• 약학회지
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• 제10권2_3호
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• pp.20-24
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• 1966

Pharmacological principles were isolated from Artemisia messer-schmidtiana B$_{ESSER}$ var. viridis B$_{ESSER}$ which has long been used as a cholagogic drug. These substances were identified as esculetin-6-methylether and esculetin-7-methylether and the latter has not yet been found in nature. Both of them possess cholagogic activity.

• 생약학회지
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• 제1권4호
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• pp.115-118
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• 1970

Antihepatotoxic effect of dimethyl-esculetin, the major constituent of herbal drug Artemisia capillaris $T_{HUNBERG}$ (Compositae) which has long been used as folk medicine for gall stone and hepatitis in Asian country (China and Japan, except Korea) was investigated on the rabbit intoxicated with carbon-tetrachloride. Ten rabbits were divided into two parts, group A and B in five each. The group A was injected with carbon-tetrachloride, 0.1ml per kg at begining of the experiments for control. The group B was injected with carbon-tetrachloride soon after 7 days treatment of dimethyl-esculetin, 30mg per day. The results obtained in this experiment were as follows.: 1) Antihepatotoxic activity of dimethyl esuletin on the rabbits intoxicated with carbon tetrachloride has shown the serum glutamic oxaloacetic transaminase activity and serum glutamic pyruvic transaminase activity decreased respectively. 2) The component of Artemisia capillaris, dimethyl-esculetin, has shown remarkable antihepatotoxic effect.

• Journal of Crop Science and Biotechnology
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• 제11권3호
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• pp.187-192
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• 2008

The effects of some coumarins(coumarin, 7-hydroxycoumarin, scopoletin and esculetin) were investigated on pumpkin(Cucurbita maxima Duch.) seedlings and on pumpkin glutathione S-transferases(GSTs). Coumarin and esculetin suppressed the growth of seedlings, especially the elongation of roots as well as hypocotyls. Among the compounds tested, only esculetin inhibited the activity of a particular pumpkin GST by 50%, CmGSTU3 toward 1-chloro-2, 4- dinitrobenzene(CDNB) and at a concentration of 22 ${\mu}M$. Both ethylacetae(EtOAc) and water fractions in pumpkin seedlings and different organs of one-month-old pumpkin plants contained esculetin or similar hydrophobic fluorescent substances as well as hydrophilic substances, which showed different degrees of inhibitory effects on CmGSTU3 activity.

• 생명과학회지
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• 제19권2호
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• pp.249-255
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• 2009

Esculetin, a coumarin compound, has been known to inhibit proliferation and induce apoptosis in several types of human cancer cells. However, the molecular mechanisms involved in esculetin-induced apoptosis are still uncharacterized in human leukemia cells. In this study, we have investigated whether esculetin exerts anti-proliferative and apoptotic effects on human leukemia U937 cells. It was found that esculetin could inhibit cell viability in a time-dependent manner, which was associated with the induction of apoptotic cell death such as increased populations of apoptotic- sub G1 phase. Apoptosis of U937 cells by esculetin was associated with an inhibition of Bcl-2/Bax binding activity, formation of tBid, down-regulation of X-linked inhibitor of apoptotic protein (XIAP) expression, and up-regulation of death receptor 4 (DR4) and FasL expression. Esculetin treatment also induced the degradation of ${\beta}$-catenin and DNA fragmentation factor 45/inhibitor of caspase-activated DNase (DFF45/ICAD). Furthermore, a caspase-3 specific inhibitor, z-DEVD-fmk, significantly inhibited sub-G1 phase DNA content, morphological changes and degradation of ${\beta}$-catenin and DEE45/ICAD. These results indicated that a key regulator in esculetin-induced apoptosis was caspase-3 in human leukemia U937 cells.

• Preventive Nutrition and Food Science
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• 제19권4호
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• pp.321-326
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• 2014

In this study, we developed a method to quantify esculetin (6,7-dihydroxycoumarin) in plasma and tissues using HPLC coupled with ultraviolet detection and measured the level of esculetin in rat plasma after oral administration. The calibration curve for esculetin was linear in the range of 4.8 ng/mL to 476.2 ng/mL, with a correlation coefficient ($r^2$) of 0.996, a limit of detection value of 33.2 ng/mL, and a limit of quantification value of 100.6 ng/mL. Recovery rates for the 95.2 ng/mL and 190.5 ng/mL samples were 95.2% and 100.3%, within-runs and 104.8% and 101.0% between-runs, respectively. The relative standard deviation was less than 7% for both runs. In the pharmacokinetic analysis, the peak plasma esculetin level was reached 5 min after administration ($C_{max}=173.3ng/mL$; $T_{1/2}=45min$; $AUC_{0{\sim}180min}=5,167.5ng{\cdot}min/mL$). At 180 min post-administration (i.e., after euthanasia), esculetin was only detectable in the liver ($30.87{\pm}11.33ng/g$) and the kidney ($20.29{\pm}7.02ng/g$).

