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The Pd(0) catalysed cyclisation reactions between tert-butyl propargyl carbonates and 2-aminotosyl benzamides or sulphonamides deliver 1,4-benzodiazepin-5-ones or sultam derivatives, key components of many biologically active compounds. But 2-amino benzamides/sulphonamides require propargyl carbonates substituted at acetylenic carbon to undergo the reaction resulting in the stereoselective formation of the said products.

Genetic variation in susceptibility to complex diseases, such as cancer, is well-established. Enrichment of disease associated alleles in specific populations could have implications for disease incidence and prevalence. Prostate cancer (PCa) is a disease with well-established higher incidence, prevalence, and worse outcomes among men of African ancestry in comparison to other populations. PCa is a multi-factorial, complex disease, but the exact mechanisms for its development and progression are unclear. The gene desert located on chromosome 8q24 is associated with aggressiveness of PCa. Interestingly, the non-protein coding gene locus Plasmacytoma Variant Translocation (PVT1) is present at chromosome 8q24 and is overexpressed in PCa. PVT1 gives rise to multiple transcripts with potentially different molecular and cellular functions. In an analysis of the PVT1 locus using data from the 1000 Genomes Project, we found the chromosomal region spanning PVT1 exons 4A and 4B to be highly differentiated between African and non-African populations. We further investigated levels of gene expression of PVT1 exons 4A and 4B and observed significant overexpression of these exons in PCa tissues relative to benign prostatic hyperplasia and to normal prostate tissues obtained from men of African ancestry. These results indicate that PVT1 exons 4A and 4B may have clinical implications in PCa a conclusion supported by the observation that transient and stable overexpression of PVT1 exons 4A and 4B significantly induce greater prostate epithelial cell migration and proliferation. We anticipate that further exploration of the role of PVT1 exons 4A and 4B may lead to the development of diagnostic, therapeutic, and other clinical applications in PCa.

Chromosome 8q24 is of particular importance for cancer susceptibility. Located in this region is the Plasmacytoma Variant Translocation 1 (PVT1) gene, a long noncoding RNA that has been implicated in multiple cancers including prostate cancer. Amplification of the PVT1 gene locus is a common event in many malignant diseases and is associated with poor clinical outcomes. The pioneering role of PVT1, and its alternatively spliced transcripts, as a cancer biomarker is progressively becoming established. We have demonstrated that copy numbers of PVT1 exons 4A, 4B and 9 is quantifiable in cancer cells, tissue, and serum from cancer patients. In this study, we assessed clinically annotated serum samples from 40 prostate cancer patients to investigate the clinical relevance of PVT1 exons 4A, 4B, and 9 as a biomarker across cancer risk levels and ethnicity/race. Explorative data analysis for the development of composite score for prostate cancer was performed using Kruskal-Wallis Rank Sum Test. We observed significantly higher copy numbers of PVT1 exons 4B and 9 across all races (White, Black and Hispanic) and Blacks and Hispanics when compared to the control. Additionally, using a 3-level cancer risk rating assessment in which 0 = healthy, 1 = low risk and 2 = high risk, we observed that PVT1 exon 9 may distinguish between cancerous and noncancerous cases across all races, but may not help distinguish between indolent and aggressive cancer cases. Notably, PVT1 exon 4B may help distinguish between indolent and aggressive cancer cases for Blacks and Hispanics. The results of this study suggest that using PVT1 exon 4B or 9 may identify cancer regardless of ethnicity/race, and that utilization of serum PVT1 exon 4B copy number may help distinguish between indolent and aggressive prostate cancer in Blacks and Hispanics. Citation Format: Fayola Levine, Emmanuel Asante-Asamani, Gargi Pal, Michael Liss, Olorunseun Ogunwobi. Investigating the clinical relevance in prostate cancer of the serum biomarkers PVT1 exons 4A, 4B and 9 across risk levels and ethnicity/race [abstract]. In: Proceedings of the 15th AACR Conference on the Science of Cancer Health Disparities in Racial/Ethnic Minorities and the Medically Underserved; 2022 Sep 16-19; Philadelphia, PA. Philadelphia (PA): AACR; Cancer Epidemiol Biomarkers Prev 2022;31(1 Suppl):Abstract nr C060.

The Pd(0) catalysed cyclisation reactions between tert-butyl propargyl carbonates and 2-aminotosyl benzamides or sulphonamides deliver 1,4-benzodiazepin-5-ones or sultam derivatives, key components of many biologically active compounds. But 2-amino benzamides/sulphonamides require propargyl carbonates substituted at acetylenic carbon to undergo the reaction resulting in the stereoselective formation of the said products.

