Recent Patents on Endocrine, Metabolic & Immune Drug Discovery

Cushing's Syndrome (CS) is associated with a specific spectrum of dementia-like symptoms, including psychiatric disorders, such as major depression, anxiety and mania, and neurocognitive alterations, like impairment of memory and concentration. This pattern of clinical complications, which significantly impair the health-related quality of life of CS patients, is sometimes referred to as "steroid dementia syndrome" (SDS). The SDS is the result of anatomical and functional anomalies in brain areas involved in the processing of emotion and cognition, which are only partially restored after the biochemical remission of the disease...

BACKGROUND: Over the last decades an increasing body of evidence suggested a possible relationship between thyroid hormone (TH) and the ageing process, and several efforts have been made to determine the actual role of TH dynamic during human life. It is still unclear whether the serum level shift of Thyroid Stimulating Hormone toward higher value, observed during ageing, is a normal adaptive response associated with senescence or an actual mild thyroid dysfunction. A growing body of evidence supports the hypothesis of a reset of the hypothalamus-pituitary-thyroid axis in order to contrast the catabolic status of the ageing process...

BACKGROUND: Parkinson's disease is a chronic neurodegenerative disorder characterized by a progressive loss of dopaminergic neurons. The pathophysiological mechanisms underlying Parkinson's are still unknown. Mitochondrial dysfunction, abnormal protein aggregation, increased neuroinflammation and impairment of brain glucose metabolism are shared processes among insulinresistance, diabetes and neurodegeneration and have been suggested as key mechanisms in development of Parkinson's and cognitive impairment...

BACKGROUND: Alzheimer's disease (AD) is the most frequent type of dementia in people over 65 years of age; type 2 diabetes mellitus is a metabolic condition affecting 382 million of adults worldwide. Glucose is the main substrate for energy for the brain, which consumes 25% of the body's glucose. Glucose metabolism, evaluated using Positron Emission Tomography (PET) scanning using 18F-fluorodeoxyglucose ([18F]-FDG) is commonly used for diagnosis and follow up in AD. Epidemiological and pathophysiological studies showed a link between AD and diabetes, particularly in relation to insulin resistance...

BACKGROUND: Heart Failure (HF) and cognitive impairment (CI) represent two high incident diseases worldwide, with extremely elevated mortality and morbidity rates. Their prevalence is expected to further increase in the next years due to the aging population, thus they pose enormous clinical, social and economic challenges. Sympathetic nervous system hyperactivity is known to play a pivotal role in HF pathophysiology and progression. In fact, increased cardiac and circulating catecholamine levels are responsible for several molecular and structural abnormalities with detrimental effects on the failing heart...

INTRODUCTION: A new method of reduction of tumor necrosis factor alpha activity via intradermal immunization with inactivated autoleukocytes (patent UA97493 (2015) [1]) has been presented in the article. New patents from various countries have been analyzed [2-7]. OBJECTIVE: Patients with psoriasis (24) with high level of tumor necrosis factor alpha in their blood (. 30pg/ml) were immunized with autoleukocytes. METHOD: Leukocytes were isolated by centrifuging plasma, obtained after precipitation of a patient's heparinized peripheral venous blood...

BACKGROUND: Inflammation is an innate immune response which is considered a common basis for several diseases such as ageing, diabetes, obesity, gout, neurodegenerative diseases and others. Among other platforms, inflammasomes are part of a superfamily of Pattern Recognition Receptors (PRR) and act as cytoplasmatic sensors for stimulation with Pathogen Associated Molecular Pattern (PAMPs) and/or Danger/Damage-Associated Molecular Patterns (DAMPs) leading to an infectious/ pathogenic or sterile inflammation...

Lipodystrophies are a heterogeneous group of disorders characterized by congenital or acquired loss of adipose tissue. Recently, metreleptin, a recombinant human leptin analog, has been approved for the treatment of patients with generalized lipodystrophy. Leptin is an adipokine which has a fundamental role in glucose and lipid homeostasis. Metreleptin treatment has been demonstrated to improve metabolic abnormalities such as hyperglycemia, hypertriglyceridemia, increased hepatic fat content and elevated liver enzymes alanine transaminase and aspartate transaminase in patients with generalized lipodystrophy, and to correct hyperphagia that likely occurs as a result of leptin deficiency...

BACKGROUND: Adjudin has been explored as a male contraceptive for the last 15 years since its initial synthesis in the late 1990s. More than 50 papers have been published and listed in PubMed in which its mechanism that induces exfoliation of germ cells from the seminiferous epithelium, such as its effects on actin microfilaments at the apical ES (ectoplasmic specialization, a testis-specific actin-rich anchoring junction) has been delineated. OBJECTIVE: Recent studies have demonstrated that, besides its activity to induce germ cell exfoliation from the seminiferous epithelium to cause reversible infertility in male rodents, adjudin possesses other biological activities, which include anti-cancer, anti-inflammation in the brain, and anti-ototoxicity induced by gentamicin in rodents...

