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Table 1 Apoptosis induced by bortezomib, Aplidin and the Aplidin derivatives PM01215 and PM02781; apoptotic cells were determined by Annexin V positive staining and flow cytometric analysis; results are displayed as % of apoptotic cells (mean ± SEM) on three different donors 24 h after incubation with the respective compounds

From: The Aplidin analogs PM01215 and PM02781 inhibit angiogenesis in vitro and in vivo

HUVEC (n = 3)

Untreated 11.0 ± 0.6

    

concentration [nM]

 

bortezomib

Aplidin™

PM01215

PM 02781

 10

 

45.0 ± 14.0*

10.7 ± 1.3

10.3 ± 0.9

11.0 ± 0.6

 50

 

68.0 ± 11.2*

22.7 ± 2.6*

12.0 ± 0.0

12.7 ± 0.9

 100

 

73.0 ± 10.8*

34.3 ± 2.7*

17.3 ± 0.3*

23.0 ± 2.6*

 200

 

78.3 ± 11.5*

56.0 ± 4.5*

31.0 ± 4.0*

44.3 ± 10. 7*

HDFs (n = 3)

Untreated 5.3 ± 0.3

    

concentration [nM]

 

bortezomib

Aplidin™

PM01215

PM 02781

 10

 

4.7 ± 0.3

4.3 ± 0.3

4.7 ± 0.7

4.7 ± 0.3

 50

 

7.7 ± 0.7

5.3 ± 0.7

4.3 ± 0.3

4.7 ± 0.3

 100

 

10.3 ± 0.7*

9.0 ± 0.4

4.3 ± 0.3

6.3 ± 0.3

 200

 

12.7 ± 1.7*

12.3 ± 0.7*

6.0 ± 1.0

7.3 ± 1.2

PBMNC (n = 3)

Untreated 11.3 ± 0.9

    

concentration [nM]

 

bortezomib

Aplidin™

PM01215

PM 02781

 10

 

9.7 ± 2.3

10.3 ± 1.2

9.7 ± 0.9

10.0 ± 1.5

 50

 

25.0 ± 1.0*

11.7 ± 1.3

9.7 ± 1.3

10.0 ± 1.2

 100

 

28.0 ± 2.0*

12.3 ± 1.7

9.7 ± 1.3

11.7 ± 2.3

 200

 

29.7 ± 2.3*

19.3 ± 1.7*

11.0 ± 1.5

12.7 ± 1.9

  1. Primary cells were human umbilical vein endothelial cells (HUVECs), human diploid fibroblasts from bone marrow (HDFs) and human peripheral blood mononuclear cells (PBMNCs). *Indicates p value < 0.05