Metal catalyzed C–H functionalization on triazole rings

The present review covers advancement in the area of C–H functionalization on triazole rings, by utilizing various substrates with palladium or copper as catalysts, and resulting in the development of various substituted 1,2,3- and 1,2,4-triazoles. Synthesis of these substituted compounds is necessary from the perspective of pharmaceutical, medicinal, and materials chemistry.

The present review covers advancement in the area of C–H functionalization on triazole rings, by utilizing various substrates with palladium or copper as catalysts, and resulting in the development of various substituted 1,2,3- and 1,2,4-triazoles.     

Can lubrication of the eyelid speculum reduce overall pain perception associated with cataract surgery by phacoemulsification performed under topical anesthesia?

Purpose:This study aimed to evaluate the effect of using the lubricated eyelid speculum on the overall pain perception by the subject patients who underwent cataract surgery by phacoemulsification technique under topical anesthesia.Methods:A prospective interventional randomized comparative study was conducted at the tertiary eye care center, wherein adult patients scheduled for bilateral cataract surgery with phacoemulsification techniques under topical anesthesia were randomized to undergo surgery with two different modes of eyelid speculum insertion, either with or without lubrication of the eyelid speculum. Fifty percent of the patients underwent surgery with eyelid speculum without lubrication, and 50% with lubrication of the eyelid speculum. The primary outcome was to compare the level of overall pain perception among the subject patients of the two groups by using the Visual Analogue Scale (VAS) in the immediate postoperative period.Results:The study included 130 patients who underwent bilateral cataract surgery (n = 260 eyes) under topical anesthesia, wherein n = 130 eyes underwent surgery using lubricated eyelid speculum and n = 130 eyes underwent surgery with dry eyelid speculum. Pain perception score assessed on the VAS (0–10 cm) ranged from 0.5 to 6, with a mean ± standard deviation of 2.06 ± 1.12. A significant correlation was found with two different methods of eyelid speculum insertion with reduced overall pain perception in patients with the use of lubricated eyelid speculum compared to the dry eyelid speculum (P = 0.0001).Conclusion:The overall pain perception associated with cataract surgery performed by phacoemulsification technique under topical anesthesia can be further minimized by lubricating the eyelid speculum prior to insertion for exposing the globe.     

Lymphangiogenesis requires Ang2/Tie/PI3K signaling for VEGFR3 cell-surface expression

Vascular endothelial growth factor C (VEGF-C) induces lymphangiogenesis via VEGF receptor 3 (VEGFR3), which is encoded by the most frequently mutated gene in human primary lymphedema. Angiopoietins (Angs) and their Tie receptors regulate lymphatic vessel development, and mutations of the ANGPT2 gene were recently found in human primary lymphedema. However, the mechanistic basis of Ang2 activity in lymphangiogenesis is not fully understood. Here, we used gene deletion, blocking Abs, transgene induction, and gene transfer to study how Ang2, its Tie2 receptor, and Tie1 regulate lymphatic vessels. We discovered that VEGF-C–induced Ang2 secretion from lymphatic endothelial cells (LECs) was involved in full Akt activation downstream of phosphoinositide 3 kinase (PI3K). Neonatal deletion of genes encoding the Tie receptors or Ang2 in LECs, or administration of an Ang2-blocking Ab decreased VEGFR3 presentation on LECs and inhibited lymphangiogenesis. A similar effect was observed in LECs upon deletion of the PI3K catalytic p110α subunit or with small-molecule inhibition of a constitutively active PI3K located downstream of Ang2. Deletion of Tie receptors or blockade of Ang2 decreased VEGF-C–induced lymphangiogenesis also in adult mice. Our results reveal an important crosstalk between the VEGF-C and Ang signaling pathways and suggest new avenues for therapeutic manipulation of lymphangiogenesis by targeting Ang2/Tie/PI3K signaling.     

