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Evodiae Fructus on Targeted Distribution of Berberine in Rats

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Evodiae Fructus on Targeted Distribution of Berberine in Rats Int J Clin Exp Med 2018;11(8):7701-7709 www.ijcem.com /ISSN:1940-5901/IJCEM0073795 Original Article Effects of Evodiae Fructus on targeted distribution of berberine in rats Rui-Feng Liang, Wen-Jing Ge, Hui-Sen Wang, She-Feng Zhang, Xue-Xia Zhang, Geng-Sheng Li Institute of Chinese Materia Medica, Henan Provincial Academy of Traditional Chinese Medicine, Zhengzhou 450003, Henan Province, China Received September 20, 2017; Accepted May 24, 2018; Epub August 15, 2018; Published August 30, 2018 Abstract: According to Traditional Chinese Medicine (TCM) theories, Evodiae Fructus (EF) was considered as a meridian guiding drug (MGD) in Zuojin Pill and could enhance the effectiveness of prescription. However, the sci- entific evidence for this effect is still unclear. In this study, the meridian guiding mechanism of EF was investigated. Rats were randomly divided into four groups, control group (water), low dose of EF (250 mg/kg), medium dose of EF (500 mg/kg) and high dose of EF (1000 mg/kg). Water or EF was given to the rats by intragastric administra- tion for 7 days. After the last administration, berberine (80 mg/kg) was administered to rats by gavage. Then the blood and tissues of interest were collected at predetermined time points. Concentrations of berberine in different tissues were analysed by ultra-performance liquid-chromatography tandem mass spectrometry (UPLC-MS/MS) and the target parameters including relative targeting efficiency (RTE), relative uptake efficiency (RUE) and maximum relative concentration (RCmax) were calculated. Compared with control group, various doses of EF could improve the targeting efficiency of berberine in liver. The value of RUE was 1.10, 1.21, 1.37 and the RTE was 4.33%, 10.78% and 18.73% for the low, medium and high dose of EF, respectively. Moreover, it appreciably reduced the distribution of berberine in spleen and lung. EF increased the Cmax of berberine in nearly all tissues except for lung and spleen, with the value range from 2% to 36%. In a word, these results suggested that EF could increase the distribution of berberine in liver and reduce the concentration in spleen and lung, which indicated that the meridian guiding action of EF was credible. Keywords: Evodiae Fructus, berberine, distribution, rat, UPLC-MS/MS Introduction in the past. Based on dose-effect relationship, the main effect of the whole prescription was Meridian guiding theory, an important principle related to the concentration of drug in target of Traditional Chinese Medicine (TCM) theory, tissues. At present, study of targeting distribu- was recorded initially in “Shennong Bencao tion of active compound in vivo was considered Jing”, which was the source of Chinese herbal as the most popular experimental method to medicine. Based on meridian guiding theory, expound the mechanism of MGD [7, 8]. meridian guiding drug (MGD) similar to target- ed vector was commonly combined with other Zuojin Pill, a classical formula in traditional herbs to enhance the effectiveness of the pre- Chinese medicine, consists of Coptis chinensis scription in target organs [1]. Meridian guiding Franch. and EF at the weight ratio of 6 to 1, and theory, which acted as a bridge which linked it was found initially in “Danxi’s experiential theory and clinical medication, was one of the therapy” for treating liver-fire invading the stom- characteristics of TCM [2]. Therefore, it was ach. Coptis chinensis Franch. has been widely necessary to investigate the mechanism of used for the treatment of gastroenteritis, diar- meridian guiding theory. rhea, cancer [9], inflammation-related diseases [10] and diabetes mellitus [11]. Berberine was Promoting absorption of drugs [3], physiologic considered as the primary bioactive constituent barrier theory [4, 5] and receptortheory [6] had and chemical marker for the quality control of been applied to explain meridian guiding theory Rhizoma coptidis [12, 13]. EF was considered Effects of EF on targeted distribution of berberine om Sigma (CA, USA). Acetonitrile used for UPLC- MS/MS was of chromatographic grade, and ob- tained from Tedia Company Inc (Beijing, China). Other solutions were analytical reagent grade. Extraction of Evodiae Fructus (EF) EF (200 g) was socked in eight times of water for 45 min, then boiled the mixture and keep boiling for 60 min, filtered the extraction. The dregs were disposed via the same procedure for a second time. The filtrate was combined and concentrated to 200 mL, and then stored at -20°C until use. Thin-layer chromatography was adopted for qualitative identification of EF. The develop- ment for the extract was hexane chloroform acetone methanol (24:10:5.5:1), using evodia- mine and rutecarpine as the reference com- pounds. The picture was taken at 254 nm and Figure 1. Thin-layer chromatog analysis of EF. Spot a was evodiamine, spot b was rutecarpine, spot