Author Correction: AZD9291 inactivates the PRC2 complex to mediate tumor growth inhibition.
Abstract An amendment to this paper has been published and can be accessed via a link at the top of the paper. PMID: 32060412 [PubMed - as supplied by publisher] (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - February 14, 2020 Category: Drugs & Pharmacology Authors: Zhang KL, Shen QQ, Fang YF, Sun YM, Ding J, Chen Y Tags: Acta Pharmacol Sin Source Type: research

Author Correction: AZD9291 inactivates the PRC2 complex to mediate tumor growth inhibition
Acta Pharmacologica Sinica, Published online: 14 February 2020; doi:10.1038/s41401-019-0344-3Author Correction: AZD9291 inactivates the PRC2 complex to mediate tumor growth inhibition (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - February 14, 2020 Category: Drugs & Pharmacology Authors: Kai-li Zhang Qian-qian Shen Yan-feng Fang Yi-ming Sun Jian Ding Yi Chen Source Type: research

A comparative pharmacogenomic analysis of three classic TCM prescriptions for coronary heart disease based on molecular network modeling.
Abstract Traditional Chinese medicine (TCM) has evolved over several thousands of years, which has been shown to be efficacious in the treatment of ischemic heart disease. Three classical TCM prescriptions, namely Xuefu Zhuyu Decoction, Zhishi Xiebai Guizhi Decoction, and Gualou Xiebai Banxia Decoction, have been extensively used in the treatment of coronary heart disease (CHD). Based on molecular network modeling, we performed a comparative pharmacogenomic analysis to systematically determine the drug-targeting spectrum of the three prescriptions at molecular level. Wide-area target molecules of CHD were covered,...
Source: Acta Pharmacologica Sinica - February 12, 2020 Category: Drugs & Pharmacology Authors: Zhang YY, Zhao ZD, Kong PY, Gao L, Yu YN, Liu J, Wang PQ, Li B, Zhang XX, Yang LQ, Wang Z Tags: Acta Pharmacol Sin Source Type: research

A comparative pharmacogenomic analysis of three classic TCM prescriptions for coronary heart disease based on molecular network modeling
Acta Pharmacologica Sinica, Published online: 12 February 2020; doi:10.1038/s41401-019-0352-3A comparative pharmacogenomic analysis of three classic TCM prescriptions for coronary heart disease based on molecular network modeling (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - February 12, 2020 Category: Drugs & Pharmacology Authors: Ying-ying Zhang Zi-de Zhao Peng-yun Kong Lin Gao Ya-nan Yu Jun Liu Peng-qian Wang Bing Li Xiao-xu Zhang Li-qiang Yang Zhong Wang Source Type: research

A novel derivative of valepotriate inhibits the PI3K/AKT pathway and causes Noxa-dependent apoptosis in human pancreatic cancer cells.
In this study, we performed a structure-based similarity search and found 16 hit compounds. Among the 16 hits, (1S,6S,7R)-6-(acetyloxy)-1-[(3-methylbutanoyl)oxy]-4a,5,6,7a-tetrahydro-1H-spiro[cyclopenta[c]pyran-7,2'-oxiran]-4-ylmethyl 3-methylbutanoate (denoted as Amcp) exhibited superior anticancer activity against human pancreatic cancer BxPC-3 and SW1990 cells. The anti-proliferation activity of Amcp was validated in human pancreatic cancer BxPC-3 and SW1990 cells in vitro. Amcp more effectively induced apoptosis in BxPC-3 and SW1990 cells than gemcitabine. At a concentration of 15 μM, Amcp significantly suppr...
Source: Acta Pharmacologica Sinica - February 11, 2020 Category: Drugs & Pharmacology Authors: Yan YY, Shi KY, Teng F, Chen J, Che JX, Dong XW, Lin NM, Zhang B Tags: Acta Pharmacol Sin Source Type: research

Identification of nagilactone E as a protein synthesis inhibitor with anticancer activity.
In conclusion, NLE is a protein synthesis inhibitor with anticancer activity. PMID: 32047261 [PubMed - as supplied by publisher] (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - February 11, 2020 Category: Drugs & Pharmacology Authors: Zhang LL, Guo J, Jiang XM, Chen XP, Wang YT, Li A, Lin LG, Li H, Lu JJ Tags: Acta Pharmacol Sin Source Type: research

