Application of adenosine in preparing medicament for treating tumors

Abstract

The invention discloses application of adenosine in preparing a medicament for treating tumors. In the invention, the adenosine in the field of tumor treatment is applied. In the application, injections, sustained-release preparations or targeting preparations can be prepared from the adenosine. Standard substance anti-tumor effect contrast proves that: when reaching certain concentration in vitro or in vivo, the adenosine participating in human metabolism has remarkable effects of tumor cell apoptosis and resisting tumor angiogenesis. The application has the advantages that: compared with other anti-tumor medicaments, the adenosine has efficient, broad-spectrum and low-toxicity anti-tumor effect, can be used in chemotherapy of gastric cancer, lung cancer, liver cancer, colon cancer, breast cancer and reproductive system and other malignant tumors, has remarkable anti-tumor effect, and does not have bone marrow suppression and vital organ injury by conventional dosage.

Description

technical field [0001] The invention relates to the application of adenosine, specifically the application of nucleoside, one of the normal components of nucleic acid, in the preparation of drugs for treating tumors, and belongs to the field of medicine. Background technique [0002] Adenosine (i.e. adenine ribonucleoside, English name: Adenosine): 6-amino-9-β-D-ribofuranosyl-9-H-purine, molecular formula C10H13N5O4, molecular weight 267.24, CAS number: 58-61- 7, (CAS number, also known as CAS Registry Number or CAS Number, CAS Rn, CAS#, CAS registration number, is a unique digital identification number for a certain substance, such as a compound, polymer material, biological sequence, mixture or alloy, etc. .) [0003] Adenosine is an endogenous nucleoside that is distributed throughout human cells. It is used as an important intermediate in the synthesis of adenosine triphosphate (ATP), adenine, adenylic acid, and vidarabine. It can directly enter the myocardium and be ph...

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Problems solved by technology

[0005] At present, there are few reports on the anti-tumor effect of adenosine at home and abroad, and the reported adenosine has a relatively weak inhibitory effect on tumors. For example, an article on "NF The role of -κB and Caspase-3 in adenosine-induced apoptosis of human HepG2 cells" proposed that the IC50 value of adenosine was 0.66 mg / ml; an article published in the Chinese Journal of Traditional Chinese Medicine, Volume 28, Issue 4, April 2010 The IC50 value of adenosine proposed in "Basic Research on Anti-tumor Effects of Different Purified Components of Paecillin in Vitro" is 2.1mg / ml; these values ​​are all in a relatively high range, such a high IC50 value, according to drug research and development It is impossible to develop into a clinical anti-tumor drug based on the routine judgment of personnel, and it is not practical

[0006] In addition, there are some literature reports about the role of adenosine channel in promoting cell proliferation and promoting angiogenesis, for example: an article on "High concentration of adenosine through Inhibiting cell proliferation and promoting cell survival"; the IC50 of adenosine mentioned in "A study of adenosine-induced apoptosis of HepG2 cells through endoplasmic reticulum stress pathway" published in China Pharmacology Bulletin 2010-May-29(1) The value is low, about 0.1mg / ml. However, this study is based on the theory of inducing tumor cell apoptosis, and there is no in-depth study on pharmacodynamics such as anti-tumor angiogenesis.

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