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Antagonistic effects of extracts from Artemisia rupetris L. and Leontopodium leontopodioides to CC chemokine receptor 2b(CCR2b)

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Chinese Journal of Natural Medicines 2016年第5期14卷 363-369页

作者： YU Qin-Wei HU Jie WANG Hao CHEN Xin ZHAO Fang GAO Peng YANG Qiu-Bin SUN Dan-Dan ZHANG Lu-Yong YAN Ming Jiangsu Key Laboratory of Drug Screening China Pharmaceutical University Department of Natural Medicinal Chemistry China Pharmaceutical University School of Life Science and Technology China Pharmaceutical University School of Traditional Chinese Medicine China Pharmaceutical University Key Laboratory of Drug Quality Control and pharmacovigilance (China Pharmaceutical University) Ministry of Education

The present study was designed to establish a suitable assay to explore CCR2 b receptor antagonists from the natural products of Artemisia rupetris and Leontopodium leontopodioides. An aequorin assay was developed as a cell-based assay suitable for 384-well microplate and used for screening CCR2 b receptor antagonists from natural products. Through establishing suitable conditions, the assay was shown to be suitable for screening of CCR2 b receptor antagonists. Seven compounds were identified in preliminary screening. Five of them showed evident dose-response relationship in secondary screening. The structure–activity relationship study suggested that 7-position hydroxyl group of flavonoids was necessary, a polar group should be introduced on the 3-position, and the substituents on 2-position benzene ring of flavonoids have little influence on the potentency of the inhibition activity on CCR2 b receptor. The ortho-position dihydroxyl structure in quinic acid compounds may be important. In conclusion, Compounds HR-1, 5, 7, and AR-20, 35 showed activity as antagonist of CCR2 b receptor, which shed lights on the development of novel drugs as CCR2 b receptor antagonists for preventing inflammation related diseases.

关键词： CCR2b antagonist Inflammation Aequorin assay Artemisia rupetris Leontopodium leontopodioides

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Synthesis and cytotoxic activity of 3, 4, 11-trihydroxyl modified derivatives of bergenin

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Chinese Journal of Natural Medicines 2014年第12期12卷 929-936页

作者： YAN De-Biao ZHANG Dong-Ping LI Ming LIU Wen-Yuan FENG Feng DI Bin GUO Qing-Long XIE Ning Department of Natural Medicinal Chemistry China Pharmaceutical University Department of Pharmaceutical Analysis China Pharmaceutical University Key Laboratory of Drug Quality Control and pharmacovigilance Ministry of Education China Pharmaceutical University Jiangsu Key Laboratory of Carcinogenesis and Intervention China Pharmaceutical University Jiangxi Qingfeng Pharmaceutical Ltd.

To synthesize a series of 3-, 4-, and/or 11-trihydroxy modified bergenin derivatives and evaluated their cytotoxic activity in vitro. The phenolic hydroxyl groups of bergenin were protected by benzyl groups with benzyl bromide. Treatment of dibenzyl bergenin with the corresponding acid in the presence of EDC·HCl and DMAP in CH2Cl2, followed by hydrogenation over Pd/C catalysts, afforded derivatives of bergenin esters. All of the target compounds were identified by IR, MS, and 1H NMR. Twenty-six novel and three known derivatives of bergenin esters were synthesized. Their cytotoxicity values were evaluated by the MTT assay on the inhibition of DU-145 and BGC-823 cells in vitro. Several triply-substituted(3a, 4a, 5a, 6a, 7a) and doublysubstituted(8b, 9b) bergenin derivatives exhibited higher cytotoxic activity than bergenin. The result showed that the size of substituents and the lipophilicity of the bergenin esters displayed an important role on their cytotoxic activity.

