Inhibition of xanthine oxidase by benzothiazinone analogues

Shiow Yunn Sheu, Chun Yu Lin, Jen Der Wu, Hsüch Ching Chiang

Research output: Contribution to journalArticle

9 Citations (Scopus)

Abstract

Fourteen synthetic benzothiazinone analogues were tested for their inhibitory effects on xanthine oxidase. The enzyme, xanthine oxidase (XO) catalyses the oxidation of hypoxanthine to xanthine and of xanthine to uric acid, which has a λmax of 295 nm, forming the basis for a spectrophotometric assay for the activity of xanthine oxidase. The results showed that 2-amino-4H-1,3-benzothiazine-4-one (1), 2-guanidino-4H-1,3-benzothiazin-4-one (2) and rhodanine (3) display inhibitory effects on xanthine oxidase with an order of activity of IC-50 = 5.54, 5.60 and 121.40 μM respectively. The apparent inhibition constants (Ki) were 5.12, 19.47 and 206.23 μM, and induced non-competitive, mixed type (non-competitive-uncompetitive) and mixed type (non-competitive-uncompetitive) inhibitions respectively with respect to the substrate xanthine.

Original languageEnglish
Pages (from-to)119-123
Number of pages5
JournalAnticancer Research
Volume19
Issue number1 A
Publication statusPublished - 1999

Fingerprint

Xanthine Oxidase
Xanthine
Rhodanine
Hypoxanthine
Uric Acid
Enzymes

Keywords

  • 2-Amino-4H-1,3-benzothiazin-4-one
  • 2-Guanidino-4H-1,3-benzothiazin-4-one
  • Antihypertension
  • Benzothiazinones
  • Xanthine oxidase inhibitors

ASJC Scopus subject areas

  • Cancer Research
  • Oncology

Cite this

Inhibition of xanthine oxidase by benzothiazinone analogues. / Sheu, Shiow Yunn; Lin, Chun Yu; Wu, Jen Der; Chiang, Hsüch Ching.

In: Anticancer Research, Vol. 19, No. 1 A, 1999, p. 119-123.

Research output: Contribution to journalArticle

Sheu, SY, Lin, CY, Wu, JD & Chiang, HC 1999, 'Inhibition of xanthine oxidase by benzothiazinone analogues', Anticancer Research, vol. 19, no. 1 A, pp. 119-123.
Sheu, Shiow Yunn ; Lin, Chun Yu ; Wu, Jen Der ; Chiang, Hsüch Ching. / Inhibition of xanthine oxidase by benzothiazinone analogues. In: Anticancer Research. 1999 ; Vol. 19, No. 1 A. pp. 119-123.
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