scholarly journals Bacterial Alkyl-4-quinolones: Discovery, Structural Diversity and Biological Properties

Molecules ◽  
2020 ◽  
Vol 25 (23) ◽  
pp. 5689
Author(s):  
Muhammad Saalim ◽  
Jessica Villegas-Moreno ◽  
Benjamin R. Clark
Keyword(s):  
Pseudomonas Aeruginosa ◽  
Antioxidant Properties ◽  
Antimicrobial Properties ◽  
Structural Diversity ◽  
Biological Properties ◽  
Side Chains ◽  
Bacterial Communication ◽  
Pseudomonas Quinolone Signal ◽  
Wide Range ◽  
History Of

The alkyl-4-quinolones (AQs) are a class of metabolites produced primarily by members of the Pseudomonas and Burkholderia genera, consisting of a 4-quinolone core substituted by a range of pendant groups, most commonly at the C-2 position. The history of this class of compounds dates back to the 1940s, when a range of alkylquinolones with notable antibiotic properties were first isolated from Pseudomonas aeruginosa. More recently, it was discovered that an alkylquinolone derivative, the Pseudomonas Quinolone Signal (PQS) plays a key role in bacterial communication and quorum sensing in Pseudomonas aeruginosa. Many of the best-studied examples contain simple hydrocarbon side-chains, but more recent studies have revealed a wide range of structurally diverse examples from multiple bacterial genera, including those with aromatic, isoprenoid, or sulfur-containing side-chains. In addition to their well-known antimicrobial properties, alkylquinolones have been reported with antimalarial, antifungal, antialgal, and antioxidant properties. Here we review the structural diversity and biological activity of these intriguing metabolites.

scholarly journals Isobornylchalcones as Scaffold for the Synthesis of Diarylpyrazolines with Antioxidant Activity

Molecules ◽  
2021 ◽  
Vol 26 (12) ◽  
pp. 3579
Author(s):  
Svetlana A. Popova ◽  
Evgenia V. Pavlova ◽  
Oksana G. Shevchenko ◽  
Irina Yu. Chukicheva ◽  
Aleksandr V. Kutchin
Keyword(s):  
Antioxidant Activity ◽  
Antioxidant Properties ◽  
Biological Properties ◽  
High Reactivity ◽  
Biologically Active ◽  
Brain Lipids ◽  
Wide Range ◽  
Privileged Structure ◽  
Vitro Model

The pyrazoline ring is defined as a “privileged structure” in medicinal chemistry. A variety of pharmacological properties of pyrazolines is associated with the nature and position of various substituents, which is especially evident in diarylpyrazolines. Compounds with a chalcone fragment show a wide range of biological properties as well as high reactivity which is primarily due to the presence of an α, β-unsaturated carbonyl system. At the same time, bicyclic monoterpenoids deserve special attention as a source of a key structural block or as one of the pharmacophore components of biologically active molecules. A series of new diarylpyrazoline derivatives based on isobornylchalcones with different substitutes (MeO, Hal, NO2, N(Me)2) was synthesized. Antioxidant properties of the obtained compounds were comparatively evaluated using in vitro model Fe2+/ascorbate-initiated lipid peroxidation in the substrate containing brain lipids of laboratory mice. It was demonstrated that the combination of the electron-donating group in the para-position of ring B and OH-group in the ring A in the structure of chalcone fragment provides significant antioxidant activity of synthesized diarylpyrazoline derivatives.

scholarly journals Thymodepressin—Unforeseen Immunosuppressor

Molecules ◽  
2021 ◽  
Vol 26 (21) ◽  
pp. 6550
Author(s):  
Vladislav I. Deigin ◽  
Julia E. Vinogradova ◽  
Dmitry L Vinogradov ◽  
Marina S. Krasilshchikova ◽  
Vadim T. Ivanov
Keyword(s):  
Experimental Evidence ◽  
Synthetic Peptide ◽  
Biomedical Applications ◽  
Biological Properties ◽  
Peptide Drug ◽  
Wide Range ◽  
History Of ◽  
Available Information

The paper summarizes the available information concerning the biological properties and biomedical applications of Thymodepressin. This synthetic peptide drug displays pronounced immunoinhibitory activity across a wide range of conditions in vitro and in vivo. The history of its unforeseen discovery is briefly reviewed, and the current as well as potential expansion areas of medicinal practice are outlined. Additional experimental evidence is obtained, demonstrating several potential advantages of Thymodepressin over another actively used immunosuppressor drug, cyclosporin A.

