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.

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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

Recent advances in metal nanoparticles supported on Montmorillonite as catalysts for organic synthesis

Recent advances in metal nanoparticles supported on Montmorillonite as catalysts for organic synthesis

urn:nbn:sciencein.jmns.2019v6.87

Published in Journal of Materials NanoScience

  • Dipak Kumar Dutta
    CSIR-North East Institute of Science and Technology, Materials Sciences and Technology Division, Jorhat 785006, Assam

Keywords: Metal-Nanoparticles, Supported Catalysts, Heterogeneous Catalysts, Organic Synthesis

Abstract

Nanostructured materials has appealed considerable attention due to their characteristic properties and applications in different fields. Metal nanoparticles supported on modified montmorillonite composites have led to the generation of new and novel heterogeneous ‘Nanocatalysts’, which are much more efficient than other catalysts and thus pave the way for developing sustainable environmentally benign catalysis and chemical procedures. Such nanocatalysts are progressing towards their use in chemical industries. This review presents the recent trend of advances in the synthesis and catalytic reactions of supported metal nanoparticles on acid activated montmorillonite. Metals nanoparticles-montmorillonite composites show efficient catalytic activities with high conversions and selectivity for hydrogenation, transfer hydrogenation, oxidations and coupling reactions. Raw montmorillonite possess no catalytic activity, however acid activated montmorillonite exhibits excellent acid catalytic activities.

Dutta, D. (2019). Recent advances in metal nanoparticles supported on Montmorillonite as catalysts for organic synthesis. Journal of Materials NanoScience, 6(1), 19-31.

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Formulation optimization of multicomponent aqueous coground mixtures of Meloxicam for dissolution enhancement

urn:nbn:sciencein.cbl.2019v6.93
Formulation optimization of multicomponent aqueous coground mixtures of Meloxicam for dissolution enhancement
Multicomponent coground mixtures of meloxicam

Published in Chemical Biology Letters

  • Sunita Dahiya University of Puerto Rico
  • Atul Kaushik
  • Kamla Pathak

Keywords: factorial design, solubility, drug delivery, hyrophilicity, PEG

Abstract

In present work, the role of various formulation excipients for dissolution enhancement of a BCS Class II drug, meloxicam was studied by formulating multicomponent aqueous coground mixtures using lactose, microcrystalline cellulose and three solubilizers; polyethylene glycol 400, propylene glycol and polyvinyl pyrrolidone. A 33 full factorial design was employed using solubilizers’ concentrations as independent variables whereas angle of repose and in vitro drug dissolution as dependent variables in order to optimize the amounts of solubilizers. The results revealed more than fivefold increase in drug dissolution in some experimental batches compared to that of pure drug powder. Full and reduced models were evolved for the dependent variables and the reduced models were further validated using extra design check points. The studies suggested that the incorporation of optimized amounts of solubilizers could be successfully employed for achieving desired flow properties and enhanced drug dissolution of poorly water soluble meloxicam. The method emerged as a simple, cost-effective, and organic solvent-free green approach toward formulation development of meloxicam and may also be applied to other limited water-soluble drugs.

Dahiya, S., Kaushik, A., & Pathak, K. (2019). Formulation optimization of multicomponent aqueous coground mixtures of Meloxicam for dissolution enhancement. Chemical Biology Letters, 6(1), 1-7.

Full text link http://pubs.thesciencein.org/journal/index.php/cbl/article/view/93

Antidiabetic effect of Carissa carandas in rats and the possible mechanism of its insulin secretagogues activity in isolated pancreatic islets

urn:nbn:sciencein.jbts.2019v6.90

Antidiabetic effect of Carissa carandas in rats and the possible mechanism of its insulin secretagogues activity in isolated pancreatic islets

  • Rambir Singh Bundelkhand University
  • Mansi Shrivastava Bundelkhand University
  • Poonam Sharma Indira Gandhi National Tribal University

Keywords: Antidiabetic, Solvent Extract, Insulin, Plant fruits, phytochemicals, diabetes

