The Triglyceride-Glucose Index Might Be a Better Indicator for Predicting Poor Cardiovascular Outcomes in Chronic Coronary Syndrome.

This study aimed to explore the potential association between the triglyceride-glucose index (TyG) and the atherogenic index of plasma (AIP)-both considered surrogate markers for atherosclerosis-and major adverse cardiovascular events (MACEs) in patients diagnosed with chronic coronary syndrome (CCS). We conducted a retrospective analysis, encompassing 715 consecutive patients with intermediate CCS risk, who presented at the outpatient clinic between June 2020 and August 2022. MACEs included non-fatal myocardial infarction, hospitalization for heart failure, cerebrovascular events, non-cardiac mortality, and cardiac mortality. The primary outcome was the composite occurrence of MACEs during the follow-up period. For time-to-event analysis of the primary outcome, we employed Kaplan-Meier plots and Cox proportional hazard models. The median age of the overall study population was 55 years, with a median follow-up duration of 17 months. Multivariate Cox regression analysis identified age, hypertension, Coronary Artery Disease-Reporting and Data System score, and TyG index as independent predictors of the primary outcome. Notably, individuals with high TyG levels exhibited a significantly higher primary outcome rate compared to those with low TyG levels (18.7% vs. 3.8%, p < 0.001). Similarly, patients with elevated TyG values demonstrated statistically higher rates of cerebrovascular events, hospitalizations for heart failure, non-fatal myocardial infarctions, non-cardiac mortality, and cardiac mortality. These findings suggest that TyG may serve as a predictive marker for adverse cardiovascular outcomes in patients with CCS.

The prognostic impact of inflammation in patients with decompensated acute heart failure, as assessed using the pan-immune inflammation value (PIV).

There is increasing evidence that composite scores based on blood counts, which are reflectors of uncontrolled inflammation in the development and progression of heart failure, can be used as prognostic biomarkers in heart failure patients. The prognostic effects of pan-immune inflammation (PIV) as an independent predictor of in-hospital mortality in patients with acute heart failure (AHF) were evaluated based on this evidence. The data of 640 consecutive patients hospitalized for New York Heart Association (NYHA) class 2-3-4 AHF with reduced ejection fraction were analyzed and 565 patients were included after exclusion. The primary outcome was in hospital all-cause death. Secondary outcomes were defined as the following in-hospital events: Acute kidney injury (AKI), malignant arrhythmias, acute renal failure (ARF) and stroke. The PIV was computed using hemogram parameters such as lymphocytes, neutrophils, monocytes and platelets. Patients were categorized as low or high PIV group according to the median value, which was 382.8. A total of 81 (14.3%) in-hospital deaths, 31 (5.4%) AKI, 34 (6%) malignant arrhythmias, 60 (10.6%) ARF and 11 (2%) strokes were reported. Patients with high PIV had a higher in-hospital mortality rate than patients with low PIV (OR: 1.51, 95% CI, 1.26-1.80, p < 0.001). Incorporating PIV into the full model significantly improved model performance (odds ratio X2, p < 0.001) compared to the baseline model constructed with other inflammatory markers. PIV is a potent predictor of prognosis with better performance than other well-known inflammatory markers for patients with AHF.

Impact of Naples Prognostic Score on midterm all-cause mortality in patients with decompensated heart failure.

Aim: This work was designed to investigate the relationship between cardiac outcomes and Naples Prognostic Score (NPS) among heart failure (HF) patients. Materials & methods: This retrospective observational study enrolled 298 consecutive individuals hospitalized for New York Heart Association class 3-4 HF. The primary outcome was all-cause mortality. Secondary outcomes were rehospitalization and in-hospital death. Results: The high NPS group had a statistically greater rate of all-cause mortality (p < 0.001). In Cox regression analysis, integrating NPS considerably improved the performance of the full model over the baseline model (adjusted hazard ratio = 2.28; p = 0.004). Based on time-dependent receiver operating characteristic curve analysis, the NPS model outperformed the baseline and CONUT score models in discriminatory power in predicting the probability of survival. Conclusion: NPS was associated with short- and midterm mortality as well as rehospitalization.

