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Application of allantoin in relieving side effects of glucocorticoid

A technology of glucocorticoids and side effects, applied in the field of compound drugs, can solve the problems of no research reports and achieve the effect of alleviating side effects and glucocorticoid-induced osteoporosis

Pending Publication Date: 2021-06-04
DONGGUAN PEOPLES HOSPITAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Studies have reported the antiallergic use of allantoin preparations in the preparation of antiallergic drugs and the use in the preparation of free radical scavenging drugs. The principle is that allantoin can be used as a free radical scavenger, but whether allantoin has Prevention and treatment of glucocorticoid-induced side effects, especially glucocorticoid-induced osteoporosis and its mechanism of action, no relevant research reports have been found so far

Method used

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  • Application of allantoin in relieving side effects of glucocorticoid
  • Application of allantoin in relieving side effects of glucocorticoid
  • Application of allantoin in relieving side effects of glucocorticoid

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0057] Example 1 MC3T3-E1 cell culture

[0058] After MC3T3-E1 cells were recovered from the liquid nitrogen tank, they were incubated in α-MEM medium (without Vc) containing 10% fetal bovine serum at 37°C, 5% CO 2 The MC3T3-E1 cells were continuously cultured in the incubator, and the medium was changed every 3 days. When the cells grew to cover about 90% of the bottom of the bottle, they were digested with 0.25% trypsin, centrifuged at 900rpm for 2min, and the cells were collected for the following procedures: experiment.

Embodiment 2

[0059] Example 2 The effect of allantoin on the activity of MC3T3-E1 cells detected by CCK-8 method

[0060] After the digested cells were prepared into a uniform single-cell suspension with α-MEM complete medium, the cell count was adjusted to a cell density of 3×10 3 cells / well; each well was inoculated with 100 μl of cell suspension in a 96-well plate, and cultured in a carbon dioxide incubator. After 24 hours of cell attachment, the cells were grouped as follows: ① 0 μM allantoin (Control group), ② 1 μM allantoin group, ③ 5 μM allantoin group, ④ 10 μM allantoin group, ⑤ 20 μM allantoin group, ⑥ 40 μM allantoin group group, ⑦60μM allantoin group, ⑧80μM allantoin group, ⑨100μM allantoin group. At 48h and 72h after administration, the cell proliferation was detected with a CCK-8 detection kit. Add 100 μl of CCK-8 working solution, put it into the incubator and continue to incubate for 2 hours. After the incubation time is reached, take out the 96-well cell culture plate, me...

Embodiment 3

[0062] Example 3 Alkaline phosphatase staining and activity detection The effect of allantoin on the ALP activity of MC3T3-E1 cells

[0063] Alkaline phosphatase (ALP) is a marker glycoprotein in the early differentiation of osteoblasts, and the activity of ALP is closely related to the osteogenic differentiation of cells. In the early stages of osteogenic differentiation and functional maturity, the activity of ALP can be used as one of the indicators to evaluate bone formation and bone turnover. However, under the action of super-physiological amounts of glucocorticoids, the activity of alkaline phosphatase in the process of osteogenic differentiation in vitro will be significantly inhibited and affect the osteogenic differentiation ability of cells. In this experiment, alkaline phosphatase staining and quantitative detection of alkaline phosphatase activity were used to explore whether allantoin could promote the activity of alkaline phosphatase in MC3T3-E1 cells.

[0064]...

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PUM

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Abstract

The invention relates to application of allantoin or pharmaceutically acceptable salts, esters or prodrugs thereof in relieving side effects of glucocorticoid. A compound shown in the formula I or pharmaceutically acceptable salts, esters or prodrugs thereof can be used for preparing drugs for relieving side effects of glucocorticoid. The compound disclosed by the invention can relieve side effects of glucocorticoid drugs, can remarkably relieve osteogenic differentiation inhibition caused by glucocorticoid, promotes osteogenic differentiation of cells induced by glucocorticoid, and has important clinical significance for developing new drugs.

Description

technical field [0001] The invention relates to the field of compound drugs, in particular to the application of allantoin in alleviating the side effects of glucocorticoids. Background technique [0002] Since P.Hench, E.Kendal and T.Reichstein first reported the use of glucocorticoids in the journal Annals of the rheumatic diseases in 1949 to treat rheumatoid arthritis, glucocorticoids have been known for their excellent anti-inflammatory activity and immune Inhibitory effect, widely used in clinical treatment of inflammation, autoimmune diseases and organ transplantation. Common clinical glucocorticoid drugs include prednisone, methylprednisone, betamethasone, beclomethasone dipropionate, prednisolone, hydrocortisone, dexamethasone, etc. Glucocorticoid drugs have various pharmacological effects such as anti-inflammatory, anti-toxic, anti-allergic, anti-shock, non-specific immune suppression and antipyretic effects, and can prevent and prevent the occurrence of immune inf...

Claims

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Application Information

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IPC IPC(8): A61K31/4166A61P43/00A61P3/04A61P5/04A61P5/00A61P25/24A61P25/28A61P3/06A61P3/10A61P9/00A61P21/00A61P19/10A61P19/08A61P1/00A61P7/04A61P27/12
CPCA61K31/4166A61P43/00A61P3/04A61P5/04A61P5/00A61P25/24A61P25/28A61P3/06A61P3/10A61P9/00A61P21/00A61P19/10A61P19/08A61P1/00A61P7/04A61P27/12
Inventor 谢保城陈世春何瑞荣丁少波
Owner DONGGUAN PEOPLES HOSPITAL
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