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Environmental toxicants on Leydig cell function
Published in C. Yan Cheng, Spermatogenesis, 2018
Leping Ye, Xiaoheng Li, Xiaomin Chen, Qingquan Lian, Ren-Shan Ge
Many azole chemicals, such as prochloraz, epoxiconazole, tebuconazole, and iprodione are used for fungicides to protect plants in the agriculture field. Prochloraz is classified as an antiandrogen. Maternal exposure to prochloraz caused malformation of male reproductive tracts in fetal male rats and reduced steroidogenesis in the testis.215 Prochloraz decreased serum testosterone levels and delayed puberty in males during pubertal exposure.216 Exposure to prochloraz (50 and 150 mg/kg BW/day) to rats from gestational day 7 to postnatal day 16 inhibited testicular testosterone levels but increased progesterone levels without affecting Cyp17a1, suggesting a direct inhibition of CYP17A1 in the Leydig cells.217 Indeed, prochloraz inhibited rat testicular CYP17A1 activity with Ki around 1 μM.215 Using human adrenal H295R cells, prochloraz also concentration-dependently inhibited human CYP17A1 activity,218 and the inhibition was more selective since it did not inhibit another CYP enzyme CYP11B1, which is required for glucocorticoid biosynthesis.218
Use of Critically Important Antimicrobials in Food Production
Published in M. Lindsay Grayson, Sara E. Cosgrove, Suzanne M. Crowe, M. Lindsay Grayson, William Hope, James S. McCarthy, John Mills, Johan W. Mouton, David L. Paterson, Kucers’ The Use of Antibiotics, 2017
Triazoles (difenoconazole, tebuconazole, and propiconazole) are used for the control of fungal diseases on lawns (Fusarium patch, anthracnose, and dollar spot) and ornamental plants (mildew and rusts). Tebuconazole and propiconazole are used to prevent wood decay by some fungi (e.g. Gloeophyllum trabeum and Poria spp.). They can be used in combination with copper carbonate and are the main components of copper organic wood preservatives used in industry to pressure-treat timbers, such as those used in fencing, cladding, plywood, roofing, and garden decking. Copper triazole combination preservatives are widely marketed in North America and across Europe. Wood preservatives containing propiconazole and tebuconazole are also available for domestic use. Propiconazole is registered for use in adhesives, paints, leather, paper, and textiles and is available in the UK as the active ingredient in an antifouling agent, biocidal paints and surface biocides (U.S. Forest Service, 2016; U.S. EPA, 2006; ECDC, 2013; Eurostat, 2001).
Application of the Mannich reaction in the structural modification of natural products
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2023
Miao-Xia Pu, Hong-Yan Guo, Zhe-Shan Quan, Xiaoting Li, Qing-Kun Shen
Magnolol, a natural product of M. officinalis, exhibits a wide range of biological activities. Yan et al.68 found that magnolol (EC50 = 3.07 µg/mL, p ≤ .001) exhibited better antifungal activity than tebuconazole against Rhizoctonia solani, with an EC50 value of 3.48 µg/mL. Therefore, Li et al.69 used magnolol as the lead compound and performed structural modifications at the C-3 and C-3′ positions and the hydroxyl and C-5 and C-5′ allyl positions to synthesise a series of magnolol derivatives. The in vitro biological activities of the compounds against phytopathogenic fungi (R. solani, Fusarium graminearum, Botrytis cinerea, and Sclerotinia sclerotiorum) were systematically evaluated (Table 3).
Genotoxic action of Luna Experience-SC 400 fungicide on rat bone marrow
Published in Biomarkers, 2019
Ayla Çelik, Gizem Güler, Cuma Aktaş, Serap Yalin
In an in vitro study of tebuconazole in bovine lymphocyte cultures, cytotoxic and genotoxic effects have been studied and results have shown increased cytotoxicity and genotoxicity (Šivikova et al.2013). In a rat-based study in which 96.2% pure tebuconazole was used, it was indicated that the liver is the target organ, the liver weight is increased and the serum enzyme levels are increased. Adenomas and carcinomas have been reported in the highest dose group (1500 ppm) (Tebuconazole, Summary of Toxicology Data 2008). According to data obtained as a result of Tebuconazole exposure study in Rhamdia quelen liver, it is shown that Tebuconazole cause the increasing oxidative damage potential (Ferreira et al.2010). Tebuconazole exposure studies in brain and liver tissues and white muscle cells of Cyprinus carpio have been shown to increase oxidative damage potential with TBA (thiobarbituric acid) (Toni et al. 2011).
A drift on liposomes to proliposomes: recent advances and promising approaches
Published in Journal of Liposome Research, 2022
Neha Dhiman, Jayrajsinh Sarvaiya, Poorti Mohindroo
A drug must be dispersed in a biodegradable and biocompatible polymer to prolong the bio-distribution kinetics and provide a time-delayed release also protects the therapeutic active ingredient from prompt degradation. An example presented by Jacobson et al. by using a supercritical carbon dioxide (sCO2) anti-solvent method (SAS) to generate Luciferin-containing nanoparticles enclosed in a biodegradable polymer (polylactic acid; PLA). Other biodegradable polymers, such as amphiphilic PEG (PEG conjugated to phosphatidylethanolamine), poly(alkyl cyanoacrylate), poly(ethylene oxide), sodium alginate (NaAlg), poly(vinyl alcohol) (PVA) can also be used to protect the liposomes from rapid elimination (Jacobson et al.2008). The so developed polymeric particles are stable in the gastrointestinal tract (GIT), shielding the drug from enzymatic degradation, acidic environment of the stomach, and other efflux pumps. Guncum et al. developed Amoxicillin-loaded polymeric nanoparticles for the controlled drug delivery on oral administration (Güncüm et al.2018, Adeyemi et al.2021). Similarly, Qureshi et al. developed Docetaxel that incorporated sustained release-lipid nanoparticles using palmityl alcohol to advance the pharmacokinetic behavior after oral and parenteral administration (Qureshi et al.2017). In addition, these solid-lipid nanoparticles (SLNPs) have not only provided an advantage in medicines but are also beneficial for the agricultural industry. Research communicated by Campos et al. characterized Carbendazim and Tebuconazole sustained release nanoparticles to tackle the fungal diseases in plants. It bids the advantage of reducing the adverse effects to the ecosystem and also waning the risks to human health (Campos et al.2015).