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Cirrhosis continues to claim the lives of people worldwide every year. Esophageal variceal bleeding due to portal hypertension is one of the dreadful complications. We compared carvedilol with propranolol to find better drug that can prevent index variceal bleed in cirrhotic patients. 220 patients with known esophageal varices on upper GI endoscopy and no previous history of GI bleed were randomized to group A (Carvedilol) and group B (Propranolol). Bleeding occurred in 37.14% and 59.04% of the patients in group A (carvedilol) and B (propranolol) respectively (p=0.02). Bleeding was more common among patients with large as compared to small varices (67.04% versus 35.48% respectively). Among patients with large varices bleeding occurred in 58.13% and 75.55% of patients in group A and B respectively while in small varices, bleeding rate was 25% and 46.66% respectively (p=0.03). Regarding the response of beta blockers, mean pulse rate dropped from 85.15±5.49 to 59.8±2.39 per minute in Group A while in Group B it was reduced to 60.5±4.21 from 83.8±5.33 per minute at 3 years follow up. No significant difference found in the side effect profile. Our study showed that carvedilol was more effective than propranolol in primary prevention of variceal hemorrhage. [ABSTRACT FROM AUTHOR]

Summary: Alkyl-substituted azolium salts (1-8) and their Se-N-heterocyclic carbene (Se-N-Het-C) adducts (9-12) were obtained in very reasonable yields. All synthesized azolium salts and their Se-N-Het-C adducts were characterized by different spectroscopic techniques such as FT-IR, 1HNMR, 13CNMR, and elemental analysis. It was found that all synthesized Se-N-Het-C adducts were stable at room temperature in both air and moisture. In-vitro these compounds (5-12) were assessed for their antimicrobial potential against Bacillus subtilis (B. subtilis), Macrococcus brunensis (M. brunensis), and Bacillus cereus (B. cereus) in vitro. Results of MIC and inhibition zone values revealed that the majority of the Selenium N-Heterocyclic carbene adducts were active against Bacillus subtilis (B. subtilis) than Macrococcus brunensis (M. brunensis) and Bacillus cereus (B. cereus) whereas opposite in the azolium salts (5-8). Compounds 5-8 have an inhibition zone of 16±0.1-26±0.3mm against all tested bacterial strains while selenium-NHC adducts 9-12 have a zone of inhibition (16±0.2 to 25 ± 0.4mm). Adduct 12 showed good activity against all tested strains with ZI values 25 ± 0.1, 22± 0.5, 17 ± 0.3 mm and MIC values 17 ± 0.2, 16 ± 0.4 and 18 ± 0.3 µg/mL against Bacillus subtilis (B. subtilis), Macrococcus brunensis (M. brunensis) and Bacillus cereus (B. cereus) respectively. Adduct 10 showed the highest thrombolysis i-e 86.9% and adduct 12 showed good hemolysis i-e 0.51%. Overall results of thrombolysis and cytotoxicity studies revealed that the compounds are safe for preclinical studies of mouse blood in vitro. [ABSTRACT FROM AUTHOR]

Tephrosia apollinea is a perennial shrublet widely distributed in Africa and is known to have medicinal properties. The current study describes the bio-assay (cytotoxicity) guided isolation of (-)-pseudosemiglabrin from the aerial parts of T. apollinea. The structural and stereochemical features have been described using spectral and x-ray crystallographic techniques. The cytotoxicity of isolated compound was evaluated against nine cancer cell lines. In addition, human fibroblast was used as a model cell line for normal cells. The results showed that (-)-pseudosemiglabrin exhibited dose-dependent antiproliferative effect on most of the tested cancer cell lines. Selectively, the compound showed significant inhibitory effect on the proliferation of leukemia, prostate and breast cancer cell lines. Further studies revealed that, the compound exhibited proapoptotic phenomenon of cytotoxicity. Interestingly, the compound did not display toxicity against the normal human fibroblast. It can be concluded that (-)-pseudosemiglabrin is worthy for further investigation as a potential chemotherapeutic agent. [ABSTRACT FROM AUTHOR]

Background: Since the first successful synthesis of Ag(I)-N-heterocyclic carbene complex in 1993, this class of compounds has been extensively used for transmetallation reactions where the direct synthesis using other metal ions was either difficult or impossible. Initially, silver(I)-NHC complexes were tested for their catalytic potential but could not get fame because of lower potential compare to other competent compounds in this field; however, these compounds proved to have vital antimicrobial activities. These encouraging biomedical applications further convinced researchers to test these compounds against cancer. The current work has been carried out with this aim. Results: N-ipropylbenzimidazole was synthesized by reaction of benzimidazole with ipropyl bromide. The subsequent treatment of the resulting N-alkylbenzimidazole with ortho/meta/para-(bromomethylene) benzene afforded corresponding bis-benzimidazolium bromides (5-7). The counter anion (Br-) of each salt was replaced by hexaflourophosphate (PF6-)for the ease of handling and further purification (8-10). Each salt (Ligand), in halide form, was further allowed to react with Ag2O with stirring at room temperature for a period of two days to synthesize dinuclear Ag(I)-NHC complexes (11-13). All synthesized compounds were characterized by spectroscopic techniques and microanalysis. Molecular structures of compounds 5, 9 & 10 were established through single crystal x-ray diffraction technique. All the compounds were assessed for their anti-proliferation test on human colorectal cancer cell line (HCT 116). Results showed that the ligands (5-10) showed mild to negligible cytotoxicity on HCT 116 cells whereas respective silver complexes (11-13) exhibited dose dependent cytotoxicity towards the colon cancer cells with IC50 ranges between 9.7 to 44.5 µM. Interestingly, the complex 13 having para-xylyl spacer was found the most active (IC50 9.7 µM) that verifies our previously reported results. Conclusions: All the bis-benzimidazolium salts (8-10) were found inactive whereas after bonding with silver cations, the Ag(I)-NHC complexes (11-13) showed a dose dependent cytotoxic activity. This proved that silver practice an important role in death of cancer cells. Also, the N-alkyl/aryl substitutions and ortho/metal/para xylyl units regulate the cytotoxicity. [ABSTRACT FROM AUTHOR]

