菟丝子水提物对人精子膜结构和功能氧化损伤的干预作用

 目的观察菟丝子水提物对活性氧(ROS)所致人精子膜结构和功能氧化损伤的干预作用及其对精子膜功能的保护作用。探讨菟丝子治疗男性不育弱精子症的作用机制。方法采用Percoll梯度离心法优选具有正常生理功能的精子作为正常精子模型,将精子悬液分为正常组、模型组、阳性药对照组(维生素C组)和菟丝子水提物小、中、大剂量组,应用次黄嘌呤-黄嘌呤氧化酶(HX-XO)体系产生ROS,在有氧环境下,不同剂量(每1 mL含0.125,0.25和0.5 g生药)的菟丝子水提物与精子悬液共同孵育后,检测精子膜脂质过氧化损伤程度,通过精子低渗膨胀试验评估精子膜功能,并与已知的抗氧化剂维生素C对照。结果菟丝子水提物小、中、大剂量组(每1 mL含0.125,0.25和0.5 g生药)在相同的条件下均可提高精子悬液超氧化物歧化酶(SOD)活力,降低丙二醛(MDA)含量,对ROS所致精子膜的损伤均具有不同程度的干预作用,对精子膜功能具有一定的保护作用。其中每1 mL含0.125,0.5 g生药的菟丝子水提物组与维生素C组(0.25 g·L^-1)无明显差别(均P>0.05),0.25 g生药的菟丝子水提物组明显优于维生素C组(P<0.001)。结论适量的菟丝子水提物能显著提高精子悬液SOD活力,降低MDA含量,通过其抗氧化作用干预ROS对精子膜的脂质过氧化反应,对精子膜结构和功能具有明显的保护作用,这可能是菟丝子治疗男性不育弱精子症的作用机制之一。     

菟丝子水提物对人精子顶体和超微结构的保护作用

目的:观察菟丝子水提物对活性氧(ROS)所致人精子顶体和超微结构的氧化损伤的保护作用,探讨菟丝子治疗男性不育弱精子症的作用机制。方法:采用Percoll梯度离心法优选具有正常生理功能的精子作为正常精子模型,将精子悬液分为正常组,模型组,阳性药对照组(维生素C组)和菟丝子小、中、大剂量组。应用次黄嘌呤-黄嘌呤氧化酶(HX-XO)体系产生活性氧,在有氧环境下,ROS、不同含量(0.125,0.25,0.5 g.mL^-1)的菟丝子水提物与精子悬液共同孵育后,计算精子顶体完整率,透射电镜观察精子顶体和超微结构,并与已知的抗氧化剂维生素C对照。结果:终含量0.125,0.5 g.mL^-1的菟丝子水提物对精子顶体和超微结构的保护作用与维生素C(0.25 mg.mL^-1)无明显差别(P均>0.05),0.25 g.mL^-1的菟丝子水提物的作用明显优于维生素C(P<0.001)。结论:适宜含量的菟丝子水提物对ROS造成的精子膜、顶体结构和精子线粒体功能损伤具有明显的保护作用。     

