abstract：:KCNQ1 channel is a member of the voltage-gated potassium channel KQT-like subfamily. The KCNQ1 gene has recently been identified as a susceptibility locus for type 2 diabetes mellitus (T2DM). In the present study, we examined the effects of KCNQ1 variants on the therapeutic response to modified-release gliclazide (gli...

journal_title：Acta pharmacologica Sinica

authors： Li Q,Tang TT,Jiang F,Zhang R,Chen M,Yin J,Bao YQ,Cheng X,Hu C,Jia WP

更新日期：2017-01-01 00:00:00

abstract：AIM:Phosphodiesterase 4 (PDE4) isozymes are involved in different functions, depending on their patterns of distribution in the brain. The PDE4 subtypes are distributed in different inflammatory cells, and appear to be important regulators of inflammatory processes. In this study we examined the effects of ferulic acid...

journal_title：Acta pharmacologica Sinica

authors： Huang H,Hong Q,Tan HL,Xiao CR,Gao Y

更新日期：2016-12-01 00:00:00

abstract：AIM:Experimental studies found that cinacalcet (CINA) markedly attenuated vascular calcification in uremic rats, but its underlying mechanisms are still largely unknown. Recent evidence have demonstrated that endothelial cells (ECs) participate in ectopic calcification in part by mediating endothelial-to-mesenchymal tr...

journal_title：Acta pharmacologica Sinica

authors： Wu M,Tang RN,Liu H,Pan MM,Liu BC

更新日期：2016-11-01 00:00:00

abstract：AIM:Retinoic acid receptor-related orphan nuclear receptors (RORs) are orphan nuclear receptors that show constitutive activity in the absence of ligands. Among 3 subtypes of RORs, RORc is a promising therapeutic target for the treatment of Th17-mediated autoimmune diseases. Here, we report novel RORc inverse agonists ...

journal_title：Acta pharmacologica Sinica

authors： Wu XS,Wang R,Xing YL,Xue XQ,Zhang Y,Lu YZ,Song Y,Luo XY,Wu C,Zhou YL,Jiang JQ,Xu Y

更新日期：2016-11-01 00:00:00

abstract：AIM:Glucagon-like peptide-1 (GLP-1) agonists and dipeptidyl peptidase-4 (DPP-4) inhibitors can not only lower blood glucose levels, but also alleviate cardiac remodeling after myocardial ischemia and hypertension. In the present study, we investigated the effects of a DPP-4 inhibitor (linagliptin) and a GLP-1 activator...

journal_title：Acta pharmacologica Sinica

authors： Wang XW,Zhang FX,Yang F,Ding ZF,Agarwal N,Guo ZK,Mehta JL

更新日期：2016-09-01 00:00:00

abstract：AIM:Pim-2 is a short-lived serine/threonine kinase, which plays a key role in metastasis of breast cancer through persistent activation of STAT3. Although the crystal structure of Pim-2 has been reported, but thus far no specific Pim-2-targeted compounds have been reported. In this study, we identified a novel Pim-2 in...

journal_title：Acta pharmacologica Sinica

authors： Zhao YQ,Yin YQ,Liu J,Wang GH,Huang J,Zhu LJ,Wang JH

更新日期：2016-09-01 00:00:00

abstract：AIM:Bufalin is one of the active components in the traditional Chinese medicine ChanSu that is used to treat arrhythmia, inflammation and cancer. BF211 is a bufalin derivative with stronger cytotoxic activity in cancer cells. The aim of this study was to identify the putative target proteins of BF211 and the signaling ...

journal_title：Acta pharmacologica Sinica

authors： Sun P,Feng LX,Zhang DM,Liu M,Liu W,Mi T,Wu WY,Jiang BH,Yang M,Hu LH,Guo DA,Liu X

更新日期：2016-07-01 00:00:00

abstract：AIM:The current therapeutic approaches have a limited effect on the dysregulated pulmonary vascular remodeling, which is characteristic of pulmonary arterial hypertension (PAH). In this study we examined whether salvianolic acid A (SAA) extracted from the traditional Chinese medicine 'Dan Shen' attenuated vascular remo...

