Effects of Platycodin D on S100A8/A9-induced inflammatory response in murine mammary carcinoma 4T1 cells

Activation of the inflammatory signaling pathway is the most vital part of the pre-metastatic events of breast cancer. Platycodin D (PlaD) shows favorable pharmacological activities in anti-inflammatory and anti-tumor effect. The main purpose of this study was to survey the effects of PlaD on S100A8/A9-induced inflammation in mouse mammary carcinoma 4T1 cells. S100A8/A9 immunolocalization and expression in pre-metastatic lung tissue were assessed by immunofluorescence staining and ELISA. 4T1 cells were treated with 2.5 μg/mL recombinant S100A8/A9 heterodimer and 7.5, 10, or 12.5 μM of PlaD. After 24 h of incubation, cell viability, migration, and invasion were evaluated by CCK-8, wound-healing, and transwell assay, respectively. Nuclear translocation of NF-κB p65 was determined by immunostaining and western blot. The levels of pro-inflammatory cytokines including IL-1β, IL-6, and TNF-α were detected by ELISA. The results showed that S100A8/A9 was actively increased and released into the extracellular space during the pre-metastatic phase of breast cancer. PlaD treatment attenuated S100A8/A9-induced growth, migration, and invasion of 4T1 cells. Furthermore, PlaD decreased the levels of IL-1β, IL-6, and TNF-α by inhibiting nuclear translocation of NF-κB p65. In conclusion, this study demonstrated that PlaD inhibited S100A8/A9-induced inflammatory response in 4T1 cells by suppressing the expression of IL-6, IL-1β, and TNF-α via inhibition of NF-κB signaling pathways.     

醋炙降低芫花二氯甲烷部位对大鼠肝肾细胞毒性的分析

目的:比较醋炙前后芫花二氯甲烷提取物对于大鼠正常肝细胞BRL及大鼠正常肾细胞NRK的细胞毒性变化。方法:选择BRL及NRK细胞为研究对象,采用噻唑蓝(MTT)比色法评价生、醋芫花二氯甲烷部位对BRL与NRK活性的影响;测定NRK细胞中尿素氮(BUN),乳酸脱氢酶(LDH),谷胱甘肽(GSH)的含量,以及BRL细胞中丙氨酸氨基转移酶(ALT),天门冬氨酸氨基转移酶(AST),碱性磷酸酶(ALP),LDH,GSH的含量,用于评价生、醋芫花二氯甲烷部位对BRL和NRK的氧化损伤作用。结果:与空白组相比,生芫花二氯甲烷部位对NRK和BRL细胞具有显著毒性,显著提高NRK细胞中BUN和LDH的含量(P 0. 05,P 0. 01);显著提高BRL细胞中AST,ALT,ALP和LDH的含量(P 0. 05,P 0. 01);降低NRK和BRL细胞中的GSH含量。与生芫花二氯甲烷部位相应剂量组相比,醋芫花二氯甲烷部位相应剂量组能提高NRK和BRL的细胞活性,降低NRK细胞中BUN和LDH的含量,降低BRL细胞中ALT,AST,ALP和LDH的含量;提高NRK和BRL细胞中GSH的含量。结论:醋炙可降低芫花二氯甲烷部位对大鼠肝肾细胞的毒性,提高大鼠肝肾细胞功能与抗氧化能力。     