c and the photograph was shown in Figure 1. d were EF in different batch drug. Animals as MGD in Zuojin Pill and could enhance the All experimental procedures were conducted in effectiveness of the prescription. Although the- conformity with NIH guidelines for the Care and re were a lot of previous studies focused on Use of Laboratory Animals and were approved the pharmacological effects of EF, few reports by the Ethics Committee for Experimental An- involved in the meridian guiding effect besides imals of Henan Provincial Academy of TCM. its clinical application. Male Sprague Dawley (SD) rats (8-10 weeks of age) were purchased from Beijing Vital River In order to investigate the meridian guiding Laboratory Animal Technology Company Limit- action of EF, the concentrations of berberine ed (Beijing, China). Animals were housed under in rat tissues were analysed by UPLC-MS/MS standard conditions and fed with free diet. after oral administration of berberine with dif- ferent doses of EF. The meridian guiding action Tissue distribution studies was estimated by relative targeting efficiency (RTE), relative uptake efficiency (RUE) and max- After five days adaptation Sprague Dawley rats imum relative concentration (RCmax). So far, were randomly divided into four groups, 60 rats this is the first investigation to use targeting in each group. The divided experimental groups parameters to study EF on meridian guiding were as follows: control group (water), low dose theory in rats. of EF (250 mg/kg), medium dose of EF (500 mg/kg), high dose of EF (1000 mg/kg). Water Materials and methods or EF was given to the rats by intragastric administration daily for 7 consecutive days. Fi- Chemicals and reagents ve minutes after the last administration at day 7, berberine (80 mg/kg) was administered in Evodia rutaecarpa was provided by Shunkang rats by gavage. Medical Company (Zhengzhou, China). Berber- ine (purity >98%) was obtained from Henan Xin- Blood and tissues of interest (heart, liver, lung, yi Phytochemistry Company, (Xinxiang, China). stomach and kidney) were collected after adm- Evodiamine and rutecarpine were provided by inistration of berberine at the predetermined National Institutes for Food and Drug Control time points (0.5, 1, 1.5, 2, 3, 4, 6, 8, 12 and 24 (Beijing, China). Paracetamol was purchased fr- h). Six rats were sacrificed from every group for 7702 Int J Clin Exp Med 2018;11(8):7701-7709 Effects of EF on targeted distribution of berberine microporous filter membrane (0.22 μm) prior to analysis. 5 μL of the sample was analysed by UPLC-MS/MS. Before extracting tissue, the collected samples were homogenized in equal weight of 0.9% normal saline, then 200 μL homogenate was processed in the same way as described above for plasma and then detected by UPLC-MS/MS. Chromatography conditions The quantitation of berberine was carried out on a Waters Acquity ultra-performance liquid chromatography equipped with an automatic sampler, a quaternionic pump and a column compartment. All chromatographic separation was achieved on the Waters ACQUITY UPLCTM BEH C18 chromatography column (50 mm × 2.1 mm, 1.7 μm). The column temperature was maintained at 30°C. The flow rate was 0.3 mL/ min. The mobile phase consisted of acetonitrile and water containing 0.1% formic acid (20:80, v/v). The sample injection volume was 5 μL. Figure 2. Chromatograms for berberine and IS in rat In order to achieve high sensitivity, a triple qu- liver samples. 1. Berberine; 2. Internal standard (IS). adrupole mass spectrometer (Xevo-TQ-S mass A. Blank liver homogenate sample; B. Blank liver ho- spectrometer, Waters Corporation) was employ- mogenate sample spiked with berberine and IS; C. ed for quantification of berberine and the inter- Liver homogenate sample obtained at 2 h after oral administration of berberine. nal standard (IS). The mass spectrometer was set in the positive electrospray ionization (ESI) mode and the quantification mode was multi- each time point. Plasma was separated by ple reaction monitoring (MRM). The capillary centrifugation and tissues were blotted dry voltage was 3.20 kV, desolvation gas (N2) tem- with filter parer after washed with 0.9% normal perature was maintained at 500°C at a flow saline. Plasma and tissue samples were stored rate of 700 L/h, and the collision gas (N2) flow at -80°C for further detection. rate was 150 L/h. The precursor-to-product ion transitions were monitored at m/z 336.2>320.2 Sample preparation for UPLC-MS/MS analysis for berberine and m/z 152.2>110.1 for the IS. Plasma samples (200 μL) were placed in Ep- Method validation pendorf tubes. Thereafter 20 μL of the internal standard (paracetamol) was added to samples The selectivity of the analytical method was to get a final concentration of 100 ng/mL. After assessed by comparing the chromatograms of shaking for 10 s, 1000 μL of acetonitrile was six different batches of blank samples with the added to each tube, shake-mixed for 5 min and corresponding spiked samples with berberine ultrasonic extracted for 20 min.
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