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1.
Molecules ; 29(7)2024 Mar 27.
Article in English | MEDLINE | ID: mdl-38611776

ABSTRACT

The aim of this case study was the evaluation of the selected metals' concentration, potential toxic compound identification, cytotoxicity analysis, estimation of the airborne dust concentration, biodiversity, and number of microorganisms in the environment (leachate, soil, air) of the biggest uncontrolled post-industrial landfills in Poland. Based on the results obtained, preliminary solutions for the future management of post-industrial objects that have become an uncontrolled landfill were indicated. In the air, the PM1 fraction dominated, constituting 78.1-98.2% of the particulate matter. Bacterial counts were in the ranges of 9.33 × 101-3.21 × 103 CFU m-3 (air), 1.87 × 105-2.30 × 106 CFU mL-1 (leachates), and 8.33 × 104-2.69 × 106 CFU g-1 (soil). In the air, the predominant bacteria were Cellulosimicrobium and Stenotrophomonas. The predominant fungi were Mycosphaerella, Cladosporium, and Chalastospora. The main bacteria in the leachates and soils were Acinetobacter, Mortierella, Proteiniclasticum, Caloramator, and Shewanella. The main fungi in the leachates and soils were Lindtneria. Elevated concentrations of Pb, Zn, and Hg were detected. The soil showed the most pronounced cytotoxic potential, with rates of 36.55%, 63.08%, and 100% for the A-549, Caco-2, and A-549 cell lines. Nine compounds were identified which may be responsible for this cytotoxic effect, including 2,4,8-trimethylquinoline, benzo(f)quinoline, and 1-(m-tolyl)isoquinoline. The microbiome included bacteria and fungi potentially metabolizing toxic compounds and pathogenic species.


Subject(s)
Dust , Mercury , Humans , Caco-2 Cells , Metals , Soil
2.
Environ Res ; 228: 115825, 2023 07 01.
Article in English | MEDLINE | ID: mdl-37011789

ABSTRACT

This study focused on assessing the microbiological and chemical contamination of air, soil and leachate in uncontrolled refuse storage areas in central Poland. The research included an analysis of the number of microorganisms (culture method), endotoxin concentration (gas chromatography-mass spectrometry), heavy metals level (atomic absorption spectrometry), elemental characteristics (elemental analyser), cytotoxicity assessment against A-549 (human lung) and Caco-2 (human colon adenocarcinoma) cell lines (PrestoBlue™ test) and toxic compound identification (ultra-high-performance liquid chromatography-quadrupole time-of-flight ultrahigh-resolution mass spectrometry). Microbial contamination differed depending on the dump and the group of tested microorganisms. The number of bacteria was: 4.3 × 102 - 1.8 × 103 CFU m-3 (air); 1.1 × 103 - 1.2 × 106 CFU mL-1 (leachate); 1.0 × 106 - 3.9 × 106 CFU g-1 (soil). Respectively, for air and soil the number of fungi was: 2.2 × 102 - 4.6 × 102 CFU m-3; 1.8 × 102 - 3.9 × 103 CFU g-1. Metal levels (Fe, Mn, Pb, Zn, Al, Hg, Cd, Cu, Cr) were higher than in the control sample; however, the average concentrations did not exceed the permissible standards. The cytotoxicity of soil and leachate samples depended on the dump, sample and cell line tested. The leachates were more cytotoxic than soil extracts. Compounds belonging to pesticides, surfactants and biocides, chemicals and/or polymer degradation products, medicinal drugs and insect repellents were found. The detection of potential pathogens in the air, soil and leachate, the presence of toxic compounds and the confirmation of the cytotoxic effect of leachate and soil on human cell lines justify the need for further research on the risks posed by illegal dumps. These studies should aim at developing a unified assessment method and a method to minimise the risk of contaminants spreading in the environment, including harmful biological agents.


