PRODRUGS AND DERIVATIVES OF ALPHA, BETA-UNSATURATED KETONES DESIGNED AS ANTICANCER AGENTS

In the chemotherapy of cancer, a number of different classes of drugs are used. Of these, alkylating agents constitute about 30% and while a few of the less common cancers can be effectively treated by chemotherapy or adjuvant therapy, the drugs are marked by lack of specificity and high toxicity. Moreover, the vast majority of cancers cannot be treated satisfactorily by any therapy at all. Therefore, there is a need for better and more selective anticancer drugs. The present project may be considered to consist of the following two areas. I) Design, synthesis and antineoplastic evaluation) of novel candidate antineoplastics of the type- a) Mannich bases and related compounds. b)0G,13-Unsaturated ketones and their derivatives. II) Physicochemical, stability and in vitro studies of selected compounds. The compounds were designed as alkylating agents so that they would alkylate important biomacromolecules in the rapidly proliferating cancer cells. They were, therefore, either strong alkylators per se or were designed to generate such a species in vivo

Optimization Of Process Parameters For Reduced Thickness Cigses Thin Film Solar Cells

With the advent of the 21st century, one of the serious problems facing mankind is harmful effects of global warming. Add to that the ever increasing cost of fuel and the importance of development of clean energy resources as alternative to fossil fuel has becomes one of the prime and pressing challenges for modern science and technology in the 21st century. Recent studies have shown that energy related sources account for 50% of the total emission of carbon dioxide in the atmosphere. All research activities are focused on developing various technologies that are capable of converting sunlight into electricity with high efficiency and can be produced using a cost-effective process. One of such technologies is the CuIn1-xGaxSe2 (CIGS) and its alloys that can be produced using cost-effective techniques and also exhibit high photo-conversion efficiency. The work presented here discusses some of the fundamental issues related to high volume production of CIGS thin film solar cells. Three principal issues that have been addressed in this work are effect of reduction in absorber thickness on device performance, micrononuniformity involved with amount of sodium and its effect on device performance and lastly the effect of working distance on the properties of molybdenum back contact. An effort has been made to understand the effect of absorber thickness on PV parameters and optimize the process parameters accordingly. Very thin

Identification of Major Degradation Products of Ketoconazole

Analytical methods were developed for the identification of major degradation products of Ketoconazole, an antifungal agent. The stressed degradation of Ketoconazole drug substance was performed under acid, base, thermal, photo and oxidative stress conditions. The major degradation was observed under acid, base and oxidative stress conditions. The degradation study was performed on Inertsil ODS-3V, length 100 X diameter 4.6 mm, particle size 3 μm column using gradient method. These degradants were identified by LC-MS technique

Influence of supercoiling on the disruption of dsDNA

We propose that supercoiling energizes double-stranded DNA (dsDNA) so as to facilitate thermal fluctuations to an unzipped state. We support this with a model of two elastic rods coupled via forces that represent base pair interactions. Supercoiling is shown to lead to a spatially localized higher energy state in a small region of dsDNA consisting of a few base pairs. This causes the distance between specific base pairs to be extended, enhancing the thermal probability for their disruption. Our theory permits the development of an analogy between this unzipping transition and a second order phase transition, for which the possibility of a new set of critical exponents is identified

Imaging diagnosis of primary pelvic hydatid: a rare case report

Hydatid disease is caused by Echinococcus granulosus a commonly encountered parasitic infection to humans in tropical countries. Humans are accidental intermediate hosts of Echinococcus. Liver is the most commonly infected organ. Any organ of the body can be affected but primary pelvic hydatid disease is rarely reported. Preoperative diagnosis can be established by imaging studies such as ultrasonography, computed tomography (CT), and magnetic resonance imaging (MRI). Here, a case is reported of pelvic hydatid in a young female who presented with recurrent episodes of abdominal pain along with an abdominal mass. General physical examination and radiological evaluation confirmed a multiloculated cystic lesion in pelvic. Patient was subjected to laparotomy which confirmed the diagnosis of a primary pelvic hydatid disease

