Aim To determine the structure of the by-product produced in Grignard reaction for preparing mifepristone derivatives, and elucidate the reaction mechanism.Methods The structure of the by-product was determined with e...Aim To determine the structure of the by-product produced in Grignard reaction for preparing mifepristone derivatives, and elucidate the reaction mechanism.Methods The structure of the by-product was determined with elemental analysis, one- and two-dimension spectra NMR (DEPT, 1H-1Hcosy, HMQC, HMBC) and compared with those of mifepristone.Results The main by-product was 11,17-di-addition product of Grignard reagent of N, N-dimethylamino phenyl bromide.Conclusion This is the first complete assignment of 1H NMR and 13C NMR of compound (3).展开更多
Objective: To compare the clinical efficacy of Cassia Twig Tuckahoe capsule (Chinese Medicine) and Mifepristone combined with laparoscopic surgery for the treatment of endometriosis. Designs: Prospective cohort study....Objective: To compare the clinical efficacy of Cassia Twig Tuckahoe capsule (Chinese Medicine) and Mifepristone combined with laparoscopic surgery for the treatment of endometriosis. Designs: Prospective cohort study. Setting: Gynecology and Obstetrics Department, Jingzhou Central Hospital, affiliated to Yangtze University. Methods: We selected 67 patients suspected with endometriosis and divided randomly into 2 groups on patient choice. Outcome Measures: Treatment efficacy, side effects, recurrence rate and pregnancy rate. Results: Comparing the effect of treatment between the two groups, the success rate was almost same (P > 0.5). However, the disappearance of pain was faster in Cassia twig Tuckahoe group (P Conclusion: After analysis of the result, Cassia twig Tuckahoe capsule combined with Laparoscopy is superior to the Mifepristone combined with Laparoscopy. Cassia twig Tuckahoe capsule is a very propitious medicine for treating endometriosis for long term benefits.展开更多
Objective To compare the effects of 2 dosage-forms (granular and decoction) of Arnebia euchroma (royle) Johnst (Arnebia EJ in short below) on medical abortion with that of mifepristone combined with misoprostol Met...Objective To compare the effects of 2 dosage-forms (granular and decoction) of Arnebia euchroma (royle) Johnst (Arnebia EJ in short below) on medical abortion with that of mifepristone combined with misoprostol Methods Totally 648 women, who had pregnancy of 38-45 d and were willing to terminate pregnancy with mifepristone and misoprostol, were randomly divided into 3 groups, each of which was respectively given granular of Arnebia EJ, placebo granular, or decoction of Arnebia EJ besides mifepristone and misoprostol. The abortion results, bleeding duration, menstruation recovery and side-effects were observed. Results Neither complete abortion rates nor average bleeding durations of the granular group and the decoction group were significantly different (P>0.05). The complete abortion rate and bleeding duration of the two groups were respectively higher and shorter than those of the placebo group (P<0.05). However, the menstruation recov- ery was not significantly different among the three groups (P>0.05). The decoction of Arnebia EJ caused significantly more nausea and vomiting than the other groups (P<0.05). Conclusion The granular form did not have the odor of Arnebia EJ, and caused much less nausea and vomiting compared with the decoction form. The granular and decoc- tion forms were equally effective in improving the results of medical abortion. There- fore it is necessary to conduct further studies on the granular form of Arnebia EJ.展开更多
