Results and discussion Stirring of L with 4-methylaniline and 4-methoxyaniline in equimolar proportion in water at room temperature for 72 h without any Lewis acid catalyst gives L.H2O and L respectively (Scheme 1). The yield of L.H2O is 90% and that of L 70%. These are obtained in 60% yield when the reactants are refluxed in water for 14 h. But the yield goes on decreasing when increasingly more refluxing time is used. Earlier Moody et al have [5] studied opening of the epoxide ring in L in connection with their total synthesis of the pentacyclic marine alkaloid ascididemin from 1,10-phenanthroline (phen).
The reported melting point for acetanilide is 114.3°C, meaning that my range provides support that the product obtained was what was desired. Next, a TLC plate was run to evaluate if the reaction was successful. I spotted three lanes on my plate, diluted pure aniline, diluted pure acetanilide product, and a co-spot of them both for reference. Ethyl acetate was used to dilute the sample to attempt to minimize streaking and I used a developing solvent of 80% ethyl acetate and 20% hexane. There was no starting material present in the product lane, meaning the reaction ran to completion.
The effect of DMBQ against S. typhimurium cells was bacteriostatic for the first 5 h of incubation after addition of the compound. The bactericidal effect DMBQ was observed against S. aureus after 12 h of incubation. Thus, doubling the MIC of DMBQ reduced the growth rate of S. aureus but did not have a siginificant effect on the final cell
An average daily dose of silymarin (420 mg/day for 41 months) was found to be non-toxic, relative to placebo, in clinical trials1. Taxifolin , silychristin, isosilychristin, and Silydianin, did not show cytotoxicity at 100 mM. Isosilybin B, which showed the highest potential as an antiproliferative agent against human prostate carcinoma cells, was toxic to cells above 10 mM9. Neither milk thistle nor silymarin are listed in the EPA's Toxic Substances Control Act (TSCA) Inventory. No studies or case reports investigating the association of exposure to milk thistle extract and cancer risks in humans were identified in the available literature12.
1.2 Statistical Testing A –Correlation check between the Start measure and End measure for those given Calcium. When running a simple scatterplot diagram so as to visually check the correlation of start and end measure for calcium, it would appear that there is no obvious correlation. Calcium Correlationsa Starting Value End Value Starting Value Pearson Correlation 1 .602 Sig. (2-tailed) .065 N 10 10 End Value Pearson Correlation .602 1 Sig. (2-tailed) .065 N 10 10 a.
The anticancer activity of samples on HepG2 was determined by the MTT assay (Mosmann 1983). Cells (1 × 105/well) were plated in 1ml of medium/well in 24-well plates (Costar Corning, Rochester, NY). After 24, 48 and 72 hours incubation the cell reaches the confluence. Then, cells were incubated in the presence of various concentrations of the samples in 0.1% DMSO for 48h at 37°C. After removal of the sample solution and washing with phosphate-buffered saline (pH 7.4), 200µl/well (5mg/ml) of 0.5% 3-(4, 5-dimethyl-2-thiazolyl)-2, 5-diphenyl--tetrazolium bromide cells (MTT) solution was added.
PREFORMULATION STUDIES Standard calibration curve In the pre-formulation studies, the λ max of Itraconazole by spectrophotometric method in phosphate buffer pH 6.8 was found to be 262nm. Table no. 1.7: Calibration Curve of Itraconazole in Phosphate Buffer pH6.8 S.no. Concentration (µg/ml) Absorbance 1 0 0 2 2 0.12 3 4 0.26 4 6 0.38 5 8 0.44 6 10 0.57 Fig 1 : Standard Graph of Itraconazole in Phosphate Buffer pH6.8 Drug excipient compatibility study Fig 2: FTIR spectra of Itraconazole Fig 3: FTIR spectra of Itraconazole final formulation CHARACTERIZATION OF TRANSFERSOMES EVALUATION OF TRANSFERSOMAL GEL Vesicle shape and type: The surface morphology was studied by Optical Microscopy. The shapes of most of
Distribution The mean volume of distribution (Vss) of meloxicam is approximately 10 L. Meloxicam is ~ 99.4% bound to human plasma proteins (primarily albumin) within the therapeutic dose range. The fraction of protein binding is independent of drug concentration, over the clinically relevant concentration range, but decreases to ~ 99% in patients with renal disease. Meloxicam penetration into human red blood cells, after oral dosing, is less than 10%. Following a radiolabeled dose, over 90% of the radioactivity detected in the plasma was present as unchanged meloxicam. Meloxicam concentrations in synovial fluid, after a single oral dose, range from 40% to 50% of those in
Staphylococcus aureus, Candida albicans and Aspergilus niger. Growth was not observed on the test sample plates whereas standard culture plates showed growth. The plant material taken for the studies observed to be pathogen free and also free from any bacterial and fungal contamination as showed in Table 9.At the initial stage we evaluated Antibacterial and Antifungal activities of aqueous as well as ethanolic extracts of Vitex negundo leaves, Emblica officinalis bark and Tridax procumbens plant. All the extrats showed most prominent zone of inhibition against a number of bacterial strains like Escherichia coli, Bacillus subtilis, Staphylococcus aureus and Pseudomonas aerµginosa in comparison to the standard drug Penicillin. All the extrats showed most prominent zone of inhibition against fungal strains like Candida albicans and Aspergillus niger when compared with standard drug Nystatin.
The eluate was further loaded on Macro-Prep High-Q medium using similar protocol and the eluate so obtained was allowed to equilibrate overnight and later loaded onto third column Macro-Prep CM at pH 4 and eluted with linear gradient of 0-1 M NaCl. The active fractions were concentrated in an Amicon ultrafiltration cell using a 10 kDa cutoff membrane. Ashraf and Hussain (2010) had attempted crude fractionation of radish peroxidase using ammonium sulphate. This technique has its own limitations and hence not used in commercial manufacturing. Aruna and Lali (2001) attempted to isolate peroxidase from the roots of Raphanus sativus using CM cellulose in the form of soluble ion-exchange macroligand to precipitate most