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2010 ; 88
(2
): 160-8
Nephropedia Template TP
gab.com Text
Twit Text FOAVip
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English Wikipedia
Identification of phenanthroindolizines and phenanthroquinolizidines as novel
potent anti-coronaviral agents for porcine enteropathogenic coronavirus
transmissible gastroenteritis virus and human severe acute respiratory syndrome
coronavirus
#MMPMID20727913
Yang CW
; Lee YZ
; Kang IJ
; Barnard DL
; Jan JT
; Lin D
; Huang CW
; Yeh TK
; Chao YS
; Lee SJ
Antiviral Res
2010[Nov]; 88
(2
): 160-8
PMID20727913
show ga
The discovery and development of new, highly potent anti-coronavirus agents and
effective approaches for controlling the potential emergence of epidemic
coronaviruses still remains an important mission. Here, we identified tylophorine
compounds, including naturally occurring and synthetic phenanthroindolizidines
and phenanthroquinolizidines, as potent in vitro inhibitors of enteropathogenic
coronavirus transmissible gastroenteritis virus (TGEV). The potent compounds
showed 50% maximal effective concentration (EC??) values ranging from 8 to 1468
nM as determined by immunofluorescent assay of the expression of TGEV N and S
proteins and by real time-quantitative PCR analysis of viral yields. Furthermore,
the potent tylophorine compounds exerted profound anti-TGEV replication activity
and thereby blocked the TGEV-induced apoptosis and subsequent cytopathic effect
in ST cells. Analysis of the structure-activity relations indicated that the most
active tylophorine analogues were compounds with a hydroxyl group at the C14
position of the indolizidine moiety or at the C3 position of the phenanthrene
moiety and that the quinolizidine counterparts were more potent than
indolizidines. In addition, tylophorine compounds strongly reduced cytopathic
effect in Vero 76 cells induced by human severe acute respiratory syndrome
coronavirus (SARS CoV), with EC?? values ranging from less than 5 to 340 nM.
Moreover, a pharmacokinetic study demonstrated high and comparable oral
bioavailabilities of 7-methoxycryptopleurine (52.7%) and the naturally occurring
tylophorine (65.7%) in rats. Thus, our results suggest that tylophorine compounds
are novel and potent anti-coronavirus agents that may be developed into
therapeutic agents for treating TGEV or SARS CoV infection.