• Proceedings of the SCSK Conference
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• 2003.09b
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• pp.201-212
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• 2003

The heartwood extract of Artocarpus lakoocha Roxb., which contains a potent tyrosinase inhibitor oxyresveratrol, was evaluated for its melanin-reducing efficacy in both guinea pigs and human volunteers. After 4 week-daily application of the extract dissolved in propylene glycol to the back of guinea pigs, significant reduction in melanin content was detected, with the effect greater than 3% kojic acid and solvent propylene glycol (P < 0.05). The extract was subsequently tested in female volunteers (3 groups of 20 subjects) using a parallel clinical trial with self-control. The first group received the A. lakoocha solution in propylene glycol whereas the second and the third group respectively received 0.25% licorice extract and 3% kojic acid in the same solvent. The subject in each group twice daily applied the test solution on one arm whereas the remaining arm was applied with only propylene glycol (self-control) for 12 weeks. The A. lakoocha extract was found to be the most effective agent, giving the shortest onset of significant whitening after only 4 weeks of application (P < 0.05), followed by 3% kojic acid (8 weeks) and 0.25% licorice extract (10 weeks). The whitening effect also increased with time, with the highest extent observed with A. lakoocha at week 12. The in vitro antityrosinase activity of A. lakoocha extract decreased with time upon storage at room temperature but could be stabilized by a combination of several antioxidants. In conclusion, the heartwood extract of A. lakoocha appeared to have promising potential for use as an effective and economical skin-whitening agent.

• KSBB Journal
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• v.24 no.6
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• pp.570-578
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• 2009

In vitro biological activities such as antioxidant, whitening, anti-hangover and anticancer activities were evaluated. The antioxidant activities of astaxanthin and H. pluvialis extract were significantly higher than that of $\alpha$-tocopherol when the antioxidant activities were determined as xanthine oxidase inhibition, hydroxyl radical scavenging and DPPH radical scavenging. The whitening effect of H. pluvialis extract was about two times as kojic acid. H. pluvialis extract indicated an anticancer activity on a cervical cancer cell line. Astaxanthin showed anti-hangover effect of 1.5 times as jiguja extract. The anti-hangover effect of the inclusion complex (As-$\beta$-CD) was about 1.2 times of jiguja extract. And, the inclusion complex of Haematococcus pluvialis (H.p.-$\beta$-CD) showed almost the same whitening effect as kojic acid.

• Korean Journal of Food Science and Technology
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• v.43 no.2
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• pp.195-199
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• 2011

This study investigated the antioxidant effects and physiological activities of extract from various parts of pumpkin (Cucurbita moschata Duch.) such as leaf, flesh, skin and seed. Different dried parts of C. moschata were boiled in ethanol for three hours, evaporated, and lyophilized with a freeze-dryer. Total polyphenol contents were the highest in leaf ($29.62{\pm}0.88mg$ GAE/g DM). The same result was observed in the measurement of the flavonoid content. The leaf extract of C. moschata had stronger DPPH radical-scavenging activities and ABTS-radical scavenging activities than any other part. Leaf extract of C. moschata was found to have the highest ferric-reducing antioxidant power (FRAP) value. Meanwhile, at 0.1 mg/mL of all extracts higher degree of tyrosinase inhibitory effects than kojic acid was observed (leaf; 49.58%, flesh; 40.20%, skin; 41.30%, seed; 36.79% and kojic acid; 20.70%). The glycation inhibitory activity decreased in the order leaf>skin>flesh>seed. The ${\alpha}$-glucosidase inhibitory activity of seed extract was the highest with a value of 63.58% at the concentration of 1 mg/mL.

• YAKHAK HOEJI
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• v.45 no.2
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• pp.214-219
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• 2001

Nineteen hydrolysable tannins isolated from the Euphorbia helioscopia (Euphorbiaceae) were tested for the inhibitory effect on mushroom tyrosinase activity in vitro. Inhibitory effect of gallotannin group exhibited more potent than that of phenolcarboxylic acid and ellagitannin groups against the enzyme activity. The inhibitory activity by pentagalloyl glucose on mushroom tyrosinase was more potent ($IC_{50}$/, 4.9 $\mu$M) than that of kojic acid ($IC_{50}$/, 8.7 $\mu$M).

