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Phloroglucinol and abietane diterpenoids, preparation method and medicinal use thereof

A technology of phloroglucinol-abietane and compound, 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: 2018-05-25
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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  • Phloroglucinol and abietane diterpenoids, preparation method and medicinal use thereof
  • Phloroglucinol and abietane diterpenoids, preparation method and medicinal use thereof

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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 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. The present invention is obtained by extracting and separating the whole plant or root of Chloranthus oldhami (Chloranthus oldhami, also known as Taiwan Chloranthaceae, Chloranthaceae) plant of the genus Chloranthaceae, and has protein tyrosine phosphatase 1B (PTP1B) inhibitory activity The new type of phloroglucinol parallel abietane diterpenoids (structure as follows), wherein R1, R2 is methyl or hydroxymethyl; R3 is a long chain olefin. The results of in vitro biological activity tests show that the compound has significant PTP1B inhibitory activity and can be used to prepare drugs for preventing, delaying or treating diabetes, obesity and its complications and other PTP1B-mediated diseases. .

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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Patent Type & Authority Patents(China)
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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