Objective To investigate effects of mifepristone (MP) on the development and ultrastructure of mouse blastocysts in vivo Methods Sixty female mice were equally divided into 4 groups: control group (group A), 1.9 ...Objective To investigate effects of mifepristone (MP) on the development and ultrastructure of mouse blastocysts in vivo Methods Sixty female mice were equally divided into 4 groups: control group (group A), 1.9 mg/kg MP group (group B), 5.6 mg/kg MP group (group C), and 16.8 mg/kg MP group (group D). The female mice of 4 groups undertook a superovulation method. The development of obtained blastocysts was evaluated, and ultrastructural changes of the blastocysts were observed by transmission electron microscope. Results In comparison with group A, the development rate of blastocysts in group B showed no difference (P〉0.05), while the development rate of blastocysts in both group C and group D was significantly lower (P〈0.05). With doses of 5.6 mg/kg and 16.8 mg/kg, the blastocysts showed granular appearance of the cytoplasm, irregular cell borders, enlarged perivitelline space and degeneration. Ultrastructure of the blastocysts in group B was similar to group A, except a little number of fat droplets in the cytoplasm. In group C, the microvilli on apical surface was decreased in number or even disappeared, mitochondria were under developed, a lot of filamentous crystals were found in the cytoplasm. Cellular junctions were defected. In group D, the blastocyst cells were irregular in shape, mitochondria were frequently vacuolated, the nucleolus was enlarged, nuclear membrane was ruptured, and chromatin was slack. Conclusion MP could damage to the ultrastructure of mouse blastocyst, and was responsible for the inhibition of blastocyst development. The inhibitory effect of MP would be in a dose-dependent fashion.展开更多
Objective: To compare the efficacy and side effects of levonorgestrel and low dose mifepristone in emergency contraception. Method: The study is a randomized double--blind multicenter comparative trial. A total of 1, ...Objective: To compare the efficacy and side effects of levonorgestrel and low dose mifepristone in emergency contraception. Method: The study is a randomized double--blind multicenter comparative trial. A total of 1, 276 women with unprotected intercourse within 72 hours were allocated to one of the two study groups. In the levonorgestrel (LNG) group, 0. 75 mg LNG was taken twice, 12 hours apart, whereas in the mifepristone (Mife) group, a single dose of 10 mg mifepristone was taken and a placebo 12 hours after. Follow--up visit was paid on the seventh day of the expected next menstruation to evaluate the contraceptive efficacy and side effects. Contraceptive efficacy was calculated by Dixon’s method. Result:In the LNG group 20 pregnancies occurred among 643 women, while in the Mife group 9 pregnancies occurred among 633 women. The pregnancy rates were 3. 10% and 1. 43% respectively. Contraceptive efficacy rate of preventing pregnancy was 59. 16% and 79. 73%, the difference was statistically significant (P<O. 05). The incidence of various side effects, which were mild, was less than 10%. There was no statistical difference between the two groups. The percentage of subjects who had their next menstruation 3 days earlier or later than their expected menstruation in LNG group and Mife group was 77. 7% and 78. 5% respectively. Conclusion: Use of levonorgestrel or low dose mifepristone for emergency contraception is effective and safe.展开更多
Objective To investigate the role of mifepristone in regulating cytokines of materno-fetal interface and serum of human early gestationMethods Thirty-five women with early pregnancy received mifepristone 50 mg orallyo...Objective To investigate the role of mifepristone in regulating cytokines of materno-fetal interface and serum of human early gestationMethods Thirty-five women with early pregnancy received mifepristone 50 mg orallyon study d 1 and d 2, respectively, followed by undergoing artificial abortion to getdecidua and villi on study d 3. Twenty-five women with early pregnancy withoutmifepristone administration as control also underwent artificial abortion to get de-cidua and villi. The expressions of TGF-β1 and TGF-β1 receptor mRNA in the earlydecidua and villi were assessed by using RT-PCR . The concentrations of serum TNF-α were measured by radioimmunoassay.Results The decidual expressions of TGF- β1 mRNA and TGF-β1 receptor mRNA in thetreated group were significantly lower than those of the control (P<0.05), while thevillus expressions of TGF-β1 and TGF-β1 receptor mRNA in the treated group were notsignificantly different from those of the control (P>0.05). The serum TNF-β1 levelselevated significantly after mifepristone treatment.Conclusion The antigestational effect of mifepristone might act through suppressingthe transcription of TGF-β1 and TGF-β1 receptor in the decidua and increasing theserum TNF-α level, which interfered in the materno-fetal interface Th2 bias.展开更多
