天花粉抗早孕作用的药理研究

小鼠妊娠第4、5日皮下注射天花粉,其抗早孕ED₅₀为1.78±0.28 mg/kg。天花粉的抗早孕作用可被甲地孕酮和HCG所部分拮抗,而为15-甲-PGF_2α所增强。抗早孕剂量天花粉对假孕小鼠的蜕膜有明显抑制作用。其抗早孕作用及抑制蜕膜作用均随剂量增加而增强。外源性甲地孕酮可对抗其抗早孕作用和抑制蜕膜作用。提示天花粉的抗早孕作用与其抑制蜕膜反应有关。外源性甲地孕酮有对抗天花粉抑制蜕膜反应的作用,提示天花粉有可能通过对抗假孕小鼠体内黄体激素作用而发挥抑制蜕膜反应的作用。本文初步探讨了这种对抗作用。     

丙酸睾丸酮抗早孕作用的药理研究

本文研究表明丙酸睾丸酮在小鼠有明显的抗早孕作用。其抗早孕作用的ED₅₀=0.11±0.03 mg/kg。甲地孕酮、HCG明显对抗丙睾抗早孕作用。丙睾在抗早孕剂量时能明显抑制假孕小鼠蜕膜反应。甲地孕酮能明显对抗丙睾抑制假孕小鼠蜕膜反应的作用。但丙睾对去卵巢小鼠应用外源性雌、孕激素诱发的蜕膜反应无明显抑制作用。丙睾无溶黄体作用,也不增强子宫对催产素和15-甲基-PGF_2α的反应。实验结果提示丙睾抗早孕作用与其抑制蜕膜反应有关。丙睾对蜕膜反应的抑制作用是其抑制下丘脑—垂体—卵巢轴,而非直接拮抗雌、孕激素的结果。     

浙贝母的抗溃疡和镇痛作用

ig浙贝母醇提物（相当生药0．8，2．4g／kg），可抑制水浸应激性和盐酸性小鼠胃溃疡形成，但对吲哚美辛－乙醇性小鼠溃疡模型中抗溃疡作用不明显；能抑制醋酸致小鼠扭体反应和热痛刺激引起的甩尾反应；小鼠LD50（ig）为12．2±2．2g／kg。     

丙酸睾丸酮抗早孕作用的药理研究

本文研究表明丙酸睾丸酮在小鼠有明显的抗早孕作用。其抗早孕作用的ED_(50)=0.11±0.03 mg/kg。甲地孕酮、HCG明显对抗丙睾抗早孕作用。丙睾在抗早孕剂量时能明显抑制假孕小鼠蜕膜反应。甲地孕酮能明显对抗丙睾抑制假孕小鼠蜕膜反应的作用。但丙睾对去卵巢小鼠应用外源性雌、孕激素诱发的蜕膜反应无明显抑制作用。丙睾无溶黄体作用,也不增强子宫对催产素和15-甲基-PGF_(2α)的反应。实验结果提示丙睾抗早孕作用与其抑制蜕膜反应有关。丙睾对蜕膜反应的抑制作用是其抑制下丘脑—垂体—卵巢轴,而非直接拮抗雌、孕激素的结果。     

吲哚拉新(Indolacin)的药理研究

吲哚拉新灌胃给药,对角叉菜胶所致大鼠踝关节肿胀具有抑制作用,其 ED_(50)为11.6±6.0mg/kg,对醋酸所致小鼠扭体反应具有抑制作用,其 ED_(50)为111.7±18.1mg/kg。吲哚拉新腹腔注射30mg/kg,对四联菌苗所致家兔体温升高具有降低作用。吲哚拉新灌胃给药80mg/kg 和100mg/kg,对部分大鼠有致胃溃疡作用;同时灌胃给予白芨—甘草和角叉菜胶,剂量均为1600mg/kg,均有抗吲哚拉新致胃溃疡作用。     

北豆根总碱的抗炎作用及毒性试验

北豆根总碱的抗炎作用在剂量为370.4和185.2mg/kg时可明显抑制二甲苯引起的小鼠耳肿胀及醋酸引起的小鼠腹腔毛细血管透透性,并有一定的量效关系其灌胃LD50=2.56±0.388g/kg;腹腔LD50=63.32±4.31mg/kg.     

