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1.
Chem Biodivers ; 20(12): e202300922, 2023 Dec.
Article in English | MEDLINE | ID: mdl-37997279

ABSTRACT

This study examined the effects of methanol extract and its sub-extracts from Epilobium angustifolium on α-glucosidase and α-amylase activity. Secondary metabolites and amino acids were quantified using LC-MS/MS. Dichloromethane sub-extract displayed the highest activity and was chosen for further investigation. Despite the widespread use of E. angustifolium, genotoxicity studies were conducted to assess its safety. Dichloromethane significantly inhibited α-glucosidase (IC50 =17.340 µg/mL), making it approximately 293 times more effective than acarbose. Six known compounds, including gallic acid (1), a mixture of quercetin-3-O-α-galactoside (2a) and quercetin-3-O-α-glucoside (2b), quercetin-3-O-α-glucuronic acid (3), quercetin-3-O-α-rhamnoside (4), and kaempferol-3-O-α-rhamnoside (5) were identified. Quercetin-3-O-α-rhamnoside exhibited the highest inhibition of α-glucosidase (IC50 =1735±85 µM), making it 3.70 times more effective than acarbose. Dichloromethane also showed significant antigenotoxic activity against mutagenesis induced by NaN3, 9-AA, 4-NPD, and MNNG. Gallic acid was found in the highest abundance (13253.6931 ng/mL) in the methanolic extract. Furthermore, L-Aspartic acid was the most concentrated amino acid (363.5620 nmol/mL) in the methanolic extract.


Subject(s)
Epilobium , Quercetin , Quercetin/chemistry , Epilobium/chemistry , Hypoglycemic Agents/pharmacology , Acarbose , alpha-Glucosidases , Chromatography, Liquid , Methylene Chloride , Plant Extracts/pharmacology , Plant Extracts/chemistry , Tandem Mass Spectrometry , Gallic Acid/pharmacology , Phytochemicals/pharmacology , Phytochemicals/analysis
2.
Chem Biodivers ; 20(9): e202300896, 2023 Sep.
Article in English | MEDLINE | ID: mdl-37605961

ABSTRACT

Heterocyclic compounds are found in a variety of drug molecules, and bioactive natural products. 4-Thiazolidinones (4-TZDs), which represent an important class of heterocyclic compounds, are of great interest today with their diverse bioactivities. In this study, ten novel 4-TZD derivatives (C1-C10) were synthesized, characterized by spectroscopic techniques, and their genotoxic, and antigenotoxic properties were investigated in vitro using the Ames Salmonella/microsome mutagenicity assay in the concentration range of 0.2-1.0 mM/plate. The results revealed that none of the compounds were mutagenic on the three different Salmonella typhimurium strains up to the highest concentration tested. Furthermore, in our study, C1, C4, C6, and C9 showed significant, ranging from moderate to strong, antigenotoxic effects against mutagen-induced DNA damage at relatively higher doses. Among these, C4 had the best potential to inhibit the number of revertant colonies induced by 9-aminoacridine (9-AA), with a maximum inhibition rate of 47.9 % for 1.0 mM/plate. As a result, preliminary knowledge about the safety of the use of ten novel synthesized 4-TZD compounds likely to exhibit many bioactivities was obtained in this study. In addition, the significant in vitro antimutagenic activity of some derivatives increases the importance of studies for the development of new pharmacological agents for cancer prevention.


Subject(s)
Antimutagenic Agents , Antimutagenic Agents/pharmacology , Antimutagenic Agents/chemistry , Mutagens/toxicity , Salmonella typhimurium , Aminacrine , DNA Damage
3.
Protoplasma ; 260(6): 1581-1601, 2023 Nov.
Article in English | MEDLINE | ID: mdl-37338647

ABSTRACT

Ferula tingitana L. is a high perennial plant and its leaf is an alternate arrangement and yellow, and its flowers are unisexual like other Apiaceae. It has been used as a spice and for various medicinal purposes in the Mediterranean region. The paper reports antidiabetic, antimicrobial, anticholinesterase, antioxidant, and genotoxic activities of leaves, flowers, stems, and fruits methanol extracts of F. tingitana. Also, quantitative determination of some secondary metabolites was also analyzed by LC-MS/MS. Moreover, chemical composition of essential oils was analyzed. Consequently, anatomical, and morphological properties of plant were investigated. Germacrene D (23.6%), 1,3,5-trimethylbenzene (18.4%), and α-pinene (50.0%) were found as the main compounds in flower, leaf, and stem oils, respectively. The cortex in stem, pedicel, and fruit is characterized by angular collenchyma cells and a distinct cambium layer. 6 compounds (quinic acid, fumaric acid, keracyanin chloride, cyanidin-3-O-glucoside, chlorogenic acid, hesperidin) were observed in samples. Leaf extract showed anticholinesterase activity. Leaf and flower extracts showed the highest % inhibition value on ABTS·+ and DPPH•. Leaf extract has the strongest antioxidant effect because it is rich in total phenolic contents. All extracts of F. tingitana were found generally effective against C. albicans. Stem extract was found effective against E. coli and flower extract was found more effective against S. enterica and C. albicans. Bacterial genotoxicity results showed that extracts did not have genotoxic activity on tester strains S. typhimurium and E. coli WP2uvrA. Thus, it revealed that extracts were genotoxic-ally safe at applied concentrations up to 3 mg/plate.