白芍总苷在急性CCl4肝损伤大鼠与正常大鼠体内的药代动力学比较研究

 目的 比较白芍总苷在急性CCl₄ 肝损伤大鼠与正常大鼠体内药物动力学过程的异同,为临床合理用药提供参考。方法 采用一次性腹腔注射CCl₄建立大鼠急性肝损伤模型,采用HPLC测定模型大鼠和正常大鼠灌胃给予白芍总苷后,不同时间点的Pae和Alb的血药浓度,根据药-时曲线计算药代动力学参数。结果 在模型组大鼠体内,白芍总苷中芍药苷（Pae）和芍药内酯苷（Alb）在高、中、低剂量（0.047、0.141、0.282 g·mL^-1）时的 t1/2分别为 5.02、4.52、4.91 h;5.22、5.04、5.05 h。ρ_max分别为22.54、14.52、5.49 μg·mL^-1;9.02、5.04、2.34 μg·mL^-1。AUC_0-t分别为（146.55±7.52）、（84.14±7.84）、（31.62±2.97）μg·h·mL^-1;（56.56±8.70）、（32.18±3.49）、（13.48±1.66） μg ·h·mL^-1。tmax 均为 2 h。在正常大鼠体内,Pae和Alb在高、中、低剂量（0.047、0.141、0.282 g·mL^-1）时的 t1/2 分别为3.95、3.69、3.95 h;3.74、3.98、3.79 h。ρ_max分别为19.16、11.60、4.46 μg·mL^-1;7.16、4.00、1.93 μg·mL^-1。AUC_0-t 分别为（116.26.6±19.99）、（67.74±12.79）、（25.01±2.62） μg·h·mL^-1;（45.03±5.84）、（27.26±3.57）、（10.59±1.86）μg·h· mL^-1。tmax为 2.5 h。结论 与正常组比较,模型组的ρ_max、AUC_0-t 显著增大,t1/2延长,t_max明显缩短。模型组和正常组的tmax和t1/2不受白芍总苷剂量影响,但剂量与ρ_max和AUC_0-t具一定的相关性。
     

地龙注射液对屋尘螨致敏气道上皮细胞TGF-β1/Smad2表达的影响

 目的 观察地龙注射液对细胞哮喘模型中转化生长因子（TGF）-β₁、Smad2表达的影响,探讨地龙在支气管哮喘治疗中的作用机制及价值。方法 给予人支气管上皮细胞系BEP2D（HBE）以不同的干预和治疗,分为：单纯培养组即对照组（A组）,屋尘螨(dermatophagoides pteronyssinus,Derp1)（10 μg·mL^-1）组（B组）,Derp1（10 μg·mL^-1）+ 地塞米松（dexamethasone,DEX）（1×10^-6mol·L^-1）组（C组）,Derp1（10 μg·mL^-1）+地龙注射液（0.9 mg·mL^-1）组（D组）,Derp1（10 μg·mL^-1）+地龙注射液（9 mg·mL^-1）组（E组）, Derp1（10 μg·mL^-1）+地龙注射液（18 mg·mL^-1）组（F组）,培养72 h,RT-PCR法检测各组细胞TGF-β₁ mRNA, Smad2 mRNA 表达;并收集以上各组上清液,作用于人胚肺成纤维细胞（HLF）72 h,免疫细胞化学法检测纤维连接蛋白(Fibronectin,FN)表达。结果 B组TGF-β₁mRNA, Smad2 mRNA表达较A组明显升高（P<0.01）;各地龙组及C组,TGF-β₁ mRNA、Smad2 mRNA表达低于B组,有显著性差异(P<0.01),与A组比较均无显著性差异（P>0.05）;各组HLF中FN表达与HBE各对应组TGF-β₁ mRNA表达呈正相关性。结论 地龙注射液有抑制哮喘气道重构的作用,其机制可能与抑制TGF-β₁/Smad2 信号通路有关。     

夏至草醇提物对大鼠淋巴循环作用的实验研究

 目的探讨夏至草醇提物对淋巴循环的调节作用。方法采用淋巴微循环观察、淋巴引流及淋巴液流变学技术,观察夏至草醇提物对32只大鼠肠淋巴循环的作用。结果静脉推注夏至草醇提物后,在6 g·kg^-1剂量时肠系膜淋巴管收缩频率及幅度均增大,3 g·kg^-1剂量时收缩幅度也增加,均显著高于给药前及对照组(P<0.05);高剂量组的肠淋巴流量、蛋白输出量和淋巴细胞输出量明显高于给药前及对照组(P<0.05);中及高剂量组均能明显降低淋巴液黏度,但1 g·kg^-1剂量对淋巴循环未发生影响。结论较大剂量夏至草醇提物具有增强淋巴管收缩性、淋巴液转运及降低淋巴液黏度的作用。     

