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从福桐(夹竹桃科)叶中提取的三萜类和甾体生物碱的抗疟原虫和抗利什曼原虫抑制活性。

Antiplasmodial and antileishmanial inhibitory activity of triterpenes and steroidal alkaloid from the leaves of Funtumia elastica (Preuss) Stapf (Apocynaceae).

机构信息

Faculty of Science, Department of Organic Chemistry, University of Yaoundé 1, Yaoundé, Cameroon; Center for Studies on Medicinal Plants and Traditional Medicine (CRPMT), Institute of Medical Research and Medicinal Plants Studies (IMPM), Yaoundé, Cameroon.

Faculty of Science, Department of Organic Chemistry, University of Yaoundé 1, Yaoundé, Cameroon; Department of Chemistry, Higher Teacher's Training College, University of Yaoundé 1, Yaoundé, Cameroon.

出版信息

Fitoterapia. 2021 Jun;151:104869. doi: 10.1016/j.fitote.2021.104869. Epub 2021 Feb 28.

Abstract

The phytochemical study of leaves of Funtumia elastica led to the isolation of three undescribed ursane derivatives, funtumic acids A, B and C (1-3), as well as one steroidal alkaloid, elasticine (4) and five other known compounds (5-9). Their structures were elucidated on the basis of NMR, MS, IR, UV spectroscopic data as well as by comparison with the literature. The compound 5-hydroxypyridine-3-carboxamide (9) was isolated for the first time from the Apocynaceae family. All the isolated compounds were evaluated for their antiparasitic effects against 3D7 and Dd2 strains of Plasmodium falciparum and promastigotes of Leishmania donovani (MHOM/SD/62/1S). Compounds 1-4 possessed good in vitro antimalarial activities against CQR Dd2 with IC values ranging from 4.68 to 5.36 μg/mL and moderate on CQS 3D7. Only compounds 1 and 2 showed leishmanicidal activities with IC values ranging between 10.49 and 13.21 μg/mL. In addition, crude extract exhibited potent antiplasmodial (IC 0.91 and 3.12 μg/mL) and antileishmanial (IC 3.32 μg/mL) activities, thus demonstrating their potential synergistic action.

摘要

对大戟科植物 Funtumia elastica 的叶进行了植物化学研究,从中分离得到了三个未被描述的 Ursane 衍生物,分别为 funtumic 酸 A、B 和 C(1-3),以及一个甾体生物碱 elasticine(4)和另外五个已知化合物(5-9)。根据 NMR、MS、IR、UV 光谱数据以及与文献的比较,确定了它们的结构。首次从夹竹桃科植物中分离得到了 5-羟基吡啶-3-甲酰胺(9)。所有分离得到的化合物均对恶性疟原虫 3D7 和 Dd2 株以及利什曼原虫 Donovan 株(MHOM/SD/62/1S)的前鞭毛体进行了抗寄生虫作用评估。化合物 1-4 对 CQR Dd2 具有良好的体外抗疟活性,IC 值范围为 4.68-5.36μg/mL,对 CQS 3D7 具有中等活性。只有化合物 1 和 2 具有杀利什曼原虫活性,IC 值范围为 10.49-13.21μg/mL。此外,粗提物表现出很强的抗疟原虫(IC 0.91 和 3.12μg/mL)和抗利什曼原虫(IC 3.32μg/mL)活性,因此表明它们具有潜在的协同作用。

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