Hydrophilic Astaxanthin: PEGylated Astaxanthin Fights Diabetes by Enhancing the Solubility and Oral Absorbability

Liu, Yanzi; Yang, Lu; Guo, Yongli; Zhang, Ting; Xiao, Qiao; Xu, Jie; Xue, Changhu

doi:10.1021/acs.jafc.0c00784

Cited by 27 publications

(15 citation statements)

References 36 publications

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“…Further, the administration of AOD reversed HFD-induced oxidative stress injury and inflammation, as supported by the reduced MDA level and the expression levels of inflammatory cytokines (e.g., TNF-α, IL-1β, and IFN-γ). Similar antidiabetic and anti-inflammatory effects were found in astaxanthin polyethylene glycol succinate conjugates, which is a synthetic hydrophilic astaxanthin with significantly enhanced solubility and stability compared with AST [25]. Further study was conducted around gut microbiota in our research.…”

Section: Discussionsupporting

confidence: 59%

Astaxanthin n-Octanoic Acid Diester Ameliorates Insulin Resistance and Modulates Gut Microbiota in High-Fat and High-Sucrose Diet-Fed Mice

Gao

Yang

Chin

et al. 2020

IJMS

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Astaxanthin n-octanoic acid diester (AOD) is a type of astaxanthin connecting medium-chain fatty acids with a more stable structure. In this study, we examined the role of AOD in ameliorating insulin resistance (IR) induced by a high-fat and high-sucrose diet (HFD) as well as its effect on modulating gut microbiota in mice, with free astaxanthin (AST) as a comparison. Four groups of male C57BL/6J mice (6 weeks old; n = 10 per group) were fed with a normal control diet (NC), HFD orally administered with AOD, AST (50 mg/kg body weight), or vehicle for 8 weeks. AOD improved glucose tolerance, IR, systematic and intestinal inflammation, and intestinal integrity better than AST. Further, both AOD and AST modulated gut microbiota. A significantly higher abundance of Bacteroides and Coprococcus was found in AOD than in AST, and the predicted pathway of carbohydrate metabolism was significantly impacted by AOD. Overall, AOD may play a role in alleviating IR and inflammation with the modulating effect on microbiota in HFD-fed mice. Our findings could facilitate the development of AOD as a bioactive nutraceutical and more stable alternative to AST.

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Section: Discussionsupporting

confidence: 59%

Astaxanthin n-Octanoic Acid Diester Ameliorates Insulin Resistance and Modulates Gut Microbiota in High-Fat and High-Sucrose Diet-Fed Mice

Gao

Yang

Chin

et al. 2020

IJMS

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“…Similarly, astaxanthin could suppress the activation of the NOD-, LRR-, and pyrin domain-containing protein 3 (NLRP3) inflammasome in macrophages (Peng et al, 2020). Moreover, multiple in vivo studies have revealed the anti-inflammatory effects of astaxanthin in different disease models, including non-alcoholic fatty liver (Bhuvaneswari et al, 2014;Ni et al, 2015;Chiu et al, 2016;Jia et al, 2016), hepatic injury or fibrosis Han et al, 2018;Liu et al, 2018;Zhang Z. et al, 2020), kidney injury (Guo et al, 2021), myocardial injury (Xie et al, 2020), diabetes mellitus (Feng et al, 2020;Liu et al, 2020;Zhuge et al, 2021), arthritis (Park MH. et al, 2020;Kumar et al, 2020), gastroenteritis inflammation (Han et al, 2020;Chen Y. et al, 2021), acute pancreatitis (Yasui et al, 2011), asthma (Hwang et al, 2017), atopic dermatitis (Park et al, 2018;Park et al, 2019), and hyperosmoticity-induced dry eye (Li H. et al, 2020).…”

Section: Astaxanthin Inhibits Peripheral Inflammationmentioning

confidence: 99%

The Putative Role of Astaxanthin in Neuroinflammation Modulation: Mechanisms and Therapeutic Potential

Wang

2022

Front. Pharmacol.

