A Clinical and Dermatoscopic Perspective of the Efficacy and Safety of Erbium: YAG Laser Ablation Versus 50% Trichloroacetic Acid for the Management of Xanthelasma Palpebrarum.

Xanthelasma palpebrarum (XP) is a benign cosmetic condition. Although the role of CO2 laser is well described, there are only a few studies on Erbium: YAG in XP. Similarly, trichloroacetic acid (TCA) is commonly used in XP. However, there are only a few studies comparing these modalities in the treatment of XP. Aim: To evaluate the effectiveness and safety of Erbium: YAG laser and 50% TCA in the treatment of XP with the role of dermoscope in the evaluation of lesions. Materials and Methods: A total of 20 subjects were randomly allocated into two groups: group A (TCA) and group B (laser). All patients were subcategorized into three grades viz. I (mild), II (moderate), and III (severe) using a self-devised scoring system. Results: About 25% and 70% of patients achieved complete clearance in groups A and B, respectively (P = 0.017). The rate of recurrence was 40% and 15% in groups A and B. Dyspigmentation and erythema were the most common side effects. Pretreatment dermoscopic evaluation of the lesion showed a network of brown streaks on a background of a yellowish structureless area and was used to assess the area and margins of the lesion where the adipose tissue was found during the procedure and serial assessment of the lesion.

Efficacy of autologous platelet rich plasma with subcision vs platelet rich plasma with microneedling in atrophic acne scars: A single-center, prospective, intra-individual split-face comparative study.

Background: Severe post-acne scarring has been implicated as a cause of considerable psychological distress, mainly among adolescents. Subcision and microneedling are cutting-edge treatment options available nowadays. Aim: In this study, we aimed to compare the efficacy of microneedling with platelet-rich plasma (PRP) against subcision with PRP in treating atrophic post-acne scars in a split-face study design. Materials and Methods: Fifty patients with atrophic post-acne facial scars were included in this prospective interventional study. Group A included the left side of the face managed by microneedling with PRP and group B included the right side of the face that was subjected to subcision with PRP. Results were assessed based on Goodman and Baron qualitative and quantitative grading. Results: In our study, at the end of the treatment, on the left side, 5 (10%) had 1 grade of improvement showing good response, 35 (70%) had 2 grades of improvement showing very good response, and 10 (20%) had 3 grades of improvement showing excellent response. On the right side, 1 (2%) patient had no improvement in acne grade showing poor response, 9 (18%) had 1 grade of improvement showing good response, 25 (50%) had 2 grades of improvement showing very good response, whereas 15 (30%) had 3 grades of improvement showing excellent response. Conclusion: Till date, apart from ours no other study has compared the two modalities head-to-head with adjuvant PRP in both groups. Although both modalities showed statistically significant results individually, there was no significant difference in qualitative improvement of acne scars between the two groups.

MAFB in macrophages regulates cold-induced neuronal density in brown adipose tissue.

Transcription factor MAFB regulates various homeostatic functions of macrophages. This study explores the role of MAFB in brown adipose tissue (BAT) thermogenesis using macrophage-specific Mafb-deficient (Mafbf/f::LysM-Cre) mice. We find that Mafb deficiency in macrophages reduces thermogenesis, energy expenditure, and sympathetic neuron (SN) density in BAT under cold conditions. This phenotype features a proinflammatory environment that is characterized by macrophage/granulocyte accumulation, increases in interleukin-6 (IL-6) production, and IL-6 trans-signaling, which lead to decreases in nerve growth factor (NGF) expression and reduction in SN density in BAT. We confirm MAFB regulation of IL-6 expression using luciferase readout driven by IL-6 promoter in RAW-264.7 macrophage cell lines. Immunohistochemistry shows clustered organization of NGF-producing cells in BAT, which are primarily TRPV1+ vascular smooth muscle cells, as additionally shown using single-cell RNA sequencing and RT-qPCR of the stromal vascular fraction. Treating Mafbf/f::LysM-Cre mice with anti-IL-6 receptor antibody rescues SN density, body temperature, and energy expenditure.

