ZHENG Lei, HE Hao, FANG Yi, et al. Antitumor Effect and Mechanism of Fructus[J]. Chinese journal of experimental traditional medical formulae, 2017, 23(9): 152-157.
ZHENG Lei, HE Hao, FANG Yi, et al. Antitumor Effect and Mechanism of Fructus[J]. Chinese journal of experimental traditional medical formulae, 2017, 23(9): 152-157. DOI: 10.13422/j.cnki.syfjx.2017090152.
目的:观察中药木鳖子不同提取部位体内体外的抗肿瘤作用,并考察其中抗肿瘤效果显著的木鳖子乙酸乙酯提取部位的抗肿瘤作用机制。方法:采用索氏提取技术将中药木鳖子按照溶剂极性顺序依次提取,得到不同成分,采用细胞增殖实验结合动物抗肿瘤模型方法进行药效评价,运用现代分子生物学技术阐明其中最优部位可能的抗肿瘤作用机制。结果:中药木鳖子乙酸乙酯提取部位在体外和体内实验中均可表现出明显的抑制肿瘤生长能力(P<0.05),且对实验动物无明显的毒副作用,本研究首次发现木鳖子乙酸乙酯提取部位可影响表皮生长因子(EGFR)激酶活性(P<0.05),并可明显抑制EGFR蛋白磷酸化表达(P<0.05),可明显抑制丝裂原活化蛋白激酶家族(mitogen activated protein kinase,MAPKs)通路上重要节点蛋白细胞外信号调节激酶(extracellular regulated protein kinases,ERK1/2),氨基末端激酶(C-Jun N-terminal kinase,JNK)和丝裂原激活蛋白激酶p38的磷酸化水平(P<0.05),且具有浓度依赖关系。结论:中药木鳖子乙酸乙酯提取部位可通过抑制EGFR蛋白及相关通路蛋白活性,在体内外实验中显著抑制肿瘤的生长。
Abstract
Objective: To investigate the antitumor activity of different solvent extracts of Momordica cochinchinensis Fructus in vivo and in vitro
and the action mechanism of ethyl acetate extracts of M. cochinchinensis with a significant antitumor effect. Method: In order to identify active components
M. cochinchinensis was extracted with solvents according to the sequence of polarities through the Soxhlet extraction method. This study assessed the potency and the underlying mechanisms of action of ethyl acetate extracts of M. cochinchinensis on cancer cells through animal experiments
and used modern biology experiment technologies to investigate its underlying mechanism. Result: Among various fractions
ethyl acetate extracts of M. cochinchinensis showed significant anti-proliferative effects in vivo and in vitro (P<0.05)
with no obvious toxic and side effect on experimental animals. This study found for the first time that ethyl acetate extracts of M. cochinchinensis could inhibit phosphorylation of epidermal growth factor (EGFR) tyrosine kinase and protein phosphorylation (P<0.05)
and expressions of phosphor-ERK1/2
phosphor-JNK and phosphor-p38 of mitogen activated protein kinase (MAPKs) in a dose-dependent manner (P<0.05). Conclusion: Ethyl acetate extracts of M. cochinchinensis could show a significant anti-cancer effect by inhibiting phosphorylation of EGFR tyrosine kinase.