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1.
Zhongguo Zhen Jiu ; 37(8): 836-839, 2017 Aug 12.
Article in Chinese | MEDLINE | ID: mdl-29231343

ABSTRACT

OBJECTIVE: To observe the efficacy differences between acupoint catgut embedding combined with auricular point pressure with beans and nilestriol on menopausal syndrome of liver-kidney deficiency type, and to explore their effects on estradiol (E2). METHODS: Sixty patients with menopausal syndrome of liver-kidney deficiency type were randomly divided into an acupoint stimulation group and a medication group, 30 cases in each group. The patients in the acupoint stimulation group were treated by acupoint catgut embedding at Taixi (KI 3), Sanyinjiao (SP 6), Shenshu (BL 23), Ganshu (BL 18) and Taichong (LR 3), combined with auricular point pressure at Gan (CO12), Shen (CO10), Neifenmi (CO18), Shenmen (TF4), Pizhixia (AT4); the treatment was given once a week for consecutive four weeks. The patients in the medication group were treated with oral administration of nilestriol, 1 mg, once a day, combined with oral administration of oryzanol, 20 mg, three times per day for consecutive four weeks. The clinical symptom score was compared between the two groups before and after treatment as well as in follow-up visit. The level of E2 was obserced before and after treatment, and the clinical effect was compared. RESULTS: (1) Compared before treatment, the clinical symptom score in the two groups was significantly reduced after treatment and in follow-up visit (all P<0.05); In follow-up visit, the clinical symptom score in the acupoint stimulation group was significantly lower than that in the medication group (P<0.05). The different value before treatment and at follow-up in the acupoint stimulation group was better than that in the medication group (P<0.05). (2) Compared before treatment, the level of E2 in the two groups were increased after treatment (both P<0.05); compared before and after treatment, the difference in the treatment group was significantly higher than that in the medication group (P<0.05). (3) After treatment, the total effective rate was 93.33% (28/30) in the acupoint stimulation group, which was similar to 90.00% (27/30) in the medication group (P>0.05). CONCLUSIONS: Compared with nilestriol, acupoint catgut embedding combined with auricular point pressure with beans could better improve clinical symptoms for patients with menopausal syndrome of liver-kidney deficiency type, and increased the level of E2.


Subject(s)
Acupuncture Points , Acupuncture, Ear/methods , Catgut , Menopause , Drug Therapy, Combination/methods , Estradiol/deficiency , Estrogens/therapeutic use , Female , Humans , Kidney , Liver , Phenylpropionates/therapeutic use , Quinestrol/analogs & derivatives , Quinestrol/therapeutic use , Syndrome , Treatment Outcome , Yang Deficiency/complications
2.
Am J Ther ; 23(6): e1630-e1636, 2016.
Article in English | MEDLINE | ID: mdl-26171988

ABSTRACT

We aim to compare the effects of simvastatin and combination of simvastatin and nylestriol on bone metabolism in ovariectomized (OVX) rats. Fifty healthy Wistar female rats were randomly allocated into 5 groups: sham + saline group (group A), OVX + saline group (group B), OVX + simvastatin (5 mg·kg·d) (group C), OVX + nylestriol (0.01 mg·kg·d) (group D), and OVX + simvastatin (3 mg·kg·d) + nylestriol (0.005 mg·kg·d) (group E). All mice were orally administrated with saline or medicine dissolved in saline for 10 weeks. Body weight of rats before and after the experiment was measured. Twenty-four hours after the experiment, calcium (Ca), creatinine (Cr), and hydroxyproline in urine were detected. Serum levels of osteocalcin (bone Gla-protein, BGP) and alkaline phosphatase (ALP) were measured. Bone mineral density was detected and trabecular bone was observed after the isolation of femur and tibia. Remarkably decreased serum BGP and increased serum ALP levels were detected in group B compared with those in group A. However, notably increased serum BGP and decreased serum ALP levels were found in groups C, D, and E compared with those in group B; femoral and tibial bone mineral density decreased in group B compared with that in group A, but increased in groups C, D, and E compared with that in group B. Simvastatin and combination of simvastatin and nylestriol promote formation of new bone, increase bone density, and improve bone microstructure damage in OVX rats.


Subject(s)
Bone Density/drug effects , Quinestrol/analogs & derivatives , Simvastatin/pharmacology , Alkaline Phosphatase/blood , Animals , Calcium/urine , Creatinine/urine , Drug Therapy, Combination , Female , Hydroxyproline/urine , Osteocalcin/blood , Ovariectomy , Quinestrol/administration & dosage , Quinestrol/pharmacology , Random Allocation , Rats , Rats, Wistar , Simvastatin/administration & dosage
3.
Mol Med Rep ; 12(1): 1066-74, 2015 Jul.
Article in English | MEDLINE | ID: mdl-25815520

