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1.
Sensitive, rapid, and simple spectrophotometric methods were developed for determination of the anticancer drugs vinblastine sulfate (VBS) and vincristine sulfate (VCS), which belong to the class of vinca alkaloids. The first method is based on the reaction of VBS and VCS with diazotized dapsone, forming yellow azo products with absorption maxima at 430 nm. The colored species obey Beer's law in the concentration range of 0.5-24 microg/mL for VBS and 0.5-12 microg/mL for VCS. The second method describes the reaction of VBS and VCS with iron(III) and subsequent reaction with ferricyanide in hydrochloric acid medium to yield blue products with absorption maxima at 750 nm. The Beer's law range for this method is 0.1-4 microg/mL for VBS and 0.5-10 microg/mL for VCS. With both methods, colored species were stable for 1 h. The methods are simple and reproducible and are applied for determination of VBS and VCS in pharmaceutical formulations. Commonly encountered pharmaceuticals added as excipients do not interfere in the analysis and the results obtained in the analysis of dosage forms agree well with the labeled contents. 相似文献
2.
Nagaraja Sreeharsha Samathoti Prasanthi Satyavarapu Veera Venkata Naga Satya Mahalakshmi Prakash S. Goudanavar Nimbagal Raghavendra Naveen Buduru Gowthami Santosh Fattepur Girish Meravanige Syed Mohammed Basheeruddin Asdaq Md. Khalid Anwer Bandar Aldhubiab Mohammed Monirul Islam Mohammed Habeebuddin Mallikarjun Telsang Mazen Al Gharsan Michelyne Haroun 《Molecules (Basel, Switzerland)》2022,27(22)
A brand-new nano-crystal (NC) version of the hydrophobic drug Paclitaxel (PT) were formulated for cancer treatment. A stable NC formulation for the administration of PT was created using the triblock co-polymer Pluronic F127. To achieve maximum entrapment effectiveness and minimal particle size, the formulation was improved using the central composite design by considering agitation speed and vacuum pressure at five levels (coded as +1.414, +1, 0, −1, and −1.414). According to the Design Expert software’s predictions, 13 runs were created and evaluated for the chosen responses. The formulation prepared with an agitation speed of 1260 RPM and a vacuum pressure of 77.53 mbar can meet the requirements of the ideal formulation in order to achieve 142.56 nm of PS and 75.18% EE, according to the level of desirability (D = 0.959). Folic acid was conjugated to Pluronic F127 to create folate receptor-targeted NC. The drug release profile of the nano-crystals in vitro demonstrated sustained release over an extended period. Folate receptor (FR)-targeted NC (O-PT-NC-Folate) has also been prepared by conjugating folic acid to Pluronic F127. MTT test is used to validate the targeting efficacy on the FR-positive human oral cancer cell line (KB). At pharmacologically relevant concentrations, the PT nano-crystal formulation did not cause hemolysis. Compared to non-targeted NC of PT, the O-PT-NC-Folate showed a comparable but more sustained anti-cancer effect, according to an in vivo anti-tumor investigation in NCI/ADR-RES cell lines. The remarkable anti-tumor effectiveness, minimal toxicity, and simplicity of scale-up manufacturing of the NC formulations indicate their potential for clinical development. Other hydrophobic medications that are formulated into nano-systems for improved therapy may benefit from the formulation approach. 相似文献
3.
Sreenivasa Nayak Meghashyama P. Bhat A.C. Udayashankar T.R. Lakshmeesha Nagaraja Geetha Sudisha Jogaiah 《应用有机金属化学》2020,34(4):e5567
Dillenia indica L. is a traditional medicinal plant well known for its ability to cure various human diseases. In the current study, silver nanoparticles have been synthesized by simple and eco-friendly method using Dillenia indica extract. The green synthesized nanoparticles were characterized by Fourier transform infrared (FTIR), UV–visible spectroscopy, Atomic force microscopy (AFM), High-resolution transmission electron microscopy (HR-TEM), Zeta Potential and Size Distribution. UV–visible and FTIR spectra, AFM, HR-TEM and Zeta Potential readings and size distribution conformed that the synthesized silver particles were in the size of nano. The green synthesized silver nanoparticles were subjected for antibacterial activity against Gram-positive bacteria Enterococcus faecalis and Gram-negative bacteria Escherichia coli by agar well diffusion method. The synthesized AgNPs exhibited significant inhibition of 27 and 16 mm against the test bacteria at 0.25 mg/ml. Further the antibacterial activity was confirmed by live and dead cell assay by fluorescence microscopy and morphological changes of bacteria were studied by Scanning electron microscope (SEM). The study recommends that the synthesized silver nanoparticles using Dillenia indica extract have potential application in inhibition of bacteria owing to their potent antibacterial activity. 相似文献
4.
M. P. Telenkov Yu. A. Mityagin V. V. Agafonov K. K. Nagaraja 《Bulletin of the Lebedev Physics Institute》2015,42(12):343-345
Kinetics of intrasubband energy relaxation of electrons in the system of Landau levels lying below the optical phonon energy is studied. Extraordinary behavior of the relaxation of electronic subsystem excitation energy is detected. Despite the fact that its main channel is optical phonon emission, the total relaxation time exceeds the characteristic times of scattering on optical phonons by several orders of magnitude. 相似文献
5.
