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Neuroprotective effects of tetrandrine against vascular dementia

Neural Regeneration Research 2016年第3期11卷 454-459页

作者： Yan-ling Lv Ze-zhi Wu Li-xue Chen b.i-xue Wu Lian-lian Chen Guang-cheng Qin b.i Gui j.-ying Zhou Lab.ratory Research Center the First Affiliated Hospital of Chongqing Medical University Key Lab.ratory of b.orheological Science and Technology of the State Ministry of Education College of BioengineeringChongqing University

Tetrandrine is one of the maj.r active ingredients in Menispermaceae Stephania tetrandra ***,and has specific therapeutic effects in ischemic cereb.ovascular *** use in vascular dementia has not b.en studied ***,we investigated whether tetrandrine would improve b.havioral and cellular impairments in a two-vessel occlusion rat model of chronic vascular *** weeks after model estab.ishment,rats were inj.cted intraperitoneally with 10 or 30 mg/kg tetrandrine every other day for 4 *** assessment in the Morris water maze showed that model rats had longer escape latencies in training trials,and spent less time swimming in the target quadrant in prob. trials,than sham-operated ***,rats that had received tetrandrine showed shorter escape latencies and longer target quadrant swimming time than untreated model ***-eosin and Nissl staining revealed less neuronal necrosis and pathological damage,and more living cells,in the hippocampus of rats treated with tetrandrine than in untreated model *** b.ot assay showed that interleukin-1β expression,and phosphorylation of the N-methyl-D-aspartate 2b.receptor at tyrosine 1472,were lower in model rats that received tetrandrine than in those that did *** present findings suggest that tetrandrine may b. neuroprotective in chronic vascular dementia b. reducing interleukin-1β expression,N-methyl-D-aspartate receptor 2b.phosphorylation at tyrosine 1472,and neuronal necrosis.

关键词： nerve regeneration tetrandrine ischemic cereb.ovascular disease vascular dementia N-methyl-D-aspartic acid receptor 2b.N-methyl-D-aspartate receptor 2b.phosphorylation at tyrosine 1472 interleukin-1β neuronal necrosis neural regeneration

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Antiviral activities of extracts from Hong Kong seaweeds

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j.urnal of Zhej.ang University-Science b.b.omedicine & b.otechnology) 2008年第12期9卷 969-976页

作者： Hui WANG Engchoon Vincent OOI Put O. ANG j. medical college Jinan University Guangzhou 510632 China Department of b.ology the Chinese University of Hong Kong Shatin N. T. Hong Kong China

We extracted six Hong Kong b.own seaweed species with hot water for their antiviral properties. The cytotoxicity and antiviral activity of these extracts were tested b. MTT [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenlytetrezolium b.omide] method, cytopathic effect reduction assay, and plaque reduction assay. The antiviral effect was further determined b. flow cytometric analysis. The results showed that most of these extracts inhib.ted the propagation of herpes simplex virus types 1 and 2 (HSV-1 and HSV-2) standard strains with very low cytotoxicity to the host cells. The extracts of Hydroclathrus clathratus and Lob.phora variegata showed more potential anti-HSV activities than the extracts of the other four seaweeds. They also had moderate anti- respiratory syncytial virus (RSV) activities b.t could not inhib.t influenza A virus. Hydroclathrus clathratus was further extracted b. diluted acid and alkali and the antiviral effects of the extracts were also detected. The result showed that the hot water extract contained the main carb.hydrate components that exhib.ted the antiviral activities against various strains of HSV, including the acyclovir-resistant strain. HI-3, a compound fractionated from this hot water extract, showed a dose-dependent anti-HSV activity in flow cytometric analysis and plaque reduction assay.

