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Aims: To assess the contrast sensitivity (CS) in different stages of primary open angle glaucoma and to correlate it with the severity (mild, moderate & severe) of glaucoma. Materials and Methods: This prospective randomized study was conducted at Sapthagiri institute of medical sciences and research centre, Bangalore between June 2017 & December 2017. A total of 100 eyes of 55 individuals aged 25-80 years diagnosed with POAG were enrolled in this prospective study. Selected subjects underwent detailed ophthalmic examination including ocular history, slit lamp examination, objective & subjective refraction (if required) to obtain best corrected visual acuity (BCVA) on Snellen visual acuity chart and dilated fundus evaluation using indirect ophthalmoscopy. Eyes with clear media and ?BCVA 6/60 were included and contrast sensitivity was measured using Pelli Robson chart at 1 meter distance. HFA report of included subjects were collected from Glaucoma department to classify them in to mild, moderate and severe groups according to their visual field findings (pattern deviation of HFA report). Classification was done according to International statistical classification of disease and related health problem (ICD 10). One way ANOVA and t-test was used to analyze the data. Results: There was 36% mild, 26% moderate and 38% severe cases of POAG classified according to ICD 10. The mean value of contrast in mild, moderate and severe POAG was 1.4341, 1.3267 and 1.1326 respectively. An analysis of variance tested whether there were significant difference in contrast sensitivity among mild, moderate and severe POAG. Results indicated that these means differed significantly p Conclusion: There was decrease in contrast sensitivity with the severity of POAG. Thus the contrast sensitivity testing should be made mandatory in evaluating POAG patients which could help in screening/diagnosis (early detection) and to assess the progression of the disease as well as response to the tre

The ubiquitous presence of non-stationarities in the EEG signals significantly perturb the feature distribution thus deteriorating the performance of Brain Computer Interface. In this work, a novel method is proposed based on Joint Approximate Diagonalization (JAD) to optimize stationarity for multiclass motor imagery Brain Computer Interface (BCI) in an information theoretic framework. Specifically, in the proposed method, we estimate the subspace which optimizes the discriminability between the classes and simultaneously preserve stationarity within the motor imagery classes. We determine the subspace for the proposed approach through optimization using gradient descent on an orthogonal manifold. The performance of the proposed stationarity enforcing algorithm is compared to that of baseline One-Versus-Rest (OVR)-CSP and JAD on publicly available BCI competition IV dataset IIa. Results show that an improvement in average classification accuracies across the subjects over the baseline algorithms and thus essence of alleviating within session non-stationarities.

Brain-Computer Interfaces (BCI) are systems that enable users to use neural signals, typically Electroencephalogram (EEG) to direct an application or an external device. Motor imagery (MI) based BCI detects subject motor intentions which could be further used as control signals. Due to spatial lateralization of different MI tasks, spatial filtering followed by band power extraction is the most commonly used algorithm for classification tasks in MI-based BCIs. Unfortunately, the spatial filtering approach significantly incorporates Amplitude characteristics when compared to Phase characteristics of the EEG signal. Single trial Phase locking value (sPLV) has been a popular statistics to extract phase based information for classification task in MI-based BCI. To utilize the phase characteristics for MI classification, this paper proposes a novel approach based on instantaneous phase difference (IPD) sequence to extract phase features that explicitly use the phase synchronization information between EEG sensors. We maximized the discriminability of IPD sequence using linear transformation calculated from common spatial pattern algorithm (CSP) on the IPD sequence. An evaluation of our method on BCI competition dataset led to around 15% increase in mean classification accuracies compared to sPLV approach and comparable accuracies to power feature based CSP algorithm. Furthermore, incorporating phase features from our method and power features from traditional algorithms using sparse feature selection technique increased the classification accuracy over both CSP and CSP on the IPD sequence.

To enhance the therapeutic efficacy of chemotherapy on glioblastoma U87MG cell line, paclitaxel-loaded phycocyanin nanoparticles (PTX-PcNPs) were prepared by modified desolvation process. PTX-PcNPs were characterised in terms of size, zeta potential, drug loading efficiency and drug release. Confocal laser scanning microscopy showed PTX-PcNPs could be internalised by U87MG cells. The anti-cancer activity was investigated in vitro by 3-(4,5-dimethylthizol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay with and without photodynamic therapy. It was observed that formulation could significantly inhibit growth of U87MG cells as compared to PTX alone and also induced apoptosis, which was evidenced by presence of apoptotic bodies and nuclear fragmentation in treated cells. The present study suggests that PTX-PcNPs can act as a promising drug delivery system for cancer treatment.