journal_title：Acta pharmacologica Sinica

authors： Chen YC,Yuan TY,Zhang HF,Wang DS,Yan Y,Niu ZR,Lin YH,Fang LH,Du GH

更新日期：2016-06-01 00:00:00

abstract：AIM:Chinese medicine CGA formula consists of polysaccharide from Cordyceps sinensis mycelia (CS-PS), gypenosides and amygdalin, which is derived from Fuzheng Huayu (FZHY) capsule for treating liver fibrosis. In this study we attempted to confirm the therapeutic effects of CGA formula in dimethylnitrosamine (DMN)-induce...

journal_title：Acta pharmacologica Sinica

authors： Li XM,Peng JH,Sun ZL,Tian HJ,Duan XH,Liu L,Ma X,Feng Q,Liu P,Hu YY

更新日期：2016-06-01 00:00:00

abstract：AIM:The substrate cocktail is frequently used to evaluate cytochrome P450 (CYP) enzyme-mediated drug interactions and potential interactions among the probe substrates. Here, we re-optimized the substrate cocktail method to increase the reliability and accuracy of screening for candidate compounds and expanded the meth...

journal_title：Acta pharmacologica Sinica

authors： Chen ZH,Zhang SX,Long N,Lin LS,Chen T,Zhang FP,Lv XQ,Ye PZ,Li N,Zhang KZ

更新日期：2016-05-01 00:00:00

abstract：AIM:Hyperoside is a flavonol glycoside mainly found in plants of the genera Hypericum and Crataegus, which has shown anti-oxidant, anti-cancer and anti-inflammatory activities. In this study, we investigated the effects of hyperoside on human rheumatoid fibroblast-like synoviocytes (FLSs) in vitro and on mouse collagen...

journal_title：Acta pharmacologica Sinica

authors： Jin XN,Yan EZ,Wang HM,Sui HJ,Liu Z,Gao W,Jin Y

更新日期：2016-05-01 00:00:00

abstract：AIM:We have shown that a combination of ligustrazine and berberine produces more effective inhibition on platelet activation and inflammatory reactions in rat acute myocardial infarction compared with either agent alone. In this study we evaluated the beneficial effects of a combination of ligustrazine and berberine in...

journal_title：Acta pharmacologica Sinica

authors： Zhang Y,Ma XJ,Guo CY,Wang MM,Kou N,Qu H,Mao HM,Shi DZ

更新日期：2016-04-01 00:00:00

abstract：:Esophageal cancer is one of the most common types of cancer in the world, and it demonstrates a distinct geographical distribution pattern in China. In the last decade, inducing apoptosis with traditional Chinese medicine (TCM) has become an active area in both fundamental and clinical research on cancer therapy. In t...

journal_title：Acta pharmacologica Sinica

authors： Zhang YS,Shen Q,Li J

更新日期：2016-03-01 00:00:00

abstract：AIM:Targeting the VEGF/VEGF receptor (VEGFR) pathway has proved to be an effective antiangiogenic approach for cancer treatment. Here, we identified 6-((2-((3-acetamidophenyl)amino)pyrimidin-4-yl)oxy)-N-phenyl-1-naphthamide (designated herein as DW10075) as a novel and highly selective inhibitor of VEGFRs. METHODS:In ...

journal_title：Acta pharmacologica Sinica

authors： Li MY,Lv YC,Tong LJ,Peng T,Qu R,Zhang T,Sun YM,Chen Y,Wei LX,Geng MY,Duan WH,Xie H,Ding J

更新日期：2016-03-01 00:00:00

abstract：AIM:To investigate the anti-neuroinflammatory activity of a novel synthetic compound, 7-methylchroman-2-carboxylic acid N-(2-trifluoromethyl) phenylamide (MCAP) against LPS-induced microglial activation in vitro. METHODS:Primary mouse microglia and BV2 microglia cells were exposed to LPS (50 or 100 ng/mL). The express...

journal_title：Acta pharmacologica Sinica

authors： Kim BW,More SV,Yun YS,Ko HM,Kwak JH,Lee H,Suk K,Kim IS,Choi DK

更新日期：2016-03-01 00:00:00

abstract：AIM:Diabetic nephropathy is one of the major complications of diabetes and the major cause of end-stage renal disease. In this study we investigated the insulin deficiency (ID) induced changes in renal mesangial cells (MCs) and in the kidney of STZ-induced diabetic rats. METHODS:Cultured rat renal MCs were incubated i...

