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Tanshinone derivative and its application in preparing aldose reduction enzyme inhibitor pharmaceutical

A kind of derivative, the technology of tanshinone, which is applied in the application field of tanshinone derivatives and in the preparation of aldose reductase inhibitor drugs, can solve the problem of unreported research and application, aldose reductase inhibitors and non-enzymatic glycosylation The inhibitor effect is not ideal, etc., to achieve a significant inhibitory effect

Inactive Publication Date: 2007-08-08
GUANGDONG UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the currently developed aldose reductase inhibitors and non-enzymatic glycosylation inhibitors have unsatisfactory effects, so it is urgent to find inhibitors with high efficiency, low toxicity and small side effects
[0003] Studies have found that Danshen and its extracts have a certain activity of inhibiting the key enzyme aldose reductase in diabetic complications, but the research and application of tanshinone derivatives as aldose reductase inhibitors have not been reported yet.

Method used

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  • Tanshinone derivative and its application in preparing aldose reduction enzyme inhibitor pharmaceutical
  • Tanshinone derivative and its application in preparing aldose reduction enzyme inhibitor pharmaceutical
  • Tanshinone derivative and its application in preparing aldose reduction enzyme inhibitor pharmaceutical

Examples

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Embodiment 1

[0020] Embodiment 1: the extraction of aldose reductase

[0021] Extraction of aldose reductase: Take fresh bovine testis, remove epididymis, blood vessels and other connective tissues, rinse with normal saline and store in a -70°C refrigerator. Weigh 100 g of testicular tissue, add three times the volume of Tris-HCl buffer solution with pH 7.4 5 mmol / L, and use a tissue grinder to make a tissue homogenate. The prepared homogenate was centrifuged at 45000 g for 30 min in a refrigerated centrifuge, the supernatant was collected, ammonium sulfate was added to 50% saturation, and then centrifuged at 15000 g for 30 min. Ammonium sulfate was added to the supernatant to reach 70% saturation, and the precipitate was collected and dialyzed to determine the activity of the enzyme. All separation steps were carried out at <4°C and 5mmol / L 2-mercaptoethanol.

Embodiment 2

[0022] Example 2: Inhibition of Tanshinone Derivatives on Aldose Reductase

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Abstract

The invention discloses a tanshinone derivant and application to make aldose reductase inhibitor drug, which possesses chemical formula as formula I-IV, wherein R in the formula II and IV represents -COOH, -NO2, -CN; NR2 in the formula V and VI represents molecular formula (A).

Description

technical field [0001] The invention relates to a tanshinone derivative and its application in the preparation of an aldose reductase inhibitor drug. technical background [0002] Diabetes is a common chronic life-long disease that seriously endangers human health. Long-term high blood sugar in diabetes can cause harm to many tissues and organs in the body and lead to many complications. These complications have become the main reason for threatening the health and life of diabetic patients. The development of drugs for the treatment of diabetic complications has always been a research hotspot for scientists. According to the research on the pathogenesis of diabetic complications, aldose reductase and non-enzymatic glycosylation are the key factors in the mechanism of diabetic complications, and inhibitors of aldose reductase and non-enzymatic glycosylation can effectively prevent and treat diabetes. or relieve diabetic complications. However, the currently developed aldo...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J73/00A61K31/58A61P3/10
Inventor 杜志云张焜方岩雄古练权黄宝华赵肃清周丽华郑杰
Owner GUANGDONG UNIV OF TECH
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