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Chinese Journal of Polymer Science 2006年第2期24卷 107-114页

作者：柏正武 department of Chemical Engineering and pharmacy Wuhan Institute of Chemical Technology

Two polyurethanes of different molecular weights were prepared by the copolymerization of phenyl diisocyanate and diisopropyl tartrate. The polyurethanes having terminal isocyanate groups were reacted with 3-aminopropyl silica gel to afford two chiral stationary phases. The M^- n of the two polyurethanes were 4057 g/mol and 6442 g/mol. The polyurethanes and the corresponding chiral stationary phases were characterized by FT-IR,^1 H NMR and elemental analysis. The loading capacities of the polyurethanes on silica gel were 0.68 mmol units/g and 0.61 mmol units/g, respectively. The separation performance and the influence of additives, triethylamine and trichloroacetic acid, on the separation of chiral compounds were investigated by HPLC. The chiral stationary phase prepared from polyurethane with M^- n of 4057 g/mol demonstrated better enantioseparation capability than that with M^- n of 6442 g/mol. Additionally, it was found that the addition of triethylamine and trichloroacetic acid in the mobile phases significantly improved the enantioseparation for these two chiral stationary phases.

关键词： Polyurethane Chiral stationary phase Enantioseparation Additive HPLC

Synthesis,Crystal Structure and Antiproliferative Activity of Ethyl 1-(Phenylcarbamoyl)-2-3,4,5-trimethoxyphenyl)cyclopropanecarboxylae

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Chinese Journal of Structural Chemistry 2014年第6期33卷 876-880页

作者：张敬一钟涵宇史国兵 department of pharmacy General Hospital of Shenyang Military Command department of pharmacy First Affiliated HospitalChina Medical University

Many small-molecule compounds have been evaluated with potential antiproliferative activities. Ethyl 1-（phenylcarbamoyl）-2-（3,4,5-trimethoxyphenyl）cyclopropanecarboxylate, one novel cyclopropylamide analogue of combretastatin-A4（CA-4）, has been synthesized and its crystal structure was characterized by X-ray single-crystal diffraction. The crystal belongs to monoclinic, space group P21/n, with a = 15.0263（3）, b = 7.6574（2）, c = 19.4117（4）, β = 111.9010（10）o, V = 2072.36（8）3, Z = 4, C22H24NO6, Mr = 398.42, Dc = 1.277 Mg/cm3, F（000） = 844, λ（MoKα） = 1.54178 , μ = 0.770 mm–1, R = 0.0546 and wR = 0.1889 for 3319 observed reflections（I 〉 2σ（I））. Meanwhile, the compound revealed potential antiproliferative activities in several cancer cells in vitro.

关键词： 3 4 5-trimethoxyphenyl synthesis crystal structure antiproliferative activities

Antiprotozoal assessment and phenolic acid profiling of five Fumaria(fumitory) species

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Asian Pacific Journal of Tropical Medicine 2015年第4期8卷 283-286页

作者： Ilkay Erdogan Orhan Nilgun Ozturk Bilge Sener department of Pharmacognosy Faculty of PharmacyGazi University department of Pharmacognosy Faculty of PharmacyAnadolu University

Objective:To explore some Fumaria species which were recorded to be traditionally used against malaria and other protozoal ***:Consequently,in the current study,antiprotozoal effect of the ethanol extracts obtained from five Fumaria species(Fumaria densiflora,Fumaria cilicica,Fumaria rostellata,Fumaria kralikii,and Fumaria parviflora)was investigated against the parasites;Plasmodium falciparum(malaria)and Trypanosoma bruceirhodesiense(human African trypanosomiasis)at 0.81 and 4.85μg/mL ***:Among them,Fumaria densiflora extract exerted the highest antiplasmodial(93.80%)and antitrypanasomal effect(55.40%),while the ethanol extracts of Fumaria kralikii(43.45%)and Fumaria rostellata(41.65%)showed moderate activity against Plasmodium ***,phenolic acid contents of the extracts were analyzed using high performance liquid chromatography(HPLC)and trans-cinnamic(4.32 mg/g)and caffeic(3.71 mg/g)acids were found to be the dominant phenolic acids in Fumaria ***:According to our results,Fumaria densiflora deserve further study for its promising antiprotozoal activity.

