Journal of Microbiology and Biotechnology

The Korean Society for Microbiology and Biotechnology (한국미생물·생명공학회)
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Cytotoxicity of Shikonin Metabolites with Biotransformation of Human Intestinal Bacteria

  • Min, Byung-Sun (Institute of National Medicine, Toyama Medical and Pharmaceutic University) ;
  • Meselhy, Meselhy-R. (Institute of National Medicine, Toyama Medical and Pharmaceutic University) ;
  • Hattori, Masao (Institute of National Medicine, Toyama Medical and Pharmaceutic University) ;
  • Kim, Hwan-Mook (Advanced Biomaterial Research Center, Korea Research Institute of Bioscience and Biotechnology) ;
  • Kim, Young-Ho (College of Pharmacy, Chungnam National University)
  • Published : 2000.08.01
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Abstract

Abstracts Six shikonin metabolites were obtained from human intestinal bacteria, Bacteriodes fragilis subsp. thetaotus. following biotransformation. The transformation of shikonin (1) was performed anaerobically for 3 day at $37^{\circ}C$ in thc bacterial suspension of B. Fagilis which was cultured overnight in GAM broth. The incubation mixture \vas extracted with EtGAc Lo give a dark-brown residue. The residue was apphed to a silica gel column, which was eluted successively with hexane (Fr. A), $CHCl_3$ (Fr. B), and $CHCl_3$:MeOH (9:I) (Fr. C). Six metabolites. Fr.A (2 and 3), Fr. B (6 and 7), and Fr. C (4 and 5) were isolated by repeated silica gel column chromatography, preparatlVe TLC, followed by Sephadex LH-20. In vitro cytotoxicities were tested against human tumor cell lines; PC-3 (prostate), ACHN (renal), A549 (lung), SW620 (colon), KS62 (leukemia), and Du145 (prostate). The shikonin metabolites 2. 4, 5, and 6 showed weaker cytotoxicity than the parenL shikonin (1). whereas shikonin monomenc metabolite 3 ($ED_{50}{\;}O.44-{\;}1.22{\;}\mu\textrm{g}/ml$) and dimeric metabolite 7 ($ED_{50}{\;}O.48-{\;}2.35{\;}\mu\textrm{g}/ml$) exhibited stronger activities compared with adriamycin, which was used as the positive control.ontrol.

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References

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