Synthesis of 2`-hydroxy-4`-isoprenyloxychalcone Derivatives with Potential Antidepressant-like Activity
Chao Xie, Zhou Peng, Shui-Lian Zhao, Cheng-Yan Pan, Li-Ping Guan and Xian-Yu Sun
Affiliation: Food and Pharmacy College, Zhejiang Ocean University, Zhoushan City, Zhejiang Province, 316022, P.R. China.
A series of 2´-hydroxy-4´-isoprenyloxychalcone derivatives was synthesized and evaluated for its antidepressant-
like activity using the FST and TST. All compounds exhibited the potential antidepressant-like activity in the FST
and the TST through intraperitoneal injection. Among them, compounds 4i, 4l and 4n exhibited more potent antidepressant-
like activity at a dose of 10 mg/kg. And, compounds 4i, 4l and 4n were also adequately absorbed in mice after oral
administration at a dose of 30 mg/kg. In the 5-HT induced head-twitch test and yohimbine induced mortality test, compound
4i could increase the head-twitch and rise mortality in mice. The results suggested that the antidepressant effects of
compound 4i may be related to via the serotonergic and noradrenergic system.
Keywords: 2´-Hydroxy-4´-isoprenyloxychalcone, synthesis, antidepressant-like activity, yohimbine, 5-hydroxytryptophan.
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