• Applied Biological Chemistry
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• v.43 no.2
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• pp.95-99
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• 2000

A series of hetero ring (X) substitued chalcone derivatives with farnesyl protein transferase (FPTase) inhibition activities $(pI_{50})$ values determined in vitro is analyzed by modified Free-Wilson (F-W) and Hansch method for quantitative structure activity relationship (QSARs). On the basis of F-W analysis on the FPTase inhibitory activity of a training set of the compounds, none of the (X)-substituents were not contribute the activity. But the net charge of ${\alpha}$ carbon atom is contribute the activity than that of ${\beta}$ carbon atom. And the relative orders of the (Y)-substituents on the activity are ortho>meta>para-substituents. According to Hansch approach, the activities would depend largely on the optimal, $(R_{opt.}=-0.35)$ resonance effect with ortho substituted $(I_o>0)$ electron donating group (R<0) and STERIMOL parameter, $B_1$ constant. The inhibition activity between hetro ring substituents have been a proportioned with each others and none substituent(H), 45 showed the highest FPTase inhibition $(pI_{50}=4.30)$ activity.

• Journal of Life Science
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• v.32 no.3
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• pp.222-231
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• 2022

This study aimed to confirm the possibility of being used as a cosmetic material material through the verification of the whitening and anti-inflammatory activities of an ethyl acetate fraction from Glechoma hederacea var. longituba (GHEA). The observed electron donating and ABTS⁺ radical scavenging abilities of GHEA were 89.6% and 88.7%, respectively, at 1,000 ㎍/ml concentration, with a tyrosinase inhibitory effect of 22.3% at the same concentration. For cell viability, a rate of 80% or more was observed in all concentrations that treated GHEA on melanoma and macrophage cells. Protein and mRNA expression inhibition was measured by Western blot and RT-PCR for 25, 50, and 100 ㎍/ ml concentrations, and it was confirmed that expression decreases in a concentration-dependent manner as GHEA concentration increases. The inhibition of the whitening-related factors MITF and TRP-2 were superior following GHEA treatment than those of the control group treated with kojic acid of 100 ㎍/ml concentration. For tyrosinase, the lowest mRNA expression rate was 29.1% at 100 ㎍/ml which confirmed excellent inhibition. In analyzing the effects of pro-inflammatory cytokines IL-1β, IL-6, and TNF-α on protein and mRNA expression, IL-6 and TNF-α showed high protein and mRNA inhibition compared to a vitamin C control group. Based on these experimental results, GHEA could be applied as a natural cosmetic material.

• Journal of the East Asian Society of Dietary Life
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• v.18 no.4
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• pp.633-640
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• 2008

In this study, the effects of feeding citrus byproducts on various qualities of pork during cold storage were investigated, such as water holding capacity, drip loss, meat color, storage stability, rancidity, and antioxidant activity. Pork samples (195 days old, $115{\pm}3\;kg$, female) used for the experiment was divided into three groups: T0(pigs not fed citrus byproducts), T1(pigs fed 3% and 5% citrus byproducts during growth and the finishing period, respectively), and T2(pigs fed 6% and 10% citrus byproducts). The loin used for the experiment was obtained from 5 pigs of each group, vacuum packaged, and then stored at $3^{\circ}C$ for 4 weeks. There was no difference among T0, T1, and T2 for pH, water holding capacity, or drip loss. As for the meat color of the loin, T1 and T2 showed higher redness($a^*$ value) during early chilling but showed higher yellowness($b^*$ value) during late chilling. T1 and T2 showed higher electron donating ability and lower volatile basic nitrogen, total plate count, and TBA values than T0, regardless of the chilling period. Thus, feeding citrus byproducts improves the storage stability of chilled pork in terms of rancidity and antioxidant activity.

• Journal of the Korean Chemical Society
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• v.29 no.4
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• pp.426-436
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• 1985

Preparative and kinetic photochemical reactions of several benzanilides were studied. Several substituted benzanilides were synthesized by acylation of substituted anilines with substituted benzoyl chlorides. While benzanilide gave a photo-Fries type reaction product, 2-chlorobenzaniline, 2-bromobenzanilide, and 2-methoxybenzanilide gave a photocyclization reaction product, phenanthridone. Since 8-chlorophenanthridone was obtained from 2,2'-dichlorobenzanilide, the carbonyl phenyl is the excited site. Quantum yield of photocyclization of 2-chlorobenzanilide, 2'-chlorobenzanilide, and 2-methoxybenzanilide were obtained. 2-Chlorobenzanilide was photocyclized effectively and 2'-chlorobenzanilide ineffectively. Since the oxygen present in the reaction medium retarded the photocyclization reaction of 2-chlorobenzanilide, the triplet state of 2-chlorobenzanilide is involved. The mechanism of the photocyclization of 2-chlorobenzanilide is suggested: $\pi-complex$ between carbonyl phenyl and N-phenyl was formed from the triplet state of 2-chlorobenzanilide; neighbour phenyl (N-phenyl) assists for leaving of chlorine from carbonyl phenyl to make an intermediate, cyclized conjugated radical, because electron donating group on the N-phenyl ring accelerated the reaction; hydrogen detachment from the intermediate is obviously not a rate determined step because there was no isotope effect on the rate of photocyclization. The photocyclization reaction rate of 2-methoxybenzanilide was faster in the presence of oxygen than in the absence of oxygen. Thus, the singlet excited state of 2-methoxybenzanilide is involved in the reaction. Probably, the intermediate, methoxyhydro-phenanthridone is oxidized by oxygen in the medium to give phenanthridone.

• Journal of the Korean Society of Food Science and Nutrition
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• v.32 no.5
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• pp.723-727
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• 2003

The antioxidant activities and their antioxidant compounds of a group of teas obtained in local markets were investigated. A total of 18 teas were tested for their antioxidant activities based on their ability to scavenge ABTS (2,2'-Azino-bis-3-ethylbenzothiazoline-6-sulfonic acid) cation radical and DPPH (1,1-diphenyl-2-picrylhydrazyl) free radical. The former was expressed as mg of ascorbic acid equivalents per 1 tea bag (L-ascorbic acid equivalent antioxidant capacity, AEAC) and the latter was expressed as percentage of electron donating activity (EDA%). A good correlation of AEAC and EDA was observed between the two methods. The concentrations of total polyphenolics and flavonoids in tea extracts were measured by spectrophotometric methods. Total ascorbic acid was determined via the 2,6-dicholoroindophenol titrimetric method. According to the AEAC value and EDA, black tea, brown rice green tea, green tea, herb tea and malva tea showed relatively high antioxidant activities. Polyphenolic compounds were the major naturally occurring antioxidant compounds found in teas and the high concentrations of polyphenolic compounds were observed in black tea, green tea and herb tea. Overall, six teas out of 18 teas tested in the study showed better antioxidant activities and higher amounts of total polyphenolic compounds.

• The Korean Journal of Pesticide Science
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• v.6 no.4
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• pp.279-286
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• 2002

To improve the growth inhibition activities and selectivities for quinclorac family, novel 3-substituted phenyl-5-(3,7-dichloro-8-quinolinyl)-1,2,4-oxadiazole derivatives as the substrate were synthesized and their the activities ($pI_{50}$) against shoot and root of rice plant (Oryza sativa L.) and barn-yard grass (Echinochloa crus-galli) were measured. And the quantitative structure-activity relationships (QSARs) between physicochemical parameters of the substitutents (R) on phenyl group and the activities ($pI_{50}$) were analyzed quantitatively. According to the SAR analyses, the substrates of planar conformation showed higher herbicidal activities against barnyard grass than rice plant. The activities against rice plant depend on the electronic effect (shoots: ${\sigma}_{opt.}=0.49$ & root: $R_{opt.}=-0.15$) of substituents, whereas the activities against shoots and roots of barnyard grass depend on hydrophobicity (${\pi}_{opt.}=0.37{\sim}2.40$). There were conditions of selective growth inhibition activity against barnyard grass when such a ortho-substituted electron donating substituents showing the hydrophobicity value, ${\pi}=2.40$ were introduced on the phenyl ring. The 2-tolyl substituent predicted from SAR equations was expected to have better growth inhibition activity and selectivity (${\Delta}pI_{50}=1.26$) for barnyard grass.

• Journal of Life Science
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• v.23 no.3
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• pp.377-382
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• 2013

In this study, we evaluated the antioxidant effects of Cordyceps, Ganoderma lucidum (Curtis) P. Karst and Phellinus linteus complexes. Three mushrooms were extracted using 70% ethanol, respectively, in ratios of 80:10:10(?). The electron-donating ability was measured using the DPPH radical mushroom complexes and showed effects of 66% in 500 ${\mu}g/ml$. ABTS radical cation decolorization measured 73% in 50 ${\mu}g/ml$ and had an effect similar to BHA in 500 ${\mu}g/ml$. In their superoxide anion radical scavenging ability, the mushroom complexes showed an effect of 41% in 10 ${\mu}g/ml$. The effect on the control of BHA was more than three times as high as BHA in 50 ${\mu}g/ml$ and 100 ${\mu}g/ml$ concentration. The results showed that lipid oxidation is an excellent inhibitor of lipid oxidation $Cu^{2+}$, compared to the $Fe^{2+}$ group. The results of superoxide dismutase (SOD) activity in the mushroom complexes showed a low effect of 13% in 500 ${\mu}g/ml$. Thus, the results of this study showed that the antioxidant effect of the mushroom complexes was excellent, indicating their potential as an antioxidant material.

