Department of Chemistry, Makerere University, P.O. Box 7062, Kampala, Uganda.
Department of Chemistry, Makerere University, P.O. Box 7062, Kampala, Uganda.
Phytochemistry. 2014 Jun;102:189-96. doi: 10.1016/j.phytochem.2014.02.005. Epub 2014 Mar 25.
Neoboutonia macrocalyx is used by people in south western Uganda around Kibale National Park in the treatment of malaria. Phytochemical investigation on the leaves of this plant led to the isolation of nine cycloartane triterpenes (1-9) and one phenanthrene; 7-methoxy-2,8 dimethyl-9,10-dihydrophenantherene-3,6 diol (10) along with three known compounds which included 22-de-O-acetyl-26-deoxyneoboutomellerone (11), mellerin B (12) and 6-hydroxystigmast-4-en-3-one (13). The chemical structures of the compounds were established mainly through a combination of spectroscopic techniques. The isolated compounds were evaluated for antiplasmodial activity against the chloroquine-resistant FcB1/Colombia strain of Plasmodium falciparum and for cytotoxicity against the KB (nasopharyngeal epidermoid carcinoma) and MRC-5 (human diploid embryonic lung) cells. Seven out of 13 compounds exhibited good antiplasmodial activity with IC50 of ⩽5μg/ml with two compounds exhibiting low cytotoxicity and five compounds having significant cytotoxicity.
大籽钩叶藤在乌干达西南部的基巴莱国家公园周围地区被人们用于治疗疟疾。对该植物叶片的植物化学研究导致分离出了 9 种环阿尔廷三萜(1-9)和 1 种菲;7-甲氧基-2,8 二甲基-9,10-二氢菲-3,6 二醇(10)以及 3 种已知化合物,包括 22-O-乙酰基-26-脱氧新钩叶藤酮(11)、钩叶藤 B(12)和 6-羟基豆甾-4-烯-3-酮(13)。化合物的化学结构主要通过光谱技术的组合来确定。对分离得到的化合物进行了抗疟原虫活性评估,针对氯喹耐药的 FcB1/Colombia 株恶性疟原虫,并针对 KB(鼻咽表皮样癌细胞)和 MRC-5(人二倍体胚肺)细胞进行了细胞毒性评估。13 种化合物中有 7 种表现出良好的抗疟原虫活性,IC50 ⩽5μg/ml,其中 2 种化合物细胞毒性低,5 种化合物细胞毒性显著。