目的 制备绵马贯众有效部位微丸,并对其进行处方优化.方法 采用单因素法考察挤出速度、滚圆速度、滚圆时间等制备工艺因素,黏合剂浓度、崩解剂种类及用量、填充剂中MCC的比例、羟丙基-β-环糊精与药物比例等处方因素对微丸成型和溶出的影响;并在此基础上,采用Box-Behnken效应面法,以5 min和30 min时的累积溶出度为评价指标,对微丸处方进行优化;建立UPLC法测定溶出介质中药物含量,并对微丸溶出度及溶出曲线进行考察.结果 制备工艺参数为挤出速度60 r·min-1,滚圆速度1500 r·min-1,滚圆时间5 min;溶出介质选择含5％吐温80和5 mg·mL-1 D-异抗坏血酸钠的PBS溶液(pH 6.8),所选定的较优处方在5 min和30 min时的累积溶出度符合要求.结论 采用单因素结合Box-Behnken效应面法成功优化得到具有较快释药特征的绵马贯众有效部位微丸.

微丸是一种多元释药系统,其稳定、可调控的释药机制常应用于中药提取物、有效部位或成分释放的改善和生物利用度的提升.本文基于中药微丸制剂研究思路总结了中药微丸的制剂工艺,并结合近年来中药微丸的体外评价研究方法和体内药动学、药效学的研究进展进行了综述,以期为中药微丸的制备工艺设计和体内外评价提供参考思路.

目的 考察不同剂量雷公藤多苷片对糖尿病肾病大鼠肾脏损伤的保护作用及其作用机制.方法 构建糖尿病肾病大鼠模型,给药第8周时,检测比较各组单侧肾指数,肾功能指标(血尿素氮、血肌酐和肌酐清除率),肾脏自噬相关蛋白(LC3B、PI3K、Akt和mTOR)的表达水平,LAMP1和LC3蛋白的荧光表达,观察肾脏病理切片.结果 6.25 mg·kg-1雷公藤多苷片组可显著降低BUN,提高LC3B蛋白表达,抑制PI3K、Akt和mTOR蛋白表达,增强LAMP1和LC3蛋白荧光表达,促进自噬,发挥肾脏保护作用;当剂量增加到25、50 mg·kg-1时,Ccr显著降低,PI3K、Akt和mTOR蛋白表达升高,LC3B蛋白表达水平降低,LAMP1和LC3表达减少,表明肾脏功能下降,自噬呈抑制状态.结论 6.25 mg·kg-1雷公藤多苷对糖尿病肾病大鼠肾脏损伤具有保护作用,可能与PI3K/Akt/mTOR自噬信号通路有关.

近年来,雷公藤多苷(TWP)在临床使用越来越广泛,多被用于治疗类风湿关节炎,还作为基本免疫抑制药物治疗各种肾脏疾病,如肾病综合征等,但其临床有多种不良反应事件发生,用药方案存在争议,尤其是使用剂量和使用时间.为了雷公藤多苷的临床合理使用和深入研究,综述其药理毒理研究进展.通过梳理近年来国内外有关雷公藤多苷的药理毒理研究文献,发现雷公藤多苷的药理作用研究多集中在抗炎、抗肿瘤、肾脏保护和免疫抑制方面,主要是通过调节核转录因子-κB(NF-κB)信号通路,雷帕霉素靶蛋白(mTOR)信号通路和细胞凋亡相关信号通路的细胞因子表达水平发挥药理作用;其毒理作用研究多集中在肝毒性、肾毒性和生殖系统毒性方面,毒性作用多与氧化应激反应和炎症因子表达相关.雷公藤多苷的主要活性成分研究集中在雷公藤内酯醇和雷公藤红素.雷公藤多苷药理毒理研究较深入,表明其效、毒存在剂量依赖性和时间依赖性,具有量-效、时-效、量-毒、时-毒关系,未见雷公藤多苷在功效背景下随使用剂量和时间变化的毒性研究,其关联机制仍需进一步深入研究与探讨.

阿魏酸及其衍生物的药用价值越来越受到重视,笔者通过系统梳理阿魏酸在来源、药理作用、安全性及临床应用4个方面近30年来的研究文献,总结其研究进展如下:1)来源包括天然来源、化学合成和生物合成;2)已发现的药理作用有抗氧化、抗血栓、降血脂、降低心肌缺血和耗氧量、抗菌、抗病毒、抗癌等;3)体外无细胞毒性作用,只抑制细胞增殖,体内与川芎嗪在半数致死量下,共同作用毒性可降低,且其毒性有随季节变化的趋势;4)临床上多用于治疗冠心病、肾病、肺动脉高压、脑梗死、阿尔茨海默病等疾病.此综述旨在为更好地开发利用阿魏酸及其衍生物提供参考.

