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Elisabetta Barocelli - One of the best experts on this subject based on the ideXlab platform.
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Protective Effect of Foeniculum Vulgare Essential Oil and Anethole in an Experimental Model of Thrombosis
Pharmacological Research, 2007Co-Authors: Massimiliano Tognolini, Vigilio Ballabeni, Simona Bertoni, Renato Bruni, Mariannina Impicciatore, Elisabetta BarocelliAbstract:Abstract In a previous screening work, Foeniculum vulgare essential oil emerged from a pool of 24 essential oils for its antiplatelet properties and its ability to destabilize the retraction of the coagulum. In the present work the main component of the oil, anethole, tested in guinea pig plasma was as potent as fennel oil in inhibiting arachidonic acid-, collagen-, ADP- and U46619-induced aggregation (IC 50 from 4 to 147 μg ml −1 ). It also prevented thrombin-induced clot retraction at concentrations similar to fennel oil. The essential oil and anethole, tested in rat aorta with or without endothelium, displayed comparable NO-independent vasorelaxant Activity at antiplatelet concentrations which have been proved to be free from cytotoxic effects in vitro . In vivo , both F. vulgare essential oil and anethole orally administered in a subacute treatment to mice (30 mg kg −1 day −1 for 5 days) showed significant Antithrombotic Activity preventing the paralysis induced by collagen-epinephrine intravenous injection (70% and 83% protection, respectively). At the Antithrombotic dosage they were free from prohemorrhagic side effect at variance with acetylsalicylic acid used as reference drug. Furthermore, both F. vulgare essential oil and anethole (100 mg kg −1 oral administration) provided significant protection toward ethanol induced gastric lesions in rats. In conclusion, these results demonstrate for F. vulgare essential oil, and its main component anethole, a safe Antithrombotic Activity that seems due to their broad spectrum antiplatelet Activity, clot destabilizing effect and vasorelaxant action.
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antiplatelet and Antithrombotic activities of essential oil from wild ocotea quixos lam kosterm lauraceae calices from amazonian ecuador
Pharmacological Research, 2007Co-Authors: Vigilio Ballabeni, Massimiliano Tognolini, Simona Bertoni, Renato Bruni, Alessandra Guerrini, Gabriela Moreno Rueda, Elisabetta BarocelliAbstract:Ocotea quixos essential oil was shown to possess significant inhibitory Activity of platelet aggregation and clot retraction in rodent plasma. This study is aimed at fully characterizing the antiplatelet Activity of the whole essential oil and its main components trans-cinnamaldehyde and methyl cinnamate also in human plasma, at investigating the mechanism underlying such Activity and at evaluating the potential Antithrombotic Activity of subacute treatment of mice with Ocotea essential oil. In vitro Ocotea essential oil and trans-cinnamaldehyde inhibited arachidonic acid-, U46619-, ADP-, phorbol12-myristate13-alcetate-, collagen-induced platelet aggregation and thrombin-induced clot retraction in human and rodent plasma; Ocotea oil and trans-cinnamaldehyde competitively antagonized contractions induced by thromboxane A2 receptor agonist U46619 in rat isolated aortic ring (K(B) = 18 and 3.2 microg ml(-1), respectively). In vivo Ocotea oil, orally administered in a subacute treatment (30-100 mg kg(-1) day(-1) for 5 days) to mice, prevented acute thrombosis induced by collagen-epinephrine intravenous injection. This Antithrombotic Activity was not accompanied by pro-haemorragic side effect, as detected by the inActivity in bleeding test, thus showing a favourable safety profile compared to the conventional antiplatelet agent, acetylsalicylic acid. Present findings indicate that Ocotea essential oil possesses potent and safe Antithrombotic Activity attributable to its antiplatelet and vasorelaxant effects. The main constituent trans-cinnamaldehyde seems to be the primary responsible for this Activity through a putative mechanism involving the inhibition of thromboxane A2 receptors.
