Synthesis, Biological Activity and Molecular Docking Studies of Heterocyclic Chalcones.

Nineteen heterocyclic chalcones were synthesized from 4-acetyl-5-methylquinolylpyrazole and heteroaryl (imidazole, pyrazole, thiophene, indole and triazole) aldehydes and were screened in vitro using four tumor cell lines for their cytotoxic capability and for antimicrobial activity. The chalcone 5b exhibited the highest activity with IC50 values 2.14 µM against colon (HCT-116) and 5.0 µM, against prostate (PC-3) cancer cell lines and also displayed good activity against fungal strain (A. niger) with MIC value 9.1 µM. The chalcones 5q and 5p displayed good activity against bacterial strains (S. aureus) having MIC value 2.6 µM and fungal strain (C. albicans) having MIC value 5.4 µM, respectively. The molecular docking outcome revealed that the synthesized heterocyclic chalcones demonstrated hydrogen bond, hydrophobic and electrostatic interactions with their respective biochemical targets.

Biomedical applications of L-alanine produced by Pediococcus acidilactici BD16 (alaD+).

L-alanine possesses extensive physiological functionality and tremendous pharmacological significance, therefore could be considered as potential ingredient for food, pharmaceutical, and personal care products. However, therapeutic properties of L-alanine still need to be addressed in detail to further strengthen its utilization as a viable ingredient for developing natural therapeutics with minimum side effects. Thus, the present study was aimed to explore the anticipated therapeutic potential of L-alanine, produced microbially using a lactic acid bacterial strain Pediococcus acidilactici BD16 (alaD+) expressing L-alanine dehydrogenase enzyme. The anticipated therapeutic potential of L-alanine was assessed in terms of anti-proliferative, anti-bacterial, and anti-urolithiatic properties. Anti-bacterial assays revealed that L-alanine successfully inhibited growth and in vitro proliferation of important human pathogens including Enterococcus faecalis, Escherichia coli, Klebsiella pneumonia, Staphylococcus aureus, Streptococcus mutans, and Vibrio cholerae in a concentration-dependent manner. Current investigation has also revealed its significant anti-proliferative potential against human lung adenocarcinoma (A549; IC50 7.32 µM) and mammary gland adenocarcinoma (MCF-7; IC50 8.81 µM) cells. The anti-urolithiatic potential of L-alanine was augmented over three different phases, viz., nucleation inhibition, aggregation inhibition, and oxalate depletion. Further, an in vitro cell culture-based kidney stone dissolution model using HEK293-T cells was also established to further strengthen its anti-urolithiatic potential. This is probably the first in vitro cell culture-based model which experimentally validates the immense therapeutic efficacy of L-alanine in treating urolithiasis disease. KEY POINTS: • Assessment of therapeutic potential of L-alanine produced by LAB. • L-alanine exhibited significant anti-proliferative and anti-bacterial activities. • L-alanine as potential anti-urolithiatic agent.

Reciprocal relation between reporter gene transcription and translation efficiency in fission yeast.

The fission yeast, Schizosaccharomyces pombe, is an excellent model for basic research but is not useful for commercial scale protein expression due to lack of strong expression vectors. Earlier, we showed that the lsd90 promoter elicited significantly greater GFP expression level than the adh1 and nmt1 promoters, albeit in different vector backbones. Here, we have systematically investigated the contribution of selectable markers, LEU2 and URA3m to GFP expression: while LEU2 elicited very low expression, the URA3m gene, with truncated promoter, elicited much greater GFP expression level with all promoters. Paradoxically, an inverse correlation was observed between the GFP transcription and translation efficiency. This system can be useful for understanding the factors governing recombinant gene expression and optimization of protein production.

Biosorption of Cr(III) from aqueous solution using algal biomass spirogyra spp.

In the present investigation, a fresh water green algae spirogyra spp. was used as an inexpensive and efficient biosorbent for Cr(III) removal from aqueous solution. The algal biomass was treated with 0.1M NaOH, 0.2M CaCl(2) and 5% HCHO. The biosorption efficiency was compared with untreated biomass. The effects of various physico-chemical parameters were studied, e.g. pH 3.0-6.0, initial metal ions concentration 20-150mgL(-1), algal dose 1.0-3.0gL(-1), and contact time 15-180min, respectively. Biosorption of Cr(III) is highly pH dependent. Maximum 81.02% adsorption of Cr(III) was observed with 0.2M CaCl(2) treated biomass at pH 5.0. Removal of Cr(III) was more than 70% in 45min of contact time with different treated and untreated algal biomass at concentration 30mgL(-1). Maximum metal uptake (Q(max)) was observed as 30.21mgg(-1) with 0.2M CaCl(2) treated algal biomass indicate good biosorbents than other treated and untreated biomass. The high values of correlation coefficient (r(2)<0.90) indicate equilibrium data of treated and untreated form of algal biomass well fitted in Freundlich than Langmuir isotherms model equations.