ICP-OES/ICP-MS技术研究枯矾及其伪品的差异特征元素及无机元素含量分布

目的:分析临床用枯矾及其伪品铵明矾炮制品的差异无机元素,并建立其特征图谱,为枯矾提供新的质量控制手段。方法:应用ICP-OES及ICP-MS测定枯矾和铵明矾炮制品中22种无机元素的含量,采用SPSS 16. 0软件对原始数据进行分层聚类分析,以SIMCA-P 13. 0软件配合t检验及秩和检验对差异性无机元素进行识别,建立枯矾与伪品的无机元素特征谱。结果:枯矾中主含K,Al等元素,伪品主含Al,Fe等元素;枯矾Cr,Sr,Mn含量相对较高,铵明矾炮制品Mn,Ti,Ga含量相对较高。其中枯矾中K元素含量约为伪品的205倍;相反,Fe,Ti,Mn,Ga等元素,伪品的平均含量远高于枯矾,分别约为枯矾平均含量的33,46,38,27倍。聚类分析将18个样品聚类为枯矾和铵明矾炮制品两大类。共筛选出18种含量具有显著性差异(P 0. 05)的元素,分别为Be,Mg,Al,K,Ti,V,Mn,Fe,Co,Ni,Cu,Ga,As,Sn,Sb,Hg,Tl,Pb。建立了枯矾、伪品枯矾含21种无机元素特征谱。结论:该分析方法可用于枯矾的质量控制。     

矿物类中药止血药理作用及临床应用研究进展

矿物药是我国传统中医药不可缺少的重要组成部分,药用矿物资源的研究与利用已有几千年的历史,是各族人民生存过程中无数次试用、观察、积累的实践医疗经验总结,极具特色。目前,矿物药的治疗范围涉及内科、外科、妇科、儿科、五官科等。矿物药对多种出血病症的临床应用广泛、用药经验丰富且疗效显著,但现代研究文献较少,主要集中在1970—1990年代。本文对近40年来临床具止血作用矿物药的药理作用及临床应用进行综述,以期为临床治疗出血病症合理用药、对矿物类中药资源的进一步开发利用、物质基础及作用机制的深入研究以及更好地挖掘矿物药资源宝库提供参考。通过对主要著作的统计,记载有止血作用的矿物药共27味。矿物类中药止血药理作用研究主要集中在对矿物药的元素分析及相关元素对止血作用的影响,以及相关止血作用的药理实验研究加以证实,但研究尚不深入和全面。矿物类中药止血的临床应用主要包括消化道出血、咯血、鼻衄、牙龈出血、颅脑出血、流产后出血、血崩、子宫出血、血便及外用止血等。     

十枣汤对大鼠的急性毒性

目的:研究十枣汤对大鼠的急性毒性反应情况,为临床用药安全和后续毒理药效实验提供参考。方法:SPF级SD大鼠40只,雌雄各半,随机分为空白组和十枣汤组,每组20只,雌雄各10只。采用最大给药量法,十枣汤组在24 h内以最大给药体积分别连续2次灌胃给予最大浓度十枣汤混悬液0. 3 g·m L-1,空白组给予生理盐水,观察大鼠在14 d内所产生的毒性反应(死亡、中毒症状)及其严重程度、恢复情况等,同时记录各组动物给药前后的体质量变化和进食情况。14 d后,处死大鼠,通过测定血清中丙氨酸氨基转移酶(ALT),门冬氨酸氨基转移酶(AST),尿素氮(BUN),肌酐(SCr),白细胞介素-2(IL-2),肿瘤坏死因子-α(TNF-α)和核转录因子-κB(NF-κB)水平,称量各组织质量并计算其脏器系数,苏木素-伊红(HE)染色观察各组织脏器的病理学变化,评价其急性毒性。结果:未见大鼠死亡、明显中毒症状和肉眼可见的脏器异常。与空白组比较,十枣汤组体质量和饲料消耗量无统计学差异,大鼠各组织脏器系数均无统计学差异,血清中ALT,AST,BUN,SCr,IL-2,TNF-α,NF-κB无统计学差异,各组织病理切片亦未见异常现象。结论:大鼠经口给予十枣汤的最大给药量为12 g·kg~(-1),为成人日用剂量的480倍,安全性良好,提示十枣汤具有一定的安全范围。     

