In Vitro and In Silico Evaluations of the Antileishmanial Activities of New Benzimidazole-Triazole Derivatives.

Benzimidazole and triazole rings are important pharmacophores, known to exhibit various pharmacological activities in drug discovery. In this study, it was purposed to synthesize new benzimidazole-triazole derivatives and evaluate their antileishmanial activities. The targeted compounds (5a-5h) were obtained after five chemical reaction steps. The structures of the compounds were confirmed by spectral data. The possible in vitro antileishmanial activities of the synthesized compounds were evaluated against the Leishmania tropica strain. Further, molecular docking and dynamics were performed to identify the probable mechanism of activity of the test compounds. The findings revealed that compounds 5a, 5d, 5e, 5f, and 5h inhibited the growth of Leishmania tropica to various extents and had significant anti-leishmanial activities, even if some orders were higher than the reference drug Amphotericin B. On the other hand, compounds 5b, 5c, and 5g were found to be ineffective. Additionally, the results of in silico studies have presented the existence of some interactions between the compounds and the active site of sterol 14-alpha-demethylase, a biosynthetic enzyme that plays a critical role in the growth of the parasite. Therefore, it can be suggested that if the results obtained from this study are confirmed with in vivo findings, it may be possible to obtain some new anti-leishmanial drug candidates.

The effects of taurine ingestion on anaerobic and physiological performance in female rugby players.

The purpose of this study was to investigate the acute effect of low, moderate, or high doses of taurine on anaerobic and physiological performance in female rugby players. A total of 16 sub-elite female rugby athletes (21.3 ± 1.5 yr, 168.0 ± 4.9 cm, 62.1 ± 3.5 kg mean ± SD) participated in this research. Following familiarization, participants attended 4 successive tests separated by 72 h in a randomized, counter-balanced, crossover research design. Following an over night fast, participants completed a 5-min 60 Watt warm-up followed by a 30-s Wingate anaerobic test on a cycle ergometer after ingestion of either 2 g taurine (LOWTAU), 4 g (MODTAU), 6 g (HIGHTAU) or placebo (PLA) 1 h before the test. Peak (PP) and mean power (MP) along with heart rate (HR), rating of perceived exertion (RPE), capillary lactate and blood glucose were measured. LOWTAU did not affect PP, MP, HR, lactate and glucose compared to PLA (p > 0.05), while MODTAU improved MP and HIGHTAU improved PP and MP compared to PLA and LOWTAU (p < 0.05). MODTAU and HIGHTAU had little effect on HR, blood lactate and glucose (p > 0.05). A single dose of taurine (MODTAU or HIGHTAU) 1 h prior to competition or training would provide an ergogenic effect on subsequent power output.

Eight Days of L-Citrulline or L-Arginine Supplementation Did Not Improve 200-m and 100-m Swimming Time Trials.

The effects of L-citrulline or L-arginine supplementation on exercise performance are equivocal, and the effects on swimming performance are unclear. We aimed to assess whether 8-day supplementation with L-arginine or L-citrulline supplementation would improve 200 m and 100 m freestyle swimming time-trial performances. After the baseline trial (first visit), in a double-blind, randomised design, 15 trained/developmental (5 females) swimmers and triathletes were assigned to three groups and underwent an 8-day supplementation period, with a daily dose of either 8 gr L-arginine (Arg, n = 5) or L-citrulline (Cit, n = 5) or placebo (Pla, n = 5). On day 9, participants completed experimental trial (second visit). In each trial, after blood sampling, participants performed both 200 m and 100 m freestyle swimming time-trials, with 30 min recovery between trials. Plasma nitric oxide (NOx) and blood lactate concentrations (BLa) were collected immediately before and after 200 m and 100 m TTs, respectively. No significant difference was observed in NOx between groups (p = 0.201). There was no significant difference in 200 m (p = 0.226) and 100 m swimming time-trials (p = 0.993) between groups. There was a main effect of time on BLa concentration (p < 0.001), but no trial × group (p = 0.243) and trial × lactate × group interaction effect (p = 0.276) was present. Furthermore, 8-day either L-citrulline or L-arginine supplementation did not enhance middle (200 m) and short-distance (100 m) swimming performance in trained/developmental swimmers and triathletes. These findings do not support the use of L-citrulline or L-arginine supplementation as ergogenic aids for swimming performance.

