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Piperine

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https://www.readbyqxmd.com/read/28918329/an-integrated-strategy-for-rapid-discovery-and-identification-of-the-sequential-piperine-metabolites-in-rats-using-ultra-high-performance-liquid-chromatography-high-resolution-mass-spectrometery
#1
Zhanpeng Shang, Wei Cai, Yanfeng Cao, Fei Wang, Zhibin Wang, Jianqiu Lu, Jiayu Zhang
Piperine, one of the major bioactive constituents isolated from natural flavorings and medicinal-culinary herbs, possesses various biological activities. In the present study, an integrated strategy based on ultra high-performance liquid chromatography/high resolution mass spectrometry was established to reveal piperine metabolism in rats. First of all, post-acquisition data-mining methods, including high resolution extracted ion chromatograms (HREICs) and multiple mass defect filtering (MMDF), were used to screen piperine metabolite candidates in a full-scan HRMS(1) level...
September 9, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28890215/piperine-pro-nanolipospheres-as-a-novel-oral-delivery-system-of-cannabinoids-pharmacokinetic-evaluation-in-healthy-volunteers-in-comparison-to-buccal-spray-administration
#2
Irina Cherniakov, Dvora Izgelov, Dinorah Barasch, Elyad Davidson, Abraham J Domb, Amnon Hoffman
Nowadays, therapeutic indications for cannabinoids, specifically Δ(9)-tetrahydrocannabinol (THC) and Cannabidiol (CBD) are widening. However, the oral consumption of the molecules is very limited due to their highly lipophilic nature that leads to poor solubility at the aqueous environment. Additionally, THC and CBD are prone to extensive first pass mechanisms. These absorption obstacles render the molecules with low and variable oral bioavailability. To overcome these limitations we designed and developed the advanced pro-nanolipospheres (PNL) formulation...
September 8, 2017: Journal of Controlled Release: Official Journal of the Controlled Release Society
https://www.readbyqxmd.com/read/28885721/targeting-intracellular-staphylococcus-aureus-to-lower-recurrence-of-orthopaedic-infection
#3
Devendra H Dusane, Douglas Kyrouac, Iris Petersen, Luke Bushrow, Jason H Calhoun, Jeffrey F Granger, Laura S Phieffer, Paul Stoodley
Staphylococcus aureus is often found in orthopaedic infections and may be protected from commonly prescribed antibiotics by forming biofilms or growing intracellularly within osteoblasts. To investigate the effect of non-antibiotic compounds in conjunction with antibiotics to clear intracellular and biofilm forming S. aureus causing osteomyelitis. SAOS-2 osteoblast-like cell lines were infected with S. aureus BB1279. Antibiotics (vancomycin, VAN; and dicloxacillin, DICLOX), bacterial efflux pump inhibitors (piperine, PIP; carbonyl cyanide m-chlorophenyl hydrazone, CCCP) and bone morphogenetic protein (BMP-2) were evaluated individually and in combination to kill intracellular bacteria...
September 8, 2017: Journal of Orthopaedic Research: Official Publication of the Orthopaedic Research Society
https://www.readbyqxmd.com/read/28852397/neuroprotective-potential-of-quercetin-in-combination-with-piperine-against-1-methyl-4-phenyl-1-2-3-6-tetrahydropyridine-induced-neurotoxicity
#4
Shamsher Singh, Sumit Jamwal, Puneet Kumar
1-Methy-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) is a neurotoxin that selectively damages dopaminergic neurons in the substantia nigra pars compacta and induces Parkinson's like symptoms in rodents. Quercetin (QC) is a natural polyphenolic bioflavonoid with potent antioxidant and anti-inflammatory properties but lacks of clinical attraction due to low oral bioavailability. Piperine is a well established bioavailability enhancer used pre-clinically to improve the bioavailability of antioxidants (e.g., Quercetin)...
July 2017: Neural Regeneration Research
https://www.readbyqxmd.com/read/28830793/piperine-inhibits-aflatoxin-b1-production-in-aspergillus-flavus-by-modulating-fungal-oxidative-stress-response
#5
Isaura Caceres, Rhoda El Khoury, Sylviane Bailly, Isabelle P Oswald, Olivier Puel, Jean-Denis Bailly
Aspergillus flavus, a soil-borne pathogen, represents a danger for humans and animals since it produces the carcinogenic mycotoxin Aflatoxin B1 (AFB1). Approaches aiming the reduction of this fungal contaminant mainly involve chemicals that may also be toxic. Therefore, identification and characterization of natural anti-aflatoxigenic products represents a sustainable alternative strategy. Piperine, a major component of black and long peppers, has been previously demonstrated asan AFB1-inhibitor; nevertheless its mechanism of action was yet to be elucidated...
