目的 研究古籍记载的闹羊花不同炮制品的毒性和药效的相关性，确定“减毒-存效”的最佳炮制方法。方法 采用分光测色仪、高效液相色谱电雾式检测器法（HPLC-CAD）、小鼠急性毒性实验、二甲苯致小鼠耳肿胀实验分别对闹羊花生品及不同炮制品的性状（颜色）、指标性成分含量、毒性、药效进行评价。结果 相较于生品，闹羊花经炮制后饮片颜色由灰黄色变为棕褐色，指标性成分闹羊花毒素Ⅱ、Ⅲ、V含量大幅度降低，3种毒性成分总量的顺序为生品（0.340%） > 清蒸（0.181%） > 酒蒸（0.178%） > 醋蒸（0.154%）。小鼠急性毒性实验表明，闹羊花不同炮制品半数致死量（median lethal dose，LD₅₀）的大小顺序为醋蒸（3.538 g/kg） > 酒蒸（3.467 g/kg） > 清蒸（2.725 g/kg） > 生品（2.172 g/kg），表明炮制达到了“减毒”的目的。抗炎药效实验表明，闹羊花炮制前后均能抑制二甲苯致小鼠耳肿胀，抑制率大小顺序为生品高剂量组（73.25%） > 生品中剂量组（58.39%） > 酒蒸高剂量组（49.63%） > 醋蒸高剂量组（42.48%） > 清蒸高剂量组（40.56%），相较于对照组均有显著性差异（P<0.05、0.01），达到了“存效”的目的。结论 闹羊花的多种炮制方法均有“减毒存效”作用，“减毒”以醋制为优，“存效”以酒制为优，为临床用药提供了依据，同时建立了毒性中药“外观性状-化学成分-毒性-药效”多元评价模式，为闹羊花炮制工艺、质量标准、减毒存效机制等研究奠定了理论基础。

Objective To study the correlation between toxicity and efficacy of different processed Rhododendri Mollis Flos according to the ancient processing, in order to define the optimal processing method for "attenuation-preservation effects". Methods The character (color), index content, toxicity, and efficacy of Rhododendri Mollis Flos and its processed products were evaluated by spectrophotometer, HPLC-CAD, acute toxicity test in mice, and ear edema method in mice. Results It showed that the color of processed slices changed from gray yellow to black brown. The contents of the rhodojaponin Ⅱ, Ⅲ, and V were significantly reduced, and the sum of the three toxic components was raw (0.340%) > steamed (0.181%) > wine steamed (0.178%) > vinegar steamed (0.154%). The acute toxicity test in mice showed that the order of LD₅₀ was vinegar steamed (3.538 g/kg) > wine steamed (3.467 g/kg) > steamed (2.725 g/kg) > raw (2.172 g/kg). The anti-inflammatory effect test showed that Rhododendri Mollis Flos could inhibit the ear swelling in mice induced by xylene before and after processing, inhibition rate was raw high dose group (73.25%) > raw medium dose group (58.39%) > wine steamed high dose group (49.63%) > vinegar steamed high dose group (42.48%) > steamed high dose group (40.56%), achieved the effect of "preservation". Conclusion Various processing methods of Rhododendri Mollis Flos have the effect of "attenuation-preservation effects". Vinegar steamed is the best for "attenuation", and wine steamed is the best for "preservation", which provides a basis for clinical drug use. Meanwhile, the combined multi-angle evaluation model of "character-constituent-toxicity-efficacy" was established, which laid a theoretical foundation for the study of processing technology, quality standard and detoxification mechanism.

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成都中医药大学双一流中药质量保障提升创新科研团队（030041011）；重庆市自然科学基金面上项目（cstc2019jcyj-msxmX0552）