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Cindinane-type sesquiterpenes, preparation method thereof, and use in pharmacy

A technology of sesquiterpenoids and compounds, applied in the field of juniperane-type sesquiterpenoids and their preparation, capable of solving problems such as chemical composition and pharmacological activity that have not been reported

Active Publication Date: 2021-02-26
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

At present, there is no report on its chemical composition and pharmacological activity.

Method used

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  • Cindinane-type sesquiterpenes, preparation method thereof, and use in pharmacy
  • Cindinane-type sesquiterpenes, preparation method thereof, and use in pharmacy
  • Cindinane-type sesquiterpenes, preparation method thereof, and use in pharmacy

Examples

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Embodiment 1

[0020] Embodiment 1 prepares juniper type sesquiterpene compound (manglietone B)

[0021] Take 1.2kg of the branches and leaves of Mangosteen, crush them and extract them by cold-soaking at room temperature with 95% ethanol for 3 times, combine the extracts and concentrate under reduced pressure to obtain 47.5 grams of extract. After the extract was dispersed with a methanol-water solution (15%, v / v), it was applied to an MCI resin column, and gradient eluted with methanol-water solution (from 50% to 100%, v / v). The fraction eluted with 60%-70% (v / v) methanol was further separated by silica gel column chromatography, and gradient eluted with petroleum ether-acetone (4:1-1:0, v / v) solution, 6 subfractions (Fr.A - Fr.F) were obtained. Subcomponent Fr.A was subjected to Sephadex LH-20 (eluent: methanol) and semi-preparative HPLC (MeOH / H 2 (0,60:40, v / v, 3.0mL / min) was further separated and purified to obtain compound manglietone B (1.1mg, t R =27.0min);

[0022] The obtained ...

Embodiment 2

[0024] Example 2: Determination of protein tyrosine phosphatase 1B inhibitory activity

[0025] Using the method of molecular biology, the hGST-PTP1B-BL21E.coli human PTP1B engineering bacteria with genetic recombination was constructed. The purified hGST-PTP1B recombinant protein can hydrolyze the phospholipid bond of the substrate para-Nitrophenyl Phosphate (pNPP). The phosphoric acid product pNP has a strong light absorption at a wavelength of 405nm, so the change of light absorption at 405nm can be directly detected to observe the change of enzyme activity and the inhibition of the compound to the enzyme activity; the concentration of the compound selected for primary screening is 20μg / ml When the percentage inhibition rate of PTP1B enzyme activity was investigated, the test results showed that the inhibition rate of manglietone B was higher than 60%; further determination of IC 50 Value: The sample is dissolved in DMSO to make a suitable concentration before use, 3-fold d...

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Abstract

The invention belongs to the field of traditional Chinese medicine preparation, and specifically relates to cadinane sesquiterpene compounds extracted and separated from branches and leaves of Manglietia aromatic Dandy. The preparation method provided by the invention uses technologies of infrared, ultraviolet, mass spectrum (high and low resolution), 1D / 2D nulcear magnetic resonance (NMR) and the like to confirm the structures of the cadinane sesquiterpene compounds, and uses a method of calculating circular dichroism (ECD) to confirm the absolute configurations of the cadinane sesquiterpene compounds. An in vitro inhibitory activity test is performed, and the result shows that the compounds have notable protein tyrosine phosphatase 1B(PTP1B) inhibitory activity, can be used as an inhibitor of the protein tyrosine phosphatase 1B and an insulin sensitizer, and can be further used for preparing medicines for preventing or curing the PTP1B mediated diseases, especially II-type diabetes, obesity and complications of the PTP1B mediated diseases, or lead compounds of the medicines.

Description

technical field [0001] The invention belongs to the field of traditional Chinese medicine pharmacy, and relates to a juniperane-type sesquiterpene compound, a preparation method thereof and a new application in preparation of medicines. Specifically, the invention relates to a juniperane-type sesquiterpene compound extracted and separated from branches and leaves of Manglietia aromatic Dandy and a preparation method thereof. The compound can be used as an inhibitor of protein tyrosine phosphatase 1B (PTP1B) and an insulin sensitizer, and can be further used to prepare drugs for preventing or treating diseases mediated by PTP1B, especially type II diabetes, obesity and its 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 family that regulates the phosphorylation level of intracellular protein tyrosine residues, and is closely related to cell ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C49/733C07C45/78A61P5/50A61P3/10A61P3/04
CPCC07B2200/07C07C45/78C07C49/733
Inventor 胡金锋王立军熊娟唐宇麻光磊
Owner FUDAN UNIV
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