沙丁胺醇联合布地奈德治疗支气管哮喘急性发作51例临床观察

目的观察临床应用沙丁胺醇联合布地奈德治疗小儿支气管哮喘急性发作治疗效果。方法选择支气管哮喘急性发作的小儿患者102例,将所有患儿随机分为观察组与对照组,各51例。对照组患儿在常规治疗的基础上单纯采用沙丁胺醇雾化吸入治疗,观察组患儿采用沙丁胺醇联合布地奈德雾化吸入治疗,观察两组的治疗效果。结果观察组的总有效率为96.08%,优于对照组的总有效率80.39%,由此可见此差异具有统计学意义(P0.05);不良反应发生率为5.8%,低于对照组9.8%,差异具有统计学意义(P0.05)。结论采用沙丁胺醇、布地奈德联合治疗支气管哮喘急性发作,具有较好的治疗效果,值得在临床上进一步推广应用。     

Binding of Chromium(III) to Transferrin Could Be Involved in Detoxification of Dietary Chromium(III) Rather than Transport of an Essential Trace Element

Cr^III binding to transferrin (Tf; the main Fe^III transport protein) has been postulated to mediate cellular uptake of Cr^III to facilitate a purported essential role for this element. Experiments using HepG2 (human hepatoma) cells, which were chosen because of high levels of the transferrin receptor, showed that Cr^III binding to vacant Fe^III‐binding sites of human Tf effectively blocks cellular Cr^III uptake. Through bio‐layer interferometry studies of the Tf cycle, it was found that both exclusion and efflux of Cr₂^IIITf from cells was caused by 1) relatively low Cr₂Tf affinity to cell‐surface Tf receptors compared to Fe₂Tf, and 2) disruption of metal release under endosomal conditions and post‐endosomal Tf dissociation from the receptor. These data support mounting evidence that Cr^III is not essential and that Tf binding is likely to be a natural protective mechanism against the toxicity and potential genotoxicity of dietary Cr through blocking Cr^III cellular accumulation.     

Modulation of antioxidant systems by subchronic exposure to the aqueous extract of leaves from Achillea millefolium L. in rats

We determined the effects of subchronic exposure to aqueous extract of leaves from Achillea millefolium (AE) on enzyme- and non-enzyme-dependent antioxidant systems in rats. Seven days treatment with AE (1 g/kg/twice a day, p.o.) altered the reduced glutathione (GSH) levels and antioxidant enzyme activities in several organs of the animals. Amount of GSH in uterus was increased (73%) while in kidneys it was decreased (23%). Besides, NAD(P)H quinone oxidoreductase 1 (NQO1) activity was increased in forestomach (26%) and in liver (64%), while glutathione S-transferase activity was decreased in the forestomach (32%) and increased in the liver (41%), kidney (35%) and uterus (37%). In preliminary experiments targeting the interaction of AE with acetaminophen (600 mg/kg, p.o.), we observed augmentation of acetaminophen-induced increase of the plasmatic alanine aminotransaminase, aspartate aminotransaminase and lactate dehydrogenase. Overall, the results indicate a potential toxic interaction of AE compounds with xenobiotics that use the glutathione pathway.     

Biological activities of Peristrophe bivalvis extracts: promising potential for anti-snake venoms against Naja kaouthia and Trimeresurus albolabris venoms

This study evaluates the in vitro anti-snake venom potential of Peristrophe bivalvis (PB) extracts against Naja kaouthia (NK) and Trimeresurus albolabris (TA) venoms, including inhibition of cytotoxic effects and enzymatic activities, and the binding-precipitation of extracts and venom proteins analysis. In addition, the antioxidant, cytotoxic and in vivo acute oral toxic activities of PB extracts are also reported. The in vitro cytotoxic and enzymatic analysis reveals that the ethanol extracts of stems and leaves of PB showed good anti-snake venom activity against NK and TA venoms. In addition, the antioxidant result indicated that only the ethanol extract of leaves exhibited weak DPPH radical-scavenging activity. The ethanol whole-plant extract of PB also showed no cytotoxicity against four cell lines. Moreover, the in vivo acute oral toxicity result of the ethanol whole-plant extract showed that all treated rats did not exhibit abnormal toxic signs or deaths.     

