Xanthium or cockleburr fruit (Xanthium sibiricum PATR., Asteraceae) is used in Traditional Chinese Medicine for nasal or sinus irritations with a viscous discharge and related headache.[1] Fixed oil, volatile oil, phenolic acids (e. g. chlorogenic, dicaffeoylquinic acid) and sesquiterpenes[1–3] are mentioned in literature as chemical constituents. Due to apparent hepatoxicity, also diterpene glycosides, like atractyloside (ATR) and carboxyatractyloside (CATR), are known to be present in the herbal drug material.[1,4,5] ATR was isolated from Xanthii fructus using Sephadex® LH20, centrifugal partition chromatography (CPC) and preparative HPLC. The cell viability in vitro, using the human hepatoma cell line Huh-7 cells with the MTT assay, was examined with isolated ATR, commercial CATR (both 25 to 500 µM) and specially prepared decoctions of Xanthii fructus (100 to 750 µg/mL). All three, ATR and CATR and decoctions inhibited, in this in vitro system slightly the cell viability in a dose dependent manner, indicating a low cytotoxicity. As literature data reported of an obviously higher toxic effect of CATR in comparison to ATR[6] further comparative pharmacological analyses of both compounds are mandatory.
[1] Chinese Herbal Medicine: Materia Medica, Eastland Press Inc, Seattle, Washington 2004.
[2] T. Han, H.-L. Li, Y. Hu, Q.-Y. Zhang, B.-K. Huang, H.-C. Zheng, K. Rahman, L.-P. Qin, Journal of Chinese Integrative Medicine 2006, 4, 194.
[3] T. Han, H.-L. Li, Q.-Y. Zhang, P. Han, H.-C. Zheng, K. Rahman, L.-P. Qin, Phytomedicine 2007, 14, 825.
[4] R. J. Cole, B. P. Stuart, J. A. Lansden, R. H. Cox, Journal of Agricultural and Food Chemistry 1980, 28, 1330.
[5] Y. Wang, T. Han, L.-M. Xue, P. Han, Q.-Y. Zhang, B.-K. Huang, H. Zhang, Q.-L. Ming, W. Peng, L.-P. Qin, Die Pharmazie 2011, 66, 445.
[6] S. Luciani, N. Martini, R. Santi, Life Sciences 1971, 10, 961.