Prostate cancer (PCa) is the most commonly diagnosed solid organ cancer in men worldwide. Current diagnosis of PCa includes use of initial prostate specific antigen assay which has a high false positive rate, low specificity, and low sensitivity. The side effects of unnecessary prostate biopsies that healthy men are subjected to, often result in unintended health complications. New PCa biomarkers are being discovered to address this unmet need. Here, we report on the creation of a composite score (Prostac) based on three recently discovered PCa biomarkers, Plasmacytoma Variant Translocation 1 (PVT1) exons 4A, 4B, and 9. Statistical analysis of copy numbers derived from a real-time quantitative polymerase chain (qPCR) reaction - based assay, showed these PCa biomarkers to be linearly separable and significantly over expressed in PCa epithelial cells. We train a supervised learning algorithm using support vector machines to generate a classification hyperplane from which a user-friendly composite score is developed. Cross validation of Prostac using data from prostate epithelial cells (RWPE1) and PCa cells (MDA PCa 2b) accurately classified 100% of PCa cells. Creation of the Prostac score lays the groundwork for clinical trial of its use in PCa diagnosis.

Background: The Temple University Fox Chase Cancer Center and Hunter College Cancer Health Disparity Partnership (TUFCCC/HC Cancer Partnership) is a collaborative effort to develop a regional comprehensive collaborative cancer health equity research infrastructure in Pennsylvania, New Jersey and New York City (PNN) Region and to establish rigorous and sustainable cancer research, education, and outreach programs at both institutions. One key component of the training efforts of this Partnership is the annual Summer Cancer Research Institute (SCRI), an 8-week intensive summer program that includes hands-on research training in laboratories or research centers under the mentorship of established investigators supplemented with cancer seminars, skill-building workshops, journal clubs, social activities, poster sessions and presentations. Methods: The goal of this study was to evaluate the recruitment process and the outcome of the first three cohorts of the SCRI. We assessed the previous recruitment and implementation process to identify successes and lessons learned. We also conducted program evaluation through pre-program and post-program evaluation, and long-term annual follow-up survey, and other formal and informal feedback among the 3 cohorts from the previous 3 years. Results: Through targeted multi-institutional recruitment strategies and by utilizing social media (e.g., Twitter, Instagram, institutional newsletters), the program received increasing numbers of applications each year, from 64 applications received in 2019, to 179 in 2020, and 345 in 2021. The number of students accepted were 10 in 2019 (admission rate 15.6%), 10 in 2020 (5.6%), and 15 in 2021 (4.3%). Among the 34 SCRI trainees, 10 (29.4%) identified as Black/African American, 6 (17.5%) as Hispanic/Latinx, 10 (29.4%) as Asian, and the rest as non-Hispanic white. Students come from a variety of majors, including biology, nutrition, biochemistry, bioengineering, public health, sociology, and medical geography. The SCRI trainees reported a high level of satisfaction with the overall SCRI program as well as the specific seminars, workshops, and journal clubs. The long-term follow-up survey data showed that among the first two cohorts (20 trainees), 4 applied to graduate or medical school, 9 completed graduate school, and 7 accepted a full-time or part-time job position. Trainees particularly enjoyed the hands-on experience in basic, translation, and population research, the skill-building workshops, and the annual symposium to gain presentation experience. Conclusion: The Partnership evaluation has identified strengths (e.g., hands-on research experience under established mentorship, multidisciplinary training) for implementing the SCRI program. Updates are being made to refine recruitment processes and adjust program components. Citation Format: Lin Zhu, Gargi Pal, Taylor Kazaoka, Rubia Shahbaz, Marsha Zibalese-Crawford, Sarah-Jane Dodd, Carolyn Y. Fang, Yin Tan, Grace X. Ma, Olorunseun O. Ogunwobi. Educating the next generation of cancer researchers: Evaluation of a cancer research partnership research training program [abstract]. In: Proceedings of the AACR Virtual Conference: 14th AACR Conference on the Science of Cancer Health Disparities in Racial/Ethnic Minorities and the Medically Underserved; 2021 Oct 6-8. Philadelphia (PA): AACR; Cancer Epidemiol Biomarkers Prev 2022;31(1 Suppl):Abstract nr PO-212.

Adult males of Cryptotendipes aculeatus sp. nov. and Cryptotendipes disparilis sp. nov. are described and illustrated from India. This is the first record of the genus Cryptotendipes Lenz f...

Pre-imaginal and adult stages of both sexes of Glyptotendipes (Glyptotendipes) harpagatus sp. nov. are described and illustrated. A revised key to adult males of the Oriental species is also provided. http://www.zoobank.org/urn:lsid:zoobank.org:pub:8B784698-35A3-41A2-940C-8895797D0FBA

