植物杀螺剂麻风树籽杀螺筛选的报告

对麻风麻籽不同制剂杀灭钉螺筛选实验观察,发现２号粉剂和６号水剂具有良好的杀钉螺效果。２号浓度１０ｍｇ／Ｌ,６号６．２５ｍｇ／Ｌ,浸杀钉螺７２ｈ死亡率无为１００．０％。现场喷洒剂量６ｇ／ｍ＾２,５ｄ钉螺死亡率均为１００．０％,２号粉剂急性鱼类毒性试验结果ＬＣ５０为６９６．３１ｍｇ／Ｌ。该两种制剂进一步提纯和定型后,具有大批量生产和在疫区推广使用的价值。     

螺灭杀(Luomiecide)的灭螺效果及毒性观察

为证实螺灭杀（５０％氯硝柳胺乙醇胺盐可湿性粉剂）的灭螺效果，进行了室内和现场灭螺试验。室内０．２－０．５ｍｇ／Ｌ浸杀灭螺４８小时钉螺死亡率为９０％－１００％；现场喷洒３ｇ／ｍ２和３ｇ／ｍ２后３－７天，钉螺死亡率分别为、７３．３３－８９．７２％和８６．９－９３．７５％，同期内五氯酸钠１０ｇ／ｍ２对照组仅４０．７１－６２．６３％．与五氨酚钠比较该药具有较好杀螺作用，但对鱼类也有毒。     

B001对氯硝柳胺杀螺增效作用的研究

本文报道了Ｂ００１对钉螺的杀灭作用和对氯硝柳胺杀螺的增效作用，结果发现Ｂ００１有一定杀螺作用，６．２５ｍｇ／Ｌ的杀螺率为１００％，其ＬＤ５０为０．６１３０ｍｇ／Ｌ。与氯硝柳胺组成混合液，在０．４ｍｇ／Ｌ的Ｂ００１溶液中，氯硝柳胺的Ｄ５０由单独浸杀的０．０５９８ｍｇ／Ｌ降为０．０２３８ｍｇ／Ｌ，杀螺效果提高了２．５１倍。Ｂ００１与氯硝柳胺组成０．５：１、１：１、１．５：１、２：１的复方时，其共毒系数     

盾叶薯蓣杀湖北钉螺的量效与时效关系

实验研究表明，盾叶薯蓣制剂具有良好的杀螺效果，其１５ｍｇ／Ｌ剂量浸泡７２ｈ钉螺死亡率达１００％，杀螺剂量效应和时间效应关系可分别由Ｙ＝１．２２０２＋４．０６０４Ｘ和Ｙ＝３．００３＋０．０６３９Ｔ式表达，进而估算出相应ＬＤ９０为１７．６ｍｇ／Ｌ浸泡时间５１．３１ｈ以此指导现场合理施用该杀螺剂具有重要意义。     

盾叶薯蓣杀湖北钉螺的量效与时效关系

实验研究表明,盾叶薯蓣制剂具有良好的杀螺效果,其１５ｍｇ／Ｌ剂量浸泡７２ｈ钉螺死亡率达１００％,杀螺剂量效应和时间效应关系可分别由Ｙ＝１．２２０２＋４．０６０４Ｘ和Ｙ＝３．００３＋０．０６３９Ｔ式表达,进而估算出相应ＬＤ９０为１７．６ｍｇ／Ｌ,浸泡时间为５１．３１ｈ,以此指导现场合理施用该杀螺剂具有重要意义。     

不同样品的氯硝柳胺乙醇胺盐可湿性粉剂的杀螺效果与质量 …

对不同来源的２种国同和１种进口的氯硝柳胺乙醇胺盐可湿性粉剂，在２５℃下室内浸泡杀螺２４ｈ、４８ｈ及７２ｈ、１ｍｇ／Ｌ浓度的３种样品杀螺率均为１００％，样品中氯硝柳胺乙醇胺盐的含量以及悬浮率，均符合ＷＨＯ／ＳＭＦ／１－Ｒ３的规格要求。     

杀虫丁与氯硝柳胺灭螺效果的比较研究

目的 研究杀虫丁的灭螺旋效果及应用价值。方法 采用室内喷洒和浸杀方法及现场喷洒试验,对杀虫丁和氯硝柳腕灭螺效果进行了比较研究。结果 杀虫丁室内喷洒用量０．２５ｇ／ｍ＾２ ２４ｈ及室内浸杀用量０．２５ｍｇ／Ｌ４８ｈ的钉螺死亡率均为１００％。现场喷漂剂量１ｇ／ｍ＾２,旋药后１、３、５、７、１５ｄ钉螺均１００％死亡。结论 杀虫丁与氯硝柳胺同等剂量,同等条件,灭螺效果基本相当,但价格低５６％。     

