砂海星海星皂甙的制备

采用甲醇提取法和乙醇提取法从砂海星提取了海星总皂甙，其产率分别为０．１２％和０．１３％，赠品经理化实验，溶血实验，紫外光谱，红外光谱及质谱分析鉴定，证明提取的为海星皂甙。砂海星海星皂甙熔点为１７１－１７５℃。     

海燕组织中海星皂甙的分布及溶血指数的测定

采用甲醇法从黄海产海燕各组织中提取了海星总皂甙,产品经理化实验,溶血实验,紫外光谱,红外光谱的分析鉴定,证明提取物为海星总皂甙。海燕海星总皂甘的熔点为２４２℃－２５５℃。     

RP-HPLC法测定重楼中甾体皂甙的含量

为寻找和合理利用植物资源及控制生药质量，用ＲＰＨＰＬＣ法分离并测定了重楼中９种甾体皂甙，其中４种为偏诺皂甙元的糖甙，５种为薯芋皂甙元的糖甙。分析柱为Ｃ８（４６ｍｍ×２５０ｍｍ），乙腈—水（４２∶５８）为流动相，检测波长２０３ｎｍ，９种甾体皂甙峰与其相邻峰能达基线分离，且线性良好，γ＝０９９９６～０９９９９，回收率９７１％～１００２％。本法简便、快速、灵敏。用此法对不同产地重楼中９种甾体皂甙类化合物进行了分析，结果提示不同产地重楼中各成分含量差异较大。     

甲壳低聚糖的制备和分析

解决壳聚精的水不溶性,拓宽壳聚精的应用范围。方法：直接用过氧化氢对高分子量、高脱乙酸化度的壳聚糖进行非均相降解、制备了水溶性甲壳低聚糖产品,对产品进行红外光谱结构表征,并用高效毛细管电泳测定了寡糖的聚合度。探讨了温度、过氧化氢浓度对降解所需时间、产品得率及甲壳低聚糖聚合度的影响。结果：选择降解温度 ８０℃～９０℃,过氧化氢浓度 ８％～１０％时,水解时间０．５ ～１．０ ｈ,水溶性产品得率为 ４０％～４５％,聚合度为３～７的寡糖占水解产物的３６％～５０％。结论：该方法制备甲壳低聚糖是可行的。如进一步研究工艺条件,有望进行工业化生产。     

高效液相色谱法测定生脉注射液中人参皂甙Rg1,Re的含量

用高效液相色谱法同时测定生脉注射液中人参皂甙ＲｇＩ和Ｒｅ含量。用十八烷基硅烷键合相柱，检测波长２０３ｎｍ，流动相乙腈－０．０５％磷酸溶液（１８：８２），人参皂甙ＲｇＩ回收率为９９．０１％，ＲＳＤ＝１．５８％，人参皂甙Ｒｅ回收率为９９．３０％，ＲＳＤ＝１．３０％，并对萃取方法进行了探讨。     

三七皂甙对慢性缺氧性肺动脉高压的影响

目的：研究三七皂甙对大鼠慢性缺氧性肺动脉高压的作用。方法：采用间断常压缺氧法制备大鼠慢性缺氧性肺动脉高压模型，腹腔注射三七皂甙（２５，５０和１００ｍｇ·ｋｇ－１·ｄ－１），连续给药２１天。结果：三七皂甙能产生剂量依赖性地抑制慢性缺氧性肺动脉高压的作用，其抑制率分别为１５．９％、４３．９％和７３．４％，并能明显抑制右心室肥厚，其抑制率分别为２２．１％、５５．６％和８３．３％，而对颈动脉血压无明显的影响。三七皂甙（２００ｇ·Ｌ－１）能明显抑制血小板生长因子所诱导的离体肺动脉平滑肌细胞ＤＮＡ的合成。结论：三七皂甙有抑制慢性缺氧性肺动脉高压的作用，可能是通过抑制血小板生长因子促肺动脉平滑肌细胞增殖而抑制肺血管结构重建来实现的。     

