Antiangiogenic activities and cisplatin-combined antitumor activities of BPR0L075

Ching Ping Chen, Chih Bo Hu, Kai Chia Yeh, Jen Shin Song, Teng Kuang Yeh, Fei Feng Tung, Ling Ling Hwang, Huan Yi Tseng, Yu Chen Huang, Horng Shing Shy, Su Huei Hsieh, Chien Chang Shen, Hsin Sheng Wang, Hsing Pang Hsieh, Jing Ping Liou, Yu Sheng Chao, Chiung Tong Chen

Research output: Contribution to journalArticlepeer-review

15 Citations (Scopus)


Background: Antimitotic tubulin-binding BPR0L075 is structurally analogous to the vascular-disrupting combretastatin A-4. Materials and Methods: In vitrei in vivo models of endothelial cells cultures, Matrigel™ plug assay, tumor-bearing nude mice, and murine leukemia cells-inoculated mice were utilized to evaluate BPR0L075 for antiangiogenic and antitumoral activity spectra. Results: BPR0L075 concentration-dependently inhibited proliferation and migration of human umbilical vein endothelial cells (HUVECs), disrupted capillary tube formations of HUVECs and rat aorta endothelial cells, and suppressed in vivo VEGF-mediated angiogenesis in Matrigel™ plugs in mice. Besides inhibiting the colony growth of cancer cells, BPR0L075 suppressed growth of subcutaneously-xenografted human lung, colorectal, and cervical solid tumors in nude mice. Combination treatments of BPR0L075 plus cisplatin, compared to either agent alone, demonstrated a stronger growth inhibition against the tumor xenografts in nude mice and longer lifespan in the leukemia mice. Conclusion: BPR0L075 is an antitumoral and antiangiogenic agent and potentiates the anticancer activity of cisplatin.

Original languageEnglish
Pages (from-to)2813-2822
Number of pages10
JournalAnticancer Research
Issue number7
Publication statusPublished - Jul 2010


  • Angiogenesis
  • Cisplatin
  • Combretastatin
  • Microtubule
  • Vascular disrupting agent

ASJC Scopus subject areas

  • Oncology
  • Cancer Research


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