Abstract
The analgesic studies on Stauntonia brachyanthera, a traditional Chinese folk medicine used to treat headache, pains and inflammatory diseases in local areas, showed that the EtOH extracts (EESB) and the characteristic ingredient YM11 could significantly inhibit the acetic acid-induced writhing responses by 43.1% and 78.95%, and decrease the xylene-induced ear edemas by 48.9% and 21.4%, respectively. EESB could significantly increase pain threshold of mice in hot-plate test, but the effect of YM11 was not obviously. Further study in formalin test showed the inhibitory effect of YM11 in 2nd phase was more significant than that in 1st phase, revealed the peripheral analgesic activity of YM11. The ELISA and Western Blot analysis suggested that the analgesic mechanisms of YM11 were related to the inhibitions of the expressions of TNF-α, IL-1β and IL-6, and down-regulations of Nav1.8 protein in the left side of L4–6 DRG regulated by MAPKs, in which the levels of p-ERK, p-JNK and p-p38 were all decreased. In addition, the electrophysiological experiments indicated YM11 could reduce the Nav1.8 currents by 46.01% in small-diameter DRG neurons. Therefore, the analgesic activity of S. brachyanthera might be based on the regulation of inflammatory mediators and the directly control of the sodium channel prompt.
Highlights
EtOH extracts of S. brachyanthera (EESB) could significantly increase pain threshold of mice in hot-plate test, but the effect ofYM11 was not obviously
The results showed that basal levels of p-p38, p-extracellular signal-regulated kinases (ERK) and p-Jun N-terminal kinase (JNK) were detected in vehicle, aspirin and YM11 groups, respectively
Among mitogen-activated protein kinase (MAPK) pathways, the expressions of p-ERK were markedly decreased in all dose groups, the level of p-JNK was significant decreased only at high dose, and that of p-p38 were significantly decreased at both middle and high doses (Fig. 12). These results suggested that YM11 could decrease the level of MAPKs channel protein in a dose-dependent manner
Summary
EESB could significantly increase pain threshold of mice in hot-plate test, but the effect ofYM11 was not obviously. The management of pathological pain is a major clinical challenge Opioids, such as morphine, one of the most commonly prescribed analgesics[2], is always accompany with many negative side effects, including drug addiction, withdrawal symptom, and respiratory depression, etc. As is known to all, the traditional Chinese medicines (TCM) have been uses for a long history and have significant therapeutic effects for many diseases due to their multi-constituents, multi-factored and multi-targeted properties, which have obvious advantages for the treatment of diseases with few side effects[4] The components from those natural resources have strong biological activities and many of them have been developed into drugs for clinical uses, such as artemisinin, paclitaxel, vinblastinecamptothecine, ginkgolide B, and so on. From these folk medicinal applications, it could be concluded that S. brachyanthera has great potential biological activities for the treatments of pain or inflammation
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