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6-hydroxymethylpyridin-3-ol capable of promoting wound healing and its application

A technology of hydroxymethylpyridine and methanol, applied in the field of chemical drugs, can solve problems such as lack of research, and achieve the effect of promoting HUVEC cell migration

Active Publication Date: 2022-04-15
SICHUAN GOODDOCTOR PANXI PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0003] The American cockroach (Periplaneta americana) is an insect belonging to the genus Periplaneta of the family Insecta Pterosae, Blatella order, Blattedae, and the Kangfuxin liquid prepared from it has positive clinical effects in treating various wounds including ulcers, which shows that it is expected to find a wound-healing agent. Active ingredients or drugs, but research in this area is still relatively lacking

Method used

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  • 6-hydroxymethylpyridin-3-ol capable of promoting wound healing and its application
  • 6-hydroxymethylpyridin-3-ol capable of promoting wound healing and its application
  • 6-hydroxymethylpyridin-3-ol capable of promoting wound healing and its application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Example 1 Extraction, separation and structural identification of 6-hydroxymethylpyridin-3-ol of the present invention

[0021] Periplaneta americana comes from the Periplaneta americana GAP base of Sichuan Good Doctor Panxi Pharmaceutical Co., Ltd. The extract of Periplaneta americana is the main component of Kangfuxin liquid.

[0022] Take 25kg of dried worm bodies of Periplaneta americana, crush them, extract with hot water under reflux (3×2h), and concentrate the extract under reduced pressure to obtain the total extract (about 2kg). The total extract was eluted by reverse phase chromatography MCI gel CHP 20P column (methanol-water, 0%-100%) gradient to obtain 11 fractions (F1-F11). F10 (10g) was subjected to Sephadex LH-20 gel (methanol-water, 80%) and RP-18 chromatographic column (methanol-water, 10%~25% gradient elution) to obtain 8 fractions (F10.1~F10 .8). F10.4 (1.5g) obtained compound 6-hydroxymethylpyridin-3-ol (13.5mg, t R =12.3) The compound results ar...

Embodiment 2

[0024] Example 2 6-Hydroxymethylpyridin-3-ol (mdl-30a) of the present invention promotes HUVEC cell migration activity test

[0025] Human umbilical vein endothelial cells (HUVECs) were obtained from Shenzhen University Medical Center and donated by Professor Liu Baohua's research group. M199 medium and fetal bovine serum were purchased from Gibco. HUVECs cells in logarithmic phase were collected and seeded in 24-well culture plates, 14×10 per well 4 cells. Placed at 37°C, 5% CO 2 After the cells were cultured for 24 hours under certain conditions, they were washed three times with 1×PBS, and then starved for 6 hours with M199 medium containing 0.5% FBS. After starvation, scratch with a P10 pipette tip, add M199 medium dissolved with different drugs (final concentration 20 μM) to the experimental group, add fresh M199 medium to the blank group, and take pictures. At 37°C, 5% CO 2 After incubating under the condition for 6h, wash 3 times with 1×PBS, add fresh M199 medium, ...

Embodiment 3

[0028] Embodiment 3 The effect of compound described in the present invention on guinea pig oral ulcer

[0029] 1 Experimental materials

[0030] 1.1 Pharmaceutical reagents

[0031] Test drug: 6-hydroxymethylpyridin-3-ol, referred to as 6OP3O, CAS: 40222-77-3; Guilin Watermelon Cream, Guilin Sanjin Pharmaceutical Co., Ltd., batch number: Z45021599; normal saline, Henan Kelun Pharmaceutical Industry Co., Ltd., batch number C217030105-2; formaldehyde solution, Yantai Shuangshuang Chemical Co., Ltd., batch number 20170201; phenol, Tianjin Zhiyuan Chemical Reagent Co., Ltd., batch number: 20140402; guinea pig tumor necrosis factor α (TNF-α) ELISA detection reagent Box, Suzhou Calvin Biotechnology Co., Ltd., batch number: CK-E30635.

[0032] 1.2 Experimental animals

[0033] Ordinary guinea pigs, weighing 270-300 g, male and female, were provided by Jinan Jinfeng Experimental Animal Co., Ltd., certificate number: 37009700000360; laboratory license number: SYXK (Yu) 2015-0005. ...

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Abstract

The invention discloses a compound with the effect of promoting wound healing. The compound 6-hydroxymethylpyridin-3-ol is isolated from Periplaneta americana for the first time; the invention also discloses the preparation method of the compound and the The compound is a composition of active ingredients, and the composition contains 6-hydroxymethylpyridin-3-ol or its pharmaceutically acceptable derivatives and salts thereof. The compound is used in the preparation of medicines for promoting wound healing, especially the application of medicines for promoting ulcer healing. The compound promotes the healing of wounds by regulating the mechanism of cell migration activity, and it is found through pharmacological experiments that it can improve oral ulcers. effect, can improve its healing rate.

Description

technical field [0001] The invention belongs to the field of chemical medicines, and relates to 6-hydroxymethylpyridin-3-ol and its application in wound healing including ulcer treatment. Background technique [0002] The causes, hazards and treatment of wounds including ulcers have been mentioned in the previous patent application CN105434450A. The tissue reconstruction process of trauma at least includes cell proliferation, migration and angiogenesis. At present, HUVEC (human umbilical vein endothelial cells) has become an important model for the study of promoting wound healing. The active compounds discovered by this method in the present invention have not been reported. [0003] The American cockroach (Periplaneta americana) is an insect belonging to the genus Periplaneta of the family Insecta Pterosae, Blatella order, Blattedae, and the Kangfuxin liquid prepared from it has positive clinical effects in treating various wounds including ulcers, which shows that it is ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/44A61P17/02A61P1/04C07D213/65
CPCA61P1/04A61P17/02A61K31/44C07D213/65
Inventor 程永现刘越飞向斌王心龙
Owner SICHUAN GOODDOCTOR PANXI PHARMA
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