Non-proteinogenic amino acids mitigate oxidative stress and enhance the resistance of common bean plants against Sclerotinia sclerotiorum.

White mold, caused by the necrotrophic fungus Sclerotinia sclerotiorum, is a challenging disease to common bean cultivation worldwide. In the current study, two non-proteinogenic amino acids (NPAAs), γ-aminobutyric acid (GABA) and ß-alanine, were suggested as innovative environmentally acceptable alternatives for more sustainable management of white mold disease. In vitro, GABA and ß-alanine individually demonstrated potent dose-dependent fungistatic activity and effectively impeded the radial growth and development of S. sclerotiorum mycelium. Moreover, the application of GABA or ß-alanine as a seed treatment followed by three root drench applications efficiently decreased the disease severity, stimulated plant growth, and boosted the content of photosynthetic pigments of treated S. sclerotiorum-infected plants. Furthermore, although higher levels of hydrogen peroxide (H2O2), superoxide anion (O2 •-), and malondialdehyde (MDA) indicated that S. sclerotiorum infection had markedly triggered oxidative stress in infected bean plants, the exogenous application of both NPAAs significantly reduced the levels of the three studied oxidative stress indicators. Additionally, the application of GABA and ß-alanine increased the levels of both non-enzymatic (total soluble phenolics and flavonoids), as well as enzymatic (catalase [CAT], peroxidases [POX], and polyphenol oxidase [PPO]) antioxidants in the leaves of S. sclerotiorum-infected plants and improved their scavenging activity and antioxidant efficiency. Applications of GABA and ß-alanine also raised the proline and total amino acid content of infected bean plants. Lastly, the application of both NPAAs upregulated the three antioxidant-related genes PvCAT1, PvCuZnSOD1, and PvGR. Collectively, the fungistatic activity of NPAAs, coupled with their ability to alleviate oxidative stress, enhance antioxidant defenses, and stimulate plant growth, establishes them as promising eco-friendly alternatives for white mold disease management for sustainable bean production.

A cross-sectional analysis of the association between diabetes self-care practices and blood glucose regulation among Egyptian diabetic patients.

OBJECTIVE: Diabetes Mellitus (DM) is a main public health issue worldwide, with Egypt among the world's top countries with diabetic patients. Data on the degree of self-care behaviors of Egyptian diabetic patients is not fully reported. Therefore, the study aimed to assess the adequacy of diabetes self-management (DSM) habits among diabetic patients in Egypt and to identify associated socio-demographic factors that could negatively impact the patients' glycemic state, using a structured questionnaire. SUBJECTS AND METHODS: This study was a cross-sectional observational study. The diabetes self-management questionnaire (DSMQ) was used to assess diabetes self-care activities, which is a 16-item questionnaire. The statistical analysis was conducted on SPSS software, and the data were significant with a p-value <0.05. RESULTS: A total of 2,164 participants were included. The majority of the patients (83.8%) had type 2 DM. The mean glycated hemoglobin (HbA1c) of the study group was 8.44±1.99. Significant differences were found between different glycemic control groups both in terms of the DSMQ sum scores and the subscale scores, with the exception of physical activity. Moreover, there was a significant weak inverse correlation between the total DSMQ sum score and HbA1c ≥9.0% (ρ=-0.116, p<0.01). The overall internal consistency (Cronbach's alpha) was acceptable (0.756). CONCLUSIONS: The study indicated that patients with controlled blood glucose had significantly higher 'glucose management', and 'total DSMQ sum' scores compared to uncontrolled diabetic patients. All significant correlations between assessed parameters and DSMQ were weak.

Antineutrophil Cytoplasmic Antibody (ANCA)-Associated Renal Vasculitis Following COVID-19 Vaccination: A Case Report and Literature Review.

