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cytochalasin B loaded nano/microparticles:preparation and in vitro drug release evaluation

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Chinese Journal of Biomedical Engineering(English Edition) 2000年第1期9卷 1-9页

作者： SONG Cun xian SUN Hong fan YANG Jin ZHU Zhen feng WANG Peng yan Robert Levy Institute of Biomedical Engineering Peking Union Medical CollegeChinese Academy of Medical SciencesTianjin 300192China

cytochalasin B (cytoB) loaded nanoparticles (NPs) and microspheres (MSs) were formed using an emulsification / solvent evaporation *** poly(lactic co glycolic acid)(PLGA) and poly(L lactic acid)(PLLA)were used as carrier and were compared in terms of drug release rate and initial *** PLGA nanoparticles and microparticles of graded diameter,150 nm,500 nm,1 μm,5 μm,10 μm and 20 μm,is *** of 150 500 nm diameter were obtained by high energy sonication,whereas larger size particles were obtained by normal *** degree of initial burst release varied depending on particle size and polymer *** the PLGA matrix,about 50% of the entrapped drug released from the 150 nm nanoparticles,whereas only 10% released from the 20 μm particles within the first 24 *** the other hand,cytoB release from 150 nm PLLA nanoparticles was much slower and showed less burst effect than the PLGA ones with same *** results suggest that desired release profile can be achieved by properly selecting the matrix material and particle size.

关键词： cytochalasin B Nanoparticle Microsphere

A new cytochalasin from endophytic Phomopsis sp. IFB-E060

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Chinese Journal of Natural Medicines 2014年第7期12卷 512-516页

作者： SHEN Li LUO Qian SHEN Zhi-Ping LI Ling-Yu ZHANG Xiao-Jun WEI Zhong-Qi FU Yi SONG Yong-Chun TAN Ren-Xiang Medical College Yangzhou University State Key Laboratory of Element Organic Chemistry Nankai University Institute of Functional Biomolecules State Key Laboratory of Pharmaceutical Biotechnology Nanjing University

AIM: To study the chemical constituents of the solid culture of the endophyte Phomopsis sp. IFB-E060 in Vatica mangachapoi. METHOD: Isolation and purification were performed through silica gel column chromatography, gel filtration over Sephadex LH-20, ODS column chromatography, and HPLC. Structures of the isolated compounds were elucidated by a combination of spectroscopic analyses(UV, CD, IR, MS, 1D, and 2D NMR). The cytotoxicity of the isolates was evaluated in vitro by the MTT method against the human hepatocarcinoma cell line SMMC-7721. RESULTS: Five compounds were isolated from the solid culture of the endophyte Phomopsis sp. IFB-E060 and their structures were identified as 18-methoxy cytochalasin J(1), cytochalasin H(2),(22E, 24S)-cerevisterol(3), ergosterol(4), and nicotinic acid(5). Compound 1 had an inhibition rate of 24.4% at 10 μg·mL-1 and 2 had an IC50 value of 15.0 μg·mL-1, while a positive control 5-fluorouracil had an inhibition rate of 28.7% at 10 μg·mL-1. CONCLUSION: 18-Methoxy cytochalasin J(1), produced by endophytic Phomopsis sp. IFB-E060, is a new cytochalasin with weak cytotoxicity to the human hepatocarcinoma cell line SMMC-7721.

关键词： Phomopsis sp. Sphaeropsidaceae Vatica mangachapoi Endophyte cytochalasin

Effects of microfllamentous depolymerization by cytochalasin B on cAMP-PKA pathway

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Chinese Science Bulletin 1996年第8期41卷 684-687页

作者：鞠文君王端顺 Department of Biology Beijing Normal University Beijing 100875 China

Diacylglycerol (DG) and cAMP, two intracellular second messengers, play importantroles in responding to the stimulation of extracellular signal. DG activates protein kinaseC (PKC), and cAMP activates protein kinase A ... 详细信息

关键词： cytochalasin B microfilament cyclic adenosine monophosphate protein kinase A G0 phase cells.

从子囊菌炭球菌中分离的活性成分L-696,474和cytochalasin D对植物病原真菌的活性(英文)

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植物保护学报 2007年第2期34卷 113-122页

作者：罗都强唐宏亮杨小龙王飞刘吉开河北大学生命科学学院保定071002 中国科学院昆明植物研究所植物化学与西部资源持续利用国家重点实验室

在我国云南省高等真菌中寻找新的天然农用抗真菌活性物质时,发现炭球菌子实体甲醇提取物具有较强的离体抗真菌活性。采用生物活性追踪和化学分离相结合的方法,从中分离得到2个具有较强农用抗真菌活性化合物,经红外、质谱、氢谱和碳谱确... 详细信息