Summary: Prostate cancer (PCa) is the most commonly diagnosed solid organ cancer in men worldwide. Current diagnosis of PCa includes use of initial prostate specific antigen assay which has a high false positive rate, low specificity, and low sensitivity. Consequently, it results in overdiagnosis and overtreatment, leaving patients with unintended health complications from the side effects of unnecessary prostate biopsies and treatment. PCa biomarkers are being discovered to address this unmet need. Here, we report creation of a composite score based on three PCa biomarkers, plasmacytoma variant translocation 1 exon 4A, exon 4B, and exon 9. Statistical analysis of copy numbers derived from a real-time quantitative polymerase chain reaction - based assay showed these PCa biomarkers to be linearly separable. We trained a supervised learning algorithm using support vector classifiers to generate a classification hyperplane from which a composite score is developed. Our aggregate score when applied to test data from non-cancerous prostate epithelial cells and PCa cells accurately classified 100% PCa cells. Creation of this 3-biomarker based composite score lays the groundwork for clinical trial of its use in PCa diagnosis. Citation Format: Gargi Pal, Emmanuel Asante-Asamani, Leslie Liu, Olorunseun O. Ogunwobi. Computation of a user-friendly composite score from three prostate cancer biomarkers [abstract]. In: Proceedings of the American Association for Cancer Research Annual Meeting 2021; 2021 Apr 10-15 and May 17-21. Philadelphia (PA): AACR; Cancer Res 2021;81(13_Suppl):Abstract nr 2391.

Background One of the most important susceptibility loci for cancer is the 8q24 human chromosomal region. The non-protein coding gene locus plasmacytoma variant translocation 1 (PVT1) is located at 8q24 and is dysregulated in prostate cancer. PVT1 gives rise to multiple transcripts which may have different functions. Here, we describe a real-time quantitative polymerase chain reaction (qPCR)-based assay for copy number-based quantitation of PVT1 exons 4A, 4B, and 9 to enable accurate, reproducible, and quantifiable detection. Methods PVT1 exons 4A, 4B, and 9 were cloned into a plasmid vector to create standards for subsequent creation of linear standard curves representing a broad range of concentrations. PCR was carried out using SYBR-Green signal detection to quantify PVT1 exons 4A, 4B, and 9. The efficacy of this assay was evaluated by using it to detect these transcripts in prostate epithelial and prostate cancer cell lines, normal and cancerous human prostate tissues, human serum, mouse plasma, and urine samples. Results The results indicate that the assay can be used to quantify both low and high copy numbers of PVT1-derived transcripts. This is the first report of a copy number-based quantification assay for non-invasive detection of PVT1 derived transcripts. Conclusions This novel assay holds promise for routine non-invasive testing in diseases where PVT1 is dysregulated.

AIM: This study analyses the socio-demographic characteristics associated with post-sterilization regret. STUDY DESIGN: The study uses cross-sectional data from the fourth round of National Family Health Surveys (2015–2016). METHODS: Simple bivariate and binary logistic regressions analyses were used. RESULTS: Research shows that 7% of women aged 15–49 reported sterilization regret, which increased by 2% from 2005 to 2016. It was found that factors significantly associated with sterilization regret were years since sterilization, child loss experience, regions of residence, and quality of services. Women who got sterilized at the age of 30 or more were more likely to express regret, than women who were sterilised before 25 years of age, when adjusted for confounding variables (aO.R= 1.006). Women having sons were less likely to report sterilization regret than women who had only daughters (aO.R.=1.3 for each) but on the contrary women having both son and daughter are significantly less likely to express regret in comparison with women having only sons (aO.R. = 0.8 for each. Women who had experienced child loss had higher odds of reporting sterilization regret in rural (aO.R =1.2) as well as in urban (aO.R = 1.3) areas respectively, compared to those who did not experience any child loss. CONCLUSION: Women need to be counselled about the permanent nature of sterilization in order to avoid future regret as sterilization is largely dominated by socio-economic conditions. Thus, couples’ decision-making towards using the contraceptive from the basket of choice would help in uplifting the social and cultural status of women in conservative societies and will have a positive effect on contraceptive use. In addition, efforts should be made to educate both the partners equally about contraceptive methods that have higher efficiency. Further, there is also a need to improve the quality of services, both in terms of counselling and service provision. Lastly, health-related policies should tackle disparities in the empowerment, and economic status of women that would result in decreased post-sterilization regret, and will improve sexual relationships following sterilization.

The incidence and mortality rate of prostate cancer (PCa) is highest in males of African ancestry. PCa is a multi-factorial, complex disease, but the exact mechanisms for its development and progression are unclear. Analysis of data from the one thousand genomes project revealed that a 26-kb region spanning PVT1 exons 4A and 4B shows a run of 75 SNPs with distinct allelic frequencies between African and non-African populations. The gene desert located on chromosome 8q24 is associated with aggressiveness of PCa in males of African ancestry. Interestingly, the non-protein coding gene locus Plasmacytoma Variant Translocation (PVT1) present at 8q24 is overexpressed in PCa. PVT1 gives rise to multiple transcripts with potentially different functions. To investigate if our observed population-level differences at the PVT1 gene locus have implications for PCa, we determined the expression of PVT1 exons 4A and 4B in histologically confirmed normal prostate (n=22), benign tumor prostate (n=35), and malignant tumor prostate tissue (n=28) samples obtained from males who had undergone prostatectomy or transrectal ultrasound-guided biopsy in Nigeria, a sub-Saharan Black African population. We have observed that PVT1 exons 4A and 4B are significantly overexpressed in PCa tissues in comparison to others. Transient and stable overexpression of PVT1 exons 4A and 4B significantly induce greater prostate epithelial cell migration and proliferation. We anticipate that further exploration of the role of PVT1 exons 4A and 4B may lead to the possibility of exploiting them for diagnosis, therapy, and other clinical applications in PCa. Citation Format: Gargi Pal, Lia Di, Akintunde Orunmuyi, E. Oluwabunmi Olapade-Olaopa, Weigang Qiu, Olorunseun O. Ogunwobi. Population level genetic differentiation at the PVT1 gene locus: Implications for prostate cancer [abstract]. In: Proceedings of the Annual Meeting of the American Association for Cancer Research 2020; 2020 Apr 27-28 and Jun 22-24. Philadelphia (PA): AACR; Cancer Res 2020;80(16 Suppl):Abstract nr 1411.

