Design, synthesis and biological evaluation of piperine derivatives as potent antitumor agents.

Autor: Wang XJ; College of Pharmacy, Jiangsu Ocean University, Lianyungang 222000, China. Electronic address: wangxiujun@jou.edu.cn., Qiao Y; College of Pharmacy, Jiangsu Ocean University, Lianyungang 222000, China., Wang XS; College of Pharmacy, Jiangsu Ocean University, Lianyungang 222000, China., Zhang SY; College of Pharmacy, Jiangsu Ocean University, Lianyungang 222000, China., Li HX; College of Pharmacy, Jiangsu Ocean University, Lianyungang 222000, China., Hao HH; College of Pharmacy, Jiangsu Ocean University, Lianyungang 222000, China., Li KQ; College of Pharmacy, Jiangsu Ocean University, Lianyungang 222000, China., Ma SJ; College of Pharmacy, Jiangsu Ocean University, Lianyungang 222000, China., Zhu QJ; College of Pharmacy, Jiangsu Ocean University, Lianyungang 222000, China., Ji J; College of Pharmacy, Jiangsu Ocean University, Lianyungang 222000, China. Electronic address: jijing@jou.edu.cn., Liu B; College of Pharmacy, Jiangsu Ocean University, Lianyungang 222000, China. Electronic address: liubin@jou.edu.cn.
Jazyk: angličtina
Zdroj: Fitoterapia [Fitoterapia] 2024 Sep; Vol. 177, pp. 106118. Date of Electronic Publication: 2024 Jul 06.
DOI: 10.1016/j.fitote.2024.106118
Abstrakt: A series of piperine derivatives were designed and successfully synthesized. The antitumor activities of these compounds against 293 T human normal cells, as well as MDA-MB-231 (breast) and Hela (cervical) cancer cell lines, were assessed through the MTT assay. Notably, compound H7 exhibited moderate activity, displaying reduced toxicity towards non-tumor 293 T cells while potently enhancing the antiproliferative effects in Hela and MDA-MB-231 cells. The IC 50 values were determined to be 147.45 ± 6.05 μM, 11.86 ± 0.32 μM, and 10.50 ± 3.74 μM for the respective cell lines. In subsequent mechanistic investigations, compound H7 demonstrated a dose-dependent inhibition of clone formation, migration, and adhesion in Hela cells. At a concentration of 15 μM, its inhibitory effect on Hela cell function surpassed that of both piperine and 5-Fu. Furthermore, compound H7 exhibited promising antitumor activity in vivo, as evidenced by significant inhibition of tumor angiogenesis and reduction in tumor weight in a chicken embryo model. These findings provide a valuable scientific foundation for the development of novel and efficacious antitumor agents, particularly highlighting the potential of compound H7 as a therapeutic candidate for cervical cancer and breast cancer.
Competing Interests: Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.
(Copyright © 2024 Elsevier B.V. All rights reserved.)
Databáze: MEDLINE
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