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来自[植物名称]地上部分的具有前体蛋白转化酶枯草溶菌素9(PCSK9)mRNA表达抑制活性的异戊烯基黄酮苷

Prenylated Flavonoid Glycosides with PCSK9 mRNA Expression Inhibitory Activity from the Aerial Parts of .

作者信息

Kim Eeray, Kim Young-Mi, Ahn Jongmin, Chae Hee-Sung, Chin Young-Won, Kim Jinwoong

机构信息

College of Pharmacy and Research Institute of Pharmaceutical Sciences, Seoul National University, Seoul 08826, Korea.

出版信息

Molecules. 2021 Jun 11;26(12):3590. doi: 10.3390/molecules26123590.

Abstract

Phytochemical investigation on the -BuOH-soluble fraction of the aerial parts of using the PCSK9 mRNA monitoring assay led to the identification of four previously undescribed acylated flavonoid glycosides and 18 known compounds. The structures of new compounds were elucidated by NMR, MS, and other chemical methods. All isolated compounds were tested for their inhibitory activity against PCSK9 mRNA expression in HepG2 cells. Of the isolates, compounds , , , , and - were found to significantly inhibit PCSK9 mRNA expression. In particular, compound was shown to increase LDLR mRNA expression. Thus, compound may potentially increase LDL uptake and lower cholesterol levels in the blood.

摘要

使用前蛋白转化酶枯草溶菌素9(PCSK9)mRNA监测试验对[植物名称]地上部分的正丁醇可溶级分进行植物化学研究,从而鉴定出四种先前未描述的酰化黄酮苷和18种已知化合物。通过核磁共振(NMR)、质谱(MS)和其他化学方法阐明了新化合物的结构。对所有分离出的化合物进行了在肝癌细胞系(HepG2)中对PCSK9 mRNA表达的抑制活性测试。在这些分离物中,发现化合物[具体化合物编号1]、[具体化合物编号2]、[具体化合物编号3]、[具体化合物编号4]和[具体化合物编号5]能显著抑制PCSK9 mRNA表达。特别地,化合物[具体化合物编号5]显示可增加低密度脂蛋白受体(LDLR)mRNA表达。因此,化合物[具体化合物编号5]可能潜在地增加低密度脂蛋白摄取并降低血液中的胆固醇水平。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2274/8230864/1861c5473d9c/molecules-26-03590-g001.jpg

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