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Acta Pharmacologica Sinica

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https://www.readbyqxmd.com/read/28552915/the-regioselective-glucuronidation-of-morphine-by-dimerized-human-ugt2b7-1a1-1a9-and-their-allelic-variants
#1
Zi-Zhao Yang, Li Li, Lu Wang, Ling-Min Yuan, Ming-Cheng Xu, Jing-Kai Gu, Hui-di Jiang, Lu-Shan Yu, Su Zeng
Uridine diphosphate-glucuronosyltransferase (UGT) 2B7 is expressed mostly in the human liver, lung and kidney and can transfer endogenous glucuronide group into its substrate and impact the pharmacological effects of several drugs such as estriol, AZT and morphine. UGT2B7 and its allelic variants can dimerize with the homologous enzymes UGT1A1 and UGT1A9, as well as their allelic variants, and then change their enzymatic activities in the process of substrate catalysis. The current study was designed to identify this mechanism using morphine as the substrate of UGT2B7...
May 29, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28552913/population-pharmacokinetic-analysis-of-tacrolimus-in-chinese-myasthenia-gravis-patients
#2
Yu-Si Chen, Zi-Qi Liu, Rong Chen, Lei Wang, Ling Huang, Xiao Zhu, Tian-Yan Zhou, Wei Lu, Ping Ma
The importance of tacrolimus in the treatment of myasthenia gravis (MG) as a substitute for corticosteroid-dependent immunosuppressive therapy is increasing. Thus far, however, no population pharmacokinetic (PopPK) analysis of tacrolimus in treating MG patients has been published. This article aimed to construct a PopPK model of tacrolimus for Chinese MG patients with the goal of improving its performance in MG treatment. A total of 253 trough concentration records were obtained from 83 Chinese MG patients...
May 29, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28552912/pterostilbene-suppresses-human-endometrial-cancer-cells-in-vitro-by-down-regulating-mir-663b
#3
Ya-Ling Wang, Yuan Shen, Jian-Ping Xu, Kun Han, Yan Zhou, Su Yang, Jun-Yi Yin, Da-Liu Min, Hai-Yan Hu
Resveratrol has long been known as an antioxidant and a chemopreventive agent. Similar to resveratrol, pterostilbene (PT) is also a phenolic compound extracted from the Vitis species. However, there are few studies on the antitumor effect of PT. Thus, we investigated the effects of PT on the endometrial cancer (EC) cells in vitro and the related molecular mechanisms. Treatment of EC cell lines HTB-111 and Ishikawa with PT (25-100 μmol/L) dose-dependently suppressed the cell viability and induced apoptosis...
May 29, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28552911/plumbagin-suppresses-chronic-periodontitis-in-rats-via-down-regulation-of-tnf-%C3%AE-il-1%C3%AE-and-il-6-expression
#4
Xin-Yi Zheng, Chuan-Yuan Mao, Han Qiao, Xi Zhang, Li Yu, Ting-Yu Wang, Eryi Lu
Chronic periodontitis (CP) is one of the most common oral diseases, which causes alveolar bone absorption and tooth loss in adults. In this study we aimed to investigate the potential of plumbagin (PL), a widely-investigated active compound extracted from the traditional Chinese herb Plumbago zeylanica L in treating CP. Human periodontal ligament stem cells (PDLSCs) were used for in vitro studies, whereas an animal model of CP was established in SD rats by ligation+Porphyromonas gingivalis (Pg) stimulation...
May 29, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28552908/xyloketal-b-alleviates-cerebral-infarction-and-neurologic-deficits-in-a-mouse-stroke-model-by-suppressing-the-ros-tlr4-nf-%C3%AE%C2%BAb-inflammatory-signaling-pathway
#5
Ni Pan, Liu-Yi Lu, Mei Li, Guo-Hao Wang, Fang-Yun Sun, Hong-Shuo Sun, Xue-Jun Wen, Jian-Ding Cheng, Jian-Wen Chen, Ji-Yan Pang, Jie Liu, Yong-Yuan Guan, Li-Yan Zhao, Wen-Liang Chen, Guan-Lei Wang
Xyloketal B (Xyl-B) is a novel marine compound isolated from mangrove fungus Xylaria sp. We previously demonstrated that pretreatment with Xyl-B exerted neuroprotective effects and attenuated hypoxic-ischemic brain injury in neonatal mice. In the present study we investigated the neuroprotective effects of pre- and post-treatment with Xyl-B in adult mice using a transient middle cerebral artery occlusion (tMCAO) model, and explored the underlying mechanisms. Adult male C57 mice were subjected to tMCAO surgery...
