• Archives of Pharmacal Research
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• v.13 no.1
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• pp.51-54
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• 1990

Effect of scoparone (6, 7-dimethoxycoumarin) on the hepatic cytosolic sulfotransferase activity was investigated. After treatment with scoparone, hepatic cytosolic sulfotransferase activity was increased with odse and time-dependent manner as compared to control. The $V_{max}$ value (control = 1.33 n moles/mg protein/min, scoparone = 2.39n moles/mg protein/min) without affecting the $K_m$ value for p-nitrophenol was increased by the scoparone treatment. Whereas, the hepatic cytosolic sulfotransferase was not changed by the addition of scoparone in vitro, and was strongly inhibited by the addition of metabolites of scoparone. The results obtained suggest that the characteristics of increase in the enzyme activity may include induction of enzyme proteins, and may be due to the metaboltes of scoparone.

• Journal of the Korean Society of Food Science and Nutrition
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• v.27 no.2
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• pp.344-349
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• 1998

The purpose of this study was carried out to investigate the effect of scoparone(6, 7-dimethoxyco-umarin) on liver function. Sprague-Dawley rats were treated with scoparone at a dose of 20mg/kg body weight for 5 days. Hepatic bile flow, liver weight, BSP(bromosulfophthalein) biliary excretion, alanine aminotransferase(ALT) and aspartate aminotransferase(AST) activities, malondialdehyde production and lactate dehydrogenase(LDH) release were assayed. Among them, ALT and AST activities, malondialdehyde production and LDH release were assayed by using primary hepatocyte cultures at a concentration of 0.1mg/ml. Scoparone treatment had no effect on liver weight and hepatic bile flow. Scoparone treatment not only increased BSP biliary excretion, but also recovered the decreased BSP biliary excretion by CCl4, Also scoparone significantly decreased with the increases of ALT and AST activities, malondialdehyde production and LDH release induced by CCl4. These results suggested that scoparone could protect the liver damage by chemicals via promoting the liver excretory function.

• Korean Journal of Pharmacognosy
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• v.23 no.2
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• pp.81-88
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• 1992

The effects of scoparone, one of coumarin derivative on the hepatic bromobenzene metabolizing enzyme system was estimated in rats. Scoparone pretreatment revealed dose-dependently the recovery of decrease in epoxide hydrolase activity due to the bromobenzene(310 mg/kg, i.p.) treatment. And also scoparone and scopoletin (each 5mg/kg, p.o.) pretreatments showed two times increase in the $V_{max}$ values compared to those of bromobenzene-treated group which were calculated from tripartite reciprocal plots. The mode of protective effect of scoparone against bromobenzene induced toxicity is considered to be due to the induction of microsomal enzyme activity by scopoletin, the intermediate metabolite of scoparone. The changes in cytochrome P-450 activity, aminopyrine N-demethylation, aniline hydroxylation and glutathione S-transferation in scoparone-treated group were not significantly different from those of the control group.

• Korean Journal of Clinical Pharmacy
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• v.21 no.1
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• pp.1-5
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• 2011

Purpose: 본 연구는 토끼의 음경해면체 조직에 대한 인진쑥의 에탄올 추출물과 그 성분 중의 하나인 scoparone의 효능을 평가하고자 하였다. Methods: 체중이 2.5-3.0 Kg의 New Zealand백색 가토를 사용하여 음경 전체를 골반골로부터 분리하여 요도를 제거한 후 백막을 보유한 음경해면체를 2 mL organ chamber 관류모형에 연결하고, $10^{-5}M$의 phenylephrine을 관류하여 음경해면체를 수축시킨 후 0.1, 0.5, 1, 2 mg/mL의 에탄올 추출물 또는 $10^{-7}$, $10^{-6}$, $10^{-5}$, $10^{-4}M$의 scoparone을 녹인 용액으로 관류시켜 음경의 장력 변화를 측정하였다. 기존의 발기부전 치료제로 사용되는 실데나필에 대한 인진쑥과의 상호작용을 검토하기 위하여$10^{-6}M$의 scoparone과 $10^{-8}M$의 실데나필을 병용 사용 시 음경해면체 조직에 대한 효과도 함께 검토하였다. Results: 인진쑥의 에탄올 추출물은 phenylephrine으로 전처리하여 수축시킨 음경해면체 평활근을 농도 의존적으로 효과적으로 이완시켰으며 scoparone도 음경해면체 조직에 대한 이완작용 또한 농도 의존적으로 강한 효과를 나타내었다. 실데나필로 전처리한 음경해면체 조직에 대한 scoparone의 효과는 scoparone만을 단독으로 관류시킨 조직에서의 효과보다 강하게 나타났으며 실데나필과 scoparone의 병용사용은 실데나필의 효능을 2배 이상 증가시켰다. Conclusions: Scoparone은 실데나필의 음경해면체평활근 작용을 증가시킴으로써 실데나필에 완전히 반응하지 않는 환자들의 발기부전 치료효과 향상에 유용할 것으로 전망된다.