熟地黄水提物含药血清对HUVECs-1细胞增殖及EPO表达的影响

目的：探讨熟地黄水提物含药血清对人脐静脉内皮细胞-1(HUVECs-1)增殖的影响及其机制。方法：熟地黄水提物3，6，10 g·kg^-1分别给SD大鼠灌胃1周，取血制备含药血清，加入血管内皮细胞培养液。采用MTT法观察血清对HUVECs-1增殖的影响，免疫细胞化学染色和Western blot检测血清对HUVECs-1表达红细胞生成素(EPO)的影响。结果：与相同浓度的NS血清组比较，3，6 g·kg^-1地黄水提液含药血清组HUVEC-1吸光度显著升高(P＜0.05)。免疫组化结果显示，3，6 g·kg^-1熟地黄水提物5%含药血清组与相同浓度NS血清组比较，3，6，10 g·kg^-1熟地黄水提物10%，20%含药血清组与相同浓度NS血清组比较，EPO免疫反应阳性细胞平均吸光度均显著增加(P＜0.05)。Western blot分析显示：与NS血清组比较，6 g·kg^-1熟地黄水提物相同浓度含药血清各组EPO相对条带吸光度值(IOD)均显著增高(P＜0.05)。结论：中药熟地黄水提物含药血清可上调血管内皮细胞EPO表达，对血管内皮细胞有显著的促增殖作用。     

双苓扶正抗癌制剂对SGC-7901细胞增殖及c-myc基因表达的研究

目的：研究双苓扶正抗癌制剂对人胃癌细胞增殖及c-myc基因表达的影响。方法：采用MTT比色法,观察双苓扶正抗癌制剂（40～640 μg·mL^-1）5个剂量组单用及其与阿霉素（0.4,4.0 μg·mL^-1）及顺铂（0.1,1.0 μg·mL^-1）分别合用在体外对人胃癌SGC-7901细胞增殖的抑制作用；采用流式细胞技术检测该制剂（80～320 μg·mL^-1）对c-myc基因阳性蛋白标记率的影响。结果：双苓扶正抗癌制剂单用体外作用24 h,对人胃癌细胞增殖具有抑制作用,在40～640 μg·mL^-1剂量下,其抑制率随剂量增加而增加；与阿霉素(0.4,4.0 μg·mL^-1)或顺铂(0.1,1.0 μg·mL^-1)分别合用,可提高对人胃癌细胞的抑制率；在80～320 μg·mL^-1剂量下,可抑制c-myc基因的表达。结论：双苓扶正抗癌制剂单用对人胃癌细胞增殖具有抑制作用,且具有量效关系；与阿霉素或顺铂分别合用对人胃癌细胞的抑制作用具有协同效应；下调c-myc基因的表达可能是该制剂抑制肿瘤细胞增殖的作用机制之一。     

赤箭和天麻调节免疫功能和肠道菌群作用比较

目的 对赤箭（天麻地上部分）和天麻中腺苷、天麻素、对羟基苯甲醇、对羟基苯甲醛、巴利森苷B和A 的成分含量,以及赤箭水提液和天麻水提液调节免疫功能和肠道菌群作用进行比较,评价赤箭进一步研究和开发的可行性。方法 采用超高效液相色谱法（UPLC）测定6种成分的含量,流动相0.1%甲酸水溶液（A）-乙腈（B）梯度洗脱（0~4 min,0.5%B; 4~5 min,0.5%~2%B;5~10 min,2%~15%B;10~12 min,15%~20%B; 12~15 min,20%~95%B;15~17 min,95%B;17~17.5 min,95%~0.5%B;17.5~20 min,0.5%B）,流速0.5 mL·min^-1,检测波长270 nm。采用环磷酰胺致小鼠免疫功能低下模型,测定廓清指数、校正廓清指数及外周血象,采用体外淋巴细胞转化试验测定B淋巴细胞增殖,基于16S rDNA技术测定肠道菌群并进行生物信息学分析,对赤箭水提液和天麻水提液进行药理活性比较。结果 赤箭粉末、醇提液中6个成分总量分别高于天麻粉末,醇提液,赤箭水提液和天麻水提液中6个成分含量总和相近,且赤箭粉末和天麻粉末中天麻素和对羟基苯甲醇总量均符合2020年版《中华人民共和国药典》的相关要求。与空白组比较,赤箭水提液中剂量（10 g·kg^-1）组和天麻水提液中、低剂量（10,5 g·kg^-1）组可明显增加免疫功能低下小鼠的廓清指数（P<0.05）;赤箭水提液、天麻水提液高剂量组（20 g·kg^-1）均可明显增高外周血中红细胞和红细胞压积水平（P<0.05,P<0.01）;400 g·L^-1天麻水提液和100 g·L^-1赤箭水提液对脂多糖诱导的B淋巴细胞增殖具有促进作用。肠道菌群研究显示,与空白组比较,在门水平上,赤箭水提液和天麻水提液增加拟杆菌门的相对丰度,降低厚壁菌门的相对丰度;在属水平上,赤箭水提液、天麻水提液均可增加Prevotellaceae_UCG-001和Ruminococcaceae_UCG-005的相对丰度,降低厌氧棍状菌属,unclassified_f_Erysipelotrichaceae和Candidatus_Stoquefichus的相对丰度,这些肠道菌与免疫系统、细胞增殖、调节代谢等相关。结论 赤箭粉末、醇提液、水提液所测腺苷、天麻素、对羟基苯甲醇、对羟基苯甲醛、巴利森苷B和A总量高于或者接近于天麻相应样品;赤箭水提液与天麻水提液药理活性相似,提示赤箭值得进一步研究与开发。     

