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Surface modified solid lipid microparticles based on homolipids and Softisan 142:preliminary characterization

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Asian pacific Journal of Tropical Medicine 2010年第3期3卷 205-210页

作者： Nnamani pO Ibezim ec Attama AA Adikwu MU Drug Delivery Research Unit Department of PharmaceuticsFaculty of Pharmaceutical SciencesUniversity of Nigeria IcS-UNIDO International center for high Technology and New Materials AREA Science Park Science and Technology Education post-Basic(STEp-B) Abuja Nigeria

ObjectiveTo preliminarily investigate three different lipid matrices consisting of two natural homolipids from capra hircus (goat fat) and Bovine Spp. (tallow fat) and one semi-synthetic lipid (Softisan? 142) separately structured with phospholipon? 90G (p90G) as potential delivery systems for poorly water soluble drugs.MethodsThe structured lipid matrices were characterized by differential scanning calorimetry (DSc) and employed to prepare solid lipid microparticles (SLMs) by the melt homogenization method using gradient concentrations of polysorbate 80 and at different emulsification times of 2, 5.and 10 min using a Silverson mixer. The SLMs were analyzed for morphology and particle size, thermal properties, stability studies and determination of injectability.ResultsThe results showed that SLM production was optimum at 5.% of lipid matrices, 1.5.% of polysorbate 80 and emulsification time of 5.min. Increase in polysorbate 80 concentrations decreased the particle size of the SLMs. The SLMs were well formed, spherical, smooth and non-porous with particle sizes in the ranges of (13.90 ± 2.10) μm - (0.09 ± 0.01) μm for SLMs produced from the structured - tallow fat; (13.40 ± 1.30) μm - (0.10 ± 0.01) μm for the structured - goat fat and (13.40±2.00) μm - (2.10± 1.00)μm for the structured Softisan? 142 lipid matrices. DSc traces showed that Softisan? 142 was the most crystalline of all three bulk matrices due to its high enthalpy (?7.962 mW/mg) while tallow fat was the least (?5.067 mW/mg) but addition of p90G to the matrices lowered their enthalpies mostly in the structured goat fat matrices. The SLMs when stored at 4-6 ° were most stable and syringeable with 27 G needle.conclusionsThis suggests that structured goat fat matrices with the enthalpy of ?2.813 mW/mg will mostly favour drug loading of some poorly soluble drugs more than tallow fat (?4.892 mW/mg) and Softisan? 142 (?5.5.1 mW/mg).

关键词： phospholipon? 90G Solid lipid microparticle Goat fat Tallow fat Softisan? 142 characterization

lercanidipine对心肌病仓鼠心力衰竭过程中冠状反应和重构的作用(英文)

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Acta pharmacologica Sinica 2003年第3期24卷 9-16页

作者： Julie MASSIcOTTE, Antoine VIENS, Ming-hui YAO~1, Amedeo leONARDI~2,Giorgio SIRONI~2, hongbo WANG, Louis DUMONT~3 Département de pharmacologie, faculté de médecine, Universitéde Montréal, Montréal, Qc, c.nada h3c 3J7 1~Department of pharmacology, School of Medicine, Fudan University, Shanghai 200032, china 2~pharmaceutical R&D Division, Recordati SpA, Milan, Italy Departement de pharmacologie faculte de medecine Universite de Montreal Montreal QC 加拿大 H3C 3J7 Department of pharmacology School of Medicine Fudan University 上海 200032 pharmaceutical R&D Division Recordati SpA Milan Italy

AIM: lercanidipine is a new vasoselective dihydropyridine calcium channel blocker with a short plasma half-life,long duration of action, and demonstrated cardioprotective properties. We hypothesized that it might be effective at attenuating the adverse impact observed on the coronary compartment and myocardium in the transition phase to heart failure in the UM-X7.1 cardiomyopathic (cM) hamster. METhODS: The effects of 4-month exposure to lercanidipine 3 and 10 mg/kg (daily oral administration) Were evaluated in 15.-day-old cM hamsters and in agematched normal hamsters. coronary reactivity (reactive hyperemia to 30-s coronary occlusion) and the response to the administration of acetylcholine (100 nmol/L) and sodium nitroprusside (1 μmol/L) were assessed monthly, using the isolated perfused heart model. The left ventricular chamber dilatation index and wall thickness, myocardial fibrosis and myocardial capillary density (papillary muscle) were estimated in selected subgroups at monthly intervals. RESULTS

