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Ldh a inhibitors

Xiao-Yan Huang, Yu-Guang Wang, Yi Wang, Yue Gao
This study aimed to investigate the effect and mechanism of ophiopogonin D (OP-D) on Ang Ⅱ-induced HUVECs apoptosis, in order to provide a reliable basis for the safety and efficacy of traditional Chinese medicines. The effect of Ang Ⅱ on survival and total proteins content of HUVECs were measured by MTT and Western blotting. The effect of OP-D on Ang Ⅱ-induced lactate dehydrogenase (LDH) release rate in HUVECs was measured by enzyme standard instrument. The effects of OP-D and 11,12-EET on phosphorylation of JNK/c-Jun induced by Ang Ⅱ were measured by Western blot and RT-PCR with the help of JNK specific inhibitor SP600125 and CYP450 isozymes selective inhibitor 6-(2-propargyloxyphenyl) hexanoic acid (PPOH)...
January 2018: Zhongguo Zhong Yao za Zhi, Zhongguo Zhongyao Zazhi, China Journal of Chinese Materia Medica
Doreen Baumann, Helen Salia, Lilo Greune, Stephanie Norkowski, Britta Körner, Zina M Uckeley, Gad Frankel, Marianne Guenot, Christian Rüter, M Alexander Schmidt
Enteropathogenic Escherichia coli (EPEC) subvert host cell signaling pathways by injecting effector proteins via a Type 3 Secretion System (T3SS). The T3SS-dependent EspB protein is a multi-functional effector protein, which contributes to adherence and translocator pore formation and after injection exhibits several intracellular activities. In addition, EspB is also secreted into the environment. Effects of secreted EspB have not been reported thus far. As a surrogate for secreted EspB we employed recombinant EspB (rEspB) derived from the prototype EPEC strain E2348/69 and investigated the interactions of the purified protein with different human epithelial and immune cells including monocytic THP-1 cells, macrophages, dendritic cells, U-937, epithelial T84, Caco-2, and HeLa cells...
March 12, 2018: International Journal of Medical Microbiology: IJMM
Cheng Zeng, Wen Jiang, Ruifang Zheng, Chenghui He, Jianguang Li, Jianguo Xing
Our previous research demonstrated that tilianin protects the myocardium in a myocardial ischemia reperfusion injury (MIRI) rat model and has prominent pharmacological potential as a cardiovascular drug. Our study aimed to investigate the molecular signaling implicated in the improvement of myocardial survival induced by tilianin, a flavonoid antioxidant. Tilianin (2.5, 5, and 10 mg/kg/d) or saline was orally administered to rats for 14 days. On the 15th day, ischemia was induced by ligating the left anterior descending artery for 45 min, followed by 4 h of reperfusion...
2018: PloS One
Yong Liang, Jing Xu, Yu Wang, Jia-Yu Tang, Song-Lin Yang, Hong-Guang Xiang, Shi-Xing Wu, Xiao-Juan Li
BACKGROUND/AIMS: Cerebral ischemia-reperfusion (I/R) injury involves multiple independently fatal terminal pathways. CK2α/NADPH oxidase is an important signaling pathway associated with ischemia-reperfusion injury, and miR-125b can regulate oxidative stress-related injury. In this study, we investigated whether the effect of miR-125b in rat brain I/R injury occurs through its modulation of the CK2α/NADPH oxidase pathway. METHODS: Rats were subjected to 2 h of cerebral ischemia followed by 24 h of reperfusion to establish an I/R injury model...
February 28, 2018: Cellular Physiology and Biochemistry
Xinrui Yuan, Yineng Xia, Peng Lu, Lijuan Zhu, Yuejiao Zhong, Yubin Wang
Excess lipid accumulation in the arterial intima and formation of macrophage-derived foam cells in the plaque could cause atherosclerotic lesion. Cholesterol absorption inhibitors could suppress the lipid accumulation of human macrophage, inflammatory response and the development of atherosclerosis. In this research, a series of 1H-pyrrole-2,5-dione derivatives were synthesized as cholesterol absorption inhibitor and tested in in vitro experiments. One of the most active inhibitors, compound 20 exhibited stronger in vitro cholesterol absorption activity than ezetimibe, no cytotoxicity in HEK293 and RAW264...
