Disclosing the potential of eleganolone for Parkinson’s disease therapeutics: Neuroprotective and anti-inflammatory activities

Silva, Joana; Alves, Celso; Pintéus, Susete; Susano, Patrícia; Simões, Marco; Guedes, Miguel; Martins, Alice; Rehfeldt, Stephanie Cristine Hepp; Gaspar, Héléna; Goettert, Márcia Inês; Alfonso, Amparo; Pedrosa, Rui

doi:10.1016/j.phrs.2021.105589

Cited by 16 publications

(10 citation statements)

References 51 publications

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“…In addition, these cytokines can stimulate p-38α MAPK, which participates in the regulation of inflammatory responses [ 49 ]. On the other hand, IL-10 plays an important role in the immune system, by acting as an anti-inflammatory mediator in the subsequent level of the inflammatory cascade [ 17 ].…”

Section: Discussionmentioning

confidence: 99%

“…Thus, the search for new skincare products is crucial and it is important to find alternatives of natural origin. In this sense, seaweeds can be the key for the development of new natural skincare formulations as they have revealed antioxidant, anti-aging, photoprotective, antimicrobial and anti-inflammatory properties [ 15 , 16 , 17 , 18 , 19 ].…”

Section: Introductionmentioning

confidence: 99%

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Saccorhiza polyschides—A Source of Natural Active Ingredients for Greener Skincare Formulations

et al. 2022

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The growing knowledge about the harmful effects caused by some synthetic ingredients present in skincare products has led to an extensive search for natural bioactives. Thus, this study aimed to investigate the dermatological potential of five fractions (F1–F5), obtained by a sequential extraction procedure, from the brown seaweed Saccorhiza polyschides. The antioxidant (DPPH, FRAP, ORAC and TPC), anti-enzymatic (collagenase, elastase, hyaluronidase and tyrosinase), antimicrobial (Staphylococcus epidermidis, Cutibacterium acnes and Malassezia furfur), anti-inflammatory (nitric oxide, tumor necrosis factor-α, interleukin-6 and interleukin-10) and photoprotective (reactive oxygen species) properties of all fractions were evaluated. The ethyl acetate fraction (F3) displayed the highest antioxidant and photoprotective capacity, reducing ROS levels in UVA/B-exposed 3T3 fibroblasts, and the highest anti-enzymatic capacity against tyrosinase (IC50 value: 89.1 µg/mL). The solid water-insoluble fraction (F5) revealed the greatest antimicrobial activity against C. acnes growth (IC50 value: 12.4 µg/mL). Furthermore, all fractions demonstrated anti-inflammatory potential, reducing TNF-α and IL-6 levels in RAW 264.7 macrophages induced with lipopolysaccharides. Chemical analysis of the S. polyschides fractions by NMR revealed the presence of different classes of compounds, including lipids, polyphenols and sugars. The results highlight the potential of S. polyschides to be incorporated into new nature-based skincare products.

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Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Saccorhiza polyschides—A Source of Natural Active Ingredients for Greener Skincare Formulations

et al. 2022

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“…Silva et al [383] isolated eleganolone, eleganonal, and fucosterol from Bifurcaria bifurcata R.Ross. The in vitro neuroprotective effects were evaluated on 6-OHDA-treated SH-SY5Y cells (PD model), and the anti-inflammatory potential was studied using LPS-stimulated RAW 264.7 macrophages.…”

Section: Other Compoundsmentioning

confidence: 99%

Biological Potential, Gastrointestinal Digestion, Absorption, and Bioavailability of Algae-Derived Compounds with Neuroprotective Activity: A Comprehensive Review

