• 대한약학회:학술대회논문집
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• 대한약학회 2002년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2
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• pp.380.2-380.2
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• 2002

Peroxisome proliferator-activated receptor (PPAR)-$\gamma$ is a nuclear hormone receptor family that plays an important role in the transcriptional regulation of genes in cellular lipid and energy metabolism. In our search for Iigands for PPAR-$\gamma$ from natural resources. two phenylpropanoids. 3.4.5-Trimethoxy cinnamylalcohol (1) and 3.4.5- Trimethoxy cinnamaldehyde (2). were isolated as PPAR-$\gamma$ agonists from the MeOH extracts of Zanthoxylum schinifolium Sieb. & ZUCCo (Rutaceae) by activity-guided fractionation. These two compoundS bind and activated PPAR-$\gamma$ transcriptional activity in a dose dependent manner assessed by ligand-binding assay. While the maximum activities for PPAR-$\gamma$ of these compounds were comparable with that of rosiglitazone. which is currently used in the treatment of Type II diabetes. the potency of these compounds were much weaker than rosiglitazone ($ED_{50}$=t.2$\mu\textrm{M}$) with the $ED_{50}$ values of 9.08 and 4.08 $\mu\textrm{M}$. respectively. To examine the structure-activity relationship of phenylpropanoids. we prepared several phenylpropanoid derivatives and measured the activity. We observed that substituents at 4'- position could playa key role in determining the potency for PPAR-$\gamma$ agonistic activity .

• 생명과학회지
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• 제23권2호
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• pp.311-318
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• 2013

예로부터 한방이나 민간요법에서 다양한 약리효능을 가진 약제로 알려져 있는 오미자 열매로부터 항염증 활성을 갖는 유용한 물질을 동정하고자 본 연구를 수행하였다. 먼저 오미자의 hexane 추출물로부터 38개의 분획물을 분리한 다음 각 분획의 항염증 활성을 측정하였다. 그 결과 오미자 분획물 중 생리활성이 높은 SCKH1을 선택하여 활성분획 추적방법을 통해 SCKH1PAIBPB을 분리하였다. SCKH1PAIBPB는 VCAM-1, MCP-1, IL-6 및 IL-8의 발현을 감소시키며, 혈관내피세포와 단핵구 사이의 부착능을 억제시킨다는 사실을 확인할 수 있었다. 따라서 본 연구를 통해 규명된 오미자 분획물 및 SCKH1PAIBPB의 항염증효과 뿐만 아니라 혈관내피세포 증식 및 생존능 촉진작용을 응용하여, 다양한 허혈성질환 뿐만 아니라 염중성질환의 예방 및 치료에 활용할 수 있을 것으로 사료된다.

• 생약학회지
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• 제33권3호통권130호
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• pp.219-223
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• 2002

In order to screen new radical scavenging principle which is expected to be antiaging drug lead, we have isolated 160 strains of the marine-derived fungi and investigated 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging activity for their acetone extracts. The significant activities (>50% Inhibition) were observed in 8 strains of fungi (MFA006, MFA0l4, MFA040, MFA133, MFA139, MFA143, MFA148, MFA153), and among them, MFA153 (Aspergillus parasiticus) showed the most significant radical scavenging activity. The active components were purified by assay-guided isolation to yield two known benzyl alcohols, l53B3 (1) and l53B4 (2), and their structures were determined by physicochemical evidence. Two compounds (1,2) showed the significant radical scavenging activity with $IC_{50}$ values of 0.6 and $1.4{\mu}M$ against DPPH, respectively.

