中药四性的生物热动力学研究—生晒参和红参药性的微量量热学比较

目的 通过生晒参和红参药性的微量量热学比较,阐明中药四性理论依据。方法 以来源于中药人参的生晒参和红参为研宄对象,用LBK2277微量量热计测定37℃条件下大肠杆菌E.coli(ACTT25922)正常生长条件下及给药后的生长代谢热谱图。结果 同一细菌在不同浓度药物抑制下热谱图形相同但随药物浓度增加,生长代谢过程的停滞期延长,生长代谢峰后移;E.coli的生长K-C曲线表明,人参加工成生晒参和红参后,药效发生了改变;在不同药液浓度下,细菌代谢过程的热功率一时间曲线与基线构成面积呈现一定规律性变化。结论 中药四性的微量量热法可作为定性定量测定中药四性的有效手段,是中药活性筛选的新工具。     

板蓝根乙酸乙酯提取物HPLC指纹图谱及体外抑菌活性的相关性分析

目的考察板蓝根乙酸乙酯提取物的HPLC指纹图谱及体外抑菌活性的相关性。方法HPLC法建立十批不同来源板蓝根的乙酸乙酯提取物的指纹图谱采用微量量热法记录大肠杆菌在板蓝根乙酸乙酯提取物作用下生长代谢的热谱图。运用系统聚类分析法考察不同来源板蓝根之间的差异，结合体外抑菌活性进行相关分析。结果不同来源板蓝根乙酸乙酯提取物的HPLC指纹图谱与体外抑菌活性之间存在很好的相关性。结论采用HPLC指纹图谱和体外抑菌活性相关性分析的方法，可以发现板蓝根乙酸乙酯部位抑菌活性有效成分。     

微量量热法研究清开灵对金葡菌生长代谢的影响

通过研究清开灵注射液对金葡菌生长代谢的影响,探索建立基于生物活性图谱的清开灵注射液的质量评价方法。本研究采用微量量热法,考察药物作用于金葡菌的生物热效应;对所测得的热输出曲线进行拟合,获得系列热动力学参数,对比分析各项热动力学参数及热输出曲线。结果显示,在一定范围内(0～5.00%),随清开灵剂量增加,金葡菌生长曲线呈下降趋势且指数生长期后延;其热动力学参数T1、T2、k1、P1、P2、I均与清开灵剂量呈现线性关系。清开灵注射液对金葡菌的半数抑菌量为3.26%,最佳抑菌量为5.47%;各类不同的清开灵注射液样品作用下的金葡菌生长曲线存在不同程度差异。实验结果表明,清开灵注射液对金葡菌生长具有较强的抑制作用,通过微量量热法研究,可对清开灵注射液的质量一致性进行初步评价。     

微量热技术在微生物和细胞研究方面的应用

用热力学和动力学原理及微量热技术研究微生物和细胞的生长代谢规律,及外界因素对其生长代谢的影响是一项新兴的研究方法。微量热分析可以绘制生物体生长热谱图,通过建立数学生长模型,可以得到生长速率常数k,最小抑菌浓度MIC,最大发热功率Pm,及总发热量Qtot等一系列热动力学参数,能定性和定量的说明问题。微量热技术是一项灵敏度高、测量准确的热分析技术,具有定量、实时、在线、动态描述等特点,已经在生命科学领域得到了广泛的应用,文章重点介绍微量热技术在微生物和细胞研究方面的应用。     

基于生物分子网络的人参皂苷Rg1的生物效应

目的:运用代谢组学及生物效应网络方法研究人参皂苷Rg1的生物效应的机制.方法:采用高效液相色谱-质谱(HPLC-MS)联用技术结合偏最小二乘判别分析方法,考察空白组与人参皂苷Rg1给药组的内源性物质差异,并确定生物标志物.结果:筛选出对分组贡献较大的25种潜在生物标记物,通过数据库确定了6个目标物的结构、代谢途径,相关酶和作用靶点,分别为吡哆醛与醛氧化酶、氨基葡萄糖和已糖激酶、甲基尿酸及黄嘌呤脱氢酶、多巴醌转化酪氨酸酶、氟尿苷与胸苷磷酸化酶、卵磷脂和卵磷脂胆固醇酰基转移酶.通过网络药理学及文献解释了人参皂苷Rg1在嘧啶代谢通路中为胸苷磷酸化酶的抑制剂;还可促进卵磷脂通过血浆卵磷脂胆固醇酰基转移酶催化成血浆胆固醇酯.结论:代谢组学及生物效应网络方法能用于人参皂苷Rg1生物效应机制的研究,为进一步揭示人参皂苷Rg1药理作用机制提供了新方法.     

