Structure activity relationships and antinociceptive activity of two novel dammarane-type sapogenins with notable anticancer effect

Publication date: October 2018 Source:Phytochemistry Letters, Volume 27 Author(s): Youzhen Zhang, Shanshan Chen, Lu Ma, Xude Wang, Guangyue Su, Yuqing Zhao This current study aimed to investigate the antinociceptive effect of 20(R)-25-methoxydammarane-3β, 12β, 20-triol (25-OCH3-PPD) and 20(R)-dammarane-3β, 12β, 20, 25-tetrol (25-OH-PPD), the two novel dammarane-type anticancer sapogenins isolated from ginseng. And the structure activity relationship of various ginseng sapogenins and saponins was also discussed. The effect was studied in hot-plate test and acetic acid induced abdominal writhing test. The results demonstrated that 25-OCH3-PPD and 25-OH-PPD (10, 20, 40 mg/kg) dose-dependently increased the latency time and antinociceptive percentage in hot-plate test. They also significantly inhibited the acetic acid-induced abdominal writhing. In structure activity relationship analysis of antinociceptive effect, we found ginseng sapogenins are more effective than saponins especially in acetic acid induced abdominal writhing test. The number of sugar moieties and substituent groups in side chain affect the antinociceptive activity between sapogenins and saponins. These findings provide original data and scientific evidence to support novel sapogenins as leading compounds in new antinociceptive agents and for newly natural product with dual effect of anticancer and antinociceptive. Graphical abstract
Source: Phytochemistry Letters - Category: Chemistry Source Type: research