scholarly journals Antimicrobial Activity of Ultrasonic Extracts of Two Chemotypes of Thymus serpyllum L. of Central Kazakhstan and their Polyphenolic Profiles

2021 ◽  
Vol 9 (A) ◽  
pp. 61-67
Author(s):  
Svetlana Ivasenko ◽  
Perizat Orazbayeva ◽  
Krystyna Skalicka–Wozniak ◽  
Agnieszka Ludwiczuk ◽  
Alexandr Marchenko ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Wide Spectrum ◽  
Biological Properties ◽  
Climatic Conditions ◽  
Biologically Active ◽  
Gram Positive Bacteria ◽  
Quantitative Content ◽  
Two Samples ◽  
Thymus Serpyllum ◽  
Bacteria And Fungi

BACKGROUND: The medicinal plant of Thymus serpyllum L. in nature, depending on the geographical region, climatic conditions, and growing environment, is represented with some chemotypes. Composition and quantitative content of the basic groups of the biologically active substances can be differed, and thus their biological properties are also various. AIM: The aim of the study was to determine possibility of the using the ultrasonic extracts of two chemotypes of T. serpyllum L. of Central Kazakhstan as an antimicrobial agent against test strains of microorganisms. MATERIALS AND METHODS: Two samples of T. serpyllum were extracted with 70% ethanol using ultrasound. The polyphenol content of the ultrasound extracts was determined using the LC-ultraviolet-ESI- tandem mass spectrometry technique. A study of an antimicrobial activity of the ultrasonic extracts was performed with eight strains of Gram-positive bacteria, six strains of Gram-negative bacteria, and four cultures of fungi. RESULTS: The ultrasonic extracts of two chemotypes of T. serpyllum L. are similar in composition of phenolic compounds but differ in a quantitative content of phenolic acids and flavonoids, except for a rosmarinic acid. The ultrasonic extracts have a wide spectrum of antimicrobial activity, exhibit the bactericidal or bacteriostatic activity against all tested bacteria and fungi at a concentration of 0.0625–20 mg/ml, but differ in their strength of action against test strains of microorganisms. CONCLUSION: The ultrasonic extracts of two chemotypes of T. serpyllum L. of Central Kazakhstan can be considered as a potential drug with a wide spectrum of antimicrobial activity. The results of chromatographic analysis will be used for standardization of a drug.

scholarly journals Microwave Synthesis, Characterization, and Antimicrobial Activity of Some Novel Isatin Derivatives

2015 ◽  
Vol 2015 ◽  
pp. 1-8 ◽  
Author(s):  
Ayman El-Faham ◽  
Wael N. Hozzein ◽  
Mohammad A. M. Wadaan ◽  
Sherine N. Khattab ◽  
Hazem A. Ghabbour ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Carboxylic Acid ◽  
Fungal Pathogens ◽  
Biologically Active ◽  
Moderate Activity ◽  
Gram Positive ◽  
X Ray Crystallography ◽  
Gram Positive Bacteria ◽  
Bacteria And Fungi ◽  
Isatin Derivatives

Three series of isatin derivatives [3-hydrazino, 3-thiosemicarbazino, and 3-imino carboxylic acid derivatives] were synthesized employing microwave irradiation. The prepared compounds were characterized by FT-IR, NMR, elemental analysis, and X-ray crystallography for derivatives5b. The synthesized compounds were screened for antimicrobial activity against selected bacteria and fungi. The results revealed that theN-alkyl isatin derivatives were biologically active with different spectrums activity. Most of the 3-hydrazino and 3-thiosemicarbazino isatin derivatives were biologically inactive and generally the active derivatives showed weak to moderate activity mainly against Gram-positive bacteria. The imino isatin carboxylic acid derivatives (2-[4-(1-benzyl-5-bromo-2-oxoindolin-3-ylideneamino) phenyl]acetic acid,5d) showed promising activity against all tested Gram-positive bacteria and against fungal pathogens.

