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Application of steroidal compounds in the preparation of anti-inflammatory drugs

An anti-inflammatory drug and compound technology, applied in the field of traditional Chinese medicine pharmacy, can solve problems such as side effects, and achieve the effects of small side effects, significant anti-inflammatory efficacy, and strong anti-inflammatory activity

Inactive Publication Date: 2019-04-26
JIANGXI HERBFINE HI TECH +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, today's anti-inflammatory drugs such as non-steroidal anti-inflammatory drugs aspirin and hormones have significant side effects

Method used

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  • Application of steroidal compounds in the preparation of anti-inflammatory drugs
  • Application of steroidal compounds in the preparation of anti-inflammatory drugs
  • Application of steroidal compounds in the preparation of anti-inflammatory drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Embodiment 1. Preparation of steroidal compounds:

[0029] according to figure 1 The flow chart shown is to extract steroids from Auspicious Grass, and the specific steps are as follows:

[0030] Take 20kg of the whole herb of Auspicious Grass, heat and reflux extraction with 80% ethanol for 3 times, the time of the 3 times of reflux extraction is 2h, 2h and 1h respectively, combine the three extracts, filter and concentrate under reduced pressure until there is no alcohol smell , to obtain 15L concentrated solution, the gained concentrated solution was extracted several times with sherwood oil, ethyl acetate, and water-saturated n-butanol successively, and the extracted extract was reclaimed each time, and each extract was concentrated under reduced pressure and dried. Obtain 28g of petroleum ether part extractum, 305g of ethyl acetate part extractum and 780g of n-butanol part extractum respectively;

[0031] Get 305g ethyl acetate part extract and carry out silica ...

Embodiment 2

[0033] Example 2. The test of anti-inflammatory activity in vitro by MTT method:

[0034] 1. Experimental principle: LPS (lipopolysaccharide) activated macrophage model is widely used to evaluate the anti-inflammatory effects of various chemical substances. When RAW264.7 cells (derived from mouse macrophage cell line) are stimulated by LPS, they release a large number of inflammatory factors (NO, PGE2, TNF-α, IL-6, etc.), if the drug can inhibit inflammatory mediators or inhibit the production of inflammation The enzymatic activity of factors (COX-2, iNOS, etc.) has anti-inflammatory effects. As an important messenger molecule in inflammatory response, NO is not only an effector of inflammatory response and immune regulation, but also a key regulator. It is catalyzed by nitric oxide synthase (iNOS), participates in various inflammatory signal transduction, and interacts with many The interaction between various inflammatory factors is produced in each stage of the inflammator...

Embodiment 3

[0051] Example 3. In vivo anti-inflammatory effects of compound 1 and compound 2 on inflammatory mice:

[0052] (1) Experimental instruments and materials:

[0053] Microplate reader (Thermo company), 7140 limb swelling measuring instrument (Italy UGO company), xylene and carboxymethylcellulose sodium (CMC-Na) were purchased from Sinopharm Reagent Company, all of which were of analytical grade, positive dexamethasone (5mg / piece) loosely purchased from Shandong Qilu Pharmaceutical. TNF-α and IL-1β ELISA kits were purchased from Beyont Biotechnology Co., Ltd., SPF mice were purchased from Beijing Weitong Lihua Experimental Animal Technology Co., Ltd., and mouse processed feed was purchased from Beijing Keao Xieli Feed Co., Ltd.

[0054] (2) Experimental method:

[0055] In order to further verify the anti-inflammatory effects of compound 1 and compound 2, SPF mice were used as experimental objects to construct a mouse ear swelling model, and then the ear swelling degree of c...

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Abstract

The invention relates to the field of traditional Chinese medicine pharmacy, in particular to an application of steroidal compounds in the preparation of anti-inflammatory drugs. The invention adoptsmodern pharmacological screening technology and adopts an activity-oriented separation method to separate two steroidal compounds (compound 1 and compound 2) from the ethyl acetate and n-butanol fractions of the ethanol extracts of reineckia carnea (andr.) kunth. In vitro anti-inflammatory activity tests have showed that both compound 1 and compound 2 have relatively strong anti-inflammatory activity, and the inhibition rates of compound 1 and compound 2 on NO are 35.6% and 19.4% respectively under the condition that the concentration is 0.1 umo / L. At the same time, in vivo anti-inflammatory experiments on inflammatory mice have showed that compound 1 and compound 2 have significant anti-inflammatory effects on ear swelling inflammation induced by xylene in mice, so the two compounds can be used to prepare anti-inflammatory drugs with high efficiency and low side effects.

Description

technical field [0001] The invention relates to the field of traditional Chinese medicine pharmacy, in particular to the use of steroidal compounds in the preparation of anti-inflammatory drugs. Background technique [0002] Inflammation is the body's defensive response to local damage caused by various inflammatory factors. It is a very common and very important basic pathological process that can occur in any part of the body and any tissue. Most diseases are related to the inflammatory process. In addition to common inflammatory diseases such as encephalitis, rheumatism, dysentery, and traumatic infection, inflammation is also closely related to the occurrence of tumors, coronary heart disease, and senile dementia, which have a higher incidence and greater harm. Therefore, effectively controlling the occurrence of inflammation is of great significance for the prevention and treatment of various clinical diseases. However, current anti-inflammatory drugs such as non-stero...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/58A61K31/57A61P29/00C07J17/00C07J7/00
CPCA61K31/58A61K31/57A61P29/00C07J7/002C07J17/005
Inventor 冯育林温泉欧阳辉谭婷杨世林徐旭
Owner JIANGXI HERBFINE HI TECH
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