Volume 5,Issue 2,2013 Table of Contents

1 Recent Advance in Chemical and Biological Studies on Cimicifugeae Pharmaceutical Resources

HAO Da-cheng , GU Xiao-jie , XIAO Pei-gen , LIANG Zhan-guo , XU Li-jia , PENG Yong

2013, 5(2):81-95. DOI: 10.7501/j.issn.1674-6384.2013.02.001

[Abstract](1958) [HTML](0) [PDF 528.04 K](3427)

Abstract:
Cimicifugeae is one of the rich sources for various active components and the health promoting and therapeutic values of the components have been corroborated by long-term use in folk medicine and traditional Chinese medicine. Increasing interest in Cimicifugeae pharmaceutical resources has led to the further discoveries of triterpenoid saponins, phenolic compounds, chromones, and many other compounds in various species of Cimicifugeae, and to the investigations on their chemotaxonomy, molecular phylogeny, and bioactivities. Based on our pharmacophylogenetic studies, the progress in phytochemistry, chemotaxonomy, molecular biology, and phylogeny of Cimicifugeae had been summarized since 2007, especially Cimicifuga L. ex Wernisch. and Actaea L., and their relevance to therapeutic efficacy. An exhaustive literature survey is used to characterize the global scientific effort in the phytochemical and biological studies of Cimicifugeae. More triterpenoid saponins have been found in various species, among which the cimigenol type (type A) is predominant. The versatile bioactivities of saponins and extracts, as well as those of phenolics and other ingredients, were summarized and discussed. The morphology-based five-genus classification of Cimicifugeae is not supported by molecular phylogeny. Molecular phylogeny based on nuclear and chloroplast DNA sequences tends to merge Cimicifuga Wernisch., Souliea Franch., and Actaea L. into a single genus. It is indispensable to integrate the emerging technologies into Cimicifugeae research for both the sustainable utilization of Cimicifugeae pharmaceutical resources and finding novel compounds with potential clinical utility and less adverse effects. Systems biology and omics technologies would play an increasingly important role in booming pharmaceutical research involving bioactive compounds of Cimicifugeae.

2 A Novel Bihomoflavanonol with an Unprecedented Skeleton from Pteridium aquilinum

CHEN Nai-dong , CHEN Nai-fu , CHEN Cun-wu , ZHANG Li

2013, 5(2):96-100. DOI: 10.7501/j.issn.1674-6384.2013.02.002

[Abstract](838) [HTML](0) [PDF 388.63 K](2166)

Abstract:
Objective To seek the flavonoids with the unique structure and to investigate the chemical ingredients in the flavonoid-rich plant—Pteridium aquilinum. Methods The 80% EthOH extract from the degreased powder of P. aquilinum was partitioned by petroleum ether, CHCl3, EtOAc, n-butanol, and water, respectively. The EtOAc fraction was sequentially subjected to silica gel column, repeated Sephadex LH-20 column, and preparative TLC to give a new compound. The antitumor activity of the novel flavonoid was primarily evaluated by MTT. Results Compound 1, a biflavonoid with the unique structure named as pteridium III with an unprecedented bihomoflavanonol skeleton, was isolated from P. aquilinum. Compound 1 showed the in vitro antitumor activity against lung cancer cell NCI-H46, melanoma cell A375, and glioma cell U-7MG corresponding to the IC50 values of 22.9, 106.7, and 1540.5 μmol/L, respectively. No inhibition on gastric carcinoma SGC-7901 and prostatic carcinoma PC-3 was observed in the experiment. Conclusion A rare bihomoflavononol derivative, pteridium III, is obtained from the plant, which could enrich our knowedge on the chemical structures of flavonoids and bioactive constituents in P. aquilinum.

