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Piperine

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https://www.readbyqxmd.com/read/28633599/mechanism-of-deltamethrin-induced-thymic-and-splenic-toxicity-in-mice-and-its-protection-by-piperine-and-curcumin-in-vivo-study
#1
Anoop Kumar, Dinakar Sasmal, Neelima Sharma
Deltamethrin (DLM) is a well-known pyrethroid insecticide which is widely used in the agriculture and home pest control due to restriction on the sale of organophosphate. DLM induced apoptosis is well known but its mechanism is still unclear. This study has been designed to find out its mechanism of apoptosis with the help of computational methods along with in vivo methods. The QikProp and ProTox results have shown that DLM has good oral absorption. The docking results reveal that DLM has a strong binding affinity toward the CD4, CD8, CD28 and CD45 receptors...
February 28, 2017: Drug and Chemical Toxicology
https://www.readbyqxmd.com/read/28625149/stability-indicating-reverse-phase-hplc-method-for-estimation-of-rifampicin-and-piperine-in-pharmaceutical-dosage-form
#2
Umang H Shah, Shraddha Patel, Manan Raval
BACKGROUND: High performance liquid chromatography is an integral analytical tool in assessing drug product stability. HPLC methods should be able to separate, detect, and quantify the various drug-related degradants that can form on storage or manufacturing, plus detect and any drug-related impurities that may be introduced during synthesis. OBJECTIVE: A simple, economic, selective, precise, and stability-indicating HPLC method has been developed and validated for analysis of Rifampicin (RIFA) and Piperine (PIPE) in bulk drug and in the formulation...
June 18, 2017: Current Drug Discovery Technologies
https://www.readbyqxmd.com/read/28584158/identification-of-novel-efflux-proteins-rv0191-rv3756c-rv3008-and-rv1667c-involved-in-pyrazinamide-resistance-in-mycobacterium-tuberculosis
#3
Yumeng Zhang, Jia Zhang, Peng Cui, Wenhong Zhang, Ying Zhang
Pyrazinamide (PZA) is a critical drug used for the treatment of tuberculosis (TB). PZA is a prodrug that requires conversion to the active component pyrazinoic acid (POA) by pyrazinamidase (PZase) encoded by the pncA gene. Although resistance to PZA is mostly caused by pncA mutations and less commonly by rpsA, panD, and clpC1, clinical strains without these mutations are known to exist. While efflux of POA was demonstrated in Mycobacterium tuberculosis previously, the efflux proteins involved have not been identified...
June 5, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28550736/piperine-attenuates-uv-r-induced-cell-damage-in-human-keratinocytes-via-nf-kb-bax-bcl-2-pathway-an-application-for-photoprotection
#4
Ankit Verma, Hari N Kushwaha, Ajeet K Srivastava, Saumya Srivastava, Naseem Jamal, Kriti Srivastava, Ratan Singh Ray
Chronic ultraviolet radiation (UV-R) exposure causes skin disorders like erythema, edema, hyperpigmentation, photoaging and photocarcinogenesis. Recent research trends of researchers have focused more attention on the identification and use of photo stable natural agents with photoprotective properties. Piperine (PIP), as a plant alkaloid, is an important constituent present in black pepper (Piper nigrum), used widely in ayurvedic and other traditional medicines and has broad pharmacological properties. The study was planned to photoprotective efficacy of PIP in human keratinocyte (HaCaT) cell line...
July 2017: Journal of Photochemistry and Photobiology. B, Biology
https://www.readbyqxmd.com/read/28545378/piperine-as-a-potential-anti-cancer-agent-a-review-on-preclinical-studies
#5
Azadeh Manayi, Seyed Mohammad Nabavi, William N Setzer, Samineh Jafari
Recently many studies showed anticancer activities of piperine, a pungent alkaloid found in black pepper and some other Piper species. We attempted to summarize acquired data that support anticancer potential of this natural agent. Piperine has been reported to possess effective chemopreventive activity. It has been studied to affect several mechanisms of action, in brief enhancing antioxidant system, increasing level and activity of detoxifying enzymes and suppressing stem cell self-renewal. Moreover, piperine has been found to inhibit proliferation and survival of various cancerous cell lines via modulating cell cycle progression and exhibiting anti-apoptotic activity, respectively...
May 23, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28533544/sex-specific-metabolic-profiles-of-androgens-and-its-main-binding-protein-shbg-in-a-middle-aged-population-without-diabetes
#6
Uwe Piontek, Henri Wallaschofski, Gabi Kastenmüller, Karsten Suhre, Henry Völzke, Kieu Trinh Do, Anna Artati, Matthias Nauck, Jerzy Adamski, Nele Friedrich, Maik Pietzner
The role of androgens in metabolism with respect to sex-specific disease associations is poorly understood. Therefore, we aimed to provide molecular signatures in plasma and urine of androgen action in a sex-specific manner using state-of-the-art metabolomics techniques. Our study population consisted of 430 men and 343 women, aged 20-80 years, who were recruited for the cross-sectional population-based Study of Health in Pomerania (SHIP-TREND), Germany. We used linear regression models to identify associations between testosterone, androstenedione and dehydroepiandrosterone-sulfate (DHEAS) as well as sex hormone-binding globulin and plasma or urine metabolites measured by mass spectrometry...
