The role of small molecule Flt3 receptor protein-tyrosine kinase inhibitors in the treatment of Flt3-positive acute myelogenous leukemias
Publication date: Available online 25 February 2020Source: Pharmacological ResearchAuthor(s): Robert Roskoski (Source: Pharmacological Research)
Source: Pharmacological Research - February 27, 2020 Category: Drugs & Pharmacology Source Type: research

Telomerase: key regulator of inflammation and cancer
Publication date: Available online 25 February 2020Source: Pharmacological ResearchAuthor(s): Lele Wu, Kerem Fidan, Jae-Young Um, Kwang Seok Ahn (Source: Pharmacological Research)
Source: Pharmacological Research - February 27, 2020 Category: Drugs & Pharmacology Source Type: research

The diverse functions of Siglec-15 in bone remodeling and antitumor responses
Publication date: Available online 26 February 2020Source: Pharmacological ResearchAuthor(s): Fu-biao Kang, Wei Chen, Ling Wang, Ying-ze Zhang (Source: Pharmacological Research)
Source: Pharmacological Research - February 27, 2020 Category: Drugs & Pharmacology Source Type: research

Anti-diabetic potential of plant alkaloids: Revisiting current findings and future perspectives
Publication date: Available online 24 February 2020Source: Pharmacological ResearchAuthor(s): Hassan Rasouli, Reza Yarani, Flemming Pociot, Jelena Popović-Djordjević (Source: Pharmacological Research)
Source: Pharmacological Research - February 25, 2020 Category: Drugs & Pharmacology Source Type: research

Urinary bladder sigma-1 receptors: A new target for cystitis treatment
Publication date: Available online 24 February 2020Source: Pharmacological ResearchAuthor(s): Rafael González-Cano, Antonia Artacho-Cordón, Lucía Romero, Miguel A. Tejada, Francisco R. Nieto, Manuel Merlos, Francisco J. Cañizares, Cruz M. Cendán, Eduardo Fernández-Segura, José M. Baeyens (Source: Pharmacological Research)
Source: Pharmacological Research - February 25, 2020 Category: Drugs & Pharmacology Source Type: research

Berberine Pharmacology and the Gut Microbiota: A Hidden Therapeutic Link
Publication date: Available online 24 February 2020Source: Pharmacological ResearchAuthor(s): Solomon Habtemariam (Source: Pharmacological Research)
Source: Pharmacological Research - February 25, 2020 Category: Drugs & Pharmacology Source Type: research

Arctigenin, a novel TMEM16A inhibitor for lung adenocarcinoma therapy
Publication date: Available online 22 February 2020Source: Pharmacological ResearchAuthor(s): Shuai Guo, Yafei Chen, Sai Shi, Xuzhao Wang, Hailin Zhang, Yong Zhan, Hailong AnAbstractTMEM16A plays critical roles in physiological process and may serve as drug targets for diverse diseases. In recently, it has started to be regarded as potential primary lung adenocarcinoma targets. Here, we identified that arctigenin, a natural compound, is a novel TMEM16A inhibitor, and it can suppress lung adenocarcinoma growth through inhibiting TMEM16A both in vitro and in vivo. Our data also showed that the IC50 of actigenin to TMEM16A wh...
Source: Pharmacological Research - February 24, 2020 Category: Drugs & Pharmacology Source Type: research

Oral administration of protein nanoparticles: An emerging route to disease treatment
Publication date: Available online 22 February 2020Source: Pharmacological ResearchAuthor(s): Samira Sadeghi, Wai Kit Lee, Shik Nie Kong, Annanya Shetty, Chester Lee DrumAbstractOver the last two decades, developments in nanomedicine have resulted in technical advances with application to clinical science. Both organic and inorganic nanoparticles (NPs) have shown tolerability, pharmacologic specificity and biodegradability. A subclass of NPs, protein NPs, have garnered recent attention due to the inherent biocompatibility of protein substrates. Protein NPs are currently being employed widely in pharmaceuticals development ...
Source: Pharmacological Research - February 24, 2020 Category: Drugs & Pharmacology Source Type: research

S1PR2 inhibitors potently reverse 5-FU resistance by downregulating DPD expression in colorectal cancer
This study provides novel insights that S1PR2 inhibitors could sensitize 5-FU therapy in colorectal cancer.Graphical abstract (Source: Pharmacological Research)
Source: Pharmacological Research - February 22, 2020 Category: Drugs & Pharmacology Source Type: research

