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    A highly sensitive LC-MS/MS method for the determination of 21-hydroxy deflazacort in nude mice plasma and its application to a pharmacokinetic study
    Qingyu Yao, Jian Li, Ye Yao, Rong Chen, Wenjun Chen, Hong Su, Liang Yang, Junsheng Xue, Wei Lu, Tianyan Zhou
    Journal of Chinese Pharmaceutical Sciences    2017, 26 (6): 404-412.   DOI: 10.5246/jcps.2017.06.044
    Abstract314)   HTML202)    PDF (1432KB)(7477)       Save

    In the current study, we established and validated a simple and sensitive liquid chromatography-tandem mass spectrometricmethod for the determination of 21-hydroxy deflazacort in nude mice plasma, and such a method was applied to a pharmacokinetic study. Using betamethasone as the internal standard, the plasma samples were pre-treated by precipitation with acetonitrile and then analyzed on a reversed-phase C18 column (50 mm×2 mm, 5 μm) with a mobile phase consisting of acetonitrile and 4.0 mM ammonium formate (pH was adjusted to 3.5 with formic acid (40:60, v/v)). The analyte was detected by a triple quadrupole tandem mass spectrometer using electrospray, and multiple reaction monitoring was employed to select 21-hydroxy deflazacort at m/z 400.2/124.0 and betamethasone at m/z 393.3/147.0 in the positive ion mode. The calibration curves were linear (r>0.99) over the range of 0.5–400 ng/mL. The intra- and inter-day precisions and accuracies were 4.5%–10.1% and –1.7%~10.7% respectively. This method was successfully applied to a preclinical pharmacokinetic study of deflazacort on female nude mice administered with a single oral dose of 4 mg/kg deflazacort, and its pharmacokinetics was characterized by a two-compartment model with first-order absorption. 

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    The Syntheses of β-Carboline-3-carboxamides Derivatives and Their Interaction with DNA
    Lin Wei, Xiao Sulong, Yang Ming *
    Abstract2065)      PDF (271KB)(1952)       Save
    To study the interactions of these compounds with calf thymus DNA(CT-DNA), seven β-carboline-3-carboxamides were designed and synthesized. The interactions of these compounds with CT-DNA were determined by the viscometric titration assay and Tm (melting temperature) value assay. Binding strengths were evaluated by spectrophotometric titration experiment and microcalorimetric measurement. The interactions of these compounds were tested with CT-DNA. It was showed that all of these compounds were able to change the Tm value of CT-DNA. The results of viscometric titration assay indicated that these compounds interacted with CT-DNA by intercalation. Spectrophotometric titration experiment showed that the binding strengths of these compounds with CT-DNA were different, which was well in agreement with the cell culture results. The binding was driven by entropy according to the results of the microcalorimetric measurement. This series of β-carboline-3-carboxamides is DNA targeting compounds. Their obvious antitumor biological effect is based on the intercalation with DNA base-pairs.
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    A new aristololactam from Asarum maximum
    Jie Yu, Chao-Mei Ma, Chang-Feng Long, Xuan Wang, Ming-Ying Shang, Shao-Qing Cai *, Masao Hattori, Tsuneo Namba
    Abstract985)      PDF (747KB)(1936)       Save
    A new aristololactam, aristololactam VII (1), was isolated from the root and rhizome of Asarum maximum Hemsl. On the basis of spectroscopic analysis, its structure was identified as 10-amino-7,8-dimethoxy-3,4-methylenedioxy-phenanthrene-1-carboxylic acid lactam.
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    Synthesis of nucleoside-peptide conjugate with disulfide bond as linker at C-5 of uridine
    Fei-Lin Nie, Xiao-Feng Wang, Yang Liu, Zhen-Jun Yang *, Liang-Ren Zhang, Li-He Zhang
    Abstract2913)      PDF (503KB)(1920)       Save

    In order to prepare pyrimidine nucleoside-peptide conjugate concisely, we developed a one-pot synthetic strategy. Started from uridine, 5-S-acetyl-thiomethyl-2',3'-di-O-isopropylidene-uridine (4) was synthesized as the key intermediate in four steps. Under acidic condition, compound 4 was deprotected and reacted with PySS-R (8, 12, 15, Py = 2-pyridyl, R = amino acid or peptide) in one pot to form uridine conjugates (9, 13, 2) with disulfide bond as linker.

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    Antioxidant phenanthrenes and lignans from Dendrobium nobile
    Xue Zhang, Jie-Kun Xu, Nai-Li Wang, Hiroshi Kurihara, Xin-Sheng Yao *
    Abstract3092)      PDF (680KB)(1911)       Save

    To study the antioxidant constituents from the stems of Dendrobium nobile, and to discuss their structure-activity relationship. Compounds were isolated from a 60% ethanolic extract by various chromatographic techniques and were identified by spectral analysis. The antioxidant activities of compounds were evaluated by DPPH free radical scavenging assay. Five phenanthrenes and four lignans were obtained from the active fractions of D. nobile. Their structures were identified as fimbriatone (1), confusarin (2), flavanthrinin (3), 2,5-dihydroxy-4,9-dimethoxyphenanthrene (4), 3,7-dihydroxy-2,4-dimethoxyphenanthrene (5), syringaresinol (6), pinoresinol (7), medioresinol (8) and lirioresinol-A (9), respectively. Compounds 2 and 6 exhibited more potent DPPH scavenging activities than vitamin C. All the above compounds were reported from this plant for the first time, and compounds 3, 4 and 9 were reported for the first time from the genus of Dendrobium. For all phenanthrenes and lignans, an electron-donating methoxyl group in the ortho position to the phenolic hydroxyl group exhibits enhanced antioxidant activities.

