GREEN SYNTHESIS, CHARACTERIZATION, AND ANTHELMINTHIC ACTIVITY OF NEWER QUINOLINE DERIVATIVES CONTAINING ACRIDINE MOIETY

  Objectives: Synthesis of newer 3,4,6,7-tetrahydro-3,3,6,6-tetramethyl-9-(2-chloro-6-substituted-quinolin-3-yl)-acridine-1,8(2H,5H,9H,10H)-diones were synthesized by reacting 5,5-dimethylcyclohexane-1,3-dione with substituted 2-chloro-quinoline-3-carbaldehyde in presence of ammonium acetate.Methods: Synthesis was carried out by microwave irradiation method and the synthesized compounds have been characterized using elemental analysis, FT-IR, 1H NMR, and 13C NMR spectroscopy and further supported by mass spectroscopy. Purity of all the compounds has been checked on thin layer chromatographic plate and high-performance liquid chromatography technique. All the synthesized compounds were tested for antibacterial and anthelminthic activities.Results: The results were revealed that the compounds AQ-4 and AQ-5 have showed good activity against both Gram-positive and Gram-negative bacteria. Compounds AQ-4 and AQ-5 showed moderate activity against all the organisms. However, all the derivatives have shown less antibacterial activity when compared to the standard drug amikacin. The compounds AQ-3 and AQ-5 showed good anthelminthic activity and compounds AQ-9 and AQ-10 showed moderate anthelminthic activity. However, all the compounds have shown less anthelmintic activity when compared to the standard drug albendazole.Conclusion: The study reveals that compounds containing quinoline derivatives with acridine moiety shown the antibacterial activity against the pathogens Bacillus subtilis, Bacillus cereus, Staphylococcus epidermidis, Salmonella typhi, Pseudomonas aeruginosa and Klebsiella pneumoniae. These derivatives also possess the good anthelmintic activity. The above green synthesis technique could be a right solution for industrial applications in the future and therapeutic needs

Molecular dynamics and Conformational flexibility in Heat Shock Protein 60.2 of Mycobacterium tuberculosis

HSP 60.2 plays important role in pathogenesis of Mycobacterium tuberculosis causing tuberculosis. This chaperonin comprises of three domains namely-apical, intermediate and equatorial which assists in proper protein folding thus preventing aggregation of unfolded polypeptides. To evaluate the structural changes during protein folding, conformations of HSP 60.2 were monitored during 10 ns time scale. Molecular dynamic simulations are used to study the large amount of molecular and biomolecular conformations with the use of high end computational assistance. The Principal component analysis and clustering techniques are used for revealing major conformational changes that occur in the MD simulation. Normal mode analysis was also performed to study the conformation and direction of motion of a protein under study for a large time scale simulation. These studies suggest that functional behavior of protein that depends on the structure. Chaperonin 60.2 is not only plays a role as protein folding machinery, but also an immunologically important biomolecule. Hence it is provided and drawn a clear path between role of chaperon in protein folding and their role in the infection showing the immunological importance of Heat Shock Protein 60.2

A Numerical Model for Analysis of Heat Transfer in MHD Casson Fluid with Radiation and Viscous Dissipation

This article is, concerned a numerical model for analysis of heat transfer (HT) in MHD Casson fluid (CF) with radiation and viscous dissipation. The governing PDE's are developed for the physical model and converted into non-dimensional form and then with the help of Galerkin finite element method (GFEM) solution is obtained. The impact of dimensionless parameters which are supervising the flow such as Magnetic parameter  , Casson parameter ( )  thermal Grashof number Permeability of porous medium    Prandtl number Heat absorption parameter  Viscous dissipation   and Radiation parameter  are analyzed through graphs for fluid properties. The  results obtained were compared with earlier reported results for correctnes

A Numerical Model for Analysis of Heat Transfer in MHD Casson Fluid with Radiation and Viscous Dissipation

This article is, concerned a numerical model for analysis of heat transfer (HT) in MHD Casson fluid (CF) with radiation and viscous dissipation. The governing PDE's are developed for the physical model and converted into non-dimensional form and then with the help of Galerkin finite element method (GFEM) solution is obtained. The impact of dimensionless parameters which are supervising the flow such as Magnetic parameter  , Casson parameter ( )  thermal Grashof number Permeability of porous medium    Prandtl number Heat absorption parameter  Viscous dissipation   and Radiation parameter  are analyzed through graphs for fluid properties. The  results obtained were compared with earlier reported results for correctnes

