穿心莲内酯对胃癌AGS细胞增殖侵袭的影响

目的观察穿心莲内酯（AD）对胃癌细胞增殖侵袭以及Na＋-K＋-ATP酶活性的影响。方法体外培养胃癌细胞系AGS,分别用1.0、3.0、5.0μmol/L穿心莲内酯作用24～72 h,无机磷法检测AGS细胞Na＋-K＋-ATP酶活性改变情况;MTT和ELISA分析AGS细胞的增殖与断裂DNA含量;同时采用ELISA检测血管内皮生长因子（VEGF）和转化生长因子β1（TGF-β1）的水平;荧光共振能量转移法检测基质金属蛋白酶9（MMP-9）的活性;小室侵袭实验检测细胞侵袭。结果 1.0～5.0μmol/L穿心莲内酯能显著降低Na＋-K＋-ATP酶活性,并能在此浓度下抑制AGS细胞生长增殖以及增加断裂DNA水平。同时,穿心莲内酯也能减少VEGF和TGF-β1的水平（P〈0.05）,降低MMP-9酶的活性,并能有效减少癌细胞的侵袭（P〈0.05）。结论穿心莲内酯是一种有效的抗胃癌药物,它可能具有阻碍胃癌细胞侵袭的能力。     

穿心莲内酯对血管性痴呆大鼠认知功能及海马突触可塑性的影响

目的探讨穿心莲内酯(andrographolide,ANDRO)对血管性痴呆(vascular dementia,VD)大鼠认知功能及海马突触可塑性的影响。方法 2012年6—8月将30只SD大鼠随机分为治疗组(10只)、模型组(10只)、假手术组(10只)。通过阻断大脑中动脉2 h制做VD大鼠模型,治疗组大鼠给予ANDRO(200 mg/kg)灌胃治疗,模型组及假手术组大鼠给予2 ml生理盐水灌胃。用Morris’s水迷宫评估大鼠认知功能,免疫印迹法检测大鼠海马突触素表达。计量资料按完全随机成组设计资料进行方差分析,组间比较采用单因素方差分析,多个样本均数两两比较采用q检验。P0.05为差异有统计学意义。结果连续4 d水迷宫潜伏期模型组[(103.87±5.22)、(88.27±5.37)、(73.95±5.46)、(67.26±5.01)s]均长于治疗组及假手术组大鼠(均P0.05),治疗组[(97.08±4.01)、(79.27±4.66)、(66.62±5.44)、(58.30±6.40)s]均长于假手术组(均P0.05)。假手术组、治疗组、模型组海马突触素灰度值比率分别为0.89±0.01、0.83±0.02、0.79±0.01,比较差异有统计学意义(F=123.27,P0.05)。结论 ANDRO改善VD大鼠认知功能可能与保护突触可塑性有关。     

穿心莲内酯对小鼠腹泻模型的治疗作用研究

目的 研究穿心莲内酯对番泻叶和蓖麻油所致小鼠腹泻模型的治疗作用.方法 以墨汁推进率为指标,观察穿心莲内酯对小鼠小肠推进性运动的影响;分别采用番泻叶和蓖麻油建立小鼠腹泻模型,观察穿心莲内酯给药组小鼠的一般状态及行为学改变,测定稀便率及腹泻指数,并计算单位长度肠质量,评价穿心莲内酯的抗腹泻作用.结果 穿心莲内酯可减缓小鼠小...     

Amelioratory effect of Andrographis paniculata Nees on liver, kidney, heart, lung and spleen during nicotine induced oxidative stress

The ameliorative properties of bioactive compound andrographolide (ANDRO), aqueous extract of Andrographis paniculata (AE-AP) and vitamin E (vit.E) were tested against nicotine induced liver, kidney, heart, lung and spleen toxicity. A group of male Wistar rats were intraperitoneally administered vehicle, nicotine (1 mg/kg body weight/day), nicotine + ANDRO (250 mg/kg body weight/day), nicotine + AE-AP (250 mg/kg body weight/day) and nicotine + vit.E (50 mg/kg body weight/day) for the period of 7 days. The significantly increased levels of lipid peroxidation, protein oxidation and the decreased antioxidant enzyme status were noted in nicotine treated group as compared to vehicle treated group. ANDRO, AE-AP and vit.E significantly reduced the lipid peroxidation, protein oxidation and increased the antioxidant enzyme status. This indicates A. paniculata and vit.E may act as putative protective agent against nicotine induced tissue injury and may pave a new path to develop suitable drug therapy.     

用化学发光法研究家兔穿心莲内酯的药物动力学参数

穿心莲内酯是穿心莲的主要有效成分之一，为了解穿心莲内酯药动学与药效学的关系，本文采用高灵敏的有机偶合化学发光法对穿心莲内酯的血药浓度进行监测，求出系列药动学参数。实验表明，穿心莲内酯在动物体内达峰快，消除半衰期长，生物利用度高。它的几个主要药动学参数为：Ｋａ＝１．３４３ｈ－１±０．０８，Ｋ１２＝０．３３６ｈ－１±０．０１，Ｋ２１＝０．６３３ｈ－１ｈ±０．０６，Ｔ１／２（α）＝０．６９２ｈ±０．０７，ｔ１／２（β）＝１２．１２ｈ±１．９，ＡＵＣ＝５０１．０９μｇ．ｈ／ｍＬ±９．８。     

Simultaneous estimation of andrographolide and wedelolactone in herbal formulations

Andrographolide and wedelolactone are active components of Andrographis paniculata and Eclipta alba, respectively. The extracts of these plants are used in many traditional hepatoprotective formulations. An attempt has been made to develop an accurate, precise and specific HPTLC method to quantify simultaneously both these chemical markers of diversified chemical structures in different dosage forms like tablet and syrup. Precoated silica 60F(254) plates with toluene:acetone:formic acid (9:6:1) as mobile phase and detection wavelength of 254 nm were used. The method was validated in terms of linearity, accuracy, precision and specificity. The calibration curve was found to be linear between 200 to 400 ng/spot for andrographolide and 100 to 200 ng/spot for wedelolactone. The limit of detection and the limit of quantification for andrographolide were 26.16 and 79.28 ng/spot, respectively and for wedelolactone 5.06 and 15.32 ng/spot, respectively.     

