Does commercial indoxacarb pose ecotoxicological consequences? Employing a multi-marker approach in the model species Theba pisana.

Indoxacarb is one of the most extensively used oxadiazine insecticides worldwide, but it may exert detrimental effects on ecosystems, population dynamics, and health. Due to the lack of knowledge on the ecotoxicity of indoxacarb, it is still challenging to assess whether this insecticide poses an ecotoxicological impact on terrestrial environments. Therefore, our study aims to provide novel data on the toxic effects of 28-day dietary exposure to commercial grade indoxacarb at two environmentally relevant concentrations, 0.02 µg/mL and tenfold (0.2 µg/mL) on the model species, Theba pisana. Their effects were studied using a multiple biomarker approach by evaluating physiological, biochemical, and histopathological responses. After 28 days of treatment, indoxacarb at both concentrations significantly reduced the food intake and growth of the treated snails. Also, it caused decreases in lipid peroxidation (LPO)  levels after 7 and 14 days of exposure, whereas an opposite effect occurred after 21 and 28 days. All treated snails were found to exhibit a lower content of glutathione (GSH) after all times of exposure. Moreover, catalase (CAT), glutathione-S-transferase (GST), and glutathione peroxidase (GPx) activities, as well as protein content (PC), were elevated in the treated snails after all time intervals. Post exposure to both realistic indoxacarb concentrations, changes in acetylcholinesterase (AChE) activity between a decrease and an increase were observed. Furthermore, indoxacarb caused histo-architectural changes in the hepatopancreas of T. pisana. Our results demonstrate that, at environmentally relevant concentrations, indoxacarb poses negative consequences for T. pisana, indicating its ecotoxicological impacts.

The impact of incorporating dried cafeteria leftover food on growing APRI rabbits productivity, profitability and meat quality.

This study was conducted to investigate the effect of dried cafeteria leftover food (DCLF) incorporation in growing APRI rabbit diets on nutrient digestibility, live body weight, body weight gain, carcass traits, meat quality, blood parameters, and economic efficiency. Thirty-six APRI rabbits (6 weeks of age), after weaning, were randomly divided into three groups (12 rabbits/group, 613 ± 5 g). During the experiment, rabbits aged 6-14 weeks participated in the experiment. An approximate isocaloric and isonitrogenous composition was achieved in three pelleted experimental diets. For the rabbit groups D1 (as the control), D2, and D3, DCLF was added at doses of 0%, 17.5%, and 35%, respectively. Digestibility trails were carried out at the end of the feeding experiment to evaluate the nutritional and feeding values of the experimental diets. To examine the characteristics of the carcasses, the quality of the meat, the histopathological analysis, and the blood plasma parameters, three rabbits were slaughtered from each group. The results showed that the feeding values (TDN and DE), which had the greatest values, as well as the digesting coefficients for dry matter, organic matter, crude fiber, and ether extract between the D1 and D3 groups were significantly different (p < 0.05). On the contrary, the curde protein, nitrogen-free extract, and digestible crude protein of the examined diets showed no signifcant differences compared with the control diet. The level of DCLF incorporation in diets significantly (p < 0.05) increased the live body weight at 14 weeks; with D3 recording the highest values (2130.9 g) when compared to the D1 and D2 groups. A similar pattern was observed for both daily increase and total body gain (6-14 weeks). Feed conversion recorded insignificant differences among the experimental diets respecting the period 6-14 weeks of age. DCLF levels had a significant effect on dressing and giblet percentages. The chemical composition and color parameters of rabbit meat were similar (p > 0.05), except for fat%, which had the highest value in the D3 group (p < 0.05) compared to the D1 and D2 groups. Economic efficiency was improved by using DLCF up to 35% in terms of gross margin and feed cost/kg gain. In conclusion, using DCLF in the feeding system of rabbits could enhance productive performance, carcass traits, meat quality, and physiological function, as well as improve economic efficiency.

Melatonin administration during the first half of pregnancy improves the reproductive performance of rabbits: Emphasis on ovarian and placental functions.

