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Compound with anti-inflammatory effect, and applications of compound in preparation of anti-inflammatory drugs

A compound and drug technology, applied in the field of medicine, can solve the problems of low absorption, great difference in efficacy, low bioavailability, etc., and achieve the effect of reducing content and significant anti-inflammatory activity

Pending Publication Date: 2019-02-01
ZHUZHOU QIANJIN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, further studies have found that andrographolide has poor water solubility, multiple unstable chemical sites, less absorption and low bioavailability in the body, which greatly limits its application.
Moreover, the composition of diterpene lactones in Andrographis paniculata is complex, about 40 kinds have been found so far, and the subtle differences in the structure of different compounds will also make their efficacy vary greatly
[0005] At present, the active mechanism of diterpene lactones in Andrographis paniculata has not yet had definite research results. At the same time, there is an urgent need in this field for new anti-inflammatory compounds derived from plants, which increase anti-inflammatory activity and chemical stability, so as to efficiently inhibit cellular inflammatory factors The expression and content of NO, TNF-α, IL-1β, IL-6 can be effectively used in the treatment of inflammation or inflammation-related diseases

Method used

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  • Compound with anti-inflammatory effect, and applications of compound in preparation of anti-inflammatory drugs
  • Compound with anti-inflammatory effect, and applications of compound in preparation of anti-inflammatory drugs
  • Compound with anti-inflammatory effect, and applications of compound in preparation of anti-inflammatory drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] The preparation of embodiment 1 anti-inflammatory compound

[0038] The present embodiment provides a kind of preparation method of the compound shown in formula (I), comprises the following steps:

[0039] S1. According to the method under the Fuke Qianjin Capsule in the Pharmacopoeia of the People's Republic of China [1] Extract from Zhuzhou Qianjin Pharmaceutical Co., Ltd. and prepare 1.5kg of Fuke Qianjin Prescription Extract Dry Cream (FKQJ). This dry paste was extracted 8 times with 3 times the volume of EtOAc to obtain an EtOAc extract (FKQJE, 156g);

[0040] S2. Take the EtOAc extract (FKQJE, 142.2g) and mix the sample with silica gel, then go through silica gel (1kg, 200-300 mesh) column chromatography, cyclohexane-EtOAc (9:1, 8:2, 7:3, 6:4 , 5:5, v / v) gradient elution, TLC detection and merging of similar fractions, a total of 10 fractions were obtained, respectively named: Fr.1, Fr.2, Fr.3, Fr.4, Fr. 5. Fr.6, Fr.7, Fr.8, Fr.9, Fr.10, spare;

[0041] S3. t...

experiment example 2

[0049] Influence of Experimental Example 2 on Inflammatory Cytokines in Vitro

[0050] Effects of the compounds of the present invention on LPS-induced oxidative stress and inflammation in RAW 264.7 macrophages. (for the convenience of recording in the experimental process, the compound label shown in the formula (I) of the present invention is as follows: drug Fr.5-1, that is, the drug Fr.5-1 described in the present invention refers to the formula of the present invention ( I) shown compound.)

[0051] 1. Materials and methods

[0052] (1) Drugs and instruments

[0053] Mouse mononuclear macrophage RAW 264.7 cell line (3111C0001CCC000146) was purchased from the Basic Medical Cell Center, Institute of Basic Medical Sciences, Chinese Academy of Medical Sciences.

[0054] DMEM medium (Dulbecco's modified Eagle medium) and fetal bovine serum (fetal bovine serum, FBS) were purchased from Gibco, USA.

[0055] 96-well plates were purchased from Corning Costar (Cambridge, MA, US...

experiment example 3

[0103] Effect of Experimental Example 3 on Rabbit Endotoxic Shock Model (Inhibitory Effect of Drug Fr.5-1 on Inflammatory Cytokines in Vivo)

[0104] Since the endotoxic shock model is a representative model of systemic inflammatory response syndrome (SIRS), septic shock, multiple organ dysfunction syndrome, and sepsis, inflammatory cytokines play an important role in the occurrence and development of the above diseases and this model is the most representative in explaining the relationship between inflammatory cytokines and inflammatory cytokine-related diseases, so the rabbit endotoxin shock model is used as a representative to illustrate the following aspects: drug Fr. The inhibitory effect of 5-1 on inflammatory cytokines in vivo; the therapeutic effect of drug Fr.5-1 on systemic inflammatory response syndrome (SIRS), septic shock, multiple organ dysfunction syndrome, and sepsis; drug Fr.5- 1 The basis for treating inflammation or inflammation-related diseases described i...

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Abstract

The invention discloses a compound with an anti-inflammatory effect, and applications of the compound in preparation of anti-inflammatory drugs. The compound has a structural formula represented by aformula (I) defined in the specification. The compound can significantly inhibit the expression of cellular inflammatory factors NO, TNF-alpha, IL-1beta and IL-6, can significantly reduce the contentsof cellular inflammatory factors in cells and tissues, and further has significant anti-inflammatory activity, good stability and good safety. According to the present invention, the compound is obtained by extraction, separation and purification from a traditional Chinese medicine Fuke Qianjin Tablet or Fuke Qianjin Capsules through secondary development by utilizing the modern technical means;meanwhile, the compound has simple and convenient extraction and separation method, is easy to synthesize, is applicable to industrial application of novel drugs, provides a direction for developmentof therapeutic drugs for inflammation or inflammation-related diseases, specifically for cervicitis, endometritis, pelvic inflammatory disease, mastitis and prostatitis, and has broad application prospects.

Description

technical field [0001] The invention belongs to the technical field of medicine, and more specifically relates to a compound with anti-inflammatory effect and its application in the preparation of anti-inflammatory drugs. Background technique [0002] As an important pathological process, inflammation is very common in the human body, and it itself is an autoimmune response of the body to external or foreign body stimuli. And when this response is dysregulated or excessively responds to the body's self-injury, it evolves into inflammation. Therefore, most diseases are accompanied by the mediation and occurrence of inflammation, and the mediation and occurrence of inflammation aggravate the damage to the body of the disease, such as rheumatoid arthritis, diabetes complications, cancer, atherosclerosis, inflammatory Enteropathy etc. In these processes, proinflammatory factors such as TNF-α, IL-6, IL-1β, etc. have played an important role. [0003] Macrophages can produce a ...

Claims

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Application Information

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IPC IPC(8): C07D307/58A61K31/365A61P29/00A61P15/00A61P13/08
CPCA61P13/08A61P15/00A61P29/00C07D307/58
Inventor 龚云王康华杨秀伟凌勇根白璐郑元青何娟娟赵威
Owner ZHUZHOU QIANJIN PHARMA
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