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Table 1 Anti-HIV activity (EC50) and cytotoxicity(LC50) data of R.I.CK-Tat9 based bioconjugates in MT-2 cell culture infected with HIV-1 strain LAV-Vbu3 (MOI of 0.01)a.

From: Novel multi-component nanopharmaceuticals derived from poly(ethylene) glycol, retro-inverso-Tat nonapeptide and saquinavir demonstrate combined anti-HIV effects

Compound

Number

EC50 (μM)

Rb

LC50 (μM)

Therapeutic Index (LC50/EC50)

L-Tat9

-

51.3

-

53.8

1

R.I.CK-Tat9

1

0.85

-

29.8

35

R.I.CK(biotin)-Tat9

2

0.018

0.02

46.8

2600

PEG10 K-(R.I.CK-Tat9)8

8

1.47

1.7

29.1

20

PEG10 K-(R.I.CK(biotin)-Tat9)8

9

1.50

1.8

29.7

20

SQV(MeSO3H) (control)

12

0.015

-

25

1667

SQV-Cys-PEG3.4 K

14

0.90

60

4.5

50

SQV-Cys(R.I.CK-Tat9)-PEG3.4 K

15

0.015

1

12.5

833

  1. aR is the ratio of the EC50 of the bioconjugate to that of its parent drugs R.I.CK-Tat9 or SQV.
  2. bSeveral assays of each compound were done with variations in the virus stock, dosage and days of incubation.