Phloroglucinolo abietane diterpenoid compound, preparation method thereof and medicinal application

A technology of phloroglucinol p-abietane and abietane diterpene, which is applied in the field of preparing protein tyrosine phosphatase 1B inhibitors, and can solve the problems that the chemical composition has not been reported yet.

Active Publication Date: 2016-08-10
FUDAN UNIV
View PDF4 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Chloranthus oldhami Solms-Laub (Chloranthus oldhami Solms-Laub., also known as Taiwan Chloranthus orchid, four-leaf gold) is Chloranthaceae (Chloranthaceae) Chloranthaceae plant, mainly distributed in southeastern my country such as Fujian, Gu

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Phloroglucinolo abietane diterpenoid compound, preparation method thereof and medicinal application
  • Phloroglucinolo abietane diterpenoid compound, preparation method thereof and medicinal application
  • Phloroglucinolo abietane diterpenoid compound, preparation method thereof and medicinal application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Embodiment 1: Preparation of phloroglucinol parallel abietane diterpenoids

[0027] Take 7kg of Southeastern Chrysanthemum Chrysalis root, crush it, extract it three times with 95% ethanol at room temperature, combine the extracts, and concentrate under reduced pressure to obtain 550g of extract; after dispersing the extract in water, extract it with petroleum ether and ethyl acetate in turn to obtain ethyl acetate 71.5g of the ester part; the ethyl acetate part was chromatographed on a 100-200 mesh silica gel column and eluted with a gradient of petroleum ether: ethyl acetate 20:1-0:1 to obtain 16 components (F1-F16); F11 (4.1g) was subjected to MCI column chromatography and eluted with a gradient of 80%-100% methanol to obtain 9 subfractions (F11a-11i), among which subfraction F11i (330.6mg) was successively passed through a silica gel column layer Analysis (eluent is dichloromethane: methanol 25:1) and gel Sephadex LH-20 column chromatography (eluent is methanol) to ...

Embodiment 2

[0032] Example 2: Determination of protein tyrosine phosphatase 1B inhibitory activity

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

PUM

No PUM Login to view more

Abstract

The invention belongs to the technical field of a medicine, and relates to a phloroglucinolo abietane diterpenoid compound, a preparation method of the compound and a medicinal application, particularly, an application to preparation of a protein-tyrosine-phosphatase 1B inhibitor. The novel phloroglucinolo abietane diterpenoid compound (having a structural formula shown in the description) capable of inhibiting activity of protein-tyrosine-phosphatase 1B (PTP1B) is extracted and separated from entire herbs or roots of chloranthus oldhami, which is a plant in chloranthus genus of the chloranthaceae family. In the structural formula, R1 and R2 are methyl or hydroxymethyl, and R3 is a long-chain alkene. An in-vitro biological activity test shows that the compound has obvious inhibition activity of PTP1B, and can be used for preparing medicines for preventing, delaying, or treating diabetes, obesity, and complication thereof, and other medicines mediated by PTP1B.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a phloroglucinol-abietane diterpenoid compound, a preparation method and a medicinal application thereof, especially the application in preparing protein tyrosine phosphatase 1B inhibitors. Background technique [0002] It is currently known that protein tyrosine phosphatase (protein tyrosine phosphatase, PTP) is an enzyme family that regulates the phosphorylation level of protein tyrosine residues in cells, and is closely related to cell proliferation and various intracellular signal transduction processes (Fischer et al., Science 1991, 253, 401-406). As the earliest purified and biologically characterized member of the PTP family, the protein tyrosine phosphatase 1B (protein tyrosine phosphatase 1B, PTP1B) is widely distributed in various human tissues; its full length is about 50KDa (Charbonneau et al., Proc. Natl. Acad. Sci. USA 1989, 86, 5252–5256). Studies have found that ...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

Application Information

Patent Timeline
no application Login to view more
IPC IPC(8): C07D493/10A61K31/343A61P3/10A61P3/04
Inventor 胡金锋熊娟洪志来杨国勋
Owner FUDAN UNIV
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap