酸水解提高绞股蓝皂苷XLVI抗肝癌活性的研究

Study on the enhancement of anti-hepatocellular carcinoma activity of gypenoside XLVI by acid hydrolysis

目的此文基于酸水解技术探讨酸水解提高绞股蓝皂苷XLVI抗肝癌活性。方法筛选不同种类酸水解绞股蓝皂苷XLVI;并采用柱层析、薄层层析等技术分离纯化盐酸水解产物;最后采用MTT法和细胞形态观察,对转化产物绞股蓝皂苷TN-1的抗癌活性进行测定。结果盐酸水解绞股蓝皂苷XLVI最为彻底,获得化合物A、化合物B和化合物C共3个酸水解产物,其中化合物B经核磁共振鉴定是绞股蓝皂苷TN-1;经过水解后的产物绞股蓝皂苷TN-1的抗肝癌活性显著增强,对SMMC7721和Bel7402的IC50达到(36.65±12.31)µg/mL、(53.42±5.83)µg/mL。结论盐酸能够水解绞股蓝皂苷XLVI生成绞股蓝皂苷TN-1,显著提高其抗肝癌活性。

Objective To investigate the effect of acid hydrolysis on the anti-hepatocellular carcinoma activity of gypenoside XLVI.Methods Various types of acid hydrolyzed gypenoside XLVI were screened.and using column chromatography,thin layer chromatography to isolate and purify the hydrochloric acid hydrolysis product;finally,the anticancer activity of the transformed product,gynosaponin TN-1,was determined using MTT assay and cell morphology observation.Results Hydrolysis of gypenoside XLVI with hydrochloric acid was the most thorough,yielding three acid hydrolysis products,namely compound A,compound B,and compound C.Compound B was identified as gynosaponin TN-1 by nuclear magnetic resonance.The anti-hepatocellular carcinoma activity of the hydrolyzed product,gynosaponin TN-1,was significantly enhanced,with IC50 values of(36.65±12.31)µg/mL and(53.42±5.83)µg/mL for SMMC7721 and Bel7402,respectively.Conclusion Hydrochloric acid can hydrolyze gypenoside XLVI to generate gynosaponin TN-1,which significantly enhances its anti-hepatocellular carcinoma activity.