Background <p>Antiplatelet therapy is crucial for preventing and treating cardio-cerebrovascular diseases. However, adverse events related to thrombosis or bleeding have been reported in instances of treatment with glycoprotein IIb/IIIa antagonists. It is anticipated that developing new selective platelet inhibitors with high anti-thrombotic efficiency and minimal hemorrhagic side effects is feasible. Qishen Yiqi Dripping Pill (QSYQ), an approved drug for ischemic heart disease, was studied for its anti-thrombotic effects.</p> Methods and results <p>Employing a microplate-based platelet aggregation assay, we systematically evaluated QSYQ and its medicinal components, chemical fractions, and compounds from the active fractions, identifying Salvianolic acid A (SAA) as one of the major active components for platelet inhibition. Our findings revealed that SAA decreased platelet [Ca<sup>2+</sup>]<sub>i</sub> via the G<sub>q</sub>/IP<sub>3</sub> pathway without affecting cAMP levels. Furthermore, 20&#xa0;mg/kg SAA reduced thrombus formation in a ferric chloride (FeCl<sub>3</sub>)-induced thrombotic model in vivo, suggesting the pharmacological significance of SAA in QSYQ.</p> Conclusion <p>This study identified SAA as one of the pharmacologically active anti-platelet components in QSYQ and revealed that its mechanism of action operates via the G<sub>q</sub>/IP<sub>3</sub> signaling pathway.</p> Graphical Abstract <p></p>

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Identification of salvianolic acid A as an ADP receptor-selective and Gq/IP3 pathway-mediated anti-platelet component in Qishen Yiqi

  • Wenli Dang,
  • Liping Chen,
  • Qinhua Shang,
  • Tiechan Zhao,
  • Lianying Chang,
  • Taiyi Wang,
  • Ming Lyu,
  • Xiaoxuan Tian,
  • Hao Guo,
  • Shuang He,
  • Jingyang Hu,
  • Peng Zhang,
  • Yan Zhu

摘要

Background

Antiplatelet therapy is crucial for preventing and treating cardio-cerebrovascular diseases. However, adverse events related to thrombosis or bleeding have been reported in instances of treatment with glycoprotein IIb/IIIa antagonists. It is anticipated that developing new selective platelet inhibitors with high anti-thrombotic efficiency and minimal hemorrhagic side effects is feasible. Qishen Yiqi Dripping Pill (QSYQ), an approved drug for ischemic heart disease, was studied for its anti-thrombotic effects.

Methods and results

Employing a microplate-based platelet aggregation assay, we systematically evaluated QSYQ and its medicinal components, chemical fractions, and compounds from the active fractions, identifying Salvianolic acid A (SAA) as one of the major active components for platelet inhibition. Our findings revealed that SAA decreased platelet [Ca2+]i via the Gq/IP3 pathway without affecting cAMP levels. Furthermore, 20 mg/kg SAA reduced thrombus formation in a ferric chloride (FeCl3)-induced thrombotic model in vivo, suggesting the pharmacological significance of SAA in QSYQ.

Conclusion

This study identified SAA as one of the pharmacologically active anti-platelet components in QSYQ and revealed that its mechanism of action operates via the Gq/IP3 signaling pathway.

Graphical Abstract