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Table 1 Summary of the pharmacological effects exerted by MH, 27a, 32, and 34a

From: 4′-O-methylhonokiol increases levels of 2-arachidonoyl glycerol in mouse brain via selective inhibition of its COX-2-mediated oxygenation

IC 50 or K i values (mean value ± SD, μM)

 

h COX-2

RAW264.7 Intact cells

CHO membranes

CHO cells

Pig brain homog.

BV-2 homog.

U937 cells

 

AA

2-AG

AA

2-AG

h CB 1

h CB 2

h CB2 [ 35 S] GTPγS

h CB2 cAMP

FAAH

MAGL

ABHDs

AEA uptake

MH

0.58 ± 0.08

**0.15 ± 0.09

1.56 ± 0.12

**0.28 ± 0.09

2.4 ± 0.6

0.19 ± 0.12

0.20 ± 0.10

0.67 ± 0.07

>10

>10

>10

6.5 ± 1.2

27a

1.21 ± 0.08

**0.42 ± 0.09

0.98 ± 0.08

**0.28 ± 0.11

0.79 ± 0.10

0.11 ± 0.09

0.18 ± 0.09

0.71 ± 0.09

>10

>10

>10

>10

32

10.2 ± 0.12

**0.63 ± 0.05

2.8 ± 0.22

**0.21 ± 0.14

>10

>10

n.d.

n.d.

>10

>10

>10

6.3 ± 1.6

34a

4.31 ± 0.10

*1.29 ± 0.07

>30

**1.57 ± 0.13

1.12 ± 0.15

0.35 ± 0.11

1.82 ± 0.14

1.52 ± 0.13

>10

>10

>10

>10

DuP-697

0.061 ± 0.005

0.07 ± 0.01

0.004 ± 0.004

0.005 ± 0.006

n.d.

n.d.

n.d.

n.d.

n.d.

n.d.

n.d.

n.d.

  1. The data are expressed as mean ± SD of at least three independent experiments each performed in triplicates. Binding affinity to CB1 and CB2 receptors is expressed as K i value while modulation of CB2 receptor activation (cAMP and [35S] GTPγS) and inhibition of enzyme activity and AEA uptake are expressed as IC50 value. *P < 0.05; **P < 0.01 PGE2-GE vs. PGE2. n.d.: not determined P < 0.05; **P < 0.01 PGE2-GE vs. PGE2. Items in bold are compound abbreviations.