Anti-estrogenic effect

Several potent anti-estrogens also have a potential to be used as 17/f-HSD inhibitors because some of them have a dual site of inhibitory action they block both the estrogen receptor (anti-estrogen effect) and estrogen formation (inhibitory effect on 17/f-HSD). Despite the complexity of a dually active agent, such inhibitors have interesting properties suitable for their potential use in the treatment of estrogen-sensitive diseases, but their potency and selectivity for 17/1-HSDl have to be improved [98]. 

Anti-estrogenic effect. Ethanol (95%) extract of the dried aerial parts, administered intragastric to rats at variable doses was inactive . Petroleum ether extract of the dried leaf, administered intraperitoneally to female rats at a dose equivalent to 10 mg/kg tetrahydrocannabinol (THC) on 11-21 days of age, was active . Antifertility effect. Petroleum ether extract of the entire plant, administered by gastric intubation to female mice at doses of 75 mg/kg and 150 mg/kg, was active. A dose of 3 mg/kg, produced weak activity ". Resin, administered by gastric intubation to male mice at variable dosage levels, was inactive . ... 

Anti-edema activity. Methanol extract of the root, applied externally to mice at a dose of 2 mg/ear, produced inhibition ratio of Anti-estrogenic effect. Ethanol (95%) extract of the dried seed, administered by gastric intubation of ovariectomized mice at a dose of 40 mg/kg daily for 3 days, produced weak activity° h Petroleum ether extract of the dried seed, at a dose of 10 mg/kg, was active° k... 

Anti-convulsant activity. Methanol (50%) extract of the dried leaf, administered to mice, was active vs leptazol-induced convulsions . Ethanol (70%) extract of the fresh leaf, administered intraperito-neally to mice of both sexes at variable doses, was active vs metrazole- and strychnine-induced convulsions . Anti-estrogenic effect. Aqueous extract of the dried leaf smoke, administered to female adults at a concentration of 25.0 pL/plate, was active on granulosa cells. Results significant atp < 0.001 level . 

Lim YC et al (2005) Endoxifen (4-hydroxy-N-desmethyl-tamoxifen) has anti-estrogenic effects in breast cancer cells with potency similar to 4-hydroxy-tamoxifen. Cancer Chemother Pharmacol 55 471 178... 

Vessey MP, Villard-Mackintosh L, Jacobs HS. Anti-estrogenic effect of cigarette smoking. NEnglJMed mi) 317, 769-70. 

Michnovicz JJ, Hershcopf RJ, Naganuma H, Bradlow HL, Fishman J. Increased 2-hydroxylation of estradiol as a possible mechanism for the anti-estrogenic effect of cigarette smokir. ... 

In mice experiments intraperitoneal administration of partially purified P-sitosterol fractions of the fruit extract showed significant estrogenic activity an anti-estrogenic effect has also been demonstrated. ... 

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