Quality by Design approach for the investigation of critical characteristics of Phyllanthus emblica from different vicinities / 数字中医药（英文）

@#[Objective] To explore the application of Quality by Design (QbD) tools in assessing geographical variations of Phyllanthus emblica (P. emblica) from five distinct Indian states. [Methods] In the current experiment, the Box-Behnken design with a reduced quartic model and 105 runs was employed with the use of the Design Expert software for randomized response surface mapping. Three different extraction methods (Soxhlet, maceration, and sonication) along with three solventst [distilled water, methanol, and water-methanol mixture (50 : 50 v/v)] were considered in the present study. The anti-oxidant activities, total flavonoid content (TFC), and total phenolic content (TPC) in the P. emblica were determined and analysed by gas chromatography-mass spectrometry (GC-MS) to identify the major components. [Results] The QbD overlay plot showed that the extractive value of the P. emblica was no less than 30% w/w, 2,2-diphenyl-1-picrylhydrazyl (DPPH) no less than 60% mcg/mL (micrograms per millilitre), TFC no less than 75 mg QE/g (milligrams of quercetin equivalents per gram), and TPC no less than 80 mg GAE/g (milligrams of gallic acid equivalents per gram). Moreover, the GC-MS data confirmed the presence of variation in the bioactives of P. emblica extracts. [Conclusion] The model was significant in describing the variation in extractive value, DPPH, TFC, and TPC. The QbD approach may tend to prioritize thoroughness in the extraction process, ultimately resulting in improved quality in the extracted products.

Bauhinia spp. (pata-de-vaca) and its biological potentialities ­ literature review / Bauhinia spp. (pata-de-vaca) e suas potencialidades biológicas ­ revisão da literatura / Bauhinia spp. (pata-de-vaca) y sus potencialidades biológicas - revisión de la literatura

The genus Bauhinia popularly known as "pata-de-vaca", "unha de vaca", "unha de boi", "unha de anta" e "casco de vaca" is widely used in the form of teas and other herbal preparations. The aim of this literature review was to show the diversity and biological potential of Bauhinia species for health promotion. A search was carried out for articles listing some species of medical interest. The pharmacological activities of B. forficata were also highlighted in articles published in the last twenty years using the PubMed database. Research has shown that Bauhinia is used as a hypoglycemic and antidiabetic agent, diuretic, cholesterol reducer, in the treatment of cystitis, intestinal parasites, elephantiasis, tumors and other ailments, including infections and painful processes. In the last eleven years, 86% of the works carried out with B. forficata used the plant collected or acquired in Brazil, predominantly publications from the southern region of the country where almost 60% reported activity on diabetes and its complications and/or antioxidant effect. Despite the literature pointing out the great medicinal potential of Bauhinia in chronic diseases and their complications, there is still a need for more translational research.

O gênero Bauhinia conhecido popularmente como "pata-de-vaca", "unha de vaca", "unha de boi", "unha de anta" e "casco de vaca" é amplamente utilizado em forma de chás e outras preparações fitoterápicas. O objetivo desta revisão de literatura foi mostrar a diversidade e potencial biológico das espécies de Bauhinia para a promoção a saúde. Foi realizada a busca de artigos elencando algumas espécies de interesse médico. Destacou-se também as atividades farmacológicas de B. forficata em artigos publicados nos últimos vinte anos utilizando a base de dados PubMed. A pesquisa mostrou que a Bauhinia é utilizada como hipoglicemiante e antidiabética, diurética, redutora de colesterol, no tratamento da cistite, parasitoses intestinais, elefantíase, tumores e outros males, incluindo infecções e processos dolorosos. Nos últimos onze anos, 86% dos trabalhos realizados com B. forficata utilizaram a planta coletada ou adquirida no Brasil sendo predominante publicações oriundas da região sul do país onde quase 60% relataram atividade sobre o diabetes e suas complicações e/ou efeito antioxidante. Apesar da literatura apontar o grande potencial medicinal da Bauhinia em doenças crônicas e suas complicações ainda há a necessidade de mais pesquisas de caráter translacional.

