Recent Developments in Chemistry and Biochemistry Research Vol. 3

This book chapter provides a thorough examination of the isolation process, structural characterization, and pharmacological properties of two novel depsides, Antarvedisides A and B, extracted from Dirinaria consimilis (Stirton) D.D. Awasthi, alongside several known depsides. The study explores the compounds' structural features and delves into their pharmacological profile, emphasizing their potential as promising candidates for future drug development. Chromatographic examination of acetone extract of D. consimilis yielded Antarvedisides A and B, sekikaic acid, atranorin, divaricatic acid and 2’-O-methyl divaricatic acid. Antioxidant activity assessment through superoxide, DPPH and ABTS radical scavenging assays reveals that Antarvedisides A-B and 2’-O-Methyldivaricatic acid exhibit remarkable antiradical scavenging capacities, surpassing the standard drug, ascorbic acid. The investigation extends to in vitro anti-inflammatory activity, where atranorin exhibits superior inhibition against protein denaturation in comparison to the standard drug indomethacin. Antarvedisides A-B showcases moderate anti-inflammatory activity, further detailed with IC₅₀ values ranging from 878-600 µg/mL. The anticancer potential of the depsides is highlighted through the Sulforhodamine B assay screening. Antarvediside B emerges as a potent inhibitor of cell growth in MCF-7 and HeLa, outperforming doxorubicin. Additionally, 2’-O-methyldivaricatic acid demonstrates significant inhibitory profiles against various cancer cell lines. In conclusion, this abstract summarizes the comprehensive pharmacological profile of Antarvedisides A and B, shedding light on their antioxidant, anti-inflammatory, and anticancer activities. These findings underscore the potential of these depsides as valuable candidates for further drug development and contribute to the expanding knowledge of natural compounds with therapeutic implications.

This study investigates Trichosanthes tricuspidata seeds as a potential novel source for bio-oil production. Employing a Soxhlet extractor, the research delves into the presence of fatty acids in oil extracted using various solvents. The primary aim is to optimize the extraction process to maximize bio-oil yield, examining factors such as extraction time and seed particle size. Initial experiments encompass a diverse range of particle sizes and extraction durations. Subsequently, to refine the process, a fixed particle size is utilized alongside different solvents. The study identifies the optimal extraction process as a 3h extraction time with a particle size of 0.55 mm, employing isopropyl alcohol as the solvent, resulting in a bio-oil extraction rate of 20% (w/w). The significance of this research lies in introducing a fresh approach to bio-oil production from an untapped plant source. By enhancing the extraction process from Trichosanthes tricuspidata seeds, this study contributes to the advancement of sustainable and economically viable bio-oil production methods. Furthermore, the study employs analytical techniques to comprehend the composition of the extracted bio-oil.

This study uses human serum acetylcholinesterase to analyze the kinetics of a few produced phenolic derivatives (A, B, C, and D). The compounds A, B, and D were observed to exhibit inhibitory effects at varying concentrations (10-4, 10-6, 10-8, and 10-10 mM). Additionally, there was an increase in inhibition with increasing concentrations (10-10 to 10-4 mM) for compounds A and B and an increase in inhibition with decreasing concentrations (10-4 to 10-10 mM) for compound D. It was reversible how A, B, and D affected things. For the C compound, every result was disregarded. In both the treated and control systems, the Michaelis-Menten constant and maximum velocity for the hydrolysis of acetylthiocholine iodide by AChE were found. The supplementary replots for the line weaver-burk plot were shown.

In the present study, we have designed and synthesized a new series of bipyrimidines by simple condensation and screened them for their in vitro antimicrobial activities. Current research has depicted the efforts towards the utilization of biphasic reaction systems in the synthesis of a variety of heterocycles. This shows the remarkable importance of the monophasic solvent system. A simple, green and efficient catalytic condensation process has been developed to synthesize the series of 2-amino-6-substituted- 4,6-diphenyl-3',4,4',5-tetrahydro[4,5'-bipyrimidine]-2'(1H)-one (3a- j) hybrids. The catalytic route was investigated efficiently in the presence of NaY zeolite in an organic-aqueous (dichloromethane-water) solvent system. In this method, biphasic solvent systems were explored for suitable applicability where catalyst exhibits remarkable reactivity. The synthesized scaffolds of bipyrimidines were studied as anti-microbial agents. The investigation of antimicrobial screening data revealed that among 10 compounds screened, compounds 3d, 3e, 3f and 3i demonstrated very good activity as compared to standard drugs and the remaining compounds showed good to moderate inhibition activities.

