Current Issue : October - December Volume : 2013 Issue Number : 4 Articles : 7 Articles
Steroidal esters of 17-oximino-5 androsten-3β-ol were synthesized from dehydroandrosterone acetate. These compounds were tested for their antiproliferating activity and 5α-Reductase inhibitory activity in comparison to finasteride. Decreased androgen levels have been found in serum of animals treated with newly synthesized compounds. These compounds have shown better cytotoxicity as comparison to the clinically used drug finasteride. Therefore these compounds can be useful in the treatment of androgen dependent disorders of prostate alone or by synergistic effect they can decrease the size of prostate due to their antiproliferating activity. The compound TRB-263 was synthesized from the diosgenin involving marker degradation, oximation, Beckmann rearrangement, acid hydrolysis, oximation and esterification. Analytical method for the synthesized compound (TRB-263) was developed using RP-HPLC. Octyldecylsilane column was selected and a rapid, sensitive HPLC method for determination of TRB-263 was optimized and validated. Optimized chromatographic conditions were achieved after a series of screening experiments with elution systems of acidified Phosphate Buffer-ACN, in various proportions. It was found that ACN and phosphate buffer of pH 3.0 gave better peaks than other mobile phase composition. Optimized chromatographic conditions consist of mobile phase Acetonitrile (ACN): Phosphate buffer (PBS) pH 3.0 in the ratio of 16:20 (%v/v). Retention time was found to be 3.9 min. for TRB-263 at flow rate of 1.0 mL/min. Bioanalytical method was developed in human plasma for simultaneous estimation of TRB-263 by RP-HPLC with UV detection at 236nm. The chromatographic conditions employed for bioanalytical method development were exactly the same as that of analytical method. For the bioanalytical method, Acetonitrile was used as a protein precipitant and the ratio of plasma: ACN (0.2: 1.8mL) was used for the extraction....
HPTLC method was developed and validated for estimation of tramadol HCl in human plasma by drug spiking method. Chromatographic separation was achieved on silicagel 60F254 aluminium plates (10 x 10 cm) as stationary phase, using mobile phase comprising toluene: 2-propanol: ammonia (8:2:0.1 v/v/v) with detection at 271 nm. The method was linear (r2>0.998) in the concentration range of 200-1000 ng/spot in human plasma. The % CV for interday and intraday precisions was 1.48-2.09% and 1.11-1.65%, respectively. The limit of quantification and the limit of detection were 75.08 ng/spot and 24.78 ng/spot, respectively....
The efficiency of oat bran and barley bran in lowering the induced hyperlipidemia and hypercholesterolemia in blood of male\r\nAlbino rats (Rattus rattus) was studied. Twenty rats were divided into four groups each consisted of five rats and fed the specified\r\ntest diets for eight weeks. The first group (G1) is the negative group which was fed basal diet, the second group (G2) was fed 1.0%\r\ncholesterol, was the third group (G3) fed 1.0% cholesterol and 10% oats bran, and the fourth group (G4) was fed 1.0% cholesterol\r\nand 10% barley bran. Feeding rats on 1% cholesterol significantly increased serum total cholesterol, low density lipoprotein, and\r\nvery low density lipoprotein and triglyceride and decreased serum high density lipoprotein. Furthermore, enzyme activity of\r\nalanine aminotransferase, aspartate aminotransferase, and alkaline phosphatase was increased, and lipid peroxide was increased,\r\nwhereas catalase and glutathione-S-transferase were decreased. Kidney functions parameters in the cholesterol supplemented\r\ngroup were elevated compared with the negative control. In addition, histological alteration in kidney, liver, heart, and testes was\r\nobserved, compared with the negative control. Hypercholesterolemic rats supplemented with oat bran and barley bran showed\r\nsignificant decrease in lipid parameters, significant increase in high density lipoprotein-cholesterol, improved antioxidant enzyme,\r\nand improved histopathology of kidney, liver, heart, and testes. In conclusion, both oat bran and barley bran had protective effects\r\nagainst induced hyperlipidemia and improved histological alterations.Oat bran appearedmore efficient than barley bran in lowering\r\nthe lipid profile levels in hypercholesterolemic rats....