In this study, the apoptosis-inducing effect of an alcoholic extract from Erythrina suberosa stem bark (ESB) was investigated using human promyelocytic leukemia HL60 cells. Cell viability was estimated by MTT assay. We found that the ESB inhibited cell proliferation in a dose- and time-dependent manner. A series of well-documented morphological changes, such as cell shrinkage, condensation of nuclear chromatin, and nuclear fragmentation, were observed by fluorescence microscopy. The gold standard scanning electron micrographs showed apoptotic bodies and formation of blebs. Cell cycle analysis showed a significant increase in Sub G(0) population of cells above 50 μg/ml. ESB treatment resulted in a dose-dependent increase in annexin V positive cells. Increase in intracellular ROS production up to sixfold was detected in ESB-treated HL60 cells by DCFH-DA assay. Dissipation of mitochondrial membrane potential of intact cells accompanied by increase in cytosolic cytochrome c was observed, which was followed by activation of caspase-9 and -3 but not caspase-8. DNA fragmentation analysis revealed typical ladders as early as 18 h indicative of caspase-3 role in the apoptotic pathway. The overall results suggest that ESB induces mitochondria-mediated intrinsic apoptotic pathway in HL60 cells and might have therapeutic value against human leukemia.

A new class of 4β-N-polyaromatic substituted podophyllotoxin congeners have been synthesized and evaluated for their DNA topoisomerase-II (topo-II) inhibition as well as anticancer potential in some human cancer cell lines. The ease of synthesis and interesting biological activities make the present series of polyaromatic-podophyllotoxin congeners as a promising new structure for the development of new anticancer agents based on podophyllotoxin scaffold.

Condensation of various amines (Ia–c) with 4-isothiocyanato-4-methyl-2-pentanone (2a) at room temperature gave tetrahydropyrimidinethiones (3a–c) whereas condensation of 1a–e with 3-isothiocyanatobutanal at room temperature gave tetrahydropyrimidinethiones (4a–e). Amines 1a, d, f–i on condensation with 4-isothiocyanato-4-methyl-2-pentanone (2a) by heating under reflux for 8 h at pH ~4 (for 1a, d) and at RT (for 1f–i) gave dihydropyrimidinethiones 5a–b and 5c–f, respectively. Condensation of 1f with 3-isothiocyanatobutanal gave dihydropyimidinethione 6. When isothiocyanate (2a) and phenylenediamine derivatives 1g, h were heated under reflux at pH ~4, tricyclic compounds 7a, b were obtained in good yields. Condensation of 3-isothiocyanatobutanal with o-phenylenediamines 1h and 1j at pH ~ 5 by refluxing in methanol for 8 h gave products 8 and 9. All these compounds were screened for anti-inflammatory activity. Compounds 3c, 4c and 7a exhibited anti-inflammatory activity comparable to standard drug ibuprofen.

Heterocyclic benzimidazole derivatives 3a-h, 5a-c and 7a-d have been synthesized by condensation of succinic acid (1) homophthalic acid (4) and 2,3-pyrazinedicarboxlic acid (6) with various substituted diamines under microwave irradiation in good yields. Structures assigned to 3a-h, 5a-c and 7a-d are fully supported by spectral data. All these compounds were screened for anti-inflammatory and anticancer activities. At a dose of 50 mg/kg p.o. compounds 3b (39.4%) and 3c (39.2%) exhibited anti-inflammatory activity, comparable to standard ibuprofen which showed 39% activity at 50 mg/kg p.o. and compound 7c exhibit good anticancer activity against ovary (IGR-OV-1), breast (MCF-7) and CNS(SF-295) human cancer cell lines.

A number of N-substituted cyclic imides 3a-e, 5a-e, 7a-d, and 9a-e have been synthesized in very high yields, by condensation of various diacids 2, 4, 6, and 8 with different amines under microwave irradiation. These compounds were screened for anticancer and anti-inflammatory activities, and compounds 3c, 3e, 5c, 9c, and 9d exhibited anticancer activity against colon (COLO 205) cancer better than 5-fluorouracil and mitomycin-C, and compound 9b exhibited anti-inflammatory activity better than standard drug phenyl butazone.

