Innovative Cosmeceutical Ingredients: Harnessing Selenosugar-Linked Hydroxycinnamic Acids for Antioxidant and Wound-Healing Properties.

Selenosugars are gaining growing interest due to their antioxidant efficacy, and their ability to inhibit glycosidases, repair skin tissue or reduce endothelial dysfunction. Among selenosugars, those in which selenium replaces heterocyclic oxygen in a 5-membered sugar were our focus, and their coupling with phenolic compounds appears to be a strategy aimed at producing new compounds with enhanced antioxidant efficacy. In this context, the Mitsunobu reaction has been advantageously explored to obtain trans-p-coumaroyl-1,4-deoxy-2,3-O-isopropylidene-4-seleno-d-ribose, trans-caffeoyl-1,4-deoxy-2,3-O-isopropylidene-4-seleno-d-ribose, and trans-feruloyl-1,4-deoxy-2,3-O-isopropylidene-4-seleno-d-ribose. These compounds underwent removal of the iso-propylidene group, to provide the corresponding hydroxycinnamoyl-1,4-deoxy-4-seleno-d-ribose. All compounds were characterized by Nuclear Magnetic Resonance (NMR) spectroscopy and High-Resolution Mass Spectrometry (HRMS). This latter technique was pivotal for ensuing cellular metabolomics analyses. In fact, after evaluating the anti-radical efficacy through 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) methods, which underline the massive role of the phenolic moiety in establishing efficacy, the compounds, whose cytotoxicity was first screened in two highly oxidative-stress-sensitive cells, were tested for their wound healing properties towards human HaCaT keratinocytes cells. Caffeoyl- and feruloyl selenosugars exerted a dose-dependent repair activity, while, as highlighted by the metabolomic approach, they were poorly taken up within the cells.

Lavandula austroapennina: Assessment of the Antiviral Activity of Lipophilic Extracts from Its Organs.

In a framework aimed at the recovery and enhancement of medicinal plants endemic to the territory of the Cilento and Vallo di Diano National Park, Lavandula austroapennina N.G. Passal., Tundis and Upson has aroused interest. An insight into the chemical composition of the corolla, calyx, leaf, stem, and root organs was carried out following ultrasound-assisted maceration in n-hexane. The obtained lipophilic extracts were explored using ultra-high-performance chromatography coupled to high-resolution mass spectrometry (UHPLC-ESI-QqTOF-MS/MS). The extracts from the different organs varied in their relative content of fatty acids, ursanes, and oleanane-type triterpenes. In particular, the oleanolic acid content appeared to increase in the order of corolla < leaf < stem. An MTT assay was performed to verify the possible cytotoxicity of the organ extracts of L. austroapennina at a concentration ranging from 12.5 to 400 µg/mL on the Vero CCL-81 cell line. Antiviral activity against herpes simplex virus type 1 (HSV-1), alpha human coronavirus 229E (HCoV-229E), and poliovirus type 1 (PV-1) was evaluated via a plaque reduction assay in the same cellular model. All the extracts did not show cytotoxic effects after 2 and 24 h exposure times, and the antiviral efficacy was particularly important for the stem extract, capable of completely inhibiting the tested viruses at low doses. The antiviral activity in a non-enveloped virus PV-1 allowed the assertion that the extracts from the organs of L. austroapennina, and especially the stem extract, interfered directly with the viral envelope. This study underlines how much knowledge of a territory's medicinal plant heritage is a harbinger of promising discoveries in the health field.

Lavandula austroapennina (Lamiaceae): Getting Insights into Bioactive Polyphenols of a Rare Italian Endemic Vascular Plant.