Subject(s)
Adenocarcinoma , Colonic Neoplasms , Metals, Heavy , Soil Pollutants , Humans , Poland , Caco-2 Cells , Soil Pollutants/toxicity , Soil Pollutants/analysis , Environmental Monitoring/methods , Metals, Heavy/toxicity , Metals, Heavy/analysis , Soil/chemistry , Risk Assessment
3.
Pharmaceuticals (Basel) ; 14(3)2021 Feb 26.
Article in English | MEDLINE | ID: mdl-33652916

ABSTRACT

Cyclophosphamide (CPX) exerts toxicity in the urogenital system. The current study was designed to evaluate the effect of morin-5'-sulfonic acid sodium salt (NaMSA) on CPX-induced urogenital toxicity in rats. NaMSA (100 mg/kg/daily) and CPX (15 mg/kg/daily) alone or in combination and 0.9% NaCl (as a control) were given intragastrically for 10 days. Testes and epididymes from male and urinary bladders from male and female rats were evaluated histologically. In testes and epididymes, morphological changes and relative decrease in sperm count were assessed. In urinary bladders edema, hemorrhage and urothelium erosions were described by 0-2 points scoring system. Reproductive score (RS-in total 6 points) and urinary bladder score (BS-in total 6 points) were thereafter calculated. In CPX-receiving group RS (2.7) and BS (3.3) were significantly higher than in the control (0.5 and 0.25 for RS and BS, respectively). Co-administration of NaMSA reversed most of the morphological changes, which was reflected by lower RS and BS score (0.5 and 1.2 for RS and BS, respectively). The preliminary findings suggest that NaMSA may attenuate CPX-induced histological changes in rat urogenital tract.

4.
Bioorg Chem ; 94: 103426, 2020 01.
Article in English | MEDLINE | ID: mdl-31784064

ABSTRACT

In the present study, we compared the anticancer potential of quercetin (3,3',4',5,7-pentahydroxyflavone, I) and its sulfonic derivatives sodium/potassium quercetin-5'-sulfonates (described as II and III) against several human carcinoma cell lines. Quercetin (I) was used as a starting compound for synthesis of II and III. In this work, a modified and more efficient method of synthesizing derivatives II and III has been described. The molecular structures of the compounds were characterized in a solution and in the solid state using 1H NMR, 13C NMR, 2D NMR, and XPS spectroscopy, respectively. The stoichiometry of these complexes was determined by elemental analysis as well as thermogravimetric and X-ray fluorescence methods. The spectral data allowed complete characterization of the investigated compounds in the solution and in the solid state and unambiguous determination of the place of substitution of the sulfonic group in the phenyl ring in the C-5' position. Our in vitro studies revealed that II and III prominently reduced the viability of the HT-29 colon cancer cell line. Additionally, we observed that sulfonic derivatives decreased proliferation of colon (HT-29, LS180), lung (A549), and breast (T47D) cancer cell lines. Moreover, we detected a lower cytotoxic effect of II and III on several normal cell lines (colon epithelial CCD 841 CoTr, mouse subcutaneous connective tissue L-929, and human skin fibroblasts HSF cell lines) than that exerted by pure quercetin. The anticancer properties were especially evident in the HT-29 colon cancer cell line, where cell cycle inhibition in the G2-M phase and prominent apoptosis induced by II and III were observed. In conclusion, the sodium/potassium quercetin-5'-sulfonates prepared from quercetin showed promising anti-proliferative and pro-apoptotic activity against colon cancer cells. Therefore, we support the opinion that sodium/potassium quercetin-5'-sulfonates should be considered as promising organometallic compounds for possible clinical applications.


Subject(s)
Adenocarcinoma/drug therapy , Antineoplastic Agents/therapeutic use , Potassium/therapeutic use , Quercetin/therapeutic use , Sodium/therapeutic use , Antineoplastic Agents/pharmacology , Apoptosis , Cell Cycle Checkpoints , Cell Line, Tumor , Cell Proliferation , HT29 Cells , Humans , Molecular Structure , Potassium/pharmacology , Quercetin/pharmacology , Sodium/pharmacology
5.
Pharmacol Rep ; 67(6): 1259-63, 2015 Dec.
Article in English | MEDLINE | ID: mdl-26481550

