• Korean Journal of Medicinal Crop Science
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• v.27 no.3
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• pp.208-217
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• 2019

Background: In the present study, we identified two cytotoxic compounds from the root of Rumex crispus L. using a bioassay-based method. Methods and Results: Compared with the other fractions, the diethyl ether ($Et_2O$) fraction of R. crispus root extract exhibited the strongest of 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical-scavenging effect [scavenging concentration 50% $(SC_{50})=63.8{\pm}1.47{\mu}g/m{\ell}$], nitric oxide (NO) production inhibitory effect on the mouse macrophage cell line RAW264.7 [inhibitory concentration 50% $(IC_{50})=60.9{\pm}7.52{\mu}g/m{\ell}$] and cytotoxicity effect on the human hepatoma cell line, HepG2 [lethal concentration 50% $(LC_{50})=115.4{\pm}1.86{\mu}g/m{\ell}$]. According to the bioassay-based method, two cytotoxic compounds were purified from the $Et_2O$ fraction by using column chromatography and preparative high performance liquid chromatography (prep-HPLC). These two compounds were identified as parietin and chrysophanol by using nuclear magnetic resonance (NMR) and liquid chromatography quadruple time of flight mass spectrometry (LC-QTOF-MS). In addition, both parietin and chrysophanol exhibited a cytotoxicity effect on HepG2 cells, their $LC_{50}$ values were $169.1{\pm}17.67{\mu}M$ and $111.5{\pm}6.62{\mu}M$, respectively. Conclusions: Parietin and chrysophanol isolated from the $Et_2O$ fraction of the R. crispus root extract showed cytotoxicity in HepG2 cell.

• Mycobiology
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• v.51 no.4
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• pp.246-255
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• 2023

Genus Penicillium comprising the most important and extensively studied fungi has been well-known as a rich source of secondary metabolites. Our study aimed to analyze and investigate biological activities, including in vitro anti-cancer, anti-inflammatory and anti-diabetic properties, of metabolites from a marine-derived fungus belonging to P. levitum. The chemical compounds in the culture broth of P. levitum strain N33.2 were extracted with ethyl acetate. Followingly, chemical analysis of the extract leaded to the isolation of three ergostane-type steroid components, namely cerevisterol (1), ergosterol peroxide (2), and (3β,5α,22E)-ergosta-6,8(14),22-triene-3,5-diol (3). Among these, (3) was the most potent cytotoxic against human cancer cell lines Hep-G2, A549 and MCF-7 with IC₅₀ values of 2.89, 18.51, and 16.47 ㎍/mL, respectively, while the compound (1) showed no significant effect against tested cancer cells. Anti-inflammatory properties of purified compounds were evaluated based on NO-production in LPS-induced murine RAW264.7 macrophages. As a result, tested compounds performed diverse inhibitory effects on NO production by the macrophages, with the most significant inhibition rate of 81.37±1.35% at 25 ㎍/mL by the compound (2). Interestingly, compounds (2) and (3) exhibited inhibitory activities against pancreatic lipase and α-glucosidase enzymes in vitro assays. Our study brought out new data concerning the chemical properties and biological activities of isolated steroids from a P. levitum fungus.

• Archives of Pharmacal Research
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• v.26 no.7
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• pp.532-534
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• 2003

Kojic acid dimethyl ether (1), and the known kojic acid mono methyl ether (2), kojic acid (3) and phomaligol A (4) have been isolated from the organic extract of the broth of the marine-derived fungus Altenaria sp. collected from the surface of the marine green alga Ulva pertusa. The structures were assigned on the basis of comprehensive spectroscopic analyses. Each isolate was tested for its tyrosinase inhibitory activity. Kojic acid (3) was found to have significant tyrosinase inhibitory activity, but compounds 1, 2, and 4 were found to be inactive.

• Journal of Microbiology and Biotechnology
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• v.18 no.4
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• pp.682-685
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• 2008

Among thirteen strains of the genus Bacillus isolated from Shrimp-jeotkal in our laboratory, a strain BA34 showing good antifungal activity against Phytophthora infestans in a previous experiment was tested for the inhibitory effect against Akt, protein kinase B. Since Akt is known to play an important role in controlling apoptosis, its inhibitors can be used as potential apoptosis-inducing agents in the treatment of cancer. Two active compounds were isolated and their structures were determined. They have similar structures, despite showing different inhibitory effects. In order to elucidate the reasons for these different effects, three-dimensional studies were carried out.