ABSTRACT

Heng-Gu-Gu-Shang-Yu-He-Ji, also known as OsteoKing, is used as a herbal Traditional Chinese Medicine for the treatment of bone disease, including femoral head necrosis and osteoarthritis. However, whether OsteoKing has anti-osteoporotic properties has remained to be elucidated. The purpose of the present study was therefore to investigate the effects of OsteoKing on ovariectomy-induced osteoporosis in rabbits. Female New Zealand white rabbits were randomly divided into an ovariectomized (OVX) group and a sham-surgery group. The rabbits in the OVX group were subjected to an ovariectomy, while the rabbits in the sham group were subjected to the removal of an area of fat near the two ovaries. Bone mineral density, mechanical properties, serum biochemical parameters and micro-architecture were examined at 150 days post-OVX to characterize the experimental animal model. Once the osteoporotic rabbit model had been established, the rabbits in the OVX group were divided into the following groups: Model group, nilestriol group and 300 and 600 mg/kg OsteoKing groups, containing 16 rabbits in each group. OsteoKing and nilestriol were administered orally. The bone mineral density, mechanical properties, serum biochemical parameters, histology and micro-architecture were examined using dual-energy X-ray absorptiometric analysis, mechanical assessments, enzyme-linked immunosorbent assays, histopathological evaluation and micro-computerized tomography examination following 60 days and 120 days of treatment, respectively. Treatment with OsteoKing led to an elevation in the bone mineral density of the vertebra and serum phosphorus levels, reduced serum concentrations of osteocalcin, procollagen type I N-terminal peptide, tartrate-resistant acid phosphatase 5b and cross-linked N-telopeptide of type I collagen, improved mechanical properties (maximum load, stiffness and energy absorption capacity), and micro-architecture of the lumbar vertebra in the OVX osteoporotic rabbit model following treatment for 120 days. In conclusion, it was demonstrated that OsteoKing is effective in the prevention of estrogen deficiency-associated bone loss and may be a promising drug for the treatment of post-menopausal osteoporosis.


Subject(s)
Bone Density Conservation Agents/pharmacology , Bone Density/drug effects , Drugs, Chinese Herbal/pharmacology , Lumbar Vertebrae/drug effects , Osteoporosis/prevention & control , Absorptiometry, Photon , Acid Phosphatase/genetics , Acid Phosphatase/metabolism , Administration, Oral , Animals , Estriol/analogs & derivatives , Estriol/pharmacology , Estrogens/pharmacology , Female , Isoenzymes/genetics , Isoenzymes/metabolism , Lumbar Vertebrae/metabolism , Lumbar Vertebrae/pathology , Osteocalcin/genetics , Osteocalcin/metabolism , Osteoporosis/etiology , Osteoporosis/genetics , Osteoporosis/pathology , Ovariectomy/adverse effects , Peptide Fragments/genetics , Peptide Fragments/metabolism , Phosphorus/metabolism , Procollagen/genetics , Procollagen/metabolism , Quinestrol/analogs & derivatives , Rabbits , Tartrate-Resistant Acid Phosphatase , Tomography, Emission-Computed
4.
Mol Cell Endocrinol ; 387(1-2): 19-34, 2014 Apr 25.
Article in English | MEDLINE | ID: mdl-24565896

ABSTRACT

Nilestriol (NIL) has been applied to treat menopausal dysfunctions, yet its mechanism has remained unknown. To understand the relationship between the changes in homeostatic metabolites and ovarian oestrogen deficiency syndromes after NIL treatment, proton Nuclear Magnetic Resonance ((1)H NMR)-based metabonomic technologies were used to analyse a rat model of oestrogen deficiency. An orthogonal partial least-squares regression (OPLS) differentiation model was used on 12-week metabolic analyses of ovariectomised (OVX) rats treated or mock treated with NIL. Furthermore, data analysis using Chenomx software quantified results to identify the most significantly altered metabolite concentrations, allowing for metabolic explanations of the effects of NIL therapies. In this study, PLS results revealed that there are considerably distinct differences between treatment groups. Additionally, a total of 45 metabolites shown to have a high variation between groups were selected for target quantification. Using a one-way LSD ANOVA analysis, 32 metabolite concentrations were significantly altered in the OVX group. A total of 21 metabolites were altered significantly in the NIL-treatment group but later returned to normal. According to the OPLS VIP calculation, the metabolites most affected by NIL treatment were mostly involved in insulin resistance. In addition, abnormal concentration changes in lactate in the NIL-treatment group and 3-indoxylsulfate in the OVX group were observed. To our knowledge, this study is the first to address the molecular mechanism of NIL from a metabonomic perspective, and, more specifically, to establish a catalogue of endo-molecular changes effected by NIL in the regulation of oestrogen deficiency disorder.


Subject(s)
Estriol/analogs & derivatives , Menopause/drug effects , Metabolome/physiology , Animals , Body Weight , Estriol/pharmacology , Female , Indican/analysis , Insulin Resistance , Lactic Acid/analysis , Metabolomics , Nuclear Magnetic Resonance, Biomolecular , Ovariectomy , Quinestrol/analogs & derivatives , Rats , Rats, Sprague-Dawley , Serum/chemistry , Urine/chemistry
5.
Int J Mol Sci ; 13(1): 56-70, 2012.
Article in English | MEDLINE | ID: mdl-22312238

