• Title/Summary/Keyword: Elastase Inhibitory Activity

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Enzymological Evaluation of Oral Inflammation inhibitory activity by Aloe vera peel extract (Aloe vera peel 추출물에 의한 구강염증 저해 효과의 효소학적 평가)

  • Pack, Chung-Sun;Ryu, Il-Hwan;Lee, Kap-Sang
    • Korean Journal of Food Science and Technology
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    • v.33 no.6
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    • pp.753-759
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    • 2001
  • To evaluate antiinflammation of Aloe vera peel, antiimflammation substances were extracted from Aloe vera peel and identified, and we investigated the effect of the its substance the inhibitory effect on the activity of hyaluoronidase, elastase, collagenase and prostaglandin endoperoxide synthase. The water extract from Aloe vera peel were successfully purified with solvent fractionation, silica gel column chromatography, preparative thin layer chromatography and UV spectrometer. Two purified active substances were identified as aloe-emodin and barbaloin by Mass Spectrometer, $^1H-NMR$ and FT-IR. Aloe-emodin and barbaloin. $IC_{50}$ values of aloe-emodin and barbaloin against hyaluronidase activity were 40 and $70\;{\mu}g/mL$, respectively. Leuckocyte elastase, which is related to the destruction of various tissue, $IC_{50}$ values of them were 50 and $60\;{\mu}g/mL$, respectively. $IC_{50}$ values of aloe-emodin and barbaloin against collagenase activity were 40 and $60\;{\mu}g/mL$, respectively. and $IC_{50}$ values of aloe-emodin and barbaloin aganist the prostaglandin endoperoxide synthase, which play an important role in inflammatory reactions, were 40 and $70\;{\mu}g/mL$, respectively. Inhibitory effects of aloe-emodin, barbaloin and aspirin against carrageenan paw edema were 74.9, 52.9 and 51.9% as inhibiton percentage, respectively, at dose of 100 mg/kg and that of indomethancin was 49.7 at dose of 10 mg/kg. Cell cytotoxicity of barbaloin against human gingival cells was lower than that of aloe-emodin. Aloe-emodin and barbaloin did not show cytotoxicity against human gingival cells at concentration of 1.0 and $5.0\;{\mu}g/mL$, However, aloe-emodin and barbaloin showed less cytotoxicity than chlorhexidine, which usually have been used as the agent of anticaries and antiinflammation. These results suggested that aloe-emodin and barbaloin from Aloe vera peel have the effect of anticaries and antiinflammation.

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Comparison of Antioxidant, Wrinkle Improvement, and Whitening Efficacies of Extracts from Pinus koraiensis Cone Scale Using Extraction Methods (추출방법에 따른 잣나무(Pinus koraiensis) 구과피 추출물의 항산화, 주름개선 및 미백 효능 비교)

  • Chae, Jungwoo;Kim, Jeongyou;Jo, Huiseon;Lee, Jin-young
    • Journal of Korean Society of Forest Science
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    • v.110 no.3
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    • pp.431-439
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    • 2021
  • The present study evaluated the antioxidant activity, skin wrinkle reduction, and whitening activity of Pinus koraiensiscone scale extracts made with three different solvents (ethanol, supercritical fluid, and a mixture of both). Total polyphenol content was 11.03 mg/g GAE in the supercritical fluid extractand 33.79 mg/g GAE in the 70% ethanol extract. Electron donating ability of 1,000 ㎍/mL extract was 13.60% in the supercritical fluid extract, 91.37% in 70% ethanol extract, and 71.62% in mixed solvent extract. SOD-like activities in 100 ㎍/mL extract using supercritical fluid, 70% ethanol, and mixed solvents were 16.49%, 21.84%, and 10.7%, respectively. The ABTS+ radical scavenging activities of 1,000 ㎍/mL extract were 38.19%, 80.23%, and 78.72%for supercritical fluid extract, 70% ethanol extract, and mixed solvent extract, respectively. Tyrosinase inhibitory activities in 1,000 ㎍/mL extract were 24.54%, 36.55%, and 15.23% for supercritical fluid extract, 70% ethanol extract, and mixed solvent extract, respectively. Elastase inhibitory activities in 1,000 ㎍/mL extract were 15.62%, 22.56%, and 26.64% for supercritical fluid extract, 70% ethanol extract, and mixed solvent extract, respectively. Skin astringent activity (81.23% with 5000 ㎍/mL extract) was only detected in the 70% ethanol extract. Supercritical fluid and mixed solvent extracts showed no such activity. Our analysis of Pinus koraiensiscone scale extracts show that the highest aggregate activity was found in the 70% ethanol extract, followed by mixed solvent and supercritical fluid extracts. Therefore, our results oppose the hypothesis stating supercritical extract has the highest total polyphenol content and antioxidant activity.

