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Search results for: antifungal drugs
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Inhibitors of glucosamine-6-phosphate synthase as potential antifungal drugs.
PublicationPrzedstawiono stan obecny i perspektywy zastosowania inhibitorów enzymu syntazy GlcN-6-P jako leków skutecznych w leczeniu grzybic układowych. Używając metod modelowania molekularnego zaprojektowano struktury inhibitorów enzymu należących do dwóch grup strukturalnych: analogów glutaminy oraz analogów stanu przejściowego reakcji katalizowanej przez enzym. Opracowano metody syntezy pochodnych zoptymalizowanych inhibitorów, wykazujących...
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Homoisocitrate dehydrogenase from Candida albicans: properties, inhibition, and targeting by an antifungal pro-drug
PublicationThe LYS12 gene from Candida albicans, coding for homoisocitrate dehydrogenase was cloned and expressed as a His-tagged protein in Escherichia coli. The purified gene product catalyzes the Mg2+- and K+-dependent oxidative decarboxylation of homoisocitrate to alpha-ketoadipate. The recombinant enzyme demonstrates strict specificity for homoisocitrate. SDS-PAGE of CaHIcDH revealed its molecular mass of 42.6±1 kDa, while in size-exclusion...
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Disposition of Drugs of Abuse and Their Metabolites in Wastewater as a Method of the Estimation of Drug Consumption
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Methods for Elucidation of DNA-Anticancer Drug Interactions and Their Applications in the Development of New Drugs
PublicationDNA damaging agents including anthracyclines, camptothecins and platinum drugs are among most frequently used drugs in the chemotherapeutic routine. Due to their relatively low selectivity for cancer cells, administration is associated with adverse side effects, whereas the inherent genotoxicity of these drugs is associated with risk of developing secondary cancers. Development of new drugs, which could be spared of these drawbacks...
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Optical properties of the chemotherapy drugs used in the central nervous system lymphoma therapy: monitoring drug delivery
PublicationOur aim is to optically monitor the delivery of the chemotherapy drugs for brain tumours, particularly used in the central nervous system (CNS) lymphoma therapy. In vivo monitoring would help to optimize the treatment and avoiding unnecessary medications. Moreover, it would be beneficial to be able to measure which of the multi-regimen drugs actually do penetrate and how well into the brain tissue. There exist several potential...
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Glutathione-mediated conjugation of anticancer drugs: an overview of reaction mechanisms and biological significance for drug detoxification and bioactivation.
PublicationThe effectiveness of many anticancer drugs depends on the creation of specific metabolites that may alter their therapeutic or toxic properties. One significant route of biotransformation is a conjugation of electrophilic compounds with reduced glutathione, which can be non-enzymatic and/or catalyzed by glutathione-dependent enzymes. Glutathione usually combines with anticancer drugs and/or their metabolites to form more polar...
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Drugs and driving
PublicationW referacie przedstawiono we wprowadzeniu pojawienie się nowego zagrożenia, jakim jest kierowanie pojazdów przez osoby będące pod wpływek narkotyków. W drugiej części przedstawiono obecnie obowiązujące sankcje, jakie mogą spotkać kierującego oraz definicję środków odurzających, po zażyciu których nie można prowadzić samochodu. W trzeciej części przedstawiono badania naukowe przeprowadzone w Polsce i Niemczech, które pokazują jak...
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Evaluation of Antifungal Properties of Titania P25
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‘Acridines’ as New Horizons in Antifungal Treatment
PublicationFrequent fungal infections in immunocompromised patients and mortality due to invasive mycosis are important clinical problems. Opportunistic pathogenic Candida species remain one of the leading causes of systemic mycosis worldwide. The repertoire of antifungal chemotherapeutic agents is very limited. Although new antifungal drugs such as lanosterol 14α-demethylase and β-glucan synthase inhibitors have been introduced into clinical...
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Novel dendrimeric lipopeptides with antifungal activity
PublicationZaprojektowano, zsyntezowano i scharakteryzowano serię nowych kationowych lipopeptydów zawierających rozgałęziony, amfifilowy polarny rdzeń strukturalny pochodzący od dendronu (Lys)(Lys)(Lys) oraz łańcuchy C8 i C12 na C-końcu. Otrzymane zwiazki wykazywały aktywność przeciwdrobnoustrojową, w tym szczególnie przeciwgrzybową wobec drożdżaków z rodzaju Candida. Najwyższą aktywność, selektywną wobec drobnoustrojów grzybowych, wykazywały...
