Manna, P. and Narang, K.K. and Manna, S.K. (2005) 1,2,4-thiadiazolidine derivative inhibits nuclear transcription factor-?B and its dependent genes activation but induces apoptosis. International Journal of Cancer, 113 (4). pp. 549-560. ISSN 0020-7136

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Abstract

The 1,2,4-thiadiazolidine derivatives have been shown to be involved in several biological responses such as anti-bacterial, anti-fungal, anti-tubercular and local anaesthetic activities. In our study, we have synthesized some new 5-substitutedarylimino-2-N-substitutedphenyl-3-oxo-1,2,4-thiadiazolidine and tested for anti-inflammatory and anti-tumor activities. The 5-(4-methoxyarylimino)-2-N-(3,4-dichlorophenyl)-3-Oxo-1,2,4-thiadiazolidine (P(3)-25) showed anti-inflammatory activity as it inhibited different inflammatory inducers mediated nuclear transcription factor kappa B (NF-kappaB), a key transcription factor involved in all forms of inflammation. P(3)-25 inhibited TNF-induced NF-kappaB activation as detected by gel shift assay and dependent reporter gene expression. It inhibited IkappaBalpha degradation, IkappaB kinase activation and p65 nuclear translocation. P(3)-25 inhibited TNF-induced Cox2 expression. It inhibited NF-kappaB activation in human epithelial and T cells. Unlike other substitutary derivatives, P(3)-25 was a potent inducer of apoptosis as it induced cell death, caspase-dependent PARP cleavage, ROI generation and lipid peroxidation. Overall our results suggest that P(3)-25 derivative exerts anti-inflammatory and anti-tumor activities, which may have a role in designing such drugs.

Item Type:	Article
Depositing User:	Users 2 not found.
Date Deposited:	08 Jul 2015 06:46
Last Modified:	16 Jul 2015 10:55
URI:	http://cdfd.sciencecentral.in/id/eprint/235

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