Posted by admin on Nov 1, 2014 in |
Pesticide uses pose a serious threat to environment and public health owing to their persistence and tendency to accumulate in animal and plant tissues. The present investigation was conducted to analyze pesticide residues mainly HCH and DDT in field, and biological samples from the plantation areas of Northern Kerala, India and the extent of DNA damage in cattle was measured. Environmental samples mainly water and fodder and biological samples milk and blood were collected from study area. All samples were analyzed using Gas Chromatography with Electron Capture Detector and confirmed by Gas Chromatography with Mass Spectrometry (GC-MS). The extent of DNA damage was analyzed using COMET assay. Among samples analyzed, water samples revealed detectable pesticide residues. One water sample was detected with all HCH isomers, and two samples were detected with p,p’-DDD. Mean concentration (ppm) of total HCH and DDT were 8.073 × 10-4 and 3.51 × 10-5 respectively. Pesticide residues in fodder and biological samples were with below detectable level. Comet assay revealed significantly higher (p<0.05) percent DNA...
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Posted by admin on Nov 1, 2014 in |
Different prokineticin receptor antagonists, based on the triazinedione scaffold, were synthesized by a new efficient method. Here we demonstrated that 5-benzyl triazinediones substituted in position para of the benzyl group with halogens provide compounds endowed with interesting selectivity for the Prokineticin receptor 1 (PKR1). BRET technology indicates that such substitution results in increased affinity for the PKR1.The affinity for PKR2, always in mM range, was never significantly affected by the para-halogen-benzyl pharmacophores. The analog bearing a para-bromobenzyl pharmacophore (PC-25) displayed the highest affinity for PKR1 (~18 times higher than the reference PC-1 that bears a para-ethyl benzyl group) and the highest selectivity (~300 times). The other halogen substituted analogs (PC-7, PC-18 and PC-35), showed selectivity for PKR1 more than 100 times higher than for PKR2. Using transgenic mice lacking one of the two PKRs we demonstrated that all these compounds were able to abolish the Bv8-induced hyperalgesia in mice still expressing the PKR1 at doses lower than those necessary to abolish hyperalgesia in mice expressing only the PKR2. The...
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Posted by admin on Nov 1, 2014 in |
Promethazine hydrochloride, one of the most effective agents for treating motion sickness, mainly acts as a strong antagonist of H1 receptor (antihistamine) and it blocks the action of acetylcholine on the receptors (anticholinergic effect). The purpose of present work was a development of fast dissolving oral film of promethazine HCl to overcome the limitation of current routes of administration, to provide faster dissolution rate and increase patient compliance, especially for outpatient setting. The amount of drug was calculated according to the area of petri plate. The amount of drug was then used for the preparation of film by solvent casting method utilizing HPMC E3, HPMC E5, HPMC E15, and HPMC E50 as a film-forming polymers. The effect of plasticizers (PEG 200, PEG 400, PEG 600, glycerine, propylene glycol, triethyl citrate) and their concentration were tested for physicomechanical properties of casted films. Aspartame was used as a sweetener. The IR spectral studies showed no interaction between drug and polymer or with other additives. Using experimental design, the prepared formulations were...
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Posted by admin on Nov 1, 2014 in |
The objective of this study was to extract ursolic acid (UA) from Ocimum sanctum,to synthesize its derivatives and to examine the improvement of antioxidative activity. Present work involved structural modification of UA at the C-3 and C-28 positions. UA derivatives namely UA-4 and UA-7 with distinct property were synthesized. Comparative evaluation of anti-oxidant activity of UA, UA-4 and UA-7 using in vitro assays and lymphocyte model system involved: (i) inhibition of liposomal lipid peroxidation by UA and its derivatives (ii) assessment of trolox equivalent antioxidative capacity (TEAC) (iii) ABTS and DPPH radicals scavenging ability and (iv) cell death (MTT assay) under hydrogen peroxide (H2O2) induced oxidative stress. Moderate increase in antioxidant activity of compound UA-4 compared to UA was observed. In contrast, significant improvement in antioxidant activity of UA-7 was observed. To evaluate antioxidant effects on lymphocytes, we exposed cells with UA and its derivatives along with hydrogen peroxide. This was followed by measurement of cell viability by trypan blue exclusion assay and cell death using MTT assay. UA-7...
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Posted by admin on Nov 1, 2014 in |
A series of some new substituted quinolines were synthesized by Doebner reaction, a three component coupling of various aromatic amines with two aldehydes and phenyl pyruvic acid, the intermediate 2, 3-diary-6-acetyl-quinoline-4-carboxylic acids were reacted with various aromatic aldehydes in the presence of basic medium using Claisen-Schmidt condensation in order to afford the corresponding chalcones. The substituted chalcones, on condensation with hydroxylamine hydrochloride in ethanol furnished isoxazoles derivatives. Another quinolines derivative were synthesized in this study by using an aryl amines with acetylacetone as Combes reaction, Knorr reaction between an aryl amines and ethylacetoacetate with heating above 100 ºC, and Conrad-Limpach quinoline synthesis a thermal condensation of an aryl amines with ethylacetoacetate. The reaction progress for all synthesized compounds was checked by thin layer chromatography (TLC) and melting point techniques, the structure of synthesized compounds were confirmed using IR, 1HNMR, 13CNMR, and GCMS. All the compounds have been screened for their antibacterial and antifungal...
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