Mechanisms of Endothelial Protection by Natural Bioactive Compounds from Fruit and Vegetables.

The endothelium is fundamental for the regulation of vascular tone and structure. Under disease conditions, including the presence of cardiovascular disease risk factors, the endothelium loses its protective role and becomes a proatherosclerotic structure. In this article we searched for strategies from PUBMED and Science Direct databases using the following key words: endothelium, natural bioactive compounds, polyphenols and cardiovascular diseases. The search was restricted to english language papers. Studies have identified the contribution of diet to the risk of developing cardiovascular diseases. In this context, high intakes of fruit and vegetables are associated with the decrease of cardiovascular diseases. Thus the most important fruit/vegetables and bioactive compounds to prevent endothelial diseases are berries, apples, virgin olive oil, tomatoes, soybeans, and polyphenols, carotenoids and unsaturated fatty acids, respectively. The bioactive compounds from fruit and vegetables provide endothelial protection through the following mechanisms: improved eNOS/NO bioavailability, attenuates oxidative stress, inhibited NF-κB pathway and decreased cell adhesion molecules expression. In this article natural bioactive compound mechanisms of endothelium protection are thoroughly reviewed.

Mechanisms of Endothelial Protection by Natural Bioactive Compounds from Fruit and Vegetables

ABSTRACT The endothelium is fundamental for the regulation of vascular tone and structure. Under disease conditions, including the presence of cardiovascular disease risk factors, the endothelium loses its protective role and becomes a proatherosclerotic structure. In this article we searched for strategies from PUBMED and Science Direct databases using the following key words: endothelium, natural bioactive compounds, polyphenols and cardiovascular diseases. The search was restricted to english language papers. Studies have identified the contribution of diet to the risk of developing cardiovascular diseases. In this context, high intakes of fruit and vegetables are associated with the decrease of cardiovascular diseases. Thus the most important fruit/vegetables and bioactive compounds to prevent endothelial diseases are berries, apples, virgin olive oil, tomatoes, soybeans, and polyphenols, carotenoids and unsaturated fatty acids, respectively. The bioactive compounds from fruit and vegetables provide endothelial protection through the following mechanisms: improved eNOS/NO bioavailability, attenuates oxidative stress, inhibited NF-κB pathway and decreased cell adhesion molecules expression. In this article natural bioactive compound mechanisms of endothelium protection are thoroughly reviewed.

[Systemic phlebotrophic agents: from active substance to clinical effect].

The article deals with the modern classification of phlebotrophic agents, followed by generalization and analysis of their mechanisms of action, peculiarities of their entering the systemic circulation, as well as a detailed description of phlebotrophic properties and clinical application of the water-soluble fraction of flavonoids.

[Primary and secondary prevention of alcoholic liver cirrhosis].

Alcohol--is the main causative factor of cirrhosis among the population in Russia. The primary prevention must be focused on exception of consumption of heavy doses of alcohol hepatitis and B vaccination. There are no healthy doses of alcohol. Secondary prevention means the use of the hepatoprotectors. List of hepatoprotectors and also amount of money spent to the purchase of these hepatoprotectors increase constantly. But, unfortunately, alongside with it, increases the mortality from hepatic disorders. Effectiveness of the most hepatoprotectors (such as Essential phospholipids, milk thistle) equals to the effectiveness of placebo.

Cardiac and neuroprotection regulated by α(1)-adrenergic receptor subtypes.

Sympathetic nervous system regulation by the α(1)-adrenergic receptor (AR) subtypes (α(1A), α(1B), α(1D)) is complex, whereby chronic activity can be either detrimental or protective for both heart and brain function. This review will summarize the evidence that this dual regulation can be mediated through the different α(1)-AR subtypes in the context of cardiac hypertrophy, heart failure, apoptosis, ischemic preconditioning, neurogenesis, locomotion, neurodegeneration, cognition, neuroplasticity, depression, anxiety, epilepsy, and mental illness.

