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Table 25 The inhibitory effects of compounds 68-79 on platelet aggregation induced by thrombin, AA., collagen and PAF (in vitro)

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Table 25 The inhibitory effects of compounds 68-79 on platelet aggregation induced by thrombin, AA., collagen and PAF (in vitro)

R

3

R

2

R

1

N O

O O

Et

CH

2

No. Conc.

µg/ml R1 R2 R3 Thrombin 0.1U/ml

10 µM AA Collagen

10 µg/ml PAF

2 ng/ml 68 <100 H H H 79.8±2.6*** 53.5±4.0*** 40.0±13.2** 80.4±2.2**

69 100 CH

3

H H 70.9±3.9*** 39.1±1.4*** 20.9±6.8*** 0.0±0.0***

50 48.2±7.0***

20 80.4±2.2**

70 <100 H CH

3

H 75.1±2.3*** 50.8±4.0*** 36.1±8.1*** 0.0±0.0***

<50 65.0±4.3***

<20 79.4±1.8***

71 100 H H CH

3

64.0 ±7.1** 45.9±4.6*** 30.4±9.5*** 60.3±3.7***

72 100 H OCH

3

H 74.3±1.7*** 56.4±11.0* 34.1±8.0*** 32.2±9.0***

73 100 H H OCH

3

本身促進血小板凝集 54.9±7.8

50 64.0±4.2*** 57.1±3.1*** 36.8±10.3*** 55.5±2.3***

74 <50 Cl H H 58.4±6.7*** 1.4±1.2*** 16.2±2.3*** 0.0±0.0***

<20 79.0±3.6** 65.0±3.3***

<10 72.9±0.6***

< 5 89.8±0.6

75 50 H Cl H 74.0±1.7*** 69.7±3.2*** 62.7±7.7** 47.2±8.0***

76 100 H H Cl 0.0±0.0*** 0.0±0.0*** 0.0±0.0*** 0.0±0.0***

50 86.1±0.5*** 0.0±0.0*** 0.0±0.0***

20 82.2±1.9*** 76.2±2.8***

77 100 F H H 12.3±7.0*** 0.0±0.0*** 0.0±0.0*** 0.0±0.0***

50 58.1±2.4*** 44.6±7.2***

20 83.0±3.1 69.6±5.1**

10 79.4±3.1**

78 50 H F H 70.5±7.5* 61.4±7.7** 7.6±4.6*** 69.4±1.2***

79 100 H H F 55.3±4.9*** 1.1±0.9*** 6.8±2.1*** 0.0±0.0***

50 56.0±7.4*** 70.9±4.8**

20 80.9±1.4***

Control 91.5±0.6 89.2±0.8 90.9±0.7 89.4±0.6

Platelet were incubated with tested sample or 0.5 % DMSO at 37°C for 1 min, then thrombin (0.1U/ml), AA

(10 µM), collagen (10 µg/ml) or PAF (2 ng/ml) was added to trigger the aggregation. Value are presented as

mean ± S.E.. *: P<0.05, **: P<0.01,***: P<0.001, N=3-4.

數據

Table 25 The inhibitory effects of compounds 68-79 on platelet aggregation             induced by thrombin, AA., collagen and PAF (in vitro)

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