端粒酶为靶的反义核酸药物癌泰德的临床前研究

癌泰德（cantide）是目前正在开发中的针对端粒酶（hTERT）的新型反义核酸药物。临床前研究表明，它能够选择性地抑制肿瘤活性并延长实验动物的生存期，通过抑制hTERT基因的表达来减少hTERT的活性，并能通过诱导Caspase依赖的凋亡起到快速的抑癌作用。现综述其毒理学和药动学的研究情况，包括体内和体外药效学、抗癌机制、急性毒性试验及药动学等。以上研究结果表明，癌泰德在体内和体外均安全和有效。     

苦参碱的药动学研究进展

苦参碱具有广泛的生物活性,如保护心、肝、肺、肾、脑、血管作用,对心脏有正性肌力、负性频率、抗心律失常作用,还有升高白细胞,平喘,抗溃疡,抗肝纤维化以及镇静、催眠、镇痛等中枢神经药理作用,也具有抗肿瘤、免疫调节、抗菌、抗病毒、抗炎等药理作用。其中抗肿瘤、心血管保护和治疗病毒性肺炎的药理作用的研究比较深入,希望生产企业开发苦参碱的这些新适应症。苦参碱是一种亲水性的弱碱性药物,易透过生物膜,口服和经皮给药易吸收和分布,约50%原型苦参碱经尿排泄。通过综述苦参碱药动学参数、体内过程,总结苦参碱的药动学研究进展,为合理用药提供参考。推荐将苦参碱试用于病毒性肺炎的治疗。     

阿昔替尼致不良反应文献分析

氧化苦参碱具有广泛的生物活性,如保护心、肝、肺、肾、脑、血管作用,对心脏有正性肌力、负性频率、抗心律失常作用,还有升高白细胞,平喘,抗溃疡,抗纤维化以及镇静、催眠、镇痛等中枢神经药理作用,也具有抗肿瘤、免疫调节、抗菌、抗病毒、抗炎等药理作用。氧化苦参碱是一种亲水性很强的弱碱性药物,易被代谢成苦参碱,尤其在口服给药时可被看做为苦参碱的前药。通过综述氧化苦参碱药动学参数、体内过程,总结氧化苦参碱的药动学研究进展,为合理用药提供参考。     

厚朴酚的药动学研究进展

厚朴酚具有广泛的生物活性，如抗菌、抗病毒、抗肿瘤、抗炎、抗氧化和抗衰老等，对消化、神经、心血管和呼吸系统等均有明显的药理作用。厚朴酚是一种疏水性联苯酚类结构化合物，难溶于水、易溶于脂，在胃肠道吸收较差，但分布广泛，约50%口服剂量的厚朴酚经胃肠道排出体外，40%以上的厚朴酚经代谢后排出体外。通过综述厚朴酚药动学参数、体内过程，总结厚朴酚的药动学研究进展，为合理用药提供参考。     

酸枣仁皂苷A的药理学研究进展

酸枣仁皂苷A(JuA)是酸枣仁中皂苷的主要成分.国内外研究表明JuA具有镇静催眠、降压降脂、抗炎、抗缺氧、增强免疫功能以及对心脏的保护等广泛的药理效应.随着药理学研究方法和技术的更新以及神经生物学的发展,JuA的药动学及其具有广泛的药理学作用不断被发现和深入研究.该文旨在对JuA的药动学研究和药理作用的研究进展作一综述,以期对以后的研究有所裨益.     

槐果碱和氧化槐果碱的药动学研究进展

槐果碱和氧化槐果碱属苦参碱类生物碱。苦参碱类生物碱具有广泛的生物活性,如保护心、肝、肺、肾、脑、血管作用,对心脏有正性肌力、负性频率、抗心律失常作用,还有升高白细胞、平喘、抗溃疡、抗肝纤维化以及镇静、催眠、镇痛等中枢神经药理作用,也具有抗肿瘤、免疫调节、抗菌、抗病毒、抗炎等药理作用。文中综述槐果碱和氧化槐果碱的药动学参数及其体内过程文献,并对其药动学的研究进展做了分析,为合理用药提供参考。     

眼部给药系统体内外评价方法的研究进展

眼部给药系统体内外评价方法的建立与研究是眼部给药系统缓控释作用的重要研究内容.其体外评价方法主要为体外释药实验,体内评价方法主要包括眼部滞留时间和药动学研究.笔者综合近年来的国内外文献报道,对眼部给药系统体内外评价方法的研究进展进行概述.     

