The differential anti-proliferation effect of white (Pueraria mirifica), red (Butea superba), and black (Mucuna collettii) Kwao Krua plants on the growth of MCF-7 cells

The differential anti-proliferation effect of white (Pueraria mirifica), red (Butea superba) and black (Mucuna collettii) Kwao Krua plant extracts on the growth of MCF-7 cells was evaluated after 4 days of incubation. The percent cell growth comparison was based on protein determination of the harvested cells in parallel with the control group and Pueraria lobata treatment group. Pueraria lobata led to no proliferation and a mild anti-proliferation effect on the growth of MCF-7 cells. Pueraria mirifica caused proliferation at 1 microg/mL and an anti-proliferative effect on the growth of MCF-7 cells at 100 and 1000 microg/mL with an ED50 value of 642.83 microg/mL. Butea superba led to no proliferation and an anti-proliferation effect on the growth of MCF-7 cells at 10, 100 and 1000 microg/mL with an ED50 value of 370.91 microg/mL. Mucuna collettii led to no proliferation and an anti-proliferation effect on the growth of MCF-7 cells at 100 and 1000 microg/mL with an ED50 value of 85.36 microg/mL. The results demonstrated that only Pueraria mirifica showed an estrogenic effect on MCF-7 cell growth and a clear antagonistic effect with E2 at high concentration. Butea superba and Mucuna collettii exhibited only anti-proliferation effects on the growth of MCF-7 cells in relation with a possible anti-estrogen mechanism or a potent cytotoxic effect.     

Evaluation of estrogenic activity of alcoholic extract of rhizomes of Curculigo orchioides

The rhizomes of Curculigo orchioides Gaertn. (Amaryllidacea) is an important Ayurvedic as well as Unani drug. It is present in several drug formulations used in the treatment of menorrhagia and other gynecological problems. In this study, we conducted a comparative study of estrogenic activity of alcoholic extract of Curculigo orchioides with diethylstilbestrol in bilaterally ovariectomized young albino rats. Bilaterally ovariectomized albino rats were divided into five groups (n=9) receiving different treatments, consisting of vehicle (0.6% w/v sodium carboxy methyl cellulose), ethanolic extract of rhizomes of Curculigo orchioides at three different doses (viz., 300, 600, 1200 mg/kg body weight) and standard drug diethylstilbestrol (DES) at a dose of 2 mg/kg body weight. All these were administered orally daily for 7 days. Estrogenic activity was assessed by taking percentage vaginal cornification, uterine wet weight, uterine glycogen content and uterine histology as parameters of assessment. Alcoholic extract of Curculigo orchioides showed a significant increase in percentage vaginal cornification, uterine wet weight (P<0.001), uterine glycogen content (P<0.001) and a proliferative changes in uterine endometrium compared to the control.     

九里香叶对去卵巢大鼠拟雌激素样作用的实验研究

目的探讨九里香叶对去卵巢大鼠的拟雌激素样作用。方法以2%戊巴比妥钠麻醉大鼠,切除大鼠双侧卵巢,对照大鼠切除卵巢旁同样大小的脂肪团。术后7天分组、给药。分为模型组:生理盐水(0.4 mg/kg/d);对照组:生理盐水(0.4 mg/kg/d);戊酸雌二醇组:0.4 m g/kg/d;九里香高剂量组:200 mg/kg/d;九里香中剂量组:100 mg/kg/d;九里香低剂量组:50 mg/kg/d。连续给药90天后,处死大鼠,测定子宫系数。放射免疫法测定血清雌二醇水平。结果给药第30天、60天、90天,与对照组比较,模型组大鼠体质量增幅较大,差异显著;与模型组比较,戊酸雌二醇组、九里香叶高剂量组大鼠体质量增幅较小,差异显著(P0.05)。与模型组比较,戊酸雌二醇组、九里香叶高剂量组大鼠子宫质量和子宫系数明显增加,差异显著(P0.05)。与模型组比较,戊酸雌二醇组、九里香叶高、中、低剂量组大鼠雌二醇明显增加,差异不显著(P0.05)。结论九里香叶具有一定的雌激素样作用。     

