Ma Xinhua, Yang Jie, Deng Shihao, Huang Mi, Zheng Sijian, Xu Shicheng, Cai Jinyan, Yang Xinzhou, Ai Honglian
a School of Pharmaceutical Sciences , South-Central University for Nationalities , Wuhan , China.
b School of Pharmacy , Guangdong Pharmaceutical University , Guangzhou , China.
Nat Prod Res. 2017 Jul;31(13):1473-1477. doi: 10.1080/14786419.2017.1280493. Epub 2017 Feb 2.
To discover new bioactive compounds from nature plants, a primary screening of traditional Chinese medicines had been taken. The screening results showed that a EtOAc extract of Sedum sarmentosum displayed a certain degree of cytotoxic activity and bioassay-directed isolation of EtOAc extract gave two new megastigmanes, (6S,9R)-2-hydroxy-4-(2,6,6-trimethyl-4-oxo-cyclohex-2-enyl)-butyric acid (1) and (6S,9R)-2-hydroxy-4-(2,6,6-trimethyl-4-oxo-cyclohex-2-enyl)-butyric acid methyl ester (2) together with seven known flavonoids. The chemical structures of 1 and 2 were elucidated on the basis of detailed 1D, 2D NMR and MS data. When tested against HepG2 and Hep3B hepatocellular carcinoma cell lines, compounds 1-9 showed weak anti-HCC activity. In addition, in vitro antioxidant activities of 1-9 were evaluated by ABTS radical cation-scavenging assay. 1 and 2 exhibited weak activity with per micromoles equivalent to 0.039 and 0.042 μM of Trolox, respectively. The flavonoid component, quercetin (9) showed the highest antioxidant activities with per micromoles equivalent 0.67 μM of Trolox.
为了从天然植物中发现新的生物活性化合物，对中药进行了初步筛选。筛选结果表明，垂盆草的乙酸乙酯提取物表现出一定程度的细胞毒活性，对乙酸乙酯提取物进行生物活性导向分离得到两种新的巨大戟烷型二萜，(6S,9R)-2-羟基-4-(2,6,6-三甲基-4-氧代环己-2-烯基)丁酸(1)和(6S,9R)-2-羟基-4-(2,6,6-三甲基-4-氧代环己-2-烯基)丁酸甲酯(2)，以及七种已知的黄酮类化合物。根据详细的一维、二维核磁共振和质谱数据阐明了1和2的化学结构。在针对HepG2和Hep3B肝癌细胞系进行测试时，化合物1-9显示出较弱的抗肝癌活性。此外，通过ABTS自由基阳离子清除试验评估了1-9的体外抗氧化活性。1和2表现出较弱的活性，每微摩尔分别相当于0.039和0.042 μM的Trolox。黄酮类成分槲皮素(9)表现出最高的抗氧化活性，每微摩尔相当于0.67 μM的Trolox。
