Flavonoid-rich fraction of Maytenus ilicifolia Mart. ex. Reiss protects the gastric mucosa of rodents through inhibition of both H+,K+ -ATPase activity and formation of nitric oxide

Maytenus ilicifolia Mart. ex. Reissek (Celastraceae), a medicinal plant known in Brazil as "espinheira-santa" is commonly used to treat gastric disorders. The effect of the flavonoid-rich fraction separated from the leaves was evaluated for its gastroprotective properties and the mechanism(s) involved in this activity. Intraperitoneal administration of the flavonoid-rich fraction potently protected rats from experimentally induced chronic (ED(50)=79 mg/kg) and acute gastric lesions by ethanol (ED(50)=25mg/kg) and indomethacin (ED(50)=4 mg/kg) without altering the decreased amount of cytoprotective glutathione and mucus amount in the injured gastric mucosa. A potent reduction of gastric acid hypersecretion (ED(50)=7 mg/kg, i.p.) was accompanied by a reduction of nitric oxide release (ED(50)=1.6 mg/kg, i.p.) in the gastric secretion of 2h pylorus ligated rats which suggests an important role for nitric oxide-dependent mechanisms. Inhibition of gastric acid secretion in vivo was correlated with the in vitro inhibition of rabbit gastric H(+),K(+)-ATPase activity (IC(50)=41 microg/mL). Chemical investigation of the fraction showed galactitol (25%), epicatechin (3.1%) and catechin (2%) as the majoritary components. Collectively, the results show that the flavonoid-rich fraction of Maytenus ilicifolia potently protects animals from gastric lesions with high potency through inhibition of gastric acid secretion.     

旋覆代赭汤对RE模型大鼠食管黏膜Na+-K+-ATP酶及 Ca2+-Mg2+-ATP酶的影响

目的: 观察旋覆代赭汤对反流性食管炎(RE)模型大鼠食管黏膜组织Na⁺-K⁺-ATP酶及Ca²⁺-Mg²⁺-ATP酶活性的影响,探讨RE食管黏膜细胞能量代谢障碍与黏膜损伤的关系以及旋覆代赭汤治疗RE的作用机制。方法: 将96只雄性Wistar大鼠随机分成6组,即假手术组、模型组、旋覆代赭汤组高、中、低剂量组(24,12,6 g·kg^-1)及西药对照组(奥美拉唑10 mg·kg^-1+2 mg·kg^-1莫沙必利),每组16只。采用"食管-十二指肠端侧吻合术"制备胃及十二指肠液混合RE模型。从术后第3天开始,假手术组、模型组给予生理盐水灌胃,药物治疗组分别给予旋覆代赭汤高、中、低剂量、西药(奥美拉唑10 mg·kg^-1+莫沙必利2 mg·kg^-1)灌胃,连续7天,记录大鼠体重变化及死亡情况,于第8天处死大鼠留取标本,观察食管下段黏膜大体及病理组织学变化;化学法检测食管黏膜组织Na⁺-K⁺-ATP和Ca²⁺-Mg²⁺-ATP酶活性。结果: 与假手术组比,模型组大鼠体重明显减轻(P<0.05),食管黏膜肉眼及镜下病理改变明显,评分增高(P<0.05);食管黏膜组织Na⁺-K⁺-ATP酶及Ca²⁺-Mg²⁺-ATP酶活性显著降低(P<0.05);与模型组及西药组比,旋覆代赭汤高、中剂量组大鼠死亡率明显降低(P<0.05):与模型组比,旋覆代赭汤高、中剂量组、西药组肉眼及病理评分显著降低(P<0.05);食管黏膜组织Na⁺-K⁺-ATP酶及Ca²⁺-Mg²⁺-ATP酶活性明显提高(P<0.05)。结论: 旋覆代赭汤能明显提高RE大鼠食管黏膜细胞膜Na⁺-K⁺-ATP 酶及Ca²⁺-Mg²⁺-ATP酶活性, 从而保持食管黏膜细胞完整性,减轻黏膜损伤。     

Influence of tetrahydrocurcumin on erythrocyte membrane bound enzymes and antioxidant status in experimental type 2 diabetic rats

