promising antifungal (MIC = 64-2048 µg/mL) and antioxidant activities. The extract of T. mauritianum displayed the highest antifungal (MIC = 64-256 µg/mL) and antioxidant (IC50 = 19.052 ± 1.11 µg/mL) activities which can be explained by its high phenolic content. Interestingly, extracts of T. mauritianum, L. macrocarpa, and C. bougheyanum displayed synergistic effects (fractional inhibitory concentration index, FICI ≤ 0.5) with ketoconazole against clinical resistant isolates. The results of the present study demonstrate promising antifungal and antioxidant activities of the tested plants that are associated to their phenol, tannin, and flavonoid contents. Hence, extracts of T. mauritianum and L. macrocarpa could be deeply investigated as antifungal alone and in combination with conventional antifungal drugs to treat infections caused by Candida spp.

RESUMEN

Chemical investigation of the ethanol extract from the whole plant of Plectranthus glandulosus led to the isolation of a new nor-triterpenoid (1) along with seventeen known compounds (2-18) including seven triterpenoids, nine flavonoids and one steroid. Their structures were established on the basis of 1D- and 2D-NMR, IR, and MS experiments, and by comparison of their spectroscopic data with those of similar compounds reported in the literature. The EtOH extract and some isolated triterpenoids (1-4 and 13) were subjected to in vitro antimicrobial assays against a panel of pathogenic microorganisms, including Gram-positive and Gram-negative bacteria, and fungi using broth microdilution method. The EtOH extract displayed moderate activity (MIC = 512 µg/mL) against Staphylococcus aureus MSSA1, Shigella flexneri SDINT and Cryptococcus neoformans H99. Compounds 1, 4 and 13 showed the most potent antimicrobial effect with MICs of 32-256 µg/mL.

Asunto(s)

Antiinfecciosos , Lamiaceae , Plectranthus , Triterpenos , Antibacterianos/química , Antiinfecciosos/química , Antiinfecciosos/farmacología , Bacterias Gramnegativas , Bacterias Grampositivas , Pruebas de Sensibilidad Microbiana , Extractos Vegetales/química , Extractos Vegetales/farmacología , Plectranthus/química , Triterpenos/farmacología

RESUMEN

The treatment of infectious diseases with antimicrobial agents continues to present problems in modern-day medicine with many studies showing significant increase in the incidence of bacterial resistance to several antibiotics. The screening of antimicrobial activity of plant extracts and natural products has shown that medicinal plants are made up of a potential source of new anti-infective agents. The aim of this study was to evaluate the antimicrobial and antioxidant activities of extracts and compounds from the whole plant Trifolium baccarinii Chiov. and to determine their modes of antibacterial action. The plant extracts were prepared by maceration in organic solvents. The antimicrobial activities were evaluated using the broth microdilution method. The antioxidant activity was evaluated using the 2,2'-diphenyl-1-picrylhydrazyl radical (DPPH) and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) diammonium salt (ABTS) assays. The mechanisms of antibacterial action were determined by lysis, salt tolerance assays, and antioxidant enzyme activities. The cytotoxic effect on the erythrocytes was determined by a spectrophotometric method. Biochanin A, formononetin, luteolin, luteolin-4'-O-ß-D-glucopyranoside, 4,7,2'-trihydroxy-4'-methoxyisoflavanol, sissotrin, 1-methyl-ß-D-glucopyranoside, ononin, D-mannitol, and 3-O-ß-D-glucuronopyranosylsoyasapogenol B were isolated from Trifolium baccarinii. The MeOH, EtOAc, and n-BuOH extracts as well as biochanin A, formononetin, luteolin, luteolin-4'-O-ß-D-glucopyranoside, 4,7,2'-trihydroxy-4'-methoxyisoflavanol, and sissotrin from Trifolium baccarinii displayed the highest antimicrobial and antioxidant activities. The MeOH extract and 4,7,2'-trihydroxy-4'-methoxyisoflavanol exhibited antibacterial activity through the bacteriolytic effect and reduction of the antioxidant defenses in the bacterial cells. The present study portrays Trifolium baccarinii as a potential natural source of antibacterial, antifungal, and antioxidant agents.

Asunto(s)

Trifolium/química , Trifolium/metabolismo , Antibacterianos/química , Antiinfecciosos/química , Antiinfecciosos/aislamiento & purificación , Antiinfecciosos/farmacología , Antifúngicos/química , Antifúngicos/aislamiento & purificación , Antifúngicos/farmacología , Antioxidantes/química , Antioxidantes/aislamiento & purificación , Antioxidantes/farmacología , Infecciones Bacterianas , Fabaceae/química , Fabaceae/metabolismo , Flavonoides/química , Pruebas de Sensibilidad Microbiana , Extractos Vegetales/química , Extractos Vegetales/farmacología , Plantas Medicinales , Solventes/química