ABSTRACT

Genistein, a major phytoestrogen of soy, is considered a potential drug for the prevention and treatment of post-menopausal osteoporosis. Mounting evidence suggested a positive correlation between genistein consumption and bone health both in vivo and in vitro. Earlier studies have revealed that genistein acted as a natural estrogen analogue which activated estrogen receptor and exerted anti-osteoporotic effect. However, it remains unclear whether PTH, the most crucial hormone that regulates mineral homeostasis, participates in the process of genistein-mediated bone protection. In the present study, we compared the therapeutic effects between genistein and nilestriol and investigated whether PTH and its specific receptor PTHR1 altered in response to genistein-containing diet in the animal model of ovariectomy. Our results showed that genistein administration significantly improved femoral mechanical properties and alleviates femoral turnover. Genistein at all doses (4.5 mg/kg, 9.0 mg/kg and 18.0 mg/kg per day, respectively) exerted improved bending strength and b-ALP limiting effects than nilestriol in the present study. However, genistein administration did not exert superior effects on bone protection than nilestriol. We also observed circulating PTH restoration in ovariectomized rats receiving genistein at the dose of 18 mg/kg per day. Meanwhile, PTHR1 abnormalities were attenuated in the presence of genistein as confirmed by RT-PCR, Western blot and immunohistochemistry. These findings strongly support the idea that besides serving as an estrogen, genistein could interact with PTH/PTHR1, causing a superior mineral restoring effect than nilestriol on certain circumstance. In conclusion, our study reported for the first time that the anti-osteoporotic effect of genistein is partly PTH/PTHR1-dependent. Genistein might be a potential option in the prevention and treatment of post-menopausal osteoporosis with good tolerance, more clinical benefits and few undesirable side effects.


Subject(s)
Femur/drug effects , Genistein/pharmacology , Parathyroid Hormone/metabolism , Phytoestrogens/pharmacology , Protective Agents/pharmacology , Receptor, Parathyroid Hormone, Type 1/metabolism , Alkaline Phosphatase/blood , Animals , Bone Density/drug effects , Creatinine/blood , Creatinine/urine , Disease Models, Animal , Estriol/analogs & derivatives , Estriol/chemistry , Estriol/pharmacology , Female , Femur/physiology , Genistein/chemistry , Genistein/therapeutic use , Humans , Kidney/metabolism , Kidney/pathology , Osteoporosis, Postmenopausal/metabolism , Osteoporosis, Postmenopausal/pathology , Osteoporosis, Postmenopausal/prevention & control , Ovariectomy , Parathyroid Hormone/blood , Parathyroid Hormone/urine , Phytoestrogens/chemistry , Phytoestrogens/therapeutic use , Protective Agents/chemistry , Protective Agents/therapeutic use , Quinestrol/analogs & derivatives , Rats , Rats, Sprague-Dawley , Receptor, Parathyroid Hormone, Type 1/genetics , Tensile Strength
6.
Sichuan Da Xue Xue Bao Yi Xue Ban ; 42(4): 519-22, 2011 Jul.
Article in Chinese | MEDLINE | ID: mdl-21866639

ABSTRACT

OBJECTIVE: To investigate the influence of nilestriol (CCE3) and exercise on bone size and bone mass in ovariectomized (OVX) rats. METHODS: Forty eight (48) female Sprague-Dawley (SD) rats were divided randomly into six groups: (1) Normal control group, (2) Sham OVX group, (3) OVX group, (4) OVX + CCE3 group, (5)) OVX + exercise group, (6) OVX + CCE3 + exercise group. CCE (0.5 mg/kg per week) was given to the rats in OVX + CCE3 group and OVX + CCE3 + exercise group from the 2nd day after the operation for 11 weeks. Exercise training was loaded to the rats in exercise groups from the 7th day after operation, each rat was subjected to running on 0 dig angle runway with the speed of 16 m per minute, 45 minutes per day, 5 days per week for 10 weeks. RESULTS: The bone diameter, bone volume, bone wet weight, bone dry weight, bone ashes weight in the OVX group were lower than those in the sham OVX group (P < 0.01). All of these measurements were increased in OVX + CCE3 group and OVX + exercise group when compared with the OVX group, but were still lower than those in sham OVX group (P < 0.01). Exercise enhances the effect of CCE3 (P < 0.01). CONCLUSION: Exercise enhances the effects of CCE3 on the improvement of both bone size and quantity in OVX rats.


Subject(s)
Bone and Bones/anatomy & histology , Estriol/analogs & derivatives , Osteoporosis/therapy , Physical Exertion , Animals , Bone Density , Combined Modality Therapy , Estriol/administration & dosage , Female , Osteoporosis/etiology , Ovariectomy , Quinestrol/analogs & derivatives , Random Allocation , Rats , Rats, Sprague-Dawley
7.
Int J Mol Sci ; 12(12): 8913-23, 2011.
Article in English | MEDLINE | ID: mdl-22272111

ABSTRACT

Pyrroloquinoline quinone (PQQ) was produced by fermentation of the Methylovorus sp. MP688 strain and purified by ion-exchange chromatography, crystallization and recrystallization. The yield of PQQ reached approximately 125 mg/L and highly pure PQQ was obtained. To determine the optimum dose of PQQ for radioprotection, three doses (2 mg/kg, 4 mg/kg, 8 mg/kg) of PQQ were orally administrated to the experimental animals subjected to a lethal dose of 8.0 Gy in survival test. Survival of mice in the irradiation + PQQ (4 mg/kg) group was found to be significantly higher in comparison with the irradiation and irradiation + nilestriol (10 mg/kg) groups. The numbers of hematocytes and bone marrow cells were measured for 21 days after sublethal 4 Gy gamma-ray irradiation with per os of 4 mg/kg of PQQ. The recovery of white blood cells, reticulocytes and bone marrow cells in the irradiation + PQQ group was faster than that in the irradiation group. Furthermore, the recovery of bone marrow cell in the irradiation + PQQ group was superior to that in irradiation + nilestriol group. Our results clearly indicate favourable effects on survival under higher lethal radiation doses and the ability of pyrroloquinoline quinine to enhance haemopoietic recovery after sublethal radiation exposure.


