Fattahian Maryam, Ghanadian Mustafa, Zolfaghari Behzad, Abdeyazdan Sara, Saberi Sedigheh, Zulfiqar Fazila, Khan Ikhlas A, Ali Zulfiqar
School of Pharmacy and Pharmaceutical Sciences, Isfahan University of Medical Sciences, Isfahan, Iran.
Shahid Beheshti Phytochemistry Research Center, Shahid Beheshti University of Medical Sciences, Tehran, Iran.
Nat Prod Res. 2024 Jan-Feb;38(1):16-27. doi: 10.1080/14786419.2022.2102630. Epub 2022 Jul 20.
Two new eudesmane-type sesquiterpene lactones, 1β,3α,8α-trihydroxy-11β,13-dihydroeudesma-4(15)-en-12,6α-olide () and 1β,4α,8α-trihydroxy-11β,13-dihydroeudesma-12,6α-olide (), and an unprecedented elemane-type sesquiterpene lactone, 1β,2β,8α-trihydroxy-11β,13-dihydroelema-12,6α-olide () along with a known eudesmanolide artapshin () were isolated from Structures were elucidated by NMR, HR-ESI-MS, and ECD spectral data analysis. The anti-protozoal activity was evaluated against promastigotes and amastigote-infected macrophages. They showed dose- and time-dependent activity against amastigotes with IC values in the range of 4.9 to 25.3 μM being favourably far below their toxicity against normal murine macrophages with CC values ranging from 432.5 to 620.7 μM after 48 h of treatment. Compound exhibited the strongest activity and the highest selectivity index (SI) with IC of 4.9 ± 0.6 μM and SI of 88.2 comparable with the standard drug, meglumine antimoniate (Glucantime), with IC and SI values of 15.5 ± 2.1 μM and 40.0, respectively.
从[具体来源未给出]中分离出两种新的桉叶烷型倍半萜内酯，1β,3α,8α-三羟基-11β,13-二氢桉叶-4(15)-烯-12,6α-内酯（）和1β,4α,8α-三羟基-11β,13-二氢桉叶-12,6α-内酯（），以及一种前所未有的榄香烷型倍半萜内酯，1β,2β,8α-三羟基-11β,13-二氢榄香-12,6α-内酯（），同时还分离出一种已知的桉叶烷醇内酯artapshin（）。通过核磁共振（NMR）、高分辨电喷雾电离质谱（HR-ESI-MS）和电子圆二色光谱（ECD）数据分析对其结构进行了阐明。针对前鞭毛体和被无鞭毛体感染的巨噬细胞评估了其抗寄生虫活性。它们对无鞭毛体表现出剂量和时间依赖性活性，IC值在4.9至25.3 μM范围内，远低于其对正常小鼠巨噬细胞的毒性，处理48小时后CC值范围为432.5至620.7 μM。化合物表现出最强的活性和最高的选择性指数（SI），IC为4.9±0.6 μM，SI为88.2，与标准药物葡甲胺锑酸盐（Glucantime）相当，其IC和SI值分别为15.5±2.1 μM和40.0。