葛根素和葛根总异黄酮的雌激素样活性

目的：研究葛根素和葛根总异黄酮的雌激素样活性。方法：去卵巢大鼠、幼年小鼠、成年小鼠和雌激素化小鼠灌胃给予葛根素和葛根总异黄酮150－600mg/kg，连续5－9天后，阴道脱落细胞检查和子宫重量法判断雌激素样作用。结果：葛根素和葛根总异黄酮能明显增加去卵巢大鼠阴道涂片中角化细胞数量，部分恢复去卵巢大鼠的性周期；使去卵巢大鼠和幼年小鼠子宫重量明显增加，这种作用呈明显的剂量依赖性。对正常成年小鼠的子宫生长无明显影响，在合用雌二醇时，葛根素和葛根总异黄酮均使雌二醇的促子宫生长作用明显减弱。结论：葛根素和葛根总异黄酮对雌激素低下动物显示弱雌激素活性，对正常雌激素水平动物无明显雌激素样活性，而在合用雌二醇时，则部分抑制雌二醇的促子宫生长作用，提示葛根素和葛根总异黄酮具有雌激素受体部分激动剂的特性。     

The transgenic Arabidopsis plant system, pER8-GFP, as a powerful tool in searching for natural product estrogen-agonists/antagonists

The transgenic Arabidopsis plant system, pER8-GFP, may be used as a powerful tool in searching for natural estrogen-agonists/antagonists. Among selected plant extracts and natural products, the method was able to distinguish active extracts (e.g., Glycine max and Pueraria lobata) and pure compounds (e.g., 17beta-estradiol (1), genistein (10), and daidzein (11)) and also to distinguish effects of structural changes on activity. Thus, this rapid sensitive system was proven to be suitable for the discovery of natural products with estrogenic activity.     

Attenuation of inflammation in streptozotocin-induced diabetic rabbits by Matricaria chamomilla oil: A focus on targeting NF- κ B and NLRP3 signaling pathways

Objectives: The present study was conducted to investigate the protective effects of chamomile oil from Matricaria chamomilla against type 1 diabetes mellitus(T1 DM) and its potential mechanisms.Methods: T1 DM was established in male New Zealand white rabbits via a single intraperitoneal infusion of streptozotocin(STZ)(80 mg/kg body weight-1, dissolved in 0.2 m L of normal saline). Different doses of chamomile oil(25, 50 and 100 mg/kg) were orally administrated to STZ induced diabetic rabbits for 21 consecutive days. The expression of pro-inflammatory cytokines was determined using ELISA assay. The expression of NF-κB and NLRP3 was measured using Western blot assay.Results: Compared with normal rabbits, STZ-induced diabetic rabbits exhibited significant increased levels of blood glucose and decreased levels of serum insulin that were reversed using middle and high tested dose of chamomile oil. Likewise, STZ-induced diabetic rabbits showed a significant increased expression of NF-κB and NLRP3 proteins in the pancreas tissue that was reversed by high tested dose of chamomile oil.Conclusion: Collectively, our findings demonstrated that chamomile oil possesses anti-hyperglycemic, and anti-inflammatory activities in STZ-induced diabetic rabbits by targeting inflammatory cytokines and NF-κB and NLRP3 signaling pathways.     

Estrogenic activity of standardized extract of Angelica sinensis

Since ancient times, extracts of plants have been used for women's health to prevent menopausal symptoms. The symptoms of menopause have been attributed to a reduction in the amount of estrogen produced by the ovaries.In this study the estrogenic activity of a commercial standardized extract of the roots of Angelica sinensis, used to relieve climacteric symptoms was evaluated using in vivo tests such as the degree of cornification of vaginal epithelium, uterotrophic assays and serum LH concentration in ovariectomized rats. Furthermore, the effects on the estrous cycle in rat were investigated.The results obtained have shown that the administration of a standardized ethanol extract in ovariectomized rats exhibited a stimulation of the uterine histoarchitecture, a significant cornification in the vaginal epithelium and a reduction of serum LH concentration showing the estrogenic nature of the extract. Furthermore, the administration of the extract in intact female rats provoked a significant modification of the vaginal smear in 67% of treated rats. The estrous cycle thus modified was characterized by a prolonged estrus stage with a temporary reduction of the regular cyclicity.     