It is not clear and little difficult to know that when a formulation administered, active principles in the formulation gain entry in to the systemic circulation or not. The present study was planned to acquire some preliminary data with regards to the absorption of bacoside from the Brahmi Ghrita formulation when administered orally in acute and chronic period. Brahmi Ghrita was administered for single dose i.e 1 day and also chronic dose for seven days to rats. Blood samples were withdrawn after 1 hr and 3 hr intervals of drug administration and presence of bacoside was detected in serum sample using High Performance Thin Liquid Chromatography.\r\nBacoside present in Brahmi Ghrita was found to get absorbed in to systemic circulation in both the groups. Maximum concentration in serum was seen in the animal after 1 hr of drug administration in comparison to animal after 3 hr of drug administration in both the acute and chronic phase. From the study it can be said that, phytochemical of the Brahmi Ghrita formulation do get absorbed in systemic circulation after 1 hr of drug administration. The simple, accurate, cost effective HPTLC method can be utilized to detect bacoside in serum....
Serum adrenal androgens (AAs), including androstenedione (?4A) and dehydroepiandrosterone sulfate (DHEAS), have been\r\nreported to be lower in female rheumatoid arthritis (RA) patients with early disease. Few data are available on hormonal status\r\nof women before the onset of clinical rheumatoid arthritis (pre-RA). A broad baseline panel of serum adrenal and sex steroids\r\nwas compared in 36 female pre-RA to 144 matched cohort control (CN) subjects to determine differences in their mean values\r\nand in patterns of hormonal correlations. Study subjects having lower versus higher baseline serum cortisol levels than the total\r\ngroupâ��s mean value were also analyzed separately to investigate differences in their hormonal levels and correlational patterns. In\r\ntotal subjects, mean (�±SE) ?4A level (nmol/L) was lower (P = 0.018) in 28 pre-RA cases (6.4�±0.40) versus 108CN(7.8�±0.28). The\r\nsignificant (P = 0.013) difference was restricted to 9 pre-RA versus 53CN subjects having lower cortisol levels (5.6 �± 0.73 versus\r\n8.0 �± 0.42 nmol/L, resp.). In total subjects, no significant difference was found between study subjects in their bivariate correlations\r\nof the hormonal panel variables, unlike results found in the subgroups stratified by lower versus higher cortisol levels. A subgroup\r\nof pre-RA females may have relative adrenal cortical insufficiency, as reflected by lower ?4A, especially observed among those\r\nsubjects with lower cortisol levels....
Introduction. Spectroscopic analysis of urine samples from laboratory animals can be used to predict the efficacy and side effects\r\nof drugs. This employs methods combining 1H NMR spectroscopy with quantification of biomarkers or with multivariate data\r\nanalysis. The most critical steps in data evaluation are analytical reproducibility of NMR data (collection, storage, and processing)\r\nand the health status of the animals, which may influence urine pH and osmolarity. Methods. We treated rats with a solvent, a\r\ndiuretic, or a nephrotoxicant and collected urine samples. Samples were titrated to pH 3 to 9, or salt concentrations increased up to\r\n20-fold.Theeffects of storage conditions and freeze-thawcycleswere monitored. Selected metabolites andmultivariate data analysis\r\nwere evaluated after 1H NMR spectroscopy. Results.We showed that variation of pH from 3 to 9 and increases in osmolarity up to\r\n6-fold had no effect on the quantification of the metabolites or on multivariate data analysis. Storage led to changes after 14 days\r\nat 4�°C or after 12 months at -20�°C, independent of sample composition. Multiple freeze-thaw cycles did not affect data analysis.\r\nConclusion. Reproducibility of NMR measurements is not dependent on sample composition under physiological or pathological\r\nconditions....
Fever is one of the most common clinical symptoms of many diseases. Qingkailing (QKL) injection is widely used in China as a\r\nclinical emergencymedicine due to its good antipyretic effects. It is a herbal formula which is composed by eight kinds of traditional\r\nChinese medicines (TCM). As a kind of typical multiple constituents and multiple actions of TCM, it is very difficult to elaborate\r\nthe antipyretic mechanism by conventional pharmacological method. Metabonomics technique provides beneficial tool for this\r\nchallenge. In this study, an ultra performance liquid chromatography quadrupole time-of-flight mass spectrometry (UPLC QTOF/\r\nMS) metabonomics method was developed to explore the changing process of biochemical substances in rats of yeast-induced\r\npyrexia. Partial least squares discriminate analysis (PLS-DA) was used to distinguish the normal control group, the pyrexia model\r\ngroup, and the pyrexia model group treated by QKL injection.The potential biomarkers related to pyrexia were confirmed and\r\nidentified.MetPA was used to find the possible metabolic pathways.Theresults indicated that the antipyretic effect ofQKL injection\r\non yeast-induced pyrexia rats was performed by repairing the perturbed metabolism of amino acids....
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