Subject(s)
Bone Marrow Cells/drug effects , Gamma Rays , Leukocytes/drug effects , PQQ Cofactor/pharmacology , Radiation-Protective Agents/pharmacology , Acute Radiation Syndrome/drug therapy , Administration, Oral , Animals , Bone Marrow Cells/radiation effects , Drug Therapy, Combination , Estriol/administration & dosage , Estriol/analogs & derivatives , Estriol/pharmacology , Estriol/therapeutic use , Fermentation , Leukocytes/radiation effects , Methylophilaceae/chemistry , Methylophilaceae/metabolism , Mice , PQQ Cofactor/administration & dosage , PQQ Cofactor/therapeutic use , Quinestrol/analogs & derivatives , Radiation-Protective Agents/administration & dosage , Radiation-Protective Agents/therapeutic use
8.
Zhong Yao Cai ; 33(9): 1445-9, 2010 Sep.
Article in Chinese | MEDLINE | ID: mdl-21243777

ABSTRACT

OBJECTIVE: To observe the estrogenic effect of formononetin and its effect on the expressions of atrial estrogen receptor subtypes alpha and beta (ERalpha and ERbeta). METHODS: 50 femal rats were randomly divided into five groups: sham group, model group, nilestriol group, formononetin groups of low and high dose. Rats in sham group were cut a piece of fat before closing the abdomen, the others were ovariectomized. Vaginal exfoliated cell were observed from the fifth day to the tenth after operation to test if the model is successful. The sham and model group were given nomal saline in 10 mL/kg by gavage, the remaining three groups were given nilestriol 2.5 mg/(kg x w), low [20 mg/(kg x d) land high dose [100 mg/(kg x d)) of formononetin by gavage respectively. In the 8th week, vaginal exfoliated cell were observed, then decapitated the rats, removed the uterus, weighed and take wright staining microscopy. The relative expressions of ERalpha and ERbeta of right atrium were detected by RT-PCR. RESULTS: The vaginal cells exhibit a change of estrus after had been fed with high dose of formononetin after 8 weeks. Formononetin increase the uterus coefficient and the expression of atrial ERbeta (P < 0.01), but it dose not have any effect on the expression of ERalpha (P > 0.05). CONCLUSION: Formononetin have estrogenic effect in ovariectomized rats, and it can markedly upregulate the expression of rats' atrial ERbeta.


Subject(s)
Estrogen Receptor alpha/metabolism , Estrogen Receptor beta/metabolism , Heart Atria/metabolism , Isoflavones/pharmacology , Phytoestrogens/pharmacology , Uterus/drug effects , Administration, Oral , Animals , Disease Models, Animal , Estriol/administration & dosage , Estriol/analogs & derivatives , Estriol/pharmacology , Female , Isoflavones/administration & dosage , Ovariectomy , Phytoestrogens/administration & dosage , Quinestrol/analogs & derivatives , Random Allocation , Rats , Rats, Sprague-Dawley , Reverse Transcriptase Polymerase Chain Reaction , Trifolium/chemistry
9.
Zhong Nan Da Xue Xue Bao Yi Xue Ban ; 35(12): 1248-53, 2010 Dec.
Article in Chinese | MEDLINE | ID: mdl-21200092

ABSTRACT

OBJECTIVE: To observe the effect of different concentrations of nylestriol (NYL) and levonorgestrel (LNG) on the expression of ERα and ERß in human osteoscarcoma MG-63 cell lines, and to explore the impact of paracrine effect on the gene expression. METHODS: MG-63 cells were treated with 3 concentrations (10(-10),10(-8), and 10(-6) mol/L) of NYL or LNG. The untreated control group and the positive control group were also established. The 2 groups treated with NYL (10(-10) mol/L) or LNG (10(-8) mol/L) were designed to renew the medium every 12 h. Semi-quantitative RT-PCR was conducted to detect the mRNA expression of ERα and ERß on the MG-63 cells treated with different concentrations of the 2 drugs, respectively. RESULTS: Both drugs up-regulated ERα and ERß mRNA expression. The best concentration for both NYL and LNG was 10(-6) mol/L for ERα expression. As for ERß, the best concentration of NYL and LNG was 10(-10) mol/L and 10(-8) mol/L. The role of medium replacement on the expression of ERα was not observed, but medium replacement inhibited ERß expression. CONCLUSION: Both NYL and LNG can up-regulate the mRNA expression of ER subtypes in MG-63 cells, with mutual restriction between the 2 subtypes. The paracrine effect on MG-63 cell lines may be involved in the regulation process of mRNA expression of ERß.


