Application of 15-benzal-14-deoxy-11, 12-dehydro-andrographolide derivatives in preparing medicines for treating diabetes mellitus
A technology of andrographolide and benzylidene, which is applied in the field of medicinal chemistry, can solve the problem of no hypoglycemic effect, achieve remarkable effects, clarify the hypoglycemic function, and expand the range of options
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Embodiment 1
[0023] Example 1 Drug A of the present invention and AD para-streptozotocin (STZ; 55mg / kg, once a day for 5 consecutive days; ip) induced hypoglycemic activity in diabetic mice
[0024] 1.1 Experimental materials
[0025] Drugs and reagents to be tested: the drug powder of the present invention is suspended in 0.5% carboxymethylcellulose sodium (CMC-Na) before use. Andrographolide (AD) was provided by Furen Pharmaceutical Group Co., Ltd. The drug of the present invention was synthesized by the inventor with a purity greater than 99.0%. Glucose determination kit (glucose oxidase-peroxidase method), produced by Shanghai Rongsheng Biopharmaceutical Co., Ltd., production batch number 20110501. Streptozotocin STZ is a product of Sigma (S-0130). Acarbose, Bayer Healthcare Co., Ltd., production batch number BJ02612, was prepared with 0.5% carboxymethylcellulose sodium (CMC-Na) to a 1 mg / mL suspension before use.
[0026] Test animals: Clean grade Kunming mice, male, weighing ...
Embodiment 2
[0038] Example 2 Hypoglycemic activity of drug B of the present invention on STZ (200mg / kg; ip) induced diabetic mice
[0039] 2.1 Experimental materials: the same as in Example 1.
[0040] 2.2 Experimental method
[0041] Take 30 healthy and normal mice, fast for 12 hours, without water, intraperitoneally inject STZ solution (25mg / ml), 200mg / (kg·d), 72 hours later, take blood to measure fasting blood glucose, blood glucose value ≥ 11.1 mmol / L That is, the modeling is successful.
[0042] Select 18 mice that successfully modeled, and randomly divide them into 3 groups: acarbose group (20 mg / kg), model group, and compound B group (1.35 mmol / kg), with 6 mice in each group. Another 6 healthy mice were used as normal control group. The normal control group and the model group were given 0.5% carboxymethylcellulose sodium (CMC-Na) by intragastric administration, the compound B group was given 0.5% CMC-Na suspension, and the acarbose group was given 0.5% CMC-Na suspension ...
Embodiment 3
[0048] Example 3 The influence of medicine A and B of the present invention on normal mouse blood sugar
[0049] 3.1 Experimental materials: the same as in Example 1.
[0050] 3.2 Experimental method
[0051] The normal control group was given 0.5% carboxymethylcellulose sodium (CMC-Na) by intragastric administration, and the normal administration group was given 0.5% CMC-Na suspension corresponding drugs: AD normal group (1.35mmol / kg), B normal group ( 1.35mmol / kg) and A normal group (1.35mmol / kg). 1 time a day, continuous administration for 15 days. Blood was collected on 3d, 7d, and 15d to measure blood sugar, and the changes in body weight, urination, drinking, and eating activities of the mice were recorded. On the 15th day, the mice were sacrificed and autopsied with naked eyes. Experimental data are presented as mean ± standard deviation said, analyzed with SPSS 11.5 statistical software, P P <0.01 means the difference is extremely significant.
[0052] 3.3 Ex...
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