Curcuma longa (Zingiberaceae) has been used traditionally as antidiabetic and has been proven scientifically to possess high antioxidant activity and anticancer properties. The active components of Curcuma longa such as curcumin and tetrahydrocurcumin (THC), a major colourless metabolite of curcumin also possesses antidiabetic, antiinflammatory and antioxidant activity. In the present study the effect of THC and curcumin on erythrocyte membrane bound enzymes and antioxidants activity in streptozotocin (STZ) and nicotinamide induced type 2 diabetic model was investigated. Oral administration of THC at 80 mg/kg body weight to diabetic rats for 45 days. The effect of THC and curcumin on glucose, insulin, haemoglobin, glycosylated haemoglobin, thiobarbituric acid reactive substances (TBARS), superoxide dismutase (SOD), catalase (CAT), glutathione peroxide (Gpx), glutathione-S-transferase (GST), reduced glutathione (GSH) and membrane bound enzymes were studied. The effect of THC was compared with curcumin. The levels of blood glucose, glycosylated haemoglobin, erythrocyte TBARS, were increased significantly whereas the level of plasma insulin and haemoglobin, erythrocyte antioxidants (SOD, CAT, GPx, GST and GSH), membrane bound total ATPase, Na(+)/K(+)-ATPase, Ca(2+)-ATPase, Mg(2+)-ATPase were decreased significantly in diabetic rats. Administration of THC and curcumin to diabetic rats showed decreased level of blood glucose, glycosylated haemoglobin and erythrocyte TBARS. In addition the levels of plasma insulin, haemoglobin, erythrocyte antioxidants and the activities of membrane bound enzymes also were increased in THC and curcumin treated diabetic rats. These biochemical observations were supplemented by histopathological examination of pancreas section. The present study indicates that the THC possesses a significant beneficial effect on erythrocyte membrane bound enzymes and antioxidants defense in addition to its antidiabetic effect.     

染料木素抗大鼠心肌肥厚作用及其与ATPase活性的关系

目的:观察染料木素(Gen)对异丙肾上腺素(iso)所致大鼠心肌肥厚的保护作用及其对心肌组织Na+-K+-ATPase,Ca2+-Mg2+-ATPase活性及羟脯氨酸含量的影响。方法:0.2 g·L-1的iso 5 mL·kg-1·d-1,背部皮下注射,连续10 d,建立大鼠心肌肥厚模型。造模第2天开始给予不同浓度的染料木素、二甲基亚砜或NS,连续14 d,末次给药后禁食12 h,称体重,麻醉,取心脏,称全心及左心室质量,计算全心质量指数及左心室质量指数,测定心肌组织Na+-K+-ATPase,Ca2+-Mg2+-ATPase活性及羟脯氨酸(Hyp)含量。结果:模型组全心质量指数及左心室质量指数分别为(3.30±0.24),(2.55±0.14)mg·kg-1,与正常对照组相比显著升高(P<0.001);心肌组织Na+-K+-ATPase和Ca2+-Mg2+-ATPase活力为(1.81±0.25),(1.00±0.22)U·mg-1,与正常对照组相比活性显著降低(P<0.01);Hyp含量为(0.80±0.05)mg·g-1,与正常对照组相比含量显著升高(P<0.001)。与模型组相比,染料木素高、低剂量组(0.3,0.1μmol.kg-1)全心质量指数分别为(2.83±0.22),(2.97±0.19)mg·kg-1;左心室质量指数分别为(2.32±0.16),(2.34±0.13)mg·kg-1均显著降低(P<0.01或P<0.05);高剂量组心肌组织Na+-K+-ATPase(2.58±0.40)U·mg-1及Ca2+-Mg2+-ATPase(1.35±0.22)U·mg-1活性升高(P<0.01或P<0.05),染料木素高、低剂量组心肌组织Hyp含量分别为(0.48±0.11),(0.57±0.14)mg·g-1显著降低(P<0.01或P<0.05)。结论:染料木素可通过提高Na+-K+-ATPase及Ca2+-Mg2+-ATPase的活性,降低Hyp含量,从而抑制心脏纤维化,起抗心肌肥厚作用。     

问荆碱对大鼠脑囊泡膜Mg2+-ATPase,Ca2+-ATPase抑制作用的动力学研究

问荆碱对大鼠脑囊泡膜Mg²⁺-ATPase,Ca²⁺-ATPase有显著的抑制作用,对Mg²⁺-ATPase的抑制机制分别为竞争性抑制(Mg²⁺,Ki=4.93×10^-5mol/L)、非竞争性抑制(ATP,Ki=1.06×10^-4mol/L),对Ca²⁺-ATPase的抑制机制分别为混合型抑制(Ca²⁺,Ki=5.07×10^-5mol/L)、非竞争性抑制(ATP,Ki=3.27×10-4mol/L)。     