聚乙二醇1000维生素E琥珀酸酯的应用优势及其抑制P-糖蛋白的作用机制

目的:总结聚乙二醇1000维生素E琥珀酸酯(TPGS)作为药用辅料的作用及其抑制P-糖蛋白的作用机理,并对其相关制剂的体内药动学和体外细胞学实验进行阐述。方法:查询、分类近期国内外文献,专利,说明书等一切相关资料,并进行归纳整理。结果:TPGS可作为高效乳化剂、缓控释载体材料、增溶剂和药物晶型稳定剂对制剂性质进行改善和提高。它是通过影响ATP酶的构象和活性来抑制P-糖蛋白对药物的外排作用。体内药动学实验表明TPGS可以提高抗癌药物的口服生物利用度,体外细胞学实验表明TPGS可以增加抗癌药物的细胞毒性。结论:TPGS是一种十分优秀的药用辅料,可以在制剂学中得到广泛的应用。     

丹参素钠、迷迭香酸和丹酚酸B在大鼠体内的药动学

目的建立用于同时测定大鼠血浆中丹参素钠、迷迭香酸和丹酚酸B的HPLC法,并研究丹参水溶性提取物在大鼠体内的药动学特征。方法大鼠灌胃给予丹参水溶性提取物(丹参素钠78.1 mg·kg-1、迷迭香酸40.4 mg·kg-1、丹酚酸B1.2 g·kg-1)后,眼眶静脉丛取血,经盐酸酸化及乙酸乙酯萃取后采用HPLC测定不同时间点的血药浓度。结果丹参素钠、迷迭香酸和丹酚酸B分别在0.4~10.0、0.24~6.00、0.8~10.0 mg·L-1内线性良好,方法回收率均在85%~115%之间,日内、日间精密度良好,稳定性符合要求。主要药动学参数t1/2(ka)分别为0.052、0.172、0.080 h;ρmax分别为1.072、2.290、4.128 mg·L-1;AUCo-t分别为6.674、6.933、8.943 mg·h·L-1。结论丹参素钠在大鼠体内的药动学过程符合单室模型,迷迭香酸和丹酚酸B符合二室模型。     

中药药动学研究进展

中药的药物代谢动力学(简称中药药动学)是借助于动力学原理,研究中草药活性成分、组分、中药单方和复方在动物或人体内的吸收、分布、代谢和排泄的动态变化规律及其体内时量或时效关系,并用数学函数加以定量描述的一门新兴边缘学科[1]。近年来国内外学者在中药药动学研究方面进行了大量的实践,内容涉及生物利用度、毒动学、透皮吸收药动学、群体药动学、时辰药动学、证治药动学、活性成分在肠道的代谢处置和在体液中浓度的测定等。中药药动学的研究对阐明和揭示中草药作用机制及其科学内涵,设计及优选给药方案,促进中药新药开发和剂型改进及…     

迷迭香酸的研究现状

迷迭香酸属酚酸类化合物,存在于多种植物中,具有明显的抗氧化、抗茵、抗肿瘤等活性．因此如何提高其提取率、纯度并建立快速有效的定量分析方法便显得尤为重要。本文对迷迭香酸的提取分离、定量分析研究现状进行综述。旨在为迷迭香酸生产和应用企业提供有价值的参考依据。     

迷迭香酸药理作用的研究进展

迷迭香酸是一种含多酚羟基的酸,广泛存在于多种植物中,具有多种药理作用。已广泛用于食品、化妆品、医药等方面。本文简述迷迭香酸近年来在药理作用及临床应用方面的研究进展,旨在为其开发利用提供参考。     

