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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
Sang Hoon Lee, Hyeon Young Kim, Seung Yun Back, Hyo-Kyung Han
Piperine has various pharmacological effects and can modulate the functional activity of metabolic enzymes and drug transporters. Consequently, there is a great interest in the application of piperine as an alternative medicine or bioavailability enhancer. Areas covered: This review deals with the effects of piperine on metabolizing enzymes and drug transporters. It provides the readers with an update on transporter-mediated and also metabolic enzyme-mediated piperine-drug interactions, with emphasis on its in vivo implications...
December 18, 2017: Expert Opinion on Drug Metabolism & Toxicology
Volha Zabela, Timm Hettich, Götz Schlotterbeck, Laurin Wimmer, Marko D Mihovilovic, Fabrice Guillet, Belkacem Bouaita, Bénédicte Shevchenko, Matthias Hamburger, Mouhssin Oufir
In a screening of natural products for allosteric modulators of GABAA receptors (γ-aminobutyric acid type A receptor), piperine was identified as a compound targeting a benzodiazepine-independent binding site. Given that piperine is also an activator of TRPV1 (transient receptor potential vanilloid type 1) receptors involved in pain signaling and thermoregulation, a series of piperine analogs were prepared in several cycles of structural optimization, with the aim of separating GABAA and TRPV1 activating properties...
December 2, 2017: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
Do-Young Kim, Eun-Jung Kim, Won-Gu Jang
Piperine is an alkaloid responsible for the pungency of black pepper and long pepper. It is reported to have various biological actions such as anti-oxidative and anti-inflammatory, and aids cancer prevention. Antioxidants have been shown to promote osteoblast differentiation. However, osteoblast differentiation by piperine has not yet been elucidated. Piperine-induced expression of the osteogenic genes such as distal-less homeobox 5 (Dlx5), inhibitor of DNA binding-1 (Id1), and runt-related transcription factor 2 (Runx2) was investigated using RT-PCR...
December 1, 2017: Biochemical and Biophysical Research Communications
Priyanka Dhiman, Neelam Malik, Anurag Khatkar
The computational development of human monoamine oxidase (MAO) inhibitors led to advancement in drug design and the treatment of many neurodegenerative diseases and neuropsychiatric disorders. Different natural heterocyclic structures are reported to display selective MAO inhibitory activity by preclinical and in-silico modeling. Currently, the major interest is devoted to the study of natural based therapeutic agents from the different categories. Therefore, we presenting the review to critically discuss and outline the recent advances in our knowledge on the importance of natural and natural based ligand-MAO in-silico methods for novel MAO inhibitors...
November 28, 2017: Current Neuropharmacology
Shu-Zhai Han, Hong-Xia Liu, Lin-Qing Yang, Li-de Cui, Yun Xu
Piperine (PP), an alkaloid from black and long peppers (Piper nigrum Linn &Piper longum Linn), exhibits antitumor activities in vitro and in vivo. We investigated the ability of piperine (PP) to reverse the drug resistance of human cervical cancer cells. In our study, the cervica cancer cells resistant to mitomycin-C (MMC) treatment were used. We found the growth inhibitory effects of piperine on human cervical cancer cell, which were resistant to MMC. Piperine and MMC co-treatment resulted in a dose-dependent suppression of the cell proliferation...
November 20, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
Tianjing Ren, Qianwen Wang, Chenrui Li, Mengbi Yang, Zhong Zuo
1. Piperine, the major biological active component in black pepper has been associated with miscellaneous pharmacological effects, especially on central nervous system. To correlates with its neurological activity, a comprehensive pharmacokinetic profile of piperine in brain, plasma and cerebrospinal fluid after oral administration in rats was investigated in the current study. 2. It was noted that piperine could efficiently penetrate and homogeneously distribute into brain with similar pharmacokinetics profiles in each region...
November 21, 2017: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
Gopichand Chinta, Mohane Selvaraj Coumar, Latha Periyasamy
Background: Piperine was widely used in traditional medicine for inducing sterility and abortion. Objective: To evaluate the effect of the piperine on testis of male albino rats. Materials and Methods: Adult male rats were divided into four groups (n = 12). Group I (control): Rats were given vehicle p.o. i.e. 0.5% carboxymethyl cellulose in normal saline daily for 60 days, Group II (ED): Rats received piperine at a dose of 10 mg/kg body weight (b...
October 2017: Pharmacognosy Magazine
Mohamed A Morsy, Azza A K El-Sheikh, Ahmed R N Ibrahim, Mohammed A Khedr, Abdulla Y Al-Taher
To investigate compound-protein binding mode and molecular dynamic simulation of P-glycoprotein (P-gp), in silico studies were performed to compare 12 naturally occurring compounds using two softwares. The net results showed that piperine (PIP) had the best binding affinity. In vitro studies on doxorubicin (DOX)-resistant NCI/ADR-RES cells, known to express P-gp, showed that, dose-dependently, PIP significantly increased intracellular accumulation of rhodamine-123 and had cytotoxic effects accessed by MTT assay...
November 11, 2017: European Journal of Pharmaceutical Sciences
Irena Philipova, Violeta Valcheva, Rositsa Mihaylova, Mina Mateeva, Irini Doytchinova, Georgi Stavrakov
Piperine amide analogues are synthesized by replacement of the piperidine moiety with different types of cyclic amines, including adamantyl and monoterpene derived fragments. The compounds are screened for activity against Mycobacterium tuberculosis H37Rv. The most potent compounds are the 1-adamantyl and the monoterpene derived hybrids, which combine nanomolar antimycobacterial activity with low cytotoxicity against human cells. The presence of quaternary carbon atom as main structural requirement for anti-TB activity is pointed out by a QSAR study...
