Functional benefits of PLGA particulates carrying VEGF and CoQ10 in an animal of myocardial ischemia.

forrás: http://www.ncbi.nlm.nih.gov/pubmed/23639291


2015-02-17 16:34:43


Myocardial ischemia (MI) remains one of the leading causes of death worldwide. Angiogenic therapy with the vascular endothelial growth factor (VEGF) is a promising strategy to overcome hypoxia and its consequences. However, from the clinical data it is clear that fulfillment of the potential of VEGF warrants a better delivery strategy. On the other hand, the compelling evidences of the role of oxidative stress in diseases like MI encourage the use of antioxidant agents. Coenzyme Q10 (CoQ10) due to its role in the electron transport chain in the mitochondria seems to be a good candidate to manage MI but is associated with poor biopharmaceutical properties seeking better delivery approaches. The female Sprague Dawley rats were induced MI and were followed up with VEGF microparticles intramyocardially and CoQ10 nanoparticles orally or their combination with appropriate controls. Cardiac function was assessed by measuring ejection fraction before and after three months of therapy. Results demonstrate significant improvement in the ejection fraction after three months with both treatment forms individually; however the combination therapy failed to offer any synergism. In conclusion, VEGF microparticles and CoQ10 nanoparticles can be considered as promising strategies for managing MI.


Mechanisms underlying the antihypertensive effects of garlic bioactives.

forrás: http://www.ncbi.nlm.nih.gov/pubmed/24461311


2015-02-17 14:32:03


Cardiovascular disease remains the leading cause of death worldwide with hypertension being a major contributing factor to cardiovascular disease-associated mortality. On a population level, non-pharmacological approaches, such as alternative/complementary medicine, including phytochemicals, have the potential to ameliorate cardiovascular risk factors, including high blood pressure. Several epidemiological studies suggest an antihypertensive effect of garlic (Allium sativum) and of many its bioactive components. The aim of this review is to present an in-depth discussion regarding the molecular, biochemical and cellular rationale underlying the antihypertensive properties of garlic and its bioactive constituents with a primary focus on S-allyl cysteine and allicin. Key studies, largely from PubMed, were selected and screened to develop a comprehensive understanding of the specific role of garlic and its bioactive constituents in the management of hypertension. We also reviewed recent advances focusing on the role of garlic bioactives, S-allyl cysteine and allicin, in modulating various parameters implicated in the pathogenesis of hypertension. These parameters include oxidative stress, nitric oxide bioavailability, hydrogen sulfide production, angiotensin converting enzyme activity, expression of nuclear factor-κB and the proliferation of vascular smooth muscle cells. This review suggests that garlic and garlic derived bioactives have significant medicinal properties with the potential for ameliorating hypertension and associated morbidity; however, further clinical and epidemiological studies are required to determine completely the specific physiological and biochemical mechanisms involved in disease prevention and management.

Copyright © 2014 Elsevier Inc. All rights reserved.


Suppression of human monocyte tissue factor induction by red wine phenolics and synthetic derivatives of resveratrol

forrás: http://www.ncbi.nlm.nih.gov/pubmed/16507316


2014-10-28 13:42:48


Prevention of cardiovascular disease through nutritional supplements is growing in popularity throughout the world. Multiple epidemiologic studies found that moderate consumption of alcohol, particularly red wine, lowers mortality rates from coronary heart diseases (CHD). Chronic inflammation and atherosclerosis associated with CHD culminate in aberrant intravascular expression of tissue factor (TF), which triggers blood coagulation leading to thrombosis, a major cause for heart attack. We showed earlier that two red wine phenolics, resveratrol and quercetin, suppressed TF induction in endothelial cells. In the present study, we investigated efficacy of seven resveratrol derivatives, which were shown to be effective in regulating cancer cell growth in vitro at much lower concentrations than the parent compound resveratrol, in inhibiting TF induction in peripheral blood mononuclear cells (PBMCs). We also tested possible synergistic effects of resveratrol and quercetin with the other major red wine phenolics in suppression of lipopolysaccharide-induced TF expression in human PBMCs. We found that several resveratrol derivatives were 2- to 10-fold more efficient than resveratrol in inhibiting TF induction. Our study found no evidence for synergism among red wine polyphenolics. These data suggest that structural alterations of resveratrol can be effective in producing potent antithrombotic agents that will have therapeutic potential in the improvement of cardiovascular health and prevention of CHD. Among major red wine phenolics, quercetin appears to be the predominant suppressor of TF induction.


