scholarly journals Evaluation of antimicrobial activity of synthesized 9H-alkylcarbazole and 10H-alkylphenothiazine derivatives on the cells of Salmonella enterica ser. Typhimurium, Saccharomyces cerevisiae, and Candida albicans

Biologija ◽  
2020 ◽  
Vol 66 (2) ◽  
Author(s):  
Simona Sutkuvienė ◽  
Sandra Sakalauskaitė ◽  
Neringa Kuliešienė ◽  
Lina Ragelienė ◽  
Rimantas Daugelavičius
Keyword(s):  
Saccharomyces Cerevisiae ◽  
Candida Albicans ◽  
Salmonella Enterica ◽  
Alkyl Chain ◽  
Efflux Pump ◽  
Inhibitory Effect ◽  
Phenothiazine Derivatives ◽  
Pharmacological Activities ◽  
Alkyl Chains ◽  
Wide Range

10H-substituted phenothiazine and 9H-substituted carbazole derivatives are important because of a very wide range of applications and especially in medical chemistry due to their pharmacological activities. In this study, we synthesized 9H-alkylcarbazole and 10H-alkylphenothiazine derivatives with various lengths of alkyl chains and evaluated their antimicrobial and efflux inhibiting activities on the cells of Salmonella enterica ser. Typhimurium, Saccharomyces cerevisiae, and Candida albicans. Results of our study revealed that an increased length of alkyl chains of the carbazoles increased the accumulation of efflux indicator tetraphenylphosphonium (TPP+) ions. Cells of S. enterica efflux mutant ΔTolC had a considerable susceptibility to the synthesized compounds. The compounds exerted synergy with fluconazole against S. cerevisiae yeast. Efflux pump mutant ΔPdr5 was hypersensitive to the investigated carbazole and phenothiazine derivatives. The inhibitory effect of the compounds with a shorter alkyl chain (10-methyl-10H-phenothiazine and 9-methyl-9H-carbazole) was the highest for Candida albicans cells.

scholarly journals CaNdt80 Is Involved in Drug Resistance in Candida albicans by Regulating CDR1

2004 ◽  
Vol 48 (12) ◽  
pp. 4505-4512 ◽  
Author(s):  
Chia-Geun Chen ◽  
Yun-Liang Yang ◽  
Hsin-I Shih ◽  
Chia-Li Su ◽  
Hsiu-Jung Lo
Keyword(s):  
Saccharomyces Cerevisiae ◽  
Drug Resistance ◽  
Candida Albicans ◽  
Type Strain ◽  
Antifungal Agents ◽  
Wild Type Strain ◽  
Efflux Pump ◽  
Antifungal Drugs ◽  
Galactosidase Activity ◽  
Wild Type

ABSTRACT Overexpression of CDR1, an efflux pump, is one of the major mechanisms contributing to drug resistance in Candida albicans. CDR1 p-lacZ was constructed and transformed into a Saccharomyces cerevisiae strain so that the lacZ gene could be used as the reporter to monitor the activity of the CDR1 promoter. Overexpression of CaNDT80, the C. albicans homolog of S. cerevisiae NDT80, increases the β-galactosidase activity of the CDR1 p-lacZ construct in S. cerevisiae. Furthermore, mutations in CaNDT80 abolish the induction of CDR1 expression by antifungal agents in C. albicans. Consistently, the Candt80/Candt80 mutant is also more susceptible to antifungal drugs than the wild-type strain. Thus, the gene for CaNdt80 may be the first gene among the regulatory factors involved in drug resistance in C. albicans whose function has been identified.

scholarly journals Effects of Hsp90 Inhibitor Ganetespib on Inhibition of Azole-Resistant Candida albicans

2021 ◽  
Vol 12 ◽  
Author(s):  
Rui Yuan ◽  
Jie Tu ◽  
Chunquan Sheng ◽  
Xi Chen ◽  
Na Liu
Keyword(s):  
Drug Resistance ◽  
Candida Albicans ◽  
Biofilm Formation ◽  
Efflux Pump ◽  
Inhibitory Effect ◽  
Hsp90 Inhibitor ◽  
Pcr Analysis ◽  
Fungal Hypha

Candida albicans is the most common fungal pathogen. Recently, drug resistance of C. albicans is increasingly severe. Hsp90 is a promising antifungal target to overcome this problem. To evaluate the effects of Hsp90 inhibitor ganetespib on the inhibition of azole-resistant C. albicans, the microdilution checkerboard method was used to measure the in vitro synergistic efficacy of ganetespib. The XTT/menadione reduction assay, microscopic observation, and Rh6G efflux assay were established to investigate the effects of ganetespib on azole-resistant C. albicans biofilm formation, filamentation, and efflux pump. Real-time RT-PCR analysis was employed to clarify the mechanism of antagonizing drug resistance. The in vivo antifungal efficacy of ganetespib was determined by the infectious model of azole-resistant C. albicans. Ganetespib showed an excellent synergistic antifungal activity in vitro and significantly inhibited the fungal biofilm formation, whereas it had no inhibitory effect on fungal hypha formation. Expression of azole-targeting enzyme gene ERG11 and efflux pump genes CDR1, CDR2, and MDR1 was significantly down-regulated when ganetespib was used in combination with FLC. In a mouse model infected with FLC-resistant C. albicans, the combination of ganetespib and FLC effectively reversed the FLC resistance and significantly decreased the kidney fungal load of mouse.

