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1.
J Sci Food Agric ; 102(12): 5200-5209, 2022 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-35289954

RESUMEN

BACKGROUND: In this study, the optimal conditions for the extraction and purification of glycyrrhizic acid from Radix Glycyrrhizae (RG) and baicalein and wogonin from Radix Scutellariae (RS) by foam fractionation were studied on the basis of central composite design (CCD) and response surface methodology. RESULTS: The results showed that herbal proportion (RG:RS), gas flow and ethanol concentration were the main factors guiding the foam fractionation of RG and RS. The optimum technological parameters were obtained as follows: herbal proportion (RG:RS), 1.86:1.14; gas flow, 109 mL min-1 ; and ethanol concentration, 53%. Under the optimal operating conditions, the maximal extraction yields of baicalein, glycyrrhizic acid and wogonin were 56.67, 13.25 and 9.51 mg g-1 , respectively, which were 2.32-, 1.22- and 1.84-fold higher than those of ultrasonic extraction and 17.28-, 1.15- and 9.91-fold higher than those of ultrasonic extraction without hydrolysis, respectively. Investigations on the antioxidant activity showed that the foam-fractionated extract exhibited better free radical scavenging activity (IC50 13.80 µg mL-1 ) than that of the ultrasonic extract (IC50 223.00 µg mL-1 ). Antibacterial activity showed that the minimum inhibitory concentrations of the foam fractionated extract against Staphylococcus aureus, Candida albicans, Group A Streptococcus and Pseudomonas aeruginosa were 1.38, 1.38, 0.69 and 5.50 mg mL-1 , respectively. CONCLUSION: The results indicate that the foam fractionated extract exhibited better extraction yields and free radical scavenging activity than did the ultrasonic extract. Therefore, this fast and eco-friendly method was established and could be a basis for the extraction and separation of other active constituents from herbal medicines. © 2022 Society of Chemical Industry.


Asunto(s)
Medicamentos Herbarios Chinos , Flavanonas , Scutellaria , Medicamentos Herbarios Chinos/farmacología , Etanol , Flavonoides , Radicales Libres , Ácido Glicirrínico , Extractos Vegetales/farmacología , Scutellaria baicalensis
2.
J Clin Tuberc Other Mycobact Dis ; 27: 100307, 2022 May.
Artículo en Inglés | MEDLINE | ID: mdl-35284659

RESUMEN

Background: Imperative need exists to search for new anti-TB drugs that are safer, and more effective against drug-resistant strains. Medicinal plants have been the source of active ingredients for drug development. However, the slow growth and biosafety level requirements of M. tuberculosis culture are considerable challenges. M. smegmatis can be used as a surrogate for M. tuberculosis. In the current study, preliminary phytochemical screening and antimycobacterial activity evaluation of crude methanolic extracts of medicinal plants against M. smegmatis, and two M. tuberculosis strains, were conducted. Materials and Methods: Crude methanolic extracts, obtained from the leaves of L. camara, roots of C. sanguinolenta, and stem barks of Z. leprieurii, were tested for antimycobacterial activity against M. smegmatis (mc2155), pan-sensitive (H37Rv), and rifampicin-resistant (TMC-331) M. tuberculosis, using visual Resazurin Microtiter Assay (REMA) on 96 well plates. Preliminary qualitative phytochemical screening tests were performed using standard chemical methods. Results: The three methanolic extracts inhibited mycobacterial growth in vitro. They were more active against rifampicin-resistant strain with MICs of 176, 97, and 45 µg/mL for L. camara, C. sanguinolenta, and Z. leprieurii extracts, respectively. The lowest activity was observed against M. smegmatis with MICs of 574, 325, and 520 µg/mL, respectively. Against H37Rv, activity was intermediate to those of TMC-331 and mc2155. However, L. camara extract showed the same activity against H37Rv and M. smegmatis. Preliminary phytochemical analysis revealed alkaloids, flavonoids, phenolic compounds, saponins, tannins, and terpenoids. Conclusions: Leaves of L. camara, roots of C. sanguinolenta, and stem barks of Z. leprieurii exhibit antimycobacterial activity against M. smegmatis, pan-sensitive, and rifampicin-resistant M. tuberculosis. This offers the possibilities for novel therapeutic opportunities against TB including multidrug-resistant TB. Further investigations on safety and mechanisms of action are required. These studies could be done using M. smegmatis as a surrogate for the highly pathogenic M. tuberculosis.