关键词： Bergenin 3-,4-,and/or 11-trihydroxyl modified derivatives Cytotoxic activity Structure-activity relationships

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Evaluation of Rational Use of Antiretrovirals before the Dolutegravir Transition in Kinshasa, Democratic Republic of Congo

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World Journal of AIDS 2021年第2期11卷 41-49页

作者： Erick N. Kamangu Ben I. Bulanda Idriss M. Mwanaut Simplice K. Makoka Gauthier K. Mesia “Focus HIV/AIDS” Research Group Kinshasa Democratic Republic of Congo HIV/AIDS unit Service of Molecular Biology Department of Basic Sciences Faculty of Medicine University of Kinshasa Kinshasa Democratic Republic of Congo unit of Clinical Pharmacology and pharmacovigilance Department of Pharmacology and Therapeutics Faculty of Pharmaceutical Sciences University of Kinshasa Kinshasa Democratic Republic of Congo

Background: The ultimate goal of AntiRetroViral Treatments (ART) is to achieve complete immune restoration and lasting viral suppression in the infected patient. In order to ensure the efficacy, safety and accessibility of antiretroviral drugs (ARVs), it is recommended that they should be prescribed according to national guidelines;which are evolving with the various recommendations of the World Health Organization (WHO) and the arrival of newer, more effective and safer molecules. Objective: The objective of this study was to assess the rational use of Antiretrovirals in patients treated in Kinshasa before the use of Dolutegravir within the national program in order to assess the correct use of these molecules. Methods: This work is a descriptive cross-sectional study to assess the rational use of first-line ARVs among People Living with HIV (PLHIV) in different Centers of Treatment (ATCs) in Kinshasa before the introduction of Dolutegravir. The records of patients on ARVs were randomly and rationally selected in 12 different ATCs for HIV in Kinshasa according to three centers per district in the period from June to September 2018. Information on use and consumption of ARVs, compliance with guidelines, change of therapeutic combination as well as their reasons were consulted for the present study. Results: 507 files of PLHIV were collected in the various ATCs. 274 (54.1%) were from female patients. The most represented age group was 26 to 35 years with 192 patients (37.9%). The mean duration of first-line treatment for all patients included was 16.30 ± 5.85 months. The most widely used combination of ARVs overall was TDF + 3TC + EFV at 45.4%. 305 (60.2%) PLHIV kept the same first-line treatment molecule throughout the treatment period with an average treatment duration of 12.9 ± 2.77 months. The most common combination found in this population was TDF + 3TC + EFV (69.2%). 202 (39.8%) PLHIV changed

关键词： Rational Use ARVs Dolutegravir Kinshasa

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Anti-inflammatory and hepatoprotective effects of total flavonoid C-glycosides from Abrus mollis extracts

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Chinese Journal of Natural Medicines 2014年第8期12卷 590-598页

作者： CHEN Mi WANG Tao JIANG Zhen-Zhou SHAN Chun WANG Hao WU Mei-Juan ZHANG Shuang ZHANG Yun ZHANG Lu-Yong Jiangsu Center for Drug Screening China Pharmaceutical University Jiangsu Center for Pharmacodynamics Research and Evaluation China Pharmaceutical University Department of Natural Medicinal Chemistry China Pharmaceutical University Biology Institute of Shandong Academy of Sciences Key Laboratory of Drug Quality Control and pharmacovigilance (China Pharmaceutical University) Ministry of Education

The aim of this study was to evaluate the anti-inflammatory and hepatoprotective effects of the total flavonoid C-glycosides isolated from Abrus mollis extracts(AME). In the anti-inflammatory tests, xylene-induced ear edema model in mice and carrageenan-induced paw edema model in rats were applied. The hepatoprotective effects of AME were evaluated with various in vivo models of acute and chronic liver injury, including carbon tetrachloride(CCl4)-induced hepatitis in mice, D-galactosamine(D-GalN)-induced hepatitis in rats, as well as CCl4-induced hepatic fibrosis in rats. In the acute inflammation experiment, AME significantly suppressed xylene-induced ear edema and carrageenan-induced paw edema, respectively. In the acute hepatitis tests, AME significantly attenuated the excessive release of ALT and AST induced by CCl4 and D-GalN. In CCl4-induced hepatic fibrosis model, AME alleviated liver injury induced by CCl4 shown by histopathological sections of livers and improved liver function as indicated by decreased liver index, serum ALT, AST, TBIL, and ALP levels and hydroxyproline contents in liver tissues, and increased serum ALB and GLU levels. These results indicated that AME possesses potent anti-inflammatory activity in acute inflammation models and hepatoprotective activity in both acute and chronic liver injury models. In conclusion, AME is a potential anti-inflammatory and hepatoprotective agent and a viable candidate for treating inflammation, hepatitis, and hepatic fibrosis.

