Thirteen novel NO-releasing derivatives of betulinic acid （BA） bearing two types of NO-donors （nitrates and furoxans） were synthesized and evaluated for their antitumor activity. The results showed that furoxan-ba...Thirteen novel NO-releasing derivatives of betulinic acid （BA） bearing two types of NO-donors （nitrates and furoxans） were synthesized and evaluated for their antitumor activity. The results showed that furoxan-based derivatives exhibited higher antitumor activity than nitrate-based derivatives, with compounds lla and llb displaying promising potency against B16 cell lines and HepG2 cell lines （IC50 〈 1 μmol/L）. We supposed that NO-releasing amount of these derivatives which can be detected by Griess method may contribute more to their antitumor activity. As a result, furoxan-based derivatives released larger amount of NO than that of nitrate-based derivatives, which partially explained the higher anti-tumor activity of the former.展开更多
基金financially supported by the National Natural Science Foundation of China (No.20972190)the Academic Leadership of ‘Qing Lan’ Project of Jiangsu Department of Education
文摘Thirteen novel NO-releasing derivatives of betulinic acid （BA） bearing two types of NO-donors （nitrates and furoxans） were synthesized and evaluated for their antitumor activity. The results showed that furoxan-based derivatives exhibited higher antitumor activity than nitrate-based derivatives, with compounds lla and llb displaying promising potency against B16 cell lines and HepG2 cell lines （IC50 〈 1 μmol/L）. We supposed that NO-releasing amount of these derivatives which can be detected by Griess method may contribute more to their antitumor activity. As a result, furoxan-based derivatives released larger amount of NO than that of nitrate-based derivatives, which partially explained the higher anti-tumor activity of the former.
