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Total 981 results found since Jan 2013.
Molecules, Vol. 21, Pages 704: Significant Improvement of Metabolic Characteristics and Bioactivities of Clopidogrel and Analogs by Selective Deuteration
In the search for prodrug analogs of clopidogrel with improved metabolic characteristics and antiplatelet bioactivity, a group of clopidogrel and vicagrel analogs selectively deuterated at the benzylic methyl ester group were synthesized, characterized, and evaluated. The compounds included clopidogrel-d3 (8), 2-oxoclopidogrel-d3 (9), vicagrel-d3 (10a), and 12 vicagrel-d3 analogs (10b–10m) with different alkyl groups in the thiophene ester moiety. The D3C-O bond length in 10a was shown by X-ray single crystal diffraction to be shorter than the H3C-O bond length in clopidogrel, consistent with the slower rate of hydrolysi...
Source: Molecules - May 29, 2016 Category: Chemistry Authors: Xueyu XuXue ZhaoZhichao YangHao WangXiangjun MengChong SuMingyuan LiuJohn FawcettYan YangJingkai Gu Tags: Article Source Type: research
Molecules, Vol. 21, Pages 731: Biologically Synthesized Gold Nanoparticles Ameliorate Cold and Heat Stress-Induced Oxidative Stress in Escherichia coli
Due to their unique physical, chemical, and optical properties, gold nanoparticles (AuNPs) have recently attracted much interest in the field of nanomedicine, especially in the areas of cancer diagnosis and photothermal therapy. Because of the enormous potential of these nanoparticles, various physical, chemical, and biological methods have been adopted for their synthesis. Synthetic antioxidants are dangerous to human health. Thus, the search for effective, nontoxic natural compounds with effective antioxidative properties is essential. Although AuNPs have been studied for use in various biological applications, explorati...
Source: Molecules - June 3, 2016 Category: Chemistry Authors: Xi-Feng ZhangWei ShenSangiliyandi Gurunathan Tags: Article Source Type: research
Molecules, Vol. 21, Pages 752: Antimicrobial Activity of Lactoferrin-Related Peptides and Applications in Human and Veterinary Medicine
Antimicrobial peptides (AMPs) represent a vast array of molecules produced by virtually all living organisms as natural barriers against infection. Among AMP sources, an interesting class regards the food-derived bioactive agents. The whey protein lactoferrin (Lf) is an iron-binding glycoprotein that plays a significant role in the innate immune system, and is considered as an important host defense molecule. In search for novel antimicrobial agents, Lf offers a new source with potential pharmaceutical applications. The Lf-derived peptides Lf(1–11), lactoferricin (Lfcin) and lactoferrampin exhibit interesting and more po...
Source: Molecules - June 10, 2016 Category: Chemistry Authors: Natascia BruniMaria CapucchioElena BiasibettiEnrica PessioneSimona CirrincioneLeonardo GiraudoAntonio CoronaFranco Dosio Tags: Review Source Type: research
Molecules, Vol. 21, Pages 892: Marine Natural Products as Models to Circumvent Multidrug Resistance
Multidrug resistance (MDR) to anticancer drugs is a serious health problem that in many cases leads to cancer treatment failure. The ATP binding cassette (ABC) transporter P-glycoprotein (P-gp), which leads to premature efflux of drugs from cancer cells, is often responsible for MDR. On the other hand, a strategy to search for modulators from natural products to overcome MDR had been in place during the last decades. However, Nature limits the amount of some natural products, which has led to the development of synthetic strategies to increase their availability. This review summarizes the research findings on marine natur...
Source: Molecules - July 7, 2016 Category: Chemistry Authors: Solida LongEmília SousaAnake KijjoaMadalena Pinto Tags: Review Source Type: research
Molecules, Vol. 21, Pages 970: Halichoblelide D, a New Elaiophylin Derivative with Potent Cytotoxic Activity from Mangrove-Derived Streptomyces sp. 219807
During our search for interesting bioactive secondary metabolites from mangrove actinomycetes, the strain Streptomyces sp. 219807 which produced a high elaiophylin yield of 4486 mg/L was obtained. A new elaiophylin derivative, halichoblelide D (1), along with seven known analogues 2 –8 was isolated and identified from the culture broth. Their chemical structures were determined by detailed analysis of 1D and 2D NMR and HRMS data. The absolute configuration of halichoblelide D (1) was confirmed by comparing the CD spectrum with those of the reported analogues. Compounds 1–7 exhibited potent cytotoxic activities against ...