3.
Microbiol Spectr ; 9(3): e0190821, 2021 12 22.
Artículo en Inglés | MEDLINE | ID: mdl-34908432

RESUMEN

Aztreonam-avibactam is under clinical development for multidrug-resistant Gram-negative infections. We evaluated in vitro activity against 341 recent clinical isolates. The addition of avibactam to aztreonam had no effect on the anaerobic activity of aztreonam. IMPORTANCE This work shows that aztreonam-avibactam lacks activity against anaerobic organisms.


Asunto(s)
Antibacterianos/farmacología , Aztreonam/farmacología , Bacterias Anaerobias/efectos de los fármacos , Infecciones Bacterianas/microbiología , Compuestos de Azabiciclo/farmacología , Bacterias Anaerobias/clasificación , Bacterias Anaerobias/genética , Bacterias Anaerobias/aislamiento & purificación , Evaluación Preclínica de Medicamentos , Humanos , Pruebas de Sensibilidad Microbiana
4.
Molecules ; 25(8)2020 Apr 24.
Artículo en Inglés | MEDLINE | ID: mdl-32344703

RESUMEN

Kava extract, an aqueous rhizome emulsion of the plant Piper methysticum, has been used for centuries by Pacific Islanders as a ceremonial beverage, and has been sold as an anxiolytic agent for some decades. Kavalactones are a major constituent of kava extract. In a previous investigation, we had identified three kavalactones that inhibit larval development of Haemonchus contortus in an in vitro-bioassay. In the present study, we synthesized two kavalactones, desmethoxyyangonin and yangonin, as well as 17 analogues thereof, and evaluated their anthelmintic activities using the same bioassay as employed previously. Structure activity relationship (SAR) studies showed that a 4-substituent on the pendant aryl ring was required for activity. In particular, compounds with 4-trifluoromethoxy, 4-difluoromethoxy, 4-phenoxy, and 4-N-morpholine substitutions had anthelmintic activities (IC50 values in the range of 1.9 to 8.9 µM) that were greater than either of the parent natural products-desmethoxyyangonin (IC50 of 37.1 µM) and yangonin (IC50 of 15.0 µM). The synthesized analogues did not exhibit toxicity on HepG2 human hepatoma cells in vitro at concentrations of up to 40 µM. These findings confirm the previously-identified kavalactone scaffold as a promising chemotype for new anthelmintics and provide a basis for a detailed SAR investigation focused on developing a novel anthelmintic agent.


Asunto(s)
Antihelmínticos/síntesis química , Antihelmínticos/farmacología , Haemonchus/efectos de los fármacos , Kava/química , Animales , Relación Dosis-Respuesta a Droga , Larva/efectos de los fármacos , Estructura Molecular , Pruebas de Sensibilidad Parasitaria
5.
Artículo en Inglés | MEDLINE | ID: mdl-31307986

RESUMEN

The use of antifungal agents in clinical settings is limited by the appearance of drug resistance and adverse side effects. There is, therefore, an urgent need to develop new drugs to strengthen the treatment of invasive fungal diseases. The aim of this study is to describe the potential repurposing of ribavirin as an adjunct therapy against Candida spp. Primary screening of a Prestwick Chemical library against Candida albicans ATCC 90028 and fluconazole-resistant Candida albicans strains was performed. Subsequently, we evaluated the responses of 100 Candida sp. strains to ribavirin, an antiviral agent, using the broth microdilution method as recommended by CLSI. We checked the involvement of efflux pump activity in the development of ribavirin resistance. We studied time-kill curves and performed a checkerboard assay for a ribavirin-antifungal combination study. Twenty-one nonstandard antifungal compounds were identified, including ribavirin. Ribavirin had antifungal activity in vitro against 63 Candida strains, including strains of C. albicans, C. parapsilosis, and C. tropicalis, with MICs ranging from 0.37 to 3.02 µg/ml, while MICs for C. krusei, C. glabrata, C. lusitaniae, and some C. albicans strains remained high (≥24.16 µg/ml). No relation was observed between efflux pump activity and ribavirin resistance. Ribavirin exhibited fungistatic activity against multidrug-resistant (MDR) C. albicans and fungicidal activity against a C. parapsilosis strain. In addition, ribavirin acted synergistically with azoles against Candida strains for which ribavirin MICs were <24.4 µg/ml. This study highlights the potential clinical application of ribavirin, alone or in association with other antifungal agents, as an adjunct anti-Candida drug.


