title: Interaction of artemisinin and its derivatives with human serum albumin studied using spectroscopies and molecular modeling methods.
abstract: The interactions of artemisinins including artemisinin, dihydroartemisinin, artemether and artesunate with human serum albumin (HSA) were studied by fluorescence spectroscopy, UV-Vis absorption spectroscopy, synchronous fluorescence, three-dimensional fluorescence, circular dichroism (CD) and molecular modeling. Results obtained from analysis of fluorescence spectrum and fluorescence intensity indicated that the artemisinins had a strong ability to quench the intrinsic fluorescence of HSA through a static quenching procedure. Furthermore, the association constants K a and the corresponding thermodynamic parameters ΔH, ΔG and ΔS at various temperatures were also calculated. Based on the mechanism of Förster's non-radiative energy transfer theory, the distance between the acceptors and HSA were found. In addition, alteration of the secondary structure of HSA in the presence of the artemisinins was tested by CD spectroscopy. Molecular modeling revealed that the artemisinins were bounded in the large hydrophobic cavity of the site I of HSA.
authors: Department of cell biology, College of life science and technology, Jinan University, Guangzhou, 510632, People's Republic of China.
authors: Rongrong
authors: R
authors: Chen
authors: Hua
authors: H
authors: Jiang
authors: Hanlin
authors: H
authors: Pu
mesh_terms: D037621:Artemisinins / Q000737:chemistry* / Q000378:metabolism*; D001665:Binding Sites / Q000235:genetics; D002942:Circular Dichroism; D006801:Humans; D008958:Models, Molecular; D015394:Molecular Structure; D011485:Protein Binding; D012709:Serum Albumin / Q000378:metabolism*; D013050:Spectrometry, Fluorescence; D013816:Thermodynamics
chemical_list: D037621:Artemisinins; D012709:Serum Albumin; C031327:artemisinin
references: Biochem Pharmacol. 1993 Jul 20;46(2):336-9
references: 8347159
references: Biochem Pharmacol. 1987 Oct 15;36(20):3531-3
references: 2890353
references: Biochemistry. 1973 Oct 9;12(21):4161-70
references: 4795686
references: Toxicol Lett. 2004 Feb 28;147(1):53-61
references: 14700528
references: Chem Biol Interact. 1995 Jun 14;96(3):263-71
references: 7750165
references: J Biol Chem. 2001 Jun 22;276(25):22804-9
references: 11285262
references: Biomacromolecules. 2008 Mar;9(3):812-7
references: 18266320
references: Chem Rev. 2006 Jun;106(6):2224-48
references: 16771448
references: J Biochem. 2006 Oct;140(4):501-8
references: 16921164
references: Pharmacol Rev. 1981 Mar;33(1):17-53
references: 7027277
references: J Pharm Biomed Anal. 2004 Nov 19;36(4):915-9
references: 15533690
references: Annu Rev Biophys Biomol Struct. 2000;29:1-26
references: 10940241
references: J Fluoresc. 2008 Jan;18(1):109-18
references: 17899332
references: Nature. 1992 Jul 16;358(6383):209-15
references: 1630489
references: Bioorg Med Chem. 2005 Jun 2;13(12):4124-9
references: 15911327
references: J Phys Chem B. 2008 Dec 25;112(51):16793-801
references: 19367911
references: Anal Biochem. 1993 Sep;213(2):407-13
references: 7694523
references: J Photochem Photobiol B. 2009 Mar 3;94(3):183-90
references: 19126446
references: J Pharm Biomed Anal. 2010 Feb 5;51(3):768-73
references: 19853398
references: J Pharm Biomed Anal. 2004 May 28;35(3):655-64
references: 15137993
references: J Mol Biol. 2001 Dec 14;314(5):955-60
references: 11743713
references: J Pharm Biomed Anal. 2010 Nov 2;53(3):660-6
references: 20579830
references: Dan Med Bull. 1990 Feb;37(1):57-84
references: 2155760
references: Bioconjug Chem. 2004 Jul-Aug;15(4):738-46
references: 15264860
references: Biochemistry. 1981 May 26;20(11):3096-102
references: 7248271
references: J Lipid Res. 2003 Sep;44(9):1790-4
references: 12837852
references: Chirality. 2010 Jan;22(1):77-87
references: 19319989
references: J Pharm Biomed Anal. 2008 May 12;47(1):134-9
references: 18261869
references: Clin Pharmacokinet. 1994 Jan;26(1):44-58
references: 8137597
references: Bioelectrochemistry. 2009 Nov;77(1):26-30
references: 19643680
references: J Pharm Biomed Anal. 2008 Aug 5;47(4-5):981-4
references: 18495406
references: J Pharm Biomed Anal. 1999 Dec;21(4):775-85
references: 10701943
references: Spectrochim Acta A Mol Biomol Spectrosc. 2006 Nov;65(3-4):811-7
references: 16530468
references: Bioorg Med Chem. 2008 Apr 1;16(7):3878-86
references: 18291660
references: Antimicrob Agents Chemother. 1994 Aug;38(8):1813-9
references: 7986012
references: Int J Biol Macromol. 2006 Nov 15;39(4-5):291-7
references: 16730793