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对β葡萄糖苷酶的抑制
XENOBIOTICA, 1993, VOL. 23, NO. 1, 5-10
Inhibition of /?-glucuronidaseby natural
glucuronides of Kampo medicines using
glucuronide of SN-38(7-ethyl-10-
hydroxycamptothecin) as a substrate
2 M. NARITAt, E. NAGAIS, H. HAGIWARA4, M. ABURADAI,
1
/
9
2 T. YOKOIT and T. KAMATAKI?
/
0
1
n t Division of Drug Metabolism, Faculty of Pharmaceutical Sciences,
o
v. Hokkaido University, Sapporo 060, Japan
i 1Research Institute, Daiichi Pharmaceutical Co. Ltd, Edogawa-ku, Tokyo 134, Japan
n
U
8Yakult Central Institute, Yakult Co. Ltd, Kunitachi, Tokyo 186, Japan
e
p T Tsumura Research Institute for Pharmacology, Tsumura Co., Ami, lbaraki 300-1 1,
e
t
t
e Japan
c
a
H
y Received 8 April 1992; accepted 26 August 1992
b
.
m y
o l 1. 7-Ethyl-lO-[4-(piperidino)-l-piperidino]carbonyloxycamptothecin (CPT-1l), a
c n
. o
e e potent anticancer agent currently under development for clinical use, is metabolized in viwo
r
a s
c u to 7-ethyl-10-hydroxycamptothecin(SN-38),which is subsequently conjugated to 7-ethyl-
h l
t a
l 10-hydroxycamptothecin glucuronide (SN-38-glucuronide). The SN-38-glucuronide was
a n
e o hydrolysed by fi-glucuronidase from E. coli to aglycones and glucuronic acid.
h s
a r
e
m p 2. Four purified nat
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