4.
Toxicol Ind Health ; 39(7): 345-355, 2023 Jul.
Article in English | MEDLINE | ID: mdl-37156264

ABSTRACT

There are various studies on the toxicological potentials of conventionally synthesized zinc oxide (ZnO) nanoparticles, which are useful tools for many medical applications. However, knowledge about the biologically synthesized ones is still limited. In this study, the potential of producing ZnO nanoparticles via a green synthesis method, which enables safer, environmentally, economical and controlled production by using the Symphoricarpos albus L. plant, was investigated. For this purpose, aqueous extract was obtained from the fruits of the plant and reacted with zinc nitrate precursor. Characterization of the synthesized product was carried out by SEM and EDAX analyzes. In addition, the biosafety of the product was also investigated by using the Ames/Salmonella, E. coli WP2, Yeast DEL, seed germination, and RAPD test systems. The results obtained from SEM studies showed that spherical nanoparticles with an average diameter of 30 nm were synthesized as a result of the reaction. EDAX findings confirmed that these nanoparticles were composed of Zn and O elements. On the other hand, according to the findings of the biocompatibility tests, the synthesized nanoparticle did not show any toxic and genotoxic effects up to a concentration of 640 µg/ml in any of the test systems. Accordingly, considering the findings of our study, it was concluded that the aqueous extract of S. albus fruits can be used for the green synthesis of ZnO nanoparticles, the products obtained successfully passed the biocompatibility tests in our study, and additionally, more comprehensive biocompatibility tests should be performed before industrial scale production.


Subject(s)
Metal Nanoparticles , Nanoparticles , Zinc Oxide , Zinc Oxide/toxicity , Anti-Bacterial Agents , Escherichia coli , Random Amplified Polymorphic DNA Technique , Nanoparticles/toxicity , Metal Nanoparticles/toxicity , Plant Extracts/toxicity , Microbial Sensitivity Tests
5.
Int J Radiat Biol ; 99(11): 1785-1793, 2023.
Article in English | MEDLINE | ID: mdl-37071465

ABSTRACT

PURPOSE: Determination of the protective property of melanin, an organic polymer class consisting of phenolic and/or indolic compounds isolated from bacteria and fungi, against fast neutron radiation. To show that these melanin samples, which also have antioxidant and metal chelating properties, can be used as an active ingredient for a drug to be developed against neutrons used in nuclear research and medicine. MATERIALS AND METHODS: Bacterial and fungal media were prepared, and melanin pigments were produced and isolated. For molecular characterization of pigments, bacterial genomic DNA extraction, 16S rDNA gene amplification processes, and fungal genomic DNA extraction, ITS1, and ITS4 Gene Regions amplification were performed. The DEL assay was implemented to determine the genotoxicity properties of bacterial and fungal melanin pigments. Samples were prepared in a pad measuring 10 ml volume (60 × 15 mm) at a concentration of 0.2-1 microgram in 1% agarose gel for radiation-absorbed dose measurements. Absorption measurements were made using 241Am-Be fast neutron source and Canberra brand NP series BF3 gaseous detector to determine the neutron radiation absorption capacity of all samples. The results obtained to determine the absorption degrees of melanin samples were compared with paraffin and normal concrete, which are widely used in neutron radiation shielding studies. RESULTS: Melanin pigments were obtained using different bacteria and fungi strains. Afterwards, the fast neutron radiation absorption capacity of these purified pigments were determined. Compared to reference samples, these pigments were found to have slightly lower radiation absorbing ability. In addition to these experiments, cytotoxicity tests were carried out using the Yeast DEL assay technique to evaluate the potential for use of these organic pigments in fields such as medicine and pharmacology. According to the results obtained from the tests, it was determined that these melanin samples did not have any toxic effects. CONCLUSION: It was determined that these melanin samples have the potential to be used as a radioprotective drug active substance to protect the tissues and cells of people exposed to neutron radiation after a nuclear accident or nuclear war.Giving a drug that will be developed by using these active ingredients before or after people are exposed to a radiation environment can provide great benefits.