旋覆代赭汤及其拆方对RE大鼠血浆Na~+-K~+-ATP酶及Ca~(2+)-Mg~(2+)-ATP酶活性的影响

[目的]探讨反流性食管炎(RE)食管黏膜血浆细胞能量代谢与黏膜损伤的关系以及旋覆代赭汤治疗RE的作用机制。[方法]将120只Wistar大鼠按照随机数字法随机分为10组,每组12只,即正常组、模型组、旋覆代赭汤全方组(全方组)、苦降组、甘升组、升降相因组、去苦降组、去甘升组、去升降相因组和西药组;除正常组外,其余9组行"4.2 mm幽门夹+胃底2/3结扎术"造模。治疗14 d后,即造模后第22天处死,检测各组大鼠血浆Na~+-K~+-ATP酶及Ca~(2+)-Mg~(2+)-ATP酶的活性。[结果]实验后各模型组大鼠ATP酶活性低于正常组;全方组、西药组酶活性较好,与正常组差异无统计学意义(P0.05),与模型组相比有统计学差异(P0.05);苦降组及去甘升组与模型组相比,差异无统计学意义(P0.05),与全方组及西药组比较差异有统计学意义(P0.05);正常组与其他各组比较,均有统计学差异(P0.05);西药组与全方组比较,差异无统计学意义。[结论]旋覆代赭汤全方组能提高模型大鼠血浆Na~+-K~+-ATP酶及Ca~(2+)-Mg~(2+)-ATP酶的活性,改善模型大鼠食管黏膜组织形态学病变,且作用优于各拆方组。     

胶艾汤对血虚模型大鼠补血作用的有效部位筛选

目的比较胶艾汤不同溶剂提取部位对血虚模型大鼠外周血象、免疫器官指数、白细胞介素2(IL-2)和促红细胞生成素(EPO)水平以及红细胞膜能量代谢酶活性的影响,筛选胶艾汤补血作用的有效部位。方法采取每天于眼底静脉丛放血5 mL/kg,连续放血12d的方法,复制大鼠血虚模型;造模同时各组动物分別ig给予胶艾汤及其正丁醉、石油醚、醋酸乙酯、水部位浸膏(剂量均为生药量12g/kg),以复方阿胶浆为阳性对照。造模第12天检测各组大鼠外周血红细胞计数(RBC)、血红蛋白(HGB)、红细胞压积(HCT)、血小板计数(PLT),计算脾脏和胸腺器官指数。检测血清中IL-2和EPO水平,检测全血红细胞膜能量代谢酶Na~+,K~+-ATP及Ca~(2+),Mg~(2+)-ATP酶活性,UPLC法初步分析胶艾汤不同提取部位的化学成分差异。结果与对照组比较,模型组大鼠RBC、HGB、HCT、PLT、胸腺指数以及IL-2水平明显降低,Na~+,K~+-ATP酶和Ca~(2+),Mg~(2+)-ATP酶活性明显减弱,脾脏指数及EPO水平明显升高,表明血虚模型复制成功。与模型组比较,胶艾汤正丁醇组可明显升高HCT、RBC、HGB、PLT(P0.05、0.01);降低脾脏指数及EPO水平(P0.05、0.01);明显升高胸腺指数、IL-2水平(P0.01),升高红细胞膜Ca~(2+),Mg~(2+)-ATP酶及Na~+,K~+-ATP酶活性(P0.05、0.01)。石油醚组可明显升高PLT及IL-2水平(P0.01),降低EPO水平及脾脏指数(P0.05、0.01)。醋酸乙酯组可明显降低脾脏指数及EPO水平(P0.01),升高红细胞膜Ca~(2+),Mg~(2+)-ATP酶活性(P0.05)。水部位组可明显升高PLT(P0.05),降低EPO水平(P0.01)。胶艾汤正丁醇提取部位中检测到其他提取部位不含有的咖啡酸、苯甲酰芍药苷、甘草酸铵,且正丁醇提取部位中没食子酸、原儿茶酸、磷酸川芎嗪、绿原酸的量均高于胶艾汤醋酸乙酯和水提取部位。结论正丁醇部位是胶艾汤补血作用的最强有效部位。     

