Effect of artemether on glyceraldehyde-3-phosphate dehydrogenase,phosphogly-cerate kinase,and pyruvate kinase of Schistosoma japonicum harbored in mice

目的：研究蒿甲醚（Ａｒｔ）对日本血吸虫３磷酸甘油醛脱氢酶（ＧＡＰＤＨ）、磷酸甘油酸激酶（ＰＧＫ）和丙酮酸激酶（ＰＫ）的影响．方法：小鼠感染血吸虫尾蚴３２－３８ｄ后ｉｇＡｒｔ１００－３００ｍｇ·ｋｇ－１，２４－７２ｈ后取虫测定上述３种酶和乳酸含量．结果：小鼠ｉｇＡｒｔ３００ｍｇ·ｋｇ－１后２４－４８ｈ，血吸虫♀、♂虫的ＰＧＫ和ＰＫ活力被抑制２７％－４８％；♀虫的ＧＡＰＤＨ对Ａｒｔ亦较敏感，♂虫则否．给药后７２ｈ，♀虫乳酸含量降低７２％，♂虫的降低４９％．结论：Ａｒｔ对血吸虫的ＰＧＫ和ＰＫ活力有明显抑制作用，♀虫的ＧＡＰＤＨ对Ａｒｔ亦较敏感，♀虫乳酸含量降低较♂虫明显     

蒿甲醚对日本血吸虫葡萄糖摄取和糖元含量的影响

目的：研究蒿甲醚（Ａｒｔ）对血吸虫摄入葡萄糖和糖原含量的影响，方法；用Ａｒｔ－３００ｍｇ．ｋｇ＾－１ｉｇ治疗感染小鼠后２４－４８ｈ取虫，作体外培养，测定♀，♂虫糖原含量，对（Ｕ＾１４Ｃ）葡萄糖的摄入及（Ｕ－＾１４Ｃ）葡萄糖掺入虫糖原的量，结果：感染小鼠用Ａｒｔ治疗后２４－４８ｈ取虫人作体外培养１－２４ｈ，♂和♀虫的糖原含量分别减少２７％－６１％和３９％－７８％，６组♂虫中，仅３缚的葡萄糖摄入减少２     

Effect of artemether on glucose uptake and glycogen content in Schistosoma japonicum

研究蒿甲醚（Ａｒｔ）对血吸虫摄入葡萄糖和糖原含量的影响．方法：用Ａｒｔ３００ｍｇ·ｋｇ－１ｉｇ治疗感染小鼠后２４－４８ｈ取虫，作体外培养，测定♀、♂虫糖原含量，对［Ｕ１４Ｃ］葡萄糖的摄入及［Ｕ１４Ｃ］葡萄糖掺入虫糖原的量．结果：感染小鼠用Ａｒｔ治疗后２４－４８ｈ取虫作体外培养１－２４ｈ，♂和♀虫的糖原含量分别减少２７％－６１％和３９％－７８％；６组♂虫中，仅３组的葡萄糖摄入减少２３％－３５％，而♀虫各组的均明显减少，减少率为１８％－３８％．除２组♂虫外，［Ｕ１４Ｃ］葡萄糖掺入虫的糖原量无明显变化．结论：Ａｒｔ引起血吸虫糖原的减少，可能与干扰糖酵解而不是与葡萄糖的摄入有关．     

氯化血红素抗贫血疗效和毒性

目的：探讨氯化血红素（ｈｅｍｉｎ）治疗贫血的疗效及其口服的毒性反应，方法：用自制的ｈｅｍｉｎ按每日９３，１６８，３００ｍｇ．ｋｇ＾－１治疗失血性贫血大鼠，并与葡萄糖酸亚铁（ＦＧ３００ｍｇ．ｋｇ＾－１．ｄ＾－１）治疗组及单纯给水组比较，２４ｈ内对２０只小鼠予ｈｅｍｉｎ６ｇ．ｋｇ＾－１灌胃以观察小鼠的急性毒性反应，对８０只大鼠连续３个月分别予ｈｅｍｉｎ０．６５，１．３，２．６ｇ．ｋｇ＾－１．ｄ＾－１灌     

