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anti-obesity drugs

Chao Tu, Jieyu He, Bei Wu, Wanchun Wang, Zhihong Li
Osteoarthritis is the most prevalent form of aging-related joint diseases, and its etiology is still not fully understood. Obesity has been recognized as one of the most significant and potentially preventable risk factors for osteoarthritis. Beyond mechanical loading, adipokines, including leptin, visfatin, adiponectin, resistin and others, are demonstrated to have metabolic implications in the pathogenesis and progression in obesity-induced osteoarthritis by modulating the pro/anti-inflammatory and anabolic/catabolic balance, apoptosis, matrix remodeling and subchondral bone ossification...
January 2019: Cytokine
Nicole Remaliah Samantha Sibuyi, Mervin Meyer, Martin Opiyo Onani, Amanda Skepu, Abram Madimabe Madiehe
Obesity is a global epidemic that poses a serious health concern due to it being a risk factor for life-threatening chronic diseases, such as type 2 diabetes, cancer, and cardiovascular diseases. Pharmacotherapy remains the mainstay for the management of obesity; however, its usefulness is limited due to poor drug efficacy, non-specificity and toxic side effects. Therefore, novel approaches that could provide insights into obesity and obesity-associated diseases as well as development of novel anti-obesity treatment modalities or improvement on the existing drugs are necessary...
2018: International Journal of Nanomedicine
Kohji Shirai, Toru Fujita, Michitaka Tanaka, Yuka Fujii, Masatsugu Shimomasuda, Soichi Sakai, Yoshishige Samukawa
INTRODUCTION: Orlistat is an inhibitor of pancreatic lipase and is used as an anti-obesity drug in many countries. However, there are no data available regarding the effects of orlistat on visceral fat accumulation in Japanese subjects. Therefore, this comparative, placebo-controlled, double-blind, randomized study aimed to evaluate the efficacy and safety of orlistat in Japanese participants with excessive visceral fat accumulation and without dyslipidemia, diabetes mellitus, and hypertension ("metabolic diseases")...
December 10, 2018: Advances in Therapy
Payal Gupta, Meenakshi Sharma, Neha Arora, Vikas Pruthi, Krishna Mohan Poluri
BACKGROUND: Farnesol is an acyclic sesquiterpene alcohol, endogenously synthesized via the ergosterol pathway. It is a quorum sensing molecule (QSM) that was first discovered in C. albicans, and is involved in the inhibition of hyphae formation. METHODS: This review focuses on the comprehensive details of occurrence, chemical/biological synthesis of farnesol and its derivatives, and the factors involved in regulation of its production. Further, the review also presents their cellular functions and diversified biomedical applications...
December 10, 2018: Current Topics in Medicinal Chemistry
Agnieszka Owczarczyk-Saczonek, Lesław Bernard Lahuta, Magdalena Ligor, Waldemar Placek, Ryszard Józef Górecki, Bogusław Buszewski
INTRODUCTION: Myo -inositol and its derivatives cyclitols play an important role in the processes of cell regulation, signal transduction, osmoregulation, and ion channel physiology, and are a component of the cell membrane. Free cyclitols present in food or released during the degradation of galactosyl cyclitols by bacteria (in digestive tract) show some physiological benefits. AIM: The aim of this paper is to present and analyze the documented data about curative and healing properties of cyclitols...
December 3, 2018: Nutrients
Chao Zhao, Chengfeng Yang, Sydney Tang Chi Wai, Yanbo Zhang, Maria P Portillo, Paolo Paoli, Yijing Wu, Wai San Cheang, Bin Liu, Christian Carpéné, Jianbo Xiao, Hui Cao
Type 2 diabetes mellitus (T2DM) is the most prevalent disease and becoming a serious public health threat worldwide. It is a severe endocrine metabolic disorder that has the ability to induce serious complications in all kinds of organs. Although mechanisms of anti-diabetics have been described before, we focus here on the cellular and physiological mechanisms involved in the modulation of insulin and glucose blood levels. As obesity and inflammation are intimately associated with the development of T2DM, their possible relationships are also described...
December 3, 2018: Critical Reviews in Food Science and Nutrition
Annie Hasib, Ming T Ng, Neil Tanday, Sarah L Craig, Victor A Gault, Peter R Flatt, Nigel Irwin
BACKGROUND: Therapeutic benefits of peptide-based drugs is limited by rapid renal elimination. METHODS: Therefore, to prolong the biological action profile of the recently characterised triple-acting hybrid peptide, exendin-4/gastrin/xenin-8-Gln, a fatty-acid (C-16) has been covalently attached, creating exendin-4(Lys27 PAL)/gastrin/xenin-8-Gln. Exendin-4/gastrin and liraglutide/gastrin/xenin-8-Gln were also synthesised as direct comparator peptides. RESULTS: All hybrid peptides evoked significant concentration-dependent increases of insulin secretion from isolated murine islets and BRIN-BD11 cells...
