OBJECTIVETo investigate the metabolism-based interaction between ipriflavone(IP) and other drugs in vitro.

METHODSIP and propafenone or estradiol, or other drugs were co-incubated with rat liver microsome induced by beta-naphthoflavone. The concentrations of residual substrate in microsomal incubates were determined by HPLC.

RESULTThe metabolism of propafenone (10 microg/ml) incubated with 2 microg/ml or 50 microg/ml IP was markedly inhibited compared with control group(P<0.01). While the metabolism of 10 microg/ml of estradiol incubated with 10 microg/ml and 100 microg/ml IP showed no marked inhibition. When IP (20 microg/ml) was incubated with 0.5 microg/ml propranolol, 0.5 microg/ml propafenone or 5.0 microg/ml estradiol respectively the metabolic activity of IP was markedly inhibited compared with control group (P<0.05 P<0.05 P<0.02 respectively).

CONCLUSIONThe results indicate that there is an interaction between ipriflavone and propafenone during in vitro metabolism, and there might also be clinical significance.

Animals ; Drug Interactions ; Estradiol ; metabolism ; Female ; Isoflavones ; metabolism ; Propafenone ; metabolism ; Propranolol ; metabolism ; Rats ; Rats, Sprague-Dawley

OBJECTIVETo investigate the effects of 17beta-estradiol on the expression of alkaline phosphatase (ALP) and osteoprotegerin in human periodontal ligament cells.

METHODSHuman periodontal ligament cells (hPDLC) were obtained from periodontal tissue explants of teeth extracted for orthodontic treatment ALP activity was determined by PNPP, and OPG protein and corresponding mRNA levels were quantitatively detected by ELISA and RT-PCR RESULTS: ALP activity was significantly increased at 14 days and 21 days (P <0.05). 17beta-E2 of physiological concentration promoted secretion of OPG protein and expression of OPG mRNA (P <0.05). 17beta-E2 with high-dose showed no effect on OPG protein secretion and decrease OPG mRNA expression.

CONCLUSIONS17beta-E2 may have a positive impact on periodontium through promoting expression of ALP and OPG in hPDLC.

Alkaline Phosphatase ; metabolism ; Cells, Cultured ; Estradiol ; pharmacology ; Humans ; Osteoprotegerin ; metabolism ; Periodontal Ligament ; cytology ; drug effects ; metabolism

As men grow older, circulating testosterone declines while the incidence of cardiovascular disease increases. Thus, the role of sex hormones as biomarkers, and possibly contributing factors to clinical manifestations of cardiovascular disease in the increasing demographic of aging men, has attracted considerable interest. This review focuses on observational studies of endogenous androgens, namely circulating testosterone and dihydrotestosterone, which have examined their associations with cardiovascular events such as myocardial infarction and stroke. Studies which have examined the associations of endogenous estrogens, namely circulating estradiol, with these outcomes are also discussed. In large prospective cohort studies of predominantly middle-aged and older men, lower circulating testosterone consistently predicts higher incidence of cardiovascular events. Of note, both lower circulating testosterone and lower dihydrotestosterone are associated with higher incidence of stroke. These associations are less apparent when myocardial infarction is considered as the outcome. Results for estradiol are inconsistent. Lower circulating testosterone has been shown to predict higher cardiovascular disease-related mortality, as has lower circulating dihydrotestosterone. It is possible that the relationship of circulating androgens to cardiovascular events or mortality outcomes may be U-shaped rather than linear, with an optimal range defining men at lowest risk. Epidemiological studies are observational in nature and do not prove causality. Associations observed in studies of endogenous androgens need not necessarily translate into similar effects of exogenous androgens. Rigorous randomized controlled trials are needed to clarify the effects of testosterone treatment on cardiovascular risk in men.
Cardiovascular Diseases/mortality* ; Dihydrotestosterone/metabolism* ; Estradiol/metabolism* ; Humans ; Incidence ; Male ; Mortality ; Myocardial Infarction/metabolism* ; Stroke/metabolism* ; Testosterone/metabolism*

Animals ; Estradiol ; blood ; pharmacology ; Hepatocyte Growth Factor ; metabolism ; Liver Cirrhosis ; metabolism ; pathology ; Male ; Rats ; Rats, Wistar

OBJECTIVETo explore the efficacy and the reproductive endocrinal mechanism of herbal-partitioned moxibustion in the treatment of primary dysmenorrhea.

