Current Perspectives on Biological Screening of Newly Synthetised Sulfanilamide Schiff Bases as Promising Antibacterial and Antibiofilm Agents.

Growing resistance to antimicrobials, combined with pathogens that form biofilms, presents significant challenges in healthcare. Modifying current antimicrobial agents is an economical approach to developing novel molecules that could exhibit biological activity. Thus, five sulfanilamide Schiff bases were synthesized under microwave irradiation and characterized spectroscopically and in silico. They were evaluated for their antimicrobial and antibiofilm activities against both Gram-positive and Gram-negative bacterial strains. Their cytotoxic potential against two cancer cell lines was also determined. Gram-positive bacteria were susceptible to the action of these compounds. Derivatives 1b and 1d inhibited S. aureus's growth (MIC from 0.014 mg/mL) and biofilm (IC from 0.029 mg/mL), while compound 1e was active against E. faecalis's planktonic and sessile forms. Two compounds significantly reduced cell viability at 5 µg/mL after 24 h of exposure (1d-HT-29 colorectal adenocarcinoma cells, 1c-LN229 glioblastoma cells). A docking study revealed the increased binding affinities of these derivatives compared to sulfanilamide. Hence, these Schiff bases exhibited higher activity compared to their parent drug, with halogen groups playing a crucial role in both their antimicrobial and cytotoxic effects.

Antioxidant Activity of Essential Oils from Pinaceae Species.

With a widespread distribution throughout the Northern Hemisphere and 11 genera, Pinaceae is the largest family of Gymnosperms in the world. Essential oils are an important chemotaxonomic marker for the species of this family, although the degree of chemical and biological investigation has not been the same for all genera. Essential oils from Abies and Cedrus (from the abietoid clade) or Pinus and Picea (from the pinoid clade) have been more extensively investigated with respect to their chemical composition and biological or pharmacological properties, including their antioxidant effects. Instead, essential oils from the other genera of the family have been less explored in this respect or even have not been investigated at all. This is a narrative review looking into the knowledge acquired up to date, the variability and limitations of the current methods used to estimate antioxidant effects, and multiple comparisons between EOs obtained from different genera, species, and plant parts, as well as potential applications and future directions of research and utilization of essential oils derived from Pinaceae species.

Safety of Innovative Nanotechnology Oral Formulations Loaded with Bioactive Menopause Molecules: Influence of Genotoxicity and Biochemical Parameters on a Menopausal Rat Model.

In recent years, nanoparticles have gained significant importance due to their unique properties, such as pharmacological, electrical, optical, and magnetic abilities, contributing to the growth of the science and technology sector. Particular naturally derived biomolecules with beneficial effects on menopause disorder have been the subject of studies of pharmaceutical formulation to obtain alternative pharmaceutical forms with increased bioavailability and without side effects, as in nanostructured lipid carriers (NLCs) loaded with such active ingredients. In the present study, one stage of a broader project, we have performed pharmacotoxicology studies for six combinatory innovative nanocapsule pharmaceutical forms containing active natural biomolecules before considering them as oral formulas for (1) in vitro toxicity studies on culture cells and (2) in vivo preclinical studies on a surgically induced menopause model of Wistar female rats, and the influence of the NLCs on key biochemical parameters: lipid profile (TG, Chol, HDL), glycemic markers (Gli), bone markers (Pac, Palc, Ca, phosphorus), renal markers (Crea, urea, URAC), inflammation (TNF), oxidative stress (GSH, MDA), and estrogen-progesterone hormonal profile. The micronucleus test did not reveal the genotoxicity of the tested compounds; the menopause model showed no significant safety concerns for the six tested formulas evaluated using the blood biochemical parameters; and the results showed the potential hypoglycemic, hypolipidemic, hypouricemic, and antioxidant potential of one of the tested formulas containing nano diosgenin and glycyrrhizic acid.

Determination of Phosphodiesterase Type-5 Inhibitors (PDE-5) in Dietary Supplements.