• Journal of Applied Biological Chemistry
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• v.62 no.4
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• pp.425-431
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• 2019

Platelet activation is essential for hemostatic process on blood vessel damage. However, excessive platelet activation can cause some cardiovascular diseases including atherosclerosis, thrombosis, and myocardial infarction. Scoparone is commonly encountered in the roots of genus Artemisia or Scopolia, and has been studied for its potential pharmacological properties including immunosuppression and vasorelaxation, but antiplatelet effects of scoparone have not been reported yet. We investigated the effect of scoparone on human platelet activation prompted by an analogue of thromboxane A₂, U46619. As the results, scoparone dose-dependently increased cyclic adenosine monophosphate (cAMP) levels as well as cyclic guanosine monophosphate (cGMP) levels, both being aggregation-inhibiting molecules. In addition, scoparone strongly phosphorylated inositol 1, 4, 5-triphosphate receptor (IP3R) and vasodilator-stimulated phosphoprotein (VASP), substrates of cAMP dependent kinase and cGMP dependent kinase. Phosphorylation of IP₃R by scoparone resulted in inhibition of Ca²⁺ mobilization in calcium channels in a dense tubular system, and phosphorylation of VASP by scoparone led to an inability of fibrinogen being able to bind to αIIb/β3. Finally, scoparone inhibited thrombin-induced fibrin clotting, thereby reducing thrombus formation. Therefore, we suggest that scoparone has a strong antiplatelet effect and is highly probable to prevent platelet-derived vascular disease.

• Toxicological Research
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• v.3 no.2
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• pp.121-128
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• 1987

Protective effect of scoparone against the acetaminophen inducible hepatic toxicity in mice was investigated. Scoparone (5mg/kg) was administered intraperitoneally to mice daily for 5 days. Scoparone pretreatment before the administration of acetaminophen has blocked subsequent increases in liver to body weight ratio. When biological changes were measured, scoparone protects against acetaminophen inducible hepatotoxicity in mice as evidenced by the decreased formation of lipid peroxide, lowered serum transaminase activity and the decreased level of serum acetaminophen. In conjuction with the results of Huh (Arch. Pharm. Res. 10, 165(1987)), these results suggest that the most likely mechanism for the observed protective effects of scoparone against the acetaminophen-induced hepatotoxicity is the induction of hepatic microsomal UDP-glucuronyltransferase activity.

• Archives of Pharmacal Research
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• v.10 no.3
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• pp.165-168
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• 1987

The effect of scoparone on UDP glucuronyltransfearase in mouse hepatic microsomes was studied. After transment with scoparone, hepatic microsomal UDP glucuronyltransferase activity was increased with dose-dependent manner as compared to control. The V$_max$ value (control = 23.2 n moles/mg protein/min, scoparone = 31.2 n moles/ mg protein /min) without affecting the $K_m$ value (414 $\mu$M) for p-nitrophenol was increased by the scoparone treatment, and the pattern of kinetic studies for UDP-glucuronic acid was also similar to those of p-nitrophenol. Whereas, the hepatic microsomal UDP glucuronyl-transferase was not changed by the addition of scoparone in vitro. The results obtained suggest that the characteristics of increase in the enzyme activity may include induction of enzyme proteins.

• The Plant Pathology Journal
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• v.17 no.5
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• pp.271-275
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• 2001

Phytoalexin scoparone (6,7-dimethoxycoumarin) was induced in flavedo tissue of lemon fruit inoculated with Penicillium digitatum during heat treatment for 3 days at $36^{\circ}$. The compound was also induced in the flavedo tissue after UV illuminatiion. Induction of scoparone was deteected in the flavedo tissue by histological analysis. This fluorescent scoparone accumulated only on the 4-5 layers of cells adjacent to the inoculation site. Preinoculation with P. digitatum and subsequent heat-treatment induced resistance in the lemon fruit tissues after challenge-inoculation at the site of the first infection. the data obtained in the study suggest that lemon fruit acquired resistance against P. digitatum parallel with the scoparone production at the infection site.

• Journal of Applied Biological Chemistry
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• v.63 no.2
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• pp.131-136
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• 2020

When blood vessels are damaged, a fast hemostatic response should occur to minimize blood loss and maintain normal circulation. Platelet activation and aggregation are essential in this process. However, excessive platelet aggregation or abnormal platelet aggregation may be the cause of cardiovascular diseases such as thrombosis, stroke, and atherosclerosis. Therefore, finding a substance capable of regulating platelet activation and suppressing agglutination reaction is important for the prevention and treatment of cardiovascular diseases. 6,7-Dimethoxy-2H-chromen-2-one (Scoparone), found primarily in the roots of Artemisia or Scopolia plants, has been reported to have a pharmacological effect on immunosuppression and vasodilation, but studies of platelet aggregation and its mechanisms are still insufficient. This study confirmed the effect of scoparone on collagen-induced human platelet aggregation, TXA₂ production, and major regulation of intracellular granule secretion (ATP and serotonin release). In addition, the effect of scoparone on the phosphorylation of the phosphoproteins PI3K/Akt and mitogen-activated protein kinases (MAPK) involved in signal transduction in platelet aggregation was studied. As a result, scoparone significantly inhibited the phosphorylation of PI3K/Akt and MAPK, which significantly inhibited platelet aggregation through TXA₂ production and intracellular granule secretion (ATP and serotonin release). Therefore, we suggest that scoparone is an antiplatelet substance that regulates the phosphorylation of phosphoproteins such as PI3K/Akt and MAPK and is of value as a preventive and therapeutic agent for platelet-derived cardiovascular disease.

• Archives of Pharmacal Research
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• v.25 no.3
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• pp.280-284
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• 2002

Six compounds were isolated from the fruits of Acanthopanax sessiliflorus. Their structures were elucidated as (-)-sesamin, scoparone, protocatechuic acid, ursolic acid, hyperin and 5-hydroxymethylfurfural by physicochemical and spectroscopic analysis. Among them, scoparone, ursolic acid and 5-hydroxymethylfurfural were isolated for the first time from Acanthopanax species.