• Title/Summary/Keyword: Bioactive agents

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Development of Natural Antioxidants and Whitening Agents for Cosmeceuticals

  • Kim, Jong-Pyung
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 2007.11a
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    • pp.79-92
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    • 2007
  • Oxidative stress have known to be a risk factor for the degenerative processes and closely related to a lot of diseases. It is well established that antioxidants are good in protection and therapeutic means against oxidative damage. There is increasing interest in natural antioxidants and many natural antioxidants have been found and utilized as the possible protection for various diseases and skin aging. We have screened natural antioxidant agents for cosmeceuticals, nutraceuticals, and drugs as therapeutic and preventive means against oxidative stress, and have developed a number of novel antioxidants from various natural sources. A novel melanin synthesis inhibitor, Melanocin A, isolated from the metabolite of a fungal strain Eupenicillium shearii F80695 inhibited mushroom tyrosinase and melanin biosynthesis of B16 melanoma cells with $IC_{50}$ value of 9.0 nM and MIC value of $0.9\;{\mu}M$, respectively. Melanocin A also exhibited potent antioxidant activity by scavenging of DPPH and superoxide anion radicals. UV was found to increase the level of hydrogen peroxides and other reactive oxygen species (ROS) in skin tissues. This increase in ROS may not only alter the structure and function of many genes and proteins directly but may also modulate their expressions through signal transduction pathways and, ultimately, lead to skin damage. We investigated the effect of Melanocin A on UV-induced premature skin aging. Firstly, the effect of Melanocin A on UV-induced matrix metalloproteinase (MMP)-9 expression in an immortalized human keratinocyte cell line, HaCaT in vitro was investigated. Acute UV irradiation induced MMP-9 expression at both the mRNA and protein levels and Melanocin A suppressed this expression in a dose-dependent manner. We then investigated UV-induced skin changes in hairless mice in vivo by Melanocin A. Chronic exposure of hairless mouse dorsal skin to UV increased skin thickness and induced wrinkle formation and the gelatinase activities of MMP-2 and MMP-9. Moreover, Melanocin A significantly suppressed UV-induced morphologic skin changes and MMP-2 and MMP-9 expression. These results show that Melanocin A can prevent the harmful effects of UV that lead to skin aging. Therefore, we suggest that Melanocin A should be viewed as a potential therapeutic agent for preventing and/or treating premature skin aging. Terrein is a bioactive fungal metabolite isolated from Penicillium species. Terrein has a relatively simple structure and can be easily synthesized. However, the biologic effects of terrein are comparatively unknown. We found for the first time that terrein potently inhibit melanin production in melanocytes and has a strong hypopigmentary effect in a spontaneously immortalized mouse melanocyte cell line, Mel-Ab. Treatment of Mel-Ab cells with terrein (10-100 mM) for 4 days significantly reduced melanin levels in a dose-dependent manner. In addition, terrein at the same concentration also reduced tyrosinase activity. We then investigated whether terrein influences the extracellular signal-regulated protein kinase (ERK) pathway and the expression of microphthalmia-associated transcription factor (MITF), which is required for tyrosinase expression. Terrein was found to induce sustained ERK activation and MITF down-regulation, and luciferase assays showed that terrein inhibits MITF promoter activity in a dose-dependent manner. To elucidate the correlation between ERK pathway activation and a decreased MITF transcriptional level, PD98059, a specific inhibitor of the ERK pathway, was applied before terrain treatment and found to abrogate the terrein-induced MITF attenuation. Terrein also reduced the tyrosinase protein level for at least 72 h. These results suggest that terrain reduces melanin synthesis by reducing tyrosinase production via ERK activation, and that this is followed by MITF down-regulation.