scholarly journals Potential Combination of Xanthone Compounds from Mangosteen Fruit (Garcinia mangostana) with Eugenol Compounds in Basic Leaf (Ocimum sanctum) as Alternative Therapy in Preeclampsia

2021 ◽  
Vol 2 (2) ◽  
pp. 113-119
Author(s):  
Muhammad Al Farisi Sutrisno
Keyword(s):  
Target Genes ◽  
Alternative Therapy ◽  
Antioxidant Properties ◽  
Biological Properties ◽  
Primary Component ◽  
Ocimum Sanctum ◽  
Garcinia Mangostana ◽  
Pilot Studies ◽  
Beneficial Effects ◽  
Wide Range

Preeclampsia is a hyperdynamic condition that is syndromed by hypertension and proteinuria after 20 weeks of pregnancy. Preeclampsia incident is the first cause of 6-8 % number morbidity/mortality maternity and fetus in the world. Preeclampsia is related to the disability of physiology adaptation that can decrease perfusion of uteroplacental. Xanthone derivatives in mangosteen have been reported to possess a wide range of biological properties, including antioxidant and antihypertensive activities. Eugenol is a primary component of basil oil. It is known for its antioxidant, antiinflammatory, and vasorelaxant actions. These beneficial effects of eugenol make it an excellent therapeutic candidate for the treatment of hypertensive disorders of pregnancy. This study wants to analyze the best available research evidence on the potential combination of xanthone compounds from mangosteen fruit (Garcinia mangostana) with eugenol compounds in basil leaf (Ocimum sanctum) as an alternative therapy in preeclampsia.  A literature review was conducted in the electronic databases PubMed and Google Scholar using the index terms "xanthone" and "eugenol" and "hypertension" and "preeclampsia." All types of studies were included for this study, such as randomized controlled trials, systematic reviews, literature reviews, and pilot studies published between 2010 and 2021. Articles which not written in English were excluded from the study. This search resulted in 10 papers. Antioxidant properties of mangosteen peel extract compounds derived from xanthone, the most significant component is α-mangosteen and γ-mangosteen. Eugenol is vasorelaxant action by increasing the expression of its target genes, Sarco/endoplasmic reticulum Ca²⁺-ATPase and adequate potassium-calcium-activated potassium channels channel, thereby relaxing vascular smooth muscle cells and decreasing blood pressure. With this review, we suggest that eugenol, which is a vasorelaxant combined with xanthone which is an antioxidant by obstructing free radical and oxidative stress, can be a potent therapeutic for preeclampsia and intend to motivate researchers (e.g., chemistry, biology, pharmaceutical, and therapeutic areas) to provide evidence of these compounds for the management of preeclampsia.

scholarly journals Antibiogram and Phytochemical Analysis of Cinnamon, Clove, and Sichuan Pepper Extracts

2021 ◽  
Vol 9 (1) ◽  
pp. 1-7
Author(s):  
Bibek Adhikari ◽  
Pradeep Kumar Shah ◽  
Roman Karki
Keyword(s):  
Escherichia Coli ◽  
Pseudomonas Aeruginosa ◽  
Antimicrobial Activity ◽  
Candida Albicans ◽  
Proteus Mirabilis ◽  
Antimicrobial Properties ◽  
Antimicrobial Activities ◽  
Soxhlet Apparatus ◽  
Medicinal Plant Extracts ◽  
Wide Range

A wide range of medicinal plant extracts has phytochemicals that possess antimicrobial properties and these plants are used to treat several infections. The study aimed to assess the antimicrobial activities of some spices extracts and to evaluate the phytochemicals present in them. The extracts of spices were prepared using Soxhlet apparatus refluxing with methanol and ethanol. The well diffusion technique was implemented for the evaluation of antimicrobial activities of the extracts and the zone of inhibitions was recorded in millimeters. The antimicrobial test was done against five bacterial isolates: Escherichia coli, Proteus mirabilis, Pseudomonas aeruginosa, Salmonella enterica serotype Typhi, and Staphylococcus aureus and a fungal isolate: Candida albicans. The extracts were concentrated by Rotary Vacuum Evaporator and a stock solution of 200 mg/mL was prepared by dissolving in 10 % DMSO. Concentrations of 40, 60, 80 and 100 mg/mL extracts were used for antimicrobial activity. The result of this study showed that clove extracts had the highest antimicrobial property against all the test microorganisms. Methanolic extract of clove had the highest inhibitory effect against Proteus mirabilis (24.21±0.15 mm), Pseudomonas aeruginosa (19.78±0.23 mm), and Candida albicans (20.07±0.08 mm) whereas ethanolic extract was effective against Escherichia coli (20.44±0.16 mm), Salmonella Typhi (21.66±0.31 mm) and Candida albicans (21.11±0.09 mm). Cinnamon and pepper extracts, leaving some exceptions, also had antimicrobial properties. The presence of phytochemicals: polyphenols, flavonoids, and tannins are the major components responsible for antimicrobial activity. Thereby, this study successfully demonstrated the possibilities of using spices extracts in the treatment of microbial infections.

