Pharmacokinetics and Biodegradation of Chitosan in Rats

Chitosan, an excellent biomedical material, has received a widespread in vivo application. In contrast, its metabolism and distribution once being implanted were less documented. In this study, the pharmacokinetics and biodegradation of fluorescein isothiocyanate(FITC) labeled and muscle implantation administrated chitosan in rats were investigated with fluorescence spectrophotometry, histological assay and gel chromatography. After implantation, chitosan was degraded gradually during its distribution to diverse organs. Among the tested organs, liver and kidney were found to be the first two highest in chitosan content, which was followed by heart, brain and spleen. Urinary excretion was believed to be the major pathway of chitosan elimination, yet 80% of chitosan administered to rats was not trackable in their urine. This indicated that the majority of chitosan was degraded in tissues. In average, the molecular weight of the degradation products of chitosan in diverse organs and urine was found to be 65 k Da. This further confirmed the in vivo degradation of chitosan. Our findings provided new evidences for the intensive and safe application of chitosan as a biomedical material.     

新型壳聚糖季铵盐衍生物的合成与表征

采用甲磺酸作为溶剂兼作氨基保护试剂,对壳聚糖上的羟基选择性酯化,再游离出氨基并对其氯乙酰化,最后进行吡啶成盐,得到新型水溶性的壳聚糖季铵盐衍生物,产物的结构通过核磁共振氢谱和红外光谱进行了表征,从而为壳聚糖季铵盐衍生物的制备提供了一种新途径。     

Synthesis and Characterization of a Hydroxyethyl Derivative of Chitosan and Evaluation of Its Biosafety

Hydroxyethyl chitosan(HE-chitosan) is a water-soluble derivative of chitosan with many apparent biological properties. For example, it is non-toxic and rapidly biodegradable. Moreover, HE-chitosan has advantages in water-solubility, moisture retention and gelling property due to its hydroxyethyl group. However, the biocompatibility and biodegradability of this multifunctional derivative have rarely been documented although they are critical for its application in biomedical and clinical treatments. The purpose of this work was to evaluate the biosafety of HE-chitosan, and draw important clues for its diverse applications. HE-chitosan was synthesized and characterized its chemical structure with FTIR. Its molecular weight(MW) was determined by gel permeation chromatography(GPC), and its deacetylation degree(DD) was investigated through potentiometric analysis. The cytotoxicity of HE-chitosan on mouse fibroblast cell L929 was tested. The biocompatibility and biodegradability of HE-chitosan in rat and rabbit were evaluated. The FTIR results indicated that the hydroxyethyl groups were linked to C6 of chitosan. The GPC analysis confirmed that its Mw was about 90.01 k Da. It was also demonstrated that HE-chitosan had excellent biocompatibility and biodegradability in vivo and had no cytotoxicity on L929. These findings indicated that HE-chitosan can potentially be applied as a biomaterial in tissue engineering, drug delivery, and other biomedical fields.     

包被壳寡糖对刺参生长性能和免疫反应的影响

为研究不同添加量的包被壳寡糖对刺参生长和免疫的影响,在基础饲料中分别添加质量分数0.00%、0.75%、1.50%、2.25%及3.00%包被壳寡糖配制成实验饲料,养殖初始质量(5.03±0.03)g刺参(Apostichopus japonicus)60 d。结果表明:1.50%添加组刺参增重率和特定生长率高于对照组(P0.05),各添加组体壁水分、粗蛋白、粗脂肪、粗灰分含量差异不显著(P0.05),1.50%添加组吞噬活性显著高于对照组(P0.05),1.50%添加组的呼吸爆发活力在各时间点较对照组有显著提高(P0.05),其体腔上清液LZM活性于实验60 d较对照组有显著提高(P0.05),体腔上清液SOD活性于实验50、60 d较对照组有显著提高(P0.05);各组ACP活性、NO活性、补体C_3活性和PO活性无显著性差异(P0.05)。饲料中添加1.50%包被壳寡糖能提高刺参生长性能,对刺参的免疫能力具有一定促进作用。     

Overview of In—Situ Biodegradation and Enhancement

Microbial degradation technologies have been developed to restore ground water quality in aquifers polluted by or-ganic contaminants effectively in recent years. However, in course of the degradation, the formation of biofilms in ground wa-ter remediation technology can be detrimental to the effectiveness of a ground water remediation project. Several alternatives are available to a remedial design engineer, such as Permeable Reactive Barriers (PRBs) and in -situ bioremediation, Hy-drogen Releasing Compounds (HRCs) barrier, Oxygen Releasing Compounds (ORCs) barrier etc. which are efficient and cost ?effective technologies. Excessive biomass formation renders a barrier ineffective in degrading the contaminants, Efforts are made to develop kinetics models which accurately determine bio - fouling and bio - film formation and to control excessive biomass formation.     

