Synthesis, structural characterization and biological properties of cyclometalated iridium(iii) complexes containing 1,2,5]-thiadiazolo-3,4-f]-1,10]-phenanthroline

Two cationic iridium(iii) complexes, Ir(ppy)(2)((tdzp))](+)(1) and Ir(bhq)(2)((tdzp))](+)(2) {ppy = 2-phenylpyridine, bhq = benzoh]quinoline, tdzp = 1,2,5]-thiadiazolo-3,4-f]-1,10]-phenanthroline}, have been synthesized and structurally characterized. The molecular structures of the iridium complexes have been confirmed by single-crystal X-ray structure determination. Extensive hydrogen bonding between lattice water molecules, solvated methanol, and chloride anions is observed in the crystal structure of complex1, which leads to the formation of 1D polymeric cyclic hybrid water-chloride-methanol clusters. The complexes show different photophysical properties in different solvents. The experimental photo-physical properties of the synthesized iridium(iii) complexes match well with the theoretically calculated results obtained by density functional theory (DFT) and time-dependent density functional theory (TD-DFT) studies. The HOMO of complexes1and2is restricted on the iridium and cyclometalated aromatic ligands, while the LUMO, LUMO+1, and LUMO+2 are primarily restricted on the polypyridyl tdzp ligand. The interaction of the complexes with calf thymus DNA (CT-DNA) was investigated by absorption titration and emission titration experiments. Furthermore, the cytotoxicity and cellular localization properties of these complexes towards HeLa cells have been investigated

Fluorophore tagged mixed ligand copper(II) complexes: synthesis, structural characterization, protein binding, DNA cleavage and anticancer activity

Two fluorophore tagged copper(II) complexes Cu(phen)(L)(ClO4)(2)] (1) and Cu(bpy)(L)(H2O)(ClO4)](ClO4) (2), (where L=2-amino-1H-benzode]isoquinoline-1,3-(2H)dione (L), phen=1,10-phenanthroline and bpy=2,2 `-bipyridine) have been synthesized and structurally characterized. Structures of the copper complexes 1 and 2 were confirmed by single-crystal X-ray structure determination. The coordination geometry around the copper center of complexes 1 and 2 is distorted octahedral. The plasmid DNA cleavage activity of the complexes has been investigated by agarose gel electrophoresis and the study reveals that both the complexes have high plasmid DNA photo-cleavage activity. The binding interaction ability of the metal complexes with bovine serum albumin (BSA) was investigated using fluorescence spectroscopy. The cytotoxicity of the complexes has been evaluated by MTT (3-4,5-dimethylthiazole-2-yl]-2,5-diphenyltetrazolium bromide) assay against A549 (adenocarcinoma human alveolar basal epithelial cells) and MCF-7 (breast cancer cell line) cell lines in comparison with cis-platin. Complexes 1 and 2 have exhibited better cytotoxic activity than cis-platin against A549 and MCF-7 cell lines. The cellular uptake study and localization of the complexes within the cells have been investigated by fluorescence microscopy. The cell staining and flow cytometry experiments suggest that complexes induce an apoptotic mode of cell death

Invitro Cytotoxicity of Various Parts of Adhahapushpi (Trichodesma Indicum Linn.R.Br.) Against 3 Cancer Cell Lines

Cancer is a leading cause of death and an important source to the mortality and morbidity worldwide. The management in contemporary medicine is having toxicity to normal cells so the world is looking forward for drugs which are cytotoxic to cancer cells and non toxic to host cells and Medicinal plants are the doing well in this aspect.  Adhahapushpi (Trichodesma indicum Linn.R.Br.)Belonging to Boraginaceae family is traditionally used as anticancer to treat breast cancer. Its cytotoxicity against breast cancer and cervical cancer is proved in previous researches. Objectives: The present study was conducted to evaluate its cytotoxicity against 3 Human cancer cell lines Viz. colon cancer cell line (HCT116), oral cancer cell line (KB) and skin cancer cell line (A375). Method: Alcohol, Methanol and Aqueous extracts of Root, Leaf, Stem and Fruit of Adhahapushpi were used to screen in-vitro cytotoxicity. Cytotoxic effect was analysed by MTT assay. Results: The ethanol Root extract was found to be more cytotoxic in vitro to colon cancer cell line (HCT116) with IC50values 176.5±13.36 µg/ml, ethanol extract of fruit to  oral cancer cell line (KB-3-1) with IC50values 154 ± 3.89 µg/ml and root ethanol extract to skin cancer cell line (A375) with  IC50values 169± 12.09 µg/ml respectively

