Monocrotophos induced Biochemical and Histopathological alterations in the Kidney tissues of Mice

urn:nbn:sciencein.cbl.2019.v6.115

Monocrotophos induced Biochemical and Histopathological alterations in the Kidney tissues of Mice

Published in: Chemical Biology Letters

  • Suman Devi Maharshi Dayanand University
  • Jagjeet Singh Maharshi Dayanand University
  • Vijay Kumar Maharshi Dayanand University
  • Vinay Malik Maharshi Dayanand University

Keywords: histopathology, oxidative stress, kidney, lipid peroxidation, toxicology

Abstract

The present study investigated the effect of monocrotophos, a commonly used organophosphate pesticide exposure in the kidney tissues of the swiss albino mice. Monocrotophos was administered at the sub-lethal doses of 1.25mg/kg, 2.5 mg/kg and 5.0 mg/kg body weight for 24 hr. Monocrotophos toxicity generated oxidative stress in the mice as evidenced by significant decrease in the activities of glutathione, superoxide dismutase and catalase enzymes. The exposure increased the lipid peroxidation and protein oxidation in a dose dependent manner. Oxidative stress generation also elicited cytotoxic effects on the mice kidney which were supported by the histopathological changes like degeneration in glomerulus, bowmen’s capsule and tubules, hemorrhage, mononuclear cell infiltration, tubular cast and congested blood vessels in a dose-dependent manner. In conclusion, the study indicated that monocrotophos exposure at various doses induces significant deleterious health effects in mice kidney tissues via oxidative stress generation.

Cite as: Devi, S., Singh, J., Kumar, V., & Malik, V. (2019). Monocrotophos induced Biochemical and Histopathological alterations in the Kidney tissues of Mice. Chemical Biology Letters, 6(2), 39-45.

Retrieved full text from http://pubs.thesciencein.org/journal/index.php/cbl/article/view/115

Synthesis of novel β-lactam and thiazolidinone compounds derived from 4-methyl-1H-isochromen-1-one and their antibacterial activity

urn:nbn:sciencein.cbl.2019v6.107

Synthesis of novel β-lactam and thiazolidinone compounds derived from 4-methyl-1H-isochromen-1-one and their antibacterial activity

Published in: Chemical Biology Letters

  • Ashish Bhatt Mewar University
  • Krishna Srivastava Shri Ramswaroop Memorial University
  • Ravi Kant Shri Ramswaroop Memorial University
  • Deepa Lakhmani Shri Ramswaroop Memorial University

Keywords: 4-methyl-1H-isochromen-1-one, 1,1-biphenyl-4,4-diamine, Antibacterial activity, anti-microbial activity

Abstract

Selected novel β-lactam and thiazolidinone derivatives have been synthesized by the reaction of 4-methyl-1H-isochromen-1-one with 1,1-biphenyl-4,4-diamine, followed by the reaction with substituted benzaldehyde and further by the reaction with chloroacetyl chloride (for β-lactam type) and with thioglycolic acid (for thiazolidinone type) respectively . All the compounds were characterised by 1H NMR, IR and mass spectroscopy. These compounds were screened for in-vitro antimicrobial activity against Staphylococus aureus, E. coli, Pseudomonas aeruginosa strain. Some compounds have shown very good efficacy against antibacterial strain.

Cite as: Bhatt, A., Srivastava, K., Kant, R., & Lakhmani, D. (2019). Synthesis of novel β-lactam and thiazolidinone compounds derived from 4-methyl-1H-isochromen-1-one and their antibacterial activity. Chemical Biology Letters, 6(2), 46-54.

Retrieved full text from http://pubs.thesciencein.org/journal/index.php/cbl/article/view/107

Synthesis of coumarin based triazolyl thiazolidinones and their apoptotic inducer activity against caspase-3

urn:nbn:sciencein.cbl.2019v6.113

Synthesis of coumarin based triazolyl thiazolidinones and their apoptotic inducer activity against caspase-3

Published in Chemical Biology Letters

  • Pooja FNU University of Delhi
  • Nimisha Sinha University of Delhi
  • Sonu Kumar University of Delhi
  • Atul FNU University of Delhi
  • Sumit Kumar University of Delhi
  • Prashant Kumar SRM University
  • Abhishek Pandey University of Delhi
  • Pragya Sharma University of Delhi
  • Vithika Aggarwal University of Delhi
  • Poonam FNU University of Delhi
  • Poonam Mothsra University of Delhi
  • Brajendra Kumar Singh University of Delhi
  • Rishi Pal Singh University of Delhi
  • Yogesh Kumar University of Delhi

Keywords: Apoptotic inducer activity, anti-cancer, anti-tumor, breast cancer, enzyme inhibition, medicinal chemistry

Abstract

Coumarin, triazoles and thiazolidinones are one of the most preferred and high valued scaffolds frequently used in medicinal chemistry. The synthesis of newly designed coumarin based triazolyl-thiazolidinones was performed and new compounds were obtained in good yields. The listed compounds were evaluated for their apoptotic activity and determined the minimal inhibitory concentrations for each of the compound on SCC-4 cells using MTT viability test. Furthermore, apoptotic inducer activity was assayed by detecting the expression of caspase-3, a key apoptotic enzyme.