蒜氨酸抗菌机制研究

目的 检测蒜氨酸最低抑菌浓度（MIC）与最低杀菌浓度（MBC）,探讨蒜氨酸体内外抗菌机制。方法 体外微量稀释法检测蒜氨酸MIC和MBC,荧光显微镜观察菌体表面蒜氨酸,探讨蒜氨酸抗菌机制。体内蒜氨酸和青霉素分别治疗金葡菌感染家兔脓肿,检测脓汁标本中细菌存活情况,探讨体内蒜氨酸抗菌作用。结果 蒜氨酸对大肠杆菌、伤寒杆菌、金黄色葡萄球菌、白色葡萄球菌的MIC分别为3.047 μg·mL^-1、6.094 μg·mL^-1、0.386 μg·mL^-1、0.386 μg·mL^-1,蒜氨酸体外无杀菌活性。浓汁标本：死菌率蒜氨酸治疗组显著高于阴性对照组（P < 0.01）,与青霉素治疗组无明显差异（P > 0.05）;活菌率蒜氨酸治疗组显著低于阴性对照组（P < 0.01）,与青霉素治疗组无明显差异（P > 0.05）。结论 蒜氨酸与菌体蛋白、细菌酶蛋白结合阻断细菌与环境物质交换,抑制细菌生命活动,具有较强的抑菌作用,无杀菌活性;蒜氨酸体内代谢成大蒜素,具有较强杀菌作用。     

β-榄香烯对非小细胞肺癌细胞迁移的影响及其机制研究＊

目的 探究β-榄香烯对非小细胞肺癌细胞迁移的影响及其作用机制。方法 将人非小细胞肺癌A549细胞分为5组：空白对照组、β-榄香烯低、中、高剂量组（10 μg·mL^-1、25 μg·mL^-1、50 μg·mL^-1）、顺铂（Cisplatin，CDDP，20 μmol/L）组。根据分组，分别用对应的药物处理细胞。Hoechst 33258染色观察细胞凋亡；Transwell小室检测细胞迁移；Western blot检测E-钙粘蛋白（E-cadherin）、波形蛋白（Vimentin）、磷酸化磷脂酰肌醇-3-激酶（Phosphorylated phosphatidylinositol-3-kinase，p-PI3K）与磷酸化蛋白激酶B（Phosphorylated protein kinase B，p-AKT）表达水平。结果 与空白对照组相比，β-榄香烯高剂量组A549细胞出现凋亡现象，各β-榄香烯组的A549细胞迁移数量均显著减少（P < 0.05），β-榄香烯中、高剂量组A549细胞E-cadherin蛋白表达水平明显升高（P < 0.05），Vimentin、p-PI3K与p-AKT蛋白表达水平明显降低（P < 0.05）。结论 β-榄香烯能诱导非小细胞肺癌A549细胞凋亡，抑制上皮-间质转化（Epithelial-Mesenchymal Transition，EMT）过程，进而减弱迁移能力，其作用机制可能与干扰PI3K/AKT信号通路的激活有关。     

