Whether plastic packaging waste is disposed of in different bins (source separation, S) or in a single bin (post source separation, P) is generally assumed to impact the waste stream's quality. To elucidate this question, we evaluated the quality of LDPE, HDPE, and PP plastic waste from both separation systems (S and P) through a concise analytical strategy. The materials received similar treatment after collection (e.
View Article and Find Full Text PDFA nanoparticle-based system, composed of the gallium(III) complex of a minimally substituted corrole that is coated by transferrin as a targeting vehicle ( NPs), has been used for pre-clinical evaluation of its efficacy against human metastatic castration-resistant prostate cancer (mCRPC) tumor xenografts. All mice ( = 9) responded to a dose of 10 mg/kg, with a remarkable tumor growth inhibition of 400% following 2 weeks of treatment; Ames and hERG tests excluded potential concerns regarding mutagenicity and cardiotoxicity, respectively. Also demonstrated is the potential application of these NPs as sonodynamic agents for the preclinical treatment of pancreatic cancer.
View Article and Find Full Text PDFAmyotrophic lateral sclerosis (ALS) is a progressive neurodegenerative disease affecting motor neurons. To date, the etiology of the disease is still unclear, with evidence of reactive oxygen species, mitochondrial dysfunction, iron homeostasis perturbation, protein misfolding and protein aggregation as key players in the pathology of the disease. Twenty percent of familial ALS and two percent of sporadic ALS instances are due to a mutation in Cu/Zn superoxide dismutase (SOD1).
View Article and Find Full Text PDFDevelopment of novel therapeutic strategies to eradicate malignant tumors is of paramount importance in cancer research. In a recent study, we have introduced a facile protocol for the preparation of corrole-protein nanoparticles (NPs). These NPs consist of a corrole-core coated with protein.
View Article and Find Full Text PDFWe report the utility of water-soluble corroles and also protein-coated nanoparticles (NPs) of lipophilic corroles as potent candidates for sonodynamic therapy (SDT), through the detection and quantification of the singlet oxygen that is produced by the ultrasonic irradiation of their aqueous solutions. Preliminary results on a cancer cell line provide evidence for the true utility of the NPs for SDT.
View Article and Find Full Text PDFIn aqueous media, hydrophobic metallocorroles form nanoparticles that are potential theranostic anticancer agents. We have analyzed the electronic and Raman spectra of Al(III), Ga(III), and Au(III) corrole nanoparticles (and made comparisons with DFT-validated assignments of the IR spectra of corresponding monomers) in order to estimate the strengths of corrole-corrole electronic couplings in these assemblies. We find that these spectra are virtually unchanged upon aggregation, confirming that the intermolecular interactions in these nanoparticles are very weak.
View Article and Find Full Text PDFRecent work has highlighted the potential of metallocorroles as versatile platforms for the development of drugs and imaging agents, since the bioavailability, physicochemical properties and therapeutic activity can be dramatically altered by metal ion substitution and/or functional group replacement. Significant advances in cancer treatment and imaging have been reported based on work with a water-soluble bis-sulfonated gallium corrole in both cellular and rodent-based models. We now show that cytotoxicities increase in the order Ga < Fe < Al < Mn < Sb < Au for bis-sulfonated corroles; and, importantly, that they correlate with metallocorrole affinities for very low density lipoprotein (VLDL), the main carrier of lipophilic drugs.
View Article and Find Full Text PDFAngew Chem Int Ed Engl
January 2018
Corrole and sapphyrin with the smallest meso-substituents reported so far were prepared in a one-pot synthesis that relies on a non-aldehydic precursor for introducing CF groups. The substantial amounts of products obtained by this facile pathway allowed for the full characterization of 5,10,15-tris(trifluoromethyl)corrole, the access to a variety of stable chelates thereof and investigations that disclose the unique structural and chemical properties induced by the CF substituents. The novel 5,10,15,20-tetra(trifluoromethyl)sapphyrin undergoes only single protonation, which according to its crystal structure is stabilized by favorable non-bonding F/H interaction between the meso-CF and the inverted pyrrolic NH.
