Antiplatelet activity of flavonoid and coumarin drugs

Zaragozá, Cristina; Monserrat, Jorge; Mantecón, Carolina; Villaescusa, Lucinda; Zaragozá, Francisco Torrens; Álvarez‐Mon, Melchor

doi:10.1016/j.vph.2016.09.002

Cited by 59 publications

(37 citation statements)

References 45 publications

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“…NGN is widely used in traditional Chinese medicine for its multiple pharmacological effects, including antiinflammatory and antioxidative actions ( 8 , 11 , 12 ). NGN has several purported beneficial cardiovascular effects and has been shown to prevent the growth of atherosclerotic plaques, improve vascular reactivity, inhibit platelet aggregation, decrease plasma lipids and lipoproteins, alleviate myocardial ischemia/reperfusion injury, and protect against doxorubicin-induced cardiac toxicity ( 8 – 10 , 13 , 14 ). A previous study reported that NGN supplementation improved hypertension in high-carbohydrate/high-fat-diet-fed obese rats ( 15 ).…”

Section: Discussionmentioning

confidence: 99%

Naringenin inhibits NG‑nitro‑L‑arginine methyl ester‑induced hypertensive left ventricular hypertrophy by decreasing angiotensin‑converting enzyme 1 expression

et al. 2018

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Naringenin (NGN) is a natural flavonoid that exerts antiinflammatory, antioxidant and cardioprotective effects. The present study investigated the effects of NGN on left ventricular hypertrophy in rats with NG-nitro-L-arginine methyl ester (L-NAME)-induced hypertension, and sought to determine the underlying mechanism of action. The rats received the following by gavage daily for 56 days: L-NAME (50 mg/kg/day) + NGN (100 mg/kg/day), L-NAME (50 mg/kg/day) + saline, or saline + saline. Blood pressure, heart rate and body weight were recorded. Left ventricular hypertrophy was assessed by echocardiography and hematoxylin-eosin staining. Angiotensin II (Ang II) and angiotensin-converting enzyme 1 (ACE1), which serve a pivotal role in cardiac remodeling, were evaluated by ELISA, reverse transcription-quantitative polymerase chain reaction and western blot analysis. NGN had no significant effect on body weight, heart rate or blood pressure. The extent of left ventricular hypertrophy in the L-NAME + NGN group was lower than in the L-NAME + saline group on day 56. NGN decreased Ang II and ACE1 protein levels in myocardial tissues. In conclusion, Ang II and ACE1 expression in cardiac tissue was inhibited by NGN in L-NAME-treated rats, which may contribute to the inhibitory effects of NGN on left ventricular hypertrophy that is induced by pressure overload.

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Section: Discussionmentioning

confidence: 99%

Naringenin inhibits NG‑nitro‑L‑arginine methyl ester‑induced hypertensive left ventricular hypertrophy by decreasing angiotensin‑converting enzyme 1 expression

et al. 2018

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“…Si bien no debemos olvidar que existen im portantes diferencias entre los productos gené ricos y los biosimilares en cuanto a costes de desarrollo y de producción. En general, para el desarrollo de un medicamento genérico se requieren entre dos y tres años y una inversión de 1 a 3 millones de euros, mientras que para el desarrollo de un biosimilar se necesitan en tre cinco y ocho años y de 100 a 300 millones de euros, según datos del «Libro blanco de los Medicamentos biosimilares en España: Inno va ción y Sostenibilidad» (Zaragozá et al, 2017).…”

Section: La Oferta En España De Genéricos Y Biosimilaresunclassified

“…Se estima que el ahorro generado en el SNS español por la introducción de los biosimi lares en el periodo 20092016 ascendió a 478 millones de euros. La mayor parte del ahorro total producido en ese periodo se debió a la in troducción del biosimilar de la insulina glargina (25 %), seguido del de somatropina (21 %), in fliximab (20 %), filgrastim (16 %) y epoetina Colaboraciones BOLETÍN ECONÓMICO DE ICE 3115 DEL 1 AL 30 DE SEPTIEMBRE DE 2019 fase de desarrollo también es un indicativo del auge previsto en este mercado (Zaragozá et al, 2017).…”

Section: La Demanda En España De Genéricos Y Biosimilaresunclassified

Supresión de barreras a la industria farmacéutica de la UE: oportunidades y retos

Goya¹

2019

BICE

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Recientemente se ha aprobado el Reglamento (UE) 2019/933 del Parlamento Europeo y del Consejo, de 20 de mayo de 2019, que modifica al Reglamento (CE) nº 469/2009 relativo al certificado complementario de protección para los medicamentos. Este artículo explica en qué ha consistido este cambio legislativo en materia de propiedad industrial en el sector farmacéutico, los motivos que han impulsado la modificación y cuáles podrían ser las consecuencias en términos de tejido industrial y de competencia en este sector en la UE.

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“…Coumarins show certain biochemical properties which exert certain biological effects in the cellular environment. Coumarin derivatives possess a remarkably broad spectrum of biological activities including antiplasmoidal, COX inhibitors, anti‐inflammatory, antifungal, anti‐tubercular, antiviral, antibacterial, and antiplatelet activities, carbonic anhydrase inhibitors, anticancer agents, α‐glucosidase inhibitors, cholinesterase inhibitors . Coumarins have also potential antifungal properties on Aspergillus species .…”

Section: Introductionmentioning

confidence: 99%

Synthesis, Anticholinesterase, Antioxidant, and Anti‐Aflatoxigenic Activity of Novel Coumarin Carbamate Derivatives

et al. 2018

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New coumarin derivatives with the carbamate moiety were synthesized and their inhibitory effects on acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) were evaluated. 4methyl-2-oxo-2H-chromen-7-yl cycloheptylcarbamate (4 h) showed the strongest inhibition against AChE with IC 50 values of 2.30 mM, and 2-oxo-2H-chromen-7-yl-(cyclohexylmethyl) carbamate (4 c) and 4-methyl-2-oxo-2H-chromen-7-yl-(cyclohexylmethyl)carbamate (4 g) were found to be the most potent BuChE inhibitors with IC 50 value of 0.003 mM and 0.004 mM, respectively. Moreover antioxidant, anti-aflatoxigenic activities, protective effects against aflatoxin-B1 (AFB1) in H4IIEÀC3 cells and effects on glutathione s-transferase of the synthesized compounds were investigated. The synthesized coumarin carbamates inhibited AFB1 in H4IIEÀC3 cells. Western blot analyses confirmed that GSTa protein was induced in cells treated with coumarin carbamates and AFB1. These results showed that the synthesized coumarin carbamates possess a potent protective effect against AFB1.[a] Dr.

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Antiplatelet activity of flavonoid and coumarin drugs

Cited by 59 publications

References 45 publications

Naringenin inhibits NG‑nitro‑L‑arginine methyl ester‑induced hypertensive left ventricular hypertrophy by decreasing angiotensin‑converting enzyme 1 expression

Naringenin inhibits NG‑nitro‑L‑arginine methyl ester‑induced hypertensive left ventricular hypertrophy by decreasing angiotensin‑converting enzyme 1 expression

Supresión de barreras a la industria farmacéutica de la UE: oportunidades y retos

Synthesis, Anticholinesterase, Antioxidant, and Anti‐Aflatoxigenic Activity of Novel Coumarin Carbamate Derivatives

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