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Molecules 2015, 20(1), 792-806;

Pinelliae Rhizoma, a Toxic Chinese Herb, Can Significantly Inhibit CYP3A Activity in Rats

International Institute for Translational Chinese Medicine, Guangzhou University of Chinese Medicine, Guangzhou 510006, China
College of Pharmacy, Fujian University of Traditional Chinese Medicine, Fuzhou 350108, China
State Key Laboratory of Quality Research in Chinese Medicine, Macau University of Science and Technology, Macau, China
Institute of Chinese Meteria Medica, China Academy of Chinese Medical Sciences, Beijing 100700, China
These authors contributed equally to this work.
Author to whom correspondence should be addressed.
Academic Editor: Marcello Iriti
Received: 24 November 2014 / Accepted: 31 December 2014 / Published: 7 January 2015
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Raw Pinelliae Rhizoma (RPR) is a representative toxic herb that is widely used for eliminating phlegm or treating cough and vomiting. Given its irritant toxicity, its processed products, including Pinelliae Rhizoma Praeparatum (PRP) and Pinelliae Rhizoma Praeparatum cum Zingibere et Alumine (PRPZA), are more commonly applied and administered concomitantly with other chemical drugs, such as cough medications. This study aimed to investigate the effects of RPR, PRP, and PRPZA on CYP3A activity. Testosterone (Tes) and buspirone (BP) were used as specific probe substrates ex vivo and in vivo, respectively. CYP3A activity was determined by the metabolite formation ratios from the substrates. Ex vivo results show that the metabolite formation ratios from Tes significantly decreased, indicating that RPR, PRP, and PRPZA could inhibit CYP3A activity in rats. CYP3A protein and mRNA levels were determined to explore the underlying mechanism. These levels showed marked and consistent down-regulation with CYP3A activity. A significant decrease in metabolite formation ratios from BP was also found in PRPZA group in vivo, implying that PRPZA could inhibit CYP3A activity. Conclusively, co-administration of PR with other CYP3A-metabolizing drugs may cause drug–drug interactions. Clinical use of PR-related formulae should be monitored carefully to avoid adverse interactions. View Full-Text
Keywords: Pinelliae Rhizoma; CYP3A; testosterone; buspirone; drug–drug interactions Pinelliae Rhizoma; CYP3A; testosterone; buspirone; drug–drug interactions

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Wu, J.; Cheng, Z.; He, S.; Shi, J.; Liu, S.; Zhang, G.; Zhu, L.; Liu, L.; Liu, Z.; Lin, N.; Lu, L. Pinelliae Rhizoma, a Toxic Chinese Herb, Can Significantly Inhibit CYP3A Activity in Rats. Molecules 2015, 20, 792-806.

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