Antineutrophil cytoplasmic antibody (ANCA)-associated vasculitis (AAV) is an immune-mediated disorder of small and medium-sized vessels, characterized by the production of autoantibodies that target the neutrophilic antigens leading to mononuclear cell infiltration and destruction of blood vessels in lungs, skin, and kidneys. Although rare, the coronavirus disease 2019 (COVID-19) vaccine may trigger autoimmune vasculitis. We report a rare case of ANCA-associated renal vasculitis following COVID-19 vaccination in a 59-year-old male who presented with flu-like symptoms and deranged renal function tests. He received his second dose of the Pfizer COVID-19 vaccine 17 days ago. His clinical picture, serological testing, and radiological imaging were concerned with glomerular disease. His serum was positive for ANCAs, and the renal biopsy specimen revealed pauci-immune glomerulonephritis. He was diagnosed with AAV-associated renal vasculitis following COVID-19 vaccination because no other etiology was identified. His clinical improvement after starting rituximab and steroids reinforced the diagnosis.

Ocular manifestations of recent viral pandemics: A literature review.

Viral pandemics often take the world by storm, urging the medical community to prioritize the most evident systemic manifestations, often causing ocular manifestations to go unnoticed. This literature review highlights the ocular complications of the Monkeypox, SARS-CoV-2, MERS, Ebola, H1N1, and Zika viruses as the most recent viral pandemics. Research into the effects of these pandemics began immediately. Moreover, it also discusses the ocular complications of the vaccines and treatments that were used in the scope of the viral pandemics. Additionally, this review discusses the role of the eye as an important route of viral transmission, and thereafter, the International recommendations to reduce the incidence of viral transmission were mentioned. Lastly, this paper wants to lay out a platform for researchers who want to learn more about how viruses show up in the eye.

Clopidogrel-Associated Interstitial Lung Disease: A Case Report and Literature Review.

Clopidogrel is an antithrombotic agent widely used for the secondary prevention of cerebrovascular and cardiovascular complications. Clopidogrel can cause serious adverse events, including gastrointestinal bleeding. Pulmonary complications caused by clopidogrel are not widely described, and clopidogrel-induced interstitial lung disease (ILD) is rare. Here, we report a case of drug-induced ILD in a patient who presented with dyspnea, chest pain, and mild fever. The patient underwent percutaneous coronary intervention two months ago and was commenced on clopidogrel. He was diagnosed with clopidogrel-induced ILD based on clinical and imaging findings, history of drug exposure without any change, exclusion of other respiratory disorders, and clinical improvement after discontinuation of clopidogrel and steroid use.

The Impact of Magnetic Field on Insecticide Toxicity Measured by Biological and Biochemical Parameters of Earias insulana (Boisd).

This study illustrates the effect of magnetic field (MF) on the toxicity of two insecticides, emamectin benzoate (Emazoate 2.15% EC) and spinosad (SpinTor 24% SC), and determines their adverse effects on the bollworm (Earias insulana) through various biological and biochemical assays. The investigation indicated that exposure to the insecticides in a MF of 180 mT resulted in stronger toxicity, with LC50 values of 0.162, 1.211, and 1.770 ppm, respectively. In addition, the results showed that magnetized insecticides significantly increased in the duration of the total immature stages (larvae and/or pupae) 32.1 and 36.6 days, compared with 27.9 and 30.5 days, respectively, in the nonmagnetized insecticides, while untreated check was 21 days. Also, the magnetized insecticides reduced the percentage of adult emergence, and increased deformations in the larval and pupal stages. Furthermore, sex ratio was greatly affected by exposure to both insecticides in conjunction with the MF. Exposure of the larvae of E insulana to magnetized insecticides can bring about malfunction in some biochemical process and significantly decreased the invertase activity, and decreased the total protein and carbohydrates. In contrast, it can increase amylase compared with nonmagnetized insecticides and untreated controls. Results concluded that the two insecticides' MF affected growth, survival time, and biological and biochemical parameters of E. insulana. © 2022 Bioelectromagnetics Society.

Frequency of Genotypes and Allelic Polymorphisms of Vitamin D Receptor in Egyptian Psoriatic Patients and Their Association With Disease Severity, Immune Modulation of IL-22 Levels and The Response to Topical Calcipotriol Treatment: A Case Control Study.

