Synthetic Kavalactone Analogues with Increased Potency and Selective Anthelmintic Activity against Larvae of Haemonchus contortus In Vitro
HMP Dilrukshi Herath, Aya C Taki, Nguyen Nghi, Jose Garcia-Bustos, Andreas Hofmann, Tao Wang, Guangxu Ma, Bill CH Chang, Abdul Jabbar, Brad E Sleebs, Robin B Gasser
Molecules | MDPI | Published : 2020
Kava extract, an aqueous rhizome emulsion of the plant Piper methysticum, has been used for centuries by Pacific Islanders as a ceremonial beverage, and has been sold as an anxiolytic agent for some decades. Kavalactones are a major constituent of kava extract. In a previous investigation, we had identified three kavalactones that inhibit larval development of Haemonchus contortus in an in vitro-bioassay. In the present study, we synthesized two kavalactones, desmethoxyyangonin and yangonin, as well as 17 analogues thereof, and evaluated their anthelmintic activities using the same bioassay as employed previously. Structure activity relationship (SAR) studies showed that a 4-substituent on t..View full abstract
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This research was funded by the Australian Research Council, Yourgene Health Singapore, and The University of Melbourne. B.E.S. is a Corin Centenary Fellow.