木犀草素对缺血再灌损伤神经元的保护作用及机制研究

目的:探讨黄酮类化合物木犀草素对缺血/再灌损伤神经元的作用以及可能的作用机制。方法:原代培养的海马神经元经2 h的氧糖剥夺和24 h的再灌处理,分别检测细胞活性,乳酸脱氢酶漏出率和细胞凋亡率,采用Pu lsinelli四动脉阻断法对SD大鼠施行10 m in全脑缺血和24 h再灌,检测钠泵活性。结果:经氧糖剥夺/再灌后,海马神经元的活性比未经氧糖剥夺/再灌组显著地降低,乳酸脱氢酶漏出率和细胞凋亡率均显著地增高。在氧糖剥夺期间给予的木犀草素,在10~100μmol.L-1能呈剂量依赖地逆转这些改变。进一步实验发现木犀草素能够显著地增强大鼠全脑缺血/再灌后的钠泵活性。在神经元氧糖剥夺/再灌模型上,利用钠泵抑制剂哇巴因能阻断木犀草素的神经元保护作用。结论:木犀草素能减轻缺血/再灌所致的神经元损伤,其保护机制可能与增强了神经元细胞膜上的钠泵活性有关。     

The anti-ulcer activities of bisabolangelone from Angelica polymorpha

Aim of the study

Evaluate the anti-ulcer effects of bisabolangelone from Angelica polymorpha Maxim and provide the basic data to further study for the Angelica polymorpha and bisabolangelone.

Materials and methods

Bisabolangelone was isolated from Angelica polymorpha Maxim collected from Shennongjia Forest District of China. The structure of bisabolangelone was elucidated by NMR and MS spectrums. The anti-ulcer effects were evaluated with length of lesion (mm) and activity of H⁺/K⁺-ATPase in two models induced by ethanol and Pylorus ligation. Experimental groups were administered with different doses of bisabolangelone (3.8, 7.6 and 15.3 mg/kg). The positive control group was administered omeprazole with a dose of 3.3 mg/kg.

Results

Bisabolangelone significantly reduced the length of lesion (3.8, 7.6 and 15.3 mg/kg, P < 0.01), inhibited the activity of H⁺/K⁺-ATPase (3.8, 7.6 and 15.3 mg/kg, P < 0.01), decreased the volume of gastric juice (7.6 and 15.3 mg/kg, P < 0.05), and increased the pH value of gastric juice (7.6 and 15.3 mg/kg, P < 0.01, 3.8 mg/kg, P < 0.05).

Conclusions

Bisabolangelone is the main anti-ulcer active compound of Angelica polymorpha, and remarkably preventive and therapeutic action on gastric ulcer. It is possible that bisabolangelone inhibited the activity of the H⁺/K⁺-ATPase, then reducing the secretion of H⁺, and the anti-ulcer mechanism of bisabolangelone was deserved to be further studied.     

Inhibition of the gastric H+,K+ -ATPase by plectrinone A, a diterpenoid isolated from Plectranthus barbatus Andrews

This work assessed the mechanism underlying the antisecretory gastric acid effect of Plectranthus barbatus Andrews (Lamiaceae) and active constituents. Popularly known as "false-boldo", this plant is used in Brazilian folk medicine to treat gastrointestinal and hepatic ailments. The plant aqueous extract (AE) and isolated compounds were assayed in vivo in pylorus-ligated mice, and in vitro on acid secretion measured as [(14)C]-aminopyrine ([(14)C]-AP) accumulation in rabbit gastric glands and gastric H(+),K(+)-ATPase preparations. Injected into the duodenal lumen, the AE of the plant leaves (0.5 and 1.0 g/kg) decreased the volume (62 and 76%) and total acidity (23 and 50%) of gastric acid secretion in pylorus-ligated mice. Bioguided purification of the AE yielded an active fraction (IC(50)=24 microg/ml) that inhibited acid secretion in rabbit gastric glands with a potency 10 to 18 times greater than that of the originating extract, on both the basal and stimulated acid secretion by histamine (His) (1 microM) or bethanechol (100 microM). At the same concentrations the gastric H(+),K(+)-ATPase activity was also inhibited. The active constituent was chemically identified as the abietanoid dienedione plectrinone A which reduced the H(+),K(+)-ATPase activity with IC(50)=171 microM. The results indicate that inhibition of the gastric proton pump by this diterpenoid may account for the antisecretory acid effect and reputed anti ulcer activity of Plectranthus barbatus.     