Objective: This study was performed to determine the genotype and allelic frequencies (polymorphisms) of the four genes of vitamin D receptor (VDR) among Egyptian psoriatic patients and healthy controls to explore their association with disease severity (PASI) score and immune modulation of IL-22 cytokine and to predict the response to topical calcipotriol treatment. Patients and Methods: The frequencies of the four VDR gene polymorphisms (FokI, ApaI, TaqI, and BsmI) in blood samples of 51 adult Egyptian patients with psoriasis vulgaris and 50 healthy controls were evaluated using restriction fragment length polymorphism (RFLP)-PCR. Serum levels of IL-22 were measured by ELISA. Results: The most frequent genotype (wild) in the studied patients was Apa1; AA (88.2%) followed by Fok1; FF (47.1%) and Taq1; TT (47%), while Bsm1; BB genotype was (27.7%). The most frequent allele polymorphisms either in one allele (Bb) or both alleles (bb) in psoriatic patients were 72.5%, followed by Ff, ff (52.9%) and Tt, tt (52.9%). The less frequent allelic polymorphism was Aa, aa (27.7%). Insignificant differences in the frequency of genotype (wild) and allelic polymorphisms were detected between patients and controls (P > 0.05). A significantly higher serum concentration of IL-22 (ng/mL) was detected in patients than controls (P = 0.001). Further, 66.6% of patients displayed a clinical response, while 33.4% were non-responders. A significantly higher expression of TaqI polymorphism was detected in (100%) of non-responders (P < 0.001), which was also correlated with disease severity (r = 0.515, P < 0.01). Conclusion: These results suggest that the VDR TaqI polymorphism is the only gene correlated to psoriasis susceptibility in the Egyptian population, and affects the response to topical calcipotriol treatment but does not affect IL-22 immune modulation.

Changes in Feeding Behavior and Feeding Stress Among Mothers of Preschoolers Before and During the Novel Coronavirus Pandemic.

Objective: To examine changes in maternal feeding behaviors (MFB) and maternal feeding stress (MFS) among mothers of preschoolers in Saudi Arabia before and during the novel coronavirus pandemic. Methods: This is a prospective cohort study including 64 mothers of preschoolers who were drawn from a sample of a 2019 study. Study questionnaire was completed during November-December 2020. MFB were assessed using the Child Feeding Questionnaire-Arabic (CFQ-A) and MFS was assessed using the MFS-mealtimes index and the MFS-maternal resentment/difficult child index. Paired samples t-tests were used to examine changes in MFB and MFS. Results: Mothers have reported an increase in perceived responsibility (M = 4.09, SD = 0.87 vs. M = 4.33, SD = 0.59, P-value < 0.05) and monitoring (M = 4.23, SD = 0.73 vs. M = 4.48, SD = 0.66, P-value < 0.05) during the pandemic period compared to the period prior to the pandemic. Mothers have reported a decrease in use of food as a reward (M = 4.11, SD = 0.87 vs. M = 2.30, SD = 0.88, P-value < 0.001) and concern about child's diet (M = 3.34, SD = 1.12 vs. M = 2.55, SD = 1.04, P-value <0.001). There was an increase in MFS-maternal resentment/difficult child (M = 2.47, SD = 0.68 vs. M = 2.71, SD = 0.72, P-value < 0.01). Conclusions: Findings can help inform future research aiming to measure the long-term effects of the pandemic on child outcomes.

Comparative study on effect of mesenchymal stem cells and endothelial progenitor cells on treatment of experimental CCL4-induced liver fibrosis.

