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Application of iridoid compound to preparation of ovarian cancer resistance medicament

A technology of iridoids and iridoids, which is applied in the field of application of iridoids in the preparation of anti-ovarian cancer drugs, and can solve the problems of insufficient research and chemical composition research

Inactive Publication Date: 2012-06-20
SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Although the research on spider incense has reached a certain scale, the research on its chemical components is still not enough, especially the research on iridoids is not thorough enough.

Method used

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  • Application of iridoid compound to preparation of ovarian cancer resistance medicament
  • Application of iridoid compound to preparation of ovarian cancer resistance medicament
  • Application of iridoid compound to preparation of ovarian cancer resistance medicament

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] The preparation of embodiment 1 isovaleryl dihydrovalerenin and valerian triester J

[0026] 8.5Kg of the dried Herba chinensis was crushed and extracted by percolation with 95% ethanol for 4 days to obtain 100 L of extract. The extract was concentrated under reduced pressure into an extract, suspended in water, and extracted 5 times with ethyl acetate, 3 L each time. After the solvent was recovered under reduced pressure, the ethyl acetate part was 420 g, and the water phase part was 315 g. The ethyl acetate part was separated by normal-phase silica gel (1500g) column chromatography, and gradient elution was carried out with petroleum ether-acetone (100:0-0:100), and the eluent was detected by thin-layer chromatography, and the eluents of similar composition were combined , and the solvent was recovered to obtain 1-×10 (the eluate was divided into 10 elution fractions according to the different spots detected by the thin layer). The 4th elution fraction was taken and ...

Embodiment 2

[0034] Example 2 The cytotoxic effect of isovaleryl dihydrovalerenin and valerian triester J on ovarian cancer cells

[0035] Isovaleryl dihydrovalerenin and valerian triester J compared the toxic killing effects of ovarian cancer cells A2780 (p53 wild type), OVCAR-3 (p53 mutant) and ovarian normal cells IOSE144.

[0036] Isovaleryl dihydrovalerenin and valerian triester J experimental drug treatment time is 48h; drug concentration is set to 0, 1, 5, 10, 50, 100 μ M; drug dissolved in DMSO (1000 ×); drug treatment When the content of DMSO is less than 0.1%.

[0037] The results of the study are shown in Table 3. Isovaleryl dihydrovalerian and valerian triester J The toxic killing effect of IOSE144 on ovarian normal cells is less than that of ovarian cancer cell lines, indicating that isovaleryl dihydrovalerian and valerian triester J has selective toxic killing effect on ovarian cancer cells.

[0038] Table 3 IC50 values ​​of isovaleryl dihydrovalerenin and valerian trieste...

Embodiment 3

[0040] Example 3 Effects of isovaleryl dihydrovalerian and valerian triester J on the proliferation of ovarian cancer cell line A2780, OVCAR-3 and normal ovarian cell line IOSE144

[0041]Isovaleryl dihydrovalerenin and valerian triester J have selective toxic and killing effects on ovarian cancer cells (compared to normal ovarian cell lines). The study explored the effects of these two compounds on ovarian cancer cell lines A2780, 3 and the effect on the proliferation of normal ovarian cell line IOSE144.

[0042] Experimental time gradient: 0, 24, 48, 72 hours; isovaleryl dihydrovalerian and valerian triester J experimental drug concentration gradient settings: 0, 1, 5, 10, 25, 50, 100 μM; drug Soluble in DMSO (1000×); the content of DMSO is less than 0.1% when the drug is treated.

[0043] Experimental method: MTT assay; cell viability was detected every 24 hours.

[0044] The results of the study showed that isovaleryl dihydrovalerian and valerian triester J can significa...

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Abstract

The invention provides the application of iridoid compound to the preparation of ovarian cancer resistance medicament. The iridoid compound is isovaleric acid base dihydro valerian element or isovaleric acid base dihydro valepotriate J which has the following structural formula. The experiments on the toxic and killing effect of the isovaleric acid base dihydro valerian element or the isovaleric acid base dihydro valepotriate J on the p 53 wild ovarian cancer cells A2780, the p53 mutated OVCAR-3 cells and the normal ovarian cells IOSE144 show that the isovaleric acid base dihydro valerian element or the isovaleric acid base dihydro valepotriate J has the selective toxic and killing effect on the ovarian cancer cells and can inhibit the proliferation of ovarian cancer cells and kill the ovarian cancer cells. The iridoid compound can be used as the active component to prepare the ovarian cancer resistance medicament. The invention provides the novel ovarian cancer treatment medicament for the clinical treatment of the ovarian cancer and brings the joyous news to the patients with the ovarian cancer. The iridoid compound has higher application value.

Description

technical field [0001] The invention relates to medicines, in particular to the application of iridoid compounds in the preparation of anti-ovarian cancer medicines. Background technique [0002] Ovarian cancer is one of the common tumors of female reproductive organs. Ovarian cancer is the leading cause of death among various gynecological tumors, posing a serious threat to women's lives, and its five-year survival rate is only 25% to 30%. According to epidemiological statistics, ovarian cancer is more likely to occur in women with ovarian insufficiency, such as delayed menarche, early menopause, dysmenorrhea, celibacy, infertility, frequent induced abortion, and people with family history. Since the ovary is located in the deep part of the pelvic cavity, there may be no or mild symptoms in the early stage of the disease. Because ovarian cancer is asymptomatic in the early clinical stage, it is very difficult to distinguish its tissue type and benign from malignant. Only ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/352A61P35/00
Inventor 张卫东苏娟林生单磊柳润辉李慧梁徐希科
Owner SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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