抗病毒新药17997抗病毒效应的细胞微量量热的研究

目的研究抗病毒新药17997对细胞代谢的影响和抑制病毒复制时细胞热效应的变化。方法利用微量量热的方法。结果热代谢曲线表明 ,在有效抑制病毒复制浓度下 ,17997不影响宿主细胞的正常代谢 ,且能明显地降低病毒复制时的细胞热代谢。结论17997能够抑制病毒复制 ,对宿主细胞的热代谢没有影响。     

基于谱-效相关及网络药理学的西洋参不同部位增强免疫药效物质基础研究和作用靶点分析

目的:探究不同部位(主根、须根、茎、叶、花、芦头)西洋参皂苷类成分的差异及增强免疫作用，明确西洋参增强免疫的药效物质基础及作用靶点。方法:利用高效液相色谱技术检测西洋参不同部位的皂苷类成分；通过检测斑马鱼尾部中性粒细胞数目考察西洋参增强免疫作用；采用偏最小二乘相关回归分析法，确定药效物质；基于网络药理学，探究西洋参皂苷类成分增强免疫作用的核心靶点及作用通路。结果:西洋参不同部位人参皂苷含量差异大，总皂苷含量排序为：花>叶>主根>须根>芦头>茎；免疫增强实验显示，西洋参不同部位提取物均可增加中性粒细胞数目，其中除茎、芦头外均有显著免疫增强作用(P<0.01);偏最小二乘相关分析显示，西洋参中人参皂苷Re、人参皂苷Rc、人参皂苷Rb₂相关性较强，VIP值大于1;网络药理学分析得出西洋参增强免疫作用核心靶点为VEGFA、JUN、FGF2等，共有靶点涉及对刺激的反应、生物调节、细胞过程的调控等生物过程，并通过PI3K-Akt、Rap1、MAPK等信号通路发挥作用。结论:西洋参具有增强免疫作用，并且不同部位皂苷类成分含量显著不同，其增强免...     

紫红獐牙菜对STZ糖尿病小鼠的降糖作用

目的:对紫红獐牙菜4个提取部位的降血糖作用进行筛选,并探查其降血糖活性的作用机制是否影响胰岛素的分泌、体重。方法:采用渗漉法提取紫红獐牙菜的乙醇提取物,并将提取物依次萃取分离出乙醚部位、乙酸乙酯部位、正丁醇部位及水溶性4个部位。通过将此4个部位对由STZ诱导的2型糖尿病小鼠进行抗高血糖作用的药理活性研究,根据实验结果对此4个部位进行有效部位筛选,设定高低剂量组从而考察其量效关系。同时观察其对STZ诱导的2型糖尿病小鼠给药物7 d后对小鼠胰岛素抵抗的影响。结果:乙酸乙酯部位及水溶性部位对STZ引起的高血糖小鼠的血糖有较强的抑制作用,而正丁醇及乙醚部位则相对较差。并且各部位对小鼠胰岛素抵抗有十分显著改善。结论:乙酸乙酯及水溶性部位降血糖作用较明显。     

人参茎叶皂苷对毛囊间充质干细胞增殖的影响

目的:研究人参茎叶皂苷对毛囊间充质干细胞(hair follicle mesenchymal stem cell)的促增殖作用。方法:采用MTT法检测其是否增殖,筛选人参茎叶皂苷对毛囊间充质干细胞促增殖作用的有效浓度,流式细胞术研究加药后细胞周期。结果:当人参皂苷浓度为12.5μg/mL时对毛囊间充质干细胞的促增殖作用最强。结论:毛囊间充质干细胞是毛囊内发育成毛发的主要细胞之一,人参茎叶皂苷可能通过促进毛囊间充质干细胞增殖而促进毛发生长。     

人参皂苷Rb1对皮肤胶原代谢的影响

目的 将人参皂苷Rb1作用于人成纤维细胞,观察其对皮肤胶原代谢的作用.方法 人成纤维细胞在不同浓度的Rb1中的增殖情况,结果 用MTT法测定.消化法检测羟脯氨酸含量.酶联免疫吸附测定法测定细胞分泌Ⅰ型前胶原、基质金属蛋白酶-1(Matrix metalloproteinase-1,MMP-1)、基质金属蛋白酶抑制酶-1(Tissue inhibitor of metalloproteinase-1,TIMP-1)的蛋白表达情况.结果与空白组比较,人参皂苷Rb1能显著提高细胞增殖水平,羟辅氨酸含量、Ⅰ型前胶原及TIMP-1的蛋白质表达量(P<0.05),显著降低MMP-1蛋白质表达量(P<0.05).结论 皮肤胶原代谢受人参皂苷Rb1调节.这表现在能促进HSF增值;通过影响成纤维细胞的蛋白质的表达促进胶原合成并抑制胶原降解,结果提高胶原蛋白总量.     