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Antioxidant Activity of Native Korean Halophyte Extracts and Their Anti-biofilmActivity against Acinetobacter baumannii (한국 자생 염생식물 추출물의 항산화 활성 및 다재내성 Acinetobacter baumannii에 대한 항생물막 활성)

  • Eun Seong Lee;Jeong Woo Park;Ki Hwan Moon;Youngwan Seo
    • Journal of Life Science
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    • v.33 no.12
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    • pp.1015-1024
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    • 2023
  • Antibiotics have greatly contributed to the treatment and prevention of bacterial diseases in humans, animals, and fish. However, antibiotic misuse has led to the emergence and spread of multidrug-resistant bacteria. In addition to antibiotic discovery research, efforts are being made to combat such multidrug-resistant bacteria using antimicrobial agents, antioxidants, host immune enhancement, probiotics, and bacteriophages, as well as various symptomatic therapies. To discover novel bioactive compounds, it is crucial to adopt approaches that incorporate fresh ideas, new targets, innovative techniques, and untapped resources. Halophytes are plants that grow in high-salt soils and are known to adapt to salt-induced stress through unique metabolic processes that produce secondary metabolites. This study aimed to investigate the effects of extracts of halophytes native to Korea on oxidative stress and to determine whether they exert inhibitory activity against biofilms, which are major pathogenic factors of infectious bacteria. The Acinetobacter baumannii strain ATCC 17978, a representative drug-resistant bacterium, was used to measure anti-biofilm activity. The results showed that Aster spathulifolius, Carex kobomugi, Rosa rugosa, and Asparagus cochinchiensis exerted strong antioxidant and anti-biofilm effects without affecting bacterial growth itself. The halophytes used in this study are promising candidates for the development of pharmaceutical agents with antioxidant and antimicrobial properties.

Effects of water and ethanol extracts from Ojeok-san on inflammation and its related diseases (오적산의 추출 용매 차이에 따른 염증 및 염증 관련 질환에 대한 효능 비교)

  • Yoo, Sae-Rom;Jeong, Soo-Jin;Kim, Ye-Ji;Lim, Hye-Sun;Jin, Seong-Eun;Jeon, Woo-Young;Shin, In-Sik;Shin, Na-Ra;Kim, Seong-Sil;Kim, Jung-Hoon;Ha, Hye-Kyung;Lee, Mee-Young;Kim, Ohn-Soon;Seo, Chang-Seob;Shin, Hyeun-Kyoo
    • The Journal of Internal Korean Medicine
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    • v.33 no.4
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    • pp.418-428
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    • 2012
  • Objectives : Ojeok-san, a traditional herbal formula, has been used for the treatment of cold illness and its related symptoms such as headache, nausea and indigestion. This study was performed to compare effects of water (OJSW) and 70% ethanol extracts (OJSE) of Ojeok-san on inflammation and its related diseases atopy, asthma and obesity in vitro. Methods : We performed HPLC to investigate contents of index components of OJSW and OJSE. We investigated the effects of OJSW and OJSE with an in vitro model, using 5 cell lines, specifically RAW 264. 7, HaCaT, MC/9, BEAS-2B and 3T3-L1. Results : HPLC analysis displayed that the contents of index components were higher in OJSE than OJSW. In lipopolysaccharide (LPS)-treated RAW 264.7 macrophages, OJSE significantly inhibited productions of interleukin (IL)-6, nitrite and prostaglandin $E_2$ ($PEG_2$). In TNF-${\alpha}$/IFN-${\gamma}$-treated HaCaT keratinocytes, OJSE significantly lowered levels of macrophage-derived chemokine (MDC) as well as regulated and normal T cell expressed and secreted (RANTES). OJSE also had a protective effect on inflammatory response by decreasing RANTES secretion in TNF-${\alpha}$-stimulated BEAS-2B cells. Conclusions : We conclude that OJSE could be more appropriate to enhance the biological activities against inflammation and its related diseases, and could be applied as a bioactive material for developing the potent anti-inflammatory agents.

Assessment of Validation Method for Bioactive Contents of Fermented Soybean Extracts by Bioconversion and Their Antioxidant Activities (생물전환된 품종별 대두 발효물의 주요 지표성분 함량 및 분석법 검증과 항산화 활성 평가)