Lavandula austroapennina N.G. Passal., Tundis and Upon has recently been described as a new species endemic to the southern Apennines (Italy). Locally, this species has a long ethnobotanical tradition of use for curative and decoration purposes and has been the protagonist of a flourishing essential oil production chain. Currently, while this tradition has long since ended, attention to the species is necessary, with a view to enhancing marginal and rural areas, as a recovery of a precious resource to (i) get insights into its (poly)phenolic fraction and (ii) address new and innovative uses of all its organs in various application fields (e.g., cosmeceutical sector). Therefore, after field sampling and dissection of its organs (i.e., corolla, calyx, leaf, stem and root), the latter, previously deterpenated and defatted, were subjected to accelerated ultrasound extraction and the related alcoholic extracts were obtained. Chemical composition, explored by UHPLC-QqTOF-MS/MS, and the following multivariate data analysis showed that the hydroxycinnamoyl derivatives are abundant in the leaf, stem and root, while flavonoids are more present in corolla and calyx. In particular, coumaroyl flavonoids with glyconic portion containing also hexuronyl moieties differentiated corolla organ, while yunnaneic acid D isomers and esculin distinguished root. When antiradical and reducing properties were evaluated (by means of ABTS, DPPH and PFRAP tests), a similar clustering of organs was achieved and the marked antioxidant efficacy of leaf, stem and root extracts was found. Thus, following cytotoxicity screening by MTT test on HaCaT keratinocytes, the protective effects of the organ extracts were assessed by wound closure observed after the scratch test. In addition, the extracts from corolla, leaf and stem were particularly active at low doses inducing rapid wound closure on HaCaT cells at a concentration of 1 µg/mL. The diversity in (poly)phenols of each organ and the promising bioactivity preliminarily assessed suggest further investigation to be carried out to fully recover and valorize this precious endemic vascular plant.

LC-HR/MS Analysis of Lipophilic Extracts from Calendula arvensis (Vaill.) L. Organs: An Unexplored Source in Cosmeceuticals.

As part of a project aimed at promoting the use of Calendula arvensis (Vaill.) L. (field marigold, Asteraceae) phytocomplexes in cosmeceutical formulations, the chemical composition in apolar specialized metabolites is herein elucidated. Furthermore, the screening of the cytotoxicity of the apolar extracts was evaluated in order to underline their safety as functional ingredients for cosmetics. After dissection of Calendula organs (florets, fruits, leaves, bracts, stems, and roots), ultrasound-assisted maceration in n-hexane as an extracting solvent allowed us to obtain oil-like mixtures, whose chemical composition has been highlighted through a UHPLC-ESI-QqTOF-MS/MS approach. Twenty-nine metabolites were tentatively identified; different compounds, among which the well-known poly-unsaturated fatty acids, and oxylipins and phosphatides were detected for the first time in Calendula genus. The screening of the dose-response cytotoxicity of the apolar extracts of C. arvensis highlighted the concentration of 10 µg/mL as the most suitable for the formulation of cosmeceutical preparations. Sera enriched with leaf and fruit apolar extracts turned out to have the best activity, suggesting it can be used as a new source in skin care thanks to their higher content in fatty acids.

Ready-to-Use Nutraceutical Formulations from Edible and Waste Organs of Algerian Artichokes.

Edible, plant-derived foodstuffs are recognized as precious sources of polyphenol compounds, whose consumption has proven to have multiple beneficial effects on human health. However, the awareness that cooking processes are able to induce quali-quantitatively changes in their native occurrence and that their bioavailability after food ingestion is poor led the research to move toward the preparation of nutraceutical supplements aimed at maximizing their content by effective extractive techniques and protecting them from degradation. The present work fits into this context, proposing a green, ready-to-use formulation of capitula, stems, and leaves of Algerian artichokes, in which natural deep eutectic solvents were exploited as extracting solvents but not removed at the end of the process. MTT test on the Caco-2 cell line highlighted that mitochondrial redox activity inhibition was absent below the 50 µg/mL tested dose. Simulated in vitro digestion was used as a predictive model for formulation bioaccessibility, where the joint approach with UHPLC-HRMS techniques allowed to define the release of each polyphenol from the investigated matrices. The capitula-based sample was the richest one in flavonoids, especially luteolin and apigenin glycosides, which survived in the intestinal digesta. On the contrary, simple phenols characterized the stem sample, whose release was mainly in the gastric chyme.

Calendula arvensis (Vaill.) L.: A Systematic Plant Analysis of the Polar Extracts from Its Organs by UHPLC-HRMS.

