Piplartine, an amide alkaloid from Piper tuberculatum, presents anxiolytic and antidepressant effects in mice

Felipe, Fernando; Filho, Jucélio Trajano Sousa; Souza, Louise Emanuele de Oliveira; SILVEIRA, JOÃO ALISON M.; Uchôa, Daniel Esdras de Andrade; Silveira, Edilberto R.; Pessoa, Otília Deusdênia Loiola; Viana, Glauce Socorro de Barros

doi:10.1016/j.phymed.2006.12.015

Cited by 92 publications

(21 citation statements)

References 44 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Piperlongumine has been used widely in traditional medicine, including the Indian Ayurvedic system of medicine, traditional Chinese medicine, Tibetan medicine, and the folk medicine of Latin America. Piperlongumine has multiple pharmacologic activities: it has been described as a platelet aggregation inhibitor (3), an anxiolytic agent (4), an antidepressant (5), an antinociceptive agent (6), an anti-atherosclerotic agent (7), an antidiabetic agent (8), an anti-inflammatory agent (9), and an infectious pathogen inhibitor (10). Furthermore, piperlongumine has been reported to kill multiple types of cancer cells, inhibit metastasis, and have antitumor activities in a variety of animal models (11)(12)(13)(14)(15)(16)(17)(18)(19)(20)(21)(22).…”

Section: Introductionmentioning

confidence: 99%

Piperlongumine Chemosensitizes Tumor Cells through Interaction with Cysteine 179 of IκBα Kinase, Leading to Suppression of NF-κB–Regulated Gene Products

Han

Gupta

Prasad

et al. 2014

Molecular Cancer Therapeutics

View full text Add to dashboard Cite

Recently, two different reports appeared in prominent journals suggesting a mechanism by which piperlongumine, a pyridine alkaloid, mediates anticancer effects. In the current report, we describe another novel mechanism by which this alkaloid mediates its anticancer effects. We found that piperlongumine blocked NF-kB activated by TNFa and various other cancer promoters. This downregulation was accompanied by inhibition of phosphorylation and degradation of IkBa. Further investigation revealed that this pyridine alkaloid directly interacts with IkBa kinase (IKK) and inhibits its activity. Inhibition of IKK occurred through interaction with its cysteine 179 as the mutation of this residue to alanine abolished the activity of piperlongumine. Inhibition in NF-kB activity downregulated the expression of proteins involved in cell survival (Bcl-2, Bcl-xL, c-IAP-1, c-IAP-2, survivin), proliferation (c-Myc, cyclin D1), inflammation (COX-2, IL6), and invasion (ICAM-1, -9, CXCR-4, VEGF). Overall, our results reveal a novel mechanism by which piperlongumine can exhibit antitumor activity through downmodulation of proinflammatory pathway. Mol Cancer Ther; 13(10); 2422-35. Ó2014 AACR.

show abstract

Section: Introductionmentioning

confidence: 99%

Piperlongumine Chemosensitizes Tumor Cells through Interaction with Cysteine 179 of IκBα Kinase, Leading to Suppression of NF-κB–Regulated Gene Products

Han

Gupta

Prasad

et al. 2014

Molecular Cancer Therapeutics

View full text Add to dashboard Cite

show abstract

“…Furthermore, a significant and dosedependent decrease in the immobility time, as evaluated by the forced swimming test, was observed after PIP administration (41% and 75% decrease, at the doses of 50 and 100 mg/kg, respectively), suggesting an antidepressant effect, similarly to that observed with imipramine, a classical antidepressant drug used as standard. In conclusion, we showed that PIP presents significant Anxiolytic and antidepressant activities, making this drug potentially useful in anxiety and depression 18 .…”

Section: Hypericum Canariense H Glandulosummentioning

confidence: 74%

Untitled

2011

IJPSR

View full text Add to dashboard Cite

Depression is a heterogenous mood disorder that has been classified and treated in variety of ways. Although a number of synthetic drugs are being used as standard treatment for clinically depressed patient, they have adverse effects that can compromise the therapeutic treatment .Thus, it is worthwhile to look for antidepressant from plants with proven advantage and favorable benefit to risk ratio. A number of medicinal plants and medicine derived from these plants have shown antidepressant properties by virtue of combined effect of their medicinal constituents. The causes of depression are decreased brain levels of monoamines like noradrenaline, dopamine and serotonin. Therefore, drugs restoring the reduced levels of these monoamines in the brain either by inhibiting monoamine oxidase or by inhibiting reuptake of these neurotransmitters might be fruitful in the treatment of depression. The present review is focused on the medicinal plants and plants based formulations having antidepressant activity in animal studies and in humans.

show abstract

“…1A), an alkaloid/amide component, is one such agent. Derived from the plant species Piper longum Linn, piperlongumine has been shown to possess numerous key biologic activities such as anti-platelet aggregation (17), antibacterial and insecticidal (18), anti-atherosclerotic (19), anxiolytic (20), antidepressant (21), antidiabetic (22,23), anti-inflammatory (23), and antitumor capabilities (24). Among the multivalent effects, the potential of piperlongumine as a novel anticancer agent have gained considerable attention recently.…”

Section: Introductionmentioning

confidence: 99%

Piperlongumine Suppresses Growth and Sensitizes Pancreatic Tumors to Gemcitabine in a Xenograft Mouse Model by Modulating the NF-kappa B Pathway

Wang

Zhou

et al. 2016

Cancer Prevention Research

View full text Add to dashboard Cite

Pancreatic cancer is an aggressive malignancy, which generally respond poorly to chemotherapy. Hence, novel agents that are safe and effective are highly needed. The aim of this study was to investigate whether piperlongumine, a natural product isolated from the fruit of the pepper Piper longum, has any efficacy against human pancreatic cancer when used either alone or in combination with gemcitabine in vitro and in a xenograft mouse model. In vitro, piperlongumine inhibited the proliferation of pancreatic cancer cell lines, potentiated the apoptotic effects of gemcitabine, inhibited the constitutive and inducible activation of NF-kB, and suppressed the NF-kB-regulated expression of c-Myc, cyclin D1, Bcl-2, Bcl-xL, Survivin, XIAP, VEGF, and matrix metalloproteinase-9 (MMP-9). Furthermore, in an in vivo xenograft model, we found piperlongumine alone significantly suppressed tumor growth and enhanced the antitumor properties of gemcitabine. These results were consistent with the downregulation of NF-kB activity and its target genes, decreased proliferation (PCNA and Ki-67), decreased microvessel density (CD31), and increased apoptosis (TUNEL) in tumor remnants. Collectively, our results suggest that piperlongumine alone exhibits significant antitumor effects against human pancreatic cancer and it further enhances the therapeutic effects of gemcitabine, possibly through the modulation of NF-kB-and NF-kB-regulated gene products.Cancer Prev Res; 9(3); 234-44. Ó2015 AACR.

show abstract

Piplartine, an amide alkaloid from Piper tuberculatum, presents anxiolytic and antidepressant effects in mice

Cited by 92 publications

References 44 publications

Piperlongumine Chemosensitizes Tumor Cells through Interaction with Cysteine 179 of IκBα Kinase, Leading to Suppression of NF-κB–Regulated Gene Products

Piperlongumine Chemosensitizes Tumor Cells through Interaction with Cysteine 179 of IκBα Kinase, Leading to Suppression of NF-κB–Regulated Gene Products

Untitled

Piperlongumine Suppresses Growth and Sensitizes Pancreatic Tumors to Gemcitabine in a Xenograft Mouse Model by Modulating the NF-kappa B Pathway

Contact Info

Product

Resources

About