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Inhibition of protein kinases by anticancer DNA intercalator, 4-butylaminopyrimido[4',5':4,5]thieno(2,3-b)quinoline

Acta Pharmaceutica Sinica B 2017年第3期7卷 303-310页

作者： HeggoduG.RohitKumar Chethan S.Kumar Hulihalli N.Kiran Kumar gopal m.advi rao Department of Biochemistry Davangere UniversityShivagangotriTholahunaseDavangere 577002India SS Institute of medical Sciences and Research Centre JnanashankaraDavangere 577005India

Targeting protein kinases(PKs) has been a promising strategy in treating cancer, as PKs are key regulators of cell survival and proliferation. Here in this study, we studied the ability of pyrimido[4',5':4,5]thieno(2,3-b)quinolines(PTQ) to inhibit different PKs by performing computational docking and in vitro screening. Docking studies revealed that 4-butylaminopyrimido[4',5':4,5]thieno(2,3-b)quinoline(BPTQ) has a higher order of interaction with the kinase receptors than other PTQ *** vitro screening confirms that BPTQ inhibits VEGFR1 and CHK2, with the IC_(50) values of 0.54 and1.70 mmol/L, respectively. Further, cytotoxicity of BPTQ was measured by trypan blue assay. Treatment with BPTQ decreased the proliferation of HL-60 cells with an IC_(50) value of 12 mmol/L and induces apoptosis, as explicated by the fall in the mitochondrial membrane potential, annexin V labeling and increased expression of caspase-3. Taken together, these data suggest that BPTQ possess ability to inhibit PKs and to induce cell death in human promyelocytic leukemia cells.

关键词： DNA intercalator molecular docking Kinase inhibitor Anticancer drugs Apoptosis Chemotherapy

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FRET from CdSe/ZnS Core-Shell Quantum Dots to Fluorescein 27 Dye

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Open Journal of Physical Chemistry 2013年第1期3卷 40-48页

作者： math A. Shivkumar Laxmi S. Inamdar mohammad Hussain K. Rabinal Basavaraj G. mulimani gopal m. advi rao Sanjeev R. Inamdar Department of Biochemistry Davangere University Davangere India Laser Spectroscopy Programme Department of Physics Karnatak University Dharwad India molecular Endocrinology and Development Laboratory Department of Zoology Karnatak University Dharwad India

Semiconductor QDs have emerged as a novel class of fluorophore with unique photoluminescence properties, in particular, CdSe/ZnS core-shell QDs have been successfully used as biocompatible fluorescence resonance energy transfer donors. Here we report FRET between CdSe/ZnS core-shell QDs (donor) and organic dye fluorescein 27 (F27) (acceptor). The results demonstrate the occurrence of efficient energy transfer in the system and the FRET efficiency is not only influenced by the spectral overlap between the QD donor emission and acceptor absorption, it might depend on QDs surface effect also. Efforts are made to correlate quantitatively spectral dependence of FRET rate with acceptor absorption spectrum, Forster distance, transfer efficiency (E) obtained employing steady-state & time-resolved technique.

关键词： Quantum Dot FRET Transfer Efficiency Spectral Overlap Forster Distance

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A Novel RP-HPLC method for Estimating Fulvestrant, Benzoyl Alcohol, and Benzyl Benzoate in Injection Formulation

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American Journal of Analytical Chemistry 2022年第7期13卷 229-240页

作者： Arjuna rao Nekkalapudi Venu gopal Veldi Sreenivas Pippalla Career Point University CP Tower 1 IPIA Kota Rajasthan India HTS Bio Pharma Aleap Industries Estate Pragathi Nagar Telangana India Sikkim Professional University Gangtok India

For the quantitative determination of Fulvestrant, Benzyl alcohol, and Benzyl benzoate in Fulvestrant injection, an original RP-HPLC approach was developed. The gradient method was developed using HPLC and a Phenomenex Luna C8, 150 × 4.6 mm, i.d 3.0 μm particle size column with a gradient programme of mobile phases A and B. With a flow rate of 1.5 mL/minute, injection volume of 10 μL, and column temperature of 35°C, UV wavelength detection at 254 nm for Benzyl alcohol and Benzoyl Benzoate and 280 nm for Fulvestrant, mobile phase-A consists of DI water and mobile phase-B consists of Acetonitrile. The current study describes a single HPLC method for developing a Fulvestrant (Active), Benzyl alcohol (Cosolvent), and Benzyl Benzoate (Cosolvent) assay for Fulvestrant injection. The assay method was determined to be suitable for quantifying three components in the pharmaceutical product and was verified according to ICH guidelines.

关键词： Fulvestrant Injection Formulation HPLC Assay Benzyl Alcohol and Benzyl Benzoate

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