In vitro-assessment of putative antiprogestin activities of phytochemicals and synthetic UV absorbers in human endometrial Ishikawa cells

Abstract

Critical steps of embryo implantation are controlled by progesterone. These processes can be interrupted by progesterone receptor (PR) antagonists, e.g. drugs used for abortion. Antiprogestin effects induced by natural compounds and environmental chemicals have been rarely addressed. In our in vitro study, we investigated putative antiprogestin activities of the plant compounds apigenin (API) and trans-ferulic acid (t-FA) as well as the UV absorbers octyl methoxycinnamate (OMC) and 4-methylbenzylidene camphor (4-MBC). They were compared with the selective progesterone receptor modulators (SPRMs) mifepristone (RU486) and ulipristal acetate (UPA) as well as the full PR-antagonist ZK137316. Effects of test compounds in combination with progesterone on the progesterone-sensitive target gene estrogen sulfotransferase (SULT1E1) were characterized by sigmoidal concentration-response curves obtained by RT-qPCR. The agonistic effect of progesterone on SULT1E1 mRNA levels was concentration-dependently antagonized by RU486, UPA and ZK137316 as well as, with lower potency, apigenin. t-FA, OMC and 4-MBC had no effect on SULT1E1 mRNA levels. We demonstrated that apigenin, although at higher concentrations, exerts a similar effect as the well-characterized SPRMs RU486 and UPA or the progesterone antagonist ZK137316 in this model. Our endometrium-specific Ishikawa cell assay is a useful complement to artificial transactivation assays for the identification of environmental substances with antiprogestin activities.

Effects of letrozole in combination with low-dose intramuscularinjection of human menopausal gonadotropin on ovulation and pregnancy of 156 patients with polycystic ovary syndrome

“…At present, CC remains the first-line drug for ovulation induction, with ovulation rates of 75% to 80%,9 but recent studies have shown that a considerable proportion of patients did not get desirable pregnancy outcomes after CC treatment 10,11. In the normal ovulation process, estrogen and progesterone play obvious regulatory roles, and CC has anti-estrogenic effects, but its exact mechanism has not been fully clarified yet 12. It has previously been reported that13,14 the chemical structure of CC is similar to that of estrogen, so it is capable of binding estrogen receptor (ER) and then competitively occupying the hypothalamic ER to inhibit the negative feedback of endogenous estrogen to the hypothalamus.…”

Therapeutic effects of mifepristone combined withGestrinone on patients with endometriosis

“…The level up- and down-regulation of sex hormone receptors are associated with sex hormones and related cytokines. The endometrium, as the target tissue of estrogen and progesterone, has corresponding estrogen receptors (ERs) and progesterone receptor (PRs) 4. The ERα and ERβ levels of eutopic endometrium of normal women of childbearing age vary with the menstrual cycle, i.e.…”

The Inhibitory Effect of Carboplatin Injection on Human Neuroblastoma SK-N-SH

“…The absorbance at 570 and 600 nm were measured by microplate photometer. The viability of the cells was then calculated by using the formula in a previous study 25 . Viability of the cells=(ODtreated—ODblank/ODcontrol—ODblank)×100%.…”