Kudavalli JS Boyd DR Coyne D Keeffe JR Lawlor DA MacCormac AC More O'Ferrall RA Rao SN Sharma ND 《Organic letters》2010,12(23):5550-5553
Benzene-cis- and trans-1,2-dihydrodiols undergo acid-catalyzed dehydration at remarkably different rates: k(cis)/k(trans) = 4500. This is explained by formation of a β-hydroxycarbocation intermediate in different initial conformations, one of which is stabilized by hyperconjugation amplified by an aromatic no-bond resonance structure (HOC(6)H(6)(+) ? HOC(6)H(5) H(+)). MP2 calculations and an unfavorable effect of benzoannelation on benzenium ion stability, implied by pK(R) measurements of -2.3, -8.0, and -11.9 for benzenium, 1-naphthalenium, and 9-phenanthrenium ions, respectively, support the explanation. 相似文献
6.
Michelyne Haroun Santosh S. Chobe Rajasekhar Reddy Alavala Savita M. Mathure Risy Namratha Jamullamudi Charushila K. Nerkar Vijay Kumar Gugulothu Christophe Tratrat Mohammed Monirul Islam Katharigatta N. Venugopala Mohammed Habeebuddin Mallikarjun Telsang Nagaraja Sreeharsha Md. Khalid Anwer 《Molecules (Basel, Switzerland)》2022,27(12)
Considering the importance of benzothiazepine pharmacophore, an attempt was carried out to synthesize novel 1,5-benzothiazepine derivatives using polyethylene glycol-400 (PEG-400)-mediated pathways. Initially, different chalcones were synthesized and then subjected to a cyclization step with benzothiazepine in the presence of bleaching clay and PEG-400. PEG-400-mediated synthesis resulted in a yield of more than 95% in less than an hour of reaction time. Synthesized compounds 2a–2j were investigated for their in vitro cytotoxic activity. Moreover, the same compounds were subjected to systematic in silico screening for the identification of target proteins such as human adenosine kinase, glycogen synthase kinase-3β, and human mitogen-activated protein kinase 1. The compounds showed promising results in cytotoxicity assays; among the tested compounds, 2c showed the most potent cytotoxic activity in the liver cancer cell line Hep G-2, with an IC50 of 3.29 ± 0.15 µM, whereas the standard drug IC50 was 4.68 ± 0.17 µM. In the prostate cancer cell line DU-145, the compounds displayed IC50 ranges of 15.42 ± 0.16 to 41.34 ± 0.12 µM, while the standard drug had an IC50 of 21.96 ± 0.15 µM. In terms of structural insights, the halogenated phenyl substitution on the second position of benzothiazepine was found to significantly improve the biological activity. This characteristic feature is supported by the binding patterns on the selected target proteins in docking simulations. In this study, 1,5-benzothiazepines have been identified as potential anticancer agents which can be further exploited for the development of more potent derivatives. 相似文献
7.
Gundibasappa K. Nagaraja Vijayavittala P. Vaidya Koodamara Sheshappa Rai Kittappa M. Mahadevan 《Phosphorus, sulfur, and silicon and the related elements》2013,188(12):2797-2806
A novel and efficient method for the synthesis of substituted thiazepines and diazepines has been developed. A simple one-pot reaction of chalcones 1a–f with 1-amino-2-mercapto-5-phenyl-1,3,4-triazole and o-phenylenediamine in the presence of a catalytic amount of sodium acetate under microwave irradiation gave 2-(3,8-diphenyl-7,8-dihydro[1,2,4]triazolo[3,4-b][1,3,4]thiadiazepin-6-yl)phenoles 2a–f and 2-(2-phenyl-2,3-dihydro-1H-1,5-benzodiazepin-4-yl)phenoles 3a–f, respectively. The structure of all the synthesized compounds was elucidated on the basis of elemental analysis, IR, 1H and 13C NMR, and mass spectral data. 相似文献
8.
9.
Kalkote Uttam Ramrao Choudhary Anil Ramkumar Natu Arvind Anant Ayyangar Nagaraja Ramanuja 《合成通讯》2013,43(10-11):1129-1135
1-Alkylaminoanthraquinones ( 2 a-f) and 1,4-bisalkylaminoanthraquinones ( 4 a-c) were prepared from aminoanthraquinones ( 1,3 ) by alkylation with alkyl sulphate/alkyl halide in presence of powdered sodium hydroxide, potassium carbonate and phase transfer catalyst. 相似文献
10.
J. Selvakumar V. S. Raghunathan K. S. Nagaraja 《Journal of Thermal Analysis and Calorimetry》2010,100(1):155-161
The volatile scandium-β-diketonates are synthesised using acetylacetone (acac) and tetramethylheptanedione (tmhd) as coordinative
ligands for CVD application. The X-ray powder patterns are indexed and analysed and found to be orthorhombic and monoclinic
phases for Sc(acac)3(1) and Sc(tmhd)3(2) respectively. The sublimation and evaporation kinetics have been analyzed using three calculating techniques. The non-isothermal
based activation energy values are found to be 38 ± 2 and 73 ± 2 kJ mol−1 by Flynn–Wall technique for (1) and (2) respectively. The measured Ea values are close to the value obtained using Kissinger method. 相似文献