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Baicalin significantly inhibit the herpes simplex virus type 1 alkaline nuclease and stop herpes simplex virus type 1 replication

Baicalin significantly inhibit the herpes simplex virus type...

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第二届世界天然药物和传统药物药理学学术会议

作者： Tian CHEN Hong-Yu CHEN Lei ZHANG Kang CAO Maria G MASUCCI School of Preclinical Medicine Chengdu Medical CollegeChengdu 610083China Department of Cell and Molecular Biology Karolinska InstituteBox 28517177 StockholmSweden School of Preclinical MedicineChengdu Medical CollegeChengdu 610083China Department of Cell and Molecular BiologyKarolinska InstituteBox 28517177 StockholmSweden

AIM In order to find an effective antiviral drug against the herpes simplex virus type 1 (HSV-1) and understand its mechanism, we have screened alkalescence endonuclease (AN)-dependent *** We have constructed a plasmid,pET28-UL12, with an insertion of a DNA fragment containing the UL12 gene of HSV-1 SM44, which is 99.2% homologous to the UL12 (Gene ID: 2703382 from the GenBank), into the prokaryotic expression vector *** transformation in Escherichia coli, only kalamycin-resistant clones were *** of recombinant proteins in Escherichia coli restored the natural activity of the *** The anti-AN activities detected in several drugs extracted from herbs were confirmed by different degrees of inhibition on the enzymatic activities, similar to the research in Vero cells that exhibited different levels of inhibiting viral infection by these *** result showed that most of these drugs can dramatically interfere with HSV-1 infection on the Veru cells, but only baicalin can significantly inhibit the rAN and stop HSV-1 *** results showed that Baicalin had a strong interaction with critical amino acid residues of AE (identity 21.12%, similar residues 41.35%, compared with rAN by DNAMAN 6.0, data not shown) which was expressed by Epstein-Barr *** This DNA degradation assay is a useful tool to rapidly screen the inhibitors of HSV-1 at the molecular level, also representing a potential target for novel antiviral therapies.

关键词： baicalin herpes virus alkaline nuclease inhibitor

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Protective effect of Zige lyophilized powder preconditioning in an hypoxia/reoxygenation model of HUVECs

Protective effect of Zige lyophilized powder preconditioning...

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第二届世界天然药物和传统药物药理学学术会议

作者： Cong-Cong ZHANG Jia-Lan LIU Hui ZHANG Xiao-Yu XU College of Pharmaceutical Sciences Southwest UniversityChongqing Engineering Research Center for Pharmacodynamics EvaluationChongqing 400716China

AIM To study whether Zige lyophilized powder may improve survival of vascular endothelial cells (EC) following ischemia/reperfusion injury was investigated in this *** EC cultured from human umbilical vein were sealed in a flowthrough chamber mounted on an inverted microscope and perfused with a constant flow of Krebs *** 1 h of equilibration,HUVEC underwent 4 h of hypoxia (H) and 1 h of reoxygenation (R) to mimic ischemia/reperfusion, addition of Zige lyophilized powder to culture medium at start of *** H/R caused significant viability loss and an release of LDH increase compared to the normoxic control, 12.5 rag.L-1 Zige lyophilized powder enhanced cell viability(P < 0.05).Also, 49.0, 24.5 and 12.5 rag· L-1 Zige lyophilized powder prevented the decline of SOD activity during H/R(P < 0.05).Furthermore, 24.5 and 12.5 mg·L-1 Zige lyophilized powder significantly inhibited the increase of MDA and NO ***, apoptotic related protein levels were measured by Western blotting ***-2 protein level increased significantly in the 24.5 and 12.5 mg·L-1 Zige lyophilized powder group.49.0, 24.5 and 12.5 mg·L-1 Zige lyophilized powder significantly decreased Bax level and up-regulated Bcl-2/Bax *** activation and apoptosis were monitored in the reoxygenated cells.49.0 and 24.5 rag· L-1 Zige lyophilized powder decreased caspase 3 expression(P <0.01).CONCLUSION The results indicate that Zige lyophilized powder prevents damage H/R induced to HUVEC,the cytoprotection of Zige lyophilized powder appears to be associated with the enhancement of the ability anti-oxidation and anti-apoptosis.

