• Archives of Pharmacal Research
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• 제28권12호
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• pp.1341-1344
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• 2005

Bioassay-guided fractionation of $CHCl_{3}$ extract from the fermentation broth of a sponge Mycale plumose-derived actinomycete Saccharopolyspora sp. nov., led to the isolation of two known prodigiosin analogs - metacycloprodigiosin (1) and undecylprodigiosin (2). These compounds exhibited significant cytotoxic activities against five cancer cell lines: P388, HL60, A-549, BEL­7402, and SPCA4. This is the first report on the significant cytotoxicity of metacycloprodigiosin (1) against human cancer cell lines.

• 대한약학회:학술대회논문집
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• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2-2
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• pp.206.2-206.2
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• 2003

In continuing search for bioactive compounds from Korean marine algae, we found cholinesterase-inhibitory activity in the methanolic extract of brown alga Sargassum sagamianum. After partitioning between CHCl$_3$ and 30% MeOH, the former layer was purified by a series of ODS flash, silica column, gel-filtration on Sephadex LH-20, and HPLC to give two farnesylacetone derivatives. Their structures were identified by comparison with the literature data. Compounds 1 and 2 showed moderate acetylcholinesterase and butyrylcholinesterase inhibitory activities with IC$\sub$50/ values of 65.0∼48.0 ${\mu}$M and 34.0∼23.0 ${\mu}$M, respectively. (omitted)

• Preventive Nutrition and Food Science
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• 제17권1호
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• pp.22-28
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• 2012

Melaleuca leucadendron L. has been used as a tranquilizing, sedating, evil-dispelling and pain-relieving agent. We examined the effects of M. leucadendron L. extracts on oxidative stress and inflammation. M. leucadendron L. was extracted with methanol (MeOH) and then fractionated with chloroform ($CHCl_3$) and butanol (BuOH). Antioxidant activity of the MeOH extract and BuOH fraction were higher than that of both ${\alpha}$-tocopherol and butyrated hydroxytoluene (BHT). Total phenol content in the extracts of M. leucadendron L., especially the BuOH fraction, well correlated with the antioxidant activity. The anti-inflammatory activity of BuOH extracts were investigated by lipopolysaccharide (LPS)-induced nitric oxide (NO) and prostaglandin $E_2$ ($PGE_2$) production, and cyclooxygenase-2 (COX-2) expression in RAW 264.7 macrophages. The BuOH fraction significantly inhibited LPS-induced NO and $PGE_2$ production. Furthermore, BuOH extract of M. leucadendron L. inhibited the expression of COX-2 and iNOS protein without an appreciable cytotoxic effect on RAW264.7 cells. The extract of M. leucadendron L. also suppressed the phosphorylation of inhibitor ${\kappa}B{\alpha}$ ($I{\kappa}B{\alpha}$) and its degradation associated with nuclear factor-${\kappa}B$ (NF-${\kappa}B$) activation. Furthermore, BuOH fraction inhibited LPS-induced NF-${\kappa}B$ transcriptional activity in a dose-dependent manner. These results suggested that M. leucadendron L. could be useful as a natural antioxidant and anti-inflammatory resource.

• Natural Product Sciences
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• 제17권2호
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• pp.85-89
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• 2011

Bioassay-guided fractionation of the $CHCl_3$-soluble fraction of a MeOH extract of the fruiting bodies of Hygrophorus russula led to the isolation of five ergosterol derivatives (1 - 5). The structures of these compounds were identified as ergosterol peroxide (1), ergosta-4,6,8(14),22-tetraen-3-one (2), ergosta-7,22-diene-3${\beta}$,5${\alpha}$,6${\alpha}$-triol (3), ergosta-7,22-diene-3${\beta}$,5${\alpha}$,6${\beta}$,9${\alpha}$-tetraol (4), and 5${\alpha}$,6${\alpha}$-epoxy-ergosta-8(14),22-diene-3${\beta}$,7${\alpha}$-diol (5) by comparing their physicochemical and spectral data with those in the literature. These compounds were evaluated for in vitro cytotoxicity against A549 and XF498 cancer cell lines. Most of the tested compounds, except for compound 3, exhibited moderate cytotoxicity against both A549 and XF498 cell lines with $IC_{50}$ values ranging from 10.2 to 18.3 ${\mu}g/ml$ and from 11.4 to 24.6 ${\mu}g/ml$, respectively.