Carbohydrate Mouth Rinse Increases High but Not Low Intensity Repetitions to Failure in Resistance-Trained Males.

Carbohydrate mouth rinsing (CMR) has been shown to enhance exercise performance. However, the influence of CMR on repetitions to failure with different intensities (40% or 80% of 1 RM) is unknown. Therefore, the purpose of this study was to examine the effects of a 6% CMR solution on muscular endurance assessed at 40% and 80% of 1 RM in resistance-trained males. Sixteen resistance-trained males (age: 25 ± 3 years, height: 182 ± 6 cm, body mass: 86 ± 3 kg, body fat: 16 ± 3%, bench press 1 RM: 106 ± 16 kg, resistance training experience: 5 ± 1 years) completed four conditions in random order. The four conditions consisted of ten seconds of mouth rinsing with 25 mL solutions containing either maltodextrin or placebo (sweetened water) prior to performing a bench press muscular endurance test at either 40% of 1 RM or 80% of 1 RM. Total repetitions, heart rate (HR), ratings of perceived exertion (RPE), glucose (GLU) and felt arousal (FA) were recorded for each condition. There was a significant condition by intensity interaction (p = 0.02). CMR significantly increased total repetitions compared with placebo at the higher intensity (80% of 1 RM; p = 0.04), while there was no effect at the lower intensity (p = 0.20). In addition, HR, RPE, GLU and FA did not differ between conditions or across intensities (p > 0.05). In conclusion, CMR-enhanced muscular endurance performed at higher but not lower intensities.

The Acute Effects of Normobaric Hypoxia on Strength, Muscular Endurance and Cognitive Function: Influence of Dose and Sex.

The aim of this study was to examine the acute effects of different levels of hypoxia on maximal strength, muscular endurance, and cognitive function in males and females. In total, 13 males (mean ± SD: age, 23.6 ± 2.8 years; height, 176.6 ± 3.9 cm; body mass, 76.6 ± 2.1 kg) and 13 females (mean ± SD: age, 22.8 ± 1.4 years; height, 166.4 ± 1.9 cm; body mass, 61.6 ± 3.4 kg) volunteered for a randomized, double-blind, crossover study. Participants completed a one repetition strength and muscular endurance test (60% of one repetition maximum to failure) for squat and bench press following four conditions; (i) normoxia (900 m altitude; FiO2: 21%); (ii) low dose hypoxia (2000 m altitude; FiO2: 16%); (iii) moderate dose hypoxia (3000 m altitude; FiO2: 14%); and (iv) high dose hypoxia (4000 m altitude; FiO2: 12%). Heart rate, blood lactate, rating of perceived exertion, and cognitive function was also determined during each condition. The one repetition maximum squat (p = 0.33) and bench press (p = 0.68) did not differ between conditions or sexes. Furthermore, squat endurance did not differ between conditions (p = 0.34). There was a significant decrease in bench press endurance following moderate (p = 0.02; p = 0.04) and high (p = 0.01; p = 0.01) doses of hypoxia in both males and females compared to normoxia and low dose hypoxia, respectively. Cognitive function, ratings of perceived exertion, and lactate were also significantly different in high and moderate dose hypoxia conditions compared to normoxia (p < 0.05). Heart rate was not different between the conditions (p = 0.30). In conclusion, high and moderate doses of acute normobaric hypoxia decrease upper body muscular endurance and cognitive performance regardless of sex; however, lower body muscular endurance and maximal strength are not altered.

The Effects of 15 or 30 s SIT in Normobaric Hypoxia on Aerobic, Anaerobic Performance and Critical Power.

