Two New Aristolochic Acid Analogues from the Roots of Aristolochia contorta with Significant Cytotoxic Activity.

Hong-Jian Ji, Jia-Yuan Li, Shi-Fei Wu, Wen-Yong Wu, Chang-Liang Yao, Shuai Yao, Jian-Qing Zhang, De-An Guo

Molecules (Basel, Switzerland) 2020 Dec 23

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Twelve compounds, including two new aristolochic acid analogues with a formyloxy moiety (9-10) and 10 known aristolochic acid derivates (1-8 and 11-12), were obtained from the roots of Aristolochiacontorta. Their structures were elucidated using extensive spectroscopic methods. Their cytotoxic activity in human proximal tubular cells HK-2 was evaluated by the MTT method, which has been widely used to assess cell viability. Among these molecules, compounds 3 and 9 were found to be more cytotoxic. Furthermore, molecular modeling was used to evaluate, for the first time, the interactions of compounds 3 and 9 with the target protein organic anionic transporter 1 (OAT1) that plays a key role in mediating aristolochic acid nephropathy. Structure-activity relationships are briefly discussed.

Citation

Hong-Jian Ji, Jia-Yuan Li, Shi-Fei Wu, Wen-Yong Wu, Chang-Liang Yao, Shuai Yao, Jian-Qing Zhang, De-An Guo. Two New Aristolochic Acid Analogues from the Roots of Aristolochia contorta with Significant Cytotoxic Activity. Molecules (Basel, Switzerland). 2020 Dec 23;26(1)