These are preliminary reports that have not been peer-reviewed. They should not be regarded as conclusive, guide clinical practice/health-related behavior, or be reported in news media as established information. For more information, please see our FAQs.
Manuscript-20200607.pdf (3.95 MB)
Photoactivatable dihydroalkaloids for cancer theranostics with AIE characteristics
Preprints are manuscripts made publicly available before they have been submitted for formal peer review and publication. They might contain new research findings or data. Preprints can be a draft or final version of an author's research but must not have been accepted for publication at the time of submission.
Chemotherapeutics with systemic administration usually suffer from low treatment efficacy and off-target toxicity. In contrary, the photoactivatable cancer theranostics can achieve image-guided precise control of therapeutic dose and location. However, the conventional photoactivatable chemotherapeutics usually require decoration of chemotherapeutics with additional photo-responsive groups through tedious synthetic procedures, which can lead to undesirable toxic byproducts and seriously restrict their applications. Herein, we propose a new strategy for photoactivatable caner theranostics based on photooxidative dehydrogenation reaction, which is only associating with water as the byproduct. To demonstrate the power of this strategy, we utilized the natural dihydrobenzo[c]phenanthridine alkaloids of DHCHE and DHSAN as photoactivatable theranostics to achieve selective imaging and killing of cancer cells by in situ transformation into nucleus-targeted CHE and SAN under light irradiation. Notably, CHE is featured with aggregation-induced emission (AIE) characteristics, which can be used for precise control of the photoactivatable therapeutic dose. This photoactivatable strategy based on dihydroalkaloids is thus promising for precise cancer treatment in clinic.
This work was financially supported by the National Science Foundation of China (21788102, 51620105009, 21877040, 21602063, U1801252); the Science and Technology Planning Project of Guangzhou (201804020060, 201607020015 and 201704030069); Pearl River S&T Nova Program of Guangzhou (201806010152); Natural Science Foundation of Guangdong Province (2020B1515020010 and 2016A030312002); the Fundamental Research Funds for the Central Universities (2018JQ01); the Innovation and Technology Commission of Hong Kong (ITC-CNERC14SC01). The authors thank Dr. Bo Situ and Dr. Kaojin Wang’s kind help for cell imaging experiment.