Cytotoxic effects of Mannich bases via induction of caspase-3 pathway on human oral squamous cell carcinoma

Year 2021, Volume: 8 Issue: 1, 187 - 194, 28.02.2021

Cem Yamalı , Halise İnci Gül

https://doi.org/10.18596/jotcsa.817007

Cited By: 2

Abstract

In anticancer drug research, there is a need for the synthesis of compounds with selective cytotoxicity compared to the drugs in the market. The current study aimed to determine the cytotoxicities of the bis Mannich bases 1-9 towards human oral squamous cell carcinoma (OSCC). Mannich bases showed cytotoxicity in low micromolar in the range of 1.7-27 µM against OSCC cell lines. The compounds 5 with the highest potency selectivity expression (PSE) value (318.1) and 7 with the highest tumor selectivity (TS) values (TS1:11.2, TS2:15.8) showed promising selective cytotoxicity towards cancer cell lines. According to Western blot analysis, representative compound 7 induced the activation of caspase-3 in HSC-2 cells. These results may suggest that the apoptosis pathway may be one of the possible mechanisms of the actions and lead compound 7 can be subjected to further bioassays.

Keywords

Mannich, anticancer, apoptosis

Supporting Institution

Research Foundation of Ataturk University

Project Number

2015-322

Thanks

The authors are thankful to Hiroshi Sakagami (Meikai University, Japan) and Noriyuki Okudaira (Meikai University, Japan) for biological studies.

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