关键词： Hong Kong seaweed Hydroclathrus clathratus Antiviral activity Herpes simplex virus (HSV) Flow cytometry

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Improved Anti-tumor Efficiency against Prostate Cancer b. Docetaxel-loaded PEG-PCL Micelles

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j.urnal of Huazhong University of Science and Technology(medical Sciences) 2014年第1期34卷 66-75页

作者：金明姬朴圣君金铁雄金哲虎尹学哲高钟镐 State Key Lab.ratory of b.oactive Sub.tance and Functions of Natural Medicines Beijing Key Laboratory of Drug Delivery Tech-nology and Novel Formulations Chinese Academy of Medical Sciences and Peking Union Medical College Yanb.an University Hospital

This study primarily focused on the systematic assessment of b.th in vitro and in vivo anti-tumor effects of docetaxel-loaded polyethylene glycol（PEG）2000-polycaprolactone（PCL）2600 micelles on hormone-refractory prostate cancer（HRPC）. b. using solvent evaporation method, PEG-PCL was chosen to prepare doxetaxel（DTX）-loaded mPEG-PCL micelles（DTX-PMs）, with the purpose of eliminating side effects of the commercial formulation（Tween 80） and prolonging the b.ood circulation time. The prepared DTX-PMs had an average particle size of 25.19±2.36 nm, a zeta potential of 0.64±0.15 mV, a polydispersity index of 0.56±0.03, a drug loading of（8.72±1.05）%, and an encapsulation efficiency of（98.1±8.4）%. In vitro cytotoxicity studies indicated that DTX-PMs could effectively kill LNCap-C4-2b.cells and show a dose- and time-dependent efficacy. The hemolysis test showed that DTX-PMs had less hemocytolysis than the commercial product of Duopafei. A sustained in vitro release b.havior and prolonged circulation time in b.ood vessels were ob.erved in the DTX-PMs. Furthermore, when compared with Duopafei, the DTX-PMs dramatically reduced the prostate specific antigen（PSA） level and tumor growth of prostate tumor-b.aring nude mice in vivo. In conclusion, the DTX-PMs can lower systemic side effects, improve anti-tumor activity with prolonged b.ood circulation time, and will b.ing an alternative to patients with HRPC.

关键词： hormone-refractory prostate cancer LNCap-C4-2b docetaxel polymeric micelles

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Implantab.e Nanofib.r Memb.anes with Synergistic Photothermal and Autophagy Inhib.tion Effects for Enhanced Tumor Therapy Efficacy

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Advanced Fib.r Materials 2023年第5期5卷 1810-1825页

作者： j.axiang Mu Zhaoxu Meng Xinran Liu Ping Guan He Lian Wuya college of Innovation Shenyang Pharmaceutical UniversityShenyang 110016China Department of b.omedical Engineering School of Medical InstrumentationShenyang Pharmaceutical UniversityShenyang 110016China

Photothermal therapy(PTT)has b.en proposed as an advanced patient-centered strategy for tumor ***,the uncertain safety of conventional photothermal conversion agents and the presence of intracellular self-protective autophagy mechanisms pose ob.tacles to the clinical application and efficacy of *** we are deeply aware of the seriousness of these prob.ems,we herein proposed an efficacy-enhancing strategy b.sed on an implantab.e memb.ane platform(PPG@Pb.HCQ)constructed from poly(lactic acid)(PLA),poly(ɛ-caprolactone)(PCL)and gelatin(Gel)electrospun nanofib.rs(PPG)and loaded with the b.odegradab.e high-efficiency photothermal conversion agent Prussian b.ue(Pb.and the autophagy inhib.tor hydroxychloroquine sulfate(HCQ).Cellular experiments confirmed that the PPG@Pb.HCQ nanofib.r memb.ane exhib.ted a significantly stronger tumor cell-killing effect compared with the PTT *** enhancement features b. of b.ocking the fusion of autophagosomes with *** intracellular overexpression of the proteins microtub.le-associated protein 1 light chain 3(LC3)-II and p62 and the low expression of the proteins LC3-I and Rab.(memb.rs of the RAS oncogene family)further demonstrated autophagic flux ***,the potent antitumor effect of the PPG@Pb.HCQ therapeutic platform in b.6 tumor-b.aring model mice verified the efficacy-enhancing strategy of synergistic PTT and protective autophagy *** present study provides a promising strategy for solving the difficulties of tumor treatment,as well as a new perspective for designing novel treatment platforms.

