Volume 8,Issue 3,2016 Table of Contents

1 Implementation of Pharmacopoeia Regulations

Chang-Xiao Liu

2016, 8(3):195-195. DOI: 10.1016/S1674-6384(16)60042-4

[Abstract](544) [HTML](0) [PDF 149.55 K](1207)

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2 Revision and Improvement of Criterion on Traditional Chinese Medicines in Chinese Pharmacopoeia 2015

Yang Dan , Zhong-zhi Qian , Yong Peng , Chang-qing Chen , Yan-ze Liu , Wen Tai , Jing-wen Qi

2016, 8(3):196-208. DOI: 10.1016/S1674-6384(16)60043-6

[Abstract](1319) [HTML](0) [PDF 311.21 K](10438)

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Chinese Pharmacopoeia is updated every five years, of which traditional Chinese medicine (TCM) is the most important part. The 2015 version completed by the 10th Pharmacopoeia Commission has come into operation since December 1, 2015. Here we introduced the revision and improvement of quality evaluation and control standards of TCMs in Chinese Pharmacopoeia 2015.

3 Genus Ilex L.: Phytochemistry, Ethnopharmacology, and Pharmacology

Fan Yi , Xiao-ling Zhao , Yong Peng , Pei-gen Xiao

2016, 8(3):209-230. DOI: 10.1016/S1674-6384(16)60044-8

[Abstract](580) [HTML](0) [PDF 981.04 K](3839)

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The genus Ilex L. has been used as remedies in traditional Chinese medicine in Aquifoliaceae and beverages for thousands of years due to abundant pharmaceutical bioactivities. There are 600 species in genus Ilex L. containing various compounds such as terpenoids, saponins, glycosides, etc. Three species, I. cornuta, I. chinensis, and I. rotunda have been admitted in Chinese Pharmacopoeia 2015 to treat dyspepsia, stomatitis, and hyperactivity cough and protect the liver and kidney. Recent studies showed that several species have been daily drunk to promote human health and prevent cardiovascular diseases in the folk. Here we reviewed the genus Ilex L. in phytochemistry, ethnopharmacology, and pharmacology.

4 Effects of Coptidis Rhizoma on Cell Cycle, DNA Damage, and Apoptosis in L929 Murine Fibroblast Cells

Yan-fei Huang , Man-man Gu , Jing Xu , Chun-yang Han , Teng-fei Liu , Cui-yan Liu

2016, 8(3):231-241. DOI: 10.1016/S1674-6384(16)60045-X

[Abstract](843) [HTML](0) [PDF 416.51 K](1274)

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Objective Coptidis Rhizoma (CR), a widely used traditional Chinese herbal medicine, is commonly believed to be non-toxic. However, little is known about its cytotoxicity and relevant mechanisms at cellular and genetic levels. The present study was conducted to explore the cytotoxicity of CR and its mechanisms related to cell cycle arrest, DNA damage, cell apoptosis, and mitochondrial membrane potential in L929 murine fibroblast cells. Methods The cells were cultured and treated with different concentration of CR aqueous extract for 24 h. Cell viability was determined by CCK-8 method, morphological changes, and mitochondrial membrane potential were observed with an inverted microscope, cell cycle and cell apoptosis were examined by flow cytometry and DNA damages were detected by comet assay. Results Our results showed that cell viability was significantly decreased in a dose-dependent manner when concentration was higher than 0.2 mg/mL. A concentration above 1 mg/mL altered the cells morphology. Each DNA damage indicator score increased in the groups with the concentration of above 0.1 mg/mL. Cells at G2/M phase, cell apoptosis and mitochondrial membrane potential changed in the 2 mg/mL group. Conclusion Overall, our study suggests that CR at a high dosage exhibits cytotoxicity on L929 cells, which is likely to be the consequences of cell cycle arrest, DNA damage, cell apoptosis and mitochondrial membrane potential reduction.