El género Bauhinia, conocido popularmente como "garra de vaca", "garra de ganado", "garra de tapir" y "pezuña de vaca", se utiliza ampliamente como té y otros preparados fitoterapéuticos. El objetivo de esta revisión bibliográfica era mostrar la diversidad y el potencial biológico de las especies de Bauhinia para la promoción de la salud. Se llevó a cabo una búsqueda de artículos que incluyeran algunas especies de interés médico. Las actividades farmacológicas de B. forficata también fueron destacadas en artículos publicados en los últimos veinte años utilizando la base de datos PubMed. La investigación demostró que la Bauhinia se utiliza como hipoglucemiante y antidiabético, diurético, reductor del colesterol, en el tratamiento de la cistitis, la parasitosis intestinal, la elefantiasis, los tumores y otras dolencias, incluyendo infecciones y procesos dolorosos. En los últimos once años, el 86% de los estudios realizados con B. forficata utilizaron la planta recolectada o adquirida en Brasil, siendo predominantes las publicaciones de la región sur del país, donde casi el 60% reportó actividad sobre la diabetes y sus complicaciones y/o efecto antioxidante. Aunque la bibliografía señala el gran potencial medicinal de la Bauhinia en las enfermedades crónicas y sus complicaciones, todavía es necesario realizar más investigaciones traslacionales.

Efecto en la composición nutricional de huevos azules de gallinas criollas Huilliches mediante la inclusión de compuestos naturales del sur de Chile ricos en antioxidantes y omega 3 / Effect on the nutritional composition of blue eggs from Huilliche Creole hens through the inclusion of natural compounds from southern Chile rich in antioxidants and omega 3 / Efeito na composição nutricional de ovos azuis de galinhas crioulas Huilliche por meio da inclusão de compostos naturais do sul do Chile ricos em antioxidantes e ômega 3

Resumen El huevo es un alimento que presenta alto valor nutritivo, aporta elevada proporción de proteínas, vitaminas y minerales, relativamente bajo de energía, lo que lo convierte en un alimento con alta densidad de nutrientes. El objetivo de este estudio fue determinar el efecto de la inclusión de materias primas autóctonas del sur de Chile que contienen compuestos bioactivos en la alimentación de las gallinas criollas sobre la composición en ácidos grasos y capacidad antioxidante de sus huevos. Para esto, se elaboraron 8 dietas experimentales y una dieta de grano comercial y una dieta control, las dietas experimentales fueron formuladas en base a tres niveles de inclusión de fuentes de omega 3 (harina de salmón, chorito y microlaga) y tres niveles de fuentes de antioxidantes (harina de mora, frutilla y pepa de uva). El ensayo experimental tuvo duración de ocho semanas, donde se alimentaron 360 gallinas, distribuidas en 9 explotaciones avícolas. Al final de este período, los huevos de los tratamientos fueron liofilizados y se determinaron los ácidos grasos por cromatografía de gases y capacidad antioxidante por el método ABTS y DPPH. Los huevos, donde las gallinas fueron alimentadas con las dietas 7 y 8, compuestas por harina de alga y de pepa de uva, fueron aquellas que presentaron un mayor contenido del Ácido docosahexaenoico (DHA), 3,43 y 3,46 / 100 g respectivamente. Por otro lado, los huevos puestos por gallinas que se alimentaron de la dieta 5, compuestas por harina de salmón, chorito, mora y frutilla, fueron los que presentaron una mayor capacidad antioxidante.

Abstract The egg is a food that has high nutritional value, provides a high proportion of proteins, vitamins and minerals, relatively low in energy, which makes it a food with high nutrient density. The objective of this study was to determine the effect of the inclusion of native raw materials from southern Chile that contain bioactive compounds in the feed of Creole hens on the fatty acid composition and antioxidant capacity of their eggs. For this, 8 experimental diets were developed and a commercial grain diet and a control diet, the experimental diets were formulated based on three levels of inclusion of omega 3 sources (salmon meal, mussel and microlala) and three levels of sources of antioxidants (blackberry flour, strawberry and grape seed). The experimental trial lasted eight weeks, where 360 hens were fed, distributed in 9 poultry farms. At the end of this period, the eggs of the treatments were lyophilized and the fatty acids were determined by gas chromatography and antioxidant capacity by the ABTS and DPPH method. The eggs, where the hens were fed diets 7 and 8, composed of algae and grape seed meal, were those that presented a higher content of docosahexaenoic acid (DHA), 3.43 and 3.46 / 100 g respectively. On the other hand, the eggs laid by hens that were fed diet 5, composed of salmon meal, mussel, blackberry and strawberry, were those that presented the highest antioxidant capacity.