Subject(s)
Melanins , Radiation Protection , Humans , Melanins/pharmacology , Radiation Protection/methods , Bacteria , DNA
6.
Int J Radiat Biol ; 99(2): 245-258, 2023.
Article in English | MEDLINE | ID: mdl-35687366

ABSTRACT

PURPOSE: Five different types of synthesized azadispiro derivatives have been analyzed for radiation absorption capacity and determined their potential to be exploited as substances for a drug to be developed against radiation has been investigated. MATERIAL AND METHODS: Fast neutron attenuation parameters like the effective mean free path, half-value layer (HVL), removal cross-sections, and neutron transmission number were found with the Monte Carlo simulation Geometry And Tracking (GEANT4) code. Gamma radiation absorption parameters, such as effective atom number (Zeff), mean free path (MFP), mass attenuation coefficient (MAC), and half-value layer (HVL) were theoretically determined with WinXCom software. Besides, the exposure build-up factor (EBF) was calculated by using GP fitting parameters. Neutron absorption dose rate was experimentally calculated with 241Am-Be fast neutron source which has 4.5 MeV of energy, 74 GBq activity, and portative BF3 neutron detector. Ames/Salmonella test systems were used for the genotoxic potentials of the azadispiro derivatives. RESULTS AND CONCLUSIONS: Experimental and theoretical results were checked with paraffin and High-Density Polyethylene. The results showed that Azadispiro derivatives have neutron radiation absorption capability close to paraffin and High-Density Polyethylene. The gamma radiation absorption properties for azadispiro derivatives have been investigated, and it has been observed that these materials can absorb gamma radiation. Ames/Salmonella assay was used to examine whether the derivatives had a genotoxic effect probability or not. The results showed that these derivatives were genotoxic and safe at test doses (up to 5 mM). Consequently, it has been understood that these azadispiro derivatives can be used as active and genotoxic safety ingredients in the production of a protective drug against both neutrons and gamma rays.


Subject(s)
Paraffin , Polyethylene , Neutrons , Fast Neutrons , Software
7.
Rev Assoc Med Bras (1992) ; 68(8): 1068-1072, 2022 Aug.
Article in English | MEDLINE | ID: mdl-36134836

ABSTRACT

OBJECTIVE: The aim of this study was to demonstrate the effect of extracorporeal shock wave lithotripsy application on the success and complications of ureteroscopic lithotripsy in proximal ureter stones. METHODS: The data of 87 patients who did not respond to shock wave lithotripsy and underwent ureteroscopic lithotripsy were retrospectively analyzed and classified as group I, and 99 patients who received ureteroscopic lithotripsy as primary treatment were classified as group II. Demographic features, response to treatment, and preoperative and postoperative complications were compared between the two groups. RESULTS: There was no difference between the two groups in terms of gender, operation times, stone sizes, and ureteroscope diameters. (p>0.05). Infective complications such as postoperative fever, pyelonephritis, and urosepsis were similar in both groups (p=0.142, p=0.291, and p=0.948). Stone migration was observed in 10 (11.5%) and 6 (6.1%) patients in groups I and II, respectively (p=0.291). Impacted stone was seen in 47 (54%) patients in group I and in 15 (15.2%) patients in group II (p<0.0001). Mucosal laceration occurred in 11 (12.6%) and 3 (3%) patients in groups I and II, respectively (p=0.028). Ureteral perforation was detected in 3 (3.4%) patients in group I and 1 (1%) patient in group II, whereas ureteral avulsion was not observed in either group (p=0.524). CONCLUSIONS: It was concluded that the application of shock wave lithotripsy before ureteroscopic lithotripsy in proximal ureter stones did not affect the success. Although the results are similar in terms of postoperative infection, shock wave lithotripsy application has been found to increase the risk of stone impaction into the mucosa and ureteral laceration.


Subject(s)
Lacerations , Lithotripsy , Ureteral Calculi , Humans , Lacerations/therapy , Lithotripsy/adverse effects , Retrospective Studies , Treatment Outcome , Ureteral Calculi/therapy , Ureteroscopy/adverse effects
8.
Rev. Assoc. Med. Bras. (1992, Impr.) ; 68(8): 1068-1072, Aug. 2022. tab, graf
Article in English | LILACS-Express | LILACS | ID: biblio-1406605

ABSTRACT

SUMMARY OBJECTIVE: The aim of this study was to demonstrate the effect of extracorporeal shock wave lithotripsy application on the success and complications of ureteroscopic lithotripsy in proximal ureter stones. METHODS: The data of 87 patients who did not respond to shock wave lithotripsy and underwent ureteroscopic lithotripsy were retrospectively analyzed and classified as group I, and 99 patients who received ureteroscopic lithotripsy as primary treatment were classified as group II. Demographic features, response to treatment, and preoperative and postoperative complications were compared between the two groups. RESULTS: There was no difference between the two groups in terms of gender, operation times, stone sizes, and ureteroscope diameters. (p>0.05). Infective complications such as postoperative fever, pyelonephritis, and urosepsis were similar in both groups (p=0.142, p=0.291, and p=0.948). Stone migration was observed in 10 (11.5%) and 6 (6.1%) patients in groups I and II, respectively (p=0.291). Impacted stone was seen in 47 (54%) patients in group I and in 15 (15.2%) patients in group II (p<0.0001). Mucosal laceration occurred in 11 (12.6%) and 3 (3%) patients in groups I and II, respectively (p=0.028). Ureteral perforation was detected in 3 (3.4%) patients in group I and 1 (1%) patient in group II, whereas ureteral avulsion was not observed in either group (p=0.524). CONCLUSIONS: It was concluded that the application of shock wave lithotripsy before ureteroscopic lithotripsy in proximal ureter stones did not affect the success. Although the results are similar in terms of postoperative infection, shock wave lithotripsy application has been found to increase the risk of stone impaction into the mucosa and ureteral laceration.