5 Effects of Zhengtian Pills on Migraine Headache in Rats via Transient Receptor Potential Vanilloid 1

Jun-hua Sun , Ke-zhu Wang , Hui Fu , Zhi Dai , Fei-fei Pu , Song Yin , Tian-xiu Qian , Xin-min Liu , Xiao-ying Wang

2016, 8(3):242-250. DOI: 10.1016/S1674-6384(16)60046-1

[Abstract](591) [HTML](0) [PDF 368.46 K](1284)

Abstract:
Objective Coptidis Rhizoma (CR), a widely used traditional Chinese herbal medicine, is commonly believed to be non-toxic. However, little is known about its cytotoxicity and relevant mechanisms at cellular and genetic levels. The present study was conducted to explore the cytotoxicity of CR and its mechanisms related to cell cycle arrest, DNA damage, cell apoptosis, and mitochondrial membrane potential in L929 murine fibroblast cells. Methods The cells were cultured and treated with different concentration of CR aqueous extract for 24 h. Cell viability was determined by CCK-8 method, morphological changes, and mitochondrial membrane potential were observed with an inverted microscope, cell cycle and cell apoptosis were examined by flow cytometry and DNA damages were detected by comet assay. Results Our results showed that cell viability was significantly decreased in a dose-dependent manner when concentration was higher than 0.2 mg/mL. A concentration above 1 mg/mL altered the cells morphology. Each DNA damage indicator score increased in the groups with the concentration of above 0.1 mg/mL. Cells at G2/M phase, cell apoptosis and mitochondrial membrane potential changed in the 2 mg/mL group. Conclusion Overall, our study suggests that CR at a high dosage exhibits cytotoxicity on L929 cells, which is likely to be the consequences of cell cycle arrest, DNA damage, cell apoptosis and mitochondrial membrane potential reduction.

6 Effect of Polygoni Cuspidati Rhizoma et Radix and Its Ingredient Resveratrol on Experimental Autoimmune Myasthenia Gravis by Suppressing Immune Response

Shen Liu , Xin-xin Zhang , Shan Zhuang , Chun-hong Li , Yan-bin Li

2016, 8(3):251-258. DOI: 10.1016/S1674-6384(16)60047-3

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Objective To investigate the effects of Polygoni Cuspidati Rhizoma et Radix (PCRR) and its ingredient resveratrol (Res) on experimental autoimmune myasthenia gravis (EAMG). Methods EAMG was induced in Lewis rats by the immunization of a synthetic peptide corresponding to region 97–116 of the rat acetylcholine receptor (AChR) α subunit (R97-116). EAMG rats were randomly divided into PCRR group, Res group, and control (C) group, and were ig administered respectively with PCRR (2 g/kg), Res (20 mg/kg), and DMSO (0.4 mL/kg) every day from day 5 after immunization to day 42. Clinical evaluation, lymphocyte proliferation, cytokines, and anti-97-116 antibodies were performed for examination of their therapeutic effects. Results Treatments with PCRR and Res significantly ameliorated clinical symptoms, down-regulated TNF-α and up-regulated IL-10 in serum and culture supernatants of lymphocytes stimulated with R97-116, and decreased levels of anti-R97-116 IgG1 and IgG2a in serum compared with C group. Unexpectedly, PCRR but not Res inhibited lymphocyte proliferation compared with C group. Conclusion PCRR and Res ameliorating EAMG is associated with suppressing immune response, and indicates a therapeutic potential for EAMG and even human myasthenia gravis (MG). Res may be the main effective ingredient from PCRR ameliorating EAMG, but further experiments are necessary.

7 Inhibition of Ovalitenin A on Proliferation of HeLa Cells via Apoptosis, G2/M Cell Cycle Arrest, and Down- regulation of COX-2

Dong-yu Liu , Yan Guo , Jian-yong Si , Gui-bo Sun , Bing Zhang , Li Cao

2016, 8(3):259-266. DOI: 10.1016/S1674-6384(16)60048-5

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Objective Ovalitenin A (1-(4-methoxybenzofuran-5-yl)-3-phenyl-2-propen-1-one) is a chalcone isolated from Millettia pulchra. The aim of the study was to investigate the antitumor effect of ovalitenin A on apoptosis in vitro and in vivo and to identify the mechanism involved. Methods The effect of ovalitenin A in human cervical cancer HeLa cells was detected by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay, morphological observation, flow cytometric measurement, Western blotting, and xenograft model. Results Ovalitenin A inhibited the proliferation of HeLa cells in a dose-dependent manner in vitro and in vivo and induced the apoptosis evidenced by characteristic apoptotic morphological changes, phosphatidylserine externalization, and activation of caspase-3. In addition, ovalitenin A induced G2/M cell cycle arrest and up-regulation of the Bax/Bcl-2 ratio. Furthermore, ovalitenin A decreased protein level of COX-2 and induced the loss of mitochondrial membrane potential. Conclusion These data suggest that ovalitenin A has the potential of anticancer properties for the treatment of cervical cancer.

