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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
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  • Abstract
  • Description
  • Claims
  • Application Information

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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, Guangdong and other places, the whole herb is used as medicine in the folk, with It has the functions of promoting blood circulation, removing blood stasis, detoxifying and reducing swelling, etc., and its chemical composition has not been reported yet

Method used

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  • 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

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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

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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

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Application Information

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IPC IPC(8): C07D493/10A61K31/343A61P3/10A61P3/04
Inventor 胡金锋熊娟洪志来杨国勋
Owner FUDAN UNIV
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