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• Fang, W
• Peng, F
• Yi, T
• Zhang, C
• Wan, C
• Xu, H
• Lam, C
• Yang, X
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• Fang, W
• Peng, F
• Yi, T
• Zhang, C
• Wan, C
• Xu, H
• Lam, C
• Yang, X
• [+] on PubMed
• Fang, W
• Peng, F
• Yi, T
• Zhang, C
• Wan, C
• Xu, H
• Lam, C
• Yang, X

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Molecules 2012, 17(9), 11113-11123; doi:10.3390/molecules170911113

Article

Biological Activity and Safety of Tripterygium Extract Prepared by Sodium Carbonate Extraction

Wei Fang ^1,† , Fan Peng ^1,† , Tao Yi ² , Cong Zhang ¹ , Chunxi Wan ¹ , Huibi Xu ^1,2 , Christopher Waikei Lam ^1,2,*  and Xiangliang Yang ^1,2,*

¹ College of Life Science and Technology, Huazhong University of Science and Technology, Wuhan 430074, China ² State Key Laboratory for Quality Research in Chinese Medicine, Macau Institute for Applied Research in Medicine and Health, Macau University of Science and Technology, Macau, China ^† These authors contributed equally to this work.

* Authors to whom correspondence should be addressed.

Received: 3 August 2012; in revised form: 6 September 2012 / Accepted: 7 September 2012 / Published: 17 September 2012

Download PDF Full-Text [201 KB, uploaded 17 September 2012 08:44 CEST]

Abstract: The commercial preparation named “Tripterygium glycosides” prepared by column chromatography has been used for the treatment of inflammatory and autoimmune diseases with significant efficacy but concurrent toxicity. The aim of this study was to reduce the toxicity of Tripterygium extracts, using cytotoxicity and anti-inflammatory activity of the three principal active components of Tripterygium wilfordii Hook. F. (TWHF) as guiding parameters. Column chromatography was replaced by sodium carbonate extraction for removing the acidic compounds and enriching epoxyditerpenoids and alkaloids in the extract. Results showed that the therapeutic index (IC₅₀/EC₅₀) on murine macrophage Raw 264.7 cells and rat mesangial HBZY-1 cells of the extract prepared by sodium carbonate extraction was significantly higher than that of Tripterygium glycosides (0.8 and 5.2 vs. 0.3 and 2.6, p < 0.05), while its cytotoxicity on human liver HL7702 cells was significantly lower (14.5 ± 1.4 vs. 6.8 ± 0.9, p < 0.05). Further acute oral toxicity experiments showed that the LD₅₀ value of this extract was 1,210 mg/kg compared to 257 mg/kg for Tripterygium glycosides. All the above results suggest that Tripterygium extract prepared by sodium carbonate extraction may represent a potentially optimal source of medicine with good therapeutic index.

Keywords: Tripterygium wilfordii Hook. F.; active components; sodium carbonate extraction; toxicity

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