关键词： Fumaria Fumitory Antiprotozoal Malaria Trypanosomiasis Phenolic acid

Enhancing effect of natural borneol on the absorption of geniposide in rat via intranasal administration

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Journal of Zhejiang University-Science B(Biomedicine & Biotechnology) 2011年第2期12卷 143-148页

作者： Yang LU Shou-ying DU Xiao-lan CHEN Qing WU Xiao SONG Bing XU Yong-song ZHAI department of Industrial pharmacy School of Chinese Pharmacy Beijing University of Chinese Medicine Beijing 100102 China department of Chinese pharmacy Guiyang College of Traditional Chinese Medicine Guiyang 550002 China

Both geniposide （Ge） and natural borneol （NB） are bioactive substances derived from traditional Chinese herbs. The effect of NB on the pharmacokinetics of Ge in rat via intranasal administration was investigated. The concentrations of Ge in plasma were determined by reversed-phase high-performance liquid chromatography （HPLC） after intranasal administration of Ge （4 mg/kg） alone and combined with different doses （0.08, 0.8, and 8 mg/kg） of NB. The intravenous administration was given as a reference （4 mg/kg of Ge and 8 mg/kg of NB）. Compared with the intravenous administration, the absolute bioavailability of Ge was 76.14% through intranasal administration combined with NB. Compared with the intranasal administration of Ge alone, Ge could be absorbed rapidly in the nasal cavity combined with NB; the peak time of Ge in the plasma became shorter （3-5 min vs. 40 min）; the peak concentration became higher （1.32-4.25 IJg/ml vs. 0.67 ug/ml）; and, the relative bioavailability of Ge combined with NB was 90.3%-237.8%. The enhancing effect was attenuated as the dose of NB decreased. The results indicated that NB can accelerate the absorption of Ge dose-dependently in the nasal cavity.

关键词： Geniposide Natural borneol Intranasal administration Intravenous administration Pharmacokinetics

Inactivation gating determines drug potency:a common mechanism for drug blockade of HERG channels

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Acta Pharmacologica Sinica 2004年第5期25卷 12-18页

作者： Bao-feng YANG1, Dong-hui XU2, Chao-qian XU, Zhe LI, Zhi-min DU, Hui-zhen WANG, De-li DONGdepartment of Pharmacology, Harbin Medical University, Harbin 150086, China 2department of pharmacy, Sun Yat-sen University, Guangzhou 510080, China department of Pharmacology Harbin Medical University department of pharmacy Sun Yat-sen University

AIM: To determine the mechanisms of interactions between different drugs and HERG channels. METHODS:Various antiarrhythmic (dofetilide, quinidine, azimilide, RP58866) and non-antiarrhythmic (terfenadine, nicotine)agents were used on HERG channels expressed in Xenopus oocyte. Whole-cell voltage-clamp techniques wereused. RESULTS: All drugs produced concentration-dependent block of HERG current. The inhibition was mark-edly facilitated with voltage protocols favoring channel inactivation (eg, less negative holding potentials). Maneu-vers that weakened channel inactivation (eg, elevation of external K+), relieved HERG blockade by all drugs. Moreover,the inhibitory potency was reduced by at least 20-300 fold with varying compounds when rapid C-type inactivationwas removed by a mutation located between the transmembrane domains 5 and 6 (S631A). CONCLUSION: Theinactivation gating of HERG channels determines the blocking potency of drugs. This mechanism might be com-mon to drugs of various classes.

关键词： antiarrhythmic agents potassium channels mutation channel inactivation patch-clamp techniques oocytes Xenopus

Comparative pharmacokinetic studies of borneol in mouse plasma and brain by different administrations

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Journal of Zhejiang University-Science B(Biomedicine & Biotechnology) 2012年第12期13卷 990-996页

作者： Jing-yi ZHAO Yang LU Shou-ying DU Xiao SONG Jie BAI Yue WANG department of Industrial pharmacy School of Chinese PharmacyBeijing University of Chinese MedicineBeijing 100102China

