Abstract
Gestrinone (R 2323) is a synthetic progestogen, and noteworthy agent for endometriosis treatment. The effect of this reagent on cultured cells from porcine granulosa, human endometrial and endometrial carcinoma origin was investigated concerning their hormonal activities and cell proliferations. Also, the effect of gestrinone on the serum levels of gonadotropins and gonadal steroids in patients with XY gonadal dysgenesis (Swyer's syndrome) and uterine myoma was studied. The monolayer cell colony established from the endometrial tissue fragments was positively stained by PAS similar to the secretory phase endometrium by 10 ng/ml gestrinone in the culture media. Endometrial carcinoma cells from a 65-year-old patient were proliferated by gestrinone at the concentration of 50 ng/ml in the culture media. The effect of gestrinone on the secretions of progesterone and estradiol-17β with or without hCG/testosterone from the cultured porcine granulosa cells was also investigated. Progesterone secretions were stimulated at the 50 ng/ml concentration of gestrinone, especially in association with hCG. Nonetheless, at the concentration of 500 ng/ml, those were inhibited. The secretions of estradiol-17β were stimulated by this reagent both with and without testosterone in dosedependent manners. The effect of 25 mg gestrinone administration for 3 days on the levels of LH, FSH, progesterone and estradiol-17β in a patient with XY gonadal dysgenesis was as follows. Both LH and FSH Ievels gradually decreased, whereas estradiol-17β Ievel was increased. The same dosage of this reagent was administered to a patient with uterine myoma on her menstrual days 7, 8 and 9. All hormone levels were within normal ovulatory limits, and her ovulation was not interrupted. In conclusion, gestrinone was thought to act as a so-called mini-pill, via the hypothalamic-pituitary axis or directly to the ovaries and endometrium more in the fashion of pseudopregnancy drugs than danazol for endometriosis.
