Two New Aristolochic Acid Analogues from the Roots of Aristolochia
contorta with Significant Cytotoxic Activity |
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| Authors: | Hong-Jian Ji Jia-Yuan Li Shi-Fei Wu Wen-Yong Wu Chang-Liang Yao Shuai Yao Jian-Qing Zhang De-An Guo |
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| Affiliation: | 1.School of Chinese Materia Medica, Nanjing University of Chinese Medicine, Xianlin Road #138, Nanjing 210023, China; (H.-J.J.); (W.-Y.W.);2.Shanghai Institue of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China; (J.-Y.L.); (S.-F.W.); (C.-L.Y.); (S.Y.); (J.-Q.Z.);3.Department of Pharmacy, Yancheng School of Clinical Medicine of Nanjing Medical University, Yancheng 224001, China |
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| Abstract: | 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 Aristolochia contorta. 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. |
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| Keywords: | Aristolochia contorta aristolochic acid cytotoxicity molecular docking |
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