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Abstract Title:

Sesquiterpenoids isolated from the flower of Inula japonica as potential antitumor leads for intervention of paclitaxel-resistant non-small-cell lung cancer.

Abstract Source:

Bioorg Chem. 2020 08 ;101:103973. Epub 2020 May 24. PMID: 32521367

Abstract Author(s):

Yahui Ding, Tianpeng Wang, Tianyang Chen, Chunfeng Xie, Quan Zhang

Article Affiliation:

Yahui Ding

Abstract:

Three new sesquiterpene lactone dimers (1-3) were isolated from the flowers of Inula japonica together with twenty-two known sesquiterpene derivatives (4-25). Their structures were established on the basis of detailed spectroscopic analyses. All isolates were evaluated for their antiproliferative activities against paclitaxel-resistant human non-small-cell lung cancer cell line A549/PTX. The preliminary structure-activity relationship was discussed. Compound 24 exhibited the most potent effect with the ICvalue of 0.34 ± 0.10 μM, even more active than the clinically used drug paclitaxel (PTX, IC = 1.40 ± 0.52 μM). Compound 24 showed significant efficacy of arresting the cell cycle at the G2-M stage, inducing apoptosis through mitochondria-mediated pathway, and inhibiting cell migration and invasion. Furthermore, compound 24 could reverse multidrug resistance through suppressing theexpression of ABC family proteins.

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Sayer Ji
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