氯硝柳胺及与五氯酚钠复配后钉螺上爬实验研究

本实验对氯硝柳胺乙醇胺盐５０％的可湿性粉剂浸泡灭螺时，出现钉螺离水上爬逃避药物作用的现象进行了研究。结果提示：药浓度小于１０ｍｇ／Ｌ，钉螺上爬较为明显，上爬率为５６１５％；药浓度达到１０ｍｇ／Ｌ及以上，钉螺上爬明显降低，上爬率为７０％。高浓度组（≥１０ｍｇ／Ｌ）钉螺上爬的最高高度为低浓度组（＜１０ｍｇ／Ｌ）的５４４％，上爬高度较低。氯硝柳胺与五氯酚钠复配后，钉螺的总上爬率为１９３３％，且上爬出混合药液面的钉螺死亡率比未复配的上爬钉螺死亡率高（Ｐ＜００１）。因此氯硝柳胺现场灭螺时，为防止钉螺上爬，提高灭螺效果，可采用药浓度１０ｍｇ／Ｌ以上，或与五氯酚钠复配使用     

钉螺经不同的浸泡后酶组织学变化的观察

目的 为研究槟榔碱（Ａｒｅｃｏｌｉｎｅ）灭螺增效的作用机制。方法 用加入和未加入增效剂的灭螺药物浸泡钉螺２４ｈ后,观察不同浓度的Ａｒｅ单用或杀螺剂合用对钉螺中枢神经节Ｍｇ＾２＋－ＡＴＰａｓｅ、ＣｈＥ、ＳＤＨ、ＬＤＨ的变化。结果 ６．２５同Ａｒｅ浸泡钉螺２４ｈ后,其中枢神经节Ｍｇ＾２＋－ＡＴＰａｓｅ被明显破坏,ＣｈＥ轻度破坏;１．５６ｍｇ／Ｌ Ａｒｅ与１．２５ｍｇ／Ｌ ＮａＰＣＰ、０．２５ｍｇ／Ｌ     

麻风树素浸杀钉螺卵效果观察

麻风树素植物杀螺剂室内浸杀螺卵结果表明，在≤１．２ｍｇ／Ｌ浓度下无杀螺卵作用，６ｍｇ／Ｌ、１２ｍｇ／Ｌ有效杀成螺浓度下，幼螺平均孵出率分别为６１％、４１％，与清水对照组有非常显著性差异，表明麻风树素高浓度对螺卵有一定毒杀作用。     

血水草生物碱对鱼类毒性实验的观察

目的 探讨植物杀螺药血水草生物碱(ECA)对鱼类的毒性作用。方法 采用常规的鱼类急性毒性实验方法，分别以氯硝柳胺和清水对照。结果 ①EcA对鲢鱼苗的急性毒性试验，在1．25mg／L及以下浓度中，96h的死亡率为0；在20．0mg／L中，2h死亡率为100％；2h的LC50为6．457mg／L，95％的可信区间为5．289-7．882mg／L。②对鲤鱼苗的急性毒性试验，在2．5mg／L及以下浓度中，96h的死亡率为0；在20．0mg／L中，2h死亡率为100％；2h的LC50为7．244mg／L，95％的可信区间为5．278—9．954mg／L。③对鲫鱼苗的急性毒性试验，在1．25mg／L及以下的浓度中，96h的死亡率为0；在20．0mg／L中，5h死亡率为100％；5h的LC50为7．080mg／L，95％的可信区间为5．202—9．635mg／L。结论 ECA对鲢鱼、鲤鱼、鲫鱼苗急性毒性作用低于氯硝柳胺，在有效杀螺浓度下对鱼毒性低。     

Efficacy and tolerability of vildagliptin monotherapy in drug-naïve patients with type 2 diabetes

