Application of betulinic acid derivatives in preparation of anti-nephropathy drug

A technology of betulinic acid and derivatives, applied in the field of medicine, can solve the problem of low anti-kidney fibrosis activity of betulinic acid, and achieve the effect of wide use and good protective effect

Active Publication Date: 2020-11-10
NANTONG UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there are few reports on the anti-renal fibrosis activity of betulinic acid

Method used

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  • Application of betulinic acid derivatives in preparation of anti-nephropathy drug
  • Application of betulinic acid derivatives in preparation of anti-nephropathy drug
  • Application of betulinic acid derivatives in preparation of anti-nephropathy drug

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] Embodiment 1, structural formula is the preparation of the compound of formula I-formula VI

[0019] The invention adopts a microbial transformation method, uses betulinic acid as a raw material, and undergoes steps such as fermentation, extraction, and separation to prepare the compound of the invention. Circinella genus strains can be purchased from the Chinese Academy of Sciences Microbial Culture Collection Center (CGMCC), using potato medium, and stored on a solid slant medium in a refrigerator at 4°C.

[0020] Taking Circinella muscae CGMCC 3.2695 as an example, the process of preparing the compound whose structural formula is formula I-formula VI is as follows:

[0021] 1) Fermentation, transformation and extraction

[0022] Put Circinella muscae CGMCC 3.2695 into two 250mL Erlenmeyer flasks (containing 100mL potato culture medium) as seed solution. After shaking and culturing on a shaker at 160 rpm and 26°C for 1 day, when the mycelium growth is in a vigorous ...

Embodiment 2

[0029] Example 2 The protective effect of compound I, compound II, compound III, compound IV, compound V and compound VI of the present invention on HK-2 cells induced by TGF-β1.

[0030] 1) Experimental materials

[0031] CO 2 Incubator (Jouan IGO150); microplate reader (Bio-TEK ELx800); fluorescent inverted microscope (OlympusIX51); flow cytometer (Thermo), RPM I 1640 medium (Gibcol BRL), RNase A, fetal bovine serum, di Methyl sulfoxide (DMSO), trypsin (Shanghai Bioengineering Co., Ltd.), TGF-β1, HK-2 cells.

[0032] Test samples: Compounds I-VI synthesized in Example 1, with a purity of over 95%, each compound was dissolved in DMSO and then diluted.

[0033] 2) Experimental method

[0034] The cell apoptosis rate was determined by flow cytometry (three independent experiments, mean±SD): HK-2 cells in the logarithmic growth phase were taken, and the cell concentration was adjusted to 5 with RPM I 1640 culture medium containing 10% calf serum. ×10 5 / mL, inoculated in 96...

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PUM

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Abstract

The invention belongs to the field of medicines, and discloses betulinic acid derivatives or pharmaceutically acceptable salts thereof, and application of the betulinic acid derivatives or pharmaceutically acceptable salts in preparation of the anti-nephropathy drug The betulinic acid is successfully subjected to structural modification by utilizing a microbial conversion technology, a plurality of novel betulinic acid derivatives are obtained, and in-vitro TGF-[beta]1 induced HK-2 cell tests prove that the compounds have a better effect of protecting HK-2 cells from being damaged. The betulinic acid derivatives can be used as active ingredients of the drug for preventing or treating nephropathy, and have wide application.

Description

technical field [0001] The invention relates to the field of medicine, in particular to the application of betulinic acid derivatives in the preparation of anti-nephropathy drugs. Background technique [0002] Renal fibrosis is a common pathological manifestation of chronic kidney disease of various causes in the later stage, and it is the main cause of CKD. The pathological features of renal fibrosis are mainly manifested as massive accumulation of interstitial extracellular matrix including collagen fibers and fibronectin, accompanied by inflammatory cell infiltration, apoptosis and loss of renal tubular epithelial cells, proliferation of fibroblasts and myofibroblasts, Peritubular vascular rarefaction changes, eventually leading to glomerulosclerosis, tubulointerstitial fibrosis, and loss of renal function. In this pathophysiological process, renal cell apoptosis plays a very important role. Abnormal apoptosis mainly includes decreased apoptosis of interstitial fibrobla...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/56A61P13/12
CPCA61K31/56A61P13/12
Inventor 陈广通储呈娇张永珍陈婷婷宋妍
Owner NANTONG UNIVERSITY
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