Chemical characterization and antimicrobial activity of essential oils from Croton grewioides Baill. accessions on the phytopathogen Xanthomonas campestris pv. campestris.

Croton grewioides Baill. is an aromatic species with proven bioactive properties. Considering the potential of the species, the aim of this study was to chemically characterize and evaluate the in vitro antibacterial activity of the essential oils of C. grewioides on Xanthomonas campestris pv. campestris. The essential oils of the accessions of C. grewioides were extracted by the hydrodistillation method and analyzed by gas chromatography - mass spectrometry. For determination of the minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) of the essential oils and of the compound eugenol, the microdilution method was used at concentrations that ranged from 125 to 4000 µg.mL-1. Streptomycin sulfate was used as a positive control (12.5 to 100 µg.mL-1). Growth kinetics and the membrane permeability trial were evaluated for the concentrations 2×, 1×, 1/2×, 1/4×, and 1/8× MIC of the essential oil CGR-108. The major compounds identified in the essential oils were eugenol, methyl eugenol, and methyl chavicol. The essential oil of the accession CGR-108 had a lower MIC (> 500 and < 1000 µg.mL-1) and MBC equal to <2000 µg.mL-1. For eugenol, MIC was obtained with contractions >250 and < 500 µg.mL-1 and MBC with >500 µg.mL-1 and < 1000 µg.mL-1. A loss of cell viability of the bacteria was observed after 30 min of exposure to the essential oil of the accession CGR-108 at the concentrations of 2× and 1× MIC, which was proven by the fluorescence intensity with propidium iodide. The essential oils of Croton grewioides Baill. and the compound eugenol show antibacterial potential on Xanthomonas campestris pv. campestris.

Development of alcohol vinegars macerated with ACAI (Euterpe precatoria Mart.) berries and their quality evaluations with emphasis on color, antioxidant capacity, and volatiles profile.

In this work, the Amazonian native acai fruit, a superfruit recognized worldwide, was used through a simple operation of maceration in alcohol vinegar to transform it into an attractive and functional product containing the acai natural colorant and its bioactive compounds. The variables studied were the proportion of alcohol vinegar to acai (8:2 and 1:1) and maceration period (7, 14, and 21 days). The final vinegar was subjected to the determination of color parameters, antioxidant capacity (DPPH, ABTS), total phenolics content (TPC), volatile compounds extracted by stir bar sorptive extraction and identified by gas-chromatography-mass spectrometry analysis. The alcohol vinegars macerated with acai presented the color according to the content of acai added and maceration period employed, whereas antioxidant capacity and TPC were comparable to vinegars elaborated from fruits and red wine. Sixty volatiles compounds classified into five chemical groups were identified. The principal volatile compounds which contributed to the aroma in the products were 3-methyl-1-butanol, phenylethyl alcohol, benzaldehyde, o-cymene, p-cymenene, isoamyl acetate, and ethyl acetate. The most attractive product regarding the parameters studied was obtained from the use of the proportion of 1:1 of alcohol vinegar:acai and maceration period of 14 days. This product retained the most similar color to acai in natura, the highest values for antioxidant capacity measured by ABTS and TPC while being rich in volatile compounds due to the contributions mainly of alcohols, esters, aldehydes, and terpenes. PRACTICAL APPLICATION: This work demonstrates the feasibility to produce an alcohol vinegar with an attractive color and functional properties by the addition of acai resulting in to a wide spectrum of chemical compounds of acai through a very simple operation of maceration during 14 days of a proportion of 1:1 of alcohol vinegar:acai.

Effect of commercial yeasts (Saccharomyces cerevisiae) on fermentation metabolites, phenolic compounds, and bioaccessibility of Brazilian fermented oranges.