Subject(s)
Estrogen Receptor alpha/metabolism , Estrogen Receptor beta/metabolism , Levonorgestrel/pharmacology , Osteosarcoma/metabolism , Quinestrol/analogs & derivatives , Cell Line, Tumor , Estrogen Receptor alpha/genetics , Estrogen Receptor beta/genetics , Humans , Osteosarcoma/pathology , Quinestrol/pharmacology , RNA, Messenger/genetics , RNA, Messenger/metabolism
10.
Climacteric ; 13(6): 544-52, 2010 Dec.
Article in English | MEDLINE | ID: mdl-19938946

ABSTRACT

OBJECTIVE: To review the experience of menopausal symptoms and low-dose hormone therapy (HT) in postmenopausal women in China. DESIGN: Literature review and critical summaries of available prospective, clinical trials (randomized, controlled trials, RCTs). RESULTS: Chinese women experience menopausal symptoms less frequently compared with women in developed countries, and the prevalence of menopausal symptoms is less in women of southern China than in women of northern China. The majority of postmenopausal Chinese women lack knowledge about HT, and the usage rate of HT is low in these women compared to that in women of developed countries. Some RCTs investigated the efficacy and safety of low- or ultra-low-dose HT, including conjugated equine estrogen, estradiol valerate, transdermal estradiol, nylestriol alone or in combination with progesterone, and tibolone in postmenopausal Chinese women. These RCTs reported that low- or ultra-low-dose HT relieved menopausal symptoms and prevented bone loss as well as standard-dose HT and was less likely to induce side-effects, including irregular vaginal bleeding and breast tenderness; there may be dose-dependent effects of HT. No study evaluated the effects of low-dose HT on cardiovascular events or breast mammographic density/risk of breast cancer. CONCLUSIONS: More RCTs are required to confirm efficacy and to assess the safety of low- or ultra-low-dose HT for a long-term period in a large group of postmenopausal women.


Subject(s)
Estrogen Replacement Therapy/methods , Postmenopause , Administration, Cutaneous , Adult , Aged , Bone Density/drug effects , Cardiovascular Diseases/embryology , Cardiovascular Diseases/epidemiology , Cardiovascular Diseases/prevention & control , China , Endometrial Hyperplasia/epidemiology , Estradiol/administration & dosage , Estradiol/analogs & derivatives , Estrogen Replacement Therapy/adverse effects , Estrogen Replacement Therapy/statistics & numerical data , Estrogens, Conjugated (USP)/administration & dosage , Female , Humans , Middle Aged , Norpregnenes/administration & dosage , Progesterone/administration & dosage , Quinestrol/administration & dosage , Quinestrol/analogs & derivatives , Randomized Controlled Trials as Topic
11.
Zhongguo Zhen Jiu ; 29(4): 303-8, 2009 Apr.
Article in Chinese | MEDLINE | ID: mdl-19565740

ABSTRACT

OBJECTIVE: To observe the effect of acupuncture on fracture in the ovariectomized rat and the mechanism. METHODS: Sixty SD female rats were randomly divided into 4 groups: normal group (group A), model group (group B), acupuncture group (group C) and Nilestriol group (group D). In all the groups, except the group A which received sham operation, the rats were overiectomized for preparing the osteoporosis model. Three months after the ovariectomy, the left femurs of the rats were closely fractured. Then, the group A and B were treated with oral administration of normal saline solution, 3 mL, weekly. The rats in the group C were treated daily with acupuncture at "Huantiao"(GB 30), "Housanli" (ST 36), "Yanglingquan"(GB 34) and "Weizhong"(BL 40) on the left hind legs; the rats in the group D were given orally Nilestriol solution (0.2 mg/mL) in a dose of 0.6 mL/100 g body weight, weekly. At the 7th, 14th, 21st and 28th days, some rats were sacrificed and their fractural callus and blood samples were taken for histological examinations and immunohistochemical examination of brain-derived neurotrophic factor (BDNF) and tyrosine kinase B (TrkB). RESULTS: HE stained callus slides observed by optical microscope showed that the process of fracture healing in the group A, C, D was faster than that in the group B. Positive immuno-stalning of BDNF and TrkB could be seen in the all groups, mainly on the 7 and 14 days after the fracture. The expression levels from high to low in turn were group A, C, D and B. CONCLUSION: Expressions of BDNF and TrkB in callus of osteoporotic fracture were less than that of the normal fracture; acupuncture can elevate the expression levels and accelerate the process of fracture healing.


Subject(s)
Acupuncture Therapy/methods , Brain-Derived Neurotrophic Factor/biosynthesis , Fractures, Bone/therapy , Ovariectomy/adverse effects , Animals , Bony Callus/metabolism , Bony Callus/pathology , Estriol/administration & dosage , Estriol/analogs & derivatives , Estriol/therapeutic use , Female , Fractures, Bone/etiology , Immunohistochemistry , Quinestrol/analogs & derivatives , Random Allocation , Rats , Rats, Sprague-Dawley , Receptor, trkB/metabolism , Treatment Outcome
12.
Phytomedicine ; 16(4): 320-6, 2009 Apr.
Article in English | MEDLINE | ID: mdl-19269147

ABSTRACT

Icariin was evaluated for its antiosteoporotic activity in an ovariectomized rat model of osteoporosis. The rats were divided into sham and OVX groups. The OVX rats were then subdivided into five groups treated with water, nylestriol (1 mg/kg body weight, weekly, orally) or icariin (ICA) (5, 25, and 125 mg/kg body weight, daily, orally) for 12 weeks. In OVX rats, the increases of body weight, serum BGP and ALP were significantly decreased by ICA treatment. In OVX rats, atrophy of uterus and descent of BMD were suppressed by treatment with ICA. In addition, ICA (125 mg/kg body weight) completely corrected the decreased serum concentration of Calcium, Phosphorus, and E(2) observed in OVX rats. ICA (125 mg/kg body weight) increased biomechanical strength significantly in comparison to the sham group. Histological results also showed its protective action through promotion of bone formation. The findings, assessed on the basis of biochemical, bone mineral density, biomechanical, and histopathological parameters, showed that ICA has a definite antiosteoporotic effect, similar to estrogen, especially effective for prevention bone fracture induced by estrogen deficiency.