Butanolic extract of Pueraria tuberosa DC.: Physiological response in the genital tract of cyclic female rats

Biochemical and physiological alterations have been observed in the genital tract of female cyclic rats treated with butanolic extract of Pueraria tuberosa DC. Its administration caused a significant increase in the glycogen contents, protein concentration, activity of acid and alkaline phosphatase and total cholesterol in the ovary, uterus, cervix and vagina. Further, in contrast to other organs vaginal glycogen decreased significantly. Its administration also stimulated the uterine structures, caused metaplastic changes in the cervical epithelium with marked keratinization and provoked considerable cornification in the vaginal epithelium. These changes have been correlated with anti-implantation action of the butanolic extract in the light of its estrogenic activity.     

Androgenic activity of the Thai traditional male potency herb, Butea superba Roxb., in female rats

Aim of the study

Butea superba Roxb. (Leguminosae) is a well-known Thai male potency herb with androgenic and anti-estrogenic activities. We evaluated whether oral administration of Butea superba has an androgenic or anti-estrogenic activity in female rats.

Materials and methods

Normal and ovariectomized adult female rats were each subdivided into five groups, DW, BS-10, BS-50, BS-250 and TP, and gavaged with 0, 10, 50 and 250 mg/kg BW/day of the crude of Butea superba and subcutaneously injected with 6 mg/kg BW/day of testosterone propionate (TP), respectively, during the treatment period.

Results

In intact rats, only BS-250 increased the uterine thickness and the number of uterine glands, and could induce a prolonged diestrous phase. In ovariectomized rats, treatment with BS-50 as well as BS-250 increased the uterine thickness and the number of uterine glands. However, serum luteinizing hormone (LH) levels were also increased. TP reduced serum follicle stimulating hormone and LH levels with the appearance of anestrous cycle, and could significantly increase the relative uterine weight and thickness and the number of uterine glands in both intact and ovariectomized rats.

Conclusions

Orally administered Butea superba tubers have an androgenic effect on the reproductive organs of intact and ovariectomized rats, and exhibit anti-estrogenic activity on LH secretion in ovariectomized rats.     

Phytochemical analysis and antifertility potential of Cynodon dactylon in female Wistar rats: A herbal approach towards contraception

ObjectiveThe objective of the present study was to evaluate the antifertility activity of ether (ErCD), chloroform (CeCD) and ethyl alcohol (EyCD) extracts of the whole plant of Cynodon dactylon in female Wistar albino rats.MethodsAcute oral toxicity and an antifertility study were performed in female Wistar rats with two dose levels (200 and 400 mg/kg, orally) of EyCD. The estrogenic and progestogenic effects of EyCD were further observed by administering it to immature Wistar rats by investigations of vaginal cornification, hormonal level, uterus weight, biochemical parameters, histopathology of the uterus and deciduoma formation, respectively. Isolation of EyCD was carried out by Flash Chromatography and isolated fraction was estimated by HPLC.ResultsNo toxicity with any of the extract was found up to the dose of 2000 mg/kg body weight. EyCD treated rats exhibited maximum reduction in pregnancy (83.33%). Estimation of EyCD on vaginal cornification, estrogen-induced uterotrophic assay and deciduoma model demonstrated vaginal cornification, significant (P < 0.01) increase in uterine weight and uterine proliferation in histopathology and reduced deciduoma formation respectively. Hormonal and biochemical parameters confirmed the above findings indicating estrogenic potential and antiprogestogenic potential of EyCD that might be attributed to the presence of phytoestrogen (apigenin) in EyCD.ConclusionThe results suggested that extracts of C. dactylon possess significant antifertility activity, which is consistent with the literature reported in folk medicine of this plant in fertility regulation.     