Chemical composition,protoscolicidal effects and acute toxicity of Pistacia atlantica Desf. fruit extract

The present study was designed to evaluate the chemical composition and scolicidal effects of Pistacia atlantica Desf. extract against protoscoleces of hydatid cysts and its acute toxicity in mice model. Various concentrations of the methanolic extract (5–50 mg/mL) were used for 10–60 min. Viability of protoscoleces was confirmed using eosin exclusion test (0.1%). Acute toxicity was also determined in mice model. The main components were β-myrcene (41.4%), α-pinene (32.48%) and limonene (4.66%). Findings demonstrated that P. atlantica extract at the concentrations of 25 and 50 mg/mL after 20 and 10 min of exposure killed 100% protoscoleces. The LD₅₀ of the intraperitoneal injection of the P. atlantica methanolic extract was 2.43 g/kg and the maximum non-fatal dose was 1.66 g/kg. Obtained results showed the potential of P. atlantica extract as a natural source with no significant toxicity for the production of new scolicidal agent to use in hydatid cyst surgery.     

Rapid structural characterization of in vivo and in vitro metabolites of tinoridine using UHPLC–QTOF–MS/MS and in silico toxicological screening of its metabolites

Tinoridine is a nonsteroidal anti‐inflammatory drug and also has potent radical scavenger and antiperoxidative activity. However, metabolism of tinoridine has not been thoroughly investigated. To identify in vivo metabolites, the drug was administered to Sprague–Dawley rats (n = 5) at a dose of 20 mg kg^?1, and blood, urine and feces were collected at different time points up to 24 h. In vitro metabolism was delved by incubating the drug with rat liver microsomes and human liver microsomes. The metabolites were enriched by optimized sample preparation involving protein precipitation using acetonitrile, followed by solid‐phase extraction. Data processes were carried out using multiple mass defects filters to eliminate false‐positive ions. A total of 11 metabolites have been identified in urine samples including hydroxyl, dealkylated, acetylated and glucuronide metabolites; among them, some were also observed in plasma and feces samples. Only two major metabolites were formed using liver microsomal incubations. These metabolites were also observed in vivo. All the 11 metabolites, which are hitherto unknown and novel, were characterized by using ultrahigh‐performance liquid chromatography–quadrupole time‐of‐flight tandem mass spectrometry in combination with accurate mass measurements. Finally, in silico toxicological screening of all metabolites was evaluated, and two metabolites were proposed to show a certain degree of lung or liver toxicity. Copyright © 2015 John Wiley & Sons, Ltd.     

Syntheses,Cytotoxicity and Properties of CO Releasing Molecules Containing Acetyl Salicylamide‐3‐pyridine

A series of CO‐releasing molecules [M(CO)₅L] (M=Cr, W, Mo, L=acetyl salicylamide 3‐pyridine, 1 – 3 ; L=N,N‐dimethyl‐4‐pyridine, 4 – 6 ; L=nicotinamide, 7 – 9 ; L=4‐CHO‐pyridine, 10 – 12 ) were synthesized. And in this paper, we have investigated mainly cytotoxicity and properties of the CO‐releasing molecules containing acetyl salicyamide‐3‐pyridine, namely complexes 1 – 3 . The stability of complexes 1 and 2 was evaluated by means of UV‐Vis spectroscopy and ¹H NMR spectra. The results indicate complexes 1 and 2 were stable in methanol and acidic aqueous solution, but unstable and decayed in basic media (pH 10.0). Among all the complexes, complex 2 was the slowest CO‐releaser, and its half‐life was 73.8 min. Complex 9 containing nicotinamide was the fastest CO‐releaser with half‐life only 6.5 min. In addition, cytotoxic effects of all the complexes on the proliferation of fibroblast line were assayed by MTT. Among all the complexes, the IC₅₀ of complex 1 was 6 µmol/L, revealing complex 1 possessed stronger antiproliferative activity than the control. Analysis by Flow cytometry revealed that complex 1 arrested Hela cells in S phase while complexes 2 and 8 arrested in G2/M phase. Cell apoptosis caused by the complexes mainly occurred in "Late apoptosis".     

