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卡德可可类A-K,来自Kadsura coccinea的三类,具有抑制PCSK9表达的活性

Yelin Duan¹, Tong Chen², Pengju Guo³

¹School of Chinese Materia Medica, Nanjing University of Chinese Medicine, Nanjing, 210023, China; State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 501 Haike Road, Shanghai, 201203, China.

|June 16, 2025

概括

从Kadsura coccinea中发现了两个新的三类. 一种化合物降低了PCSK9蛋白水平,并增加了细胞中的LDL吸收,这表明了潜在的治疗应用.

科学领域:

自然产品化学自然产品化学
药用化学医学化学
药理学药理学是指药理学的学科.

背景情况:

卡德苏拉 (Kadsura coccinea) 是生物活性化合物的植物来源.
三聚类是一种多样化的自然产品类别,具有各种各样的生物活动.
蛋白转化酶亚素/素9型 (PCSK9) 在胆固醇代谢中起着至关重要的作用.

研究的目的:

从Kadsura coccinea中分离和表征新的三类植物.
评估孤立化合物在调节PCSK9蛋白水平和低密度脂蛋白 (LDL) 吸收方面的潜力.

主要方法:

使用色谱技术分离化合物.
通过广泛的光谱分析 (NMR,MS),莫舍尔方法,X射线晶体学和电子圆二元化 (ECD) 计算来阐明结构.
使用HepG2细胞进行体外测定,以评估PCSK9蛋白水平和LDL吸收.

主要成果:

分离了两种新型原类型三基 (Kadcoccinoid A和B) 和九种新型lanostane类型三基,以及九种已知的化合物.
卡德科奇诺伊德A具有独特的6/6/8融合式碳循环核心,具有双循环[4.2.1]无-9-one系统.
卡德科西诺伊德B显著降低了PCSK9蛋白水平 (78.4%在10μM的抑制) 并增强了HepG2细胞中的LDL吸收.
化合物12-14表现出中度的PCSK9抑制活性.

结论:

对Kadsura coccinea的化学研究产生了结构多样化的三类,包括具有独特骨的新型化合物.
卡德科西诺伊德B通过向PCSK9通路,显示出对管理高胆固醇血清症有前途的潜力.
对Kadcoccinoid B的作用机制和体内疗效的进一步研究是有必要的.

关键词:

卡德苏拉科奇尼亚 (Kadsura coccinea) 是一个虫.拉诺斯坦类型的三烯酸.在PCSK9中原始体类型的三基化物.石树科 (Schisandraceae) 是一个植物.

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