非甾体抗炎新药舒林酸的抗炎,镇痛和解热作用

舒林酸有明显的抗炎，镇痛、解热作用。灌胃给药使巴豆油致小鼠耳廓肿胀、角叉菜胶致大鼠足碱肿胀抑制２５％的半数有数量分别为３６±ｓ６和１４±５ｍｇ／ｋｇ，２０和４０ｍｇ／（ｋｇ．ｄ）或连续５ｄ对棉球肉芽肿和佐剂性关节炎也有显抑制作用，镇痛试验：小鼠热板法醋酸扭体法测得ＥＤ５０分别为４６±１９５２±１１ｍｇ／ｋｇ；命名酵母致热大鼠降低１℃的ＥＤ５０为６．２±２．５ｍｇ／ｋｇ；使大鼠试验群５０％致胃内血     

去氧乌头碱的抗炎、镇痛和解热作用

本文报告了新近以伏毛铁棒锤中提得的去氧乌头碱(DAC)的抗炎、镇痛和解热作用实验结果,并与已报道过的3-乙酰乌头碱(3AAC)进行比较。DAC0.8mg/kg (ip)显著抑制巴豆油所致小鼠耳廓肿;0.2mg/kg(ip或sc)显著抑制角叉菜胶或甲醛所致大鼠足爪肿、组胺所致大鼠皮肤渗出及醋酸所致小鼠腹腔渗出。于大鼠角叉菜胶足爪肿模型,测得DAC(ip)的抗炎治疗指数(6.38)略高于3AAC(5.92)。醋酸扭体法测得DAC抑制小鼠扭体反应50％的剂量为0.22±0.06mg/kg(sc);热板法测得DAC的小鼠镇痛ED_(50)为0.41±0.10mg/kg(ip),其镇痛治疗指数(6.37)高于3AAC(4.60)。DAC0.24mg/kg(ip)对伤寒副伤寒混合菌苗所致家兔发热有显著解热作用。     

非甾体抗炎新药舒林酸的抗炎、镇痛和解热作用

舒林酸有明显的抗炎、镇痛、解热作用。灌胃给药使巴豆油致小鼠耳廓肿胀、角叉菜胶致大鼠足跖肿胀抑制２５％的半数有效量（ＥＤ５０）分别为３６±５６和１４±５ｍｇ／ｋｇ，２０和４０ｍｇ／（ｋｇ·ｄ）或连续５ｄ对棉球肉芽肿和佐剂性关节炎也有显著抑制作用。镇痛试验：小鼠热板法和醋酸扭体法测得ＥＤ５０分别为４６±１９和５２±１１ｍｇ／ｋｇ；使酵母致热大鼠降低１℃的ＥＤ５０为６．２±２．５ｍｇ／ｋｇ；使大鼠试验群５０％致胃出血的半数致溃疡量（ＵＤ５０）为５６±１２ｍｇ／ｋｇ。     

心得安抗惊厥作用的机理

本文初步分析了心得安抗小鼠SCZS和MES的作用机理。皮下注射低剂量心得安0.025～1mg/kg对抗SCZS呈剂量反应关系,表明此效应可能通过中枢β-肾上腺素受体阻断机制。用不改变MES反应率剂量的氨氧乙酸和氨基脲预先处理后,腹腔注射心得安抗MES的ED₆₀分別为3.8±0.9mg/kg和15.74±2.3mg/kg,对照组为10.74±1.6mg/kg,说明心得安抗MES与脑内GABA神经系统的功能有关。     

