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Artocarpesin acts on human platelet aggregation through inhibition of cyclic nucleotides and MAPKs
Applied Biological Chemistry ( IF 3.2 ) Pub Date : 2022-04-16 , DOI: 10.1186/s13765-022-00694-x
Hyuk-Woo Kwon 1 , Muhammad Irfan 2, 3 , Yuan Yee Lee 3, 4 , Man Hee Rhee 3, 4 , Jung-Hae Shin 3, 4
Affiliation  

The cardiovascular diseases (CVDs) are becoming a critical threat to our lives in these years. It is now widely accepted that platelets play an important role in cardiovascular disease as they have a fundamental role in thrombosis. Therefore, many drugs or natural substances have been developed to treat CVDs. Cudrania tricuspidata is a regional plant containing various constituents, such as xanthones, flavonoids, organic acids, and polysaccharides. It has been widely used in East Asia as an important ethnomedicine for the treatment of many diseases such as eczema, mumps, tuberculosis and acute arthritis. Therefore, we evaluated antiplatelet effects using artocarpesin isolated from C. tricuspidata. Confirmation of the antiplatelet function of artocarpesin was made according to the following analyzes. Artocarpesin inhibited collagen-induced human platelet aggregation, calcium mobilization, glycoprotein IIb/IIIa activation and thrombin-induced clot retraction through the regulation of associated signaling molecules. Artocarpesin increased the phosphorylation of vasodilator-stimulated phosphoprotein (VASP) and inositol 1, 4, 5-triphosphate receptor I (IP3RI). On the other hand, the phosphorylation of cytosolic phospholipase A2 (cPLA2), mitogen-activated protein kinases p38, JNK and phosphoinositide 3-kinase (PI3K)/Akt decreased. Thus, the study highlights that artocarpesin has an inhibitory effect on platelet activity and thrombus formation, showing its potential value in preventing platelet-induced cardiovascular disease.

中文翻译:

Artocarpesin 通过抑制环核苷酸和 MAPKs 作用于人血小板聚集

近年来,心血管疾病 (CVDs) 正在成为我们生活的严重威胁。现在人们普遍认为,血小板在心血管疾病中起重要作用,因为它们在血栓形成中起重要作用。因此,已经开发了许多药物或天然物质来治疗心血管疾病。柘木是一种区域性植物,含有多种成分,如黄酮、黄酮、有机酸和多糖。它作为一种重要的民族药在东亚被广泛使用,用于治疗湿疹、腮腺炎、肺结核和急性关节炎等多种疾病。因此,我们使用从 C. tricuspidata 中分离的 artocarpesin 评估了抗血小板作用。根据以下分析确认了artocarpesin的抗血小板功能。Artocarpesin 通过调节相关信号分子抑制胶原蛋白诱导的人血小板聚集、钙动员、糖蛋白 IIb/IIIa 活化和凝血酶诱导的凝块收缩。Artocarpesin 增加了血管扩张剂刺激的磷蛋白 (VASP) 和肌醇 1, 4, 5-三磷酸受体 I (IP3RI) 的磷酸化。另一方面,胞质磷脂酶 A2 (cPLA2)、丝裂原活化蛋白激酶 p38、JNK 和磷酸肌醇 3-激酶 (PI3K)/Akt 的磷酸化降低。因此,该研究强调,artocarpesin 对血小板活性和血栓形成具有抑制作用,显示其在预防血小板诱导的心血管疾病方面的潜在价值。通过调节相关信号分子,糖蛋白 IIb/IIIa 激活和凝血酶诱导的凝块收缩。Artocarpesin 增加了血管扩张剂刺激的磷蛋白 (VASP) 和肌醇 1, 4, 5-三磷酸受体 I (IP3RI) 的磷酸化。另一方面,胞质磷脂酶 A2 (cPLA2)、丝裂原活化蛋白激酶 p38、JNK 和磷酸肌醇 3-激酶 (PI3K)/Akt 的磷酸化降低。因此,该研究强调,artocarpesin 对血小板活性和血栓形成具有抑制作用,显示其在预防血小板诱导的心血管疾病方面的潜在价值。通过调节相关信号分子,糖蛋白 IIb/IIIa 激活和凝血酶诱导的凝块收缩。Artocarpesin 增加了血管扩张剂刺激的磷蛋白 (VASP) 和肌醇 1, 4, 5-三磷酸受体 I (IP3RI) 的磷酸化。另一方面,胞质磷脂酶 A2 (cPLA2)、丝裂原活化蛋白激酶 p38、JNK 和磷酸肌醇 3-激酶 (PI3K)/Akt 的磷酸化降低。因此,该研究强调,artocarpesin 对血小板活性和血栓形成具有抑制作用,显示其在预防血小板诱导的心血管疾病方面的潜在价值。胞质磷脂酶 A2 (cPLA2)、丝裂原活化蛋白激酶 p38、JNK 和磷酸肌醇 3-激酶 (PI3K)/Akt 的磷酸化降低。因此,该研究强调,artocarpesin 对血小板活性和血栓形成具有抑制作用,显示其在预防血小板诱导的心血管疾病方面的潜在价值。胞质磷脂酶 A2 (cPLA2)、丝裂原活化蛋白激酶 p38、JNK 和磷酸肌醇 3-激酶 (PI3K)/Akt 的磷酸化降低。因此,该研究强调,artocarpesin 对血小板活性和血栓形成具有抑制作用,显示其在预防血小板诱导的心血管疾病方面的潜在价值。
更新日期:2022-04-18
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