Taccalonolide A

Taccalonolide A, a steroid found in Tacca chantrieri, is a microtubule stabilizer. Taccalonolide A promotes tubulin polymerization, stabilizes microtubules, and shows little cross-resistance with Paclitaxel (HY-B0015) in cell lines with β-tubulin Paclitaxel-binding region mutations. Taccalonolide A is transported less efficiently by P-glycoprotein. Taccalonolide A induces increased cellular microtubule density, thick interphase microtubule bundles, abnormal multipolar mitotic spindles, G₂-M phase cell cycle accumulation, Bcl-2 phosphorylation, and apoptosis. Taccalonolide A inhibits cell proliferation in drug-sensitive and multidrug-resistant cell lines. Taccalonolide A has cytotoxic and antimalarial activities. Taccalonolide A can be used for the researches of ovarian cancer and infection^[1][2]. IC50 & Target:microtubule^[1] In Vitro:Taccalonolide A (1-10 μM; 18 h) induces concentration-dependent Paclitaxel-like microtubule reorganization in A-10 cells, including increased microtubule density, thick bundle formation, and short, centrosome-independent tufts^[1].
Taccalonolide A (1-5 μM; 18 h) induces concentration-dependent formation of multipolar mitotic spindles with failed DNA alignment in A-10 and HeLa cells^[1].
Taccalonolide A (2.59-8.89 μM; 48 h) inhibits proliferation of drug-sensitive and drug-resistant cancer cell lines with IC₅₀ values ranging from 2.59 μM to 8.89 μM after 48 h of incubation, showing minimal cross-resistance to Paclitaxel (HY-B0015)- and epothilone-resistant cell lines and reduced P-glycoprotein-mediated resistance relative to Paclitaxel^[1].
Taccalonolide A (1-5 μM; 18 h) induces micronucleation in interphase A-10 and HeLa cells^[1].
Taccalonolide A (6-24 h) induces G₂-M phase arrest, failed cytokinesis, and apoptotic cell death in MDA-MB-435 cells within 24 h of treatment at the IC₈₅ concentration^[1].
Taccalonolide A (4-30 h) induces Bcl-2 phosphorylation starting at 4 h and caspase-mediated PARP cleavage (a marker of apoptosis) starting at 12 h in MDA-MB-435 cells treated at the IC₈₅ concentration for up to 30 h^[1].