Antidepressant properties of bioactive fractions from the extract of <Emphasis Type="Italic">Crocus sativus</Emphasis> L.

The aim of this study was to investigate the antidepressant properties of stigmas and corms of Crocus sativus L. The aqueous ethanol extract of C. sativus corms was fractionated on the basis of polarity. Among the different fractions, the petroleum ether fraction and dichloromethane fraction at doses of 150, 300, and 600 mg/kg showed significant antidepressant-like activities in dose-dependent manners, by means of behavioral models of depression. The immobility time in the forced swimming test and tail suspending test was significantly reduced by the two fractions, without accompanying changes in ambulation when assessed in the open-field test. By means of a gas chromatography–mass spectrometry technique, twelve compounds of the petroleum ether fraction were identified. These data show that administration of C. sativus corms extract produces antidepressant-like effects. Aqueous stigmas extract also exerted antidepressive effects in the behavioral models. Crocin 1 and crocin 2 of the aqueous stigmas extract were identified by a reversed-phase HPLC analysis. In addition, the bioactive compound crocin 1 in this herb was quantitatively determined. The data indicate that antidepressant-like properties of aqueous stigma extracts may be due to crocin 1, giving support to the validity of the use of this plant in traditional medicine. All these results suggest that the low polarity parts of C. sativus corms should be considered as a new plant material for curing depression, which merit further studies regarding antidepressive-like activities of chemical compounds isolated from the two fractions and mechanism of action.     

高剪切方法制备穿心莲干浸膏颗粒的影响因素考察

目的以3批流动性不同的穿心莲干浸膏为模型药,研究高剪切方法在制粒过程中的主要影响因素。方法分别以3批穿心莲干浸膏为原料,以颗粒粒径分布及各粒径范围内脱水穿心莲内酯含量分布的相对标准偏差(RSD%)为指标,对高剪切制粒过程中黏合剂用量、搅拌桨转速及制粒时间进行三因素两水平完全析因设计实验。结果黏合剂用量及制粒时间对3批流动性不同穿心莲干浸膏制得颗粒的几何平均粒径均有显著影响;流动性较差穿心莲干浸膏进行高剪切制粒时,最终颗粒群中脱水穿心莲内酯含量均匀度受搅拌桨转速影响程度最大;浸膏流动性不同,三因素之间交互作用有所不同。结论控制高剪切制粒过程的技术参数,可以改善流动性不同的中药浸膏制得颗粒的粒径分布及含量均匀度。     

Anti-inflammatory and Antioxidant Activity of Ageratum conyzoides

Ageratum conyzoides L., a plant widely used in African and South American folk medicine, contains many active principles, including pyrrolizidine alkaloids and polymethoxyflavones. We undertook the present study to evaluate the effect of the methanol extract and of the flavonoid fraction of the aerial part of the plant on carrageenan-induced edema in rat. We subjected the methanol extract to column chromatography to separate the flavonoids and assayed the radical scavenging activity of this fraction by the DPPH method. The two preparations produced significant inhibition on carrageenan-induced rat paw edema, until 2 h after carrageenan treatment. The flavonoids exhibited a strong inhibitory activity on the DPPH radical. The anti-inflammatory effect of A. conyzoides methanol extract depends on the flavonoid fraction, which could produce a protective action against free-radical mediated damage in cells and tissue. Therefore, it is possible to hypothesize that flavonoids influence inflammatory gene protein expression.     

