Oxidative stress is viewed as an imbalance between the production of reactive oxygen species (ROS) and their elimination by protective mechanisms, which can lead to chronic inflammation. Oxidative stress can activate a variety of transcription factors, which lead to the differential expression of some genes involved in inflammatory pathways. The inflammation triggered by oxidative stress is the cause of many chronic diseases. Polyphenols have been proposed to be useful as adjuvant therapy for their potential anti-inflammatory effect, associated with antioxidant activity, and inhibition of enzymes involved in the production of eicosanoids. This review aims at exploring the properties of polyphenols in anti-inflammation and oxidation and the mechanisms of polyphenols inhibiting molecular signaling pathways which are activated by oxidative stress, as well as the possible roles of polyphenols in inflammation-mediated chronic disorders. Such data can be helpful for the development of future antioxidant therapeutics and new anti-inflammatory drugs.

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Oxidative Stress and Inflammation: What Polyphenols Can Do for Us?

Chronic inflammation is being shown to be increasingly involved in the onset and development of several pathological disturbances such as arteriosclerosis, obesity, diabetes, neurodegenerative diseases and even cancer. Treatment for chronic inflammatory disorders has not been solved, and there is an urgent need to find new and safe anti-inflammatory compounds. Flavonoids belong to a group of natural substances occurring normally in the diet that exhibit a variety of beneficial effects on health. The anti-inflammatory properties of flavonoids have been studied recently, in order to establish and characterize their potential utility as therapeutic agents in the treatment of inflammatory diseases. Several mechanisms of action have been proposed to explain in vivo flavonoid anti-inflammatory actions, such as antioxidant activity, inhibition of eicosanoid generating enzymes or the modulation of the production of proinflammatory molecules. Recent studies have also shown that some flavonoids are modulators of proinflammatory gene expression, thus leading to the attenuation of the inflammatory response. However, much work remains to be done in order to achieve definitive conclusions about their potential usefulness. This review summarizes the known mechanisms involved in the anti-inflammatory activity of flavonoids and the implications of these effects on the protection against cancer and cardiovascular disease.

Flavonoids as anti-inflammatory agents: implications in cancer and cardiovascular disease.

https://www.jstage.jst.go.jp/article/jphs/advpub/0/advpub_0_0411110005/_pdf

Anti-inflammatory plant flavonoids and cellular action mechanisms.

Antioxidants are substances that may protect cells from the damage caused by unstable molecules such as free radicals. Flavonoids are phenolic substances widely found in fruits and vegetables. The previous studies showed that the ingestion of flavonoids reduces the risk of cardiovascular diseases, metabolic disorders, and certain types of cancer. These effects are due to the physiological activity of flavonoids in the reduction of oxidative stress, inhibiting low-density lipoproteins oxidation and platelet aggregation, and acting as vasodilators in blood vessels. Free radicals are constantly generated resulting in extensive damage to tissues leading to various disease conditions such as cancer, Alzheimer's, renal diseases, cardiac abnormalities, etc., Medicinal plants with antioxidant properties play a vital functions in exhibiting beneficial effects and employed as an alternative source of medicine to mitigate the disease associated with oxidative stress. Flavonoids have existed over one billion years and possess wide spectrum of biological activities that might be able to influence processes which are dysregulated in a disease. Quercetin, a plant pigment is a potent antioxidant flavonoid and more specifically a flavonol, found mostly in onions, grapes, berries, cherries, broccoli, and citrus fruits. It is a versatile antioxidant known to possess protective abilities against tissue injury induced by various drug toxicities.

Overviews of Biological Importance of Quercetin: A Bioactive Flavonoid.

The contemporary scientific community has presently recognized flavonoids to be a unique class of therapeutic molecules due to their diverse therapeutic properties. Of these, rutin, also known as vitamin P or rutoside, has been explored for a number of pharmacological effects. Tea leaves, apples, and many more possess rutin as one of the active constituents. Today, rutin has been observed for its nutraceutical effect. The present review highlights current information and health-promoting effects of rutin. Along with this, safety pharmacology issues and SAR of the same have also been discussed.

The Pharmacological Potential of Rutin.

The anti-inflammatory activities of three flavonoids were investigated in rats using the Mizushima et al. model of acute and chronic inflammation. Intraperitoneal administration of rutin, quercetin (flavonols) and hesperidin (flavanone), given at daily doses equivalent to 80 mg/kg, inhibited both acute and chronic phases of this experimental model of inflammation. Rutin was the most active in the chronic phase.

Anti-inflammatory properties of plant flavonoids. Effects of rutin, quercetin and hesperidin on adjuvant arthritis in rat.

Comparative study of flavonoids in experimental models of inflammation.

The antiinflammatory activities of 30 flavonoids isolated from several plants of the Compositae family were investigated using carrageenan-induced mouse paw edema and cotton pellet-induced rat granuloma. Compounds were administered with a unique dose of 75 mg/kg i.p. in the acute test with carrageenan and 25 mg/kg/day in the chronic granuloma test. Flavonoids inhibit the development of the induced granuloma, mostly when a catechol or guaiacol-like B ring is contained in the compound structure, jaceosidin being the most active flavonoid screened. Flavonoids significantly inhibited the maximum edema response in the acute test. We conclude that several of the isolated flavonoids tested here showed antiinflammatory effects, depending on the experimental model used.

Acute and chronic antiinflammatory effects of plant flavonoids.

Anti-inflammatory activity and effect on gastric acid secretion of dehydroleucodine isolated from Artemisia douglasiana.

As part of our project devoted to the search of new antifungal agents, we report here the in vitro–in vivo antifungal evaluations and a structure–activity relationship (SAR) study of 17 thione derivatives.Some compounds of this series exhibited remarkable antifungal activity against a broad spectrum of pathogenic opportunistic fungi. SAR studies provide a useful information for the determination of the minimum structural requirements for producing the biological response.

Américo Juárez

Papers

Anti-inflammatory properties of plant flavonoids. Effects of rutin, quercetin and hesperidin on adjuvant arthritis in rat.

Comparative study of flavonoids in experimental models of inflammation.

Acute and chronic antiinflammatory effects of plant flavonoids.

Anti-inflammatory activity and effect on gastric acid secretion of dehydroleucodine isolated from Artemisia douglasiana.

In vitro-in vivo antifungal evaluation and structure-activity relationships of 3H-1,2-dithiole-3-thione derivatives.