Extracts and Terpenoids from Stevia Species as Potential Anthelmintics for Neglected Tropical Diseases Caused by Cestode Parasites.

Cestodes are etiological agents of neglected diseases such as echinococcosis and cysticercosis, which are major public health problems. Antiparasitic treatment relies on a small number of approved drugs, which are often only partially effective, poorly tolerated and require prolonged administration. Thus, the discovery of novel potential treatments is critical. The Stevia genus (Asteraceae) includes species that are recognized as a source of bioactive compounds, with many species associated with medicinal uses. In this study, the cestocidal activity of four South American Stevia species that previously showed antiprotozoal activity was analyzed using a motility assay on the laboratory cestode model, Mesocestoides vogae. The four Stevia extracts showed cestocidal activity, with S. alpina var. alpina as the most active. The sesquiterpene lactones estafietin and eupatoriopicrin were purified from S. alpina var. alpina and S. maimarensis, respectively, and tested on M. vogae. Estafietin showed cestocidal activity, inhibiting parasite viability in a dose-dependent manner, even from the first day of incubation. Consistent with the motility effects, the extract of S. alpina var. alpina and estafietin induced marked alterations in the morphology of the parasite. The results of this report show that Stevia species represent a source of new molecules with potential for the treatment of neglected tropical diseases caused by cestodes.

Unraveling the Neuroprotective Effect of Natural Bioactive Compounds Involved in the Modulation of Ischemic Stroke by Network Pharmacology.

Ischemic stroke (IS) is one of the leading causes of mortality worldwide. It is characterized by the partial or total occlusion of arteries that supply blood to the brain, leading to the death of brain cells. In recent years, natural bioactive compounds (NBCs) have shown properties that ameliorate the injury after IS and improve the patient's outcome, which has proven to be a potential therapeutic strategy due to their neuroprotective effects. Hence, in the present study, we use both systems pharmacology and chemoinformatic analyses to identify which NBCs have the most potential to be used against IS in clinics. Our results identify that flavonoids and terpenoids are the most studied NBCs, and, mainly, salidrosides, ginkgolides A, B, C, and K, cordycepin, curcumin, baicalin, resveratrol, fucose, and cannabidiol, target the main pathological processes occurring in IS. However, the medicinal chemistry properties of such compounds demonstrate that only six fulfill such criteria. However, only cordycepin and salidroside possess properties as leader molecules, suggesting that these compounds may be considered in developing novel drugs against IS.

Effect of Gastrointestinal Digestion on the Bioaccessibility of Phenolic Compounds and Antioxidant Activity of Fermented Aloe vera Juices.

Plant-based beverages are enriched by the fermentation process. However, their biocompounds are transformed during gastrointestinal digestion, improving their bioaccessibility, which is of primary importance when considering the associated health benefits. This study aimed to evaluate the effect of in vitro gastrointestinal digestion on phenolic compound bioaccessibility and antioxidant activity of novel Aloe vera juices fermented by probiotic Enterococcus faecium and Lactococcus lactis. Aloe vera juices were digested using the standardized static INFOGEST protocol. During digestion, phenolic compounds and antioxidant activity (DPPH, ABTS, and FRAP) were accessed. The digestion process was seen to significantly increase the total phenolic content of the fermented Aloe vera juices. The fermentation of Aloe vera increased the bioaccessibility of juice biocompounds, particularly for kaempferol, ellagic acid, resveratrol, hesperidin, ferulic acid, and aloin. The phenolics released during digestion were able to reduce the oxidative radicals assessed by ABTS and FRAP tests, increasing the antioxidant action in the intestine, where they are absorbed. The fermentation of Aloe vera by probiotics is an excellent process to increase the bioavailability of beverages, resulting in natural added-value functional products.

The Role of Coffee and its Bioactive Components in Platelet Function and Aging.