  • Jung, Tae-Dong;Shin, Gi-Hae;Kim, Jae-Min;Oh, Ji-Won;Choi, Sun-Il;Lee, Jin-Ha;Lee, Sang Jong;Heo, In Young;Park, Seon Ju;Kim, Hyun Tae;Kang, Beom Kyu;Lee, Ok-Hwan
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.45 no.5
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    • pp.680-689
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    • 2016
  • The present study evaluated the validation method for isoflavone contents of fermented soybean extracts by bioconversion as well as their antioxidant activities. Our results show that the total isoflavone contents of non-fermented and fermented soybean extract ranged between 119.8 to $637.7{\mu}g/g$ and between 567.3 to $2,074.6{\mu}g/g$, respectively. Moreover, fermented soybean extracts had higher contents of isoflavone aglycones, including daidzein, glycitein, and genistein than non-fermented soybean extracts as well as lower contents of isoflavone glucosides such as daidzin, glycitin, and genistin. FRAP and ORAC values ranged between 0.15 to 0.22 and between 195.24 to $753.79{\mu}M$ Trolox equivalents/g in non-fermented and fermented soybean extracts, respectively. These results indicate that fermented soybean extracts had higher total isoflavone contents and antioxidant activities than non-fermented soybean extracts. Bioconversion process in this study may have the potential to produce isoflavone-enriched natural antioxidant agents with high added value from soybean matrices.

In vitro Effect of Ecklonia stolonifera Okamura Extract on the Cell Growth in CCD-986sk Human Fibroblast and Melanin Formation Inhibition in Clone M-3 Mouse Melanocyte Cell Line (청정해역 곰피추출물의 세포생리활성 연구)

  • Whang, Eun-Kyoung;Cho, Myung-Hwan;Park, Chan-Sun;Kim, Myung-Hee;Park, Kap-Joo
    • Korean Journal of Environmental Biology
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    • v.26 no.1
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    • pp.30-35
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    • 2008
  • In order to investigate whether or not CCD-986sk cell line can be affected by Korean Ecklonia stolonifera Okamura, we examined the MTT assay when we treated Korean Ecklonia stolonifera Okamura extract in CCD-986sk human fibroblast cell line. The sample were tested for cell proliferation activity by means of a modification of the MTT assay. Ecklonia stolonifera Okamura extract showed significantly strong cell proliferation activity at the range of from 6.25 mg $mL^{-1}$ to 1.56 mg $mL^{-1}$ compared with control group. And in order to search for inhibition agents of skin melanin formation, we tested for inhibition effect of melanin pigmentation of Korean Ecklonia stolonifera Okamura using Clone M-3 mouse melanocyte cell lines. when we treated the extracts of Ecklonia stolonifera Okamura to the mouse melanocyte cell lines, the sample showed a significantly little formation of melanin pigments compared with control group at the only range of 200 mg $mL^{-1}$. These results suggest that extract of Korean Ecklonia stolonifera Okamura may represents an excellent candidate for inhibition of melanin pigmentation and for protection of human skin aging at in vitro level.

Development of New Functional Dairy Products Containing Probiotics for Improving Human Health: A Review (Probiotics를 이용한 새로운 건강 증진 기능성 유제품 개발에 관한 연구: 총설)

  • Kim, Dong-Hyeon;Chon, Jung-Whan;Kim, Hyun-Sook;Kim, Hong-Seok;Song, Kwang-Young;Kim, Soo-Ki;Jeong, Dong-Gwan;Seo, Kun-Ho
    • Journal of Dairy Science and Biotechnology
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    • v.33 no.1
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    • pp.35-46
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    • 2015
  • Recently, much attention has been paid to the development of a value-added food category containing probiotics so as to improve human health and prevent diseases. Among various foods, the health benefits of milk and dairy products are known to humanity, and could be attributed to the bioactive components present in milk. In fermented milk products, the health benefits could be due to suitable modulation activities produced by the action of probiotic bacteria. Besides the modification of various milk components, probiotics might also act directly as preventive and therapeutic agents against some severe diseases. Probiotics promote health via their positive effects on the immune response, stimulation of natural immunity, and modulation of the production of antimicrobial peptides, cytokines, and so on. Whey proteins, a byproduct of cheese production could also have anticarcinogenic, immunostimulatory, antimicrobial, and health-promoting activities such as improving insulin sensitivity and reducing fat deposition. Therefore, milk and dairy products containing probiotics could provide various opportunities in the field of functional foods. Additionally, these functional foods may be important in the human diet and may help improve human health and prevent diseases.