• 대한화장품학회지
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• 제49권3호
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• pp.277-283
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• 2023

물푸레나무(Fraxinus rhynchophylla Hance, F. rhynchophylla)는 동아시아에서 널리 사용되어 온 전통적인 약용 식물로, 만성 기관지염, 세균성 이질과 시력 개선 등을 위해 사용돼 왔다. 물푸레나무에는 esculin, esculetin, fraxin 및 fraxetin과 같은 다양한 형태의 쿠마린이 존재하며, esculetin은 항산화, 항염, 항균, 항암 및 아토피성 피부 염증 완화 등의 효과를 가지고 있다. 지금까지 물푸레나무 내 유효 성분을 증가시키는 공정개발에 관한 연구는 보고되지 않았다. 따라서 본 연구의 목적은 물푸레나무 내 esculetin함량을 증가시키고, 항염 및 항산화 효능을 증대시키기 위한 물푸레나무 생물전환 공정을 개발하는 것이다. 당분해효소 viscozyme L을 이용하여 물푸레나무에 처리한 결과 물푸레나무 효소처리물(FRE-VL)은 물푸레나무 추출물(FRE)대비 esculetin 함량이 3.1배 증가하였으며, 항염 활성 증대와 DPPH 라디칼 소거 활성의 효과를 나타내었다. 본 연구를 통해 화장품 분야에서 생물전환 기술을 적용한 물푸레나무 효소처리물의 신규 화장품 기능성 소재로의 활용 가능성을 확인하였다.

• Archives of Pharmacal Research
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• 제23권3호
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• pp.237-239
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• 2000

The antioxidant activity of Artemisia montana was determined by measuring the radical scavenging effect on 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical and inhibitory activity against free radical generation of hepatocytes ($AC_2$F). The methanol extract of A. montana showed strong radical scavenging activity at a concentration of $10.1{\mu}g/m{\ell}$, and thus fractionated by solvent extraction. Esculetin and luteolin 7-O-rutinoside (scolymoside) were isolated as the active principles from the EtOAc and interphase fractions, respectively. The antioxidant activity of these compounds were comparable to that of L-ascorbic acid.

• 한국생명과학회:학술대회논문집
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• 한국생명과학회 2007년도 제48회 학술심포지움 및 추계국제학술대회
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• pp.41.2-41.2
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• 2007

See Full Text

• Journal of Applied Biological Chemistry
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• 제65권1호
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• pp.33-41
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• 2022

Esculetin (also known as 6, 7-dihydroxycoumarin) a type of coumarin, has been exhibited anti-inflammatory and anti-aging effects. Biorenovation is the microbe-mediated enhancement of biological efficacies and structurally diversified compounds relative to their substrate compounds. The production of different kinds of esculetin derivatives using Bacillus sp. JD3-7 and their effects on lipopolysaccharide (LPS)-triggered inflammatory response in RAW 26.7 cells were assessed. One of the biorenovation products, identified as esculetin 6-O-phosphate (ESP), at concentrations of 1.25, 2.5, and 5 μM inhibited the LPS-stimulated production of inflammation markers of nitric oxide synthase 2 and cyclooxygenase 2 as well as their respective enzymatic reaction products of nitric oxide and prostaglandin E2 in the order of increasing concentrations (1.25, 2.5, and 5 μM). Additionally, ESP treatment suppressed the LPS-stimulated secretion of pro-inflammatory cytokines of interleukin (IL)-1β, IL-6, and tumor necrosis factor- α. Furthermore, these anti-inflammatory effect of ESP was associated with the downregulation of mitogen-activated protein kinase signaling, that is, extracellular signal-regulated kinase, c-Jun NH2-terminal kinase, and p38 mitogen-activated protein kinase signaling pathways. This study would therefore provide interesting insights into the biorenovation-assisted generation of a novel anti-inflammatory compound. ESP may be used to develop treatments for inflammatory disorders.

• KSBB Journal
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• 제15권2호
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• pp.120-124
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• 2000

한국산 재배인삼과 장뇌산삼 그리고 중국산 장뇌산삼에 포함되어 있는 총 페놀성 성분 함량에는 큰 차이가 없었다. 그러나 개별적인 페놀성 성분들의 함량에서는 몇 가지 특정적인 경향을 나타내었다. Cinnamic acid와 p-hydroxybenzoic acid는 재배인삼보다 장뇌산삼에서 각각 3~4배, 2~3배 더 높은 함량을 나타내었다. Esculetin은 한국산 재배인삼과 장뇌산삼에서 중국산 장뇌산삼보다 더 높은 함량 수준을 나타내었는데, KM-1의 경우 $47.2\mu\textrm{g}/g$으로 가장 높았다. Ferulic acid와 caffeic acid의 경우 KM-2에서 가장 높은 수준을 나타내었는데, 인삼의 적변현상에 관련된 성분으로 사료된다. Ester 상태의 총 페놀성 성분 함량은 장뇌산삼에서 재배인삼보다 3~4배 더 높았다. Panax ginseng에 포함되어 있는 페놀성 성분들은 완전한 성장연령이 지난 후에는 총 함량에 있어서 큰 차이를 나타내지 않았지만, 개별적인 페놀성 성분 함량과 존재 형태에 있어서는 서식지별 또는 재배방법 등에 따라 구분되는 함량차이를 나타내었다.