دورية أكاديمية

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

التفاصيل البيبلوغرافية
العنوان: Design, synthesis and biological evaluation of piperine derivatives as potent antitumor agents.
المؤلفون: 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.
المصدر: Fitoterapia [Fitoterapia] 2024 Sep; Vol. 177, pp. 106118. Date of Electronic Publication: 2024 Jul 06.
نوع المنشور: Journal Article
اللغة: English
بيانات الدورية: Publisher: Elsevier Country of Publication: Netherlands NLM ID: 16930290R Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1873-6971 (Electronic) Linking ISSN: 0367326X NLM ISO Abbreviation: Fitoterapia Subsets: MEDLINE
أسماء مطبوعة: Publication: 1999- : [Amsterdam] : Elsevier
Original Publication: Milano : Inverni & Della Beffa S.p.A.
مواضيع طبية MeSH: Piperidines*/pharmacology , Piperidines*/chemical synthesis , Piperidines*/chemistry , Benzodioxoles*/pharmacology , Benzodioxoles*/chemical synthesis , Polyunsaturated Alkamides*/pharmacology , Polyunsaturated Alkamides*/chemical synthesis , Polyunsaturated Alkamides*/chemistry , Alkaloids*/pharmacology , Alkaloids*/chemical synthesis , Alkaloids*/chemistry, Humans ; Animals ; Molecular Structure ; Cell Line, Tumor ; HeLa Cells ; Chick Embryo ; Cell Movement/drug effects ; Antineoplastic Agents, Phytogenic/pharmacology ; Antineoplastic Agents, Phytogenic/chemical synthesis ; Antineoplastic Agents/pharmacology ; Antineoplastic Agents/chemical synthesis ; Antineoplastic Agents/chemistry ; Drug Design ; Cell Proliferation/drug effects
مستخلص: 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.)
فهرسة مساهمة: Keywords: Antitumor activity; Chicken embryo model; Piperine derivatives
المشرفين على المادة: 0 (Piperidines)
0 (Benzodioxoles)
U71XL721QK (piperine)
0 (Polyunsaturated Alkamides)
0 (Alkaloids)
0 (Antineoplastic Agents, Phytogenic)
0 (Antineoplastic Agents)
تواريخ الأحداث: Date Created: 20240708 Date Completed: 20240809 Latest Revision: 20240809
رمز التحديث: 20240812
DOI: 10.1016/j.fitote.2024.106118
PMID: 38977252
قاعدة البيانات: MEDLINE