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Application of 22 (R)-hydroxycholesterol as PARP1 inhibitor

A technology of hydroxycholesterol and inhibitor, applied in the field of medicine

Active Publication Date: 2016-01-13
XIEHE HOSPITAL ATTACHED TO TONGJI MEDICAL COLLEGE HUAZHONG SCI & TECH UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Existing studies believe that elevated cholesterol is clearly related to the incidence of tumors, but there is no evidence for cholesterol-related drugs in this regard

Method used

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  • Application of 22 (R)-hydroxycholesterol as PARP1 inhibitor
  • Application of 22 (R)-hydroxycholesterol as PARP1 inhibitor
  • Application of 22 (R)-hydroxycholesterol as PARP1 inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Example 1 Detection by Cell-Free PARP1 Enzymatic Reaction System

[0027] The PARP1 activity detection kit was used to construct a cell-free PARP1 enzymatic reaction system, which can activate the activity of PARP1 enzyme in vitro.

[0028] The PARP1 activity detection kit used in the examples was purchased from Trevigen, produced in the United States, with a model number of 4676-096-K.

[0029] PARP1 activity detection kit includes buffer, PARP1 recombinant protein, NAD + , single-strand break DNA, recombinant histone 1 (HistoneH1).

[0030] Configure the cell-free PARP1 enzymatic reaction system according to the PARP1 activity detection kit, the specific operation steps are as follows: add 50ng PARP1 recombinant protein (PARP1protein) to the buffer solution, the final concentration is 10mmol / LNAD + , The final concentration is 20mg / mL after single-strand break DNA. The final concentrations of the various components that make up the buffer solution in the reaction s...

Embodiment 2

[0037] Embodiment 2 Utilizes in vitro cell experiment detection

[0038] In the in vitro cell experiment, HepG2 (derived from American Type Culture Collection) cells were selected as experimental cells. The inventors treated HepG2 cells with different concentrations of 22(R)-hydroxycholesterol (abbreviated as 22(R)-HC). For treatment methods, see HuangD, YangC, WangY, LiaoY, & HuangK. PARP-1 suppresses adiponectin expression through poly(ADP-ribosyl)ation of PPARgammaincardiacfibroblasts. Cardiovascularresearch, 2009, 81(1): 98-107.

[0039] HepG2 cells were stimulated with 22(R)-hydroxycholesterol (i, 0.5 μmol / L, 1 μmol / L, 3 μmol / L) or nicotinic acid (iv, 1 μmol / L, 5 μmol / L, 10 μmol / L) for 24 hours. The concentrations in brackets are the final concentrations.

[0040] PARP1 activity was detected using a PARP1 activity detection kit (purchased from Trevigen, produced in the United States, model number 4676-096-K). For specific methods, refer to the instructions of the kit. ...

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Abstract

The invention relates to an application of 22 (R)-hydroxycholesterol as 1-type poly (ADP-ribose) synthetase inhibitor. 22 (R)-hydroxycholesterol as a cholesterol analogue does not have the cytotoxic effects of common anti-tumor drugs or other 1-type poly (ADP-ribose) synthetase inhibitors, and the safety of the 22 (R)-hydroxycholesterol can be predicated. The 22 (R)-hydroxycholesterol can be widely applied as the medicine for treating cholesterol related diseases, including cardiovascular diseases, tumour and the like.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to the application of 22(R)-hydroxycholesterol as a PARP1 inhibitor. Background technique [0002] 22(R)-hydroxycholesterol, CAS number is 17954-98-2, English name is 22(R)-HYDROXYCHOLESTEROL, abbreviated as 22(R)-HC; molecular formula is C 27 h 46 o 2 , the molecular weight is 402.65. [0003] 22(R)-Hydroxycholesterol is a hydroxylated cholesterol analogue, which has the effect of lowering cholesterol. In the current research, it is mainly used as an agonist of the liver X receptor (LXR), that is, to activate LXR, such as activating the gene LXRα (liver X receptor α subtype), so the above drugs are widely used in LXR-related research middle. [0004] Poly ADP-ribose synthase type 1, abbreviated as PARP1, is a ribozyme widely expressed in eukaryotic cells. When intracellular oxidative stress causes DNA breakage damage, PARP1 is activated by binding to the broken DNA to unde...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/575A61P9/00A61P35/00
Inventor 黄恺张冯筱黄丹
Owner XIEHE HOSPITAL ATTACHED TO TONGJI MEDICAL COLLEGE HUAZHONG SCI & TECH UNIV
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