scholarly journals Phytochemical Characterization and Biological Evaluation of the Aqueous and Supercritical Fluid Extracts from Salvia sclareoides Brot

2017 ◽  
Vol 15 (1) ◽  
pp. 82-91
Author(s):  
Daniela Batista ◽  
Pedro L. Falé ◽  
Maria L. Serralheiro ◽  
Maria-Eduarda Araújo ◽  
Catarina Dias ◽  
...  
Keyword(s):  
Linoleic Acid ◽  
Supercritical Fluid ◽  
Antioxidant Properties ◽  
Biological Properties ◽  
Biological Evaluation ◽  
Cyclooxygenase 1 ◽  
Wide Range ◽  
Anti Inflammatory ◽  
Β Carotene

AbstractPlants belonging to the genus Salvia (Lamiaceae) are known to have a wide range of biological properties. In this work, extracts obtained from the aerial parts of Salvia sclareoides Brot. were evaluated to investigate their chemical composition, toxicity, bioactivity, and stability under in vitro gastrointestinal conditions. The composition of the supercritical fluid extract was determined by GC and GC-MS, while the identification of the infusion constituents was performed by HPLC-DAD and LC-MS. The in vitro cytotoxicity of both extracts (0-2 mg/mL) was evaluated in Caco-2 cell lines by the MTT assay. The anti-inflammatory and anticholinesterase activities were determined through the inhibition of cyclooxygenase-1 and acetylcholinesterase enzymes, while β-carotene/linoleic acid bleaching test and the DPPH assays were used to evaluate the antioxidant activity. The infusion inhibited cyclooxygenase-1 (IC50 = 271.0 μg/mL), and acetylcholinesterase (IC50 = 487.7 μg/ mL) enzymes, also demonstrated significant antioxidant properties, as evaluated by the DPPH (IC50 = 10.4 μg/mL) and β-carotene/linoleic acid (IC50 = 30.0 μg/mL) assays. No remarkable alterations in the composition or in the bioactivities of the infusion were observed after in vitro digestion, which supports the potential of S. sclareoides as a source of bioactive ingredients with neuroprotective, anti-inflammatory and antioxidant properties.

scholarly journals Phage phiKZ—The First of Giants

Viruses ◽  
2021 ◽  
Vol 13 (2) ◽  
pp. 149
Author(s):  
Victor Krylov ◽  
Maria Bourkaltseva ◽  
Elena Pleteneva ◽  
Olga Shaburova ◽  
Sergey Krylov ◽  
...  
Keyword(s):  
Pseudomonas Aeruginosa ◽  
Phage Therapy ◽  
Phage Genome ◽  
Lytic Activity ◽  
Wide Range ◽  
History Of ◽  
Dna Packing ◽  
Characteristic Manner

The paper covers the history of the discovery and description of phiKZ, the first known giant bacteriophage active on Pseudomonas aeruginosa. It also describes its unique features, especially the characteristic manner of DNA packing in the head around a cylinder-shaped structure (“inner body”), which probably governs an ordered and tight packaging of the phage genome. Important properties of phiKZ-like phages include a wide range of lytic activity and the blue opalescence of their negative colonies, and provide a background for the search and discovery of new P. aeruginosa giant phages. The importance of the phiKZ species and of other giant phage species in practical phage therapy is noted given their broad use in commercial phage preparations.

Vitamins in Human Health

2006 ◽  
Author(s):  
Yu.M. Parkhomenko ◽  
◽  
G.V. Donchenko ◽  
Keyword(s):  
Human Health ◽  
Biological Properties ◽  
General Information ◽  
Health Issues ◽  
Wide Range ◽  
Modern Classification ◽  
History Of ◽  
Fat Soluble Vitamins ◽  
And Storage

The book describes the history of the discovery of vitamins, presents modern ideas about the properties of vitamins and their importance for humans as essential nutritional factors. General information is provided about the modern classification of vitamins, physicochemical and biological properties of water- and fat-soluble vitamins and vitamin-like compounds, their role in metabolism and, in general, in human health. The causes of hypovitaminosis are analyzed, advice is given on their prevention and storage of vitamins in food. The book is intended for specialists in the field of biology, medicine, as well as for a wide range of readers, including teachers, students and other people interested in health issues.