Asunto(s)
Antifúngicos/farmacología , Candida albicans/efectos de los fármacos , Candida parapsilosis/efectos de los fármacos , Candida tropicalis/efectos de los fármacos , Reposicionamiento de Medicamentos , Farmacorresistencia Fúngica/efectos de los fármacos , Ribavirina/farmacología , Candida albicans/genética , Candida albicans/crecimiento & desarrollo , Candida parapsilosis/genética , Candida parapsilosis/crecimiento & desarrollo , Candida tropicalis/genética , Candida tropicalis/crecimiento & desarrollo , Candidiasis Invasiva/tratamiento farmacológico , Candidiasis Invasiva/microbiología , Sinergismo Farmacológico , Fluconazol/farmacología , Expresión Génica , Genes MDR , Humanos , Pruebas de Sensibilidad Microbiana , Medicamentos bajo Prescripción/farmacología , Triazoles/farmacología
6.
Lett Appl Microbiol ; 69(1): 41-49, 2019 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-31044446

RESUMEN

Plumbagin (5-hydroxy-2-methyl-1,4-napthoquinone) is a bicyclic naphthoquinone, found in three major plant families viz. Plumbaginaceae, Ebenceae and Droseraceae. The phytochemical is reported to exhibit various pharmacological properties. In this study, plumbagin isolated from Plumbago zeylanica L. was investigated for its in vitro activity against methicillin-resistant Staphylococcus aureus (MRSA). Against 100 MRSA isolates that included multi-drug-resistant phenotypes, plumbagin showed consistent activity with a narrow minimum inhibitory concentration (MIC) range of 4-8 µg ml-1 . The time-kill study revealed 99% kill of a reference MRSA strain, 8 h after exposure to plumbagin. In the combination MIC study using the reference MRSA strain, plumbagin showed synergistic effect with ciprofloxacin and piperacillin while additive or indifference effect with other commonly used antibiotics. The transmission electron micrograph of the reference MRSA strain treated with plumbagin confirmed cell wall and cytoplasmic changes. Our results demonstrated potent anti-MRSA activity of plumbagin which was not impacted by multi-drug resistance. This is a first ever study that evaluated in vitro anti-MRSA activity of plumbagin employing large number of MRSA isolates. The findings of this study support the need for the further investigation on this phytochemical agent for therapeutic application. SIGNIFICANCE AND IMPACT OF THE STUDY: This study revealed phytochemical plumbagin's potent and consistent in vitro antibacterial activity against clinically problematic methicillin-resistant Staphylococcus aureus (MRSA) including multi-drug-resistant (MDR) phenotypes. The study results support further research to assess the clinical scope of plumbagin.


Asunto(s)
Antibacterianos/farmacología , Staphylococcus aureus Resistente a Meticilina/efectos de los fármacos , Naftoquinonas/farmacología , Extractos Vegetales/farmacología , Plumbaginaceae/química , Pared Celular/efectos de los fármacos , Ciprofloxacina/farmacología , Citoplasma/efectos de los fármacos , Sinergismo Farmacológico , Humanos , Staphylococcus aureus Resistente a Meticilina/aislamiento & purificación , Pruebas de Sensibilidad Microbiana , Fitoquímicos/farmacología , Piperacilina/farmacología
7.
Future Med Chem ; 10(22): 2607-2617, 2018 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-30511591

RESUMEN

Aim: Antiprotozoal activity of 36 medicinal plants was evaluated. Materials & methods: In vitro potency against Trypanosoma brucei brucei, T. b. rhodesiense, T. cruzi and Leishmania infantum beside cytotoxicity on MRC-5 fibroblasts were determined. Results & conclusion: Maytenus parviflora showed the highest activity against T. b. brucei (IC50 of 0.6 µg/ml) and T. b. rhodesiense (IC50 of 0.5 µg/ml) with low cytotoxicity (CC50 of 30 µg/ml). Saussurea costus and Commiphora wightii, showed pronounced potency against T. cruzi with an IC50 of 3.6 and 2.5 µg/ml, respectively. Jatropha pelargonifolia and Solanum villosum exhibited pronounced activity toward L. infantum with an IC50 of 3.2 and 2.0 µg/ml, respectively. M. parviflora, S. costus, C. wightii, J. pelargonifolia and S. villosum showed relevant selectivity.