Resumo Os ovos têm alto valor nutricional, com uma alta proporção de proteínas, vitaminas e minerais, e uma ingestão energética relativamente baixa, tornando-os um alimento com alta densidade nutricional. Este estudo tem por objetivo analisar o efeito da inclusão de matérias-primas nativas do sul do Chile que contêm compostos bioativos na ração de galinhas crioulas sobre a composição de ácidos graxos e a capacidade antioxidante de seus ovos. Para tanto, foram elaboradas 8 dietas experimentais e uma dieta comercial de grãos, além de uma dieta controle. As dietas experimentais foram formuladas com base em três níveis de inclusão de fontes ômega 3 (farinhas de salmão, de mexilhão e de microalgas) e três níveis de fontes antioxidantes (farinhas de amora, de morango e de semente de uva). O ensaio experimental durou oito semanas. Durante o experimento, 360 galinhas em 9 granjas foram alimentadas com as dietas. Ao final desse período, os ovos dos tratamentos foram liofilizados, os ácidos graxos mensurados por cromatografia gasosa e a capacidade antioxidante, pelos métodos ABTS e DPPH. Os ovos de galinhas alimentadas com as dietas 7 e 8, compostas de farelo de algas e grainha de uva, apresentaram maior teor de ácido docosaexaenoico (DHA), 3,43 e 3,46 / 100 g, respectivamente. Por sua vez, os ovos postos por galinhas alimentadas com a dieta 5, composta por farinha de salmão, mexilhão, amora e morango, apresentaram a maior capacidade antioxidante.

Characterization of Seed Oils of Pterodon emarginatus Vogel (Sucupira) Obtained by Different Extraction Methods

Abstract The present study aims to evaluate the influence of extraction methods on the quality of bioactive compounds and antioxidant capacity in Pterodon emarginatusVogel (sucupira) oils. The oils were extracted from the sucupira seeds by Soxhlet and by the extraction system of Bligh & Dyer. The oils were analyzed as to fatty acid profile, tocopherols, phytosterols, carotenoids, total phenolics, and total antioxidant capacity. The extraction by Soxhlet showed better yield of total lipids and was more efficient to extract tocopherols, phytosterols, and carotenoids, besides presenting better antioxidant activity by DPPH•. However, this method showed insufficient capacity to extract the polar lipid components of the sample, as evidenced by the low results of total phenolic compounds. On the other hand, the Bligh & Dyer method preserved the fatty acid profile and was also effective to extract higher phenolic compounds content and presented superior antioxidant activity when assessed by FRAP, ABTS•+, and oxidative stability index.

Methanolic extract of Euchelus asper exhibits in-ovo anti-angiogenic and in vitro anti-proliferative activities

BACKGROUND: The marine environment is a rich source of bioactive natural products. Many of the marine bioactive compounds have been derived successfully from molluscs. Euchelus asper is a marine mollusc which is commonly found in the intertidal rocky regions of the Mumbai coast. The present study was focused on evaluating the anti-angiogenic and anti- proliferative activities of methanolic extract of Euchelus asper (EAME). METHODS: The anti-angiogenic activity of EAME (50-800 µg/mL) was assessed by chick chorio-allantoic membrane (CAM) model wherein multiple parameters in the CAM blood vessels were analysed through morphometric and histo-logical investigations. In vitro testing of EAME (5-20 µg/mL) included its cytotoxicity against three different cancer cell lines, its effect on cell proliferation by wound healing assay as well as their relevant molecular mechanisms. Statistical analysis was carried out by two-tailed student's t test for two unpaired groups. RESULTS: Analysis of CAM revealed that the extract is effective in reducing the branching points of the 1st order blood vessels or capillaries of CAM. Histological analysis of CAM showed significant decrease in capillary plexus and compartmentalization along with increase in mesodermal blood vessels, thus establishing its anti-angiogenicity. Further, EAME exhibited moderate but significant cytotoxicity against A549 non-small cell lung carcinoma cell line. We also demonstrated that the cytotoxicity of EAME in A549 was associated with its apoptotic activity by subG1 phase arrest. Lastly, EAME significantly reduced A549 proliferation by reducing the expression of Matrix metalloproteinase-2 (MMP-2) and Matrix metalloproteinase-9 (MMP-9). CONCLUSION: Overall, our study suggested that EAME has potential to inhibit tumour angiogenic and proliferative activity and may be a potential source for development of new anti-cancer pharmaceuticals.

