Roles of detoxification enzymes in pyrethroid resistance of Helicoverpa armigera from Turkey

Abstracts / Toxicology Letters 180S (2008) S32–S246S169Helicoverpa armigera, cotton bollworm, is a polyphagous insect. Itis one of the most important preharvest pests for economicallyimportant crops including cotton, legumes, and vegetables.In this study, midguts ofH. armigeraobtained from Adana,Antalya, C ̧ anakkale and Mardin field populations were used. GSTactivities were determined using 1-chloro-2,4-dinitrobenzene asa substrate. Adana and Antalya field populations showed statisti-cally significant (p 0.05) compared to susceptiblepopulation, it exhibited tendency to increase.The role of cytochrome P-450 monooxygenases (CYP6B6,CYP6B7, and CYP9A12) in pyrethroid resistance developmentanalyzed using Reverse Transcriptase-PCR method. In these exper-iments, C ̧ anakkale and Mardin field populations ofH. armigerawere used. Some individuals in both field populations exhibitedslight increases in gene expressions of CYP6B7 and CYP9A12 genescompared to susceptible individuals. CYP6B6 gene expressionwas not detected in susceptible strain; nonetheless, expressionof the same gene was observed in some of the individuals fromMardin and C ̧ anakkale field populations. Increased GST activity inconjunction with activation of CYP6B6 appears to play a role in theresistance of TurkishH. armigerain monitored fieldThe performance of muon reconstruction in CMS is evaluated using a large data sample of cosmic-ray muons recorded in 2008. Efficiencies of various high-level trigger, identification, and reconstruction algorithms have been measured for a broad range of muon momenta, and were found to be in good agreement with expectations from Monte Carlo simulation. The relative momentum resolution for muons crossing the barrel part of the detector is better than 1% at 10 GeV/c and is about 8% at 500 GeV/c, the latter being only a factor of two worse than expected with ideal alignment conditions. Muon charge misassignment ranges from less than 0.01% at 10 GeV/c to about 1% at 500 GeV/c

Investigation of the role of glutathione S-transferase isozymes in pyrethroid resistance of Helicoverpa armigera in Turkey

Helicoverpa armigera, cotton bollworm, is one of the insects causing severe yield loss of economically important crops including cotton, legumes and vegetables. It has developed resistance against the pyrethroid insecticides that have been introduced into market. Resistance against pyrethroids have been reported in H. armigera populations at various parts of the world, however, except 1-chloro-2,4-dinitrobenzene substrate (CDNB), almost no any other substrates used for analysis of the role of glutathione S-transferases (GST) in pyrethroid resistance of H. armigera. In this study, in addition to CDNB, GST activities were determined using 4-nitrobenzylchloride (PNBC), 3,4-dichloronitrobenzene (DCNB) and 1,2-epoxy-3-(p-nitrophenoxy)propane (EPNP) as substrates. Midguts of H. armigera obtained from Çanakkale (n = 30) and Mardin (n = 30) field populations and a susceptible (n = 30) population obtained from Germany. GST-PNBC activities in Çanakkale and Mardin field populations showed statistically significant (p < 0.05), 2.2- and 4.8-fold increase, respectively, compared to susceptible population. Similarly, GST-DCNB activities showed statistically significant (p < 0.05), 2.0- and 4.8-fold increase in Çanakkale and Mardin field populations, respectively. However, as GST activities of both populations were determined using common substrate CDNB, only Mardin field population showed statistically significant (p < 0.05), 1.5-fold increase compared to susceptible population, no change in the GST-CDNB activity was observed in Çanakkale field population. Finally, GST activities against EPNP in Çanakkale and Mardin field populations were not detected. Thus, it may be concluded that GST isozymes using DCNB and PNBC as substrates play a role in pyrethroid resistance of Çanakkale and Mardin field populations

Note: Pyrethroid resistance and possible involvement of glutathione S-transferases in Helicoverpa armigera from Turkey

An introductory study was conducted to investigate the pyrethroid resistance of Helicoverpa armigera (Hubner) (Lepidoptera: Noctuidae) strains in Turkey, collected from cotton fields in the Adana and Antalya provinces, through two different synthetic pyrethroid insecticides: lambda-cyhalothrin and esfenvalerate. In addition, the roles of glutathione S-transferases (GSTs) in this resistance mechanism were analyzed. It was found that whereas resistance ratios for lambda-cyhalothrin (LD50 levels) were 3- and 98-fold increased in the Adana and Antalya strains, respectively, esfenvalerate ratios were 3.3- and 92.3-fold increased in the Adana and Antalya strains, respectively, with respect to the susceptible strain. Furthermore, Adana and Antalya strains showed 2.4- and 2.9-fold higher GST activities than the susceptible strain, respectively. In the Antalya field strain, the minor increase in GST activity compared with the resistance levels implies that GSTs may be not greatly involved in this resistance. It also provides evidence that they could not be the only metabolic mechanism responsible for resistance to lambda-cyhalothrin and esfenvalerate in H. armigera from Turkey