IL-27-containing exosomes secreted by innate B-1a cells suppress and ameliorate uveitis.

Introduction: IL-27 is a heterodimeric cytokine composed of Ebi3 and IL-27p28 and can exert proinflammatory or immune suppressive effects depending on the physiological context. Ebi3 does not contain membrane-anchoring motifs, suggesting that it is a secreted protein while IL-27p28 is poorly secreted. How IL-27p28 and Ebi3 dimerize in-vivo to form biologically active IL-27 is unknown. Major impediment to clinical use of IL-27 derives from difficulty of determining exact amount of bioavailable heterodimeric IL-27 needed for therapy. Methods: To understand how IL-27 mediates immune suppression, we characterized an innate IL-27-producing B-1a regulatory B cell population (i27-Breg) and mechanisms i27-Bregs utilize to suppress neuroinflammation in mouse model of uveitis. We also investigated biosynthesis of IL-27 and i27-Breg immunobiology by FACS, immunohistochemical and confocal microscopy. Results: Contrary to prevailing view that IL-27 is a soluble cytokine, we show that i27-Bregs express membrane-bound IL-27. Immunohistochemical and confocal analyses co-localized expression of IL-27p28 at the plasma membrane in association with CD81 tetraspanin, a BCR-coreceptor protein and revealed that IL-27p28 is a transmembrane protein in B cells. Most surprising, we found that i27-Bregs secrete IL-27-containing exosomes (i27-exosomes) and adoptive transfer of i27-exosomes suppressed uveitis by antagonizing Th1/Th17 cells, up-regulating inhibitory-receptors associated with T-cell exhaustion while inducing Treg expansion. Discussion: Use of i27-exosomes thus obviates the IL-27 dosing problem, making it possible to determine bioavailable heterodimeric IL-27 needed for therapy. Moreover, as exosomes readily cross the blood-retina-barrier and no adverse effects were observed in mice treated with i27-exosome, results of this study suggest that i27-exosomes might be a promising therapeutic approach for CNS autoimmune diseases.

Urinary flow rates in anterior hypospadias: Before and after repair and its clinical implication.

Context: Hypospadias is a common urological anomaly which could be surgically corrected with good cosmetic results. Aims: We aimed to detect changes in urinary flow parameters both before and after tubularised incised plate urethroplasty (TIPU) using uroflowmetry. Settings and Design: Data collected were clinically implemented hypothesising the probability of urethrocutaneous fistula following stricture with Qmax variation. Materials and Methods: This study is a prospective analysis done from December 2017 to October 2019. A total of 104 cases of anterior hypospadias were included in the study. A single surgical unit did TIPU. Pre-operative and post-operative uroflowmetry was done, and Qmax was recorded at 3 months, 6 months and 1 year after surgery. Mean Qmax was calculated for all intervals. A significant decrease in Qmax of a child (<2 standard deviation) was ascertained. Urethral calibration was done in those cases with a significant decrease of Qmax and analysed statistically. Results: The mean age was 6.97 ± 2.41 years. Out of 104 children, 73 (70.2%) and 31 (29.8%) had distal and mid-shaft hypospadias, respectively. The pre-operative mean Qmax of the population was 6.20 ± 0.42 ml/s. Arithmetic mean Qmax at 3 months, 6 months and 1 year was 8.53 ± 0.42, 11.18 ± 0.47 and 13.71 ± 0.44 ml/s, respectively. On comparing the pre-operative with post-operative mean Qmax, a significant increase was found postoperatively (P < 0.0001). Twenty-four patients had significantly decreased Qmax value after 6 months. In these patients, follow-up urethral dilation was done with significant improvement. Conclusion: The changes in maximum flow rate (Qmax) are suitable for use in routine follow-up. A significant decrease in Qmax over time indicates the onset of urethral stricture. These cases are to be intervened before venturing to redo urethroplasty.