8.
Artículo en Inglés | MEDLINE | ID: mdl-29686147

RESUMEN

The increasing prevalence of multidrug-resistant Gram-negative pathogens has generated a requirement for new treatment options. Avibactam, a novel non-ß-lactam-ß-lactamase inhibitor, restores the activity of ceftazidime against Ambler class A, C, and some class D ß-lactamase-producing strains of Enterobacteriaceae and Pseudomonas aeruginosa The in vitro activities of ceftazidime-avibactam versus comparators were evaluated against 1,440 clinical isolates obtained in a phase 3 clinical trial in patients with complicated intra-abdominal infections (cIAI; ClinicalTrials.gov identifier NCT01499290). Overall, in vitro activities were determined for 803 Enterobacteriaceae, 70 P. aeruginosa, 304 Gram-positive aerobic, and 255 anaerobic isolates obtained from 1,066 randomized patients at baseline. Susceptibility was determined by broth microdilution. The most commonly isolated Gram-negative, Gram-positive, and anaerobic pathogens were Escherichia coli (n = 549), Streptococcus anginosus (n = 130), and Bacteroides fragilis (n = 96), respectively. Ceftazidime-avibactam was highly active against isolates of Enterobacteriaceae, with an overall MIC90 of 0.25 mg/liter. In contrast, the MIC90 for ceftazidime alone was 32 mg/liter. The MIC90 value for ceftazidime-avibactam (4 mg/liter) was one dilution lower than that of ceftazidime alone (8 mg/liter) against isolates of Pseudomonas aeruginosa The ceftazidime-avibactam MIC90 for 109 ceftazidime-nonsusceptible Enterobacteriaceae isolates was 2 mg/liter, and the MIC range for 6 ceftazidime-nonsusceptible P. aeruginosa isolates was 8 to 32 mg/liter. The MIC90 values were within the range of susceptibility for the study drugs permitted per the protocol in the phase 3 study to provide coverage for aerobic Gram-positive and anaerobic pathogens. These findings demonstrate the in vitro activity of ceftazidime-avibactam against bacterial pathogens commonly observed in cIAI patients, including ceftazidime-nonsusceptible Enterobacteriaceae (This study has been registered at ClinicalTrials.gov under identifier NCT01499290.).


Asunto(s)
Antibacterianos/farmacología , Compuestos de Azabiciclo/farmacología , Ceftazidima/farmacología , Infecciones Intraabdominales/microbiología , Bacteroides fragilis/efectos de los fármacos , Método Doble Ciego , Combinación de Medicamentos , Escherichia coli/efectos de los fármacos , Humanos , Pruebas de Sensibilidad Microbiana , Pseudomonas aeruginosa/efectos de los fármacos , Streptococcus anginosus/efectos de los fármacos
9.
Environ Sci Pollut Res Int ; 25(30): 29971-29982, 2018 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-29516419

RESUMEN

Five plant extracts traditionally used in organic and biodynamic farming for pest control and antifungal (downy mildew) disease management were selected after a farmer survey and analyzed for their chemical composition in LC-PDA-MS-MS and using adapted analytical method from food chemistry for determination of class of component (e.g., protein, sugar, lipids…). Their antifungal activity against Penicillium expansum, Botrytis cinerea, Botrytis allii, brown rot causing agents (Monilinia laxa and Monilinia fructigena), and grape downy mildew (Plasmopara viticola) was examined in vitro. White willow (Salix alba) and absinthe (Artemisia absinthium) ethanolic extracts were found to be the most effective in particular against Plasmopara viticola, with a total inhibition of spores germination when applied at 1000 mg/L. These extracts also showed a relatively low toxicity during preliminary ecotoxicological assays on Daphnia pulex. Extract from the bark of white willow contained some flavonoids, especially flavanones (eriodyctiol and derivates) and flavanols (catechins and derivates), as major compounds, whereas absinthe extract was rich in O-methylated flavanols and hydroxycinnamic acids. Thujone content in this extract was also determined by external calibration in GC-MS analysis, and its value was 0.004% dry extract.


Asunto(s)
Antifúngicos/química , Antifúngicos/farmacología , Enfermedades de las Plantas/microbiología , Extractos Vegetales/química , Extractos Vegetales/farmacología , Vitis/microbiología , Agricultura , Ascomicetos/efectos de los fármacos , Botrytis/efectos de los fármacos , Cromatografía de Gases y Espectrometría de Masas , Penicillium/efectos de los fármacos , Polifenoles/análisis
10.
Afr Health Sci ; 17(3): 780-789, 2017 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-29085406

