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Yücel Baspinar, Mehmet Üstündas, Oguz Bayraktar, Canfeza Sezgin
Curcumin as the active compound of turmeric has antioxidative, antiinflammatory, antimicrobial and anticancer properties among others. However, its disadvantageous properties like low solubility, poor bioavailability and rapid degradation under neutral or alkaline pH conditions or when exposed to light limit its clinical application. These problems can be solved by a smart combination of using a natural enhancer like piperine and preparing nanoparticles by a proper method like electrospray. Due to these facts it was aimed in this study to develop curcumin and piperine loaded zein-chitosan nanoparticles step by step...
March 2018: Saudi Pharmaceutical Journal: SPJ: the Official Publication of the Saudi Pharmaceutical Society
Nick Zwart, Shan Li Nio, Corine J Houtman, Jacob De Boer, Jeroen Kool, Timo Hamers, Marja H Lamoree
Effect-Directed Analysis (EDA) is a commonly used approach for effect-based identification of endocrine disruptive chemicals in complex (environmental) mixtures. For routine toxicity assessment of e.g. water samples however, current EDA approaches are considered time consuming and laborious. We achieved faster EDA and identification, by downscaling of sensitive cell-based hormone reporter gene assays and increasing fractionation resolution to allow testing of smaller fractions with reduced complexity. The high-resolution EDA approach is demonstrated by analysis of four environmental passive sampler extracts...
March 16, 2018: Environmental Science & Technology
Behjat Javadi
Cancer is the second leading cause of death with profound socio-economic consequences worldwide. Growing evidence suggests the crucial role of diet on cancer prevention and treatment. In Traditional Persian Medicine (TPM) there is a major focus on contribution of special diet and foods to cancer management. In the present article, the cytotoxic and antitumor activities of several food items including plants and animal products recommended by TPM as anticancer agents are discussed. Strong evidence supports the anticancer effects of beetroot (Beta vulgris) and its major compound betanin, cinnamon and cinnamaldehyde, barley (H...
March 15, 2018: Nutrition and Cancer
Dvora Izgelov, Irina Cherniakov, Gefen Aldouby Bier, Abraham J Domb, Amnon Hoffman
In recent years, Phase II metabolism, as a first pass metabolism process occurring to the parent drug, is gaining more and more attention. This is due to its acknowledged significance in drug development as well as drug-drug interactions. However, the predominant role of Phase I metabolism has always overshadowed Phase II metabolism, resulting in insufficient data regarding its mechanisms. In this paper, we investigate the effect of an advanced lipid based drug delivery system on Phase II metabolism at the intestinal level of the enterocytes monolayer...
March 14, 2018: Molecular Pharmaceutics
Nagamalai Vasimalai, Vânia Vilas-Boas, Juan Gallo, María de Fátima Cerqueira, Mario Menéndez-Miranda, José Manuel Costa-Fernández, Lorena Diéguez, Begoña Espiña, María Teresa Fernández-Argüelles
Carbon dots have demonstrated great potential as luminescent nanoparticles in bioapplications. Although such nanoparticles appear to exhibit low toxicity compared to other metal luminescent nanomaterials, today we know that the toxicity of carbon dots (C-dots) strongly depends on the protocol of fabrication. In this work, aqueous fluorescent C-dots have been synthesized from cinnamon, red chilli, turmeric and black pepper, by a one-pot green hydrothermal method. The synthesized C-dots were firstly characterized by means of UV-vis, fluorescence, Fourier transform infrared and Raman spectroscopy, dynamic light scattering and transmission electron microscopy...
2018: Beilstein Journal of Nanotechnology
Hanmei Li, Sonja Krstin, Shihui Wang, Michael Wink
BACKGROUND: Multidrug resistance (MDR) can develop in cancer cells after treatment with anticancer drugs, mainly due to the overexpression of the ATP-binding cassette (ABC) transporters. We analyzed the ability of two pungent-tasting alkaloids-capsaicin and piperine from Capsicum frutescens and Piper nigrum , respectively-to reverse multidrug resistance in the cancer cell lines Caco-2 and CEM/ADR 5000, which overexpress P-glycoprotein (P-gp) and other ABC transporters. METHODS: The MTT assay was first used to determine the cytotoxicity of doxorubicin, the alkaloids, and digitonin alone, and then their combinations...
March 2, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Rafiq A Rather, Madhulika Bhagat
Cancer is a genetic disease characterized by unregulated growth and dissemination of malignantly transformed neoplastic cells. The process of cancer development goes through several stages of biochemical and genetic alterations in a target cell. Several dietary alkaloids have been found to inhibit the molecular events and signaling pathways associated with various stages of cancer development and therefore are useful in cancer chemoprevention. Cancer chemoprevention has long been recognized as an important prophylactic strategy to reduce the burden of cancer on health care system...
