Antiplasmodial and cytotoxic activities of secondary metabolites from the leaves of Pleiocarpa bicarpellata Stapf (Apocynaceae).

IF 2.1
Aurore M Bella, Guy R Ebede, Gaetan B N Bayiha, Christelle Tsaffo, Lauve R Y Tchokouaha, Rabia Farooq, Fabrice F Boyom, Muhammad I Choudhary, Josephine N Mbing, Joseph T Ndongo, Christian G Bochet, Hartmut Laatsch
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Abstract

Phytochemical studies of the leaves of Pleiocarpa bicarpellata led to the isolation of a new indole C-glycoside, Bicarpellatoside A (1), along with eight known compounds (2-9), including three indoles, two indolines, an iridoid monoterpenoid, a triterpenoid, and a phenolic acid. The structures of all isolated compounds were elucidated using NMR, MS, and IR spectroscopic data, in comparison with the literature. Compounds 1, 3, and 9 are reported in this genus for the first time. In vitro antiplasmodial activity tests were conducted against both chloroquine-sensitive (3D7) and chloroquine-resistant (Dd2) strains of Plasmodium falciparum, using the crude extract and isolated compounds 1-4. The crude extract exhibited promising activity, with IC50 values of 4.07 ± 0.78 μg/mL (Dd2) and 4.32 ± 0.42 μg/mL (3D7). Bicarpellatoside A (1) showed good activity, with IC50 values of 2.24 ± 0.05 µM and 2.74 ± 0.05 µM against Dd2 and 3D7 strains of P. falciparum, respectively. Compound 4 showed moderate activity (IC50 of 40.93 ± 3.39 µM and 48.13 ± 5.63 µM on Dd2 and 3D7 strains of P. falciparum, respectively, with a high selectivity index of 34.48, indicating potential for further development. Overall, these findings highlight and confirm the antiplasmodial potential of compounds from P. bicarpellata.

夹竹桃叶次生代谢物的抗疟原虫和细胞毒活性。
通过对百香菇(Pleiocarpa bicarpellata)叶片的植物化学研究,分离出一种新的吲哚c -糖苷,Bicarpellatoside a(1),以及八种已知化合物(2-9),包括三种吲哚、两种吲哚类、一种环烯醚萜类单萜、一种三萜和一种酚酸。所有分离化合物的结构通过核磁共振,质谱和红外光谱数据进行了阐明,并与文献进行了比较。化合物1、3、9为首次在该属中发现。采用粗提物和分离化合物1 ~ 4对氯喹敏感(3D7)和耐氯喹(Dd2)恶性疟原虫进行体外抗疟原虫活性试验。粗提物具有良好的活性,IC50分别为4.07±0.78 μg/mL (Dd2)和4.32±0.42 μg/mL (3D7)。Bicarpellatoside A(1)对恶性疟原虫Dd2和3D7株的IC50值分别为2.24±0.05 µM和2.74±0.05 µM。化合物4对恶性疟原虫Dd2和3D7株的IC50分别为40.93±3.39 µM和48.13±5.63 µM,选择性指数为34.48,具有较好的开发潜力。总的来说,这些发现强调并证实了双头藻化合物的抗疟原虫潜力。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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