Decreased Human Platelet Activation and Mouse Pulmonary Thrombosis by Rutaecarpine and Comparison of the Relative Effectiveness with BAY11-7082: Crucial Signals of p38-NF-κB

Platelets play a critical role in arterial thrombosis. Rutaecarpine (RUT) was purified from Tetradium ruticarpum, a well-known Chinese medicine. This study examined the relative activity of RUT with NF-κB inhibitors in human platelets. BAY11-7082 (an inhibitor of IκB kinase [IKK]), Ro106-9920 (an inhibitor of proteasomes), and RUT concentration-dependently (1–6 μM) inhibited platelet aggregation and P-selectin expression. RUT was found to have a similar effect to that of BAY11-7082; however, it exhibits more effectiveness than Ro106-9920. RUT suppresses the NF-κB pathway as it inhibits IKK, IκBα, and p65 phosphorylation and reverses IκBα degradation in activated platelets. This study also investigated the role of p38 and NF-κB in cell signaling events and found that SB203580 (an inhibitor of p38) markedly reduced p38, IKK, and p65 phosphorylation and reversed IκBα degradation as well as p65 activation in a confocal microscope, whereas BAY11-7082 had no effects in p38 phosphorylation. The 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay shows that RUT and BAY11-7082 did not exhibit free radical scavenging activity. In the in vivo study, compared with BAY11-7082, RUT more effectively reduced mortality in adenosine diphosphate (ADP)-induced acute pulmonary thromboembolism without affecting the bleeding time. In conclusion, a distinctive pathway of p38-mediated NF-κB activation may involve RUT-mediated antiplatelet activation, and RUT could act as a strong prophylactic or therapeutic drug for cardiovascular diseases.

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Halofuginone functions as a therapeutic drug for chronic periodontitis in a mouse model

International Journal of Immunopathology and Pharmacology ◽

10.1177/2058738420974893 ◽

2020 ◽

Vol 34 ◽

pp. 205873842097489

Author(s):

Jiang Wang ◽

Bo Wang ◽

Xin Lv ◽

Yingjie Wang

Keyword(s):

Alveolar Bone ◽

Immune Cell ◽

Critical Role ◽

Therapeutic Drug ◽

Mice Model ◽

T Helper 17 ◽

Th17 Cell Differentiation ◽

Tnf Α

Periodontitis is an inflammatory disease caused by host immune response, resulting in a loss of periodontium and alveolar bone. Immune cells, such as T cells and macrophages, play a critical role in the periodontitis onset. Halofuginone, a natural quinazolinone alkaloid, has been shown to possess anti-fibrosis, anti-cancer, and immunomodulatory properties. However, the effect of halofuginone on periodontitis has never been reported. In this study, a ligature-induced mice model of periodontitis was applied to investigate the potential beneficial effect of halofuginone on periodontitis. We demonstrated that the administration of halofuginone significantly reduced the expression levels of pro-inflammatory cytokines (IL-1β, IL-6, and TNF-α) in vivo, and markedly suppressed immune cell infiltration into the infected sites. Furthermore, we also observed that halofuginone treatment blocked the T-helper 17 (Th17) cell differentiation in vivo and in vitro. We demonstrated for the first time that halofuginone alleviated the onset of periodontitis through reducing immune responses.

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Study of Antimicrobial, Antioxidant and Cytotoxicity Properties of Selected Plant Extracts for Food Preservative Applications

International Journal of Food Studies ◽

10.7455/ijfs/10.si.2021.a8 ◽

2021 ◽

pp. 95-111

Author(s):

Tania Islam ◽

Md Nazrul Islam ◽

Wahidu Zzaman ◽

Md Morsaline Billah

Keyword(s):

