Synthesis and in vitro evaluation of 12-(substituted aminomethyl) berberrubine derivatives as anti-diabetics |
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| Institution: | 1. State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China;2. Beijing Analytical Application Center, Shimadzu (China) Company, Ltd., Beijing 100020, China;1. School of Chinese Materia Medica, Tianjin University of Traditional Chinese Medicine, Tianjin 300193, PR China;2. Tianjin State Key Laboratory of Modern Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin 300193, PR China |
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| 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. |
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| Keywords: | Anti-diabetic activity Type 2 diabetes mellitus 12-(Substituted aminomethyl) berberrubine derivatives Synthesis |
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