Selective estrogen receptor modulators regulate stromal proliferation in human benign prostatic hyperplasia by multiple beneficial mechanisms - Action of two new agents

Investigational New Drugs

Volumn 30, Issue 2, 2012, Pages 582-593

  Kumar, Rajeev ^a   Verma, Vikas ^a   Sarswat, Amit ^a   Maikhuri, J P ^a   Jain, Ashish ^a   Jain, Rajeev K ^a   Sharma, V L ^a   Dalela, Diwakar ^b   Gupta, Gopal ^a  

^a CENTRAL DRUG RESEARCH INSTITUTE   (India)

^b KING GEORGE'S MEDICAL UNIVERSITY   (India)

Author keywords

Benign prostatic hyperplasia; Estrogen receptor beta; Finasteride; Selective estrogen receptor modulators; Tamoxifen

Indexed keywords

2 [4 (2 PIPERIDINOETHOXY)PHENYL] 3 PHENYL 2H 1 BENZOPYRAN; ANDROGEN RECEPTOR; ANDROSTANOLONE; CASPASE 3; CENTCHROMAN; EPIDERMAL GROWTH FACTOR RECEPTOR; ESTRADIOL; ESTROGEN RECEPTOR ALPHA; ESTROGEN RECEPTOR BETA; FAS ANTIGEN; FAS LIGAND; FINASTERIDE; HYDROXYTAMOXIFEN; NICOTINAMIDE ADENINE DINUCLEOTIDE ADENOSINE DIPHOSPHATE RIBOSYLTRANSFERASE; PROTEIN BAX; PROTEIN BCL 2; SOMATOMEDIN C; TAMOXIFEN; TESTOSTERONE; TRANSFORMING GROWTH FACTOR BETA1; 4-HYDROXYTAMOXIFEN; AFIMOXIFENE; AR PROTEIN, HUMAN; AROMATASE; BENZOPYRAN DERIVATIVE; DRUG DERIVATIVE; ESTROGEN RECEPTOR ALPHA, HUMAN; MESSENGER RNA; PIPERIDINE DERIVATIVE; SELECTIVE ESTROGEN RECEPTOR MODULATOR; STEROID 5ALPHA REDUCTASE INHIBITOR;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ARTICLE; CELL PROLIFERATION; CONTROLLED STUDY; DRUG EFFICACY; DRUG MECHANISM; DRUG POTENCY; ENZYME ACTIVITY; EPITHELIUM CELL; EX VIVO STUDY; HISTOLOGY; HUMAN; HUMAN CELL; HUMAN TISSUE; IMMUNOBLOTTING; IN VITRO STUDY; MALE; NONHUMAN; POLYACRYLAMIDE GEL ELECTROPHORESIS; PRIORITY JOURNAL; PROSTATE HYPERTROPHY; PROTEIN CLEAVAGE; PROTEIN EXPRESSION; RAT; REAL TIME POLYMERASE CHAIN REACTION; STROMA CELL; ANIMAL; APOPTOSIS; CELL CULTURE; CELL SURVIVAL; COMPARATIVE STUDY; DOSE RESPONSE; DRUG COMBINATION; DRUG EFFECT; GENE EXPRESSION REGULATION; GENETICS; METABOLISM; PATHOLOGY; PROSTATE; SIGNAL TRANSDUCTION; SPRAGUE DAWLEY RAT; TISSUE CULTURE TECHNIQUE;

5-ALPHA REDUCTASE INHIBITORS; ANIMALS; APOPTOSIS; AROMATASE; BENZOPYRANS; CELL PROLIFERATION; CELL SURVIVAL; CELLS, CULTURED; DIHYDROTESTOSTERONE; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG THERAPY, COMBINATION; ESTRADIOL; ESTROGEN RECEPTOR ALPHA; ESTROGEN RECEPTOR BETA; FINASTERIDE; GENE EXPRESSION REGULATION; HUMANS; MALE; PIPERIDINES; PROSTATE; PROSTATIC HYPERPLASIA; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, ANDROGEN; RNA, MESSENGER; SELECTIVE ESTROGEN RECEPTOR MODULATORS; SIGNAL TRANSDUCTION; STROMAL CELLS; TAMOXIFEN; TESTOSTERONE; TISSUE CULTURE TECHNIQUES;

EID: 84861479395     PISSN: 01676997     EISSN: 15730646     Source Type: Journal    
DOI: 10.1007/s10637-010-9620-2     Document Type: Article

References (57)

