TY - JOUR
T1 - A Second Near-Infrared Ru(II) Polypyridyl Complex for Synergistic Chemo-Photothermal Therapy
AU - Liu, Yishen
AU - Li, Qianqian
AU - Gu, Meijia
AU - Lu, Disheng
AU - Xiong, Xiaoxing
AU - Zhang, Zhiyun
AU - Pan, Yanna
AU - Liao, Yuqin
AU - Ding, Qihang
AU - Gong, Wanxia
AU - Chen, Dean Shuailin
AU - Guan, Mengting
AU - Wu, Junzhu
AU - Tian, Zhiquan
AU - Deng, Hai
AU - Gu, Lijuan
AU - Hong, Xuechuan
AU - Xiao, Yuling
N1 - Funding Information:
This work was supported by the National Key R&D Program of China (2020YFA0908800), NSFC (81773674, 81573383, 82111530209, and 91959103), Shenzhen Science and Technology Research Grant (JCYJ20190808152019182), Hubei Province Scientific and Technical Innovation Key Project (2020BAB058), the Natural Science Foundation of Hubei Province (Grant No. 2021CFB014), the Applied Basic Research Program of Wuhan Municipal Bureau of Science and Technology (2019020701011429), the Doctoral Foundation of Huanggang Normal University (2042021007 and 20420218704), Tibet Autonomous Region Science and Technology Plan Project Key Project (XZ201901-GB-11), the Local Development Funds of Science and Technology Department of Tibet (XZ202102YD0033C and XZ202001YD0028C), and the Fundamental Research Funds for the Central Universities.
PY - 2022/2/10
Y1 - 2022/2/10
N2 - The clinical success of cisplatin ushered in a new era of the application of metallodrugs. When it comes to practice, however, drug resistance, tumor recurrence, and drug systemic toxicity make it implausible to completely heal the patients. Herein, we successfully transform an electron acceptor [1, 2, 5]thiadiazolo[3,4-g]quinoxaline into a novel second near-infrared (NIR-II) fluorophore H7. After PEGylation and chelation, HL-PEG2k exhibits a wavelength bathochromic shift, enhanced photothermal conversion efficiency (41.77%), and an antineoplastic effect against glioma. Its potential for in vivo tumor tracking and image-guided chemo-photothermal therapy is explored. High levels of uptake and high-resolution NIR-II imaging results are thereafter obtained. The hyperthermia effect could disrupt the lysosomal membranes, which in turn aggravate the mitochondria dysfunction, arrest the cell cycle in the G2 phase, and finally lead to cancer cell apoptosis. HL-PEG2k displays a superior biocompatibility and thus can be a potential theranostic platform to combat the growth and recurrence of tumors.
AB - The clinical success of cisplatin ushered in a new era of the application of metallodrugs. When it comes to practice, however, drug resistance, tumor recurrence, and drug systemic toxicity make it implausible to completely heal the patients. Herein, we successfully transform an electron acceptor [1, 2, 5]thiadiazolo[3,4-g]quinoxaline into a novel second near-infrared (NIR-II) fluorophore H7. After PEGylation and chelation, HL-PEG2k exhibits a wavelength bathochromic shift, enhanced photothermal conversion efficiency (41.77%), and an antineoplastic effect against glioma. Its potential for in vivo tumor tracking and image-guided chemo-photothermal therapy is explored. High levels of uptake and high-resolution NIR-II imaging results are thereafter obtained. The hyperthermia effect could disrupt the lysosomal membranes, which in turn aggravate the mitochondria dysfunction, arrest the cell cycle in the G2 phase, and finally lead to cancer cell apoptosis. HL-PEG2k displays a superior biocompatibility and thus can be a potential theranostic platform to combat the growth and recurrence of tumors.
KW - Antineoplastic agents
KW - Fluorescence
KW - Lasers
KW - Rodent models
KW - Tumors
UR - http://www.scopus.com/inward/record.url?scp=85123302870&partnerID=8YFLogxK
U2 - 10.1021/acs.jmedchem.1c01736
DO - 10.1021/acs.jmedchem.1c01736
M3 - Article
C2 - 34994554
AN - SCOPUS:85123302870
VL - 65
SP - 2225
EP - 2237
JO - Journal of Medicinal Chemistry
JF - Journal of Medicinal Chemistry
SN - 0022-2623
IS - 3
ER -