• Biomolecules & Therapeutics
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• 제7권4호
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• pp.371-376
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• 1999

By cytotoxicity screening of the 65 Korean medicinal plants against leukemia L1210 and P388D$_{1}$ cell line using the MTT assay in vitro, Albizzia julibrissin was studied. This plant was extracted with MeOH and MeOH extract was solvent-fractionated with CHCl$_{3}$, EtOAc and n-BuOH in sequence. Each fraction by various solvents system was purified by column chromatography and preparative TLC, and four compounds were isolated. The structure of each compound was deduced from UV, IR, $^{1}$H-HMR, $^{13}$ C-NMR and CI-MS spectral data. The cytotoxic activity ($IC_{50}$/_ of the compounds, quercetin-3-rhamnoside, 4',5,7-trihydroxyfla-van-3-glucoside, spinasterol-3-glucoside and acacic acid lactone, were evaluated as 5 $\mu\textrm{g}$/ml, 2$\mu\textrm{g}$/ml, 1 $\mu\textrm{g}$/ml against L1210 and as 9$\mu\textrm{g}$/ml, 10$\mu\textrm{g}$/ml, 1.5 $\mu\textrm{g}$/ml, 1.5 $\mu\textrm{g}$/ml and 0.9 $\mu\textrm{g}$/ml against P388D$_{1}$, respectively.

• 농업과학연구
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• 제45권3호
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• pp.509-519
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• 2018

This study was investigated the anti-oxidant property and neuro-protective effect of Cirsium japonicum var. maackii (CJM) against oxidative stress in hydrogen peroxide ($H_2O_2$)-induced C6 glial cells. We measured the 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical, hydroxyl radical (${\cdot}OH$), and superoxide ($O_2{^-}$) radical scavenging activities of an ethanol extract and four fractions [n-Butanol, ethyl acetate (EtOAc), $CHCl_3$, and n-Hexane] from CJM. The results of this study show that the extract and all fractions from CJM had a dose-dependent DPPH radical scavenging activity. In particular, the EtOAc fraction exhibited the strongest scavenging effect with 88.23% at a concentration of $500{\mu}g/mL$. In addition, the EtOAc fraction from CJM also effectively scavenged ${\cdot}OH$ radicals and $O_2{^-}$ radicals, compared to other extract and fractions. In C6 glial cells, $H_2O_2$ markedly decreased the cell viability as well as increased lactate dehydrogenase (LDH) release and reactive oxygen species (ROS) production. However, the EtOAc fraction of CJM attenuated the cellular damage from the oxidative stress by elevating the cell viability and inhibiting the LDH release and ROS over-production compared with the $H_2O_2$-treated control group. Our findings indicate that the EtOAc fraction from CJM has antioxidant effect and neuro-protective effect against oxidative stress, suggesting that it can be used as a natural antioxidant and therapeutic agent for the prevention of neurodegenerative disorders.

• 한국식품과학회지
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• 제35권1호
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• pp.138-143
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• 2003

쑥갓의 total methanol 추출물이 galactosamine으로 독성을 유발시킨 흰쥐의 일차배양 간세포에서 유리되는 GPT의 활성을 유의성 있게 감소시켜 간세포 보호활성을 보임을 알 수 있었다. Total methanol 추출물을 다시 $CHCl_3$, n-buthanol, $H_2O$ 분획으로 나누어 galactosamine 독성에 의한 간세포 보호작용을 재검색한 결과, 50 ppm의 농도에서 간세포 보호작용을 가지는 대조약물 silybin의 41.3% 보호효과에 비하여 각각 51.2%, 10.6%, 23.1%의 보호활성을 나타내었다. 이 중 가장 활성이 큰 $CHCl_3$, 분획을 가지고 활성의 추적 분리 방법으로 소분획 CH-II, V, VI의 활성 subfraction을 얻고 이를 다시 TLC와 활성검색을 병용하여 CH-(V+VI)-d, -e, -j의 sub-subfraction을 얻을 수 있었으며 이들은 50 ppm의 농도에서 각각 41.3%, 51.3%, 47.3%의 보호활성을 보였다. 활성 소분획 CH-II, V, VI는 모두 $[^3H]-uridine$ uptake 시험을 통한 RNA 생합성에는 영향을 미치지 않았으나 total GSH 값은 간세포 보호약물인 silymarin 대조구 $100\;{\mu}M$ 농도에서의 59.7% 수준의 회복효과에 비하여 각각 49.8%, 43.9%, 47.5%의 회복효과를 보였다. 또한 (reduced GSH)/(total GSH) 값도 silymarin $100\;{\mu}M$에서의 0.850에 비하여 각각 0.871, 0.863, 0.872로 유사한 수치를 타나내었다. 이 연구결과로 쑥갓의 간세포 보호작용을 처음으로 검색, 확인하였으며 컬럼 크로마토그래피를 이용하여 활성이 있는$CHCl_3$ 소분획을 분리하였으므로 이들 소분획으로 부터 더욱 활성물질을 순수분리하여 그 구조를 밝히고 간세포 보호활성의 기전에 대하여도 다양한 방향의 연구가 수행되어야 할 것이다.