May 29, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28502980/w2476-ameliorates-%C3%AE-cell-dysfunction-and-exerts-therapeutic-effects-in-mouse-models-of-diabetes-via-modulation-of-the-thioredoxin-interacting-protein-signaling-pathway
#6
Ting Li, Guang-Yao Lin, Li Zhong, Yan Zhou, Jia Wang, Yue Zhu, Yang Feng, Xiao-Qing Cai, Qing Liu, Olivier Nosjean, Jean A Boutin, Pierre Renard, De-Hua Yang, Ming-Wei Wang
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, the discovery of compounds that either inhibit TXNIP activity or suppress its expression was the focus of the present study. INS-1E cells stably transfected with either a txnip proximal glucose response element connected to a luciferase reporter plasmid (BG73) or full-length txnip promoter connected to a luciferase reporter plasmid (CL108) were used in primary and secondary high-throughput screening campaigns, respectively...
May 15, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28502979/chrysin-ameliorates-podocyte-injury-and-slit-diaphragm-protein-loss-via-inhibition-of-the-perk-eif2%C3%AE-atf-chop-pathway-in-diabetic-mice
#7
Min-Kyung Kang, Sin-Hye Park, Yun-Ho Kim, Eun-Jung Lee, Lucia Dwi Antika, Dong Yeon Kim, Yean-Jung Choi, Young-Hee Kang
Glomerular epithelial podocytes are highly specialized cells that play a crucial role in maintaining normal function of the glomerular filtration barrier via their foot processes. Chrysin (5,7-dihydroxyflavone) is a natural flavonoid found in propolis and mushrooms that has anti-inflammatory, antioxidant and anticancer properties. This study aimed to evaluate the renoprotective effects of chrysin on podocyte apoptotic loss and slit diaphragm protein deficiency in high glucose-exposed podocytes and in db/db mouse kidneys...
May 15, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28502978/the-opioid-receptor-triple-agonist-dpi-125-produces-analgesia-with-less-respiratory-depression-and-reduced-abuse-liability
#8
Shou-Pu Yi, Qing-Hong Kong, Yu-Lei Li, Chen-Ling Pan, Jie Yu, Ben-Qiang Cui, Ying-Fei Wang, Guan-Lin Wang, Pei-Lan Zhou, Li-Li Wang, Ze-Hui Gong, Rui-Bin Su, Yue-Hai Shen, Gang Yu, Kwen-Jen Chang
Opioid analgesics remain the first choice for the treatment of moderate to severe pain, but they are also notorious for their respiratory depression and addictive effects. This study focused on the pharmacology of a novel opioid receptor mixed agonist DPI-125 and attempted to elucidate the relationship between the δ-, μ- and κ-receptor potency ratio and respiratory depression and abuse liability. Five diarylmethylpiperazine compounds (DPI-125, DPI-3290, DPI-130, KUST202 and KUST13T02) were selected for this study...
May 15, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28504250/curcumin-enhances-vascular-contractility-via-induction-of-myocardin-in-mouse-smooth-muscle-cells
#9
Shao-Wei Sun, Wen-Juan Tong, Zi-Fen Guo, Qin-Hui Tuo, Xiao-Yong Lei, Cai-Ping Zhang, Duan-Fang Liao, Jian-Xiong Chen
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, ig) for 6 weeks, the contractile responses of the thoracic aorta to KCl and phenylephrine were significantly enhanced compared with the control group. Furthermore, the contractility of vascular smooth muscle (SM) was significantly enhanced after incubation in curcumin (25 μmol/L) for 4 days, which was accompanied by upregulated expression of SM marker contractile proteins SM22α and SM α-actin...