α-玉米赤霉醇对去卵巢大鼠骨代谢生化指标的影响

目的:应用去卵巢大鼠建立绝经后骨质疏松症模型,观察α-ZAL对绝经后骨质疏松症的骨代谢生化指标的影响。方法:40只6月龄雌性SD大鼠随机分为4组:假手术组(Sham)、模型组(OVX)、雌二醇组(OVX+E2)、α-ZAL(OVX+α-ZAL)。术后三周灌胃给予假手术组和模型组生理盐水1mL/100g·d,雌二醇组给予戊酸雌二醇1mg/kg/d,α-ZAL组给予α-ZAL1mg/kg/d。12周后处死动物,分离血清,测定ALP、BGP、TRACP和ICTP等血清骨代谢生化指标。结果:E2组和α-ZAL组TRACP和ICTP较模型显著降低。E2和α-ZAL能降低血清ALP和BGP浓度,但较假手术组升高。结论:α-ZAL对绝经后骨质疏松症模型动物具有与E2类似的调节骨代谢生化指标的作用,提示可能具有广阔的治疗绝经后骨质疏松症的应用前景。     

Antifertility profile of the aqueous extract of Moringa oleifera roots

An aqueous extract of Moringa oleifera roots was investigated for its estrogenic, anti-estrogenic, progestational and antiprogestational activities. Oral administration of extract progressively increased the uterine wet weight of bilaterally ovariectomized rats. This estrogenic activity was supported by stimulation of uterine histo-architecture. When the extract was given conjointly with estradiol dipropionate (EDP), there was a successive reduction in the uterine wet weight when compared to the gain with EDP alone and uterine histological structures were also inhibited. In the deciduoma test, the highest dose of 600 mg/kg interfered with the formation of deciduoma in 50% of the rats, showing some antiprogestational activity. Doses up to 600 mg/kg of the extract orally failed to induce a decidual response in the traumatized uterus of ovariectomized rats. The antifertility effect of the extract appears to be due to multiple attributes.     

Antifertility effect of hydroalcoholic leaves extract of Michelia champaca L.: An ethnomedicine used by Bhatra women in Chhattisgarh state of India

Ethnopharmacological relevance

Michelia champaca L. (family: Magnoliaceae), commonly known as Champa [Hindi], is traditionally used for fertility regulation by the women of Chhattisgarh state in India. No scientific evidence regarding the antifertility effect of this plant is available till date.

Aim of the study

To study the anti-fertility effect of hydroalcoholic leaf extract of Michelia champaca Linn. in female rats.

Materials and methods

The antifertility activity of the extract (HAEMC) administered at dose levels (100 and 200 mg/kg body weight, p.o.) was evaluated in two experimental animal models i.e. antiimplantation activity in female wistar rats and esterogenic/antiestrogenic activity in ovariectomized female rats. In anti-implantation activity, the extract (200 and 400 mg/kg body weight, p.o.) was administered to female rats from 1 to 7 days of pregnancy and on 10th day, laprotomy was performed to count the no. of implants. For estrogenic/anti-estrogenic activity, ovariectomized female rats were administered with the extract at both the doses alone as well as along with 17α-ethinyl estradiol (1 μ/rat/day) for 7 consecutive days. On the 8th day, all animals were sacrificed and blood serum was further processed for the estimation of biochemical parameters such as estrogen level, alkaline phosphates, cholesterol, tryglycerides, total protein etc.

Results

The extract (HAEMC) showed significant (p<0.01) 49.95% and 71.03% antiimplantation activities at 100 and 200 mg/kg doses respectively. The extract also exhibited significant (p<0.01) estrogenic activity as evidenced by increase in body weight, uterine weight, increased thickness and height of endometrium, vaginal cornification and significant (p<0.01) increase in estrogen, cholesterol, alkaline phosphate and triglycerides levels at higher dose when administered alone as well as along with ethinyl estradiol. Phytochemical screening showed the presence of steroids, flavonoids and alkaloids in the extract.

Conclusions

Hydroalchoholic extract of Michelia champaca leaves possesses significant antifertility effect which might be due to the inhibition of implantation and estrogenic effect which in turn might be due to the presence of some phytoconstituents in the plant.     

