无毒棉籽液抗腹泻作用研究

通过对正常小鼠、生大黄致泻小鼠及脾虚小鼠的作用研究表明，无毒棉籽液有较好的抑制排便频度、治疗腹泻的作用．无毒棉籽液６ｇ／ｋｇ可极其显著地抑制正常小鼠的排便频度，无毒棉籽液６ｇ／ｋｇ和３ｇ／ｋｇ可极其显著地抑制生大黄致泻小鼠及脾虚小鼠的排便频度．６ｇ／ｋｇ无毒棉籽液且可极其显著地抑制正常小鼠及脾虚小鼠的小肠推进运动．     

扶脾止泻散止泻作用的实验研究

目的:通过药效学试验验证扶脾止泻散的功能与主治,为临床用药提供科学依据。方法:利用小鼠致泻作用实验法及小鼠小肠推进运动实验法观察药物对实验动物的影响。结果:扶脾止泻散能明显减少番泻叶致小鼠腹泻次数,能明显降低小鼠的小肠推进运动。结论:扶脾止泻散具有明显的止泻作用。     

四神丸治疗腹泻的实验研究

目的：通过观察腹泻小鼠胃肠运动和腹泻大鼠结肠中胃肠肽蛋白表达的变化,探讨四神丸对腹泻的影响。方法采用大黄泻下法复制模型,以稀便级、腹泻率、稀便率、腹泻指数、碳末推进法观测小肠碳末推进率代表胃肠运动情况,将造模成功实验大鼠分为空白对照组、模型对照组、西药对照组、四神丸组,给药后对大鼠结肠通过免疫组织化学方法检测5-羟色胺（5-HT）、P物质（SP）蛋白表达的情况,观察四神丸对其干预作用。结果经大黄泻下法复制模型后,生大黄使小鼠的胃肠运动加快,大鼠结肠中5-HT和SP蛋白表达明显升高。四神丸可以减慢腹泻小鼠胃肠运动,降低腹泻大鼠结肠中5-HT和SP蛋白表达。结论四神丸有止泻作用,可明显抑制胃肠运动,可能是通过干预5-HT、SP蛋白表达而起作用。     

米汤止泻作用及其机制

目的探讨粳米、籼米、小米米汤的止泻作用及其止泻机制。方法制备番泻叶致小鼠急性腹泻模型和新斯的明致小鼠小肠运动亢进模型,分别评价粳米、籼米、小米米汤对小鼠腹泻次数、小肠推进率的影响,考察不同浓度粳米米汤的止泻作用。结果与模型对照组比较,3种米汤均能不同程度对抗番泻叶致小鼠腹泻(P<0.05或P<0.01),粳米、籼米和小米对新斯的明小鼠小肠推进率分别为(61.7±15.6)%,(72.8±13.9)%,(71.3±21.2)%;大、中、小剂量粳米汤对新斯的明小鼠小肠推进率分别为(58.8±11.4)%,(63.1±12.9)%,(72.3±5.8)%,对正常小鼠小肠推进率分别为(68.2±6.1)%,(65.7±7.2)%,(64.4±6.8)%。结论 3种米汤都有不同程度的止泻作用,尤以粳米米汤作用显著,其止泻作用可能是通过抗胆碱作用产生。     

乌梅肉提取物抗腹泻作用研究

目的 研究乌梅提取物抗腹泻作用,为临床应用提供依据。方法 通过蓖麻油致小鼠腹泻模型、小肠炭墨推进实验、大鼠肠腔积液实验,以腹泻抑制率、小肠推进率、肠腔积液体积为指标,研究乌梅提取物的抗腹泻作用。结果 乌梅水提物及水提醇沉提取物均具有抗腹泻作用,其中水提醇沉提取物的活性明显高于水提物(P<0.05),显著抑制正常小鼠的小肠推进运动(P<0.05或0.01),但对肠腔积液作用不显著。结论 乌梅提取物具有一定的抗腹泻作用,其抗腹泻机制可能与抑制小肠运动有关。     