scholarly journals Plant antimicrobial peptides: structures, functions, and applications

2021 ◽  
Vol 62 (1) ◽  
Author(s):  
Junpeng Li ◽  
Shuping Hu ◽  
Wei Jian ◽  
Chengjian Xie ◽  
Xingyong Yang
Keyword(s):  
Antimicrobial Activity ◽  
Antimicrobial Peptides ◽  
Agricultural Production ◽  
Food Additives ◽  
Antimicrobial Activities ◽  
Gram Positive Bacteria ◽  
Potential Applications ◽  
Potential Applicability ◽  
Bacteria And Fungi ◽  
Positively Charged

AbstractAntimicrobial peptides (AMPs) are a class of short, usually positively charged polypeptides that exist in humans, animals, and plants. Considering the increasing number of drug-resistant pathogens, the antimicrobial activity of AMPs has attracted much attention. AMPs with broad-spectrum antimicrobial activity against many gram-positive bacteria, gram-negative bacteria, and fungi are an important defensive barrier against pathogens for many organisms. With continuing research, many other physiological functions of plant AMPs have been found in addition to their antimicrobial roles, such as regulating plant growth and development and treating many diseases with high efficacy. The potential applicability of plant AMPs in agricultural production, as food additives and disease treatments, has garnered much interest. This review focuses on the types of plant AMPs, their mechanisms of action, the parameters affecting the antimicrobial activities of AMPs, and their potential applications in agricultural production, the food industry, breeding industry, and medical field.

scholarly journals The Search for Biologically Active Compounds in the Series of N-ethoxyethylpiperidine Derivatives

2019 ◽  
Vol 21 (2) ◽  
pp. 125
Author(s):  
U.B. Issayeva ◽  
G.S. Akhmetova ◽  
U.M. Datkhayev ◽  
M.T. Omyrzakov ◽  
K.D. Praliyev ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Biologically Active ◽  
Hydroxyl Group ◽  
Diffusion Method ◽  
Acylation Reaction ◽  
Gram Positive Bacteria ◽  
Cyclopropanecarboxylic Acid ◽  
Yeast Fungus ◽  
Acid Esters

With the aim to introduce fragment of cyclopropane and fragments of p-, m-, o-fluorophenyls into the structures of N-ethoxyethylpiperidines, acylation of oxime and phenylacetylenic alcohol of 1-(2-ethoxyethyl)-4-ketopiperidine by cyclopropanecarbonylchloride was carried out; on the basis of 1-(2-ethoxyethyl)-4-ethynyl-4-hydroxypiperidine (cascaine alcohol), acylation by 4-fluoro-, 3-fluoro-, 2-fluorobenzoylchlorides was carried out with formation of the corresponding piperidine containing hydrochlorides of cyclopropanecarboxylic acid esters and para-, meta-, ortho-fluorobenzoic esters. Acylation reaction on the hydroxyl group of compounds is carried out in absolute dioxane, the acylating agents are cyclopropanecarbonylchloride, p-, m-, o-fluorobenzoyl chlorides taken in excess. The obtained esters of cyclopropanecarboxylic and para-, meta-, ortho-fluorobenzoic acids are crystalline substances with a clear melting point, well soluble in water, ethanol, acetone. P-fluorobenzoates are obtained with better yields, m-fluorobenzoates occupy an intermediate position, and o-fluorobenzoates are formed with the lowest yields. The best yields of fluorobenzoates are obtained using dioxane as a solvent. Para-, meta-, ortho-fluorobenzoic esters of 1-(2-ethoxyethyl)-4-ethynyl-4-hydroxypiperidine coded A-4 – A-6 were studied for the presence of antimicrobial activity, the actions of these preparations were evaluated in vitro in relation to strains of gram-positive bacteria Staphylococcus aureus, Bacillus subtilis, gram-negative strains of Escheriсhia coli, Pseudomonas aeruginosa and to yeast fungus Сandida albicans by the diffusion method into agar (holes). Introduction of fluorine atom into the structure of cascaine lead to manifestation of antimicrobial activity.

