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Table 2 Inhibition parameters of circulating alkaloids and saponins against several CYP and UGT isozymes

From: Multiple circulating alkaloids and saponins from intravenous Kang-Ai injection inhibit human cytochrome P450 and UDP-glucuronosyltransferase isozymes: potential drug–drug interactions

Compounds

Isozymes

Inhibition type

Ki (μM)

α

R2

AICs

SCs

Selection

Cmax/Ki

Astragaloside IV (B2)

CYP2C9

Competitive

17.4 ± 3.7

0.9480

− 113.3

− 110.3

  
  

Noncompetitive

55.8 ± 5.3

0.9708

− 124.8

− 121.8

0.04

  

Mixed-type

45.0 ± 16.6

1.5 ± 1.0

0.9713

− 123.1

− 119.2

  

Ginsenoside Rg1 (C6)

UGT1A1

Competitive

140.6 ± 10.5

0.9952

176.4

179.4

0.01

  

Noncompetitive

187.2 ± 12.7

0.9943

179.8

182.8

  
  

Mixed-type

147.3 ± 29.9

8.3 ± 37.2

0.9952

178.7

182.7

  

Ginsenoside Re (C9)

CYP2C8

Competitive

8.2 ± 1.1

0.9790

− 121.3

− 118.3

  
  

Noncompetitive

26.5 ± 2.2

0.9793

− 121.6

− 118.6

  
  

Mixed-type

13.3 ± 2.9

4.2 ± 2.3

0.9862

− 127.8

− 123.8

0.1

Ginsenoside Rd (D2)

CYP2B6

Competitive

10.2 ± 2.1

0.9484

19.4

22.4

  
  

Noncompetitive

37.2 ± 2.3

0.9877

− 9.2

− 6.2

0.02

  

Mixed-type

36.3 ± 10.2

1.0 ± 0.4

0.9877

− 7.2

− 3.2

  

Ginsenoside Rd (D2)

CYP3A4

Competitive

8.7 ± 2.3

0.9226

− 31.9

− 28.9

  
  

Noncompetitive

32.8 ± 2.2

0.9846

− 64.2

− 61.2

0.02

  

Mixed-type

44.2 ± 16.2

0.6 ± 0.3

0.9854

− 63.3

− 59.3

  

Ginsenoside Rc (D3)

UGT1A9

Competitive

8.9 ± 1.5

0.9634

122.8

125.8

  
  

Noncompetitive

22.3 ± 1.4

0.9877

100.9

103.9

0.04

  

Mixed-type

27.0 ± 7.5

0.7 ± 0.3

0.9881

102.3

106.3

  

Ginsenoside Rb1 (D5)

CYP2C9

Competitive

8.2 ± 1.0

0.9812

− 115.9

− 112.9

  
  

Noncompetitive

16.1 ± 0.9

0.9921

− 133.2

− 130.3

0.03

  

Mixed-type

18.8 ± 4.3

0.7 ± 0.3

0.9923

− 131.8

− 127.9

  
  1. Data represent the mean ± standard deviation of triplicate
  2. Cmax/Ki also named [I]/Ki standard ([I]/Ki < 0.1, low possibility DDI; 1 > [I]/Ki > 0.1, medium possibility DDI; [I]/Ki > 1, high possibility DDI)