Table of Content

24 November 2014, Volume 23 Issue 11

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Contents

Journal of Chinese Pharmaceutical Sciences

2014, 23(11):  739-742. 

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Original articles

Silencing the expression and function of breast cancer resistance protein in MCF-7/MX100 cells by shRNA expressing lentivirus

Caihong Yu, Siyun Xu, Aiming Yu, Yanqing Liu, Haihong Hu, Liping Li, Lushan Yu, Hui Zhou, Huidi Jiang, Su Zeng

2014, 23(11):  743-750.  DOI: 10.5246/jcps.2014.11.094

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Overexpression of breast cancer resistance protein (ABCG2/BCRP) in cancer cells may cause tumor resistance to chemotherapeutic drugs. RNA interference (RNAi) can selectively silence the expression of a target gene of interest. In the present study, we aimed to modulate the BCRP expression and examine the functional consequence using RNAi approach. Three siRNAs (si-BCRP1, si-BCRP2 and si-BCRP3) targeting BCRP were evaluated in drug-resistant MCF-7/MX100 cells overexpressing BCRP. The BCRP expression at the mRNA and protein levels was inhibited by si-BCRP2 and si-BCRP3 over 90% and 70%, respectively. As a result, the intracellular mitoxantrone accumulation was sharply increased in MCF-7/MX100 cells after the transfection. Furthermore, shRNA sequences bearing si-BCRP2 and siBCRP3 were cloned into lentiviral expression plasmid (pTRIPZ) to package lentivirus, and MCF-7/MX100 cells stably expressing siRNA targeted to human ABCG2/BCRP were established by lentivector-mediated gene transfer system. The stable cells exhibited an increased miotxantrone accumulation, among which the BCRP expression at the mRNA level was reduced by Lenti-BCRP2 and Lenti-BCRP3 around 72% and 56%, respectively. Moreover, the BCRP expression at the protein level was reduced by 70% and 53%, respectively. Furthermore, the cell lines were used to screen active ingredients in traditional herbal medicines in order to evaluate BCRP substrates or inhibitors. Our data suggested that the BCRP knockdown cell lines could serve as good cell models for preclinical studies.



The anti-tumor efficacy of c9, t11-CLA-PTX and t10, c12-CLA-PTX on MCF-7 breast cancer cells: in vitro and in vivo

Ke Yang, Xinghuo Li, Dan Li, Xiyu Ke, Xuan Zhang, Qiang Zhang

2014, 23(11):  751-759.  DOI: R965, R943

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Considering the results of our previous research that conjugated linoleic acid mixture-paclitaxel (CLA-mixture-PTX) possesses anti-tumor activity against melanoma and brain glioma, the purpose of this study was to investigate the potential anti-tumorefficacy of cis-9, trans-11-conjugated linoleic acid­paclitaxel (c9, t11-CLA-PTX) and trans-10, cis-12-conjugated linoleic acid­paclitaxel (t10, c12-CLA-PTX) on MCF-7 breast cancer cell line in vitro and in vivo. The in vitro cytotoxicity, apoptosis induction effect and cell cycle arresting effect of c9, t11-CLA-PTX and t10, c12-CLA-PTX were investigated. The in vitro cellularuptake of c9, t11-CLA-PTX and t10, c12-CLA-PTX in MCF-7 cells were also analyzed. Besides, the anti-tumor activity of c9, t11-CLA-PTX and t10, c12-CLA-PTX was evaluated in MCF-7 tumor bearing nude mice in vivo. The in vitro cytotoxicityresults showed that the value of IC₅₀ of the t10, c12-CLA-PTX is (0.17±0.02) µM, compared with that of (1.08±0.15) µM in CLA-mixture-PTX and (6.50±1.20) µM in c9, t11-CLA­PTX treatment group (P<0.01). Both t10, c12-CLA-PTX and c9, t11-CLA­PTX increased the percentage of total apoptotic cells compared with that of control (P<0.01). And the rank of apoptosis induction efficacy was t10, c12-CLA-PTX>CLA-mixture-PTX>c9, t11-CLA­PTX (P<0.01). Compared with untreated cells, the t10, c12-CLA-PTX and c9, t11-CLA­PTX arrested cell cycle progression at the S and G₂–M phase. The amount of cellular uptake of t10, c12-CLA-PTX was significantly higher than that of CLA-mixture-PTX (P<0.01), which was significantly higherthan that of c9, t11-CLA­PTX (P<0.01). The rank of in vivo anti-tumor activity was t10, c12-CLA-PTX>CLA-mixture-PTX> c9, t11-CLA­PTX (P<0.01). In conclusion, our study demonstrated that both t10, c12-CLA-PTX and c9, t11-CLA­PTX has significant anti-tumor activity in MCF-7 cell line. And while c9, t11-CLA­PTX showed weaker inhibitory effect than CLA-mixture-PTX, stronger inhibitory effect was presented by t10, c12-CLA-PTX, which could be a promising alternative for CLA-mixture-PTX.                      



