Pharmacokinetics and first-pass metabolism of astaxanthin in rats

Choi, Hye Duck; Kang, Hee Eun; Yang, Sihyung; Lee, Myung Gull; Shin, Wonjae

doi:10.1017/s0007114510003454

Cited by 80 publications

(60 citation statements)

References 24 publications

(23 reference statements)

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“…Samples were prepared as previously reported. (19) Brieﬂy, 600 µl of acetone containing 2 µg/ml of β-apo-8'-carotenal, as an internal standard, was added to 100 µl of a serum sample. After vortex-mixing for 1 min, the mixture was extracted with 600 µl of hexane.…”

Section: Methodsmentioning

confidence: 99%

Astaxanthin prevents changes in the activities of thioredoxin reductase and paraoxonase in hypercholesterolemic rabbits

Augusti

Quatrin

Somacal

et al. 2012

J. Clin. Biochem. Nutr.

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This study explored the effects of the antioxidant astaxanthin on paraoxonase and thioredoxin reductase activities as well as on other oxidative stress parameters and on the lipid profile in hypercholesterolemic rabbits. Rabbits were fed a standard or a hypercholesterolemic diet alone or supplemented with 50, 100 and 500 mg/100 g of astaxanthin for 60 days. Antioxidant enzymes activities, lipid profile and oxidative stress markers were evaluated in the serum. The hypercholesterolemic diet increased lipids, including unsaturated fatty acids level, whereas it decreased saturated fatty acids level. These changes were accompanied by increased levels of oxidized low-density lipoprotein and oxidized low-density lipoprotein antibodies, as well as lipid and protein oxidation. Astaxanthin (100 and 500 mg/100 g) prevented hypercholesterolemia-induced protein oxidation, whereas 500 mg/100 g of astaxanthin decreased protein oxidation per se . The activities of superoxide dismutase and thioredoxin reductase were enhanced, whereas paraoxonase activity was inhibited in hypercholesterolemic rabbits. All astaxanthin doses prevented changes in thioredoxin reductase and paraoxonase activities. This effect was not related to a direct effect of astaxanthin on these enzymes, because in vitro astaxanthin enhanced thioredoxin reductase and had no effect on paraoxonase activity. Astaxanthin could be helpful in cardiovascular diseases by restoring thioredoxin reductase and paraoxonase activities.

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Section: Methodsmentioning

confidence: 99%

Astaxanthin prevents changes in the activities of thioredoxin reductase and paraoxonase in hypercholesterolemic rabbits

Augusti

Quatrin

Somacal

et al. 2012

J. Clin. Biochem. Nutr.

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“…It was reported that the parameters of ASX were dose dependent if administrated intravenously, but dose independent if taken orally, due to primary metabolizm by hepatic cytochrome P450 [41]. Besides, diet could elevate the bioavailability of ASX significantly [42].…”

Section: Discussionmentioning

confidence: 99%

Astaxanthin mitigates cobalt cytotoxicity in the MG-63 cells by modulating the oxidative stress

Da-he

Tong

Liu

et al. 2017

BMC Pharmacol Toxicol

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BackgroundWith the re-popularity of metal-on-metal (MoM) bearing in recent years, the cobalt toxicity has been a cause for concern in the total hip replacement surgery by both physicians and patients.MethodsMG-63 cell line was cultured in vitro and incubated with cobalt (II) chloride (CoCl2) and/or with astaxanthin (ASX) for 24 h. MTT assay was conducted to evaluate the cell viability after cobalt exposure and ASX treatment. Fluorescence-activated cell sorting (FACS) analysis was performed to examine the reactive oxygen species (ROS) level. Quantitative real-time polymerase chain reaction (PCR) was adopted to determine the mRNA levels of related targets. And western blot analysis was used to examine the protein expressions. One-way ANOVA with posttest Newman-Keuls multiple comparisons was adopted to analysis all the obtained data.ResultsIn the current study, ASX exhibited significant protective effect against the Co(II)-induced cytotoxicity in MG-63 cell line. We also found that ASX protected the cells against Co-induced apoptosis by regulating the expression of Bcl-2 family proteins. Besides, heme oxygenase 1 (HO-1) could be activated by Co exposure; ASX treatment significantly inhibited HO-1 activation, suppressing the oxidative stress induced by Co exposure. Moreover, c-Jun N-terminal Kinase (JNK) phosphorylation was shown to participate in the signaling pathway of the protective effect of ASX. However, knockdown of JNK expression by siRNA transfection or JNK inhibitor SP600125 treatment did not affect the protective effect of ASX against cobalt cytotoxicity in MG-63 cells.ConclusionsASX mitigated cobalt cytotoxicity in the MG-63 cells by modulating the oxidative stress. And ASX could be a promising therapy against cobalt toxicity in the hip articulation surgery.Electronic supplementary materialThe online version of this article (doi:10.1186/s40360-017-0166-1) contains supplementary material, which is available to authorized users.

