Volume 4,Issue 2,2012 Table of Contents

  • Display Type:
  • Text List
  • Abstract List
  • 1  A New Phenylpropanol Glycoside from Twigs and Leaves of Rhododendron primulaeflorum
    ZHOU Xian-li WU Nai-zhu HUANG Shuai WANG Cui-juan WANG You-song ZHANG Yu
    2012, 4(2):81-83. DOI: 10.3969/j.issn.1674-6384.2012.02.001
    [Abstract](1157) [HTML](0) [PDF 260.68 K](2543)
    Abstract:
    Objective To study the constituents in the twigs and leaves of Rhododendron primulaeflorum. Methods The constituents were separated and purified with chromatographic methods. Their structures were elucidated by spectroscopic methods (1D, 2D NMR, IR, and HR-ESI-MS) and chemical analyses. Results One new phenylpropanol glycoside, 4-hydroxyl-5-methoxyl-phenylpropanol-3-O-β-D-glucopyranoside (1), and its aglycone (2) were successfully isolated from the twigs and leaves of R. primulaeflorum. Conclusion Compound 1 is a new phenylpropanol glycoside. Compounds 1 and 2 are isolated from this plant for the first time.
    2  A New Triterpenoid Saponin from Aidi Injection
    ZHANG Miao-miao LIU Yan-li CHEN Zhong LI Xiao-ran XU Qiong-ming YANG Shi-lin
    2012, 4(2):84-86. DOI: 10.3969/j.issn.1674-6384.2012.021.002
    [Abstract](1775) [HTML](0) [PDF 176.69 K](4098)
    Abstract:
    Objective To investigate the chemical constituents from Aidi Injection. Methods The chemical constituents were isolated by chromatography on Sephadex LH-20 gel columns and reverse phase semi-preparative HPLC repeatedly. Their structures were identified by spectroscopic analysis (NMR and MS). Results Twenty-two compounds were isolated and identified to be 3-O-3′,4′-diacetyl-β-D-xylopyranosyl-6-O-β-D-glucopyranosyl- cycloastragenol (1), astragaloside IV (2), astragaloside II (3), astragaloside I (4), isoastragaloside I (5), acetylastragaloside I (6), ginsenosid Re (7), ginsenoside Rf (8), ginsenoside Rg1 (9), ginsenoside Rb3 (10), notoginsenoside R4 (11), ginsenoside Rb1 (12), ginsenoside Rc (13), ginsenoside Rb2 (14), ginsenoside Rd (15), lucyoside H (16), 3-O-β-D-glucopyranosyl(1→4)-β-D-glucopyranosyl(1→3)-α-L-rhamnopyranosyl (1→2)-α-L- arabinopyranosyl oleanolic acid 28-O-α-L-rhamnopyranosyl(1→4)-β-D-glucopyranosyl(1→6)-β-D-glucopyranoside (17), 3-O-β-D-glucopyranosyl(1→3)-α-L-rhamnopyranosyl [β-D-glucopyranosyl-(1→4)]-(1→2)-α-L-arabinopyranosyl oleanolic acid 28-O-α-L-arabinopyranosyl(1→4)-β-D-glucopyranosyl(1→6)-β-D-glucopyranoside (18), syringin (19), elentheroside E (20), 4-(1,2,3-trihydroxypropyl)-2,6-dimethoxyphenyl-1-O-β-D-glucopyranoside (21), and coniferin (22). Conclusion Compounds 1-6 are originated from Astragalus membranceus, compounds 7-18 are originated from Panax ginseng, and compounds 19-22 are originated from Acanthopanax senticosus by LC-MS analysis. Compound 1 is a new compound.
    3  Advances in Isolation and Synthesis of Xanthone Derivatives
    YANG Chun-hui MA Li WEI Zhen-ping HAN Feng GAO Jing
    2012, 4(2):87-102. DOI: 10.3969/j.issn.1674-6384.2012.02.003
    [Abstract](1572) [HTML](0) [PDF 620.56 K](5077)
    Abstract:
    Xanthone and its derivatives occupy a large part of the family of natural polyphenolic compounds with various biological and pharmacological activities. In recent years (from 2006 to 2011), it was reported that 127 xanthones were discovered from plants and fungi using various modern separation methods including silica gel/polyamide column chromatography, HPLC, high-speed counter-current chromatography, high-performance centrifugal partition chromatography, etc. Since total synthesis and structure modification for xanthone and its derivatives have been given attention worldwide, we introduced the synthetic methods of xanthone skeletons as well. Unfortunately, to date, there are still weaknesses in current methods of separation and synthesis, which need to be improved. This review, to a certain extent, provides necessary foundation for the further research and development of medicines containing xanthone and its derivatives.