Brazil is the largest producer of oranges worldwide, as well as one of the largest producers of orange juice. Alcoholic fermented beverages have been considered a marketable alternative for oranges. In this study, four S. cerevisiae commercial yeasts were evaluated for metabolites generated during orange juice (cv. 'Pêra D9') fermentation. Alcohols, sugars, and organic acids were evaluated by HPLC-DAD-RID during fermentation, and phenolic compounds were analyzed in fermented orange. Orange juice and fermented oranges were also subjected to digestion simulations. The yeasts presented an adequate fermentation activity, based on sugar consumption, and high ethanol (>10.5%) and glycerol (4.8-5.5 g/L) contents. The yeast strains T-58 and US-05 produced high levels of lactic acid. Phenolic compounds and antioxidant activity did not differ amongst yeasts, presenting hesperidin levels between 115 and 127 mg/L, respectively. The fermented orange showed a >70% bioaccessibility, compared to juice, especially for catechin, epigallocatechin-gallate, procyanidin-B2, rutin, and procyanidin-B1.

Process optimization for simultaneous production of phenolic acids and enzymes with high transfructosylation activity in cupuassu (Theobroma grandiflorum) residue by submerged fermentation with Aspergillus carbonarius.

Cupuassu (Theobroma grandiflorum) generates a large amount of waste, which can be better used to obtain products with high added value through biotechnological processes. Thus, the present study aimed to obtain optimized conditions for the simultaneous production of phenolic acids, invertases and transferases enzymes in cupuassu residue with Aspergillus carbonarius. The main methodologies used to select the variables that influence the system were a Plackett-Burman design, followed by a Central Composite Rotational Design. The optimal conditions were use of 17.3% sucrose, 5.1% residue and 4.6% yeast extract to produce 2204.89 ± 5.75 mg GAE/100 g, 39.84 ± 2.08 U/mL of hydrolytic activity, 168.09 ± 3.81 U/mL of transfructosylation activity and 4.23 ± 0.19 of transfructosylation and hydrolytic activity ratio. Among the phenolic acids identified by the UFLC-DAD system, there was an increase of 148.17% in gallic acid and 205.51% in protocatechuic acid. The antioxidant activities also showed changes after fermentation, with an increase of 350% for the ABTS assay, 51.97% for FRAP, 22.65% for ORAC and 16.03% for DPPH. To the best of our knowledge, this is the first time that cupuassu residue is fermented with Aspergillus carbonarius to obtain invertases and transferases enzymes and phenolic acids. Supplementary Information: The online version contains supplementary material available at 10.1007/s13197-022-05418-z.

α-Amylase inhibition, cytotoxicity and influence of the in vitro gastrointestinal digestion on the bioaccessibility of phenolic compounds in the peel and seed of Theobroma grandiflorum.

The aim of this work was to evaluate the bioaccessibility, cytotoxicity, antioxidant and antidiabetic potential of peel and seeds of cupuassu (Theobroma grandiflorum). Thus, the extracts of cupuassu were evaluated for inhibition of α-amylase, cytotoxicity, and bioaccessibility after gastrointestinal digestion and probiotic fermentation (Lactobacillus delbrueckii, Lactobacillus jhonsoni, Lactobacillus rhamus and Bifidobacterium longum). Digestion increased concentrations of phenolics, showing bioaccessibility of up to 274.13% (total phenolics) and 1105.15% (ORAC). ß-carotene, quinic, tartaric, malic, citric, epicatechin, ethyl gallate, epigallocatechin gallate, gallic acid, pyrocatechol, vanillin, ramnetine were the main compounds while the epicatechin, ethyl gallate, gallic acid and pyrocatechol were the major effective phenolic compounds. The extracts did not show toxic effects and the cupuassu seeds showed 97% inhibition of α-amylase and 47.91% bioaccessibility of pyrocatechol. This study suggests that cupuassu extracts are sources of natural antioxidants with promising antidiabetic potential, and probiotics are able to increase phenolic compounds, responsible for health benefits.

Bioactive compounds and antioxidant activities in the agro-industrial residues of acerola (Malpighia emarginata L.), guava (Psidium guajava L.), genipap (Genipa americana L.) and umbu (Spondias tuberosa L.) fruits assisted by ultrasonic or shaker extraction.

