A Terphenyllin Derivative CHNQD-00824 from the Marine Compound Library Induced DNA Damage as a Potential Anticancer Agent

Author:

Cao Xi-Zhen12,Zhang Bo-Qi12,Wang Cui-Fang12,Yin Jun-Na12,Haider Waqas12ORCID,Said Gulab13ORCID,Wei Mei-Yan12,Lu Ling12

Affiliation:

1. Key Laboratory of Marine Drugs, The Ministry of Education of China, School of Medicine and Pharmacy, Ocean University of China, Qingdao 266003, China

2. Laboratory for Marine Drugs and Biological Products, Laoshan Laboratory, Qingdao 266003, China

3. Department of Chemistry, Women University Swabi, Swabi 23430, Pakistan

Abstract

With the emergence of drug resistance and the consequential high morbidity and mortality rates, there is an urgent need to screen and identify new agents for the effective treatment of cancer. Terphenyls—a group of aromatic hydrocarbons consisting of a linear 1,4-diaryl-substituted benzene core—has exhibited a wide range of biological activities. In this study, we discovered a terphenyllin derivative—CHNQD-00824—derived from the marine compound library as a potential anticancer agent. The cytotoxic activities of the CHNQD-00824 compound were evaluated against 13 different cell lines with IC50 values from 0.16 to 7.64 μM. Further study showed that CHNQD-00824 inhibited the proliferation and migration of cancer cells, possibly by inducing DNA damage. Acridine orange staining demonstrated that CHNQD-00824 promoted apoptosis in zebrafish embryos. Notably, the anti-cancer effectiveness was verified in a doxycin hydrochloride (DOX)-induced liver-specific enlargement model in zebrafish. With Solafinib as a positive control, CHNQD-00824 markedly suppressed tumor growth at concentrations of 2.5 and 5 μM, further highlighting its potential as an effective anticancer agent.

Funder

Qingdao Marine Science and Technology Center

National Natural Science Foundation of China

National Key Research and Development Program of China

Shandong Province Special Fund “Frontier Technology and Free Exploration” from Laoshan Laboratory

Fundamental Research Funds for the Central Universities

Publisher

MDPI AG

Subject

Drug Discovery,Pharmacology, Toxicology and Pharmaceutics (miscellaneous),Pharmaceutical Science

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