Pathogenic Bacteria ◽

Radical Scavenging Activity ◽

Radical Scavenging ◽

Antimicrobial Properties ◽

In Vivo Studies ◽

Diffusion Method ◽

Plant Materials ◽

Food Preservative

An attempt has been made to evaluate antimicrobial, antioxidant and cytotoxicity properties of extracts from onion (Allium cepa L.), garlic (Allium sativum), leaves of guava (Psidium guajava), papaya (Carica papaya), tea (Camellia sinensis), baen (Avicennia alba) and keora (Sonneratia apetala), respectively to apply as natural preservatives for tomatoes. The air-dried plant materials of the respective plant species were subjected to ethanol-methanol extraction, concentrated and stored at 4 °C before use. The extracts were dissolved in 95% ethanol for analysis of antioxidant and antimicrobial properties. Of the extracts tested, tea extracts showed the highest zone of inhibition against several pathogenic bacteria (E. coli 35.0±3.2 mm; P. aeruginosa 29.3±2.6 mm; S. typhi 28.4±2.1 mm and S. pyogenes 27.7±3.7 mm) using the disc diffusion method. In regard to DPPH free radical scavenging assay, keora and guava extracts showed the highest percentage of radical scavenging activity with the values of 89.64± 0.18 and 89.39± 0.88, respectively, which were in agreement with higher total antioxidant capacity (TAC) of these extracts obtained by the phosphomolybdenum method. Brine shrimp lethality bioassay for cytotoxicity assessment showed LC50 of 132.54 ± 18.99 µg/mL for the leaf extract of keora which was found to be most toxic among all studied extracts. The initial results indicated that the extracts could be used for food preservative applications based on the antimicrobial, antioxidant and cytotoxicity properties of the tested extracts. However, efficacy, stability and safety issues need to be addressed with both in vitro and in vivo studies.

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Chromatographic Analysis and Anti-Oxidative Property of Naoxinqing Tablet, a Proprietary Preparation of Diospyros Kaki Leaves

Molecules ◽

10.3390/molecules24061101 ◽

2019 ◽

Vol 24 (6) ◽

pp. 1101 ◽

Cited By ~ 1

Author(s):

Magdy Kazzem ◽

Yu-Ting Sun ◽

Mitchell Low ◽

Sai Seto ◽

Dennis Chang ◽

...

Keyword(s):

Cell Injury ◽

Vascular Endothelial Cells ◽

Radical Scavenging Activity ◽

Critical Role ◽

Radical Scavenging ◽

Herbal Product ◽

Ros Generation ◽

Diospyros Kaki ◽

Bioactive Components ◽

Oxidative Property

The Naoxinqing (NXQ) tablet is a standardised proprietary herbal product containing an extract of persimmon leaves (Diospyros kaki) for the management of cardio- and cerebrovascular diseases. Although previous reports suggested that the efficacy of NXQ is at least partly mediated by its anti-oxidative property, the anti-oxidative effect of the major components of NXQ has not been studied systematically. For quality control purposes, only analytical methods limited to 3 marker analytes have been reported, the extent to which the other components affect efficacy has not been explored. In this study, we developed an ultra-performance liquid chromatography-tandem mass spectrometry (UPLC MS/MS) method for the identification of seven analytes (kaempferol-3-O-glucoside (astragalin), quercetin-3-O-galactoside (hypericin), quercetin-3-O-glucoside (isoquercitin), kaempferol, 3,4-dihydroxybenzoic acid (protocatechuic acid), and furan-2-carboxylic acid (pyromucic acid) and quercetin) in the NXQ. This is the first method reported and validated for the quantification of the seven major secondary metabolites in NXQ. The results for the quantified analytes were then compared in 15 different batches of NXQ. The variation observed in the seven components highlights the need to quantify key bioactive components to ensure product consistency. Radical scavenging activity and abundance was used to rank the analytes. The anti-oxidative effects of NXQ were examined using cultured human vascular endothelial cells (EA.hy926). Corrected 2,2-di(4-tert-octylphenyl)-1-picrylhydrazyl (DPPH) activity results revealed that quercetin and kaempferol have the strongest anti-oxidant capacity in the extract. Both quercetin and kaempferol significantly inhibited the hydrogen peroxide (H2O2)-induced EA.hy926 cell injury and intracellular reactive oxygen species (ROS) generation. In conclusion, we established and validated an UPLC-MS/MC method for the analysis of major bioactive components in the NXQ and demonstrated that its anti-oxidative property may play a critical role in cerebrovascular protection.