Intercellular crosstalk of hepatic stellate cells in liver fibrosis: new insights into therapy
Publication date: Available online 21 February 2020Source: Pharmacological ResearchAuthor(s): Xuanyan Cai, Jiajia Wang, Jincheng Wang, Qian Zhou, Bo Yang, Qiaojun He, Qinjie WengAbstractLiver fibrosis is a dynamic wound-healing process characterized by the net accumulation of extracellular matrix. There is no efficient antifibrotic therapy other than liver transplantation to date. Activated hepatic stellate cells (HSCs) are the major cellular source of matrix-producing myofibroblasts, playing a central role in the initiation and progression of liver fibrosis. Paracrine signals from resident and inflammatory cells such as h...
Source: Pharmacological Research - February 22, 2020 Category: Drugs & Pharmacology Source Type: research

Kinin B1 Receptor: A Target for Neuroinflammation in Hypertension
Publication date: Available online 19 February 2020Source: Pharmacological ResearchAuthor(s): Srinivas SriramulaAbstractKinins are a family of oligopeptides of the kallikrein-kinin system that act as potent vasoactive hormones and inflammatory mediators. The bioactive kinins mainly consist of bradykinin and kallidin, and their metabolites des-Arg9-bradykinin and des-Arg10-kallidin. Physiological effects of kinins are mediated by activation of highly selective G-protein coupled kinin B1 and B2 receptors. Growing evidence suggests that B1 receptor activation mediates diverse physiological and pathological features of cardiov...
Source: Pharmacological Research - February 20, 2020 Category: Drugs & Pharmacology Source Type: research

Statin therapy in athletes and patients performing regular intense exercise – Position Paper from the International Lipid Expert Panel (ILEP)
Publication date: Available online 19 February 2020Source: Pharmacological ResearchAuthor(s): Niki Katsiki, Dimitri P. Mikhailidis, Gani Bajraktari, Andre R. Miserez, Arrigo F.G. Cicero, Eric Bruckert, Maria-Corina Serban, Erkin Mirrakhimov, Fahad Alnouri, Željko Reiner, György Paragh, Amirhossein Sahebkar, Maciej Banach, on behalf of the International Lipid Expert Panel (ILEP) (Source: Pharmacological Research)
Source: Pharmacological Research - February 20, 2020 Category: Drugs & Pharmacology Source Type: research

TRAIL in oncology: From recombinant TRAIL to nano- and self-targeted TRAIL-based therapies
Publication date: Available online 18 February 2020Source: Pharmacological ResearchAuthor(s): Hassan Dianat-Moghadam, Maryam Heidarifard, Amir Mahari, Mehdi Shahgolzari, Mohsen Keshavarz, Mohammad Nouri, Zohreh AmoozgarAbstractTNF-related apoptosis-inducing ligand (TRAIL) selectively induces the apoptosis pathway in tumor cells leading to tumor cell death. Because TRAIL induction can kill tumor cells, cancer researchers have developed many agents to target TRAIL and some of these agents have entered clinical trials in oncology. Unfortunately, these trials have failed for many reasons, including drug resistance, off-target ...
Source: Pharmacological Research - February 19, 2020 Category: Drugs & Pharmacology Source Type: research

MicroRNA-27a-3p aggravates renal ischemia/reperfusion injury by promoting oxidative stress via targeting growth factor receptor-bound protein 2
Publication date: Available online 19 February 2020Source: Pharmacological ResearchAuthor(s): X.-R. Zhao, Z. Zhang, M. Gao, L. Li, P.-Y. Sun, L.-N. Xu, Y. Qi, L.-H. Yin, J.-Y. PengAbstractRenal ischemia-reperfusion (RI/R) injury with high morbidity and mortality is one common clinical disease. Development of drug targets to treat the disorder is critical important. MiR-27a-3p plays important roles in regulating oxidative stress. However, its effects on RI/R injury have not been reported. In this paper, hypoxia/reoxygenation (H/R) models on NRK-52E and HK-2 cells, and RI/R model in C57BL/6 mice were established. The results...
Source: Pharmacological Research - February 19, 2020 Category: Drugs & Pharmacology Source Type: research

Natural Killer Cells as a Double-edged Sword in Cancer Immunotherapy: A Comprehensive Review from Cytokine Therapy to Adoptive Cell Immunotherapy
Publication date: Available online 15 February 2020Source: Pharmacological ResearchAuthor(s): Yuanlin Wu, Jing Li, Parham Jabbarzadeh Kaboli, Jing Shen, Xu Wu, Yueshui Zhao, Huijiao Ji, Fukuan Du, Yejiang Zhou, Yongzhou Wang, Hanyu Zhang, Jianhua Yin, Qinglian Wen, Chi Hin Cho, Mingxing Li, Zhangang XiaoAbstractNatural killer (NK) cells are immune cells which are able to kill tumor and virus-infected cells and play an important role in both innate immunity and acquired immunity. Tumor immunotherapy is an emerging model of tumor treatment in the clinic. It is a re-emerging type of anticancer immunotherapy with the purpose o...
Source: Pharmacological Research - February 16, 2020 Category: Drugs & Pharmacology Source Type: research