9.
Int J Radiat Biol ; 96(11): 1423-1434, 2020 11.
Article in English | MEDLINE | ID: mdl-32813583

ABSTRACT

PURPOSE: Quinoline is formed by various natural compounds, such as alkaloids from the cinchona plant, which exhibit various biological activities, and is an important building material for the development of new drugs. Quinoline can be used in anti-radiation drug development but radiation interaction properties must be determined. MATERIAL AND METHODS: In this study, six types of synthesized quinoline derivatives were used. Fast neutron removal cross-section, mean free path, half value layer and transmission number were theoretically determined by using GEometry ANd Tracking 4 and FLUktuierende KAskade simulation codes for neutron shielding. Neutron dose absorption rates were determined using the 241Am-Be fast neutron source and the Canberra NP series portable BF3 gas proportional neutron detector. Gamma radiation shielding parameters were determined by using WinXCom and PSY-X/PSD software. Additionally, the genotoxic potentials of the derivatives were assessed by using the Ames/Salmonella bacterial reversion assay. RESULTS AND CONCLUSIONS: Neutron shielding parameters such as removal cross-section, mean free path, half value layer and transmission number were theoretically determined for fast neutrons. To determine neutron absorption capacity of quinoline derivatives, neutron absorption, experiments were conducted. In addition, gamma radiation shielding parameters were calculated such as the mean free path (MFP), mass attenuation coefficient (µt), half value thickness layer (HVL) and effective atomic number (Zeff) in the energy range of 0.015-15 MeV. The results of the all quinoline derivatives have excellent fast neutron shielding power compared to ordinary concrete. In addition, all quinoline derivatives have been found to have the capacity to attenuate gamma radiation. Moreover, they absorb well in both types of radiation, do not cause secondary radiation, and they are genotoxically safe at the tested concentrations. This study has demonstrated that these products can be used as active ingredients for a drug to be developed against radiation.


Subject(s)
Gamma Rays/adverse effects , Neutrons/adverse effects , Quinolines/chemistry , Quinolines/pharmacology , Radiation-Protective Agents/chemistry , Radiation-Protective Agents/pharmacology , Quinolines/chemical synthesis , Radiation-Protective Agents/chemical synthesis
10.
World J Microbiol Biotechnol ; 36(7): 93, 2020 Jun 20.
Article in English | MEDLINE | ID: mdl-32562106

ABSTRACT

Phosphorus (P) is the second most crucial nutrient for plant growth after nitrogen. However, its highly reactive nature causes formation of insoluble derivatives and limits uptake by the plant roots. The wide spread applications of P based chemical fertilizers cause detrimental effects on soil fertility, agricultural product quality and environment. In this regard, phosphate-solubilizing microorganisms (PSMs) stand out as the most remarkable and promising tools for the development of safer and sustainable technologies. As a result of this, many bacterial and fungal species with significant phosphate-solubilizing activity have been discovered by using the conventional screening methods. However, the growing need for the discovery of new strains of PSMs necessitates the replacement or support to the time-consuming conventional methods with techniques that are more sensitive, reliable, reproducible and less time consuming. In this context, molecular tools and techniques provide novel approaches for microbial phosphate solubilization research. Hence, in this review information on the molecular approaches for the PSMs research is provided and its importance explained. The review also discusses the genes related to phosphate solubilizing mechanisms and molecular tools for screening these genes.


Subject(s)
Agriculture/methods , Phosphates/metabolism , Bacteria/classification , Bacteria/isolation & purification , Bacteria/metabolism , Cloning, Molecular , Crops, Agricultural/microbiology , Fertilizers , Fungi/classification , Fungi/isolation & purification , Fungi/metabolism , Metagenomics , Oligonucleotide Array Sequence Analysis , Plant Development , Plant Roots/microbiology , Soil/chemistry , Soil Microbiology
11.
Andrologia ; 52(4): e13544, 2020 May.
Article in English | MEDLINE | ID: mdl-32072659

ABSTRACT

Aortic stiffness increases in patients with erectile dysfunction (ED) but it is not known whether aortic stiffness affects the degree of ED. In the present study, we aimed to determine whether there is any relationship between aortic stiffness and the severity of ED. Patients with ED were divided into 3 groups according to the International Index of Erectile Function (IIEF) scores. Mild ED was named as group 1, moderate ED as group 2 and severe ED as group 3. The values of fasting blood glucose (FBG), serum lipid values, total testosterone (T. tes), and free testosterone (F tes) were recorded. Aortic stiffness was determined by pulse wave velocity (PWV) and augmentation index (AIX) measurements. The mean or median values of the laboratory parameters among the groups were similar (p > .05). No statistical difference was found between the groups in terms of AIX value (p = .386). Mean PWV values were calculated as 7.26, 8.30 and 8.78 in group 1, group 2 and group 3 respectively. PWV values were significantly different between groups (p < .0001). PWV values were found to be increased with increasing severity of erectile dysfunction.