This study proposed a high-performance thin-layer chromatography (HPTLC) screening method to detect phosphodiesterase 5 (PDE-5) inhibitors as possible adulterant agents in various dietary supplements. Chromatographic analysis was performed on silica gel 60F254 plates using a mixture of ethyl acetate:toluene:methanol:ammonia in a volume ratio of 50:30:20:0.5 as a mobile phase. The system provided compact spots and symmetrical peaks of sildenafil and tadalafil with retardation factor values of 0.55 and 0.90, respectively. The analysis of products purchased from the internet or specialized stores demonstrated the presence of sildenafil, tadalafil, or both compounds in 73.3% of products, highlighting inadequacies and inconsistencies in the labeling, as all dietary supplements were declared to be natural. The results were confirmed using ultra-high-performance liquid chromatography coupled with a positive electrospray ionization high-resolution tandem mass spectrometry (UHPLC-HRMS-MS) method. Furthermore, in some samples, vardenafil and various analogs of PDE-5 inhibitors were detected using a non-target HRMS-MS approach. The results of the quantitative analysis revealed similar findings between the two methods, with adulterant quantities found to be similar to or higher than those in approved medicinal products. This study demonstrated that the HPTLC method is a suitable and economical method for screening PDE-5 inhibitors as adulterants in dietary supplements intended for sexual activity enhancement.

GC-MS Analysis of Methadone and EDDP in Addicted Patients under Methadone Substitution Treatment: Comparison of Urine and Plasma as Biological Samples.

(1) Background: Methadone, along with buprenorphine, is the most commonly used drug for the treatment of opioid dependence. This study aimed to analyze methadone and its major metabolite, 2-ethylidene-1,5-dimethyl-3,3-diphenyl pyrrolidine (EDDP), in the urine and plasma of opiate addicts. The study group consisted of drug users voluntarily admitted to the detoxification center C.E.T.T.T. "St. Stelian" of Bucharest. Secondly, the study aimed to identify whether urine or plasma provides better results for the proposed method. (2) Methods: A GC-MS method, using an internal standard (diphenylamine) in the FULL-SCAN and SIM modes of operation and using the m/z = 72 ion for methadone and the m/z = 277 ion for EDDP, combined with a liquid-liquid extraction procedure was performed. (3) Results: The applied procedure allows the detection and quantification of methadone in both urine and plasma samples. EDDP was identified in patients with higher levels of methadone. Higher levels of methadone were detected in urine than in plasma samples. (4) Conclusions: This procedure can be used in clinical laboratories for the rapid determination of methadone levels in urine rather than in plasma. The procedure can be applied for the monitoring of methadone substitution treatment.

Attention deficit among preschool and school-aged children living near former metal-processing plants in Romania.

Industrial areas affected by high and long-term heavy metal pollution have a great impact on health of the resident population. Children represent a group at high-risk with an increased susceptibility to chronic heavy metal intoxication. Our work included the assessment of attention particularities through a case-control study in pre-school and school-aged children (4-6 years and 8-11 years) from two study areas, Copsa Mica and Zlatna, compared to a non-polluted locality with no history of heavy metal pollution. Copsa Mica and Zlatna are two of the most polluted heavy metals regions in Romania due to non-ferrous metallurgy for a long period of time. Recruitment of participants was made by a random selection of an entire class for each age within the schools and kindergartens from the study areas (Copsa Mica and Zlatna) and from the non-polluted region. Interpretation of data was performed using statistical analysis (ANOVA and Student's t-test). Preschool children (4-6 years) were tested using Wechsler Preschool and Primary Scale of Intelligence (WPPSI) tests, Animal House and labyrinth samples. The results of the attention tests applied to pre-school children were lower in the study areas compared to the control group, but no statistical differences were found. The results of the attention tests applied to children aged between 8 and 11 years (Toulouse-Pieron test and Traffic light test) indicate lower average scores within the study groups from polluted areas, compared to the control group. Differences with statistically significance were registered for the 8 years age group (p = 0.037). In these areas efficient strategies and precise intervention measures are needed in order to limit or remove the heavy metal exposure and protect the human health, especially the groups exposed to a high level of risk.

Environmental metal contamination and health impact assessment in two industrial regions of Romania.