关键词： Zige lyophilized powder hypoxia/reoxygenation injury HUVEC

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ZX-1201 inhibits pancreatic cancer cell PANC-1 epithelial-mesenchymal transition by targeting aquaporin-1 and transforming growth factor-β1

ZX-1201 inhibits pancreatic cancer cell PANC-1 epithelial-me...

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第二届世界天然药物和传统药物药理学学术会议

作者： Yu AN Ye-Fan WANG Yu ZHANG Xue-Jun LI Institute of Systems Biomedicine Peking UniversityBeijing 100191China Institute of Systems BiomedicinePeking UniversityBeijing 100191China State Key Laboratory of Natural & Biomimetic Drugs Department of PharmacologySchool of Basic Medical Sciences

AIM Our present study aimed to test the anti-cancer effect of natural product ZX-1201 on pancreatic cancer cell *** After incubation with different concentrations of drug or vehicle, PANC-1 cell viability was measured by MTS assay, and Scratch assay and Transwell assay were utilized to detect PANC-1 cell ***, morphological changes were recorded by light ***-time PCR, immunofluorescence and Western blot were used to examine change of aquaporin-1 (AQP1) and TGF-β1 related EMT *** addition, we performed AQP1 and TGF-β1 RNAi and over-expression experiments to elucidate their role in anti migratiou effect of *** We found ZX-1201 showed significant inhibitory effect on cell migration in a dose-dependent manner, however, slight cell viability suppression was ***, we demonstrated ZX-1201 could prevent PANC-1 cell from epithelial-mesenehymal transition (EMT), by reducing mesenehymal phenotype, decrease AQP1 and TGF-β1 expression, and dramatically down-regulating EMT markers and signaling ***, we verified that ZX-1201 reversed EMT by targeting AQP1 and TGF-β1, because either AQP1 or TGF-β1 over-expression abolished the inhibitory effect of ZX-1201 on *** ZX-1201 significantly inhibits pancreatic cancer cell PANC-1 EMT process through an AQP1 and TGF-β1 targeting manner.

关键词： ZX-1201 pancreatic cancer PANC-1 epithelial-mesenchymal transition aquaporin-1 transforming growth factor-β1

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Curcumin inhibits renal cyst formation and enlargement in vitro models by regulating MAPK signaling pathway

Curcumin inhibits renal cyst formation and enlargement in vi...

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第二届世界天然药物和传统药物药理学学术会议

作者： Jin-Sheng GAO Hong ZHOU Tian-Luo EEI Li ZHOU Wei-Dong LI Xue-Jun LI Bao-Xue YANG Department of Oncology Shanxi Province hospital of Traditional Chinese MedicineTaiyuan 030012China Department of PharmacologySchool of Basic Medical SciencesPeking Universityand Key Laboratory of Molecular Cardiovascular-SciencesMinistry of EducationBeijing 100191China Department of Pharmacology School of Basic Medical SciencesPeking Universityand Key Laboratory of Molecular Cardiovascular-SciencesMinistry of EducationBeijing 100191China

AIM To identify the inhibitory effect of curcumin on renal cyst development and to explore the molecular *** Madin-Darby canine kidney (MDCK) cyst model and murine embryonic kidney cyst model were used to evaluate inhibitory *** viabihty, proliferation, apoptosis, CFTR function and expression, and MAPK signaling pathway in MDCK cells were determined to clarify the mechanism of curcumin cyst inhibition *** Curcumin was found to significantly inhibit MDCK cyst formation and *** maximum dose curcumin caused 62% inhibition of the cyst formation (IC50 was 0.12 μmol·L-1).Curcumin reduced cyst formation and prevented cyst enlargement in both MDCK cyst model and embryonic kidney cyst model with doseresponse *** neither induced cytotoxicity nor apoptosis in MDCK cells at < 100 *** failed to affect the chloride transporter CFTR expression and ***, cureumin inhibited forskolin-promoted cell proliferation and promoted the tubule formation in MDCK cells, which indicates curcumin promotes MDCK cell ***, curcumin reduced the expressions of MAPK signaling pathway proteins including Ras, B-raf, p-MEK, p-ERK, p-JNK, and p-P38, but increased the expressions of Raf-1 in MDCK cells in the present of *** These results demonstrate that eurcumin inhibits renal cyst formation and enlargement by regulating MAPK signaling pathway, and suggest that curcumin might be developed as a candidate drug for the treatment of polycysfic kidney disease.

