Erythropalum scandens extract and application thereof in health product for treating gout

Abstract

The invention relates to the technical field of gout treatment, in particular to an erythropalum scandens extract and application of the erythropalum scandens extract in health products for treating gout. In a first aspect, the invention discloses an erythropalum scandens extract with a structural formula as shown in the specification. On the second aspect, the erythropalum scandens extract can be applied to health products for treating gout, the health products comprise pharmaceutical preparations, health-care products or functional foods, any clinically or pharmaceutically acceptable pharmaceutical dosage form, health-care product or functional food can be prepared in a known mode in the field, and the erythropalum scandens extract can be used for oral administration and can be used for treating gout. An oral liquid preparation can be prepared, and a proper filling agent, a binding agent, a disintegrating agent and a lubricating agent can be added. The erythropalum scandens extract provided by the invention has a treatment effect on gout inflammation, and has good development prospects of medicines, health care products and functional foods. # imgabs0 #

Description

Technical Field

[0001] The present application relates to the technical field of gout treatment, and more specifically, to a Caulis Spatholobi extract and its application in health products for treating gout. Background Art

[0002] Gout is the second largest metabolic disease in my country, characterized by elevated uric acid levels. The global prevalence is about 10%. From 1990 to 2017, the age-standardized disability-adjusted life year (DALY) rate, prevalence and incidence of gout in my country increased by 6.92%, 6.88% and 6.16%, respectively. The pathological mechanism of gout is a chronic inflammatory disease caused by the deposition of monosodium urate (MSU) crystals in joints and surrounding tissues. It releases a variety of inflammatory mediators such as interleukins and tumor necrosis factor, triggering an inflammatory cascade reaction, resulting in symptoms such as redness, swelling, heat and pain in the joints. Gout can recur repeatedly, leading to joint dislocation or pathological fractures, and is often accompanied by kidney disease and a variety of chronic diseases such as hypertension, diabetes, and hyperlipidemia, which seriously endangers human health.

[0003] Currently, there are very limited drugs for the treatment of gout. Even colchicine, the first-line drug for the clinical treatment of gout, has limited efficacy, which affects its clinical application. Therefore, finding new anti-gout health substances is of great significance for more effective management of gout symptoms and prevention of recurrence. Summary of the invention

[0004] The primary purpose of the present invention is to provide a new extract of Caulis dahuricae and to provide the application of the extract of Caulis dahuricae in anti-gout health products. In the first aspect, the Caulis dahuricae extract provided in the present application adopts the following technical scheme:

[0005] The structural formula of the extract of red cangcunia is as follows:

[0006]

[0007] In the second aspect, the extract of the present application can be used in health products for treating gout.

[0008] This application has the following beneficial effects:

[0009] The extract of the present application of the red cang vine can be applied to health products to promote or maintain human health. Health products include but are not limited to pharmaceutical preparations, health products and functional foods. It can be formulated into any dosage form that is clinically or pharmaceutically acceptable in a manner known in the art, and can also be processed into health products or functional foods in a manner known in the art. When used for oral administration, it can be made into conventional solid preparations, such as tablets, capsules, pills, granules, etc.; it can also be made into oral liquid preparations, such as oral solutions, oral suspensions, syrups, etc. When making oral preparations, suitable fillers, adhesives, disintegrants, lubricants, etc. can be added. When used for parenteral administration, it can be made into injections, including injections, sterile powders for injection and concentrated solutions for injection. When making injections, conventional methods in the existing pharmaceutical field can be used for production. When preparing injections, additives can be omitted, or suitable additives can be added according to the properties of the drug.

[0010] The extract of the red cang vine provided in the present application can have a therapeutic effect on gout inflammation and has good development prospects for drugs, health products and functional foods. BRIEF DESCRIPTION OF THE DRAWINGS

[0011] Figure 1 Compound Palumoid A 1 H NMR spectrum;

[0012] Figure 2 Compound Palumoid A 13 C NMR spectrum;

[0013] Figure 3 is the HSQC spectrum of compound PalumoidA;

[0014] Figure 4 Compound Palumoid A 1 H- 1 H COSY spectrum;

[0015] Figure 5 is the HMBC spectrum of compound PalumoidA;

[0016] Figure 6 It is the NOESY spectrum of compound PalumoidA;

[0017] Figure 7 Compound Palumoid B 1 H NMR spectrum;

[0018] Figure 8 Compound Palumoid B 13 C NMR spectrum;

[0019] Fig. 9is the HSQC spectrum of compound Palumoid B;

[0020] Fig.10 Compound Palumoid B 1 H- 1 H COSY spectrum;

[0021] Fig.11 is the HMBC spectrum of compound Palumoid B;

[0022] Fig.12 This is the NOESY spectrum of compound Palumoid B. DETAILED DESCRIPTION

[0023] The present application is further described in detail below in conjunction with embodiments.