1. Rosen RC, Wei JT, Althof SE, Seftel AD, Miner M, Perelman MA (2009) Association of sexual dysfunction with lower urinary tract symptoms of BPH and BPH medical therapies: results from the BPH Registry. Urology 73:562-566
2. Greco KA, McVary KT (2008) The role of combination medical therapy in benign prostatic hyperplasia. Int J Impot Res 20 (Suppl3):S33-S43
3. Tacklind J, Fink HA, MacDonald R, Rutks I, Wilt TJ (2010) Finasteride for benign prostatic hyperplasia. Cochrane Database of Systematic Reviews, Issue10. Art. No.:CD006015. doi:10.1002/14651858.CD006015.pub3
4. Li J, Tripathi RC, Tripathi BJ (2008) Drug-induced ocular disorders. Drug Saf 31:127-141
5. Weihua Z, Lathe R, Warner M, Gustafsson JA (2002) An endocrine pathway in the prostate, ERbeta, AR, 5alpha-androstane-3beta, 17beta-diol, and CYP7B1, regulates prostate growth. Proc Natl Acad Sci U S A 99:13589-13594
6. Lee DK, Chang C (2003) Endocrine mechanisms of disease: Expression and degradation of androgen receptor: mechanism and clinical implication. J Clin Endocrinol Metab 88:4043-4054
7. Harkonen PL, Makela SI (2004) Role of estrogens in development of prostate cancer. J Steroid Biochem Mol Biol 92:297-305
8. Johnson JJ, Syed DN, Suh Y, Heren CR, Saleem M, Siddiqui IA, Mukhtar H (2010) Disruption of androgen and estrogen receptor activity in prostate cancer by a novel dietary diterpene carnosol: implications for chemoprevention. Cancer Prev Res (Phila) 3:1112-1123
9. Glienke W, Dolgova Y, Muller I, Grosch S, Binder J, Geisslinger G, Jonas D (2004) Induction of apoptosis in human prostate stromal cells by 4-hydroxytamoxifen: an alternative therapy for benign prostate hyperplasia. World J Urol 22:452-456
10. Huang YW, Wang LS, Chang HL, Ye W, Shu S, Sugimoto Y, Lin YC (2006) Effect of keratinocyte growth factor on cell viability in primary cultured human prostate cancer stromal cells. J Steroid Biochem Mol Biol 100:24-33
11. Hirsimaki P, Aaltonen A, Mäntyla E (2002) Toxicity of antiestrogens. Breast J 8:92-96
12. Santeufemia DA, Capobianco G, Dessole S, Tolu F, Fadda GM, Di Meglio G, Farris A (2009) Tamoxifen induced severe hypertriglyceridemia in a male patient with breast carcinoma. Breast J 15:675-676
13. Chen HY, Dykstra KD, Birzin ET, Frisch K, Chan W, Yang YT, Mosley RT, DiNinno F, Rohrer SP, Schaeffer JM, Hammond ML (2004) Estrogen receptor ligands. Part 1: The discovery of flavanoids with subtype selectivity. Bioorg Med Chem Lett 14:1417-1421
14. Brössner C, Petritsch K, Fink K, Auprich M, Madersbacher S, Adlercreutz H, Rehak P, Petritsch P (2004) Phytoestrogen tissue levels in benign prostatic hyperplasia and prostate cancer and their association with prostatic diseases. Urology 64:707-711
15. Hong SJ, Kim SI, Kwon SM, Lee JR, Chung BC, Yonsei (2002) Comparative study of concentration of isoflavones and lignans in plasma and prostatic tissues of normal control and benign prostatic hyperplasia. Med J 43:236-241
16. Griffiths K, Denis L, Turkes A, Morton MS, Baillieres (1998) Phytoestrogens and diseases of the prostate gland. Clin Endocrinol Metab 12:625-647
17. Denis L, Morton MS, Griffiths K (1999) Diet and its preventive role in prostatic disease. Eur Urol 35:377-387
18. Royuela M, de Miguel MP, Bethencourt FR, Sanchez-Chapado M, Fraile B, Arenas MI, Paniagua R (2001) Estrogen receptors alpha and beta in the normal, hyperplastic and carcinomatous human prostate. J Endocrinol 168:447-454
19. McPherson SJ, Ellem SJ, Simpson ER, Patchev V, Fritzemeier KH, Risbridger GP (2007) Essential role for estrogen receptor beta in stromal-epithelial regulation of prostatic hyperplasia. Endocrinology 148:566-574
20. Norman BH, Dodge JA, Richardson TI, Borromeo PS, Lugar CW, Jones SA, Chen K, Wang Y, Durst GL, Barr RJ, Montrose-Rafizadeh C, Osborne HE, Amos RM, Guo S, Boodhoo A, Krishnan V (2006) Benzopyrans are selective estrogen receptor beta agonists with novel activity in models of benign prostatic hyperplasia. J Med Chem 49:6155-6157
