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Yunnanterpene G, a spiro-triterpene from the roots of Cimicifuga foetida, downregulates the expression of CD147 and MMPs in PMA differentiated THP-1 cells†
RSC Advances ( IF 3.9 ) Pub Date : 2018-04-20 00:00:00 , DOI: 10.1039/c8ra01895b
Ni-Hong Lu 1 , Zi-Wei Zhang 2 , Rui-Wei Guo 2 , Li-Xia Yang 2 , Ya-Xian Song 1 , Jin-Shan Ye 2 , Yan-Kun Shi 2
Affiliation  

A new cycloartane triterpene, yunnanterpene G (1), containing an oxaspiro[5.4]decane moiety, was purified from the roots of Cimicifuga foetida. 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.

中文翻译:

Yunterpene G 是一种来自 Cimicifuga foetida 根的螺三萜,可下调 PMA 分化的 THP-1 细胞中 CD147 和 MMPs 的表达†

从Cimicifuga foetida的根中提纯出一种新的环阿坦三萜,即 yunnanterpene G ( 1 ),它含有氧螺[5.4]癸烷部分。新结构由光谱数据和 X 射线衍射法确定。生物学评估表明,化合物1在佛波醇中以剂量依赖性方式显着抑制动脉粥样硬化相关粘附分子 CD147(细胞外基质金属蛋白酶诱导剂,EMMPRIN)和蛋白水解酶基质金属蛋白酶 2(MMP-2)、MMP-9 和 MMP-14 的 mRNA 表达-12-myristate-13-acetate 通过定量实时 PCR 方法诱导人单核细胞 THP-1 细胞。同时,诱导的THP-1细胞的迁移能力被有效抑制。此外,蛋白质印迹实验表明,25 μM 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。
更新日期:2018-04-20
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