依布硒啉对四氯化碳及内毒素+D-氨基半乳糖致肝损伤的保护作用

目的：考察依布硒啉(ebselen)对肝损伤的保护作用。方法：以0.2%四氯化碳(5 ml.kg^-1)和内毒素（1μg.kg^-1)+D-氨基半乳糖（800 mg.kg^-1)分别ip ICR小鼠形成肝损伤,观察病理改变及血清谷丙转氨酶(ALT)、总胆红素(TBIL)和总胆汁酸(TBA)活性。培养大鼠肝细胞以CCl₄和LPS＋D-GalN诱发损伤。测定了乳酸脱氢酶活性和细胞TBARS含量。结果：依伯硒啉可改善CCl₄和LPS＋D-GalN诱发的小鼠肝损伤变化,减小相关损伤指标的改变;并可拮抗培养肝细胞的LDH释放和TBARS含量上升。结论：依布硒啉能保护肝损伤,可能与抗自由基的脂质过氧化有关。     

6,7-二乙酰黄芩素对四氯化碳和D-氨基半乳糖所致的急性肝损伤的保护作用

目的:研究6,7-二乙酰黄芩素对四氯化碳(CCl4)和D-氨基半乳糖(D-GalN)所致急性肝损伤的保护作用。方法:分别用CCl4和D-GalN诱导化学性急性肝损伤模型,测定血清中丙氨酸氨基转移酶(ALT)、天冬氨酸氨基转移酶(AST)水平;并用苏木素-伊红(HE)染色处理肝脏组织切片,光镜观察病理学改变;用试剂盒测定肝线粒体中AST,SOD和GSH-PX的活性及脂质过氧化产物MDA含量。结果:在CCl4和D-GalN诱导和的小鼠肝急性损伤模型中,6,7-二乙酰黄芩素给药(50,100 mg.kg-1,ig)明显降低血清ALT,AST水平;明显改善肝脏病理组织状况;6,7-二乙酰黄芩素给药(25,50,100 mg.kg-1,ig)明显降低CCl4诱导的肝急性损伤小鼠的肝线粒体中AST活性和MDA的含量,显著增加SOD和GSH-PX的活性。结论:6,7-二乙酰黄芩对CCl4和D-GalN诱导和的小鼠肝急性损伤均具有保护作用,该作用与其增加线粒体中抗氧化酶的酶的活性、降低脂质过氧化水平有关。     

鹅不食草煎液对小鼠肝损伤的保护作用

目的:观察鹅不食草煎液对小鼠3种肝损伤模型的保护作用.方法:采用四氯化碳(CCl4)、对乙酰氨基酚(APAP)、D-氨基半乳糖 脂多糖(D-GalN LPS)致3种小鼠肝损伤模型,测定血清谷丙转氨酶(ALT).结果:鹅不食草煎液能明显降低CCl4,APAP,D-GalN LPS引起的肝损伤后小鼠血清中升高的ALT水平.结论:鹅不食草煎液对实验性肝损伤有明显的保护作用.     

南沙参多糖对小鼠CCl4急性肝损伤的保护作用

目的探讨南沙参多糖(RAPS)对肝损伤的保护作用.方法采用四氯化碳(CCl4)诱导小鼠急性肝损伤模型,测定血清丙氨酸氨基转移酶(ALT)、天冬氨酸氨基转移酶(AST)活性、肝匀浆中超氧化物歧化酶(SOD)活性及丙二醛(MDA)含量,观察肝组织病理学改变.结果RAPS各剂量组(2000,1000,500 mg·kg-1)不仅能显著降低肝损伤小鼠血清AST、ALT活性,而且能够降低肝损伤小鼠肝组织MDA含量,并能提高SOD活性;病理形态学观察显示,RAPS能够明显减轻肝细胞肿胀、减少中性粒细胞浸润,其对急性肝损伤具有治疗作用.结论RAPS对CCl4诱导的急性肝损伤具有显著的保护作用,该保护作用可能与其抗氧化作用有关.     

