Furcellaran-Coated Microcapsules as Carriers of Cyprinus carpio Skin-Derived Antioxidant Hydrolysate: An In Vitro and In Vivo Study

Carp skin gelatine hydrolysate (CSGH) may be a possible bioactive peptide source, as promising antioxidant properties have been noted during in vivo testing. Hence, the present study focused on improving the bioavailability of the antioxidant peptides from CSGH and on the use of furcellaran (FUR), which can protect the biopeptides during digestion in the gastrointestinal tract. Therefore, in this study, microcapsules coated with furcellaran and containing CSGH cores were prepared. The structural properties of the sample were determined using FT-IR and SEM analysis. The antioxidant properties of hydrolysate, uncoated, and encapsulated samples were investigated. In vivo analysis included determination of its safety in an animal organism and evaluation of the lipid profile, antioxidant blood status, and mRNA expression of some genes involved in antioxidant status in Wistar rats. The results showed no adverse effects of microencapsulated protein hydrolysates in laboratory animals. Nonetheless, there was a statistically significant rise in the level of total antioxidant status blood serum among animals consuming CSGH and not inducing oxidative stress. This can be viewed as a promising indication of the positive effects of antioxidant properties tested in vivo. The process of CSGH microencapsulation in FUR cause a decrease in antioxidant hydrolysate activity, both in vitro, as well as in healthy Wistar rats. When considering the results of the presented diverse therapeutic potential, further research on CSGH being a potential bioactive peptide source used as a functional food or nutraceutical, but with a different microencapsulation coating, is encouraged.

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In Vitro Evaluation of the Anti-Inflammatory Effect of KMUP-1 and in Vivo Analysis of Its Therapeutic Potential in Osteoarthritis

Biomedicines ◽

10.3390/biomedicines9060615 ◽

2021 ◽

Vol 9 (6) ◽

pp. 615

Author(s):

Shang-En Huang ◽

Erna Sulistyowati ◽

Yu-Ying Chao ◽

Bin-Nan Wu ◽

Zen-Kong Dai ◽

...

Keyword(s):

Articular Cartilage ◽

Inflammatory Responses ◽

Therapeutic Potential ◽

Antioxidant Properties ◽

Serum Levels ◽

Gene Expressions ◽

Tnf Α ◽

Anti Inflammatory

Osteoarthritis is a degenerative arthropathy that is mainly characterized by dysregulation of inflammatory responses. KMUP-1, a derived chemical synthetic of xanthine, has been shown to have anti-inflammatory and antioxidant properties. Here, we aimed to investigate the in vitro anti-inflammatory and in vivo anti-osteoarthritis effects of KMUP-1. Protein and gene expressions of inflammation markers were determined by ELISA, Western blotting and microarray, respectively. RAW264.7 mouse macrophages were cultured and pretreated with KMUP-1 (1, 5, 10 μM). The productions of TNF-α, IL-6, MMP-2 and MMP- 9 were reduced by KMUP-1 pretreatment in LPS-induced inflammation of RAW264.7 cells. The expressions of iNOS, TNF-α, COX-2, MMP-2 and MMP-9 were also inhibited by KMUP-1 pretreatment. The gene expression levels of TNF and COX families were also downregulated. In addition, KMUP-1 suppressed the activations of ERK, JNK and p38 as well as phosphorylation of IκBα/NF-κB signaling pathways. Furthermore, SIRT1 inhibitor attenuated the inhibitory effect of KMUP-1 in LPS-induced NF-κB activation. In vivo study showed that KMUP-1 reduced mechanical hyperalgesia in monoiodoacetic acid (MIA)-induced rats OA. Additionally, KMUP-1 pretreatment reduced the serum levels of TNF-α and IL-6 in MIA-injected rats. Moreover, macroscopic and histological observation showed that KMUP-1 reduced articular cartilage erosion in rats. Our results demonstrated that KMUP-1 inhibited the inflammatory responses and restored SIRT1 in vitro, alleviated joint-related pain and cartilage destruction in vivo. Taken together, KMUP-1 has the potential to improve MIA-induced articular cartilage degradation by inhibiting the levels and expression of inflammatory mediators suggesting that KMUP-1 might be a potential therapeutic agent for OA.

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Dickkopf-1 Inhibition Reactivates Wnt/β-Catenin Signaling in Rhabdomyosarcoma, Induces Myogenic Markers In Vitro and Impairs Tumor Cell Survival In Vivo

International Journal of Molecular Sciences ◽

10.3390/ijms222312921 ◽

2021 ◽

Vol 22 (23) ◽

pp. 12921

Author(s):

Irina Giralt ◽

Gabriel Gallo-Oller ◽

Natalia Navarro ◽

Patricia Zarzosa ◽

Guillem Pons ◽

...