RESUMEN

BACKGROUND: Antibiotic resistance has contributed to the burden of infectious diseases both in the hospital and community setting, and represents a great threat to public health. Previous studies have revealed the role of reactive oxygen species as intermediate mediators of tissue damage, following antibiotherapies, indicating the need of associating antioxidants to these treatments. Therefore, the present work was designed to study the antibacterial, antifungal and antioxidant activities of extracts and compounds from Rumex abyssinicus Jacq. (Polygonaceae), as well as to investigate the antibacterial mechanisms of action of the most effective agents. METHODS: The plant extracts were prepared by maceration in organic solvents followed by column chromatography of the EtOAc fraction and purification of different fractions which led to the isolation and characterization of pure compounds. The antimicrobial activities of the extracts/compounds and their combinations with ciprofloxacin and fluconazole were evaluated using the broth microdilution method by determining the minimum inhibitory concentration (MIC) and minimum microbicidal concentration (MMC). The effects of the extracts on the bacterial cell membrane and microbial respiratory chain dehydrogenase enzyme activity were determined by spectrophotometric methods. Antioxidant activity was evaluated using 1,1-diphenyl-2-picrylhydrazyl (DPPH) and gallic acid equivalent antioxidant capacity (GAEAC) assays. RESULTS: Chrysophanol (1), physcion (2), Ergosta-6,22-diene-3,5,8-triol (3), emodin (4), 6-hydroxyemodin (citreorosein) (5), chrysophanein (6) and physcionin (7) were isolated from EtOAc fraction of R. abyssinicus and displayed different degrees of antimicrobial activities (MIC = 8-256 µg/mL). The MeOH extract and compounds 2 and 4 exhibited synergistic effects with ciprofloxacin and fluconazole. Compounds 1, 2 and the combined mixture of 6 + 7 displayed the highest antioxidant activity (GAEAC = 83.38-106.03 µg/mL). CONCLUSION: R. abyssinicus is a potential source of antibacterial, antifungal and antioxidant agents. The antibacterial mechanisms of action of the MeOH extract and compound 2 are due to disruption of the cytoplasmic membrane and inhibition of the microbial respiratory chain dehydrogenase enzyme activity. To the best of our knowledge, this is the first report of test samples and ciprofloxacin / fluconazole association against MDR strains. The observed activity of the isolated compounds against bacteria and fungi including MDR strains deserves further exploration.

Asunto(s)

Antiinfecciosos/farmacología , Antioxidantes/farmacología , Extractos Vegetales/farmacología , Rumex/química , Animales , Antiinfecciosos/química , Antioxidantes/química , Bacterias/efectos de los fármacos , Compuestos de Bifenilo/metabolismo , Supervivencia Celular/efectos de los fármacos , Eritrocitos/efectos de los fármacos , Hongos/efectos de los fármacos , Masculino , Fitoquímicos/química , Fitoquímicos/farmacología , Picratos/metabolismo , Extractos Vegetales/química , Ratas , Ratas Wistar

RESUMEN

BACKGROUND: Resistance of bacteria and fungi to antibiotics is one of the biggest problems that faces public health. The present work was designated to evaluate the antimicrobial activities of saponins from Melanthera elliptica and their synergistic effects with standard antibiotics against pathogenic phenotypes. The plant extract was prepared by maceration in methanol. The methanol extract was partitioned into ethyl acetate and n-butanol extracts. Column chromatography of the n-butanol extract followed by purification of different fractions led to the isolation of four saponins. Their structures were elucidated on the basis of spectra analysis, and by comparison with those from the literature. The antimicrobial activities of the extracts/compounds alone and their combinations with tetracycline and fluconazole were evaluated using the broth microdilution method through the determination of minimum inhibitory concentration (MIC) and minimum microbicidal concentration. RESULTS: Four compounds: 3-O-ß-D-glucuronopyranosyl-oleanolic acid (1), 3-O-ß-D-glucuronopyranosyloleanolic acid 28-O-ß-D-glucopyranosyl ester (2), 3-O-ß-D-glucopyranosyl(1 → 2)-ß-D-glucuronopyranosyl oleanolic acid (3) and 3-O-ß-D-glucopyranosyl(1 → 2)-ß-D-glucuronopyranosyl oleanolic acid 28-O-ß-D-glucopyranosyl ester (4) were isolated. Compounds 1, 2 and 3 showed the largest antibacterial activities (MIC = 8-128 µg/mL) whereas compound 4 displayed the highest antifungal activities (MIC = 8-16 µg/mL). The antibacterial activities of compounds 1 and 2 (MIC = 16-32 µg/mL) against multi-drug-resistant Escherichia coli S2 (1) and Shigella flexneri SDINT are equal to those of vancomycin (MIC = 16-32 µg/mL) used as reference antibiotic. CONCLUSIONS: The present study showed significant antimicrobial activity of compounds 1, 2, 3 and 4 against the tested microorganisms. The saponins act in synergy with the tested standard antibiotics. This synergy could lead to new options for the treatment of infectious diseases and emerging drug resistance.

RESUMEN

BACKGROUND: A series of recently reported phenolic azo dyes 7a-e were prepared by coupling the thienyl diazonium sulfate of 3-Amino-4H-benzo[f]thieno[3,4-c](2H)chromen-4-one with selected diversely substituted phenolic and naphtholic derivatives. These compounds were evaluated for their antibacterial and antifungal activities. Furthermore their voltammetric behavior was compared at a glassy carbon electrode. RESULTS: The voltammetric behavior of the five recently reported azo dyes has been compared at a glassy carbon electrode. It is shown that the azo dyes 7a-e with a hydroxyl group in the ortho position with respect to the azo bridge give rise to well defined, irreversible peaks for the oxidation and reduction process within a pH range of 2-7. The mechanisms of electrochemical oxidation of compound 7a-c and 7e are proposed. For the hydroxyl-substituted dyes, re-oxidation peaks were obtained in the subsequent scan. The antimicrobial activities of the reported compounds 7a-e along with the entire precursors 1-4 and 6a-e were performed against selected bacterial and fungal species and their activities compared to those of nystatin, griseofulvin and ciprofloxacin used as reference drugs. CONCLUSIONS: The present study showed significant antimicrobial activity of compounds 6d, 7a and 7c,e against the tested microorganisms; this result confirms the antimicrobial potency of azo compounds and some of their precursors.