Volume 8,Issue 1,2016 Table of Contents

1 Medicinal Model Plants: Breaking the Traditional Medicine Research Methods

Chang-xiao Liu

2016, 8(1):1-2. DOI: 10.1016/S1674-6384(16)60001-1

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2 Biosynthesis and Regulation of Active Compounds in Medicinal Model Plant Salvia miltiorrhiza

Zhi-chao Xu , Ai-jia Ji , Xin Zhang , Jing-yuan Song , Shi-lin Chen

2016, 8(1):3-11. DOI: 10.1016/S1674-6384(16)60002-3

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Natural products from plant secondary metabolits are a major source of clinical drugs and industrial chemicals. Salvia miltiorrhiza is one of the most important plants in traditional Chinese medicine. Its dried roots and rhizomes are highly valued for use in the treatment of vascular diseases and for their anti-oxidative activities. Furthermore, S. miltiorrhiza is described as a medicinal model plant mainly due to its biosynthesis of active compounds. Here, we reviewed the research on S. miltiorrhiza in genomics, transcriptomics, biosynthesis of tanshinones and phenolic acids, biotic and abiotic elicitors, and regulation of transcription factors. This will provide a solid foundation for new breeding and synthetic biology approaches to produce and study natural products.

3 Pharmacology and Clinical Application of Plants in Epimedium L.

Jun Jiang , Bing-jie Zhao , Jie Song , Xiao-bin Jia

2016, 8(1):12-23. DOI: 10.1016/S1674-6384(16)60003-5

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Herba Epimedii is widely used as a traditional Chinese medicine for “strengthening the kidney” and “reinforcing bone” for a long time in China and other Asian countries. In this study, based on the large number of domestic and international references and research results, the authors reviewed pharmacological effects and the clinical application of species in genus Epimedium L. Meanwhile, chemical conversion and biotransformation of the major active compounds during the processing of the plants in Epimedium L. and their metabolism in vivo were summarized. This provides a guidance for the application and development in clinical therapy in the future.

4 Phytopharmacological Review on Vitex agnus-castus: A Potential Medicinal Plant

Hina Zahid , Ghazala H. Rizwani , Sumaira Ishaqe

2016, 8(1):24-29. DOI: 10.1016/S1674-6384(16)60004-7

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Vitex agnus-castus is a small tree or shrub, belonging to the family Verbenaceae. It is a deciduous shrub native to European, Mediterranean, and Central Asian countries. V. agnus castus has a long tradition as a herbal remedy and was used in ancient times not only as an anaphrodisiac but also against diverse disturbances of the female genital system. The major constituents in V. agnus-castus are flavonoids, essential oils, diterpenes, and glycosides. The flavonoids (casticin, quercetagetin, and isovitexin) have been shown in vitro to affect estrogen receptors. V. agnus-castus could be used to treat acne, digestive complaints, menstrual irregularities, premen-strual syndrome (PMS), mastalgia, and infertility, and also for lactation support. Although V. agnus-castus has been used for centuries and enjoys wide support from practitioners and the general public for many gynecological com-plaints, few clinical studies support its documented uses. The presence of phytochemical and pharmacological activities has proved that the plant has a leading capacity for the development of new good efficacy drug in future.