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Agrimonia procera Wallr. Extract Increases Stress Resistance and Prolongs Life Span in Caenorhabditis elegans via Transcription Factor DAF-16 (FoxO Orthologue)

Antioxidants ◽

10.3390/antiox7120192 ◽

2018 ◽

Vol 7 (12) ◽

pp. 192 ◽

Cited By ~ 2

Author(s):

Christina Saier ◽

Inge Gommlich ◽

Volker Hiemann ◽

Sabrina Baier ◽

Karoline Koch ◽

...

Keyword(s):

Transcription Factor ◽

Caenorhabditis Elegans ◽

Life Span ◽

Stress Resistance ◽

Radical Scavenging Activity ◽

Radical Scavenging ◽

Model Organism ◽

Amyloid Β ◽

Ethanol Extract

Agrimonia procera is a pharmacologically interesting plant which is proposed to protect against various diseases due to its high amount of phytochemicals, e.g., polyphenols. However, in spite of the amount of postulated health benefits, studies concerning the mechanistic effects of Agrimonia procera are limited. Using the nematode Caenorhabditis elegans, we were able to show that an ethanol extract of Agrimonia procera herba (eAE) mediates strong antioxidative effects in the nematode: Beside a strong radical-scavenging activity, eAE reduces accumulation of reactive oxygen species (ROS) accumulation and protects against paraquat-induced oxidative stress. The extract does not protect against amyloid-β-mediated toxicity, but efficiently increases the life span (up to 12.7%), as well as the resistance to thermal stress (prolongation of survival up to 22%), of this model organism. Using nematodes deficient in the forkhead box O (FoxO)-orthologue DAF-16, we were able to demonstrate that beneficial effects of eAE on stress resistance and life span were mediated via this transcription factor. We showed antioxidative, stress-reducing, and life-prolonging effects of eAE in vivo and were able to demonstrate a molecular mechanism of this extract. These results may be important for identifying further molecular targets of eAE in humans.

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A Review of Recent Studies on the Antioxidant Activities of a Third-Millennium Food: Amaranthus spp.

Antioxidants ◽

10.3390/antiox9121236 ◽

2020 ◽

Vol 9 (12) ◽

pp. 1236

Author(s):

Seon-Joo Park ◽

Anshul Sharma ◽

Hae-Jeung Lee

Keyword(s):

Antioxidant Activity ◽

Bioactive Peptides ◽

Antioxidant Activities ◽

Radical Scavenging Activity ◽

Radical Scavenging ◽

Sustainable Food ◽

Amaranth Species ◽

Amaranthus Spp

Amaranth (Amaranthus spp.) plant commonly refers to the sustainable food crop for the 21st century. The crop has witnessed significant attention in recent years due to its high nutritional value and agronomic advantages. It is a relatively well-balanced cosmopolitan food that is a protector against chronic diseases. Usually, the antioxidant activities of amaranth are held responsible for its defensive behavior. Antioxidant activity of plants, generally, is attributed to their phytochemical compounds. The current interest, however, lies in hydrolysates and bioactive peptides because of their numerous biological functions, including antioxidant effect. While the importance of bioactive peptides has been progressively recognized, an integrated review of recent studies on the antioxidant ability of amaranth species, especially their hydrolysates and peptides has not been generated. Hence, in this review, we summarize studies focused on the antioxidant capacity of amaranth renewal over the period 2015–2020. It starts with a background and overall image of the amaranth-related published reviews. The current research focusing on in vitro, in vivo, and chemical assays-based antioxidant activity of different amaranth species are addressed. Finally, the last segment includes the latest studies concerning free radical scavenging activity and metal chelation capacity of amaranth protein hydrolysates and bioactive peptides.