用蒿甲醚和吡喹酮早期治疗兔的血吸虫感染

兔于感染血吸虫尾蚴后ｄ７或２１分别开始ｉｇ１次蒿甲醚（Ａｒｔ）１０ｍｇ．ｋｇ＾－１和吡喹酮（Ｐｒａ）４０ｍｇ．ｋｇ＾－１，然后每隔１ｗｋｉｇ１次相同剂量的Ａｒｔ或Ｐｒａ连给３－４次，减♀虫率达９８％以上，且部分兔无♀虫，上述兔相仿，或仅有轻度变化，一些与急性血吸虫病有关的指标测定亦为阴性。     

甲苯达唑和吡喹酮对小鼠细粒棘球蚴囊壁的葡萄糖磷酸异构酶和甘油醛磷酸脱氢酶的影响(英文)

目的：测定抗包虫药物对细粒棘球蚴囊壁的葡萄糖磷酸异构酶（ＧＰＩ）和甘油醛磷酸脱氢酶（ＧＡＰＤＨ）的影响．方法：感染细粒棘球蚴囊达８－１０个月的小鼠ｉｇ甲苯达唑（Ｍｅｂ）或吡喹酮（Ｐｒａ）治疗，然后剖杀取囊，用生化方法测定ＧＰＩ和ＧＡＰＤＨ活力．结果：感染小鼠用Ｍｅｂ２５－５０ｍｇ·ｋｇ－１·ｄ－１治疗，连续７－１４ｄ，未见对ＧＡＰＤＨ活力有明显影响．若用Ｐｒａ５００ｍｇ·ｋｇ－１·ｄ－１ｉｇ１４ｄ，囊壁的ＧＡＰＤＨ活力被抑制２６５％．至于ＧＰＩ，仅Ｍｅｂ２５ｍｇ·ｋｇ－１·ｄ－１×１４ｄ组的瘪囊示该酶活力被抑制３３２％．结论：ＧＰＩ和ＧＡＰＤＨ不是有效的抗包虫药的主要作用靶．     

蒿甲中吡喹酮早期治疗感染血吸虫尾蚴兔和犬的肝脏显…

观察感染血吸虫尾蚴后早期用蒿甲醚或吡喹酮治疗，对宿主肝组织的影响。犬感染１９８－２０２条尾蚴后ｄ７ｉｇＡｒｔ１０ｍｇ．ｋｇ＾－１，Ａｒｔ胶囊（ＡｒｔＣ）１５ｍｇ．ｋｇ＾－１或感染后ｄ２１ｉｇＰｒａ３０－４０ｍｇ．ｋｇ＾－１，１－２ｗｋ重复约药１次，共２－４次；兔每隔日感染４８－５２条尾蚴，共５次，并于第１次感染后ｄ７或ｄ２１ｉｇ上述剂量的Ａｒｔ和Ｐｒａ，停药后４－５ｗｋ剖杀取肝作切片观察。犬与兔经     

N-乙酰半胱氨酸对硫代乙酰胺致大鼠肝衰竭的防治作用

目的：观察Ｎ－乙酰半胱氨酸（Ｎ－ａｃｅｔｙｌｃｙｓｔｅｉｎｅ,ＮＡＣ）对硫代乙酰胺（Ｔｈｉｏａｃｅｔａｍｉｄｅ,ＴＡＡ）引起大鼠暴发性肝衰竭（Ｆｕｌｍｉｎａｎｔ Ｈｅｐａｔｉｃ Ｆａｉｌｕｒｅ,ＦＨＦ）的预防治疗作用。方法：取ＳＤ♂大鼠分６组,除正常对照组外,均ｉｐ ＴＡＡ３００ｍｇ／ｋｇ,给药组同时ｉｐＮＡＣ２４ｈ后取血及肝脏,进行血清生化、血浆一氧化氮（Ｎｉｔｒｉｃ ｏｘｉｄｅ,ＮＯ）、肝脏还     

左旋千金藤立定对大鼠血清中催乳素水平的影响

目的：观察左旋千金藤立定（ＳＰＤ）对血清催乳素（ＰＲＬ）水平的影响，研究ＳＰＤ的药理作用，方法：成熟♀鼠ｉｐ多巴胺受体激动剂，拮抗剂或ＳＰＤ后断头取血，然后用放射免疫法测定血清中的催乳素水平。结果：ＳＰＤ引起血清ＰＲＬ水平迅速而显著的增增加，效应持续效约１ｈ，具有剂量依赖性，ＳＰＤ的半数有效剂量为３．７ｍｇ．ｋｇ＾－１（９５％可信限为２．６－４．３ｍｇ．ｋｇ＾－１）剂量为２０ｍｇ．ｋｇ＾－１时产生     

