Inhibiting Activity of Some Glucoindolalkaloids and Iridoids from Sickingia williamsii on Electrically Induced Contractions of Isolated Guinea-pig Ileum

The present study examined the effects of the extracts (petroleum ether, CHCl₃, CHCl₃/MeOH (9:1) and MeOH), partially purified fractions and pure compounds (mainly alkaloids and iridoids) from Sickingia williamsii on the electrically induced contractions of the isolated guinea-pig ileum. The results of our experiments indicate that CHCl₃/MeOH (9:1) and CHCl₃ extracts, tested at concentrations of 300, 150 and 30 μg/mL, dose-dependently reduced the guinea-pig ileum electrical contractions, whereas MeOH and petroleum ether extracts did not affect it. Furthermore, both the partially purified fractions I–IV each tested at concentrations of 500, 250 and 100 μg/mL from the CHCl₃/MeOH (9:1) extract and some pure compounds (10⁻⁴ M , 5×10⁻⁵ M and 2.5×10⁻⁵ M ) isolated and purified from the above fractions significantly reduced, in a dose dependent manner, the electrical contractions of the ileum. As the active pure compounds possess an indole nucleus or/and an iridoid nucleus in their structures, the inhibitory effects appear to depend on these structures.     

Effect of molluscicidal components of Abrus precatorius,Argemone mexicana and Nerium indicum on certain biochemical parameters of Lymnaeu acuminata

Exposure to 40% and 80% of the 24 h LC₅₀ of the molluscicidal component of Abrus precatorius (abrin and glycyrrhizin), Argemone mexicana (protopine and sanguinarine) and Nerium indicum (oleandrin) caused a significant decrease in the levels of protein, free amino acid, DNA and RNA in the nervous tissue of Lymnaea acuminata. Except for glycyrrhizin, all the above molluscicides caused a significant reduction in phospholipid levels and a simultaneous increase in the rate of lipid peroxidation in the nervous tissue of treated snails. Copyright © 1999 John Wiley & Sons, Ltd.     

川芎嗪对吗啡依赖离体豚鼠回肠戒断收缩的影响

目的观察中药川芎的主要成分川芎嗪对吗啡依赖离体豚鼠回肠催促戒断反应的影响,评价川芎嗪对吗啡依赖豚鼠回肠的作用。方法采用豚鼠回肠体外孵育方法。催促戒断收缩由1μmol/L纳络酮加入已在含3μmol/L吗啡的37.5℃Krebs液中孵育4 h的离体豚鼠回肠引起。分别在给予纳络酮前、后1 min加入不同浓度的盐酸川芎嗪,观察豚鼠回肠的收缩反应。结果川芎嗪100,200,300μmol/L对正常回肠收缩未见明显影响。当川芎嗪100,200,300μmol/L在加入纳洛酮前1 min给药,纳洛酮催促的回肠戒断性收缩被明显抑制,与吗啡依赖对照组相比较有显著性差异(P<0.05或P<0.01)。川芎嗪200,300μmol/L在加入纳洛酮后1 min给药,对戒断性收缩也有明显抑制作用。结论川芎嗪对纳洛酮催促的吗啡依赖豚鼠离体回肠戒断性收缩的形成有抑制作用,对已出现的戒断收缩也有明显阻断作用。提示川芎嗪具有抑制吗啡戒断症状的作用。     

小半夏汤对豚鼠离体肠管运动的影响

目的: 观察小半夏汤对豚鼠离体肠管收缩的影响,初步探讨其止吐的作用机制。 方法: 利用离体浴槽,观察小半夏汤[(生药,下同) 0, 0.1, 0.25, 0.5, 1, 2.5, 5, 10, 20, 40 g·L^-1]对豚鼠离体肠管自主收缩平均张力、振幅和频率的影响;以呕吐相关受体激动剂乙酰胆碱(Ach)、组胺(His)、五羟色胺(5-HT)、多巴胺(DA)为工具药,观察小半夏汤0, 2, 5, 10 g·L^-1对各工具药致豚鼠离体肠管收缩平均张力、振幅、频率和最大张力的影响。 结果: 小半夏汤能剂量依赖性地抑制豚鼠离体肠管自主收缩,降低其收缩平均张力、振幅和频率(与空白对照组相比,P<0.05或P<0.01);先加Ach,His,5-HT再加小半夏汤2,5,10 g·L^-1或小半夏汤2,5,10 g·L^-1预处理均能明显抑制3种工具药所致肠管收缩,减少肠管收缩平均张力、振幅、频率和最大张力(分别与给小半夏汤前和不给小半夏汤相比,P<0.05或P<0.01);小半夏汤能够增大DA致肠管收缩平均张力、振幅和频率(分别与给小半夏汤前和不给小半夏汤相比,P<0.05或P<0.01),但对肠管收缩最小张力无明显影响。 结论: 小半夏汤能够抑制豚鼠离体肠管自主收缩,其作用机制可能是通过阻断M受体、H₁受体、5-HT受体和D₂受体等呕吐相关受体而介导,或直接作用于肠平滑肌而起作用,其止呕机制有待进一步研究。     