• Natural Product Sciences
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• 제17권4호
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• pp.267-272
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• 2011

In our search for bioactive phenolics from plants, the culms of Phyllostachys bambusoides has been selected for investigation of anti-cariogenic and 1,1-diphenylpicrylhydrazyl (DPPH) radical scavenging agents based on the initial screening results. Fractionation process of n-hexane and $CHCl_3$ extracts afforded four phenolic constituents, ferulic acid (1), vanillin (2), coniferaldehyde (3), and coniferyl alcohol (4) as guided by their DPPH free radical scavenging activities. Additionally, activity-guided fractionation of EtOAc extract with anti-cariogenic activity has resulted in the isolation of coniferaldehyde (3), 2,6-dimethoxy-p-benzoquinone (5), p-methoxycinnamic acid (6), (${\pm}$)-balanophonin (7), and 6-methoxychromanone (8). The structures of 1 - 8 were determined by spectroscopic data interpretation, and also by comparison of their data with the published values. Phenolic compounds 1 - 4 exhibited similar DPPH radical scavenging activities compared with the synthetic antioxidant, butylated hydroxytoluene (BHT), and compounds 3 and 5 - 8 showed significant antibacterial activity against cariogenic oral streptococci, Streptococcus mutans and S. sobrinus.

• 한국식생활문화학회지
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• 제19권2호
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• pp.170-176
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• 2004

천연첨가물검색의 일환으로 초피의 용매 추출물의 항산화성과 항균성을 실험하고, 소비자의 수용도를 검토하기 위하여 초피를 첨가한 육원전의 관능 검사를 실시한 결과는 다음과 같았다. 1. 초피 용매 추출물들의 옥수수유에 대한 항산화 효과는 가장 많이 사용되는 합성항산화 제인 BHT과 같은 농도에서 BUex는 월등히 높았으며, MEex, EAex는 유사한 경향을 나타냈다. 2. 초피의 용매 추출물의 중 CHex와 BUex가 Escheria coli, Salmonella typhimurium, Psudomonas aeruginosa, Staphylococcus aureus, Bacillus cereus 및 Listeria monocytogenes 모두에 대하여 항균효과를 보였다. 3. 초피 가루를 식품에 첨가하여 제조한 육완자전에 대한 소비자의 기호도를 검사한 결과는 0.1%를 첨가한 경우는 초피를 첨가하지 않은 본래의 육완자전과 같은 수준의 기호도를 나타내므로써(P<0.05) 초피 가루에 의한 이미(異味)가 없어 육와자전 제조에 초피가루를 사용 할 수 있을 것으로 사료된다.

• 한국자원식물학회지
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• 제19권6호
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• pp.660-664
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• 2006

The aerial part of Siegesbeckia pubescens (Compositae) has been used to treat rheumatoid arthritis and hypertension in the Oriental medicine. This crude drug has been used without process (SP-0) or with three times-process of steaming and drying (SP-3) or the nine times of that process (SP-9). To search for the antinociceptive anti-inflammatory components from this crude drug, activity-directed fractionation was performed on this crude drug. Since the $CHCl_3$ extract was shown to have a more potent effect than other extracts, it was subjected to silica gel & ODS column chromatography to yield two diterpene compounds (1). Compound 1 was structurally identified as ent-16 (H, 17-hydroxykauran-19-oic acid, which were tentatively named siegeskaurolic acid A. A main diterpene, siegeskaurolic acid A was tested for the antiiflammatory antinociceptive effects using both hot plate- and writhing anti-nociceptive assays and carrageenan-induced anti-inflammatory assays in mice and rats. Pretreatment with siegeskaurolic acid A (20 and 30mg/kg) significantly reduced the stretching episodes, action time of mice and carrageenan-induced edema. These results support that siegeskaurolic acid is a main diterpene responsible for antinociceptive and antiiflammatory action of S. pubescens. In addition, the assays on SP-0, SP-3 and SP-9 produced the experimental results that SP-9 had more significant effects than other two crude drugs. These results suggest that the processing on the original plant may lead to the higher pharmacological effect.