徳島大学 教育・研究者情報データベース(EDB)

1. 福田 達也

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2. (英) Hirai Shota / (日) 平井 将太 / (読) ひらい しょうた

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3. 吉田 達貞

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4. (英) Maoka T

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5. 小暮 健太朗([徳島大学.大学院医歯薬学研究部.薬学域.薬科学部門.創薬科学系.衛生薬学])

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(英) Protective effect of antioxidative liposomes co-encapsulating astaxanthin and capsaicin on CCl₄-induced liver injury

(英) Our previous study reported that co-encapsulation of potent antioxidants astaxanthin (Asx) and capsaisin (Cap) into liposomes brought about synergistically higher antioxidative activity than the calculated additive activity of each single antioxidant encapsulating liposome. Based on the previous computational chemistry analysis, the synergistic effect was revealed to be resulted from intermolecular interactions between Asx, especially 3R,3'R-form of Asx stereoisomer (Asx-R), and Cap, by which changes of electronic states of the polyene moiety of Asx-R were induced. Although liposomes co-encapsulating Asx-R and Cap (Asx-R/Cap-Lipo) at an optimal ratio clearly showed synergistic antioxidative activity in vitro, it is unclear whether the effective antioxidative activity derived from intermolecular interaction between Asx-R and Cap is also exerted in vivo. Therefore, in this study, we investigated therapeutic potential of Asx-R/Cap-Lipo as an antioxidant formulation in vivo. For this purpose, we employed carbon tetrachloride (CCl)-induced acute liver injury rat model, since CCl is known to cause oxidative damage in liver. CCl administration significantly increased the levels of aspartate transaminase (AST) and alanine aminotransferase (ALT). Intravenous combined administration of liposomes encapsulating Asx-R (Asx-R-Lipo) and liposomes encapsulating Cap (Cap-Lipo) significantly decreased CCl-induced increase of AST and ALT levels. Importantly, the treatment with Asx-R/Cap-Lipo tended to show higher protective effect on acute liver injury than combined treatment with Asx-R-Lipo plus Cap-Lipo. These results suggest that co-encapsulated Asx-R and Cap in liposomal membranes could exert more effective antioxidative activities in vivo, and that Asx-R/Cap-Lipo would be a hopeful antioxidant formulation for treating reactive oxygen species-related diseases.

1. (英) Article.ELocationID: 10.1248/bpb.b20-00116

2. (英) Article.PublicationTypeList.PublicationType: Journal Article

3. (英) KeywordList.Keyword: antioxidant

4. (英) KeywordList.Keyword: astaxanthin

5. (英) KeywordList.Keyword: capsaicin

6. (英) KeywordList.Keyword: intermolecular interaction

7. (英) KeywordList.Keyword: liposome

8. (英) KeywordList.Keyword: stereochemistry