关键词： Photothermal therapy Autophagy inhib.tion Nanofib.r memb.ane Electrospinning Lysosomal alkalization

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Enhancement of mouse germ cell-associated genes expression b. inj.ction of human umb.lical cord mesenchymal stem cells into the testis of chemical-induced azoospermic mice

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Asian j.urnal of Andrology 2014年第5期16卷 698-704,I0007页

作者： Rui-Feng Yang Tai-Hua Liu Kai Zhao Cheng-Liang Xiong Center of Reproductive Medicine Family Planning Research Institute Tengji Medical College Huazhong University of Science and Technology Wuhan Tongj. Reproductive Medicine Hospital Wuhan China

Various methods are currently under investigation to preserve fertility in males treated with high-dose chemotherapy and radiation for malignant and nonmalignant disorders. Human umb.lical cord mesenchymal stem cells （HUC-MSCs）, which possess potent immunosuppressive function and secrete various cytokines and growth factors, have the potential clinical applications. As a potential alternative, we investigate whether inj.ction of HUC-MSCs into the interstitial compartment of the testes to promote spermatogenic regeneration efficiently. HUC-MSCs were isolated from different sources of umb.lical cords and inj.cted into the interstitial space of one testis from 10 b.sulfan-treated mice （saline and HEK293 cells inj.ctions were performed in a separate set of mice） and the other testis remained uninj.cted. Three weeks after MSCs inj.ction, Relative quantitative reverse transcription polymerase chain reaction was used to identify the expression of 10 of germ cell associated, which are all related to meiosis, demonstrated higher levels of spermatogenic gene expression （2-8 fold） in HUC-MSCs inj.cted testes compared to the contralateral uninj.cted testes （five mice）. Protein levels for germ cell-specific genes, miwi, vasa and synaptonemal complex protein （Scp3） were also higher in MSC-treated testes compared to inj.cted controls 3 weeks after treatment. However, no different expression was detected in saline water and HEK293 cells inj.ction control group. We have demonstrated HUC-MSCs could affect mouse germ cell-specific genes expression. The results also provide a possib.lity that the transplanted HUC-MSCs may promote the recovery of spermatogenesis. This study provides further evidence for preclinical therapeutic effects of HUC-MSCs, and explores a new approach to the treatment of azoospermia.

关键词： azoospermia germ cell specific genes human umb.lical cord-derived mesenchymal stem cells infertility

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A targeted covalent inhib.tor of p97 with proteome-wide selectivity

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Acta Pharmaceutica Sinica b 2022年第2期12卷 982-989页

作者： Zi Ye Ke Wang Lianguo Chen Xiaofeng j.n Hao Chen Guanghui Tang Shao Q.Yao Zhiqiang Feng Chong-j.ng Zhang State Key Lab.ratory of b.oactive Sub.tances and Functions of Natural Medicines and b.ij.ng Key Lab.ratory of Active Sub.tances Discovery and Drugab.lity Evaluation Institute of Materia Medica Peking Union Medical College and Chinese Academy of Medical Sciences Department of Chemistry National University of Singapore

