Rutaecarpine is an indolopyridoquinazoline alkaloid isolated from Evodia rutaecarpa and known to inhibit COX-2 with an IC50 of 0.28μM at the cellular level[1]. Rutaecarpine exhibits various pharmacological effects, such as anti‑inflammatory[2], anti‑apoptotic and antioxidant effects[3]. Rutaecarpine plays critical roles in cardiovascular[4], nervous system, inflammatory and tumor diseases[5].
Rutaecarpine at concentrations of 10µM for 24h effectively attenuated IL‑1β‑induced chondrocyte apoptosis, senescence and autophagy impairment in chondrocytes[6]. In HepG2 cells, Rutaecarpine at concentrations of 40µM for 24h increases p-GSK-3b and p-AMPK, and decreased G6Pase expression[7].
Rutaecarpine (20mg/kg, intragastric administration, daily for 9 days) inhibited oxidative stress in NTG-induced mice and improves migraine by activation of the Nrf2 antioxidant system through the PTEN/PGK1 pathway[8]. Rutaecarpine (10mg/kg, 20mg/kg, 40mg/kg) significantly decreased the number of antibody-forming cells and caused weight decrease in mouse spleen in a dose-dependent manner[9].
References:
[1]. Moon TC, Murakami M, Kudo I, et al. A new class of COX-2 inhibitor, rutaecarpine from Evodia rutaecarpa. Inflamm Res. 1999 Dec;48(12):621-5. doi: 10.1007/s000110050512. PMID: 10669112.
[2]. Jayakumar T, Lin KC, Chang CC, et al. Targeting MAPK/NF-κB Pathways in Anti-Inflammatory Potential of Rutaecarpine: Impact on Src/FAK-Mediated Macrophage Migration. Int J Mol Sci. 2021 Dec 22;23(1):92. doi: 10.3390/ijms23010092. PMID: 35008520; PMCID: PMC8745017.
[3]. Choi JH, Jin SW, Lee GH, et al. Rutaecarpine Protects against Acetaminophen-Induced Acute Liver Injury in Mice by Activating Antioxidant Enzymes. Antioxidants (Basel). 2021 Jan 10;10(1):86. doi: 10.3390/antiox10010086. PMID: 33435214; PMCID: PMC7827407.
[4]. Jia S, Hu C. Pharmacological effects of rutaecarpine as a cardiovascular protective agent. Molecules. 2010 Mar 15;15(3):1873-81. doi: 10.3390/molecules15031873. PMID: 20336017; PMCID: PMC6257227.
[5]. Chan S, Sun R, Tu X, et al. Rutaecarpine suppresses the proliferation and metastasis of colon cancer cells by regulating the STAT3 signaling. J Cancer. 2022 Jan 1;13(3):847-857. doi: 10.7150/jca.66177. PMID: 35154453; PMCID: PMC8824880.
[6]. Wan J, Li M, Yuan X, et al. Rutaecarpine ameliorates osteoarthritis by inhibiting PI3K/AKT/NF‑κB and MAPK signalling transduction through integrin αVβ3. Int J Mol Med. 2023 Oct;52(4):97. doi: 10.3892/ijmm.2023.5300. Epub 2023 Sep 1. PMID: 37654229; PMCID: PMC10555473.
[7]. Surbala L, Singh CB, Devi RV, et al. Rutaecarpine exhibits anti-diabetic potential in high fat diet-multiple low dose streptozotocin induced type 2 diabetic mice and in vitro by modulating hepatic glucose homeostasis. J Pharmacol Sci. 2020 Aug;143(4):307-314. doi: 10.1016/j.jphs.2020.04.008. Epub 2020 Jun 9. PMID: 32536591.
[8]. Xu M, Shi Z, He Z, et al. Rutaecarpine alleviates migraine in nitroglycerin-induced mice by regulating PTEN/PGK1 signaling pathway to activate NRF2 antioxidant system. Biomed Pharmacother. 2023 Oct;166:115300. doi: 10.1016/j.biopha.2023.115300. Epub 2023 Aug 7. PMID: 37557014.
[9]. Jeon TW, Jin CH, Lee SK, et al. Immunosuppressive effects of rutaecarpine in female BALB/c mice. Toxicol Lett. 2006 Jul 1;164(2):155-66. doi: 10.1016/j.toxlet.2005.12.005. Epub 2006 Jan 18. PMID: 16412592.
Rutaecarpine是一种从吴茱萸中分离出的吲哚并吡啶喹唑啉生物碱，已知在细胞水平上以0.28μM的IC50抑制COX-2[1]。Rutaecarpine表现出多种药理作用，如抗炎[2]、抗凋亡和抗氧化作用[3]。Rutaecarpine在心血管[4]、神经系统、炎症和肿瘤疾病中发挥关键作用[5]。
Rutaecarpine (10µM) 处理24小时有效减轻了IL-1β诱导的软骨细胞凋亡、衰老和自噬障碍[6]。在HepG2细胞中，40µM浓度的Rutaecarpine处理24小时增加了p-GSK-3β和p-AMPK的表达，并降低了G6Pase的表达[7]。
Rutaecarpine（20mg/kg，灌胃，每日一次，连续9天）在NTG诱导的小鼠中抑制了氧化应激，并通过PTEN/PGK1通路激活Nrf2抗氧化系统，从而改善偏头痛[8]。Rutaecarpine处理（10mg/kg、20mg/kg、40mg/kg）显著减少了抗体形成细胞的数量，并以剂量依赖性方式导致小鼠脾脏重量减少[9]。