TY - JOUR
T1 - Antiplatelet effects of rhus verniciflua stokes heartwood and its active constituents -Fisetin, Butein, and Sulfuretin -In Rats
AU - Lee, Jun Hyeong
AU - Kim, Mikyung
AU - Chang, Kyung Hwa
AU - Hong, Cheol Yi
AU - Na, Chun Soo
AU - Dong, Mi Sook
AU - Lee, Dongho
AU - Lee, Moo Yeol
PY - 2015/1/1
Y1 - 2015/1/1
N2 - Rhus verniciflua stokes (RVS) is known to promote blood circulation by preventing blood stasis, although the active ingredients and the underlying mechanism are unclear. Platelets are the primary cells that regulate circulation and contribute to the development of diverse cardiovascular diseases by aggregation and thrombosis. The study assessed the antiplatelet activity of RVS and sought to identify the active constituents. Pretreatment of washed platelets with RVS heartwood extract blunted the aggregatory response of platelets to collagen. In the subfractions, fisetin, butein, and sulfuretin were identified as effective inhibitors of platelet aggregation by collagen, thrombin, and adenosine-5′-diphosphate. Antiplatelet activities of all three compounds were concentration dependent, and fisetin had longer in vitro duration of action compared with butein or sulfuretin. Extracellular signal-regulated kinase (ERK) mitogen-Activated protein kinase activation by collagen was prevented by fisetin, whereas butein and sulfuretin failed to inhibit ERK and p38 activation was not affected by any of the compounds. Rats orally administered 100mg/(kgday-1) fisetin for 7 days were resistant to arterial thrombosis, although total extract of RVS heartwood exhibited little effect at a dose of 1000mg/(kgday-1). RVS heartwood may have cardiovascular protective activity by inhibiting platelet aggregation. The active constituents are fisetin, butein, and sulfuretin, and fisetin is orally effective against thrombosis.
AB - Rhus verniciflua stokes (RVS) is known to promote blood circulation by preventing blood stasis, although the active ingredients and the underlying mechanism are unclear. Platelets are the primary cells that regulate circulation and contribute to the development of diverse cardiovascular diseases by aggregation and thrombosis. The study assessed the antiplatelet activity of RVS and sought to identify the active constituents. Pretreatment of washed platelets with RVS heartwood extract blunted the aggregatory response of platelets to collagen. In the subfractions, fisetin, butein, and sulfuretin were identified as effective inhibitors of platelet aggregation by collagen, thrombin, and adenosine-5′-diphosphate. Antiplatelet activities of all three compounds were concentration dependent, and fisetin had longer in vitro duration of action compared with butein or sulfuretin. Extracellular signal-regulated kinase (ERK) mitogen-Activated protein kinase activation by collagen was prevented by fisetin, whereas butein and sulfuretin failed to inhibit ERK and p38 activation was not affected by any of the compounds. Rats orally administered 100mg/(kgday-1) fisetin for 7 days were resistant to arterial thrombosis, although total extract of RVS heartwood exhibited little effect at a dose of 1000mg/(kgday-1). RVS heartwood may have cardiovascular protective activity by inhibiting platelet aggregation. The active constituents are fisetin, butein, and sulfuretin, and fisetin is orally effective against thrombosis.
KW - Rhus verniciflua stokes
KW - antiplatelet
KW - butein
KW - fisetin
KW - sulfuretin
UR - http://www.scopus.com/inward/record.url?scp=84920719836&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=84920719836&partnerID=8YFLogxK
U2 - 10.1089/jmf.2013.3116
DO - 10.1089/jmf.2013.3116
M3 - Article
C2 - 25372471
AN - SCOPUS:84920719836
VL - 18
SP - 21
EP - 30
JO - Journal of Medicinal Food
JF - Journal of Medicinal Food
SN - 1096-620X
IS - 1
ER -