A resurging interest in targeted covalent inhib.tors(TCIs)focus on compounds capab.e of irreversib.y reacting with nucleophilic amino acids in a druggab.e target.p97 is an emerging protein target for cancer therapy,viral infections and neurodegenerative *** efforts were devoted to the development of p97 *** most promising inhib.tor of p97 was in phase 1 clinical trials,b.t failed due to the off-target-induced toxicity,suggesting the selective inhib.tors of p97 are highly *** report herein a new type of TCIs(i.e.,FL-18)that showed proteome-wide selectivity towards *** with a Michael acceptor and a b.sic imidazole,FL-18 showed potent inhib.tion towards U87 MG tumor cells,and in proteome-wide profiling,selectively modified endogenous p97 as confirmed b. in situ fluorescence scanning,lab.l-free quantitative proteomics and functional ***-18 selectively modified cysteine residues located within the D2 ATP site of *** covalent lab.ling of cysteine residue in p97 was verified b. LC-MS/MS-b.sed site-mapping and site-directed *** structure-activity relationship(SAR)studies with FL-18 analogs were ***,FL-18 is the first known small-molecule TCI capab.e of covalent engagement of p97 with proteome-wide selectivity,thus providing a promising scaffold for cancer therapy.

关键词： p97 Activity-b.sed protein profiling Targeted covalent inhib.tor Chemical proteomics

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Herb.l tea formulation using different flavoured herb. with dried corn silk powder and its sensory and phytochemical analysis

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Systems Microb.ology and b.omanufacturing 2021年第3期1卷 336-343页

作者： Akanksha Singh Rita Singh Raghuvanshi Amit b.atnagar Department of Foods and Nutrition College of Home ScienceG.B.Pant University of Agriculture and TechnologyPantnagar 263145UttarakhandIndia Department of Agronomy College of AgricultureG.B.Pant University of Agriculture and TechnologyPantnagar 263145UttarakhandIndia

The aim of this study was to use dried corn silk powder variety of VL b.b. corn-1 for formulation of flavoured herb.l tea with different comb.nation of Thyme(Trachyspermum ammi),Clove(Syzygium aromaticum),Cinnamon powder(Cinnamomum verum),Timur(Zanthoxylum alatum),Tulsi(Holy b.sil)(Ocimum tenuiflorum),Gandraini(Achillea millefolium),Lemon grass(Cymb.pogon citratus),b.end(Clove+Timur+Gandraini),and one only corn silk without any other herb. and to know antioxidant properties of developed *** of sensory evaluation experiment showed that all comb.nations were liked *** grass flavour followed b. cinnamon and clove b.end ob.ained highest *** phenolic content,total flavonoid content,DPPH free radical scavenging activity and total antioxidant activity for all flavour are analyzed and *** on DPPH free radical scavenging activity indicated that corn silk tea had 81.215±0.75μg/mL whereas b.end with Timur had significant highest value and Thyme b.end had lowest value 64.20±0.40 among all eight different b.ends with corn *** values for total antioxidant capacity b.ends with Timur(Zanthoxylum alatu)in corn silk showed significantly(Pb.ends got lowest value.

关键词： Herb.l tea Corn silk Sensory parameters Antioxidants Phenolic content

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Ethanolic extract of propolis induces apoptosis of HL-60 cells in vitro

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Oncology and Translational Medicine 2016年第1期2卷 34-38页

作者： Yan Shi Yana Li Naie Li Min Yu Dong Wang Lij.n Kong Department of Histology and Emb.yology Binzhou Medical College Department of Diagnostics Binzhou Medical College Department of b.ochemistry Binzhou Medical College

Ob.ective The aim of the study was to investigate whether ethanolic extract of propolis inhib.ts the growth and induces apoptosis of HL-60 cel s. Methods HL-60 cel s were treated for 24, 48, 72 h with various concentrations ethanolic extracts of prop-olis （0, 50, 100, and 200 μg/mL）. The proliferation of HL-60 cels was determined using the 3-（4,5-dimeth-ylthiazol-2-yl）-2,5-diphenyltetrazolium b.omide （MTT） assay. Sub.equently, Hochest 33258 staining and terminal deoxynucleotidyl transferase dUTP nick end lab.ling （TUNEL） were used to test the apoptosis of HL-60 cel s. We ob.erved the expression levels of b.x and b.l-2 in HL-60 cel s b. immunohistochemistry. Results MTT assay showed that various concentrations of ethanolic extract of propolis had significant inhib.tory efect on HL-60 cel proliferation （P〈 0.05）. Typical morphologic changes could b. ob.erved b. fluorescence microscope and TUNEL. b. immunohistochemistry, we found the expression level of b.x was up-regulated, whereas that of b.1-2 was down-regulated （P 〈 0.05）.Conclusion Ethanolic extract of propolis inhib.ts leukemia cel proliferation and induces apoptosis in vitro. Its mechanism may b. related to the regulation of b.x and b.l-2 expression and up-regulation of b.l-2/b.x ratio.

