Application of bixanthone compound FLBG-1108 or its pharmaceutical salts in preparation of anti-cancer drugs

A technology of ketone compounds and anticancer drugs, which is applied to the application field of bixanthone compounds in the preparation of anti-lung cancer drugs, can solve the problems of rarity, toxicity, side effects, and gastrointestinal discomfort of patients, and achieve anti-cancer drugs. Clear cancer effect, less toxic and side effects, strong selective effect

Active Publication Date: 2014-07-16
SHENZHEN XIANHU BOTANICAL GARDEN ADMINISTRATION
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, among the many anticancer drugs, selective anticancer drugs are very rare
Moreover, the currently used broad-spectrum anticancer drugs have varying degrees of toxicity and side effects, causing patients to suffer from physical weakness, hair loss, vomiting, gastrointestinal discomfort, and neurological diseases during chemotherapy.

Method used

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  • Application of bixanthone compound FLBG-1108 or its pharmaceutical salts in preparation of anti-cancer drugs
  • Application of bixanthone compound FLBG-1108 or its pharmaceutical salts in preparation of anti-cancer drugs
  • Application of bixanthone compound FLBG-1108 or its pharmaceutical salts in preparation of anti-cancer drugs

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Antitumor activity of bixanthone compound FLBG-1108

[0030] The present invention adopts an in vitro cytotoxicity test to measure the antitumor activity of the compound FLBG-1108 by detecting the survival rate of human cancer cells cultured in vitro after being treated with different concentrations of the FLBG-1108 for 48 hours.

[0031] The selected tumor cell lines are: human non-small cell lung cancer H520, A549, H549, 1299, human liver cancer cell HepG2, human breast cancer cell MCF7, human prostate cancer cell PC3, LNcaP, DU145, human intestinal cancer cell SW480, HT-2P . The MTT method (reference Mosmann T. Rapid colorimetric assay for cellular growth and survival-application to proliferation and cytotoxicity assays. J Immunol Methods, 1983, 65(1-2), 55-63.) was used to determine the concentration of each tumor cell. The half-inhibitory concentration IC when the survival rate (or mortality rate) is 50% 50 . As normal cells, human kidney epidermal cells HKC-8 w...

Embodiment 2

[0040] Selective tumor suppressor effect of bixanthone compound FLBG-1108

[0041] The test method (MTT) is similar to Example 1, using the same human cancer cell line and normal renal epidermal cells, the administration concentration of FLBG-1108 is set at three concentration gradients of 3.125, 6.25, and 12.5 μM, and mixed with various cells After 48 h of culture, the viability of the cells was measured.

[0042] Further, three concentration gradients (3.125, 6.25, 12.5μM) were used to measure the selective inhibitory effect of FLBG-1108 on various cancer cells. The results are as follows: figure 1 shown. The diketone (bixanthone) compound FLBG-1108 showed inhibitory effects on the proliferation of human lung cancer cells H520, H549, 1299, and A549, but it showed obvious selective inhibitory effects on human lung cancer cells H520. The inhibitory rate was gradually enhanced with the increase of the concentration, and the inhibitory degree was obviously stronger than that o...

Embodiment 3

[0044] Dose-effect relationship of bixanthone compound FLBG-1108 in inhibiting the growth of lung cancer cell line H520

[0045] The method is similar to that of Example 1, and the human lung cancer cell line H520 is mainly used for determination, and the administration concentration is set at seven concentration gradients of 0.34, 0.78, 1.56, 3.12, 6.25, 12.5, and 25.0 μM, and the drug is mixed with the cancer cell H520 for 24 hours. After 48h and 72h, the survival rate of cancer cells was measured respectively.

[0046] The dose-effect relationship of FLBG-1108 inhibiting the growth of lung cancer cell H520 is as follows: figure 2 As shown, the results show that when the bixanthone compound FLBG-1108 acts on lung cancer cell H520 for 24 hours, its inhibitory activity is weak, but its inhibitory activity is significantly enhanced after 48 hours and 72 hours, showing a good concentration and time dependent effect. Especially after 48h and 72h of action, there is a good line...

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Abstract

The invention discloses an application of bixanthone compound FLBG-1108 or its pharmaceutical salts in the preparation of anti-cancer drugs. It is found in the invention through experiments that the bixanthone compound FLBG-1108 has an obvious inhibitory effect on the multiplication of human non-small cells lung cancer cells H520, A549, H549, 1299, a human breast cancer cell MCF7, human prostatic cancer cells PC3, LNcaP, and DU145 and human intestinal cancer cells SW480 and HT-2P. The multiplication of human lung cancer cells H520 can be inhibited selectively by the bixanthone compound FLBG-1108. The good time and the concentration dependence can be presented. The value of IC50 after 48 h action is 2.90 muM. The cytotoxicity is not expressed at this concentration on normal renal epidermal cells. Further, the bixanthone compound FLBG-1108 can effectively induce the apoptosis of lung cancer cells H520 and prevent the multiplication of cancer cells. Meanwhile, no toxicity will be presented. The bixanthone compound FLBG-1108 can specifically interdict the cell cycle of lung cancer cells H520 in S phase and can therefore inhibit the multiplication of cancer cells. Therefore, the bixanthone compound FLBG-1108 can be developed into a new candidate drug with an anti-cancer effect especially an anti-lung cancer effect.

Description

[0001] The patent application of the present invention is a patent application number: 201110333543.1, and the name of the invention is a divisional application for the application of bixanthone compound FLBG-1108 or its medicinal salt in the preparation of anticancer drugs. The filing date is: 2011 October 28. Technical field: [0002] The invention belongs to the field of pharmaceutical compounds, and in particular relates to the application of a natural plant-derived bixanthone compound FLBG-1108 or a medicinal salt thereof in the preparation of anticancer drugs, especially in the preparation of anti-lung cancer drugs. Background technique: [0003] In recent years, cancer has gradually risen to become the second major disease threatening human life. Among many cancers, the incidence of lung cancer has remained high and is increasing year by year. At present, most of the broad-spectrum anticancer drugs used clinically to treat lung cancer are cytotoxic drugs, such as cyc...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/352A61P35/00
Inventor 冯世秀陈涛
Owner SHENZHEN XIANHU BOTANICAL GARDEN ADMINISTRATION
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