Heart failure is a serious condition that affects millions of individuals around the world. This study was designed to investigate whether there is a relationship between Naples Prognostic Score (NPS) and worse outcomes in heart failure patients. A total of 298 patients with advanced heart failure were included in the study. Patients with a high NPS are more likely to pass away and need to be readmitted to the hospital. NPS also predicted survival more accurately than some other variables at an average of 15 months follow-up. In conclusion, NPS was found to be useful in predicting short- and medium-term mortality and readmissions in patients with advanced heart failure.

Right atrial reservoir strain and right ventricular strain improves in patients recovered from hospitalisation for non-severe COVID-19.

PURPOSE: Those hospitalised with coronavirus disease 2019 (COVID-19) have recently been shown to have impaired right ventricular (RV) strain, but data about the course of heart function after discharge are limited. Our aim was to compare right ventricular strain and right atrial reservoir strain (RASr) associated with COVID-19 between acute disease (during hospitalisation) and follow-up (after discharge). METHODS: In this retrospective single-center study, we analysed the echocardiograms of 43 patients hospitalised for non-severe COVID-19 between December 2020 and March 2021, undergoing echocardiography both during and after hospitalisation. In addition to conventional echocardiographic parameters, we applied 2-dimensional speckle tracking to obtain RV global longitudinal strain (RV-GLS), RV free wall strain (RV-FWS), and RASr. RESULTS: Mean (standard deviation) age of the study population was 50 (9) years, and 18 (42%) of the participants were women. Median duration between exams was 6 months (range, 5-7 months). Both mean RV-GLS and mean RV-FWS significantly increased at follow-up (-20.8 [3.8] vs. -23.5 [2.8], p < 0.001 and -23.3 [4.2] vs. -28.2 [2.8], p < 0.001; respectively), and RASr significantly improved as well (-32.3 [6.6] vs. -41.9 [9.8], p < 0.001). CONCLUSION: In patients hospitalised for non-severe COVID-19 pneumonia, RV-GLS, RV-FWS, and RASr improved significantly between acute disease and 6 months after discharge.

Preparation of hydrophobic macroinimer-based novel hybrid sorbents for efficient removal of organic liquids from wastewater.

Herein, the synthesis of hydrophobic macroinimer-based hybrid sorbents and their use in the removal of organic solvents from wastewater is explored. Polydimethylsiloxane (PDMS), 4,-4'-azobis-4-cyanopentanoyl chloride (ACPC), and methacryloyl chloride were reacted via bulk condensation polymerization to synthesize the macroinimer. The organogel systems were then prepared with macroinimer using different acrylic monomers of methyl acrylate, ethyl acrylate, and butyl acrylate without any additional crosslinker and initiator. The structural properties of the obtained final products were characterized by FT-IR, 1H-NMR, and TGA. The effect of alkyl chain length and macroinimer moieties in the organogel networks, as well as the swelling capacities of the prepared gels, was evaluated for different organic solvents and oils. The maximum solvent absorbencies of macroinimer-based organogels were determined as 85.3%, 100.9%, 1422.1%, 1660.0%, 3809.3%, and 5032.2% for diesel oil, gasoline, acetone, benzene, tetrahydrofuran (THF), and dichloromethane (DCM), respectively. Furthermore, adsorption-desorption kinetics, selective absorption from oil/water mixtures, temperature effect on the absorption capacity, and reusability tests were investigated. Obtained results showed that the prepared organogels possessed high swelling, efficient absorption capacity, and good oil separation performance in the removal of organic solvents from wastewater. The temperature-dependent absorption study shows no significant change in absorption capacity. Thus, the prepared macroinimer-based organogels in the present study demonstrate potential as prospective sorbents for organic pollutant cleanup from wastewater.

Pickering stabilized nanocellulose-alginate: A diosgenin-mediated delivery of quinalizarin as a potent cyto-inhibitor in human lung/breast cancer cell lines.

