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| 1 | Preparation and evaluation of a new releasable PEGylated tumor necrosis factor-α(TNF-α) conjugate for therapeutic application显示文摘To design a releasable PEGylated TNF-α(rPEG-TNF-α ), a cathepsin B-sensitive dipeptide (Val-Cit moiety) was inserted into conventional PEG-modified TNF- (PEG-TNF- ), facilitating its clinical use for anti-tumor therapy. Comparative pharmaco- kinetic and pharmacodynamic studies showed that the half-lives of both PEGylated forms of TNF-α were ~60-fold greater than that of unmodified TNF-α . In addition, the in vitro bioactivity of rPEG-TNF-α was greater than that of PEG-TNF-α with the same degree of PEG modification. Release of TNF-α from rPEG-TNF-α in vitro was dependent on the presence of cathepsin B and was inhibited by a cathepsin B inhibitor. Despite the potent cytotoxicity of unmodified TNF-α against normal cells, its PEGylated forms at higher TNF-α concentrations showed low cytotoxic activity against these cells. In contrast, both forms of PEGylated TNF-α showed potent cytotoxic activity against the B16 and L929 cell lines, with rPEG-TNF-α being 5- and 9- fold more potent, respectively, than PEG-TNF-α . Moreover, rPEG-TNF-α was a more potent in vivo antitumor agent than PEG-TNF-α . | DAI ChuanYun FU Ya CHEN ShaoCheng LI Biao YAO Bo LIU WanHong ZHU LiQing CHEN Nan CHEN Ji ZHANG Qiang | 2013 | Science China(Life Sciences)2013，56，1： | 4 |
| 2 | Linkage with cathepsin B-sensitive dipeptide promotes the in vitro and in vivo anticancer activity of PEGylated tumor necrosis factor-alpha(TNF-α) against murine fibrosarcoma显示文摘To improve the pharmacological profile of tumor necrosis factor alpha(TNF-α),we have synthesized a new PEGylated prodrug,PEG-vcTNF-α,using a cathepsin B-sensitive dipeptide(valine-citrulline,vc) to link branched PEG and TNF-α.PEG-modified TNF-α without the dipeptide linker(PEG-TNF-α) and unconjugated TNF-α were also tested as controls.It was found for the first time that TNF-α released from PEG-vcTNF-α was specifically dependent on the presence of cathepsin B.PEG-vcTNF-α induced higher cytotoxicity and greater apoptosis against L929 murine fibrosarcoma cells than PEG-TNF-α.Reversal of these effects by a cathepsin-B inhibitor confirmed that these effects were mediated by cathepsin B-specific release of TNF-α.In vivo pharmacokinetics studies demonstrated that the plasma stability of PEG-vcTNF-α was significantly increased compared to TNF-α.Finally,the improved anticancer efficacy of PEG-vcTNF-α and the distinct activities among the three formulations confirmed the positive contribution of both PEGylation and the dipeptide linkage to the improved drug-like properties of PEG-vcTNF-α.The results here indicate that linking proteins and PEG via the cathepsin B-sensitive dipeptide may be a promising strategy for developing protein therapeutics. | DAI ChuanYun FU Ya LI Biao WANG YiGuang ZHANG Xuan WANG JianCheng ZHANG Qiang | 2011 | Science China(Life Sciences)2011，54，2： | 4 |
| 3 | Low ultrasonic stimulates fermentation of riboflavin producing strain Ecemothecium ashbyii 显示文摘 | Dai Chuanyun Wang Bochu Duan Chuanren | 2003 | Colloids Sur B : Biointerfaces2003，30，1： | 1 |
| 4 | SeDeM Expert System: A review and new perspectives显示文摘The SeDeM Expert System was first known as a galenic pre-formulation system, which was based on the experimental research and quantitative determination of powdered substances. And the mathematical formula provided by the SeDeM Expert System has plays an important role in the study of powder properties. The system can be used not only to evaluate the powder direct compression (DC) of excipients and active pharmaceutical ingredients (API’s), but also to predict the possible formulations, so it can reduce unnecessary research and trials, and shorten the time of development. In this paper, the research development and application of SeDeM Expert System in DC was summarized, and the results showed that with a few exceptions, the system was skilled in predicting acceptable tablet formulations. Finally, the new application prospect of the system is presented, including the application of the Internet traffic and content management (iTCM) database and the new co-processed excipients. | Mingxian Gu Tianbing Guan Shulin Wan Han Zhang Xuelian Li Songtao Kong Jianbing Ren Huimin Sun Chuanyun Dai | 2019 | Journal of Pharmaceutical and Biopharmaceutical Research2019，1，1： | 1 |
| 5 | Optimization of preparative separation and purification of total flavonoids from Radix Puerariae by macroporous resin method 显示文摘 | LIU Huoan WANG Bochu DAI Chuanyun | 2006 | J Chn Pharrnaceut Sci2006，15，2： | 1 |
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