• Archives of Pharmacal Research
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• 제26권9호
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• pp.731-734
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• 2003

Five known kaurane type diterpenoids, 16$\alpha$H, 17-isovaleryloxy-ent-kauran-19-oic acid (1), 16$\alpha$-hydroxy-17-isovaleryloxy-ent-kauran-19-oic acid (2), paniculoside-IV (3), 16$\alpha$-hydroxy-ent-kauran-19-oic acid (4), and ent-kaur-16-en-19-oic acid (5) were isolated from the root of Acanthopanax koreanum by repeated column chromatography and reversed phase preparative HPLC. The structures of these compounds were established from physicochemical and spectral data. Among the isolated compounds 16$\alpha$H, 17-isovaleryloxy-ent-kauran-19-oic acid (1) showed potent inhibitory activity ($IC_50$ value, 16.2 $\mu$ M) on TNF-$\alpha$ secretion from HMC-1, a trypsin-stimulated human leukemic mast cell line.

• Natural Product Sciences
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• 제25권2호
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• pp.115-121
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• 2019

Alzheimer's disease is a chronic neurodegenerative disorder with no curative treatment. The commercially available drugs, which target acetylcholinesterase, are not satisfactory. The aim of this study was to investigate the cholinesterase inhibitory activity of Solenostemma argel aerial part. Eight compounds were isolated and identified by NMR: kaempferol-3-O-glucopyranoside (1), kaempferol (2), kaempferol-3-glucopyranosyl($1{\rightarrow}6$)rhamnopyranose (3) p-hydroxybenzoic acid (4), dehydrovomifoliol (5), 14,15-dihydroxypregn-4-ene-3,20-dione (6), 14,15-dihydroxy-pregn-4-ene-3,20-dione-$15{\beta}$-D-glucopyranoside (7) and solargin I (8). Two of them (compounds 2 and 3) could inhibit over 50 % of butyrylcholinesterase activity at $100{\mu}M$. Compound (2) displayed the highest inhibitory effect against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) with a slight selectivity towards the latter. Molecular docking studies supported the in vitro results and revealed that (2) had made several hydrogen and ${\pi}-{\pi}$ stacking interactions which could explain the compound potency to inhibit AChE and BChE.

• 생약학회지
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• 제51권4호
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• pp.238-243
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• 2020

Perilla frutescens Britton var. acuta Kudo, an annual plant primarily cultivated in China, Japan, and Korea, has been used as a traditional medicine to treat inflammatory diseases, depression, and many anxiety-related disorders. Previously, we reported the inhibitory effects of n-hexane layer of P. frutescens var. acuta extract against beta-amyloid (Aβ) aggregation, and the isolation of asarone derivatives as active constituents from n-hexane layer. In this study, dichloromethane layer of P. frutescens var. acuta was applied to bioassay-guided isolation methods accompanied with Thioflavin T (Th T) fluorescence assay to investigate the inhibitory effect on Aβ aggregation and disaggregation. As the results, three triterpenoids including ursolic acid (1), tormentic acid (2) and corosolic acid (3) were isolated. All compounds reduced Aβ aggregation and increased disaggregation of preformed Aβ aggregates in a dose-dependent manner. However, the inhibitory effect of three compounds on Aβ aggregation was not correlated with antioxidant activity, which was measured by DPPH assay. Taken together, these results suggest that the triterpenoid derivatives from P. frutescens have the potential to be developed as good therapeutics or preventatives for AD.

• Archives of Pharmacal Research
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• 제25권6호
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• pp.856-859
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• 2002

In the course of finding Korean natural products for acetylcholinesterase (AChE) inhibitory activity, we found that a methanolic extract of the roots of Angelica dahurica showed significant inhibitory effects on AChE. Bioassay-guided fractionation of the methanolic extract resulted in the isolation of three furanocoumarins, isoimperatorin (1), imperatorin (2) and oxypeucedanin (3), as active principles. These compounds inhibited AChE activity in a dosedependent manner, and the $IC_{50}$ values of compounds 1-3 were 74.6, 63.7 and 89.1 uM, respectively.

