Diphtheria toxin (DTx) is an extremely potent inhibitor of protein synthesis. Cell death has been generally accepted as a straightforward effect of translation inhibition. Using human U937 cells, we found that DTx intoxication leads to cytolysis; indeed, release of 51Cr- and 75Se-labeled proteins could be detected within 7 h. However, little or no cell lysis was observed over a 20-50-h period w...

Docetaxel (DTX) is a very important member of taxoid family. Despite several alternative delivery systems reported recently, DTX formulated by Polysorbate 80 and alcohol (Taxotere®) is still the most frequent administration in clinical practice. In this study, we incorporated DTX into Polysorbate 80/Phospholipid mixed micelles and compared its structural characteristics, pharmacokinetics, biodi...

Microvesicles shed from cells carry constituents of the cell cytoplasm, including, of importance in multidrug resistance to cancer chemotherapy, drugs that the tumor cell attempts to efflux. To see whether such drugs could be used at lower concentrations with the same efficacy, it was first shown that microvesiculation of prostate cancer (PCa) cells, PC3, could be inhibited pharmacologically wi...

The blockade of K+ channels and enhancement of neuromuscular transmission by dendrotoxin (DTX), a convulsant peptide from mamba snake venom, were examined in normal and mutant larval preparations of Drosophila. Two-microelectrode voltage-clamp experiments showed that DTX reduced the transient K+ current, IA, in muscle membrane. This effect was suppressed by raising the Mg2+ concentration or by ...

We describe here three different hamster cell mutants which are resistant to diphtheria toxin and which provide models for investigating some of the functions required by the toxin inactivates elongation factor 2 (EF-2). Cell-free extracts from mutants Dtx(r)-3 was codominant. The evidence suggests that the codominant phenotype is the result of a mutation in a gene coding for EF-2. The recessiv...

Ceramide (CE)-based combination therapy (CE combination) as a novel therapeutic strategy has attracted great attention in the field of anti-cancer therapy. The principal purposes of this study were to investigate the synergistic effect of CE in combination with docetaxel (DTX) (CE + DTX) and to explore the synergy mechanisms of CE + DTX. The 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium ...

Peritoneal carcinomatosis (PC) of gastric origin has a poor prognosis with short survival due to lack of effective therapeutic modalities. Here, we evaluated the therapeutic efficacy of an injectable thermosensitive poly (organophosphazene) (PPZ) hydrogel with docetaxel (DTX-gel) to develop an effective therapeutic agent for patient with PC. Three days after inoculation of highly metastatic 44A...

In the present work, docetaxel (DTX) and retinoic acid (RA) co-loaded micelles were developed for synergistic prostate cancer therapy. PEG-RA RA-PEG-RA synthesized subsequently used loading of DTX RA. The as prepared DTX/RA@RA-PEG-RA exhibit smaller size higher drug capacity compared to DTX/RA@PEG-RA micelles. in vitro release study shows that similar behaviours which exhibits fast RA sustained...

DTX, a single-chain polypeptide of M, 7000 from the venom of the eastern green mamba Dendroaspis angusticeps, has been shown to facilitate transmitter release at the neuromuscular junction (Harvey & Karlsson, 1982) and in the central nervous system (Docherty et al., 1983). It is highly toxic when administered centrally (Dolly et al., 19831, producing a convulsant action arising from its facilit...

Amphiphilic block copolymers have attracted a great deal of attention in drug delivery systems. In this work, a series of monomethoxy-poly (ethylene glycol)-poly (ε-caprolactone-co-D,L-lactide) (MPEG-PCLA) copolymers with variable composition of poly (ε-caprolactone) (PCL) and poly (D,L-lactide) (PDLLA) were prepared via ring-opening copolymerization of ε-CL and D,L-LA in the presence of MPEG a...