柳珊瑚酸及其衍生物对小鼠学习和记忆的影响

目的：研究柳珊瑚酸（Ｓｕｂ），Ｎ－柳珊瑚酰胺－Ｎ－Ｎ－二环己基脲（Ｓｕｂ－ＤＵ）Ｎ－环己基柳珊瑚酰胺（Ｎ－ＣＳ）在影响记忆与抗胆碱酯酶（ＡＣｈＥ）作用间的关系，方法：在被动回避操作装置上测定了小鼠ｉｐＳｕｂ或其衍生物后的跳台潜伏期（ＳＤＬ）和逃避潜伏期（ＥＬ），比色法测定ＡＣｈＥ活力。结果：Ｓｕｂ１．９，Ｓｕｂ－ＤＵ３．０和Ｐｈｙｓ０．１５ｍｇ．ｋｇ＾－１分别使成年小鼠的ＳＤＬ延长１９５％，２７１     

Effect of artemether on glucose uptake and glycogen content in Schistosoma japonicum.

AIM: To study the effect of artemether (Art) on glucose uptake and glycogen content in schistosomes. METHODS: Schistosomes recovered from mice treated intragastrically with Art 300 mg.kg-1 for 24-48 h, were incubated in the drug-free medium containing [U-14C]glucose 11.1 MBq.L-1. The glycogen content, [U-14C]glucose uptake, and incorporation of [U-14C]glucose into worm glycogen in both male and female worms were determined. RESULTS: When above-mentioned schistosomes were exposed to drug-free medium containing [U-14C]glucose for 1-24 h, the glycogen contents of male and female worms decreased 27%-61% and 39%-78%, respectively. Only 3 out of 6 male worm groups showed 23%-35% decrease in glucose uptake, while much less glucose uptake was found in female worms in all groups with reduction rates of 18%-38%. Apart from 2 male groups no apparent change in the incorporation of [U-14C]glucose into the worm glycogen was seen. CONCLUSIONS: Art-induced glycogen reduction in schistosomes was related to an inhibition of glycolysis rather than an interference with glucose uptake.     

蒿甲醚对小鼠体内日本血吸虫3—磷酸甘油醛脱氢酶,磷酸甘油酸激？…

AIM: To study the effect of artemether (Art) on glyceraldehyde-phosphate dehydrogenase (GAPDH), phosphoglycerate kinase (PGK), and pyruvate kinase (PK) of S japanicum. METHODS: Mice infected with schistosome cercariae for 32-38 d were treated ig with Art 100-300 mg.kg-1 and killed 24-72 h after medication for collection of schistosomes. The activities of GAPDH, PGK, and PK of the worms were determined by measuring the formation of NADH or consumption of NAD. The lactate content of the worms was also measured. RESULTS: After the infected mice were treated ig with Art 300 mg.kg-1 for 24 h, the inhibition rates of GAPDH were 13% (Male) and 21% (Female), and 48 h later the inhibition rates of the enzyme were 6% (Male) and 28% (Female). When Art 300 mg.kg-1 was given to infected mice for 24 h and 48 h, the inhibition rates of PGK were 60% (Male) and 48% (Female) as well as 75% (Male) and 62% (Female), respectively. Similar results were seen in PK activity. At 72 h after treatment the reduction rate of lactate content in Female worm was 72%, while that of Male was 48%. CONCLUSION: In the glycolytic pathway of both Male and Female schistosomes, PGK and PK activities were inhibited by Art. The GAPDH activity of Female worms was also susceptible to Art, While that of Male worms showed only temporary inhibition after treatment with Art. The Art reduced lactate content more in Female than in Male worms.     

嵩乙醚的抗血吸虫作用

实验感染日本血吸虫的小鼠,用蒿乙醚或蒿甲醚100～200mg·kg^-1·d^-1×2d灌胃治疗,显示两药对小鼠体内不同发育期血吸虫的减虫率相仿。特别是d7童虫和d35成虫组的减虫率较高,分别达77.5～87.2%和51.7～61.3%。经蒿乙醚作用后,d7童虫和d35成虫的糖原明显减少或消失,虫的皮层和实质组织中的碱性磷酸酶活力亦明显受抑制,表明蒿乙醚具有抗日本血吸虫童虫和成虫的作用。     

