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Table 1 Effects of various compounds on the chymotrypsin-like activity of 20S rabbit muscle proteasomes1

From: Suppression of nitric oxide induction and pro-inflammatory cytokines by novel proteasome inhibitors in various experimental models

 

Treatment

   

Absorption2

    

#

Assay Mixture

Dexame

Mevino

α-Tocop

δ-Tocotri

Ribofl

Querce

Amilor

(-) Cor Lact

1

20S Prot (20S P)

28486

28486

28486

28486

28486

28486

28486

28486

2

Tris + 20S P = A

25259

25259

25259

25259

25259

25259

25259

25259

3

A + DMSO3 = B

27792 (100)4

27792 (100)4

27792 (100)4

27792 (100)4

27792 (100)4

27792 (100)4

27792 (100)4

27792 (100)4

4

B + 5 μM

22340 (81)

24120 (87)

27389 (99)

21348 (77)

24567 (88)

21670 (78)

33072 (119)

31961 (115)

5

B + 10 μM

19250 (69)

2439 (88)

26890 (97)

20122 (72)

22459 (81)

18768 (68)

55306 (199)

34740 (125)

6

B + 20 μM

16789 (60)

22412 (81)

27560 (99)

15904 (57)

20670 (74)

16342 (59)

77262 (278)

38353 (138)

7

B + 40 μM

15490 (56)

18704 (67)

27180 (98)

16458 (59)

18272 (66)

15246 (55)

115336 (415)

44745 (161)

8

B + 80 μM

12540 (45)

19870 (71)

27141 (98)

18690 (67)

17650 (64)

12560 (45)

178147 (641)

39187 (141)

9

B + 160 μM

9635 (35)

23460 (84)

26870 (97)

21405 (77)

15890 (57)

11345 (41)

191209 (688)

51415 (185)

10

B + 320 μM

8726 (31)

23960 (86)

26560 (96)

25670 (92)

12780 (46)

9650 (35)

219557 (790)

65033 (234)

  1. Dexame = Dexamethasone; Mevino = Mevinolin; α-Tocop = α-Tocopherol; δ-Tocotri = δ-Tocotrienol; Ribofl = Riboflavin; Querce = Quercetin;
  2. Amilor = Amiloride; (-) Cor Lact = (-) Corey Lactone; 20S Prot = 20S Proteasomes.
  3. 1Chymotrypsin-like activity was carried out by using synthetic dipeptide substrate III (Suc-Leu-Leu-Val-Tyr-AMC) in Tris buffer pH 7.5, 0.02 M. 20S rabbit muscle proteasomes was used. Time of incubation was 30 minutes.
  4. 2Fluorescence absorption was measured at excitation = 360 nm and emission = 460 nm.
  5. 3Each compound was dissolved in dimethyl sulfoxide (0.5% DMSO). Appropriate amount of each compound (highest concentration) was dissolved in 1.0 mL DMSO = A stock solution; 50 μL of stock solution A was mixed with 950 μL of media = B solution. The remaining concentrations were prepared from B solution (1:2 dilution) successively.
  6. 4Percentage of control values are in parentheses.