Chityal Ganesh Kumar

Synthesis and biological evaluation of novel alkyl amide functionalized trifluoromethyl substituted pyrazolo[3,4-b]pyridine derivatives as potential anticancer agents

A series of novel alkyl amide functionalized trifluoromethyl substituted pyrazolo[3,4-b]pyridine derivatives 5, 6 and 7 were prepared starting from 6-phenyl-4-(trifluoromethyl)-1H-pyrazolo[3,4-b]pyridin-3-amine 3 via selective N-alkylation, followed by reaction with different primary aliphatic amines, cyclic secondary amines or l-amino acids under different set of conditions. All the synthesized compounds 5, 6 and 7 were screened for anticancer activity against four cancer cell lines such as A549-Lung cancer (CCL-185), MCF7-Breast cancer (HTB-22), DU145-Prostate cancer (HTB-81) and HeLa-Cervical cancer (CCL-2). The compounds 5i and 6e are found to have promising bioactivity at micro molar concentration.

A marine sponge associated strain of Bacillus subtilis and other marine bacteria can produce anticholinesterase compounds

BackgroundAcetylcholinesterase (AChE) inhibitors or anticholinesterases reduce the activity of enzyme acetylcholinesterase that degrades the neurotransmitter acetylcholine in the brain. The inhibitors have a significant pharmacological role in neurodegenerative diseases like Alzheimer’s and Parkinson’s etc. Although plants have been a significant source of these compounds, there are very few sporadic reports of microorganisms producing such inhibitors. Anticholinesterase activity in bacterial associates of marine soft corals and sponges were not previously reported.ResultsWe screened 887 marine bacteria for the presence of acetylcholinesterase inhibitors, in a microplate based assay, and found that 140 (15.8%) of them inhibit the electric eel enzyme, acetylcholinesterase. Majority of the active isolates were bacterial associates of soft corals followed by sediment isolates while most of the potent inhibitors belonged to the bacterial associates of marine sponges. Maximum inhibition (54%) was exhibited by a bacterial strain M18SP4P (ii), isolated from the marine sponge Fasciospongia cavernosa. Based on phenotypic characterization and 16S rDNA sequencing, the strain was identified as Bacillus subtilis - revealing yet another activity in a strain of the model organism that is considered to be a cell factory. TLC bioautography of the methanol extract of this culture, showed the presence of two major components having this activity, when compared to Galanthamine, the positive control.ConclusionFrom the results of our study, we conclude that acetylcholinesterase inhibitors are quite prevalent in marine bacteria, particularly the bacterial associates of marine invertebrates. Several potential AChE inhibitors in marine bacteria are waiting to be discovered to provide easily manipulable natural sources for the mass production of these therapeutic compounds.

Evaluation of critical nutritional parameters and their significance in the production of rhamnolipid biosurfactants from Pseudomonas aeruginosa BS-161R

Eleven biosurfactant producing bacteria were isolated from different petroleum‐contaminated soil and sludge samples. Among these 11 isolates, two were identified as promising, as they reduced the surface tension of culture medium to values below 27 mN m−1. Besides biosurfactant production property, they exhibited good flocculating activity. Microbacterium sp. was identified as a new addition to the list of biosurfactant and bioflocculant‐producers. Optimization of various conditions for rhamnolipid production was carried out for one of the promising isolate, Pseudomonas aeruginosa BS‐161R. Bioglycerol (2.5%), as a cheap renewable carbon source, attained better rhamnolipid yield, while sodium nitrate appeared to be the preferable nitrogen source. The optimum carbon to nitrogen (C/N) and carbon to iron (C/Fe) ratios achieved were 15 and 28,350, respectively, which favored rhamnolipid production. Physical parameters like pH, temperature, and agitation speed also affected the production of rhamnolipids. Results from shake flask optimization indicated that the concentration of bioglycerol, sodium nitrate, and iron were the most significant factors affecting rhamnolipid production, which was supported by the results of central composite rotatable design. After optimization of the culture conditions, the production of rhamnolipids increased by ninefold from 0.369 to 3.312 g L−1.

New bioactive macrocyclic diterpenoids from Jatropha multifida.

Two new macrocyclic diterpenoids, multifidanol (1) and multifidenol (2) along with several known compounds have been isolated from the stem of Jatropha multifida. The structures of the new compounds were established from the extensive studies of their 1D and 2D NMR spectra. The cytotoxic and antimicrobial activities of these two constituents were examined.

