Molecules, Vol. 27, Pages 8104: Synthesis and Biological Evaluation of Novel Pyrimidine Amine Derivatives Bearing Bicyclic Monoterpene Moieties
gyan Wu A series of novel pinanyl pyrimidine amine derivatives (1e~1n) and camphoryl pyrimidine amine derivatives (2b~2f) bearing bicyclic monoterpene moieties were designed and synthesized from natural and renewable nopinone and camphor. All chemical structures of target compounds were characterized by 1H NMR, 13C NMR and HRMS spectra analyses, and the antimicrobial activities were evaluated. The results indicated that most compounds showed considerable antibacterial and antifungal activities against Klebsiella pneumoniae, Streptococcus pneumoniae, Pseudomonas aeruginosa, Staphylococcus aureus, Escherichia coli, Methi...
Source: Molecules - November 21, 2022 Category: Chemistry Authors: Mingguang Zhang Yunyun Wang Shifa Wang Hongyan Wu Tags: Article Source Type: research

CYP51-mediated cholesterol biosynthesis is required for the proliferation of CD4+ T cells in Sjogren ’s syndrome
AbstractCYtochrome P450, family 51 (CYP51) is an important enzyme for de novo cholesterol synthesis in mammalian cells. In the present study, we found that the expression of CYP51 positively correlated with CD4+ T cell activation both in vivo and in vitro. The addition of ketoconazole, a pharmacological inhibitor of CYP51, prevented the proliferation and activation of anti-CD3/CD28-expanded mouse CD4+ T cells in a dose-dependent fashion. Liquid chromatography-tandem mass spectrometry indicated an increase in levels of lanosterol in T cells treated with ketoconazole during activation. Ketoconazole-induced blockade of the ch...
Source: Clinical and Experimental Medicine - November 21, 2022 Category: Research Source Type: research

Human leukocyte antigen system associations in Malassezia-related skin diseases
ConclusionFive novel associations between HLA alleles and MRSD were identified in our cohort, and one previous association was confirmed. Future studies should assess the correlation betweenMalassezia antigens and antigen-binding properties of the associated HLA alleles. (Source: Archives of Dermatological Research)
Source: Archives of Dermatological Research - November 17, 2022 Category: Dermatology Source Type: research

Chemicals of environmental concern as inhibitors of human placental 3 β-hydroxysteroid dehydrogenase 1 and aromatase: Screening and docking analysis
In conclusion, 17β-estradiol, diethylstilbestrol, bisphenol A, and bisphenol AF are human HSD3B1 inhibitors, and ketoconazole, zearalenone, diethylstilbestrol, bisphenol A, and bisphenol AF are human CYP19A1 inhibitors.PMID:36374910 | DOI:10.1016/j.cbi.2022.110243 (Source: Chemico-Biological Interactions)
Source: Chemico-Biological Interactions - November 14, 2022 Category: Molecular Biology Authors: Luming Tang Lei Shi Yunbing Tang Yingfen Ying Yaoyao Dong Huitao Li Ren-Shan Ge Source Type: research

Chemicals of environmental concern as inhibitors of human placental 3 β-hydroxysteroid dehydrogenase 1 and aromatase: Screening and docking analysis
In conclusion, 17β-estradiol, diethylstilbestrol, bisphenol A, and bisphenol AF are human HSD3B1 inhibitors, and ketoconazole, zearalenone, diethylstilbestrol, bisphenol A, and bisphenol AF are human CYP19A1 inhibitors.PMID:36374910 | DOI:10.1016/j.cbi.2022.110243 (Source: Chemico-Biological Interactions)
Source: Chemico-Biological Interactions - November 14, 2022 Category: Molecular Biology Authors: Luming Tang Lei Shi Yunbing Tang Yingfen Ying Yaoyao Dong Huitao Li Ren-Shan Ge Source Type: research

Chemicals of environmental concern as inhibitors of human placental 3 β-hydroxysteroid dehydrogenase 1 and aromatase: Screening and docking analysis
In conclusion, 17β-estradiol, diethylstilbestrol, bisphenol A, and bisphenol AF are human HSD3B1 inhibitors, and ketoconazole, zearalenone, diethylstilbestrol, bisphenol A, and bisphenol AF are human CYP19A1 inhibitors.PMID:36374910 | DOI:10.1016/j.cbi.2022.110243 (Source: Chemico-Biological Interactions)
Source: Chemico-Biological Interactions - November 14, 2022 Category: Molecular Biology Authors: Luming Tang Lei Shi Yunbing Tang Yingfen Ying Yaoyao Dong Huitao Li Ren-Shan Ge Source Type: research

GSE217187 Interplay between acetylation and ubiquitination of Isw1 confers multidrug resistance in Cryptococcus neoformans
Contributor : Chen DingSeries Type : Expression profiling by high throughput sequencingOrganism : Cryptococcus neoformans var. grubii H99Cryptococcus neoformans poses a great threat to human communities, given that it quickly becomes resistant to available antifungal drugs. Herein, a conserved chromatin remodeler, Isw1, is shown to function as a master transcriptional modulator of genes responsible for multidrug resistance. It reciprocally controls drug resistance, and cells with disrupted ISW1 demonstrate profound resistance to fluconazole, ketoconazole, 5-fluorocytosine and 5-fluorouracil. Mass spectrometry reveals that...
Source: GEO: Gene Expression Omnibus - November 10, 2022 Category: Genetics & Stem Cells Tags: Expression profiling by high throughput sequencing Cryptococcus neoformans var. grubii H99 Source Type: research

