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Hokkaido University Collection of Scholarly and Academic Papers >
Graduate School of Environmental Science / Faculty of Environmental Earth Science >
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Effective Synthesis and Antifouling Activity of Dolastatin 16 Derivatives
| Title: | Effective Synthesis and Antifouling Activity of Dolastatin 16 Derivatives |
| Authors: | Casalme, Loida O. Browse this author | | Katayama, Keisuke Browse this author | | Hayakawa, Yoshiki Browse this author | | Nakamura, Kensuke Browse this author | | Yamauchi, Arisa Browse this author | | Nogata, Yasuyuki Browse this author →KAKEN DB | | Yoshimura, Erina Browse this author | | Matsuda, Fuyuhiko Browse this author →KAKEN DB | | Umezawa, Taiki Browse this author →KAKEN DB |
| Keywords: | natural product | | antifouling | | dolastatin 16 | | peptide | | Amphibalanus amphitrite |
| Issue Date: | Feb-2022 |
| Publisher: | MDPI |
| Journal Title: | Marine Drugs |
| Volume: | 20 |
| Issue: | 2 |
| Start Page: | 124 |
| Publisher DOI: | 10.3390/md20020124 |
| Abstract: | Some derivatives of dolastatin 16, a depsipeptide natural product first obtained from the sea hare Dolabella auricularia, were synthesized through second-generation synthesis of two unusual amino acids, dolaphenvaline and dolamethylleuine. The second-generation synthesis enabled derivatizations such as functionalization of the aromatic ring in dolaphenvaline. The derivatives of fragments and whole structures were evaluated for antifouling activity against the cypris larvae of Amphibalanus amphitrite. Small fragments inhibited the settlement of the cypris larvae at potent to moderate concentrations (EC50 = 0.60-4.62 mu g/mL), although dolastatin 16 with a substituent on the aromatic ring (24) was much less potent than dolastatin 16. |
| Type: | article |
| URI: | http://hdl.handle.net/2115/85339 |
| Appears in Collections: | 環境科学院・地球環境科学研究院 (Graduate School of Environmental Science / Faculty of Environmental Earth Science) > 雑誌発表論文等 (Peer-reviewed Journal Articles, etc)
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