Prostate cancer (PCa) is the most common non-skin cancer and the second leading cause of cancer-related death for men in the United States. PCa is the greatest source of cancer-related mortality in males of African ancestry. One of the most important susceptibility loci for cancer is the 8q24 human chromosomal region. The non-protein coding gene locus plasmacytoma variant translocation 1 (PVT1) is located at 8q24 and is dysregulated in different cancers. PVT1 gives rise to several alternatively spliced transcripts and microRNAs. There are at least twelve exons of PVT1, which make separate transcripts, and likely have different functions. The transcript from PVT1 exon 9 is significantly overexpressed in PCa tissues in comparison to normal prostate tissues obtained from Black males. Both transient and stable overexpression of PVT1 exon 9 induce significantly increased prostate epithelial cell proliferation, migration, and proliferating cell nuclear antigen (PCNA) expression. Notably, implantation into mice of a novel subline of a non-tumorigenic prostate epithelial cell line stably overexpressing PVT1 exon 9 results in the formation of malignant tumors with features characteristic of aggressive PCa. Further, PVT1 exon 9 overexpression significantly induces castration-resistance in prostate epithelial cells. Consequently, PVT1 exon 9 expression is important for PCa initiation and progression and may have potential diagnostic and therapeutic applications in PCa in Black males. Citation Format: Gargi Pal, Jeannette Huaman, Fayola Levine, Akintunde Orunmuyi, E. Oluwabunmi Olapade-Olaopa, Olorunseun O. Ogunwobi. The long noncoding RNA from PVT1 exon 9 is overexpressed in prostate cancer in Black males and induces malignant transformation, invasiveness, and castration-resistance in prostate epithelial cells [abstract]. In: Proceedings of the Twelfth AACR Conference on the Science of Cancer Health Disparities in Racial/Ethnic Minorities and the Medically Underserved; 2019 Sep 20-23; San Francisco, CA. Philadelphia (PA): AACR; Cancer Epidemiol Biomarkers Prev 2020;29(6 Suppl_2):Abstract nr B074.

Prostate cancer (PCa) is the second most common cause of cancer-specific deaths in the United States, accounting for approximately 13% of cancer-related deaths. PCa is also the leading cancer in terms of incidence and mortality in men from Africa and the Caribbean. PCa is a multifactorial, complex disease, with the exact mechanisms for its development and progression unclear. Understanding the molecular mechanisms underlying the development and progression of PCa is necessary. This will aid in the discovery of novel and efficacious biomarkers with applications in early PCa detection and molecular therapeutic targeting. The non-protein coding gene locus Plasmacytoma Variant Translocation (PVT1) is located at 8q24 and is overexpressed in PCa. PVT1 has at least 12 exons that make separate transcripts having different functions. We have recently shown that PVT1 exons 4A and 4B are significantly overexpressed in prostate cancer tissues of Black males and are potential clinical biomarkers for prostate cancer in Black males. In this study, the role of PVT1 exons 4A and 4B in the migration and proliferation of prostate epithelial cells was examined. PVT1 exons 4A and 4B gene fragments were cloned into plasmid expression vectors and transfected into the RWPE1 prostate epithelial cell line to examine their effect on prostate epithelial cell proliferation and migration. We observed that overexpression of either PVT1 exon 4A, or PVT1 exon 4B significantly increased prostate epithelial cell migration and proliferation. This indicates that PVT1 exons 4A and 4B are functional biomarkers for prostate cancer. Better understanding of the roles of PVT1 exons 4A and 4B in PCa may lead to the future possibility of exploiting them for diagnosis, therapy, and other clinical applications in PCa. Citation Format: Gargi Pal, Olorunseun Ogunwobi. PVT1 exons 4A and 4B overexpressed in prostate cancer in black males regulate prostate epithelial cell proliferation and migration [abstract]. In: Proceedings of the Eleventh AACR Conference on the Science of Cancer Health Disparities in Racial/Ethnic Minorities and the Medically Underserved; 2018 Nov 2-5; New Orleans, LA. Philadelphia (PA): AACR; Cancer Epidemiol Biomarkers Prev 2020;29(6 Suppl):Abstract nr B044.