The current study explores the facile fabrication of multilayer self-assembled electrostatic oil-in-water Pickering emulsions (PEs) using quaternized nanocellulose (Q-NC) and diosgenin-conjugate alginate (DGN-ALG) particles as stabilizers to form hydrocolloid nanocarriers. The conditions of formulation such as storage time, pH, temperature and salt effect on the emulsion stability were evaluated. The results deduced showed good emulsion droplet stability over a period of 30 days. Morphological analysis revealed the hydrodynamic sizes of the PE droplets to be spherically shaped with an average diameter of 150 ± 3.51 nm. Creaming index, wettability and critical aggregation concentrations (CAC) as well as chemical characterization of the PEs were examined. In vitro release kinetics of encapsulated quinalizarin as a model drug was investigated with a determined cumulative drug release (CDR) of 89 ± 1.21% in simulated pH blood medium of pH 7.4. In addition, cellular internalization of the PEs was studied via confocal microscopy imaging and showed high cellular uptake. Also, evaluated in vitro cytotoxicity by MTT assay demonstrated excellent anticancer activity in human lung (A549) and breast (MCF-7) cancer cell lines.

Synthesis of naphthalimide derivatives with potential anticancer activity, their comparative ds- and G-quadruplex-DNA binding studies and related biological activities.

Two new cytotoxic 1,8-naphthalimide derivatives have been synthesized and characterized. Their biological activities as cytotoxicity and antimicrobial activities and inhibitory activities against DNA-polymerase were evaluated. The interactions of compounds with double-stranded- and quadruple-DNA have been studied by UV-Vis, fluorescent intercalator displacement, competition dialysis, circular dichroism and the findings were compared with the parent naphthalimide and the other compounds. The results show that both compounds (1 and 2) and the parent compound NI have strong cytotoxic activities against Beas-2B, MCF-7, HepG2 and MDA-MB-231 cancer cell lines, antimicrobial activities against Staphylococcus aureus ATCC 29213, Enterococcus faecalis ATCC 29212 and inhibitory activities towards Taq-polymerase and transcriptase. These novel cationic compounds 1 and 2 can stabilize G-quadruplexes DNA according to thermal denaturation experiments, they change the 3D structure of the DNA (see details in CD experiments) and they exhibit different binding affinities for q-DNA and ds-DNA revealed by spectrophotometric titrations and competitive dialysis studies.

Genipin crosslinked gelatin-diosgenin-nanocellulose hydrogels for potential wound dressing and healing applications.

The present study focuses on the synthesis and evaluation of neomycin-loaded hydrogels as potential substrate for wound healing application. Herein, genipin crosslinked gelatin interpenetrated diosgenin-modified nanocellulose (DGN-NC) hydrogels were synthesized. The hydrogels' chemical structures as well as surface morphology, mechanical property, and thermal behavior were characterized. Swelling analysis and gelation kinetics of the hydrogels were studied and the results obtained showed good swelling capacity as well as high gel yield. In addition, the prepared loaded hydrogels were evaluated for antibacterial activity against human pathogenic E. coli and S. aureus bacteria with inhibition capacity determined in the range of 50-88%. In vitro cytocompatibility and drug release studies were also explored under simulated physiological conditions achieving high cell viability and release percentage >80% and >90% after 24 h, respectively. In effect, the design hydrogels in the present study possess adequate incorporated antibacterial properties with significant potentials towards wound dressing and healing applications.

The comparative study of the DNA binding and biological activities of the quaternized dicnq as a dicationic form and its platinum(II) heteroleptic cationic complex.

