2. Academic Validation
  3. Rhamnazin, a novel inhibitor of VEGFR2 signaling with potent antiangiogenic activity and antitumor efficacy

Rhamnazin, a novel inhibitor of VEGFR2 signaling with potent antiangiogenic activity and antitumor efficacy

  • Biochem Biophys Res Commun. 2015 Mar 20;458(4):913-9. doi: 10.1016/j.bbrc.2015.02.059.
Yao Yu 1,  Wei Cai 2,  Chong-gang Pei 3,  Yi Shao 4
Affiliations

Affiliations

  • 1 Department of Ophthalmology, The First Affiliated Hospital of Nanchang University, Jiangxi Province Clinical Ophthalmology Institute, No.17 Yongwaizheng Street, Donghu District, Nanchang 330006, Jiangxi Province, China; Department of Endocrinology and Metabolism, The Third Hospital of Nanchang, Nanchang Key Laboratory of Diabetes, No.1 Qianjing Road, Xihu District, Nanchang 330009, Jiangxi Province, China.
  • 2 Department of Medical Genetics, College of Basic Medical Science of Nanchang University, No.461 Bayi Road, Donghu District, Nanchang 330006, Jiangxi Province, China.
  • 3 Department of Ophthalmology, The First Affiliated Hospital of Nanchang University, Jiangxi Province Clinical Ophthalmology Institute, No.17 Yongwaizheng Street, Donghu District, Nanchang 330006, Jiangxi Province, China. Electronic address: profchonggangpei@163.com.
  • 4 Department of Ophthalmology, The First Affiliated Hospital of Nanchang University, Jiangxi Province Clinical Ophthalmology Institute, No.17 Yongwaizheng Street, Donghu District, Nanchang 330006, Jiangxi Province, China. Electronic address: profyishao@163.com.
PMID: 25704088 DOI: 10.1016/j.bbrc.2015.02.059
Abstract

Anti-angiogenesis targeting vascular endothelial growth factor receptor 2 (VEGFR2/KDR/Flk-1) has emerged as an important tool for Cancer therapy. The identification of new drugs from Natural Products has a long and successful history. In this study, we described a novel VEGFR2/KDR/Flk-1 inhibitor, rhamnazin, which inhibits tumor angiogenesis and growth. Rhamnazin significantly inhibited proliferation, migration and tube formation of human umbilical vascular endothelial cells (HUVECs) in vitro as well as inhibited sprouts formation of rat aorta ring. In addition, it inhibited vascular endothelial growth factor (VEGF)-induced phosphorylation of VEGFR2/KDR/Flk-1 and its downstream signaling regulator in HUVECs. Moreover, rhamnazin could directly inhibit proliferation of breast Cancer cells MDA-MB-231 in vitro and in vivo. Oral administration of rhamnazin at a dose of 200 mg/kg/day could markedly inhibited human tumor xenograft growth and decreased microvessel densities (MVD) in tumor sections. Taken together, these preclinical evaluations suggest that rhamnazin inhibits angiogenesis and may be a promising Anticancer drug candidate.

Keywords

Angiogenesis; Breast cancer; Rhamnazin; VEGFR2.

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