21. Richardson TI, Norman BH, Lugar CW, Jones SA, Wang Y, Durbin JD, Krishnan V, Dodge JA (2007) Benzopyrans as selective estrogen receptor beta agonists (SERBAs). Part 2: structure-activity relationship studies on the benzopyran scaffold. Bioorg Med Chem Lett 17:3570-3574
22. Saeed A, Sharma AP, Durani N, Jain R, Durani S, Kapil RS (1990) Structure-activity relationship of antiestrogens. Studies on 2, 3-diaryl-1-benzopyrans. J Med Chem 33:3210-3216
23. Sharma AP, Saeed A, Durani S, Kapil RS (1990) Structure-activity relationship of antiestrogens. Effect of the side chain and its position on the activity of 2, 3-diaryl-2 H-1-benzopyrans. J Med Chem 33:3216-3222
24. Sharma AP, Saeed A, Durani S, Kapil RS (1990) Structure-activity relationship of antiestrogens. Phenolic analogues of 2, 3-diaryl-2 H-1-benzopyrans. J Med Chem 33:3222-3229
25. Singh MM (2001) Centchroman, a selective estrogen receptor modulator, as a contraceptive and for the management of hormone-related clinical disorders. Med Res Rev 21:302-347
26. Padayatty SJ, Marcelli M, Shao TC, Cunningham GR (1997) Lovastatin-induced apoptosis in prostate stromal cells. J Clin Endocrinol Metab 82:1434-1439
27. Le Tortorec A, Satie AP, Denis H, Rioux-Leclercq N, Havard L, Ruffault A, Jegou B, Dejucq-Rainsford N (2008) Human prostate supports more efficient replication of HIV-1 R5 than X4 strains ex vivo. Retrovirology 5:119
28. Gao W, Kearbey JD, Nair VA, Chung K, Parlow AF, Miller DD, Dalton JT (2004) Comparison of the pharmacological effects of a novel selective androgen receptor modulator, the 5alpha-reductase inhibitor finasteride, and the antiandrogen hydroxyflutamide in intact rats: new approach for benign prostate hyperplasia. Endocrinology 145(12):5420-5428
29. Fitts JM, Klein RM, Powers CA (2004) Comparison of tamoxifen and testosterone propionate in male rats: differential prevention of orchidectomy effects on sex organs, bone mass, growth, and the growth hormone-IGF-I axis. J Androl 25(4):523-534
30. Weihua Z, Lathe R, Warner M, Gustafsson JA (2002) An endocrine pathway in the prostate, ERbeta, AR, 5alpha-androstane-3beta, 17beta-diol, and CYP7B1, regulates prostate growth. Proc Natl Acad Sci USA 99:13589-13594
31. Kuiper GG, Enmark E, Pelto-Huikko M, Nilsson S, Gustafsson JA (1996) Cloning of a novel receptor expressed in rat prostate and ovary. Proc Natl Acad Sci USA 93:5925-5930
32. Dhar JD, Dwivedi A, Srivastava A, Setty BS (1994) Structure activity relationship of some 2, 3-diaryl-2 H-1-benzopyrans to their anti-implantation, estrogenic and antiestrogenic activities in rat. Contraception 49:609-616
33. Trukhacheva E, Lin Z, Reierstad S, Cheng YH, Milad M, Bulun SE (2009) Estrogen receptor (ER) beta regulates ERalpha expression in stromal cells derived from ovarian endometriosis. J Clin Endocrinol Metab 94(2):615-622
34. Steiner MS, Pound CR (2003) Phase IIA clinical trial to test the efficacy and safety of Toremifene in men with high-grade prostatic intraepithelial neoplasia. Clin Prostate Cancer 2:24-31
35. Price D, Stein B, Sieber P, Tutrone R, Bailen J, Goluboff E, Burzon D, Bostwick D, Steiner M (2006) Toremifene for the prevention of prostate cancer in men with high grade prostatic intraepithelial neoplasia: results of a double-blind, placebo controlled, phase IIB clinical trial. J Urol 176:965-970
36. Mobbs BG, Johnson IE, Connolly JG, Thompson J (1983) Concentration and cellular distribution of androgen receptor in human prostatic neoplasia: can estrogen treatment increase androgen receptor content? J Steroid Biochem 19:1279-1290
37. Blanchere M, Berthaut I, Portois MC, Mestayer C, Mowszowicz I (1998) Hormonal regulation of the androgen receptor expression in human prostatic cells in culture. J Steroid Biochem Mol Biol 66:319-326
38. McPherson SJ, Ellem SJ, Risbridger GP (2008) Estrogenregulated development and differentiation of the prostate. Differentiation 76:660-670
39. Ricke WA, McPherson SJ, Bianco JJ, Cunha GR, Wang Y, Risbridger GP (2008) Prostatic hormonal carcinogenesis is mediated by in situ estrogen production and estrogen receptor alpha signaling. Faseb J 22:1512-1520
