期刊
PHARMACEUTICS
卷 13, 期 12, 页码 -出版社
MDPI
DOI: 10.3390/pharmaceutics13122138
关键词
berberine derivative; hypoglycemic agents; hyperglycemia; in vivo; antidiabetic
The new berberine derivative SHE-196 showed significant hypoglycemic activity by increasing insulin sensitivity and improving glucose tolerance, reducing obesity and fat mass, and increasing brown fat activity in obese T2DM mice. These effects were confirmed histologically, indicating potential as a therapeutic agent for diabetes mellitus treatment.
Berberine is well known for its ability to reduce the blood glucose level, but its high effective dose and poor bioavailability limits its use. In this work we synthesized a new derivative of berberine, 9-(hexylamino)-2,3-methylenedioxy-10-methoxyprotoberberine chloride (SHE-196), and analyzed the profile of its hypoglycemic effects. Biological tests have shown that the substance has a very pronounced hypoglycemic activity due to increased insulin sensitivity after single and multiple dosing. In obese type 2 diabetes mellitus (T2DM) mice, it was characterized by improved glucose tolerance, decreased fasting insulin levels and sensitivity, decreased total body weight and interscapular fat mass, and increased interscapular brown fat activity. All these effects were also confirmed histologically, where a decrease in fatty degeneration of the liver, an improvement in the condition of the islets of Langerhans and a decrease in the size of fat droplets in brown adipose tissue were found. Our results indicate that 9-(hexylamino)-2,3-methylenedioxy-10-methoxyprotoberberine chloride could be the first in a new series of therapeutic agents for the treatment of diabetes mellitus.
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