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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
Molecules, Vol. 21, Pages 1649: Phenols and Polyphenols as Carbonic Anhydrase Inhibitors
Phenols are among the largest and most widely distributed groups of secondary metabolites within the plant kingdom. They are implicated in multiple and essential physiological functions. In humans they play an important role as microconstituents of the daily diet, their consumption being considered healthy. The physical and chemical properties of phenolic compounds make these molecules versatile ligands, capable of interacting with a wide range of targets, such as the Carbonic Anhydrases (CAs, EC 4.2.1.1). CAs reversibly catalyze the fundamental reaction of CO2 hydration to bicarbonate and protons in all living organisms, ...
Source: Molecules - December 1, 2016 Category: Chemistry Authors: Anastasia Karioti Fabrizio Carta Claudiu Supuran Tags: Review Source Type: research
Molecules, Vol. 21, Pages 1692: Bioassay-Guided Isolation of Cytotoxic Isocryptoporic Acids from Cryptoporus volvatus
The present work constitutes a contribution to the phytochemical investigation of Cryptoporus volvatus aiming to search for effective cytotoxic constituents against tumor cell lines in vivo. Bioassay-guided separation of the ethylacetate extract of C. volvatus afforded four new isocryptoporic acid (ICA) derivatives, ICA-B trimethyl ester (1), ICA-E (2), ICA-E pentamethyl ester (3), and ICA-G (4), together with nine known cryptoporic acids. These isocryptoporic acids are isomers of the cryptoporic acids with drimenol instead of albicanol as the terpenoid fragment; their structures were elucidated on the basis of spectroscop...
Source: Molecules - December 7, 2016 Category: Chemistry Authors: Ling-Yun Zhou Xiao-Hong Yu Bin Lu Yan Hua Tags: Article Source Type: research
Molecules, Vol. 21, Pages 1700: Six New Triterpene Derivatives from Aralia chinensis Var. dasyphylloides
Aralia chinensis var. dasyphylloides is widely distributed in China and used as a traditional herbal medicine for the treatment of digestive and immune system diseases. The present study aimed to search for novel oleanolic-type triterpenoids in low-polarity fractions. Six new triterpene derivatives (1 –6), together with two known compounds were isolated from the barks of A. chinensis var. dasyphylloides. Their structures were elucidated by 1D- and 2D-NMR spectroscopic analysis and chemical methods. They were identified as 3-oxo-oleana-11,13(18)-dien-28,30-dioic acid (1), 30-hydroxy-3-oxo-oleana -11,13(18)-dien-28-oic aci...
Source: Molecules - December 8, 2016 Category: Chemistry Authors: Rui-xi Gao Maochuan Liao Xianju Huang Yu Chen Guangzhong Yang Jun Li Tags: Article Source Type: research
Molecules, Vol. 22, Pages 16: Meadowsweet Teas as New Functional Beverages: Comparative Analysis of Nutrients, Phytochemicals and Biological Effects of Four Filipendula Species
The objective of this study was to investigate the nutritional, phytochemical profiles and bioactivities of possible functional beverages produced from F. ulmaria and its alternative substitutes (F. camtschatica, F. denudata, F. stepposa). The investigated decoctions were analyzed regarding their macronutrient, carbohydrate, organic acid, amino acid and mineral composition. Quantification of the main phenolic compounds in the decoctions of meadowsweet floral teas was performed by a microcolumn RP-HPLC-UV procedure; the highest content was revealed in F. stepposa tea. The investigation of the essential oil of four meadowswe...
Source: Molecules - December 25, 2016 Category: Chemistry Authors: Daniil Olennikov Nina Kashchenko Nadezhda Chirikova Tags: Article Source Type: research
Molecules, Vol. 22, Pages 27: Anti-Neuroinflammatory ent-Kaurane Diterpenoids from Pteris multifida Roots
Activated microglia are known to be a major source of cellular neuroinflammation which causes various neurodegenerative diseases, including Alzheimer ’s disease. In our continuing efforts to search for new bioactive phytochemicals against neuroinflammatory diseases, the 80% methanolic extract of Pteris multifida (Pteridaceae) roots was found to exhibit significant NO inhibitory activity in lipopolysaccharide (LPS)-activated BV-2 microglia cells . Three new ent-kaurane diterpenoids, pterokaurane M1 2-O-β-d-glucopyranoside (4), 2β,16α-dihydroxy-ent-kaurane 2,16-di-O-β-d-glucopyranoside (10), and 2β,16α,17-trihydroxy-...
Source: Molecules - December 25, 2016 Category: Chemistry Authors: Jung Kim Ji Seo Won Oh Sang Sung Tags: Article Source Type: research
Molecules, Vol. 22, Pages 66: Plant Growth Biostimulants, Dietary Feed Supplements and Cosmetics Formulated with Supercritical CO2 Algal Extracts
The review paper presents the use of algal extracts as safe and solvent-free components of plant growth biostimulants, dietary feed additives and cosmetics. Innovative technology that uses extracts obtained by supercritical CO2 extraction, as a method of isolation of biologically active compounds from algal biomass, is presented. An important part of the complete technology is the final formulation of the product. This enabled realization of the further step which was assessment of the utilitarian properties of the extract-based products. The extracts were analysed for the presence of biologically active molecules (e.g., p...