METHODSOne hundred and seventy-one cases of primary dysmenorrhea were randomized into an herbal-partitioned moxibustion group (group A), an starch-partitioned moxibustion group (group B) and an acupuncture group (group C), 57 cases in each one. In the group A, moxibustion isolated with herbal medicine was applied to Shenque (CV 8). In the group B, moxibustion isolated with starch was used at Shenque (CV 8). In the group C, acupuncture was given at Sanyinjiao (SP 6). The changes of estradiol (E2), progesterone (P) and prostaglandin levels (PGF2alpha) were observed before and after treatment, and the therapeutic effects were compared among the 3 groups.

RESULTSThe therapeutic effect in the group A was better than those in the other two groups [compared the cured rate: 89.8% (44/49) vs 60.0% (30/50), 60.4% (32/53), both P < 0.05]. In the group A, E2 level [(110.99 +/- 12.90) pg/mL vs (83.94 +/- 8.91) pg/mL, P < 0.05] and PGF2alpha level [(24.58 +/- 3.01) pg/mL vs (14.34 +/- 1.48) pg/mL, P < 0.01] were decreased and P level was increased [(4.65 +/- 0.68) ng/mL vs (6.68 +/- 0.95) pg/mL, P < 0.05]. In the group B and C, PGF2alpha level were reduced. Concerning to the regulating of E2 and PGF2alpha levels, the results in the group A were better than those in the group B and C [(-30.16 +/- 10.20) pg/mL vs (10.79 +/- 15.01) pg/mL, (22.81 +/- 12.22) pg/mL; (-13.10 +/- 2.40) pg/mL vs (-6.52 +/- 1.88) pg/mL, (-3.14 +/- 1.19) pg/mL, (see text) P < 0.05]. Concerning to the regulation of P level, the results in the group A and B were better than that in the group C (all P < 0.05).

CONCLUSIONThe herbal-partitioned moxibustion achieves the significant efficacy on primary dysmenorrhea, which could be related to regulating the reproductive endocrinal level. It decreases E2 and PGF2alpha levels and increases P level.

Acupuncture Points ; Adult ; Dinoprost ; metabolism ; Dysmenorrhea ; metabolism ; therapy ; Estradiol ; metabolism ; Female ; Humans ; Moxibustion ; Progesterone ; metabolism ; Young Adult

Animals ; Cadherins ; metabolism ; Catenins ; metabolism ; Estradiol ; pharmacology ; Estrogen Receptor Modulators ; pharmacology ; Female ; Ovariectomy ; Rats ; Uterus ; drug effects ; metabolism

OBJECTIVETo analyze the changes of heme oxygenase-1 (HO-1) and heme oxygenase-2 (HO-2) in the vaginal smooth muscle of ovariectomized female rats and to investigate the effects of estrogen on the expressions of HO-1 and HO-2 in the vaginal smooth muscle.

METHODSTwenty-four 8-week old female SD rats were equally randomized into Group A (2-week castrated) , B (4-week castrated), C (2-week sham operation) and D (4-week sham operation). The levels of plasma estradiol were measured by radio-immunoassay for all the rats and the expressions of HO-1 and HO-2 in the vaginal muscle were detected and analyzed by immunohistochemistry and RT-PCR.

RESULTSThe postoperative level of plasma estradiol was significantly lower in Groups A and B than in C and D (P < 0.05). And the expressions of HO-1 and HO-2 in the vaginal smooth muscle were significantly decreased in the first two groups as compared with the latter two.

CONCLUSIONHO-1 and HO-2 are expressed in the vaginal smooth muscle of the female rats, and their decreased expressions are correlated with the lowered level of plasma estradiol. Estrogen may play a physiological role in the vaginal smooth muscle via HO/CO.

Animals ; Estradiol ; blood ; Female ; Heme Oxygenase (Decyclizing) ; metabolism ; Muscle, Smooth ; metabolism ; Ovariectomy ; Rats ; Rats, Sprague-Dawley ; Vagina ; metabolism

OBJECTIVETo explore the clinical efficacy and action mechanism of acupuncture for premature ovarian failure (POF).

