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Acta Pharmacologica Sinica

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https://www.readbyqxmd.com/read/29789664/the-bet-bromodomain-inhibitor-apabetalone-induces-apoptosis-of-latent-hiv-1-reservoir-cells-following-viral-reactivation
#1
Xuan-Xuan Zhang, Jian Lin, Tai-Zhen Liang, Heng Duan, Xing-Hua Tan, Bao-Min Xi, Lin Li, Shu-Wen Liu
The persistence of latent HIV-1 reservoirs throughout combination antiretroviral therapy (cART) is a major barrier on the path to achieving a cure for AIDS. It has been shown that bromodomain and extra-terminal (BET) inhibitors could reactivate HIV-1 latency, but restrained from clinical application due to their toxicity and side effects. Thus, identifying a new type of BET inhibitor with high degrees of selectivity and safety is urgently needed. Apabetalone is a small-molecule selective BET inhibitor specific for second bromodomains, and has been evaluated in phase III clinical trials that enrolled patients with high-risk cardiovascular disorders, dyslipidemia, and low HDL cholesterol...
May 22, 2018: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/29777203/ginkgo-biloba-extracts-prevent-aortic-rupture-in-angiotensin-ii-infused-hypercholesterolemic-mice
#2
Xiao-Fang Huang, Song-Zhao Zhang, Ya-Yu You, Na Zhang, Hong Lu, Alan Daugherty, Xiao-Jie Xie
Abdominal aortic aneurysms (AAAs) are a chronic vascular disease characterized by pathological luminal dilation. Aortic rupture is the fatal consequence of AAAs. Ginkgo biloba extracts (GBEs), a natural herb extract widely used as food supplements, drugs, and cosmetics, has been reported to suppress development of calcium chloride-induced AAAs in mice. Calcium chloride-induced AAAs do not rupture, while angiotensin II (AngII)-induced AAAs in mice have high rate of aortic rupture, implicating potentially different mechanisms from calcium chloride-induced AAAs...
May 18, 2018: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/29777202/aberrant-modulation-of-ribosomal-protein-s6-phosphorylation-confers-acquired-resistance-to-mapk-pathway-inhibitors-in-braf-mutant-melanoma
#3
Ming-Zhao Gao, Hong-Bin Wang, Xiang-Ling Chen, Wen-Ting Cao, Li Fu, Yun Li, Hai-Tian Quan, Cheng-Ying Xie, Li-Guang Lou
BRAF and MEK inhibitors have shown remarkable clinical efficacy in BRAF-mutant melanoma; however, most patients develop resistance, which limits the clinical benefit of these agents. In this study, we found that the human melanoma cell clones, A375-DR and A375-TR, with acquired resistance to BRAF inhibitor dabrafenib and MEK inhibitor trametinib, were cross resistant to other MAPK pathway inhibitors. In these resistant cells, phosphorylation of ribosomal protein S6 (rpS6) but not phosphorylation of ERK or p90 ribosomal S6 kinase (RSK) were unable to be inhibited by MAPK pathway inhibitors...
May 18, 2018: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/29777201/novel-smoothened-inhibitors-for-therapeutic-targeting-of-na%C3%A3-ve-and-drug-resistant-hedgehog-pathway-driven-cancers
#4
Qing-Rou Li, Hui Zhao, Xue-Sai Zhang, Henk Lang, Ker Yu
The G protein-coupled receptor (GPCR) smoothened (SMO) is a key signaling component of the sonic hedgehog (Hh) pathway and a clinically validated target for cancer treatment. The FDA-approved SMO inhibitors GDC-0449/Vismodegib and LDE225/Sonidegib demonstrated clinical antitumor efficacy. Nevertheless, relatively high percentage of treated patients would eventually develop acquired cross resistance to both drugs. Here, based on published structure and activity of GDC-0449 inhibitor class, we replaced its amide core with benzimidazole which retained bulk of the SMO-targeting activity as measured in our Hh/SMO/Gli1-reporter system...
May 18, 2018: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/29773888/antitumor-effect-of-axitinib-combined-with-dopamine-and-pk-pd-modeling-in-the-treatment-of-human-breast-cancer-xenograft
#5
Yuan-Heng Ma, Si-Yuan Wang, Yu-Peng Ren, Jian Li, Ting-Jie Guo, Wei Lu, Tian-Yan Zhou
Rising evidence has shown the development of resistance to vascular endothelial growth factor receptor (VEGFR) inhibitors in the practices of cancer therapy. It is reported that the efficacy of axitinib (AX), a VEGFR inhibitor, is limited in the treatment of breast cancer as a single agent or in combination with other chemotherapeutic drugs due to the probability of rising population of cancer stem-like cells (CSCs) caused by AX. The present study evaluated the effect of dopamine (DA) improving AX's efficacy on MCF-7/ADR breast cancer in vitro and in vivo, and developed a pharmacokinetic-pharmacodynamic (PK-PD) model describing the in vivo experimental data and characterizing the interaction of effect between AX and DA...