May 1, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28504248/the-flavonoid-tl-2-8-induces-cell-death-and-immature-mitophagy-in-breast-cancer-cells-via-abrogating-the-function-of-the-aha1-hsp90-complex
#10
Hui-Juan Liu, Xiao-Xiao Jiang, Yi-Zhen Guo, Fang-Hui Sun, Xin-Hui Kou, Yong Bao, Zhu-Qing Zhang, Zhao-Hu Lin, Ting-Bo Ding, Lan Jiang, Xin-Sheng Lei, Yong-Hua Yang
The flavonoid quercetin exhibits significant anticancer activities with few side effects. In the current study, we characterized TL-2-8, a quercetin derivative, as a novel anticancer agent in vitro and in vivo. Cell proliferation and viability were assessed using Cell Counting Kit-8 and CellTiter-Blue assay, respectively. Cell death was examined using PI staining or a TUNEL assay. Mitophagy was determined by measuring autophagic flux and by confocal imaging. Protein expression was examined by Western blotting...
May 1, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28414207/defining-the-minimum-substrate-and-charge-recognition-model-of-gamma-secretase
#11
Yan Yan, Ting-Hai Xu, Karsten Melcher, H Eric Xu
γ-Secretase is an intramembrane aspartyl protease that cleaves the C99 fragment of amyloid precursor protein to generate extracellular Aβ peptides. These peptides can oligomerize and aggregate to form amyloid plaques, processes that are widely believed to be causal for Alzheimer's disease. In spite of this critical function, it remains unknown how γ-secretase recognizes C99 and its other substrates, including Notch. In this study we determined E22-K55 as the minimal C99 fragment that was sufficient and required for initial cleavage...
April 17, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28414206/wenshen-zhuanggu-formula-effectively-suppresses-breast-cancer-bone-metastases-in-a-mouse-xenograft-model
#12
Jia-Jia Li, Wei-Ling Chen, Jian-Yi Wang, Qian-Wen Hu, Zhen-Ping Sun, Shuai Zhang, Sheng Liu, Xiang-Hui Han
Wenshen Zhuanggu formula (WSZG) is a traditional Chinese medicine used as an adjuvant for the prevention of bone metastases in breast cancer patients. In this study we investigated the efficacy of WSZG in preventing bone metastases and the potential mechanisms in a mouse xenograft model of breast cancer bone metastases. This model was established by injection of human MDA-MB-231BO-Luc breast cancer cells alone or a mixture of the cancer cells with bone marrow-derived mesenchymal stem cells (BMSCs) into left ventricle of the heart in female nude mice...
April 17, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28414204/docking-based-structural-splicing-and-reassembly-strategy-to-develop-novel-deazapurine-derivatives-as-potent-b-raf-v600e-inhibitors
#13
Gui-Min Wang, Xiang Wang, Jian-Ming Zhu, Bin-Bin Guo, Zhuo Yang, Zhi-Jian Xu, Bo Li, He-Yao Wang, Ling-Hua Meng, Wei-Liang Zhu, Jian Ding
The mutation of B-Raf(V600E) is widespread in a variety of human cancers. Its inhibitors vemurafenib and dabrafenib have been launched as drugs for treating unresectable melanoma, demonstrating that B-Raf(V600E) is an ideal drug target. This study focused on developing novel B-Raf(V600E) inhibitors as drug leads against various cancers with B-Raf(V600E) mutation. Using molecular modeling approaches, 200 blockbuster drugs were spliced to generate 283 fragments followed by molecular docking to identify potent fragments...
April 17, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28414200/combining-53bp1-with-brca1-as-a-biomarker-to-predict-the-sensitivity-of-poly-adp-ribose-polymerase-parp-inhibitors
#14
Zhong-Min Yang, Xue-Mei Liao, Yi Chen, Yan-Yan Shen, Xin-Ying Yang, Yi Su, Yi-Ming Sun, Ying-Lei Gao, Jian Ding, Ao Zhang, Jin-Xue He, Ze-Hong Miao
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) genes and PARP inhibitor sensitivity, we selected BRCA1-deficient MDA-MB-436 cells to conduct RNA interference. Reducing expression of 53BP1, but not the other three HR genes, was found to lower simmiparib sensitivity...
