Planta Med 2010; 76 - WSI_3
DOI: 10.1055/s-0030-1264207

Bioactive fatty acids and cerebrosides from the TCM drug Arisaema sp.

E Rozema 1, N Fakhrudin 1, A Atanasov 1, D Schuster 2, E Heiss 1, H Sonderegger 3, C Krieg 3, C Gruber 1, C Huck 3, V Dirsch 1, G Bonn 3, B Kopp 1
  • 1University of Vienna, Department of Pharmacognosy, Althanstrasse 14, 1090 Vienna, Austria
  • 2University of Innsbruck, Department of Pharmaceutical Chemistry, Innrain 52c, 6020 Innsbruck, Austria
  • 3University of Innsbruck, Institute of Analytical Chemistry and Radiochemistry, Innrain 52a, 6020 Innsbruck, Austria

In this study active compounds from the TCM drug Arisaema sp. [1] were characterized by bioassay-guided isolation. Extracts and fractions of Arisaema sp. were tested for agonistic activity towards peroxisome proliferator-activated receptor-α and -γ (PPAR) and for activation of the AMP-activated protein kinase (AMPK). These proteins are therapeutical targets in treatment of metabolic disorders [2,3].

An apolar fraction strongly activated PPAR-α and -γ and had positive effects on AMPK activity in vitro. Among the main compounds identified by GC-MS were n-hexadecanoic acid, 9,12-octadecadienoic acid, 9-octadecenoic acid, octadecanoic acid, 13-phenyltridecanoic acid and pentadecanoic acid. Since cerebrosides from Arisaema with antihepatotoxic activity reported by Jung et al [4], were found to bind PPAR-α and -γin silico, isolation and activity studies on these glycosphingolipids were continued. From a polar fraction, with moderate agonistic effect on PPAR-α and -γin vitro, cerebrosides I-VI were isolated. Their structures were elucidated by NMR, ESI-MS-MS and matrix free LDI-TOF-MS-MS. In conclusion, in the present activity and analytical studies chemical constituents of Arisaema sp. that showed in vitro activity on important anti-diabetic targets were revealed. These findings affirm the great value and rich source of Chinese herbal drugs for natural product research.

Acknowledgements: Sino-Austria Project, supported by the Austrian Federal Ministry of Science and Research and Federal Ministry of Health, Women and Youth. This project was also supported in part by the Austrian Science Fund [NFN S10704-B037] and the Austrian Federal Ministry for Science and Research [ACM-2009–01206].

References: 1. Bensky D. et al (2004) Chinese Herbal Medicine Materia Medica. Eastland Press. Seattle.

2. Kersten, S. et al (2000) Nature 405:421–424.

3. Winder W.W. et al (1999) Am. J. Physiol. Endocrinol. Metab. 277:1–10.

4. Jung, J.H. et al. (1996)J. Nat. Prod. 59:319–322.