1,3-Dicaffeoylquinic acid inhibits the 3' end processing, terminal connection, and disintegration process of HIV-1 integrase, with IC50 values of 0.35, 0.56, and 0.84μg/ml respectively [1]. 1,3-Dicaffeoylquinic acid is a type of phenolic compound found in artichokes [2]. 1,3-Dicaffeoylquinic acid possesses antioxidant activity and is a free radical scavenger [3].
In vitro, 1,3-Dicaffeoylquinic acid (0.25-1μM; 30min) reduces the free radical levels released by human polymorphonuclear cells (PMNs) stimulated by the chemokine N-formyl-Met-Leu-Phe in a dose-dependent manner [4]. 1,3-Dicaffeoylquinic acid (0, 5, 10, 50, 100, and 500μM; 2h) pretreatment increases the cell viability of rat primary cortical neurons stimulated by amyloid β1-42 (Aβ42) in a concentration-dependent manner, activates Trk A and PI3K/Akt and Erkl/2 pathways, inhibits GSK3β and regulates Bcl-2/Bax expression [5].
In vivo, local administration of 1,3-Dicaffeoylquinic acid (5-500μg/mL; 5μL; 7 days) dose-dependently reduces corneal epithelial defects in dry eye disease (DED) model mice and increases tear production, while inhibiting inflammatory cytokines and T cell infiltration in the ocular surface and lacrimal glands [6]. In the forced swimming test and tail suspension test, treatment with 1,3-Dicaffeoylquinic acid (30mg/kg/day; 5 days; p.o.) significantly improves depressive-like behavior in ovariectomized (OVX) model mice [7].
References:
[1] Robinson, W.E., Jr., Cordeiro, M., Abdel-Malek, S., et al. Dicaffeoylquinic acid inhibitors of human immunodeficiency virus integrase: Inhibition of the core catalytic domain of human immunodeficiency virus integrase. Mol. Pharmacol. 50(4), 846-855 (1996).
[2] Jun N J, Jang K C, Kim S C, et al. Radical scavenging activity and content of cynarin (1, 3-dicaffeoylquinic acid) in Artichoke (Cynara scolymus L.)[J]. Journal of applied biological chemistry, 2007, 50(4): 244-248.
[3] Danino O, Gottlieb H E, Grossman S, et al. Antioxidant activity of 1, 3-dicaffeoylquinic acid isolated from Inula viscosa[J]. Food research international, 2009, 42(9): 1273-1280.
[4] Heilmann, J., Merfort, I., and Weiss, M.Radical scavenger activity of different 3',4'-dihydroxyflavonols and 1,5-dicaffeoylquinic acid studied by inhibition of chemiluminescencePlanta Med.61(5)435-438(1995).
[5] Xiao HB, Cao X, Wang L, et al. 1,5-dicaffeoylquinic acid protects primary neurons from amyloid β 1-42-induced apoptosis via PI3K/Akt signaling pathway. Chin Med J (Engl). 2011;124(17):2628-2635.
[6] Yoon CH, Jang HJ, Ryu JS, et al. 1,5-Dicaffeoylquinic acid from Pseudognaphalium affine ameliorates dry eye disease via suppression of inflammation and protection of the ocular surface. Ocul Surf. 2023;29:469-479.
[7] Lim D W, Kim M, Yoon M, et al. 1, 3-Dicaffeoylquinic acid as an active compound of Arctium lappa root extract ameliorates depressive-like behavior by regulating hippocampal nitric oxide synthesis in ovariectomized mice[J]. Antioxidants, 2021, 10(8): 1281.
1,3-Dicaffeoylquinic acid能抑制HIV-1整合酶的3'端加工、末端连接以及解体过程，IC50值分别为0.35、0.56和0.84μg/ml [1]。1,3-Dicaffeoylquinic acid是一种存在于洋蓟中的酚类化合物 [2]。1,3-Dicaffeoylquinic acid具有抗氧化活性，是一种自由基清除剂 [3]。
在体外，1,3-Dicaffeoylquinic acid（0.25-1μM; 30min)以剂量依赖性方式降低了趋化因子N-formyl-Met-Leu-Phe刺激的人多形核细胞（PMNs）释放的自由基水平 [4]。1,3-Dicaffeoylquinic acid（0、5、10、50、100和500μM; 2h）预处理以浓度依赖性方式增加了淀粉样β1-42（Aβ42）刺激的大鼠原代皮质神经元的细胞活力，激活了Trk A和PI3K/Akt和Erkl/2途径，抑制GSK3β并调节Bcl-2/Bax表达 [5]。
在体内，1,3-Dicaffeoylquinic acid（5–500μg/mL; 5μL; 7 days）的局部施用剂量依赖性地减少了干眼病（DED）模型小鼠的角膜上皮缺陷并增加泪液产生，同时抑制眼表面和泪腺中的炎症细胞因子和T细胞浸润 [6]。在强迫游泳测试和尾悬测试中，1,3-Dicaffeoylquinic acid（30mg/kg/day; 5 days; p.o.）治疗显著改善了卵巢切除术（OVX）模型小鼠的抑郁样行为 [7]。