The square-planar heteroleptic Pt(II) coordination compound [Pt(bpy)(dicnq)](NO3)2 (1) and the quaternized dicnq ligand, namely 12,13-dicyano-5,6-dihydrodipyrazino[2,3-f:1',2',3',4'-lmn][1,10]phenanthroline-4,7-diium dibromide (2) (Fig. 1) were synthesized and fully characterized by means of FTIR, NMR, MALDI-TOF MS and the purity was confirmed by CHN analyses. The DNA binding profiles of 1 and 2 were identified in an identical condition. The biological activities of these compounds were investigated by the assays of transcription and replication inhibition, cytotoxic and antimicrobial activity. The result of this study indicates that, both compounds strongly bind to DNA via intercalation but only 1 has a strong nuclease activity. The coordination compound of dicnq (1) binds to the DNA only slightly stronger than the quaternized form of dicnq (2), and is more potent as an inhibitor of transcription and replication and therefore, 1 has more potential as an anticancer agent but the compounds did not show cytotoxic activity against MCF-7 and MDA-MB-231 breast cancer, and DLD-1 colon cancer cell lines it was found that they only had activities against HepG2 liver cancer cell line with following IC50 values; 94.75 and 159.60 µM for 1 and 2, respectively. In addition, tested bacteria are more susceptible to compound 1. These biological activities of 1 may strongly be due to its ability to digest DNA as a chemical nuclease. According to this study, the quaternization of the ligand does not make biologically more active than the coordination compound of the same ligand in this case. The compound (1) is worth further investigation for its antitumor activities.

Outcomes of survivors of ST-segment elevation myocardial infarction complicated by out-of-hospital cardiac arrest: a single-center surveillance study.

OBJECTIVE: The aim of the present study was to evaluate in-hospital and long-term outcomes of ST-segment elevation myocardial infarction (STEMI) survivors who experienced out-of-hospital cardiac arrest (OHCA) and underwent primary percutaneous coronary intervention (PCI) at a high-volume center within the STEMI network. METHODS: The records of 2681 consecutive STEMI patients who underwent primary PCI between January 2009 and December 2014 at a single center in the STEMI network were retrospectively analyzed. Patients with STEMI complicated by OHCA were compared with a reference group of STEMI patients who did not experience OHCA. RESULTS: Compared with STEMI survivors without OHCA (n=2587, 96.5%), the frequency of anterior myocardial infarction, duration of hospitalization, rate of in-hospital major adverse cardiovascular and cerebrovascular events, and the incidence of ischemic cerebrovascular disease and major bleeding during in-hospital follow-up were significantly greater in those with OHCA (n=94, 3.5%). The distribution of age and gender was similar between the 2 groups. The primary PCI success rate was high and was similar in both groups. In-hospital mortality was significantly higher (18.1% vs. 1.5%; p<0.001) and survival at the 12th and 60th months was lower (74.5% vs. 96.5%; p<0.001 and 71.3% vs. 93.7%; p<0.001) in STEMI survivors with OHCA. OHCA was an independent predictor for in-hospital mortality (Odds ratio [OR]: 3.413; 95% confidence interval [CI]: 1.534-7.597; p=0.003) and all-cause mortality at 60 months (OR: 3.285; 95% CI: 2.020-5.340; p<0.001). CONCLUSION: Mortality was high in patients with STEMI complicated by OHCA, even though PCI was performed with the same success rate seen in patients without OHCA.

Effects of Bailout Tirofiban on In-Hospital Outcomes and Long-Term Mortality in Patients With ST-Segment Elevation Myocardial Infarction Undergoing Primary Percutaneous Intervention.

We retrospectively analyzed short- and long-term outcomes of patients who received bailout tirofiban during primary percutaneous intervention (pPCI). A total of 2681patients who underwent pPCI between 2009 and 2014 were analyzed; 1331 (49.6%) out of 2681 patients received bailout tirofiban. Using propensity score matching, 2100 patients (1050 patient received bail-out tirofiban) with similar preprocedural characteristics were identified. Patients who received bailout tirofiban had a significantly higher incidence of acute stent thrombosis, myocardial infarction, and major cardiac or cerebrovascular events during the in-hospital period. There were numerically fewer deaths in the bailout tirofiban group in the unmatched cohort (1.7% vs 2.5%, P = .118). In the matched cohort, in-hospital mortality was significantly lower (1.1% vs 2.4%, P = .03), and survival at 12 and 60 months were higher (96.9% vs 95.2%, P = .056 for 12 months and 95.1% vs 92.0%, P = .01 for 60 months) in the bailout tirofiban group. After multivariate adjustment, bailout tirofiban was associated with a lower mortality at 12 months (odds ratio [OR]: 0.554, 95% confidence interval [CI], 0.349-0.880, P = .012) and 60 months (OR: 0.595, 95% CI, 0.413-0.859, P = .006). In conclusion, bailout tirofiban strategy during pPCI is associated with a lower short- and long-term mortality, although in-hospital complications were more frequent.