April 17, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28414199/structure-of-the-prc2-complex-and-application-to-drug-discovery
#15
REVIEW
Yi Shi, Xiao-Xi Wang, You-Wen Zhuang, Yi Jiang, Karsten Melcher, H Eric Xu
The polycomb repressive complexes 2 (PRC2) complex catalyzes tri-methylation of histone H3 lysine 27 (H3K27), a repressive chromatin marker associated with gene silencing. Overexpression and mutations of PRC2 are found in a wide variety of cancers, making the catalytic activity of PRC2 an important target of cancer therapy. This review highlights recent structural breakthroughs of the human PRC2 complex bound to the H3K27 peptide and a small molecule inhibitor, which provide critically needed insight into PRC2-targeted drug discovery...
April 17, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28414198/ly333531-a-pkc%C3%AE-inhibitor-attenuates-glomerular-endothelial-cell-apoptosis-in-the-early-stage-of-mouse-diabetic-nephropathy-via-down-regulating-swiprosin-1
#16
Zhi-Bin Wang, Su Zhang, Ya Li, Rong-Mei Wang, Ling-Chang Tong, Yue Wang, Wei-Ye Liu, Ding-Feng Su, Ye Tu, Li-Chao Zhang, Ling Li
Glomerular endothelial cell (GEC) injury plays an important role in the early stage of diabetic nephropathy (DN). Previous studies show that a PKCβ inhibitor is effective for treating DN. In the current study we further explored the effects and molecular mechanisms of PKCβ inhibitors on GEC apoptosis in DN in streptozotocin-induced diabetic mice in vivo and high glucose- or PMA-treated human renal glomerular endothelial cells (HRGECs) in vitro. In the diabetic mice, hyperglycemia caused aggravated nephropathy and GEC apoptosis accompanied by significantly increased expression of swiprosin-1, a potentally pro-apoptotic protein...
April 17, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28392570/human-t-cell-lymphotropic-virus-type-1-and-its-oncogenesis
#17
REVIEW
Lan-Lan Zhang, Jing-Yun Wei, Long Wang, Shi-le Huang, Ji-Long Chen
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 efficient therapies against the viral infection and associated leukemia/lymphoma. It has been demonstrated to date that several HTLV-1 proteins play key roles in the cellular transformation and immortalization of infected T lymphocytes...
April 10, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28569768/cancer-nanobiotechnolgy
#18
EDITORIAL
Yong-Zhuo Huang, Ya-Ping Li
No abstract text is available yet for this article.
June 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28552914/claudin-4-targeted-nanographene-phototherapy-using-a-clostridium-perfringens-enterotoxin-peptide-photosensitizer-conjugate
#19
Gayong Shim, Mi-Gyeong Kim, Hyerim Jin, Jinyoung Kim, Yu-Kyoung Oh
In this study we designed a claudin 4-directed dual photodynamic and photothermal system, in which a 30-amino acid claudin 4-binding peptide, Clostridium perfringens enterotoxin (CPE), was linked to a photodynamic agent chlorin e6 (Ce6) through a polyethylene glycol spacer (CPC) and anchored onto reduced graphene oxide (rGO) nanosheets to form CPC/rGO nanosheets. For comparison, a conjugate of polyethylene glycol and Ce6 (PC) was anchored onto the rGO nanosheets to generate PC/rGO. Both PC and CPC generated reactive oxygen species upon irradiation at 660 nm...
June 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28552910/conjugated-polymer-nanomaterials-for-theranostics
#20
REVIEW
Cheng-Gen Qian, Yu-Lei Chen, Pei-Jian Feng, Xuan-Zhong Xiao, Mei Dong, Ji-Cheng Yu, Quan-Yin Hu, Qun-Dong Shen, Zhen Gu
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-infrared (NIR) imaging, two-photon (TP) imaging, photoacoustic (PA) imaging, and multimodal (MM) imaging, are introduced. Then, CPN-based photodynamic therapy (PDT) and photothermal therapy (PTT) are surveyed...
June 2017: Acta Pharmacologica Sinica
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