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Thrombolysis of plasmin and its derivatives:research advances

Journal of International Pharmaceutical Research.2014;(3):296-300. doi:10.13220/j.cnki.jipr.2014.03.010

All of the thrombolytic agents currently approved for use in humans are plasminogen activators, the application of which is limited by bleeding complications at vascular injury sites and plasminogen content in the thrombus. Plasmin is rapidly neutral-ized in the circulation by α2-antiplasmin and tolerated without bleeding. With the application of catheter-based delivery, the unique bio-chemical properties of plasmin make it a safe and effective direct fibrinolytics. Plasmin derivatives, including miniplasmin,Δ-plasmin and microplsmin, display more thrombolysis efficacy and better hemostatic safety in preclinical study and clinical trials. This review sum-marizes the current information on plasmin and its derivatives, including the advances on biochemical properties, preclinical and clinical trials.

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Competitiveα-amino-3-hydroxyl-5-methyl-4-isoxazole propionic acid receptor antagonists:research advances

Dian XIAO ; Lingxiao WANG ; Xinbo ZHOU ; Song LI

Journal of International Pharmaceutical Research.2014;(4):407-412. doi:10.13220/j.cnki.jipr.2014.04.04

α-Amino-3-hydroxyl-5-methyl-4-isoxazole propionic acid (AMPA) receptor, a subtype of ionotropic glutamate receptors widely distributed in the central nervous system, mediates the fast excitatory neurotransmission. Meanwhile more and more evidence indicates that AMPA receptor plays an important role in synaptic plasticity as well as central sensitization, and it also has close relationships with nervous system diseases. Over stimulation of AMPA receptor would produce excitotoxicity, leading to neuronal damage and finally resulting in a multitude of nervous system diseases, such as epilepsy, amyotrophic lateral scelerosis,Parkinson′s dis-ease. Competitive AMPA receptor antagonists that downregulate AMPA receptor′s function are of great importance in the prevention and treatment of nervous system diseases. This article reviews the research advances of competitive AMPA receptor antagonists.

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Overviews and analysis of the U.S. FDA′s new approvals in 2014 first half year

Zhongming TANG

Journal of International Pharmaceutical Research.2014;(4):493-502. doi:10.13220/j.cnki.jipr2014.04.020

In the first half of 2014, the U.S. Food and Drug Administration (FDA) approved 46 new drugs, including 10 new molecular entities and 10 new biologic license applications. According to the prescription information for professionals, this article introduces the description, mechanism of action and clinical studies, briefly describs the box warning, indications and usage, dosage and administration, dosage form and strength, contraindications, warning and precautions, adverse reactions, drug interaction and use in special population of these new drugs. In addition, the “first events” in the history of new drug research, development and approval are also discussed.

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Galloyl glucosidic constituents of Choerospondias axillaries and their in vitro anti-tumor, anti-hypoxia and anti-bacteria activities

Changwei LI ; Chengbin CUI ; Bing CAI ; Bing HAN ; Mingming LI ; Ming FAN

Journal of International Pharmaceutical Research.2014;(4):449-455. doi:10.13220/j.cnki.jipr2014.04.012

Objective To investigate gallic acid-derived chemical constituents of Choerospondias axillaries (Roxb.) Burtt. et Hill., and evaluate their in vitro anti-tumor, anti-hypoxia and anti-bacteria activities. Methods The aimed chemical constituents were isolated by various chromatographic means, and their structures were identified by physicochemical and spectroscopic data. MTT method was employed to evaluate anti-tumor and anti-hypoxia activities. Antibacterial activities were tested by paper disc method. Results Seven compounds 1-7 were isolated from the stem barks of Choerospondias axillaries (Roxb.) Burtt. et Hill. and identified as gallic acid(1), gallic acid ethyl ether(2), 1-O-galloyl-β-D-glucose(3), 1,6-di-O-galloyl-β-D-glucose(4), 1,4-di-O-galloyl-β-D-glucose(5), 1,4,6-tri-O-galloyl-β-D-glucose(6), and 1,3,4,6-tetra-O-galloyl-β-D-glucose(7). Compounds 1, 2 and 4-6 significantly inhibited K562 cells with the IC50 values of 2.9, 14.6, 39.1, 40.2, 41.2 μg/ml, respectively, and 3 and 7 also showed a slight inhibition of the K562 cells with the inhibition rate of 20.8% and 30.1% at 100 μg/ml respectively. Compounds 1-7 showed protective effects on anoxia-induced injury in cultured ECV304 and PC12 cells at the concentrations showing no significant cytotoxicity, and 5-7 also showed an antibacterial effect on Staphylococcus aureus ATCC6538 to a certain extent. Conclusion Compounds 2-7 were isolated from the genus Choerospondias for the first time. It was the first time to report 1-7 as anti-tumor and anti-hypoxia constituents of Choerospondias axillaries, and the anti-hypoxia activity for 1-7 was also recorded for the first time in the present study.