May 17, 2018: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/29773887/varacin-1-a-novel-analog-of-varacin-c-induces-p53-independent-apoptosis-in-cancer-cells-through-ros-mediated-reduction-of-xiap
#6
Jing Zhou, Wen-Li Li, Zi-Xuan Wang, Nai-Yuan Chen, Yue Tang, Xiao-Xiao Hu, Jing-Huan Deng, Yixin Lu, Guo-Dong Lu
Varacin C is a promising anticancer agent and possesses acid-promoted and photo-induced DNA-damaging activities. In this study, we synthesized an analog varacin-1 (VCA-1) and examined its anticancer potentials. The results demonstrated that VCA-1 caused dose-dependent apoptotic cell death in cancer cells. Note that this action is independent of p53 status, because VCA-1 induced similar levels of apoptosis in two different panels of cell lines (HCT116 p53- wild-type vs. HCT116 p53-knockout colon cancer cells, and p53-expressing U2OS vs...
May 17, 2018: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/29773886/pretreatment-with-broad-spectrum-antibiotics-alters-the-pharmacokinetics-of-major-constituents-of-shaoyao-gancao-decoction-in-rats-after-oral-administration
#7
Meng Liu, Jie Yuan, Wen-Juan Hu, Chang-Qiang Ke, Yi-Fan Zhang, Yang Ye, Da-Fang Zhong, Guang-Rong Zhao, Sheng Yao, Jia Liu
The influence of broad-spectrum antibiotics on the pharmacokinetics and biotransformation of major constituents of Shaoyao-Gancao decoction (SGD) in rats was investigated. The pharmacokinetic behaviors of paeoniflorin (PF), albiflorin (AF), liquiritin (LT), isoliquiritin (ILT), liquiritin apioside (LA), isoliquiritin apioside (ILA), and glycyrrhizic acid (GL), seven major constituents of SGD, as well as glycyrrhetinic acid (GA), a major metabolite of GL, were analyzed. A 1-week pretreatment with broad-spectrum antibiotics (ampicillin, metronidazole, neomycin, 1 g L-1 ; and vancomycin, 0...
May 17, 2018: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/29773885/metabolic-perturbations-of-post-load-hyperglycemia-vs-fasting-hyperglycemia
#8
Jing-Yi Lu, Jia-Hui Peng, Xiao-Jing Ma, Yi-Nan Zhang, Wei Zhu, Xing-Xing He, Ling-Wen Ying, Yu-Qian Bao, Jian Zhou, Wei-Ping Jia
There is evidence that post-load/post-meal hyperglycemia is a stronger risk factor for cardiovascular disease than fasting hyperglycemia. The underlying mechanism remains to be elucidated. The current study aimed to compare the metabolic profiles of post-load hyperglycemia and fasting hyperglycemia. All subjects received an oral glucose tolerance test (OGTT) and were stratified into fasting hyperglycemia (FH) or post-load hyperglycemia (PH). Forty-six (FH, n = 23; PH, n = 23) and 40 patients (FH, n = 20; PH, n = 20) were recruited as the exploratory and the validation set, respectively, and underwent metabolic profiling...
May 17, 2018: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/29770800/current-and-future-circulating-biomarkers-for-cardiac-amyloidosis
#9
REVIEW
Marco Luciani, Luca Troncone, Federica Del Monte
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 formation of a single misfolded protein (monomer) that progressively evolves and ultimately forms amyloid fibers. Additionally, by seeding out from the organs of origin, intermediates called oligomers metastasize and restart the process...
May 17, 2018: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/29770799/heart-type-fatty-acid-binding-protein-h-fabp-as-a-biomarker-for-acute-myocardial-injury-and-long-term-post-ischemic-prognosis
#10
REVIEW
Xiao-Dong Ye, Yi He, Sheng Wang, Gordon T Wong, Michael G Irwin, Zhengyuan Xia
Acute myocardial infarction (AMI) is a life-threatening event. Even with timely treatment, acute ischemic myocardial injury and ensuing ischemia reperfusion injury (IRI) can still be difficult issues to tackle. Apart from radiological and other auxiliary examinations, laboratory tests of applicable cardiac biomarkers are also necessary for early diagnosis and close monitoring of this disorder. Heart-type fatty acid binding protein (H-FABP), which mainly exists inside cardiomyocytes, has recently emerged as a potentially promising biomarker for myocardial injury...
