苍术具燥湿健脾，祛风散寒，明目等功效。焦苍术为临床常用饮片之一，炒焦后可增强其健脾止泻作用，并可缓和辛燥之性，其作用在临床上已被验证，但其炮制机理未见报道。课题组前期对麸炒苍术增效减燥机理进行了研究，明确了麸炒法对其化学成分、药效和毒性的影响。本课题拟在前期研究的基础上，以腹泻指数、胃排空和肠推进、胃动素、胃泌素、肠道菌群及水通道蛋白等为药效指标，对比研究苍术炒焦前后药效变化。在药效指标指导下，确定药效变化的关键化学部位，并对生品和焦品提取物的整体化学成分进行对比分析，为系统阐释苍术炒焦的炮制原理奠定基础。

Rhizoma Atractylodis have efficacy of invigorating the spleen to dry, relieving rheumatism and cold, improving eyesight and so on. It is known that deep-fried Rhizoma Atractylodis is widely used in clinic today, and it is thought to have the following functions: enhancing the function of strengthening the spleen and relieving diarrhea, alleviating dryness and such effects have been verified in clinic. However, its processing mechanism has not been reported. Our previous study is about the mechanism of increasing efficiency and alleviating dryness of the bran-fried Rhizoma Atractylod, and we have studied the effect of processing method on chemical constituents, pharmacodynamics and its toxicity. Based on our previous studies, the changes of pharmacodynamics between non-processed and deep-fried Rhizoma Atractylodis will be clarified with following indexes: the index of diarrhea, the rates of intestinal propulsion and gastric emptying, the serum level of motilin and gastrin, intestinal flora and the electrolyte level of aquaporin. Moreover, under the guidance of these phamacodynamic indexes, the effective fractions would be found and we can do further study on the comparison of key chemical constituents between non-processed and deep-fried Rhizoma Atractylodis. Above of all, this work will establish a firm foundation for explaining processing mechanism of deep-fried Rhizoma Atractylodis.

本课题主要从苍术炒焦前后各化学部位的成分变化以及药效、毒性变化进行了研究，初步探讨了苍术炒焦长于“健脾止泻”的物质基础，为后期阐释其作用机理奠定基础。研究了苍术炒焦前后化学成分的量变和质变规律。分析比较了生、焦苍术挥发油含量及化学成分变化规律，采用水蒸汽蒸馏法提取挥发油，研究表明，炒焦后挥发油含量降低30%以上；采用 GC技术分析显示，炒焦前后挥发油成分的种类无明显变化，但量变明显，其中6种成分的含量显著降低（29%以上）。对水提物萃取制得的氯仿部位、正丁醇部位和剩余水部位进行成分比较研究。运用HPLC技术，分析发现，焦品氯仿部位较生品有16成分的含量升高或降低25%以上，其中5-羟甲基糠醛显著增加，在8.386min有1新的色谱峰产生；正丁醇部位有5种成分含量增加1倍以上，另外焦品正丁醇部位在5.365min和8.652min新产生了2个色谱峰；炒焦前后剩余水部位没有明显的质变，但有3种成分的量变30%以上。对苍术炒焦前后药效及毒性进行了比较研究。以胃残留、肠推进、胃泌素、胃动素作为健脾指标，以结肠粘膜APQ3、TNF-α、IL-10、肠道菌群结构为为止泻指标，以肾脏AQP2、血清醛固酮及电解质水平为指标，研究苍术炒焦前后的各部位药效。同时，对生苍术和焦苍术挥发油进行毒性研究。水提物部位药效学研究， 分别以脾虚泄泻、湿阻中焦大鼠为模型，结果显示，水提物、氯仿部位、正丁醇部位均能增强模型大鼠的健脾作用；而止泻指标显示，焦品正丁醇部位是其主要止泻的有效部位；燥湿指标结果显示，苍术生品燥湿作用强于焦品，且以生品正丁醇部位药效焦明显；而剩余水部位药效作用不明显。挥发油急性毒性研究对其挥发油进行急性毒性实验。结果显示，炮制后LD50显著提高（13.13%），表明炒焦后挥发油毒性降低。综上，苍术炒焦后健脾和止泻作用药效增强，且以正丁醇部位增强最为明显，氯仿部位其次，剩余水部位不明显。炒焦前后各部位化学成分有明显的量变和质变，特别是氯仿和正丁醇部位，均有新增成分，这可能是炒焦后药效变化的物质基础，该部位将是今后重点研究对象。