scholarly journals Explorative Screening of Bioactivities Generated by Plant-Based Proteins after In Vitro Static Gastrointestinal Digestion

Nutrients ◽  
2020 ◽  
Vol 12 (12) ◽  
pp. 3746
Author(s):  
Camille Dugardin ◽  
Benoit Cudennec ◽  
Mélissa Tourret ◽  
Juliette Caron ◽  
Laetitia Guérin-Deremaux ◽  
...  
Keyword(s):  
Opioid Receptors ◽  
Biological Activities ◽  
Hormone Secretion ◽  
Antioxidant Properties ◽  
Gastrointestinal Digestion ◽  
Fava Bean ◽  
Dpp Iv ◽  
Wide Range ◽  
Anti Inflammatory

The gastrointestinal digestion of food proteins can generate peptides with a wide range of biological activities. In this study, we screened various potential bioactivities generated by plant-based proteins. Whey protein as an animal protein reference, five grades of pea protein, two grades of wheat protein, and potato, fava bean, and oat proteins were submitted to in vitro SGID. They were then tested in vitro for several bioactivities including measures on: (1) energy homeostasis through their ability to modulate intestinal hormone secretion, to inhibit DPP-IV activity, and to interact with opioid receptors; (2) anti-hypertensive properties through their ability to inhibit ACE activity; (3) anti-inflammatory properties in Caco-2 cells; (4) antioxidant properties through their ability to inhibit production of reactive oxygen species (ROS). Protein intestinal digestions were able to stimulate intestinal hormone secretion by enteroendocrine cells, to inhibit DPP-IV and ACE activities, to bind opioid receptors, and surprisingly, to decrease production of ROS. Neither pro- nor anti-inflammatory effects have been highlighted and some proteins lost their pro-inflammatory potential after digestion. The best candidates were pea, potato, and fava bean proteins.

scholarly journals Explorative screening of potential peptide activities generated by plant-based proteins after in vitro simulation of static digestion

2020 ◽  
Vol 79 (OCE2) ◽  
Author(s):  
Camille Dugardin ◽  
Benoît Cudennec ◽  
Juliette Caron ◽  
Laetitia Guérin-Deremaux ◽  
Catherine Lefranc-Millot ◽  
...  
Keyword(s):  
Opioid Receptors ◽  
Biological Activities ◽  
Antioxidant Properties ◽  
Dependent Manner ◽  
Gastrointestinal Digestion ◽  
Pea Protein ◽  
Dpp Iv ◽  
Wide Range ◽  
Anti Inflammatory

AbstractIntroductionThe gastrointestinal digestion of food proteins can generate peptides having a wide range of biological activities and possibly involved in many physiological processes. In this study, we screened various potential bioactivities generated by plant-based protein samples as compared to one animal-based protein after in vitro simulation of gastrointestinal digestion (SGID).Materials and methods1 protein samples: Whey protein (WhP) as an animal protein reference (tested twice, in each set), 3 grades of pea protein (PeaP1, PeaP2 and PeaP3) and an hydrolyzed pea protein (HPeaP), pea and wheat albumins (PeaA and WA), wheat protein (WP), potato, fava bean and oat proteins (PP, FBP and OP) were submitted to SGID.Undigested and digested protein samples were then tested in different in vitro, cellular or acellular models, including measures on : 1/energy homeostasis through their ability to promote satiety hormones (CCK and GLP-1) secretion by STC-1 cells, to inhibit DPP-IV activity and to interact with opioid receptors; 2/anti-hypertensive properties through their ability to inhibit ACE activity; 3/anti-inflammatory properties through their ability to decrease IL-8 secretion by Caco-2 cells submitted or not to LPS; 4/antioxidant properties through their ability to inhibit production of the 3 reactive oxygen species (ROS): O2.-, H2O2 and HO..ResultsThe SGID of the 11 protein samples led to bioactive peptides able to stimulate CCK and GLP-1 secretion by enteroendocrine cells in a dose-dependent manner, to inhibit in vitro DPP-IV and ACE activity and to bind opioid receptors. They were also able to decrease production of ROS. Anyway, no anti-inflammatory impact through inhibition of IL-8 secretion has been highlighted in this study but no pro-inflammatory impact was detected neither; even more, some protein samples lost their pro-inflammatory potential after digestion. The best candidates answering globally to the main activities explored were PeaP1, PeaP2, HPeaP, PP and FBP with some specificities.DiscussionThese protein samples could thus be potentially valorized in the future in the context of type 2 diabetes and related cardiovascular risk prevention, or for their antioxidant properties in the context of cardiovascular diseases or ageing. Moreover, those peptides could offer natural preventive alternatives to some drugs. This will need further exploration and in vivo validation.

