Volume 4,Issue 3,2012 Table of Contents

1 New Collection of Crude Drugs in Chinese Pharmacopoeia 2010 III. Kadsurae Caulis

XU Li-jia , MA Pei , LI Li , WANG Wan-ying , XIAO Wei , PENG Yong , XIAO Pei-gen

2012, 4(3):177-182. DOI: 10.3969/j.issn.1674-6384.2012.03.001

[Abstract](1239) [HTML](0) [PDF 314.58 K](3410)

Abstract:
The dried cane of Kadsura interior (Kadsurae Caulis) is recorded in Chinese Pharmacopoeia 2010 as Dian Jixueteng for the treatment of rheumatism, irregular menstruation, and deficiency of Qi and blood. In this paper, morphological characteristics, chemical constituents, and pharmacological activities in the cane of K. interior were summarized. Moreover, some suggestions about application and quality control of Kadsurae Caulis were proposed in order to provide a theoretical basis for further scientific use.

2 Triterpene Glycosides from Sea Cucumber Holothuria scabra with Cytotoxic Activity

HAN Hua , LI Ling , YI Yang-hua , WANG Xiao-hua , PAN Min-xiang

2012, 4(3):183-188. DOI: 10.3969/j.issn.1674-6384.2012.03.002

[Abstract](1841) [HTML](0) [PDF 330.97 K](3925)

Abstract:
Objective To study the new triterpene glycosides from sea cucumber Holothuria scabra with cytotoxic activity. Methods Triterpene glycosides from H. scabra were separated and purified by chromatography on DA-101, silica gel, and reversed-phase silica gel column, as well as RP-HPLC. Their structures were elucidated on the basis of spectral data and chemical evidence. Results Three triterpene glycosides were identified as scabraside D (1), fuscocineroside C (2), and 24-dehydroechinoside A (3). Their inhibition on P-388, A549, MKN-28, HCT116, and MCF-7 cells were significant. Conclusion Scabraside D (1) is a new triterpene glycoside, and compounds 2 and 3 are isolated from H. scabra for the first time. The glycosides 1－3 show the in vitro cytotoxicity against five human tumor cell lines in comparison to 10-hydroxycamptothecin.

3 Inhibition of Ptychopetalum olacoides on Acetylcholinesterase Isoforms in Brain of Mice

FIGUEIRó Micheli , POCHMANN Daniela , PORCIúNCULA Lisiane Oliveira , NUNES Domingos Sávio , ELISABESTKY Elaine

2012, 4(3):189-194. DOI: 10.3969/j.issn.1674-6384.2012.03.003

[Abstract](1224) [HTML](0) [PDF 278.38 K](2712)

Abstract:
Objective To further characterize the acetylcholinesterase inhibitors (AChE-Is) pattern of Ptychopetalum olacoides ethanol extract (POEE) on the cytosolic globular monomer (G1) and membrane bound globular tetramer (G4) AChE isoforms in brain areas relevant for cognition. Methods The G1 and G4 AChE isoforms were prepared according to the reported methods and the determination of AChE activity used was adapted from colorimetric method. Results POEE mostly inhibited G1 in hippocampus (75%), and G4 in frontal cortex (58%) and striatum (75%) (P < 0.05). Kinetic analysis indicated that POEE-induced AChE inhibition in hippocampus was of a competitive nature for G1 but uncompetitive for G4. Conclusion Considering the high density of cholinergic projection to the cortex and striatum, and the usefulness of conserving cytosolic acetylcholine to replenish synaptic vesicles in a highly active cognition site such as hippocampus, we argue that this could be a desirable profile for a clinically relevant AChE-I.

4 Neuroprotection of n-Butanol Extract from Roots of Potentilla anserina on Hypoxic Injury in Primary Hippocampal Neurons

QIN Xiao-jing , LI Ling-zhi , LV Qi , YU Bao-guo , YANG Shu-wang , HE Tao , ZHANG Yong-liang

2012, 4(3):195-200. DOI: 10.3969/j.issn.1674-6384.2012.03.004

[Abstract](1236) [HTML](0) [PDF 281.89 K](2291)