迷迭香酸的研究进展

目的探讨迷迭香酸药理研究近况。方法 从迷迭香酸抗炎、抗氧化、免疫抑制等方面研究概况进行综述。结果 迷迭香酸抗炎,抗氧化、免疫抑制等作用显著,并探讨了作用机理。     

迷迭香酸的研究概况

迷迭香酸是一种含多酚羟基的酸,广泛存在于多种植物中,具有抗菌、抗病毒、抗氧化、抗炎等多种药理作用。本文对其提取分离、生物合成、定性鉴别、定量分析、药理作用研究概况进行了综述,旨在为其开发利用提供科学参考。     

Neurobehavioral and genotoxic aspects of rosmarinic acid.

Rosmarinic acid is a naturally occurring hydroxylated compound. It is present in many plants, for example, it occurs in Artemisia capillaris, Calendulla officinalis, Melissa officinalis, Salvia officinalis and in other several plant families. It also shows a number of interesting biological activities, e.g. antiviral, antibacterial, antiinflammatory and antioxidant. The aim of the present study was to investigate the effect of the i.p. administration of rosmarinic acid (1, 2, 4 or 8 mg kg(-1)) on elevated plus-maze, step-down inhibitory avoidance and open field task in rats. In addition, we evaluated its genotoxic effect on brain tissue using the comet assay. Rosmarinic acid (2 and 4 mg kg(-1)) increased the number of entries in the open arms, suggesting an anxiolytic-like activity when used in lower doses, without affecting the short-term memory (STM) and long-term memory (LTM) retention on inhibitory avoidance task. Eight milligrams per kilograms of this acid was enough to increase the locomotion and motivation of the animals, but not 1, 2 or 4 mg kg(-1), suggesting that in lower doses, this compound can produce anxiolytic-like effect without exerting locomotor alterations or DNA damage in brain tissue.     

Rosmarinic acid antagonized 1-methyl-4-phenylpyridinium (MPP+)-induced neurotoxicity in MES23.5 dopaminergic cells

Rosmarinic acid (RA) is a naturally occurring polyphenolic compound found in various plant families. We previously reported that RA exerted protective effects against 6-hydroxydopamine (6-OHDA)-induced neurotoxicity through antioxidative properties. In this study, we investigated whether RA could prevent effects of 1-methyl-4-phenylpyridinium (MPP(+))-induced insult in MES23.5 dopamineric cells. 1-Methyl-4-phenylpyridinium treatment decreased cell viability and dopamine content, as well as caused apoptotic morphological changes. 1-Methyl-4-phenylpyridinium-induced mitochondrial dysfunction, indicated by inhibition of activity associated with mitochondrial respiratory chain complex I, suggested mitochondrial transmembrane potential collapse and generation of reactive oxygen species. Decreased Bcl-2/Bax ratio and caspase 3 activation were also observed. Rosmarinic acid pretreatment restored the complex I activity of the mitochondrial respiratory chain and partially reversed the other damaging effects of MPP(+). Our results indicate that RA plays a neuroprotective role by ameliorating mitochondrial dysfunction against MPP(+)-induced cell apoptosis and suggest that RA has the potential to be considered an aid for prevention of Parkinson's disease.     

Rosmarinic acid in Perilla frutescens and perilla herb analyzed by HPLC

High-quality perilla leaves are defined as those having purple upper and lower surfaces and a pleasant smell. The Japanese Pharmacopoeia specifies the content of essential oils in perilla leaves but not the content of rosmarinic acid. Rosmarinic acid is a common component of Labiatae plants such as shiso (Perilla frutescens Britton var. crispa W. Deane). Rosmarinic acid has been reported to exhibit anti-inflammatory and anti-oxidant activity but the factors affecting the content of rosmarinic acid in plants remain unknown. This study describes a simple and reproducible method for quantifying rosmarinic acid. We elucidated the main causes for the different rosmarinic acid contents of plants by examining various samples of perilla using the proposed method. Significant differences in rosmarinic acid content between varieties and cultivators were observed. The rosmarinic acid content was higher in green perilla compared with red perilla, in wild species compared with cultivated species, and in plants cultivated in outdoor nurseries compared with in indoor nurseries. The proposed quantitative method was used to examine the rosmarinic acid content in a Kampo formula, Hangekobokuto, and was found to be higher in decoctions prepared using the Kouge method compared with the typical preparation method. We examined the chlorophyll and caffeic acid contents of several samples and their relationship with the rosmarinic acid content.     