5 Cell Cycle Arrest, Apoptosis, and Autophagy Induced by Chabamide in Human Leukemia Cells

Kun Hu , Meng Yang , Yuan-yuan Xu , Kun Wei , Jie Ren

2016, 8(1):30-38. DOI: 10.1016/S1674-6384(16)60005-9

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Objective To investigate the antitumor effect of chabamide in K562 (human leukemia cell line) cells. Methods The cytotoxicity was assessed by a standard colorimetric assay using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT). The morphological changes were observed by Hoechst 33258 staining. Induction of apoptosis, loss of the mitochondrial membrane potential (ΔΨm), and cell cycle analysis were evaluated by flow cytometry (FCM) analysis. Levels of apoptosis-related proteins, cell cycle-related proteins, and LC3 protein were detected by Western blotting. Moreover, the autophagy induced by chabamide was also detected by MDC fluorescent staining. Results Chabamide significantly inhibited cell proliferation by cell cycle arrest in the G0/G1 phase. This phenomenon was associated with an obvious increase in p21 expression and decrease in cyclin D1 and cyclin-dependent kinase 2/4/6 protein expression. Moreover, chabamide could regulate the changes in mitochondrial membrane potential, increase the expression of apoptosis-related proteins, such as Bax and cytochrome C, and decrease the protein expression of Bcl-2, caspase-9, caspase-3, and PARP-1. JNK, ERK1/2, and p38 were also regulated by chabamide in K562 cells. Furthermore, induction of autophagy, marked by autophagic vacuole formation, was detected. Conversion of LC3-I to LC3-II, a marker of active autophagosome formation, was also detected following chabamide treatment. Conclusion The antitumor activity of chabamide with the results of apoptosis and autophagy induction was confirmed in K562 cells.

6 PERK Signaling of Unfolded Protein Response Activated in Acute Hypobaric Hypoxia and Effect of Ginsenoside Rb1

Yun Li , Hong-bo Luo , Xiang-qun Shi , Chun-sheng Xi , Jian-kui Guo , Zhi-qiang Zhang , Li Cao , Xiao-yan Zhang , Zhao Liu

2016, 8(1):39-43. DOI: 10.1016/S1674-6384(16)60006-0

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Objective To observe pancreatic ER kinase (PERK) signaling of unfolded protein response (UPR). Methods The rats were divided into control, model, and ginsenoside Rb1 (Rb1) groups, and put into hypoxia chamber to establish the acute plateau stress model. The water solutions of Rb1 were given to rats in Rb1 group for 7 d. After that, The behavior of rats was observed by Y-maze and passive avoidance test and the rats were sacrificed in a batch for detection by Western blotting. Results Hypobaric hypoxia mediated UPR pathway accompanied the activation of protective pathways such as PERK-eIF2a-ATF4 and Grp78/Bip pathways. On the other hand, Rb1, the extract from herbal medicine ginseng, increased on the expression of PERK, eIF2a, ATF4, and Grp78/Bip in rats. Conclusion The results indicate that PERK-eIF2a-ATF4-GRP78 pathway is a potential target for therapeutic applications in high altitude diseases and Rb1 can attenuate the injury to memory function caused by hypobaric hypoxia neurotoxicity.

7 Preparation of Colon-specific and Synchronous Release Pellet Containing Total Alkaloids of Sophora alopecuroides

Li-ping Liang , Hong-lang Chen , Shu-ming Zhao , Wen-feng Chen , Li-jun Song , Wen-chang Zhao

2016, 8(1):44-52. DOI: 10.1016/S1674-6384(16)60007-2

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Objective To deliver multiple component drugs to colon site and sustain a synchronous release for better therapeutic effect. For achieving this purpose, colon specific pellet containing total alkaloids of Sophora alopecuroides (TASA) was prepared. Methods The pellet was prepared by extrasion-spheronizing and subsequently coated with three layers of two polymers. Results The pellet core consisted of 40% TASA, 1:2 in ratio of Bletilla striata polysaccharide (BSP), an enzyme-degradable material, to microcrystalline cellulose (MCC), filler, and 1% CMC-Na solution as binder by optimization. Concerning of the three coated layers, the outer layer was coated with Eudragit RS30D for controlling drug release in colon, the intermediate layer and the inner layer were coated with same polymer, Eudragit S100, for preventing drug release in upper gastrointestinal tract, which required 23.2%, 21.7%, and 9.3% weigh gain, respectively. The coated pellets released 1.20% of sophoridine and 1.98% of matrine in media mimicking the stomach condition for 2 h, and 23.88% of sophoridine and 22.91% of matrine in media mimicking the intestine for 3 h and finally 90.25% of sophoridine and 89.94% of matrine in colonic conditions within 24 h. And the similarity factor f2 of sophoridine and matrine of release curve for investigated formulation was internal in (50?100) and > 80, demonstrating that sophoridine and matrine in formulation achieved a synchronous release. Conclusion The coated pellets achieve a certain colon-specific release and synchronous release.