RESUMEN

BACKGROUND: The emergence of drug-resistant strains of Mycobacterium tuberculosis has become a global public health problem. Polyherbal medicines offer great hope for developing alternative drugs for the treatment of tuberculosis. OBJECTIVE: To evaluate the anti-tubercular activity of polyherbal medicines used for the treatment of tuberculosis. METHODS: The remedies were screened against Mycobacterium tuberculosis H37Rv using Middlebrook 7H9 media and MGIT BACTEC 960 system. They were liquid preparations from King Williams Town site A (KWTa), King Williams Town site B (KWTb), King Williams Town site C (KWTc), Hogsback first site (HBfs), Hogsback second site (HBss), Hogsback third site (HBts), East London (EL), Alice (AL) and Fort Beaufort (FB). RESULTS: The susceptibility testing revealed that all the remedies contain anti-tubercular activity with KWTa, KWTb, KWTc, HBfs, HBts, AL and FB exhibiting more activity at a concentration below 25 µl/ml. Furthermore, MIC values exhibited inhibitory activity with the most active remedies from KWTa, HBfs and HBts at 1.562 µg/ml. However, isoniazid showed more inhibitory activity against M. tuberculosis at 0.05 µg/ml when compare to the polyherbal remedies. CONCLUSION: This study has indicated that these remedies could be potential sources of new anti-mycobacterial agents against M. tuberculosis. However, the activity of these preparations and their active principles still require in vivo study in order to assess their future as new anti-tuberculosis agents.


Asunto(s)
Antituberculosos/uso terapéutico , Contaminación de Medicamentos , Isoniazida/uso terapéutico , Fitoterapia , Extractos Vegetales/uso terapéutico , Plantas Medicinales/microbiología , Tuberculosis/tratamiento farmacológico , Humanos , Pruebas de Sensibilidad Microbiana , Mycobacterium tuberculosis/efectos de los fármacos , Sudáfrica
11.
Anaesthesiol Intensive Ther ; 49(3): 210-214, 2017.
Artículo en Inglés | MEDLINE | ID: mdl-28712104

RESUMEN

BACKGROUND: Enterobacteriaceae are currently causing the majority of healthcare-associated infections (HAI) and simultaneously expressing increasing levels of antibiotic resistance. The purpose of this study is to assess the in vitro sensitivity of MDR strains from the family Enterobacteriaceae to tigecycline in relation to their origin from patients hospitalized in intensive care units (ICUs) and non-ICUs. METHODS: The study involved 156 clinically significant strains of the Enterobacteriaceae family isolated from patients with complicated intraabdominal infections (cIAIs) and/or complicated skin and skin structure infections (cSSSIs) hospitalized in ICUs and other surgical departments. Tigecycline MICs were determined by Etest. RESULTS: The highest percentage of tigecycline non-susceptible (intermediate + resistant strains) in vitro strains among the Enterobacteriaceae species were observed for Serratia spp. 77.3%, followed by Citrobacter spp. (76.9%) and Enterobacter spp. (70%); whereas K. pneumoniae and E. coli showed 73-73.8% tigecycline susceptibility rates. CONCLUSION: Tigecycline demonstrates a high level of antimicrobial in vitro activity when tested against E. coli and K. pneumoniae, even those with the ESBL-phenotype. Tigecycline retained activity against merely 22-30% of Enterobacter, Citrobacter and Serratia genera.


Asunto(s)
Antibacterianos/farmacología , Infección Hospitalaria/tratamiento farmacológico , Enterobacteriaceae/efectos de los fármacos , Minociclina/análogos & derivados , Infección Hospitalaria/microbiología , Enterobacteriaceae/aislamiento & purificación , Humanos , Unidades de Cuidados Intensivos , Infecciones Intraabdominales/tratamiento farmacológico , Infecciones Intraabdominales/microbiología , Pruebas de Sensibilidad Microbiana , Minociclina/farmacología , Enfermedades Cutáneas Bacterianas/tratamiento farmacológico , Enfermedades Cutáneas Bacterianas/microbiología , Tigeciclina
12.
Bol. latinoam. Caribe plantas med. aromát ; 15(2): 112-121, mar. 2016. tab, ilus, graf
Artículo en Español | LILACS | ID: biblio-907525

RESUMEN

La familia Asclepiadaceae posee tradición en etnomedicina. En el nordeste argentino, A.mellodora y A. curassavica se utilizan como cataplasmas en accidentes de ofidios. En este trabajo, los extractos acuosos, etanólicos y hexánicos de A. mellodora y A. curassavica se evaluaron por SDS-PAGE para determinar su actividad alexitérica. El estudio in vitro de la capacidad inhibitoria de las actividades proteolítica, hemolítica indirecta y coagulante permitieron determinar que ambas especies manifiestan actividad, siendo A. mellodora más activa. Estadísticamente los extractos de A. mellodora fueron igualmente activos contra el veneno de Bothrops diporus y no mostraron diferencias significativas respecto del órgano utilizado en la inhibición de la actividad coagulante. Este resultado está en consonancia con la forma tradicional de su uso como cataplasma. Sobre el extracto etanólico de las raíces de A. mellodora se realizó un fraccionamiento bioguiado que permitió identificar fracciones de compuestos responsables de la actividad.