[Towards the estimation of survival curves parameters and geroprotectors classification].

The following parameters are proposed to estimate in survival curves analysis: Median Life Span, Hill slope, Expected Maximal Life Span. Those estimates enable to classify geroprotectors as weak, moderate and strong.

Fluorinated amphiphilic amino acid derivatives as antioxidant carriers: a new class of protective agents.

The use of classical antioxidants is limited by their low bioavailabilities, and therefore, high doses are usually required to display significant protective activity. In a recent article (J. Med. Chem. 2003, 46, 5230) we showed that the ability of the alpha-phenyl-N-tert-butylnitrone (PBN) to restore the viability of ATPase-deficient human skin fibroblasts was greatly enhanced by grafting it on a fluorinated amphiphilic carrier. With the aim of extending this concept to other antioxidants, we present here the design, the synthesis, and the physicochemical measurements of a new series of fluorinated amphiphilic antioxidant derivatives. The hydroxyl radical scavenging activity and the radical reducing potency of these newly designed compounds were respectively demonstrated in an ABTS competition and an ABTS(*+) reduction assay. We also showed that the protective effects of amphiphilic antioxidants derived from PBN, Trolox (6-hydroxy-2,5,7,8-tetramethylchroman-2-carboxylic acid) or lipoic acid (5-[1,2]-dithiolan-3-ylpentanoic acid) in primary cortical mixed cell cultures exposed to oxidotoxins are greatly improved compared to their parent compounds in the following rank-order: (1) PBN, (2) Trolox, and (3) lipoic acid. In contrast, the protective activity of indole-3-propionic acid was slightly decreased by grafting it on the amphiphilic carrier. Similar observations were made in in vivo experiments using aquatic invertebrate microorganisms, called rotifers, which were exposed to lethal concentrations of nonselective (H(2)O(2)) and mitochondria-selective (doxorubicin) oxidotoxins. The conclusion of these studies is that fluorinated amphiphilic PBN, Trolox, and lipoic acid derivatives exhibit very potent protective activities in in vitro and in vivo experiments. The findings demonstrated herein therefore strongly suggest that the amphiphilic character enhances the bioavailability of the antioxidants and allows for a selective targeting of mitochondria.

Evaluation of protective ointments used against dermal effects of nitrogen mustard, a vesicant warfare agent.

Mustard, a vesicant warfare agent, has cytotoxic, mutagenic, and cytostatic effects via alkylation of DNA and inhibition of DNA replication. Since symptoms appear following a latent period, it can cause some subacute and chronic effects to occur and delay in the treatment. Therefore, the main approach should be the use of protective preparation to reduce the skin toxicity. Thus, this study was conducted in guinea pigs (350-400 g) shaved in areas of 10 x 10 cm. Mechlorethamine HCl (100 mg), a nitrogen mustard derivative, in ethanol was applied by spraying on hairless regions where previously prepared pharmaceutical topical formulations were medicated before. The experimental regions of the animals were kept preserved from environmental factors. Forty-eight hours after the application of the protective ointments and mechlorethamine consecutively, skin-damaging effects were macroscopically evaluated in terms of erythema formation, ulceration, necrosis, and inflammation occurrences. Then, punch biopsy was performed from these damaged sites for histopathological evaluation. Although numerous topical formulations were prepared and tested for protection, according to microscopic examination of the pathologic sections, tissue specimen treated with the ointment containing the mixture of zinc oxide, zinc chloride, dimethylpolysiloxane in a base of petroleum jelly was determined as being the most effective protective against skin injury caused by the vesicant agent.

Skin protectant drug products for over-the-counter human use; final monograph; technical amendment. Final rule; technical amendment.

The Food and Drug Administration (FDA) is amending the regulation that established conditions under which over-the-counter (OTC) skin protectant drug products are generally recognized as safe and effective and not misbranded as part of FDA's ongoing review of OTC drug products. This amendment revises several of the indications for OTC skin protectant drug products to provide additional labeling claims that should not have been excluded from the final monograph (FM).