ABSTRACT

BACKGROUND: The aim of this study was to evaluate the effect of morin-5'-sulfonic acid sodium salt (NaMSA) on cyclophosphamide-induced gastrointestinal changes in rats. METHODS: Rats received intragastrically 0.9% saline (group C), cyclophosphamide (15 mg/kg) (group CX), NaMSA (100 mg/kg) (group M) or cyclophosphamide (15 mg/kg) with NaMSA (100 mg/kg) (group M-CX), respectively, for 10 days. RESULTS: No histological lesions were observed in the liver and the large intestine in the control group and group receiving NaMSA. In the cyclophosphamide-treated group, a generalized blurred trabecular structure, hepatocyte apoptosis, focal and diffuse necrosis were noticed in the liver and atypia of epithelial cells or adenoma were noticed in the large intestine. In the group receiving both cyclophosphamide and NaMSA, hepatocyte apoptosis in the liver was observed less frequently. Histological examination of the small intestine revealed: low-grade dysplasia adenoma in the C, M, CX and M-CX group (in 44%, 0%, 100%, and 55.6% of specimens, respectively) with adenocarcinoma in 55.6% of specimens in the cyclophosphamide-receiving group only. Adenoma with high-grade dysplasia was observed in the control and NaMSA-receiving group with a similar frequency (22%). In addition to the histological evaluation, blood cell count parameters, as well as total protein concentration, blood glucose level, amylase, ALT, AST and GGTP activities were evaluated. Cyclophosphamide impaired weight gain, decreased blood cell count parameters and total protein concentration, and increased the GGTP activity. Those changes were not reversed by NaMSA. CONCLUSIONS: Summing up, NaMSA may protect against some cyclophosphamide-induced histological abnormalities in the gastrointestinal tract, including intestinal neoplasia in rats.


Subject(s)
Cyclophosphamide/adverse effects , Flavonoids/pharmacology , Gastrointestinal Diseases/chemically induced , Gastrointestinal Diseases/prevention & control , Intestine, Large/drug effects , Sulfonic Acids/pharmacology , Adenoma/chemically induced , Adenoma/drug therapy , Animals , Apoptosis/drug effects , Blood Cell Count , Body Weight/drug effects , Female , Flavonoids/therapeutic use , Gastrointestinal Diseases/drug therapy , Gastrointestinal Diseases/pathology , Hepatocytes/drug effects , Hepatocytes/pathology , Intestine, Large/pathology , Liver/drug effects , Liver/pathology , Male , Necrosis/drug therapy , Necrosis/pathology , Rats , Sulfonic Acids/therapeutic use , gamma-Glutamyltransferase/blood
6.
Acta Pol Pharm ; 70(3): 567-71, 2013.
Article in English | MEDLINE | ID: mdl-23757948

ABSTRACT

The antibacterial activity of quercetin, morin, sodium salt of quercetin-5'-sulfonic acid (NaQSA) and sodium salt of morin-5'-sulfonic acid (NaMSA) were tested against six bacterial strains: Escherichia coli (ATCC 25922 and clinical isolates--ESBL), Pseudomonas aeruginosa (ATCC 27853 and clinical isolates--carbapenem resistant), Staphylococcus aureus (ATCC 29213 and clinical isolats- MRSA). The most effective inhibitors against the model strain S. aureus are NaQSA and NaMSA (MIC = 3.9 microg/mL). Among polyhydroxyflavones used in this investigation, morin exhibits the highest antibacterial activity against tested strains. The structure-activity relationship indicates that 2',4'-dihydroxylation of the B ring in the flavanone structure is important for significant antibacterial activity and that substitution of the sulfo group at position 5' on the lateral phenyl ring enhances antistaphylococcal activity of flavonoids.


Subject(s)
Anti-Bacterial Agents/pharmacology , Flavonoids/pharmacology , Quercetin/analogs & derivatives , Sulfonic Acids/pharmacology , Anti-Bacterial Agents/chemistry , Flavonoids/chemistry , Quercetin/pharmacology , Structure-Activity Relationship
7.
Pharmacol Rep ; 65(1): 201-7, 2013.
Article in English | MEDLINE | ID: mdl-23563039

ABSTRACT

BACKGROUND: The aim of the study was to evaluate the effect of cyclophosphamide (CPX) and morin-5'-sulfonic acid sodium salt (NaMSA) on plasma asymmetric dimethylarginine (ADMA) level and dimethylarginine dimethylaminohydrolase (DDAH) activity in rat liver. METHODS: The study was performed on Wistar rats receiving normal saline, CPX (15 mg/kg/day), NaMSA (100 mg/kg/day) or both CPX and NaMSA for 10 consecutive days. RESULTS: Significant decrease in ADMA level was found in all groups when compared to the control. DDAH activity in the liver was significantly higher in CX group compared to the control group. CONCLUSION: Obtained results of ADMA/DDAH pathway parameters require further research.


