Journal
MARINE DRUGS
Volume 18, Issue 1, Pages -Publisher
MDPI
DOI: 10.3390/md18010039
Keywords
proteasome inhibition; dolabellane; secosteroids; soft coral
Categories
Funding
- Ministry of Science and Technology, Taiwan, Republic of China [MOST108-2320-B110-005]
- Kaohsiung Medical University [NSYSU-KMU 108-P018]
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We performed a high-content screening (HCS) assay aiming to discover bioactive molecules with proteasome inhibitory activity. By structural elucidation, we identified six compounds purified from soft coral Clavularia flava, which potentiates proteasome inhibition. Chemical structure elucidation revealed they are dolabellane- and secosteroid-based compounds including a new dolabellane, clavinflol C (1), three known dolabellanes, stolonidiol (2), stolonidiol-17-acetate (3), and clavinflol B (4) as well as two new secosteroids, 3 beta,11-dihydroxy-24-methyl-9,11-secocholest-5-en-9,23-dione (5) and 3 beta,11-dihydroxy-24-methylene-9,11-secocholest-5-en-9,23-dione (6). All six compounds show less cytotoxicity than those of known proteasome inhibitors, bortezomib and MG132. In summary, the high-content measurements of control inhibitors, bortezomib and MG132, manifest the highest ratio >2 in high-content measurement. Of the isolated compounds, 2 and 5 showed higher activity, followed by 3 and 6, and then 1 and 4 exhibited moderate inhibition.
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