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Piperlongumine

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https://www.readbyqxmd.com/read/29119225/piperlongumine-inhibits-the-proliferation-migration-and-invasion-of-fibroblast-like-synoviocytes-from-patients-with-rheumatoid-arthritis
#1
Siqi Xu, Youjun Xiao, Shan Zeng, Yaoyao Zou, Qian Qiu, Mingcheng Huang, Zhongping Zhan, Liuqin Liang, Xiuyan Yang, Hanshi Xu
OBJECTIVES: Recent studies have indicated that piperlongumine (PLM) may exert anti-inflammatory effects. In the present study, we determined the effect of PLM on the proliferation, apoptosis, migration and invasion of fibroblast-like synoviocytes (FLS) from patients with rheumatoid arthritis (RA) (referred to herein as RA FLS). We further explored the mechanisms by which the studied compound inhibits the functions of RA FLS. METHODS: RA FLS viability and apoptosis were tested using MTT and Annexin V/PI assays, respectively...
November 8, 2017: Inflammation Research: Official Journal of the European Histamine Research Society ... [et Al.]
https://www.readbyqxmd.com/read/29109039/piperlongumine-decreases-cell-proliferation-and-the-expression-of-cell-cycle-associated-proteins-by-inhibiting-akt-pathway-in-human-lung-cancer-cells
#2
Jin Sil Seok, Chang Hee Jeong, Michael C Petriello, Han Geuk Seo, Hyunjin Yoo, Kwonho Hong, Sung Gu Han
Piperlongumine (PL) is an alkaloid of a pepper plant found in Southeast Asia. PL is known to induce selective toxicity towards a variety of cancer cell types. To explore the possible anti-lung cancer effects of PL, A549 cells were treated with PL (0-40 μM) for 24 h. Alterations in the expression of cell cycle-associated proteins (cyclin D1, cyclin-dependent kinase 4 (CDK4), CDK6 and retinoblastoma (Rb)) and intracellular signaling molecules (extracellular signal receptor-activated kinase 1/2 (ERK1/2), Akt, p38 and nuclear factor-κB (NF-κB)) were examined in cells following treatment of PL using Western blot analysis...
November 6, 2017: Food and Chemical Toxicology
https://www.readbyqxmd.com/read/29044986/spectroscopic-investigation-of-the-anticancer-alkaloid-piperlongumine-binding-to-human-serum-albumin-from-the-viewpoint-of-drug-delivery
#3
Yu Liu, Qian-Yu Li, Yu-Ping Wang, Yi-Ming Liu, Bin Liu, Mei-Mei Liu, Bing-Mi Liu
Piperlongumine (PL) is a very promising natural agent with a high potential for cancer treatment. To overcome the poor water solubility of PL, there is a need to develop a novel water-soluble formulation in which PL is non-covalently bound to human serum albumin (HSA). PL binding to HSA was studied by various spectroscopic techniques under simulated physiological conditions. Spectroscopic evidence showed that the interaction of PL with HSA could form a PL-HSA complex. The binding constant (Ka ) values increased with increasing temperature, and a similar dependence was observed for the number of binding sites (n) values...
October 18, 2017: Luminescence: the Journal of Biological and Chemical Luminescence
https://www.readbyqxmd.com/read/29037814/piperlongumine-suppresses-bladder-cancer-invasion-via-inhibiting-epithelial-mesenchymal-transition-and-f-actin-reorganization
#4
Di Liu, Xin Yao Qiu, Xi Wu, Dian Xing Hu, Chun Yang Li, Shang Bin Yu, Feng Pan, Xiao Qian Chen
Piperlongumine (PL), a natural alkaloid isolated from longer pepper plants, is recently found to be a potent selective anti-cancer compound. We first tested its anti-cancer effects on bladder cancer, the fifth most common and aggressive cancer worldwide, to further explore the therapeutic spectrum and molecular mechanisms of PL. PL significantly suppressed bladder cancer cell proliferation, the transition of G2/M phase to next phase, migration/invasion in vitro and bladder cancer growth/development in vivo...
October 14, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28928246/exploiting-mitochondrial-and-oxidative-vulnerabilities-with-a-synthetic-analog-of-pancratistatin-in-combination-with-piperlongumine-for-cancer-therapy
#5
Dennis Ma, Tyler Gilbert, Christopher Pignanelli, Daniel Tarade, Megan Noel, Fadi Mansour, Manika Gupta, Sabrina Ma, Jesse Ropat, Colin Curran, Sergey Vshyvenko, Tomas Hudlicky, Siyaram Pandey
Harsh adverse effects as a result of nonspecific targeting of chemotherapeutics currently pose obstacles in cancer therapy; thus, it would be invaluable to devise novel approaches to specifically target cancer cells. The natural compound pancratistatin (PST) has been shown to preferentially induce apoptosis in a variety of cancer cell types. Recently, several analogs of PST were shown to be efficacious in inducing apoptosis in a variety of aggressive cancer cell types via cancer cell mitochondrial targeting; it caused dissipation of mitochondrial membrane potential and decreased oxygen consumption, and with isolated mitochondria, it induced the release of apoptogenic factors...