Overview of In-Situ Biodegradation and Enhancement

ＩｎｔｒｏｄｕｃｔｉｏｎＲｅｍｅｄｉａｔｉｏｎｂｙｎａｔｕｒａｌａｔｔｅｎｕａｔｉｏｎ (ＲＮＡ)ｉｓｔｈｅｐｒｅｆｅｒｒｅｄｍｅｔｈｏｄｆｏｒｒｅｍｅｄｉａｔｉｎｇｇｒｏｕｎｄｗａｔｅｒｃｏｎｔａｍｉ ｎａｔｅｄｂｙｔｈｅａｒｏｍａｔｉｃｆｕｅｌｈｙｄｒｏｃａｒｂｏｎｓ ,ｂｅｎｚｅｎｅ ,ｔｏｌｕｅｎｅ ,ｅｔｈｙｌｂｅｎｚｅｎｅ ,ａｎｄｘｙｌｅｎｅ (ＢＴＥＸ)ｅｔｃ .(Ｊｅｆ ｆｒｅｙ ,2 0 0 1) .ＢｕｔｔｈｅｒｅａｒｅｃｅｒｔａｉｎｃｏｎｄｉｔｉｏｎｓｕｎｄｅｒｗｈｉｃｈＲＮＡｉｓｉｎａｄｅｑｕａｔｅ…     

壳寡糖对吉富罗非鱼幼鱼生长性能、非特异性免疫及血液学指标的影响

用添加质量分数0.00(对照组)、0.10%、0.30%、0.50%和0.70%壳寡糖的饲料饲喂初始体重(3.81±0.23)g的吉富罗非鱼幼鱼(Oreochromis niloticus)10周,研究不同浓度壳寡糖的添加对吉富罗非鱼幼鱼的生长、非特异性免疫功能以及血脂指标的影响。结果表明:与对照组相比,在4个不同浓度添加组中,添加质量分数0.50%壳寡糖能显著提高幼鱼的增重率(P<0.05)、特定生长率(P<0.05),并降低饲料系数(P<0.05);添加质量分数0.3%和0.5%壳寡糖能显著提高幼鱼抗嗜水气单胞菌感染的能力(P<0.01);添加质量分数0.10%、0.30%、0.50%壳寡糖能显著提高幼鱼血清中碱性磷酸酶活性(P<0.05)。同时,各浓度的壳寡糖均能明显提高幼鱼血清中溶菌酶和超氧化物歧化酶活性以及抗嗜水气单胞菌感染的能力(P<0.05),并降低幼鱼血清中总胆固醇和低密度脂蛋白胆固醇水平(P<0.05)。在本实验条件下,添加壳寡糖可提高吉富罗非鱼幼鱼生长性能、饲料利用率、非特异性免疫功能和调节血脂水平,添加量以质量分数0.30%~0.50%为宜。     

Bioaccumulation and Biodegradation of Sulfamethazine in Chlorella pyrenoidosa

Intensive use of sulfamethazine(SM_2) in aquaculture has resulted in some detrimental effects to non-targeted organisms. In order to assess its potential ecological risk, it is crucial to have a good understanding on the bioaccumulation and biodegradation of SM_2 in Chlorella pyrenoidosa. The microalgae were treated with 2, 4, and 8 mg L~(-1) of sulfamethazine for 13 days, respectively, showing that the inhibition effects of sulfamethazine on the growth of Chlorella pyrenoidosa increased progressively as the concentrations of sulfamethazine increasing from 2 to 8 mg L~(-1). The peak concentrations of sulfamethazine accumulated in C. pyrenoidosa were 0.225, 0.325, and 0.596 ng per mg FW on day 13 for three treatment groups, respectively, showing a great ability to deplete sulfamethazine from the culture media. On day 13, the percentages of biotic degradation were 48.45%, 60.21% and 69.93%, respectively. The EC_(50) of 10.05 mg L~(-1) was derived which showed no significant risk for C. pyrenoidosa with a calculated risk quotient 1. The activities of superoxide dismutase and catalase increased progressively in response to sulfamethazine and showed a positive correlation to the treatment concentrations. The highest superoxide dismutase activity was achieved at the concentration of 8 mg L~(-1) after 2 d of exposure, which was 1.89 folds higher than that of the control. The activity of catalase has a similar pattern to that of superoxide dismutase with the maximum activity achieved at day 2, which was 3.11 folds higher compared to that of the control. In contrast to superoxide dismutase and catalase, the maximum glutathione S-transferase activity was observed at day 6, showing 2.2 folds higher than that of the control.     