Cite as: FNU, P., Sinha, N., Kumar, S., FNU, A., Kumar, S., Kumar, P., Pandey, A., Sharma, P., Aggarwal, V., FNU, P., Mothsra, P., Singh, B., Singh, R., & Kumar, Y. (2019). Synthesis of coumarin based triazolyl thiazolidinones and their apoptotic inducer activity against caspase-3. Chemical Biology Letters, 6(2), 30-38.

Retrieved full text from http://pubs.thesciencein.org/journal/index.php/cbl/article/view/113

Design, synthesis and evaluation of Coumarin-Phenylthiazole conjugates as cholinesterase inhibitors

Design, synthesis and evaluation of Coumarin-Phenylthiazole conjugates as cholinesterase inhibitors

urn:nbn:sciencein.cbl.2019v6.111

Published in Chemical Biology Letters

  • Deepak Mishra Delhi Technological University
  • Atiya Fatima Delhi Technological University
  • Ram Singh Delhi Technological University
  • Nupur S Munjal Jaypee University of Information Technology
  • Vineet Mehta Jaypee University of Information Technology
  • Udayabanu Malairaman Jaypee University of Information Technology

Keywords: Alzheimer’s Disease, Brain disease, medicinal chemistry, coumarin derivative, AChE, BuChE, Nervous system, Neurological

Abstract

In this paper, we report the design, synthesis, in-silico, and in-vitro evaluations of a series of coumarin-phenylthiazole conjugates to inhibit cholinesterase enzymes. The coumarin and phenylthiazole derivatives have been synthesized separately, and further combined through covalent amine bond linkage. The synthesized compounds showed more inhibition towards BuChE than AChE, where 4-(3-bromophenyl)-1,3-thiazol-2-amine (7i) exhibited the strongest inhibition against BuChE with an IC50 value of 3.54 μM. For the conjugates, 3-{2-[4-(3-nitrophenyl)thiazol-2-ylamino]acetyl}chromen-2-one (8j) exhibited strongest inhibition with an IC50 value of 46.47 μM.  The better inhibition activities towards BuChE are also shown by 3-bromo and 2-fluoro derivatives. It was also observed that the substitution at 3-position, on phenylthiazole moiety produced better results against BuChE than 4-substituted counterparts.

Cite as: Mishra, D., Fatima, A., Singh, R., Munjal, N., Mehta, V., & Malairaman, U. (2019). Design, synthesis and evaluation of Coumarin-Phenylthiazole conjugates as cholinesterase inhibitors. Chemical Biology Letters6(2), 23-30.

Retrieved full text from http://pubs.thesciencein.org/journal/index.php/cbl/article/view/111

Novel synthesis and Optical investigation of trivalent Europium doped MGd2Si3O10 (M = Mg2+, Ca2+, Sr2+ and Ba2+) nanophosphors for full-color displays

urn:nbn:sciencein.jmns.2019v6.109

Novel synthesis and Optical investigation of trivalent Europium doped MGd2Si3O10 (M = Mg2+, Ca2+, Sr2+ and Ba2+) nanophosphors for full-color displays

Published in Journal of Materials NanoScience

  • Suman Sheoran M.D. University
  • Sitender Singh M.D. University
  • Ajay Mann M.D. University
  • Anura Samantilleke Universidade of Minho
  • Bernabe Mani Universitat Politecnica de Valencia
  • Devender Singh M.D. University

Keywords: nanophosphors, displays, lanthanide, luminescence, composites, LED

Abstract

A series of Eu3+ doped MGd2Si3O10 (M = Mg2+, Ca2+, Sr2+ and Ba2+) was synthesized via sol-gel procedure at 950 oC. The optical characteristics of the materials were studied by Photoluminescence (PL) emission spectra. Upon 395 nm excitation and at 0.03 mole concentration of Eu3+ ion, these nanophosphors display optimum photoluminescence with most intense peak due to 5D07F2 (614-616) of dopant. Powder X-ray diffraction (PXRD) analysis proves that all synthesized materials are of crystalline nature and crystallinity improves on increasing temperature. Transmission electron microscopy (TEM) exhibited the spherical shape of particles in 13-30 nm size. Fourier Transformation infrared (FTIR) spectra showed peaks in 400-1000 cm-1 corresponding to gadolinium-oxygen and silicon-oxygen bond vibrations. In BaGd2Si3O10 material, Gd-O vibration is centered at 492 cm-1 and absorption band at 855 cm-1 is result of asymmetric vibrations of SiO in silicate tetrahedral unit. Due to excellent photoluminescence and suitable CIE coordinates, these materials could have brilliant applications in innovative displays.

