In-vitro Antiproliferative Activity of New Tetrahydroisoquinolines (THIQs) on Ishikawa Cells and their 3D Pharmacophore Models.

The antiproliferative activities of new substituted tetrahydroisoquinolines (THIQs) are described. Their cytotoxicities against Ishikawa human endometrial cell line were determined after 72 h drug expose employing Celtiter-Glo assay at concentrations ranging from 0.01 to 100,000 nM. The antiproliferative activities of the compounds understudy were compared to tamoxifen (TAM). In-vitro results indicated that most of the compounds showed better activity than TAM. The most active compounds obtained in this study were 1, 2, 3 and 22 whose IC50 values are 1.41, 0.91, 0.74 and 0.36 µM respectively. This study helped us to evaluate the risk of developing endometrial cancer in the design of non-steroid estrogen receptor modulators with no agonistic effects on uterus. In-silico pharmacophore hypotheses were generated using GALAHAD and PHASE and the best models with a probable bioactive conformation(s) for these compounds were proposed. These conformations and the alignments of the molecular structures give us an insight in designing compounds with better biological activity.

A Clinical and Radiographic Comparison of Platelet-rich Fibrin and Lyophilized Platelet-derived Preparation as Pulpotomy Agent in Primary Molars.

INTRODUCTION: Vital pulpotomy in primary molar teeth is aimed to retain the tooth in function until it is replaced by its successors. AIM: The aim of this study was to evaluate and compare platelet-rich fibrin (PRF) and lyophilized platelet-derived preparation (LPDP) as a pulpotomy agent in primary molars. MATERIALS AND METHODS: Forty primary molars from 20 healthy children aged 5-9 years requiring pulpotomy in the contralateral side of mandible were randomly selected. In both the groups, pulpotomy was carried out by removing coronal pulp and achieving hemostasis, the radicular part of pulp tissue was packed with PRF preparation in Group I and LPDP (Mothercell Research Centre, Trichy, Tamil Nadu, India) in Group II. The teeth were restored with zinc oxide eugenol and glass ionomer cement (GIC), followed by stainless steel crown in the same visit. Clinical and radiographic evaluation was undertaken at 1, 3, and 6 months interval. RESULTS: The overall success rate was 90% in PRF group and 95% in LPDP group at the end of 6 months. The results were statistically nonsignificant between the groups (P > 0.05). CONCLUSION: The overall outcome of the study suggests that PRF and LPDP are acceptable pulpotomy agents and are promising in the era of new vital pulp therapy procedure.

Dependence of the V/III Ratio on Indium Incorporation in InGaN Films Grown by Metalorganic Vapour Phase Epitaxy.

InGaN epitaxial layers were grown on c-plane sapphire substrates using the metalorganic vapour phase epitaxy (MOVPE) system at 760 °C. By varying the total flow rate of group-III sources (TMI+TEG) with a fixed molar ratio of group-III sources [TMI/(TMI+TEG)], the influence of V/III ratio were investigated from 4500 to 20000. The grown N-polar InGaN layers were investigated by atomic force microscopy and it is found that the surface roughness decreases with increasing the V/III ratios. High resolution X-ray diffraction analyses show that the phase separation decreases with increasing the V/III ratios. Photoluminescence measurements reveal that the peak position of the band-edge emission shifted toward the shorter wavelength with increasing the V/III ratios. Reciprocal space mapping (RSM) analyses were carried out on InGaN films. At low V/III ratio, the phase separation can be detected in InGaN films.

Inborn errors of metabolism: Review and data from a tertiary care center.

Inherited metabolic disorders are a heterogeneous group of genetic conditions mostly occurring in childhood. They are individually rare but collectively numerous, causing substantial morbidity and mortality. We have retrospectively reviewed a total of eight hundred and sixty nine cases with different age groups that had been referred from several diagnostic centers and hospitals of India to the Department of Metabolism in Narayana Hrudayalaya, as cases suspected with inborn errors of metabolism. Advanced techniques applied were to diagnose the disorders of inborn errors of metabolism. Data analyzed indicates occurrence of several metabolic disorders in our population. The need to screen for an inborn error of metabolism arises out of the fact that most cases take to irreversible effects as time progress. Emphasis has to be laid on early detection and prompt management, which could help in alleviating symptoms and preventing complications and consequent incapacitation.

Biotin metabolism defect - A case report.

