Spirostaphylotrichin X from a Marine-Derived Fungus
as an Anti-influenza Agent Targeting RNA Polymerase PB2
Posted on 2018-12-05 - 21:18
A new spirocyclic γ-lactam,
named spirostaphylotrichin X (1), and three related known
spirostaphylotrichins (2–4) were
isolated from the marine-derived fungus Cochliobolus lunatus SCSIO41401. Their structures were determined by spectroscopic analyses.
Spirostaphylotrichin X (1) displayed obvious inhibitory
activities against multiple influenza virus strains, with IC50 values from 1.2 to 5.5 μM. Investigation of the mechanism
showed that 1 inhibited viral polymerase activity and
interfered with the production of progeny viral RNA. Homogeneous time-resolved
fluorescence, surface plasmon resonance assays, and a molecular docking
study revealed that 1 could inhibit polymerase PB2 protein
activity by binding to the highly conserved region of the cap-binding
domain of PB2. These results suggest that 1 inhibits
the replication of influenza A virus by interfering with the activity
of PB2 protein and that 1 represents a new type of potential
lead compound for the development of anti-influenza therapeutics.
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Wang, Jianjiao; Chen, Feimin; Liu, Yunhao; Liu, Yuxuan; Li, Kunlong; Yang, Xiliang; et al. (2018). Spirostaphylotrichin X from a Marine-Derived Fungus
as an Anti-influenza Agent Targeting RNA Polymerase PB2. ACS Publications. Collection. https://doi.org/10.1021/acs.jnatprod.8b00656
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AUTHORS (9)
JW
Jianjiao Wang
FC
Feimin Chen
YL
Yunhao Liu
YL
Yuxuan Liu
KL
Kunlong Li
XY
Xiliang Yang
SL
Shuwen Liu
XZ
Xuefeng Zhou
JY
Jie Yang
KEYWORDS
polymerase PB 2 protein activity5.5 μ MAnti-influenza Agent Targeting RNA Polymerase PB 2spirocyclic γ- lactamIC 50 valuessurface plasmon resonance assaysHomogeneous time-resolved fluorescenceSpirostaphylotrichin Xinfluenza virus strainsmarine-derived fungus Cochliobolus lunatus SCSIO 41401.spirostaphylotrichinPB 2 protein