| Description: |
Oxysophocarpine shows anti-inflammatory, neuroprotective,
anticonvulsant, and anti-nociceptive effects, it also attenuates inflammatory pain by suppressing the levels of phosphorylation of extracellular signal-regulated kinase 1/2, cyclooxygenase-2, prostaglandin E2, tumor necrosis factor α, interleukin-1 beta and interleukin-6.
|
| Targets: |
ERK | COX | PGE | TNF-α | IL Receptor | Caspase | GABA Receptor | Bcl-2/Bax | P450 (e.g. CYP17) |
| In vitro: |
| Pharm Biol. 2014 Aug;52(8):1052-9. | | Neuroprotective effects of oxysophocarpine on neonatal rat primary cultured hippocampal neurons injured by oxygen-glucose deprivation and reperfusion.[Pubmed: 24601951] | Oxysophocarpine (OSC), a quinolizidine alkaloid extracted from leguminous plants of the genus Robinia, is traditionally used for various diseases including neuronal disorders. This study investigated the protective effects of Oxysophocarpine on neonatal rat primary-cultured hippocampal neurons were injured by oxygen-glucose deprivation and reperfusion (OGD/RP).
METHODS AND RESULTS:
Cultured hippocampal neurons were exposed to OGD for 2 h followed by a 24 h RP. Oxysophocarpine (1, 2, and 5 μmol/L) and nimodipine (Nim) (12 μmol/L) were added to the culture after OGD but before RP. The cultures of the control group were not exposed to OGD/RP. MTT and LDH assay were used to evaluate the protective effects of Oxysophocarpine. The IC50 of OSC was found to be 100 μmol/L. Treatment with Oxysophocarpine (1, 2, and 5 μmol/L) attenuated neuronal damage (p < 0.001), with evidence of increased cell viability (p < 0.001) and decreased cell morphologic impairment. Furthermore, Oxysophocarpine increased MMP (p < 0.001), but it inhibited [Ca(2+)]i (p < 0.001) elevation in a dose-dependent manner at OGD/RP. Oxysophocarpine (5 μmol/L) also decreased the expression of caspase-3 (p < 0.05) and caspase-12 (p < 0.05).
CONCLUSIONS:
The results suggested that Oxysophocarpine has significant neuroprotective effects that can be attributed to inhibiting endoplasmic reticulum (ER) stress-induced apoptosis. |
|
| In vivo: |
| Planta Med. 2015 Jul;81(10):791-7. | | Oxysophocarpine Ameliorates Carrageenan-induced Inflammatory Pain via Inhibiting Expressions of Prostaglandin E2 and Cytokines in Mice.[Pubmed: 26132856] | Oxysophocarpine is an alkaloid extracted from Sophora alopecuroides.
METHODS AND RESULTS:
Mouse ear swelling tests and carrageenan-induced paw edema tests were used to investigate the effects of Oxysophocarpine on inflammatory pain in mice. Morphological changes on inflamed paw sections were measured by hematoxylin-eosin staining. Oxysophocarpine also significantly reduced the paw edema volume and improved mechanical allodynia threshold value on carrageenan-induced inflammatory pain, as well as relieved paw tissues inflammatory damage and reduced the numbers of neutrophils in mice. Oxysophocarpine significantly suppressed over-expression of cyclooxygenase-2, tumor necrosis factor α, interleukin-1 beta, interleukin-6 and prostaglandin E2, and inhibited the over-phosphorylation of extracellular signal-regulated kinase 1/2.
CONCLUSIONS:
Based on these findings we propose that Oxysophocarpine attenuates inflammatory pain by suppressing the levels of phosphorylation of extracellular signal-regulated kinase 1/2, cyclooxygenase-2, prostaglandin E2, tumor necrosis factor α, interleukin-1 beta and interleukin-6. | | Mol Med Rep. 2013 Jun;7(6):1819-25. | | Oxysophocarpine induces anti-nociception and increases the expression of GABAAα1 receptors in mice.[Pubmed: 23563643] | Oxysophocarpine (OSC) is an alkaloid extracted from Siphocampylus verticillatus. The aim of this study was to investigate the anti-nociceptive effects of Oxysophocarpine through systemic and intracerebroventricular administration in mice. Moreover, to evaluate its effectiveness and mechanism of action, this study investigated whether Oxysophocarpine altered the expression of γ-aminobutyric acid type A α1 (GABAAα1) receptors in the central nervous system.
METHODS AND RESULTS:
Thermal and chemical behavioral models of nociception were used to assess the anti‑nociceptive action of Oxysophocarpine.Oxysophocarpine was administered intraperitoneally (i.p.) or intracerebroventricularly (i.c.v.). Results showed that Oxysophocarpine (80 mg/kg, i.p.) significantly increased the tail withdrawal threshold with a peak effect of 25.46% maximal possible effect (MPE) at 60 min (P﹤0.01). Additionally, Oxysophocarpine (80 mg/kg) increased the positive staining of GABAAα1 receptors in cells.
CONCLUSIONS:
In conclusion, Oxysophocarpine administration is suggested to have anti-nociceptive effects on the central and peripheral nervous systems. The involvement of GABAA receptors in the anti-nociceptive activity of Oxysophocarpine is currently being investigated. |
|
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)