3 A New Prenylated Xanthone from Root Barks of Cudrania cochinchinensis

LIU Zhi-ping , WEI Wan-xing , ZHOU Min , GAN Chun-fang , LIU Sheng

2013, 5(2):101-103. DOI: 10.7501/j.issn.1674-6384.2013.02.003

[Abstract](898) [HTML](0) [PDF 262.40 K](2155)

Abstract:
Objective To study the chemical constituents from the root barks of Cudrania cochinchinensis. Methods The chemical constituents were isolated and purified by silica gel column chromatography. The structures of the compounds were identified on the basis of spectral data (MS, 1H-NMR, 13C-NMR, and 2D NMR) and by the comparison of spectroscopic data with the reported values in the literatures. Results A new xanthone, 1,6,7-trihydroxy-4-(1,1- dimethylallyl)-3-methoxyxanthone (1) and a known prenylated xanthone 1,5,6-trihydroxy-4-(1,1-dimethylallyl)-3- methoxyxanthone (isocudraniaxanthone B, 2) were isolated from the root barks of C. cochinchinensis. Conclusion Compound 1 is a new prenylated xanthone. Isomers 1 and 2 are obtained from this plant for the first time.

4 Chemical Constituents in Essential Oils from Elsholtzia ciliata and Their Antimicrobial Activities

TIAN Guang-hui

2013, 5(2):104-108. DOI: 10.7501/j.issn.1674-6384.2013.02.004

[Abstract](1057) [HTML](0) [PDF 234.99 K](3282)

Abstract:
Objective To compare the chemical constituents in the essential oils from the leaves, flowers, and seeds of Elsholtzia ciliata and their antimicrobial activities. Methods The chemical constituents in essential oils were extracted by the hydro-distillation method and analyzed by GC-MS. The chemical constituents in essential oils were identified on the basis of comparison on their retention indices and MS spectrum with published data. Moreover, the antimicrobial activities of the chemical constituents in the oils against the growth of six bacteria strains and one pathogenic yeast strain were evaluated by using minimum inhibitory concentration and minimum bactericidal concentration methods. Results A total of 58 compounds were identified, while compounds 31, 35, and 36 were identified in the essential oils from the leaves, flowers, and seeds, respectively. Fifteen compounds were identified as shared constituents in the leaves, flowers, and seeds. The chemical constituents in the essential oils showed the inhibitory activities against the six bacteria strains and the yeast strain. Conclusion The major constituents are different in the essential oils of the leaves, flowers, and seeds. The major chemical constituents in the essential oils are monoterpenoids and sesquiterpenoids. And the chemical constituents in the essential oils obtained from the leaves show higher inhibitory activities especially against Bacillus subtillis CMCC63501 and Escherichia coli ATCC25922.

5 Pharmacology and Toxicology of Extract from Arcangelisia gusanlung

HU Hai-zhen , DONG Zhi , ZHU Yi , CHEN Guo-biao

2013, 5(2):109-115. DOI: 10.3969/j.issn.1674-6348.2013.02.005

[Abstract](1000) [HTML](0) [PDF 305.09 K](2729)

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Objective To study the pharmacology and toxicology of the extracts from Arcangelisia gusanlung (EAG). Methods The anti-inflammatory activities were investigated using various inflammatory models including ear edema induced by xylene in mice, paw edema induced by carrageenan, and cotton pellet granuloma in rats. The analgesic effect was observed in hot-plate test and writhing test in mice and the antipyretic effect was observed in rat fever model induced by yeast. The antitussive action was tested in mice by sequential method and expectorant action was evaluated by tracheal excretion of phenol red. The antidiarrhea function was observed on normal intestinal propulsion of mouse model of diarrhea induced by decoction of Sennae Folium. The toxicity was measured by toxicological experiment. Results Each dose of EAG could significantly inhibit the paw edema, cotton pellet granuloma, and intestinal propulsion. EAG significantly reduced writhing times and amount of wet manure. Obvious antipyretic action to fevered rat was observed. EAG obviously increased the tracheal excretion of phenol red and prolonged the latency of cough. No toxic reaction was shown in the observed period, and the maximum tolerance dose of mice was equivalent to 1360 times of common-used dose in human. Conclusion The clinical dosage of EAG is safe, and its anti-inflammatory, analgesia, antipyresis, antitussive, expectorant, and antidiarrhea effects are significant