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    Modeling the molecular interactions of budesonide with bovine serum albumin guides the rational preparation of nanoparticles for pulmonary delivery
    Shuai Meng, Wei Cui, Shaohui Lin, Guiling Wang, Yu Hei, Bo Deng, Shuang Ma, Zhan Zhang, Yingchun Liu, Ying Xie
    Journal of Chinese Pharmaceutical Sciences    2018, 27 (6): 415-428.   DOI: 10.5246/jcps.2018.06.042
    Abstract241)   HTML111)    PDF (2094KB)(1904)       Save

    Large Hollow nanoparticulate aggregates (LHNAs) based on albumin nanoparticles is a promising technology for developing dry powder inhaler (DPI) with good aerodynamic properties in order to provide a new drug delivery system (DDS) for the treatment of lung disease. Improved understanding of molecular interactions could lead to prepare the DDS rationally. Therefore, this investigation utilized computations and experiments to reveal the mechanisms of budesonide (BUD) interactions with bovine serum albumin (BSA) at the molecular level. The molecular dynamics (MD) simulation revealed that there were three critical stable binding sites of BUD on BSA (P1, P2, P3) mainly by hydrophobic interaction and hydrogen bond. The energydecomposition of each residue to the whole BUD-BSA complex system in P1-P3 showed that nonpolar residues in or around the binding site played an important role in the binding of BUD to BSA. The molar ratio was close to 3 in preparations in drug-loading efficiency experiment, which was confirmed to the simulation results. The details of the binding sites from computation provided a guideline for the design of the BSA nanoparticles carrying BUD, which was prepared successfully at last. Combination of the MD simulation and experiment as well as the mechanism of the molecular interaction provided a solid theoretical basis for the preparation of BSA-LHNAs for DPI in the future.

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    Chemical constituents from the aerial parts of Plumbago zeylanica L.
    Xiao-Yan Huang, Ming-Xiong Tan, Qiang Wu, Yong Chen, Heng-Shan Wang *
    Abstract2328)      PDF (503KB)(1845)       Save

    To investigate the chemical constituents from the aerial parts of Plumbago zeylanica L. The chemical constituents were isolated by various column chromatographic methods and the structures were elucidated by various spectroscopic methods, especially 2D NMR spectra. A new triterpenoid, 1β,3β,11α-trihydroxy-urs-12-ene (1), together with six known compounds, androsta-1,4-diene-3,17- dione (2), isoshinznolone (3), neoechinulin A (4), harman (5), ergostadiene-3β,5α,6β-triol (6) and N-(N'-benzoyl-S-phenylalaninyl)-Sphenylalaninol (7) were isolated from the aerial parts of P. zeylanica. Compound 1 was a new compound, and compounds 2, 4-7 were obtained from this genus for the first time.

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    Chemical composition and anti-MRSA activity of the essential oil from Chinese eaglewood
    Wen-Li Mei, Yan-Bo Zeng, Jiao Wu, Hai-Bin Cui, Hao-Fu Dai *
    Abstract3025)      PDF (455KB)(1836)       Save

    To analyze the constituents of essential oil from Chinese eaglewood [resinous wood of Aquilaria sinensis (Lour.) Gilg] and its anti-methicillin-resistant Staphylococcus aureus (MRSA) activity. The essential oil was extracted by water-steam distillation and analyzed by GC/MS method. The relative contents of the compounds were determined by normalization. The compounds were characterized by NIST05 and WILEY275L database matching and comparison of their MS spectra with those of literature data. Antibacterial activity of the oil was assayed by the filter paper disc agar diffusion method. The oil showed significant antibacterial activity against MRSA. Sixty-six chromatographic peaks were detected, among them thirty compounds comprising 59.80% of the total essential oil were characterized. Twenty-six compounds comprising 54.26% of the oil were identified as sesquiterpenes. β-Agarofuran (8.96%), kusunol (7.82%), (-)-jinkoh-eremol (5.04%), agarospirol (4.53%), baimuxifuranic acid (4.09%) were the major sesquiterpenes. Four nor-sesquiterpenes and some other sesquiterpenes, such as 10-epi-γ-eudesmol, α-agarofuran, epi-ligulyl oxide, etc. were detected in Chinese eaglewood oil for the first time. This is the first report about anti-MRSA activity of Chinese eaglewood oil from A. sinensis.

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    Effects of angelica sinensis polysaccharide-iron complex on hemolytic anemia and bone marrow injury in mice
    Pei-Pei Wang, Yu Zhang, Kai-Ping Wang *, Ke Li
    Abstract359)      PDF (543KB)(1750)       Save
    To investigate the therapeutic effects of angelica sinensis polysaccharide-iron complex (APIC) on hemolytic anemia and bone marrow injury in mice models. The hemolytic anemia mouse model was established by i.p. of phenylhydrazine (PHZ). Changes of the indices including red blood cell count (RBC), hemoglobin (Hb) and hematocrit (HCT) were determined by blood analyzer, and reticulocytes were observed by brilliant cresol blue staining during administration. Bone marrow injured mouse model was established by i.p. of cytoxan (CY) and chloramphenicol (CH), and the therapeutic effect was observed by H-E staining. The indices of APIC treated groups with the medium and high doses were higher than those of the model group significantly. Moreover, the Hb and HCT were restored to the normal level after drug treatments. In addition, APIC can promote the proliferation and differentiation of reticulocytes obviously in the early stage of anemia mice, decrease adipose cell proliferation in bone marrow of injured mice and hasten the recuperation. In conclusion, APIC has therapeutic efficacy on hemolytic anemia and bone marrow injury caused by chemicals, which is reported for the first time.
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    Facile synthesis of a core trisaccharide of laminin as a potential metastatic antagonist
    Xiao-Feng Jin, Xiang-Bao Meng, Kai-Jun Liao, Qing Li, Zhong-Jun Li*
    Abstract2017)      PDF (691KB)(1746)       Save

