Chemical profiles and bioactivities of polyphenolic extracts of Lavandula stoechas L., Artemisia dracunculus L. and Ocimum basilicum L.

This study assessed the chemical profiles and bioactivities of the infusions, decoctions and hydroethanolic extracts of tarragon, basil and French lavender. The extracts were chemically characterised (HPLC-DAD-ESI/MS) and their bioactivities were evaluated in vitro. All extracts revealed antimicrobial, antifungal and antioxidant properties. French lavender extracts showed higher total phenolic content, regardless of the extraction method used, and antioxidant and antitumour capacities, but no anti-inflammatory action. All basil and two of the tarragon extracts revealed anti-inflammatory power. Thus, tarragon, basil and French lavender extracts may be considered for inclusion in foods, as preservatives or functional ingredients. Nonetheless, further studies must be conducted to evaluate the pharmacokinetic parameters of the bioactive compounds.

Evaluation of quality of life in patients with schizophrenia: An inpatient social welfare institution-based cross-sectional study.

Schizophrenia is a chronic mental illness with a poor quality of life (QoL). The main aim of this study was to measure the QoL and factors that affect the QoL of patients with schizophrenia placed in a social welfare institution. This cross-sectional study included 287 patients with schizophrenia who were treated in a long-stay social care institution in which QoL was assessed using five different instruments: the World Health Organization Quality of Life scale, the EuroQoL Five-Dimension-Five-Level scale (including the visual analog scale), the Quality of Life Enjoyment and Satisfaction Questionnaire - Short Form, and the Brief Psychiatric Rating Scale. To determine the impact of patients' characteristics on score values, multiple linear regression using backward elimination was employed. Due to non-normality in the distribution of the dependent variables, a Box-Cox power transformation was applied to each dependent variable prior to conducting multiple linear regression analysis. Results revealed that patients with schizophrenia have lower QoL. Our study revealed that age, level of education, type of accommodation, type of pavilion, age of onset of the disease, number of prescribed antipsychotics, number of psychiatric comorbidities, duration of therapy, and the number of daily doses of antipsychotics are dominant contributors to the QoL in patients with schizophrenia who were treated in social welfare institution.

Exposure to Stress and Burnout Syndrome in Healthcare Workers, Expert Workers, Professional Associates, and Associates in Social Service Institutions.

Background and Objectives: Workplace burnout syndrome is often as sociated with particular aspects of certain job positions, especially those that entail working with people with special needs. The burnout syndrome in healthcare jobs is a serious problem that has grown into an epidemic among healthcare workers and associates. The aim of this research is to assess the presence of stress and burnout syndrome at work with healthcare workers, expert workers, professional associates, and associates in social service institutions in Belgrade. Materials and Methods: This research was conducted in the form of a cross-sectional study of a representative sample in social institutions in Belgrade. It was conducted from March to the end of June of 2023. The sample of the study had 491 participants. The questionnaires used were a structured instrument with social-demographic and social-economic characteristics, workplace characteristics, lifestyle characteristics, and the following questionnaires: DASS-21, Copenhagen, Brief Resilience Scale, and Brief Resilient Coping Scale. Results: The end results indicate the following to be significant risk factors for the occurrence of workplace burnout syndrome: overtime (OR = 2.62; CI = 1.50-4.56), BRS average score (OR = 0.28; CI = 0.17-0.44), DASS21 D heightened depression (OR = 2.09; CI = 1.1-4.04), DASS21 A heightened anxiety (OR = 2.38; CI = 1.34-4.21), and DASS21 S heightened stress (OR = 2.08; CI = 1.11-3.89). The only protective risk factor that stood out was the self-assessment of health levels (OR = 0.60; CI = 0.42-0.85). Conclusion: Overtime is a significant factor associated with workplace burnout. Apart from it, other significant factors associated with workplace burnout were heightened depression, anxiety, and stress levels.

Risk Factors for Potential Drug-Drug Interactions in Outpatients with Dyslipidemia.