Ganoderic acid A protects neural cells against NO stress injury in vitro via stimulating β adrenergic receptors.
In this study, we investigated the effect of ganoderic acid A (GA A) against SNP injury in neural cells and the role of adrenergic receptors in GA A neuroprotection. We found that SNP (0.125-2 mM) dose-dependently decreased the viability of both SH-SY5Y and PC12 cells and markedly increased NO contents. Pretreatment with GA A (10 μM) significantly attenuated SNP-induced cytotoxicity and NO increase in SH-SY5Y cells, but not in PC12 cells. Furthermore, pretreatment with GA A caused significantly higher adrenaline content in SH-SY5Y cells than in PC12 cells. In order to elucidate the mechanism of GA A-protec...
Source: Acta Pharmacologica Sinica - February 11, 2020 Category: Drugs & Pharmacology Authors: Yu ZR, Jia WH, Liu C, Wang HQ, Yang HG, He GR, Chen RY, Du GH Tags: Acta Pharmacol Sin Source Type: research

A novel derivative of valepotriate inhibits the PI3K/AKT pathway and causes Noxa-dependent apoptosis in human pancreatic cancer cells
Acta Pharmacologica Sinica, Published online: 11 February 2020; doi:10.1038/s41401-019-0354-1A novel derivative of valepotriate inhibits the PI3K/AKT pathway and causes Noxa-dependent apoptosis in human pancreatic cancer cells (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - February 11, 2020 Category: Drugs & Pharmacology Authors: You-you Yan Ke-yu Shi Fei Teng Jing Chen Jin-xin Che Xiao-wu Dong Neng-ming Lin Bo Zhang Source Type: research

Identification of nagilactone E as a protein synthesis inhibitor with anticancer activity
Acta Pharmacologica Sinica, Published online: 11 February 2020; doi:10.1038/s41401-019-0332-7Identification of nagilactone E as a protein synthesis inhibitor with anticancer activity (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - February 11, 2020 Category: Drugs & Pharmacology Authors: Le-le Zhang Jing Guo Xiao-ming Jiang Xiu-ping Chen Yi-tao Wang Ao Li Li-gen Lin Hua Li Jin-jian Lu Source Type: research

Ganoderic acid A protects neural cells against NO stress injury in vitro via stimulating β adrenergic receptors
Acta Pharmacologica Sinica, Published online: 11 February 2020; doi:10.1038/s41401-020-0356-zGanoderic acid A protects neural cells against NO stress injury in vitro via stimulating β adrenergic receptors (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - February 11, 2020 Category: Drugs & Pharmacology Authors: Zi-ru Yu Wei-hua Jia Chao Liu Hong-qing Wang Hai-guang Yang Guo-rong He Ruo-yun Chen Guan-hua Du Source Type: research

Tissue-specific relaxin-2 is differentially associated with the presence/size of an arterial aneurysm and the severity of atherosclerotic disease in humans.
Abstract Circulating or tissue-related biomarkers are of clinical value for risk stratification in patients with abdominal aortic aneurysms. Relaxin-2 (RL2) has been linked to the presence and size of arterial aneurysms, and to the extent of atherosclerosis in human subjects. Here, we assessed the expression levels of RL2 in aneurysmal (AA, n = 16) and atherosclerotic (ATH, n = 22) arteries, and established the correlation between RL2 levels and the presence/size of AA and the clinical severity of atherosclerosis. The expression levels of metalloproteinases (MMPs) and endothelial nitric...
Source: Acta Pharmacologica Sinica - February 5, 2020 Category: Drugs & Pharmacology Authors: Papoutsis K, Kapelouzou A, Georgiopoulos G, Kontogiannis C, Kourek C, Mylonas KS, Patelis N, Cokkinos DV, Karavokyros I, Georgopoulos S Tags: Acta Pharmacol Sin Source Type: research

Tissue-specific relaxin-2 is differentially associated with the presence/size of an arterial aneurysm and the severity of atherosclerotic disease in humans
Acta Pharmacologica Sinica, Published online: 05 February 2020; doi:10.1038/s41401-019-0350-5Tissue-specific relaxin-2 is differentially associated with the presence/size of an arterial aneurysm and the severity of atherosclerotic disease in humans (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - February 5, 2020 Category: Drugs & Pharmacology Authors: Konstantinos Papoutsis Alkistis Kapelouzou Georgios Georgiopoulos Christos Kontogiannis Christos Kourek Konstantinos S Mylonas Nikolaos Patelis Dennis V Cokkinos Ioannis Karavokyros Sotirios Georgopoulos Source Type: research

Physiologically based pharmacokinetic-pharmacodynamic modeling for prediction of vonoprazan pharmacokinetics and its inhibition on gastric acid secretion following intravenous/oral administration to rats, dogs and humans.
In this study we developed a physiologically based pharmacokinetic (PBPK)-pharmacodynamic (PD) model linking to stomach to simultaneously predict vonoprazan pharmacokinetics and its antisecretory effects following administration to rats, dogs, and humans based on in vitro parameters. The vonoprazan disposition in the stomach was illustrated using a limited-membrane model. In vitro metabolic and transport parameters were derived from hepatic microsomes and Caco-2 cells, respectively. We found the most predicted plasma concentrations and pharmacokinetic parameters of vonoprazan in rats, dogs and humans were within twofold er...
Source: Acta Pharmacologica Sinica - January 22, 2020 Category: Drugs & Pharmacology Authors: Kong WM, Sun BB, Wang ZJ, Zheng XK, Zhao KJ, Chen Y, Zhang JX, Liu PH, Zhu L, Xu RJ, Li P, Liu L, Liu XD Tags: Acta Pharmacol Sin Source Type: research