scholarly journals Mitoprotective Effects of Centella asiatica (L.) Urb.: Anti-Inflammatory and Neuroprotective Opportunities in Neurodegenerative Disease

2021 ◽  
Vol 12 ◽  
Author(s):  
Jia Hui Wong ◽  
Anna M. Barron ◽  
Jafri Malin Abdullah
Keyword(s):  
Neurodegenerative Disease ◽  
Healthy Aging ◽  
Brain Aging ◽  
Antioxidant Properties ◽  
Centella Asiatica ◽  
Asiatic Acid ◽  
Wide Range ◽  
Anti Inflammatory

Natural products remain a crucial source of drug discovery for accessible and affordable solutions for healthy aging. Centella asiatica (L.) Urb. (CA) is an important medicinal plant with a wide range of ethnomedicinal uses. Past in vivo and in vitro studies have shown that the plant extract and its key components, such as asiatic acid, asiaticoside, madecassic acid and madecassoside, exhibit a range of anti-inflammatory, neuroprotective, and cognitive benefits mechanistically linked to mitoprotective and antioxidant properties of the plant. Mitochondrial dysfunction and oxidative stress are key drivers of aging and neurodegenerative disease, including Alzheimer’s disease and Parkinson’s disease. Here we appraise the growing body of evidence that the mitoprotective and antioxidative effects of CA may potentially be harnessed for the treatment of brain aging and neurodegenerative disease.

scholarly journals Inclusion Complexes of β and HPβ-Cyclodextrin with α, β Amyrin and In Vitro Anti-Inflammatory Activity

Biomolecules ◽  
2019 ◽  
Vol 9 (6) ◽  
pp. 241 ◽  
Author(s):  
Walter Ferreira da Silva Júnior ◽  
Danielle Lima Bezerra de Menezes ◽  
Luana Carvalho de Oliveira ◽  
Letícia Scherer Koester ◽  
Patrícia Danielle Oliveira de Almeida ◽  
...  
Keyword(s):  
Inclusion Complexes ◽  
Biological Activities ◽  
Physicochemical Characterization ◽  
Inflammatory Activity ◽  
Scanning Calorimetry ◽  
Promising Alternative ◽  
Wide Range ◽  
Natural Mixture ◽  
Anti Inflammatory

α, β amyrin (ABAM) is a natural mixture of pentacyclic triterpenes that has a wide range of biological activities. ABAM is isolated from the species of the Burseraceae family, in which the species Protium is commonly found in the Amazon region of Brazil. The aim of this work was to develop inclusion complexes (ICs) of ABAM and β-cyclodextrin (βCD) and hydroxypropyl-β-cyclodextrin (HPβCD) by physical mixing (PM) and kneading (KN) methods. Interactions between ABAM and the CD’s as well as the formation of ICs were confirmed by physicochemical characterization in the solid state by Fourier transform infrared (FTIR), scanning electron microscopy (SEM), X-ray diffraction (XRD), thermogravimetry (TG) and differential scanning calorimetry (DSC). Physicochemical characterization indicated the formation of ICs with both βCD and HPβCD. Such ICs were able to induce changes in the physicochemical properties of ABAM. In addition, the formation of ICs with cyclodextrins showed to be an effective and promising alternative to enhance the anti-inflammatory activity and safety of ABAM.

scholarly journals Phytochemical Characterization and Biological Evaluation of the Aqueous and Supercritical Fluid Extracts from Salvia sclareoides Brot

2017 ◽  
Vol 15 (1) ◽  
pp. 82-91
Author(s):  
Daniela Batista ◽  
Pedro L. Falé ◽  
Maria L. Serralheiro ◽  
Maria-Eduarda Araújo ◽  
Catarina Dias ◽  
...  
Keyword(s):  
Linoleic Acid ◽  
Supercritical Fluid ◽  
Antioxidant Properties ◽  
Biological Properties ◽  
Biological Evaluation ◽  
Cyclooxygenase 1 ◽  
Wide Range ◽  
Anti Inflammatory ◽  
Β Carotene