The primary aim of present work was to develop effective combination drug therapy for topical treatment of psoriasis.Betamethasone dipropionate and calcipotriol loaded solid lipid nanoparticles (CT-BD-SLNs) were prepared by hot melt high shear homogenization technique, which were then incorporated in Carbopol gel matrix. The anti-psoriatic potential was tested by sequential in vitro (skin permeation and dermal distribution, anti-proliferative effect in HaCaT cells) and in vivo (Draize patch irritation, transepidermal water loss (TEWL) and anti-psoriatic mouse tail studies) experiments.A negligible amount in receptor compartment, yet confined distribution of drugs to epidermal and dermal region of skin was observed in case of SLNs, which is essential for safe and effective anti-psoriatic therapy. Draize patch test and TEWL demonstrated negligible skin irritation and better skin tolerability of SLNs. The in vitro HaCaT cell line study demonstrated that SLNs delayed the abrupt growth of keratinocytes, while in vivo mouse tail model showed that SLNs gel significantly decreased the epidermal thickness and increased melanocyte count in comparison to commercial Daivobet® ointment.The developed SLNs gel is expected to be potential strategies for treatment of psoriasis and other topical diseases.

Compounds (IIIa) and (IIIb) exhibit anti-inflammatory activity comparable to that of ibuprofen, and some of the synthesized compounds, e.g. (VI), show moderate anticancer activity against five human cancer cell lines.

In the present study root extracts of Schleichera oleosa were prepared and analysed for hydroxyl radical scavenging potential in different in vitro models, such as deoxyribose degradation (site-specific and non-site specific) and plasmid nicking assays. The extracts were found to have profound effects in both assays by scavenging of hydroxyl radicals. The extracts were also assessed for in vitro cytotoxicity in a sulphorhodamine B dye assay against a panel of cell lines representing different types of human cancers and tissues, wherein the methanol, ethyl acetate and water extracts were found to effectively inhibit the growth of selective cell lines. The results of the present study suggests the presence of antioxidant constituents in the methanol and ethyl acetate extracts of the roots of S. oleosa, results which are in concurrence with preliminary 1H NMR and IR studies that suggest the presence of polyphenolic compounds.

Compounds (IIIa) and (IIIc) exhibit antiinflammatory activity comparable to standard ibuprofen and compound (IX) exhibits good anticancer activity against ovary (IGR-OV-1), breast (MCF-7), and CNS (SF-295) human cancer cell lines.

A series of 4beta-[(4-substituted)-1,2,3-triazol-1-yl] podophyllotoxin congeners have been designed and synthesized with significant regioselectivity by employing Cu(I) catalyzed 1,3-dipolar cycloaddition reaction of C4beta-azido podophyllotoxin and C4beta-azido-4'-O-demethyl podophyllotoxin with N-prop-2-yn-1-ylanilines. These compounds were evaluated for anticancer activity against a panel of seven human cancer cell lines. It was interesting to note that all the compounds exhibited promising activity especially against SF-295 (CNS), HCT-15 (colon) and 502713 (colon) cell lines. Compound 11e was found to be the most promising in this study.

Condensation of 9-chloro-2,4-(un)substituted acridines (1a-c) with various amines (2a-e) and 9-isothiocyanato-2,4-(un)substituted acridines (4a,b) with different amines (2a,b,d,e) gave condensed products 3a-o and 5a-g respectively. Compounds 3a-o and 5a-g were screened for anti-inflammatory activity at a dose of 50mg/kg p.o. Compound 3e exhibited 41.17% anti-inflammatory activity which is better than most commonly used standard drug ibuprofen which showed 39% anti-inflammatory (at 50mg/kg p.o.) activity. Anticancer activity evaluation of compounds 3a-o and 5a-g was carried out against a small panel of human cancer cell lines and compounds 3g, 3m and 5g exhibited good anticancer activity against breast (MCF-7), liver (HEP-2), colon (COLO-205, 502713, HCT-15), lung (A-549) and neuroblastoma (IMR-32) cancer cell lines at a concentration of 1 x 10(-5)M.

