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Mar Drugs ; 17(1)2018 Dec 24.
Artigo em Inglês | MEDLINE | ID: mdl-30586918


A new alkaloid paenidigyamycin A (1) was obtained from the novel Ghanaian Paenibacillus sp. isolated from the mangrove rhizosphere soils of the Pterocarpus santalinoides tree growing in the wetlands of the Digya National Park, Ghana. Compound 1 was isolated on HPLC at tR = 37.0 min and its structure determined by MS, 1D, and 2D-NMR data. When tested against L. major, 1 (IC50 0.75 µM) was just as effective as amphotericin B (IC50 0.31 µM). Against L. donovani, 1 (IC50 7.02 µM) was twenty-two times less active than amphotericin B (IC50 0.32 µM), reinforcing the unique effectiveness of 1 against L. major. For T. brucei brucei, 1 (IC50 0.78 µM) was ten times more active than the laboratory standard Coptis japonica (IC50 8.20 µM). The IC50 of 9.08 µM for 1 against P. falciparum 3d7 compared to artesunate (IC50 36 nM) was not strong, but this result suggests the possibility of using the paenidigyamycin scaffold for the development of potent antimalarial drugs. Against cercariae, 1 showed high anticercaricidal activity compared to artesunate. The minimal lethal concentration (MLC) and minimal effective concentration (MEC) of the compound were 25 and 6.25 µM, respectively, while artesunate was needed in higher quantities to produce such results. However, 1 (IC50 > 100 µM) was not active against T. mobilensis.

Alcaloides/farmacologia , Antiparasitários/farmacologia , Paenibacillus/química , Pterocarpus/microbiologia , Alcaloides/química , Alcaloides/isolamento & purificação , Alcaloides/uso terapêutico , Anfotericina B/farmacologia , Animais , Antiparasitários/química , Antiparasitários/isolamento & purificação , Antiparasitários/uso terapêutico , Artesunato/farmacologia , Cercárias/efeitos dos fármacos , Avaliação Pré-Clínica de Medicamentos , Gana , Imidazóis/química , Concentração Inibidora 50 , Leishmania donovani/efeitos dos fármacos , Doenças Parasitárias/tratamento farmacológico , Plasmodium falciparum/efeitos dos fármacos , Rizosfera , Microbiologia do Solo , Trypanosoma brucei brucei/efeitos dos fármacos , Áreas Alagadas