Bioassays for estrogenic activity: Development and validation of estrogen receptor (ERα/ERβ) and breast cancer proliferation bioassays to measure serum estrogenic activity in clinical studies

Assay and Drug Development Technologies

Volumn 7, Issue 1, 2009, Pages 80-89

  Li, J ^a   Lee, L ^a   Gong, Y ^a   Shen, P ^a   Wong, S P ^a   Wise, Stephen D ^b   Yong, E L ^a  

^a NATIONAL UNIVERSITY HOSPITAL   (Singapore)

^b Eli Lilly Singapore Pte Ltd   (Singapore)

Author keywords

[No Author keywords available]

Indexed keywords

EPIMEDIUM EXTRACT; ESTRADIOL; ESTRADIOL VALERATE; ESTROGEN RECEPTOR ALPHA; ESTROGEN RECEPTOR BETA; ESTRONE;

ADULT; ARTICLE; BIOASSAY; BREAST CANCER; CANCER CELL CULTURE; CELL PROLIFERATION; CELL STRAIN MCF 7; CHINESE MEDICINE; CLINICAL ARTICLE; CLINICAL TRIAL; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; CROSSOVER PROCEDURE; DIAGNOSTIC VALUE; DIARRHEA; ESTRADIOL BLOOD LEVEL; ESTROGEN ACTIVITY; ESTROGEN BLOOD LEVEL; ESTRONE BLOOD LEVEL; FEMALE; HUMAN; HUMAN CELL; PREDICTION; RANDOMIZED CONTROLLED TRIAL; REPORTER GENE; SINGLE DRUG DOSE; TANDEM MASS SPECTROMETRY; TRANSACTIVATION;

ADULT; AGED; ANDROGENS; BIOLOGICAL ASSAY; BREAST NEOPLASMS; CALIBRATION; CELL LINE, TUMOR; CELL PROLIFERATION; CHROMATOGRAPHY, HIGH PRESSURE LIQUID; CROSS-OVER STUDIES; DOUBLE-BLIND METHOD; EPIMEDIUM; ESTROGEN RECEPTOR ALPHA; ESTROGEN RECEPTOR BETA; ESTROGENS; FEMALE; HUMANS; MIDDLE AGED; PHYTOESTROGENS; PLANT EXTRACTS; STEROIDS; TANDEM MASS SPECTROMETRY; YOUNG ADULT;

EID: 65349116538     PISSN: 1540658X     EISSN: None     Source Type: Journal    
DOI: 10.1089/adt.2008.154     Document Type: Article

References (40)