The Aclepiadaceae family has been reported by its use in ethnomedicine. In the northeast of Argentina, A. mellodora and A. curassavica are traditionally used in ofidic accidents as poultices. In this work, aqueous, alcoholic and hexanoic extracts were analyzed by SDS-PAGE to determine their anti-snake activity. The in vitro study of the inhibitory ability of the following activities: proteolytic, indirect hemolytic activity and inhibition of the coagulant activity, allowed demonstrating that both species were active against venom, being A. mellodora the most active. Statistically, all extracts of A. mellodora were active against venom in the inhibition of the coagulant activity, without significant differences with respect to the organ used; which is consistent with the traditional use as external poultice. The alcoholic extract of A. mellodora roots was subjected to a bio-guided separation. The fractions obtained were enriched in compounds which could probably be responsible for the activity against venom.


Asunto(s)
Antivenenos/farmacología , Asclepias/química , Venenos de Crotálidos , Extractos Vegetales/farmacología , Argentina , Bothrops , Electroforesis en Gel de Poliacrilamida , Técnicas In Vitro , Medicina Tradicional
13.
Pharm Biol ; 54(3): 445-50, 2016.
Artículo en Inglés | MEDLINE | ID: mdl-25963227

RESUMEN

CONTEXT: Trichomonosis, caused by the flagellate protozoan Trichomonas vaginalis, is the most common non-viral sexually transmitted disease (STD) and 5-nitroimidazole drugs are used for the treatment. However, a growing number of T. vaginalis isolates are resistant to these drugs, which make it becomes an urgent issue. OBJECTIVE: The current study was designed to evaluate the anti-T. vaginalis activity of the essential oil from A. tsao-ko used in traditional Chinese medicine and as a spice and its main component, geraniol. MATERIALS AND METHODS: The anti-T. vaginalis activities of A. tsao-ko essential oil and geraniol were evaluated by the minimum lethal concentration (MLC) and 50% inhibitory concentration (IC50) in vitro. The morphological changes of T. vaginalis were observed by transmission electron microscopy (TEM). Additionally, sub-MLC concentration treatment with sub-MLC A. tsao-ko essential oil and geraniol was also performed. RESULTS: This study shows that MLC/IC50 of A. tsao-ko essential oil was 44.97 µg/ml/22.49 µg/ml for T. vaginalis isolate Tv1, and 89.93 µg/ml/44.97 µg/ml for T. vaginalis isolate Tv2. Those of geraniol were 342.96 µg/ml/171.48 µg/ml, respectively. After A. tsao-ko essential oil or geraniol treatment, obvious similar morphological changes of T. vaginalis were observed by TEM: the nuclear membrane was damaged, nuclei were dissolved, and the chromatin was accumulated; in the cytoplasm, numerous vacuoles appeared, rough endoplasmic reticulum dilated, the number of ribosomes were reduced, organelles disintegrated, the cell membrane was partially damaged, with cytoplasmic leakage, and cell disintegration was observed. The action time did not increase the effect of A. tsao-ko essential oil or geraniol against T. vaginalis, as no significant difference was observed after sub-MLC concentration treatment for 1, 3, and 5 h with A. tsao-ko essential oil and geraniol. DISCUSSION AND CONCLUSION: The study describes the first report on the activity and morphological changes of A. tsao-ko essential oil and geraniol against T. vaginalis. The results obtained herein presented new opportunities for antitrichomonal drugs.