在我国云南省高等真菌中寻找新的天然农用抗真菌活性物质时,发现炭球菌子实体甲醇提取物具有较强的离体抗真菌活性。采用生物活性追踪和化学分离相结合的方法,从中分离得到2个具有较强农用抗真菌活性化合物,经红外、质谱、氢谱和碳谱确定其为L-696,474和cytochalasin D。在离体和活体条件下分别测定了L-696,474和cytochalasin D对10种植物病原菌的菌丝抑制率和2种植物病原菌的孢子萌发率,并评价了其对小麦白粉病的治疗和保护作用。结果表明:小麦纹枯病菌、油菜菌核病菌对L-696,474最为敏感,浓度为10μg/mL时菌丝抑制率分别为83.5%和82.9%;小麦赤霉病菌、小麦全蚀病菌、油菜菌核病菌、小麦叶枯病菌和苹果炭疽病菌对cytochalasin D最为敏感,浓度为10μg/mL时菌丝抑制率分别为83.6%、82.4%、81.9%、80.5%和79.7%。L-696,474和cytochalasin D在200μg/mL时完全抑制苹果炭疽病的孢子萌发;在500μg/mL时对小麦白粉病10天后的治疗作用分别为74.3%和85.7%,保护作用为67.1%和79.5%。

关键词： L-696,474 cytochalasin D 炭球菌抗真菌活性

1株花柳珊瑚来源真菌Curvularia lunata产cytochalasin B发酵优化及其化学表观遗传修饰研究

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中国海洋药物 2016年第5期35卷 14-20页

作者：李德宝张雪晴张秀丽侯雪梅管菲菲王长云邵长伦中国海洋大学海洋药物教育部重点实验室医药学院山东青岛266003

目的通过对中国南海花柳珊瑚来源真菌Curvularia lunata(RA16-1)进行发酵优化以提高该菌的cytochalasin B产量,并加入组蛋白去乙酰化酶抑制剂丁酸钠以考察对该菌次级代谢产物的影响。方法运用单因素试验设计,对菌株产cytochalasin B的... 详细信息

目的通过对中国南海花柳珊瑚来源真菌Curvularia lunata(RA16-1)进行发酵优化以提高该菌的cytochalasin B产量,并加入组蛋白去乙酰化酶抑制剂丁酸钠以考察对该菌次级代谢产物的影响。方法运用单因素试验设计,对菌株产cytochalasin B的碳源、氮源、初始pH值、盐浓度等发酵条件进行优化;运用柱色谱层析技术对加入丁酸钠的真菌Curvularia lunata(RA16-1)发酵产物进行分离,以及核磁与质谱技术对分离的化合物进行结构鉴定。结果单因素试验表明最优发酵条件为:碳源为蔗糖(30g·L^(-1))、氮源为蛋白胨(30g·L-1)、发酵时间为96h、初始pH为5.0、盐浓度为2%。此外,从加入丁酸钠的发酵产物中分离得到了4个化合物,其中2个化合物(化合物2和3)为首次从该物种中获得。结论在优化条件下,cytochalasin B的产量可达到2.3g·L^(-1)。组蛋白去乙酰化酶抑制剂丁酸钠的加入后使得该菌发酵产物的结构类型发生较大变化。

关键词：花柳珊瑚来源真菌优化 cytochalasin B 丁酸钠

分子内D-A反应用于合成六氢异色烯-1-酮及cytochalasin Z8中六氢异吲哚-1-酮骨架

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分子内D-A反应用于合成六氢异色烯-1-酮及Cytochalasin Z8中六氢...

作者：林本国浙江大学

学位级别：硕士

分子内Diels-Alder反应是一类极其重要的有机反应,能够高效地形成碳碳键,是构筑复杂的多元环结构的有效方法。本论文主要论述微波辅助分子内Diels-Alder(简称IMDA)反应用于合成六氢异色烯-1-酮化合物,以及天然产物cytochalasin Z8中六... 详细信息

分子内Diels-Alder反应是一类极其重要的有机反应,能够高效地形成碳碳键,是构筑复杂的多元环结构的有效方法。本论文主要论述微波辅助分子内Diels-Alder(简称IMDA)反应用于合成六氢异色烯-1-酮化合物,以及天然产物cytochalasin Z8中六氢异吲哚-1-片段的合成。本论文第一章主要是介绍IMDA反应和天然产物cytochalasins系列大环内酯化合物的全合成。首先是介绍了IMDA反应合成六氢异色烯-1-酮化合物立体化学的选择性问题;其次是简单列举了几个IMDA反应应用于天然产物全合成的例子;最后介绍了在cytochalasins系列大环内酯化合物的全合成中不同小组的合成策略。第二章的内容是微波辅助分子内Diels-Alder反应合成六氢异色烯-1-酮化合物。详细介绍在C6位连接甲基的含酯基的1,3,9-癸三烯原料的制备,再通过微波辅助的方式,利用分子内Diels-Alder反应合成六氢异色烯-1-酮化合物,探索产物的立体选择性规律。并通过与己具有单晶数据的化合物的核磁共振谱对比,确定了反应产物的立体化学。本文的第三章介绍了对天然产物cytochalasin Z8中六氢异吲哚-1-片段的合成的探索。叙述了第一代和第二代合成路线的研究,以及更换内酰胺的保护基团的第三代合成路线,通过引入强吸电子的Boc保护基活化酰胺的羰基,成功的将C9位氧化并翻转其构型。论文在最后部分叙述了主要的实验操作步骤、化合物结构的表征数据、参考文献、部分化合物的1H NMR和13C NMR核磁共振谱图及X射线单晶衍射解析数据等。