August 30, 2017: Bioorganic & Medicinal Chemistry
Hai-Jing Zhang, Rong-Chang Chen, Gui-Bo Sun, Long-Po Yang, Yin-di Zhu, Xu-Dong Xu, Xiao-Bo Sun
BACKGROUND: Clinopodium chinense (Benth.) O. Ktze is a traditional Chinese herbal medicine, which comprises the plant's total flavonoids. TFCC plays an important role in the treatment of cardiovascular disease. PURPOSE: The aim of the study was to study the protective effects and possible mechanism of TFCC against isoproterenol (ISO)-mediated myocardial injury in vivo and anoxia/reoxygenation (A/R)-induced H9c2 cell injury in vitro. METHODS: Male Sprague-Dawley (SD) rats were intragastrically pretreated with TFCC for 15 days...
February 1, 2018: Phytomedicine: International Journal of Phytotherapy and Phytopharmacology
Hadjer Saidi, Julie Bérubé, Fatima Laraba-Djebari, Djelila Hammoudi-Triki
Androctonus australis hector (Aah) scorpion venom is well known to induce a systemic inflammatory response associated with cell infiltration in lung and edema formation. The present study investigate (i) in vivo the evolution of lung and systemic inflammation triggered by Aah venom and (ii) analyze in vitro the signaling cascade, upstream of inflammatory cytokine expression after Aah venom-stimulated mouse alveolar macrophage (MH-S), the main resident immune cells in the lung. The inflammation induced by Aah venom was assessed in mice through inflammatory cell count, nitric oxide metabolite, and lactate dehydrogenase (LDH) activity in blood, concordantly with neutrophil sequestration in tissue and lung histology...
February 28, 2018: Inflammation
Li Cong, Shuting Yang, Yong Zhang, Jianguo Cao, Xiaohua Fu
7‑difluoromethoxy‑5,4'‑dimethoxy‑genistein (DFMG) is a novel active chemical entity, which modulates the function and signal transduction of endothelial cells and macrophages (MPs), and is essential in the prevention of atherosclerosis. In the present study, the activity and molecular mechanism of DFMG on MPs was investigated using a Transwell assay to construct a non‑contact co‑culture model. Human umbilical vein endothelial cells (HUVE‑12), which were incubated with lysophosphatidylcholine (LPC), were seeded in the upper chambers, whereas PMA‑induced MPs were grown in the lower chambers...
February 23, 2018: International Journal of Molecular Medicine
Hiroyuki Ariyasu, Hidefumi Inaba, Takayuki Ota, Hiroyuki Yamaoka, Yasushi Furukawa, Hiroshi Iwakura, Naotaka Doi, Yuki Yamamoto, Takashi Akamizu
BACKGROUND: Immune-checkpoint inhibitors (ICIs) are novel promising agents for the treatment of malignant tumors. However, critical endocrine immune-related adverse events (irAEs) by ICIs often occur. CASE REPORT: A 63-year-old woman with advanced malignant melanoma had received anti-PD-1 antibody (nivolumab, 2 mg/kg every 3 weeks) for 8 cycles (from day 0 to day 147). On day 168, nivolumab was switched to anti-CTLA-4 antibody (ipilimumab, 3mg/kg every 3 weeks)...
March 2018: In Vivo
Nádia Weber Dimer, Bruna Klippel Ferreira, Jotele Fontana Agostini, Maria Luiza Gomes, Luiza Wilges Kist, Fernanda Malgarin, Milena Carvalho-Silva, Lara Mezari Gomes, Joyce Rebelo, Marisa Jádna Silva Frederico, Fátima Regina Mena Barreto Silva, Eduardo Pacheco Rico, Mauricio Reis Bogo, Emilio Luiz Streck, Gustavo Costa Ferreira, Patrícia Fernanda Schuck
Phenylketonuria (PKU) is a disorder of phenylalanine (Phe) metabolism caused by deficient phenylalanine hydroxylase activity. The deficiency results in increased levels of Phe and its metabolites in fluids and tissues of patients. PKU patients present neurological signals and symptoms including hypomyelination and intellectual deficit. This study assessed brain bioenergetics at 1 h after acute Phe administration to induce hyperphenylalaninemia (HPA) in rats. Wistar rats were randomized in two groups: HPA animals received a single subcutaneous administration of Phe (5...