AbstractPlants belonging to the genus Salvia (Lamiaceae) are known to have a wide range of biological properties. In this work, extracts obtained from the aerial parts of Salvia sclareoides Brot. were evaluated to investigate their chemical composition, toxicity, bioactivity, and stability under in vitro gastrointestinal conditions. The composition of the supercritical fluid extract was determined by GC and GC-MS, while the identification of the infusion constituents was performed by HPLC-DAD and LC-MS. The in vitro cytotoxicity of both extracts (0-2 mg/mL) was evaluated in Caco-2 cell lines by the MTT assay. The anti-inflammatory and anticholinesterase activities were determined through the inhibition of cyclooxygenase-1 and acetylcholinesterase enzymes, while β-carotene/linoleic acid bleaching test and the DPPH assays were used to evaluate the antioxidant activity. The infusion inhibited cyclooxygenase-1 (IC50 = 271.0 μg/mL), and acetylcholinesterase (IC50 = 487.7 μg/ mL) enzymes, also demonstrated significant antioxidant properties, as evaluated by the DPPH (IC50 = 10.4 μg/mL) and β-carotene/linoleic acid (IC50 = 30.0 μg/mL) assays. No remarkable alterations in the composition or in the bioactivities of the infusion were observed after in vitro digestion, which supports the potential of S. sclareoides as a source of bioactive ingredients with neuroprotective, anti-inflammatory and antioxidant properties.

scholarly journals Bioactive Bioflavonoids from Platonia insignis (Bacuri) Residues as Added Value Compounds

2021 ◽  
Author(s):  
Dayane Ribeiro ◽  
Helena Russo ◽  
Karina Fraige ◽  
Maria Zeraik ◽  
Cláudio Nogueira ◽  
...  
Keyword(s):  
Liquid Chromatography ◽  
Solid Phase ◽  
Biological Activities ◽  
Drug Carrier ◽  
Antioxidant Properties ◽  
Added Value ◽  
Main Compound ◽  
Anti Inflammatory

Platonia insignis fruit, popularly known as bacuri, is traditionally used in folk medicine for its anti-inflammatory and antioxidant properties. Therefore, this study determined the chemical composition and biological activities of the bacuri’s shell and seeds extracts, considered residues from its consumption and industrial uses. Four biflavonoids (GB-2a, GB-1a, morelloflavone, and volkensiflavone) were identified in the extracts by high-performance liquid chromatography-diode array detection (HPLC-DAD), liquid chromatography tandem mass spectrometry (LC-MS/MS), and liquid chromatography-solid phase extraction-nuclear magnetic resonance (LC-SPE-NMR) techniques. Morelloflavone was identified as the main compound in the shell ethyl acetate extract, being responsible for the high in vitro antioxidant (50% effective concentration (EC50) ranging from 8.0-10.5 µg mL−1 in different protocols), anti-glycant (80%), and moderate inhibition of nitric oxide (1.56 µg mL−1 for > 90% cell viability) activities. This extract showed promising in vivo anti-inflammatory activity evaluated through the paw edema protocol after its incorporation into a liquid-crystalline drug carrier system, reducing the edema by up to 31%. The results demonstrated the potential of the fruit for the development of drugs of natural origin and corroborated to add economic value to these discarded residues.

scholarly journals 2-Arylidene-1-indandiones as Pleiotropic Agents with Antioxidant and Inhibitory Enzymes Activities

Molecules ◽  
2019 ◽  
Vol 24 (23) ◽  
pp. 4411 ◽  
Author(s):  
Olympia Kouzi ◽  
Eleni Pontiki ◽  
Dimitra Hadjipavlou-Litina
Keyword(s):  
Antioxidant Activities ◽  
Biological Activities ◽  
Knoevenagel Reaction ◽  
The Novel ◽  
Hydrophobic Domain ◽  
Antioxidant Agents ◽  
Wide Range ◽  
Anti Inflammatory

