具有前蛋白转化酶枯草杆菌蛋白酶/kexin 9型表达和分泌抑制活性的化学成分。
Chemical constituents from with proprotein convertase subtilisin/kexin type 9 expression and secretion inhibitory activity.
作者信息
Won Hongic, Son Min-Gyung, Pel Pisey, Nhoek Piseth, An Chae-Yeong, Kim Young-Mi, Chae Hee-Sung, Chin Young-Won
机构信息
College of Pharmacy and Research Institute of Pharmaceutical Sciences, Seoul National University, Seoul 08826, Republic of Korea.
出版信息
Org Biomol Chem. 2023 Mar 29;21(13):2801-2808. doi: 10.1039/d3ob00225j.
Six new flavanones, including sanggenol W (1), morusalnol D-F (2-4) and neovanone A and B (5 and6), and fourteen known compounds were isolated from the methanol extract of the dried root bark of using various column chromatographic methods. Their structures were elucidated using spectroscopic methods. The isolated compounds were tested for LDLR, PCSK9 and IDOL mRNA regulatory activity, and it was found that betulinic acid (13) showed the most potent effect on downregulation of PCSK9 and upregulation of LDLR at both mRNA and protein levels, showing comparable results to berberine, the positive control. In addition, betulinic acid (13) inhibited PCSK9 secretion, indicating its role as a future PCSK9 synthesis inhibitor.
采用多种柱色谱方法，从桑根干燥根皮的甲醇提取物中分离出6种新的黄烷酮，包括桑根醇W（1）、桑莫醇D - F（2 - 4）以及新黄烷酮A和B（5和6），还有14种已知化合物。通过光谱方法阐明了它们的结构。对分离得到的化合物进行了低密度脂蛋白受体（LDLR）、前蛋白转化酶枯草溶菌素9（PCSK9）和诱导降解物1（IDOL）mRNA调节活性测试，发现桦木酸（13）在mRNA和蛋白质水平上对PCSK9的下调和LDLR的上调显示出最显著的效果，与阳性对照黄连素的结果相当。此外，桦木酸（13）抑制PCSK9分泌，表明其作为未来PCSK9合成抑制剂的作用。
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