关键词：钙通道阻滞药心肌病冠状血管心力衰竭 lercanidipine 心肌

Salt Dynamics in Rhizosphere of puccinellia ciliata Bor. in a Loamy Soil

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pedosphere 2005年第6期15卷 784-791页

作者： ZhANG Zhen-hua c. TANG Z. RENGEL Agricultural Resource and Environmental Research center Jiangsu Academy of Agricultural Sciences Nanjing 210014 （China）. Soil Science and plant Nutrition School of Earth and Geographical Sciences The University of Western Australia 35 Stirling Highway Crawley WA 6009 （Australia） cRc plant-Based Management of Dryland Salinity The University of Western Australia 35 Stirling Highway Crawley WA 6009 （Australia） Department of Agricultural Sciences La Trobe University Bundoora Vic 3086 （Australia）

A glasshouse experiment using a rhizobox technique was conducted to examine salt dynamics in the rhizosphere of a salt-tolerant grass, puccinellia ciliata Bor. ’Irwin hunter’, grown in a loamy soil, and to study the effect of rainfall flush on salt accumulation in the rhizosphere. The rhizobox (10 × 5.5.× 5. cm) had a nylon mesh (1 μm) positioned vertically in the middle to create two compartments filled with soil amended with 1 g Nacl kg-1. The plants were grown in one compartment only. Flushed treatments received 275.mL of deionized water two days before harvest. In the plant-growing compartment, soils were sectioned vertically at 5.cm intervals. Significant differences in soil electrical conductivity (ec) (p 5. and ph (p 5. were observed for depths, but not between flushed and non-flushed treatments. In the no-plant compartment (rhizosphere), soil cores were taken horizontally at depths of 5. 20 and 40 cm and sliced at 1, 2, 3, 4, 5. 7, 10, 15.and 20 mm away from the roots. Soil ec and cl- concentration at the 5.and 20 cm depths, and Na+ concentration at the 5.cm depth significantly decreased (p 5. with the distance away from the root, but no significant differences were observed in soil ph and concentrations of the K+ and ca2+. The flush treatment only had significant influence on soil ec, ph, and cl- concentration at the 20 cm depth. Thus, salt accumulation could occur in the rhizosphere of salt-tolerant species on saline soils, and the periodic low rainfall might not have a strong influence on salt distribution in the rhizosphere and/or root zone.

关键词： leaching puccinellia ciliata Bor. rhizosphere salt dynamics

Functioal studies of MLc1 gene novel variants in six chinese patients with megalencephalic leukoencephalopathy with subcortical cysts

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Functioal studies of MLC1 gene novel variants in six Chinese...

Seasonal variations and sources of mass and chemical composition for pM_(10) aerosol in hangzhou,china

中国神经科学学会第四次会员代表大会暨第八届全国学术会议

作者： Jing-Min WANG~(1 #) Ajit Sigh Dhauchak~(2 #) hong-En WEI~3 hui XIONG~1 Ye WU~1 David colman~2 Xi-Ru WU~1 Yu-Wu JIANG~(1 *) 1 Department of pediatrics peking University First hospital Beijing china 2 montreal Neurological Institute montreal Quebec c.nada 3 Shanxi Medical University Taiyuan china

＜正＞Objective Megalencephalic leukoencephalopathy with subcortical cysts（MLc,MIM# 604004） is an autosomal recessively inherited disease resulting from a deficiency of MLc 1 *** previous data about this gene mutation in china have been *** objective was to identify and analyze MLc1 mutations in six chinese patients with（MLc） and functional studies of MLc1 gene novel *** Direct DNA sequencing,Immunoblots,and *** patient 1 was identified compound heterozygous mutations which one allele with the c. 218G＞A（p.G73E） missense mutation in exon 3 and the other allele with the c.772-1 G＞c splicing mutation in *** 2 was with the c.823G＞A（p.A275.） in exon 10 and the same splicing mutation with patient *** 3 was a homozygous mutation at c.772-1 G＞c in *** 4 was identified to be one allele with the c.5.3delcTcA（p.Y198X） in exon 7,and the other allele with the c.*48A＞T in 3’*** 5.and 6 were both with the same heterozygous variation c.65.＞A（p. R22Q） in exon 2,and the other allele with the c.206c＞T（p.S69L） in exon 3 for patient 5.and with the c.5.2G＞T（p.c171p） in exon 6 for patient *** immunostained transfected arstrocyte cells for hA-MLc1 and calnexin,an ER *** MLc1 was at astrocyte borders,whereas MLc 1 mutants G73E and Y198X are mainly intracellularly localized,except for A275., which mainly at cell *** blot analysis in arstrocyte cells transfected with WT MLc1 and with the amino acid changes G73E,Y198X and A275.,in comparison with the WT MLc1 in MLc1 expression,G73E mutation showed a reduced protein expression in transfected astrocytes,Y198X reduced at 36kDa and showed a band at about 25.Da in artrocyte cells,and no changes were observed for the *** Eight DNA variations of MLc 1 gene were identified:three novel missense mutations（p.R22Q,p.G73E,and p.A275.）,one novel splicing mutation（c.772-1 G＞c in IVS9-1）,one known nonsense mutation（p.Y198X）,one known missense

