76652-99-8Relevant academic research and scientific papers
A polybromodiphenyl ether from an Indonesian marine sponge Lamellodysidea herbacea and its chemical derivatives inhibit protein tyrosine phosphatase 1B, an important target for diabetes treatment
Yamazaki, Hiroyuki,Sumilat, Deiske A.,Kanno, Syu-Ichi,Ukai, Kazuyo,Rotinsulu, Henki,Wewengkang, Defny S.,Ishikawa, Masaaki,Mangindaan, Remy E. P.,Namikoshi, Michio
, p. 730 - 735 (2013/09/24)
The ethanol extract of an Indonesian marine sponge Lamellodysidea herbacea inhibited the activity of protein tyrosine phosphatase 1B (PTP1B), an important target enzyme for the treatment of type II diabetes. Bioassay-guided isolation yielded a known polybromodiphenyl ether (1) as a sole bioactive component. The structure of 1 was confirmed by spectroscopic data for 1 and its methyl ether derivative (2). Compound 1 markedly inhibited the PTP1B activity (IC 50 = 0.85 μM) and showed a moderate cytotoxicity against two human cancer cell lines, HCT-15 (colon) and Jurkat (T-cell lymphoma) cells. On the other hand, compound 2 maintained potent inhibitory activity against PTP1B (IC50 = 1.7 μM) but did not show apparent cytotoxicity at 18 μM against these cancer cells. Four ester derivatives [acetyl (3), butyryl (4), hexanoyl (5), and benzoyl (6)] were prepared from 1 and their activities evaluated against PTP1B and two cancer cell lines to investigate the structure-activity relationships. Although compounds 3-6 exhibited potent inhibitory effects against PTP1B activity, cytotoxicity against HCT-15 and Jurkat cells was observed as a similar efficacy to that of 1. From these results, compound 2 was found to be the best inhibitor of PTP1B with no apparent cytotoxicity. Therefore, 2 may be a lead compound for making a new type of PTP1B inhibitor. Moreover, compound 2 did not inhibit the cell growth of Huh-7 cells (hepatoma). Hepatocytes are one of the locations of PTP1B, and Huh-7 cells are used to study the mechanism of action of compound 2.
Antibacterial compounds and uses thereof
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Page/Page column 9-10, (2008/06/13)
The invention relates to antibacterial compounds and their use to treat bacterial infections. More particularly, the invention relates to substituted biphenyl compounds having antibacterial activity. The invention provides methods for treating bacterial infections using PBDEs that have not previously been used to treat bacterial infections. The invention further provides novel PBDEs that are useful in such methods.