• Journal of dental hygiene science
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• v.4 no.2
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• pp.81-84
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• 2004

Gingival hyperpigmentation may cause esthetic problems and embarrassment. Especially in patients with a gummy smile. Melanin pigmentation is related to estiologic factor such as hormon, systemic factor, drug, smoking and gingival inflamation. During our search for new inhibitory components on melanogenesis from natural resources, MeOH extracts of more than 100 higher plants were tested for the inhibitory effect on melanogenesis in cultured B-16 mouse melanoma cell lines, and methylene chloride soluble part extract of Cnidii Rhizoma MeoH extraction was found to have potent activity. Cnidii Rhizoma, the root of Cnidium officinale Makino (Umbelliferae), is used for the treatment of abdominal pain, arthralgia, headache, hypertension, intestinal colic and for menstrual disorders and uterine cramps for its anti-blood stagnation effect. Two compounds were isolated and their chemical structures were determined as linoleic acid methyl ester(1), 1,3-dilinoleoyl-2-stearoyl glycerol(2), on the basis of physical and spectral data.

• Proceedings of the SCSK Conference
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• 2003.09a
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• pp.780-803
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• 2003

Exposure of skin cells, particularly keratinocytes to various nuclear factor-kappaB ($\textrm{NF}_{-{\kappa}}\textrm{B}$) activators [e.g. tumor necrosis factor-$\alpha$, interleukin-1, lipopolysaccharides, and ultraviolet light] leads to phosphorylation and degradation of the inhibitory protein, $\textrm{I}_{{\kappa}}\textrm{B}$. Liberated $\textrm{NF}_{-{\kappa}}\textrm{B}$ is translocated into the nucleus where it can change or alter expression of target genes, resulting in the secretion of extracellular signaling molecules including melanotrophic factors affecting melanocyte. In order to demonstrate the possible role of $\textrm{NF}_{-{\kappa}}\textrm{B}$ activation on the synthesis of melanotrophic factors from the keratinocytes, the activities of $\textrm{NF}_{-{\kappa}}\textrm{B}$ induced by melanogenic inhibitors (MIs) were determined in human HaCaT keratinocytes transfected with $\textrm{pNF}_{-{\kappa}}\textrm{B}$-SEAP-NPT plasmid. Transfectant cells released the secretory alkaline phosphatase (SEAP) as a transcription reporter in response to the $\textrm{NF}_{-{\kappa}}\textrm{B}$ activity and contain the neomycin phosphotransferase (NPT) gene for the dominant selection marker for geneticin resistance. MIs such as niacinamide, kojic acid, hydroquinone, resorcinol, arbutin, and glycolic acid were preincubated with transfectant HaCaT cells for 3 h and then ultraviolet B (UVB) was irradiated. $\textrm{NF}_{-{\kappa}}\textrm{B}$ activation was measured with the SEAP reporter gene assay using a fluorescence detection method. Of the Mis tested, kojic acid ($IC_{50}$/ = 60 $\mu$M) was found to be the most potent inhibitor of UVB-upregulating $\textrm{NF}_{-{\kappa}}\textrm{B}$ activation in transfectant HaCaT cells, which is followed by niacinamide ($IC_{50}$/= 540 $\mu$M). Pretreatment of the transfectant HaCaT cells with the Mis, especially kojic acid and niacinamide, effectively lowered $\textrm{NF}_{-{\kappa}}\textrm{B}$ binding measured by electrophoretic mobility shift assay. Furthermore, these two inhibitors remarkably reduced the secretion level of IL-6, one of melanotrophic factors, triggered by UV-radiation of the HaCaT cells. These observations suggest that Mis working at the in vivo level might act partially through the modulation of the synthesis of melanotrophic factors in keratinocyte.

• Natural Product Sciences
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• v.10 no.2
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• pp.80-84
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• 2004

Rosmarinic acid and its methyl ester, isolated from the ethyl acetate soluble fraction of the methanolic extract of Salvia miltiorrhiza Bunge (Labiatae), were found to inhibit the oxidation of L-tyrosine catalyzed by mushroom tyrosinase with the $IC_{50}$ values of 16.8 and $21.5\;{\mu}M$, respectively. It was comparable with kojic acid, a well-known tyrosinase inhibitor, with an $IC_{50}$ of $22.4\;{\mu}M$. The inhibitory kinetics analyzed by the Lineweaver-Burk plots, were found rosmarinic acid and its methyl ester to be competitive inhibitors with $K_i\;of\;2.4{\times}10^{-5}\;and\;1.5{\times}10^{-5}\;M$, respectively.