加锡果宁抗惊厥作用的机理

采用小鼠最大电休克惊厥法(MES),应用工具药物分析了加锡果宁(Ed)抗小鼠惊厥作用机理.结果,Ed具有较强的抗小鼠MES作用,其作用能被利血平、对氯苯丙胺、氟哌啶醇所对抗,被帕吉林、丙磺舒、L-色氨酸及L-多巴所增强.但α-甲基酪氨酸和酚妥拉明对其抗惊厥作用无明显影响。表明Ed抗惊厥作用与脑内5-MT,DA神经递质有关。     

苦杏仁甙药物动力学及其毒理初步研究

本文应用GC-RIA(岛津)气相色谱仪,分析了8只健康家兔在接受苦杏仁甙(Ⅰ)后的血药浓度,绘制药-时曲线,求生物半减期((?)±SD),t_(1/(2α))(分布相)=38±4min,t_(1/(2β))(消除相)=77±18min。(Ⅰ)对正常小鼠毒性实验提示(Ⅰ)引起中毒的主要因素,除了与用药剂量大小有关外,与用药途径的关系更为重要。剂量相同条件下,非胃肠道给药(静注)较之胃肠道给药安全得多。1例食管癌病人用苦杏仁甙治疗,对用药后血、尿进行检测。     

关于抗肿瘤药物的研究 Ⅶ.N-甲酰溶肉瘤素的抗瘤谱及毒性

N-甲酰溶肉瘤素是一种有效的抗肿瘤药,抗瘤譜广,在12种动物肿瘤中,对9种具有明显的抑制作用。对大鼠吉田肉瘤腹水型及实体型,Walker癌-肉瘤256等抑制作用最明显,抑制率为96—100%。对小鼠网織細胞肉瘤L₂抑制率为60—70%;对腹水瘤L₁及Krebs-2腹水癌亦有明显抑制作用,分別延长寿命5天及7天;对Ehrlich癌腹水型小鼠,可延长寿命2.2—2.6天;对Ehrlich癌实体型及梭形細胞肉瘤B₂₂抑制率分別为30—41%及36—43%。在不致中毒的剂量下,对小鼠肉瘤180,肉瘤AK,黑色素瘤Me則无明显抑制作用。口服N-甲酰溶肉瘤素对小鼠及大鼠的半数致死量(LD₅₀±S.E.)分別为730±79毫克/公斤及700±79毫克/公斤;腹腔內給药則分別为152±7毫克/公斤及80±10毫克/公斤。靜脉注射对小鼠的半数致死量为155±10毫克/公斤。     

Absence of anxiolytic effects of calcium channel antagonists

The potential anxiolytic effects of some calcium channel antagonists (nifedipine, nicardipine, and ±verapamil) were investigated in the elevated plus-maze test in mice. The acute effects of the above-mentioned drugs were compared with those of phenobarbitone and ±propanolol. Results showed that control mice spent less time in the open than in the closed arms, reflecting increased anxiety. Both phenobarbitone (20 mg/kg i.p.) and ±propanolol (5 mg/kg i.p.) increased the percentage of entries into open arms as well as the time spent on the open arms. Nifedipine (2 and 4 mg/kg i.p.), nicardipine (0.5 and 1.0 mg/kg i.p.), and ±verapamil (5 and 10 mg/kg i.p.) failed to alter significantly the behavior of mice. In summary, although there have been some reports based on other tests that calcium antagonists may have potential anxiolytic properties, this conclusion has not been supported by our results from the elevated plus-maze test.     

蜂花粉对小鼠血清IgM和IgG含量的影响

以单向免疫扩散试验观察蜂花粉对小鼠血清IgM和IgG含量的影响,结果表明蜂花粉提高正常小鼠及环磷酰胺、氢化可的松、~(60)Co照射与荷瘤所致免疫低下小鼠的血清IgM和IgG含量。并初步分析了作用机理。     

