九里香抗生育活性物质——月橘烯碱的仿生合成研究

月橘烯碱是从芸香科植物九里香根中分出的双吲哚生物碱。药理实验结果表明它具有抗着床和抗早孕的活性。本文报道其仿生合成:吲哚经3位醛基化、与丙酮缩合成化合物Ⅱ;将氮原子保护后进行wittig反应,脱保护基得到β-异戊二烯吲哚(Ⅴ);经分子间Diels-Alder加成反应得消旋月橘烯碱(Ⅵ)。     

月橘烯碱抗着床作用及其激素活性的研究

小鼠于妊娠第1～3天,po或sc月橘烯碱(yuehchukene)2mg或4mg/kg·d有明显的抗着床作用。金黄地鼠于妊娠1～3天,sc月橘烯碱4mg/kg·d却无此作用。月橘烯碱有明显的雌激素活性,与雌二醇合用有协同作用。该化合物无雄激素或抗雄激素活性;无孕激素或抗孕激素活性。放射受体竞争实验测得月橘烯碱对[³H]-雌二醇与雌激素受体特异性结合抑制50%的浓度(IC₅₀)为4.2×10^-6mol/L,表观解离常数(KI)为1.24×10^-6mol/L。说明月橘烯碱与雌激素受体有一定的亲和力。     

广西九里香化学成分研究

目的　对广西九里香(Murraya kwangsiensis)的化学成分进行研究。方法　利用硅胶柱色谱和薄层色谱方法对广西九里香的95%乙醇提取物进行分离;采用UV,IR,MS,¹HNMR和¹³CNMR等技术对所得化合物进行结构研究。结果　分离鉴定了7个化合物,其中5个为咔巴唑生物碱:murrayafoline-A,murrayanine,koenine,isomahanine和广西九里香碱(kwangsine),两个非生物碱化合物：棕榈酸和β-谷甾醇。结论　广西九里香碱(kwangsine)为新化合物,其他化合物均为首次从该植物中分离得到。     

九里香化学成分的研究

自广东产芸香科(Rutaceae)植物九里香(Murraya paniculata(L.)Jack.)叶中分离得到六个香豆精,其中三个化合物为新的香豆精,根据光谱(UV,IR,NMR和MS)分析和化学方法确定九里香甲素(isomexoticin)九里香乙素(murpanidin)和九里香丙素(murpanicin)分别为(一)5,7-二甲氧基-8-(2′,3′-二羟基-3′-甲基丁基)香豆精(Ⅰ),(+)7-甲氧基-8-(1′,2′-二羟基-3′-甲基-3′-丁烯基香豆精(Ⅲ)和7-甲氧基-8-(1′-乙氧基-2′-羟基-3′-甲基-3′-丁烯基)香豆精(Ⅳ)。同时也得到三个已知香豆精murragatin(Ⅱ),murralongin(Ⅴ)和5,7-二甲氧基-8-(3′-甲基-2′-酮基丁基)香豆精(Ⅵ),最后一个是首次自本植物中得到的。     

单二乙氨基丙胺棉酚的合成及口服抗生育活性研究

单二乙氨基丙胺棉酚的合成及口服抗生育活性研究孔爱华１）朱崇泉薛慧中吴国沛（南京药物研究所，南京２１０００９）茅百勇赵世兴顾芝萍（上海药物研究所，上海２０００３１）在改变棉酚单个基团的结构改造工作中，作者先后合成了单甲氧基棉酚〔１〕、单醛棉酚和单苯胺棉...     

豆叶九里香挥发油化学成分的研究

豆叶九里香(Murraya euchrestifolia Hayata)系云香科九里香属植物,产在广西、云南等地。民间用其枝叶入药,有祛风活血、消炎止痛作用。我所药理研究室抗菌试验表明豆叶九里香挥发油对流感杆菌、枯草杆菌、肺炎球菌等11种菌株有明显的抑制作用,其中对流感杆菌(1:1600)抑制作用最强。广西北流县医药研究所用豆叶九里香油做成外用油膏治疗感     

豆叶九里香挥发油化学成分的研究

The essential oil from the branches and leaves of Murraya euchrestifolia Hayata was examined by GC, fractional distillation, column chromatography and GC/MS. Two main components were isolated from the essential oil by using fractional distillation and column chromatography on silica ogel and were identified as limonene (56.10%) and perillaldehyde (34.10%) respectively by IR, NMR and MS spectra. Seven other components were isolated in small amounts and identified as n-propyl-benzene, aromadendrene, elemol, 1-keto-4-hydroxy-decalin, 1-cycloheptyl-1-methyl-ethanol, myrtenal and eicosane.In addition, another seven compounds in this essential oil were identified as α-pinene, camphene, β-pinene, pulegone, perillylalcohol, dihydrocarveyl acetate and cis-carveyl acetate.     

