Volume 8,Issue 4,2016 Table of Contents

1 Chinmedomics Builds a Bridge from Traditional to Modern Research of Traditional Chinese Medicine

Chang-xiao Liu

2016, 8(4):297-298. DOI: 10.1016/S1674-6384(16)60054-0

[Abstract](783) [HTML](0) [PDF 153.92 K](851)

Abstract:
Objective Pinoresinol di-glucopyranoside (PDG) is one of the main active lignans ingredients of Eucommiae Cortex considered to be a high-quality antihypertensive drug. In this study the pharmacokinetic process of PDG and its primary in vivo metabolite PG in the portal and jugular vein were surveyed and evaluated simultaneously. Methods A sensitive high-performance liquid chromatography coupled with tandem quadruple mass spectrometry (HPLC-MS/MS) method and sample preparation protocol were developed and validated in method of selectivity, sensitivity, precision, stability, and extraction recovery for the simultaneous determination of PDG and its primary metabolite pinoresinol glucoside (PG) in rat plasma.The double intubation technique was used to simultaneously collect blood from common jugular vein and hepatic portal vein after single ig administration of PDG. Results Using this method, the quantification linearity ranges of PDG and PG in rat plasma were both 0.05-100 ng/mL.This method was successfully applied to the evaluation of the absolute oral bioavailability of PDG and determination of the pharmacokinetic properties of PDG and PG after ig administration of single dose in rats. The bioavailability of PDG at common jugular vein ws 51.3% compared to that of 91.6% at hepatic portal vein. Conclusion We conclude that liver is the major conversion site of PDG to PG.

2 Chinmedomics: Newer Theory and Application

Xi-jun Wang , Ai-hua Zhang , Hui Sun , Guang-li Yan

2016, 8(4):299-307. DOI: 10.1016/S1674-6384(16)60055-2

[Abstract](537) [HTML](0) [PDF 982.57 K](887)

Abstract:
The scientific interpretation of the effectiveness of traditional Chinese medicine (TCM) is a communication channel between Chinese medicine and modern medicine. The evaluation of TCM efficacy is an important prerequisite for discovering active constituents. Therefore, there is an urgent need to establish a biological language for scientific explanation of the effectiveness of TCM, and modern scientists can further accept the significant value of TCM theory and its clinical practice. The syndrome and corresponding formulation are two important parts in TCM, and they are directly related to the effectiveness of TCM. Our team has taken syndrome and formulation as the research objects, integrated serum pharm-chemistry of TCM with metabolomics technology, developed a new platform termed Chinmedomics, which is capable of evaluating effectiveness of TCM and discovering the syndrome biomarkers as well as the effective substances. The correlation between the endogenous biomarkers of syndrome and exogenous constituents of formulation is analyzed to find the highly associated compounds as the effective substances, and further clarifying their activities, and may discover lead compounds. This effective strategy could speed the drug discovery from natural resources. This article systematically introduced the establishment and application of Chinmedomics theory, in order to provide references for studies on TCM, and some characteristic examples are presented to highlight the application of this new strategy for discovering the potential active constituents of TCM.

3 Clinical Implementation of Arsenic Trioxide

Lu-yao Sun , Hong Wang , Jin Zhou ,

2016, 8(4):308-313. DOI: 10.1016/S1674-6384(16)60056-4

[Abstract](473) [HTML](0) [PDF 244.81 K](780)

Abstract:
Introduction of arsenic trioxide (ATO, As2O3) to the treatment of acute promyelocytic leukemia in the 1970s enlightened an effective treatment approach for the disease. Decades later, knowledge on this agent’s further functions has rapidly advanced so that it has entered common use in hematology and oncology. In addition, As2O3 reportedly induces DNA and chromosomal damage, inhibits DNA repair, and alters DNA methylation in mammalian cells. The compound is becoming increasingly reasonable as a treatment modality to rectify genetic blood disorders and other cancer types. Nevertheless, limitations of As2O3 typically emerged from drug resistance, adverse effects and secondary tumors, which may result in a myriad of outcomes. Though prolonged exposure to As2O3 ensues poisons and genome alternations that do not permanently change the DNA sequence, other synergistic alterations should be considered as replacement. In this review, we recollect the discovery and clinical implementation of As2O3, describe its advantages and shortcomings for leukemia and solid cancer treatment, and consider future prospects for engendering useful impacts.

