Synthesis, biological evaluation of prenylflavonoids as vasorelaxant and neuroprotective agents.
A series of prenylflavonoids with multiple hydroxyl groups were synthesized and evaluated for their vasorelaxant activities against rat aorta rings pre-contracted by phenylephrine (PE), as well as their neuroprotective effects against OGD induced PC12 cell injury. The results indicated that the prenyl group at A-ring of prenylflavonoids, as well as hydroxyl groups at B-ring was important for their activities. (+/-)Leachianone G 1b, bearing 8-prenyl and 2',4'-dihydoxyl groups, exhibited the most potent vasorelaxant and neuroprotective effects.
Dong
Xiaowu
X
ZJU-ENS Joint Laboratory of Medicinal Chemistry, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, China.
Qi
Lingling
L
Jiang
Chaoyi
C
Chen
Jing
J
Wei
Erqing
E
Hu
Yongzhou
Y
D000818:Animals; D001011:Aorta / Q000187:drug effects / Q000502:physiology; D002867:Chromones; D005419:Flavonoids / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D018696:Neuroprotective Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D016716:PC12 Cells; D051381:Rats; D013329:Structure-Activity Relationship; D014664:Vasodilation / Q000187:drug effects*
D002867:Chromones; D005419:Flavonoids; D018696:Neuroprotective Agents; C523322:leachianone A