Pharmacological Characterization of Natural Antioxidants

A special issue of Antioxidants (ISSN 2076-3921). This special issue belongs to the section "Natural and Synthetic Antioxidants".

Deadline for manuscript submissions: closed (15 October 2022) | Viewed by 16109

Special Issue Editor

College of Pharmacy, Federal University of Bahia, Rua Barão de Jeremoabo 147, Salvador 40170-115, Bahia, Brazil
Interests: pain; analgesic; anti-inflammatory; pharmacology; mechanisms of chronic pain
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Special Issue Information

Dear Colleagues,

Natural antioxidants—phenolic compounds, carotenoids and vitamins—are mainly derived from food and medicinal plants. These natural compounds exhibit a wide range of biological activities, which may support their therapeutic potential in diseases such as diabetes, cancer, brain stroke, neurodegenerative disorders, and cardiovascular diseases.  In addition, natural antioxidants exhibit beneficial effect on human health by protection against free radicals, a property that has increased the consumption of these compounds in nutraceuticals and food supplements. In fact, the rise in prevalence of lifestyle diseases, such as obesity and diabetes, has shifted the consumption pattern towards the adoption of healthy habits, expanding the world market for natural antioxidants. The potential benefits for human health motivate a constant search for natural substances that are able to treat or prevent many diseases in which oxidative stress is a key pathophysiological event.

It has recently been proposed that the pharmacological mechanisms of natural antioxidants are more complex than their classical hydrogen-donating antioxidant activity, and likely include the modulation of intracellular signaling cascades as well as the modulation of gene expression and epigenetic mechanisms. On the other hand, although the understanding of the effects and mechanisms of natural antioxidants has advanced in recent years, the characterization of the pharmacological properties and mechanisms of action of these compounds is still a topic under investigation.

The Special Issue " Pharmacological Characterization of Natural Antioxidants" invites researchers to contribute to original research articles and review articles related to the pharmacology of natural antioxidants, including clinical and preclinical studies of pharmacodynamics and pharmacokinetics, with in silico, in vitro and in vivo approaches.

Prof. Dr. Cristiane Flora Villarreal
Guest Editor

Manuscript Submission Information

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Keywords

  • antioxidant
  • pharmacology
  • natural products
  • nutraceuticals

Published Papers (4 papers)

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Research

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13 pages, 1837 KiB  
Article
Aniba canelilla (Kunth) Mez (Lauraceae) Essential Oil: Effects on Oxidative Stress and Vascular Permeability
Antioxidants 2022, 11(10), 1903; https://doi.org/10.3390/antiox11101903 - 26 Sep 2022
Cited by 1 | Viewed by 1704
Abstract
The present study aimed to investigate the antioxidant activity of Aniba canelilla (kunth) Mez (Lauraceae) essential oil (AcEO), exploring its potential for prevention and/or treatment of oxidative stress and associated inflammatory process. With this aim, Wistar rats (n = 6/group) were pre-treated [...] Read more.
The present study aimed to investigate the antioxidant activity of Aniba canelilla (kunth) Mez (Lauraceae) essential oil (AcEO), exploring its potential for prevention and/or treatment of oxidative stress and associated inflammatory process. With this aim, Wistar rats (n = 6/group) were pre-treated intraperitoneally with saline (0.9%) or AcEO (2 or 5 mg/kg) for 5 days. One hour after the last dose, inflammation and oxidative stress were induced by carrageenan (0.3 mg/kg; ip.) administration. Total antioxidant capacity, reduced glutathione (GSH) and lipid peroxidation levels, protein concentration, and leukocyte migration were evaluated in peritoneal fluid. Lipid peroxidation was also evaluated in plasma. Carrageenan strongly reduced the peritoneal antioxidant capacity and GSH concentration, increasing peritoneal and plasma lipid peroxidation. It also promoted increased plasma leakage and leukocyte migration. Treatment with AcEO (2 and 5 mg/kg), whose major constituent was 1-nitro-2-phenylethane (77.5%), increased the peritoneal antioxidant capacity and GSH concentrations, and reduced lipid peroxidation, both peritoneal and plasma, thus inhibiting the carrageenan-induced oxidative imbalance. AcEO also reduced the carrageenan-induced plasma leakage and leukocyte migration. These data demonstrate the AcEO antioxidant activity and its ability to modulate plasma leakage and leukocyte migration, confirming its potential for treating diseases associated with inflammation and oxidative stress. Full article
(This article belongs to the Special Issue Pharmacological Characterization of Natural Antioxidants)
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17 pages, 3837 KiB  
Article
Chelerythrine-Induced Apoptotic Cell Death in HepG2 Cells Involves the Inhibition of Akt Pathway and the Activation of Oxidative Stress and Mitochondrial Apoptotic Pathway
Antioxidants 2022, 11(9), 1837; https://doi.org/10.3390/antiox11091837 - 18 Sep 2022
Cited by 1 | Viewed by 1880
Abstract
Chelerythrine (CHE) is a majorly harmful isoquinoline alkaloid ingredient in Chelidonium majus that could trigger potential hepatotoxicity, but the pivotal molecular mechanisms remain largely unknown. In the present study, CHE-induced cytotoxicity and the underlying toxic mechanisms were investigated using human HepG2 cells in [...] Read more.
Chelerythrine (CHE) is a majorly harmful isoquinoline alkaloid ingredient in Chelidonium majus that could trigger potential hepatotoxicity, but the pivotal molecular mechanisms remain largely unknown. In the present study, CHE-induced cytotoxicity and the underlying toxic mechanisms were investigated using human HepG2 cells in vitro. Data showed that CHE treatment (at 1.25–10 μM)-induced cytotoxicity in HepG2 cells is dose-dependent. CHE treatment increased the production of ROS and induced oxidative stress in HepG2 cells. Additionally, CHE treatment triggered the loss of mitochondrial membrane potential, decreased the expression of mitochondrial complexes, upregulated the expression of Bax, CytC, and cleaved-PARP1 proteins and the activities of caspase-9 and caspase-3, and downregulated the expression of Bcl-XL, and HO-1 proteins, finally resulting in cell apoptosis. N-acetylcysteine supplementation significantly inhibited CHE-induced ROS production and apoptosis. Furthermore, CHE treatment significantly downregulated the expression of phosphorylation (p)-Akt (Ser473), p-mTOR (Ser2448), and p-AMPK (Thr172) proteins in HepG2 cells. Pharmacology inhibition of Akt promoted CHE-induced the downregulation of HO-1 protein, caspase activation, and apoptosis. In conclusion, CHE-induced cytotoxicity may involve the inhibition of Akt pathway and the activation of oxidative stress-mediated mitochondrial apoptotic pathway in HepG2 cells. This study sheds new insights into understanding the toxic mechanisms and health risks of CHE. Full article
(This article belongs to the Special Issue Pharmacological Characterization of Natural Antioxidants)
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Review

