glochidiol

Glochidiol is an orally active tubulin polymerization inhibitor with an IC50 of 2.76 μM. Glochidiol shows anti-cancer activity[1].

Research Areas >> Cancer

Signaling Pathways >> Cell Cycle/DNA Damage >> Microtubule/Tubulin

Signaling Pathways >> Cytoskeleton >> Microtubule/Tubulin

IC50: 2.76 μΜ (tubulin polymerization)[1]

Glochidiol (1-8 μM; 48 h) 对肺癌细胞系显示出强效的抗增殖活性，且呈浓度依赖性[1]。 Glochidiol 通过靶向秋水仙碱结合位点与微管蛋白相互作用[1]。 Cell Proliferation Assay[1] Cell Line: NCI-H2087, HOP-62, NCI-H520, HCC-44, HARA, EPLC-272H, NCI-H3122, COR-L105 and Calu-6 Concentration: 1, 2, 4 and 8 μM Incubation Time: 48 h Result: Showed potent antiproliferative activity against lung cancer cell lines NCI-H2087, HOP-62, NCI-H520, HCC-44, HARA, EPLC-272H, NCI-H3122, COR-L105 and Calu-6 with IC50 values of 4.12 µM, 2.01 µM, 7.53 µM, 1.62 µM, 4.79 µM, 7.69 µM, 2.36 µM, 6.07 µM and 2.10 µM, respectively.

Glochidiol (60 mg/kg/day; i.g.; 21 days) 在裸鼠中有效抑制肺癌 HCC-44 异种移植瘤生长[1]。 Animal Model: BALB/c nude mice bearing HCC-44 xenografts[1] Dosage: 60 mg/kg/day Administration: Intragastric administration for a period of 21 days Result: Decreased average tumor weight and relative tumor volume with no obvious cytotoxic effect on the major organs, including heart, liver, and kidney.

[1]. Chen H, et al. Glochidiol, a natural triterpenoid, exerts its anti-cancer effects by targeting the colchicine binding site of tubulin. Invest New Drugs. 2021 Apr;39(2):578-586.