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1.
Cent Eur J Immunol ; 44(4): 423-432, 2019.
Article in English | MEDLINE | ID: mdl-32140055

ABSTRACT

Post-traumatic mortality rates are still very high and show an increasing tendency. Early identification of patients at high risk of severe complications has a significant impact on treatment outcomes. The aim of the study was to better understand the early pathological inflammatory response to injury and infection, and to determine the usefulness of the assessment of TNF-α and sTNFR1 concentrations in the peripheral blood as early indicators of severe post-traumatic complications. The study was carried out in a group of 51 patients after trauma, treated in the ED, including 32 patients who met the inclusion criteria for immunological analysis. Patients were divided into two groups using the ISS scale (A ISS ≥ 20, B ISS < 20). The highest TNF-α and sTNFR1 concentrations in both groups were recorded at admission and were significantly higher in group A compared to group B (A vs. B TNF-α 2.46 pg/ml vs. 1.78 pg/ml; sTNFR1 1667.5 pg/ml vs. 875.2 p < 0.005). The concentration of sTNFR1 in patients with severe complications was significantly higher compared to patients without complications and preceded clinical symptoms of complications (C+ vs. C- 1561.5 pg/ml vs. 930.6 pg/ml, p < 0,005). The high diagnostic sensitivity calculated from the ROC curves was found for the concentrations of both cytokines: TNF-α (AUC = 0.91, p = 0.004) and sTNFR1 (AUC = 0.86, p = 0.011). Elevated levels of sTNFR1, determined in the peripheral blood shortly after injury, are significantly associated with the occurrence of later complications, which in some patients lead to death. In contrast, high levels of TNF-α shortly after injury are associated with mortality.

2.
Cent Eur J Immunol ; 43(1): 33-41, 2018.
Article in English | MEDLINE | ID: mdl-29731690

ABSTRACT

This study was aimed to give a better understanding of the mechanisms of early immune response to trauma by assessing the concentration of cytokines in peripheral blood. The study group comprised 32 patients admitted to the Emergency Department due to injury. Depending on the magnitude of the Injury Severity Score (ISS) trauma patients were divided into two groups. In group A (ISS ≥ 20), 13 patients had complications, and five died, while in group B (ISS < 20) only three patients had complications (e.g. respiratory failure and infections). Depending on the extent of the injury, significant differences were observed in the concentrations of cytokines in the treatment groups. The highest levels of IL-6 and IL-1Ra in both groups were recorded in the third hour of hospitalisation and were considerably higher in group A compared to the concentration of these cytokines in group B (p = 0.001). In patients with complications, IL-6 and IL-1Ra concentrations were significantly higher compared to those without complications. Spearman's rho-correlation showed a statistically significant positive correlation between baseline concentrations of IL-6 (r = 0.64, p < 0.001) and IL-1Ra (r = 0.37, p = 0.042) and the values of the ISS. A high diagnostic sensitivity calculated from ROC curves was found for IL-6 concentrations. In summary, our findings suggest that elevated levels of the cytokines tested, determined in the peripheral blood shortly after injury, may be significantly associated with the occurrence of severe complications, which in some patients can lead to death. Monitoring the levels of these cytokines in patients with a high risk of serious complications should be used routinely.

3.
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
4.
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
5.
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
6.
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
7.
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
8.
J Inorg Biochem ; 103(9): 1189-95, 2009 Sep.
Article in English | MEDLINE | ID: mdl-19631988

ABSTRACT

Two complexes of calcium ions containing monodeprotonated caffeate ligands were synthesized and physicochemically (IR, FIR, NMR, thermal analysis) and theoretically (DFT and pharmacokinetical parameters) characterized. [Ca(C(9)H(7)O(4))(2)].2H(2)O 1a and [Ca(C(9)H(7)O(4))(2)].2H(2)O KNO(3)1b are compounds with unusual four coordinate calcium ion containing the ligand coordinated to the metal ion through two carboxylic groups arranged with tetrahedrally-like mode (CaO(4)). Two water molecules are outside the first coordination sphere bound non-equivalently to the ligand through a net of hydrogen bonding. The compounds were found to be cytotoxically inactive. Finally, in silico parameters predict the potential application of the compound as a supplement and/or drug.


