Barrigenol-like triterpenoids, and preparation method and pharmaceutical application thereof

A kind of technology of triterpene compound, uricol, applied in the field of medicine

Inactive Publication Date: 2018-07-31
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there is no report on its chemical composition. If we can collect a few samples of the red-skin rough fruit tea plant for a systematic study on the chemical composition, it will actively promote the protection and utilization of this rare plant resource to serve human beings.

Method used

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  • Barrigenol-like triterpenoids, and preparation method and pharmaceutical application thereof
  • Barrigenol-like triterpenoids, and preparation method and pharmaceutical application thereof
  • Barrigenol-like triterpenoids, and preparation method and pharmaceutical application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Embodiment 1: prepare described triterpenoid compound

[0028] 3.5 kg of red bark rough fruit tea ( Camellia crapnelliana ) branches and leaves were dried and pulverized, extracted 6 times with 6 L of 90% methanol at room temperature, each time for 24 hours, combined the extracts, concentrated and evaporated methanol to obtain a total extract of 237 g. After the total extract was dispersed with 1.2L of water, it was extracted three times with equal volumes of petroleum ether, ethyl acetate, and n-butanol, respectively, to obtain 2 g of petroleum ether, 13.1 g of ethyl acetate, and 99.3 g of n-butanol. Water 4 components. The ethyl acetate fraction (13.1 mg) was eluted through the MCI column with a gradient of methanol-water (50: 50 - 70: 30 - 85: 15 - 100: 0, v / v), and were combined into 7 groups according to the color development of TLC Divided Fr.1 - Fr.7. Fr.6 (3.1 g) was packed on a silica gel column and eluted with PE-EtOAc gradient (10:1 - 5:1 -1:1, v / v) to obt...

Embodiment 2

[0042] Example 2: Determination of protein tyrosine phosphatase 1B inhibitory activity

[0043] 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 -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 of PTP1B enzyme activity when the concentration of the compound was selected as 100 μM for primary screening, the test results showed that the inhibition rates of compounds 1-4 were 94.14%, 94.24%, 95.67% and 89.05% respectively ; Further determination of IC 50 Value: the sample is dissolved in DMSO to make a suitable concentra...

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Abstract

The invention relates to barrigenol-like (polyhydroxy-substituted oleanane) triterpenoids separated from the branches and leaves of Camellia crapnelliana Tutch, Camellia, Theaceae, a preparation method thereof, and application of the barrigenol-like triterpenoids as protein tyrosine phosphatase 1B (PTP1B) inhibitors to preparation of drugs, especially to preparation of drugs used for treating diabetes, obesity and other PTP1B-mediated diseases. The general structural formula of the barrigenol-like triterpenoids of the invention is as shown in the specification. In the formula, R1 and R2 are hydroxyl groups or acetoxy groups, and R3 and R4 hydroxyl groups, acetoxy groups or angeloyl groups.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to red skin rough fruit tea ( Camellia crapnelliana The new pharmaceutical application of the eumantyl alcohol triterpenoid compound extracted and separated from the branches and leaves of ) specifically relates to the ermanthyl alcohol triterpenoid compound and its preparation method and its use in the preparation of medicines for preventing or treating diseases mediated by PTP1B. Biological activity tests show that this type of compound can significantly inhibit protein tyrosine phosphatase 1B (PTP1B), 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 protein ...

Claims

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Application Information

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IPC IPC(8): C07J63/00A61P3/04A61P3/10
CPCC07J63/008
Inventor 胡金锋熊娟万江
Owner FUDAN UNIV
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