Calendula arvensis (Vaill.) L. (field marigold, Asteraceae) is an alimurgic plant, whose flowers and leaves are a common part of local food dishes. The diversity in polar specialized metabolites is herein unraveled, with the aim to further promote and valorize the food use of the plant. To this purpose, following the plant dissection of its organs (florets, fruits, leaves, bracts, stems, and roots), ultrasound assisted maceration has been employed in order to recover phenols and polyphenols. Through an untargeted UHPLC-HR MS (Ultra-High-Performance Liquid Chromatography-High-Resolution Mass Spectrometry) approach, and deeper investigation of the fragmentation patterns of each compound by tandem mass spectrometry, the florets' constitution in triterpene saponins and flavonol glycosides has been highlighted, whereas hydroxycinnamoyl compounds are mainly in bracts and fruits. The antiradical and reducing capabilities of the organs' extracts have been assessed, and data acquired have been analyzed by cluster analysis, which allowed bracts and fruits to be observed, despite their negligible food use, as the most active extracts. Chemical and antioxidant data on the diverse organs of field marigold suggest new investigative food and nutraceutical scenarios of this plant, also revalorizing and preserving its traditional uses.

Encapsulating Calendula arvensis (Vaill.) L. Florets: UHPLC-HRMS Insights into Bioactive Compounds Preservation and Oral Bioaccessibility.

Wild edible plants, once consumed in times of famine or for health purposes, today represent an interesting dietary supplement, aimed at enriching local dishes and/or formulating healthy nutraceutical products. In fact, the broad content of different, and diversely bioactive, specialized metabolites therein suggests new scenarios of use which, in order to be as functional as possible, must maximize the bioactivity of these compounds while preserving their chemistry. In this context, based on a recent investigation on the metabolic profile of the organs of Calendula arvensis that highlighted that florets are abundant in flavonol glycosides and triterpene saponins, the freeze-drying encapsulation of their alcoholic extract (FE) into maltodextrin (MD) was investigated. FE-MD chemical composition was evaluated using Fourier Transform InfraRed spectroscopy (FTIR), while ultra-high performance liquid chromatography coupled with high-resolution tandem mass spectrometry (UHPLC-HRMS/MS) techniques were employed to unravel FE compound preservation also during in vitro simulated digestion. The establishment of H-bonds between FE compounds and MD hydroxyl groups was in line with FE-MD biocompatibility in Caco-2 cells, while in vitro digestion mostly affected structural integrity and/or diversity. Flavonol compounds underwent deglycosylation and demethylation, while deacylation, beyond oxidation, involved triterpene saponins, which massively preserve their aglycone core.

Combined Exercise Training Performed by Elderly Women Reduces Redox Indexes and Proinflammatory Cytokines Related to Atherogenesis.

Cardiovascular benefits for the general population of combined aerobic-resistance exercise training are well-known, but the impact of this exercise training modality on the plasma lipid, inflammatory, and antioxidant status in elderly women that are exposed to a great risk of developing ischemic cardio- and cerebrovascular diseases has not been well investigated. So, we aimed to evaluate the plasma lipids, oxidative stress, and inflammatory cytokines in 27 elderly women (TRAINED group, 69.1 ± 8.1 yrs) that were performing moderate intensity combined aerobic-resistance exercise training (3 times/week for at least 18 months) and in 27 sedentary elderly women (SED group, 72.0 ± 6.4 yrs), not submitted to exercise training for at least 5 yrs. Our results showed that BMI was lower in the TRAINED group than in the SED group (25.1 ± 3.2 vs. 28.7 ± 5.1, p < 0.05). The TRAINED group had lower glycemia (92 ± 3 vs. 118 ± 12, p < 0.05), glycated hemoglobin (5.9 ± 0.1 vs. 6.4 ± 0.2, p < 0.05), and triglycerides (98 (75-122) vs. 139 (109-214), p < 0.01); equal total cholesterol (199 (175-230) vs. 194 (165-220)), LDL-cholesterol (108 (83-133) vs. 109 (98-136)), and non-HDL-cholesterol (54 (30-74) vs. 62 (26-80)); and also higher HDL-cholesterol (64 (52-77) vs. 52 (44-63), p < 0.01) and LDL-C/oxLDL ratio (13378 ± 2570 vs. 11639 ± 3113, p < 0.05) compared to the SED group. Proinflammatory cytokines as IL-1ß (11.31 ± 2.4 vs. 28.01 ± 4.7, p < 0.05), IL-6 (26.25 ± 7.4 vs. 49.41 ± 17.8, p < 0.05), and TNF-α (25.72 ± 2.8 vs. 51.73 ± 4.2, p < 0.05) were lower in the TRAINED group than in the SED group. The TRAINED group had lower total peroxides (26.3 ± 7.4 vs. 49.0 ± 17.8, p < 0.05) and oxidized LDL (1551 ± 50.33 vs. 1773 ± 74, p < 0.02) and higher total antioxidant capacity (26.25 ± 7.4 vs. 49.41 ± 17.8, p < 0.001) compared to the SED group. In conclusion, in TRAINED women, BMI was lower, plasma lipid profile was better, plasma oxidative stress was diminished, and there was less expression of proinflammatory interleukins than in SED, suggesting that combined aerobic-resistance exercise training may promote the protection against the complications of ischemic cardio- and cerebrovascular disease in elderly women.

