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 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 Anti-Inflammatory Effects of Formononetin 7-O-phosphate, a Novel Biorenovation Product, on LPS-Stimulated RAW 264.7 Macrophage Cells

Molecules ◽  
2019 ◽  
Vol 24 (21) ◽  
pp. 3910 ◽  
Author(s):  
Min-Seon Kim ◽  
Jin-Soo Park ◽  
You Chul Chung ◽  
Sungchan Jang ◽  
Chang-Gu Hyun ◽  
...  
Keyword(s):  
Biological Properties ◽  
In Vitro Assays ◽  
Raw 264.7 Cells ◽  
No Production ◽  
Raw 264.7 ◽  
Dependent Manner ◽  
Macrophage Cells ◽  
Anti Inflammatory ◽  
Reduced Toxicity

Biorenovation is a microbial enzyme-catalyzed structural modification of organic compounds with the potential benefits of reduced toxicity and improved biological properties relative to their precursor compounds. In this study, we synthesized a novel compound verified as formononetin 7-O-phosphate (FMP) from formononetin (FM) using microbial biotransformation. We further compared the anti-inflammatory properties of FMP to FM in lipopolysaccharide (LPS)-treated RAW264.7 macrophage cells. We observed that cell viabilities and inhibitory effects on LPS-induced nitric oxide (NO) production were greater in FMP-treated RAW 264.7 cells than in their FM-treated counterparts. In addition, FMP treatment suppressed the production of proinflammatory cytokines such as prostaglandin-E2 (PGE2), interleukin-6 (IL-6), and interleukin-1β (IL-1β) in a dose-dependent manner and concomitantly decreased the mRNA expression of inducible NO synthase (iNOS) and cyclooxygenase-2 (COX-2). We also found that FMP exerted its anti-inflammatory effects through the downregulation of the extracellular signal-regulated kinase (ERK), c-Jun N-terminal kinase (JNK), and nuclear factor kappa B (NF-κB) signaling pathways. In conclusion, we generated a novel anti-inflammatory compound using biorenovation and demonstrated its efficacy in cell-based in vitro assays.

scholarly journals Antioxidant and Anti-Inflammatory Activities of Safflower (Carthamus tinctorius L.) Honey Extract

Foods ◽  
2020 ◽  
Vol 9 (8) ◽  
pp. 1039
Author(s):  
Li-Ping Sun ◽  
Feng-Feng Shi ◽  
Wen-Wen Zhang ◽  
Zhi-Hao Zhang ◽  
Kai Wang
Keyword(s):  
Chemical Composition ◽  
Biological Activities ◽  
Carthamus Tinctorius ◽  
Raw 264.7 Cells ◽  
Dependent Manner ◽  
Concentration Dependent Manner ◽  
Unique Type ◽  
Antioxidant Genes ◽  
Anti Inflammatory

Safflower honey is a unique type of monofloral honey collected from the nectar of Carthamus tinctorius L. in the Apis mellifera colonies of northwestern China. Scant information is available regarding its chemical composition and biological activities. Here, for the first time, we investigated this honey’s chemical composition and evaluated its in vitro antioxidant and anti-inflammatory activities. Basic physicochemical parameters of the safflower honey samples in comparison to established quality standards suggested that safflower honeys presented a good level of quality. The in vitro antioxidant tests showed that extract from Carthamus tinctorius L. honey (ECH) effectively scavenged DPPH and ABTS+ free radicals. In lipopolysaccharides (LPS) activated murine macrophages inflammatory model, ECH treatment to the cells inhibited the release of nitric oxide and down-regulated the expressions of inflammatory-relating genes (iNOS, IL-1β, TNF-α and MCP-1). The expressions of the antioxidant genes TXNRD, HO-1, and NQO-1, were significantly boosted in a concentration-dependent manner. ECH decreased the phosphorylation of IκBα and inhibited the nuclear entry of the NF-κB-p65 protein, in LPS-stimulated Raw 264.7 cells, accompany with the increased expressions of Nrf-2 and HO-1, suggesting that ECH achieved the anti-inflammatory effects by inhibiting NF-κB signal transduction and boosting the antioxidant system via activating Nrf-2/HO-1 signaling. These results, taken together, indicated that safflower honey has great potential into developing as a high-quality agriproduct.

scholarly journals Anti-Inflammatory and Antinociceptive Activity of Pollen Extract Collected by Stingless Bee Melipona fasciculata

2019 ◽  
Vol 20 (18) ◽  
pp. 4512 ◽  
Author(s):  
Alberto Jorge Oliveira Lopes ◽  
Cleydlenne Costa Vasconcelos ◽  
Francisco Assis Nascimento Pereira ◽  
Rosa Helena Moraes Silva ◽  
Pedro Felipe dos Santos Queiroz ◽  
...  
Keyword(s):  
Native Species ◽  
Biological Activities ◽  
Stingless Bee ◽  
In Vitro Assays ◽  
Pollen Extract ◽  
Biological Potential ◽  
Anti Inflammatory ◽  
Analgesic Activities