甘遂和醋甘遂醇提物及其不同极性部位的药效和毒性研究

目的考察甘遂和醋甘遂乙醇提取物及其不同极性部位的泻下作用和毒性。方法采用炭末推进法进行肠推进试验，观察甘遂和醋甘遂醇提物及其石油醚部位、乙酸乙酯部位、正丁醇部位和水部位对小鼠小肠推进和肠水分吸收的影响；急性毒性试验采用改良寇氏法测定其半数致死量（LD50）：结果与对照组相比，甘遂、醋甘遂醇提物、石油醚部位、乙酸乙酯部位可明显促进小肠推进运动。但与生品比较，醋制后各组墨汁推进率皆有所降低，泻下作用有所缓和；甘遂醋制后醇提物毒性下降4倍左右，石油醚部位毒性下降1倍左右，乙酸乙酯部位毒性下降4倍左右，而正丁醇部位和水部位无毒。结论甘遂醋制后泻下作用减弱，毒性显著降低：甘遂的石油醚部位和乙酸乙酯部位既是其药效学部位，又是其毒性部位。     

左金丸对胃肠道的调节作用

目的 研究左金丸在胃肠道调节方面的作用。方法 通过ig给予0.1%甲基橙溶液,计算其胃残留率,观察左金丸对小鼠胃排空的影响;通过ig 5%的炭末,计算炭末推进率,观察左金丸对正常小鼠小肠运动的影响、对新斯的明致小肠运动亢进的拮抗作用;观察左金丸对组胺致豚鼠离体回肠收缩的影响;ig给予大鼠D-木糖溶液,1 h后测定血清木糖值,观察左金丸对大鼠小肠吸收的影响;ig给予小鼠蓖麻油,观察左金丸的止泻作用。以戊己丸（加味左金）和黄连有效成份小檗碱作参比。结果 左金丸对胃肠道有明显的调节作用,延长小鼠的胃排空时间,抑制胃排空;对正常小鼠小肠运动的无明显影响,但能明显拮抗新斯的明所致的小鼠小肠运动亢进;明显抑制组胺引起的豚鼠离体回肠收缩;明显抑制大鼠的小肠吸收功能;明显抑制蓖麻油造成的小鼠腹泻。结论 古方左金丸对胃肠道有明显的调节作用,组方科学、合理。     

新疆沙枣提取物抗腹泻的初步药效学研究

目的:评价新疆沙枣提取物抗腹泻作用.方法:采用小鼠番泻叶致泻和毛果芸香碱致小鼠小肠运动亢进2种模型,观察沙枣的抗腹泻作用.小鼠随机分为4组:沙枣水提取物组、沙枣醇提取物组、阳性药思密达组、模型组.各组预防性给药,连续灌胃给予番泻叶或毛果芸香碱,观察各组小鼠的排便和炭粒推进情况.在离体豚鼠回肠上研究沙枣2种提取物对抗毛果芸香碱和磷酸组胺引起的收缩作用.结果:在番泻叶致泻中,沙枣提取物可使小鼠湿粪数明显减少,尤以醇提物明显;对毛果芸香碱致小鼠肠管炭粒推进有抑制作用.体外试验沙枣提取物对毛果芸香碱致肠管收缩有明显抑制作用,对磷酸组胺无抑制作用.结论:沙枣提取物有一定的止泻作用.     

小儿便通颗粒泻下通便作用的实验研究

目的研究小儿便通颗粒的泻下通便作用。方法选择正常小鼠小肠推进试验,阿托品所致小鼠小肠抑制试验,小鼠胃排空肠推进模型及正常小鼠排便试验,自身粪便所致便秘模型,失水性便秘模型,对小儿便通颗粒的药理作用进行评价。结果小儿便通颗粒可以促进正常小鼠小肠蠕动;对抗小鼠因阿托品所致小鼠小肠抑制状态;增加食物在胃中的排空作用和肠道中的推进率;缩短正常小鼠的排便时间,增加排便量和粒数,水分吸引减少;对因食自身粪便和失水造成的便秘模型具有一定的治疗作用。结论小儿便通颗粒具有一定的泻下通便作用,为该药治疗小儿便秘提供了实验依据。     

葛根止泻作用实验研究

目的:研究中药葛根抗腹泻作用,为临床应用提供实验基础.方法:用胃排空及小肠推进运动实验结合小鼠腹泻止泻作用实验共同研究葛根抗腹泻作用.结果:在胃排空及小肠推进运动实验中葛根高、中剂量组与阴性对照组比较均有统计学意义(P<0.01);在小鼠腹泻止泻作用实验中葛根各剂量组与阴性对照组比较均有统计学意义(P<0.01).结论:实验证实葛根具有良好的抗腹泻作用.     

