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101.
102.
Alteration of extracellular calcium concentration may be involved in glucose metabolism in a number of pathways. The present study was designed to investigate the relationship between total serum calcium and 1) fasting serum glucose, 2) insulin, 3) insulin resistance, and 4) beta-cell function in 1,182 healthy subjects from the province of Newfoundland and Labrador, Canada. All variables were log10 transformed, and confounding factors including age, trunk fat percentage, serum phosphorus, magnesium, 25-OH vitamin D, and parathyroid hormone were adjusted before analyses. Significant positive correlations between glucose and insulin resistance with calcium were found in both sexes, whereas an inverse correlation between beta-cell function and calcium was found only in women. Similar results were found in medication-free women and men, as well as in pre- and postmenopausal women. Subjects with low calcium levels had the lowest concentration of glucose and the least insulin resistance, whereas subjects with high calcium levels had the highest concentration of glucose and insulin resistance in women but not in men. This relationship remained after calcium was adjusted for 25-OH vitamin D and parathyroid hormone. Our results suggest that alteration of serum calcium homeostasis is significantly correlated with the abnormality of glucose level, insulin resistance, and beta-cell function. 相似文献
103.
104.
Malavalli Madaiah Maralekere K. Prashanth Hosakere D. Revanasiddappa Bantal Veeresh 《Archiv der Pharmazie》2013,346(3):200-209
New 3‐[(2,4‐dioxo‐1,3,8‐triazaspiro[4.6]undec‐3‐yl)methyl]benzonitrile derivatives 8 – 37 were synthesized and their pharmacological activities were determined with the objective to better understand their structure–activity relationship (SAR) for anticonvulsant activity. All the compounds were evaluated for their possible anticonvulsant activity by maximal electroshock seizure (MES) and pentylenetetrazole (PTZ) test. Compounds 11 , 18 , 31 , and 32 showed significant and protective effect on seizure, when compared with the standard drug valproate. The same compounds were found to exhibit advanced anticonvulsant activity as well as lower neurotoxicity than the reference drug. From this study, it is quite apparent that there are at least three parameters for the activity of anticonvulsant drugs, that is, a lipophilic domain, a hydrophobic center, and a two‐electron donor. 相似文献
105.
Srinivas Maddi Shravan Kumar Yamsani Adukondalu Devandla Gerhard Scriba Madhusudan Rao Yamsani 《Medicinal chemistry research》2013,22(5):2403-2410
The purpose of the study was to investigate whether efflux and stereoselective mechanisms play any role in the transport of nateglinide (NA) enantiomers in rat. The transport of individual enantiomers and racemate was studied with and without the presence of an inhibitor for P-glycoprotein and MRP2, verapamil using duodenal, jejunal, and ileal intestinal sacs prepared from rat intestine. The intestinal samples were analyzed by a validated chiral HPLC method. Generally, higher concentrations of R-NA and its S-enantiomer were observed when the racemate was administered compared to administration of the individual enantiomers. Transport of NA enantiomers when co-incubated with verapamil was increased in the ileum by twofold to threefold with corresponding decreased secretion by almost threefold, while little change in the duodenum and jejunum. The transport of NA from everted sac segments (basal-to-apical side, secretion) was higher than the transport from the normal sac segments (apical-to-basal side, absorption) indicated an involvement of efflux-mediated transport. It has been found that the transport of NA is stereoselective and also regioselective, i.e., R-NA displayed higher efflux than S-NA and it was higher in ileum than the duodenum and jejunum. This study will really pave the way to understand how efflux transporters influence the absorption of chiral compounds when moving across the gastrointestinal tract. 相似文献
106.
Basavapatna N. Prasanna Kumar Kikkeri N. Mohana Lingappa Mallesha Bantal Veeresh 《Medicinal chemistry research》2014,23(7):3363-3373
A series of new 2,5-disubstituted-1,3,4-oxadiazoles 6(a–j) have been conveniently synthesized by intermolecular oxidative cyclization of (E)-2-(arylbenzylidene)-2-[(4-methoxyphenyl)amino]acetohydrazides promoted by iodobenzene diacetate as an oxidant. The synthesized compounds were characterized by elemental analyses, FT-IR, LCMS, 1H NMR, and 13C NMR spectral studies. All the compounds were evaluated for their in vitro antiproliferative effect using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide assay method against four human cancer cell lines (K562, Colo-205, MDA-MB 231, IMR-32) for the time period of 24 h. Among the analogs, compounds 6h and 6i showed good activity on all cell lines, whereas the other compounds in the series exhibited moderate activity. 相似文献
107.