November 30, 2018: Diabetes/metabolism Research and Reviews
Tanya Sapundzhieva, Rositsa Karalilova, Anastas Batalov
AIM: To investigate the impact of body mass index (BMI) on clinical disease activity indices and clinical and sonographic remission rates in patients with rheumatoid arthritis (RA). PATIENTS AND METHODS: Sixty-three patients with RA were categorized according to BMI score into three groups: normal (BMI<25), overweight (BMI 25-30) and obese (BMI≥30). Thirty-three of them were treated with conventional synthetic disease-modifying anti-rheumatic drugs (csDMARDs), and 30 with biologic DMARDs (bDMARDs)...
November 30, 2018: Current Rheumatology Reviews
Umesh Panwar, Sanjeev Kumar Singh
BACKGROUND: Obesity is well known multifactorial disorder towards the public health concern in front of the world. Increasing rates of obesity has characterized with liver diseases, chronic diseases, diabetes mellitus, hypertension, and stroke, hearts improper function, reproductive and gastrointestinal, gallstones. An essential enzyme pancreatic lipase recognized for the digestion and absorption of lipids, can be a pleasing drug target towards the future development of anti-obesity therapeutics in cure of obesity disorders...
November 27, 2018: Endocrine, Metabolic & Immune Disorders Drug Targets
Hicham Abou Zeid, Rita Kallab, Marie Antoinette Najm, Hisham Jabbour, Roger Noun, Fadi Sleilati, Salim Chucri, Christine Dagher, Ghassan Sleilaty, Nicole Naccache
BACKGROUND: Non-steroidal anti-inflammatory drugs (NSAIDs) are cornerstone in multimodal analgesia protocols. This point is of great value in morbidly obese patients due to the high prevalence of restrictive pulmonary disease and obstructive sleep apnea. The aim of this study was to test the hypothesis that NSAIDs do not increase acute bariatric surgery complications while optimizing postoperative analgesia. METHODS: Databases of two medical centers were retrospectively reviewed to find all patients who underwent bariatric surgery between 1 January 2017 and 31 December 2017...
November 27, 2018: Obesity Surgery
Emilie Montastier, Diane Beuzelin, Frédéric Martins, Lucile Mir, Marie-Adeline Marqués, Claire Thalamas, Jason Iacovoni, Dominique Langin, Nathalie Viguerie
MicroRNAs have been involved in insulin resistance (IR). As the mechanism whereby niacin, an anti-dyslipidemic agent, leads to IR remains elusive, we sought to identify differentially expressed microRNAs in adipose tissue (AT) of individuals receiving niacin and to explore the link between microRNAs, niacin and IR in human adipocytes.In a double-blind controlled study, 22 obese men received extended-release niacin or placebo over 8 weeks. Bioclinical data and subcutaneous AT biopsies were obtained before and after treatment...
November 27, 2018: International Journal of Obesity: Journal of the International Association for the Study of Obesity
Shanat Baig, Vishy Veeranna, Shaun Bolton, Nicola Edwards, Jeremy W Tomlinson, Konstantinos Manolopoulos, John Moran, Richard P Steeds, Tarekegn Geberhiwot
BACKGROUND: Alström syndrome (ALMS) is a very rare autosomal recessive monogenic disorder caused by a mutation in the ALMS1 gene and characterised by childhood onset obesity, dyslipidaemia, advanced non-alcoholic fatty liver disease, diabetes and extreme insulin resistance. There is evidence of multi-organ fibrosis in ALMS and severity of the disease often leads to organ failure with associated morbidities, resulting in reduced life expectancy. There are no specific treatments for this disease, and current management consists of only symptomatic therapies...
November 26, 2018: BMC Endocrine Disorders
Young-Lai Cho, Jong-Gil Park, Hyo Jin Kang, Wooil Kim, Min Ji Cho, Ju-Hong Jang, Min-Gi Kwon, Sungsik Kim, Sang-Hyun Lee, Jangwook Lee, Yeon-Gu Kim, Young-Jun Park, Won Kon Kim, Kwang-Hee Bae, Byoung-Mog Kwon, Sang J Chung, Jeong-Ki Min
Adipogenesis involved in hypertrophy and hyperplasia of adipocytes is responsible for expanding the mass of adipose tissues in obese individuals. Peroxisome proliferator-activated receptor γ (PPARγ) and CCAAT/enhancer-binding protein α (C/EBPα) are two principal transcription factors induced by delicate signaling pathways, including signal transducer and activator of transcription 5 (STAT5), in adipogenesis. Here, we demonstrated a novel role of ginkgetin, a biflavone from Ginkgo biloba leaves, as a STAT5 inhibitor that blocks the differentiation of preadipocytes into adipocytes...
November 22, 2018: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
Yumeng Zhang, Lei Xu, Meng Ding, Guangyue Su, Yuqing Zhao
ETHNOPHARMACOLOGICAL RELEVANCE: Shenque is an acupoint located in the umbilicus and connected with the meridians. Thus, acupoint herbs applied at Shenque plays a pivotal role in the Chinese traditional medicine due to its sensitivity, permeability, and absorption. Many studies reported the use of Shenque point as a successful therapeutic approach. However, the effect of garlic oil (GO) applied at Shenque point to combat obesity is unmet. Consequently, we investigated the potential benefit of GO applied at Shenque point against obesity...