血根碱、白屈菜红碱衍生物的合成与体外抗HBV活性研究

目的合成季铵类苯并菲啶生物碱血根碱(1)和白屈菜红碱(2)的衍生物,评价其体外抗HBV活性,初步探讨抗HBV活性。方法以血根碱和白屈菜红碱为原料,通过结构修饰获得衍生物,采用Hep G2.2.15细胞模型评价衍生物对HBsAg和HBeAg分泌抑制活性和HBV DNA复制的抑制活性。结果血根碱和白屈菜红碱对HBsAg、HBeAg和HBV DNA复制具有较高的抑制活性,但细胞毒性较高。氧化白屈菜红碱(6)对HBV DNA的复制具有一定的抑制作用(IC50=0.75 mmol·L-1),细胞毒性较白屈菜红碱明显降低(CC50>3.0 mmol·L-1)。6-乙氧基二氢血根碱(7)和6-乙氧基二氢白屈菜红碱(8)对HBsAg和HBeAg和HBV DNA复制具有一定的抑制活性。结论季铵类苯并菲啶生物碱具有显著的体外抗HBV活性,烯胺正离子结构单元对化合物的抗HBV活性产生重要的影响。     

中药九里香两种不同基原植物的药效学比较研究

对中药九里香的两种基原植物九里香(Murrayaexotica L.)和千里香(Murrayapaniculata(L.)Jack)的药效进行对比研究,为其多基原收载的合理性及临床用药的等同性提供参考.根据中药九里香的传统功效,采用小鼠扭体反应模型、大鼠足肿胀模型、小鼠胃排空及小肠推进试验、大鼠急性血瘀模型,系统地评价...     

2-(E)-(4-甲基亚苄基)环戊酮曼尼希碱的合成及其抗炎活性研究

目的 合成2－（E）－（4－甲基亚苄基）环戊酮的曼尼希碱及其类似物并研究目标化合物的抗炎作用。方法 以N－环戊烯基吗啉、4－甲基苯甲醛及多种胺类为原料合成目标化合物，并以二甲苯致小鼠耳肿胀模型测试目标化合物的抗炎活性。结果 共合成13个新化合物，经IR，^1H-NMR和MS确证其结构；部分化合物对二甲苯致小鼠耳肿胀具有较强的抑制作用。结论 2－（E）－（4－甲基亚苄基）环戊酮曼尼希碱类化合物具有较强的抗炎活性。     

Three new indole alkaloid derivatives from the roots of Murraya paniculata

Three new indole alkaloid derivatives, named paniculidines D?F (1?3), and six known analogs (4?9) were isolated from the roots of Murraya paniculata. The structures were elucidated on the basis of comprehensive HRESIMS, UV, IR, and NMR spectroscopic data analysis and comparison with the data reported in literature. The absolute configurations of new compounds were assigned via the determination of specific optical rotation, Mosher′s method, and ECD spectra. Compound 3 is the first heterodimer of C-N linked indole and coumarin derivatives.     

New heteroyohimbine-type oxindole alkaloid from the leaves of Thai <Emphasis Type="Italic">Mitragyna hirsuta</Emphasis>

A new oxindole alkaloid, isomitraphyllinol (1), was isolated from the leaves of Thai Mitragyna hirsuta, together with five known oxindole alkaloids (2–6). The structure of the new compound was determined by spectroscopic analysis.     

