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植酸(肌醇六磷酸,IP6)对不同肝模型细胞色素 P450 及外源物质代谢系统的可能影响。

On the Possible Effect of Phytic Acid (Myo-Inositol Hexaphosphoric Acid, IP6) on Cytochromes P450 and Systems of Xenobiotic Metabolism in Different Hepatic Models.

机构信息

Department of Medical Chemistry and Biochemistry, Faculty of Medicine and Dentistry, Palacky University Olomouc, 775 15 Olomouc, Czech Republic.

Department of Pharmacology, Faculty of Medicine and Dentistry, Palacky University Olomouc, 775 15 Olomouc, Czech Republic.

出版信息

Int J Mol Sci. 2024 Mar 23;25(7):3610. doi: 10.3390/ijms25073610.

Abstract

As compounds of natural origin enter human body, it is necessary to investigate their possible interactions with the metabolism of drugs and xenobiotics in general, namely with the cytochrome P450 (CYP) system. Phytic acid (myo-inositol hexaphosphoric acid, IP6) is mainly present in plants but is also an endogenous compound present in mammalian cells and tissues. It has been shown to exhibit protective effect in many pathological conditions. For this paper, its interaction with CYPs was studied using human liver microsomes, primary human hepatocytes, the HepG2 cell line, and molecular docking. Docking experiments and absorption spectra demonstrated the weak ability of IP6 to interact in the heme active site of CYP1A. Molecular docking suggested that IP6 preferentially binds to the protein surface, whereas binding to the active site of CYP1A2 was found to be less probable. Subsequently, we investigated the ability of IP6 to modulate the metabolism of xenobiotics for both the mRNA expression and enzymatic activity of CYP1A enzymes. Our findings revealed that IP6 can slightly modulate the mRNA levels and enzyme activity of CYP1A. However, thanks to the relatively weak interactions of IP6 with CYPs, the chances of the mechanisms of clinically important drug-drug interactions involving IP6 are low.

摘要

当天然化合物进入人体时,有必要研究它们与药物和外源性物质代谢的相互作用,特别是与细胞色素 P450(CYP)系统的相互作用。植酸(肌醇六磷酸,IP6)主要存在于植物中,但也是哺乳动物细胞和组织中的内源性化合物。已证明它在许多病理条件下具有保护作用。在本文中,使用人肝微粒体、原代人肝细胞、HepG2 细胞系和分子对接研究了其与 CYP 的相互作用。对接实验和吸收光谱表明,IP6 与 CYP1A 的血红素活性位点相互作用的能力较弱。分子对接表明,IP6 优先与蛋白质表面结合,而与 CYP1A2 的活性位点结合的可能性较小。随后,我们研究了 IP6 调节外源性物质代谢的能力,包括 CYP1A 酶的 mRNA 表达和酶活性。我们的研究结果表明,IP6 可以轻微调节 CYP1A 的 mRNA 水平和酶活性。然而,由于 IP6 与 CYP 相互作用较弱,涉及 IP6 的临床上重要药物-药物相互作用的机制的可能性较低。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ab28/11011971/a3ddc735cfc9/ijms-25-03610-g001.jpg

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