Subject(s)
Erectile Dysfunction/physiopathology , Vascular Stiffness , Humans , Male , Middle Aged , Severity of Illness Index
12.
Curr Microbiol ; 76(7): 804-809, 2019 Jul.
Article in English | MEDLINE | ID: mdl-31025087

ABSTRACT

In this study, the newly designed pqq gene-specific primer sets were used for determination of phosphate-solubilizing capabilities of bacterial isolates from the agricultural regions of Erzurum. The specificity of newly designed primer sets (PqqA2F/PqqA2R, Pqq5F/Pqq5R, PqqF2/PqqF2R) were tested against ten isolates, whose phosphate-solubilizing activities were initially proved by the conventional methods. Non-phosphate-solubilizing bacteria were also chosen as negative control. According to the results, five of ten phosphate-solubilizing bacteria with PqqA2F/PqqA2R, two of ten phosphate-solubilizing bacteria with Pqq5F/Pqq5R primer set, and one of ten phosphate solubilizing with PqqF2F/PqqF2R bacteria were successfully amplificated in the PCR assay and none of the non-phosphate-solubilizing bacteria was amplificated. Then, the molecular characterization of the active phosphate-solubilizing strains was done based on the partial 16S ribosomal RNA gene region sequence analysis method. Two isolates of Enterobacter sp., 1 Rhizobium sp., 1 Enterococcus sp., 1 Bacillus cereus, 1 Bacillus atrophaeus, 1 Bacillus aryabhattai, 1 Acinetobacter sp., 1 Pseudomonas japonica, and 1 Enterobacter cloacae were identified as active phosphate-solubilizing strains. Consequently, the results showed that this specific primer sets could be used as an economic, rapid, and useful tool for the detection of phosphate-solubilizing strains in the agricultural researches.


Subject(s)
Bacteria/isolation & purification , Bacteria/metabolism , Bacteriological Techniques/methods , Phosphates/metabolism , Soil Microbiology , Agriculture , Bacteria/classification , Bacteria/genetics , Bacterial Proteins/genetics , DNA, Bacterial/genetics , PQQ Cofactor/genetics , Phylogeny , Polymerase Chain Reaction , RNA, Ribosomal, 16S/genetics , Sequence Analysis, DNA , Solubility , Turkey
13.
Arch Ital Urol Androl ; 91(1): 11-15, 2019 Mar 29.
Article in English | MEDLINE | ID: mdl-30932423

ABSTRACT

OBJECTIVE: Urinoma is a rare entity and mainly occurs due to acute obstruction such as ureteral stone. We aimed to demonstrate factors associated with urinoma accompanied by ureteral calculi. MATERIAL AND METHODS: Data of 550 patients who were diagnosed with ureteral stone by computed tomography (CT) were analyzed retrospectively. In 20 patients perirenal urinoma was associated with ureteral calculi (group I), whereas in other 530 patients no urinoma was detected (group II). Gender, age, size, side and localization of the stone, hydronephrosis, fever, sepsis, urinary tract infections (UTIs), hematuria, serum creatinine, blood urea nitrogen (BUN), white blood cell (WBC), C-reactive protein (CRP), presence of diabetes mellitus (DM), hypertension (HT) and cronic kidney disease (CKD) of the two groups were compared. RESULTS: The average age of the patients were 46.2 (20-71) and 44.9 (10-82) years in group I and group II, respectively (p > 0.05). According to our results leukocytosis, microscopic and macroscopic hematuria, UTIs, increase of serum creatinine, BUN and CRP, diagnosis of DM and HT were significantly associated with urinoma (p < 0.05). In addition, patients with distal ureteral stones are more prone to urinoma (p = 0.001). An interesting finding of the study was that the stone size in group I (median 5 mm [range 3-8]) was significantly smaller than in group II (9.3 mm [4-25]; p = 0.001). CONCLUSIONS: Small stone size, distal localisation of the stone in ureter, leukocytosis, hematuria, UTIs, increase of serum creatinine, BUN and CRP, presence of DM and HT are associated with perirenal urinoma.