Most bacteriocins of lactic acid bacteria (LAB) are initially synthesized as pre-peptides with an N-terminal extension (leader peptides). Generally, the precursor peptides containing a double-glycine-type leader are processed by a dedicated ATP-binding cassette (ABC) transporter. The ABC transporter and an accessory protein lead to the cleavage of inactive pre-peptide with the concomitant export of the mature peptide across the cytoplasmic membrane. Plantaricins E, F, J, and K belong to class IIb 2-peptide bacteriocins and are synthesized as pre-peptides containing N-terminal G-G leader peptide. In this study, the heterologous expression, purification, and characterization of PlnE pre-peptide, ABC transporter (PlnG), and accessory protein (PlnH) from Lactobacillus plantarum LR/14 in Escherichia coli BL21 (DE3) strain were reported. An in vitro assay was conducted with the inactive PlnE pre-peptide, which after cleavage by the addition of ABC transporter protein exhibited antimicrobial activity against some LAB species. The activity of cleaved pre-peptide was comparable to the activity of mature peptide. Accessory protein was also heterologously expressed and purified; however, no effect on processing activity was detected by the addition of the accessory protein, which suggests that accessory protein is not involved in cleavage, but it might help in the transport of mature plantaricins across the membrane.

Plantaricins are small bioactive peptides produced by Lactobacillus plantarum strains that exhibit significant antimicrobial activity against closely-related Gram-positive bacteria, including food spoilage organisms. In comparison, bacteriocins including plantaricins, are usually less effective against Gram-negative organisms. In this study, we demonstrate that heterologously expressed and purified plantaricins, Pln E, -F, -J, and -K when tested against Gram negative model organism Escherichia coli K-12 were highly effective under certain conditions. The apparent tolerance of Gram-negative members to these peptides has been explained on the basis of the presence of the outer membrane (OM) that acts as a protective barrier. We have shown that agents and/or conditions that destabilize OM of E. coli K-12, make it susceptible to plantaricin peptides. In order to further strengthen this conclusion, an OM lipoprotein-defective lpp mutant strain of E. coli K-12 was also studied and compared. A significant loss of cell viability both in terms of CFU/ml as well as with live-dead dual staining combined with flow cytometry, could be demonstrated with the lpp mutant in comparison to the wild type strain. The results indicate that plantaricins can inhibit Gram-negative bacteria if the outer-membrane is weakened and it can be used in preservation of food with the help of some food-grade chelating agents.

Nano-CuFe2O4 spinel has been found to exhibit strong catalytic activity in the cascade reaction involving 1,4-addition and intramolecular electrophilic cyclization in a perfectly regiocontrolled manner and a series of functionalized 4-oxo-2-(phenylimino)thiazolidin-5-ylideneacetate derivatives were generated successfully. The reaction is mild and selective with good to high yields and displays significant functional group tolerance. The dual role of the thiocarbonyl moiety as an electrophile and as a nucleophile has been observed in this three component coupling reaction. CuFe2O4 magnetic nanoparticles were prepared by a simple and effective citric acid complex method and characterized by using XRD, FT-IR, and TEM analysis. The catalyst was recycled for six cycles without any loss of catalytic activity. All reactions were easily performed and proceeded with high efficiency under very simple and mild conditions and gave excellent yields avoiding time-consuming, costly syntheses, tedious workup and purification hazards.

Cucurbitacins which are structurally unlike triterpenes found in the members of Cucurbitaceae and several other plant families possess immense pharmacological activity. This diverse group of compounds may substantiate to be important lead molecules for the treatment of cancer. Research focused on these unattended medicinal compounds can prove the significance and explore the hidden potential to cure various diseases. These compounds show their proposed mode of action, probable molecular targets and have future aspects of their use as a medicinal agent. This review is aimed to provide the chemical nature and medicinal property of cucurbitacins.

A convenient protocol for the efficient synthesis of aryloxycoumarins and (aryloxyimino)ethylcoumarins is described. The synthetic route developed involves the Cu-promoted C-O and N-O coupling reactions from readily available hydroxycoumarin and (hydroxyimino)ethylcoumarin derivatives in the presence of the catalytic system Cu(OAc)2/Et3N. By applying this condition, a series of arylboronic acids have been successfully reacted to afford the coupled products in fair to good yields.

A series of novel coumarinyl 1,4-benzodioxanes were successfully synthesized from electronically diverse 2-[(o-iodophenoxy)methyl]oxiranes and different positional isomers of hydroxycoumarin via one-pot tandem nucleophilic displacement and copper-mediated intramolecular C–O coupling reaction using CuI and 1,10-phenanthroline as the efficient catalytic system. All the compounds were characterized by 1 H, 13 C NMR, IR, HRMS spectra and a selected set of newly synthesized compounds offered noticeable in vitro free hydroxyl radical scavenging activity in a systematic dose dependent manner which signifies their excellent biological potential.