关键词： curcumin polycystic kidney disease MAPK signaling pathway

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Echinacoside attenuates 6-hydroxydopmnine-induced neurotoxicity in PC12 cells

Echinacoside attenuates 6-hydroxydopmnine-induced neurotoxic...

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第二届世界天然药物和传统药物药理学学术会议

作者： Yue-Hua WANG Shuo TIAN Guo-Rong HE Lian-Hua FANG Xiao-Ping PU Guan-Hua DU Beijing Key Laboratory of Drug Target Identification and Drug Screening Institute of Materia MedicaChinese Academy of Medical Sciences & Peking Union Medical CollegeBeijing 100050China Beijing Key Laboratory of Drug Target Identification and Drug ScreeningInstitute of Materia MedicaChinese Academy of Medical Sciences & Peking Union Medical CollegeBeijing 100050China Department of Molecular and Cellular PharmacologySchool of Pharmaceutical SciencesPeking UniversityBeijing 100191China Department of Molecular and Cellular Pharmacology School of Pharmaceutical SciencesPeking UniversityBeijing 100191China

AIM To investigate the effects and the underlying mechanism of Echinacoside (ECH) against 6-OHDA-induced injury in *** 6-OHDA was added to cultured PC12 cells after pretreatment for 1 h with different concentration of ECH or saline and co-incubated for another 24 *** evaluate the protective effects of ECH, the morphological change was observed by microscope, the viability of PC12 cells was assayed by MTT *** explore the mechanism of ECH against 6-OHDA neurotoxicity,the mitochondrial oxidation-reduction activity (REDOX), mitochondrial membrane potential (△Ψm), reactive oxygen species (ROS)production, ATP level, cytochrome c release, the activity of caspase 3, and apoptosis in PC12 cells were *** 6-OHDA induced the decrease of cell viability, ROS generation increase, ATP content decrease, mitochondrial dysfunction, and mitochondfia-mediated apoptosis in PC12 *** could attenuate 6-OHDA-induced neurotoxicity, inhibit the collapse of △Ψm, reduce the mitochondrial *** also inhibited cyt c release and caspase 3 *** Our results indicate that ECH attenuates 6-OHDA-induced neurotoxicity through anti-oxidative and anti-apoptosis mediated by mitochondria.

关键词： echinacoside Parkinson' s disease 6-hydroxydopamine

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Hawthorn leaves flavonoids decreases inflammation related to acute myocardial ischemia/reperfusion in anesthetized dogs

Hawthorn leaves flavonoids decreases inflammation related to...

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第二届世界天然药物和传统药物药理学学术会议

作者： Yong-Qiu ZHENG Jian-Hua FU Peng LI Xin-Zhi LI Xiao-Hong SHANG Jian-Xun LIU Xiyuan Hospital of China Academy of Chinese Medical Sciences Beijing 100091China

AIM To investigate the effects and mechanisms of hawthorn leaves flavonoids (HLF) on acute myocardial ischemia/reperfusion in anesthetized *** The acute ischemia models were prepared by ligating left anterior descending (LAD)artery for 60 *** 15 male dogs were divided into 3 groups at random (5 in each group) : blank control (treated with normal saline 3 ml·kg-1) group, HLF 5 and 10 mg·kg-1 group, with an once injection through a femoral vein 5 min before *** experiments adopted epicardial electrocardiogram (EECG) to measure the scope and degree of myocardial ***,neutrophil infiltration in infarct (Inf) and remote site (RS) of myocardial tissue was measured by myeloperoxidase (MPO) activity *** serum interleukin-1 (IL-1) and tumor necrosis factor α (TNF-α) content was quantified by ***, expression of G protein-coupled receptor kinase 2 (GRK2) and NF-κB in Inf and RS tissue were detected by Western *** Ischemia and reperfusion increased the MPO activity and IL-1 and TNF-α *** showed that HLF 10 and 5 mg·kg-1could significantly decrease the degree and scope of myocardial ischemia; markedly inhibit the increase of MPO activity, and IL-1 and TNF-α content induced by myocardial ischemia/***, HLF increased GRK2 expression and inhibited NF-κB expression in Inf *** HLF could improve the situation of acute myocardial ischemia and inhibit the inflammation in dogs, which might be due to its increasing the GRK2 and NF-κB expression.