The prediction of the spectrum of biological activity and antimicrobial properties of diaminoazoles

2019 ◽  
Vol 65 (2) ◽  
pp. 99-102 ◽  
Author(s):  
Yu.V. Butina ◽  
T.V. Kudayarova ◽  
E.A. Danilova ◽  
M.K. Islyaikin
Keyword(s):  
Antibacterial Activity ◽  
Biological Activity ◽  
Antimicrobial Properties ◽  
Biological Properties ◽  
Diffusion Method ◽  
Bacterial Strains ◽  
Wide Range ◽  
Alternative Drugs

The work is devoted to predicting and studying biological properties of N-substituted analogs of 3,5-diamino-1,2,4-thiadiazole, which, in their turn, include in the composition of many drugs that exhibit a wide range of pharmacological actions. For searching of new alternative drugs with an antibacterial activity, but lacking resistance of microorganism strains to them, a computer screening of 2N-alkyl-substituted 5-amino-3-imino-1,2,4-thiadiazolines previously synthesized by us was carried out. The prediction of the spectrum of biological activity, as well as the determination of the probable toxicity of these compounds, was performed using the freely available computer programs PASS, Anti-Bac-Pred, and GUSAR. The study of the antibacterial activity in vitro against gram-positive (Staphylococcus aureus, Staphylococcus saprophyticus, Staphylococcus epidermidis) and gram-negative (Escherichia coli, Pseudomonas aeruginosae) bacterial strains was performed by the disco-diffusion method. Experimental data roughly correspond to the predictions.

scholarly journals Forbidden triads and innovation

2019 ◽  
Author(s):  
Balazs Vedres ◽  
Tunde Cserpes
Keyword(s):  
Network Structure ◽  
High Weight ◽  
Structural Diversity ◽  
Project Teams ◽  
Weak Ties ◽  
Strong Ties ◽  
Wide Range ◽  
History Of

This article investigates the importance of forbidden triads – high weight open triads – for a wide range of success measures in the history of recorded jazz. Innovative teams face the paradox of relying on experience to generate novelty. We argue that forbidden triads, as conjunctures of dyadic experience, are the locations where successful novel combinations can be recognized and realized. Prior scholarship has sidelined such network structural diversity with strong ties, and assumed that strong ties are mostly closed, and weak ties connect to diverse structural locations. We use data on all recording sessions of more than a century of jazz to show that forbidden triad is the only consistent predictor of six measures of success that span the dualities of insiders and outsiders, and voice and trace. This network structure is also the only predictor of deep success: coinciding success in all four quadrants. Furthermore, forbidden triads that require effort beyond easy structural availability contribute in addition to voice measures of success. We discuss implications for project teams and organizations where innovation is a key goal.

Biomedical and Pharmaceutical-Related Applications of Laccases

2020 ◽  
Vol 21 (1) ◽  
pp. 78-98
Author(s):  
Elham Mohit ◽  
Maryam Tabarzad ◽  
Mohammad Ali Faramarzi
Keyword(s):  
Oxidative Polymerization ◽  
Antioxidant Properties ◽  
Antimicrobial Properties ◽  
Wound Dressings ◽  
Biotechnological Applications ◽  
Antiproliferative Agents ◽  
Lignocellulosic Fiber ◽  
Wide Range ◽  
Catalyzed Reactions ◽  
Vast Range

The oxidation of a vast range of phenolic and non-phenolic substrates has been catalyzed by laccases. Given a wide range of substrates, laccases can be applied in different biotechnological applications. The present review was conducted to provide a broad context in pharmaceutical- and biomedical- related applications of laccases for academic and industrial researchers. First, an overview of biological roles of laccases was presented. Furthermore, laccase-mediated strategies for imparting antimicrobial and antioxidant properties to different surfaces were discussed. In this review, laccase-mediated mechanisms for endowing antimicrobial properties were divided into laccase-mediated bio-grafting of phenolic compounds on lignocellulosic fiber, chitosan and catheters, and laccase-catalyzed iodination. Accordingly, a special emphasis was placed on laccase-mediated functionalization for creating antimicrobials, particularly chitosan-based wound dressings. Additionally, oxidative bio-grafting and oxidative polymerization were described as the two main laccase-catalyzed reactions for imparting antioxidant properties. Recent laccase-related studies were also summarized regarding the synthesis of antibacterial and antiproliferative agents and the degradation of pharmaceuticals and personal care products.

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