Etiology of atherosclerosis informs choice of animal models and tissues for initial functional genomic studies of resveratrol
Publication date: Available online 14 February 2020Source: Pharmacological ResearchAuthor(s): Lukasz Huminiecki, Atanas G. Atanasov, Jarosław HorbańczukAbstractResveratrol, a phytoalexin, is a natural polyphenol synthesized exclusively by plants in response to environmental stresses. However, the molecule has also many exogenous bioactivities in animal cells. These bioactivities may lead to anti-cancer and cardio-protective health benefits. Because cellular responses to the treatment with resveratrol include the changes of expression patterns, functional genomics is an attractive tool to study them. In recent and today&r...
Source: Pharmacological Research - February 15, 2020 Category: Drugs & Pharmacology Source Type: research

Epigenetic histone modulations of PPARγ and related pathways contribute to olanzapine-induced metabolic disorders
This study aimed to investigate epigenetic modulations of the hepatic PPARγ pathway in olanzapine-induced lipid dysfunctions. Olanzapine led to significant increases of body weight gain, white adipose tissue, fasting triglyceride, and fat accumulation in the liver. A significant upregulation of PPARγ was observed in olanzapine-treated rats. ChIP-deep sequencing showed the increase of H3K4me2 binding on the whole gene loci of key regulators of adipogenesis and lipogenesis, the Pparg, Srebp-1, Cebps families (Cebpa, Cebpb and Cebpd), the Signal transducer and activator of transcription 5 families (Stat5a and Stat...
Source: Pharmacological Research - February 15, 2020 Category: Drugs & Pharmacology Source Type: research

A unique cdk4/6 inhibitor: current and future therapeutic strategies of abemaciclib
Publication date: Available online 14 February 2020Source: Pharmacological ResearchAuthor(s): Qing-Yun Chong, Ze-Hui Kok, Ngoc-Linh-Chi Bui, Xiaoqiang Xiang, Andrea Li-Ann Wong, Wei Peng Yong, Gautam Sethi, Peter E. Lobie, Lingzhi Wang, Boon-Cher GohAbstractCell cycle dysregulation, characterised by aberrant activation of cyclin dependent kinases (CDKs), is a hallmark of cancer. After years of research on the first and second generations of less selective CDK inhibitors with unfavourable clinical activity and toxicity profiles, CDK4/6 inhibitors become the first and only class of highly specific CDK inhibitors being approv...
Source: Pharmacological Research - February 15, 2020 Category: Drugs & Pharmacology Source Type: research

Endoplasmic reticulum stress signaling in cancer and neurodegenerative disorders: tools and strategies to understand its complexity
Publication date: Available online 14 February 2020Source: Pharmacological ResearchAuthor(s): Daniela Correia da Silva, Patrícia Valentão, Paula B. Andrade, David M. PereiraAbstractThe endoplasmic reticulum (ER) comprises a network of tubules and vesicles that constitutes the largest organelle of the eukaryotic cell. Being the location where most proteins are synthesized and folded, it is crucial for the upkeep of cellular homeostasis.Disturbed ER homeostasis triggers the activation of a conserved molecular machinery, termed the unfolded protein response (UPR), that comprises three major signaling branches, i...
Source: Pharmacological Research - February 15, 2020 Category: Drugs & Pharmacology Source Type: research

Pre-Eclampsia: microbiota possibly playing a role
Publication date: Available online 15 February 2020Source: Pharmacological ResearchAuthor(s): Elham Ahmadian, Yalda Rahbar Saadat, Seyed Mahdi Hosseiniyan Khatibi, Nariman-Saleh-Fam Ziba, Bastami Milad, Vahed Fatemeh Zununi, Ardalan Mohammadreza, Vahed Sepideh ZununiAbstractPre-eclampsia (PE) is a complication of pregnancy that is associated with mortality and morbidity in mothers and fetuses worldwide. Oxygen dysregulation in the placenta, abnormal remodeling of the spiral artery, defective placentation, oxidative stress at the fetal-maternal border, inflammation and angiogenic impairment in the maternal circulation are t...
Source: Pharmacological Research - February 15, 2020 Category: Drugs & Pharmacology Source Type: research

