Time: 2022-10-10

News Source: School of Chemistry and Chemical Engineering

Editor: Duan Kailong Reviewer:Wang Zhenhua

Recently, Liu Kanglei, a postdoctoral from School of Chemistry and Chemical Engineering of BIT, published her research paper in the top international journal Advanced Materials titled Triarylboron-doped Acenethiophenes as Organic Sonosensitizers for Highly Efficient Sonodynamic Therapy with Low Phototoxicity (DOI:10.1002/adma.202206594) as the first author. BIT is the first corresponding institution for the paper. Special Researcher Yin Xiaodong of the School of Chemistry and Chemical Engineering of BIT, Dr. Jiang Zhenqi of the School of Medical Technology, and Professor Frieder Jakle of Rutgers University-Newark are the co-corresponding authors.

Sonodynamic Therapy (SDT) is an emerging non-invasive cancer therapeutic strategy, which was approved by the US Food and Drug Administration (FDA) in July this year through the green channel for the clinical treatment of malignant tumors. SDT uses ultrasound (US) to stimulate acoustic sensitizers to generate reactive oxygen species (ROS) to induce tumor cell death, so as to achieve the purpose of treatment. Based on the deep tissue penetration ability of ultrasound, SDT can realize the treatment of deeper tumors and has broad clinical transformation prospects. However, the problems of oxygen dependence and skin phototoxicity generally exist in the current clinical use of sound sensitizers. Therefore, it is very important to develop new acoustic sensitizers with high ROS free radical yield, low phototoxicity and good biocompatibility to promote the treatment of SDT and achieve clinical application.

The researchers designed and prepared a triarylboron-doped acenethiophenes, an effective compound in the production of hydroxyl radicals under ultrasound, which is ideal for the treatment of tumor hypoxic microenvironment. More importantly, reactive oxygen species studies have shown that boron-doped acenethiophenes is unlike conventional organic sound sensitizers, as it has overcome the problem of skin phototoxicity at therapeutic concentrations.

In the 4T1 mouse model, boron-doped acenethiophenes, serving as sonosensitizer, could effective and significantly inhibited tumor growth without any signs of tumor recurrence within 14 days after treatment. In addition, vivo experiments showed that it had no obvious damage to normal tissues, high biological safety.

In this work, a novel small molecule structure based on triarylboron-doped acenethiophenes has been successfully prepared, which has good sonodynamic effect in tumor treatment and achieves low phototoxicity and biosafety at the same time. The boron functionalization strategy of acenethiophenes has opened up a new way for the development of efficient organic sonosensitizers.

The above work was supported by the National Natural Science Foundation of China, Postdoctoral Foundation and other projects. We would also like to thank the Analysis & Testing Center of BIT for its support in related tests.

About the authors:

Yin Xiaodong, a special researcher and doctoral supervisor of the School of Chemistry and Chemical Engineering, BIT. In 2011, he graduated from the Institute of Chemistry, Chinese Academy of Sciences with a PhD in organic chemistry. He studied under Academician Li Yuliang and then worked as a postdoctoral researcher at Rutgers University, the University of South Carolina and Columbia University. In September 2018, he joined the School of Chemistry and Chemical Engineering of BIT. His main research direction is the development and application of organoborate functional materials. He has published more than 70 papers in international academic journals such as Nat. Chem., Sci. Adv., Angew. Chem. Int. Ed., Adv. Mater.

Liu Kanglei, a "Teri" postdoctoral fellow at the School of Chemistry and Chemical Engineering, BIT. In 2020, she graduated from Rutgers University with a PhD from Professor Frieder Jakle. She joined BIT in May 2020. Her main research direction is the application of boron-containing small molecules in biomedical fields. Currently, she has published several academic papers in internationally renowned journals, including 3 papers in J. Am. Chem. Soc. journal as the first/corresponding author, 1 paper in Adv. Mater. Journal, 2 papers in Chem. Sci. journal, and 1 patent application. She also holds the National Natural Science Foundation of China Youth Project and Postdoctoral Science Foundation General Project.

Jiang Zhenqi, a postdoctoral fellow at the School of Medical Technology, BIT. In 2020, he graduated from Ningbo Institute of Materials, Chinese Academy of Sciences and studied under researcher Wu Aiguo. He joined BIT in July 2020. His main research direction is image-guided minimally invasive treatment. Currently, he has published more than 30 papers in international journals such as Adv. Mater., J. Am. Chem. Soc., Nano Lett., etc., and has hosted many projects such as National Nature Youth Foundation and key research and development sub-projects of the Ministry of Science and Technology.