Application of a kind of quercetin derivative in preparation of antitumor drug

An anti-tumor drug and tumor technology, applied in anti-tumor drugs, drug combinations, pharmaceutical formulations, etc., can solve the problems of quercetin activity research and clinical application limitations, large intermolecular attraction, and low bioavailability

Inactive Publication Date: 2014-10-29
ZHENGZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003]However, because quercetin is a planar molecule, the molecular packing is relatively tight, the intermolecular attraction is strong, and it is not easily dispersed by solvent or solute, so the dissolution of quercetin Poor activity and low bioavailability (the peak plasma concentration is only 0.13~7.6 μmol / L), which greatly limits the activity research and clinical application of quercetin (Sun Tiemin, Sun Changshan, Dai Guangyuan, etc. Chinese medicine Journal of Chemistry, 2003,13(6):345~348; Bakhtiyor F. Rasulev, Nasrulla D. Abdullaev, Vladimir N. Syrov, et al. QSAR Comb. Sci.24,2005, 9:1056~1065.)

Method used

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  • Application of a kind of quercetin derivative in preparation of antitumor drug
  • Application of a kind of quercetin derivative in preparation of antitumor drug

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0013] Example 1 The structural representation of the compound QB

[0014] M.P: 294.9 ~ 296.8 ℃;

[0015] 1 H NMR (400 MHz, DMSO) Δ 12.43 (s, 1H, 5-OH), 10.90 (S, 1H, 7-OH), 10.59 (s, 1H, NH), 9.80 (s, 1H, 4′-OH), 9.45 (s, 1H, 3′-OH), 7.95 (d, j = 8.8 Hz, 2H, 2′-H, 6′-H), 7.83 (d, j = 8.8 Hz, 2H, 2 × pH-H), 7.61-7.54 (m, 2H, 2 × PH-H), 6.91 (d, j = 9.0 Hz, 1H, 5′-H), 6.46 (d, j = 2.0 Hz, 1H, 8-H, 8-H,), 6.24 (d, j = 2.0 Hz, 1H, 6-H), 4.65 (S, 2H, COCH 2 ), 4.30 (q, j = 7.1 Hz, 2H, CH 3 CH 2 ), 1.32 (t, j = 7.1 Hz, 3H, CH 3 ).

[0016] 13 , 71.67, 60.95, 14.68.

Embodiment 2

[0017] Example 2 Anti -tumor activity test

[0018] 2.1 Cell strain and reagent

[0019] Human esophageal squamous cell carcinoma cell EC109, human esophageal squamous cell carcinoma cell EC9706, human gastric cancer cell SGC7901 and mouse melanoma cell B16-F10, purchased at the cell library of the Shanghai Institute of Life Sciences of the Chinese Academy of Sciences.

[0020] Two Kobeya (DMSO), Sigma Company

[0021] Sigma Company

[0022] RPMI-1640 medium, Saimo Fei Shil Biochemical Products (Beijing) Co., Ltd.

[0023] Fetal Bull Serum, Simerfei Shier Biochemical Products (Beijing) Co., Ltd.

[0024] Fasterase, Hangzhou Gino Biomedical Technology Co., Ltd.

[0025] Cultivation base: Take the RPMI-1640 medium, add 10%fetal beef serum, penicillin 100U / ml, rinsein 100 μg / ml, mix well, and store for later use at 4 ° C.

[0026] Cell frozen liquid: Add DMSO to the cultivation base of 10%fetal cattle serum, so that the DMSO concentration is 10%, and it is now available.

[0027] Cor...

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Abstract

The invention discloses application of a compound (QB) shown in a formula I in preparation of medicines for prevention and / or treatment. The MTT experiment displays that the proliferation inhibition effects of the compound QB on the four tumor cells, such as human esophageal squamous carcinoma cell EC109, the human esophageal squamous carcinoma cell EC9706, the human gastric carcinoma cell SGC7901 and mouse melanoma cell B16-F10, are obviously superior to those of quercetin. The inhibition effect of (IC50=5.201mu g / mL) on the EC109 cells is equivalent to that of fluorouracil 5-FU(IC50=5.426mu g / mL), the toxic or side effect is relatively small, and the compound is a potential antitumor candidate compound.

Description

Technical field [0001] The present invention is a pharmaceutical chemistry field. Specifically, the application of dermatin derivatives in preparing anti -tumor drugs. Background technique [0002] C c 槲 (querCetin, 3,3 ', 4', 5,7-pentoxylkyevyloflavonoids) are one of the most abundant flavonoids in the plant world, existing in vegetables (onions, ginger, celery, etc.), fruits), fruits), fruits)(Apple, strawberry, etc.), Chinese herbal medicine (ginkgo, Sanqi, locust rice, etc.) and many beverages (tea, coffee, red wine and fruit juice).Cyidin has a variety of pharmacological activity, such as antioxidant, anti-tumor, anti-inflammatory, diastolic blood vessels, etc.Bischoff sc. Curr Opin clin nutr metab care., 2008, 11 (6): 733-740.).Cyidin has chemical prevention and anticancer effects. It can play an anti -tumor effect by regulating the expression of cancer suppressing genes, blocking cell cycles, inducing apoptosis, blocking and metastasis of cells, blocking and metastasis.A h...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/352A61P35/00
Inventor 翟广玉颜子童渠文涛段艳丹
Owner ZHENGZHOU UNIV
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