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Antifungal Activity of Homoaconitate and Homoisocitrate Analogs
PublicationThirteen structural analogs of two initial intermediates of the L-alpha-aminoadipate pathway of L-lysine biosynthesis in fungi have been designed and synthesized, including fluoro- and epoxy-derivatives of homoaconitate and homoisocitrate. Some of the obtainedcompounds exhibited at milimolar range moderate enzyme inhibitory properties against homoaconitase and/or homoisocitrate dehydrogenase of Candida albicans. The structural...
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How do sterols determine the antufungal activitiy of amphotericin B? Free energy of binding between the drug and its membrane targets.
PublicationAmphotericin B (AmB) is a well-known polyene antibiotic used to treat systemic fungal infections. It is commonly accepted that the presence of sterols in the membrane is essential for the AmB biological activity, that is, for the formation of transmembrane ion channels. The selective toxicity of AmB for fungal cells is attributed to the fact that it is more potent against fungal cell membranes containing ergosterol than against...
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Piperine Targets Different Drug Resistance Mechanisms in Human Ovarian Cancer Cell Lines Leading to Increased Sensitivity to Cytotoxic Drugs
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Antifungal Activity and Synergism with Azoles of Polish Propolis
PublicationThe aim of our work was to check if one of the products of natural origin, namely honey 19 bee propolis may be an alternative or supplement to currently used antifungal agents. The activity 20 of 50 ethanolic extracts of propolis (EEPs), harvested in Polish apiaries, was tested on a group of 69 21 clinical isolates of C. albicans. Most of the EEPs showed satisfactory activity, with minimum 22 fungicidal concentrations (MFC) mainly...
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Antifungal action of the oxathiolone-fused chalcone derivative
PublicationAMG-148, pochodna chalkonu z pierścieniem oksatiolonowym, wykazuje aktywność przeciwgrzybową in vitro wobec szczepów grzybowych patogennych dla człowieka, z wartościami minimalnych stężeń hamujących wzrost mieszczących się w zakresie 1-16 mikrogramów na mililitr, natomiast w wyższych stężeniach związek ten działa grzybobójczo. Obecność głównych białek oporności wielolekowej, Cdr1p, Cgr2p lub Mdr1p nie wpływa znacząco na aktywność...
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Antifungal dipeptides incorporating an inhibitor of homoserine dehydrogenase
PublicationThe antifungal activity of 5‐hydroxy‐4‐oxo‐L‐norvaline (HONV), exhibited under conditions mimicking human serum, may be improved upon incorporation of this amino acid into a dipeptide structure. Several HONV‐containing dipeptides inhibited growth of human pathogenic yeasts of the Candida genus in the RPMI‐1640 medium, with minimal inhibitory concentration values in the 32 to 64 μg mL−1 range. This activity was not affected by multidrug...
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Inhibitors of amino acids biosynthesis as antifungal agents
PublicationFungal microorganisms, including the human pathogenic yeast and filamentous fungi, are able to synthesize all proteinogenic amino acids, including nine that are essential for humans. A number of enzymes catalyzing particular steps of human-essential amino acid biosynthesis are fungi specific. Numerous studies have shown that auxotrophic mutants of human pathogenic fungi impaired in biosynthesis of particular amino acids exhibit...
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Targeting DNA Topoisomerase II in Antifungal Chemotherapy.
PublicationTopoisomerase inhibitors have been in use clinically for the treatment of several diseases for decades. Although those enzymes are significant molecular targets in antibacterial and anticancer chemotherapy very little is known about the possibilities to target fungal topoisomerase II (topo II). Raising concern for the fungal infections, lack of effective drugs and a phenomenon of multidrug resistance underlie a strong need to expand...