BACKGROUND: We speculated impacts of BM-MSCs and UC-EPCs on reversal of hepatic injury induced by carbon tetrachloride (CCl4). Fifty adult rats were divided into five groups: control group, CCl4A group, CCl4B group, CCl4/BM-MSCs group and CCl4/UC-EPCs group. Blood samples were driven to measure concentration of albumin and ALT. Quantitative expression of HGF, TGF-ß, MMP-2, and VEGF were assessed by PCR. Histological and immunohistochemistry examination of the liver tissue were performed. RESULTS: There was elevating albumin (p < .05) and reducing ALT (p < .05) concentrations in groups treated with BM-MSCs and UC-EPCs compared to untreated CCL4A&B groups. UC-EPCs treated group have significantly higher MMP-2 and VEGF (p < .01) genes expression than BM-MSCs treated group. Furthermore, UC-EPCs were more valuable than BMMSCs in increasing gene expression of HGF (p < .05) and immunohistochemistry of α-SMA and Ki-67 (p < .01). BM-MSCs have significantly lower TGF-ß (p < .00) compared to UC-EPCs. CONCLUSION: This study highlighted on liver regeneration role of both UC-EPCs and BM-MSCs in liver fibrosis.

Effects of ABO blood groups and RH-factor on COVID-19 transmission, course and outcome: A review.

ABO and Rh blood grouping systems are two of the non-modifiable risk factors that play an important role in the susceptibility, severity and outcomes of COVID-19 infection. This review explores these associations all over the world, in an attempt to conclude a clear idea for future reference in clinical practice. In the present review, a link has been drawn between blood groups and COVID-19 transmission, course and prognosis, as literature suggests that blood group O plays a protective role against the infection, while blood group A exhibits a higher risk of exacerbation. In contrast with Rh negative individuals, Rh positive individuals are prone to more severe infection and complications, despite the fact that the underlying mechanisms of this association remain understudied. Nevertheless, the connection remains subject to controversy; since some studies report doubts about it. Thus, this association requires further investigation.

Hemphagocytic Lymphohistiocytosis Secondary to COVID-19: A Case Report.

Hemophagocytic lymphohistiocytosis (HLH) is categorized into primary HLH and secondary HLH. Primary or familial HLH is an autosomal recessive disorder due to mutation in immune regulatory genes. Secondary HLH is an uncommon hyperinflammatory disease triggered by a critical illness (malignancies or viral infection) that induces an uncontrollable excessive immune response, which results in multiorgan failure. Due to the rarity of the syndrome, HLH is associated with worse outcomes. Severe coronavirus disease-19 (COVID-19) is identified as a trigger of HLH, and published literature suggests that patients with severe COVID-19 are at high risk of developing HLH. COVID-19-associated HLH is rarely reported in the literature. Herein we present a case of secondary HLH due to COVID-19 presented in the emergency department with prolonged non-resolving fever.

Caught Between External Pressures and Internal Battles: Psychosocial Factors Affecting Gestational Weight Gain - A Scoping Review.

Many physical factors (including maternal comorbidities) affecting gestational weight gain (GWG) have been widely studied; however, the psychosocial aspects pertaining to this need to be put under the microscope, especially in countries characterized by low indicators of socioeconomic development. Gaining and maintaining an adequate amount of weight during pregnancy is important to prevent premature deliveries, fetal demise, fetal macrosomia, shoulder dystocia during delivery, emergency cesarean sections, postpartum weight retention, childhood obesity, etc. A scoping review of the articles published in the last five years has revealed that perinatal outcomes like gestational weight are influenced by certain psychosocial factors, including, but not limited to, intimate partner violence, lack of social support and recognition, financial distress, household food insecurity, chronic stress and depression related to pregnancy, eating pathologies, and low self-esteem. Employing a multi-disciplinary approach, which involves seeking the help of psychiatrists/psychologists, obstetricians, nutritionists, and public health specialists, can help us mitigate undesirable outcomes related to inadequate and excessive weight gain during pregnancy. More intervention-based research focusing on psychosocial factors relating to GWG is needed in regions like South Asia, which is associated with low indicators of socioeconomic development.

First Successful Large-Scale Introduction of an Enhanced Recovery after Bariatric Surgery (ERABS) Program in the Middle East: The Results and Lessons Learned of Tawam Hospital/Johns Hopkins, a Tertiary Governmental Center in the UAE.

