<i>Ginkgo biloba L.</i> flavonoids inhibit CYP 2A5; potential dietary supplement for nicotine replacement therapy enhancement

Eleftheriou, Constantina; Zacharia, Lefteris C.

doi:10.1080/14786419.2021.1972419

Natural Product Research

2021

DOI: 10.1080/14786419.2021.1972419

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Ginkgo biloba L. flavonoids inhibit CYP 2A5; potential dietary supplement for nicotine replacement therapy enhancement

Constantina Eleftheriou

Lefteris C. Zacharia

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Cited by 2 publications

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Coumaroyl and feruloyl flavonoid glycosides from the male flowers of Ginkgo biloba L. and their inhibitory activity against α-glucosidase

Zhou

Zhu

et al. 2021

Natural Product Research

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Four flavonoid glycosides containing coumaroyl or feruloyl groups were isolated from the male flowers of Ginkgo biloba L., and compounds 3 and 4 were identified as novel compounds. The inhibitory activities against α-glucosidase were investigated by docking studies, in vitro assays and kinetic studies. The docking results showed that all compounds mainly formed hydrogen-bond and π-π-stacking interactions with α-glucosidase. Compound 4 had the lowest binding energy and maximum number of hydrogen bonds. Subsequently, the in vitro assays showed that compound 4 exhibited the strongest inhibitory potency. Finally, the kinetic studies indicated the inhibitory mode of compounds 1-4 against α-glucosidase were mixed types of competitive and non-competitive. Together, these findings suggested that the isolated flavonoid glycosides in this study, especially compound 4, have potential as α-glucosidase inhibitors.

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Coumaroyl and feruloyl flavonoid glycosides from the male flowers of Ginkgo biloba L. and their inhibitory activity against α-glucosidase

Zhou

Zhu

et al. 2021

Natural Product Research

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Systematic Review of Naturally Derived Substances That Act as Inhibitors of the Nicotine Metabolizing Enzyme Cytochrome P450 2A6

Tzoupis,

Papavasileiou,

Papatzelos

et al. 2024

IJMS

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Tobacco smoking has been highlighted as a major health challenge in modern societies. Despite not causing death directly, smoking has been associated with several health issues, such as cardiovascular diseases, respiratory disorders, and several cancer types. Moreover, exposure to nicotine during pregnancy has been associated with adverse neurological disorders in babies. Nicotine Replacement Therapy (NRT) is the most common strategy employed for smoking cessation, but despite its widespread use, NRT presents with low success and adherence rates. This is attributed partially to the rate of nicotine metabolism by cytochrome P450 2A6 (CYP2A6) in each individual. Nicotine addiction is correlated with the high rate of its metabolism, and thus, novel strategies need to be implemented in NRT protocols. Naturally derived products are a cost-efficient and rich source for potential inhibitors, with the main advantages being their abundance and ease of isolation. This systematic review aims to summarize the natural products that have been identified as CYP2A6 inhibitors, validated through in vitro and/or in vivo assays, and could be implemented as nicotine metabolism inhibitors. The scope is to present the different compounds and highlight their possible implementation in NRT strategies. Additionally, this information would provide valuable insight regarding CYP2A6 inhibitors, that can be utilized in drug development via the use of in silico methodologies and machine-learning models to identify new potential lead compounds for optimization and implementation in NRT regimes.

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Ginkgo biloba L. flavonoids inhibit CYP 2A5; potential dietary supplement for nicotine replacement therapy enhancement

Cited by 2 publications

References 21 publications

Coumaroyl and feruloyl flavonoid glycosides from the male flowers of Ginkgo biloba L. and their inhibitory activity against α-glucosidase

Coumaroyl and feruloyl flavonoid glycosides from the male flowers of Ginkgo biloba L. and their inhibitory activity against α-glucosidase

Systematic Review of Naturally Derived Substances That Act as Inhibitors of the Nicotine Metabolizing Enzyme Cytochrome P450 2A6

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