Treatment of Primary Pigmented Nodular Adrenocortical Disease
Horm Metab Res 2022; 54: 721-730 DOI: 10.1055/a-1948-6990Primary pigmented nodular adrenocortical disease (PPNAD) is a rare cause of adrenocorticotropin hormone (ACTH)-independent Cushing’s syndrome (CS), which mainly occurs in children and young adults. Treatment options with proven clinical efficacy for PPNAD include adrenalectomy (bilateral or unilateral adrenalectomy) and drug treatment to control hypercortisolemia. Previously, the main treatment of PPNAD is bilateral adrenal resection and long-term hormone replacement after surgery. In recent years, cases r...
Source: Hormone and Metabolic Research - November 10, 2022 Category: Endocrinology Authors: Liu, Xinming Zhang, Siwen Guo, Yunran Gang, Xiaokun Wang, Guixia Tags: Review Source Type: research

Genotoxicity of pyrrolizidine alkaloids in metabolically inactive human cervical cancer HeLa cells co-cultured with human hepatoma HepG2 cells
Arch Toxicol. 2022 Oct 23. doi: 10.1007/s00204-022-03394-z. Online ahead of print.ABSTRACTPyrrolizidine alkaloids (PAs) are secondary plant metabolites, which can be found as contaminant in various foods and herbal products. Several PAs can cause hepatotoxicity and liver cancer via damaging hepatic sinusoidal endothelial cells (HSECs) after hepatic metabolization. HSECs themselves do not express the required metabolic enzymes for activation of PAs. Here we applied a co-culture model to mimic the in vivo hepatic environment and to study PA-induced effects on not metabolically active neighbour cells. In this co-culture model...
Source: Archives of Toxicology - October 23, 2022 Category: Toxicology Authors: Naji Said Aboud Hadi Ezgi Eyluel Bankoglu Helga Stopper Source Type: research

Genotoxicity of pyrrolizidine alkaloids in metabolically inactive human cervical cancer HeLa cells co-cultured with human hepatoma HepG2 cells
Arch Toxicol. 2022 Oct 23. doi: 10.1007/s00204-022-03394-z. Online ahead of print.ABSTRACTPyrrolizidine alkaloids (PAs) are secondary plant metabolites, which can be found as contaminant in various foods and herbal products. Several PAs can cause hepatotoxicity and liver cancer via damaging hepatic sinusoidal endothelial cells (HSECs) after hepatic metabolization. HSECs themselves do not express the required metabolic enzymes for activation of PAs. Here we applied a co-culture model to mimic the in vivo hepatic environment and to study PA-induced effects on not metabolically active neighbour cells. In this co-culture model...
Source: Archives of Toxicology - October 23, 2022 Category: Toxicology Authors: Naji Said Aboud Hadi Ezgi Eyluel Bankoglu Helga Stopper Source Type: research

Genotoxicity of pyrrolizidine alkaloids in metabolically inactive human cervical cancer HeLa cells co-cultured with human hepatoma HepG2 cells
Arch Toxicol. 2022 Oct 23. doi: 10.1007/s00204-022-03394-z. Online ahead of print.ABSTRACTPyrrolizidine alkaloids (PAs) are secondary plant metabolites, which can be found as contaminant in various foods and herbal products. Several PAs can cause hepatotoxicity and liver cancer via damaging hepatic sinusoidal endothelial cells (HSECs) after hepatic metabolization. HSECs themselves do not express the required metabolic enzymes for activation of PAs. Here we applied a co-culture model to mimic the in vivo hepatic environment and to study PA-induced effects on not metabolically active neighbour cells. In this co-culture model...
Source: Archives of Toxicology - October 23, 2022 Category: Toxicology Authors: Naji Said Aboud Hadi Ezgi Eyluel Bankoglu Helga Stopper Source Type: research

Genotoxicity of pyrrolizidine alkaloids in metabolically inactive human cervical cancer HeLa cells co-cultured with human hepatoma HepG2 cells
Arch Toxicol. 2022 Oct 23. doi: 10.1007/s00204-022-03394-z. Online ahead of print.ABSTRACTPyrrolizidine alkaloids (PAs) are secondary plant metabolites, which can be found as contaminant in various foods and herbal products. Several PAs can cause hepatotoxicity and liver cancer via damaging hepatic sinusoidal endothelial cells (HSECs) after hepatic metabolization. HSECs themselves do not express the required metabolic enzymes for activation of PAs. Here we applied a co-culture model to mimic the in vivo hepatic environment and to study PA-induced effects on not metabolically active neighbour cells. In this co-culture model...
Source: Archives of Toxicology - October 23, 2022 Category: Toxicology Authors: Naji Said Aboud Hadi Ezgi Eyluel Bankoglu Helga Stopper Source Type: research

Genotoxicity of pyrrolizidine alkaloids in metabolically inactive human cervical cancer HeLa cells co-cultured with human hepatoma HepG2 cells
Arch Toxicol. 2022 Oct 23. doi: 10.1007/s00204-022-03394-z. Online ahead of print.ABSTRACTPyrrolizidine alkaloids (PAs) are secondary plant metabolites, which can be found as contaminant in various foods and herbal products. Several PAs can cause hepatotoxicity and liver cancer via damaging hepatic sinusoidal endothelial cells (HSECs) after hepatic metabolization. HSECs themselves do not express the required metabolic enzymes for activation of PAs. Here we applied a co-culture model to mimic the in vivo hepatic environment and to study PA-induced effects on not metabolically active neighbour cells. In this co-culture model...
Source: Archives of Toxicology - October 23, 2022 Category: Toxicology Authors: Naji Said Aboud Hadi Ezgi Eyluel Bankoglu Helga Stopper Source Type: research