• Natural Product Sciences
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• v.20 no.4
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• pp.232-236
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• 2014

Acanthopanax divaricatus var. albeofructus (ADA) is commonly ingested as a traditional medicine or as a component of a health drink in Korea. In this phytochemical study, nine phenolics (1 - 9) and three lignans (10 - 12) were isolated from the MeOH extract of the stems of ADA. Chemical structures were elucidated by comparing spectroscopic data with reported values. Nuclear factor kappa B ($NF-{\kappa}B$) inhibitory activity of the isolated compounds was evaluated using an $NF-{\kappa}B$ luciferase assay in HepG2 cells. Among them, compounds 1, 3 - 8, and 11 showed significant inhibitory effects on $TNF{\alpha}$-induced $NF-{\kappa}B$ transcriptional activity in a dosedependent manner, with $IC_{50}$ values ranging from 13.25 to $37.36{\mu}M$. Further studies on potential anti-inflammatory effects and the benefits of phenolic and lignan components from ADA are warranted.

• The Journal of Internal Korean Medicine
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• v.27 no.4
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• pp.888-894
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• 2006

Objectives : For the purpose of developing new anti-HIV agents from natural sources, the extracts of Ricinus communis were tested for their inhibitory effects on essential enzymes reverse transcriptase (RT), protease and alpha-glucosidase. Inhibition activity of major compounds of Ricinus communis were predicted from quantitative structure activity relationships (QSAR) in silico. Methods and Results : In the anti-HIV-1 RT using enzyme-linked oligonucleotide sorbent assay (ELOSA) method, water and methanol extracts (100ug/ml) of Ricinus communis showed strong activity of 94.2% and 82.7%, respectively. In the HIV-1 protease and alpha-glucosidase inhibition assay, neither water nor methanol extracts of Ricinus communis inhibited the activity of the enzyme to cleave any substrates as oligopeptides and oligosaccharides. Conclusions : We found that for these samples it is possible that the inhibition of the RT in vitro is due to the secondary metabolites of Ricinus communis such as ricinine and quercetin. It would beof great interest to identify the compounds which are responsible for this inhibition, since all therapeutically useful agents up to date are RT inhibitors.

• Korean Journal of Pharmacognosy
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• v.36 no.1 s.140
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• pp.9-16
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• 2005

Twenty eight compounds were isolated from the whole plant of Euphorbia jolkinii and evaluated for inhibitory effect on $5{\alpha}-reductase$ activity. Among the tested compounds, 1-desgalloyl eugeniin, hippomanin A, euphorbin D, exocoecarianin, rugosin E, and pentagalloyl glucose showed potent inhibitory effect on the enzyme activity. The inhibitory potency of rugosin E and euphorbin D, which are dimeric ellagitannins on $5{\alpha}-reductase$ activity, was 7-to 8-fold stronger than that of ${\gamma}-linolenic$ acid.

• Korean Journal of Fisheries and Aquatic Sciences
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• v.43 no.5
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• pp.421-427
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• 2010

To isolate natural antihypertensive substances from edible seaweeds, we screened for and separated active compounds contained in natural Underia pinnatifida, cultural Underia pinnatifida, Laminaria japonica, Sporophylls and Agarum cribrosum. They were extracted using room temperature water, boiling water, acetone, and methanol in turn or using room temperature water, ether, acetone, methanol and boiling water in order. The in vitro antihypertensive activity was quantified as inhibitory efficacy against angiotensin-I converting enzyme (ACE), which is a factor inducing hypertension. For all of the seaweeds tested, the fractions soluble in room temperature water and in boiling water showed the strongest ACE inhibitory effect among the extracted fractions. Conversely, the methanol-extracted fractions for all of the seaweeds tested showed no antihypertensive activity. While the ether and acetone fractions had slight antihypertensive effects. The compounds in the aqueous extracts that had antihypertensive activity were presumed to be polysaccharides, such as fucoidan and alginate.

• YAKHAK HOEJI
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• v.42 no.2
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• pp.125-131
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• 1998

The total ethanol extract of Angelica koreana radix (UmbeUiferae) showed potent inhibitory effect on tumor necrosis factors (TNF-${\alpha}$) production from LPS-stimulated RAW 264.7 cells in screening studies on 118 Korean medicinal plants. The activity-guided fractionation of the total ethanol extract resulted in the isolation of 4 compounds, including active substances. The chemical structures of the compounds isolated were established by chemical and spectrometric analyses as imperatorin, isoimperatorin, osthol and oxypeucedanin. Among them, osthol, oxypeucedariin and isoimperatorin showed significant inhibitory activities on TNF-${\alpha}$ production as 54.3${\pm}$2.1%, 33.6${\pm}$1.0% and 17.7${\pm}$3.0%, respectively, at 12.5${\mu}$g/ml.

• YAKHAK HOEJI
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• v.42 no.4
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• pp.353-358
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• 1998

The MeOH extract of the bark of Paeonia moutan showed potent inhibitory effect on the mushroom tyrosinase activity in vitro. The activity-guided fractionation of t he MeOH extract resulted in the isolation of three active compounds. The chemical structures of these compounds were elucidated by chemical and spectroscopic evidence as catechin, 1,2,3,6-tetra-O-galloyl-${\beta}$-D-glucose and 1,2,3,4,6-penta-0-galloyl-${\beta}$-D-glucose, respectively. Among them, the inhibitory activity by 1,2,3,6-tetra-galloyl-${\beta}$-D-glucose on mushroom tyrosinase was more potent $(IC_{50}=3.5\;{\mu}M)$ than that of kojic acid $(IC_{50}=8.7\;{\mu}M)$ ,but catechin enhanced the mushroom tyrosinase activity 50% in the concentration of 34.5M.

