1,721,279 research outputs found
Flavonoids and mitochondrial pharmacology: A new paradigm for cardioprotection
Acute myocardial ischemia is one of the major causes of illness and of deaths in Western society; therefore the definition of the signaling pathways involved in the cardioprotection represents a challenging goal in order to discover novel pharmacological approaches. In this regard, a number of epidemiologic studies demonstrate a relationship between intake of flavonoid-rich foods and reduction of cardiovascular risk factors and mortality. Moreover, numerous experimental studies have examined flavonoid-induced cardioprotective effects on several animal models of myocardial ischemia/reperfusion. As concerns the mechanisms of action, although the antioxidant effect of flavonoids has been long thought to be a crucial factor accounting for cardioprotection, mitochondrial pathways (ion channels, protein kinases, etc.) are presently emerging as specific pharmacological targets more relevantly involved in the anti-ischemic effects of some flavonoids. Since these pharmacodynamic features seem to be poorly considered, this review examines the mitochondrial role in the cardioprotective mechanisms of some members of this phytochemical class, by describing the biological pathways and reporting an overview of the most important experimental evidence in this field
Valore nutraceutico dei flavonoidi presenti nel genere Citrus. Evidenze epidemiologiche, cliniche e pre-cliniche degli effetti protettivi dei Citrus flavanoni sulle funzioni cardiovascolari
I flavonoidi presenti nei frutti del genere Citrus (costituiti per il 95% da fl avanoni) stanno emergendo per il loro notevole valore nutraceutico. Evidenze epidemiologiche, cliniche e pre-cliniche dimostrano che l’assunzione di frutti appartenenti al genere Citrus riduce, in modo signifi cativo, l’incidenza delle patologie cardiovascolari.
In questo articolo si dà una disamina degli studi che prendono in esame le loro proprietà benefiche, tentando di dar spazio anche al chiarimento dei più importanti meccanismi d’azione
Rimedi fitoterapici per la sindrome dell’ovaio policistico. Review di clinical trials
Polycystic ovary syndrome (PCOS) is the most common endocrine dysfunction that affects fertile women, it manifests with following symptoms: oligo-amenorrhea and hyperandrogenism,
accompanied by manifestations of acne, hirsutism and alopecia, until morphological alterations of the ovary, evident by ultra-sonographic evaluation and metabolic alterations, with several complications above all at cardiovascular level.
Conventional pharmacological approaches are focused to the treatment of symptoms, through which syndrome manifests; although these aren�t always effi cacy, and also when they are effi cacy, due to the complexity of the disease, there are numerous adverse effects and the probability of pregnancy remains very low. For these reasons, many women affected to PCOS express the desire to use alternative treatments; hoping to can restore its physiological balance without debilitating adverse effects.
Aim of this paper was to analyze medicinal plants with a scientifi c value in the treatments of PCOS symptoms. As regard, a prominent place is occupied from berberine, alkaloid widely used in the clinical as remedy of insulin-resistance, such as effectiveness to metformin; it is accompanied by cinnamon bark extract, used for glycaemia control in mellitus diabetes of type 2. Herbal remedies more used to treat the oligo-amenorrea are based on soia, Cimicifuga racemosa or Grifola frondosa, in particular this is a mushroom, little known in western medicine, but very interesting in therapy with clomifene citrate, and also in mono-therapy is effective as ovulation inductor.
Other herbal remedies could be added at the list, such as Gymnema sylvestre, Dioscorea villosa and Vitex Agnus Castus, medicinal plants of which at the present there are promising results for PCOS treatment, but only at pre-clinical level.