et al. 2022

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Currently, there is no known cure for neurodegenerative disease. However, the available therapies aim to manage some of the symptoms of the disease. Human neurodegenerative diseases are a heterogeneous group of illnesses characterized by progressive loss of neuronal cells and nervous system dysfunction related to several mechanisms such as protein aggregation, neuroinflammation, oxidative stress, and neurotransmission dysfunction. Neuroprotective compounds are essential in the prevention and management of neurodegenerative diseases. This review will focus on the neurodegeneration mechanisms and the compounds (proteins, polyunsaturated fatty acids (PUFAs), polysaccharides, carotenoids, phycobiliproteins, phenolic compounds, among others) present in seaweeds that have shown in vivo and in vitro neuroprotective activity. Additionally, it will cover the recent findings on the neuroprotective effects of bioactive compounds from macroalgae, with a focus on their biological potential and possible mechanism of action, including microbiota modulation. Furthermore, gastrointestinal digestion, absorption, and bioavailability will be discussed. Moreover, the clinical trials using seaweed-based drugs or extracts to treat neurodegenerative disorders will be presented, showing the real potential and limitations that a specific metabolite or extract may have as a new therapeutic agent considering the recent approval of a seaweed-based drug to treat Alzheimer’s disease.

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“…Its potential benefits to the CNS include the decrease of microglia activation and neuronal protection [ 3 , 4 , 5 ]. However, the glycosylated form of luteolin, known as cyranoside or luteolin-7-O-glucoside (Lut7) (PubChem ID 5280637), was reported as a selective JNK3 inhibitor, five times more selective than luteolin [ 6 ], which plays a key role in neurodegenerative diseases [ 7 , 8 , 9 , 10 , 11 ], suggesting that patients with neurodegenerative diseases might benefit from a natural or bio-inspired product-based therapy [ 12 , 13 , 14 , 15 , 16 ].…”

Section: Introductionmentioning

confidence: 99%

Neuroprotective Effect of Luteolin-7-O-Glucoside against 6-OHDA-Induced Damage in Undifferentiated and RA-Differentiated SH-SY5Y Cells

Rehfeldt

Silva

Alves

et al. 2022

IJMS

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Luteolin is one of the most common flavonoids present in edible plants and its potential benefits to the central nervous system include decrease of microglia activation, neuronal damage and high antioxidant properties. The aim of this research was to evaluate the neuroprotective, antioxidant and anti-inflammatory activities of luteolin-7-O-glucoside (Lut7). Undifferentiated and retinoic acid (RA)-differentiated SH-SY5Y cells were pretreated with Lut7 and incubated with 6-hydroxydopamine (6-OHDA). Cytotoxic and neuroprotective effects were determined by MTT assay. Antioxidant capacity was determined by DPPH, FRAP, and ORAC assays. ROS production, mitochondrial membrane potential (ΔΨm), Caspase–3 activity, acetylcholinesterase inhibition (AChEI) and nuclear damage were also determined in SH-SY5Y cells. TNF-α, IL-6 and IL-10 release were evaluated in LPS-induced RAW264.7 cells by ELISA. In undifferentiated SH-SY5Y cells, Lut7 increased cell viability after 24 h, while in RA-differentiated SH-SY5Y cells, Lut7 increased cell viability after 24 and 48 h. Lut7 showed a high antioxidant activity when compared with synthetic antioxidants. In undifferentiated cells, Lut7 prevented mitochondrial membrane depolarization induced by 6-OHDA treatment, decreased Caspase-3 and AChE activity, and inhibited nuclear condensation and fragmentation. In LPS-stimulated RAW264.7 cells, Lut7 treatment reduced TNF-α levels and increased IL-10 levels after 3 and 24 h, respectively. In summary, the results suggest that Lut7 has neuroprotective effects, thus, further studies should be considered to validate its pharmacological potential in more complex models, aiming the treatment of neurodegenerative diseases.

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Disclosing the potential of eleganolone for Parkinson’s disease therapeutics: Neuroprotective and anti-inflammatory activities

Cited by 16 publications

References 51 publications

Saccorhiza polyschides—A Source of Natural Active Ingredients for Greener Skincare Formulations

Saccorhiza polyschides—A Source of Natural Active Ingredients for Greener Skincare Formulations

Biological Potential, Gastrointestinal Digestion, Absorption, and Bioavailability of Algae-Derived Compounds with Neuroprotective Activity: A Comprehensive Review

Neuroprotective Effect of Luteolin-7-O-Glucoside against 6-OHDA-Induced Damage in Undifferentiated and RA-Differentiated SH-SY5Y Cells

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