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effects of subacute treatment with benzopyranopyrimidines in hemostasis and experimental thrombosis in mice
Life Sciences, 2004Co-Authors: Vigilio Ballabeni, Massimiliano Tognolini, Francesco Calcina, Olga Bruno, Cesare Manotti, Elisabetta BarocelliAbstract:The Antithrombotic Activity of a series of benzopyranopyrimidine derivatives was investigated in platelet-dependent and independent pulmonary thromboembolism in mice. Intraperitoneal subacute treatment with 2-morpholino derivative 3c significantly prevented paralysis due to collagen plus epinephrine-induced pulmonary thrombosis while 2-piperidino substituted derivative 3h significantly protected mice from paralysis caused by thrombin-induced intravascular fibrin formation at dosage not affecting bleeding time. These compounds, previously proved to be effective as antiplatelet agents in vitro, were in vivo more potent as Antithrombotics than lysine acetylsalicylate and possessed lower prohemorrhagic Activity than the reference drug. Although their ineffectiveness on clotting times, PT and APTT, allows the involvement of coagulation pathways to be ruled out, the mechanisms underlying the favourable benefit risk ratio for these two compounds remain to be further clarified.
Bafang Li - One of the best experts on this subject based on the ideXlab platform.
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Antithrombotic Activity of oral administered low molecular weight fucoidan from laminaria japonica
Thrombosis Research, 2016Co-Authors: Xue Zhao, Jing Hu, Lijuan Zhang, Zhaohui Zhang, Bafang LiAbstract:Abstract Introduction Fucoidans extracted from brown algae have been documented to have excellent Antithrombotic Activity when administered by either intravenous or subcutaneous route in animal models. However, it is unknown if the fucoidans also have Antithrombotic Activity when administered orally, a highly desirable feature of oral Antithrombotic agents. In the present study, we compared the oral absorption, bioavailability and Antithrombotic Activity of two fucoidan fractions from Laminaria japonica with different molecular weight by oral administration in an electricity induced arterial thrombosis model and the underlying molecular mechanisms. Results and conclusions After a single dose of oral administration, the fucoidan content in plasma and urine in rats was assessed using the reverse-phased HPLC analysis of 1-phenyl-3-methyl-5-pyrazolone (PMP)-labeled fucose. The fucose content in the low molecular weight (LMW) fucoidan-treated rats increased up to 2-fold and peaked at 15 h, indicating that the LMW fucoidan had much better absorption and bioavailability than the MMW fucoidan in vivo. Oral administration of the LMW fucoidan at 400 and 800 mg/kg for 30 days inhibited the arterial thrombosis formation effectively induced by electrical shock in rats, accompanied by moderate anticoagulation Activity, regulation on TXB 2 and 6-keto-PGF1α, significant antiplatelet Activity and effective fibrinolysis. The LMW fucoidan showed better oral absorption and Antithrombotic Activity in addition to different Antithrombotic mechanisms compared to those of the medium molecular weight (MMW) fucoidan. Thus, the LMW fucoidan has a potential to become an oral Antithrombotic agent.
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a comparative study of Antithrombotic and antiplatelet activities of different fucoidans from laminaria japonica
Thrombosis Research, 2012Co-Authors: Xue Zhao, Shizhu Dong, Jingfeng Wang, Fang Li, Anjin Chen, Bafang LiAbstract:Abstract Introduction Fucoidans extracted from brown algae represent an intriguing group of natural fucose-enriched sulfated polysaccharide, with excellent anticoagulant, antimetastatic, antiangiogenic and anti-inflammatory activities. In the present study, we compared Antithrombotic activities of four fucoidan fractions with different molecular weight and sulfated ester content from Laminaria japonica in an electrical induced arterial thrombosis and their potential mechanism underlying such Activity. Results and Conclusions In vivo middle molecular weight (MMW) fucoidan fractions with molecular weight about 28000 and 35000 exhibited better Antithrombotic Activity in electrical induced arterial thrombosis than low molecular weight (LMW) fucoidan LF1 and LF2 (Mw 7600 and 3900). Inhibition of arterial thrombosis occurred at dose of 0.1-0.25 mg/kg for MMW fucoidans, accompanied with moderate anticoagulant Activity and significant decrease of whole blood viscosity and hematocrit. The Antithrombotic effects of MMW Fucoidans might be related with promotion of TFPI content and decrease of TXB2 content, without affecting platelet aggregation and 6-keto-PGF1α content in vivo . In contrast, LMW fucoidans showed a correlation among anticoagulant, antiplatelet and Antithrombotic effects in vivo . Antithrombotic action of LF1 and LF2 required high dose of 2.5-10 mg/kg, concomitantly with anticoagulant Activity and specific inhibition of platelet aggregation in vivo . Their Antithrombotic effect might be related to their promotion of TFPI and 6-keto-PGF1α, down regulation of TXB2, without affecting hemorheology. These findings suggested that fucoidan fractions with different molecular weight acted on the Antithrombotic action by different mechanism. By comparison, highly sulfated fucoidan LF2 with molecular weight of 3900 seemed to be a more suitable choice of Antithrombotic drug for its Antithrombotic Activity accompanied with specific inhibitory Activity on platelet aggregation, low anticoagulant Activity and low hemorrhagic risk in vivo .
