4.3 Article

Isolation of Salsolinol, a Tetrahydroisoquinoline Alkaloid, from the Marine Sponge Xestospongia cf. vansoesti as a Proteasome Inhibitor

Journal

CHEMICAL & PHARMACEUTICAL BULLETIN
Volume 59, Issue 2, Pages 287-290

Publisher

PHARMACEUTICAL SOC JAPAN
DOI: 10.1248/cpb.59.287

Keywords

tetrahydroisoquinoline alkaloid; proteasome; chymotrypsin-like activity; marine sponge

Funding

  1. Ministry of Education, Culture, Sports, Science and Technology of Japan [18032033, 19310140]
  2. Naito Foundation
  3. Astellas Foundation for Research on Metabolic Disorders
  4. Grants-in-Aid for Scientific Research [19310140, 18032033] Funding Source: KAKEN

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Salsolinol (1), a tetrahydroisoquinoline alkaloid, was isolated from the marine sponge Xestospongia cf. vansoesti collected in Indonesia as a proteasome inhibitor, along with three salsolinol derivatives, norsalsolinol (2), cis-4-hydroxysalsolinol (3), and trans-4-hydroxysalsolinol (4). Compounds 1 and 2 inhibited the chymotrypsin-like activity of the proteasome with IC50 values of 50 and 32 mu g/ml, respectively, but 3 and 4 showed no inhibitory effect even at 100 mu g/ml.

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