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Abstract：
Objective: The aim of this study was to systematically explore the pyrrolizidine alkaloids (PAs) type, content and risk assessment in the three Boraginaceae used in TCM, involving Arnebia euchroma (AE), A. guttata (AG), and Lithospermum erythrorhizon (LE). Method: A UHPLC-MS/MS method was established to simultaneously determine eight pyrrolizidine alkaloids (PAs), namely intermedine, lycopsamine, intermedine N-oxide, lycopsamine N-oxide, 7-acetyllycopsamine, 7-acetyllycopsamine N-oxide, echimidine N-oxide, and echimidine in the three herbs. Based on these results, the risk assessment was explored using the routine margin of exposure (MOE) combined with relative potency (REP) for oral and external usage, respectively. Results and Conclusion: Imermedine and imermedine N-oxide were common components in the eight tested PAs. 7-acetyllycopsamine and its N-oxide were not detected in AE; echimidine and its N-oxide were not detected in AG; lycopsamine and its N-oxide, 7-acetyllycopsamine and its N-oxide were not detected in LE. The total contents of 8 PAs in 11 batches of AG was341.56-519.51 μg/g; the content in 15 batches of LE was 71.16-515.73 μg/g, and the content in 11 batches of AE was 23.35-207.13 μg/g. Based on these results, the risk assessment was explored using MOE combined with REP for oral and external usage, respectively. The findings of the risk assessment method of PAs based on MOE combined with the REP factor were consistent with the clinical toxicity results. As an oral herb, AE had low risk or no risk due to its low PA contents, and individual batches of LE were medium risk, while attention should be paid to their clinical use.AG was also low risk. The external use of the three Boraginaceae used in TCM was not associated with any risk. This study systematically explored the PA type and content of the three Boraginaceae used in TCM. Additionally, the refined risk assessment of PAs based on REP provided a more scientific basis for quality evaluation and rational use of the medicinal Boraginaceae used in TCM to improve public health.
摘要：
目的:本研究的目的是系统探索吡咯烷类化合物生物碱(PAs)的类型,三种中药紫草的含量和风险评估，涉及Arnebiaeuchroma（AE），A.古塔塔(AG)，和紫草红斑（LE）。方法:建立UHPLC-MS/MS法同时测定8种吡咯嗪类生物碱,即midine，lycopamine,中间N-氧化物，lycopamineN-氧化物，7-乙酰吡喃胺，7-乙酰基椰子胺N-氧化物，异希咪定N-氧化物，和echimidine在三种草药中。基于这些结果,风险评估是使用常规暴露界限（MOE）结合口服和外部使用的相对效力（REP）进行探索的，分别。结果与结论：艾美碱和艾美碱N-氧化物是8种测试PA中的常见成分。在AE中未检测到7-乙酰氨基吡啶及其N-氧化物；在AG中未检测到echimidine及其N-氧化物；lycopamine及其N-氧化物，在LE中未检测到7-乙酰基吡喃胺及其N-氧化物。11批AG中8种PAs的总含量为341.56-519.51μg/g；15批LE的含量为71.16-515.73μg/g，11批AE的含量为23.35-207.13μg/g。基于这些结果,使用MOE结合REP进行口腔和外部使用的风险评估进行了探索，分别。基于MOE结合REP因子的PAs风险评估方法的结果与临床毒性结果一致。作为一种口腔草药，AE具有低风险或没有风险，由于其低PA含量，个别批次的LE是中等风险，同时应注意其临床使用。AG也是低风险的。中药中使用的三种紫草科的外用与任何风险无关。本研究系统地探讨了中药中使用的三种紫草科的PA类型和含量。此外,基于REP的PAs的精细化风险评估为中药紫草属植物的质量评价和合理使用提供了更科学的依据，以改善公众健康。
