岩蔷薇属植物天然二萜及其半合成衍生物的抗利什曼原虫活性

Antileishmanial activity of natural diterpenes from Cistus sp. and semisynthetic derivatives thereof.

作者信息

Fokialakis Nikolas, Kalpoutzakis Eleftherios, Tekwani Babu Lal, Skaltsounis Alexios Leandros, Duke Stephen Oscar

机构信息

Natural Products Utilization Research Unit, USDA/ARS, University of Mississippi, USA.

出版信息

Biol Pharm Bull. 2006 Aug;29(8):1775-8. doi: 10.1248/bpb.29.1775.

DOI:10.1248/bpb.29.1775

PMID:16880643

Abstract

Eleven cis-clerodane diterpenes, seven labdane type diterpenes and one triterpene isolated from Cistus monspeliensis and the resin "Ladano" of Cistus creticus subsp. creticus were evaluated against Leishmania donovani promastigotes, the causative agent for visceral leishmaniasis. In addition, eleven semisynthetic manoyl oxide, seventeen labdane type derivatives and a triterpene were also evaluated for their antileishmanial activity. 18-Acetoxy-cis-clerod-3-en-15-ol, 15,18-diacetoxy-cis-clerod-3-ene and 13-(E)-8a-hydroxylabd-13-en-15-ol 2-chloroethylcarbamate exhibited the most potent and selective leishmanicidal activity with IC50 values of 3.3 microg/ml, 3.4 microg/ml and 3.5 microg/ml, respectively.

摘要

从蒙氏岩蔷薇以及克里特岩蔷薇亚种克里特岩蔷薇的树脂“拉达诺”中分离出的11种顺式克罗烷二萜、7种半日花烷型二萜和1种三萜，针对内脏利什曼病的病原体杜氏利什曼原虫前鞭毛体进行了评估。此外，还对11种半合成的氧化曼诺醇、17种半日花烷型衍生物和1种三萜的抗利什曼活性进行了评估。18-乙酰氧基-顺式克罗-3-烯-15-醇、15,18-二乙酰氧基-顺式克罗-3-烯和13-(E)-8a-羟基-labd-13-烯-15-醇2-氯乙基氨基甲酸酯表现出最强且最具选择性的杀利什曼活性，IC50值分别为3.3微克/毫升、3.4微克/毫升和3.5微克/毫升。