Background: Patients with dyslipidemia are usually multimorbid and require polypharmacy. Therefore, it is important to identify potential drug-drug interactions (pDDIs) in time to prevent their consequences. We aimed to identify and analyze risk factors contributing to their occurrence to guide health professionals. Methods: A prospective cross-sectional study of 216 outpatients with dyslipidemia was conducted from May 2021 to April 2022 in Podgorica, the capital of Montenegro. pDDIs were identified using Medscape, Epocrates, and Drugs online interaction checkers. Multivariate regression analysis was performed to evaluate the potential predictors of interactions. Results: pDDIs were detected in 212 (98.1%) participants, whereas pDDIs with high clinical significance were detected in 25.46%, 40.74%, and 58.8% of subjects by Drugs, Epocrates, and Medscape, respectively. Polypharmacy emerged as a risk factor for the occurrence of pDDIs in all three checkers in each category of clinical significance. The use of non-steroidal anti-inflammatory drugs and antiplatelet drugs contributes to the incidence of severe pDDIs B=1.014, 95%CI 0.681-1.346, P=0.000 and B=0.492, 95%CI 0.286-0.698, P=0.000, by Epocrates and Medscape respectively. The number of prescribers per patient was a protective factor against moderate pDDI B= -0.858, 95%CI -1.572-(-0.144), P=0.019 and B= -0.956, 95%CI -1.671-(-0.241), P=0.009, by Medscape and Epocrates, respectively, but a risk factor for the occurrence of minor pDDIs B=0.373, 95%CI 0.033-0.712 P=0.032 and B=0.143, 95%CI 0.042-0.244, P=0.006, by the same checkers. Conclusion: Knowledge of the risk factors contributing to the occurrence of pDDIs is important for the development and implementation of strategies for their prevention, and given the high prevalence of dyslipidemia, understanding these factors seems crucial nowadays.

Natural extracts against agricultural pathogens: A case study of Celtis australis L.

Plant extracts and other plant products have been used as an alternative to synthetic fungicides or an additional way to reduce their use. The choice of plant extracts and their application depends on their functional characteristics, availability, cost-effectiveness, and their impact on phytopathogens, and also on the environment. Therefore, the present study aims to assess the potential of Celtis australis methanolic extracts as source of compounds with antifungal activity. Methanolic extracts prepared from leaves and unripe mesocarps of C. australis collected from different localities of Montenegro (Podgorica-PG, Donja Gorica-DG, and Bar-BR) were evaluated for their phenolic compounds' composition as well as antifungal and cytotoxic properties. Obtained results revealed that extracts contain various bioactive constituents including phenolic acids, flavonoids, and their derivatives. The predominant phenolic acid was ferulic acid, identified in leaf samples from DG (187.97 mg/100 g dw), while isoorientin was the most abundant phenolic compound found in all examined samples. Regarding antifungal potential of the tested samples, all but one (prepared from mesocarp BR) possessed higher activity than Previcur, a commercial systemic fungicide intended to control seedlings. In vitro studies on HaCaT cell line showed that the extracts had no toxic effect toward the tested cell line. These results lead to the conclusion that methanolic extracts of C. australis can become an alternative to the use of synthetic fungicides in agriculture. Those extracts represent natural biodegradable fungicides and enable more efficient control of pathogenic fungi.

Phytochemical Composition and Bioactive Potential of Melissa officinalis L., Salvia officinalis L. and Mentha spicata L. Extracts.

Plants are rich in bioactive phytochemicals that often display medicinal properties. These can play an important role in the production of health-promoting food additives and the replacement of artificial ones. In this sense, this study aimed to characterise the polyphenolic profile and bioactive properties of the decoctions, infusions and hydroethanolic extracts of three plants: lemon balm (Melissa officinalis L.), sage (Salvia officinalis L.) and spearmint (Mentha spicata L.). Total phenolic content ranged from 38.79 mg/g extract to 84.51 mg/g extract, depending on the extract. The main phenolic compound detected in all cases was rosmarinic acid. The results highlighted that some of these extracts may have the ability to prevent food spoilage (due to antibacterial and antifungal effects) and promote health benefits (due to anti-inflammatory and antioxidant capacities) while not displaying toxicity against healthy cells. Furthermore, although no anti-inflammatory capacity was observed from sage extracts, these stood out for often displaying the best outcomes in terms of other bioactivities. Overall, the results of our research provide insight into the potential of plant extracts as a source of active phytochemicals and as natural food additives. They also support the current trends in the food industry of replacing synthetic additives and developing foods with added beneficial health effects beyond basic nutrition.