journal_title：Acta pharmacologica Sinica

authors： Kong YL,Shen Y,Ni J,Shao DC,Miao NJ,Xu JL,Zhou L,Xue H,Zhang W,Wang XX,Lu LM

更新日期：2016-02-01 00:00:00

abstract：AIM:Recent evidence shows that cultured mycelium Cordyceps sinensis (CMCS) effectively protects against liver fibrosis in mice. Here, we investigated whether the anti-fibrotic action of CMCS was related to its regulation of the activity of hepatic natural killer (NK) cells in CCl4-treated mice. METHODS:C57BL/6 mice we...

journal_title：Acta pharmacologica Sinica

authors： Peng Y,Huang K,Shen L,Tao YY,Liu CH

更新日期：2016-02-01 00:00:00

abstract：AIM:KCNQ1 and KCNE1 form a complex in human ventricular cardiomyocytes, which are important in maintaining a normal heart rhythm. In the present study we investigated the effects of a homologous series of 1-alkanols on KCNQ1/KCNE1 channels expressed in Xenopus oocytes. METHODS:ECG recording was made in rats injected w...

journal_title：Acta pharmacologica Sinica

authors： Xie C,Liu HW,Pan N,Ding JP,Yao J

更新日期：2016-01-01 00:00:00

abstract：AIM:To investigate the mechanisms underlying the isomer-selective distribution of 3-n-butylphthalide (NBP) hydroxylated metabolites, 3-hydroxy-NBP (3-OH-NBP) and 10-hydroxy-NBP (10-OH-NBP), across the blood brain barrier (BBB). METHODS:After oral administration of NBP (20 mg/kg) to rats, the pharmacokinetics of two ma...

journal_title：Acta pharmacologica Sinica

authors： Diao XX,Zhong K,Li XL,Zhong DF,Chen XY

更新日期：2015-12-01 00:00:00

abstract：AIM:Apolipoprotein E (ApoE) plays an important role in the transport and metabolism of lipids. Recent studies show that bone mass is increased in young apoE(-/-) mice. In this study we investigated the bone phenotype and metabolism in aged apoE(-/-) mice. METHODS:Femurs and tibias were collected from 18- and 72-week-o...

journal_title：Acta pharmacologica Sinica

authors： Hong W,Xu XY,Qiu ZH,Gao JJ,Wei ZY,Zhen L,Zhang XL,Ye ZB

更新日期：2015-12-01 00:00:00

abstract：AIM:Radiation-induced brain injury (RIBI) is the most common and severe adverse effect induced by cranial radiation therapy (CRT). In the present study, we examined the effects of the traditional Chinese medicine Shenqi Fuzheng Injection (SFI) on RIBI in mice, and explored the underlying mechanisms. METHODS:C57BL/6J m...

journal_title：Acta pharmacologica Sinica

authors： Zhang J,Tong F,Cai Q,Chen LJ,Dong JH,Wu G,Dong XR

更新日期：2015-11-01 00:00:00

abstract：AIM:To investigate the effects of 3,4,4'-trihydroxy-trans-stilbene (3,4,4'-THS), an analogue of resveratrol, on human non-small-cell lung cancer (NSCLC) cells in vitro. METHODS:Cell viability of NSCLC A549 cells was determined by MTT assay. Cell apoptosis was evaluated using flow cytometry and TUNEL assay. Cell necros...

journal_title：Acta pharmacologica Sinica

authors： Zhang L,Dai F,Sheng PL,Chen ZQ,Xu QP,Guo YQ

更新日期：2015-10-01 00:00:00

abstract：:Alternative splicing is a key process of multi-exonic gene expression during pre-mRNA maturation. In this process, particular exons of a gene will be included within or excluded from the final matured mRNA, and the resulting transcripts generate diverse protein isoforms. Recent evidence demonstrates that approximately...

journal_title：Acta pharmacologica Sinica

authors： Le KQ,Prabhakar BS,Hong WJ,Li LC

更新日期：2015-10-01 00:00:00

abstract：:Angiogenesis, the formation of new blood vessels from the pre-existing vasculature is essential for embryonic development and tissue homeostasis. It also plays critical roles in diseases such as cancer and retinopathy. A delicate balance between pro- and anti-angiogenic factors ensures normal physiological homeostasis...

