In Vitro Evaluation of Monohalogenated Semicarbazones and Thiosemicarbazones as Potential Cytotoxic Agents Induction of Apoptosis and Genotoxicity

A series of halogenated Semicarbazones (SCs) and Thiosemicarbazones (TSCs) (11-30) were synthesized from mono fluorinated-, bromine- and chlorinated acetophenones (1-10). Structures were confirmed by Nuclear Magnetic Resonance (NMR) spectral data. Both effects, thehalogenated substituent and the position of the substitution on the antiproliferative activity, were systematically investigated for the first time.Cytotoxic activity was evaluated, using tetrazolium salt method (MTT), in two murine cell lines: CT26 (colon cancer) and B16 (melanoma). Only, o-, m- and p-fluorinated SCs and TSCs showed significant cytotoxic activity. Among them, compounds with fluorine at m-position in the phenyl ring showed the superior antiproliferative activity. The most actives derivatives were: m-Fluoroacetophenone semicarbazone (13) (µM; IC50 =7.2 ± 0.5, IC50=8.1 ± 0.2) and m-Fluoroacetophenone Thiosemicarbazone (23) (µM; IC50 = 3.1 ± 0.4, IC50=4.9 ± 0.5) in CT26 and B16, respectively. In addition, studying the genes Bcl-2 and Bax, compound 23 showed apoptosis induction and non-genotoxic properties.
Dna, Microscopic, Cell, Gene, Helix, Science, Medical

Comments

Post a Comment

Popular posts from this blog

Synthesis Characterization and Evaluation of Novel Substituted Azole Derivatives

Image
Benzimidazole is a very stable nucleus and the derivatives of 2-methyl benzimidazole may show different and better biological activity. Thepresence of the thiazolidinone ring in a benzimidazole derivative enhances its antimicrobial activity. 2-methyl benzimidazole derivative are formed by the condensation of o-phenylenediamine with acetic acid. Combination of two or more active moieties into one is a common procedure, can result in augmenting the activity and removes untoward side effects. Hence, the present work focuses on synthesis of potent antimicrobial benzimidazole derivatives by the condensation of Schiff's bases of 2-methyl benzimidazole moiety with thiomalic acid affording the thiazolidinone ring and to study their antimicrobial activity. In antibacterial activity (Staphylococcus aureus and Escherichia coli), it shows that compound TE6 is the most active compound and in antifungal activity (Candida albicans), TE3 & TE4 are found to be most active.
Read more

Separation and Identification of the Components of Acacia Sieberiana Stem Bark Plant Extract and Study its Safety as a Treatment Drug for Diarrhea

Image
The Safety of the stem bark of Acacia Siberian, as an antidiarrheal, in Albino rats (four groups) has not yet been evaluated. Thisstudy to identify the effect of the acetone extract of the stem bark of Acacia Siberian (AESBAS) on Albino rats, Separation andidentification of the acetone extract of the stem bark of Acacia Siberian by GC-MS-TMS analysis. Albino rats (four groups) were subjected to the sub-chronic oral administration of the AESBAS for Twenty-eight days. Phytochemical screening test of the AESBAS confirmed by GC-MS-TMS analysis. Non-significant effect (p>0.05) in mean weight gain during the end of the experiment between groups. Also, some hematological analysis in the twenty-ninth day was estimated using standard steps. The AESBAS had non-significant effect (p>0.05) on some hematological analysis on study groups compared with the control group, that were given varying doses of the AESBAS. The components of AESBAS confirmed by GC-MS-TMS analysis. The results of this ...
Read more

Reuse of Treated Wastewater of the City of Salé in Agriculture

Image
The city of Salé produces about 24 millions m3 /year of wastewater. The majority of this water is discharged directly into the Atlantic coast and Bouregreg estuary without any treatment. To preserve the quality of the receiving waters. treating wastewater and reusing it in agricultureproves very interesting. The objective of this study is thus to investigate the treatment and recycling of wastewater in agriculture. We are particularly interested in studying the growth of the stem and the average number of leaves in order to prove the positive effects of reusing treated wastewater in agriculture as compared to untreated wastewater. To achieve this objective. we have investigated the irrigation of the broad bean by three types of water: Untreated wastewater (UW). Well water (WW) and biologically treated wastewater (TW).
Read more