Inhibition of 5-lipoxygenase and skin inflammation by the aerial parts of Artemisia capillaris and its constituents

Abstract

The aerial parts of Artemisia capillaris Thunberg (Compositae) have been used in Chinese medicine as a liver protective agent, diuretic, and for amelioration of skin inflammatory conditions. This study was conducted to establish the scientific rationale for treating skin inflammation and to find active principles from A. capillaris. To accomplish these goals, the 70% ethanol extract of the aerial parts of A. capillaris (AR) was prepared and its 5-lipoxygenase (5-LOX) inhibitory action was studied since 5-LOX products are known to be involved in several allergic and skin inflammatory disorders. AR showed potent inhibitory activity against 5-LOX-catalyzed leukotriene production by ionophore-induced rat basophilic leukemia-1 cells, with an IC(50) of < 1.0 μg/mL. Nine major compounds, scopoletin, scopolin, scoparone, esculetin, quercetin, capillarisin, isorhamnetin, 3-O-robinobioside, isorhamnetin 3-O-galactoside and chlorogenic acid, were isolated from A. capillaris, and their effects were examined to identify the active principle(s). Several coumarin and flavonoid derivatives were found to be 5-LOX inhibitors. In particular, esculetin and quercetin were potent inhibitors, with IC(50) values of 6.6 and 0.7 μM, respectively. Against arachidonic acid-induced ear edema in mice, AR, and esculetin strongly inhibited edematic response. AR and esculetin also inhibited delayed-type hypersensitivity response in mice. In conclusion, AR and some of their major constituents are 5-LOX inhibitors, and these in vitro and in vivo activities may contribute to the therapeutic potential of AR in skin inflammatory disorders in traditional medicine.

Capillarisin attenuates exercise-induced muscle damage through MAPK and NF-κB signaling

“…The entire plant was dried and ground into a powder. CAP was isolated and determined by HPLC as described from the previous report (Kwon et al, 2011). …”

Additive effects of Artemisia capillaris extract and scopoletin on the relaxation of penile corpus cavernosum smooth muscle

“…21 Several compounds have been isolated form A. capillaris, including coumarin derivatives such as 6,7-dimethylesculetin, esculetin and scopoletin. 22 Scopoletin (7-hydroxy-6-methoxy-2H-1-benzopyran-2-one) is one of the active components of A. capillaris used as 7-hydroxyl group that demonstrated antioxidant activities 23 and anti-inflammatory activity in vivo. 24 The objective of this study was to clarify the relaxation effects and mechanism of A. capillaris extract (ACE) or scopoletin on penile corpus cavernosum smooth muscle (PCCSM).…”

UPEI-400, a Conjugate of Lipoic Acid and Scopoletin, Mediates Neuroprotection in a Rat Model of Ischemia/Reperfusion

“…The coumarin derivative esculetin has been shown to reduce oxidative stress in several in vitro models [44,45] and demonstrate anti-inflammatory properties in vivo [46,47]. Esculetin has been shown to be neuroprotective in a mouse model of I/R following transient occlusion of the middle cerebral artery [48].…”