Anticancer and antioxidant activity of ethanolic extract of Clove (Syzygium aromaticum) on oral squamous cell carcinoma cell lines (KB cell lines)- An In-vitro study

Cloves (Syzygium aromaticum) as been used as traditional medicine for many years and they possess antibacterial, antifungal and antiviral properties. Clove is known for its anticancer property on various cancer cell lines and is well established, but its anticancer effect on OSCC cell lines is less known.  Aim of the study was to determine the anticancer and antioxidant effect of Syzygium aromaticum extract on OSCC cell lines (KB cell lines) and compare the same with normal mouse fibroblasts cell lines (L292 cell lines). KB cell lines and L292 cell lines were commercially obtained.  Clove was obtained from local market and ethanolic extract (EC) of clove was prepared. Anticancer activity was assessed by MTT, neutral red, DAPI and Double staining assay and antioxidant assay was carried out by FRAP, PM and DPPH assay. The antioxidant property of EC of clove increased with increase in the concentration in a dose dependent manner. Both MTT and Neutral Red assay showed increase in cell death with increase in concentration of EC of clove. Double staining and DAPI showed increase in cell death when treated with EC of clove. The anticancer and antioxidant activity of EC of clove was comparable with standard drug used in the assay. This in vitro study demonstrates effective anticancer and antioxidant activity on KB cell lines when compared to standard control. However, further studies are to be conducted in order to characterize other potential antitumor components of the clove, so that it can be used as therapeutic agent in treating oral carcinoma

Application of fluorescent In situ hybridization for rapid detection of aggregatibacter actinomycetemcomitans in patients with chronic periodontitis

Background: Aggregatibacter actinomycetemcomitans is a proven periodontal pathogen. In dentistry, there is a need to identify and quantitate the organisms from the diseased sites quickly and reliably. Since culture requires several days, molecular methods are being used frequently to detect A. actinomycetemcomitans. Among them, fluorescent in situ hybridization (FISH) is rapid, sensitive and quantitative. An attempt is made here to evaluate the applicability of this technique as a diagnostic tool in periodontology. Materials and Methods: A total of 77 healthy individuals and 77 patients with chronic periodontitis were enrolled for the study. Subgingival plaque was collected, fixed with paraformaldehyde and subjected to FISH. Oligonucleotide probe labelled with 6-carboxyfluorescein (FAM) was used for hybridization. After the procedure, the fluorescently stained A. actinomycetemcomitans were identified and counted from the smear and quantitated using a simple grading. Results: The data revealed that plaques from 84.5% of healthy individuals and 98.7% of chronic periodontitis showed the presence of A. actinomycetemcomitans. However, the number of these bacteria were very low in most positive samples from healthy subjects in contrast to patients with chronic periodontitis, who had higher number of organisms. Statistical analysis using Mann–Whitney test revealed a significant difference among the two groups with P ≤ 0.001 and Z = −5.833. Conclusions: The procedure used in the study is simple, rapid and can be easily adaptable. It also has a high sensitivity and has the ability to detect a single bacterial cell. The method can be directly applied to the clinical samples and can be used as a rapid diagnostic tool in periodontics

A DoE-based development and characterization of Nadifloxacin-loaded transethosomal gel for the treatment of Acne vulgaris

Abstract Background The objective of this current research was to enhance the topical delivery of Nadifloxacin (NDFX) by incorporating it into a transethosomal gel formulation. NDFX has limited penetration into the deep layer of the skin because it is poorly water soluble and it has a log p value of 2.47. To optimize the formulation, the “Box–Behnken design” was utilized. The independent variables included phosphatidylcholine 90, tween 80 and ethanol. The produced formulations underwent evaluation for entrapment efficiency, vesicle size and zeta potential. The optimized formulation was then incorporated into suitable gel bases and subjected to further investigation, including in vitro diffusion, ex vivo penetration, in vitro antimicrobial assay and in vivo anti-acne activity. Results The optimized formulation exhibited an entrapment efficiency of 80.12%, a vesicle size of 156.1 nm and a zeta potential of − 33.23 mV. TEM images confirmed the presence of encapsulated vesicles with a spherical shape. The in vitro diffusion study demonstrated that the transethosomal gel containing Carbopol 934 (1%) exhibited higher drug release compared to the HPMC K4M gels. Furthermore, the ex vivo permeation study revealed that the optimized transethosomal gel demonstrated increased permeation compared to the commercially available formulation. Conclusion The optimized transethosomal formulation displayed enhanced in vitro antimicrobial and in vivo anti-acne effects against Propionibacterium acnes in Wistar albino rats when compared to the marketed formulation