We investigated two Romanian industrial regions- Copsa Mica and Zlatna, to assess the current situation of soil pollution and bioaccumulation of Pb, Cd, Cu and Zn in different vegetable species and possible risks to consumers. Both total and mobile forms of the metals were determined in soil samples, and metal content in the edible parts of root vegetable samples was also assessed. The concentrations of Pb and Zn in soil were higher in Copsa Mica than in Zlatna (566mg/kg vs 271mg/kg for Pb and 1143mg/kg vs 368mg/kg for Zn)·The metal mobility in soil from Copsa Mica decreases in the order Zn>Cu>Cd>Pb (1.88mg/kg, 0.40mg/kg, 0.22mg/kg, 0.16mg/kg, respectively), while in Zlatna, the order was Cu>Zn>Pb>Cd (0.88mg/kg, 0.29mg/kg, 0.04mg/kg, 0.01mg/kg, respectively), apparently depending on metal and soil conditions. In Copsa Mica, the amount of Pb and Cd in vegetable samples exceeded the maximum permissible limits in carrots (median concentration 0.32mg/kg for Pb and Cd) and in yellow onions (median concentration 0.24mg/kg for Cd). In Zlatna region, the content of Cd exceeded the maximum limits in yellow onions (median concentration 0.11mg/kg). The amount of Pb was higher than the maximum acceptable level in carrots from the Zlatna region (median concentration 0.12mg/kg). Cu and Zn levels were within the normal range in all vegetable samples. In the Zlatna region, the transfer factors for Pb and Cd were higher in carrots (median values of 9.9 for Pb and 21.0 for Cd) compared to carrots harvested in Copsa Mica (median values of 4.0 for Pb and 2.0 for Cd). Daily intake rates of metals through local vegetable consumption exceeded the limit values established by the European Food Safety Authority for Pb (1.2 to 2.4 times) and Cd (5.5 to 9.1 times) in both regions, with potential adverse health effects for the local population. The results highlight the need for total soil remediation action before fruit and vegetables produced in these polluted areas can be safely consumed.

Investigation of the toxicity of some organophosphorus pesticides in a repeated dose study in rats.

The study aimed to the investigation of the toxicity of organophosphorus pesticides malathion (MLT) and diazinon (DZN) in Wistar rats in a repeated dose study for 35 days. MLT and DZN in corn oil vehicle were oral administered. Body and organs weights, plasma and brain cholinesterase activities, serum aspartate aminotransferase (AST) and alanine aminotransferase (ALT) activities, histopathological changes in liver and kidney, and some parameters of the immune function, such as leukocyte formula, spleen weight and cellularity, spleen lymphocytes proliferation in response to concanavalin A (Con A) were investigated; the potential oxidative stress (malondialdehyde in plasma and brain, and blood catalase activity) was also evaluated. No clinical toxicity signs attributed to pesticides were noted; no significant changes in the organ weights have been found. Body weight tends slightly to increase, predominantly in DZN treated rats. The results suggest that plasma cholinesterase is more susceptible than brain cholinesterase to the inhibitory effect of DZN and MLT. Other serum biochemical parameters showed no significant difference. DZN produced a marked increase of the number of spleen lymphocytes without a significant gain of the relative spleen weight. The both pesticides produced an increase of the number of mononuclear cells÷weight spleen. The splenic lymphocyte proliferation has not been influenced by MLT or DZN treatment. Histopathological observations identified some changes (vasodilatation, microvacuoles, and granular dystrophy) in the liver, with MLT, inducing macrovacuolar steatosis. The study indicates that repeated exposure, at subclinical doses, to organophosphorus MLT and DZN causes some biochemical, histopathological and immune alterations in rats.

[Semi-quantitative determination of methadone by TLC]. / Evaluarea semicantitativa a metadonei prin metoda cromatografiei în strat subtire (CSS).

UNLABELLED: Methadone is the main therapeutic option in heroin addiction treatment, but also an abuse substance. Given the analytical focus on the diagnosis of drug abuse and the usefulness of toxicological analysis methods in both overdose and monitoring substitution therapy, this study was aimed at the semi-quantitative determination of methadone by using Thin Layer Chromatography (TLC). By having the advantage of simplicity and rapidity, TLC finds its rightful place among the analysis methods when other relatively costly methods that involve instrumental performance are not available. MATERIALS AND METHODS: TLC plates (silicagel GF 254 Merck), developing system methanol: strong ammonia 100: 1,5, photometric quantification at 254 nm, using TLC Scanner 3 (Camag). RESULTS: The results show that methadone can be determined semi-quantitatively in the chromatographic conditions mentioned in the two domains tested (5 - 40 microg and 10 - 80 microg), with the best results obtained in the 5 - 40 microg domain. CONCLUSIONS: Semi-quantitative TLC evaluation proposed by us has as main advantages the rapidity, simplicity and relatively low cost compared to other useful methods.