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In vitro and in vivo structure and activity relationship analysis of polymethoxylated flavonoids: Identifying sinensetin as a novel antiangiogenesis agent
Lam I.K.1; Alex D.1; Wang Y.-H.2; Liu P.2; Liu A.-L.1; Du G.-H.3; Yuen Lee S.M.1
2012
Source PublicationMolecular Nutrition and Food Research
ISSN16134125
Volume56Issue:6Pages:945
Abstract

Scope: Polymethoxylated flavonoids are present in citrus fruit in a range of chemical structures and abundance. These compounds have potential for anticarcinogenesis, antitumor, and cardiovascular protective activity, but the effect on angiogenesis has not been well studied. Methods and results: Human umbilical vein endothelial cells (HUVECs) in vitro and zebrafish (Danio rerio) in vivo models were used to screen and identify the antiangiogenesis activity of seven polymethoxylated flavonoids; namely, hesperetin, naringin, neohesperidin, nobiletin, scutellarein, scutellarein tetramethylether, and sinensetin. Five, excluding naringin and neohesperidin, showed different degrees of potency of antiangiogenesis activity. Sinensetin, which had the most potent antiangiogenesis activity and the lowest toxicity, inhibited angiogenesis by inducing cell cycle arrest in the G0/G1 phase in HUVEC culture and downregulating the mRNA expressions of angiogenesis genes flt1, kdrl, and hras in zebrafish. Conclusion: The in vivo structure-activity relationship (SAR) analysis indicated that a flavonoid with a methoxylated group at the C3' position offers a stronger antiangiogenesis activity, whereas the absence of a methoxylated group at the C8 position offers lower lethal toxicity in addition to enhancing the antiangiogenesis activity. This study provides new insight into how modification of the chemical structure of polymethoxylated flavonoids affects this newly identified antiangiogenesis activity. © 2012 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

KeywordAngiogenesis Polymethoxylated Flavonoid Sinensetin Structure-activity Relationship Zebrafish
DOI10.1002/mnfr.201100680
URLView the original
Indexed BySCI
Language英语
WOS Research AreaFood Science & Technology
WOS SubjectFood Science & Technology
WOS IDWOS:000305323100011
The Source to ArticleScopus
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Cited Times [WOS]:47   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionInstitute of Chinese Medical Sciences
Corresponding AuthorYuen Lee S.M.
Affiliation1.Institute of Chinese Medical Sciences, University of Macau, , Taipa, Macao SAR, P. R. China
2.Longhua Hospital, Shanghai University of Traditional Chinese Medicine, , Shanghai, P. R. China
3.Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, , Beijing, P. R. China
First Author AffilicationInstitute of Chinese Medical Sciences
Corresponding Author AffilicationInstitute of Chinese Medical Sciences
Recommended Citation
GB/T 7714
Lam I.K.,Alex D.,Wang Y.-H.,et al. In vitro and in vivo structure and activity relationship analysis of polymethoxylated flavonoids: Identifying sinensetin as a novel antiangiogenesis agent[J]. Molecular Nutrition and Food Research,2012,56(6):945.
APA Lam I.K..,Alex D..,Wang Y.-H..,Liu P..,Liu A.-L..,...&Yuen Lee S.M..(2012).In vitro and in vivo structure and activity relationship analysis of polymethoxylated flavonoids: Identifying sinensetin as a novel antiangiogenesis agent.Molecular Nutrition and Food Research,56(6),945.
MLA Lam I.K.,et al."In vitro and in vivo structure and activity relationship analysis of polymethoxylated flavonoids: Identifying sinensetin as a novel antiangiogenesis agent".Molecular Nutrition and Food Research 56.6(2012):945.
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