老鹳草鞣质类化合物的抗腹泻作用研究

对老鹳草总鞣质(HGT)的抗腹泻作用研究表明：HGT有较好的治疗腹泻作用，可减少番泻叶或蓖麻油所引起腹泻次数；并可显著抑制正常及推进功能亢进小鼠的墨水胃肠推进率。结果提示抑制胃肠推进运动是HGT止泻机理之一。     

An analysis of the respiratory stimulant effect of physostigmine and neostigmine in the conscious rabbit

1. The effects of physostigmine and neostigmine, given by continuous intravenous infusion, were studied on respiration in conscious rabbits. 2. Physostigmine (5 mg/kg per min) significantly increased respiration rate, decreased arterial PaCO2 from 25.4 +/- 0.9 to 19.8 +/- 1.5 mmHg, increased PaO2 from 100.3 +/- 1.9 to 108 +/- 3.0 and pH from 7.42 +/- 0.01 to 7.46 +/- 0.01 within 30 min of its infusion. 3. Neostigmine (2.5 mg/kg per min) also decreased PaCO2 and increased PaO2 significantly, but caused a concomitant lactic acidosis, which was associated with the increased muscular activity and fasciculations. 4. The respiratory stimulant effect of neostigmine, but not that of physostigmine, was abolished by hexamethonium 2 X (1.5 mg/kg). Atropine methyl nitrate (1 mg/kg) failed to influence the respiratory stimulant effect of physostigmine, but hyoscine (10 mg/kg) blocked it completely. 5. It is suggested that augmentation of respiratory activity by neostigmine is mediated via peripheral nicotinic receptors in the carotid and aortic bodies. This may occur either through the accumulation of acetylcholine or H+ ions from raised blood lactic acid. 6. It is further suggested that physostigmine stimulates respiration by raising the concentration of acetylcholine in the central nervous system which, in turn, activates muscarinic receptors.     

Pharmacodynamic effects of nicotine and acetylcholine biosynthesis in mouse brain

Nicotine (4; 8 mg/kg) given intraperitoneally to mice had a marked hypothermic effect with a duration of more than 2 hours. Mecamylamine (0.5; 2.5 mg/kg) prevented the hypothermic effect of 2 mg/kg nicotine but had no effect on 4 mg/kg nicotine. Atropine (5 mg/kg) did not affect the hypothermia produced by nicotine. Other symptoms induced by nicotine (0.5-4 mg/kg) were convulsions, rigidity, tremor and decrease in motor activity. Pretreatment with mecamylamine (0.5 mg/kg) prevented convulsions but had only a slight effect on the decreased motor activity. Atropine pretreatment was ineffective. It thus seems as if the effects of nicotine at least to some part are mediated by nicotine-like receptors. When a tracer dose of labelled choline (3H-Ch) was given to mice treated with nicotine (4 mg/kg) a marked increase (+100%) in the biosynthesis of labelled acetylcholine (ACh) in the striatum was found when the animals were killed by decapitation. If the mice were killed by a more rapid technique, microwave irradiation of the head, no change in 3H-ACh formation was observed in comparison to controls. The findings indicate that nicotine can preserve a very labile pool of newly synthesized ACh in the striatum.     

肠泻停胶囊止泻作用研究

目的 观察肠泻停胶囊的止泻作用。方法 采用新斯的明负荷肠推进亢进以及番泻叶、蓖麻油诱导的腹泻模型，通过测定肠推进百分率、腹泻潜伏期以及腹泻次数等指标来评价肠泻停胶囊的止泻作用，通过离体豚鼠回肠试验，观察其可能的作用机制。结果 肠泻停胶囊明显降低正常小鼠以及新斯的明负荷小鼠的小肠推进百分率；对口服番泻叶浸荆或蓖麻油所致的腹泻模型小鼠均有明显的保护作用；对豚鼠离体回肠的收缩幅度和张力有明显的抑制作用。结论 肠泻停胶囊具有明显的止泻作用。     

