Shikonin inhibits the growth and N-acetylation of 2-aminofluorene in Helicobacter pylori from ulcer patients.
N-acetyltransferase (NAT) plays an important role in the N-acetylation of arylamine carcinogens and drugs. Shikonin has been shown to induce apoptosis and inhibit angiogenesis in vivo and in vitro. In this study, shikonin elicited dose-dependent bacteriostatic activity in Helicobacter pylori cultures. Arylamine N-acetyltransferase (NAT) activity (N-acetylation of 2-aminofluorene) was determined in the Helicobacter pylori isolated from peptic ulcer patients. Bacterial cytosols or intact cells with or without specific concentrations of shikonin co-treatment showed different percentages of 2-aminofluorene acetylation. Shikonin also inhibited N-acetylation of 2-aminofluorene in these examined Helicobacter pylori cytosols and intact cells in a dose-dependent manner. The apparent values of Km and Vmax were decreased after co-treatment with 4 microM shikonin in the cytosol of Helicobacter pylori.
Kuo
Hsiu-Maan
HM
Department of Parasitology, China Medical University, Taichung 400, Taiwan, ROC.
Hsia
Te-Chun
TC
Chuang
Yao-Chen
YC
Lu
Hsu-Feng
HF
Lin
Shuw-Yun
SY
Chung
Jing-Gung
JG
D000107:Acetylation / Q000187:drug effects; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000494:pharmacology*; D001191:Arylamine N-Acetyltransferase / Q000037:antagonists & inhibitors* / Q000378:metabolism; D004305:Dose-Response Relationship, Drug; D005449:Fluorenes / Q000378:metabolism*; D016480:Helicobacter pylori / Q000187:drug effects* / Q000201:enzymology / Q000254:growth & development / Q000378:metabolism; D006801:Humans; D007700:Kinetics; D009285:Naphthoquinones / Q000494:pharmacology*; D010437:Peptic Ulcer / Q000382:microbiology
D000894:Anti-Inflammatory Agents, Non-Steroidal; D005449:Fluorenes; D009285:Naphthoquinones; C012177:2-aminofluorene; C016101:shikonin; D001191:Arylamine N-Acetyltransferase