Stability and Bioavailability of Lentztrehaloses A, B, and C as Replacements for Trehalose.
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.
Institute of Microbial Chemistry (BIKAKEN) , 3-14-23 Kamiosaki, Shinagawa-ku, Tokyo 141-0021, Japan.
Shun-Ichi
S
Wada
Institute of Microbial Chemistry (BIKAKEN) , 3-14-23 Kamiosaki, Shinagawa-ku, Tokyo 141-0021, Japan.
Ryuichi
R
Sawa
Institute of Microbial Chemistry (BIKAKEN) , 3-14-23 Kamiosaki, Shinagawa-ku, Tokyo 141-0021, Japan.
Shun-Ichi
S
Ohba
Institute of Microbial Chemistry (BIKAKEN) , 3-14-23 Kamiosaki, Shinagawa-ku, Tokyo 141-0021, Japan.
Chigusa
C
Hayashi
Institute of Microbial Chemistry (BIKAKEN) , 3-14-23 Kamiosaki, Shinagawa-ku, Tokyo 141-0021, Japan.
Maya
M
Umekita
Institute of Microbial Chemistry (BIKAKEN) , 3-14-23 Kamiosaki, Shinagawa-ku, Tokyo 141-0021, Japan.
Yuko
Y
Shibuya
Institute of Microbial Chemistry (BIKAKEN) , 3-14-23 Kamiosaki, Shinagawa-ku, Tokyo 141-0021, Japan.
Kiyoko
K
Iijima
Institute of Microbial Chemistry (BIKAKEN) , 3-14-23 Kamiosaki, Shinagawa-ku, Tokyo 141-0021, Japan.
Fumiki
F
Iwanami
Institute of Microbial Chemistry (BIKAKEN) , 3-14-23 Kamiosaki, Shinagawa-ku, Tokyo 141-0021, Japan.
Masayuki
M
Igarashi
D000818:Animals; D001441:Bacteroides fragilis / Q000187:drug effects / Q000378:metabolism; D001682:Biological Availability; D002176:Candida albicans / Q000187:drug effects / Q000254:growth & development; D045744:Cell Line, Tumor; D004195:Disease Models, Animal; D013293:Enterococcus faecalis / Q000187:drug effects / Q000378:metabolism; D005243:Feces / Q000737:chemistry; D005260:Female; D006801:Humans; D007413:Intestinal Mucosa / Q000378:metabolism; D007422:Intestines / Q000166:cytology / Q000187:drug effects; D051379:Mice; D008813:Mice, Inbred ICR; D016982:Micrococcus luteus / Q000187:drug effects / Q000254:growth & development; D020102:Mycobacterium smegmatis / Q000187:drug effects / Q000378:metabolism; D014199:Trehalose / Q000031:analogs & derivatives* / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics* / Q000652:urine
C000588806:4-O-(2,3-dihydroxy-3-methylbutyl)trehalose; D014199:Trehalose
bioavailability; lentztrehalose; pharmacokinetics; stability; trehalase; trehalose