关键词： Megalencephalic leukoencephalopathy with subcortical cysts MLc1 mutation

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particuology 2009年第3期7卷 161-168页

作者： Junji cao Zhenxing Shen Judith c. chow Guowei Qi John G. Watson State Key Lab of Loess and Quaternary Geology - SKLLQG. Institute of Earth Environment ChineseAcademy of Sciences Xi'an. Shaanxi 710075 China Department of Environmental Science and Engineering. xi'an Jiaotong University. Xi'an 710049. china Division of Atmospheric Sciences. Desert Research Institute. Reno. USA hangzhou Municipal Environmental Monitoring center Hangzhou 310007 China

Aerosol observation was conducted for four seasons from September 2001 to August 2002 at five sampling sites in hangzhou, South china, on pM10 mass, 22 elements （Na, Mg, AI, Si, p, S, K, ca, Ti, V, cr, Mn, Fe, Ni, cu, Zn, As. Se, Br, cd, Ba, and pb）, 5.major ions （F^-, cl^ , NO3^-, SO4^2- , and Nh4^＋）, and organic and elemental carbon （Oc and ec）, showing that pM10 mass ranged from 46.7 to 270.8 μg/m^3, with an annual average of 119.2 μg/m^3. Na, AI, Si, S, K, ca, and Fe were the most abundant elements in pM10, most of S being in the form of SO4^2- . SO4^2-, NO3^-, and Nh4^＋ were the major ions, which contributed to about 20% of the pM10 mass. The mean seasonal concentrations for SO4^2- , averaged over all sites, were found to be 18.0, 18.5. 24,Z and 21.4 μg/m^3, for spring, summer, autumn, and winter, respectively, while the corresponding loadings for NO3^- were 7.2, 4.7, 7.1, and 11.2 μg/m^3, and for Nh4^＋ were 6.0, 5.9, 8.2, and 9.3 μg/m^3, in the form mostly of Nh4NO3 in spring, autumn, and winter, and mostly of （Nh4）2SO4 in summer. The low NO3^-/SO4^2- ratio found indicates coal combustion as the major source throughout the year. The mean annual concentrations of Oc and ec in pM10 were found to be 21.4, and 4.1 μg/m^3, respectively. Material balance calculation indicated that fugitive dust, the secondary aerosol, and carbonaceous matter were the most abundant species in pM10 for the four seasons, as is characteristic for cities in South china.

关键词： pM10 Elements lons carbon Material balance

competition for food in 2 populations of a wild-caught fish

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current Zoology 2018年第5期64卷 615-622页

作者： pierre J.c. chUARD Grant E. BROWN James W.A. GRANT Research School of Biology The Australian National University Canberra ACT 0200 Australia Departmentof Biology Concordia University 7141 Sherbrooke Street West Montreal Quebec Canada H4B 1R6

