Semi-Synthesis,Cytotoxic Evaluation,and Structure—Activity Relationships of Brefeldin A Derivatives with Antileukemia Activity     

Xu-Xiu Lu  Yao-Yao Jiang  Yan-Wei Wu  Guang-Ying Chen  Chang-Lun Shao  Yu-Cheng Gu  Ming Liu  Mei-Yan Wei 《Marine drugs》2022,20(1)

Brefeldin A (1), a potent cytotoxic natural macrolactone, was produced by the marine fungus Penicillium sp. (HS-N-29) from the medicinal mangrove Acanthus ilicifolius. Series of its ester derivatives 2–16 were designed and semi-synthesized, and their structures were characterized by spectroscopic methods. Their cytotoxic activities were evaluated against human chronic myelogenous leukemia K562 cell line in vitro, and the preliminary structure–activity relationships revealed that the hydroxy group played an important role. Moreover, the monoester derivatives exhibited stronger cytotoxic activity than the diester derivatives. Among them, brefeldin A 7-O-2-chloro-4,5-difluorobenzoate (7) exhibited the strongest inhibitory effect on the proliferation of K562 cells with an IC₅₀ value of 0.84 µM. Further evaluations indicated that 7 induced cell cycle arrest, stimulated cell apoptosis, inhibited phosphorylation of BCR-ABL, and thereby inactivated its downstream AKT signaling pathway. The expression of downstream signaling molecules in the AKT pathway, including mTOR and p70S6K, was also attenuated after 7-treatment in a dose-dependent manner. Furthermore, molecular modeling of 7 docked into 1 binding site of an ARF1–GDP-GEF complex represented well-tolerance. Taken together, 7 had the potential to be served as an effective antileukemia agent or lead compound for further exploration.  相似文献   

Exogenous application of melatonin improves plant resistance to virus infection     

L. Zhao  L. Chen  P. Gu  X. Zhan  Y. Zhang  C. Hou  Z. Wu  Y.-F. Wu  Q.-C. Wang 《Plant pathology》2019,68(7):1287-1295

In this study, melatonin (MEL)-mediated plant resistance to tobacco mosaic virus (TMV) was examined to study local infection in Nicotiana glutinosa and systemic infection in Solanum lycopersicum. Exogenous application of 100 µm MEL increased anti-virus infection activity to 37.4% in virus-infected N. glutinosa plants. The same treatment significantly reduced relative levels of virus RNA analysed by qRT-PCR and virus titres measured by dot-ELISA, and increased the relative expression levels of the PR1 and PR5 genes analysed by qRT-PCR, in virus-infected S. lycopersicum. MEL treatment induced considerable accumulations of salicylic acid (SA) and nitric oxide (NO) but did not significantly affect production of hydrogen peroxide (H₂O₂) in the virus-infected S. lycopersicum plants. Transgenic nahG N. tabacum was used to determine whether MEL-induced TMV resistance was dependent on the SA pathway. The results showed that the relative RNA level of the TMV analysed by qRT-PCR and virus titres analysed by dot-ELISA were not reduced by the MEL treatment in the nahG transgenic N. tabacum seedlings treated twice with 100 µm MEL. The increased relative expression levels of PR1 and PR5 were greatly reduced when cPTIO, an NO scavenger, was included in the MEL treatment. A working model of MEL-mediated plant resistance to TMV is proposed. MEL-mediated plant resistance to viruses provides a new avenue to control plant viral diseases.  相似文献   