Anti-thrombotic effect of W007B, a newly synthesized compound, in vitro and in vivo

Kun Hu, Xiaoyan Liu, Yuanjun Zhu, Jingliang Zhang, Ye Liu, Yinye Wang

2014, 23(11):  760-764.  DOI: 10.5246/jcps.2014.11.096

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In the present study, we investigated anti-thrombotic effects of W007B, a water-soluble derivative of honokiol, with different models both in vitro and in vivo. Rat platelet aggregation was induced by adenosine diphosphate (ADP), thrombin, arachidonic acid (AA) and collagen in vitro. The anti-thrombotic effects were evaluated with the arterio-venous shunt model, electrode-stimulated carotid thrombosis model in rats and ADP-induced acute pulmonary embolic model in mice. The bleeding time in vivo was examined with tail incision in mice. W007B inhibited ADP-, thrombin-, collagen- and AA-induced platelet aggregation in a concentration-dependent manner, with an IC₅₀ value of899.5 μM, 212.9 μM, 266.0 μM and 52.5 μM, respectively. In vivo, W007B (2–10 mg/kg, ig) significantly reduced the thrombus weight in the model of arterio-venous shunt. Besides, W007B could effectively prolong the occlusion time in the electrode-stimulated carotid thrombosis model. Moreover, in the ADP-induced acute pulmonary embolism model in mice, 2.8–14 mg/kg of W007B significantly reduced the death of mice. In conclusion, W007B is effective on platelet aggregation, and it is most sensitive on AA-induced aggregation. W007B has potent anti-thrombotic effect on different arterial thrombosis models. It may be an orally active candidate of anti-thrombotic agents.



Synthesis and cytotoxic evaluation of hybrids of indolin-2-one and quinazoline-4(3H)-one linked via carbon-carbon double bond

Boying Shi, Jingjing Zhang, Shengli Cao, Man Gao, Panpan Ding, Zhongfeng Li, Ji Liao, Xingzhi Xu

2014, 23(11):  765-771.  DOI: 10.5246/jcps.2014.11.097

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A novel series of compounds combining indolin-2-one and quinazolin-4(3H)-one moietyvia a carbon-carbon double bond were synthesized by aldol-condensation of 2-methylquinazolin-4(3H)-one-6-carbaldehyde with various indolin-2-ones. The synthesized compounds were evaluated for their cytotoxic activity against five human cancer cell lines, namely, A549, MCF-7, HeLa, HT-29 and HCT-116. We found that compound 5e with two bromine atoms at the 5- and 7-positions of the indolin-2-one ring was most potent, which inhibited proliferation of five cancer cell lines in the range of32.0%–62.3% at a concentration of 50 µM. Our results further indicate that the connection of 5,7-dibromoindolin-2-one and 2-methylquinazolin-4(3H)-one moiety witha carbon-carbon double bondis essential for compound 5e to exert cytotoxicity.



The involvement of signaling activation of protein kinase C in gadolinium chloride-induced cell survival and cell cycle progression in NIH3T3 cells

Min Feng, Jinxia Li, Xiaojie Ma,Yunzhou Fan, Jingxuan Wu, Qun Zeng, Xiaogai Yang

2014, 23(11):  772-777.  DOI: 10.5246/jcps.2014.11.098

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In the present study, we investigated the activation of protein kinase C (PKC) family in mouse embryonic fibroblast NIH3T3 cells using gadolinium chloride as a representative lanthanide ion. With live cell imaging system and confocal laser scanning microscopy, we found that the treatment of 50 μM GdCl₃ promoted cell survival under the condition of serum-starvation. Moreover, better cell attachment and cytoskeleton reorganization were also observed. Additionally, GdCl₃ treatment resulted in the phosphorylation of PKC family at different time points. Furthermore, bisindolylmaleimide (a PKCpan inhibitor) could efficiently reduce the level of phosphorylated PKCpan (βII^Ser660), alleviating ERK activation induced by GdCl₃. This finding indicated that the PKC activation was involved in GdCl₃-induced MAPK/ERK signaling and thus might contribute to GdCl₃-induced cell cycle progression and cell survival.