scholarly journals Study the Inhibitory effect of Rose and blossom bitter orange flowers extracts against different types of bacteria isolated from the oral cavity

2014 ◽  
Vol 11 (2) ◽  
pp. 795-802
Author(s):  
Baghdad Science Journal
Keyword(s):  
Candida Albicans ◽  
Oral Cavity ◽  
Cold Water ◽  
Inhibitory Effect ◽  
Isolation And Identification ◽  
Active Compounds ◽  
Bitter Orange ◽  
Wide Range ◽  
Different Types ◽  
Amoxicillin Clavulanic Acid

The study in duded isolation and identification of microbial isolates from oral cavity to 10 volunteers, diagnosed within the three groups: Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus spp. and Candida albicans . The sensitivity test of all isolates bacteria Streptococcus spp. , S. aureus and S. epidermidis showed high resistance to Ampicillin(100)%,followed Methicillin (88.88)% and Amoxicillin / clavulanic acid(77.77)%, while the resistance for each of Vancomycin and Amoxicillin were (66.66)%, and the resistance to Erythromycin and Pencillin (55.55)% to each of them. The results showed less resistance to Trimethoprim (22.22)% and Cefalotine (11.11)% of all bacteria isolate. Investigation of the presence of active compounds in each of the hot and cold (water and alcoholic) extracts flowers Rose and flowers blossom bitter orange ( new preparatory 2012) (Alkaloids, Quartet alkaloids, sugars, Saponine, Flavones and comarins ) was carried out includes. While it was all kinds of extracts does not contain resins. The results showed the presence of active compounds (Sugars, Flavones and comarins) in old extracts that preparation after a year (2011). PH values of the plant extracts hot and cold (water and alcoholic) for each of orange flowers blossom and Rose flowers (Old and new preparatory) with a wide range ranging between (3.6 -6.4). All extracts hot and cold (alcoholic) (new preparatory 2012) showed most effective towards Streptococcus spp., S. epidermidis and Candida albicans, while the extracts show weak effective against S. aureus. Hot alcohol extracts of Rose (old preparatory 2011) showed most effective towards S. aureus and S. epidermidis only, while the other extracts of old perpetration show weak effective against Streptococcus spp. and C. albicans.

scholarly journals The DNA-binding domain of CaNdt80p is required to activate CDR1 involved in drug resistance in Candida albicans

2006 ◽  
Vol 55 (10) ◽  
pp. 1403-1411 ◽  
Author(s):  
Jang-Shiun Wang ◽  
Yun-Liang Yang ◽  
Chin-Jung Wu ◽  
Karen J. Ouyang ◽  
Kuo-Yun Tseng ◽  
...  
Keyword(s):  
Saccharomyces Cerevisiae ◽  
Drug Resistance ◽  
Transcription Factor ◽  
Candida Albicans ◽  
Dna Binding ◽  
Efflux Pump ◽  
Binding Domain ◽  
Null Mutation ◽  
Dna Binding Domain ◽  
Positive Regulator

CaNdt80p, the Candida albicans homologue of the Saccharomyces cerevisiae transcription factor ScNdt80p, has been identified as a positive regulator of CDR1, which encodes an efflux pump involved in drug resistance in C. albicans. To investigate the involvement of the putative DNA-binding domain of CaNdt80p in drug resistance, chimeras of CaNdt80p and ScNdt80p were constructed. Interestingly, the DNA-binding domain of ScNdt80p could functionally complement that of CaNdt80p to activate CDR1p–lacZ in S. cerevisiae. Consistently, CaNdt80p containing a mutation in the DNA-binding domain failed to activate CDR1p–lacZ in S. cerevisiae. Furthermore, a copy of CaNDT80 with the same mutation also failed to complement the drug-sensitive phenotype caused by a null mutation in C. albicans. Thus, the DNA-binding domain of CaNdt80p is critical for its function in drug resistance in C. albicans.

scholarly journals Assessment of antimicrobial activity in Diplostephium phylicoides and Diplostephium revolutum extracts by plates and wells method

