Artemisia annua L.: evidence of sesquiterpene lactones’ fraction antinociceptive activity

Abstract

BackgroundArtemisia annua L. has been used for many centuries in Chinese traditional medicine. Artemisinin, the active principle was first isolated and identified in the 1970s becoming the global back bone to the fight against malaria. Our research group previously developed an economic and ecological friendly process to obtain this compound. In the pursuit to also exploit the residue generated throughout the process we further evaluated the pharmacological potential of that extract.MethodsThe alcoholic crude extract after artemisinin precipitation maintained an enriched sesquiterpene lactones content with residue artemisinin (1.72%) and deoxyartemisinin (0.31%), used as chemical markers for this sample. This study evaluated the pharmacological potential of the enriched sesquiterpene lactone fraction (Lac-FR) on different nociceptive and inflammatory experimental animal models. Previous findings on the biological properties of lactones obtained from natural products permitted us to explore the antinociceptive activities of these compounds based on in vivo chemical-induced behavioral assays.ResultsThe enriched sesquiterpene lactone fraction (Lac-FR) was administrated by intraperitoneal injection producing a relevant reduction in the reaction time of the animals in both phases of the formalin test, significantly reduced the sensitivity to mechanical allodynia stimulus, reduced the paw edema caused by carrageenan injection and promoted high antinociceptive activity in tail flick model suggesting relationship with the opioid system. Further studies are being undertaken to elucidate the active components involved with the antinociceptive activity as well as evaluation of synergy effect that is seen by combination of substances that is greater than would be expected from consideration of individual contributions.ConclusionFor the first time, results presented herein provided consistent data to support the potential use of these lactones for pain relief as revealed by chemical-induced nociception assays in mice.

Antinociceptive Potential of Zinnia grandiflora

“…In this test, two different periods of high licking activity could be identified, an early phase lasting 10 min and a late phase occurring from 10 to 30 min after the injection of formalin . The early phase seems to be caused predominantly by C-fiber activation due to the peripheral stimulus (neurogenic activity), while the late phase appears to be dependent on the combination of an inflammatory reaction in the peripheral tissue and functional changes in the dorsal horn of the spinal cord; this pain can be inhibited by anti-inflammatory drugs. − Diclofenac (DIC, 31.6 mg/kg) was chosen as the positive control as previously reported . Thus, oral administration (31.6 to 562.3 mg/kg) of the infusion provoked a dose-dependent antinociceptive activity (Figure ; Figure S1, Supporting Information); the highest effect, in both phases, was observed at the doses of 100, 316.2, and 562.3 mg/kg, which reduced significantly the licking time by 39.5%, 52.5%, and 57.3%, respectively (ED 50 = 224.6 ± 38.1 mg/kg, p.o.).…”

The antinociceptive effect of artemisinin on the inflammatory pain and role of GABAergic and opioidergic systems

“…The acetic acid writhing test is an animal model of inflammatory pain that has been created for the assessment of the anti-inflammatory/analgesic potency of different compounds [13,16,22]. Intraperitoneal administration of acetic acid induces chemical peritonitis, releases pro-inflammatory mediators, activates peripheral nociceptors on the sensory nerve fibers, and induces abdominal constriction via the synthesis of prostaglandins, especially PGE 2 , which leads to pain and hyperalgesia.…”

“…Naloxone is a nonselective opioid antagonist for μ, κ and δ receptors which was used to study the probable role of the opioidergic system on the analgesic effects of artemisinin [13,16]. Because naloxone administration could not inhibit the antinociceptive effects of artemisinin, it seems that opioid receptors are not involved in the analgesic effect of artemisinin [1,13,25].…”

Desafios e estratégias para segurança alimentar mundial

“…Estudos realizados indicam os benefícios da astaxantina na vida de prateleira, assim como, Carr A planta vem mostrando uma opção relevante para a terapêutica em diversas doenças e possui uma gama de propriedades, incluindo atividade antibacteriana, antimalárica, antifúngica, antileishmanial, antioxidante, antitumoral e anti-inflamatória (KONKIMALLA et al, 2008;FERREIRA et al, 2010;EFFERTH, 2017). Além de nas últimas décadas o composto também ter sido amplamente utilizado no tratamento de antiúlcera (FOGLIO et al, 2002), antinociceptiva, com envolvimento do sistema opióide (DE FAVERI FAVERO et al, 2014) e anti-HIV (LUBBE et al, 2012). Esse composto pode ser útil como uma alternativa para o tratamento de muitas doenças inflamatórias (FERREIRA et al, 2011;SPRENGER et al, 2015), incluindo atividade imunossupressora tanto "in vitro" quanto "in vivo", além dos efeitos de aumento das espécies reativas de oxigênio (ROS)…”