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体外抗氧化潜力以及一种谷胱甘肽增强剂膳食补充剂对选定大鼠肝脏细胞色素P450酶活性的影响。

In Vitro Antioxidant Potential and Effect of a Glutathione-Enhancer Dietary Supplement on Selected Rat Liver Cytochrome P450 Enzyme Activity.

作者信息

N'guessan Benoit B, Amponsah Seth K, Dugbartey George J, Awuah Kwabena D, Dotse Eunice, Aning Abigail, Kukuia Kennedy K E, Asiedu-Gyekye Isaac J, Appiah-Opong Regina

机构信息

Department of Pharmacology and Toxicology, School of Pharmacy, College of Health Sciences, University of Ghana, Ghana.

Department of Clinical Pathology, Noguchi Memorial Institute for Medical Research, College of Health Sciences, University of Ghana, Ghana.

出版信息

Evid Based Complement Alternat Med. 2018 May 24;2018:7462839. doi: 10.1155/2018/7462839. eCollection 2018.

DOI:10.1155/2018/7462839
PMID:29977317
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC5994258/
Abstract

BACKGROUND

There is considerable evidence that many people take dietary supplements including those of herbal origin as an alternative therapy to improve their health. One such supplement, with an amalgam of constituents, is CellGevity®. However, the effect of this dietary supplement on drug-metabolizing enzymes is poorly understood, as it has not been studied extensively. Therefore, we investigated the effect of CellGevity dietary supplement on selected rat liver microsomal cytochrome P450 (CYP) enzymes, the most common drug-metabolizing enzymes. We also determined the total antioxidant potential of this dietary supplement .

METHODS

To determine the antioxidant potential of CellGevity dietary supplement, 2,2-diphenyl-2-picryl-hydrazyl (DPPH), total phenolic, and flavonoid assays were used after initial preparation of a solution form of the supplement (low dose, LD; 4 mg/kg and high dose, HD; 8 mg/kg). Rats received oral administration of these doses of the supplement for 7 days, after which the effect of the supplement on selected liver CYP enzymes was assessed using probe substrates and spectroscopic and high-performance liquid chromatographic methods. Rats which received daily administration of 80 mg/kg of phenobarbitone and distilled water served as positive and negative controls, respectively.

RESULTS

The IC value of the supplement 0.34 ± 0.07 mg/ml compared to 0.076 ± 0.03 mg/ml of the BHT (positive control). The total phenolic content of the supplement at a concentration of 2.5 mg/ml was 34.97 g gallic acid equivalent (GAE)/100 g while its total flavonoid content at a concentration of 2.5 mg/ml was 6 g quercetin equivalent (QE)/100 g. The supplement significantly inhibited rat CYP2B1/2B2 (LDT 92.4%; HDT 100%), CYP3A4 (LDT 81.2%; HDT 71.7%), and CYP2C9 (LDT 21.7%; HDT 28.5%) while it had no significant inhibitory effect on CYPs 1A1/1A2, CYP1A2, and CYP2D6.

CONCLUSION

CellGevity dietary supplement possesses moderate antioxidant activity and has an inhibitory effect on selected rat liver CYP enzymes, suggesting its potential interaction with drugs metabolized by CYP enzymes.

摘要

背景

有大量证据表明,许多人将膳食补充剂(包括草药来源的补充剂)作为改善健康的替代疗法。一种这样的补充剂是CellGevity®,它含有多种成分。然而,这种膳食补充剂对药物代谢酶的影响了解甚少,因为尚未进行广泛研究。因此,我们研究了CellGevity膳食补充剂对选定的大鼠肝脏微粒体细胞色素P450(CYP)酶(最常见的药物代谢酶)的影响。我们还测定了这种膳食补充剂的总抗氧化潜力。

方法

为了测定CellGevity膳食补充剂的抗氧化潜力,在将补充剂制成溶液形式(低剂量,LD;4mg/kg和高剂量,HD;8mg/kg)后,使用2,2-二苯基-2-苦基肼(DPPH)、总酚和类黄酮测定法。大鼠口服这些剂量的补充剂7天,之后使用探针底物以及光谱和高效液相色谱法评估补充剂对选定的肝脏CYP酶的影响。每天分别给予80mg/kg苯巴比妥和蒸馏水的大鼠作为阳性和阴性对照。

结果

补充剂的IC值为0.34±0.07mg/ml,而丁基羟基甲苯(阳性对照)为0.076±0.03mg/ml。补充剂在浓度为2.5mg/ml时的总酚含量为34.97g没食子酸当量(GAE)/100g,而其在浓度为2.5mg/ml时的总黄酮含量为6g槲皮素当量(QE)/100g。该补充剂显著抑制大鼠CYP2B1/2B2(低剂量组抑制率92.4%;高剂量组抑制率100%)、CYP3A4(低剂量组抑制率81.2%;高剂量组抑制率71.7%)和CYP2C9(低剂量组抑制率21.7%;高剂量组抑制率28.5%),而对CYP1A1/1A2、CYP1A2和CYP2D6没有显著抑制作用。

结论

CellGevity膳食补充剂具有适度的抗氧化活性,并且对选定的大鼠肝脏CYP酶有抑制作用,表明其可能与由CYP酶代谢的药物发生相互作用。

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