Synthesis,Characterization And Studies On Anti-cancer Activities Of 18β-Glycyrrhetinic Acid Derivatives

Malignant neoplasm (also known as cancer) seriously threat to human health, medicine workers have been committed to research cancer treatment over the years and tried to find the most effective way to treat cancer. A great deal of scientific researches proved that one of methods to obtain drug with high anticancer activity is that natural products with certain anticancer activity can be used as lead compounds and modified to synthesis novel anticancer drug.18β-Glycyrrhetinic acid, the main component of the extracts from liquorice root, is a pentacyclic triterpenoid compound. Glycyrrhizic acid can be metabolized to produce glycyrrhetinic acid in vivo. Glycyrrhetinic acid has been widely used in clinic and has a very broad development prospect because of its variety pharmacological effects such as anti-inflammatory, anticancer, anti-viral, anti-ulcer, anti-allergenic and anti-oxidative.In order to obtain drugs with high anticancer activity for cancer treatment, a natural compound,18β-glycyrrhetinic acid, with certain anticancer activity was used as lead compound. We modified its structure to synthesis novel derivatives and tested their anticancer activities to find some safe, low toxicity and stable innovative target molecules drugs or new lead compounds, meanwhile discussing the structure-activity relationship and lay the foundation for future research.In this paper, the research work can be divided into three parts:The first part has a brief introduction about glycyrrhetinic acid and introduced its biological activity, research progress and developmental prospects. Then we introduced the foundation, objective, significance, research content and innovations of this project.The second part we designed a series derivatives of glycyrrhetinic acid. We obtained a total of 40 derivatives through the modified and transformed the 30-COOH, 3-OH of glycyrrhetinic acid and used NMR, MS to identify the structure of those derivatives.The third part we used MTT assay to study the anticancer activity of those derivatives we have obtained against human breast cancer MCF-7, MBA-MD-231 cell lines and discussed the structure-activity relationship of those compounds. Meanwhile, we made the conclusion and prospect about our work.