Aggressive behavior when competing for resources is expected to increase as the ratio of competitors-to-resource ratio （cRR） units increases. Females are expected to be more aggressive than males when competing for food when body size is more strongly related to reproductive suc- cess in females than in males, whereas aggression is predicted to decrease under high ambient predation risk by natural selection. Under the risk allocation model, however, individuals under high ambient predation risk are expected to be more aggressive, and forage more in the absence of imminent risk than their low risk counterparts. An interaction between adult sex ratio （i.e., adult males/females）, ambient predation risk （high vs. low）, and sex on intrasexual competition for mates in Trinidadian guppies poecilia reticulata has been shown. The interaction suggested an increase in aggression rates as cRR increased, except for males from the high predation population. To compare the patterns of competition for food versus mates, we replicated this study by using food patches. We allowed 4 male or 4 female guppies from high and low predation populations to com- pete for 5. 3, or 1 food patches. The foraging rate was higher in a high rather than low ambient pre- dation risk population. Surprisingly, cRR, sex, and population of origin had no effect on aggression rates. Despite other environmental differences between the 2 populations, the effect of ambient predation risk may be a likely explanation for differences in foraging rates. These results highlight the importance for individuals to secure food despite the cost of competition and predation.

关键词： aggression competitor-to-resource ratio foraging poecifia reticulata population differences predation risk sex

疏血通联合丁苯酞对急性缺血性脑卒中患者神经功能及炎症反应的影响

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Journal of chinese pharmaceutical Sciences 2024年第3期33卷 241-247页

作者：楼昆昂卢栋升潘奕杨乐言闫焕付浩李银丹杨金姬曲苗浙江中医药大学浙江杭州310053 重庆市人民医院重庆400010 武警特色医学中心天津300162 黑龙江中医药大学黑龙江哈尔滨150006

为了观察疏血通联合丁苯酞对急性缺血性脑卒中(AIS)患者神经功能及炎症反的影响,本研究以2019年6月~2020年6月住院的98例AIS患者为研究对象,随机分为两组,每组49例。对照组给予丁苯酞注射液治疗,静脉滴注, 100 mL/次, 2次/天;观察组在... 详细信息

为了观察疏血通联合丁苯酞对急性缺血性脑卒中(AIS)患者神经功能及炎症反的影响,本研究以2019年6月~2020年6月住院的98例AIS患者为研究对象,随机分为两组,每组49例。对照组给予丁苯酞注射液治疗,静脉滴注, 100 mL/次, 2次/天;观察组在对照组基础上,静脉滴注疏血通注射液, 6 mL溶于25. mL 5.的葡糖糖溶液中, 1次/天。两组均治疗14天。观察两组入院当天、治疗后7天、14天美国国立卫生院脑卒中量表(NIhSS)、改良Barthel指数(MBI)量表评分及血清白介素-6(IL-6)、肿瘤坏死因子-α(TNF-α)、c-反应蛋白(cRp)、可溶性细胞间粘附分子(sIcAM-1)水平变化,并观察两组蒙特利尔认知评估量表(MocA)和简易精神状态检查量表(MMSE)评分变化。治疗后两组NIhSS评分显著降低(p5.,MBI评分显著升高(p 5.,且治疗后7天、14天观察组NIhSS和MBI评分明显优于对照组(p 5.;治疗后两组MocA和MMSE评分均明显升高(p 5.,且治疗后7天、14天观察组认知功能评分明显高于对照组(p 5.;治疗后两组血清IL-6、TNF-α、cRp、s IcAM-1水平均明显降低(p 5.,且治疗后7天、14天观察组炎症因子水平明显低于对照组(p5.。提示疏血通联合丁苯酞治疗AIS患者可更好的促进神经功能恢复、提高生活能力,减轻炎症反应,改善认知功能,具有很好的临床应用价值。

关键词：疏血通丁苯酞急性缺血性脑卒中炎症反应认知功能

Bradykinin potentiates 5.hT3 receptor-mediated current in rat trigeminal ganglion neurons

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Acta pharmacologica Sinica 2005年第4期26卷 428-434页

作者： Wang-ping hU~(1,2) Xue-mei LI~2 Ji-liang WU~3 Min ZhENG~3 Zhi-wang LI~4 2 Department of physiology,3 Department of pharmacology,Xianning college,Xianning 437100,china 4 Department of Neurobiology,Tongji Medical college of huazhong University of Science and Technology,Wuhan 430030,china Departmentofphysiology XianningCollegeXianning437100China