The Status Quo and way forwards on the development of Tibetan Medicine and the Pharmacological Research of Tibetan Materia Medica
Publication date: Available online 13 February 2020Source: Pharmacological ResearchAuthor(s): Ke Fu, Min Xu, You Zhou, Xiaoli Li, Zhang Wang, Xianwu Liu, Xianli Meng, Yong Zeng, Hai ZhangAbstractTibetan medicine (TM), the second largest traditional Chinese medicine system in China, boasts a long history and an integrated theoretical system. It abounds with classical medical works constituing a unique corpus of Tibetan materia medica (TMM). China has now conceived a modern education system of TM, and Tibetan medical hospitals at different levels have been set up. Many enterprises are granted the privileges to produce prepar...
Source: Pharmacological Research - February 15, 2020 Category: Drugs & Pharmacology Source Type: research

MDA-9/Syntenin (SDCBP): Novel gene and therapeutic target for cancer metastasis
Publication date: Available online 13 February 2020Source: Pharmacological ResearchAuthor(s): Swadesh K. Das, Santanu Maji, Stephen L. Wechman, Praveen Bhoopathi, Anjan K. Pradhan, Sarmistha Talukdar, Devanand Sarkar, Joseph Landry, Chunqing Guo, Xiang-Yang Wang, Webster K. Cavenee, Luni Emdad, Paul B. FisherAbstractThe primary cause of cancer-related death from solid tumors is metastasis. While unraveling the mechanisms of this complicated process continues, our ability to effectively target and treat it to decrease patient morbidity and mortality remains disappointing. Early detection of metastatic lesions and approaches...
Source: Pharmacological Research - February 15, 2020 Category: Drugs & Pharmacology Source Type: research

Pirfenidone is a Cardioprotective Drug: Mechanisms of Action and Preclinical Evidence
Publication date: Available online 12 February 2020Source: Pharmacological ResearchAuthor(s): Alberto Aimo, Elisabetta Cerbai, Gianluca Bartolucci, Luigi Adamo, Andrea Barison, Giuseppa Lo Surdo, Stefania Biagini, Claudio Passino, Michele EmdinAbstractMyocardial fibrosis is an endogenous response to different cardiac insults that may become maladaptive over time and contribute to the onset and progression of heart failure (HF). Fibrosis is a direct and indirect target of established HF therapies, namely inhibitors of the renin-angiotensin-aldosterone system, but its resilience to therapy warrants a search for novel, more t...
Source: Pharmacological Research - February 13, 2020 Category: Drugs & Pharmacology Source Type: research

Berberine-mediated up-regulation of surfactant protein D facilitates cartilage repair by modulating immune responses via the inhibition of TLR4/NF-ĸB signaling
Publication date: Available online 11 February 2020Source: Pharmacological ResearchAuthor(s): Yan Zhou, Jianghua Ming, Ming Deng, Yaming Li, Bochun Li, Jia Li, Yonggang Ma, Zhonghui Chen, Shiqing LiuAbstractThe innate immune system drives inflammatory joint damage in osteoarthritis (OA) and regulates cartilage repair. Berberine chloride (BBR) is an isoquinoline alkaloid that shows immunomodulatory activity in a variety of cell lines. However, the immunomodulatory mechanisms of BBR in chondrocytes during OA are largely unknown. Herein, we assessed the ability of BBR to mediate chondroprotection through its effects on innate...
Source: Pharmacological Research - February 12, 2020 Category: Drugs & Pharmacology Source Type: research

Postmenopausal hormone therapy and Alzheimer's disease, dementia, and Parkinson's disease: A systematic review and time-response meta-analysis
Publication date: Available online 11 February 2020Source: Pharmacological ResearchAuthor(s): Minghua Wu, Min Li, Jun Yuan, Sen Liang, Zhaoyao Chen, Min Ye, Paul M. Ryan, Cain Clark, Shing Cheng Tan, Jamal Rahmani, Hamed kord Varkaneh, Akshaya Srikanth BhagavathulaAbstractHormone therapy continues to be a favourable option in the management of menopausal symptomatology, but the associated risk-benefit ratios with respect to neurodegenerative diseases remain controversial. The study aim was to determine the relation between menopausal hormone therapy and Alzheimer's disease, dementia, and Parkinson's disease in human subjec...
Source: Pharmacological Research - February 12, 2020 Category: Drugs & Pharmacology Source Type: research

