title: Synthesis and preliminary biologic activity evaluation of nitric oxide-releasing andrographolide derivatives in RIN-m cells.
abstract: Pancreatic β-cell dysfunction and death are important feature of diabetes mellitus. Beta-cell protection has demonstrated clinical benefits in the treatment of this disease. In the present study, andrographolide derivatives with nitric oxide (NO)-releasing capability were synthesized and their protective effects against tert-butyl hydroperoxide (t-BHP) induced cell damage were investigated in RIN-m cells. Compound 6b was found to release a moderate amount of NO and was more potent than its natural parent andrographolide in inhibiting cell apoptosis. These findings suggested that andrographolide derivatives with NO-releasing capacity may be a potential therapy for diabetes.
authors.affiliation: Institute of New Drug Research and Guangdong Province Key Laboratory of Pharmacodynamic Constituents of Traditional Chinese Medicine, Jinan University College of Pharmacy.
authors.forename: Zhibin
authors.initials: Z
authors.lastname: Liang
authors.forename: Enming
authors.initials: E
authors.lastname: Du
authors.forename: Lipeng
authors.initials: L
authors.lastname: Xu
authors.forename: Yewei
authors.initials: Y
authors.lastname: Sun
authors.forename: Gaoxiao
authors.initials: G
authors.lastname: Zhang
authors.forename: Pei
authors.initials: P
authors.lastname: Yu
authors.forename: Yuqiang
authors.initials: Y
authors.lastname: Wang
mesh_terms: D000818:Animals; D017209:Apoptosis / Q000187:drug effects; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D004224:Diterpenes / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D008968:Molecular Conformation; D009569:Nitric Oxide / Q000737:chemistry / Q000378:metabolism*; D051381:Rats; D013329:Structure-Activity Relationship; D020122:tert-Butylhydroperoxide / Q000037:antagonists & inhibitors / Q000494:pharmacology
chemical_list: D004224:Diterpenes; D009569:Nitric Oxide; C030419:andrographolide; D020122:tert-Butylhydroperoxide