Upcycling Quince Peel into Bioactive Ingredients and Fiber Concentrates through Multicomponent Extraction Processes.

This study aimed to promote the total upcycling of quince (Cydonia oblonga Mill.) peel into bioactive extracts (BEs) and fiber concentrates (FCs). The multicomponent extraction processes were optimized using response surface methodology (RSM) coupled with a 20-run experimental design, where the effects of time (1-120 min), temperature (25-95 °C), and EtOH percentage (0-100%) were combined. In addition to the extraction yields, BEs were analyzed for phenolic compounds, organic acids, and other water-soluble constituents, while FCs were characterized for their color and dietary fiber content. Statistically valid theoretical models were obtained by fitting these dependent variables to a quadratic equation and used to predict optimal extraction conditions. Those obtained for phenolic compounds and malic acid were experimentally validated, yielding 9.3 mg/g and 7.6 g/100 g of these bioactive constituents, respectively, and about 51% (w/w) FC. These BEs showed in vitro antioxidant activity and antimicrobial effects against foodborne fungi and bacteria, standing out in some aspects in relation to synthetic food additives, mainly the malic acid-enriched BE. Overall, the developed extraction processes allowed valorizing of quince peel in FCs and BEs that could be used as natural fortifiers or preservatives in the formulation of foods, beverages and dietary supplements.

Mirtazapine-induced Acute Pancreatitis in Patients With Depression: A Systematic Review.

OBJECTIVE: Antidepressant-induced pancreatitis is a rare, albeit serious, adverse effect, with a frequency of occurrence that is not equally distributed among antidepressant drugs. The goal of this study was to investigate the association and causal relationship between mirtazapine treatment of patients with depression and pancreatitis. METHODS: The study was designed as a systematic review of the literature, accompanied by the description of a new case of mirtazapine-associated acute pancreatitis. RESULTS: Nine cases of mirtazapine-associated pancreatitis have been reported, involving 7 female patients and 2 male patients with a mean age of 46.4 years (range: 26 to 83 y of age). All of the patients were hospitalized, with an average length of stay of 16.2 days (range: 3 to 34 d). In 6 cases, "de-challenge" followed by improvement was reported. The patients for whom the outcome was reported (7 of 9) recovered completely. CONCLUSION: Although a rare adverse effect, mirtazapine-induced pancreatitis should be considered when patients taking mirtazapine report abdominal discomfort.

Chemical Composition and Biological Activity of Commelina erecta: An Edible Wild Plant Consumed in Brazil.

In recent years, the interest in products of natural origin has boosted the exploitation and use of plants as food and sources of bioactive compounds, especially wild plants widely used in different cultures for several purposes. Commelina erecta is a wild edible plant (WEP) traditionally used as food and medicine, about which few studies exist. Thus, this study aimed at enhancing the knowledge about its nutritional, chemical and bioactive profile, considering different plant parts and development stages, in order to increase its inclusion in the diet of South American communities. The nutritional profile was found to be similar to other WEP frequently consumed in Brazil. Thirteen phenolic compounds (HPLC-DAD-ESI/MS) were tentatively identified, with apigenin, luteolin and quercetin derivatives being the most abundant. Fructose and oxalic acid were the major sugar and organic acid, respectively, in the aerial parts of C. erecta, and four isoforms of tocopherols were also identified. Regarding the plant's antioxidant activity, the EC50 values varied between 18.4 and 1060 µg/mL in the inhibition of lipid peroxidation assay (TBARS) and between 53 and 115 µg/mL in the oxidative haemolysis inhibition (OxHLIA) assay. The hydroethanolic extract obtained from stems at the flowering stage also presented anti-inflammatory activity. In general, all the extracts evidenced promising antimicrobial activity. Altogether, these results reinforce the traditional use of this plant species as food and medicine to support the diet of needier populations and also promote food sovereignty and sustainability.

