abstract：:Lappaconitine (LA) has been widely used for postoperative and cancer pain control. LA exhibits excellent analgesic activity with a longer effective time than common local anesthetics such as tetracaine and bupivacaine. However, the mechanisms underlying the featured analgesic activity of LA remain largely unknown. Her...

journal_title：Acta pharmacologica Sinica

authors： Li YF,Zheng YM,Yu Y,Gan Y,Gao ZB

更新日期：2019-04-01 00:00:00

abstract：:The chemokine receptor CCR5 is an important anti-HIV (human immunodeficiency virus) drug target owning to its pivotal role in HIV-1 viral entry as a co-receptor. Here, we present a 2.9 Å resolution crystal structure of CCR5 bound to PF-232798, a second-generation oral CCR5 antagonist currently in phase II clinical tri...

journal_title：Acta pharmacologica Sinica

authors： Zhu Y,Zhao YL,Li J,Liu H,Zhao Q,Wu BL,Yang ZL

更新日期：2019-04-01 00:00:00

abstract：:Volatile anesthetics improve postischemic cardiac function and reduce infarction even when administered for only a brief time at the onset of reperfusion. A recent study showed that sevoflurane postconditioning (SPC) attenuated myocardial reperfusion injury, but the underlying mechanisms remain unclear. In this study,...

journal_title：Acta pharmacologica Sinica

authors： Qiao SG,Sun Y,Sun B,Wang A,Qiu J,Hong L,An JZ,Wang C,Zhang HL

更新日期：2019-01-01 00:00:00

abstract：:Terpene lactones are a class of bioactive constituents of standardized preparations of Ginkgo biloba leaf extract, extensively used as add-on therapies in patients with ischemic cardiovascular and cerebrovascular diseases. This investigation evaluated human pharmacokinetics of ginkgo terpene lactones and impact of the...

journal_title：Acta pharmacologica Sinica

authors： Liu XW,Yang JL,Niu W,Jia WW,Olaleye OE,Wen Q,Duan XN,Huang YH,Wang FQ,Du FF,Zhong CC,Li YF,Xu F,Gao Q,Li L,Li C

更新日期：2018-12-01 00:00:00

abstract：:The serum and glucocorticoid-regulated kinase (SGK) family has been implicated in the regulation of many cellular processes downstream of the PI3K pathway. It plays a crucial role in PI3K-mediated tumorigenesis, making it a potential therapeutic target for cancer. SGK family consists of three isoforms (SGK1, SGK2, and...

journal_title：Acta pharmacologica Sinica

authors： Gong GQ,Wang K,Dai XC,Zhou Y,Basnet R,Chen Y,Yang DH,Lee WJ,Buchanan CM,Flanagan JU,Shepherd PR,Chen Y,Wang MW

更新日期：2018-12-01 00:00:00

abstract：:Telomere shortening is associated with idiopathic pulmonary fibrosis (IPF), a high-morbidity and high-mortality lung disease of unknown etiology. However, the underlying mechanisms remain largely unclear. In this study, wild-type (WT) mice with normal telomeres and generation 3 (G3) or G2 telomerase RNA component (TER...

journal_title：Acta pharmacologica Sinica

authors： Liu YY,Shi Y,Liu Y,Pan XH,Zhang KX

更新日期：2018-11-01 00:00:00

abstract：:Activation of the Ca2+/calmodulin-dependent protein kinase II isoform δA (CaMKIIδA) disturbs intracellular Ca2+ homeostasis in cardiomyocytes during chronic heart failure (CHF). We hypothesized that upregulation of CaMKIIδA in cardiomyocytes might enhance Ca2+ leak from the sarcoplasmic reticulum (SR) via activation o...

journal_title：Acta pharmacologica Sinica

authors： Gui L,Guo X,Zhang Z,Xu H,Ji YW,Wang RJ,Zhu JH,Chen QH

更新日期：2018-10-01 00:00:00

abstract：:Liver fibrosis is excessive accumulation of extracellular matrix proteins that results from various chronic liver diseases. Hepatic stellate cells (HSCs) play an essential role in the pathogenesis of liver fibrosis. Danggui Buxue Tang (DBT) is a classic formula of Chinese traditional medicine. We previously showed tha...

