Table 2. Adduct Formation with Albumin (Alb) and/or Plasma Proteins (PP) in Rodents Exposed to Arylamines and Nitroarenes.
PB-indexa total 14C or 3H-label | PB-indexa hydrolyzable adduct | Dose [mmol/kg] | % of dose boundb | Adduct ratio Hb/PPe | Adduct ratio Hb/Albe | |
---|---|---|---|---|---|---|
Benzidine | 1632 (PP)i | ND (PP)186 | 0.0011 | 0.360% | 0.5186 | |
3,3′-Dichlorobenzidine (DCBz) | 529 (PP)i | 138 (PP)186 | 0.05 | 0.166% | 0.2186 | |
1-Nitropyrene | 181 (PP)337 | adductg,337 | 0.00004–0.004 | 0.04%337 | 0.25338 | |
Nitrobenzene | 136 (PP)61 | 79 (PP)186 | 0.2 | 0.0300% | 7.6186 | |
4-Chloroaniline (4CA) | 82 (PP)339 | 19.7 (PP)186 | 0.014 | 0.0181% | 29.3i,186 | |
Acetanilide | 70 (PP)61 | 11.2 (PP)186 | 0.15 | 0.0154% | 2.5186 | |
2-Aminofluorene | 72 (PP)340 | 0.5 | 0.0159% | 2.38f,340 | ||
2-Nitrofluorene | 5.0 (PP)340 | 0.5 | 0.0011% | 0.32f,340 | ||
1-Aminopyrene | 0.44 (PP)340 | 0.5 | 0.0001% | 0.73f,340 | ||
2-Aminonaphthalene | 0.2 (PP)340 | 0.5 | 0.00004% | 50f,340 | ||
2-Nitronaphthalene | NDh(PP)340 | only Hb-adduct340 | ||||
Aniline | ND (PP)340 | 0.5 | only Hb-adductf,h,340 42 in humanf,341 | |||
2-Methylaniline (2MA) | 297 (Alb)193 | ND (Alb)193 | 0.466 | 0.0291% | 0.94193 | |
4,4′-Methylenebis(2-chloroaniline) (MOCA)192 | 279 (Alb)192 | ND (Alb)192 | 0.0037 | 0.027% | 1.0192 | |
2-Amino-3-methylimidazo [4,5-f]quinoline (IQ)88,191 | 223 (Alb) | 22.3 (Alb) | 0.15 | 0.022%d | 0.33–0.288 | |
4-Aminobiphenyl (4ABP)c220 | 204 (Alb)c,j | 0.012 | 0.02% | 25189 |
Protein binding (PB)-index: (pmol compound/mg protein)/(mmol compound/kg body weight).
Calculated with the assumptions: per kg rat there are 0.98 g Alb and or 2.205g plasma proteins (PP).342
After pronase digestion: isolation of the adduct with Trp214 (Ala-Trp-Ala-Val).20
After pronase digestion: N2-(Pro-Tyr-cysteinesulfinyl-)IQ; 0.014–0.043% of the dose bound to Alb = experimental value.
Total binding (= hydrolyzable plus nonhydrolyzable) to Hb devided by total binding to Alb and/or PP.
Ratio of hydrolyzable adducts.
1-Acetylamino-X,Y-diacetoxy-pyrenes.337
ND = not detected
Neumann186 used a PB-index expressed as (mmol compound/mol protein)/(mmol/kg body weight). A molecular weight of 68000 was taken for the calculations.339 Therefore, (106/68000)·[(mmol compound/mol PP)/(mmol compound/kg body weight)] yields the values expressed as [(pmol compound/mg PP)/(mmol compound/kg body weight)]. Differences from the experimental results are due to rounding errors.
This value was calculated from the percentage of the dose bound to Alb and from the dose.