Preparation and evaluation of a new releasable PEGylated tumor necrosis factor-α (TNF-α) conjugate for therapeutic application.

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-α (PEG-TNF-α), facilitating its clinical use for anti-tumor therapy. Comparative pharmacokinetic 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.

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.

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.

[Determination of the contents of chlorogenic acid and phillyrin of Shuanghuanglian oral fluid using NIRS].

The aim of the present study was to establish the model of predicting the contents of chlorogenic acid and phillyrin in Shuanghuanglian oral fluid using NIR to realize quick quality evaluation of Shuanghuanglian oral fluid. To this end, many batches of Shuanghuanglian oral fluid were selected, and the contents of chlorogenic acid and phillyrin were determined using HPLC. Meanwhile, the NIR spectra of the same samples were determined.