Subject(s)
Antineoplastic Agents/chemistry , Antioxidants/chemistry , Caffeic Acids/chemistry , Calcium/chemistry , Chelating Agents/chemistry , Organometallic Compounds/chemistry , Antineoplastic Agents/chemical synthesis , Antineoplastic Agents/pharmacokinetics , Antineoplastic Agents/pharmacology , Antioxidants/toxicity , Calorimetry, Differential Scanning , Cell Line, Tumor , Cell Proliferation , Chelating Agents/pharmacology , Computer Simulation , Drug Design , Drug Screening Assays, Antitumor , HL-60 Cells , Humans , Ligands , Magnetic Resonance Spectroscopy , Models, Biological , Molecular Structure , Organometallic Compounds/pharmacokinetics , Organometallic Compounds/pharmacology , Spectrophotometry, Atomic , Spectroscopy, Fourier Transform Infrared , Thermogravimetry , X-Ray Diffraction
9.
Eur J Cardiothorac Surg ; 32(6): 868-72, 2007 Dec.
Article in English | MEDLINE | ID: mdl-17923413

ABSTRACT

OBJECTIVE: To assess the influence of mediastinal lymphadenectomy on postoperative concentration of interleukin 6 (IL-6) and interleukin 1 receptor antagonist (IL-1 ra) in serum, sputum, and pleural fluid, in patients operated upon due to lung cancer and benign pulmonary diseases. METHODS: Thirty-three patients undergoing uncomplicated resections, including 23 with lung cancer and 10 with benign diseases, were analyzed. In patients with right lung cancer we performed a systematic lymphadenectomy, while in patients with left lung cancer systematic sampling was performed. Serum IL-6 and IL-1 ra concentration was measured before and after surgery, and on postoperative days 1, 3, and 7, as well as in sputum at the end of surgery and in pleural fluid on postoperative day 1, by ELISA test. RESULTS: In 23 patients with cancer, 19.0+/-11.43 mediastinal lymph nodes were removed (in 11 patients with right lung cancer 27.6+/-7.6 and in 12 patients with left lung cancer 11.1+/-8.1). No differences were found in serum and sputum concentration of IL-6 and IL-1 ra between patients after right and left thoracotomy due to cancer and between patients with cancer and patients with benign diseases. Patients with cancer had a lower concentration of IL-1 ra in pleural fluid (median 16950, range 16050-45470.05 pg/ml) than patients with benign diseases (76665.6 pg/ml (range 53618-89617.9); p=0.0008). In 23 cancer patients a negative correlation between concentration of cytokines in pleural fluid and a number of mediastinal lymph nodes resected was observed (Spearman correlation coefficient for IL-6: r=-0.44, p=0.04; for IL-1 ra: r=-0.57, p=0.01). Such correlation was not observed for a number of positive N2 lymph nodes. CONCLUSIONS: Systematic lymphadenectomy added to major lung resection does not increase postoperative humoral immune response in uncomplicated cases, as measured by levels of IL-6 and IL-1 ra in serum, pleural fluid, and sputum.


Subject(s)
Lung Neoplasms/surgery , Lymph Node Excision , Adult , Aged , Carcinoma, Non-Small-Cell Lung/immunology , Carcinoma, Non-Small-Cell Lung/surgery , Female , Humans , Interleukin 1 Receptor Antagonist Protein/metabolism , Interleukin-6/metabolism , Lung Diseases/immunology , Lung Diseases/surgery , Lung Neoplasms/immunology , Male , Mediastinum , Middle Aged , Pleural Effusion/immunology , Pneumonectomy , Postoperative Period , Prospective Studies , Sputum/immunology
10.
J Inorg Biochem ; 101(5): 774-82, 2007 May.
Article in English | MEDLINE | ID: mdl-17368778

ABSTRACT

New solid complex compounds of La(III), Ce(III), Pr(III), Nd(III), Sm(III), Eu(III) and Gd(III) ions with morin were synthesized. The molecular formula of the complexes is Ln(C(15)H(9)O(7))(3).nH(2)O, where Ln is the cation of lanthanide and n=6 for La(III), Sm(III), Gd(III) or n=8 for Ce(III), Pr(III), Nd(III) and Eu(III). Thermogravimetric studies and the values of dehydration enthalpy indicate that water occurring in the compounds is not present in the inner coordination sphere of the complex. The structure of the complexes was determined on the basis of UV-visible, IR, MS, (1)H NMR and (13)C NMR analyses. It was found that in binding the lanthanide ions the following groups of morin take part: 3OH and 4CO in the case of complexes of La, Pr, Nd, Sm and Eu, or 5OH and 4CO in the case of complexes of Ce and Gd. The complexes are five- and six-membered chelate compounds.