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Physiological Activity of Methanol Extracts from Sambucus sieboldiana var. miquelii (Nakai) Hara (지렁쿠나무 메탄올 추출물의 생리활성 연구)

  • Oh, Yu Jin;Cho, Hae Jin;Woo, Hyun Sim;Byeon, Jun-Gi;Kim, Yeong-Su;Kim, Dae Wook
    • Journal of Life Science
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    • v.30 no.11
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    • pp.965-972
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    • 2020
  • Sambucus sieboldiana var. miquelii (Nakai) Hara is distributed in Korea, China, and Japan, and has been used as an anti-rheumatic in folk medicine in oriental countries. The present study aims to investigate the potential use of this species in health functional foods, cosmetics, and food preservatives. Methanol extracts of leaves and branches from this plant were prepared to quantitatively analyze the total phenol and flavonoid contents, and to investigate the antioxidative and enzyme inhibitory activities, and the inhibition of nitric oxide (NO) production activity. The results showed that the total polyphenol and flavonoid contents of the crude extract were 1.52±0.1 mg/g and 1.73±0.1 mg/g, respectively. S. sieboldiana polyphenols exhibited potent scavenging activity shown by 2, 2'-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging assay and 2, 2-azinobis-(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) radical cation assay. The crude extract also exhibited significant α-glucosidase and tyrosinase inhibitory activity with IC50 values of 183.5 ㎍/ml and 323.9 ㎍/ ml, respectively. Additionally, the crude extract exhibited strong anti-inflammatory activity determined through the nitric oxide inhibition assay in a dose-dependent manner with an IC50 value of 36.7 ㎍/ml and no cytotoxic effect on the macrophages. Therefore, we demonstrated that the leaves and branches of S. sieboldiana extract possess antioxidant, anti-diabetic, depigmentation potential, and NO production inhibitory activities. According to recent research, S. sieboldiana has great potential as a source of the bioactive compound which could be used as food, cosmetics, and pharmaceutical agents.

Study on the Antioxidant and Human Neutrophil Elastase Inhibitory Activities of Mushroom Ramaria formosa Extracts (붉은싸리버섯 추출물의 항산화 및 Human Neutrophil Elastase 저해활성)

  • Kim, Kwan-Chul;Kwon, Yong-Beom;Jang, Hae-Dong;Kim, Jae Wha;Jeong, Jae Cheol;Lee, Ik-Soo;Ha, Byung-Jo;Yoo, Ick-Dong
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.42 no.3
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    • pp.269-278
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    • 2016
  • In searching for novel agents for skin anti-aging from natural resources, we found that the extract of the fruiting bodies of Ramaria formosa (R. formosa) had significant antioxidant and human neutrophil elastase (HNE) inhibitory activities. R. formosa extract exhibited a considerable DPPH radical scavenging activity with an antioxidant content of 117.0mg/mL (ascorbic acid equivalents) at the concentration of $500{\mu}g/mL$. The capacity of R. formosa extract to scavenge peroxy radicals measured by ORAC assay also showed dose-dependent antioxidant effect with $ORAC_{Roo}$ (trolox equivalents, $1{\mu}M$) values of 0.8, 5.2, and 7.8 at the concentrations of 1, 10, and $20{\mu}g/mL$. The cellular antioxidant capacity of R. formosa extract was investigated by assaying the cellular fluorescence intensity using dichlorodihydrofluorescein (DCF). The cellular oxidative stress induced by AAPH, $Cu^{2+}$ or $H_2O_2$ in HepG2 cells was significantly attenuated by more than 30% at $20{\mu}g/mL$ of R. formosa extract. HNE activity was reduced by treatment with R. formosa extract in a dose-dependent manner, and the $ED_{50}$ value for the ethanol extract of R. formosa was $42.9{\mu}g/mL$. R. formosa extract did not exhibited antimicrobial activity against four microorganisms including Bacillus subtilis (B. subtilis), Escherichia coli (E. coli), Candida albicans (C. albicans), Aspergillus oryzae (A. oryzae). Furthermore, the extract did not affect the inflammatory cytokine production of interleukin-10 and interferon-${\gamma}$ in NK92 cells. From the above results, we found that R. formosa extract has considerable antioxidant and elastase inhibitory effects, and does not stimulate immune cells. These findings suggest that R. formosa extract may be used as a bioactive component in cosmetic composition.