柚皮素对四氯化碳致小鼠化学性肝损伤中氧化应激介质生成影响的实验研究

目的 考察柚皮素(黄酮类化合物)对小鼠化学性肝损伤中氧化应激介质生成的影响.方法 用灌胃法,小鼠连续7天预给予柚皮素(25,50,100 mg·kg-1),第7日经腹腔单次注射四氯化碳(CCl4,1 mL·kg-1)诱发化学性肝损伤.24 h后用紫外分光光度法测定血清转氨酶(ALT、AST)水平,氧化应激介质丙二醛(MDA)含量,及肝微粒体超氧化物歧化酶(SOD)活性;用单细胞凝胶电泳法检测肝细胞中DNA氧化损伤水平.结果 与对照组相比,CCl4化学损伤组小鼠的血清ALT水平显著升高,氧化应激介质生成增多,肝细胞DNA氧化损伤断裂显著增多.柚皮素预处理组,CC4l急性肝损伤中血清转氨酶水平虽然未见明显变化,但柚皮素在其高剂量组(100 mg·kg-1)可使MDA水平有下降趋势,SOD活性有升高趋势且可显著性地降低CCl4损伤所致彗星拖尾细胞的百分率.结论 预先给予柚皮素(25,50,100mg·kg-1)可使CCl4所致急性肝损伤中氧化应激反应减轻,并可显著降低肝细胞核DNA单链断裂氧化损伤水平.     

肝心康胶囊对小鼠肝损伤的保护作用

目的 观察肝心康胶囊(GXK)对小鼠3种肝损伤模型的保护作用：方法采用四氯化碳(CCl4)、对乙酰氨基酚(APAP)、D-氨基半乳糖 脂多糖(D-GalN LPS)致小鼠肝损伤的3种模型，测定用药前后血清谷丙转氨酶(ALT)。结果GXK能明显降低CCl4,APAP,D-GalN LPS引起的肝损伤后小鼠血清中升高的ALT水平。结论GXK对实验性肝损伤有明显的保护作用。     

18-α异构体甘草酸对化学损伤人肝细胞的保护作用

目的:研究18-α异构体甘草酸(异甘草酸镁)对半乳糖胺(D-GalN)和四氯化碳(CCl4)损伤培养人肝细胞(L-02)的保护作用及机制.方法:培养L-02,用异甘草酸镁进行保护,再经D-GalN或CCl4处理.观察细胞上清活性氮终产物(NOx)含量及细胞线粒体膜电位.结果:浓度为1 mg/mL时,异甘草酸镁能显著减少D-GaLN和CCl4损伤细胞导致的NOx释放(P＜0.05),明显升高D-GaLN损伤所降低的细胞线粒体膜电位.结论:1 mg/mL的异甘草酸镁对D-GaLN和CCl4致人肝细胞损伤有明显保护作用,其机制与抑制细胞NOx释放,改善细胞线粒体膜电位作用相关.     

口服1,6-二磷酸果糖对动物肝损伤模型的保护作用

目的研究长期口服1,6-二磷酸果糖(FDP)对不同的肝损伤模型的影响,探索口服FDP作为慢性肝损伤保护药物的可能性。方法用CCl4所致的肝损伤模型来观察FDP对慢性肝损伤的作用;用D-半乳糖(GalN)和脂多糖(LPS)所致的小鼠肝损伤模型来评价FDP对急性肝损伤的作用。结果在CCl4所致的大鼠慢性肝损伤模型中,FDP (1 -4 g·kg-1·d-1ig)连续用药10周,可明显降低血清中病理性升高的ALT、AST、γ-GT、T-BIL和ALP的含量,同时升高病理性降低的TP、ALB和T-CHO的水平;并明显降低肝组织中羟脯氨酸的含量;FDP 4.0 g·kg-1·d-1可明显减少肝硬化发生率和减轻肝组织病理改变。在GalN所致的小鼠急性肝损伤模型中,FDP 1.0 -4.0 g·kg-1·d-1(ig 3 d)显著降低血清中ALT和AST的水平(P<0.01)和肝系数,4.0 g·kg-1·d-1可明显减轻肝细胞超微结构的病理性改变。在LPS所致的小鼠急性肝损伤模型中,FDP最大剂量(4.0 g·kg-1·d-1, ig 12 d)可明显降低血清中的ALT。结论本研究首次证明了长期口服FDP对CCl4所致的慢性肝损伤具有保护作用,同时证实了它对急性肝损伤的保护作用,提示口服FDP对不同原因引起的肝损伤有效,有可能作为口服肝保护药用于临床。     

白首乌C21甾体酯苷对小鼠急性四氯化碳肝损伤的保护作用

目的 研究白首乌C21甾体酯苷对四氯化碳(CCl4)所致小鼠急性肝损伤的保护作用.方法 以CCl4灌胃(ig.)小鼠制备急性肝损伤模型.测定血清中丙氨酸氨基转移酶(ALT)和天门冬氨酸氨基转移酶(AST)的活性、肝组织中超氧化物歧化酶(SOD)活力及丙二醛(MDA)含量,并做肝脏形态组织学观察.结果 白首乌C21甾体酯苷高、中、低剂量(40、20、10 mg·kg-1·d-1)均能明显抑制肝损伤小鼠血清中ALT和AST活性(P＜0.01)及肝组织中MDA含量的升高(P＜0.05),增强SOD活力(P＜0.05),减轻肝细胞的损伤程度.结论 白首乌C21甾体酯苷对CCl4引起的小鼠急性肝损伤具有保护作用,其机制可能与抗脂质过氧化有关.     

