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Early determination of quality fluctuation of herbal injection by chromatographic coupled with biothermodynamic fingerprinting

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Early determination of quality fluctuation of herbal injecti...

第十一届全国青年药学工作者最新科研成果交流会

作者： Dan Yan a,Yong-shen Ren a,b,Ping Zhang a,c,Jia-bo Wang a,Xiao-xi Du d,Xiao-he Xiao a a Military Institute of Chinese Materia Medica,302th Military Hospital of china,beijing 100039,china b College of Pharmacy,Chengdu University of Traditional Chinese Medicine,Chengdu 610075,china c Postgraduate Team,Military Medical Postgraduate School of china,beijing 100853,china d Center for drug Reevaluation,State food and drug Administration,beijing 100045,china

Herbal injection is one of the most powerful preparations of modern Traditional Chinese Medicine;however the quality control of it is fairly difficult for their complicated ***,chromatographic fingerprint（CF） has been recommended as a potential strategy for the quality control of herbal injection,nevertheless there are still various substances absent from the inspection of chromatographic method for no spectrum absorption,which might cause grievous drug-induced *** establish a comprehensive and early prediction security control process,biothermodynamic fingerprint（BF） was adopted as a complement for CF to detection the quality fluctuation of herbal injection from both chemical and bioactive *** this work,Yinzhihuang Injection（YZHI） was selected as a representative of herbal injection,10 batches of normal samples and 6 batches of artificial abnormal samples were collected,high performance liquid chromatography and Thermal Active Monitor were applied to develop their CF and BF *** results showed that the CF and BF of normal samples were similar with good stability and consistence;however the abnormal samples deviated from *** abnormal samples could be correctly distinguished when coupled CF with BF,the recognition ratio was higher than CF and BF respectively,and the key factors of quality fluctuation extent could be ordered as bacterial contamination,high temperature,lighting and sterilizing *** established method could be used for early prediction adverse drug events,which would be potentially helpful to improve the safety level of herbal injection in clinical application.

关键词： herbal injection Yinzhihuang Injection quality fluctuation chromatographic fingerprinting biothermodynamic fingerprinting

I-Stepholidine increases the frequency of sEPSC via the activation of D1 dopamine signaling pathway in rat prelimbic cortical neurons

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Acta Pharmacologica Sinica 2007年第5期 627-633页

作者： Ming GAO Chang-liang LIU Shen YANG Xue-chu ZHEN Guo-zhang JIN Department of Pharmacology,State Key Laboratory of drug Research,Institute of Materia Medica,Shanghai institutes for Biological Sciences,Chinese Academy of Sciences,Shanghai 201203,china

Aim:To investigate the effect of l-stepholidine (SPD) on the frequency of spon-taneous excitatory postsynaptic currents (sEPSC) in the pyramidal cells betweenlayers Ⅴ and Ⅵ in the prelimbic cortex (PL).Methods:A whole-cell patch clamp inrat brain slices was ***:SPD significantly increased the frequency ofsEPSC in a concentration-dependent manner.A selective D1dopamine receptorantagonist SCH23390 blocked SPD-mediated effects,whereas the D1agonistSKF38393,but not the D2/3antagonist sulpiride,mimicked SPD-mediated increasein the frequency of ***,both protein kinase A (PKA) inhibitor N-(2-[p-bromocinnamylamino]-ethyl)-5-isoquinolinesulfonamide hydrochloride andprotein kinase C (PKC) inhibitor chelerythrine attenuated the effect of SPD ***:SPD elicits its effect on the frequency of sEPSC on the PLpyramidal cells via presynaptic D1receptors,and is dependent on PKA and PKCsignaling pathways.