关键词： hawthorn leaves flavonoids acute myocardial ischemia reperfusion injury inflammation G protein-coupled receptor kinase 2

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S-propargyl-cysteine-induced angiogenesis was mediated through a H2S/VEGFR2/STAT3 axis

S-propargyl-cysteine-induced angiogenesis was mediated throu...

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第二届世界天然药物和传统药物药理学学术会议

作者： Jun-Tao KAN Wei GUO Cheng-Rong HUANG Yi-Zhun ZHU School of Pharmacy Fudan UniversityShanghai 201203China Institutes of Biomedical Sciences Fudan UniversityShanghai 201203China School of PharmacyFudan UniversityShanghai 201203China

AIM We investigated the pro-angiogenic effect of S-propargyl-cysteine (SPRC), a novel water-soluble modulator of endogenous hydrogen sulfide, to provide experimental basis for angiogenesis-mediated dmg therapy of ischemic heart *** Some models such as Transwell and Matrigel plug were carried out to determine the pro-angiogenic effect of SPRC under normal ***-limb ischemia model was induced to explore the angiogenesis in ischemic condition by laser doppler imaging and *** blot and immunofluorescence were used to detect the level and location of *** and CHIP were performed to determine the activation of STAT3 and its downstream *** SPRC promoted cell proliferation, adhesion, migration and tube formation of primary HUVEC and increased angiogenesis ex vivo and in vivo under both normal and ischemic *** former research reported H2S could directly active VEGFR2 by disrupting the disulfide bonds within ***, we found the interaction between VEGFR2 and STAT3 was also enhanced after ***, the elevated phosphorylation of STAT3 induced by SPRC could be abolished by addition of SU5416, an inhibitor of *** addition, SPRC induced translocation of STAT3 to nucleus, followed by transcriptional activation of downstream *** critical roles of STAT3 in SPRC-induced angiogenesis were confirmed by RNA *** SPRC promoted angiogenesis under both normal and ischemic conditions, and effected through a H2S/VEGFR2/STAT3 axis.

关键词： angiogenesis hydrogen sulfide S-propargyl-cysteine STAT3

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Protective effect of Eucalyptus globulus oil on acute and chronic lung inflammation in rats

Protective effect of Eucalyptus globulus oil on acute and ch...

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第二届世界天然药物和传统药物药理学学术会议

作者： Chun-Zhen ZHAO Jian-Ya ZHOU Wei ZHAO Yan WANG Fa-Di TANG Zhejiang Respiratory Drugs Research Laboratory College of MedicineZhejiang UniversityHangzhou 310058China

AIM The effects of Eucalyptus globulus oil (EO) were studied on airway inflammation of chronic obstructive pulmonary disease (COPD) and acute lung injury (ALI) in *** COPD was induced by instilling intratracheally with LPS and Klebsiella pneumonia, and ALI was induced by instilling intratracheally with *** were divided into six groups : control (saline), model group, EO (30, 100 and 300 mg-kg-1, ig), pretnisone acetate (10 mg-kg-1, ig).RESULTS The total leukocyte number in BALF were singnificantly reduced with 300 mg· kg-1 group in acute inflammation of ALI, while in chronic inflammation of COPD, the inflammatory cells in BALF and blood were significantly decreased with 30,100 mg·kg-1 *** is characterized by emphysema and irreversible airway narrowing, and EO group attenuated emphysematous alveolar destruction and thickness of *** 300 mg· kg-1 group obviously decreased expression of activated NF-κB in rat lung tissues of ALI and in vitro inhibited nuclear translocation of NF-κB in alveolar macrophages from ALI *** The most remarkable finding of this study is that EO,characterized by anti-inflammatory and antioxidant property, defended the development of emphysema and remodeling of small airways induced by intratracheal instillation of LPS and Klebsiella pneumonia in *** significantly reduced inflammatory response in both pulmonary and systemic levels, inhibited oxidative stress and regulated antioxidantive transcription factor Nrf2 expression in emphysematous lungs of *** EO protected against LPS-induced inflammatory cell infiltration in lungs of rats possibly through molecular mechanisms of inhibition of NF-κB *** vitro study suggested that EO inhibited nuclear translocation of NF-κB in alveolar macrophages.

