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Piperine

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https://www.readbyqxmd.com/read/28427563/neuroinflammation-in-alzheimer-s-disease-the-preventive-and-therapeutic-potential-of-polyphenolic-nutraceuticals
#1
Yousef Sawikr, Nagendra Sastry Yarla, Ilaria Peluso, Mohammad Amjad Kamal, Gjumrakch Aliev, Anupam Bishayee
Brain inflammation, characterized by increased microglia and astrocyte activation, increases during aging and is a key feature of neurodegenerative diseases, such as Alzheimer's disease (AD). In AD, neuronal death and synaptic impairment, induced by amyloid-β (Aβ) peptide, are at least in part mediated by microglia and astrocyte activation. Glial activation results in the sustained production of proinflammatory cytokines and reactive oxygen species, giving rise to a chronic inflammatory process. Astrocytes are the most abundant glial cells in the central nervous system and are involved in the neuroinflammation...
2017: Advances in Protein Chemistry and Structural Biology
https://www.readbyqxmd.com/read/28426244/piperine-triggers-apoptosis-of-human-oral-squamous-carcinoma-through-cell-cycle-arrest-and-mitochondrial-oxidative-stress
#2
Sahabjada Siddiqui, Md Sultan Ahamad, Asif Jafri, Mohd Afzal, Md Arshad
Piperine is a nitrogenous pungent substance exhibiting multifunctional pharmacological properties. However, the mechanism underlying its anticancer potential is not well elucidated in human oral squamous carcinoma (KB) cell line. The anticancer potential of piperine was evaluated through potent biomarkers viz. reactive oxygen species (ROS), cellular apoptosis, and loss of mitochondrial membrane potential (MMP). In addition, cell cycle kinetics and caspases-3 activity were also carried out to confirm anticancer activity of piperine...
April 20, 2017: Nutrition and Cancer
https://www.readbyqxmd.com/read/28425323/enhanced-solubility-of-piperine-using-hydrophilic-carrier-based-potent-solid-dispersion-systems
#3
Thenmozhi Kathavarayan, Young Je Yoo
CONTEXT: Piperine alkaloid, an important constituent of black pepper exhibits numerous therapeutic properties whereas its usage as a drug is limited due to its poor solubility in aqueous medium, which leads to poor bioavailability. OBJECTIVE: Herein a new method has been developed to improve the solubility of this drug based on the development of solid dispersions with improved dissolution rate using hydrophilic carriers such as sorbitol (Sor), polyethylene glycol (PEG) and polyvinyl pyrrolidone K30 (PVP) by solvent method...
April 20, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28414236/thermal-rearrangement-of-sulfamoyl-azides-reactivity-and-mechanistic-study
#4
Xiaodong Zou, Jiaqi Zou, Lizheng Yang, Guigen Li, Hongjian Lu
The rearrangement of sulfamoyl azides under thermal conditions to form a C-C bond while breaking two C-N bonds is reported. Mechanistic study shows that this reaction goes through a Curtius-type rearrangement to form a 1,1-diazene, then which rearranges possibly through both a concerted rearrangement process and a stepwise radical process. This rearrangement could be used in the synthesis of complex biologically active molecules such as sterols, and piperine derivatives.
April 17, 2017: Journal of Organic Chemistry
https://www.readbyqxmd.com/read/28413973/docking-related-survey-on-natural-product-based-new-monoamine-oxidase-inhibitors-and-their-therapeutic-potential
#5
Priyanka Dhiman, Neelam Malik, Anurag Khatkar
This is an exciting period for research on monoamine oxidase and its effects on central nervous system. As the current hitting-one-target therapeutic strategy has become quite inefficient for the treatment of various neurological disorders. The objective of this review is to identify and critically discuss the computational development of multi-target natural and related ligand-MAO protein docking approaches in the study of monoamine oxidase (MAO) enzymes. Computational development of the new compounds form natural and related synthetic origin, active as MAO inhibitors (MAOIs) were discussed in some detail...
April 14, 2017: Combinatorial Chemistry & High Throughput Screening
https://www.readbyqxmd.com/read/28397086/structure-activity-relationship-of-piperine-and-its-synthetic-amide-analogs-for-therapeutic-potential-to-prevent-experimentally-induced-er-stress-in-vitro
#6
Ayat S Hammad, Sreenithya Ravindran, Ashraf Khalil, Shankar Munusamy
Endoplasmic reticulum (ER) is the key organelle involved in protein folding and maturation. Emerging studies implicate the role of ER stress in the development of chronic kidney disease. Thus, there is an urgent need for compounds that could ameliorate ER stress and prevent CKD. Piperine and its analogs have been reported to exhibit multiple pharmacological activities; however, their efficacy against ER stress in kidney cells has not been studied yet. Hence, the goal of this study was to synthesize amide-substituted piperine analogs and screen them for pharmacological activity to relieve ER stress using an in vitro model of tunicamycin-induced ER stress using normal rat kidney (NRK-52E) cells...
