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Azacarbazole n-3 and n-6 polyunsaturated fatty acids ethyl esters nanoemulsion with enhanced efficacy against Plasmodium falciparum

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Bioactive Materials 2021年第4期6卷 1163-1174页

作者： anna jaromin Silvia Parapini Nicoletta Basilico Magdalena Zaremba-Czogalla Agnieszka Lewi´nska Agnieszka Zag´orska Maria Walczak Bozena Tyliszczak Aleksandra Grzeszczak MarcinŁukaszewicz Łukasz Kaczmarek Jerzy Gubernator Department of Lipids and Liposomes Faculty of BiotechnologyUniversity of WroclawWroclawPoland Dipartimento di Scienze Biomediche per la Salute Universit`a degli Studi di MilanoMilanItaly Dipartimento di Scienze Biomediche Chirurgiche e OdontoiatricheUniversit`a degli Studi di MilanoMilanItaly Faculty of Chemistry University of WroclawWroclawPoland Department of Medicinal Chemistry Jagiellonian University Medical CollegeCracowPoland Chair and Department of Toxicology Jagiellonian University Medical CollegeFaculty of PharmacyCracowPoland Instytute of Materials Science Cracow University of TechnologyCracowPoland Department of Biotransformation Faculty of BiotechnologyUniversity of WroclawWroclawPoland Pharmaceutical Research Institute WarsawPoland

Alternative therapies are necessary for the treatment of malaria due to emerging drug ***,many promising antimalarial compounds have poor water solubility and suffer from the lack of suitable delivery systems,which seriously limits their *** address this problem,we synthesized a series of azacarbazoles that were evaluated for antimalarial activity against D10(chloroquine-sensitive)and W2(chloroquine-resistant)strains of *** most active compound,9H-3-azacarbazole(3),was encapsulated in a novel o/w nanoemulsion consisting of ethyl esters of polyunsaturated fatty acids n-3 and n-6 obtained from flax oil as the oil phase,Smix(Tween 80 and Transcutol HP)and *** formulation was further analyzed using transmission electron microscopy,dynamic light scattering and in vitro and in vivo *** was shown that droplets of the 3-loaded nanosystem were spherical,with satisfactory stability,without cytotoxicity towards fibroblasts and intestinal cell lines at concentrations corresponding to twice the IC50 for ***,the nanoemulsion with this type of oil phase was internalized by Caco-2 ***,pharmacokinetics demonstrated rapid absorption of compound 3(tmax=5.0 min)after intragastric administration of 3-encapsulated nanoemulsion at a dose of 0.02 mg/kg in mice,with penetration of compound 3 to deep *** 3-encapsulated nanoemulsion was found to be 2.8 and 4.2 times more effective in inhibiting the D10 and W2 strains of the parasite,respectively,compared to non-encapsulated *** findings support a role for novel o/w nanoemulsions as delivery vehicles for antimalarial drugs.

关键词： Azacarbazoles Flax oil n-3 and n-6 polyunsaturated fatty acids ethyl esters Nanoemulsion P.falciparum Malaria

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Community structure of Lumbricidae in beech woodland of the Bieszczady National Park, Southeast Poland

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Pedosphere 2021年第3期31卷 391-397页

作者： anna MAZUR-PĄCZKA Grzegorz PĄCZKA Joanna KOSTECKA Kevin R.BUTT Marcin jaromin Mariola GARCZYŃSKA Agnieszka PODOLAK University of Rzeszów Faculty of Biology and AgricultureDepartment of Natural Theories of Agriculture and Environmental Education1a Cwiklinskiej St.Rzeszów 35-959Poland University of Central Lancashire Forensic and Applied SciencesPreston PR12HEUK Rzeszów University of Technology Faculty of ChemistryDepartment of Biotechnology and Bioinformatics6 Powstancow Warszawy AvenueRzeszów 35-959Poland

As ecosystem engineers,earthworms play a key role in the soil ***,due to increasing anthropogenic pressure,soil organisms,including earthworms,are being threatened by habitat *** this study,we undertook a qualitative and quantitative investigation of earthworms of the family Lumbricidae in four types of Carpathian beech woodland(Fagetum carpaticum),characterized by their understory vegetation(I,*** drymejae;Ⅱ,***;Ⅲ,***;and IV,***),in the Bieszczady National Park(Eastern Carpathians,Southeast Poland).At each investigated site,soil monoliths(25 cm×25 cm×25 cm)were examined by hand *** were expelled from deep soil layers using a weak formalin solution(0.4%).Depending on the phytocoenosis,7 species of Lumbricidae were identified at each of the sites I,Ⅱ,andⅢand 10 at site *** IV(***)differed significantly(P<0.05)from the other three sites with respect to earthworm biomass(59.71±39.53 g m^(-2))and the Shannon-Wiener diversity index(0.52±0.12).Although present three decades ago,the deep-burrowing species Octodrilus transpadanus and the litter-dwelling species Dendrobaena octaedra were not found at site IV in the present *** suspect that these two species may have been displaced by the invasive Lumbricus terrestris,which was not found at the same site in the *** observations warrant further investigation to verify the predicted effects of an invasive earthworm,including the potential effects on soils and other fauna and flora,which have been documented in numerous countries.

