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Piperine

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https://www.readbyqxmd.com/read/28185326/alkaloids-from-piper-nigrum-exhibit-antiinflammatory-activity-via-activating-the-nrf2-ho-1-pathway
#1
Quynh Mai Thi Ngo, Phuong Thao Tran, Manh Hung Tran, Jeong Ah Kim, Seong Soo Rho, Chi-Hwan Lim, Jin-Cheol Kim, Mi Hee Woo, Jae Sui Choi, Jeong-Hyung Lee, Byung Sun Min
In the present study, ten alkaloids, namely chabamide (1), pellitorine (2), retrofractamide A (3), pyrroperine (4), isopiperolein B (5), piperamide C9:1 (8E) (6), 6,7-dehydrobrachyamide B (7), 4,5-dihydropiperine (8), dehydropipernonaline (9), and piperine (10), were isolated from the fruits of Piper nigrum. Among these, chabamide (1), pellitorine (2), retrofractamide A (3), isopiperolein B (5), and 6,7-dehydrobrachyamide B (7) exhibited significant inhibitory activity on lipopolysaccharide-induced nitric oxide (NO) production in RAW264...
February 10, 2017: Phytotherapy Research: PTR
https://www.readbyqxmd.com/read/28166943/cold-adaptive-thermogenesis-following-consumption-of-certain-pungent-spice-principles-a-validation-study
#2
Chaitanya Pandit, K R Anilakumar
Identifying a means to activate or potentiate thermogenic mechanisms through ingestion of dietary compounds have important implications in cold endurance and survival. Although many reports discuss the thermogenic potential of spices, it is surprising that none of the studies verify whether consumption of spices can improve cold endurance. In this study, we have attempted to evaluate if ingestion of certain spices can activate heat-generating mechanisms in the body such that a fall in. core body temperature (CBT) can be delayed or prevented when faced with a cold challenge...
February 2017: Journal of Thermal Biology
https://www.readbyqxmd.com/read/28165813/piperine-ameliorates-collagenase-induced-achilles-tendon-injury-in-the-rat
#3
Fengyan Gong, Lifeng Cui, Xiaona Zhang, Xiangbo Zhan, Xu Gong, Yan Wen
Tendinopathy is a common clinical pathology found in athletes and workers with mixed treatment results. Piperine, a major alkaloid found in the black and long pepper, has been demonstrated to have variety of pharmacological properties such as analgesic and anti-inflammatory effects. The present study was designed to investigate the effects of piperine on collagenase-induced Achilles tendon injury. Rats were intratendineously injected with collagenase in the right Achilles tendon, followed by intragastrical administration of piperine (100 mg/kg)...
February 6, 2017: Connective Tissue Research
https://www.readbyqxmd.com/read/28161984/formulation-of-piperine-solid-lipid-nanoparticles-sln-for-treatment-of-rheumatoid-arthritis
#4
M R Bhalekar, A R Madgulkar, Puja S Desale, Gyce Marium
The purpose of this work was to formulate piperine solid lipid nanoparticle (SLN) dispersion to exploit its efficacy orally and topically. Piperine-SLN were prepared by melt emulsification method and formula was optimized by the application of 3(2) factorial design. The nanoparticulate dispersion was evaluated for particle size, entrapment efficiency (EE) and zeta potential(ZP). Optimized batch (128.80 nm average size, 78.71% EE and -23.34 Mv Zeta Potential) was characterized for differential scanning calorimetry (DSC), X-ray diffraction(XRD) which revealed amorphous nature of piperine in SLN...
February 6, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28160856/vasculoprotective-and-vasodilatation-effects-of-herbal-formula-sahatsatara-and-piperine-in-spontaneously-hypertensive-rats
#5
Suksalin Booranasubkajorn, Sukit Huabprasert, Jantanee Wattanarangsan, Pruksa Chotitham, Pinpilai Jutasompakorn, Tawee Laohapand, Pravit Akarasereenont, Pinpat Tripatara
BACKGROUND: The herbal formula (Sahatsatara, STF), the Thai traditional poly-herbal recipe, has been used for treatment of muscle pain, anti-flatulence and numbness on hands and feet, with the caution when used in hypertensive patients. However, there is no scientific evidence to prove its effects on cardiovascular system. Piperine is the proposed major active compound in STF. It is shown to have antihypertensive effect in the L-NAME-induced endothelial dysfunction rats. PURPOSE: This study investigated the pharmacokinetics, mechanism of action, as well as the hemodynamic and vasoactive effect and toxicity of STF and piperine using spontaneously hypertensive rats (SHR) and normal Wistar rats (NWR)...