April 10, 2017: Cell Stress & Chaperones
https://www.readbyqxmd.com/read/28370557/characterization-of-piperine-metabolites-in-rats-by-ultra-high-performance-liquid-chromatography-with-electrospray-ionization-quadruple-time-of-flight-tandem-mass-spectrometry
#7
Tingting Gao, Haiping Xue, Lu Lu, Tong Zhang, Han Han
RATIONALE: Piperine is a major constituent of Piper nigrum L. and is a naturally bio-active alkaloid. Piperine structural changes have been shown to result in different biological effects. The present study aims to investigate piperine metabolites in rat plasma, bile, urine, and feces after oral administration. METHODS: The metabolic pathway of piperine in vivo was carried out using ultra-high-performance liquid chromatography (UHLPC) combined with electrospray ionization quadruple time-of-flight tandem mass spectrometry (Q-TOF-MS)...
March 31, 2017: Rapid Communications in Mass Spectrometry: RCM
https://www.readbyqxmd.com/read/28352353/anticonvulsant-effect-of-piperine-ameliorates-memory-impairment-inflammation-and-oxidative-stress-in-a-rat-model-of-pilocarpine-induced-epilepsy
#8
Ke Mao, Ding Lei, Heng Zhang, Chao You
The primary active component of black pepper is piperine, which is purified and used to treat epilepsy, achieving higher efficiency when purified. The present study was conducted to evaluate whether the anticonvulsant effect of piperine ameliorates pilocarpine-induced epilepsy, and to investigate the mechanism underlying these effects. Epilepsy was induced in Sprague Dawley rats using pilocarpine. Pilocarpine-induced epilepsy in the rats was treated with 40 mg/kg piperine for 45 consecutive days. Status epilepticus and a Morris water maze test were used to analyze the anticonvulsant effects of piperine in the epileptic rats...
February 2017: Experimental and Therapeutic Medicine
https://www.readbyqxmd.com/read/28344463/curcumin-and-piperine-supplementation-and-recovery-following-exercise-induced-muscle-damage-a-randomized-controlled-trial
#9
Barthélémy Delecroix, Abd Elbasset Abaïdia, Cédric Leduc, Brian Dawson, Grégory Dupont
The aim of this study was to analyze the effects of oral consumption of curcumin and piperine in combination on the recovery kinetics after exercise-induced muscle damage. Forty-eight hours before and following exercise-induced muscle damage, ten elite rugby players consumed curcumin and piperine (experimental condition) or placebo. A randomized cross-over design was performed. Concentric and isometric peak torque for the knee extensors, one leg 6 seconds sprint performance on a non-motorized treadmill, counter movement jump performance, blood creatine kinase concentration and muscle soreness were assessed immediately after exercise, then at 24h, 48h and 72h post-exercise...
March 2017: Journal of Sports Science & Medicine
https://www.readbyqxmd.com/read/28341137/targeting-hepatocellular-carcinoma-with-piperine-by-radical-mediated-mitochondrial-pathway-of-apoptosis-an-in%C3%A2-vitro-and-in%C3%A2-vivo-study
#10
Vetrichelvi Gunasekaran, Kannan Elangovan, S Niranjali Devaraj
Redox mediated cancer therapeutics are of immense interest in the recent decade due to their anticancer activity. Piperine is the principal alkaloid of black and long pepper. Although its anticancer activity has been reported in number of cancers , the precise molecular mechanism of action remains to be unravelled. Hence, in this study, for the first time, we delineated the mechanistic insight into the effect of piperine against hepatocellular carcinoma (HCC).MTT analysis determined the dose and time dependent cytotoxicity of piperine against Hep G2 cells...
March 21, 2017: Food and Chemical Toxicology
https://www.readbyqxmd.com/read/28330809/piperine-attenuates-pathological-cardiac-fibrosis-via-ppar-%C3%AE-akt-pathways
#11
Zhen-Guo Ma, Yu-Pei Yuan, Xin Zhang, Si-Chi Xu, Sha-Sha Wang, Qi-Zhu Tang
Mitogen-activated protein kinases (MAPKs) and AMP-activated protein kinase α (AMPKα) play critical roles in the process of cardiac hypertrophy. Previous studies have demonstrated that piperine activates AMPKα and reduces the phosphorylation of extracellular signal-regulated kinase (ERK). However, the effect of piperine on cardiac hypertrophy remains completely unknown. Here, we show that piperine-treated mice had similar hypertrophic responses as mice treated with vehicle but exhibited significantly attenuated cardiac fibrosis after pressure overload or isoprenaline (ISO) injection...