关键词： l-stepholidine prelimbic cortex whole-cell patch clamp spontaneous excitatory postsynaptic currents dopamine receptor

Biphasic firing response of nucleus accumbens neurons elicited by THPB-18 and its correlation with DA receptor subtypes

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Acta Pharmacologica Sinica 2004年第12期25卷 31-39页

作者： Yu FU2,3,4, Zi-tao ZHU2,5, Xing-zu ZHU2, Guo-zhang JIN2,6 2State KeyLaboratory of drug Research,Shanghai Institute ofMateria Medica, Shanghai institutes for BiologicalSciences, ChineseAcademy of Sciences, Graduate Schoolof the Chinese Academy of Sciences, Shanghai 201203, chinaNow in Department of Pharmacology and Toxicology, Univer-sity of Texas Medical Branch, USA.Now in Department of Physiology & Pharmacology, OregonHealth Sciences University, USA,5Now in Department of Physiology & Pharmacology, OregonHealth Sciences University, USA, State Key Laboratory of drug Research Shanghai Institute of Materia Medica Shanghai Institutes for Biological Sciences Chinese Academy of Sciences Shanghai 201203 China

AIM: To investigate the possibility whether THPB-18 (l-12-shloroscoulerine) possesses the D1 agonist-D2 antago- nist action on meso-accumbens-mPFC DA system. METHODS: Single unit spontaneous firing activity was re- corded in the nucleus accumbens (NAc) neurons of na?ve and unilateral-6-hydroxydopamine (6-OHDA)-lesioned Sprague-Dawley rats. The effects of drugs applied intravenously or iontophoretically were determined by the change of firing rates. RESULTS: Under normal conditions, the systemic administration of THPB-18 produced a decrease-increase biphasic firing pattern in the NAc neurons during cumulative doses. High dose of THPB-18 was capable of reversing the inhibition induced by both D2 agonist LY171555 and D1/D2 agonist APO on NAc firing activity. Spiperone pretreatment could not block the high dose of THPB-18-induced firing rate increase, which was reversed by the D1 selective antagonist SCH23390. The tested NAc neurons were effectively inhibited by iontophoretically applied THPB-18 in 90 % of 6-OHDA-lesioned rats, while THPB-18 caused variable effects on the firing of NAc neurons in the neurons of unlesioned rats. The inhibitory effect of THPB-18 was blocked by iontophoretic application of SCH23390, but not D2 antagonist spiperone. CONCLUSION: Similar to l-stepholidine, THPB-18 also possesses the “D1 agonistic-D2 antagonistic” dual action on the VTA-NAc DA system.4Now in Department of Pharmacology and Toxicology, Univer-sity of Texas Medical Branch, USA.5Now in Department of Physiology & Pharmacology, OregonHealth Sciences University, USA,4Now in Department of Pharmacology and Toxicology, Univer-sity of Texas Medical Branch, USA.5Now in Department of Physiology & Pharmacology, OregonHealth Sciences University, USA,5Now in Department of Physiology & Pharmacology, OregonHealth Sciences University, USA,

关键词： berberine dopamine D1 receptors dopamine D2 receptors nucleus accumbens

Triptolide suppresses CD80 and CD86 expressions and IL-12 production in THP-1 cells

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Acta Pharmacologica Sinica 2005年第2期26卷 223-227页

作者： Jing LIU,Qing-li WU,Yong-hong FENG,Yi-fu YANG,Xiao-yu LI,Jian-ping ZUO~2State Key Laboratory of drug Research,Shanghai Institute of Materia Medica,Shanghai institutes for Biological Sciences,Chinese Academyof Sciences,Shanghai 201203,china StateKeyLaboratoryofdrugResearch ShanghaiInstituteofMateriaMedicaShanghaiInstitutesforBiologicalSciencesCh

Aim:To investigate the effects of triptolide,a diterpenoid triepoxide fromTripterygium wilfordii Hook F(TWHF),on the co-stimulatory molecule expres-sion and interleukin-12(IL-12)production from THP-1 ***:THP-1 cellswere differentiated into macrophage-like cells by Me2SO,and then cultured withIFN-γ(500kU/L)and lipopolysaccharide(LPS)(1mg/L)with or without *** surface molecule expressions were analyzed on a FACScan flow ***-12p40,IL-12p70 were assayed by ***:Tripolide suppressed CD80and CD86 expressions on IFN-γ(500kU/L)and LPS(1mg/L)activated THP-1 cellsat nontoxic dosages of 2.5-0.625μg/***,the production of IL-12p40and IL-12p70 were also significantly reduced in THP-1 cells exposed to ***:Triptolide impairs the antigen-presenting function by inhibiting CD80and CD86 expressions and decreased IL-12p40 and IL-12p70(bioactive form)pro-ductions from the activated THP-1 cells.

