A new lanostanoid ester glucoside, 3 alpha-acetoxy-5 alpha-lanosta-8,24-dien-21-oic acid ester beta-d-glucoside (1), and a known steroid, 2 beta,3 alpha,9 alpha-trihydroxy-5 alpha-ergosta-7,22-diene (2), were isolated from the fruit bodies of Ganoderma tsugae and their structures determined by spectroscopic methods. To study the cytotoxicity of 1 and 2, the changes of DNA content in human hepatocytes (Hep 3B) were studied. A sub-G1 cell stage was drastically increased after 24-h incubation with 1 (24 micrograms/mL). Compound 2 (100 micrograms/mL) inhibited the cell cycle progression of Hep 3B cells at the G2/M phase with an IC50 value of about 87.1 micrograms/mL. These results indicate that 1 causes cell death by apoptosis and 2 may possess the activity of cell cycle inhibition.
Various xanthones as well as quercetin have been shown to exhibit antiplatelet activity. A series of anthraquinones analogues structurally related to xanthones and a series of quercetin-related compounds were tested for their antiplatelet effects. Emodin, frangulin B, kaempferol tetraacetate, quercetin-3-O-galactoside octaacetate, rhamnazin triacetate, and rhamnetin tetraacetate were found to be potent antiplatelet agents, and 1,8-dihydroxy-6-methoxy-3-methylanthraquinone 8-O-rhamnosyl-(1-->2)-glucoside, rhamnustrioside undecaacetate, rutin decaacetate, and quercetin-3-O-(6-O-alpha-L-arabinopyranosyl)-beta-D-galactopyranos ide decaacetate showed significant antiplatelet effects. Quercetin showed vasorelaxing action in rat thoracic aorta.
In continuation of work on Solanum incanum a new steroidal alkaloid glycoside has been isolated from the fresh berries, which is named incanumine, and characterized as O(3)-[beta-D-xylopyranosyl-(1----3glu)-[beta-D-xylopyranosyl-(1--- -4rha)- alpha-L-rhamnopyranosyl-(1----4)]-beta-D-glucopyranosyl)-solasodine++ +. Solamargine, solasodine, ursolic acid, and ursolic acid derivatives (3-O-palmitoyl ursolic acid, 3-O-crotonyl ursolic acid, 3-O-propionyl ursolic acid) exhibited significant cytotoxic effects against human PLC/PRF/5 cells in vitro. Esterification of ursolic acid with aliphatic acids clearly enhanced the cytotoxic effects against human PLC/PRF/5 cells in vitro.
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