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Application of geniposide in alleviating side effects of glucocorticoid

A technology of glucocorticoids and side effects, which is applied in the application field of geniposide in alleviating the side effects of glucocorticoids, and can solve problems such as frequent administration, limited applicable population, and high treatment cost

Inactive Publication Date: 2019-07-26
GUANGDONG MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the above drugs do have certain curative effects in the treatment of GIOP, there are still problems such as limited applicable population, frequent administration, drug resistance, high treatment cost, and many side effects.

Method used

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  • Application of geniposide in alleviating side effects of glucocorticoid
  • Application of geniposide in alleviating side effects of glucocorticoid
  • Application of geniposide in alleviating side effects of glucocorticoid

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] Example 1 MC3T3-E1 cell proliferation experiment

[0045] 1.1 Drugs and reagents

[0046] MC3T3-E1 cell line (Cell Bank, Chinese Academy of Sciences), α-MEM medium (without Vc) (GIBCO, USA), Fetal bovine serum (FBS), dexamethasone (Dex) (Sigma, USA) ), ascorbic acid (vitamin C, Vc) (US Sigma), β-sodium glycerophosphate (US Sigma) NBT / BCIP mixed reagent (US Sigma), alizarin red, CCK-8 (Cell Counting Kit-8) (Japanese colleagues ), alkaline phosphatase activity detection kit (Beiyuntian Biotechnology Co., Ltd.), BCA protein concentration assay kit (Beiyuntian Biotechnology Co., Ltd.), absolute ethanol, geniposide (Chengdu Best Reagent Co., Ltd.).

[0047] 1.2 MC3T3-E1 cell culture

[0048] Use α-MEM medium (without Vc) containing 10% fetal bovine serum to culture MC3T3-E1 cells in a 5% CO2 incubator at 37°C, change the medium every 3 days, and when the cells grow to about 90% of the bottom of the bottle , digested with 0.25% trypsin, centrifuged, collected cells, and ca...

Embodiment 2

[0052] Example 2 Cell alkaline phosphatase staining and activity detection

[0053] Alkaline phosphatase (ALP) is a marker glycoprotein in the early differentiation of osteoblasts, and its activity is closely related to the activity of osteogenic differentiation. The early stages of osteogenic differentiation and functional maturation can be used as one of the indicators to evaluate bone formation and bone turnover. However, under the action of superphysiological glucocorticoids, the activity of alkaline phosphatase in the process of osteogenic differentiation in vitro will be inhibited and affect the osteogenic differentiation of cells. In this experiment, alkaline phosphatase staining and quantitative detection of alkaline phosphatase activity were used to study the effect of geniposide on the inhibition of alkaline phosphatase activity in MC3T3-E1 cells induced by dexamethasone.

[0054] Cell digestion and inoculation: Take well-grown MC3T3-E1, digest and count, and use 2×...

Embodiment 3

[0057] Example 3 Mineralized nodule staining and quantitative detection

[0058] Mineralized nodules appear in the late stage of osteogenic differentiation, and are formed when hydroxyapatite crystals and amorphous calcium phosphate produced during osteoblast differentiation are secreted into the extracellular matrix and combined with osteocalcin, osteopontin, collagen, etc. Hydroxyapatite crystallization is one of the indicators of late osteogenic differentiation. Therefore, in this experiment, Alizarin red staining and calcium nodule quantification were used to study the effect of geniposide on the inhibition of MC3T3-E1 cell mineralization by dexamethasone.

[0059] Cell digestion and inoculation: take well-grown MC3T3-E1 cells, digest and count them, and use 5×10 4 Cells / well were inoculated in 24-well plates, grouped as in Example 2, transferred to a carbon dioxide incubator for culture, and after 14 days of drug treatment, the mineralization of cells was observed by ali...

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Abstract

The invention belongs to the field of synthetic drugs, and relates to an application of geniposide in alleviating side effects of glucocorticoid, and an application of compounds represented by the formula I or pharmaceutically acceptable salts, esters, or prodrugs in preparation of drugs for alleviating side effects of glucocorticoid. The molecular action mechanism of the compounds in alleviatingthe side effects of glucocorticoid drugs has important clinical significance for developing new drugs.

Description

technical field [0001] The invention relates to the application of a natural compound 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 for the treatment of rheumatoid arthritis in 1949, glucocorticoids have been known for their excellent anti-inflammatory activity and Immunosuppression is widely used clinically in inflammation, autoimmune diseases and organ transplantation. It has been reported that about 1% of the population in the United States is receiving long-term treatment with glucocorticoids, and the proportion of oral glucocorticoids in the community is between 0.5% and 0.9% (65% of whom are women). The proportion is as high as 2.7% in women aged ≥50 years; in the female osteoporosis study covering 10 countries, about 4.6% of the 60,393 postmenopausal women who were followed up daily were receiving gluco...

Claims

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Application Information

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IPC IPC(8): A61K31/7048A61K31/573A61P19/02A61P29/00A61P37/06A61P3/04A61P25/24A61P25/00A61P3/06A61P3/10A61P9/00A61P19/10A61P19/08A61P1/00A61P7/04A61P27/12A61P21/00A61P5/00
CPCA61K31/573A61K31/7048A61P1/00A61P3/04A61P3/06A61P3/10A61P5/00A61P7/04A61P9/00A61P19/02A61P19/08A61P19/10A61P21/00A61P25/00A61P25/24A61P27/12A61P29/00A61P37/06A61K2300/00
Inventor 徐道华周晨慧谢保城吴佳欢
Owner GUANGDONG MEDICAL UNIV
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