苗药了哥王不同部位提取物的肾毒性研究

目的研究苗药了哥王不同部位提取物对健康大鼠的肾毒性作用,为了哥王的毒性作用机制及临床用药提供参考。方法以70%乙醇为溶剂,采用渗漉法提取,得了哥王乙醇总提取物;将上述提取物用水分散后,依次用石油醚、乙酸乙酯、正丁醇萃取得相应部位提取物,剩余为水部位提取物。将SD大鼠随机分为乙醇总提取物组、石油醚部位组、乙酸乙酯部位组、正丁醇部位组、水部位组和空白组,每组12只(雌雄各半)。给药组大鼠灌胃相应剂量的药液(乙醇总提取物317.520 mg/kg、石油醚部位7.875 mg/kg、乙酸乙酯部位78.435 mg/kg、正丁醇部位53.865 mg/kg、水部位76.545 mg/kg),每天1次,连续给药2周,再停药恢复2周;空白组大鼠灌胃等体积1.0%羧甲基纤维素钠溶液。实验期间观察大鼠的一般情况,取尿液(第14、28天)、血清和双肾组织(第15、29天),计算其肾脏指数,检测血清和尿液中的肾功能指标水平并观察肾组织的病理形态学变化。结果给药期间,与空白组比较,乙醇总提取物组、乙酸乙酯部位组大鼠出现精神萎靡、活动量和饮食量减少、大便稀薄、体质量下降等中毒行为活动特征;石油醚部位组、正丁醇部位组和水部位组大鼠精神状态较空白组稍差,活动量和饮食量稍减少,大便稀薄,体质量增长缓慢;但各组大鼠肛温无较大变化。给药2周后,乙醇总提取物组大鼠的肾脏指数,乙醇总提取物组、乙酸乙酯部位组大鼠血清中N-乙酰氨基葡萄糖苷酶(NAG)、尿素氮(BUN)、肌酐(Cr)水平,正丁醇部位组大鼠血清中NAG水平,水部位组大鼠血清中Cr水平,以及乙醇总提取物组、石油醚部位组大鼠尿液中NAG水平,乙酸乙酯部位组大鼠尿液中NAG、尿蛋白水平均显著升高(P<0.05或P<0.01);在病理形态学观察中,乙醇总提取物组、石油醚部位组和乙酸乙酯部位组大鼠有不同程度的肾小管结构不清、细胞肿胀、少数细胞坏死,伴有肾小球固缩、肾小管硬化、炎症细胞浸润。停药后,大鼠以上症状逐渐好转,精神状态有明显改善,活动量和饮食量增加,大便趋于正常。停药恢复2周后,各给药组大鼠血清和尿液中上述指标水平均恢复至与空白组接近(P>0.05);各给药组大鼠的肾小球结构逐渐恢复清晰,乙醇总提取物组、石油醚部位组和乙酸乙酯部位组大鼠少见细胞肿胀和炎症细胞浸润。结论苗药了哥王乙醇总提取物、石油醚部位和乙酸乙酯部位均具有一定的肾毒性,且具有一定的可逆性。其毒性成分可能为脂溶性成分。     

Imaging analysis of antiulcer action and the active constituent of Atractylodis rhizoma

Examination of the sizes of gastric mucosal injury has been conducted by visual means. However, the human visual-eye examination may sometimes involve personal biases and errors. In order to reduce these errors, automated analytical apparatuses have been developed. The equipment is generally expensive. In the present study, a low-cost imaging analytical method to examine the antiulcer action of drugs is reported. By using our imaging analytical method, an antiulcer effect of herbal medicine was examined on hydrochloric acid-ethanol induced gastric mucosal injury. Acetone extract of Atractylodis Rhizoma was found to have antiulcer action. In addition, the examination of fractions of the acetone extract, obtained through column chromatography, indicated that atractylon, at 17.5 mg/kg, p.o. significantly inhibits gastric mucosal injury.     

Immature Rubus coreanus Shows a Free Radical-Scavenging Effect and Inhibits Cholesterol Synthesis and Secretion in Liver Cells

Rubus coreanus fruits have been employed as a traditional medicine for centuries in the Asia-Pacific region. Its pharmacological action differs according to the different extraction methods utilized and the degree of fruit ripening. In this study, we determined the cellular effect of different ethanol extracts of mature and immature Rubus coreanus fruits in human hepatic cell line, HepG2 cells. The antioxidant activity, effect on superoxide dismutase activity and cholesterol biosynthesis efficiency was also evaluated. Immature Rubus coreanus extract showed higher antioxidant capability, compared with that of its mature fractions. Cellular antioxidant proteins including HO-1, Cu/Zn-superoxide dismutase and catalase were highly expressed in the presence of Rubus coreanus. Cholesterol levels in HepG2 cells treated with the water fraction of immature Rubus coreanus were significantly reduced. This antihyperlipidaemic action of Rubus coreanus is a consequence of cholesterol biosynthesis and extracellular secretion in HepG2 cells. These results indicate that among different ethanol fraction of mature and immature Rubus coreanus fruit extracts, water extract of immature fruit extract shows higher antioxidant as well as higher antihyperlipidaemic action.     