Cupric chloride showed efficient catalytic activity for the cross coupling reaction of arylboronic acids and (hydroxyi mino)ethylcoumarins at room temperature in the presence of NEt3 as base. A simple and convenient protocol for the synthesis of O-aryloxime ethers having the highly base sensitive coumarin nucleus is reported. O-Aryloxime ethers are important as they provide access to scaffolds for the generation of various biologically active compounds. They are potential precursors to benzofurans and benzisoxazoles.

A library of pyranoquinolines, pyranopyrans and 4H-pyrans are synthesized from the title methods.

Enhanced production of heterologously expressed plantaricin (plnE) from Escherichia coli BL21 (DE3) was achieved from a small- to large-scale batch culture. Starting from a 15-ml shake-flask culture grown in Luria–Bertani (LB) broth, the protein expression could be scaled up using 50 ml, 100 ml, 1 l, and 2 l batch culture. Using similar condition, plantaricin E (PlnE) was successfully expressed in a 30-l stirred fermenter. The protein was expressed as TRX-(His)6-fusion protein and separated by Ni2+ affinity chromatography. Growth in two complex media, LB and Terrific broth (TB), was optimized and compared for the production of PlnE, which was higher in LB in comparison with that of TB. In the fermenter, 140 and 180 mg of PlnE could be produced from 12 l of culture volume at 30 and 25 °C, respectively. The yield of heterologously purified PlnE was found to be 1.2–1.5 %, which was much higher in comparison with the plantaricins produced from the native strain of Lactobacillus plantarum (0.3–0.7 %). Overproduction of PlnE with the help of heterologous expression can overcome the constraint of the low yield from producer strain and provides an easy and low-cost strategy for large-scale production.

Nano-CuFe2O4 spinel has been found to exhibit strong catalytic activity in the cascade reaction involving 1,4-addition and intramolecular electrophilic cyclization in a perfectly regiocontrolled manner and a series of functionalized 4-oxo-2-(phenylimino)thiazolidin-5-ylideneacetate derivatives were generated successfully. The reaction is mild and selective with good to high yields and displays significant functional group tolerance. The dual role of the thiocarbonyl moiety as an electrophile and as a nucleophile has been observed in this three component coupling reaction. CuFe2O4 magnetic nanoparticles were prepared by a simple and effective citric acid complex method and characterized by using XRD, FT-IR, and TEM analysis. The catalyst was recycled for six cycles without any loss of catalytic activity. All reactions were easily performed and proceeded with high efficiency under very simple and mild conditions and gave excellent yields avoiding time-consuming, costly syntheses, tedious workup and purification hazards.

A highly efficient and general protocol has been developed for the facile synthesis of highly diversified 1,3,5-trisubstituted pyrazoles and 3,5-disubstituted 2-isoxazolines through one-pot tandem intermolecular, as well as intramolecular, dipolar [3 + 2] cycloaddition reactions. Chemoselective oxidation of aldohydrazone to nitrile imine and aldoximes to nitrile oxides by iodosobenzene in neutral aqueous media was performed. The scope of the reactions in regiocontrolled dipolar cycloaddition with olefins in the presence of PhIO toward highly substituted pyrazole and isoxazoline derivatives has been demonstrated. SDS converted the initially floating reaction mass and the organo-oxidant PhIO into a homogeneous mixture, which on stirring became a turbid emulsion. The micellar arrangement was confirmed by dynamic light scattering and optical microscopy. The new, green and metal free synthetic method enabled the execution of regiocontrolled tandem cycloaddition oxidation sequences leading to a library of pyrazole and isoxazoline derivatives.

Indirect interactions among community members impact on organisms. The effects of two snails, banded pond snail,Bellamya bengalensis(Lamarck), and Red-rimmed melania,Melanoides tuberculata(Müller), and tadpoles of Asian common toad,Duttaphrynus melanostictus(Schneider), on nonbiting midge larvae,Chironomus striatipennisKieffer, were observed in experimental microcosm. Decrease in tube number and tube length of midge larvae was observed compared to control condition due to introduction of selected above mentioned organisms. The direct effects of non-predator organisms on the midge larvae are due to physical disturbance that destroys their tubes. This may result in vulnerability of midge larvae to predators in the wild. So the community structure may be altered by indirect effects, where one or more species, through their direct disturbance, indirectly change the abundance of other species.

A novel, one-pot, three-component condensation reaction of 3-(bromoacetyl)coumarin, acetylacetone, and an amine using the inexpensive, environmentally benign, and mild catalyst alum as an efficient catalyst and the water–PEG 400 binary solvent system gives 3-(1-aryl-4-acetyl-5-methyl-1H-pyrrol-2-yl)-2H-chromen-2-ones, a new heterocyclic scaffold containing both the coumarin and pyrrole nuclei in a single molecule, in good to excellent yields. This methodology offers several advantages: simple procedure, excellent yields, short reaction times, and green aspects such as avoiding toxic catalysts and solvents.

The synthetic approach for the synthesis of the title compounds involves the Cu-promoted C-O and N-O coupling reactions of readily available hydroxycoumarin and (hydroxyimino)ethylcoumarin derivatives with various arylboronic acids in the presence of the system Cu(O-Ac)2/Et3N.