Fractional Erbium YAG Laser Resurfacing Versus 20% Trichloroacetic Acid Chemical Peeling in the Treatment of Acne Scars: A Comparative Study.

Background: Acne scarring not only affects the aesthetic appearance of an individual but also has a detrimental effect on mental health and social life. Various treatment modalities are available for acne scars. Aim: In this study, fractional erbium-doped yttrium-aluminum-garnet (Er:YAG) laser resurfacing was compared with 20% trichloroacetic acid (TCA) peeling in terms of efficacy and safety. Materials and Methods: This prospective comparative study included 50 subjects of acne scar who were randomly divided into Groups A and B, 25 patients in each group. Group A was treated with 4 sessions of fractional Er:YAG laser and Group B with 4 session of 20% TCA application as chemical peeling, repeated every 21 days over a period of 3 months. The patients were evaluated for improvement at each visit using Goodman and Baron's qualitative and quantitative acne scar grading. Results: Statistically significant improvement in Goodman and Barron's qualitative acne scar grades was observed in both groups. At the end of therapy, that is, after 12 weeks of therapy, the mean percentage reduction in Goodman and Baron's quantitative acne scar scores was 21.69% ± 16% in Group A and 20.97% ± 8.70% in Group B. In regards of complications, both procedures were well tolerated. Conclusion: We concluded that fractional Er:YAG laser resurfacing and 20% TCA peel application in the treatment of atrophic acne scar are equally efficacious. Both procedures are safe and well tolerated by the patients.

Transcription Factor MAFB as a Prognostic Biomarker for the Lung Adenocarcinoma.

MAFB is a basic leucine zipper (bZIP) transcription factor specifically expressed in macrophages. We have previously identified MAFB as a candidate marker for tumor-associated macrophages (TAMs) in human and mouse models. Here, we analyzed single-cell sequencing data of patients with lung adenocarcinoma obtained from the GEO database (GSE131907). Analyzed data showed that general macrophage marker CD68 and macrophage scavenger receptor 1 (CD204) were expressed in TAM and lung tissue macrophage clusters, while transcription factor MAFB was expressed specifically in TAM clusters. Clinical records of 120 patients with lung adenocarcinoma stage I (n = 57), II (n = 21), and III (n = 42) were retrieved from Tsukuba Human Tissue Biobank Center (THB) in the University of Tsukuba Hospital, Japan. Tumor tissues from these patients were extracted and stained with anti-human MAFB antibody, and then MAFB-positive cells relative to the tissue area (MAFB+ cells/tissue area) were morphometrically quantified. Our results indicated that higher numbers of MAFB+ cells significantly correlated to increased local lymph node metastasis (nodal involvement), high recurrence rate, poor pathological stage, increased lymphatic permeation, higher vascular invasion, and pleural infiltration. Moreover, increased amounts of MAFB+ cells were related to poor overall survival and disease-free survival, especially in smokers. These data indicate that MAFB may be a suitable prognostic biomarker for smoker lung cancer patients.

Probiotics, prebiotics and synbiotics: Safe options for next-generation therapeutics.

Probiotics have been considered as an economical and safe alternative for the treatment of a large number of chronic diseases and improvement of human health. They are known to modulate the host immunity and protect from several infectious and non-infectious diseases. The colonization, killing of pathogens and induction of host cells are few of the important probiotic attributes which affect several functions of the host. In addition, prebiotics and non-digestible food substances selectively promote the growth of probiotics and human health through nutrient enrichment, and modulation of gut microbiota and immune system. This review highlights the role of probiotics and prebiotics alone and in combination (synbiotics) in the modulation of immune system, treatment of infections, management of inflammatory bowel disease and cancer therapy. KEY POINTS: • Probiotics and their derivatives against several human diseases. • Prebiotics feed probiotics and induce several functions in the host. • Discovery of novel and biosafe products needs attention for human health.

Impact of ErbB Receptors and Anticancer Drugs against Breast Cancer: A Review.

