Journal
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
Volume 60, Issue 29, Pages 16215-16223Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/anie.202105607
Keywords
chemotherapy; fluorescence image; molecular mechanism; perylene; twisted skeleton
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Funding
- National Natural Science Foundation of China [U1904150, 81372147]
- Natural Science Foundation of Henan for Distinguished Young Scholars [:212300410003]
- Program for Innovative Research Team (in Science and Technology) in University of Henan Province [21IRTSTHN002]
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The study presents a proof-of-concept demonstration of twisted perylene-derived PDIC-NC for achieving lung-specific drug delivery, targeting mitochondria as a cellular respiration inhibitor to induce apoptosis and endoplasmic reticulum stress in lung cancer cells, showing promising antitumor effects in vivo.
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 H2O2 and (OH)-O-. 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.
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