荞麦花叶芦丁对小鼠酒精性肝损伤的保护作用

目的探讨荞麦花叶芦丁(RBFL)对小鼠酒精性肝损伤的保护作用。方法 72只小鼠随机均分为6组:正常组(A)、模型对照组(B)、三个剂量RBFL组(R1组:75 mg.kg-1.d-1;R2组:150 mg.kg-1.d-1;R3组:300 mg.kg-1.d-1)和RBFL标准品对照组(D组:150 mg.kg-1.d-1)。用50%乙醇按10 ml.kg-1.d-1连续灌胃10 d,制备小鼠酒精性肝损伤模型。测定血清AST、ALT活力,计算肝重指数(LI),测定肝组织超氧化物歧化酶(SOD)活性和丙二醛(MDA)含量,镜下观察肝组织病理改变来判断RBFL对酒精性肝损伤小鼠的保护作用。结果 RBFL不同程度地降低了酒精性肝损伤小鼠的死亡率和体重下降率,抑制肝损伤小鼠的LI、AST和MDA,显著增强肝损伤小鼠肝组织SOD活性;病理组织学显示,RBFL能显著改善酒精损伤肝细胞的形态学变化。结论 RBFL对小鼠酒精性肝损伤有显著的保护作用,其机制可能与抑制脂质过氧化损伤有关。     

青霉烷砜和氨苄青霉素在小鼠和狗的药代动力学(英文)

青霉烷砜是一新的β-内酰胺酶抑制剂。本文报告青霉烷砜与氨苄青霉素在小鼠和狗的药代动学,两药血清药物浓度采用TLC法测定。在小鼠分别静脉注射青霉烷砜和氨苄青霉素,前者的药代动力学特征与后者相似,半衰期约为50min,两药均可在中央室和外周室间迅速平衡,并能广泛分布于细胞外液和组织。两药合并静脉注射给药,在两种动物上两药的药代动力学基本互不影响。     

SODIUM AND NORADRENALINE IN CEREBROSPINAL FLUID AND BLOOD IN SALT-SENSITIVE AND NON-SALT-SENSITIVE ESSENTIAL HYPERTENSION

1. The effects of dietary sodium on blood pressure and levels of sodium, other electrolytes and noradrenaline (NA) in the cerebrospinal fluid (CSF) and blood of 15 patients with essential hypertension were studied. The CSF and blood sampling was carried out after 7 days of a high salt intake (16-18 g/day) and after 7 days of a low salt intake (1-3 g/day). 2. Blood pressure and sodium concentrations in CSF and serum were significantly higher in the high salt period than the low salt period (CSF Na+ concentration: 147.7 +/- 0.4 mmol/L vs 145.3 +/- 0.5 mmol/L; P less than 0.001). Levels of CSF pressure and potassium or calcium concentrations were not different between the two periods. Plasma NA and plasma renin activity (PRA) were lower and CSF NA levels tended to be lower in the high salt period. 3. The levels and the changes in sodium and NA in CSF were not significantly different between the salt-sensitive (n = 8) and the non-salt-sensitive (n = 7) subjects, but the changes in plasma NA and PRA were smaller in the salt-sensitive subjects. 4. These results indicate that the sympathetic nervous system is less suppressed in salt-sensitive subjects during high salt intake. This may be due to altered neural responsiveness to sodium loading rather than being greater increases in sodium concentration in the central nervous system.     

RITANSERIN AND SEROTONERGIC MECHANISMS IN BLOOD PRESSURE AND FLUID REGULATION IN SHEEP

1. In previous studies, exogenous serotonin (5-HT), administered intravenously, caused dose-related increases in mean arterial pressure and heart rate in conscious sheep. The 5-HT2 antagonist ketanserin (0.1 mg/kg per h, i.v.) was shown to lower blood pressure in the conscious sheep primarily through antagonism of alpha-adrenoceptors. 2. A newer 5-HT2 antagonist, ritanserin, is a more selective antagonist in vivo, as it attenuated or abolished pressor responses to exogenous 5-HT, but not to phenylephrine. 3. When infused alone, ritanserin (0.1 mg/kg per h, i.v.) failed to produce a decrease in blood pressure, suggesting that 5-HT antagonistic properties are not sufficient by themselves to lower blood pressure. 4. Ritanserin displayed a different metabolic profile to ketanserin, with a markedly decreased water intake. The mechanism of this effect is unresolved, but may imply a permissive role for 5-HT in the modulation of drinking responses in the sheep. 5. Ritanserin did not modify ACTH-induced hypertension in sheep.     