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Neutralization Effect of Tithonia diversifolia (Hemsl.) A. Gray against Bitis arietans and Naja nigricollis venoms-induced toxicity

Ethiopian Pharmaceutical Journal ◽

10.4314/epj.v35i1.4 ◽

2020 ◽

Vol 35 (1) ◽

pp. 41-50

Author(s):

Adebayo Gbolade ◽

Ifunanya Ukaigwe ◽

Anastasia Omorogbe

Keyword(s):

Platelet Aggregation ◽

Methanol Extract ◽

Radical Scavenging Activity ◽

Radical Scavenging ◽

Adenosine Diphosphate ◽

Total Phenolic ◽

Total Phenol Content ◽

Tithonia Diversifolia ◽

Aqueous Fraction ◽

Active Inhibitor

Leaf methanol extract and fractions of Tithonia diversifolia (Hemsl.) A. Gray (Asteraceae) used in traditional medicine was evaluated for neutralization of toxicity induced by Bitis arietans and Naja nigricollis snake venoms in mice and rats. Inhibition of adenosine diphosphate-induced platelet aggregation, antioxidant activity, total phenol content and neutralization of venom-induced toxicity were evaluated by standard methods. The methanol extract was the most active inhibitor of platelet aggregation (66.7 - 84.8%) in the B. arietans model at 100 - 500 μg/ml. The methanol extract and fractions appear to be equipotent in inhibiting platelet aggregation (68 - 74%) induced by N. nigricollis. The aqueous fraction was more active against B. arietans venom at 500 μg/ml as an inhibitor of platelet aggregation (59.4% inhibition), while the dichloromethane (DCM) fraction was more potent against N. nigricollis (70.97% inhibition). The methanol extract showed highest DPPH radical scavenging activity followed by the aqueous and DCM fractions. Total phenolic content was in the order: methanol extract > DCM fraction > aqueous fraction. The aqueous fraction was a better antivenin agent in both B. arietans (complete protection at 24 h) and N. nigricollis-envenomed mice and rat models. Anti-snake venom activity was more prominent at 24 h. The results herein, being the very first report, indicate the potential antiophidic activity of T. diversifolia leaf particularly against B. arietans-induced toxicity.

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Comparative Real Time EPR Investigation of Natural and Synthetic Antioxidants: As Potential Anticancer Agents and Radio-protectors

Defence Life Science Journal ◽

10.14429/dlsj.2.11676 ◽

2017 ◽

Vol 2 (3) ◽

pp. 301

Author(s):

Yanka Karamalakova ◽

Galina Nikolova ◽

Rakesh Kumar Sharma ◽

Raj Kumar ◽

Rajesh Arora ◽

...

Keyword(s):

Free Radical ◽

Anticancer Agents ◽

Antioxidant Activities ◽

Radical Scavenging Activity ◽

Radical Scavenging ◽

Natural Antioxidants ◽

Synthetic Antioxidants ◽

Anticancer Chemotherapy ◽

Natural And Synthetic

<p>The purpose of this study was to evaluate and compare the free-radical scavenging activity against DPPH stable radical and protective properties of the natural products SQGD and P. corylifolia and synthetic nitroxyl- free radical containing nitrosoureas SLENU and SLCNUgly against in vivo oxidative toxicity of antitumor drug CCNU. It was found statistically significant increase in the DPPH radical-scavenging capacity of both extracts with increase of radiation. The natural antioxidants were localised mainly in the organs and blood after EPR biodistribution study. All combinations of natural extracts/ synthetics agents exhibited considerably lower levels of Asc. radicals as compared to controls. It should be mentioned that the natural antioxidants possess higher oxidative protection in comparison with the synthetic antioxidants. Considerable decrease in ROS production in livers of mice was found after treatment with SQGD, P. corylifolia and SLENU, alone, compared to controls.In conclusion, because of well-expressed antioxidant activities of natural and synthetic antioxidants they might be used in the combination anticancer chemotherapy for reducing toxicity caused by anticancer drugs and/or low levels radiation therapy.</p>

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In Vivo Processing of Ceria Nanoparticles inside Liver: Impact on Free-Radical Scavenging Activity and Oxidative Stress

ChemPlusChem ◽

10.1002/cplu.201402080 ◽

2014 ◽

Vol 79 (8) ◽

pp. 1083-1088 ◽

Cited By ~ 49

Author(s):

Uschi M. Graham ◽

Michael T. Tseng ◽

Jacek B. Jasinski ◽

Robert A. Yokel ◽

Jason M. Unrine ◽

...

