Abstract
The present study was aimed at discovering novel biologically active compounds based on the skeletons of gingerol and shogaol, the pungent principles from the rhizomes of Zingiber officinale. Therefore, eight groups of analogues were synthesized and examined for their inhibitory activities of platelet aggregation induced by arachidonic acid, collagen, platelet activating factor, and thrombin. Among the tested compounds, [6]-paradol (5b) exhibited the most significant anti-platelet aggregation activity. It was the most potent candidate, which could be used in further investigation to explore new drug leads.
Highlights
Ginger (Chinese name: Shengjiang), derived from the rhizomes of Zingiber officinale Roscoe, is a well-known spice and is most frequently prescribed as a traditional Chinese medicine for its stomachic, antiemetic, antidiarrheal, expectorant, antiasthmatic, hemostatic and cardiologic properties for the treatment of several gastrointestinal and respiratory diseases [1,2,3]
Eight groups of derivatives based on the skeletons of shogaol and gingerol, the active pungent principles from ginger, were synthesized and evaluated for their antiplatelet bioactivity
Among the compounds synthesized, [6]-paradol 5b displayed the most significant inhibition of platelet aggregation induced by arachidonic acid (AA)
Summary
Ginger (Chinese name: Shengjiang), derived from the rhizomes of Zingiber officinale Roscoe, is a well-known spice and is most frequently prescribed as a traditional Chinese medicine for its stomachic, antiemetic, antidiarrheal, expectorant, antiasthmatic, hemostatic and cardiologic properties for the treatment of several gastrointestinal and respiratory diseases [1,2,3]. The pungent principles reported from the rhizomes of Zingiber officinale include: zingerone, gingerols, gingerdiols, gingerdiones, and shogaols (Figure 1). In the course of our continuing research program aimed at discovering novel bioactive constituents from natural sources, thrombolytic and vasoactive activity examinations were carried out, and the ether extracts of the rhizomes of Z. officinale were found to exhibit significant anti-platelet aggregation activity and vasorelaxing effects. In our previous article [20], twenty-nine compounds were identified, and [6]-gingerol and [6]-shogaol exhibited potent anti-platelet aggregation bioactivity. These results initiated our interest in searching for more potent antiplatelet aggregation agents from the analogues of gingerol and shogaol. In the present study eight groups of compounds (Figure 2) were prepared and subjected to examinations of their anti-platelet aggregation activity
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