Activity based evaluation of a traditional Ayurvedic medicinal plant: Saraca asoca (Roxb.) de Wilde flowers as estrogenic agents using ovariectomized rat model.

Saraca asoca (Roxb.) de Wilde, Ashok, is a popular traditional plant used for gynecological disorders. In India, the juice of Ashok flowers is traditionally consumed as a tonic by women in case of uterine disorders. But despite the use, its estrogenic potency is not yet evaluated and thus lacks the scientific recognition and acclaim. This study is designed to investigate the estrogenic potential of standardized ethanolic extract of Saraca asoca flowers (SAF) using ovariectomized (OVX) female albino Wistar rat model. Saraca asoca flowers were extracted in ethanol using hot maceration technique and the extract was standardized in terms of content of four phytoestrogens like quercetin, kaempferol, β-sitosterol and luteolin using HPTLC technique. Safety of the extract was evaluated at a dose of 2000mg/kg body weight in female albino Wistar rats as per the OECD guidelines. Bilateral ovariectomy surgery was performed for the excision of both the ovaries. The OVX animals were treated with the ethanolic extract of SAF at three dose levels- 100mg/kg, 200mg/kg and 400mg/kg body weight in distilled water as a vehicle, orally once a day for two weeks. Estradiol valerate was employed as a modern drug for comparative evaluation of the results. Estrogenic potency was studied by assaying the activities of serum and plasma marker enzymes and hormones viz. G6PDH, LDH, 17β-estradiol, progesterone along with cholesterol, triglycerides and HDL, and vaginal cornification. The uterotrophic effect was evaluated by studying the histoarchitecture of the uterus, effect on uterine weight and changes in the levels of uterine glycogen content. HPTLC revealed the presence of markers like quercetin, kaempferol, β-sitosterol and luteolin from the ethanolic extract of SAF. The content of the four markers was found to be 1.543mg/g, 0.924mg/g, 4.481mg/g and 2.349mg/g, respectively. SAF extract was found to be safe at an oral dose of 2000mg/kg body weight in rats. Among the three doses administered to ovariectomized rats, treatment with high dose was found to be more efficacious when compared with ovariectomized rats. The findings of this study firmly support the estrogenic potency of ethanolic extract of SAF which may be by the reason of phytoestrogens.

Swar G ，Shailajan S ，Menon S 《-》

Eriosema laurentii De Wild (Leguminosae) methanol extract has estrogenic properties and prevents menopausal symptoms in ovariectomized Wistar rats.

Eriosema laurentii De Wild (Leguminosae) is a medicinal plant used in West and Central Africa for different diseases. In Cameroon, this plant is used as a treatment for infertility, and various gynecological and menopausal complaints. However, despite this use as a natural remedy, the biological activity of Eriosema laurentii has not been studied until now. In order to determine the potential use of this plant in gynecological conditions/disorders, we evaluated the estrogenic properties of a methanol extract of its aerial parts and its ability to prevent different menopausal health problems induced by bilateral oophorectomy. Two approaches were used. In vitro, recombinant yeast systems were applied, featuring either the respective human receptors (ERα, AR, and PR) or into chromosome III integrated human aryl hydrocarbon receptor (AhR) and the respective reporter plasmid. In vivo, the investigation was carried out using the 3 days uterotrophic assay and 9 weeks oral treatment in ovariectomized rats. The results showed that the methanol extract of the aerial parts of Eriosema laurentii transactivated the estrogen receptor-α and displayed AhR agonistic activity but was neither androgenic nor progesteronic. In rats, the extract did not induce endometrium proliferation either in the 3-day or the 9-week treatment regimens, but induced vaginal stratification and cornification, prevented loss of femur bone mass, increased high density lipoprotein cholesterol (HDL-C), and reduced total cholesterol (TC), low density lipoprotein cholesterol (LDL-C), TC/HDL-C ratio, LDL-C/HDL-C ratio and the atherogenic index of plasma (AIP). These results suggest that the methanol extract of the aerial parts of Eriosema laurentii does not seem to have an undesirable influence on the endometrium but might prevent vaginal dryness and bone mass loss and improve the lipid profile.

Ateba SB ，Njamen D ，Medjakovic S ，Hobiger S ，Mbanya JC ，Jungbauer A ，Krenn L ... -  《-》

In vivo estrogenic-like activities of Gouania longipetala Hemsl. (Rhamnaceae) bark extracts in a post-menopause-like model of ovariectomized Wistar rats.