关键词： beech forest earthworm invasive species Shannon-Wiener diversity index species diversity species dominance

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A dopamine and noradrenaline reuptake inhibitor （bupropion） does not alter exercise performance of bank voles

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Current Zoology 2016年第3期62卷 307-315页

作者： Ewa jaromin Edyta Teresa SADOWSKA Pawet KOTEJA Institute of Environmental Sciences Jagiellonian University Gronostajowa 7 Krakow 30-387 Poland

Physical performance is determined both by biophysical and physiological limitations and behavioral characteristic, specifically motivation. We applied an experimental evolution approach combined with pharmacological manipulation to test the hypothesis that evolution of increased aerobic exercise performance can be triggered by evolution of motivation to undertake physical activity. We used a unique model system: bank voles from A lines, selected for high swim-induced aerobic metabolism (VOswim), which achieved a 61% higher mass-adjusted VOswim than those from unselected C lines. Because the voles could float on the water surface with only a minimum activity, the maximum rate of metabolism achieved in that test depended not only on their aerobic capacity, but also on motivation to undertake intensive activity. Therefore, we hypothesized that signaling of neurotransmitters putatively involved in regulating physical activity (dopamine and noradrenaline) had changed in response to selection. We measured VOswim after intraperitoneal injections of saline or the norepinephrine and dopamine reuptake inhibitor bupropion (20 mg/kg or 30 mg/kg). Additionally, we measured forced-exercise VO (VOmax). In C lines, VOswim (mass-adjusted mean ± standard error (): 4.0 ± 0.1 mLO/min) was lower than VOmax (5.0 ± 0.1 mLO/min), but in A lines VO2swim (6.0 ± 0.1 mLO/min) was as high as VOmax (6.0 ± 0.1 mLO/min). Thus, the selection effectively changed both the physiological-physical performance limit and mechanisms responsible for the willingness to undertake vigorous locomotor activity. Surprisingly, the drug had no effect on the achieved level of VOswim. Thus, the results did not allow firm conclusions concerning involvement of these neurotransmitters in evolution of increased aerobic exercise performance in the experimental evolution model system.

关键词：去甲肾上腺素盐酸安非他酮运动性能多巴胺抑制剂田鼠银行摄取

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The effect of monoamines reuptake inhibitors on aerobic exercise performance in bank voles from a selection experiment

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Current Zoology 2019年第4期65卷 409-419页

作者： Ewa jaromin Edyta T. Sadowska Pawet Koteja Institute of Environ metal Sciences Jagiellonian University 7 Gronostajowa Street 30-387 Krakow Poland

Exercise performance depends on both physiological abilities (e.g., muscle strength) and behavioral characteristics (e.g., motivati on). We tested the hypothesis that evoluti on of in creased aerobic exercise performanee can be facilitated by evolution of neuropsychological mechanisms responsible for motivation to undertake physical activity. We used a unique model system: lines of bank voles Myodes glareolus selected for high swim-induced aerobic metabolism ("aerobic" A lines). In gen eration 21, voles from the 4 A lines achieved a 57% higher /y voluntary maximum" swiminduced aerobic metabolism (V02swim) than voles from 4 unselected,"control" C lines. In C lines, V02swim was 9% lower than the maximum forced-exercise aerobic metabolism (VO2run;P= 0.007), while in A lines it was even higher than VO2run, although not significantly (4%, P=0.15). Thus, we hypothesized that selection changed both the aerobic capacity and the neuronal mechanisms behi nd motivation to un dertake activity. We investigated the influe nee of reuptake in hibitors of dopamine (DARI), serotonin (SSRI), and norepinephrine (NERI) on VOaSwim. The drugs decreased V02swim both in C and A lines (% decrease compared with saline: DARI 8%, P< 0.001;SSRI 6%, P< 0.001;NERI 8%, P< 0.001), but the proportional response differed between selection directions only for NERI (stronger effect in C lines: P= 0.008) and the difference was marginally non-significant for SSRI (P= 0.07) and DARI (P= 0.06). Thus, the results suggest that all the 3 monoamines are involved in signaling pathways controlling the motivation to be active and that norepinephrine could have played a role in the evolution of increased aerobic exercise performance in our animal model.

关键词： experimental evolution monoamines motivation physical activity selective breeding voluntary exercise

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微泡成象工艺

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感光材料 1976年第5期 37-39页

作者： jaromin Kosav 青岛市轻工业研究所情报室

在微泡成象过程中,重氮化合物经光解能释放出氮气。重氮化合物作为感光剂分散在合适的载体中,并经涂布、干燥成为微泡胶片。曝光后气体膨胀形成微泡,因微泡对光的折射率不同,而将所受的光散射开形成影象。因此,微泡影象是以入射光的散... 详细信息

在微泡成象过程中,重氮化合物经光解能释放出氮气。重氮化合物作为感光剂分散在合适的载体中,并经涂布、干燥成为微泡胶片。曝光后气体膨胀形成微泡,因微泡对光的折射率不同,而将所受的光散射开形成影象。因此,微泡影象是以入射光的散射为基础的;这同重氮化过程靠光线的吸收相反。从光的入射方向看微泡影象呈白色,用它作透明投影时,画面呈现暗色,因而能够用作黑白幻灯片或电影正片。

关键词：微泡影象气体膨胀重氮化成象黑白幻灯片

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