Physiologically based pharmacokinetic–pharmacodynamic modeling for prediction of vonoprazan pharmacokinetics and its inhibition on gastric acid secretion following intravenous/oral administration to rats, dogs and humans
Acta Pharmacologica Sinica, Published online: 22 January 2020; doi:10.1038/s41401-019-0353-2Physiologically based pharmacokinetic–pharmacodynamic modeling for prediction of vonoprazan pharmacokinetics and its inhibition on gastric acid secretion following intravenous/oral administration to rats, dogs and humans (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - January 22, 2020 Category: Drugs & Pharmacology Authors: Wei-min Kong Bin-bin Sun Zhong-jian Wang Xiao-ke Zheng Kai-jing Zhao Yang Chen Jia-xin Zhang Pei-hua Liu Liang Zhu Ru-jun Xu Ping Li Li Liu Xiao-dong Liu Source Type: research

Retraction Note: Resveratrol rescues hyperglycemia-induced endothelial dysfunction via activation of Akt.
Abstract An amendment to this paper has been published and can be accessed via a link at the top of the paper. PMID: 31953509 [PubMed - as supplied by publisher] (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - January 17, 2020 Category: Drugs & Pharmacology Authors: Li JY, Huang WQ, Tu RH, Zhong GQ, Luo BB, He Y Tags: Acta Pharmacol Sin Source Type: research

Retraction Note: Resveratrol rescues hyperglycemia-induced endothelial dysfunction via activation of Akt
Acta Pharmacologica Sinica, Published online: 17 January 2020; doi:10.1038/s41401-020-0363-0Retraction Note: Resveratrol rescues hyperglycemia-induced endothelial dysfunction via activation of Akt (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - January 17, 2020 Category: Drugs & Pharmacology Authors: Jin-yi Li Wei-qiang Huang Rong-hui Tu Guo-qiang Zhong Bei-bei Luo Yan He Source Type: research

Aggravated ulcerative colitis caused by intestinal Metrnl deficiency is associated with reduced autophagy in epithelial cells.
This study aimed to explore the role and mechanism of intestinal epithelial Metrnl in ulcerative colitis. Metrnl-/- (intestinal epithelial cell-specific Metrnl knockout) mice did not display any phenotypes of colitis under basal conditions. However, under administration of 3% dextran sodium sulfate (DSS) drinking water, colitis was more severe in Metrnl-/- mice than in WT mice, as indicated by comparisons of body weight loss, the presence of occult or gross blood per rectum, stool consistency, shrinkage in the colon, intestinal damage, and serum levels of inflammatory factors. DSS-induced colitis activated autophagy in the...
Source: Acta Pharmacologica Sinica - January 16, 2020 Category: Drugs & Pharmacology Authors: Zhang SL, Li ZY, Wang DS, Xu TY, Fan MB, Cheng MH, Miao CY Tags: Acta Pharmacol Sin Source Type: research

RGD-hirudin-based low molecular weight peptide prevents blood coagulation via subcutaneous injection.
Abstract Thromboembolic disease is a common cardio-cerebral vascular disease that threatens human life and health. Thrombin not only affects the exogenous coagulation pathway, but also the endogenous pathway. Thus, it becomes one of the most important targets of anticoagulant drugs. RGD-hirudin is an anticoagulant drug targeting thrombin, but it can only be administered intravenously. We designed a low molecular weight peptide based on RGD-hirudin that could prevent blood clots. We first used NMR to identify the key amino acid residues of RGD-hirudin that interacted with thrombin. Then, we designed a novel direct ...
Source: Acta Pharmacologica Sinica - January 16, 2020 Category: Drugs & Pharmacology Authors: Li YR, Huang YN, Zhao B, Wu MF, Li TY, Zhang YL, Chen D, Yu M, Mo W Tags: Acta Pharmacol Sin Source Type: research