骨碎补总黄酮对IL-1β介导的软骨肉瘤细胞SW1353干预的最适浓度范围

目的通过检测不同浓度的骨碎补总黄酮对IL-1β介导的SW1353细胞增殖、凋亡以及细胞形态的影响,探索最适药物干预浓度范围。方法细胞分为正常组、骨碎补1.0组、骨碎补0.5组、骨碎补0.25组、骨碎补0.125组、骨碎补0.0625组共6组,每组均以IL-1β10 ng/mL诱导细胞致炎,骨碎补1.0组以骨碎补1.0 mg/mL加药干预,骨碎补0.5组以骨碎补0.5 mg/mL加药干预,骨碎补0.25组以骨碎补0.25 mg/mL加药干预,骨碎补0.125组以骨碎补0.125 mg/mL加药干预,骨碎补0.0625组以骨碎补0.0625 mg/mL加药干预,在12、24、36、48 h 4个时间点检测SW1353细胞的增殖率与凋亡率,光镜下观察细胞形态。结果细胞增殖情况可见:骨碎补1.0组、骨碎补0.5组、骨碎补0.25组、骨碎补0.125组4组细胞在不同时间点,细胞均呈不增殖状态(P<0.01),0.0625组细胞增殖在12 h与36 h时与正常组无差异(P>0.05),在24 h与48 h时较正常组略低(P<0.01);细胞凋亡情况可见:骨碎补1.0组与骨碎补0.5组两组细胞凋亡率在10%以上,存活率不足正常组90%(P<0.01),骨碎补0.25组、骨碎补0.125组、骨碎补0.0625组3组细胞凋亡率<10%;光镜下结果可见:骨碎补1.0组、骨碎补0.5组两组细胞状态不佳,数量较少,骨碎补0.25组、骨碎补0.125组、骨碎补0.0625组3组细胞状态与正常组细胞相仿,但骨碎补0.25组细胞数量较少,骨碎补0.125组、骨碎补0.0625组细胞数量与正常细胞无明显差异。结论骨碎补总黄酮干预IL-1β介导的SW1353细胞选择的最适浓度范围为0.0625~0.25 mg/mL。     

In Vitro Cholinomimetic Effect of Loranthus Ferrugineus in Isolated Guinea Pig Ileum

This study aimed to elucidate the mechanism(s) of the spasmogenic action of Loranthus ferrugineus in isolated guinea pig ileum. Thus the contractile responses of guinea pig ileum to graded additions of either L. ferrugineus methanol extract or its n-butanol fraction were tested in the presence and absence of various pharmacological interventions. The data showed that L. ferrugineus methanol extract and the n-butanol fraction produced a concentration-dependent spasmogenic effect in isolated guinea pig ileum segments. These effects were significantly inhibited in the presence of 1 μM atropine. In contrast, the response to the lowest concentrations of L. ferrugineus methanol extract (0.25, 0.5 and 1 mg/mL) and n-butanol fraction of L. ferrugineus (0.125, 0.25 and 0.5 mg/mL) were considerably enhanced in the presence of 0.05 μM neostigmine. Neither L. ferrugineus methanol extract nor n-butanol fraction contractile responses were affected upon the incubation of the ileal segments with 100 μM hexamethonium. The results of this study show that the spasmogenic effect of L. ferrugineus is possibly mediated through a direct action on intestinal muscarinic receptors. It is suggested that the bioactive constituents of L. ferrugineus serve as a substrate for acetylcholinesterase.     