华山参对中枢神经系统的药理作用

作者研究了华山参(Physochlaina infundibularis Kuang)对中枢神经系统的药理作用.华山参煎剂腹腔注射对小白鼠的LD₅₀为43(28.7-64.5)克/公斤;腹腔注射1克/公斤使大白鼠防御运动性条件反射潜伏期延长,部分动物条件反射破坏及分化抑制有解除现象;灌胃给药(2克/公斤)仅使条件反射潜伏期延长.腹腔注射1-4克/公斤显著降低大、小白鼠和家兔的自由活动,维持3-6小时,但不降低小白鼠的被动活动.腹腔注射4克/公斤,能协同硫喷妥钠及水合氯醛对小白鼠的催眠、麻醉作用;降低苯丙胺、咖啡因对小白鼠的兴奋活动,但在10克/公斤时对本丙胺的毒性作用及士的宁,戊四唑性惊厥无影响.给狗灌胃2-5克/公斤,有明显的镇静作用,但不能对抗去水吗啡的催吐效果.     

Effect of the anticarcinogenic drug 6-mercaptopurine on mineral metabolism in the mouse

The effect of 6-mercaptopurine (6-MP) on mineral metabolism was investigated in mice. C57BL mice were given 6-MP for 5 consecutive days. Treatments were: no injection; saline; vehicle injection (carboxymethylcellulose (CMC]; 5 mg/kg 6-MP; 25 mg/kg 6-MP; 50 mg/kg 6-MP; 100 mg/kg 6-MP; and 150 mg/kg 6-MP. After the 5-day period, tissues were removed and the levels of calcium (Ca), magnesium (Mg), zinc (Zn), copper (Cn) and manganese (Mn) were measured. In liver, but not in intestine or kidney, zinc and calcium levels increased in a dose-dependent manner. The weight of the stomach relative to body weight was significantly greater in mice receiving 100 mg/kg and 150 mg/kg BW doses of 6-MP than in those given lower doses, despite significantly lower body weight. This result indicated that 6-MP produced gastric toxicity. Injection of saline or vehicle had no effect on any of the parameters measured. The effect of 6-MP on mineral changes and on stomach-emptying may be partly responsible for at least some of its negative side-effects.     

Peripheral control of inflammatory but not neuropathic pain by endogenous cholinergic system

This study investigated the role of the cholinergic system in the modulation of inflammatory and neuropathic pain. The paw pressure test was used with inflammatory pain induced by intraplantar injection of carrageenan and neuropathic pain induced by sciatic nerve constriction. All drugs were locally administered into the right hindpaw of rats. Neostigmine, an acetylcholinesterase inhibitor (2, 4, 8 or 16 μg), inhibited the inflammatory pain induced by carrageenan (250 μg/paw), but not the hyperalgesia induced by prostaglandin E? (2 μg/paw). Neostigmine (8 μg) increased the nociceptive threshold only in the treated paw, suggesting only a local effect. The muscarinic antagonist atropine (150, 300 and 600 μg) caused a reduction in the nociceptive threshold induced by carrageenan (125 μg/paw), but not by prostaglandin E? (1 μg/paw). Atropine significantly decreased the nociceptive threshold only in the treated paw. On the other hand, in the presence of neuropathic pain, atropine (300 μg) did not alter the nociceptive threshold induced by constriction of the sciatic nerve. This study suggests that a peripheral endogenous cholinergic system involving muscarinic receptors may be activated during inflammation as a modulatory negative feedback control of inflammatory pain.     

