Morphologie

Ohne Zusammenfassung     

Comparison of different serum sample extraction methods and their suitability for mass spectrometry analysis

Mass spectrometry has been widely used, particularly in pharmacokinetic investigations and for therapeutic drug monitoring purposes. Like any other analytical method some difficulties exist in employing mass spectrometry, mainly when it is used to test biological samples, such as to detect drug candidates in mammalian serum, which is rich in proteins, lipids and other contents that may interfere with the investigational drug. The complexity of the serum proteome presents challenges for efficient sample preparation and adequate sensitivity for mass spectrometry analysis of drugs. Enrichment procedures prior to the drug analysis are often needed and as a result, the study of serum or plasma components usually demands either methods of purification or depletion of one or more. Selection of the best combination of sample introduction method is a crucial determinant of the sensitivity and accuracy of mass spectrometry. The aim of this study was to determine the highest serum protein precipitation activity of five commonly used sample preparation methods and test their suitability for mass spectrometry. We spiked three small molecules into rabbit serum and applied different protein precipitation methods to determine their precipitation activity and applicability as a mass spectrometry introductory tool.     

Synthesis, biopharmaceutical characterization, antimicrobial and antioxidant activities of 1-(4'-O-β-D-glucopyranosyloxy-2'-hydroxyphenyl)-3-aryl-propane-1,3-diones

This research communication is toward the investigation of the antibacterial, antifungal and antioxidant activities of the synthesized compounds 1-(4′-O-β-d-glucopyranosyloxy-2′-hydroxyphenyl)-3-aryl-propane-1,3-diones (5a)-(5h). These compounds have been obtained by the interaction of α-acetobromoglucose with 1-(2′,4′-dihydroxyphenyl)-3-aryl-propane-1,3-diones (3a)-(3h) under anhydrous condition and at lower temperature. The structures of these newly synthesized O-β-d-glucopyranosides were established on the basis of chemical, elemental, and spectral analyses. Further, the compounds (5b), (5c), (5d) and (5g) showed potent antibacterial and antifungal activity. A good correlation was obtained between the theoretical predictions of bioavailability using Lipinski’s rule-of-five and experimental verification.     

Predictions and correlations of structure activity relationship of some aminoantipyrine derivatives on the basis of theoretical and experimental ground

A series of 4-aminoantipyrine derivatives were produced by condensing aromatic primary amine, namely, 4-aminoantipyrine with different aryl carbonyls which occurred cleanly and efficiently without using any catalyst at room temperature. Their structures were confirmed on the basis of ¹H NMR, IR, Mass spectra, and elemental analysis. The synthesized library was screened virtually using versatile bioinformatics parameters owing to the quick access, biological response, and utility of the produced moieties. The virtually screened molecules were subjected to screen practically against certain some strain of microorganisms: Staphylococcus aureus (Gram positive), Pseudomonas vulgaris (Gram positive), Pseudomonas Aeruginosa (Gram negative), and Escherichia coli (Gram negative). A correlation of structure and activities relationship of these compounds with respect to molecular modeling, Lipinski rule of five, drug-likeness, toxicity profiles, and other physico-chemical properties of drugs is described and verified experimentally.     

High prevalence of malnutrition and deranged relationship between energy demands and food intake in advanced non‐small cell lung cancer

The relation between dietary intake and metabolic profile in non‐small cell lung cancer (NSCLC) was evaluated. Patients with NSCLC were recruited and their caloric requirement and resting energy expenditure (REE) were calculated using the Harris–Benedict equation and Katch–McArdle formula respectively. Hypermetabolic state was defined as REE more than 10% above the basal metabolic rate (BMR). Body composition parameters were calculated by bioelectric impedance method. The 24‐h dietary intake method and Malnutrition Universal Screening Tool assessed nutritional intake. One hundred and forty‐eight subjects were included (87% males). Of these, 46.6% subjects were hypermetabolic and 31% cachexic, with lower calorie and protein intakes than recommended, although per cent of total energy derived from protein, fat and carbohydrates were similar. Hypermetabolic patients had lower BMI, though the per cent deficit in energy and protein consumption was similar. Cachexia was associated with lower BMR but not with deficit in energy or protein consumption. No correlation was seen between dietary intake and body composition parameters. The calorie and protein intake of NSCLC patients is lower than recommended. The discordance between elevated REE and dietary intake implies that the relationship between increased energy demands and food intake may be altered.     

Patient profile and comparison of three diagnostic criteria for cardiac sarcoidosis in a tuberculosis endemic population

Background:Cardiac sarcoidosis (CS) is an underdiagnosed and life-threatening condition. Histopathological diagnosis is difficult due to the risks and variable diagnostic yield of endomyocardial biopsy.Objectives:To study the clinical profile and compare the diagnostic criteria of CS in a cohort of sarcoidosis.Methods:A retrospective review of the Sarcoidosis database (375 patients) was performed to identify patients with CS. Demographic and clinical details were retrieved. We applied the available diagnostic criteria for the diagnosis of CS: The World Association of Sarcoidosis and Other Granulomatous Diseases (WASOG), Heart Rhythm Society (HRS), and Japanese Ministry of Health and Welfare (JMHW) criteria.Results:Out of the 375 patients, 15 (4%) were identified with CS. The median age was 41 years, and 53% were female. The most common symptoms were breathlessness, palpitation, and fatigue in 80%, 53.3%, and 46.6% of patients, respectively. Tuberculin positivity (≥ 10mm induration) was seen in 26.6%. 80% and 53.3% of the patients had abnormal ECG and 2D echocardiography findings, respectively. Six patients had a history of Ventricular tachycardia (40%). LV Ejection fraction was reduced in 12 subjects (80%). Cardiac-MRI showed late gadolinium enhancement in 53.3%. A definitive histopathological diagnosis for sarcoidosis was established in 86.6% (13/15) patients. Of the 15, all satisfied JMHW criteria and WASOG criteria (12 (80%) at least probable category, 3 (20%) possible CS), and 13 (86.6%) met HRS criteria for a diagnosis of CS.Conclusion:In a cohort of 375 patients with sarcoidosis in a tuberculosis endemic setting, 4% were diagnosed with cardiac sarcoidosis. Histopathological diagnosis may be obtained by sampling from extracardiac sites. JMHW and WASOG criteria perform equally well in TB endemic settings.