In vitro inhibition of human cytochrome P450 by cudratricusxanthone A

Sim, Juhee; Choi, Eunhwa; Lee, You‐Mie; Jeong, Gil‐Saeng; Lee, Sangkyu

doi:10.1016/j.fct.2015.04.024

Cited by 10 publications

(4 citation statements)

References 26 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…138 In a follow-up study, CTXA has been demonstrated to exhibit reversible competitive inhibition of CYP1A2 and CYP2C9 and non-competitive inhibition of CYP2C8 in human liver microsomes, which has begun to shed light on the in vivo metabolism of CTXA. 139 Cudratricusxanthone B, as another example, has also been investigated for its pharmacokinetics by a fast and sensitive HPLC-MS/ MS method, but its oral bioavailability (OB) remains unclear and merits future investigation. 140 Therefore, it is suggested that the pharmacokinetics of this plant should be studied systematically.…”

Section: Othersmentioning

confidence: 99%

Cudrania tricuspidata: an updated review on ethnomedicine, phytochemistry and pharmacology

et al. 2017

View full text Add to dashboard Cite

show abstract

Section: Othersmentioning

confidence: 99%

Cudrania tricuspidata: an updated review on ethnomedicine, phytochemistry and pharmacology

et al. 2017

View full text Add to dashboard Cite

show abstract

“…Each compound was incubated with cocktail substrates, including nine CYP substrates, in HLMs in order to explore the selective inhibitory ability of HYIpro‐3‐1 and its analogs (Sim, Choi, Lee, Jeong, & Lee, 2015; Table 1). The amounts of metabolites selectively produced by each CYP were measured with LC‐MS/MS in SRM mode to evaluate the activity effect of the compound on nine CYPs.…”

Section: Resultsmentioning

confidence: 99%

Selective inhibitory effects of HYIpro‐3‐1 on CYP1A2 in human liver microsomes

Kim

Lee

et al. 2021

Biopharm & Drug Disp

Self Cite

View full text Add to dashboard Cite

CYP1A2 is one of the main Cytochrome P450 enzymes in the human liver associated with the metabolism of several xenobiotics. CYP1A2 is especially involved in the metabolic activation of different procarcinogens. Therefore, the development of cancer may be inhibited by inhibiting CYP1A2 activity. Here, the inhibitory effect of HYIpro‐3‐1 and its derivatives on CYP1A2 activity in human liver microsomes (HLM) was studied through LC‐MS/MS using a cocktail assay. Among the four compounds, HYIpro‐3‐1 showed the most selective and strongest inhibitory effect on CYP1A2 at IC50 values of 0.1 µM in HLMs and inhibition was confirmed using purified human CYP1A2. It was determined that inhibition is reversible because the inhibitory effect of HYIpro‐3‐1 is not dependent on preincubation time. HYIpro‐3‐1 showed a typical pattern of competitive inhibition for CYP1A2‐catalyzed phenacetin O‐deethylation, based on the Lineweaver‐Burk plot, with a Ki value of 0.05 μM in HLMs; the secondary plot also showed a linear pattern. In our study, HYIpro‐3‐1 was proposed as a novel inhibitor with the capacity to selectively inhibit CYP1A activity in HLMs.

show abstract

“…Cudratricusxanthone A ( 1 ), a prenylated xanthone isolated from C. tricuspidata , has been reported to have diverse biological effects, including hepatoprotective [8,26], neuroprotective [10], antiplatelet, anticoagulant, profobrinolytic [27], pancreatic beta cell-protective [28], and human cytochrome P450 inhibitory activities [29]. Additionally, although this compound has been shown to have anti-inflammatory effects in LPS-induced RAW264.7 cells [8], the antineuroinflammatory mechanisms of cudratricusxanthone A had not yet been examined in BV2 microglial cells.…”

Section: Discussionmentioning

confidence: 99%

A Prenylated Xanthone, Cudratricusxanthone A, Isolated from Cudrania tricuspidata Inhibits Lipopolysaccharide-Induced Neuroinflammation through Inhibition of NF-κB and p38 MAPK Pathways in BV2 Microglia

et al. 2016

View full text Add to dashboard Cite

Cudrania tricuspidata Bureau (Moraceae) is an important source of traditional Korean and Chinese medicines used to treat neuritis and inflammation. Cudratricusxanthone A (1), a prenylated xanthone, isolated from C. tricuspidata, has a variety of biological and therapeutic activities. The goal of this study was to examine the effects of compound 1 on neuroinflammation and characterize its mechanism of action in lipopolysaccharide (LPS)-stimulated BV2 microglia. Cudratricusxanthone A (1) suppressed the expression of inducible nitric oxide synthase (iNOS) and cyclooxygenase (COX)-2 enzymes and decreased the production of iNOS-derived nitric oxide and COX-2-derived prostaglandin E2 in LPS-stimulated mouse BV2 microglia. The compound also decreased tumor necrosis factor-α, interleukin (IL)-1β, and IL-12 production; inhibited the phosphorylation and degradation of IκB-α; and blocked the nuclear translocation of p50 and p65 in mouse BV2 microglia induced by LPS. Cudratricusxanthone A (1) had inhibitory effects on nuclear factor kappa B DNA-binding activity. Additionally, it inhibited the p38 mitogen-activated protein kinase signaling pathway. Our data suggests that cudratricusxanthone A (1) may be a useful therapeutic agent in the treatment of neurodegenerative diseases caused by neuroinflammation.

show abstract

In vitro inhibition of human cytochrome P450 by cudratricusxanthone A

Cited by 10 publications

References 26 publications

Cudrania tricuspidata: an updated review on ethnomedicine, phytochemistry and pharmacology

Cudrania tricuspidata: an updated review on ethnomedicine, phytochemistry and pharmacology

Selective inhibitory effects of HYIpro‐3‐1 on CYP1A2 in human liver microsomes

A Prenylated Xanthone, Cudratricusxanthone A, Isolated from Cudrania tricuspidata Inhibits Lipopolysaccharide-Induced Neuroinflammation through Inhibition of NF-κB and p38 MAPK Pathways in BV2 Microglia

Contact Info

Product

Resources

About