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Sesquiterpene spirolide compound and its preparation method and use

A technology of ester compounds and sesquiterpenes, which is applied in the field of medicine, can solve the problems that there are no reports on chemical components and pharmacological activities

Active Publication Date: 2019-02-26
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

At present, there are no reports on its chemical composition and pharmacological activity.

Method used

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  • Sesquiterpene spirolide compound and its preparation method and use

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Effect test

Embodiment 1

[0017] Embodiment 1: Preparation of myrrhalkane-type sesquiterpene spirolide compounds

[0018]Take 500 g of the bark of Abies Baishanzu, crush it, extract it five times by cold soaking with 90% methanol at room temperature, combine the extracts, concentrate under reduced pressure, and obtain 30 g of extract. The extract was dispersed in water and then extracted with petroleum ether and ethyl acetate to obtain 12.0 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 15:1-0:1 and ethyl acetate: methanol 15:1-0:1 to obtain 6 components (Fr. 1-Fr. 6). Subfraction Fr.6 was further separated by semi-preparative HPLC and eluted isocratically with 55% methanol (flow rate: 3 mL / min) to obtain compound beshanzuenone C (3.0 mg, t R =8.4 min) and beshanzuenone D (1.5 mg, t R = 16.0 min);

[0019] Compounds beshanzuenone C and beshanzuenone D are neobisabolane-type sesquiter...

Embodiment 2

[0022] Example 2: Determination of protein tyrosine phosphatase 1B inhibitory activity

[0023] Using the method of molecular biology, construct the recombinant hGST-PTP1B-BL21 E. coli Human PTP1B engineering bacteria, the purified hGST-PTP1B recombinant protein can hydrolyze the substrate para The phospholipid bond of -Nitrophenyl Phosphate(pNPP), the obtained dephosphorylated product pNP has a strong light absorption at a wavelength of 405 nm, so the change of the light absorption at 405 nm can be directly detected to observe the change of the enzyme activity and the effect of the compound on the enzyme activity Inhibition situation; The initial screening selection of the compound concentration is 20 µ The percentage inhibition rate of PTP1B enzyme activity was investigated at g / ml, and the test results showed that the inhibition rates of beshanzueone C and beshanzuenone D were higher than 65% and 85% respectively; further determination of IC 50 Value: the sample is dis...

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Abstract

The invention belongs to the technical field of medicines, relates to a sesquiterpene spiro cyclical lactone compound as well as a preparation method and application thereof, and in particular to a preparation method of a sesquiterpene spiro cyclical lactone compound in Abies beshanzuensis and application of the compound as a protein-tyrosine-phosphatase 1B inhibitor. According to the method, the myrrh alkyl type sesquiterpene spiro cyclical lactone compound of formula (I) as shown in the specification is extracted and separated from barks of Abies beshanzuensis, biological activity tests show that the compound can remarkably inhibit protein-tyrosine-phosphatase 1B (PTP1B), and can be further prepared into medicines for preventing, retarding or treating diabetes, obesity, complications of diabetes and obesity and other diseases mediated by PTP1B.

Description

technical field [0001] The present invention relates to the technical field of medicine, and relates to a sesquiterpene spirolide compound and its preparation method and application, in particular to a preparation method of a novel sesquiterpene spirolide compound in Baishanzu fir and its use as protein tyramine Uses of acid phosphatase 1B inhibitors. The present invention is from Baishanzu fir ( Abies beshanzuensis The new bisabolane sesquiterpene spirolide compound extracted and separated from the bark of ), the biological activity test shows that this kind of compound can significantly inhibit protein tyrosine phosphatase 1B (PTP1B), and can be further used in the preparation of Drugs for preventing or treating diseases mediated by PTP1B, especially type II diabetes, obesity and their complications, or lead compounds of such drugs. Background technique [0002] The prior art discloses that protein tyrosine phosphatase (protein tyrosine phosphatase, PTP) is an enzyme fam...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D493/10A61P3/10A61P3/04
CPCC07D493/10
Inventor 胡金锋胡长玲熊娟
Owner FUDAN UNIV
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