Differential antagonistic effect of hydroalcoholic extract from Hymenaea martiana hayne arzeik on kinin and other agonist-induced contractions of the isolated rat uterus and Guinea-pig ileum

This study was undertaken to evaluate the action of the hydroalcoholic extract (HE) from the bark of Hymenaea martiana on bradykinin (BK), lysyl-bradykinin (L-BK), acetylcholine (ACh), angiotensin II (AII), prostaglandin F_2a (PGF_2a), serotonin (5-HT), oxytocin (Ot) and histamine (His)-induced contractions of the isolated rat uterine muscle and guinea-pig ileum. The HE (50–200 μg/mL) added to the bath for 20 min caused a concentration-dependent rightward displacement of BK, L-BK and ACh-induced contractions in the rat uterus, allied to a discrete but significant reduction of maximal responses to the latter two agonists. By contrast, at the same range of concentrations the HE antagonized in a concentration-dependent but noncompetitive manner the contractions induced by AII, but only at high concentrations (200 μg/mL) it significantly inhibited contractions evoked by both PGF_2a and Ot, while contractile responses induced by 5-HT were not affected. In the guinea-pig ileum, the HE of H. martiana (50 and 100 μg/ml) caused a discrete rightward displacement of the BK and ACh concentration—response curves. Higher concentrations of the HE of H. martiana (200 μg/mL) caused a marked depression of BK and ACh-induced maximal responses. These findings show that the active principle(s) presents in the HE from the bark of H. martiana exhibits an interesting pharmacological profile against several neurotransmitter-induced contractions in nonvascular smooth muscles. Such actions may be relevant for supporting, at least in part, the use of this plant in folk medicine.     

檀香不同萃取物对豚鼠离体肠平滑肌收缩的影响

目的:观察檀香不同萃取物对豚鼠离体回肠平滑肌收缩的影响,探讨其作用机制.方法:利用BL-420F生物机能实验系统,在HW-400S恒温平滑肌浴槽中,37℃下观察檀香不同萃取物对豚鼠离体回肠运动功能的影响.结果:檀香水提液乙醚萃取物、檀香水提液乙酸乙酯萃取物、檀香醇提液乙醚萃取物、檀香醇提液乙酸乙酯萃取物对豚鼠离体肠自主运动有抑制作用(P＜0.01),表现为振幅减低;檀香水提液乙醚萃取物、檀香水提液乙酸乙酯萃取物、檀香醇提液石油醚萃取物、檀香醇提液乙醚萃取物、檀香醇提液乙酸乙酯萃取物对乙酰胆碱( Ach)造成的豚鼠离体肠痉挛状态有拮抗作用(P＜0.01),表现为振幅减低;檀香水提液乙酸乙酯萃取物对阿托品造成的松弛状态有明显的协同作用(P＜0.01),表现为振幅减低.结论:檀香不同萃取物对豚鼠离体肠平滑肌有抑制作用.     

湖北利川黄连不同生长龄期主要生物碱的分布及变化

目的:研究湖北利川黄连不同生长龄期主要生物碱的累积变化过程,为标准化种植提供科学依据.方法:采用紫外分光光度法和HPLC测定黄连有效成分.结果:随着生长龄期的增长,黄连叶片数、根茎干重都在不断的增加;黄连不同部位中总生物碱含量的由大到小的顺序依次是根茎＞须根＞叶片;在黄连2～3龄阶段为黄连生长最旺盛的时期,酪氨酸、总生物碱、小檗碱、黄连碱、巴马汀和小檗碱的含量增长速度最快;在5龄阶段,这4种生物碱含量的大小顺序依次是小檗碱、黄连碱、表小檗碱、巴马汀,且这4种生物碱含量之和占总生物碱含量的比例在不断增加.结论:为黄连的种植管理提供了参考.     

