α-Cyperone, extracted from Cyperus rotundus, can inhibit microglia-mediated neuroinflammation. α-cyperone substantially decreased H2O2-induced death, release of LDH, and the production of ROS in SH-SY5Y cells. α-cyperone attenuated H2O2-induced cellular apoptosis. Moreover, α-cyperone remarkably reduced the expression of cleaved-caspase-3 and Bax, and upregulated Bcl-2. Furthermore, α-cyperone enhanced the nuclear translocation of Nrf2[3]. The anti-inflammatory activity of α-cyperone is associated with the down-regulation of COX-2 and IL-6 via the negative regulation of the NFκB pathway in LPS-stimulated RAW 264.7 cells[4]. In addition, in vivo studies based on a mouse model of arthritis showed that α-Cyperone prevented the development of osteoarthritis[5]. In addition, α-cyperone is also a promising inhibitor of Hla production by S. aureus and protects lung cells from this bacterium[6].
alpha-Cyperone/α-香附酮 细胞实验
Cell Line
Concentration
Treated Time
Description
References
NIH 3T3 cells
10 ng/mL to 1 μg/mL
8 h
evaluate antioxidant activity, significant decrease in ROS levels
Int J Nanomedicine. 2024 Aug 16;19:8403-8415
Cryptococcus neoformans
16 µg/mL
48 h
α-Cyperone significantly reduced the capsule size of Cryp. neoformans.
Antibiotics (Basel). 2021 Jan 6;10(1):51
Candida krusei
125 µg/mL
14 h
α-Cyperone completely inhibited the growth of C. krusei, showing fungicidal activity.
Antibiotics (Basel). 2021 Jan 6;10(1):51
rat aortic endothelial cells (RAECs)
1.25-5 µg/mL
3 h
To evaluate the effect of α-Cyperone on LPS-induced cell death in RAECs. Results showed that α-Cyperone significantly improved cell viability, reduced IL-1β and IL-18 release, and downregulated mRNA and protein expression of NLRP3, ASC, caspase-1, and GSDMD.
Pharmaceuticals (Basel). 2025 Feb 22;18(3):303
rat chondrocytes
0.75-6μM
24 or 48 h
To evaluate the effect of CYP on cell viability, results showed that various CYP concentrations did not exert significant cytotoxicity on chondrocytes
Aging (Albany NY). 2021 Jul 8;13(13):17690-17706
SH-SY5Y cells
15 or 30 µM
2 h
To assess the apoptotic rate. alpha-Cyperone significantly reduced H2O2-induced apoptosis.
Front Pharmacol. 2020 Apr 8;11:281
human neuroblastoma SH-SY5Y cells
50–150 μg/mL
24 h
To evaluate cytotoxicity, results showed no significant change in cell viability at 50–150 μg/mL, but a significant decrease was observed above 150 μg/mL.
Sci Rep. 2017 Mar 24;7:45231
alpha-Cyperone/α-香附酮 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
C57BL/6 mice
Chronic unpredictable mild stress (CUMS) model
Intragastric administration
5 mg/kg and 10 mg/kg
Once daily for 2 weeks
To evaluate the antidepressant effects of alpha-Cyperone, results showed it significantly improved depressive-like behaviors in CUMS mice, increased SIRT3 expression in the hippocampus, reduced ROS production, and inhibited NLRP3 inflammasome activation
Front Pharmacol. 2020 Oct 8;11:577062
C57BL/6 mice
Paclitaxel-induced neuropathic pain model
Intraperitoneal injection
480 and 800µg/kg
Administered on D0, D2, D4, and D6, total of 4 times
Prevented paclitaxel-induced cold and mechanical pain, alleviated pain by modulating the norepinephrine pathway
Metabolites. 2024 Dec 20;14(12):719
C57BL/6 wild-type mice
Surgery-induced DMM mouse model
Intraperitoneal injection
10 mg/kg
Once daily for 8 weeks
To evaluate the effect of CYP on OA development, results showed that CYP treatment significantly alleviated joint degeneration
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