Douglas M Tollefsen - One of the best experts on this subject based on the ideXlab platform.
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vascular dermatan sulfate regulates the Antithrombotic Activity of heparin cofactor ii
Blood, 2008Co-Authors: Li He, Tusar Giri, Cristina P Vicente, Douglas M TollefsenAbstract:Heparin cofactor II (HCII)–deficient mice form occlusive thrombi more rapidly than do wild-type mice following injury to the carotid arterial endothelium. Dermatan sulfate (DS) and heparan sulfate (HS) increase the rate of inhibition of thrombin by HCII in vitro, but it is unknown whether vascular glycosaminoglycans play a role in the Antithrombotic effect of HCII in vivo. In this study, we found that intravenous injection of either wild-type recombinant HCII or a variant with low affinity for HS (K173H) corrected the abnormally short thrombosis time of HCII-deficient mice, while a variant with low affinity for DS (R189H) had no effect. When HCII was incubated with frozen sections of the mouse carotid artery, it bound specifically to DS in the adventitia. HCII was undetectable in the wall of the uninjured carotid artery, but it became concentrated in the adventitia following endothelial injury. These results support the hypothesis that HCII interacts with DS in the vessel wall after disruption of the endothelium and that this interaction regulates thrombus formation in vivo.
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Antithrombotic Activity of dermatan sulfate in heparin cofactor ii deficient mice
Blood, 2004Co-Authors: Cristina P Vicente, Mauro S G Pavao, Li He, Douglas M TollefsenAbstract:Heparin cofactor II (HCII) is a plasma protein that inhibits thrombin rapidly in the presence of dermatan sulfate or heparin. We previously reported that the time to thrombotic occlusion of the carotid artery after photochemical injury was shorter in HCII-deficient mice than in wild-type control animals. In this paper, we describe the Antithrombotic Activity of dermatan sulfate in wild-type and HCII-deficient mice. Intravenous administration of porcine skin dermatan sulfate induced a dose-dependent prolongation of the carotid artery occlusion time in HCII+/+ mice that was not observed in HCII-/- animals. Pharmacokinetic studies suggested that porcine skin dermatan sulfate expresses Antithrombotic Activity after being transferred from the plasma to sites in the vessel wall. Using invertebrate dermatan sulfate preparations, we showed that N-acetylgalactosamine-4-O-sulfate residues are required for the HCII-dependent Antithrombotic effect. Furthermore, the invertebrate dermatan sulfates, which have higher charge densities than mammalian dermatan sulfate, slightly prolonged the thrombotic occlusion time of HCII-/- mice. These results indicate that HCII mediates the Antithrombotic effect of porcine skin dermatan sulfate after injury to the carotid arterial endothelium in mice, whereas more highly charged dermatan sulfates possess weak Antithrombotic Activity independent of HCII. (Blood. 2004;104:3965-3970)
Vigilio Ballabeni - One of the best experts on this subject based on the ideXlab platform.
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Protective Effect of Foeniculum Vulgare Essential Oil and Anethole in an Experimental Model of Thrombosis
Pharmacological Research, 2007Co-Authors: Massimiliano Tognolini, Vigilio Ballabeni, Simona Bertoni, Renato Bruni, Mariannina Impicciatore, Elisabetta BarocelliAbstract:Abstract In a previous screening work, Foeniculum vulgare essential oil emerged from a pool of 24 essential oils for its antiplatelet properties and its ability to destabilize the retraction of the coagulum. In the present work the main component of the oil, anethole, tested in guinea pig plasma was as potent as fennel oil in inhibiting arachidonic acid-, collagen-, ADP- and U46619-induced aggregation (IC 50 from 4 to 147 μg ml −1 ). It also prevented thrombin-induced clot retraction at concentrations similar to fennel oil. The essential oil and anethole, tested in rat aorta with or without endothelium, displayed comparable NO-independent vasorelaxant Activity at antiplatelet concentrations which have been proved to be free from cytotoxic effects in vitro . In vivo , both F. vulgare essential oil and anethole orally administered in a subacute treatment to mice (30 mg kg −1 day −1 for 5 days) showed significant Antithrombotic Activity preventing the paralysis induced by collagen-epinephrine intravenous injection (70% and 83% protection, respectively). At the Antithrombotic dosage they were free from prohemorrhagic side effect at variance with acetylsalicylic acid used as reference drug. Furthermore, both F. vulgare essential oil and anethole (100 mg kg −1 oral administration) provided significant protection toward ethanol induced gastric lesions in rats. In conclusion, these results demonstrate for F. vulgare essential oil, and its main component anethole, a safe Antithrombotic Activity that seems due to their broad spectrum antiplatelet Activity, clot destabilizing effect and vasorelaxant action.