关键词： Abrus mollis Flavonoid C-glycosides Inflammation Liver injury

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Triterpenoid saponins from Patrinia scabra

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Chinese Journal of Natural Medicines 2014年第1期12卷 43-46页

作者： FENG Feng XU Xi-Yu LIU Fu-Lei LIU Wen-Yuan XIE Ning Department of Natural Products Chemistry China Pharmaceutical University Key Laboratory of Carcinogenesis and Intervention China Pharmaceutical University Department of Pharmaceutical Analysis China Pharmaceutical University Key Laboratory of Drug Quality Control and pharmacovigilance China Pharmaceutical University Ministry of Education Qingfeng Pharmaceutical Inc.

AIM： To study the chemical constituents and bioactivity of the roots ofPatrinia scabra Bunge. METHODS： The chemical constituents were isolated using various chromatographic methods, and the structures were elucidated on the basis of spectral analysis and chemical methods. In addition, cytotoxic activities toward HepG2 cells were tested by the MTT method. RESULTS： A new triterpenoid saponin, 3-O-（4＇-isovaleryl）-O-β-D-xylose-12,30-dihydroxy-oleanane-28,13-1actone-22-O- β-D-glucoside （1）, along with two known triterpenoid saponins, acanthopanax saponin CP3 （2） and foetoside C （3）, were isolated. CONCLUSION： The aglycone of compound 1 was a new skeleton derivative of oleanolic acid. Compound 2 showed strong cyto- toxicity to HePG2 cells （IC50 1.49 umol.L-1）.

关键词： Patrinia scabra Bunge Chemical constituents Triterpenoid saponins Cytotoxicity

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Noninvasive Detection and Imaging of Matrix Metalloproteinases for Cancer Diagnosis

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Journal of Analysis and Testing 2017年第3期1卷 203-212页

作者： Jin Hong Yu-Feng Chen Jia-Jia Shen Ya Ding Key Laboratory of Drug Quality Control and pharmacovigilance China Pharmaceutical UniversityMinistry of EducationNanjing 21009China Key Laboratory of Biomedical Functional Materials School of SciencesChina Pharmaceutical UniversityMinistry of EducationNanjing 211198China

Matrix metalloproteinases(MMPs)are important cancer biomarkers and the sensitive detection of MMPs is of great importance to improve clinical diagnosis and therapy of cancer at its early *** imaging,including fluorescent optical imaging,radiolabeled imaging,and magnetic resonance imaging,is a powerful tool to visualize and characterize biological processes at the cellular and molecular *** recognition of MMPs via imaging strategies by utilizing MMP-responsive probes has been a hot pursuit in recent *** designed for MMP detection commonly have two features:(1)off-thenon state in detection signal response to the appearance of MMPs,which has been applied in optical imaging and magnetic resonance imaging;(2)specific retention upon sensing MMPs,which has been applied in radiolabeled *** development of theory and technology in the field of biomarker probes will be beneficial to the accurate diagnosis and effective treatment of cancer.

关键词： MMPs Noninvasive detection Optical imaging Radiolabeled imaging Magnetic resonance imaging

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Degradation of proteins by PROTACs and other strategies

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Acta Pharmaceutica Sinica B 2020年第2期10卷 207-238页

作者： Yang Wang Xueyang Jiang Feng Feng Wenyuan Liu Haopeng Sun Department of Pharmaceutical Analysis Key Laboratory of Drug Quality Control and PharmacovigilanceMinistry of EducationChina Pharmaceutical UniversityNanjing 210009China Department of Natural Medicinal Chemistry China Pharmaceutical UniversityNanjing 211198China Jiangsu Food and Pharmaceutical Science College Huaian 223003 China Department of Medicinal Chemistry China Pharmaceutical UniversityNanjing 211198China