journal_title：Acta pharmacologica Sinica

authors： Guo T,Liu ZL,Zhao Q,Zhao ZM,Liu CH

更新日期：2018-09-01 00:00:00

abstract：:Pulmonary fibrosis may be partially the result of deregulated tissue repair in response to chronic hypoxia. In this study we explored the effects of hypoxia on lung fibroblasts and the effects of neotuberostemonine (NTS), a natural alkaloid isolated from Stemona tuberosa, on activation of fibroblasts in vitro and in v...

journal_title：Acta pharmacologica Sinica

authors： Lv XM,Li MD,Cheng S,Liu BL,Liu K,Zhang CF,Xu XH,Zhang M

更新日期：2018-09-01 00:00:00

abstract：:Neuritin is a member of the neurotrophic factor family, which is activated by neural activity and neurotrophins, and promotes neurite growth and branching. It has shown to play an important role in neuronal plasticity and regeneration. It is also involved in other biological processes such as angiogenesis, tumorigenes...

journal_title：Acta pharmacologica Sinica

authors： Yao JJ,Zhao QR,Lu JM,Mei YA

更新日期：2018-09-01 00:00:00

abstract：:Due to the lack of typical clinical symptoms, the average delay time for diagnosis of pulmonary hypertension (PH) is longer than 2 years. It is urgent to find biomarkers for PH diagnosis. In this study we investigated whether plasma microRNAs (miRNAs) can be used as biomarkers for PH diagnosis. We used microarray to i...

journal_title：Acta pharmacologica Sinica

authors： Song XW,Zou LL,Cui L,Li SH,Qin YW,Zhao XX,Jing Q

更新日期：2018-07-01 00:00:00

abstract：:Cardiovascular diseases (CVD) are the leading cause of morbidity and mortality in the world. Although considerable progress has been made in the diagnosis, treatment and prognosis of CVD, there is still a critical need for novel diagnostic biomarkers and new therapeutic interventions to decrease the incidence of this ...

journal_title：Acta pharmacologica Sinica

authors： Zhou SS,Jin JP,Wang JQ,Zhang ZG,Freedman JH,Zheng Y,Cai L

更新日期：2018-07-01 00:00:00

abstract：:miRNAs have shown promise as potential biomarkers for acute myocardial infarction (AMI). However, the current used quantitative real-time PCR (qRT-PCR) allows solely for relative expression of nucleic acids and it is susceptible to day-to-day variability, which has limited the validity of using the miRNAs as biomarker...

journal_title：Acta pharmacologica Sinica

authors： Robinson S,Follo M,Haenel D,Mauler M,Stallmann D,Heger LA,Helbing T,Duerschmied D,Peter K,Bode C,Ahrens I,Hortmann M

更新日期：2018-07-01 00:00:00

abstract：:An early intervention using biomarkers to predict acute myocardial infarction (AMI) will effectively reduce global heart attack incidence, particularly among high-risk patients with type 2 diabetes mellitus (T2DM). This study attempted to identify potential biomarkers by detecting changes in the levels of plasma prote...

journal_title：Acta pharmacologica Sinica

authors： Rahim MAA,Rahim ZHA,Ahmad WAW,Bakri MM,Ismail MD,Hashim OH

更新日期：2018-07-01 00:00:00

abstract：:Cardiac amyloidosis (CA) comprises a heterogeneous group of medical conditions affecting the myocardium. It presents with proteinaceous infiltration with variable degrees of severity, prevalence and evolution. Despite this heterogeneity, erroneous protein folding is the common pathophysiologic process, yielding the fo...

journal_title：Acta pharmacologica Sinica

authors： Luciani M,Troncone L,Monte FD

更新日期：2018-07-01 00:00:00

abstract：:Anlotinib is a new oral tyrosine kinase inhibitor; this study was designed to characterize its pharmacokinetics and disposition. Anlotinib was evaluated in rats, tumor-bearing mice, and dogs and also assessed in vitro to characterize its pharmacokinetics and disposition and drug interaction potential. Samples were ana...

journal_title：Acta pharmacologica Sinica

authors： Zhong CC,Chen F,Yang JL,Jia WW,Li L,Cheng C,Du FF,Zhang SP,Xie CY,Zhang NT,Olaleye OE,Wang FQ,Xu F,Lou LG,Chen DY,Niu W,Li C

