Novel application of garcinia mangostana L pericarp extract in prevention and treatment of hyperuricemia and gout

Abstract

The invention relates to novel application of garcinia mangostana L pericarp extract in prevention and treatment of hyperuricemia and gout. Researches find that the garcinia mangostana L pericarp extract is capable of in-vitro inhibiting activities of xanthine oxidase, and IC50 of the garcinia mangostana L pericarp extract is 31.39ml / L. in vivo studies show that the garcinia mangostana L pericarpextract has a strong uric acid lowering effect, by feeding 20mg / kg of the garcinia mangostana L pericarp extract to a mouse with oteracil potassium induced hyperuricemia intragastrically, the serum uric acid level of the mouse can be obviously lowered, which means the uric acid lowering effect of the garcinia mangostana L pericarp extract is related to inhibition of the xanthine oxidase activities, and generation of the uric acid is inhibited. By feeding 2.0g / kg of the garcinia mangostana L pericarp extract to the mouse intragastrically, no animal dies, and no obvious toxic and side effect isfound, so that the garcinia mangostana L pericarp extract can be used for preparing oral medicaments for treating the gout and the hyperuricemia and medicament and health care products for diseases related to the hyperuricemia.

Description

technical field

[0001] The invention relates to a new application of mangosteen peel extract in the prevention and treatment of hyperuricemia and gout, and belongs to the technical field of medicine. Background technique

[0002] Gout is a group of metabolic diseases caused by the excessive production of uric acid due to purine metabolism disorder and / or the decrease of uric acid excretion, which leads to the increase of uric acid level and the formation of uric acid crystals deposited in joints, soft tissues, and kidneys. Uric acid is the end product of human purine metabolism, and hyperuricemia is usually considered a sign of gout. According to statistics, about 5% to 12% of patients with hyperuricemia will eventually develop gout [1] . In Europe, North America, Japan and other regions and countries, the incidence of gout is relatively high, but with the improvement of people's living standards in our country, the extension of life span, the change of diet structure, and ...

Examples

Embodiment 1

[0022] Embodiment 1: preparation of mangosteen peel extract

[0023] Take 10 kg of mangosteen peel, coarsely crush it, pass through a 10-mesh sieve, add 30L of 75% ethanol, soak for 24 hours, then extract twice in the same way, combine the three extracts, and concentrate under reduced pressure at 60°C to a small volume (until there is no ethanol smell) , vacuum-dried (60° C.), and pulverized to obtain 2.58 kg.

Embodiment 2

[0024] Example 2: Effect of mangosteen peel extract on blood uric acid in mice with hyperuricemia induced by potassium oxonate

[0025] Healthy male Kunming mice (body weight 18-22g) were provided by Beijing Huafukang Biotechnology Co., Ltd., certificate number: SCXK (Beijing) 2014-0004. Animals were randomly divided into normal control group, hyperuricemia model group, mangosteen peel ethanol extract 5.0, 10.0, 20.0 mg / kg and positive control group allopurinol 5 mg / kg. The test compound was formulated with 0.5% sodium carboxymethylcellulose (0.5% CMC-Na) to an appropriate concentration, administered orally, twice a day, 7 doses in total. Reference [Hall IH, Scoville JP, Reynolds DJ, Simlot R, Duncan P.Substituted cyclic imides aspotencial anti-gout agents.Life Sciences.1990, 46:923-1927.Stavric B, ClaymanS, Gradd REA, Hebert D.Some in vivo effects in the rat induced by chlorprothixene and potassium oxonate Pharmacology Research, 1975, 7: 117-124] using the uricase inhibitor ...