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Neuroinflammation is a protective mechanism against insults from exogenous pathogens and endogenous cellular debris and is essential for reestablishing homeostasis in the brain. However, excessive prolonged neuroinflammation inevitably leads to lesions and disease. The use of natural compounds targeting pathways involved in neuroinflammation remains a promising strategy for treating different neurological and neurodegenerative diseases. Astaxanthin, a natural xanthophyll carotenoid, is a well known antioxidant. Mounting evidence has revealed that astaxanthin is neuroprotective and has therapeutic potential by inhibiting neuroinflammation, however, its functional roles and underlying mechanisms in modulating neuroinflammation have not been systematically summarized. Hence, this review summarizes recent progress in this field and provides an update on the medical value of astaxanthin. Astaxanthin modulates neuroinflammation by alleviating oxidative stress, reducing the production of neuroinflammatory factors, inhibiting peripheral inflammation and maintaining the integrity of the blood-brain barrier. Mechanistically, astaxanthin scavenges radicals, triggers the Nrf2-induced activation of the antioxidant system, and suppresses the activation of the NF-κB and mitogen-activated protein kinase pathways. With its good biosafety and high bioavailability, astaxanthin has strong potential for modulating neuroinflammation, although some outstanding issues still require further investigation.

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“…It produced PEG-6HF in 10 mM HEPES pH 7.4 solution at 37 °C for 6 hours, mimicking the biological environment. A sufficient number of samples were collected every hour, and the changes were constantly monitored using a UV-Vis spectrophotometer (Charoensit et al, 2019;Liu et al, 2020). The percentages of the degradation 6HF were calculated based on the initial absorbance of both samples.…”

Section: Resultsmentioning

confidence: 99%

A Facile Conjugation of 6-Hydroxylflavone Biomolecule with Polyethylene Glycol for Enhancing Conjugate Stability

Jamaludin¹,

Harun²

2022

IJTech

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6-Hydroxyflavone (6HF) contains attractive biological properties of significance pharmacologically and has been discovered as an effective diabetic medication. However, due to its high degradation in aqueous solution, its efficacy in biological treatment remains a considerable obstacle. Thus, conjugating a polymer, polyethylene-glycol, to 6HF by direct esterification between the carboxyl group of PEG and the hydroxyl group at the sixth carbon of the 6HF biomolecule is one of the approaches applied in this research to increase its stability while maintaining the inherent biological characteristics. This study examined the optimum esterification reaction conditions for conjugate PEG-6HF utilizing EDC and DMAP as conjugation reagents in various solvents, such as DMSO, PBS, and PBS 10 mM HEPES pH7.4 with the assistance of HOBt, including its stability in the biomimicking environment. For this purpose, PEG-6HF connected through the ester bond was validated using various analytical techniques such as FTIR, UV-Vis spectroscopy, and HPLC. , Notably, esterification at 25 °C for 24 hours in a 10 mM HEPES pH 7.4 buffer solution using EDC with HOBt resulted in the most significant conjugation percentage, 42 percent. Furthermore, PEG-6HF revealed 1.3 times lower degradation percentages of 6HF biomolecules than unconjugated-6HF following 6 hours of incubation in 10 mM HEPES pH 7.4 at 37 °C. Hence, the optimal conditions and the resulting conjugation percentage with high stability are expected to be a fundamental approach to conjugated polymer with a biomolecule.

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Hydrophilic Astaxanthin: PEGylated Astaxanthin Fights Diabetes by Enhancing the Solubility and Oral Absorbability

Cited by 27 publications

References 36 publications

Astaxanthin n-Octanoic Acid Diester Ameliorates Insulin Resistance and Modulates Gut Microbiota in High-Fat and High-Sucrose Diet-Fed Mice

Astaxanthin n-Octanoic Acid Diester Ameliorates Insulin Resistance and Modulates Gut Microbiota in High-Fat and High-Sucrose Diet-Fed Mice

The Putative Role of Astaxanthin in Neuroinflammation Modulation: Mechanisms and Therapeutic Potential

A Facile Conjugation of 6-Hydroxylflavone Biomolecule with Polyethylene Glycol for Enhancing Conjugate Stability

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