The aim of this study was to analyze the residue powders of Malpighia emarginata L., Psidium guajava L., Genipa americana L. and Spondias tuberosa L. regarding their total phenolic compounds contents, antioxidant activity (ABTS, DPPH and FRAP), soluble sugars, carotenoids, organic acids by HPLC-DAD/RID and individual phenolic compounds by the UPLC-QDa-MS system. The genipap residue had a high content of soluble sugars (422.72 ± 19.15 mg.g-1 DW), with a higher content of sucrose (170.83 ± 10.89 mg.g-1 DW). Nystose was found in the residues of guava (6.59 ± 0.56 mg.g-1 DW) and umbu (65.61 ± 2.31 mg.g-1 DW). The residues of acerola and umbu showed contents of ß-carotene of 5.84 ± 0.01 mg.g-1 DW and 0.10 ± 0.05 mg.g-1 DW, respectively while high concentration (1116.00 ± 2.00 mg.100 g-1 DW) of tartaric acid was found in acerola residue and quinic acid (6340 ± 104.00 mg.100 g-1 DW) in umbu residue. Acetone (80%) and ultrasonic extraction were the best conditions for the residues of acerola, guava and genipap, however, for the umbu residue, extraction with shaker showed better results. The acerola and umbu residues showed higher yields of total phenolics, the values being 378.69-444.05 mg GAE.100 g-1 DW and 326.14-404.36 mg GAE.100 g-1 DW, respectively, as well as antioxidant activity. Naringenin was the individual phenolic compound with the highest concentration in the residue of acerola and genipap, vanillin in guava and rutin in umbu. Thus, residues powders from acerola, guava, genipap and umbu constitute potential sources of bioactive compounds, which could be used in the food, pharmaceutical and cosmetic industries.

Oil impact on the environment and aquatic organisms on the coasts of the states of Alagoas and Sergipe, Brazil - A preliminary evaluation.

The oil spill off the coast of the Brazilian Northeast region is one of the most significant global events regarding contamination and environmental impact in recent years. This work evaluates the effects of oil spills on the Northeast coasts between Alagoas and Sergipe states from October 2019 to January 2020. Analysis of some sampling points of seawater revealed the presence of Hg, Cd, Pb, and Cu in levels above the maximum concentration limits established by the Brazilian legislation. For water quality parameters, phosphorus, nitrite, and turbidity showed statistically different values. However, the chromatographic profiles of oil obtained from different beaches were quite similar. Seawater, fishes, and massunins (bivalve) presented the main polycyclic aromatic hydrocarbons: naphthalene, phenanthrene, fluoranthene, fluorene, and acenaphthalene. Therefore, the concentration of organic and inorganic contaminants determined in different environmental locations served as a subsidy to assess the effect of the preliminary oil spill on the Brazilian coast.

Evaluation of bioactive compounds, phytochemicals profile and antioxidant potential of the aqueous and ethanolic extracts of some traditional fruit tree leaves used in Brazilian folk medicine.

The aim of this study was to analyze eight selected species of leaves, used in the traditional medicine of the Northeast region of Brazil obtained from several fruit trees (grageru, soursop, jambolanum, passion fruit, insulin, nogueira, pedra ume kaá and stévia), regarding their polyphenols contents and antioxidant activity. Condensed and hydrolysable tannins, phenolics and flavonoids contents were determined and the antioxidant activities measured by ABTS, FRAP and ORAC assays. Organic acids were analyzed by HPLC-DAD system. Phenolic compounds of aqueous and ethanolic extracts were determined by UHPLC-DAD-MS. The results revealed high contents of total phenolics (13.34 ± 0.19 - 127.65 ± 0.21 mg.g-1 of GAE:QE (2:1) of sample) and flavonoids (12.30 ± 0.42 - 71.79 ± 0.00 mg.g-1 QE of sample). The ABTS results exhibited extraordinary activity in the extracts (74.48 ± 6.23 - 1487.33 ± 2.67 µmol Trolox.g-1 of sample). Acids quinic, tartaric, citric, gallic, chlorogenic, p-coumaric, ferulic and vanillic along with naringenin, rutin, vanillin, catechin, epicatechin, kaempferol were the most important compounds. Thus, these leaves extracts may be considered as sources of phenolics compounds having a high potential as natural antioxidants. In addition, the polyphenols present in these leaves have many beneficial effects and can also be used in medicinal and nutraceuticals products with enhanced bioactivities.