Objective To investigate the efficacy, safety and acceptability of mifepristone combined with misoprostol used for late luteal fertility regulationMaterials & Methods Sixty-one female volunteers were recruited and...Objective To investigate the efficacy, safety and acceptability of mifepristone combined with misoprostol used for late luteal fertility regulationMaterials & Methods Sixty-one female volunteers were recruited and there were 261 treatment cycles in total. Subjects were planned to receive treatment with 25 mg of mifepristone, Q12 h × 4 orally for five days prior to expected menstruation followed by 400 μg of misoprostol 48 h later for up to six cycles.Results There were 13 pregnancies in the 267 treatment cycles and among them complete abortion and continuing pregnancy occurred in 7 and 6 cycles respectively. So the overall pregnancy rate was 4. 87% (13/267) and the rate of continuing pregnancy was 2. 25% (6/267) , while the failure rate per pregnant cycle was 46. 15% (6/13). In treatment cycles the vaginal bleeding patterns changed insignificantly as compared with those in control cycles.Conclusion The efficacy, compliance and acceptability of the regimen should be further improved when it was administered for late luteal fertility regulation.展开更多
To inverstgate the safety, effectiveness and acceptability Of conbination Of mifepristone and misoproslol for termination of high-risk pregnancy (amenorrhea≤ 70 days ).Three hundred and eighty-eight high-risk pregnan...To inverstgate the safety, effectiveness and acceptability Of conbination Of mifepristone and misoproslol for termination of high-risk pregnancy (amenorrhea≤ 70 days ).Three hundred and eighty-eight high-risk pregnant women, complicated with scarreduterus, or reproductive tract malformation, or uterus fibromyoma, or histories of recentabortion or repeated abortions, or pregnancy during lactation, and having duration of gestation ranging from 34 to 69 days, were administered orally 150 mg mifepristone (50 mgat the first time, and then 25 mg q 12 h × 4), and 600 μg misoprostol on the third day.The complete abortion rate ωas 92. 3%, while the incomplete abortion rate was 6. 2%, ongoing and pregnancy rate was 1. 5%. It was shown that combination of mifepristone andmisoprostol was effective in inducing abortion Of those high-risk pregnancies. Theregimen's effectiveness for high-risk population was similar to that for general population. Its safety, effectiveness and acceptability were satifactory. In addition, the softenedand dilated cervix made it easier and less painful to make vacuum aspiration in case offailure of the abortion.展开更多
Objective To investigate telomerase activity in chorion and decidua from abortion induced by mifepristone incorporated with misoprostol at early pregnancy. Methods TRAP-SYBR Green assay was used to detect the expressi...Objective To investigate telomerase activity in chorion and decidua from abortion induced by mifepristone incorporated with misoprostol at early pregnancy. Methods TRAP-SYBR Green assay was used to detect the expression of telomerase. Forty specimen were obtained from medicinal abortion (experiment group) and forty were from normal induced abortion (control group). Results Positive expression of chorion telomerase was significantly different between the experimental group (28%, 11/40) and the control group (73%, 29/40) (P〈0.05). While in decidua, the positive rate was 28% (11/40) in the experimental group and 20% (9/40) in the control group, there was no significant difference (P〉0.05). Conclusion It is suggested that miferistone may significantly decrease the telomerase activity in chorion but not in decidua.展开更多
