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3 results on '"choline derivative"'

1. In vivo antimalarial activity and pharmacokinetics of artelinic acid-choline derivative liposomes in rodents.

Author

Duan, Shuai, Wang, Ruili, Wang, Rongrong, Tang, Jiaqi, Xiao, Xiaoyang, Li, Ning, Guo, Wenju, Yang, Qingshan, Ren, Guolian, and Zhang, Shuqiu

Subjects
*LIPOSOMES, *PLASMODIUM yoelii, *PHARMACOKINETICS, *DEHYDRATION reactions, *DRUG resistance, *TREATMENT effectiveness
Abstract

It is urgent to develop new antimalarial drugs with good therapeutic effects to address the emergence of drug resistance. Here, the artelinic acid-choline derivative (AD) was synthesized by dehydration reaction and esterification reaction, aimed to avoid the emergence of drug resistance by synergistic effect of artemisinins and choline derivative, which could compete with choline for rate-limiting enzymes in the phosphatidylcholine (PC) biosynthetic pathway. AD was formulated into liposomes (ADLs) by the thin-film hydration method. Efficacy of ADLs was evaluated by Peters 4-day suppression test. The suppression percentage against Plasmodium yoelii BY265 (Py BY265) in ADLs group was higher than those of positive control groups (dihydroartemisinin liposomes, P < 0.05) and other control groups (P ⩽ 0.05) at the doses of 4.4, 8.8, 17.6 µ mol (kg·d)−1, respectively. The negative conversion fraction, recrudescence fraction and survival fraction of ADLs group were superior to other control groups. Pharmacokinetics in rats after intravenous injection suggested that ADLs exhibited higher exposure levels (indexed by area under concentration-time curve) than that of AD solution, artelinic acid liposomes or artelinic acid solution (P < 0.01). Taken together, ADLs exhibited promising antimalarial efficacy and pharmacokinetic characteristics. [ABSTRACT FROM AUTHOR]

Published
2020
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2. Choline derivative ionic liquids-based aqueous two-phase systems: Phase diagrams and partition of purine alkaloids.

Author

Ren, Jiao, Li, Zhiyong, Liu, Jing, Pei, Yuanchao, Wang, Huiyong, and Wang, Jianji

Subjects
*CHOLINE, *IONIC liquids, *AQUEOUS solutions, *PHASE diagrams, *PHASE partition, *ALKALOIDS
Abstract

Searching for environmentally friendly aqueous two-phase systems is imperative for the sustainable development of separation technologies. In this work, five kinds of environmentally benign choline derivative ionic liquids were synthesized and used for the formation of aqueous two-phase systems with K 3 PO 4 , K 3 C 6 H 5 O 7 or K 2 CO 3 . In order to understand the phase formation processes of these aqueous two-phase systems and their possible application in extraction, phase diagrams and partition coefficients of purine alkaloids were determined at T  = 298.2 K, and the effects of structure of the ionic liquids, nature of the purine alkaloids, composition and temperature of the systems on the partitioning behaviour of purine alkaloids were investigated systematically. It was shown that caffeine, theobromine and 2,6-amino purine could be extracted effectively into the ionic liquid-rich phase of the aqueous two-phase systems, and the partition coefficients were as high as 4.5–42 under the optimized conditions. The partitioning was found to decrease with the increase of the ratio of H 2 O weight fraction (in the ionic liquid-rich phase and in the salt-rich phase) and hydrophobicity of both the purine alkaloids and the ionic liquids, but not sensitive to the change of temperature. [ABSTRACT FROM AUTHOR]

Published
2018
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3. Potential use of the oligochaete Limnodrilus profundicola V., as a bioindicator of contaminant exposure

Author

Adile Ozdemir, Alaattin Sen, and Mustafa Duran

Subjects
methomyl, Water samples, Insecticides, Turkey, Organoplatinum Compounds, Health, Toxicology and Mutagenesis, environmental exposure, Methomyl, Aromatic hydrocarbons, Fresh Water, Methyl Parathion, Toxicology, Turkey (republic), chemistry.chemical_compound, Model substrates, biochemical composition, water sampling, Pyrethrins, Bioindicator species, acetylthiocholine, Cholinesterases, Polycyclic Aromatic Hydrocarbons, enzyme inhibition, media_common, Platinum compounds, butyrylthiocholine, water pollution, ethoxyresorufin deethylase, integumentary system, Freshwater oligochaetes, choline derivative, article, General Medicine, biological marker, Pollution, Polychlorinated Biphenyls, Polycyclic aromatic hydrocarbons, inhibition, unclassified drug, enzyme activity, streamwater, Polycyclic Hydrocarbons, Aromatic, Oil-contaminated sediments, priority journal, Environmental chemistry, Toxicity, biomarker, annelid worm, Biological Markers, Environmental Monitoring, sampling, cholinesterase, media_common.quotation_subject, substrate, Management, Monitoring, Policy and Law, Biology, Limnodrilus profundicola, propionylthiocholine, Anoxic sediments, In-vivo, Nitriles, Cytochrome P-450 CYP1A1, Ecotoxicology, bioindicator, Animals, Oligochaeta, Contaminant exposure, Pollutant, EROD activity, parathion methyl, nonhuman, Ethoxyresorufin-O-deethylase, insecticide, pollution exposure, deltamethrin, PAH, Biochemical tools, Deltamethrin, chemistry, sediment, Acetylthiocholine, annelid, Bioindicator, Biomarkers, Water Pollutants, Chemical
Abstract

Cholinesterase (ChE) and ethoxyresorufin-O-deethylase (EROD) were of special interest to this study as these biochemical tools have been widely used for the determination of exposure to pollutants. In this study, the freshwater oligochaete Limnodrilus profundicola was tested for its potential as a bioindicator of freshwater pollution. For this purpose, the ChE and EROD activities of L. profundicola and the level of polycyclic aromatic hydrocarbons (PAH) of water samples collected from different sites along the Curuksu stream on the Menderes River (the ancient Meander) running through south-western Turkey were studied. First, these activities were characterized using, as model substrates, acetylthiocholine (ATC), propionylthiocholine (PTC), and butyrylthiocholine (BTC). Then, the in vivo effects of insecticides and pollutants on these activities were investigated. L. profundicola were exposed to various doses of methyl-parathion, methomyl, and deltamethrin. Although significant inhibition of ChE was detected with each of the insecticides, the highest level of inhibition was observed with methyl-parathion. In addition to the inhibition of ChE, the activity of EROD was induced by exposure to oil-contaminated sediments. Thus, although L. profundicola has a reputation for being very resistant to pollution (although it is not insensitive to it), we demonstrated that it may potentially be used as a bioindicator species for contaminant exposure when ChE and EROD are used as biomarkers. © 2010 Wiley Periodicals, Inc.

Published
2010

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