May 17, 2018: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/29770798/combined-treatment-with-apatinib-and-docetaxel-in-a549-xenograft-mice-and-its-cellular-pharmacokinetic-basis
#11
Si-Qi Feng, Guang-Ji Wang, Jing-Wei Zhang, Yuan Xie, Run-Bin Sun, Fei Fei, Jing-Qiu Huang, Ying Wang, Ji-Ye Aa, Fang Zhou
Apatinib, a small-molecule inhibitor of VEGFR-2, has attracted much attention due to its encouraging anticancer activity in third-line clinical treatment for many malignancies, including non-small cell lung cancer (NSCLC). Its usage in second-line therapy with chemotherapeutic drugs is still under exploration. In this study we investigated the antitumor effect of apatinib combined with docetaxel against NSCLC and its cellular pharmacokinetic basis. A549 xenograft nude mice were treated with apatinib (100 mg/kg every day for 20 days) combined with docetaxel (8 mg/kg, ip, every four days for 5 times)...
May 17, 2018: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/29770797/correlation-of-the-predisposition-of-chinese-children-to-cerebral-palsy-with-nucleotide-variation-in-pri-mir-124-that-alters-the-non-canonical-apoptosis-pathway
#12
Hui Li, Xiu-Li Wang, Yan-Qiu Wu, Xiu-Mei Liu, Ai-Min Li
Cerebral palsy is a group of non-progressive motor impairment syndromes caused by brain lesions during development. Herein, we investigated the relationship between nucleotide variations in a miRNA coding region and the predisposition of Chinese children to cerebral palsy. A total of 233 CP patients and 256 healthy participants were enrolled, and 60 children were selected from each group for plasma miRNA detection. We screened the coding regions of pri-miR-124-1, -2, and -3 using PCR and sequencing. The expression of miR-124 was determined by qRT-PCR...
May 17, 2018: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/29770796/suppression-of-mif-induced-neuronal-apoptosis-may-underlie-the-therapeutic-effects-of-effective-components-of-fufang-danshen-in-the-treatment-of-alzheimer-s-disease
#13
Cheng-Jie Liang, Jia-Huang Li, Zhen Zhang, Ju-Yan Zhang, Shu-Qun Liu, Jie Yang
Fufang Danshen (FFDS or Compound Danshen) consists of three Chinese herbs Danshen (Salviae miltiorrhizae radix et rhizome), Sanqi (Notoginseng radix et rhizome) and Tianranbingpian (Borneolum, or D-borneol), which has been show to significantly improve the function of the nervous system and brain metabolism. In this study we explored the possible mechanisms underlying the therapeutic effects of the combination of the effective components of FFDS (Tan IIA, NG-R1 and Borneol) in the treatment of Alzheimer's disease (AD) based on network pharmacology...
May 17, 2018: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/29770795/cytokines-as-biomarkers-of-inflammatory-response-after-open-versus-endovascular-repair-of-abdominal-aortic-aneurysms-a-systematic-review
#14
REVIEW
Diamantis I Tsilimigras, Fragiska Sigala, Georgios Karaolanis, Ioannis Ntanasis-Stathopoulos, Eleftherios Spartalis, Michael Spartalis, Nikolaos Patelis, Alexandros Papalampros, Chandler Long, Demetrios Moris
The repair of an abdominal aortic aneurysm (AAA) is a high-risk surgical procedure related to hormonal and metabolic stress-related response with an ensuing activation of the inflammatory cascade. In contrast to open repair (OR), endovascular aortic aneurysm repair (EVAR) seems to decrease the postoperative stress by offering less extensive incisions, dissection, and tissue manipulation. However, these beneficial effects may be offset by the release of cytokines and arachidonic acid metabolites during intra-luminal manipulation of the thrombus using catheters in endovascular repair, resulting in systemic inflammatory response (SIR), which is clinically called post-implantation syndrome...
May 17, 2018: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/29770794/ursodeoxycholic-acid-protects-interstitial-cajal-like-cells-in-the-gallbladder-from-undergoing-apoptosis-by-inhibiting-tnf-%C3%AE-expression
#15
Jiang-Fan Wan, Shi-Feng Chu, Xin Zhou, Yue-Ting Li, Wen-Bin He, Feng Tan, Piao Luo, Qi-di Ai, Qi Wang, Nai-Hong Chen
Hypomotility is a common symptom of gallstone disease, which is accompanied by a loss of interstitial Cajal-like cells (ICLCs) in the gallbladder. Ursodeoxycholic acid (UDCA) is widely used in treating gallstone disease, and has shown anti-apoptotic and anti-inflammatory effects apart from its ability to dissolve gallstones. In this study, we investigated the anti-apoptotic and anti-inflammatory effects of UDCA on ICLCs in guinea pigs with gallstones. Guinea pigs were fed a high-cholesterol diet for 8 weeks to induce the formation of gallstones...
