从绵毛胡桐芽中提取的 DMC 逆转人肝癌移植瘤多药耐药的作用。
Multidrug resistance reversal effect of DMC derived from buds of Cleistocalyx operculatus in human hepatocellular tumor xenograft model.
机构信息
State Key Laboratory of Bioreactor Engineering, East China University of Science and Technology, Shanghai, PR China.
出版信息
J Sci Food Agric. 2012 Jan 15;92(1):135-40. doi: 10.1002/jsfa.4551. Epub 2011 Jul 21.
BACKGROUND
Multidrug resistance (MDR) is a major obstacle in the chemotherapeutic treatment of many human cancers. 2',4'-Dihydroxy-6'-methoxy-3',5'-dimethylchalcone (DMC) isolated from the buds of Cleistocalyx operculatus (Roxb.) Merr. et Perry (Myrtaceae), was investigated for its reversal effects on cancer cell MDR.
RESULTS
A human hepatocellular tumor xenograft model was established with the BEL-7402/5-FU cell line. Combined 5-fluorouracil (5-FU) and DMC (40 mg kg(-1) ) treatment significantly elevated tumor inhibition rate to 72.2%. DMC could also increase 5-FU concentrations in tumor tissues and increase caspase-3 activity. Also, combined therapy resulted in enhanced tumor apoptotic and reduced proliferative activities relative to 5-FU alone. Examining body weight and other signs of unwanted toxicity of the different treatment groups revealed no significant signs of adverse effects.
CONCLUSION
All results suggested that DMC reverses 5-FU resistance, with a benign side effects profile.
背景
多药耐药性（MDR）是许多人类癌症化疗治疗的主要障碍。2'，4'-二羟基-6'-甲氧基-3'，5'-二甲基查尔酮（DMC）从桃金娘科的闭鞘姜（Cleistocalyx operculatus（Roxb.）Merr. et Perry）的芽中分离出来，研究了其对癌细胞 MDR 的逆转作用。
结果
用人肝癌 BEL-7402/5-FU 细胞系建立了人肝癌异种移植模型。联合使用 5-氟尿嘧啶（5-FU）和 DMC（40 mg kg（-1））治疗可使肿瘤抑制率显著提高至 72.2%。DMC 还可以增加肿瘤组织中 5-FU 的浓度并增加 caspase-3 的活性。此外，与单独使用 5-FU 相比，联合治疗导致肿瘤凋亡增加和增殖活性降低。检查不同治疗组的体重和其他不良毒性迹象，未发现明显的不良反应迹象。
结论
所有结果均表明 DMC 逆转了 5-FU 耐药性，且具有良性的副作用特征。
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