February 14, 2018: Neurochemistry International
Riyoko Tamai, Yusuke Kiyoura
Alendronate (ALN) is a nitrogen-containing bisphosphonate (NBP) that inhibits bone resorption. NBPs have inflammatory side effects, and ALN augments bacteria-induced interleukin (IL)-1β production. The present study aimed to examine whether ALN induces pyroptosis, a form of cell death associated with IL-1β release, in macrophage-like J774.1 cells incubated with lipid A, a component of gram-negative bacteria. Pretreatment of J774.1 cells with ALN increased lipid A-induced IL-1β production and cell death, but not IL-6 and TNF-α production...
February 10, 2018: Life Sciences
Fangming Zhang, Max Brenner, Weng-Lang Yang, Ping Wang
Cold-inducible RNA-binding protein (CIRP) is a novel sepsis inflammatory mediator and C23 is a putative CIRP competitive inhibitor. Therefore, we hypothesized that C23 can ameliorate sepsis-associated injury to the lungs and kidneys. First, we confirmed that C23 dose-dependently inhibited TNF-α release, IκBα degradation, and NF-κB nuclear translocation in macrophages stimulated with CIRP. Next, we observed that male C57BL/6 mice treated with C23 (8 mg/kg BW) at 2 h after cecal ligation and puncture (CLP) had lower serum levels of LDH, ALT, IL-6, TNF-α, and IL-1β (reduced by ≥39%) at 20 h after CLP compared with mice treated with vehicle...
February 12, 2018: Scientific Reports
Muhammad Zubair Afzal, Rodwell Mabaera, Keisuke Shirai
BACKGROUND: Uveal melanoma accounts for 85% of the ocular melanomas and has an increased risk of hematogenous spread, most commonly to the liver. After curative intent therapy like surgery and radiation, fifty percent of patients present with distant metastasis. Metastatic uveal melanoma (MUM) does not harbor typically targetable mutations, e.g., BRAF as in cutaneous melanoma. As a result, there is no proven therapy for MUM. Various chemotherapy and immunotherapy regimens have been tried and only partial response (PR) is the best that has been achieved in most of the cases...
February 12, 2018: Journal for Immunotherapy of Cancer
Baiping Ren, Yonglan Liu, Yanxian Zhang, Yongqing Cai, Xiong Gong, Yung Chang, Lijian Xu, Jie Zheng
Abnormal misfolding and aggregation of amyloid peptides into amyloid fibrils are a common and critical pathological event in many neurodegenerative diseases. Most of inhibitors or drugs have been developed to prevent amyloid aggregation of a specific peptide, exhibiting sequence-dependent inhibition mechanisms. It is more challenging to develop or discover inhibitors capable of preventing the aggregation of two or more different amyloid peptides. Genistein, a major phytoestrogen in soybean, has been widely used as anti-inflammation and cerebrovascular drugs due to their anti-oxidation and anti-acetylcholinesterase effects...
February 12, 2018: ACS Chemical Neuroscience
Xianxian Wu, Haiying Zhang, Wei Qi, Ying Zhang, Jiamin Li, Zhange Li, Yuan Lin, Xue Bai, Xin Liu, Xiaohui Chen, Huan Yang, Chaoqian Xu, Yong Zhang, Baofeng Yang
Cigarette smoking is a major risk factor for atherosclerosis and other cardiovascular diseases. Increasing evidence has demonstrated that nicotine impairs the cardiovascular system by targeting vascular endothelial cells, but the underlying mechanisms remain obscure. It is known that cell death and inflammation are crucial processes leading to atherosclerosis. We proposed that pyroptosis may be implicated in nicotine-induced atherosclerosis and therefore conducted the present study. We found that nicotine resulted in larger atherosclerotic plaques and secretion of inflammatory cytokines in ApoE-/- mice fed with a high-fat diet (HFD)...