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Molecular Umbrella as A Nanocarrier for Antifungals
PublicationA molecular umbrella composed of two O‐sulfated cholic acid residues was applied for the construction of conjugates with cispentacin, containing a “trimethyl lock” (TML) or o‐dithiobenzylcarbamoyl moiety as a cleavable linker. Three out of five conjugates demonstrated antifungal in vitro activity against C. albicans and C. glabrata but not against C. krusei, with MIC90 values in the 0.22–0.99 mM range and were not hemolytic. Antifungal...
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Fatty acids as molecular carriers in cleavable antifungal conjugates
PublicationConjugates composed of C2-18 fatty acid (FA) residues as a molecular carrier and 5-fluorocytosine (5-FC) as an active agent, released upon the action of intracellular esterases on the ester bond between FA and “trimethyl lock” intramolecular linker, demonstrate good in vitro activity against human pathogenic yeasts of Candida spp. The minimal inhibitory concentrations (MIC) values for the most active conjugates containing caprylic...
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Investigation of antifungal and antibacterial potential of green extracts of propolis
PublicationPropolis extracts have been used in traditional medicines since ages due to its advantageous complex chemical composition. However, the antibacterial and antifungal activity of poplar propolis extracts prepared in Natural Deep Eutectic Solvent (NADES) are seldom studied. This study investigates suitable alternate for ethanol as a solvent for extraction for Polish poplar propolis. It also attempts to identify suitable extraction...
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Polyurethanes as a carrier of drugs for gentamicin
PublicationGentamicin is one of the most popular drug and is widely used due to its antibiotic properties. 3% of world production of polyurethanes (PU) is dedicated to biomedical applications, where they can serve are parts of orthopedic prosthesis or artificial organs, disposable medical devices, wound and burn dressing, contact lenses among others. In the study, to obtain drug carriers, a combination of these two materials were prepared...
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Primary degradation of antidiabetic drugs
PublicationType 2 diabetes is a chronic disease affecting a large portion of the world population and is treated by orally administered drugs. Since these drugs are often taken in high doses and are excreted unchanged or partially metabolised many of them are nowadays detected in surface waters or wastewater treatment plants effluents. Unmetabolised antidiabetics or some of their transformation products retain their pharmacological activity,...
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Peptide dendrimers as antifungal agents and carriers for potential antifungal agent—N3‐(4‐methoxyfumaroyl)‐(S)‐2,3‐ diaminopropanoic acid—synthesis and antimicrobial activity
PublicationA series of peptide dendrimers and their conjugates with antimicrobial agent FMDP (N3‐(4‐methoxyfumaroyl)‐(S)‐2,3‐diamino‐propanoic acid) were synthesized. The obtained compounds were tested for the antibacterial and antifungal activity. All novel dendrimers displayed much better activity against the tested strains than FMDP itself. Moreover, their conjugates with FMDP also exhibited antimicrobial activity. The most promising molecules...
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Antimicrobial and antifungal activities of the extracts and essential oils of Bidens tripartita.
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Enzymes of the lysine biosynthetic pathway as targets for antifungals ?
PublicationSystemic infections caused by human pathogenic fungi in immunocompromized patients continue to be one of the important clinical problems. Limited availability of safe and efficacious antifungal chemotherapeutics and emerging resistance to existing drugs stimulates search for novel molecular targets for antifungals. The α-aminoadipate pathway (AAP) of L-lysine biosynthesis is unique in fungi and thus has been so far considered...
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Synthesis and Study of Antifungal Properties of New Cationic Beta-Glucan Derivatives
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Antifungal activity of thionated analogues of nva-fmdp and lys-nva-fmdp
Publicationotrzymano dwa peptydy w których wiązanie amidowe łączące aminokwasy zamieniono na tioamidowe w wyniku kilkunastoetapowej syntezy chemicznej. do reakcji tionowania zastosowano odczynnik lawessona. otrzymane związki poddano badaniom aktywności z wykorzystaniem pięciu szczepów candida , w tym szczepów opornych na flukonazol. stwierdzono, ze obecniość wiązania tioamidowego znacznie obniża aktywność przeciwgrzybową testowanych związków...
