Coumestrol, a phytoestrogen in
the class of coumestans, belonging to the group of Flavonoids
(polyphenols) found abundantly in red clover, alfalfa sprouts, soy,
peas, brussels sprouts, etc.
Health Benefits
1. Intestinal alkaline phosphatase activity
In the clarification of the effects of coumestrol administration on Ca metabolism during pregnancy and in lactating mice, found that coumestrol did not affect serum Ca and the expression of vitamin D receptor protein in the duodenum and jejunum. Thus, coumestrol
administration during pregnancy may decrease the mRNA expression of
IAP and the ALP activity in the intestine of the pre-delivery mice
through ERα, but coumestrol had little effect on intestinal ALP activity at 10 days after parturition, according to "Effects of coumestrol administration to pregnant and lactating mice on intestinal alkaline phosphatase activity" by Kirihata Y, Horiguchi Y, Ueda M, Sugimoto M, Ikeda S, Kume S.(1)
2. Cervical cancer
In
the evaluation of Endogenous estrogens dramatic and differential
effects on classical endocrine organ and proliferation, found that Using
human cervical cancer cells (HeLa cells) as a model, the effects of
representative xenoestrogens (Coumestrol-a
phytoestrogen, tetrachlorodioxin (TCDD)-a herbicide and DDT-a
pesticide) on proliferation, cell cycle, and apoptosis were examined.
These xenoestrogens and estrogen inhibited the proliferation of Hela
cells in a dose dependent manner from 20 to 120 nM suggesting, that
17-beta-estrtadiol and xenoestrogens induced cytotoxic effects. Coumestrol
produced accumulation of HeLa cells in G2/M phase, and subsequently
induced apoptosis. Similar effects were observed in estrogen treated
cells, according to "Estrogenic activity of coumestrol, DDT, and TCDD in human cervical cancer cells" by Ndebele K, Graham B, Tchounwou PB.(2)
3. Anti-inflammatory activities
In
the investigation of A new coumestan (solalyratin A, 1) and a novel
cyclic eight-membered α,β-unsaturated ketone (solalyratin B, 3),
together with three known compounds, puerariafuran (2), coumestrol
(4) and 9-hydroxy-2',2'-dimethylpyrano[5',6':2,3]-coumestan (5),
isolated from the whole plant of Solanum lyratum, found that in vitro,
compounds 1-5 showed anti-inflammatory activities, with IC(50) values in
the range 6.3-9.1 μM, according to "Solalyratins A and B, new anti-inflammatory metabolites from Solanum lyratum" by Zhang DW, Yang Y, Yao F, Yu QY, Dai SJ.(3)
4. Neuroprotective effects
In the investigation in vitro of protective effects of coumestrol on mice astrocytes, found that coumestrol
induced a modest but significant increase in viability of astrocytes,
while the viability of astrocytes was reduced following exposure to LPS
and amyloid-beta peptide. The addition of coumestrol
could reverse the toxic effect induced by LPS and amyloid-beta
peptide. Both the LPS and amyloid-beta peptide enhanced interleukin 1,
interleukin 6, and tumor necrosis factor-alpha synthesis and these
effects were inhibited by 10(-9)M coumestrol, according to "The protective effects of coumestrol against amyloid-beta peptide- and lipopolysaccharide-induced toxicity on mice astrocytes" by Liu MH, Tsuang FY, Sheu SY, Sun JS, Shih CM.(4)
5. Antiseizure effects
In
the investigation of the effects of 3alpha-diol (1 mg/kg, SC) and/or an
androgen receptor blocker (flutamide 10 mg, SC), 1 hour prior to
administration of pentylenetetrazol (85 mg/kg, IP), found that
selective estrogen receptor modulators that favor ERalpha (propyl
pyrazole triol, 17alpha-E(2)) or ERbeta (diarylpropionitrile, coumestrol,
3alpha-diol), or both (17beta-E(2)), were administered (0.1 mg/kg, SC)
to juvenile male rats 1 hour before pentylenetetrazol. Estrogens with
activity at ERbeta, but not those selective for ERalpha, produced
antiseizure effects. Actions at ERbeta may underlie some antiseizure
effects of T's metabolites, according to "Antiseizure effects of 3alpha-androstanediol and/or 17beta-estradiol may involve actions at estrogen receptor beta" by Frye CA, Ryan A, Rhodes M.(5)
6. Gastric cancer (GC)
In
the estimation the risk of gastric cancer (GC) in relation to the
individual and combined consumption of polyphenols and NOC precursors
(nitrate and nitrite), found that for the first time, a protective
effect for GC because of higher intake of cinnamic acids,
secoisolariciresinol and coumestrol,
and suggest that these polyphenols reduce GC risk through inhibition
of endogenous nitrosation. The main sources of these polyphenols were
pears, mangos and beans for cinnamic acids; beans, carrots and squash
for secoisolariciresinol and legumes for coumestrol, according to "Dietary intake of polyphenols, nitrate and nitrite and gastric cancer risk in Mexico City"
by Hernández-Ramírez RU, Galván-Portillo MV, Ward MH, Agudo A, González
CA, Oñate-Ocaña LF, Herrera-Goepfert R, Palma-Coca O, López-Carrillo