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Main biologics for anti-autoimmune disease:research advances

Weihua HOU ; Wei MO ; Min YU

Journal of International Pharmaceutical Research.2014;(4):424-428. doi:10.13220/j.cnki.jipr2014.04.007

Immune system is a security guard to help human body repel or remove bacteria, viruses, parasites and other fore-ign invaders .But when some tissue components or the immune system itself become abnormal, it can not distinguish friend from foe accurately and may attack our own tissue then cause some clinical symptoms, leading to autoimmune diseases. Nearly 5 % of the world's population suffer from various autoimmune diseases. By now in addition to control the formation of autoantigens such as infection,tiredness, the main biologics used in clinic are immunoregulators to block pathological autoimmune response and then to create a new proper immune response. Recently, new biologics to treat autoimmune disease come into being one after another, and this article gives a brief overview about research progress in anti-autoimmune disease biologics.

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Physicochemical properties of a polysaccharide RAP-B-1 from Rubus amabilis and its immunomodulating effects

Yulin DIAO ; Hao MA ; Jinwei REN ; Guiqiang ZHANG ; Shuai LI ; Junjie SHAN ; Bin LIU

Journal of International Pharmaceutical Research.2014;(4):461-467. doi:10.13220/j.cnki.jipr2014.04.014

Objective To investigate the physicochemica l properties and immunobiological activity of a polysaccharide (RAP-B-1) from stems of Rubus amabilis. Methods The crude polysaccharide (RAP) was obtained successively by boiling, ethanol precipitating and dialyzing. RAP was isolated with DEAE-cellulose and Sephadex G-100 to obtain a polysaccharide RAP-B-1. The physicochemical properties of RAP-B-1 were studied by hydrolysis, periodate oxidation, Smith degradation and methylation, CE, IR, NMR and GC-MS. The immunobiological activities were estimated by the proliferative activity of spleen lymphocytes and phagocytic activity of peritoneal macrophages in mice. Results The molecular weight of RAP-B-1 was 4.80×104 with specific optical rotation value [α] 20D+68.3 (c=1,H2O), and was composed of eight monosaccharides. The molar ratios were as Xyl: Ara: Glc: Rha:Gal: Man: GlcA: GalA = 1.0:6.9:0.8:1.1:6.9:0.3:0.5:3.3. RAP-B-1 was an arabinogalactan. The linkages of arabinose were →1) Ara (2,3→,→1) Ara(5→and→1) Ara, and the linkages of galactose were→1) Gal(4→,→1) Gal(6→and→1) Gal. RAP-B-1 could improve the proliferative activity of spleen T cells(P<0.05) and booste phagocytic activity of peritoneal macrophages at 50μg/ml concentration(P<0.01). Conclusion RAP-B-1 is an arabinogalactan and has immunobiological activity.