• 대한화장품학회지
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• 제23권3호
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• pp.115-121
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• 1997

To identify inhibitors of melanogenesis, we compared the effects of 5 compounds on mushroom tyrosinase, human melanocytic tyrosinase activity and melanin content. The cytotoxicyty of the components were also tested on cultured human melanoctes. Kojic acid showed marked inhibitory effect both on mushroom and human tyrosinase activity. This action of kijic acid is stronger than that of ascorbic acid. Arbutin inhibited human tyrosinase activity of cultured melanocytes although it had slightly inhibitory effect on mushroom tyrosinase activity. Azelaic acid had no effect on human tyrosinase activity. Melanin production was inhibited significantly by kojic acid and tranexamic acid. MTT assay showed that all of the compounds were non-cytotoxic to melanocytes at the concentrations tested. These results suggest that the effect of kojic acid on cultured meanocytes involve inhibition of tyrosinase activity and melanogenesis without affection the cell number.

• The Korean Journal of Ecology
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• 제19권4호
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• pp.295-304
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• 1996

KDICical substances from Artemisia scoparia were analyzed by gas chromatography. Seven phenolic compounds and thirty nine terpenoids were identified. Most abundant within each group were cinnamic acid and camphor, respectively. The KDICicals were prepared as aqueous extracts and then used for germination, growth, and chlorophyll content tests. The extracts were inhibitory to germination and seedling growth of the receptor lants. This inhibitory effect was dependent on concentration. When the effect of the aqueous extract on chlorophyll content was assayed, both chlorophylls a and b were shown to be reduced. The reduction in seedling elongation and growth in dry weight paralleled the reduction in chlorophyll concentration. These KDICical substances, including phenolic compounds and terpenoids, from Artemisia scoparia were responsible for the growth inhibition of the selected species.

• Natural Product Sciences
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• 제10권3호
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• pp.104-108
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• 2004

Five lignans including gomisin N (1), wuweizisu C (2), gomisin L1 (3), (+)-deoxyschizandrin (4), and gomisin J (5) have been isolated from the fruits of Schizandra chinensis. The structures of the isolated compounds were elucidated by analyzing MS and NMR spectra. Effects of the compounds isolated in this study on the dopamine content in PC12 cells were investigated to evaluate their inhibitory effectiveness. The gomisin N, wuweizisu C, and gomisin J showed 25.4%, 39.8%, and 35.1 %, respectively, inhibition effect on dopamine content in PC12 cells at the concentration of $50\;{\mu}g/ml$.

• 약학회지
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• 제38권6호
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• pp.791-794
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• 1994

Sixteen kinds of naturally occurring phenolic compounds including 5 stilbenes, 7 flavonoids and 4 anthraquinones were examined in the inhibitory activity against rat liver AADC(aromatic L-amino acid decarboxylase) in vitro, using 5-hydroxytryptophan as a substrate. Three hydroxystilbenes, resveratrol 1, rhapontigenin 3 and piceatanol 5, which were known to be monoamine oxidase A inhibitors, exhibited a significant inhibition against AADC($IC_{50}$=20, 8 and $5\;{\mu}M$, respectively). By the comparison of the activity of each phenolic compound, it was suggested that the 3',4'-dihydroxyphenyl group of stilbenes or flavones was the best pharmacophore for the AADC inhibitory activity.

• Bulletin of the Korean Chemical Society
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• 제29권1호
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• pp.43-46
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• 2008

The aim of present study was to examine the inhibitory effects of hydroxamic acid derivatives on the melanogenesis. We found that hydroxamic acid moiety was important for anti-melanogenic activity. Compounds 1a and 1b strongly inhibited melanin synthesis via deactivation of tyrosinase. Hydroxamic acid has metal ion chelating ability which is similar to that kojic acid, however, anti-tyrosinase mechanism of compounds 1a and 1b was different from that of kojic acid. They showed noncompetitive inhibition kinetics

• 한국환경보건학회지
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• 제21권1호
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• pp.74-77
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• 1995

The insecticidal and antibacterial activity of new synthesized carbamate derivatives(8-Hydroxy-5-chloroquinolyl-N-methylcarbamate(I), 8-Hydroxy-5-chloroquinolyl-N-ethylcarbamate(II)) was examined using 0.2 w/v% acetone solutiolas and 50 r/ml~1000 r/m N,N'-dimethylformamide-$H_2O$(2:3) solutions of each compounds, respectively. 1) Two carbamates exerted insecticidal effects on Sogata furcifera HORVATH, Delphacodes Striatella FAUEN, Whereas no significant effects were observed on the Nilaparvate lugens STAL, Inazuma dorasails MOISCHIULSKY and Nephateffix apicalis Cincticeps UHLER. 2) These compounds exhibited growth-inhibitory activity against Staphylococcus aureus, Salmonella paratyphi A, Shigella dysenteriae 1a, Escherichia coli NL 1401,at the concentration range of 100~500 r/ml in general.