This 24-week, double-blind, randomized, multicenter, placebo-controlled, parallel-group study performed in 354 drug-na?ve patients with type 2 diabetes (T2DM) assessed efficacy and tolerability of vildagliptin (50mg qd, 50mg bid, or 100mg qd). The primary assessment was change from baseline to endpoint in hemoglobin A1c (A1C), comparing vildagliptin to placebo by ANCOVA. Baseline A1C averaged 8.4% and the between-treatment difference (vildagliptin-placebo) in adjusted mean change (AMDelta) in A1C was -0.5+/-0.2% (P=0.011), -0.7+/-0.2% (P<0.001), and -0.9+/-0.2% (P<0.001) in patients receiving vildagliptin 50 mg qd, 50 mg bid, or 100 mg qd, respectively. Baseline FPG averaged 10.5 mmol/L; the between-treatment difference in AMDelta FPG was -0.6+/-0.4 mmol/L in patients receiving vildagliptin 50mg qd and -1.3+/-0.4 mmol/L (P=0.001) in both groups receiving 100mg daily. Relative to baseline, body weight did not change significantly in any of the three vildagliptin groups and decreased by 1.4+/-0.4 kg in the placebo group. Adverse events (AEs) occurred with similar frequency in each group: 55.8%, 59.3%, 59.3%, and 57.6% of patients receiving vildagliptin 50 mg qd, 50 mg bid, 100 mg qd, or placebo, respectively, experienced an AE. No confirmed hypoglycemia was reported. Conclusion: Vildagliptin is effective and well-tolerated in drug-na?ve patients with T2DM and 100 mg vildagliptin provides similar clinical benefit whether given as single or in divided doses.     

红霉素对豚鼠心电图及心室乳头肌细胞慢反应动作电位的影响

目的 研究红霉素对豚鼠心电图和心室乳头肌细胞慢反应动作电位的影响。方法 常规心电图记录法,观察红霉素（每100 g体重0. 5,1. 0,2. 0,4. 0,8. 0 mg）对豚鼠体表心电图PR间期、QRS波时限、QT间期、QTc、RR间期和HR的影响;应用细胞内微电极技术,记录并观察红霉素（0. 01,0. 03,0. 1,0. 3 mmol/ L）对心室乳头肌细胞慢反应动作电位静息电位（RP）、动作电位幅值（APA）、动作电位复极50%、90%的里程（APD50、APD90）、有效不应期（ERP）和0期最大除极速率（Vmax）的作用。结果 2. 0,4. 0和8. 0 mg三种剂量下,红霉素使PR间期分别延长7.0%、14. 2%和54. 1%,4. 0或8. 0 mg与0. 5 mg相比,药物对PR间期的影响有显著性差异; 0. 03 mmol/ L的红霉素使APD50和APD90分别延长9. 4%和7. 7%,0. 1 mmol/ L时,红霉素使APD50和APD90分别延长16. 3%和14. 4%,0. 3mmol/ L时,APD50和APD90分别延长21. 4%和18. 3%;0. 1和0. 3 mmol/ L时,Vmax分别下降7. 6%和12. 3%。 0. 1与0. 01 mmol/ L相比,红霉素对APD50和APD90两指标的影响有显著性差异,0. 3 mmol/ L与0. 01 mmol/ L相比,该药对APD50、 APD90和Vmax的影响都有显著性差异。结论 红霉素可抑制豚鼠心室乳头肌细胞L鄄型钙通道,减慢房室交界部位的兴奋传导,导致心电图PR间期延长。     

新型灭螺剂氯代水杨胺灭螺效果研究

 目的观察新型灭螺剂氯代水杨胺(LDS)的灭螺效果。方法采用浸杀法、喷洒法和撒粉法，将10% LDS和50%氯硝柳胺乙醇胺盐(WPN)在实验室分别配成0.05、0.1、0.2、0.4、0.8、1.6、3.2 mg/L (g/m2)7个浓度，在现场分别配成0.2、0.4、0.8 mg/L (g／m2)3个浓度，平行比较两种药物实验室24、48、72 h和现场1、3、7d的灭螺效果。两种药物均以0.4 mg/L (g/mz)浓度评价其灭螺效果。结果  在实验室温度23-25℃条件下，LDS和WPN的钉螺死亡率，浸杀72 h分别为100. 0%和96.7%；喷洒7 d分别为100.0%和96.0%；撤粉7d分别为92.0%和94.0%。在现场温度15-24℃条件下，LDS和WPN的钉螺死亡率，浸杀72 h丹别为100.0%和96.0%；喷洒7d分别为100.0%和96.9%；撒粉7d分别为100.0%和94.1%。结论新型灭螺剂氯代水杨胺的灭螺效果与氯硝柳胺乙醇胺盐基本相同，但灭螺费用降低。     

Pharmacokinetics of antimony in children treated for leishmaniasis with meglumine antimoniate

