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Acta Pharmacologica Sinica

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https://www.readbyqxmd.com/read/28317873/a-new-method-to-evaluate-the-dose-effect-relationship-of-a-tcm-formula-gegen-qinlian-decoction-focus-mode-of-integrated-biomarkers
#1
Zhi-Qiang Huang, Xue-Mei Fan, Yi-Ming Wang, Qiong-Lin Liang, Xiao-Lin Tong, Yu Bai, Ying-Meng Li, Guo-An Luo, Chao Chen
It is difficult to accurately evaluate the efficacy of traditional Chinese medicine (TCM), which leads to the uncertainty and complexity of dose-effect analysis. In this study we established the "Focus" mode of biomarkers to characterize the dose-effect relationship of Gegen Qinlian Decoction (GQD), a TCM formula for treating type 2 diabetes mellitus (2-DM). A rat model of 2-DM was established through high fat diet feeding combined with low-dose STZ injection. Rats with 2-DM were administered high, middle or low doses (6...
March 20, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28317872/preclinical-evaluation-of-the-efficacy-pharmacokinetics-and-immunogenicity-of-js-001-a-programmed-cell-death-protein-1-pd-1-monoclonal-antibody
#2
Jie Fu, Fang Wang, Li-Hou Dong, Jing Zhang, Cheng-Lian Deng, Xue-Li Wang, Xin-Yao Xie, Jing Zhang, Ruo-Xian Deng, Li-Bo Zhang, Hai Wu, Hui Feng, Bo Chen, Hai-Feng Song
JS-001 is the first monoclonal antibody (mAb) against programmed cell death protein-1 (PD-1) approved by the China Food and Drug Administration (CFDA) into the clinical trails. To date, however, no pre-clinical pharmacological and pharmacokinetic (PK) data are available. In this study, we investigated the efficacy of JS-001 and conducted a preclinical PK study, including the monitoring of anti-drug antibodies (ADAs). We found that JS-001 specifically bound to PD-1 antigen with an EC50 of 21 nmol/L, and competently blocked the binding of PD-1 antigen to PD-L1 and PD-L2 with IC50 of 3...
March 20, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28317871/insights-into-molecular-therapy-of-glioma-current-challenges-and-next-generation-blueprint
#3
REVIEW
Y Rajesh, Ipsita Pal, Payel Banik, Sandipan Chakraborty, Sachin A Borkar, Goutam Dey, Ahona Mukherjee, Mahitosh Mandal
Glioma accounts for the majority of human brain tumors. With prevailing treatment regimens, the patients have poor survival rates. In spite of current development in mainstream glioma therapy, a cure for glioma appears to be out of reach. The infiltrative nature of glioma and acquired resistance substancially restrict the therapeutic options. Better elucidation of the complicated pathobiology of glioma and proteogenomic characterization might eventually open novel avenues for the design of more sophisticated and effective combination regimens...
March 20, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28260803/reversal-of-paclitaxel-resistance-in-human-ovarian-cancer-cells-with-redox-responsive-micelles-consisting-of-%C3%AE-tocopheryl-succinate-based-polyphosphoester-copolymers
#4
Feng-Qian Chen, Jin-Ming Zhang, Xie-Fan Fang, Hua Yu, Yu-Ling Liu, Hui Li, Yi-Tao Wang, Mei-Wan Chen
P-glycoprotein (P-gp)-mediated multidrug resistance (MDR) is a major obstacle in achieving the therapeutic benefits of paclitaxel (PTX) in the treatment of human ovarian carcinoma. This study is aimed to develop an efficient PTX drug delivery approach to overcome MDR. Redox-responsive micelles consisting of amphiphilic polymers containing disulfide linkages, ie, poly (phosphate ester)-SS-D-α-tocopheryl succinate (POPEA-SS-TOS, PSST) were prepared. PTX-loaded PSST micelles (PTX/PSST-M) designed to display synergistic functions, including reversible inhibition of P-gp, intracellular redox-sensitive release and potent anticancer activities...
March 6, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28260802/autophagy-inhibitor-3-methyladenine-alleviates-overload-exercise-induced-cardiac-injury-in-rats
#5
Hua Liu, Hui Lei, Yue Shi, Jin-Ju Wang, Ning Chen, Zhang-Hua Li, Yang-Fang Chen, Qi-Fa Ye, Yi Yang
Overload-exercise (OE) causes myocardial injury through inducing autophagy and apoptosis. In this study we examined whether an autophagy inhibitor 3-methyladenine (3-MA) could alleviate OE-induced cardiac injury. Rats were injected with 3-MA (15 mg/kg, iv) or saline before subjected to various intensities of OE, including no swim (control), 2 h swim (mild-intensity exercise, MIE), 2 h swim with 2.5% body weight overload (moderate OE; MOE), 5% overload (intensive OE; IOE) or 2.5% overload until exhausted (exhaustive OE; EOE)...
