7 research outputs found
A huge foreign body lodgement in the soft palate (uvula) – A rarest case report with literature review
Foreign body retention in young children is commonly encountered phenomenon during dental practice. Because chewing and keeping of different objects is ususal finding seen in most of children. Foreign body lodgement in both primary and permanent dentition of teeth as well as in the soft tissues of the oral cavity have been reported. But retention of a huge foreign object in the uvula of the soft palate is not reported so far. Therefore the aim of this article is to report such a rarest case of huge foreign object and its successful removal
Synthesis of 1,2-benzisoxazole tethered 1,2,3-triazoles that exhibit anticancer activity in acute myeloid leukemia cell lines by inhibiting histone deacetylases, and inducing p21 and tubulin acetylation
1,2,3-Triazole-based heterocycles have previously been shown to possess significant anticancer activity in various tumor models. In the present study, we attached a 1,2,3-triazole moiety to the third position of a 1,2-benzisoxazole heterocycle via copper(I)-catalyzed azide-alkyne cycloaddition (CuAAC) with various alkynes and established for the title compounds significant antiproliferative effect against human acute myeloid leukemia (AML) cells. Among the tested compounds, 3-(4-(4-phenoxyphenyl)-1H-1,2,3-triazol-1-yl)benzodisoxazole (PTB) was found to be the most potent antiproliferative agent with an IC50 of 2 μM against MV4-11 cells using MTT assay. Notably, PTB induced cytotoxicity in MOLM13, MOLM14 and MV4-11 cells with selectivity over normal bone marrow cells (C57BL/6). Furthermore, PTB was found to induce cytotoxicity by increasing apoptosis of AML cells (MOLM13, MOLM14 and MV4-11) as well as sub-G1 cell population and apoptotic cells at submicromolar concentrations, as shown by flow cytometry and Annexin-V staining, respectively. On the protein level we suggested histone deacetylases (HDACs) as the potential protein target of those compounds in silico, and the predicted target was next experimentally validated by measuring the variations in the levels of p21, cyclin D and acetylation of histone H3 and tubulin. Molecular docking analysis of the title compounds with the second deacetylase domain of HDAC6 displayed high degree of shape complementarity to the binding site of the enzyme, forming multiple molecular interactions in the hydrophobic region as well as a hydrogen bond to the phenol side-chain of Tyr-782. Thus, 1,2,3-triazole derivatives appear to represent a class of novel, biologically active ligands against histone deacetylases which deserve to be further evaluated in their applications in the cancer field. © 2015 Elsevier Ltd. All rights reserved
Traditional utilization and phytochemical analysis of medicinal herb Exacum Linn. from central Western Ghats
In the present study, we focused on the traditional utilization and phytochemical screening of Exacum Linn., a traditional medicinal herb in the Western Ghats of Karnataka, India. There are five species of Exacum viz., E. bicolor, E. pedunculatum, E. lawii, E. carniatum and E. pluminum reported from Western Ghats of Karnataka. Exacum species were used to treat fever, dysentery, sore throat in addition to treat cough, body pain and eye diseases. Analysis of methanol and aqueous extracts showed the presence of phytochemicals such as flavonoids, saponins and alkaloids