• 한국약용작물학회지
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• 제19권6호
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• pp.426-434
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• 2011

In this study, to evaluate the anti-inflammatory effects of kaempferol and its rhamnosides isolated from Hibiscus cannabinus L. leaves, we investigated UVB-induced inhibitory effects on inflammatory reaction by measuring the cytokine as the prostaglandin ($PGE_2$), interleukine-6 (IL-6) and interleukine-8 (IL-8). We investigated the inhibitory effects of kaempferol and its rhamnosides on TARC (thymus and activation-regulated chemokine) and $PGE_2$. Kaempferol and ${\alpha}$-rhamnoisorobin showed inhibition activity of TARC generated to compared to positive control. Kaempferol, ${\alpha}$-rhamnoisorobin and afzelin Inhibited the release of $PGE_2$. Also, only kaempferol significantly inhibited interleukine-6 (IL-6), interleukine-8 (IL-8) among UVB-induced inflammatory cytokine.

• 한국약용작물학회지
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• 제20권6호
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• pp.454-460
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• 2012

In this study, kaempferol and its rhamnosides (${\alpha}$-rhamnoisorobin, afzelin, kaempferitrin) were isolated electively by bioconversion technology from Hibiscus cannabinus L. leaves to evaluate the anti-wrinkles effects and anti-microbial effects. In order to evaluate anti-wrinkles activity, reduction of expression matrix metalloproteinase-1 (MMP-1) protein and proliferation/ pro-collagen production were investigated. Kaempferol and ${\alpha}$-rhamnoisorobin showed inhibition activity of MMP-1 generated to compared to positive control. In HaCaT cell proliferation assay, kaempferol and ${\alpha}$-rhamnoisorobin significantly promoted cell proliferation in a concentration-dependent manner. In addition, procollagen synthesis assays (by HDF-N cell) showd that TGF-${\beta}$ induced procollagen production and also, all four kinds of experimental significantly promoted procollagen synthesis in a concentration-dependent manner. Kaempferol and ${\alpha}$-rhamnoisorobin exhibited strong antimicrobial activities on five of microbes, Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa, Candida albicans and Aspergillus niger.

• 대한화장품학회지
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• 제37권3호
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• pp.257-264
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• 2011

본 연구에서는 kaempferol 및 그 배당체의 항산화 및 항염증 효능을 평가하기 위해 free radical 소거활성, ROS inhibition assay, TARC 생성 억제 관련 실험을 수행하였다. 또한 kaempferol과 그들의 rhamnosides (${\alpha}$-rhamnoisorobin, afzelin, kaempferitrin)의 구조에 따른 생리적 활성의 상관관계를 조사하였다. Kaempferol과 ${\alpha}$-rhamnoisorobin은 free radical (1,1-diphenyl-2-picrylhydrazyl, DPPH) 소거활성($FSC_{50}$)에서 각각 62.5, 50.0 ${\mu}M$이 측정되었으며 afzelin과 kaempferitrin은 농도와 상관없이 free radical 소거활성을 나타내지 않았다. ROS inhibition assay에서는 시료 농도를 10, 50, 100 ${\mu}M$을 처리한 결과 kaempferol은 대조군(100 %)에 비하여 ROS 발현 농도를 각각 97.5, 57.8, 47.8 %로 감소하였으며 ${\alpha}$-rhamnoisorobin은 93.1, 59.1, 41.4 %의 감소를 나타내었다. TARC (thymus and activation regualted chemokine) 생성 억제능 실험을 통해 시료의 항염증 효능을 평가한 결과 kaempferol은 10, 50, 100 ${\mu}M$ 농도에서 대조군(100 %)에 대비하여 각각 48.8, 5.5, 4.4 %로 농도 의존적으로 TARC 생성을 감소시켰으며, ${\alpha}$-rhamnoisorobin은 88.1, 19.0, 1.0 %로 TARC 생성의 감소 효능을 나타내었다. 결론적으로 kaempferol과 그들의 rhamnoside 중 kaempferol과 ${\alpha}$-rhamnoisorobin은 항산화, 항염증에 대한 우수한 효능을 나타내는 것으로 사료되며 더 나아가서는 항노화 및 항염증에 효과가 있는 기능성 화장품에 응용 가능성이 있음을 시사한다.