    A core trisaccharide of laminin, β-D-Gal-(14)-β-D-GlcpNAc-(16)-α-D-Manp-OMe, with potential anti-tumor metastatic activity was designed and prepared. 2-Iodoglactosyl azide was used as the donor to construct 2-N-acetamido-2-deoxylactosyl moiety through an azidoiodo-glycosylation reaction. Simultaneously, 1, 2-trans-β-glycosic bond was formed stereoselectively in one step with a moderate yield. This novel procedure avoided the use of 2-amino-2-deoxyglucose as both donor and acceptor.

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    Structural elucidation of a new cembranoid diterpene from the Chinese soft coral Sarcophyton sp.
    Wei Bie, Zhi-Wei Deng, Min-Juan Xu, Wen-Han Lin *
    Abstract1605)      PDF (492KB)(1735)       Save

    To investigate the cembranoid diterpenes from the soft coral Sarcophyton sp. collected in the South China Sea. Repeatedly column chromatography was performed for the isolation and purification. The structures were elucidated on the basis of extensive spectral data (IR, MS, 1D- and 2D-NMR) analysis by comparing with literature data. A new cembranoid diterpene namely sarcophyolide A (1), together with 7α, 8β-dihydroxydeepoxysarcophine (2) were isolated from this species. The cembranoid diterpenes with γ-lactone could be chemotaxonomic markers of Sarcophyton sp.

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    A continued study on the bisoprolol and isosorbide dinitrate transdermal patches: cardiovascular protection in spontaneously hypertensive rats
    Wei Wei, Ji-Hua Fu *, Chang-Hai Su , Ying Shan, Yuan Wang, Shu-Jia Kong, Ji-Hui Zhao, Wan-Liang Lu * *, Shu-Ming Wang, Li Wang
    Abstract3206)      PDF (512KB)(1632)       Save

    The objective of the present study is to examine cardiovascular protective action of a newly developed transdermal patch by incorporating bisoprolol and isosorbide dinitrate in spontaneously hypertensive rats. As the combination therapy with these two synergistic drugs at low doses through a suitable form of administration could provide optimal therapeutic benefit, we further evaluated the effects of a 42 d period of anti-hypertensive treatment in spontaneously hypertensive rats. Rats were divided into the following five groups: control (blank patch), bisoprolol fumarate tablets (BP-FT, 20.0 mg/kg, i.g.), bisoprolol transdermal patch (BP-TP, 20.0 mg/kg), isosorbide dinitrate transdermal patch (ISDN-TP, 20.0 mg/kg), and the combination of BP and ISDN in a transdermal patch at low doses (8 and 12 mg/kg, respectively). The effects of treatment were evaluated via biochemical indicators related to cardiovascular protection, structure and function. The combination therapy had synergistic anti-hypertensive effects and significantly reduced blood pressure with the benefit of controlling blood pressure variability compared to BP-FT and BP-TP. The combined treatment also reduced heart rate as well as BP-FT and BP-TP, while ISDN-TP had no evident effects on blood pressure, heart rate, and cardiovascular protection. Combination therapy was superior to BP-TP and BP-FT at increasing blood atrial natriuretic peptide and nitric oxide, while also reducing cardiac hydroxyproline and endothelin-1 with no difference in blood endothelin-1 and cardiac malondialdehyde levels. Cardiovascular remodeling differed among the groups, with the combination therapy reducing cardiac hypertrophy and the aortic media/lumen ratio. The consequential improvements in relaxation in response to cumulative concentrations of acetylcholine may explain the associated improvement in endothelial function. Combination treatment with a transdermal patch exhibited a synergistic therapeutic effect. Such favorable cardiovascular effects with nitric oxide donors and β-blockade combination through a transdermal patch may provide long-term cardiovascular protection during anti-hypertensive treatment.

