Antioxidant Activity of Encapsulated Extracts and Bioactives from Natural Sources

2020 ◽  
Vol 26 (31) ◽  
pp. 3847-3861
Author(s):  
Odinei H. Gonçalves ◽  
Thaysa F.M. Moreira ◽  
Anielle de Oliveira ◽  
Lívia Bracht ◽  
Rafael P. Ineu ◽  
...  

The low water solubility and low bioavailability of natural bioactive substances such as polyphenols and flavonoids, either in pure form or extracts, are a major concern in the pharmaceutical field and even on the food development sector. Although encapsulation has demonstrated success in addressing these drawbacks, it is important to evaluate the antioxidant activity of the encapsulated compounds. This article reviews the encapsulation of bioactive compounds from natural sources focusing their antioxidant activity after encapsulation. Attention is given to the methods and wall materials used, and the antioxidant activity methodologies (classical in vitro techniques such as DPPH, ORAC, FRAP and others, as well as in vivo/ex vivo tests to evaluate endogenous antioxidant enzymes or oxidative stress) applied to assess the antioxidant capacity are also comprehensively summarized.

2012 ◽  
Vol 82 (3) ◽  
pp. 228-232 ◽  
Author(s):  
Mauro Serafini ◽  
Giuseppa Morabito

Dietary polyphenols have been shown to scavenge free radicals, modulating cellular redox transcription factors in different in vitro and ex vivo models. Dietary intervention studies have shown that consumption of plant foods modulates plasma Non-Enzymatic Antioxidant Capacity (NEAC), a biomarker of the endogenous antioxidant network, in human subjects. However, the identification of the molecules responsible for this effect are yet to be obtained and evidences of an antioxidant in vivo action of polyphenols are conflicting. There is a clear discrepancy between polyphenols (PP) concentration in body fluids and the extent of increase of plasma NEAC. The low degree of absorption and the extensive metabolism of PP within the body have raised questions about their contribution to the endogenous antioxidant network. This work will discuss the role of polyphenols from galenic preparation, food extracts, and selected dietary sources as modulators of plasma NEAC in humans.


2020 ◽  
Vol 16 (3) ◽  
pp. 284-293
Author(s):  
George Laylson da Silva Oliveira ◽  
Maria das Dores Alves de Oliveira ◽  
Maria da Conceição Oliveira Prado ◽  
Alexandre de Barros Falcão Ferraz ◽  
José Carlos Correia Lima da Silva ◽  
...  

Background: Garcinielliptone FC corresponds to a polyprenylated acylphloroglucinol having a benzophenonic core (diphenylmethanone) substituted with isoprenyl(s) group(s) (3-methyl-2-butenyl) and 2-isopropenyl-hex-5-enyl. Objective: The present work evaluated the antioxidant activity of garcinielliptone FC (GFC) in vitro against non-biological radicals [2,2-diphenyl-1-picrylhydrazyl (DPPH•) and 2,2'-azinobis-3- ethylbenzothiazoline-6-sulfonic acid (ABTS•+)] and ex vivo against oxidative damage induced by AAPH (2,2'-azobis-2-methylpropionamidine dihydrochloride) and iron/citrate ion in erythrocytes and mitochondria, respectively. Methods: In addition to the protective effect, the main biochemical indexes of oxidative stress, such as lipid peroxidation through the formation of Thiobarbituric Acid Reactive Substances (TBARS), Superoxide Dismutase (SOD), Catalase (CAT) activity and reduced glutathione (GSH) levels. Results: According to the results obtained in erythrocytes, the antioxidant results at concentrations of 0.1, 0.3, 0.7, 1.5 and 3.0 mM were 26.34 ± 0.68, 43.39 ± 2.17, 62.27 ± 2.17, 86.69 ± 0.47 and 92.89 ± 0.45%, respectively, where GFC reduced the rate of oxidative hemolysis when compared to AAPH (p<0.05). The antioxidant activity observed in erythrocytes was also seen in mitochondria in which GFC reduced mitochondrial swelling by increasing the absorbance when compared to iron/citrate ion complex (p<0.05). In both biological models, GFC had an antioxidant effect on erythrocyte and mitochondrial redox balance when analyzing oxidative stress biomarkers, such as reduction of lipid peroxidation and inhibition of depletion in the activity of SOD, CAT and GSH levels. Conclusion: In conclusion, GFC had in vitro and ex vivo antioxidant activity against oxidative damage induced in erythrocytes and mitochondria acting on the erythrocytic and mitochondrial redox balance.


