Synthesis of huaicarbon A/B and their activating effects on platelet glycoprotein VI receptor to mediate collagen-induced platelet aggregation.
Quercetin and rhamnose were efficiently converted into huaicarbon A/B by heating at 250°C for 10-15 min or at 200°C for 25-30 min. With the optimum molar ratio of quercetin/rhamnose (1:3), huaicarbon A and B yields reached 25% and 16% respectively after heating at 250°C, with 55% quercetin conversion. Huaicarbon A/B both promoted washed platelet aggregation dose-dependently, which was antagonized by an inhibitor of glycoprotein VI (GPVI) receptor. Similarly, they both promoted collagen-induced platelet aggregation in platelet-rich plasma in dose-dependent manners. According to the S type dose-response model, EC50values of huaicarbon A and huaicarbon B were calculated as 33.48 μM and 48.73 μM respectively. They induced intracellular Ca2+accumulation that was specifically blocked by GPVI antagonist. Huaicarbon A/B enhanced intracellular Ca2+accumulation and facilitated collagen-induced platelet aggregation, which were blocked by GPVI antagonist. They were conducive to collagen-induced platelet aggregation by activating platelet GPVI receptor.
School of Pharmacy, Nanjing University of Chinese MedicineNanjing 210023, P. R. China; Jiangsu Key Laboratory of Chinese Medicine Processing, Nanjing University of Chinese MedicineNanjing 210023, P. R. China; Engineering Center of State Ministry of Education for Standardization of Chinese Medicine ProcessingNanjing 210023, P. R. China.
Hongli
H
Yu
School of Pharmacy, Nanjing University of Chinese Medicine Nanjing 210023, P. R. China.
Yeqing
Y
Chen
School of Pharmacy, Nanjing University of Chinese MedicineNanjing 210023, P. R. China; Jiangsu Key Laboratory of Chinese Medicine Processing, Nanjing University of Chinese MedicineNanjing 210023, P. R. China; Engineering Center of State Ministry of Education for Standardization of Chinese Medicine ProcessingNanjing 210023, P. R. China.
Hao
H
Wu
School of Pharmacy, Nanjing University of Chinese Medicine Nanjing 210023, P. R. China.
Kuilong
K
Wang
School of Pharmacy, Nanjing University of Chinese Medicine Nanjing 210023, P. R. China.
Liping
L
Liu
School of Pharmacy, Nanjing University of Chinese Medicine Nanjing 210023, P. R. China.
Xingde
X
Zhang
Heating reaction; huaicarbon A/B; quercetin; rhamnose