• Natural Product Sciences
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• 제20권4호
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• pp.269-273
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• 2014

Activity guided phytochemical examination of the rhizome of Phragmites communis has led to the isolation of two phenolic acids and two lignans. Structures of these compounds were elucidated as methyl gallate (1), ${\rho}$ -hydroxy cinnamic acid (2), (+) -lyoniresinol (3), (+)-lyoniresinol-9'-O-${\beta}$-D-glucopyranoside (4) by comparisons with previously reported spectral data. To investigate the melanogenesis inhibitory effects of these compounds, the melanin level and tyrosinase activity were examined in B16F10 melanoma cell. Each compound inhibited both tyrosinase activity and melanin synthesis compared with positive control, kojic acid and arbutin. These results suggest that the phenolic compounds from Phragmites communis might be developed as a potent skin whitenting cosmeceuticals.

• Natural Product Sciences
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• 제26권2호
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• pp.158-164
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• 2020

Helicobacter pylori is a well-known pathogen that is responsible for gastric disorders. Overcoming of the antibiotic-resistance is a main barrier to treat H. pylori infection. In our search for anti-H. pylori compounds from natural resources, bioactivity-guided isolation on the ethyl acetate fraction of Fraxinus mandshurica bark that had shown anti-H. pylori activity gave twelve compounds (1 - 12) of six coumarins, three phenylethanoids, two secoiridoids, and a lignan using silica gel column chromatography, Sephadex-LH 20, and recrystallization. The chemical structures were identified by spectroscopic data analysis, including 1D, 2D NMR, and mass spectrometry. Among them, compounds 2, 10, and 11 showed moderate growth inhibitory activity against three strains of H. pylori, compared with positive controls of quercetin and metronidazole. Compounds 5, 6, 8, and 12 exhibited the inhibitory activity against strains 26695 or 43504. This is the first report on the anti-H. pylori activity of this plant and the isolated compounds.

• Archives of Pharmacal Research
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• 제28권2호
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• pp.180-185
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• 2005

In the process of investigating anti-obesity effect of Platycodi Radix, we found that aqueous extract of Platycodi Radix might inhibit intestinal absorption of dietary fat by inhibiting pancreatic lipase (PL) activity. In order to clarify the anti-obesity mechanism of Platycodi Radix, activity-guided isolation was performed to find active components. The total saponin fraction of Platycodi Radix appeared to have a potent inhibitory activity against the hydrolysis of triolein emulsified with phosphatidycholine by pancreatic lipase in vitro. Based on these results, further purification of active components yielded 10 known triterpenoidal saponins, among these compounds, platycodin A, C, D, and deapioplatycodin D exhibited significant inhibitory effects on PL at the concentration of $500\;{\mu}g/mL$ with 3.3, 5.2, 34.8, and $11.67\%$ pancreatic lipase activity vs control, respectively. Platycodin D was found to inhibit the PL activity in a dose-dependent manner. Therefore, the anti-obesity effect of Platycodi Radix might be due to the inhibition of pancreatic lipase by its saponins.

• 약학회지
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• 제47권5호
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• pp.300-306
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• 2003

Rhizoma of Smilax china has been used as anti-inflammatory and analgesic, antiedemic agent in Korean folk medicine. In order to investigate the efficacy of anti-oxidative activity, the activity-guided fractionation and the isolation were performed. Each fractions ($H_2O$ fraction, 20％, 40％, 60％, 100％ MeOH fractions and CHCl$_3$ fraction) was examined antioxidant activity by 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging potential. It was revealed that 40％, 20％ MeOH fractions and $H_2O$ fractions have significant anti-oxidative activity. From 40％ and 20％ MeOH fractions two flavonoid glycosides and one procyanidin were isolated and elucidated apigenin-7-Ο-$\alpha$-L-rhamnopyranosyl(1\longrightarrow2)-$\beta$-D-glucopyranoside, apigenin-7-Ο-$\alpha$-L-rhamnopyranosyl(1\longrightarrow6)-$\beta$-D-glucopyranoside and catechin(4$\alpha$\longrightarrow6)epicatechin through their physicochemical data and IR, FAB-MS, $^{13}$ C-NMR, and $^1$H-NMR analysis with authentics, respectively. The isolated compounds were examined by DPPH method. Apigenin-7-Ο-$\alpha$-L-rhamnopyranosyl(1\longrightarrow2)-$\beta$-D-glucopyranoside and catechin (4$\alpha$\longrightarrow6) epicatechin showed powerful radical scavenging activities on DPPH radical among three compounds.