Enzymatic and ultrasonic-assisted pretreatment in the extraction of bioactive compounds from Monguba (Pachira aquatic Aubl) leaf, bark and seed.

The present study aims to characterize leaf, bark and seed of monguba in terms of their physicochemical and bioactive composition, and to determine total phenolic compounds (TPC) and total flavonoids (TF), well as their antioxidant activities (AA), of three organic solvent extracts with and without enzyme pretreatment by ultrasonic assisted extraction. Physicochemical composition was measured by pH, total titratable acidity, total soluble solids, moisture, ashes, lipids, crude protein, raw fiber, total carbohydrates, and water activity as well as, phytochemical composition analysis constituted of sugars, condensed (CT) and hydrolysable tannins (HT), carotenoids, total anthocyanins (TA), and organic acids contents. TPC and TF contents, and UHPLC/PDA/QDa flavonoids and phenolic acids quantification were performed for the solvent extracts. Antioxidant activity was determined by radical scavenging capacity assays (ABTS, DPPH, and ORAC), and reducing power assay (FRAP). Results showed that the leaf stood out with higher concentrations of ash, HT, TA and carotenoids; the bark with higher concentrations of raw fiber, total carbohydrates and organic acids (tartaric, quinic and 3.4-dihydroxybenzoic acids); in contrast, the seeds showed high concentrations of lipids, crude protein, sugars (fructose and sucrose), CT, and high values in all AA. The solvents significantly influenced the extraction of TPC and TF, highlighting ethanol. In general, the enzymatic treatments empowered the phenolic extraction and AA. The monguba seed extracts showed higher concentrations of hydroxycinnamic acids (chlorogenic acid, mainly), and flavanols (catechin and epicatechin), whereas the leaf extracts, flavanones (narigenin), flavonols (rutin, mainly) and flavones (acacetin). The bark extracts stood out for the presence of vanillin. The monguba seed extract can be used in functional foods production.

Synbiotic açaí juice (Euterpe oleracea) containing sucralose as noncaloric sweetener: Processing optimization, bioactive compounds, and acceptance during storage.

This study aimed to evaluate the fermentation process of Lacticaseibacillus casei in the açaí juice, and to evaluate the addition of fructooligosaccharides and sucrose. The organic acids, anthocyanins, polyphenolic compounds, and antioxidant activity were also investigated during fermentation. Moreover, the impact of sucrose and sucralose on microbial viability and sensory acceptance of synbiotic products was evaluated during 42 days storage at refrigerated conditions. The conditions for synbiotic juice production were the initial pH of 6.1 and fermentation undertaken at 28 °C for 22 hr. During fermentation, the higher viability was obtained when a combination of 40 g/L of FOS+10 g/L of sucrose was used (9.70 ± 0.01 log CFU/mL). The lactic acid increased from 0.82 to 1.29 g/L during the fermentation while citric acid decreased from 1.05 to 0.75 g/L. The cyanidin-3-O-rutinoside, polyphenolic compounds, and antioxidant activity increased. Thus, fermentation improved the functional value of the beverage. The L. casei viability reduced from 9.71 ± 0.04 to 8.90 ± 0.06 log CFU/ mL in the juice with sucrose, and from 9.71 ± 0.04 to 8.71 ± 0.14 log CFU/ mL in the juice with sucralose. Thus, the açaí juice is a viable matrix for the synbiotic food, which allows the viability maintenance during the storage. Regarding sensory acceptance, the internal preference mapping indicated an increase in the color preference with the storage of synbiotic juices. However, the flavor and overall acceptance reduced with storage. Nevertheless, the flavor and overall acceptance of juice with sucralose were better than the juice with sucrose. After 42 days of storage, penalty analysis revealed that beverage with sucrose showed a lack of sweet taste and excess of sour taste. Thus, a high-quality açaí product with viable probiotic microorganism, high anthocyanins, and polyphenolic compounds contents could be obtained, which can be exploited for commercial use. PRACTICAL APPLICATION: Synbiotic açaí juice is a healthier alternative to consuming products containing this fruit. The inclusion of probiotic microorganisms and prebiotic fructooligosaccharides increased bioactive compounds contents during the shelf life of the juice. The sensory evaluation using the internal preference mapping revealed that the juice flavor with sucralose was better accepted than the juice formulated with addition of sucrose.

