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Table of Content

    18 July 2014, Volume 23 Issue 7
    Contents
    Contents
    Journal of Chinese Pharmaceutical Sciences
    2014, 23(7):  429-432. 
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    Review
    Chemical constituents from the Rhodiola genus plants
    Jiangtao Zhou, Lei Xu, Yanyan Chen, Xiaonan Li, Miaomiao Jiang
    2014, 23(7):  433-445.  DOI: 10.5246/jcps.2014.07.058
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    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.

    Original articles
    Scalable synthesis of salidroside
    Qingzhao Liang, Hui Li, Wenxuan Zhang, Xiangbao Meng, Zhongjun Li
    2014, 23(7):  446-453.  DOI: 10.5246/jcps.2014.07.059
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    By analyzing the key steps that restricted the industrial synthesis of salidroside, selective protection of tyrosol with different acylation reagents was adopted. The strategy facilitated the crystallization of intermediates, which allowed the scalable synthesis of salidroside. It included a reaction of penta-O-acetyl-β-D-glucose with acyl protected tyrosol in the presence of Lewis acid catalyst (ZnCl2), followed by deacylation under basic condition (NaOMe/MeOH) to give the salidroside. The total yield of this three-step reaction was 47%. Final product and intermediates were purified by recrystallization, which significantly reduced the cost and made the large scale synthesis feasible.

    Supramolecular self-assembly for delivery of oligonucleotides and its phototriggered unpacking in living cells
    Peng Wang, Yuzhuo Ji, Zhixuan Wang, Xinjing Tang
    2014, 23(7):  454-462.  DOI: 10.5246/jcps.2014.07.060
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    Two photolabile amphiphilic supramolecules were designed and synthesized with mono-dendrite and tri-dendrite, which can reversibly self-assemble to spheroid and wedge-shaped nanoparticles. With multiple branches of terminal amine labeled PEG, these nanoparticles can associate with a negatively charged oligonucleotide and their usage for oligonucleotide delivery was evaluated. Oligonucleotide/nanoparticle complex containing tri-dendrite can efficiently deliver oligonucleotide into cells via endocytosis, while the complex containing mono-dendrite almost lost their ability to deliver oligonucleotide. Further light activation triggered the dissociation of tri-dendrite supramolecular assembly via 1,4- and 1,6-quinone-methide rearrangement, leading to the efficient unpacking of the oligonucleotide in cells.

    The preparation and characteristics of febuxostat SiO2 solid dispersions
    Wending Song, Ruo Du, Ping Song, Ting Zhong, Weiqiang Zhang, Yang Zhao, Chao Wang, Xuan Zhang, Qiang Zhang
    2014, 23(7):  463-470.  DOI: 10.5246/jcps.2014.07.061
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    In the present research, we selected Sylysia as a porous material and febuxostat (FBT) as model drug to prepare the FBT SiO2 solid dispersions using a solvent evaporation method. We firstly established an HPLC method for determining FBT in our prepared FBT SiO2 solid dispersions. And then, the characteristics of FBT SiO2 solid dispersions were investigated, including differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), scanning electron microscope (SEM), particle size and distribution. The solubility and dissolution of FBT SiO2 solid dispersion were also evaluated. The results of DSC and PXRD showed that the FBT existed in an amorphous state in FBT SiO2 solid dispersions. The SEM and particle size results indicated that the shape and average particle size of FBT SiO2 solid dispersions was similar to the Sylysia. The solubility and dissolution of FBT in FBT SiO2 solid dispersions were significantly enhanced compared with the pure FBT. In conclusion, we successfully prepared FBT SiO2 solid dispersions to increase the solubility and dissolution rate of the poorly water-soluble FBT.

    Comparison of dopamine with levodopa in the induction of aryl sulfotransferases and estrogen sulfotransferase in rat liver
    Xueyan Shao, Jian Li, Siyuan Wang, Guangping Chen, Jiaojiao Xu, Xiwei Ji, Liang Li, Wei Lu, Tianyan Zhou
    2014, 23(7):  471-479.  DOI: 10.5246/jcps.2014.07.062
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    Sulfotransferases (SULTs) are one of the most important phase IIdrug-metabolizing enzymes. Among them, aryl sulfotransferases (SULT1A1) and estrogen sulfotransferase (EST, SULT1E1) belong to the rSULT1family that catalyzes sulfation of phenoliccompounds. Dopamine (DA) acts as a vital neurotransmitter in central nervous system(CNS) and regulates a variety of activities in periphery. In our study, we aim to detect the effects of exogenous DA and levodopa (L-DOPA) on rSULTs (rSULT1A1 and rSULT1E1) in rat liver. In order to achieve this target, varying doses of DA (0, 2, 10 and 100 mg/kg/d) and L-DOPA (0, 5, 25 and 125 mg/kg/d) were provided to male and female rats, respectively. Real-time PCR assay and western blot were used in the determination of the mRNA and protein expression of rSULTs. PNPS assay and radioactivity assay were applied to the detection of enzyme activity of rSULT1A1 and rSULT1E1, respectively. Our results showed that DA inducedthe expression and activity of rSULT1A1 in the liver of male and female rats and DA had little effect on rSULT1E1. However, L-DOPA caused no evident change of rSULT1A1 in both sex and had no significant effect on rSULT1E1 in female rat liver, but increased rSULT1E1 expression and activity only in male rat liver when administered at high dose. Our results suggest that DA plays different roles in the regulation of rSULT1A1 and rSULT1E1 when it is in periphery or in the CNS.

