大黄素及衍生物的合成与抗肿瘤活性的研究进展  

Research progress in synthesis and antitumor activity of emodin and its derivatives

作　　者：王洁 张启立 赵磊[1,2] 夏鹏飞 续艳丽[1] 杜浩 李娇娇 WANG Jie;ZHANG Qili;ZHAO Lei;XIA Pengfei;XU Yanli;DU Hao;LI Jiaojiao(Gansu University of Chinese Medicine,Lanzhou,Northwest Collaborative Innovation Center for Traditional Chinese Medicine Co-constructed by Gansu Province&MOE of PRC,Key Laboratory of Chemistry and Quality for TCM of Colleges of Gansu Province,Gansu Province Engineering Laboratory for TCM Standardization Technology and Popularization,Lanzhou,Gansu,730000 P.R.China;Lanzhou Institute for Food and Drug Control,Lanzhou,Gansu,730000 P.R.China;Gansu Institute for Drug Control,Lanzhou,Gansu,730000 P.R.China)

机构地区：[1]甘肃中医药大学西北中藏药省部共建协同创新中心甘肃省高校中藏药化学与质量研究省级重点实验室甘肃省道地药材质量标准化技术研究与推广工程实验室,甘肃兰州730000 [2]兰州市食品药品检验检测研究院,甘肃兰州730000 [3]甘肃省药品检验研究院,甘肃兰州730000

出　　处：《华西药学杂志》2023年第2期214-221,共8页West China Journal of Pharmaceutical Sciences

基　　金：国家自然科学基金资助项目(批准号:82160457,81660577);甘肃省教育厅"双一流"科研重点项目(GSSYLXM-05);甘肃省科技计划资助项目(21JR7RA564);甘肃省道地药材质量标准化技术研究与推广工程实验室开放基金(ddyc-2022-03);甘肃中医药大学研究生创新创业基(2022CX85)。

摘　　要：大黄素属于蒽醌类化合物,主要存在于大黄、虎杖等中药中,具有抗炎、抑菌、镇痛等药理作用。大黄素具有广谱抗肿瘤活性,对肺癌、胃癌、胰腺癌等均有抑制作用。大黄素水溶性差,生物利用度较低,限制了其生物活性。对大黄素进行化学结构修饰,增大水溶性,改善生物利用度,可提高抗肿瘤活性。现从大黄素来源、结构修饰、衍生物合成及抗肿瘤活性等方面进行整理和总结,为大黄素的开发提供理论依据。Emodin is an anthraquinone compound,which mainly exists in traditional Chinese medicines such as Rhei Radix et Rhizome and Polygoni Cuspidati Rhizome et Radi.It has a wide range of pharmacological effects such as anti-inflammatory,antibacterial and analgesic activities.It has been found that emodin also displays antitumor activity against various tumors such as lung cancer,gastric cancer,and pancreatic cancer.However,due to its poor water solubility and low bioavailability,which limits the effective exertion of its biological activity.Therefore,chemical structure modifications of emodin may help increase its water solubility,and bioavailability.In this paper,the source of emodin,structural modification,synthesis of derivatives and its anti-tumor activity were sorted out and summarized,in order to provide a theoretical basis for the in-depth study of emodin.

关 键 词：大黄素 蒽醌化合物 结构修饰 衍生物 抗肿瘤 生物活性 作用机制 构效关系 

分 类 号：R914[医药卫生—药物化学]