November 11, 2017: Chemical Biology & Drug Design
Chang Yang, Shou-Ying Du, Jie Bai, Peng-Yue Li, Ya-Hua Cui, Bing Yang
To establish a determination method for the contents of paeonol, eugenol and piperine in receptor liquid and to research the transdermal permeability of Huoxue Zhitong patch. The contents of paeonol, eugenol and piperine in receptor liquid were determined by high pressure liquid chromatography(HPLC); and the receptor liquid was optimized by taking accumulative amount penetrated within 24 hours, percutaneous permeation rate and skin irritation as indexes. In vitro Franz diffusion experiment was applied to assess the percutaneous penetration characteristics and regularity of Huoxue Zhitong patch...
April 2017: Zhongguo Zhong Yao za Zhi, Zhongguo Zhongyao Zazhi, China Journal of Chinese Materia Medica
Toshinari Ezawa, Yutaka Inoue, Isamu Murata, Koichi Takao, Yoshiaki Sugita, Ikuo Kanamoto
In this study, the physicochemical properties and solubility of inclusion complexes of ground mixtures (GMs) of piperine (PP), a pungent ingredient of pepper, with α- and γ-cyclodextrin (CD) were studied. From the solubility results, the PP/αCD inclusion molar ratio was determined to be 1/2, while that of PP/γCD was 1/1, according to the AP-type phase diagram of PP/αCD and the BS-type one of PP/γCD. The powder X-ray diffraction and differential scanning calorimetry analyses confirmed the formation of GM complexes with molar ratios of PP/αCD = 1/2 and PP/γCD = 1/1...
October 25, 2017: AAPS PharmSciTech
Susan J Hewlings, Douglas S Kalman
Turmeric, a spice that has long been recognized for its medicinal properties, has received interest from both the medical/scientific world and from culinary enthusiasts, as it is the major source of the polyphenol curcumin. It aids in the management of oxidative and inflammatory conditions, metabolic syndrome, arthritis, anxiety, and hyperlipidemia. It may also help in the management of exercise-induced inflammation and muscle soreness, thus enhancing recovery and performance in active people. In addition, a relatively low dose of the complex can provide health benefits for people that do not have diagnosed health conditions...
October 22, 2017: Foods (Basel, Switzerland)
Young Sook Yun, Sachie Noda, Shigeru Takahashi, Yuji Takahashi, Hideshi Inoue
Black pepper (Piper nigrum) contains a variety of alkamides. Among them, piperine has been reported to have antidepressant-like effects in chronically stressed mice, but little is known about the biological activity of other alkamides. In this study, we investigated the effects of alkamides from white pepper (P. nigrum) on neuronal cells. Twelve alkamides were isolated from white pepper MeOH extracts, and their chemical structures were identified by NMR and MS analyses. The compounds were subjected to assays using the luciferase-reporter gene under the control of the BDNF promoter or cAMP response element in mouse neuroblastoma Neuro-2a cells...
October 23, 2017: Journal of Natural Medicines
Shamsher Singh, Puneet Kumar
Parkinson's disease (PD) is a multifactorial neurological disorder caused by selective dopaminergic neuronal loss. Quercetin (QC) in combination with piperine (bioenhancer) acts as potential antioxidant, anti-inflammatory and neuroprotective against 6-OHDA rat model of PD. Rats were injected 6-OHDA (8μg/2μl, saline) unilaterally, intranigrally once into right SNpc. Pre-treatment with QC (25 and 50mg/kg, p.o.) alone and combination of QC (25mg/kg, p.o.) with piperine (2.5mg/kg, p.o.) were given for 14days starting from 8th day of 6-OHDA infusion...
October 19, 2017: Neuroscience Research
Elizeu S Farias, Eliete M P Silva, Milena G Teixeira, Jhulyana S Ferreira, Elson S Alvarenga, Marcelo C Picanço
In this study, the insecticide potential of eight phthalides derived from furan-2(5H)-one was evaluated against Tuta absoluta (Meyrick) (Lepidoptera: Gelechiidae) larvae. The potency of the most active phthalides and the susceptibility of six different T. absoluta populations to these compounds were determined. The toxicity of these molecules to two non-target species (Solenopsis saevissima Smith and Tetragonisca angustula Latreille) was also evaluated. Two phthalides (3 and 4) presented insecticide potential against T...
October 16, 2017: Journal of Environmental Science and Health. Part. B, Pesticides, Food Contaminants, and Agricultural Wastes
Jonathan Cheong, Jason S Halladay, Jasleen K Sodhi, Emile Plise, Laurent Salphati
BACKGROUND: Non-selective chemical inhibitors of phase I and phase II enzymes are commonly used in in vitro metabolic studies to elucidate the biotransformation pathways of drugs. However, the inhibition of the inhibitors on efflux and uptake transporters is not well investigated, potentially leading to unexpected and ambiguous results in these studies. OBJECTIVE: The commonly used metabolizing enzyme inhibitors, 1-aminobenzotriazole (ABT), SKF-525A, pargyline, allopurinol, menadione, methimazole, piperine and raloxifene, were examined for their potential inhibition of the major hepatic ABC (ATP binding cassette) and SLC (solute carrier) transporters...
October 10, 2017: Drug Metabolism Letters
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