Cardiovascular diseases (CVD) are known to be the world's leading cause of death and different factors are known to increase the risk of death, including aging, mainly due to increased oxidative stress and inflammation observed in older people. Acute myocardial infarctions and cerebrovascular accidents belong to CVD, and are the ones that cause the most deaths and disabilities, where greater platelet activation plays an important role in pathophysiology. These diseases are more prevalent in older people, which have a clear relationship with increased platelet function and are strongly related to aging. Platelet function is affected by diet, which varies in its requirements and characteristics according to age. Coffee belongs to the family of diet elements that can alter platelet function and an increase in coffee consumption with advancing age, and a U-shaped correlation with the risk of CVD have been reported. However, the effect of coffee consumption and its bioactive compounds on platelet function and aging presents controversial evidence, and therefore, a complex effect is not fully elucidated in the cardiovascular system. This review focuses on the relationship between coffee consumption (and its constituent bioactive compounds), and platelet function, and aging.

Toxicity and Anticancer Potential of Karwinskia: A Review.

Karwinskia genus consists of shrubs and small trees. Four toxic compounds have been isolated from Karwinskia plants, which were typified as dimeric anthracenones and named T496, T514, T516, and T544. Moreover, several related compounds have been isolated and characterized. Here we review the toxicity of the fruit of Karwinskia plants when ingested (accidentally or experimentally), as well as the toxicity of its isolated compounds. Additionally, we analyze the probable antineoplastic effect of T514. Toxins cause damage mainly to nervous system, liver, lung, and kidney. The pathophysiological mechanism has not been fully understood but includes metabolic and structural alterations that can lead cells to apoptosis or necrosis. T514 has shown selective toxicity in vitro against human cancer cells. T514 causes selective and irreversible damage to peroxisomes; for this reason, it was renamed peroxisomicine A1 (PA1). Since a significant number of malignant cell types contain fewer peroxisomes than normal cells, tumor cells would be more easily destroyed by PA1 than healthy cells. Inhibition of topoisomerase II has also been suggested to play a role in the effect of PA1 on malignant cells. More research is needed, but the evidence obtained so far indicates that PA1 could be an effective anticancer agent.

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.

High temperature and UV-C treatments affect stilbenoid accumulation and related gene expression levels in Gnetum parvifolium

Background: Gnetum parvifolium stems and roots have been used for a long time in traditional Chinese medicines. Stilbenes are bioactive compounds present in G. parvifolium plants, and they possess antioxidative and anticancer properties. However, little is known about the responses of G. parvifolium stilbene biosynthetic pathways to stress conditions. Therefore, we investigated stilbene biosynthesis, including the expression of relevant genes, in G. parvifolium exposed to high-temperature and ultraviolet-C treatments. Results: High temperatures did not influence the accumulation of total stilbenes in stems but decreased stilbene concentrations in roots at 3 h, with a subsequent restoration to control levels. In contrast, ultraviolet irradiation induced the accumulation of total stilbenes in stems but not in roots. We also observed that high temperatures inhibited the production of resveratrol and piceatannol in G. parvifolium stems and roots, whereas ultraviolet treatments initially inhibited their accumulation (up to 6 h) but induced their production at later time points. Analyses of specific genes (i.e., PAL, C4H, 4CL, STS, and CYP) revealed that their expression levels generally increased in stress-treated stems and roots, although there was some variability in the expression profiles during treatments. Conclusions: Our results indicated that high temperatures and ultraviolet irradiation differentially affect the biosynthesis of specific stilbenes in G. parvifolium stems and roots. Therefore, cultivating G. parvifolium seedlings under optimal stress conditions may increase the biosynthesis of specific stilbene compounds.

Mechanism of the anti-platelet effect of natural bioactive compounds: role of peroxisome proliferator-activated receptors activation.

Platelets are crucial mediators of the acute complications of atherosclerosis causing life-threatening ischemic events throughout plaque development. The inhibition of the platelet function has been used for a long time in an effort to prevent and treat cardiovascular diseases. However, morbidity and mortality figures indicate that current anti-platelet strategies are far from a panacea. In this context, a large number of natural bioactive compounds (NBCs) (polyphenols, terpenoids, alkaloids and fatty acids, among others) have been reported with apparent inhibitory activity on human platelets and each constituent may possess multiple targets. In this sense, the article describes how the mechanism of anti-platelet action by NBCs peroxisome proliferator-activated receptors agonists is mediated by inhibition of protein kinase-α, cyclooxygenase-1, thromboxane A2, cytosolic calcium, and indirect stimulation of protein kinase A (increased in cyclic adenosine monophosphate levels) and protein kinase G (increased in cyclic guanosine monophosphate levels).