Astaxanthin anticancer effects are mediated through multiple molecular mechanisms: a systematic review
Publication date: Available online 11 February 2020Source: Pharmacological ResearchAuthor(s): Immacolata Faraone, Chiara Sinisgalli, Angela Ostuni, Maria Francesca Armentano, Monica Carmosino, Luigi Milella, Daniela Russo, Fabiana Labanca, Haroon KhanAbstractDuring the latest decades, the interest on the effectiveness of natural compounds and their impact on human health constantly increased, especially on those demonstrating to be effective on cancer. Molecules coming from nature are currently used in chemotherapy like Taxol, Vincristine or Vinblastine, and several other natural substances have been showed to be active in...
Source: Pharmacological Research - February 12, 2020 Category: Drugs & Pharmacology Source Type: research

Editorial Board
Publication date: February 2020Source: Pharmacological Research, Volume 152Author(s): (Source: Pharmacological Research)
Source: Pharmacological Research - February 12, 2020 Category: Drugs & Pharmacology Source Type: research

Venom natriuretic peptides guide the design of heart failure therapeutics
Publication date: Available online 11 February 2020Source: Pharmacological ResearchAuthor(s): Sindhuja Sridharan, R. Manjunatha Kini, Arthur Mark RichardsAbstractHeart failure (HF) affects over 26 million people world-wide. It is a syndrome triggered by loss of normal cardiac function due to many acute (eg myocardial infarction) and/or chronic (eg hypertension) causes and characterized by mixed beneficial and deleterious activation of a complex of multifaceted neurohormonal systems the net effect of which frequently is further adverse disruption of pressure-volume homeostasis. Unlike the situation in chronic heart failure,...
Source: Pharmacological Research - February 12, 2020 Category: Drugs & Pharmacology Source Type: research

Targeting Obesity with plant-derived pancreatic lipase inhibitors: A comprehensive review
Publication date: Available online 8 February 2020Source: Pharmacological ResearchAuthor(s): Logesh Rajan, Dhanabal Palaniswamy, Suresh Kumar MohankumarAbstractThe prevalence of obesity is alarmingly increasing in the last few decades and leading to many serious public health concerns worldwide. The dysregulated lipid homeostasis due to various genetic, environmental and lifestyle factors is considered one of the critical putative pathways mediating obesity. Nonetheless, the scientific advancements unleashing the molecular dynamics of lipid metabolism have provided deeper insights on the emerging roles of lipid hydrolysing...
Source: Pharmacological Research - February 9, 2020 Category: Drugs & Pharmacology Source Type: research

Human antigen R: A potential therapeutic target for liver diseases
In conclusion, although characterizing the liver-specific HuR function and demonstrating the multi-level regulative networks of HuR in the liver are still required, emerging evidence supports the notion that HuR represents a potential therapeutic target for the treatment of chronic liver diseases.Graphical abstract (Source: Pharmacological Research)
Source: Pharmacological Research - February 9, 2020 Category: Drugs & Pharmacology Source Type: research

Tumor Microenvironment: Challenges and Opportunities in Targeting Metastasis of Triple Negative Breast Cancer
Publication date: Available online 9 February 2020Source: Pharmacological ResearchAuthor(s): Deepak KGK, Vempati Rahul, Purnachandra Nagaraju Ganji, Ramesh Dasari Venkata, Nagini S., Rao D.N., Rao Malla RamaAbstractTriple negative breast cancer (TNBC) is most aggressive subtype of breast cancers with high probability of metastasis as well as lack of specific targets and targeted therapeutics. TNBC is characterized with unique tumor microenvironment (TME), which differs from other subtypes. TME is associated with induction of proliferation, angiogenesis, inhibition of apoptosis and immune system suppression, and drug resist...
Source: Pharmacological Research - February 9, 2020 Category: Drugs & Pharmacology Source Type: research

Activation of Siglec-7 results in inhibition of in vitro and in vivo growth of human mast cell leukemia cells
Publication date: Available online 5 February 2020Source: Pharmacological ResearchAuthor(s): Nadine Landolina, Ilan Zaffran, Dubravka Smiljkovic, Eva Serrano-Candelas, Dominik Schmiedel, Sheli Friedman, Michel Arock, Karin Hartmann, Eli Pikarsky, Ofer Mandelboim, Margarita Martin, Peter Valent, Francesca Levi-SchafferAbstractAdvanced systemic mastocytosis is a rare and still untreatable disease. Blocking antibodies against inhibitory receptors, also known as "immune checkpoints", have revolutionized anti-cancer treatment. Inhibitory receptors are expressed not only on normal immune cells, including mast cells but...
Source: Pharmacological Research - February 6, 2020 Category: Drugs & Pharmacology Source Type: research