October 2017: Fungal Genetics and Biology: FG & B
https://www.readbyqxmd.com/read/28801675/targeting-p-glycoprotein-investigation-of-piperine-analogs-for-overcoming-drug-resistance-in-cancer
#6
Safiulla Basha Syed, Hemant Arya, I-Hsuan Fu, Teng-Kuang Yeh, Latha Periyasamy, Hsing-Pang Hsieh, Mohane Selvaraj Coumar
P-glycoprotein (P-gp) is a drug transporter that effluxes chemotherapeutic drugs and is implicated in the development of resistance of cancer cells to chemotherapeutic drugs. To date, no drug has been approved to inhibit P-gp and restore chemotherapy efficacy. Moreover, majority of the reported inhibitors have high molecular weight and complex structures, making it difficult to understand the basic structural requirement for P-gp inhibition. In this study, two structurally simple, low molecular weight piperine analogs Pip1 and Pip2 were designed and found to better interact with P-gp than piperine in silico...
August 11, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28799699/a-comparative-study-on-the-therapeutic-effect-of-trpv1-trpa1-and-trpm8-agonists-on-swallowing-dysfunction-associated-with-aging-and-neurological-diseases
#7
D Alvarez-Berdugo, L Rofes, V Arreola, A Martin, L Molina, P Clavé
BACKGROUND: Oropharyngeal sensory impairment is a potential target to treat swallowing dysfunction in patients with oropharyngeal dysphagia (OD). AIM: To assess the therapeutic effect of stimulating oropharyngeal sensory afferents with TRPV1, TRPA1, or TRPM8 agonists vs increasing bolus viscosity in older and neurologic patients with OD by comparing four studies of similar experimental design. METHODS: Swallow function of 142 older patients with impaired safety of swallow at nectar ([50-350] mPa·s) viscosity was evaluated with videofluoroscopy (VFS) while treated with TRPV1 (150 μmol/L), TRPV1/A1 (150 μmol/L and 1 mmol/L), or TRPM8 (1 mmol/L or 10 mmol/L) agonists or modified starch (MS) at spoon thick viscosity (>1750 mPa·s)...
August 11, 2017: Neurogastroenterology and Motility: the Official Journal of the European Gastrointestinal Motility Society
https://www.readbyqxmd.com/read/28764063/hard-cap-espresso-extraction-and-liquid-chromatography-determination-of-bioactive-compounds-in-vegetables-and-spices
#8
María Teresa Martinez-Sena, Miguel de la Guardia, Francesc A Esteve-Turrillas, Sergio Armenta
A new analytical procedure, based on liquid chromatography with diode array and fluorescence detection, has been proposed for the determination of bioactive compounds in vegetables and spices after hard cap espresso extraction. This novel extraction system has been tested for the determination of capsaicin and dihydrocapsaicin from fresh chilli and sweet pepper, piperine from ground pepper, curcumin from turmeric and curry, and myristicin from nutmeg. Extraction efficiency was evaluated by using acetonitrile:water and ethanol:water mixtures...
December 15, 2017: Food Chemistry
https://www.readbyqxmd.com/read/28739698/highly-eribulin-resistant-kbv20c-oral-cancer-cells-can-be-sensitized-by-co-treatment-with-the-third-generation-p-glycoprotein-inhibitor-elacridar-at-a-low-dose
#9
Yujin Park, Ji-Yeon Son, Byung-Mu Lee, Hyung Sik Kim, Sungpil Yoon
BACKGROUND/AIM: Eribulin mesylate, also called Halaven® (HAL), was recently developed as a microtubule-targeting drug and is used in the clinic for resistant or metastatic cancer. Previously, we showed that P-glycoprotein (P-gp)-overexpressing KBV20C oral cancer cells are highly resistant to HAL compared to sensitive KB cells. This qualitative study was designed to identify specific P-gp inhibitors that increase the sensitivity of highly resistant cancer cells to HAL. MATERIALS AND METHODS: In order to identify functional P-gp inhibitors, HAL-treated KBV20C cells were co-treated with P-gp inhibitors, verapamil, elacridar, cyclosporine A, mitotane, piperine, fumagillin, curcumin, indomethacin, probenecid, sulindac, tesmilifene, and C-4...