目的:筛选紫萁贯众中具有良好抗流感病毒神经氨酸酶(neuraminidase,NA)活性的化合物.方法:将紫萁贯众已分离得到的23个化合物与18种流感病毒神经氨酸酶进行分子对接,通过评价结合能、结合模式及发生相互作用的氨基酸等指标进行虚拟筛选,得到候选化合物,并通过神经氨酸酶抑制剂实验验证候选化合物抑制NA的活性.结果:候选化合物异银杏双黄酮对NA抑制作用较强,IC50值为(42.54±2.85) μmol· L-1.结论:紫萁贯众中化合物异银杏双黄酮具有较好的流感病毒神经氨酸酶抑制作用,为紫萁贯众在抗流感病毒临床方面的应用提供了科学依据,也为紫萁贯众的深入研究奠定了基础.

目的:筛选绵马贯众中流感病毒H5N1神经氨酸酶(NA,neuraminidase)抑制剂.方法:将绵马贯众中已分离得到的99个化合物建立配体库,从Protein Data Bank(PDB)中下载NA(H5N1)的X-ray晶体三维结构文件,采用AutoDock Vina软件筛选出与NA有较好结合作用的化合物,并通过神经氨酸酶抑制实验验证筛选出的化合物对NA的作用.结果:通过分子对接筛选出5个与NA有较好结合的化合物,神经氨酸酶抑制实验结果表明候选化合物中Dryocrassin ABBA对NA的抑制作用最强,IC50为(18.59±4.53) μmol/L.结论:绵马贯众中化合物DryocrassinABBA具有较好的抗H5N1流感病毒神经氨酸酶的作用.

目的:建立UPLC法同时测定绵马贯众抗病毒有效部位(GZP部位)中绵马酸ABB、绵马贯众素ABBA和绵马贯众素ABBP的含量.方法:采用Zorbax SB-C18色谱柱(50 mm×2.1 mm,1.8 μm),以含0.1％甲酸的甲醇(A)-0.1％甲酸溶液(B)为流动相,梯度洗脱;流速:0.5 mL/min;检测波长:298 nm;柱温:40℃.结果:绵马酸ABB、绵马贯众素ABBA和绵马贯众素ABBP在相应的浓度范围内均有良好的线性关系,平均加样回收率分别为97.98％、98.03％、98.97％.结论:该含量测定方法准确可靠,灵敏度高,可为绵马贯众及其抗流感病毒有效部位的质量控制提供参考.

Phytochemical investigation on Ilex asprella stems by using various chromatographic techniques led to the isolation of 18 phenolic constituents. Based on spectroscopic data analyses and/or comparison of the spectroscopic data with those in literature, these constituents were identified, including two lignans (1, 2), five phenylpropanes (3-7), six chlorogenic analogues (8-13), and five benzoic analogues (14-18). Among them, compounds 3-7, 9, 11, 13, 14, 17, and 18 were isolated from genus Ilex for the first time, and 2, 8, 10, 15, and 16 were isolated from this species for the first time. The in vitro anti-inflammatory assay results showed that compounds 8, 9, 11, 13, and 15 possessed moderate inhibition on the NO production in RAW264.7 cells with IC₅₀ values of 51.1-85.8 μmol·L⁻¹. The present study brought preliminary reference for the clarification of therapeutic ingredients of I. asprella with anti-inflammatory efficacy and its quality evaluation.

Objective To study the inhibitory effect of phloroglucinols in Mianma Guanzhong(Dryopteris crassirhizoma Nakai,Basket Fern Nakai)on neuraminidase(NA)of H1N1 influenza virus.Methods A library of 34 phloroglucinols ligands was established through retrieving, and X-ray three-dimensional crystal structure file of NA(H1N1)was downloaded from Protein Data Bank.The phloroglucinols possessing lower binding energy and stronger hydrogen bond interaction with NA were screened by using AutoDock Vina software and LigPlot +software, and the inhibitory effect of candidate phloroglucinols on NA was verified by using fluorometric assay.Results There were 4 phloroglucinols(filixic acids ABA, ABB, ABP and ABBA)with better combination with NA screened through molecular docking.The results of fluorometric assay showed that dryocrassin ABBA had the strongest inhibitory effect on NA [(IC50)=(26.73 ±0.57)μmol/L].Conclusion Dryocrassin ABBA in Mianma Guanzhong has higher effect of anti-NA of H1N1 influenza virus, which lays a foundation for further study on new anti-influenza drugs.

流感是由流感病毒引起的呼吸道疾病,发病率高、流行广泛、变异性强.中药在抑制流感病毒方面有其独特优势,目前在我国临床已有广泛应用,研究表明其具有多方面确切疗效,具有更广泛的适应性.通过采用文献查阅法,对抗流感病毒中药的有效成分、体内外抗流感病毒作用及其机制进行阐述.