4 Optimization of Supercritical Fluid Extraction and Rapid Resolution LC-MS/ESI Identification of Chromones from Saposhnikoviae Radix through Orthogonal Array Design

Zhong-ming Han , Xue Wang , Miao-miao Xu , Yun-he Wang , Li-min Yang , Mei Han

2016, 8(4):314-322. DOI: 10.1016/S1674-6384(16)60057-6

[Abstract](468) [HTML](0) [PDF 329.12 K](761)

Abstract:
Objective To establish a rapid and effective supercritical fluid extraction (SFE) and rapid resolution liquid chromatography method coupled with diode-array detector (RRLC-DAD) to quantify the chromones in a species. Methods The effects of four parameters including ethanol concentration (50%-90%), pressure (25-45 MPa), temperature (40-60 oC), and time (30-90 min) on the chromones yields, namely prim-O-glucosylcimifugin, cimifugin, 5-O-methylvisammioside, and sec-O-gluco- sylhamaudol, were investigated using SFE system with orthogonal array design (OAD). Furthermore, the extracts were analyzed using rapid resolution liquid chromatography coupled with diode-array detector (RRLC-DAD) system to confirm the results. Results Under the optimized conditions, i. e., 35 MPa of pressure, 60 °C of temperature, 70% ethanol, and 60 min of time, the yields of prim-O-glucosylcimifugin, cimifugin, 5-O-methylvisammioside, sec-O-glucosylhamaudol, and total chromones were 3.514, 0.132, 6.242, 0.342, and 10.231 mg/g, respectively. In comparison with ultrasonic assisted extraction (UAE), SFE was able to yield a 20.7% increase in the total chromones from Saposhnikoviae Radix. Conclusion SFE is an alternative and promising method to extract chromones from this species, and the established RRLC-DAD method could serve as a rapid and effective method for the identification of chromones from Saposhnikoviae Radix.

5 Qualitative Analysis and Quality Evaluation of Cnidium monnieri Using UHPLC-ESI-Q-TOF/MS

Min Jia , Yi-min Li , Xin Zhai , Yang Yang , Chun-yan Li

2016, 8(4):323-330. DOI: 10.1016/S1674-6384(16)60058-8

[Abstract](924) [HTML](0) [PDF 0.00 Byte](13)

Abstract:
Objective To identify the coumarins constituents in Cnidium monnieri and classify ten samples into three groups and this helpful chemical information could be used for the further pharmacological and clinical study on C. monnieri. Methods Qualitative analysis of coumarins in C. monnieri was detected by UHPLC-ESI-Q-TOF/MS. Quadrupole TOF/MS in either full scan mode or extracted ion mode was used for the qualitative analysis of the constituents. Relative peak area of each component was used for the hierarchical cluster analysis. Results According to UHPLC-ESI-QTOF-MS data, chemical structures of 28 coumarins in the fruits of C. monnieri were identified, including 19 simple coumarins, seven linear coumarins, and two angular coumarins. Among these constituents, ten coumarins were firstly identified in C. monnieri. In addition, hierarchical cluster analysis suggested that C. monnieri from different regions could be classified into four groups, and this clustering was correlated to the distribution significantly, Xuzhou could be regarded as the genuine producing area. Conclusion UHPLC-ESI-Q-TOF-MS is a viable method for qualitative analysis and quality evaluation of coumarins from the fruit of C. monnieri. Coumarins in C. monnieri exists intra-species variance, which indicates significant meaning for the quality control and choice of famous region drug for C. monnieri in the clinic medication.