更新日期：2018-06-01 00:00:00

abstract：:Contact inhibition and its disruption of vascular smooth muscle cells (VSMCs) are important cellular events in vascular diseases. But the underlying molecular mechanisms are unclear. In this study we investigated the roles of microRNAs (miRNAs) in the contact inhibition and its disruption of VSMCs and the molecular me...

journal_title：Acta pharmacologica Sinica

authors： Sun YY,Qin SS,Cheng YH,Wang CY,Liu XJ,Liu Y,Zhang XL,Zhang W,Zhan JX,Shao S,Bian WH,Luo BH,Lu DF,Yang J,Wang CH,Zhang CX

更新日期：2018-05-01 00:00:00

abstract：:In this brief review we summarize the current fndings relative to the discovery of a small peptide ligand, phoenixin (PNX). Using a bioinformatic approach, two novel peptides PNX-14 and PNX-20 containing 14 and 20 amino acids, respectively, were isolated from diverse tissues including the brain, heart, lung and stomac...

journal_title：Acta pharmacologica Sinica

authors： Lyu RM,Cowan A,Zhang Y,Chen YH,Dun SL,Chang JK,Dun NJ,Luo JJ

更新日期：2018-05-01 00:00:00

abstract：:Organ transplantation is the most effective therapy for patients with end-stage disease. Preservation solutions and techniques are crucial for donor organ quality, which is directly related to morbidity and survival after transplantation. Currently, static cold storage (SCS) is the standard method for organ preservati...

journal_title：Acta pharmacologica Sinica

authors： Jing L,Yao L,Zhao M,Peng LP,Liu M

更新日期：2018-05-01 00:00:00

abstract：:Extracellular vesicles (EVs) comprise apoptotic bodies, microvesicles and exosomes, and they perform as key regulators in cell-to-cell communication in normal as well as diseased states. EVs contain natural cargo molecules, such as miRNA, mRNA and proteins, and transfer these functional cargos to neighboring cells or ...

journal_title：Acta pharmacologica Sinica

authors： Samanta S,Rajasingh S,Drosos N,Zhou Z,Dawn B,Rajasingh J

更新日期：2018-04-01 00:00:00

abstract：:Recent evidence shows that raddeanin A (RA), an oleanane-type triterpenoid saponin extracted from Anemone raddeana Regel, exerts remarkable cytotoxicity against cancer cells in vitro and in vivo. In addition, RA has also been found to activate autophagy in human gastric cancer cells. In this study, we investigated the...

journal_title：Acta pharmacologica Sinica

authors： Guan YD,Jiang SL,Yu P,Wen M,Zhang Y,Xiao SS,Xu XJ,Cheng Y

更新日期：2018-04-01 00:00:00

abstract：:In drug design and discovery, binding affinity and selectivity are two basic properties of a drug candidate. Opioid receptors (ORs) are the main targets of strong analgesics. Like some other class A members of G-protein-coupled receptors (GPCRs), ORs exhibit complex selectivity on their ligands. The diversity of bindi...

journal_title：Acta pharmacologica Sinica

authors： Cheng JX,Cheng T,Li WH,Liu GX,Zhu WL,Tang Y

更新日期：2018-03-01 00:00:00

abstract：:Aberrant activity of enhancer of zeste homolog 2 (EZH2) is associated with a wide range of human cancers. The interaction of EZH2 with embryonic ectoderm development (EED) is required for EZH2's catalytic activity. Inhibition of the EZH2-EED complex thus represents a novel strategy for interfering with the oncogenic p...

journal_title：Acta pharmacologica Sinica

authors： Zhu MR,Du DH,Hu JC,Li LC,Liu JQ,Ding H,Kong XQ,Jiang HL,Chen KX,Luo C

更新日期：2018-02-01 00:00:00

abstract：:Cancer metastasis is responsible for over 90% of breast cancer-related deaths, and inhibiting lymph node metastasis is an option to treat metastatic disease. Herein, we report the use of IR-780-loaded polymeric micelles (IPMs) for effective photothermal therapy (PTT) of breast cancer lymphatic metastasis. The IPMs wer...