Subject(s)
Amidohydrolases/metabolism , Arginine/analogs & derivatives , Cyclophosphamide/pharmacology , Flavonoids/pharmacology , Sulfonic Acids/pharmacology , Animals , Antioxidants/administration & dosage , Antioxidants/pharmacology , Arginine/blood , Arginine/metabolism , Cyclophosphamide/administration & dosage , Drug Therapy, Combination , Female , Flavonoids/administration & dosage , Immunosuppressive Agents/administration & dosage , Immunosuppressive Agents/pharmacology , Liver/drug effects , Liver/metabolism , Male , Rats , Rats, Wistar , Sulfonic Acids/administration & dosage
8.
Adv Clin Exp Med ; 21(4): 423-31, 2012.
Article in English | MEDLINE | ID: mdl-23240447

ABSTRACT

BACKGROUND: Quercetin-5'-sulfonic acid sodium salt (NaQSA) exerts good aqueous solubility, strong antioxidant activity and low toxicity. OBJECTIVES: The aims of this study were to investigate the effect of NaQSA on superoxide dismutase (SOD) activity and ADMA/DDAH pathway during extracorporeal liver perfusion (ELP). MATERIAL AND METHODS: The study was carried out on male Wistar rats. Isolated livers were perfused with Krebs-Henseleit bicarbonate buffer (KHB) + 1 microM ADMA (group C), or with KHB + 1 microM ADMA and either 10 microM NaQSA (Q10) or 50 microM NaQSA (Q50). In group 0 (sham) livers were perfused with KHB alone. Levels of ADMA, alanine (ALT) and aspartate (AST) aminotransferases activities were measured during perfusion. After 90 min. of perfusion superoxide dismutase (SOD) and dimethylarginine dimethylaminohydrolase (DDAH) activities were estimated in liver homogenates. RESULTS: DDAH activity in Q10 group was significantly higher as compared to control and Q50 groups. No significant differences were observed between Q50 and control group. The decrease in ADMA concentration during perfusion was observed in all groups, but the most pronounced in the group Q10 and the least in group Q50. During perfusion AST activities were the lowest in Q50 group. No significant difference in SOD activity in groups perfused with NaQSA as compared to control group was noted. CONCLUSIONS: The impact of NaQSA on ADMA/DDAH system depends on its concentration. In lower concentration NaQSA exerted some beneficial properties which vanished in higher concentration. No increase in SOD activity during perfusion with NaQSA was observed.


Subject(s)
Amidohydrolases/metabolism , Arginine/analogs & derivatives , Liver/drug effects , Quercetin/analogs & derivatives , Superoxide Dismutase/metabolism , Alanine Transaminase/metabolism , Animals , Arginine/metabolism , Aspartate Aminotransferases/metabolism , Liver/enzymology , Liver/metabolism , Male , Perfusion , Quercetin/pharmacology , Rats , Rats, Wistar
9.
Przegl Lek ; 67(1): 25-7, 2010.
Article in Polish | MEDLINE | ID: mdl-20509567

ABSTRACT

Wide spectrum of infectious causes should be considered while diagnosing febrile states in infants.The aim of study is to present the case of 3-month-old infant with febrile states. Boy was admitted to Department of Pediatrics to Infant Unit because of the febrile states lasting for 4 weeks. Perinatal history: first pregnancy, cesarean section in 39 weeks of gestation due to mother's pointed condyloma, birth weight 3140 g, Apgar score 10 in first minute. There was no information about the course of pregnancy, mother's diseases, father was unknown. The child was ambulatory cured with several antibiotics because of the respiratory tract infections. On admission to hospital the general status of the infant was quite good, there was respiratory tract infection, hepatomegaly, and aphthae found in physical examination. Increased levels of inflammation markers and elevated activity of liver enzymes were observed in laboratory tests. Perihilar inflammatory density was found in chest radiogram. After finishing pharmacological treatment there were no pathological changes on auscultation of the lungs. The hospital course was complicated with Rotaviral infection. As the febrile states and hyperactivity of liver enzymes persisted, the diagnostics was extended. There was sepsis, neuroinfection, number of bacterial and viral infections excluded. There was also urine collected for the levels of catecholamines, the result was normal. Due to reverse proportion of the CD4 and CD8 lymphocytes, persistent active CMV infection and clinical status of the child, HIV test was performed. There was confirmed presence of p24 antigen of HIV in immunological test. The child was transfered to Child's Infectious Diseases Unit of Stefan Zeromski Hospital in Cracow to verify the result of laboratory test and start therapy.


