Chinese loropetalum extract comprising quinate and glucoside compounds and pharmaceutical application thereof

A technology of extract and quinic acid, which is used in the treatment of bleeding diseases and the preparation of hemostatic drugs.

Active Publication Date: 2016-02-03
INST OF PHARMACOLOGY & TOXICOLOGY ACAD OF MILITARY MEDICAL SCI P L A
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There are no related reports on obtaining quinic acid derivatives and glycoside compounds with good hemostatic activity from P.

Method used

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  • Chinese loropetalum extract comprising quinate and glucoside compounds and pharmaceutical application thereof
  • Chinese loropetalum extract comprising quinate and glucoside compounds and pharmaceutical application thereof
  • Chinese loropetalum extract comprising quinate and glucoside compounds and pharmaceutical application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Implementation Example 1: Preparation of the total extract of Roropetus alba and different polar parts

[0039] Take 20kg of dried medicinal materials of P. chinensis, cut into 2-3cm segments, soak and extract 3 times with 8-10 times acetone at room temperature, 5 days each time, combine the extracts, concentrate under reduced pressure to dryness, and obtain 902g of total extract of P. . Weigh 793.5 g of acetone extract, add 4 L of deionized water for ultrasonic dispersion, and add 4 L of petroleum ether for extraction 5 times. The water layer was evaporated to dryness to obtain 564.5 g of the water-soluble fraction. Add 2L of deionized water to dissolve, apply HP20 macroporous resin after filtration, the ratio of resin column diameter to height is 1:8, use 10%, 20%, 30%, 40%, 50%, 70% of 2 times BV after sample loading 95% ethanol-water gradient elution, collect 20%, 30%, 40% ethanol eluate and evaporate to dryness under reduced pressure to obtain 20%, 30%, 40% ethan...

Embodiment 2

[0040] Implementation example 2: preparation and spectral analysis of each monomeric compound

[0041] Take 20kg of dried medicinal materials of P. chinensis, and use the method of Example 1 to prepare the elution site of 30% ethanol of P. spp. Take 30.7g of the obtained 30% ethanol elution fraction, dissolve it in 20ml water, filter and use reverse phase C 18 Silica gel column chromatography, gradient elution with different concentrations of aqueous methanol (10%, 20%, 30%, 40%, 50%, 70%, 95%), divided into sections F1-F46. Sections F19-20 are combined and recorded as component B, and then reversed phase C 18 Silica gel column chromatography, gradient elution with different concentrations of aqueous methanol (5%, 10%, 15%, 20%, 25%, 30%, 40%, 50%, 100%), divided into B1-B58. Where B8-B10 are combined, use LH-20 column chromatography, elute with methanol, and divide into B-8-1 to B-8-58, where components B-8-16 to B-8-26 are combined, and use silica gel Column chromatograph...

Embodiment 3

[0054] Implementation Example 3: Evaluation of the hemostatic effect of the total extract of Roropetus alba, different polar parts and monomeric compounds.

[0055] 1. The impact of the total extract of Example 1 on the bleeding time and bleeding amount by rat tail docking method

[0056] Experimental animals: Wistar rats, half male and half male, weighing 180g±10g, purchased from Beijing Weitong Lihua Company, and bred in the experimental animal center of the unit.

[0057] Test sample: the total extract of Example 1, dissolved with physiological saline.

[0058] Experimental method and results: 18 Wistar rats were randomly divided into 3 groups, 6 rats in each group. After the tail was docked 3cm from the root of the tail, intraperitoneal injection was administered, and the bleeding stop time and bleeding volume were observed; or intraperitoneal injection for 30 minutes Finally, the tail was docked at 3 cm from the root of the tail, and the bleeding stop time and bleeding v...

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Abstract

The invention relates to white-flower Chinese loropetalum extract which comprises quinate derivative ingredients and glucoside ingredients. The quinate derivative ingredients include one or multiple of chlorogenate methyl ester, chlorogenate ethyl ester and 5-O-p-coumaroyl quinate methyl ester, and the glucoside ingredients include one or multiple of rhodioside, (Z)-3-hexenyl-O-alpha-L-rhamnopyranosyl-(1->6)-beta-D-glucopyranoside, benzyl-O-alpha-L-rhamnopyranosyl-(1->6)-beta-D-glucopyranoside, myricitrin and quercetin-3-O-(6'-O-galloyl)-beta-glucoside. The invention further relates to a preparation method of and a drug combination of the white-flower Chinese loropetalum extract and application of the extract in preparing hemostatic drug or products. Pharmacodynamic and acute toxicity experiments of the extract show that the extract has the advantages of clear active ingredients, strong pharmacodynamic effect, little toxic and side effect, high product purity, low administration dosage and controllable quality.

Description

technical field [0001] The present invention belongs to the field of traditional Chinese medicine and chemical medicine, in particular, the present invention relates to the extract of Loropetalum officinalis rich in quinic acid derivatives and glycosides, its preparation method and its application in the treatment of hemorrhagic diseases and the preparation of hemostatic drugs . Background technique [0002] Bleeding is the clinical manifestation of many diseases, and it is also one of the important causes of death of patients. Clinical hemorrhagic disorders are a group of diseases that cause spontaneous or traumatic bleeding due to abnormalities in congenital or acquired hemostatic mechanisms (including blood vessels, platelet quantity and quality, and coagulation factors), which seriously threaten patients life and health. Hemostatic drugs can produce hemostatic effect by constricting small arteries and capillaries, enhancing platelet function, accelerating blood coagula...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K36/185A23L1/29A61P7/04C07H1/08C07H15/18C07H15/10C07H17/07C07C69/757C07C67/48
Inventor 张杨任凤霞杨郁魏雷赵毅民
Owner INST OF PHARMACOLOGY & TOXICOLOGY ACAD OF MILITARY MEDICAL SCI P L A
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