Source: Molecules - July 24, 2016 Category: Chemistry Authors: Ying Han Erli Tian Dongbo Xu Min Ma Zixin Deng Kui Hong Tags: Article Source Type: research
Molecules, Vol. 21, Pages 1170: Commentary: The Search for Covalently Ligandable Proteins in Biological Systems
This commentary highlights the recent article published in Nature, June 2016, titled: “Proteome-wide covalent ligand discovery in native biological systems”. They screened the whole proteome of different human cell lines and cell lysates. Around 700 druggable cysteines in the whole proteome were found to bind the electrophilic fragments in both active and inactive states of the p roteins. Their experiment and computational docking results agreed with one another. The usefulness of this study in terms of bringing a change in medicinal chemistry is highlighted here.
Source: Molecules - September 1, 2016 Category: Chemistry Authors: Syed Badshah Yahia Mabkhot Tags: Commentary Source Type: research
Molecules, Vol. 21, Pages 1170: The Search for Covalently Ligandable Proteins in Biological Systems
This commentary highlights the recent article published in Nature, June 2016, titled: “Proteome-wide covalent ligand discovery in native biological systems”. They screened the whole proteome of different human cell lines and cell lysates. Around 700 druggable cysteines in the whole proteome were found to bind the electrophilic fragments in both active and inactive states of the p roteins. Their experiment and computational docking results agreed with one another. The usefulness of this study in terms of bringing a change in medicinal chemistry is highlighted here.
Source: Molecules - September 1, 2016 Category: Chemistry Authors: Syed Badshah Yahia Mabkhot Tags: Commentary Source Type: research
Molecules, Vol. 21, Pages 1198: Synthesis and Anti-HIV-1 Activity Evaluation for Novel 3a,6a-Dihydro-1H-pyrrolo3,4-cpyrazole-4,6-dione Derivatives
The search for new molecular constructs that resemble the critical two-metal binding pharmacophore and the halo-substituted phenyl functionality required for HIV-1 integrase (IN) inhibition represents a vibrant area of research within drug discovery. As reported herein, we have modified our recently disclosed 1-[2-(4-fluorophenyl)ethyl]-pyrrole-2,5-dione scaffolds to design 35 novel compounds with improved biological activities against HIV-1. These new compounds show single-digit micromolar antiviral potencies against HIV-1 and low toxicity. Among of them, compound 9g and 15i had potent anti-HIV-1 activities (EC50< ...
Source: Molecules - September 7, 2016 Category: Chemistry Authors: Guan-Nan Liu Rong-Hua Luo Yu Zhou Xing-Jie Zhang Jian Li Liu-Meng Yang Yong-Tang Zheng Hong Liu Tags: Article Source Type: research
Molecules, Vol. 21, Pages 1211: Flavones as Quorum Sensing Inhibitors Identified by a Newly Optimized Screening Platform Using Chromobacterium violaceum as Reporter Bacteria
Quorum sensing (QS) is the process by which bacteria produce and detect signal molecules to coordinate their collective behavior. This intercellular communication is a relevant target for anti-biofilm therapies. Here we have optimized a screening-applicable assay to search for new quorum sensing inhibitors from natural compound libraries. In this system, QS is correlated with the production of violacein, which is directly controlled by the LuxI/LuxR system in Chromobacterium violaceum ATCC 31532. The parallel use of C. violaceum Tn5-mutant CV026, which depends on auto-inducer addition, allows simultaneous discrimination of...
Source: Molecules - September 9, 2016 Category: Chemistry Authors: Malena Skogman Sonja Kanerva Suvi Manner Pia Vuorela Adyary Fallarero Tags: Article Source Type: research
Molecules, Vol. 21, Pages 1243: Curcumin and Resveratrol in the Management of Cognitive Disorders: What is the Clinical Evidence?
A growing body of in vitro and in vivo evidences shows a possible role of polyphenols in counteracting neurodegeneration: curcumin and resveratrol are attractive substances in this regard. In fact, epidemiological studies highlight a neuroprotective effect of turmeric (rhizome of Curcuma longa L.), the main source of curcumin. Moreover, the consumption of red wine, the main source of resveratrol, has been related to a lower risk of developing dementia. In this review, we analyzed the published clinical trials investigating curcumin and resveratrol in the prevention or treatment of cognitive disorders. The ongoing studies w...