Sprint interval training (SIT) is a concept that has been shown to enhance aerobic-anaerobic training adaptations and induce larger effects in hypoxia. The purpose of this study was to examine the effects of 4 weeks of SIT with 15 or 30 s in hypoxia on aerobic, anaerobic performance and critical power (CP). A total of 32 male team players were divided into four groups: SIT with 15 s at FiO2: 0.209 (15 N); FiO2: 0.135 (15 H); SIT with 30 s at FiO2: 0.209 (30 N); and FiO2: 0.135 (30 H). VO2max did not significantly increase, however time-to-exhaustion (TTE) was found to be significantly longer in the post test compared to pre test (p = 0.001) with no difference between groups (p = 0.86). Mean power (MPw.kg) after repeated wingate tests was significantly higher compared to pre training in all groups (p = 0.001) with no difference between groups (p = 0.66). Similarly, CP was increased in all groups with 4 weeks of SIT (p = 0.001) with no difference between groups (p = 0.82). This study showed that 4 weeks of SIT with 15 and 30 s sprint bouts in normoxia or hypoxia did not increased VO2max in trained athletes. However, anerobic performance and CP can be increased with 4 weeks of SIT both in normoxia or hypoxia with 15 or 30 s of sprint durations.

Infections of Larval Stages of Dicrocoelium dendriticum and Brachylaima sp. in Brown Garden Snail, Helix aspersa, in Turkey.

The aim of this study was to determine the presence and prevalence of larval stages of Dicrocoelium dendriticum and Brachylaima sp. in the first intermediate host, a species of land snail, Helix aspersa, in Turkey. A total of 211 snails were collected in April-May 2014 from pastures in Mersin District. Larval stages of D. dendriticum were identified under a light microscope. Hepatopancreas from naturally infected H. aspersa snails were examined histologically. The prevalence of larval stages of D. dendriticum and Brachylaima sp. in H. aspersa snails was found to be 2.4% and 1.9%, respectively, in Mersin, Turkey. Cercariae were not matured in sporocysts at the beginning of April; however, it was observed that cercariae matured and started to leave sporocysts by early-May. Thus, it was concluded that H. aspersa acts as an intermediate host to D. dendriticumin and Brachylaima sp. in Mersin, Turkey. A digenean trematode Brachylaima sp. was seen for the first time in Turkey.

[Seroprevalence of Toxoplasma gondii in Pirlak sheep in the Afyonkarahisar Province of Turkey]. / Afyonkarahisar ilinde Pirlak irki koyunlarda Toxoplasma gondii'nin seroprevalansi.

OBJECTIVE: This study was carried out between June-December 2008 to determine the prevalence of toxoplasmosis in Pirlak sheep in the Suhut district of Afyonkarahisar. METHODS: Blood samples technically collected from 123 sheep older than one year old and 63 sheep younger than one year old were tested for Toxoplasma gondii antibodies using the Sabin- Feldman dye test. RESULTS: Out of the 186 sera examined, 184 (98.92%) were seropositive at different dilutions (84 samples at 1/16, 79 at 1/64 and 21 at 1/256). The seroprevalence was 99.19% for sheep above 1 year old and 98.41% for sheep under 1 year old. CONCLUSION: We believe that this study carried out on Pirlak sheep would be useful for other studies on the effect of parasitism on the economy.

Prevalence and economic significance of bovine hypodermosis in Afyonkarahisar province of Turkey.

This study was carried out to investigate the prevalence and economic losses due to in cattle of hypodermosis between May 2008 and April 2009 in Afyonkarahisar province of Turkey. A total of 6,598 cattle-3,498 in pasture and 3,100 in slaughterhouse-were examined for hypodermosis. One hundred ninety-five out of 6,598 cattle (2.96%) were found positive. Concerning this infestation rate, the prevalence of hypodermosis in field was 5.3%, whereas the prevalence was 0.3% in slaughter house. Hypoderma bovis and Hypoderma lineatum were recorded in slaughter house. First-stage Hypoderma spp. larvae weren't found in cattle organs in slaughterhouse. The annual economic loss on skins is estimated to be about 18,288 TL (currency exchange rate is 1 USD:1.499 TL).

