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. 2021 Jul 27;14(8):726. doi: 10.3390/ph14080726

Table 8.

Anti-inflammatory targets of Harpagophytum preparations and compounds.

IC50 Reference
Extract/Fraction Harpagoside (%) Cys-LT TXB2 Enzyme
Inhibitors
IL-6 IL-1β NF-κB COX-2
Special extract WS1531 7.3 9.2 µM/L 55.3 µM/L [332,333]
7.3 62 µg/mL 373 µg/mL [285]
Aqueous ethanolic H. procumbens extract 2.1 1450 µg/mL - [285]
542 μg/mL (HNE) [199,201]
547.69/601.49 µg/mL (MPO) * [349]
<100 µg/mL [297]
H. procumbens tincture 915.55/776.49 µg/mL (MPO) * [349]
Aqueous ethanolic H. zeyheri extract 1012 µg/mL (HNE) [199,201]
Aqueous H. procumbens extract 8.9 0.55 µg/mL [350]
27 0.2 µg/mL [350]
Ethanolic H. procumbens extract 65.5 µg/mL (FAAH) [304]
Ethyl acetate fraction of aqueous ethanolic H. procumbens extract 19.95 391 µg/mL - [285]
Butanol fraction of aqueous ethanolic H. procumbens extract 19.5 565 µg/mL 203 µg/mL [285]
Methanolic H. procumbens extract 1046 µg/mL [295]
H. procumbens extracts and isolates ~125 µg/mL [296]
Isolated compounds
Harpagoside 30 µM/L 48.6 µM/L [332,333]
39 μM/L 49 μM/L [285]
1041 µg/mL [295]
>600 µg/mL (HNE) [199,201]
92.7 µM (AChE) [351]
95.6 µM (AChE) [351]
96.4 µM [293]
14.04 µM [302]
Harpagide 1186 µg/mL [295]
8-PCHG 179 µg/mL (HNE) [199,201]
95.6 µM (AChE) [351]
Pagoside 154 µg/mL (HNE) [199,201]
Caffeic acid 86 µg/mL (HNE) [199,201]
Acetoside >500 µg/mL (HNE) [199,201]
19.9 µM (AChE), 35 µM (BChE) [351]
Isoacetocide 179 µg/mL (HNE) [199,201]
21.6 µM (AChE), 29.7 µM (BChE) [351]
Decaffeoylverbascoside 16.1 µM (AChE), 46 µM (BChE) [351]
6′-O-Acetylacteosid 47 µg/mL (HNE) [199,201]

* Formyl methionyl leucine phenylalanine- and arachidonic acid-stimulated, respectively.