Synthesis and in vitro Anti-proliferative Activities on LNCaP, LS180 and MKN45 of Novel 20(R)-Panaxadiol Derivatives

  • Autores: Deng J.1, Yang X.2, Luan M.2, Liu S.2, Zhang J.2, Jiang S.3, Wang W.4, Hou G.5, Meng Q.2, Wang H.2
  • Afiliações:
    1. School of Pharmacy, Key Laboratory of Molecular Pharmacology and Drug Evaluation, Yantai University), Ministry of Education, Collaborative Innovation Center of Advanced Drug Delivery System and Biotech Drugs in Universities of Shandong, Yantai Universit
    2. School of Pharmacy, Key Laboratory of Molecular Pharmacology and Drug Evaluation, Yantai University), Ministry of Education, Collaborative Innovation Center of Advanced Drug Delivery System and Biotech Drugs in Universities of Shandong, Yantai University
    3. , Shandong Shenxiangchuanqi Biotechnology Co., Ltd
    4. , Shandong Shenxiangchuanqi Biotechnology Co., Ltd.
    5. School of Basic Medical Sciences, Binzhou Medical University
  • Edição: Volume 23, Nº 15 (2023)
  • Páginas: 1731-1739
  • Seção: Oncology
  • URL: https://kld-journal.fedlab.ru/1871-5206/article/view/694346
  • DOI: https://doi.org/10.2174/1871520623666230412095428
  • ID: 694346

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Resumo

Background: 20(R)-PD, a tetracyclic triterpenoid, is a non-natural saponin present in the form of protopanaxadiol. Because of its essential biological activities, especially anti-tumor activity, structural modification of 20(R)-PD and the development of innovative and novel 20(R)-PD derivatives with better anti-tumor activity are increasingly relevant.

Aims:20(R)-Panaxadiol (20(R)-PD) can inhibit tumor proliferation. Three series of novel 20(R)-PD derivatives were synthesized by modifying the A-ring.

Objective: The objective of this work was to synthesize and evaluate the in vitro anti-proliferative activities of 20(R)- PD derivatives in LNCaP, LS180, and MKN45 cancer cells. Structural modifications were performed at the C-3 position and A-ring.

Methods: The in vitro anti-proliferative activities of novel derivatives in LNCaP, LS180, and MKN45 cells were evaluated by the MTT assay. The effects of compounds 5 and C9 on apoptosis were determined by flow cytometry.

Results: Compounds 5, B2, C2, C4, C7, C8, C9, C10, and C11 exhibited good anti-proliferative activities in LNCaP, LS180, and MKN45 cells in vitro. The best anti-proliferative activity was observed for the C-series derivatives with the introduction of amino acids at the C-3 position. C9 exhibited good potent activity with an IC50 of 2.89 µM.

Conclusion: Compound C9 is a potential candidate with potent anti-proliferative activity.

Sobre autores

Jianqiang Deng

School of Pharmacy, Key Laboratory of Molecular Pharmacology and Drug Evaluation, Yantai University), Ministry of Education, Collaborative Innovation Center of Advanced Drug Delivery System and Biotech Drugs in Universities of Shandong, Yantai Universit

Email: info@benthamscience.net

Xinyu Yang

School of Pharmacy, Key Laboratory of Molecular Pharmacology and Drug Evaluation, Yantai University), Ministry of Education, Collaborative Innovation Center of Advanced Drug Delivery System and Biotech Drugs in Universities of Shandong, Yantai University

Email: info@benthamscience.net

Mingzhu Luan

School of Pharmacy, Key Laboratory of Molecular Pharmacology and Drug Evaluation, Yantai University), Ministry of Education, Collaborative Innovation Center of Advanced Drug Delivery System and Biotech Drugs in Universities of Shandong, Yantai University

Email: info@benthamscience.net

Shuqi Liu

School of Pharmacy, Key Laboratory of Molecular Pharmacology and Drug Evaluation, Yantai University), Ministry of Education, Collaborative Innovation Center of Advanced Drug Delivery System and Biotech Drugs in Universities of Shandong, Yantai University

Email: info@benthamscience.net

Juan Zhang

School of Pharmacy, Key Laboratory of Molecular Pharmacology and Drug Evaluation, Yantai University), Ministry of Education, Collaborative Innovation Center of Advanced Drug Delivery System and Biotech Drugs in Universities of Shandong, Yantai University

Email: info@benthamscience.net

Sheng Jiang

, Shandong Shenxiangchuanqi Biotechnology Co., Ltd

Email: info@benthamscience.net

Wenshui Wang

, Shandong Shenxiangchuanqi Biotechnology Co., Ltd.

Email: info@benthamscience.net

Guige Hou

School of Basic Medical Sciences, Binzhou Medical University

Email: info@benthamscience.net

Qingguo Meng

School of Pharmacy, Key Laboratory of Molecular Pharmacology and Drug Evaluation, Yantai University), Ministry of Education, Collaborative Innovation Center of Advanced Drug Delivery System and Biotech Drugs in Universities of Shandong, Yantai University

Autor responsável pela correspondência
Email: info@benthamscience.net

Hongbo Wang

School of Pharmacy, Key Laboratory of Molecular Pharmacology and Drug Evaluation, Yantai University), Ministry of Education, Collaborative Innovation Center of Advanced Drug Delivery System and Biotech Drugs in Universities of Shandong, Yantai University

Autor responsável pela correspondência
Email: info@benthamscience.net

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