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Regulating Twisted Skeleton to Construct Organ‐Specific Perylene for Intensive Cancer Chemotherapy
Author(s) -
Liu Zhonghua,
Wang Xuejuan,
Chen Qing,
Ma Feiyan,
Huang Yongwei,
Gao Yijian,
Deng Qingyuan,
Qiao ZengYing,
Xing Xiaoyi,
Zhu Jianling,
Lu Feng,
Wang Hao
Publication year - 2021
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.202105607
Subject(s) - lung cancer , perylene , autophagy , endoplasmic reticulum , in vivo , chemotherapy , cancer , lung , cancer research , medicine , drug , distribution (mathematics) , pharmacology , chemistry , microbiology and biotechnology , biology , apoptosis , biochemistry , organic chemistry , molecule , mathematical analysis , mathematics
The systemic use of pharmaceutical drugs for cancer patients is a compromise between desirable therapy and side effects because of the intrinsic shortage of organ‐specific pharmaceutical drug. Design and construction of pharmaceutical drug to achieve the organ‐specific delivery is thus desperately desirable. We herein regulate perylene skeleton to effect organ‐specificity and present an example of lung‐specific distribution on the basis of bay‐twisted PDIC‐NC. We further demonstrate that PDIC‐NC can target into mitochondria to act as cellular respiration inhibitor, inducing insufficient production of adenosine triphosphate, promoting endogenous H 2 O 2 and . OH burst, elevating calcium overload, efficiently triggering the synergistic apoptosis, autophagy and endoplasmic reticulum stress of lung cancer cells. The antitumor performance of PDIC‐NC is verified on in vivo xenografted, metastasis and orthotopic lung cancer, presenting overwhelming evidences for potentially clinical application. This study contributes a proof‐of‐concept demonstration of twisted perylene to well attain lung‐specific distribution, and meanwhile achieves intensive lung cancer chemotherapy.