journal_title：Acta pharmacologica Sinica

authors： He B,Hu HY,Tan T,Wang H,Sun KX,Li YP,Zhang ZW

更新日期：2018-01-01 00:00:00

abstract：:Recent evidence shows that resveratrol (RSV) may ameliorate high-glucose-induced cardiac oxidative stress, mitochondrial dysfunction and myocardial fibrosis in diabetes. However, the mechanisms by which RSV regulates mitochondrial function in diabetic cardiomyopathy have not been fully elucidated. Mitochondrial dysfun...

journal_title：Acta pharmacologica Sinica

authors： Fang WJ,Wang CJ,He Y,Zhou YL,Peng XD,Liu SK

更新日期：2018-01-01 00:00:00

abstract：:Diabetic retinopathy (DR) is a common complication of diabetes and has been recognized as the leading cause of blindness in adults. Several interrelated molecular pathways are involved in the development of DR. Microvesicles (MVs) are cell membrane vesicles, which carry many biologic molecules, such as mRNAs, microRNA...

journal_title：Acta pharmacologica Sinica

authors： Zhang W,Chen S,Liu ML

更新日期：2018-01-01 00:00:00

abstract：:Hispidulin, a polyphenolic flavonoid extracted from the traditional Chinese medicinal plant S involucrata, exhibits anti-tumor effects in a wide array of human cancer cells, mainly through growth inhibition, apoptosis induction and cell cycle arrest. However, its precise anticancer mechanisms remain unclear. In this s...

journal_title：Acta pharmacologica Sinica

authors： Gao H,Gao MQ,Peng JJ,Han M,Liu KL,Han YT

更新日期：2017-12-01 00:00:00

abstract：:The intercellular communication between leukemia cells and bone marrow mesenchymal stem cells (BM-MSCs) plays more important role in chronic myeloid leukemia (CML) than we previously understood. Recently, we found that microvesicles released from human leukemia cell line K562 (K562-MVs) containing BCR-ABL1 mRNA malign...

journal_title：Acta pharmacologica Sinica

authors： Fu FF,Zhu XJ,Wang HX,Zhang LM,Yuan GL,Chen ZC,Li QB

更新日期：2017-11-01 00:00:00

abstract：:A variety of cardiovascular diseases is accompanied by the loss of vascular contractility. This study sought to investigate the effects of curcumin, a natural polyphenolic compound present in turmeric, on mouse vascular contractility and the underlying mechanisms. After mice were administered curcumin (100 mg·kg-1·d-1...

journal_title：Acta pharmacologica Sinica

authors： Sun SW,Tong WJ,Guo ZF,Tuo QH,Lei XY,Zhang CP,Liao DF,Chen JX

更新日期：2017-10-01 00:00:00

abstract：:Recent evidence shows that dopamine D2-like receptor (D2DR) antagonists, such as trifluoperazine and thioridazine, are effective for cancer therapy and inhibition of cancer stem-like cells (CSCs). In this study, we investigated the anti-cancer effects of combination therapy of dexamethasone (DEX) and sulpiride (SUL), ...

journal_title：Acta pharmacologica Sinica

authors： Li J,Yao QY,Xue JS,Wang LJ,Yuan Y,Tian XY,Su H,Wang SY,Chen WJ,Lu W,Zhou TY

更新日期：2017-09-01 00:00:00

abstract：:Human T-cell lymphotropic virus type 1 (HTLV-1) is the etiologic agent of adult T-cell leukemia/lymphoma (ATL), a rapidly progressing clonal malignancy of CD4+ T lymphocytes. Exploring the host-HTLV-1 interactions and the molecular mechanisms underlying HTLV-1-mediated tumorigenesis is critical for developing efficien...

journal_title：Acta pharmacologica Sinica

authors： Zhang LL,Wei JY,Wang L,Huang SL,Chen JL

更新日期：2017-08-01 00:00:00

abstract：:Over half of patients with BRCA1-deficient cancers do not respond to treatment with poly(ADP-ribose) polymerase (PARP) inhibitors. In this study, we report that a combination of 53BP1 and BRCA1 may serve as a biomarker of PARP inhibitor sensitivity. Based on the mRNA levels of four homologous recombination repair (HR)...

journal_title：Acta pharmacologica Sinica

authors： Yang ZM,Liao XM,Chen Y,Shen YY,Yang XY,Su Y,Sun YM,Gao YL,Ding J,Zhang A,He JX,Miao ZH