40. Montanaro D, Maggiolini M, Recchia AG, Sirianni R, Aquila S, Barzon L, Fallo F, Andò S, Pezzi V (2005) Antiestrogens upregulate estrogen receptor beta expression and inhibit adrenocortical H295R cell proliferation. J Mol Endocrinol 35:245-256
41. Stettner M, Kaulfuss S, Burfeind P, Schweyer S, Strauss A, Ringert RH, Thelen P (2007) The relevance of estrogen receptorbeta expression to the antiproliferative effects observed with histone deacetylase inhibitors and phytoestrogens in prostate cancer treatment. Mol Cancer Ther 6:2626-2633
42. Brolin J, Skoog L, Ekman P (1992) Immunohistochemistry and biochemistry in detection of androgen, progesterone, and estrogen receptors in benign and malignant human prostatic tissue. Prostate 20:281-295
43. Horwitz KB, Jackson TA, Bain DL, Richer JK, Takimoto GS, Tung L (1996) Nuclear receptor coactivators and corepressors. Mol Endocrinol 10:1167-1177
44. Ho CK, Nanda J, Chapman KE, Habib FK (2008) Oestrogen and benign prostatic hyperplasia: effects on stromal cell proliferation and local formation from androgen. J Endocrinol 197:483-491
45. Soulitzis N, Karyotis I, Delakas D, Spandidos DA (2006) Expression analysis of peptide growth factors VEGF, FGF2, TGFB1, EGF and IGF1 in prostate cancer and benign prostatic hyperplasia. Int J Oncol 29:305-314
46. Rana S, Sen R, Kalra R, Arora B, Sharma P, Gahlawat S (2006) Immunohistochemical study of the expression of epidermal growth factor receptor in benign prostatic hypertrophy, prostatic intraepithelial neoplasia and prostatic carcinoma. Indian J Pathol Microbiol 49:495-499
47. de Miguel MP, Royuela M, Bethencourt FR, Santamaria L, Fraile B, Paniagua R (2000) Immunoexpression of tumour necrosis factor-alpha and its receptors 1 and 2 correlates with proliferation/apoptosis equilibrium in normal, hyperplasic and carcinomatous human prostate. Cytokine 12:535-538
48. Li Z, Habuchi T, Tsuchiya N, Mitsumori K, Wang L, Ohyama C, Sato K, Kamoto T, Ogawa O, Kato T (2004) Increased risk of prostate cancer and benign prostatic hyperplasia associated with transforming growth factor-beta 1 gene polymorphism at codon10. Carcinogenesis 25:237-240
49. Fleisch MC, Maxwell CA, Barcellos-Hoff MH (2006) The pleiotropic roles of transforming growth factor beta in homeostasis and carcinogenesis of endocrine organs. Endocr Relat Cancer 13:379-400
50. Symes JC, Kurin M, Fleshner NE, Medin JA (2008) Fas-mediated killing of primary prostate cancer cells is increased by mitoxantrone and docetaxel. Mol Cancer Ther 7:3018-3028
51. King KJ, Nicholson HD, Assinder SJ (2005) Effect of increasing ratio of estrogen:androgen on proliferation of normal human prostate stromal and epithelial cells, and the malignant cell line LNCaP. Prostate 66:105-114
52. Shibata Y, Ito K, Suzuki K, Nakano K, Fukabori Y, Suzuki R, Kawabe Y, Honma S, Yamanaka H (2000) Changes in the endocrine environment of the human prostate transition zone with aging: Simultaneous quantitative analysis of prostatic sex steroids and comparison with human prostatic histological composition. Prostate 42:45-55
53. Banerjee PP, Banerjee S, Lai JM, Strandberg JD, Zirkin BR, Brown TR (1998) Age-dependent and lobe-specific spontaneous hyperplasia in the brown Norway rat prostate. Biol Reprod 59:1163-1170
54. Habenicht UF, Tunn UW, Senge T, Schröder FH, Schweikert HU, Bartsch G, El Etreby MF (1993) Management of benign prostatic hyperplasia with particular emphasis on aromatase inhibitors. J Steroid Biochem Mol Biol 44:557-563
55. Benign Prostatic Hyperplasia (BPH) Management in Primary Care - Screening and Therapy, Final Report 2007, available at http://www.hsrd.research.va.gov/ publications/esp/BPH-2007.pdf
56. Nomura H, Kawashima H, Masaki S, Hosono TY, Matsumura K, Tamada S, Tanaka T, Nakatani T (2009) Effect of selective estrogen receptor modulators on cell proliferation and estrogen receptor activities in normal human prostate stromal and epithelial cells. Prostate Cancer Prostatic Dis 12:375-381
57. Steiner MS, Raghow S (2003) Antiestrogens and selective estrogen receptor modulators reduce prostate cancer risk. World J Urol 21:31-36