Application of cycloaltin-type triterpene compounds in the preparation of anti-lung cancer drugs

A cycloaltin-type, anti-lung cancer drug technology, applied in the direction of active ingredients of hydroxyl compounds, drug combinations, anti-tumor drugs, etc., to achieve the effect of inhibiting proliferation and rich in plant sources

Active Publication Date: 2016-08-24
DALIAN OCEAN UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] However, so far there has been no report that (23Z)-9,19-cycloartin-23-ene-3α,25-diol, a cycloaltin-type tetracyclic triterpenoid, has anti-lung cancer activity

Method used

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  • Application of cycloaltin-type triterpene compounds in the preparation of anti-lung cancer drugs
  • Application of cycloaltin-type triterpene compounds in the preparation of anti-lung cancer drugs
  • Application of cycloaltin-type triterpene compounds in the preparation of anti-lung cancer drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0012] a. Take the dried and pulverized aerial part of the whole leaf of Indigo spinosa, soak it in 6-10 times the amount of ethanol or methanol with a volume fraction of 50-100%, and then heat and reflux for extraction. The extraction time is 2-3 hours each time, and the extraction times are 2-2 3 times, combined extracts, decompressed recovery extracts to alcohol concentration lower than 5%;

[0013] b. extract the resulting extract through petroleum ether, n-hexane or cyclohexane for 2 to 5 times, the volume ratio of the extraction solvent to the extract is 1 to 3: 3 to 1, combine the extracts, and recover the solvent to obtain the extract;

[0014] c. The obtained extract was separated by silica gel column chromatography, and the mixed solvent of petroleum ether and ethyl acetate was used for gradient elution, and the eluted fraction with a volume ratio of petroleum ether and ethyl acetate of 100:6~8 was collected;

[0015] d. The solvent was distilled off under reduced pr...

Embodiment 2

[0028]The cycloaltin-type triterpenoid compound (23Z)-9,19-cycloaltin-23-ene-3α,25-diol isolated in Example 1 was determined by the above-mentioned MTT method for the effect of the compound on the lung cancer cell line H1944 Inhibition experiment steps were carried out, and the results showed that its inhibitory effect on lung cancer cell line H1944 IC 50 The value is 7.8 μmol / L.

Embodiment 3

[0030] The cycloaltin-type triterpenoid compound (23Z)-9,19-cycloaltin-23-ene-3α,25-diol isolated in Example 1 was determined by the above-mentioned MTT method for the effect of the compound on lung cancer cell line H292 Inhibition experiment steps were carried out to measure its inhibitory effect on the proliferation of lung cancer cell line H292 IC 50 The value is 4.9 μmol / L.

[0031] According to the above-mentioned MTT method, the compound is tested against the lung cancer cell line inhibition test steps, and its IC for inhibiting the proliferation of the lung cancer cell line H358 is measured. 50 The value is 8.7 μmol / L.

[0032] The inhibitory effects of the compound (23Z)-9,19-cycloaltin-23-ene-3α,25-diol obtained in the examples of the present invention on four lung cancer cell lines are as follows: image 3 shown.

[0033] The compound is (23Z)-9,19-cycloaltin-23-ene-3α,25-diol, which can be mixed with pharmaceutically acceptable drug excipients to form various for...

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Abstract

The invention discloses an application of cycloartane triterpenoid (23Z)-9,19-cycloartane-23-alkene-3alpha, 25-glycol in preparation of an anti-lung cancer medicine. The plant source of cycloartane triterpenoid is abundant; when the effective in vitro acting concentration of the prepared cycloartane triterpenoid (23Z)-9,19-cycloartane-23-alkene-3alpha, 25-glycol for a lung cancer cell strain is 5-20mu mol / L, the cycloartane triterpenoid has obvious proliferation inhibition action on the lung cancer cell strains H1299, H1944, H292 and H358 and the IC50 values are respectively 2.6mu mol / L, 7.8mu mol / L, 4.9mu mol / L and 8.7mu mol / L. The cycloartane triterpenoid can be applied to preparation of the anti-lung cancer medicine.

Description

technical field [0001] The invention relates to a new application of a cycloaltin-type triterpene compound, in particular to an application of a cycloaltin-type triterpene compound in the preparation of anti-lung cancer drugs. Background technique [0002] At present, the anti-tumor mechanism of Chinese herbal medicine is mainly through inducing tumor cell differentiation, inducing tumor cell apoptosis, inhibiting tumor cell proliferation, inhibiting tumor cell telomere enzyme activity, reversing tumor cell drug resistance, and improving the sensitivity of other anti-tumor drugs. Anti-tumor effects of traditional Chinese medicines, blocking tumor cell migration pathways, inhibiting tumor angiogenesis, and improving the body's immune level, etc. Among the antineoplastic drugs commonly used in clinical practice, the drugs directly derived from natural products or obtained through structural modification mainly include paclitaxel, hydroxycamptothecin, matrine, cantharidin, vinb...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/047A61P35/00
CPCA61K31/575
Inventor 谭成玉孔亮李敏晶李伟孟繁桐
Owner DALIAN OCEAN UNIV
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