关键词：微波辅助分子内Diels-Alder反应六氢异色烯-1-酮 cytochalasin 六氢异吲哚-1-酮

cytochalasins from Xylaria sp. CFL5, an Endophytic Fungus of Cephalotaxus fortunei

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Natural Products and Bioprospecting 2021年第1期11卷 87-98页

作者： Kai-Liang Ma Shi-Hui Dong Hang-Ying Li Wen-Jun Wei Yong-Qiang Tu Kun Gao State Key Laboratory of Applied Organic Chemistry College of Chemistry and Chemical EngineeringLanzhou UniversityLanzhou 730000People’s Republic of China

Three previously undescribed cytochalasins,named xylariasins A‒C(1‒3),together with six known ones(4‒9)were iso-lated from Xylaria ***5,an endophytic fungus of Cephalotaxus *** chemical structures of all new compounds were elucidated on the basis of extensive spectroscopic data analyses and electronic circular dichroism calculation,as well as optical rotation *** activities of compounds 1,4‒9 were evaluated,including cytotoxic,LAG3/MHC II binding inhibition and LAG3/FGL1 binding inhibition *** 6 and 9 possessed cytotoxicity against AGS cells at 5μM,with inhibition rates of 94%and 64%,*** addition,all tested isolates,except compound 6,exhibited obvious inhibitory activity against the interaction of both LAG3/MHC II and LAG3/*** 1,5,7,and 8 inhibited LAG3/MHC II with IC50 values ranging from 2.37 to 4.74μ***,the IC50 values of compounds 1,7,and 8 against LAG3/FGL1 were 11.78,4.39,and 7.45μM,respectively.

关键词： cytochalasin Xylaria sp. Cephalotaxus fortunei LAG3/MHC II binding inhibition LAG3/FGL1 binding inhibition

Chemical Components from the Fungus Engleromyces goetzei

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Acta Botanica Sinica 2003年第2期45卷 248-252页

作者：占扎君孙汉董吴厚铭岳建民中国科学院上海生命科学院上海药物研究所新药研究国家重点实验室上海200031 中国科学院昆明植物研究所植物化学开放实验室昆明650204 中国科学院上海有机化学研究所生命有机国家重点实验室上海200032

A new ceramide, (2S,3S,4R, 10E)-2-[(2'R)-2'-hydroxytetracosanoyl amino]-10-octadecene-1, 3,4-triol (1), together with twelve known compounds, cerebroside A, cerebroside B, cerebroside D, cytochalasin D, epoxycytochalasin D, cytochalasin C, loganin, cerevisterol, ergosta-7,22-dien-3beta, 5alpha, 6alpha-triol, ergosta-4,6,8(14),22-tetraen-3-one, ergosterol peroxide and ergosta-5,7,22-trien-3-ol, was isolated from ethyl acetate fraction of Engleromyces goetzei P. Henn. The structure of new ceramide (1) was elucidated by spectral data and chemical method, especially by 2D-NMR techniques. All of the compounds except cytochalasin D were first obtained from this fungus.

关键词： Engleromyces goetzei cytochalasin iridoid glucoside ceramide

FFECTS OF OOPLASM CYTOSKELETON ON MIGRATION AND DEVELOPMENT OF SPERM-NUCLEI IN MOUSE EGGS

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Chinese Science Bulletin 1990年第10期35卷 851-856页

作者：陈大元潘忠宗张天荫 Laboratory of Reproductive Biology Institute of Zoology Academia Sinica Bering 100080 PRC Department of Biology Shandong University Jinan 250100 PRC

Longo and CHEN elucidated in 1985 that the origin of polarity of mouse oocytes, the germinal vesicle breakdown and resumption of meiosis are temporospatially related to one another, and further demonstrated the responsibility of microfilaments for the peripheral movement of the meiotic apparatus including chromosomes. Recently, it has been shown by CHEN et al. that the chromosomal movement of the mitotic apparatus at the ear-

关键词： pronuclei cytoskeleton colchicine cytochalasin B.