Probe substrates assay estimates the effect of polyphyllin H on the activity of cytochrome P450 enzymes in human liver microsomes

Pharmacology Research & Perspectives, Год журнала: 2024, Номер 12(5)

Опубликована: Авг. 29, 2024

Cytochrome P450 enzymes (CYPs) play a crucial role in phase I metabolic reactions. The activity of CYPs would affect therapeutic efficacy and may even induce toxicity. Given the complex components traditional Chinese medicine, it is important to understand effect active ingredients on guide their prescription. This study aimed evaluate polyphyllin H major isoforms providing reference for clinical prescription its source herbs. effects were evaluated pooled human liver microsomes using probe substrates CYP1A2, 2A6, 2C8, 2C9, 2C19, 2D6, 2E1, 3A4 determine activities. Lineweaver-Burk was used model inhibition, time-dependent inhibition experiment performed characteristics inhibition. Polyphyllin significantly suppressed with IC

Язык: Английский

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Ligand Oxidation Activates a Ruthenium(II) Precatalyst for C–H Hydroxylation

Journal of the American Chemical Society, Год журнала: 2024, Номер 146(33), С. 23067 - 23074

Опубликована: Авг. 12, 2024

A new class of Ru-sulfonamidate precatalysts for sp

Язык: Английский

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Basicity of Mn^III-Hydroxo Complexes Controls the Thermodynamics of Proton-Coupled Electron Transfer Reactions

Inorganic Chemistry, Год журнала: 2024, Номер 63(46), С. 21941 - 21953

Опубликована: Ноя. 5, 2024

Several manganese-dependent enzymes utilize MnIII-hydroxo units in concerted proton–electron transfer (CPET) reactions. We recently demonstrated that hydrogen bonding to the hydroxo ligand synthetic [MnIII(OH)(PaPy2N)]+ complex increased rates of CPET reactions compared [MnIII(OH)(PaPy2Q)]+ lacks a bond. In this work, we determine effect on basicity and evaluate corresponding Both react with strong acids yield MnIII-aqua complexes [MnIII(OH2)(PaPy2Q)]2+ [MnIII(OH2)(PaPy2N)]2+, for which determined pKa values 7.6 13.1, respectively. Reactions one-electron reductants yielded estimates reduction potentials, were combined give O–H bond dissociation free energies (BDFEs) 77 85 kcal mol–1 MnII-aqua [MnII(OH2)(PaPy2Q)]+ [MnII(OH2)(PaPy2N)]+. Using these BDFEs, performed an analysis thermodynamic driving force phenol oxidation by observed unexpected result slower are associated more asynchronous CPET. addition, acidic phenols show deviate from trends, consistent change mechanism proton transfer.

Язык: Английский

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Exploring the Site Selectivity of Arene Oxidation in [(η⁵-C₅Me₅)Ir(η⁶-arene)](OTf)₂ Complexes

Organometallics, Год журнала: 2024, Номер unknown

Опубликована: Ноя. 26, 2024

The oxidation selectivity of the η6-arene ligand in a series [(η5-C5Me5)Ir(η6-arene)](OTf)2 complexes to corresponding [(η5-C5Me5)Ir(η5-phenoxo)](OTf) derivatives was studied as complementary protocol metal-catalyzed borylation-oxidation. A representative compounds prepared with mono-, di-, and trisubstituted arenes well two examples biphenyls rationally explore site C(sp2)–H oxidation. isolated organometallic arene were treated NaClO2 formed desired iridium η5-phenoxo products. While site-selective observed for some compounds, most yielded mixture regioisomers. Regioselectivity primarily determined by electronic factors, while sterics influenced sites that electronically similar.

Язык: Английский

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Platinum Glutamate Acid Complex as a Peroxidase Mimic: High Activity, Controllable Chemical Modification, and Application in Biosensor

Опубликована: Янв. 1, 2023

The rapid progress of nanotechnology has catalyzed the emergence nanozymes, nanomaterials endowed with enzyme-like catalytic activity. Nonetheless, challenges persist, including variations in performance between batches and restricted atomic utilization. This study introduces a platinum glutamic acid complex, Pt(Glu)2, as small molecule peroxidase mimic boasting high efficacy. Notably, Pt(Glu)2 is easily synthesized seamlessly integrated into natural enzymes without compromising their functionality. resulting Pt(Glu)2-modified exhibit amplified cascade reactions, outperforming capabilities nanozymes. Leveraging this complex biosensors, we successfully detected cholesterol alkaline phosphatase human serum, underscoring its potential clinical testing. These findings offer insights development mimetics versatile applications catalysis biosensing.

Язык: Английский

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Predictable, Scalable Aliphatic C–H Oxidation of Complex, Drug-Like Molecules

Synfacts, Год журнала: 2023, Номер 19(11), С. 1075 - 1075

Опубликована: Окт. 14, 2023

Key words manganese catalysis - N-heterocycles metabolites gram-scale synthesis C–H oxidation

Язык: Английский

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