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荔枝草中的桉叶烷型倍半萜类化合物抑制白细胞介素-6诱导的信号转导和转录激活因子3激活。

Eudesmane-type sesquiterpenoids from Salvia plebeia inhibit IL-6-induced STAT3 activation.

作者信息

Jang Hyun-Jae, Oh Hyun-Mee, Hwang Joo Tae, Kim Mi-Hwa, Lee Soyoung, Jung Kyungsook, Kim Young-Ho, Lee Seung Woong, Rho Mun-Chual

机构信息

Natural Product Research Center, Korea Research Institute of Bioscience and Biotechnology, 181 Ipsin-gil, Jeongeup-si, Jeonbuk 56212, South Korea; College of Pharmacy, Chungnam National University, Daejeon 34134, South Korea.

Natural Product Research Center, Korea Research Institute of Bioscience and Biotechnology, 181 Ipsin-gil, Jeongeup-si, Jeonbuk 56212, South Korea.

出版信息

Phytochemistry. 2016 Oct;130:335-42. doi: 10.1016/j.phytochem.2016.08.001. Epub 2016 Aug 6.

Abstract

Seven eudesmane-type sesquiterpenoid lactones and the known plebeiolide C were isolated from an ethanol-soluble extract of the aerial parts of Salvia plebeia R. Br. Their structures were determined via NMR and MS, and their absolute configurations were elucidated using ECD, and X-ray crystallographic analysis, as well as the modified Mosher ester method. All isolates were evaluated for their inhibitory effects on IL6-induced STAT3 promoter activation in stably transfected Hep3B cells. Of these isolates, eudebeiolide D exhibited an inhibitory effect with the IC50 value of 1.1 μM.

摘要

从荔枝草地上部分的乙醇可溶提取物中分离出7种桉叶烷型倍半萜内酯和已知的柔毛内酯C。通过核磁共振(NMR)和质谱(MS)确定了它们的结构,并使用电子圆二色谱(ECD)、X射线晶体学分析以及改良的莫舍尔酯法阐明了它们的绝对构型。评估了所有分离物对稳定转染的Hep3B细胞中白细胞介素6(IL6)诱导的信号转导和转录激活因子3(STAT3)启动子激活的抑制作用。在这些分离物中,桉叶柔毛内酯D表现出抑制作用,半数抑制浓度(IC50)值为1.1 μM。

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