Guidance of neural regeneration on the biomimetic nanostructured matrix

Biomimetic materials are used for creating microsystems to control cell growth spatially and elicit specific cellular responses by combining complex biomolecules with nanostructured surfaces. Intercellular cell-to-cell and cell-to-extracellular matrix (ECM) interactions in biomimetic materials have demonstrated potential in the development of drug discovery platforms and regeneration medicine. In this study, we developed a biomimetic nanostructured matrix by using various ECM molecular layers to create a biomimetic and biocompatible environment for realizing neuronal guidance in neural regeneration medicine. Silicon-based substrates possessing nanostructures were modified using different ECM proteins and peptides to develop a biomimetic and biocompatible environment for studying neural behaviors in adhesion, proliferation, and differentiation. The substrates were flat glass, flat silicon wafers (FWs), and nanorod-structured wafers prepared using wet etching. The three substrates were then functionalized using laminin-1 peptide, PA22-2-contained active isoleucine-lysine-valine-alanine-valine (IKVAV) peptide, and poly-d-lysine (PDL), separately. When PC12 cells were cultured and differentiated on the modified substrates, the cells were able to elongate the neurites on the glass and FW, which was coated with three types of peptide. More differentiated neurons were observed on the nanorod-structured wafers coated with laminin than on those coated with IKVAV or PDL. For achieving directional guidance of neurite outgrowth, substrates exhibiting a grating pattern of nanorods were partially collapsed by the pulling force of water, leaving few nanorods, which support the net form of laminin on the surface. Furthermore, we fabricated the topological nanostructure-patterned wafer coated with laminin and successfully manipulated the extension and direction of neurites by using more than 80 μm of a single soma. This approach demonstrates potential as a facile and efficient method for guiding the direction of single axons and for enhancing neurite outgrowth in studies on nerve regenerative medicine.     

A concise total synthesis of secoisolariciresinol

A concise total synthesis of (R,R)-secoisolariciresinol was achieved in four steps, featuring a biomimetic β-β’ radical coupling of two dihydroferulic acid derivatives. The conversion of secoisolariciresinol to other related lignans was ongoing.     

A new carbazole alkaloid from the leaves of Malayan Murraya koenigii

New carbazole alkaloid, 7-hydroxymurrayazolinine (1), was isolated from the ethanol extract of the leaves of Malayan Murraya koenigii, together with five known carbazole alkaloids, mahanimbine (2), bicyclomahanimbine (3), girinimbine (4), koenimbine (5), and murrayamine-D (6). Their structures were elucidated on the basis of spectroscopic analysis.     

消炎镇痛药尼美舒利的合成工艺研究

目的　对尼美舒利的合成路线和工艺进行研究。方法　从 2 -氯硝基苯经苯氧基取代、还原、甲磺酰化和选择性硝化制得尼美舒利 ,并对各步反应的原料配比、反应时间进行了比较研究。结果　尼美舒利总收率达 63 %。结论　本工艺优化了反应条件。     

Recent advances of biomimetic nano-systems in the diagnosis and treatment of tumor

The lack of effective methods of diagnosis and treatment presents a major barrier to combat against tumor. The biomimetic concept is an emerging field that expresses great application potential in tumor fighting. Strategy for combining nano-systems with biomimetic technology has gained increasing attention that is proved bioinspired, environmentally benign, and promising. Herein, we provide an up-to-date review of biomimetic nano-systems as well as their applications in tumor therapy. In addition, the challenges and future directions of biomimetic nano-systems to achieve clinical translation are also pointed out.     

7-甲磺酰胺基-6-苯氧基-4-色满酮衍生物的合成及抗炎活性研究

目的 设计合成7-甲磺酰胺基-6-苯氧基-4-色满酮衍生物，并研究其抗炎活性。方法：以4-氨基-3-硝基苯甲醚、芳香醛等为原料。经多步反应合成目标化合物。以二甲苯致小鼠耳肿胀炎症模型筛选所合成化合物的抗炎活性。结果 共合成9个未见CA报道的化合物。经^1H-MNR、IR和MS确证其结构，其中有3个化合物在200mg／kg的剂量下，活性好于10mg／kg剂量的吲哚美辛(indomethacin)，4个化合物的活性略低于10mg／kg剂量下的吲哚美辛。结论 部分7-甲磺酰胺基-6一苯氧基-4-色满酮的3位取代芳基亚甲基类化合物有较强的抗炎活性，活性与芳香环的结构密切相关.     

Synthetic study toward the total synthesis of fumigaclavines A–D

In the present study, we developed a novel approach for the synthesis of the tetracyclic core of fumigaclavines A–D. A palladium-catalyzed intramolecular Larock indole synthesis was utilized to assemble the B/C rings of the tetracyclic core in one step. Although all attempts to convert compound 18 to fumigaclavine B failed, this study provided useful information for the total synthesis of fumigaclavines A–D.