那法瑞林埋植型长效制剂对大鼠子宫内膜异位的抑制作用

INHIBITORY EFFECTS OF DEPOT FORMULATION OF NAFARELIN ON EXPERIMENTAL ENDOMETRIOSIS IN RATS

研究那法瑞林埋植型长效制剂单次应用对大鼠子宫内膜异位的作用及作用机制。采用手术方法建立大鼠模型，血清雌二醇（E2）、孕酮（Pg）水平和异位内膜雌激素受体（ER）、孕激素受体（PR）分别用酶免疫和亲和组化一步法检测。结果：那法瑞林长效制剂对异位内膜的抑制率（70．4±25．1）％接近去势组；血清E2和Pg的周期性分泌高峰消失;子宫和卵巢萎缩退化，重量减轻；异位内膜ER和PR阳性率也显著降低。结论：那法瑞林长效制剂对大鼠子宫内膜异位有显著抑制作用，低甾体激素水平是其主要作用机制。

To study the effect of depot formulation of domestic nafarelin administrated single sc implant on experimental endomatriosis in rats and study the mechanisms of action.METHODS Endometriosis was surgically induced in SD rats. An enzyme immunassay was used to determine the serum concentrations of estradiol (E2) and progesterone (Pg). Estrogen and progesterone receptors (ER and PR) in ectopic endometrium were analyzed by affinity histochemistry assay.RESULTS Profound suppression of explant volumes occurred in nafarelin depot formulation-treated rats after 3 weeks treatment (P<0.01 vs controls), which comparable to that of castration. The peak concentrations of serum E2 and Pg in the estrous cycle were decreased significantly. Uterine and ovarian weights, the contents of ER and PR in explant were also reduced in treated rats.CONCLUSIONS A single administration of nafarelin depot formulation causes drastic atrophy and regrssion of endometriosis, reaching to a state of ' medical ovariectomy'; this action results from an complete block of pituitary-ovarian function.