2018: Frontiers in Cell and Developmental Biology
Yuan Zeng, Ying Yang
Piperine, an alkaloid derived from natural products, has been demonstrated to exert antitumor activities in vivo and in vitro. However, its anti‑tumor effect has not yet been illustrated in the prostate cancer (PCa) metastatic process. Thus, the present study explored the influence of piperine on PCa and the underlying molecular mechanism. Cell migration was detected via the Transwell chamber model. Total protein was identified by western blot analysis. The data revealed that piperine markedly repressed cell proliferation and migration, and induced apoptosis in PCa DU145...
February 28, 2018: Molecular Medicine Reports
Yunes Panahi, Nahid Khalili, Ebrahim Sahebi, Soha Namazi, Luis E Simental-Mendía, Muhammed Majeed, Amirhossein Sahebkar
INTRODUCTION: Curcuminoids have been shown to reduce glycemia and related complications in diabetes. In the present study, we evaluated the impact of curcuminoids plus piperine administration on glycemic, hepatic and inflammatory biomarkers in type 2 diabetes (T2D) patients. METHODS: T2D patients aged 18-65 years were enrolled in a randomized double-blind placebo-controlled trial and randomly allocated to standard-of-care treatment and dietary advises plus either curcuminoids (daily dose of 500 mg/day co-administered with piperine 5 mg/day) or placebo for a period of 3 months...
February 19, 2018: Drug Research
Zhao-Hui Jin, Wen Qiu, Hui Liu, Xue-Hua Jiang, Ling Wang
Ginsenoside Rh2 (Rh2) is one of the major bioactive ginsenosides in Panax ginseng. However, the oral bioavailability of Rh2 is low, with P-glycoprotein (P-gp) and CYP3A4 being reported to be the main factors. The purpose of the present study was to determine the enhancing effect of piperine on the oral bioavailability as well as bioactivity of Rh2. The inhibitory effect of piperine on P-gp and CYP3A4 was determined using a Caco-2 monolayer model and a recombinant CYP3A4 metabolic system, respectively. The pharmacokinetics of oral Rh2 (10 mg·kg-1 ) administered alone or in combination with piperine (10 and 20 mg·kg-1 ) was performed in rats...
February 2018: Chinese Journal of Natural Medicines
Taiki Miyazawa, Kiyotaka Nakagawa, Sharon H Kim, Michael J Thomas, Ligi Paul, Jean-Marc Zingg, Gregory G Dolnikowski, Susan B Roberts, Fumiko Kimura, Teruo Miyazawa, Angelo Azzi, Mohsen Meydani
Background: Dietary bioactive compounds capable of improving metabolic profiles would be of great value, especially for overweight individuals undergoing a caloric restriction (CR) regimen. Curcumin (Cur), a possible anti-obesity compound, and piperine (Pip), a plausible enhancer of Cur's bioavailability and efficacy, may be candidate agents for controlling body fat, metabolism and low grade inflammation. Methods: 47 eight-week-old male C57BL/6 mice were fed a high fat diet (HFD) for 23 weeks to induce obesity...
2018: Nutrition & Metabolism
Chenrui Li, Zhijun Wang, Qian Wang, Rebecca Lucinda Ka Yan Ho, Ying Huang, Moses S S Chow, Christopher Wai Kei Lam, Zhong Zuo
Docetaxel (DTX) is widely used for metastatic castrated resistant prostate cancer, but its efficacy is often compromised by drug resistance associated with low intracellular concentrations. Piperine (PIP) could enhance the bioavailability of other drugs via the inhibition of CYPs and P-gp activities. Thus, we hypothesize a positive effect with the DTX-PIP combination on the anti-tumor efficacy and intra-tumor DTX concentrations in taxane-resistant prostate cancer. ICR-NOD/SCID mice implanted with taxane-resistant human prostate cancer cells were administrated with saline as well as PIP and DTX separately or in combination...
January 9, 2018: Oncotarget
Tae Hwan Kim, Soyoung Shin, Sun Dong Yoo, Beom Soo Shin
Pungent spice constituents such as piperine, capsaicin and [6]-gingerol consumed via daily diet or traditional Chinese medicine, have been reported to possess various pharmacological activities. These dietary phytochemicals have also been reported to inhibit P-glycoprotein (P-gp) in vitro and act as an alternative to synthetic P-gp modulators. However, the in vivo effects on P-gp inhibition are currently unknown. This study aimed to test the hypothesis that phytochemical P-gp inhibitors, i.e., piperine, capsaicin and [6]-gingerol, modulate the in vivo tissue distribution of doxorubicin, a representative P-gp substrate...