Keyword(s):

Therapeutic Potential ◽

Positive Effects ◽

Novel Therapeutic Strategies ◽

And Function ◽

Myogenic Markers ◽

First Time ◽

Dickkopf 1 ◽

Proliferation And Invasion

The Wnt/β-catenin signaling pathway plays a pivotal role during embryogenesis and its deregulation is a key mechanism in the origin and progression of several tumors. Wnt antagonists have been described as key modulators of Wnt/β-catenin signaling in cancer, with Dickkopf-1 (DKK-1) being the most studied member of the DKK family. Although the therapeutic potential of DKK-1 inhibition has been evaluated in several diseases and malignancies, little is known in pediatric tumors. Only a few works have studied the genetic inhibition and function of DKK-1 in rhabdomyosarcoma. Here, for the first time, we report the analysis of the therapeutic potential of DKK-1 pharmaceutical inhibition in rhabdomyosarcoma, the most common soft tissue sarcoma in children. We performed DKK-1 inhibition via shRNA technology and via the chemical inhibitor WAY-2626211. Its inhibition led to β-catenin activation and the modulation of focal adhesion kinase (FAK), with positive effects on in vitro expression of myogenic markers and a reduction in proliferation and invasion. In addition, WAY-262611 was able to impair survival of tumor cells in vivo. Therefore, DKK-1 could constitute a molecular target, which could lead to novel therapeutic strategies in RMS, especially in those patients with high DKK-1 expression.

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In Vitro and In Vivo Immunomodulator Activities of Allium sativum L.

Evidence-based Complementary and Alternative Medicine ◽

10.1155/2018/4984659 ◽

2018 ◽

Vol 2018 ◽

pp. 1-10 ◽

Cited By ~ 9

Author(s):

Mouna Moutia ◽

Norddine Habti ◽

Abdallah Badou

Keyword(s):

Immune Cells ◽

Allium Sativum ◽

Therapeutic Potential ◽

Inflammatory Diseases ◽

Biological Activities ◽

Antioxidant Properties ◽

Allergic Airway Inflammation ◽

Cytokine Gene Expression

Allium Sativum L. (garlic), which is a species of the onion family, Alliaceae, is one of the most used plants in traditional medicine worldwide. More than 200 chemicals with diverse properties have been found in garlic extracts. Several garlic compounds were suggested to be efficient in improving various pathologies including certain types of cancer. This paper is an overview of data about garlic biological activities in vitro and/or in vivo on immune cells, on the development of certain inflammatory diseases, and on different types of carcinomas and sarcomas. Garlic and its compounds were found to have notable antioxidant properties. Garlic therapeutic potential has also been studied in several inflammatory diseases such as allergic-airway inflammation, inflammatory bowel disease, arthritic rheumatism, and atherosclerosis. Furthermore, garlic was found to be able to maintain the immune system homeostasis and to exhibit beneficial effects on immune cells especially through regulation of proliferation and cytokine gene expression. Finally, we will show how major garlic components such as sulfur compounds and polyphenols might be responsible for the garlic biological activities revealed in different situations. If identified, specific compounds present in garlic could potentially be used in therapy.

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Nanocurcumin-Loaded UCNPs for Cancer Theranostics: Physicochemical Properties, In Vitro Toxicity, and In Vivo Imaging Studies

Nanomaterials ◽

10.3390/nano11092234 ◽

2021 ◽

Vol 11 (9) ◽

pp. 2234

Author(s):

Anbharasi Lakshmanan ◽

Roman A. Akasov ◽

Natalya V. Sholina ◽

Polina A. Demina ◽

Alla N. Generalova ◽

...

Keyword(s):