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Establishment of LC-MS/MS method for the determination of forsklin in rat plasma and its pharmacokinetics

Dianwei SONG ; Decai WANG ; Zhiyun MENG ; Ruolan GU ; Meihui SHI ; Zhuona WU ; Jingze WANG ; Guifang DOU

Journal of International Pharmaceutical Research.2012;(2):149-153. doi:10.3969/j.issn.1674-0440.2012.02.010

Objective To develop a sensitive liquid chromatography-tandem mass spectrometric (LC-MS/MS) method for the determination of forsklin in rat plasma.Methods After extraction with methyl tert-butyl ether,chromatographic separation was performed on a C18 column with the mobile phase consisting of water ( 0.1％ formic acid)-acetonitrile in a gradient elution mode.A tandem mass spectrometer equipped with electrospray ionization (ESI) source was used as detector in the positive ion mode.Quantification was performed using multiple reaction monitoring (MRM) with the precursor product combination ions of m/z 411→375.3 and 285→193 for forsklin and diazepam.Results Good linearity was obtained in the 0.5-1000 ng/ml range for the analyte and the analytical method was validated in terms of specificity,precision,accuracy,recovery,stability and matrix effect.These assays gave RSD values always lower than 14.4％ and RE values between -3.5 ％ and 3.8％.In addition,the specificity,extraction recovery,stability and matrix effect were satisfactory.Conclusion Due to its high sensitivity,specificity and simplicity,the method could be used for pharmacokinetic studies of forsklin.

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Determination of aconitine in dog tissue homogenates by HPLC-MS/MS and its application to in vitro metabolic stability study

Cuiping YANG ; Sha LIAO ; Tianhong ZHANG ; Jinglai LI ; Xiaoying WANG ; Jinxiu RUAN ; Zhenqing ZHANG

Journal of International Pharmaceutical Research.2012;(3):256-260. doi:10.3969/j.issn.1674-0440.2012.03.015

Objective To develop a HPLC-MS/MS method for the determination of aconitine and study thein vitro metabolic stability of aconitine in dog tissue homogenates.Methods The chromatographic separation was performed on a C18 column.The mobile phase consisted of acetonitrile and water with 0.2％ formic acid and 5 mmol/L ammonium acetate.A triple quadrupole tandem mass spectrometer equipped with an electrospray ionization interface source was used for the quantitative determination in the positive selective reaction monitor mode.Aconitine was incubated with dog tissue homogenates and samples were withdrawn at different time points and precipitated by acetonitrile with internal standards citalopram.Results Aconitine showed good linear relationship over the range from 5 to 500 ng/ml.The recoveries of aconitine were between 85.73％ and 92.12％ at three QC concentration levels.The intra- and inter-day precisions were 5.32％ - 8.95％ and 5.45％ - 8.86％,respectively.After incubation,about 20％ of aconitine were cleared in the liver and small intestine,and t1/2 were 460.6 and 521.3 min,respectively.But none was metabolized in the stomach and kidney.Conclusion These results demonstrated that aconitine was mainly metabolized in the liver and small intestine at a slow rate.

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Pulsatile delivery pellets:research advances

Hang FENG ; Ying LI ; Xingguo MEI

Journal of International Pharmaceutical Research.2015;(4):483-487. doi:10.13220/j.cnki.jipr.2015.04.010

Under physiological conditions, many vital functions of the body are controlled by transient release of bioactive substances at a specific time and site. Based on the circadian rhythm character of disease and chronotherapeutic conceptions, pulsatile delivery system has been designed to achieve optimal therapeutic effect and reduce the toxic and side-effect. In recent years, more and more studies are focused on the pulsatile multiparticulate drug delivery system. Pulsatile multiparticulate system possesses many benefits, such as no risk of dose dumping, predictable gastric emptying, flexible release patterns and increased bioavailability. Based on these premises, the aim of this review is to summarize the major design methods of pulsatile multiparticulate and the research progress.

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Techniques and strategies for characterization and isolation of chemical components of traditional Chinese medicines

Baiping MA ; Liping KANG ; Xu PANG ; Renyi YAN

Journal of International Pharmaceutical Research.2015;(4):413-426. doi:10.13220/j.cnki.jipr.2015.04.001

The chemic al composition of traditional Chinese medicine (TCM) is the material base for its prevention and treatment of disease. Characterization, analysis and isolation of chemical constituents, important fields of modern research on TCM, however, are still a great challenge due to the complexity. In recent years, considerable progress has been made in these fields with the application of new chromatographic packing materials and methods, analysis technologies represented by LC-MS and the associated databases and softwares. Here, the advancement of methods and strategies used in the research on the chemical constituents of TCM is briefly reviewed.

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