Human EGFR (epidermal growth factor receptor) family of tyrosine kinase receptors consists of four members, ErbB1-4. Abnormalities in the ErbB family characterize a variety of human cancers, including breast cancer. Tyrosine kinase is recruited by the activated EGFR cell surface receptor, which transmitted signals from the receptor to interact with intracellular signaling pathways and regulate cellular functions and biological processes. Targeting the intracellular signaling pathways has been aided in the drug development that was already in use and more continually being developed. The review article highlights the function of ErbB receptors/ligands, their role in signaling pathways, effective targeted drugs, and a combination of targeted drug strategies in the treatment of breast cancer that could be leading to the novel combination of anticancer drug delivery systems.

Modeling defluoridation of real-life groundwater by a green adsorbent aluminum/olivine composite: Isotherm, kinetics, thermodynamics and novel framework based on artificial neural network and support vector machine.

The kinetic, isotherm, and thermodynamics of adsorptive removal of fluoride from the real-life groundwater was evaluated to assess the applicability of a green adsorbent, aluminum/olivine composite (AOC). The isotherm and kinetics were demonstrated by the Freundlich and Elovich model indicating significant surface heterogeneity of AOC in favouring the fluoride sorption. The fluoride removal efficiency of AOC was achieved as 87.5% after 240 min of contact time. The diffusion kinetic model exhibited that both the intra-particle and film diffusion together control the rate-limiting step of fluoride adsorption. A negative value of ΔG0 (-19.919 kJ/mol) at 303 K confirmed the spontaneous adsorption reaction of fluoride, and its endothermic nature was supported by the negative value of ΔH0 (39.504 kJ/mol). A novel framework for a predictive model by artificial neural network (ANN), and support vector machine (SVM) considering the real and synthetic fluoride-containing water was developed to assess the efficiency of adsorbent under different scenarios. ANN model was observed to be statistically significant (RMSE: 1.0955 and R2: 0.9982) and the proposed method may be instrumental in a similar area for benchmarking the synthetic and real-life samples. The low desorption potential of the spent adsorbent exhibited safe disposal of sludge and the secondary-pollutant-free treated water by the efficient and green adsorbent AOC enhanced the field-scale applicability of the green technology.

Neuroprotective effects of arbutin against oxygen and glucose deprivation-induced oxidative stress and neuroinflammation in rat cortical neurons.

In this study, the neuroprotective potential of arbutin (100 µmol L-1) pre-treatment and post-treatment against oxygen/ glucose deprivation (OGD) and reoxygenation (R) induced ischemic injury in cultured rat cortical neurons was explored. The OGD (60 min) and reoxygenation (24 h) treatment significantly (p < 0.001) compromised the antioxidant defence in cultured neurons. Subsequently, an increase (p < 0.001) in lipid peroxidation and inflammatory cytokines (tumour necrosis factor-α and nuclear factor kappa-B) declined neuron survival. In pre- and post-condition experiments, treatment with arbutin enhanced both survival (p < 0.01) and integrity (p < 0.05) of cultured neurons. Results showed that arbutin protects (p < 0.05) against peroxidative changes, inflammation, and enhanced the antioxidant activity (e.g., glutathione, superoxide dismutase and catalase) in cultured neurons subjected to OGD/R. It can be inferred that arbutin could protect against ischemic injuries and stroke. The anti-ischemic activity of arbutin can arrest post-stroke damage to the brain.

Albino mice with the point mutation at the tyrosinase locus show high cholesterol diet-induced NASH susceptibility.

