BACKGROUND Herbal medicine represents a significant component of disease prevention and therapy in most African countries. Herb-drug interactions (HDI) can arise from the co-administration of herbal and orthodox medicines. OBJECTIVE This study assessed the potential for HDI of V. amygdalina, O. gratissimum, M. oleifera, A. indica, and P. nitida extracts using in vitro assays. Little is known about these medicinal plants' potential for drug interaction despite their extensive use in Nigeria for several disease conditions. METHOD The medicinal plant crude extracts were evaluated for Cytochrome P450 (CYP) enzyme induction using cryopreserved human hepatocytes. Enzyme activity was determined by quantifying probe substrate metabolism and metabolite formation using liquid chromatography-mass spectrometry/mass spectrometry. The extracts were evaluated for the potential to inhibit P-glycoprotein (P-gp) activity using human embryonic kidney membrane vesicles over-expressing human P-gp. The herbal extracts in vivo drug interaction potential was predicted based on the USFDA drug interaction guidance. RESULT O. gratissimum and P. nitida methanol extracts induced CYP1A2 enzyme activity by greater than 3-fold. P. nitida methanol extracts showed over 2-fold induction of CYP1A2 mRNA expression. O. gratissimum methanol extract induced CYP2B6 mRNA expression over 2-fold. P. nitida and A. indica methanol extracts showed potent inhibition of P-gp activity (IC50: 3.8 and 5.4 μg/mL), respectively, while V. amygdalina and M. oleifera methanol extracts showed moderate P-gp inhibition (IC50: 12.1 and 37.2 μg/mL, respectively). CONCLUSION Our studies suggested that the medicinal plants' extracts can modulate CYP enzymes and P-gp activity with the potential to cause herb-drug interaction in vivo.

中文翻译：

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尼日利亚药用植物提取物对人 P-糖蛋白和细胞色素 P450 酶诱导的评估：对草药-药物相互作用的影响。

背景技术在大多数非洲国家，草药是疾病预防和治疗的重要组成部分。草药与传统药物的共同服用可能会产生草药-药物相互作用（HDI）。目的 本研究使用体外测定评估了杏仁、O. gratissimum、M. oleifera、A. indica 和 P. nitida 提取物的 HDI 潜力。尽管这些药用植物在尼日利亚广泛用于治疗多种疾病，但人们对它们的药物相互作用潜力知之甚少。方法 使用冷冻保存的人肝细胞评估药用植物粗提物对细胞色素 P450 (CYP) 酶的诱导作用。通过使用液相色谱-质谱/质谱定量探针底物代谢和代谢物形成来测定酶活性。使用过表达人 P-gp 的人胚胎肾膜囊泡评估提取物抑制 P-糖蛋白 (P-gp) 活性的潜力。根据USFDA药物相互作用指南预测草药提取物体内药物相互作用潜力。结果 O. gratissimum 和 P. nitida 甲醇提取物诱导 CYP1A2 酶活性超过 3 倍。P. niida 甲醇提取物显示 CYP1A2 mRNA 表达诱导超过 2 倍。O. gratissimum 甲醇提取物诱导 CYP2B6 mRNA 表达超过 2 倍。P. nitida 和 A. indica 甲醇提取物分别显示出对 P-gp 活性的有效抑制（IC50：3.8 和 5.4 μg/mL），而 V. amygdalina 和 M. oleifera 甲醇提取物显示出中度 P-gp 抑制作用（IC50：12.1）和 37.2 μg/mL，分别）。结论 我们的研究表明药用植物提取物可以调节 CYP 酶和 P-gp 活性，有可能在体内引起草药-药物相互作用。