September 19, 2017: FASEB Journal: Official Publication of the Federation of American Societies for Experimental Biology
https://www.readbyqxmd.com/read/28913568/piperlongumine-induces-g2-m-phase-arrest-and-apoptosis-in-cholangiocarcinoma-cells-through-the-ros-jnk-erk-signaling-pathway
#6
Sunisa Thongsom, Wipa Suginta, Kyung Jin Lee, Han Choe, Chutima Talabnin
Cholangiocarcinoma (CCA) is an aggressive, metastatic bile duct cancer. CCA is difficult to diagnose, and responds poorly to current radio- and chemo-therapy. Piperlongumine (PL) is a naturally-occurring small molecule selectively toxic to cancer cells by targeting reactive oxygen species (ROS). In this study, we demonstrated the potential anticancer activity of PL in CCA. PL markedly induced death in CCA cell lines in a dose- and time-dependent manner through the activation of caspase-3 and PARP. PL also stimulated ROS accumulation in CCA...
September 14, 2017: Apoptosis: An International Journal on Programmed Cell Death
https://www.readbyqxmd.com/read/28892098/correlation-between-e-cadherin-interactions-survivin-expression-and-apoptosis-in-mdck-and-ts-src-mdck-cell-culture-models
#7
Janne Capra, Sinikka Eskelinen
Survivin, a member of inhibitor of apoptosis (IAP) protein family, is a multifunctional protein expressed in most cancers. In addition to inhibition of apoptosis, it regulates proliferation and promotes migration. Its presence and function in cells is strongly regulated via transcription factors, intracellular localization, and degradation. We analyzed the presence of survivin at protein level in various culture environments and under activation of Src tyrosine kinase in epithelial canine kidney MDCK cells in order to elucidate factors controlling survivin 'lifespan'...
September 11, 2017: Laboratory Investigation; a Journal of Technical Methods and Pathology
https://www.readbyqxmd.com/read/28802122/piperlongumine-b-and-analogs-are-promising-and-selective-inhibitors-for-acetylcholinesterase
#8
Jana Wiemann, Julia Karasch, Anne Loesche, Lucie Heller, Wolfgang Brandt, René Csuk
Piperlongumine B (19), an alkaloid previously isolated from long pepper (Piper longum) has been synthesized for the first time in a short sequence and in good yield together with 19 analogs. Screening of these compounds in Ellman's assays showed several of them to be good inhibitors of acetylcholinesterase while being less active for butyrylcholinesterase. Activity of the compounds increased with the ring size of the heterocycle, and a maximum of activity was observed for an analog holding 12 methylene groups in the aliphatic side chain...
October 20, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28734931/piperlongumine-inhibits-tgf-%C3%AE-induced-epithelial-to-mesenchymal-transition-by-modulating-the-expression-of-e-cadherin-snail1-and-twist1
#9
Min-Ju Park, Da-Eun Lee, Man Kyu Shim, Eun Hyang Jang, Jong Kil Lee, Seo Young Jeong, Jong-Ho Kim
Cancer is a life-threatening disease, and the occurrence of metastasis, which increases the lethality of primary tumors, is increasing. The epithelial-to-mesenchymal transition (EMT) is a biological process by which epithelial cells lose cell-cell adhesion properties and acquire mesenchymal properties, including motility and invasiveness. EMT is considered an early stage of metastasis; therefore, inhibiting EMT may be an effective anticancer therapy. In the present study, the antimetastatic effect of piperlongumine (PL) was assessed in human cancer cells...
July 19, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28686911/synthesis-and-evaluation-of-n-heteroaromatic-ring-based-analogs-of-piperlongumine-as-potent-anticancer-agents
#10
Yu Zou, Chang Yan, Huibin Zhang, Jinyi Xu, Dayong Zhang, Zhangjian Huang, Yihua Zhang
Piperlongumine (PL) selectively targets a wide spectrum of cancer cells and induces their death by triggering various pathways, including apoptosis, necrosis and autophagy. However, the poor solubility is a serious concern for intensive study and clinical application. We synthesized its analogs 1-9 by replacement of the trimethoxyphenyl of PL with an N-heteroaromatic ring and/or not introduction of 2-Cl. These compounds improved aqueous solubility and displayed potent anticancer activity. The most active compound 9 selectively enhanced ROS levels in colon cancer cells and inhibited the cell proliferation but sparing non-tumor colon cells...