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“…Sebuah studi mengenai farmakokinetik dan adanya mekanisme degradasi via first pass metabolism menyatakan bahwa rasio ekstraksi eliminasi astaxanthin oleh hepatik dan gastrointestinal masing-masing 0,490 dan 0,901. Nilai rasio ekstraksi eliminasi berkisar antara 0 dan 1 dimana nilai rasio mendekati 1 menunjukkan bahwa obat tereliminasi oleh organ yang dimaksud [7].…”

Section: Pendahuluanunclassified

Formulasi dan Karakterisasi SNE (Self Nanoemulsion) Astaxanthin dari Haematococcus pluvialis sebagai Super Antioksidan Alami

2017

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ABSTRACT:Astaxanthin is a group of fat-soluble xanthophyll carotenoid found in many microorganisms and marine animals. The problem that exists in its use as active compound of antioxidants is due to lipophilicity and poor stability in the gastrointestinal tract thereby making low bioavailability. In this research offers the nanotechnology to develop astaxanthin nanoemulsion which is intended to improve the stability in the dosage form and also further developing new delivery paths in the use of antioxidants through transdermal delivery route so it has the optimal deliveries. In this research will be made nanoemulsion astaxanthin formulation to produce good physical and chemical characteristics. Nanoemulsion were prepared by using the self-nanoemulsifying (SNE) method. Optimizations of formula were performed ranging from oil phase screening, surfactant type screening, and optimization of ratio of oil phase : surfactant : co-surfactant. Characterization of nanoemulsion were carried out by physical characterizations including globul size and polydispersity index, zeta potential, visual appearance, and globul morphology. Chemical Characterization included the entrapment efficiency test. The results showed that the nanoemulsion Astaxanthin has a 10-20 nm globul size (with normal size distribution curve), the polydispersity index value is less than 0.5, the zeta potential is greater than (-20) mV, the entrapment efficiency is between 80-87%, and has spherical globules form. ABSTRAK:Astaxanthin merupakan kelompok karotenoid xantofil larut lemak yang banyak ditemukan pada berbagai mikroorganisme dan hewan laut. Permasalahan yang terdapat di dalam pengunaannya sebagai bahan aktif sumber antioksidan adalah karena lipofilisitasnya dan stabilitas astaxanthin yang rendah di dalam saluran cerna sehingga membuat ketersediaan hayati yang rendah. Di dalam penelitian ini menawarkan teknologi nano untuk mengembangkan nanoemulsi astaxanthin yang ditujukan untuk meningkatkan stabilitas astaxanthin di dalam sediaan dan juga kedepannya untuk mengembangkan jalur penghantaran baru dalam pemakaian antioksidan yakni melalui rute transdermal sehingga ditujukan agar penggunaan astaxanthin dapat optimal. Di dalam penelitian ini akan dibuat formulasi nanoemulsi astaxanthin untuk menghasilkan karakteristik fisik dan kimia yang baik. Nanoemulsi dibuat dengan menggunakan metode Nanoemulsi spontan (SNE). Dilakukan optimasi formula mulai dari skrining fase minyak, skrining jenis surfaktan, dan optimasi rasio fase minyak:surfaktan:kosurfaktan. Karakterisasi nanoemulsi berupa karakterisasi secara fisik meliputi ukuran globul dan indeks polidispersitas, potensial zeta, tampilan visual, dan morfologi globul. Karakterisasi secara kimia meliputi uji efisiensi penjeratan. Hasil penelitian menunjukkan nanoemulsi Astaxanthin yang dikembangkan memiliki ukuran globul 10-20 nm (dengan kurva distribusi ukuran globul normal), nilai indeks polidispersitas kurang dari 0.5, potensial zeta lebih besar dari (-20) mV, dan efisiensi penjeratan berkisar antara 80-87% s...

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Pharmacokinetics and first-pass metabolism of astaxanthin in rats

Cited by 80 publications

References 24 publications

Astaxanthin prevents changes in the activities of thioredoxin reductase and paraoxonase in hypercholesterolemic rabbits

Astaxanthin prevents changes in the activities of thioredoxin reductase and paraoxonase in hypercholesterolemic rabbits

Astaxanthin mitigates cobalt cytotoxicity in the MG-63 cells by modulating the oxidative stress

Formulasi dan Karakterisasi SNE (Self Nanoemulsion) Astaxanthin dari Haematococcus pluvialis sebagai Super Antioksidan Alami

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