CN-122005586-A - Application of saikosaponin B2 in preparation of medicines

Abstract

The invention provides application of saikosaponin B2 in preparation of a medicament, and belongs to the technical field of natural medicaments. The invention discovers that the saikosaponin B2 has obvious effect of inhibiting the activation of NLRP3 inflammation bodies, can be used for preparing NLRP3 inflammation body inhibitors, is used for preparing medicines for treating diseases (including gout and gouty arthritis) related to NLRP3 inflammation bodies, and has wide application prospect.

Inventors

• WANG FEI
• Cao Dongyi
• Xi Ruiying
• JI MINGHUI

Assignees

• 中国科学院成都生物研究所

Dates

Publication Date

20260512

Application Date

20260408

Priority Date

20250410

Claims (5)

1. 1. Use of saikosaponin B2 in preparing medicine for preventing and/or treating gout or gouty arthritis is provided.
2. 2. The use according to claim 1, wherein the gout is acute gout.
3. 3. The use according to claim 1, wherein the gouty arthritis is acute gouty arthritis.
4. 4. The use according to any one of claims 1 to 3, wherein the medicament is a preparation prepared by adding pharmaceutically acceptable auxiliary materials to Hu Zaogan B2 as an active ingredient.
5. 5. The use according to claim 4, wherein the formulation is an oral formulation or an injectable formulation.

Description

Application of saikosaponin B2 in preparation of medicines Technical Field The invention belongs to the technical field of natural medicines, and particularly relates to application of saikosaponin B2 in preparation of an NLRP3 inflammation small body inhibitor and a medicine for treating diseases related to NLRP3 inflammation small bodies. Background Hyperuricemia refers to that an adult does not divide men and women under normal purine diet, and the fasting blood uric acid level of 2 times a day is more than 420 mu mol/L. Hyperuricemia caused by abnormal purine metabolism has become a high-incidence chronic disease affecting the life and health of the population in China. Uric acid (uric acid) forms crystals (monosodium urate crystal, MSU) at joints, kidneys, etc. as a main cause of gout. However, gout and hyperuricemia are two diseases, and the therapeutic drugs are not universal. Currently patients with gout reduce serum uric acid levels mainly by prophylactic treatment to inhibit uric acid synthesis (e.g., huang Piao-one of the oxidase inhibitor febuxostat) or to promote uric acid excretion (e.g., phenylbromomarone, which inhibits the transport of uric acid by tubular URAT-1, etc.). The first-line medicine in the acute onset stage of gout is colchicine or a non-steroidal anti-inflammatory medicine, but has the condition of poor curative effect and larger side reaction, and the second-line medicine is glucocorticoid accompanied with joint and bone injury, so no good treatment means is known at present. The development of a novel anti-gout drug which is safe, effective, economical and convenient has important significance. The Bupleurum is dried root of Bupleurum Bupleurum chinense DC or Bupleurum scorzonerifolium Bupleurum scorzonerifolium Willd. Has the functions of relieving exterior and interior, soothing liver and raising yang. Can be used for treating common cold, fever, distending pain in chest and hypochondrium, menoxenia, uterine prolapse, and rectocele. Annual output is 5000-7000 tons. Although about 87 clinical traditional Chinese medicine varieties taking bupleurum as a main component in the domestic market are developing clinical researches on related diseases such as fever, depression, tumor, sepsis and the like caused by cold at present, the researches on gout are very few. If the components in the bupleurum can inhibit the inflammatory reaction of gout, the bupleurum has wide application prospect in the second largest metabolic disease gout in China, thereby being hopeful to fill up the market gap of acute gout drugs. Disclosure of Invention The invention aims to provide application of saikosaponin B2 in preparing an NLRP3 inflammation small body inhibitor and a medicine for treating diseases related to NLRP3 inflammation small bodies. The invention provides an application of Hu Zaogan B2 in preparing an NLRP3 inflammation small inhibitor. The invention also provides application of Hu Zaogan B2 in preparing a medicament for preventing and/or treating diseases related to NLRP3 inflammation small body. Further, the disease associated with NLRP3 inflammatory minibody is gout. Further, the gout is acute gout. Further, the disease associated with NLRP3 inflammatory minibody is gouty arthritis. Further, the gouty arthritis is acute gouty arthritis. Further, the medicine is a preparation prepared by taking Hu Zaogan B2 as an active ingredient and adding pharmaceutically acceptable auxiliary materials. Further, the preparation is an oral preparation or an injection preparation. The invention has the following beneficial effects: 1. The invention discovers that the bupleurum root effective component saikosaponin B2 (Saikosaponin B2, SSB2 for short) has obvious effect of inhibiting the activation of NLRP3 inflammatory corpuscles. In experiments on activation of NLRP3 inflammatory bodies in the mouse macrophage cell line j774a.1, saikosaponin B2 was able to significantly inhibit release of cellular IL-1β with IC 50 at 3.544 μm. Further researches show that the saikosaponin B2 can target an ASC protein which is an important component of an NLRP3 inflammatory corpuscle, and the affinity between the saikosaponin B2 and the ASC is about 9.39 mu M by adopting a biological film interference technology. 2. The saikosaponin B2 has no obvious toxicity to macrophages and hepatocytes. Whereas saikosaponin A, saikosaponin D, saikosaponin B1 showed cytotoxicity to SK-Hep-1, HCCLM3 and J774A.1 macrophages at a concentration of 25. Mu.M. It can be seen from the data reported in the literature (PLANTA MEDICA, 1978, 34 (2): 160-166) that saikosaponin B2 has a lower hemolysis than saikosaponin A and saikosaponin D, and has better safety. 3. In the pharmacokinetic test, the result of the invention shows that the saikosaponin B2 reaches a peak value at 1.6h and the maximum concentration is 378ng/ml and is reduced to half at about 4h when 20mg/kg is orally administered, but according to the literature report, the saikos