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Table 4 The IC50 values of NK-B transactivation and pro-inflammatory mediators of the compounds isolated or semi-synthesized from A. paniculat a EtOAc extract

From: Isolation and identification of bioactive compounds in Andrographis paniculata (Chuanxinlian)

Compounds

NF-κB

TNFα

IL-6

MIP-2

NO

Semi-synthetic analogues

  

(μg/ml)

  

   3,19-O-diacetylanhydroandrographolide

2.2

2.89

2.08

1.29

2.02

   19-O-acetylanhydroandrographolide

2.4

3.85

2.75

2.29

2.08

Diterpenoids

     

   14-deoxy-14,15-dehydroandrographolide

2.0

2.18

2.14

2.07

2.05

   19-O-acetyl-14-deoxy-11,12-didehydroandrographolide

4.4

5.07

3.94

4.41

4.11

Synthetic analogues

     

   hexahydro-14-dehydroxyandrographolide

4.2

5.2

3.78

4.52

4.24

   3,19-dioxolabda-8(17),11E, 13-trien-16,15-olide

4.1

5.78

3.97

4.67

4.52

Steroids

     

   ergosterol peroxide

4.7

4.71

5.32

4.55

4.67

   β-sitosterol and stigmasterol

5.2

5.34

5.97

4.88

4.55

Flavonoids

     

   5-hydroxy-7,8-dimethoxyflavone

6.1

4.33

5.34

3.63

5.11

   5-hydroxy-7,8-dimethoxyflavanone

6.7

4.37

5.14

4.01

4.57

Diterpenoids

     

   andrographolide (major compound)

9.4

5.62

8.93

5.48

8.48

   14-deoxy-11,12-didehydroandrographolide

17.1

20.64

23.6

15.03

11.26

  1. NF-κB trans-activation activity was assay as following: RAW 264.7 macrophages transiently transfected with NF-κB reporter plasmids were pretreated various compounds and then stimulated with LPS 100 ng/mL/IFN-γ 1000 units/mL for further was estimated by the Dual-Glo Luciferase reporter assay. The collected cell supernatants were assayed for TNFα, IL-6, and MIP-2 productions using commercial ELISA kits. NO was determined by Griess assay [17].