Arai, Masayoshi and Kawachi, Takashi and sato, hiroki and Setiawan, Andi and Kobayashi, Motomasa (2014) Marine spongian sesquiterpene phenols, dictyoceratin-C and smenospondiol, display hypoxia-selective growth inhibition against cancer cells. Bioorganic & Medicinal Chemistry Letters, 24 (14). pp. 3155-3157. ISSN 0960894X, 14643405

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Official URL: http://doi:10.1016/j.bmcl.2014.04.116


n the course of our search for hypoxia-selective growth inhibitors against cancer cells, a sesquiterpene phenol, dictyoceratin-C (1), was isolated from the Indonesian marine sponge of Dactylospongia elegans under the guidance of the constructed bioassay. Dictyoceratin-C (1) inhibited proliferation of human prostate cancer DU145 cells selectively under hypoxic condition in a dose-dependent manner at the concentrations ranging from 1.0 to 10 M. The subsequent structure-activity relationship study using nine sesquiterpene phenol/quinones (2-10), which were isolated from marine sponge, was executed. We found that smenospondiol (2) also exhibited the similar hypoxia-selective growth inhibitory activity against DU145 cells, and the para-hydroxybenzoyl ester moiety would be important for hypoxia-selective growth inhibitory activity of 1. In addition, the mechanistic analysis of dictyoceratin-C (1) revealed that the 10 M of 1 inhibited accumulation of Hypoxia-Inducible Factor-1 under hypoxic condition.

Item Type: Article
Subjects: Q Science > Q Science (General)
Divisions: Fakultas Matematika dan Ilmu Pengetahuan Alam (FMIPA) > Prodi Kimia
Depositing User: Prof Andi Setiawan
Date Deposited: 06 Jun 2021 14:34
Last Modified: 06 Jun 2021 14:34

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