Clotrimazole causes membrane depolarization and induces sub G < sub > 0 < /sub > cell cycle arrest in Leishmania donovani
In this study we have explored the possibility of repurposing clotrimazole as an antileishmanial drug. We have assessed its efficacy on the parasites and attempted to understand its mode of action. We found that it has a half-maximal inhibitory concentration (IC50) of 35.75 ± 1.06 μM, 12.75 ± 0.35 μM and 73 ± 1.41 μM in promastigotes, intracellular amastigotes and macrophages, respectively. Clotrimazole is 5.73 times more selective for the intracellular amastigotes as compared to the mammalian cell. Effect of clotrimazole was reduced by ergosterol supplementation. It leads to impaired parasite morphology. It alters p...
Source: Acta Tropica - February 2, 2024 Category: Infectious Diseases Authors: Anindita Paul Pradyot Kumar Roy Neerupudi Kishore Babu Sushma Singh Source Type: research

Clotrimazole reverses macrophage M2 polarization by disrupting the PI3K/AKT/mTOR pathway
In this study, we show that CTZ downregulated M2-activation markers in macrophages polarized to the M2 profile. This effect occurred without interfering with the expression of M1-polarized markers or pro-inflammatory cytokines and signaling. Moreover, CTZ suppressed NFkB pathway intermediates and disrupted PI3K/AKT/mTOR signaling. We concluded that CTZ reverses macrophage M2 polarization by disrupting the PI3K/AKT/mTOR pathway, which results in the suppression of NFkB induction of M2 polarization. In addition, we find that CTZ represents a promising therapeutic tool as an antitumor agent.PMID:38176247 | DOI:10.1016/j.bbrc....
Source: Biochemical and Biophysical Research communications - January 4, 2024 Category: Biochemistry Authors: Jos é Xavier do Nascimento Júnior Mauro Sola-Penna Patricia Zancan Source Type: research

Clotrimazole reverses macrophage M2 polarization by disrupting the PI3K/AKT/mTOR pathway
In this study, we show that CTZ downregulated M2-activation markers in macrophages polarized to the M2 profile. This effect occurred without interfering with the expression of M1-polarized markers or pro-inflammatory cytokines and signaling. Moreover, CTZ suppressed NFkB pathway intermediates and disrupted PI3K/AKT/mTOR signaling. We concluded that CTZ reverses macrophage M2 polarization by disrupting the PI3K/AKT/mTOR pathway, which results in the suppression of NFkB induction of M2 polarization. In addition, we find that CTZ represents a promising therapeutic tool as an antitumor agent.PMID:38176247 | DOI:10.1016/j.bbrc....
Source: Biochemical and Biophysical Research communications - January 4, 2024 Category: Biochemistry Authors: Jos é Xavier do Nascimento Júnior Mauro Sola-Penna Patricia Zancan Source Type: research

Species distribution and antifungal susceptibility profiles of yeasts isolated from onychomycosis: a cross-sectional study with insights into emerging species
Antonie Van Leeuwenhoek. 2023 Dec 28;117(1):6. doi: 10.1007/s10482-023-01914-0.ABSTRACTCandida onychomycosis is a common fungal infection affecting the nails, primarily caused by Candida (C.) species. Regarding the increasing trend of Candida onychomycosis and the antifungal resistant phenomenon in recent years, this study aims to evaluate the epidemiological characteristics of Candida onychomycosis, the distribution of emerging species, and the antifungal susceptibility profiles of isolates. Onychomycosis caused by yeast species was confirmed through direct examination and culture of nail scraping among all individuals su...
Source: Antonie van Leeuwenhoek - December 28, 2023 Category: Microbiology Authors: Somayeh Yazdanpanah Ahmad Jabrodini Marjan Motamedi Kamiar Zomorodian Mahboobeh Kharazi Shafigheh Shabanzadeh Farnia Ghasemi Sahar Shariat Maryam Rezaei Arab Source Type: research

Species distribution and antifungal susceptibility profiles of yeasts isolated from onychomycosis: a cross-sectional study with insights into emerging species
Antonie Van Leeuwenhoek. 2023 Dec 28;117(1):6. doi: 10.1007/s10482-023-01914-0.ABSTRACTCandida onychomycosis is a common fungal infection affecting the nails, primarily caused by Candida (C.) species. Regarding the increasing trend of Candida onychomycosis and the antifungal resistant phenomenon in recent years, this study aims to evaluate the epidemiological characteristics of Candida onychomycosis, the distribution of emerging species, and the antifungal susceptibility profiles of isolates. Onychomycosis caused by yeast species was confirmed through direct examination and culture of nail scraping among all individuals su...
Source: Antonie van Leeuwenhoek - December 28, 2023 Category: Microbiology Authors: Somayeh Yazdanpanah Ahmad Jabrodini Marjan Motamedi Kamiar Zomorodian Mahboobeh Kharazi Shafigheh Shabanzadeh Farnia Ghasemi Sahar Shariat Maryam Rezaei Arab Source Type: research