Improvement of bioactive compounds content in granadilla (Passiflora ligularis) seeds after solid-state fermentation.

Fermentation improves the bioactivity of fruit by-products; therefore, this study aimed to increase the bioactive compound content in granadilla (Passiflora ligularis) seed flour (with 50% and 70% initial moisture) through solid-state fermentation using the fungus Aspergillus niger. The extracts were obtained with distilled water, 40% acetone, 80% acetone, 40% ethanol, or 80% ethanol. The highest total phenolic (4713.3 of gallic acid equivalent/100 g of granadilla seed flour in dry basis) and total flavonoid (1910.4 mg of quercetin/100 g of granadilla seed flour in dry basis) contents were obtained with granadilla flour at 50% initial moisture fermented for 48 h with 80% acetone extractor solvent. The highest antioxidant activity was obtained with 80% acetone from flour fermented for 168 h. The chromatographic analysis showed 10 compounds identified in the 80% acetone extracts of fermented flour; gallic acid and epigallocatechin were the major compounds. Gallic acid, catechin, 6,2'-di-hydroxyflavone, ethyl gallate and coumarin had higher concentrations in extracts of fermented flours when compared with unfermented ones. Only fermented flours showed the presence of protocatechuic acid compound. The solid-state fermentation was efficient to obtain extracts of granadilla seed flour enrichment of antioxidant bioactive compounds with potential of application in food, cosmetic and pharmaceutical industries.

Citrus Flavonoids as Promising Phytochemicals Targeting Diabetes and Related Complications: A Systematic Review of In Vitro and In Vivo Studies.

The consumption of plant-based food is important for health promotion, especially concerning the prevention and management of chronic diseases. Flavonoids are the main bioactive compounds in citrus fruits, with multiple beneficial effects, especially antidiabetic effects. We systematically review the potential antidiabetic action and molecular mechanisms of citrus flavonoids based on in vitro and in vivo studies. A search of the PubMed, EMBASE, Scopus, and Web of Science Core Collection databases for articles published since 2010 was carried out using the keywords citrus, flavonoid, and diabetes. All articles identified were analyzed, and data were extracted using a standardized form. The search identified 38 articles, which reported that 19 citrus flavonoids, including 8-prenylnaringenin, cosmosiin, didymin, diosmin, hesperetin, hesperidin, isosiennsetin, naringenin, naringin, neohesperidin, nobiletin, poncirin, quercetin, rhoifolin, rutin, sineesytin, sudachitin, tangeretin, and xanthohumol, have antidiabetic potential. These flavonoids regulated biomarkers of glycemic control, lipid profiles, renal function, hepatic enzymes, and antioxidant enzymes, and modulated signaling pathways related to glucose uptake and insulin sensitivity that are involved in the pathogenesis of diabetes and its related complications. Citrus flavonoids, therefore, are promising antidiabetic candidates, while their antidiabetic effects remain to be verified in forthcoming human studies.

In vitro gastrointestinal digestion and probiotics fermentation impact on bioaccessbility of phenolics compounds and antioxidant capacity of some native and exotic fruit residues with potential antidiabetic effects.