Defects in biotin metabolism are mainly associated with either the enzyme Biotinidase or Holocarboxylase synthetase. Defects in either enzymes depletes biotin utilization by the cells. Holocarboxylase synthetase deficiency is an inherited disorder in which the body is unable to use the vitamin biotin effectively. This condition is inherited in an autosomal recessive pattern. We present a case of a 9 year old girl with atypical symptomology as a case holocarboxylase synthetase deficiency, who demonstrated an increased excretion of propionic and methyl malonic acids, with her biotinidase activity being normal. She demonstrated remarkable improvement on biotin supplementation.

Evans hole and non linear optical activity in Bis(melaminium) sulphate dihydrate: A vibrational spectral study.

Bis(melaminium) sulphate dihydrate (BMSD), an interesting melaminium derivative for nonlinear optical activity, has been subjected to vibrational spectral analysis using FT IR and FT Raman spectra. The analysis has been aided by the Potential Energy Distribution (PED) of vibrational spectral bands, derived using density functional theory (DFT) at B3LYP/6-31G(d) level. The geometry is found to correlate well with the XRD structure and the band profiles for certain vibrations in the finger print region have been theoretically explained using Evans hole. The detailed Natural Bond Orbital (NBO) analysis of the hydrogen bonding in BMSD has also been carried out to understand the correlation between the stabilization energy of hyperconjugation of the lone pair of donor with the σ(∗) orbital of hydrogen-acceptor bond and the strength of hydrogen bond. The theoretical calculation shows that BMSD has NLO efficiency, 2.66 times that of urea. The frontier molecular orbital analysis points to a charge transfer, which contributes to NLO activity, through N-H…O intermolecular hydrogen bonding between the melaminium ring and the sulphate. The molecular electrostatic potential (MEP) mapping has also been performed for the detailed analysis of the mutual interactions between melaminium ring and sulphate ion.

Steroidogenic alterations in testes and sera of rats exposed to formulated Fenvalerate by inhalation.

Fenvalerate (Fen) is a synthetic pyrethroid, which is commonly used for destroying a variety of insect pests damaging several vegetable, fruit, and cotton crops. This insecticide is also used to mitigate household insects like flies, cockroaches, mosquitoes, and so forth. Human beings are exposed to formulated Fen preparations mostly by inhalation during spraying in fields for crop protection, for control of household insects, and also during handling and packaging at manufacturing plants. Limited online information is available regarding toxic effects of formulated Fen exposure on mammalian reproductive system. The present study has been undertaken to investigate male reproductive toxic effects of a formulated preparation of Fen (20% EC) particularly in relation to steroidogenic alterations in testes and sera of rats exposed by nose-only inhalation for (4 hours/day and five days a week) for three months. The results indicate significant reduction in the weight of testes, epididymal sperm counts, and sperm motility, along with decrease in marker testicular enzymes for testosterone biosynthesis viz. 17-beta-hydroxy steroid dehydrogenase (17-beta-HSD) and glucose-6-phosphate dehydrogenase (G6PDH), leading to net decrease in serum testosterone concentration in group of rats exposed to one-fifth LC50 of Fen (20% EC) by inhalation (4 hours/day, five days a week) subchronically for three months. These results for the first time indicate the role of testosterone in Fen (20% EC)-induced male reproductive toxicity of rats subchronically exposed by inhalation probably due to neuroendocrine-mediated phenomenon and hormone-disrupting property of the insecticide.

Effect of fly ash inhalation on biochemical and histomorphological changes in rat liver.

The effect of fly ash inhalation (4h daily, 5 days a week) for 28 days on the deposition of metal ions and histopathological changes in the liver and serum clinical enzymes has been studied. The results showed an increase in the concentration of metals such as cadmium (Cd), chromium (Cr), copper (Cu), manganese (Mn), and lead (Pb) in the tissues of exposed rats. The level of metals varied from metal to metal and from organ to organ. Level of serum enzymes such as serum glutamate oxaloacetate transaminase, serum glutamate pyruvate transaminase, and alkaline phosphatase were increased in fly ash exposed rats using whole body inhalation exposure as compared to sham controls. Histopathological studies of rat liver exposed to fly ash revealed infiltration of mononuclear cells in and around the portal triads, which seems to be laden with fly ash particles. Hepatocytes showed necrotic changes such as pyknotic nuclei, karyorrhexis, and karyolytic. These changes were more towards the centrolobular areas than the midzonal and periportal areas. These findings demonstrate that the toxic metals of inhaled fly ash in rats may get translocated into extrapulmonary organs, become deposited and hence may manifest their toxic effects on different tissues.