Posted by admin on Aug 31, 2015 in |
E7010 (N-[2-[(4-hydroxyphenyl)amino] – 3 pyridinyl] – 4 -methoxybenzenesulfonamide), an orally active sulfonamide antitumor agent that is currently in a Phase I clinical trial, showed rather consistent growth-inhibitory activities against a panel of 26 human tumor cell lines (IC50 = 0.06–0.8 µg/ml), in contrast to vincristine (VCR; IC50 = 0.0002–0.04 µg/ml), 5-fluorouracil (IC50 = 0.2–30 µg/ml), Adriamycin (IC50 = 0.002–0.7 µg/ml), 1-β-D-arabinofuranoxylcytosine (IC50 = 0.005 to >30 µg/ml), camptothecin (IC50 = 0.002–0.4 µg/ml), and cisplatin (IC50 = 0.5–20 µg/ml). It caused a dose-dependent increase in the percentage of mitotic cells in parallel with a decrease in cell proliferation, like VCR. It also showed a dose-dependent inhibition of tubulin polymerization, which correlated well with the cell growth-inhibitory activity. 14C-labeled E7010 bound to purified tubulin, and this binding was inhibited by colchicine but not by VCR. However, its binding properties were different from those of colchicine, as well as those of VCR. E7010 was active against two kinds of VCR-resistant P388 cell lines, one of which showed multidrug resistance due to the over expression of P-glycoprotein (resistant to Taxol), and...
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Posted by admin on Aug 31, 2015 in |
A novel, simple, rapid and sensitive UV spectrophotometric method has been developed for simultaneous estimation of Gemcitabine and Tamoxifen. Gemcitabine and Tamoxifen show maximum absorbance at 269 nm and 238 nm respectively. The method employs first order derivative method. Here in this method, TAM show zero absorbance i.e Zero Crossing Point (ZCP) at 285 nm and at this wavelength GEM show measureable absorbance and ZCP of GEM is 224 nm and at this wavelength TAM show measurable absorbance. So absorbance of GEM and TAM is measured at 285 nm and 224 nm respectively. Both the drugs obey Beer’s Law in the concentration ranges employed for this method. R2 value of GEM and TAM was found to be 0.996 and 0.998 respectively. Accuracy and reproducibility of the proposed method was statistically validated by recovery studies. Limit of detection and (LOD) and limit of quantification (LOQ) of GEM was found to be 0.02833 and 0.08586 respectively. LOD and LOQ of TAM was found to be 0.09565 and 0.2898 respectively. The method...
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Posted by admin on Aug 31, 2015 in |
A simple, economical, specific, accurate, precise and validated Reverse phase high performance liquid chromatography (RP-HPLC) method has been developed for simultaneous estimation of Phenylepherine hydrochloride (PPEH) and Cetirizine hydrochloride (CETH) in combine dosage form. The chromatographic separation was achieved on Princeton SPHER C18 column (250 mm x 4.6 mm id, 5 μ particle size) at ambient temperature using mobile phase buffer (0.1 M Ammonium dihydrogen phosphate pH 5.2 ± 0.05) : Acetonitrile (50:50% v/v) at flow rate 1.0 ml/min. Quantification was achieved with UV detector at 225 nm. Retention time of Phenylepherine hydrochloride and Cetirizine hydrochloride were found to be 2.19 ± 0.05 minute and 4.16 ± 0.05 minute respectively. Linearity was studied in the concentration range 5-30 μg/ml and 10-60 μg/ml for Cetirizine hydrochloride and Phenylepherine hydrochloride respectively with a correlation coefficient of 0.9998 and 0.9998 respectively. The proposed method was validated according to ICH guidelines with respect to linearity, accuracy, precision, robustness, LOD, and LOQ. The developed method with good separation, successfully applied for determination of PPEH...
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Posted by admin on Aug 31, 2015 in |
This paper presents the synthesis and physical-chemical characterization of a new terpyridine (tpy) ruthenium complex coordinated to the L-type calcium blocker channels verapamil (vera) obtained from commercial pill. Elemental analysis (%C N H), infrared (IR) and ultraviolet-visible (UV-vis.) spectroscopy, mass spectrometry (MS), and 13CNMR (nuclear magnetic resonance), and HPLC (high performance liquid chromatography) confirmed the pure and structure of the ligand verapamil and of the ruthenium complex structurally designed as [RuIICl2(tpy)(vera)] Cyclic voltammetry aided investigation of the electrochemical behavior of [RuIICl2(tpy)(vera)] based in the metal ion redox potential. Verapamil ligand and [RuIICl2(tpy)(vera)] induced vascular relaxation in endothelium-intact and endothelium-denuded aortic rings. Verapamil drug and [RuIICl2(tpy)(vera)] complex coupled to verapamil elicited similar pharmacological results. The calcium ion chelating effects (Kd) promoted for verapamil ligand and [RuIICl2(tpy)(vera)] complex were found based in the fluorescence technic. The smooth muscle cell images studied to [RuIICl2(tpy)(vera)] complex acting as a luminescent agent important as biological...
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Posted by admin on Aug 31, 2015 in |
This study was carried out to evaluate the effect of boiling on amino acids contents of the fruits of four species of the family Cucurbitaceae which were Cucurbita maxima D, Cucurbita pepo L, Cucurbita moschata and Lagenaria siceraria variety supreme court. In this study, fresh fruit of the four species were subjected to conventional processing technique which is boiling as well as drying. The dry and boiled fruits were evaluated for essential and nonessential amino acids content as well as total amino acids. Amino acids profile of boiled and dry fruits showed the presence of eight essential and nine non essential amino acids. The four species recorded a considerable amount of proline as follows: L. s. uncooked (370 mg/100gm), C. mo. uncooked (318 mg/100gm) L. s. cooked (258.8 mg/100gm), C. p. uncooked (232mg/100gm) and C. p. cooked (208mg/100gm). The highest total amount of amino acids of boiled fruits was recorded in Lagenaria siceraria (4977.6mg/100gm) followed by Cucurbita pepo (2870.1mg/100gm) where as the lowest was recorded in Cucurbita maxima (1427mg/100gm). ...
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