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Meletin with cell apoptosis inductive effect and metallic complex of glycoside compounds thereof

A technology of metal complexes and apoptosis induction, applied in the field of drugs for the treatment of tumors, can solve the problems of no specific way to kill tumor cells, no clinical application value, and large toxic and side effects of compounds

Inactive Publication Date: 2008-07-16
CHONGQING UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Published by Zhou J. et al. (Transition Metal Chemistry 26:57-63, 2001; Journal of Inorganic Biochemistry 83:41-48, 2001) and Ferrer E.G et al. (Journal of Biology Inorganic Chemistry 11:791-801, 2006) The metal complexes of quercetin with Cu(II), Mn(II), Zn(II), Pb(II), La(III), Eu(III), Gd(III), V(IV) are described Drugs can inhibit the proliferation of liver cancer cells, but these documents do not provide specific ways for them to kill tumor cells
If only the proliferation of liver cancer cells is inhibited, the compound may have high toxicity and side effects, which has no clinical application value, thus limiting the development of quercetin metal complexes as anticancer drugs

Method used

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  • Meletin with cell apoptosis inductive effect and metallic complex of glycoside compounds thereof
  • Meletin with cell apoptosis inductive effect and metallic complex of glycoside compounds thereof
  • Meletin with cell apoptosis inductive effect and metallic complex of glycoside compounds thereof

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Experimental program
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Effect test

Embodiment 1

[0028] The synthesis of embodiment 1 quercetin metal complex

[0029] In 50ml methanol or ethanol at 30-80℃, dissolve 2mmol quercetin, add appropriate amount of divalent metal nitrates such as V, Cr, Mn, Fe, Co, Ni, Cu, Zn, Mg, Ca, Pb, chlorine Compounds, sulfates or acetates; Al, Fe, La, Ce, Pr, Nd, Sm, Eu, Gd, Tb, Dy, Ho, Er, Tm, Yb, Lu and other trivalent metal nitrates, chlorides, Sulphate or acetate (the molar ratio of metal salt to quercetin is 5:1~1:5), heated and stirred, adjusted to pH=3.0~10.0, heated and refluxed for 4~30 hours, left at room temperature for 8~30 hours , filtered, washed the precipitate three times with aqueous methanol, and dried in vacuo to obtain the product.

[0030] The synthesis method of other quercetins and their glycoside metal complexes is basically the same as the above method.

Embodiment 2

[0031] Example 2 Inhibition of tumor cell growth by quercetin metal complexes

[0032] Liver cancer cells SMMC-7721, HepG2 and lung adenocarcinoma cells A549 in the logarithmic growth phase were digested and separated by trypsin-EDTA, and the cell density was adjusted to 4.0×10 with RPMI-1640 culture medium containing 10% newborn calf serum. 4 cells / mL, add 150 μL per well into a 96-well culture plate, place in an incubator at 37°C, 5% CO 2 Cultivate for 24h. The cells were synchronized according to the method of serum starvation, and a blank group, a normal control group, and a drug-dosing experimental group were set up (except for the blank group without adding cells and drugs, and the normal control group without adding drugs, the rest were treated in the same way as the drug-dosing experimental group. ), each group had 4 duplicate wells, and the experimental group was added with drug-containing medium, so that the final concentration of quercetin metal complexes was 6.25,...

Embodiment 3

[0036] Example 3 Light Microscopic Morphological Observation of Quercetin Metal Complexes Inhibiting Tumor Cell Growth

[0037] Digest adherent cells HepG2 with 0.25% trypsin to make 5×10 6 Cells / mL single cell suspension was inoculated into 24-well plates, 1 mL per well, cultured for 24 hours, and drug-containing medium was added, and the final concentrations of the complexes were 0 and 40 μmol L -1 . After culturing for 48 hours, the morphology of the tumor cell HepG2 was observed and photographed under an inverted microscope (200×), as shown in FIGS. 1 and 2 . It can be seen from the figure that the HepG2 cells without drug (control group) grow well, basically adhere to the wall, the cells are full, the edges are clear, and they can fuse to form colonies. After changing the liquid and adding the drug, observe daily, and found that the -1 The cells under the action of quercetin metal complexes gradually became round, smaller in volume, weaker in refraction, rougher in cel...

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Abstract

The invention relates to a metal complex of the ouercetin and the glucoside compounds provided with cell apoptosis inducing effect, and the application of the complex in preparing tumor treatment medicine. As reported by experiments, the ouercetin metal complex can inhibit the proliferation of tumor cells, but the uncertainty of the action mechanism restricts the development of the ouercetin metal complex as anticarcinogen medicine. The metal complex of the ouercetin and the glucoside compounds provided with a cell apoptosis inducing effect finds that the metal complex of the ouercetin and the glucoside compounds can induce apoptosis of the tumor cells and can be applied in tumor treatment medicine as a cell apoptosis revulsive.

Description

Technical field: [0001] The invention relates to a metal complex of quercetins and glycoside compounds, an apoptosis inducing agent, which has a good apoptosis inducing effect and is used as a drug for treating tumors. Background technique: [0002] Quercetin (Quercetin, Que, 3, 5, 7, 3', 4'-pentahydroxyflavone) widely exists in the plant kingdom, and about 68% of plants contain it. , expansion of coronary arteries, anti-platelet aggregation, anti-inflammatory, anti-allergic, scavenging oxygen free radicals and anti-arrhythmia and other biological activities and pharmacological effects. In addition, quercetin has inhibitory effects on the growth of various tumor cells. But quercetin has not yet been clinically listed. [0003] Quercetin and metal elements can form a variety of metal complexes. The complexes formed by quercetin and metal ions often have strong fluorescence, so quercetin is often used in the fluorescence analysis of metal ions. In recent years, studies hav...

Claims

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Application Information

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IPC IPC(8): C07D311/30C07F19/00A61K31/353A61K31/555A61P35/00
Inventor 谭君王伯初祝连彩贺蕊
Owner CHONGQING UNIV
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