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Asian Journal of Pharmaceutical Sciences 2017年第3期12卷 292-298页

作者： Haonan Xing Mei Lu Lei Xian Jinmin Zhang Tianzhi Yang Li Yang Pingtian Ding School of Pharmacy Shenyang Pharmaceutical UniversityShenyangChina Department of Basic Pharmaceutical Sciences School of PharmacyHusson UniversityBangorMEUSA

A cationic gene delivery vector, guanidinylated disulfide-containing poly(amido amine)(CARCBA), was synthesized by Michael addition reaction between N,N′-cystaminebisacrylamide(CBA) and guanidine hydrochloride(CAR). Gel permeation chromatography(GPC) was used to evaluate the molecular weight of synthesized CAR-CBA. Polyethyleneimine(PEI) with molecular weight of 25 kDa was adopted as a reference, and polyethylene glycols(PEG) with different molecular weights were used to establish a standard curve for determining the molecular weight of CAR-CBA. The effects of two critical factors, namely columns and eluents,on the molecular weight measurement of CAR-CBA were investigated to optimize the GPC quantitative method. The results showed that Ultrahydrogel columns(120, 250) and HAc–NaAc(0.5 M, pH 4.5) buffer solution were the optimal column and GPC eluent, respectively.The molecular weight of the synthesized CAR-CBA was analyzed by the optimized GPC method and determined to be 24.66 kDa.

关键词： Guanidinylated disulfide-containing poly(amido amine) Synthesis Cationic gene delivery vector Molecular weight determination Gel permeation chromatography

3D-QSAR and Surflex Docking Studies of a Series of Alkaline Phosphatase Inhibitors

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Chinese Journal of Structural Chemistry 2019年第1期38卷 7-16,1页

作者：舒茂武涛王必武李静徐春媚林治华 School of Pharmacy and Bioengineering Chongqing University of Technology

Alkaline phosphatases(APs) include the placental AP(PLAP), germ cell AP(GCAP), intestinal AP(IAP) and tissue nonspecific AP(TNAP). Over expression of TNAP in smooth muscle cells of kidney and vessels provokes the progress of such serious diseases as end-stage renal disease, idiopathic infantile arterial calcification, ankylosis, osteoarthritis and diabetes. In order to design and optimize the potent TNAP inhibitors, comparative molecular field analysis(CoMFA) and comparative molecular similarity indices analysis(CoMSIA) were used to analyze 3D structure-activity relationships(3D-QSAR) of TNAP inhibitors. The 3D-QSAR model(CoMFA with q^2 = 0.521, r^2 = 0.930; CoMSIA with q^2 = 0.529, r^2 = 0.933) had a good predictability. Surflex-dock was used to reveal the binding mode between the inhibitors and TNAP protein. CoMFA, CoMSIA and docking results provide guidance for the discovery of TNAP inhibitors. Finally, eight new compounds as potential TNAP inhibitors were designed.

关键词： 3D-QSAR surflex-dock alkaline phosphatase inhibitors

Network pharmacology unveils spleen-fortifying effect of Codonopsis Radix on different gastric diseases based on theory of “same treatment for different diseases” in traditional Chinese medicine

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Chinese Herbal Medicines 2021年第2期13卷 189-201页

作者： Ru-pu He Zheng Jin Ru-yun Ma Fang-di Hu Jian-ye Dai School of Pharmacy Lanzhou UniversityLanzhou 730000China

Objective: "Same treatment for different diseases" is a unique treatment strategy under the guidance of traditional Chinese medicine(TCM) theory.Codonopsis Radix(Codonopsis pilosula,Dangshen in Chinese)with spleen-fortifying effect was employed to understand the strategy of "Same treatment for different diseases",based on its common mechanism in the treatment of gastric diseases including gastric ulcer,gastritis and gastric cancer via network pharmacology research.Methods:Network pharmacology research methods were used to analyze the interaction network and potential mechanisms of Dangshen in treating gastric ulcer,gastritis and gastric cancer.The active components and their target proteins of Dangshen were integrated from TCMSP,BATMAN-TCM databases.The targets of gastric ulcer,gastritis and gastric cancer were collected through GeneCards,PubMed,TDD and DisGeNET Database.Through screening,the key components and the key targets of Dangshen in treating gastric ulcer,gastritis and gastric cancer were obtained.After KEGG pathway analysis and GO analysis,the important pathways and biological processes were analyzed.Results:Through data and literature mining,the common and specific pharmaceutical effects and mechanism of Dangshen were summarized in these three gastric lesions.It was shown that Dangshen mainly acted on gastric ulcer,gastritis and gastric cancer through the overall regulation of the PI3K-AkT signaling pathway.With the development of the disease,it will gradually increase the control of inflammation through TNF,NF-κB and other inflammation-related signaling pathways to reduce inflammatory damage.For tumorigenesis,it pays more attention to inhibiting the ErbB signaling pathways to reduce the proliferation and migration of tumor cells.In addition,Dangshen's regulation of HIF-1 signaling pathway may also be beneficial for the treatment of gastric ulcer,gastritis and gastric cancer.Conclusion:Dangshen achieves spleen-fortifying effect on gastric diseases including gastric ulcer,gastritis and gastric cancer th