Non-alcoholic fatty liver disease (NAFLD) constitutes a metabolic disorder with high worldwide prevalence and increasing incidence. The inflammatory progressive state, non-alcoholic steatohepatitis (NASH), leads to liver fibrosis and carcinogenesis. Here, we evaluated whether tyrosinase mutation underlies NASH pathophysiology. Tyrosinase point-mutated B6 (Cg)-Tyrc-2J/J mice (B6 albino) and C57BL/6J black mice (B6 black) were fed with high cholesterol diet (HCD) for 10 weeks. Normal diet-fed mice served as controls. HCD-fed B6 albino exhibited high NASH susceptibility compared to B6 black, a phenotype not previously reported. Liver injury occurred in approximately 50% of B6 albino from one post HCD feeding, with elevated serum alanine aminotransferase and aspartate aminotransferase levels. NASH was induced following 2 weeks in severe-phenotypic B6 albino (sB6), but B6 black exhibited no symptoms, even after 10 weeks. HCD-fed sB6 albino showed significantly higher mortality rate. Histological analysis of the liver revealed significant inflammatory cell and lipid infiltration and severe fibrosis. Serum lipoprotein analysis revealed significantly higher chylomicron and very low-density lipoprotein levels in sB6 albino. Moreover, significantly higher small intestinal lipid absorption and lower fecal lipid excretion occurred together with elevated intestinal NPC1L1 expression. As the tyrosinase point mutation represents the only genetic difference between B6 albino and B6 black, our work will facilitate the identification of susceptible genetic factors for NASH development and expand the understanding of NASH pathophysiology.

Vitreous substitutes: An overview of the properties, importance, and development.

Vitreous or vitreous humor is a complex transparent gel that fills the space between the lens and retina of an eye and acts as a transparent medium that allows light to pass through it to reach the photoreceptor layer (retina) of the eye. The vitreous humor is removed in ocular surgery (vitrectomy) for pathologies like retinal detachment, macular hole, diabetes-related vitreous hemorrhage detachment, and ocular trauma. Since the vitreous is not actively regenerated or replenished, there is a need for a vitreous substitute to fill the vitreous cavity to provide a temporary or permanent tamponade to the retina following some vitreoretinal surgeries. An ideal vitreous substitute could probably be left inside the eye forever. The vitreous humor is transparent, biocompatible, viscoelastic and highly hydrophilic; polymeric hydrogels with these properties can be a potential candidate to be used as vitreous substitutes. To meet the tremendous demand for the vitreous substitute, many scientists all over the world have developed various kinds of vitreous substitutes or tamponade agent. Vitreous substitutes, whatsoever developed till date, are associated with several advantages and disadvantages, and there is no ideal vitreous substitute available till date. This review highlights the polymer-based vitreous substitutes developed so far, along with their advantages and limitations. The gas-based and oil-based substitutes have also been discussed but very briefly.

Low-dose naltrexone rescues inflammation and insulin resistance associated with hyperinsulinemia.

The incidence of diabetes, obesity, and metabolic diseases has reached an epidemic status worldwide. Insulin resistance is a common link in the development of these conditions, and hyperinsulinemia is a central hallmark of peripheral insulin resistance. However, how hyperinsulinemia leads to systemic insulin resistance is less clear. We now provide evidence that hyperinsulinemia promotes the release of soluble pro-inflammatory mediators from macrophages that lead to systemic insulin resistance. Our observations suggest that hyperinsulinemia induces sirtuin1 (SIRT1) repression and stimulates NF-κB p65 nuclear translocation and transactivation of NF-κB to promote the extracellular release of pro-inflammatory mediators. We further showed that low-dose naltrexone (LDN) abrogates hyperinsulinemia-mediated SIRT1 repression and prevents NF-κB p65 nuclear translocation. This, in turn, attenuates the hyperinsulinemia-induced release of pro-inflammatory cytokines and reinstates insulin sensitivity both in in vitro and in vivo diet-induced hyperinsulinemic mouse model. Notably, our data indicate that Sirt1 knockdown or inhibition blunts the anti-inflammatory properties of LDN in vitro Using numerous complementary in silico and in vitro experimental approaches, we demonstrated that LDN can bind to SIRT1 and increase its deacetylase activity. Together, these data support a critical role of SIRT1 in inflammation and insulin resistance in hyperinsulinemia. LDN improves hyperinsulinemia-induced insulin resistance by reorienting macrophages toward anti-inflammation. Thus, LDN treatment may provide a novel therapeutic approach against hyperinsulinemia-associated insulin resistance.

