Studies On Chemical Constituents Of Acid Degration Products Of The Total Ginsenosides From The Panax Ginseng And Structural Modification Of Panaxadiol

Ginsenosides are considered to be the main bioactive constituents of Panax ginseng,which have a range of biological activities including anticancer, angiogenesis, andneuroprotective effects. Ginsenosides have shown better anticancer activities in earlierstudyies, and can overcome the common serious adverse reaction of chemotherapy drugs.Thus, ginsenosides could serve as the lead compounds and structural modification may benecessary to obtain effective antitumor drugs.In this paper, based on the previous work of our group, we designed and synthesized20(R)-panaxadiol,20(R)-panaxatriol, neopanaxadiol,20(S)-damar ane-3β,12β,20,25-tetroland dammar-24-ene-3β,6α,12β,20(R)-tetrol, which achieved from acid hydrolysate of thetotal ginsenosides of Panax ginseng C. A. Meyer (Araliaceae). Our structural modificationwas mainly objective to20(R)-panaxadiol (compound1) with the reaction of BF3-Et2O; themethod operation was simple, and the product yield was higher. Here we got a new skeletonof ginsenosides, A-neo-dammar-8-ene-19,24-epoxy-11-hydroxy (compound6) that was notseen in the literature so far.We also studied the antitumor activity of the structure modified product in vitro byMTT method to exam the inhibitory effect against human cancer HePG-2, HCT116,SH-SY5Y cells. Preliminary results showed that the structure modified product had thedifferent degree on damaging effect to the cancer HePG-2, HCT116, SH-SY5Y cells. Andcompound6performaned better anti-tumor activity against HCT116cells than other twocells.