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- W2794469180 abstract "Plasmodium falciparum dihydroorotate dehydrogenase (Pf DHODH ) is a promising drug target for antimalarial chemotherapy. In our continuous efforts to develop more potent Pf DHODH inhibitors, a unique library of active ingredients from traditional Chinese medicine ( TCM ) has been collected and was screened in this study. Through the initial screening, we found that coptisine, a natural alkaloid from TCM Coptidis Rhizoma , was a novel and potent inhibitor of Pf DHODH with an IC 50 value of 1.83 ± 0.08 μ m . At the same time, enzyme kinetic analysis using Lineweaver‐Burk plot indicated that coptisine is an uncompetitive inhibitor for Pf DHODH . Thermal shift assay and molecular docking simulation research reveal that coptisine is capable of binding with Pf DHODH . Moreover, coptisine exhibits weak inhibition activity against human DHODH , indicating that coptisine is a selective inhibitor of Pf DHODH . Taken together, our study highlights the potential of active ingredients in TCM as valuable resource for discovering novel chemical scaffolds for Pf DHODH ." @default.
- W2794469180 created "2018-04-06" @default.
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- W2794469180 date "2018-05-12" @default.
- W2794469180 modified "2023-09-30" @default.
- W2794469180 title "Coptisine, a natural alkaloid from <i>Coptidis Rhizoma</i> , inhibits plasmodium falciparum dihydroorotate dehydrogenase" @default.
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- W2794469180 doi "https://doi.org/10.1111/cbdd.13197" @default.
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