关键词： triptolide CD80 antigens CD86 antigens interleukin-12

Anticonvulsant effect of BmK IT2,a sodium channel- specific neurotoxin,in experimental epilepsy models of rats

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Anticonvulsant effect of BmK IT2,a sodium channel- specific ...

中国神经科学学会第四次会员代表大会暨第七届全国学术会议

作者： Rong ZHAO~1,Xu-Ying ZHANG~(1,3),Jun YANG~2,Chun-Chun WENG~2,Jian-Wei ZHANG~2,Yong-Hua JI~(1,2) 1 Institute of Physiology,Shanghai institutes for Biological Sciences,Chinese Academy of Sciences,Shanghai 200031, china 2 School of Life Sciences,Shanghai University,Shanghai 200444,china 3 Membrane Signaling Group,Laboratory of Neurobiology,national Institute of Environmental Health Sciences,national institutes of Health,Research Triangle Park,NC 27709,USA

＜正＞In the present study,the anticonvulsant effect of BmK IT2,a sodium channel-specific polypeptide purified from the venom of Chinese scorpion Buthus martensi Karsch,has been investigated in experimental epilepsy models of rats. BmK IT2 significantly inhibited pentylenetetrazol-induced generalized seizures in behavior and electroencephalograph （EEG） by unilateral injection into CA1 region of *** addition,the latency to status epilepticus onset induced by pilocarpine was prolonged by BmK IT2 ***,the hippocampal c-Fos expression during status epilepticus were suppressed by BmK IT2 compared to *** optimal doses of BmK IT2 were 0.1μg and 0.5μ*** results indicate that BmK IT2 has significant anticonvulsant properties on pentylenetetrazol-induced generalized seizures and pilocarpine-induced status epilepticus,providing a potential new antiepileptic drug（AED） in the therapy of epilepsy.

关键词： BmK IT2 Intrahippocampal injection Status epilepticus Seizures Voltage-gated sodium channels

Transgenic Animal Mutation Assays

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Transgenic Animal Mutation Assays

中国毒理学会第四届全国学术会议

作者： Tao Chen, Ph.D. D.A.B.T. ( national Center for Toxicological Research, US food and drug Administration, Jefferson, AR 72079)

＜正＞The novel transgenic mouse and rat mutation assays have provided a tool for analyzing in vivo mutation in any tissue, thus permitting the direct comparison of cancer incidence with mutant frequency. In these systems, the chromosomally-integrated foreign genes are used as the targets for mutations. Following recovery of the transgenes from the tissues of choice, the target DNA can be assayed in vitro to identify and quantity mutations produced in vivo. There is a great progress in the development, validation, and use of transgenic in vivo mutation models. Although there are several transgenic animal assays for testing mutagenicity, I will mainly discuss two systems: Big Blue rodent model and Muta Mouse model because the database for other

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Molecular biology evaluation of Polyacrylamide Hydrogel using real time PCR

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Molecular biology evaluation of Polyacrylamide Hydrogel usin...