Current status of ruminant theileriosis and its economical impact in Turkey.

The diagnosis of ruminant theileriosis in Turkey is based on microscopical examination of thin blood and lymph smears, serology, traditional staining methods of the salivary glands of ticks and molecular techniques. Although some investigators reported that T. mutans was found in cattle with microscopic examination (7.4%-36.7%) and experimental study, they did not detect this parasite using molecular techniques. On the other hand, the prevalence of T. buffeli/orientalis was found to differ between 0.9% and 13.6% using molecular techniques in different regions of Turkey. Tropical theileriosis caused by T. annulata is widespread, and constitutes a major health and management problem in cattle in Turkey. The economic losses resulting from the tropical theileriosis were estimated to be US $598,000, $133,000 and $130,000 in the endemic stable zones of Turkey. Microscopic prevalence of T. annulata has been reported to be between 0% and 60.5% in different parts of Turkey. The serologic prevalence of T. annulata was found to differ between 1.8% and 91.4% by IFAT. In subsequent studies, the prevalence of this parasite was found to differ between 15.4% and 61.2% by molecular techniques. Clinical cases of ovine theileriosis have not been documented in Turkey. The prevalence of T. ovis/recondita was found to differ between 0% and 41.3% by microscopic examination of thin blood smears and its seroprevalence was found to be between 8.2% and 63.2% by IFAT. This parasite has also been reported to be present between 41.8% and 67.7% by molecular techniques.

[Genital myiasis in a cat]. / Bir Kedide Genital Myiasis Olgusu.

Genital myiasis was diagnosed in a cat which was brought to the clinic for therapy six days after giving birth. Ten dead larvae were collected from its genital organs. During the microscopic examination, the larvae were identified as the third stage larva of Lucilia sericata.

[Examination of helminth contaminated wastewaters used for agricultural purposes in Afyonkarahisar]. / Afyonkarahisar'da tarimsal amaçli kullanilan atik sularin helmint kontaminasyonu yönünden incelenmesi.

This research was performed in order to examine helminth contaminated wastewaters used in agriculture in Afyonkarahisar. Ten rural areas were selected that used water for agricultural purposes from a creek contaminated with human and animal wastes. Between September 2004 and August 2005, these areas were visited once every two weeks, and a total of 240 water samples were collected. Out of untreated water samples, 32 samples (26.70%) had helminth eggs, whereas there were neither helminths nor developmental stages of helminths (p < 0.001) in treated water samples. Cestode eggs were seen in 10.00% of untreated water samples and nematode eggs were seen in 16.70%. Out of the helminth eggs, 13 (40.60%) were hookworm eggs; 6 (18.75%), Taenia spp.; 5 (5.60%), Ascaris lumbricoides; 3 (9.40%), Hymenolepis diminuta; 3 (9.40%), H. nana; and 2 (6.25%), Toxocara spp. In conclusion; the creek was found to be contaminated by helminths originating from human and animal wastes in Afyonkarahisar. This type of water presents a risk for human and animal health and contaminated waters, therefore, should be avoided in irrigation of vegetables and fruit consumed raw.

Prevalence of coccidia in beef cattle in western Turkey.

A total of 504 bovine faecal samples collected from intensively managed beef farms in Afyon province of Turkey were examined to determine the types and prevalence of coccidian parasites present. Coccidian oocysts were found in 20.04% of all the samples examined by sucrose-flotation. The species detected and their prevalence were Eimeria bovis (34.55%), E. auburnensis (23.03%), E. canadensis (14.55%), E. brasiliensis (10.91%), E. zuernii (6.67%), E. bukidnonensis (3.03%), E. cylindrica (2.42%), E. ellipsoidalis (1.21%), E. illinoisensis (1.21%), E. alabamensis (1.21%) and Isospora sp. (1.21%). Mixed infections of two to four species were found in 43.6% of the animals. The overall prevalence of coccidial oocysts in faecal samples was 27.23% for calves, 15.65% for cows. Linear regression analysis showed that there is a significant reduction in the OPG (the number of oocysts per gram of feces) levels (P<0.05) in cows infected with Eimeria. No cases of clinical coccidiosis were observed in this survey.

