RU-486 is an abortifacient which is used to terminate early pregnancy. It acts by blocking progesterone receptor. In our earlier study with progesterone, RU-486 was used as a progesterone receptor antagonist to find o...RU-486 is an abortifacient which is used to terminate early pregnancy. It acts by blocking progesterone receptor. In our earlier study with progesterone, RU-486 was used as a progesterone receptor antagonist to find out the mechanism of progesterone action on melanoma cells. Results indicated that the effect of progesterone was not mediated through progesterone receptor. In the course of experiments, it was observed that RU-486 by itself inhibited mouse melanoma cell growth. Further research work with RU-486 showed a dose dependent inhibition of human melanoma cell growth. The mechanism of inhibition of cell growth was due to apoptosis and this effect of RU-486 was neither mediated through progesterone receptor nor glucocorticoid receptor. This in-vitro study suggested that melanoma also could be a target for RU-486 action, apart from breast, ovary and prostate cancers.展开更多
Objective To study the effect of single and low dose of RU486 on endometrial receptivity of healthy women. Methods A total of 5 healthy women were followed for one control and one treatment cycle. In the treatment c...Objective To study the effect of single and low dose of RU486 on endometrial receptivity of healthy women. Methods A total of 5 healthy women were followed for one control and one treatment cycle. In the treatment cycle, a dose of 10 mg RU486 was administered on day luteinizing hormone (LH)-2. In both the control and treatment cycle, an endometrial biopsy was obtained on LH+7. These biopsies were assessed by immunohistochemical analysis to find the difference in expression of integrins and progesterone receptor (PR) between the control and treatment cycle. Results The treatment with RU486 increased the expression of α 1 and α 4 subunits of integrin in glandular epithelial cells, but did not influence β 3 subunit. Moreover, the normal down regulation of PR in epitherial cell nuclei was inhibited by 10 mg RU486. Conclusion Single dose of 10 mg RU486 impairs the establishment of endometrial receptivity on time.展开更多
Twenty-four healthy female volunteers with amenorrhea for seven weeks or less.asking for legal termination of pregnancy were recruited and divided into 4 groups (6 each). The subjects were orally administered with RU4...Twenty-four healthy female volunteers with amenorrhea for seven weeks or less.asking for legal termination of pregnancy were recruited and divided into 4 groups (6 each). The subjects were orally administered with RU486 of 50mg (Group Ⅰ). 50mg Q12hx 6 (GrouP Ⅱ),200mg(GrouP Ⅲ)or 600mg(Group Ⅳ).Vacuum aspiration(GrouP Ⅰ)or Methyl Carprost Suppository(PGOS 1.0mg)(GrouP Ⅱ-Ⅳ)was given 72h after the firsl dose followed by a 6--hour medl'cal survel'llance.Blood samples were collected on day 1-6,8,15,43 to measure the serum levels of β-hCG,E2,P,PRL,ACTH, Cortisol,T3,T4 and TSH in each subject.The results showed that no significant dose-effect relationship was observed in terms of clinical efficacy,vaginal bleeding or side effects.All four groups shared the same tendency of changes in serum levels of β-hCG,E2 and P.β-hCG levels increased by 50-100% (P<0.01)24h prior to treatment,and continued ic ipcrease following lreatment until the sac expulsion.EZ levels l'n each group reinal'ned higher than pre-treatment values with the gradual decline in P levels.β-hCG,E2 and P decreased drastically after abortion,levels of β-hCG,E2,P on day 5 were only 35-60% (P<0.01),32-46%(P<0.01)and 30-56%(P<0.01)of those on day 4 respectively.The mean PRL levels on day 2-4 in each group increased obviously but declined gradually following the sac ex.pulsion.During treatment,the respective cortisol levels increased dramatically,the average levels ofcortisol on day 2-4 were 30-40%(P<0.05) l'n GrouP Ⅰ-Ⅲ and 60%(P< 0.01) in Group Ⅳ higher as compared with day 1 values, while decreased rapidly af ter termination of pregnancy as indicated that cortisol levels on day 5 were only 67-81%(P<0.05) of those on day 4.The changes in ACTH,T3,T4,TSH levels were of no statistic sigulAance(P>0.05).This study indicated that RU486 has no dose-effect relationship when used for interruption of early pregnancy and its main action site seems neither in ovary nor in villi.It has some effects on pituitary-adrenal axis,especially in large dosage,however,it has no obvious impact on pituilary-thyroid axis.It seems that the changes in PRL serum levels were directly due to the drug itsed ifs clinical significance should be further studied.展开更多
文摘RU-486 is an abortifacient which is used to terminate early pregnancy. It acts by blocking progesterone receptor. In our earlier study with progesterone, RU-486 was used as a progesterone receptor antagonist to find out the mechanism of progesterone action on melanoma cells. Results indicated that the effect of progesterone was not mediated through progesterone receptor. In the course of experiments, it was observed that RU-486 by itself inhibited mouse melanoma cell growth. Further research work with RU-486 showed a dose dependent inhibition of human melanoma cell growth. The mechanism of inhibition of cell growth was due to apoptosis and this effect of RU-486 was neither mediated through progesterone receptor nor glucocorticoid receptor. This in-vitro study suggested that melanoma also could be a target for RU-486 action, apart from breast, ovary and prostate cancers.