8 LC–MS/MS Method for Quantification of Liquiritigenin in Rat Plasma: Application to Pharmacokinetic Study of Liquiritin

Shi-qi Dong , Hui-rong Fan , Quan-sheng Li , Guang-li Wei , Ya-zhuo Li , Chang-xiao Liu , Duan-yun Si

2016, 8(1):53-60. DOI: 10.1016/S1674-6384(16)60008-4

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Objective A simple, sensitive, and rapid LC-MS/MS method has been established and validated for the determination of liquiritigenin (LG) in rat plasma. Methods Naringenin was chosen as internal standard (IS). LG and IS were separated on a Diamonsil C18 analytical column with a mobile phase of methanol-10% methanol in water containing 0.5 mmol/L ammonium formate and 0.2% formic acid (55:45) at the isocratic flow rate of 0.6 mL/min for 10 min. The multiple reaction monitoring (MRM) was performed on a mass spectrometer in the negative ion mode with electro-spray ionization (ESI) source and the transition from precursor ion to product ion was m/z 255.0→119.0 for LG and m/z 271.0→151.0 for IS, respectively. Results The linearity was acceptable in the range of 5-5000 ng/mL (r = 0.9973). The inter-day and intra-day accuracies were in the ranges of ?0.09%?3.25% and ?5.02%?9.21%, respectively. The precision was in the ranges of 3.60%?12.4% and 0.909%?6.89%, respectively. LG was stable in the course of analysis and storage. Conclusion The LC-MS/MS method was successfully applied to the pharmacokinetic study for the first time in rats after ig and iv administration of liquiritin (LQ), a glycoside of LG, at pharmacologically effective levels.

9 Hemolytic assay for Huangqi Injection

Hang Xiao , Yu-bin Xu , Xia Liu , De-qiang Dou

2016, 8(1):61-66. DOI: 10.1016/S1674-6384(16)60009-6

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Objective Huangqi Injection is a preparation with an extract of Astragali Radix which has a long history of being used as a tonic to strengthen the body’s immunity. Anaphylaxis and hemolysis are two main adverse drug reaction (ADR) of injections. Our study was aimed to establish an approach for the (ADR) prediagnosis of Huangqi Injection. Methods An in vitro model for anaphylactoid assay of Huangqi Injection based on the release rate of histamine and β-hexosaminidase of RBL-2H3 cells induced by injections and a colorimetric method based on the detection of hemoglobin resulted in the erythrocyte hemolysis for prediagnostic assaying the hemolytic ADR of injections were established. Results Both histamine and β-hexosaminidase are the anaphylactiod mediators, but β-hexosaminidase release induced by Huangqi Injection could not be determined by spectrophotometry due to the interference of the injection itself. In addition, normal hemolysis and abnormal hemolysis were discovered during the experiment. The fingerprints and tannins in different batches of injections showed obvious differences, indicating that the content of tannins was related to abnormal hemolysis and higher histamine-secreting from RBL-2H3 cells. Conclusion The results indicate that the hemolytic assaying method is not only suitable for prediagnostic assaying of hemolytic ADR of herbal medicine injection, but also partly reflects the anaphylaxis of herbal injections, and tannins may be the major factors causing abnormal hemolysis.