关键词： Eucalyptus globulus oil chronic obstructive pulmonary disease acute lung injury inflammation NF-κB

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Acute toxicity of YSY-O1A in zebrafish is evaluated by still water method and ip method

Acute toxicity of YSY-O1A in zebrafish is evaluated by still...

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第二届世界天然药物和传统药物药理学学术会议

作者： Bing-Jie XUE Wei GUO Kan TONG Mei ZHANG Jing-Rong CUI State Key Laboratory of Natural and Biomimetic Drugs School of Pharmaceutical SciencesPeking UniversityBeijing 100091China

AIM YSY-01A, a synthetic derivative of the Bortezomib, shows distictive anticancer action, while there is no any reports about its acute *** order to evaluate the acute toxicity of YSY-01A using the least volume of YSY-01A, the zebrafish model through two delivery mode in vivo were *** addition, we cheek the LD5o of YSY-01A by zebrafish against by *** The zebrafish acute toxicity testing was taken to evaluate the LD5o of YSY-01A treated 96 h by both ip and still water method.0.1 ml YSY-01A solution of 9, 12.9, 18.5, 26.4, 37.7 and 53.9 mg·kg-1 were delivered by ip injection respectively,25 ml YSY-01A solution of 16.8, 24, 34.3, 49, 70 and 100 rag· L-1 were delivered by still water *** mice acute toxicity testing was taken according to the classical acute toxicity method for *** The zebrafish acute toxicity testing suggested that after YSY-01A treated for 96 h, the LD50 by ip was 21.26 mg·kg-1 , while the LD50 by still water method was 32.594 mg·L-1,sorted as acute toxicity level Ⅲ.The LD50 by mice was 22.35 mg· kg-1, which was similar to the value of LD50 by *** Both still water method and ip could measure the LD50 in zebrafish acute toxicity testing, ip method need less drug and very close to the result of acute toxicity of mice.

关键词： YSY-01A acute toxicity testing zebrafish

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Low molecular weight fucoidan (LMWF) against renal ischemia-reperfusion injury via inhibition of the MAPK signaling pathway

Low molecular weight fucoidan (LMWF) against renal ischemia-...

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第二届世界天然药物和传统药物药理学学术会议

作者： Ji-Hui CHEN Bao-Xue YANG Hong ZHOU Department of Pharmacology School of Basic Medical SciencesPeking Universityand Key Laboratory of Molecular Cardiovascular SciencesMinistry of EducationBeijing 100191China

To explore the effect of low molecular weight fucoidan (LMWF) on renal ischemia-reperfusion injury (RIRI) and its *** studied the effects of LMWF in vivo using a RIR *** from mice that underwent IR showed characteristic morphological changes, such as tubular dilatation, and loss of brush border, with renal dysfunction which was demonstrated by increased serum creatinine and BUN *** vitro, we used CoCl2-induced hypoxic model and hypoxia-reoxygenation injury model which is known to mirror the response obtained in animal models of *** treatment protected kidney against renal damage induced by IR in *** suppressed activation of MAPK, which consequently resulted in a significant decrease in the expression of cyto-c, Bax/Bcl-2 and cleaved caspase 3/caspase 3 ratios, phosphorylation of *** accordance with these biochemical changes,the histologic evaluation of the tissues revealed that LMWF was effective at protecting the kidneys against IR, and that this protective effect led to the restoration of renal function and balance of oxidative stress and antioxidative *** vitro we also investigated the effect of LMWF on cells subjected to chemical hypoxia or hypoxia-reoxygenation, and the intracelhlar signaling pathways in HK2 *** of HK-2 cells with LMWF1-20 g·ml-1 alleviated both the CoCl2-induced and hypoxia-reoxygenation induced loss of cell viability and dissipation of ΔΨ*** also inhibited activation of MAPK, which resulted in a significant decrease in the expression of cyto-c, Bax/Bcl-2 and cleaved caspase 3/caspase 3 ratios, and reduced pbosphorylation of p53 in a dose-dependent *** conclusion, our results firstly indicated LMWF ameliorates acute RIRI via suppressing MAPK signaling pathway in vivo and in vitro,which suggests that LMWF may serve as an potential therapeutic agent for the treatment of acute RIRI.

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