Blackberry Vinegar Produced By Successive Acetification Cycles: Production, Characterization And Bioactivity Parameters

ABSTRACT: Blackberry vinegar was produced in successive acetification cycles and content of total phenolics, anthocyanins and antioxidant activity were evaluated along the production. Firstly, blackberry wine was obtained in bench-scale bioreactor, being verified 0.39 g/g ethanol yield, 1.78 g/L.h volumetric productivity and 76% efficiency. After, three successive acetification cycles were conducted efficiently in grapia barrel with average acetic acid production of 51.6 g/L, 72.2 % acetic acid yield and 0.4 g/L.h volumetric productivity. Appreciable contents of polyphenolic compounds, anthocyanins and high antioxidant activity were observed in the raw material, wine and vinegar obtained in each cycle of acetic acid transformation. Acetic acid transformation led the small reduction of antioxidant activity compared to alcoholic fermentation, but the antioxidant potential was maintained along the cycles. The content of total phenolics and anthocyanins also suffered a reduction in step of acetification.

Efeito de diferentes técnicas extrativas no rendimento, atividade antioxidante, doseamentos totais e no perfil por clae-dad de dicksonia sellowiana (presl. ). Hook, dicksoniaceae / Effect of different extraction techniques on the yield, antioxidant activity, total dosages, and profile by hplc-dad of Dicksonia sellowiana (Presl. ). Hook, dicksoniaceae.

RESUMO A espécie Dicksonia sellowiana, conhecida popularmente como xaxim, é uma samambaia natural do continente americano e encontrada no Brasil na Mata Atlântica. Em 2001 sua utilização para confecção de vasos para jardinagem foi proibida, e a mesma foi inserida na lista do IBAMA como espécie ameaçada de extinção. O presente trabalho descreve o efeito de diferentes técnicas de extração, incluindo ultra-som, turbólise, maceração, infusão, decocto e soxhlet utilizando etanol e solvente hidroalcoólico 70%, sob aspectos físicos e químicos. Foi avaliado o rendimento de cada extração, o perfil por CLAE-DAD, o conteúdo de polifenóis, flavonoides, proantocianidinas e esteroides além das atividades antioxidantes pelos métodos DPPH e redução do complexo fosfomolibdênio. Os dados foram avaliados estatisticamente através de desvio padrão, Tuckey e PCA. Os resultados demonstraram que a extração por Soxhlet utilizando ambos os solventes é a que possui maior rendimento final, porém o rendimento não está diretamente relacionado com o aumento nos teores de bioativos totais e atividades antioxidantes. As extrações por decocção e turbólise utilizando solvente hidroalcoólico foram as que apresentaram melhores resultados nos teores totais e na atividade antioxidante, resultados que ficam evidentes quando avaliados por PCA, demonstrando que este solvente e estas extrações são mais seletivas no estudo proposto.

