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Protoapigenone derivatives: Albumin binding properties and effects on HepG2 cells

Paper ID Volume ID Publish Year Pages File Format Full-Text
30356 44472 2013 7 PDF Available
Title
Protoapigenone derivatives: Albumin binding properties and effects on HepG2 cells
Abstract

•Effects of protoapigenone (Pa) and its derivatives were studied in HepG2 cells.•Anticancer effects of 1′-O-alkyl derivatives of Pa is increased compared to Pa.•Pa derivatives elevate apoptotic or necrotic rate and cell cycle arrest vs. Pa.•Fluorescence approaches indicated major differences in their albumin binding.•Our study gives pharmacokinetic data for designing further in vivo experiments.

Protoapigenone (Pa) is a flavone aglycone with a p-quinol structure in its B-ring. It was first discovered in Thelypteris torresiana, a native fern in Taiwan. Recent studies highlighted that protoapigenone and some of its derivatives show very potent anticancer activity against several types of tumors, using both in vitro and in vivo models. Despite the growing body of evidence on the selective anticancer potential of protoapigenone and its derivatives, no data are available on their pharmacokinetical properties. In our present research, albumin binding properties of Pa and seven different 1′-O-alkyl protoapigenone derivatives were analyzed as well as their biochemical effects on HepG2 tumor cell line in comparison with the flavone apigenin. Our results are in good accordance with the data of previous investigations of 1′-O-alkylated derivatives of protoapigenone (with the exception of isopropyl and allyl derivatives) showing similar or higher antitumor effects than Pa. Furthermore structural changes in Pa cause a very remarkable influence on plasma albumin binding affinity of the derivatives. Our investigation proves that parallel with changes of lipophilic character and extent of plasma protein binding properties of Pa derivatives a consequent alteration occurs in their pharmacokinetic behavior without losing the pharmacodynamic effect. Based on our study a better understanding of the structural and biochemical behavior of different chemically modified flavonoid derivatives could be achieved making further design of in vivo experiments feasible.

Keywords
Flavonoids; Protoapigenone derivatives; Anticancer effect; Albumin binding; Cell viability
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Publisher
Database: Elsevier - ScienceDirect
Journal: Journal of Photochemistry and Photobiology B: Biology - Volume 124, 5 July 2013, Pages 20–26
Authors
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Subjects
Physical Sciences and Engineering Chemical Engineering Bioengineering
Get Full-Text Now
Don't Miss Today's Special Offer
Price was $35.95
You save - $31
Price after discount Only $4.95
100% Money Back Guarantee
Full-text PDF Download
Online Support
Any Questions? feel free to contact us