In this paper an Exact Simultaneous Iterative Reconstruction Algorithm is developed and applied on a large semi human size normal biological model and a diseased model (liver region affected) to verify the efficiency of the algorithm. The algorithm is successfully reconstructed the normal model having 15%-20% perturbation i.e. change in permittivity during disease. In diseased case, reconstructed imaginary part of complex permittivity clearly detects the affected zone and it may help the medical diagnosis. Hence it may be a powerful tool for early detection of cancerous tumors as the interrogating wave is a noninvasive one at the ultra high frequency range. The resolution of this system is increased with the reduction of wavelength by immersing the antenna system and the model in saline water region. The advantage of this algorithm is that the calculation of cofactor are done offline to save the computational time and cofactors are expressed as a function of distances irrespective of their positions .

Preliminary investigations reveal that some products exhibit a significant in vitro free hydroxyl radical scavenging activity.

A combinatorial library of benzylpyrazolyl coumarin derivatives have been synthesized by a green one-pot four-component reaction between aryl hydrazine/hydrazine hydrate (1), ethyl acetoacetate (2), aromatic aldehydes (3) and 4-hydroxycoumarin (4). Molecular scaffolds which assimilate bio-active 3-benzylsubstituted 4-hydroxycoumarins as well as a pyrazolone ring in a single nucleus may be worthwhile molecules from a biological point of view. The reactions were performed in water and employed glacial acetic acid as the right choice of catalyst, and was demonstrated to be the key for rendering the reaction possible and obtained good to excellent yields under reflux conditions within a short period of time. The crystal structures of (R/S)-benzylpyrazolyl coumarin, easily produced by a chromatography-free highly product-selective reaction, were explored by means of single crystal X-ray diffraction analysis and the main intra- and intermolecular interactions perceivable through crystal structure analysis. The presence of a strong intramolecular hydrogen bond was confirmed. In addition, the whole crystal structure consists of other intermolecular hydrogen bonds, such as CH⋯O and aromatic CH⋯π interactions between R- and S-molecules and CH⋯O, NH⋯O and aromatic CH⋯π interactions among only R-molecules and S-molecules in the asymmetric unit.

The use of traditional microbiological culturing methods for the study of microbes had limited success since it has been estimated that 99% of microbes cannot be cultivated easily. Over the past decade, “metagenomics,” which is the culture-independent genomic analysis of microbes, has been developed to overcome these difficulties. Metagenomic analysis involves the basic steps like (1) the selection of an environmental niche, (2) the isolation of genetic material directly from an environmental sample, (3) manipulation of the genetic material, (4) library construction, and (5) the analysis of genetic material in the metagenomic library. The screening of clones can be done for phylogenetic markers or for other conserved genes by hybridization or multiplex PCR or for expression of specific traits, such as enzyme activity or antibiotic production, or they can be sequenced randomly. This chapter gives an overview of metagenomics including its success as well as future biotechnological applications in pharmaceuticals, bioactive molecules, biocatalysts, biomaterials, and others. There can be little doubt that the field of metagenomics gene discovery offers enormous scope and potential for both fundamental microbiology and biotechnological development.

Cupric chloride showed efficient catalytic activity for the cross coupling reaction of arylboronic acids and (hydroxyi mino)ethylcoumarins at room temperature in the presence of NEt3 as base. A sim...

The Landau level spectrum of graphene superlattices is studied using a tight-binding approach. We consider non-interacting particles moving on a hexagonal lattice with an additional one-dimensional superlattice made up of periodic square potential barriers, which are oriented along the zig-zag or along the arm-chair directions of graphene. In the presence of a perpendicular magnetic field, such systems can be described by a set of one-dimensional tight-binding equations, the Harper equations. The qualitative behavior of the energy spectrum with respect to the strength of the superlattice potential depends on the relation between the superlattice period and the magnetic length. When the potential barriers are oriented along the arm-chair direction of graphene, we find for strong magnetic fields that the zeroth Landau level of graphene splits into two well separated sublevels, if the width of the barriers is smaller than the magnetic length. In this situation, which persists even in the presence of disorder, a plateau with zero Hall conductivity can be observed around the Dirac point. This Landau level splitting is a true lattice effect that cannot be obtained from the generally used continuum Dirac-fermion model., Comment: 12 pages, 9 figures

The electronic states of an electrostatically confined cylindrical graphene quantum dot and the electric transport through this device are studied theoretically within the continuum Dirac-equation approximation and compared with numerical results obtained from a tight-binding lattice description. A spectral gap, which may originate from strain effects, additional adsorbed atoms or substrate-induced sublattice-symmetry breaking, allows for bound and scattering states. As long as the diameter of the dot is much larger than the lattice constant, the results of the continuum and the lattice model are in very good agreement. We also investigate the influence of a sloping dot-potential step, of on-site disorder along the sample edges, of uncorrelated short-range disorder potentials in the bulk, and of random magnetic-fluxes that mimic ripple-disorder. The quantum dot's spectral and transport properties depend crucially on the specific type of disorder. In general, the peaks in the density of bound states are broadened but remain sharp only in the case of edge disorder., 9 pages, 9 figures, published version