ABSTRACT The species Dicksonia sellowiana, popularly known as xaxim, is a fern native to the Americas and found in Brazil in the Atlantic Forest. In 2001, its use for making gardening pots was banned, and it was added to the IBAMA [Brazilian Institute of the Environment and Renewable Natural Resources] list as an endangered species. This paper describes the effect of different extraction techniques – including ultrasound, turbolysis, maceration, infusion, decoction, and soxhlet using ethanol and 70% hydroalcoholic solvent on its physical and chemical aspects. The yield of each extraction was evaluated, as well as the profile by HPLC-DAD, the polyphenol content, flavonoids, proanthocyanidins, and steroids, in addition to the antioxidant activities through the DPPH and phosphomolybdenum complex reduction methods. The data were statistically analyzed through standard deviation, Tukey, and PCA. The results showed that the soxhlet extraction using both solvents had the highest overall yield; however, the yield is not directly related to the increase in total bioactive content and antioxidant activities. Extractions by decoction and turbolysis using a hydroalcoholic solvent exhibited the best results in total content and antioxidant activity – results that are evident when evaluated through PCA, demonstrating that this solvent and these extractions are the most selective in the proposed study.

Prospecção de bioativos farmacológicos em algas marinhas Rhodophyta e Heterokontophyta e avaliação de citotoxicidade / Prospection of pharmaceutical bioactive compounds in marine algae Rhodophyta and Heterokontophyta and cytotoxicity evaluation

Muitas drogas terapêuticas produzidas pela indústria farmacêutica são estruturas químicas isoladas de organismos encontrados na natureza ou moléculas baseadas nelas. Podem ser incluídas nesse grupo drogas isoladas de organismos marinhos, como corais, esponjas e algas marinhas, conhecidos como produtores de grandes quantidades de metabólitos secundários. Com base neste fato o presente estudo teve como objetivo realizar a prospecção de moléculas bioativas com propósito farmacológico, em extratos de algas marinhas vermelhas (Rhodophyta) e pardas (Heterokontophyta) coletadas no litoral brasileiro. A prospecção foi realizada por meio de avaliação de seus potenciais antioxidante, antibacteriano, antifúngico, anticancerígeno, e antiparasitário contra organismos causadores de leishmaniose e esquistossomose. Para as avaliações foram empregadas os extratos supercríticos de 5 espécies diferentes, sendo 2 pardas: Dictyota dichotoma e D. menstrualis e três vermelhas: Chondria littoralis, Spyridia hypnoides e Plocamium brasiliense. Os extratos foram avaliados quanto aos seus potenciais bioativos e os resultados mais promissores foram selecionados para as etapas seguintes do fracionamento. Em uma avaliação geral os extratos apresentaram bons resultados e representam uma potencial fonte de bioativos. Os extratos das espécies de D. dichotoma e D. menstrualis foram então submetidos a um procedimento de fracionamento bioguiado pela atividade esquistossomicida. Incorporou-se ainda um terceiro extrato de D. mertensii aos estudos e todas as etapas do fracionamento foram monitoradas por LC-MS. Comparando-se as massas detectadas em todas as frações que apresentaram atividade, para os 3 extratos, foi verificado que a substância de m/z 271,24 estava presente em todas elas, portanto os procedimentos de isolamento foram direcionados a esta molécula para a qual foi possível isolar 7 mg. Diferentemente do que era esperado a molécula quando avaliada isoladamente não apresentou atividade esquistossomicida, levando a hipótese de que a atividade seja decorrente de uma molécula diferente para cada espécie ou ainda que a mesma seja decorrente de uma interação com outras substâncias por um mecanismo de ação aditivo ou sinérgico. O trabalho avaliado de forma geral apresentou resultados promissores e representa um grande embasamento para servir como base para posteriores trabalho de fracionamento

