PDF(Pubmed)
Abstract：
UNASSIGNED: Cephaeline is a natural product isolated from ipecac (Cephaelis ipecacuanha [Brot.] A. Rich. [Rubiaceae]). It exhibits promising anti-lung cancer activity and ferroptosis induction may be a key mechanism for its anti-lung cancer effect.
UNASSIGNED: This study investigates the anti-lung cancer activity and mechanisms of cephaeline both in vitro and in vivo.
UNASSIGNED: H460 and A549 lung cancer cells were used. The cephaeline inhibition rate on lung cancer cells was detected via a Cell Counting Kit-8 assay after treatment with cephaeline for 24 h. Subsequently, the concentrations of 25, 50 and 100 nM were used for in vitro experiments. In addition, the antitumour effects of cephaeline (5, 10 mg/kg) in vivo were evaluated after 12 d of cephaeline treatment.
UNASSIGNED: Cephaeline showed significant inhibitory effects on lung cancer cells, and the IC50 of cephaeline on H460 and A549 at 24, 48 and 72 h were 88, 58 and 35 nM, respectively, for H460 cells and 89, 65 and 43 nM, respectively, for A549 cells. Meanwhile, we demonstrated that ferroptosis is the key mechanism of cephaeline against lung cancer. Finally, we found that cephaeline induced ferroptosis in lung cancer cells by targeting NRF2.
UNASSIGNED: We demonstrated for the first time that cephaeline inhibits NRF2, leading to ferroptosis in lung cancer cells. These findings may contribute to the development of innovative therapeutics for lung cancer.
UNASSIGNED: This study investigates the anti-lung cancer activity and mechanisms of cephaeline both in vitro and in vivo.
UNASSIGNED: H460 and A549 lung cancer cells were used. The cephaeline inhibition rate on lung cancer cells was detected via a Cell Counting Kit-8 assay after treatment with cephaeline for 24 h. Subsequently, the concentrations of 25, 50 and 100 nM were used for in vitro experiments. In addition, the antitumour effects of cephaeline (5, 10 mg/kg) in vivo were evaluated after 12 d of cephaeline treatment.
UNASSIGNED: Cephaeline showed significant inhibitory effects on lung cancer cells, and the IC50 of cephaeline on H460 and A549 at 24, 48 and 72 h were 88, 58 and 35 nM, respectively, for H460 cells and 89, 65 and 43 nM, respectively, for A549 cells. Meanwhile, we demonstrated that ferroptosis is the key mechanism of cephaeline against lung cancer. Finally, we found that cephaeline induced ferroptosis in lung cancer cells by targeting NRF2.
UNASSIGNED: We demonstrated for the first time that cephaeline inhibits NRF2, leading to ferroptosis in lung cancer cells. These findings may contribute to the development of innovative therapeutics for lung cancer.
摘要：
■Cephaeline是从吐根（Cephaelisipecacuanha[Brot。]A.富有。[茜草科]）。它显示出有希望的抗肺癌活性，铁凋亡诱导可能是其抗肺癌作用的关键机制。
■本研究在体外和体内研究了cephaeline的抗肺癌活性和机制。
■使用H460和A549肺癌细胞。通过细胞计数试剂盒-8测定,在用cephaeline处理24小时后,检测了cephaeline对肺癌细胞的抑制率。25、50和100nM的浓度用于体外实验。此外,在接受了12d的cephaeline治疗后，评估了cephaeline（5，10mg/kg）的体内抗肿瘤作用。
■Cephaeline对肺癌细胞有明显的抑制作用，在24、48和72h时，cephaeline对H460和A549的IC50分别为88、58和35nM，分别,对于H460细胞和89、65和43nM，分别,A549细胞。同时,我们证明铁凋亡是cephaeline抗肺癌的关键机制。最后,我们发现，通过靶向NRF2，cephaeline在肺癌细胞中诱导铁凋亡。
■我们首次证明了头孢碱抑制NRF2，导致肺癌细胞中的铁凋亡。这些发现可能有助于肺癌创新疗法的发展。
■本研究在体外和体内研究了cephaeline的抗肺癌活性和机制。
■使用H460和A549肺癌细胞。通过细胞计数试剂盒-8测定,在用cephaeline处理24小时后,检测了cephaeline对肺癌细胞的抑制率。25、50和100nM的浓度用于体外实验。此外,在接受了12d的cephaeline治疗后，评估了cephaeline（5，10mg/kg）的体内抗肿瘤作用。
■Cephaeline对肺癌细胞有明显的抑制作用，在24、48和72h时，cephaeline对H460和A549的IC50分别为88、58和35nM，分别,对于H460细胞和89、65和43nM，分别,A549细胞。同时,我们证明铁凋亡是cephaeline抗肺癌的关键机制。最后,我们发现，通过靶向NRF2，cephaeline在肺癌细胞中诱导铁凋亡。
■我们首次证明了头孢碱抑制NRF2，导致肺癌细胞中的铁凋亡。这些发现可能有助于肺癌创新疗法的发展。
