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Synthesis and evaluation of [14C]-Labelled and fluorescent-Tagged paclitaxel derivatives as new biological probes by Ch.Srinivasa Rao; ab Jao-Jia Chu; Rai-Shung Liu; Yiu-Kay Lai is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.
What is Synthesis and evaluation of [14C]-Labelled and fluorescent-Tagged paclitaxel derivatives as new biological probes about?
Our present report deals with the preparation of hitherto unreported 7-([carbonyl-14C]-acetyl)paclitaxel 4 and two new bioactive 7-substituted fluorescent taxoids (FITC 9 and rhodamine 11), as well as evaluation towards their applications as biological probes. The results in this report demonstrate that (a) the new paclitaxel derivatives 4, 9, 11 could be prepared with good yields starting from paclitaxel; (b) the [14C]acetylation step was found to be better by using [14C]acetic anhydride rather than [14C]sodium acetate; (c) the radiochemical purity of 4 was 96% and its specific activity was 48 mCi/mmol; (d) the cytotoxicity of 4 was close to that of paclitaxel whereas 9, 11 were far less active than paclitaxel, but these cytotoxic levels were good enough for their biological applications; (e) the drug-quantitation by flow cytometric analysis using 9 and 11 was proved to be equally efficient with respect to the radioactivity-based determination employing 4; (f) the intracellular fluorescence mapping by 9 and 11 was found to be effective and the microtubule network pattern was visible in both the cases; (g) the overall fluorescence imaging efficiency was better with 11 while the int
Who reads Synthesis and evaluation of [14C]-Labelled and fluorescent-Tagged paclitaxel derivatives as new biological probes?
It is typically read by researchers, students, and practitioners in Biochemistry, Genetics and Molecular Biology.
- Author
- Ch.Srinivasa Rao; ab Jao-Jia Chu; Rai-Shung Liu; Yiu-Kay Lai
- Publisher
- Elsevier Science; Elsevier ; Elsevier Ltd.; Elsevier BV (ISSN 0968-0896)
- Published
- 1998
- Language
- EN
- Field
- Biochemistry, Genetics and Molecular Biology (Life Sciences)