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云南萜烯G,一种从[植物名称]根中提取的螺环三萜,可下调佛波酯分化的THP-1细胞中CD147和基质金属蛋白酶的表达。

Yunnanterpene G, a spiro-triterpene from the roots of , downregulates the expression of CD147 and MMPs in PMA differentiated THP-1 cells.

作者信息

Lu Ni-Hong, Zhang Zi-Wei, Guo Rui-Wei, Yang Li-Xia, Song Ya-Xian, Ye Jin-Shan, Shi Yan-Kun

机构信息

Department of Postgraduate, Kunming Medical University Yunnan 650500 P. R. China.

Department of Cardiology, Kunming General Hospital of Chengdu Military Area Yunnan 650032 P. R. China

出版信息

RSC Adv. 2018 Apr 20;8(27):15036-15043. doi: 10.1039/c8ra01895b. eCollection 2018 Apr 18.

Abstract

A new cycloartane triterpene, yunnanterpene G (1), containing an oxaspiro[5.4]decane moiety, was purified from the roots of . The new structure was determined from spectroscopic data and the X-ray diffraction method. Biological evaluations revealed that compound 1 significantly inhibited the mRNA expression of the atherosclerosis-related adhesion molecule CD147 (extracellular matrix metalloproteinase inducer, EMMPRIN), and proteolytic enzymes matrix metalloproteinase 2 (MMP-2), MMP-9 and MMP-14, in a dose-dependent manner in phorbol-12-myristate-13-acetate-induced human monocytic THP-1 cells by quantitative real-time PCR method. At the same time, the migration ability of the induced THP-1 cells was potently inhibited. Furthermore, western blot experiments showed that compound 1 at 25 μM strongly suppressed phosphorylation of NF-κB p65 and p38 MAPK in the differentiated THP-1 cells.

摘要

从……的根中纯化出一种新的环阿尔廷烷三萜,云南萜G(1),其含有氧杂螺[5.4]癸烷部分。通过光谱数据和X射线衍射方法确定了新结构。生物学评价显示,化合物1在佛波醇-12-肉豆蔻酸酯-13-乙酸酯诱导的人单核细胞THP-1细胞中,通过定量实时PCR法以剂量依赖性方式显著抑制动脉粥样硬化相关黏附分子CD147(细胞外基质金属蛋白酶诱导剂,EMMPRIN)以及蛋白水解酶基质金属蛋白酶2(MMP-2)、MMP-9和MMP-14的mRNA表达。同时,诱导的THP-1细胞的迁移能力受到有效抑制。此外,蛋白质印迹实验表明,25μM的化合物1强烈抑制分化的THP-1细胞中NF-κB p65和p38 MAPK的磷酸化。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c2d2/9079972/b65b098a4a37/c8ra01895b-f1.jpg

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