L.(6)
7. Pituitary tumor
In
the investigation of the activation of different nongenomic pathways,
and determine the involvement of mERalpha, with measurement the
prolactin (PRL) release by radio-immunoassay, MAPK activations (ERK1/2
and JNK1/2/3) via a quantitative plate immunoassay, and intracellular
[Ca2+] by Fura-2 fluorescence imaging in cells treated with E2 or four
different phytoestrogens (coumestrol,
daidzein, genistein, and trans-resveratrol), found that phytoestrogens
were much more potent in mediating these nongenomic responses
(activation of MAPKs, PRL release, and increased intracellular [Ca2+])
via mERalpha than was previously reported for genomic responses. The
unique non-monotonic dose responses and variant signaling patterns
caused by E2 and all tested phytoestrogens suggest that complex and
multiple signaling pathways or binding partners could be involved. By
activating these different nongenomic signaling pathways,
phytoestrogens could have significant physiological consequences for
pituitary cell functions, according to "Membrane estrogen receptor-alpha-mediated nongenomic actions of phytoestrogens in GH3/B6/F10 pituitary tumor cells" by Jeng YJ, Kochukov MY, Watson CS.(7)
8. Bone health
In the investigation of the effects of coumestrol on osteoblasts and osteoclasts, inducated that phytoestrogen coumestrol
has a direct enhancing effect on the proliferation and osteogenic
differentiation of bone marrow stromal cells, which would lead to
stimulation of bone formation, and it can also protect the whole
skeletal system by regulating OPG/RANKL expression, and these effects
may be mediated by ERalpha, according to "Coumestrol promotes proliferation and osteoblastic differentiation in rat bone marrow stromal cells" by Wu XT, Wang B, Wei JN.(8)
9. Ovarian apoptosis
In the examination of the increased apoptosis in the adult rat ovary after lactational exposure to coumestrol
(COU), a potent phytoestrogen. Lactating dams were gavaged at doses of
0.01, 0.1, 1, and 10 mg/kg COU during the lactation period and the
reproductive effects of female pups in young adults, found that Ovarian
weights were reduced significantly at 0.1 and 1.0 mg/kg COU. The
reduction in the ovarian weight occurred in parallel with an increase
in the apoptosis at PND 135-140. A marked dose-dependent increase in the
expressions of active caspase-3 and -7 was observed in ovarian
granulosa cells. Immunostaining for active caspase-3 and the TUNEL
staining of apoptotic cells were also increased in ovaries exposed to
COU in a dose-dependent manner, according to "Lactational coumestrol exposure increases ovarian apoptosis in adult rats" by Moon HJ, Seok JH, Kim SS, Rhee GS, Lee RD, Yang JY, Chae SY, Kim SH, Kim JY, Chung JY, Kim JM, Chung SY.(9)
10. Breast cancer
In the evaluation of the associations between dietary phytoestrogen (isoflavonoids, lignans, and coumestrol)
intake and risk of breast cancer and whether the ER/PR statuses of the
tumor influence this relationship, found that the effects of lignans or
isoflavonoids were independent of receptor status. However, intake of coumestrol
was associated with decreased risk of receptor negative tumors
(ER-PR-) but not positive tumors. The risk of ER-PR- tumors was
significantly lower (50%) in women with intermediate coumestrol intake compared with those who did not consume any, according to "Dietary phytoestrogens are not associated with risk of overall breast cancer but diets rich in coumestrol are inversely associated with risk of estrogen receptor and progesterone receptor negative breast tumors in Swedish women" by Hedelin M, Löf M, Olsson M, Adlercreutz H, Sandin S, Weiderpass E.(10)
11. Antimicrobial activity
in the determination of the effects of the isoflavonoids coumestrol,
genistein and daidzein isolated and identified by bioassay-guided
fractionation from the acetone extract of Erythrina crista galli young
twigs infected with Phomopsis sp, found that these compounds showed
antimicrobial activity against Bacillus brevis (MIC values 16.3, 64.8
and 137.8 microM, respectively), according to "Antimicrobial isoflavonoids from Erythrina crista galli infected with Phomopsis sp" by Redko F, Clavin ML, Weber D, Ranea F, Anke T, Martino V.(11)
12. Etc.
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Sources
(1) http://www.ncbi.nlm.nih.gov/pubmed/21031635
(2) http://www.ncbi.nlm.nih.gov/pubmed/20623010
(3) http://www.ncbi.nlm.nih.gov/pubmed/21898133
(4) http://www.ncbi.nlm.nih.gov/pubmed/21708076
(5) http://www.ncbi.nlm.nih.gov/pubmed/19854112
(6) http://www.ncbi.nlm.nih.gov/pubmed/19449378
(7) http://www.ncbi.nlm.nih.gov/pubmed/19400946
(8) http://www.ncbi.nlm.nih.gov/pubmed/19165772
(9) http://www.ncbi.nlm.nih.gov/pubmed/19165469
(10) http://www.ncbi.nlm.nih.gov/pubmed/18424605
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