Berberine derivatives with a long alkyl chain branched by hydroxyl group and methoxycarbonyl group at 9-position show improved anti-proliferation activity and membrane permeability in A549 cells.
In this study, we designed and synthesized a series of 9-O position modified BBR derivatives aiming to improve its cell permeability and anticancer activity, utilizing a long alkyl chain branched by hydroxyl group and methoxycarbonyl group. Among these compounds, B10 showed 3.6-fold higher intracellular concentration than BBR, as well as 60-fold increased anti-proliferation activity against human lung cancer A549 cells compared with BBR. Treatment with B10 (1, 2 μM) induced apoptosis of A549 cells. Further investigations showed that B10 treatment dose-dependently affected mitochondrial functions, including oxygen...
Source: Acta Pharmacologica Sinica - January 16, 2020 Category: Drugs & Pharmacology Authors: Liu Y, Zhu KX, Cao L, Xie ZF, Gu M, Lü W, Li JY, Nan FJ Tags: Acta Pharmacol Sin Source Type: research

RGD-hirudin-based low molecular weight peptide prevents blood coagulation via subcutaneous injection
Acta Pharmacologica Sinica, Published online: 16 January 2020; doi:10.1038/s41401-019-0347-0RGD-hirudin-based low molecular weight peptide prevents blood coagulation via subcutaneous injection (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - January 16, 2020 Category: Drugs & Pharmacology Authors: Ya-ran Li Yi-nong Huang Bing Zhao Meng-fang Wu Tian-yu Li Yan-ling Zhang Di Chen Min Yu Wei Mo Source Type: research

Berberine derivatives with a long alkyl chain branched by hydroxyl group and methoxycarbonyl group at 9-position show improved anti-proliferation activity and membrane permeability in A549 cells
Acta Pharmacologica Sinica, Published online: 16 January 2020; doi:10.1038/s41401-019-0346-1 (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - January 16, 2020 Category: Drugs & Pharmacology Authors: Yi Liu Ke-xin Zhu Lei Cao Zhi-fu Xie Min Gu Wei L ü Jing-ya Li Fa-jun Nan Source Type: research

Aggravated ulcerative colitis caused by intestinal Metrnl deficiency is associated with reduced autophagy in epithelial cells
Acta Pharmacologica Sinica, Published online: 16 January 2020; doi:10.1038/s41401-019-0343-4Aggravated ulcerative colitis caused by intestinal Metrnl deficiency is associated with reduced autophagy in epithelial cells (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - January 16, 2020 Category: Drugs & Pharmacology Authors: Sai-long Zhang Zhi-yong Li Dong-sheng Wang Tian-ying Xu Mao-bing Fan Ming-he Cheng Chao-yu Miao Source Type: research

Oroxindin inhibits macrophage NLRP3 inflammasome activation in DSS-induced ulcerative colitis in mice via suppressing TXNIP-dependent NF- κB pathway.
In conclusion, these results demonstrate that oroxindin could be absorbed by the colon and attenuate inflammatory responses via inhibiting NLRP3 inflammasome formation and activation, which is related to the inhibitory effect on TXNIP-dependent NF-κB-signaling pathway. Hence, oroxindin has the potential of becoming an effective drug for treating UC. PMID: 31937929 [PubMed - as supplied by publisher] (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - January 14, 2020 Category: Drugs & Pharmacology Authors: Liu Q, Zuo R, Wang K, Nong FF, Fu YJ, Huang SW, Pan ZF, Zhang Y, Luo X, Deng XL, Zhang XX, Zhou L, Chen Y Tags: Acta Pharmacol Sin Source Type: research

Mechanisms and pharmacokinetic/pharmacodynamic profiles underlying the low nephrotoxicity and ototoxicity of etimicin.
Abstract Etimicin (ETM), a fourth-generation aminoglycosides (AGs), is now widely clinically used in China due to its high efficacy and low toxicity. However, the mechanisms underlying its low nephrotoxicity and ototoxicity remain unclear. In the present study we compared the antibacterial and toxicity profiles of etimicin, gentamicin (GM, a second-generation AG), and amikacin (AMK, a third-generation AG), and investigated their pharmacokinetic properties in the toxicity target organs (kidney and inner ear) and subcellular compartments. We first demonstrated that ETM exhibited superior antibacterial activities aga...
Source: Acta Pharmacologica Sinica - January 14, 2020 Category: Drugs & Pharmacology Authors: Yao L, Zhang JW, Chen B, Cai MM, Feng D, Wang QZ, Wang XY, Sun JG, Zheng YW, Wang GJ, Zhou F Tags: Acta Pharmacol Sin Source Type: research

The hypoglycemic mechanism of catalpol involves increased AMPK-mediated mitochondrial biogenesis.
Abstract Mitochondria serve as sensors of energy regulation and glucose levels, which are impaired by diabetes progression. Catalpol is an iridoid glycoside that exerts a hypoglycemic effect by improving mitochondrial function, but the underlying mechanism has not been fully elucidated. In the current study we explored the effects of catalpol on mitochondrial function in db/db mice and C2C12 myotubes in vitro. After oral administration of catalpol (200 mg·kg-1·d-1) for 8 weeks, db/db mice exhibited a decreased fasting blood glucose level and restored mitochondrial function in skeletal muscle. ...
Source: Acta Pharmacologica Sinica - January 14, 2020 Category: Drugs & Pharmacology Authors: Xu DQ, Li CJ, Jiang ZZ, Wang L, Huang HF, Li ZJ, Sun LX, Fan SS, Zhang LY, Wang T Tags: Acta Pharmacol Sin Source Type: research

