Ethnopharmacological relevance: Belamcanda chinensis (L.) DC. (BC) and Iris tectorum Maxim. (ITM) have been widely used in recent years due to their remarkable curative effects on sore throat, cough and asthma. but they are often misused due to their similar appearance. A comprehensive comparison of the chemical composition, biological activity, pharmacokinetics and tissue distribution between the two active differential components has not been performed. Differences in their specific effects have not been fully elucidated. Aim of the study: This work aims at differentiating between BC and ITM in terms of appearance, chemical composition, biological activity, pharmacokinetics and tissue distribution. Materials and methods: In this study, the HPLC-FP method was used to find the differences between the chemical components of BC and ITM. The pharmacological experiments were used to compare the differences in activity, including in vitro anti-inflammatory activity with LPS-induced inflammation model of RAW 264.7 cells, inhibition of AChE activity, and the regulation of isolated small intestinal smooth muscle in mice. The pharmacokinetic and tissue distribution profiles were used to analyze the differences between the two in rats. Results: The types of isoflavones in BC and ITM are basically the same, but their contents in ITM is much higher than that in BC. At the same doses, the release of TNF-& alpha;, NO, IL-1 & beta; and IL-6 from RAW 264.7 cells in the ITM group was lower than that of the BC group, and the in vitro anti-inflammatory activity of ITM was stronger than that of BC. Meanwhile, ITM had stronger inhibition ability to inhibit AChE activity than BC. The BC extract exhibited an inhibitory effect on the isolated small intestinal smooth muscle of mice, and the ITM extract showed stimulatory effect at low concentration and inhibitory effect at high concentration. There were significant differences in drug-time profiles, kinetic parameters and tissue distribution. Conclusions: There are significant differences in the multidimensional aspects of appearance, chemical composition, biological activity, pharmacokinetics, and tissue distribution between BC and ITM. This study provides a theoretical basis for the quality control, pharmacological efficacy and clinical application of the two herbs.

目的:研究藏药尖突黄堇的解热、镇痛、抗炎作用.方法:昆明小鼠分为模型组,阳性药阿司匹林组,尖突黄堇醇提物低、中、高剂量组(生药 0.5、1.0、1.5 g/kg).通过皮下注射干酵母诱导小鼠发热模型探究其解热作用;通过冰醋酸致小鼠扭体法探究其镇痛作用;通过二甲苯诱导小鼠耳廓肿胀方法探究其抗炎作用.结果:尖突黄堇总醇提物可显著抑制干酵母所致发热小鼠的肛温上升;显著抑制冰醋酸所致小鼠疼痛,减少扭体次数;显著降低二甲苯致小鼠耳廓肿胀,减少肿胀度.结论:尖突黄堇具有明显的解热、镇痛、抗炎作用,但其具体的药效作用还有待进一步研究.

射干和川射干为中医临床常用的清热解毒药,《中国药典》中记载两味药的功效主治相同,但其植物基原、药材与饮片质量控制指标成分却完全不同.该文通过对射干和川射干的研究现状进行综述,探讨射干和川射干的清热解毒(抗炎)药效物质基础及其作用机制的研究思路,并揭示为何两味中药的功效主治基本相同却一直被单列记载的科学内涵,为建立射干和川射干的客观评价的质量标准和中医临床用药提供科学依据.

采用HPLC法测定橙皮苷、橙皮素单葡萄糖苷和橙皮素在水和不同pH缓冲溶液中的平衡溶解度;结合摇瓶法测定其在正辛醇-水体系和正辛醇-不同pH缓冲溶液体系中的油水分配系数.37℃时,橙皮苷、橙皮素单葡萄糖苷和橙皮素在水中的平衡溶解度分别为 18.94、632.34、15.37 μg·mL-1;pH值升高,橙皮苷平衡溶解度逐渐降低,对橙皮素单葡萄糖苷和橙皮素无影响,但在pH 7.4时,二者均有最大值,分别为836.57、71.82 μg·mL-1.橙皮苷、橙皮素单葡萄糖苷和橙皮素在正辛醇-水体系中lg P值分别为 0.094、0.573、2.876,在不同缓冲溶液中(pH3.4～7.4)的lg P值范围分别为 0.069～0.281、0.603～0.664、2.459～2.905.橙皮素单葡萄糖苷的平衡溶解度远大于橙皮苷和橙皮素,其lg P值在 0.6左右,具有一定的亲水亲脂性,预测其在胃肠道中有较好的吸收;橙皮苷的lg P值小于 0.3,推测其不易被胃肠吸收;橙皮素的lg P值大于 2,其脂溶性极强,易通过主动转运进入生物膜.上述结果可为 3个单体成分的成药性,以及中药陈皮中的橙皮苷酶转化为橙皮素单葡萄糖苷的研究,提供实验基础和科学依据.