Objective To investigate the efficacy and safety in women after caesarian section for termination of early pregnancies by treatment, or repeated treatment with mifepristone and misoprostol. Subjects and Methods A t...Objective To investigate the efficacy and safety in women after caesarian section for termination of early pregnancies by treatment, or repeated treatment with mifepristone and misoprostol. Subjects and Methods A total of 213 pregnant women with amenorrhea of 34~69 d after caesarian section who asked for medical abortion were recruited, including 63 cases undergoing their second medical abortion. A total amount of mifeprisstone of 150 mg given in separate doses (25 mg×4 and 50 mg at the first time) was administered orally within 3 d, followed by misoprostol of 0.6 mg orally in the morning of d 3. Results The complete abortion rate was 92.5%, incomplete abortion was 4.7% and failure was 2.8%. Conclusion The sequential use of mifepristone and misoprostol could be successfully and repeatedly used for induced abortion in those women with a caesarian section history. Its efficacy was similar to that for ordinary population. Its safety and effectiveness were satisfactory.展开更多
Objective To explore the effects of mifepristone on the growth of human gastric cancer cell line MKN-45 and its possible mechanisms. Methods In situ hybridization was used to detect the expression of progesterone rece...Objective To explore the effects of mifepristone on the growth of human gastric cancer cell line MKN-45 and its possible mechanisms. Methods In situ hybridization was used to detect the expression of progesterone receptor (PR) mRNA in MKN-45 cells. Proliferation, cell cycle distribution, and the expression of Bcl-xL and vascular endothelial growth factor (VEGF) of MKN-45 cells incubated with various concentrations of mifepristone (1, 5, 10, and 20 μmol/L) were analyzed using MTT reduction assay, flow cytometry, reverse transcription-polymerase chain reaction (RT-PCR), and enzyme-linked immunoab-sorbent assay (ELISA), respectively. After transplantation of MKN-45 cells underneath the skin of athymic mice, mifepristone was administrated with the dose of 50 mg/(kg·d) for 6 weeks to evaluate the tumor growth. Apoptosis and the expression of proliferating cell nuclear antigen (PCNA) in xenografted tumors were detected using transmission electron microscopy and immunohistochemical staining, respectively. Results PR mRNA was highly expressed in cultured MKN-45 cell. Mifepristone dose-dependently inhibited the pr-oliferation of MKN-45 cells, and the inhibitory rate was dramatically increased from 7.21% to 47.23%. The inhibitory effect was accompanied by a dose-dependent increase in the percentage of cells in G 0 /G 1 phase, and with a concurrent decrease in the proportion of S- and G 2 /M-phase cells and the proliferative index from 57.65% to 24.54%. Meanwhile, mifepristone down-regulated the expression of Bcl-xL and VEGF in a dose-dependent manner. In vivo, mifepristone effectively inhibited the growth of xenografted tumors in nude mice (55.14% for inhibitory rate), induced apoptosis, and down-regulated PCNA expression in gastric cancer. Conclusion Mifepristone exerts significant growth inhibitory effects on PR-positive human MKN-45 gastric cancer cells via multiple mechanisms, and may be a beneficial agent against the tumor.展开更多
To explore the reversal effect of mifepristone on multidrug resistance (MDR) in drug-resistant human breast cancer cell line MCF7/ADR and its mechanisms. Methods: Expression of MDR1 and MDR-associated protein(MRP) mRN...To explore the reversal effect of mifepristone on multidrug resistance (MDR) in drug-resistant human breast cancer cell line MCF7/ADR and its mechanisms. Methods: Expression of MDR1 and MDR-associated protein(MRP) mRNA in MCF7/ADR cells was detected using reverse transcription- polymerase chain reaction(RT-PCR). Western blotting was used to assay the protein levels of P-glycoprotein (P-gp) and MRP. Intracellular rhodamine 123 retention and [3H]vincristine (VCR) accumulation were measured by flow cytometry and liquid scintillation counter, respectively. MTT reduction assay was used to determine the sensitivity of cells to the anticancer agent, adriamycin (ADR). Additionally, a MCF7/ADR cell xenograft model was established to assess the reversal effect of mifeprisone on MDR in MCF7/ADR cells in vivo. Results: Miferpristone dose-dependently down- regulated the expression of MDR1 and