6 Simultaneous Determination of Eight Active Components in Liuwei Wuling Tablet Using HPLC

He-rong Cui , Gen-hua Xu , Wen-yan Jiang , Jing-jing Han , Jia-bo Wang , Zhao-fang Bai , Guang-ming Cai , Xiao-he Xiao

2016, 8(4):331-336. DOI: 10.1016/S1674-6384(16)60059-X

[Abstract](601) [HTML](0) [PDF 0.00 Byte](9)

Abstract:
Objective To develop an effective method for simultaneous determination of eight major components in Liuwei Wuling Tablet (LWT). Methods Reversed phase HPLC method was used with variously improved conditions. Results Salidroside, forsythoside A, specnuezhenide, phillyrin, schisandrol A, schizandrol A, schizandrin A, and schizandrin B in LWT were successfully separated on a Kromasil 100-5-C18 reverse phase column (250 mm × 4.6 mm, 5 μm) using acetonitrile-0.1% phosphoric acid (gradient elution) as mobile phase. The detection wavelength was 275 nm with flow rate of 1.0 mL/min, and the column temperature was maintained at 35 oC. The recovery rate of the method was within the range of 95.13%?104.56% and the precision (RSD) was less than 3% for all eight analytes. All the compounds showed good linearities (r 2 > 0.9980) in a relatively wide concentration range. Conclusion Simultaneous quantification of the multiple components by HPLC would be a better strategy for the quality evaluation of LWT.

7 Simultaneous Determination of Pinoresinol Di-gluco- pyranoside and Pinoresinol Glucoside in Rat Plasma by HPLC-tandem MS/MS for Pharmacokinetic Study

Er-wei Liu , Yan-ping Lin , Lei Wang , Yan Huo , Ying-yue Zhang , Jia-ding Guo , Li-feng Han , Yan-xu Chang , Xiu-mei Gao

2016, 8(4):337-343. DOI: 10.1016/S1674-6384(16)60060-6

[Abstract](896) [HTML](0) [PDF 0.00 Byte](14)

Abstract:
Objective Pinoresinol di-glucopyranoside (PDG) is one of the main active lignans of Eucommiae Cortex considered to be a high-quality antihypertensive drug. In this study the pharmacokinetic process of PDG and its primary in vivo metabolite pinoresinol glucoside (PG) in the portal and jugular vein were surveyed and evaluated simultaneously. Methods A sensitive high-performance liquid chromatography coupled with tandem quadruple mass spectrometry (HPLC-MS/MS) method and sample preparation protocol were developed and validated in method of selectivity, sensitivity, precision, stability, and extraction recovery for the simultaneous determination of PDG and its primary metabolite PG in rat plasma. The double intubation technique was used to simultaneously collect blood from common jugular vein and hepatic portal vein after single ig administration of PDG. Results Using this method, the quantification linearity ranges of PDG and PG in rat plasma were both 0.05-100 ng/mL. This method was successfully applied to the evaluation of the absolute oral bioavailability of PDG and determination of the pharmacokinetic properties of PDG and PG after ig administration of single dose in rats. The bioavailability of PDG at common jugular vein was 51.3% compared to that of 91.6% at hepatic portal vein. Conclusion We conclude that liver is the major conversion site of PDG to PG.

8 Cloning and Bioinformatic Analysis of HMGS and HMGR Genes from Panax notoginseng

Wan-jing Liu , Hai-zhou Lv , Liu He , Jing-yuan Song , Chao Sun , Hong-mei Luo , Shi-lin Chen

2016, 8(4):344-351. DOI: 10.1016/S1674-6384(16)60061-8

[Abstract](584) [HTML](0) [PDF 0.00 Byte](9)