Aim:To explore the modulatory effect of bradykinin （BK） on 5.hT3receptor-mediated current in trigeminal ganglion （TG） neurons in ***:The whole-cell patch-clamp technique was used to record 5.hT-activated currents (I5.hT) inneurons freshly dissociated from rat *** were applied by rapid ***:The majority of the neurons examined responded to 5.hTapplied externally with an inward current （76.3%,74/97） that could be blocked bythe 5.hT3receptor antagonist,IcS-205.930 (1×10-6mol/L).In 66 of the 74 cellssensitive to 5.hT （89.2%）,pretreatment for 30 s with BK (1×10-6-1×10-10mol/L)could potentiate I5.hTwith the maximal modulatory effect occurring at10-7mol/L BK （71.6%+4.9%）.BK shifted the 5.hT concentration-response curveupwards with an increase of 68.9%±7.2% in the maximal current response,but withno significant change in the ec5.value （19.1±3.2 μmol/L vs 20.9±3.5.μmol/L;t-test,p>0.05.n=8）.BK potentiated I5.hTin a holding potential-independent manner anddid not alter the reverse potential of *** BK-induced potentiation ofI5.hTwas almost completely blocked by hoe 140 (5.10-7mol/L),a selective B2BKreceptor antagonist,and was removed after intracellular dialysis of GF-109203X（2 μmol/L）,a selective protein kinase c （pKc） inhibitor,with the re-patch ***:pre-application of BK exerts an enhancing effect on I5.hTvia a pKc-dependent pathway in rat TG neurons,which may explain the peripheral'mecha-nism of pain and hyperalgesia caused by,for example,tissue damage andinflammation.

关键词： bradykinin 5.hT3 serotonin receptor regulation patch-clamp techniques trigeminal ganglion

protective effects of Amaranthus hybridus against aflatoxin B1 and fumonisin B1-induced genotoxicity in h4IIE-luc cells

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hepatoma Research 2015年第1期1卷 136-146页

作者： Mohamed I.M.Ibrahim Rialet pieters Sekena h.Abdel-Aziem Anna M.vander Walt cornelius c.Bezuidenhout John p.Giesy Mosaad A.Abdel-Wahhab Food Toxicology and contaminants Department National Research CenterDokkiCairo 12622Egypt Unit of Environmental Sciences and Management North-West UniversityPrivate Bag X6001Potchefstroom 2520South Africa cell Biology Department National Research CenterDokkiCairo 12622Egypt Department of Veterinary Biomedical Sciences and Toxicology centre University of SaskatchewanSaskatoonSaskatchewan S7N 5B4Canada Department of Zoology and Center for Integrative ToxicologyMichigan State UniversityEast LansingMI 48824USA Department of Biology and chemistry and State Key Laboratory in Marine pollution City University of Hong KongKowloonHong KongChina School of Biological Sciences University of Hong KongHong KongChina State Key Laboratory of pollution control and Resource Reuse School of the EnvironmentNanjing UniversityNanjing 210093JiangsuChina Department of Biology Hong Kong Baptist UniversityHong KongChina

Aim:protective effects of aqueous extract of Amaranthus hybridus against afl atoxin B1(AFB_(1))and/or fumonisin B1(FB_(1))on the h4IIE-luc cell line were determined by use of the methyl thiazol tetrazolium viability assay and disruption of DNA ***:h4IIE-luc cells were incubated with different concentrations of AFB_(1) and/or FB_(1) for 24 and 48 h with or without aqueous extract of ***:AFB_(1) decreased the viability of cells after 24 and 48 h of ***_(5.)values for AFB_(1) were 10.5.and 1.8μmol/L for the two periods,*** the 48 h exposure to mycotoxin repeated with a pre-treatment of 20 and 40μg/mL extract of ***,the ec_(5.)changed to 3.88 and 7.67μmol/L,respectively.h4IIE-luc cells exposed to FB_(1) for 24 h responded more than those incubated for 48 *** treated with a combination of AFB_(1) and FB_(1) were less viable with a signifi cant decrease in the greater *** mixture of AFB_(1) and FB_(1) resulted in a signifi cant threat to h4IIE-luc as indicated by the absence or appearance of new bands in random amplifi ed polymorphic DNA analysis,which demonstrated damage to *** protective effects were probably due to greater content of total phenolics,carotenoids,β-carotene,folic-,linolenic-,linoleic and palmitic acids,as well as calcium,magnesium,iron,zinc,and selenium observed in the ***:Exposure to 40μg/mL of extract of *** protected cells from damage to DNA by stabilizing DNA.

关键词： Afl atoxin B1 Amaranthus hybridus cytotoxicity DNA fumonisin B1 hepatoma cells methyl thiazol tetrazolium assay