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. 2020 Oct 23;83(10):3012-3020. doi: 10.1021/acs.jnatprod.0c00564. Epub 2020 Oct 1.
In a screening of an extract library from plants used in Traditional Chinese Medicine the MeOH extract of inhibited proliferation of human primary T cells with an IC of 25.8 μg/mL. Activity in the extract was tracked by HPLC activity profiling, and a total of 15 compounds were characterized. Three compounds, toddalic acid () and both enantiomers ( and ) of toddanolic acid (), were new natural products, and two recently published compounds, (2')-toddalolactone 3'--β-d-glucopyranoside () and (2')-toddalolactone 2'--β-d-glucopyranoside (), were described in detail for the first time. The absolute configurations of compounds , , , , , and were determined by comparison of experimental and calculated ECD spectra. For glucosides and , ECD data and chiral-phase HPLC of the aglycones after enzymatic hydrolysis confirmed the results. Nitidine chloride () inhibited proliferation of primary human T cells with an IC of 0.4 μM.
在对中药植物提取物文库进行筛选时,发现甲醇提取物对人原代 T 细胞的增殖具有抑制作用,IC 为 25.8μg/mL。通过 HPLC 活性分析追踪提取物中的活性,共鉴定出 15 种化合物。其中,托丹酸()和托丹醇酸()的两种对映异构体(和)是新的天然产物,另外两种最近发表的化合物(2')-托达洛内酯 3'--β-d-吡喃葡萄糖苷()和(2')-托达洛内酯 2'--β-d-吡喃葡萄糖苷(),首次对其进行了详细描述。通过比较实验和计算的 ECD 光谱,确定了化合物、、、、、和的绝对构型。对于糖苷和,通过酶解后苷元的 ECD 数据和手性相 HPLC 进一步证实了结果。盐酸小檗碱()对原代人 T 细胞的增殖具有抑制作用,IC 为 0.4μM。