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. 2017 Aug 16;80(8):2284–2294. doi: 10.1021/acs.jnatprod.7b00284

Table 2. Alkaline Phosphatase (AP) Induction (Estrogenicity), Cytotoxicity, and NQO1 Induction Potency of the Hop DESIGNER Extracts and Hop Purified Constituents.

    Ishikawa cells
Hepa1c1c7 cells
  potency efficacy cytotoxicity NQO1 induction
cytotoxicity
material EC50 AP [μg/mL; μM]a max AP induction IC50 [μg/mL; μM]a CDb [μg/mL; μM]a slope r2 IC50 [μg/mL; μM]a
DESIGNER Extracts      
Ex1 0.1 ± 0.02 136.4 ± 7.6 7.0 ± 0.7 6.8 ± 1.9 0.1 ± 0.01 0.80 >20
Ex2 0.4 ± 0.07 119.8 ± 11.4 28.1 ± 8.6 6.3 ± 2.1 0.1 ± 0.008 0.82 >20
Ex3 0.3 ± 0.008 74.7 ± 7.2 3.3 ± 0.4 0.8 ± 0.1 1.3 ± 0.03 0.98 >20
Ex4 0.7 ± 0.05 71.4 ± 8.2 10.3 ± 0.8 1.5 ± 0.2 0.6 ± 0.04 0.86 27.1 ± 2.9
Ex5 NAc NAc 4.8 ± 1.4 1.0 ± 0.1 0.8 ± 0.03 0.96 >20
Ex6 2.2 ± 0.6 66.6 ± 10.8 >80 7.0 ± 0.6 0.1 ± 0.005 0.94 >20
Ex7 NAc NAc 6.2 ± 0.4 1.8 ± 0.2 0.5 ± 0.03 0.85 >20
Ex8 12.0 ± 3.7 52.3 ± 11.2 >80 11.7 ± 3.8 0.08 ± 0.004 0.89 >20
Compounds          
8-PN 0.007 ± 0.004 97.1 ± 2.6 19.1 ± 4.7 >30d NA   >20d
IX 1.4 ± 0.4 80.7 ± 14.5 24.9 ± 3.7 >50d NA   30.7 ± 2.9d
XH NAc NAc 4.2 ± 0.2 1.3 ± 0.7 1.3 ± 0.08 0.88 17.5 ± 2.3
6-PN 0.4 ± 0.1 57.4 ± 10.2 >5 >30d NA   >20d
17β-estradiol (E2)e 0.0002 ± 0.00005 137.0 ± 2.5 NA NDf ND   ND
4′-bromoflavone NDf ND ND 0.02 ± 0.001 19.6 ± 1.5 0.8 >0.7 (>166)g
a

μg/mL for extracts and μM for compounds.

b

CD value: concentration to double NQO1 activity.

c

NA: not active.

d

Dietz et al., 2005.21

e

Hajirahimkhan et al., 2013.29

f

ND: not determined.

g

Song et al., 1999.69