February 7, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Emma R Collings, M Carmen Alamar Gavidia, Katherine Cools, Sally Redfern, Leon A Terry
Application of UV-C has been shown to enhance the biochemical profile of various plant materials. This could be used to increase biochemical load, reducing the amount of material required but still impart equivalent flavour. As spices, such as black pepper (Piper nigrum L.), are typically dried to low moisture content to create a stable product for transportation and storage, little work has explored the use of modern postharvest treatments to enhance flavour. In this work, fresh P. nigrum berries were exposed to four UV-C doses (0, 1, 5 and 15 kJ m-2) and subsequently stored at 5 °C for ca...
February 2018: Postharvest Biology and Technology
Jifeng Guo, Yiting Cui, Qiong Liu, Yang Yang, Yujing Li, Ling Weng, Beisha Tang, Peng Jin, Xiao-Jiang Li, Su Yang, Shihua Li
BACKGROUND: Spinocerebellar ataxia 17 (SCA17) belongs to the family of neurodegenerative diseases caused by polyglutamine (polyQ) expansion. In SCA17, polyQ expansion occurs in the TATA box binding protein (TBP) and leads to the misfolding of TBP and the preferential degeneration in the cerebellar Purkinje neurons. Currently there is no effective treatment for SCA17. Mesencephalic astrocyte-derived neurotrophic factor (MANF) is a recently identified neurotrophic factor, and increasing MANF expression ameliorated SCA17 neuropathology in TBP-105Q knock-in (KI) mouse model, indicating that MANF could be a therapeutic target for treating SCA17...
January 30, 2018: Molecular Neurodegeneration
Shengli Han, Yanni Lv, Liyun Kong, Yueming Sun, Jia Fu, Lingjun Li, Langchong He
Traditional Chinese medicine (TCM) has been used for prevention and treatment of various diseases for many decades. TCM injection is a new dosage form, with incidence of anaphylactoid reactions increasing every year. In this study, the rat basophilic leukemia 2H3 (RBL-2H3) and laboratory of allergic disease 2 (LAD2) dual-mixed/CMC was established and was coupled with an HPLC-ESI-IT-TOF-MS system to identify the potential allergenic components in Haqing injection. Cinobufagin, piperine, osthole, praeruptorin A, and schizandrin A were screened from Haqing injection via this coupled system...
January 22, 2018: Electrophoresis
Vasanti M Suvarna, Preeti C Sangave
Darunavir ethanolate (DRV) is an efficient protease inhibitor (PI) used in the treatment of human immunodeficiency virus (HIV) type-1 patients. An isocratic reversed-phase HPLC method was developed to monitor concentration of darunavir in in vitro intestinal fluid samples in everted sac absorption model in the presence of bioenhancers, viz., piperine, quercetin, naringenin. The method was validated and successfully applied to everted sac and pharmacokinetic studies in rats. The absorption profiles of DRV and apparent permeability coefficients were determined...
January 12, 2018: Journal of Chromatographic Science
Naresh Patel, K Jagannath, Agam Vora, Mukesh Patel, Anand Patel
Background: The overall goals for treatment of Tuberculosis (TB) are to cure individual patient and to minimize the transmission of Mycobacterium tuberculosis. At the time of study conduction, the standard treatment for newly diagnosed tuberculosis patients consisted of an intensive phase for two months with four drugs (HRZE), followed by continuation phase for four months with two drugs (HR). Rifampicin, which is very effective against Mycobacterium tuberculosis, in both the phases of treatment, has certain concerns, which includes, decreased bioavailability with chronic use and hepatotoxicity...
September 2017: Journal of the Association of Physicians of India
Amirhossein Sahebkar, Yunes Panahi, Nahid Khalili, Ebrahim Sahebi, Soha Namazi, Stephen L Atkin, Muhammed Majeed
OBJECTIVE: Curcumin is a naturally occurring polyphenol derived from tumeric that has been reported to have anti-inflammatory properties with effects on adipokine and ghrelin levels. Adiponectin, leptin and ghrelin modulate energy homeostasis but each have modulatory effects on inflammatory cytokines and the immune system. Therefore this analysis was performed to investigate the effect of curcumin on adiponectin, leptin and ghrelin. METHODS: A double blind randomised control trial comparing curcumin 1000mg with 10mg of piperine daily to placebo over a 12 week period...
January 3, 2018: Current Clinical Pharmacology
Sri Agus Sudjarwo, Koerniasari Eraiko, Giftania Wardani Sudjarwo, Koerniasari
Objectives: In this study, we investigated the protective effects of piperine on lead acetate-induced renal damage in rat kidney tissue. Materials and Methods: Forty male rats were divided into 5 groups: negative control (rats were given aquadest daily), positive control (rats were given lead acetate 30 mg/kg BW orally once a day for 60 days), and the treatment group (rats were given piperine 50 mg; 100 mg and 200 mg/kg BW orally once a day for 65 days, and on 5th day, were given lead acetate 30 mg/kg BW one hr after piperine administration for 60 days)...
November 2017: Iranian Journal of Basic Medical Sciences
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