Gingipain Genotyping as a Potential Predictor for the Assessment of Periodontal Health and Disease Condition

Oral hygiene maintenance is important to maintain optimal oral health. Oral health is affected by dysbiotic oral microflora in the dental plaque. Virulent factors of pathogenic organisms, such as gingipain, are responsible for tissue degradation and host tissue invasion in periodontal disease. We sought to investigate the distribution of gingipain genotypes (rgpA and kgp) of P. gingivalis in patients with chronic periodontitis and healthy individuals. The study included individuals positive for P. gingivalis, with 95 samples in the chronic periodontitis (CP) group and 35 samples in the healthy (H) group. We found that kgp-I and kgp-II types were prevalent in 67.36% and 32.64% of the samples in the CP group, respectively. In the H group, kgp-II was highly prevalent (97.14%). The rgpA genotype, type A was found in 78.95% and 82.85% of the samples in the CP and H group, respectively. The mean level of PD and CAL were increased in the presence of kgp-I and decreased in the presence of kgp-II. The mean level of P. gingivalis was increased in the presence of kgp-I and rgpA, type A. Our results show that kgp-I and kgp-II are strongly associated with disease and health condition, respectively

Study of microbial diversity in saliva and plaque samples from caries-free and caries-affected children using denaturing gradient gel electrophoresis

Background: Recent investigations have shown the possible involvement of bacteria other than mutans group and Lactobacilli in the etiology of caries. Molecular methods have been used to study the microbial diversity in caries-active (CA) and caries-free (CF) children. Among them, denaturing gradient gel electrophoresis (DGGE) is more popular and has been used in the present study. Aims: The aim of the present study was to investigate the difference in bacterial diversity in saliva and plaque samples from CF and CA children using DGGE. Materials and Methods: The study involved saliva and plaque samples from 56 children of which 28 were CF, 20 with CA, and 8 with white spot lesions (WSP). DNA was extracted and subjected to polymerase chain reaction amplification with universal primers. It was then run in polyacrylamide gel electrophoresis with gradients of urea and formamide and stained with SYBR green. Multiple bands were produced in each sample lane and each band represents one organism. Statistical Analysis: A dendrogram was generated using Phoretix software and similarity index was calculated using a specific formula. Results: Samples in each group formed several clusters indicating a specific pattern of the bacterial profile. Similarity coefficient was calculated based on the number of bands, intensity, and location. The diversity was less in the saliva and plaque samples of CA group as compared to those of CF and WSP groups. Conclusions: DGGE can be used to study distinctive bacterial profiles in healthy and caries-affected sites. DGGE can be further developed as a pattern recognition tool with which to identify specific groups of bacteria. Saliva may be used to study bacterial diversity in dental caries

Synthesis, structural characterization and biological properties of phosphorescent iridium(III) complexes

Two phosphorescent cyclometalated iridium(III)-triptycenyl-1,10-phenanthroline complexes Ir(ppy)2(tpt-phen)+ (1) and Ir(bhq)2(tpt-phen)+ (2) {ppy=2-phenylpyridine, bhq=Benzohquinoline, tpt-phen=triptycenyl-1,10-phenanthroline} have been synthesized and structurally characterized. The structure of complex 2 has been studied by single crystal X-ray crystallography. The photophysical properties of complexes in a different solvent have also been investigated. The binding of complexes to the double stranded calf thymus (CT-DNA) has been investigated by spectroscopic techniques. These complexes condense originally circular plasmid DNA into particulate structures. The DNA-condensation induced by these complexes have been investigated by electrophoretic mobilty shift assay, dynamic light scattering, and fluorescence microscopy. Furthermore, the cytotoxicity of these complexes towards HeLa cells have been studied and their cellular localisation properties have been investigated by fluorescence microscopy