6 Pharmacokinetics and Tissue Distribution of Orientin from Trollius chinensis in Rabbits

TAN Xiao-hong , QU Cai-hong , WANG Shu-hua , AN Fang

2013, 5(2):116-120. DOI: 10.3969/j.issn.1674-6348.2013.02.006

[Abstract](929) [HTML](0) [PDF 280.14 K](2128)

Abstract:
Objective To study the pharmacokinetics (PK) and tissue distribution of orientin in rabbits. Methods The high-performance liquid chromatography method was developed and validated for the determination of orientin in rabbit plasma and tissues. The PK characteristics of orientin in rabbits were compared by three kinds of administration, iv, im, and ip injection, using 3P97 pharmacokinetic software to examine the PK parameters. Results The elimination half-life (t1/2β) of three kinds of administration was higher than the distribution half-life (t1/2α). The PK of orientin eliminating in rabbit fitted the two compartment model. Orientin was mainly eliminated in rabbit. The distribution of orientin in tissue after iv injection was investigated, and the order of orientin AUC in each group was kidney > liver > lung > spleen > heart > brain. Conclusion Orientin is distributed extensively in tissues such as kidney, liver, and lung. It is difficult for orientin to cross the blood brain barrier.

7 Immunological Effects of Total Flavones from Leaves of Choerospondias axillaris on Mice

LIU Xin-yuan , YANG Yu-mei , HAN Feng , ZHANG Hao-nan , DU Jian-xi , HAO Xin-min

2013, 5(2):121-124. DOI: 10.3969/j.issn.1674-6348.2013.02.007

[Abstract](869) [HTML](0) [PDF 254.72 K](2474)

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Objective To investigate the effect of total flavones from the leaves of Choerospondias axillaris (TFLCA) on the immune function of normal mice and to provide the experimental basis for the reasonable application of C. axillaris. Methods The carbon clearance method, cutaneous delayed hypersensitivity reaction method, serum hemolysin method, and index of immune organs were used to study the effect of TFLCA on the immune function of mice. Results TFLCA could enhance the phagocytic function of mononuclear macrophage and the cutaneous delayed hypersensitivity reaction of mice, and increase the content of hemolysin antibody and the thymus index in mice. Conclusion TFLCA could improve the celiac macrophage activity and specific immunity of mice, and TFLCA, consisting with the total flavones of Choerospondiatis Fructus (TFCF), has the effect on the immune function of mice. So both TFLCA and TFCF have the regulatory effects on the immune function of mice.

8 Anticancer Effects of Zaoxiu Compound Decoction on H22 Mice with Heps

JIANG Yan-qing , ZHANG Wen-yun , YAN Sheng-ying

2013, 5(2):125-128. DOI: 10.3969/j.issn.1674-6348.2013.02.008

[Abstract](1320) [HTML](0) [PDF 422.88 K](2017)

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Objective To investigate the anticancer effects of the Zaoxiu Compound Decoction (ZCD) on H22 mice with Heps and the influence on the construction of H22 cells. Methods With in vivo techniques, the antineoplastic drugs were given to hepatoma H22 model mice which were randomly divided into negative control (physiological saline), positive control (cyclophosphamide), high- and low-dose ZCD groups. After 10-d administration, the pathological examinations of tumor tissue, livers, and kidneys in mice were carried out and the inhibitory rate on tumor was calculated. Results The high- and low-dose ZCD had obvious inhibition on H22 cells. The pathological observation showed that high- and low-dose ZCD had a strong inhibitory effect on H22 cells as well as positive control, with few toxic effects to the livers and kidneys in mice. Conclusion ZCD has the anticancer effect and has no obvious toxic effects on the model mice.