关键词： Codonopsis Radix gastric cancer gastric ulcer gastritis network pharmacology same treatment for different diseases spleen-fortifying effect

“Omics” in pharmaceutical research: overview, applications, challenges, and future perspectives

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Chinese Journal of Natural Medicines 2015年第1期13卷 3-21页

作者： YAN Shi-Kai LIU Run-Hui JIN Hui-Zi LIU Xin-Ru YE Ji SHAN Lei ZHANG Wei-Dong School of Pharmacy Shanghai Jiao Tong University School of Pharmacy Second Military Medical University Shanghai Institute of Pharmaceutical Industry

In the post-genomic era, biological studies are characterized by the rapid development and wide application of a series of "omics" technologies, including genomics, proteomics, metabolomics, transcriptomics, lipidomics, cytomics, metallomics, ionomics, interactomics, and phenomics. These "omics" are often based on global analyses of biological samples using high through-put analytical approaches and bioinformatics and may provide new insights into biological phenomena. In this paper, the development and advances in these omics made in the past decades are reviewed, especially genomics, transcriptomics, proteomics and metabolomics; the applications of omics technologies in pharmaceutical research are then summarized in the fields of drug target discovery, toxicity evaluation, personalized medicine, and traditional Chinese medicine; and finally, the limitations of omics are discussed, along with the future challenges associated with the multi-omics data processing, dynamics omics analysis, and analytical approaches, as well as amenable solutions and future prospects.

关键词：传统医药药理学网络中国药物发现生物制药生物医学生物系统

Humulus lupulus L. Extract Prevents Ovariectomy-Induced Osteoporosis in Mice and Regulates Activities of Osteoblasts and Osteoclasts

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Chinese Journal of Integrative Medicine 2021年第1期27卷 31-38页

作者： XIA Tian-shuang LIN Liu-yue ZHANG Qiao-yan JIANG Yi-ping LI Chang-hui LIU Xiao-yan QIN Lu-ping XIN Hai-liang Department of Pharmacognosy School of PharmacySecond Military Medical UniversityShanghai(200433)China schoolof pharmacy Fujian University of Traditional Chinese MedicineFuzhou(350108)China School of Pharmacy Zhejiang Chinese Medical UniversityHangzhou(310053)China

Objective:To systematically evaluate the protective effects of Humulus lupulus L.extract(HLE)on osteoporosis mice.Methods:In vivo experiment,a total of 3512-week-old female ICR mice were equally divided into 5 groups:the sham control group(sham);the ovariectomy with vehicle group(OVX);the OVX with estradiol valerate[EV,0.2 mg/(kg·d)];the OVX with low-or high-dose HLE groups[HLE,1 g/(kg·d)and 3 g/(kg·d)],7 in each group.Treatment began 1 week after the ovariectomized surgery and lasted for 12 weeks.Bone mass and trabecular bone mircoarchitecture were evaluated by micro computed tomography,and bone turnover markers in serum were evaluated using enzyme-linked immunosorbent assay(ELISA)kits.In vitro experiment,osteoblasts and osteoclasts were treated with HLE at doses of 0,4,20 and 100μg/mL.Biomarkers for bone formation in osteoblasts and bone resorption in osteoclasts were analyzed.Results:Compared with the OVX group,HLE exerted bone protective effects by the increase of estradiol(P<0.05),the improvement of cancellous bone structure,bone mineral density(P<0.01)and the reduction of serum alkaline phosphatase(ALP),tartrate resistant acid phosphatase(TRAP),bone gla-protein,c-terminal telopeptides of typeⅠcollagen(CTX-Ⅰ)and deoxypyridinoline levels(P<0.01 for all).In vitro experiment,compared with the control group,HLE at 20μg/mL promoted the cell proliferation(P<0.01),and increased the expression of bone morphogenetic protein-2 and osteopontin levels in osteoblasts(both P<0.05).HLE at 100μg/mL increased the osteoblastic ALP activities,and HLE at all dose enhanced the extracellular matrix mineralization(both P<0.01).Furthermore,compared with the control group,HLE at 20μg/m L and 100μg/m L inhibited osteoclastic TRAP activity(P<0.01),and reduced the expression of matrix metalloproteinase-9 and cathepsin K(both P<0.05).Conclusion:HLE may protect against bone loss,and have potentials in the treatment of osteoporosis.

