Stability and Bioavailability of Lentztrehaloses A, B, and C as Replacements for Trehalose

• Published in: Journal of agricultural and food chemistry Vol. 64; no. 38; pp. 7121 - 7126
• Main Authors: Wada, Shun-ichi, Sawa, Ryuichi, Ohba, Shun-ichi, Hayashi, Chigusa, Umekita, Maya, Shibuya, Yuko, Iijima, Kiyoko, Iwanami, Fumiki, Igarashi, Masayuki
• Format: Journal Article
• Language: English
• Published: United States American Chemical Society 28-09-2016
• Subjects: Animals; Bacteroides fragilis - drug effects; Bacteroides fragilis - metabolism; Biological Availability; Candida albicans - drug effects; Candida albicans - growth & development; Cell Line, Tumor; Disease Models, Animal; Enterococcus faecalis - drug effects; Enterococcus faecalis - metabolism; Feces - chemistry; Female; Humans; Intestines - cytology; Intestines - drug effects; Intestines - metabolism; Mice; Mice, Inbred ICR; Micrococcus luteus - drug effects; Micrococcus luteus - growth & development; Mycobacterium smegmatis - drug effects; Mycobacterium smegmatis - metabolism; Trehalose - analogs & derivatives; Trehalose - blood; Trehalose - chemistry; Trehalose - pharmacokinetics; Trehalose - urine; trehalase; pharmacokinetics; trehalose; bioavailability; lentztrehalose; stability
• ISSN: 0021-8561; 1520-5118
• DOI: 10.1021/acs.jafc.6b02782

Trehalose is widely used as a sweetener, humectant, and stabilizer, but is ubiquitously degraded by the enzyme trehalase expressed in a broad variety of organisms. The stability of the new trehalose analogues lentztrehaloses A, B, and C in microbial and mammalian cell cultures and their pharmacokinetics in mice were analyzed to evaluate their potential as successors of trehalose. Among the 12 species of microbes and 2 cancer cell lines tested, 7 digested trehalose, whereas no definitive digestion of the lentztrehaloses was observed in any of them. When orally administered to mice (0.5 g/kg), trehalose was not clearly detected in blood and urine and only slightly detected in feces. However, lentztrehaloses were detected in blood at >1 μg/mL over several hours and were eventually excreted in feces and urine. These results indicate that lentztrehaloses may potentially replace trehalose as nonperishable materials and drug candidates with better bioavailabilities.