Dyslipidemia: evidence of efficacy of the pharmacological and non-pharmacological treatment in the elderly.

THE CLINICAL DECISION TO CONTROL RISK FACTORS FOR CARDIOVASCULAR DISEASE (CVD) IN THE ELDERLY TAKES THE FOLLOWINGS INTO CONSIDERATION: (1) the elderly life expectancy; (2) the elderly biological age and functional capacity; (3) the role of cardiovascular disease in the elderly group; (4) the prevalence of risk factors in the elderly; and (5) The effectiveness of treatment of risk factors in the elderly. A large number of studies showed the efficacy of secondary and primary prevention of dyslipidemia in the elderly. However, the only trial that included patients over 80 years was the Heart Protection Study (HPS). Statins are considered the first line therapy for lowering low-density lipoprotein cholesterol (LDL-C). Because lifestyle changes are very difficult to achieve, doctors in general tend to prescribe many drugs to control cardiovascular risk factors. However, healthy food consumption remains a cornerstone in primary and secondary cardiovascular prevention and should be implemented by everyone.

Envelhecimento e risco cardiovascular: como prevenir / Aging and cardiovascular risk: how to prevent

O envelhecimento é inevitável. O que é evitável, no entanto, é o chamado envelhecimento mal-sucedido, com aumento de morbidades e redução na expectativa de vida ativa. As doenças cardiovasculares representam a principal causa de incapacidade e mortalidade entre os idosos. A doença aterosclerótica, tanto coronária como encefálica ou periférica, tem na hipertensão arterial, dislipidemia, diabete melito, sedentarismo e tabagismo seus maiores fatores causais ou de risco modificáveis por meio de intervenção terapêutica ou corpontamental. A sensibilização dos indivíduos pelo conhecimento pode predispô-lo a aderir ao tripé de medidas intervencionistas no chamado estilo de vida: a saber, abandono do tabagismo, mudança de hábito nutricionais, prática de atividade física...

Peculiaridades da farmacoterapêutica cardiovascular no idoso / Peculiarities of the cardiovascular pharmacotherapeutic in the elderly

O incremento da população geriátrica representa importante alteração demográfica do final do século XX e início do XXI. Como um grupo, idosos requerem cuidados médicos e terapêuticos mais freqüentes e utilizam o serviço de saúde em maior escala que indivíduos mais jovens. Essa revolução demográfica tem importantes implicações práticas, diagnósticas e terapêuticas. A utilização apropriada de medicamentos na população geriátrica requer o conhecimento das alterações fisiológicas do envelhecimento e dos efeitos das doenças concomitantes, que podem influenciar a farmacocinética e a farmacodinâmica, assim como das respostas terapêutica e tóxica aos medicamentos, de forma clinicamente importante. A falta de atenção cuidadosa na seleção, na posologia e na monitoração dos fármacos nessa população pode induzir benefício terapêutico incompleto e alta incidência de reações adversas. Isso é particularmente significante para os medicamentos cardiovasculares, muitos dos quais têm índice tóxico/terapêutico estreito. Como as idades cronológica e biológica freqüentemente não são comparáveis, e como existem grandes variações entre os idosos nas respostas farmacocinética e farmacodinâmica, é difícil estabelecer generalizações. Fatores socioeconômicos e a não-observância adequada da prescrição são causa importante da falha terapêutica em qualquer idade, e particularmente nos idosos. Polifarmácia, esquemas terapêuticos complicados, distúrbios visuais, auditivos ou mentais, falta de compreensão, ausência de auxílio de familiares ou afins são alguns dos muitos fatores que contribuem para a não-observância ao tratamento.