喷头和施药液量对水稻植株上农药沉积和药剂防治效果的影响   总被引：2，自引：0，他引：2  

徐德进  徐广春  许小龙  徐鹿  顾中言  邱白晶 《植物保护学报》2019,46(2):409-416

为明确喷头及施药液量对水稻植株上农药沉积及药剂防治效果的影响,采用丽春红-G示踪法测定了4种喷头ST11001、ST11002、TR8001、TR8002在不同施药液量条件下喷雾农药在水稻植株上的沉积分布特性,并比较了4种喷头施用相同剂量的40%氯虫苯甲酰胺·噻虫嗪WDG对水稻纵卷叶螟Cnaphalocrocis medinalis和褐飞虱Nilaparvata lugens的防治效果。结果表明,选择ST11002和TR8001喷头,在施药液量300 L/hm~2条件下喷雾,单株水稻上的丽春红-G沉积量分别达到27.55μg和28.16μg;选择ST11001和TR8002喷头,在施药液量900 L/hm~2条件下喷雾,单株水稻上的丽春红-G沉积量仅分别为12.27μg和14.86μg。喷头和施药液量的改变不影响水稻植株上农药沉积分布特性,均为上层沉积量中层沉积量下层沉积量。当施药液量从300 L/hm~2增加到900 L/hm~2,4种喷头ST11001、ST11002、TR8001、TR8002喷雾在水稻基部的雾滴密度分别增加了8.21、8.54、7.79和9.69倍;但在相同施药液量下,4种喷头在水稻基部的雾滴密度没有显著差异。同一剂量下,喷头和施药液量不同组合的防治效果间差异显著。表明针对稻田不同防治对象,选择合适的喷头及施药液量将有助于提高农药沉积及防治效果。  相似文献   

Transport‐induced changes in hypothalamic–pituitary–interrenal axis gene expression and oxidative stress responses in Coilia nasus          下载免费PDF全文

Fukuan Du  Gangchun Xu  Jinwei Gao  Zhijuan Nie  Pao Xu  Ruobo Gu 《Aquaculture Research》2016,47(11):3599-3607

  相似文献   

植物收割对人工湿地基质酶活性的影响     

曾梦兆  李谷  吴恢碧  陶玲  姚雁鸿 《淡水渔业》2008,38(2):51-53,45

研究了7月份植物收割对人工湿地基质磷酸酶、脲酶、蛋白酶、脱氢酶活性及养殖废水中总氮(TN)、总磷(TP)、COD去除率的影响。结果显示:植物收割后磷酸酶、脲酶、蛋白酶活性开始增高,分别于第20天(13.7 mg/100 g)、第16天(1.9 mg/100 g)、第12天(61.7 mg/100 g)达到最大值,均于第28天(10.1 mg/100 g、1.1 mg/100 g、43.2 mg/100 g)恢复到收割前水平。脱氢酶活性在植物收割后第4天(142.3μL/100 g)降到最小值,此后开始增高,第16天(249.5μL/100 g)达到最大值,于第24天(195.6μL/100 g)恢复到收割前水平。净化效果研究表明,植物收割后TP、TN去除率开始增高,分别在植物收割后第20天(75.1%)、16天(60.6%)达到最大值,均于第28天(51.1%、34.1%)恢复到收割前水平。COD去除率在收割后第4天(25.3%)降到最小值,此后开始增高,第16天(70.2%)达到最高值,第24天(46.5%)恢复到收割前水平。  相似文献   

刺参南移与人工育苗试验   总被引：4，自引：0，他引：4  

肖树旭  顾功超 《水产学报》1981,5(2):147-154

本文报道了将刺参从山东南移到厦门的试验结果及在人工饲养条件下的生长、发育和度夏情况,并介绍了人工培育刺参幼体的几种方法。  相似文献   

池塘养殖尾水经稻田生态工程净化后的浮游细菌群落特征     

陶玲  李晓丽  朱建强  李谷 《淡水渔业》2017,47(1):71-77

为利用稻田生态工程对精养池塘尾水进行循环利用,采用Illumina Mi Seq第二代测序技术比较分析了稻田生态工程进出水中浮游细菌群落结构和多样性差异,以探讨稻田生态工程净化回用水中浮游细菌群落变化对池塘养殖的影响。结果显示,稻田生态工程进出水中优势浮游细菌在门水平上的组成相同,均为蓝细菌门(Cyanobacteria)、变形菌门(Proteobacteria)、放线菌门(Actinobacteria)、浮霉菌门(Planctomycetes)和拟杆菌门(Bacteroidetes)。但优势门类的相对丰度发生变化,蓝细菌门的相对丰度由进水中的46.72%显著降低至表面流出水中的41.82%和渗流出水中的34.77%;而放线菌门的相对丰度由3.90%增加至表面流出水中的5.65%和渗流出水中的6.45%。属水平上优势浮游细菌组成也相同,但微囊藻属(Microcystis)的相对丰度由0.83%显著降低至渗流出水中的0.46%(P0.05)。另外,稻田生态工程表面流出水中浮游细菌物种丰富度指数(Chao 1)显著提高,渗流出水中Shannon多样性指数显著提高,且Simpson指数显著降低(P0.05)。  相似文献   