Source: Molecules - September 16, 2016 Category: Chemistry Authors: Gabriela Mazzanti Silvia Di Giacomo Tags: Review Source Type: research
Molecules, Vol. 21, Pages 1372: Development of Mushroom-Based Cosmeceutical Formulations with Anti-Inflammatory, Anti-Tyrosinase, Antioxidant, and Antibacterial Properties
The cosmetic industry is in a constant search for natural compounds or extracts with relevant bioactive properties, which became valuable ingredients to design cosmeceutical formulations. Mushrooms have been markedly studied in terms of nutritional value and medicinal properties. However, there is still slow progress in the biotechnological application of mushroom extracts in cosmetic formulations, either as antioxidants, anti-aging, antimicrobial, and anti-inflammatory agents or as hyperpigmentation correctors. In the present work, the cosmeceutical potential of ethanolic extracts prepared from Agaricus bisporus, Pleurotu...
Source: Molecules - October 13, 2016 Category: Chemistry Authors: Oludemi Taofiq Sandrina Heleno Ricardo Calhelha Maria Alves Lillian Barros Maria Barreiro Ana Gonz ález-Paramás Isabel Ferreira Tags: Article Source Type: research
Molecules, Vol. 21, Pages 1375: Novel Natural Product- and Privileged Scaffold-Based Tubulin Inhibitors Targeting the Colchicine Binding Site
Tubulin inhibitors are effective anticancer agents, however, there are many limitations to the use of available tubulin inhibitors in the clinic, such as multidrug resistance, severe side-effects, and generally poor bioavailability. Thus, there is a constant need to search for novel tubulin inhibitors that can overcome these limitations. Natural product and privileged structures targeting tubulin have promoted the discovery and optimization of tubulin inhibitors. This review will focus on novel tubulin inhibitors derived from natural products and privileged structures targeting the colchicine binding site on tubulin.
Source: Molecules - October 14, 2016 Category: Chemistry Authors: Mengqi Dong Fang Liu Hongyu Zhou Shumei Zhai Bing Yan Tags: Review Source Type: research
Molecules, Vol. 21, Pages 1398: Proteome and Peptidome of Vipera berus berus Venom
Snake venom is a rich source of peptides and proteins with a wide range of actions. Many of the venom components are currently being tested for their usefulness in the treatment of many diseases ranging from neurological and cardiovascular to cancer. It is also important to constantly search for new proteins and peptides with properties not yet described. The venom of Vipera berus berus has hemolytic, proteolytic and cytotoxic properties, but its exact composition and the factors responsible for these properties are not known. Therefore, an attempt was made to identify proteins and peptides derived from this species venom ...
Source: Molecules - October 18, 2016 Category: Chemistry Authors: Aleksandra Bocian Ma łgorzata Urbanik Konrad Hus Andrzej Łyskowski Vladim ír Petrilla Zuzana Andrej čáková Monika Petrillov á Jaroslav Legath Tags: Article Source Type: research
Molecules, Vol. 21, Pages 1415: Antimalarial Activity of the Chemical Constituents of the Leaf Latex of Aloe pulcherrima Gilbert and Sebsebe
Malaria is one of the three major global public health threats due to a wide spread resistance of the parasites to the standard antimalarial drugs. Considering this growing problem, the ethnomedicinal approach in the search for new antimalarial drugs from plant sources has proven to be more effective and inexpensive. The leaves of Aloe pulcherrima Gilbert and Sebsebe, an endemic Ethiopian plant, are locally used for the treatment of malaria and other infectious diseases. Application of the leaf latex of A. pulcherrima on preparative silica gel TLC led to the isolation of two C-glycosylated anthrones, identified as nataloin...
Source: Molecules - October 27, 2016 Category: Chemistry Authors: Tekleab Teka Daniel Bisrat Mariamawit Yeshak Kaleab Asres Tags: Article Source Type: research
Molecules, Vol. 21, Pages 1638: Water Will Be the Coal of the Future—The Untamed Dream of Jules Verne for a Solar Fuel
This article evokes the futuristic visions of two giants, one a writer, Jules Verne, who foresaw water as the coal of the future, and the other a scientist, Giacomo Ciamician, who foresaw the utilization of solar energy as an energy source with which to drive photochemical and photocatalytic reactions for the betterment of mankind. Specifically, we examine briefly the early work of the 1960s and 1970s on the photosplitting of free water and water adsorbed on solid supports, based mostly on metal oxides, from which both hydrogen and oxygen evolve in the expected stoichiometric ratio of 2 to 1. The two oil crises of the 1970...
Source: Molecules - November 28, 2016 Category: Chemistry Authors: Vladimir Ryabchuk Vyacheslav Kuznetsov Alexei Emeline Yurii Artem ’ev Galina Kataeva Satoshi Horikoshi Nick Serpone Tags: Review Source Type: research