Elemental Analysis of Edible Mountain Nettle (Obetia tenax) and the Influence of Soil on Its Chemical Composition

In developing countries, the dietary intake of essential elements is largely dependent on the consumption of edible fruits and leafy vegetables. The distribution of elements in the indigenous edible plant, Obetia tenax (mountain nettle), was investigated as a function of soil quality from eight sites in KwaZulu-Natal, South Africa. The results show concentrations of elements in the leaves to be in decreasing order of Ca?>?Mg?>?Fe?>?Mn?>?Zn?>?Cr?>?Cu?>?Ni?>?Pb?>?Co?>?As?>?Cd?>?Se, and in the stems and roots to be in decreasing order of Ca?>?Mg?>?Fe?>?Mn?>?Zn?>?Cu?>?Ni?>?As?>?Pb?>?Co?>?Cd?>?Cr?>?Se. The quality and pollution status of soil was evaluated by geoaccumulation indices and enrichment factors, which indicated moderate cadmium contamination at the Msinga location that was confirmed by the pollution index and ecological risk levels of single-factor pollution. An assessment of overall contamination of soil using Nemerow pollution index showed moderate pollution by cadmium, while the potential toxicity index indicated low-grade risk for all elements at all sites. Principal component and cluster analysis revealed two groups of elements with similarities, As, Cd, Co, Cr, Cu, Mn, Ni, and Fe, suggesting a lithogenic source and an anthropogenic source for Pb and Zn. Correlation analysis showed significantly positive correlations between As, Co, Cr, Cu, Fe, and Ni/Cd in the soil, confirming the elements’ common origin.     

Characterisation of captopril photolysis and photocatalysis by-products in water by direct infusion,electrospray ionisation,high-resolution mass spectrometry and the assessment of their toxicities

Pharmaceuticals of different therapeutic classes are found in the environment. Captopril is used worldwide as an antihypertensive drug, and it has been found in the influent, effluent and secondary sludge of wastewater treatment plants. Advanced oxidation processes, such as direct photolysis (UV-C) and heterogeneous photocatalysis (TiO₂/UV-C), are alternatives to enhance mineralisation of pharmaceuticals and their removal during water treatment. In this article, it was evaluated the degradation of captopril in aqueous solution induced by UV-C and TiO₂/UV-C systems. The process focused on the identification and monitoring of the by-products formed under these conditions by applying direct-infusion electrospray ionisation high-resolution mass spectrometry in the negative ion mode (ESI(-)-HRMS) and high-performance liquid chromatography coupled to high-resolution mass spectrometry (HPLC/HRMS). To evaluate the by-products toxicity, acute ecotoxicity tests were performed with the crustacean Artemia salina, and the cytotoxicity was evaluated with (4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay using HepG2 cells. It was observed by ESI(-)-HRMS that after 120 min of light exposure, there was almost complete removal of captopril, with 93.5% removal efficiency during photolysis and 99.9% during photocatalysis. At these conditions, the rate of mineralisation, by total organic carbon (TOC), was only 2.92% for photolysis and 9.09% for photocatalysis, evidencing the formation of degradation by-products. Nine by-products of captopril photodegradation were identified, and their respective chemical structure elucidations were proposed. The treated samples were nontoxic to A. salina and HepG2 cells, indicating that both oxidative treatments (photocatalytic or photolytic processes) can be conveniently employed to remove captopril from aqueous media.     

Effects of neonicotinoid insecticide formulations and their components on Daphnia magna – the role of active ingredients and co-formulants

Formulating agents used in pesticide products have been regarded as inactive/inert components; however, several studies confirmed additive, synergistic or antagonistic effects between the active ingredients (AIs) and additives, or the individual toxicity of the formulating agents. The worldwide used neonicotinoid insecticides and their components can reach surface waters, due to their physico-chemical properties (e.g. water solubility) or improper application in chemical plant protection technology, and can adversely affect non-target aquatic organisms. Formulated pesticides were analysed for alkane sulphonate surfactants by using liquid chromatography coupled with tandem mass spectrometry. In acute immobilisation tests on Daphnia magna, differences were found among the toxicity of the investigated neonicotinoid AIs and formulations. The toxicity of a formulated insecticide (Apache 50 WG®– AI: clothianidin) was found to be 46.5 times more toxic than explained by its AI, probably due to toxic effect of the formulating agents on D. magna. In contrast, two preparations (Calypso 480SC® – AI: thiacloprid, Actara 240 SC®– AI: thiamethoxam) were 2–3 times less toxic than their AIs. Results indicate possible synergistic/antagonistic interaction with the AIs.