炙甘草汤对哇巴因所致心肌细胞触发活动及Na+,K+-ATP酶活性的影响

目的探索炙甘草汤对哇巴因所致心肌细胞触发活动的影响及作用机理.方法应用微电极技术及单相动作电位技术观察炙甘草汤对哇巴因所致触发性离体及在体心肌触发活动的影响,并运用Na+,K+-ATP酶活性测定试剂盒测定心肌细胞的Na+,K+-ATP酶活性. 结果(1)哇巴因( 0.5×10-6 mmol·mL-1)高钙台氏液灌流可引起豚鼠离体左心室乳头肌触发活动,炙甘草汤(3、6、12mg·mL-1)明显降低触发活动的幅度、时程和发生率,高浓度时完全抑制触发活动的发生.(2)哇巴因(4×1 0-5 mmol·kg-1, iv)可引起豚鼠在体心肌触发活动.炙甘草汤(10、20、3 0g生药/kg,ig)明显延迟触发活动的发生,降低触发活动的幅度和发生率,并提高触发性心肌细胞Na+,K+-ATP酶活性. 结论炙甘草汤抑制哇巴因所致触发活动的发生可能是通过提高Na+,K+-ATP酶活性而实现的.     

参芦、根总皂甙对小鼠不同脏器组织ATP酶活性的影响

参芦和根中的总皂甙对正常小鼠心、肝、脑、肾和脾组织匀浆中的Mg²⁺-ATP酶均有抑制作用,对Na⁺-K⁺-ATP酶却有激活作用,尤以参芦总皂甙的作用更为显著。证明它们对不同组织的能量代谢均有一定的影响。     

龙葵总碱对肿瘤细胞膜钠泵及钙泵活性影响的研究

目的：观察龙葵总碱对S180小鼠及H22小鼠肿瘤细胞膜Na^＋，K^＋-ATPase及Ca^＋＋，Mg^＋＋-ATPase活性的影响。方法：荷瘤小鼠分为治疗组（高剂量、中剂量、低剂量）和对照组（生理盐水组、环磷酰胺组），分别测定各组肿瘤细胞膜的Na^＋，K^＋ ATPase及Ca^＋＋，Mg^＋＋ -ATPase活性。结果：龙葵总碱对S180小鼠及H22小鼠肿瘤细胞膜Na^＋，K^＋ -ATPase及Ca^＋＋，Mg^＋＋ -ATPase活性均有明显的抑制作用，并且其抑制作用呈量效正相关。结论：龙葵总碱这一作用可能是其抗肿瘤作用机理之一。关键词：龙葵总碱肿瘤细胞膜钠泵钙泵     

侯氏黑散对大鼠大脑中动脉闭塞模型缺血脑组织Na+-K+-ATP酶及一氧化氮合酶活性的影响

目的:观察侯氏黑散对大脑中动脉闭塞模型大鼠缺血脑组织Na+-K+-ATP酶、一氧化氮合酶(NOS)活性以及诱导型一氧化氮合酶(iNOS)的影响。方法:采用线栓法复制大鼠大脑中动脉闭塞模型,利用比色法观察侯氏黑散对大鼠缺血脑组织Na+-K+-ATP酶、NOS、iNOS活性的影响。结果:与模型组比较,侯氏黑散组大,中剂量组缺血脑组织Na+-K+-ATP酶活性显著提高(P&lt;0.05)。侯氏黑散大,中,小剂量组NOS、iNOS的活性明显降低(P&lt;0.05)。结论:侯氏黑散可能是通过提高脑组织Na+-K+-ATP酶活性和降低NOS、iNOS的活性保护和修复缺血性脑损伤。     

青蒿总香豆素解热作用及其机理初步研究

目的:研究青蒿总香豆素解热(降温)作用并探讨其作用机理。方法:从黄花蒿中提取总香豆素,利用内生致热原性家兔发热模型,观察青蒿总香豆素对发热家兔体温的影响并测定脑脊液、血清中前列腺素E₂(PGE₂)、环单磷酸腺苷(cAMP)水平以及肝脏、腓肠肌钠泵活性。结果:青蒿总香豆素可以显著降低正常及发热家兔体温,抑制肝脏、腓肠肌组织钠泵活性,降低发热家兔血液及脑脊液PGE₂水平,对血液及脑脊液cAMP水平变化无明显影响。结论:香豆素成分可能是青蒿解热降温的有效部位,其作用机制与抑制钠泵活性及降低中枢PGE₂水平有关。     

Anti-secretory,anti-inflammatory and anti-Helicobacter pylori activities of several fractions isolated from Piper carpunya Ruiz & Pav.

