| Description: |
Pristimerin is a naturally occurring triterpenoid that has been shown to suppress the proliferation of various cancer cell lines at the concentration (IC50) range of 0.2-4 μM, including those of breast, glioma, prostate, pancreatic, ovarian, colon. Pristimerin exhibits inhibitory effects against diverse phytopathogenic fungi, it shows good preventive effect and curative effect against wheat powdery mildew in vivo. It has a wide spectrum of targets including ROS, IKK, NF-κB, Akt, mTOR, Bcr-Abl. |
| Targets: |
TNF-α | IL Receptor | ROS | NF-kB | p65 | IkB | HIF | PARP | Akt | mTOR | COX | VEGFR | PKC | Bcl-2/Bax | DNA/RNA Synthesis | Bcr-Abl | Antifection | IKK |
| In vitro: |
| Int Immunopharmacol. 2014 Aug;21(2):501-8. | | Pristimerin, a natural anti-tumor triterpenoid, inhibits LPS-induced TNF-α and IL-8 production through down-regulation of ROS-related classical NF-κB pathway in THP-1 cells.[Pubmed: 24957686] |
Pristimerin, a naturally occurring quinonemethide triterpenoid compound, is known to exert a variety of pharmacological activities.
METHODS AND RESULTS:
In the present study, we investigated the molecular actions of Pristimerin against LPS-induced inflammatory responses in human monocytic THP-1 cells. The results showed that Pristimerin inhibited the production of TNF-α and IL-8 in a dose-dependent manner. To explore the possible mechanisms underlying these inhibitions by Pristimerin, we examined the intracellular ROS level and the NF-κB protein signaling pathway. Pristimerin clearly scavenged LPS-induced intracellular ROS production. In addition, Pristimerin prevented LPS-induced NF-κB activation through the inhibition of phosphorylation of IKKα/β, phosphorylation and degradation of IκBα, as well as phosphorylation and nuclear translocation of NF-κB p65.
CONCLUSIONS:
These findings suggest that Pristimerin down-regulates the expression of pro-inflammatory mediators through blocking of NF-κB activation by inhibiting interconnected ROS/IKK/NF-κB signaling pathways. | | Pest Manag Sci. 2005 Jan;61(1):85-90. | | Antifungal properties of pristimerin and celastrol isolated from Celastrus hypoleucus.[Pubmed: 15593077 ] | Pristimerin and celastrol isolated from the roots of Celastrus hypoleucus (Oliv) Warb f argutior Loes exhibited inhibitory effects against diverse phytopathogenic fungi.
METHODS AND RESULTS:
Pristimerin and celastrol were found to inhibit the mycelial growth of Rhizoctonia solani Kuhn and Glomerella cingulata (Stonem) Spauld & Schrenk in vitro by 83.6 and 62.6%, respectively, at 10 microg ml(-1). Pristimerin showed good preventive effect (96.7% at 100 microg ml(-1)) and curative effect (66.5% at 100 microg ml(-1)) against wheat powdery mildew in vivo. For celastrol, the preventive and curative effects against wheat powdery mildew were 80.5 and 45.4%, respectively, at 100 microg ml(-1). |
|
| In vivo: |
| Clin Immunol. 2014 Dec;155(2):220-30. | | Pristimerin, a naturally occurring triterpenoid, protects against autoimmune arthritis by modulating the cellular and soluble immune mediators of inflammation and tissue damage.[Pubmed: 25308129] | Rheumatoid arthritis (RA) is a chronic autoimmune disorder affecting the synovial joints. The currently available drugs for RA are effective only in a proportion of patients and their prolonged use is associated with severe adverse effects.
Thus, new anti-arthritic agents are being sought.
METHODS AND RESULTS:
We tested Pristimerin, a naturally occurring triterpenoid, for its therapeutic activity against rat adjuvant arthritis. Pristimerin effectively inhibited both arthritic inflammation and cartilage and bone damage in the joints. Pristimerin-treated rats exhibited a reduction in the pro-inflammatory cytokines (IL-6, IL-17, IL-18, and IL-23) and the IL-6/IL-17-associated transcription factors (pSTAT3 and ROR-γt), coupled with an increase in the immunomodulatory cytokine IL-10. Also increased was IFN-γ, which can inhibit IL-17 response. In addition, the Th17/Treg ratio was altered in favor of immune suppression and the RANKL/OPG ratio was skewed towards anti-osteoclastogenesis.
CONCLUSIONS:
This is the first report on testing Pristimerin in arthritis. We suggest further evaluation of Pristimerin in RA patients. |
|
Cell. 2018 Jan 11;172(1-2):249-261.e12. doi: 10.1016/j.cell.2017.12.019.IF=36.216(2019)
Cell Metab. 2020 Mar 3;31(3):534-548.e5. doi: 10.1016/j.cmet.2020.01.002.IF=22.415(2019)
Mol Cell. 2017 Nov 16;68(4):673-685.e6. doi: 10.1016/j.molcel.2017.10.022.IF=14.548(2019)
ACS Nano. 2018 Apr 24;12(4): 3385-3396. doi: 10.1021/acsnano.7b08969.IF=13.903(2019)
Nature Plants. 2016 Dec 22;3: 16206. doi: 10.1038/nplants.2016.205.IF=13.297(2019)
Sci Adv. 2018 Oct 24;4(10): eaat6994. doi: 10.1126/sciadv.aat6994.IF=12.804(2019)