This study was designed to investigate the roles of melatonin administration during different sensitive windows of the first half of pregnancy in the function and gene expression of the ovary and placenta, hormone profile, and pregnancy outcomes in rabbits. Four equal experimental groups of 20 rabbits each were used. The first (FW), second (SW), and third (F + SW) groups comprised rabbits that orally received 0.7-mg melatonin/kg body weight during the first week, second weeks, and during both weeks of pregnancy; and the fourth group served as the control group (C). The total number of visible follicles significantly increased in all melatonin-treated groups compared with that in the C group. In all melatonin-treated groups, the number of absorbed fetuses was significantly reduced, whereas the weights of embryonic sacs and fetuses were higher than in the C group. The placenta efficiency was significantly increased in the F + SW group compared with that in the C group, followed by the SW group, whereas no significant difference in the placenta efficiency was found between the FW and C groups. Melatonin treatments significantly improved the expression of antioxidants, gonadotropin receptors, and cell cycle regulatory genes in the ovary, whereas only FW treatment upregulated steroidogenic acute regulatory gene. Compared with the C and FW groups, melatonin treatments during the SW and F + SW significantly upregulated the expression of most genes in the placenta. The concentrations of estradiol were significantly higher in the SW and F + SW groups than in the FW and C groups. The concentrations of progesterone were significantly increased in the FW group compared with those in the C and SW groups, whereas the F + SW group showed intermediate values. The litter size and weight at birth significantly increased in all melatonin-treated groups compared with those in the C group. The second week of pregnancy seems to be a sensitive window for melatonin actions during pregnancy. Thus, melatonin administration during the second week of pregnancy can be effective in improving pregnancy outcomes in rabbits.

Bio-molluscicidal potential and biochemical mechanisms of clove oil and its main component eugenol against the land snail, Theba pisana.

The land snail, Theba pisana is a serious pest that adversely affects various crops in sustainable agriculture. Essential oils and their constituents represent an environmentally sound alternative to synthetic pesticides. Our study aimed to investigate the lethal and sub-lethal toxicity of clove oil and its main component eugenol to understand the mechanisms underlying its toxic action against T. pisana. The GC-MS profile of the clove oil composition was characterized. In the laboratory experiment, LD50 of clove oil and eugenol via the contact testing were determined after 48 and 72 h. Moreover, sub-lethal effects of clove oil or eugenol on the survivors following the exposure of snails to the 25 and 50% of the LD50/48 and 72 h were evaluated through using snail tissues for biochemical measurments. The GC-MS analysis showed that eugenol (64.87%) was the major constituent present in the oil. The results also showed that LD50 values at 48 and 72 h were 2006.5 and 1493.5 µg/g b.w for oil and 239.6 and 195.3 µg/g b.w for eugenol, respectively. Compared to control, the sub-lethal effects of clove oil or eugenol at 48 and 72 h showed a significant increase in reduced glutathione (GSH) levels. Catalase (CAT) and glutathione-S-transferase (GST) activities significantly elevated in oil- or eugenol-treated snails, except at low dose after 48 h. After two exposure times, snails exposed to oil or eugenol at both sub-lethal effects had considerably higher γ-glutamyltransferase (γ-GT) and aspartate aminotransferase (AST) activities. Moreover, markedly augmentation in alkaline phosphatase (ALP) and alanine aminotransferase (ALT) activities at all exposure times, with the exception of snails treated with low dose of eugenol after 48 h was observed. Both clove oil and eugenol at the tested doses caused a significant inhibition in acetylcholinesterase (AChE) activity at two exposure times. Our findings highlight the potential of clove oil and eugenol, as an efficient natural molluscicide alternative to its synthetic counterparts for snail control.

Dietary utilization of mealworm frass in rabbit feeding regimes and its effect on growth, carcass characteristics, and meat quality.

