DISCOVERY OF POTENT NON-OPIOID ANALGESICS
Abstract
Based on our research system for natural product screening and new drug discovery, authentic medicinal Uyghur herbs endemic to Xinjiang were selected. Modern separation and purification techniques guided by bioactivity tracking were adopted to systematically isolate constituents from extracts of medicinal parts. Chemical structures of isolated compounds were elucidated by spectroscopic technologies including mass spectrometry and nuclear magnetic resonance (NMR). In vivo analgesic activity was evaluated via classic analgesic models in mice, such as the hot-plate test and acetic acid writhing test, so as to screen lead compounds with high activity and low toxicity. More than one hundred natural compounds were isolated and identified from multiple characteristic Uyghur medicinal plants from Xinjiang. Among them, six compounds with novel skeletons exhibited remarkable analgesic potency comparable to morphine, a widely used potent clinical analgesic. Pharmacological verification confirmed that these compounds do not activate opioid receptors, indicating they act as multi-target potent analgesic agents.
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