Chemistry Department, College of Natural and Applied Sciences, University of Dar es Salaam, Dar es Salaam P.O. Box 35061, Tanzania.
Department of Chemistry and Molecular Biology, University of Gothenburg, SE-412 96 Gothenburg, Sweden.
Molecules. 2019 Jul 29;24(15):2746. doi: 10.3390/molecules24152746.
Phytochemical investigations of ethanol root bark and stem bark extracts of (Benth.) Oliv. (Annonaceae) yielded a new benzopyranyl cadinane-type sesquiterpene (cleistonol, ) alongside 12 known compounds (-). The structures of the isolated compounds were established from NMR spectroscopic and mass spectrometric analyses. Structures of compounds and were further confirmed by single crystal X-ray crystallographic analyses, which also established their absolute stereochemical configuration. The ethanolic crude extract of root bark gave 72% inhibition against the chloroquine-sensitive 3D7-strain malaria parasite at 0.01 μg/mL. The isolated metabolites dichamanetin, ()-acetylmelodorinol, and cleistenolide showed IC = 9.3, 7.6 and 15.2 μM, respectively, against 3D7. Both the crude extract and the isolated compounds exhibited cytotoxicity against the triple-negative, aggressive breast cancer cell line, MDA-MB-231, with IC = 42.0 μg/mL (crude extract) and 9.6-30.7 μM (isolated compounds). Our findings demonstrate the potential applicability of as a source of antimalarial and anticancer agents.
植物化学研究表明，（Benth.）Oliv.（番荔枝科）的乙醇根皮和茎皮提取物中含有一种新的苯并吡喃-卡丹烷型倍半萜（cleistonol，）以及 12 种已知化合物（-）。从 NMR 光谱和质谱分析确定了分离化合物的结构。化合物和的结构通过单晶 X 射线晶体学分析进一步证实，这也确定了它们的绝对立体化学构型。根皮的乙醇粗提取物在 0.01 μg/mL 时对氯喹敏感的 3D7 株疟原虫 抑制率达到 72%。分离得到的代谢物二氢马钱素、（）-乙酰美多醇和 cleistenolide 对 3D7 的 IC = 9.3、7.6 和 15.2 μM。粗提取物和分离得到的化合物均对三阴性、侵袭性乳腺癌细胞系 MDA-MB-231 表现出细胞毒性，IC = 42.0 μg/mL（粗提取物）和 9.6-30.7 μM（分离化合物）。我们的研究结果表明，作为抗疟和抗癌药物的来源，具有潜在的适用性。
