Hwang Su-Jung, Song Ye-Seul, Lee Hyo-Jong
School of Pharmacy, Sungkyunkwan University, 2066 Seobu-ro, Jangan-gu, Suwon 16419, Gyeonggi-do, Korea.
Biomedicines. 2021 Apr 13;9(4):420. doi: 10.3390/biomedicines9040420.
Kushen (Radix ) is used to treat ulcerative colitis, tumors, and pruritus. Recently, phaseolin, formononetin, matrine, luteolin, and quercetin, through a network pharmacology approach, were tentatively identified as five bioactive constituents responsible for the anti-inflammatory effects of . However, the role of phaseolin (one of the primary components of ) in the direct regulation of inflammation and inflammatory processes is not well known. In this study, the beneficial role of phaseolin against inflammation was explored in lipopolysaccharide (LPS)-induced inflammation models of RAW 264.7 macrophages and zebrafish larvae. Phaseolin inhibited LPS-mediated production of nitric oxide (NO) and the expression of inducible nitric oxide synthase (iNOS), without affecting cell viability. In addition, phaseolin suppressed pro-inflammatory mediators such as cyclooxygenase 2 (COX-2), interleukin-1β (IL-1β), tumor necrosis factor α (TNF-α), monocyte chemoattractant protein-1 (MCP-1), and interleukin-6 (IL-6) in a dose-dependent manner. Furthermore, phaseolin reduced matrix metalloproteinase (MMP) activity as well as macrophage adhesion in vitro and the recruitment of leukocytes in vivo by downregulating Ninjurin 1 (Ninj1), an adhesion molecule. Finally, phaseolin inhibited the nuclear translocation of nuclear factor-kappa B (NF-κB). In view of the above, our results suggest that phaseolin could be a potential therapeutic candidate for the management of inflammation.
苦参用于治疗溃疡性结肠炎、肿瘤和瘙痒症。最近,通过网络药理学方法,初步确定菜豆素、芒柄花素、苦参碱、木犀草素和槲皮素是苦参抗炎作用的五种生物活性成分。然而,菜豆素(苦参的主要成分之一)在直接调节炎症和炎症过程中的作用尚不清楚。在本研究中,在脂多糖(LPS)诱导的RAW 264.7巨噬细胞和斑马鱼幼虫炎症模型中探索了菜豆素对炎症的有益作用。菜豆素抑制LPS介导的一氧化氮(NO)生成和诱导型一氧化氮合酶(iNOS)的表达,而不影响细胞活力。此外,菜豆素以剂量依赖性方式抑制促炎介质,如环氧合酶2(COX-2)、白细胞介素-1β(IL-1β)、肿瘤坏死因子-α(TNF-α)、单核细胞趋化蛋白-1(MCP-1)和白细胞介素-6(IL-6)。此外,菜豆素通过下调粘附分子Ninjurin 1(Ninj1)降低体外基质金属蛋白酶(MMP)活性以及巨噬细胞粘附和体内白细胞募集。最后,菜豆素抑制核因子-κB(NF-κB)的核转位。鉴于上述情况,我们的结果表明菜豆素可能是一种潜在的炎症治疗候选药物。