View Article and Find Full Text PDFFacile, one-pot conversion of free base 5,10,15-tris(pentafluorophenyl)corrole, (H)tpfc, into the coinage metal complexes of 2,3,17,18-tetraiodo-5,10,15-tris(pentafluorophenyl)corrole, (I-tpfc)M (M = Cu, Ag, Au), is reported. The iodination/metalation procedures provide much higher yields and larger selectivity than both conceivable stepwise syntheses. Photophysical analysis shows that the gold(III) complex (I-tpfc)Au displays phosphorescence at room temperature and a substantial quantum yield for singlet oxygen formation.
View Article and Find Full Text PDFThe effect of the bis-sulfonated iron(III) corrole (1-Fe), a potent decomposition catalyst of reactive oxygen species, on rescuing SN4741 cells that were damaged by 6-hydroxydopamine (6-OHDA) was investigated as an in vitro model system for studying cell death of dopaminergic neurons in the substantia nigra. Important findings that accompanied the ability to rescue dopaminergic neurons were increased expression of phenotypic dopaminergic proteins, such as tyrosine hydroxylase (TH) and dopamine transporter (DAT), which were significantly depleted upon 6-OHDA-mediated damage. 1-Fe also elevated expression levels of aldehyde dehydrogenase 1 (ALDH-1), previously disclosed as a cardinal protein in the pathogenesis of Parkinson's disease.
View Article and Find Full Text PDFBackground: Three laboratory studies were conducted to assess the repellent and insecticidal efficacy of a combination of fipronil and permethrin (Frontline Tri- Act/Frontect) against three mosquito species (Aedes albopictus, Aedes aegypti and Culex pipiens) on dogs.
Methods: In each study, 16 healthy adult dogs were allocated to two groups. Eight dogs were treated with the new topical spot-on combination of fipronil and permethrin on Day 0 and the other eight dogs served as untreated controls.
Background: Five studies were conducted to evaluate the effect of a new combination of fipronil and permethrin on cat fleas, Ctenocephalides felis, when applied to dogs, including dogs that underwent water exposure or shampooing.
Methods: In each study, 16 dogs were allocated to two groups. Each dog was infested with 100 unfed adult fleas on Days -1, 7, 14, 21 and 28.
Background: A laboratory study was conducted to assess the repellent and insecticidal efficacy of a new combination of fipronil and permethrin (Frontline Tri- Act/Frontect Merial) against Stomoxys calcitrans (stable flies).
Methods: Sixteen dogs were allocated to two treatment groups. Eight dogs were treated with a new topical spot-on formulation containing 6.
Background: Dermacentor reticulatus is a European hard tick of major veterinary importance because it is the vector of canine babesiosis due to Babesia canis. The efficacy against this particular tick species is therefore a key characteristic for an acaricidal solution for dogs. The repellency, prevention of attachment and acaricidal efficacy of Frontline Tri- Act/Frontect, a new combination of fipronil and permethrin against induced infestations of Dermacentor reticulatus ticks on dogs were evaluated after a single topical administration.
View Article and Find Full Text PDFBackground: Two blinded, controlled laboratory studies were conducted to assess the acaricidal efficacy of a new combination of fipronil and permethrin (Frontline Tri-Act/Frontect) against two tick species. Study A evaluated the efficacy of the product against both Ixodes ricinus and Rhipicephalus sanguineus and Study B evaluated the efficacy against R. sanguineus only.
View Article and Find Full Text PDFBackground: Ctenocephalides canis is a major flea species in dogs in several European countries. The new topical combination of fipronil and permethrin (Frontline Tri-Act/Frontect, Merial) has been developed to control fleas, ticks, mosquitoes, sandflies and biting flies on dogs. Considering the repellent and insecticidal effects of permethrin and the insecticidal effect of fipronil, the efficacy of the combination against fleas including C.
View Article and Find Full Text PDFThe pharmacokinetics of afoxolaner in dogs was evaluated following either intravenous or after oral administration of NEXGARD(®), a soft chewable formulation. Afoxolaner is a member of one of the newest classes of antiparasitic agents, known as antiparasitic isoxazolines. The soft chewable formulation underwent rapid dissolution, and afoxolaner was absorbed quickly following oral administration of the minimum effective dose of 2.
