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
School of Pharmaceutical Sciences, College of Medical, Pharmaceutical and Health Sciences, Kanazawa University.
Chem Pharm Bull (Tokyo). 2017;65(1):116-120. doi: 10.1248/cpb.c16-00775.
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.
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。