文摘Objective To study the effect of single and low dose of RU486 on endometrial receptivity of healthy women. Methods A total of 5 healthy women were followed for one control and one treatment cycle. In the treatment cycle, a dose of 10 mg RU486 was administered on day luteinizing hormone (LH)-2. In both the control and treatment cycle, an endometrial biopsy was obtained on LH+7. These biopsies were assessed by immunohistochemical analysis to find the difference in expression of integrins and progesterone receptor (PR) between the control and treatment cycle. Results The treatment with RU486 increased the expression of α 1 and α 4 subunits of integrin in glandular epithelial cells, but did not influence β 3 subunit. Moreover, the normal down regulation of PR in epitherial cell nuclei was inhibited by 10 mg RU486. Conclusion Single dose of 10 mg RU486 impairs the establishment of endometrial receptivity on time.
文摘Twenty-four healthy female volunteers with amenorrhea for seven weeks or less.asking for legal termination of pregnancy were recruited and divided into 4 groups (6 each). The subjects were orally administered with RU486 of 50mg (Group Ⅰ). 50mg Q12hx 6 (GrouP Ⅱ),200mg(GrouP Ⅲ)or 600mg(Group Ⅳ).Vacuum aspiration(GrouP Ⅰ)or Methyl Carprost Suppository(PGOS 1.0mg)(GrouP Ⅱ-Ⅳ)was given 72h after the firsl dose followed by a 6--hour medl'cal survel'llance.Blood samples were collected on day 1-6,8,15,43 to measure the serum levels of β-hCG,E2,P,PRL,ACTH, Cortisol,T3,T4 and TSH in each subject.The results showed that no significant dose-effect relationship was observed in terms of clinical efficacy,vaginal bleeding or side effects.All four groups shared the same tendency of changes in serum levels of β-hCG,E2 and P.β-hCG levels increased by 50-100% (P<0.01)24h prior to treatment,and continued ic ipcrease following lreatment until the sac expulsion.EZ levels l'n each group reinal'ned higher than pre-treatment values with the gradual decline in P levels.β-hCG,E2 and P decreased drastically after abortion,levels of β-hCG,E2,P on day 5 were only 35-60% (P<0.01),32-46%(P<0.01)and 30-56%(P<0.01)of those on day 4 respectively.The mean PRL levels on day 2-4 in each group increased obviously but declined gradually following the sac ex.pulsion.During treatment,the respective cortisol levels increased dramatically,the average levels ofcortisol on day 2-4 were 30-40%(P<0.05) l'n GrouP Ⅰ-Ⅲ and 60%(P< 0.01) in Group Ⅳ higher as compared with day 1 values, while decreased rapidly af ter termination of pregnancy as indicated that cortisol levels on day 5 were only 67-81%(P<0.05) of those on day 4.The changes in ACTH,T3,T4,TSH levels were of no statistic sigulAance(P>0.05).This study indicated that RU486 has no dose-effect relationship when used for interruption of early pregnancy and its main action site seems neither in ovary nor in villi.It has some effects on pituitary-adrenal axis,especially in large dosage,however,it has no obvious impact on pituilary-thyroid axis.It seems that the changes in PRL serum levels were directly due to the drug itsed ifs clinical significance should be further studied.