BACKGROUND: Although enhanced recovery after bariatric surgery (ERABS) has proven to be safe and cost-effective, this concept is relatively new in the Middle East. METHODS: A retrospective analysis of consecutive registered cohorts of patients who underwent primary and purely laparoscopic sleeve gastrectomy (LSG) or laparoscopic Roux-en-Y gastric bypass (LRYGB) were compared before introduction of ERABS (2010-2014) and after ERABS (2015-2017) at Tawam Hospital/Johns Hopkins, the UAE. RESULTS: A total of 462 eligible bariatric patients (LSG 414 and LRYGB 48) were operated on before and 1602 (LSG 1436 and LRYGB 166) after introduction of the ERABS. Significant improvements of mean patient time of the patient being within the OR for LSG (from 2:27 to 1:23 min, p = 0.000) and LRYGB (from 3:17 to 1:59 min, p = 0.000) were achieved when comparing pre-ERABS with after introduction of ERABS. Furthermore, there was a significant decrease in LOS in both LSG (from 3.2 to 1.5 days, p = 0.000) and in LRYGB (from 3.5 to 1.7 days, p = 0.000). Major (CD classification III-IV) complications decreased significantly in LSG (from 13.8 to 0.8%, p = 0.000) and were similar in LRYGB (from 4.2% to 3.0%, p = NS). The readmission rate for LSG (from 2.9 to 2.6%, p = NS) or LRYGB (from 0 to 4.8%, p = NS) and the reoperation rates after LSG (from 0.7 to 0.5%, p = NS) and LRYGB (from 0 to 2.4%, p = NS) did not differ between both groups following introduction of ERABS. CONCLUSIONS: Implementation of a standardized ERABS program in the Middle East is feasible and safe and leads to reduced LOS and OR times.

Anti-proliferative and anti-apoptotic potential effects of epigallocatechin-3-gallate and/or metformin on hepatocellular carcinoma cells: in vitro study.

The effects of epigallocatechin-3-gallate (EGCG) and metformin single treatment have been tested against hepatocellular carcinoma (HCC). This study aimed to assess the combination effects of EGCG and metformin on proliferation and apoptosis of HepG2cells and identified new potential molecular targets. The effect of EGCG and metformin against cell proliferation in HepG2 was determined using MTT assay. Reverse transcription polymerase chain reaction was applied to examine the gene expression of cyclin D1, lncRNA-AF085935, caspase-3, survivin and VEGF. The level of protein expression of glypican-3 was assessed by western blot. In HepG2 cells, EGCG and metformin combination treatment exhibited high significant effect against tumor proliferation. It significantly reduced cyclin D1, lncRNA-AF085935, glypican-3 and promoted apoptosis through increasing caspase3 and decreasing survivin compared to control cells. Moreover, EGCG and metformin treated cells showed decreased expression levels of VEGF. Our study provided new insights of the anticarcinogenic effects of EGCG and metformin on HCC through their effects on glypican-3 and lncRNA-AF085935.

Marginal analysis in assessing factors contributing time to physician in the Emergency Department using operations data.

Background: Standard Emergency Department (ED) operations goals include minimization of the time interval (tMD) between patients' initial ED presentation and initial physician evaluation. This study assessed factors known (or suspected) to influence tMD with a two-step goal. The first step was generation of a multivariate model identifying parameters associated with prolongation of tMD at a single study center. The second step was the use of a study center-specific multivariate tMD model as a basis for predictive marginal probability analysis; the marginal model allowed for prediction of the degree of ED operations benefit that would be affected with specific ED operations improvements. Methods: The study was conducted using one month (May 2015) of data obtained from an ED administrative database (EDAD) in an urban academic tertiary ED with an annual census of approximately 500,000; during the study month, the ED saw 39,593 cases. The EDAD data were used to generate a multivariate linear regression model assessing the various demographic and operational covariates' effects on the dependent variable tMD. Predictive marginal probability analysis was used to calculate the relative contributions of key covariates as well as demonstrate the likely tMD impact on modifying those covariates with operational improvements. Analyses were conducted with Stata 14MP, with significance defined at p < 0.05 and confidence intervals (CIs) reported at the 95% level. Results: In an acceptable linear regression model that accounted for just over half of the overall variance in tMD (adjusted r2 0.51), important contributors to tMD included shift census (p = 0.008), shift time of day (p = 0.002), and physician coverage n (p = 0.004). These strong associations remained even after adjusting for each other and other covariates. Marginal predictive probability analysis was used to predict the overall tMD impact (improvement from 50 to 43 minutes, p < 0.001) of consistent staffing with 22 physicians. Conclusions: The analysis identified expected variables contributing to tMD with regression demonstrating significance and effect magnitude of alterations in covariates including patient census, shift time of day, and number of physicians. Marginal analysis provided operationally useful demonstration of the need to adjust physician coverage numbers, prompting changes at the study ED. The methods used in this analysis may prove useful in other EDs wishing to analyze operations information with the goal of predicting which interventions may have the most benefit.

