Metabolic activation and cytotoxicity of 4-Methylquinoline mediated by CYP3A4 and sulfotransferases in rats
This study aimed to elucidate the metabolic activation of 4-MQ and to determine the possible role of reactive metabolites in 4-MQ-induced liver injury in rats. In the present study, a hydroxylation metabolite (M1), a GSH conjugate (M2) and an NAC conjugate (M3) derived from 4-MQ were detected in vitro and in vivo. The structures of the two conjugates were verified by chemical synthesis, mass spectrometry, and nuclear magnetic resonance. CYP3A4 was found to dominate the hydroxylation of 4-MQ. Sulfotransferases also participated in the metabolic activation of 4-MQ. Pretreatment of primary hepatocytes with ketoconazole (KTC) ...
Source: Food and Chemical Toxicology - June 2, 2023 Category: Food Science Authors: Kaixuan Li Guode Zhao Lan Yang Xingyu Gao Yudi Jia Yang Wang Xiaohong Zhang Weiwei Li Ying Peng Jiang Zheng Source Type: research
Functionally substituted 2-aminothiazoles as antimicrobial agents: in vitro and in silico evaluation
SAR QSAR Environ Res. 2023 May 30:1-20. doi: 10.1080/1062936X.2023.2214869. Online ahead of print.ABSTRACTNine new functionally substituted derivatives of 2-aminothiazole were evaluated for antimicrobial activity using microdilution method against the panel of eight bacterial and eight fungal strains. Evaluation of antibacterial activity revealed that compounds are potent antibacterial agents, more active than ampicillin and streptomycin except of some compounds against B. cereus and En. cloacae. The best compound appeared to be compound 8. The most sensitive bacteria appeared to be En. cloacae, while L. monocytogenes was ...
Source: SAR and QSAR in Environmental Research - May 30, 2023 Category: Environmental Health Authors: A Petrou V Kartsev A Geronikaki J Glamo člija A Ciric M Sokovic Source Type: research
Functionally substituted 2-aminothiazoles as antimicrobial agents: in vitro and in silico evaluation
SAR QSAR Environ Res. 2023 May;34(5):395-414. doi: 10.1080/1062936X.2023.2214869. Epub 2023 May 30.ABSTRACTNine new functionally substituted derivatives of 2-aminothiazole were evaluated for antimicrobial activity using microdilution method against the panel of eight bacterial and eight fungal strains. Evaluation of antibacterial activity revealed that compounds are potent antibacterial agents, more active than ampicillin and streptomycin except of some compounds against B. cereus and En. cloacae. The best compound appeared to be compound 8. The most sensitive bacteria appeared to be En. cloacae, while L. monocytogenes was...
Source: SAR and QSAR in Environmental Research - May 30, 2023 Category: Environmental Health Authors: A Petrou V Kartsev A Geronikaki J Glamo člija A Ciric M Sokovic Source Type: research
Tumour induction in BALB/c mice for imaging studies: An improved protocol
J Cell Mol Med. 2023 May 29. doi: 10.1111/jcmm.17792. Online ahead of print.ABSTRACTDealing with nude mice, which lack thymus and therefore are sensitive to unsterile conditions, needs special care and laboratory conditions. For preclinical studies, especially tumour imaging purposes, in which therapeutic properties of drugs or therapeutic compounds are not studied, mice with normal immune system can be a favourable alternative if they carry tumours of interest. In the current study, we introduce an optimized protocol for induction of human tumours in BALB/c mice for preclinical studies. Immune system of BALB/c mice was su...
Source: J Cell Mol Med - May 29, 2023 Category: Molecular Biology Authors: Abolfazl Amini Gholamreza Mesbah Fatemeh Tash Shamsabadi Mohammad Ali Zeyghami Yaghoub Safdari Source Type: research
Tumour induction in BALB/c mice for imaging studies: An improved protocol
J Cell Mol Med. 2023 May 29. doi: 10.1111/jcmm.17792. Online ahead of print.ABSTRACTDealing with nude mice, which lack thymus and therefore are sensitive to unsterile conditions, needs special care and laboratory conditions. For preclinical studies, especially tumour imaging purposes, in which therapeutic properties of drugs or therapeutic compounds are not studied, mice with normal immune system can be a favourable alternative if they carry tumours of interest. In the current study, we introduce an optimized protocol for induction of human tumours in BALB/c mice for preclinical studies. Immune system of BALB/c mice was su...