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    Increased stability and solubility of dihydroartemisinin in aqueous solution through the formation of complexes with 2-hydroxypropyl-β-cyclodextrin
    Xiao-Yun Zhang, Jian-Ping Liu*, Hua Qiao, Kui-Yuan Huang, Yan-Bin Shi, Shu-Mei Song, Jing-Man Ni
    Abstract1464)      PDF (1037KB)(1622)       Save
    The effect of various concentrations of 2-hydroxypropyl-β-cyclodextrin (HP-β-CD) on the solubility of dihydroartemisinin (DHA) in aqueous solution at different pHs was investigated. The influence of different concentrations of 2-hydroxypropyl-β-cyclodextrin on the stability of dihydroartemisinin at 50, 60, 70 and 80 ºC was also studied. Inclusion complex of dihydroartemisinin with 2-hydroxypropyl-β-cyclodextrin was prepared and characterized by X-ray diffraction and differential scanning calorimetry. The 2-hydroxypropyl-β-cyclodextrin effectively inhibited the hydrolysis of dihydroartemisinin and greatly increased its solubility. Furthermore, we showed that the higher concentrations of 2-hydroxypropyl-β-cyclodextrin, the better stability and solubility of dihydroartemisinin. When the temperature was increased, the stability of dihydroartemisinin decreased. Our results indicated that 2-hydroxypropyl-β-cyclodextrin can be used as a stabilizer and solubilizer of dihydroartemisinin.
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    Fenofibrate solid dispersion pellets prepared by fluid-bed coating: physical characterization, improved dissolution and oral bioavailability in beagle dogs
    Ning Tang, Jie Lai, Ya-Pin Chen, Yi Lu *, Wei Wu *
    Abstract1633)      PDF (1017KB)(1619)       Save
    Solid dispersion of fenofibrate (FNB), a poorly water-soluble drug, was prepared by a fluid-bed coating technique with PEG 6000 as the carrier. The physical state was characterized by DSC and X-ray powder diffractometry, which indicated the existence of fenofibrate in crystalline form in the solid dispersion. In vitro dissolution was studied in water containing 1% sodium lauryl sulfate, FASSIF and FESSIF. Significant enhancement in dissolution was achieved at PEG/FNB ratio of 4/1 with near complete dissolution within 30 min. Moderate improvement in dissolution rate was observed at smaller PEG/FNB ratios. Oral bioavailability was studied in beagle dogs after oral administration of fenofibrate solid dispersion pellets by monitoring fenofibric acid in plasma. The oral bioavailability of PEG/FNB 3/1 and 4/1 solid dispersion pellets was improved by 3.4 and 4.4-fold as compared to Lipanthyl®, a commercial micronized fenofibrate formulation. There was a strong dependence of oral bioavailability on the in vitro dissolution rate. Good correlation was observed between the in vivo absorption fraction and the in vitro dissolution rate in each of the dissolution media, water containing 1% sodium lauryl sulfate, FASSIF and FESSIF. It could be concluded that PEG/FNB solid dispersion pellets were able to improve the dissolution and oral bioavailability of fenofibrate.
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    Determination of ganoderic acids in rat plasma after oral administration of total triterpenoids from Ganoderma lucidum
    Bin-Bin Xue, Xiao-Yu Guo, Qing-Ming Che *
    Abstract1656)      PDF (478KB)(1586)       Save
    To investigate the absorption of total triterpenoids from Ganoderma lucidum in rats. HPLC-DAD and LC-MS methods were used to identify ganoderic acids in rat plasma after oral administration of total triterpenoids from G. lucidum by comparing their HPLC retention behaviors, UV absorption spectra, and mass spectra with authentic samples. Five ganoderic acids, ganoderic acid C2, C6, G, B and A were simultaneously detected in rat plasma. Ganoderic acids can be directly absorbed into circulation after oral administration of total triterpenoids from G. lucidum in rats.
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    Determination of silymarin in microemulsion by RP-HPLC
    Xin-Ru Li, Yan-Fang Li, Yan-Xia Zhou, Xiao-Yan Li, Yan Liu *
    Abstract1402)      PDF (744KB)(1574)       Save
    We established a RP-HPLC method for the analysis of silymarin in microemulsion. Silymarin was separated using a ODS C18 column and monitored at the wavelength 288 nm. The mobile phase consisting of methanol-water-acetic acid (42:58:0.5, v/v/v) was pumped at a flow rate of 1.0 mL/min. The linear range of calibration curve was 10-1000 μg/mL. The average recovery was 99.0%-100.7% for silybin isomers. The RSD values of inter-day and intra-day assays were lower than 1.6% for silybin isomers. The method is simple, rapid, reproducible and precise for the quantitative determination of silymarin in microemulsion.
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    Application of high-titred IgY antibodies in orthopox virus diagnostics
    Xiao-Ying Zhang *, Andreas Kurth, Diana Pauly, Georg Pauli, Rüdiger Schade, Heinz Ellerbrok
    Abstract3605)      PDF (930KB)(1570)       Save
    Layer chickens were immunized with three species of inactivated orthopox virus (vaccinia virus, calpox virus and cowpox virus). Antibodies (IgY) were purified from egg yolks by improved polyethylene glycol precipitation. The development of IgY directed against orthopox virus antigens was followed by immunofluorescence assay, plaque reduction neutraliztion test and immunoelectron microscopy. Cross-reactivity of two IgY antibodies with cells infected by the different strains of the pox viruses was also investigated by different methods (immunofluorescence assay, plaque reduction neutraliztion test and Western blot). Even in very high dilutions in immunofluorescence assay (titres up to 1:106 and 1:105, respectively) and persisted on a plateau over 10 months after four booster injections, it was showed that anti-vaccinia virus IgY and anti-calpox virus IgY were positive. Neutralizing activity and ultra-structural detection of antigen with gold-labelled antibodies were respectively observed in plaque reduction neutralization test and immunoelectron microscopy. Western blot analysis revealed specific binding of IgY to virus proteins. Thus, there was cross-reactivity between different orthopox viruses. Finally, orthopox virus-specific IgY antibodies bounded magnetic beads (Dynabead) were used to concentration of orthopox viruses. This study suggests that anti-pox virus IgY could serve as a useful tool for orthopox viruses diagnosis.
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    Simultaneous determination of four active compounds in Dangguilonghui tablet by high-performance liquid chromatography
    Chun-Li Hu, Dong-Mei Wang, Peng Zhang, Huai-Qing Zhao*
    Abstract1457)      PDF (475KB)(1567)       Save

    high-performance liquid chromatography (HPLC) method has been developed for the first time to simultaneously quantify the four active ingredients, namely aloin, baicalein, aloe-emodin and wogonin, in Dangguilonghui tablet. The marker compounds were separated on the Diamonsil C18 column at a flow rate of 1.0 mL/min with a mobile phase of methanol-acetonitrile-0.3% aqueous phosphoric acid (220: 4: 200, v/v/v) and while the detection wavelength was set at 225 nm. The assay was linear over the range of 1.450 - 29.00 μg/mL (r = 0.9992) for aloin, 0.4050 - 8.100 μg/mL (r = 0.9994) for baicalein, 0.1100 - 2.200 μg/mL (r = 0.9997) for aloe-emodin, 0.2160 - 4.320 μg/mL (r = 0.9991) for wogonin, respectively. The average sample recoveries at three concentration levels were 100.7% (RSD = 0.88%), 101.0% (RSD = 0.89%), 100.0% (RSD = 1.3%) and 100.1% (RSD = 1.1%) for these constituents, respectively. This method is suitable for the quality control of Dangguilonghui tablet.

