Preclinical safety evaluation of drone brood homogenate and justification of pharmacological action

The problem of studying the metabolic syndrome, as well as its integration into other pathological processes, despite large-scale research, remains relevant. The complexity of the interaction of different links in pathogenesis requires scientists to find new tools and methods for both diagnosis and treatment. Drone brood homogenate, which is a multifactorial pharmacological agent in terms of chemical composition, seems to be promising to study for today. And the lack of contraindications and a wide age range makes it an excellent object of research. The current study evaluated the pharmacological aspects of safety: acute toxicity, effects on the functional and motor activity of the gastrointestinal tract, as well as local irritation of the gastric mucosa, the secretory function of the stomach. All experiments were performed according to the classical methods. The specific pharmacological activity of the drone brood homogenate was determined in comparison with metformin in the experimental fructose metabolic syndrome. Animals obtained from the Vivarium of I.Horbachevsky Ternopil National Medical University were used to implement the set goals. Working with animals was met all bioethical requirements. The study found that the lyophilized drone brood homogenate does not have a local irritant effect and does not cause ulcers on the surface of the gastric mucosa, does not affect the secretory function of the stomach and motor-evacuatory activity of the gastrointestinal tract and is a low-toxic substance, indicating the possibility of its long-term safe use. As expected, glucose, insulin, and HOMA index were significantly increased in animals that were simulated metabolic syndrome. The use of drone brood homogenate by animals contributed to a relatively positive effect on selected indicators of the metabolic syndrome. Accordingly, drone brood homogenate is a promising active pharmaceutical ingredient for the normalization of biochemical disorders in metabolic syndrome.

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Microcirculation: nexus of comorbidities in diabetes

AJP Renal Physiology ◽

10.1152/ajprenal.00503.2006 ◽

2007 ◽

Vol 293 (2) ◽

pp. F486-F493 ◽

Cited By ~ 14

Author(s):

Constance Temm ◽

Jesus H. Dominguez

Keyword(s):

Metabolic Syndrome ◽

Large Scale ◽

Interstitial Fibrosis ◽

Peritubular Capillary ◽

Tubular Atrophy ◽

The Metabolic Syndrome ◽

Peritubular Capillaries ◽

Obese Rats ◽

Capillary Dysfunction

Generalized capillary dysfunction is a morbid element in the metabolic syndrome, and it is likely involved in its complications. We tested the hypothesis that vast amounts of serum albumin previously observed in kidneys of rats with the metabolic syndrome were caused, in part, by leakage from renal peritubular capillaries. We report herein large scale leaks of plasma fluid in peritubular capillaries of rats with the metabolic syndrome. This finding was directly demonstrated in vivo, and the presence of leftover albumin residue confirmed the leak in postmortem kidney specimens. Moreover, renal interstitial fibrosis and tubular atrophy were found in a distribution similar to the leaked renal albumin in obese rats. We suggest that there is an important link between peritubular capillary damage and interstitial fibrosis, represented as tubulointerstitial disease in the metabolic syndrome. We propose that maintenance of the peritubular microcirculation may improve renal outcomes in diabetes and the metabolic syndrome.

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Evidence for substantial effect modification by gender in a large-scale genetic association study of the metabolic syndrome among coronary heart disease patients

Human Genetics ◽

10.1007/s00439-003-1026-1 ◽

2003 ◽

Vol 114 (1) ◽

pp. 87-98 ◽

Cited By ~ 70

Author(s):

Jeanette J. McCarthy ◽

Joanne Meyer ◽

David J. Moliterno ◽

L. Kristin Newby ◽

William J. Rogers ◽

...

