Russian Journal of BiotherapyRussian Journal of BiotherapyРоссийский биотерапевтический журнал1726-97841726-9792Publishing House ABV Press88110.17650/1726-9784-2017-16-3-63-68ORIGINAL REPORTSОРИГИНАЛЬНЫЕ СТАТЬИSynthesis and investigation of modified gastrin fragmentsСинтез и изучение модифицированных фрагментов гастринаSushininaL. P.СушининаЛ. П.
Russian Federation
SmirnovaA. P.СмирноваА. П.
Russian Federation
chemlab@ronc.ruUstinkinaS. V.УстинкинаС. В.
Russian Federation
SmirnovaL. I.СмирноваЛ. И.
Russian Federation
SidorovaT. A.СидороваТ. А.
Russian Federation
KiselevaM. P.КиселеваМ. П.
Russian Federation
BorisovaL. M.БорисоваЛ. М.
Russian Federation
ShprakhZ. S.ШпрахЗ. С.
Russian Federation
N.N. Blokhin National Medical Research Oncology Center, Ministry of Health of RussiaФГБУ«НМИЦ онкологии им. Н.Н. Блохина» Минздрава России30092017163636810042018https://bioterapevt.abvpress.ru/jour/article/view/881

Background. The purpose of this investigation is the search of new compounds with high selectivity of antitumor action on the tumor of the gastrointestinal tract (GIT) in the series of analogues of the peptide hormone gastrin. Objective: synthesis of 2 analogues of gastrin, 1 of which contains the cytotoxic group, the study of their cytotoxic and antitumor activity. Materials and methods. Synthesis of peptides was carried out by classical methods of peptide chemistry. Cytotoxic activity was studied on the cell culture НСТ116. Antitumor activity of analogues of gastrin were studied on transplanted tumors of the GIT of mice AKATOL and AKATON. Results. Two analogues of gastrin (octapeptide) were synthesized, 1 of which contains a cytotoxic group. Analogue containing cytotoxic group revealed the cytotoxic activity. Antitumor activity of two analogues of gastrin were studied on transplanted tumors of the GIT of mice AKATOL and AKATON. The cytotoxic and non-cytotoxic analogues of gastrin showed antitumor activity only on AKATON. Inhibition of tumor growth is 74 and 84 %, respectively. Conclusions. The therapeutic effect of two analogues of gastrin on adenocarcinome AKATON, probably, is associated with the expression of gastrin receptors ССК2 in this tumor.

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