This study aimed to shed light on the use of mealworm (Tenebrio molitor) frass (TMF) in rabbit diets and its effects on growth performance, blood profiles, rabbit meat quality, and fatty acid profiles. A total of 48 Gabali rabbits were divided equally and randomly into four groups to be fed one of four dietary treatments: a control (T0) group and three TMF groups, which included TMF meal at 1 (T1), 2 (T2), and 3 (T3) %, respectively. The rabbits were fed on isonitrogenous and isoenergetic diets for 11 weeks, and the growth performance data were recorded. Six rabbits per group were slaughtered at the end of the 11th week, then the pharmacochemical parameters and carcass traits were measured, and meat quality and fatty acid profiles were analyzed. The results indicated that the growth performance of different groups was similar (P > 0.05). The levels of globulin, glucose, and alanine transaminase (ALT) were lower in the mealworm frass groups compared with the control group. Carcass traits were not affected by experimental regimes. Fat was higher in the TMF treatment groups, while moisture was lower compared with the control group. The shear force had a lower value in the treatment groups T3 and T2 compared with the control group. The highest values of redness and chroma (color parameter) of rabbit meat were observed in the treatment groups vs. the control group. Moreover, the proportion of total saturated fatty acids in the meat of rabbits that were fed on the T2 and T3 diets was higher compared to those fed on the control (i.e., T0) and T1 diets. Furthermore, the proportion of monounsaturated fatty acid was higher in the T2, T3, and T1 groups vs. T0 rabbits, whereas the PUFA proportions were lower. It could be concluded that frass has great potential to be used as a partial substitute for rabbit diets.

Exploring the mechanisms underlying the toxicity of boric acid against the land snail, Theba pisana.

BACKGROUND: The land snail, Theba pisana, is one of the most important threats facing agriculture around the globe. Boric acid (BOA) is currently used as a safe alternative molluscicide to control land snails in sustainable agriculture, but the mechanisms of toxicity have not yet been investigated. The present study characterizes the lethal and sub-lethal (0.5 and 1 mg g-1 ) toxic effects of BOA-contaminated food for 14 days by examining physiological, biochemical and histopathological indicators in T. pisana to understand the mechanisms underlying its toxic action. RESULTS: BOA was found to be lethal against T. pisana with LC50 values of 24.7 and 8.05 mg g-1 after 3 and 7 days of exposure, respectively. BOA sublethal concentrations led to a significant reduction in food consumption and growth of snails after 14 days of exposure. BOA also caused a significant increase in testosterone levels, whereas an opposite effect was observed in estradiol levels. An increase in progesterone levels in snails in the 0.5 mg g-1 BOA group and a decrease in the 1 mg g-1 BOA group were observed after all exposure times. Moreover, the lipid peroxidation level and catalase activity were elevated, whereas acetylcholinesterase activity was inhibited in the treated snails. Alteration in glutathione-S-transferase activity was noticed after exposure to both sublethal concentrations. In addition, BOA induced histopathological alterations in the digestive gland of T. pisana. CONCLUSION: Our findings provide novel insights into how physiological, biochemical and histopathological alterations can be used to explore the mechanisms underlying BOA toxicity against snails. © 2022 Society of Chemical Industry.

Evidence for origin of lavender foal syndrome among Egyptian Arabian horses in Egypt.

BACKGROUND: Lavender foal syndrome (LFS) is a fatal hereditary condition that is inherited in an autosomal recessive pattern. This detrimental mutation is more common in Arabian foals of Egyptian origin than foals from other bloodlines. Heterozygous horses are carriers of the LFS trait and appear normal, while recessive homozygous foals died shortly after birth due to serious complications. In Egypt, in 2014, an Egyptian foal died after manifestations of neurological signs and abnormal coat colour as LFS signs. Therefore, it is important to identify LFS carriers in the population of Arabian horses in Egypt and to encourage improvement of the Arabian horse industry in Egypt by constructing a breeding system based on genetic background in order to avoid mating between carriers and reduce financial losses from deaths of affected foals. OBJECTIVES: To establish a PCR-based test for detecting the MYO5A gene mutation causing LFS in the registered Arabian horse population in Egypt prior to breeding. STUDY DESIGN: Cross sectional survey (n = 170) plus targeted sampling (n = 30). METHODS: A total of 200 samples were collected from an Arabian farm in Egypt and some of them were traced for LFS based on the farm records. The LFS genotypes were identified using the PCR-RFLP technique, fragment analysis followed by sequence analysis. RESULTS: The overall mutated allele and genotype frequencies (N/L) were 0.08 and 16%, respectively. CONCLUSION: The observed frequency of heterozygotes suggests foals affected with LFS will be produced among Arabian horses in Egypt. Therefore, screening of the entire population for this mutation should be undertaken in the breeding program.

Performance and nutrigenomics modulations in response to the inclusion of biologically treated date-palm mulch and enzyme mixture in the diets of growing rabbits.