January 15, 2017: Phytomedicine: International Journal of Phytotherapy and Phytopharmacology
https://www.readbyqxmd.com/read/28123572/solid-lipid-nanoparticles-with-tpgs-and-brij-78-a-co-delivery-vehicle-of-curcumin-and-piperine-for-reversing-p-glycoprotein-mediated-multidrug-resistance-in-vitro
#6
Jingling Tang, Hongyu Ji, Jinmei Ren, Mengting Li, Nannan Zheng, Linhua Wu
Multidrug resistance (MDR) is a main clinical hurdle for chemotherapy of cancer, and overexpression of P-glycoprotein (P-gp) is a key factor. In the present study, a new co-delivery system for reversing MDR was designed and developed. The system was composed of curcumin (Cur) and piperine (Pip) encapsulated in solid lipid nanoparticles (SLNs) with tocopheryl polyethylene glycol succinate (TPGS) and Brij 78 [(Cur+Pip)-SLNs]. TPGS and Brij 78 could sensitize MDR tumors by inhibiting the P-gp drug efflux system...
January 2017: Oncology Letters
https://www.readbyqxmd.com/read/28117414/piperine-regulates-ucp1-through-the-ampk-pathway-by-generating-intracellular-lactate-production-in-muscle-cells
#7
Nami Kim, Miso Nam, Mi Sun Kang, Jung Ok Lee, Yong Woo Lee, Geum-Sook Hwang, Hyeon Soo Kim
This study characterizes the human metabolic response to piperine, a curcumin extract, and the details of its underlying molecular mechanism. Using (1)H-NMR-based metabolome analysis, we showed the metabolic effect of piperine on skeletal muscle and found that piperine increased the level of intracellular lactate, an important metabolic intermediate that controls expression of several genes involved in mitochondrial activity. Piperine also induced the phosphorylation of AMP-activated protein kinase (AMPK) and its downstream target, acetyl-CoA carboxylase (ACC), while additionally stimulating glucose uptake in an AMPK dependent manner...
January 24, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28102026/piperine-a-pungent-alkaloid-from-black-pepper-inhibits-b-lymphocyte-activation-and-effector-functions
#8
David A Soutar, Carolyn D Doucette, Robert S Liwski, David W Hoskin
Piperine has several well-documented anti-inflammatory properties; however, little is known regarding its effect on humoral immunity. In this study, we describe the immunosuppressive effect of piperine on B lymphocytes, which are integral to the humoral immune response. Mouse B cells were cultured in the absence or presence of non-cytotoxic concentrations (25, 50, and 100 μM) of piperine during T-dependent or T-independent stimulation. Piperine inhibited B cell proliferation by causing G0/G1 phase cell cycle arrest in association with reduced expression of cyclin D2 and D3...
January 19, 2017: Phytotherapy Research: PTR
https://www.readbyqxmd.com/read/28088738/piperine-modulates-isoproterenol-induced-myocardial-ischemia-through-antioxidant-and-anti-dyslipidemic-effect-in-male-wistar-rats
#9
Velumani Dhivya, Lohanathan Bharathi Priya, Hilda T Chirayil, Swamiappan Sathiskumar, Chih-Yang Huang, Viswanadha Vijaya Padma
Myocardial infarction due to ischemia accounts for majority of deaths among cardiovascular disorders. Isoproterenol (ISO) induced myocardial infarction and the protection offered by piperine was investigated in the present report. Lipid profile analysis by determining the levels of cholesterol, phospholipids, triglycerides and lipoproteins in serum and heart tissues showed anti-dyslipidemic action of piperine against ISO induced myocardial injury by modulating the ISO induced altered lipid profiles, maintaining to near control values...
January 12, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28068976/il-1%C3%AE-induced-modulation-of-gene-expression-profile-in-human-dermal-fibroblasts-the-effects-of-thai-herbal-sahatsatara-formula-piperine-and-gallic-acid-possessing-antioxidant-properties
#10
Onusa Thamsermsang, Pravit Akarasereenont, Tawee Laohapand, Uraiwan Panich
BACKGROUND: Pain is the main symptom of most musculoskeletal disorders and can be caused by inflammation in association with oxidative stress. Thai herbal Sahatsatara formula (STF), a polyherbal formula, has been traditionally used for relieving muscle pain and limb numbness. This study aimed to investigate biologically active compounds of STF and its pharmacological effects related to antioxidant and anti-inflammatory activities. METHODS: The identification of possibly active compounds of STF was performed by high performance liquid chromatography (HPLC)...