A PLG VEGF-et és CoQ10-et hordozó részecskéinek funkcionális hasznossága az állatok szívizomzati ischemiájában.

forrás: http://www.ncbi.nlm.nih.gov/pubmed/23639291


2015-02-17 16:34:43


Simón-Yarza T1, Tamayo E, Benavides C, Lana H, Formiga FR, Grama CN, Ortiz-de-Solorzano C, Kumar MNProsper FBlanco-Prieto MJ

Információk a szerzőről

  • 1Gyógyszerészeti és Gyógyszerészeti Technológiai Szak, Gyógyszerészeti Iskola, Navarrai Egyetem, Pamplona, Spanyolország.

Kivonat

Világszerte a szívizomzati ischemia (MI) marad a vezető halálok. Az angiogén (ér eredetű) terápia vaszkuláris (véredény-) belhám növekedési faktor (VEGF) egy ígéretes stratégia, hogy le lehessen győzni a hypoxiát (oxigénhiány) és annak következményeit. A klinikai adatokból azonban világos, hogy a lehetséges VEGF elvégzése jobb kivitelezési stratégiát tud biztosítani. Másrészt az oxidatív stressz kényszerítő bizonyítékai az olyan betegségekben, mint az MI, arra bátorítanak, hogy antioxidáns hatóanyagokat használjunk. A Coenzyme Q10 (CoQ10) szerepénél fogva, mellyel részt vesz az elektrontovábbító láncban a mitokondriumban, jó jelöltnek tűnik, hogy felügyelje az MI-t, bár gyenge bio-gyógyszerészeti tulajdonságokkal bír, és jobb közvetítői megközelítést kell keresni hozzá. A Sprague Dawley nőstény patkányoknál MI-t indítottak be, amit VEGF mikrorészecskés kezelés követett miokardiálisan (a szívizomba adva), majd CoQ10 nano-részecskéket kaptak szájon keresztül, vagy pedig ezek kombinációját a megfelelő kontroll alatt. Szívfunkciójukat begyűjtötték a kivetési frakció mérésével, három hónappal a terápia előtt és után. Az eredmények azt mutatják, hogy jelentős javulás mutatkozott a frakció kidobásában három hónappal mindkét fajta kezelés után három hónappal, egyénileg; ám a kombinált gyógymód sikertelen volt bármiféle szinergikus (kölcsönös) lehetőség nyújtásában. Következésképpen a VEGF mikro-részecskéket és a CoQ10 nano-részecskéket ígéretes stratégiának lehet tekinteni az MI kezelésében.


Inducţia factorului de supresie a monocitelor umane de către fenolii din vinul roşu şi derivaţii sintetici ai resveratrolului

forrás: http://www.ncbi.nlm.nih.gov/pubmed/16507316


2014-10-28 13:42:48


Prevenirea afecţiunilor cardio-vasculare prin suplimenţi nutriţionali creşte în popularitate pretutindeni în lume. Studii epidemiologice multiple au găsit că utilizarea moderată de alcool, în mod particular de vin roşu, scade rata de mortalitate cauzată de afecţiunile coronariene ale inimii (CHD). Inflamaţia cronică şi ateroscleroza asociată cu CHD culminează cu o expresie intravasculară aberantă a factorului de ţesut (TF), care declanşează coagularea sângelui, ceea ce conduce la tromboză, o cauză majoră a atacului de cord. Am arătat mai devreme că doi fenoli din vinul roşu, resveratrolul şi quercetina, au supresat  inducţia TF la celulele endoteliale. În studiul prezent noi am investigat eficacitatea a şapte derivaţi ai resveratrolului, care s-au arătat a fi eficienţi în reglarea creşterii celulelor canceroase in vitro, la concentraţii mult mai joase decât compusul de origine, resveratrolul, şi am urmărit cu ajutorul acestor derivaţi inhibarea inducţiei TF în celulele mononucleare periferice ale sângelui (PBMC). Am testat de asemenea posibilul efect sinergic al resveratrolului şi quercetinei cu alţi polifenoli majori din vinul roşu, în supresarea expresiei TF indusă de lipopolizaharide,  în PBMC-ul uman. Am găsit că anumiţi derivaţi ai resveratrolului erau de 2 pana la 10 ori mai eficienţi decât resveratrolul în inhibarea inducerii TF. Studiul nostru nu a găsit nici o dovadă pentru sinergie la polifenolii din vinul roşu. Aceste date sugerează că alteraţiile structurale ale resveratrolului pot fi eficiente în a produce agenţi antitrombotici puternici care vor avea potenţial terapeutic în îmbunătăţirea sănătăţii cardiovasculare şi prevenirea CHD. Printre fenolii majori ai vinului roşu, quercetina apare ca fiind supresorul predominant al inducţiei TF.


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