AN OBSERVATIONAL STUDY ON NIDANARTHAKARA ROGA SIDDHANTA W.S.R. TO PRATISHYAYAT SANJAYTE KASA

Nidan (causative factor) plays important role in course and onset of any disease. Many times one disease may become the cause of another disease. The concept is explained by Acharya Charaka under the heading Nidanarthakara Roga. Further he has narrated the examples of Nidanarthakara roga as Pratishyaya, Kasa, Kshaya, Shosha, Udara etc. In day to day practice it is very important to know the Nidanarthakaratwa of any disease. It not only leads to development of another disease but also hampers the immunity of patient also. The present observational study was carried out with the prime aim of assessing Nidanarthakaratwa of Pratishyaya. The study included 60 patients between the age group 16-60 having the clinical sign and symptoms of Kasa. Along with general observations the observations relating previous history of Pratishyaya in Kasa patient were also noted to find out Nidanarthakaratwa of Pratishyaya in Kasa. The detail observations like course, onset and type of Nidan were also noted to find out Nidanarthakaratwa of Pratishyaya in Kasa Vyadhi. It was found that more than 50% patients of Kasa were previously suffered from Pratishyaya which supports the Charakokta Nidanarthakara Roga Siddhant Pratishyayat Sanjayte Kasa. The importance or scope of the present study is to make aware the people about Nidanarthakaratwa of Pratishyaya. Also early intervention is necessary in Pratishyaya and Dushta condition of Pratishyaya should not be neglected

Synthesis, in vitro biological evaluation and molecular docking study of coumarin-1,4-dihydropyridine derivatives as potent anti-inflammatory agents

The green chemistry approach provides for the synthesis of coumarin-1,4-dihydropyridine scaffolds 6a-o via sequential multicomponent reaction using catalytic amount of triethylamine (TEA). These new coumarin scaffolds have been successfully explored for the effective inflammatory as well as microbial infection inhibitors. The antimicrobial activity results of the title compounds have shown potent activity against both gram positive and gram negative bacterial, and fungal stains. Additionally, anti-inflammatory activity of all the compounds has been found to be quite promising in comparison with standard Diclofenac sodium. Furthermore, the in silico docking study has been performed for all the compounds with S. aureus DNA gyrase and cyclooxygenase-2 (PDB ID 4PH9). The computational results are in good agreement with the in vitro antibacterial and anti-inflammatory experimental results.

Synthesis, in vitro biological evaluation and molecular docking study of coumarin-1,4-dihydropyridine derivatives as potent anti-inflammatory agents

418-432The green chemistry approach provides for the synthesis of coumarin-1,4-dihydropyridine scaffolds 6a-o via sequential multicomponent reaction using catalytic amount of triethylamine (TEA). These new coumarin scaffolds have been successfully explored for the effective inflammatory as well as microbial infection inhibitors. The antimicrobial activity results of the title compounds have shown potent activity against both gram positive and gram negative bacterial, and fungal stains. Additionally, anti-inflammatory activity of all the compounds has been found to be quite promising in comparison with standard Diclofenac sodium. Furthermore, the in silico docking study has been performed for all the compounds with S. aureus DNA gyrase and cyclooxygenase-2 (PDB ID 4PH9). The computational results are in good agreement with the in vitro antibacterial and anti-inflammatory experimental results

Synthesis, molecular docking, and biological evaluation of methyl-5-(hydroxyimino)-3-(aryl-substituted)hexanoate derivatives

Beta-aryl keto hexanoic acids (5a-l) were synthesized efficiently, followed by esterification that afforded beta-aryl keto methylhexanoates (6a-l). The chemo-selective ketoxime beta-aryl methyl hexanoates (7a-l) were isolated in good yields. Spectroscopic methods were used to characterize the obtained moieties. The antioxidant, anti-inflammatory, and antibacterial properties of the effectively synthesized compounds 7a-l were also investigated. The anti-inflammatory activity of the compounds 7c, 7f, 7i, and 7l was excellent, with a low IC50 value at micromolar concentration, which was much better than the reference diclofenac. All synthesized compounds 7a-l were assessed for their in vitro antibacterial activity against S. aureus, B. subtilis and E. coli.  Most of the compounds exhibited promising activity against Gram-positive bacterial strain, compound 7i showed excellent activity compared to standard streptomycin and in the case of E. coli, compounds 7b, 7c, 7j, 7k and 7l have shown moderate activity. Further, the cytotoxic activities of the compounds were assessed against lung cancer cells (A549) by using MTT assay. The possible interaction mechanism of the molecules 7c and 7g with Gram-negative strain E. coli DNA gyrase B in complex with PDB ID: 4DUH was studied