January 10, 2017: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/28065397/sensory-active-piperine-analogues-from-macropiper-excelsum-and-their-effects-on-intestinal-nutrient-uptake-in-caco-2%C3%A2-cells
#11
Katja Obst, Barbara Lieder, Katharina V Reichelt, Michael Backes, Susanne Paetz, Katrin Geißler, Gerhard Krammer, Veronika Somoza, Jakob P Ley, Karl-Heinz Engel
The phytochemical profile of Macropiper excelsum (G.Forst.) Miq. subsp. excelsum (Piperaceae), a shrub which is widespread in New Zealand, was investigated by LC-MS-guided isolation and characterization via HR-ESI-TOF-MS and NMR spectroscopy. The isolated compounds were sensorily evaluated to identify their contribution to the overall taste of the crude extract with sweet, bitter, herbal and trigeminal impressions. Besides the known non-volatile Macropiper compounds, the lignans (+)-diayangambin and (+)-excelsin, four further excelsin isomers, (+)-diasesartemin, (+)-sesartemin, (+)-episesartemin A and B were newly characterized...
March 2017: Phytochemistry
https://www.readbyqxmd.com/read/28018704/synthesis-and-characterization-of-molecular-imprinting-polymer-microspheres-of-piperine-extraction-of-piperine-from-spiked-urine
#12
Rachel Marcella Roland, Showkat Ahmad Bhawani
Molecularly imprinted polymer (MIP) microspheres for Piperine were synthesized by precipitation polymerization with a noncovalent approach. In this research Piperine was used as a template, acrylic acid as a functional monomer, ethylene glycol dimethacrylate as a cross-linker, and 2,2'-azobisisobutyronitrile (AIBN) as an initiator and acetonitrile as a solvent. The imprinted and nonimprinted polymer particles were characterized by using Fourier transform infrared spectroscopy (FT-IR) and Scanning Electron Microscopy (SEM)...
2016: Journal of Analytical Methods in Chemistry
https://www.readbyqxmd.com/read/28001214/a-biodegradable-device-for-the-controlled-release-of-piper-nigrum-piperaceae-standardized-extract-to-control-aedes-aegypti-diptera-culicidae-larvae
#13
Kauê Muller Custódio, Joice Guilherme de Oliveira, Diego Moterle, Karine Modolon Zepon, Josiane Somariva Prophiro, Luiz Alberto Kanis
INTRODUCTION: The significant increase in dengue, Zika, and chikungunya and the resistance of the Aedes aegypti mosquito to major insecticides emphasize the importance of studying alternatives to control this vector. The aim of this study was to develop a controlled-release device containing Piper nigrum extract and to study its larvicidal activity against Aedes aegypti. METHODS: Piper nigrum extract was produced by maceration, standardized in piperine, and incorporated into cotton threads, which were inserted into hydrogel cylinders manufactured by the extrusion of carrageenan and carob...
November 2016: Revista da Sociedade Brasileira de Medicina Tropical
https://www.readbyqxmd.com/read/27995955/evidences-for-piperine-inhibiting-cancer-by-targeting-human-g-quadruplex-dna-sequences
#14
Arpita Tawani, Ayeman Amanullah, Amit Mishra, Amit Kumar
Piperine, a naturally occurring alkaloid, is well known as anti-oxidant, anti-mutagenic, anti-tumor and anti-proliferative agent. Piperine exerts such pharmacological activities by binding or interacting with various cellular targets. Recently, the first report for Piperine interaction with duplex DNA has been published last year but its interaction with G-quadruplex structures has not been studied yet. Herein, we report for the first time the interaction of Piperine with various DNA G-quadruplex structures...
December 20, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27991959/local-anesthetic-activity-from-extracts-fractions-and-pure-compounds-from-the-roots-of-ottonia-anisum-spreng-piperaceae
#15
Kelvin S E López, André M Marques, Davyson DE L Moreira, Leosvaldo S Velozo, Roberto T Sudo, Gisele Zapata-Sudo, Elsie F Guimarães, Maria Auxiliadora C Kaplan
Piperaceae species can be found worldwide in tropical and subtropical areas and many of them have been used for centuries in traditional folk medicine and in culinary. In Brazil, species of Piperaceae are commonly used in some communities as local anesthetic and analgesic. Countrified communities have known some species of the genus Ottonia as "anestesia" and it is a common habit of chewing leaves and roots of Ottonia species to relief toothache. The purpose of this study is to report our findings on new molecules entities obtained from the roots of Ottonia anisum Spreng, in which local anesthetic activity (sensory blockage) is demonstrated for the first time in vivo guinea pig model...
