塞德龙宁的抗疟活性。

Antimalarial activity of cedronin.

作者信息

Moretti C, Deharo E, Sauvain M, Jardel C, David P T, Gasquet M

机构信息

Laboratorio de Farmacognosia, ORSTRM-IBBA, La Paz, Bolivia.

出版信息

J Ethnopharmacol. 1994 Jun;43(1):57-61. doi: 10.1016/0378-8741(94)90117-1.

DOI:10.1016/0378-8741(94)90117-1

PMID:7967650

Abstract

Cedronin was isolated from Simaba cedron Planchon (Simaroubaceae), a species popularly believed in South America to have antimalarial properties. It was examined for in vitro and in vivo antimalarial activities and for cytotoxicity against KB cells. Experimental results showed that cedronin was active against chloroquine-sensitive and resistant strain, with an IC50 of 0.25 micrograms/ml (0.65 mumol/ml). It was also found to be active in vivo against Plasmodium vinkei with an IC50 of 1.8 mg/kg (4.7 nM/kg) in the classic 4-day test. Cedronin belongs to the small group of quassinoids with a C19 basic skeleton and shows a rather low cytotoxicity against KB cells (IC50 = 4 micrograms/ml, 10.4 microM) as compared with C20 biologically active quassinoids; however its toxic/therapeutic ratio (10/1.8) remains lower than chloroquine (10/0.5).

摘要

雪松苦素是从南美苦木（苦木科）中分离得到的，在南美洲人们普遍认为该植物具有抗疟特性。对其进行了体外和体内抗疟活性以及对KB细胞的细胞毒性研究。实验结果表明，雪松苦素对氯喹敏感株和耐药株均有活性，IC50为0.25微克/毫升（0.65微摩尔/毫升）。在经典的4天试验中还发现，雪松苦素在体内对文氏疟原虫也有活性，IC50为1.8毫克/千克（4.7纳摩尔/千克）。雪松苦素属于具有C19基本骨架的小檗碱类化合物，与具有C20生物活性的小檗碱类化合物相比，其对KB细胞的细胞毒性相当低（IC50 = 4微克/毫升，10.4微摩尔）；然而，其毒/治疗比（10/1.8）仍低于氯喹（10/0.5）。