Posted by admin on Feb 28, 2021 in |
Benzofuranones and nitrogen mustards have been reported as highly potential alkylating agents; with this evidence, the synthesis of some benzofuranones fused with nitrogen mustards was planned and was subjected to in-vitro cytotoxic studies. Substituted benzofuranones were synthesized by condensation of 2-hydroxy benzaldehydes and substituted 2-hydroxy acetophenones and further fused with nitrogen mustards gave high yields of target compounds 2 – (2 – (2 – (Bis (2 -chloroethyl) amino) ethoxy) benzylidene) benzofuran-3(2H)-one derivative. The derivatives synthesized had various halo substitutions such as chloro, bromo, fluro and methyl chloro derivatives. These synthesized compounds were characterized by FTIR, 1H NMR and LCMS spectral studies. Further, the synthesized compounds were subjected to 3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyl tetrazolium bromide assay on human lung carcinoma cells, A-549 and breast cancer cells, MCF-7 for its in-vitro cytotoxic activity. All the synthesized compounds showed promising cytotoxic activity in which AN– O – 04, (Z) – 2 – (2 – (2 – (bis (2 -chloroethyl) amino) ethoxy) benzylidene) -5 – chloro – 6-methylbenzofuran-3(2H)-oneshowed minimum CTC-50 of 119.32 ± 8.98...
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Posted by admin on Feb 28, 2021 in |
The effect of constant lighting on the level of some hematological parameters and their daily dynamics was studied in male Wistar rats at the age of 6 months. It was found that staying in constant light for 3 weeks leads to a rise in hematocrit level, mainly due to an increase in the number of red blood cells, while a decrease in the oxygen-transporting properties of these cells is noted. An analysis of the diurnal dynamics of the studied parameters, it was found that the keeping of animals under constant illumination destroys the circadian rhythms of HGB, MCV, RDWc, PCT, MPV, PDWc, and MCHC. The destruction of the circadian rhythms found in control is most likely due to both a decrease in the level of melatonin in constant light and a violation of its own circadian rhythm in the absence of a pacemaker, which role is played by the alternation of light and...
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Posted by admin on Jan 31, 2021 in |
The present UV Spectrophotometric and RP-HPLC method was simple, accurate, precise, specific, and sensitive. Spectrophotometric method was developed in water and very useful for analysis of bulk drug and injection formulation. RP-HPLC method was developed in Phosphate buffer (pH 3.0 adjusted with orthophosporic acid) and acetonitrile (70:30) using column HiQsil C18 column (250 × 4.6 mm; 5 μm). Flow Rate: 1.0 ml / min. The method was validated for the determination of granisetron hydrochloride in bulk and parenteral dosage form. The standard solution of granisetron hydrochloride in water showed maximum absorption at 301 nm with correlation, slope, and intercept 0.9998, 0.04198, and 0.01255, respectively and the percentage recovery of the formulation was 99.965% by UV spectrophotometry. By RP-HPLC, the % RSD of intraday and interday precision was 0.82% and 1.40 %, respectively. The % means recovery amount of Granisetron hydrochloride in 80 %, 100%, 120% was 94.3%, 94.9%, 95.2%, respectively, which reflect that the method was free from the interference of the impurities and other additives during the estimation...
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Posted by admin on Jan 31, 2021 in |
The present study was designed to evaluate the anticancer potential as well as cytotoxity of Chloroform extract of Thulasivettilacv of Piper betle L. is an evergreen perennial creeper belonging to family Piperaceae, and known to possess numerous medicinal properties. Current study focuses on evaluating antiproliferative potentialities of Betel leaves. The antiproliferative effect was tested against two cancer cell lines HeLa and HT 29, while cytotoxity was tested against in a normal myoblast cell line, L6 by MTT assay. Five different concentration of the chloroform extract were used for this study. Qualitative phytochemical analysis of leaf extracts showed the presence of tannins, alkaloids, phenols, flavonoids and glycosides. HeLa cell lines exhibited less antiproliferative activity 25.8 µg/ml ± 0.05% viability at 100µg/ml of extract by MTT assay and the IC50 value was found to be 45.19 µg/ml. In case of HT 29 colon cancer cell line, chloroform extract of plant showed 30.32 ± 0.04% µg/ml viability compared with the L6 normal cell line was24.00 ± 0.08% µg/ml. The IC50 values were...
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Posted by admin on Jan 31, 2021 in |
Fatty acid vesicles are novel vesicles incorporating fatty acids which enhance the brain targeting efficiency when compared to conventional liposomes. This study’s objective was to prepare, characterize, and evaluate fatty acid vesicles for brain targeting of a water-soluble drug, atomoxetine HCl through nasal route. The atomoxetine HCl loaded fatty acid vesicles were prepared by using the reverse phase evaporation method using Phospholipon 90 H, oleic acid, and ethanol. Prepared formulations were evaluated for parameters like particle size (152.9 nm), drug entrapment (90.4%), zeta potential (-9.41 mv), and in-vitro release was found to be 98% up to 4 h. SEM results showed spherical shaped vesicles. The ability of the prepared atomoxetine HCl loaded fatty acid vesicles to deliver atomoxetine HCl through the nasal route was studied by ex-vivo studies using goat nasal mucosa, which showed sustained release of 51% of the drug up to 4...
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