10 Molecular Cloning and Expression of Squalene Epoxidase from a Medicinal Plant, Bupleurum chinense

Ke Gao , Jie-sen Xu , Jing Sun , Yan-hong Xu , Jian-he Wei , Chun Sui

2016, 8(1):67-74. DOI: 10.1016/S1674-6384(16)60010-2

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Objective In plant, squalene epoxidase (SE) catalyzes the first oxygenation step in the biosynthetic pathway of triterpenoid and phytosterol, representing one of the rate-limiting enzymes in this pathway. Bupleurum chinense is an important medicinal herb with its major active constituents such as triterpenoid saponins and saikosaponins. In order to obtain the series of enzymatic genes involved in saikosaponin biosynthesis, a cDNA of SE, designated BcSE1, was cloned from B. chinense. Methods The BcSE1 gene was cloned by homology-based PCR and 5’/3’ RACE methods from the adventitious roots of B. chinense. The physical and chemical parameters of BcSE1 protein were predicted by protparam. In order to discover hints in amino acid sequences on the dominant functions in the biosynthesis of saponin or phytosterol, sequences of SE from other plants were downloaded from NCBI for sequences alignment and phylogenetic analysis. BcSE1 was cloned into a yeast mutant KLN1 (MATa, erg1::URA3, leu2, ura3, and trp1) to verify the enzyme activity of BcSE1. Additionally, the tissue-specific expression and methyl jasmonate (MeJA) inducibility of BcSE1 were investigated using quantitative real-time PCR. Results The predicted protein of BcSE1 is highly similar to SEs from other plants sharing amino acid sequence identities of up to 88%. The BcSE1 can functionally complement with yeast SE gene (ERG1) when expressed in the KLN1 mutant (MATa, erg1::URA3, leu2, ura3, and trp1). Using as controls with β-amyrin synthase (β-AS) which is presumed to catalyze the first committed step in saikosaponin biosynthesis and a cycloartenol synthase (CAS) relating to the phytosterol biosynthesis, the transcript of BcSE1 was significantly elevated by MeJA in adventitious roots of B. chinense and the transcript of BcSE1 was most abundant in the fruits and flowers of plants, followed by that in the leaves and roots, and least in stems. Conclusion It is the first time to illustrate the molecular information of SE in B. chinense and to clone the full-length SE gene in plants of genus Bupleurum L.

11 Isolation and Chemotaxonomic Significance of Chemical Constituents from Rubus parvifolius

Quan-xi Mei , Xiao-lu Chen , Xue Xia , Zhi-jian Fang , Hong-bo Zhou , Yu-qiao Gao , Wei-bo Dai , Ren-wang Jiang

2016, 8(1):75-79. DOI: 10.1016/S1674-6384(16)60011-4

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Objective To study the chemical constituents from the roots of Rubus parvifolius. Methods The chemical constituents were extracted and purified by silica gel column chromatography. NMR spectra were used for structural identification. Results Phytochemical study on the roots of R. parvifolius led to the isolation of one ceramide (1), two anthraquinones (2 and 3), four triterpenoids (4-7), two flavonoids (8 and 9), one fatty acid ester (10), and two sterols (11 and 12). Conclusion Compound 1 is isolated from the plants of family Rosaceae for the first time, and compounds 2-5 are isolated from genus Rubus for the first time. Though R. parvifolius shares the same major chemical types (triterpenoid, flavonoid, and anthraquinone) with those of R. alceaefolius, a substituent of R. parvifolius, their individual constituents are different. In addition, R. parvifolius contains ceramide (1) with high concentration, while caffeoylquinic acid reported in R. alceaefolius has not been found in R. parvifolius. Furthermore, the results from our phytochemical study are consistent with the DNA phylogenic relationship between R. parvifolius and R. alceaefolius (two separated subgenera), suggesting that the substitution of the former species with the latter one in folk medicine might not be suitable.

12 Chemical Constituents from Leaves of Camellia nitidissima and Their Potential Cytotoxicity on SGC7901 Cells

Jing Qi , Ruo-fu Shi , Jian-ming Yu , Yi Li , Sheng-tao Yuan , Ji-zhu Yang , Jiang-miao Hu , Ai-qun Jia

