Most Cited Article: Next Generation Biofilm Inhibitors for Pseudomonas aeruginosa: Synthesis and Rational Design Approaches

Next Generation Biofilm Inhibitors for Pseudomonas aeruginosa: Synthesis and Rational Design Approaches

Author(s):

Mahesh S. Majik and Prakash T. ParvatkarPages 81-109 (29)

Abstract:

The bacterial biofilms and the emergence of multiple drug resistance have become a major threat for current medical treatment of nosocomial infections. It has been estimated that about 65-80% of microbial infections in the developed countries are associated with biofilms. Given the prominence of biofilms in infectious diseases, increasing efforts toward the development of small molecules that will modulate bacterial biofilm development and maintenance is on the rise. Till date, marine natural products have shown a tremendous potential as pharma leads and also given new skeletons which would be used as biofilm/QS inhibitors. Medically relevant biofilm forming bacteria such as Pseudomonas aeruginosa which is most frequently isolated bacteria in nosocomial infection is believed to be a model organism for biofilm studies. Hence, in this review, we have highlighted the development of small molecules that inhibit and/or disperse bacterial biofilms of P. aeruginosa in particular. Additionally, the rational design approaches as well as synthetic methodologies along with biological studies has been accounted in this article.

Keywords:

Marine natural products, biofilms, quorum sensing inhibitors, antifouling, chemical signaling.

Affiliation:

Bio-organic Chemistry Laboratory, CSIR-National Institute of Oceanography, Dona-Paula Goa 403 004, India

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Copper Homeostasis for the Developmental Progression of Intraerythrocytic Malarial Parasite

Article Details

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Copper Homeostasis for the Developmental Progression of Intraerythrocytic Malarial Parasite

[ Vol. 16 , Issue. 27 ]

Author(s):

Hiroko Asahi, Fumie Kobayashi, Shin-Ichi Inoue, Mamoru Niikura, Kenji Yagita and Mohammed Essa Marghany TolbaPages 3048-3057 (10)

Abstract:

Malaria is one of the world’s most devastating diseases, particularly in the tropics. In humans, Plasmodium falciparum lives mainly within red blood cells, and malaria pathogenesis depends on the red blood cells being infected with the parasite. Nonesterified fatty acids (NEFAs), including cis-9-octadecenoic acid, and phospholipids have been critical for complete parasite growth in serum-free culture, although the efficacy of NEFAs in sustaining the growth of P. falciparum has varied markedly. Hexadecanoic acid and trans-9-octadecenoic acid have arrested development of the parasite, in association with down-regulation of genes encoding copper-binding proteins. Selective removal of Cu⁺ ions has blockaded completely the ring–trophozoite–schizont progression of the parasite. The importance of copper homeostasis for the developmental progression of P. falciparum has been confirmed by inhibition of copper-binding proteins that regulate copper physiology and function by associating with copper ions. These data have provided strong evidence for a link between healthy copper homeostasis and successive developmental progression of P. falciparum. Perturbation of copper homeostasis may be, thus, instrumental in drug and vaccine development for the malaria medication. We review the importance of copper homeostasis in the asexual growth of P. falciparum in relation to NEFAs, copperbinding proteins, apoptosis, mitochondria, and gene expression.

Keywords:

Copper-binding protein, Copper homeostasis, Developmental arrest, Gene expression, Non-esterified fatty acids, Plasmodium falciparum, Copper ion.

Affiliation:

Division of Tropical Diseases and Parasitology, Department of Infectious Diseases, Kyorin University School of Medicine, Tokyo 181 8611, Japan.

Graphical Abstract:

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New Issue ::: Current Topics in Medicinal Chemistry, Volume 16 Issue 18

Current Topics in Medicinal Chemistry is a forum for the review of areas of keen and topical interest to medicinal chemists and others in the allied disciplines. Each issue is solely devoted to a specific topic, containing six to nine reviews, which provide the reader a comprehensive survey of that area. A Guest Editor who is an expert in the topic under review, will assemble each issue. The scope of Current Topics in Medicinal Chemistry will cover all areas of medicinal chemistry, including current developments in rational drug design, synthetic chemistry, bioorganic chemistry, high-throughput screening, combinatorial chemistry, compound diversity measurements, drug absorption, drug distribution, metabolism, new and emerging drug targets, natural products, pharmacogenomics, and structure-activity relationships. Medicinal chemistry is a rapidly maturing discipline. The study of how structure and function are related is absolutely essential to understanding the molecular basis of life. Current Topics in Medicinal Chemistry aims to contribute to the growth of scientific knowledge and insight, and facilitate the discovery and development of new therapeutic agents to treat debilitating human disorders. The journal is essential for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important advances.