• Mycobiology
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• 제42권2호
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• pp.185-188
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• 2014

We investigated a total of 335 samples of Korean native mushroom extracts as part of our lipoxygenase (LOX) inhibitor screening program. Among the mushroom-methanolic extracts we investigated, 35 exhibited an inhibitory activity greater than 30% against LOX at a concentration of 100 ${\mu}g/mL$. Especially, Collybia maculata, Tylopilus neofelleus, Strobilomyces confusus, Phellinus gilvus, P. linteus, P. baumii, and Inonotus mikadoi exhibited relatively potent LOX inhibitory activities of 73.3%, 51.6%, 52.4%, 66.7%, 59.5%, 100.0%, and 85.2%, respectively. Bioassay-guided fractionation led to the isolation of inoscavin A from the methanolic extract of P. baumii, which showed the most potent activity and was identified by spectroscopic methods. Specifically, inoscavin A exhibited potent LOX inhibitory activity with an $IC_{50}$ value of $6.8{\mu}M$.

• Food Science and Biotechnology
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• 제17권6호
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• pp.1214-1220
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• 2008

Secondary metabolites from the fruit body of Phellinus linteus were evaluated for their proliferative effect on human osteoblast-like cells. 3-[4,5-Dimethylthiazole-2-y1]-2,5-diphenyl-tetraxolium bromide (MTT) assay and alkaline phosphatase (ALP) activity assay were used to assess the effect those isolates on the human osteoblast-like cell line (Saos-2). Activity-guided fractionation led to the isolation of ALP-activating phenolic compounds through the extraction of P. linteus, solvent partitioning, and repeated silica gel and octadecyl silica gel (ODS) column chromatographic separations. From the result of spectroscopic data including nuclear magnetic resonance (NMR), mass spectrometry (MS), and infrared spectroscopy (IR), the chemical structures of the compounds were determined as 4-(4-hydroxyphenyl)-3-buten-2-one(1), 2-(3',4'-dihydroxyphenyl)-1,3-benzodioxole-5-aldehyde (2), 4-(3,4-dihydroxyphenyl)-3-buten-2-one (3), 3,4-dihydroxybenzaldehyde (4), and protocatechuic acid methyl ester (5), respectively. This study reports the first isolation of compounds 1-3 and 5 from P. linteus. In addition, all phenolic compounds stimulated proliferation of the osteoblast-like cells and increased their ALP activity in a dose-dependent manner ($10^{-8}$ to $10^{-1}\;mg/mL$). The present data demonstrate that phenolic compounds in P. linteus stimulated mineralization in bone formation caused by osteoporosis. The bone-formation effect of P. linteus seems to be mediated, at least partly, by the stimulating effect of the phenolic compounds on the growth of osteoblasts.

• 생약학회지
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• 제41권4호
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• pp.245-249
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• 2010

As part of ongoing study focused on the discovery of natural antioxidants from Korean plants by measuring the DPPH (1,1-diphenyl-2-picrylhydrazyl) radical scavenging effect and superoxide quenching activity, methanol extract of Cedrela sinensis (Meliaceae) was found to show potent antioxidant activities. Subsequent activity-guided fractionation of the methanolic extract led to the isolation of four phenolic compounds, (+)-catechin (1), (-)-epicatechin (2), catechin-($4{\alpha}{\rightarrow}8$)-catechin (3) and catechin-($4{\alpha}{\rightarrow}8$)-epicatechin (4). Their structures were elucidated by spectroscopic studies. These compounds showed the significant antioxidative effects on DPPH. In riboflavin originated superoxide quenching activity, four compounds exhibited the formation of the blue formazan in a dose dependant manner.