IgD-Fc-Ig fusion protein, a new biological agent, inhibits T cell function in CIA rats by inhibiting IgD-IgDR-Lck-NF- κB signaling pathways.
In this study we investigated whether IgD-Fc-Ig exerted therapeutic effects in collagen-induced arthritis (CIA) rats. CIA rats were treated with IgD-Fc-Ig (1, 3, and 9 mg/kg) or injected with biological agents etanercept (3 mg/kg) once every 3 days for 40 days. In the PBMCs and spleen lymphocytes of CIA rats, both T and B cells exhibited abnormal proliferation; the percentages of CD3+ total T cells, CD3+CD4+ Th cells, CD3+CD4+CD25+-activated Th cells, Th1(CD4+IFN-γ+), and Th17(CD4+IL-17+) were significantly increased, whereas the Treg (CD4+CD25+Foxp3+) cell percentage was decreased. IgD-Fc-Ig administra...
Source: Acta Pharmacologica Sinica - January 14, 2020 Category: Drugs & Pharmacology Authors: Han L, Zhang XZ, Wang C, Tang XY, Zhu Y, Cai XY, Wu YJ, Shu JL, Wang QT, Chen JY, Chang Y, Wu HX, Zhang LL, Wei W Tags: Acta Pharmacol Sin Source Type: research

Fecal microbiota transplantation improves metabolism and gut microbiome composition in db/db mice.
In this study, we investigated the effects of transplanted fecal bacteria from Kazaks with normal glucose tolerance (KNGT) in db/db mice. The mice were treated with 0.2 mL of fecal bacteria solution from KNGT daily for 10 weeks. We showed that the fecal bacteria from KNGT successfully colonized in the intestinal tract of db/db mice detected on day 14. In the FMT-treated db/db mice, the levels of fasting blood glucose, postprandial glucose, total cholesterol, triglyceride, and low-density lipoprotein-cholesterol were significantly downregulated, whereas high-density lipoprotein-cholesterol levels were upregulated. In...
Source: Acta Pharmacologica Sinica - January 14, 2020 Category: Drugs & Pharmacology Authors: Zhang PP, Li LL, Han X, Li QW, Zhang XH, Liu JJ, Wang Y Tags: Acta Pharmacol Sin Source Type: research

Fecal microbiota transplantation improves metabolism and gut microbiome composition in db/db mice
Acta Pharmacologica Sinica, Published online: 14 January 2020; doi:10.1038/s41401-019-0330-9Fecal microbiota transplantation improves metabolism and gut microbiome composition in db/db mice (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - January 14, 2020 Category: Drugs & Pharmacology Authors: Pei-pei Zhang Lin-lin Li Xue Han Qin-wei Li Xu-hua Zhang Johnson J. Liu Ye Wang Source Type: research

The hypoglycemic mechanism of catalpol involves increased AMPK-mediated mitochondrial biogenesis
Acta Pharmacologica Sinica, Published online: 14 January 2020; doi:10.1038/s41401-019-0345-2The hypoglycemic mechanism of catalpol involves increased AMPK-mediated mitochondrial biogenesis (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - January 14, 2020 Category: Drugs & Pharmacology Authors: Deng-qiu Xu Chun-jie Li Zhen-zhou Jiang Lu Wang Hong-fei Huang Zhi-jian Li Li-xin Sun Si-si Fan Lu-yong Zhang Tao Wang Source Type: research

Mechanisms and pharmacokinetic/pharmacodynamic profiles underlying the low nephrotoxicity and ototoxicity of etimicin
Acta Pharmacologica Sinica, Published online: 14 January 2020; doi:10.1038/s41401-019-0342-5Mechanisms and pharmacokinetic/pharmacodynamic profiles underlying the low nephrotoxicity and ototoxicity of etimicin (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - January 14, 2020 Category: Drugs & Pharmacology Authors: Lan Yao Jing-wei Zhang Bin Chen Ming-min Cai Dong Feng Qi-zhi Wang Xin-yu Wang Jian-guo Sun Yi-wen Zheng Guang-ji Wang Fang Zhou Source Type: research