2019 ◽  
pp. 219-223
Author(s):  
Janeth Arias Palacios
Keyword(s):  
Saccharomyces Cerevisiae ◽  
Staphylococcus Aureus ◽  
Antimicrobial Activity ◽  
Candida Albicans ◽  
Ethyl Acetate ◽  
Penicillium Chrysogenum ◽  
Ethyl Acetate Extract ◽  
Salmonella Typhi ◽  
Inhibitory Effect ◽  
The One

Abstract. In the present work, the evaluation of the antimicrobial activity of Diplostephium phylicoides and Diplostephium revolutum on different microorganisms was carried out on using bacteria such as Escherichia coli (CMPUJ:034), Staphylococcus aureus (CMPUJ:370), Salmonella typhi (CMPUJ:045) and Pseudomonas aeruginosa (CMPUJ:065), yeasts such as Saccharomyces cerevisiae (CMPUJ:H042) and Candida albicans (CMPUJ:H022), and filamentous fungi such as Penicillium chrysogenum (CMPUJ:H061) and Aspergillus niger (CMPUJ:H002). This assessment was made by the method of plates and wells using extracts from the leaves of the previously mentioned plants. The extracts were made with different solvents, ethanol, ethyl acetate, dichloromethane and petroleum ether. The results showed that the ethyl acetate extract of Diplostephium phylicoides has antimicrobial activity against Staphylococcus aureus and Candida albicans; furthermore, the dichloromethane extract showed an inhibitory effect against Saccharomyces cerevisiae. When comparing the extracts of the two plants, under the evaluated conditions, the extracts presented antimicrobial activity, and the ethyl acetate extract of Diplostephium revolutum the one that showed better activity against all the microorganisms.

scholarly journals Functional Expression of Candida albicans Drug Efflux Pump Cdr1p in a Saccharomyces cerevisiae Strain Deficient in Membrane Transporters

2001 ◽  
Vol 45 (12) ◽  
pp. 3366-3374 ◽  
Author(s):  
Kenjirou Nakamura ◽  
Masakazu Niimi ◽  
Kyoko Niimi ◽  
Ann R. Holmes ◽  
Jenine E. Yates ◽  
...  
Keyword(s):  
Saccharomyces Cerevisiae ◽  
Drug Resistance ◽  
Candida Albicans ◽  
Plasma Membrane ◽  
Efflux Pump ◽  
Multiple Drug Resistance ◽  
Functional Expression ◽  
Multiple Drug ◽  
Drug Efflux ◽  
High Level

ABSTRACT Analysis of the transport functions of individualCandida albicans plasma membrane drug efflux pumps is hampered by the multitude of endogenous transporters. We have stably expressed C. albicans Cdr1p, the major pump implicated in multiple-drug-resistance phenotypes, from the genomicPDR5 locus in a Saccharomyces cerevisiae mutant (AD1-8u−) from which seven major transporters of the ATP-binding cassette (ABC) family have been deleted. High-level expression of Cdr1p, under the control of the S. cerevisiae PDR5 promoter and driven by S. cerevisiae Pdr1p transcriptional regulator mutation pdr1-3, was demonstrated by increased levels of mRNA transcription, increased levels of nucleoside triphosphatase activity, and immunodetection in plasma membrane fractions. S. cerevisiae AD1-8u− was hypersensitive to azole antifungals (the MICs at which 80% of cells were inhibited [MIC80s] were 0.625 μg/ml for fluconazole, <0.016 μg/ml for ketoconazole, and <0.016 μg/ml for itraconazole), whereas the strain (AD1002) that overexpressed C. albicans Cdr1p was resistant to azoles (MIC80s of fluconazole, ketoconazole, and itraconazole, 30, 0.5, and 4 μg/ml, respectively). Drug resistance correlated with energy-dependent drug efflux. AD1002 demonstrated resistance to a variety of structurally unrelated chemicals which are potential drug pump substrates. The controlled overexpression of C. albicansCdr1p in an S. cerevisiae background deficient in other pumps allows the functional analysis of pumping specificity and mechanisms of a major ABC transporter involved in drug efflux from an important human pathogen.

Ethnomedicinal uses, Phytochemistry and Pharmacological Aspects of the Genus Berberis Linn: A Comprehensive Review

2020 ◽  
Vol 23 ◽  
Author(s):  
Roohi Mohi-ud-din ◽  
Reyaz Hassan Mir ◽  
Prince Ahad Mir ◽  
Saeema Farooq ◽  
Syed Naiem Raza ◽  
...  
Keyword(s):  
Chemical Constituents ◽  
Pharmacological Activities ◽  
Traditional Use ◽  
Comprehensive Review ◽  
Wide Range ◽  
Anti Cancer ◽  
Comprehensive Survey ◽  
Ethnomedicinal Uses

