Synthesis of novel carbazole hydrazine-carbothioamide scaffold as potent antioxidant, anticancer and antimicrobial agents.

BACKGROUND: Carbazole-based molecules containing thiosemicarbazide functional groups are recognized for their diverse biological activities, particularly in enhancing therapeutic anticancer effects through inhibiting crucial pathways. These derivatives also exhibit noteworthy antioxidant properties. OBJECTIVES: This study aims to synthesize, characterize, and evaluate the antioxidant and anticancer activities of 18 novel carbazole derivatives. METHODS: The radical scavenging capabilities of the compounds were assessed using the 2,2-diphenyl-1-picrylhydrazyl assay. Antiproliferative activities were evaluated on MCF-7 cancer cell lines through viability assays. Additionally, the modulation of the PI3K/Akt/mTOR pathway, apoptosis/necrosis induction, and cell cycle analysis were conducted for the most promising anticancer agents. RESULTS: nine compounds showed potent antioxidant activities with IC50 values lower than the positive control acarbose, with compounds 4 h and 4y exhibiting the highest potency (IC50 values of 0.73 and 0.38 µM, respectively). Furthermore, compounds 4o and 4r displayed significant anticancer effects, with IC50 values of 2.02 and 4.99 µM, respectively. Compound 4o, in particular, exhibited promising activity by targeting the PI3K/Akt/mTOR signaling pathway, inhibiting tumor survival, inducing apoptosis, and causing cell cycle arrest in MCF-7 cell lines. Furthermore, compound 4o was showed significant antimicrobial activities against S. aureus and E. coli, and antifungal effect against C. albicans. Its potential to overcome drug resistance through this pathway inhibition highlights its promise as an anticancer agent. Molecular docking simulations supported these findings, revealing favorable binding profiles and interactions within the active sites of the enzymes PI3K, AKT1, and mTOR. Moreover, assessing the druggability of the newly synthesized thiosemicarbazide derivatives demonstrated optimal physicochemical properties, further endorsing their potential as drug candidates.

Influences of phenolic compounds on citric acid productivity by Aspergillus niger in stirred fermentor

Influences of phenol, alpha-naphtol and beta-naphtol, which are toxic chemicals, on citric acid biosynthesis and biomass in the artificial culture setting of Aspergillus niger using batch fermenter are examined in the most favorable fermentation conditions, and a model is proposed. Addition of certain concentrations of phenol, alpha-naphtol and beta-naphtol to the culture increases the citric acid production. According to this model, maximum citric acid concentration is 48.3 g L-1 in a culture that does not contain any toxic chemicals, whereas the maximum concentrations obtained in cultures containing 25 mg L-1 phenol, 25 mg L-1 alpha-naphtol and 15 mg L-1 beta-naphtol are 62.5 g L-1, 78.1 g L-1 and 86.0 g L-1, respectively. Moreover, addition of toxic chemicals to the culture reduces fermentation time by 24 hrs.

Application of silica gel 60 loaded with Aspergillus niger as a solid phase extractor for the separation/preconcentration of chromium(III), copper(II), zinc(II), and cadmium(II).

Sorption properties of silica gel 60 loaded with fungi cells characterized as Aspergillus niger were evaluated for trace enrichment of Cr(III), Cu(II), Zn(II), and Cd(II) from various water samples prior to the description of flame atomic absorption spectrometric analysis. The proposed SPE method is cheap, simple, highly sensitive, accurate, and selective for enrichment of analytes. The effect of experimental parameters, such as pH of sample solution, amount of solid phase, eluent type, and volume of sample solution on the recovery of the metal ions has been investigated. The effect of diverse ions was also investigated. The recoveries of Cr(III), Cu(II), Zn(II), and Cd(II) under the optimum experimental conditions were 98 +/- 2, 98 +/- 3, 99 +/- 2, 100 +/- 2%, respectively, at the 95% confidence level. The analytical detection limits were found to be 3.1, 1.6, 1.1, and 1.4 microg/L for Cr(III), Cu(II), Zn(II), and Cd(II), respectively. The proposed enrichment method was applied to the determination of analytes in Atatürk Dam, Egirdir Lake, and tap-water samples. The analytes were determined with a relative error lower than 8% in various water samples. The method has been validated by analyzing spiked water samples.