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8-epi-Hypophyllin E and derivatives and pharmaceutical composition thereof and application of 8-epi-Hypophyllin E in pharmacy

A technology of derivatives and compositions, applied in the field of preparation and treatment of metabolic syndrome, which can solve the problems of compound separation and no report of activity

Active Publication Date: 2017-06-13
KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Phyllostin G is a diterpenoid compound of furan hemelane, and the isolation and activity of this compound have not been reported at present

Method used

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  • 8-epi-Hypophyllin E and derivatives and pharmaceutical composition thereof and application of 8-epi-Hypophyllin E in pharmacy
  • 8-epi-Hypophyllin E and derivatives and pharmaceutical composition thereof and application of 8-epi-Hypophyllin E in pharmacy
  • 8-epi-Hypophyllin E and derivatives and pharmaceutical composition thereof and application of 8-epi-Hypophyllin E in pharmacy

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Isolation, extraction and structural identification of compound 8‐epi‐hypophyllin E:

[0038] Erythema gun knife medicine (H.phyllostachya) 8kg, crushed, soaked and extracted with acetone at room temperature three times, each time for 48 hours, combined extracts concentrated under reduced pressure to obtain crude extract (950g). The crude extract was dispersed in water, extracted four times with an equal volume of ethyl acetate, and the extract was concentrated under reduced pressure. Ethyl acetate extract (680g) was subjected to silica gel column chromatography (100-200 mesh, 2kg), petroleum ether-acetone gradient elution (1:0, 8:2, 6:4, 1:1, 0:1 , the amount of each gradient solvent is 10L), which were detected by TLC and combined into five components (Fr1-Fr5). Component 2 (Fr2) was separated by reverse-phase medium-pressure liquid chromatography (MPLC, MCI), and eluted with methanol-water system gradient (70:30, 75:25, 80:20, 85:15, 90:10 and 95:5), which were det...

Embodiment 2

[0042] Activity of 8‐epi‐Hypophyllin E in diabetes and metabolic syndrome-related diseases.

[0043] C57BL / KsJdb / db mouse (db / db mouse) is a mouse model of type Ⅱ diabetes, mainly exhibiting leptin deficiency, hyperglycemia, hyperinsulinemia, abnormal glucose metabolism, abnormal lipid metabolism, obesity, fatty liver and other features.

[0044] The tested C57BL / KsJdb / db mice were 8-week-old female mice, SPF grade, purchased from Shanghai Institute of Materia Medica, Chinese Academy of Sciences. The feeding conditions were raised in accordance with the SPF grade animal standard feeding operation procedures. Except for the necessary fasting time, they were allowed to eat and drink freely, and the feed was conventional feed.

[0045] Experimental Materials:

[0046] Compound 8‐epi‐hypophyllin E is a white powder, and a mixture of PEG400 and water is used as a solvent (VPEG400:Vwater=3:7). Grind it into a fine powder with a mortar first, then add PEG400 to grind until uniform...

Embodiment 3

[0097] Preparation of tablets:

[0098] The compound 8-epi-hypophyllin E was first prepared according to the method of Example 1, and the excipient was added in a weight ratio of 1:5-1:10 to the excipient, and then granulated and compressed into tablets.

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Abstract

The invention discloses a compound 8-epi-Hypophyllin E which is separated from hypoestesphyllostachya (Hypoestesphyllostachya) and has a structure in a formula (I), derivatives of the 8-epi-hypophyllin E, a pharmaceutical composition employing the 8-epi-hypophyllin E as an effective component and an application in preparation of medicines for treating metabolic syndromes, such as type II diabetes. The 8-epi-hypophyllin E is capable of significantly reducing blood glucose of db / db mice with the type II diabetes C57BL / KsJ, significantly improving the sugar tolerance and the insulin tolerance of the db / db mice, partially improving the liver function and significantly reducing the content of serum triglyceride and free fatty acid and can be used for preparing the metabolic syndrome, such as a therapeutic medicine for the type II diabetes.

Description

technical field [0001] The invention belongs to the technical field of medicines, and specifically relates to compound 8-epi-hypophyllin E and its derivatives, a pharmaceutical composition containing it as an active ingredient, and its application in the preparation of drugs for treating metabolic syndrome, such as type II diabetes. Background technique [0002] Metabolic syndrome is a syndrome of glucose metabolism and lipid metabolism disorders characterized by abnormal blood lipids, abnormal blood sugar, obesity, fatty liver, hypertension, hypercoagulability, type 2 diabetes, atherosclerosis, non-alcoholic fatty liver, etc. . With economic development and changes in people's lifestyles, the incidence of diabetes and cardiovascular diseases caused by metabolic syndrome has increased dramatically. Type Ⅱ diabetes, also known as non-insulin-dependent diabetes, is a metabolic syndrome characterized by hyperglycemia. In addition to concurrent ketoacidosis, limb gangrene, mult...

Claims

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Application Information

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IPC IPC(8): C07D307/46A61K31/341A61P3/06A61P1/16A61P3/00A61P3/10
CPCC07D307/46
Inventor 赵勤实苏佳吴兴德彭丽艳邵立东
Owner KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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