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Diterpenoid compounds in euphorbia pekinensis, medicine composition thereof, and application of same in pharmacy

A technology of compounds and diterpenoids, applied in the direction of drug combination, separation/purification of carboxylic acid esters, medical preparations containing active ingredients, etc.

Inactive Publication Date: 2014-07-23
KUNMING INST OF BOTANY - CHINESE ACAD OF SCI +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there is no report in the prior art that the above-mentioned 3 ingenane-type and 1 tiglicane-type diterpenoids can be extracted from Euphorbia plants, which have obvious anti-tumor cell proliferation activity.

Method used

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  • Diterpenoid compounds in euphorbia pekinensis, medicine composition thereof, and application of same in pharmacy
  • Diterpenoid compounds in euphorbia pekinensis, medicine composition thereof, and application of same in pharmacy
  • Diterpenoid compounds in euphorbia pekinensis, medicine composition thereof, and application of same in pharmacy

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Preparation of diterpenoids:

[0028] The dried whole plant of Euphorbia euphorbia (1.5kg) was pulverized, cold-soaked in 90% ethanol (4×6L) at room temperature for 24 hours, filtered, the extracts were combined, and the ethanol was recovered under reduced pressure to obtain a crude extract. Ester was extracted 3 times to obtain 103 g of ethyl acetate extract, which was eluted with polyamide and MCI series methanol-water (20:80 to 100:0) gradient, and the same fractions were combined to obtain 5 fractions (F1-F5) . Take F4 and get 4 small fractions (F4a-F4d) by gradient elution of silica gel column chloroform-ethyl acetate (10:1 to 3:2), and take F4c and go through Sephadex LH-20 column chromatography (chloroform:methanol=1:1) After purification, compound 1 (1.3 mg) was semi-prepared by HPLC (methanol:water=82:18). Take F5 through silica gel column petroleum ether-ethyl acetate (10:1 to 2:3) gradient elution to obtain 3 small fractions (F5a-F5c), take F5a and semi-pre...

Embodiment 2

[0038] The pharmacological test of diterpenoid compound (1-4) of the present invention:

[0039] Experimental materials: DMEM medium, newborn calf serum, trypsin, MTT, DMSO, human lung adenocarcinoma cell line A549, liver cancer cell line Hep G2, human cervical cancer cell line Hela, CO 2 Incubator, ultra-clean bench, microplate reader, inverted microscope, cell culture flask, 96-well cell culture plate.

[0040] experimental method:

[0041] 1. Medium preparation: GIBCO DMEM liquid medium, refrigerated at 4°C for later use.

[0042] 2. Inactivation of calf serum: 200mL super newborn calf serum, take it out of the -40℃ refrigerator and thaw at room temperature, and bathe in 56℃ water for 30min. After cooling, aliquot them into 15mL centrifuge tubes and freeze them in a -40°C refrigerator for later use.

[0043] 3. Complete culture medium: 95 mL of DMEM medium, add 5 mL of inactivated newborn calf serum, and mix well.

[0044] 4. Sample stock solution: Accurately measure 10.0...

Embodiment 3

[0063] Preparation of Injections

[0064] Prepare diterpene compound earlier by the method for embodiment 1, mix it with 20% polyoxyethylene ether castor oil, dissolve into Suspension injection made in water.

[0065] It is also possible to dissolve the diterpene compounds prepared by the method of Example 1 with a small amount of DMSO, add water for injection as usual, perform fine filtration, potting, and sterilize to make an injection.

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Abstract

The invention relates to a novel ingenane-type diterpenoid (1) and a tiglic alkane-type diterpenoid (2) obtained by separating from euphorbia stracheyi, and two ingenane-type diterpenoids (3, 4) obtained by separating from ewuphorbia wallichii, as well as a preparation method of the same, and an application of the ingenane-type diterpenoid (1) and a tiglic alkane-type diterpenoid (2) in preparation for anti-tumour medicines. In-vitro anti-tumour active screening indicates that the compounds disclosed by the invention are obvious in the effect of inhibiting tumour cell proliferative activity, and are capable of being combined with pharmaceutically acceptable carriers to prepare clinically acceptable medicine dosage forms for treating various cancers. The invention provides lead compounds for researching novel anti-tumour medicines, and has an important value in development and utilization for the resources of medicinal plants.

Description

technical field [0001] The invention belongs to the technical field of medicines, and relates to three ingenane-type diterpenes and one tigalane-type diterpenoids isolated from Euphorbia alpine and Euphorbia euphorbia and their preparation methods and applications. The above-mentioned compound has obvious inhibitory effect on tumor cell lines, and can be used as a lead compound for developing new anti-tumor drugs, and can also be used as drugs for developing and treating various common clinical multiple cancers. technical background [0002] Tumor is a common and frequently-occurring disease, among which malignant tumor is the most serious disease that endangers human health. In recent years, the effects of surgical resection and radiotherapy have stagnated, so more and more people pay more and more attention to chemical drug therapy that acts on the whole body. However, while chemotherapeutic drugs kill cancer cells, they also produce toxic and side effects on normal cells...

Claims

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Application Information

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IPC IPC(8): C07C69/587C07C69/33C07C69/30C07C67/48A61K31/23A61K31/231A61P35/00
CPCC07C67/48C07C69/33C07C69/587C07C2603/86C07C2603/98
Inventor 杨大松李晓莉杨永平彭维兵刘可春
Owner KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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