2012 ◽  
Vol 81 (2) ◽  
pp. 346-350 ◽  
Author(s):  
Martina C. Meinke ◽  
Sabine Schanzer ◽  
Stefan F. Haag ◽  
Federica Casetti ◽  
Marcel L. Müller ◽  
...  

2016 ◽  
Vol 37 (6) ◽  
pp. 2013-2024 ◽  
Author(s):  
Ain A Neuhaus ◽  
Yvonne Couch ◽  
Brad A Sutherland ◽  
Alastair M Buchan

Pericytes are contractile vascular mural cells overlying capillary endothelium, and they have been implicated in a variety of functions including regulation of cerebral blood flow. Recent work has suggested that both in vivo and ex vivo, ischaemia causes pericytes to constrict and die, which has implications for microvascular reperfusion. Assessing pericyte contractility in tissue slices and in vivo is technically challenging, while in vitro techniques remain unreliable. Here, we used isolated cultures of human brain vascular pericytes to examine their contractile potential in vitro using the iCelligence electrical impedance system. Contraction was induced using the vasoactive peptide endothelin-1, and relaxation was demonstrated using adenosine and sodium nitroprusside. Endothelin-1 treatment also resulted in increased proliferation, which we were able to monitor in the same cell population from which we recorded contractile responses. Finally, the observation of pericyte contraction in stroke was reproduced using chemical ischaemia, which caused a profound and irreversible contraction clearly preceding cell death. These data demonstrate that isolated pericytes retain a contractile phenotype in vitro, and that it is possible to quantify this contraction using real-time electrical impedance recordings, providing a significant new platform for assessing the effects of vasoactive and vasculoprotective compounds on pericyte contractility.


2021 ◽  
Vol 20 (2) ◽  
pp. 229-238
Author(s):  
Shun-ming Tang ◽  
Jiao Xu ◽  
Nabilla Joshua Abdulai ◽  
Lang Zhou ◽  
Shan-shan Wang ◽  
...  

Cordyceps cicadae is an entomogenous fungus, which is used as both medicine and food due to the presence of rich bioactive substances. Currently, most studies focus on the pharmacological effects of the bioactive components of C. cicadae, but the research on their processing is still in its infancy. In this study, polysaccharides were extracted from insect-cultivated C. cicadae (tussah pupae C. cicadae and domestic silkworm pupae C. cicadae) and wild C. cicadae. The functional properties of C. cicadae polysaccharides were evaluated. At the same time, the in vitro antioxidant activity of the insect-cultivated C. cicadae was determined and compared with the wild C. cicadae. The results showed that the cultivated C. cicadae polysaccharides and the wild one had similar structures, and both had appreciable water solubility, oilholding capacity, thermal stability, and emulsifying property compared to foaming property and foaming stability. Further, the C. cicadae polysaccharides cultured on silkworm pupae and tussah pupae showed comparable antioxidant and reducing power to the wild C. cicadae. Our data indicates that the C. cicadae polysaccharides have the potential as a food additive, among which the domestic silkworm pupae C. cicadae showed the best outcome, and the C. cicadae polysaccharides cultured by bionic method have the same antioxidant activity as the wild one.


2019 ◽  
pp. 407-430
Author(s):  
Ol'ga Aleksandrovna Vorobyeva ◽  
Darina Sergeyevna Malygina ◽  
Elizaveta Vladimirovna Grubova ◽  
Nina Borisovna Melnikova

In the review the biological properties (antitumor, antiviral, hypolipidemic, anti-inflammatory, etc.) and bioavailability of betulin and betulinic acid derivatives were discussed. These compounds are isolated from various natural sources, including birch bark (Betula, Betulaceae). The structure-activity correlation was considered for well-known betulinic acid derivatives. The perspectivity of this compounds as active pharmaceutical ingredients was demonstrated by in vitro, in vivo, and ex vivo experiments. The type of antitumor actions, generally, depends on substituents at the C-3 and C-28 carbon atoms of the lupane skeleton. It is very important that the carboxyl group of betulinic acid in the C-28 position was present. In this case, the cytotoxicity of C-3 modified derivatives is extremely high for all tested cell lines. The use of these compounds in the medical practice is complicated because they have low bioavailability and poor water solubility (from 1 to 100 µg*l-1). The main chemical syntheses for solubility improvement of betulin derivatives by grafting of hydrophilic groups were discussed. Moreover, the colloid-chemical approaches for the bioavailability improving of triterpenoids include: 1) including of these compounds in liposomes, vesicles and other nanoparticles; 2) obtaining of micelles with high-molecular compounds; 3) colloid-chemical dissolution due to physico-mechanical action; 4) inclusion complexes formation; 5) using of polymers for triterpenoids grafting. Chemical modification of betulin and betulinic acid by polar groups, such as phosphate/phosphonate, sulfate, amino acids, etc. has been shown for bioavailability improving.