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antiplatelet and Antithrombotic activities of essential oil from wild ocotea quixos lam kosterm lauraceae calices from amazonian ecuador
Pharmacological Research, 2007Co-Authors: Vigilio Ballabeni, Massimiliano Tognolini, Simona Bertoni, Renato Bruni, Alessandra Guerrini, Gabriela Moreno Rueda, Elisabetta BarocelliAbstract:Ocotea quixos essential oil was shown to possess significant inhibitory Activity of platelet aggregation and clot retraction in rodent plasma. This study is aimed at fully characterizing the antiplatelet Activity of the whole essential oil and its main components trans-cinnamaldehyde and methyl cinnamate also in human plasma, at investigating the mechanism underlying such Activity and at evaluating the potential Antithrombotic Activity of subacute treatment of mice with Ocotea essential oil. In vitro Ocotea essential oil and trans-cinnamaldehyde inhibited arachidonic acid-, U46619-, ADP-, phorbol12-myristate13-alcetate-, collagen-induced platelet aggregation and thrombin-induced clot retraction in human and rodent plasma; Ocotea oil and trans-cinnamaldehyde competitively antagonized contractions induced by thromboxane A2 receptor agonist U46619 in rat isolated aortic ring (K(B) = 18 and 3.2 microg ml(-1), respectively). In vivo Ocotea oil, orally administered in a subacute treatment (30-100 mg kg(-1) day(-1) for 5 days) to mice, prevented acute thrombosis induced by collagen-epinephrine intravenous injection. This Antithrombotic Activity was not accompanied by pro-haemorragic side effect, as detected by the inActivity in bleeding test, thus showing a favourable safety profile compared to the conventional antiplatelet agent, acetylsalicylic acid. Present findings indicate that Ocotea essential oil possesses potent and safe Antithrombotic Activity attributable to its antiplatelet and vasorelaxant effects. The main constituent trans-cinnamaldehyde seems to be the primary responsible for this Activity through a putative mechanism involving the inhibition of thromboxane A2 receptors.
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effects of subacute treatment with benzopyranopyrimidines in hemostasis and experimental thrombosis in mice
Life Sciences, 2004Co-Authors: Vigilio Ballabeni, Massimiliano Tognolini, Francesco Calcina, Olga Bruno, Cesare Manotti, Elisabetta BarocelliAbstract:The Antithrombotic Activity of a series of benzopyranopyrimidine derivatives was investigated in platelet-dependent and independent pulmonary thromboembolism in mice. Intraperitoneal subacute treatment with 2-morpholino derivative 3c significantly prevented paralysis due to collagen plus epinephrine-induced pulmonary thrombosis while 2-piperidino substituted derivative 3h significantly protected mice from paralysis caused by thrombin-induced intravascular fibrin formation at dosage not affecting bleeding time. These compounds, previously proved to be effective as antiplatelet agents in vitro, were in vivo more potent as Antithrombotics than lysine acetylsalicylate and possessed lower prohemorrhagic Activity than the reference drug. Although their ineffectiveness on clotting times, PT and APTT, allows the involvement of coagulation pathways to be ruled out, the mechanisms underlying the favourable benefit risk ratio for these two compounds remain to be further clarified.
Massimiliano Tognolini - One of the best experts on this subject based on the ideXlab platform.
