Novel inhibitory actions on platelet thromboxane and inositolphosphate formation by xanthones and their glycosides.
Xanthones and their glycosides were tested for their antiplatelet activities in washed rabbit platelets. Tripteroside acetate and norathyriol acetate were the most potent inhibitors. Tripteroside acetate inhibited platelet aggregation and ATP release induced by ADP, arachidonic acid, platelet-activating factor (PAF), collagen, ionophore A23187 and thrombin. The IC50 values of tripteroside acetate toward arachidonic acid- (100 microM) and collagen- (10 micrograms/ml) induced platelet aggregation were 10 and 30 micrograms/ml respectively. It inhibited thromboxane B2 formation of washed platelets caused by arachidonic acid, collagen, thrombin and ionophore A23187 and also that caused by the incubation of lysed platelet homogenate with arachidonic acid. Tripteroside acetate decreased the formation of inositolphosphate caused by thrombin, collagen and PAF, whereas it had no direct effect on fibrinogen-platelet interaction. It is concluded that xanthone derivatives inhibited platelet aggregation and release reaction by diminishing thromboxane formation and phosphoinositide breakdown.
Teng
C M
CM
Pharmacological Institute, College of Medicine, National Taiwan University, Taipei, Republic of China.
Lin
C N
CN
Ko
F N
FN
Cheng
K L
KL
Huang
T F
TF
D000244:Adenosine Diphosphate / Q000494:pharmacology; D000255:Adenosine Triphosphate / Q000378:metabolism; D000818:Animals; D016718:Arachidonic Acid; D001095:Arachidonic Acids / Q000494:pharmacology; D001792:Blood Platelets / Q000187:drug effects / Q000378:metabolism*; D000001:Calcimycin / Q000494:pharmacology; D003094:Collagen / Q000494:pharmacology; D006027:Glycosides / Q000494:pharmacology*; D007295:Inositol Phosphates / Q000378:metabolism*; D010974:Platelet Aggregation / Q000187:drug effects*; D010975:Platelet Aggregation Inhibitors; D011817:Rabbits; D013329:Structure-Activity Relationship; D013917:Thrombin / Q000494:pharmacology; D013931:Thromboxanes / Q000378:metabolism*; D014966:Xanthenes / Q000494:pharmacology*; D044004:Xanthones
D001095:Arachidonic Acids; D006027:Glycosides; D007295:Inositol Phosphates; D010975:Platelet Aggregation Inhibitors; D013931:Thromboxanes; D014966:Xanthenes; D044004:Xanthones; D016718:Arachidonic Acid; D000001:Calcimycin; D000244:Adenosine Diphosphate; D000255:Adenosine Triphosphate; D003094:Collagen; C009689:xanthone; D013917:Thrombin