Figure 6. Antitumor effect of Z-GP-DAVLBH in multiple tumor xenografts.

(A) Comparative therapeutic efficacy of VLB, DAVLBH, Z-GP-DAVLBH, and Boc-AP-DAVLBH in MDA-MB-231 xenografts. Mice bearing MDA-MB-231 xenografts received an i.v. injection of saline (containing 1% DMSO), VLB, DAVLBH, Z-GP-DAVLBH, or Boc-AP-DAVLBH once every other day for 14 days. Each curve represents the growth of a single tumor in an individual mouse. The dotted vertical lines denote the final day of dosing. (B) Detection of the anticancer spectrum of Z-GP-DAVLBH. Mice bearing HepG2 xenografts (n = 5), A549 xenografts (n = 5), HeLa xenografts (n = 5), CNE-2 xenografts (n = 6), invasive ductal carcinoma patient-derived xenografts (PDX, n = 5), and hepatocellular carcinoma PDX (n = 5) received an i.v. injection of Z-GP-DAVLBH (2.0 μmol/kg) once every other day for 12 or 14 days. Mice in the vehicle group received saline (containing 1% DMSO) only. (C and D) The antitumor effects of Z-GP-DAVLBH in the large MDA-MB-231 tumor experiment. Mice bearing MDA-MB-231 xenografts received 2.0 μmol/kg i.v. injection of Z-GP-DAVLBH or saline containing 1% DMSO once every other day for 16 or 32 days, until the tumor volume reached approximately (C) 750 mm³ (n = 5) or (D) 2,500 mm³ (n = 5). For B–D, the tumor volume (left) and the tumor weight (right) are shown. The results are expressed as mean ± SEM. *P < 0.05; **P < 0.01; ***P < 0.001 versus the vehicle group based on a 2-tailed unpaired t test.