更新日期：2017-07-01 00:00:00

abstract：:Recent evidence shows that high glucose levels recruit carbohydrate response element-binding protein, which binds the promoter of thioredoxin-interacting protein (txnip), thereby regulating its expression in β-cells. Overexpression of txnip not only induces β-cell apoptosis but also reduces insulin production. Thus, t...

journal_title：Acta pharmacologica Sinica

authors： Li T,Lin GY,Zhong L,Zhou Y,Wang J,Zhu Y,Feng Y,Cai XQ,Liu Q,Nosjean O,Boutin JA,Renard P,Yang DH,Wang MW

更新日期：2017-07-01 00:00:00

abstract：:Conjugated polymer nanomaterials (CPNs), as optically and electronically active materials, hold promise for biomedical imaging and drug delivery applications. This review highlights the recent advances in the utilization of CPNs in theranostics. Specifically, CPN-based in vivo imaging techniques, including near-infrar...

journal_title：Acta pharmacologica Sinica

authors： Qian CG,Chen YL,Feng PJ,Xiao XZ,Dong M,Yu JC,Hu QY,Shen QD,Gu Z

更新日期：2017-06-01 00:00:00

abstract：:An increasing number of cases of herb-induced liver injury (HILI) have been reported, presenting new clinical challenges. In this study, taking Polygonum multiflorum Thunb (PmT) as an example, we proposed a computational systems toxicology approach to explore the molecular mechanisms of HILI. First, the chemical compo...

journal_title：Acta pharmacologica Sinica

authors： Wang YY,Li J,Wu ZR,Zhang B,Yang HB,Wang Q,Cai YC,Liu GX,Li WH,Tang Y

更新日期：2017-05-01 00:00:00

abstract：:The signal transducer and activator of transcription 3 (STAT3) plays a critical role in platelet functions. This study sought to understand the effects of the STAT3 inhibitor SC99 on platelet activation and aggregation. Immunoblotting assays were applied to measure the effects of SC99 on the STAT3 signaling pathway. A...

journal_title：Acta pharmacologica Sinica

authors： Xu Z,Xu YJ,Hao YN,Ren LJ,Zhang ZB,Xu X,Cao BY,Dai KS,Zhu L,Fang Q,Kong Y,Mao XL

更新日期：2017-05-01 00:00:00

abstract：:Aspirin (ASA) is a cardioprotective drug with anti-cardiac fibrosis action in vivo. This study was aimed to clarify the anti-cardiac fibrosis action of ASA and the underlying mechanisms. Two heart injury models (injection of isoproterenol and ligation of the left anterior descending branch) were used in mice to induce...

journal_title：Acta pharmacologica Sinica

authors： Liu PP,Liu HH,Sun SH,Shi XX,Yang WC,Su GH,Zhao J

更新日期：2017-04-01 00:00:00

abstract：:Human enterovirus 71 (EV71) is the primary causative agent of recent large-scale outbreaks of hand, foot, and mouth disease (HFMD) in Asia. Currently, there are no drugs available for the prevention and treatment of HFMD. In this study, we compared the anti-EV71 activities of three natural compounds, rheum emodin, art...

journal_title：Acta pharmacologica Sinica

authors： Zhong T,Zhang LY,Wang ZY,Wang Y,Song FM,Zhang YH,Yu JH

更新日期：2017-03-01 00:00:00

abstract：:Proprotein convertase subtilisin/kexin type 9 (PCSK9), also known as neural apoptosis regulated convertase (NARC1), is a key modulator of cholesterol metabolism. PCSK9 increases the serum concentration of low-density lipoprotein cholesterol by escorting low-density lipoprotein receptors (LDLRs) from the membrane of he...

journal_title：Acta pharmacologica Sinica

authors： He NY,Li Q,Wu CY,Ren Z,Gao Y,Pan LH,Wang MM,Wen HY,Jiang ZS,Tang ZH,Liu LS

更新日期：2017-03-01 00:00:00

abstract：:The therapeutic outcome of chemotherapy is severely limited by intrinsic or acquired drug resistance, the most common causes of chemotherapy failure. In the past few decades, advancements in nanotechnology have provided alternative strategies for combating tumor drug resistance. Drug-loaded nanoparticles (NPs) have se...

journal_title：Acta pharmacologica Sinica

authors： Liu JP,Wang TT,Wang DG,Dong AJ,Li YP,Yu HJ

更新日期：2017-01-01 00:00:00