Xanthohumol, a prenylated flavonoid from hops (Humulus lupulus), prevents platelet activation in human platelets

Ye Ming Lee, Kuo Hsien Hsieh, Wan-Jung Lu, Hsiu Chu Chou, Duen Suey Chou, Li Ming Lien, Joen Rong Sheu, Kuan Hung Lin

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20 Citations (Scopus)

Abstract

Xanthohumol is the principal prenylated flavonoid in the hop plant (Humulus lupulus L.). Xanthohumol was found to be a very potent cancer chemopreventive agent through regulation of diverse mechanisms. However, no data are available concerning the effects of xanthohumol on platelet activation. The aim of this paper was to examine the antiplatelet effect of xanthohumol in washed human platelets. In the present paper, xanthohumol exhibited more-potent activity in inhibiting platelet aggregation stimulated by collagen. Xanthohumol inhibited platelet activation accompanied by relative [Ca+] i mobilization, thromboxane A2 formation, hydroxyl radical (OH()) formation, and phospholipase C (PLC)2, protein kinase C (PKC), mitogen-activated protein kinase (MAPK), and Akt phosphorylation. Neither SQ22536, an inhibitor of adenylate cyclase, nor ODQ, an inhibitor of guanylate cyclase, reversed the xanthohumol-mediated inhibitory effect on platelet aggregation. Furthermore, xanthohumol did not significantly increase nitrate formation in platelets. This study demonstrates for the first time that xanthohumol possesses potent antiplatelet activity which may initially inhibit the PI3-kinase/Akt, p38 MAPK, and PLC2-PKC cascades, followed by inhibition of the thromboxane A2 formation, thereby leading to inhibition of [Ca+] i and finally inhibition of platelet aggregation. Therefore, this novel role of xanthohumol may represent a high therapeutic potential for treatment or prevention of cardiovascular diseases.

Original languageEnglish
Article number852362
JournalEvidence-based Complementary and Alternative Medicine
Volume2012
DOIs
Publication statusPublished - 2012

Fingerprint

Humulus
Platelet Activation
Flavonoids
Blood Platelets
Platelet Aggregation
Thromboxane A2
Protein Kinase C
xanthohumol
Guanylate Cyclase
Type C Phospholipases
p38 Mitogen-Activated Protein Kinases
Mitogen-Activated Protein Kinases
Phosphatidylinositol 3-Kinases
Hydroxyl Radical
Nitrates
Cardiovascular Diseases
Collagen
Phosphorylation

ASJC Scopus subject areas

  • Complementary and alternative medicine

Cite this

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title = "Xanthohumol, a prenylated flavonoid from hops (Humulus lupulus), prevents platelet activation in human platelets",
abstract = "Xanthohumol is the principal prenylated flavonoid in the hop plant (Humulus lupulus L.). Xanthohumol was found to be a very potent cancer chemopreventive agent through regulation of diverse mechanisms. However, no data are available concerning the effects of xanthohumol on platelet activation. The aim of this paper was to examine the antiplatelet effect of xanthohumol in washed human platelets. In the present paper, xanthohumol exhibited more-potent activity in inhibiting platelet aggregation stimulated by collagen. Xanthohumol inhibited platelet activation accompanied by relative [Ca+] i mobilization, thromboxane A2 formation, hydroxyl radical (OH()) formation, and phospholipase C (PLC)2, protein kinase C (PKC), mitogen-activated protein kinase (MAPK), and Akt phosphorylation. Neither SQ22536, an inhibitor of adenylate cyclase, nor ODQ, an inhibitor of guanylate cyclase, reversed the xanthohumol-mediated inhibitory effect on platelet aggregation. Furthermore, xanthohumol did not significantly increase nitrate formation in platelets. This study demonstrates for the first time that xanthohumol possesses potent antiplatelet activity which may initially inhibit the PI3-kinase/Akt, p38 MAPK, and PLC2-PKC cascades, followed by inhibition of the thromboxane A2 formation, thereby leading to inhibition of [Ca+] i and finally inhibition of platelet aggregation. Therefore, this novel role of xanthohumol may represent a high therapeutic potential for treatment or prevention of cardiovascular diseases.",
author = "Lee, {Ye Ming} and Hsieh, {Kuo Hsien} and Wan-Jung Lu and Chou, {Hsiu Chu} and Chou, {Duen Suey} and Lien, {Li Ming} and Sheu, {Joen Rong} and Lin, {Kuan Hung}",
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T1 - Xanthohumol, a prenylated flavonoid from hops (Humulus lupulus), prevents platelet activation in human platelets

AU - Lee, Ye Ming

AU - Hsieh, Kuo Hsien

AU - Lu, Wan-Jung

AU - Chou, Hsiu Chu

AU - Chou, Duen Suey

AU - Lien, Li Ming

AU - Sheu, Joen Rong

AU - Lin, Kuan Hung

PY - 2012

Y1 - 2012

N2 - Xanthohumol is the principal prenylated flavonoid in the hop plant (Humulus lupulus L.). Xanthohumol was found to be a very potent cancer chemopreventive agent through regulation of diverse mechanisms. However, no data are available concerning the effects of xanthohumol on platelet activation. The aim of this paper was to examine the antiplatelet effect of xanthohumol in washed human platelets. In the present paper, xanthohumol exhibited more-potent activity in inhibiting platelet aggregation stimulated by collagen. Xanthohumol inhibited platelet activation accompanied by relative [Ca+] i mobilization, thromboxane A2 formation, hydroxyl radical (OH()) formation, and phospholipase C (PLC)2, protein kinase C (PKC), mitogen-activated protein kinase (MAPK), and Akt phosphorylation. Neither SQ22536, an inhibitor of adenylate cyclase, nor ODQ, an inhibitor of guanylate cyclase, reversed the xanthohumol-mediated inhibitory effect on platelet aggregation. Furthermore, xanthohumol did not significantly increase nitrate formation in platelets. This study demonstrates for the first time that xanthohumol possesses potent antiplatelet activity which may initially inhibit the PI3-kinase/Akt, p38 MAPK, and PLC2-PKC cascades, followed by inhibition of the thromboxane A2 formation, thereby leading to inhibition of [Ca+] i and finally inhibition of platelet aggregation. Therefore, this novel role of xanthohumol may represent a high therapeutic potential for treatment or prevention of cardiovascular diseases.

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