Borneol,a monoterpenoid alcohol,is used widely,particularly in combined formulas for preventing and curing cardiovascular and cerebrovascular diseases in traditional Chinese *** order to understand the blood and brain pharmacokinetics after intravenous,intranasal,or oral administration and to investigate the superiority and feasibility of intranasal administration,a simple gas chromatographic (GC) method with flame ionization detection (FID) was developed for the quantification of *** samples and brain were collected from mice at 1,3,5,10,20,30,60,90,and 120 min after intravenous,intranasal,or oral administration of borneol at a dosage of 30.0 mg/*** preparations were carried out by liquid-liquid extraction with an internal standard solution of *** pharmacokinetic parameters were calculated by the software of *** calibration curves were linear in the range of 0.11-84.24 μg/ml and 0.16-63.18 μg/g for borneol in plasma and brain,*** methodological and extraction recoveries were both in the range of 85%-115%.The intra-day and inter-day variabilities for plasma and brain samples were ≤5.00% relative standard deviation (RSD).The absolute bioavailabilities F of intranasal and oral administrations were 90.68% and 42.99%.The relative brain targeted coefficients Re of intranasal and oral administrations were 68.37% and 38.40%.The GC-FID method developed could be applied to determination and pharmacokinetic *** borneol from injection was distributed and metabolized fast without absorption *** borneol from oral administration was distributed more slowly and had the lowest absolute *** administration of borneol was quickly absorbed into the blood and brain,was easy to use and had a greater safety than infection,which makes it worthy of further development as an administration route for encephalopathy treatment.

关键词： Borneol Intravenous administration lntranasal administration Oral administration Pharmacokinetics

Efficacy and Safety of Ombitasvir plus Paritaprevir,Ritonavir and Ribavirin in Non-cirrhotic Treatment-naive and Treatment-experienced Egyptians with Chronic HCV Genotype-4 Infection

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Current Medical Science 2021年第3期41卷 581-586页

作者： Manar Ahmed Azza E.Mansey Engy A.Wahsh Ahmed A.Gomaa Hoda M.Rabea department of Clinical pharmacy Faculty of PharmacyBeni Suef UniversityBeni Suef 62521Egypt department of Clinical pharmacy Faculty of PharmacyMenoufia UniversityAl Menoufia 32511Egypt department of Clinical pharmacy Faculty of PharmacyOctober 6 universityGiza 12573Egypt department of Tropical Medicine Faculty of MedicineFayoum UniversityFayoum 63511Egypt

Hepatitis C virus genotype 4(HCV-GT4)is a risk factor for cirrhosis,hepatocellular carcinoma and liver failure.A combination of three new direct-acting antivirals ombitasvir,paritaprevir,and ritonavir has been recommended for treatment of HCV-GT4 *** current study was aimed to assess the efficacy and safety of this combination plus ribavirin in non-cirrhotic,treatment-naive and-experienced Egyptians with HCV-GT4 infection in a real-world setting.A total of 255 Egyptians with HCV-GT4 infection were enrolled,including 82 treatment-experienced and 173 treatment-naive *** of them completed 12-week treatment protocol of ombitasvir,paritaprevir and ritonavir as an oral dose combination with *** response(VR)was measured,as well as the biochemical parameters related to treatment efficacy and adverse events at baseline and after treatment,at 4(VR4)and 12(VR12)weeks *** results showed that the VR4 rates were 98.8%in both groups,and VR12 rates were 97.7%and 96.3%in treatment-naive and-experienced patients,respectively,with no significant differences found between the groups concerning VR4(P=0.9)and VR 12(P=0.3).The most common adverse events were headache and fatigue,which were significantly more common(P=0.001 and 0.003,respectively)in treatment-experienced than in treatment-naive *** quadruple regimen was well-tolerated,and the reported adverse events were generally mild to *** real-world setting study confirms that the combination of ombitasvir,paritaprevir,ritonavir,and ribavirin is highly effective in the treatment of HCV-GT4 infection with a good safety and tolerability profile.

关键词： hepatitis C virus genotype-4 ombitasvir paritaprevir ribavirin

N-Substituted benzoxazolyl ureas and thioureas in Biginelli reaction promoted by trifluoromethane sulfonic acid:An efficient and convenient synthesis of substituted benzoxazolyl 3,4-dihydropyrimidine(1H)-(thio)-ones

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Chinese Chemical Letters 2009年第8期20卷 909-912页

作者： M.Saranga Pani M.Arjun D.Sridhar K.Srinivas T.Raviprasad department of pharmacy Kakatiya University department of Chemistry Kakatitya University

An efficient synthesis of 3,4-dihydropyrimidine 2 （1H）-ones and thiones （3,4-DHPMs） core was prepared by one-pot threecomponent Biginelli condensation and which was catalyzed by trifluoromethane sulfonic acid. The classical BigneUi reaction has been extended by the use of N-substituted benzoxazolyl semicarbazides and thiosemicarbazides and this method has the advantage of excellent yields and short reaction times. ？2009 M. Saranga Pard. Published by Elsevier B.V. on behalf of Chinese Chemical Society. All rights reserved.