Subject(s)
Tomography, X-Ray Computed/methods , Ureteral Calculi/diagnostic imaging , Urinoma/diagnostic imaging , Adolescent , Adult , Aged , Aged, 80 and over , Child , Diabetes Mellitus/epidemiology , Female , Hematuria/epidemiology , Humans , Hydronephrosis/epidemiology , Hypertension/epidemiology , Leukocytosis/epidemiology , Male , Middle Aged , Retrospective Studies , Risk Factors , Urinary Tract Infections/epidemiology , Urinoma/etiology , Young Adult
14.
Toxicol Ind Health ; 33(11): 811-820, 2017 Nov.
Article in English | MEDLINE | ID: mdl-29050532

ABSTRACT

The current study was designed to assess the potential toxicological effects of newly synthesized iminothiazolidinones by employing Ames Salmonella, Escherichia coli WP2, Zea mays seed germination, and random amplified polymorphic DNA (RAPD) assay systems. The bacterial tester strains S. typhimurium TA1535, TA1537, TA1538, TA98, TA100, and E. coli WP2 uvrA were chosen to test the direct gene mutation inducing capabilities of the test materials in prokaryotic systems and Z. mays seeds for determination of potential toxicological effects in eukaryotic systems. OPA-3 and OPA-6 primers were used in the RAPD analysis to determine genotoxic activities on the eukaryotic genomes. According to the results, none of the test materials showed significant mutagenic activity on the bacterial tester strains at the chosen concentrations. Additionally, none of the tested compounds showed inhibition of the germination of Z. mays seeds. In contrast, the RAPD analysis results were inconsistent with the bacterial reversion assays and the seed germination assay results. All test materials significantly changed the RAPD profiles for OPA-3; however, only compound 5 showed a significant change for OPA-6 when compared with the control groups. In conclusion, the newly synthesized iminothiazolidinone derivatives (C1-C5) were determined as potentially genotoxic compounds and they should be checked with multiple toxicology test systems before further studies to determine their actual use.


Subject(s)
Anti-Bacterial Agents/adverse effects , Drug Design , Mutagenesis/drug effects , Pesticides/toxicity , Thiazoles/toxicity , Anti-Bacterial Agents/chemical synthesis , Anti-Bacterial Agents/chemistry , Antitubercular Agents/adverse effects , Antitubercular Agents/chemical synthesis , Antitubercular Agents/chemistry , Escherichia coli/drug effects , Escherichia coli/growth & development , Germination/drug effects , Microbial Viability/drug effects , Molecular Structure , Mutagenicity Tests , Pesticides/chemical synthesis , Pesticides/chemistry , Random Amplified Polymorphic DNA Technique , Salmonella/drug effects , Salmonella/growth & development , Salmonella typhimurium/drug effects , Salmonella typhimurium/growth & development , Seeds/drug effects , Seeds/growth & development , Thiazoles/chemical synthesis , Thiazoles/chemistry , Zea mays/drug effects , Zea mays/growth & development
15.
Pharm Biol ; 53(6): 888-96, 2015 Jun.
Article in English | MEDLINE | ID: mdl-25429992

ABSTRACT

CONTEXT: Mentha L. (Labiatae) species (mint) with their flavoring properties have been used in food industries for centuries. Besides they have a great importance in drug development and medicinal applications due to various bioactive compounds of several members of the genus. OBJECTIVE: The aim of this study was to isolate bioactive compounds with antimutagenic potential by bio-guided fractionation and determine their structures by spectroscopic methods. MATERIALS AND METHODS: The structural elucidation of the isolated compounds was done based on spectroscopic methods, including MALDI-MS, UV, IR, and 2D NMR experiments, and the bio-guided fractionation process was done by using the Ames/Salmonella test system. Henceforth, solely genotoxic and antigenotoxic potential of the new compounds were also confirmed up to 2 µM/plate by using the same test system. RESULTS: Two new chalcone glycosides: (ßR)-ß,3,2',6'-tetrahydroxy-4-methoxy-4'-O-rutinosyldihydrochalcone and (ßR)-ß,4,2',6'-tetrahydroxy-4'-O-rutinosyldihydrochalcone, were isolated from Mentha longifolia (L.) Hudson subsp. longifolia, together with known six flavonoid glycosides and one phenolic acid: apigenin-7-O-glucoside, luteolin-7-O-glucoside, apigenin-7-O-rutinoside, luteolin-7-O-rutinoside, apigenin-7-O-glucuronide, luteolin-7-O-glucuronide, rosmarinic acid. According to the antimutagenicity results, both new test compounds significantly inhibited the mutagenic activity of 9-aminoacridine in a dose-dependent manner at the tested concentrations from 0.8 to 2 µM/plate. (ßR)-ß,4,2',6'-Tetrahydroxy-4'-O-rutinosyldihydrochalcone showed the maximum inhibition rate as 75.94% at 2 µM/plate concentration. CONCLUSIONS: This is the first report that two new chalcone glycosides were isolated from Mentha longifolia subsp. longifolia and their antimutagenic potentials by using mutant bacterial tester strains. In conclusion, the two new chalcone glycosides showed a significant antigenotoxic effect on 9-aminoacridine-induced mutagenesis at tested concentrations.