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    Synthesis of allyl 4-O-{3-deoxy-3-[4-benzylaminocarbonyl-1H-(1,2,3)-triazol-1-yl]-β-D-galactopyranosyl}-2-deoxy-2-acetamido-β-D-glucopyranoside as a potential inhibitor of galectin-3
    Chen Li, Xiang-Bao Meng, Xiao-Feng Jin, Zhong-Jun Li, Qing Li *
    Abstract2736)      PDF (531KB)(1557)       Save
    Allyl 4-O-{3-deoxy-3-[4-benzylaminocarbonyl-1H-(1,2,3)-triazol-1-yl]-β- D -galactopyranosyl}-2-deoxy-2-acetamido-β- D -glucopyranoside, a potential inhibitor of galectin-3, was designed and synthesized using lactose as staring material. The modifications of lactose included in introducing of N-acetamino group at the C-2 position through an azidoiodoglycosylation meanwhile constructing the β-aminolactoside stereoselectively and replacing 3'-OH with substituent 1,2,3-triazolyl group to enhance the affinity toward galectin-3.
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    Augmentative effect of tetrandrine on pentobarbital hypnosis mediated by 5-HT1A and 5-HT2A/2C receptors in mice
    Nan Du, Li-En Wang, Xiao-Rong Shi, Xiang-Yu Cui, Su-Ying Cui, Fan Zhang, Yong-He Zhang *
    Abstract2873)      PDF (477KB)(1552)       Save
    It has been reported that augmentative effect of tetrandrine on pentobarbital hypnosis in mice may be related to serotonergic system. The present study was undertaken to investigate the interaction of tetrandrine and different 5-HT receptors on pentobarbital-induced sleep by using the loss-of-righting reflex method. The results showed that augmentative effect of tetrandrine on pentobarbital hypnosis in mice were potentiated by the p-MPPI (5-HT 1A receptor antagonist) (1 mg/kg, i.p.) and ketanserin (5-HT 2A/2C receptor antagonist) (1.5 mg/kg, i.p.), respectively. Pretreatment with either 8-OH-DPAT (5-HT 1A receptor agonist) (0.1 mg/kg, s.c.) or DOI (5-HT 2A/2C receptor agonist) (0.2 mg/kg, i.p.) significantly decreased pentobarbital-induced sleep time, and tetrandrine (60 mg/kg, i.g.) significantly reversed this effect. These results suggest that both the 5-HT 1A and 5-HT 2A/2C subfamily may be involved in the potentiating mechanism of tetrandrine’s effects on pentobarbital hypnosis.
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    Journal of Chinese Pharmaceutical Sciences
    Abstract874)      PDF (971KB)(1521)       Save
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    Synthesis and activity of hydroxyethylene peptidomimetic inhibitors of human β-secretase
    Chao Ma, Yue-Hua Wang, Xiao-Ming Yang, Xiao-Min Zou,Yang Lü, Guan-Hua Du, Ping Xu *
    Abstract275)      PDF (512KB)(1519)       Save
    A series of β-secretase peptidomimetic inhibitors with Leu*Ala hydroxyethylene dipeptide isostere were synthesized and their β-secretase inhibitory activities were measured. The most potent compound N9 showed an inhibitory rate of 59.66% (10 mg/mL). Compound N9 might be further modified by means of computational chemical methodology.
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    Quantitative Variations of Five Anthraglucosides in Rhubarb
    Jun-Hua Zheng, Qin Huang, Zhi-Guo Zhang, Shuang-Xin Gao, Zhi-Cen Lou
    Abstract2497)      PDF (322KB)(1432)       Save
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    Determination of Dehydroepiandrosterone Sulfate with High Performance Liquid Chromatography
    Hua Chi Yu-Ling Liu Shi-Jie Gu
    Abstract1949)      PDF (334KB)(1427)       Save
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    Allicin induces apoptosis, cell cycle arrest and microtubule disassembly in human nasopharyngeal carcinoma KB cells
    Ya-Ping Yang, Min Li *, Bo Xu, Wei Guo, Jing-Rong Cui, Kui Wang
    Abstract1475)      PDF (1001KB)(1396)       Save
    Allicin, a major biologically active component of garlic, is produced from its inactive precursor alliin by the enzyme alliinase. In this study, we investigated its effects on human nasopharyngeal carcinoma KB cells. After incubation for 48 h, allicin inhibited the growth of KB cells in a concentration-dependent manner with an IC50 value of (2.2±0.2) μg/mL. Incubation with allicin for 48 h caused a concentration-dependent induction of apoptosis in the concentration range of (16–48) μg/mL, and the induction of apoptosis was confirmed by the changes of mitochondrial membrane potential, F-actin contents and nuclear condensation in KB cells. Moreover, allicin concentration-dependently arrested KB cells at the S-phase of the cell cycle in the range of (16–48) μg/mL. In addition, treatment with the compound caused concentration-dependent disassembly of microtubule cytoskeleton in KB cells, which is similar to the effect of colchicine, a well-known microtubule destabilizing agent. We concluded that the abilities of allicin to inhibit the proliferation of KB cells probably relate to its apoptosis induction, cell cycle arrest and microtubule destabilizing properties
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    Cited: Baidu(11)
    Drug delivery via the transferrin receptor-mediated endocytosis pathway
    Qing Xia, Xiu-Wei Yang, Xiao-Da Yang *, Zhong-Ming Qian, Kui Wang
    Abstract2315)      PDF (897KB)(1383)       Save