MRP mRNA in MCF7/ADR cells, accompanied by a significant decrease in the protein levels of P-gp and MRP. After exposure to 5, 10, and 20 mmol/L mifepristone, MCF7/ADR cells showed a 3.87-, 5.81-, and 7.40-fold increase in the accumulation of intracellular VCR(a known substrate of MRP), and a 2.14-, 4.39-, and 5.53-fold increase in the retention of intracellular rhodamine 123(an indicator of P-gp function), respectively. MTT analysis showed that the sensitivity of MCF7/ADR cells to ADR was enhanced by 7.23-, 13.62-, and 20.96-fold after incubation with mifepristone as above-mentioned doses for 96 h. In vivo, mifepristone effectively restored the chemosensitivity of MCF7/ADR cells to ADR. After 8 weeks of administration with ADR(2 mg穔g-1穌-1) alone or in combination with mifepristone(50 mg穔g-1穌-1), the growth inhibitory rate of xenografted tumors in nude mice was 8.08% and 37.25%, respectively. Conclusion: Mifepristone exerts potent reversal effects on MDR in MCF7/ADR cells in vitro and in vivo through down- regulation of MDR1/P-gp and MRP expression and inhibition of P-gp- and MRP-dependent drug efflux, thus increasing the sensitivity to anticancer drug.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
文摘Aim To determine the structure of the by-product produced in Grignard reaction for preparing mifepristone derivatives, and elucidate the reaction mechanism.Methods The structure of the by-product was determined with elemental analysis, one- and two-dimension spectra NMR (DEPT, 1H-1Hcosy, HMQC, HMBC) and compared with those of mifepristone.Results The main by-product was 11,17-di-addition product of Grignard reagent of N, N-dimethylamino phenyl bromide.Conclusion This is the first complete assignment of 1H NMR and 13C NMR of compound (3).
文摘Objective: To compare the clinical efficacy of Cassia Twig Tuckahoe capsule (Chinese Medicine) and Mifepristone combined with laparoscopic surgery for the treatment of endometriosis. Designs: Prospective cohort study. Setting: Gynecology and Obstetrics Department, Jingzhou Central Hospital, affiliated to Yangtze University. Methods: We selected 67 patients suspected with endometriosis and divided randomly into 2 groups on patient choice. Outcome Measures: Treatment efficacy, side effects, recurrence rate and pregnancy rate. Results: Comparing the effect of treatment between the two groups, the success rate was almost same (P > 0.5). However, the disappearance of pain was faster in Cassia twig Tuckahoe group (P Conclusion: After analysis of the result, Cassia twig Tuckahoe capsule combined with Laparoscopy is superior to the Mifepristone combined with Laparoscopy. Cassia twig Tuckahoe capsule is a very propitious medicine for treating endometriosis for long term benefits.
文摘Objective To compare the effects of 2 dosage-forms (granular and decoction) of Arnebia euchroma (royle) Johnst (Arnebia EJ in short below) on medical abortion with that of mifepristone combined with misoprostol Methods Totally 648 women, who had pregnancy of 38-45 d and were willing to terminate pregnancy with mifepristone and misoprostol, were randomly divided into 3 groups, each of which was respectively given granular of Arnebia EJ, placebo granular, or decoction of Arnebia EJ besides mifepristone and misoprostol. The abortion results, bleeding duration, menstruation recovery and side-effects were observed. Results Neither complete abortion rates nor average bleeding durations of the granular group and the decoction group were significantly different (P>0.05). The complete abortion rate and bleeding duration of the two groups were respectively higher and shorter than those of the placebo group (P<0.05). However, the menstruation recov- ery was not significantly different among the three groups (P>0.05). The decoction of Arnebia EJ caused significantly more nausea and vomiting than the other groups (P<0.05). Conclusion The granular form did not have the odor of Arnebia EJ, and caused much less nausea and vomiting compared with the decoction form. The granular and decoc- tion forms were equally effective in improving the results of medical abortion. There- fore it is necessary to conduct further studies on the granular form of Arnebia EJ.