Subject(s)
Bone Density Conservation Agents/pharmacology , Bone Density/drug effects , Drugs, Chinese Herbal/pharmacology , Flavonoids/pharmacology , Osteoporosis/prevention & control , Alkaline Phosphatase/blood , Animals , Biomechanical Phenomena , Body Weight/drug effects , Bone and Bones/drug effects , Bone and Bones/metabolism , Bone and Bones/pathology , Calcium/blood , Estradiol/blood , Female , Osteocalcin/blood , Ovariectomy , Phosphorus/blood , Quinestrol/analogs & derivatives , Quinestrol/pharmacology , Rats , Rats, Sprague-Dawley , Uterus/drug effects
13.
Zhongguo Ying Yong Sheng Li Xue Za Zhi ; 25(1): 129-32, 2009 Feb.
Article in Chinese | MEDLINE | ID: mdl-21186636

ABSTRACT

AIM: To investigate the influence of CCE3 on bone mineral element metabolism and relative hormone in ovariectomized rats. METHODS: 24 female SD rats were divided randomly into 4 groups (n = 6): (1) Normal control; (2) sham ovariectomy; (3) ovariectomy(OVX); (4) OVX + CCE3. RESULTS: (1) Ca, Mg, S, Co, Mn, Zn reduced obviously and P increased in the bone of the OVX rats. (2) E2, P, TSH, T4, CT, cortisol, GH reduced obviously and IL-6, FSH, LH increased obviously in serum of the OVX rats. (3) CCE3 corrected the changes of Ca, Mg, S, Co, Mn, Zn and P in bone as well as the changes of E2, P, TSH, T4, CT, cortisol, GH and IL-6, FSH, LH in serum of the OVX rats. CONCLUSION: Changes of relative hormone and IL-6 induced by CCE3 are the important mechanism of the influence of CCE3 on bone mineral element metabolism in ovariectomized rats.


Subject(s)
Bone Density/drug effects , Estriol/analogs & derivatives , Osteoporosis/prevention & control , Animals , Estriol/therapeutic use , Female , Follicle Stimulating Hormone/blood , Interleukin-6/blood , Luteinizing Hormone/blood , Osteoporosis/drug therapy , Osteoporosis/physiopathology , Ovariectomy , Quinestrol/analogs & derivatives , Rats , Rats, Sprague-Dawley
14.
J Pharm Biomed Anal ; 46(4): 663-9, 2008 Mar 13.
Article in English | MEDLINE | ID: mdl-18215486

ABSTRACT

A set of simple HPLC methods employing UV detection were developed for detection of counterfeit drugs by the qualitative and quantitative analysis of nine steroidal drugs, ethinylestradiol, diethylstilbestrol, norethisterone, norgestrel, methyltestosterone, medroxyprogesterone acetate, progesterone, testosterone propionate and nilestriol. The methods were based on studies of the relationships between the retention factors (k) of the nine compounds and the percentages of water to methanol in the mobile phases on a reverse phase Alltima C(18) column giving reliable separation of the compounds under three sets of chromatographic conditions. The methods were validated using statistical tests and were used on nine commercial samples for detection of possible counterfeit drugs.


Subject(s)
Chromatography, High Pressure Liquid/methods , Steroids/analysis , Diethylstilbestrol/analysis , Estriol/analogs & derivatives , Estriol/analysis , Ethinyl Estradiol/analysis , Medroxyprogesterone Acetate/analysis , Methyltestosterone/analysis , Norgestrel/analysis , Progesterone/analysis , Quinestrol/analogs & derivatives , Sensitivity and Specificity , Testosterone Propionate/analysis
15.
Chin J Integr Med ; 12(2): 132-6, 2006 Jun.
Article in English | MEDLINE | ID: mdl-16800993

ABSTRACT

OBJECTIVE: To observe the effect of Gengnianchun Recipe (GNC) on bone mineral density (BMD), bone biomechanical parameters and serum lipid level in the bilaterally ovariectomized (OVX) rats and to explore the prophylactic and therapeutic action of GNC on ovariectomy induced osteoporosis and hyperlipidemia. METHODS: OVX SD rats, 10 - 12 months old, were divided into different groups and fed with GNC 2 g/d, GNC 1 g/d and Nilestriol 0.125 mg/week, respectively for 4 months to observe the change of BMD and bone biomechanical parameters of the lumbar vertebrae, and the serum levels of total cholesterol (TC), triglyceride (TG), high-density lipoprotein cholesterol (HDL-C) and low-density lipoprotein cholesterol (LDL-C), and to compare the effect of the two drugs on the morphology of the uterus. RESULTS: There was marked reduction in BMD and biomechanical parameters in lumbar vertebrae (P < 0.01) and increase of serum TC and LDL-C levels (P < 0.01) in rats after OVX. GNC or Nilestriol significantly improved the decreased BMD and biomechanical parameters of the lumbar vertebrae (P < 0.05 or P < 0.01), and reduced the serum TC and LDL-C levels (P < 0.01). In the Nilestriol group, the wet weight of uterus got increased obviously (P < 0.01), the number of uterine glands increased, uterine columnar epithelium thickened, and the mitotic figures in the epithelial stroma and myointimal cells augmented. But no such effect in wet weight and morphology of uterus was found in the GNC group. CONCLUSION: GNC could increase the BMD and biomechanical parameters of the lumbar vertebrae, reduce the serum TC and LDL-C levels, yet produce no adverse reaction in stimulating proliferation and hypertrophy of uterus.


