Effects of alpinumisoflavone and abyssinone V-4'-methyl ether derived from Erythrina lysistemon (Fabaceae) on the genital tract of ovariectomized female Wistar rat

Erythrina lysistemon is an African medicinal plant used as a palliative for problems in women. The crude extract of this plant was shown to exhibit estrogenic effects on the female rat reproductive tract and on cell cuture. Using classic chromatographic methods, two compounds have been isolated as major constituents of this extract: alpinumisoflavone (1) and abyssinone V‐4′‐methyl ether (2). To determine whether both compounds are actives principles accounting for E. lysistemon effects, we applied the classic 3‐day uterotrophic assay. We also carried out a ligand binding assay to determine whether the observed effects are estrogen receptor (ER) mediated. This study showed that whereas compound 1 displayed a fourfold preference for ERα, compound 2 bound ERα and ERβ with a same affinity. The in vivo study showed that compound 1 increased the uterine wet weight by 182.23% (p < 0.01) and 71.79% (p < 0.05) at doses of 0.1 and 1 mg/kg BW/day respectively. The uterine epithelium thickened dose‐dependently. Vaginal epithelial height also increased by 369.97 and 226.76% respectively (p < 0.01). Compound 2 acted only on the vagina and increased vaginal epithelial height by 244.56% (p < 0.01) at 1 mg/kg BW/day. These results suggest that compounds 1 and 2 are endowed with estrogenic properties accounting, at least in part, for E. lysistemon effects. Copyright © 2011 John Wiley & Sons, Ltd.     

The use of LeptiCore<Superscript>®</Superscript> in reducing fat gain and managing weight loss in patients with metabolic syndrome

Background

LeptiCore^® is a proprietary combination of various ingredients which have been shown to have properties which could be beneficial to weight loss in obese and overweight human subjects. This study evaluates the effect of Lepticore^® on bodyweight as well as parameters associated with obesity and metabolic syndrome.

Methods

The study was an 8 week randomized, double-blind, placebo-controlled design involving 92 obese (mean BMI > 30 kg/m²) participants (37 males; 55 females; ages 19-52; mean age = 30.7). The participants were randomly divided into three groups: placebo (n = 30), LeptiCore^® formula A (low dose) (n = 31) and LeptiCore^® formula B (high dose) (n = 31). Capsules containing the placebo or active formulations were administered twice daily before meals with 300 ml of water. None of the participants followed any specific diet nor took any weight-reducing medications for the duration of the study. A total of 12 anthropomorphic and serological measurements were taken at the beginning of the study and after 2, 4, 6, and 8 weeks of treatment.

Results

Compared to the placebo group, the two active groups showed statistically significant differences on all 12 variables by week 8. These included four anthropomorphic variables (body weight, body fat, waist and hip size) and eight measures of serological levels (plasma total cholesterol, LDL, HDL, triglycerides, blood glucose, serotonin, leptin, C-reactive protein). The two active groups also showed significant intra-group differences on all 12 variables between study onset and week 8.

Conclusion

The LeptiCore^® formulation at both the low and high dosages appears to be helpful in the management of fat gain and its related complications. The higher dosage resulted in significantly greater reductions in body weight and triglyceride, blood glucose, and C-reactive protein levels, as well as increased serotonin levels.

     

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

Ethnopharmacological relevance

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.

Aim of study

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.

Material and methods

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.

Results

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).

Conclusion

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.     

Polycystic ovary syndrome in pubertal period: clinical, biological, metabolic and genetic polymorphism

Polycystic ovary syndrome (PCOS) is a common cause of hyperandrogenism in adolescent girls. In its complete post menarchal expression, the syndrome is characterized by the association of typical clinical, biological, and ultrasonographic findings. Many factors have contributed to our knowledge of different clinical forms of PCOS in adolescent girls. They are helpful for clarifying misleading situations in a period of life when diagnosis of PCOS implies a treatment for many years and may interfere with gynecological outcome. During the last 3 years, we had the opportunity to manage in our unit 45 adolescent girls with ovarian hyperandrogenism: 32 of them had PCOS and the other 13 functional ovarian hyperandrogenism defined by clinical and biological hyperandrogenism without ultrasonographic abnormality. In this review, we report, from our personal experience as well as from recent literature data, the different clinical expressions of PCOS in the pubertal period: the classical post menarchal form, the exceptional pre menarchal form, the post precocious pubarche and the post precocious puberty forms, the familial expression as well as the dominant metabolic expression.     

Prevention of postoperative pain after thyroid surgery: a double-blind randomized study of bilateral superficial cervical plexus blocks

Local anesthetic infiltration may reduce postthyroidectomy pain. We performed a double-blinded, randomized, placebo-controlled trial to assess the analgesic efficacy of bilateral superficial cervical plexus blocks performed at the end of surgery. Ninety patients undergoing elective thyroid surgery by the same surgeon under general anesthesia were randomized to receive 20 mL isotonic sodium chloride or 20 mL bupivacaine 0.25% with 1:200,000 epinephrine. Postoperative pain was assessed every 4 h using an 11-point numeric rating scale (NRS-11). All patients received acetaminophen every 6 h. In addition, morphine was administered following a standardized protocol if the NRS-11 score was > or = 4. The main outcome variables were pain scores (NRS-11), the proportion of patients given morphine at any time during the 24-h period, and the amount of morphine administered. The Bupivacaine group had a smaller proportion of patients given morphine (66.0% vs 90.0%; P = 0.016), and lower initial median pain scores (P = 0.002). We conclude that bilateral superficial cervical plexus blocks significantly reduce pain intensity in the postoperative period after thyroid surgery but do not provide optimal pain relief alone.     

Evidence that testosterone modulates in vivo the adenylate cyclase activity in fat cells

In male hamster fat cell membranes, the alpha 2-adrenoreceptor-mediated inhibitory response of adenylate cyclase was almost completely suppressed by castration and was restored to control values after testosterone treatment, whereas the cyclase inhibitory response to nicotinic acid was insensitive to androgenic status. Basal and forskolin-, guanylylimidodiphosphate- and isoproterenol-stimulated cyclase activities were decreased by 30-40% after castration and restored to control values after testosterone treatment. In addition, Mn2+ + forskolin-stimulated activity in the presence or absence of GDP beta S was lower (-30%) after castration and normalized after testosterone treatment. Finally, the effects of testosterone described above were completely abolished when the potent androgen receptor antagonist RU 23908 was administered together with testosterone. These results indicate that both the inhibitory and stimulatory responses of adenylate cyclase are promoted by testosterone through an androgen receptor-dependent mechanism; promotion of the inhibitory response concerns specifically the alpha 2-receptor-mediated pathway, whereas promotion of the stimulatory response appears unspecific and mainly due to increased activity of the cyclase catalytic subunit.