An insight into sustainable and green chemistry approaches for the synthesis of quinoline derivatives as anticancer agents.

Quinolones, a key class of heterocyclics, are gaining popularity among organic and medicinal chemists due to their promising properties. Quinoline, with its broad spectrum of action, plays a primordial role in chemotherapy for cancer. Drugs include lenvatinib and its structural derivatives carbozantinib and bosutinib, and tipifarnib are the popular anticancer agents. Owing to the importance of quinoline, there are several classical methods for the synthesis such as, such as Gould-Jacobs, Conrad-Limpach, Camps cyclization, Skraup, Doebnervon Miller, Combes, Friedlander, Pfitzinger, and Niementowski synthesis. These methods are well-commended for developing an infinite variety of quinoline analogues. However, these procedures are associated with several drawbacks such as long reaction times, use of hazardous chemicals or stoichiometric proportions, difficulty of working up conditions, high temperatures, organic solvents, and the presence of numerous steps, all of which have an impact on the environment and the economy. As a result, researchers are working hard to develop green quinoline compounds in the hopes of making groundbreaking discoveries in the realm of cancer. In this review, we have highlighted significant research on quinoline-based compounds and their structure-activity relationship (SAR). Furthermore, because of the significant economic and environmental health and safety (EHS) concerns, more research is being dedicated to the green synthesis of quinolone derivatives. The current review offers recent advances in quinoline derivatives as anticancer agents for green synthesis using microwave, ultrasound, and one-pot synthesis. We believe that our findings will provide useful insight and inspire more green research on this framework to produce powerful and selective quinoline derivatives.

FT-IR fingerprinting as an Analytical tool for determination of Melamine leaching from Melamine tablewares and their Biological implications.

In recent years Melamine is upgraded as a type three carcinogen. It is a sorry fact that still; people are in the fantasy mode and abaft the melamine tableware as they are a good piece of decorative material which sets dining an opulent look. The present study focuses on the determination of melamine leaching from melamine tablewares. The food stimulants culled for this study are conventional Indian cuisines. FT-IR is used as an analytical tool to determine the leaching of melamine from melamine diners. The present study reveals melamine leaching when hot food articles are in contact with melamine wares. Microwave heating is unsuitable for melamine tablewares. This is the first report in India, on the leaching of melamine from melamine tablewares. Calf thymus (ct) DNA is added to the samples and the extent of DNA damage in vitro is analyzed by Comet assay (also called Single cell gel electrophoresis). The results from comet assay portray significant DNA damage with the treated samples. This is a vigilance study that helps the mundane man to avoid such decorative materials and to voluntarily move to our traditional dining culture.

Antimicrobial and antioxidant activities and chemical profiling of Curvularia tsudae endophytic in Cynodon dactylon (L.) Pers.

There is a growing body of evidence that endophytic fungal metabolites possess important biological activities. Cynodon dactylon (L.) Pers., a well-known grass species with potential medicinal properties, is under-explored for the diversity of endophytic fungal species and their metabolites. We report here the diversity of endophytic fungi in the culm, leaf and inflorescence of Cynodon dactylon when cultured on moist blotter (MB), potato dextrose agar (PDA) and malt extract agar (MEA). Species richness, Shannon and Simpson diversity and evenness indices showed that PDA followed by MEA supported the growth of the largest number of fungal species. Amongst four fungal species tested, Curvularia tsudae was selected for further studies on antimicrobial and antioxidant activities. The mycelial mat (MM) and culture filtrate (CF) of PD broth grown Curvularia tsudae extracted with ethyl acetate and methanol, respectively, were subjected to antimicrobial assay against five bacterial and four fungal test isolates. Results indicated that the ethyl acetate extract of CF had moderate activity against Enterococcus faecalis, Escherichia coli, Pseudomonas fluorescence and Staphylococcus aureus whereas the methanolic MM extract showed high to moderate activity to Aspergillus flavus, A. niger and Fusarium oxysporum. Cyclic voltammetric analysis of ethyl acetate extract showed very good antioxidant activity and the extract contained coumarins when determined by HPLC. High-resolution orbitrap LC-MS of ethyl acetate extract revealed the presence of metabolites with antimicrobial and antioxidant and other biological activities. Finding of the present study suggested that Curvularia tsudae could be exploited for pharmaceutical applications.