February 7, 2018: Cell Death & Disease
Mitsuhiro Abe, Kenji Tsushima, Jun Ikari, Naoko Kawata, Jiro Terada, Nobuhiro Tanabe, Koichiro Tatsumi
BACKGROUND: Everolimus (ERL), a mammalian target of rapamycin (mTOR) inhibitor, has been used for the management of several advanced cancers. ERL frequently causes lung injury, although the clinical and radiographic features have not been clarified. The aim of this study was to assess the clinical features of ERL-induced lung injury and determine the associated risk factors. METHODS: This single-center, retrospective study included 45 patients (29 men, 16 women; age, 12-78 years) who had received ERL at our hospital between August 2010 and March 2016...
January 2018: Respiratory Medicine
Beibei Wu, Lexiang Yu, Pingdong Hu, Yang Lu, Juan Li, Yan Wei, Rongqiao He
d-ribose (Rib), a reactive glycation compound that exists in organisms, abnormally increases in the urine of diabetic patients and can yield large amounts of advanced glycation end products (AGEs), leading to cell dysfunction. However, whether cellular proteins are sensitive to this type of glycation is unknown. In this study, we found that cellular AGEs accumulate in Chinese hamster ovary (CHO) cells with increased Rib concentration and administration time. Mass spectrum analysis of isolated AGE-modified proteins from cell lysates showed that glucose-regulated protein 78 kD (GRP78) is one of the main ribosylated proteins...
February 1, 2018: Biochimica et Biophysica Acta
Lei Cao, Yu Zhang, Shuai Zhang, Tian-Peng Jiang, Li Chen, Jing Liu, Shi Zhou
Cerebral ischemic injury causes severe brain damage and remains one of the leading causes of morbidity and mortality worldwide. Members of the microRNA-29 (miR-29) family are involved in regulating the process of ischemia and may be developed as biomarkers to diagnose and treat cerebral ischemia. The role of miR-29b in cerebral ischemia injury remains poorly understood. The purpose of the present study was to investigate whether miR-29b overexpression suppressed cerebral ischemic injury and to explore its underlying mechanism of action...
January 2018: Experimental and Therapeutic Medicine
B M Lang, A Peveling-Oberhag, D Faidt, A M Hötker, V Weyer-Elberich, S Grabbe, C Loquai
Despite new therapeutic options, metastatic melanoma remains to be one of the most fatal tumors. With the development of BRAF inhibitors and immune checkpoint inhibitors, overall survival could be prolonged significantly for the first time. Clinical studies implied that even long-term survival is possible with both types of drugs, but predictive markers are so far missing. In this study, we analyzed survival data from patients that received the first-in-class substances vemurafenib and ipilimumab, respectively, during the time period from registration of the drugs until availability of combination treatments...
January 31, 2018: Medical Oncology
Xiaofang Zhao, Guosong Luo, Ying Cheng, Wenjing Yu, Run Chen, Bin Xiao, Yuancai Xiang, Chunhong Feng, Wenguang Fu, Chunyan Duan, Fuli Yao, Xianming Xia, Qinghua Tao, Mei Wei, Rongyang Dai
Compound C, a well-known inhibitor of AMP-activated protein kinase (AMPK), has been reported to exert antitumor activities in some types of cells. Whether compound C can exert antitumor effects in human cholangiocarcinoma (CCA) remains unknown. Here, we demonstrated that compound C is a potent inducer of cell death and autophagy in human CCA cells. Autophagy inhibitors increased the cytotoxicity of compound C towards human CCA cells, as confirmed by increased LDH release and PARP cleavage. It is notable that compound C treatment increased phosphorylated Akt, sustained high levels of phosphorylated p70S6K and decreased mTOR regulated p-ULK1 (ser757)...
January 31, 2018: Journal of Cellular Biochemistry
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