ts e aplicações

In recent years, much interest has been focused on the biotechnological potential of microalgae, mainly due the identification of several substances synthesized by these organisms. The great biodiversity and consequent variability in the biochemical composition of the biomass obtained from the microalgal cultures, allied to the genetic improvement and to the establishment of technology in massive production, have allowed various species to be commercially cultivated. In this sense, microalgae cultivations have been developed aiming at the biomass production not only for use in the food elaboration but also for the obtainment of natural compounds with high value in the world market. Among the main extracted substances, or with potential of commercial exploration, can be related polyunsaturated fatty acids, carotenoids, phycobilins, polysaccharides, vitamins, sterols and several bioactive compounds (antioxidants, cholesterol reducers etc.), the which ones can be especially used in the development of functional food, for its nutritional and pharmaceutical properties.

Nos últimos anos, muito interesse tem sido focado no potencial biotecnológico das microalgas, principalmente devido à identificação de diversas substâncias sintetizadas por estes organismos. A imensa biodiversidade e conseqüente variabilidade na composição bioquímica da biomassa obtida das culturas microalgais, aliadas ao emprego de melhoramento genético e ao estabelecimento de tecnologia de cultivo em grande escala, vêm permitindo que determinadas espécies sejam comercialmente utilizadas. Nesse sentido, cultivos de microalgas têm sido realizados visando à produção de biomassa tanto para uso na elaboração de alimentos quanto para a obtenção de compostos naturais com alto valor no mercado mundial. Dentre os inúmeros compostos extraídos, ou com potencial de exploração comercial, podem ser relacionados ácidos graxos poliinsaturados, carotenóides, ficobilinas, polissacarídeos, vitaminas, esteróis e diversos compostos bioativos naturais (antioxidantes, redutores do colesterol etc.), os quais podem ser empregados especialmente no desenvolvimento de alimentos funcionais, por suas propriedades nutricionais e farmacêuticas.

ts e aplicações

In recent years, much interest has been focused on the biotechnological potential of microalgae, mainly due the identification of several substances synthesized by these organisms. The great biodiversity and consequent variability in the biochemical composition of the biomass obtained from the microalgal cultures, allied to the genetic improvement and to the establishment of technology in massive production, have allowed various species to be commercially cultivated. In this sense, microalgae cultivations have been developed aiming at the biomass production not only for use in the food elaboration but also for the obtainment of natural compounds with high value in the world market. Among the main extracted substances, or with potential of commercial exploration, can be related polyunsaturated fatty acids, carotenoids, phycobilins, polysaccharides, vitamins, sterols and several bioactive compounds (antioxidants, cholesterol reducers etc.), the which ones can be especially used in the development of functional food, for its nutritional and pharmaceutical properties.

Nos últimos anos, muito interesse tem sido focado no potencial biotecnológico das microalgas, principalmente devido à identificação de diversas substâncias sintetizadas por estes organismos. A imensa biodiversidade e conseqüente variabilidade na composição bioquímica da biomassa obtida das culturas microalgais, aliadas ao emprego de melhoramento genético e ao estabelecimento de tecnologia de cultivo em grande escala, vêm permitindo que determinadas espécies sejam comercialmente utilizadas. Nesse sentido, cultivos de microalgas têm sido realizados visando à produção de biomassa tanto para uso na elaboração de alimentos quanto para a obtenção de compostos naturais com alto valor no mercado mundial. Dentre os inúmeros compostos extraídos, ou com potencial de exploração comercial, podem ser relacionados ácidos graxos poliinsaturados, carotenóides, ficobilinas, polissacarídeos, vitaminas, esteróis e diversos compostos bioativos naturais (antioxidantes, redutores do colesterol etc.), os quais podem ser empregados especialmente no desenvolvimento de alimentos funcionais, por suas propriedades nutricionais e farmacêuticas.