A Comparative Study of Lactarius Mushrooms: Chemical Characterization, Antibacterial, Antibiofilm, Antioxidant and Cytotoxic Activity.

Mushrooms are valued worldwide for their nutritional, organoleptic and chemical properties. The aim of this study was to determine the chemical composition (free sugars, organic acids, fatty acids, tocopherols and phenolic compounds) and bioactivity of three wild mushrooms (Lactarius piperatus, Lactarius quietus and Lactarius vellereus) from Serbia. Chemical analysis was performed with HPLC-RI and UFLC-PDA (for hydrophilic compounds) and with GC-FID and HPLC-FP (for lipophilic compounds). The analysis of phenolic compounds was performed by UFLC-DAD. Biological activities were evaluated using three different assays (microdilution, TBARS and SRB assays). The results showed that the fruiting bodies were rich in mannitol and trehalose. The main organic acids were oxalic acid and citric acid. As for lipophilic components, stearic, oleic and linoleic acids and ß-tocopherol dominated in all the species studied. In addition, the methanolic and ethanolic extracts obtained showed antibacterial, antibiofilm and antioxidant properties. As for cytotoxicity, the extracts were not toxic or only moderately toxic toward different tumor cell lines. According to the results, the selected Serbian mushrooms are a rich source of bioactive compounds, and due to their good biological potential, they can be further exploited as functional ingredients beneficial to human health (antimicrobial agents, antioxidants).

N-Derivatives of (Z)-Methyl 3-(4-Oxo-2-thioxothiazolidin-5-ylidene)methyl)-1H-indole-2-carboxylates as Antimicrobial Agents-In Silico and In Vitro Evaluation.

Herein, we report the experimental evaluation of the antimicrobial activity of seventeen new (Z)-methyl 3-(4-oxo-2-thioxothiazolidin-5-ylidene)methyl)-1H-indole-2-carboxylate derivatives. All tested compounds exhibited antibacterial activity against eight Gram-positive and Gram-negative bacteria. Their activity exceeded those of ampicillin as well as streptomycin by 10-50 fold. The most sensitive bacterium was En. Cloacae, while E. coli was the most resistant one, followed by M. flavus. The most active compound appeared to be compound 8 with MIC at 0.004-0.03 mg/mL and MBC at 0.008-0.06 mg/mL. The antifungal activity of tested compounds was good to excellent with MIC in the range of 0.004-0.06 mg/mL, with compound 15 being the most potent. T. viride was the most sensitive fungal, while A. fumigatus was the most resistant one. Docking studies revealed that the inhibition of E. coli MurB is probably responsible for their antibacterial activity, while 14a-lanosterol demethylase of CYP51Ca is involved in the mechanism of antifungal activity. Furthermore, drug-likeness and ADMET profile prediction were performed. Finally, the cytotoxicity studies were performed for the most active compounds using MTT assay against normal MRC5 cells.

Synthesis and Antioxidant Properties of Organoselenium Compounds.

BACKGROUND: The chemistry of organoselenium reagents provides an asset for organic synthesis. The versatility of these reagents as electrophiles and nucleophiles makes them one of the key components of organic synthesis. Various synthetic transformations such as oxyselenenylations, selenocyclization and selenoxide elimination have been successfully achieved using organoselenium reagents under mild reaction conditions. The presence of selenocysteine in a few mammalian enzymes was the key information for selenium chemists to explore the biochemistry of selenium compounds. Glutathione peroxidase (GPx), a mammalian selenoenzyme, is well known for maintaining redox equilibrium by detoxifying reactive oxygen species. OBJECTIVE: The aim is to critically analyze the recent development and prospects of synthesis and antioxidant properties of organoselenium compounds. METHODS: In this review, we summarised research and review papers from the PubMed and Scopus databases. The primary themes were linked to the synthesis of organoselenium compounds and their capacity to maintain cellular redox equilibrium when exposed to oxidative stress. RESULTS: The study reveals that diselenide compounds synthesised by various methods showed a better antioxidant activity profile compared to selenides. In a few cases, the activity was found better than the standard compound ebselen. Moreover, the synthesis and antioxidant activity of Selenium-based nanoparticles have been also included. CONCLUSION: In the past two decades, various biological properties of organoselenium compounds have been extensively studied, including the antioxidant properties. This review article will give insight into the synthesis of different types of recently synthesised organoselenium compounds. The review would be helpful to the researchers working in the field of medicinal chemistry in directing the synthesis of new organoselenium compounds as antioxidants.