Articles from the journal Current Topics in Medicinal Chemistry, Volume 16 Issue 18:

• Editorial (Thematic Issue: Nanoinformatics to Organic Synthesis, ADMET Profiling, and Application of Nanomaterials in Medicinal Chemistry, Medicine, and Biotechnology)
• Nano Particles: Emerging Warheads Against Bacterial Superbugs
• The Glitter of Carbon Nanostructures in Hybrid/Composite Hydrogels for Medicinal Use
• Advancements in Devices and Particle Engineering in Dry Powder Inhalation Technology
• The Unexpected Advantages of Using D-Amino Acids for Peptide Self- Assembly into Nanostructured Hydrogels for Medicine
• Biosynthesis of Fluorescent Bi2S3 Nanoparticles and their Application as Dual-Function SPECT-CT Probe for Animal Imaging
• Development of Crystalline Cellulosic Fibres for Sustained Release of Drug
• Biosynthesis of Anti-Proliferative Gold Nanoparticles Using Endophytic Fusarium oxysporum Strain Isolated from Neem (A. indica) Leaves
• Synthesis of Gold Mediated Biocompatible Nanocomposite of Lactone Enriched Fraction from Sahadevi (Vernonia cinerea Lees): An Assessment of Antimalarial Potential
• Development of Quercetin Based Nanodispersions
• Development and Characterization of Cassia grandis and Bixa orellana Nanoformulations

For details on the articles, please visit this link :: http://bit.ly/1tllt9c

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Podcast Integrin-Targeted Peptide/Peptidomimetic-Drug Conjugates: In-Depth Analysis of the Linker Technology

Integrin-Targeted Peptide/Peptidomimetic-Drug Conjugates: In-Depth Analysis of the Linker Technology

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Podcast Nuclear Targeting of Gold Nanoparticles for Improved Therapeutics

 Nuclear Targeting of Gold Nanoparticles for Improved Therapeutics

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Highlighted Article Flyer for the journal “Current Topics in Medicinal Chemistry”

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Current Topics in Medicinal Chemistry

Current Topics in Medicinal Chemistry is a forum for the review of areas of keen and topical interest to medicinal chemists and others in the allied disciplines. Each issue is solely devoted to a specific topic, containing six to nine reviews, which provide the reader a comprehensive survey of that area. A Guest Editor who is an expert in the topic under review, will assemble each issue. The scope of Current Topics in Medicinal Chemistry will cover all areas of medicinal chemistry, including current developments in rational drug design, synthetic chemistry, bioorganic chemistry, high-throughput screening, combinatorial chemistry, compound diversity measurements, drug absorption, drug distribution, metabolism, new and emerging drug targets, natural products, pharmacogenomics, and structure-activity relationships. Medicinal chemistry is a rapidly maturing discipline. The study of how structure and function are related is absolutely essential to understanding the molecular basis of life. Current Topics in Medicinal Chemistry aims to contribute to the growth of scientific knowledge and insight, and facilitate the discovery and development of new therapeutic agents to treat debilitating human disorders. The journal is essential for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important advances.

Articles from the journal Current Topics in Medicinal Chemistry, Volume 16 Issue 18:

• Editorial (Thematic Issue: Nanoinformatics to Organic Synthesis, ADMET Profiling, and Application of Nanomaterials in Medicinal Chemistry, Medicine, and Biotechnology)
• Nano Particles: Emerging Warheads Against Bacterial Superbugs
• The Glitter of Carbon Nanostructures in Hybrid/Composite Hydrogels for Medicinal Use
• Advancements in Devices and Particle Engineering in Dry Powder Inhalation Technology
• The Unexpected Advantages of Using D-Amino Acids for Peptide Self- Assembly into Nanostructured Hydrogels for Medicine
• Biosynthesis of Fluorescent Bi2S3 Nanoparticles and their Application as Dual-Function SPECT-CT Probe for Animal Imaging
• Development of Crystalline Cellulosic Fibres for Sustained Release of Drug
• Biosynthesis of Anti-Proliferative Gold Nanoparticles Using Endophytic Fusarium oxysporum Strain Isolated from Neem (A. indica) Leaves
• Synthesis of Gold Mediated Biocompatible Nanocomposite of Lactone Enriched Fraction from Sahadevi (Vernonia cinerea Lees): An Assessment of Antimalarial Potential
• Development of Quercetin Based Nanodispersions
• Development and Characterization of Cassia grandis and Bixa orellana Nanoformulations

For details on the articles, please visit this link :: http://bit.ly/1tllt9c

courtesy by : Bentham Insight

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Highlighted Article Flyer – Current Topics in Medicinal Chemistry Vol 16, Issue 20

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