• Preventive Nutrition and Food Science
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• v.12 no.2
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• pp.119-121
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• 2007

The tyrosinase inhibition activity and mutagenicity as assessed by the Ames test on phenolic antioxidants (5-Caffeoyl quinic acid, 3,4-Dihydroxy cinnamic acid, Quercetin 3-O-${\beta}$-D-glucopyranose, Kaempferol 3-O-${\beta}$- D-glucopyranose) and the ethyl acetate fraction isolated from mulberry leaves were examined. The ethyl acetate fraction and chlorogenic acid exhibited weaker tyrosinase inhibitory activities than kojic acid. In addition, the ethyl acetate fraction from mulberry leaves, containing phenolic antioxidants, showed no mutagenicity by the Ames test.

• Journal of Microbiology and Biotechnology
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• v.34 no.7
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• pp.1452-1463
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• 2024

Fungi generate different metabolites some of which are intrinsically bioactive and could therefore serve as templates for drug development. In the current study, six endophytic fungi namely Aspergillus flavus, Aspergillus tubigenesis, Aspergillus oryzae, Penicillium oxalicum, Aspergillus niger, and Aspergillus brasiliensis were isolated and identified from the medicinal plant, Silybum marianum. These endophytic fungi were identified through intra transcribed sequence (ITS) gene sequencing. The bioactive potentials of fungal extracts were investigated using several bioassays such as antibacterial activity by well-diffusion, MIC, MBC, anti-biofilm, antioxidant, and haemolysis. The Pseudomonas aeruginosa PAO1 was used to determine the antibiofilm activity. The ethyl acetate extract of Aspergillus flavus showed strong to moderate efficacy against Staphylococcus aureus, Escherichia coli, P. aeruginosa, and Bacillus spizizenii. Aspergillus flavus and Aspergillus brasiliensis exhibited significant antibiofilm activity with IC₅₀ at 4.02 and 3.63 mg/ml, while A. flavus exhibited maximum antioxidant activity of 50.8%. Based on HPLC, LC-MS, and NMR experiments kojic acid (1) and carbamic acid (methylene-4, 1-phenylene) bis-dimethyl ester (2) were identified from A. flavus. Kojic acid exhibited DPPH free radical scavenging activity with an IC₅₀ value of 99.3 ㎍/ml and moderate activity against ovarian teratocarcinoma (CH1), colon carcinoma (SW480), and non-small cell lung cancer (A549) cell lines. These findings suggest that endophytic fungi are able to produce promising bioactive compounds which deserve further investigation.

• YAKHAK HOEJI
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• v.45 no.4
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• pp.387-396
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• 2001

The effects of ascorbic acid, thiols such as cysteine, n-acetyl-ι-cyteine, glutathione, thiourea, 2-mercaptoethanol and dithiotreithol and organic acids such as magic acid, citric acid, glycolic acid, taurine and kojic acid on polyphenol oxidate (PPO) activity were studied in order to establish if it reacts with oxidized product and/or directly inhibits the enzyme. To investigate the mechanism, the quantification of t-butylcatechol and 4-methylcatechol (phenolic compounds) as substates, their oxidized product and sulphydryl colorless additional compounds were determined by high performance liquid chromatograph (HPLC) method. Chromatographic results indicate that ascorbic acid, organic acids and lower level of cysteine reduced oxidized product of substrates back to their respective positions uf ο-diphenols. On the other hand, other thiols and high level of cysteine reacted with oxidative product of ο-diphenols and then produced sulphydryl colorless compounds. Cysteine apperars to have two types of mechanism of actions in the formation of oxidative products of substrates depending on its concentration; ascorbic acid-type and other thiols-types. The effect of ascorbic acid with thiols on polyphenol oxidase was determined by same method. Chromatographic results indicate that ascorbic acid was more reactive with oxidized product of substrates than thiols.