低分子肝素对肾病综合征抗凝疗效的临床观察

目的：观察低分子肝素对肾病综合征的抗凝疗效。方法：34例原发性肾病综合征患者随机分为两组。一组用强的松治疗，另一组在强的松治疗基础上加用低分子肝素。结果：使用低分子肝素组尿蛋白明显下降，血浆白蛋白上升，纤维蛋白原（FIB）下降。结论：低分子肝素可作为肾病综合征抗凝药物。     

应用低分子肝素治疗心肌梗死临床观察

目的：探讨低分子肝素对心肌梗死的治疗作用。方法：80例患者随机分为治疗组和对照组。对照组行心肌梗死常规治疗；治疗组在对照组的基础上加用低分子肝素0．4ml，腹壁皮下注射，12h1次，10d为1个疗程，3个疗程后进行评估。结果：治疗组和对照组总有效率分别为90％和60％，经统计学分析差异有统计学意义。结论：低分子肝素对于心肌梗死有较好的治疗作用，值得临床推广使用。     

低分子质量肝素临床应用与研究

目的 探讨、研究低分子质量肝素在临床应用上起到的作用和效果.方法 选自2009年12月到2010年4月来本院治疗的42例采用低分子质量肝素进行临床抗凝治疗的患者,分析、研究使用低分子质量肝素的治疗效果.结果 42例采取低分子质量肝素进行抗凝治疗的患者中,14例心绞痛病例效果明显10例,起效4例;15例脑梗死病例效果明显13例效果明显,2例起效;8例心肌梗死病例6例效果明显,2例起效;5例静脉血栓病例2例效果明显,3例起效.结论 在抗凝治疗中低分子质量肝素起到非常好的治疗效果,值得临床上广泛使用.     

糖胺聚糖分子质量测定方法综述

糖胺聚糖(GAG)的生物活性和功能与其分子质量密切相关,而准确测定不同性质GAG的分子质量是目前GAG类药物研究的难题。本文对GAG分子质量测定方法的原理、优缺点及应用情况进行了综述,为GAG分子质量测定提供参考。     

肝素联合低分子右旋糖酐治疗难治性肾病综合征顽固性水肿观察

目的 观察低分子肝素联合低分子右旋糖酐治疗难治性肾病综合征顽固性水肿治疗作用.方法 对27例难治性肾病综合征顽固性水肿患者均给予常规治疗.其中14例加用低分子肝素联合低分子右旋糖酐治疗.结果 用低分子肝素联合低分子右旋糖酐治疗难治性肾病综合征顽固性水肿总有效率占86%.结论 肝素联合低分子右旋糖酐治疗非少尿型难治性肾病综合征顽固性水肿疗效确切,不良反应小,使用安全、方便.     

低分子肝素分子量的测定

用高效液相色谱法，以低分子肝素的标准对照品为标准，测定了低分子肝素的平均分子量。其重均分子量范围在3500～5000，分子县在8000以下者占85％以上。对该法的实验条件进行了探讨。     

低分子肝素钙治疗儿童紫癜肾炎疗效观察

目的:探讨低分子肝素钙对儿童紫癜肾炎的治疗效果。方法:两组均使用复方丹参、雷公藤常规治疗,治疗组加用低分子肝素钙10u/(kg·d)皮下注射,疗程7d,对照组给予双嘧达莫。结果:治疗组24h尿蛋白、血纤维蛋白原恢复正常明显快于对照组(P<0.01)。结论:低分子肝素钙对儿童紫癜肾炎疗效明显,使用安全。     