The Potential of the Novel NAD+ Supplementing Agent, SNH6, as a Therapeutic Strategy for the Treatment of Friedreich’s Ataxia
Publication date: Available online 4 February 2020Source: Pharmacological ResearchAuthor(s): Shannon Chiang, Danuta S. Kalinowski, Mahendiran Dharmasivam, Nady Braidy, Des R. Richardson, Michael L.-H. HuangAbstractFriedreich’s ataxia (FA) is due to deficiency of the mitochondrial protein, frataxin, which results in multiple pathologies including a deadly, hypertrophic cardiomyopathy. Frataxin loss leads to deleterious accumulations of redox-active, mitochondrial iron, and suppressed mitochondrial bioenergetics. Hence, there is an urgent need to develop innovative pharmaceuticals. Herein, the activity of the novel com...
Source: Pharmacological Research - February 5, 2020 Category: Drugs & Pharmacology Source Type: research

Gut microbiota and neuroinflammation in pathogenesis of hypertension: A potential role for hydrogen sulfide
Publication date: Available online 2 February 2020Source: Pharmacological ResearchAuthor(s): Basak Donertas Ayaz, Jasenka ZubcevicAbstractInflammation and gut dysbiosis are hallmarks of hypertension (HTN). Hydrogen sulfide (H2S) is an important freely diffusing molecule that modulates the function of neural, cardiovascular and immune systems, and circulating levels of H2S are reduced in animals and humans with HTN. While most research to date has focused on H₂S produced endogenously by the host, H2S is also produced by the gut bacteria and may affect the host homeostasis. Here, we review an association between neuroinfla...
Source: Pharmacological Research - February 3, 2020 Category: Drugs & Pharmacology Source Type: research

A novel FFA1 agonist, CPU025, improves glucose-lipid metabolism and alleviates fatty liver in obese-diabetic (ob/ob) mice
Publication date: Available online 31 January 2020Source: Pharmacological ResearchAuthor(s): Zheng Li, Chunxia Liu, Zongtao Zhou, Lijun Hu, Liming Deng, Qiang Ren, Hai QianAbstractIn the effort to identify anti-diabetic drug, we discovered a novel free fatty acid receptor 1 (FFA1) agonist CPU025, which is structurally different from previously reported FFA1 agonists. The present study revealed CPU025 is a potent FFA1 agonist (EC50 = 38.7 nM) with moderate agonistic activity on PPARδ (EC50 = 625.6 nM), and promotes insulin secretion at a glucose-dependent manner. Modeling study also illuminated CPU025 forms interactio...
Source: Pharmacological Research - February 1, 2020 Category: Drugs & Pharmacology Source Type: research

Tectorigenin attenuates diabetic nephropathy by improving vascular endothelium dysfunction through activating AdipoR1/2 pathway
In this study, we examined the effects of TEC on DN development in db/db mice, a type of genetic defect diabetic mice that can spontaneously develop into severe renal dysfunction. Intriguingly, TEC treatment restored diabetes-induced glucose and lipid metabolic disorder; and improved the deterioration of renal function, particularly the renal endothelium function in db/db mice. Additionally, TEC inhibited the renal inflammation via reducing macrophages infiltration and M1 polarization. Moreover, TEC inhibited lipopolysaccharide (LPS)-induced endothelial injury and M1 polarization in vitro. Mechanistically, TEC partially re...
Source: Pharmacological Research - February 1, 2020 Category: Drugs & Pharmacology Source Type: research

Corrigendum to “The new entries in the therapeutic armamentarium: The small molecule JAK inhibitors” [Pharmacol. Res. 147 (2019) 104392]
Publication date: Available online 1 February 2020Source: Pharmacological ResearchAuthor(s): Katie Bechman, Mark Yates, James B. Galloway (Source: Pharmacological Research)
Source: Pharmacological Research - February 1, 2020 Category: Drugs & Pharmacology Source Type: research

Effect of Lactobacillusplantarum containing probiotics on blood pressure: A systematic review and meta-analysis
Publication date: March 2020Source: Pharmacological Research, Volume 153Author(s): Anne-Mary Lewis-Mikhael, Amirhossein Davoodvandi, Sadegh JafarnejadAbstractPrevious studies have recommended that probiotics may have blood pressure (BP)-lowering effects. However, they examined all probiotic strains (multi/single probiotics) simultaneously. In respect to strain specificity properties of probiotic, the aim of the present study was to systematically investigate the role of Lactobacillus plantarum as an anti-hypertensive agent by performing a meta-analysis of randomized controlled trials. PubMed, Scopus, Cochrane Library and G...
Source: Pharmacological Research - January 31, 2020 Category: Drugs & Pharmacology Source Type: research