Abstract:
Objective To investigate the protective effect of n-butanol extract from the roots of Potentilla anserina (NP) on hypoxic hippocampal neurons in neonatal rats. Methods Primary cultured hippocampal neurons were pretreated with different concentration of NP (0.25, 0.0625, and 0.0156 mg/mL) before incubation in a low oxygen (0.1%) environment for 4 h. Cell viability was evaluated by Trypan blue staining assay. Lactate dehydrogenase (LDH) released by neurons into the medium was measured. The activity of superoxide dismutase (SOD) in cell cytosol was determined using nitroblue tetrazolium. Morphological changes and mitochondrial function were observed by transmission electron microscopy. Results Hypoxic injury could decrease the cells viability of neuron, enhance LDH release (P < 0.05), decrease SOD activity, and increase mitochondrial injury. Pretreatment with NP significantly increased cell viability, decreased LDH release (P < 0.05), promoted SOD activity (P < 0.05), and remarkably improved cellular ultra-microstructure compared with the model group. Conclusion NP could protect the primary hippocampal neurons from hypoxic injury by attenuating mitochondrial cell death.

5 Effects of Two Curcuminoids on Candida albicans

ZHANG Da , LUO Jiao-yang , YAN Dan , JIN Cheng , DONG Xiao-ping , XIAO Xiao-he

2012, 4(3):205-212. DOI: 10.3969/j.issn.1674-6384.2012.03.006

[Abstract](1355) [HTML](0) [PDF 293.06 K](2296)

Abstract:
Objective To investigate and compare the action of curcuminoids on the causal pathogens of Candida albicans growth. Methods The effects of curcumin (CUR) and demethoxycurcumin (DMC) on C. albicans growth were first investigated and compared by microcalorimetry coupled with multiple analytical methods. The quantitative thermo-kinetic parameters obtained from these curves were analyzed to show difference of the actions. Results By analyzing the main parameters screened from principal component analysis together with 50% inhibiting concentration values, it was demonstrated that both CUR and DMC showed good antifungal activities and CUR was stronger. It was further concluded from structure-activity relationship that the existence of methoxy group might enhance lipophilicity of the mother nucleus, which made it easier for the molecular to enter into the cell membrane of fungi to inhibit its growth. Conclusion This study provides a new method for screening new antifungal agents with high efficacy and low toxicity. Meanwhile, it contributes to the application of curcuminoids as food additive, colorant, and drug. Microcalorimetry is real-time, online, and dynamic, and it could be used to characterize the subtle difference among the effects of synthetic and natural products on the vital process of fungi.

6 Pharmacokinetic Study on Hyperoside in Beagle’s Dogs

AI Guo , HUANG Zheng-ming , LIU Chang-xiao

2012, 4(3):213-217. DOI: 10.3969/j.issn.1674-6384.2012.03.007

[Abstract](996) [HTML](0) [PDF 184.98 K](3072)

Abstract:
Objective To develop and validate a simple, rapid, sensitive, and reproducible HPLC method for determination of hyperoside in plasma of dogs and for the subsequent pharmacokinetic (PK) study. Methods An accurate and reproducible HPLC-UV method was developed and validated for the determination of hyperoside in plasma of dogs, using kaempferol as internal standard. The plasma samples of dogs following ig administration of hyperoside were analyzed for the detection of quercetin after enzymatic hydrolysis treatment with combined β-glucuronidase and sulphatase. The analytes were separated on a Diamonsil C18 column (250 mm × 4.6 mm, 5 μm). The mobile phase consisted of methanol-buffer solution (0.1 mol/L NH4Ac + 0.3 mmol/L EDTA-Na2)-acetic acid (60:40:1) and was delivered at a flow rate of 1 mL/min. The UV detector was set at 370 nm and the column temperature was maintained at 35 ℃. The sample injection volume was 20 μL. Data were collected and analyzed using the ANASTAR software. PK parameters were calculated with DAS software (2.0). Results Linear relationships were validated over the range of 0.01－1 μg/mL for hyperoside (r = 0.9997). The intra- and inter-day precision values for all samples were within 10.0%, and the accuracies of intra- and inter-day assays were within the range of 92.4%－102.4%. The validated method was successfully used to determine the hyperoside concentration in plasma of dogs for up to 12 h, after a single ig administration (25 mg/kg). The mean PK parameters for male and female dogs were as follows: Cmax (0.18 ± 0.05) and (0.16 ± 0.05) μg/mL, AUC0-∞ (0.79 ± 0.34) and (0.86 ± 0.27) μg/(mL?h), t1/2(ka) (0.89 ± 0.41) and (0.88 ± 0.28) h, respectively. Statistical analysis on the PK of hyperoside in male and female groups showed that sex had no significant impact on the PK of hyperoside (P > 0.05). Conclusion The method is able and sufficient to be used in drug PK studies of hyperoside.