Pickering emulsions stabilized nanocellulosic-based nanoparticles for coumarin and curcumin nanoencapsulations: In vitro release, anticancer and antimicrobial activities.

Coumarin and curcumin have a wide spectrum of biological and pharmacological activities including antioxidant, anti-inflammatory, antimicrobial and anticancer but hindered therapeutic applications due to low stability and poor solubility in water. The main objective of the current study was to overcome these drawbacks via improved bioavailability by nanoencapsulated emulsions. Pickering emulsion (PE) via oil-in-water approach were stabilized by aminated nanocellulose (ANC) particles through application of a full factorial optimization design for nanoemulsions containing different composition of oil phase with medium chain triglyceride (MCT) and Tween 80. The fabricated nanoemulsions and PEs with average particle sizes (≤150 nm) were obtained. Influencing factors such as ANC concentration, storage time and pH on the stability of emulsions were examined alongside zeta potentials. Encapsulation efficiency (EE) of coumarin and curcumin were determined as >90%. Release kinetic profiles for encapsulated PEs displayed sustained release with supposed increase bioavailability. Higher release percent were detected for curcumin encapsulated PE in contrast to coumarin. In vitro cytotoxicity evaluation for coumarin and curcumin loaded PEs were further investigated for anticancer and antimicrobial activities using human cell lines (L929 and MCF-7) and different microorganisms (Gram (+), Gram (-) and fungi), respectively. The results clearly demonstrated PE coumarin and curcumin as promising candidates to inhibit microbial growth and to prevent preferential killing of cancer cells compared to normal cells.

Gastrointestinal stromal tumors: A clinical and histopathological presentation of 27 cases.

OBJECTIVE: Gastrointestinal stromal tumors (GISTs) are mesenchymal tumors that express type 3 tyrosine kinase receptors and are thought to develop from the neoplastic transformation of the interstitial Cajal cells. The present study was performed to morphologically and immunohistologically evaluate GISTs, to compare their qualities using a GIST risk categorization system, and to identify the diagnostic and prognostic parameters of GISTs. MATERIAL AND METHODS: A total of 27 patients with GISTs underwent treatment and were followed up at the Gaziosmanpasa Taksim Training and Research Hospital. Descriptive statistics was used to calculate the mean and median values. Survival analysis was performed by the Kaplan-Meier method. The analyses were performed using the SPSS version 22.0 software. RESULTS: The mean follow-up time was 3.5 (5 months to 13 years) years. The mean age was 60.4 (29-82) years. The tumors were localized in the stomach (62.9%), extraintestinal areas (14.8%), intestine (7.4%), esophagus (7.4%), and rectum (7.4%). Twenty-four patients were classified according to the Fletcher system. Of these patients, 7 (25.9%) were classified as very low risk, 8 (29.6%) as low risk, 7 (25.9%) as intermediate risk, and 2 (7.4%) as high risk. Twenty-four patients underwent surgery. Of the 3 patients who did not undergo surgery, 1 had metastatic disease at the time of diagnosis, and 2 had mini- or micro-GISTs in the stomach. On endoscopic surveillance, all tumors remained stable. Three out of the 27 patients were lost to follow-up. Two patients developed recurrence, and 1 patient died of GIST. CONCLUSION: We analyzed the clinical and pathological characteristics of GIST. The most common site of tumor origin was the stomach. The size, mitotic index, and Ki-67 values were to be found high in intermediate- and high-risk groups and metastatic diseases.

Interatrial block as a predictor of atrial fibrillation in patients with ST-segment elevation myocardial infarction.