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Protective Effect of Foeniculum Vulgare Essential Oil and Anethole in an Experimental Model of Thrombosis
Pharmacological Research, 2007Co-Authors: Massimiliano Tognolini, Vigilio Ballabeni, Simona Bertoni, Renato Bruni, Mariannina Impicciatore, Elisabetta BarocelliAbstract:Abstract In a previous screening work, Foeniculum vulgare essential oil emerged from a pool of 24 essential oils for its antiplatelet properties and its ability to destabilize the retraction of the coagulum. In the present work the main component of the oil, anethole, tested in guinea pig plasma was as potent as fennel oil in inhibiting arachidonic acid-, collagen-, ADP- and U46619-induced aggregation (IC 50 from 4 to 147 μg ml −1 ). It also prevented thrombin-induced clot retraction at concentrations similar to fennel oil. The essential oil and anethole, tested in rat aorta with or without endothelium, displayed comparable NO-independent vasorelaxant Activity at antiplatelet concentrations which have been proved to be free from cytotoxic effects in vitro . In vivo , both F. vulgare essential oil and anethole orally administered in a subacute treatment to mice (30 mg kg −1 day −1 for 5 days) showed significant Antithrombotic Activity preventing the paralysis induced by collagen-epinephrine intravenous injection (70% and 83% protection, respectively). At the Antithrombotic dosage they were free from prohemorrhagic side effect at variance with acetylsalicylic acid used as reference drug. Furthermore, both F. vulgare essential oil and anethole (100 mg kg −1 oral administration) provided significant protection toward ethanol induced gastric lesions in rats. In conclusion, these results demonstrate for F. vulgare essential oil, and its main component anethole, a safe Antithrombotic Activity that seems due to their broad spectrum antiplatelet Activity, clot destabilizing effect and vasorelaxant action.
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antiplatelet and Antithrombotic activities of essential oil from wild ocotea quixos lam kosterm lauraceae calices from amazonian ecuador
Pharmacological Research, 2007Co-Authors: Vigilio Ballabeni, Massimiliano Tognolini, Simona Bertoni, Renato Bruni, Alessandra Guerrini, Gabriela Moreno Rueda, Elisabetta BarocelliAbstract:Ocotea quixos essential oil was shown to possess significant inhibitory Activity of platelet aggregation and clot retraction in rodent plasma. This study is aimed at fully characterizing the antiplatelet Activity of the whole essential oil and its main components trans-cinnamaldehyde and methyl cinnamate also in human plasma, at investigating the mechanism underlying such Activity and at evaluating the potential Antithrombotic Activity of subacute treatment of mice with Ocotea essential oil. In vitro Ocotea essential oil and trans-cinnamaldehyde inhibited arachidonic acid-, U46619-, ADP-, phorbol12-myristate13-alcetate-, collagen-induced platelet aggregation and thrombin-induced clot retraction in human and rodent plasma; Ocotea oil and trans-cinnamaldehyde competitively antagonized contractions induced by thromboxane A2 receptor agonist U46619 in rat isolated aortic ring (K(B) = 18 and 3.2 microg ml(-1), respectively). In vivo Ocotea oil, orally administered in a subacute treatment (30-100 mg kg(-1) day(-1) for 5 days) to mice, prevented acute thrombosis induced by collagen-epinephrine intravenous injection. This Antithrombotic Activity was not accompanied by pro-haemorragic side effect, as detected by the inActivity in bleeding test, thus showing a favourable safety profile compared to the conventional antiplatelet agent, acetylsalicylic acid. Present findings indicate that Ocotea essential oil possesses potent and safe Antithrombotic Activity attributable to its antiplatelet and vasorelaxant effects. The main constituent trans-cinnamaldehyde seems to be the primary responsible for this Activity through a putative mechanism involving the inhibition of thromboxane A2 receptors.
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effects of subacute treatment with benzopyranopyrimidines in hemostasis and experimental thrombosis in mice
Life Sciences, 2004Co-Authors: Vigilio Ballabeni, Massimiliano Tognolini, Francesco Calcina, Olga Bruno, Cesare Manotti, Elisabetta BarocelliAbstract:The Antithrombotic Activity of a series of benzopyranopyrimidine derivatives was investigated in platelet-dependent and independent pulmonary thromboembolism in mice. Intraperitoneal subacute treatment with 2-morpholino derivative 3c significantly prevented paralysis due to collagen plus epinephrine-induced pulmonary thrombosis while 2-piperidino substituted derivative 3h significantly protected mice from paralysis caused by thrombin-induced intravascular fibrin formation at dosage not affecting bleeding time. These compounds, previously proved to be effective as antiplatelet agents in vitro, were in vivo more potent as Antithrombotics than lysine acetylsalicylate and possessed lower prohemorrhagic Activity than the reference drug. Although their ineffectiveness on clotting times, PT and APTT, allows the involvement of coagulation pathways to be ruled out, the mechanisms underlying the favourable benefit risk ratio for these two compounds remain to be further clarified.