Chemical Profile and Skin-Beneficial Activities of the Petal Extracts of Paeonia tenuifolia L. from Serbia.

Without being aware of its chemical makeup, many ancient societies have used Steppe peony in their traditional medicine. Given that modern phytopreparation intended for use on human skin requires, above all, knowledge of its chemical composition, the goal of this study was to make a screening of the composition of aqueous and methanolic extracts of the petals of P. tenuifolia L. and to examine them for various skin-beneficial properties. The extracts were prepared by maceration, ultrasound-assisted, and microwave-assisted extraction procedures. The chemical profiling was conducted by the use of UHPLC-LTQ-OrbiTrap MS and UHPLC/MS, and spectrophotometric methods for the determination of total polyphenol and total flavonoid contents. The biological activities entailed antioxidant ABTS, DPPH, CUPRAC (Cupric Ion Reducing Antioxidant Capacity), and FRAP (Ferric Reducing Antioxidant Power) assays, antimicrobial (antibacterial and antifungal) and antibiofilm activities, cytotoxicity, wound healing potential, as well as the adhesion and invasion of Staphylococcus lugdunensis. The results showed that the petals are rich in phenolic acids and flavonoids, which are commonly associated with numerous biological activities. The aqueous extracts were more efficient in the majority of the bioactivity assays then the methanolic ones, whereas the optimal extraction method varied between the assays. This study is the first step towards the safe use of the aqueous extracts of P. tenuifolia petals for therapeutic skin treatments.

Resource Use and Costs Related to Hematological Complications of Chemotherapy: Cost of Illness Study Based on Data from Balkan Country with Recent History of Socioeconomic Transition.

Background: The administration of chemotherapy positively correlates with diverse adverse drug reactions, including the significant impact of hematological hazards such as anemia, leukopenia-neutropenia, thrombocytopenia, and pancytopenia. This pilot pharmacoeconomic study aimed to estimate the total direct costs of treating hematological toxicity induced by chemotherapy and its main determinants. Methods: The study was conducted as a retrospective cost of illness study using the "from bottom to the top" approach from the perspective of the Republic Health Insurance Fund. This study included 88 patients treated due to developing at least one episode of one of the types of hematological complications of cytostatics in 2018 at the Oncology Clinic of the University Clinical Center Kragujevac, Kragujevac, the Republic of Serbia. Results: Among cancer patients who developed haematological toxicity, treating pancytopenia was most demanding in a pharmacoeconomic manner compared to neutropenia and thrombocytopenia, with an estimated value of direct costs of 264,14, 178,19 and 157,76 euros per patient per year respectively. Regarding total direct costs, the main determinants were the costs of drugs, their parenteral administration, and costs due to hospitalization. Conclusion: Due to the rising cancer incidence and obligatory hospital treatment of hematological toxicity induced by chemotherapy, the identification of the pharmacoeconomic aspects of the treatment of these complications is needed. Future research should focus on the development of new modalities of treatment regarding patient characteristics anticipating high costs.

Analysis of Tonsil Tissues from Patients Diagnosed with Chronic Tonsillitis-Microbiological Profile, Biofilm-Forming Capacity and Histology.