9 Effect of Jiaosanxian on Reducing Blood Lipid

YIN Ai-wu , TIAN Run , ZHAO Jiao

2013, 5(2):129-132. DOI: 10.3969/j.issn.1674-6348.2013.02.009

[Abstract](941) [HTML](0) [PDF 259.36 K](2119)

Abstract:
Objective To investigate the effects of Jiaosanxian (JSX, consisted of stir-baked Hordei Fructus Germinatus- Crataegi Fructus-Massa Fermentata Medicinalis) on reducing blood lipid. Methods The model of hyperlipidemic mice was established by feeding high-fat diet. Kunming mice were randomly divided into six groups: blank, hyperlipidemic, Zhibituo, low-, mid-, and high-dose [100, 200, and 400 mg/(kg·d)] JSX groups, and were continuously ig administered for 28 d. The contents of total cholesterol (TC), triglyceride (TG), low-density lipoprotein cholesterol (LDL-C), and high density lipoprotein cholesterol (HDL-C) in serum and liver and liver index were determined. Results The contents of TC, TG, and LDL-C in serum or liver were decreased significantly but the contents of HDL-C were increased more significantly in the mid- and high-dose JSX groups than those in hyperlipemic group. The weight and liver index were decreased significantly with the dose increasing of JSX. The lipid-decreasing effects were improved with the dose increasing. Conclusion These results suggest that JSX has the significant effects on hyperlipidemia. It could provide the experimental basis for the clinical use of JSX for the treatment of hyperlipidemia.

10 A New Procedure for Separation and Purification of Scutellarin from Erigeron multiradiatus

ZHANG Zhi-feng , LU Lu-yang , LIU Yuan

2013, 5(2):133-137. DOI: 10.3969/j.issn.1674-6348.2013.02.010

[Abstract](1305) [HTML](0) [PDF 264.10 K](2835)

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Objective To establish a new procedure for isolating scutellarin from Erigeron multiradiatus. Methods A proposed method was developed by combining macroporous resins with ODS column. Firstly, E. multiradiatus was extracted by ultrasound with 80% methanol. Preliminary separation was performed on macroporous resin column. The performance and adsorption characteristics of three macroporous resins, D140, D141, and D605, were compared and the enrichment procedure was optimized. Further purification was carried out by medium pressure liquid chromatography (MPLC) with ODS column. Results It was demonstrated that D141 had better extractive effects on scutellarin. The MPLC conditions were optimized as follows: 15% ethanol aqueous as mobile phase with flow rate at 2.5 mL/min. The yield and purity of the isolated scutellarin were 1.20 mg/g and 96.5%, respectively. Conclusion The overall procedure is efficient and low-cost, which is considered suitable for the separation and purification of scutellarin from E. multiradiatus. The results provide the scientific basis for developing and using scutellarin in clinic.

11 Optimization of Jiawei Qing’e Oral Fast Disintegrating Tablets Based on Response Surface-Central Composite Design

ZHANG Wei-ling , WANG Ya-jing , GAO Xiu-mei , GAO Xu , PENG Shu-juan , ZHENG Yin , OKEKE Chukwunweike Ikechukwu

2013, 5(2):138-144. DOI: 10.3969/j.issn.1674-6348.2013.02.011

[Abstract](1551) [HTML](0) [PDF 324.09 K](2995)

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Objective To apply the response surface-central composite design to developing and optimizing the oral fast disintegrating tablets (ODT) formulation for Jiawei Qing’e, a kind of prescription of Chinese herbal medicine. Methods The bitterness of Jiawei Qing’e was masked using Eudragit E-100 by solvent evaporation technique. Response surface approach was applied to investigating the interaction of formulation parameters in optimizing the formulation. The independent variables were Eudragit E-100/drug ratio (X1), amount of disintegrants (X2), and the amount of diluents (X3). The disintegration time (Y1), hardness (Y2), and weight variations of the tablets were characterized. Results The models predicted levels of X1 = 4.63%, X2 = 5.25%, and X3 = 34.33%, for the optimal formulation having a hardness of 3.0 kg with the disintegration time of 30 s within experimental region. The observed response of Y1 = 26.5 s and Y2 = 3.14 kg reasonably agreed with the predicted response. Conclusion Response surface methodology shows the good predictability and reliability in optimizing the formulation. The optimized ODT of Jiawei Qing’e has acceptable taste, rapid disintegrating ability, and good mechanical strength.