Species distribution and antifungal susceptibility profiles of yeasts isolated from onychomycosis: a cross-sectional study with insights into emerging species
Antonie Van Leeuwenhoek. 2023 Dec 28;117(1):6. doi: 10.1007/s10482-023-01914-0.ABSTRACTCandida onychomycosis is a common fungal infection affecting the nails, primarily caused by Candida (C.) species. Regarding the increasing trend of Candida onychomycosis and the antifungal resistant phenomenon in recent years, this study aims to evaluate the epidemiological characteristics of Candida onychomycosis, the distribution of emerging species, and the antifungal susceptibility profiles of isolates. Onychomycosis caused by yeast species was confirmed through direct examination and culture of nail scraping among all individuals su...
Source: Antonie van Leeuwenhoek - December 28, 2023 Category: Microbiology Authors: Somayeh Yazdanpanah Ahmad Jabrodini Marjan Motamedi Kamiar Zomorodian Mahboobeh Kharazi Shafigheh Shabanzadeh Farnia Ghasemi Sahar Shariat Maryam Rezaei Arab Source Type: research

Species distribution and antifungal susceptibility profiles of yeasts isolated from onychomycosis: a cross-sectional study with insights into emerging species
Antonie Van Leeuwenhoek. 2023 Dec 28;117(1):6. doi: 10.1007/s10482-023-01914-0.ABSTRACTCandida onychomycosis is a common fungal infection affecting the nails, primarily caused by Candida (C.) species. Regarding the increasing trend of Candida onychomycosis and the antifungal resistant phenomenon in recent years, this study aims to evaluate the epidemiological characteristics of Candida onychomycosis, the distribution of emerging species, and the antifungal susceptibility profiles of isolates. Onychomycosis caused by yeast species was confirmed through direct examination and culture of nail scraping among all individuals su...
Source: Antonie van Leeuwenhoek - December 28, 2023 Category: Microbiology Authors: Somayeh Yazdanpanah Ahmad Jabrodini Marjan Motamedi Kamiar Zomorodian Mahboobeh Kharazi Shafigheh Shabanzadeh Farnia Ghasemi Sahar Shariat Maryam Rezaei Arab Source Type: research

Species distribution and antifungal susceptibility profiles of yeasts isolated from onychomycosis: a cross-sectional study with insights into emerging species
Antonie Van Leeuwenhoek. 2023 Dec 28;117(1):6. doi: 10.1007/s10482-023-01914-0.ABSTRACTCandida onychomycosis is a common fungal infection affecting the nails, primarily caused by Candida (C.) species. Regarding the increasing trend of Candida onychomycosis and the antifungal resistant phenomenon in recent years, this study aims to evaluate the epidemiological characteristics of Candida onychomycosis, the distribution of emerging species, and the antifungal susceptibility profiles of isolates. Onychomycosis caused by yeast species was confirmed through direct examination and culture of nail scraping among all individuals su...
Source: Antonie van Leeuwenhoek - December 28, 2023 Category: Microbiology Authors: Somayeh Yazdanpanah Ahmad Jabrodini Marjan Motamedi Kamiar Zomorodian Mahboobeh Kharazi Shafigheh Shabanzadeh Farnia Ghasemi Sahar Shariat Maryam Rezaei Arab Source Type: research

Development and Validation of Reverse-Phase High-Performance Liquid Chromatography Method for Simultaneous Estimation of Doxorubicin and Clotrimazole
ASSAY and Drug Development Technologies, Ahead of Print. (Source: ASSAY and Drug Development Technologies)
Source: ASSAY and Drug Development Technologies - December 27, 2023 Category: Drugs & Pharmacology Authors: Priyanka Sharma Bhupinder Kapoor Md Sadique Hussain Gurvinder Singh Pooja Rani Balraj Saini Pankaj Wadhwa Rajesh Kumar Source Type: research

Delayed clearance of the pro-carcinogen benzo[a]pyrene in PLHC-1 cells when co-exposed to the antifungal drug clotrimazole and effects on the CYP1A biomarker
Toxicol In Vitro. 2023 Dec 18:105767. doi: 10.1016/j.tiv.2023.105767. Online ahead of print.ABSTRACTCytochrome P450 1 A (CYP1A) is a key enzyme in the metabolism of the polycyclic aromatic hydrocarbon (PAH) benzo[a]pyrene (BaP) in animals, and a biomarker for environmental PAH exposure. The common antimycotic imidazole drug clotrimazole (CLO) has been detected in the aquatic environment and likely co-exists with BaP. Like BaP, CLO can bind to CYP1A enzymes and can act as a CYP1A inhibitor. Co-exposure of BaP with CLO significantly delayed BaP elimination in a fish liver cell line (PLHC-1). Intracellular BaP concentration w...
Source: Toxicology in Vitro - December 20, 2023 Category: Toxicology Authors: Maja Edenius Anne Farbrot Anders Blom Malin C Celander Source Type: research