Near Infrared ◽

Therapeutic Potential ◽

Ex Vivo ◽

Laboratory Animals ◽

In Vitro Toxicity ◽

Upconversion Nanoparticles ◽

Lewis Lung Cancer ◽

Spectral Bands

Formulation of promising anticancer herbal drug curcumin as a nanoscale-sized curcumin (nanocurcumin) improved its delivery to cells and organisms both in vitro and in vivo. We report on coupling nanocurcumin with upconversion nanoparticles (UCNPs) using Poly (lactic-co-glycolic Acid) (PLGA) to endow visualisation in the near-infrared transparency window. Nanocurcumin was prepared by solvent-antisolvent method. NaYF4:Yb,Er (UCNP1) and NaYF4:Yb,Tm (UCNP2) nanoparticles were synthesised by reverse microemulsion method and then functionalized it with PLGA to form UCNP-PLGA nanocarrier followed up by loading with the solvent-antisolvent process synthesized herbal nanocurcumin. The UCNP samples were extensively characterised with XRD, Raman, FTIR, DSC, TGA, UV-VIS-NIR spectrophotometer, Upconversion spectrofluorometer, HRSEM, EDAX and Zeta Potential analyses. UCNP1-PLGA-nanocurcumin exhibited emission at 520, 540, 660 nm and UCNP2-PLGA-nanocurmin showed emission at 480 and 800 nm spectral bands. UCNP-PLGA-nanocurcumin incubated with rat glioblastoma cells demonstrated moderate cytotoxicity, 60–80% cell viability at 0.12–0.02 mg/mL marginally suitable for therapeutic applications. The cytotoxicity of UCNPs evaluated in tumour spheroids models confirmed UCNP-PLGA-nanocurcumin therapeutic potential. As-synthesised curcumin-loaded nanocomplexes were administered in tumour-bearing laboratory animals (Lewis lung cancer model) and showed adequate contrast to enable in vivo and ex vivo study of UCNP-PLGA-nanocurcumin bio distribution in organs, with dominant distribution in the liver and lungs. Our studies demonstrate promise of nanocurcumin-loaded upconversion nanoparticles for theranostics applications.

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Designing of Chitosan Derivatives Nanoparticles with Antiangiogenic Effect for Cancer Therapy

Nanomaterials ◽

10.3390/nano10040698 ◽

2020 ◽

Vol 10 (4) ◽

pp. 698

Author(s):

Oana-Maria Dragostin ◽

Rodica Tatia ◽

Sangram Keshari Samal ◽

Anca Oancea ◽

Alexandra Simona Zamfir ◽

...

Keyword(s):

Cancer Therapy ◽

Tumor Cells ◽

Therapeutic Potential ◽

Antioxidant Properties ◽

Chorioallantoic Membrane ◽

Cancer Therapies ◽

Antiangiogenic Effect ◽

Chitosan Derivatives

Angiogenesis is a physiological process involving the growth of new blood vessels, which provides oxygen and required nutrients for the development of various pathological conditions. In a tumor microenvironment, this process upregulates the growth and proliferation of tumor cells, thus any stage of angiogenesis can be a potential target for cancer therapies. In the present study, chitosan and his derivatives have been used to design novel polymer-based nanoparticles. The therapeutic potential of these newly designed nanoparticles has been evaluated. The antioxidant and MTT assays were performed to know the antioxidant properties and their biocompatibility. The in vivo antiangiogenic properties of the nanoparticles were evaluated by using a chick Chorioallantoic Membrane (CAM) model. The obtained results demonstrate that chitosan derivatives-based nanostructures strongly enhance the therapeutic effect compared to chitosan alone, which also correlates with antitumor activity, demonstrated by the in vitro MTT assay on human epithelial cervical Hep-2 tumor cells. This study opens up new direction for the use of the chitosan derivatives-based nanoparticles for designing of antiangiogenic nanostructured materials, for future cancer therapy.

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Evaluating Antiplasmodial and Antimalarial Activities of Soybean (Glycine max) Seed Extracts on P. falciparum Parasite Cultures and P. berghei-Infected Mice

Journal of Pathogens ◽

10.1155/2020/7605730 ◽

2020 ◽

Vol 2020 ◽

pp. 1-8

Author(s):

Kevin Nyandwaro ◽

Job Oyweri ◽

Francis Kimani ◽

Amos Mbugua

Keyword(s):

