Spartinoxide, a New Enantiomer of A82775C with Inhibitory Activity Toward HLE from the Marine-derived Fungus Phaeosphaeria spartinae

作者：Elsebai Mahmoud Fahmi; Kehraus Stefan; Guetschow Michael; Koenig Gabriele M

来源：Natural Product Communications, 2010, 5(7): 1071-1076.

DOI：10.1177/1934578x1000500718

• Spartinoxide
• Phaeosphaeria spartinae
• natural product
• HMBA
• anofinic acid
• human leukocyte elastase (HLE)

The fungus Phaeosphaeria spartinae is an endophyte or the marine alga Ceramium sp. Investigation of this marine-derived fungus led to the isolation of spartinoxide (1), which is the enantiomer of the known compound A82775C (2). Additionally, the known metabolites 4-hydroxy-3-prenyl-benzoic acid (4) and anofinic acid (5) were obtained. The structures of all compounds were established from extensive spectroscopic investigations. Compounds 1, 4 and 5 were assayed against the enzymes human leukocyte elastase (HLE), trypsin, acetylcholinesterase and cholesterolesterase. Compounds 1 and 4 showed potent inhibition of HLE with IC(50) values of 1.71 +/- 0.30 mu g/mL (6.5 mu M) and 1.67 +/- 0.32 mu g/mL (8.1 mu M), respectively.

• 出版日期2010-7