12 Seasonal Variation, Microscopic and Chromatographic Analysis of Leaves in Malus hupehensis: A Protocol for Its Quality Control

SHEN Tao , XIANG Lan , REN Dong-mei , WANG Shu-qi , YANG Ming-ren , LOU Hong-xiang

2013, 5(2):145-150. DOI: 10.3969/j.issn.1674-6348.2013.02.012

[Abstract](1364) [HTML](0) [PDF 471.92 K](4195)

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Objective To establish a quality control protocol based on microscopic, TLC, and HPLC methods, and to verify the optimal harvesting time for the leaves of Malus hupehensis (LMH). Methods The LMH were pulverized into powder for microscopic identification or TLC and HPLC analysis after ultrasonic extraction with methanol. Seasonal variations of the phlorizin content and average leaf weight were determined by HPLC analysis and weighing up the leaves collected from May to October. Results Microscopic and macromorphologic characteristics have been described for the leaf identification. A qualitative TLC assay and a quantitative HPLC method have been established for the quality control of LMH. Phlorizin was selected as a reference marker, which resolved at Rf 0.53 in TLC assay and at 14.0 min in HPLC assay. The content of phlorizin decreased gradually from 17.0% in leaves collected in May to 7.5% in October. The average leaf weight reached the level of 0.6 g in August and maintained until its falling. Conclusion These methods are simple, selective, accurate, and reliable for the quality control of LMH. The period from late August to early September is suggested as the optimal harvesting time of the LMH.

13 Effects of Postharvest Processing and Geographical Source on Phytochemical Variation of Corydalis Rhizoma

ZHAO Yun-peng , LI Jing-hui , YANG Shu-ting , FAN Jie , FU Cheng-xin

2013, 5(2):151-157. DOI: 10.3969/j.issn.1674-6348.2013.02.013

[Abstract](1350) [HTML](0) [PDF 298.98 K](2312)

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Objective To assess the relative contributions of postharvest processing and geographical source to phytochemical variation of Corydalis Rhizoma, and rhizome of Corydalis yanhusuo, and to examine what phytochemical components are the most sensitive to the differences of each factor and how they change. Methods HPLC fingerprinting and LC-MS coupled with chemometric approaches were applied. Results The results of principal component analysis (PCA) and hierarchical cluster analysis (HCA) explicitly demonstrated the postharvest processing could produce a greater impact on the phytochemical profiles of Corydalis Rhizoma than geographical source. The contents of most compounds increased after water boiling while decreased after sulphur-fumigation. Protopine, coptisine, and palmatine were the most variable components in processing. Geographical sources also led to a remarkable phytochemical differentiation, in which the environmental variation of the three regions might play a role. Dehydrocorybulbine, coptisine, dehydrocorydaline, and protopine varied most among the three production regions and decreased sequentially in Zhejiang, Shaanxi, and Jiangsu provinces, China. Conclusion Both postharvest processing and geographical source should be enhanced with the priority for the former in the quality control of Corydalis Rhizoma. The application of boiling is supported but the consistency should be improved in practice. Sulphur-fumigation is strongly suggested to be abandoned.

14 Preparation and Crystal Structure of Acetyl Hemerocallin and Structural Revision of Hemerocallin

LIU Yan-ze , WU Jie , ZHU Yu , DU Chen-xia , CHANG Jun-biao , XIE Jing-xi

2013, 5(2):158-162. DOI: 10.3969/j.issn.1674-6348.2013.02.014

[Abstract](1062) [HTML](0) [PDF 338.77 K](2059)

Abstract:
Objective To revise the structure of hemerocallin, an active and toxic compound isolated from the roots of Hemerocallis fulva, which was first reported in 1974 based on the chemical and spectral data. Methods The structure of acetyl hemerocallin was determined through the acetyl derivative preparing and X-ray diffraction. Results The title compound acetyl hemerocallin (1) has been prepared and structurally characterized by X-ray single-crystal diffraction method. X-ray analysis revealed that the two naphthalene rings in compound 1 were significantly twisted with an average dihedral angle of 44.1°. The two acetate groups in each naphthalene ring adopted anti-parallel conformation. In addition, the π-π stacking interactions were found in the crystal structure, the molecules were linked into a supramolecular network, and the crystal structure was stabilized. Conclusion The structure of hemerocallin is identified as 2,2′-bi(1,8-dihydroxy-6-methyl-7-acetylnaphthalene) (3)

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