Subject(s)
Fever/etiology , HIV Seropositivity/complications , HIV Seropositivity/diagnosis , Hepatomegaly/diagnosis , Respiratory Tract Infections/complications , Respiratory Tract Infections/diagnosis , Child, Preschool , Diagnosis, Differential , Hepatomegaly/etiology , Humans , Male , Rotavirus Infections/complications , Rotavirus Infections/diagnosis
10.
Exp Toxicol Pathol ; 62(2): 105-8, 2010 Mar.
Article in English | MEDLINE | ID: mdl-19297139

ABSTRACT

Water-soluble quercetin-5'-sulfonic acid sodium salt (NaQSA) and morin-5'-sulfonic acid sodium salt (NaMSA) could exert an antagonistic effect on cadmium intoxication. The aim of the study was to examine the influence of these substances on superoxide dismutase (SOD) and glutathione (GSH) levels in the mouse liver in the subacute cadmium intoxication model. NaQSA and NaMSA significantly counteracted cadmium-induced decreases in SOD and GSH levels. No significant differences in SOD and GSH levels between groups exposed to cadmium receiving NaQSA or/and NaMSA were observed.


Subject(s)
Antioxidants/pharmacology , Cadmium Poisoning/drug therapy , Flavonoids/pharmacology , Quercetin/analogs & derivatives , Animals , Glutathione/drug effects , Lipid Peroxidation/drug effects , Liver/drug effects , Male , Mice , Mice, Inbred BALB C , Oxidative Stress/drug effects , Quercetin/pharmacology , Superoxide Dismutase/drug effects
11.
Pol J Pharmacol ; 55(6): 1097-103, 2003.
Article in English | MEDLINE | ID: mdl-14730106

ABSTRACT

Hexavalent chromium compounds exhibit higher toxicity than its trivalent compounds since chromium ions in the +6 oxidation state easily cross biological membranes. It has recently been proposed that substances reducing chromium ions from the +6 to the less toxic +3 oxidation state can be beneficial in management of acute chromium poisoning. In vitro studies also demonstrated quercetin-5 '-sulfonic acid sodium salt (NaQSA) to reduce chromium ions from the +6 to the +3 oxidation state. The aim of the study was to determine efficacy of NaQSA in treatment of acute poisoning with a hexavalent chromium compound. The experiment was carried out on male and female Wistar rats which were divided into 4 experimental (A,B,C,D) and control (K) groups. All animals received intragastrically a single CrO3 dose equal to its LD50. Thirty minutes after administration of CrO3, NaQSA was administered intragastrically at a dose of 50 mg/kg (group A) and 100 mg/kg (group B). In groups C and D, NaQSA was administered ip 2 h after administration of CrO3 and then twice a day for 4 days at doses of 50 mg/kg (group C) and 100 mg/kg (group D). Only intragastric administration of NaQSA at a dose of 100 mg/kg decreased mortality in acute poisoning with CrO3. In groups B and D, aminotransferase activity was statistically significantly dropping from day 7 of the experiment in comparison with the group K, which indicates lesser damage to the liver in animals treated with NaQSA. Bilirubin concentrations in groups B and D were also much lower than in the group K, but the difference between average bilirubin levels in these groups and the K was not statistically significant. The results of the study suggest the usefulness of NaQSA in the treatment of poisoning with hexavalent chromium compounds.


Subject(s)
Antidotes/therapeutic use , Chromium Compounds/poisoning , Quercetin/analogs & derivatives , Quercetin/therapeutic use , Acute Disease , Animals , Chromium Compounds/blood , Dose-Response Relationship, Drug , Female , In Vitro Techniques , Injections, Intraperitoneal , Male , Poisoning/drug therapy , Poisoning/mortality , Poisoning/pathology , Rats , Rats, Wistar
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