The bark extract of the five-needled pine of Dabie Mountains, its preparation method and its application in pharmacy

A technology for the preparation and use of medicines, which is applied to the bark extract of Pinus dabies and its preparation and use in pharmaceuticals, and can solve the problems of low germination rate, no reports on chemical components, and difficulties in natural regeneration

Active Publication Date: 2019-12-20
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

The distribution range is narrow, the fruiting mother plant is rare, the pollination rate is extremely low, the cone seeds are ten to nine empty, the seed abortion rate is extremely high, and the germination rate is extremely low, and the cone seeds are often harmed by squirrels, so the saplings in the forest are extremely less, natural renewal is very difficult, and its chemical composition has not been reported

Method used

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  • The bark extract of the five-needled pine of Dabie Mountains, its preparation method and its application in pharmacy
  • The bark extract of the five-needled pine of Dabie Mountains, its preparation method and its application in pharmacy

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Embodiment 1: the preparation of diterpenoids

[0024] Take 180 g of Dabie Mountain five-needle pine bark, crush it, extract it five times by cold soaking with 90% methanol at room temperature, combine the extracts, concentrate under reduced pressure, and obtain 50 g of extract. The extract was dispersed in water and then extracted with petroleum ether and ethyl acetate to obtain 40.0 g of ethyl acetate. The ethyl acetate part was chromatographed on a 100-200 mesh silica gel column and eluted with a gradient of petroleum ether: ethyl acetate 30:1-0:1 and ethyl acetate: methanol 15:1-0:1 to obtain 8 components (Fr.A-Fr.H), component Fr.B (1.9 g) was subjected to 200-300 mesh silica gel column chromatography (eluent: petroleum ether: ethyl acetate 10:1-2:1) to obtain 3 Subfractions (Fr.B1-3), of which subfraction Fr.B1 (30.6 mg) were further separated by semi-preparative HPLC, and eluted isocratically with 73% acetonitrile (flow rate: 3 mL / min) to obtain the compound 3 ...

Embodiment 2

[0031] Example 2: Determination of protein tyrosine phosphatase 1B inhibitory activity

[0032] Experimental method: Using molecular biology methods to construct genetically recombined hGST-PTP1B-BL21 E. coli Human PTP1B engineering bacteria, the purified hGST-PTP1B recombinant protein can hydrolyze the substrate para The phospholipid bond of -NitrophenylPhosphate (pNPP), the obtained dephosphorylated product pNP has a strong light absorption at a wavelength of 405 nm, so the change of the enzyme activity and the effect of the compound on the enzyme activity can be observed by directly detecting the change of the light absorption at 405 nm Inhibition situation; initial screening selects described compound concentration as 20 µ The percentage inhibition rate of PTP1B enzyme activity was investigated at g / ml. The test results showed that the inhibition rates of compounds 4 and 5 were higher than 95%, and the inhibition rates of compounds 1-3 were higher than 60%. Further det...

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Abstract

The present invention belongs to the field of traditional Chinese medicines, and relates to Pinus dabeshanensis Cheng et Law bark extracts. According to the present invention, the diterpene compounds having structures defined in the specification and having protein-tyrosine phosphatase 1B (PTP1B) inhibition activity are extracted and separated from the bark of the Pinaceae Pinus plant Pinus dabeshanensis Cheng et Law, and the in vitro biological activity test results prove that the compounds have the significant PTP1B inhibition activity; and the obtained compounds can be used for preparing drugs for prevention, delaying or treatment of diabetes, obesity and complications thereof, and other PTP1B-mediated diseases.

Description

technical field [0001] The invention belongs to the field of traditional Chinese medicine, and relates to a bark extract of Pinus dabies and its preparation method and its application in pharmacy. Pinus dabeshanensis ) bark to obtain isopimarane-type and abietane-type diterpene compounds. The biological activity test shows that these compounds can significantly inhibit protein tyrosine phosphatase 1B (PTP1B), which can be used for the preparation of prevention or treatment of PTP1B-mediated Drugs for leading diseases, especially type II diabetes, obesity and their complications, or lead compounds of such drugs. The present invention also relates to the preparation method of this kind of compound. Background technique [0002] The prior art discloses 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 i...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D301/32C07D303/38C07C51/47C07C61/39C07C62/06A61K31/336A61K31/192A61P3/10A61P3/04
CPCC07C51/47C07C61/39C07C62/06C07D301/32C07D303/38
Inventor 胡金锋胡长玲熊娟杨国勋
Owner FUDAN UNIV
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