title: Synthesis and in vitro evaluation of 12-(substituted aminomethyl) berberrubine derivatives as anti-diabetics.
abstract: By introducing various amino methyl groups into 12-position of berberrubine, a series of 12-(substituted aminomethyl) berberrubine derivatives were synthesized and evaluated for their anti-diabetic activity against type 2 diabetes mellitus. The results indicated that most of the prepared compounds exhibited moderate to good anti-diabetic activity, which were comparable to or even better than the berberine, the positive control rosiglitazone and insulin. Especially, compound 3b with an N-methyl piperazine-4-methyl group at C-12, exerted the most powerful anti-diabetic activity.
authors.affiliation: Key Laboratory of Drug-Targeting and Drug Delivery System of the Education Ministry, Department of Medicinal Chemistry, West China School of Pharmacy, Sichuan University, Chengdu 610041, China.
authors.forename: Renjun
authors.initials: R
authors.lastname: Li
authors.affiliation: Key Laboratory of Drug-Targeting and Drug Delivery System of the Education Ministry, Department of Medicinal Chemistry, West China School of Pharmacy, Sichuan University, Chengdu 610041, China.
authors.forename: Jianbo
authors.initials: J
authors.lastname: Wu
authors.affiliation: Key Laboratory of Drug-Targeting and Drug Delivery System of the Education Ministry, Department of Medicinal Chemistry, West China School of Pharmacy, Sichuan University, Chengdu 610041, China.
authors.forename: Yun
authors.initials: Y
authors.lastname: He
authors.affiliation: Key Laboratory of Drug-Targeting and Drug Delivery System of the Education Ministry, Department of Medicinal Chemistry, West China School of Pharmacy, Sichuan University, Chengdu 610041, China.
authors.forename: Li
authors.initials: L
authors.lastname: Hai
authors.affiliation: Key Laboratory of Drug-Targeting and Drug Delivery System of the Education Ministry, Department of Medicinal Chemistry, West China School of Pharmacy, Sichuan University, Chengdu 610041, China. Electronic address: wyong@scu.edu.cn.
authors.forename: Yong
authors.initials: Y
authors.lastname: Wu
mesh_terms: D041721:3T3-L1 Cells; D017667:Adipocytes / Q000187:drug effects*; D000818:Animals; D001599:Berberine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D003924:Diabetes Mellitus, Type 2 / Q000188:drug therapy* / Q000473:pathology; D004305:Dose-Response Relationship, Drug; D005947:Glucose / Q000493:pharmacokinetics; D007004:Hypoglycemic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D007333:Insulin Resistance; D051379:Mice; D015394:Molecular Structure; D018485:Muscle Fibers, Skeletal / Q000187:drug effects*; D051381:Rats; D013329:Structure-Activity Relationship
chemical_list: D007004:Hypoglycemic Agents; D001599:Berberine; C115958:berberrubine; D005947:Glucose
keywords: 12-(Substituted aminomethyl) berberrubine derivatives; Anti-diabetic activity; Synthesis; Type 2 diabetes mellitus