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Use of pachycladous algal onychin

A technology of phycocyanin and thick branch, applied in the field of medicine, can solve the problems such as the same structure and activity that are not seen

Inactive Publication Date: 2009-10-28
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] Crassicaulisine is a new type of glycolipid compound isolated from the red alga Chondriacrassicaulis Harv. for the first time. After searching the literature, there is no report with the same structure and activity.

Method used

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  • Use of pachycladous algal onychin
  • Use of pachycladous algal onychin
  • Use of pachycladous algal onychin

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Embodiment one: the preparation of compound Crassicaulisine (Crassicaulisine)

[0029] (1) Extraction: soak 4.6 (kg) of air-dried Chondria crassicaulis Harv. in industrial methanol at room temperature and extract completely. The extract was concentrated under reduced pressure to obtain methanol extract. Dissolve the methanol extract in water to form a suspension with CH 2 Cl 2 Extract, concentrate the extract to get CH 2 Cl 2 Extract (70g).

[0030] (2) Separation: CH 2 Cl 2 The extract was subjected to repeated silica gel column chromatography, and the elution gradient was gradually increased with petroleum ether-ethyl acetate-methanol, and the fractions eluted with MeOH:EtOAc=1:4 were collected, then applied to the silica gel column, and used CHCl 3 :MeOH=9:1, the compound Crassicaulisine (538 mg) was obtained.

Embodiment 2

[0031] Example 2: PTP1B inhibitory activity experiment of the compound Crassicaulisine

[0032] experimental method:

[0033] The protein tyrosine phosphatase PTP1B gene used for screening was constructed on the pGEX-KG vector by the method of molecular cloning, and then transformed into E. coli expression strain BL21(DE3), induced by IPTG and broken through the glutathione agarose affinity layer The GST fusion protein was obtained by column purification. After separation and identification by 12% SDS-PAGE gel, the purity reached above 90%. Further analysis of its enzymatic properties (K m 、k cat ) are consistent with the recombinant protein reported in the literature.

[0034] Using the ultraviolet substrate pNPP (test principle in the summary of the invention), the product obtained by hydrolyzing the phospholipid bond in the substrate pNPP by PTP1B has a strong light absorption at 410nm, and the change of light absorption at 410nm can be directly monitored to observe the...

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Abstract

The invention relates to the field of medical technology, in particular to a new type of compound Chondria crassicaulis Harv., which is extracted and isolated from Chinese marine red algae Chondria crassicaulis Harv. Crassicaulisine has the following structure: multiple in vitro protein tyrosine phosphatase 1B inhibition experiments show that this type of compound has obvious PTP1B inhibitory activity and can be used in the preparation of drugs for diabetes, obesity and complications. It is of great significance to the development and utilization of medicinal plant resources in China.

Description

technical field [0001] The invention relates to the field of medical technology, in particular to a compound Crassicaulisine extracted and separated from Chinese marine red algae Chondria crassicaulis Harv. After biological activity tests, the results show that the compound Has the activity of inhibiting protein tyrosine phosphatase 1B. The compound can be used as a PTP1B inhibitor and an insulin sensitizer, and can be used for treating various diabetes, obesity and the complications thereof. Background technique [0002] Diabetes mellitus (diabetes mellitus) is a group of clinical syndromes caused by the interaction of genetic and environmental factors. Due to the absolute or relative insufficiency of insulin secretion and the decreased sensitivity of target tissue cells to insulin, sugar, protein, fat, water, and electrolytes are caused. and other metabolic disorders. Severe complications such as coronary heart disease, iron deficiency or hemorrhagic cerebrovascular dise...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/7028A61P3/10A61P3/04
Inventor 郭跃伟李佳邵志宇南发俊姚励功
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI