• Journal of Life Science
• /
• v.24 no.4
• /
• pp.377-385
• /
• 2014

This study was conducted to investigate the physicochemical characteristics and biological activities of water and 30%, 50%, 70%, 100% ethanol extracts from Artemisia Argyi H. and fermented Artemisia Argyi H. The yield was the highest in the 30% ethanol extract with Argyi H. at 29.74%. Total phenol and flavonoid contents were the highest in 70% ethanol extract with Argyi H. at 72.25 mg/g and 33.34 mg/g, respectively. The antioxidant activities of all extracts were significantly increased in a dose dependent manner. The 70% ethanol extract from Argyi H. show the highest level of DPPH, ABTS radical scavenging activity and bleaching inhibition activity in ${\beta}$-carotene linoleic acid system. Tyrosinase inhibition activity was also higher in the 70% ethanol extract, and the lowest in the 100% ethanol extract with Argyi H. at 50.01% and 11.44% at $500{\mu}g/ml$ concentration, respectively. At $250{\mu}g/ml$ concentration, the xanthin oxidase inhibition activity of water extract was more than 60%, and it was higher than the extracts. These results suggest that the 70% ethanol extract of Artemisia Argyi H. has a high rate of biological activities and can be useful to develop functional food ingredients.

• Preventive Nutrition and Food Science
• /
• v.7 no.3
• /
• pp.231-237
• /
• 2002

This study was conducted to determine biological activities, such as lipid peroxidation inhibition, cytotoxicity, sun blocker, inhibition of tyrosinase, and antioxidative effect, of ethanol extracts, and of solvent fractionated ethanol extracts obtained from grape seeds and skins. The strongest lipid oxidative inhibition of 66.9% and 67.6% was observed respectively, in the presence of 20 $\mu\textrm{g}$/$m\ell$ of both ethanol extract and water fraction of grape seeds. Overall, the ethanol extracts and their fractions of grape seeds exhibited stronger lipid oxidative inhibition than that of skin extracts. On the other hand, the ethanol extracts of grape skins showed stronger cytotoxicity than that of seeds on MCF-7, Hep3B, and A549 cancer cell lines. However, the water fraction of seed ethanol extracts showed the strongest cytotoxic effect of 76.52% and 67.01% on MCF-7 and Hep3B, respectively among their fractions. Ethanol seed extracts obtained at 3$0^{\circ}C$ had the strongest absorbance both at UVA region (350 nm) and UVB region (308 nm) and the chloroform fraction showed the strongest absorbance at W region and butanol fraction at UVA region among their tractions, respectively. In the meantime, the ethanol extracts obtained at 3$0^{\circ}C$ and butanol fraction showed the strongest tyrosinase inhibitory effect of 39.4% and 37.6%, respectively. This study shows that ethanol extracts and their fractions of grape seeds and skins could be potential good materials for functional food and cosmetic products.

• Journal of Applied Biological Chemistry
• /
• v.57 no.1
• /
• pp.41-45
• /
• 2014

In the present study, red ginseng extracts were fermented by Paecilomyces tenuipes and the protopanaxdiol-type ginsenosides in the extracts were bio-transformed to F2, Rg3, Rg5, Rk1, Rh2, and CK determined by a high-pressure liquid chromatography analysis. It indicates that P. tenuipes is a microorganism to biotransform protopanaxdiol-type ginsenosides to their less glucosidic metabolites. Other biotransformed metabolites during fermentation were also analyzed using a GC-MS and identified as 2-methyl-benzaldehyde, 4-vinyl-2-methylphenol, palmitic acid, and linoleic acid. Antiulcerogenic activity of the fermented red ginseng extract (FRGE) on gastric mucosal damage induced by 0.15 M HCl in ethanol in rats was evaluated. FRGE was shown to have a potent protective effect on gastritis with 60.5% of inhibition rate at the dose of 40 mg/kg when compared to 54.5% of the inhibition rate at the same dose for stillen, the currently used medicine for treating gastritis. Linoleic acid showed a strong inhibition on gastritis with 79.3% of inhibition rate at the dose of 40.0 mg/kg. FRGE exhibited a distinct anticancer activity including growth inhibition of the two human colon cancer cells HT29 and HCT116. HT29 cells were less susceptible to FRGE in comparison with HCT116 cells. Taken together, fungal fermentation of the red ginseng extract induced hydrolysis of some ginsenosides and FRGE exhibited potent antiulcerogenic and anticancer activities. These results refer to use FRGE as a new source for treating human diseases.

• Biomolecules & Therapeutics
• /
• v.16 no.4
• /
• pp.336-342
• /
• 2008

The resveratrol analogue piceatannol (3,5,3',4'-tetrahydroxy-trans-stilbene) is a polyphenol present in grapes and wine and reported to have anti-carcinogenic activities. To investigate the mechanism of anticarcinogenic activities of piceatannol, the effects on CYP 1 enzymes were determined in Escherichia coli membranes coexpressing recombinant human CYP1A1, CYP1A2 or CYP1B1 with human NADPH-P450 reductase. Piceatannol showed a strong inhibition of CYP1A1 and CYP1B1 in a concentration-dependent manner, and $IC_{50}$ of human CYP1A1 and CYP1B1 was 5.8 ${\mu}M$ and 16.6 ${\mu}M$, respectively. However, piceatannol did not inhibit CYP1A2 activity in the concentration of up to 100 ${\mu}M$. Piceatannol exhibited 3-fold selectivity for CYP1B1 over CYP1A1. The mode of inhibition of piceatannol was non-competitive for CYP1A1 and CYP1B1. The result that piceatannol did not inhibit CYP1B1-mediated $\alpha$-naphthoflavone ($\alpha$-NF) metabolism suggests piceatannol may act as a non-competitive inhibitor as well. In human prostate carcinoma PC-3 cells, piceatannol induces apoptosis and prevents Aktmediated signal pathway. Taken together, abilities of piceatannol to induce apoptotic cell death as well as CYP1 enzyme inhibition make this compound a useful tool for cancer chemoprevention.

• The Journal of Korean Medicine Ophthalmology and Otolaryngology and Dermatology
• /
• v.30 no.2
• /
• pp.100-111
• /
• 2017

Objectives : The purpose of this study was to research the antibiotic, antioxidant and whitening effects of Jwa Kum-Whan(JKW) and Soo Ryeon-Whan(SRW). Both Jwa Kum-Whan and Soo Ryeon-Whan are composed of Coptidis rhizoma and Evodiae fructus, but the ratios of the two species are different. JKW is composed of Coptidis rhizoma and Evodiae fructus by ratio of 6:1 and SRW's ratio is 1:1. Methods : Antibiotic activities of JKW and SRW's water extracts were studied by paper disc diffusion method. Four kinds of bacteria were applied in paper disc, and each extract was dropped, individually. The diameter of inhibition zone was measured. DPPH assay was used for studying free radical scavenging activity. DPPH is quantitatively decolorized from purple color by antioxidant material. Change of color was measured by spectrophotometer. Whitening activity was analyzed by tyrosinase inhibition assay. Tyrosinase is major enzyme for control process of making eumelanin. Optical Density was measured by spectrophotometer. Results : Candida albicans and Staphylococcus aureus's inhibition zone were made large available by Both prescriptions. Inhibition zone's diameter of JKW was preferable to SRW's. Radical scavenging activity was better at SRW, but JKW's activity was available, too. Tyrosinase inhibition activity was found out available only for JKW, not for SRW. Conclusions : JKW had antibiotic effects for Candida albicans, Staphylococcus aureus. And had antioxidant, whitening effects. SRW had antibiotic, antioxidant activities but not whitening effect.

• Biomolecules & Therapeutics
• /
• v.10 no.4
• /
• pp.240-245
• /
• 2002

Cancer metastasis represents the most important cause of cancer death and antitumor agents that may inhibit this process have been extensively pursued. Invasion and metastasis of malignantly transformed cells involve degradation of the extracellular matrix (ECM) components by matrix metalloproteinases (MMP), especially MMP-2 and -9. We previously showed that H-ras-induced invasive phenotype may involve MMP-2, rather than MMP-9, in MCF10A cells. In the present study, we investigated the chemopreventive effect of Aster, a widely used culinary vegetable in Korea. We screened twelve extracts from three Aster species (Aster scaber, Aster oharai and Aster glehni) for the inhibitory effect on MMP activities of H-ras MCF10A human breast epithelial cells. All of the extracts tested in this study efficiently inhibited the gelatinolytic activities of MMP-2 and MMP-9. A more prominent inhibition was observed in MMP-2 activity compared to MMP-9. Out of twelve extracts, eight extracts showed>90％ inhibition of MMP-2 activity in H-ras MCF10A cells while only one extract showed>90％ inhibition of MMP-9 activity. We selected three extracts (AO-3, AG-3 and AS-EA) for further studies since they exerted a marked inhibition in the ratio of MMP-2 to MMP-9. Treatment with AO-3, AG-3 and AS-EA in H-ras MCF10A cells caused a significant inhibition of invasive phenotype and migration, proving a chemopreventive potential of these extracts. Taken together, our results demonstrate that extracts of Aster effectively inhibit invasion and migration of highly malignant human breast cells, possibly via downregulation of MMP-2 and MMP-9.