journal_title：Acta pharmacologica Sinica

authors： Rao N,Lee YF,Ge R

更新日期：2015-10-01 00:00:00

abstract：AIM:Cathepsin L is a lysosomal cysteine protease that plays important roles in cancer tumorigenesis, proliferation and chemotherapy resistance. The aim of this study was to determine how cathepsin L regulated the radiosensitivity of human glioma cells in vitro. METHODS:Human glioma U251 cells (harboring the mutant typ...

journal_title：Acta pharmacologica Sinica

authors： Zhang QQ,Wang WJ,Li J,Yang N,Chen G,Wang Z,Liang ZQ

更新日期：2015-09-01 00:00:00

abstract：AIM:Previous study has shown that endometrial cancers with LKB1 inactivation are highly responsive to mTOR inhibitors. In this study we examined the effect of LKB1 gene status on mTOR inhibitor responses in non-small cell lung cancer (NSCLC) cells. METHODS:Lung cancer cell lines Calu-1, H460, H1299, H1792, and A549 we...

journal_title：Acta pharmacologica Sinica

authors： Xiao P,Sun LL,Wang J,Han RL,Ma Q,Zhong DS

更新日期：2015-09-01 00:00:00

abstract：AIM:Omi is an ATP-independent serine protease that is necessary for neuronal function and survival. The aim of this study was to investigate the role of protease Omi in regulating differentiation of mouse neuroblastoma cells and to identify the substrate of Omi involved in this process. METHODS:Mouse neuroblastoma N2a...

journal_title：Acta pharmacologica Sinica

authors： Ma Q,Hu QS,Xu RJ,Zhen XC,Wang GH

更新日期：2015-08-01 00:00:00

abstract：AIM:Aquaporins (AQPs) are the water-channels that play important roles in brain water homeostasis and in cerebral edema induced by brain injury. In this study we investigated the relationship between AQPs and a neuroprotective agent curcumin that was effective in the treatment of brain edema in mice with intracerebral ...

journal_title：Acta pharmacologica Sinica

authors： Wang BF,Cui ZW,Zhong ZH,Sun YH,Sun QF,Yang GY,Bian LG

更新日期：2015-08-01 00:00:00

abstract：AIM:NLRP3 inflammasome plays an important role in renal injury and may be a therapeutic target in the treatment of patients with progressive chronic kidney disease. In this study we investigated whether angiotensin II (Ang II)-induced NLRP3 inflammasome activation was linked to endoplasmic reticulum stress (ERS) in hum...

journal_title：Acta pharmacologica Sinica

authors： Wang J,Wen Y,Lv LL,Liu H,Tang RN,Ma KL,Liu BC

更新日期：2015-07-01 00:00:00

abstract：AIM:Oral risedronate is effective in the treatment of postmenopausal osteoporosis when administered daily, weekly, or monthly. In this 1-year, randomized, double-blind, multicenter study we compared the weekly 35-mg and daily 5-mg risedronate dosing regimens in the treatment of Chinese postmenopausal women with osteopo...

journal_title：Acta pharmacologica Sinica

authors： Gu JM,Wang L,Lin H,Chen DC,Tang H,Jin XL,Xia WB,Hu YQ,Fu WZ,He JW,Zhang H,Wang C,Yue H,Hu WW,Liu YJ,Zhang ZL

更新日期：2015-07-01 00:00:00

abstract：:Single-target drugs have not achieved satisfactory therapeutic effects for complex diseases involving multiple factors. Instead, innovations in recent drug research and development have revealed the emergence of compound drugs, such as cocktail therapies and "polypills", as the frontier in new drug development. A trad...

journal_title：Acta pharmacologica Sinica

authors： Zhang JH,Zhu Y,Fan XH,Zhang BL

更新日期：2015-06-01 00:00:00

abstract：:Kushen (Radix Sophorae Flavescentis) has a long history of use for the treatment of tumors, inflammation and other diseases in traditional Chinese medicine. Compound Kushen Injection (CKI) is a mixture of natural compounds extracted from Kushen and Baituling (Rhizoma Smilacis Glabrae). The main principles of CKI are m...

journal_title：Acta pharmacologica Sinica

authors： Wang W,You RL,Qin WJ,Hai LN,Fang MJ,Huang GH,Kang RX,Li MH,Qiao YF,Li JW,Li AP