The kinetics of reversal of pre-sickled erythrocytes by the aqueous extract of Cajanus cajan seeds

The aqueous methanol extract (3:1, v/v) of the seeds of Cajanus cajan was investigated for antisickling properties. The extract possessed significant antisickling activity and was found to be concentration-dependent. The kinetics of reversal of presickled erythrocyte (HbSS) cells using the extract at 0.5 mg/mL, 1.0 mg/mL, 1.5 mg/mL, 2.0 mg/mL and 2.5 mg/mL showed first-order kinetics with rate constants of 5.833 x 10(-3) min(-1), 6.143 x 10(-3) min(-1), 5.957 x 10(-3) min(-1) 6.00 x 10(-3) min(-1) and 6.046 x 10(-3) min(-1), respectively, and with an average half-life 115.6 min. Phytochemical screening of the extract revealed the presence of free amino acids, phenolic compounds, tannins, globulins and saponins. These results show that the extract has potential use in the management of painful episodes experienced by sickle cell patients.     

巴戟天寡糖对小鼠精子生成作用的研究

 目的探讨巴戟天寡糖促进雄性小鼠生精的药理作用。方法采用环磷酰胺(CTX)引起的精子减少雄性小鼠模型。小鼠随机分为对照组、CTX模型组、巴戟天水提液组、巴戟天体积分数80%乙醇提取液组、巴戟天寡糖结晶组、甲睾酮组。建模后连续给药4周,观察给药组、模型组与对照组小鼠性器官以及精子数的差异。结果与模型组比较,巴戟天水提液组、巴戟天体积分数80%乙醇提取液、巴戟天总寡糖结晶组均具有明显的促进精子生成作用,其中以总寡糖结晶组作用最明显。结论巴戟天寡糖可能是巴戟天促进雄性小鼠生精作用的主要物质。     

枳棋子对酒后血中乙醇质量浓度和肝中乙醇脱氢酶活性的影响

目的探讨枳棋子对急性乙醇中毒的防治作用.方法雄性小鼠随机分为空白组、模型组、枳棋子提取物组,给药30 min后,模型组与枳棋子组灌酒0.015 mL·g-1,在灌酒后0.5,1,1.5,2,2.5,3 h分别摘眼球取血和取肝组织.采用生化酶法,测定小鼠酒后不同时间内血中乙醇浓度和肝中乙醇脱氢酶(ADH)活性.结果小鼠血中乙醇浓度在酒后0.5～1.5 h达到高峰,与模型组相比,枳棋子提取物组0.5～3 h内的血中乙醇浓度数值降低.枳棋子提取物组对小鼠酒后1～1.5 h肝中ADH的影响较为明显,使其活性增加;酒后2～3 h肝中ADH活性虽然也增强,但与模型组比较无显著差异.结论枳棋子提取物可降低酒后血中乙醇浓度,增强肝中ADH活性,其机制可能是通过抑制消化道对乙醇的吸收,从而起到有效的降醇解酒作用.     

Antiglycation and antioxidation properties of juglans regia and calendula officinalis: possible role in reducing diabetic complications and slowing down ageing

Objective

Accumulation of advanced glycation end products (AGEs) in the body due to the non-enzymatic glycation of proteins and oxidation is associated with aging and diabetes mellitus. In this study we wanted to investigate the antiglycation and antioxidation potential of two medicinal plants: Juglans regia and Calendula officinalis.

Methods

In-vitro investigation was carried out to discover the antiglycation and antioxidation potential of J. regia and C. officinalis. Using an Ultraviolet Double-beam Spectrophotometer, we evaluated the antiglycation property of the crude methanolic extracts of J. regia and C. officinalis by assessing their ability to inhibit the Maillard reaction. Employing the same instrument we also measured the antioxidation potential of these plant extracts using the nitric oxide (NO) free radical-scavenging assay.

Results

J. regia had greater antiglycation ability, with a minimum inhibitory concentration (MIC50) of 28 μg/mL as compared with that of C. officinalis (270 μg/mL). C. officinalis had greater antioxidation potential (26.10, 22.07 and 16.06% at 0.5 mg, 0.25 mg and 0.125 mg, respectively, as compared with 18.15, 16.50 and 16.06% of J. regia, respectively).

Conclusion

J. regia and C. officinalis inhibited the Maillard reaction and prevented oxidation in-vitro. Hence, the extracts of these plants could have therapeutic uses in curbing chronic diabetic complications and slowing down aging.     

