Lobetyol

Lobetyol is a natural compound that can be isolated from Lobelia chinensis. Lobetyol induces apoptosis and cell cycle arrest in MKN45 cells. Lobetyol shows anti-virus, anti-inflammation and anti-tumor activity[1][2].

Signaling Pathways >> Apoptosis >> Bcl-2 Family

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

Research Areas >> Infection

Signaling Pathways >> Apoptosis >> MDM-2/p53

Research Areas >> Inflammation/Immunology

Bax

Bcl-2

Lobetyol (0-100 μg/mL, 0-48 h) 在 MKN45 细胞中导致剂量和时间依赖性增殖抑制[1]。 Lobetyol (0-100 μg/mL, 48 h) 以时间和剂量依赖的方式诱导 MKN45 细胞细胞凋亡和细胞周期停滞[1]。 Lobetyol (0-100 μg/mL, 48 h) 增加 Bax、P53 的表达水平，降低 Bcl-2 的表达水平[1]。 Cell Proliferation Assay[1] Cell Line: MKN45 cells Concentration: 0 μg/mL, 50 μg/mL, 75 μg/mL, 100 μg/mL Incubation Time: 12 h, 24 h, 48 h Result: Showed a dose-and time-dependent proliferation inhibition in MKN45 cells, with an IC50 of 71.47 ± 4.29 μg/mL at 48 h. Exhibited more safety on L02 and HEK293 human normal cell lines. Apoptosis Analysis[1] Cell Line: MKN45 cells Concentration: 0 μg/mL, 50 μg/mL, 75 μg/mL, 100 μg/mL Incubation Time: 48 h Result: Increased the apoptotic population in MKN45 cells in a dose-dependent manner. Flow cytometic assay of Annexin-V/PI revealed apoptotic populations under increasing dose of lobetyol ranging from 0 μg/mL, 50 μg/mL, 75 μg/mL, to 100 μg/mL are 5.5%, 13.74%, 27.32% to 31.57%, respectively. Western Blot Analysis[1] Cell Line: MKN45 cells Concentration: 0 μg/mL, 50 μg/mL, 75 μg/mL, 100 μg/mL Incubation Time: 12 h, 24 h, 48 h Result: Increased the expression level of Bax, P53, and decreased the expression level of Bcl-2. The release of cytochrome c was detected, followed by caspase-9 and -3 activations.

Lobetyol (0-10 mg/kg，每3天一次)抑制 MKN45 裸鼠模型中的肿瘤生长[1]。 Animal Model: BALB/C nude mice (6 weeks-old, injected intraperitoneally with MKN45 cells)[1] Dosage: 0, 2, 5, 10 mg/kg Administration: Once per 3 days Result: Suppressed tumor growth in MKN45 nude models. The protein levels of Ki67 in MKN45 cells were significantly decreased. Meanwhile, cleaved-caspase-3 positive MKN45 cells were found increased with the tendency of lobetyol concentrations in the study in vivo.

[1]. Shen J, et al. Lobetyol activate MAPK pathways associated with G1/S cell cycle arrest and apoptosis in MKN45 cells in vitro and in vivo. Biomed Pharmacother. 2016 Jul;81:120-127.  

[2]. Xie Q, et al. The in vitro/in vivo metabolic pathways analysis of lobetyol, lobetyolin, and lobetyolinin, three polyacetylenes from Codonopsis Radix, by UHPLC-Q/TOF-MS and UHPLC-MS/MS. J Pharm Biomed Anal. 2023 Jan 20;223:115140.