Overview of In - Situ Biodegradation and Enhancement

Microbial degradation technologies have been developed to restore ground water quality in aquifers polluted by organic contaminants effectively in recent years. However, in course of the degradation, the formation of biofilms in ground water remediation technology can be detrimental to the effectiveness of a ground water remediation project. Several alternatives are available to a remedial design engineer, such as Permeable Reactive Barriers (PRBs) and in -situ bioremediation, Hydrogen Releasing Compounds (HRCs) barrier, Oxygen Releasing Compounds (ORCs) barrier etc. which are efficient and cost- effective technologies. Excessive biomass formation renders a barrier ineffective in degrading the contaminants, Efforts are made to develop kinetics models which accurately determine bio - fouling and bio - filn formation and to control excessive biomass formation.     

Influence of Cathode Modification by Chitosan and Fe3+ on the Electrochemical Performance of Marine Sediment Microbial Fuel Cell

The electrochemical performances of cathode play a key role in the marine sediment microbial fuel cells(MSMFCs) as a long lasting power source to drive instruments, especially when the dissolved oxygen concentration is very low in seawater. A CTS-Fe³⁺ modified cathode is prepared here by grafting chitosan(CTS) on a carbon fiber surface and then chelating Fe³⁺ through the coordination process. The electrochemical performance in seawater and the output power of the assembled ...     

壳聚糖对腐生葡萄球菌的作用机制

【目的】探究壳聚糖处理对腐生葡萄球菌(Staphylococcus saprophytic)的作用机制。【方法】通过光密度值结合菌液澄清度法综合确定壳聚糖对腐生葡萄球菌的最小抑菌浓度(Minimum Inhibitory Concentration,MIC),分析其在MIC与2MIC的壳聚糖作用下的微生物生长曲线、电导率值、碱性磷酸酶(Alkaline Phosphatase,AKP)含量、过氧化氢酶(Catalase,CAT)含量、苹果酸脱氢酶(Malatedehydrogenase,MDH)含量与生物膜生成量等指标变化,并结合扫描电镜(ScanningElectronMicroscopy,SEM)观察其作用后对菌体细胞形态变化影响,综合评价壳聚糖处理对腐生葡萄球菌的作用机制。【结果与结论】壳聚糖对腐生葡萄球菌的MIC为1.25 mg/mL;菌体经MIC和2MIC处理后,其正常生长受到抑制,细胞壁被破坏,细胞膜通透性改变,CAT与MDH含量降低,其作用效果与壳聚糖浓度正相关;SEM结果显示,与对照CK组对比,腐生葡萄球菌经MIC壳聚糖处理后,菌体形状不规则,表面皱褶;经2MIC壳聚糖处理后,菌体表面产生泡状物且黏附明显,表明壳聚糖使腐生葡萄球菌菌体细胞壁受损,菌体生长受到抑制,胞内保护酶与三羧酸循环中的关键酶活性降低,细胞代谢能力随之下降,细胞膜结构完整度受到破坏,最终导致菌体死亡。     

恩诺沙星在红笛鲷体内的药代动力学

在水温26±2℃、盐度28条件下,恩诺沙星(enrofloxacin,EF)按5 mg/kg的剂量腹腔注射和口灌红笛鲷(Lutjanus sanguineus),用反相高效液相色谱法研究恩诺沙星在红笛鲷体内的药代动力学和组织分布。结果显示:注射和口灌后红笛鲷血浆的药时数据均符合一级吸收二室模型;血药达峰时间(tp)分别为0.75和1.5 h,血药质量浓度峰值(cmax)分别为5.22和3.94μg/mL,药时曲线下面积(AUC)分别36.98和17.24 mg/(L.h),消除半衰期(t1/2β)分别为13.28和9.18 h;恩诺沙星在组织中分布较广,注射和灌服给药肌肉、肝脏和肾脏的cmax分别为3.53和3.40μg/g、4.08和3.98μg/g、11.23和5.40μg/g,tp分别为1.5和2.0 h、1.0和2.0 h、0.75和1.5 h,AUC分别33.17和23.12 mg/(L.h)、39.36和18.20 mg/(L.h)、98.97和56.69 mg/(L.h);EF在红笛鲷体内消除速度较慢,注射和灌服给药肌肉、肝脏和肾脏的t1/2β分别为22.08和83.32 h、41.52和94.47 h、20.94和21.81 h。表明恩诺沙星注射给药在红笛鲷体内的吸收和消除均快于口灌给药。     

