Faculty Publications
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Item 6-[3-(4-Fluorophenyl)-1H-pyrazol-4-yl]-3-[(2-naphthyloxy)methyl][1,2,4]triazolo[3,4-b][1,3,4]thiadiazole as a potent antioxidant and an anticancer agent induces growth inhibition followed by apoptosis in HepG2 cells(2010) Dhanya, D.; Isloor, A.M.; Shetty, P.; Satyamoorthy, K.; Bharath Prasad, A.S.In this paper we have investigated the in vitro antioxidant property of two triazolo-thiadiazoles, 6-[3-(4-fluorophenyl)-1H-pyrazol-4-yl]-3-[(2-naphthyloxy)methyl][1,2,4]triazolo[3,4-b][1,3,4]thiadiazole (FPNT) and 6-[3-(4-chlororophenyl)-1H-pyrazol-4-yl]-3-[(phenyloxy)methyl][1,2,4]triazolo[3,4-b][1,3,4]thiadiazole (CPPT) by spectrophotometric DPPH and ABTS radical scavenging methods as well as by lipid peroxide assay. The anticancer activity along with possible mechanism of action of triazolo-thiadiazoles in Hep G2 cells was explored using MTT assay, [3H] thymidine assay, flow cytometry and chromatin condensation studies. Both FPNT and CPPT exhibited a dose dependent cytotoxic effect on hepatocellular carcinoma cell line, HepG2. The IC50 value was very low for both the compounds when compared to standard drug, doxorubicin. Incorporation of [3H] thymidine in conjunction with cell cycle analysis suggested that FPNT inhibited the growth of HepG2 cells. Flow cytometric studies revealed more percentage of cells in sub-G1 phase, indicating apoptosis, which was further confirmed through chromatin condensation studies by Hoechst staining. FPNT was found to be a potent antioxidant when compared to the standard in DPPH, ABTS radical scavenging assays and lipid peroxidation studies. © 2010 .Item Numerical simulation of bioheat transfer: a comparative study on hyperbolic and parabolic heat conduction(Springer, 2020) Akula, S.C.; Maniyeri, R.Cancer is one of the most death-causing diseases across the world. Radiotherapy is an important modality with which it is treated. In the present study, temperature distributions due to the application of radiation on skin are estimated using parabolic and hyperbolic models of heat transfer and are compared as to which one better estimates the practical temperature distribution. From the temperature distributions obtained, it can be inferred that parabolic and hyperbolic models produce similar results for smaller phase lag times, while they predict significantly different results when the lag times are large, suggesting that hyperbolic models are suitable to be used for biological systems with very complex internal structure. Thermal damage is also calculated for three different models of heat transfer. It is observed that thermal wave model predicts higher damage, followed by dual phase lag model and Pennes model. Time required for tumor necrosis is more for higher phase lag values, suggesting longer radiation exposure durations for treating complex biological systems. When phase lag times for heat flux and temperature gradient are equal, both dual phase lag model and Pennes model have shown similar results. Effect of Gaussian distribution of applied heat flux on time required for tumor necrosis is also studied. © 2019, The Brazilian Society of Mechanical Sciences and Engineering.Item Design, synthesis and molecular docking of 5-fluoro indole derivatives as inhibitors of PI3K/Akt signalling pathway in cervical cancer(Elsevier B.V., 2024) Etikyala, U.; Reddyrajula, R.; Pasha, A.; Udayakumar, U.; Pawar, S.C.; Vijjulatha, V.The PI3K/Akt signalling pathway promotes variety of cellular processes and the inhibition of PI3K/Akt signalling pathway could lead to decrease in tumour growth effectively in cancer cells. AD412, an indole derivative, is a potent immunosuppressive agent which also reported as an anticancer agent through significant inhibition of PI3K/Akt signalling pathway. In this current work, we designed and synthesized the two diverse lead series of 5-fluoro indole derivatives (6a-l and 11a-l) by specific structural modifications of AD412. In total, 24 new derivatives were evaluated for their antiproliferative activity against two cervical cancer cell lines (HeLa and SiHa) and a normal cell line (HEK 293). Among them, 6e exhibited excellent antiproliferative activity against HeLa and SiHa cells with IC50 values of 9.366 and 8.475 µM respectively, as well displayed a low toxicity profile. Further, 6e inhibited the migration and invasion of HeLa cells in a dose-dependent manner by affecting the synthesis of DNA. Moreover, the Western blot analysis revealed that 6e could inhibit cervical cancer progression by downregulating the PI3K-p85 and phosphorylation of Akt in Hela cells. In vitro mechanism studies demonstrated that 6e could significantly increase apoptosis in HeLa cells by upregulating the expression of proapoptosis related protein Bax. The binding mechanism and the activity profile of 5-fluoro indole derivatives were validated by employing molecular docking studies against the active sites of Akt and PI3K enzymes. In addition, in silico ADME and pharmacokinetic parameters prediction of compound 6e resulted in good oral bioavailability. Therefore, compound 6e could be a lead compound for further development of PI3K/Akt inhibitors and anticancer agents. © 2024Item Synthesis and characteristics of Fe/Ni/Cr oxide nanoparticles/PLA hybrid composite coatings on Mg–Zn–Ca alloy(Elsevier Editora Ltda, 2025) Kumar, P.; Kudva S, A.; T, A.; S, R.; Ramesh, M.R.; Prabhu, A.; Anne, G.Biodegradable materials research is dominated by magnesium and alloys thereof due to their excellent compatibility with biological barriers and biomechanical strength. Despite this, the rapid degradation of these materials in the physiological environment is the primary obstacle hindering their utilization in biomedical applications. This issue must be resolved before considering their use in clinical applications. To improve resistance towards corrosion and enhance biological efficacy and compatibility, the surfaces were coated with polylactic acid (PLA) using dip-coating. In this study, iron (Fe), nickel (Ni), and chromium (Cr) oxide nanoparticles from the Coleus amboinicus extract are synthesized and mixed with PLA to develop hybrid composite coatings, which are then applied onto the Mg–4Zn–1Ca alloy. Coleus amboinicus is known for its various medicinal properties, including immunoregulatory effects, antimicrobial activity, anti-inflammatory properties, and potential use in treating sepsis and other ailments. The extracted FeNiCr was used the develop composite coatings on Mg–4Zn–1Ca alloy. The coating improves biocompatibility, antibacterial properties, and overall performance of biomedical implants. These composite coatings were evaluated for their morphological and optical characteristics using a scanning electron microscope (SEM), 3-D non-contact profilometer, Fourier transform infrared spectroscopy (FTIR), and X-ray diffraction (XRD). The corrosion characteristics of developed samples were measured by electrochemical corrosion in standard simulation body fluid (SBF) at 37 °C. Furthermore, cytocompatibility of the PLA hybrid composites on osteoblast cells and apoptosis detection using acridine orange-ethidium bromide. Our developed coating showed ratings of 5B and 4B were obtained for FeNiCr/PLA NC- ball burnished (BB) Mg and FeNiCr/PLA nano composite (NC)–Mg samples, respectively, demonstrating the exceptional coating strength and the substrate. The corrosion rate of the FeNiCr/PLA NC-BB-Mg sample (0.02890 mm/y) is two-fold times increased against comparison with the H Mg sample (0.00012 mm/y). Cytocompatibility indicates their cytocompatibility for bone implant applications. © 2025 The Authors