COX, LOX and platelet aggregation inhibitory properties of Lauraceae neolignans

Coy, Ericsson David; Suárez, Luís Enríque Cuca; Sefkow, Michael

doi:10.1016/j.bmcl.2009.10.069

Cited by 56 publications

(37 citation statements)

References 25 publications

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“…Previous phytochemical analysis from N. amazonum has shown the presence of tannins, steroids, triterpenes, coumarins and flavonoids, although terpene lactones, neolignans and chalcone-related compounds seem to be the main source of the antiplatelet metabolites [10][11][12]. According to the results of the present work, active compounds are also present in the bark fraction of this species.…”

Section: Discussionsupporting

confidence: 68%

“…In fact, chalcone and dihydrochalcone related compounds isolated from leaves of N. amazonum display selectivity towards COX-1 inhibition in the range 1.6 -36.1 µM [10]. Further studies on the bark of this species will determine the bioactive metabolites and their mechanisms of actions [10,11].…”

Section: Discussionmentioning

confidence: 99%

“…In fact, Kadsurenone, a neolignan compound also isolated from the leaves of N. amazonum, inhibits the platelet activated factor (PAF) in the range 0.13 -0.17 nM [11]. In any case, a marked antiaggregant potency would not be desirable because it would increase the risk of bleeding events [15].…”

Section: Discussionmentioning

confidence: 99%

“…(Lauraceae) has shown antiplatelet properties in experimental models. Chalcone derivatives isolated from this species display inhibition of cyclooxygenase I (COX-1) and bicyclooctane neolignan metabolites, selectively inhibiting the platelet-activating factor (PAF) [10][11][12]. The antiagreggant potency of these compounds varies from the micromolar to the nanomolar range.…”

Section: Introductionmentioning

confidence: 99%

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ASSESMENT OF PLATELET ANTIAGGREGANT ACTIVITY OF A FRACTION FROM AN ETHANOLIC EXTRACT OF THE BARK OF Nectandra amazonum Nees

Espitia-Corredor

Suárez

Pabón

2016

Vitae

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Background: Some species of the Lauraceae family are known to produce secondary metabolites that have antiplatelet properties. Studies on the leaves of Nectandra amazonum Nees. have shown antiaggregant activity but the bark of this species has not been studied. Objectives: To assess the antiplatelet effect of the ethanolic fraction obtained from the bark of Nectandra amazonum Nees. [N.V. "laurel amarillo", Lauraceae] applying the "Born" turbidimetric method. Methods: The screening test compared the effects of a fraction of N. amazonum (0.1 mg/mL), acetylsalicylic acid (ASA, 0.5 mM, as reference standard) and dimethylsulphoxide (DMSO, 0.1%, as control) on human platelets stimulated with adenosine diphosphate (ADP, 2 µM), epinephrine (EPI, 1 uM (one micromolar)), collagen (COLL, 1 µg/mL) and arachidonic acid (AA, 0.2 mg/mL). Subsequently, the study focused on determining the antiaggregant potency of the N. amazonum fraction through concentration -response curves (from 1 µg/mL to 0.4 mg/ mL), obtaining pIC 50 ) values against the platelet agonists. Results: Control platelets attained the highest percentage values of aggregation (96% AA, 89% EPI, 85% COLL, and 77% ADP). The N. amazonum fraction significantly reduced the aggregation effects (6% AA, 45% EPI, 10% COLL, 21% ADP), with values close to those obtained with ASA (17% AA, 21% EPI, 10% COLL, 20% ADP). According to concentration -response curves, the pIC 50 values of the ethanolic fraction indicated the following order of potency: AA, 4.90 > ADP, 4.51 > COLL, 4.33 > EPI, 3.85. Conclusions: These results suggest that the N. amazonum Nees. ethanolic fraction elicited antiplatelet effects mainly related to the inhibition of the arachidonic acid pathway.

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Section: Discussionsupporting

confidence: 68%

Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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ASSESMENT OF PLATELET ANTIAGGREGANT ACTIVITY OF A FRACTION FROM AN ETHANOLIC EXTRACT OF THE BARK OF Nectandra amazonum Nees

Espitia-Corredor

Suárez

Pabón

2016

Vitae

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“…Lignans are of great interest in the search for novel agents with antiproliferative, antioxidant and anti-inflammatory properties (Coy, Cuca, & Sefkow, 2009;Di Micco et al, 2011). These compounds represent 1.63% (w/w) of BS-EAc f .…”

Section: Lignansmentioning

confidence: 99%