The Rho guanine nucleotide exchange factor P-Rex1 as a potential drug target for cancer metastasis and inflammatory diseases
Publication date: Available online 30 January 2020Source: Pharmacological ResearchAuthor(s): Richard D. YeAbstractPhosphatidylinositol 3,4,5-trisphosphate (PIP3)-dependent Rac exchanger 1 (P-Rex1) is a guanine nucleotide exchange factor (GEF) for Rac small GTPases and the Rac-related GTPase RhoG. P-Rex1 plays an important role in cell migration and relays intracellular signals generated through activation of G protein-coupled receptors and receptor tyrosine kinases. Studies of mouse models have found that P-Rex1 expression and activation is associated with tumor cell migration, brain development and pathological changes su...
Source: Pharmacological Research - January 30, 2020 Category: Drugs & Pharmacology Source Type: research

Exploring and Characterizing a Novel Combination of Paeoniflorin and Talatizidine for the Treatment of Rheumatoid Arthritis
In conclusion, this study identified PAE and TLT as the main BACs of WTD in alleviating the severity of RA, and also developed a novel combination of PAE and TLT as a promising candidate drug for RA therapy.Graphical abstract (Source: Pharmacological Research)
Source: Pharmacological Research - January 28, 2020 Category: Drugs & Pharmacology Source Type: research

Urolithin B, a Gut Microbiota Metabolite, Protects against Myocardial Ischemia/Reperfusion Injury via p62/Keap1/Nrf2 Signaling Pathway
Publication date: Available online 26 January 2020Source: Pharmacological ResearchAuthor(s): Dechong Zheng, Zumei Liu, You Zhou, Ning Hou, Wei Yan, Yuan Qin, Qianfang Ye, XinYi Cheng, Qing Xiao, Yonglin Bao, Jiandong Luo, Xiaoqian WuAbstractIschemia/reperfusion (IR) induces additional damage during the restoration of blood flow to ischemic myocardium. Urolithin B (UB) is one of the gut metabolites of ellagitannins, a class of antioxidant polyphenols, which was found to be protective against oxidative stress in multiple organs. However, the role of UB in cardiovascular disease remains elusive. Adult Sprague Dawley rats were...
Source: Pharmacological Research - January 27, 2020 Category: Drugs & Pharmacology Source Type: research

The Role of Hepcidin and Iron Homeostasis in Atherosclerosis
Publication date: Available online 25 January 2020Source: Pharmacological ResearchAuthor(s): Florian Wunderer, Lisa Traeger, Haakon H. Sigurslid, Patrick Meybohm, Donald B. Bloch, Rajeev MalhotraAbstractAtherosclerotic cardiovascular disease is a major burden on global health and a leading cause of death worldwide. The pathophysiology of this chronic disease is complex, involving inflammation, lipoprotein oxidation and accumulation, plaque formation, and calcification. In 1981, Dr. Jerome Sullivan formulated the ‘Iron Hypothesis’, suggesting that higher levels of stored iron promote cardiovascular diseases, whe...
Source: Pharmacological Research - January 26, 2020 Category: Drugs & Pharmacology Source Type: research

Effect of Lactobacillus Plantarum Containing Probiotics on Blood Pressure: A systematic review and meta-analysis
Publication date: Available online 24 January 2020Source: Pharmacological ResearchAuthor(s): Anne-Mary Lewis-Mikhael, Amirhossein Davoodvandi, Sadegh JafarnejadAbstractPrevious studies have recommended that probiotics may have blood pressure (BP)-lowering effects. However, they examined all probiotic strains (multi/single probiotics) simultaneously. In respect to strain specificity properties of probiotic, the aim of the present study was to systematically investigate the role of Lactobacillus plantarum as an anti-hypertensive agent by performing a meta-analysis of randomized controlled trials. PubMed, Scopus, Cochrane Lib...
Source: Pharmacological Research - January 25, 2020 Category: Drugs & Pharmacology Source Type: research

SERCA and P-glycoprotein inhibition and ATP depletion are necessary for celastrol-induced autophagic cell death and collateral sensitivity in multidrug-resistant tumor cells
Publication date: Available online 23 January 2020Source: Pharmacological ResearchAuthor(s): Su-Wei Xu, Betty Yuen Kwan Law, Steven Li Qun Qu, Sami Hamdoun, Juan Chen, Wei Zhang, Jian-Ru Guo, An-Guo Wu, Simon Wing Fai Mok, David Wei Zhang, Chenglai Xia, Yoshikazu Sugimoto, Thomas Efferth, Liang Liu, Vincent Kam Wai WongAbstractMultidrug resistance (MDR) represents an obstacle in anti-cancer therapy. MDR is caused by multiple mechanisms, involving ATP-binding cassette (ABC) transporters such as P-glycoprotein (P-gp), which reduces intracellular drug levels to sub-therapeutic concentrations. Therefore, sensitizing agents ret...
Source: Pharmacological Research - January 25, 2020 Category: Drugs & Pharmacology Source Type: research