Gallium nitrate suppresses lupus in MRL/lpr mice

Gallium (Ga) nitrate, a drug which prevents a variety of experimental autoimmune diseases, was investigated in a murine model of systemic lupus erythematosus (SLE). In one experiment, female MRL/Mp lpr/lpr (MRL/lpr) mice were randomized into 2 groups of 6:1) vehicle (trisodium citrate) and 2) Ga. Subcutaneous injections began at 3 weeks of age and continued weekly until the mice were euthanized a week after the thirteenth injection. The loading dose of Ga (calculated as elemental Ga) was 45 mg/kg, followed by 15 mg/kg/week. In another experiment (n = 18) with 3 males and 3 females per group, mice received 1) vehicle, 2) Ga × 1 (one 45 mg/kg dose), and 3) Ga × 13. In the experiment with 12 mice, axillary lymph nodes from Ga-treated mice were significantly smaller than those from vehicle-treated mice (91 ± 42 and 360 ± 358 mg respectively, mean ± SD), and spleens as well as lymph nodes from the former showed significantly less lymphoid infiltrate. In the experiment with 18 mice, prescapular lymph nodes weighed 312 ± 98, 217 ± 52, and 42 ± 34 mg, and spleens weighed 732 ± 492, 409 ± 164, and 192 ± 93 mg in the groups which received vehicle, Ga × 1, and Ga × 13 respectively. Control mice had significantly more lymphoid infiltrates in the lungs, spleen, and lymph nodes and, unlike Ga × 13 mice, exhibited glomerulitis and renal vasculitis. Within groups, females developed more severe disease than males. The Ga × 13 group had increased percentages of CD4-bearing and CD8-bearing lymphocytes in lymph nodes and increased CD4-bearing lymphocytes in the spleen, with an increased proliferative response to mitogen stimulation in vitro in lymph nodes, although not in the spleen. The Ga × 13 group also gained less weight and developed osteosclerosis. Although preliminary, our findings suggest that clinical trials with Ga in SLE are merited. Received: 9 January 1997 / Accepted: 30 May 1997     

Inhibition effect of dehydroascorbic acid on insulin secretion from mouse pancreatic islets.

Intravenous doses of 200 mg/kg dehydroascorbic acid (DHA) produced hyperglycemia, hypoinsulinemia, and decreased glucose tolerance in mice. This effect of DHA is mediated, at least in part, through a direct inhibition of pancreatic insulin release. Exposure of isolated pancreatic islets to a concentration of 2.0 mg/dl DHA reduces the responsiveness of the islets to both glucose (300 mg/dl) and tolbutamide (6±10^?3m). Exposure of isolated islets to DHA in a high concentration of d-glucose (300 mg/dl) partially protected them against the inhibitory effect of DHA. Exposure of islets to 4.0 mg/dl of DHA causes a leakage of insulin. Similarly, islets isolated from mice which had been treated with 300 mg/kg DHA iv exhibited increased insulin release in the presence of only 60 mg/dl glucose. Intravenous administration of either 200 or 300 mg/kg DHA prior to islet isolation results in increased insulin secretion in response to 300 mg/dl glucose. The results show that the pancreatic effects of DHA are similar to those of the diabetogen, alloxan.     

Antidiarrheal,antisecretory, and bronchodilatory activities of Hypericum perforatum

This study describes the antidiarrheal, antisecretory, and bronchodilatory activities of Hypericum perforatum Linn. (Hypericaceae), commonly known as St. John’s wort, to justify its traditional use in the hyperactivity of the gastrointestinal and respiratory systems. The crude extract of Hypericum perforatum (Hp.Cr) at a dose of 500?mg/kg caused 20% protection against castor oil-induced diarrhea in mice and 60% at 1000?mg/kg (p?<?0.05 vs. saline). Hp.Cr at 300 and 1000?mg/kg reduced the castor oil-induced fluid accumulation in mice to 107.0?±?3.3?g (p?<?0.01) and 84.0?±?4.2?g (p?<?0.001) respectively, whereas in the castor oil-treated group, it was 126.9?±?3.9?g. When tested against carbachol (CCh)-mediated bronchoconstriction in rats under anesthesia, Hp.Cr dose-dependently (3–?30?mg/kg) suppressed the CCh (1?μmol/kg)-induced increase in the inspiratory pressure. Thus this study rationalizes the Hypericum perforatum usefulness in overactive gut and airways disorders, such as diarrhea and asthma.