Progress in Isoindolone Alkaloid Derivatives from Marine Microorganism: Pharmacology,Preparation, and Mechanism

Compound 1 (SMTP-7, also FGFC1), an isoindolone alkaloid from marine fungi Starchbotrys longispora FG216 and fungi Stachybotrys microspora IFO 30018, possessed diverse bioactivities such as thrombolysis, anti-inflammatory and anti-oxidative properties, and so on. It may be widely used for the treatment of various diseases, including cerebral infarction, stroke, ischemia/reperfusion damage, acute kidney injury, etc. Especially in cerebral infarction, compound 1 could reduce hemorrhagic transformation along with thrombolytic therapy, as the traditional therapies are accompanied with bleeding risks. In the latest studies, compound 1 selectively inhibited the growth of NSCLC cells with EGFR mutation, thus demonstrating its excellent anti-cancer activity. Herein, we summarized pharmacological activities, preparation of staplabin congeners—especially compound 1—and the mechanism of compound 1, with potential therapeutic applications.     

Reversal effect of FG020318 on multidrug resistance in retinoblastoma cell line SO-Rb50

AIM: To investigate the multidrug resistance (MDR),reversal activity of 2-［4-(2-pyridin-2-yl-vinyl) henyl］-4,5-bis-(4-N,N-diethylaminophenyl)-1 (H)-imidazole (FG020318) in a retinoblastoma subline SO-Rb50/VCR,which is resistant to vincristine.METHODS: The procedure of stepwise increase in drug concentrations was used to obtain SO-Rb50/VCR,which was resistant to 200 μg/L vincristine.The chemosensitivity of this drug resistant cell line with and without FG020318 or cyclosporine A (CSA) were detected by MTT assay and the function of p-glycoprotein (P-gp) was examined by rhodamine 123 accumulation detected with flow cytometry (FCM).RESULTS: FG020318 (2.5 μmol/L) significantly reduced IC50 and increased the rhodamine accumulation in a concentration-dependent manner.It was much stronger than the positive control CSA in reversal of MDR.CONCLUSION: A new tumor MDR modulator FG020318 partly reverses MDR in SO-Rb50/VCR.It may be a promising new drug to tackling MDR.     

鸡蛋游离棉酚残留与蛋鸡日粮棉酚水平及饲喂期限的关系

【目的】研究鸡蛋游离棉酚(FG)残留与蛋鸡日粮棉酚水平及饲喂期限的关系。【方法】选480只30周龄健康的海兰褐蛋鸡随机等分为5个处理组,每个处理组设6个重复。预饲期1周,试验期24周。试验设玉米-豆粕基础日粮组(对照组)及含50,100,150,200g/kg棉粕日粮组(FG含量分别为43.15,86.30,129.45,172.60mg/kg),研究高棉粕饲粮对蛋鸡生产性能、蛋品质以及鸡蛋FG残留量的影响。【结果】用不同棉粕水平日粮饲喂蛋鸡24周,当日粮FG含量达到129.45mg/kg时,能显著降低产蛋率、平均蛋质量和日采食量,料蛋比显著升高;当日粮FG含量达到172.60mg/kg时,能显著降低蛋壳强度和蛋黄颜色。鸡蛋FG残留测定结果表明,试验第12周,当蛋鸡每日平均FG摄入量分别为5.29,10.26,15.04,19.09mg时,鸡蛋FG残留分别为20.64,31.86,39.13,43.32mg/kg;试验第24周,当蛋鸡每日平均FG摄入量分别为5.02,9.83,14.24,17.55mg时,鸡蛋FG残留分别为27.38,42.40,45.17,53.44mg/kg。【结论】日粮棉粕添加量不宜超过100g/kg,否则会影响蛋鸡生产性能和蛋品质;鸡蛋中FG残留量随FG摄入量的增加而增加;随着饲养期限的延长,鸡蛋中FG残留率提高。     

Characterisation of starch during germination and seedling development of a rice mutant with a high content of resistant starch

To acquire a better understanding of whether RS influences the dynamics of in vivo starch digestion and seed vigour, the high-RS rice mutant RS4 (RS ca. 10%) and the wild type R7954 were used to investigate total amylase activity, seedling vigour, starch content and starch granule structure during germination. RS4 exhibited similar seed vigour to R7954. Amylose and amylopectin in R7954 showed synchronous degradation throughout the whole process, while amylopectin was hydrolysed significantly faster than amylose in RS4 during the earlier germination stages. The starch residues of RS4 after germination (GD) lost endotherm peaks and showed a special X-ray diffraction pattern with only two peaks at around 16.90° and 21.62°, probably due to remnants of amylopectin and its tight crosslinking with the cell wall. The remaining starch after 10 GD, primarily amylopectin may make a critical contribution to total resistant starch content. These results indicated that RS had no negative impact on seed vigour in rice lines, although RS cannot be hydrolysed by α-amylase from human and animal in vitro. By appropriately increasing the special amylopectin fraction, a new breeding programme of high RS crops and improvement in the eating quality of high RS rice varieties might be achieved.     

牙鲆NOD2基因的表达分析及在抗迟缓爱德华氏菌感染过程中的功能

本研究利用实验室已建牙鲆(Paralichthys olivaceus)转录组数据库预测得到牙鲆NOD2基因(PoNOD2),并利用PCR技术进行序列验证。同时,设计迟缓爱德华氏菌注射感染牙鲆成鱼和体外免疫刺激牙鲆鳃细胞系实验,探究PoNOD2基因在抗菌免疫反应中的作用。PoNOD2基因的开放阅读框长度为2964 bp,编码988个氨基酸。PoNOD2蛋白有3种保守结构域,包括C-末端LRR,中心NACHT和N-末端CARD结构域。实时荧光定量PCR结果显示,在所检测牙鲆组织中,迟缓爱德华氏菌的侵染能显著上调PoNOD2的表达。体外免疫刺激牙鲆鳃细胞系实验显示,在PGN、PolyⅠ:C和迟缓爱德华氏菌刺激下,PoNOD2表达上调。亚细胞定位显示,PoNOD2蛋白定位于牙鲆鳃细胞的细胞质中。在迟缓爱德华氏菌侵染牙鲆鳃细胞过程中,PoNOD2基因的过表达能够抑制细菌生长,并引起IL-1β、IL-6和IL-8等炎性细胞因子的表达上调。结果表明,PoNOD2在抑制迟缓爱德华氏菌生长以及调节牙鲆对病原菌的免疫应答中发挥重要作用。     

高堰式双螺旋分级机螺旋轴组焊新工艺的研究

以2FG12高堰式双螺旋分级机为例,介绍螺旋轴组焊制造新工艺,在保证产品质量要求的前提下,用在空心轴上氧割三条槽,并在槽上焊装螺母来调整圆跳动再分段焊接的工艺方案,替代细长轴装配焊接的传统制作工艺,解决了传统工艺制造中存在的同轴度要求高、圆跳动大、制造困难的问题.