Metabolism of 6"-O-xylosyltectoridin and tectoridin by human intestinal bacteria and their hypoglycemic and in vitro cytotoxic activities.
6"-O-Xylosyltectoridin and tectoridin isolated from the flowers of Pueraria thunbergiana (Leguminosae), are metabolized to tectorigenin by human intestinal bacteria. Although tectoridin is metabolized to tectorigenin by most intestinal bacteria, 6"-O-xylosyltectoridin is metabolized to tectorigenin via tectoridin by only a few intestinal bacteria, such as Bifidobacterium breve K-110 and Eubacterium A-44. The metabolite, tectorigenin, had more potent hypoglycemic activity as well as in vitro cytotoxic activity against tumor cell lines than 6"-O-xylosyltectoridin and tectoridin. These results suggest that 6"-O-xylosyltectoridin and tectoridin are prodrugs which can be transformed to the active agents by human intestinal bacteria.
Bae
E A
EA
Department of Food and Nutrition, Kyung Hee University, Seoul, Korea.
Han
M J
MJ
Lee
K T
KT
Choi
J W
JW
Park
H J
HJ
Kim
D H
DH
D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000302:isolation & purification / Q000494:pharmacology*; D001644:Bifidobacterium / Q000378:metabolism; D004354:Drug Screening Assays, Antitumor; D005051:Eubacterium / Q000378:metabolism; D007887:Fabaceae / Q000737:chemistry*; D006801:Humans; D006943:Hyperglycemia / Q000139:chemically induced / Q000188:drug therapy; D007004:Hypoglycemic Agents / Q000494:pharmacology / Q000627:therapeutic use*; D007422:Intestines / Q000382:microbiology; D007529:Isoflavones / Q000378:metabolism* / Q000494:pharmacology / Q000627:therapeutic use*; D008297:Male; D010946:Plants, Medicinal; D051381:Rats; D017207:Rats, Sprague-Dawley; D013311:Streptozocin; D013997:Time Factors; D014407:Tumor Cells, Cultured
C407685:6''-O-xylosyltectoridin; D000972:Antineoplastic Agents, Phytogenic; D007004:Hypoglycemic Agents; D007529:Isoflavones; D013311:Streptozocin; C120039:tectorigenin; C120040:tectoridin