2. Academic Validation
  3. Antibacterial AZT derivative regulates metastasis of breast cancer cells

Antibacterial AZT derivative regulates metastasis of breast cancer cells

  • Eur J Med Chem. 2020 May 1;193:112233. doi: 10.1016/j.ejmech.2020.112233.
Sridhar Chirumarry 1,  Nak-Kyun Soung 2,  Junyeol Han 2,  Eun Young Kim 3,  Eun Kyoung Ryu 4,  Young-Ho Lee 4,  Song Yub Shin 3,  Pethaiah Gunasekaran 5,  Jeong Kyu Bang 6
Affiliations

Affiliations

  • 1 Division of Magnetic Resonance, Korea Basic Science Institute (KBSI), Ochang, Chung Buk, 28119, Republic of Korea.
  • 2 Anticancer Agent Research Center, Korea Research Institute of Bioscience and Biotechnology, Ochang, Cheongju, 28116, Republic of Korea.
  • 3 Department of Biomedical Science, Graduate School, Cellular and Molecular Medicine, Chosun University, Gwangju, 61452, Republic of Korea.
  • 4 Division of Magnetic Resonance, Korea Basic Science Institute (KBSI), Ochang, Chung Buk, 28119, Republic of Korea; Department of Bio-analytical Science, University of Science & Technology, Daejeon, 34113, Republic of Korea.
  • 5 Division of Magnetic Resonance, Korea Basic Science Institute (KBSI), Ochang, Chung Buk, 28119, Republic of Korea. Electronic address: gunaharaks@kbsi.re.kr.
  • 6 Division of Magnetic Resonance, Korea Basic Science Institute (KBSI), Ochang, Chung Buk, 28119, Republic of Korea; Department of Bio-analytical Science, University of Science & Technology, Daejeon, 34113, Republic of Korea. Electronic address: bangjk@kbsi.re.kr.
PMID: 32199136 DOI: 10.1016/j.ejmech.2020.112233
Abstract

Antimicrobial Peptides (AMP) with Anticancer activity have drawn remarkable attention in modern treatments. However, long peptide length and Protease instability are the most addressing factors, which hampers their further development as therapeutic agents. In view of this, herein, we designed and synthesized a series of AZT-based cationic small molecule incorporating a variety of hydrophobic groups and cationic charges, including amine and guanidine groups to mimic the amphipathic structure of AMPs. These compounds were evaluated for their Antibacterial activity against Gram-positive and Gram-negative bacteria. Through an extensive structure activity relationship study (SAR), we identified ADG-2e as the most potent Antibacterial agent, which exhibited remarkable potency against drug resistant Bacterial strains such as MRSA and MDRPA. Further, ADG-2e was examined for their anti-metastatic ability by investigating the Cancer cell migration and invasiveness through scratch wound-healing assay and transwell invasive assay, respectively. In addition, time-lapse cell tracking analysis also performed for analyzing the cell movement pattern. Treatment of ADG-2e against metastatic breast Cancer cells (MDA-MB-231) suppressed tumor cell migration by multi-directional lamellipodium formation, indicating their anti-metastatic potential. Thus, our cationic AZT based small molecules may evolve as an appealing class of Antibacterial agents with anti-metastasis potential.

Keywords

Amphipathic small molecule; Anti-Metastasis; Antibacterials; Cell motility; Lamellipodia.

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