Abstract

Carissa carandas (CC) has been used in folklore medicine for treatment of diabetes. In the present study, hexane, chloroform, ethyl acetate, methanol and aqueous extracts of CC fruit were examined for hypoglycemic activity in healthy Wistar rats. Aqueous Extract of CC (AECC) was most active and showed fall of 67.08% in fasting blood glucose from 0 to 1h in glucose tolerance test (GTT). The ED50 of AECC was 300mg/kgbw in streptozotocin induced diabetic rats. Treatment of diabetic rats with ED50 of AECC for 28 days significantly reduced post prandial glucose (PPG) by 33.65% (p<0.01), glycosylated hemoglobin (HbA1c) by 45.79% (p<0.01) and increased insulin level by 69.7% (p<0.05). The results indicated that increase in insulin secretion may be partly responsible for antidiabetic effect of AECC. To assess the mechanism of secretagogues activity, AECC was incubated with isolated pancreatic islets of healthy Wistar rats at basal (3.3mM) and high (16.7mM) level of glucose in presence or absence of Diazoxide (K-ATP channel opener), Nimodipine (Ca2+ Channel blocker) and Calphostin-C (PKC inhibitor). AECC induced insulin secretion at 16.7mM of glucose was significantly (p<0.01) reduced by Diazoxide and Nimodipine but non significantly (p>0.05) by Calphostin-C. The study indicated that the phytochemicals present in AECC may be inducing insulin secretion by closing K-ATP channels in β-cells of pancreatic islets.

Full text link: http://pubs.thesciencein.org/journal/index.php/jbts/article/view/90

Nanochemistry and Nanocatalysis Science: Research advances and future perspective

urn:nbn:sciencein.jmns.2019v6.88

Nanochemistry and Nanocatalysis Science: Research advances and future perspective

Bhupender S. Chhikara, Rajender S. Varma

The development of nanomaterials has made its mark in nanocatalytic applications and ensuing plethora of nanotechnological advances. The size-dependent chemistry of nanomaterials and consequent controlled and designed synthesis of smart materials with desired end application has provided us a number of new products recently which are already making impact on quality of human life. The fundamental nano paradigm shift would influence future research advances in field of nanoscience chemistry, ranging from drug delivery to exquisite designs of novel catalysts that drive innovations in chemical synthesis and transformations.  The nanoscience is an interdisciplinary field that will see increased role in the diverse and emerging newer areas like artificial intelligence; nanochemistry would help speed up the development of applications in the real world with artificial intelligence.

Full text link: http://pubs.thesciencein.org/journal/index.php/jmns/article/view/88

Synthesis and Biodegradation Study of Starch/PVA/Nanoclay Blend

urn:nbn:sciencein.jmns.2018v5.60

Synthesis and Biodegradation Study of Starch/PVA/Nanoclay Blend

Geeta Saini University of Delhi
Himani Chauhan University of Delhi
Aeshna Gupta University of Delhi
Disha Gangotia University of Delhi

Keywords: Food packaging, Nanoclay, Biodegradable, PVA, Starch
Abstract

In this research work, we have synthesized blend of starch/PVA/nanoclay via solution cast method. The composition of blend was starch and PVA in 1:1 ratio by weight with citric acid as plasticizer. The amount of nanoclay was varied between 0.5 to 2 wt%. The structure elucidation of the film by Scanning electron microscopy reveals homogeneous dispersion of nanoclay into polymer matrix. The biodegradation of the films were studied by soil burial method and enzymatic hydrolysis and it was found that completely biodegradable films were produced which could serve as potential candidate for food packaging.

Link http://pubs.thesciencein.org/journal/index.php/jmns/article/view/60

Herbal nanomedicine interactions to enhance pharmacokinetics, pharmaco-dynamics, and therapeutic index for better bioavailability and biocompatibility of herbal formulations

urn:nbn:sciencein.jmns.2018v5.61

Herbal nanomedicine interactions to enhance pharmacokinetics, pharmaco-dynamics, and therapeutic index for better bioavailability and biocompatibility of herbal formulations

Rajiv Kumar University of Delhi
Munesh Sharma Arogya Nidhi Ayurveda Clinic

Keywords: Phyto-medicine, Hydrophilicity, Nanocarriers, Drug Delivery
Abstract

The recent technological advancement in nanotechnology has opened new avenues for research and development in the field of phyto-medicine. Development of reliable and eco-friendly synthesis of nanoparticles is a significant advancement for introduction nanotechnology to develop noble nanomedical delivery system of herbs (HNMDS), and have to overcome the downsides of old-style herbs-medicines delivery through analyzing the interactions between nanocarriers and herbs or phyto-medicine. The application of nanotechnological methods for bioavailability and biocompatibility enhancement of phyto-medicine must be reviewed and need urgent prompt efforts to develop new formulations. Nanotechnology enables the combination of hitherto separate approaches to health care by permitting the realization of so-called ’theranostic’ applications, as well as targeted combination products. Formulation must also release active ingredient from phyto-formulation as developing nano dosage forms has number of benefits for phyto-medicine. This review discusses nano sized herbs-nanomedicines delivery carries and potential current and futuristic advances for enhancing the activity and overcoming problems associated with herbal medicines for novel HNMDS.

Link: http://pubs.thesciencein.org/journal/index.php/jmns/article/view/61