    The membrane transferrin receptor-mediated endocytosis has been exploited for developing novel targeted drug delivery systems, which could have a variety of applications in the site-specific delivery of anticancer drugs, proteins and therapeutic genes into proliferating malignant cells that overexpress the transferrin receptors. This is achieved by coupling transferrin or monoclonal antibody to transferrin receptor with therapeutic drugs or drug delivery vesicles. The transferrin conjugates can be obtained by use of either bifunctional chemical linkers or by genetic infusion of therapeutic peptides/proteins into the structure of transferrin / and monoclonal antibody to transferrin receptor. A variety of drug carriers such as liposomes, nanoparticles and DNA-polymer complexes (i.e. polyplex and lipoplex) were used to efficiently deliver the transferrin conjugates. Use of transferrin conjugates results in improvement in drug efficacy, selectivity and drug release as well as reduction in drug toxicity. This paper reviews the basic biochemistry of transferrin and the transferrin receptor as well as the strategy for developing targeted drug delivery system.

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    Studies on Active Polysaccharides from Ganoderma lucidum
    Yun-Qing He, Rong-Zhi Li, Qi Chen, Zhi-Bin Lin, Dong Xin, Li Ma
    Abstract2346)      PDF (356KB)(1382)       Save
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    High performance liquid chromatography for the determination of flavonoids
    Ming-Lei Chen, Wei Hu, Chao Zhang, Yun Fang *
       DOI: 10.5246/jcps.2011.04.039
    Abstract1353)      PDF (1187KB)(1363)       Save
    Due to their biological and physiological importance, flavonoids receive considerable attention in the literature. Nowadays, high performance liquid chromatography (HPLC) is the most widely used analytical method. In this review, we summarize the principle of the choice of HPLC column and mobile phase, discuss and compare the features of various detections such as UV, fluorescence detection, electrochemical detection, chemiluminescence detection, UV-MS etc. Recent developments in HPLC including ultra-LC and miniaturization of LC (micro-LC, capillary-LC, and nano-LC), are also discussed.
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    Cited: Baidu(6)
    Chemical Constituents of Echinops talassicus Root
    De-An Guo, Xiao-Yang Liu, Liang Qiao, Cong-Yuan Gao, Zhi-Cen Lou
    Abstract2120)      PDF (337KB)(1359)       Save
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    Pharmacokinetics of two modified release system of dipyridamole in beagle dogs
    Zhi-Hong Zhang, Chang-Guang Wang, Guang-Mei Sun, Ning Li, Bo Peng, Wei-San Pan *
    Abstract2582)      PDF (703KB)(1354)       Save
    A novel floating osmotic pump controlled release system (FOP) and traditional matrix sustained release tablets (MT) of dipyridamole (DIP) were characterized in terms of pharmacokinetics, drug release, and in vitro-in vivo correlation. In vivo study was performed by a three-crossover study in six beagle dogs relative to the conventional tablet (CT). A HPLC method for the determination of DIP in the plasma was developed. Cumulative percent of absorption fraction was compared to that of in vitro cumulative release. Both FOP and MT displayed obvious extended release characteristic in vivo while FOP showed a better extended release behavior. The bioavailability of FOP was higher than that of MT and a zero-order release linear correlation of DIP between fraction absorbed in vivo and fraction dissolved in vitro was established for FOP while not for MT. The results indicated the existence of an absorption window in upper part of the GI track of DIP, which meant that floating system could be excellent for the drug delivery. In addition, the in vitro model was a good choice for depicting in vivo absorption and for optimization of the formulation of FOP if it is needed to be bio-equivalent to MT.
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    Chemical constituents from the Rhodiola genus plants
    Jiangtao Zhou, Lei Xu, Yanyan Chen, Xiaonan Li, Miaomiao Jiang
    Journal of Chinese Pharmaceutical Sciences    2014, 23 (7): 433-445.   DOI: 10.5246/jcps.2014.07.058
    Abstract437)   HTML2)    PDF (828KB)(1333)       Save

    The Rhodiola genus (Crassulaceae) is composed of about 90 species, mainly growing in high and cold regions. Some species are used as medicinal herbs to treat many diseases, such as cerebral hypoxia, cardiovascular disease, plateau response and so on. Up to now, about 180 constituents which are mainly glycosides, flavonoids, terpenoids, tannins, sterol and other compounds have been identified in the genus. The present review summarizes the chemical constituents isolated from the Rhodiola genus over the past few decades, with particular emphasis on Rhodiola crenulata (HK. f. et Thoms.) H. Ohba which is being studied by our research group.