Keyword(s):

Metabolic Syndrome ◽

Coronary Heart Disease ◽

Heart Disease ◽

Association Study ◽

Genetic Association ◽

Genetic Association Study ◽

Large Scale ◽

Substantial Effect ◽

Effect Modification ◽

The Metabolic Syndrome

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MODERN ONCO DRUG FOR INTERNAL USE

Pharmacy & Pharmacology ◽

10.19163/2307-9266-2018-6-5-440-461 ◽

2018 ◽

Vol 6 (5) ◽

pp. 440-461

Author(s):

O. L. Orlova ◽

L. L. Nikolaeva ◽

L. A. Korol ◽

M. V. Dmitrieva ◽

A. P. Polozkova ◽

...

Keyword(s):

Gastrointestinal Tract ◽

Oral Administration ◽

Anticancer Drugs ◽

Active Pharmaceutical Ingredient ◽

Pharmacological Action ◽

The Body ◽

Cytotoxic Drugs ◽

New Drugs ◽

Oral Dosage ◽

Tissue Reactions

Despite the development of biotherapy, chemotherapy remains one of the main methods of treatment of cancer patients. Currently, there are more than 100 anticancer drug substances, however, every year new drugs enter clinical practice and various therapeutic regimens are tested, expanding the possibilities of therapy and improving the results of treatment. Therefore, the adequate use of modern chemotherapy requires constant updating of information about anticancer drugs and methods of their use. Oral administration of drugs is the most natural and convenient way to introduce drugs into the human body. There are about 75% of orally administered drugs that have the ability to be absorbed in the gastrointestinal tract within 1−3 hours after administration. Oral dosage forms (DF) are most common due to the relative simplicity of their production, convenience of use, accuracy of dosing and high stability. Therefore, pharmaceutical companies often reproduce generics in the form of tablets and capsules for oral administration. However, most active pharmaceutical ingredient (API) are destroyed by the action of the gastrointestinal tract environment, which makes it impossible to use the oral administration. This review of the literature describes the main groups of anticancer drugs that are effective when taken orally.The aimof the study is to compile the information on the main groups of anticancer drugs used internally.Materials and methods.The object of the study was well-known anticancer drugs approved for oral administration. The study was conducted using search information and library databases (eLibrary, PubMed, CyberLeninka, ResearchGate), as well as State Register of Medicinal Remedies.Results and discussion.Analyzing the arsenal of cytotoxic drugs, it should be noted that antitumor substances are characterized by high chemical lability they are photosensitive, heat-labile, hygroscopic and hydrolytically unstable. These properties complicate both obtaining reproducible therapeutic effect when taken orally and technological inprocesses. In addition, anticancer drugs have mutagenic, teratogenic, sensitizing and allergenic effects.Conclusion.Lack of sufficient selectivity of the antitumor effect of cytotoxic drugs and a small breadth of pharmacological action require the use of DF, ensuring control of drug delivery to the body, including dosage accuracy and standard bioavailability. DF plays a very important role in the delivery of drugs to the lesion site. Capsules and coated tablets are necessarily created to avoid high toxicity of anticancer drugs and local tissue reactions when taken orally.

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Abstract 18686: Association of Obesity Susceptibility Gene Variants With Cardiometabolic Phenotypes in Morbid Obesity

Circulation ◽

10.1161/circ.130.suppl_2.18686 ◽

2014 ◽

Vol 130 (suppl_2) ◽

Author(s):

Sabine Fenk ◽

Marissa Koehler ◽

Christina Strack ◽

Ute Hubauer ◽

Judith Zeller ◽

...

Keyword(s):