Remediation of carcinogenic arsenic by pyroaurite-based green adsorbent: isotherm, kinetic, mechanistic study, and applicability in real-life groundwater.

The removal of the harmful carcinogen arsenic from drinking water by a green technology is a major concern in the field of environmental engineering. The sorptive profile of arsenic remediation by calcined Mg-Fe-layered double hydroxide, fabricated by a one-pot synthesis technique, was investigated to delineate its applicability in real-life water. The physicochemical properties of adsorbent, as demonstrated from spectroscopy and microscopy, which described the existence of amorphous material with significant surface roughness possess selectivity towards arsenic. The isotherm and kinetic along with thermodynamic modeling exhibited the occurrence of spontaneous (ΔG0 value = - 8.084 kJ/mol to - 10.942 kJ/mol), endothermic (ΔH0 value = 12.135 kJ/mol), and physisorption reactions (Ead = 4.103-5.832 kJ/mol, Ea = 11.546 kJ/mol, S* = 0.0005 << 1, and ΔHx = 9.23-16.29 kJ/mol) with high uptake rate and adsorption potential of adsorbent. The isotherm and kinetics were demonstrated by Temkin (R2 = 0.944-0.969) and Elovich (R2 = 0.996-0.998) models, respectively, with high statistical significance. The intraparticle diffusion model which established the rate-limiting step is the combination of both film and pore diffusions. The applicability of layered double hydroxide (LDH) material in the real-life water was confirmed by isotherm and kinetic modeling along with the regeneration/reuse potential. The adsorptive removal of arsenic by the LDH material exhibited to be a promising technique without creating any secondary hazard.

Role of MafB in macrophages.

The transcription factor MafB regulates macrophage differentiation. However, studies on the phenotype of Mafb-deficient macrophages are still limited. Recently, it was shown that the specific expression of MafB permits macrophages to be distinguished from dendritic cells. In addition, MafB has been reported to be involved in various diseases related to macrophages. Studies using macrophage-specific Mafb-deficient mice show that MafB is linked to atherosclerosis, autoimmunity, obesity, and ischemic stroke, all of which exhibit macrophage abnormality. Therefore, MafB is hypothesized to be indispensable for the regulation of macrophages to maintain systemic homeostasis and may serve as an innovative target for treating macrophage-related diseases.

Transcription factor MafB is a marker of tumor-associated macrophages in both mouse and humans.

The transcription factor MafB is specifically expressed in macrophages. We have recently demonstrated that MafB is expressed in anti-inflammatory alternatively activated M2 macrophages in vitro. Tumor-associated macrophages (TAMs) are a subset of M2 type macrophages that can promote immunosuppressive activity, induce angiogenesis, and promote tumor cell proliferation. To examine whether MafB express in TAMs, we analyzed green fluorescent protein (GFP) expression in Lewis lung carcinoma tumors of MafB-GFP knock-in heterozygous mice. FACS analysis demonstrated GFP fluorescence in cells positive for macrophage-markers (F4/80, CD11b, CD68, and CD204). Moreover, quantitative RT-PCR analysis with F4/80+GFP+ and F4/80+GFP- sorted cells showed that the GFP-positive macrophages express IL-10, Arg-1, and TNF-α, which were known to be expressed in TAMs. These results indicate that MafB is expressed in TAMs. Furthermore, immunostaining analysis using an anti-MAFB antibody revealed that MAFB is expressed in CD204-and CD68-positive macrophages in human lung cancer samples. In conclusion, MafB can be a suitable marker of TAMs in both mouse and human tumor tissues.

Minimally invasive transgingival implant therapy: A literature review.