March 6, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28260801/regulation-of-microglial-activation-in-stroke
#6
REVIEW
Shou-Cai Zhao, Ling-Song Ma, Zhao-Hu Chu, Heng Xu, Wen-Qian Wu, Fudong Liu
When ischemic stroke occurs, oxygen and energy depletion triggers a cascade of events, including inflammatory responses, glutamate excitotoxicity, oxidative stress, and apoptosis that result in a profound brain injury. The inflammatory response contributes to secondary neuronal damage, which exerts a substantial impact on both acute ischemic injury and the chronic recovery of the brain function. Microglia are the resident immune cells in the brain that constantly monitor brain microenvironment under normal conditions...
March 6, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28260800/a-novel-stat3-inhibitor-negatively-modulates-platelet-activation-and-aggregation
#7
Zhuan Xu, Yu-Jia Xu, Ya-Nan Hao, Li-Jie Ren, Zu-Bin Zhang, Xin Xu, Bi-Yin Cao, Ke-Sheng Dai, Li Zhu, Qi Fang, Yan Kong, Xin-Liang Mao
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 ChronoLog aggregometer was used to evaluate platelet aggregation. A flow cytometer was used to evaluate P-selectin expression in the presence of SC99. AlamarBlue and Annexin-V staining were used to evaluate platelet viability and apoptosis, respectively...
March 6, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28260799/bisindolylmaleimide-alkaloid-bma-155cl-induces-autophagy-and-apoptosis-in-human-hepatocarcinoma-hepg-2-cells-through-the-nf-%C3%AE%C2%BAb-p65-pathway
#8
Xiao Sun, Lin Li, Hong-Guang Ma, Pu Sun, Qi-Lin Wang, Ting-Ting Zhang, Yue-Mao Shen, Wei-Ming Zhu, Xia Li
Bisindolylmaleimides, a series of derivatives of a PKC inhibitor staurosporine, exhibit potential as anti-cancer drugs and have received considerable attention in clinical trials. This study aims to investigate the effects of a bisindolylmaleimide alkaloid 155Cl (BMA-155Cl) with a novel structure on autophagy and apoptosis in human hepatocarcinoma HepG-2 cells in vitro and in vivo. The cell poliferation was assessed with a MTT assay. Autophagy was evaluated by MDC staining and TEM analysis. Apoptosis was investigated using Annexin V-FITC/PI and DAPI staining...
March 6, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28260798/geniposide-ameliorates-tnbs-induced-experimental-colitis-in-rats-via-reducing-inflammatory-cytokine-release-and-restoring-impaired-intestinal-barrier-function
#9
Bin Xu, Yan-Li Li, Ming Xu, Chang-Chun Yu, Meng-Qiao Lian, Ze-Yao Tang, Chuan-Xun Li, Yuan Lin
Geniposide is an iridoid glycosides purified from the fruit of Gardenia jasminoides Ellis, which is known to have antiinflammatory, anti-oxidative and anti-tumor activities. The present study aimed to investigate the effects of geniposide on experimental rat colitis and to reveal the related mechanisms. Experimental rat colitis was induced by rectal administration of a TNBS solution. The rats were treated with geniposide (25, 50 mg·kg(-1)·d(-1), ig) or with sulfasalazine (SASP, 100 mg·kg(-1)·d(-1), ig) as positive control for 14 consecutive days...
March 6, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28260797/molecular-design-and-synthesis-of-self-assembling-camptothecin-drug-amphiphiles
#10
Andrew G Cheetham, Yi-An Lin, Ran Lin, Honggang Cui
The conjugation of small molecular hydrophobic anticancer drugs onto a short peptide with overall hydrophilicity to create self-assembling drug amphiphiles offers a new prodrug strategy, producing well-defined, discrete nanostructures with a high and quantitative drug loading. Here we show the detailed synthesis procedure and how the molecular structure can influence the synthesis of the self-assembling prodrugs and the physicochemical properties of their assemblies. A series of camptothecin-based drug amphiphiles were synthesized via combined solid- and solution-phase synthetic techniques, and the physicochemical properties of their self-assembled nanostructures were probed using a number of imaging and spectroscopic techniques...