Therapeutic Potential ◽

Antimalarial Activity ◽

Antioxidant Properties ◽

Antiplasmodial Activity ◽

Methanol Extracts ◽

Lead Compounds ◽

High Parasite ◽

Seed Extracts

Background. Plasmodium parasite resistance to artemisinin-based combination therapies (ACTs) calls for development of new, affordable, safe, and effective antimalarial drugs. Studies conducted previously on soybean extracts have established that they possess antimicrobial, anti-inflammatory, anticancerous, and antioxidant properties. The activity of such extracts on Plasmodium parasites has not been potentially exploited. Objectives. The aim of this study was to determine the antiplasmodial activity of soybean extracts using Plasmodium falciparum cultures, followed by an in vivo evaluation of safety and antimalarial activity of the extracts in Plasmodium berghei ANKA strain-infected mice. Method. Aqueous, methanol, and peptide extracts of soybean seeds were prepared. An in vitro evaluation of the extracts for antiplasmodial activity was carried out using two P. falciparum strains: D6, a chloroquine-sensitive Sierra Leone 1 strain and W2, a chloroquine-resistant Indochina 1 strain. Following the in vitro assessment, two active extracts (peptide and methanol) were selected for in vivo assay with mice infected with P. berghei ANKA strain. The two extracts were tested for their therapeutic potential (curative test). The peptide extract was further assessed to determine whether it could prevent the establishment of a P. berghei infection (prophylactic test). For the curative tests, methanol and peptide extracts were separately administered orally to three groups of five P. berghei-infected Swiss albino mice for four days, at three dosage levels: 800, 400, and 200 mg/kg/day. In the prophylactic test, the similar dosage regimen was applied at baseline to 3 groups of uninfected mice using the peptide extract which was administered orally for 4 days. Results. Peptide and methanol extracts showed good activity with IC50 of 19.97 ± 2.57 μg/ml and 10.14 ± 9.04 μg/ml, respectively, against the D6 strain. The IC50 values for the peptide and methanol extracts were 28.61 ± 1.32 μg/ml and 14.87 ± 3.43 μg/ml, respectively, against the W2 strain. Methanol and peptide extracts exhibited high parasite-suppressive (therapeutic) activity of 72.9% and 71.9%, respectively, using the 800 mg/kg dose. In the prophylactic test, the peptide extract exhibited suppressive activity of 64.7% upon use of 800 mg/kg. Notably, there was a significant decrease (P<0.001) in suppression with lower doses. Conclusion. The results show the presence of antimalarial properties in soybean extracts with higher curative activity when compared to the prophylactic activity. However, more research needs to be conducted on this plant to possibly establish lead compounds.

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Antioxidant Effect of Flavonoids Present in Euterpe oleracea Martius and Neurodegenerative Diseases: A Literature Review

Central Nervous System Agents in Medicinal Chemistry ◽

10.2174/1871524919666190502105855 ◽

2019 ◽

Vol 19 (2) ◽

pp. 75-99 ◽

Cited By ~ 4

Author(s):

Nayana Keyla Seabra de Oliveira ◽

Marcos Rafael Silva Almeida ◽

Franco Márcio Maciel Pontes ◽

Mariana Pegrucci Barcelos ◽

Carlos Henrique Tomich de Paula da Silva ◽

...

Keyword(s):

Oxidative Stress ◽

Neurodegenerative Diseases ◽

Therapeutic Potential ◽

Antioxidant Properties ◽

In Vivo Studies ◽

Euterpe Oleracea ◽

Case Review ◽

The Central Nervous System

Introduction:Neurodegenerative diseases (NDDs) are progressive, directly affecting the central nervous system (CNS), the most common and recurrent are Alzheimer's disease (AD) and Parkinson's disease (PD). One factor frequently mentioned in the etiology of NDDs is the generation of free radicals and oxidative stress, producing cellular damages. Studies have shown that the consumption of foods rich in polyphenols, especially those of the flavonoid class, has been related to the low risk in the development of several diseases. Due to the antioxidant properties present in the food, a fruit that has been gaining prominence among these foods is the Euterpe oleracea Mart. (açaí), because it presents in its composition significant amounts of a subclass of the flavonoids, the anthocyanins.Methods:In the case review, the authors receive a basic background on the most common NDDs, oxidative stress and antioxidants. In addition, revisiting the various studies related to NDDs, including flavonoids and consumption of açaí.Results:Detailed analysis of the recently reported case studies reveal that dietary consumption of flavonoid-rich foods, such as açaí fruits, suggests the efficacy to attenuate neurodegeneration and prevent or reverse the age-dependent deterioration of cognitive function.Conclusion:This systematic review points out that flavonoids presenting in açaí have the potential for the treatment of diseases such as PD and AD and are candidates for drugs in future clinical research. However, there is a need for in vitro and in vivo studies with polyphenol that prove and ratify the therapeutic potential of this fruit for several NDDs.

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Antioxidant Properties of Amazonian Fruits: A Mini Review of In Vivo and In Vitro Studies

Oxidative Medicine and Cellular Longevity ◽

10.1155/2019/8204129 ◽

2019 ◽

Vol 2019 ◽

pp. 1-11 ◽

Cited By ~ 8

Author(s):

Raúl Avila-Sosa ◽

Andrés Felipe Montero-Rodríguez ◽

Patricia Aguilar-Alonso ◽

Obdulia Vera-López ◽

Martin Lazcano-Hernández ◽

...