7 Inhibition of Aloperine on Dextran Sulphate Sodium-induced Chronic Colitis in C57BL/6 Mice

SONG Li-jun , ZHAO Wen-chang , DENG Hong-zhu

2012, 4(3):218-223. DOI: 10.3969/j.issn.1674-6384.2012.03.008

[Abstract](1070) [HTML](0) [PDF 350.19 K](2326)

Abstract:
Objective To investigate the effects of aloperine (ALO) on a model of dextran sulphate sodium (DSS)-induced chronic colitis in C57BL/6 mice. Methods Repeated colitis was induced by administration of four cycles of 4% DSS. The severity of colitis was assessed on the basis of clinical signs, ratio of colon weight and colon length, and histological grading scores. Moreover, secretory immunoglobulin A (S-IgA) and plasma haptoglobin (HP) were analyzed by enzyme-linked immunosorbent assay, and the changes of mRNA expression of ICAM-1 and MIF gene in colorectal tissue were detected by quantitative reverse transcriptase real-time polymerase chain reaction using SYBR Green I. Results ALO administration significantly attenuated the colon damage, caused substantial reductions of the rise in HP, and maintained the level of cecum S-IgA. ALO inhibited the ICAM-1 mRNA expression and had no effect on MIF mRNA expression. Conclusion The effect of ALO on DSS-induced chronic colitis in mice is investigated for the first time, which suggests that ALO could be an attractive therapeutic candidate in the treatment of inflammatory bowel disease.

8 Physicochemical Properties and Gastric Mucosa Irritation of Cantharidin-hydroxypropyl-β-cyclodextrin Inclusion Complex

AN Lin-na , DANG Yun-jie , HU Chun-hui , ZHU Chun-yan

2012, 4(3):224-229. DOI: 10.3969/j.issn.1674-6384.2012.03.009

[Abstract](1413) [HTML](0) [PDF 358.14 K](2855)

Abstract:
Objective To increase the solubility and relieve the mucous irritation of cantharidin (CA) by preparing cantharidin-hydroxypropyl-β-cyclodextrin (CA/HP-β-CD) inclusion complex. Methods The inclusion complex was prepared by co-evaporation method and characterized by differential scanning calorimetry (DSC), X-ray diffractometry (XRD), and nuclear magnetic resonance (NMR). Results The disappearance of CA as well as the shift of exothermic peaks shown in DSC results indicated the complexation phenomenon. XRD results showed that the crystalline CA pattern had disappeared, and in NMR results, H-5 shifted from δ 3.731 to 3.695 after complexation and H-2 shifted from δ 3.626 to 3.598, which suggested that part of the drug had entered the HP-β-CD cavity to form an inclusion complex. The solubility increased 10.3 times after complexation and the mucous irritation of CA was relieved remarkably. Conclusion Through complexation with HP-β-CD, the solubility and dissolution rate of CA are improved significantly, and the irritation of musous is relieved.

9 Simultaneous Determination of Seven Alkaloids in Fufang Zhenzhu Tiaozhi Capsule by HPLC Coupled with DAD

CHEN Yuan-yuan , GUO Jiao , FAN Hui , HUANG Li-hua

2012, 4(3):230-236. DOI: 10.3969/j.issn.1674-6384.2012.03.010

[Abstract](1074) [HTML](0) [PDF 222.37 K](2253)

Abstract:
Objective To establish a reverse-phase liquid chromatography method for the determination of seven alkaloids (magnoflorine, columbamine, jatrorrhizine, epiberberine, coptisine, palmatine, and berberine) in Fufang Zhenzhu Tiaozhi Capsule. Methods Chromatography was performed on a Dionex Acclaim C18 column (250 mm × 4.6 mm, 5.0 μm) at 30 ℃. The mobile phase was composed of acetonitrile-potassium dihydrogen phosphate solution (0.015 mol/L, 40:60, including 1.7 g/L sodium dodecyl sulfate and phosphoric acid used to regulate pH value to 3.0), with a flow rate of 1.0 mL/min. The detection wavelength was 270 nm. Results The calibration curves of magnoflorine, columbamine, jatrorrhizine, epiberberine, coptisine, palmatine, and berberine were linear in the range of 1.07－10.65, 0.78－7.55, 0.75－7.50, 1.60－15.95, 2.69－26.85, 2.31－23.10, and 6.04－60.40 mg/mL. The average recoveries of magnoflorine, columbamine, jatrorrhizine, epiberberine, coptisine, palmatine, and berberine were 101.0%, 101.2%, 100.1%, 100.0%, 100.1%, 101.1%, and 99.7%, respectively. Conclusion The method could be used for the quantitative determination of the preparation.