The increase of the geriatric population represents a major demographic change in the end of the 20th Century and beginning of the 21st. As a group, the elderly require a closer and more frequent medical and therapeutic care and use health services in a larger scale than younger individuals. Such demographic revolution comprehends major practical, diagnostic and therapeutic implications. The appropriate use of medication in the geriatric population requires knowledge on the physiologic changing of the aging and on the effects of the collateral diseases that may impact on the pharmacokinetics and pharmacodynamics, the therapeutic and toxic response to medication, in a substantial clinical way. The lack of careful attention in the selection, posology and monitoring of the pharmaceutical drugs in this population may incite an incomplete therapeutic benefit and a high occurrence of conflicting reactions. This is particularly meaningful in the case of cardiovascular medication, many of which have a very critical toxic/therapeutic rate. Since the chronologic and biologic ages are usually not comparable, and since there are great variation among the elderly in the harmacokinetics and pharmacodynamics responses, it is difficult to establish generalization. Social and economical factors as well as the non-observance of adequate prescription are major reasons for therapeutic failure in any age, and particularly with the elderly. Polypharmacy, complicated therapeutic schemes, visual, hearing or mental impairment, lack of comprehension, absence of assistance from family members or relatives, are some of the many factors that contribute for non-observance of treatment.

Tratamento não-medicamentoso da hipertensão no idoso / Non-pharmacological treatment of hypertension in the elderly

O tratamento não-farmacológico da hipertensão arterial no idoso é realizado por meio de mudanças no estilo de vida. Essas mudanças podem prevenir ou retardar a instalação de hipertensão em idosos pré-hipertensos e reduzir níveis pressóricos elevados em idosos hipertensos. Entretanto, mudanças do comportamento habitual adquirido ao longo da vida não são facilmente realizadas, pois exigem disciplina e paciência para obter resultados. Além disso, é necessário que o idoso receba orientação e conscientização da importância do controle desses fatores para que se motive a executar tais mudanças comportamentais.As principais modificações no estilo de vida que podem reduzir a pressão arterial são: a prática de atividade física e a mudança de hábitos nutricionais. A atividade física deve ser de fácil realização, com exercícios de curta duração e baixa intensidade, visando desenvolver a resistência, flexibilidade articular e força muscular sem provocar lesões, e pode ser fracionada ao longo do dia, com aumento gradativo do tempo e da intensidade do exercício. Os hábitos nutricionais devem visar à redução c de sódio e ao controle de peso. A pressão arterial aumenta progressivamente à medida que o índice de massa corporal aumenta. O idoso obeso ou com sobrepeso se beneficiará com a redução de peso tanto quanto o jovem. Recomenda-se um programa de redução de peso que E inclua atividade física e restrição de calorias para idosos com 10 acima de seu peso ideal, além de redução do sal da dieta para 2,4 g de sódio ou 6 g de cloreto de sódio (correspondente a uma colher de chá).

Implantable cardioverter-defibrillators: expectations in the Brazilian elderly.

By 2025, Brazil will have the sixth largest elderly population in the world. Thirty percent of the elderly currently have private health insurance and 70% have their health care paid for by the Unified Health System. The system, founded through a governmental entity, provides free health service to all citizens. In 2003, the government passed the Elderly Statement Law, claiming that the elderly have equal access to prevention, promotion, protection, and recovery of health. In spite of the high costs, the placement of implantable cardioverter-defibrillators (ICDs) in the elderly is growing. There is a significant regional difference in the number of ICD placements, and there is also a significant sex bias: 73% of the ICDs were placed in elderly men. The majority of ICDs were placed in the elderly from ages 65 to 79 years. Nevertheless, 9.5% of ICDs were placed in octogenarians and nonagenarians, reflecting the valuation of biologic age rather than chronologic age.