Inhibition of acid-sensing ion channels by chlorogenic acid in rat dorsal root ganglion neurons

Pharmacology of acid-sensing ion channels – Physiological and therapeutical perspectives

“…In addition to its antioxidant, anti-inflammatory and neuroprotective properties, chlorogenic acid has potent analgesic properties explaining the effects of traditional medicinal plants in several countries. Chlorogenic acid was shown to inhibit native ASIC currents in rat sensory neurons (IC 50 ∼ 0.2 µM) and to subsequently reduce acid-induced neuronal excitability (Qu et al, 2014).…”

“…In mice, sevanol significantly reverses inflammatory hyperalgesia and acid-triggered visceral pain (Dubinnyi et al, 2012), thus explaining the known analgesic effects of thyme extracts. Chlorogenic acid, and Thalassiolin B alleviates inflammatory, neuropathic and visceral pain, as well as intraplantar acid-evoked pain in rats (Garateix et al, 2011;Qu et al, 2014). Finally, subcutaneous injection of gastrodin relieves chemical and acid-evoked pain in rats, without involving peripheral opioid receptors (Qiu et al, 2014).…”

Subtype‐selective inhibition of acid‐sensing ion channel 3 by a natural flavonoid

“…For the compound 9 targeting ASICs in sensory neurons, it is reasonable to speculate that this compound is likely capable of inhibiting ASIC3 channels due to the dominant expression of this channel subunit in sensory neurons . However, the subunit selectivity of compound 9 on different ASICs has not been examined yet . In the present study, we identified that compound 11 but not its structurally analogs (i.e compounds 17–21 ) subtype‐specifically antagonized ASIC3 channels, which indeed contains substantially new information on the mechanisms underlying the phenolic compound modulation on ASICs.…”

“…52 Chlorogenic acid (9) is a natural phenolic compound with 1 carboxylic group in the structure. And it inhibits ASIC-like currents in sensory neurons 53 with an IC 50 around 0.2 μmol/L. Interestingly, puerarin (10), a natural flavonoid with neither basic groups nor carboxylic groups in the structure, but only several phenol groups, also inhibits ASIC-like currents in hippocampal neurons 54 with the F I G U R E 1 Reported small molecule antagonists targeting the ASIC channel with an emphasis on its capability on ASIC3 subtypes IC 50 at 38.4 μmol/L.…”

Effects of chlorogenic acid on voltage-gated potassium channels of trigeminal ganglion neurons in an inflammatory environment

“…(Mikami and Yamazawa, 2015) reported that CGA could prevent neurons from glutamate neurotoxicity by regulating Ca 2+ entry into neurons. The latest study indicated that CGA may exert an inhibitory effect on the functional activity of native acidsensing ion channels in rat dorsal root ganglion neurons to alleviate nociceptive response (Qu et al, 2014). According above discoveries, CGA may be useful for novel treatments of inflammatory pain or neuropathic pain through modulating ion channels in neurons.…”