• Journal of Microbiology and Biotechnology
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• 제10권3호
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• pp.394-398
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• 2000

A methanol extract of the root of Peucedanum japonicum, used as a medicinal herb, showed an inhibitory effect on mammalian topoisomerase I activity. The methanol extract was suspended in ethyl acetate, and a topoisomerase I inhibitor in the organic soluble fraction was then isolated by silica gel and thin layer chromatography. The topoisomerase I inhibitory compound was indentified as falcarindiol based on the analysis of EI-MS, $^1$H and \ulcornerC NMR spectroscopy. This inhibitory showed cytotoxicity against human leukemia Jurkat T and HL60 cells with an IC\ulcorner value of 7 $\mu\textrm{g}$/ml. These results suggest the possibility of falcarindiol as a new anticancer agent which can be expected to have a synergistic effect on other anticancer drugs. In addition, the present data show that falcarindiol has antifungal, yet not antibacterial, activity.

• Natural Product Sciences
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• 제18권2호
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• pp.102-105
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• 2012

Marine organism extracts were prepared from 26 species of Korean indigenous marine organisms, including 25 species belonging in class Anthozoa of phylum Cnidaria and a species belonging to subphylum Urochordata of phylum Chordata, and screened their inhibitory effects against ${\mu}$-calpain. As a result, the thirteen extracts were found to be active in the criteria of $IC_{50}$ < 100 ${\mu}g/ml$. Among them, the MeOH extracts of Plexauroides praelonga and Alveopora japonica showed remarkable ${\mu}$-calpain inhibitory activity with $IC_{50}$ values of $4.62{\pm}0.22$ and $4.82{\pm}0.07{\mu}g/ml$, respectively. In addition, chemical investigation of A. japonica led to the isolation of an active compound, hexadecyl tetradecanoate, as a selective cathepsin B inhibitor ($IC_{50}=9.05{\pm}2.45{\mu}M$). This compound was isolated as constituent of A. japonica for the first time in the present study.

• 한국식품조리과학회지
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• 제28권6호
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• pp.773-779
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• 2012

This study was conducted to investigate the physiological activities of saccharified cherry tomato gruel containing different levels(0, 15, 30, and 45%) of cherry tomato puree. The total phenolic compound and flavonoids contents of saccharified cherry tomato gruel with cherry tomato puree were 1.73-5.09 mg/g and 0.28-7.01 mg/g, respectively. DPPH radical scavenging activities of saccharified cherry tomato gruel with cherry tomato puree were 8.67-92.58%, respectively. The ABTS radical scavenging activities of saccharified cherry tomato gruel with cherry tomato puree ranged from 6.02 to 61.59%. The ACE inhibitory activity of cherry tomato rice gruel increased with cherry tomato puree showed a range of 38.85-62.15%, respectively. With increasing additions of cherry tomato puree, the total phenolic compound and flavonoid contents, DPPH and ABTS radical scavenging activities and, ACE inhibitory activities were increased significantly (p<0.05). In conclusion, saccharified cherry tomato gruel could be used as a gruel processing method to in order to increase the functional values of gruels.

• 약학회지
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• 제41권5호
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• pp.547-553
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• 1997

The purpose of this investigation was to determine the inhibition on $Na^+,\;K^+$-ATPase, cyclic AMP phosphodiesterase and platelet activation by marine sterols isolated from octocorals. Three marine polyhydroxysterols, 7${\alpha},\;8{\alpha}-epoxy-3b{\beta},\;5{\alpha},\;6{\alpha}-trihydroxycholestane (1),\;24-methyl-7{\alpha},\;8{\alpha}-epoxy-3{\beta},\;5{\alpha},\;6{\alpha}-trihydroxycholest-22-ene (2),\;and\;7{\alpha},\;8{\alpha}-epoxy-3{\beta},\;5{\alpha},\;6{\alpha}-trihydroxycholest-22-ene (3)$, were isolated from the Gorgonian Acabaria undulata. Five marine sterols(compound 4, 5, 6, 7, 8) were isolated from the soft coral Alcyonium gracillimum. Three marine polyhydroxysterols (1, 2, 3) and pregna-1. 20-diene-3-one (8) exhibit a potent inhibitory effect on rabbit platelet aggregation induced by collagen and thrombin. Those polyhydroxysterols also exhibit a potent inhibitory effect on cyclic AMP phosphodiesterase. Compound 6 with an unusual cyclic enolether exhibit a inhibitory effect on $Na^+,\;K^+$-ATPase.