Cr (VI) induced oxidative stress and toxicity in cultured cerebellar granule neurons at different stages of development and protective effect of Rosmarinic acid

Chromium (Cr) is a widespread metal ion in the workplace, industrial effluent, and water. The toxicity of chromium (VI) on various organs including the liver, kidneys, and lung were studied, but little is known about neurotoxicity. In this study, neurotoxic effects of Cr (VI) have been investigated by cultured cerebellar granule neurons (CGNs). Immature and mature neurons were exposed to different concentrations of potassium dichromate for 24 h and cytotoxicity was measured by MTT assay. In addition, immature neurons were exposed for 5 days as regards cytotoxic effect in development stages. The reactive oxygen species (ROS), mitochondrial membrane potential (MMP) and the protective effect of Rosmarinic acid on mature and immature neurons exposed to potassium dichromate, were measured. Furthermore, lipid peroxidation, glutathione peroxidase (GPx), and acetylcholinesterase activity in mature neurons were assessed following exposure to potassium dichromate. The results indicate that toxicity of Cr (VI) dependent on maturation steps. Cr (VI) was less toxic for immature neurons. Also, Cr (VI) induced MMP reduction and ROS production in both immature and mature neurons. In Cr (VI) treated neurons, increased lipid peroxidation and GPx activity but not acetylcholinesterase activity was observed. Interestingly, Rosmarinic acid, as a natural antioxidant, could protect mature but not immature neurons against Cr (VI) induced toxicity. Our findings revealed vulnerability of mature neurons to Cr (VI) induced toxicity and oxidative stress. © 2014 Wiley Periodicals, Inc. Environ Toxicol 31: 269–277, 2016.     

迷迭香酸对前列腺癌细胞生物行为学的影响

目的初步探讨迷迭香酸对人前列腺癌细胞DU-145恶性生物行为学的影响。方法培养前列腺癌细胞DU-145,利用MTT方法检测药物对癌细胞存活率和生长状态的影响;用流式细胞仪分析细胞总体的凋亡情况;采用细胞划痕试验和利用Transwell小室检测不同浓度的药物处理一定时间后前列腺癌细胞DU-145的运动、迁移、侵袭能力的变化;通过Western blot法检测迷迭香酸作用前列腺癌细胞DU-145后丝裂原活化蛋白激酶(mitogen-activated protein kinase,MAPK)通路P38,ERK、JNK蛋白表达量的情况。结果MTT结果显示迷迭香酸呈浓度梯度抑制前列腺癌细胞DU-145的生长;迷迭香酸能够抑制前列腺癌细胞DU-145的运动、迁移、侵袭;通过Western blot方法检测表明,迷迭香酸增加磷酸化的P38和JNK蛋白表达,降低磷酸化的ERK蛋白量表达。结论迷迭香酸可以抑制前列腺癌细胞DU-145的存活率,促进癌细胞凋亡,抑制其迁移能力,其机理可能与调节MAPK通路有关。     

Influence of rosmarinic acid on opsonization and intracellular killing of Escherichia coli and Staphylococcus aureus by porcine and human polymorphonuclear leucocytes

The influence of rosmarinic acid on the function of porcine and human polymorphonuclear leucocytes was tested. Rosmarinic acid inhibited the chemiluminescence of PMNL, induced by preopsonized Zymosan or phorbol myristate acetate. The killing of Escherichia coli was inhibited by rosmarinic acid at a concentration of 2 mM, but not that of Staphylococcus aureus. The inhibition of the killing was due to an impaired opsonization, caused by an adverse influence of rosmarinic acid on complement activation. Direct effects of rosmarinic acid on the killing mechanisms of PMNL were not observed.