    4  Phytochemicals and Their Biological Activities of Plants in Tagetes L.
    XU Li-wei CHEN Juan QI Huan-yang SHI Yan-ping
    2012, 4(2):103-117. DOI: 10.3969/j.issn.1674-6384.2012.02.004
    [Abstract](1811) [HTML](0) [PDF 347.10 K](5200)
    Abstract:
    Tagetes L., the genus in the family Asteraceae, consists of about 30 species spread in South and Middle America as well as Mexico. More than one hundred secondary metabolites have been obtained in phytochemical investigation on the species, some of which have potent biological activities. The advances in phytochemical studies and biological activities of the plants in Tagetes L. from 1925 to 2011 are summarized in this paper.
    5  In vitro Metabolism of Strychnine by Human Cytochrome P450 and Its Interaction with Glycyrrhetic Acid
    LIU Li XIAO Juan PENG Zhi-hong WU Wen-hua DU Peng CHEN Yong
    2012, 4(2):118-125. DOI: 10.3969/j.issn.1674-6384.2012.02.005
    [Abstract](1353) [HTML](0) [PDF 359.84 K](3330)
    Abstract:
    Objective To investigate the metabolism of strychnine (STN) and the metabolic interaction between STN and glycyrrhetic acid (GA) in vitro. Methods Human liver microsomes (HLM) and human recombinant cytochrome P450 (CYP) isoforms were employed to study the metabolism of STN and the metabolic interaction of STN with GA in vitro. Results In HLM, the Km, Vmax, and clearance of STN were 88.50 μmol/L, 0.88 nmol/(mg?min), and 9.93 mL/(mg?min), respectively. STN was metabolized mainly by CYP3A4. However, STN noncompetitively inhibited CYP3A4-catalyzed testosterone 6β-hydroxylation with IC50 value of 5.9 μmol/L and Ki value of 5.5 μmol/L. Moreover, GA competitively inhibited STN metabolism with IC50 value of 10.6 μmol/L and Ki value of 17.7 μmol/L. Conclusion Although STN is mainly metabolized by CYP3A4 in vitro, STN has noncompetitive inhibition on CYP3A4-catalyzed testosterone 6β-hydroxylation. Moreover, GA could competitively inhibit STN metabolism. The present work is helpful to elucidate the metabolic interaction between STN and GA.
    6  Antihepatocarcinoma Effect of Solanine and Its Mechanisms
    JI Yu-bin GAO Shi-yong
    2012, 4(2):126-135. DOI: 10.3969/j.issn.1674-6384.2012.02.006
    [Abstract](1425) [HTML](0) [PDF 499.56 K](3005)
    Abstract:
    Objective To explore the antitumor effect of solanine and its mechanisms. Methods The in vivo antitumor effect of solanine was observed using models developed through in vivo transplantation of tumor cells; In vitro lines of sensitive antitumor cells were selected from the digestive system using MTT assay; The effect of solanine on cell morphology was observed using transmission electronic microscopy; The morphology of apoptotic cells was observed using Annexin V/PI double staining and laser confocal scanning microscopy (LCSM); The rate of cell apoptosis was measured using Annexin V/PI double staining and flow cytometry; The concentration of intracellular Ca2+ ([Ca2+]i) was determined using Fluo-3/AM staining and LCSM; The membrane potential of cellular mitochondria was determined using TMRE staining and LCSM; The protein expression of Bcl-2 and Bax was measured using immunological marking and LCSM; And the activity of caspase-3 was measured using the colorimetric method. Results Solanine could inhibit the growth of tumor weight in S180 tumor-bearing mice and prolong the survival time of H22 tumor-bearing mice. MTT assay revealed that HepG2 cells were quite sensitive to solanine because solanine could induce morphological changes in HepG2 cells, with the rate of early apoptosis being 4%, 8.5%, and 20.1%, for HepG2 cells