硫酸软骨素钠分子质量及其分布的测定

目的:采用两种方法测定硫酸软骨素钠的相对和绝对分子质量及其分布,并对两种分析方法进行比较。方法:色谱柱为TSKgel G3000SWXL,流动相为2.84%硫酸钠(pH 5.0,含0.02%叠氮化钠),流速为0.5 mL·min-1,柱温为35℃,分子排阻色谱(SEC)法为示差折光(RI)检测器,分子排阻色谱和多角度激光光散射联用(SEC-MALLS)法的检测器为示差折光检测器(DNDC仪)和激光光散射仪联用。结果:SEC法和SEC-MALLS法测得的分子质量结果存在较大差异。结论:由于目前国内没有合适的硫酸软骨素钠分子质量测定用标样,SEC法测定结果与真实分子质量存在较大误差,SEC-MALLS法准确,可靠。     

麻黄碱分子印迹整体柱的制备

目的：合成对麻黄碱具有特异识别能力的分子印迹聚合物整体柱。方法：以麻黄碱为模板分子，甲基丙烯酸为功能单体，乙二酸二甲基丙烯酸酯作为交联剂，以甲苯和十二醇混合溶液为致孔剂，用原位分子印迹技术，合成了麻黄碱分子印迹聚合物整体柱。结果：通过优化合成条件，结果显示模板分子、功能单体与交联剂之间的比例以1：2为最佳，致孔剂中甲苯的最佳含量为20-25％（v／V）；合成温度和合成时间分别为50℃和12h。通过扫描电镜和孔径分布曲线对得到的麻黄碱分子印迹聚合物进行了表征，结果显示聚合物中存在三种孔结构。在此基础上，研究了整体柱在有机相和水相中的识别能力。结论：得到的分子印迹聚合物整体柱，对模板分子具有特异的识别能力，在优化色谱条件下，麻黄碱和伪麻黄碱可以得到较好的分离。     

基于分子对接和分子动力学模拟技术筛选SARS-CoV-23CL蛋白酶抑制剂

目的 以分子对接和分子动力学模拟技术相结合的方法筛选得到严重急性呼吸系统综合征冠状病毒2 (severe acute respiratory syndrome coronavirus 2,SARS-CoV-2) 3CL蛋白酶的小分子抑制剂。方法 基于SARS-CoV-2 3CL蛋白酶的晶体结构(PDB ID:7K3T和7SI9),从PubChem数据库中筛选得到SARS-CoV-2 3CL蛋白酶的特异性抑制剂nirmatrelvir的结构类似物，使用Autodock进行非共价分子对接，使用AutoDockFR进行共价分子对接，采用Pymol和Ligplot软件对SARS-CoV-2 3CL蛋白酶和小分子进行相互作用模式分析，最后使用AMBER18进行小分子化合物与SARS-CoV-2 3CL蛋白酶复合物的分子动力学模拟，进一步验证分子对接结果，使用SwissADME对化合物进行成药性分析。结果 将78个nirmatrelvir结构类似物与SARS-CoV-2 3CL蛋白酶进行虚拟筛选和分子对接，得到了2个与nirmatrelvir作用相当的小分子化合物(PubChem ID:57842...     

高效凝胶渗透色谱法测定多糖纯度及分子量

用已知平均分子量(w)的T系列葡聚糖为标准,分别用两种不同的流动相,在Bio-Gel TSK柱上测定多糖的纯度及分子量。用线性回归法得出校正曲线。分子量w的平均偏差不超过5%。     

Antiviral and interferon-inducing activities of a new peptidomannan, KS-2, extracted from culture mycelia of Lentinus edodes

Oral (PO) administration of KS-2 to adult DDI mice resulted in a peak serum interferon (IF) titer of 800 units (U)/ml 20 hours after administration with detectable levels persisting until 30 hours. After intraperitoneal (IP) injection, a peak serum IF titer of 1,600 U/ml was detected and it followed the same time course as that of oral administration. The IF induced by KS-2 shared certain physico-chemical properties with the standard preparation of immune IF and was not neutralized by an antiserum against type I IF. In mice infected intranasally (IN) with influenza A2 (H2N2) virus, KS-2 was found to possess significant protective activities. Efficacy of the agent was evidenced by an increase in survivor number, a prolongation of mean survival time, an inhibition of the development of lung consolidation induced by the viral infection and a decrease in virus titer in lung tissues. Both PO and IP administrations of KS-2 protected mice against infection and significant antiviral activities were achieved not only by prophylactic but also chemotherapeutic administration. The protective activities of KS-2 against influenza virus infection in mice are discussed in view of the immunopotentiation of the host animals.     

