Abstract
Duhaldea pterocaula (Franch.) Anderb, also known as Inula pterocaula Franch (I. pterocaula), is a folk medicine of the Yi nationality in China. The Inula plants display various biological activities, including anti-nociceptive and anti-inflammatory properties. I. pterocaula has been traditionally used for the treatment of bronchitis, vasculitis, and dizziness. However, very few studies have been reported on the pharmacology of I. pterocaula. The present study aims to characterize the anti-nociceptive and anti-inflammatory properties of I. pterocaula and explore the underlying mechanism. I. pterocaula was extracted by 95% ethanol and further portioned with petroleum ether, ethyl acetate (EA) and n-butanol, sequentially, to obtain corresponding factions with different polarities. The EA fraction (IPEA) was found to be one of the most effective fractions. It demonstrated potent analgesic effects in both acute and inflammatory pain mouse models, and caused no anti-nociceptive tolerance. Furthermore, IPEA improved the tolerance of mice to morphine. IPEA also showed potent anti-inflammatory effects on LPS-induced septic mice. BIC, a GABAAR antagonist, reversed the effects of IPEA in pain and inflammation models. Collectively, GABAARs play a key role in the pharmacological effects of IPEA. I. pterocaula may be useful as a complementary or alternative therapeutic agent for the treatment of pain and inflammation.
Highlights
Pain is a complex biological response and usually accompanies inflammation and injury
The acute anti-nociceptive activity of I. pterocaula (IPEA) was measured in the hot plate assay, which recorded responses to a thermal stimulus
As part of our ongoing project of discovering new analgesics, the present study aims to investigate the analgesic properties of I. pterocaula, a folk medicine in China
Summary
Pain is a complex biological response and usually accompanies inflammation and injury. Chronic pain is maladaptive and associated with inflammation (Oh et al, 2001; Basbaum et al, 2009; Dawes et al, 2011; Ji et al, 2018). Inflammatory mediators, such as nitric oxide and proinflammatory cytokines (eg., TNF-α, interleukin 1β), are able to activate or sensitize nociceptors and elicit chronic pain (Oh et al, 2001; Basbaum et al, 2009; Gold and Gebhart, 2010). The opiate drugs and nonsterioidal anti-inflammatory drugs (NSAIDs) are common and effective against
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