文摘Objective To investigate effects of mifepristone (MP) on the development and ultrastructure of mouse blastocysts in vivo Methods Sixty female mice were equally divided into 4 groups: control group (group A), 1.9 mg/kg MP group (group B), 5.6 mg/kg MP group (group C), and 16.8 mg/kg MP group (group D). The female mice of 4 groups undertook a superovulation method. The development of obtained blastocysts was evaluated, and ultrastructural changes of the blastocysts were observed by transmission electron microscope. Results In comparison with group A, the development rate of blastocysts in group B showed no difference (P〉0.05), while the development rate of blastocysts in both group C and group D was significantly lower (P〈0.05). With doses of 5.6 mg/kg and 16.8 mg/kg, the blastocysts showed granular appearance of the cytoplasm, irregular cell borders, enlarged perivitelline space and degeneration. Ultrastructure of the blastocysts in group B was similar to group A, except a little number of fat droplets in the cytoplasm. In group C, the microvilli on apical surface was decreased in number or even disappeared, mitochondria were under developed, a lot of filamentous crystals were found in the cytoplasm. Cellular junctions were defected. In group D, the blastocyst cells were irregular in shape, mitochondria were frequently vacuolated, the nucleolus was enlarged, nuclear membrane was ruptured, and chromatin was slack. Conclusion MP could damage to the ultrastructure of mouse blastocyst, and was responsible for the inhibition of blastocyst development. The inhibitory effect of MP would be in a dose-dependent fashion.
文摘Objective: To compare the efficacy and side effects of levonorgestrel and low dose mifepristone in emergency contraception. Method: The study is a randomized double--blind multicenter comparative trial. A total of 1, 276 women with unprotected intercourse within 72 hours were allocated to one of the two study groups. In the levonorgestrel (LNG) group, 0. 75 mg LNG was taken twice, 12 hours apart, whereas in the mifepristone (Mife) group, a single dose of 10 mg mifepristone was taken and a placebo 12 hours after. Follow--up visit was paid on the seventh day of the expected next menstruation to evaluate the contraceptive efficacy and side effects. Contraceptive efficacy was calculated by Dixon’s method. Result:In the LNG group 20 pregnancies occurred among 643 women, while in the Mife group 9 pregnancies occurred among 633 women. The pregnancy rates were 3. 10% and 1. 43% respectively. Contraceptive efficacy rate of preventing pregnancy was 59. 16% and 79. 73%, the difference was statistically significant (P<O. 05). The incidence of various side effects, which were mild, was less than 10%. There was no statistical difference between the two groups. The percentage of subjects who had their next menstruation 3 days earlier or later than their expected menstruation in LNG group and Mife group was 77. 7% and 78. 5% respectively. Conclusion: Use of levonorgestrel or low dose mifepristone for emergency contraception is effective and safe.
文摘Objective To investigate the role of mifepristone in regulating cytokines of materno-fetal interface and serum of human early gestationMethods Thirty-five women with early pregnancy received mifepristone 50 mg orallyon study d 1 and d 2, respectively, followed by undergoing artificial abortion to getdecidua and villi on study d 3. Twenty-five women with early pregnancy withoutmifepristone administration as control also underwent artificial abortion to get de-cidua and villi. The expressions of TGF-β1 and TGF-β1 receptor mRNA in the earlydecidua and villi were assessed by using RT-PCR . The concentrations of serum TNF-α were measured by radioimmunoassay.Results The decidual expressions of TGF- β1 mRNA and TGF-β1 receptor mRNA in thetreated group were significantly lower than those of the control (P<0.05), while thevillus expressions of TGF-β1 and TGF-β1 receptor mRNA in the treated group were notsignificantly different from those of the control (P>0.05). The serum TNF-β1 levelselevated significantly after mifepristone treatment.Conclusion The antigestational effect of mifepristone might act through suppressingthe transcription of TGF-β1 and TGF-β1 receptor in the decidua and increasing theserum TNF-α level, which interfered in the materno-fetal interface Th2 bias.
