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Review Article Open Access
Astaxanthin as a Medical Food
Eiji Yamashita
Department of Research & Development, Medical Nutrition Division, AstaReal Co., Ltd.,
Tokyo, Japan
Corresponding author: Eiji Yamashita, 2-6-3-12F, Shibakoen, Minato-ku, Tokyo 105-0011,
Japan
Submission date: April 28, 2013; Acceptance date: July 3, 2013; Publication date: July 3, 2013
ABSTRACT:
Astaxanthin is a red pigment that belongs to the carotenoid family like β-carotene. And it’s found
in seafood such as crustaceans: shrimp and crabs and fish: salmon and sea bream. Recently,
astaxanthin has been reported to have antioxidant activity up to 100 times more potent than that
of vitamin E against lipid peroxidation and about 40 times more potent than that of β-carotene on
singlet oxygen quenching. Astaxanthin does not show any pro-oxidant activity and its main sight
of action is on/in the cell membrane. Various important benefits to date have suggested for
human health such as immunomodulation, anti-stress, anti-inflammation, LDL cholesterol
oxidation suppression, enhanced skin health, improved semen quality, attenuating eye fatigue,
sport performance and endurance, limiting exercised induced muscle damage, suppressing the
development of life-style related diseases such as obesity, atherosclerosis, diabetes,
hyperlipidemia and hypertension. Nowadays, the research and demand for natural astaxanthin in
human health application are explosively growing worldwide. Especially, the clinicians use the
astaxanthin extracted from the microalgae, Haematotoccus pluvialis, as an add-on
supplementation for the patients who are unsatisfied with the current medications or who can’t
receive any medications because of their serious symptom. For example, the treatment enhances
their daily activity levels or QOL in heart failure or benign prostatic hypertrophy/lower urinary
tract symptom patients. Other studies and trials are under way on chronic diseases such as non-
alcoholic steatohepatitis, diabetes and CVD. We may call astaxanthin “a medical food” in the
near future.
Keywords: astaxanthin, medical food, Haematococcus, add-on supplementation
BACKGROUND:
Astaxanthin is widely and naturally distributed in marine organisms including crustaceans such
as shrimps and crabs and fish such as salmon and sea bream. In fact, it is one of the oldest
carotenoids isolated and identified from lobster, Astacus gammarus [1]. Astaxanthin was first
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commercially used for pigmentation only in the aquaculture industry. Later in 1991, when the
biological activity of potent antioxidative property was reported [2], astaxanthin as a food
supplement started gaining acceptance. Nowadays, the research and demand for natural
astaxanthin in human health application are explosively growing worldwide. In this article the
underlying basis to astaxanthin’s bioactivity and health promotional effects of natural
astaxanthin extracted from the microalgae, Haematotoccus pluvialis, are reviewed. And the
practical medical applications of natural astaxanthin are disclosed with the cases and reports by
the clinicians using the astaxanthin as an add-on supplementation for the patients who are
unsatisfied with the current medications or who can’t receive any medications because of their
serious symptom.
Uunderlying basis to astaxanthin’s bioactivity: Astaxanthin is a totally unique antioxidant,
because it possesses three novel distinctions at once.
Powerful antioxidant: The inhibitory activity of astaxanthin on the peroxyl radical mediated
lipid peroxidation was more than 100 times greater than that of α-tocopherol in the homogenate
of rat mitochondria [2]. Among twenty seven common hydrophilic and lipophilic antioxidants
such as polyphenols, toco-pherols, carotenoids, ascorbic acid, coenzyme Q10 and α-lipoic acid
astaxanthin showed the strongest singlet oxygen (1O2) quenching activity under the same test
condition of the chemilu-minescence detection system for direct 1O2 counting using the
thermodissociable endoperoxides of 1,4-dimethylnaphthalene as 1O2 generator in DMF : CDCl3
(9 : 1) [3]. Hydroxyl radical scavenging ability of astaxanthin encapsulated in liposomes was
more potent than that of α-tocopherol [4].
