Inhibitory effects of tilianin on the expression of inducible nitric oxide synthase in low density lipoprotein receptor deficiency mice

Abstract

We investigated the effect of tilianin upon inducible nitric oxide synthesis in the plasma of low-density lipoprotein receptor knock-out (Ldlr-/-) mice fed with high cholesterol diet and in primary peritoneal macrophages of Ldlr-/-mice. High cholesterol diet induced nitric oxide production in the plasma of Ldlr-/-mice. Tilianin reduced the level of nitric oxide (NO) in plasma from Ldlr-/-mice induced by the high cholesterol diet. Tilianin also inhibited the NO production from the primary culture of peritoneal macrophages treated with lipopolysaccharide. The inhibition of NO production was caused by the suppression of inducible nitric oxide synthase (iNOS) gene expression in peritoneal macrophages isolated from Ldlr-/-mice. Moreover, tilianin inhibited the transcriptional activation of iNOS promoter that has NF-κB binding element. Thus, these results provide the first evidence that tilianin inhibit iNOS expression and production of NO and may act as a potential anti-inflammatory agent.

Tilianin Inhibits MUC5AC Expression Mediated Via Down-Regulation of EGFR-MEK-ERK-Sp1 Signaling Pathway in NCI-H292 Human Airway Cells

“…Agastache rugosa Kuntze (Korean mint) is a perennial herb and well known as Bangah in the southern region of Korea [16]. Tilianin is a major constituent of A. rugosa and has been associated with numerous pharmacologic effects, such as antioxidant, antiatherogenic, antitumor, and antiinflammatory activities [17,18]. This plant contains flavonoids, including acacetin, tilianin, and rosmarinic acid, which contribute to these pharmacological activities [17,19].…”

The role of peroxidases in the pathogenesis of atherosclerosis

“…The novel compound KR-31378 is another potent antioxidant, ameliorating atherosclerosis in LDL receptor-deficient mice by blocking monocyte recruitment and downregulating VCAM-1 and interleukin-8 and (101). We also reported that tilianin, a major component of Agastache rugosa (Labiatae), suppresses the TNF-α-induced expression of VCAM-1 in human umbilical vein endothelial cells by inhibiting NO production via inducible nitric oxide synthase (102). However, despite numerous in vitro and animal studies, results of clinical trials evaluating the use of antioxidants (e.g., vitamin C and E, carotenoids, N-acetyl-cysteine) as chronic preventative therapy for cardiovascular diseases have been primarily negative (103).…”

Anti-nociceptive and anti-inflammatory activities of the Agastache mexicana extracts by using several experimental models in rodents

“…Flavonoids are well known effective natural anti-inflammatory agents (Ueda et al, 2004) that can produce antispasmodic effect as well (Yonathan et al, 2006). Studies have reported that acacetin and tilianin produce inhibition in the nitric oxide (NO) pathway to produce anti-inflammatory (Nam et al, 2006) and antihypertensive (Herná ndez-Abreu et al, 2009) responses. However, the involvement of NO in nociception has been controversial given that it is described that NO synthesis or inhibition is involved in both the reduction (Sakurada et al, 1992;Beirith et al, 2002;Caruso et al, 2005) and increase of nociceptive response (Kawabata et al, 1993;Abacioglu et al, 2000).…”