蒿甲醚预防兔感染日本血吸虫尾蚴

AIM: To study the effect of artemether (Art) for prevention of schistosomal infection. METHODS: Rabbits with single infection or reinfection with Schistosoma japonicum cercariae were treated intramuscularly (i.m.) or intragastrically (i.g.) with Art 5 -20 mg.kg-1 on d 7-15 after the first infection, followed by various regimens. RESULTS: When rabbits were injected i.m. Art 7.5 mg.kg-1 (i.e., one half of the effective dose given i.g. on d 7) followed by once every week for twice, the female worm reduction rate was only 42%. In infected rabbits treated i.g. with Art 10-20 mg.kg-1 given in the same administration schedule, the female worm reduction rates were > 91%. When Art 15 mg.kg-1 was given to rabbits on d 7-14 and the following dose of the drug was given at intervals of 7-14 d, the female worm reduction rates were > 94%. In rabbits reinfected with cercariae, the female reduction rate of Art given i.g. once a week for 3 times since d 8 after the first infection was 96% which was similar to that given once a week twice since d 14 after the first infection. CONCLUSION: Art should be given i.g. on d 7-15 after infection, followed by repeated dosing once every 7-15 d for a total of 3 doses. Art given i.g. daily for 2 consecutive days or given at 1-wk intervals since 7-15 d after infection also showed preventive effect.     

磷,砷,四氯化碳肝损伤线粒体和微粒体乳酸脱氢酶同工酶的改变

本文对P4,NaAsO_2,CCl_4亚慢性肝损伤大鼠肝细胞线粒体,微粒体LDH同工酶进行聚丙烯酰胺凝胶电泳,光密度扫描定量,对其标志酶组化染色,微机图象定量分析,结果表明,三组动物肝小叶线粒体标志酶SDH活性均有下降,其中以CCl_4组SDH下降较迟.NaAsO_2组染毒第8wk可见线粒体LDH_5升高,染毒12wk LDH_(2,3)下降,LDH_5升高与对照组比较无显著性差异,但仍高于P_4组,各组间微粒体LDH同工酶和其标志酶G-6-P酶活性变化存在差异;P_4组微粒体LDH同工酶改变明显且较其他两组早。     

Organ- and species-specific properties of glucose-6-phosphate dehydrogenase and the effect of molsidomine

Glucose-6-phosphate dehydrogenase (G-6-PDH) is the key enzyme of the pentose phosphate cycle and therefore regulates the synthesis of the nucleic acid constituent ribose-5-phosphate. At the same time the enzyme is coupled to the synthesis of reduced glutathione (GSH) which detoxifies electrophilic molecules (radicals) in the organism. Activity and stability of G-6-PDH and the influence of SIN 1--the active metabolite of molsidomine (Corvaton)--dithiothreitol (DTT) and NADP on these parameters were studied in enzyme preparations from different organs of the rat (liver, ethmoturbinates, blood) and from blood of mouse, guinea pig, rabbit, dog and man. The highest activity of G-6-PDH was measured in rat ethmoturbinates (69.26 +/- 5.91 mU/mg protein/min), the lowest in human blood (2.99 +/- 0.18 mU/mg protein/min). G-6-PDH of rat ethmoturbinates and of rat and dog blood was unstable and nearly completely inhibited by SIN 1. The enzyme of rat liver and of human, mouse, guinea pig and rabbit blood was stable and not influenced by SIN 1. These organ-and species-specific findings are discussed with respect to the toxicological actions of SIN 1.(ABSTRACT TRUNCATED AT 250 WORDS)     

不同地区日本血吸虫对吡喹酮的敏感性

小鼠感染浙江杭州、江苏无锡、安徽贵池、江西南昌、湖北汉阳、湖南岳阳和云南大理等7个地区日本血吸虫后32～35d,分别单次ig吡喹酮400mg/kg治疗。结果发现云南大理地区血吸虫感染组的疗效最差,而其他6个地区血吸虫感染组间的疗效无明显差别。认为云南大理地区血吸虫对吡喹酮的敏感性低于安徽等6个地区血吸虫。     

氯丙嗪和维拉帕米对大鼠镉肾毒性的影响(英文)