Embodiment 3

[0031] Example 3: Inhibitory effect of mangosteen peel extract on xanthine oxidase activity in vitro

[0032] Xanthine oxidase (EC 1.1.3.22) is a product of Sigma Company, prepared with sodium pyrophosphate buffer solution to an appropriate concentration for use. The mangosteen peel extract was prepared into a series of concentrations with sodium pyrophosphate buffer, and DMSO was used to help dissolve. After incubating a series of concentrations of mangosteen peel alcohol extract solution and xanthine oxidase at 25°C for 15 minutes, refer to the literature method [Zhu Shenyin, Zhou Yuanda, Liu Qingshan, Du Guanhua. Establishment and application of high-throughput screening model for xanthine oxidase inhibitors . Chinese Journal of Pharmaceutical Sciences, 2007, 42 (3): 187-190] measure the activity of xanthine oxidase, the result shows that mangosteen peel ethanol extract has certain inhibition to the activity of xanthine oxidase, and its IC 50 It was 31.39 mg / L (Table 2). ...

technical field

[0001] The invention relates to a new application of mangosteen peel extract in the prevention and treatment of hyperuricemia and gout, and belongs to the technical field of medicine. Background technique

[0002] Gout is a group of metabolic diseases caused by the excessive production of uric acid due to purine metabolism disorder and / or the decrease of uric acid excretion, which leads to the increase of uric acid level and the formation of uric acid crystals deposited in joints, soft tissues, and kidneys. Uric acid is the end product of human purine metabolism, and hyperuricemia is usually considered a sign of gout. According to statistics, about 5% to 12% of patients with hyperuricemia will eventually develop gout [1] . In Europe, North America, Japan and other regions and countries, the incidence of gout is relatively high, but with the improvement of people's living standards in our country, the extension of life span, the change of diet structure, and ...

Examples

Embodiment 1

[0022] Embodiment 1: preparation of mangosteen peel extract

[0023] Take 10 kg of mangosteen peel, coarsely crush it, pass through a 10-mesh sieve, add 30L of 75% ethanol, soak for 24 hours, then extract twice in the same way, combine the three extracts, and concentrate under reduced pressure at 60°C to a small volume (until there is no ethanol smell) , vacuum-dried (60° C.), and pulverized to obtain 2.58 kg.

Embodiment 2

[0024] Example 2: Effect of mangosteen peel extract on blood uric acid in mice with hyperuricemia induced by potassium oxonate

[0025] Healthy male Kunming mice (body weight 18-22g) were provided by Beijing Huafukang Biotechnology Co., Ltd., certificate number: SCXK (Beijing) 2014-0004. Animals were randomly divided into normal control group, hyperuricemia model group, mangosteen peel ethanol extract 5.0, 10.0, 20.0 mg / kg and positive control group allopurinol 5 mg / kg. The test compound was formulated with 0.5% sodium carboxymethylcellulose (0.5% CMC-Na) to an appropriate concentration, administered orally, twice a day, 7 doses in total. Reference [Hall IH, Scoville JP, Reynolds DJ, Simlot R, Duncan P.Substituted cyclic imides aspotencial anti-gout agents.Life Sciences.1990, 46:923-1927.Stavric B, ClaymanS, Gradd REA, Hebert D.Some in vivo effects in the rat induced by chlorprothixene and potassium oxonate Pharmacology Research, 1975, 7: 117-124] using the uricase inhibitor ...

Embodiment 3

[0031] Example 3: Inhibitory effect of mangosteen peel extract on xanthine oxidase activity in vitro

[0032] Xanthine oxidase (EC 1.1.3.22) is a product of Sigma Company, prepared with sodium pyrophosphate buffer solution to an appropriate concentration for use. The mangosteen peel extract was prepared into a series of concentrations with sodium pyrophosphate buffer, and DMSO was used to help dissolve. After incubating a series of concentrations of mangosteen peel alcohol extract solution and xanthine oxidase at 25°C for 15 minutes, refer to the literature method [Zhu Shenyin, Zhou Yuanda, Liu Qingshan, Du Guanhua. Establishment and application of high-throughput screening model for xanthine oxidase inhibitors . Chinese Journal of Pharmaceutical Sciences, 2007, 42 (3): 187-190] measure the activity of xanthine oxidase, the result shows that mangosteen peel ethanol extract has certain inhibition to the activity of xanthine oxidase, and its IC 50 It was 31.39 mg / L (Table 2). ...

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