treated for 24 h with solanine at concentration of 0.4, 2, and 10 μg/mL, respectively. Solanine could raise the [Ca2+]i and lower the membrane potential. It could reduce the protein expression of Bcl-2 while increase that of Bax, thus increasing the activity of caspase-3. Conclusion The obvious antitumor activity of solanine in human hepatocarcinoma is demonstrated. This inhibitory effect is achieved through solanine decreasing the Bcl-2/Bax ratio, thus increasing [Ca2+]i, which could enhance the enzymatic activity of the caspase family, thus inducing the apoptosis of HepG2 cells.
    7  Effects of Total Alkaloids in Buxus microphylla Leaves on Aorta Smooth Muscle of Rats and Their Mechanisms
    ZHANG Hui-qin LIU Yan-yan LI Yong-wen LI Li CUI Zhi-qing
    2012, 4(2):136-141. DOI: 10.3969/j.issn.1674-6384.2012.02.007
    [Abstract](1238) [HTML](0) [PDF 166.48 K](2163)
    Abstract:
    Objective To investigate the effects of total alkaloids in Buxus microphylla leaves (ABML) on isolated rats thoracic aorta rings, and then to explore the possible mechanisms underlying the effects. Methods Thoracic aortas of Wistar rats were isolated, removed, and mounted onto an organ bath. The effects of ABML at different concentration on the contraction of isolated thoracic aorta rings (with and without endothelium) precontracted with KCl or PE were observed with organ bath technique. Dose-effect curves of CaCl2 were recorded by organ bath technique. The concentration of intracellular Ca2+ ([Ca2+]i) increased by PE, KCI, and caffeine in the presence of ABML was determined using Ca2+ sensitive fluorescence indicator Fura-2/AM loaded thoracic aorta vascular smooth muscle (VSM) cells of rats. Results In aorta rings precontracted with PE and KCl, ABML produced concentration- dependent relaxation in both intact and denuded endothelium ring groups. There was no difference in the inhibition of contraction between the intact and denuded endothelium ring groups at the same concentration. Exposure of isolated thoracic aorta rings to ABML led to a significant reduction in the contracting response induced by CaCl2, and shifted the cumulative concentration-response curves to right. ABML could significantly inhibit the extracellular Ca2+ influx induced by PE and KCl under [Ca2+]0 of 1.5 mmol/L, with inhibitory ratios of 40.2% and 49.9%, respectively. In the case of Ca2+-free, ABML could significantly inhibit the intracellular Ca2+ release induced by PE, with inhibitory ratio of 72.4%. Conclusion ABML relaxes thoracic aorta VSM cells by suppressing influx of extracellular Ca2+ via voltage-dependent Ca2+ channel and receptor-operated Ca2+ channel.
    8  Effect of n-butanol Extract from Potentilla anserina on Hypoxia- induced Calcium Overload and SERCA2 Expression of Rat Cardiomyocytes
    LI Ling-zhi WANG Lu-jun WANG Yue CUI Ying LI Jian-yu ZHANG Li ZHANG Yong-liang
    2012, 4(2):142-149. DOI: 10.3969/j.issn.1674-6384.2012.02.008
    [Abstract](1284) [HTML](0) [PDF 541.86 K](2695)
    Abstract:
    Objective To investigate the effect of n-butanol extract from Potentilla anserina (NP) intervention on hypoxia-induced Ca2+ overload and SERCA2 expression of rat cardiomyocytes. Methods Primary cultured myocardial cell from SD neonatal rat (1-3 d) was used in the establishment of hypoxia model. After hypoxia for 3 h, the Ca2+ concentration of myocardial cells was measured with fura-2/AM fluorescent probe, and the biochemical indicator intracellular Ca2+-ATPase was examined and the mRNA and its protective protein levels of the sarcoplasmic reticulum (SR) Ca2+-ATPases (SERCA2) were assayed with RT-PCR, Western-blotting, and immune-cytochemical staining in each group. Results The results showed that NP decreased Ca2+ concentration, increased the activity of Ca2+-ATPase, and improved the mRNA and protein expression of SERCA2 in hypoxia-injured myocardial cells as compared with the model group. Conclusion These results indicate that NP could attenuate the Ca2+ overload. The mechanism might be explained as that NP could elevate the SERCA2 level, increase the activity of myocardium in rats, and further enhance the capacity of SR Ca2+ re-uptake.