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    Cited: Baidu(6)
    A convenient synthesis of 1-alkyl-5-amino-6-phenylethyluracils as potential non-nucleoside HIV-1RT inhibitors
    Xiao-Yan Ma, Zhi-Jian Cheng, Yan-Li Chen, A-Min Li, Zhi-Li Zhang, Xiao-Wei Wang, Jun-Yi Liu *
    Abstract2505)      PDF (662KB)(1309)       Save

    1-Alkyl-5-amino-6-phenylethyluracils (1a, 1b) were synthesized as potential non-nucleoside HIV-1RT inhibitors. A convenient synthetic procedure was developed for the preparation of 1-alkyl-5-amino or 5-aminosubstituted-6-phenylethyluracils, which were synthesized in three or four steps from 6-methyluracil in good yield. The development of a one-pot reaction that simultaneously removed the benzyl protection group and reduced the nitro group greatly improved the yield of the synthesis. Compounds 1a and 1b are analogs of MKC-442, which is an efficient inhibitor of HIV-1 reverse transcriptase. 1a and 1b were tested for their inhibition of HIV-1RT, and moderate activity was found for 1a.

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    Preparation, physicochemical characterization and cyctotoxicity of solid
    dispersion of paclitaxel and polyvinylpyrrolidone

    Jia-Bei Sun, Xiang-Rui Liu, Jian-Cheng Wang, Wan-Liang Lu, Xuan Zhang*,
    Qiang Zhang
    Abstract2027)      PDF (591KB)(1303)       Save

    The objective of this study was to prepare and characterize paclitaxel-polyvinylpyrrolidone (PTX-PVP) solid dispersions with the intention of improving its solubility and dissolution properties. The PTX-PVP solid dispersion systems were prepared by solvent method. The release rate of paclitaxel was determined from dissolution studies and the physicochemical properties of solid dispersion were investigated by differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD) and scanning electron microscopy (SEM). The cytotoxicities of paclitaxel in solid dispersion to the SKOV-3 cells were assayed by a SRB staining method. The results showed that the solubility and dissolution rate of paclitaxel were significantly improved in solid dispersion system compared with that of the pure drug and physical mixture. The results of DSC and PXRD showed that the paclitaxel in solid dispersion was amorphous form. No paclitaxel crystals in the solid dispersions was found during SEM analysis. Cytotoxicity study suggested that the inhibitory rates of PTX-PVP solid dispersion to SKOV-3 cells were higher than that of pure paclitaxel. The solubility and dissolution of paclitaxel were improved by solid dispersion technique. In vitro cytotoxicity of paclitaxel in solid dispersion was higher than that of pure drug.

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    In vitro investigation of RGD-modified stabilized cationic liposomes as non-viral vehicle for siRNA delivery
    Shi-Jin Yang, Li-Juan Yang, Juan Jiang, Jian-Cheng Wang *, Qiang Zhang
    Abstract2921)      PDF (816KB)(1298)       Save

    In this study, the novel RGD-modified stabilized cationic liposomes were developed as the delivery vehicle for siRNA targeting human MDR1 gene. The complex of cationic liposomes and siRNA, RGD-Lipo-siRNA, was prepared with a narrow size distribution below 200 nm. It was shown that the encapsulated siRNA in the liposomes could be effectively protected from serum degradation. Also, enhanced cell binding and intracellular uptake of siRNA in the doxorubicin-resistant human ovarian cancer cell lines SKOV3/A were found in RGD-Lipo-siRNA preparation as compared to that of unmodified cationic lipsomes (Lipo-siRNA). Using the post-insertion method for RGD modification, lysosome release of siRNA in pRGD-Lipo-siRNA was improved. From flow cytometry, significant increase of doxorubicin accumulation was observed in the SKOV3/A cells treated with pRGD-Lipo-siRNA targeting human MDR1 gene. In vitro cytotoxicity assay showed that the significant cell growth inhibition was achieved in the SKOV3/A cells after treating with the combined use of siRNA and doxorubicin. In conclusions, postinserted RGD modified lipoplex, pRGD-Lipo-siRNA, was successfully used for siRNA transfection and achieved drug resistance reversal in human ovarian cancer SKOV3/A (doxorubicin-resistant) cells. It suggested that this liposomes might be a potential vehicle for siRNA delivery in vivo.

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    Doxorubicin Stealth Liposomes Prepared with PEG-Distearoyl Phosphatidylethanolamine and Distribution as well as Antitumor Activity in Mice
    Lu Wanliang, Wei Shuli, Zhang Qiang, Qi Xianrong, Sun Huadong
    Abstract1522)      PDF (309KB)(1288)       Save
    The stealth liposomal doxorubicin and regular liposomal doxorubicin were prepared with and without polyethylene glycol-distearoylphosphatidylethanolamine (PEG2000-DSPE) by the method of ammonium sulfate gradient, respectively. A reversed HPLC-UV method was established to determine the concentrations of doxorubicin in mice tissues after administration. The tissue distribution of stealth liposomal, regular liposomal and free doxorubicin (doxorubicin hydrochloride solution) in mice and pharmacokinetics were investigated. The results showed that the distribution and pharmacokinetics of stealth liposomal doxorubicin in mice were pronouncedly changed as compared with regular liposomal doxorubicin and free doxorubicin. The levels of liposomal doxorubincin in the heart tissues were reduced and those of in the blood increased, especially of stealth liposomal doxorubicin. In evaluation of antitumor activity, the differences between stealth liposomal doxorubicin and regular liposomal doxorubicin were that the inhibition rate of solid tumor weight for stealth liposomal doxorubicin was higher than that of regular liposomal doxorubicin. It is concluded that the PEG ylation of liposomes can pronouncedly prolong the circulation time of doxorubicin in mice blood and increase the antitumor activity.
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    Synergistic effect of pinellia total alkaloids and uncaria total alkaloids on anticonvulsant action in mice and rats
    Yin-Xia Cheng, Ming-Zheng Wang *, Jing-Jing Chen, Rong Yang, Xin-Gu He,
    Yong-Gang Ma, Li-Hua Yang, Ming-Sheng Zhang
    Abstract2336)      PDF (732KB)(1272)       Save