INTRODUCTION: Interatrial block (IAB) is strongly associated with recurrence of atrial fibrillation (AF) in different clinical scenarios. Atrial fibrosis is considered the responsible mechanism underlying the pathogenesis of IAB. The aim of this study was to investigate whether IAB predicted AF at 12 months follow-up in a population of patients with ST segment elevation myocardial infarction (STEMI). HYPOTHESIS: We aimed to investigate whether IAB predicted AF at 12 months follow up in a population of patients with STEMI. METHODS: Prospective, single center, observational study of patients presenting with ST-segment elevation myocardial infarction (STEMI) and referred to primary percutaneous coronary intervention (P-PCI). Surface electrocardiograms (ECG) were recorded on admission and at 6th hour post P-PCI. Patients were screened for the occurrence of AF at a 12-months visit. RESULTS: A total of 198 patients were included between September 2015 and September 2016. IAB (partial and advanced) was detected in 102 (51.5%) patients on admission. Remodeling of the P-wave and subsequent normalization reduced the prevalence of IAB to 47 (23.7%) patients at 6th hour. AF was detected in 17.7% of study patients at 12 months. Partial IAB (p-IAB) on admission (OR 5.10; 95% CI, 1.46-17.8; P = 0.011) and on 6th hour (OR 4.15; 95% CI, 1.29-13.4; P = 0.017), presence of a lesion in more than one coronary artery (OR 3.29; 95% CI, 1.32-8.16; P = 0.010) found to be independent predictors of AF at 12 months. CONCLUSION: IAB is common in patients with STEMI and along with the presence of diffuse coronary artery disease is associated with new onset of AF.

Novel Naphthalimide Derivatives as Selective G-Quadruplex DNA Binders.

A new derivate of 4-bromo-1,8-naphthalic anhydride and its quaternized analogue have been prepared and characterized. The interactions of both derivatives with human telomere quadruplex-DNA and ds-DNA have been comparatively studied by UV-visible (UV-Vis), fluorescent intercalator displacement assays, competition dialysis, circular dichroism (CD), agarose gel electrophoresis, and polyacrylamide gel electrophoresis. The results show that both derivatives can stabilize G-quadruplexes DNA, and they show different binding affinities for G-quadruplexes-DNA and ds-DNA. All spectroscopic studies have shown that the derivatives have a modest selectivity for G-quadruplex versus ds-DNA.

A design optimization study on synthesized nanocrystalline cellulose, evaluation and surface modification as a potential biomaterial for prospective biomedical applications.

In the present study, nanocrystalline cellulose (NCC) was prepared via acid hydrolysis and synthesis parameters were optimized via response surface modelling with a determined maximum NCC yield of 43.8%. The optimized NCC sample was subsequently surface modified via epichlorohydrin-mediated amination forming aminated nanocrystalline cellulose (A-NCC) with an amine content calculated as 1500µmol/g. The average particle size and zeta potential were determined 100nm and 325nm for NCC and A-NCC, respectively. Structural properties were analyzed by FTIR, TEM and XRD techniques. The obtained A-NCC as final product depicted a pKa value of 10.86±0.07 demonstrating favourable protonation of amine groups at physiological pH allowing the material to be suitable for prospective application in drug delivery and tissue engineering.

The effects of weight loss after sleeve gastrectomy on left ventricular systolic function in men versus women.

PURPOSE: To evaluate and compare the effects of weight lost after sleeve gastrectomy on left ventricular (LV) systolic function using both two-dimensional speckle tracking (2D-STE) and three-dimensional echocardiography (3DE) in men versus women. METHODS: In 53 obese patients referred for sleeve gastrectomy, 2D-STE and 3DE were performed prior to and 6 months after surgery. RESULTS: The study included 53 obese patients (62.3% female; mean age 36.8 ± 10.7 years). Six months after surgery, all patients demonstrated a significant decrease in body mass index, body weight, blood pressure, heart rate, LV end-diastolic dimension, myocardial wall thickness, LV mass, LV mass index, LV mass/height(2.7) , LV end-diastolic volume, LV end-systolic volume, and stroke volume as well as an increase in SV index and ejection fraction. There was no significant difference in measured variables between men and women at baseline or postsurgery, except for baseline LV end-diastolic dimension, and baseline and after surgery LV mass, LV mass index, and LV mass/height(2.7) , which were all significantly higher in men. CONCLUSIONS: Sleeve gastrectomy improves LV systolic function and contributes to reverse LV remodeling in both genders. © 2016 Wiley Periodicals, Inc. J Clin Ultrasound 44:492-499, 2016.

