Novel uses of bisbenzylisoquinoline alkaloid derivative or analogue of general formula I

A technology of bisbenzylisoquinoline and alkaloid derivatives, which is applied in the field of medicine to achieve good inhibitory effect, reduce the thickening of the basement membrane, and restore the effect of the charge barrier

Inactive Publication Date: 2012-09-12
李宏
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] At present, there are no reports that the bisbenzylisoquinoline alkaloid derivatives shown in general formula I and compounds such as liensinine, isoliensinine and methylliensinine are used for the treatment of diabetic nephropathy

Method used

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  • Novel uses of bisbenzylisoquinoline alkaloid derivative or analogue of general formula I
  • Novel uses of bisbenzylisoquinoline alkaloid derivative or analogue of general formula I
  • Novel uses of bisbenzylisoquinoline alkaloid derivative or analogue of general formula I

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Example 1 Clinical experiment of bisbenzylisoquinoline alkaloid derivatives of the present invention

[0033] 1.1 Test drug

[0034] Liensinine, isoliensinine, and neferine were separately packed into capsules, and placebo capsules (containing the same amount of starch) were made at the same time. The appearance and color of the capsules were consistent with those of Kaibotong capsules.

[0035] 1.2 Subject

[0036] A total of 100 patients with diabetic nephropathy (stage III or IV) entered the study and were randomly assigned to the liensinine group 30mg / Tid, isoliensinine group 30mg / Tid, neferine group 30mg / Tid, Kaibotong capsule group, and Placebo group / Tid. There was no significant difference in gender, age, course of disease and clinical symptoms in each group before entry (P>0.05), and they were comparable.

[0037] The patients in each group met the following conditions: (1) In line with diabetic nephropathy, according to Mogensen diabetic nephropathy stage III or IV, ur...

Embodiment 2

[0046] Example 2 Pharmacodynamic study of bisbenzylisoquinoline alkaloid derivatives of the present invention

[0047] 1Materials and methods

[0048] 1.1 Experimental materials

[0049] 1.1.1 Animals

[0050] Clean-grade healthy male Sprague-Dawley (SD) rats, weighing 180-200 g, were purchased from West China Experimental Animal Center of Sichuan University. In the environment of room temperature (22±1)℃, relative humidity (55±5)%, and photoperiod of 12h to 12h, they were adapted to rearing for 1wk and tested.

[0051] 1.1.2 Drugs

[0052] Liensinine, isoliensinine, neferine. Use normal saline to prepare gavage; Kaibotong (kaibotong) tablets, produced by Shanghai Zhongmei Squibb Pharmaceutical Co., Ltd., batch number: 1006041.

[0053] 1.1.3 Main reagents

[0054] Streptozotocin (STZ), Sigma company, dissolved in 0.01mol / L citrate buffer, pH 4.5 before use; rabbit anti-rat nephrin, podocin and HPSE polyclonal antibodies, Wuhan Boster; Biotin-labeled goat anti-rabbit IgG, horseradish pe...

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PUM

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Abstract

The invention provides a use of a bisbenzylisoquinoline alkaloid derivative or analogue to prepare medicine medicines for treating diabetic nephropathy. The bisbenzylisoquinoline alkaloid derivative of general formula I provided by the invention by relieving glomerular basement membrane thickening, reduces foot process fusion of glomerular epithelial cells and restores mechanical barrier and charge barrier of glomerulus, thus reducing protein leakage, having a good therapeutic effect on diabetic nephropathy (stage III or stage IV) patients, reducing 24h micro-albumin (UAE) and 24h urine protein (UPQ), having a good inhibitory effect on the albuminuria symptom of the diabetic nephropathy, and providing a new choice for the clinical treatment of the diabetic nephropathy.

Description

Technical field [0001] The invention relates to the use of bisbenzylisoquinoline alkaloid derivatives or analogues in the preparation of drugs for treating diabetic nephropathy, and belongs to the field of medicine. Background technique [0002] Diabetic nephropathy is one of the most serious complications of diabetes and the main reason for end-stage renal disease. With the development of economy and the change of lifestyle, the incidence of diabetes has gradually increased, and there is currently no better treatment method. Other pathological changes of diabetic nephropathy include thickening of the glomerular basement membrane, fusion of glomerular epithelial cell foot processes, and enlargement of the glomeruli due to an increase in extracellular mesangial matrix. In the late stage of the disease, renal tubular atrophy may appear and intrarenal fibrosis may occur. Approximately 50% of patients with diabetes with a course of more than 10 years have diabetic nephropathy. At ...

Claims

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Application Information

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IPC IPC(8): A61K31/4725A61P13/12A23L1/29A23L1/30A23L33/00
Inventor 马松涛李宏李丰
Owner 李宏
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