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Rosin type diterpene derivative as well as preparation method and application thereof

A technology of derivatives and diterpenes, applied in the field of rosin-type diterpene derivatives and their preparation

Active Publication Date: 2015-04-29
SHANGHAI UNIV OF T C M
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there is no report on the treatment of abnormal lipid metabolism by the extract of stinky peony and its chemical components

Method used

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  • Rosin type diterpene derivative as well as preparation method and application thereof
  • Rosin type diterpene derivative as well as preparation method and application thereof
  • Rosin type diterpene derivative as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Take 1 kg of stinky peony root, crush it and add it to 3L of ethanol with a volume fraction of 95% for reflux extraction, reflux extraction twice, each time for 2 hours, filter and combine the extracts, recover the ethanol under reduced pressure, and suspend the extract in water , extract the suspension with petroleum ether (60-90°C) for 5 times, combine the petroleum ether layers and recover the solvent under reduced pressure to obtain petroleum ether fractions; pass the obtained petroleum ether fractions through silica gel column chromatography, and use a volume ratio of 20 :1, 10:1, 8.5:1.5, 7:3 and 1:1 mixture of petroleum ether and ethyl acetate for gradient elution, TLC inspection, segmented collection, and 5 parts (Fr. 1~Fr.5), wherein, Fr.2 and Fr.4 were firstly subjected to Sephadex LH-20 column chromatography, eluted with a mixture of dichloromethane and methanol at a volume ratio of 1:1, and then passed through a silica gel column Chromatography, using a mixt...

Embodiment 2

[0029] Take 2kg of the whole plant of Smelly Peony, crush it, add 6L ethanol with a volume fraction of 95% for ultrasonic extraction, extract 3 times, each time for 30 minutes, filter and combine the extracts, recover the ethanol under reduced pressure, and suspend the extract in water; Extract the suspension with petroleum ether (60-90°C) for 5 times, combine the petroleum ether layers and recover the solvent under reduced pressure to obtain petroleum ether fractions; pass the obtained petroleum ether fractions through silica gel column chromatography, and sequentially use a volume ratio of 20:1 , 10:1, 8:2, and 1:1 mixture of petroleum ether and ethyl acetate for gradient elution, thin-layer chromatography inspection, segmental collection of diterpene-containing fractions to obtain 4 parts (Fr .1~Fr.4); Among them, Fr.2 and Fr.3 were firstly subjected to Sephadex LH-20 column chromatography, eluted with a mixture of dichloromethane and methanol at a volume ratio of 1:1, and t...

Embodiment 3

[0052] The sterol regulatory element binding protein (SREBP) signal transduction pathway is one of the main pathways of lipid metabolism signal transduction. As a powerful activator, SREBP can directly activate more than 30 pathways involved in the synthesis and uptake of fatty acids, triglycerides and phospholipids. gene expression. Therefore, inhibiting the expression of SREBP can achieve the purpose of lowering blood lipids. In the present invention, the inhibitory effect of compounds 1-6 on SREBP expression is tested to reflect its lipid-lowering efficacy.

[0053] The pSRE-Luciferase plasmid and pEGFP-N1 plasmid (Invitrogen) were transferred into Huh-7 cell line at a ratio of 5:1 to obtain Huh-7 / SRE-Luc cell line. Huh-7 / SRE-Luc cells in good growth condition were taken for experiments, and the cell concentration was adjusted to about 10000 / well. Liquid was added to the 96 wells with a pipette, and 200 μL of cell solution was injected into each well for cell culture for ...

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Abstract

The invention provides a rosin type diterpene derivative as well as a preparation method and application thereof. The derivative is a compound with structure shown in a general formula I, II or III which is shown in the description or an addition salt formed by the compound and an acid or an alkali which is acceptable in pharmacy, wherein R1 is hydrogen, hydroxyl or alkoxy or acyloxy of C1-C3; R2 is saturated or unsaturated alkyl of C1-C3, oxygen-containing alkyl of C1-C3 or acid of C1-C3 and ester or salt of the acid; the derivative is prepared in the way that Clerodendrum bungei as a labiatae clerodendrum plant is used as a raw material and subjected to solvent extraction, and column chromatography separation and purification. According to the invention, on the basis that the rosin type diterpene derivative is obtained through separation, the fact that the compound has the function of suppressing the expression of SREBP is confirmed, a lead compound is provided for developing medicines capable of treating dyslipidemia, and important significance on the development of new application of natural products and botanical drugs is achieved.

Description

technical field [0001] The invention relates to a rosin-type diterpene derivative, a preparation method and application thereof, and belongs to the technical field of medicine. Background technique [0002] Clerodendrum bungei Steud. is a plant of the genus Clerodendrum bungei Steud. Alias: Stinky Babao, Dahongpao (Plant Test of Botanical Name), Dwarf Tongzi (Classification of Herbs), Stinky Indus (Guangxi Medicinal Plant List), Fengxiancao (Hunan Drug Records), Smelly Yellow Root, Smelly Jasmine (Lushan Chinese herbal medicine). The roots, stems, and leaves are used as medicine, and are flat in nature, pungent in taste, and non-toxic. It has the effects of expelling wind and detoxification, reducing swelling and relieving pain. It is mainly used to treat carbuncle, hemorrhoids, high blood pressure, rheumatic arthralgia, and uterine prolapse. The main chemical constituents of stink peony include diterpenes, phenylethanol glycosides, flavonoids, organic acids, etc. These ...

Claims

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Application Information

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IPC IPC(8): C07D307/77A61P3/00A61P3/04A61P3/06A61P9/10
CPCC07D307/77
Inventor 王峥涛刘青丁丽丽宋宝亮祁萌杨莉侴桂新
Owner SHANGHAI UNIV OF T C M
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