The development of the present study was based on selections using random, direct ethnopharmacological, and indirect ethnopharmacological approaches, aiming to evaluate which method is the best for bioprospecting new antimicrobial plant drugs. A crude extract of 53 species of herbaceous plants collected in the semiarid region of Northeast Brazil was tested against 11 microorganisms. Well-agar diffusion and minimum inhibitory concentration (MIC) techniques were used. Ten extracts from direct, six from random, and three from indirect ethnopharmacological selections exhibited activities that ranged from weak to very active against the organisms tested. The strain most susceptible to the evaluated extracts was Staphylococcus aureus. The MIC analysis revealed the best result for the direct ethnopharmacological approach, considering that some species yielded extracts classified as active or moderately active (MICs between 250 and 1000 µg/mL). Furthermore, one species from this approach inhibited the growth of the three Candida strains. Thus, it was concluded that the direct ethnopharmacological approach is the most effective when selecting species for bioprospecting new plant drugs with antimicrobial activities.
RESUMO: O uso popular de plantas medicinais continua sendo de grande interesse para a população, principalmente em países em desenvolvimento, nos quais o acesso à medicina alopática ainda é muito restrito. Assim, além de sua importância na medicina tradicional, o conhecimento das plantas pode fornecer para a indústria farmacêutica, direta ou indiretamente, princípios ativos de interesse terapêutico. No presente trabalho foi avaliada a atividade antimicrobiana dos extratos metanólicos secos de Croton pulegioides Baill. obtidos a partir da raiz, do caule e das folhas nas concentrações de 25, 50 e 100mg/mL utilizando o método de difusão em Agar (técnica de poços) frente a cinco cepas Gram-positivas, três cepas de fungos e três cepas de bactérias Gram-negativas. Na execução do estudo foi utilizado o antibiótico Gentamicina (100µg/mL) no teste com bactérias, e Cetoconazol (300µg/mL) para as Candidas verificando-se, ao mesmo tempo, a ausência de atividade para o diluente DMSO 20% em água. Na observação dos resultados evidenciaram-se halos de inibição indicando atividade dos extratos metanólicos da raiz, caule e folhas, nas concentrações de 50 e 100mg/ml, frente Bacillus subtilis AM 04; dos extratos metanólicos da raiz e do caule, nas concentrações de 50 e 100mg/ml, frente Staphylococcus aureus AM 103 (ATCC 6538); e do extrato metanólico do caule, nas concentrações de 50 e 100mg/ml, frente S. epidermidis AM 235. Por outro lado, todos os extratos foram inativos nas concentrações avaliadas frente às bactérias Gram-negativas utilizadas no estudo (Pseudomonas aeruginosa AM 206, Escherichia coli AM 1050 e Klebsiella pneumoniae AM 410). Referente à atividade sobre fungos, os extratos metanólicos da raiz e do caule inibiram, nas três concentrações avaliadas, o crescimento de Candida tropicalis AM 1181 e C. albicans AM 1140, enquanto o extrato das folhas, inibiu o crescimento de C. tropicalis AM 1181 nas concentrações de 50 e 100mg/ml e de C. albicans AM 1140 apenas na concentração de 100mg/mL. Finalmente o extrato metanólico das folhas, na concentração de 100mg/mL, foi o único a inibir o crescimento de Candida krusei. Os resultados preliminares apresentados pelo presente trabalho sugeriram que a espécie Croton pulegioides Baill. apresentou resultados promissores quanto ao potencial antimicrobiano. Palavras-chave:Plantas medicinais, Croton pulegioides Baill., Atividade antimicrobiana.ABSTRACT: Antimicrobial activity of methanol extracts of root, stem and leaves of Croton pulegioides Baill. The employment of medicinal plants as a folk custom remains important to the present time, mainly in developing countries, where access to allopathic medicine is restricted. Besides their importance in traditional medicine, the knowledge on these plants can, directly or indirectly, provide information about the active ingredients involved, which may be of interest to the pharmaceutical industry. The present study evaluated the antimicrobial activity of dried methanolic extracts of Croton pulegioides Baill, extracted from its roots, stalk, an...
Background: In a study recently published by our research group, the compounds isoxazoline-acylhydrazone derivatives R-99 and R-123 presented promising antinociceptive activity. However, the mechanism of action of this compound is still unknown. Objective: This study aimed to assess the mechanisms involved in the antinociceptive activity of these compounds in chemical models of pain. Methods: Animals were orally pretreated and evaluated in the acetic acid-, formalin-, capsaicin-, carrageenan- and Complete Freund's Adjuvant (CFA)-induced pain models in mice. The effects of the compounds after pretreatment with naloxone, prazosin, yohimbine, atropine, L-arginine, or glibenclamide were studied, using the acetic acid-induced writhing test to verify the possible involvement of opioid, α1-adrenergic, α2-adrenergic or cholinergic receptors, and nitric oxide or potassium channels pathways, respectively. Results: R-99 and R-123 compounds showed significant antinociceptive activity on pain models induced by acetic acid, formalin, and capsaicin. Both compounds decreased the mechanical hyperalgesia induced by carrageenan or CFA in mice. The antinociceptive effects of R-99 and R-123 on the acetic acid-induced writhing test were significantly attenuated by pretreatment with naloxone, yohimbine or atropine. R-99 also showed an attenuated response after pretreatment with atropine and glibenclamide. However, on the pretreatment with prazosin, there was no change in the animals' response to both compounds. Conclusion: R-99 and R-123 showed antinociceptive effects related to mechanisms that involve, at least in part, interaction with the opioid and adrenergic systems and TRPV1 pathways. The compound R-99 also interacts with the cholinergic pathways and potassium channels.
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