1. Margeat E, Bourdoncle A, Margueron R, Poujol N, Cavailles V, Royer C: Ligands differentially modulate the protein interactions of the human estrogen receptors alpha and beta. J Mol Biol 2003;326:77-92.
2. Koehler KF, Helguero LA, Haldosen LA, Warner M, Gustafsson JA: Reflections on the discovery and significance of estrogen receptor beta. Endocr Rev 2005;26:465-478.
3. Johnson KA: The SERM of my dreams. J Clin Endocrinol Metab 2006;91:3754-3756.
4. Rossouw JE, Anderson GL, Prentice RL, LaCroix AZ, Kooperberg C, Stefanick ML, et al.: Risks and benefits of estrogen plus progestin in healthy postmenopausal women: principal results from the Women's Health Initiative randomized controlled trial. JAMA 2002;288:321-333.
5. Nikander E, Metsa-Heikkila M, Ylikorkala O, Tiitinen A: Effects of phytoestrogens on bone turnover in postmenopausal women with a history of breast cancer. J Clin Endocrinol Metab 2004;89:1207-1212.
6. Verheus M, van Gils CH, Keinan-Boker L, Grace PB, Bingham SA, Peeters PH: Plasma phytoestrogens and subsequent breast cancer risk. J Clin Oncol 2007;25:648-655.
7. Mcintosh J, Blalock SJ: Effects of media coverage of Women's Health Initiative study on attitudes and behavior of women receiving hormone replacement therapy. Am J Health Syst Pharm 2005;62:69-74.
8. Yap SP, Shen P, Butler MS, Gong Y, Loy CJ, Yong EL: New estrogenic prenyl- flavone from Epimedium brevicornum inhibits the growth of breast cancer cells. Planta Med 2005;71:114-119.
9. Yap SP, Shen P, Li J, Lee LS, Yong EL: Molecular and pharmacodynamic properties of estrogenic extracts from the traditional Chinese medicinal herb, Epimedium. J Ethnopharmacol 2007;1 13:218-224.
10. De Naeyer A, Pocock V, Milligan S, De Keukeleire D: Estrogenic activity of a polyphenc extract of the leaves of Epimedium brevicornum. Fitoterapia 2005;76:35-40.
11. Wang ZQ, Lou YJ: Proliferation-stimulating effects of icaritin and desmethyli- caritin in MCF-7 cells. Eur J Pharmacol 2004;504:147-153.
12. Chen KM, Ge BF, Ma HP, Liu XY, Bai MH, Wang Y: Icariin, a flavonoid from the herb Epimedium enhances the osteogenic differentiation of rat primary bone marrow stromal cells. Pharmazie 2005;60:939-942.
13. Meng FH, Li YB, Xiong ZL, Jiang ZM, Li FM: Osteoblastic proliferative activity of Epimedium brevicornum Maxim. Phytomedicine 2005;12: 189-193.
14. Zhang G, Qin L, Hung WY, Shi YY, Leung PC, Yeung HY, et al.: Flavonoids derived from herbal Epimedium brevicornum Maxim prevent OVX-induced osteoporosis in rats independent of its enhancement in intestinal calcium absorption. Bone 2006;38:818-825.
15. Zhang G, Qin L, Shi Y: Epimedium-derived phytoestrogen flavonoids exert beneficial effect on preventing bone loss in late postmenopausal women: a 24-month randomized, double-blind and placebo-controlled trial. J Bone Miner Res 2007; 22:1072-1079.
16. Prestwood KM: The search for alternative therapies for menopausal women: estrogenic effects of herbs. J Clin Endocrinol Metab 2003; 88:4075-4076.
17. Yong EL, Wong SP, Shen P, Gong YH, Li J, Hong Y: Standardization and evaluation of botanical mixtures: lessons from a traditional Chinese herb, Epimedium, with oestrogenic properties. Novartis FoundSymp 2007;282:173-188; discussion 188-191, 212-178.
18. Messina M, McCaskill-Stevens W, Lampe JW: Addressing the soy and breast cancer relationship: review, commentary, and workshop proceedings. J Natl Cancer Inst 2006;98:1275-1284.
19. Gagnier JJ, Boon H, Rochon P, Moher D, Barnes J, Bombardier C: Reporting randomized, controlled trials of herbal interventions: an elaborated CONSORT statement. Ann Intern Med 2006;144:364-367.
20. Chen XJ, Guo BL, Li SP, Zhang QW, Tu PF, Wang YT: Simultaneous determination of 15 flavonoids in Epimedium using pressurized liquid extraction and high-performance liquid chromatography. J Chromatogr A 2007;1163:96-104.
