灵芝β-葡聚糖磷酸化衍生物体外抑制肿瘤细胞增殖的作用  

Phosphorylated Derivatives of Ganoderma lucidumβ-glucan Inhibited Tumor Cells K562 and L1210 in Vitro

作　　者：张忠[1] 张劲松[1] 唐庆九[1] 周帅[1] 杨焱[1] 冯娜[1] 王金艳[1] 刘艳芳[1] ZHANG Zhong;ZHANG Jinsong;TANG Qingjiu;ZHOU Shuai;YANG Yan;FENG Na;WANG Jingyan;LIU Yanfang(Institute of Edible Fungi,Shanghai Academy of Agricultural Sciences,Key Laboratory of Edible Fungi Resources and Utilization(South),Ministry of Agriculture,P.R.China,National Engineering Research Center of Edible Fungi,National R&D Center for Edible Fungi Processing,Key Laboratory of Agricultural Genetics and Breeding of Shanghai,Shanghai 201403,China)

机构地区：[1]上海市农业科学院食用菌研究所,农业部南方食用菌资源利用重点实验室,国家食用菌工程技术研究中心,国家食用菌加工技术研发分中心,上海市农业遗传育种重点开放实验室,上海201403

出　　处：《食用菌学报》2020年第1期63-68,共6页Acta Edulis Fungi

基　　金：上海市农委青年人才成长计划项目[沪农青字(2017)第1-10号]。

摘　　要：采用磷酸盐法对灵芝(Ganoderma lucidum)β-葡聚糖进行磷酸化修饰,在不同反应温度下(60、70、80、90、100℃)得到灵芝β-葡聚糖磷酸化衍生物(PGLP1~5),随着反应温度的上升,衍生物取代度(degree of substitution,DS)逐渐增大,重均分子量(average molecular weight,Mw)逐渐下降,反应温度为100℃时取代度最大为1.02。灵芝β-葡聚糖磷酸化衍生物体外对肿瘤细胞K562和L1210的增殖均有抑制作用,随着取代度增加,抑制率增高,且呈浓度依赖性;取代度最大的磷酸化衍生物PGLP5(DS=1.02,Mw=0.8×10^4)在200μg·mL^-1浓度下,对K562和L1210细胞增殖的抑制率分别为58.74%和50.05%,其IC50值分别为99.61μg·mL^-1和187.52μg·mL^-1。研究结果表明,灵芝β-葡聚糖磷酸化衍生物具有体外抗肿瘤活性,且抗肿瘤活性强弱与其取代度大小有关,取代度越大,抗肿瘤活性越强。Using the phosphate method,Ganoderma lucidumβ-glucan was phosphorylated at different reaction temperatures(60,70,80,90,and 100℃)to yield phosphorylated derivatives PGLP1-PGLP5,respectively.As the reaction temperature increased,the degree of substitution(DS)of the phosphorylated derivatives gradually increased from PGLP1 to PGLP5,reaching a maximum of 1.02 at 100℃for PGLP5.On the other hand,the average molecular weight(Mw)of the derivatives decreased with increasing reaction temperature.The five phosphorylated derivatives PGLP1 to PGLP5 inhibited the proliferation of tumor cells L1210 and K562 in vitro in a concentrationdependent manner.At the same concentration,the inhibition rates of PGLP1 to PGLP5 stepwisely increased.At 200μg·mL^-1,PGLP5(DS=1.02,Mw=0.8×10^4)inhibited tumer cells L1210 and K562 with inhibition rates of 50.05%and 58.74%respectively,and IC50 values of 187.52μg/mL^-1 and 99.61μg·mL^-1 respectively.These results suggested that phosphorylated G.lucidumβ-glucan has DS-associated anti-tumor activity in vitro.

关 键 词：灵芝β-葡聚糖 磷酸化 K562 L1210 抗肿瘤 

分 类 号：R285.5[医药卫生—中药学]