Source: Molecules - January 2, 2017 Category: Chemistry Authors: Izabela Michalak Katarzyna Chojnacka Agnieszka Saeid Tags: Review Source Type: research
Molecules, Vol. 22, Pages 132: Hair Growth Promoting and Anticancer Effects of p21-activated kinase 1 (PAK1) Inhibitors Isolated from Different Parts of Alpinia zerumbet
In this study, we evaluated the anti-alopecia and anticancer effects of PAK1 inhibitors isolated from Alpinia zerumbet (alpinia) in cell culture. The bioactive compounds isolated from alpinia were found to markedly promote hair cell growth. Kaempferol-3-O- β-d-glucuronide (KOG) and labdadiene, two of the isolated compounds, increased the proliferation of human follicle dermal papilla cells by approximately 117%–180% and 132%–226%, respectively, at 10–100 μM. MTD (2,5-bis(1E,3E,5E)-6-methoxyhexa-1,3,5-trien-1-yl)-2,5-dihydrofuran) and TMOQ ((E) -2,2,3,3-tetramethyl-8-methylene-7-(oct-6-en-1-yl)octahydro-1H-quinolizi...
Source: Molecules - January 13, 2017 Category: Chemistry Authors: Nozomi Taira Binh Nguyen Shinkichi Tawata Tags: Article Source Type: research
Molecules, Vol. 22, Pages 205: Identification of Larvicidal Constituents of the Essential Oil of Echinops grijsii Roots against the Three Species of Mosquitoes
The screening of Chinese medicinal herbs for insecticidal principles showed that the essential oil of Echinops grijsii Hance roots possessed significant larvicidal activity against mosquitoes. The essential oil was extracted via hydrodistillation and its constituents were determined by gas chromatography ‐mass spectrometry (GC‐MS) analysis. GC‐MS analyses revealed the presence of 31 components, with 5‐(3‐buten‐1‐yn‐1‐yl)‐2,2′‐bithiophene (5‐BBT, 27.63%), αterthienyl (α‐T, 14.95%),1,8‐cineole (5.56%) and cis‐β‐ocimene (5.01%) being the four major constituents. Ba sed bioactivity‐direct...
Source: Molecules - January 26, 2017 Category: Chemistry Authors: Mei Zhao Qi Liu Qiyong Liu Zhi Liu Tags: Article Source Type: research
Molecules, Vol. 22, Pages 219: The Transcription Profile Unveils the Cardioprotective Effect of Aspalathin against Lipid Toxicity in an In Vitro H9c2 Model
Aspalathin, a C-glucosyl dihydrochalcone, has previously been shown to protect cardiomyocytes against hyperglycemia-induced shifts in substrate preference and subsequent apoptosis. However, the precise gene regulatory network remains to be elucidated. To unravel the mechanism and provide insight into this supposition, the direct effect of aspalathin in an isolated cell-based system, without the influence of any variables, was tested using an H9c2 cardiomyocyte model. Cardiomyocytes were exposed to high glucose (33 mM) for 48 h before post-treatment with or without aspalathin. Thereafter, RNA was extracted and RT2 PCR Profi...
Source: Molecules - January 30, 2017 Category: Chemistry Authors: Rabia Johnson Phiwayinkosi Dludla Christo Muller Barbara Huisamen M. Essop Johan Louw Tags: Article Source Type: research
Molecules, Vol. 22, Pages 272: Experimental Evidence and In Silico Identification of Tryptophan Decarboxylase in Citrus Genus
Plant tryptophan decarboxylase (TDC) converts tryptophan into tryptamine, precursor of indolealkylamine alkaloids. The recent finding of tryptamine metabolites in Citrus plants leads to hypothesize the existence of TDC activity in this genus. Here, we report for the first time that, in Citrus x limon seedlings, deuterium labeled tryptophan is decarboxylated into tryptamine, from which successively deuterated N,N,N-trimethyltryptamine is formed. These results give an evidence of the occurrence of the TDC activity and the successive methylation pathway of the tryptamine produced from the tryptophan decarboxylation. In additi...
Source: Molecules - February 10, 2017 Category: Chemistry Authors: Luigi De Masi Domenico Castaldo Domenico Pignone Luigi Servillo Angelo Facchiano Tags: Article Source Type: research
Molecules, Vol. 22, Pages 273: Synthesis and Positive Inotropic Activity of 1,2,4Triazolo4,3-a Quinoxaline Derivatives Bearing Substituted Benzylpiperazine and Benzoylpiperazine Moieties
In an attempt to search for more potent positive inotropic agents, two series of [1,2,4]triazolo[4,3-a] quinoxaline derivatives bearing substituted benzylpiperazine and benzoylpiperazine moieties were synthesized and their positive inotropic activities evaluated by measuring left atrial stroke volume in isolated rabbit heart preparations. Several compounds showed favorable activities compared with the standard drug, milrinone. Compound 6c was the most potent agent, with an increased stroke volume of 12.53% ± 0.30% (milrinone: 2.46% ± 0.07%) at 3 × 10−5 M. The chronotropic effects of compounds having considerable inotr...
Source: Molecules - February 10, 2017 Category: Chemistry Authors: Xue-Kun Liu Long-Xu Ma Zhi-Yu Wei Xun Cui Shi Zhan Xiu-Mei Yin Hu-Ri Piao Tags: Article Source Type: research