October 2016: Anais da Academia Brasileira de Ciências
https://www.readbyqxmd.com/read/27981349/the-influence-of-piperine-on-the-pharmacokinetics-of-fexofenadine-a-p-glycoprotein-substrate-in-healthy-volunteers
#16
Satish Kumar Bedada, Praveen Kumar Boga
PURPOSE: Piperine (PIP) has been found to inhibit P-glycoprotein (P-gp) function in rats, suggesting that it may have the potential to modulate P-gp-mediated drug efflux in humans. The aim of this study was to evaluate the effect of PIP on the pharmacokinetics of fexofenadine (FEX), a P-gp substrate, in healthy volunteers. METHODS: An open-label, two-period, sequential study involving 12 healthy volunteers was conducted. A single oral dose of FEX 120 mg was given to volunteers during the control phase and after the treatment phase...
December 15, 2016: European Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/27960631/exploring-the-binding-mechanism-and-kinetics-of-piperine-with-snake-venom-secretory-phospholipase-a2
#17
Christian Bharathi A, Srinivas Sistla, Syed Ibrahim B
Secreted venom Phospholipase A2 is highly responsible for pharmacological effects like neurotoxicity, myotoxicity, hemolytic, anti-coagulation and platelet aggregation. Neutralization of these pharmacological behaviors is one of the challenges existing for many decades and a potent drug compound for this is very much needed to control local effects of venom sPLA2. In this study, we investigated binding mechanism and kinetics of inhibition of Piperine (major constitute of Piper nigrum) with sPLA2 using DFT, MD simulation, MM-PBSA and SPR method...
December 14, 2016: Journal of Biomolecular Structure & Dynamics
https://www.readbyqxmd.com/read/27928704/antioxidant-effects-of-curcuminoids-in-patients-with-type-2-diabetes-mellitus-a-randomized-controlled-trial
#18
Yunes Panahi, Nahid Khalili, Ebrahim Sahebi, Soha Namazi, Maryam Saberi Karimian, Muhammed Majeed, Amirhossein Sahebkar
BACKGROUND: Oxidative stress has a key role in the pathogenesis of type II diabetes mellitus (T2DM) and its vascular complications. Antioxidant therapy has been suggested as a potential approach to blunt T2DM development and progression. The aim of this study was to assess the effects of supplementation with curcuminoids, which are natural polyphenolics from turmeric, on oxidative indices in diabetic individuals. METHODS: In this randomized double-blind placebo-controlled trial, 118 subjects with T2DM were randomized to curcuminoids (1000 mg/day co-administered with piperine 10 mg/day) or matching placebo for a period of 8 weeks...
February 2017: Inflammopharmacology
https://www.readbyqxmd.com/read/27882569/selective-reduction-in-the-expression-of-ugts-and-sults-a-novel-mechanism-by-which-piperine-enhances-the-bioavailability-of-curcumin-in-rat
#19
Xiaohui Zeng, Dake Cai, Qiaohuang Zeng, Zhao Chen, Guoping Zhong, Juncheng Zhuo, Haining Gan, Xuejun Huang, Ziming Zhao, Nan Yao, Dane Huang, Chengzhe Zhang, Dongmei Sun, Yuxing Chen
Curcumin (CUR) is known to exert numerous health-promoting effects in pharmacological studies, but its low bioavailability hinders the development of curcumin as a feasible therapeutic agent. Piperine (PIP) has been reported to enhance the bioavailability of curcumin, but the underlying mechanism remains poorly understood. In an attempt to find the mechanism by which piperine enhances the bioavailability of curcumin, the dosage ratio (CUR: PIP) and pre-treatment with piperine were hypothesized as key factors for improving the bioavailability in this combination...
January 2017: Biopharmaceutics & Drug Disposition
https://www.readbyqxmd.com/read/27875748/piperine-attenuates-lipopolysaccharide-lps-induced-inflammatory-responses-in-bv2-microglia
#20
Chen Wang-Sheng, An Jie, Li Jian-Jun, Hong Lan, Xing Zeng-Bao, Li Chang-Qing
Piperine, the chief alkaloid isolated from Piper nigrum, has been known to have anti-inflammatory effect. However, the effects of piperine on neuroinflammation have not been reported. In the present study, we evaluated the effects of piperine on neuroinflammation in BV2 microglia and investigated the molecular mechanism. The results showed that piperine significantly inhibited LPS-induced TNF-α, IL-6, IL-1β, and PGE2 production in BV2 cells. Western blot analysis showed that piperine dose-dependently inhibited LPS-induced NF-κB activation...
January 2017: International Immunopharmacology
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