Objective To find the most active phloroglucinol compound on influenza virus from Dryopteris crassirhizoma.Methods Twenty-five phloroglucinols from D.crassirhizoma were docked into 12 kinds neuraminidase (NA) for molecular docking.The binding energies,the combination of compound and neuraminidase and the interaction with the important amino acid residues were used for virtual screening.The inhibitory effect in vitro of four candidate compounds on NA was tested by NA inhibition assay,on this basis,M22 was evaluated for its antiviral activity on MDCK cells via CPE assay.Results Virtual screening suggested that five candidates had strong binding abilities with NA.NA inhibition assay showed that M22 have the strongest activity against NA of all candidates.CPE assays demonstrated that M22 exhibited inhibitory activity on various influenza virus.Conclusion M22 from D.crassirhizoma have significant inhibitory efficacy on influenza virus.The results provide us with useful information for the development of novel anti-influenza drugs.

Encouraged by the in vivo anti-inflammatory effect of aqueous extract of Ilex asprella stems, a further phytochemical investigation on I. asprella stems oriented by the in vitro NO production inhibition in RAW264.7 cells was conducted, which led to the isolation of eight new phenolic constituents, namely asprenols A-H (1-8), together with 12 known ones (9-20). The structures of the new compounds were established by extensive spectroscopic data analyses of HR-ESI-MS, IR, UV, and 1D and 2D NMR, and the absolute configurations were determined by comparison of experimental and calculated ECD analyses. All isolated were evaluated for the inhibition against NO production in RAW 264.7 cells, and several compounds showed moderate inhibitory effect.

Ahmpatinin iBu and statinin iBu, two new linear peptides, were isolated from Streptomyces sp. CPCC 202950. Ahmpatinin iBu exhibited significant inhibitory activity against HIV-1 protease with an IC50 value of 1.79 nM.

In the present work, fruits of Prangos platychlaena Boiss. ex Tchihat. ssp. platychlaena (Apiaceae) collected from eastern (sample A) and central (sample B) parts of Turkey were subjected to hydrodistillation to yield essential oils (EOs). The chemical composition of P. platychlaena ssp. platychlaena fruit oil was analyzed by gas chromatography—flame ionization detector (GC—FID) and gas chromatography—mass spectrometry (GC—MS) techniques. An unknown compound with m/z 178 [M]+ in high percentages was detected in both EOs (45.8% and 11.2% in samples A and B, respectively). Column chromatography on silica gel was subsequently followed by the sample A and yielded a new acetylenic derivative (1), which was characterized by spectroscopic techniques as (2S)- 3,5-nonadiyne-2-yl acetate. Samples A and B oils were characterized by a series of acetylenic derivatives like 3,5-nonadiyne (24.5% and 5.8% in A and B, respectively), (Z)-3,5-nonadiyne-7-ene (0.2% in A), and (E)-3,5-nonadiyne-7-ene (0.5% in A). Monoterpenes α-pinene (6.8% and 12.8%), α-phellandrene (0.1% and 17.1%), and β-phellandrene (4.2% and 22.4%) were found to be the major components in P. platychlaena ssp. platychlaena EOs in samples A and B, respectively. The components of P. platychlaena ssp. platychlaena EOs were separated on the overpressured layer chromatography (OPLC) plates, and the plates were subsequently subjected to direct-bioautography assays using three plant pathogens such as Colletotrichum acutatum, C. fragariae, and C. gloeosporioides; however, no antifungal activity was observed. Due to a high yield, sample A was evaluated for its repellent activity against female mosquito Aedes aegypti and attraction of sterile male Mediterranean fruit fly Ceratitis capitata. Sample A demonstrated good repellency against Ae. aegypti in human-based cloth patch bioassays and no attraction to C. capitata in short range bioassays.

Objective:To study the constituents of aerial part of Morinda parvifolia.Methods:The chemical constituents were isolated and purified by means of chromatographic techniques and their structures were elucidated by spectroscopic methods.Results:Eleven compounds were isolated from dichloromethane part of ethanol extract,and identified as 1-hydroxy-3-hydroxymethyl-anthraquinone(1),1-hydroxy-6-hydroxymethyl-anthraquinone (2),ficusic acid (3),8-hydroxy-6,7-dimethoxy-coumarin (4),6-hydroxy-7,8-dimethoxy-coumarin (5),7-hydroxy-6,8-dimethoxy-coumarin (6),methyl 2-carboxyl-5-methoxy-benzoate (7),methyl 3,4-dihydroxy benzoate (8),ethyl 2-carboxyl-5-methoxy-benzoate (9),4-hydroxybenzaldehyde (10) and 4-hydroxy benzoic acid (11).Conclusion:All the compounds are isolated from this plant for the first time.