Oroxindin inhibits macrophage NLRP3 inflammasome activation in DSS-induced ulcerative colitis in mice via suppressing TXNIP-dependent NF-κB pathway
Acta Pharmacologica Sinica, Published online: 14 January 2020; doi:10.1038/s41401-019-0335-4Oroxindin inhibits macrophage NLRP3 inflammasome activation in DSS-induced ulcerative colitis in mice via suppressing TXNIP-dependent NF-κB pathway (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - January 14, 2020 Category: Drugs & Pharmacology Authors: Qi Liu Rui Zuo Kai Wang Fei-fei Nong Ya-jun Fu Shao-wei Huang Zeng-feng Pan Yi Zhang Xia Luo Xiang-liang Deng Xiao-xue Zhang Lian Zhou Yang Chen Source Type: research

IgD-Fc-Ig fusion protein, a new biological agent, inhibits T cell function in CIA rats by inhibiting IgD-IgDR-Lck-NF-κB signaling pathways
Acta Pharmacologica Sinica, Published online: 14 January 2020; doi:10.1038/s41401-019-0337-2IgD-Fc-Ig fusion protein, a new biological agent, inhibits T cell function in CIA rats by inhibiting IgD-IgDR-Lck-NF-κB signaling pathways (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - January 14, 2020 Category: Drugs & Pharmacology Authors: Le Han Xian-zheng Zhang Chen Wang Xiao-yu Tang Yue Zhu Xiao-yu Cai Yu-jing Wu Jin-ling Shu Qing-tong Wang Jing-yu Chen Yan Chang Hua-xun Wu Ling-ling Zhang Wei Wei Source Type: research

A novel biphenyl compound IMB-S7 ameliorates hepatic fibrosis in BDL rats by suppressing Sp1-mediated integrin αv expression.
A novel biphenyl compound IMB-S7 ameliorates hepatic fibrosis in BDL rats by suppressing Sp1-mediated integrin αv expression. Acta Pharmacol Sin. 2020 Jan 13;: Authors: Zhang N, Zhao SS, Zhang YX, Wang YC, Shao RG, Wang JX, He HW Abstract Chronic tissue injury with fibrosis results in the disruption of tissue architecture, organ dysfunction, and eventual organ failure. Therefore, the development of effective antifibrotic drugs is urgently required. IMB-S7 is novel biphenyl compound derived from bifendate (biphenyldicarboxylate) that is used for the treatment of chronic hepatitis in China. In the...
Source: Acta Pharmacologica Sinica - January 13, 2020 Category: Drugs & Pharmacology Authors: Zhang N, Zhao SS, Zhang YX, Wang YC, Shao RG, Wang JX, He HW Tags: Acta Pharmacol Sin Source Type: research

The novel sophoridine derivate IMB-HDC induced lessened phosphorylation of STAT5a at 694 and 780 and promoted DNA breakage and cell apoptosis via blocking STAT5a nuclear translocation.
Abstract Sophoridine is a quinolizidine natural product and the exploration of its derivatives has been carried out, and the potent anticancer compound IMB-HDC was acquired. Although previous studies have revealed that some sophoridine derivatives could induce DNA breakage, the underlying mechanisms of inhibition of DNA damage repair (ATR inactivation) and the apoptosis independent of p53, have not been elucidated. Our research reveals a novel DNA response mechanism different from general DNA-damaging agents, and that sophoridine derivate inhibits the phosphorylation of Tyr694 and Ser780 of STAT5a to induce the le...
Source: Acta Pharmacologica Sinica - January 13, 2020 Category: Drugs & Pharmacology Authors: Zhao WL, Xing Y, Ye C, Qiu YH, Li Y, Liu XJ, Wang MY, Bi CW, Song DQ, Shao RG Tags: Acta Pharmacol Sin Source Type: research

PK/PD modeling based on NO-ET homeostasis for improving management of sunitinib-induced hypertension in rats.
Abstract Sunitinib is an oral small molecule multitargeted tyrosine kinase inhibitor, which is currently used to treat severe cancers. Clinical research has shown that patients treated with sunitinib develop hypertension. As soon as sunitinib-induced hypertension appears, it is usual to administer anti-hypertension agent. But this treatment may cause acute blood pressure fluctuation which may lead to additional cardiovascular risk. The aim of this study is to establish a mathematical model for managing sunitinib-induced hypertension and blood pressure fluctuation. A mechanism-based PK/PD model was developed based ...
Source: Acta Pharmacologica Sinica - January 13, 2020 Category: Drugs & Pharmacology Authors: Liu HC, Zhou XT, Zheng YS, He H, Liu XQ Tags: Acta Pharmacol Sin Source Type: research