第2届世界华人生物医学工程研讨会

作者： Chengxiang Fan1 Tingfei Xi1 a Ziyi Wan2 Xixiong Kang3 Yajie Wang3 Chunren Wang1 1. Center for Medical Devices national Institute for the control of Pharmaceutical & Biological Products beijing 100050 P.R.china 2. School of Materials Science and Engineering beijing Institute of Technology beijing 100081 P.R.china 3. Titan Hospital Capital University of Medical Science beijing 100050 P.R.china a

Polyacrylamide Hydrogel, which is widely used in ophthalmic operations, drug treatment, food packaging products, and water purification etc, is a watery gel consisting of approximately 2.5% cross-lin

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Purification and Characterization of Alginate Lyase from Marine Vibrio ***

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Acta Biochimica et Biophysica Sinica 2006年第9期38卷 633-638页

作者： Yuan-Hong WANG* Guang-Li YU Xin-Min WANG Zhi-Hua LV Xia ZHAO Zhi-Hong WU Wei-Shang JI Marine drug and food Institute,Key Laboratory of Marine drugs of Shandong Province,Key Laboratory of Marine drugs,Ministry of Education,Ocean University of china,Qingdao 266003,china Marine drug and food Institute Key Laboratory of Marine Drugs of Shandong Province Key Laboratory of Marine Drugs Ministry of Education Ocean University of China Qingdao 266003 China. yhwang@***

Extracellular alginate lyase secreted by marine Vibrio ***,isolated from decayedLaminaria japonica,was purified by a combination of ammonium sulfate precipitation and diethylaminoethyl-Sephacel column *** results show that the molecular mass of alginate lyase wasapproximately 62.5 kDa,with an optimal pH and temperature at pH 7.0 and 25℃,*** wasapproximately 72.73 g/*** activity of the enzyme was enhanced by EDTA and Zn2+,but inhibited by Ba2+.The substrates specificity analysis shows that it was specific for hydrolyzing poly-β-D-1,4-mannuronate inalginate.

关键词： marine Vibrio alginate alginate lyase purification characterization

Pharmacokinetic,pharmacodynamic,and efficacy profiles of ergosta-4,6,8(14),22-tetraen-3-one,a natural product with diuretic activity from Polyporus umbellatus

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Pharmacokinetic,pharmacodynamic,and efficacy profiles of erg...

中药与天然药高峰论坛暨第十二届全国中药和天然药物学术研...

作者： Ying-Yong Zhao~(a,*),Xian-Long Cheng~b,Feng Wei~b,Rui-Chao Lin~b,Shuang-Cheng Ma~(b,*) a Key Laboratory of Resource Biology and Biotechnology in Western china,Ministry of Education, the College of Life Sciences,Northwest University,No.229 Taibai North Road,Xi’an,Shaanxi 710069,P.R china b Institute for the control of Chinese Traditional Medicine and Ethnic Medicine,national Institute for food and drug Cotrol,beijing 100050,P.R.china

The aim of the present study was to characterize the pharmacokinetic, pharmacodynamic,and efficacy profiles of ergosta-4,6,8(14),22-tetraen-3-one(ergone)from Polyporus *** pharmacokinetic study was carried out to determine plasma concentration of ergone in rats after oral administration at a dose of 20 mg/*** amount of ergone in plasma was measured by HPLC/*** pharmacodynamic study was carried out to evaluate the diuretic effects after oral/intraperitoneal adrninistration of 2.5,20 mg/kg of *** established method was applied for the pharmacokinetics study of ergone in six rats with the mean values of C,T,AUC,***/F,and V/F of ergone after oral administration a single 20 mg/kg dose obtained were 1.29μg/mL,3.41 h,13.7μg h/mL,3.32 h,1.98 1/h/kg,and 9.25 1/kg,respectively. The high-dose ergone provoked a significant increase in urine output and urinary excretion of K, Na and Cl after oral/intraperitoneal *** urinary rate of sodium excretion was parallel to the ergone concentration of plasma curve throughout the period under *** summary,these data suggest that ergone induced significantly greater diuretic and natriuretic effects after oral *** was also a linear relationship between ergone plasma concentration and rate of sodium excretion.

关键词： Polyporus umbellatus Ergosta-4,6,8(14),22-tetraen-3-one Pharmacokinetics Pharmacodynamic Diuretic effect