• Fisheries and Aquatic Sciences
• /
• v.25 no.2
• /
• pp.49-63
• /
• 2022

Anti-cholinesterase (ChE)s are commonly prescribed as the symptomatic treatment of Alzheimer's disease. They are applied to prevent the breakdown of neurotransmitter acetylcholine (ACh) that bind to muscarinic and nicotinic receptors in the synaptic cleft. Seaweeds are one of the richest sources of bioactive compounds for both nutraceuticals and pharmacognosy applications. This study aimed to determine the anti-ChEs activity of Gracilaria manilaensis, one of the red seaweeds notables for its economic importance as food and raw materials for agar production. Methanol extracts (GMM) of G. manilaensis were prepared through maceration, and further purified with column chromatography into a semi-pure fraction. Ellman assay was carried out to determine the anti-acetylcholinesterase (AChE) and anti-butyrylcholinesterase (BuChE) activities of extracts and fractions. Lineweaver-Burk plot analysis was carried out to determine the inhibition kinetic of potent extract and fraction. Major compound(s) from the most potent fraction was determined by liquid chromatography-mass spectrometry (LCMS). GMM and fraction G (GMMG) showed significant inhibitory activity AChE with EC₅₀ of 2.6 mg/mL and 2.3 mg/mL respectively. GMM and GMMG exhibit mixed-inhibition and uncompetitive inhibition respectively against AChE. GMMG possesses neuroprotective compounds such as cynerine A, graveolinine, militarinone A, eplerenone and curumenol. These findings showed a promising insight of G. manilaensis to be served as a nutraceutical for neuronal health care in the future.

• BMB Reports
• /
• v.28 no.3
• /
• pp.227-231
• /
• 1995

In order to figure out the relationships between structural features and biological activity of the host-specific HC-toxin in maize, structurally related cyclic tetrapeptides, chlamydocin and CYL-2 were isolated, and their biological activities in maize were examined. Biological activities of preparations were determined by root growth inhibition and electrolyte leakage bioassays. Chlamydocin and CYL-2 showed toxicities to maize. However, the toxicities of these compounds were non-specific. Thus, the precise peptide ring structure of HC-toxin apparently does not play an important role in toxicity, while resistance of maize to HC-toxin is based on a precise ring conformation.

• Applied Biological Chemistry
• /
• v.47 no.4
• /
• pp.414-421
• /
• 2004

3D QSAR studies for protox inhibition activities against root and shoot of the rice plant (Orysa sativa L.) and barnyardgrass (Echinochloa crus-galli) by a series of new 1-(5-methyl-3-phenylisoxazolin-5-yl)methoxy-2-chloro-4-fluorobenzene derivatives were conducted based on the results (Sung, N. D. et al.'s, (2004) J. Korean Soc. Appl. Biol. Chem. 47(3), 351-356) using comparative molecular similarity indices analysis (CoMSIA) methodology. Four CoMSIA models, without hydrogen bond donor field for the protox inhibition activities against root and shoot of the two plants, were derived from the combination of several fields using steric field, hydrophobic field, hydrogen bond acceptor field, LUMO molecular orbital field, dipole moment (DM) and molar refractivity (MR) as additional descriptors. The predictabilities and fitness of CoMSIA models for protox inhibition activities against barnyard-grass were higher than that of rice plant. The statistical results of these models showed the best predictability of the protox inhibition activities against barnyard-grass based on the cross-validated value $r^2\;_{cv}\;(q^2=0.635{\sim}0.924)$, non cross-validated, conventional coefficient $r^2\;_{ncv.}$ value $(r^2=0.928{\sim}0.977)$ and PRESS value $(0.255{\sim}0.273)$. The protox inhibition activities exhibited a strong correlation with the steric $(5.4{\sim}15.7%)$ and hydrophobic $(68.0{\sim}84.3%)$ factors of the molecules. Particularly, the CoMSIA models indicated that the groups of increasing steric bulk at ortho-position on the C-phenyl ring will enhance the protox inhibition activities against barnyard-grass and subsequently increase the selectivity.

• Biomedical Science Letters
• /
• v.23 no.3
• /
• pp.230-237
• /
• 2017

Changes in the activity of alkaline phosphatase (ALP) isoenzymes and isoforms in human serum have a major diagnostic value, therefore the regulation of ALP activities is a valuable target for therapeutic interventions. To assess the pharmacological activity of retinoids, i.e., all-trans retinoic acid and 13-cis retinoic acid, their tissue-specific inhibitory effect on human serum ALP activity was elucidated by chemical inhibition methods, heat-sensitive inactivation, and wheat-germ lectin precipitation test. Retinoids showed significant inhibition of the total ALP activity in human serum at a concentration of 5 mM. All-trans retinoic acid (5 mM) and 13-cis retinoic acid (5 mM) inhibited ALP activities by up to 12% and 15%, respectively, compared to that by guanidine hydrochloride (200 mM). L-phenylalanine (100 mM) and urea (30 mM) had no further inhibitory effect on ALP activities in human serum pretreated with retinoids (5 mM). Retinoids significantly inhibited ALP activities by up to 20% compared with that of tetramisole (30 mM). The ALP activities in retinoid-pretreated serum remained unchanged after the heat inactivation process. These results suggest that retinoids are inhibitors of the intestinal ALP isoenzyme. Remarkably, retinoids revealed potent inhibitory activities against ALP in wheat-germ lectin precipitant serum, indicating that they also function as inhibitors of the bone ALP isoform. The results show that retinoids inhibit the specific tissue-derived human serum ALP activities, moreover, the inhibitory effect of retinoids against bone ALP activity suggests their clinical utility as monitoring and prevention of metastasis of bone cancer.