Chronic tonsillitis (CT) is a global health issue which can impair patient's quality of life and has an important socioeconomic impact due to the nonrational use of antibiotics, increased antimicrobial resistance and frequent need for surgical treatment. In order to isolate and identify the causing agents of CT, a total of 79 postoperative palatine and adenoid tissue samples were obtained from the ENT Clinic, KBC Zvezdara, Belgrade, Serbia. Culture identification was performed by MALDI-TOF MS and the Staphylococcus aureus isolates were tested for biofilm forming capability and antibiotic susceptibility. Additionally, a histological examination of palatine and adenoid tissue was performed in order to detect the presence of CT-causing bacteria. The slight majority of participants were females with median age of 28 years for adult patients (group I) and 6 years for children (group II). Analysis of the incidence of bacteria isolated from tissue samples in both groups showed the highest prevalence of S. aureus, Streptococcus oralis and Streptococcus parasanquinis. In addition to interfollicular hyperplasia, colonies of species S. aureus were detected in histological material. The presence of biofilm might be the reason for the recurrence of infection. Therefore, searching for a new treatment of CT is of great importance.

VALIDATION OF THE BRIEF INTERNATIONAL COGNITIVE ASSESSMENT FOR MULTIPLE SCLEROSIS (BICAMS) IN A LARGE COHORT OF RELAPSING-REMITTING MS PATIENTS.

Cognitive impairment is one of the most frequently reported symptoms in persons with multiple sclerosis (MS). The Brief International Cognitive Assessment for Multiple Sclerosis (BICAMS) has been recommended as a standardized international screening and monitoring tool for brief cognitive assessment. The aim of our study was to assess the reliability and validity of the Serbian version of the BICAMS. A total of 500 relapsing-remitting MS (RRMS) patients and 69 age-, gender- and education-matched healthy control (HC) subjects were examined. All participants performed the BICAMS test battery, which includes the oral version of the Symbol Digit Modalities Test (SDMT), California Verbal Learning Test second edition (CVLT-II), and Brief Visuospatial Memory Test Revised (BVMTR). A randomly selected subset of patients were retested one to three weeks after baseline. Statistically significant differences between patients and HCs were evident on the SDMT and BVMTR (p<0.001). HCs had higher CVLT-II scores but this difference did not reach statistical significance (p=0.063). Cognitive impairment, defined as an abnormal test score on ≥1 subtest, was found in 62.9% of MS patients. There were statistically significant correlations between BICAMS scores and age, education, EDSS and disease duration in patient sample. Test-retest reliability was confirmed with Pearson correlation coefficient of 0.70 in all measures. This study supported the reliability and validity of the Serbian BICAMS, although the CVLT-II version tested here lacked sensitivity to detect MS compared to healthy volunteers.

Comparative study on the phenolic composition and in vitro bioactivity of medicinal and aromatic plants from the Lamiaceae family.

Medicinal and aromatic plants (MAP) have been described as a source of phenolic compounds with potential as antioxidant, antiproliferative and antimicrobial agents. MAP from the Lamiaceae family (Origanum vulgare L., Thymus vulgaris L., Ocimum basilicum L., Salvia officinalis L., Melissa officinalis L., and MatricariachamomillaL.) were selected to perform a phytochemical and biological screening for their further exploitation as natural bioactive ingredients. The total content of phenolic compounds varied from 184.02 mg/g extract in M. officinalis to 17.97 mg/g extract in M. chamomilla. Caffeic and rosmarinic acids were the main phenolic acids found in the respective hydroalcoholic extracts. The extracts showed a promising antioxidant activity in vitro, being related the phenolic compositions of the extracts, furthermore, all extracts being able to combat lipid peroxidation in TBARS assays with an IC50 under 26 µg/mL, moreover all the plant extract has prevented the oxidative haemolysis in OxHLIA assays at concentrations below 67 µg/mL in a Δt 60 min and under 118 µg/mL for a Δt 120 min. Regarding to the bactericidal and fungicidal action the plant extracts were able to inhibit growth against bacteria associated with food hazards, such as Salmonella typhimurium (MIC < 1) and Listeria monocytogenes (MIC < 1), regarding to fungicidal activity it can be highlighted the MIC values under to 0.25 for Aspergillus versicolor and Trichoderma viride. Overall, the selected Lamiaceae plants stood out as a source of active phytochemicals that can be used by different industries, such as food and cosmetics.

Hesperetin-Between the Ability to Diminish Mono- and Polymicrobial Biofilms and Toxicity.

