Abstract
Sanguinarine is a plant alkaloid present in the root of Sanguinaria canadensis and Poppy fumaria species. Sanguinarine has been used as an antiseptic mouth rinse and a toothpaste additive to reduce dental plaque and gingival inflammation. In this study, we investigated the antiplatelet effects of sanguinarine, aiming to extend its potential pharmacological applications. Sanguinarine inhibited platelet aggregation induced by arachidonic acid (AA), collagen, U46619 and sub-threshold concentration of thrombin (0.05 U/ml) with IC 50 concentrations of 8.3, 7.7, 8.6 and 4.4 μM, respectively. Sanguinarine (5-10 μM) inhibited 10-31% of platelet TXB 2 production, but not platelet aggregation induced by higher concentration of thrombin (0.1 U/ml). SQ29548, a thromboxane receptor antagonist, inhibited the AA-induced platelet aggregation but not TXB 2 production. Sanguinarine suppressed cyclooxygenase-1 (COX-1) activity (IC 50 = 28 μM), whereas its effect on COX-2 activity was minimal. Sanguinarine (8, 10 μM) further inhibited the AA-induced Ca 2+ mobilization by 27-62%. In addition, SQ22536, an adenylate cyclase inhibitor, attenuated the inhibitory effect of sanguinarine toward AA-induced platelet Ca 2+ mobilization and aggregation. These results suggest that sanguinarine is a potent antiplatelet agent, which activates adenylate cyclase, inhibits platelet Ca 2+ mobilization, TXB 2 production as well as suppresses COX-1 enzyme activity. Sanguinarine may have therapeutic potential for treatment of cardiovascular diseases related to platelet aggregation.
| Original language | English |
|---|---|
| Pages (from-to) | 250-258 |
| Number of pages | 9 |
| Journal | Atherosclerosis |
| Volume | 191 |
| Issue number | 2 |
| DOIs | |
| Publication status | Published - 2007 Apr 1 |
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All Science Journal Classification (ASJC) codes
- Cardiology and Cardiovascular Medicine
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Antiplatelet effect of sanguinarine is correlated to calcium mobilization, thromboxane and cAMP production. / Jeng, Jiiang Huei; Wu, Hui Lin; Lin, Bor Ru; Lan, Wan Hong; Chang, Hsiao Hwa; Ho, Yuan Soon; Lee, Po Hsuen; Wang, Ying-Jan; Wang, Juo Song; Chen, Yi Jane; Chang, Mei Chi.
In: Atherosclerosis, Vol. 191, No. 2, 01.04.2007, p. 250-258.Research output: Contribution to journal › Article
TY - JOUR
T1 - Antiplatelet effect of sanguinarine is correlated to calcium mobilization, thromboxane and cAMP production
AU - Jeng, Jiiang Huei
AU - Wu, Hui Lin
AU - Lin, Bor Ru
AU - Lan, Wan Hong
AU - Chang, Hsiao Hwa
AU - Ho, Yuan Soon
AU - Lee, Po Hsuen
AU - Wang, Ying-Jan
AU - Wang, Juo Song
AU - Chen, Yi Jane
AU - Chang, Mei Chi
PY - 2007/4/1
Y1 - 2007/4/1
N2 - Sanguinarine is a plant alkaloid present in the root of Sanguinaria canadensis and Poppy fumaria species. Sanguinarine has been used as an antiseptic mouth rinse and a toothpaste additive to reduce dental plaque and gingival inflammation. In this study, we investigated the antiplatelet effects of sanguinarine, aiming to extend its potential pharmacological applications. Sanguinarine inhibited platelet aggregation induced by arachidonic acid (AA), collagen, U46619 and sub-threshold concentration of thrombin (0.05 U/ml) with IC 50 concentrations of 8.3, 7.7, 8.6 and 4.4 μM, respectively. Sanguinarine (5-10 μM) inhibited 10-31% of platelet TXB 2 production, but not platelet aggregation induced by higher concentration of thrombin (0.1 U/ml). SQ29548, a thromboxane receptor antagonist, inhibited the AA-induced platelet aggregation but not TXB 2 production. Sanguinarine suppressed cyclooxygenase-1 (COX-1) activity (IC 50 = 28 μM), whereas its effect on COX-2 activity was minimal. Sanguinarine (8, 10 μM) further inhibited the AA-induced Ca 2+ mobilization by 27-62%. In addition, SQ22536, an adenylate cyclase inhibitor, attenuated the inhibitory effect of sanguinarine toward AA-induced platelet Ca 2+ mobilization and aggregation. These results suggest that sanguinarine is a potent antiplatelet agent, which activates adenylate cyclase, inhibits platelet Ca 2+ mobilization, TXB 2 production as well as suppresses COX-1 enzyme activity. Sanguinarine may have therapeutic potential for treatment of cardiovascular diseases related to platelet aggregation.
AB - Sanguinarine is a plant alkaloid present in the root of Sanguinaria canadensis and Poppy fumaria species. Sanguinarine has been used as an antiseptic mouth rinse and a toothpaste additive to reduce dental plaque and gingival inflammation. In this study, we investigated the antiplatelet effects of sanguinarine, aiming to extend its potential pharmacological applications. Sanguinarine inhibited platelet aggregation induced by arachidonic acid (AA), collagen, U46619 and sub-threshold concentration of thrombin (0.05 U/ml) with IC 50 concentrations of 8.3, 7.7, 8.6 and 4.4 μM, respectively. Sanguinarine (5-10 μM) inhibited 10-31% of platelet TXB 2 production, but not platelet aggregation induced by higher concentration of thrombin (0.1 U/ml). SQ29548, a thromboxane receptor antagonist, inhibited the AA-induced platelet aggregation but not TXB 2 production. Sanguinarine suppressed cyclooxygenase-1 (COX-1) activity (IC 50 = 28 μM), whereas its effect on COX-2 activity was minimal. Sanguinarine (8, 10 μM) further inhibited the AA-induced Ca 2+ mobilization by 27-62%. In addition, SQ22536, an adenylate cyclase inhibitor, attenuated the inhibitory effect of sanguinarine toward AA-induced platelet Ca 2+ mobilization and aggregation. These results suggest that sanguinarine is a potent antiplatelet agent, which activates adenylate cyclase, inhibits platelet Ca 2+ mobilization, TXB 2 production as well as suppresses COX-1 enzyme activity. Sanguinarine may have therapeutic potential for treatment of cardiovascular diseases related to platelet aggregation.
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UR - http://www.scopus.com/inward/citedby.url?scp=33947198685&partnerID=8YFLogxK
U2 - 10.1016/j.atherosclerosis.2006.05.023
DO - 10.1016/j.atherosclerosis.2006.05.023
M3 - Article
VL - 191
SP - 250
EP - 258
JO - Atherosclerosis
JF - Atherosclerosis
SN - 0021-9150
IS - 2
ER -