[Gastrointestinal nematodes and their seasonal distribution in cattle raised in central Afyonkarahisar, Turkey]. / Afyonkarahisar il merkezinde yetistirilen sigirlarin mide bagirsak nematodlari ve mevsimsel dagilimlari.

This study was conducted during the period of September 2004-August 2005 in two villages with simple raising of cattle located in the center of the Afyonkarahisar province. Fecal samples collected from 985 cattle and the gastrointestinal tracts of 24 cattle were inspected. Strongyle types of eggs were observed in 26.39% of the fecal samples. The infection was found to be less prevalent in the spring (22%) and most prevalent in autumn (32.53%). The genus of larvae observed in fecal cultures were Haemonchus spp. 25.25%, Trichostrongylus spp. 23.71%, Nematodirus spp. 16.49%, Ostertagia spp. 10.30%, Cooperia spp. 8.76%, Bunostomum spp. 6.70%, Oesophagostomum spp. 6.18% and Chabertia ovina. 2.57%. H. contortus and Oesophagostomum venulosum (20.83%), O. radiatum (16.66%), Cooperia onchophora and Ostertagia ostertagi (8.3%), O. trifurcata, C. punctata and Chabertia ovina (4.16%) were found during inspections of the gastrointestinal tracts which were performed in order to determine the infective species. Based on these results, it was concluded that there are infections caused by gastrointestinal nematodes in this province but the severity of the infection is low and the seasons with highest infection risk are late spring and autumn.

The resistance of nematode parasites in sheep against anthelmintic drugs widely used in Western Turkey.

This study was carried out in seven sheep herds infected by gastro-intestinal nematodes in the Afyonkarahisar district (Western Turkey) from June to July 2005. Sixty sheep in each herd were distributed into 3 groups as anthelmintic treatment groups along with a control group containing 15 animals. The anthelmintic groups were treated with albendazole (7.5 mg/kg BW), oxfendazole (7.5 mg/kg BW)-oxyclosanide (15 mg/kg BW) combination and ivermectin (0.2 mg/kg BW-injectable). The faecal samples were collected before treatment and after 10 days of treatment. Nematode egg counts per gram of faeces (EPG) were examined in the faecal samples using the McMaster technique. To identify the genus, the faecal samples were cultured. The faecal egg count reduction test (FECR) was employed to determine the resistance. In ivermectin treated groups, the FECR% values and the lower confidence limits were estimated as A: 68.57(14.77), B: 46.42(22.47), C: 84.41(35.38), D: 95.23(61.64), E: 97.14(76.94), F: 65.21(80.46) and G: 91.66(31.69), respectively. In the A, B, C, F and G herds, statistical analysis showed that the FECR% values were less then 95% and the estimated lower confidence limits were less then 90%. In all herds, albendazole treated, oxfendazole-oxyclosanide treated and control group, there were no eggs in the feacal samples. In these groups, the FECR% values were 100. In ivermectin treated groups, the third stage larvae from the genera Haemonchus, Oesophagostomum, Trichostrongylus, Cooperia, Nematodirus and Ostertagia were detected in coprocultures before treatment and the larvae from the genera Haemonchus and Oesophagostomum were detected in post-treatment coprocultures in the resistant herds. In conclusion, there was no evidence of resistance in sheep gastro-intestinal nematodes against albendazole and oxfendazole-oxyclosanide; in contrast, the resistance against ivermectin was detected in five sheep herds in the Afyonkarahisar district.