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酒制对升降的影响:大鼠口服生黄芩和酒制黄芩后黄酮类化合物在组织中的分布

The effects of wine-processing on ascending and descending: The distribution of flavonoids in rat tissues after oral administration of crude and wine-processed Radix scutellariae.

作者信息

Huang Ping, Tan Shanzhong, Zhang Yong-xin, Li Jun-song, Chai Chuan, Li Jin-ji, Cai Bao-chang

机构信息

College of Pharmacy, Nanjing University of Chinese Medicine , Nanjing 210023 , PR China; Jiangsu Provincial TCM Engineering Technology Research Center of High Efficient Drug Delivery System (DDS), Nanjing 210023, PR China; Jiangsu Key Laboratory of Chinese Medicine Processing, Nanjing 210023, PR China.

The Second Hospital of Nanjing, 1-1 Zhongfu Road, Nanjing 210003, PR China.

出版信息

J Ethnopharmacol. 2014 Aug 8;155(1):649-64. doi: 10.1016/j.jep.2014.05.063. Epub 2014 Jun 12.

Abstract

ETHNOPHARMACOLOGICAL RELEVANCE

Ascending and descending theory is a core principle of traditional Chinese medicine (TCM) theories. It plays an essential role in TCM clinical applications. Some TCM medicine has specific properties, which could alter the inclination and direction of their actions. The properties of the ascending and floating process of one herbal medicine are affected by means of herb processing. Wine-processing, which is sautéing with rice wine, is one of the most popular technologies of herb processing. Wine-processing increases the inclination and direction of its actions, thereby producing or strengthening their efficacy in cleaning the upper-energizer heat. Radix scutellariae, the dried roots of Scutellaria baicalensis Georgi, is a well-known TCM used for the treatment of inflammation, pyrexia, jaundice, etc. Recently, wine-processed Radix scutellariae was normally applied in clinical studies for the treatment of upper-energizer syndrome. In order to investigate the effects of wine-processing on ascending and descending of Radix scutellariae, the comparative study of distribution of flavonoids in rat tissues of triple energizers (SanJiao-upper, middle, lower jiao) after oral administration of crude and wine-processed Radix scutellariae aqueous extracts was carried out.

MATERIALS AND METHODS

The rats were randomly assigned to two groups and orally administered with crude and wine-processed Radix scutellariae aqueous extracts, respectively. At different pre-determined time points after administration, the concentrations of compounds in rat tissue homogenate were determined, and the main tissue pharmacokinetic parameters were investigated. Tissue pharmacokinetic parameters including AUC0-t, t1/2, Tmax and Cmax were calculated using DAS 2.0. An unpaired Student t-test was used to compare the differences in tissue pharmacokinetic parameters between the two groups. All the results were expressed as arithmetic mean±S.D.

RESULTS

The parameters of Cmax and AUC0-t of some flavonoids in wine-processed Radix scutellariae were remarkably increased (p<0.05, p<0.01, p<0.001) in the rat upper-energizer tissues (lung and heart) compared with those of the crude group. However, in the rat middle- and lower-energizer tissues (spleen, liver and kidney), the Cmax and AUC0-t of some flavonoids were significantly decreased (p<0.05, p<0.01) compared with the crude group. The main explanation for these differences seems to the effects of wine-processing on ascending and descending theory.

CONCLUSIONS

All of these differences in the distribution of triple energizers after oral administration of crude and wine-processed Radix scutellariae aqueous extracts may lead to the increase of efficacy on the upper-energizer tissues and were in compliance with the ascending and descending theory. Therefore, wine-processing was recommended when Radix scutellariae was used for cleaning the upper-energizer heat and humidity. The obtained knowledge can be used to evaluate the impact of these differences on the efficacy of both the drugs in clinical applications and might be helpful in explaining the effects of wine-processing on ascending and descending theory.

摘要

民族药理学相关性

升降理论是中医理论的核心原则。它在中医临床应用中起着至关重要的作用。一些中药具有特定的特性,这可能会改变其作用的倾向和方向。一味草药升浮过程的特性会受到炮制方法的影响。酒炙,即用米酒炒制,是最常用的草药炮制技术之一。酒炙可增加其作用的倾向和方向,从而产生或增强其清上焦热的功效。黄芩,即黄芩干燥的根,是一种著名的用于治疗炎症、发热、黄疸等病症的中药。最近,酒炙黄芩常用于治疗上焦证的临床研究。为了研究酒炙对黄芩升降特性的影响,进行了口服生黄芩和酒炙黄芩水提取物后大鼠三焦(上焦、中焦、下焦)组织中黄酮类化合物分布的比较研究。

材料与方法

将大鼠随机分为两组,分别口服生黄芩和酒炙黄芩水提取物。在给药后的不同预定时间点,测定大鼠组织匀浆中化合物的浓度,并研究主要的组织药代动力学参数。使用DAS 2.0计算包括AUC0-t、t1/2、Tmax和Cmax在内的组织药代动力学参数。采用非配对学生t检验比较两组之间组织药代动力学参数的差异。所有结果均以算术平均值±标准差表示。

结果

与生黄芩组相比,酒炙黄芩中一些黄酮类化合物在大鼠上焦组织(肺和心脏)中的Cmax和AUC0-t参数显著增加(p<0.05,p<0.01,p<0.001)。然而,在大鼠中焦和下焦组织(脾、肝和肾)中,一些黄酮类化合物的Cmax和AUC0-t与生黄芩组相比显著降低(p<0.05,p<0.01)。这些差异的主要原因似乎是酒炙对升降理论的影响。

结论

口服生黄芩和酒炙黄芩水提取物后三焦分布的所有这些差异可能导致上焦组织功效的增加,并且符合升降理论。因此,当黄芩用于清上焦湿热时,建议采用酒炙。所获得的知识可用于评估这些差异对临床应用中药物疗效的影响,并可能有助于解释酒炙对升降理论的作用。

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