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Influence of the Extraction Conditions on the Antifungal Properties of Walnut Green Husk Isolates
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Transport deficiency is the molecular basis of Candida albicans resistance to antifungal oligopeptides
Publication(FMDP), an inhibitor of glucosamine-6-phosphate synthase, exhibited growth inhibitory activity against Candida albicans, with minimal inhibitory concentration values in the 0.05–50 mg/L range. Uptake by the peptide permeases was found to be the main factor limiting an anticandidal activity of these compounds. Di- and tripeptide containing FMDP (F2 and F3) were transported by Ptr2p/Ptr22p peptide transporters (PTR) and FMDP-containing...
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Efficient synthesis and antifungal investigation of nucleosides’ quaternary ammonium salt derivatives
PublicationQuaternary ammonium salts are a group of compounds with diverse biological properties, the most important of which are their antiviral, antibacterial, and antifungal activities. The quaternization reactions of 5'-O-tosyl derivatives of uridine and thymidine with triethylamine, trimethylamine, 4-(N ,N -dimethylamino)pyridine, 2-methylpyridine, and pyridine are described in this article. Two of the synthesized compounds are exceptional...
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Studies of the effects of antifungal cationic derivatives of amphotericin B on human erythrocytes.
PublicationBadano nową grupę kationowych pochodnych amfoterycyny B pod kątem zależności pomiędzy ich zdolnością do asocjacji i selektywną toksycznością. We wszystkich przypadkach stosowano amfoterycynę B jako związek odniesienia. Jako miarę efektu toksycznego in vitro badanych związków stosowano wypływ wewnątrzkomórkowego potasu oraz hemolizę. Miarą aktywności przeciwgrzybowej był MIC i utrata potasu wewnatrzkomórkowego. Do oceny stopnia...
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Sensing of anesthetic drugs in blood with Raman spectroscopy
PublicationA proof-of-concept study of a Raman spectroscopy-based approach for measuring the content of anesthesia drugs in blood is presented. Spectra of spiked blood from several patients exhibit prominent changes in regions associated with the drug.
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A preliminary study on antifungal effect of TiO2-based paints in natural indoor light
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Cinnamon powder: an in vitro and in vivo evaluation of antifungal and plant growth promoting activity
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Comparison of antifungal activity of extracts from different Juglans regia cultivars and juglone
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Antifungal Effect of Penicillamine Due to the Selective Targeting of L-Homoserine O-Acetyltransferase
PublicationDue to the apparent similarity of fungal and mammalian metabolic pathways, the number of established antifungal targets is low, and the identification of novel ones is highly desirable. The results of our studies, presented in this work, indicate that the fungal biosynthetic pathway of L-methionine, an amino acid essential for humans, seems to be an attractive perspective. The MET2 gene from Candida albicans encoding L-homoserine...
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The Effect of Conjugation with Octaarginine, a Cell-Penetrating Peptide on Antifungal Activity of Imidazoacridinone Derivative
PublicationAcridine cell-penetrating peptide conjugates are an extremely important family of compounds in antitumor chemotherapy. These conjugates are not so widely analysed in antimicrobial therapy, although bioactive peptides could be used as nanocarriers to smuggle antimicrobial compounds. An octaarginine conjugate of an imidazoacridinone derivative (Compound 1-R8) synthetized by us exhibited high antifungal activity against reference...
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Characterization of PVDF/Graphene Nanocomposite Membranes for Water Desalination with Enhanced Antifungal Activity
PublicationSeawater desalination is a worldwide concern for the sustainable production of drinking water. In this regard, membrane distillation (MD) has shown the potential for effective brine treatment. However, the lack of appropriate MD membranes limits its industrial expansion since they experience fouling and wetting issues. Therefore, hydrophobic membranes are promising candidates to successfully deal with such phenomena that are typical...
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Targeting yeast topoisomerase II by imidazo and triazoloacridinone derivatives resulting in their antifungal activity
PublicationFungal pathogens are considered as serious factors for deadly diseases and are a case of medical concern. Invasive fungal infections also complicate the clinical course of COVID-19, leading to a significant increase in mortality. Furthermore, fungal strains' multidrug resistance has increased the demand for antifungals with a different mechanism of action. The present study aimed to identify antifungal compounds targeting yeast...
