Phytoestrogen-derived multifunctional ligands for targeted therapy of breast cancer  

作　　者：Ying Zhang Hao Pan Changxiang Yu Rui Liu Bin Xing Bei Jia Jiachen He Xintao Jia Xiaojiao Feng Qingqing Zhang Wenli Dang Zheming Hu Xiuping Deng Pan Guo Zhidong Liu Weisan Pan 

机构地区：[1]State Key Laboratory of Component-based Chinese Medicine,Tianjin University of Traditional Chinese Medicine,Tianjin 301617,China [2]Ministry of Education,Tianjin University of Traditional Chinese Medicine,Tianjin 301617,China [3]School of Pharmacy,Liaoning University,Shenyang 110036,China [4]School of Pharmacy,Shenyang Pharmaceutical University,Shenyang 110016,China

出　　处：《Asian Journal of Pharmaceutical Sciences》2023年第4期96-108,共13页亚洲药物制剂科学（英文）

基　　金：supported by the Tianjin University of Traditional Chinese Medicine Scientific Research Project for the NewTeacher[grant number:XJS2022212];The Science and Technology Program of Tianjin[grant number:21YJDJC00020];The Science and Technology Project of Haihe Laboratory of Modern Chinese Medicine[grant number:22HHZYSS00005].

摘　　要：Nano-targeted delivery systems have been widely used for breast tumor drug delivery.Estrogen receptors are considered to be significant drug delivery target receptors due to their overexpression in a variety of tumor cells.However,targeted ligands have a significant impact on the safety and effectiveness of active delivery systems,limiting the clinical transformation of nanoparticles.Phytoestrogens have shown good biosafety characteristics and some affinity with the estrogen receptor.In the present study,molecular docking was used to select tanshinone IIA(Tan IIA)among phytoestrogens as a target ligand to be used in nanodelivery systems with somemodifications.Modified Tan IIA(Tan-NH2)showed a good biosafety profile and demonstrated tumor-targeting,anti-tumor and anti-tumor metastasis effects.Moreover,the ligand was utilized with the anti-tumor drug Dox-loaded mesoporous silica nanoparticles via chemical modification to generate a nanocomposite Tan-Dox-MSN.Tan-Dox-MSN had a uniform particle size,good dispersibility and high drug loading capacity.Validation experiments in vivo and in vitro showed that it also had a better targeting ability,anti-tumor effect and lower toxicity in normal organs.These results supported the idea that phytoestrogens with high affinity for the estrogen receptor could improve the therapeutic efficacy of nano-targeted delivery systems in breast tumors.

关 键 词：PHYTOESTROGEN Tanshinone IIA DOXORUBICIN Breast cancer Targeting delivery 

分 类 号：R943[医药卫生—药剂学]