Draft genome sequence of plastic degrading Bacillus sp. AIIW2 isolated from the Arabian ocean

The endemic spread of plastic in the environment requires urgent need of a sustainable approach. Marine microbes found to have vast bioactivity and play a central role in biogeochemical cycling in the ocean; however, very few of them had been explored for biochemical cycling or plastic degradation. In the present study, we report the draft genome sequence of marine Bacillus sp. AIIW2 which was found to utilize plastic as a carbon source. The Bacillus sonorensis SRCM101395 was used as a reference genome for mapping the reads. The genome size of strain AIIW2 was approximately 4.4 Mb and composed of 4737 coding sequences with 45.7% G + C contents. The whole genome comparison of strain AIIW2 with three closest Bacillus strains showed strain specificity, the 16S ribosomal RNA sequence shows 99.93% similarity with Bacillus paralicheniformis KJ-16^T (KY694465). This genome data would provide the genetic basis in developing plastic bioremediation approaches and discover the enzymes pertinent in the biodegradation processes.     

Antidiabetic and antioxidant activity of hydroxycinnamic acids from Calamintha Officinalis Moench.

This study was undertaken to investigate the antidiabetic and antioxidant activities of crude extracts and pure compounds from the aerial parts of Calamintha officinalis Moench. (Lamiaceae). The aqueous extract showed the promising antidiabetic and antioxidant activities. Based on these findings, the aqueous extract was fractionated on a silica gel column chromatography in a bioassay-guided fractionation affording two known hydroxycinnamic acids showing potent activity (1) rosamarinic acid and (2) caffeic acid. Both rosamarinic acid and caffeic acid exhibited significant activity, even more than the positive control, glibenclamide. The results indicated that Calamintha officinalis aqueous extract and the isolated compounds are potential natural agents for the control of diabetes.     

TIP60-miR-22 axis as a prognostic marker of breast cancer progression

MicroRNAs (miRNAs) are 22- to 24-nucleotide, small, non-coding RNAs that bind to the 3′UTR of target genes to control gene expression. Consequently, their dysregulation contributes to many diseases, including diabetes and cancer. miR-22 is up-regulated in numerous metastatic cancers and recent studies have suggested a role for miR-22 in promoting stemness and metastasis. TIP60 is a lysine acetyl-transferase reported to be down-regulated in cancer but the molecular mechanism of this reduction is still unclear. In this study, we identify TIP60 as a target of miR-22. We show a negative correlation in the expression of TIP60 and miR-22 in breast cancer patients, and show that low levels of TIP60 and high levels of miR-22 are associated with poor overall survival. Furthermore, pathway analysis using high miR-22/low TIP60 and low miR-22/high TIP60 breast cancer patient datasets suggests association of TIP60/miR-22 with epithelial-mesenchymal transition (EMT), a key alteration in progression of cancer cells. We show that blocking endogenous miR-22 can restore TIP60 levels, which in turn decreases the migration and invasion capacity of metastatic breast cancer cell line. These results provide mechanistic insight into TIP60 regulation and evidence for the utility of the combination of TIP60 and miR-22 as prognostic indicator of breast cancer progression.     

Utility-Fuzzy-Taguchi based hybrid approach in investment casting process

In this paper, the use of the Utility-Fuzzy-Taguchi based hybrid approach in investment casting process for optimizing multiple quality characteristics of wax patterns has been conceptualized. Selection of an appropriate orthogonal array, preference scale construction followed by preference values, generation of multi-performance index (MPI) by fuzzy logic, analysis of means and analysis of variance are employed to study the performance characteristics of the process. The control factors considered are injection temperature, injection pressure and injection time, whereas linear shrinkage, surface roughness and penetration are the corresponding responses. The optimal setting obtained by the proposed method is validated by confirmatory experiments. This concludes the application feasibility of the proposed method for parametric optimizations in investment casting process. Further, the result of the aforementioned optimization technique has been compared with that of Utility-Taguchi technique. It is found that the optimal condition for both is same, while the most influential process parameter is different in both cases due to employment of random selection of weights in Utility-Taguchi method.