The metabolites of tebufenozide, a model compound, formed by the yeast-expressed human CYP3A4 and CYP2C19 were identified to clarify the substrate recognition mechanism of the human cytochrome P450 (CYP) isozymes. We then determined whether tebufenozide metabolites may be predicted in silico. Hy...
Adult development and production of up to 400 eggs within the pupal case of female silkmoths are both dependent on 20-hydroxyecdysone (20E), the steroid hormone of insects. When adult development was initiated with tebufenozide, the non-steroidal ecdysteroid agonist, instead of 20E, full develop...
The novel nonsteroidal ecdysone agonist tebufenozide is capable of controlling a wide range of lepidopteran pests. However its intensive use in vegetables has raised concerns towards the safety of food and environment. Here, we developed an easy and reliable method to analyze tebufenozide in cab...
Tebufenozide is a non-steroidal insect growth regulator and is extensively used to control pests, although it is considered to be safe for mammals and environmentally friendly. However, previous studies have found that tebufenozide is cytotoxic to man, although the exact mechanism remains elusiv...
Tebufenozide, a newly-developed nonsteroidal ecdysone agonist, is in pre-regulation phase (before approval for use) on stem lettuce in China. Aiming at the safe application of tebufenozide, the dissipation and terminal residue trials on stem lettuce were performed under good agricultural practic...
Tebufenozide is considered an environmentally friendly pesticide due to its specificity on target insects, but the effects on human are well studied. Studies on the toxicity of tebufenozide at molecular and cellular level is poorly understood. The present study reveals non-selective cytotoxic ef...
The velvetbean caterpillar, Anticarsia gemmatalis Hübner (Lepidoptera: Noctuidae), is an important soybean pest in the Americas. Tebufenozide, a novel nonsteroidal ecdysone agonist is used to control this pest. Bioassays were conducted to assess tebufenozide toxicity and their ultrastructural e...
Based on the confirmation of asymmetrical cross-resistance between abamectin and tebufenozide in Plutella xylostella, the present work proved that the cytochrome P450 monooxygenase plays a decisive role in cross-resistance, and the expression of various cytochrome P450 (CYP450) genes in differen...
3-Deoxysappanchalcone (3-DSC), isolated from Caesalpinia sappan (Leguminosae), is a chalcone that exerts a variety of pharmacological activities. In the present study, we demonstrated that 3-DSC exerts anti-inflammatory activity in murine macrophages by inducing heme oxygenase-1 (HO-1) expressio...
BackgroundColorectal cancer is one of the most common causes of cancer death worldwide. Unfortunately, chemotherapies are limited due to many complications and development of resistance and recurrence. The T-lymphokine-activated killer cell-originated protein kinase (TOPK) is highly expressed an...
The goal of this study is to find out the exhaust emissions differences produced by different kinds of fatty acid methyl esters (FAME) derived from used cooking oils and animal fats, as well as the importance of the purification step in exhaust emissions production. A total of 120 L of waste veg...
The organocatalyzed enantioselective synthesis of a series of chiral 2-amino-5,6,7,8-tetrahydro-5-oxo-4H-chromene-3-carbonitriles was achieved using bifunctional squaramides as the catalysts. The tandem Michael addition–cyclization reaction of cyclohexane-1,3-diones and benzylidenemalononitrile...
A series of benzofuran-based N-benzylpyridinium derivatives 5a–o were designed and synthesized as novel AChE inhibitors. The synthetic pathway of the compounds involved the preparation of 4-(benzofuran-2-yl)pyridine intermediates via the reaction of different salicylaldehyde derivatives and 4-(...
Danofloxacin, a fluoroquinolone derivative antibiotic, was synthesized, successfully labeled with technetium-99m and formulated for the development of a potential diagnostic imaging agent of the bacterial infection and inflammation with higher efficiency than that of the commercially available 9...
Danofloxacin (DAN) is one of the Fluoroquinolone drugs (FQs) that has been widely used in the control and prevention of bacterial infectious disease in animal production. Most of the FQs have an obvious protective effect against lipopolysaccharide (LPS) induced Immune stress. However, the effect...
Residue depletion of danofloxacin was investigated in European sea bass after a multiple (5 days) in-feed administration of danofloxacin mesylate (10 mg/kg bw per day) under experimental field conditions at water temperature of 16 °C and 27 °C. Ten fish per sampling point were examined during ...
Street dust samples from Durgapur, the steel city of eastern India, were collected from five different land use patterns, i.e., national highways, urban residential area, sensitive area, industrial area and busy traffic zone during summer, monsoon, and winter to analyze the pollution characteris...
SummaryIntroductionTriazolam belongs to the group of benzodiazepines and may have side effects on the respiratory system which include not only respiratory depression, but also transient benign non cardiac pulmonary edema.
ObjectiveMost previous studies have concluded that decreased cognitive function and performance due to ultra-short acting hypnotics do not persist after 6–9 h post-administration. This study examined the effects of ultra-short acting hypnotics on cognitive function and performance 12 h after ad...
A series of pyridine derivatives in the C-region of N-((6-trifluoromethyl-pyridin-3-yl)methyl) 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides were investigated as hTRPV1 antagonists. The SAR analysis indicated that 6-difluorochloromethyl pyridine derivatives were the best surrogates of the...
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