Transgingival (flapless) implant placement procedure is a minimally invasive surgical technique in which implant is placed without reflecting mucoperiosteal flap and hence the blood supply of bone is not hampered which is advantageous in many ways. To compare the outcomes of various implant placement techniques, an electronic database of various journals from January 1990 to March 2017 were analyzed and only human clinical trials with 6 months follow-up and at least five implants in each group were reviewed. The present literature review focuses on the comparative aspects of flapped versus flapless implants in terms of their survival, marginal bone loss, soft-tissue parameters, and patient-centered outcomes. When the proper protocol is followed by experienced surgeons, no significant difference was observed in survival rate, marginal bone loss, and keratinized mucosal width between flapless and conventional flap technique. Although transgingival approach for implant placement is reported to significantly reduce the surgical time, increased patient comfort and acceptance, i.e. the patient centered outcomes such as postoperative pain, swelling, and visual analog score, are minimized. Hence, it is concluded that transgingival (flapless) implant placement technique is well accepted by the patient with potential outcomes as compared to the conventional implant placement approach.

Identification and characterization of ErbB4 kinase inhibitors for effective breast cancer therapy.

The overexpression of ErbB4 is associated with aggressive disease biology and reduced the survival of breast cancer patients. We have used ErbB4 receptor as a novel drug target to spearhead the rational drug design. The present study is divided into two parts. In the first part, we have exploited the hidden information inside ErbB4 kinase receptor both at sequence and structural level. PSI-BLAST algorithm is used to search similar sequences against ErbB4 kinase sequence. Top 15 sequences with high identity were selected for finding conserved and variable regions among sequences using multiple sequence alignment. In the second part, available 3 D structure of ErbB4 kinase is curated using loop modeling, and anomalies in the modeled structure is improved by energy minimization. The resultant structure is validated by analyzing dihedral angles by Ramachandran plot analysis. Furthermore, the potential binding sites were detected by using DoGSite and CASTp server. The similarity-search criterion is used for the preparation of our in-house database of drugs from DrugBank database. In total, 409 drugs yet to be tested against ErbB4 kinase is used for screening purpose. Virtual screening results in identification of 11 compounds with better binding affinity than lapatinib and canertinib. Study of protein-ligand interactions reveals information about amino acid residues; Lys726, Thr771, Met774, Cys778, Arg822, Thr835, Asp836 and Phe837 at the binding pocket. The physicochemical properties and bioactivity score calculation of selected compounds suggest them as biological active. This study presents a rich array that assist in expediting new drug discovery for breast cancer.

Phospholipid/Polydiacetylene Vesicle-Based Colorimetric Assay for High-Throughput Screening of Bacteriocins and Halocins.

The colorimetric assay is phospholipid/polydiacetylene vesicle-based assay used for the detection of membrane-acting peptides. Bacteriocins and halocins are antimicrobial peptides known to kill target cells by membrane disruption. Therefore, the assay was applied for high-throughput (HTP) screening of bacteriocins and halocins produced by lactic acid bacteria and haloarchaea, respectively. The assay consisted of vesicles which were synthesized using four different phospholipids: dipalmitoylphosphatydilcholine (DPPC), dimyristoylphosphatidylcholine (DMPC), dimyristoylphosphoethanolamine (DMPE) and dimyristoylphosphatidylglycerol (DMPG) in combination with diacetylene monomer 10,12-tricosadiy noic acid (TRCDA). These vesicles demonstrated blue colour at 640 nm and turned pink/red after interaction with nisin. DMPE/TRCDA vesicles showed pink colour with the highest colorimetric response (CR %) after treatment with nisin and, therefore, selected for the screening of bacteriocins and halocins. The colour of the vesicles was changed within 5 min in the presence of 5 µM nisin suggesting the sensitivity of assay. The assay was applied on 54 strains of lactic acid bacteria (LAB) and 53 haloarchaea for screening of bacteriocins and halocins, respectively. Out of these strains, three strains of LAB and five strains of haloarchaea were found to be bacteriocin and halocin non-producer, respectively. The other strains demonstrated the presence of bacteriocins and halocins. The colorimetric assay was found to be rapid, specific and reliable for HTP screening of antimicrobial peptides such as bacteriocins and halocins from producer strains isolated from various natural resources.