Protective role of intestinal bacterial metabolism against baicalin-induced toxicity in HepG2 cell cultures

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  • Khanal Tilak
    Department of Toxicology, College of Pharmacy, Chungnam National University
  • Kim Hyung Gyun
    Department of Toxicology, College of Pharmacy, Chungnam National University
  • Choi Jae Ho
    Department of Toxicology, College of Pharmacy, Chungnam National University
  • Park Bong Hwan
    Department of Toxicology, College of Pharmacy, Chungnam National University
  • Do Minh Truong
    Department of Toxicology, College of Pharmacy, Chungnam National University
  • Kang Mi Jeong
    College of Pharmacy, Yeungnam University, South Korea
  • Yeo Hee Kyung
    Department of Food and Nutrition, Kyung Hee University, South Korea
  • Kim Dong Hyun
    College of Pharmacy, Kyung Hee University, South Korea
  • Kang Wonku
    College of Pharmacy, Yeungnam University, South Korea
  • Jeong Tae Cheon
    College of Pharmacy, Yeungnam University, South Korea
  • Jeong Hye Gwang
    Department of Toxicology, College of Pharmacy, Chungnam National University

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Baicalin, a glycoside present in Scutellaria baicalensis Georgi, is metabolized to its aglycone, baicalein, in intestine. In the present study, possible role of metabolism of baicalin by intestinal bacteria to baicalein in baicalin-induced toxicity was investigated in HepG2 cell cultures. As an intestinal bacterial metabolic system for baicalin, human fecal preparation containing intestinal microflora (fecalase) was employed. Initially, when cytotoxic effects of baicalin and baicalein were compared, baicalin was more cytotoxic than baicalein in HepG2 cells. When baicalin was incubated with fecalase, it was metabolized to baicalein. In addition, baicalin-incubated with fecalase reduced cytotoxicity of HepG2 cells in a concentration-dependent manner. Moreover, baicalin-incubated with fecalase significantly caused an increase in Bcl-2 expression together with a decrease in Bax expression and cleaved Caspase-3. Furthermore, anti-apoptotic effect by the incubation of baicalin with fecalase was also confirmed by the terminal deoxynucleotidyltransferase-mediated dUTP-biotin nick-end labeling assay. Taken all together, the findings suggested that metabolism of baicalin by human fecalase to baicalein might have protective effects against baicalin-induced toxicity in HepG2 cells.

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