This study was conducted to evaluate the effects of Allzyme addition on biologically-treated date-palm mulch (DPM) based diets for growing rabbits. DPM was treated by Trichoderma viride, Trichoderma reesi 230, Plorotus oysterous, and Phanaerochyte chrysosporium. Eighty rabbits were assigned to four groups: a control group, tDPM (10% tDPM inclusion of total diet), Allzyme (Allzyme supplementation), and tDPM + Allzyme (tDPM and Allzyme supplementation). The biological treatment resulted in a significant increase in crude protein and reductions in crude fiber. There was an interaction between tDPM and Allzyme at 9- and 10-week BW. The negative effects of tDPM on BW started at 8-week of age. The tDPM had unfavorable effects on slaughter and meat quality traits. The tDPM-by-Allzyme interaction affected total protein and globulin concentrations. However, blood glucose concentration was influenced by both tDPM and Allzyme. A significant tDPM effect was detected on the expression of INSR, GHSR, and IGF1 genes. However, the Allzyme effect was significant for PPARg and FASN genes. In conclusion, feeding tDPM negatively impacted rabbit's performance, however, Allzyme supplementation alleviated some of those effects. Accordingly, tDPM is recommended to be included in the diets of growing rabbits along with Allzyme supplementation.

Insights into the ecotoxicological perturbations induced by the biocide Abamectin in the white snail, Theba pisana.

Abamectin (avermectin B1, ABM) has been widely used as a biocide in agriculture, veterinary and medicine around the world. Yet, there is still a lack of knowledge about the ecotoxicological effects of ABM. In this study, we investigated the acute toxicity and sub-lethal (20% and 60% LD50) biochemical responses of ABM on the non-target land snail, Theba pisana. Mortality of snails increased with the dose increase, resulting 48 h- LD50 value of 1.048 µg/snail. The biochemical results showed a decrease in glycogen content and lipids for two sub-lethal doses after all time intervals, whereas increased the level of total proteins after exposure to 60% LD50 ABM. Overall, the tested sub-lethal doses significantly decreased the total energy reserves. ABM-exposure to snails elevated γ-Glutamyl transferase and Lactate dehydrogenase activities at all-time intervals. A significant increase of Glutathione-S-transferase activity was also recorded in snails exposed to 20% and 60% LD50 after 7 days and all time intervals, respectively. However, ABM inhibited the activity of Aspartate aminotransferase and Alanine aminotransferase after 7 days of exposure. Our investigation provides new insights into the disturbances of energy reserves and enzyme activities in T. pisana that are sensitive and may be used as biomarkers for assessing ABM toxicity.

Effect of feeding Sesbania sesban and reed grass on growth performance, blood parameters, and meat quality of growing lambs.

This study was conducted to evaluate the effects of green fodders, fresh Sesbania sesban, and reed grass, on growth performance, blood metabolites, and meat quality of growing lambs. Twenty-one male Farafra lambs (19.0 ± 1.87 kg body weight) were randomly distributed into three groups, each with seven animals. The first group was fed on 60% concentrates and 40% fresh alfalfa, and served as a control. The second and third groups were fed also on 60% concentrates plus 40% fresh Sesbania sesban and reed grass, respectively. Lambs were fed the diets until reaching the target slaughter weight of about 50.0 kg, which was obtained after a period of 215 days. Five lambs from each group were randomly selected and slaughtered at the end of the experiment. Slaughter body weight, carcass traits weight, and dressing percentage were estimated. Chemical composition and physical properties of longissimus dorsi muscle, from the animals' right side, were determined. It was found that no significant (P > 0.05) differences among groups in body weight, average daily gain, feed conversion rate, hot carcass, dressing percentage, and carcass components were observed. The forage intake of Sesbania and alfalfa tended to be higher than that of reed forage. There were no significant (P > 0.05) differences in the blood parameters among the treatments, except the urea level which was higher in Sesbania sesban group than the reed one. However, the serum urea concentration in Sesbania and reed groups was similar to that of alfalfa. Sesbania sesban and reed forages decreased (P < 0.05) the eye muscle area and shear force in lambs when compared to the control group. The longissimus dorsi muscle of the Sesbania and reed treatments was found to be numerically higher in the moisture and lower in the fat and collagen contents than the alfalfa group. Most of meat and fat color parameters were improved by feeding of Sesbania and reed forages. In conclusion, Sesbania sesban or reed grass, as unconventional forage sources, can be used as alternatives of the commonly used alfalfa feed. Moreover, these sources could enhance the meat quality of lambs and increasing the tenderness with accepted meat and fat color. So, it can be recommended to use Sesbania or reed grass forages in diets of sheep, to overcome the rising in the price or shortage in the availability of traditional green fodders.

