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Published on: May 26, 2023
Design, Synthesis, and Insecticidal Activity of the Derivatives of Taiwanin E, an Insecticidal Lignan from Taiwania
Feng Hao1, Chenzhe Li1, Yan Luo1
1Yunnan Characteristic Plant Extraction Laboratory, Key Laboratory of Medicinal Chemistry for Natural Resource, Functional Molecules Analysis and Biotransformation Key Laboratory of Universities in Yunnan Province, School of Pharmacy, School of Chemical Science and Technology, Yunnan University, Kunming 650091, China.
Abstract:
Rising environmental and health risks of synthetic pesticides have fueled the search for eco-friendly alternatives. Taiwania flousiana Gaussen, a rare evergreen, is a valuable source of bioactive compounds, with the lignan Taiwanin E (from its discarded bark in Yunnan, China) showing potential insecticidal activity. Herein, we chemically modified Taiwanin E to improve its solubility and insecticidal activity, and the resultant derivative E13 exhibited potent larvicidal activity against Armigeres subalbatus larvae. Enzyme assays, molecular docking, and dynamics simulations validated this activity, while DFT calculations clarified the structural basis for E13's superior performance. Bee toxicity tests further confirmed its environmental safety. This study identifies Taiwanin E derivatives as promising sustainable alternatives to conventional insecticides, advancing eco-friendly pest control and enabling resource utilization of the endangered T. flousiana.