• Journal of Ecology and Environment
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• v.29 no.4
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• pp.337-342
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• 2006

The total monoterpenoid content of the pine litter layer and the availability of these compounds as inhibitors/stimulators on Polysphondylium violaceum of cellular slime molds were investigated. In order to determine the several monoterpenoids in the natural environment, we examined their concentrations in fresh, senescent, and decaying needles from 3 pine species (Pinus densiflora, P. thunbergii, P. rigida) by litter bag method. Total monoterpenoid content was highest in the fresh needles, but also remained relatively high in senescent needles. The effect of monoterpenoids identified from Pinus plants on the growth of P. violaceum was studied. We tested four concentrations (1, 0.1, 0.01, and $0.001\;{\mu}g/{\mu}L$) of each compound by using a disk volatilization technique. Each compound was treated after germination of spores of P. violaceum. All of the compounds at $1\;{\mu}g/{\mu}L$ concentration had a very strong inhibitory effect on cell growth of P. violaceum. Fenchone at all concentrations, myrcene, verbenone, bornyl acetate, and limonene at low concentrations stimulated the growth of P. violaceum. These results suggest that inhibitory or enhancing effects of selected monoterpenoids depend upon the concentration of the individual compound.

• Natural Product Sciences
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• v.22 no.2
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• pp.102-106
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• 2016

A methanolic extract of Corydalis ternata having aldose reductase inhibitory activity was examined as a possible aldose reductase (ALR2) inhibitor, a key enzyme involved in diabetic complications. Seven alkaloids, tetrahydrocoptisine (1), corydaline (2), tetrahydropalmatine (3), isocorybulbine (4), corybulbine (5), dehydrocorydaline (6), and N-methyltetrahydroberbinium (7) were isolated from $CHCl_3$ fraction of C. ternata methanol extract. Among them, compounds 1, 5, and 7 exhibited $5.04{\pm}1.97%$, $5.00{\pm}1.26%$, and $1.80{\pm}2.33%$ inhibitions, respectively at $40{\mu}M$. The activities of the single compounds were not comparable to that of the whole extract, suggesting that the whole combination of each single compound was responsible for the activity of the extract as shown in many cases of natural medicines. Even though this is the second report on aldose reductase inhibition activity of C. ternata, recombinant human aldose reductase was employed in this study unlike in the previous report. Furthermore, the aldose reductase inhibitory activities of isocorybulbine, corybulbine, and N-methyltetrahydroberbinium, to the best of our knowledge, were evaluated for the first time in this study. These results suggest a use of the extract of C. ternata for ameliorating diabetic complications.

• YAKHAK HOEJI
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• v.50 no.4
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• pp.278-286
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• 2006

Classical dihydropyrrole[3,4-f]quinazoline antifolates 7,8 and 9, in which the tricyclic ring is structurally similar to the pteridine ring of $CH_2-THF(1)$, the cofactor of thymidylate synthase (TS), were synthesized, and their in vitro antitumor activity was evaluated by measuring the cell growth inhibitory activity against cancer cell lines. The target compounds were cytotoxic against CCRF-CEM, human T-cell acute lymphoblastic leukemia, with the cell growth inhibitory activity $(IC_{50})$ of $0.8{\sim}8.3\;{\mu}M$. Among the three compounds, 3-amino analog 7 was 10- and 3.5-fold more cytotoxic compared to the 3-methyl analogs 8 and 9, and its cytotoxicity was similar to that of the reference compound with the $IC_{50}$ value of $0.83\;{\mu}M$. This result was supposed as the consequence of the fact that dihydropyrroloquinazolinone ring with amino group was able to bind well in the active site of TS. In the case of 3-methyl analogs, analog 9, which has two-carbon bridge between the dihydropyrroloquinazolinone ring and benzoyl-L-glutamic acid, was 3-times more potent in cytotoxicity than analog 8 which has one-carbon bridge, and this result indicates that the distance and conformational orientation of the benzoyl-L-glutamic acid moiety with respect to the tricyclic ring may also be a crucial determinant of cell growth inhibitory activity.

• YAKHAK HOEJI
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• v.48 no.5
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• pp.291-296
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• 2004

Sparganium stoloniferum Buch.-Ham. (Sparganiaceae) is a perennial herb which has been used as treatments for menstrual disorder, galactagogue and endometriosis in folk remedies. The Sparganii Rhizoma processed, heated with vinegar, used to different purpose compared with origin in medicine. In order to estimate the different effects between processed (PSR) and unprocessed (USR) Sparganii Rhizoma, extraction and systemic fractionation of the rhizomes were archived. Inhibitory effects of the extracts as well as the fractions of PSR and USR on rat lens aldose reductase and on rat platelet aggregation were investigated for the prevention or the treatment of chronic diabetic complications. Their antioxidant effects, measured using lipid peroxidation of liver tissue and radical scavenging activities on 1,1-diphenyl-picrylhydrazyl in vitro, were evaluated. The most of biological activities tested except rat platelet aggregation, fractions from PSR were shown to exhibit stronger activities than those from USR. It seems that caused by changing of the chemical components by heating process in conditioned with acetic acid. Compounds isolated were shown to significant inhibitory activity on rat lens aldose reductase. Inhibitory activity of compounds isolated on rat lens aldose reductase have been tested in vitro. $IC_{50}$/ (6.31 $\mu$M) of cerebroside I (V) was nearly equal to that (6.32 $\mu$M) of a reference compound, tetrametbylene glutaric acid (TMG).