Betulin derivative as well as preparation method and application thereof

A technology of betulin and derivatives, applied in the field of betulin derivatives and their preparation, can solve the problems of lack of active groups, few reaction sites, special structure and the like of the parent nucleus, and achieve the effect of wide use and good protection effect.

Active Publication Date: 2019-07-09
NANTONG UNIVERSITY +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, pentacyclic triterpenoids have a special structure, lack of active groups in the mother nucleus, and few reaction sites, so it is difficult to prepare derivatives that meet the requirements by conventional chemical reaction methods

Method used

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  • Betulin derivative as well as preparation method and application thereof
  • Betulin derivative as well as preparation method and application thereof
  • Betulin derivative as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
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Embodiment 1

[0035] Embodiment 1 structural formula is the preparation of the compound of formula I, formula II, formula III, formula IV, formula V, formula VI and formula VII

[0036] The invention adopts a microbial conversion method, uses betulin as a raw material, and undergoes steps such as fermentation, extraction, and separation to prepare the compound of the invention. Microorganisms capable of transformation include: Absidia, Cunninghamella, Mucor, Alternaria, Rhodotorula, Syncephalastrum or Rhizopus (Rhizopus) genus microorganisms; among them, strains of Mucor (Mucor) genus have stronger transforming ability. These strains can be purchased from the Chinese Academy of Sciences Microbial Culture Collection Center (CGMCC) or the China Institute of Food Fermentation Industrial Microbiology Collection Center (CICC), and stored on a solid slant medium in a refrigerator at 4 °C. Potato medium was selected as the fungal medium, and LB medium was selected as the bacterial medium.

[003...

Embodiment 2

[0069] Example 2 The protective effect of compound I, compound II, compound III, compound IV, compound V, compound VI and compound VII of the present invention on HK-2 cells induced by TGF-β1.

[0070] (1) Experimental materials

[0071] 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.

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Abstract

The invention discloses a betulin derivative as well as a preparation method and application thereof. The structural formula of the betulin derivative provided by the invention is shown as a formula I, a formula II, a formula III, a formula IV, a formula V, a formula VI or a formula VII. According to the invention, the betulin is successfully subjected to structural modification by utilizing a microbial conversion technology, so that a plurality of novel compounds are obtained. In vitro TGF-beta 1 induced HK-2 cell experiments prove that the compounds have a relatively good protection effect on HK-2 cell damage. The compounds can be used as active ingredients of a medicine for preventing or treating nephropathy and have wide application.

Description

technical field [0001] The invention relates to the field of biomedicine, in particular to a betulin derivative, a preparation method thereof and a medical application of the derivative. 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 f...

Claims

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Application Information

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IPC IPC(8): C07J63/00A61K31/56A61P13/12A61P35/00C12P33/00C12R1/785
CPCA61P13/12A61P35/00C07J63/008C12P33/00
Inventor 陈广通杨圣菊宋妍姜宝成
Owner NANTONG UNIVERSITY
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