• Natural Product Sciences
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• 제25권1호
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• pp.76-80
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• 2019

Bioactivity-guided fractionation of MeOH extract of the dried fruits of Amomum tsao-ko led to isolation of nine compounds (1 - 9). Their structures were elucidated by spectroscopic methods including extensive 1D and 2D-NMR, as alpinetin (1), naringenin-5-O-methyl ether (2), naringenin (3), hesperetin (4), 2',4',6'-trihydroxy-4-methoxy chalcone (5), tsaokoin (6), boesenbergin B (7), 4-hydroxyboesenbergin B (8), and tsaokoarylone (9). Of these, compound 8 was isolated from a natural source for the first time, which was previously reported as a synthetic product. The isolated compounds (1 - 9) were tested for their inhibitory effects on LPS-induced nitric oxide production in RAW 264.7 macrophages. Among them, three chalcone derivatives (compounds 5, 7, and 8) and a diarylheptanoid (compound 9) exhibited significant inhibitory activity on the NO production with $IC_{50}$ values ranging from 10.9 to $22.5{\mu}M$.

• Journal of Applied Biological Chemistry
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• 제62권1호
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• pp.81-86
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• 2019

A yellow resin (gamboge) from Garcinia hanburyi has been widely used as folk medicine due to its antibacterial and antitumor activities. We isolated four ${\alpha}$-glucosidase inhibitory compounds from the methanol extract of gamboge. The compounds (1-4) were identified as gambogoic acid (1), moreollic acid (2), gambogic acid (3), and 10-methoxygambogenic acid (4), respectively through spectroscopic data including 2D-NMR and HREIMS. All compounds were examined in the enzyme inhibition assay against ${\alpha}$-glucosidase to identify their inhibitory potencies and kinetic behavior. All compounds (1-4) showed enzyme inhibition against ${\alpha}$-glucosidase, but the activity was significantly affected by the methoxy group on C-10 of ring A and pentenyl pyran moiety of ring D. For example, compound 1 ($IC_{50}=41.4{\mu}M$) bearing pyran ring eight times effective that 4 ($IC_{50}=350.6{\mu}M$) having geranyl group itself. Most active compound was found out to be gambogoic acid (1) which was analyzed most abundant metabolite in gamboge by LC-ESI-MS/MS. In kinetic study, compounds 1 and 2 were proved as noncompetitive inhibitors.

• 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.

• 한국양봉학회지
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• 제34권2호
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• pp.131-136
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• 2019

Recently, number of honeybees (Apis mellifera) has visibly decreased because they are vulnerable to some diseases like American foulbrood disease. American foulbrood disease, which is caused by Paenibacillus larvae, is emerged as great cause of decrease in number of honeybees. After antibiotic-resistant strain emerged, it is now more difficult to treat those pathogens successfully. Researches on finding alternative antibacterial compound are ongoing. In this study, we examined the antibacterial effect of honokiol on P. larvae. Honokiol showed great antibacterial effect with minimum inhibitory concentration of 12.5 ㎍/mL and minimum bactericidal concentration of 50 ㎍/mL. An agar diffusion test also confirmed the anti-Paenibacillus larvae activity of honokiol with an inhibitory zone of 9±0.5 mm. Since honokiol is known to interact membrane of some bacteria, we measured 260 nm absorbing particles, which could be induced by leakage of cells, and confirmed that the leakage of P. larvae occurred in dose-dependent manners. However, result of crystal violet assay suggested that honokiol has only mild anti-biofilm formation effect on P. larvae, which means honokiol controls the bacteria by inducing the bursting of membrane. Finally, an additive effect of honokiol with tetracycline and terramycin was found using a checkerboard assay with a fractional inhibitory concentration index value of 0.5.

• Archives of Pharmacal Research
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• 제28권5호
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• pp.541-545
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• 2005

Flowers of Erigeron annuus L. were extracted with 80% aqueous MeOH, and the concentrated extract was partitioned with EtOAc, n-BuOH, and H$_2$O. Repeated silica gel and OD S column chromatography of the EtOAc fraction led to the isolation of a sterol, through activityguided fractionation, using ACAT inhibitory activity measurements. From the physico-chemical data, including NMR, MS, and IR, the chemical structure of the compound was determined to be an ergosterol peroxide (1), which has been isolated for the first time from this plant. This compound exhibited hACAT-1 and Lp-PLA$_2$ inhibitory effects, with inhibitory values of 51.6 ${\pm}$ 0.9 and 51 .7 ${\pm}$ 1.2%, at a treatment concentration of 0.23 mM.

• Bulletin of the Korean Chemical Society
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• 제23권10호
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• pp.1373-1374
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• 2002