三七3-羟基-3-甲基戊二酸单酰辅酶A还原酶基因的克隆和生物信息学分析

目的克隆三七总皂苷甲羟戊酸合成途径中的1个关键酶3-羟基-3-甲基戊二酸单酰辅酶A还原酶(3-hydroxy-3-methylglutaryl coenzyme-A reductase,HMGR)基因,为进一步研究HMGR蛋白的功能及开展三七皂苷的合成生物学研究奠定基础。方法根据NCBI上已公布的同属人参的HMGR基因全长序列(登录号GU565097.1)设计特异性引物。利用RT-PCR技术,以三七愈伤组织总RNA反转录的cDNA为模板扩增基因片段;并对其编码的蛋白进行生物信息学预测和基因表达分析。结果序列分析表明,获得的三七HMGR(命名为PnHMGR)基因的cDNA序列大小为1 893 bp,该序列与人参、刺五加和杜仲中HMGR基因的一致性分别达到98%、93%、80%,且含有大小为1 725 bp的开放阅读框,经Genbank查询为一新的cDNA。生物信息学预测PnHMGR基因编码蛋白包含2个跨膜区,不含信号肽,具有HMGR催化作用的活性中心结构域。实时荧光定量PCR检测到PnHMGR基因在三七细胞生长30 d表达量最高。结论首次从药用植物三七中克隆得到HMGR基因的编码区序列,为进一步鉴定PnHMGR的功能和开展三七皂苷的合成生物学研究奠定了基础。     

推拿手法对高血压患者血压及血压变异性的影响(英文)

目的:观察推拿手法对高血压患者的血压及血压变异性的影响。方法:选取高血压患者40例,将其随机分为观察组和药物组,每组20例。观察组在常规药物治疗基础上予以"益肾活血通脉"推拿手法治疗,药物组仅采用与观察组相同的常规药物治疗。分别于治疗前及治疗3个月后行24-hour动态血压监测,比较两组患者血压及血压变异性的变化。结果:治疗前两组患者的血压及血压变异系数组间差异无统计学意义(P>0.05);治疗3个月后,两组患者血压及血压变异系数均较本组治疗前显著改善(P<0.05);观察组改善情况优于对照组,两组间差异有统计学意义(P<0.05)。结论:"益肾活血通脉"推拿手法结合常规药物对高血压患者的血压及血压变异性改善情况优于单纯常规药物治疗,且操作方便,无毒副作用,适宜临床推广应用。     

消痔灵注射液治疗内痔出血疗效观察

目的 评价消痔灵注射液治疗内痔出血的临床疗效.方法 80例内痔出血患者经口服泻药或者灌肠,排便后自腔缘3、6、9点注入麻醉药,观察应用消痔灵注射液治疗80例内痔出血患者的疗效进行回顾性分析.结果 80例内痔出血患者中76例次日出血停止,4例便后偶有滴血症状,经局部换药、使用痔疮栓及局部熏洗等保守治疗后出血消失,随访6～24个月无复发.结论 消痔灵注射液治疗内痔出血是一种简单、有效、可靠的方法.

Abstract：

Objective To assess the clinical effect and safety of Xiaozhiling injection on bleeding caused by hemorrhoids.Methods A retrospective analysis was performed on 80 hemorrhoid patients treated with Xiaozhiling injection.Results Among 80 patients.76 bleeding stopped after the injection.Four bleeding had interrupted outbreak and was cured after symptomatic treatment.Conclusion Xiaozhiling is an effective medicine for treatment of hemorrhoids bleeding.     

Binding and Anticancer Properties of Plumbagin with Human Serum Albumin

Plumbagin has received extensive attention as a promising anticancer drug. Therefore, we investigated the binding and anticancer properties of plumbagin with human serum albumin. Fluorescence results demonstrated that plumbagin interacts with human serum albumin, although its binding affinity may be affected to various extents by different compounds. The human serum albumin–plumbagin complex structure revealed that plumbagin binds to the hydrophobic cavity in the IIA subdomain of human serum albumin through hydrogen bonding and hydrophobic interactions. The plumbagin–human serum albumin complex enhances cytotoxicity by 2‐ to 3‐fold particularly in cancer cells but has no effect on normal cells in vitro. Compared with the unbound drug, the human serum albumin–plumbagin complex promotes HeLa cell apoptosis and has a stronger capacity for cell cycle arrest at the G2/M phase of HeLa cells. In conclusion, this study contributes to the rational design and development of plumbagin‐based drugs and a drug–human serum albumin delivery system.     

Triptolide induced cell death through apoptosis and autophagy in murine leukemia WEHI‐3 cells in vitro and promoting immune responses in WEHI‐3 generated leukemia mice in vivo