    9  Rational Daily Administration Times of Yinchenhao Decoction in Rats with Jaundice Based on PD/PK
    LV Jun-lan JIN Shi-ying YUAN Hai-long HAN Jin FU Shan-shan JIN Shi-xiao GUO Jing-jing XIAO Xiao-he
    2012, 4(2):150-156. DOI: 10.3969/j.issn.1674-6384.2012.02.009
    [Abstract](1194) [HTML](0) [PDF 165.88 K](2665)
    Abstract:
    Objective To study the rational daily administration times of Yinchenhao Decoction (YCHD) when it was used to treat experimental jaundice in rats based on pharmacodynamics/pharmacokinetics model. Methods Rats were modeled by 4% 1-naphthylisothiocyanate (75 mg/kg) for 48 h, then YCHD was drenched with doses of 0.324 g/kg (extract, calculated with the clinical dosage) once, 0.162 g/kg twice, and 0.108 g/kg thrice a day, respectively. The total bile and the flow rate of bile were observed after the first administration; Blood samples collected from the orbital sinus at different intervals were used to investigate the levels of liver enzymes (ALT and AST) and bilirubins (TBIL and DBIL), and determine the concentration of 6,7-dimethoxycoumarin (DME) in the plasma using UPLC at the same time, then we obtained the time-effect and time-dose curves. The rational daily administration times of YCHD when treating experimental jaundice were determined based on the comprehensive analysis of time-effect and time-concentration relationships. Results Within 10 h the total bile of rats which were administered once daily (G1) was 1.65 and 1.33 times higher than that of twice and thrice (G2 and G3) a day, respectively, and the four biochemical indexes (TBIL, ALT, DBIL, and AST) of G1 decreased faster than those of G2 and G3 (P < 0.05). On the other hand, the blood drug level of DME when administrated once daily could maintain at a higher level for a longer time, and its Cmax and AUC0→t were higher than those of G2 and G3, which might be the main reason why its effect was the most significant. Conclusion It is more appropriate to administrate once daily when YCHD is used to treat jaundice.
    10  A Quantitative Method for Simultaneous Determination of Four Anthraquinones with One Marker in Rhei Radix et Rhizoma
    ZHU Jing-jing WANG Zhi-min MA Xin-yu FENG Wei-hong ZHANG Qi-wei
    2012, 4(2):157-163. DOI: 10.3969/j.issn.1674-6384.2012.02.010
    [Abstract](1865) [HTML](0) [PDF 196.87 K](3663)
    Abstract:
    Objective To develop a quantitative method for simultaneously determining multi-components in Rhei Radix et Rhizoma using one chemical reference substance. Methods The contents of multi-components were calculated by the UV relative correction factors (RCFs) of chrysophanol, physcion, and rhein to emodin. Results The values of RCFs at 274 nm for rhein, chrysophanol, and physcion to emodin were 0.712, 0.674, and 1.051. The calibration curves were linear over the ranges of 0.02-4.08, 0.02-4.12, 0.07-12.92, and 0.02-3.68 μg/mL for rhein, emodin, chrysophanol, and physcion, respectively. The contents of emodin in 18 samples were determined by the external standard method, and the contents of the other three anthraquinone aglycones were calculated according to their RCFs. Conclusion No significant difference is found in comparison with the classical method, indicating that the RCFs have high reliability within their linear ranges and could be used in quality control of Rhei Radix et Rhizoma. The quantitative analysis of multi-component with a single marker is especially suitable for herbal medicines containing unstable or hard to be purified components as quality control markers.