甲砜霉素在眼斑拟石首鱼体内的药代动力学研究

在水温(20±2)℃条件下,以10 mg/kg的剂量对健康眼斑拟石首鱼(Sciaenops ocellatus)腹注和口灌甲砜霉素,采用HPLC-MS/MS方法测定组织中的药物浓度,研究甲砜霉素在该鱼种体内的代谢动力学。结果显示,两种给药方式下眼斑拟石首鱼血浆药时数据均符合一级吸收二室模型;腹注给药后血浆、肾脏、肝脏和肌肉的药物峰值(C_(max))分别为5.50μg/m L、10.96μg/g、6.61μg/g和3.50μg/g,达峰时间(tp)分别为1.2、1.5、2.0和6.0 h,消除半衰期(t1/2β)分别为44.82、17.27、29.39和26.99 h;口灌给药后血浆、肾脏、肝脏和肌肉的Cmax分别为4.62μg/m L、7.11μg/g、4.99μg/g和3.58μg/g,tp分别为2.4、4.0、4.0和4.0 h,t1/2β分别为14.67、27.34、37.68和32.65 h。腹注给药方式下甲砜霉素在眼斑拟石首鱼体内的吸收快于口灌给药,在肾脏、肝脏和和肌肉中的消除快于口灌给药,在血浆中的消除则慢于口灌给药。     

氟苯尼考在美国红鱼体内的药代动力学和组织分布

在水温20±2℃的条件下,按10 mg/kg的剂量通过腹腔注射和口灌方式,以液-质联用法研究氟苯尼考在美国红鱼(Sciaenops ocellatus)体内的药代动力学和组织分布,所得药时数据用DAS3.0软件分析。结果显示,美国红鱼腹注氟苯尼考后血药经时符合一级吸收二室模型,而口灌氟苯尼考则符合一级吸收一室模型;腹腔注射组,美国红鱼血浆、肝脏、肾脏、肌肉的氟苯尼考出峰时间(tp)分别为0.5、4、0.5、4 h,峰浓度(ρmax)分别为15.47、9.90、6.83、2.73μg/g,药时曲线下面积(AUC)分别为394.10、105.66、157.37、120.01 mg/(L·h),消除半衰期分别为45.39、7.42、148.25、39.22 h;口灌组,美国红鱼血浆、肝脏、肾脏、肌肉的氟苯尼考出峰时间(tp)分别为2、1.5、4、4 h,峰浓度(ρmax)分别为6.31、5.44、9.10、5.12μg/g,药时曲线下面积(AUC)分别为136.21、162.32、213.32、157.37 mg/(L·h),消除半衰期t1/2β分别为12.08、27.9、14.85、38.53 h。结果表明,氟苯尼考注射给药在美国红鱼体内的吸收快于口灌给药,腹注给药氟苯尼考除在肝脏中的消除快于口灌给药外,在血浆、肌肉和肾脏中的消除均慢于口灌给药。     

Biodegradation of Enteromorpha Polysaccharides by Intestinal Micro-Community from Siganus oramin

Micro-communities are supposed to have more potential functions of biodegradation of polysaccharides than single strain; however, the intestinal micro-communities involved in the biodegradation of Enteromorpha polysaccharides(EP) were seldom reported. In order to obtain the EP-degrading micro-community, the intestines of Siganus oramin was obtained to isolate the micro-communities, which were enriched by 0.3% of EP as the sole carbon source. A stable micro-community with EP degradative capability was achieved after seven generations of subculture, named H1. Results showed that H1 was able to degrade 75% of EP within 24 hours, and the activity of EP lyases reached 500 U m L~(-1) in 32 hours. With denaturing gradient gel electrophoresis(DGGE) and 16 S r RNA gene clone library analysis, ten bacteria closely related to Marinomonas pontica, Microbacterium sp., Leucobacter chironomi, Cyclobacterium sp., Algoriphagus winogradskyi, Pseudoalteromonas sp. and Vibrio sp. were determined. Furthermore, compared with the DGGE bands sequence and the clone library analysis, the dominant bacteria of the EP-biodegrading micro-community were Pseudoalteromonas sp. and Vibrio sp., with the respective proportion of 38% and 46%, and they should play an important role in EP degradation together with other degrading bacteria in the micro-community H1.     

