N-isoquinoline-3-carbonyl-L-Leucine-benzylester as a new agent of inhibiting esophageal carcinoma proliferation

Abstract

Abstract: AIM: To determine whether N-isoquinoline-3-carbonyl-L-Leucine-benzylester(IQ-L-OBzl)inhibited the growth of human esophageal cancer cell in vitro and in vivo. METHODS: MTT assays were performed to assess the proliferation of esophageal carcinoma cell lines. The model of esophageal carcinoma in nude mice was established, then the weight of tumor tissue was measured, the growth inhibition rates of tumor were calculated and the WBC were counted on peripheral blood of the mice. Intracellular reactive oxygen species(ROS)were detected by flow cytometry analysis. RESULTS: The IC₅₀ of IQ-L-OBzl inhibiting esophageal carcinoma cell lines(Eca-109 and EC-9706)proliferation were (405.06±23.49) nmol/L and (485.79±48.47) nmol/L. The best growth inhibition rate was (42.42±7.47) %. The growth inhibition rate and the weight of tumor exhibited dose-dependent manner. The ROS level of IQ-L-OBzl was (98.68±13.19) MFI, higher than that in control groups (P<0.05). CONCLUSION: IQ-L-OBzl has anti-esophageal carcinoma ability in vitro and in vivo, and this ability have related to ROS without significant side effects on WBC.

Key words: N-isoquinoline-3-carbonyl-L-Phenylalanine-benzylester, esophageal carcinoma, reactive oxygen species

CLC Number:

R735.1

YANG Guo-dong, ZHANG Xiao-ying, FENG Zhi-song, HE Guo-bin, JIANG Yi-min. N-isoquinoline-3-carbonyl-L-Leucine-benzylester as a new agent of inhibiting esophageal carcinoma proliferation[J]. Chinese Journal of Clinical Pharmacology and Therapeutics, 2014, 19(8): 877-881.

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