March 6, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28260796/association-between-well-characterized-lung-cancer-lncrna-polymorphisms-and-platinum-based-chemotherapy-toxicity-in-chinese-patients-with-lung-cancer
#11
Wei-Jing Gong, Jing-Bo Peng, Ji-Ye Yin, Xiang-Ping Li, Wei Zheng, Ling Xiao, Li-Ming Tan, Di Xiao, Yi-Xin Chen, Xi Li, Hong-Hao Zhou, Zhao-Qian Liu
Platinum-based chemotherapy is the standard first-line treatment for most lung cancer patients. However, the toxicity induced by platinum-based chemotherapy greatly impedes its clinical use. Previous studies showed that long non-coding RNAs (lncRNAs) with over 200 nucleotides in length affect drug response and toxicity. In the present study, we investigated the association of well-characterized lung cancer lncRNA polymorphisms with platinum-based chemotherapy toxicity in Chinese patients with lung cancer. A total of 467 lung cancer patients treated with platinum-based chemotherapy for at least two cycles were recruited...
March 6, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28239160/insights-into-the-molecular-mechanisms-of-polygonum-multiflorum-thunb-induced-liver-injury-a-computational-systems-toxicology-approach
#12
Yin-Yin Wang, Jie Li, Zeng-Rui Wu, Bo Zhang, Hong-Bin Yang, Qin Wang, Ying-Chun Cai, Gui-Xia Liu, Wei-Hua Li, Yun Tang
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 components of PmT were extracted from 3 main TCM databases as well as the literature related to natural products. Then, the known targets were collected through data integration, and the potential compound-target interactions (CTIs) were predicted using our substructure-drug-target network-based inference (SDTNBI) method...
February 27, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28239159/sarsasapogenin-aa13-inhibits-lps-induced-inflammatory-responses-in-macrophage-cells-in-vitro-and-relieves-dimethylbenzene-induced-ear-edema-in-mice
#13
Dong Dong, Nan-Nan Zhou, Rui-Xuan Liu, Jia-Wei Xiong, Hui Pan, Si-Qi Sun, Lei Ma, Rui Wang
Sarsasapogenin-AA13 (AA13) is a novel synthetic derivative of sarsasapogenin extracted from the Chinese herb Rhizoma Anemarrhenae. In this study we investigated the effects of AA13 on lipopolysaccharide (LPS)-induced production of inflammatory factors in macrophage cells and the anti-inflammatory activity of AA13 in an inflammatory model of dimethylbenzene-induced ear edema. Macrophage cells (RAW264.7 cells and mouse peritoneal macrophages) were exposed to LPS (1 μg/mL); pretreatment with AA13 (5-20 μmol/L) dose-dependently inhibited LPS-induced production of NO, TNF-α and PGE2, and LPS-stimulated expression levels of COX-2 and iNOS...
February 27, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28239158/synthesis-of-the-novel-parp-1-inhibitor-ag-690-11026014-and-its-protective-effects-on-angiotensin-ii-induced-mouse-cardiac-remodeling
#14
Guo-Shuai Feng, Cui-Ge Zhu, Zhuo-Ming Li, Pan-Xia Wang, Yi Huang, Min Liu, Ping He, Lan-Lan Lou, Shao-Rui Chen, Pei-Qing Liu
We previously identified AG-690/11026014 (6014) as a novel poly(ADP-ribose) polymerase-1 (PARP-1) inhibitor that effectively prevented angiotensin II (Ang II)-induced cardiomyocyte hypertrophy. In the present study, we reported a new synthesis route for 6014, and investigated its protective effects on Ang II-induced cardiac remodeling and cardiac dysfunction and the underlying mechanisms in mice. We designed a new synthesis route to obtain a sufficient quantity of 6014 for this in vivo study. C57BL/6J mice were infused with Ang II and treated with 6014 (10, 30, 90 mg·kg(-1)·d(-1), ig) for 4 weeks...
February 27, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28216625/endothelial-overexpression-of-endothelin-1-modulates-aortic-carotid-iliac-and-renal-arterial-responses-in-obese-mice
#15
Oliver Baretella, Sookja K Chung, Aimin Xu, Paul M Vanhoutte
Endothelin-1 (ET-1) is essential for mammalian development and life, but it has also been implicated in increased cardiovascular risk under pathophysiological conditions. The aim of this study was to determine the impact of endothelial overexpression of the prepro-endothelin-1 gene on endothelium-dependent and endothelium-independent responses in the conduit and renal arteries of lean and obese mice. Obesity was induced by high-fat-diet (HFD) consumption in mice with Tie-1 promoter-driven, endothelium-specific overexpression of the prepro-endothelin-1 gene (TET(het)) and in wild-type (WT) littermates on a C57BL/6N background...
