Abstract

ObjectiveOral squamous cell carcinoma (OSCC) is a prevalent cancer, especially in developing countries. Anthracyclines and their anthraquinone derivatives, such as doxorubicin, exhibit a cell growth inhibitory effect and have been used as anti-cancer drugs for many years. However, the cardiotoxicity of anthracycline antibiotics is a major concern in their clinical application. NSC745885 is a novel compound synthesized from 1,2-diaminoanthraquinone, which subsequently reacts with thionyl chloride and triethylamine. The present study aimed to investigate the anti-oral cancer potential and the safety of NSC745885.MethodsWe investigated the anti-cancer potential of NSC745885 in oral squamous carcinoma cell lines and in an in vivo oral cancer xenograft mouse model. The expression of apoptotic related genes were evaluated by real-time RT-PCR and western bloting, and the in vivo assessment of apoptotic marker were measured by immunohistochemical staining. The anti-tumor efficiency and safety between doxorubicin and NSC745885 were also compared.ResultsOur results demonstrated that NSC745885 exhibits anti-oral cancer activity through the induction of apoptosis in cancer cells and in tumor-bearing mice, and this treatment did not induce marked toxicity in experimental mice. This compound also exhibits a comparable anti-tumor efficiency and a higher safety in experimental mice when compared to doxorubicin.ConclusionsThe data of this study provide evidence for NSC745885 as a potential novel therapeutic drug for the treatment of human OSCC.

Highlights

  • Among oral squamous cell carcinomas (OSCCs), the greatest majority of malignancies are head and neck squamous cell carcinomas (HNSCCs)

  • We investigated the anti-cancer potential of NSC745885 in oral squamous carcinoma cell lines and in an in vivo oral cancer xenograft mouse model

  • Our results demonstrated that NSC745885 exhibits anti-oral cancer activity through the induction of apoptosis in cancer cells and in tumor-bearing mice, and this treatment did not induce marked toxicity in experimental mice

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Summary

Introduction

Among oral squamous cell carcinomas (OSCCs), the greatest majority of malignancies are head and neck squamous cell carcinomas (HNSCCs). OSCC is the sixth most prevalent cancer worldwide [1], and the third most common cancer in developing countries [2,3,4]. Traditional therapies for OSCC include surgery, radiotherapy, and chemotherapy. The remedial effect of such therapies on end-stage oral cancer is uniformly poor. Even after successful tumor resection, approximately 20% of patients may have recurrence of tumors at other site [5]. Developing novel therapeutic strategies for malignant oral tumors is an urgent issue

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