November 22, 2018: Journal of Ethnopharmacology
Chia Li, Jovana Navarrete, Jing Liang-Guallpa, Chunxia Lu, Samuel C Funderburk, Rui B Chang, Stephen D Liberles, David P Olson, Michael J Krashes
Understanding the neural framework behind appetite control is fundamental to developing effective therapies to combat the obesity epidemic. The paraventricular hypothalamus (PVH) is critical for appetite regulation, yet, the real-time, physiological response properties of PVH neurons to nutrients are unknown. Using a combination of fiber photometry, electrophysiology, immunohistochemistry, and neural manipulation strategies, we determined the population dynamics of four molecularly delineated PVH subsets implicated in feeding behavior: glucagon-like peptide 1 receptor (PVHGlp1r ), melanocortin-4 receptor (PVHMc4r ), oxytocin (PVHOxt ), and corticotropin-releasing hormone (PVHCrh )...
November 13, 2018: Cell Metabolism
Dae Hun Kim, Jae Yeol Kim, Rae Man Kim, Pooja Maharjan, Yu-Geun Ji, Dong-Jin Jang, Kyoung Ah Min, Tae-Sung Koo, Kwan Hyung Cho
Background: The present study aimed to develop orlistat-loaded solid self-nanoemulsifying drug delivery system preconcentrate (SSP) with the minimum use of lipid excipients for the enhanced solubility, in vitro dissolution, lipase inhibition, and in vivo performance. Materials and methods: In the screening of solubilizing vehicles, Solutol HS15 and Lauroglycol 90 were selected as the surfactant and oil phase, respectively. A pseudo-ternary phase diagram composed of Solutol HS15, Lauroglycol 90, and orlistat as an anti-obesity agent and lipid component was constructed, and the SSP regions were confirmed in terms of the particle size distribution in water, melting point by differential scanning calorimetry, and crystallinity by X-ray diffraction...
2018: International Journal of Nanomedicine
Kendall Murphy, Michael Hendley, Christopher Isely, Prakasam Annamalai, Edsel A Peña, Michael Gower
As biomaterial therapies emerge to address adipose tissue dysfunction that underlies metabolic disease, the immune response to these systems must be established. As a potential therapy, we are investigating resveratrol delivery from porous poly(lactide-co-glycolide) scaffolds designed to integrate with adipose tissue. Resveratrol was selected for its ability to protect mice and primates from high fat diet and broad anti-inflammatory properties. Herein, we report fabrication of scaffolds with high resveratrol loading that are stable and active for up to one year...
November 21, 2018: ACS Applied Materials & Interfaces
Eline H van den Berg, Eke G Gruppen, Richard W James, Stephan J L Bakker, Robin P F Dullaart
Non-alcoholic fatty liver disease (NAFLD) is featured by low HDL cholesterol, but activity of the HDL-associated anti-oxidative enzyme paraoxonase-1 (PON-1) remains unclear. To determine the association of PON-1 with suspected NAFLD, we measured serum enzyme activity in 7,622 participants of the Prevention of Renal and Vascular End-Stage Disease (PREVEND) cohort. Fatty Liver Index (FLI)≥60, a proxy of NAFLD, was present in 2,083 participants (27.3%), and coincided with increased prevalence of type 2 diabetes mellitus (T2D), metabolic syndrome (MetS), (central) obesity, elevated triglycerides and low HDL cholesterol (all P<0...
November 19, 2018: Journal of Lipid Research
Saraswoti Khadge, John Graham Sharp, Timothy R McGuire, Geoffrey M Thiele, Paul Black, Concetta DiRusso, Leah Cook, Lynell W Klassen, James E Talmadge
Rodent and clinical studies have documented that myeloid cell infiltration of tumors is associated with poor outcomes, neutrophilia and lymphocytopenia. This contrasts with increased lymphocyte infiltration of tumors, which is correlated with improved outcomes. Lifestyle parameters, such as obesity and diets with high levels of saturated fat and/or omega (ω)-6 polyunsaturated fatty acids (PUFAs), can influence these inflammatory parameters, including an increase in extramedullary myelopoiesis (EMM). While tumor secretion of growth factors (GFs) and chemokines regulate tumor-immune-cell crosstalk, lifestyle choices also contribute to inflammation, abnormal pathology and leukocyte infiltration of tumors...
December 2018: International Immunopharmacology
Beatriz T Meneguetti, Marlon H Cardoso, Camila F Acosta Ribeiro, Mário R Felício, Ingrid B Pinto, Nuno C Santos, Cristiano Marcelo E Carvalho, Octávio L Franco
Obesity is a chronic multifactorial disease, characterized by an excessive accumulation of adipose tissue. It is usually the result of excessive food intake and/or low energy expenditure. Obesity can be triggered by lifestyle, nutritional, genetic, environmental, hormonal and psychological factors. Several strategies are used to treat obesity, including dietary reeducation, with balanced food intake, increased physical exercise, in order to promote energy expenditure and to overcome the insufficiency in weight reduction by other strategies, and the administration of drugs to treat obesity...
November 12, 2018: Pharmacology & Therapeutics
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