The relaxation of isolated rabbit corpus cavernosum by the herbal medicine Catuama and its constituents

The effects of the Brazilian herbal medicine Catuama and each of its plant constituents (Paullinia cupana, Trichilia catigua, Zingiber officinalis and Ptychopetalum olacoides) were investigated on rabbit corpus cavernosum (RbCC) using a bioassay cascade. Catuama caused short-lived and dose-dependent relaxations (11% +/- 7%, 26% +/- 5% and 82% +/- 9%, at doses of 1, 3 and 10 mg, respectively). Neither the nitric oxide synthesis inhibitor N(omega)-nitro-L-arginine methyl ester (L-NAME; 10 microM) nor the soluble guanylate cyclase inhibitor ODQ (10 microM) significantly affected the Catuama-induced relaxations. Similarly, the selective ATP-dependent K(+) channel (K(ATP)) blocker glibenclamide (10 microM), the muscarinic receptor antagonist atropine (1 microM) and the voltage-dependent Na(+) channel blocker tetrodotoxin (1 microM) all failed to affect significantly the Catuama-induced relaxations. These results indicate that the relaxations induced by Catuama involve neither nitric oxide release nor K(ATP) channel activation. The extracts of P. cupana, Z. officinalis and P. olacoides caused short-lived and dose-dependent RbCC relaxations, whereas T. catigua evoked long-lasting relaxations which were occasionally preceded by a brief contractile effect. The extract of P. cupana was the most active in relaxing RbCC strips. The relaxations induced by all extracts were not significantly affected by L-NAME (10 microM). The infusion of ODQ (10 microM) had no significant effect on the P. cupana- and Z. officinalis-induced relaxations but reduced by >50% (p < 0.05) those evoked by P. olacoides and T. catigua. Incubations of RbCC with Catuama(10 mg/mL for 0.25 to 5 min) caused increases of cAMP levels (143% increase at 5 min of incubation). Incubations of RbCC with P. cupana extract (1 mg/mL) increased the cAMP levels by 200% whereas higher doses (10 and 100 mg/mL) caused smaller increases in the nucleotide levels (150% and 89%, respectively). The extracts of Z. officinalis and P. olacoides (same doses) caused smaller increases of the cAMP levels compared with the P. cupana extract, whereas T. catigua (1-100 mg) did not increase the levels of this nucleotide above the basal values. Our results show that of the four extracts assayed, P. cupana was the most effective, indicating that it is the main extract responsible for the relaxing effect of Catuama on rabbit cavernosal tissue.     

The in vitro screening for acetylcholinesterase inhibition and antioxidant activity of medicinal plants from Portugal

Essential oil, ethanolic extract and decoction of 10 plant species from interior Portugal were analyzed for their activity towards acetylcholinesterase (AChE) enzyme and their antioxidant activity. Of these, Melissa officinalis, Paronychia argentea, Sanguisorba minor, Hypericum undulatum and Malva silvestris are used in herbal medicine, Laurus nobilis and Mentha suaveolens as condiments, and Salvia officinalis, Lavandula angustifolia and Lavandula pedunculata also as aromatics. Melissa officinalis and Mentha suaveolens showed AChE inhibitory capacity higher then 50% in the essential oil fraction. Laurus nobilis, Hypericum undulatum, and Sanguisorba minor showed a high inhibition value of AChE in the ethanolic fraction, 64% (1 mg ml(-1)) 68% (0.5 mg ml(-1)), and 78% (1 mg ml(-1)), respectively. Higher values of AChE inhibitory activity were found using decoctions of Lavandula pedunculata, Mentha suaveolens and Hypericum undulatum, 68, 69 and 82% (at a concentration of 5mg dry plant ml(-1) of assay), respectively. The free radical scavenger activity was higher for the polar extracts. In the water extracts most of the plants showed values around 90%. When antioxidant activity was measured with the beta-carotene-linoleic acid assay high activity (65-95%) was also found in the water extracts. Hypericum undulatum, Melissa officinalis and Laurus nobilis showed both high AChE inhibitory capacity and antioxidant activity.