Andrographolide downregulates the v-Src and Bcr-Abl oncoproteins and induces Hsp90 cleavage in the ROS-dependent suppression of cancer malignancy

Andrographolide is a diterpenoid compound isolated from Andrographis paniculata that exhibits anticancer activity. We previously reported that andrographolide suppressed v-Src-mediated cellular transformation by promoting the degradation of Src. In the present study, we demonstrated the involvement of Hsp90 in the andrographolide-mediated inhibition of Src oncogenic activity. Using a proteomics approach, a cleavage fragment of Hsp90α was identified in andrographolide-treated cells. The concentration- and time-dependent induction of Hsp90 cleavage that accompanied the reduction in Src was validated in RK3E cells transformed with either v-Src or a human truncated c-Src variant and treated with andrographolide. In cancer cells, the induction of Hsp90 cleavage by andrographolide and its structural derivatives correlated well with decreased Src levels, the suppression of transformation, and the induction of apoptosis. Moreover, the andrographolide-induced Hsp90 cleavage, Src degradation, inhibition of transformation, and induction of apoptosis were abolished by a ROS inhibitor, N-acetyl-cysteine. Notably, Hsp90 cleavage, decreased levels of Bcr-Abl (another known Hsp90 client protein), and the induction of apoptosis were also observed in human K562 leukemia cells treated with andrographolide or its active derivatives. Together, we demonstrated a novel mechanism by which andrographolide suppressed cancer malignancy that involved inhibiting Hsp90 function and reducing the levels of Hsp90 client proteins. Our results broaden the molecular basis of andrographolide-mediated anticancer activity.     

穿心莲内酯干预异丙肾诱导的心力衰竭小鼠的效应及其机制研究

[目的]评价穿心莲内酯干预过量异丙肾上腺素(ISO)致心力衰竭小鼠的药效,运用网络药理学的方法预测其作用靶点并验证。[方法]制备过量盐酸异丙肾上腺素诱导的心力衰竭小鼠模型,随机分为空白组、模型组、穿心莲内酯组、地高辛组。通过心脏超声、形态学与病理分析,评价各组小鼠心功能。采用生物信息学分析工具(BATMAN-TCM)预测药物靶点,运用实时荧光定量PCR法检测候选靶点m RNA水平。[结果]与空白组比较,模型组小鼠射血分数(EF)、短轴缩短率(FS)和舒张早期二尖瓣血流速度与舒张晚期二尖瓣血流速度比值(E/A)显著降低(P0.05),左室收缩末内径(LVIDs)显著增大(P0.05),心肌细胞肥大,伴有血窦扩张和结缔组织增生,心肌组织羟甲基戊二酸单酰辅酶A还原酶(HMGCR,HMG-Co A还原酶)基因表达显著上调(P0.05)。与模型组相比,穿心莲内酯组小鼠EF、FS和E/A显著升高(P0.05),LVIDs显著降低(P0.01),心肌细胞肥大减轻,心肌组织HMGCR基因表达显著下调(P0.05)。[结论]穿心莲内酯可以改善过量异丙肾上腺素诱导的心力衰竭,其机制可能与抑制HMG-Co A还原酶、调节胆固醇合成有关。     

穿心莲内酯磺化物雾化治疗支气管哮喘急性发作期的护理干预

目的探讨穿心莲内酯磺化物雾化治疗支气管哮喘急性发作期及其护理干预的临床效果。方法 120例支气管哮喘急性发作期患者随机分为干预组和对照组各60例,治疗7天后观察比较两组的临床疗效、血气指标、第1秒用力呼气容积（FEV1）占预计值（%）和最大呼气流量（PEF）个人最佳值（%）。结果干预组与对照组比较,干预组患者的临床疗效明显优于对照组,差异有显着性（P〈0.05）。治疗后血气分析各指标及FEV1占预计值（%）和PEF个人最佳值（%）比较,干预组比对照组均有明显差异（P〈0.05）。结论通过采取一系列的精心、有针对性的护理干预措施后,穿心莲内酯磺化物雾化吸入治疗支气管哮喘急性发作期疗效好,值得临床推广和应用。     

炎琥宁治疗重症病毒性上呼吸道感染的疗效观察

目的观察炎琥宁粉针剂治疗重症病毒性上呼吸道感染的安全性和有效性。方法将195例重症病毒性上呼吸道感染患者随机分为两组,对照组给予常规利巴韦林抗病毒、布洛芬解热镇痛、补液等对症支持治疗;治疗组在上述治疗基础上加用炎琥宁粉针剂200mg稀释后静脉滴注,1次/d。结果 72h后治疗组与对照组比较,治愈率有显著性差异（P〈0.01）,总有效率有显著性差异（P〈0.01）。结论炎琥宁粉针剂治疗重症病毒性上呼吸道感染使用方便,毒副作用小,是安全有效的治疗重症病毒性上呼吸道感染药物。