RENIN AND PRORENIN IN REPRODUCTIVE TISSUES DURING GESTATION IN PIGS AND CATTLE

1. High concentrations of prorenin and active renin were previously found in ovarian follicular fluid from cattle but not from pigs. In the present study female reproductive tissues and fluids from cattle and pigs during gestation were investigated to clarify a possible species difference in active renin and prorenin concentrations. 2. Very high concentrations of active renin but no prorenin were found in corpus luteum from both species. 3. Relatively low concentrations of active renin, in the same order as in maternal blood plasma, were found in myometrium, endometrium, placenta and fetal membranes from both species. Prorenin was undetectable in these tissues except for bovine myometrium and porcine endometrium in some animals. 4. The concentrations of active renin and prorenin in amnionic fluid from both species were below the maternal plasma values. In allantoic fluid the concentrations were higher than in amnionic fluid. 5. The plasma concentrations of active renin and prorenin did not change during gestation in pigs. This finding is in contrast to the observations in humans and does not support a systemic effect of prorenin during gestation. 6. The presence of renin in the reproductive tissues, especially the very high concentrations in the corpus luteum, indicates a local function of the renin-angiotensin system during gestation.     

布洛芬缓释胶囊的研制及体内外评价

用糖衣锅包衣法制得的布洛芬（１）微囊，其释放速率与芬必得（２）相仿。８名健康受试者交叉口服６００ｍｇ１微囊及２胶囊，两者的药时曲线下面积（ＡＵＣ）、达峰时间（Ｔｍａｘ）、峰浓度（Ｃｍａｘ）均无显著差异（Ｐ＞０．０５）。     

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。     

IN VIVO ESTIMATION OF CHANGES IN DISTAL TUBULE FLOW AND THEIR ROLE IN DEXAMETHASONE-INDUCED KALIURESIS IN CONTROL AND POTASSIUM-ADAPTED RATS

The aim of this study was to determine whether the kaliuresis associated with glucocorticoids is due to a direct tubular action or is secondary to effects of glucocorticoids on distal tubule flow. A whole kidney technique was used to avoid the problem, inherent in microperfusion and micropuncture studies, of deciding whether (all) the appropriate nephron segment(s) are being studied. The method used was to determine the best whole kidney measure of distal tubule flow (the independent variable) by correlating this with the dependent variable (potassium excretion, corrected for differences in plasma potassium, UkV/PIK+) in conscious intact and adrenalectomized control and potassium-adapted rats. After an intragastric potassium chloride load, the correlation of UkV/PIK+ with UkV + UNaV was better than with either UNaV or UV, as measures of distal tubule flow. From the relationship a measure of potassium excretion independent of distal tubule flow can thus be calculated as UkV/PIK+ divided by (UkV + UNaV), defined as UK#. Measurement of UK# clearly demonstrates decreases in potassium excretion with adrenalectomy and increases in potassium excretion with aldosterone and in the potassium-adapted rat, consistent with described changes in potassium secretion. In contrast, with dexamethasone treatment, whilst there was an increase in UkV and UkV/PIK+, there was no change in UK# either in the control of potassium-adapted rats. These results suggest that the kaliuretic effect of dexamethasone cannot be attributed to direct tubular effects of glucocorticoids but rather can be explained by its effect on distal tubule flow.     

绞股蓝总皂苷对体内外血栓及凝血功能的影响

以静脉注射高分子右旋糖苷(higher molecular weight dextran,HMWD)造模,使实验动物的体内外血栓形成时间延长,凝血功能发生障碍.绞股蓝总皂苷(gypenosides,GPs)对以HMWD所致的血栓形成时间缩短具有较强的对抗作用,对HMWD引起的凝血时间及凝血酶原时间(PT)的缩短亦具有较强对抗作用,对白陶土部分凝血活酶时间(KPTT)缩短有一定的延长作用,但无统计学意义.     

粉防己碱在体内的代谢转化

粉防已碱有多种药理作用,近年我国又发现它可以防治矽肺。薄层层析及高压液相层析结果表明,粉防己碱进入大鼠及人体内,大部分以原形存在,少部分被转化,在大鼠的肝、肺、尿及人尿中,代谢产物可能有两个粉防己碱-N-2′-氧化物异构体和N-2′-去甲基粉防己碱。在两个粉防己碱-N-2′-氧化物中,其一前人已有报道,另一个为新化合物,根据核磁共振谱、质谱以及它能还原成粉防己碱,确定了其化学结构。本文给出了粉防己碱的气相层析及高压液相层析的实验条件。