In Combo Studies for the Optimization of 5-Aminoanthranilic Acid Derivatives as Potential Multitarget Drugs for the Management of Metabolic Syndrome.

Metabolic syndrome is a set of risk factors that consist of abdominal obesity, arterial hypertension, alterations in the lipid profile, and hyperglycemia. The current therapeutic strategy includes polypharmacy, using three or more drugs to control each syndrome component. However, this approach has drawbacks that could lead to therapeutic failure.

High Fructose and High Fat Diet Impair Different Types of Memory through Oxidative Stress in a Sex- and Hormone-Dependent Manner.

Metabolic syndrome (MetS) contributes to the spread of cardiovascular diseases, diabetes mellitus type 2, and neurodegenerative diseases. Evaluation of sex- and hormone-dependent changes in body weight, blood pressure, blood lipids, oxidative stress markers, and alterations in different types of memory in Sprague-Dawley rats fed with a high fat and high fructose (HFHF) diet were evaluated. After 12 weeks of feeding the male and female rats with HFHF, body weight gain, increase in blood pressure, and generation of dyslipidemia compared to the animals fed with chow diet were observed.

In Silico-Based Design and In Vivo Evaluation of an Anthranilic Acid Derivative as a Multitarget Drug in a Diet-Induced Metabolic Syndrome Model.

Metabolic syndrome (MetS) is a complex disease that affects almost a quarter of the world's adult population. In MetS, diabetes, obesity, hyperglycemia, high cholesterol, and high blood pressure are the most common disorders. Polypharmacy is the most used strategy for managing conditions related to MetS, but it has drawbacks such as low medication adherence.

Hormone catalysis: role of protecting and modifying reagents of sulfhydryl groups on estrogen receptor in breast cancer.

We have studied the modulation and differential sensitivity of the estrogen receptor (ER) in breast cancer in the presence of protecting or modifying agents of disulfide bonds and sulfhydryl groups present in the ER steroid-binding domain. Protecting agents such as mercaptoethanol and dithiotreitol increased the [(3)H]estradiol binding to ER by 25% and 50%, respectively. Modifying agents such as p-chloromercuribenzensulfonate decreased the [(3)H]estradiol binding by 70% and this was nearly completely abolished by N-ethylmaleimide (94%).

The role of progesterone in endometrial estradiol- and progesterone-receptor synthesis in women with menstrual disorders and habitual abortion.

The objective of this comparative study was to determine the influence of changes in estradiol and progesterone during ovulatory vs. anovulatory cycles on levels of estradiol receptor (ER) and progesterone receptor (PgR) in endometrium. Thirty women (range age 20-35 years) were divided into three groups: women with a history of habitual abortion, obese women with menstrual disorders, and women with regular ovulatory cycles as well as proven fertility.

Endometrium estradiol receptors type I and type II during early pregnancy of rat.

By centrifugation in a sucrose density gradient we studied the citosol 17beta-estradiol binding sites of blastocyst receptive and non-receptive endometrial zones, as well as uterine horn endometrium whose ovary was extirpated three weeks before pregnancy. The cytosol was prelabelled with [3H]-17beta-estradiol 2 and 25 nM. In this work two incubation temperatures were studied.

Endometrial thickness of postmenopausal breast cancer patients treated with tamoxifen.

The effect of administration time of tamoxifen was assessed in 52 postmenopausal patients with mammary cancer in order to evaluate its effect on endometrium and serum levels of luteinizing hormone (LH), follicle-stimulating hormone (FSH) and estradiol. Mean age of the patients was 61.5 years, 23% had a history of smoking, mean body mass index (BMI) was 26.