May 17, 2018: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/29769744/nadph-ameliorates-mptp-induced-dopaminergic-neurodegeneration-through-inhibiting-p38mapk-activation
#16
Jing-Si Zhou, Zhou Zhu, Feng Wu, Ying Zhou, Rui Sheng, Jun-Chao Wu, Zheng-Hong Qin
Parkinson's disease (PD) is the second most common neurodegenerative disorder characterized by the selective loss of dopaminergic neurons in substantia nigra pars compacta (SNpc). Although the pathogenic mechanism underlying PD remains largely unknown, decreased nigral glutathione (GSH) in postmortem brains of PD patients supports the presence of oxidative stress in PD. We found that Nicotinamide adenine dinucleotide phosphate (NADPH), which is important for maintaining the level of GSH, protected dopaminergic (DA) neurons from neurotoxicity of MPTP/MPP+ ...
May 16, 2018: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/29769743/tigar-knockdown-enhanced-the-anticancer-effect-of-aescin-via-regulating-autophagy-and-apoptosis-in-colorectal-cancer-cells
#17
Bin Li, Zhong Wang, Jia-Ming Xie, Gang Wang, Li-Qiang Qian, Xue-Mei Guan, Xue-Ping Shen, Zheng-Hong Qin, Gen-Hai Shen, Xiao-Qiang Li, Quan-Gen Gao
Our previous study showed that TP53-induced glycolysis and apoptosis regulator (TIGAR) regulated ROS, autophagy, and apoptosis in response to hypoxia and chemotherapeutic drugs. Aescin, a triterpene saponin, exerts anticancer effects and increases ROS levels. The ROS is a key upstream signaling to activate autophagy. Whether there is a crosstalk between TIGAR and aescin in regulating ROS, autophagy, and apoptosis is unknown. In this study, we found that aescin inhibited cell viability and colony formation, and induced DNA damage, cell cycle arrest, and apoptosis in cancer cell lines HCT-116 and HCT-8 cells...
May 16, 2018: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/29769742/modified-citrus-pectin-inhibited-bladder-tumor-growth-through-downregulation-of-galectin-3
#18
Tian Fang, Dan-Dan Liu, He-Ming Ning, Dan Liu, Jing-Ya Sun, Xiao-Jing Huang, Yu Dong, Mei-Yu Geng, Shi-Feng Yun, Jun Yan, Rui-Min Huang
Modified citrus pectin (MCP) is a carbohydrate enriched complex, which has been implicated in cancer treatment and prevention. However, the effects of MCP on urinary bladder cancer (UBC) are unknown. In this study, MCP was first tested in T24 and J82 human UBC cells and showed the inhibition of cell viability by the sulforhodamine B (SRB) assay. The MCP-treated UBC cells exhibited G2 /M phase arrest with the decrease of Cyclin B1 and phosphorylated Cdc2. Caspase-3 was also activated, leading to the cleavage of Caspase-3 and PARP...
May 16, 2018: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/29698390/microrna-expression-profile-and-functional-analysis-reveal-their-roles-in-contact-inhibition-and-its-disruption-switch-of-rat-vascular-smooth-muscle-cells
#19
REVIEW
Ye-Ying Sun, Shan-Shan Qin, Yun-Hui Cheng, Chao-Yun Wang, Xiao-Jun Liu, Ying Liu, Xiu-Li Zhang, Wendy Zhang, Jia-Xin Zhan, Shuai Shao, Wei-Hua Bian, Bi-Hui Luo, Dong-Feng Lu, Jian Yang, Chun-Hua Wang, Chun-Xiang Zhang
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 mechanisms involved. Rat VSMCs were seeded at 30% or 90% confluence. MiRNA expression profiles in contact-inhibited confluent VSMCs (90% confluence) and non-contact-inhibited low-density VSMCs (30% confluence) were determined...
April 26, 2018: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/29698388/overview-of-the-anti-inflammatory-effects-pharmacokinetic-properties-and-clinical-efficacies-of-arctigenin-and-arctiin-from-arctium-lappa-l
#20
REVIEW
Qiong Gao, Mengbi Yang, Zhong Zuo
Arctigenin (AR) and its glycoside, arctiin, are two major active ingredients of Arctium lappa L (A lappa), a popular medicinal herb and health supplement frequently used in Asia. In the past several decades, bioactive components from A lappa have attracted the attention of researchers due to their promising therapeutic effects. In the current article, we aimed to provide an overview of the pharmacology of AR and arctiin, focusing on their anti-inflammatory effects, pharmacokinetics properties and clinical efficacies...
April 26, 2018: Acta Pharmacologica Sinica
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