防治血吸虫病药物的研究 ⅩⅩⅧ.敌百虫的毒性及其对日本血吸虫病的实验治疗

敌百虫是有机磷杀虫剂,又是胆碱酯酶抑制剂。本文試驗动物內用敌百虫的毒性和对日本血吸虫病的疗效,以及阿託品和PAM对敌百虫毒性与疗效的影响。小白鼠灌胃和皮下注射敌百虫1次的LD₅₀分別为0.8和0.6克/公斤。小白鼠在服敌百虫前30分钟注射阿託品和PAM的解毒效能比单用阿託品或单用PAM为佳。家兔每天灌胃30或60毫克/公斤共2周,抑制血浆胆碱酯酶活力70%左右。猴子灌胃剂量从4毫克/公斤开始,逐日递增4毫克/公斤,至第6天不食,胆碱酯酶活力也明显受到抑制,第7天躺臥不动,停药5天后恢复。小白鼠每天灌胃敌百虫200毫克/公斤,經2周后平均每鼠余存虫13±5条,和对照组24±6条相差非常显著.兔每天灌胃30毫克/公斤或皮下注射40毫克/公斤历2周后虫数也有减少.狗口服敌百虫2周后粪便转为阴性.然后停药2周解剖,平均每狗余存虫8±9条,比对照组6狗平均47±29条显著减少。在病狗治程中,血清磺溴酞钠存留率与血象无明显改变,血浆胆碱酯酶活力降为原来水平的25%左右.停药2周后恢复至原来水平的75%左右。敌百虫与吐酒石合并使用比单独应用一药治疗的效果要更好。阿品及PAM并不减弱敌百虫的疗效。敌百虫对动物的日本血吸虫病确有疗效,价格低廉,且可口服,为找寻有效的非锑剂开辟了新的途径。     

Pharmacological studies on timiperone, a new neuroleptic drug Part II: General pharmacological properties

General pharmacological properties of 4'-fluoro-4-[4-(2-thioxo-1-benzimidazolinyl) piperidino] butyrophenone (timiperone), a new neuroleptic drug, were compared with those of haloperidol. 1. Central nervous system: In behavioral observation, timiperone showed a typical neuroleptic profile at doses of 0.1 mg/kg p.o. and more (mice). The drug produced a moderate hypothermia at 10 mg/kg p.o. (rabbits), a mild increase in pain threshold at 3 mg/kg p.o. (mice and rats) and a slowing of cortical EEG at 1 mg/kg i.v. (cats). ED50 values of drug for the potentiation of ether and alcohol anesthesia were 0.34 and 0.22 mg/kg p.o., respectively (mice). Timiperone ahd neither an anticonvulsant activity at 30 mg/kg p.o. (mice) nor an effect on the spinal reflex at 1 mg/kg i.v. (cats). These effects of timiperone on the central nervous system were almost similar to those of haloperidol. 2. Respiratory and cardiovascular system: At dose of 0.03 mg/kg i.v. and more, timiperone produced transient increases in respiratory rate and regional arterial blood flow which were accompanied by a fall in blood pressure (dogs). Haloperidol had qualitatively similar effect, but was weaker than timiperone. Both drugs at high concentration (3X10-6 g/ml) exerted negative inotropic and chronotropic effect in isolated atrial preparations (guinea-pigs), and non-competitively antagonized the positive chronotropic action of isoprenaline. Atropine (2.5X10-7 g/ml) failed to modify the chronotropic action of timiperone (3X10-6 g/ml). 3. Autonomic nervous system: Timiperone at 0.1 mg/kg p.o. and haloperidol at 0.3 mg/kg p.o. induced a moderate miosis (rabbits) and antagonized blood responses to noradrenaline and acetylcholine (dogs). Both drugs at 1 mg/kg i.v. had no ganglion-blocking activity (cats). 4. Smooth muscle: In isolated guinea-pig ileum and vas deferens, timiperone and haloperidol (10-5 g/ml) antagonized the contractile responses of the muscles to various spasmogens, Both drugs at approximately 10-6 g/ml decreased spontaneous motility of the isolated rat uterus and inhibited the gastric secretion at 1 mg/kg i.p. (rats). At high doses, both drugs inhibited the gastrointestinal propulsion (mice), motility (dogs) and gastric emptying rate (rats), and had no damaging effect on the gastric mucosa (rats). 5. Skeletal muscle: At 0.1 mg/kg i.v., timiperone and haloperidol slightly enhanced twitch response of the anterior tibial muscle to electrical stimulation (rabbits). 6. Urine volume and urinary electrolytes: Timiperone and haloperidol showed a diuretic effect at 3 mg/kg p.o. whereas they inhibited urine output and electrolytes excretion at 30 mg/kg p.o. (rats).