Pharmaceutical Biology, Pharmacenter , University of Basel , Klingelbergstrasse 50 , 4056 Basel , Switzerland.
Center for Complementary Medicine, Institute for Infection Prevention and Hospital Epidemiology, Faculty of Medicine , University of Freiburg , Breisacher Straße 115 B , 79106 Freiburg , Germany.
J Nat Prod. 2019 Jun 28;82(6):1424-1433. doi: 10.1021/acs.jnatprod.8b00791. Epub 2019 Jun 5.
A library of extracts from plants used in Chinese Traditional Medicine was screened for inhibition of T lymphocyte proliferation. An ethyl acetate extract from aerial parts of Artemisia argyi showed promising activity and was submitted to HPLC-based activity profiling to track the active compounds. From the most active time window, three guaianolides (1, 2, and 5) and two seco-tanapartholides (3 and 4) were identified and, in a less active time window, five new sesquiterpene lactones (8-11, 17), along with six known sesquiterpene lactones and two known flavonoids. The absolute configurations of compounds 1, 2, 5-10, 13-15, 17, and 18 were established by comparison of experimental with calculated electronic circular dichroism (ECD) spectra. For seco-tanapartholides B (3) and A (4), ECD yielded ambiguous results, and their absolute configurations were determined by comparing experimental and calculated vibrational circular dichroism (VCD) spectra. Compounds 1-5 showed significant, noncytotoxic inhibition of T lymphocyte proliferation, with IC values between 1.0 and 3.7 μM.
从中国传统医学中使用的植物提取物文库中筛选出抑制 T 淋巴细胞增殖的物质。艾叶的乙酸乙酯提取物表现出有希望的活性，并通过基于 HPLC 的活性分析来跟踪活性化合物。从最活跃的时间窗口中，鉴定出三种愈创木烷内酯（1、2 和 5）和两种倍半萜内酯（3 和 4），在活性较弱的时间窗口中，鉴定出五种新的倍半萜内酯（8-11、17），以及六种已知的倍半萜内酯和两种已知的黄酮类化合物。通过比较实验与计算的电子圆二色性（ECD）光谱，确定了化合物 1、2、5-10、13-15、17 和 18 的绝对构型。对于倍半萜内酯 B（3）和 A（4），ECD 产生了模糊的结果，通过比较实验和计算的振动圆二色性（VCD）光谱确定了它们的绝对构型。化合物 1-5 对 T 淋巴细胞增殖具有显著的非细胞毒性抑制作用，IC 值在 1.0 至 3.7 μM 之间。
