The acute and short term chronic toxicity of both the herbicide butyl ester of 2,4-Dichlorophenoxyacetic acid (2,4-D) and a commercial formulation (CF) were evaluated on Rhinella (= Bufo) arenarum embryos at different developmental stages. Adverse effects were analyzed by means of the isotoxicity curves for lethality, malformations, stage-dependent susceptibility, and ultrastructural features. For all experimental conditions, the CF was more toxic, up to 10 times, than the active ingredient, being the open mouth stage (S.21) the most susceptible to the herbicide. For continuous treatment conditions, the early embryonic development was the most susceptible to 2,4-D and the LC50s for 96 and 168 h were 9.06 and 7.76 mg L(-1) respectively. In addition, both the active ingredient and the CF were highly teratogenic, resulting in reduced body size, delayed development, microcephaly, agenesis of gills, and abnormal cellular proliferation processes as the main adverse effects. According to US EPA, 2,4-D in agricultural scenarios may be up to three times higher than the NOEC values for teratogenic effects reported in this study. Therefore, they might represent a risk for amphibians. This study also points out the relevance of reporting the susceptibility of embryos at different developmental stages to both the active ingredient and the CF of agrochemicals in order to protect nontarget organisms.
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http://dx.doi.org/10.1002/tox.20564 | DOI Listing |
Chin J Nat Med
December 2024
National and Local Collaborative Engineering Center of Chinese Medicinal Resources Industrialization and Formulae Innovative Medicine, Jiangsu Collaborative Innovation Center of Chinese Medicinal Resources Industrialization, Jiangsu Province Key Laboratory of High Technology Research, Nanjing University of Chinese Medicine, Nanjing 210023, China; School of Medicine, Nanjing University of Chinese Medicine, Nanjing 210023, China. Electronic address:
Active herbal ingredients are gaining recognition for their potent anti-tumor efficacy, attributable to various mechanisms including tumor cell inhibition, immune system activation, and tumor angiogenesis inhibition. Recent studies have revealed that numerous anti-tumor herbal ingredients, such as ginsenosides, ursolic acid, oleanolic acid, and Angelica sinensis polysaccharides, can be utilized to develop smart drug carriers like liposomes, micelles, and nanoparticles. These carriers can deliver active herbal ingredients and co-deliver anti-tumor drugs to enhance drug accumulation at tumor sites, thereby improving anti-tumor efficacy.
View Article and Find Full Text PDFJ Ethnopharmacol
December 2024
Encephalopathy Hospital, the First Affiliated Hospital of Henan University of Chinese Medicine, Henan 450000, China. Electronic address:
Ethnopharmacological Relevance: Xiao-xu-ming decoction (XXMD), a prominent traditional Chinese medicinal formula historically revered for stroke treatment, demonstrates pronounced efficacy in ameliorating ischemic stroke injury.
Aim Of The Study: This study aims to investigate the effects and mechanisms of XXMD on neuroprotection subsequent to cerebral ischemia/reperfusion in vivo and in vitro.
Materials And Methods: Neurobehavioral test, TTC staining, HE staining and nissl staining were used to examine the neuroprotective effect of XXMD on cerebral ischemia-reperfusion injury induced by middle cerebral artery occlusion (MCAO) in rats.
Environ Toxicol Pharmacol
December 2024
Department of Pharmacy and Pharmaceutical Sciences, National University of Singapore, Lower Kent Ridge Road, 4 Science Drive 2, Singapore 117544. Electronic address:
The metabolic conversion of aromatic amines to N-acetylated forms in skin and keratinocytes depends on N-acetyltransferase-1 (NAT1). Common hair color ingredient such as para-phenylenediamine (PPD) causes allergic contact dermatitis. We explored how different electronic substituents on PPD aided NAT1 enzyme biotransform oxidative arylamine (AA) compounds G1-G13 by N-acetylation, NAT-1 activity assays, metabolism, and in vitro clearance investigations in human keratinocytes, while identifying NAT-1 protein levels by Western blot and qRT-PCR.
View Article and Find Full Text PDFEur J Pharm Sci
December 2024
Institute of Pharmaceutical Technology, Center of pharmaceutical nanotechnology, Faculty of Pharmacy, Ss. Cyril & Methodius University in Skopje, Majka Tereza 47, 1000 Skopje, R North Macedonia.
In this study 3D printed tablets (printlets) with extended release of hydrochlorothiazide (HHT) as model active ingredient were designed and developed. Four formulations, F0.1, F1, F0.
View Article and Find Full Text PDFJ Pharm Sci
December 2024
Janssen Research & Development, LLC, Discovery Pharmaceutics, San Diego, CA, USA.
Rat pharmacokinetic studies are commonly utilized in early discovery to support absorption, distribution, metabolism, and excretion optimization of active pharmaceutical ingredients (APIs). The aim of this work was to compare exposures from fit-for-purpose oral suspension and solution formulations in rats to guidance provided by the refined Developability Classification System (rDCS) with respect to identifying potential limits to oral absorption, formulation strategy selection, and to optimize oral bioavailability (BA). This investigation utilized six diverse APIs covering a large range of biorelevant solubility, metabolic stability, and oral BA in rats.
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