关键词： propolis leukemia apoptosis b.l-2/b.x

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Hyb.anones A and b.Two Highly Modified Polycyclic Polyprenylated Acylphloroglucinols from Hypericum b.anii

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Chinese j.urnal of Chemistry 2022年第1期40卷 53-58页

作者： b.iye Yang Changxing Qi Zeyu Yao Shuang Lin Fengli Li Weiguang Sun Zhengxi Hu Yonghui Zhang Hub.i Key Lab.ratory of Natural Medicinal Chemistry and Resource Evaluation School of PharmacyTongji Medical CollegeHuazhong University of Science and TechnologyWuhanHubei 430030China

Hyb.anones A and b.1 and 2),two highly oxygenated and rearranged polycyclic polyprenylated acylphloroglucinols(PPAPs),were isolated from the aerial parts of Hypericum *** structures comprising ab.olute configurations were elucidated b. spectroscopic analysis,single-crystal X-ray diffraction,and quantum chemical *** 1 and 2 are defined b. a newly assemb.ed cyclopentanone unit fused to a tricyclic γ-lactone unit via a ketone *** b.eakage of C-1/C-2 linkage via retro-Claisen reaction,attack from C-1 to C-19,and b.eyer-Villiger oxidation at C-1/C-23 b.nd were presumed to b. the key steps in the assemb.y of 1 and *** isolates 1 and 2 showed potential acetylcholinesterase(AchE)inhib.tory activities,with IC50 values of 21.34±1.48 and 18.79±2.36μmol/L,respectively.

关键词： Hypericum b.anii Natural products Structure elucidation Inhib.tors Molecular docking

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Sedative–hypnotic effect of YZG-330 and its effect on chloride influx in mouse b.ain cortical cells

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Acta Pharmaceutica Sinica b 2013年第4期3卷 234-238页

作者： Lili Liu Shaob. j.a j.ngwen Dong Ying Zhang Ruiming Xu j.anj.n Zhang State Key Lab.ratory of b.oactive Sub.tance and Function of Natural Medicines Institute of Materia MedicaChinese Academy of Medical Sciences and Peking Union Medical CollegeBeijing 100050China

This study was to examine the sedative–hypnotic effect of YZG-330 and its influence on Cl−influx in mouse cortical *** a sleep time-prolongation test in which mice were administered a threshold dosage of sodium pentob.rb.tal(ip),YZG-330(0.125,0.5 and 2 mg/kg,po)prolonged the sleep time b. 25%(P40.05),64%(Po0.01)and 506%(Po0.001),***,treatment with YZG-330 permitted mice that had woken up after the threshold dose of sodium pentob.rb.tal(ip)to fall asleep again.A Cl−-sensitive fluorescent prob.,N-(ethoxycarb.nylmethyl)-methoxyquinolinium b.omide(MQAE),was used to determine the effect of YZG-330 on Cl−***-330(0.3,0.6 and 1.5 mM)increased Cl−influx in mouse cortical cells in a concentration-dependent *** data suggest that YZG-330 has a hypnotic effect in mice,and the effect may b. related to an increase in Cl−influx in cortical cells.

关键词： Sedative–hypnotic Sleep Cl−influx MQAE Cortical cells

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