DNA studies of newly synthesized heteroleptic platinum(II) complexes [Pt(bpy)(iip)](2+) and [Pt(bpy)(miip)](2.).

Two new mono-nuclear heteroleptic platinum(II) complexes, [Pt(bpy)(iip)](PF6)2 (1) and [Pt(bpy)(miip)](PF6)2·2H2O (2) (bpy is 2,2'-bipyridine; iip is 2-(imidazo-4-yl)-1H-imidazo[4,5-f] [1,10] phenanthroline; miip is 2-(1-methylimidazo-2-yl)-1H-imidazo[4,5-f] [1, 10] phenanthroline), have been synthesized and fully characterized by CHN analysis, electrospray ionization and MALDI-TOF mass spectrometry, (1)H NMR, FT-IR (ATR), and UV-Vis spectrophotometer. Cytotoxicity, ability to inhibit DNA transcription and DNAse activity of the complexes were studied. The DNA-binding behaviors of both complexes have also been studied by spectroscopic methods, cyclic voltammetry and viscosity measurements. Both complexes showed cytotoxic properties and 2 was more cytotoxic than 1. DNA transcription was inhibited upon increasing concentrations of both complexes. The complex 2 was found to be a better inhibitor than 1. The same pattern can be seen in the DNAse profile of the complexes. In addition, 2 was found to promote cleavage of pBR322 DNA at a lower concentration than 1. The spectroscopic, electrochemical and viscometric results indicate that both complexes show some degree of binding to DNA in an intercalative mode, resulting in intrinsic binding constants K b = 3.55 ± 0.6 × 10(4) M(-1) and 7.01 ± 0.9 × 10(4) M(-1) for 1 and 2, respectively. The difference in the DNA-binding affinities of 1 and 2 may presumably be explained by the methylated imidazole nitrogen atom that makes the compound more hydrophobic and gives better intercalative binding ability to DNA's hydrophobic environment.

DNA-binding studies and antitumor evaluation of novel water soluble organic pip and hpip analogs.

Two new water-soluble pip and hpip analogs, 1 and 2 pip = 2-phenylimidazo[4,5-f][1, 10]phenanthroline; hpip = 2-(2-hydroxyphenyl)imidazo[4,5-f][1, 10]phenanthroline, have been synthesized and fully characterized by CHN analysis, MALDI-TOF MS, (1)H-NMR, IR (ATR), and UV-Vis methods. The DNA-binding behaviors of both compounds have been studied by viscosity measurements, spectroscopic methods, and gel electrophoresis studies, and potential for antitumor activity was evaluated by measuring their ability to inhibit DNA transcription. The results indicate that both compounds show some strong binding to DNA in a mixture of electrostatic and intercalative mode resulting in the intrinsic binding constants Kb of (4.0 ± 0.5) × 10(5) M(-1) and (7.5 ± 0.5) × 10(5) M(-1) for 1 and 2, respectively. These strong binding affinities for DNA are comparable for that seen for many transition metal-based intercalators. Comparatively, observed difference in the DNA-binding affinities of two complexes can be reasonably explained by the presence of an intra-molecular hydrogen-bonding between the ortho-phenolic group and the nitrogen atom of the imidazole ring. The extended co-planarity of 2 due to the intramolecular hydrogen bonding may lead to an enhancement of DNA binding affinity of 2. In addition, 2 can promote cleavage of pBR322 DNA upon irradiation, it inhibits DNA transcription and it is more cytotoxic at lower concentrations in comparison to 1, as revealed by the spectroscopic measurements.