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N-acylpeptides with glucosamine-6-phosphate synthase inhibitors - synthesisand antifungal activity
PublicationOpracowano syntezę kilku peptydów (di i tripeptydów) zawierających inhibitory syntazy glukozamino-6-fosforanu oraz przeprowadzono je w N-acylopochodne (acetylowe, heksanoilowe, dekanoilowe) oraz zbadano ich aktywność przeciwgrzybową w stosunku do szczepów Candida albicans z opornością wielolekową. Stwierdzono, że N-acylopeptydy wykazują aktywność przeciwgrzybową oraz określono wartości MIC.
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Facilitated diffusion of glucosamine-6-phosphate synthase inhibitors enhances their antifungal activity
PublicationKwas N-3(4-metoksyfumaroilo)-L-2,3-diaminopropanowy (FMDP) i 2-amino-2-deo-ksy-D-glucitolo-6-fosforan (ADGP) są silnymi inhibitorami syntazy glukoza-mino-6-fosforanu, istotnego enzymu grzybowego, jednak ich aktywność przeciwgrzybowa jest słaba, ze względu na powolną penetrację tych związków przez błonę cytoplazmatyczną. W tej pracy badaliśmy możliwość poprawy działania przeciwgrzybowego ADGP i FMDP poprzez zwiększenie ich własności...
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Molecular modelling of membrane activity of amphotericin B, a polyene macrolide antifungal antibiotic
PublicationPraca dotyczy różnego typu modelowań molekularnych cząsteczki przeciwgrzybowego antybiotyku (amfoterycyny B). Praca przeglądowa obejmuje opis badań nad właściwościami molekularnymi samej cząsteczki antybiotyku, jej oddziaływań z powierzchnią błony oraz struktur kanałowych jakie tworzą cząsteczki amfoterycyny wewnątrz błony lipidowej.
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The impact of various azole antifungals on the liquid crystalline ordering in itraconazole
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Oligopeptide antifungals are exceptionally active against multidrug-resistant yeast
PublicationPermeazy peptydowe w komórkach drożdżowych są zdolne do transportu do wnętrza komórek oligopeptydów, zawierających w swojej strukturze niebiałkowe aminokwasy o właściwościach przeciwgrzybowych. Wśród szerokiego wachlarza tego rodzaju związków przebadanych pod względem aktywności biologicznej na wielolekoopornych komórkach drożdżowych, zaobserwowano liczna grupę, wykazującą zwiększoną aktywność względem komórek eksprymujących transportery...
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Molecular Umbrellas Modulate the Selective Toxicity of Polyene Macrolide Antifungals
PublicationAntifungal polyene macrolide antibiotics Amphotericin B (AmB) and Nystatin (NYS) were conjugated through the ω-amino acid linkers with diwalled “molecular umbrellas” composed of spermidine-linked deoxycholic or cholic acids. The presence of “umbrella” substituents modulated biological properties of the antibiotics, especially their selective toxicity. Some of the AmB-umbrella conjugates demonstrated antifungal in vitro activity...
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Molecular targets for antifungals in amino acid and protein biosynthetic pathways
PublicationFungi cause death of over 1.5 million people every year, while cutaneous mycoses are among the most common infections in the world. Mycoses vary greatly in severity, there are long-term skin (ringworm), nail or hair infections (tinea capitis), recurrent like vaginal candidiasis or severe, life-threatening systemic, multiorgan infections. In the last few years, increasing importance is attached to the health and economic problems...
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Machine learning applied to bi-heterocyclic drugs recognition
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Ultimate biodegradability and ecotoxicity of orally administered antidiabetic drugs
PublicationHypoglycaemic pharmaceuticals are recently more and more frequently detected in the environment. In our previous study, we have shown that even though many of them undergo significant primary degradation some are transformed to stable products or undergo such transformation that a large part of the structure is still preserved. One of the main routes of elimination from wastewaters or surface waters is biodegradation and a lack...
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Glucosinolates from lepidium peruvianum as potential antiamnestic drugs
PublicationLepidium peruvianum (maca) (Brassicaceae) is a naturally occurring plant mainly in the high Andes of Peru. In recent years, it has been intensively researched in terms of its influence on various diseases and towards health improvement. Alzheimer’s disease is an incurable disease that most often affects adults over the age of 60. As since 2003 the US Food and Drug Administration (FDA) did not approve any new drug for Alzheimer’s...