A bioaccessibility study on polyphenols, flavonoids and antioxidant capacity after the in vitro simulated digestion was evaluated for extract of fruit (caja-umbu, cashew apple, canafistula, cupuassu, soursop, manguba and strawberry) residues. The results show that ORAC assay presented a significant increase (p ≤ 0.05) in bioaccessibility varying from 35.99 ± 0.02% (caja-umbu residue) to 339.83 ± 0.06% (cupuassu residue) after the digestion process. Approximately 15.01 ± 1.54 to 237.77 ± 4.10% of phenolic compounds were bioaccessible after probiotics fermentation. The identification and quantification of phenolic compounds were performed through the UHPLC-QDa-MS system. Catechin and epicatechin were widely detected in all fruit residues. After the gastrointestinal digestion and probiotics fermentation the contents of simple phenolics and hydroxybenzoic acids increased. Also, the α-amylase inhibitory activity exhibited a maximum value of 98.66 ± 1.41% for soursop residue. To the best of our knowledge, for the first time, bioaccessibility study on caja-umbu, canafistula and manguba residues was performed in association with antidiabetic effects. The soursop residue presented the highest bioaccessibility and can be potentially explored for application in functional foods and pharmaceuticals. Therefore, the joint consumption of probiotics and phytochemicals are essential for the effective assimilation by the human organism.

Volatile profiling and UHPLC-QqQ-MS/MS polyphenol analysis of Passiflora leschenaultii DC. fruits and its anti-radical and anti-diabetic properties.

Twenty-four phenolic compounds including daidzein, epicatechin and artepillin C were identified in Passiflora leschenaultii DC. fruit by UHPLC-QqQ-MS/MS analysis. The aroma profile has been studied using the HS-SPME/GC-MS which revealed 67 volatile compounds including 13 terpenes, 18 alcoholics, 15 esters, ketones and phenolic acids. Further, the proximate composition, anti-radical and anti-diabetic activities of fruit pulp were also determined. The fresh fruit pulp of P. leschenaultii registered higher total phenolic (691.90 mg GAE/g extract) and tannin (313.81 mg GAE/g extract) contents and it also exhibited maximum DPPH (IC50 of 6.69 µg/ml) and ABTS+ (9760.44 µM trolox equivalent/g extract) scavenging activities. The fresh fruit pulp showed a strong inhibition towards the α-Amylase and α-Glucosidase (IC50 of 32.20 and 19.81 µg/mL, respectively) enzymes. Thus, the work stipulates that phenolic compounds rich P. leschenaultii fruit can serve as a potential nutraceutical, antioxidative and anti-diabetic agent in food and pharmaceutical formulations.

Modulation of interleukin expression by medicinal plants and their secondary metabolites: A systematic review on anti-asthmatic and immunopharmacological mechanisms.

BACKGROUND: Asthma is one of the most common chronic inflammatory conditions of the lungs in modern society. Asthma is associated with airway hyperresponsiveness and remodeling of the airways, with typical symptoms of cough, wheezing, shortness of breath and chest tightness. Interleukins (IL) play an integral role in its inflammatory pathogenesis. Medicinal herbs and secondary metabolites are gaining considerable attention due to their potential therapeutic role and pharmacological mechanisms as adjunct tools to synthetic bronchodilator drugs. PURPOSE: To systematically review the literature on the use of single or mixed plants extracts therapy in vivo experimental systems for asthma, emphasizing their regulations on IL production to improve lung. METHODS: Literature searches were performed on PubMed, EMBASE, Scopus and Web of Science databases. All articles in English were extracted from 1999 up to September 2019, assessed critically for data extraction. Studies investigating the effectiveness and safety of plant extracts administered; inflammatory cell count, immunoglobulin E (IgE) production and regulation of pro-inflammatory cytokine and T helper (Th) 1 and Th2-driven cytokine expression in bronchoalveolar lavage fluid (BALF) and lung of asthmatic animals were included. RESULTS: Four hundred and eighteen publications were identified and 51 met the inclusion criteria. Twenty-six studies described bioactive compounds from plant extracts. The most frequent immunopharmacological mechanisms described included reduction in IgE and eosinophilic recruitment, decreased mucus hypersecretion and airway hyperreactivity, enhancement of the balance of Th1/Th2 cytokine ratio, suppression of matrix metallopeptidase 9 (MMP-9) and reversal of structural alterations. CONCLUSION: Plant extract therapies have potential control activities on asthma symptoms by modulating the secretion of pro-inflammatory (IL-1ß, IL-8), Th17 (IL-17), anti-inflammatory (IL-10, IL-23, IL-31, IL-33), Th1 (IL-2, IL-12) and Th2 (IL-4, IL-5, IL-6, IL-13) cytokines, reducing the level of biomarkers of airway inflammation.

