澳大利亚植物 Drummondita calida 中的一种新的喹啉环氧化物。

A new quinoline epoxide from the Australian plant Drummondita calida.

机构信息

Eskitis Institute, Griffith University, Brisbane, Australia.

出版信息

Planta Med. 2011 Sep;77(14):1644-7. doi: 10.1055/s-0030-1270963. Epub 2011 Apr 6.

Abstract

A drug discovery program aimed at identifying new antimalarial leads from a prefractionated natural product library has resulted in the purification of a new quinoline alkaloid, (2' R)-2',3'-epoxy- N-methylatanine (1), along with eight known natural products, skimmianin, γ-fagarine, maculosidine, evolitrine, dictamnine, pteleine, N-methylatanine, and werneria chromene. Compound 1 displayed 74 % inhibition at 80 µM against a chloroquine -resistant Plasmodium falciparum strain (Dd2).

摘要

一个旨在从预分馏天然产物库中鉴定新型抗疟先导化合物的药物发现计划，已成功分离得到一种新型喹啉生物碱（2'R）-2'，3'-环氧-N-甲基阿替宁（1），以及八种已知天然产物：skimmianin、γ-fagarine、maculosidine、evolitrine、dictamnine、ptelein、N-甲基阿替宁和 werneria chromene。化合物 1 在 80µM 时对氯喹耐药的恶性疟原虫株（Dd2）表现出 74%的抑制活性。