Subject(s)
Flavonoids/chemical synthesis , Lanthanoid Series Elements/chemistry , Organometallic Compounds/chemical synthesis , Flavonoids/chemistry , Magnetic Resonance Spectroscopy , Organometallic Compounds/chemistry , Spectrometry, Mass, Secondary Ion , Spectrophotometry, Infrared , Spectrophotometry, Ultraviolet , Thermodynamics , Thermogravimetry
11.
Eur J Cardiothorac Surg ; 31(4): 719-24, 2007 Apr.
Article in English | MEDLINE | ID: mdl-17317198

ABSTRACT

OBJECTIVE: To assess changes of interleukin 6 (IL-6) and interleukin 1 receptor antagonist (IL-1ra) in serum, sputum, and drained pleural fluid of patients operated on due to lung cancer. METHODS: Twenty-seven patients treated with lobectomy or pneumonectomy, including 14 with complications and 13 without complications, were analyzed. Serum IL-6 and IL-1ra concentration was measured before, at the end of surgery, and on postoperative day 1, 3, and 7, by ELISA test. Additionally, concentration of IL-6 and IL-1ra was measured in sputum at the end of surgery and in pleural fluid on postoperative day 1. RESULTS: In the entire group serum concentrations of IL-6 and IL-1ra were significantly elevated after surgery, in comparison with preoperative values. Serum IL-6 concentration was higher in patients with complications only on day 7 (median 59.0 (range: 41.25-76.65) pg/ml vs 21.5 (9.87-35.0) pg/ml; p=0.012). Patients with complications had higher concentration of IL-6 in pleural fluid (91312 (51812-94872) pg/ml vs 2006 (1926-2108) pg/ml; p=0.00008). Serum IL-1ra concentration was higher in patients with complications on day 1 (1832.4 (1144.7-2362.2) pg/ml vs 1088.4 (817.5-1312.5) pg/ml; p=0.01). Concentration of IL-1ra in drained fluid was higher in patients with complications (68128.8 (48104-108564) pg/ml vs 16470 (15930-16875) pg/ml; p=0.0003). On day 1 after surgery a significant correlation between serum and pleural fluid concentration for IL-6 as well as for IL-1ra were observed (Spearman test for IL-6: r=0.47; p=0.02; for IL-1ra: r=0.48; p=0.02). CONCLUSIONS: Elevated concentrations of IL-6 and IL-1ra in pleural fluid on postoperative day 1 are promising early markers of postoperative complications. Elevated concentrations of IL-6 and IL-1ra in serum are good early markers of severity of surgical injury and may reflect development of postoperative complications.


Subject(s)
Interleukin 1 Receptor Antagonist Protein/analysis , Interleukin-6/analysis , Lung Neoplasms/surgery , Postoperative Complications/metabolism , Adolescent , Adult , Aged , Biomarkers/analysis , Biomarkers/blood , Female , Humans , Interleukin 1 Receptor Antagonist Protein/blood , Interleukin-6/blood , Lung/surgery , Male , Middle Aged , Pleural Effusion/chemistry , Prospective Studies , Sputum/chemistry
12.
Acta Pol Pharm ; 62(1): 65-7, 2005.
Article in English | MEDLINE | ID: mdl-16022496

ABSTRACT

The antibacterial activity of morin, sodium salt of morin-5"-sulfonic acid (NaMSA) and new complexes of La (II), Gd (III) and Lu (III) with morin were tested against three bacterial strains: Escherichia coli G (-), Klebsiella pneumoniae G (-), Staphylococcus aureus G (+) and compared with the activity of penicillin. All of the complexes possess inhibitory action against the tested strains. The activity of the studies compounds depends on their concentration. The complexes at a concentration of 10 microg/cylinder demonstrated higher activity than morin alone, but at a concentration of 100 microg/cylinder morin was the most effective inhibitor against the strains used in this investigation.