This paper describes synthesis, characterization (NMR, FT-IR, microanalysis, and X-ray crystallography), in vitro anticancer activity of ortho/para-xylyl linked bis-imidazolium salts (4-5) and respective dinuclear Ag(I) N-heterocyclic carbene (NHC) complexes (6-7). All the compounds were tested for their cytotoxicity against human colorectal cancer (HCT 116) and breast cancer (MCF-7) cell lines. According to cell viability measurements using MTT assay, all the complexes (6-7) showed a dose-dependent cytotoxic activity against both the cell lines, whereas respective salts (4-5) proved to be inactive. The complexes (6-7) demonstrated significant activity with IC50 values range 5.6-20.3 µM for HCT 116 and 1.12-6.38 µM for MCF-7. 5-Fluorouracil was used as standard drug (IC50 = 5.9 µM) for HCT 116, whereas tamoxifen was used as standard drug for MCF-7 (IC50 = 14 µM) cell line. [ABSTRACT FROM AUTHOR]

Tephrosia apollinea is a perennial shrublet widely distributed in Africa and is known to have medicinal properties. The current study describes the bio-assay (cytotoxicity) guided isolation of (-)-pseudosemiglabrin from the aerial parts of T. apollinea. The structural and stereochemical features have been described using spectral and x-ray crystallographic techniques. The cytotoxicity of isolated compound was evaluated against nine cancer cell lines. In addition, human fibroblast was used as a model cell line for normal cells. The results showed that (-)-pseudosemiglabrin exhibited dose-dependent antiproliferative effect on most of the tested cancer cell lines. Selectively, the compound showed significant inhibitory effect on the proliferation of leukemia, prostate and breast cancer cell lines. Further studies revealed that, the compound exhibited proapoptotic phenomenon of cytotoxicity. Interestingly, the compound did not display toxicity against the normal human fibroblast. It can be concluded that (-)-pseudosemiglabrin is worthy for further investigation as a potential chemotherapeutic agent. [ABSTRACT FROM AUTHOR]

Crystal violet (CV) dye, because of its non-biodegradability and harmful effects, poses a significant challenge for wastewater treatment. This study addresses the efficiency of easily accessible coal fly ash (CFA)-based adsorbents such as raw coal fly ash (RCFA) and surface enhanced coal fly ash (SECFA), in removing CV dye from waste effluents. Various analytical techniques such as FTIR, XRD, SEM, TEM, BET, zeta sizer and zeta potential were employed for the characterization of the adsorbents and dye-loaded samples. BET revealed that RCFA possesses a surface area of 19.370 m 2 g -1 and SECFA of 27.391 m 2 g -1 , exhibiting pore volumes of 0.1365 cm 3 g -1 and 0.1919 cm 3 g -1 respectively. Zeta-sizer and potential analysis showed the static charges of RCFA as -27.3 mV and SECFA as -28.2 mV, with average particle sizes of 346.6 and 315.3 nm, respectively. Langmuir and Freundlich adsorption isotherms were also employed for adsorption studies. Employing central composite design (CCD) of response surface methodology (RSM), the maximum CV removal was 81.52% for RCFA and 97.52% for SECFA, providing one minute contact time, 0.0125 g adsorbent dose and 10 ppm dye concentration. From the thermodynamic studies, all the negative values of Δ G ° showed that all the adsorption processes of both adsorbents were spontaneous in nature., Competing Interests: The authors declare that they have no competing interests as denied by Journal, or other interests that might be perceived to influence the results and/or discussion reported in this paper., (This journal is © The Royal Society of Chemistry.)

Bacterial resistance towards antibiotics is a significant challenge for public health, and surface-enhanced Raman spectroscopy (SERS) has great potential to be a promising technique to provide detailed information about the effect of antibiotics against biofilms. SERS is employed to check the antibacterial potential of a lab synthesized drug ([bis(1,3-dipentyl-1 H -imidazol-2(3 H )-ylidene)silver(i)] bromide) against Bacillus subtilis and to analyze various SERS spectral features of unexposed and exposed Bacillus strains by observing biochemical changes in DNA, protein, lipid and carbohydrate contents induced by the lab synthesized imidazole derivative. Further, PCA and PLS-DA are employed to differentiate the SERS features. PCA was employed to differentiate the biochemical contents of unexposed and exposed Bacillus strains in the form of clusters of their representative SERS spectra and is also helpful in the pairwise comparison of two spectral data sets. PLS-DA provides authentic information to discriminate different unexposed and exposed Bacillus strains with 91% specificity, 93% sensitivity and 97% accuracy. SERS can be employed to characterize the complex and heterogeneous system of biofilms and to check the changes in spectral features of Bacillus strains by exposure to the lab synthesized imidazole derivative., Competing Interests: The authors have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (This journal is © The Royal Society of Chemistry.)