August 2017: Anticancer Research
https://www.readbyqxmd.com/read/28736128/the-effect-of-pro-nanolipospheres-pnl-formulation-containing-natural-absorption-enhancers-on-the-oral-bioavailability-of-delta-9-tetrahydrocannabinol-thc-and-cannabidiol-cbd-in-a-rat-model
#10
Irina Cherniakov, Dvora Izgelov, Abraham J Domb, Amnon Hoffman
The lipophilic phytocannabinoids cannabidiol (CBD) and Δ(9)-tetrahydrocannabinol (THC) show therapeutic efficacy in various medical conditions. Both molecules are poorly water soluble and subjected to extensive first pass metabolism in the gastrointestinal tract, leading to a limited oral bioavailability of approximately 9%. We have developed an advanced lipid based Self-Emulsifying Drug Delivery System termed Advanced Pro-NanoLiposphere (PNL) pre-concentrate. The PNL is composed of lipid and emulsifying excipients of GRAS status and are known to increase solubility and reduce Phase I metabolism of lipophilic active compounds...
July 20, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28735818/curcuminoids-modify-lipid-profile-in-type-2-diabetes-mellitus-a-randomized-controlled-trial
#11
RANDOMIZED CONTROLLED TRIAL
Yunes Panahi, Nahid Khalili, Ebrahim Sahebi, Soha Namazi, Željko Reiner, Muhammed Majeed, Amirhossein Sahbekar
BACKGROUND: Type 2 diabetes (T2D) is an established risk factor for cardiovascular disease (CVD) and is associated with disturbed metabolism of lipids and lipoproteins. Curcuminoids are natural products with anti-diabetic and lipid-modifying actions but their efficacy in improving dyslipidemia in diabetic individuals has not been sufficiently studied. OBJECTIVE: To investigate the efficacy of supplementation with curcuminoids, plus piperine as an absorption enhancer, in improving serum lipids in patients with T2D...
August 2017: Complementary Therapies in Medicine
https://www.readbyqxmd.com/read/28694780/the-effect-of-pungent-and-tingling-compounds-from-piper-nigrum-l-on-background-k-currents
#12
Leopoldo R Beltrán, Corinna Dawid, Madeline Beltrán, Janina Levermann, Sascha Titt, Sini Thomas, Viktoria Pürschel, Miriam Satalik, Günter Gisselmann, Thomas Hofmann, Hanns Hatt
Black peppercorns (Piper nigrum L.) elicit a pungent and tingling oral impression. Their pungency is partially explained by the agonist activity of some of their active principles, especially piperine, on TRP channels. However, we recently showed that piperine, as well as other pungent compounds, also possess a marked effect on two-pore domain (KCNK, K2P) K(+) channels. Members of this family play a key role in maintaining the resting membrane potential of excitable cells. Interestingly, tingling compounds have been shown to induce neuronal excitation by inhibiting KCNK channels...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28680454/piperine-enhances-carbohydrate-fat-metabolism-in-skeletal-muscle-during-acute-exercise-in-mice
#13
Jisu Kim, Kang-Pa Lee, Dae-Won Lee, Kiwon Lim
BACKGROUND: Exercise promotes energy metabolism (e.g., metabolism of glucose and lipids) in skeletal muscles; however, reactive oxygen species are also generated during exercise. Various spices have been reported to have beneficial effects in sports medicine. Here, we investigated the effects of piperine, an active compound in black pepper, to determine its effects on metabolism during acute endurance exercise. METHODS: ICR mice (n = 18) were divided into three groups: nonexercise (CON), exercise (EX), and exercise with piperine (5 mg/kg) treatment (EP)...