Synthesized compounds were screened for their in vitro antibacterial activity against Staphylococcus aureus, E. coli and Pseudomonas aurigenosa and also antifungal activity against the opportunistic pathogens Candida albicans and Aspergillus niger.

The production of polyhydroxyalkanoates (PHAs) using raw sewage has been previously attempted to derive value from waste; however, the yields of PHAs were low. Therefore, we attempted to increase the yield by applying different strategies, such as supplementation of sewage with additional carbon sources, dilution of high-carbon-containing wastewater (cheese whey) with low-carbon-containing wastewater (sewage), and concentration of sewage to improve the available carbon source. After applying these strategies, the PHA production capacity of the bacterium Bacillus sp. CYR1 is enhanced 22-fold. CYR1 incubated using cheese whey (CW) diluted with sewage showed higher PHA production than those incubated using CW diluted with distilled water. The PHA produced in this study was identified as poly-\(\beta\)-polyhydroxybutyrate (PHB), and the characteristics of the produced PHB were comparable to those of standard PHB. We believe that our study makes a significant contribution to the literature because we show the potential of CYR1 strain in PHB production using low- or high-carbon-containing wastewater. The reuse of sewage will help to reduce the ecological burden and energy consumption on a global scale.

The increasing burden placed by plastic waste on the environment has necessitated the protection of our planet from environmental disasters. Thus, switching from limited natural and fossil resources to PHAs for plastic production matches today's concrete initiatives to reach the global Climate and Sustainable Development Goals. On a related note, the constant generation of sewage in our daily activities accounts for a high proportion of the environmental load, and the energy and cost required for sewage treatment are extensive. Thus, the reuse of sewage is essential for reducing the ecological burden and energy consumption on a global scale. Consequently, painstaking efforts have been taken to transform waste management into resource management. Our group has been working on the production of bioplastics using rejected materials. Therefore, in this study, we aimed to enhance PHA production from sewage by applying different strategies using Bacillus sp. CYR1. A high rate of glucose consumption (83.6%) was also observed. Higher phaC gene expression levels were observed in high-carbon-containing sewage but at lower nitrogen concentrations. Based on these analyses, it was confirmed that the CYR1 strain can be useful for producing PHA using low- or high-carbon-containing wastewater.

Phthalazine derivatives are an essential component of biological systems that serve as a structural template for biologically active molecules. In this chapter, Novel N-(4-(1,2-dihydrophthalazin-1-yl) phenyl) amides were synthesized in good yields, beginning with inexpensive and easily accessible phthalic anhydride using Pd (OAc)₂ catalyzed Suzuki-mayura coupling and N-acylation reactions as key steps. All the prepared compounds were characterized by various spectroscopic techniques such as ¹H NMR, ¹³C NMR, IR, and LCMS and all the data showed good agreement with the predicted structures. Additionally, the produced compounds' in vitro anti-microbial activity was examined. In comparison to Xanthomonas campestris, the target compounds 7i, 7f, and 7a demonstrated superior activity. In contrast, the compounds 7j, 7a, and 7h demonstrated excellent activity against Bacillus megaterium. Escherichia coli was effectively inhibited by compounds 7j and 7a. The obtained N-(4-(1,2-dihydrophthalazin-1-yl) phenyl) amide derivatives offer an intriguing profile in the field of antimicrobial research.

Purpose: This study aimed to investigate the prognostic significance of the Family with Sequence Similarity 72 member (FAM72) gene family in clear cell renal carcinoma (ccRCC) using a bioinformatic approach.

Background: The Family with Sequence Similarity 72 (FAM72) gene family, specific to neural stem cells, has emerged as a potential biomarker in various cancers, including glioblastoma multiforme, adrenocortical carcinoma, and lung adenocarcinoma.

Methods: We conducted an analysis of FAM72 expression levels in ccRCC tissues and normal kidney tissues using TCGA data. We performed univariate and multivariate Cox regression analysis to assess the prognostic value of FAM72 expression. Furthermore, to find enriched biological processes connected to FAM72 expression, Gene Ontology (GO) and Gene Set Enrichment Analysis (GSEA) were used. We also examined the degree of methylation and immune cell infiltration in patients with ccRCC.