Role of Heterogeneous Regulatory T Cells in the Tumor Microenvironment
Publication date: Available online 23 January 2020Source: Pharmacological ResearchAuthor(s): Ting Wei, Weijie Zhong, Qingshan LiAbstractRegulatory T cells (Tregs) modulate ongoing immune responses to prevent autoimmunity in healthy bodies and inhibit effective anti-tumor immunity responses in tumor patients, leading to tumor progression. The function of Tregs in tumor immunity suggests that elimination of Tregs in the host may enhance the anti-tumor immune response. Despite the success of strategies for depleting Tregs in tumor-bearing patients, the overall clinical efficacy is limited and accompanied by undesirable side e...
Source: Pharmacological Research - January 25, 2020 Category: Drugs & Pharmacology Source Type: research

LYW-6, a Novel Cryptotanshinone Derived STAT3 Targeting Inhibitor, Suppresses Colorectal Cancer Growth and Metastasis
Publication date: Available online 23 January 2020Source: Pharmacological ResearchAuthor(s): Huan Wang, Zhe Liu, Lingnan Guan, Jiankang Li, Siyi Chen, Wenying Yu, Maode LaiAbstractThe constitutive activation of signal transducer and activator of transcription 3(STAT3) is associated with aggressive development and metastasis in colorectal cancer (CRC), but STAT3-targeting drugs remain elusive in clinic. Here, structure-based strategy was used to remodel the natural compound cryptotanshinone into a more effective STAT3 inhibitor LYW-6. Using the Biolayer Interferometry assay, we observed that LYW-6 exhibited specific interac...
Source: Pharmacological Research - January 25, 2020 Category: Drugs & Pharmacology Source Type: research

Hypericin attenuates nonalcoholic fatty liver disease and abnormal lipid metabolism via the PKA-mediated AMPK signaling pathway in vitro and in vivo
In this study, we aimed to explore the preventive and therapeutic effects of HP against NAFLD and the underlying mechanisms in vitro and in vivo. Here, we demonstrated that HP improved cell viability by reducing apoptosis and attenuated lipid accumulation in hepatocytes both in vitro and in vivo via attenuating oxidative stress, inhibiting lipogenesis and enhancing lipid oxidization. Thus, HP exhibited significant preventive and therapeutic effects against HFHS-induced NAFLD and dyslipidemia in mice. Furthermore, we demonstrated that HP directly bound to PKACα and activated PKA/AMPK signaling to elicit its effects ag...
Source: Pharmacological Research - January 25, 2020 Category: Drugs & Pharmacology Source Type: research

Incretins and microRNAs: interactions and physiological relevance
Publication date: Available online 23 January 2020Source: Pharmacological ResearchAuthor(s): Shabnam Radbakhsh, Thozhukat Sathyapalan, Maciej Banach, Amirhossein SahebkarAbstractMicroRNAs (miRNA) are one class of the small regulatory RNAs that can impact the expression of numerous genes including incretin hormones and their G protein-coupled receptors. Incretin peptides, including GLP-1, GLP-2, and GIP, are released from the gastrointestinal tract and have an crucial role in the glucose hemostasis and pancreatic beta-cell function. These hormones and their analogs with a longer half-life, glucagon like peptide-1 receptor a...
Source: Pharmacological Research - January 23, 2020 Category: Drugs & Pharmacology Source Type: research

Probing Biological Mechanisms with Chemical Tools
Publication date: Available online 18 January 2020Source: Pharmacological ResearchAuthor(s): Congbao Kang, Thomas H. KellerAbstractTraditionally small molecules have mainly been used to inhibit biochemical activities of proteins, however such compounds can also be used to change the conformational energy landscape of proteins. Tool compounds that allosterically modulate protein conformations often reveal unexpected biological mechanisms, which have therapeutic potential. We discuss two examples where screening hits were found to bind to unexpected binding pockets on well know proteins, establishing new routes for the inhib...
Source: Pharmacological Research - January 19, 2020 Category: Drugs & Pharmacology Source Type: research

Editorial Board
Publication date: January 2020Source: Pharmacological Research, Volume 151Author(s): (Source: Pharmacological Research)
Source: Pharmacological Research - January 18, 2020 Category: Drugs & Pharmacology Source Type: research