with the prevalence of every type of cancer increasing globally, the inability to treat and the severe side effects caused by chemotherapy and radiotherapy are some of the biggest problems facing cancer patients and their physicians.1many herbal medicines have replaced their chemical rivals; for example, emetine lost its ground to metronidazole as an amoebicidal agent, and digoxin has given its...

Microtubules (MTs) are key components of the cytoskeleton for all eukaryotes and are vital for cellular processes such as mitotic spindle formation, intracellular transport, vesicle formation, cellular signaling, and migration. These functions depend on the dynamic nature of MTs, which arises from the polymerization and depolymerization events of individual heterodimers, made up of αand β-tubul...

BACKGROUND Prostate cancer is the second leading cause of cancer death among men. Multiple evidence suggests that a population of tumor-initiating, or cancer stem cells (CSCs) is responsible for cancer development and exceptional drug resistance, representing a highly important therapeutic target. The present study evaluated CSC-specific alterations induced by new-generation taxoid SBT-1214 and...

The main aim of this study was to evaluate the therapeutic efficacy of an oil-in-water nanoemulsion formulation encapsulating DHA-SBT-1214, a novel omega-3 fatty acid conjugated taxoid prodrug, against prostate cancer stem cells. Nanoemulsions of DHA-SBT-1214 (NE-DHA-SBT-1214) were prepared and characterized. In vitro delivery efficiency and cytotoxicity of NE-DHA-SBT-1214 was compared with sol...

Breast cancer is the leading cause of cancer death among women. Paclitaxel, a mitotic inhibitor, is highly effective in the treatment of breast cancer. However, development of resistance to paclitaxel limits its clinical use. Identifying new compounds and new strategies that are effective against breast cancer, in particular drug-resistant cancer, is of great importance. the aim of the present ...

Zampanolide, first discovered in a sponge extract in 1996 and later identified as a microtubule-stabilizing agent in 2009, is a covalent binding secondary metabolite with potent, low nanomolar activity in mammalian cells. Zampanolide was not susceptible to single amino acid mutations at the taxoid site of β-tubulin in human ovarian cancer 1A9 cells, despite evidence that it selectively binds to...

A central feature in the biosynthesis of Taxol is oxygenation at multiple positions of the taxane core structure, reactions that are considered to be mediated by cytochrome P450-dependent monooxygenases. A PCR-based differential display-cloning approach, using Taxus (yew) cells induced for Taxol production, yielded a family of related cytochrome P450 genes, one of which was assigned as a taxane...

BACKGROUND XRP6258 is a novel taxoid with a low affinity for P-glycoprotein. This multicenter phase II study assessed the activity of XRP6258 in the treatment of taxane-resistant metastatic breast cancer (MBC). PATIENTS AND METHODS XRP6258 was administered as a 1-h i.v. infusion every 3 weeks at 20 mg/m(2) (then, in the absence of severe toxicity, at 25 mg/m(2) from cycle 2). The primary end ...

The metabolism of docetaxel by human liver microsomes was investigated in vitro and compared with that of paclitaxel. A main docetaxel metabolite was generated by human liver microsomes in the presence of NADPH: retention time in high pressure liquid chromatography and its ion fragmentation in mass spectrometry were identical to those of the authentic derivative hydroxylated at the butyl group ...

s and the ICI Web of Science from November 1, 1999 to November 1, 2001. The literature search was augmented by consulting Analytical Abstracts, and the following journals publishing papers on TLC were searched directly: Journal of Chromatography (parts A and B and the bibliography issues), Journal of Chromatographic Science, Chromatographia, Analytical Chemistry, Journal of Liquid Chromatograph...