BACKGROUND: In some settings, the response to pentavalent antimonial therapy for leishmaniasis may be lower in children than in adults. We hypothesized that there are age-dependent pharmacokinetic differences of potential clinical relevance. METHODS: We compared the pharmacokinetics of antimony (Sb) in adults and 2 groups of children 3-6 years old who had cutaneous leishmaniasis treated with intramuscular meglumine antimoniate. Adults (n=9) and the first group of children (n=9) received 20 mg Sb/kg/day for 20 days; the second group of children (n=6) received 20 mg Sb/kg for 19 days and 30 mg Sb/kg on day 20. Drug exposure was assessed by the area under the 24-h time-concentration curve (AUC(0-24)) in plasma. RESULTS: Children (vs. adults) who received 20 mg/kg had a 42% lower AUC(0-24) (mean +/- SE, 111+/-7 vs. 190+/-10 mg x h/L, compared with adults; P<.001), a 16% lower peak concentration (32.7+/-0.9 vs. 38.8+/-2.1 mg/L; P=.04), and a 75% higher weight-adjusted clearance (0.185+/-0.013 vs. 0.106+/-0.006 L/h/kg; P<.001). The 30 mg/kg dose in children increased the AUC(0-24) to 164+/-10 mg x h/L and the peak concentration to 43.8+/-2.3 mg/L. CONCLUSIONS: Drug exposure is significantly lower in children than in adults treated with the same weight-adjusted regimen of meglumine antimoniate, which primarily stems from a higher antimony clearance rate.     

透明质酸对体外培养大骨节病软骨细胞增殖与凋亡的影响

目的 通过观察透明质酸(HA)对体外培养的大骨节病(Kashin-Beck disease,KBD)软骨细胞增殖、凋亡的影响,为临床上HA治疗KBD提供实验依据.方法 依据<大骨节病诊断标准>(GB 16003-1995)收集KBD患者和遭遇意外事故的病人(对照组)关节软骨,分离、体外培养关节软骨细胞.选用第2代细胞进行实验.两组软骨细胞分别给予不同剂量的HA,按HA剂量分为0、100、500 mg/L组.通过二苯甲唑溴盐(MTT)实验,测定第2、4、6天HA对KBD组、对照组软骨细胞增殖的影响.并通过流式细胞检测观察HA对软骨细胞凋亡的影响.结果 对照组在第4天时,500 mg/L组(0.140 ±0.049)促软骨细胞增殖作用大于0 mg/L组(0.116±0.021);KBD组在第6天时,500 mg/L组(0.179±0.081)与0 mg/L组(0.128 ±0.017)比较,显示了明显的促增殖作用(P<0.05).KBD组细胞凋亡率100、500 mg/L组(10.458±1.143、7.877±1.346)均较0 mg/L组(12.860±2.159)下降(P<0.05);对照组500 ms/L组(4.045±1.204)较0 mg/L组(7.128±1.244)细胞凋亡率下降(P<0.05).结论 HA对KBD软骨细胞具有促进增殖和抑制软骨细胞凋亡的作用,其中500 mg/L的HA改善KBD软骨细胞代谢的作用较100 mg/L明显.     

氯硝柳胺悬浮剂杀螺效果评价

目的 评价25％氯硝柳胺悬浮剂(SCN)的实验室和现场杀螺效果。方法 在实验室和现场采用浸杀法和喷洒法进行SCN和50％氯硝柳胺乙醇胺盐可湿性粉剂(WPN)两种剂型的杀螺试验。结果 实验室SCN 0.5mg/L(有效浓度0.125mg/L)和WPN 0.5mg/L(有效浓度0.25mg/L),浸杀24h,钉螺死亡率均为100％;有效浓度0.063mg/L浸杀24h,钉螺死亡率SCN为80.0％,WPN为66.7％。喷洒SCN 0.5g/m~2和WPN 1.0g/m~2,钉螺死亡率均为100％。现场浸杀SCN 0.5mg/L和WPN 1.0mg/L的钉螺死亡率均为100％。现场喷洒SCN 2.0g/m~2和WPN2.0g/m~2,SCN有效成份含量为WPN的1/2,3d和7d杀螺效果均高于WPN(x_(3d)~2=30.21,P<0.01;x_(7d)~2=7.62,P<0.01),差异均有非常显著性;15d杀螺效果相近(x_(15d)~2=0.02,P>0.05)。SCN1.0g/m~2与WPN 2.0g/m~2喷洒,SCN有效成份含量为WPN的1/4,杀螺效果相近(x_(3d)~2=0.90,P>0.05;x_(7d)~2=1.99,P>0.05;x_(15d)~2=0.03,P>0.05)。结论 现场SCN浸杀和喷洒有效药物剂量为WPN的1/4时,均能达到与WPN相同的杀螺效果,SCN是一种高效、使用方便、水溶性好的新型杀螺剂,值得在现场推广应用。     