Triptolide, a traditional Chinese medicine, obtained from Tripterygium wilfordii Hook F, has anti‐inflammatory, antiproliferative, and proapoptotic properties. We investigated the potential efficacy of triptolide on murine leukemia by measuring the triptolide‐induced cytotoxicity in murine leukemia WEHI‐3 cells in vitro. Results indicated that triptolide induced cell morphological changes and induced cytotoxic effects through G0/G1 phase arrest, induction of apoptosis. Flow cytometric assays showed that triptolide increased the production of reactive oxygen species, Ca²⁺ release and mitochondrial membrane potential (ΔΨ_m), and activations of caspase‐8, ‐9, and ‐3. Triptolide increased protein levels of Fas, Fas‐L, Bax, cytochrome c, caspase‐9, Endo G, Apaf‐1, PARP, caspase‐3 but reduced levels of AIF, ATF6α, ATF6β, and GRP78 in WEHI‐3 cells. Triptolide stimulated autophagy based on an increase in acidic vacuoles, monodansylcadaverine staining for LC‐3 expression and increased protein levels of ATG 5, ATG 7, and ATG 12. The in vitro data suggest that the cytotoxic effects of triptolide may involve cross‐talk between cross‐interaction of apoptosis and autophagy. Normal BALB/c mice were i.p. injected with WEHI‐3 cells to generate leukemia and were oral treatment with triptolide at 0, 0.02, and 0.2 mg/kg for 3 weeks then animals were weighted and blood, liver, spleen samples were collected. Results indicated that triptolide did not significantly affect the weights of animal body, spleen and liver of leukemia mice, however, triptolide significant increased the cell populations of T cells (CD3), B cells (CD19), monocytes (CD11b), and macrophage (Mac‐3). Furthermore, triptolide increased the phagocytosis of macrophage from peripheral blood mononuclear cells (PBMC) but not effects from peritoneum. Triptolide promoted T and B cell proliferation at 0.02 and 0.2 mg/kg treatment when cells were pretreated with Con A and LPS stimulation, respectively; however, triptolide did not significant affect NK cell activities in vivo. © 2016 Wiley Periodicals, Inc. Environ Toxicol 32: 550–568, 2017.     

苦碟子中的新黄酮苷(Ⅱ)

苦碟子为菊科植物抱茎苦荬菜〔Ｉｘｅｒｉｓｓｏｎｃｈｉｆｏｌｉａ(Ｂｇｅ.)Ｈａｎｃｅ〕的当年生干燥全草,具有清热解毒、消肿止痛之功效〔1〕。其主要成分为以木犀草素、芹菜素为苷元的黄酮苷.继前报〔2〕报道了两个新黄酮苷之后,又从该植物中提取分离得到一种新的黄酮苷,命名为木犀草素7ＯβＤ吡喃葡萄糖醛酸苷乙酯(ｌｕｔｅｏｌｉｎ7ＯβＤｇｌｕｃｕｒｏｎｉｄｅｅｔｈｙｌｅｓｔｅｒ,Ⅰ),此化合物为一个未见文献报道的新化合物,结构见图1.提取分离:苦碟子全草5ｋｇ,用70%的乙醇加热回流,过滤,滤液回收乙醇,经真空干燥后,浓缩液混悬于…     

美洛昔康口腔崩解片中美洛昔康含量测定方法研 究简

目的 建立测定美洛昔康口腔崩解片中美洛昔康含量的反相高效液相色谱法.方法 色谱柱为KromasilC18柱（250 mm×4.6mm,5 μm）,流动相为0.1 mol/L醋酸铵溶液-甲醇（50：50）,柱温为室温,流速为1.0 mL/min,检测波长为271 nm.结果 美洛昔康质量浓度在40 ～ 60 μg/mL范围内与峰面积呈良好线性关系（r=0.999 8）,平均回收率为100.45％,RSD为0.55％（n=9）.结论 该方法简便、灵敏、准确、专属性强、重现性好,为产品的质量标准研究提供了理论依据.     

吗替麦考酚酯在原发性肾病综合征患者中的群体药动学研究

目的：研究吗替麦考酚酯在原发性肾病综合征患者中的群体药动学模型,为临床个体化用药提供参考。方法选取2011年1月~2014年2月期间我院收治的56例原发性肾病综合征患者作为本组研究的观察对象,所有患者在给予吗替麦考酚酯对症治疗后,采集其血液样本,通过非线性混合效应模型构建出麦考酚酯的群体药动学模型,从而探讨患者的年龄、性别、身高、体重、剂量、血清肌酐、治疗时间等对药动学参数的影响。结果药动学基本模型采用一级吸收和消除的二房室模型最为有效;患者体重与治疗时间是吗替麦考酚酯清除率的主要因素;最终群体药动学模型为：清除率=0.476×体重×(1-e-1.17POD)。结论吗替麦考酚酯在原发性肾病综合征患者中的药动学模型具有明显的代表性,为个体化给药方案的确定提供依据。     

哌拉西林钠-他唑巴坦钠优选给药方案的评估及应用的研究现状

目的为哌拉西林钠-他唑巴坦钠的临床合理用药提供参考。方法对哌拉西林钠-他唑巴坦钠的优选给药方案的药动/药效学研究、临床试验及具体实施情况进行综述。结果哌拉西林钠-他唑巴坦钠的优选给药方案（延长输注或持续输注）可最大化地达到药效学目标,改善临床有效性。结论需积极完善优化方案用于临床实践的策略。     

通痹胶囊对佐剂关节炎大鼠的继发关节病变及免疫功能的影响

目的初步探讨复方中药通痹胶囊对类风湿关节炎(RA)的治疗作用及机制。方法取Wistar雄性大鼠,制成佐剂关节炎(AA)模型,设正常组、模型组、雷公藤多甙对照组、通痹胶囊治疗组,观察不同处理因素对各组实验鼠继发关节肿胀度,继发病变分级,胸腺、脾脏重量及白细胞介素(IL)-1β的影响。结果治疗后通痹胶囊组、雷公藤组的继发关节肿胀,继发病变分级以及对实验鼠的胸腺、脾脏重量、IL-1β的影响与模型组相比差异均有显著性(P<0.05);通痹胶囊组与雷公藤组相比差异无显著性(P<0.05)。结论通痹胶囊对佐剂关节炎大鼠继发病变有明显的治疗作用;对模型大鼠胸腺、脾脏重量及IL-1β的抑制说明该方有一定的免疫抑制作用,这可能是该方治疗RA的机制之一。