Research Highlights

  • Series of trivalent europium doped MGd2Si3O10 (M = Mg2+, Ca2+, Sr2+ and Ba2+)fluorescent materials were synthesized successfully with sol-gel procedure.
  • The prepared samples were characterized using Photoluminescence analysis, X-ray diffraction study, Transmission Electron Microscopic analysis and Fourier Transform Infrared spectroscopy.
  • The CIE color coordinates values of phosphor confirmed the red color of complex approving the PL results.
  • X-ray diffraction pattern of these materials determined the particle size using Debye Scherrer’s equation.
  • Excellent photoluminescence response and nano size of these materials made them suitable for various innovative display applications.

Cite as: Sheoran, S., Singh, S., Mann, A., Samantilleke, A., Mani, B., & Singh, D. (2019). Novel synthesis and Optical investigation of trivalent Europium doped MGd2Si3O10 (M = Mg2+, Ca2+, Sr2+ and Ba2+) nanophosphors for full-color displays. Journal of Materials NanoScience, 6(2), 73-81.

Retrieved full text from http://pubs.thesciencein.org/journal/index.php/jmns/article/view/109

Critical evaluation of pharmaceutical rational design of Nano-Delivery systems for Doxorubicin in Cancer therapy

Critical evaluation of pharmaceutical rational design of Nano-Delivery systems for Doxorubicin in Cancer therapy

Published in: Journal of Materials NanoScience

urn:nbn:sciencein.jmns.2019v6.95

Running title: Rationale of designing of nanoparticular delivery systems and impact of chemistry used with doxorubicin for anti-cancer therapy

  • Bhupender S. Chhikara University of Delhi
  • Brijesh Rathi University of Delhi
  • Keykavous Parang Chapman University

Keywords: Adriamycin, Cancer Drug, CPP, Drug Delivery System, Lipophilic Dox, TAT peptide

Abstract

Doxorubicin (Dox), an antineoplastic drug, has been extensively used for the treatment of different cancers. Dox is hydrophilic and therefore distributes to normal organs at a faster rate. Due to its required high doses, it poses severe toxicity, such as cardiotoxicity and nephrotoxicity. Diverse approaches, including nanoparticulate delivery systems, have been designed and evaluated to improve its delivery to the target site and reduce toxicity to normal organs; however, this has met little success. Here in this review, we have discussed various systems (metal nanoparticles, carbon nanotubes, fullerenes, liposomes, dendrimers, cyclic peptides, and other covalent/non-covalent systems) that have been used for Dox. We have critically evaluated their designing and outcome (in vitro and in vivo) with potential applications in the clinical setting.

Cite as: Chhikara, B., Rathi, B., & Parang, K. (2019). Critical evaluation of pharmaceutical rational design of Nano-Delivery systems for Doxorubicin in Cancer therapy. Journal of Materials NanoScience, 6(2), 47-66.

Retrieved full text from http://pubs.thesciencein.org/journal/index.php/jmns/article/view/95

Chemical libraries targeting Liver Stage Malarial infection

urn:nbn:sciencein.cbl.2019v6.96

Chemical Scaffolds Targeting liver-stage malaria parasite lifecycle

Published in: Chemical Biology Letters

  • Neha Sharma
  • Poonam FNU
  • Prakasha Kempaiah
  • Brijesh Rathi University of Delhi

Keywords: Malaria, Liver stage, Primaquine, Atovaquone, Clinical trials

Abstract

Despite the noteworthy advances in the use of chemotherapy for malaria, it continues to constantly affect large number of individuals. New molecules capable of blocking life-cycle of the parasite, preferably through targeting novel pathways and various modes of action, are increasingly becoming area of interest. Phenotypic screening of large chemical libraries is certainly one of the important criteria for the discovery of new and effective drugs. In recent years, diverse research groups including pharmaceutical industries have performed this large-scale phenotypic screening to identify the potential drug molecules. Most of the antimalarial drugs target blood-stage malarial infection and remain either less potent or ineffective against other life stages i.e. liver-stage, and the gametocyte stages of the parasite. Although, liver stage is considered as a crucial drug target, limited clinical options have significantly hampered the discovery of effective treatments. This short review presents the collection of selective molecules targeting specifically liver stage malaria parasites.

Cite as: Sharma, N., FNU, P., Kempaiah, P., & Rathi, B. (2019). Chemical libraries targeting Liver Stage Malarial infection. Chemical Biology Letters, 6(1), 14-22.