Chemical constituents from the leaves of Ilex asprella (Hook. et Arn.) Champ. ex Benth.

Chao Wang, Jun Li, Pengfei Tu

2014, 23(11):  778-782.  DOI: 10.5246/jcps.2014.11.099

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Phytochemical investigation of the leaves of Ilex aspralla (Hook. et Arn.) Champ. ex Benth. led to the isolation of eleven compounds (1-11). By comparison with those reported data in the literatures their structures were identified as kaempferol-3-O-β-D-6′′-acetylglucopyranoside (1), kaempferol-4′-methylether (2), quercetin (3), quercetin-3-O-glucopyranoside (4), tormentoside (5), suavissimoside R₁ (6), 3β,19α-dihydroxyolean-12-ene-24,28-dioicacid-28-O-β-D-glucopyranoside (7), 3-O-β-sulfooxy-19-hydroxy-urs-12-ene-28-oic acid (8), coniferin (9), adenoside (10), 1′-O-benzyl-α-L-rhamnopyranosyl-(1′′→6′)-β-D-glucopyranoside (11). Among these, six compounds (1, 2, 5, 9-11) were firstly reported from the genus Ilex, and five compounds (3, 4, 6-8) were isolated for the first time from Ilex aspralla.



High-performance liquid chromatographic fingerprint analysis of Oxytropis falcata Bunge and Oxytropis chiliophylla Royle

Kelsang Norbo, Quesheng, Kelsang Padro, Xiaojing Zhang, Samnor, Hong Liang, Qingying Zhang

2014, 23(11):  783-789.  DOI: 10.5246/jcps.2014.11.100

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A simple, sensible and reliable HPLC-DAD fingerprint analysis method for the raw materials ofOxytropis falcata and Oxytropis chiliophylla, both of which were used as “Er-Da-Xia” in Tibetan medicines, was developed and then subsequently applied to analyze samples collected from different locations or times. 19 common fingerprint peaks for O. falcata, 24 for O. chiliophylla, and11 for the two herbs were designated respectively, including 7 identified characteristic peaks existing in both herbs and 1 uniquely presenting in O. chiliophylla. Although there were some slight differences in the chemicals of O. falcata and O. chiliophylla, the main components of both herbs were consistent generally. The resultsprovided scientific basis, at least from the chemical point of view, for the reasonablity of two herbs being used as the same drug in Tibetan medicines and for the necessary of further investigation on their detailed chemical and pharmacological differences.



Formulation and characterization of extruded and spheronized pellets using pectin and crosslinking agents

Pallavi M. Chaudhari, Pravin D. Chaudhari

2014, 23(11):  790-798.  DOI: 10.5246/jcps.2014.11.101

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The aim of this study was to prepare pellets of gliclazide by extrusion spheronization process by use of two methods in situ cross linking method and interfacial complexation method and to study the effect of different cross linking agents on the formed pellets. Extrusion/spheronization being an established technique for producing spherical pellets so this technique was used to prepare pellets. The gliclazide pellets prepared by extrusion-spheronization techniques and then the formed pellets were coated with pectin solution by interfacial complexation method. The effect of cross-linkers calcium chloride and aluminium chloride concentration, by in situ cross linking on properties of gliclazide pellets like swelling and drug release were studied. The formed pellets were subjected to swelling, analysis of morphology, in dissolution and vivo studies. Most of the pellets were of acceptable shape. From the results calcium chloride when coated with pectin, retarded drug release. As the concentration of calcium chloride increased, it led to slow release of the drug. This may be due to the water solubility of calcium salt, which induced cross linking with pectin. Thus pellets with calcium chloride cross linked with pectin were beneficial, because it retarded the release of the drug. Though the release from interfacial coated pellets was retarded, it was less as compared to the in situ formed pellets. The in vivo studies on alloxan-induced diabetic rats indicated the significant hypoglycemic effect that was observed 24 h after oral administration of optimized pellets. Thus, the developed and optimized pellets were suitable for prolonged systemic absorption of gliclazide to maintain lower blood glucose level and improved patient compliance. The results suggested that the in situ cross linking pellets were able to retard the release of gliclazide greater than the interfacial complexation method. Therefore, this approach has been effectively achieved.



