Bioactive fatty acids and cerebrosides from the TCM drug Arisaema sp

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 prot...

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Published inPlanta Medica
Main Authors Rozema, E, Fakhrudin, N, Atanasov, A, Schuster, D, Heiss, E, Sonderegger, H, Krieg, C, Gruber, C, Huck, C, Dirsch, V, Bonn, G, Kopp, B
Format Conference Proceeding
LanguageEnglish
Published 24.08.2010
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Summary: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 -γ in silico , isolation and activity studies on these glycosphingolipids were continued. From a polar fraction, with moderate agonistic effect on PPAR-α and -γ in 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.
ISSN:0032-0943
1439-0221
DOI:10.1055/s-0030-1264207