Alpinetin suppresses CYP3A4, 2C9, and 2E1 activity
            <i>in vitro</i>

Song, Hongming; Wei, Chuankui; Yang, Wu; Niu, Zhao-He; Gong, Mingkai; Hu, Haiyan; Wang, Haibo

doi:10.1080/13880209.2022.2071450

Cited by 2 publications

(2 citation statements)

References 31 publications

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“…In the examination of the remaining activity of the CYP3A4 enzyme after the use of flavonoids as inhibitors, alpinetin proved to be the most potent inhibitor. At a concentration of 100 μM, it caused an inhibitory effect on CYP3A4, whereby the activity of this enzyme decreased to 20% on human liver microsomes [ 137 ] ( Table 8 ). Pinocembrin, for example, showed a smaller effect.…”

Section: Flavonoidsmentioning

confidence: 99%

Flavonoids as CYP3A4 Inhibitors In Vitro

Kondža,

Brizić,

Jokić

2024

Biomedicines

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Flavonoids, a diverse group of polyphenolic compounds found abundantly in fruits, vegetables, and beverages like tea and wine, offer a plethora of health benefits. However, they have a potential interaction with drug metabolism, particularly through the inhibition of the cytochrome P450 3A4 enzyme, the most versatile and abundant enzyme in the liver. CYP3A4 is responsible for metabolizing approximately 50% of clinically prescribed drugs across diverse therapeutic classes, so these interactions have raised concerns about potential adverse effects. This review delves into the scientific evidence surrounding flavonoid-mediated CYP3A4 inhibition, exploring the inhibitory potential of investigated flavonoids and future implications. Kusehnol I, chrysin, leachianone A, and sophoraflavone G showed the largest inhibitory potentials and lowest IC50 values. While the clinical significance of flavonoid-mediated CYP3A4 inhibition in dietary contexts is generally considered low due to moderate intake and complex interactions, it poses a potential concern for individuals consuming high doses of flavonoid supplements or concurrently taking medications metabolized by CYP3A4. This can lead to increased drug exposure, potentially triggering adverse reactions or reduced efficacy.

show abstract

Section: Flavonoidsmentioning

confidence: 99%

Flavonoids as CYP3A4 Inhibitors In Vitro

Kondža,

Brizić,

Jokić

2024

Biomedicines

View full text Add to dashboard Cite

show abstract

“…In the examination of the remaining activity of the CYP3A4 enzyme after the use of flavonoids as inhibitors, alpinetin proved to be the most potent inhibitor. At a concentration of 100 μM, it caused an inhibitory effect on CYP3A4, whereby the activity of this enzyme decreased to 20% on human liver microsomes [132] (Table 8). Pinocembrin, for example, showed a smaller effect.…”

Section: Flavanonesmentioning

confidence: 99%

Flavonoids As CYP3A4 Inhibitors In Vitro

Kondža,

Brizić,

Jokić

2024

Preprint

View full text Add to dashboard Cite

Flavonoids, a diverse group of polyphenolic compounds found abundantly in fruits, vegetables, and beverages like tea and wine, offer a plethora of health benefits. However, their potential interaction with drug metabolism, particularly through inhibition of the cytochrome P450 3A4 enzyme, the most versatile and abundant enzyme in the liver. CYP3A4 is responsible for metabolizing approximately 50% of clinically prescribed drugs across diverse therapeutic classes, so these interactions have raised concerns about potential adverse effects. This review delves into the scientific evidence surrounding flavonoid-mediated CYP3A4 inhibition, exploring the inhibitory potential of investigated flavonoids and future implications. Kusehnol I, chrysin, leachianone A and sophoraflavone G showed the largest inhibitory potentials and lowest IC50 values. While the clinical significance of flavonoid-mediated CYP3A4 inhibition in dietary contexts is generally considered low due to moderate intake and complex interactions, it poses a potential concern for individuals consuming high doses of flavonoid supplements or concurrently taking medications metabolized by CYP3A4. This can lead to increased drug exposure, potentially triggering adverse reactions or reduced efficacy.

show abstract

Alpinetin suppresses CYP3A4, 2C9, and 2E1 activity in vitro

Cited by 2 publications

References 31 publications

Flavonoids as CYP3A4 Inhibitors In Vitro

Flavonoids as CYP3A4 Inhibitors In Vitro

Flavonoids As CYP3A4 Inhibitors In Vitro

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