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Astaxanthin as a Peroxisome Proliferator-Activated Receptor (PPAR) Modulator: Its Therapeutic Implications

College of Pharmacy, Dongguk University-Seoul, Goyang 10326, Korea
Mar. Drugs 2019, 17(4), 242; https://doi.org/10.3390/md17040242
Received: 4 April 2019 / Revised: 19 April 2019 / Accepted: 19 April 2019 / Published: 23 April 2019
(This article belongs to the Special Issue Astaxanthin: A Potential Therapeutic Agent)
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Abstract

Peroxisome proliferator-activated receptors (PPARs) are part of the nuclear hormone receptors superfamily that plays a pivotal role in functions such as glucose and lipid homeostasis. Astaxanthin (ASX) is a lipid-soluble xanthophyll carotenoid synthesized by many microorganisms and various types of marine life that is known to possess antioxidant, anti-inflammatory, antidiabetic, anti-atherosclerotic, and anticancer activities. As such, it is a promising nutraceutical resource. ASX-mediated modulation of PPARs and its therapeutic implications in various pathophysiological conditions are described in this review. ASX primarily enhances the action of PPARα and suppresses that of PPARβ/δ and PPARγ, but it has also been confirmed that ASX displays the opposite effects on PPARs, depending on the cell context. Anti-inflammatory effects of ASX are mediated by PPARγ activation, which induces the expression of pro-inflammatory cytokines in macrophages and gastric epithelial cells. The PPARγ-agonistic effect of ASX treatment results in the inhibition of cellular growth and apoptosis in tumor cells. Simultaneous and differential regulation of PPARα and PPARγ activity by ASX has demonstrated a hepatoprotective effect, maintaining hepatic lipid homeostasis and preventing related hepatic problems. Considering additional therapeutic benefits of ASX such as anti-gastric, cardioprotective, immuno-modulatory, neuroprotective, retinoprotective, and osteogenic effects, more studies on the association between ASX-mediated PPAR regulation and its therapeutic outcomes in various pathophysiological conditions are needed to further elucidate the role of ASX as a novel nutraceutical PPAR modulator. View Full-Text
Keywords: astaxanthin; peroxisome proliferator-activated receptors (PPARs); anti-inflammation; anticancer; lipid and glucose metabolism; PPAR modulator astaxanthin; peroxisome proliferator-activated receptors (PPARs); anti-inflammation; anticancer; lipid and glucose metabolism; PPAR modulator
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Choi, C.-I. Astaxanthin as a Peroxisome Proliferator-Activated Receptor (PPAR) Modulator: Its Therapeutic Implications. Mar. Drugs 2019, 17, 242.

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