Metabolic Syndrome ◽

Large Scale ◽

Risk Allele ◽

Association Studies ◽

Susceptibility Gene ◽

Genome Wide Association Studies ◽

Gene Variants ◽

Anthropometric Parameters ◽

Insulin Metabolism ◽

The Metabolic Syndrome

Introduction: Genome-wide association studies (GWAs) have identified several gene variants strongly associated with increased body mass index (BMI) and obesity. However, their association with the cardiometabolic consequences of obesity is unclear. We performed a study of 40 validated variants recently identified in two large metaanalysis GWAS and analyzed their association with related cardiovascular and metabolic traits of severe obesity. Methods: Genotyping was performed in 320 deeply-phenotyped obese subjects (mean BMI 41±9 kg/m2, aged 44±12 years), participating in a standardized weight reduction program. Anthropometric parameters, parameters of glucose/insulin metabolism, oxidative stress and early atherogenesis, adipokines, adhesion molecules, apolipoproteins, cardiac function and structure, intima media thickness and arterial elasticity were assessed standardized after 12h fast. Results: The transmembran protein TMEM18 rs939583 variant was significantly related to several parameters of adiposity (i.e. BMI β-estimate 1/2 risk alleles vs. no risk allele: 3.7±2.2/ 5.5±1.9, p=0.0009), epicardial fat thickness (p=0.023), insulin (p=0.002), fasting glucose (p=0.007), HOMA-IR (p=0.0008), and leptin (p=0.008) levels, systolic (p=0.007) and diastolic (p=0.009) blood pressure, arterial hypertension (frequency in subjects with 0/1/2 risk allele(s): 14/30/46%, p=0.001), and the metabolic syndrome (29/29/48%, p=0.029). Moreover, the BDNF rs10767664 variant was significantly associated with ApoA1, ApoA2, HDL cholesterol and soluble CD40L levels. Conclusion: TMEM18 and BDNF variants increased the risk of metabolic syndrome components, probably through their effect of abdominal obesity. However, several gene variants that have been found to be associated with BMI with small effects in large scale GWAS, did not seriously alter obesity related cardiometabolic traits.

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Influence of metabolic syndrome on the result of ischemic cardioembolic stroke due to atrial fibrillation

Psychiatry Neurology and Medical Psychology ◽

10.26565/2312-5675-2020-15-05 ◽

2020 ◽

Keyword(s):

Atrial Fibrillation ◽

Metabolic Syndrome ◽

Ischemic Stroke ◽

Large Scale ◽

Persistent Atrial Fibrillation ◽

Cardioembolic Stroke ◽

Motor Deficit ◽

High Density Lipoproteins ◽

Clinical Feature ◽

The Metabolic Syndrome

Metabolic syndrome is a complex of metabolic, hormonal, and clinical disorders, which are based on insulin resistance and compensatory hyperinsulinemia, abdominal obesity, disorders of lipid, purine metabolism, and arterial hypertension, is a combination of factors, each of which, both individually and in combination with others, has a significant effect on the risk of occurrence and the characteristics of the course of cardiovascular diseases, in particular ischemic strokes. The clinical feature of metabolic syndrome is the frequent development of paroxysms of atrial fibrillation, as a manifestation of the late stages of "hypertensive heart", which is illustrated in a number of large-scale population studies on the relationship between metabolic syndrome and the risk of atrial fibrillation. Our work raises the question of the features of the relations between metabolic syndrome and ischemic stroke caused by atrial fibrillation. Information concerning the qualitative and quantitative characteristics of the components of the metabolic syndrome with a breakdown of the clinical features of ischemic cardioembolic stroke in persons with the pathology under discussion, their natural course, the prognosis of the outcome, and sensitivity to treatment is very low. The article presents the results of the analysis of factors that make it possible to predict the course and outcome of acute ischemic stroke caused by atrial fibrillation against the background of metabolic syndrome. In order to determine the prognostic criteria for the outcome of cardioembolic stroke, 86 patients were examined, 41 patients were diagnosed with a cardioembolic stroke on the background of metabolic syndrome, 45 patients with cardioembolic stroke without metabolic syndrome. The analysis was based on the construction of correlation pleiades. A similar factor structure of indicators in both studied groups of patients with cardioembolic stroke indicates the same nature of changes in the state against the background of acute vascular catastrophe. A more severe course of the disease, based on the data of correlation analysis and data obtained by comparing indicators, is noted in the presence of the metabolic syndrome. Prognostically significant factors that allow predicting the course and outcome of cardioembolic stroke are the degree of a motor deficit on a five-point scale, total cholesterol, high-density lipoproteins, blood glucose, persistent atrial fibrillation, degree of stenosis of the internal carotid arteries, CHA2DS2-VASc scale indices.