Short communication

Age, gender and type 2 diabetes contribute to the risk of gastric cancer: a retrospective single institution analysis

Zeng Wang, Xinjun Cai, Mengjuan Liu, Hongyang Lu, Nengming Lin

2014, 23(11):  799-803.  DOI: 10.5246/jcps.2014.11.102

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Diabetes is involved in the development of several cancers. However, whether type 2 diabetes mellitus (T2DM) as well as other potential risk factors are related to gastric cancer (GC) remains unclear. In this study, 1320 patients with gastric cancer (gastric cancer group) and 1252 thyroid nodule patients (control group), who were admitted in our hospital from Jan 2010 to Dec 2012, were analyzed in a case-control study. Logistic regression analysis was applied to evaluate the risk of diabetes condition, gender, age, body-mass index (BMI) level and other factors for GC. There were 416 patients with DM in the gastric cancer group (31.5%) and 120 patients with DM in the control group (9.6%). The differences between the two groups were significant (P = 0.000). Compared with the control group, the logistic regression analyses suggested that male patients had a higher risk of GC. Moreover, older individuals (especially over 65 years) were more susceptible to GC, and as for T2DM, it was found to be associated with GC, that is, the incidence in the gastric cancer group was significantly higher than in the control group. The OR values of age, T2DM, gender and BMI were 16.951, 15.130, 2.658 and 0.224, respectively. In conclusion, age, gender and T2DM are the risk factors of gastric cancer. Furthermore, male patient over 65 years with T2DM is susceptible to GC, and T2DM is the risk factor only second to age, and there might be synergistic effects among these factors.



Editor profile

Introduction of Professor Su Zeng

Journal of Chinese Pharmaceutical Sciences

2014, 23(11):  804-805. 

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Introduction of Professor Gang Liu

Journal of Chinese Pharmaceutical Sciences

2014, 23(11):  806-806. 

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Others

Ebola virus disease

Media Centre http://www.who.int/mediacentre/factsheets/fs103/en/

2014, 23(11):  807-808. 

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Journal of Chinese Pharmaceutical Sciences attended the 10th China Science Journal Development Forum

Journal of Chinese Pharmaceutical Sciences

2014, 23(11):  809-809. 

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The 10^th China Science Journal Development Forum was held in Guangzhou on Nov 13^th to 14^th, 2014. The theme of this forum was “the development of sci-tech journals in deepening reform”. Jinghai Li, the vice chairman of China Association for Science and Technology, vice-president of Chinese Academy of Sciences and academician of China Academy of Science; Xiong Lin, the head of the United Front Work Department and committee member of Guangdong Provincial Party, provided the policy for the future Domestic and international participants gathered, discussing various topics of policy and development orientation of China sci-tech journals. Associate Prof. Heqing Huang, executive associate editor-in-chief of Journal of Chinese Pharmaceutical Sciences (JCPS) attended the Forum.development of sci-tech journals.



Executive associate editor-in-chief of Journal of Chinese Pharmaceutical Sciences attending the 18th Conference of Chinese University Science and Technology Journal Council and receiving the award

Journal of Chinese Pharmaceutical Sciences

2014, 23(11):  810-810. 

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The 18^th Conference of Chinese University Science and Technology Journal Council was held in Guangzhou on Nov 11^th–12^th, 2014. More than 400 participants gathered, and the executive associate editor-in-chief of Journal of Chinese Pharmaceutical Sciences (JCPS), associate Prof. Heqing Huang attended the conference.

Several leaders, such Jiansheng Liu, vice Minister of Publications Department of Chinese Propagandizing Department; Runsheng Gao, deputy Director-general, Technology Department of Ministry of Education, attended the conference and made wonderful presentations.

Vice Minister Jiansheng Liu made an important speech of “several questions of the reform on sci-tech journals sponsored by universities”. He said, under the leadership of Society of China University Journals (SCUJ), editors of sci-tech journals have achieved remarkable results on academic activities, training business, improvement of academic quality, strengthen international cooperation, and expanding the impact of sci-tech journals, which played a big role on the developing of Chinese university sci-tech journals and promoting the subject construction and personnel training in colleges and universities. These presentations promoted information exchanges, found out the cooperative opportunities, and deepened understanding as well as enhanced work relationship between each other.

The executive associate editor-in-chief of JCPS, associate Prof. Heqing Huang attended the conference, and received the award “2014 Excellent Editor-in-Chief of Chinese University Medical Journals”. In 2013, JCPS has received the support of “the International Influence of Chinese Science and Technology Journals Promotion Plan C class”. In 2014, JCPS has also received the support of “Chinese University Quality Science and Technology Journals Project”. At present, this project is well on the way.