Background: Genus Berberis (family Berberidaceae), which contains about 650 species and 17 genera worldwide, has been used in folklore and various traditional medicine systems. Berberis Linn. is the most established group among genera with around 450-500 species across the world. This comprehensive review will not only help researchers for further evaluation but also provide substantial information for future exploitation of species to develop novel herbal formulations. Objective: The present review is focussed to summarize and collect the updated review of information of Genus Berberis species reported to date regarding their ethnomedicinal information, chemical constituents, traditional/folklore use, and reported pharmacological activities on more than 40 species of Berberis. Conclusion: A comprehensive survey of the literature reveals that various species of the genus possess various phytoconstituents mainly alkaloids, flavonoid based compounds isolated from different parts of a plant with a wide range of pharmacological activities. So far, many pharmacological activities like anti-cancer, anti-hyperlipidemic, hepatoprotective, immunomodulatory, anti-inflammatory both in vitro & in vivo and clinical study of different extracts/isolated compounds of different species of Berberis have been reported, proving their importance as a medicinal plant and claiming their traditional use.

Nanoparticles Functionalized with Venom-Derived Peptides and Toxins for Pharmaceutical Applications

2020 ◽  
Vol 21 (2) ◽  
pp. 97-109 ◽  
Author(s):  
Ana P. dos Santos ◽  
Tamara G. de Araújo ◽  
Gandhi Rádis-Baptista
Keyword(s):  
Oral Absorption ◽  
Current Data ◽  
Pharmacological Activities ◽  
Venom Peptides ◽  
Essential Components ◽  
Wide Range ◽  
Different Types ◽  
Direct Use ◽  
Animal Venoms ◽  
Pharmaceutical Biotechnology

Venom-derived peptides display diverse biological and pharmacological activities, making them useful in drug discovery platforms and for a wide range of applications in medicine and pharmaceutical biotechnology. Due to their target specificities, venom peptides have the potential to be developed into biopharmaceuticals to treat various health conditions such as diabetes mellitus, hypertension, and chronic pain. Despite the high potential for drug development, several limitations preclude the direct use of peptides as therapeutics and hamper the process of converting venom peptides into pharmaceuticals. These limitations include, for instance, chemical instability, poor oral absorption, short halflife, and off-target cytotoxicity. One strategy to overcome these disadvantages relies on the formulation of bioactive peptides with nanocarriers. A range of biocompatible materials are now available that can serve as nanocarriers and can improve the bioavailability of therapeutic and venom-derived peptides for clinical and diagnostic application. Examples of isolated venom peptides and crude animal venoms that have been encapsulated and formulated with different types of nanomaterials with promising results are increasingly reported. Based on the current data, a wealth of information can be collected regarding the utilization of nanocarriers to encapsulate venom peptides and render them bioavailable for pharmaceutical use. Overall, nanomaterials arise as essential components in the preparation of biopharmaceuticals that are based on biological and pharmacological active venom-derived peptides.

Inhibition of Yeast Growth by Tryptamine and Recovery with Tryptophan

2020 ◽  
Vol 16 (1) ◽  
pp. 48-52 ◽  
Author(s):  
Chandrika Kadkol ◽  
Ian Macreadie
Keyword(s):  
Saccharomyces Cerevisiae ◽  
Carbon Source ◽  
Competitive Inhibition ◽  
Yeast Species ◽  
Inhibitory Effect ◽  
The Body ◽  
Inhibitory Effects ◽  
Trna Synthetases ◽  
Fermentative Growth ◽  
Biogenic Monoamine

Background: Tryptamine, a biogenic monoamine that is present in trace levels in the mammalian central nervous system, has probable roles as a neurotransmitter and/or a neuromodulator and may be associated with various neuropsychiatric disorders. One of the ways tryptamine may affect the body is by the competitive inhibition of the attachment of tryptophan to tryptophanyl tRNA synthetases. Methods: This study has explored the effects of tryptamine on growth of six yeast species (Saccharomyces cerevisiae, Candida glabrata, C. krusei, C. dubliniensis, C. tropicalis and C. lusitaniae) in media with glucose or ethanol as the carbon source, as well as recovery of growth inhibition by the addition of tryptophan. Results: Tryptamine was found to have an inhibitory effect on respiratory growth of all yeast species when grown with ethanol as the carbon source. Tryptamine also inhibited fermentative growth of Saccharomyces cerevisiae, C. krusei and C. tropicalis with glucose as the carbon source. In most cases the inhibitory effects were reduced by added tryptophan. Conclusion: The results obtained in this study are consistent with tryptamine competing with tryptophan to bind mitochondrial and cytoplasmic tryptophanyl tRNA synthetases in yeast: effects on mitochondrial and cytoplasmic protein synthesis can be studied as a function of growth with glucose or ethanol as a carbon source. Of the yeast species tested, there is variation in the sensitivity to tryptamine and the rescue by tryptophan. The current study suggests appropriate yeast strains and approaches for further studies.

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