Abnormal protein expression or activities are associated with many diseases,especially ***,down-regulating the proteins involved in cancer cell survival proved to be an effective strategy for cancer treatment—a number of drugs based on proteolysis-targeting chimaera(PROTAC)mechanism have demonstrated clinical *** progress in the PROTAC strategy includes identification of the structure of the first ternary eutectic complex,extra-terminal domain-4-PROTAC-VonHippel-Lindau(BRD4-PROTAC-VHL),and PROTAC ARV-110 has entered clinical trials for the treatment of prostate cancer in *** discoveries strongly proved the value of the PROTAC *** this review,we summarize recent meaningful research of PROTACs,including the molecular design and optimization strategy as well as clinical application of candidate *** hope to provide useful insights for rational design of PROTACs.

关键词： Protein degradation PROTAC Ubiquitin-proteasome system E3 ubiquitin ligase Target protein Heterobifunctional molecule

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Protective effect of total flavonoid C-glycosides from Abrus mollis extract on lipopolysaccharide-induced lipotoxicity in mice

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Chinese Journal of Natural Medicines 2014年第6期12卷 461-468页

作者： WANG Yun JIANG Zhen-Zhou CHEN Mi WU Mei-Juan GUO Hong-Li SUN Li-Xin WANG Hao ZHANG Shuang WANG Tao ZHANG Lu-Yong Jiangsu Center for Drug Screening China Pharmaceutical University Key Laboratory of Drug Quality Control and pharmacovigilance China Pharmaceutical University Department of Natural Medicinal Chemistry China Pharmaceutical University Jiangsu Center for Pharmacodynamics Research and Evaluation China Pharmaceutical University State Key Laboratory of Natural Medicines China Pharmaceutical University

Abrus mollis is a widely used traditional Chinese medicine for treating acute and chronic hepatitis, steatosis, and fibrosis. It was found that the total flavonoid C-glycosides from Abrus mollis extract(AME) showed potent antioxidant, anti-inflammatory, and hepatoprotective activities. To further investigate the hepatoprotective effect of AME and its possible mechanisms, lipopolysaccharide(LPS)-induced liver injury models were applied in the current study. The results indicated that AME significantly attenuated LPS-induced lipid accumulation in mouse primary hepatocytes as measured by triglyceride(TG) and total cholesterol(TC) assays and Oil Red O staining. Meanwhile, AME exerted a protective effect on LPS-induced liver injury as shown by decreased liver index, serum aminotransferase levels, and hepatic lipid accumulation. Real-time PCR and immunoblot data suggested that AME reversed the LPS-mediated lipid metabolism gene expression, such as sterol regulatory element-binding protein-1(SREBP-1), fatty acid synthase(FAS), and acetyl-CoA carboxylase 1(ACC1). In addition, LPS-induced overexpression of activating transcription factor 4(ATF4), X-box-binding protein-1(XBP-1), and C/EBP homologous protein(CHOP) were dramatically reversed by AME. Furthermore, AME also decreased the expression of LPS-enhanced interleukin-6(IL-6) and cyclooxygenase-2(COX-2). Here, it is demonstrated for the first time that AME ameliorated LPS-induced hepatic lipid accumulation and that this effect of AME can be attributed to its modulation of hepatic de novo fatty acid synthesis. This study also suggested that the hepatoprotective effect of AME may be related to its down-regulation of unfolded protein response(UPR) activation.

关键词： Flavonoid C-glycosides Endotoxin Unfolded protein response Lipid metabolism Inflammation

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NIR-Ⅱ photothermal therapy for effective tumor eradication enhanced by heterogeneous nanorods with dual catalytic activities

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Nano Research 2022年第5期15卷 4310-4319页

作者： Linghua Zhang Wenjie Wang Meng Ou Xiaoxiao Huang Yu Ma Jiayue Tang Ting Hou Sheng Zhang Li Yin Huan Chen Yanglong Hou Ya Ding Key Laboratory of Drug Quality Control and pharmacovigilance Ministry of EducationChina Pharmaceutical UniversityNanjing 210009China Beijing Key Laboratory for Magnetoelectric Materials and Devices Beijing Innovation Center for Engineering Science and Advanced TechnologySchool of Materials Science and EngineeringPeking UniversityBeijing 100871China Department of Biochemistry School of Life Science and TechnologyChina Pharmaceutical UniversityNanjing 210009China

