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Application of bixanthone compound FLBG-1108 or its medicinal salt in preparing anticancer medicaments

A technology of FLBG-1108 and anti-cancer drugs, which is applied in drug combinations, medical preparations containing active ingredients, anti-tumor drugs, etc., can solve problems such as toxicity, side effects, rare anti-cancer drugs, and gastrointestinal discomfort of patients, and achieve toxicity Small side effects, clear anticancer effect, strong selective effect

Inactive Publication Date: 2012-05-09
SHENZHEN XIANHU BOTANICAL GARDEN ADMINISTRATION
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

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 medicinal salt in preparing anticancer medicaments
  • Application of bixanthone compound FLBG-1108 or its medicinal salt in preparing anticancer medicaments
  • Application of bixanthone compound FLBG-1108 or its medicinal salt in preparing anticancer medicaments

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Antitumor activity of bixanthone compound FLBG-1108

[0028] 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.

[0029] 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 measure the tumor cell The half-inhibitory concentration IC when the survival rate (or death rate) is 50% 50 . As normal cells, human kidney epidermal cells HKC-8 were used as the control.

[00...

Embodiment 2

[0038] Selective tumor suppressor effect of bixanthone compound FLBG-1108

[0039] 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.

[0040] Further use three concentration gradients (3.125, 6.25, 12.5μM) 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 effect on the proliferation of human lung cancer cells H520, H549, 1299 and A549, but showed obvious selective inhibitory effect on human lung cancer cell H520. The inhibitory rate was gradually enhanced with the increase of the concentration, and the inhibitory degree was obviously stronger than that of other cancer ...

Embodiment 3

[0042] Dose-effect relationship of bixanthone compound FLBG-1108 in inhibiting the growth of lung cancer cell line H520

[0043] The method is similar to that of Example 1. 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. 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.

[0044] 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 cells H520 for 24 hours, its inhibitory activity is weak, but its inhibitory activity is significantly enhanced after acting for 48 hours and 72 hours, showing a good concentration and time. Dependency effect. Especially after 48h and 72h of action, there is a goo...

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Abstract

The invention discloses application of a bixanthone compound FLBG-1108 or its medicinal salt in preparing anticancer medicaments. The invention, by means of experiments, finds that the bixanthone compound FLBG-1108 has an obvious inhibition effect on propagation of human non-small cell lung cancer H520, A549, H549, 1299, human breast cancer cell MCF7, human prostatic cancer cell PC3, LNcaP, DU145, as well as human intestinal cancer cell SW480 and HT-2P, can selectively inhibit the propagation of the human lung cancer cell H520, and presents good time and concentration dependence. After 48h of action, the IC50 value is 2.90 micrometers, which shows no cytotoxicity to a normal kidney epidermal cell. Further, the bixanthone compound FLBG-1108 is found to play an effective role in inducing apoptosis of the lung cancer cell H520, preventing propagation of cancer cells but showing no toxicity, and can specifically block the cell cycle of the lung cancer cell H520 in S stage, thus inhibiting the propagation of cancer cells. Therefore, the bixanthone compound FLBG-1108 can be developed into novel candidate medicaments with an anticancer effect, especially an anti-lung cancer effect.

Description

Technical field: [0001] 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: [0002] 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 cyclophosphamide, cisplatin, mitomycin, and podophyllotoxin derivatives that affect the DNA structure and function of cancer cells. etc.; anthracyclines, such as doxorubicin, that interfere with the transcription process of cancer cell RNA and prevent RNA synthesis; and plant-derived anticancer drugs that inhibit the...

Claims

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Application Information

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IPC IPC(8): A61K31/352A61P35/00A61P11/00
Inventor 冯世秀陈涛
Owner SHENZHEN XIANHU BOTANICAL GARDEN ADMINISTRATION
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