Intestinal absorption and urinary excretion of antitumor peptidomannan KS-2 after oral administration in rats

A peptidomannan fraction designated as KS-2 was subjected for distribution study after oral administration. KS-2, exhibiting antitumor- and interferon-inducing action, was isolated from hot water extracts of mycelia of Basidiomycetes. For this purpose, KS-2 was labelled with fluorescein isothiocyanate. The amount and location of the labelled KS-2 (F-KS) was determined quantitatively by fluorescence intensity, and the molecular sizes were estimated by the fluorescence polarization method. The present data indicated that F-KS, when given orally, was absorbed partially via portal vein and intestinal lymphatics into the general circulation with intact molecular size. Moreover, F-KS was recovered in urine with concomitant breakdown in molecular weight. Histological evaluation revealed that F-KS was accumulated in the mesenteric lymph nodes, Peyer's patches, spleen, liver, and kidneys. These findings provide evidence that the polysaccharide KS-2 becomes accessible to the immune tissues and the vascular system; thus it may exert potentiating activity of defense system.     

Structure of a novel Ca2+ and calmodulin-dependent cyclic nucleotide phosphodiesterase inhibitor KS-619-1

The structure of KS-619-1, a potent inhibitor of Ca2+ and calmodulin-dependent cyclic nucleotide phosphodiesterase, was determined to be 8,13-dioxo-3-(2-oxopropyl)-5,6,8,13-tetrahydro-1,7,9,11- tetrahydroxybenz[a]naphtacene-2-carboxylic acid by spectral studies of KS-619-1 and its methyl derivative.     

KS-504 compounds, novel inhibitors of Ca2+ and calmodulin-dependent cyclic nucleotide phosphodiesterase from Mollisia ventosa

Novel inhibitors of Ca2+ and calmodulin-dependent cyclic nucleotide phosphodiesterase were isolated from the culture broth of a fungus, Mollisia ventosa KAC-1148. They were designated as KS-504a, KS-504b and KS-504d. A degradative product of KS-504a, called KS-504e, was also isolated and found to inhibit the enzyme. The 50% inhibitory concentration (IC50) values of KS-504a, KS-504b, KS-504d and KS-504e for bovine brain enzyme were 122, 109, greater than 500 and 139 microM, respectively.     

Structures of KS-501 and KS-502, the new inhibitors of Ca2+ and calmodulin-dependent cyclic nucleotide phosphodiesterase

The structures of KS-501 and KS-502, new inhibitors of Ca2+ and calmodulin-dependent cyclic nucleotide phosphodiesterase, were determined to be 2-(beta-D-galactofuranosyloxy)-6-heptyl-4-hydroxybenzoic acid 3-heptyl-5-hydroxyphenyl ester and 2-(beta-D-galactofuranosyloxy)6-heptyl-4-hydroxybenzoic acid 4-carboxy-3-heptyl-5-hydroxyphenyl ester, respectively, on the basis of chemical and physico-chemical evidences.     

芦荟多糖的分离纯化及其相对分子质量和含量测定

目的 研究库拉索芦荟多糖的分离纯化,测定分离得到的纯化多糖PSA2的相对分子质量及其多糖和蛋白质的含量. 方法采用水提醇沉法提取粗多糖,反复冻融法除蛋白质,DEAE-cellulose 52和Sephadex G-100凝胶色谱柱纯化多糖,得到纯化组分(PSA2),高效凝胶渗透色谱(HPGPC)法测定PSA2的相对分子质量,苯酚 硫酸法测定其多糖含量,考马斯亮蓝G-250法测定其蛋白质含量. 结果 PSA2的相对分子质量为8 457.4,其多糖含量为 61.0%,蛋白质含量为0.7%. 结论 多糖的提取工艺简单可行,HPGPC法,苯酚 硫酸法和考马斯亮蓝G-250法准确快捷.     

