Amakusamine from a Psammocinia sp. Sponge: Isolation, Synthesis, and SAR Study on the Inhibition of RANKL-Induced Formation of Multinuclear Osteoclasts
| Autor: | Hayato Ishikawa, Sachiko Tsukamoto, Tomoaki Inazumi, Yukihiko Sugimoto, Yuta Nakashima, Yuji Ise, Natsumi Inada, Yuka Maeyama, Yuki Hitora, Kazuhiko Maki, Shunya Murakami, Hikaru Kato |
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| Rok vydání: | 2021 |
| Předmět: |
Pharmacology
biology Stereochemistry Activator (genetics) Alkaloid Organic Chemistry Pharmaceutical Science Ligand (biochemistry) biology.organism_classification Methylenedioxy Analytical Chemistry chemistry.chemical_compound Sponge Complementary and alternative medicine chemistry RANKL Drug Discovery biology.protein Molecular Medicine Receptor IC50 |
| Zdroj: | Journal of Natural Products. 84:2738-2743 |
| ISSN: | 1520-6025 0163-3864 |
| DOI: | 10.1021/acs.jnatprod.1c00758 |
| Popis: | A simple methylenedioxy dibromoindole alkaloid, amakusamine (1), was isolated from a marine sponge of the genus Psammocinia, and its structure was determined from spectroscopic data, time-dependent density-functional theory calculations, and synthesis. Compound 1 inhibited the receptor activator of nuclear factor-κB ligand (RANKL)-induced formation of multinuclear osteoclasts with an IC50 value of 10.5 μM in RAW264 cells. The structure-activity relationship of 1 was also investigated with synthetic derivatives. |
| Databáze: | OpenAIRE |
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