Infected Thyroglossal Duct Cyst Involving Submandibular Region: A Case Report

Thyroglossal duct cyst presents most frequently in the midline of the neck, either at or just below the level of the hyoid bone. They generally manifest as painless neck swelling, and they move on protrusion of tongue and during swallowing. A case of thyroglossal cyst was reported in the left submandibular region in a 14-year-old girl, above the level of hyoid bone; ultrasound examination favored a cystic lesion which moved in a vertical fashion on swallowing whereas fine needle aspiration cytology report was suggestive of simple cystic lesion of thyroglossal cyst. No lymphoid or malignant cells were present. The cyst was excised completely by surgical procedure under general anesthesia. Histopathological analysis revealed thyroglossal cyst showing columnar and flattened epithelium of cyst with focal aggregate of chronic inflammatory cells supported by fibrocollagenous cyst wall. The clinical, ultrasound, and histopathological findings suggested that the lesion was an infected thyroglossal cyst. There was no evidence of recurrence 6 months after surgery

Evaluation of the anti-depressant potential of metformin in conditioned defeat model in golden Syrian hamsters

Background: Depression is a prevalent mood condition that has an impact on daily functioning. Globally, depression affects 264 million people. The current pharmacotherapy of depression has a lot of shortcomings. Therefore, there is a need to explore newer therapy that alleviate the symptoms of depression. Metformin was found to possess antioxidant potential and hypothesized to decrease the levels of branched-chain amino-acids essential for tryptophan uptake (precursor for serotonin synthesis). The study was designed to validate the efficacy of metformin as an anti-depressant in conditioned defeat model in male golden Syrian hamsters using open field test (OFT), forced swim test (FST) and Serum serotonin levels. Methods: After obtaining IAEC approval, the study was carried out using 8 golden Syrian hamsters each that were randomly assigned to four groups. The disease control group received 1mL normal saline, positive control was given fluoxetine 12 mg/kg, two groups of metformin 240 mg/kg given pre-insult and post-insult. The variables assessed on every third day included OFT and FST. Following the behavioral tests, serotonin-ELISA was done. To analyse the outcomes, appropriate statistical tests were applied. Results: On standardization, the model was established to a 16-day model. Further, results highlighted a significant difference in OFT, FST and serotonin levels with the metformin group and fluoxetine compared to disease control (p<0.001). However, no significant difference was observed between the fluoxetine and metformin groups (p>0.05), signifying the comparable results. Conclusions: Metformin (240 mg/kg) alleviated the depressive symptoms by modulating both behavioral and serotonin levels

Study of evaluation of hepatoprotective potential of lycopene in rat models of paracetamol and antitubercular drugs (isoniazid + rifampicin) induced hepatotoxicity

Background: The exact role of lycopene has not been studied in the past for its hepatoprotective effects. Hence it was decided to explore its anti-oxidant and anti-inflammatory properties in acute and chronic models of drug- induced hepatotoxicity with the aim to evaluate hepatoprotective potential in rat models of paracetamol and antitubercular drugs (isoniazid + rifampicin) induced hepatotoxicity.Methods: The study was carried out in 70 Wistar rats in two phases. In phase I, models of paracetamol and anti-tubercular drugs induced hepatotoxicity were standardized in 22 Wistar rats and in phase II, hepatoprotective potential of lycopene was evaluated in paracetamol and anti-tubercular drugs induced hepatic damage using 48 Wistar rats. The effects of lycopene were compared with silymarin.Results: There was a significant (p <0.05) reduction in serum bilirubin levels with silymarin and lycopene 10mg/kg treated groups signifying protection against hepatic damage, while vehicle control and lycopene 5mg/kg treated groups had high bilirubin values. Similarly, significant (p <0.001) reduction in the levels of serum transaminases were observed with all the treatment groups though more evident in the positive control and lycopene 10mg/kg treated groups.Conclusions: The results of the present study prove that lycopene exerts hepatoprotective effect against paracetamol and anti-tubercular drugs induced hepatic damage in rats. Lycopene needs to be evaluated in other models of hepatotoxicity and further studies are required to delineate its mechanism of action. Lycopene could be a potential hepatoprotective for clinical use in future