Design, synthesis and anticancer activity of novel pyrimidine and pyrimidine-thiadiazole hybrid glycosides.

New 1,3,4-thiadiazole thioglycosides linked to substituted pyrimidines were synthesized via glycosylation of 1,3,4-thiadiazole thiol compounds. Also, novel 1,2,3-triazole derivatives linked to carbohydrate units were prepared using the standard click chemistry conditions employing the Cu(I)-catalyzed azide-alkyne cycloaddition of substituted-aryl-azides with a selection of alkyne-functionalized sugars. The chemical structures of the new derivatives were verified using various spectroscopic techniques, such as IR, 1H NMR, 13C NMR and elemental analyses. The cytotoxic activities of the prepared compounds were investigated in vitro against human liver cancer (HepG-2) and human breast adenocarcinoma (MCF7) cell lines. In addition, the biological evaluation of the new compounds involved the investigation of their effects on a human normal retinal pigmented epithelial cell line (RPE1) using the MTT assay.

Synthesis, molecular docking and antimicrobial activity of new fused pyrimidine and pyridine derivatives.

Synthesis of some new heterocyclic ring systems incorporated pyrimidine and pyridine moieties starting from 1-(furan-2-yl)-3-(thiophen-2-yl) chalcone was achieved. The structure of the new compounds was interpreted by spectral studies and ESI-MS analysis. Antimicrobial investigations of the designated compounds were performed towards some harmful pathogenic microbes. Antimicrobial tests proved that compound 11 unveiled a greater antimicrobial activity than other designed compounds. Docking of compound 11 into active site of DNA gyrase B chain displayed binding-energy of -13.05 kJ mol-1 and distance at 3.18 Ao. Furthermore, docking investigation was approved for the goal compounds into DNA gyrase B chain and exhibiting binding energy extended from -13.05 to -20.48 kJ mol-1.

One-Pot Multicomponent Synthesis and Cytotoxic Evaluation of Novel 7-Substituted-5-(1H-Indol-3-yl)Tetrazolo[1,5-a] Pyrimidine-6-Carbonitrile.

A series of novel 7-substituted-5-(1H-indol-3-yl)tetrazolo[1,5-a]pyrimidine-6-carbonitrile was synthesized via a one-pot, three-multicomponent reaction of appropriate aldehydes, 1H-tetrazole-5-amine and 3-cyanoacetyl indole in catalytic triethylamine. The cytotoxic activity of the new synthesized tetrazolopyrimidine-6-carbonitrile compounds was investigated against HCT-116, MCF-7, MDA-MB-231, A549 human cancer cell lines and one human healthy normal cell line (RPE-1) using the MTT cytotoxicity assay. Compounds 4h, 4b, 4c, 4i and 4a showed potent anticancer activities against human colon cancer. Additionally, all the compounds showed potent anticancer activities on human lung cancer.

Ecotoxicological biomarkers as investigating tools to evaluate the impact of acrylamide on Theba pisana snails.

Acrylamide (ACR) is a widespread industrial chemical with recognized adverse effects not only to humans but to other organisms in the environment as well. In the present study, the ecotoxicological effects of dietary exposure to sublethal concentration (1/20 LC50) of ACR on the land snail, Theba pisana after 2 weeks of exposure and 1-week recovery with respect to oxidative stress parameters; lipid peroxidation (LPO), reduced glutathione (GSH), catalase (CAT), and glutathione-S-transferase (GST), cytogenetic parameter; deoxyribonucleic acid (DNA) content, as well as immunological parameters; cell death, phagocytosis, lysosomal membrane stability (LMS), lectins, superoxide anion (O2-) generation, phenoloxidase (PO), peroxidase (POD), and hemocyanin (Hc) were examined. The results showed that ACR significantly increased LPO level and the activity of CAT and GST, cell death, and Hc level, whereas a significant decline in DNA and GSH contents, phagocytic activity, LMS, lectins, O2- generation, POD, and PO activities compared to the controls after 2-week exposure was observed. After 1-week recovery, most of the tested parameters in exposed snails were permanent and not reversible to the control levels. This study suggests that the tested multiple parameters of T. pisana species may be used as biomarkers of ACR exposure. Besides, T. pisana snails could be used as a good sentinel organism for ACR exposure in pollution monitoring studies.