Condensation of 3,4-diaryl-2-imino-4-thiazoli-nes 1a-j with methanesulfonyl chloride gave methanesulfonamide derivatives 2a-j. Condensation of 2-cyanopyrazine, 4-cyanopyridine, and 2-cyanopyridine with 3,4-diaryl-2- imino-4-thiazolines 1h-m in the presence of sodium methoxide afforded amidine derivatives 3a-j. Compounds 2a-j and 3a-j were screened against various human cancer cell lines (COLO-205, HEP-2, A-549, IMR-32) and their percentage growth inhibition profile determined at 1 x 10(-5)M. The anti-inflammatory activity of these compounds was assessed using the carrageenan-induced paw edema model. Compound 2i exhibited 34.7% anti-inflammatory activity at 50 mg/kg p.o., which is comparable to standard care drug phenyl butazone (37% activity at 50 mg/kg p.o.).

A series of novel 4beta-[(4-substituted)-1,2,3-triazol-1-yl]podophyllotoxin derivatives were synthesized by employing Cu(I)-catalyzed click chemistry and evaluated for their anticancer activity against a panel of seven human cancer cell lines (HT-29, HCT-15, 502713, HOP-62, A-549, MCF-7, and SF-295). The compounds 9b, 9c, 9e, 9f, and 9h showed significant cytotoxic activities especially against HT-29, HCT-15, 502713 cell lines.

A series of 4beta-[(4-substituted)-1,2,3-triazol-1-yl]podophyllotoxin analogues have been synthesized with high regio-selectivity by employing copper(I)-catalyzed 1,3-dipolar cycloaddition of 1-O-propargyl monosaccharides with C4beta-azido podophyllotoxin and C4beta-azido-4'-O-demethyl podophyllotoxin. All the compounds were evaluated for their anticancer activity against a panel of six human cancer cell lines. Among these, 4'-O-demethyl podophyllotoxin congeners are showing promising anticancer activity mainly against HCT-15 (colon) and DU-145 (prostate) cells.

A series of 4beta-[(4-substituted)-1,2,3-triazol-1-yl]podophyllotoxin analogues have been synthesized with high regio-selectivity by employing copper(I)-catalyzed 1,3-dipolar cycloaddition of 1-O-propargyl monosaccharides with C4beta-azido podophyllotoxin and C4beta-azido-4'-O-demethyl podophyllotoxin. All the compounds were evaluated for their anticancer activity against a panel of six human cancer cell lines. Among these, 4'-O-demethyl podophyllotoxin congeners are showing promising anticancer activity mainly against HCT-15 (colon) and DU-145 (prostate) cells.

In the present investigation, the cytotoxic, hydroxyl radical scavenging and topoisomerase inhibition activities of Tabernaemontana divaricata (Apocynaceae) were evaluated. The extracts from leaves of the plant were prepared with different solvents viz. chloroform, methanol, ethyl acetate and hexane. In, in vitro cytotoxicity assay, with cell lines viz HCT-15 (Colon), HT-29 (Colon), 502713 (Colon), MCF-7 (Breast), PC- 3 (Prostrate), it was observed that the ethyl acetate extract was effective against only one colon cell line (502713) at the lowest dose i.e. 10 micro g/ml, whereas the chloroform extract was effective against all the three colon cancer cell lines, at 30 microg/ ml. In order to evaluate the mechanism of cytotoxicity of these extracts, they were assessed for their ability to scavenge hydroxyl radicals in plasmid nicking assay with pBR322. It was observed that all the extracts effectively inhibited the unwinding of supercoiled DNA except hexane extract, which showed the least effect. Since the expression of topo enzymes is linked with cell proliferation so the extracts were also checked for topo I and topo II inhibitory activities. It was noticed that ethyl acetate extract selectively showed inhibition of topo II in topoisomerase II relaxation assay.

A series of 4beta-[(4-substituted)-1,2,3-triazol-1-yl] podophyllotoxin congeners have been designed and synthesized with significant regioselectivity by employing Cu(I) catalyzed 1,3-dipolar cycloaddition reaction of C4beta-azido podophyllotoxin and C4beta-azido-4'-O-demethyl podophyllotoxin with N-prop-2-yn-1-ylanilines. These compounds were evaluated for anticancer activity against a panel of seven human cancer cell lines. It was interesting to note that all the compounds exhibited promising activity especially against SF-295 (CNS), HCT-15 (colon) and 502713 (colon) cell lines. Compound 11e was found to be the most promising in this study.