Abstract:
:Cancer is one of the most fatal diseases in the world and it has been years that finding new drugs and chemotherapeutic techniques with lowest side effects become one of the most important challenging matters needs really hard efforts. Chlorambucil (CBL), an ancient direct-acting alkylating anticancer agent, is commonly used for initial treatment of some kinds of cancers but the use of CBL is often limited because of the unpleasant side effects due to its lack of specificity for targeting cancer cells. In this research we tried to increase the specificity of CBL by producing a novel conjugate by using glutamine amino acid (Glut). Based on previous studies, poly amines and nitrogen compounds noticeably are used by cancer cells increasingly; therefore we decided to increase the efficiency and specificity of CBL by designing and producing a novel anti cancer conjugate using glutamine amino acid as an uptake enhancer, CBL, and Adipic acid Dihydrazide (ADH) as a spacer and linker. The biological tests were carried out on HT29 colorectal cancer cell line to evaluate its anticancer properties. Biological tests like MTT assay, finding IC50, evaluating the induced mechanism of the death of our novel CBL-Glutamine conjugate on HT29 cells, testing abnormal toxicity of this conjugate on mice in comparison with CBL drug were careid out. We found that not only CBL-Glutamine conjugate preserved its anti cancer property with regard to CBL drug, but also it represent lower abnormal toxicity in mice. Apoptosis was detected as its mechanism of the death. Our present study provides a promising strategy for targeting cancer cells using amino acids nano-conjugate drugs. The future perspectives have also been highlighted in continuing similar and relative researches.
journal_name
Anticancer Agents Med Chemjournal_title
Anti-cancer agents in medicinal chemistryauthors
Tabasi MA,Amanlou M,Siadat SD,Nourmohammadi Z,Omoomi FD,Ebrahimi SE,Aghasadeghi MR,Rahimi P,Pourhosseini S,Mehravi B,Ardestani MSdoi
10.2174/18715206113139990132subject
Has Abstractpub_date
2013-11-01 00:00:00pages
1449-59issue
9eissn
1871-5206issn
1875-5992pii
CMCACA-EPUB-20130102-2journal_volume
13pub_type
杂志文章abstract::Cancer is the deadliest disease worldwide and the development of safer chemical entities to treat cancer is one of the major challenges of medicinal chemistry. Emergence of new cases every year and development of multiple drug resistance against available molecular entities has turned the focus of researchers towards ...
journal_title:Anti-cancer agents in medicinal chemistry
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