测定低分子量透明质酸相对分子质量的3种方法比较

目的比较3种测定低分子量透明质酸(LMWHA)相对分子质量(Mr)方法。方法分别采用特性黏度法、高效凝胶渗透色谱(HPGPC)法及多角度激光散射仪结合凝胶渗透色谱(GPC/MALLS)法测定LMWHA的Mr,并对所得结果进行对比分析。结果对于Mr介于10 000~100 000范围内的LMWHA,特性黏度法测得的Mr值与GPC/MALLS法测得的Mr值基本相同,而HPGPC法由于所用标准Mr对照品结构上的差异,测得的Mr与其它两种方法测得的值差异较大。结论在一定Mr范围内,特性黏度法和GPC/MALLS法均可用于测定LMWHA的Mr。     

Paralytic shellfish poisoning toxins in green mussels (Perna viridis) from the Gulf of Paria, Trinidad.

Paralytic shellfish poisoning (PSP) toxins were determined in green mussels (Perna viridis) collected from one collection site in the Gulf of Paria in Trinidad in 1999 and 2000. Aqueous extracts of PSP were purified by passage through C-18 SPE cartridges, oxidized with peroxide and periodate, respectively, then analyzed by HPLC with fluorescence detection. This procedure provided rapid and highly sensitive screening of samples for PSP toxins. Further purification of PSP-containing extracts using COOH SPE cartridges resulted in the separation and identification of individual PSP toxins. The method of analysis was validated by spike and recovery experiments, with 85-103% recoveries of mixed toxins. PSP toxins determined in our samples in both years were GTX2,3, dcGTX2,3, STX, and dcSTX, while GTX1,4 and NeoSTX were only identified in 1999 and 2000, respectively. In 1999, GTX1,4, GTX2,3 and dcGTX2,3 predominated, as compared to NeoSTX, GTX2,3 and dcGTX2,3 in 2000. However, mussel samples in 2000 contained higher total concentrations of detected PSP toxins than those of 1999. These results represent the first identification of specific PSP toxins in local shellfish and provide a basis for effective monitoring and control of these toxins in Trinidad.     

Clinico-biochemical study of experimental renal injuries in rats. 3. Relations between serum half-life of phenolsulfonphthalein and renal injuries

The serum half-life of PSP(PSP t/2) was determined in normal and nephropathy rats by repeated blood collection under an unanesthetized condition to estimate its usefulness as a renal functional parameter. In normal rats, the serum disappearance curve of PSP (5 mg/kg) could be resolved into two exponential components, and the mean PSP t/2 in the second component was 12 min (n=100). About 71% of the PSP loaded was excreted in urine and 19% in bile. A single subcutaneous injection of HgCl2 delayed the serum disappearance of PSP and simultaneously decreased its urinary excretion and increased its biliary excretion. The serum protein binding ratio of PSP became higher when the serum concentration of PSP was decreased, while it became lower when the serum albumin level was decreased. PSP t/2 in rats treated with gentamicin or puromycin amino-nucleoside as well as that in rats given HgCl2 was increased in correlation with changes in common renal functional parameters such as serum urea nitrogen, serum creatinine, urinary protein and morphologic changes of the kidney. Masugi-type nephritis rats showed no change in PSP t/2. Moreover, PSP t/2 was well correlated with the maximal tubular secretion rate of p-amino-hippuric acid. Since PSP t/2 can be determined periodically on the same animal, it is considered to have effective application as a renal functional test in rats, especially for examining tubular secretion.