A new sterol sulfate, Sch 572423, from a marine sponge, Topsentia sp

• Published in: Bioorganic & medicinal chemistry letters Vol. 13; no. 10; pp. 1791 - 1794
• Main Authors: Yang, Shu-Wei, Buivich, Alexei, Chan, Tze-Ming, Smith, Michelle, Lachowicz, Jean, Pomponi, Shirley A, Wright, Amy E, Mierzwa, Ronald, Patel, Mahesh, Gullo, Vincent, Chu, Min
• Format: Journal Article
• Language: English
• Published: Oxford Elsevier Ltd 19-05-2003; Elsevier
• Subjects: Animals; Biological and medical sciences; General pharmacology; Medical sciences; Membrane Proteins - antagonists & inhibitors; Molecular Structure; Nuclear Magnetic Resonance, Biomolecular; Pharmacognosy. Homeopathy. Health food; Pharmacology. Drug treatments; Porifera - chemistry; Purinergic P2 Receptor Antagonists; Receptors, Purinergic P2Y12; Sterols - chemistry; Sterols - isolation & purification; Structure-Activity Relationship; Central America; America; West Indies; Bahamas; Steroid; P2Y12 purinergic receptor; Pharmacognosy; Saturated compound; Animal origin; Selectivity; In vitro; Biological activity; Marine environment; Porifera; Organic sulfate; Affinity; Isolation; Antagonist; Polyol; Invertebrata; Structural analysis; Sterol
• ISSN: 0960-894X; 1464-3405
• DOI: 10.1016/S0960-894X(03)00260-9

Bioassay-guided fractionation of an active fraction from a marine sponge
Topsentia sp. in our marine fraction library (MFL) led to the isolation and identification of halistanol sulfate (
1) and a new sterol sulfate Sch 572423 (
2). Compounds
1 and
2 were identified as P2Y
12 inhibitors with IC
50 of 0.48 and 2.2 μM, respectively. The general method of purification for the MFL library and the structure elucidation of compound
2 are described.
A new sterol sulfate, Sch 572423, discovered from
Topsentia sp. exhibited a P2Y
12 inhibition (IC
50 2.2 μM). Its structure was elucidated by spectroscopic data analyses.