View Article and Find Full Text PDFThe therapeutic efficacy of eprinomectin in an extended-release injection (ERI) formulation was evaluated against induced infections of developing fourth-stage larval or adult gastrointestinal and pulmonary nematodes of cattle in a series of six studies under two identical protocols (three each for developing fourth-stage larvae or adults) conducted in the USA, Germany or the UK (two studies at each location, one per stage). Each study initially included 16 nematode-free cattle. The cattle were of various breeds or crosses, weighed 109-186.
View Article and Find Full Text PDFThe efficacy of eprinomectin in an extended-release injection (ERI) formulation was evaluated against infections with third-stage larvae or eggs of gastrointestinal and pulmonary nematodes in cattle under 120-day natural challenge conditions in a series of five studies conducted in the USA (three studies) and in Europe (two studies). For each study, 30 nematode-free (four studies) or 30 cattle harboring naturally acquired nematode infections (one study) were included. The cattle were of various breeds or crosses, weighed 107.
View Article and Find Full Text PDFA series of 10 dose confirmation studies was conducted to evaluate the persistent activity of an extended-release injectable (ERI) formulation of eprinomectin against single point challenge infections of gastrointestinal and pulmonary nematodes of cattle. The formulation, selected based on the optimal combination of high nematode efficacy, appropriate plasma profile, and satisfactory tissue residue levels, includes 5% poly(D,L-lactide-co-glycolic)acid (PLGA) and is designed to deliver eprinomectin at a dose of 1.0mg/kg bodyweight.
View Article and Find Full Text PDFThe gamma-amino butyric acid (GABA)-gated chloride ion channel in the insect central nervous system is the target of cyclodiene and phenylpyrazole insecticides. Resistance to dieldrin has been reported in several insect species and was associated with a point mutation (Ala285 to Ser substitution) in the M2 transmembrane domain of the GABA-gated chloride ion channel (the resistant to dieldrin [Rdl] gene). A partial Rdl gene sequence was reported previously in specimens of the cat flea, Ctenocephalides felis (Bouché).
View Article and Find Full Text PDFMultidrug resistance (MDR) phenotypes in cancer cells are associated with overexpression of the drug carrier P-glycoprotein. The antiparasitic drug ivermectin, one of its substrates, abnormally accumulates in the brain of transgenic mice lacking the P-glycoprotein, resulting in neurotoxicity. Similarly, an enhanced sensitivity to ivermectin has been reported in certain dogs of the Collie breed.
View Article and Find Full Text PDFThe efficacy of FRONTLINE SPRAY (0.25% (w/v) fipronil), FRONTLINE SPOT-ON FOR DOGS (10% (w/v) fipronil) and FRONTLINE PLUS FOR DOGS (10% (w/v) fipronil and 9% (S)-methoprene) against the biting louse Trichodectes canis on dogs was confirmed under laboratory conditions. A field study evaluated the efficacy of a single topical application of FRONTLINE SPRAY and FRONTLINE SPOT-ON against the parasite on dogs.
View Article and Find Full Text PDFTo assess the persistence of the activity of topical ivermectin against a natural challenge with biting lice (Bovicola bovis), 90 mixed-breed cattle that had been treated to remove lice, were blocked by bodyweight within sex and randomly allocated to three treatments: untreated control, doramectin at 200 micrograms/kg by subcutaneous injection, and ivermectin at 500 micrograms/kg by topical application. Forty-five pens were blocked into three groups of 15, and the blocks of pens were randomly allocated to three 14-day challenge periods starting 21, 28 and 35 days after treatment. There were five pens per treatment for each challenge period, and one B bovis-infested donor calf was introduced into each pen containing two principal calves at the start of the challenge period for that block of pens.
View Article and Find Full Text PDFObjective: To assess the persistent activity of injectable formulations of abamectin and doramectin against gastrointestinal nematodes of cattle.
Design: Controlled slaughter study assessing residual efficacy.
Procedure: Nematode-free calves were treated with abamectin or doramectin (each at a dose of 200 micrograms/kg) and infections then induced with repeated doses of infective larvae of Trichostrongylus axei, Haemonchus placei, Ostertagia ostertagi and Cooperia species.