A Novel 4H-Chromen-4-One Derivative from Marine Streptomyces ovatisporus S4702T as Potential Antibacterial and Anti-Cancer Agent

Background: Marine actinomycetes are among indispensable sources of natural bioactive compounds with unique antimicrobial and anti-cancer activities. Objective: Herein, it was aimed to elucidate the bioactive potential of a marine-derived Streptomyces ovatisporus Methods: Streptomyces ovatisporus S4702T was cultured in N-Z Amine broth, and extraction was carried out using different organic solvents. Bioassay-guided purification was followed by chemical characterization using NMR and LC-MS/MS. The compound was then evaluated for its antibacterial, antioxidant and cytotoxic activities. Results: Etyl acetate extracts gave the highest antibacterial activity, and chemical characterization of this extract indicated the formula as C15H29O5N3 and the corresponding possible molecular structure as 4H-chromen-4-one derivative. It was found highly potent against Bacillus subtilis ATCC 6633 (MIC: 0.25 mu g ml-1) and Micrococcus luteus ATCC 9341 (MBC: 0.5 mu g ml-1). It has no remarkable antioxidant activity, but a higher EC50 value and less cytotoxicity against normal cells. The EC50 values of this chromen derivative were found as 9.68 mu g ml-1 for human colon carcinoma, 9.93 mu g ml-1 for human prostate adenocarcinoma and 25.5 mu g ml-1 for human embryonic kidney cells. Conclusion: Overall, the presented 4H-chromen-4-one derivative is a remarkable bioactive compound with potent antibacterial and cytotoxic activity. With its high bioactive potential, it is proposed as a good candidate in medicine.This study was supported by Ondokuz Mays University Research Fund [grant number: PYO.ZRT.1904.17.053] . The reactant and reagents for MTT and antioxidant assays were funded by Pamukkale University (PAU-BAP-2018-KRM-011) and Yuzuncu Yil University (YYU BAP Project No:2015-FBE-YL365) , respectively.Ondokuz Mays University Research Fund [PYO.ZRT.1904.17.053]; Pamukkale University [PAU-BAP-2018-KRM-011]; Yuzuncu Yil University (YYU BAP Project) [2015-FBE-YL365

Synthesis and biological activity of new indole based derivatives as potent anticancer, antioxidant and antimicrobial agents

Indoles have very critical roles to design new biologically active molecules in medicinal chemistry. They display higher biological activities or create new biological properties when compared to the other heteroaromatic compounds. In the present study, 1-ethyl-2-phenyl-3-(thiophen-2-yl)-1H-indole (3), 8-ethyl-8H-benzo[a]thieno[3,2-c]carbazole (4), 1-ethyl-2-phenyl-3-(5-(phenylethynyl)thiophen-2-yl)-1H-indole (6) and 1-ethyl-3-(furan-2-yl)-2-phenyl-1H-indole (7) are prepared via Pd-catalyzed cross-coupling reactions and iodocyclization reactions. It was determined that compound 3 and 7 were also seemed to be better drug candidates at the end of in silico evaluation. Furthermore, compound 7 provided the best antibacterial and antifungal activity against the test indicator strains. It showed a potent antifungal effect on Aspergillus niger ATCC 16404 (MIC: 1.17 mu g mL(-1); MFC: 2.7 mu g mL(-1)). In addition, while compounds 3, 6 and 7 showed significantly high molybdenum reducing activity compared to trolox, 7 exhibited almost the same antioxidant activity (EC50 = 7.1 mu M) compared to the trolox standard (EC50 = 5.07 mu M). After characterization, the cytotoxic activities of novel indoles were tested against different cancer cell lines and non-cancerous human cell line. Compound 3 and 7 had selective cytotoxic activity towards cancer cells. EC50 values of compound 3 were found to be 248.15 mu M for LnCap, 139.81 mu M for HepG2, and 164.72 mu M for the Caco-2 cell line. Similarly, The EC50 value of 7 was found as 38.725 mu M for LnCap, 70.02 mu M for HepG2, and 86.98 mu M for Caco-2, and 90.97 mu M for Hek293 cell line. Moreover, it was revealed that these two compounds showed strong apoptotic properties towards these cancer cell lines as described by image cytometry and real time PCR. Consequently, these results improved that our molecules 3 and 7 could be new candidates as anticancer agents and apoptosis inducers. (C) 2022 Elsevier B.V. All rights reserved.COST Action [CA17104]; Ondokuz Mayis University Research Fund [PYO.ZRT.1904.20.010]; YuzuncuYil University [FBA-2020-8663]The author (A. Kivrak) would like to acknowledge networking contribution by the COST Action CA17104 New diagnostic and therapeutic tools against multidrug resistant tumours. The author (A.Kurt-Kizildo.gan) would like to acknowledge Ondokuz Mayis University Research Fund [Grant No.: PYO.ZRT.1904.20.010] for supporting this study. The author (M.Konus) would like to acknowledge Van YuzuncuYil University (FBA-2020-8663) for supporting this study