Indandiones are a relatively new group of compounds presenting a wide range of biological activities. The synthesis of these compounds was performed via a Knoevenagel reaction between an aldehyde and 1,3-indandione and were obtained with a yield up to 54%. IR, 1H-Nucleic Magnetic Resonance (NMR), 13C-NMR, LC/MS ESI+ and elemental analysis were used for the confirmation of the structures of the novel derivatives. Lipophilicity values of compounds were calculated theoretically and experimentally by reversed chromatography method as values RM. The novel derivatives were studied through in vitro and in vivo experiments for their activity as anti-inflammatory and antioxidant agents and as inhibitors of lipoxygenase, trypsin, and thrombin. The inhibition of the carrageenin-induced paw edema (CPE) was also determined for representative structures. In the above series of experiments, we find that all the compounds showed moderate to satisfying interaction with the stable DPPH free radical in relation to the concentration and the time 2-arylidene-1-indandione (10) was the strongest. We observed moderate or very low antioxidant activities for selected compounds in the decolorization assay with ABTS+•. Most of the compounds showed high anti-lipid peroxidation of linoleic acid induced by AAPH.2-arylidene-1-indandione (7) showed a strongly inhibited soybean LOX. Only 2-arylidene-1-indandione (3) showed moderate scavenging activity of superoxide anion, whereas 2-arylidene-1-indandione (8) and 2-arylidene-1-indandione (9) showed very strong inhibition on proteolysis. 2-arylidene-1-indandione (8) highly inhibited serine protease thrombin. 2-arylidene-1-indandiones (7, 8 and 9) can be used as lead multifunctional molecules. The compounds were active for the inhibition of the CPE (30–57%) with 2-arylidene-1-indandione (1) being the most potent (57%). According to the predicted results a great number of the derivatives can cross the Blood–Brain Barrier (BBB), act in CNS and easily transported, diffused, and absorbed. Efforts are conducted a) to correlate quantitatively the in vitro/in vivo results with the most important physicochemical properties of the structural components of the molecules and b) to clarify the correlation of actions among them to propose a possible mechanism of action. Hydration energy as EHYDR and highest occupied molecular orbital (HOMO) better describe their antioxidant profile whereas the lipophilicity as RM values governs the in vivo anti-inflammatory activity. Docking studies are performed and showed that soybean LOX oxidation was prevented by blocking into the hydrophobic domain the substrates to the active site.

scholarly journals The Antiaging Effect of Active Fractions and Ent-11α-Hydroxy-15-Oxo-Kaur-16-En-19-Oic Acid Isolated from Adenostemma lavenia (L.) O. Kuntze at the Cellular Level

Antioxidants ◽  
2020 ◽  
Vol 9 (8) ◽  
pp. 719
Author(s):  
Irmanida Batubara ◽  
Rika Indri Astuti ◽  
Muhammad Eka Prastya ◽  
Auliya Ilmiawati ◽  
Miwa Maeda ◽  
...  
Keyword(s):  
Mammalian Cells ◽  
Biological Activities ◽  
Antioxidant Properties ◽  
In Vitro Assays ◽  
Mitochondrial Activity ◽  
Related Factor ◽  
Dependent Manner ◽  
B16f10 Cells ◽  
Anti Inflammatory

Background: The extract of Adenostemma lavenia (L.) O. Kuntze leaves has anti-inflammatory activities and is used as a folk medicine to treat patients with hepatitis and pneumonia in China and Taiwan. The diterpenoid ent-11α-hydroxy-15-oxo-kaur-16-en-19-oic acid (11αOH-KA) is the major ingredient in the extract and has wide-spectrum biological activities, such as antitumor and antimelanogenic activities, as well as anti-inflammatory activity. However, the physical and biological properties of this compound as an antioxidant or antiaging agent have not been reported yet. Methods: In addition to in vitro assays, we monitored antioxidative and antiaging signals in Schizosaccharomyces pombe (yeast) and mouse melanoma B16F10 cells. Results: A. lavenia water and chloroform fractions showed antioxidant properties in vitro. The A. lavenia extracts and 11αOH-KA conferred resistance to H2O2 to S. pombe and B16F10 cells and extended the yeast lifespan in a concentration-dependent manner. These materials maintained the yeast mitochondrial activity, even in a high-glucose medium, and induced an antioxidant gene program, the transcriptional factor pap1+ and its downstream ctt1+. Accordingly, 11αOH-KA activated the antioxidative transcription factor NF-E2-related factor 2, NRF2, the mammalian ortholog of pap1+, in B16F10 cells, which was accompanied by enhanced hemeoxygenase expression levels. These results suggest that 11αOH-KA and A. lavenia extracts may protect yeast and mammalian cells from oxidative stress and aging. Finally, we hope that these materials could be helpful in treating COVID-19 patients, because A. lavenia extracts and NRF2 activators have been reported to alleviate the symptoms of pneumonia in model animals.