目的 从中药射干中分离制备野鸢尾苷单体,并初步研其体外抗炎活性及作用机制.方法 采用多溶剂萃取法制备野鸢尾苷;在野鸢尾苷溶液对小鼠单核巨噬细胞RAW 264.7无细胞毒性的浓度范围内,采用脂多糖诱导并建立体外细胞炎症模型,给予不同浓度野鸢尾苷溶液干预,采用Griess法检测细胞上清液中一氧化氮(NO)的含量、ELISA法检测肿瘤坏死因子α(TNF-α)、白细胞介素1β(IL-1β)、白细胞介素6(IL-6)的含量;并结合野鸢尾苷对乙酰胆碱酯酶活性的影响,初步揭示野鸢尾苷的抗炎活性及作用机制.结果 多溶剂萃取法所得的野鸢尾苷单体,经HPLC峰面积归一化法计算其纯度大于98％;给药12.5-100 μg·mL-1野鸢尾苷对RAW 264.7无细胞毒性;与模型组比较,在给药12.5～100 μg·mL-1野鸢尾苷时,对抑制巨噬细胞中TNF-α、NO、IL-1β、IL-6的释放具有极显著性差异,且呈剂量关系;野鸢尾苷对乙酰胆碱酯酶的活性具有抑制作用,其数半抑制浓度(IC50)为4.09 mg·mL-1,且呈剂量关系.结论 多溶剂萃取法是一种简单、高效分离制备射干中野鸢尾苷的方法;野鸢尾苷的抗炎机制可能是通过胆碱能抗炎通路,调节巨噬细胞释放TNF-α、IL-1β、IL-6炎性介质,并结合调节NO抗炎途径,从而实现多途径的抗炎作用.

目的:考察小承气汤水煎液不同干燥方法制备得到的物质基准化学成分的差异,从物质基准化学成分的角度,为小承气汤颗粒剂工厂化制备确定最佳干燥方法提供依据.方法:采用HPLC指纹图谱方法,分别对水煎液及其在冷冻干燥、喷雾干燥、减压干燥和脉动真空干燥方法制得的小承气汤物质基准进行HPLC指纹图谱相似度等分析.结果:通过对4种干燥方法制得的样品与水煎液相似度的比较,发现干燥后的物质基准与水煎液相似度均达到0.9以上,相似度较好.水煎液及其物质基准的HPLC指纹图谱能够反映小承气汤水煎液浓缩干燥的整体化学成分轮廓,且脉动真空干燥更适合工厂化生产.结论:脉动真空干燥可作为小承气汤颗粒剂工厂化制备的干燥方法.

目的:建立橙皮苷酶转化最佳工艺并应用于陈皮酶转化;比较橙皮苷和陈皮酶转化前后产物对正常小鼠小肠推进作用,为陈皮酶转化研究提供依据.方法:以橙皮苷酶转化产物橙皮素单葡萄糖苷含量为指标,采用单因素方法考察酶用量、pH、反应时间和温度,建立其最佳工艺,并用于陈皮的酶转化实验;采用正常小鼠促小肠动力实验比较陈皮酶转化前后橙皮苷及其酶解产物橙皮素单葡萄糖苷的药效.结果:橙皮苷酶转化最佳工艺为:酶使用量0.1 g,pH=4,反应时间60 min,温度65℃;在小肠推进实验中,与空白组对比,陈皮酶转化后与橙皮素单葡萄糖苷各剂量组及橙皮苷高、中剂量组有显著性差异(P<0.05),其中陈皮酶转化后高、中剂量组及橙皮苷高剂量组与橙皮素单葡萄糖苷各剂量组均有极显著差异(P<0.01);组间对比,陈皮酶转化前后中剂量组存在显著差异(P<0.05),陈皮酶转化前后高剂量组存在极显著差异(P<0.01);橙皮素单葡萄糖苷高剂量组与橙皮苷高剂量组对比有显著性差异(P<0.05).结论:同摩尔数的橙皮素单葡萄糖苷对正常小鼠小肠推进作用优于橙皮苷;陈皮酶转化后小肠推进作用优于陈皮.该酶解方法操作简便、反应可控,预测性良好,可进一步用于橙皮苷和陈皮的酶转化研究.

目的 采用傅里叶变换红外光谱(FT-IR)和高效液相色谱(HPLC)方法对37批不同品种和产地的大黄药材进行分析.方法 分别采用FT-IR和HPLC测量37批大黄药材的红外光谱和液相指纹图谱,并对结果进行聚类分析.从每一产地中选择一批药材,分析红外原始光谱,并对原始光谱进行二阶导数处理,根据所得二阶导数光谱对各产地大黄进行分析;同时对HPLC指纹图谱进行相似度分析.结果 FT-IR和HPLC两种方法聚类分析结果基本一致.通过分析不同产地的大黄药材原始红外光谱特征峰能够区分各产地大黄品种,但无法区分其产地,而二阶导数特征峰有明显的位置、形态和强度上的差异,能够将不同产地大黄药材鉴别出来.HPLC指纹图谱相似度分析无法将其产地进行区分.结论 与HPLC指纹图谱相比,FT-IR能够更加全面的反映大黄药材的化学成分,并对其品种和产地进行区分.