Hesperetin is the aglycone of citrus flavonoid hesperidin. Due to the limited information regarding hesperetin antimicrobial potential and emerging need for novel antimicrobials, we have studied its antimicrobial activity (microdilution assay), antibiofilm activity with different assays in two models (mono- and polymicrobial biofilm), and toxicity (MTT and brine shrimp lethality assays). Hesperetin inhibited growth of all Candida isolates (minimal inhibitory concentration, MIC, 0.165 mg/mL), while it's inhibitory potential towards Staphylococcus aureus was lower (MIC 4 mg/mL). Hesperetin (0.165 mg/mL) reduced ability of Candida to form biofilms and moderately reduced exopolysaccharide levels in biofilm matrix. Effect on the eradication of 24 h old C. albicans biofilms was promising at 1.320 mg/mL. Inhibition of staphylococcal biofilm formation required higher concentrations of hesperetin (<50% inhibition with MIC 4 mg/mL). Establishment of polymicrobial C. albicans-S. aureus biofilm was significantly inhibited with the lowest examined hesperetin concentration (1 mg/mL) in crystal violet and CFU assays. Hesperetin toxicity was examined towards MRC-5 fibroblasts (IC50 0.340 mg/mL) and in brine shrimp lethality assay (LC50 > 1 mg/mL). Hesperetin is efficient in combating growth and biofilm formation of Candida species. However, its antibacterial application should be further examined due to the cytotoxic effects provoked in the antibacterial concentrations.

Phenolic Composition and Antioxidant, Anti-Inflammatory, Cytotoxic, and Antimicrobial Activities of Cardoon Blades at Different Growth Stages.

Cardoon (Cynara cardunculus var. altilis) blades were collected at sixteen sampling dates (B1-B16) to study the influence of the phenological growth stage on the phenolic composition and biological properties. Twenty phenolic compounds were identified, among which trans 3,4-O-dicaffeoylquinic acid, 5-O-caffeoylquinic acid, and luteolin-O-hexoside (39.6, 42.6, and 101.0 mg/g extract, respectively) were the main compounds. Immature blades (B3) had a higher content of phenolic compounds (178 mg/g extract) and a greater ability to inhibit the formation of thiobarbituric acid reactive substances (IC50 of 1.61 µg/mL). Samples at more advanced growth stages revealed a greater capacity to inhibit oxidative hemolysis (B8, IC50 of 25 and 47.4 µg/mL for Δt of 60 and 120 min, respectively) and higher cytotoxic (B8-B13, GI50 between 7.1 and 17 µg/mL), anti-inflammatory (B13, IC50 of 10 µg/mL), and antibacterial activities. In turn, the antifungal activity varied depending on the tested fungi. All these results suggest that maturity influences the phenolic composition and bioactive properties of cardoon blades, which reveal great potential for the development of bioactive ingredients for food and pharmaceutical applications, among others.

Thiazolidin-4-Ones as Potential Antimicrobial Agents: Experimental and In Silico Evaluation.

Herein, we report computational and experimental evaluations of the antimicrobial activity of twenty one 2,3-diaryl-thiazolidin-4-ones. All synthesized compounds exhibited an antibacterial activity against six Gram-positive and Gram-negative bacteria to different extents. Thus, the MIC was in the range of 0.008-0.24 mg/mL, while the MBC was 0.0016-0.48 mg/mL. The most sensitive bacterium was S. Typhimurium, whereas S. aureus was the most resistant. The best antibacterial activity was observed for compound 5 (MIC at 0.008-0.06 mg/mL). The three most active compounds 5, 8, and 15, as well as compound 6, which were evaluated against three resistant strains, MRSA, P. aeruginosa, and E. coli, were more potent against all bacterial strains used than ampicillin. The antifungal activity of some compounds exceeded or were equipotent with those of the reference antifungal agents bifonazole and ketoconazole. The best activity was expressed by compound 5. All compounds exhibited moderate to good drug-likeness scores ranging from -0.39 to 0.39. The docking studies indicated a probable involvement of E. coli Mur B inhibition in the antibacterial action, while CYP51 inhibition is likely responsible for the antifungal activity of the tested compounds. Finally, the assessment of cellular cytotoxicity of the compounds in normal human MRC-5 cells revealed that the compounds were not toxic.