scholarly journals RECENTES AVANÇOS NA FUNCIONALIZAÇÃO SELETIVA DE QUINOLINAS

Química Nova ◽  
2021 ◽  
Author(s):  
Dartagnan Ferreira ◽  
Valter Murie ◽  
Thiago Santos ◽  
Paulo Vieira ◽  
Giuliano Clososki
Keyword(s):  
Wide Spectrum ◽  
Structural Diversity ◽  
Biological Properties ◽  
Biologically Active ◽  
Chemical Transformations ◽  
Heterocyclic Molecules ◽  
Point Of Interest ◽  
Selective Functionalization ◽  
Biological Interest ◽  
Approved Drugs

RECENT ADVANCES IN SELECTIVE FUNCTIONALIZATION OF QUINOLINES. Heterocyclic compounds form an important and extensive group of organic substances. Among nitrogenous heterocyclic molecules, quinolines stand out for exhibiting attractive chemical and biological properties. These substances can be used as ligands, sensors, luminescent and agrochemical materials. In addition, quinoline-containing compounds can exhibit a wide spectrum of pharmacological properties, allowing their use in several approved drugs nowadays. Due to its importance, the synthesis of molecules containing this nucleus becomes a point of interest for synthetic chemists. In this way, several methodologies have been recently developed to prepare quinoline derivatives with high structural diversity. Such chemical transformations allow the chemical modification of these rings with high selectivity and tolerance to diverse functional groups and these properties have been conveniently used in the preparation of biologically active molecules containing this unit. Herein, we present a review of the main methodologies employed in the selective functionalization of quinolines in the last twenty years. In this context, a brief introduction addressing general synthetic and medicinal aspects related to the functionalization positions of the quinoline ring is presented. Several methodologies used in the functionalization of this moiety are discussed, as well relevant synthetic applications, both in the preparation and functionalization of substances of biological interest.

ANTIMICROBIAL ACTIVITY OF COPPER KAOLINITE AND SURFACTANT MODIFIED COPPER KAOLINITE AGAINST GRAM POSITIVE AND GRAM NEGATIVE BACTERIA

2016 ◽  
Vol 78 (3-2) ◽  
Author(s):  
Nor Syafawani Sarah Md Saad ◽  
Nik Ahmad Nizam Nik Malek ◽  
Chun Shiong Chong
Keyword(s):  
Antimicrobial Activity ◽  
Synergistic Effects ◽  
Wide Spectrum ◽  
Copper Nitrate ◽  
Gram Negative Bacteria ◽  
Gram Positive ◽  
Gram Negative ◽  
X Ray ◽  
Gram Positive Bacteria ◽  
Diffusion Technique

The aim of this research was to determine the antimicrobial activity of kaolinite modified with antimicrobial compounds against Gram positive and Gram negative bacteria. Copper kaolinite (Cu-kaolinite) was prepared by loading raw kaolinite with copper nitrate trihydrate (CuNO3) while surfactant modified Cu-kaolinite (SM-Cu-kaolinite) was prepared by adding cationic surfactants hexadecyltrimethyl ammonium (HDTMA) on Cu-Kaolinite. Samples was characterized by Fourier transform infrared spectroscopy (FTIR), X-ray diffraction (XRD), scanning electron microscopy (SEM) and energy dispersive X-ray (EDX) analyzer. The antimicrobial activity of the samples was tested against Gram negative bacteria (Escherichia coli ATCC 11229 and Pseudomonas aeruginosa ATCC 15442), and Gram positive bacteria (Staphylococcus aureus ATCC 6538 and Enterococcus faecalis ATCC 29212) through disc diffusion technique (DDT) and minimum inhibition concentration (MIC). The results showed that the antimicrobial activity of Cu-kaolinite increased after modified with HDTMA due to the synergistic effects of Cu ions and HDTMA molecules on the kaolinite. The antimicrobial activity for surfactant modified Cu-kaolinite was greater for Gram positive bacteria compared to Gram negative bacteria. In conclusion, the attachment of HDTMA on Cu-kaolinite contributed to the enhanced antimicrobial activity against wide spectrum of bacteria (Gram positive and Gram negative bacteria).