关键词： Humulus lupulus L. osteoporosis ovariectomy-induced mice osteoblasts osteoclasts

Percutaneous absorption and brain distribution facilitation of borneol on tetramethylpyrazine in a microemulsion-based transdermal therapeutic system

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Asian Journal of Pharmaceutical Sciences 2019年第3期14卷 305-312页

作者： Xiaoge Hu Ning Cheng Jihui Zhao Xianghua Piao Yulu Yan Qibo Zhang Kuan Zhou Yongtai Zhang Nianping Feng School of Pharmacy Shanghai University of Traditional Chinese Medicine

In this study, we show that the percutaneous absorption and brain distribution of tetramethylpyrazine(TMP) is enhanced when combined with borneol(BN) in a microemulsionbased transdermal therapeutic system(ME-TTS). The formulation of the TMP and BN microemulsion(TEM-BN-ME) was optimized in skin permeation studies in vitro following a uniform experimental design. Male Sprague-Dawley rats were used for the in vivo pharmacokinetic and tissue distribution studies of TMP-BN-ME-TTS. In the pharmacokinetic study, the TMP-BN-ME-TTS treated rats had significantly higher( P < 0.05) C max and AUC of TMP than the TMP-ME-TTS treated rats, indicating that BN improves the rate and extent of TMP percutaneous absorption. In the tissue distribution study, the AUC of TMP in brain was significantly higher in the TMP-BN-ME-TTS group( P < 0.05), indicating that BN facilitates the distribution of TMP in brain. In summary, BN enhanced the percutaneous absorption and brain distribution of TMP in a microemulsion-based transdermal therapeutic system.

关键词： Tetramethylpyrazine Borneol Microemulsion Percutaneous absorption Brain distribution

Chrysophanol localizes in mitochondria to promote cell death through upregulation of mitochondrial cyclophilin D in HepG2 cells

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Chinese Herbal Medicines 2021年第2期13卷 221-227页

作者： Yu Xie Ling Zhang Yuan-yuan Li Dian He Li-fang Zheng School of Pharmacy Lanzhou UniversityLanzhou 730000China

Objective:Chrysophanol(Chry) displays potent anticancer activity in human cancer cells and animal models,but the cellular targets of Chry have not been fully defined.Herein,we speculated whether mitochondria were a target involved in Chry-induced cytotoxicity.Methods:Human liver cancer cell line HepG2 was incubated.The cytotoxicity was evaluated by MTT assay.Mitochondria localization was evaluated by a confocal microscopy.Mitochondrial membrane potential ΔΨm was detected by TMRE staining and determined by the flow cytometer.The levels of ATP,mitochondrial superoxide anions,and GSH/GSSG were determined according to the assay kits.The apoptosis were evaluated through Hoechst33342/PI and Annexin V/PI staining,respectively.The expression of cyclophilin D(CyPD) was determined by immunoblot method,and the interaction between CyPD and Chry was analyzed by molecule docking procedure.Results:Chry itself mainly localized in mitocho ndria to cause mitochondrial dysfunction and cell death in HepG2 cells.As regard to the mechanism,cyclosporin A as the inhibitor for the formation of mitochondrial permeability transition pore(mPTP) moderately suppressed cell death,indicating mPTP involved in the process of cell death.Further,Chry enhanced the protein expression of Cyclophilin D(CyPD) which is a molecular componentry and a modulator of mPTP,while antioxidant N-acetyl-L-cysteine inhibited the expression of CyPD.Molecule docking procedure disclosed two hydrogen-bonds existed in CyPD-Chry complex with-11.94 kal/mol of the binding affinity value.Besides,the mtDNA-deficient HepG_2-ρ0 cells were much resistant to Chry-induced cell death,indicating mtDNA at least partly participated in cell death.A combination of Chry and VP-16 produced the synergism effect toward cell viability andΔΨm,while Chry combined with Cis-Pt elicited the antagonism effect.Conclusion:Taken together,enrichment in mitochondria and actions on mPTP,CyPD and mtDNA provides an insight into the anticancer mechanism of Chry.The combination therapy for Chry with clinica

关键词： chrysophanol combination therapy mitochondria mitochondrial permeability transition pore mtDNA

Preparation of CaP/pDNA nanoparticles by reverse micro-emulsion method: Optimization of formulation variables using experimental design

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Asian Journal of Pharmaceutical Sciences 2017年第2期12卷 179-186页

