A new inhibitor of synovial phospholipase A2 from fermentations of Penicillium sp. 62-92.
Penidiamide, a new tripetide containing dehydrotryptamine, glycine and anthranilic acid linked together by two amide bonds, and oxindole were isolated from submerged cultures of Penicillium sp. 62-92. Both compounds preferentially inhibited human synovial phospholipase A2, penidiamide with an IC50 of 30 microM and oxindole of 380 microM. With the exception of U 937 cells (leukemia, human), no cytotoxic activities were detected against HL-60- (leukemia, human), HeLa S3- (epitheloid carcinoma, human), BHK 21- (kidney fibroblasts, hamster), and L1210-cells (leukemia, mouse). No antimicrobial activity was detected for oxindole, and only weak antibacterial activity for penidiamide. The structure of penidiamide was elucidated by spectroscopic methods.
Witter
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L
Lehrbereich Biotechnologie, Universität Kaiserslautern, Germany.
Anke
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T
Sterner
O
O
D000818:Animals; D002460:Cell Line; D006224:Cricetinae; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D005285:Fermentation; D005998:Glycine / Q000031:analogs & derivatives* / Q000096:biosynthesis / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D006367:HeLa Cells; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D051379:Mice; D010407:Penicillium / Q000378:metabolism*; D010741:Phospholipases A / Q000037:antagonists & inhibitors*; D054467:Phospholipases A2; D011994:Recombinant Proteins / Q000037:antagonists & inhibitors; D013583:Synovial Membrane / Q000201:enzymology*; D062367:ortho-Aminobenzoates / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
D004791:Enzyme Inhibitors; D011994:Recombinant Proteins; D062367:ortho-Aminobenzoates; C111412:penidiamide; D010741:Phospholipases A; D054467:Phospholipases A2; D005998:Glycine