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МОРФОФУНКЦІОНАЛЬНІ ОСОБЛИВОСТІ ЗМІН ШЛУНКОВОЇ СТІНКИ ПРИ МЕТАБОЛІЧНОМУ СИНДРОМІ

Scientific Issue Ternopil Volodymyr Hnatiuk National Pedagogical University. Series: Biology ◽

10.25128/2078-2357.19.2.12 ◽

2019 ◽

Vol 76 (2) ◽

pp. 72-78

Author(s):

M. S. Kaznacheevа

Keyword(s):

Metabolic Syndrome ◽

Gastric Mucosa ◽

Gastric Wall ◽

Cell Swelling ◽

External Diameter ◽

Intercellular Substance ◽

The Metabolic Syndrome ◽

Literary Sources ◽

Ec Cells ◽

Cellular Immune

The article discusses the histological component of the metabolic syndrome, reveals the main pathomorphological processes of the gastric wall that accompanies it. The histological features of changes of the microcirculatory channel and glandular epithelium of the gastric mucosa during metabolic syndrome are given. The histological changes of lymphoid formations and features of cellular immune response of gastric mucosal components in patients with metabolic syndrome are characterized. As a result of the analysis of literary sources the following conclusions were formed: 1) the most significant changes in the wall of the stomach during the development of MS are the mucous and submucosal membranes of the cardiac, fundal and portal sections, as the most active layers of the gastric wall in the functional plan; 2) endothelial cell swelling, destruction of superficial mucocytes, destruction of gastric holes, change of permeability and barrier function of the walls of microvessels, spasm and dilation of arterioles, reversible increase of permeability of venules and capillary walls are observed in MS; 3) the characteristic feature of MS is an increase in the number of macrophages and mast cells, which causes the release into the perivascular intercellular substance of plasmocytes and lymphocytes from the gaps of microvessels; 4) since the reaction of the glandular component of the gastric mucosa is a reflection of the compensatory-restorative mechanisms occurring in MS, the most characteristic is the decrease in the number of cardiac exocrinocytes and P-cells, an increase in the number of parietal and goblet cells, EC and EC cells. The reactive changes in exocrinocytes are reflected in the differences in the metric parameters of the external diameter of the gland, the diameter of the lumen, and the height of the epitheliocytes.

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Screening for the metabolic syndrome in subjects with migraine

Cephalalgia ◽

10.1177/0333102416672494 ◽

2016 ◽

Vol 37 (12) ◽

pp. 1180-1188 ◽

Cited By ~ 4

Author(s):

Sylvie Streel ◽

Anne-Françoise Donneau ◽

Nadia Dardenne ◽

Axelle Hoge ◽

Adelin Albert ◽

...

Keyword(s):

Metabolic Syndrome ◽

Large Scale ◽

Cardiovascular Health ◽

Smoking Status ◽

Hdl Cholesterol ◽

Cross Sectional Survey ◽

Cross Sectional ◽

Systematic Screening ◽

The Metabolic Syndrome ◽

Low Hdl

Background Metabolic syndrome (MetS) and migraine are known to be associated. This study assessed the risk of MetS and its clinical characteristics in migraine with aura (MA) and without aura (MO) based on a large-scale cross-sectional survey. Methods The study material consisted of 751 participants in the Nutrition, Environment and CardioVascular Health (NESCaV) survey. Diagnosis of migraine was based on the ef-ID migraine questionnaire and MetS was defined according to the Revised-Adult Treatment Panel III criteria. Sociodemographic and risk factors were also recorded. Weighted logistic regression was used to assess the risk of MetS. Results After adjusting for stratification (gender, age, district) and other factors (smoking status, sedentary lifestyle, family history of stroke, myocardial infarction and hypertension), MA subjects were at higher risk of MetS (OR 3.45; 95% CI: 1.63–7.29) while MO individuals were not, when compared to non-migraineurs. When considering MetS components, MA was positively associated with low HDL-cholesterol (OR 2.26; 95% CI: 1.08–4.74), hyperglycemia (OR 2.77; 95% CI: 1.30–5.88) and abdominal obesity (OR 2.03; 95% CI: 1.07–3.86). Conclusion Migraineurs with aura are at higher risk of MetS, suggesting that these subjects, already more exposed to stroke, may benefit from a systematic screening for the metabolic syndrome.