Molecular and pharmacodynamic properties of estrogenic extracts from the traditional Chinese medicinal herb, Epimedium

The Chinese medicinal herb, Epimedium, used traditionally for bone health exerts estrogenic activity (EA) in vitro. A genetically characterized Epimedium brevicornum (EB) extract induced biphasic responses in the mRNA and protein expression of the estrogen-regulated progesterone receptor gene in breast cancer (MCF-7) cells. These changes were mirrored changes in estrogenic receptor (ERalpha) content. In male Sprague-Dawley rats, administration of the estrogenic prodrug, estradiol valerate increased area-under-curve of serum effects for ERalpha (AUC difference: 18,900EA(ERalpha) min; 95% CI: 0-37,800; p = 0.05) and breast cancer cell (MCF-7) growth (AUC difference: 30,200EA(MCF-7) min; 95% CI: 24,200-36,200; p<0.001), compared to placebo. Oral administration of Epimedium brevicornum increased ERalpha activity (1320EA(ERalpha) min, p<0.01). Our data indicate that estrogen-responsive bioassays can measure the pharmacokinetic/pharmacodynamics of estrogenic activity in serum. Epimedium brevicornum extract increases estrogenic activity in serum and human studies are required to evaluate whether Epimedium extracts have utility for estrogen replacement therapy.     

桂枝加葛根汤治疗椎动脉型颈椎病的疗效观察

目的：观察椎动脉型颈椎病患者服用桂枝加葛根汤前后椎动脉血流改善情况。方法：2008年5月~2010年1月间,将150例椎动脉型颈椎病患者随机分为观察组和对照组,分别施以不同的治疗方法。观察组治疗方案为桂枝加葛根汤口服并配合颈椎牵引,将中药汤剂煎煮后,分两次口服,每日1次,1个月为1个疗程。颈椎牵引取患者体重的1/5~1/7,每日2次,每次30min,3周为1疗程。对照组治疗方案为口服颈复康颗粒配合颈椎牵引,治疗时间同观察组。通过超声经颅多谱勒（TCD）观察椎动脉血流改善情况。结果：通过TCD观察,观察组87例病人治疗后椎动脉各项血流参数均较治疗前有明显改善,差异有统计学意义（P〈0.05）。观察组椎动脉改善情况及临床疗效均明显优于对照组（P〈0.05）。并能明显减轻眩晕症状。结论：桂枝加葛根汤对椎动脉血流改善有显著效果,对椎动脉型颈椎病有明显治疗作用。     

补骨脂对去卵巢大鼠雌激素样作用研究

目的:观察补骨脂对去卵巢大鼠的雌激素样作用。方法:SD雌性大鼠行双侧卵巢摘除术(假手术组只切除卵巢附近脂肪),随机分为去卵巢模型组、补骨脂组(0.59 g.kg)、补佳乐组(0.8 g×10-4 g·kg-1)和假手术组,ig 4周后分别观察大鼠肛温、子宫和肾上腺系数,ELISA法检测血清雌二醇(E2)、黄体生成素(LH)、促卵泡生成素(FSH)水平。结果:模型组大鼠与假手术组比较肛温升高,子宫和肾上腺萎缩,血清中E2水平下降,LH,FSH水平升高。与模型组比较,补骨脂组、补佳乐组大鼠的肛温明显降低(P<0.01),子宫和肾上腺系数明显提高(P<0.05,P<0.01),血中E2浓度明显升高,LH,FSH水平明显降低(P<0.01)。结论:补骨脂能降低去卵巢大鼠的肛温,增加子宫和肾上腺系数,升高血中E2水平并降低LH,FSH水平,表明补骨脂对去卵巢大鼠有雌激素样作用。     

Estrogenic Activity Including Bone Enhancement and Effect on Lipid Profile of Luteolin‐7‐O‐glucoside Isolated from Trifolium alexandrinum L. in Ovariectomized Rats