    Comparative study of chemical composition, antinociceptive effect and acute toxicity of the essential oils of three Asarum drugs
    Bingbing Wang, Wen Qi, Lili Wang, Deqiang Kong, Yoshihiro Kano, Jingxin Li, Dan Yuan
    2014, 23(7):  480-489.  DOI: 10.5246/jcps.2014.07.063
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    In the present study, the chemical composition, antinociceptive effect and acute toxicity of essential oils (EOs) of Asarumheterotropoides Fr. Schmidt var. mandshuricum (Maxim.) Kitag. (AHM),A. sieboldii Miq. var. seoulense Nakai (ASS) and A. himalaicum Hook. f. et Thoms. ex Klotzsch. (AH) were comparatively evaluated. A total of 55 compounds were identified in EOs of AHM, ASS andAH by GC-MS. Methyleugenol (20.16%–62.89%), safrole (2.67%-32.42%), 3,5-dimethoxytoluene (2.00%-18.59%) and eucarvone (1.52%-19.16%) were the major constituents of EO of AHM, and methyleugenol (48.35%-61.06%), eucarvone (11.13%-13.93%) and elemicin (4.79%-11.14%) were the major constituents of EO of ASS. The EO of AH was different from that of AHM and ASS, in which patchouli alcohol (27.42%-51.95%) and elemicin (13.11%-42.23%) were found in a greater amount. Moreover, the antinociceptive effect of EOs of AHM (5.5, 11.0, 16.5 μL/kg) and AH (2.0, 4.0, 6.0 μL/kg) was comparatively assayed in acetic acid-induced writhing, hot plate and formalin tests. The results indicated a weak central, but potent peripheral antinociceptive effect of EO of AHM, and more potent central and peripheral antinociceptive effect of EO of AH. The LD50 of the EOs of AHM and AH were 1.7 and 7.7 mL/kg, respectively. These findings suggest that EOs of AHM and AH possess evident antinociceptive activity and are probably safe within the range of its clinical doses. However, their chemical compositions are quite different. Therefore, AH can be clinically used as an herbal medicinal product with broad analgesic effects, but should not be confused with AHM and ASS used in traditional Chinese medicine.
    HPLC fingerprint-oriented preparative separation of major flavonoids from safflower extract by preparative pressurized liquid chromatography
    Jinfeng Chen, Pengfei Tu, Yong Jiang
    2014, 23(7):  490-495.  DOI: 10.5246/jcps.2014.07.064
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    The aim of this study was to rapidly isolate the major effective flavanoids from the extract of safflower (Carthamus tinctorius) using ODSmedium pressure liquidchromatography (MPLC) and semi-preparative HPLC, guided by a developed fingerprint. Twelve compounds were isolated and their structures were elucidated as kaempferol 3-O-β-D-rutinoside (1), kaempferol 3-O-β-D-glucoside (2), rutin (3),quercetin 3-O-β-D-glucoside (4), 6-hydroxykaempferol 3,6,7-tri-O-β-D-glucoside (5), 6-hydroxykaempferol 3-O-β-D-glucoside (6), 6-hydroxykaempferol 6,7-di-O-β-D-glucoside (7), 6-hydroxykaempferol 3-O-β-D-rutinoside (8), 6-hydroxykaempferol 3,6-di-O-β-D-glucosyl 7-O-β-D-glucuronide (9), isosafflomin C (10), safflomin C (11) and hydroxysafflor yellow A (12) by spectroscopic analysis and comparing with the literature. Our results demonstratedthat preparative pressurized liquid chromatography combined with HPLC fingerprint guide is an efficient tool to isolate the target compounds quickly.
    Flavonoids from Artemisia gmelinii Web. ex Stechm.
    Wenzhi Zeng, Quesheng, Qingying Zhang, Hong Liang
    2014, 23(7):  496-499.  DOI: 10.5246/jcps.2014.07.065
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    Phytochemical investigation of Artemisia gmelinii Web. ex Stechm. led to the isolation of 11 known flavonoids. Their structures were identified as genkwanin (1), hispidulin (2), 3'-hydroxy-genkwanin (3), chrysoeriol (4), apigenin (5), 5,7,3',4'-tetrahydroxy-6,5'-dimethoxy-flavone (6), kumatakenin (7), quercetin (8), patuletin (9), quercetagetin-3,6,7-trimethylether (10) and 7,3',4'-trihydroxy-3-methoxy-flavone (11) by spectroscopic methods. Ten compounds (2-11)were isolated from this title plant for the first time, and five compounds (3, 6, 7, 10 and 11) were isolated from genus Artemisia for the first time.

    Short communication
    Silver nitrate restores susceptibility of clinical multidrug resistant gram-negative and gram-positive bacteria to amikacin in vitro
    Cunbao Liu, Weiwei Huang, Xu Yang, Yufeng Yao, Wenjia Sun, Yanbing Ma
    2014, 23(7):  500-503.  DOI: 10.5246/jcps.2014.07.066
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    Silver nitrate could inhibit the clinical multidrug resistant isolates at high concentrations (with minimal inhibitory concentrations (MICs) from 32 µM to 64 µM).The activities of amikacin in the presence of sub-lethal silver nitrate (15 µM) were tested for the combinational effects against multidrug resistant clinical isolates in vitro. Silver nitrate restored the susceptibility of drug-resistant Acinetobacter baumannii andmethicillin-resistant Staphylococcus aureus to amikacin. It lowered the MICs of amikacin from >128 µg/mL to (2-16) µg/mL and 32 µg/mL, respectively, and lowered the MICs of amikacin on extended spectrumβ-lactamase-producing Pseudomonas aeruginosa and Escherichia coli from (16-32) µg/mL and 16 µg/mL to (<1-4) µg/mL and <1 µg/mL, respectively.

    Editor profile
    ● Introduction of Professor Guse               ● Introduction of Professor Shilin Chen
    Journal of Chinese Pharmaceutical Sciences
    2014, 23(7):  504-506. 
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