2016, 8(1):80-84. DOI: 10.1016/S1674-6384(16)60012-6

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Objective To isolate and identify the bioactive phytochemicals from the leaves of Camellia nitidissima. Methods The chemical constituents were isolated and purified by repeated silica gel, Sephadex LH-20, MCI gel columns, recrystallization， and semi-preparative HPLC techniques. The chemicl structures of these compounds were identified on the basis of spectral data including NMR and MS. Then quorum sensing inhibition (QSI) activities of these compounds were tested using Chromobacterium violaceum CV026 as the bioindicator strain. The antitumor activities of these compounds were measured using SGC7901 as cell proliferation and cytotoxicity. Results α-Spinasteryl-β-D-glucopyranoside (1), stigmasta-7,22-diene-3-O-[α-L-arabinopyranosyl (1→2)]-β-D-galactopyranoside (2), kaempferol 3-O-[2-O-(trans-p-coumaroyl)-3-O- α-D-glucopyranosyl]-α-D-glucopyranoside (3), aromadendrin (4), catechin (5), phlorizin 4′-O-β-D-glucopyranoside (6), (3R,6R,7E)-3-hydroxy-4,7-megastigmadien- 9-one (7), dodecanoic acid (8), 3β-acetoxy-20-lupanol (9), and 3β,6α,13β- trihydroxyolean- 7-one (10) were successively isolated from the leaves of C. nitidissima. Unfortunately, these compounds had no QSI activity. Based on Cell Counting Kit-8 (CCK-8) assay, compound 10 showed the best anti-tumor activity of all compounds (IC50 = 91.7 μg/mL). Conclusion Apart from compounds 4 and 5, other eight compounds are reported in this plant for the first time. All compounds show no QSI activity, compound 10 shows potential cytotoxic activity on SGC7901 cells in vitro.

13 Minor Compounds from Fungus Ganoderma cochlear

Man Dou , Rong-tao Li , Yong-xian Cheng

2016, 8(1):85-88. DOI: 10.1016/S1674-6384(16)60013-8

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Objective To study the chemical constituents of the fungus Ganoderma cochlear. Methods The compounds were isolated by using MCI gel CHP 20P, Sephadex LH-20, RP-18 column chromatography, and preparative TLC. The structures were identified by means of spectroscopic methods. Results Two phenolic normeroterpenoid and meroterpenoid, cochlearols C and D (1 and 2), together with six benzene derivatives, 3- methoxy-4-hydroxy-phenylethanol (3), 4-hydroxyacetophenone (4), p-hydroxycinnamic methyl ester (5), 2-methoxy-4-hydroxybenzaldehyde (6), 4-hydroxy-3-methoxy benzoic acid (7), and 2-hydroxy-5-ethoxybenzoic acid (8), were isolated from the fruiting bodies of Ganoderma cochlear. Conclusion Compounds 1 and 2 are new phenolic normeroterpenoid and meroterpenoid, respectively.

14 Flavonoids from Heartwood of Dalbergia cochinchinensis

Rong-hua Liu , Xin-chao Wen , Feng Shao , Pu-zhao Zhang , Hui-lian Huang , Shuang Zhang

2016, 8(1):89-93. DOI: 10.1016/S1674-6384(16)60014-X

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Objective To study the flavonoids from the heartwood of Dalbergia cochinchinensis. Methods The chemical constituents were isolated and purified by combination of silica gel, macroporous resin, Sephadex LH-20, and ODS column chromatography. Their structures were identified by means of spectral analysis. Results Fifteen flavonoids were isolated and identified as pinocembrin (1), liquiritigenin (2), galangin (3), 7-hydroxy- 6-methoxyflavone (4), naringenin (5), alpinetin (6), 2,3-dimethoxyxanthone (7), 6,4′-dihydroxy-7-methoxy-flavan (8), mucronulatol (9), 7,8-dihydroxyflavanone (10), 5,7,3′,5′-tetrahydroxyflavanone (11), 4,2′,5′-trihydroxy-4′-methoxychalcone (12), isoliquiritigenin (13), butein (14), and 3′,5′,5,7-tetrahydroxy-6-C-β-D-glucopyranosyl- flavanone (15), respectively. Conclusion Compounds 7, 8, 10, and 15 are isolated from the plants of Dalbergia L. f. for the first time, and compounds 1, 3, 5, 6, 9, 11, 12, and 14 are isolated from this plant for the first time.

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