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Association between consumption frequency of honey and non-alcoholic fatty liver disease: results from a cross-sectional analysis based on the Tianjin Chronic Low-grade Systemic Inflammation and Health (TCLSIH) Cohort Study

British Journal Of Nutrition ◽

10.1017/s0007114520003190 ◽

2020 ◽

pp. 1-9 ◽

Cited By ~ 1

Author(s):

Shunming Zhang ◽

Xiaohui Wu ◽

Shanshan Bian ◽

Qing Zhang ◽

Li Liu ◽

...

Keyword(s):

Metabolic Syndrome ◽

Liver Disease ◽

Fatty Liver ◽

Fatty Liver Disease ◽

Large Scale ◽

Cross Sectional ◽

Alcoholic Fatty Liver ◽

The Metabolic Syndrome ◽

Consumption Frequency ◽

Alcoholic Fatty Liver Disease

Abstract Non-alcoholic fatty liver disease (NAFLD) is the hepatic manifestation of the metabolic syndrome. Recent evidence has suggested the protective effects of honey consumption against the metabolic syndrome, but the association between honey intake and NAFLD is still unclear. We investigated how the consumption frequency of honey was associated with NAFLD in the general population. This was a cross-sectional study of 21 979 adults aged 20–90 years. NAFLD was diagnosed based on the ultrasound-diagnosed fatty liver without significant alcohol intake and other liver diseases. Diet information, including consumption frequency of honey, was assessed by a validated 100-item FFQ. OR with 95 % CI were calculated by the binary logistic regression model, adjusting for confounding factors identified by the directed acyclic graph. Overall, 6513 adults (29·6 %) had NAFLD. Compared with participants consuming ≤1 time/week of honey, the multivariable OR of NAFLD were 0·86 (95 % CI 0·77, 0·97) for 2–6 times/week and 1·10 (95 % CI 0·95, 1·27) for ≥1 times/d (Pfor trend = 0·90). The results were generally similar in subgroups of BMI at a cut-point of 24·0 kg/m2 (Pfor interaction = 0·10). In this large-scale study, consuming honey 2–6 times/week was inversely associated with NAFLD, whereas consuming honey ≥1 times/d had no association with NAFLD. These results need replication in other large-scale prospective studies.

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Pathogenetic relationship of oral microbiota and obesity in children and adolescents

Rossiyskiy Vestnik Perinatologii i Pediatrii (Russian Bulletin of Perinatology and Pediatrics) ◽

10.21508/1027-4065-2021-66-5-38-41 ◽

2021 ◽

Vol 66 (5) ◽

pp. 38-41

Author(s):

Yu. G. Samoilova ◽

O. A. Oleynik ◽

D. A. Kudlay ◽

E. V. Sagan ◽

N. S. Denisov

Keyword(s):

Metabolic Syndrome ◽

Gastrointestinal Tract ◽

Conservative Treatment ◽

Taxonomic Diversity ◽

Point Of View ◽

Oral Microbiota ◽

Scientific Interest ◽

The Metabolic Syndrome ◽

Relationship Of ◽

The Relationship

The review summarizes the data of foreign studies on the relationship of the taxonomic diversity of the oral microbiota and changes in its composition with the development of the metabolic syndrome in children with obesity. This information is of scientific interest from the point of view of the search for new targets and possible ways of conservative treatment in order to prevent and treat obesity through maintaining the microflora of the gastrointestinal tract.

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