8 Effects of Zhengtian Pills on Migraine Headache in Rats via Transient Receptor Potential Vanilloid 1

Jun-hua Sun , Ke-zhu Wang , Hui Fu , Zhi Dai , Fei-fei Pu , Song Yin , Tian-xiu Qian , Xin-min Liu , Xiao-ying Wang

2016, 8(3):267-272. DOI: 10.1016/S1674-6384(16)60049-7

[Abstract](479) [HTML](0) [PDF 0.00 Byte](12)

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Objective To investigate the effects and molecular mechanism of Zhengtian Pills (ZTP) on migraine headache. Methods All rats were randomly divided into control, positive control, migraine model, low- and high-dose ZTP groups, and glyceryl trinitrate was injected to induce migraine headache. The time of ears turning red, frequency of scratching head, climbing the cage, and head-twitching were used to evaluate rat behaviors. After 10 d administration of ZTP, the expression levels of transient receptor potential vanilloid 1 (TRPV1) both in cortex and hippocampus were determined by Western blotting. Results After 2 min of glyceryl trinitrate injection, rats showed headache phenomena that parallels the clinical symptoms of migraine, which peaked in 30 min, and lasted for 60 min. Frequency of head-twitching and numbers of scratching head in glyceryl trinitrate (GTN) group were significantly increased. In contrast, after ZTP (1.08 g/kg, ig) treatment, the numbers of scratching head with fore-limb, hind-limb and the frequency of head-twitching were significantly decreased. Flunarizine (FLU) and low-dose ZTP (0.54 g/kg) also showed a trend to decrease the numbers of scratching head and head-twitching frequency, but no significant difference. Besides, ZTP significantly decreased the up-regulated TRPV1 protein expression level both in cortex and hippocampus. Conclusion The present study shows that ZTP could significantly improve the migraine symptoms of headache in rats and TRPV1 might be one of the important molecular mechanisms. This is the first report about the effect of ZTP on TRPV1 protein expression level both in cortex and hippocampus of rats.

9 Evaluation of Antinociceptive Activity of Methanol Extract from Cleome rutidosperma in Mice

Prawej Ansari , Mitali Debnath , Md. Foyez Ahmad , Shofiul Azam , Shafia Akther , Gazi Md. Mustakim , Md. Hamza Naquib , JMA Hannan

2016, 8(3):273-279. DOI: 10.1016/S1674-6384(16)60050-3

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Objective Cleome rutidosperma (Capparidaceae), commonly known as “Fringed Spider Flower”, is a medicinal plant found in Southeast Asia. C. rutidosperma is used in folk medicine for diuretic, laxative, analgesic, anti-inflammatory, antipyretic, antimicrobial, anti-oxidant, hypoglycemic, and anthelmintic activities. We have evaluated the anti-nociceptive properties of methanol extract from C. rutidosperma (MECR) in vivo. Methods Thermal method (hot plate test and tail flick test) was induced to judge the anti-inflammatory effect and couple of chemical method also used (formalin induced licking test; writhing test carried by acetic acid) to evaluate analgesic effect. Both of these tests were made over animal models, like mice and rats. Two different doses (100 and 200 mg/kg) were used for each case of test, while morphine sulphate (5mg/kg, ip) was used as reference drug. Results MECR demonstrated the significantly anti-nociceptive activity in the analgesic and anti-inflammatory tests by reducing nociception in mice models (P < 0.001). In the hot-plate and tail-flick tests, MECR significantly elongated the time to response to the thermal stimuli (100 and 200 mg/kg with P < 0.05, 0.001). The remarkable increase in the latency was observed at 90 and 120 min. In acetic acid-induced writhing test and formalin induced licking test for anti-inflammatory activity, MECR at 100 and 200 mg/kg doses exhibited significant (P < 0.001) reduction of writhing and licking response. Conclusion The anti-inflammatory and analgesic effects of C. rutidosperma propose that this effect may be a result of both peripheral and central mechanisms. Further study is required to ensure the proper mechanism of action as well as the active ingredient.