Keyword(s):

Functional Properties ◽

Unsaturated Fatty Acids ◽

Therapeutic Potential ◽

Protective Action ◽

Antioxidant Properties ◽

Fruit Trees ◽

Antidepressant Effects ◽

Living Species

Brazil, Colombia, Ecuador, Peru, Bolivia, Venezuela, Suriname, Guyana, and French Guiana share an area of 7,295,710 km2 of the Amazon region. It is estimated that the Amazonian forest offers the greatest flora and fauna biodiversity on the planet and on its surface could cohabit 50% of the total existing living species; according to some botanists, it would contain about 16-20% of the species that exist today. This region has native fruit trees in which functional properties are reported as antioxidant and antiproliferative characteristics. Amazon plants offer a great therapeutic potential attributed to the content of bioactive phytochemicals. The aim of this mini review is to examine the state of the art of the main bioactive components of the most studied Amazonian plants. Among the main functional compounds reported were phenolic compounds, unsaturated fatty acids, carotenoids, phytosterols, and tocopherols, with flavonoids and carotenoids being the groups of greatest interest. The main beneficial effect reported has been the antioxidant effect, evaluated in most of the fruits investigated; other reported functional properties were antimicrobial, antimutagenic, antigenotoxic, analgesic, immunomodulatory, anticancer, bronchodilator, antiproliferative, and anti-inflammatory, including hypercholesterolemic effects, leishmanicidal activity, induction of apoptosis, protective action against diabetes, gastroprotective activity, and antidepressant effects.

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Protective Effects of the Flavonoid Chrysin against Methylmercury-Induced Genotoxicity and Alterations of Antioxidant Status,In Vivo

Oxidative Medicine and Cellular Longevity ◽

10.1155/2015/602360 ◽

2015 ◽

Vol 2015 ◽

pp. 1-7 ◽

Cited By ~ 15

Author(s):

Eduardo Scandinari Manzolli ◽

Juliana Mara Serpeloni ◽

Denise Grotto ◽

Jairo Kennup Bastos ◽

Lusânia Maria Greggi Antunes ◽

...

Keyword(s):

Oxidative Damage ◽

Antioxidant Status ◽

Wistar Rats ◽

Antioxidant Properties ◽

Toxic Metal ◽

Protective Effects ◽

Adverse Health Effects ◽

Dietary Flavonoids ◽

Antioxidant Effects

The use of phytochemicals has been widely used as inexpensive approach for prevention of diseases related to oxidative damage due to its antioxidant properties. One of dietary flavonoids is chrysin (CR), found mainly in passion fruit, honey, and propolis. Methylmercury (MeHg) is a toxic metal whose main toxic mechanism is oxidative damage. Thus, the study aimed to evaluate the antioxidant effects of CR against oxidative damage induced by MeHg in Wistar rats. Animals were treated with MeHg (30 µg/kg/bw) in presence and absence of CR (0.10, 1.0, and 10 mg/kg/bw) by gavage for 45 days. Glutathione (GSH) in blood was quantified spectrophotometrically and for monitoring of DNA damage, comet assay was used in leukocytes and hepatocytes. MeHg led to a significant increase in the formation of comets; when the animals were exposed to the metal in the presence of CR, higher concentrations of CR showed protective effects. Moreover, exposure to MeHg decreased the levels of GSH and GSH levels were restored in the animals that received CR plus MeHg. Taken together the findings of the present work indicate that consumption of flavonoids such as CR may protect humans against the adverse health effects caused by MeHg.

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The Anti-cancer Effect of Olea europaea L. Products: a Review

Current Nutrition Reports ◽

10.1007/s13668-021-00350-8 ◽

2021 ◽

Author(s):

Chrystalla Antoniou ◽

Jonathon Hull

Keyword(s):

Animal Models ◽

Olea Europaea ◽

Therapeutic Potential ◽

Folk Medicine ◽

Olive Tree ◽

Future Research ◽

Positive Effects ◽

Olea Europaéa

Abstract Purpose of Review The olive tree (Olea europaea L.) has featured as a significant part of medicinal history, used to treat a variety of ailments within folk medicine. The Mediterranean diet, which is rich in olive products, is testament to Olea europaeas positive effects on health, associated with reduced incidences of cancer and cardiovascular disease. This review aims to summarise the current literature regarding the therapeutic potential of Olea europaea products in cancer, detailing the possible compounds responsible for its chemotherapeutic effects. Recent Findings Much of the existing research has focused on the use of cell culture models of disease, demonstrating Olea europaea extracts, and specific compounds within these extracts, have efficacy in a range of in vitro and in vivo cancer models. The source of Olea europaeas cytotoxicity is yet to be fully defined; however, compounds such as oleuropein and verbascoside have independent cytotoxic effects on animal models of cancer. Summary Initial results from animal models are promising but need to be translated to a clinical setting. Treatments utilising these compounds are likely to be well tolerated and represent a promising direction for future research.

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