Subject(s)
Bone Density/drug effects , Bone and Bones/drug effects , Drugs, Chinese Herbal/pharmacology , Lipids/blood , Animals , Biomechanical Phenomena , Cholesterol/blood , Cholesterol, HDL/blood , Cholesterol, LDL/blood , Estriol/analogs & derivatives , Estriol/pharmacology , Female , Ovariectomy , Quinestrol/analogs & derivatives , Rats , Rats, Sprague-Dawley , Triglycerides/blood , Uterus/cytology , Uterus/drug effects
16.
J Ethnopharmacol ; 108(1): 96-102, 2006 Nov 03.
Article in English | MEDLINE | ID: mdl-16765003

ABSTRACT

The antiosteoporotic effect of a herbal formula, Er-Xian Decoction (EXD), in ovariectomized (OVX) rats model of osteoporosis was investigated. The rats were divided into Sham and OVX groups. The OVX rats were further sub-divided into four groups administered orally with water, nylestriol (1 mg/kg, weekly) or EXD (300, 600 mg/kg, daily) for 12 weeks. In OVX rats, the increases of body weight, serum BGP and ALP were significantly decreased by EXD treatment. In OVX rats, atrophy of uterus and descent of BMD were suppressed by treatment with EXD and nylestriol. In addition, EXD completely corrected the decreased concentration of calcium, phosphorus, and estradiol in serum observed in OVX rats. EXD also significantly increased biomechanical strength comparable to the Sham group. This was also confirmed by histological results that showed its protective action. The findings assessed on the basis of biochemical, bone mineral density, biomechanical, and histopathological parameters strongly suggested that EXD had a definite antiosteoporotic effect, which is similar to estrogen.


Subject(s)
Bone Density Conservation Agents/pharmacology , Drugs, Chinese Herbal/pharmacology , Medicine, Chinese Traditional , Osteoporosis/prevention & control , Ovariectomy , Plants, Medicinal , Animals , Body Weight/drug effects , Bone Density Conservation Agents/therapeutic use , Dose-Response Relationship, Drug , Drugs, Chinese Herbal/therapeutic use , Female , Organ Size/drug effects , Quinestrol/analogs & derivatives , Quinestrol/therapeutic use , Rats , Rats, Sprague-Dawley , Uterus/anatomy & histology , Uterus/drug effects
17.
Zhongguo Zhong Yao Za Zhi ; 30(11): 855-7, 2005 Jun.
Article in Chinese | MEDLINE | ID: mdl-16110871

ABSTRACT

OBJECTIVE: To study the protective effect of purariae isoflavone on apoptosis cells of atrophic nasal mucosas in ovariectomized rats. METHOD: 60 rats were divided into four groups as control, ovariectomized, ovariectomized + nylestriol (O + N) and ovariectomized + purariae isoflavone (O + P), each with 15 rats. Earlier apotosis cells of mucosas taken from nasal septum were measured with flow cytometry. RESULT: Compared with control group, and the number of apoptosis cells of mucosas increased after being ovariectomized,and the number of apoptosis cells of mucosas in O + N and O + D group didn't change. CONCLUSION: Nylestriol and purariae isoflavone might have effects on protecting cells of mucosas from lacking of estrogen by decreasing apoptosis cells in ovariectomized rats.


Subject(s)
Apoptosis/drug effects , Epithelial Cells/pathology , Isoflavones/pharmacology , Nasal Mucosa/pathology , Pueraria , Animals , Estradiol Congeners/pharmacology , Female , Isoflavones/isolation & purification , Ovariectomy , Plants, Medicinal/chemistry , Protective Agents/isolation & purification , Protective Agents/pharmacology , Pueraria/chemistry , Quinestrol/analogs & derivatives , Quinestrol/pharmacology , Rats , Rats, Sprague-Dawley
18.
Lin Chuang Er Bi Yan Hou Ke Za Zhi ; 19(5): 222-4, 2005 Mar.
Article in Chinese | MEDLINE | ID: mdl-15934292

ABSTRACT

OBJECTIVE: To study the protective effect of nylestriol on apoptosis cells of atrophic nasal mucosas in ovariectomized rats and the difference between nasal drip and gastrogavage. METHOD: Sixty rats with atrophic rhinitis were divided into four groups at random (each with 15 rats): contrary group (Cg), ovariectomized group (Og), ovariectomized + nylestriol nasal drip group (ONNDg), and ovariectomized + nylestriol by gastrogavage (ONGg). Earlier apoptosis cells of nasal mucosas taken from nasal septum were measured with flow cytometry. RESULT: After being ovariectomized, the number of apoptosis cells of mucosas increased. In ONGg, the number of apoptosis cells of mucosas increased at 15 d after operation (P < 0.05), but it recovered at 30 d and 60 d after operation. In ONGg, the number of apoptosis cells of mucosas increased at 15 d and 30 d after operation (P < 0.05), but it recovered at 60 d after operation. CONCLUSION: Estrogen replacement by gastrogavage and via nasal drip have effects on protecting cells of mucosas from lacking of estrogen by decreasing apoptosis cells in ovariectomized rats. It might cost more time to get therapeutic effectiveness via nasal drip than by gastrogavage.