Asunto(s)
Amomum , Antiprotozoarios/farmacología , Aceites Volátiles/farmacología , Aceites de Plantas/farmacología , Terpenos/farmacología , Trichomonas vaginalis/efectos de los fármacos , Monoterpenos Acíclicos , Antiprotozoarios/aislamiento & purificación , Femenino , Humanos , Pruebas de Sensibilidad Microbiana/métodos , Aceites Volátiles/aislamiento & purificación , Aceites de Plantas/aislamiento & purificación , Trichomonas vaginalis/aislamiento & purificación , Trichomonas vaginalis/ultraestructura
14.
Int J Antimicrob Agents ; 45(5): 537-40, 2015 May.
Artículo en Inglés | MEDLINE | ID: mdl-25813393

RESUMEN

Recently, the aerobic growth of strictly anaerobic bacteria was demonstrated using antioxidants. Metronidazole is frequently used to treat infections caused by anaerobic bacteria; however, to date its antibacterial activity was only tested in anaerobic conditions. Here we aerobically tested using antioxidants the in vitro activities of metronidazole, gentamicin, doxycycline and imipenem against 10 common anaerobic and aerobic bacteria. In vitro susceptibility testing was performed by the disk diffusion method, and minimum inhibitory concentrations (MICs) were determined by Etest. Aerobic culture of the bacteria was performed at 37°C using Schaedler agar medium supplemented with 1mg/mL ascorbic acid and 0.1mg/mL glutathione; the pH was adjusted to 7.2 by 10M KOH. Growth of anaerobic bacteria cultured aerobically using antioxidants was inhibited by metronidazole after 72h of incubation at 37°C, with a mean inhibition diameter of 37.76mm and an MIC of 1µg/mL; however, strains remained non-sensitive to gentamicin. No growth inhibition of aerobic bacteria was observed after 24h of incubation at 37°C with metronidazole; however, inhibition was observed with doxycycline and imipenem used as controls. These results indicate that bacterial sensitivity to metronidazole is not related to the oxygen tension but is a result of the sensitivity of the micro-organism. In future, both culture and antibiotic susceptibility testing of strictly anaerobic bacteria will be performed in an aerobic atmosphere using antioxidants in clinical microbiology laboratories.


Asunto(s)
Antibacterianos/farmacología , Bacterias Anaerobias/efectos de los fármacos , Bacterias Anaerobias/metabolismo , Metronidazol/farmacología , Aerobiosis , Anaerobiosis , Antioxidantes/metabolismo , Ácido Ascórbico/metabolismo , Bacterias Aerobias/efectos de los fármacos , Bacterias Aerobias/metabolismo , Medios de Cultivo/química , Glutatión/metabolismo , Concentración de Iones de Hidrógeno , Pruebas de Sensibilidad Microbiana , Temperatura
15.
Artículo en Inglés | MEDLINE | ID: mdl-24146450

RESUMEN

The aim of this study was to evaluate extracts from two medicinal plants, Acanthospermum hispidum and Ficus thonningii, used in traditional medicine in Congo Brazzaville, for in vitro antiplasmodial activities against two laboratory strains of Plasmodium falciparum: the chloroquine sensitive 3D7 and the chloroquine resistant Dd2. ELISA HRP2 assay was used to evaluate the in vitro inhibitory activity of the extracts alone or in combination with chloroquine. Cytotoxicity was assessed on human HeLa cell line and reflected by the selectivity index. Methanolic extract of Acanthospermum hispidum exhibited a strong and a moderate inhibitory activity on the growth of Dd2 and 3D7 at 2.8 µg/ml and 9.2 µg/ml concentrations respectively with a selectivity index >10. The combination of the most active extract (methanolic extract of Acanthospermum hispidum) with chloroquine showed a synergistic interaction on both strains. The good selectivity index of Acanthospermum hispidum on HeLa cells reflects the safety of this plant. Extracts from Ficus thonningii did not show any promising antiplasmodial activity on both 3D7 and Dd2. Except the methanolic extract which exhibited a slight antiplasmodial activity with inhibitory concentration and selectivity index corresponding to 9.61 µg/ml and 11.16 respectively. Methanolic extract of Acanthospermum hispidum exhibited moderate to high inhibitory activity on 3D7 and Dd2 laboratory strains and a synergistic antimalarial effect when combined with chloroquine. Ficus thonningii seems to have no antimalarial activity. Phytochemical analysis, in vivo investigations using animal models and later clinical trials in collaboration with traditional practitioners are necessary to clarify the potential antimalarial activity of both plants.