February 20, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28216624/dual-targeted-hybrid-nanoparticles-of-synergistic-drugs-for-treating-lung-metastases-of-triple-negative-breast-cancer-in-mice
#16
Tian Zhang, Preethy Prasad, Ping Cai, Chunsheng He, Dan Shan, Andrew Michael Rauth, Xiao Yu Wu
Lung metastasis is the major cause of death in patients with triple negative breast cancer (TNBC), an aggressive subtype of breast cancer with no effective therapy at present. It has been proposed that dual-targeted therapy, ie, targeting chemotherapeutic agents to both tumor vasculature and cancer cells, may offer some advantages. The present work was aimed to develop a dual-targeted synergistic drug combination nanomedicine for the treatment of lung metastases of TNBC. Thus, Arg-Gly-Asp peptide (RGD)-conjugated, doxorubicin (DOX) and mitomycin C (MMC) co-loaded polymer-lipid hybrid nanoparticles (RGD-DMPLN) were prepared and characterized...
February 20, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28216622/effects-of-gene-polymorphisms-in-the-endoplasmic-reticulum-stress-pathway-on-clinical-outcomes-of-chemoradiotherapy-in-chinese-patients-with-nasopharyngeal-carcinoma
#17
Xiao-Bin Guo, Wan-le Ma, Li-Juan Liu, Yu-Ling Huang, Jing Wang, Li-Hua Huang, Xiang-Dong Peng, Ji-Ye Yin, Jin-Gao Li, Shao-Jun Chen, Guo-Ping Yang, Hui Wang, Cheng-Xian Guo
There is considerable inter-individual variabil¬ity in chemoradiotherapy responses in nasopharyngeal carcinoma (NPC) patients receiv¬ing the same or similar treatment protocols. In this study we evaluated the association between the gene polymorphisms in endoplasmic reticulum (ER) stress pathway and chemoradiation responses in Chinese NPC patients. A total of 150 patients with histopathologically conformed NPC and treated with concurrent chemoradiotherapy were enrolled. Genotypes in ER stress pathway genes, including VCP (valosin-containing protein) rs2074549, HSP90B1 rs17034943, CANX (calnexin) rs7566, HSPA5 [heat shock protein family A (Hsp70) member 5] rs430397, CALCR (calcitonin receptor) rs2528521, and XBP1 (X-box binding protein 1) rs2269577 were analyzed by Sequenom MassARRAY system...
February 20, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28216621/dual-anti-ischemic-effects-of-rosmarinic-acid-n-butyl-ester-via-alleviation-of-dapk-p53-mediated-neuronal-damage-and-microglial-inflammation
#18
Lei Wu, Hong-Min Wang, Jin-Long Li, Hong-Xuan Feng, Wei-Min Zhao, Hai-Yan Zhang
The discovery of efficacious anti-ischemic drugs remains a challenge. Recently we have found that rosmarinic acid n-butyl ester (RABE), a derivative of rosmarinic acid, significantly protects SH-SY5Y cells against oxygen glucose deprivation (OGD)-induced cell death. In the present study we simultaneously investigated the effects of RABE on the two key players in the pathophysiology of cerebral ischemia, ischemic neuronal damage and microglial inflammation. Pretreatment with RABE (1, 10 μmol/L) dose-dependently attenuated OGD- or H2O2-induced reduction of the viability of SH-SY5Y neuroblastoma cells...
February 20, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28216620/aspirin-alleviates-cardiac-fibrosis-in-mice-by-inhibiting-autophagy
#19
Ping-Ping Liu, Hong-Hong Liu, Shu-Hong Sun, Xing-Xing Shi, Wan-Cheng Yang, Guo-Hai Su, Jing Zhao
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 cardiac fibrosis. The animals were treated with ASA (10 mg·kg(-1)·d(-1), ig) for 21 and 14 d, respectively. ASA administration significantly improved cardiac function, and ameliorated heart damage and fibrosis in the mice...
February 20, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28216619/15-deoxy-%C3%AE-12-14-prostaglandin-j2-alleviates-hepatic-ischemia-reperfusion-injury-in-mice-via-inducing-antioxidant-response-and-inhibiting-apoptosis-and-autophagy
#20
Kan Chen, Jing-Jing Li, Sai-Nan Li, Jiao Feng, Tong Liu, Fan Wang, Wei-Qi Dai, Yu-Jing Xia, Jie Lu, Ying-Qun Zhou, Chuan-Yong Guo
Hepatic ischemia-reperfusion (I/R) injury is a common clinical impairment that occurs in many circumstances and leads to poor prognosis. Both apoptosis and autophagy have been shown to contribute to cell death in hepatic I/R injury. 15-Deoxy-Δ(12,14)-prostaglandin J2 (15d-PGJ2) is one of the best-studied anti-inflammatory prostaglandins, which has been verified to exert anti-inflammatory and cell-protective functions in various types of cells and animal models. In this study we explored the effects of 15d-PGJ2 on both apoptosis and autophagy in mouse hepatic I/R injury and its possible mechanisms...
February 20, 2017: Acta Pharmacologica Sinica
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