Topic
Piperlonguminine
About: Piperlonguminine is a research topic. Over the lifetime, 106 publications have been published within this topic receiving 3046 citations.
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TL;DR: It can be stated that CEPC, piperovatine, and FRPI showed promising in vitro results for the development of new drugs, and further studies are in progress to explain the mechanism of action and the in vivo activity is necessary to confirm their effectiveness.
10 citations
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TL;DR: Activation of ALDH2 by piperlonguminine ameliorates cell damage generated in heart ischemia/reperfusion events, by decreasing lipid aldehydes concentration promoting cardioprotection.
9 citations
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TL;DR: Two natural piperamides and their derivatives were synthesized and evaluated for inhibitory activity against histone deacetylases, as well as the HCT-116 human colon cancer cell line.
9 citations
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TL;DR: This is the first investigation of potential herb–drug interactions associated with PL conducted by identifying the competitive inhibitory effects of PL on CYP1A2 in HLMs.
Abstract: Piperlonguminine (PL), a major alkaloid isolated from Piper longum fruits, shows several biological activities including anti-tumor, anti-hyperlipidemic and anti-inflammatory effects. Although there have been studies of the biological effects of PL, the potential drug-interaction effect of PL following evaluation of inhibitory effects of cytochrome P450 (CYP) activities was not investigated. Here, to investigate the inhibitory effects of PL on the activities of CYP isoforms, CYP inhibition assays were conducted using a cocktail of probe substrates in pooled human liver microsome (HLMs) and human recombinant cDNA-expressed CYP. PL strongly inhibited CYP1A2-mediated phenacetin O-deethylation with an IC50 value of 8.8 μM, as NADPH-independent inhibition, while other CYPs were not significantly inhibited. A Lineweaver–Burk plot resulted in the inhibition mechanism of PL being divided into two different modes, reversible competitive inhibition in a low concentration range of 0–16 μM with a Ki value of 1.39 μM and uncompetitive inhibitory behavior at a high concentration range of 16–40 μM. In addition, PL only decreased CYP 1A2-catalyzed phenacetin O-deethylase activity with IC50 values of 10.0 μM in human recombinant cDNA-expressed 1A2, not 1A1. Overall, this is the first investigation of potential herb–drug interactions associated with PL conducted by identifying the competitive inhibitory effects of PL on CYP1A2 in HLMs.
8 citations
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15 Aug 2016TL;DR: The present findings suggest that the clinical advantages of the crude extract and isolated compounds of P. retrofractum Vahl lie in combination therapy in order to enhance the efficacy of conventional antitubercular or anticancer drugs.
Abstract: A bioassay guided fractionation procedure used on the crude methanol extract of Piper retrofractum fruit identified 4 compounds: piperine, methyl piperate, sylvatine, and piperlonguminine. The bioactivities of 4 compounds and the crude methanol extract were examined. The crude methanol extract showed antibacterial activity against Mycobacterium tuberculosis , with a minimum inhibitory concentration (MIC) of 25.00 µg/mL. Piperine and piperlonguminine inhibited M. tuberculosis with MIC values of 50.00 mg/mL, whereas methyl piperate and sylvatine were inactive (% inhibition less than 90 % at a 50.00 mg/mL concentration). The crude extract and all isolated compounds were tested for cytotoxic activity against lung cancer cells (SCLC-H22 and NCI-H187) and human gingival fibroblasts (HGF) in cell cultures. All 4 isolated compounds showed weak cytotoxic activity against lung cancer cells (SCLC-H22 and NCI-H187) and human gingival fibroblasts (HGF) (% inhibition less than 20 % at a 5 mg/mL concentration, or a % inhibition less than 50 % at a 50 mg/mL concentration). However the crude methanol extract showed moderate cytotoxic behavior against lung cancer cells (NCI-H187) and human gingival fibroblasts (HGF), with an IC 50 of 20.98 mg/mL and % inhibition = 56.83 at 25 µg/mL concentration, respectively. The present findings suggest that the clinical advantages of the crude extract and isolated compounds of P. retrofractum Vahl lie in combination therapy in order to enhance the efficacy of conventional antitubercular or anticancer drugs.
8 citations