Gouania longipetala is commonly used in Cameroonian traditional medicine to manage women fertility and menopausal complaints. However, despite this use, the estrogenic properties of G. longipetala have not been studied until now. The present study was aimed to assess estrogenic activities of the stem bark aqueous (GLA) and ethanolic (GLE) extracts of G. longipetala in post-menopause-like model of ovariectomized (Ovx) Wistar rats. Animals were either sham-operated or Ovx. 84 days after ovariectomy, animals were divided into seven groups of five animals and were daily treated for 28 days with distilled water (10 mL/kg) for group 1, 2% solution of Tween 80 (10 mL/kg) for group 2, estradiol valerate (1 mg/kg) for group 3, GLA (45 or 180 mg/kg) and GLE (40 or 160 mg/kg) for groups 4 to 7 respectively. Sham-operated animals daily received distilled water (10 mL/kg). During the experimental period, the body weight was registered every week. At the day 29, blood pressure was registered by invasive method while uterine and vagina morphometry as well as body, uterine and abdominal fat weights changes were analyzed. Serum levels of total cholesterol, triglycerides, HDL-cholesterol and LDL-cholesterol were determined. Moreover, oxidative stress markers such as nitrites, reduced glutathione (GSH) and malondialdehyde (MDA) were measured in homogenized liver and aorta. Compared with the sham control, vagina and uterine dystrophy and elevated blood pressure were observed in Ovx rats treated with vehicles. Biochemical parameters showed a significant increase of total cholesterol, triglycerides, LDL-cholesterol and MDA as well as a significant decrease of nitrites and GSH in Ovx animals treated with vehicle as compared to sham group. GLA and GLE displayed estrogen-like effects on vagina and did not affect uterine wet weight and epithelial height compared with vehicle groups. Both extracts displayed anti-atherogenic properties by reducing AI, AIP and LDL-cholesterol level as compared to vehicles groups. GLA and GLE significantly prevented the increase of MDA induced by ovariectomy as compared to rats treated with vehicles. This study showed that GLA and GLE exhibited estrogenic effects by providing vaginal lubrication, by modulating blood pressure and improving lipid profile, oxidative status and endothelial function and may not have an undesirable influence on the endometrium in ovariectomized rats.

Paul Désiré DD ，Yolande Sandrine MN ，Danielle Claude B ，Mireille K ，Oumarou Bibi-Farouck A ，Théophile D ，Pierre K ... -  《-》

Serum lipidomics analysis of ovariectomized rats under Curcuma comosa treatment.

Curcuma comosa Roxb. (C. comosa) or Wan Chak Motluk, Zingiberaceae family, has been used in Thai traditional medicine for the treatment of gynecological problems and inflammation. This study aimed to investigate the therapeutic potential of C. comosa by determining the changes in the lipid profiles in the ovariectomized rats, as a model of estrogen-deficiency-induced hyperlipidemia, after treatment with different components of C. comosa using an untargeted lipidomics approach. Lipids were extracted from the serum of adult female rats subjected to a sham operation (SHAM; control), ovariectomy (OVX), or OVX with 12-week daily doses of estrogen (17β-estradiol; E2), (3R)-1,7-diphenyl-(4E,6E)-4,6-heptadien-3-ol (DPHD; a phytoestrogen from C. comosa), powdered C. comosa rhizomes or its crude ethanol extract. They were then analyzed by liquid chromatography-mass spectrometry, characterized, and subjected to the orthogonal projections to latent structures discriminant analysis statistical model to identify tentative biomarkers. Levels of five classes of lipids (ceramide, ceramide-1-phosphate, sphingomyelin, 1-O-alkenyl-lysophosphatidylethanolamine and lysophosphatidylethanolamine) were elevated in the OVX rats compared to those in the SHAM rats, while the monoacylglycerols and triacylglycerols were decreased. The E2 treatment only reversed the levels of ceramides, whereas treatments with DPHD, C. comosa extract or powder returned the levels of all upregulated lipids back to those in the SHAM control rats. The findings suggest the potential beneficial effects of C. comosa on preventing the increased ceramide levels in OVX rats, a possible cause of metabolic disturbance under estrogen deficiency. Overall, the results demonstrated the power of untargeted lipidomics in discovering disease-relevant biomarkers, as well as evaluating the effectiveness of treatment by C. comosa components (DPHD, extract or powder) as utilized in Thai traditional medicine, and also providing scientific support for its folklore use.

Vinayavekhin N ，Sueajai J ，Chaihad N ，Panrak R ，Chokchaisiri R ，Sangvanich P ，Suksamrarn A ，Piyachaturawat P ... -  《-》

Effect of Saraca asoca (Asoka) on estradiol-induced keratinizing metaplasia in rat uterus.

Shahid AP ，Salini S ，Sasidharan N ，Padikkala J ，Raghavamenon AC ，Babu TD ... -  《-》