Highly sensitive and selective anticancer effect by conjugated HA-cisplatin in non-small cell lung cancer overexpressed with CD44

Yu Hua Quan, Byungji Kim, Ji Ho Park, Yeonho Choi, Young Ho Choi, Hyun Koo Kim

Research output: Contribution to journalArticlepeer-review

34 Citations (Scopus)


In spite of severe side effects, chemotherapy is widely used as a major anticancer treatment in non-small cell lung cancer (NSCLC). In order to enhance the therapeutic properties and reduce side effects, enormous efforts have been devoted to direct anticancer agents specifically to tumor tissues by the use of nanoparticles, or cancer cell marker attached drugs. However, cell-specific chemotherapy is still in its infancy and is not applicable to all types of cancers due to the complexity of the cancer occurrence and progress. In this study, we demonstrate that hyaluronan (HA)-conjugated cisplatin has highly selective and sensitive anticancer effects in NSCLC cells that overexpress the trans-membrane receptor, CD44, as HA is a specific ligand for CD44. In proliferation experiments, HA-conjugated cisplatin showed dramatic cell viability decreases (from 100% to 42.31%) in H1299 cells, which overexpress CD44, whereas no such change was observed in A549 and HFL1, which have little to no expression of CD44. More importantly, conjugation with HA decreased the dosage concentration of cisplatin by 50-fold for both cytotoxic and anti-metastatic effects. In addition, HA-cisplatin conjugate treatment selectively decreased migration (from 100% to 7.8%) and invasiveness (from 100% to 21.4%, respectively) of H1299. Based on our experimental results, we strongly believe that HA-cisplatin conjugate is a potential anticancer chemo-agent, which target CD44 overexpression in NSCLC, with minimal side effects and high therapeutic properties.

Original languageEnglish
Pages (from-to)475-484
Number of pages10
JournalExperimental Lung Research
Issue number10
Publication statusPublished - 2014 Dec 1

Bibliographical note

Funding Information:
This work was supported by the National Research Foundation of Korea (NRF) grant funded by the Korea government (MEST) (no.: 2012012166). Address correspondence to Hyun Koo Kim, Department of Thoracic and Cardiovascular Surgery, Korea University College of Medicine, Seoul 152–703, Korea. E-mail: kimhyunkoo@korea.ac.kr and Yeonho Choi, Department of Biomedical Engineering, Korea University, Seoul 136–703, Korea. E-mail: yeonhochoi@korea.ac.kr

Publisher Copyright:
© 2014 Informa Healthcare USA, Inc.


  • CD44
  • Hyaluronan-cisplatin conjugate
  • Lung cancer

ASJC Scopus subject areas

  • Molecular Biology
  • Pulmonary and Respiratory Medicine
  • Clinical Biochemistry


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