The novel sophoridine derivate IMB-HDC induced lessened phosphorylation of STAT5a at 694 and 780 and promoted DNA breakage and cell apoptosis via blocking STAT5a nuclear translocation
Acta Pharmacologica Sinica, Published online: 13 January 2020; doi:10.1038/s41401-019-0333-6The novel sophoridine derivate IMB-HDC induced lessened phosphorylation of STAT5a at 694 and 780 and promoted DNA breakage and cell apoptosis via blocking STAT5a nuclear translocation (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - January 13, 2020 Category: Drugs & Pharmacology Authors: Wu-li Zhao Yan Xing Cheng Ye Yu-han Qiu Yi Li Xiu-jun Liu Meng-yan Wang Chong-wen Bi Dan-qing Song Rong-guang Shao Source Type: research

A novel biphenyl compound IMB-S7 ameliorates hepatic fibrosis in BDL rats by suppressing Sp1-mediated integrin αv expression
Acta Pharmacologica Sinica, Published online: 13 January 2020; doi:10.1038/s41401-019-0325-6A novel biphenyl compound IMB-S7 ameliorates hepatic fibrosis in BDL rats by suppressing Sp1-mediated integrin αv expression (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - January 13, 2020 Category: Drugs & Pharmacology Authors: Na Zhang Shuang-shuang Zhao Yi-xuan Zhang Yu-cheng Wang Rong-guang Shao Ju-xian Wang Hong-wei He Source Type: research

PK/PD modeling based on NO-ET homeostasis for improving management of sunitinib-induced hypertension in rats
Acta Pharmacologica Sinica, Published online: 13 January 2020; doi:10.1038/s41401-019-0331-8PK/PD modeling based on NO-ET homeostasis for improving management of sunitinib-induced hypertension in rats (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - January 13, 2020 Category: Drugs & Pharmacology Authors: Hao-chen Liu Xiao-ting Zhou Yun-si Zheng Hua He Xiao-quan Liu Source Type: research

Nimesulide increases the aldehyde oxidase activity of humans and rats.
In this study, we investigated the potential induction of AOX activity by NIM using methotrexate as the probe substrate. Treatment of primary human and rat hepatocytes with NIM (20 μM) for 24 h caused a 2.0- and 3.1-fold, respectively, increase in 7-OH MTX formation. Oral administration of NIM (100 mg·kg-1·d-1, for 5 days) to rats significantly increased the systematic exposure (6.5-fold), liver distribution (2.5-fold), and excretion (5.2-fold for urinary excretion and 2.1-fold for fecal excretion) of 7-OH MTX. The 7-OH MTX formation in liver cytosol from rats pretreated with 20, 50, a...
Source: Acta Pharmacologica Sinica - January 8, 2020 Category: Drugs & Pharmacology Authors: Zhou L, Pang XY, Hou XY, Liu L, Guo ZT, Chen XY Tags: Acta Pharmacol Sin Source Type: research

Donepezil attenuates vascular dementia in rats through increasing BDNF induced by reducing HDAC6 nuclear translocation.
In conclusion, our results demonstrate that donepezil attenuates neurodegeneration in cortex and hippocampus via increasing BDNF expression; the regulation of donepezil on HDAC6 occurred in cortex, but not in the hippocampus. This study further clarifies the pharmacological mechanism of donepezil, while also emphasizes the promising epigenetic regulation of HDAC6. PMID: 31913348 [PubMed - as supplied by publisher] (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - January 8, 2020 Category: Drugs & Pharmacology Authors: Jian WX, Zhang Z, Zhan JH, Chu SF, Peng Y, Zhao M, Wang Q, Chen NH Tags: Acta Pharmacol Sin Source Type: research

Donepezil attenuates vascular dementia in rats through increasing BDNF induced by reducing HDAC6 nuclear translocation
Acta Pharmacologica Sinica, Published online: 08 January 2020; doi:10.1038/s41401-019-0334-5Donepezil attenuates vascular dementia in rats through increasing BDNF induced by reducing HDAC6 nuclear translocation (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - January 8, 2020 Category: Drugs & Pharmacology Authors: Wen-xuan Jian Zhao Zhang Jia-hong Zhan Shi-feng Chu Ye Peng Ming Zhao Qi Wang Nai-hong Chen Source Type: research

Nimesulide increases the aldehyde oxidase activity of humans and rats
Acta Pharmacologica Sinica, Published online: 08 January 2020; doi:10.1038/s41401-019-0336-3Nimesulide increases the aldehyde oxidase activity of humans and rats (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - January 8, 2020 Category: Drugs & Pharmacology Authors: Lei Zhou Xiao-yan Pang Xiang-yu Hou Lu Liu Zi-tao Guo Xiao-yan Chen Source Type: research

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Acta Pharmacologica Sinica, Published online: 08 January 2020; doi:10.1038/s41401-019-0334-5 (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - January 8, 2020 Category: Drugs & Pharmacology Authors: Wen-xuan Jian Zhao Zhang Jia-hong Zhan Shi-feng Chu Ye Peng Ming Zhao Qi Wang Nai-hong Chen Source Type: research