• The Korean Journal of Pesticide Science
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• v.7 no.2
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• pp.100-107
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• 2003

To improve the growth inhibitory activity against the shoot and root of rice plant (Oryza sativa L) and barnyard grass (Echinochloa crus-galli), a series of N-substituted phenyl-3,4-dimethylmaleimdes derivatives as substrates were synthesized and then their the inhibitory activities of protoporphyrinogen oxidase (1.3.3.4), protox were measured. The quantitative structure-activity relationships (QSAR) between structures and the inhibitory activities were studied quantitatively using the 2D-QSAR method. And also, molecular sharp similarity between the substrate derivatives and protogen, substrare of protox enzyme were studied. The activities of the two plants indicated that barnyard grass had a higher activity than the rice plant and their correlation relationships have shown in proportion for each. Accordingly, the results of SARs suggest that the electron donating groups as $R_2=Sub.X$ group will bind to phenyl ring because the bigger surface area of negative charged atoms in the substrate molecule derivatives may increase to the higher the activity against barnyard grass. Based on the molecular shape similarity, when the derivatives and protogen, subsbrate of protox enzyme were superimposed by atom fitting, the similarity indices (S) were above 0.8 level but the correlation coefficients (r) between S values and the activities showed not good.

• Korean Journal of Clinical Laboratory Science
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• v.53 no.4
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• pp.363-370
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• 2021

This study was conducted to evaluate the dermal cytotoxicity of lead acetate (LA) and other heavy metal compounds, and the protective effect of Lespedeza bicolor (LB) extract on LA-induced cytotoxicity in cultured B16-/F10 melanoma cells. The study evaluated the antioxidative effects of LB due to its electron-donating ability (EDA), inhibitory effects on melanization and improving cell viability. LA significantly decreased cell viability in a dose-dependent manner, and the XTT₅₀ value was determined at 52.7 µM in the studied cultures. Based on the Borenfreund and Puerner's toxicity criteria, LA was estimated to be highly cytotoxic. LA-induced cytotoxicity and cell damage was reversed by the antioxidant activity of kaempferol (KAE), thereby remarkably improving cell viability. A study of the protective effects of the LB extract on LA-induced cytotoxicity showed that the LB extract remarkably increased cell viability in the LA-treated group, and also inhibited the EDA and the total amount of melanin. The above results suggest oxidative stress-mediated cytotoxicity of LA. In the study, LB extract effectively prevented LA-induced cytotoxicity via its antioxidative activity and inhibition of melanization. In conclusion, natural resources like LB extracts may be useful agents for the prevention of oxidative stress-mediated cytotoxicity and melanization by heavy metallic compounds such as LA.

• Journal of Life Science
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• v.32 no.9
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• pp.667-677
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• 2022

Dolsan mustard seeds (DMS) were added in whole, crushed, and roasted form at 0.5 g (S-1), 1.0 g (S-2), and 1.5 g (S-3), respectively to broth and heated for 10 or 15 min. After cooling, the quality characteristics were measured. Salinity and pH decreased with boiling time. The antioxidant activities of the experimental broth were measured in terms of total polyphenol content, total flavonoid content, electron donating ability (EDA), 2,2-azino-bis (3-ethyl-benzothizoline-6-sulfonic acid) (ABTS) radical scavenging activity, and ferric reducing antioxidant power (FRAP). The overall, antioxidant activity was higher in broths containing 1.0 g and 1.5 g DMS than in those containing 0.5 g DMS and the activity increased with increasing boiling time. Sinigrin was not detected in the control group, and no significant difference in sinigrin content was noted among broths containing different concentrations of DMS. A high glutamic acid content was detected in the control broth, whereas glutamic acid, aspartic acid, glycine, proline, alanine, and arginine were detected in the broths containing DMS. The free amino acid contents, particularly aspartic acid and glutamic acid contents, were high in umami. Volatile components, such as 2-propenyl-isothiocyanate (ITC), allylthiocyanate, n-butyl ITC, and 3-butenyl ITC, were detected in the DMS-containing broths. Sensory evaluation revealed that a higher amount of DMS added and a longer heating time increased the overall taste preference, and the difference was statistically significant. The purpose of this study was to present basic data on the quality characteristics of DMS-added broths to aid in the development of new products using DMS.