September 29, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28673967/piperlongumine-induces-reactive-oxygen-species-ros-dependent-downregulation-of-specificity-protein-transcription-factors
#11
Keshav Karki, Erik Hedrick, Ravi Kasiappan, Un-Ho Jin, Stephen Safe
Piperlongumine is a natural product found in the plant species Piper longum, and this compound exhibits potent anticancer activity in multiple tumor types and has been characterized as an inducer of reactive oxygen species (ROS). Treatment of Panc1 and L3.6pL pancreatic, A549 lung, 786-O kidney, and SKBR3 breast cancer cell lines with 5 to 15 μmol/L piperlongumine inhibited cell proliferation and induced apoptosis and ROS, and these responses were attenuated after cotreatment with the antioxidant glutathione...
August 2017: Cancer Prevention Research
https://www.readbyqxmd.com/read/28552690/coloaded-nanoparticles-of-paclitaxel-and-piperlongumine-for-enhancing-synergistic-antitumor-activities-and-reducing-toxicity
#12
Qi Liu, Di Zhao, Xiaojie Zhu, Huili Chen, Yue Yang, Jiaqiu Xu, Qing Zhang, Ali Fan, Ning Li, Chaorui Guo, Ying Kong, Yang Lu, Xijing Chen
The purpose of this study was to develop a nanocarrier system for codelivery of paclitaxel (PTX) and piperlongumine (PL) and investigate the therapeutic potential of improving efficacy and reducing toxicity. PTX and PL were formulated into poly lactic-co-glycolic acid and D-α-tocopheryl polyethylene glycol succinate via organic solvent evaporation method. The average diameter was 117.1 ± 1.9 nm, and the zeta potential was -43.25 ± 2.76 mV. PL facilitated the cellular uptake of PTX, and the increased cytotoxicity was similarly displayed...
May 26, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28538206/spectroscopic-far-or-terahertz-mid-infrared-and-raman-investigation-thermal-analysis-and-biological-activity-of-piplartine
#13
Anubha Srivastava, T Karthick, B D Joshi, Rashmi Mishra, Poonam Tandon, A P Ayala, Javier Ellena
Research in the field of medicinal plants including Piper species like long pepper (Piper longum L.- Piperaceae) is increasing all over the world due to its use in traditional and Ayurvedic medicine. Piplartine (piperlongumine, 5,6-dihydro-1-[(2E)-1-oxo-3-(3,4,5-trimethoxyphenyl)-2-propenyl]-2(1H)-pyridinone), a biologically active alkaloid/amide was isolated from the phytochemical investigations of Piper species, as long pepper. This alkaloid has cytotoxic, anti-fungal, anti-diabetic, anti-platelet aggregation, anti-tumoral, anxiolytic, anti-depressant, anti-leishmanial, and genotoxic activities, but, its anticancer property is the most promising and has been widely explored...
May 5, 2017: Spectrochimica Acta. Part A, Molecular and Biomolecular Spectroscopy
https://www.readbyqxmd.com/read/28439094/selective-targeting-of-cancer-cells-by-oxidative-vulnerabilities-with-novel-curcumin-analogs
#14
Christopher Pignanelli, Dennis Ma, Megan Noel, Jesse Ropat, Fadi Mansour, Colin Curran, Simon Pupulin, Kristen Larocque, Jianzhang Wu, Guang Liang, Yi Wang, Siyaram Pandey
Recently, research has focused on targeting the oxidative and metabolic vulnerabilities in cancer cells. Natural compounds like curcumin that target such susceptibilities have failed further clinical advancements due to the poor stability and bioavailability as well as the need of high effective doses. We have synthesized and evaluated the anti-cancer activity of several monocarbonyl analogs of curcumin. Interestingly, two novel analogs (Compound A and I) in comparison to curcumin, have increased chemical stability and have greater anti-cancer activity in a variety of human cancer cells, including triple-negative, inflammatory breast cancer cells...
April 24, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28434764/novel-non-trimethoxylphenyl-piperlongumine-derivatives-selectively-kill-cancer-cells
#15
Youjun Zhang, Hao Ma, Yuelin Wu, Zhongli Wu, Zhengguang Yao, Wannian Zhang, Chunlin Zhuang, Zhenyuan Miao
Piperlongumine (PL) is a natural alkaloid with broad biological activities. Twelve analogues have been designed and synthesized with non-substituted benzyl rings or heterocycles in this work. Most of the compounds showed better anticancer activities than the parent PL without apparent toxicity in normal cells. Elevation of cellular ROS levels was one of the main anticancer mechanisms of these compounds. Cell apoptosis and cell cycle arrest for the best compound ZM90 were evaluated and similar mechanism of action with PL was demonstrated...