文摘Objective To investigate the efficacy, safety and acceptability of mifepristone combined with misoprostol used for late luteal fertility regulationMaterials & Methods Sixty-one female volunteers were recruited and there were 261 treatment cycles in total. Subjects were planned to receive treatment with 25 mg of mifepristone, Q12 h × 4 orally for five days prior to expected menstruation followed by 400 μg of misoprostol 48 h later for up to six cycles.Results There were 13 pregnancies in the 267 treatment cycles and among them complete abortion and continuing pregnancy occurred in 7 and 6 cycles respectively. So the overall pregnancy rate was 4. 87% (13/267) and the rate of continuing pregnancy was 2. 25% (6/267) , while the failure rate per pregnant cycle was 46. 15% (6/13). In treatment cycles the vaginal bleeding patterns changed insignificantly as compared with those in control cycles.Conclusion The efficacy, compliance and acceptability of the regimen should be further improved when it was administered for late luteal fertility regulation.
文摘To inverstgate the safety, effectiveness and acceptability Of conbination Of mifepristone and misoproslol for termination of high-risk pregnancy (amenorrhea≤ 70 days ).Three hundred and eighty-eight high-risk pregnant women, complicated with scarreduterus, or reproductive tract malformation, or uterus fibromyoma, or histories of recentabortion or repeated abortions, or pregnancy during lactation, and having duration of gestation ranging from 34 to 69 days, were administered orally 150 mg mifepristone (50 mgat the first time, and then 25 mg q 12 h × 4), and 600 μg misoprostol on the third day.The complete abortion rate ωas 92. 3%, while the incomplete abortion rate was 6. 2%, ongoing and pregnancy rate was 1. 5%. It was shown that combination of mifepristone andmisoprostol was effective in inducing abortion Of those high-risk pregnancies. Theregimen's effectiveness for high-risk population was similar to that for general population. Its safety, effectiveness and acceptability were satifactory. In addition, the softenedand dilated cervix made it easier and less painful to make vacuum aspiration in case offailure of the abortion.
文摘Objective To investigate telomerase activity in chorion and decidua from abortion induced by mifepristone incorporated with misoprostol at early pregnancy. Methods TRAP-SYBR Green assay was used to detect the expression of telomerase. Forty specimen were obtained from medicinal abortion (experiment group) and forty were from normal induced abortion (control group). Results Positive expression of chorion telomerase was significantly different between the experimental group (28%, 11/40) and the control group (73%, 29/40) (P〈0.05). While in decidua, the positive rate was 28% (11/40) in the experimental group and 20% (9/40) in the control group, there was no significant difference (P〉0.05). Conclusion It is suggested that miferistone may significantly decrease the telomerase activity in chorion but not in decidua.
文摘Objective To investigate the efficacy and safety in women after caesarian section for termination of early pregnancies by treatment, or repeated treatment with mifepristone and misoprostol. Subjects and Methods A total of 213 pregnant women with amenorrhea of 34~69 d after caesarian section who asked for medical abortion were recruited, including 63 cases undergoing their second medical abortion. A total amount of mifeprisstone of 150 mg given in separate doses (25 mg×4 and 50 mg at the first time) was administered orally within 3 d, followed by misoprostol of 0.6 mg orally in the morning of d 3. Results The complete abortion rate was 92.5%, incomplete abortion was 4.7% and failure was 2.8%. Conclusion The sequential use of mifepristone and misoprostol could be successfully and repeatedly used for induced abortion in those women with a caesarian section history. Its efficacy was similar to that for ordinary population. Its safety and effectiveness were satisfactory.