21. Gong Y, Yip SC, Thamarai SK, Zhang J, Lee HK, Yong EL: Trace analysis of icariin in human serum with dansyl chloride derivatization after oral administration of Epimedium decoction by liquid chromatography tandem mass spectrometry. J Chromatogr B Analyt Technol Biomed Life Sci 2007;860:166-172.
22. Shen P, Guo BL, Gong Y, Hong DY, Hong Y, Yong EL: Taxonomic, genetic, chemical and estrogenic characteristics of Epimedium species. Phytochemistry 2007;68:1448-1458.
23. Sonneveld E, Riteco JA, Jansen HJ, Pieterse B, Brouwer A, Schoonen WG, et al.: Comparison of in vitro and in vivo screening models for androgenic and estrogenic activities. Toxicol Sci 2006;89:173-187.
24. Paris F, Servant N, Terouanne B, Balaguer P, Nicolas JC, Sultan C: A new recombinant cell bioassay for ultrasensitive determination of serum estrogenic bioactivity in children. J Clin Endocrinol Metab 2002;87:791-797.
25. Wang S, Paris F, Sultan CS, Song RX, Demers LM, Sundaram B, et al.: Recombinant cell ultrasensitive bioassay for measurement of estrogens in postmenopausal women. J Clin Endocrinol Metab 2005;90:1407-1413.
26. Wong SP, Li J, Shen P, Gong Y, Yap SP, Yong EL: Ultrasensitive cell-based bioassay for the measurement of global estrogenic activity of flavonoid mixtures revealing additive, restrictive, and enhanced actions in binary and higher order combinations. Assay Drug Dev Technol 2007;5:355-362.
27. Gong Y, Chin HS, Lim LS, Loy CJ, Obbard JP, Yong EL: Clustering of sex hormone disruptors in Singapore's marine environment. Environ Health Perspect 2003;111:1448-1453.
28. Rey deCastro B, Neuberg D: The statistical performance of an MCF-7 cell culture assay evaluated using generalized linear mixed models and a score test. Stat Med 2007;26:2501-2518.
29. Nelson RE, Grebe SK, O'Kane DJ, Singh RJ: Liquid chromatography-tandem mass spectrometry assay for simultaneous measurement of estradiol and estrone in human plasma. Clin Chem 2004;50:373-384.
30. Rabe-Hesketh SA, Pickles A: Reliable estimation of generalized linear mixed models using adaptive quadrature. Stata J 2002;2:1-21.
31. Miller KJ, Bowsher RR, Celniker A, Gibbons J, Gupta S, Lee JW, et al.: Workshop on bioanalytical methods validation for macromolecules: summary report. Pharm Res 2001;18:1373-1383.
32. Vree TB, Timmer CJ: Enterohepatic cycling and pharmacokinetics of estradiol in post-menopausal women. J Pharm Pharmacol 1998;50:857-864.
33. Kuiper GG, Carlsson B, Grandien K, Enmark E, Haggblad J, Nilsson S, et al.: Comparison of the ligand binding specificity and transcript tissue distribution of estrogen receptors alpha and beta. Endocrinology 1997;138:863-870.
34. Ozers MS, Ervin KM, Steffen CL, Fronczak JA, Lebakken CS, Carnahan KA, et al.: Analysis of ligand-dependent recruitment of coactivator peptides to estrogen receptor using fluorescence polarization. Mol Endocrinol 2005;19:25-34.
35. Miyoshi Y, Tanji Y, Taguchi T, Tamaki Y, Noguchi S: Association of serum estrone levels with estrogen receptor-positive breast cancer risk in post- menopausal Japanese women. Clin Cancer Res 2003;9:2229-2233.
36. Missmer SA, Eliassen AH, Barbieri RL, Hankinson SE: Endogenous estrogen, androgen, and progesterone concentrations and breast cancer risk among postmenopausal women. J Natl Cancer Inst 2004;96:1856-1865.
37. van den Beld AW, de Jong FH, Grobbee DE, Pols HA, Lamberts SW: Measures of bioavailable serum testosterone and estradiol and their relationships with muscle strength, bone density, and body composition in elderly men. J Clin Endocrinol Metab 2000;85:3276-3282.
38. Albertsson-Wikland K, Rosberg S, Lannering B, Dunkel L, Selstam G, Norjavaara E: Twenty-four-hour profiles of luteinizing hormone, follicle-stimulating hormone, testosterone, and estradiol levels: a semilongitudinal study throughout puberty in healthy boys. J Clin Endocrinol Metab 1997;82:541-549.
39. Williamson G, Manach C: Bioavailability and bioefficacy of polyphenols in humans. II. Review of 93 intervention studies. Am J Clin Nutr 2005;81(Suppl):243S-255S.
40. 41Ca. J Clin Endocrinol Metab 2007;92:577-582.