Levo‐Tetrahydropalmatine Attenuates Bone Cancer Pain by Inhibiting Microglial Cells Activation

Abstract

Objective. The present study is to investigate the analgesic roles of L-THP in rats with bone cancer pain caused by tumor cell implantation (TCI). Methods. Thermal hyperalgesia and mechanical allodynia were measured at different time points before and after operation. L-THP (20, 40, and 60 mg/kg) were administrated intragastrically at early phase of postoperation (before pain appearance) and later phase of postoperation (after pain appearance), respectively. The concentrations of TNF-α, IL-1β, and IL-18 in spinal cord were measured by enzyme-linked immunosorbent assay. Western blot was used to test the activation of astrocytes and microglial cells in spinal cord after TCI treatment. Results. TCI treatment induced significant thermal hyperalgesia and mechanical allodynia. Administration of L-THP at high doses significantly prevented and/or reversed bone cancer-related pain behaviors. Besides, TCI-induced activation of microglial cells and the increased levels of TNF-α and IL-18 were inhibited by L-THP administration. However, L-THP failed to affect TCI-induced astrocytes activation and IL-1β increase. Conclusion. This study suggests the possible clinical utility of L-THP in the treatment of bone cancer pain. The analgesic effects of L-THP on bone cancer pain maybe underlying the inhibition of microglial cells activation and proinflammatory cytokines increase.

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“…Clinically, L-THP is traditional Chinese medicine for 40 years and used for the treatment of cardiovascular and a lot of pains [14,15]. Studies have been demonstrated that L-THP shows a protective role in cardio, blood vessels and neural tissues via anti-apoptosis, anti-oxidant and anti-inflammation [16][17][18]. As previously reported, natural alkaloids have also been shown their brilliant anti-cancer activities in some human cancers, such as leukemia and prostate cancer [19,20].…”

Dehydrocorydaline attenuates bone cancer pain by shifting microglial M1/M2 polarization toward the M2 phenotype

“… 2 , 25 Microglia exert a function in the spinal cord similar to that of macrophages in the periphery and play an important role in promoting the development of BCP. 6 , 7 , 26 – 28 It is observed that microglia in resting state are highly dynamic in vivo. They continuously scan their immediate environment and interact with other elements in central nervous system (CNS).…”

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“…One of the main active ingredients of CYHS, tetrahydropalmatine, also known as fumarate B (dl-THP), 90 prevents hyperlipidemia, 91 attenuates neuronal apoptosis induced by cerebral ischemia-reperfusion injury, 92 offers neuroprotection, 93 has antitumor effects, 94 provides analgesia, 95 prevents memory impairment, 96 and ameliorates the development of anxiety and depression. 97,98 Asparagus cochinchinensis (Lour.)…”