Phytoserm

PhytoSERM ("phyto" = plant, "SERM" = selective estrogen receptor modulator) is the medical term used to describe botanically derived substances that have been scientificaly proven to possess SERM qualities [cite journal |author=Boudes P, Bailly G |title= [Endocrinolgy of estrogens: some recent developments and future applications] |language=French |journal=Therapie |volume=55 |issue=2 |pages=237–47 |year=2000 |pmid=10967695 |doi= |url=] , similar to synthetically manufactured drugs of the same category.

Mechanism of action

Similarly to SERMs, phyto-SERMs act on the estrogen receptor in a selective manner, either as agonists, or as antagonists, thereby granting the possibility to selectively stimulate or inhibit estrogen-like responses in different tissues. The molecular basis for this discrimination lies in the variability of transcription coregulators in different tissues which interact with the estrogen receptor.cite journal | author = Dutertre M, Smith CL | title = Molecular mechanisms of selective estrogen receptor modulator (SERM) action | journal = J. Pharmacol. Exp. Ther. | volume = 295 | issue = 2 | pages = 431–7 | year = 2000 | month = November | pmid = 11046073 | doi = | url = http://jpet.aspetjournals.org/cgi/content/abstract/295/2/431 | issn = ] Furthermore many phytoestrogen (including phyto-SERMs) appear to be somewhat selective in binding for the estrogen receptor beta (ERβ) compared to the estrogen receptor alpha (ERα) paralog.cite journal | author = An J, Tzagarakis-Foster C, Scharschmidt TC, Lomri N, Leitman DC | title = Estrogen receptor beta-selective transcriptional activity and recruitment of coregulators by phytoestrogens | journal = J. Biol. Chem. | volume = 276 | issue = 21 | pages = 17808–14 | year = 2001 | month = May | pmid = 11279159 | doi = 10.1074/jbc.M100953200 | url = | issn = ] cite journal | author = Chang EC, Charn TH, Park SH, Helferich WG, Komm B, Katzenellenbogen JA, Katzenellenbogen BS | title = Estrogen Receptors alpha and beta as determinants of gene expression: influence of ligand, dose, and chromatin binding | journal = Mol. Endocrinol. | volume = 22 | issue = 5 | pages = 1032–43 | year = 2008 | month = May | pmid = 18258689 | doi = 10.1210/me.2007-0356 | url = | issn = ] These two forms of the estrogen receptor display somewhat different tissue distributionscite journal | author = Couse JF, Lindzey J, Grandien K, Gustafsson JA, Korach KS | title = Tissue distribution and quantitative analysis of estrogen receptor-alpha (ERalpha) and estrogen receptor-beta (ERbeta) messenger ribonucleic acid in the wild-type and ERalpha-knockout mouse | journal = Endocrinology | volume = 138 | issue = 11 | pages = 4613–21 | year = 1997 | month = November | pmid = 9348186 | doi = 10.1210/en.138.11.4613 | url = | issn = ] and regulate a partially-overlapping set of genes.cite journal | author = Hurst AG, Goad DW, Mohan M, Malayer JR | title = Independent downstream gene expression profiles in the presence of estrogen receptor alpha or beta | journal = Biol. Reprod. | volume = 71 | issue = 4 | pages = 1252–61 | year = 2004 | month = October | pmid = 15201200 | doi = 10.1095/biolreprod.104.029421 | url = | issn = ] cite journal | author = Kian Tee M, Rogatsky I, Tzagarakis-Foster C, Cvoro A, An J, Christy RJ, Yamamoto KR, Leitman DC | title = Estradiol and selective estrogen receptor modulators differentially regulate target genes with estrogen receptors alpha and beta | journal = Mol. Biol. Cell | volume = 15 | issue = 3 | pages = 1262–72 | year = 2004 | month = March | pmid = 14699072 | pmc = 363122 | doi = 10.1091/mbc.E03-06-0360 | url = | issn = ]

PhytoSERMs' unique mechanism of action, being able to target specific tissues precisely while unaffecting others, may make them safer candidates for treatment of estrogen deficiencies.

Category members

*Femarelle (DT56a) - a phytoSERM used for the treatment of menopause symptoms and bone health [cite journal |author=Somjen D, Katzburg S, Knoll E, "et al" |title=DT56a (Femarelle): a natural selective estrogen receptor modulator (SERM) |journal=J. Steroid Biochem. Mol. Biol. |volume=104 |issue=3-5 |pages=252–8 |year=2007 |month=May |pmid=17428655 |doi=10.1016/j.jsbmb.2007.03.004 |url=]

Indications

PhytoSERMs are suitable for treating estrogen defficiencies that cause menopause symptoms, osteopenia and osteoporosis.

References

Also See

*Selective estrogen receptor modulator
*Femarelle (DT56a), [http://www.femarelle.com Femarelle web site]
*Phytoestrogen