Effect of Substituted Benzimidazoles and Somatostatin Analogs on the Vitality of Tumor Cell Lines and on the Oxidative Burst of Phagocytes

Author(s): Ivan Goshev, Emilia Naydenova, Svetlana Staykova, Anelia Mavrova, Ljubomir Vezenkov, Diana Wesselinova.

Journal Name: Letters in Drug Design & Discovery

Volume 13 , Issue 8 , 2016

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Abstract:

Background: For studying the antioxidant activity a synthesized 1,3-bis(3-phenylpropyl-1)- 1,3-dihydro-2H-benzimidazol-2-imine hydrobromide (M1) has been chosen because of its most pronounced antiproliferative effect (preliminary studies) to human colorectal cancer cell line HT-29, breast cancer cells MDA-MB-231 and its nontoxicity to normal Lep 3, determined by means of MTS-test. It is believed that this suppressive activity is due to its antioxidant capacity. Other two new linear somatostatin analogs which contain hydrophobic aminoacids 3c (D-Phe-c(Cys-Phe-D-Trp-Lys-Tle-Cys)-Thr-NH2) and 3L (Pro-Phe-Val-Tyr-Leu-Ile-D-Trp-Lys-Tle-Thr-NH2) were tested for their toxicity to the same cells and all experiment substances were tested to activated macrophages.

Methods: the ROS-scavenging ability was examined (by HORAC and ORAC) using the same cells and the obtained results confirmed a considerable suppressive capacity of the compounds.

Results: The compounds 3c and 3L exerted the most pronounced inhibition of the tumor cell vitality (up to 77%) at higher concentrations and were not toxic to normal Lep-3 cells. After similar incubations with the substances activated human peritoneal macrophages displayed also emission of ROS determined by chemiluminiscence (CL). Compound M1 showed pronounced activity against activated peritoneal macrophages (PMA) mainly in the 100000x dilution in comparison to the HORAC and ORAC; 3L is most effective only in the 100x concentration.

Conclusion: All tested compounds showed different suppressive activities depending on the cell line and on the substances amount applied by performing HORAC / ORAC and CL investigations.

Keywords: 2-iminobenzimidazoles, somatostatin analogs, ROS emission of tumor cells.

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Article Details

VOLUME: 13
ISSUE: 8
Year: 2016
Page: [725 - 728]
Pages: 4
DOI: 10.2174/1570180813999160429112829
Price: $58

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