目的研究氯丙嗪(CPZ)和维拉帕米(Ver)对由镉引起的大鼠肾毒性是否有预防作用。方法32只大鼠随机分成4组,分别为对照组、单纯染镉组、CPZ和Ver预处理组。单纯染镉组大鼠sc7μmol·kg-1氯化镉;CPZ和Ver预处理组分别ipCPZ5mg·kg-1和Ver4mg·kg-1,1h后sc7μmol·kg-1氯化镉;对照组在相应时间内给予生理盐水,注射容量均为2mL·kg-1。最后一次注射24h后,收集24h尿样,测定尿乳酸脱氢酶(LDH)活性、尿蛋白、尿镉、肾镉和肾皮质中的Na+K+ATP酶,Ca2+ATP酶和蛋白激酶C(PKC)的活性。结果单纯染镉组与对照组比较,尿镉和肾镉含量明显升高。CPZ和Ver预处理组尿镉明显低于单纯染镉组,但肾镉无明显变化。与对照组比较,单纯染镉组尿LDH活性、尿蛋白和肾皮质中的Na+K+ATP酶,Ca2+ATP酶和PKC活性明显升高。CPZ和Ver预处理组大鼠尿LDH活性、尿蛋白和肾皮质中的Na+K+ATP酶,Ca2+ATP酶和PKC活性明显低于单纯染镉组。结论镉能激活Na+K+ATP酶,Ca2+ATP酶和PKC的活性,而且,CPZ和Ver均可不同程度地减轻肾毒性。     

匹诺塞林对急性局灶性脑缺血大鼠脑线粒体功能的影响

目的考察匹诺塞林对大鼠急性局灶性脑缺血组织能量代谢及线粒体功能的影响。方法制备永久性大鼠大脑中动脉栓塞(pMCAO)模型,大鼠随机分为假手术组、模型组、匹诺塞林给药组(1、3、10 mg.kg-1)、尼莫地平给药组(3mg.kg-1)。给药组于手术后10 min、12 h分别给予静脉注射,假手术组与模型组给予生理盐水。于手术24 h应用生化方法检测脑组织中LDH的活性,HPLC法检测大鼠脑组织ATP、ADP、AMP、磷酸肌酸含量。通过检测线粒体超氧化物歧化酶(Mn-SOD)、线粒体Ca2+-ATP酶活性,超氧阴离子含量、线粒体膜肿胀度、线粒体钙离子含量综合评价线粒体功能。结果匹诺塞林(3、10 mg.kg-1)给药组大鼠缺血脑组织中乳酸脱氢酶活性降低,能量指数比模型组分别提高了34.6%和45.8%(P<0.05);匹诺塞林(10 mg.kg-1)组线粒体SOD活性提高了24.4%、Na+,K+-ATP酶、Ca2+-ATP酶活性分别升高了24.9%及34.0%,线粒体钙离子浓度降低了22.0%,与模型组相比差异均具有显著性(P<0.05)。匹诺塞林(3、10 mg.kg-1)组线粒体超氧阴离子水平分别降低了20.2%及30.6%、线粒体肿胀程度分别降低了26.1%及46.0%,与模型组相比差异均具有显著性(P<0.05)。结论匹诺塞林可减轻大鼠脑缺血后能量损伤,提高脑组织抗缺血缺氧能力,其对线粒体功能的保护作用可能是改善缺血脑组织能量代谢的重要机制。     

Glucose-6-phosphate dehydrogenase and gama-glutamyltranspeptidase activities in the liver during chemically induced hepatocarcinogenesis in rats and mice

Glucose-6-phosphate dehydrogenase (G-6-PDH) and γ-glutamyltranspeptidase (γ-GTP) were studied in the liver of rats and mice receiving a diet which contained 3′-methyl-4-(dimethylamino)azobenzene (3′-Me-DAB), diethylnitrosamine (DEN), or o-aminoazotoluene (o-AT). Elevated G-6-PDH activity was first observed within 2 weeks after the start of 3′-Me-DAB feeding, reaching a maximum at 4 weeks. There was a decrease from the 4-week level at about 6 weeks, followed by a sustained increase. The maintained activity after 8 weeks was about 6 times higher than in control rat liver. γ-GTP activity in rat liver increased immediately after the start of 3′-Me-DAB feeding; it was about 12 times the control value after 3–4 weeks. At 5–6 weeks, the activity decreased somewhat from the 3 to 4-week level, but this was followed by a further sustained increase. In rats receiving the DEN-containing water, the liver G-6-PDH and γ-GTP activities changed in the same way as in the 3′-Me-DAB-fed rats. Both activities increased in the early stage, reaching a maximum by 6 weeks, subsided at 7 weeks, and rose again from 9 weeks. In mice receiving o-AT-containing diet, hepatic G-6-PDH activity also changed in a biphasic pattern and closely related with that of liver γ-GTP activity.