Abstract
Sphingomyelinase is considered to be involved in the regulation of apoptosis and cell growth. In the course of our screening for acidic sphingomyelinase inhibitors we isolated three xanthone compounds, α-mangostin, cowanin, and cowanol, from the bark of Garcinia speciosa. These compounds competitively inhibited bovine brain-derived acidic sphingomyelinase with IC50 values of 14.1, 19.2, and 10.9 μM, respectively and inhibited the acidic sphingomyelinase more effectively than the neutral sphingomyelinase of bovine brain. α-Mangostin inhibited the acidic sphingomyelinase in the most selective manner. α-Mangostin was chemically modified and its structure-activity relationships are discussed.