Evaluation of the biological activity of novel monocationic fluoroaryl-2,2'-bichalcophenes and their analogues.

A series of bichalcophene fluorobenzamidines 5a-e was synthesized from the corresponding mononitriles 4a-e via a direct reaction with lithium bis(trimethylsilyl)amide LiN(TMS)2 followed by de-protection with ethanolic HCl (gas). Bichalcophene fluorobenzonitriles 4a-e were prepared adopting a Stille coupling reaction between the bromo compounds 3a-c and 2-(tri-n-butylstannyl)furan or analogues. As an approach to drug discovery, the structure-antimutagenicity relationship of novel fluoroarylbichalcophenes was examined using the Ames Salmonella/microsomal assay. At nontoxic concentrations (10 and 20 µM), all derivatives alone or in combination with sodium azide (NaN3; 2 µg/plate) or benzo[a]pyrene (B[a]P; 20 µM) in the presence of S9 mix were not mutagenic. The fluoroaryl derivatives significantly reduced the NaN3-induced and B[a]P-induced mutagenicity under pre-exposure and co-exposure conditions. The recorded antimutagenic activity of fluoroaryl derivatives varied depending on the kind of mutagen and the exposure regimen. Monocationic fluoroarylbichalcophenes were superior to the corresponding mononitriles in reducing B[a]P-induced mutagenicity. Nevertheless, mononitriles were more active against NaN3, especially at low concentrations and under pre-exposure treatments. The antimutagenic activity was congruent with a high antioxidant activity that could promote the DNA repair system. The fluorine substitution changed the antimutagenic signature of bichalcophenes. Some of these compounds could be selected for further anticancer studies.

The Conyza triloba extracts with high chlorophyll content and free radical scavenging activity had anticancer activity in cell lines.

The discovery of anticancer agents paradigm has been shifted to natural resources to overcome the toxicity of many synthetic agents at early clinical stages. In the present study, the antimutagenic, anticancer, phytochemistry, and free radical scavenging activities of five extracts of Conyza triloba were investigated. Extracts II (water : methanol), III (methylene chloride), and IV (methylene chloride : methanol) had the highest chlorophyll content and the highest superoxide scavenging, and metal chelating activities comparable to that of trolox. They also showed DPPH(•) scavenging activities better than that of α -tocopherol. Virtually all extracts exerted a strong (>40% reduction) antimutagenic activity against sodium azide and benzopyrene. Extracts II, III, and IV showed a remarkable growth inhibition profile with GI50 of 0.07-0.87 µg for Hepa1c1c7 and H4IIE1, A549, HT29, and PC3 cell lines and totally abated the growth of all cell lines, except for the breast cells, at 0.3-7.0 µg. The present study found a strong correlation between the chlorophyll content of Conyza extracts and their DDPH scavenging, metal chelating, and in vitro cytotoxic and cytostatic activities most probably through triggering apoptosis. This study could offer a platform for future studies and help selecting the vital features that identify the extract with potential anticancer activities.

The position of imidazopyridine and metabolic activation are pivotal factors in the antimutagenic activity of novel imidazo[1,2-a]pyridine derivatives.