Concluding, phytotherapy potentially plays interesting role to cure PCOS syndrome, having wide possibilities of treatment and allowing integration/support to conventional pharmacology
Cardiac ATP-sensitive potassium channels, a potential target for an anti-ischaemic pharmacological strategy
Brief periods of ischaemia induce in the myocardium an increased resistance to the injury due to a subsequent, more prolonged ischaemic episode. This phenomenon, known as ischaemic pre-conditioning (IPC), articulated in two distinct phases (an early and a delayed one), is ensured by different biological mechanisms. Although an exhaustive comprehension of these mechanisms has not yet been reached, it is widely accepted that among the various signals involved as triggers and/or end-effectors, an important role is undoubtedly played by the activation of cardiac ATP-sensitive potassium channels (KATP). In the myocardial cells, KATP channels have been identified both in the sarcolemmal membrane (sarc-KATP) and in the mitochondrial inner membrane (mito-KATP). Although many experimental findings suggest that a role of sarc-KATP channel activation in IPC cannot be excluded, in the last few years, many authors have indicated that this phenomenon could be attributed to the exclusive (or at least prevalent) activation of the mito-KATP channels. Conversely, drugs modulating the KATP channels (as activators or blockers), on one hand, have been employed as useful experimental tools for basic studies on IPC. On the other hand, KATP-openers have been viewed as promising possible therapeutic agents for limiting the myocardial injury due to ischaemic episodes. In particular, those molecules exhibiting a good degree of selectivity towards the mito-KATP channels have been indicated as potential anti-ischaemic cardio-protective pharmacological tools, devoid of other biological effects (such as negative inotropic activity, hypotension or hyperglycaemia) linked to the activation of cardiac and non-cardiac sarcKATP channels. In this paper, we wish to report the experimental evidence supporting the role of sarc- and mito-KATP channels in IPC the relative signalling pathways potentially involved in the mechanisms of cardio-protection and, finally, an overview of the most important molecules acting as activators or blockers of KATP channels, with their selectivity profile
Nutraceutical Value of Citrus Flavanones and Their Implications in Cardiovascular Disease
Background- Cardiovascular diseases, including myocardial infarction, dyslipidaemia and coronary artery pathology, are a major cause of illness and death in Western countries. Therefore, identifying effective therapeutic approaches and their cellular signalling pathways is a challenging goal for medicine. In this regard, several epidemiological studies demonstrate a relationship between the intake of flavonoid-rich foods and the reduction of cardiovascular risk factors and mortality. In particular, flavonoids present in citrus fruits, such as oranges, bergamots, lemons and grapefruit (95% from flavanones), are emerging for their considerable nutraceutical value. Methods- In this review an examination of literature was performed while considering both epidemiological, clinical and pre-clinical evidence supporting the beneficial role of the flavanone class. We evaluated studies in which citrus fruit juices or single flavanone administration and cardiovascular risk factors were analysed; to identify these studies, an electronic search was conducted in PUBMED for papers fulfilling these criteria and written in English. Results- In addition to epidemiological evidence and clinical studies demonstrating that fruits in the Citrus genus significantly reduce the incidence of cardiovascular disease risk, pre-clinical investigations highlight cellular and subcellular targets that are responsible for these beneficial effects. There has been special attention on evaluating intracellular pathways involved in direct cardiovascular and cardiometabolic effects mediated by naringenin, hesperetin and eriodictyol or their glycosylated derivatives. Conclusions- Although some mechanisms of action remain unclear and bioavailability problems remain to be solved, the current evidence supports the use of a nutraceutical approach with citrus fruits to prevent and cure several aspects of cardiovascular disease
Organic Isothiocyanates as Hydrogen Sulfide Donors
Significance: Hydrogen sulfide (H2S), the "new entry" in the series of endogenous gasotransmitters, plays a fundamental role in regulating the biological functions of various organs and systems. Consequently, the lack of adequate levels of H2S may represent the etiopathogenetic factor of multiple pathological alterations. In these diseases, the use of H2S donors represents a precious and innovative opportunity. Recent Advances: Natural isothiocyanates (ITCs), sulfur compounds typical of some botanical species, have long been investigated because of their intriguing pharmacological profile. Recently, the ITC moiety has been proposed as a new H2S-donor chemotype (with a l-cysteine-mediated reaction). Based on this recent discovery, we can clearly observe that almost all the effects of natural ITCs can be explained by the H2S release. Consistently, the ITC function was also used as an original H2S-releasing moiety for the design of synthetic H2S donors and original "pharmacological hybrids." Very recently, the chemical mechanism of H2S release, resulting from the reaction between l-cysteine and some ITCs, has been elucidated. Critical Issues: Available literature gives convincing demonstration that H2S is the real player in ITC pharmacology. Further, countless studies have been carried out on natural ITCs, but this versatile moiety has been used only rarely for the design of synthetic H2S donors with optimal drug-like properties. Future Directions: The development of more ITC-based synthetic H2S donors with optimal drug-like properties and selectivity toward specific tissues/pathologies seem to represent a stimulating and indispensable prospect of future experimental activities
AN IN VIVO EXPERIMENTAL METHOD TO PREDICT THE TORSADOGENIC POTENTIALITY OF DRUGS: EVALUATION OF QT PROLONGATION IN ANAESTHETISED GUINEA-PIG
Role of mitochondrial KATP channels in the reduced cardiac tolerance to ischemic injury in the ageing
APRIKALIM ABOLISHES THE QT INTERVAL PROLONGATION THIORIDAZINE-INDUCED BY THE ACTIVATION OF SARCOPLASMIC KATP CHANNELS
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