Enantioselective inhibitory abilities of enantiomers of notoamides against RANKL-induced formation of multinuclear osteoclasts
| Autor: | Sunderhaus, James D., McAfoos, Timothy J., Finefield, Jennifer M., Williams, Robert M., Hikaru, Kato, Aika, Kai, Tetsuro, Kawabata, ames D. , SunderhausJ, Timothy J. , McAfoos, Jennifer M. , Finefield, Yukihiko, Sugimoto, Robert M. , Williams, Sachiko, Tsukamoto |
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| Jazyk: | angličtina |
| Rok vydání: | 2017 |
| Předmět: |
Osteoclastogenesis
Stereochemistry Clinical Biochemistry Osteoclasts Pharmaceutical Science 010402 general chemistry 01 natural sciences Biochemistry Indole Alkaloids Notoamide 474.73 Inhibitory Concentration 50 Mice Prenylation 499.3 Drug Discovery Animals Receptor Molecular Biology IC50 Indole test Fungus biology Enantiomer 010405 organic chemistry Chemistry Activator (genetics) RANK Ligand Organic Chemistry Fungi Cell Differentiation Stereoisomerism Ligand (biochemistry) 0104 chemical sciences RAW 264.7 Cells Aspergillus RANKL biology.protein Molecular Medicine |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 27(22):4975-4978 |
| ISSN: | 0960-894X |
| Popis: | The marine-derived Aspergillus protuberus MF297-2 and the terrestrial A. amoenus NRRL 35600 produce enantiomeric prenylated indole alkaloids. Investigation of biological activities of the natural and synthetic derivatives revealed that (−)-enantiomers of notoamides A and B, 6-epi-notoamide T, and stephacidin A inhibited receptor activator of nuclear factor-κB (NF-κB) ligand (RANKL)–induced osteoclastogenic differentiation of murine RAW264 cells more strongly than their respective (+)-enantiomers. Among them, (−)-6-epi-notoamide T was the most potent inhibitor with an IC50 value of 1.7 μM. |
| Databáze: | OpenAIRE |
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