Luteolin‐7‐O‐glycoside (LG), an abundant component in many edible plants, was found to be one of the major constituents of the aqueous methanol extract of Trifolium alexandrinum L. family Fabaceae, a fodder plant widely cultivated in Egypt. The estrogenic activity of LG concerning the effect on uterotrophy, lipid profile, weight gain and bone enhancement activity was determined in ovariectomized rat model at a dose of 5 mg/kg. Luteolin‐7‐O‐glycoside showed significant estrogenic effect through the preservation of normal uterine weight and plasma estradiol level. It also significantly inhibited the bone turnover markers plasma bone‐specific alkaline phosphatase, plasma osteocalsin, type I procollagen N‐terminal, and C‐telopeptide of type II collagen levels. It induced a significant improvement in plasma lipid profile. The effect of LG was comparable with estradiol with lower effect on uterine weight. Liver and kidney functions revealed a wide safety of LG at this dose level. The present study revealed that LG may be a promising hormone replacement therapy after being examined thoroughly on human. Copyright © 2016 John Wiley & Sons, Ltd.     

补肾健脾中药复方对去势大鼠血清中Bcl-2和Bax水平的影响

目的:探讨补肾健脾中药复方对去势大鼠血清中Bcl-2和Bax水平的影响。方法:48只6月龄的雌性SD大鼠随机分为对照组、模型组、中药组(补肾健脾中药复方)、西药组(雌激素)。治疗12周后,收集左侧股骨、血清分别行骨矿含量、骨密度测量和Bcl-2、Bax水平含量的检测。结果:模型组的骨密度值和骨矿含量均低于对照组(P0.05);中药组和西药组的骨密度值高于模型组(P0.05)。与空白组相比,模型组血清中Bcl-2表达水平下降,Bax表达水平上升(P0.05)。经过药物干预后,中药组和西药组均能提高血清中Bcl-2表达,降低Bax表达(P0.05)。结论:补肾健脾中药复方对去势大鼠血清中Bcl-2和Bax水平的影响作用与雌激素一致,有可能在一定程度上抑制细胞的凋亡。     

In vitro estrogenic activities of Chinese medicinal plants traditionally used for the management of menopausal symptoms

The estrogenic activity of 70% EtOH extracts of 32 traditional Chinese medicinal plants, selected according to their reported efficacy for the treatment of menopausal symptoms, was assessed using a recombinant yeast system with both a human estrogen receptor expression plasmid and a reporter plasmid. Among them, 11 (34%) species proved to be active. Polygonum cuspidatum had the highest estrogenic relative potency (RP) (3.28 x 10(-3)), followed by Rheumpalmatum (3.85 x 10(-4)), Cassia obtusifolia (3.49 x 10(-4)), Polygonum multiflorum (2.87 x 10(-4)), Epimedium brevicornum (2.30 x 10(-4)), Psoralea corylifolia (1.90 x 10(-4)), Cynomorium songaricum (1.78 x 10(-4)), Belamcanda chinensis (1.26 x 10(-4)), Scutellaria baicalensis (8.77 x 10(-5)), Astragalus membranaceus (8.47 x 10(-5)) and Pueraria lobata (6.17 x 10(-5)). The EC(50) value of 17beta-estradiol used as the positive control was 0.205+/-0.025 ng/ml (RP=100). This study gave support to the reported efficacy of Chinese medicines used for hormone replacement therapy.     

Anticonceptive and estrogenic effects of a seed extract of Ricinus communis var. minor.

An ether-soluble fraction of a methanol extract of Ricinus communis var. minor seeds administered subcutaneously to adult female rats and rabbits at doses up to 1.2 g/kg and 600 mg/kg, respectively, in divided doses showed anti-implantation and anticonceptive activities. Laparotomy performed on Day 10 and Day 15 of pregnancy on mated female rats and rabbits treated with the extract did not reveal any uterine implantation sites. The animals were protected against pregnancy for over three gestation periods and among those that later delivered, there was no evidence of abnormality in the pups. In ovariectomized young female rats as well as in immature mice, the extract dose-dependently increased uterine wet weight. Furthermore, the extract induced premature opening of the vagina, increased the number of epithelial cells and cornified cells and decreased the leucocyte number in the vaginal smear. The estrogen-like activities exhibited by the extract were dose-dependent and the anticonceptive effect may be due at least in part to such estrogenic action.