Nuclear lamins, namely lamins A, B and C, surround the nucleoplasmic contents in a meshlike network called the nuclear lamina. These intermediate filaments provide a structural framework to the nuclear envelope (NE), play a role in arrangement of the chromatin within the nucleus, in DNA replication and also participate in DNA damage repair. In order for lamins to be involved in these important nuclear processes and to be functionally active, they undergo a series of post-translational modifications (farnesylation, endoproteolytic cleavage, carboxylmethylation etc...

Congenital adrenal hyperplasia (CAH) is one of the most common diseases transmitted in an autosomal recessive manner and is caused by mutations of enzymes which are responsible for the process of adrenal steroidogenesis. According to the impairment of enzymes involved in steroidogenesis, several types of CAH can be distinguished. The most common type is associated with mutations in the CYP21A2 gene, encoding 21-hydroxylase enzyme and has different clinical forms: Classical (in which there are two types: salt wasting and simple virilization) and non-classical, characterized by less severe symptoms and late onset...

Leishmaniasis is considered a neglected tropical disease having a worldwide distribution. The disease is caused by protozoa belonging to the genus Leishmania, being clinically divided into visceral leishmaniasis (VL), cutaneous leishmaniasis (CL) and mucocutaneous leishmaniasis (MCL). Domestic dogs are the main parasite reservoir and effectively participate in the protozoa transmission. The human leishmaniasis treatment is based on a selection of therapeutic compounds, but the available drugs are toxic, presenting adverse side effects...

Inflammatory bowel disease (IBD) is a chronic intestinal inflammatory disease in humans constituting a major health concern today whose prevalence has been increasing over the world. Production of reactive oxygen species (ROS) and disturbed capacity of antioxidant defense in IBD subjects have been reported. Antioxidants may play a significant role in IBD treatment. This study aimed at evaluating ameliorative effects of intraperitoneal resveratrol pretreatment on trinitrobenzene sulphonic acid (TNBS)-induced colitis in rats...

Osteoporosis diagnosis, which is nowadays generally made based on bone mineral density (BMD) measurements, suffers from certain limitations. Thus it is believed that bone turnover markers (BTMs) can help improve osteoporosis detection. The shifting interest toward this topic made us perform a review to gather information on existing markers and their role in osteoporosis diagnosis. Based on the results, in this review, a list of existing markers and some of their characteristics is provided. Moreover, a brief explanation of different types of variability met while using these markers is also described...

Current study has invented a new method for utilizing spot urine protein among diabetic patients. There have been various efforts and strategies in research internationally to detect, diagnose and monitor nephropathy/DKD. Although 24-hour urine studies are gold standard, however, there exist some controversies about microalbuminuria and spot urine protein. The current study was designed to utilize spot urine protein among diabetic patients and to find its association with routine dipstick urine test for albumin, and microalbuminuria...

Sulforaphane (SFN) is a molecule within the isothiocyanate (ITC) group of organosulfur compounds. SFN is a phytochemical commonly found in cruciferous vegetables such as broccoli, brussels sprouts and cabbages. It has been widely studied in order to evaluate its chemopreventive properties and some of those have already been established by means of animal and human models. The SFN induces Phase I and II enzymes involved in detoxification processes of chemical carcinogens in order to prevent the start of carcinogenesis...

OBJECTIVE: Assess the state of the art on the relationship between infertility and the sexual function of couples. DATA SOURCES: The PubMed, Lilacs, and Google Scholar databases were searched for articles that assessed the sexual function of infertile couples (IC). Recent patents on this subject were assessed. STUDY SELECTION: Quantitative studies published in the English language (case-control, cross-sectional, cohort, multicenter, observational studies, randomized controlled trials, meta-analyses, systematic reviews) that used structured and semi-structured questionnaires for quantitative assessment of the sexual function of infertile couples were identified using the search terms: "infertile couple" and "sexuality", "sexual dysfunction", "sexual function", "sexual disorder", "hypoactive sexual desire"...

Amyotrophic Lateral Sclerosis (ALS) or Lou Gehrig's disease is an axonopathy with adultonset, progressive and irreversible degeneration of upper and lower motor neurons. Around 90% of ALS is considered as sporadic ALS (sALS) without apparent genetic cause while in the familial type of ALS (fALS) at least one affected blood relative needs to be identified. Both sALS and fALS show similar progression and pathological profile. Biochemical and immunological roles have been reported for both types of ALS. It has been suggested that mutation in SOD1 gene would be responsible for the oxidative stress and neurotoxicity...

Glomerulopathy is the third most important cause of kidney disease. Proteinuria is the hallmark of glomerular damage, and a marker of progression of kidney disease, cardiovascular morbidity and mortality. Strategies to reduce proteinuria are partially successful, and despite proteinuria management, renal disease may still progress. Immunosuppression to treat glomerulopathies is nonspecific, partially effective and presents side-effects. It is critical to find safe drugs with specific podocyte molecular targets...

Cancer is a leading cause of death in the population and despite the significant technological advances that have been made over the last years, there is a great need for new and better treatments with fewer side effects. Among the various types, hormone-dependent cancers are stimulated by the presence of certain steroidal hormones such as androgens and estrogens, which act through a nuclear receptor. The use of small molecules to block the biosynthesis (steroidogenesis) or the action of hormones (androgens or estrogens) is a therapeutic approach that has yielded interesting results and whose development continues...