Elsevier

Fitoterapia

Volume 115, December 2016, Pages 74-85
Fitoterapia

Review
A review on the pharmacological effects of vitexin and isovitexin

https://doi.org/10.1016/j.fitote.2016.09.011Get rights and content

Abstract

Vitexin and isovitexin are active components of many traditional Chinese medicines, and were found in various medicinal plants. Vitexin (apigenin-8-C-glucoside) has recently received increased attention due to its wide range of pharmacological effects, including but not limited to anti-oxidant, anti-cancer, anti-inflammatory, anti-hyperalgesic, and neuroprotective effects. Isovitexin (apigenin-6-C-glucoside), an isomer of vitexin, generally purified together with vitexin, also exhibits diverse biological activities. Latest research has suggested that vitexin and isovitexin could be potential substitute medicines for diversity diseases, and may be adjuvants for stubborn diseases or health products. This review summarized recent findings on various pharmacological activities and associative signalling pathways of vitexin and isovitexin to provide a reference for future research and clinical applications.

Section snippets

Chemical compounds referred in this article

Vitexin (PubChem CID: 5,280,441)

Isovitexin (PubChem CID: 162,350).

Chemical features of vitexin and isovitexin

Flavones are a class of flavonoids, which name after their common yellow colour, that is, flavus. Flavones are based on the backbone of 2-phenylchromen-4-one (2-phenyl-1-benzopyran-4-one) (flavone). Apigenin (4′,5,7-trihydroxyflavone) is one of typical natural flavones.

Vitexin and isovitexin, whose structures are shown in Fig. 1, belong to the class of flavones and are as derivatives of apigenin with 8/6-C-glucoside. Chemical properties of vitexin and isovitexin are similar. Vitexin is

Toxicity

As candidates of promising drugs, it is vital to examine safety of vitexin and isovitexin to human body. Until now, plenty of studies in vitro and in vivo have focused on the safety of vitexin, but very rare on isovitexin. Vitexin presents no cytotoxicity (IC50 > 200 μg/ml) in vitro [26]. In vivo, studies on Ficus deltoidea leaf extract, which contains high levels of vitexin and isovitexin, showed no significant acute and subchronic toxicity and genotoxicity [60]. Furthermore, regarding the liver

A brief overview of pharmacokinetic

Unusually, vitexin and isovitexin are poorly absorbed in the gastrointestinal tract [61]. They directly reached the colon where they were hydrolysed by the gut microflora through deglycosylation and ring-opening of the heterocyclic C ring [61]. It is likely that vitexin and isovitexin are degraded into small-molecule phenols and various aromatic acids such as phloretic acid (PA) [61]. Deglycosylated by intestinal bacterium Eubacterium cellulosolvens, isovitexin, rather than vitexin, was

Anti-oxidant effects

Oxidative stress at the cellular or subcellular level is a deleterious process that can be an important mediator of damage to cell structures and, consequently, various disease states. In addition, reactive oxygen radicals induced lipid peroxidation in cellular membranes and generate lipid peroxides, which caused extensive damage to membranes and membrane-mediated chromosomal damage [80], [81]. Thus, the anti-oxidant effects of some medicinal plants have garnered scientific interests; analyzing

Discussion

Flavonoids were found various bioactivities, including anti-oxidant and anti-inflammatory properties [155], [156] anti-neoplasia effect [157], [158], cognitive effects [159], [160], protective effect from cardiovascular disease [161], anti-diabetic effects [162] and many other effects. From structure of flavonids and known evidences for their bioactivities, structure of phenolic hydrogen in their molecules, especially o-tri- or o-di-hydroxyl structure in the A or B ring may be the active group

Acknowledgements

This study is supported by the National Natural Science Foundation of China (No. 81370737, 81371422 and 81571481), the Foundation of Health and Family Planning Commission of Hubei Province (WJ2015MB112). The authors have no conflicts of interest to declare.

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