Subject(s)
Apoptosis/drug effects , Epithelial Cells/drug effects , Estrogen Replacement Therapy , Nasal Mucosa/drug effects , Quinestrol/analogs & derivatives , Administration, Intranasal , Animals , Epithelial Cells/pathology , Female , Nasal Mucosa/pathology , Ovariectomy , Quinestrol/administration & dosage , Quinestrol/pharmacology , Random Allocation , Rats , Rats, Sprague-Dawley
19.
Zhonghua Bing Li Xue Za Zhi ; 33(3): 255-9, 2004 Jun.
Article in Chinese | MEDLINE | ID: mdl-15256120

ABSTRACT

OBJECTIVE: To clarify the effects of nylestriol on microarchitecture and interleukin-6 (IL-6) mRNA expression in tibial bone in ovariectomized rats. METHODS: 30 female rats were randomly allocated into 3 groups: sham, OVX and nylestriol-treated group. Nylestriol-treated group were ovariectomized, then fed with nylestriol for 3 months and the bone mineral density (BMD) was measured in lumbar vertebra by dual energy x-ray absorptiometry. After sacrifice of the animal, bone histomorphometric parameters were measured to study the changes in bone microarchitecture, and RT-PCR was performed to detect the expression of IL-6 mRNA in bone tissue. RESULTS: BMD was significantly reduced, while IL-6 mRNA level elevated in the OVX group compared with the sham group. Static histomorphometric data showed that the trabecular bone volume, mean trabecular plate thickness and density were reduced while the mean trabecular plate space elevated remarkably in the OVX group in comparison with that in the sham group. As for dynamic parameters, trabecular osteoid surface, tetracyclin labeled surface and bone turnover rate were increased while osteoid maturation rate decreased significantly in the OVX group compared with the sham group. BMD, IL-6 mRNA expression and bone histomorphometric parameters were improved in nylestriol-treated rats. CONCLUSION: Nylestriol plays an important role in maintaining bone volume and improving bone microarchitecture by markedly inhibiting bone turnover and bone resorption, which might be to some degree attributed to reduced IL-6 expression.


Subject(s)
Bone Remodeling/drug effects , Osteoporosis/pathology , Quinestrol/analogs & derivatives , Quinestrol/pharmacology , Animals , Bone Resorption/prevention & control , Estradiol Congeners/pharmacology , Estradiol Congeners/therapeutic use , Female , Interleukin-6/biosynthesis , Interleukin-6/genetics , Osteoporosis/drug therapy , Osteoporosis/etiology , Ovariectomy , Quinestrol/therapeutic use , RNA, Messenger/biosynthesis , RNA, Messenger/genetics , Random Allocation , Rats , Rats, Wistar , Tibia/pathology
20.
Zhong Nan Da Xue Xue Bao Yi Xue Ban ; 29(6): 667-70, 2004 Dec.
Article in Chinese | MEDLINE | ID: mdl-16114553

ABSTRACT

OBJECTIVE: To determine the effect of nylestriol and levonorgestrel on mRNA expression of OPG/OPGL in MG-63 cell lines, and to explore whether the paracrine effect is involved in the regulation course. Methods Semi-quantitive RT-PCR was conducted to analyze mRNA expression of OPG/OPGL in MG-63 cell lines treated with nylestriol and levonorgestrel. Results Both medicines could stimulate MG-63 cell lines to express OPG, and the best action levels of the two medicines were 10(-6) mol/L. Both medicines could decrease mRNA expression levels of OPGL dramatically. In NYL 10(-10) mol/L treatment group, medium renewal has negative effect on mRNA expression of OPG. Conclusion Both the two medicines can promote mRNA expression of OPG in MG-63 cell lines, while decrease mRNA expression of OPGL. The paracrine effect of MG-63 cell lines may be involved in the regulation of mRNA expression of OPG by NYL.


Subject(s)
Carrier Proteins/biosynthesis , Glycoproteins/biosynthesis , Levonorgestrel/pharmacology , Membrane Glycoproteins/biosynthesis , Osteosarcoma/pathology , Quinestrol/analogs & derivatives , Receptors, Cytoplasmic and Nuclear/biosynthesis , Receptors, Tumor Necrosis Factor/biosynthesis , Carrier Proteins/genetics , Female , Glycoproteins/genetics , Humans , Membrane Glycoproteins/genetics , Osteoprotegerin , Quinestrol/pharmacology , RANK Ligand , RNA, Messenger/biosynthesis , RNA, Messenger/genetics , Receptor Activator of Nuclear Factor-kappa B , Receptors, Cytoplasmic and Nuclear/genetics , Receptors, Tumor Necrosis Factor/genetics , Tumor Cells, Cultured
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