人参皂甙Rg1对老年人淋巴细胞蛋白质酪氨酸激酶活性的调控作用

选择７名健康老年人为对象，研究了人参皂甙Ｒｇ１对其淋巴细胞表面抗原。受体及蛋白质酪氨酸激酶（ＰＴＫ）活性的作用，用间接免疫荧光法测定了ＣＤ２５、ＣＤ４５ＲＡ及ＣＤ４５Ｒ阳性细胞百分率。单独ＰＨＡ（５μｇ／ｍｌ）培养７２小时分别为３８．３％±１７３％、４６．０％±１５．１％、５２６％±１４．４％；而用ＰＨＡ（５μｇ／ｍｌ）和Ｒｇ＿１（μｇ／ｍｌ）联合培养时则分别为５８．０％±１２．５％。６４．１％±１２．４％、７４．１％＋８．０％。两者相比分别皆有显著性（Ｐ＜０．０５），用ＥＬＩＳＡ法测定了经ＰＨＡ及ＰＨＡ＋Ｒｇ＿１培养３０分钟和７２小时细胞浆ＰＴＫ的吸光度值，ＰＨＡ组为０．１２０±０．０２０，ＰＨＡ±Ｒｇ＿１组为０．１３８±０．０１５，（Ｐ＜０００１）。结果证明，Ｒｇ＿１显著升高ＰＴＫ活性。据此得出几点结论，并讨论广Ｒｇ＿１对ＰＴＫ的作用机理。     

扇贝裙边中糖胺聚糖的气相色谱定性定量分析及红外光谱分析

目的 对栉孔扇贝和海湾扇贝裙边中提取分离的糖胺聚糖进行化学组成及结构研究。方法 样品经盐酸—甲醇试剂醇解成单糖．采用标准对照法及内标法进行气相色谱定性定量测定。样品经KBr压片，红外光谱扫描(4000～500cm^-1)。结果 测定出栉孔扇贝糖胺聚糖中单糖含量分别为鼠李糖0．75％，木糖0．63％，岩藻糖0．67％，甘露糖0．97％，葡萄糖1．11％，半乳糖1．59％。红外光谱测定结果显示，栉孔扇贝和海湾扇贝糖胺聚糖具有典型酸性黏多糖的吸收特征。结论 从栉孔扇贝裙边中提取分离的糖胺聚糖，分子中含有中性糖基。与标准品的红外光谱进行比较．两种扇贝糖胺聚糖均与透明质酸的红外光谱相似。     

罗氏海盘车皂苷类成分提取纯化工艺优化研究

目的优化罗氏海盘车中抗炎成分总皂苷的提取纯化工艺,为罗氏海盘车抗炎药效物质基础及作用机制研究奠定基础。方法采用正交试验设计法,以总皂苷含量和出膏率的综合评分为考察指标,优化罗氏海盘车总皂苷提取工艺参数;采用大孔吸附树脂法,以总皂苷含量为考察指标,通过静、动态吸附与解吸实验优化罗氏海盘车总皂苷纯化工艺参数;采用噻唑蓝(MTT)法比较纯化前后提取物对脂多糖(LPS)诱导RAW264.7细胞的抑制作用。结果罗氏海盘车最佳提取条件为10倍量80%乙醇,回流提取3次,每次1 h;最佳纯化条件为采用NKA-9型号树脂,以浓度为0.4 g生药/m L的药液,按0.5 g·m L~(-1)(生药量/树脂体积)比例上样,3 BV水除杂后,4 BV 90%乙醇洗脱,石油醚脱脂,水饱和正丁醇萃取,纯化后样品纯度为75.44%,收率为1.43%;二次纯化物抗炎IC_(50)值比粗提物IC_(50)值降低63%。结论按此优化工艺,可获得纯度较高的罗氏海盘车皂苷类成分。     

高效液相色谱法同时测定普罗帕酮,氢化奎尼丁的血药浓度

本文建立了用高效液相色谱法同时测定普罗帕酮、氢化奎尼丁血药浓度的方法。所用色谱柱为ＯＤＳ柱，流动相为改性甲醇，检测波长为２５４ｎｍ，流速１．２ｍｌ／ｍｉｎ，内标物采用盐酸异丙嗪，用氯仿作为提取剂，提取后分离有机层，于５０℃水浴以氮气流吹干，残渣用甲醇重溶，取１０μｌ进样。以样品峰面积对内标峰的峰面积比对样品浓度进行直线回归，计算直线回归方程，线性范围普罗帕酮为０．１～８．０ｍｇ／Ｌ，氢化奎尼丁０．５～６．０ｍｇ／Ｌ；普罗帕酮和氢化奎尼丁的最低检出限分别为：５ｎｇ和２．５ｎｇ，日内误差ＲＳＤ％分别为：４．３９％和３．８２％，日间误差ＲＳＤ％分别为：４．８３％和３．６３％。普罗帕酮、氢化奎尼丁和异丙嗪的绝对回收率分别为９８．３１％、９２．１７％和８７．１７％。本法方便、快速、灵敏、准确，特别适用于常规临床血药浓度监测。     