The electronic properties of graphene zig-zag nanoribbons with electrostatic potentials along the edges are investigated. Using the Dirac-fermion approach, we calculate the energy spectrum of an infinitely long nanoribbon of finite width $w$, terminated by Dirichlet boundary conditions in the transverse direction. We show that a structured external potential that acts within the edge regions of the ribbon, can induce a spectral gap and thus switches the nanoribbon from metallic to insulating behavior. The basic mechanism of this effect is the selective influence of the external potentials on the spinorial wavefunctions that are topological in nature and localized along the boundary of the graphene nanoribbon. Within this single particle description, the maximal obtainable energy gap is $E_{\rm max}\propto \pi\hbar v_{\rm F}/w$, i.e., $\approx 0.12$\,eV for $w=$15\,nm. The stability of the spectral gap against edge disorder and the effect of disorder on the two-terminal conductance is studied numerically within a tight-binding lattice model. We find that the energy gap persists as long as the applied external effective potential is larger than $\simeq 0.55\times W$, where $W$ is a measure of the disorder strength. We argue that there is a transport gap due to localization effects even in the absence of a spectral gap., Comment: 7 pages, 8 figures; minor revisions, 2 references added, published version

A novel, one-pot, three-component condensation reaction of 3-(bromoacetyl)coumarin, acetylacetone, and an amine using the inexpensive, environmentally benign, and mild catalyst alum as an efficient catalyst and the water–PEG 400 binary solvent system gives 3-(1-aryl-4-acetyl-5-methyl-1H-pyrrol-2-yl)-2H-chromen-2-ones, a new heterocyclic scaffold containing both the coumarin and pyrrole nuclei in a single molecule, in good to excellent yields. This methodology offers several advantages: simple procedure, excellent yields, short reaction times, and green aspects such as avoiding toxic catalysts and solvents.

A highly efficient and general protocol has been developed for the facile synthesis of highly diversified 1,3,5-trisubstituted pyrazoles and 3,5-disubstituted 2-isoxazolines through one-pot tandem intermolecular, as well as intramolecular, dipolar [3 + 2] cycloaddition reactions. Chemoselective oxidation of aldohydrazone to nitrile imine and aldoximes to nitrile oxides by iodosobenzene in neutral aqueous media was performed. The scope of the reactions in regiocontrolled dipolar cycloaddition with olefins in the presence of PhIO toward highly substituted pyrazole and isoxazoline derivatives has been demonstrated. SDS converted the initially floating reaction mass and the organo-oxidant PhIO into a homogeneous mixture, which on stirring became a turbid emulsion. The micellar arrangement was confirmed by dynamic light scattering and optical microscopy. The new, green and metal free synthetic method enabled the execution of regiocontrolled tandem cycloaddition oxidation sequences leading to a library of pyrazole and isoxazoline derivatives.

A highly convergent, efficient and practical heteroannulation protocol for the synthesis of a library of coumarin and uracil fused pyrrole derivatives has been developed. Reactions involving the CuFe2O4 catalyzed one-pot three-component domino coupling of 6-aminouracil/4-aminocoumarin, aldehydes and nitromethane resulted in highly substituted coumarin and uracil fused pyrrole derivatives, making this strategy very useful in diversity-oriented synthesis (DOS). CuFe2O4 magnetic nanoparticles were prepared by a simple and effective citric acid complex method and characterized by using XRD, FT-IR, and TEM images. The easy recovery of the catalyst and high yield of the products makes the protocol attractive, sustainable and economic. The catalyst was recycled for six cycles with almost unaltered catalytic activity.

A combinatorial library of benzylpyrazolyl coumarin derivatives have been synthesized by a green one-pot four-component reaction between aryl hydrazine/hydrazine hydrate (1), ethyl acetoacetate (2), aromatic aldehydes (3) and 4-hydroxycoumarin (4). Molecular scaffolds which assimilate bio-active 3-benzylsubstituted 4-hydroxycoumarins as well as a pyrazolone ring in a single nucleus may be worthwhile molecules from a biological point of view. The reactions were performed in water and employed glacial acetic acid as the right choice of catalyst, and was demonstrated to be the key for rendering the reaction possible and obtained good to excellent yields under reflux conditions within a short period of time. The crystal structures of (R/S)-benzylpyrazolyl coumarin, easily produced by a chromatography-free highly product-selective reaction, were explored by means of single crystal X-ray diffraction analysis and the main intra- and intermolecular interactions perceivable through crystal structure analysis. The presence of a strong intramolecular hydrogen bond was confirmed. In addition, the whole crystal structure consists of other intermolecular hydrogen bonds, such as CH⋯O and aromatic CH⋯π interactions between R- and S-molecules and CH⋯O, NH⋯O and aromatic CH⋯π interactions among only R-molecules and S-molecules in the asymmetric unit.