June 1, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28377224/piperlongumine-downregulates-the-expression-of-her-family-in-breast-cancer-cells
#16
Hyeon-Ok Jin, Jin-Ah Park, Hyun-Ah Kim, Yoon Hwan Chang, Young Jun Hong, In-Chul Park, Jin Kyung Lee
HER family receptors are frequently deregulated in breast cancer and the deregulation of these receptors is associated with poor prognosis. Thus, these receptors are considered therapeutic targets. In the present study, we found that piperlongumine (PL) downregulates the expression of HER family receptors HER1, HER2, and HER3 in breast cancer cells. Downregulation of these receptors by PL is mediated through the generation of reactive oxygen species (ROS), as N-acetyl-cysteine blocks it. Interestingly, the HER2-overexpressing cell lines BT474 and SkBr3 are somewhat more sensitive to PL than the low HER2-expressing cell line MCF7...
May 13, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28273655/new-agents-that-target-senescent-cells-the-flavone-fisetin-and-the-bcl-xl-inhibitors-a1331852-and-a1155463
#17
Yi Zhu, Ewald J Doornebal, Tamar Pirtskhalava, Nino Giorgadze, Mark Wentworth, Heike Fuhrmann-Stroissnigg, Laura J Niedernhofer, Paul D Robbins, Tamara Tchkonia, James L Kirkland
Senescent cells accumulate with aging and at sites of pathology in multiple chronic diseases. Senolytics are drugs that selectively promote apoptosis of senescent cells by temporarily disabling the pro-survival pathways that enable senescent cells to resist the pro-apoptotic, pro-inflammatory factors that they themselves secrete. Reducing senescent cell burden by genetic approaches or by administering senolytics delays or alleviates multiple age- and disease-related adverse phenotypes in preclinical models...
March 8, 2017: Aging
https://www.readbyqxmd.com/read/28159415/identification-of-novel-ros-inducer-by-merging-the-fragments-of-piperlongumine-and-dicoumarol
#18
Xiaojuan Xu, Xia Fang, Jun Wang, Hong Zhu
A series of novel ROS inducers were designed by merging the fragments of piperlongumine and dicoumarol. Most of these derivatives showed potent in vitro activity against three cancer cell lines and good selectivity towards normal lung cells. The most potent and selective compound 3e was proven to exhibit obvious ROS elevation and excellent in vivo antitumor activity with suppressed tumor growth by 48.46% at the dose of 5mg/kg. Supported by these investigation, these findings encourage further investigation around this interesting antitumor chemotype...
March 1, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28011150/piperlongumine-attenuates-experimental-autoimmune-encephalomyelitis-through-inhibition-of-nf-kappab-activity
#19
Sun Mi Gu, Jaesuk Yun, Dong Ju Son, Hoi Yeong Kim, Kyung Tak Nam, Hae Deun Kim, Min Gi Choi, Jeong Soon Choi, Young Min Kim, Sang-Bae Han, Jin Tae Hong
Multiple sclerosis (MS) is a chronic, autoimmune and neurodegenerative disease in which demyelination sporadically and repeatedly occurs in the central nervous system (CNS). The activity of nuclear factor kappa B (NF-κB), a family of transcription factors, was increased in the cerebrospinal fluid (CSF) and/or the serum and brain and/or spinal cord of MS patients than in a healthy donors. In our study, we investigated whether piperlongumine (PL), which is known to have inhibitory effect on activity of NF-κB, can alleviate an experimental autoimmune encephalomyelitis (EAE)...
December 21, 2016: Free Radical Biology & Medicine
https://www.readbyqxmd.com/read/27987486/piperlongumine-derived-cyclic-sulfonamides-sultams-synthesis-and-in%C3%A2-vitro-exploration-for-therapeutic-potential-against-hela-cancer-cell-lines
#20
Nitin P Lad, Sarang Kulkarni, Rajiv Sharma, Malcolm Mascarenhas, Mahesh R Kulkarni, Shivaji S Pandit
A novel modification of piperlongumine is designed, bearing a cyclic sulphonamide (sultam) and its synthesis is described. For the first time herein we report the synthesis and biological evaluation of the natural product derived cyclic sulfonamides using Grubbs second generation catalyst (Grubbs II) via ring closing metathesis approach. Synthesis of a series of piperlongumine derived sultams is done in a moderate to good yield using Wittig reaction, Ring-Closing Metathesis (RCM) and, amide synthesis by using mixed anhydride, approach...
January 27, 2017: European Journal of Medicinal Chemistry
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