• Bulletin of the Korean Chemical Society
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• v.26 no.12
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• pp.1975-1980
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• 2005

A series of substituted rutaecarpines were prepared by employing Fischer indole synthesis as key step and their inhibitory activities on COX-1 and 2 as well as selectivity on COX-2 were evaluated. The compounds with a methanesulfonyl and a bromo group at C10 showed promising inhibitory activity ($IC_{50}$ = 0.27, 0.35 $\mu$M, respectively) with selectivity.

• Archives of Pharmacal Research
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• v.28 no.6
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• pp.652-656
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• 2005

A number of thioflavones has been synthesized and evaluated for their iNOS inhibitory activities. Thiowogonin (6) was obtained from naturally occurring chrysin in 5 steps. Other thioflavones were prepared from the corresponding flavones in a single step by the reaction with Lawesson's reagent. The biological activities of thioflavones were not enhanced by the functional group conversion from carbonyl to thiocarbonyl. Compounds 11 and 13 showed potent. NO inhibitory activity at high concentration (40 uM), leading to the possible development of novel neuroprotective agents based on wogonin.

• Archives of Pharmacal Research
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• v.27 no.8
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• pp.825-828
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• 2004

Two triterpenoids (1,4) and two triterpenoid glycosides (2,3) were isolated from the root of Acanthopanax koreanum (Araliaceae). Their structures were identified as impressic acid (1), acankoreoside A (2), 3-epi-betulinic acid 28-O-［(${\alpha}-L-rhamnopyranosyl(1{\rightarrow}4)-{\beta}-D-glucopyrano-syl(1{\rightarrow}6)]-{\beta}-D-glucopyranosyl]$ ester (3), and ursolic acid (4) by physicochemical and spectro-scopic methods. Of these compounds, impressic acid (1) exhibited a potent inhibitory activity against NFAT transcription factor ($IC_{50}:{\;}12.65{\;}{\mu\textrm{m}}$).

• Korean Journal of Pharmacognosy
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• v.33 no.2 s.129
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• pp.144-150
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• 2002

The methanol extracts of 132 herbal medicines were screened for the inhibitory activity against heparinase enzyme from Flavobacterium heparinum. Eleven medicinal plants, Amomum xanthiodides, Agrimonia pilosa, Paeonia lactiflora, Rubia cordifolia, Sanguisorba officinalis, Torrega grandis, Morus alba, Gleditsia sinensis, Crataegus pinnatifida, Cornus officinalis, Paeonia japonica showed potent inhibition on heparinase activity. The active substituents of those herbal medicine could be extracted into butanol fraction and the inhibitory compounds of Morus alba are now isolating.

• Natural Product Sciences
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• v.7 no.2
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• pp.60-62
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• 2001

Ulmus davidiana, Formitella fraxinea, and Aloe vera extracts were detected to have inhibitory effects against topoisomerase I at treatment of $5{\mu}g$. Ulmus davidiana and Aloe vera extracts were found to show inhibitory effect similar to camptothecin, Formitella fraxinea extract was found to have weak activity. We also found the potential use of those extracts as a radiation sensitizer. Radiosensitizing effect at combination treatment was increased more than 2 times at single treatment of radiation, Ulmus davidiana or Formitella fraxinea extracts. Ulmus davidiana and Formitella fraxinea extracts were found to have significant radiosensitizing effect on test tumor cell line. But, Aloe vera extract was not detected to have activity as a radiosensitizer. Ulmus davidiana and Formitella fraxinea extracts are potent radiosensitizers on tumor cell lines and should be considered for further study of active compounds.

• Korean Journal of Pharmacognosy
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• v.34 no.4 s.135
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• pp.314-317
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• 2003

Inhibitory effects of the whole extract and isolated compounds from the leaves of Vaccinium koreanum (Ericaceae) on rat lens aldose reductase (RLAR) and on platelet aggregation were investigated for the prevention or the treatment of chronic diabetic complications. Arbutin, isolated from n-butanol fraction of methanol extract, exhibited a potent inhibitory effects on rat platelet aggregation induced by ADP $(IC_{50}=0.12\;{\mu}M)$ and collagen $(IC_{50}=0.039\;{\mu}M)$ and showed same inhibitory activities with positive control, tetramethylene glutaric acid, on RLAR.