Retrieved full text from http://pubs.thesciencein.org/journal/index.php/cbl/article/view/96

Synthesis, DNA photocleavage, molecular docking and anticancer studies of 2-methyl-1,2,3,4-tetrahydroquinolines

urn:nbn:sciencein.cbl.2019v6.97

Published in: Chemical Biology Letters

  • P.J. Bindu Kuvempu University
  • T. R. Ravikumar Naik Indian Institute of Science
  • K.M. Mahadevan Kuvempu University
  • G. Krishnamurthy Sahyadri Science College

Keywords: Anti-oxidant, photodynamic therapy, DNA-Drug, tetrahydroquinolin

Abstract

2-Methyl-1,2,3,4-tetrahydroquinolin-4-yl)pyrrolidin-2-ones (3a−g) were synthesized by one pot multicomponent aza Diels-alder reaction between N-arylimines with two molecules of N-vinyl-2-pyrrolidinone in presence of Sm(III)nitrate as catalyst in acetonitrile solvent at room temperature stirring. The photocleavage studies with 2-methyl-1,2,3,4-tetrahydroquinolin-4-yl)pyrrolidin-2-ones (3a−g) revealed that almost all derivatives exhibited effective photocleavage of pUC−19 DNA at 365 nm, The The anticancer activities of newly synthesized compounds (3a−g) were more potent than doxorubicin on MCF−7 cells. The docking of PBR receptor (1EQ1) protein with newly synthesized THQ’s (3a-g) exhibited well established bonds with one or more amino acids in the receptor active pocket.

How to Cite Bindu, P., Naik, T. R. R., Mahadevan, K., & Krishnamurthy, G. (2019). Synthesis, DNA photocleavage, molecular docking and anticancer studies of 2-methyl-1,2,3,4-tetrahydroquinolines. Chemical Biology Letters, 6(1), 8-13.

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Pharmacy periodicals in India – a review by research

by Prof. Anant Hardas

Published in Journal of Biomedical and Therapeutic Sciences BiomedFrontiers section (Print)

The first issue of Pharmacy Journal in India – The Indian Journal of Pharmacy was published in Dec 1894, however it was defunct after 3 years. The Modern Pharmaceutical Journalism in India was Pioneered by Mr. Premnath Bazaz, who started the Eastern Pharmacist in 1958 and equal contribution was by Dr. A.K. Patni, who edited Indian Drug since its inception published by IDMA. Today there are nearly 175 Pharmacy Journal published in mostly English (and also in Marathi, Hindi & Bengali) by 5 different categories of publishers in India. The PCI has set out official Journals – seven – for D. Pharm Course and 20 for B. Pharm Degree Course, and minimum 2 international Journals for each discipline of specialization at M. Pharm, Ph.D and Pharm. D Courses structure in India. This article brings out short History and progress of Indian Pharmacy Periodical as on today.

Improved electrochemical performance of free standing electrospun graphene incorporated carbon nanofibers for supercapacitor

urn:nbn:sciencein.jmns.2019v6.94

Improved electrochemical performance of free standing electrospun graphene incorporated carbon nanofibers for supercapacitor

Published in Journal of Materials NanoScience

  • Dipti V Jamkar Rashtrasant Tukadoji Maharaj Nagpur University
  • Balkrishna J. Lokhande Solapur University
  • Subhash B. Kondawar Rashtrasant Tukadoji Maharaj Nagpur University

Keywords: Carbon nanofibers, graphene, electrospinning, electrochemical performance, supercapacitor

Abstract

In this paper, we report the fabrication of carbon nanofibers (CNFs) by electrospinning of polyacrylonitrile (PAN) solution in N,N-dimethylformamide (DMF)with different concentrations followed by stabilization and carbonization in a tubular quartz furnace. To improve the electrochemical performance, graphene nanosheets have been used to prepare porous graphene/carbon nanofibers (G-CNFs). The morphology of the porous G-CNFs were characterized by means of scanning electron microscopy (SEM). Diameter of CNFs and G-CNFs were found to be in the range of 400 – 500 nm reveals the fibers in nanoscale with high porosity. The electrochemical performance of as-synthesized CNFs and G-CNFs was studied by cyclic voltammetry (CV), galvanostatic charge discharge (GCD) and electrochemical impedance spectroscopy. The CV curve of the pure CNFs show distorted rectangular shape whereas CV curve of G-CNFs exhibit a nearly rectangle-shaped profile which is the characteristic of an ideal electric double-layer capacitor. The improved electrochemical performance of G-CNFs is due to the improved internal electrical conductivity of G-CNFs via graphene nanosheets interlaying.

Jamkar, D., Lokhande, B., & Kondawar, S. (2019). Improved electrochemical performance of free standing electrospun graphene incorporated carbon nanofibers for supercapacitor. Journal of Materials NanoScience, 6(1), 32-37.

Retrieved full text from http://pubs.thesciencein.org/journal/index.php/jmns/article/view/94