壳聚糖希夫碱铜配合物的制备及其催化性能

采用微波辐射加热法使壳聚糖与水杨醛反应生成壳聚糖希夫碱,然后将其与铜盐配位得到壳聚糖希夫碱铜配合物,用UV、FTIR、TG表征产物的结构,并探讨该配合物对过氧化氢分解的催化性能。研究结果表明:壳聚糖希夫碱铜配合物对过氧化氢有良好的催化活性,常温(25℃)常压,pH=7.0的条件下放置12 h,催化H2O2的分解达99.8%,该配合物重复使用3次还保持较好的催化活性。     

壳聚糖希夫碱铜配合物的制备及其催化性能

采用微波辐射加热法使壳聚糖与水杨醛反应生成壳聚糖希夫碱。然后将其与铜盐配位得到壳聚糖希夫碱铜配合物。用UV、FTIR、TG表征产物的结构，并探讨该配合物对过氧化氢分解的催化性能。研究结果表明：壳聚糖希夫碱铜配合物对过氧化氢有良好的催化活性。常温（25℃）常压．pH=7．0的条件下放置12h,催化H2O2的分解达99．8％。该配合物重复使用3次还保持较好的催化活性。     

Enhanced Biodegradation of High-Salinity and Low- Temperature Crude-Oil Wastewater by Immobilized Crude-Oil Biodegrading Microbiota

High salt and low temperature are the bottlenecks for the remove of oil contaminants by enriched crude-oil degrading microbiota in Liaohe Estuarine Wetland(LEW),China.To improve the performance of crude-oil removal,microbiota was further immobilized by two methods,i.e.,sodium alginate(SA),and polyvinyl alcohol and sodium alginate(PVA+SA).Results showed that the crude oil was effectively removed by the enrichment with an average degrading ratio of 19.42-31.45 mg(L d)^?1.The optimal inoculum size for the n-alkanes removal was 10%and 99.89%.Some members of genera Acinetobacter,Actinophytocola,Aquabac-terium,Dysgonomonas,Frigidibacter,Sphingobium,Serpens,and Pseudomonas dominated in crude-oil degrading microflora.Though the removal efficiency was lower than free bacteria when the temperature was 15℃,SA and PVA+SA immobilization im-proved the resistance to salinity.The composite crude-oil degrading microbiota in this study demonstrated a perspective potential for crude oil removal from surface water under high salinity and low temperature conditions.     

盐酸氯苯胍在红笛鲷体内的药代动力学及残留消除规律

在水温(28±2)℃、盐度28条件下,将盐酸氯苯胍(Robenidine hydrochloride,ROBH)按30 mg/kg的剂量口灌红笛鲷(Luthjanus sanguineus),用HPLC-MS/MS法研究ROBH在红笛鲷体内的药代动力学和残留消除规律。结果表明:单剂量口灌给药后,红笛鲷血浆中ROBH的药时数据符合一级吸收二室模型,药物在血浆中的达峰时间t_p为1.79 h,血药浓度峰值C_(max)为211.38μg/L,药时曲线下面积(AUC_(0-∞))为5 229.16μg/(L·h),消除半衰期(t1/2β)为46.99 h。ROBH在红笛鲷其他组织中分布较广,消除速度较慢,肌肉、肝脏和肾脏的C_(max)分别为37.58、863.02、1 063.24μg/kg,t_p均为1.5 h,AUC0-∞分别1 017.03、20 841.20、30 743.04μg/(kg·h);t1/2β分别为26.35、14.05和24.31 h。连续5 d口灌给药后,红笛鲷血浆、肌肉、肝脏和肾脏中的药物消除半衰期t1/2分别为46.14、36.11、28.62、26.92 h。以10μg/kg为最高残留限量,肌肉作为食用靶组织,在本试验条件下,建议休药期不少于7 d。     

复方新诺明在罗氏沼虾中的药代动力学和组织分布

研究了单剂量肌肉注射给药[甲氧苄氨嘧啶(SMZ)0 60 mg/kg]、口灌给药[磺胺甲基异噁唑(SMZ)100 mg/kg]和复方口灌给药(SMZ 100 mg/kg和TMP 20 mg/kg)三种给药方式下,SMZ和TMP在罗氏沼虾中的代谢动力学,分析了SMZ和TMP血淋巴、肌肉和肝胰腺中的分布特征。结果表明,SMZ以肌肉注射方式给药后的血淋巴中,药物经时浓度曲线符合二室开放房室模型,而SMZ&TMP口灌给药后却不能用房室模型拟合。肌注给药后,SMZ的消除半衰期(t1/2β)为24.92 h,单方和复方口灌给药后SMZ的消除半衰期(t1/2β)分别为40.70和47.197 h。复方口灌给药后TMP的消除半衰期(t1/2β)为28.77 h,TMP对SMZ的药代动力学并无显著影响。口灌给药后,SMZ和TMP在肝胰腺中的药物浓度高于同时间肌肉中的药物浓度,但肌肉和肝胰腺中的SMZ消除速度基本一致。