Labdane diterpene derivatives as well as pharmaceutical composition and application thereof

The technology of a derivative and a composition is applied in the field of helichanoid diterpene derivatives and pharmaceutical compositions thereof, which can solve the problems of high toxicity and poor activity, and achieve the effect of eliminating interference.

Active Publication Date: 2019-08-02
YUNNAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Aiming at the technical problems of high toxicity and poor activity of inhibitors of the pronuclear factor-κB (NF-κB) signaling pathway in the prior art, it provides a helicanane-type...

Method used

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  • Labdane diterpene derivatives as well as pharmaceutical composition and application thereof
  • Labdane diterpene derivatives as well as pharmaceutical composition and application thereof
  • Labdane diterpene derivatives as well as pharmaceutical composition and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] Embodiment 1: the extraction method of helianthane type diterpene derivatives, the specific steps are as follows:

[0048] (1) Dry and pulverize the Leonurus branch;

[0049] (2) At room temperature, the motherwort sticks pulverized in step (1) were extracted 3 times with an aqueous ethanol solution with a volume fraction of 85%, each extraction was 24 hours, the ethanol extract was combined, filtered, and the filtrate was concentrated under reduced pressure get the extract;

[0050] (3) suspending the medicinal extract of step (2) in water, and extracting with sherwood oil, ethyl acetate and n-butanol successively to obtain sherwood oil extract, ethyl acetate extract and n-butanol extract;

[0051] (4) The ethyl acetate extract of step (3) is concentrated under reduced pressure to reclaim the solvent to obtain the ethyl acetate extract, then the ethyl acetate extract is dissolved in chloroform and adsorbed on silica gel, and the solvent chloroform is evaporated and gr...

Embodiment 2

[0125] Embodiment 2: The structural formula of embodiment 1 is the pharmacological experiment of I~XII helianthin type diterpene derivatives;

[0126] Cell culture: RAW264.7 cells (ATCC) gradually converge after growing for a period of time and cover the bottom of the bottle to form a monolayer cell membrane. When the coverage of adherent cells reaches 70-80% (about 1-2 days); Wash the cells once with PBS solution (Gibco fetal bovine serum), add 1 mL of trypsin (Gibco), digest at room temperature for 5 min, add 10 mL of DMEM complete medium containing 10% fetal bovine serum, blow off the cells, and culture in a cell incubator;

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PUM

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Abstract

The invention discloses labdane diterpene derivatives as well as a pharmaceutical composition and application thereof, and belongs to the technical field of medicine. In the invention, based on the isolation of the labdane diterpene derivatives, it is confirmed that any one of the labdane diterpene derivatives having structural formulas I-XII as shown in the specification can be used as an inhibitor of a nuclear factor-kappaB (NF-kappaB) signal pathway, and can inhibit the NF-kappaB signal pathway and treat NF-kappaB-mediated diseases.

Description

technical field [0001] The invention relates to a helianthene-type diterpene derivative, a pharmaceutical composition and application thereof, and belongs to the technical field of medicines. Background technique [0002] Inflammatory response is a common clinical pathological process, and it is also the primary response measure of the immune system to harmful stimuli. Its symptoms often manifest as tissue redness, swelling, hair, heat, and pain. In general, inflammation is beneficial: exudates and tissue hyperplasia caused by inflammation dilute harmful stimuli and limit their spread; leukocytes in exudates destroy inflammatory factors and remove necrotic tissue. On the contrary, inflammation is also potentially harmful, which is manifested as: the degeneration and necrosis of vital organs caused by inflammation will seriously affect their normal functions, and excessive inflammatory responses may cause shock or multiple organ dysfunction. [0003] There are many stimuli t...

Claims

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Application Information

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IPC IPC(8): C07D307/20C07D307/60C07D307/88C07D307/36C07C47/46C07C45/78C07C45/79C07C62/32C07C51/42C07C51/47A61K31/341A61K31/365A61K31/11A61K31/19A61P29/00A61P37/00A61P31/04A61P19/02A61P19/06
CPCC07D307/20C07D307/60C07D307/88C07D307/36C07C47/46C07C45/78C07C45/79C07C62/32C07C51/42C07C51/47A61P29/00A61P37/00A61P31/04A61P19/02A61P19/06C07C2602/28Y02A50/30
Inventor 肖伟烈张兴杰刘瑞雪张芮菡李晓莉秦华炎李一明
Owner YUNNAN UNIV
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