An opioid peptide analog relieves inflammatory allodynia by the direct
inhibition of microglial activation: a μ opioid receptor independent
effect
Abstract
Background and Purpose: Opioids are widely used in the treatment of
moderate and severe pain. Nociceptive stimulation and classical opioids
have been reported to potentially promote microglial activation and
neuroinflammation, which also reduces the analgesic effect of opioid
drugs and causes chronic pain sensitization. The aim of this study was
to demonstrate whether the novel opioid agonist MEL-0614 could inhibit
activated microglia and neuroinflammation while facilitating recovery
from persistent pain. Experimental approach: Mice were administered
lipopolysaccharide and formalin to induce allodynia. Von Frey test was
used to detect the anti-allodynia effect of MEL-0614 before and after
LPS and formalin injection. In the spinal cord, the levels of
proinflammatory cytokines and microglial activation were determined
after MEL-0614 administration. BV2 and primary microglia were cultured
to further explore the effect of MEL-0614 on LPS-induced microglial
activation and key signalling pathways involved. Key results: MEL-0614
prevented and reversed allodynia induced by LPS and formalin in vivo,
which was not inhibited by the μ opioid receptor antagonist CTAP.
MEL-0614 also downregulated the activation of microglia and related
proinflammatory cytokines in the spinal cord. Additionally, in BV2 and
primary microglia, MEL-0614 inhibited the LPS-induced upregulation of
proinflammatory factors, which was unaffected by CTAP. The NOD-like
receptor protein 3-related signalling pathway may be involved in the
interaction between MEL-0614 and microglia. Conclusion and Implications:
The opioid agonist MEL-0614 inhibited the activation of microglia and
the subsequent upregulation of proinflammatory factors both in vivo and
in vitro. Notably, this effect is not mediated by the opioid receptors.