转Bt-基因棉棉仁粉对鲤鱼营养价值的研究     

李谷  陈松  游文章  黄骏麒  吴建开  张震林  文华  周宝良 《水产科学》2000,19(5):6-9

为评估转Ｂｔ－基因棉棉仁粉用作鱼饲料的有效性和安全性,将其配成试验饲料进行了１４周鲤鱼喂养,前８周着重就鲤钱垢增重率、特定生长率、铒料系数、鱼体化学成分含量等营养学指标进行了观察。上述各项指标经统计分析,在试验组和对照组之间均无显著性差异。表明转Ｂｔ－基因棉棉仁粉经脱棉酚处理后,与常规棉棉仁粉一样可作鱼用饲料的蛋白源。  相似文献   

加州鲈迟缓爱德华氏菌病的检测和防治     

宣云峰  沈勇亮  杨小猛  曹勇  顾泽茂 《水产养殖》2014,35(10):8-10

以江苏省吴江市八坼镇区域养殖场加州鲈鱼病鱼的细菌性病原体为研究对象。通过分离纯化,形态学观察,结合16S rRNA基因序列同源性检索,对该病原菌进行初步判断。同时进行药敏实验,了解该病原菌对各种抗生素的耐药性和敏感程度。研究结果:分离纯化得到2株纯菌株L2F和L2P2,革兰染色均呈红色,阴性杆状菌。16S rDNA序列分析,L2F和L2P2菌株与迟缓爱德华氏菌(Edwardsiella tarda)的同源性达99%。初步判断该菌为迟缓爱德华氏菌。药敏实验结果,该菌对磺胺异恶唑、链霉素和利福平等药物不敏感或耐药,对左氧氟沙星、诺氟沙星、恩诺沙星、强力霉素、氟苯尼考、头孢哌酮相对敏感。  相似文献   

多棘海盘车用作新型海洋食品原料的可行性研究   总被引：3，自引：0，他引：3  

王长云  顾谦群  周鹏 《中国水产科学》1999,6(4):67-71

多棘海盘车（ Ａｓｔｅｒｉａｓ ａｍｕｒｅｎｓｉｓ） 在中国沿海居民中有长期食用的历史,其可食部为生殖腺（ 海星黄） ,但有麻辣感。海星黄含蛋白质达１５ ．４６ ％ ,其氨基酸组成齐全,必需氨基酸间比例合理。海星黄还富含微量元素、维生素、脂肪等营养元素,脂质中不饱和脂肪酸含量尤为丰富。海星黄麻辣味可能由硫酸酯甾体皂甙引起,大部分可通过脱麻辣味及脱毒操作除去。急性毒性试验中,小鼠灌胃８ 和１２ ｇ／ｋｇ 脱毒的海星黄,未见毒性反应;短期喂养试验（１２ ｇ／ｋｇ ,３０ ｄ） 也未见毒性反应。两项试验中,小鼠肝、心、肾、肺和脾均未见异常。建议人的最大无毒剂量１ ｇ／ｋｇ ,最大允许摄入剂量０ ．５ ｇ／ｋｇ 。海星黄经脱麻辣味及脱毒、调味等步骤,制得２ 种食品,具有较好的感观且营养丰富。海星壳所含蛋白质主要为胶原蛋白,以胃蛋白酶促溶蛋白为主,具有典型胶原蛋白氨基酸组成特点,可在食品工业用作明胶。初步结论为,多棘海盘车可用作高营养、无毒、加工利用性好的新型海洋食品原料。  相似文献