Delayed clearance of the pro-carcinogen benzo[a]pyrene in PLHC-1 cells when co-exposed to the antifungal drug clotrimazole and effects on the CYP1A biomarker
Toxicol In Vitro. 2023 Dec 18:105767. doi: 10.1016/j.tiv.2023.105767. Online ahead of print.ABSTRACTCytochrome P450 1 A (CYP1A) is a key enzyme in the metabolism of the polycyclic aromatic hydrocarbon (PAH) benzo[a]pyrene (BaP) in animals, and a biomarker for environmental PAH exposure. The common antimycotic imidazole drug clotrimazole (CLO) has been detected in the aquatic environment and likely co-exists with BaP. Like BaP, CLO can bind to CYP1A enzymes and can act as a CYP1A inhibitor. Co-exposure of BaP with CLO significantly delayed BaP elimination in a fish liver cell line (PLHC-1). Intracellular BaP concentration w...
Source: Toxicology in Vitro - December 20, 2023 Category: Toxicology Authors: Maja Edenius Anne Farbrot Anders Blom Malin C Celander Source Type: research

Delayed clearance of the pro-carcinogen benzo[a]pyrene in PLHC-1 cells when co-exposed to the antifungal drug clotrimazole and effects on the CYP1A biomarker
Toxicol In Vitro. 2023 Dec 18:105767. doi: 10.1016/j.tiv.2023.105767. Online ahead of print.ABSTRACTCytochrome P450 1 A (CYP1A) is a key enzyme in the metabolism of the polycyclic aromatic hydrocarbon (PAH) benzo[a]pyrene (BaP) in animals, and a biomarker for environmental PAH exposure. The common antimycotic imidazole drug clotrimazole (CLO) has been detected in the aquatic environment and likely co-exists with BaP. Like BaP, CLO can bind to CYP1A enzymes and can act as a CYP1A inhibitor. Co-exposure of BaP with CLO significantly delayed BaP elimination in a fish liver cell line (PLHC-1). Intracellular BaP concentration w...
Source: Toxicology in Vitro - December 20, 2023 Category: Toxicology Authors: Maja Edenius Anne Farbrot Anders Blom Malin C Celander Source Type: research

Ivermectin Toxicokinetics in Rainbow Trout (Oncorhynchus mykiss) following P-glycoprotein Induction
Arch Environ Contam Toxicol. 2023 Dec 16. doi: 10.1007/s00244-023-01045-7. Online ahead of print.ABSTRACTAlterations in ivermectin (IVM, 22,23-dihydro avermectin B1a+22,23-dihydro avermectin B1b) toxicokinetics following P-glycoprotein (P-gp) induction by clotrimazole (CTZ) were examined in rainbow trout (Oncorhynchus mykiss) to assess the potential importance of P-gp activity levels in xenobiotic distribution and kinetics in fish. Control and fish pretreated with CTZ (30 µmol/kg) were administered 175 µg/kg 3H-IVM into the caudal vasculature. At various time points (0.25, 0.5, 1, 3, 24, 48, 96, and 168 h) following inje...
Source: Archives of Environmental Contamination and Toxicology - December 16, 2023 Category: Environmental Health Authors: Vinicius Cavicchioli Azevedo Christina U Johnston Christopher J Kennedy Source Type: research

Clotrimazole ameliorates chronic mild stress-induced depressive-like behavior in rats; crosstalk between the HPA, NLRP3 inflammasome, and Wnt/ β-catenin pathways
Int Immunopharmacol. 2023 Dec 15;127:111354. doi: 10.1016/j.intimp.2023.111354. Online ahead of print.ABSTRACTDepression is a major emotional disorder that has a detrimental effect on quality of life. The chronic mild stress (CMS)-depression model was adopted in rats to evaluate the neurotherapeutic effect of Clotrimazole (CLO) and investigate the possible mechanisms of its antidepressant action via its impact on the hypothalamic pituitary adrenal (HPA) axis and the stress hormone, cortisol. It was found that azole antifungals affect steroidogenesis and the HPA axis. Behavioral, histopathological, inflammatory, and apoptot...
Source: International Immunopharmacology - December 16, 2023 Category: Allergy & Immunology Authors: Sylvia F Fawzi Haidy E Michel Esther T Menze Mariane G Tadros Mina Y George Source Type: research

Ivermectin Toxicokinetics in Rainbow Trout (Oncorhynchus mykiss) following P-glycoprotein Induction
Arch Environ Contam Toxicol. 2023 Dec 16. doi: 10.1007/s00244-023-01045-7. Online ahead of print.ABSTRACTAlterations in ivermectin (IVM, 22,23-dihydro avermectin B1a+22,23-dihydro avermectin B1b) toxicokinetics following P-glycoprotein (P-gp) induction by clotrimazole (CTZ) were examined in rainbow trout (Oncorhynchus mykiss) to assess the potential importance of P-gp activity levels in xenobiotic distribution and kinetics in fish. Control and fish pretreated with CTZ (30 µmol/kg) were administered 175 µg/kg 3H-IVM into the caudal vasculature. At various time points (0.25, 0.5, 1, 3, 24, 48, 96, and 168 h) following inje...
Source: Archives of Environmental Contamination and Toxicology - December 16, 2023 Category: Environmental Health Authors: Vinicius Cavicchioli Azevedo Christina U Johnston Christopher J Kennedy Source Type: research