METHODSAccording to prospective cohort study design, 30 cases were included. Based on theory of regulating Chong and Conception Vessels as well as soothing the liver and calming the nerves, acupuncture at Guanyuan (CV 4), Dahe (KI 12), Taixi (KI 3), Taichong (LR 3), Baihui (GV 20) was applied, three times per week and 3 months were considered as one session. Totally two sessions were performed. The menstruation condition, estradiol (E2), follicle-stimulating hormone (FSH) and scores of the clinical perimenopausal symptoms were taken as treatment outcomes.

RESULTSThe total effective rate was 86.7% (26/30) and the cured rate was 16.7% (5/30). The recovery rate of menstruation was 16.7% (5/30) and the regain rate of menstruation was 56.7% (17/30). After the treatment, the level of E2 was significantly increased from (45.41 +/- 18. 09) pmol/L to (59.07 +/- 24.21) pmol/L (P < 0.05), and the score of perimenopausal symptoms was obviously reduced from 14.28 +/- 8. 30 to 4.04 +/- 3.28 (P < 0.01). However, no statistical differences could be seen in FSH before and after treatment (P > 0.05).

CONCLUSIONAcupuncture has certain effect on improving menstruation and perimenopausal symptoms in POF patients, which is likely to he related with increasing the level of E2.

Acupuncture Therapy ; Adolescent ; Estradiol ; metabolism ; Female ; Humans ; Luteinizing Hormone ; metabolism ; Primary Ovarian Insufficiency ; metabolism ; therapy ; Prospective Studies ; Young Adult

A rapid decline in egg production of laying hens begins after 480 d of age. Such a rapid decrease results predominantly from the ovarian aging, accompanied by endocrine changes, decreased yolk synthesis and accumulation, and the reduction in follicles selected into the preovulatory hierarchy. In this study, hens at 90, 150, 280, and 580 d old (D90, D150, D280, and D580, respectively) were compared for yolk precursor formation in the liver to elucidate effects of aging on laying performance. The results showed that liver lipid synthesis increased remarkably in hens from D90 to D150, but decreased sharply at D580 as indicated by the changes in triglyceride (TG) levels. This result was consistent with the age-related changes of the laying performance. The levels of liver antioxidants and total antioxidant capacity decreased significantly in D580 hens and the methane dicarboxylic aldehyde in D580 hens was much higher than that at other stages. The serum 17β-estradiol level increased from D90 to D280, but decreased at D580 (P<0.05). The expression of estrogen receptor α and β mRNAs in the liver displayed similar changes to the serum 17β-estradiol in D580 hens. Expressions of the genes related to yolk precursor formation and enzymes responsible for fat acid synthesis were all decreased in D580 hens. These results indicated that decreased yolk precursor formation in the liver of the aged hens resulted from concomitant decreases of serum 17β-estradiol level, transcription levels of estrogen receptors and critical genes involved in yolk precursor synthesis, and liver antioxidant status.
Age Factors ; Animals ; Antioxidants ; metabolism ; Chickens ; Egg Yolk ; metabolism ; Estradiol ; blood ; Female ; Lipids ; biosynthesis ; Liver ; metabolism ; Oviposition ; Receptors, Estrogen ; genetics

We reported clinical and physical responses to 7 weeks of anabolic-androgenic steroid (AAS) self-administration in a male recreational bodybuilder. He was self-administrating a total of 3,250 mg of testosterone when his previous and current clinical and physical trials records were revisited. Body shape, performance, and biochemistry results were clustered into three phases labeled PRE (before the self-use), POST I (immediately at the cessation of the 7-week administration), and POST II (12 weeks after the cessation). Elevated testosterone and estradiol levels were observed in the POST I phase, while hepatic and renal functions remained altered in the POST II phase. Body mass and body fat percentages increased throughout the three phases. When adjusted according to body mass, drops in aerobic and anaerobic power and capacity (2.1% to 12.9%) were observed across the phases. This case report shows that overall performance decreased when a bodybuilding practitioner self-administered AAS.
Adipose Tissue ; Biochemistry ; Doping in Sports ; Estradiol ; Humans ; Lipid Metabolism ; Male ; Resistance Training ; Steroids* ; Testosterone