• Archives of Pharmacal Research
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• 제27권1호
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• pp.44-47
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• 2004

Loranthus tanakae Fr. et Sav. (Loranthaceae) is a species of mistletoe, a semiparasitic plant growing on the branches of Quercus and Betula species as host trees. In our ongoing search for bioactive compounds from endemic species in Korea, we have investigated to isolate the chemical constituents responsible for the antitumor effect of the MeOH extract of L. tanakae. The ethyl acetate soluble part of the MeOH extract demonstrated a marginal inhibition on the proliferation of the tumor cell lines such as A549 (non small cell lung), SK-OV-3 (ovary), SK-MEL-2 (melanoma), XF498 (central nerve system), and HCT-15 (colon) in vitro. Thus, the activity-guided isolation procedure upon the ethyl acetate soluble part of the extract has been carried out and finally four flavonoid rhamnopyranosides (1-4) were isolated as active principle. The structures of 1-4 were elucidated by the physicochemical and spectral data as rhamnetin 3-O-$\alpha$-L-rhamnoside (1), quercetin 3-O-$\alpha$-L-rhamnoside (2), rhamnocitrin 3-O-$\alpha$rhamnoside (3), and kaempferol 3-O-$\alpha$-L-rhamnoside (4).

• Archives of Pharmacal Research
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• 제22권2호
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• pp.213-218
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• 1999

The antioxidant activity of Eriobotrya japonica was determined by measuring the radical scavenging effect on DPPH (1,1-diphenyl-2-picrylhydrazyl) radical and lipid peroxidation produced when mouse liver homogenate was exposed to the air at $37^{\circ}C$, using 2-thiobarbituric acid (TBA). The methanol extract and its factions of Eriobotrya japonica leaves showed strong antioxidant activity. The antioxidant activity of EtOAc and n-BuOH soluble fractions were stronger than the others, and were further purified by repeated silica gel, MCl gel CHP-20P, and Sephadex LH-20 column chromatography. Antioxidant chlorogenic acid, quercetin-3-sambubioside from n-BuOH fraction and methyl chlorogenate, kaempferol- and quercetin-3-rhamnosides, together with the inactive ursolic acid and$ 2{\alpha}$-hydroxyursolic acid from EtOAc fraction were isolated. Antioxidant flavonoids and chlorogenic acid also showed prominent inhibitory activity against free radical generation in dichlorofluorescein (DCF) method.

• 생약학회지
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• 제30권4호
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• pp.397-403
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• 1999

Tyrosinase plays an important role in the process of melanin polymer biosynthesis. Therefore, the enzyme inhibitors have been of great concern as cosmetics to have skin-whitening effects on the local hyperpigmentation. During the search for new inhibitory compounds on melanin polymer biosynthesis from natural sources, MeOH extracts of 589 higher plants were tested for the inhibitory effect on tyrosinase activity by the muschroom tyrosinase assay in vitro. Among plants tested, the leaves of Cercis chinensis exhibited potent inhibitory effect on mushroom tyrosinase activity. Subsequently seven active compounds were isolated from the ethyl acetate soluble part of acetone extract of the leaves of C. chinensis by the activity guided fractionation monitoring the inhibitory effect on tyrosinase activity. Their chemical structures were identified as $kaempferol-3-0-{\alpha}-L-rhamnoside$, quercitrin, $myricetin-3-0-{\alpha}-L-rhamnoside$, myricetin-3-0-(2'-O-galloyl)- ${\alpha}$ -L-rhamopyranoside (desmanthin), (-)-epicatechin-3-0-gallate, (-)-epigallocatechin-3-0-gallate, and methyl gallate on the basis of the speculation of spectral data and chemical reaction. Among the flavonol rhamnosides, myricetin-3-0-(2'-O-galloyl)- -L-rhamnoside(desmanthin) showed most potent inhibitory effect on tyrosinase activity and the structure of B-ring in flavonol moiety was related to the activity. (-)-Epigallocatechin-3-O-gallate having pyrogallol group in flavan-3-ol moiety exhibited more potent inhibitory effect than (-)-epicatechin-3-0-gallate having catechol group in flavan-3-ol moiety on mushroom tyrosinase activity.