榄香素和榄香酮可诱导小细胞肺癌和大细胞肺癌细胞系的细胞周期停滞和凋亡。

Eurycomanol and eurycomanone as potent inducers for cell-cycle arrest and apoptosis in small and large human lung cancer cell lines.

机构信息

Pharmacognosy Department, Cairo University, Cairo, Egypt.

Department of Botany and Microbiology, Al-Azhar University, Cairo, Egypt.

出版信息

Nat Prod Res. 2023 Jun;37(11):1856-1862. doi: 10.1080/14786419.2022.2119387. Epub 2022 Sep 2.

DOI:10.1080/14786419.2022.2119387

PMID:36054770

Abstract

Jack is one of traditional herbal medicines in South-East Asia. This study evaluated the anticancer, cell-cycle arrest, and apoptotic induction potentials of eurycomanone (EONE) and eurycomanol (EOL), highly oxygenated quassinoids previously isolated from its roots, against large (H460) and small (A549) lung cancer cells. EOL and EONE exhibited IC of 386 and 424 µg/mL on normal human lung cell line. EONE exhibited higher anticancer activity with an IC of 1.78 µg/mL and 20.66 μg/mL than EOL which exhibited an IC of 3.22 µg/mL and 38.05 µg/mL against H460 and A549, respectively. Both reduced the viability of H460 and A549 and arrested G0/G1 phase. The increase in the apoptotic rates was mainly in the percentage of late apoptosis. Moreover, they inhibited A549 by inducing the accumulation of S and G2/M phases. This study revealed EOL and EONE potential as novel leads exhibiting cell-cycle arrest and apoptosis induction potentials.

摘要

杰克是东南亚的一种传统草药。本研究评估了 previously isolated from its roots（从其根部分离出的）高度氧化的 quassinoids（苦木苦味素）eurycomanone（EONE）和 eurycomanol（EOL）对大（H460）小（A549）肺癌细胞的抗癌、细胞周期停滞和凋亡诱导潜力。EOL 和 EONE 在正常人类肺细胞系中的 IC 为 386 和 424 µg/mL。EONE 表现出更高的抗癌活性，其对 H460 和 A549 的 IC 分别为 1.78 µg/mL 和 20.66 µg/mL，而 EOL 的 IC 分别为 3.22 µg/mL 和 38.05 µg/mL。两者均降低了 H460 和 A549 的活力并使 G0/G1 期停滞。凋亡率的增加主要在晚期凋亡的百分比中。此外，它们通过诱导 S 和 G2/M 期的积累来抑制 A549。本研究揭示了 EOL 和 EONE 作为具有细胞周期停滞和凋亡诱导潜力的新型先导化合物的潜力。