Sappanone A is a homoisoflavanone with strong antioxidant and anti-inflammatory activities. It is one of the active ingredients of Sappan Lignum, it can inhibit microglia activation in the brain and has a neuroinflammatory effect[1-2].
Sappanone A(0-30µM；30min) inhibited the production of nitric oxide (NO), prostaglandin E2 (PGE2) and interleukin-6 (IL-6) as well as the expression of inducible nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2) and IL-6 in lipopolysaccharide (LPS)-stimulated RAW264.7 cells[3]. sappanone A (1.1 µM )significantly inhibited IBMX-induced increase of melanin content in B16 cells [4].40 µM sappanone A produced a significant inhibitory effect on cell viability. Concentrations of 5, 10, and 20 µM showed no significant change in cell viability. Sappanone A inhibited the IL-1β-stimulated production of NO, PGE2, iNOS, COX-2, TNF-α, IL-6, and IL-8 in OA chondrocytes[5].Sappanone A decreased cell viability of HOK cells and mouse salivary gland cells under ionising radiation[6].
Sappanone A (12.5, 25 and 50 mg/kg; 3days;i.p.) was found to attenuate the airway inflammation and mucus hypersecretion induced by the Ovalbumin(OVA) challenge in BALB/c mice[7]. Sappanone A(50 mg/kg；p.o.；5 days) significantly improved left ventricular (LV) systolic and diastolic function in a rat myocardial ischemia/reperfusion injury model, especially in the early phase development of myocardial infarction[8]. Sappanone A (10、20、40 mg/kg;i.p. ) reduced myocardial infarct size and the release of lactate dehydrogenase (LDH) and creatine kinase-MB (CK-MB) in a dose-dependent manner in myocardial ischemia reperfusion injury (MIRI) mice [9].
References:
[1]. Kang L, Zhao H, et,al. Sappanone A protects mice against cisplatin-induced kidney injury. Int Immunopharmacol. 2016 Sep;38:246-51. doi: 10.1016/j.intimp.2016.05.019. Epub 2016 Jun 16. PMID: 27318179.
[2]. Syamsunarno MRA, Safitri R, et,al.Protective Effects of Caesalpinia sappan Linn. and Its Bioactive Compounds on Cardiovascular Organs. Front Pharmacol. 2021 Sep 15;12:725745. doi: 10.3389/fphar.2021.725745. PMID: 34603037; PMCID: PMC8479160.
[3]. Lee S, Choi SY, et,al.Sappanone A exhibits anti-inflammatory effects via modulation of Nrf2 and NF-κB. Int Immunopharmacol. 2015 Sep;28(1):328-36. doi: 10.1016/j.intimp.2015.06.015. Epub 2015 Jun 26. PMID: 26122134.
[4]. Chang TS, Chao SY, et,al.Melanogenesis inhibition by homoisoflavavone sappanone A from Caesalpinia sappan. Int J Mol Sci. 2012;13(8):10359-10367. doi: 10.3390/ijms130810359. Epub 2012 Aug 20. PMID: 22949866; PMCID: PMC3431864.
[5]. Zhang Z, Zhang NZ, et,al. Sappanone A Alleviated IL-1β-Induced Inflammation in OA Chondrocytes through Modulating the NF-κB and Nrf2/HO-1 Pathways. Dis Markers. 2022 Sep 16;2022:2380879. doi: 10.1155/2022/2380879. PMID: 36157214; PMCID: PMC9507726.
[6]. Zhao XF, Wang ZY, et,al.Sappanone A Aggrandises Ionising Radiation-induced Damage in Oral Epithelial Cells. Chin J Dent Res. 2022 Dec 8;25(4):261-267. doi: 10.3290/j.cjdr.b3628117. PMID: 36479890.
[7]. Liu X, Yu D, et,al.Sappanone A Attenuates Allergic Airway Inflammation in Ovalbumin-Induced Asthma. Int Arch Allergy Immunol. 2016;170(3):180-6. doi: 10.1159/000448331. Epub 2016 Aug 30. PMID: 27576536.
[8]. Jo W, Min BS, et,al.Sappanone A Prevents Left Ventricular Dysfunction in a Rat Myocardial Ischemia Reperfusion Injury Model. Int J Mol Sci. 2020 Sep 21;21(18):6935. doi: 10.3390/ijms21186935. PMID: 32967328; PMCID: PMC7555706.
[9].Shi X, Tao G, et,al. Sappanone A Protects Against Myocardial Ischemia Reperfusion Injury by Modulation of Nrf2. Drug Des Devel Ther. 2020 Jan 8;14:61-71. doi: 10.2147/DDDT.S230358. PMID: 32021092; PMCID: PMC6955610.
Sappanone A是一种具有较强抗氧化和抗炎活性的同型异黄酮。它是木质素的有效成分之一,可以抑制大脑小胶质细胞的激活,具有神经炎症作用[1-2]。
Sappanone A(0-30µM;30min)可抑制脂多糖(LPS)刺激的RAW264.7细胞中一氧化氮(NO)、前列腺素E2 (PGE2)和白细胞介素6 (IL-6)的生成以及诱导型一氧化氮合酶(iNOS)、环氧合酶-2 (COX-2)和IL-6的表达[3]。sappanone A (1.1 µM)显著抑制IBMX诱导的B16细胞黑色素含量升高[4]。40 µM的sappanone A对细胞活力有明显的抑制作用。5、10、20 µM浓度对细胞活力无显著影响。Sappanone A抑制IL-1β刺激的OA软骨细胞NO、PGE2、iNOS、COX-2、TNF-α、IL-6和IL-8的产生[5]。在电离辐射作用下,Sappanone A可降低HOK细胞和小鼠唾液腺细胞的活力[6]。
Sappanone A(12.5、25和50 mg/kg;3days;i.p.)可减轻BALB/c小鼠因卵清蛋白OVA攻击引起的气道炎症和粘液分泌亢进[7]。在大鼠心肌缺血/再灌注损伤模型中,Sappanone A(50 mg/kg;p.o;5天)显著改善左室(LV)收缩和舒张功能,尤其是在心肌梗死早期发展阶段[8]。Sappanone A(10、20、40 mg/kg; i.p.)以剂量依赖的方式减少了心肌缺血再灌注损伤(MIRI)小鼠的心肌梗死面积和乳酸脱氢酶(LDH)和肌酸激酶-MB(CK-MB)的释放[9]。