ecdysterone and Metabolic-Syndrome

Beside ecdysone (1), ecdysterone (2) is one of the most common 5beta-cholest-7-en-6-one (ecdysteroid) derivatives, which, besides having a hormonal effect on invertebrates, possesses a number of favorable non-hormonal biological effects on mammals. The most interesting of these is that on degenerative diseases, one of which, up to now not clarified in detail, is the so-called adaptogenic effect (protection of the organism against adverse stress factors) associated with anabolic, gastroprotective, and antioxidant effects. A second group of favorable effects is the possibility of suppression of neurodegenerative processes and protection of the cardiovascular system (metabolic syndrome symptom suppression, antidiabetic activity, and protection of heart and blood vessels). Because of these properties, ecdysterone has the potential to be developed as a medicinal agent.

Topics: Anabolic Agents; Animals; Antioxidants; Cardiovascular System; Diabetes Mellitus; Ecdysterone; Humans; Hypoglycemic Agents; Metabolic Syndrome; Neurodegenerative Diseases; Ulcer

Topics: Animals; Biological Availability; Ecdysterone; Gerbillinae; Metabolic Syndrome; Tandem Mass Spectrometry

The aim of this study was to reveal the effects of obesity and phytotherapy with 20-hydroxyecdysone (20E) on the nuclei of adrenal zona fasciculata (ZF) in the gerbil Gerbillus tarabuli by analyzing nuclear shape and gray-level co-occurrence matrix (GLCM) texture characteristics and by quantifying heterochromatin. Twelve gerbils were divided into three groups: control (C), HC and HC-20E (animals receiving a high-calorie-diet without or with a supplement of 20E, respectively). The adrenals were removed and fixed for histological and statistical analysis. Principal component analysis showed a positive correlation of area, perimeter and textural correlation in C. Nevertheless, a negative correlation was recorded for contrast and entropy. The obesity caused a disorder in nuclear texture; negative correlation was noted with heterochromatin fraction, which may be related to increased ZF activity. However, administration of 20E seems to improve the nuclear state by preserving circularity, uniformity and homogeneity of nuclei as well as the proportion of heterochromatin, which could be a sign of a downregulation of cell activity.Our results suggest that new techniques of image processing could contribute to the understanding of nuclear changes associated with obesity and its possible therapy in this gerbil model for metabolic syndrome.

Topics: Animals; Ecdysterone; Gerbillinae; Heterochromatin; Metabolic Syndrome; Obesity; Zona Fasciculata

Ecdysteroids are polyhydroxylated steroids present in invertebrates and plants. 20-Hydroxyecdysone (20E) is the most common and the main biologically active compound of ecdysteroids. Previous studies have demonstrated anabolic and metabolic effects of 20E in mammals. However, it is unknown whether 20E has a positive effect on all aspects of cardiometabolic syndrome. The aims of this study were to investigate the favorable effect and possible underlying mechanisms of 20E in a rat model of cardiometabolic syndrome (CMS) induced by a high-calorie diet combined with female sex hormone deprivation.. 20E (5 mg/kg, 10 mg/kg, or 20 mg/kg) or pioglitazone (PIO) (10 mg/kg) was intragastrically administered to sham-operated Sprague-Dawley female rats and ovariectomized rats fed a high-fat-high-fructose diet (OHFFD) for 8 weeks. The phenotypic characteristics of CMS, including central adiposity, blood pressure, serum lipid profile, glucose tolerance, insulin action on skeletal muscle glucose transport activity and hepatic protein expression, were determined.. Some CMS characteristics were improved by 20E treatment. Rats treated with 20E had lower body weight, abdominal fat accumulation than rats treated with vehicle control without changes in total caloric intake and fat-free mass. OHFFD rats exhibited high blood pressure, but 20E-treated rats maintained normal blood pressure with a lower level of low-density lipoprotein (LDL)-cholesterol. Although 20E showed no positive effect on inducing insulin-mediated glucose transport in the skeletal muscle of OHFFD rats, 20E improved whole body glucose homeostasis. Analysis of protein expression in livers from 20E-treated rats revealed significantly increased expression of pAkt Ser. 20E treatment can alleviate cardiometabolic disorder caused by a high-fat-high-fructose diet and female sex hormone deprivation. In particular, 20E helps improve whole body insulin sensitivity in OHFFD rats, and the mechanisms that underlie this favorable effect are potentially mediated by the activation of AMPK and FGF21. The present study indicates that 20E could be an alternative therapeutic option for the prevention and alleviation of cardiometabolic syndrome.

Topics: Animals; Blood Pressure; Diet, High-Fat; Disease Models, Animal; Ecdysterone; Female; Fructose; Metabolic Syndrome; Ovariectomy; Rats; Rats, Sprague-Dawley

Postmenopausal women develop often obesity which may be prevented by 20-OH-Ecdysone (Ecd). This was investigated in ovariectomized (ovx) rats. They were orally treated with 3 doses of Ecd (18, 56 or 116 mg/day/animal). Positive controls received 159 microg estradiol (E2). Quantitative computer tomography at the level of the abdomen and the metaphysis of the tibia allowed estimation of surface, fat depots and muscles. The highest dose of Ecd resulted in serum concentrations of 0.4 x 10(-6)M. Serum E2 concentrations in the positive controls were 73.3+/-24.41 pg/ml. E2 but not Ecd stimulated uterine weights. Under Ecd ovx animals gained less fat but had more muscle mass. Serum TSH, T4 and T3 levels remained unaffected while E2 treatment increases T4 but decreases T3 levels. Ecd at the lowest dose lowered serum LDL and did not result in increased serum triglycerides, an effect seen in the E2 treated rats. At the Ecd highest dose serum HDL was higher than in the controls. In conclusion Ecd has beneficial effects on fat and muscle tissue and may be able to prevent the metabolic syndrome and sarcopenia by a non-estrogenic mechanism.

Topics: Animals; Body Composition; Dose-Response Relationship, Drug; Ecdysterone; Estrogens; Female; Hindlimb; Intra-Abdominal Fat; Leptin; Lipids; Metabolic Syndrome; Obesity; Organ Size; Ovariectomy; Postmenopause; Rats; Rats, Sprague-Dawley; Sarcopenia; Thyroid Hormones; Thyrotropin; Uterus