Understanding the etiopathogenesis and diagnosis of malignancy in the framework of Ayurveda: A review based on experience of working in an institute of oncology.

BACKGROUND: The etiopathogenesis and diagnosis of cancer has intrigued modern oncology researchers for decades, and it is still a rapidly growing area in medicine. Cancer is not a single disease, but rather a collection of related diseases which is diagnosed on the basis of aberrant cellular changes. Since this is established by the modern medical science, it becomes important to understand it from the perspective of Ayurveda. Despite the fact that there are a few endeavors in this area, there is no common agreement among the experts. The current article is an effort to fulfill this knowledge gap. AIMS AND OBJECTIVES: To understand the cancer systematically in the frame work of Ayurveda and propose its probable Samprapti (pathogenic process) based on clinical observations. MATERIALS AND METHODS: It is based on the clinical observation and detailed examination of 400 cancer patients, following modern and Ayurvedic methods in an institution dedicated to oncology. RESULTS: After careful study of each type of cases of cancer at its all stages to understand the natural history and clinical behavior, Ayurvedic pathogenesis, diagnosis with possible etiologic association has been arrived at. Three main conditions, namely Udara (enlargement of abdomen), Gulma (lump in abdomen) and Vidradhi (abscess) can be equated with cancer. CONCLUSION: Modern diagnosis of cancer cannot be equated with any single disease entity mentioned in the Ayurvedic literature. Udara-Gulma-Vidradhi is the abdominal tumors present as benign and possess cancerous potential.

Assessment of dental anxiety and its correlation with denture satisfaction in edentulous patients.

OBJECTIVE: The objectives of this study were to measure the level of dental anxiety and its correlation with dental history, denture satisfaction and other variables. MATERIALS AND METHODS: A cross-sectional study was conducted on 150 completely edentulous patients reporting to the Department of Prosthodontics, KLES's Institute of Dental Sciences, Belgaum, over a period of 17 months (August 2005 to March 2007). The anxiety level of the patients was assessed with the help of a questionnaire, after obtaining an informed consent. Reliability of the dental anxiety scale was assessed by means of coefficient alpha. RESULTS: The results of this study concluded that dental anxiety scale for edentulous patients was a reliable scale for measuring dental anxiety. The anxiety score was higher for female than male patients. A significant correlation was found between denture satisfaction score and anxiety. DISCUSSION: Anxiety plays a major role in denture satisfaction. The variables included: Previous denture experience, occupation, medical history, age, gender, dental anxiety scale, period of edentulousness, age of previous dentures, number of complete dentures, denture satisfaction score, and the score on the Hamilton anxiety scale. CONCLUSION: The study indicated that gender correlates significantly with dental anxiety. Patients with medical history were found to be more anxious than normal patients. Patients with higher anxiety values were less satisfied with the treatment. Lastly, subjects with higher general anxiety showed greater values on the dental anxiety scale. CLINICAL SIGNIFICANCE: The assessment of dental anxiety will help the prosthodontist in the management of anxious patients and secondly to provide evidence-based research into this psychological construct which has been shown to predict dental avoidance.

Ayurvedic identification and conceptual analysis of cancer.

Modern oncology is a rapidly growing area in medicine. Cancer is a disease diagnosed on the basis of cellular changes hence objectivity takes the lead. Clinical observation, detailed examination and some feasibility studies were conducted in Ayurvedic methods to understand and identify cancer systematically. Abdominal presentation as tumour is discussed since it is one of the major area for clinical diagnosis of cancer. More than 100 cases were followed in each type at all stages to understand the natural history and clinical behaviour. After careful study, the Ayurvedic diagnosis with possible aetiologic association has been arrived at and discussed. Three main classification has been made and presented separately. Visha concept of Ayurveda has been very closely found to be associated in malignancy.