The antimutagenic activity of eight novel imidazo[1,2-a]pyridine derivatives (I-VIII) against sodium azide (NaN3) and benzo[a]pyrene (B[a]P) was evaluated using the Salmonella reverse mutation assay. At non-toxic concentrations (12.5-50 µM), imidazopyridines I, II, III, and V with a terminal imidazopyridine group were mutagenic, while derivatives VII and VIII with a central imidazopyridine group were not mutagenic. Compounds IV, VII, and VIII exerted a moderate antimutagenic activity against NaN3 under pre-exposure conditions, and a strong activity (>40%) against B[a]P in the presence of S9 under both pre- and co-exposure conditions and mostly independent on the dose. Imidazopyridines possibly inhibited the microsomal-dependent activation of B[a]P. The demethylated derivative VII was the most active antimutagen. All imidazopyridines had a low to moderate antioxidant activity. The antibacterial activity of imidazopyridines was sporadic and moderate probably due to the failure of bacteria to convert imidazopyridines into active metabolites. The position of imidazopyridine was a pivotal factor in the mutagenic/antimutagenic activity. The strong antimutagenic compounds were dicationic planar compounds with a centered imidazo[1,2-a]pyridine spacer. With LD50 of 60 mg/kg in mice for both derivatives VII and VIII, it is safe to investigate the anticancer activity of these derivatives in animal models.

Novel 4-substituted phenyl-2,2'-bichalcophenes and aza-analogs as antibacterial agents: a structural activity relationship.

Antibiotic resistance is a major health problem; therefore, new antibacterial agents will need to be continuously developed. A series of novel bichalcophenes has been tested and found to have antimicrobial activity against selected bacteria. Due to the promising antimicrobial effects of these 4-substituted phenyl bichalcophene derivatives, the study reported here was launched to examine the interaction between novel bichalcophenes and tetracycline. The minimum inhibitory concentration values for all bichalcophenes were between 8 and 64 µM. Many of the bichalcophenes had synergistic activity that increased the inhibitory effect of tetracycline against bacterial growth, as indicated by the fractional inhibitory concentration index. The post-antibiotic effects of the novel bichalcophenes were determined. Many bichalcophenes were able to elongate the period required for bacteria to recover and grow after a brief exposure to tetracycline. Escherichia coli did not develop resistance to many bichalcophenes over a period of 7 days. A structural activity relationship could be characterized, as monocationic derivatives were more active than the corresponding mononitriles. The presence of a pyridyl group and/or furan ring reduced the activity, while the presence of a phenyl or thiophene ring enhanced the antibacterial activity. Our results suggest that bichalcophenes could be useful to elevate the shelf life of many antibiotics.

Antimutagenic and antioxidant activity of novel 4-substituted phenyl-2,2'-bichalcophenes and aza-analogs.

Evaluation of the potential antimutagenic activities of new compounds by Ames assay has been of great interest for the development of novel therapeutics for many diseases including cancer. Ten novel bichalcophenes with in vitro and in vivo broad spectrum activities against various microbial strains were investigated throughout the present study for their cytotoxic, antioxidant, and antimutagenic potential in a Salmonella reverse mutation assay system against sodium azide (NaN(3)) and benzo[a]pyrene (B[a]P). At nontoxic concentrations, all bichalcophenes alone or in combination with NaN(3) (1 µg/plate) or B[a]P (20 µM) with S9 mix were not mutagenic. The bichalcophenes significantly reduced NaN(3)- and B[a]P-induced mutagenicity under pre-exposure and co-exposure conditions in a concentration-independent manner. However, the antimutagenic activity of bichalcophenes against B[a]P varied depending on the exposure regimen, being more effective under pre-exposure conditions. The antimutagenic activity was correlated with a high antioxidant activity that could promote the DNA repair system. Bichalcophenes are least likely to interfere with the microsomal bioactivation of B[a]P. Monocationic bichalcophenes were superior to the corresponding mononitriles as antimutagenic agents against both mutagens investigated, possibly due to the higher nucleophilic centers they have which could bind and protect the bacterial DNA. Three monocationic compounds were shown to have a strong anticancer activity against the 58 cell line. Based on the results of the present investigation, monocationic compounds (1, 4, and 5B) will be selected for further time consuming and costly chemoprevention studies in animal models.