QUANTITATIVE DETERMINATION OF RESIDUAL SOLVENTS IN PALONOSETRON API BY HS-GC METHOD

Objectives: Palonosetron is an antidote to 5-HT3 in the prevention and treatment of chemotherapy-induced nausea and vomiting (CINV). The presence of residual solvents in pharmaceutical drug substances or products, as well as excipients, can have a detrimental effect on the product’s quality and stability. These substances must be evaluated for safety and efficacy. The primary purpose of this work is to establish a method for validating and quantifying residual solvents in palonosetron API using Head Space Gas Chromatography (HS-GC). Methods: In the proposed HS-GC technique for the quantifying residual solvents - ethanol, acetone, methanol, acetonitrile, and isopropyl alcohol (IPA) in Palonosetron API, the headspace equilibrium was achieved at 100°C and analyzed by DB-624 column (30 m × 0.24 mm, 1.8 μm) with injector and detector temperature set at 200°C and 230°C respectively. The dissolving solvent was dimethyl sulfoxide (DMSO). After the initial holding time of 5mins, the temperature was increased to 120°C from 40°C in 20mins at a rate of 10°C/min using a flow rate of 10 ml/min and a split ratio of 1:25 with nitrogen as carrier gas. The approach created has been validated and quantified as per International Conference on Harmonization’s (ICH) guidelines. Results: All the results obtained were within the ICH specified limits. The validation results for repeatability studies (%RSD values) were found to be <10; recovery studies values were in the range of 90–110% and for the selected linearity range 25–150 μg/ml the correlation coefficients(γ2) for all the solvents were observed to be >0.99. Conclusion: A sensitive, simple, precise, and economic HS-GC method with Flame Ionization Detector (FID) was developed and validated to quantitatively determine the residual solvents in Palonosetron API

Identification of causative pathogen and its antibiotic sensitivity in cases of preterm premature rupture of membranes

Background: Pre-labor rupture of membranes is defined as amniotic membrane rupture before the onset of labor contractions, and if it happens before 37 weeks, it is called preterm premature rupture of membranes (PPROM). Several organisms commonly present in the vaginal tract are E.coli, Group-B streptococci, staphylococcus aureus, chlamydia trachomatis, Gardnerella vaginalis and Enterococcus faecalis which secrete proteases that degrade collagen thereby weakening  the fetal membranes leading to PPROM. Appropriate antibiotic therapy has a significant role in the prevention and treatment of maternal and neonatal complications.Methods: This was a prospective observational study done in the department of obstetrics and gynaecology, Narayana medical college, Nellore. Selectively 100 patients with complaint of PPROM admitted to labor room were included in the study. Diagnosis of membrane rupture was established by speculum examination, and high vaginal swabs are taken and sent to laboratory for identifying bacteria using gram staining and cultured in aerobic and anaerobic methods. Antimicrobial susceptibility testing of the organisms was performed by disk diffusion method by Kirby and Bauer.Results: Out of 100, high vaginal swabs had growth in 82 patients, and 18 were sterile. The repeatedly isolated organism in patients with PPROM is E.coli amounting 32%, followed by candidal species 20%. Staphylococci are scoring 11% and enterococci 8%. However, organisms like gardenella vaginalis and Group B streptococcus are least common with a score of 6% and 5% respectively. In this study, E.coli is highly sensitive to tigecycline, colistin 100% each and highly resistant to gentamycin and amikacin.Conclusions: In this study, E.coli is related to the maximum number of cases with preterm premature rupture of membranes. Appropriate use of antibiotics significantly lowers maternal morbidity and neonatal mortality

Assessment of knowledge, awareness, practices and misconceptions among hypothyroid and hyperthyroid patients

Background: In chronic illness there is a greater need for patient education to manage their symptoms, prevent complications, and have better therapeutic outcome and increase quality of life. Among chronic illnesses thyroid disorders are more common in the world. Our study aimed to assess knowledge, awareness, practices and misconceptions in thyroid patients in order to estimate the need of patient education and also counsel the patients for the same using counselling aids. Methods: A descriptive cross sectional study was conducted among 300 subjects in a secondary care hospital for a period of 6 months (February 2017- July 2017). The interviews were conducted in semi private areas in the hospital after taking informed consent by using a structured questionnaire which has been established for its validity and reliability. The results were calculated using descriptive statistical methods (frequency, percentage and mean). Results: Among the participants 23.33% were co-morbidities, majority of patients (83%) do not have family history. Only 32% of the participants have good knowledge, 52.66% have average knowledge and 15.33% patients have poor knowledge about symptoms. Though the knowledge on the dietary factors is considerable in participants, 31.95% of hypothyroid, 58.82% of hyperthyroid patients followed inappropriate dietary habits. 86.3% believed that patients with thyroid disorders need to take medications for their lifetime. Conclusions: The results conclude the need for patient education in thyroid disorders and also a need for clinical pharmacists in hospital setup to fill the gap between physician and patient to provide patient education and clarify misconceptions.