Abstract:
Objective To clone and analyze 3-hydroxy-3-methylglutaryl coenzyme-A synthase (HMGS) and 3-hydroxy-3-methylglutaryl coenzyme-A reductase (HMGR) genes from Panax notoginseng of four-year old during the flowering period, the key genes involved in the mevalonic acid pathway for saponin biosynthesis. Methods The cDNA sequences of PnHMGS1 and PnHMGR2 were obtained by reverse transcription PCR (RT-PCR) and rapid amplification of cDNA ends (RACE) methods and were analyzed in their secondary structures, subcellular localizations, domains, and the three-dimensional structures of putative proteins by the bioinformatics tools. Fusion genes were constructed by the prokaryotic expression system. Results The two genes were cloned, named as PnHMGS1 and PnHMGR2, respectively, and were both predicted to be located in the chloroplast. PnHMGS1 (1410 bp) encoded a predictive unstable protein with 469 amino acids and covered hydroxymethylglutaryl-CoA synthase domain. PnHMGR2 (1690 bp) also encoded an unstable protein with 589 amino acids and possessed a hydroxymethylglutaryl-coenzyme A reductase domain and two transmembrane regions. Both of the genes were expressed most in flowers followed by roots, stems, and least in leaves. Conclusion PnHMGS1 and PnHMGR2 are firstly cloned from P. notoginseng as the new member of the HMGR family, and they show the same expression profile as P. ginseng and P. quinquefolius.

9 ITS2, a Better DNA Barcode than ITS in Identification of Species in Artemisia L.

Xiao-yue Wang , Si-hao Zheng , Yang Liu , Jian-ping Han

2016, 8(4):352-358. DOI: 10.1016/S1674-6384(16)60062-X

[Abstract](662) [HTML](0) [PDF 0.00 Byte](9)

Abstract:
Objective To select a more suitable DNA barcode to identify the species in Artemisia L. Methods ITS, ITS2, and three other major universal barcode candidates (matK, rbcL, and psbA-trnH ) were evaluated in the identification efficiency using a total of 1433 sequences downloaded from GenBank representing 343 species in Artemisia L. ITS and ITS2 were evaluated in the PCR and sequencing rate, sequencing peak quality (Q value), and misread rate. One hundred and twelve A. annua samples were collected from 11 populations across over China, which were amplified with universal primers on the ITS and ITS2 regions. Results ITS and ITS2 shared a higher identification efficiency and exhibited 71.43% and 64.11% detectability at the species level, respectively. The Q values of ITS and ITS2 showed that the direct PCR sequencing data were reliable for the ITS2 region and ITS exhibited poor sequencing trace quality. In certain sites, the ITS sequences exhibited reading ambiguities and errors, indicating that the misread and deletion sites in the ITS region would incorrectly inflate the identification ratio. Conclusion ITS2 is a suitable barcode for identification of species in Artemisia L., which enlarges the optimal range of divergence levels for taxonomic inferences using ITS2 sequences.

10 Effects of Berberine on Hepatic Sirtuin 1-uncoupling Protein 2 Pathway in Non-alcoholic Fatty Liver Disease Rats Induced by High-fat Diet

Yuan-jun Deng , Yu-pei Zhang , Qin-he Yang , Li Han , Yin-ji Liang

2016, 8(4):359-365. DOI: 10.1016/S1674-6384(16)60063-1

[Abstract](974) [HTML](0) [PDF 0.00 Byte](11)

Abstract:
Objective To investigate the involvement of sirtuin 1 (SIRT1)-uncoupling protein 2 (UCP2) pathway in the development of non-alcoholic fatty liver disease and whether berberine exerts its effects by regulating this pathway. Methods Male SD rats were divided into three groups: normal control group, high-fat diet group, and berberine supplement group. The rats in the normal control group were given normal diet while the rats in the other two groups were fed with high-fat diet. Rats in the berberine supplement group were concurrently given berberine (100 mg/kg body weight) once daily. After 16 weeks, the levels of serum, liver lipids, and serum aminotransferase were measured using an automatic biochemical analyzer. Superoxide dismutase (SOD) activity and malondialdehyde (MDA) content in the liver were measured using commercial kits. Histopathological changes of liver tissues were observed by hematoxylin and eosin (HE) staining and Oil Red O staining. The hepatic mRNA and protein levels of SIRT1 and UCP2 were assayed by reverse transcription polymerase chain reaction (RT-PCR) or Western blotting. Results Berberine supplement could significantly decrease the serum and liver lipid contents in rats fed with high-fat diet. Meanwhile, SOD level was significantly elevated, but MDA level was reduced in the liver. The results of HE and Oil Red O staining showed that the hepatic steatosis was alleviated in berberine supplement group. Furthermore, berberine induced an increase in SIRT1 expression but a decrease in UCP2 expression. Conclusion The regulation of hepatic SIRT1-UCP2 pathway may be an important mechanism by which berberine exerts the beneficial effects in NAFLD rats.