Ethnopharmacological relevance

The leaves of Piper carpunya Ruiz & Pav. (syn Piper lenticellosum C.D.C.) (Piperaceae), are widely used in folk medicine in tropical and subtropical countries of South America as an anti-inflammatory, anti-ulcer, anti-diarrheal and anti-parasitical remedy as well as an ailment for skin irritations.

Aims of the study

To study the anti-inflammatory, anti-secretory and anti-Helicobacter pylori activities of different fractions isolated from an ethanolic extract of the leaves of Piper carpunya, in order to provide evidence for the use of this plant as an anti-ulcer remedy. Moreover, to isolate the main compounds of the extract and relate their biological activity to the experimental results obtained with the fractions.

Materials and methods

Sixteen fractions were obtained from the ethanolic extract (F I–XVI) and 16 pure compounds were isolated and identified from these fractions. We studied the effects of the fractions (0.1–400 μg/mL) on the release of myeloperoxidase (MPO) enzyme from rat peritoneal leukocytes, on rabbit gastric microsomal H⁺, K⁺-ATPase activity and anti-Helicobacter pylori anti-microbial activity using the microdilution method (MM). The main compounds contained in the fractions were isolated and identified by ¹H- and ¹³C NMR spectra analysis and comparison with the literature data.

Results

Eight fractions showed inhibition of MPO enzyme (F I–IV, X, XII, XIV and XV). The highest inhibition was observed with F XIV (50 μg/mL, 60.9%, p < 0.001). F X and XII were the most active ones, inhibiting the gastric H⁺, K⁺-ATPase activity with IC₅₀ values equal to 22.3 μg/mL and 28.1 μg/mL, respectively. All fractions, except F XV, presented detectable anti-Helicobacter pylori activity, with a diameter of inhibition zones ranging from 11 mm up to 50 mm. The best anti-Helicobacter pylori activity was obtained with F III and V. Both fractions killed Helicobacter pylori with lowest concentration values, about 6.25 μg/mL. Sixteen pure compounds were isolated, five of them are flavonoids that possess strong anti-oxidant and free radical scavenging activity, e.g. vitexin, isovitexin, and rhamnopyranosylvitexin. Terpenoids like sitosterol, stigmasterol and phytol, which have shown gastroprotective activity, and dihydrochalcones, like asebogenin, with anti-bacterial activity, were also isolated. Furthermore, the rare neolignan 1, that is a DNA polymerase β lyase inhibitor, and (6S, 9S)-roseoside, that shows strong anti-bacterial activity, were isolated, for the first time, from the genus Piper.

Conclusions

We suggest that the flavonoids isolated from F I and II (vitexin, isovitexin, rhamnopyranosylvitexin and isoembigenin) contribute to the anti-MPO activity, as well as to their anti-Helicobacter pylori activity. These flavonoids may also be responsible for the important inhibition of H⁺, K⁺-ATPase activity. Also the phytosterols and phytol obtained from F XIV and XV could be involved in these gastroprotective activities. These results encourage us to continue phytochemical studies on these fractions in order to obtain full scientific validation for this species.     

玉郎伞黄酮对心肌缺血再灌注损伤心肌组织ATP酶和凋亡蛋白的影响

目的 :研究玉郎伞黄酮(FYLS)对大鼠离体心肌缺血再灌注损伤(I/R)心肌组织Na⁺-K⁺-ATP酶、Ca²⁺-ATP酶和凋亡蛋白的影响。 方法 :离体大鼠心脏采用Langendorff法灌流,停灌30 min再灌30 min造成I/R模型。测定心肌组织Na⁺-K⁺-ATP酶、Ca²⁺-ATP酶活性。同时观察药物对缺血再灌注后心肌组织病理形态、凋亡相关蛋白Bcl-2,Bax表达的影响。 结果 :FYLS高剂量(8×10^-3g ·L^-1)可显著改善缺血-再灌注所致的心功能损伤,增加Na⁺-K⁺-ATP酶、Ca²⁺-ATP酶的活性;与模型组比较,FYLS高剂量组病理结果显示心肌组织受损程度明显减轻(P<0.05),且明显降低心肌Bax蛋白表达(P<0.01),对Bcl-2蛋白表达无明显影响,但能显著增加Bcl-2/Bax的比率(P<0.05)。 结论 :FYLS对I/R具有保护作用,其机制可能与减轻钙超载、下调Bax蛋白表达、增加Bcl-2/Bax的比率有关。     

