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Based on the pharmacological experiments, the xanthonoids related to the constitutents of Gentianaceous plants , such as tripteroside peracetate and northyriol peracetate exhibited potent effect on platelet aggregation. In our laboratory, we synthesized a series of xanthone analogues for study the pharmacological tests and found that 3-hydroxyxanthone, 2,3-dihydroxyxanthone diacetate, 3,4-dihydroxyxanthone and 3,4-dihydroxyxanthone diacetate showed potent inhibition of platelet aggregation induced by arachidonic acid and collagen, respectively. Recently we synthesized monooxygenated, dioxygenated xanthones and their derivatives with different substituted partern for study the antiplatelet effect. The result showed 1,7-dihydroxyxanthone and 2,5-dihydroxyxanthone exhibited significant inhibition of platelet aggregation induced by arachidonic acid and collagen respectively. Acetylation of 2-hydroxyxanthone and 2,5-dihydroxyxanthone enhanced antiplatelet effects on platelet aggregation induced by arachidonic acid.
In anti-tumor activity, the xanthones also showed potent activity. Therefore, We further synthesized various epoxypropoxyxanthones, analogues of psorospermin and screened on PLC/PRF/5 cells and KB cells, respectively. The result indicated that the xanthones such as 2,6-di(2,3-epoxypropoxy) xanthone (ED50=0.23μg/ml (PLC/PRF/5 cell) ; ED50=0.0043μg/ml (KB cell)) , 3,5-di(2,3-epoxypropoxy) xanthone (ED50=0.066 μg/ml (PLC/PRF/5 cell) ; ED50=0.0049 μg/ml (KB cell)) and 3,6-di(2,3-epoxypropoxy) xanthone (ED50=0.24μg/ml (PLC/PRF/5 cell) ; ED50=0.11 μg/ml (KB cell)) with epoxide group exhibited significant anti-tumor activity .
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