Abstract
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.
Highlights
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
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
Summary
Работа посвящена поиску новых соединений с высокой избирательностью противоопухолевого действия на опухоли желудочно-кишечного тракта (ЖКТ) в ряду аналогов пептидного гормона гастрина. Цель исследования – синтез 2 аналогов гастрина, 1 из которых содержит цитотоксическую группу; изучение их цитотоксической и противоопухолевой активности. Противоопухолевую активность аналогов гастрина оценивали на моделях перевиваемых опухолей мышей: аденокарциноме тонкой кишки АКАТОН и аденокарциноме толстой кишки АКАТОЛ. Синтезированы 2 аналога гастрина (октапептиды), 1 из которых содержит цитотоксическую группу. Изучена противоопухолевая активность 2 аналогов гастрина на перевиваемых опухолях ЖКТ мышей: АКАТОЛ и АКАТОН. Установлена противоопухолевая активность цитотоксического и нецитотоксического аналогов гастрина на аденокарциноме тонкой кишки АКАТОН: 74 и 84 % торможения роста опухоли соответственно. На аденокарциноме толстой кишки мышей АКАТОЛ исследованные аналоги гастрина противоопухолевого действия не показали. Терапевтический эффект 2 аналогов гастрина на аденокарциноме тонкой кишки АКАТОН, вероятно, связан с экспрессией рецепторов гастрина ССК2 в этой опухоли.
Sign-in/Register to view highlights & summary Sign-in/Register to access full text options 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
