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7-Epi 10-Desacetyl Paclitaxel The report

Cell Cycle/DNA Damage

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#1 mcechina



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Posted 20 October 2014 - 11:05 PM

Biological Activity of 7-Epi 10-Desacetyl Paclitaxel

7-Epi 10-Desacetyl Paclitaxel is a derivative of Paclitaxel, which is a microtubule polymer stabilizer with IC50 of 0.1 pM in human endothelial cells.
IC50 Value: 0.1 pM (Paclitaxel)
Target: microtubule; Bcl-2
in vitro: Paclitaxel inhibits non-endothelial type human cells at 104 - to 105 -fold higher concentrations, with IC50 of 1 nM-10 nM. The selectivity of Paclitaxel inhibition of cell proliferation is also species specific, as mouse ECs are not sensitive to Paclitaxel at ultra low concentrations. Inhibition of human ECs by Paclitaxel at ultra low concentrations does not affect the cellular microtubule structure, and the treated cells do not show G2/M cell cycle arrest and apoptosis, suggesting a novel but as yet unidentified mechanism of action. In an in vitro angiogenesis assay, Paclitaxel at ultra low concentrations blocks human ECs from forming sprouts and tubes in the three-dimensional fibrin matrix. In the presence of SMF, the efficient concentration of Paclitaxel on K562 cells is decreased from 50 to 10 ng/mL. The cell cycle arrest effect of Paclitaxel with or without SMF on K562 cells is correlated with DNA damage. Paclitaxel alone causes a time-dependent inhibition of CDK1 in four cell lines including A549 cells, H358, H1395 cells and H1666 cells.
in vivo: The inhibition rations of Paclitaxel alone on BC-V and BC-ER tumors are 49.78% and 51.23%, respectively. Treatment of six cycles of 20 mg/kg Paclitaxel significantly reduces the percentages of Ki-67-positive cells to 20.4% in BC-V tumors and 25.1% in BC-ER tumors, respectively.

References on 7-Epi 10-Desacetyl Paclitaxel

[1]. Weber B, Largillier R, Ray-Coquard I, et al. A potentially neuroprotective role for erythropoietin with paclitaxel treatment in ovarian cancer patients: a prospective phase II GINECO trial. Support Care Cancer. 2013 Feb 19.
[2]. Pan Z, Gollahon L. Paclitaxel attenuates Bcl-2 resistance to apoptosis in breast cancer cells through an endoplasmic reticulum-mediated calciumrelease in a dosage dependent manner. Biochem Biophys Res Commun. 2013 Feb 13. pii: S0006-291X(13)00259-3.
[3]. Habib S, Delourme J, Dhalluin X, et al. Bevacizumab and weekly paclitaxel for non-squamous non small cell lung cancer patients: A retrospective study. Lung Cancer. 2013 Feb 13. pii: S0169-5002(13)00025-1.
[4]. Park SJ, Wu CH, Gordon JD, et al. Taxol induces caspase-10-dependent apoptosis. J Biol Chem. 2004 Dec 3;279(49):51057-67. Epub 2004 Sep 27.
[5]. Rao S, He L, Chakravarty S, et al. Characterization of the Taxol binding site on the microtubule. Identification of Arg(282) in beta-tubulin as the site of photoincorporation of a 7-benzophenone analogue of Taxol. J Biol Chem. 1999 Dec 31;274(53):37990-4.
[6]. Paclitaxel
Contact us:http://www.medchemex...Paclitaxel.html

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