scholarly journals Synthesis and Evaluation of Antimicrobial and Cytotoxic Activity of Oxathiine-Fused Quinone-Thioglucoside Conjugates of Substituted 1,4-Naphthoquinones

Molecules ◽  
2020 ◽  
Vol 25 (16) ◽  
pp. 3577
Author(s):  
Yuri E. Sabutski ◽  
Ekaterina S. Menchinskaya ◽  
Ludmila S. Shevchenko ◽  
Ekaterina A. Chingizova ◽  
Artur R. Chingizov ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Cytotoxic Activity ◽  
Antimicrobial Activities ◽  
Biologically Active ◽  
Hydroxyl Group ◽  
Diffusion Method ◽  
Gram Positive ◽  
Gram Positive Bacteria ◽  
High Cytotoxic Activity ◽  
Derivatives Of

A series of new tetracyclic oxathiine-fused quinone-thioglycoside conjugates based on biologically active 1,4-naphthoquinones and 1-mercapto derivatives of per-O-acetyl d-glucose, d-galactose, d-xylose, and l-arabinose have been synthesized, characterized, and evaluated for their cytotoxic and antimicrobial activities. Six tetracyclic conjugates bearing a hydroxyl group in naphthoquinone core showed high cytotoxic activity with EC50 values in the range of 0.3 to 0.9 μM for various types of cancer and normal cells and no hemolytic activity up to 25 μM. The antimicrobial activity of conjugates was screened against Gram-positive bacteria (Staphylococcus aureus, Bacillus cereus), Gram-negative bacteria (Pseudomonas aeruginosa and Escherichia coli), and fungus Candida albicans by the agar diffusion method. The most effective juglone conjugates with d-xylose or l-arabinose moiety and hydroxyl group at C-7 position of naphthoquinone core at concentration 10 µg/well showed antimicrobial activity comparable with antibiotics vancomicin and gentamicin against Gram-positive bacteria strains. In liquid media, juglone-arabinosidic tetracycles showed highest activity with MIC 6.25 µM. Thus, a positive effect of heterocyclization with mercaptosugars on cytotoxic and antimicrobial activity for group of 1,4-naphthoquinones was shown.

Influence of structure of lactones with the methylcyclohexene and dimethylcyclohexene ring on their biotransformation and antimicrobial activity

2017 ◽  
Vol 72 (5-6) ◽  
pp. 209-217 ◽  
Author(s):  
Katarzyna Wińska ◽  
Małgorzata Grabarczyk ◽  
Wanda Mączka ◽  
Barbara Żarowska ◽  
Gabriela Maciejewska ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Biological Properties ◽  
Penicillium Expansum ◽  
Equatorial Position ◽  
Substrate Structure ◽  
Cyclohexene Ring ◽  
Yeast Strains ◽  
Bacteria And Fungi ◽  
Unsaturated Lactones ◽  
The Relationship

Abstract The aim of this article is influence of the structure of lactones with the methylcyclohexene and dimethylcyclohexene ring on their biotransformation and antimicrobial activity. This work was based on the general remark that even the smallest change in the structure of a compound can affect its biological properties. The results of the biotransformation of four bicyclic unsaturated lactones with one or two methyl groups in the cyclohexene ring was tested using fifteen fungal strains (Fusarium species, Penicillium species, Absidia species, Cunninghamella japonica, and Pleurotus ostreatus) and five yeast strains (Yarrowia lipolytica, Rhodorula marina, Rhodorula rubra, Candida viswanathii, and Saccharomyces cerevisiae). During these transformations, new epoxylactone and hydroxylactone were obtained. The relationship between the substrate structure and the ability of the microorganisms to transform them were analysed. Only compounds with C–O bond of lactone ring in the equatorial position were transformed by fungus. All presented here lactones were examined also for their antimicrobial activity. It turned out that these compounds exhibited growth inhibition of bacteria and fungi, mainly Bacillus subtilis, Candida albicans, Aspergillus niger, and Penicillium expansum.