苦参碱及氧化苦参碱的药代动力学与药效动力学

以QTc延长率为效应指标,用药代动力学-药效动力学结合模型对苦参碱、氧化苦参碱iv后在免体内的处置和效应动力学作定量分析,两药的血浓时程均符合二房室模型,两药的效应与效应室浓度之间的关系均符合S形E_max模型。两药彼此的药动学和药效学性质均有明显差异,但它们各自的劳动学和药效学性质在所用剂量范围内均为非剂量依赖性。     

TOXIC AND CARCINOGENIC EFFECTS OF PARENTERAL AND PERCUTANEOUS ATP AND ITS IRON COMPLEX

ABSTRACT

The long term effects of percutaneous, subcutaneous and intraperitoneal administration of sodium–ATP (NaATP) and ferric iron–ATP (FeATP) were studied on an animal model. Both compounds induce a generalized lymphoadenitis which in the case of FeATP led to lymphomas. The analytical study of the involved target tissues showed intracellular composition changes that result from the impairment of the cell membrane permeability. The morbidity and mortality rate were higher with FeATP which seems to be the result of two different, in intensity and duration, interactions with the cell plasma membrane. The influence of the changes in cellular calcium homeostasis, and its relationship with carcinogenesis and immuno response are discussed.     

HPLC和~1HNMR分析确定cis－A－和cis－B－羟甲芬太尼的组成和构型

羟甲芬太尼（１）是一个强效的镇痛剂和高亲和、高选择性的阿片μ受体激动剂。通过ＨＰＬＣ和１ＨＮＭＲ分析，ｃｉｓ－Ａ－ｌ被确定为由等量的ｃｉｓ－（＋）－（３Ｒ，４Ｓ，２＇Ｓ）－ｌ和：ｃｉｓ－（—）－（３Ｓ，４Ｒ，２＇Ｒ）－１组成的外消旋体，ｃｉｓ－Ｂ－ｌ被确定为由等量的ｃｉｓ－（—）－（３Ｒ，４Ｓ，２＇Ｒ）－１和ｃｉｓ－（＋）－（３Ｓ，４Ｒ，２＇Ｓ）－１组成的外消旋体。     

冰毒吸食者焦虑抑郁情绪和自我概念的测评及相关分析

目的:了解冰毒吸食者焦虑抑郁情绪和自我概念状况,探讨二者之间的关系,为临床心理干预提供依据。方法:采用抑郁自评量表(SDS),焦虑自评量表(SAS)和田纳西自我概念量表(TSCS)对36例强制戒毒的冰毒吸食者(研究组)和36例健康人群(对照组)进行调查,将结果进行统计学处理分析。结果:(1)研究组SDS,SAS评分明显高于对照组,差别具有统计学意义(P<0.01);(2)TSCS评分比较,研究组除自我批评因子分高于对照组外,其余各因子分均低于对照组,差异具有统计学意义(P<0.01);(3)TSCS与SAS和SDS之间具有高度相关性(r=0.411-0.462,P<0.01)。结论:冰毒吸食者焦虑抑郁情绪明显,表现为消极的自我概念;焦虑抑郁情绪影响自我概念。临床治疗中应关注戒毒者负性情绪和自我概念,采取有效措施帮助他们消除负性情绪,树立积极的自我概念,促进心理康复。     

顶头孢霉229与12的分生孢子及原生质体的形成和再生

头孢菌素产生菌顶头孢霉菌株229的沉没培养或斜面培养都可形成分生孢子,并可用普通滤纸将它们与菌丝及节孢子分开,但是它们成活率极低.这种成活的分生孢子的数量与培养基成分有关.菌丝培养基成分对制备顶头孢霉原生质体有显著影响.用一种MM培养基培养的菌丝,不经巯基化合物预处理,酶解(1%纤维素酶)3小时后,可得到大量原生质体.原生质体的再生频率为1.8～4.6%.与分生孢子形成的菌落相比,原生质体再生菌落的产抗生素能力显示出较大的变异性.本文还讨论了山梨醇与Nikkomycin对菌丝生长形态及原生质体形成的影响.     