May 22, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28482590/sustained-drug-release-from-multi-layered-sequentially-crosslinked-electrospun-gelatin-nanofiber-mesh
#7
Anindita Laha, Chandra S Sharma, Saptarshi Majumdar
The aim of this study is to develop electrospun gelatin nanofibers based drug delivery carrier to achieve controlled and sustainable release of hydrophobic drug (piperine) for prolonged time. To accomplish this, we devised some strategies such as sandwiching the drug loaded gelatin nanofiber mesh with another gelatin nanofiber matrix without drug (acting as diffusion barrier), sequential crosslinking and finally, a combination of both. As fabricated multilayered electrospun nanofibers mesh was first characterized in terms of degradation study, morphology, drug-polymer interactions, thermal stability followed by studying their release kinetics in different physiological pH as per the gastrointestinal tract...
July 1, 2017: Materials Science & Engineering. C, Materials for Biological Applications
https://www.readbyqxmd.com/read/28467790/the-synthetic-antihyperlipidemic-drug-potassium-piperate-selectively-kills-breast-cancer-cells-through-inhibiting-g1-s-phase-transition-and-inducing-apoptosis
#8
Lifei Fan, Xuemin Cao, Huijuan Yan, Qian Wang, Xiaoxia Tian, Lan Zhang, Xiaoyan He, Gereltu Borjihan, Morigen
Piper longum L. is a well-known traditional antihyperlipidemic medicine in China, containing medicinal constituents of piperine, pipernonaline and piperlonguminine in its fruit. However, the antitumor properties of these constituents have not yet been studied. We found that potassium piperate (GBK), a derivative of piperine, inhibited proliferation of cancer cells. GBK selectively inhibited the G1-S-phase transition in breast cancer cells and the G1 arrest was correlated with induction of p27 expression, which is an inhibitor for cyclin-dependent kinases, and inhibition of cyclin A, cyclin E and cyclin B expression...
April 12, 2017: Oncotarget
https://www.readbyqxmd.com/read/28459658/enhanced-oral-bioavailability-of-domperidone-with-piperine-in-male-wistar-rats-involvement-of-cyp3a1-and-p-gp-inhibition
#9
Bhargavi Latha Athukuri, Prasad Neerati
PURPOSE: Domperidone is a commonly used antiemetic drug. The oral bioavailability of domperidone is very low due to its rapid first pass metabolism in the intestine and liver. Piperine, the main alkaloid present in black pepper has been reported to show inhibitory effects on Cytochrome P-450 (CYP-450) enzymes and P-glycoprotein (P-gp). In the present study we investigated the effect of piperine pretreatment on the intestinal transport and oral bioavailability of domperidone in male Wistar rats...
2017: Journal of Pharmacy & Pharmaceutical Sciences: a Publication of the Canadian Society for Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28458425/cardioprotective-effect-of-curcumin-and-piperine-combination-against-cyclophosphamide-induced-cardiotoxicity
#10
Manodeep Chakraborty, Ananya Bhattacharjee, Jagadish Vasudev Kamath
OBJECTIVE: Curcumin is a well-established cardioprotective phytoconstituent, but the poor bioavailability associated with it is always a matter of therapeutic challenge. The present study was undertaken to increase the therapeutic efficacy of curcumin by combining with bio-enhancer like piperine against cyclophosphamide (CP)-induced cardiotoxicity in rats. MATERIALS AND METHODS: Rats (n = 8) were treated with curcumin (200 mg/kg, p.o.) alone and different dose combination of curcumin (100, 50, 25 mg/kg, p...
January 2017: Indian Journal of Pharmacology
https://www.readbyqxmd.com/read/28449595/pharmaceutical-perspectives-of-spices-and-condiments-as-alternative-antimicrobial-remedy
#11
Savita P D'Souza, Suvarna V Chavannavar, B Kanchanashri, S B Niveditha
Medicinal values of spices and condiments are being revived by biologists through in vitro and in vivo trials providing evidence for its antimicrobial activities. The essential oils and extracts of spices like black pepper, cloves, cinnamon, and nutmeg contain active compounds like piperine, eugenol, cinnamaldehyde, and lignans. Similarly, condiments like coriander, black cumin, turmeric, garlic, and ginger are recognized for constituents like linalool, thymoquinones, curcumin, allicin, and geranial respectively...
January 1, 2017: Journal of Evidence-based Complementary & Alternative Medicine
https://www.readbyqxmd.com/read/28427563/neuroinflammation-in-alzheimer-s-disease-the-preventive-and-therapeutic-potential-of-polyphenolic-nutraceuticals
#12
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
#13
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
#14
Kathavarayan Thenmozhi, 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...
May 5, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28414236/thermal-rearrangement-of-sulfamoyl-azides-reactivity-and-mechanistic-study
#15
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.
May 5, 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
#16
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
#17
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...
May 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
#18
Tingting Gao, Haiping Xue, Lu Lu, Tong Zhang, Han Han
RATIONALE: Piperine is a major constituent of Piper nigrum L. and is a naturally bioactive alkaloid. Structural changes in piperine 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 investigated using ultra-high-performance liquid chromatography (UHLPC) combined with electrospray ionization quadruple time-of-flight tandem mass spectrometry (QTOF-MS)...
June 15, 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
#19
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
#20
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
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