Application of disubstituted phenyl biguanide to inducing malignant tumor cell for anoikis

A technology for phenylbiguanides and malignant tumors, which can be used in antineoplastic drugs, medical preparations containing active ingredients, organic active ingredients, etc., and can solve problems that have not been studied

Inactive Publication Date: 2010-10-20
INST OF HEMATOLOGY & BLOOD DISEASES HOSPITAL CHINESE ACADEMY OF MEDICAL SCI & PEKING UNION MEDICAL COLLEGE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the application of disubstituted phenylbiguanides in antitumor, especially in inducing anoikis, inhibiting tumor growth and metastasis has not been studied.

Method used

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  • Application of disubstituted phenyl biguanide to inducing malignant tumor cell for anoikis
  • Application of disubstituted phenyl biguanide to inducing malignant tumor cell for anoikis
  • Application of disubstituted phenyl biguanide to inducing malignant tumor cell for anoikis

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Effect test

preparation example Construction

[0146] Preparation of Injections

[0147] Compound (1) 200mg

[0148] Mannitol 700mg

[0149] PEG4000 10mg

[0150] Distilled water 100ml

[0151] Make the pH value 7.0-7.5 and filter the filtrate concentration to be 3 mg / ml, pack in 2 ml per ampoule, and freeze-dry to obtain the injection.

[0152] Preparation 3

[0153] Capsules containing 100 mg of active ingredient per capsule are prepared as follows:

[0154] Dosage / Capsule Weight Concentration (%)

[0155] Compound (3) 100mg 30.0

[0156] Polyoxyethylene sorrel 0.05mg 0.02

[0157] Sugar Alcohol Monooleate

[0158] Starch 250mg 69.98

[0159] Total 350.05mg 100.00.

Embodiment 4

[0161] 100 g of N-(2-chloro-5-trifluoromethylphenyl) biguanide, 100 g of dextrin and 270 g of lactose were added, granulated with 70% alcohol, dried, and packed into capsules to obtain 1000 capsules.

Embodiment 5

[0163] N-(3,5-dichlorophenyl) biguanide 80g, add 2M NaOH to adjust the pH to 8.0, add water for injection to 2000ml, filter through a 0.22μm microporous membrane, subpackage (2ml per bottle), and sterilize to obtain non-toxic Buxostat injection.

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Abstract

The invention relates to disubstituted phenyl biguanide compounds and application containing the same to inducing malignant tumor cell for anoikis and inhibiting tumor growth and transfer. Proved by in vitro-in vivo experiments, the disubstituted phenyl biguanide compounds show the remarkable functions of inducing the malignant tumor cell for anoikis, starting caspase cascade and inhibiting tumor growth and transfer and also have the characteristics of high efficiency and low toxicity, so the disubstituted phenyl biguanide compounds as pharmaceutical compounds are expected to be applied to a plurality of malignant tumor medicaments for inhibiting the tumor growth, invasion and metastasis and treating human melanoma, neurospongioma, lung cancer, gastric cancer, prostate cancer, ovarian cancer and the like.

Description

technical field [0001] The invention belongs to the technical field of pharmacological experiment research, and relates to the application of a series of double-substituted phenylbiguanide compounds in causing anoikis of malignant tumor cells, more specifically, a double-substituted phenylbiguanide with anti-tumor activity Application of compound and pharmaceutical composition containing such compound in inhibiting tumor growth and metastasis and treating human melanoma, glioma, lung cancer, gastric cancer, prostate cancer, ovarian cancer and other malignant tumors with high expression of integrin αvβ3 . Background technique [0002] Integrin αvβ3 is composed of αv and β3 subunits, of which αv subunit (CD51) has 1018 amino acid residues and a molecular weight of 125 kD, and β3 subunit (CD61) has 762 amino acid residues and a molecular weight of 105 kD. It is an important adhesion molecule on the cell surface. On the one hand, it mediates the adhesion between cells and the e...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/155A61P35/00
Inventor 周圆张永慈纪庆彭辉杨铭高瀛岱朱惠芳熊冬生杨纯正
Owner INST OF HEMATOLOGY & BLOOD DISEASES HOSPITAL CHINESE ACADEMY OF MEDICAL SCI & PEKING UNION MEDICAL COLLEGE
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