来源于绞股蓝的具有前蛋白转化酶枯草溶菌素 9 抑制活性的达玛烷型皂甙。
Dammarane-type saponins with proprotein convertase subtilisin/kexin type 9 inhibitory activity from Gynostemma pentaphyllum.
机构信息
Department of TCMs Pharmaceuticals ＆ Department of Natural Medicinal Chemistry, School of Traditional Chinese Pharmacy, China Pharmaceutical University, Nanjing, 211198, People's Republic of China; Cardiology Department, Nanjing Lishui District Hospital of Traditional Chinese Medicine, Nanjing, 211200, People's Republic of China; Laboratory of Translational Medicine, Affiliated Hospital of Integrated Traditional Chinese and Western Medicine, Nanjing University of Chinese Medicine, Nanjing, 210028, People's Republic of China.
Department of TCMs Pharmaceuticals ＆ Department of Natural Medicinal Chemistry, School of Traditional Chinese Pharmacy, China Pharmaceutical University, Nanjing, 211198, People's Republic of China; Laboratory of Translational Medicine, Affiliated Hospital of Integrated Traditional Chinese and Western Medicine, Nanjing University of Chinese Medicine, Nanjing, 210028, People's Republic of China.
出版信息
Phytochemistry. 2022 Feb;194:113005. doi: 10.1016/j.phytochem.2021.113005. Epub 2021 Nov 16.
Seven undescribed dammarane-type saponins, gypenosides LXXXI-LXXXVII, together with four known compounds, were isolated from the whole herb of Gynostemma pentaphyllum. The chemical structures of these undescribed compounds were elucidated on the basis of physical and spectroscopic analysis and comparison with literature data. All the isolates were evaluated for their proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitory activities in HepG2 cells. Among them, gypenosides LXXXII-LXXXVII, gynosaponin II, IV and VI suppressed the expression of PCSK9 in LPDS-induced HepG2 cells at 20 μM; gypenosides LXXXII, LXXXV and LXXXVII showed inhibitory activities against PCSK9 at 10 μM; notably, gypenoside LXXXII still exhibited inhibitory activity against PCSK9 at 5 μM.
从绞股蓝全草中分离得到了七种新的达玛烷型皂苷，即绞股蓝皂苷 LXXXI-LXXXVII，以及四种已知化合物。根据物理和光谱分析以及与文献数据的比较，确定了这些未知化合物的化学结构。所有分离得到的化合物均在 HepG2 细胞中进行了前蛋白转化酶枯草杆菌蛋白酶/κexin 型 9（PCSK9）抑制活性评估。其中，绞股蓝皂苷 LXXXII-LXXXVII、绞股蓝皂苷 II、IV 和 VI 在 20 μM 时可抑制 LPDS 诱导的 HepG2 细胞中 PCSK9 的表达；绞股蓝皂苷 LXXXII、LXXXV 和 LXXXVII 在 10 μM 时对 PCSK9 表现出抑制活性；值得注意的是，绞股蓝皂苷 LXXXII 在 5 μM 时仍对 PCSK9 表现出抑制活性。
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