Innovation Center of Molecular Diagnostics, College of Life Science and Technology, Beijing University of Chemical Technology, Beijing, China.
Key Laboratory of Protection and Utilization of Biological Resources in Tarim Basin of Xinjiang Production and Construction Corps, College of Life Science and Technology, Tarim University, Alar, China.
Chem Biol Drug Des. 2023 Jun;101(6):1252-1261. doi: 10.1111/cbdd.14207. Epub 2023 Feb 15.
Ligustilide (LIG), the bioactive constituent of Angelica sinensis, may exert potential benefits in cancer treatment. However, the potential mechanism of LIG in the suppression of bladder cancer (BC) has not been reported yet. This study uncovered the inhibitory effect of LIG on the proliferation and cell cycle arrest of BC cells (T24 and EJ-1) along with unveiling the underlying molecular mechanism. The IC values of LIG-treated T24 for 24 and 48 h are 39.91 μg/mL (209.8 μM) and 40.94 μg/mL (215.2 μM) separately. The same conditions, the IC values of EJ-1 are 45.73 μg/mL (240.4 μM) and 43.81 μg/mL (230.3 μM), separately. Additionally, LIG induced apoptosis and cycle arrest of T24 and EJ-1 cells in sub-G1 phase. Further studies showed that LIG induced apoptosis of BC cells by upregulating Caspase-8, truncated BID (tBID) and BAX proteins, and downregulating NFκB1 (p50) protein. In conclusion, LIG significantly inhibits the growth of BC cells in vitro and in vivo by inducing apoptosis and is inexpensive, making it a promising candidate for novel anti-BC drugs.
藁本内酯（LIG）是当归的生物活性成分，可能在癌症治疗中发挥潜在益处。然而，LIG 抑制膀胱癌（BC）的潜在机制尚未报道。本研究揭示了 LIG 对 BC 细胞（T24 和 EJ-1）增殖和细胞周期阻滞的抑制作用，并揭示了其潜在的分子机制。LIG 处理 T24 24 和 48 h 的 IC 值分别为 39.91 μg/mL（209.8 μM）和 40.94 μg/mL（215.2 μM）。相同条件下，EJ-1 的 IC 值分别为 45.73 μg/mL（240.4 μM）和 43.81 μg/mL（230.3 μM）。此外，LIG 诱导 T24 和 EJ-1 细胞在 sub-G1 期的凋亡和细胞周期阻滞。进一步的研究表明，LIG 通过上调 Caspase-8、截断的 BID（tBID）和 BAX 蛋白，下调 NFκB1（p50）蛋白，诱导 BC 细胞凋亡。总之，LIG 通过诱导细胞凋亡显著抑制 BC 细胞的体外和体内生长，且价格低廉，有望成为新型抗 BC 药物的候选药物。