    Aim To investigate the synergistic effect of the combination of pinellia total alkaloid (PTA) and uncaria total alkaloid (UTA), and explore the mechanism of anticonvulsant action. Methods Anticonvulsant and toxic effect profiles of combinations of PTA with UTA, alone and at three fixed ratios of 1:4, 1:1, 4:1, were evaluated in maximal electroshock (MES)-induced seizures and acute toxicity test in mice. Respective ED50 and LD50 were calculated with Bliss’s method. Their synergistic effect were evaluated by isobolographic analysis and allowed the determination of benefit indices (BI) for respective combinations. The model of convulsive rats kindled by penicillin topically injected into cortex was used to investigated the content of Glu, Asp, Gly and GABA in hippocampus using high performance liquid chromatography (HPLC). Results Combinations of PTA and UTA at the ratio of 4:1 were synergistic in MES test and antagonistic in acute toxicity test, showing the best profile for combinations of PTA with UTA. In contrast, the ratios of 1:4 and 1:1, despite synergistic in MES test, were additive in acute toxicity test. The 4:1 combination and two drugs alone significantly decreased Glu level and increased GABA level in the hippocampusbut the GABA level in the 4:1 combination group was higher than that in the two drugs alone groups. They did not have significant influence on the levels of Asp and Gly. Conclusion Combinations of PTA and UTA at 4:1 ratio demonstrated synergistic effect in anticonvulsant action and antagonistic effect in toxicity. The anticonvulsant mechanism might be related to decreasing the excitability of Glutamatergic neurons and increasing the inhibition of GABAergic neurons.

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    Cited: Baidu(21)

    Graphical contents list

    Journal of Chinese Pharmaceutical Sciences
    Abstract112)      PDF (859KB)(1263)       Save
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    The anti-hyperlipidemia activities of six herbs before and after fermentation with white rot fungi
    Jun-Yan Tao #, Guo-Hua Zheng #, Lei Zhao, Zhi-Jun Huang, Qiong-Guang Zhang, Jian-Guo Wu, Xiao-Yu Zhang *
    Abstract1478)      PDF (863KB)(1261)       Save

    Hyperlipidemia has high morbidity. We explored the novel activities of six Chinese herbs before and after fermentation for preventing hyperlipidemia. The herbs were fermented with white rot fungi Ganoderma lucidum, a strain of EN2. Lovastatin was used as the positive control. Mice were treated with those herbs before and after fermentation treatment for 15 d and then injected peritoneally with Triton 3393. After the treatment, the serum total cholesterol (TC) and triglyceride (TG) were measured. Moreover, the changes of the ingredients of those herbs were analyzed by fingerprint chromatography. The results showed that Herba leonuri before fermentation, Ramulus mori and Caulis lonicerae after fermentation, Radix sophorae flavescentis before and after fermentation showed activities to prevent hypertriglyceridemia, while Ramulus mori and Herba leonuri before fermentation showed activities to prevent hypercholesterolemia. In addition, some new ingredients were appeared after fermentation. In conclusion, the novel activities of these herbs to prevent hyperlipidemia were identified and the new ingredients that emerged after fermentation warrant further exploration.

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    Cited: Baidu(11)
    Metabolites of baicalein 6,7-diacetate in rats
    Yun Hu, Xiao-Yu Guo, Lin Yang, Qing-Ming Che *
    Abstract2401)      PDF (679KB)(1241)       Save

    To investigate the metabolites of baicalein 6,7-diacetate in rats. HPLC-DAD and LC/MSn methods were used to analyze the metabolites in intestinal tract and plasma after oral administration of baicalein 6,7-diacetate to rats. Baicalein 6,7-diacetate was degraded into baicalein 6-monoacetate and baicalein in rat intestinal tract, and four baicalein glucuronides, baicalein 6-O-glucuronide, baicalein 6-methoxyl-7-O-glucuronide, baicalein 6,7-di-O-glucuronide, and baicalein 6-O-glucose-7-O-glucuronide were detected and tentatively identified in rat plasma. This is the first time to report the metabolites of baicalein 6,7-diacetate in rats. Six metabolites were identified in rat intestinal tract and plasma.

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    Cited: Baidu(2)
    Analysis of principal isoflavone glycosides and aglycones in Radix astragali
    Xin-Gang Du, Yan-Jing Bai, Bin Wang, Yu-Ying Zhao, Qing-Ying Zhang *, Lu-Qi Huang
    Abstract1907)      PDF (482KB)(1234)       Save

    Two major isoflavone glycosides [calycosin 7-O-β-D-glucopyranoside (1) and ononin (2)] and their aglycones [calycosin (3) and formononetin (4)] were simultaneously quantified with HPLC/DAD method. Two unknown compounds were identified as calycosin 7-O-β-D-glucopyranoside-6'''-O-malonate (U1) and formononetin 7-O-β-D-glucopyranoside-6'''-O-malonate (U2), respectively, with LC/MSn. Raw Radix astragli were shown to have higher contents of isoflavone glycosides (1, 2), but lower contents of aglycones (3, 4) than the processed herbal materials. After being moistened with water and stored up for 24 h at 35 ºC, the glycosides and their malonates were almost completely transformed to their corresponding aglycones. The different contents of the isoflavone glycosides and their aglycones in raw and processed Radix astragali materials might be due to enzymolysis of the glycosides during processing.

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