Phytochemicals screening, antioxidant capacity and chemometric characterization of four edible flowers from Brazil.

Edible flowers are receiving renewed interest as potential sources of bioactive compounds. The present study aimed to investigate the presence of bioactive compounds and antioxidant activity of some exotic flowers present in Brazil such as Amaranthus hypochondriacus, Tropaeolum majus (red), Tropaeolum majus (orange) and Spilanthes oleracea L. The content of total phenolic compounds, flavonoids, condensed, hydrolysable tannins and antioxidante capacity were determined. The identification and quantification of the phenolic compounds was performed through the UHPLC-QDa-MS system. The compounds p-coumaric acid and ferulic acid were identified and quantified for the first time in all flowers. Tropaeolum majus (red) presented the hightest amounts of total phenolic compounds and hydrolysable tannins. Also, it presented the highest antioxidant capacity for ORAC and FRAP assays. Thus, this study showed the diversity and abudance of natural antioxidants present in edible flowers, which could be explored for application in functional foods and pharmaceuticals.

In situ microemulsion-gel obtained from bioadhesive hydroxypropyl methylcellulose films for transdermal administration of zidovudine.

This study aims to develop in situ microemulsion-gel (ME-Gel) obtained from hydroxypropyl methylcellulose (HPMC) films for transdermal administration of Zidovudine (AZT). Firstly, HPMC films containing propylene glycol (PG) and eucalyptus oil (EO) were obtained and characterized. Later, a pseudo-ternary phase diagram composed of water, EO, tween 80 and PG was obtained and one microemulsion (ME) with a similar proportion of the film components was obtained. ME was transformed in ME-Gel by the incorporation of HPMC. Finally, HPMC films were hydrated with Tween 80 solution to yield in situ ME-Gel and its effect on AZT skin permeation was compared with HPMC film hydrated with water (F5hyd). The results showed that the ME and ME-Gel presented a droplet size of 16.79 and 122.13 µm, respectively, polydispersity index (PDI) < 0.39 and pH between 5.10 and 5.40. The incorporation of HPMC resulted in viscosity about 2 times higher than the use of ME. The presence of AZT did not alter the formulation properties. The in situ ME-Gel promoted a two-fold increase in the permeated amount of AZT compared to F5hyd. The results suggest that it was possible to obtain an ME-Gel in situ from HPMC films and that its effect on transdermal permeation of AZT was significant.

Essential oils and its bioactive compounds modulating cytokines: A systematic review on anti-asthmatic and immunomodulatory properties.

BACKGROUND: Asthma, the main inflammatory chronic condition affecting the respiratory system, is characterized by hyperresponsiveness and reversible airway obstruction, recruitment of inflammatory cells and excessive production of mucus. Cytokines as biochemical messengers of immune cells, play an important role in the regulation of allergic inflammatory and infectious airway processes. Essential oils of plant origin are complex mixtures of volatile and semi volatile organic compounds that determine the specific aroma of plants and are categorized by their biological activities. PURPOSE: We reviewed whether essential oils and their bioactive compounds of plant origin could modulate cytokines' immune responses and improve asthma therapy in experimental systems in vitro and in vivo. METHODS: Electronic and manual search of articles in English available from inception up to November 2018 reporting the immunomodulatory activity of essential oils and their bioactive compounds for the management of asthma. We used PubMed, EMBASE, Scopus and Web of Science. Publications reporting preclinical experiments where cytokines were examined to evaluate the consequence of anti-asthmatic therapy were included. RESULTS: 914 publications were identified and 13 were included in the systematic review. Four articles described the role of essential oils and their bioactive compounds on bronchial asthma using cell lines; nine in vivo studies evaluated the anti-inflammatory efficacy and immunomodulating effects of essential oil and their secondary metabolites on cytokines production and inflammatory responses. The most important immunopharmacological mechanisms reported were the regulation of cytokine production, inhibition of reactive oxygen species accumulation, inactivation of eosinophil migration and remodeling of the airways and lung tissue, modulation of FOXP3 gene expression, regulation of inflammatory cells in the airways and decreasing inflammatory mediator expression levels. CONCLUSION: Plant derived essential oils and related active compounds have potential therapeutic activity for the treatment of asthma by modulating the release of pro-inflammatory (TNF-α, IL-1ß, IL-8), Th17 (IL-17), anti-inflammatory (IL-10), Th1 (IFN-γ, IL-2, IL-12) and Th2 (IL-4, IL-5, IL-6, IL-13) cytokines and the suppression of inflammatory cell accumulation.

