Pharmacological activities of steroidal saponins

The biological activity research and clinical application of natural steroidal saponins was first patented in France. It was reported that diosgenin and its glycosides have anti-arthritic effects. Researchers from the former Soviet Union discovered that the saponin extract in Caucasian dioscorea has a cholesterol-lowering effect, and clinical experiments have also proven this. In the 1980s, Ravikumer et al. [8] discovered that diosgenin in Yunnan Baiyao has anti-cancer activity. A new steroidal saponin (afromontoside) isolated from the Agave plant (Dracaena afromontan) has the activity of inhibiting KB cells [9]. In addition, the cellobioside synthesized by Pfizer Pharmaceuticals Company of the United States using tigogenin and hecogenin as the steroid core has a strong hypolipidemic effect [10]. There are also many reports on the biological activities of steroidal saponins in my country. For example, steroidal saponins isolated from plants of the genus Chonglou have hemostatic, immunomodulatory, anti-tumor and effects on the cardiovascular system [11]. Dioscorea saponin II isolated from Dioscorea collettii has obvious cholesterol-lowering activity. Dioscin extracted from D. nipponica has obvious antitussive, expectorant and antiasthmatic activities. At present, several domestic factories use different species of Dioscorea plants as raw materials to extract total steroidal saponins as clinical anti-hyperlipidemic drugs. Among them, the new drug "D. zingibernsis" was successfully developed using Dioscorea zingibernsis as raw materials "Ye Guan Xin Ning" has certain curative effect in the clinical treatment of coronary heart disease and angina pectoris. The marketed "Di'ao Xinxuekang" is also a drug for lowering blood lipids. The drug is a mixture of diosgenin extracted from the rhizome of D. panthaica, which includes monosaccharide, disaccharide, etc., but so far the author There are no reports proving its active ingredients.

It has always been our goal to systematically study the chemical and biological activities of steroidal saponins, find active lead compounds, and further develop them into new drugs. However, through the work of isolating and purifying steroidal saponins, we found that it is time-consuming, laborious and uneconomical to separate and purify the mixed saponins with very low content from plants one by one to obtain pure products, and then screen their pharmacological activities. Because the content of saponins in plants is very low and the separation process is complicated, it is difficult to use in industrial production. Compared with saponin, sapogenin is easier to separate and obtain, and the separation and purification process is easier to industrialize. Therefore, steroidal saponins can be used as the mother core, and directional semi-synthetic steroidal saponins can be screened for pharmacological activity by referring to the known connection methods of sugars in natural steroidal saponins, and then the relationship between structure and activity can be studied to develop effective but toxic New drugs with few side effects. Glycosylation of saponins to synthesize a large number of various saponins with pharmacological activity is not only beneficial to the development of new drugs, but also promotes the further deepening of steroidal saponin research. Therefore, the study of natural and semi-synthetic steroidal saponins is an area worthy of development in drug innovation.