更新日期：2015-06-01 00:00:00

abstract：AIM:Seipin is a protein that resides in endoplasmic reticulum, and involved in both lipid metabolic disorders and motor neuropathy. The aim of this study was to investigate the effects of mutant seipin on autophagy system and the morphology of lipid droplets in vitro. METHODS:HEK-293, H1299 and MES23.5 cells were tran...

journal_title：Acta pharmacologica Sinica

authors： Fan HD,Chen SP,Sun YX,Xu SH,Wu LJ

更新日期：2015-04-01 00:00:00

abstract：AIM:Matrine is an alkaloid from Sophora alopecuroides L, which has shown a variety of pharmacological activities and potential therapeutic value in cardiovascular diseases. In this study we examined the protective effects of matrine against diabetic cardiomyopathy (DCM) in rats. METHODS:Male SD rats were injected with...

journal_title：Acta pharmacologica Sinica

authors： Liu ZW,Wang JK,Qiu C,Guan GC,Liu XH,Li SJ,Deng ZR

更新日期：2015-03-01 00:00:00

abstract：AIM:To study the effects of tanshinone IIA (TIIA) on lipopolysaccharide (LPS)-induced acute lung injury in mice and the underlying mechanisms. METHODS:Mice were injected with LPS (10 mg/kg, i.p.), then treated with TIIA (10 mg/kg, i.p.). Seven hours after LPS injection, the lungs were collected for histological study....

journal_title：Acta pharmacologica Sinica

authors： Xu M,Cao FL,Zhang YF,Shan L,Jiang XL,An XJ,Xu W,Liu XZ,Wang XY

更新日期：2015-02-01 00:00:00

abstract：:Estrogens are important endocrine hormones that control physiological functions in reproductive organs, and play a pivotal role in the generation and progression of breast cancer. Therapeutic drugs including anti-estrogen and aromatase inhibitors are used to treat patients with breast cancer. The estrogen receptors, E...

journal_title：Acta pharmacologica Sinica

authors： Ikeda K,Horie-Inoue K,Inoue S

更新日期：2015-01-01 00:00:00

abstract：:Retinoid X receptor-α (RXRα), a unique member of the nuclear receptor superfamily, represents an intriguing and unusual target for pharmacologic interventions and therapeutic applications in cancer, metabolic disorders and neurodegenerative diseases. Despite the fact that the RXR-based drug Targretin (bexarotene) is c...

journal_title：Acta pharmacologica Sinica

authors： Zhang XK,Su Y,Chen L,Chen F,Liu J,Zhou H

更新日期：2015-01-01 00:00:00

abstract：AIM:To investigate the antidepressant-like effects of a novel 5-HT3 receptor antagonist N-(benzo[d]thiazol-2-yl)-3-methoxyquinoxalin-2-carboxamide (6z) in acute and chronic murine models of depression. METHODS:5-HT3 receptor antagonism was examined in guinea pig ileum in vitro. A tail suspension test (TST) was used as...

journal_title：Acta pharmacologica Sinica

authors： Gupta D,Radhakrishnan M,Kurhe Y,Thangaraj D,Prabhakar V,Kanade P

更新日期：2014-12-01 00:00:00

abstract：AIM:Probucol, an anti-hyperlipidemic drug, has been reported to exert antitumor activities at various stages of tumor initiation, promotion and progression. In this study we examined whether the drug affected glioma cell growth in vitro and the underlying mechanisms. METHODS:Human glioma U87 and glioblastoma SF295 cel...

journal_title：Acta pharmacologica Sinica

authors： Jiang YS,Lei JA,Feng F,Liang QM,Wang FR

更新日期：2014-12-01 00:00:00

abstract：AIM:To discover novel ligands of estrogen receptor (ER) β using pharmacophore mapping and structure-based screening. METHODS:A computer-aided strategy combining pharmacophore mapping and structure-based screening was used to screen the Maybridge and Enamine databases. Yeast two-hybrid (Y2H) assay was used to detect th...

journal_title：Acta pharmacologica Sinica

authors： Chen L,Wu D,Bian HP,Kuang GL,Jiang J,Li WH,Liu GX,Zou SE,Huang J,Tang Y

更新日期：2014-10-01 00:00:00