March 14, 2017: EBioMedicine
https://www.readbyqxmd.com/read/28326461/toxicity-and-detoxification-mechanism-of-black-pepper-and-its-major-constituent-in-controlling-rhynchophorus-ferrugineus-olivier-curculionidae-coleoptera
#12
A Hussain, M Rizwan-Ul-Haq, H Al-Ayedh, A M Aljabr
The survival, feeding response, and detoxification mechanism of Rhynchophorus ferrugineus Olivier, a key pest responsible for destruction of date palm, was examined with different extracts of Piper nigrum and its major constituent (piperine) identified by GC-MS. In the present study, toxicity of different extracts of black pepper was evaluated by incorporating diffferent doses of extracts into the artificial diet of red palm weevil larvae. All extracts showed dose-dependent insecticidal activity to the tested eighth-instar red palm weevil larvae...
March 21, 2017: Neotropical Entomology
https://www.readbyqxmd.com/read/28314475/pharmacokinetic-based-study-on-lagged-stimulation-of-curcumae-longae-rhizoma-piper-nigrum-couplet-in-their-main-active-components-metabolism-using-uplc-ms-ms
#13
Zhao Chen, Dongmei Sun, Xiaoli Bi, Xiaohui Zeng, Wenhui Luo, Dake Cai, Qiaohuang Zeng, Aili Xu
BACKGROUND: Curcumae Longae Rhizoma is one of the commonly used traditional Chinese medicines, which has multiple biological activities such as relieving stagnation and stasis, pain alleviation, curing amenorrhea and wounds. However, its main active component-curcumin has poor absorption and very fast metabolism in body. To solve this problem, Piper nigrum was introduced for its ability to strengthen bioavailability of other compounds. PURPOSE: In most cases of TCM couplets, all ingredients were prepared and taken simultaneously, which in our opinion did not take full advantage of their interactions...
April 15, 2017: Phytomedicine: International Journal of Phytotherapy and Phytopharmacology
https://www.readbyqxmd.com/read/28254575/in-vivo-cough-suppressive-activity-of-pectic-polysaccharide-with-arabinogalactan-type-ii-side-chains-of-piper-nigrum-fruits-and-its-synergistic-effect-with-piperine
#14
Sadhana Khawas, Gabriela Nosáľová, Sujay Kumar Majee, Kanika Ghosh, Washim Raja, Veronika Sivová, Bimalendu Ray
Piper nigrum L. fruits are not only a prized spice, but also highly valued therapeutic agent that heals many ailments including asthma, cold and respiratory problems. Herein, we have investigated structural features and in vivo antitussive activity of three fractions isolated from Piper nigrum fruits. The water extract (PN-WE) upon fractionation with EtOH yielded two fractions: a soluble fraction (PN-eSf) and a precipitated (PN-ePf) one. The existence of a pectic polysaccharide with arabinogalactan type II side chains (147kDa) in PN-ePf and piperine in PN-eSf were revealed...
June 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/28224643/endophytic-phomopsis-sp-colonization-in-oryza-sativa-was-found-to-result-in-plant-growth-promotion-and-piperine-production
#15
Chithra S, Jasim B, Jyothis Mathew, Radhakrishnan E K
Endophytic fungi have been reported to have the acquired ability to synthesize host plant specific medicinal natural products. Many fungi with such properties have been characterized and optimized for the conditions which favor maximal production of desired products. However, the inherent plant colonization property of promising endophytic fungi is least studied. Exploiting the transgenome functioning of these fungi have immense applications to add beneficial features to non-host plants. In the present study, endophytic fungus Phomopsis sp...
February 22, 2017: Physiologia Plantarum
https://www.readbyqxmd.com/read/28224392/investigation-of-need-of-natural-bioenhancer-for-a-metabolism-susceptible-drug-raloxifene-in-a-designed-self-emulsifying-drug-delivery-system
#16
Poonam Singh Thakur, Narinder Singh, Abhay T Sangamwar, Arvind Kumar Bansal
Bioenhancers can increase the bioavailability of metabolism susceptible drugs. The present study was designed to understand the impact of bioenhancer on permeability and bioavailability of a biopharmaceutical drug disposition classification system (BDDCS) class II drug raloxifene (RLX). RLX undergoes extensive first pass metabolism by UGT enzymes in gastrointestinal tract (GIT) and has an oral bioavailability of about 2%. Self-emulsifying drug delivery system (SEDDS) of RLX was developed using a designed approach and this formulation was loaded with reported bioenhancers: quercetin and piperine...
February 21, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28185326/alkaloids-from-piper-nigrum-exhibit-antiinflammatory-activity-via-activating-the-nrf2-ho-1-pathway
#17
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
#18
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
#19
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
#20
Mangesh R Bhalekar, Ashwini 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 and zeta potential (ZP). Optimized batch (128.80 nm average size, 78.71% entrapment efficiency and -23.34 mV zeta potential) was characterized for differential scanning calorimetry (DSC), X-ray diffraction which revealed amorphous nature of piperine in SLN...
June 2017: Drug Development and Industrial Pharmacy
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