Synthesis, Surface Active Properties and Cytotoxicity of Sodium N -Acyl Prolines

Sodium N-acyl prolines (NaNAPro) were synthesized using mixture of fatty acids obtained from coconut, palm, karanja, Sterculia foetida and high oleic sunflower oils via Schotten-Baumann reaction in 58-75% yields to study the synergetic effect of mixture of hydrophobic fatty acyl functionalities like saturation, unsaturation and cyclopropene fatty acids with different chain lengths and aliphatic hetero cyclic proline head group on their surface and cytotoxicity activities. The products were characterized by chromatographic and spectral techniques. The synthesized products were evaluated for their surface active properties such as surface tension, wetting power, foaming characteristics, emulsion stability, calcium tolerance, critical micelle concentration (CMC) and thermodynamic properties. The results revealed that all the products exhibited superior surface active properties like CMC, calcium tolerance and emulsion stability as compared to the standard surfactant, sodium lauryl sulphate (SLS). In addition, palm, Sterculia foetida and high oleic sunflower fatty N-acyl prolines exhibited promising cytotoxicity against different tumor cell lines.

Status and Future Prospects of Fructooligosaccharides as Nutraceuticals

Abstract Fructooligosaccharides (FOS) are gaining tremendous importance as functional food ingredients in view of their multifarious health benefits and pharmaceutical applications. FOS are fructan oligomers available naturally in honey, fruits, and vegetables. FOS are commercially being produced by the transfructosylation of sucrose or hydrolysis of inulin, with the application of enzymes derived from plant and microbial sources. This transfructosylation results in various FOS, such as kestose, nystose, and fructofuranosyl nystose. Inulin hydrolysis results in a similar mixture, although with slightly different end products. These FOS are more soluble in comparison to inulin and are being used as additives in various food products. FOS serves as prebiotics that play a pivotal role in maintaining a healthy gut environment. Low glycemic index, low calorimetric value, increased mineral adsorption are some of the advantages they provide when included in the diet at the appropriate dose. Different fermentation methods employed for the production of FOS and various analytical techniques used for separation and structural elucidation have been discussed in this chapter. In addition, the functional properties and the application of FOS in variety of food formulations and their implications in nutrition and health will be delineated.

Therapeutic nanomaterials: from a drug delivery perspective

Limitations in conventional chemotherapy have resulted in efforts to develop a good drug delivery system for the treatment of several diseases. Many promising drugs that were identified failed to reach the market due to associated drug delivery problems. The ultimate aim of drug delivery systems is to tailor-make the drug formulation to meet the individual requirements under the control of pathophysiological or in vivo conditions, rather than the in vitro characteristics. However, a challenge remains to develop cost-effective, better, and safer nanomaterials for efficient drug loading and controlled drug release. In the recent past, several nanomaterials have been identified with appreciable biocompatibility and therapeutic properties. This chapter focuses on the subject of nanomaterials with regard to their synthetic routes and application as potential drug delivery agents. Different nanomaterial types, including polymeric nanomaterials, dendrimers, nanoparticles, carbon nanotubes, and quantum dots, have been discussed and a number of case studies have been presented.

Synthesis, characterization, and applications of nanobiomaterials for antimicrobial therapy

Abstract Antibiotics have long been considered as “wonder weapons” playing an important role for the treatment of microbial infections resulting in lower mortality rates. In the recent past, the emergence of antibiotic resistance in bacteria has exacerbated the global worldwide health and has compelled the search for new antimicrobial agents. In the recent past, nanobiomaterials have gained interest due to their appreciable biocompatibility with broad spectrum and long-lasting antimicrobial properties for combating microbial infections. This chapter focuses attention on the subject of nanobiomaterials with regard to their several synthetic routes, characterization and application as potential antimicrobial agents. A number of case studies on the biosynthesis of nanobiomaterials have been presented. The characterization methods that elucidate the physicochemical properties of the nanoparticles have been summarized. Different nanobiomaterial types that find application as antimicrobial agents in various sectors like medicine, food industry, sanitation etc. has been presented. Thus, nanobiomaterials are considered as new “magic bullets” in the area of antimicrobial therapeutics.

Synthesis, biological evaluation and molecular docking studies of some novel cyclopropane carbohydrazide derivatives as potential anticancer agents

AbstractThe synthesis of novel series of cyclopropane carbohydrazides is described viaKnoevenagel condensation of 2-furfuraldehyde with malonic acid in five steps. Condensation of the key intermediate 2-(furan-2-yl)cyclopropanecarbohydrazide (4)with heteroaryl/aryl aldehydes (a-t) in presence of ZnO NP in ethanol resulted in substituted N- hetero/arylidene-2-(furan-2-yl) cyclopropane carbohydrazides (5a-t). These compounds were screened for their anticancer activity against a panel of four cancer cell lines and four compounds showed promising activity at micromolar concentration against all the tested cell lines with IC50 values ranging between 1.9-8.45 μM. These compounds were further validated with in silico methods at the anticancer target, colchicine binding site. Graphical AbstractSynthesis of substituted N- hetero/arylidene-2-(furan-2-yl) cyclopropane carbohydrazides. These compounds were screened for their anticancer activity against a panel of four cancer cell lines and four compounds showed promising activity at micromolar concentration against all the tested cell lines with IC50 values ranging between 1.9-8.45 µM.