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
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
The Impact of Surface Area per Volume (SA/V) Ratio on Drug Transport from Supersaturated Solutions of Ketoconazole
Eur J Pharm Biopharm. 2023 May 16:S0939-6411(23)00138-8. doi: 10.1016/j.ejpb.2023.05.016. Online ahead of print.ABSTRACTThe purpose of this study aimed to evaluate the impact of the surface area per volume (SA/V) ratio on drug transport from two supersaturated solutions (SSs) of ketoconazole with and without hydroxypropyl methylcellulose (HPMC), used as a precipitation inhibitor. In vitro dissolution, membrane permeation with two SA/V ratios, and in vivo absorption profiles for both SSs were determined. For the SS without HPMC, a two-step precipitation process due to the liquid-liquid phase separation was observed; the con...
Source: European Journal of Pharmaceutics and Biopharmaceutics - May 18, 2023 Category: Drugs & Pharmacology Authors: Haruki Higashino Corey Develin Chie Higashino Tyler Lim Blair Miezeiewski Robert Strab Rachana Patel Siddhartha Bhoopathy Ismael Hidalgo Source Type: research
Isolation and Identification of Flavanone Derivative Eriodictyol from the Methanol Extract of < em > Afzelia africana < /em > Bark and Its Antimicrobial and Antioxidant Activities
CONCLUSION: The study reports for the first time the identification of eriodictyol from the bark of A. africana which exhibited significant antioxidant and antimicrobial properties.PMID:37200890 | PMC:PMC10188263 | DOI:10.1155/2023/9345047 (Source: Evidence-based Complementary and Alternative Medicine)
Source: Evidence-based Complementary and Alternative Medicine - May 18, 2023 Category: Complementary Medicine Authors: Bright Yaw Vigbedor Clement Osei Akoto David Neglo Source Type: research
The Impact of Surface Area per Volume (SA/V) Ratio on Drug Transport from Supersaturated Solutions of Ketoconazole
Eur J Pharm Biopharm. 2023 May 16:S0939-6411(23)00138-8. doi: 10.1016/j.ejpb.2023.05.016. Online ahead of print.ABSTRACTThe purpose of this study aimed to evaluate the impact of the surface area per volume (SA/V) ratio on drug transport from two supersaturated solutions (SSs) of ketoconazole with and without hydroxypropyl methylcellulose (HPMC), used as a precipitation inhibitor. In vitro dissolution, membrane permeation with two SA/V ratios, and in vivo absorption profiles for both SSs were determined. For the SS without HPMC, a two-step precipitation process due to the liquid-liquid phase separation was observed; the con...
Source: European Journal of Pharmaceutics and Biopharmaceutics - May 18, 2023 Category: Drugs & Pharmacology Authors: Haruki Higashino Corey Develin Chie Higashino Tyler Lim Blair Miezeiewski Robert Strab Rachana Patel Siddhartha Bhoopathy Ismael Hidalgo Source Type: research
Isolation and Identification of Flavanone Derivative Eriodictyol from the Methanol Extract of < em > Afzelia africana < /em > Bark and Its Antimicrobial and Antioxidant Activities
CONCLUSION: The study reports for the first time the identification of eriodictyol from the bark of A. africana which exhibited significant antioxidant and antimicrobial properties.PMID:37200890 | PMC:PMC10188263 | DOI:10.1155/2023/9345047 (Source: Evidence-based Complementary and Alternative Medicine)
Source: Evidence-based Complementary and Alternative Medicine - May 18, 2023 Category: Complementary Medicine Authors: Bright Yaw Vigbedor Clement Osei Akoto David Neglo Source Type: research
Ketoconazole as second-line treatment for Cushing ’s disease after transsphenoidal surgery: systematic review and meta-analysis
ConclusionKetoconazole can be considered a safe and efficacious option for Cushing’s disease treatment after pituitary surgery.Systematic review registrationhttps://www.crd.york.ac.uk/prospero/#searchadvanced, (CRD42022308041). (Source: Frontiers in Endocrinology)
Source: Frontiers in Endocrinology - May 8, 2023 Category: Endocrinology Source Type: research
Studies on the inhibitory effect of isavuconazole on flumatinib metabolism in vitro and in vivo
As the validated agent for the treatment of chronic myelogenous leukemia (CML), flumatinib is a novel oral tyrosine kinase inhibitor (TKI) with higher potency and selectivity for BCR-ABL1 kinase compared to imatinib. Many patients experience aspergillosis infection and they may start using isavuconazole, which is an inhibitor of CYP3A4. However, there is no study on their interaction in vitro and in vivo. In the present study, the concentrations of flumatinib and its major metabolite M1 were rapidly determined using an stable ultra-performance liquid chromatography tandem mass spectrometry (UPLC-MS/MS) method. The half-max...