Subject(s)
Anti-Bacterial Agents/pharmacology , Flavonoids/pharmacology , Bacteria/drug effects , Flavonoids/chemistry , Gadolinium/chemistry , Lanthanum/chemistry , Lutetium/chemistry , Microbial Sensitivity Tests
13.
Anal Sci ; 20(9): 1333-7, 2004 Sep.
Article in English | MEDLINE | ID: mdl-15478345

ABSTRACT

Results of some studies on the interaction of noble metals with quercetin (Q) and quercetin-5'-sulfonic acid (QSA), the compounds of flavonoid group, are presented. The reactions of chloride complexes of the metals: RuOHCl5(2-), PdCl4(2-), OsCl6(2-), PtCl6(2-) and AuCl4- with both reagents were examined. The redox reactions of ruthenium and gold with Q and QSA have been identified. The reaction of the metals with both reagents results in the formation of the oxidized form of Q that exhibits maximum absorbance at 291 nm. Ruthenium and gold react with the examined reagents under similar conditions: 0.04 M HCl and 1 x 10(-4) M Q (or QSA). The CH3OH + H2O (1:1) (Q) and pure aqueous (QSA) media can be used. The reaction of gold with Q is slow at room temperature. It can be accelerated by heating the solution being examined. The reaction proceeds significantly faster when the water-soluble sulfonic derivative of quercetin, quercetin-5'-sulfonic acid, is used as a reagent. The new species formed can make the basis of spectrophotometric methods for the determination of ruthenium and gold. The molar absorptivities at 291 nm are equal to 5.0 x 10(3) and 2.2 x 10(4) L mol(-1) cm(-1) for Ru and Au, respectively, independently of the reagent used. Some methods for the determination of the content of gold (0.04%) in a cosmetic cream were developed.


Subject(s)
Gold Compounds/analysis , Quercetin/analogs & derivatives , Quercetin/chemistry , Ruthenium Compounds/analysis , Cosmetics/analysis , Gold Compounds/chemistry , Osmium Compounds/analysis , Osmium Compounds/chemistry , Oxidation-Reduction , Palladium/analysis , Palladium/chemistry , Platinum Compounds/analysis , Platinum Compounds/chemistry , Reference Standards , Ruthenium Compounds/chemistry , Spectrophotometry, Ultraviolet
14.
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
15.
Acta Pol Pharm ; 59(1): 77-9, 2002.
Article in English | MEDLINE | ID: mdl-12026118

ABSTRACT

Flavonoids are a group of naturally occurring compounds with interesting medical properties, such as antiinflammatory, antiallergic, antiviral, antibacterial and antitumor activities. In our experiments we were trying to examine the tumoricidal activity of newly synthesized derivatives of two flavonoids: 3,5,7,2',4'-pentahydroxyflavone (morin) and 3,5,7,3',4'-pentahydroxyflavone (quercetin). These derivatives were: natrium salt of morin-5'-sulfonic acid (NaMSA), natrium salt of quercetin-5'-sulfonic acid (NaQSA), complex of Mg2+ with quercetin-5'-sulfonic acid (QSA), complex of iron(II) with QSA. The antitumor activity of these agents was tested in vitro on two cell lines: L1210--murine lymphocytic leukaemia and P-815--murine mastocytoma. Our experiments showed that sulfonic derivatives of these two flavonoids were less potent than the original agents in their cytostatic and cytotoxic activities. However, their solubility in water was greater than that of the original agents and higher culture medium concentration of these derivatives was obtained. The results indicate that the ability of flavonoids to act tumoricidally is reciprocally correlated with their lipophilicity.


Subject(s)
Drug Screening Assays, Antitumor , Flavonoids/pharmacology , Proteasome Endopeptidase Complex/chemistry , Proteasome Endopeptidase Complex/isolation & purification , Quercetin/pharmacology , Animals , Antioxidants/chemical synthesis , Antioxidants/pharmacology , Cell Survival/drug effects , Drug Screening Assays, Antitumor/methods , Drug Screening Assays, Antitumor/statistics & numerical data , Flavonoids/chemical synthesis , Mice , Proteasome Endopeptidase Complex/genetics , Quercetin/chemical synthesis , Sulfonic Acids/chemical synthesis , Sulfonic Acids/pharmacology , Tumor Cells, Cultured/drug effects
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