Therapy of P388 leukemia with benzaldehyde

Optimal schedules of benzaldehyde (50-100 mg kg-1 intraperitoneally) on day 1 or on several days after inoculation of 10(5) P388 leukemia cells to DBA 2J mice increased survival by 70-100%. No significant prolongation of survival was observed between the various schedules of benzaldehyde treatment. Significantly longer survival was observed on day 30 after benzaldehyde treatment with 100 mg kg-1 on day 1 or 50 mg kg-1 on days 1-4 as compared to untreated controls, but no cure was achieved with any schedule and dose of benzaldehyde. No or minimal activity of benzaldehyde on L1210 and L5178Y leukemias, Ehrlich adenocarcinoma and Yoshida sarcoma was observed.     

Bilirubin diglucuronide transport by rat liver canalicular membrane vesicles: stimulation by bicarbonate ion

The purpose of this study was to provide further insight into the mechanism of bilirubin diglucuronide excretion through the hepatocyte canalicular membrane by investigating the uptake of (3H)bilirubin diglucuronide by purified canalicular membrane vesicles of rat liver. The uptake was analyzed by a rapid filtration technique. The difference between vesicle-associated (3H)bilirubin diglucuronide at 37 degrees C and at 0 degree C during the initial 1 min was regarded as uptake. Twenty second uptake was saturated by increasing the (3H)bilirubin diglucuronide concentration at a vesicle-inside-directed 100 mmol/L KCl gradient (Km = 75 mumol/L, Vmax = 320 pmol/mg protein.20 sec at 37 degrees C). No sodium dependency was observed. When canalicular membrane vesicles were preincubated with nonlabeled bilirubin diglucuronide, the uptake increased 1.3-fold (transstimulation). Vesicle-inside-positive potential induced by valinomycin and potassium caused a 1.4-fold increase in the uptake. When Cl- was replaced by equivalent ion concentrations of SO4(2-), HCO3-, NO3- and SCN-, the uptake was 78%, 244%, 68% and 50%, respectively, and specific stimulation by HCO3- was observed (Km = 75 mumol/L, Vmax = 700 pmol/mg protein.20 sec at a vesicle-inside-directed 100 mmol/L KHCO3 gradient at 37 degrees C). The uptake was inhibited in a dose-dependent manner by the addition of 4,4'-diisothiocyanatostilbene-2,2'-disulfonic acid. The uptake was ATP independent. From these results, it was concluded that bilirubin diglucuronide transport through the canalicular membrane is carrier mediated, electrogenic and stimulated by HCO3-.     

吸入一氧化氮对脂多糖所致大鼠急性肺损伤环氧合酶-2及TOLL样受体4表达的影响

目的 建立脂多糖致大鼠急性肺损伤的模型,观察一氧化氮对大鼠气道环氧合酶-2(cox-2)和Toll样受体4(TLR4)的分布及表达的影响.方法 健康雄性SD大鼠24只,按随机数字表法分为正常对照组、单用脂多糖(脂多糖组)、脂多糖加NO 20×10-6mg/L(低浓度NO组),脂多糖加NO 100×10-6mg/L(高浓度NO组).气管内滴注脂多糖(5 mg/kg)建立大鼠急性肺损伤模型.观察6 h后的肺水肿程度、免疫组织化学(SP染色)和实时荧光定量PCR检测肺组织中COX-2和TLR4的表达,以及分别吸入20×10-6、100×10-6mg/L浓度NO后的影响.所得数据采用单因素方差分析进行统计学分析,多个样本均数之间的两两比较采用LSD-t检验.结果 COX-2和TLR4在对照组大鼠气道内有广泛的分布和表达.脂多糖组大鼠肺水肿程度明显高于对照组,其主支气管和肺内细支气管上皮细胞内COX-2(6.5±2.8)及TLR4(44.9±11.3)表达高于对照组(分别为2.8 4±0.8、2.1±0.7),差异有统计学意义(t值分别为3.003、10.480,均P<0.01).低浓度NO组肺水肿程度明显减轻,其COX-2表达量(5.0±2.0)低于脂多糖组,但差异无统计学意义(t=1.227,P>0.05).而低浓度NO组TLR4(16.2±3.8)的表达量与脂多糖组(44.9±11.3)比较差异具有统计学意义(t=7.030,P<0.001).结论 COX-2和TLR4在大鼠气道内广泛分布,脂多糖刺激可使COX-2和TLR4的表达增强,吸入适当浓度NO可降低由脂多糖引起的COX-2和TLR4表达的增高.