Cycloartane-type triterpenes from Euphorbia fischeriana stimulate human CYP3A4 promoter activity |
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| Institution: | 1. College of Chemistry and Chemical Engineering, Yunnan Normal University, Kunming 650500, China;2. State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650201, China;1. Beijing Key Laboratory of Traditional Chinese Medicine Protection and Utilization, College of Resources Science and Technology, Beijing Normal University, Haidian District, Beijing 100875, China;2. Department of Entomology, China Agricultural University, Haidian District, Beijing 100094, China;3. Analytical and Testing Center, Beijing Normal University, Haidian District, Beijing 100875, China;1. College of Chemistry and Chemical Engineering, Yunnan Normal University, Kunming 650500, China;2. State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650201, China;1. College of Pharmacy, Academy of Integrative Medicine, College of Medical Laboratory, The National & Local Joint Engineering Research Center for Drug Development of Neurodegenerative Disease, Dalian Medical University, Dalian 116044, China;2. The First Affiliated Hospital of Dalian Medical University, No. 222 Zhongshan Road, Dalian 116011, China;1. Department of Natural Products and Alternative Medicine, Faculty of Pharmacy, King Abdulaziz University, Jeddah, Saudi Arabia;2. Department of Pharmacognosy, Faculty of Pharmacy, Al- Azhar University, Assiut, Egypt;3. Department of Pharmacognosy, Faculty of Pharmacy, Cairo University, Cairo, Egypt;4. King Khalid University, Faculty of Science, Biology Department, Abha, Saudi Arabia;5. Cell Culture Lab, Egyptian Organization for Biological Products and Vaccines (VACSERA Holding Company), 51 Wezaret El-Zeraa St., Agouza, Giza, Egypt;6. Department of Pharmacognosy and Pharmaceutical Chemistry, College of Pharmacy, Taibah University, Al Madinah Al Munawwarah, Saudi Arabia;7. Department of Pharmacognosy, Faculty of Pharmacy, Assiut University, Assiut, Egypt;1. College of Pharmacy, Academy of Integrative Medicine, The National & Local Joint Engineering Research Center for Drug Development of Neurodegenerative Disease, Dalian Medical University, Dalian 116044, China;2. The First Affiliated Hospital of Dalian Medical University, No. 222 Zhongshan Road, Dalian 116011, China;3. Beijing University of Chinese Medicine, Beijing 100029, China |
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| Abstract: | A chemical study of the roots of Euphorbia fischeriana resulted in the isolation of seven triterpenes (1–7), including two new compounds: (24R,S)-3β-24,31-epoxy-24-methylcycloartane (1) and (24R,S)-3β,31-dihydroxy-24-methoxy-24-methylcycloartane (2). Their structures were elucidated through extensive spectroscopic analyses. Cycloartanes 1–4 showed significant human CYP3A4 promoter activity through a series of luciferase reporter assays. Of these compounds, 3 and 4 activated the pregnane X receptor (PXR) and induced CYP3A4 mRNA expression in human primary hepatocytes. However, despite showing the most potent human CYP3A4 promoter activity via a PXR-independent pathway, 2 did not affect CYP3A4 mRNA expression in human primary hepatocytes. This difference is correlated to substitutions in C-24 and C-25 of the cycloartane structure. |
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| Keywords: | Cycloartane CYP3A4 Promoter Pregnane X receptor |
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