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Shrishailnath S. Sajjan,M. Santoshkumar,S. Sanjeevkumar,T. B. Karegoudar 한국약제학회 2013 Journal of Pharmaceutical Investigation Vol.43 No.4
Amlodipine, atorvastatin and telmisartan are the most commonly used pharmaceutical drugs against cardiovascular disease, management of hypertension and in the treatment of angina. They have side-effects like edema,allergic reactions, breathing problems, etc. The melanin pigment from Klebsiella sp. GSK has the ability to adsorb pharmaceutical drugs, metals ions and to scavenge free radicals. We have studied here the binding of these drugs to melanin pigment at different concentrations and temperatures. It shows that these drugs in higher concentrations form stable complexes with melanin pigment. The amount of drug bound to melanin increases with increase in initial drug concentration. The drug-binding properties of melanin pigment were investigated kinetically. Telmisartan and amlodipine bind strongly at 40 C (59 and 25.8 lg/mg,respectively) than atorvastatin (18 lg/mg). Batch adsorption,uptake kinetics, Langmuir and Freundlich equations and temperature adsorption studies were also conducted with melanin pigment.
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Purification and Physiochemical Characterization of Melanin Pigment from Klebsiella sp. GSK
( Sajjan,Shrishailnath ),( Guruprasad Kulkarni ),( Veeranagouda Yaligara ),( Kyoung Lee ),( T. B. Karegoudar ) 한국미생물 · 생명공학회 2010 Journal of microbiology and biotechnology Vol.20 No.11
A bacterium capable of producing melanin pigment in the presence of L-tyrosine was isolated from a crop field soil sample and identified as Klebsiella sp. GSK based on morphological, biochemical, and 16S rDNA sequencing. The polymerization of this pigment occurs outside the cell wall, which has a granular structure as melanin ghosts. Chemical characterization of the pigment particles showed then to be acid resistant, alkali soluble, and insoluble in most of the organic solvents and water. The pigment got bleached when subjected to the action of oxidants as well as reductants. This pigment was precipitated with FeCl3, ammoniacal silver nitrate, and potassium ferricynide. The pigment showed high absorbance in the UV region and decreased absorbance when shifted towards the visible region. The melanin pigment was further charecterized by FT-IR and EPR spectroscopies. A key enzyme, 4- hydroxyphenylacetic acid hydroxylase, that catalyzes the formation of melanin pigment by hydroxylation of Ltyrosine was detected in this bacterium. Inhibition studies with specific inhibitors, kojic acid and KCN, proved that melanin is synthesized by the DOPA-melanin pathway.
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Properties and Functions of Melanin Pigment from Klebsiella sp. GSK
( Sajjan ),( Shrishailnath S ),( Anjaneya O ),( Guruprasad B Kulkarni ),( Anand S Nayak ),( Suresh B Mashetty ),( T B Karegoudar ) 한국미생물생명공학회(구 한국산업미생물학회) 2013 한국미생물·생명공학회지 Vol.41 No.1
Purified melanin pigment from Klebsiella sp. GSK was characterized by thermogravimetric, differential thermal, X ray diffraction and elemental analysis. This melanin pigment is structurally amorphous in nature. It is thermally stable up to 300oC and emits a strong exothermic peak at 700oC. Its carbon, hydrogen and nitrogen composition is 47.9%, 6.9% and 12.0%, respectively. It was used to scavenge metal ions and free radicals. After immobilizing the pigment and using it to adsorb copper and lead ions, the metal ion adsorption capacity was evaluated by atomic absorption spectroscopy (AAS) and the identity of melanin functional groups involved in the binding of metal ions was determined by Fourier transform infrared (FT-IR) spectroscopy. Batch adsorption studies showed that 169 mg/g of copper and 280 mg/g of lead were adsorbed onto melanin-alginate beads. The metal ion adsorption capacity of the melanin-alginate beads was relatively significant compared to alginate beads. The metal ion desorption capacity of HCl was greater (81.5% and 99% for copper and lead, respectively) than that of EDTA (80% and 71% for copper and lead, respectively). The ability of the melanin pigment to scavenge free radicals was evaluated by inhibition of the oxidation of 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2`-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) and was shown to be about 74% and 98%, respectively, compared with standard antioxidants.
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Urvashi Balekundri,Shrishailnath S. Sajjan,Shivakumar B. Madagi 한국약제학회 2015 Journal of Pharmaceutical Investigation Vol.45 No.3
Prostate cancer in men is the major cause of cancer mortality and is the active area for the researchers to discover new drugs for prostate cancer. 5alpha-reductase inhibitors have been proved to inhibit the growth and development of prostate cancer, hence identifying the potential of such compounds is necessary to invent new drugs. Quantitative structure activity relationship (QSAR) modeling is a well-known in silico drug designing approach that relates the chemical structure of compounds with their biological activities. In the present work 2D QSAR models are built using machine learning techniques such as linear regression, SMO, simple logistic, decision tree j48 and random forest, from the functions available in Weka 3.7 version. The present in silico QSAR study will help to identify new bioactivities for the drug discovery of prostate cancer and also narrow down the time required for drug discovery process.
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In silico prediction of epitopes for Chikungunya viral strains
Priyanka Kori,Shrishailnath S. Sajjan,Shivakumar B. Madagi 한국약제학회 2015 Journal of Pharmaceutical Investigation Vol.45 No.6
Chikungunya is a viral infection transmitted by Aedes mosquitoes in humans. Currently there is no drug available for the treatment of this infection. In absence of a proven therapeutic, vaccines provide an alternative preventive measure for the spread of viral infection in risk prone population. The identification of epitopes is an important step in designing vaccines for viral infections. Traditional methods for vaccine production can be augmented by incorporation of in silico methods at epitopes identification stage. Protein sequences were retrieved for three different viral strains from primary database. Multiple sequence alignment for the retrieved sequences was performed by using MEGA 6.06 to spot the conserved regions. Various immunological databases were utilized to determine the binding affinity with T cells and B cells from structural and non-structural proteins from three different isolates of Chikungunya virus. Five different epitopes were predicted for both structural and non-structural proteins. The epitopes ‘‘KKKPGRRERMCMKIE’’ and ‘‘DAEKEAEEEREAELT’’ and ‘‘AEEEREAEL’’ were predicted as core sequences for class I and class II MHC molecules whereas ‘‘SSKYDLECAQ’’ and ‘‘QVLKAKNIGL’’ were predicted as probable B cell epitopes for structural and non-structural proteins respectively. The identified epitopes can be used for developing a broad spectrum vaccines having effectiveness against different strains of Chikungunya.
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