[0024] Example

[0025] In the first aspect, the extract of the red cangcun extract disclosed in the examples of the present application has the following structural formula:

[0026] The present application example discloses a method for extracting a Caulis Aconitifolia extract having a structural formula of the above formula (I), comprising the following steps:

[0027] S1. Extraction: Weigh 20 kg of dried rhizomes of Caulis Sinensis and crush them into coarse powder, and heat and reflux them with 40 L of 95% (w / w) ethanol for 5 times, each time for 1 hour, to obtain multiple extracts; combine the extracts and concentrate them under reduced pressure until there is no ethanol smell, to obtain 1.75 kg of total extract; suspend the total extract in water, extract it with dichloromethane, and obtain 372.6 g of dichloromethane extract fraction;

[0028] S2, one elution:

[0029] (1) The dichloromethane extraction portion was subjected to silica gel column chromatography, using petroleum ether-ethyl acetate as an eluent, and preliminary elution was performed according to an elution gradient of petroleum ether to ethyl acetate in a volume ratio of 100:0 to 0:100. In this embodiment, the elution was performed according to an elution gradient of petroleum ether to ethyl acetate in a volume ratio of 100:0, 100:5, 100:10, 100:20, 100:50, and 0:100;

[0030] (2) Through thin layer chromatography (TLC) analysis, similar fractions were combined to obtain five main fractions, Fr.A, Fr.B, Fr.C, Fr.D and Fr.E; the fraction Fr.D was subjected to MCI column chromatography, and eluted according to a gradient of acetonitrile and acid water in a volume ratio of 50:50 to 100:0 to obtain four sub-fractions, Fr.Da, Fr.Db, Fr.Dc and Fr.Dd;

[0031] S3, secondary elution:

[0032] (1) Dissolving the fraction Fr.Db and applying it to a Sephadex LH-20 column, eluting with a solvent of a mixture of dichloromethane and methanol in a volume ratio of 1:1 as an eluent, collecting the eluate, analyzing it by TLC and HPLC, combining similar fractions, and obtaining 6 fractions Fr.DBa, Fr.DBb, Fr.DBc, Fr.DBd, Fr.DBe, and Fr.DBf;

[0033] (2) The fraction Fr.DBe was concentrated and dissolved in methanol, and separated and purified by reverse phase preparative HPLC using acetonitrile-acid water in a volume ratio of 70:30 as the eluent, and the acid water was eluted with trifluoroacetic acid at a mass percentage of 0.01% to obtain compound Palumoid A.

[0034] The present application also discloses an extraction method of a Caulis Atractylodis Macrocephala extract having a structural formula of the above formula (II), which is different from the method for preparing the Caulis Atractylodis Macrocephala extract of formula (I) in that step S3, the second step of the secondary elution, is as follows: the fraction Fr.DBd is concentrated and then dissolved in methanol, separated and purified by reverse phase preparative HPLC, and eluted with acetonitrile-acid water in a volume ratio of 60:40 to obtain compound Palumoid B;

[0035] The remaining steps and conditions are the same as those for preparing the Caulis Spatholobi extract of formula (Ⅰ).

[0036] In a second aspect, the Palumoid A and Palumoid B prepared in the examples of the present application can be applied to health products for the treatment of gout, including pharmaceutical preparations, health products or functional foods, and have a therapeutic effect on gout inflammation.

[0037] (1) Structural identification of compound Palumoid A

[0038] Pale yellow oil, its specific rotation is (c 0.1, methanol); HRMS m / z 367.1516 [M+Na] + (Calculated value C 20 H 24 O5Na:367.1521); 1 HNMR, 13 CNMR, HSQC, 1 H- 1 HCOSY, HMBC and NOESY NMR spectra are shown in Figures 1 to 6 . Proton spectrum ( 1 HNMR) and carbon spectra ( 13 CNMR) attributes are shown in Table 1.

[0039] Based on the above physicochemical and spectral data, the structure of the identified compound Palumoid A is shown in the following formula (II), which is consistent with formula (I).

[0040] (2) Structural identification of compound Palumoid B

[0041] Pale yellow oil, its specific rotation (c 0.1, methanol); UV (methanol) λmax 210, 280 nm; HRMS m / z 433.2351 [M+Na] + (Calculated value C 26 H 34 O4Na:433.2351); 1 H NMR, 13 C NMR, HSQC, 1 H- 1 H COSY, HMBC and NOESY NMR spectra are shown in Figures 7 to 12 . Proton spectrum ( 1 H NMR) and carbon spectroscopy ( 13 C NMR) assignments are shown in Table 2.

[0042] Based on the above physicochemical and spectral data, the structure of the identified compound Palumoid B is shown in the following formula (IV), which is consistent with formula (II).

[0043] Table 1 NMR data of compound Palumoid A (CD3OD, Jin Hz)

[0044]

[0045] Table 2 NMR data of compound Palumoid B (CDCl3, Jin Hz)

[0046]

[0047] Based on the above physicochemical and spectral data, the structure of compound Palumoid A is shown in the following formula (III), which is consistent with formula (I); the structure of compound Palumoid B is shown in the following formula (IV), which is consistent with formula (II).

[0048]

[0049] Performance testing

[0050] Detection Methods

[0051] Elisa was used to test the therapeutic effects of the two compounds on gout inflammation:

[0052] Enzyme-linked immunosorbent assay (ELISA)

[0053] In this example, THP-1 cells were induced to differentiate by treatment with phorbol lipids, and then LPS and compounds were added to incubate the cells, and finally sodium urate was added to induce the cells to produce inflammatory factors. After 24 hours, the cell supernatant was taken to detect the content of IL-1β.

[0054] The results are shown in Table 3

[0055] Table 3 Inhibition rate of compounds on IL-1β at 10 μM concentration

[0056]

[0057] The results showed that compound Palumoid A and compound Palumoid B can significantly inhibit the production of IL-1β induced by sodium urate, and their activity is better than that of the clinical anti-gout drug colchicine. This specific embodiment is only an explanation of the present application, and it is not a limitation of the present application. After reading this specification, those skilled in the art can make modifications to the present embodiment as needed without creative contribution, but as long as they are within the scope of the claims of the present application, they are protected by the patent law.

Claims

1. A Caulis Spatholobi extract, characterized in that The general structure is as follows:

2. Use of the Caulis Cangcunii extract as claimed in claim 1 in health products for treating gout, wherein the health products include pharmaceutical preparations, health products or functional foods.

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