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19 pages, 2078 KiB  
Review
Alpha-Lipoic Acid as an Antioxidant Strategy for Managing Neuropathic Pain
Antioxidants 2022, 11(12), 2420; https://doi.org/10.3390/antiox11122420 - 08 Dec 2022
Cited by 6 | Viewed by 5109
Abstract
Neuropathic pain (NP) is the most prevalent and debilitating form of chronic pain, caused by injuries or diseases of the somatosensory system. Since current first-line treatments only provide poor symptomatic relief, the search for new therapeutic strategies for managing NP is an active [...] Read more.
Neuropathic pain (NP) is the most prevalent and debilitating form of chronic pain, caused by injuries or diseases of the somatosensory system. Since current first-line treatments only provide poor symptomatic relief, the search for new therapeutic strategies for managing NP is an active field of investigation. Multiple mechanisms contribute to the genesis and maintenance of NP, including damage caused by oxidative stress. The naturally occurring antioxidant alpha-lipoic acid (ALA) is a promising therapeutic agent for the management of NP. Several pre-clinical in vitro and in vivo studies as well as clinical trials demonstrate the analgesic potential of ALA in the management of NP. The beneficial biological activities of ALA are reflected in the various patents for the development of ALA-based innovative products. This review demonstrates the therapeutic potential of ALA in the management of NP by discussing its analgesic effects by multiple antioxidant mechanisms as well as the use of patented ALA-based products and how technological approaches have been applied to enhance ALA’s pharmacological properties. Full article
(This article belongs to the Special Issue Pharmacological Characterization of Natural Antioxidants)
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32 pages, 917 KiB  
Review
Health Benefits and Pharmacological Properties of Stigmasterol
Antioxidants 2022, 11(10), 1912; https://doi.org/10.3390/antiox11101912 - 27 Sep 2022
Cited by 54 | Viewed by 6633
Abstract
Stigmasterol is an unsaturated phytosterol belonging to the class of tetracyclic triterpenes. It is one of the most common plant sterols, found in a variety of natural sources, including vegetable fats or oils from many plants. Currently, stigmasterol has been examined via in [...] Read more.
Stigmasterol is an unsaturated phytosterol belonging to the class of tetracyclic triterpenes. It is one of the most common plant sterols, found in a variety of natural sources, including vegetable fats or oils from many plants. Currently, stigmasterol has been examined via in vitro and in vivo assays and molecular docking for its various biological activities on different metabolic disorders. The findings indicate potent pharmacological effects such as anticancer, anti-osteoarthritis, anti-inflammatory, anti-diabetic, immunomodulatory, antiparasitic, antifungal, antibacterial, antioxidant, and neuroprotective properties. Indeed, stigmasterol from plants and algae is a promising molecule in the development of drugs for cancer therapy by triggering intracellular signaling pathways in numerous cancers. It acts on the Akt/mTOR and JAK/STAT pathways in ovarian and gastric cancers. In addition, stigmasterol markedly disrupted angiogenesis in human cholangiocarcinoma by tumor necrosis factor-α (TNF-α) and vascular endothelial growth factor receptor-2 (VEGFR-2) signaling down-regulation. The association of stigmasterol and sorafenib promoted caspase-3 activity and down-regulated levels of the anti-apoptotic protein Bcl-2 in breast cancer. Antioxidant activities ensuring lipid peroxidation and DNA damage lowering conferred to stigmasterol chemoprotective activities in skin cancer. Reactive oxygen species (ROS) regulation also contributes to the neuroprotective effects of stigmasterol, as well as dopamine depletion and acetylcholinesterase inhibition. The anti-inflammatory properties of phytosterols involve the production of anti-inflammatory cytokines, the decrease in inflammatory mediator release, and the inhibition of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2). Stigmasterol exerts anti-diabetic effects by reducing fasting glucose, serum insulin levels, and oral glucose tolerance. Other findings showed the antiparasitic activities of this molecule against certain strains of parasites such as Trypanosoma congolense (in vivo) and on promastigotes and amastigotes of the Leishmania major (in vitro). Some stigmasterol-rich plants were able to inhibit Candida albicans, virusei, and tropicalis at low doses. Accordingly, this review outlines key insights into the pharmacological abilities of stigmasterol and the specific mechanisms of action underlying some of these effects. Additionally, further investigation regarding pharmacodynamics, pharmacokinetics, and toxicology is recommended. Full article
(This article belongs to the Special Issue Pharmacological Characterization of Natural Antioxidants)
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