11 1,5-O-Dicaffeoyl-quinic Acid as a Novel Potential NMDA Receptor Inhibitor from Traditional Chinese Medicine Database by Virtual Screening

Xing Tian , Jian Wang , Jun Zhu , Yan-hua Fan , Wei-hong Meng , Rong Fan , Qing-chun Zhao

2016, 8(4):366-370. DOI: 10.1016/S1674-6384(16)60064-3

[Abstract](938) [HTML](0) [PDF 0.00 Byte](5)

Abstract:
Objective Neurodegenerative diseases, such as ischemia, traumatic injury, Alzheimer’s disease, and Parkinson’s disease are characterized by neuronal loss and dysfunction. It is known that glutamate-induced toxicity plays an important role in neurodegenerative diseases. Glutamate toxicity seems to be mediated by excessive influx of Ca2+ into neuronal cells through activation of N-methyl-D-aspartate (NMDA) receptor. To search for potential NMDA receptor inhibitors in traditional Chinese medicine. Methods A series of computer methods including drug-likeness evaluation, ADMET tests as well as molecular docking have been used. Results 1,5-O-dicaffeoyl-quinic acid was identified as NMDA receptor inhibitor by virtual screening. Its neuroprotective activity was further confirmed by in vitro test. 1,5-O-dicaffeoyl-quinic acid showed strong neuroprotection against NMDA-induced cell injury. Conclusion 1,5-O-Dicaffeoyl- quinic acid may be regarded as a potential NMDA receptor inhibitor for the prevention and treatment of neurodegenerative disorders.

12 Preparation of Rutin-liposome Drug Delivery Systems and Evaluation on Their in vitro Antioxidant Activity

Yu Guo , Li-xian Shen , Yan-feng Lu , Hai-yan Li , Ke Min , Lan-fang Li , Cui-yun Yu , Xing Zheng

2016, 8(4):371-375. DOI: 10.1016/S1674-6384(16)60065-5

[Abstract](1231) [HTML](0) [PDF 0.00 Byte](9)

Abstract:
Objective To prepare, characterize and evaluate the antioxidant activity of rutin-liposome (RL). Methods Liposomes of rutin were prepared by film dispersion method and the encapsulation efficiency (EE) was determined by RP-HPLC. Human umbilical vein endothelial cells (HUVECs) were injuried by H2O2 and treated with either free aqueous rutin or the RL delivery systems. The viability of HUVECs was determined by MTT and ELISA. Results The drug delivery system showed uniform rutin loaded nanoparticles with average particle size of (147.20 ± 1.42) nm, polydispersity index of (0.191 ± 0.003) nm, Zeta potential of (-20.0 ± 1.0) mV, and the drug EE was closed to 90.0%. The antioxidant effect of the drug delivery system to H2O2-damaged HUVECs showed that RL could increase injury cells viability compared to free aqueous rutin, which was accompanied with an obvious decrease in malondialdehyde (MDA), lactate dehydrogenase (LDH) while increase the level of nitrogen oxide (NOS). Conclusion The nanostructured RL is improved on the antioxidant effect and may be treating the different diseases caused by free radicals.

Volume 8,Issue 4,2016 Table of Contents

Current Issue

Volume

Issue

Most Read

Most Cited

Most Downloaded

WeChat

Mobile website