关键词： Trifluoromcthane sulfonic acid N-substituted scmicarbazidcs and thioscmicarbazidcs β-Ketocster Substituted benzoxazolyl 3,4-dihydropyrimidinc (IH)-(thio)-ones

Effect of processing on the alkaloids in Aconitum tubers by HPLC-TOF/MS

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Journal of Pharmaceutical Analysis 2017年第3期7卷 170-175页

作者： Min Liu Yan Cao Diya Lv Wen Zhang Zhenyu Zhu Hai Zhang Yifeng Chai department of pharmacy Shanghai Changhai Hospital Second Military Medical University School of pharmacy Second Military Medical University department of pharmacy Eastern Hepatobiliary Surgery Hospital Second Military Medical University

According to the Chinese Pharmacopoeia 2015, only processed Aconitum tubers can be clinically applied, and the effect of processing is unclear. This research aimed to explore the effect of processing on cardiac efficacy of alkaloids in Aconitum tubers. First, the chemical ingredients in unprocessed and processed Aconitum tubers were identified and compared by using high performance liquid chromatography time-of-flight mass spectrometry(HPLC-TOF/MS) and multivariate pattern recognition methods. Then the representative alkaloids in Aconitum tubers, aconitine, benzoylaconine, and aconine, which belong to diester-diterpenoid alkaloids,monoester-diterpenoid alkaloids, and amine-diterpenoid alkaloids, respectively, were selected for further validation of attenuated mechanism. Subsequent pharmacological experiments with aconitine, benzoylaconine,and aconine in SD rats were used to validate the effect of processing on cardiac functions. After processing the Aconitum tubers, it was found that the contents of diester-diterpenoid alkaloids were reduced, and those of monoester-diterpenoid alkaloids and amine-diterpenoid alkaloids were increased, suggesting that diesterditerpenoid alkaloids were transformed into monoester-diterpenoid alkaloids and amine-diterpenoid *** further decocting the aconitine in boiling water, it was confirmed that the three alkaloids could be progressively transformed. Pharmacological experiments with aconitine, benzoylaconine, and aconine in SD rats showed that aconitine at a dose of 0.01 mg/kg and aconine at a dose of 10 mg/kg enhanced the cardiac function, while benzoylaconine at a dose of 2 mg/kg weakened the cardiac function. The effect of processing is attributed to the transformation of the most toxic diester-diterpenoid alkaloids into less toxic monoesterditerpenoid alkaloids and amine-diterpenoid alkaloids.

关键词： Aconitum tubers Alkaloids Processing HPLC-TOF/MS

Nanomedicine strategies for sustained,controlled,and targeted treatment of cancer stem cells of the digestive system

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World Journal of Gastrointestinal Oncology 2016年第10期8卷 735-744页

作者： Fang-Yuan Xie Wei-Heng Xu Chuan Yin Guo-Qing Zhang Yan-Qiang Zhong Jie Gao department of pharmacy Shanghai Eastern Hepatobiliary Surgery Hospital department of Pharmaceutical Sciences School of Pharmacythe Second Military Medical University department of Biochemical pharmacy School of Pharmacythe Second Military Medical University department of Gastroenterology Changzheng HospitalSecond Military Medical University

Cancer stem cells(CSCs) constitute a small proportion of the cancer cells that have self-renewal capacity and tumor-initiating *** have been identified in a variety of tumors,including tumors of the digestive *** exhibit some unique characteristics,which are responsible for cancer metastasis and ***,the development of effective therapeutic strategies against CSCs plays a key role in increasing the efficacy of cancer *** potential approaches to target CSCs of the digestive system have been explored,including targeting CSC surface markers and signaling pathways,inducing the differentiation of CSCs,altering the tumor microenvironment or niche,and inhibiting ATP-driven efflux ***,conventional therapies may not successfully eradicate CSCs owing to various problems,including poor solubility,stability,rapid clearance,poor cellular uptake,and unacceptable *** strategies,which include drug,gene,targeted,and combinational delivery,could solve these problems and significantly improve the therapeutic *** review briefly summarizes the ongoing development of strategies and nanomedicine-based therapies against CSCs of the digestive system.

关键词： Nanomedicine Cancer stem cells Digestive system Drug delivery Gene delivery