Asunto(s)
Antimaláricos/farmacología , Asteraceae , Ficus , Medicinas Tradicionales Africanas , Extractos Vegetales/farmacología , Plasmodium falciparum/efectos de los fármacos , Cloroquina/farmacología , Congo , Sinergismo Farmacológico , Células HeLa , Humanos , Concentración 50 Inhibidora , Pruebas de Sensibilidad Parasitaria
16.
Cancer Nanotechnol ; 2(1-6): 57-65, 2011.
Artículo en Inglés | MEDLINE | ID: mdl-26069485

RESUMEN

Biofunctionalized gold and silver nanoparticles synthesized using different plant extracts of guava and clove in vitro anti-cancer efficacy against four different cancer cell lines human colorectal adenocarcinoma, human kidney, human chronic myelogenous, leukemia, bone marrow, and human cervix have been studied and reported. The present experimental study suggests that flavonoids functionalized gold nanoparticles synthesized using aqueous clove buds extract are more potential than guava leaf extract towards anti-cancer activities. The microscopic and 2,3-bis (2-methoxy-4-nitro-5-sulfophenyl)-5-[(phenylamino)carbonyl]-2H-tetrazolium hydroxide (XTT) assay infer that the functionalized irregular shaped gold nanoparticles synthesized with aqueous clove bud extract showed a satisfactory anti-cancer effect on all the cell lines. The silver nanoparticles synthesized using same extracts are devoid of anti-cancer activity. The XTT assay revealed dose-dependent cytotoxicity to cancer cell lines. The study revealed that the free radicals generated by gold nanoparticles are responsible for anti-cancer effect. To confirm the free-radical scavenging efficacy of gold nanoparticle, nitric oxide assay is followed. We observed that the gold nanoparticles swabbed the free radicals in dose-dependent manner. With continued improvements, these nanoparticles may prove to be potential anti-cancer agents.

17.
Biol. Res ; 43(2): 165-168, 2010. ilus
Artículo en Inglés | LILACS | ID: lil-567530

RESUMEN

Extracts prepared from seeds of Manilkara zapota, Anona squamosa, and Tamarindus indica were screened for their antibacterial activity by disc diffusion and broth dilution methods. Acetone and methanol extracts of T. indica seeds were found active against both gram-positive and gram-negative organisms. MIC values of potent extracts against susceptible organisms ranged from 53-380 μg/mL. Methanol extract of T. indica and acetone extract of M. zapota seeds were found to be bactericidal.


Asunto(s)
Annona/química , Antibacterianos/farmacología , Bacterias Gramnegativas/efectos de los fármacos , Bacterias Grampositivas/efectos de los fármacos , Manilkara/química , Extractos Vegetales/farmacología , Tamarindus/química , Antibacterianos/aislamiento & purificación , Pruebas de Sensibilidad Microbiana/métodos , Semillas/química
18.
Afr Health Sci ; 9(1): 40-5, 2009 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-20842241

RESUMEN

INTRODUCTION: Tuberculosis continues to be a devastating public health problem. Many communities in Uganda use medicinal plants to treat various infections, including respiratory tract infections. There are claims that some can treat tuberculosis. Verifying some of these claims could lead to discovery of lead compounds for development of a TB drug. METHODS: Chloroform and methanol extracts of L. camara collected from South-western Uganda were screened against three strains of Mycobacterium tuberculosis using the agar-well diffusion method. H37Rv, the rifampicin-resistant TMC-331 and a non-resistant wild strain (28-25271). The MIC and MBC were determined using the Agar dilution method on Middle brook 7H11. RESULTS: The methanol extract showed the highest activity against all the three strains used, with zones of inhibition of 18.0-22.5 mm and MIC values of 20 µg/ml for H37Rv and 15 µg/ml for both TMC-331 and wild stain. The values for rifampicin were 1.0 µg/ml for both H37Rv and wild strain but rifampicin hardly showed any activity on TMC-331. The MBC value for the methanol extract of L. camara was 30µg/ml for the H37Rv, and 20µg/ml for both the TMC-331 and wild strains of M. tuberculosis. The MBC for rifampicin was 2.0µg/ml for both H37Rv and the wild strain. CONCLUSION: We conclude that L. camara contains principles active against M. tuberculosis, which merit further research.


Asunto(s)
Antituberculosos/uso terapéutico , Lantana/química , Mycobacterium tuberculosis/efectos de los fármacos , Fitoterapia , Extractos Vegetales/farmacología , Tuberculosis/tratamiento farmacológico , Cloroformo , Farmacorresistencia Bacteriana Múltiple , Humanos , Medicina Tradicional , Metanol , Pruebas de Sensibilidad Microbiana , Mycobacterium tuberculosis/clasificación , Hojas de la Planta/química , Enfermedades Respiratorias/tratamiento farmacológico , Uganda
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