Raghu TY Venkatesulu GA Kantharaj GR Suresh T Veeresh V Hanumanthappa Y 《Indian journal of dermatology, venereology and leprology》2001,67(5):261-262
Progeria is an autosomal dominant, premature aging syndrome. Six and three year old female siblings had sclerodermatous changes over the extremities, alopecia, beaked nose, prominent veins and bird-like facies. Radiological features were consistent with features of progeria. The present case highlights rarity of progeria in siblings with a possible autosomal recessive pattern. 相似文献
108.
Serum magnesium (SMg) has been reported to negatively correlate with an atherogenic lipid profile in individuals with diabetes mellitus (DM) and metabolic syndrome. This study examines whether the relationships between SMg levels and biochemical and anthropometric risk factors for these conditions are also present in the general adult population.Design and methodsBiochemical parameters and anthropometric variables were assessed in 1318 healthy adult subjects recruited from the Newfoundland population.ResultsSMg positively correlated with age, and serum phosphate, calcium, albumin, total cholesterol, HDL-cholesterol, LDL-cholesterol and triglyceride levels. SMg negatively correlated with HOMA-β and percent body fat measured by DEXA. On sub-grouping subjects according to sex, menopausal status or after excluding subjects with DM, only a significant correlation of SMg with albumin, calcium, phosphate, and total cholesterol was common to all. Stepwise linear regression analysis revealed albumin, phosphate, age, total cholesterol, glucose, and body mass index as independent predictors of SMg levels.ConclusionsThese results indicate that SMg levels positively correlate with total cholesterol and possibly all lipoproteins in a large adult study population which suggests that variation of SMg with serum lipid levels may be different in healthy individuals compared with those with DM. We speculate on a possible binding interaction. 相似文献
109.
A series of new 2-methyl-3-(2-piperazin-1-yl-ethyl)-pyrido[1,2-a]pyrimidin-4-one derivatives 6a-j were synthesized by a nucleophilic substitution reaction of 2-methyl-3-(2-piperazin-1-ylethyl)-pyrido[1,2-a]pyrimidin-4-one
with various sulfonyl chlorides. The compounds were characterized by different spectral studies. All the compounds were evaluated
for their antiproliferative effect using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay method
against four human cancer cell lines (K562, Colo-205, MDA-MB 231, IMR-32) for the time period of 24 h. Among the series, compounds
6d, 6e and 6i showed good activity on all cell lines except K562, whereas the other compounds in the series exhibited moderate activity.
Compound 6d could be a potential anticancer agent and therefore deserves further research. 相似文献
110.
Ozbak H Dark P Maddi S Chadwick P Warhurst G 《The Journal of molecular diagnostics : JMD》2012,14(2):176-184
Effective diagnosis and treatment of bloodstream infections are often hampered by a lack of time-critical information from blood cultures. Molecular techniques aimed at the detection of circulating pathogen DNA have the potential to dramatically improve the timeliness of infection diagnosis. Our aim in this study was to establish a rapid, low-cost PCR approach using high-resolution melting analysis to identify a syndromic panel of 21 pathogens responsible for most bloodstream bacterial infections encountered in critical care environments. A broad-range, real-time PCR technique that combines primers for molecular Gram classification and high-resolution melting analysis in a single run was established. The differentiation of bacterial species was achieved using a multiparameter, decision-tree approach that was based on Gram type, grouping according to melting temperature, and sequential comparisons of melting profiles against multiple reference organisms. A preliminary validation study was undertaken by blinded analysis of 53 consecutive bloodstream isolates from a clinical microbiology laboratory. Fifty isolates contained organisms that were present in the panel, and 96% of these were identified correctly at the genus or species level. A correct Gram classification was reported for all 53 isolates. This technique shows promise as a cost-effective tool for the timely identification of bloodstream pathogens, allowing clinicians to make informed decisions on appropriate antibiotic therapies at an earlier stage. 相似文献