不同透皮促渗剂对苦豆子凝胶剂中生物碱体外透皮吸收的影响

目的：研究透皮促渗剂对苦豆子凝胶中槐定碱和苦参碱透皮吸收的影响,筛选最佳透皮促渗剂。方法：以SD大鼠皮肤为渗透屏障,采用Franz扩散池进行体外透皮吸收实验,高效液相色谱法(HPLC)测定槐定碱和苦参碱的含量,计算渗透动力学参数,评价不同促渗剂及联合使用对苦豆子凝胶剂透皮吸收的作用。结果：3种促渗剂单用时,对苦豆子凝胶剂中槐定碱和苦参碱透皮性能较好的为3%氮酮、4%冰片和4%薄荷醇。联合使用时,优选出的较佳复合促渗剂为1%冰片+1%薄荷脑,两者联合使用优于氮酮、冰片、薄荷脑单独使用及其他组合,其槐定碱和苦参碱24 h单位面积累积透过量(Q₂₄)可达6.858、7.018 mg·cm^-2,促渗倍数(ER)可达4.402、3.658,协同作用明显。结论：优选出的复合促渗剂对苦豆子凝胶剂中的槐定碱和苦参碱促渗效果较好,为苦豆子凝胶剂制备工艺及功效研究提供参考。     

Analgesic Activity and Effects on Isolated Smooth Muscle of Different Fractions of Hexane Extract from Araujia sericifera Brot

The present study analyses the analgesic activity and action on in vitro motility of methanol soluble and methanol insoluble fractions obtained from the hexane extract of fruits from Araujia sericifera . The methanol fraction did not show any pharmacological activity on the different tests evaluated. However, the insoluble methanol fraction exhibited an interesting analgesic effect in models of chemical and thermal stimulus and it reduced the E _max induced by histamine in vitro on guinea-pig ileum. This extract lacked any central depressor activity since it did not modify the number of mouse movements in the activity cage.     

栝楼不同部位对卷烟烟气总粒相物诱导人支气管上皮细胞增殖及炎症因子表达的影响

目的研究栝楼不同部位(瓜蒌皮、瓜蒌子、天花粉)对卷烟烟气总粒相物(Total particulate matter,TPM)诱导的人支气管上皮细胞(BEAS-2B)增殖以及白细胞介素6(IL-6)、白细胞介素8(IL-8)、肿瘤坏死因子α(TNF-α)表达的影响。方法采用TPM诱导BEAS-2B建立细胞损伤模型。实验分为空白对照组、模型组(10μg·mL-1TPM)、红霉素组(阳性对照,10μg·mL-1TPM+5μg·mL-1红霉素)及瓜蒌皮、瓜蒌子、天花粉不同浓度给药组[10μg·mL-1TPM+400、800、1200 ng·mL-1瓜蒌皮/瓜蒌子/天花粉(正丁醇提取物)]。药物作用24 h后,采用MTT法检测细胞增殖情况;采用实时荧光定量PCR法检测细胞IL-6、IL-8、TNF-αmRNA的表达;采用ELISA法检测细胞上清液中IL-6、IL-8和TNF-α的含量。结果与空白对照组比较,模型组的BEAS-2B细胞增殖受到明显抑制(P<0.01),细胞上清液中IL-6、IL-8和TNF-α含量明显升高(P<0.01),细胞IL-6、IL-8、TNF-αmRNA表达明显上调(P<0.01)。与模型组比较,不同浓度组的瓜蒌皮、瓜蒌子、天花粉均可以促进BEAS-2B细胞的增殖(P<0.05,P<0.01);400、800、1200 ng·mL-1瓜蒌皮组的细胞上清液中的IL-6、TNF-α含量及mRNA表达明显下调(P<0.01),800、1200 ng·mL-1瓜蒌皮组的细胞上清液中的IL-8含量及mRNA表达明显下调(P<0.01);400、800、1200 ng·mL-1瓜蒌子组的细胞上清液中的IL-8、TNF-α含量及mRNA表达明显下调(P<0.01);400、800、1200 ng·mL-1天花粉组的细胞上清液中的IL-6、TNF-α含量及mRNA表达明显下调(P<0.05,P<0.01)。结论栝楼不同部位(瓜蒌皮、瓜蒌子和天花粉)正丁醇提取物可能通过促进BEAS-2B细胞增殖,抑制TNF-α、IL-6、IL-8等炎症因子表达,从而发挥其抗炎作用。