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Acta Pharmacologica Sinica, Published online: 08 January 2020; doi:10.1038/s41401-019-0336-3 (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - January 8, 2020 Category: Drugs & Pharmacology Authors: Lei Zhou Xiao-yan Pang Xiang-yu Hou Lu Liu Zi-tao Guo Xiao-yan Chen Source Type: research

Ganoderic acid A is the effective ingredient of Ganoderma triterpenes in retarding renal cyst development in polycystic kidney disease.
Abstract Autosomal dominant polycystic kidney disease (ADPKD) is one of the most common life-threatening monogenetic diseases characterized by progressive enlargement of fluid-filled renal cysts. Our previous study has shown that Ganoderma triterpenes (GT) retards PKD renal cyst development. In the present study we identified the effective ingredient of GT in suppression of kidney cyst development. Using an in vitro MDCK cystogenesis model, we identified ganoderic acid A (GA-A) as the most promising candidate among the 12 ganoderic acid (GA) monomers. We further showed that GA-A (6.25-100 μM) significant...
Source: Acta Pharmacologica Sinica - January 7, 2020 Category: Drugs & Pharmacology Authors: Meng J, Sai-Zhen Wang, He JZ, Zhu S, Huang BY, Wang SY, Li M, Zhou H, Lin SQ, Yang BX Tags: Acta Pharmacol Sin Source Type: research

Antiepileptic geissoschizine methyl ether is an inhibitor of multiple neuronal channels.
In this study, electrophysiological technique was used to explore the mechanism underlying the antiepileptic activity of GM. We first showed that GM (1-30 μmol/L) dose-dependently suppressed the spontaneous firing and prolonged the action potential duration in cultured mouse and rat hippocampal neurons. Given the pivotal roles of ion channels in regulating neuronal excitability, we then examined the effects of GM on both voltage-gated and ligand-gated channels in rat hippocampal neurons. We found that GM is an inhibitor of multiple neuronal channels: GM potently inhibited the voltage-gated sodium (NaV), calcium (...
Source: Acta Pharmacologica Sinica - January 7, 2020 Category: Drugs & Pharmacology Authors: Xie ZQ, Tian XT, Zheng YM, Zhan L, Chen XQ, Xin XM, Huang CG, Gao ZB Tags: Acta Pharmacol Sin Source Type: research

Antiepileptic geissoschizine methyl ether is an inhibitor of multiple neuronal channels
Acta Pharmacologica Sinica, Published online: 07 January 2020; doi:10.1038/s41401-019-0327-4Antiepileptic geissoschizine methyl ether is an inhibitor of multiple neuronal channels (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - January 7, 2020 Category: Drugs & Pharmacology Authors: Zhu-qing Xie Xiao-ting Tian Yue-ming Zheng Li Zhan Xue-qin Chen Xiao-ming Xin Cheng-gang Huang Zhao-bing Gao Source Type: research

Ganoderic acid A is the effective ingredient of Ganoderma triterpenes in retarding renal cyst development in polycystic kidney disease
Acta Pharmacologica Sinica, Published online: 07 January 2020; doi:10.1038/s41401-019-0329-2Ganoderic acid A is the effective ingredient of Ganoderma triterpenes in retarding renal cyst development in polycystic kidney disease (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - January 7, 2020 Category: Drugs & Pharmacology Authors: Jia Meng Sai-zhen Wang Jin-zhao He Shuai Zhu Bo-yue Huang Shu-yuan Wang Min Li Hong Zhou Shu-qian Lin Bao-xue Yang Source Type: research

Metoprolol prevents neuronal dendrite remodeling in a canine model of chronic obstructive sleep apnea.
In conclusion, metoprolol protects against neuronal dendritic remodeling in hippocampi and prefrontal cortices induced by chronic OSA in canine. PMID: 31863057 [PubMed - as supplied by publisher] (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - December 20, 2019 Category: Drugs & Pharmacology Authors: Yang L, Zhao J, Qu Y, Sun Q, Li TT, Yan ML, Duan MJ, Li KX, Wang YR, Huang SY, Zhang S, Li Y, Ai J Tags: Acta Pharmacol Sin Source Type: research

Metoprolol prevents neuronal dendrite remodeling in a canine model of chronic obstructive sleep apnea
Acta Pharmacologica Sinica, Published online: 20 December 2019; doi:10.1038/s41401-019-0323-8Metoprolol prevents neuronal dendrite remodeling in a canine model of chronic obstructive sleep apnea (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - December 20, 2019 Category: Drugs & Pharmacology Authors: Lin Yang Jing Zhao Yang Qu Qiang Sun Ting-ting Li Mei-ling Yan Ming-jing Duan Ke-xin Li Yan-ru Wang Si-yu Huang Shuai Zhang Yue Li Jing Ai Source Type: research