Keyword(s):

Oxidative Stress ◽

Free Radical ◽

Radical Scavenging Activity ◽

Radical Scavenging ◽

Free Radical Scavenging ◽

Free Radical Scavenging Activity ◽

Scavenging Activity ◽

Ceria Nanoparticles ◽

And Oxidative Stress

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Evaluation of Anti-Inflammatory and Analgesic Activities of Methanolic Extract of Aitchisonia Rosea in Albino Mice

RADS Journal of Pharmacy and Pharmaceutical Sciences ◽

10.37962/jpps.v8i1.371 ◽

2020 ◽

Vol 8 (1) ◽

pp. 31-36

Author(s):

Shahid Rasool ◽

Ambreen Malik Uttra ◽

Mehreen Malik Uttra ◽

Faheem Ahmed ◽

Khizar Abbas

Keyword(s):

Acetic Acid ◽

Methanolic Extract ◽

Radical Scavenging Activity ◽

Radical Scavenging ◽

Paw Edema ◽

Egg Albumin ◽

Inflammatory Conditions ◽

Albino Mice ◽

Anti Inflammatory

Objective: Current analysis aims at in-vivo investigation of analgesic and anti-inflammatory activities of Aitchisonia rosea methanolic extract. Methods: Albino mice (20-30 g) were used in the study. Extract at 200, 400 and 800 mg/kg doses was tested against egg albumin and carrageenan induced mice paw edema along with formalin persuaded paw licking and acetic acid prompted writhing for analgesic activity. Results: Results depicted dose reliant and significant (p<0.001) inhibition of carrageenan as well as egg albumin brought paw edema, abdominal constrictions/ hind limb stretching tempted by acetic acid and formalin instigated paw licking. Capability of crude extract to halt inflammatory and analgesic response was akin to that of ibuprofen in all models. Conclusion: The current findings support the use of Aitchisonia rosea for inflammatory conditions, which might be attributed to its previously proven high alkaloid, flavonoids, phenol, tannins content and free radical scavenging activity.

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Role of antioxidants in the treatment of hepatocellular carcinoma: Integrative review

Research Society and Development ◽

10.33448/rsd-v10i1.12028 ◽

2021 ◽

Vol 10 (1) ◽

pp. e46310112028

Author(s):

Claudriana Locatelli ◽

Joyce Kelly Busolin Jardim ◽

Vilmair Zancanaro

Keyword(s):

Hepatocellular Carcinoma ◽

Radical Scavenging Activity ◽

Treatment Options ◽

Radical Scavenging ◽

Integrative Review ◽

Advanced Hepatocellular Carcinoma ◽

Rate Dependent

Theorical framework: Hepatocellular carcinoma is a unique cancer that typically arises in the setting of chronic liver disease at a rate dependent upon the complex interplay between the host, disease, and environmental factors. Unfortunately, with contemporary management, patients with advanced hepatocellular carcinoma have few treatment options, and the prognosis is poor. Objective: Evaluate the role of antioxidants in the treatment of hepatocellular carcinoma. Methodology: It is an integrative review, with a qualitative approach. Based on research on ScienceDirect and PubMed databases, 12 articles were selected that were consistent with the theme and the inclusion and exclusion criteria, through the association of descriptors and keywords. Results: Studies in vivo demonstrated a positive correlation of antioxidants in the treatment of hepatocellular carcinoma. The antioxidants were able to promote inhibition of development tumor through promotes decrease of proinflammatory cytokines IL-1 and IL-6 and changes the ratios of Bax/Bcl2 that supports apoptosis. In oxidative stress, may be able to direct free radical scavenging activity. Among the main antioxidants with advanced preclinical evidence in the treatment of hepatocellular carcinoma is curcumin with tests in humans, and gallic acid, quercetin and resveratrol with several tests in vitro and in vivo. Conclusion: This study highlights that antioxidants can be a promising therapy in the treatment of hepatocellular carcinoma.

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