10 Simultaneous Determination of Eight Constituents in Fruits of Rubus chingii by UPLC

Xin Chai , Long-fei Du , Jing Yang , Zhen-zuo Jiang , Long Yang , Yue-fei Wang , Yan Zhu ,

2016, 8(3):280-285. DOI: 10.1016/S1674-6384(16)60051-5

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Objective To develop a simple, efficient, and reliable method for routine quantitative analysis of main constituents presented in the fruits of Rubus chingii, which is widely used in Chinese materia medica (CMM), known as Fupenzi (FPZ) in Chinese. Methods An ultra performance liquid chromatography-photo diode array (UPLC-PDA) system was employed for simultaneous quantification of eight compounds, i. e. adenosine, gallic acid, brevifolin carboxylic acid, ethyl gallate, ellagic acid, kaempferol-3-O-rutinoside, kaempferol-3-O-b-D-glucopyranoside, and tiliroside. The chromatographic analysis was performed on a C18 column using a gradient elution of acetonitrile -0.1% formic acid aqueous solution within a runtime of 25 min. Results All calibration curves were linear (R2 > 0.9997) over the tested ranges. The intra- and inter-day precisions as determined from sample solutions were both less than 2.45% and 2.78%, respectively. The average recoveries for the eight constituents ranged from 94.77% to 101.35% with RSD ￡ 4.41%. The newly-developed method was applied to the quality assessment of various R. chingii samples, including both ripe and unripe fruits of R. chingii from different habitats. Conclusion The relative levels of the investigated compounds vary remarkably in the fruits of R. chingii collected from different habitats. As only two of the eight compounds, adenosine and ellagic acid, are determined in the ripe fruits of R. chingii, the results may explain the reason why only the unripe fruits can be used in CMM.

11 Comprehensive Evaluation of Powdered Chinese Herbal Medicines-An Exemplification of Isatidis Radix

Xue Han , Ming-quan Wu , Zhi-rui Yang , Ding-kun Zhang , Yi Mao , Jin Han , Yin-qiu Huang , Yong-feng Zhou , Yan-ling Zhao , Jia-bo Wang , Xiao-he Xiao

2016, 8(3):286-292. DOI: 10.1016/S1674-6384(16)60052-7

[Abstract](557) [HTML](0) [PDF 0.00 Byte](12)

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Objective Currently, powdered Chinese herbal medicines (CHMs) were mainly evaluated through physical property, chemical dissolution, and bioactivity independently. It could not reflect the quality comprehensively. This paper was to explore and establish a comprehensive evaluation method for powdered CHMs. Methods Isatidis Radix was chosen as an exemple. Firstly, powdered Isatidis Radix in different particle size was prepared. Then, their physical properties were characterized. The dissolution of index component epigoitrin was determined, and their antiviral activities were evaluated by neuraminidase-based bioassay. Results As the particle size decreased, powder distribution tended to be uniform, and the dissolution of epigoitrin increased, antiviral activity enhanced. According to cluster analysis of above results, the sequence of evaluation consequence was ultrafine powder S2 (D90: 32.80 ± 0.29) > ultrafine powder S1 (D90: 52.08 ± 0.53) > fine powder S0 (D90: 118.16 ± 0.76) (from the superior to the inferior). Conclusion Overall, the comprehensive evaluation for powdered CHMs based on the physical characterization, chemical dissolution, and bioassay could not only be used to evaluate powdered herbs, but also guide the screening and optimization of the particle size of powder.

12 Chemical Constituents from Stems of Cistanches deserticola

Mavis Boakye-Yiadom , Li-feng Han , Wei Li , Yi Zhang , Er-wei Liu , Xin-bo Song , Tao Wang

2016, 8(3):293-296. DOI: 10.1016/S1674-6384(16)60053-9

[Abstract](655) [HTML](0) [PDF 0.00 Byte](14)

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Objective To study the chemical constituents in the stems of Cistanches deserticola. Methods The compounds were purified by various column chromatographic methods and their structures were elucidated by spectroscopic (1D, 2D NMR, IR, [a]D, and MS) and chemical analyses. Results Seven compounds were isolated and identified as kankanoside D1 (1), ajugol (2), cistanin (3), uridine (4), adenosine (5), 6-deoxycatalpol (6), and kankanoside D (7). Conclusion Compound 1 is a new compound.

Volume 8,Issue 3,2016 Table of Contents

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