Key Laboratory of Ethnomedicine (Minzu University of China), Ministry of Education, Beijing 100081, PR China; School of Pharmacy, Minzu University of China, Beijing 100081, China.
School of Pharmacy, Minzu University of China, Beijing 100081, China.
Bioorg Chem. 2021 Jan;106:104470. doi: 10.1016/j.bioorg.2020.104470. Epub 2020 Nov 10.
Gynostemma pentaphyllum has been used as a medicine-food homologious health product in China for a long time. This research aimed to isolate and identify its active compounds with protective effects against hydrogen peroxide induced SH-SY5Y cell death. Four new dammarane-type saponins were isolated from G. pentaphyllum using various chromatographic methods. They were identified as gypenoside S (1), gypenoside S (2), gypenoside S (3) and gypenoside S (4), respectively by HRESIMS and NMR spectra. Their cytotoxic activity was evaluated against three human cancer cell lines, A549 (lung), HepG2 (liver), SH-SY5Y (nerve), by MTT method. They showed low cytotoxicities with the IC values of more than 100 μM on three cancer cell lines. However, they appeared protective effects against hydrogen peroxide induced SH-SY5Y cell death in a dose-dependent manner. They recovered cell viability more than 69% at the concentration of 20 μM from 66%, while as vitamin C to 67%. Compound 3 and 4 recovered more than 79% at 100 μM. The present study suggests that G. pentaphyllum has antioxidative potential and the saponins from G. pentaphyllum are considered as the active compounds with safe and neuroprotecitve effect.
绞股蓝在中国长期以来一直被用作药食同源的保健品。本研究旨在分离和鉴定其具有保护作用的活性化合物，以对抗过氧化氢诱导的 SH-SY5Y 细胞死亡。通过各种色谱方法从绞股蓝中分离得到四种新的达玛烷型皂苷。通过 HRESIMS 和 NMR 光谱分别鉴定为绞股蓝皂苷 S（1）、绞股蓝皂苷 S（2）、绞股蓝皂苷 S（3）和绞股蓝皂苷 S（4）。通过 MTT 法评估它们对三种人癌细胞系 A549（肺）、HepG2（肝）和 SH-SY5Y（神经）的细胞毒性。它们对三种癌细胞系的 IC 值均大于 100 μM，显示出低细胞毒性。然而，它们以剂量依赖性方式表现出对过氧化氢诱导的 SH-SY5Y 细胞死亡的保护作用。在 20 μM 浓度下，它们的细胞活力恢复超过 69%，而维生素 C 则恢复到 67%。化合物 3 和 4 在 100 μM 时恢复超过 79%。本研究表明，绞股蓝具有抗氧化潜力，绞股蓝中的皂苷被认为是具有安全和神经保护作用的活性化合物。