Rational design and exploitation of nanomaterials with superior treatment properties for suitable indications is a way out to relieve cost constraint of therapy and solve the unsatisfactory efficacy for cancer *** this work,we propose a greatly facile approach to produce heterogeneous Pd-Au nanorods(Pd-Au NRs)that solve the current bottleneck problems of photothermal thermal therapy(PTT)as well as completely eliminate tumors in animal models without toxic side *** Pd clusters on both tips of Au NRs offers Pd-Au NRs three novel functions,i.e.,the extension of the absorption into NIR-Ⅱ region,the activation of prodrug of 5-fluorouracil(5-Fu)via the bioorthogonal reaction,and the peroxidase-mimic activity to produce·*** heterogeneous nanorods showed a high and stable photothermal conversion efficiency(52.07%)in a safer NIR-Ⅱ irradiation region(1,064 nm),which not only eliminate most of tumor cells at only one dose of the irradiation for 5 min but also improve the in situ conversion of 5-fluoro-1-propargyluracil and H2O2 into active 5-Fu and·OH to eradicate residual tumors for inhibiting tumor *** dual catalytic activity-synergistic mechanism of PTT demonstrates the importance of material design in solving current bottleneck problem of tumor therapy.

关键词： heterogeneous nanorods Pd-Au photothermal therapy bioorthogonal catalysis peroxidase-mimic activity

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Rapid quantification of the metabolite of valacyclovir hydrochloride in human plasma by liquid chromatography-tandem mass spectrometry

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Journal of Pharmaceutical Analysis 2010年第2期22卷 83-90页

作者： Yuan Tian1,2,Hui Lin1,2,Xue-Yu Zhang1,2,Zun-Jian Zhang1,2,Guo-Guang Mao31. Key Laboratory of Drug Quality Control and pharmacovigilance (China Pharmaceutical University),Ministry of Education,Nanjing 210009 2. Center for Instrumental Analysis,China Pharmaceutical University,Nanjing 210009 3. Department of Clinical Pharmacology,Wannan Medical College,Wuhu 241000,China. Key Laboratory of Drug Quality Control and pharmacovigilance (China Pharmaceutical University) Ministry of Education Nanjing 210009 China Center for Instrumental Analysis China Pharmaceutical University Nanjing 210009 China Department of Clinical Pharmacology Wannan Medical College Wuhu 241000 China

Objective To establish a rapid,sensitive and selective liquid chromatography-tandem mass spectrometry (LC-MS/MS) method for the determination of acyclovir (the metabolite of valacyclovir hydrochloride) in human plasma. Methods After addition of ganciclovir as internal standard (IS),plasma samples were prepared by one-step protein precipitation using acetonitrile as precipitant,followed by an isocratic elution with 0.1% formic acid solution-methanol (95∶5,v/v) on an Agilent ZORBAX SB-C18 (150mm×2.1mm i.d.,3.5μm) column. Detection was performed on a triple-quadrupole mass spectrometer utilizing electrospray ionization (ESI) interface operating in positive ion and selected reaction monitoring (SRM) mode with the precursor to product ion transitions m/z 226.2→152.1 for acyclovir and m/z 256.2→152.1 for the IS. Results The analytical results demonstrated a good linearity over the ranges from 0.005 to 4μg/mL (r=0.9999) for valacyclovir hydrochloride. The relative standard deviations (RSD) of intra-batch and inter-batch were less than 4.06% and 9.23%,respectively. The limit of detection and lower limit of quantification in human plasma were 2ng/mL and 5ng/mL,respectively. Conclusion The method was simple,sensitive,accurate and reproducible and has been successfully applied to a bioequivalence study of valacyclovir hydrochloride capsules in Chinese healthy male volunteers.

关键词： valacyclovir hydrochloride acyclovir liquid chromatography-tandem mass spectrometry method validation human plasma

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