Evaluation of the anxiolytic-like effects of Cecropia glazioui Sneth in mice.

Cecropia glazioui Sneth has been used in most Latin American countries as an antihypertensive, cardiotonic, and antiasthmatic folk medicine. In the cardiovascular studies to define its antihypertensive action it was noteworthy that animals treated with the aqueous extract (AE) of C. glazioui were much calmer than control animals. That observation prompted the present study, aimed at an investigation of the effects of AE and of two semipurified fractions on mouse behavior as evaluated in the elevated plus-maze test (EPM). Male adult Swiss mice were treated with AE (0.25-1 g/kg po) acutely (1 h) or repeatedly (24, 7, and 1.5 h before the test). After repeated administration of AE, the frequency of entries in the open arms of EPM was increased threefold. A similar profile of action was observed after treatment with the butanolic fraction (Fbut) but not with the aqueous fraction (Faq). These findings suggest that the AE of C. glazioui promotes an anxiolytic-like effect in mice. The active principles responsible for this action are present in the less polar fraction of the extract, the main constituents of which are flavonoids and terpenes, among other compounds.     

翅柄铁线蕨治疗小鼠实验性良性前列腺增生有效部位的筛选

目的:研究翅柄铁线蕨对良性前列腺增生（BPH）模型小鼠的治疗作用,并筛选其有效部位。方法:皮下注射丙酸睾酮连续21d复制小鼠BPH模型,同时给药组分别灌胃给予翅柄铁线蕨总提取物及不同极性部位（石油醚、乙酸乙酯、正丁醇）(600mg·kg^-1·d^-1)。于末次给药后禁食,于次日剥离前列腺组织,称取前列腺湿质量,计算前列腺指数并进行病理学观察。结果:总提取物和乙酸乙酯部位组前列腺指数明显减小（P<0.05）,各用药组前列腺组织病理学变化均有不同程度的改善,其中乙酸乙酯部位组对BPH小鼠前列腺病理学改善效果最显著。结论:翅柄铁线蕨对BPH有一定的疗效,其中乙酸乙酯部位效果最好,初步确定为翅柄铁线蕨治疗BPH的有效部位。     

Stimulative activity of Drynaria fortunei (Kunze) J. Sm. extracts and two of its flavonoids on the proliferation of osteoblastic like cells

The osteoblastic activity of extracts of Drynaria fortunei (Kunze) J. Sm. rhizome was assayed in the UMR106 cell line cultured in vitro. An ethanol extract and its fractions were added to the cell culture at different concentrations. Osteoblastic proliferation stimulating activity was determined using the MTT method. The ethanol extract, and its ethyl acetate and n-butanol fractions exhibited stimulating activity. Two active constituents were isolated from n-butanol fraction by bioassay-directed isolation, and identified as naringin and neoeriocitrin. The latter is reported for the first time from this herbal medicine.     

Mechanisms of petroleum hydrocarbon toxicity: studies on the response of rat liver mitochondria to Prudhoe Bay crude oil and its aliphatic, aromatic and heterocyclic fractions

The effect of Prudhoe Bay crude oil (PBCO) and its different fractions [aliphatic, aromatic, heterocyclic (NOS)] on the bioenergetic functions of isolated rat liver mitochondria were studied. A DMSO extract of PBCO inhibited state 3 respiration (in the presence of ADP) with either succinate or beta-hydroxybutyrate as substrate. The ascorbate-TMPD dependent state 3 respiration was not affected. Succinate dehydrogenase and beta-hydroxybutyrate dehydrogenase activities were also lost in the presence of the PBCO extract suggesting that inhibition of state 3 respiration may be due to blockage of the electron transport chain. Stimulation of state 4 respiration (in the absence of ADP) and of the oligomycin sensitive ATPase activity by the PBCO extract was observed. Fractionation of PBCO indicated that the aromatic fraction was mainly responsible for its inhibitory effects. By comparison, the heterocyclic fraction had weak inhibitory properties while the aliphatic fraction was essentially inactive. It is concluded that the aromatic components of PBCO inhibit mitochondrial respiration and oxidative phosphorylation mainly through impairment of the mitochondrial membrane and inhibition of beta-hydroxybutyrate and succinate dehydrogenase supported electron transfer activities of the respiratory chain.