    11  Simultaneous Determination of Six Quaternary Ammonium Alkaloids in Coptidis Rhizoma by UPLC
    QIU Ling-ling CHEN Long-hu YAN Dan ZHANG Ping TAN Man-rong DU Xiao-xi XIAO Xiao-he
    2012, 4(2):164-169. DOI: 10.3969/j.issn.1674-6384.2012.02.011
    [Abstract](1177) [HTML](0) [PDF 222.95 K](2934)
    Abstract:
    Objective To establish a new, rapid, and reliable reversed-phase ultra performance liquid chromatography (RP-UPLC) method for the simultaneous determination of six quaternary ammonium alkaloids (QAAs) in Coptidis Rhizoma. Methods The effect of different experimental parameters on the analysis of QAAs by RP-UPLC was evaluated. Results Optimal resolution was achieved with an Acquity UPLC BEH C18 column using a gradient elution profile and a mobile phase consisting of water spiked with 10 mmol/L ammonium bicarbonate (A, pH adjusted to 10.0 by ammonia water) and acetonitrile (B), at a flow rate of 0.30 mL/min and wavelength of 345 nm. The column temperature was set at 30 ℃. The proposed method was found to be reproducible, precise, and rapid according to the method validation. Conclusion The proposed method, which is compatible with MS analysis and the preparation of QAA, provides some helpful insights into the quality control of Coptidis Rhizoma.
    12  Preparation, Pharmacokinetics, and Tissue Distribution Properties of Icariin-Loaded Stealth Solid Lipid Nanoparticles in Mice
    LIU Ke-pan WANG Li-feng LI Yang YANG Bin DU Chao WANG Yang
    2012, 4(2):170-174. DOI: 10.3969/j.issn.1674-6384.2012.02.012
    [Abstract](1167) [HTML](0) [PDF 155.43 K](3205)
    Abstract:
    Objective To evaluate the difference of the pharmacokinetic (PK) and tissue distribution properties in mice administrated with lyophilized icariin stealth solid lipid nanoparticles (Ica-SSLN) modified by polyethylene glycol and icariin control solution (Ica-Sol). Meanwhile, to establish a sensitive, specific, and stable HPLC method for the determination of Ica in mice plasma and various tissues. Methods Ica-SSLN was prepared by high temperature melt-cool solidification method. Particle size and Zeta potentials were measured by a ZetaPlus. After iv administration of Ica-SSLN and Ica-Sol at a single dose of 7.46 mg/kg, the blood and tissues including brain, liver, spleen, lung, heart, and kidney were collected at different time points. The obtained concentration from HPLC analysis was statistically treated to determine the PK model and the relevant PK parameters using DAS1.0. Tissue distribution studies of Ica-SSLN were carried out in Kunming mice after iv administration and compared to Ica-Sol. Results The characteristic data showed that the mean particle size of Ica-SSLN was (50.03 ± 0.90) nm, entrapment efficiency was (71.67 ± 1.09)%, and the particles carried negative charge, Zeta potential was (?22.77 ± 1.89) mV. The concentration-time profiles of Ica in mice after iv administrated with Ica-SSLN and Ica-Sol were shown to fit a two-compartment open model. Compared with Ica-Sol, the t1/2β of Ica-SSLN was prolonged by seven times and the AUC was increased by four times. The levels of Ica concentration in the kidney tissues were significantly increased. In addition, compared with Ica-Sol, the relative target efficiency to kidney tissue was 79% and the relative tissue exposure was 16.95. Conclusion It demonstrates that Ica-SSLN has selective targeting to kidney tissue and the kidney targeted Ica-SSLN seems to have significant advantages and good development value.

    Current Issue


    Volume , No.

    Table of Contents

    Archive

    Volume

    Issue

    Most Read

    Most Cited

    Most Downloaded

    WeChat

    Mobile website