Objective To probe into the influence of polysaccharides of Luotuopeng (Peganum harmala L.,Herb of Common Peganum) on toxicity of PolyQ accumulation in the muscle cells of AM141 strain of Caenorhabditis elegans (C.elegans).Methods The polysaccharides of Luotuopeng were extracted by using water extraction followed by sequential alcohol deposition method,and the content of each precipitation was determined by using phenol-sulfuric acid method.The polysaccharides were added to medium,and then samples were collected for counting the number of fluorescence dots due to PolyQ-YFP accumulation in the muscle cells of C.elegans.The influence of the polysaccharides on toxicity of PolyQ accumulation in AM141 strain of C.elegans was reviewed.The precipitation precipitated by 60％ ethanol with higher activity was purified by using macroporous resin for re-reviewing the activity.Results The mass fractions of the polysaccharides precipitated by 30％ ethanol,60％ ethanol or 80％ ethanol were,respectively,20.07％,21.80％,19.98％.The inhibition rates of the polysaccharides on the fluorescence dots due to PolyQ-YFP accumulation in the muscle cells of C.elegans were,respectively,7.9％,17％ and-1.72％.After the precipitation precipitated by 60％ ethanol purified with macroporous resin,the mass fractions of the polysaccharides,in 10％ and 20％ ethanol elution with higher mass fractions,were,respectively,49.76％ and 38.26％,and the inhibition rates were,respectively,35.25％ and 18.03％.Conclusion The method for reviewing the influence of the polysaccharides on toxicity of PolyQ accumulation through model of AM141 strain of C.elegans is easy,stable and reliable.The polysaccharide precipitated by 60％ ethanol has the highest inhibitory effect on PolyQ accumulation with a dose-effect relationship.

目的 探索中药类研究生专业英语课程的教学思路.方法 对在读硕士研究生进行关于专业英语教学的无记名问卷调查,统计学生对于专业英语课程的实际需求,针对统计结果设计专业英语课程的教学方法、教学内容以及考核方式.结果 92％的研究生认为需要开设专业英语课程,且66％的学生希望能重点提高SCI论文的写作能力,因此,中药类研究生的专业英语课程需要选择近期发表的SCI论文作为主要教学内容,采用情景模拟式和研讨式的教学方法,并且引入学生互评的手段让学生参与到考核环节.结论 中药类研究生专业英语课程的教学应从学生的实际需求出发,将教学重点放在提高学生SCI论文的阅读和写作能力方面.

For screening the active phloroglucinols on influenza virus (H5N1) from Dryopteris crassirhizoma NaKai, a database was established including twenty-three phloroglucinols that had been isolated from Dryopteris crassirhizoma. Their inhibitory effect on the neuraminidase (NA) of influenza virus H5N1 was screened by molecular docking. As a result, three candidates were selected. The rhizomes of D. crassirhizoma were subjected to isolation and purification processes to obtain the inhibitor candidates. Thirteen phloroglucinols were obtained, including three selected candidates and two new phloroglucinols. The five phloroglucinols were investigated for their inhibitory activity on NA in vitro. The results showed that dryocrassin ABBA and filixic acid ABA exhibited inhibitory effects on NA with IC50 as 18.59 ± 4.53 and 29.57 ± 2.48 μM, respectively, and the other three phloroglucinols showed moderate inhibitory activity. Moreover, the anti-influenza virus (H5N1) activity and cytotoxicity of dryocrassin ABBA and filixic acid ABA were tested on Madin-Darby canine kidney (MDCK) cells with the cell counting kit-8 (CCK8) method. The results confirmed that dryocrassin ABBA exhibited an inhibitory activity with low cytotoxicity (TC50 > 400 μM) against influenza virus (H5N1) which will have to be investigated in further detail. In conclusion, phloroglucinols from D. crassirhizoma were shown to have anti-influenza virus activity, and especially dryocrassin ABBA, one of the phloroglucinols, may have the potential to control influenza virus (H5N1) infection.

Ilex asprella is one of representative medicinal plants in South of the Five Ridges of China. The roots and rhizomes of I. asprella have the effects of clearing heat and detoxifying, stimulating salvia, and reducing thirst, which has been used to treat wind-heat cold, acute and chronic pharyngitis, and sore throat. Contemporary studies showed that I. asprella contains the major triterpenoids and glycosides, phenolic acids, and minor steroids. The extracts and compounds show activities of anti-inflammatory, antiviral, anti-tumor, and regulating lipid metabolism.The present paper summarizes a phytochemical and pharmacological advance on this species to provide reference for clarification of its pharmacologically active ingredients, quality evaluation, and further explorations.