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Pretreatment with naloxone did not alter the effect of incarvillateine.
Incarvillea sinensis is a Bignoniaceae plant used to treat rheumatism and relieve pain in traditional Chinese medicine. As a major component of I. sinensis, incarvillateine has shown analgesic activity in mice formalin tests. Using a series of animal models, this study further evaluated the effects of incarvillateine against acute, inflammatory, and neuropathic pain. Incarvillateine (10 or 20 mg/kg, i.p.) dose-dependently attenuated acetic acid-induced writhing, but did not affect thermal threshold in the hot plate test. In a Complete Freund’s Adjuvant model, incarvillateine inhibited both thermal hyperalgesia and paw edema, and increased interleukin-1β levels. Additionally, incarvillateine attenuated mechanical allodynia induced by spared nerve injury or paclitaxel, whereas normal mechanical sensation was not affected. Incarvillateine did not affect locomotor activity and time on the rotarod at analgesic doses, and no tolerance was observed after 7 consecutive daily doses. Moreover, incarvillateine-induced antinociception was attenuated by theophylline, 1,3-dipropyl-8-cyclopentylxanthine, and 3,7-dimethyl-1-propargylxanthine, but not naloxone, indicating that the effects of incarvillateine on chronic pain were related to the adenosine system, but not opioid system. These results indicate that incarvillateine is a novel analgesic compound that is effective against inflammatory and neuropathic pain, and that its effects are associated with activation of the adenosine system.
Pain is the most common reason people seek medical care, and treatment of pain remains challenging in the clinic. In particular, chronic inflammatory and neuropathic pain can persist and significantly affect the health and quality of life of patients. Various drug classes, including antidepressants, anti-epileptics, opioids, and topical anesthetics, are used to treat pain in the clinic1. However, their clinical applications are limited by either poor therapeutic action and/or marked side effects2. Therefore, there is a constant demand for novel compounds that will effectively inhibit pathological pain with limited influence on normal nociception and other physiological functions.
Among various therapeutic targets, the adenosine receptor system is promising for the treatment of pain3. Adenosine receptors, namely A1, A2A, A2B, and A3 receptors, are widely distributed in the spinal cord and brain areas involved in pain transmission, as well as peripheral sensory afferents or adjacent cells4,5,6. Administration of adenosine or adenosine receptor agonists inhibits pain-related behaviors in animal and human models7,8,9,10. Compared to classical analgesics, such as opioids, adenosine receptor agonists are particularly effective in chronic pain that arises from inflammation and neuropathy11,12. However, direct-acting agonists may exert CNS side-effects, including general sedation and locomotor suppression, which raises serious concerns when considering the development of agents affecting the adenosine system13,14.
Incarvillea sinensis is a Bignoniaceae plant that has been widely used as a herbal medicine for more than 1400 years in China. In traditional Chinese medicine, I. sinensis is used to treat rheumatism, bruises, and wounds, and is effective in attenuating pain and inflammation15. Since the 1990 s, photochemists and pharmacologists have investigated the active components in I. sinensis, isolating more than 13 monoterpene alkaloids and 7 macrocyclic spermine alkaloids16,17,18,19,20,21,22,23,24. Incarvillateine (Fig. 1) is considered the major active component, with a characteristic dimeric structure and five contiguous stereocenters on the bicyclic piperidine moiety16. Previous reports showed that incarvillateine attenuates formalin-induced pain in mice with a higher potency than morphine25. Moreover, the antinociceptive effect of incarvillateine in this model can be attenuated by non-selective adenosine receptor antagonist, non-selective opioid receptor antagonist, and μ and κ opioid receptor antagonists25,26. Nevertheless, no other study has addressed the pharmacological effects of incarvillateine. The difficult isolation procedure and small quantity yield also pose hurdles for further research and development of incarvillateine.
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