文摘Objective To explore the effects of mifepristone on the growth of human gastric cancer cell line MKN-45 and its possible mechanisms. Methods In situ hybridization was used to detect the expression of progesterone receptor (PR) mRNA in MKN-45 cells. Proliferation, cell cycle distribution, and the expression of Bcl-xL and vascular endothelial growth factor (VEGF) of MKN-45 cells incubated with various concentrations of mifepristone (1, 5, 10, and 20 μmol/L) were analyzed using MTT reduction assay, flow cytometry, reverse transcription-polymerase chain reaction (RT-PCR), and enzyme-linked immunoab-sorbent assay (ELISA), respectively. After transplantation of MKN-45 cells underneath the skin of athymic mice, mifepristone was administrated with the dose of 50 mg/(kg·d) for 6 weeks to evaluate the tumor growth. Apoptosis and the expression of proliferating cell nuclear antigen (PCNA) in xenografted tumors were detected using transmission electron microscopy and immunohistochemical staining, respectively. Results PR mRNA was highly expressed in cultured MKN-45 cell. Mifepristone dose-dependently inhibited the pr-oliferation of MKN-45 cells, and the inhibitory rate was dramatically increased from 7.21% to 47.23%. The inhibitory effect was accompanied by a dose-dependent increase in the percentage of cells in G 0 /G 1 phase, and with a concurrent decrease in the proportion of S- and G 2 /M-phase cells and the proliferative index from 57.65% to 24.54%. Meanwhile, mifepristone down-regulated the expression of Bcl-xL and VEGF in a dose-dependent manner. In vivo, mifepristone effectively inhibited the growth of xenografted tumors in nude mice (55.14% for inhibitory rate), induced apoptosis, and down-regulated PCNA expression in gastric cancer. Conclusion Mifepristone exerts significant growth inhibitory effects on PR-positive human MKN-45 gastric cancer cells via multiple mechanisms, and may be a beneficial agent against the tumor.
文摘To explore the reversal effect of mifepristone on multidrug resistance (MDR) in drug-resistant human breast cancer cell line MCF7/ADR and its mechanisms. Methods: Expression of MDR1 and MDR-associated protein(MRP) mRNA in MCF7/ADR cells was detected using reverse transcription- polymerase chain reaction(RT-PCR). Western blotting was used to assay the protein levels of P-glycoprotein (P-gp) and MRP. Intracellular rhodamine 123 retention and [3H]vincristine (VCR) accumulation were measured by flow cytometry and liquid scintillation counter, respectively. MTT reduction assay was used to determine the sensitivity of cells to the anticancer agent, adriamycin (ADR). Additionally, a MCF7/ADR cell xenograft model was established to assess the reversal effect of mifeprisone on MDR in MCF7/ADR cells in vivo. Results: Miferpristone dose-dependently down- regulated the expression of MDR1 and MRP mRNA in MCF7/ADR cells, accompanied by a significant decrease in the protein levels of P-gp and MRP. After exposure to 5, 10, and 20 mmol/L mifepristone, MCF7/ADR cells showed a 3.87-, 5.81-, and 7.40-fold increase in the accumulation of intracellular VCR(a known substrate of MRP), and a 2.14-, 4.39-, and 5.53-fold increase in the retention of intracellular rhodamine 123(an indicator of P-gp function), respectively. MTT analysis showed that the sensitivity of MCF7/ADR cells to ADR was enhanced by 7.23-, 13.62-, and 20.96-fold after incubation with mifepristone as above-mentioned doses for 96 h. In vivo, mifepristone effectively restored the chemosensitivity of MCF7/ADR cells to ADR. After 8 weeks of administration with ADR(2 mg穔g-1穌-1) alone or in combination with mifepristone(50 mg穔g-1穌-1), the growth inhibitory rate of xenografted tumors in nude mice was 8.08% and 37.25%, respectively. Conclusion: Mifepristone exerts potent reversal effects on MDR in MCF7/ADR cells in vitro and in vivo through down- regulation of MDR1/P-gp and MRP expression and inhibition of P-gp- and MRP-dependent drug efflux, thus increasing the sensitivity to anticancer drug.
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.