Source: Molecular Medicine - May 29, 2023 Category: Molecular Biology Authors: Abolfazl Amini Gholamreza Mesbah Fatemeh Tash Shamsabadi Mohammad Ali Zeyghami Yaghoub Safdari Source Type: research
Tumour induction in BALB/c mice for imaging studies: An improved protocol
J Cell Mol Med. 2023 May 29. doi: 10.1111/jcmm.17792. Online ahead of print.ABSTRACTDealing with nude mice, which lack thymus and therefore are sensitive to unsterile conditions, needs special care and laboratory conditions. For preclinical studies, especially tumour imaging purposes, in which therapeutic properties of drugs or therapeutic compounds are not studied, mice with normal immune system can be a favourable alternative if they carry tumours of interest. In the current study, we introduce an optimized protocol for induction of human tumours in BALB/c mice for preclinical studies. Immune system of BALB/c mice was su...
Source: J Cell Mol Med - May 29, 2023 Category: Molecular Biology Authors: Abolfazl Amini Gholamreza Mesbah Fatemeh Tash Shamsabadi Mohammad Ali Zeyghami Yaghoub Safdari Source Type: research
Tumour induction in BALB/c mice for imaging studies: An improved protocol
J Cell Mol Med. 2023 May 29. doi: 10.1111/jcmm.17792. Online ahead of print.ABSTRACTDealing with nude mice, which lack thymus and therefore are sensitive to unsterile conditions, needs special care and laboratory conditions. For preclinical studies, especially tumour imaging purposes, in which therapeutic properties of drugs or therapeutic compounds are not studied, mice with normal immune system can be a favourable alternative if they carry tumours of interest. In the current study, we introduce an optimized protocol for induction of human tumours in BALB/c mice for preclinical studies. Immune system of BALB/c mice was su...
Source: Molecular Medicine - May 29, 2023 Category: Molecular Biology Authors: Abolfazl Amini Gholamreza Mesbah Fatemeh Tash Shamsabadi Mohammad Ali Zeyghami Yaghoub Safdari Source Type: research
Concurrent oral delivery of non-oncology drugs through solid self-emulsifying system for repurposing in hepatocellular carcinoma
CONCLUSION: The current study revealed a non-oncology drug combination effective against hepatocellular carcinoma. Further, it is concluded that the developed S-SEDDS containing non-oncology drug combination alone and in combination with DTX could be a promising alternative to toxic chemotherapeutics for the effective oral treatment of hepatic cancer.PMID:37216496 | DOI:10.1080/03639045.2023.2216785 (Source: Drug Development and Industrial Pharmacy)
Source: Drug Development and Industrial Pharmacy - May 22, 2023 Category: Drugs & Pharmacology Authors: Rameshwar M Ardad Arehalli S Manjappa Shashikant C Dhawale Popat S Kumbhar Yogesh V Pore Source Type: research
Structural modeling of cytochrome P450 51 from a deep-sea fish points to a novel structural feature in other CYP51s
J Inorg Biochem. 2023 Apr 28;245:112241. doi: 10.1016/j.jinorgbio.2023.112241. Online ahead of print.ABSTRACTCytochromes P450 (CYP), enzymes involved in the metabolism of endogenous and xenobiotic substrates, provide an excellent model system to study how membrane proteins with unique functions have catalytically adapted through evolution. Molecular adaptation of deep-sea proteins to high hydrostatic pressure remains poorly understood. Herein, we have characterized recombinant cytochrome P450 sterol 14α-demethylase (CYP51), an essential enzyme of cholesterol biosynthesis, from an abyssal fish species, Coryphaenoides armat...
Source: Journal of Inorganic Biochemistry - May 20, 2023 Category: Biochemistry Authors: Jared V Goldstone David C Lamb Steven L Kelly Galina I Lepesheva John J Stegeman Source Type: research
