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一种来自钝叶黄荆的新型克罗烷二萜。

A Novel Clerodane Diterpene from Vitex cofassus.

作者信息

Rasyid Faradiba Abdul, Fukuyoshi Shuichi, Ando Hirokazu, Miyake Katsunori, Atsumi Toshiyuki, Fujie Tetsuo, Saito Yohei, Goto Masuo, Shinya Tomohiro, Mikage Masayuki, Sasaki Yohei, Nakagawa-Goto Kyoko

机构信息

School of Pharmaceutical Sciences, College of Medical, Pharmaceutical and Health Sciences, Kanazawa University.

出版信息

Chem Pharm Bull (Tokyo). 2017;65(1):116-120. doi: 10.1248/cpb.c16-00775.

Abstract

New clerodane diterpene, 16-hydroxy-pentandralactone (1) and known diterpene acuminolide (2) were isolated from the methanol extract of Vitex cofassus leaves. The chemical structure and the absolute configuration of 1 were determined by MS, NMR and electron circular dichroism (ECD) experiments. The isolated compounds were evaluated for their antiproliferative activities against a panel of human tumor cell lines, including a multidrug-resistant (MDR) cell line. Both compounds showed potent antiproliferative activities against all the tested cell lines with IC values of 5.4-11.4 µM. Their effects on cell viability were also tested using vascular endothelial growth factor (VEGF)-stimulated human umbilical vein endothelial cells (HUVECs). Compound 1 inhibited VEGF-stimulated HUVEC proliferation in a dose-dependent manner. Based on these results, compound 1 could be a candidate for antitumor agent and inhibitor of angiogenesis.

摘要

从钝叶牡荆叶的甲醇提取物中分离得到了新的克罗烷二萜16-羟基-戊醛内酯(1)和已知的二萜尖叶荆内酯(2)。通过质谱、核磁共振和电子圆二色光谱(ECD)实验确定了1的化学结构和绝对构型。对分离得到的化合物进行了针对一组人类肿瘤细胞系(包括多药耐药(MDR)细胞系)的抗增殖活性评估。两种化合物对所有测试细胞系均显示出强效抗增殖活性,IC值为5.4 - 11.4 μM。还使用血管内皮生长因子(VEGF)刺激的人脐静脉内皮细胞(HUVECs)测试了它们对细胞活力的影响。化合物1以剂量依赖性方式抑制VEGF刺激的HUVEC增殖。基于这些结果,化合物1可能是抗肿瘤剂和血管生成抑制剂的候选物。

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