正交试验优化文蛤水溶性多糖的水提醇沉工艺

目的:优选文蛤水溶性多糖的水提醇沉工艺,为该有效部位的保健品开发提供实验依据。方法:采用蒽酮-硫酸法测定水溶性多糖的含量,检测波长625 nm。以水溶性多糖转移率为指标,通过单因素试验考察提取溶剂p H及绞碎程度对文蛤水溶性多糖转移率的影响。以水溶性多糖转移率为指标,通过正交试验考察加水量、提取时间、提取次数对文蛤水溶性多糖水提工艺的影响。以水溶性多糖得率及质量分数的综合评分为指标,通过正交试验考察浓缩程度、醇沉浓度、醇沉时间对文蛤水溶性多糖醇沉工艺的影响。结果:文蛤水溶性多糖的最佳水提工艺为加3倍水煎煮3次,每次40 min,水提液浓缩至原料的1/2,加乙醇醇沉至体积分数达80%,醇沉12 h,抽滤,60℃减压干燥。文蛤水溶性多糖得率7.71%,质量分数42.53%。结论:优选的文蛤水溶性多糖水提醇沉工艺稳定可行,可兼顾该有效部位的得率和纯度,为该部位的研究与开发提供参考。     

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??OBJECTIVE To proteins in toad venom. To investigate the by proteomic approach. METHODS The total proteins from the ear-side gland of toad were digested by trypsin, and the peptides were further analyzed by the NanoLC-linear trap quadropole (LTQ)-Orbitrap Velos Pro.. The raw data acquired by mass spectrometer were imported into MaxQuant software for the identification of peptides and proteins. The proteins were categorized based on gene ontology annotation in biological process, cellular component and molecular function. RESULTS A total of 407 protein groups and 880 peptides were identified. There were 76 pathways associated with the identified proteins in toad venom, including the 5-HT receptor mediated signaling pathway, beta adrenergic receptor signaling pathway, blood coagulation, cadherin signaling pathway, cholesterol biosynthesis, etc.. CONCLUSION This study lays the foundation for further exploration of the proteins in toad venom and their functions.     

Effects of VA-045 on peripheral and central circulation in anesthetized dogs

• 1.1. The effects of VA-045, a novel apovincaminic acid derivative, vinpocetine, apovincaminic acid, brovincamine and nicergoline on peripheral and cerebral circulation were examined in anesthetized dogs.
• 2.2. Peripheral circulation: VA-045 induced a transient decrease in both blood pressure (BP) and heart rate (HR) and an increase in vertebral arterial blood flow (VBF) without affecting femoral arterial blood flow (FBF) or carotid arterial blood flow (CBF). Vinpocetine had no effect on BP, HR, VBF, FBF or CBF. Apovincaminic acid decreased HR and increased VBF without affecting FBF, CBF or BP. Brovincamine increased VBF and decreased CBF without affecting BP or FBF. Nicergoline decreased BP without affecting VBF, FBA or CBF.
• 3.3. Cerebral circulation: VA-045 increased cerebral blood flow (CerBF) without affecting BP. Brovincamine also increased CerBF and decreased BP. The potency of VA-045 in increasing CerBF was stronger than that of brovincamine. Vinpocetine and apovincaminic acid had no effect on BP or CerBF. Nicergoline decreased BP but did not affect CerBF.
• 4.4. These findings indicate that VA-045 has a more selective vasodilative effect on the vertebral and cerebral arteries than the other reference drugs.

     

A radioimmunoassay combined with solid-phase extraction for the determination of a novel anti-obesity agent,ARL 15849XX,in dog plasma

A radioimmunoassay has been developed for the determination of ARL 15849XX, a cholecystokinin-8 (CCK-8) analogue, in dog plasma. The method incorporates solid-phase sample extraction and is suitable for the determination of the analyte at picogram per millilitre concentrations. The antiserum was raised in Suffolk-cross sheep following primary and booster immunisations with an immunogen prepared by conjugating ARL 16935XX, an analogue of ARL 15849KF, to bovine serum albumin. The radioligand was prepared by the no-carrier-added ¹²⁵I iodination of a non-sulphated derivative, ARL 15745XX. The solid-phase extraction procedure, carried out using ion-exchange aminopropyl and octadecyl sorbents sequentially, was introduced to remove matrix interferences in the plasma and to enhance the method sensitivity. The calibration range is 20–1000 pg ml⁻¹, using a 1 ml sample of undiluted dog plasma.