| Description: |
Auraptene possesses anticarcinogenic, cardioprotective, anti-inflammatory, anti-oxidant, antihelicobacter, antigenotoxic, and neuroprotective effects. Auraptene has a potential to attenuate chronic inflammation in adipose tissue and to improve obesity-related insulin resistance, and has protective effects in transgenic rats developing adenocarcinoma of the prostate (TRAP) and human prostate carcinoma cells. |
| Targets: |
IFN-γ | IL Receptor | PGE | COX | BACE | JNK | Beta Amyloid | TNF-α | p38MAPK | NO |
| In vitro: |
| Eur J Pharmacol. 2015 Mar 5;750:8-13. | | Auraptene has the inhibitory property on murine T lymphocyte activation.[Pubmed: 25620131] | Auraptene, a citrus fruit-derived coumarin, has been reported to exert valuable pharmacological properties as anti-tumor, anti-inflammatory, and anti-oxidant agent. However, little is known about auraptene on immune responses.
METHODS AND RESULTS:
In this study, we conducted an investigation to evaluate auraptene as an anti-T lymphocyte proliferation agent using CD3/CD28-activated lymphocytes isolated from C57BL/6 mice. We found that administration of auraptene inhibited CD3/CD28-activated lymphocyte proliferation in a dose dependent manner, but the inhibition at a wide range of doses used in this study did not induce cytotoxicity or apoptosis. In addition, auraptene dose dependently decreased the CD3/CD28-activated T lymphocyte secreting T helper (Th)1 cytokines (interleukin (IL)-2 and interferon (IFN)-γ); whereas, auraptene could decrease Th2 cytokine (IL-4) at a higher level (40μM) but had not at lower levels (10 and 20μM). Further mechanistic study demonstrated that auraptene doses dependently suppressed T cell early and middle/late activation marker CD69 and CD25 expression, respectively. Finally, auraptene could suppress cell cycle progression which contributes to inhibiting T cell proliferation and cell division.
CONCLUSIONS:
These findings indicate that auraptene exhibits anti-inflammatory properties via inhibiting T cell proliferation and their inflammatory cytokine secretion that may mediate the interaction between T cells and autoimmune disorders, suggesting that auraptene is a potential food-derived compound with a benefit to those with abnormally over-activation T cell mediated response and chronic inflammation such as autoimmune and inflammatory diseases. | | Inflammation. 2013 Dec;36(6):1525-32. | | Anti-inflammatory effect of auraptene extracted from trifoliate orange (Poncirus trifoliate) on LPS-stimulated RAW 264.7 cells.[Pubmed: 23872723] | Poncirus trifoliate is a traditional Chinese medicinal plant used for treating inflammation-related diseases for a long time and trifoliate orange contains abundant auraptene.
METHODS AND RESULTS:
The present study was to evaluate auraptene as a potential anti-inflammatory agent and investigate the mechanism of auraptene against prostaglandins E2 (PGE2) and cyclooxygenase-2 (COX-2) on lipopolysaccharide (LPS)-stimulated RAW 264.7 cells by comparing it with aspirin as a positive control group. The methods of enzyme-linked immunosorbent assay, reverse transcriptive polymerase chain reaction, real-time PCR, and western-blotting were used in the study. The results showed that auraptene exhibited better biocompatibility and lower cytotoxicity. At the same time, it significantly inhibited the production of PGE2 on LPS-stimulated macrophage cells. The auraptene-treated group had a higher COX-2 mRNA expression but relatively lower COX-2 protein level which implied that auraptene suppressed the post-transcriptional expression of COX-2 protein but not the transcriptional process.
CONCLUSIONS:
Compared with aspirin, the lower cytotoxicity of auraptene can make it a potential source for medicine that can benefit patients who are suffering from chronic inflammatory diseases and need long-term medication. |
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| In vivo: |
| Iran J Basic Med Sci. 2015 Feb;18(2):153-8. | | Antihypertensive effect of auraptene, a monoterpene coumarin from the genus Citrus, upon chronic administration.[Pubmed: 25810889] | Auraptene, a monoterpene coumarin from Citrus species, exhibits cardioprotective effects. In this study, the effects of auraptene administration were investigated on blood pressure of normotensive and desoxycorticosterone acetate (DOCA) salt induced hypertensive rats.
METHODS AND RESULTS:
Five weeks administration of auraptene (2, 4, 8 and 16 mg/kg/day) and nifedipine (0.25, 0.5, 1, 2 and 4 mg/kg/day) in different groups of normotensive and hypertensive rats (at the end of 3 weeks treatment by DOCA salt) was carried out and their effects on mean systolic blood pressure (MSBP) and mean heart rate (MHR) were evaluated using tail cuff method.
Our results indicated that chronic administration of auraptene (2, 4, 8 and 16 mg/kg/day) significantly reduced the MSBP in DOCA salt treated rats in a dose and time dependent manner. The percent of decreases in MSBP levels by the highest dose of auraptene (16 mg/kg) at the end of 4 (th) to 8 (th) weeks, were 7.00%, 10.78%, 16.07%, 21.28% and 27.54% respectively (P<0.001). Moreover the antihypertensive effect of auraptene was less than nifedipine (ED50 value of nifedipine = 0.7 mg/kg at 8(th) week and ED50 value of auraptene = 5.64 mg/kg at 8 week).
CONCLUSIONS:
Auraptene considerably reduced MSBP in hypertensive rats, but not in normotensive (normal saline treated) rats. The results of MHR measurement showed that the increase in MHR was not significant in comparison with DOCA treated rats. |
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