scholarly journals Synthesis and Antimicrobial Activity of Burkholderia-Related 4-Hydroxy-3-Methyl-2-Alkenylquinolones (HMAQs) and Their N-Oxide Counterparts

2020 ◽  
Author(s):  
Marianne Piochon ◽  
Pauline M. L. Coulon ◽  
Armand Caulet ◽  
Marie-Christine Groleau ◽  
Eric Déziel ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Biologically Active ◽  
Specific Class ◽  
Gram Positive ◽  
Carbonate Group ◽  
Gram Positive Bacteria ◽  
Alkenyl Chain ◽  
Optimized Conditions ◽  
Burkholderia Ambifaria

ABSTRACT: The Burkholderia genus offers a promising potential in medicine because of the diversity of biologically active natural products encoded in its genome. Some pathogenic Burkholderia spp. biosynthesize a specific class of antimicrobial 2-alkyl-4(1H)-quinolones, i.e., 4-hydroxy-3-methyl-2-alkenylquinolones (HMAQs) and their N-oxide derivatives (HMAQNOs). Herein, we report the synthesis of a series of six HMAQs and HMAQNOs featuring a trans-∆<sup>2</sup> double bond at the C2-alkyl chain. The quinolone scaffold was obtained via the Conrad-Limpach approach while the (E)-2-alkenyl chain was inserted through Suzuki-Miyaura cross-coupling under microwave radiation without noticeable isomerization according to the optimized conditions. Subsequent oxidation of enolate-protected HMAQs cleanly led to the formation of HMAQNOs following cleavage of the ethyl carbonate group. Synthetic HMAQs and HMAQNOs were in vitro evaluated for their antimicrobial activity against different Gram-negative and Gram-positive bacteria as well as against fungi and yeasts. The biological results support and extend the potential of HMAQs and HMAQNOs as antimicrobials, especially against Gram-positive bacteria. We also confirm the involvement of HMAQs in the autoregulation of the Hmq system in Burkholderia ambifaria.

scholarly journals Applications substituted 2-aminothiophenes in drug design

2021 ◽  
Vol 9 (2) ◽  
Author(s):  
Zita Puterová ◽  
Alžbeta Krutošíková ◽  
Daniel Végh
Keyword(s):  
Antimicrobial Activity ◽  
Drug Design ◽  
Adenosine Receptor ◽  
Biologically Active Compounds ◽  
Biologically Active ◽  
A1 Adenosine Receptor ◽  
Active Compounds ◽  
Thiophene Derivatives ◽  
Anti Inflammatory ◽  
Bacteria And Fungi

Highly substituted thiophene derivatives are important heterocycles found in numerous biologically active compounds. Title compounds are attractive derivatives because their applications in pharmaceuticals, agriculture and pesticides. They exhibit antimicrobial activity against various Gram(+) and Gram(-) bacteria and fungi. Many of these molecules act as allosteric enhancers of A1-adenosine receptor, glucagon antagonists as well as antioxidant and anti-inflammatory agents.

Biologically active binaphthol-scaffolded imidazolium salts

MedChemComm ◽  
2014 ◽  
Vol 5 (4) ◽  
pp. 436-440 ◽  
Author(s):  
Marc Vidal ◽  
Claude-Rosny Elie ◽  
Shirley Campbell ◽  
Audrey Claing ◽  
Andreea R. Schmitzer
Keyword(s):  
Antimicrobial Activity ◽  
Lipid Membrane ◽  
Biologically Active ◽  
Imidazolium Salts ◽  
Gram Positive ◽  
Gram Positive Bacteria

This work describes the antimicrobial activity and selectivity for Gram-positive bacteria of imidazolium-functionalized binols, as a result of their insertion into the lipid membrane and alteration of its permeability.

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