The stingless bee, Melipona fasciculata Smith (Apidae, Meliponini), is a native species from Brazil. Their products have high biotechnological potential, however there are no studies about the biological activities of pollen collected by M. fasciculata. In this context, the present study investigated the chemical composition, anti-oxidant, anti-inflammatory, and analgesic activities of hydroethanolic pollen extracts collected by M. fasciculata in three cities in Maranhão State, Brazil. We verified the antioxidant activity of the extracts and inhibitory activity against the cyclooxygenase enzyme using in vitro assays and in allowed to select the extract with higher efficiency to be used on in vivo assays. In these trials, the selected extract showed high anti-inflammatory activity as well as nociceptive effects at central and peripheral level, suggesting that this extract acts on inhibition of histamine release and decreased synthesis of prostaglandins and the in-silico study suggested that polyphenols and acids fatty acids in the extract may be associated with these activities. The results of the present study report the high biological potential of pollen extract and we conclude that the pollen collected by M. fasciculata can be considered as the object of research for new pharmacological alternatives.

scholarly journals Synthesis and Evaluation of Biological Activities of Bis(spiropyrazolone)cyclopropanes: A Potential Application against Leishmaniasis

Molecules ◽  
2021 ◽  
Vol 26 (16) ◽  
pp. 4960
Author(s):  
Olalla Barreiro-Costa ◽  
Gabriela Morales-Noboa ◽  
Patricio Rojas-Silva ◽  
Eliana Lara-Barba ◽  
Javier Santamaría-Aguirre ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
In Silico ◽  
Potential Application ◽  
Mammalian Cells ◽  
Biological Activities ◽  
Antioxidant Properties ◽  
Therapeutic Use ◽  
Derivatives Of

This work focuses on the search and development of drugs that may become new alternatives to the commercial drugs currently available for treatment of leishmaniasis. We have designed and synthesized 12 derivatives of bis(spiropyrazolone)cyclopropanes. We then characterized their potential application in therapeutic use. For this, the in vitro biological activities against three eukaryotic models—S. cerevisiae, five cancer cell lines, and the parasite L. mexicana—were evaluated. In addition, cytotoxicity against non-cancerous mammalian cells has been evaluated and other properties of interest have been characterized, such as genotoxicity, antioxidant properties and, in silico predictive adsorption, distribution, metabolism, and excretion (ADME). The results that we present here represent a first screening, indicating two derivatives of bis(spiropyrazolone)cyclopropanes as good candidates for the treatment of leishmaniasis. They have good specificity against parasites with respect to mammalian cells.

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.

In Vitro and In Vivo Experimental Model-based Approaches for Investigating Anti-inflammatory Properties of Coumarins

2018 ◽  
Vol 25 (12) ◽  
pp. 1446-1476 ◽  
Author(s):  
Silvana Virginia Gagliotti Vigil de Mello ◽  
Tania Silvia Frode
Keyword(s):  
Antioxidant Activities ◽  
Orphan Receptor ◽  
Mitogen Activated Protein Kinase ◽  
In Vitro Assays ◽  
Related Factor ◽  
Nuclear Factor ◽  
Activated T Cells ◽  
Anti Inflammatory

Background: Coumarins are polyphenolic compounds that are often used to treat inflammatory conditions in complementary and alternative medicine. Objective: In this study, we reviewed reports of in vivo and in vitro experimental modelbased approaches investigating the potential anti-inflammatory properties of coumarins. Methods: A literature search of PUBMED, MEDLINE, Web of Science, and Scopus was performed covering the period from 1 January 2005 to 31 December 2015. The keywords used to search were ‘anti-inflammatory' and ‘coumarin' and ‘in vivo' or ‘in vitro'. This search identified 425 article titles. Results: Of the 425 article titles, 127 full-text articles were reviewed, and 69 of them were included in the analysis. Most of the studies (81.2%) used in vitro assays. The studies focused on cytokines such as tumour necrosis factor (TNF), interleukin (IL)-6, and IL-1-β (55.1%), as well as oedema (46.5%), nitric oxide (NO, 23.2%), oxidative stress (21.7%), inflammatory cells (21.7%), nuclear factor (NF)-κB (24.6%), mitogen-activated protein kinase (MAPK, 13%), myeloperoxidase (MPO, (15.9%), cyclooxygenase (COX)-2 (14.5%), prostaglandin E2 (PGE2, 8.7%), 5-lipoxygenase (LOX, 4.3%), and adhesion molecules (7.2%). Coumarins inhibited all these parameters except for IL-10, nuclear factor erythroid 2 (NFE2)-related-factor 2 (Nrf2), and regulatory T cell (Treg) differentiation. Conclusion: In vitro methods were the most commonly used to study the antiinflammatory effects of coumarins. The results showed that coumarins exerted antiinflammatory and antioxidant activities by inhibiting NF-κB, nuclear factor of activated T cells (NFAT), retinoic acid-related orphan receptor γτ (RORγτ), and MAPK and increasing Nrf2 activation. These results suggest that coumarins could be important candidates for the development of novel anti-inflammatory therapeutic drugs.