Several therapeutic drugs manufactured by the pharmaceutical industry are chemical structures isolated from organisms that are found in nature or molecules based on that. May be included at this group drugs isolated from marine organisms, like corals, sponges and seaweeds, known as great secondary metabolites producers. Based on this facts the objective of the present study is to perform a prospection study to achieve bioactive molecules with pharmaceutical purposes, on extracts made from red (Rhodophyta) and brown (Heterokontophyta) seaweed collected in the Brazilian shore. The prospection studies was performed by means of evaluation of the antioxidant, antibacterial, antifungal, anticancer and antiparasitic (against Leishmania and Schistosoma) potential. In the evaluation were tested the supercritical extracts of 5 different species, including 2 brown species: Dictyota dichotoma and D. menstrualis and 3 red species: Chondria littoralis, Spyridia hypnoides and Plocamium brasiliense. The extracts were evaluated by their potential bioactive compounds and the most promising results were selected for the following fractionation steps. Overall the extracts have shown good results and may be represent a potential source of bioactive molecules. The extracts of both D. dichotoma and D. menstrualis were submitted to a bioguided fractionation process by their antischistosomal activities. It was still included a third extract from D. mertensii to the studies and every step was monitored by LC-MS techniques. Comparing the detected mass for each active fraction, it was observed the presence of a substance with m/z 271,24 in all of the extracts, so the isolating procedures were directed to obtain that specific molecule, which was obtained in a biomass of 7 mg. Differently than expected the molecule when evaluated isolated do not show the antischistosomal activity, leading to the hypothesis that the activity was related to different molecules for each species or even the observed effect is resulted by an interaction mechanism with another substances by an additive or synergist mechanism. The overall evaluation of the whole work show some promising results and it represent a great support for future fractionation works

ACTIVO-I Study Report - A Retrospective Prescription Event Monitoring for Safety and Efficacy of Waist Circumference in the Management of Overweight and Obesity.

The study was conducted on the combination of bioactive ingredients [Bioactives; Hoodia Gordonii, Hydroxycitric Acid (the active ingredient in Garcinia cambogia), Green tea extract, Ginger extract and Piperine] to estimate its safety and efficacy in decreasing the body weight (BW), body mass index (BMI) and waist circumference (WC) after treatment. Design and methods: The study was retrospective prescription event monitoring study. Total 99 overweight and obese patients (52 males and 47 females; mean age 45.45 ± 10.20 years) were enrolled in the study. Subjects were administered one capsule of Bioactives orally one hour before lunch and dinner daily for 90 days. All subjects were given standard advice regarding healthy food choices in their diet and physical activity. However, subjects were not advised to restrict dietary calorie intake. Clinical examination, BW, BMI and WC were estimated in all subjects at baseline and at the end of 30, 60 and 90 days. Observations: Bioactives was found to be significantly effective in decreasing BW by 4.36%, 7.12 % and 10.25% at 30, 60 and 90 days respectively and these results were statistically significant (p = 0.002, p <0.0001 and p <0.0001 respectively). BMI was also reduced with Bioactives by 5.11%, 9.83% and 11.88% at 30, 60 and 90 days respectively and results were statistically significant (p <0.0001, p <0.0001 and p <0.0001 respectively). Bioactives was found to be significantly effective in decreasing WC by 3.28%, 5.29% and 7.31% at 30, 60 and 90 days respectively and these results were statistically significant (p = 0.0023, p <0.0001 and p <0.0001 respectively). Bioactives can be rated as good to very good based on results observed on 66% patients. Side effect or adverse event was not reported in any case. Conclusion: Bioactives appears to be significantly effective in decreasing the BW, BMI and WC within 30, 60 and 90 days in overweight and obese patients. Bioactives has excellent tolerability as adverse event was not reported in any case.

The inhibitory effect of natural bioactives on the growth of pathogenic bacteria

The objective of this study was to evaluate the inhibitory activity of natural products, against growth of Escherichia coli (ATCC 25922) and Salmonella typhimurium (KCCM 11862). Chitosan, epigallocatechin gallate (EGCG), and garlic were used as natural bioactives for antibacterial activity. The testing method was carried out according to the disk diffusion method. All of chitosan, EGCG, and garlic showed inhibitory effect against the growth of E. coli and Salmonella typhi. To evaluate the antibacterial activity of natural products during storage, chicken skins were inoculated with 106 of E. coli or Salmonella typhi. The inoculated chicken skins, treated with 0.5, 1, or 2% natural bioactives, were stored during 8 day at 4degrees C. The numbers of microorganisms were measured at 8 day. Both chitosan and EGCG showed significant decrease in the number of E. coli and Salmonella typhi in dose dependent manner (P < 0.05). These results suggest that natural bioactives such as chitosan, EGCG may be possible to be used as antimicrobial agents for the improvement of food safety.