作者： Wenpan Li Shasha Jing Xiu Xin Xirui Zhang Kang Chen Dawei Chen Haiyang Hu Department of Pharmaceutics School of Pharmacy Shenyang Pharmaceutical University

In this study, the CaP/pDNA nanoparticles were prepared using Triton X-100/Butanol/Cyclohexane/Water reverse microemulsion system. Optimization of preparation conditions was based on evaluation of particle size by Box–Behnken design method. The particle sizes of the optimized CaP/pDNA nanoparticles were found to be 60.23 ± 4.72 nm, polydispersity index was 0.252 and pDNA encapsulate efficiency was more than 90%. The optimized CaP/pDNA nanoparticles have pH sensitivity and biocompatibility. Further, optimized CaP/pDNA nanoparticles showed higher transfection efficiency.

关键词： CaP nanoparticles pDNA Reverse microemulsion method Box–Behnken design Transfection and expression

Mitochondria-targeted cancer therapy based on functional peptides

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Chinese Chemical Letters 2023年第5期34卷 104-110页

作者： Yuhan Sun He Zhang Guangzhao Lu Huan Wang Ying Lu Li Fan Department of Pharmaceutical Sciences School of PharmacyNaval Medical UniversityShanghai 200433China

Mitochondria are critical for tumor growth and metastasis.A number of traditional antitumor drugs have poor water solubility and must penetrate multiple cellular barriers to reach the mitochondria.Because mitochondria have a unique transmembrane potential and an inner membrane with a low permeability,it is difficult for most drugs to enter mitochondria.In recent years,mitochondria-targeted delivery systems that use functional peptides to modify drugs have received increasing attention.Introducing functional peptides can change the original physicochemical properties of drugs and actively target mitochondria.Functional peptide-drug conjugates(PDCs,peptide-drug conjugates)can decompose and release drugs over time or due to certain stimuli in tumors.This preserves the biological activity of the drug while increasing intratumor uptake through the enhanced permeability and retention effect(EPR,the enhanced permeability and retention effect).In this review,we focus on the direction of cancer therapy and review the application of different functional peptides in the mitochondria-targeted tumor treatments reported in recent years.

关键词： Peptides Mitochondria Cancer therapy Targeting Cell uptake

Characterization of antioxidant and antibacterial compounds from aerial parts of Haplophyllum tuberculatum

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Journal of Bioresources and Bioproducts 2022年第1期7卷 52-62页

作者： Salma Salim Al-Saeghi Mohammad Amzad Hossain Salem Said Jaroof Al-Touby School of Pharmacy College of Pharmacy and NursingUniversity of NizwaP.O.Box 33Postal Code 616NizwaOman school of Nursing College of Pharmacy and NursingUniversity of NizwaP.O.Box 33Postal Code 616NizwaOman

The aerial parts of Haplophyllum tuberculatum(H.tuberculatum)have traditionally been used by local communities to treat fever,gastrointestinal disorders,worms,malaria and fractures,how-ever,the responsible ingredients of the selected medicinal plant have not been identified.In the present study,antibacterial and antioxidant ingredients were isolated and characterized from the plant parts of locally grown H.tuberculatum,and their biological activity was evaluated.The powder aerial parts were extracted with methanol and the extract was successively frac-tionated with different polarities of solvents.All polarities of extracts(hexane,chloroform,ethyl acetate,butanol,methanol and water)were used to determine their antibacterial and antioxi-dant activity by established in-vitro method.The disk diffusion and free radical scavenging 2,2-diphenyl-1-picrylhydrazyl(DPPH)methods were used to evaluate antibacterial and antioxidant activities of the prepared extracts and pure isolated compounds at different concentrations against three strains of Gram-positive and three Gram-negative bacteria.The antibacterial activity results showed that all prepared fractions and isolated pure compounds of the plant species gave signif-icant activity against all Gram(+and-)bacterial strains with the range of inhibition 0-20 mm.The antioxidant activity of the prepared extracts at all concentrations also showed substantial activity.Based on the highest activity,ethyl acetate and chloroform extracts were selected for the separation and isolation of antioxidant and antibacterial compounds by thin layer chromatogra-phy(TLC),column chromatography(CC),and preparative thin layer chromatography(PTLIC).The structure of the isolated antioxidant and antibacterial compounds from the ethyl acetate and chloroform extracts were determined on the basis of nuclear magnetic resonance(NMR)and mass spectra.The isolated pure compounds and active extracts could be used as a medicine for various infectious related diseases.

关键词： H.tuberculatum Soxhlet extraction Antioxidant activity Antibacterial activity Chromatography Pure compound