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Guaiane-type sesquiterpenes compound, preparation method and application thereof

A technology of guaiacol and sesquiterpenes, applied in the field of phytochemistry, can solve problems such as unreported

Active Publication Date: 2016-06-15
HAINAN NORMAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The guaiac-type sesquiterpenoids isolated from Melaleuca sinensis have not been reported, nor have there been reports on the application of such compounds in inhibiting the proliferation of rheumatoid arthritis synoviocytes

Method used

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  • Guaiane-type sesquiterpenes compound, preparation method and application thereof
  • Guaiane-type sesquiterpenes compound, preparation method and application thereof
  • Guaiane-type sesquiterpenes compound, preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Embodiment 1: Preparation of sesquiterpenoids.

[0028] 10Kg of the dried stems of S. mellifera were routinely extracted with 75% v / v ethanol 3 times for 7 days each time to obtain an extract, which was concentrated under reduced pressure into a paste to obtain 1200 g of S. mellifera extract. The extract was diluted into a suspension with distilled water (3 L), extracted with petroleum ether (3 L x 3 times) and ethyl acetate (3 L x 3 times) successively, and the ethyl acetate extract was concentrated into an extract (about 250 g), Carry out silica gel column chromatography, use petroleum ether-ethyl acetate mixed solvent (100:0-0:100, V / V) and ethyl acetate-methanol (100:0-0:100, V / V) according to polarity Perform silica gel column chromatography incrementally, and collect fractions of about 400 mL each time. Through TLC detection, the combined similar fractions were divided into 8 components, namely Fr.1-8. Fr.3 Use 200-300 mesh silica gel on the column, use ethyl ac...

Embodiment 2

[0033] Embodiment 2: pharmacological activity experiment

[0034] Experimental Materials

[0035] Cells: synoviocytes (primary rat synoviocytes).

[0036] Cell culture medium: primary rat synoviocyte culture medium.

[0037] Reagent: thiazolium blue (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazoliumbromide, MTT, manufactured by Sigma). Lactate dehydrogenase (lactatedehydrogenase, LDH) kit (purchased from Biyuntian Company). Methotrexate (methotrexate, MTX, Shanghai Xinyi Pharmaceutical Co., Ltd., batch number 20140307).

[0038] 1.4 Instrument: 96-well cell culture plate; infinite200Pro multifunctional microplate reader.

[0039] experimental method

[0040] Determination of the Inhibitory Effect of Drugs on Synoviocytes by MTT Method

[0041] Synoviocytes in the logarithmic phase were inoculated into 96-well culture plates (1×10 4 cells / well), which were set as blank group (no drug administration), methotrexate group (administration of 1 μg / mL methotrexate), drug tr...

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PUM

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Abstract

The invention discloses a guaiane-type sesquiterpenes compound, of which the structural formula is represented as follows, and also discloses a preparation method of the compound and an application thereof in preparation of an anti-rheumatoid arthritis medicines. The invention, for the first time, develops the activity of the guaiane-type sesquiterpenes compound in inhibition on rheumatoid arthritis synovial cell proliferation. The compound can be used for preparing the anti-rheumatoid arthritis medicines.

Description

technical field [0001] The invention relates to the technical field of phytochemistry, in particular to a guaiac-type sesquiterpene compound and a preparation method and application thereof. Background technique [0002] Fissistigma oldhamii (Hemsl.) Merr., also known as Fissistigma oldhamii (Hemsl.) Merr., is a plant of the genus Fissistigma oldhamii (Annonaceae) in the family Annonaceae. The plant can be used as medicine, the stems and leaves can cure fractures and edema, and the whole plant can treat rheumatic bone pain, numbness of hands and feet, etc. The guaiac-type sesquiterpenoids isolated from Melaleuca japonica have not been reported, nor have there been reports on the application of such compounds in inhibiting the proliferation of rheumatoid arthritis synoviocytes. Contents of the invention [0003] The technical problem to be solved by the present invention is to provide a guaiac-type sesquiterpene compound extracted and separated from melamine. [0004] The...

Claims

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Application Information

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IPC IPC(8): C07C49/733C07C45/78A61K31/122A61P19/02
CPCA61K31/122C07C45/78C07C49/733
Inventor 陈光英周学明韩长日宋小平徐伟郑彩娟
Owner HAINAN NORMAL UNIVERSITY
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