Protective effects of flavonoid composition rich P. subpeltata Ortega. on indomethacin induced experimental ulcerative colitis in rat models of inflammatory bowel diseases.

ETHNOPHARMACOLOGICAL RELEVANCE: Polyphenolics (flavonoid and phenolic) rich plants are the effective source for the treatment of acute and chronic degenerative diseases including inflammatory bowel disease. OBJECTIVE: This study was aimed to examine the effects of polyphenolics rich leaf acetone extract of P. subpeltata against the indomethacin induced ulcerative colitis in rats. MATERIALS AND METHODS: Two consecutive days administration of indomethacin produced chronic inflammation in GIT tissues of rats. Further, the plant extract 200 and 400 mg/kg treatment were continued until 11th day. Then hematological, enzymatic antioxidants, MPO and histological evaluations were analyzed. Moreover, the extracts were treated with RAW267.4 cells for the cytotoxicity, NO and TNF-α analysis. RESULTS: The obtained results revealed, that higher dose of the plant extract dropped neutrophil infiltration followed by inhibiting the MPO enzyme levels and controls the enzymatic antioxidants such as SOD, CAT, GSH and LPO. RAW cells study also proved that the plant extract effectively inhibits NO and TNF-α production. CONCLUSIONS: Thus, these results suggest that P. subpeltata extract may have therapeutic potential for the treatment of IBD although further clinical research is still warranted.

Effect of spray drying on bioactive and volatile compounds in soursop (Annona muricata) fruit pulp.

Soursop is seasonal and highly perishable fruit, which limits its commercialization. Thus it is necessary to conserve its pulp so that it is available throughout the year. One of the most common forms of fruit preservation is by dehydration. This work had an objective to dehydrate soursop pulp by spray drying at optimum conditions and to analyze the retention of bioactive and volatile compounds in soursop powder, besides analyzing its antioxidant capacity. The total phenolics, carotenoids and flavonoids contents were determined, while volatile compounds were analyzed by Stir Bar Sorptive Extraction (SBSE) coupled with GC-MS system. The total content of the phenolic compounds and flavonoids in the fresh pulp were 160.28 mg of GAE/100 g and 87.17 mg of quercetin/100 g, respectively while for rehydrated dried powder their values were 158.95 mg of GAE/100 g and 85.17 mg of quercetin/100 g, respectively. The total phenolic compounds, flavonoids and antioxidant capacity did not show any significant difference (p < .05) between the fresh fruit pulp and dehydrated powder. A total of 85 volatile compounds were identified, of which 33 were esters, representing the major class of organic compounds, 15 were terpenes, 10 aldehydes, 7 acids, 5 alcohols, 5 lactones, 3 ketones, and 6 other compounds. Of the total 85 compounds, identified in soursop pulp, 58 compounds were identified in the rehydrated dried powder. The principal compounds for both samples were methyl (E)-2-hexenoate, methyl hexanoate and methyl (E)-2-butanoate, which contribute to soursop aroma according to their Odor Active Values (OAV). Considering that there was no significant difference (p < .05) between fresh pulp and the rehydrated dried powder in concentrations of bioactive compounds and even with the reduction in the concentration of the main volatile compounds while the OAVs of these compounds were relatively high, it is concluded that spray dried powder of soursop pulp retains its nutritional and aroma quality, besides maintaining the antioxidant capacity.