LIVER ALCOHOL AND ALDEHYDE DEHYDROGENASE: INHIBITION AND POTENTIATION BY HISTAMINE AGONISTS AND ANTAGONISTS

1. The in vitro effects of histamine, some other Hi- and H₂-receptor agonists and some antagonists were studied on the specific activities and kinetics of rat liver alcohol dehydrogenase (ADH), and cytoplasmic and mitochondrial liver aldehyde dehydrogenase (ALDH). 2. Histamine (H₁- and H₂-agonist) non-competitively inhibited ADH and ALDH, 2-(2-aminoethyl) pyridine (Hi-receptor agonist) non-competitively inhibited ADH. There were no changes of cytoplasmic and mitochondrial liver ALDH activities in the presence of 2-(2-aminoethyl) pyridine. 3. Betazole (H₂-receptor agonist) produced a competitive inhibition of mitochondrial ALDH but not of ADH or cytoplasmic ALDH. 4. Diphenhydramine (H₁-receptor antagonist) non-competitively inhibited ADH at a lower concentration. It stimulated mitochondrial ALDH activity without changes in cytoplasmic ALDH from control values. 5. Burimamide (H₂-receptor antagonist) produced a biphasic and dose-dependent stimulation and non-competitive inhibition of ADH and it non-competitively inhibited ALDH in both cytoplasmic and mitochondrial fractions. Metiamide (H₂-receptor antagonist) non-competitively inhibited all ADH and ALDH of both liver fraction studied. 6. It is concluded that liver ADH and ALDH activity can be altered by compounds which affect both Hi- and H₂-histamine receptors and that these compounds may cause an in vivo potentiation and/or reduction of the toxic effect of ethanol.     

TOXICOKINETICS AND EFFECTS OF FIBROUS AND NONFIBROUS PARTICLES

Chronic inhalation of fibrous and nonfibrous particles by rats at high concentrations results in lung tumor formation if the particles are poorly soluble in the lung. Even rather benign nonfibrous particles such as TiO 2 produce this result. One significant change during a chronic inhalation exposure of poorly soluble particles of low cytotoxicity (PSP) is an impairment of normal clearance mechanisms in the alveolar region of the lung in rats, resulting in a continued buildup to high lung burdens accompanied by chronic alveolar inflammation, fibrosis, and mutational events. Since these are obviously high-dose effects, questions about their extrapolation to humans exposed to much lower concentrations have been raised. Results of key studies reported for chronic inhalation of PSP in rats indicate that mechanisms of PSP-induced lung tumors at high doses do not operate at low dose levels. Furthermore, the existence of two thresholds can be postulated: One is a dosimetric threshold for the endpoint alveolar macrophage-mediated clearance, which is related to lung particle overload. The other is a mechanistic threshold for the endpoint mutation, which is determined by the level of antioxidant defenses to counter-balance reactive oxidant species released by activated inflammatory cells. A no-observed-adverse-effect level (NOAEL) could therefore be based on avoiding alteration of the toxicokinetic of the particles such that the lung burdens stay below the dosimetric threshold. The suggestion that PSP-associated organic compounds (e.g., diesel particulate matter) contribute to the lung tumor responses in rats observed in chronic inhalation studies is not supported by experimental data from in vivo studies. It can be concluded that high-dose rat lung tumors due to PSP should not be used for low-dose extrapolations, and no significant contribution to human lung cancer risk can be predicted from levels of PSP below lung overload. With respect to the pulmonary toxicokinetics of inhaled fibrous particles, the biopersistence of long fibers (>20 µm) which cannot be phagocytized by alveolar macrophages is a key parameter related to long-term carcinogenic effects. Long fibers with a very low biopersistence should not be considered as carcinogenic. Since the clearance kinetics of fibers can generally be described by a biphasic or multiphasic pattern - fast initial and slow final phase - it is essential that the slow phase of the retention kinetics of fibers longer than 20 µm is considered in a biopersistence assay. Based on the results of such assay, fibers can be classified into one of two categories: a biopersistent fiber that cannot be dissolved in the lung within an acceptable time period; or a biosoluble fiber when even long nonphagocytizable fibers will be disappearing rapidly from the lung. However, in addition to biopersistence, it should be mandatory to evaluate fiber toxicity in an appropriate assay relative to a fiber whose long-term effects are well known. Moreover, for organic fibers it is likely that different rules may have to be established for characterization of their toxic and carcinogenic potential.     

珍珠母贝中糖胺聚糖的提取分离纯化

目的:对马氏珍珠母贝中提取、分离得到的糖胺聚糖(glycosam inog lycans,GAG)进行化学组分研究。方法:样品经还原、水解和乙酰化,采用气相色谱-质谱法定性测定。结果:测定出马氏珍珠母贝中经提取、分离得到的GAG中的3种主要成分,其骨架结构分别与(硫酸乙酰)肝素、(硫酸)软骨素和透明质酸相符。结论:马氏珍珠母贝中提取分离的糖胺聚糖中含有肝素、软骨素和透明质酸。