title: Visualization of sialidase activity in Mammalian tissues and cancer detection with a novel fluorescent sialidase substrate.
abstract: Sialidase removes sialic acid from sialoglycoconjugates and plays crucial roles in many physiological and pathological processes. Various human cancers express an abnormally high level of the plasma membrane-associated sialidase isoform.Visualization of sialidase activity in living mammalian tissues would be useful not only for understanding sialidase functions but also for cancer diagnosis. However, since enzyme activity of mammalian sialidase is remarkably weak compared with that of bacterial and viral sialidases, it has been difficult to detect sialidase activity in mammalian tissues. We synthesized a novel benzothiazolylphenol-based sialic acid derivative (BTP-Neu5Ac) as a fluorescent sialidase substrate. BTP-Neu5Ac can visualize sialidase activities sensitively and selectively in acute rat brain slices. Cancer cells implanted orthotopically in mouse colons and human colon cancers (stages T3-T4) were also clearly detected with BTP-Neu5Ac. The results suggest that BTP-Neu5Ac is useful for histochemical imaging of sialidase activities.
authors.affiliation: Department of Biochemistry, School of Pharmaceutical Sciences, University of Shizuoka, Shizuoka, Japan.
authors.forename: Akira
authors.initials: A
authors.lastname: Minami
authors.affiliation: Department of Organic Chemistry, School of Pharmaceutical Sciences, Hiroshima International University, Hiroshima, Japan.
authors.forename: Tadamune
authors.initials: T
authors.lastname: Otsubo
authors.affiliation: Department of Biochemistry, School of Pharmaceutical Sciences, University of Shizuoka, Shizuoka, Japan.
authors.forename: Daisuke
authors.initials: D
authors.lastname: Ieno
authors.affiliation: Department of Organic Chemistry, School of Pharmaceutical Sciences, Hiroshima International University, Hiroshima, Japan.
authors.forename: Kiyoshi
authors.initials: K
authors.lastname: Ikeda
authors.affiliation: Department of Functional Anatomy, School of Nursing, University of Shizuoka, Shizuoka, Japan.
authors.forename: Hiroaki
authors.initials: H
authors.lastname: Kanazawa
authors.affiliation: Department of Medical Biochemistry, School of Pharmaceutical Sciences, University of Shizuoka, Shizuoka, Japan.
authors.forename: Kosuke
authors.initials: K
authors.lastname: Shimizu
authors.affiliation: Department of Gastroenterological Surgery, Shizuoka General Hospital, Shizuoka, Japan.
authors.forename: Ko
authors.initials: K
authors.lastname: Ohata
authors.affiliation: Department of Medical Technology, Shizuoka General Hospital, Shizuoka, Japan.
authors.forename: Tsunehiro
authors.initials: T
authors.lastname: Yokochi
authors.affiliation: Department of Biochemistry, School of Pharmaceutical Sciences, University of Shizuoka, Shizuoka, Japan.
authors.forename: Yuuki
authors.initials: Y
authors.lastname: Horii
authors.affiliation: Department of Biochemistry, School of Pharmaceutical Sciences, University of Shizuoka, Shizuoka, Japan.
authors.forename: Hokuto
authors.initials: H
authors.lastname: Fukumoto
authors.affiliation: Department of Biochemistry, School of Pharmaceutical Sciences, University of Shizuoka, Shizuoka, Japan.
authors.forename: Risa
authors.initials: R
authors.lastname: Taguchi
authors.affiliation: Department of Biochemistry, School of Pharmaceutical Sciences, University of Shizuoka, Shizuoka, Japan.
authors.forename: Tadanobu
authors.initials: T
authors.lastname: Takahashi
authors.affiliation: Department of Medical Biochemistry, School of Pharmaceutical Sciences, University of Shizuoka, Shizuoka, Japan.
authors.forename: Naoto
authors.initials: N
authors.lastname: Oku
authors.affiliation: Department of Biochemistry, School of Pharmaceutical Sciences, University of Shizuoka, Shizuoka, Japan.
authors.forename: Takashi
authors.initials: T
authors.lastname: Suzuki
mesh_terms: D000818:Animals; D001419:Bacteria / Q000201:enzymology; D001921:Brain / Q000378:metabolism; D045744:Cell Line, Tumor; D004789:Enzyme Activation; D005456:Fluorescent Dyes / Q000737:chemistry / Q000633:toxicity; D006801:Humans; D006868:Hydrolysis; D008297:Male; D008322:Mammals; D051379:Mice; D057054:Molecular Imaging / Q000379:methods*; D009369:Neoplasms / Q000175:diagnosis / Q000378:metabolism; D009439:Neuraminidase / Q000378:metabolism*; D051381:Rats; D013379:Substrate Specificity
chemical_list: D005456:Fluorescent Dyes; D009439:Neuraminidase