Physiological traits of land snails Theba pisana as simple endpoints to assess the exposure to some pollutants.

In the current study, the toxicity bioassay of three pollutants abamectin (ABM), thiamethoxam (TMX), and acrylamide (ACR) against land snails Theba pisana was measured. Also, the ecotoxicological effects of dietary exposure to sublethal concentration (1/20 LC50) of these pollutants for 2-week exposure and 1-week recovery on some physiological endpoints evaluated as feeding activity, growth response, and carbonic anhydrase activity as a marker in charge of shell formation and seromucoid level as a marker in charge of mucus synthesis of the snails were studied. The results exhibited that the 48-h LC50 values were 0.91, 313.8, and 45.7 µg/g dry food for ABM, TMX, and ACR, respectively. The sublethal concentrations of these pollutants in the diet after 2-week exposure were found to reduce the food consumption and inhibit growth rate of the snails. Also, the data illustrated that carbonic anhydrase activity was significantly decreased. On the other hand, there was a significant increase in the seromucoid level as a marker responsible for mucus synthesis in ABM- and TMX-exposed snails, while ACR showed significantly decreased level when compared to control. After 1-week recovery, the tested endpoints of treated snails were slightly repaired but still less than that of the untreated animals. The overall outcome of this investigation suggests the utility of this animal as a good bioindicator organism for ABM, TMX, and ACR exposure in pollution monitoring studies.

Synthesis and Antitumor Activity of Novel [1,2,4,5]-tetrazepino[6,7-b] indole Derivatives: Marine Natural Product Hyrtioreticuline C and D Analogues.

BACKGROUND: Several biologically active indole alkaloids have been isolated from marine organisms over the previous few years. Many scientsts interested in synthesis of the marine azepinoindole alkaloids due to their wide range of bioliogical activies. OBJECTIVE: We interested herein to synthesize a new series of some analogues of new naturally occurring azepinoindole alkaloids. METHOD: A novel series of [1,2,4,5]tetrazepino[6,7-b]indoles, Marine natural product Hyrtioreticuline C and D analogues, were synthesized via the reaction of 3-hydrazonoindolin-2-one with hydrzaonoyl chlorides in basic medium. RESULTS: The spectral data of the products proved their structure. All new derivatives were tested against two carcinoma cell lines ((A-549 & HepG2)) in comparison with the well-known anticancer standard drug (cisplatin) and two derivatives from the tested compounds showed activity more potent than the reference drug. CONCLUSION: We succeeded in synthesis of new antitumor active azepinoindole alkaloids.

Laparoscopic pyelolithotomy in selected patients with ectopic pelvic kidney: a feasible minimally invasive treatment option.

BACKGROUND AND PURPOSE: Ectopic pelvic kidney is a rare congenital anomaly. It carries more risks for obstruction and stone formation than a normal located kidney. The treatment of renal stones in these patients is challenging. We present our experience with laparoscopic pyelolithotomy for treatment of selected patients with large and multiple renal stones in ectopic pelvic kidneys. PATIENTS AND METHODS: After insertion of a ureteral catheter, pneumoperitoneum was achieved by Veress needle, and the kidney was exposed. The renal pelvis was identified, dissected, and opened. The stones were extracted using laparoscopic forceps. The rigid nephroscope was used to extract any caliceal stones. The renal pelvis was sutured, and the stones were removed from the peritoneal cavity. The procedure was concluded after placement of an intraperitoneal drain. RESULTS: A total of 11 patients with large renal pelvic and/or multiple stones underwent laparoscopic transperitoneal pyelolithotomy. A transmesenteric approach was used in eight patients while the colon was mobilized off the kidney in three patients. All stones were removed except one that needed Double-J stent placement and one session of shockwave lithotripsy. After one auxiliary procedure, the stone-free rate was 100%. There were no major intraopertive or postoperative complications. Within a mean follow-up period of 23 months, no stone recurrence occurred. CONCLUSIONS: Laparoscopic pyelolithotomy for large and multiple stones in ectopic pelvic kidneys is a feasible minimally invasive treatment option. The technique allows removal of all the stones without fragmentation, which may decrease the possibility for rapid stone recurrence.