Skin protectant drug products for over-the-counter human use; final monograph. Final rule.

The Food and Drug Administration (FDA) is issuing a final rule in the form of a final monograph establishing conditions under which over-the-counter (OTC) skin protectant drug products are generally recognized as safe and effective and not misbranded as part of the ongoing review of OTC drug products conducted by FDA. The final monograph includes OTC skin protectant drug products for minor cuts, scrapes, burns, chapped skin and lips, poison ivy, poison oak, poison sumac, and insect bites. FDA is issuing this final rule after considering public comments on the agency's proposed regulation, which was issued in the form of a tentative final monograph, and all new data and information on skin protectant drug products for these specific uses that have come to the agency's attention. This final rule amends the regulation that lists nonmonograph active ingredients by adding those OTC skin protectant ingredients that have been found to be not generally recognized as safe and effective. This final rule also lifts the stay of 21 CFR part 352 (published at 66 FR 67485, December 31, 2001) to amend the final monograph for OTC sunscreen drug products to include sunscreen-skin protectant combination drug products, and then stays Sec. 347.20(d) (21 CFR 347.20(d)) and part 352 until further notice in the Federal Register.

Skin protectant drug products for over-the-counter human use; astringent drug products; final monograph; direct final rule. Direct final rule.

The Food and Drug Administration (FDA) is amending the regulation that established conditions under which over-the-counter (OTC) skin protectant astringent drug products are generally recognized as safe and effective and not misbranded. This action revises some labeling for astringent drug products to be consistent with the final rule for OTC skin protectant drug products (68 FR 33362, June 4, 2003) and adds labeling for certain small packages (styptic pencils). This action is part of FDA's ongoing review of OTC drug products. Elsewhere in this issue of the Federal Register, FDA is publishing a companion proposed rule, under FDA's usual procedure for notice-and-comment rulemaking, to provide a procedural framework to finalize the rule in the event the agency receives any significant adverse comments and withdraws this direct final rule.

[Clinical pharmacology of hepatoprotectors]. / Klinichna farmakolohiia hepatoprotektoriv.

Data from published literature are summarized together with findings secured in the author's investigations on clinical pharmacology of hepatoprotectors. Classification of hepatoprotectors is submitted, their effects on the functional condition and metabolism in hepatocytes are discussed. Details are given of clinical and pharmacological properties of hepabene, legalon, essentiale, sirepara, wobenzime, phebichol, antral, thiotriazone.

Ionômero de vidro: agentes protetores de superfície / Glass ionomer: superficial protectors agents

O cimento de ionômero de vidro qualifica-se como um material bastante crítico quanto à sua utilizaçäo. A indicaçäo da proporçäo pó-líquido feita pelo fabricante deve ser rigorosamente obedecida. A manipulaçäo, inserçäo e proteçäo do material precisam ser feitas sempre de maneira apropriada. Foi pensando nisso, que este experimento de baseou, a fim de avaliar três diferentes protetores de superfície para restauraçöes de cimento de ionômero de vidro: Finishing Gloss (Vitrimer), Fortify e esmalte para unha Colorama. Os cimentos ionométricos utilizados para este experimento foram Vidrion R, Chelon Fil e Vitrimer. Os resultados indicaram que as melhores proteçöes foram obtidas quando se usou a resina fluída Finishing Gloss e esmalte para unha Colorama; näo havendo diferença significante entre eles. Já o Fortify näo deve ser o produto de primeira escolha para proteçäo superficial

Past and present scenario of hepatoprotectants.

The liver plays a significant role not only in metabolism and disposition of the chemicals to which it is exposed directly or indirectly but also plays a pivotal role in the metabolism of fats, carbohydrates, proteins and immunomodulations. The impairment of liver generally results from viral or portozoal infections, excessive use of alcohol, drugs and xenobiotics. This review provides an overall view about the past and present status of the hepatoprotectants resulted from synthetic and plant origins.