Subject(s)
Antimutagenic Agents/pharmacology , Chalcones/pharmacology , Mentha/chemistry , Carbohydrate Conformation , Carbohydrate Sequence , Glycosides/pharmacology , Magnetic Resonance Spectroscopy , Molecular Sequence Data , Mutagenicity Tests , Plant Extracts/chemistry , Plant Extracts/pharmacology , Salmonella typhimurium/drug effects , Salmonella typhimurium/genetics
16.
Toxicol Ind Health ; 31(10): 911-9, 2015 Oct.
Article in English | MEDLINE | ID: mdl-23572392

ABSTRACT

Direct-type catalytic Mannich reaction for the synthesis of ß-aminoketones from cyclohexanone, substituted aromatic amines and aromatic or hetero-aromatic aldehydes has been applied in water with bismuth triflate under ultrasound. Good yields of the expected ß-aminoketones were obtained from available substrates, at room temperature in 1-2 hours. This study was designed to evaluate the mutagenic and antimutagenic potential of synthesized ß-aminoketones compounds using Ames/Salmonella and Escherichia coli WP2 bacterial reverse mutation assay systems.


Subject(s)
Ketones/pharmacology , Mesylates/chemistry , Mutagens/pharmacology , Protective Agents/pharmacology , Bacteria/drug effects , Bacteria/genetics , Ketones/chemical synthesis , Microbial Viability/drug effects , Mutation/drug effects , Protective Agents/chemical synthesis , Sonication
17.
Dalton Trans ; 43(16): 6148-64, 2014 Apr 28.
Article in English | MEDLINE | ID: mdl-24589530

ABSTRACT

Novel multifunctional hydroxyphenylimino ligands (L1, L2 and L3) were synthesized by the condensation of 2-aminophenol, 3-aminophenol and 4-aminophenol with usnic acid, a lichen metabolite. The synthesized ligands and their Cu(II), Co(II), Ni(II) and Mn(II) complexes were characterized using FT-IR, UV-Vis, (1)H-NMR, (13)C-NMR, 1D- and 2D NMR (DEPT, COSY, HMQC and HMBC), LC-MS and TGA. In addition, the metal complexes of the novel ligands were prepared with high yields using Cu(II), Co(II), Ni(II) and Mn(II) salts and were characterized using the FT-MIR/FAR, UV-Vis, elemental analysis, ICP-OES and TG/DTA techniques. The ligands and their complexes were tested against ten important pathogen microorganisms using the disc diffusion method and the metal complexes of the ligands were more active against all of the microorganisms tested with a broad spectrum than the ligands exhibiting 11­32 mm inhibition zones. On the other hand, a broad spectrum of the strongest antimicrobial activity was determined for the Mn(II) and Cu(II) complexes of the hydroxyphenylimino ligand with usnic acid (L3). In addition, the antimutagenic activities of all of the ligands and their metal complexes were determined using the Ames-Salmonella and E. coli WP2 microbial assay systems and they showed varied and strong antimutagenic effects. In general, it has been found that the Co and Mn complexes of the ligands possess potent antimutagenic activity. In view of these results, it can be concluded that some metal complexes can be used as antimicrobial and anticancer agents.


Subject(s)
Anti-Infective Agents , Antimutagenic Agents , Benzofurans , Coordination Complexes , Metals, Heavy , Aminophenols/chemistry , Anti-Infective Agents/chemistry , Anti-Infective Agents/pharmacology , Antimutagenic Agents/chemistry , Antimutagenic Agents/pharmacology , Bacteria/drug effects , Bacteria/genetics , Benzofurans/chemistry , Benzofurans/pharmacology , Coordination Complexes/chemistry , Coordination Complexes/pharmacology , Ligands , Metals, Heavy/chemistry , Metals, Heavy/pharmacology , Mutagens/toxicity , Usnea , Yeasts/drug effects
18.
Drug Chem Toxicol ; 37(4): 365-9, 2014 Oct.
Article in English | MEDLINE | ID: mdl-24341665

ABSTRACT

The goal of the present research was to determine the protective potential of five newly synthesized indenopyridine derivatives against N-methyl-N'-nitro-N-nitrosoguanidine (MNNG) and 9-aminoacridine (9-AA) induced mutagenesis. MNNG sensitive Escherichia coli WP2uvrA and 9-AA sensitive Salmonella typhimurium TA1537 were chosen as the bacterial tester strains. All of the test compounds showed significant antimutagenic activity at various tested concentrations. The inhibition rates ranged from 25.6% (Compound 2 - 1 mM/plate) to 68.2% (Compound 1 - 2.5 mM/plate) for MNNG and from 25.7% (Compound 4 - 1 mM/plate) to 76.1% (Compound 3 - 2.5 mM/plate) for 9-AA genotoxicity. Moreover, the mutagenicity of the test compounds was investigated by using the same strains. None of the test compounds has mutagenic properties on the bacterial strains at the highest concentration of 2.5 mM. Thus, the findings of the present study give valuable clues to develop new strategies for chemical prevention from MNNG and 9-AA genotoxicity by using synthetic indenopyridine derivatives.