Source: Frontiers in Pharmacology - May 4, 2023 Category: Drugs & Pharmacology Source Type: research
Mechanism-Based Inactivation of Cytochrome P450 3A by Evodol
Xenobiotica. 2023 Apr 24:1-33. doi: 10.1080/00498254.2023.2207200. Online ahead of print.ABSTRACT1. Evodol is one of the furanoids isolated from the fruits of Evodia rutaecarpa that has been widely prescribed for the treatment of gastrointestinal diseases in China. The aim of this study was to investigate the inhibitory effect of evodol on CYP3A.2. A 30-min preincubation of evodol with human liver microsomes raised an obvious left IC50 shift, 3.9-fold for midazolam 1'-hydroxylation and 3.2-fold for testosterone 6β-hydroxylation. Evodol inactivated CYP3A in a time-, concentration- and NADPH-dependent manner, with KI and ki...
Source: Xenobiotica - April 24, 2023 Category: Research Authors: Jie Zhao Jingyu He Jie Xu Source Type: research
Mechanism-Based Inactivation of Cytochrome P450 3A by Evodol
Xenobiotica. 2023 Apr 24:1-33. doi: 10.1080/00498254.2023.2207200. Online ahead of print.ABSTRACT1. Evodol is one of the furanoids isolated from the fruits of Evodia rutaecarpa that has been widely prescribed for the treatment of gastrointestinal diseases in China. The aim of this study was to investigate the inhibitory effect of evodol on CYP3A.2. A 30-min preincubation of evodol with human liver microsomes raised an obvious left IC50 shift, 3.9-fold for midazolam 1'-hydroxylation and 3.2-fold for testosterone 6β-hydroxylation. Evodol inactivated CYP3A in a time-, concentration- and NADPH-dependent manner, with KI and ki...
Source: Xenobiotica - April 24, 2023 Category: Research Authors: Jie Zhao Jingyu He Jie Xu Source Type: research
Mechanism-Based Inactivation of Cytochrome P450 3A by Evodol
Xenobiotica. 2023 Apr 24:1-33. doi: 10.1080/00498254.2023.2207200. Online ahead of print.ABSTRACT1. Evodol is one of the furanoids isolated from the fruits of Evodia rutaecarpa that has been widely prescribed for the treatment of gastrointestinal diseases in China. The aim of this study was to investigate the inhibitory effect of evodol on CYP3A.2. A 30-min preincubation of evodol with human liver microsomes raised an obvious left IC50 shift, 3.9-fold for midazolam 1'-hydroxylation and 3.2-fold for testosterone 6β-hydroxylation. Evodol inactivated CYP3A in a time-, concentration- and NADPH-dependent manner, with KI and ki...
Source: Xenobiotica - April 24, 2023 Category: Research Authors: Jie Zhao Jingyu He Jie Xu Source Type: research
Mechanism-Based Inactivation of Cytochrome P450 3A by Evodol
Xenobiotica. 2023 Apr 24:1-33. doi: 10.1080/00498254.2023.2207200. Online ahead of print.ABSTRACT1. Evodol is one of the furanoids isolated from the fruits of Evodia rutaecarpa that has been widely prescribed for the treatment of gastrointestinal diseases in China. The aim of this study was to investigate the inhibitory effect of evodol on CYP3A.2. A 30-min preincubation of evodol with human liver microsomes raised an obvious left IC50 shift, 3.9-fold for midazolam 1'-hydroxylation and 3.2-fold for testosterone 6β-hydroxylation. Evodol inactivated CYP3A in a time-, concentration- and NADPH-dependent manner, with KI and ki...
Source: Xenobiotica - April 24, 2023 Category: Research Authors: Jie Zhao Jingyu He Jie Xu Source Type: research
The conjunctival fungal microflora of horses in a North Queensland tropical environment and their in vitro susceptibilities to antifungal agents
The objectives of this study were to determine the fungal species specific to the eyes of horses in the Townsville region; to investigate the potential risk factors associated with the presence of fungi; and to test their susceptibility to antifungals to create an empirical guide for treatment. The eyes of forty ophthalmologically normal horses from James Cook University were sampled throughout the summer months of December 2017, January 2018, and January and February 2020. Cultured fungi were identified morphologically, and their identity confirmed by comparing partial 18sRNA DNA sequences with the NCBI nucleotide databas...
Source: Veterinary Research Communications - April 6, 2023 Category: Veterinary Research Source Type: research