2017: Nutrition & Metabolism
https://www.readbyqxmd.com/read/28678344/prebiotic-potential-and-chemical-composition-of-seven-culinary-spice-extracts
#14
Qing-Yi Lu, Paula H Summanen, Ru-Po Lee, Jianjun Huang, Susanne M Henning, David Heber, Sydney M Finegold, Zhaoping Li
The objective of this study was to investigate prebiotic potential, chemical composition, and antioxidant capacity of spice extracts. Seven culinary spices including black pepper, cayenne pepper, cinnamon, ginger, Mediterranean oregano, rosemary, and turmeric were extracted with boiling water. Major chemical constituents were characterized by RP-HPLC-DAD method and antioxidant capacity was determined by measuring colorimetrically the extent to scavenge ABTS radical cations. Effects of spice extracts on the viability of 88 anaerobic and facultative isolates from intestinal microbiota were determined by using Brucella agar plates containing serial dilutions of extracts...
July 5, 2017: Journal of Food Science
https://www.readbyqxmd.com/read/28671634/regressions-of-breast-carcinoma-syngraft-following-treatment-with-piperine-in-combination-with-thymoquinone
#15
Wamidh H Talib
Thymoquinone (TQ) and piperine, the active ingredients in cumin (Nigella sativa) and black pepper (Piper longum), respectively, exhibit various bioactivities including anticancer effects. The aim of the present study is to investigate the antineoplastic activity of a combination of TQ and piperine against breast cancer implanted in mice. The antiproliferative effects of TQ, piperine, and a combination of both agents were tested against mouse epithelial breast cancer cell line (EMT6/P) using MTT assay. The isobolographic method was used to calculate the combination index (CI)...
July 3, 2017: Scientia Pharmaceutica
https://www.readbyqxmd.com/read/28671328/electrostimulated-release-of-neutral-drugs-from-polythiophene-nanoparticles-smart-regulation-of-drug-polymer-interactions
#16
Anna Puiggalí-Jou, Paolo Micheletti, Francesc Estrany, Luis J Del Valle, Carlos Alemán
Poly(3,4-ethylenedioxythiophene) (PEDOT) nanoparticles are loaded with curcumin and piperine by in situ emulsion polymerization using dodecyl benzene sulfonic acid both as a stabilizer and a doping agent. The loaded drugs affect the morphology, size, and colloidal stability of the nanoparticles. Furthermore, kinetics studies of nonstimulated drug release have evidenced that polymer···drug interactions are stronger for curcumin than for piperine. This observation suggests that drug delivery systems based on combination of the former drug with PEDOT are much appropriated to show an externally tailored release profile...
July 3, 2017: Advanced Healthcare Materials
https://www.readbyqxmd.com/read/28669317/effect-of-piperine-on-the-bioavailability-and-pharmacokinetics-of-rosmarinic-acid-in-rat-plasma-using-uplc-ms-ms
#17
Jun-Hui Yang, Kun-Jun Mao, Ping Huang, Yin-Jun Ye, Hua-Shan Guo, Bao-Chang Cai
1. The purpose of the present study was to investigate the effect of piperine (PP) on the pharmacokinetics of rosmarinic acid (RA) in rat plasma and to determine whether PP could enhance the oral bioavailability of RA via inhibition of its glucuronidation. 2. The pharmacokinetic profiles of RA between oral administration of RA (50 mg/kg) alone and in combination with different oral dose PP (20, 40, 60, and 80 mg/kg) to rats were investigated via a validated UPLC/MS/MS method. 3. The AUC and Cmax of RA were significantly increased in combination with different dose PP dose dependently, especially in the presence of 60 and 80 mg/kg PP (p < 0...
July 3, 2017: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/28641526/biology-oriented-synthesis-bios-of-piperine-derivatives-and-their-comparative-analgesic-and-antiinflammatory-activities
#18
Ammar Yasir, Saiqa Ishtiaq, Muhammad Jahangir, Muhammad Ajaib, Uzma Salar, Khalid Mohammed Khan
BACKGROUND: Serious side effects such as gastric intestinal ulcer, bleeding etc. are associated with most of the antiinflammatory and analgesic drugs. So there is a need to search novel, potent, and safer antiinflammatory and analgesic drug. METHOD: Based on "biology-oriented synthesis approach", piperine alkaloid was isolated from Piper nigrum L. and some derivatives of piperine having azomethine, sulfamoyl, propanoyl, acetamoyl and heterocyclic oxadiazole were synthesized...
June 22, 2017: Medicinal Chemistry
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
#19
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
#20
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
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