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Combined product containing limonin compounds and biguanide compounds

A technology of limonoids and combined products, applied in the field of medicine, can solve problems such as toxic side effects, hypoglycemia, lactic acid accumulation, etc., achieve the effect of weight loss treatment, reduce side effects, and improve the effect of hypoglycemia

Active Publication Date: 2019-02-26
NATURAL MEDICINE INST OF ZHEJIANG YANGSHENGTANG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, oral drugs mainly include: sulfonylureas, biguanides, α-glucosidase inhibitors, thiazolidinediones, DPP-4 inhibitors, etc., but because the oral hypoglycemic drugs are prone to drug resistance, low Serious side effects of blood sugar and liver and kidney toxicity
For example, biguanide compounds have a hypoglycemic effect, but at the same time, according to the existing clinical data, for patients with renal function damage or renal defects, after taking it, it will lead to the accumulation of lactic acid, causing lactic acidosis, which has a certain risk of side effects

Method used

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  • Combined product containing limonin compounds and biguanide compounds
  • Combined product containing limonin compounds and biguanide compounds
  • Combined product containing limonin compounds and biguanide compounds

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Effects of limonoids, metformin or their combination on blood glucose in mouse islet β-cell injury model

[0032] In this embodiment, ICR mice were modeled with streptozotocin (STZ) to obtain a mouse islet beta cell injury model (refer to prior art literature: Li Nan et al., The protective effect of pine pollen on kidney damage in diabetic nephropathy mice, Science and Technology Herald, 2014, 32(4 / 5): 95-99), completed the animal hypoglycemic efficacy evaluation experiment (this model can simulate the damage state of islet β cells in type I and type II diabetes). For limonoid compounds, choose limonin, isocitrinic acid, limonin glycoside, and isocitrinic acid glycoside, and set up separate metformin administration group, limonin administration group, and isocitrolactone administration group. group, limonin glycoside administration group, isocitrolactone glycoside administration group and combined administration group compounded with metformin.

[0033] Experimental fe...

Embodiment 2

[0044] Effects of limonoids, metformin, or their combination on blood glucose and leptin in a mouse model of type II diabetes

[0045] In this embodiment, db / db mice (strain name BKS.Cg-Dock7 m+ / + Lepr db / Nju) completed the animal hypoglycemic efficacy evaluation experiment (blood sugar level and leptin). For the limonoid compounds, choose phellodendrones, isofordone glucosides, and phellodendron glucosides, and set up separate metformin administration groups, phellodendrones administration groups, isofortoides acid administration groups, phellodendron glucosides administration groups, and Metformin combined administration group.

[0046]Experimental feeding conditions: as type II diabetes model mice, 6-week-old SPF-grade db / db mice were purchased from the Nanjing Institute of Model Organisms, and the experimental feeding was carried out after 7 days of preparatory feeding. It should be noted that the feeding conditions of the mice were temperature of 23±1°C, humidity of ...

Embodiment 3

[0058] Effects of limonoids, metformin or their combination on blood glucose in mouse islet β-cell injury model

[0059] In this embodiment, ICR mice were modeled with streptozotocin (STZ) to obtain a mouse islet beta cell injury model (refer to prior art literature: Li Nan et al., The protective effect of pine pollen on kidney damage in diabetic nephropathy mice, Science and Technology Herald, 2014, 32(4 / 5): 95-99), completed the animal hypoglycemic efficacy evaluation experiment (this model can simulate the damage state of islet β cells in type I and type II diabetes). For limonoid compounds, choose Yichang Hesin, Yichang Hesin, and Yichang Hesin Glycoside, and set up separate metformin administration group, Yichang Hesin administration group, Yichang Genxin drug group and the combined administration group compounded with metformin.

[0060] Experimental feeding conditions: ICR mice (20±2g), 6 weeks old, were purchased from Zhejiang Academy of Medical Sciences, and were fed...

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Abstract

The invention relates to a combined product containing limonin compounds (and pharmaceutically acceptable derivatives, esters, stereoisomers, salts or prodrugs thereof) and biguanide compounds (e.g.,metformin, metformin hydrochloride, buformin and phenformin). The invention also relates to the application of the combined product to treatment and / or prevention of diseases associated with diabetes,lipid reduction, weight loss, etc.

Description

technical field [0001] The invention belongs to the technical field of medicine, in particular to a limonoid compound (and pharmaceutically acceptable derivatives, esters, stereoisomers, salts or prodrugs thereof) and a biguanide compound (or its pharmaceutically acceptable accepted salts). The present invention also relates to the use of the combined product in treating and / or preventing diseases related to diabetes, obesity and metabolic syndrome. Background technique [0002] According to IDF statistics, there were about 415 million people with diabetes worldwide in 2015, and 1 in every 11 people has diabetes. The number of diabetic patients in China is about 110 million, ranking first in the world. It is predicted that by 2040, there will be 642 million people with diabetes worldwide, and 151 million people with diabetes in China. Diabetes requires lifelong monitoring and treatment. If it is not well controlled, it will lead to secondary cardiovascular diseases, blind...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/585A61K31/155A61K31/7048A61P3/10A61P3/04A61P3/00
CPCA61K31/155A61K31/585A61K31/7048A61K2300/00A61K31/366A61P3/00A61P3/04A61P3/10C07J73/00
Inventor 李栋韩铨胡柳薛莲
Owner NATURAL MEDICINE INST OF ZHEJIANG YANGSHENGTANG
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