Safe antioxidant: Martin divided seventeen investigated carotenoids into three classes ; i)
without significant antioxidative properties, ii) anti- and pro-oxidants and iii) pure anti-oxidants.
Astaxanthin was classified as “pure anti-oxidants” not possessing any pro-oxidative properties
like β-carotene and lycopene [5]. Non-polar carotenoids such as lycopene and β-carotene
disordered the membrane bilayer enriched with polyunsaturated fatty acids and showed a potent
pro-oxidant effect (>85% increase in lipid hydroperoxide (LOOH) levels) while astaxanthin
preserved membrane structure and exhibited significant antioxidant activity (40% decrease in
LOOH levels) [6]. The photostability of the three carotenoids in the human dermal fibroblasts
was astaxanthin > canthaxanthin >> β-carotene. Only astaxantin efficiently abrogated the
apoptotic response to UVA. β-Carotene dose-dependently induced caspase-3 activity following
UVA exposure [7].
Superior position in cell membrane: Astaxanthin traps radicals not only at the conjugated
polyene chain but also in the terminal ring moiety, in which the hydrogen atom at the C3 methine
is suggested to be a radical trapping site. Owing to the equivalent amounts of the hydrophobic
intramolecular hydrogen-bonded ring and intermolecular hydrogen bonding with phospholipid
polar heads, and the interconversion between the two hydrogen bond formations, the terminal
ring of astaxanthin is able to scavenge radicals both at the surface and in the interior of the
phospholipid membrane, although its unsaturated polyene chain trapped radicals only in the
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membrane [8]. Figure 1 shows astaxanthin’s unique ability to span through the double layer cell
membrane. β-carotene and vitamin C only reside inside and outside the lipid bilayer membrane
respectively. The astaxanthin molecule is exposed both in- and outside of the cell giving better
overall protection.
Figure 1. Superior position in cell membrane. No other antioxidants possess the three unique
characters at once. This should be associated with its potent bioactivity.
Health promotional effects of natural astaxanthin: Numerous studies have shown that
astaxanthin has potential health-promoting effects in the prevention and treatment of various
diseases, such as cancers, chronic inflammatory diseases, metabolic syndrome, diabetes, diabetic
nephropathy, cardiovascular diseases, gastrointestinal diseases, liver diseases, neurodegenerative
diseases, eye diseases, skin diseases, exercise-induced fatigue, male infertility as reviewed by
Yuan [9]. It has been proven in over 65 clinical studies, featured in over 300 peer-reviewed
publications. Figure 2 shows the main benefits for human health. “Eye fatigue relieve” [10],
“skin aging defense” (anti-photoaging) [11] and “muscle resilience” (sports performance
enhancement) [12, 13] have been most clinically substantiated.
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©AstraReal 2012
Figure 2. Health promotional effects of astaxanthin
Practical medical applications of natural astaxanthin: Mostly two soft gel capsules of the
dietary supplement containing 12 mg of AstaREAL® astaxanthin extracted from the microalgae,
Haematotoccus pluvialis were used by the clinicians. Add-on supplementations of AstaREAL®
astaxanthin dramatically exhibited improvements in the patients who were unsatisfied with the
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current medications or who couldn’t receive any medications because of their serious symptom.
There were the cases that the administration improved the cardiac function in the heart failure
patients who is difficult to control with drug therapy and in the patients whose activity levels
were reduced because of chronic heart failure resulting in enhancing their daily activity levels
and QOL. The add-on effects of astaxanthin for treatment of benign prostatic hypertrophy/lower
urinary tract symptom (BPH/LUTS) were reported as an open-label preliminary study. A total of
thirty patients who had been treated with a1-blockers for more than 12 weeks and still had LUTS
intook the astaxanthin for eight weeks. The subjective symptoms and objective voiding
parameters were improved including QOL. Other studies and trials are under way on chronic
diseases such as non-alcoholic steatohepatitis, diabetes and CVD as well as infertility, atopic
dermatitis and androgenetic alopecia.
CONCLUSION:
A practical medical application of astaxanthin from Haematococcus will expand into medical
institution worldwide not only into the consumer space. We may call astaxanthin “a medical
food” at the moment.
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