Subject(s)
Antimutagenic Agents/pharmacology , Indenes/pharmacology , Mutagens/toxicity , Pyridines/pharmacology , Aminacrine/toxicity , Antimutagenic Agents/administration & dosage , Antimutagenic Agents/chemistry , Dose-Response Relationship, Drug , Escherichia coli/genetics , Indenes/administration & dosage , Indenes/chemistry , Methylnitronitrosoguanidine/toxicity , Mutagenicity Tests , Pyridines/administration & dosage , Pyridines/chemistry , Salmonella typhimurium/genetics
19.
Toxicol Ind Health ; 30(3): 275-83, 2014 Apr.
Article in English | MEDLINE | ID: mdl-22903173

ABSTRACT

The current study aims to determine the genotoxic and antigenotoxic potential of four newly synthesized dihydropyridine derivatives using Escherichia coli WP2 and Ames/Salmonella bacterial reversion assay systems. The bacterial mutant tester strains, E. coli WP2uvrA with a point mutation and Salmonella typhimurium TA1537 with a frameshift mutation, were used to determine genotoxic potentials of the test compounds. To determine antigenotoxic potentials of the test compounds, the same strains were also used together with positive mutagens N-methyl-N'-nitro-N-nitrosoguanidine (MNNG) for E. coli WP2uvrA and 9-aminoacridine (9-AA) for S. typhimurium TA1537. According to the results, neither of the test compounds showed significant genotoxic activity on both tester strains at the tested concentrations. However, except compound 4, all the test compounds showed significant antigenotoxic activity on MNNG- or/and 9-AA-induced mutations. The inhibition rates of mutagenesis ranged from 27.0% (compound 2: 2.5 mM/plate) to 65.0% (compound 2: 0.5 mM/plate) for MNNG and from 30.6% (compound 2: 2 mM/plate) to 58.5% (compound 1: 1 mM/plate) for 9-AA genotoxicity. According to these results, it is concluded that all the test compounds do not have a mutagenic potential on the bacterial strains at the tested concentrations, and some of them have antigenotoxic potentials against MNNG- and 9-AA-induced mutagenesis.


Subject(s)
Dihydropyridines/toxicity , Mutagenicity Tests/methods , Mutagens/toxicity , Aminacrine/toxicity , Escherichia coli/drug effects , Escherichia coli/genetics , Methylnitronitrosoguanidine/toxicity , Salmonella typhimurium/drug effects , Salmonella typhimurium/genetics
20.
Toxicol Ind Health ; 30(8): 714-23, 2014 Sep.
Article in English | MEDLINE | ID: mdl-23064766

ABSTRACT

The essential oils having many application fields such as medicine, flavoring, cosmetics are natural products obtained from aromatic plants. As the natural products of Ferula species have a wide range of use in folk medicine, this study was planned to evaluate the mutagenic and antimutagenic activities of essential oils of leaves and flowers of Ferula orientalis grown in Erzurum, through the bacterial reverse mutation assay. Furthermore, the chemical compositions of essential oils isolated by the hyrodistillation method were analysed by gas chromatography (GC) and gas chromatography-mass spectroscopy (GC-MS), as their biological activities were connected to their contents. According to our results, any tested essential oil at any used concentration on Salmonella typhimurium TA1535 and TA1537 strains and in Escherichia coli WP2 uvrA strain showed no mutagenic activity. However, the tested materials at different concentrations showed antimutagenic activities against the used mutagens. The inhibition rates ranged against sodium azide (NaN3) on S. typhimurium TA1535 from 29% to 36%, against 9-aminoacridine (9-AA) on S. typhimurium TA1537 from 40% to 68% and against N-methyl-N'-nitro-N-nitrosoguanidine (MNNG) on E. coli WP2 uvrA from 23% to 52%, respectively. Also, it is revealed by GC and GC/MS analysis of the essential oils isolated from the leaves and flowers, respectively. The major compounds in these oils were determined as α-cadinol, δ-cadinene and germacrene D-4-ol. The results of this study indicate that as the essential oils of F. orientalis have many constituents, they show no mutagenic activity but significant antimutagenic activity, and these materials can be safely used in medicinal applications after further investigations.


Subject(s)
Antimutagenic Agents/pharmacology , Ferula/chemistry , Oils, Volatile/pharmacology , Plant Extracts/pharmacology , Antimutagenic Agents/chemistry , Antimutagenic Agents/toxicity , Escherichia coli/drug effects , Mutagenicity Tests , Oils, Volatile/chemistry , Plant Extracts/chemistry , Plant Extracts/toxicity , Salmonella typhimurium/drug effects
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