Results: Our bioinformatic analysis revealed that FAM72 expression levels were significantly higher in ccRCC tissues than in normal kidney tissues. High expression of FAM72 was associated with poor prognosis in ccRCC patients and was found to be an independent prognostic factor for ccRCC. GO and GSEA analyses indicated that FAM72 was enriched in biological processes related to mitosis, cell cycle, and DNA metabolism. Moreover, a significant correlation was found between FAM72 and immune cell infiltration and the level of methylation in ccRCC patients.

Conclusion: Our findings suggest that FAM72 could serve as an unfavorable prognostic molecular marker for ccRCC. A comprehensive understanding of FAM72 could provide crucial insights into tumor progression and prognosis. The results not only contribute to the understanding of FAM72's role in ccRCC but also pave the way for future research aimed at exploring the therapeutic potential of targeting the FAM72 gene family. The development of targeted therapies that modulate FAM72 expression or function could offer a novel approach to improving treatment outcomes for ccRCC patients.

Organophosphorus flame retardants (OPFRs) are high-production volume chemicals. Recent reports reveal that OPFRs are ubiquitous in the environment. Unfortunately, the toxicity profiles for OPFRs on organisms remain limited. Concerns over possible toxicity are growing as organophosphorus flame retardants have been developed and used more frequently. The majority of research on possible toxicity to date has concentrated on simple phosphate esters, which can comprise aryl, alkyl, or even halogenated phosphate esters in certain situations (which belong more appropriately in the category of organohalogen flame retardants).  The inclusion of several kinds of esters into a single study leads to muddled conclusions. Each class of phosphate esters should be subjected to toxicity assessment separately. Further, the potential toxicity of the more effective (lower level of oxygenation at phosphorus: phosphonates, phosphinates, phosphine oxides) organophosphorus flame retardants has been little explored. The few results available suggest that these compounds exhibit no or minimal toxicity (lower than that of phosphates). This represents an area that should be the focus of careful detailed studies to establish any potential toxicity. Studies of the toxicity of phosphonates, phosphonites and phosphine oxides, as separate classes, should be conducted. Reliable toxicity data for organophosphorus compounds as a function of structure are needed.

The present study investigates the role of oxidative stress-related genetic variants in type 2 diabetes mellitus-associated nephropathy. Type 2 diabetes is thought to be associated with microvascular complications that comprise retinopathy, nephropathy, and neuropathy. Oxidative stress is a predominant factor involved in the pathogenesis of DN and alters metabolic endeavour and its hemodynamic pathways, which have varied correlations with renal problems, one of which is diabetic nephropathy, which leads to end-stage renal disease. Renal injury in DN occurs primarily through oxidative stress, which disrupts metabolic and hemodynamic pathways. Hyperglycemia is regarded as a hallmark feature of diabetes that increases reactive oxygen species generation, which eventually leads to increased oxidative stress, and this is considered the most essential event in the onset of DN. To prevent tubular injury in DN, antioxidants can be used to combat oxidative stress, which is primarily caused by several pathways. The most significant antioxidative enzymes are superoxide dismutase, catalase, glutathione-S-transferase, and glutathione peroxidase. As a result, this chapter emphasizes antioxidant gene polymorphisms and hypothesizes that these antioxidant genes may be an essential component of DN pathogenesis. Moreover, this chapter also retorts to the research questions raised by the physicians and illustrates the importance of regional population studies on detecting the SNPs of antioxidant genes and targeting therapeutic approaches aiding to lessen the severity of the disease at its initial stages.

We synthesized a novel series of transition metal(II) complexes 5a-h by reacting key transition metals (Co, Cu, Zn, Ni) with the Schiff base 3, derived from (E)-N-(4-methylbenzylidene)-2-((Z)-(4-methylbenzylidene)amino)benzamide. Schiff base 3 was previously prepared by reacting 2-aminobenzohydrazide 1 with 4-methylbenzaldehyde 2. The structures of the metal complexes were characterized using IR, NMR, mass spectrometry, and elemental analysis. We evaluated the synthesized metal complexes for antioxidant, antimicrobial, and antifungal activities. Notably, compounds 5e and 5c exhibited enhanced antimicrobial activity compared to the free ligand. Compounds 5g and 5a showed significant activity against various bacterial strains. Additionally, the hydrated metal complexes 5b, 5d, 5f, and 5h demonstrated moderate to good antimicrobial activity. In terms of antioxidant activity, most of the metal complexes displayed moderate to good activity comparable to ascorbic acid. Our bioassay results highlighted compounds 5e and 5c as effective antimicrobial agents against highly resistant microbial strains.