scholarly journals Turkish Endemic Achillea Species Protect Human Neuroblastoma SH-SY5Y Cells Against Hydrogen Peroxide-Induced Cytotoxicity

Proceedings ◽  
2020 ◽  
Vol 40 (1) ◽  
pp. 43
Author(s):  
Kübra Uzun ◽  
Ayşe Kübra Karaboğa Arslan
Keyword(s):  
Oxidative Stress ◽  
Hydrogen Peroxide ◽  
Phenolic Compounds ◽  
Neurodegenerative Diseases ◽  
Biological Activities ◽  
Antioxidant Properties ◽  
Antioxidant Systems ◽  
Human Neuroblastoma ◽  
Wide Range ◽  
Anti Inflammatory

The genus Achillea L. belongs to Asteraceae (Compositae), the largest family of vascular plants. There are 50 species, which of 24 is endemic in this genus in Turkey. Achillae species are used as a tonic, anti-inflammatory, anti-spasmodic, diaphoretic, diuretic and emmenagogic agents and have been used for treatment of hemorrhage, pneumonia, rheumatic pain and wounds healing traditionally. The imbalanced antioxidant systems leads to various pathophysiological conditions such as inflammation, neurodegenerative diseases and cancer. Achillea species have several components; essential oils, sesquiterpenes and phenolic compounds such as flavonoids and phenolic acids. Phenolic compounds and flavonoids are the most important medicinal metabolites of Achillea species. Flavonoids have been reported to exert a wide range of biological activities including anti-inflammatory, antioxidant and anti-tumor effects. This study aimed to assess the in vitro antioxidant properties of the methanol extracts from the aerial parts of A. cucullata (ACME) and A. sieheana (ASME) against hydrogen peroxide (H2O2)-induced oxidative stress in human SH-SY5Y neuronal cells. Our study showed that the ACME and ASME provided neuroprotection against H2O2-induced oxidative stress. In conclusion, ACME and ASME might help in reducing oxidative stress for preventive therapy associated with neurodegenerative diseases and cancer.

Pharmacologically potentials of different substituted coumarin derivatives

2019 ◽  
Author(s):  
Chem Int
Keyword(s):  
Benzene Ring ◽  
Bioactive Compounds ◽  
Biological Activities ◽  
Pharmacological Properties ◽  
Coumarin Derivatives ◽  
Wide Range ◽  
Anti Oxidant ◽  
Anti Inflammatory ◽  
Coumarin Compounds

Coumarin and its derivatives are widely spread in nature. Coumarin goes to agroup as benzopyrones, which consists of a benzene ring connected to a pyronemoiety. Coumarins displayed a broad range of pharmacologically useful profile.Coumarins are considered as a promising group of bioactive compounds thatexhibited a wide range of biological activities like anti-microbial, anti-viral,antiparasitic, anti-helmintic, analgesic, anti-inflammatory, anti-diabetic, anticancer,anti-oxidant, anti-proliferative, anti-convulsant, and antihypertensiveactivities etc. The coumarin compounds have immense interest due to theirdiverse pharmacological properties. In particular, these biological activities makecoumarin compounds more attractive and testing as novel therapeuticcompounds.

A Brief Review on the Development of Novel Potentially Active Azetidin-2-ones Against Cancer

2020 ◽  
Vol 24 (5) ◽  
pp. 473-486 ◽  
Author(s):  
Ligia S. da Silveira Pinto ◽  
Thatyana R. Alves Vasconcelos ◽  
Claudia Regina B. Gomes ◽  
Marcus Vinícius N. de Souza
Keyword(s):  
Side Effects ◽  
Anticancer Agents ◽  
Heterocyclic Compounds ◽  
Biological Activities ◽  
Present Review ◽  
Pharmacological Properties ◽  
Important Group ◽  
Wide Range ◽  
Anti Inflammatory

Azetidin-2-ones (β-lactams) and its derivatives are an important group of heterocyclic compounds that exhibit a wide range of pharmacological properties such as antibacterial, anticancer, anti-diabetic, anti-inflammatory and anticonvulsant. Efforts have been made over the years to develop novel congeners with superior biological activities and minimal potential for undesirable side effects. The present review aimed to highlight some recent discoveries (2013-2019) on the development of novel azetidin-2-one-based compounds as potential anticancer agents.

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