scholarly journals Assessment of the Quality and Evaluation of the Antioxidant Potential of a Novel Sri Lankan Ayurvedic Polyherbal Formulation

2020 ◽  
Vol 2020 ◽  
pp. 1-7
Author(s):  
H. P. Wakkumbura ◽  
W. M. D. Wickramaarachchi ◽  
L. D. A. M. Arawwawala ◽  
J. A. Liyanage ◽  
R. P. V. J. Rajapakse
Keyword(s):  
Cold Water ◽  
Antioxidant Properties ◽  
Water Soluble ◽  
Hot Water ◽  
Antioxidant Potential ◽  
In Vitro Assays ◽  
Phytochemical Screening ◽  
Anti Inflammatory ◽  
Water Extractable

Background. In Sri Lanka, a Polyherbal Ayurvedic Formulation (PHAF), which consists of powders of seven medicinal plants, is being trialed for use as an anti-inflammatory drug. In general, anti-inflammatory drugs have good antioxidant properties. Therefore, in the present study, an attempt was made to assess the quality and evaluate the antioxidant potential of PHAF. Methods. Physicochemical parameters such as ash content, extractable matter, phytochemical screening for secondary metabolites, levels of heavy metals, and microbes were determined according to standard protocols. Antioxidant activity was evaluated using five in vitro assays: total polyphenolic content (TPC), total flavonoid content (TFC), ORAC (oxygen radical absorbance capacity), DPPH (1,1-diphenyl-2-picryl-hydrazyl), and ABTS (2,2-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt. Results. PHAF contained 5.6 ± 0.2% of moisture, 6.5 ± 0.1% of total ash, 1.4 ± 0.1% of water soluble ash, 0.9 ± 0.0% of acid insoluble ash, 7.7 ± 0.2% of hot water extractable matter, 3.9 ± 0.1% of cold water extractable matter, 10.5 ± 4.1% of hot-ethanol extractable matter, and 8.4 ± 0.2% of cold-ethanol extractable matter. Phytochemical screening revealed the presence of phenolic compounds, tannins, flavonoids, coumarins, and saponins in both aqueous and ethanolic extracts of the drug. TPC, TFC, ORAC, DPPH, and ABTS of aqueous and ethanol extracts of PHAF were 103.65 ± 4.94 and 327.07 ± 9.65 mg gallic acid equivalents/g extract, 76.6 ± 5.83 and 224.6 ± 8.42 mg quercetin equivalents/g of extract, 481.11 ± 17.30 and 1481.44 ± 30.20 mg trolox equivalents/g of extract, 79.50 ± 4.42 and 227.17 ± 6.16 mg trolox equivalents/g of extract, and 198.20 ± 4.55 and 577.08 ± 5.48 mg trolox equivalents/g of extract, respectively. Conclusion. Ethanolic extract of PHAF is better than aqueous extract in terms of antioxidant properties.

scholarly journals 7-Acetoxycoumarin Inhibits LPS-Induced Inflammatory Cytokine Synthesis by IκBα Degradation and MAPK Activation in Macrophage Cells

Molecules ◽  
2020 ◽  
Vol 25 (14) ◽  
pp. 3124 ◽  
Author(s):  
Taejin Park ◽  
Jin-Soo Park ◽  
Ji Han Sim ◽  
Seung-Young Kim
Keyword(s):  
Inflammatory Cytokines ◽  
Mitogen Activated Protein Kinase ◽  
In Vitro Assays ◽  
Raw 264.7 ◽  
Dependent Manner ◽  
Concentration Dependent Manner ◽  
Macrophage Cells ◽  
Anti Inflammatory ◽  
Pro Inflammatory Cytokines

Acetylation involves the chemical introduction of an acetyl group in place of an active hydrogen group into a compound. In this study, we synthesized 7-acetoxycoumarin (7AC) from acetylation of umbelliferone (UMB). We examined the anti-inflammatory properties of 7AC in lipopolysaccharide (LPS)-treated RAW 264.7 macrophage cells. The anti-inflammatory activity of 7AC on viability of treated cells was assessed by measuring the level of expression of NO, PGE2 and pro-inflammatory cytokines, namely interleukin-1β (IL-1β), interleukin-6 (IL-6) and tumor necrosis factor-α (TNF-α) in 7AC-treated RAW 264.7 macrophages. The 7AC was nontoxic to cells and inhibited the production of cytokines in a concentration-dependent manner. In addition, its treatment suppressed the production of pro-inflammatory cytokines in a dose-dependent manner and concomitantly decreased the protein and mRNA expressions of inducible NO synthase (iNOS) and cyclooxygenase-2 (COX-2). Moreover, the levels of the phosphorylation of mitogen-activated protein kinase (MAPK) family proteins such as extracellular signal-regulated kinase (ERK), c-Jun N-terminal kinase (JNK), p38 and nuclear factor kappa B (NF-κB) were reduced by 7AC. In conclusion, we generated an anti-inflammatory compound through acetylation and demonstrated its efficacy in cell-based in vitro assays.

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.

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