In vivo inhibition of gastric acid secretion by the aqueous extract of Scoparia dulcis L. in rodents

The freeze-dried aqueous extract (AE) from the aerial parts of Scoparia dulcis was tested for its effects on experimental gastric hypersecretion and ulcer in rodents. Administration of AE to animals with 4h pylorus ligature potently reduced the gastric secretion with ED(50)s of 195 mg/kg (rats) and 306 mg/kg (mice). The AE also inhibited the histamine- or bethanechol-stimulated gastric secretion in pylorus-ligated mice with similar potency suggesting inhibition of the proton pump. Bio-guided purification of the AE yielded a flavonoid-rich fraction (BuF), with a specific activity 4-8 times higher than the AE in the pylorus ligature model. BuF also inhibited the hydrolysis of ATP by H(+),K(+)-ATPase with an IC(50) of 500 microg/ml, indicating that the inhibition of gastric acid secretion of Scoparia dulcis is related to the inhibition of the proton pump. Furthermore, the AE inhibited the establishment of acute gastric lesions induced in rats by indomethacin (ED(50)=313 mg/kg, p.o.) and ethanol (ED(50)=490 mg/kg, p.o.). No influence of the AE on gastrointestinal transit allowed discarding a possible CNS or a cholinergic interaction in the inhibition of gastric secretion by the AE. Collectively, the present data pharmacologically validates the popular use of Scoparia dulcis in gastric disturbances.     

青蒿总香豆素抗热应激作用及其机理的研究

目的:研究青蒿抗热应激作用及其机理。方法:利用高温高湿环境造成家兔热应激模型,观察青蒿总香豆素对家兔肛温上升及血液、肺组织磷脂酶A₂活性和循环内皮细胞数目的变化,并测定其对脑、心脏、肾组织钠泵活性及小鼠抗脑缺氧能力的影响。结果:青蒿总香豆素可明显降低热应激家兔体温上升速度,并伴随血清、肺组织磷脂酶A₂活性降低,循环内皮细胞减少,显著抑制脑、心、肾组织钠泵活性,延长断头小鼠张口喘气时间几近1倍。结论:香豆素部位可能是青蒿祛暑功效的活性成分群之一。     

外源Ca~(2+)及NO供体硝普钠(SNP)对盐胁迫下紫苏种子萌发及幼苗抗氧化酶活性的影响

目的:通过对紫苏种子萌发及幼苗生理特性的研究,寻找提高紫苏种子及幼苗在盐胁迫条件下抗性能力的途径。方法:测定在外源Ca2+及NO供体硝普钠(SNP)处理后,NaCl胁迫下紫苏种子的发芽势(Gv)、发芽率(Gr)、发芽指数(Gi)和活力指数(Vi),并对紫苏幼苗总生物量以及叶片的丙二醛(MDA)含量、超氧化物歧化酶(SOD)、过氧化物酶(POD)和过氧化氢酶(CAT)活性进行测定。结果:100 mmol.L-1的NaCl胁迫下的紫苏种子萌发受到显著抑制,但是经过Ca2+和SNP处理后,萌发指标均有升高。外施10 mmol.L-1的Ca2+或0.1 mmol.L-1的SNP都能够有效的缓解NaCl对紫苏种子及幼苗造成的胁迫伤害,经过SNP,Ca2+的复合处理后,效果最为显著,各项指标均达到最大值,发芽势为65.1%,发芽率为89.3%,发芽指数为13.9,活力指数为为0.110 9。复合处理提高了幼苗的总生物量,降低了叶片的MDA含量,显著的提高了SOD,POD,CAT的活性,其结果分别达到0.84,5.71,4.92 U.mg-1,但是乙二醇双(2-氨基乙醚)四乙酸(EGTA)却显著的抑制了SNP对盐害的缓解作用。结论:10 mmol.L-1的Ca2+和0.1 mmol.L-1的SNP的复合处理能够有效的减缓NaCl胁迫对紫苏种子及幼苗产生的伤害,提高了种子及幼苗的抗盐能力。NO可能通过激活紫苏细胞质膜Ca2+通道促进Ca2+的吸收,改变胞内Ca2+浓度来发挥其对NaCl胁迫伤害的缓解作用。