Structure-based design of benzimidazole sugar conjugates: synthesis, SAR and in vivo anti-inflammatory and analgesic activities.

A series of 2-methyl-N-substituted-benzimidazoles, bearing hydroxypyrrolidinon-5-yl or hydroxypyrrolidin-2-yl, 2,3:5,6-di-O-isopropylidene-alpha-D-mannofuranoside, 2,3,5,6-tetrahydroxy-alpha-D-mannofuranoside, 1:2,5:6-di-O-isopropylidene-alpha-D-gluco-furanose,3-O-benzyl-6,7-dideoxy-1:2-O-isopropylidene-alpha-D-xylo-heptofuranos-5-ulose, 3-O-benzyl-6,7-dideoxy-1,2-dihydroxy-alpha-D-xylo-heptofuranos-5-ulose, 1,2,5,6-tetrahydroxy-alpha-D-glucofuranose sugar moieties, were obtained in good yields from 2-methyl N-(trichloroacetamidomethyl)benzimidazole as a donor and carbohydrate residues as acceptor precursors in the presence of catalytic amount of trimethylsilyl trifluoromethanesulfonate (TMSOTf) as Lewis acid. Compounds 6, 7, 10, 13, 15, and 16 showed significant anti-inflammatory and analgesic activities.

Neuropathological effect of carbamate molluscicides on the land snail, Eobania vermiculata.

The present study was designed to investigate the neuropathological effect of the two carbamate pesticides: methomyl and methiocarb on the neurons of the buccal ganglia in the land snail Eobania vermiculata using topical application and baiting technique. Their in vivo effects on acetylcholinesterase (AChE, EC 3.1.1.7) activity were also investigated. Sublethal dose and concentration (1/4 LD(50) and 1/4 LC(50)) of both pesticides were used, and the experiment lasted for 14 days. Histopathological and ultrastuctural alterations in the buccal ganglia were more obvious after the baiting technique treatment than after the topical application method, and methomyl was found to be more toxic than methiocarb. These alterations included shrinkage of the perikarya of neurons, increased cytoplasmic basophilia, and extreme indentation of the plasma membrane. In addition, the nuclei appeared karyolitic, eccentric, and highly shrunken with an irregular nuclear envelope. The most outstanding symptom observed after topical application of methiocarb was a highly vacuolated cytoplasm with a peripheral increase in electron density associated with dense accumulations of free ribosomes. On the other hand, an increased number of lysosomes and autophagosomes were observed after topical application of methomyl. Mitochondrial damage, increased number of lipid droplets, and myelin figures were frequently observed in ganglia treated with either methomyl or methiocarb. Moreover, it was noticed that both compounds induced reductions in AChE activity. However, methomyl exhibited more potency in reducing AChE activity than methiocarb.

Synthesis and pharmacological evaluation of 2-substituted benzo[b]thiophenes as anti-inflammatory and analgesic agents.

An efficient method for trapping isocyanate 4, generated from the Curtius rearrangement, with ethyl alcohol to afford the carbamate 5 is reported. 5-Nitrobenzo[b]thiophene-2-carboxylic acid 1 is converted to the corresponding hydrazide 2 by the reaction with hydrazine hydrate and then to the azide 3 with nitrous acid, followed by thermal rearrangement, cooling, and trapping in one pot reaction. The carbamate 5 is treated with hydrazine hydrate to afford the desired, Zileuton analogue, 4-(5-nitrobenzo[b]thiophene-2-yl)semicarbazide 6. Also the reactivity of hydrazide 2 towards some carboxyaldehydes and phenylisothiocyanate afforded the corresponding carbohydrazides 7, 8 and phenylthiosemicarbazide 9, respectively. Compounds 9, 2 and 6, respectively, were more potent as anti-inflammatory and anti-nociceptive agents.