10 Standardization and Identification of Minor Components of Silymarin (MK-001)

LIU Yan-ze , LEE David Yue-wei

2012, 4(3):237-244. DOI: 10.3969/j.issn.1674-6384.2012.03.011

[Abstract](1082) [HTML](0) [PDF 269.75 K](2340)

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Objective To develop a highly effective HPLC method for standardization of silymarin and for characterization of minor components, which has not been reported previously. Methods An HPLC fingerprinting method and 1H-NMR spectroscopy were employed to provide assurance for a standardized silymarin product (MK-001). Results A total of 18 marker compounds were identified and characterized including ten flavonolignans and eight small molecules including adenine, adenosine, uridine, and 3,5,7-trihydroxychromone which were first isolated and characterized from silymarin. The HPLC fingerprinting method and 1H-NMR had been established for complete assignments of HPLC peaks with intensity over 1.0%. Conclusion The successfully established HPLC fingerprinting method and 1H-NMR could be applied for the standardization of commercial silymarin products. MK-001 represents the first standardized silymarin with the highest content of flavonolignans ( > 90%).

11 HPLC Fingerprint and LC-TOF-MS Analysis on Extract from Roots of Gentiana macrophylla

SU Qi , SHANG Ping-ping , ZHANG Yong-min , JIA Na , HE Jiao , ZHAO Wen-na , SUN Wen-ji

2012, 4(3):245-251. DOI: 10.3969/j.issn.1674-6384.2012.03.012

[Abstract](2857) [HTML](0) [PDF 221.06 K](11293)

Abstract:
Objective Establishing a ?ngerprint method to identify the characteristic chemicals in the roots of Gentiana macrophylla and evaluate their quality. Methods RP-HPLC was developed for ?ngerprint analysis and determination of four ingredients in G. macrophylla roots from different sources. LC-ESI-TOF-MS was employed to identify the chromatographic peaks of the ?ngerprint. Results Five common peaks were identified by comparing their retention time with reference secoiridoid glucosides. Eight major peaks in chromatographic fingerprint were analyzed by on-line LC-ESI-TOF-MS. Four secoiridoid glucosides were identified based on their MS data. Conclusion The method is specific and could be served for the quality identi?cation and comprehensive evaluation of G. macrophylla.

12 Simultaneous Determination of Seven Flavonoids in Aerial Parts of Artemisia frigida by HPLC

WANG Qing-hu , AO Wu-li-ji , TAI Wen-quan

2012, 4(3):252-258. DOI: 10.3969/j.issn.1674-6384.2012.03.013

[Abstract](1098) [HTML](0) [PDF 210.37 K](1899)

Abstract:
Objective To establish an HPLC method for the determination of seven flavonoids from the aerial part of Artemisia frigida. Methods Hypersil ODS-2 (300 mm × 4.6 mm, 5 μm) column was used, with acetonitril-0.2% phosphoric acid (gradient elution) as a mobile phase, and the detection wavelength was at 283 nm with flow rate at 1 mL/min. Results All calibration curves showed good linear regression (r > 0.9990) within the tested range. All average recovery was more than 98.00% and RSD was less than 3.0% (n = 6). Conclusion The method is steady and with good repeatability, and could be used to determine the content of flavonoids in A. frigida from different areas.

13 Optimization of Smashing Tissue Extraction Technology of Schisandra chinensis Fruits by Orthogonal Test

TANG Yun , LIU Yan-ze , HAN Ling , ZHAO Yu-qing

2012, 4(3):259-262. DOI: 10.3969/j.issn.1674-6384.2012.03.014

[Abstract](1112) [HTML](0) [PDF 133.73 K](2405)

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Objective To optimize the extract technology of active lignins from the fruits of Schisandra chinensis. Methods The content of schizandrin, gomisin A, and deoxyschizandrin were selected as standards to evaluate the efficiency of smashing tissue extraction (STE). Solid-liquid ratio, extracting times, ethanol concentration, and extracting time were investigated through orthogonal test. Results The optimized conditions for STE were ten times amount of 80% EtOH, extracting for three times, and 2 min for each time. Conclusion STE could obtain relatively higher yield, simplicity of operation, and benefit for environment protection. It could be better choice for the extraction of S. chinensis.

Volume 4,Issue 3,2012 Table of Contents

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