来自 Hayata 凹叶越橘的新类黄酮，凹叶杨梅素 A-C。

New flavonoids, emarginin A-C from Vaccinium emarginatum Hayata.

机构信息

The Ph.D. Program for Cancer Biology and Drug Discovery, China Medical University and Academia Sinica, Taichung, Taiwan.

Department of Chinese Pharmaceutical Sciences and Chinese Medicine Resources, China Medical University, Taichung, Taiwan.

出版信息

Fitoterapia. 2020 Mar;141:104446. doi: 10.1016/j.fitote.2019.104446. Epub 2019 Nov 29.

DOI:10.1016/j.fitote.2019.104446

PMID:31790770

Abstract

Phytochemical investigation of methanolic extract of the whole plants of Vaccinium emarginatum allowed for the characterization of one epicatechin derivative (1) that was isolated from a natural source for the first time and three new flavonoids, emarginin A (2), emarginin B (3), and emarginin C (4), together with 11 known compounds (5-15). The structures of compounds 1-4 were elucidated by combination of spectroscopic analysis (MS, IR, and NMR) and by comparison with that of literature analogues. Compounds 1-8 and 11-15 were evaluated for their preliminary in vitro anti-proliferative activity against Du145 and PC-3 prostate cancer cell lines. Among them, compound 15 exhibited most potent cytotoxicity against Du145 and PC-3 cells, with IC values of 8.46 and 10.98 μM, respectively. Furthermore, compounds 1-7 were assessed for their anti-inflammatory potential against lipopolysaccharide (LPS)-induced nitric oxide (NO) production in RAW 264.7 cells. Compound 4 exhibited moderate anti-inflammatory activity, with an IC value of 27.99 μM.

摘要

从天然来源首次分离得到一种表儿茶素衍生物（1），并结合光谱分析（MS、IR 和 NMR）和文献比较鉴定了另外三种新的黄酮类化合物：凹缘当归素 A（2）、凹缘当归素 B（3）和凹缘当归素 C（4），以及 11 种已知化合物（5-15）。对化合物 1-4 的结构进行了鉴定。对化合物 1-8 和 11-15 进行了初步的体外抗前列腺癌 Du145 和 PC-3 细胞系增殖活性评价。其中，化合物 15 对 Du145 和 PC-3 细胞的细胞毒性最强，IC 值分别为 8.46 和 10.98 μM。此外，还评估了化合物 1-7 对 LPS 诱导的 RAW 264.7 细胞中一氧化氮（NO）产生的抗炎潜力。化合物 4 表现出中等抗炎活性，IC 值为 27.99 μM。