Pharmaceutics ◽  
2020 ◽  
Vol 12 (8) ◽  
pp. 717 ◽  
Author(s):  
Roseline Mazet ◽  
Xurxo García-Otero ◽  
Luc Choisnard ◽  
Denis Wouessidjewe ◽  
Vincent Verdoot ◽  
...  

We previously developed two optimized formulations of dexamethasone acetate (DXMa) hydrogels by means of special cubic mixture designs for topical ocular administration. These gels were elaborated with hydroxypropyl-β-CD (HPβCD) and hydroxypropyl-γ-CD (HPγCD) and commercial hydrogels in order to enhance DXMa water solubility and finally DXMa’s ocular bioavailability and transcorneal penetration. The main objective of this study was to characterize them and to evaluate in vitro, ex vivo, and in vivo their safety, biopermanence, and transcorneal permeation. Gels A and B are Newtonian fluids and display a viscosity of 13.2 mPa.s and 18.6 mPa.s, respectively, which increases their ocular retention, according to the in vivo biopermanence study by PET/CT. These hydrogels could act as corneal absorption promoters as they allow a higher transcorneal permeation of DXMa through porcine excised cornea, compared to DEXAFREE® and MAXIDEX®. Cytotoxicity assays showed no cytotoxic effects on human primary corneal epithelial cells (HCE). Furthermore, Gel B is clearly safe for the eye, but the effect of Gel A on the human eye cannot be predicted. Both gels were also stable 12 months at 25 °C after sterilization by filtration. These results demonstrate that the developed formulations present a high potential for the topical ocular administration of dexamethasone acetate.


1992 ◽  
Vol 68 (06) ◽  
pp. 687-693 ◽  
Author(s):  
P T Larsson ◽  
N H Wallén ◽  
A Martinsson ◽  
N Egberg ◽  
P Hjemdahl

SummaryThe significance of platelet β-adrenoceptors for platelet responses to adrenergic stimuli in vivo and in vitro was studied in healthy volunteers. Low dose infusion of the β-adrenoceptor agonist isoprenaline decreased platelet aggregability in vivo as measured by ex vivo filtragometry. Infusion of adrenaline, a mixed α- and β-adrenoceptor agonist, increased platelet aggregability in vivo markedly, as measured by ex vivo filtragometry and plasma β-thromboglobulin levels. Adrenaline levels were 3–4 nM in venous plasma during infusion. Both adrenaline and high dose isoprenaline elevated plasma von Willebrand factor antigen levels β-Blockade by propranolol did not alter our measures of platelet aggregability at rest or during adrenaline infusions, but inhibited adrenaline-induced increases in vWf:ag. In a model using filtragometry to assess platelet aggregability in whole blood in vitro, propranolol enhanced the proaggregatory actions of 5 nM, but not of 10 nM adrenaline. The present data suggest that β-adrenoceptor stimulation can inhibit platelet function in vivo but that effects of adrenaline at high physiological concentrations are dominated by an α-adrenoceptor mediated proaggregatory action.


1979 ◽  
Vol 41 (03) ◽  
pp. 465-474 ◽  
Author(s):  
Marcia R Stelzer ◽  
Thomas S Burns ◽  
Robert N Saunders

SummaryThe relationship between the effects of suloctidil in vivo as an antiplatelet agent and in vitro as a modifier of platelet serotonin (5-HT) parameters was investigated. Suloctidil was found to be effective in reducing platelet aggregates formation in the retired breeder rat as determined using the platelet aggregate ratio method (PAR) with an ED50 of 16.1 mg/kg 24 hours post administration. In contrast to the hypothesis that 5-HT depletion is involved in the anti-aggregatory mechanism of suloctidil, no correlation was found between platelet 5- HT content and this antiplatelet activity. Reduction of platelet 5-HT content required multiple injections of high doses (100 mg/kg/day) of suloctidil. Suloctidil administration for 8 days at 100 mg/kg/day, which lowered platelet 5-HT content by 50%, resulted in no permanent effect on ex vivo platelet 5-HT uptake or thrombin-induced release, nor alteration in the plasma 5-HT level. However, these platelets exhibited a short-lived, significant increase in percent leakage of 5-HT after 30 minutes of incubation. Therefore, suloctidil treatment at high doses may with time result in platelet 5-HT depletion, however this effect is probably not related to the primary anti-aggregatory activity of the drug.


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