(3R,4R)-3-[(1,3-Benzodioxole-5-yl)methyl]-4-(3,4-dimethoxybenzyl)-4,5-dihydrofuran-2(3H)-one

Kusunokinin ((-)-Kusunokinin) is a nature product that could be isolated form P. nigrum. Kusunokinin has anticancer activity. Kusunokinin arrests cell cycle at G2/M phase and induce apoptosis[1].

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

Kusunokinin ((-)-Kusunokinin; 0.625-10 µg/mL; 72 h) 抑制癌细胞的活力，对 MCF-7、HT-29、MDA-MB-468、SW-620、A-549 和 MDA-MB-231 细胞的 IC50 值分别为 3.08、3.59、3.98、5.75、5.77 和 7.86 µM[1]。 Cell Viability Assay[1] Cell Line: Cancer cells Concentration: 0.625, 1.25, 2.5, 5 and 10 µg/mL Incubation Time: 72 hours Result: Had anticancer activity and inhibited cancer cells growth.

Kusunokinin ((-)-Kusunokinin; 7 和 14 mg/kg; i.h.; 每周 3 次, 持续 2 周) 通过下调信号分子 (c-Src、PI3K、Akt 和 Erk1/2) 抑制 NMU 诱导的乳腺癌大鼠的肿瘤生长[1]。 Animal Model: Female Sprague Dawley rats (7 weeks of age)[1] Dosage: 7 and 14 mg/kg Administration: Subcutaneous injection, 3 times a week for 2 weeks Result: Inhibited the mammary tumor growth and decreased tumor volume. Down-regulated c-Src, Erk1/2 and PI3K proteins and decreased Akt proteins. Inhibited downstream molecules in the cell cycle (c-Myc, E2f-1, CDK1 and cyclin B1) and metastasis (E-cadherin, MMP-2 and MMP-9).

[1]. Tedasen A, et, al. (-)-Kusunokinin inhibits breast cancer in N-nitrosomethylurea-induced mammary tumor rats. Eur J Pharmacol. 2020 Sep 5;882:173311.