拟雌内酯

Coumestrol是大豆产品中存在的植物雌激素。对癌症,神经障碍和自身免疫疾病有潜在治疗活性。抑制ES2细胞增殖的IC50值为50 μM。

信号通路 >> 其他 >> 雌激素受体/ERR

研究领域 >> 癌症

天然产物 >> 苯丙酸类

IC50: 50 μM[1]

Coumestrol通过PI3K和ERK1/2MAPK途径发挥化学治疗作用。 Coumestrol抑制活力和侵袭,并诱导ES2(透明细胞/浆液性癌)细胞的凋亡。此外,免疫反应性PCNA和ERBB2(卵巢癌增殖的标志物)在它们在香豆雌酚诱导的ES2细胞死亡中的表达减弱。 AKT,p70S6K,ERK1/2,JNK1/2和p90RSK的磷酸化通过香豆雌酚治疗以剂量和时间依赖性方式灭活[1]。 Coumestrol抑制MCF-7细胞的增殖并诱导细胞凋亡,铜螯合剂新铜嘌呤和ROS清除剂可阻止MCF-7细胞的凋亡。 Coumestrol治疗诱导ROS生成,伴随DNA片段化,p53/p21上调,G1/S期细胞周期停滞,线粒体膜去极化和半胱天冬酶9/3激活[2]。

为了确定香豆雌酚的剂量依赖性作用，用不同浓度（0,1,10,20,50或100μM）的香豆雌酚处理ES2细胞[1]。将Coumestrol溶解在DMSO中以制备3mM原液。用递增浓度的香豆雌酚处理乳腺癌MCF-7细胞24,48和72小时。然后，每孔加入20μLMTT（5mg / mL）并再孵育3小时。将形成的Formazan蓝色晶体溶解在100μLDMSO中。使用ELISA平板读数器在570nm处读取吸光度[2]。

[1]. Lim W, et al. Coumestrol suppresses proliferation of ES2 human epithelial ovarian cancer cells. J Endocrinol. 2016 Mar;228(3):149-60.

[2]. Zafar A, et al. Cytotoxic activity of soy phytoestrogen coumestrol against human breast cancer MCF-7 cells: Insights into the molecular mechanism. Food Chem Toxicol. 2017 Jan;99:149-161.

Elacestrant dihydrochloride | AZD9496 | 山奈酚 | 3-[4-[[2,4-二(三氟甲基)苄基]氧基]-3-甲氧基苯基]-2-氰基-N-(5-三氟甲基-[1,3,4]噻二唑-2-基)丙烯酰胺 | 雌酚酮 | Brilanestrant | 20(S)-原人参三醇 | 27-羟基胆固醇 | 己烯雌酚 | PHTPP | 2,3-双(4-羟苯基)丙腈 | 雌马酚 | 胆固醇 | 白杨素 | Endoxifen Z-异构体盐酸盐

DATA ITEMS CITED :

8

MOLECULAR FORMULA :

C15-H8-O5

MOLECULAR WEIGHT :

268.23

WISWESSER LINE NOTATION :

T D6 B566 CO KVOJ FQ OQ

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :

TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :

Subcutaneous

DOSE :

2500 ug/kg

SEX/DURATION :

lactating female 1-5 day(s) post-birth

TOXIC EFFECTS :

Reproductive - Maternal Effects - uterus, cervix, vagina Reproductive - Maternal Effects - other effects Endocrine - estrogenic

TYPE OF TEST :

TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :

Oral

DOSE :

234 mg/kg

SEX/DURATION :

female 1-13 day(s) after conception

TOXIC EFFECTS :

Reproductive - Fertility - other measures of fertility

TYPE OF TEST :

TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :

Oral

DOSE :

35 gm/kg

SEX/DURATION :

female 14 day(s) pre-mating

TOXIC EFFECTS :

Reproductive - Maternal Effects - menstrual cycle changes or disorders Reproductive - Fertility - female fertility index (e.g. # females pregnant per # sperm positive females; # females pregnant per # females mated) Reproductive - Effects on Embryo or Fetus - other effects to embryo

TYPE OF TEST :

Unscheduled DNA synthesis

MUTATION DATA

TYPE OF TEST :

Mutation in mammalian somatic cells

TEST SYSTEM :

Rodent - hamster Lung

DOSE/DURATION :

10 umol/L

REFERENCE :

FCTOD7 Food and Chemical Toxicology. (Pergamon Press Inc., Maxwell House, Fairview Park, Elmsford, NY 10523) V.20- 1982- Volume(issue)/page/year: 35,605,1997