An In Vitro Study on the Activity of Abelmoschus manihot L. Flower Extract on Skin Anti-wrinkle and Skin Whitening (금화규(Abelmoschus manihot ) 꽃 추출물의 In Vitro 피부 미백 및 주름 개선 효능 연구)

  • Kwon, Hyun-Ji;Beom, Seok-Hyun;Hyun, Jin-A;Kang, Eun-Bin;Park, Ha-Eun;Han, Dong-Geun;Kim, Hyun-Jeong;Choi, Eun-Young;An, Bong-Jeon
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.47 no.4
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    • pp.353-360
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    • 2021
  • In this study, the skin whitening and anti-wrinkle activity of Abelmoschus manihot (A. manihot) flowers were evaluated as a cosmetic material. A. manihot flowers were extracted using water and 70% ethanol. Tyrosinase inhibitory activity was evaluated to increase concentration-dependent inhibitory activity in both water (AMW) and 70% ethanol extracts (AME), and was found to inhibit melanin biosynthesis at concentrations that did not affect survival in B16F10 cell lines at 10, 25, 50, 75, and 100 ㎍/mL. As a result of measuring the anti-wrinkle effectiveness of A. manihot flowers, 70% ethanol extract (AME) showed higher anti-wrinkle activity than water extract (AMW). Through the results of this study, it is considered that the A. manihot flower extract can be used as a functional cosmetic material with whitening and anti-wrinkle activity.

A Study on the Anti-wrinkle Activities of Sesamum indicum L. Ethanol Extracts on CCD-986sk (CCD-986sk 세포 내 참깨 에탄올 추출물의 항주름 활성 연구)

  • Joo, Da-Hye;Yoo, Dan-Hee;Lee, Jin-Young
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.42 no.4
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    • pp.377-385
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    • 2016
  • In order to investigate the possibility of Sesamum indicum L. (S. indicum) extract as an active ingredient for wrinkle-care cosmetics, we prepared 70% ethanolic extract of S. indicum and measured its elastase inhibitory activity and collagenase inhibitory activity. We also evaluated the effect of S. indicum extract on protein and mRNA expression of MMPs in fibroblast cell (CCD-986sk). For anti-wrinkle effects, elastase inhibition activities and collagenase inhibition activities were 37.8% and 45% at a dose of $1,000{\mu}g/mL$ of S. indicum 70% ethanol extract. For a cell viability test, measured on fibroblast cell by ethanol extract of S. indicum, results showed 96% with cell viability at $100{\mu}g/mL$ concentration. According to the results of western blot of ethanol extract from S. indicum the expression of the matrix metalloproteinase-1 (MMP-1), matrix metalloproteinase-2 (MMP-2), matrix metalloproteinase-3 (MMP-3) protein was decreased by 63%, 43%, 49% at $100{\mu}g/mL$ concentration. Reverse transcription-polymerase chain reaction (PCR) of ethanol extract from S. indicum showed that the expression of MMP-1, MMP-2, MMP-3 mRNA was decreased by 82%, 79%, 82% at $100{\mu}g/mL$ concentration. The findings suggest that 70% ethanol extract from S. indicum has potential as a cosmeceutical ingredient with anti-wrinkle effects.

Effectiveness and Preparation of Microsome containing Fermented Squalene (발효 스쿠알렌을 함유한 마이크로좀의 제조 및 효능효과)

  • Kim, Ye-Jin;Kim, Tae-Hyun;Cho, Heui-Kyoung;Seong, Nak-Jun;Kim, In-Young;Yoo, Kwang-Ho;Kim, Young-Ho
    • Journal of the Korean Applied Science and Technology
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    • v.37 no.5
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    • pp.1159-1170
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    • 2020
  • In this study, to improve the stability of fermented squalene developed using microorganisms, Microsome-SQ20 was prepared, and its physical behavior, properties, and efficacy were studied. The appearance of Microsome-SQ20 was a transparent liquid, no smell, and had a specific smell. The color was a transparent liquid, and the specific gravity was 0.928 and the pH was 5.82 (20% solution), forming a nano-emulsion suitable for use in cosmetics. It was confirmed that the content of the main component of squalene was 20.05%, which was stably sealed. The particle size measured by 0.1% aqueous solution of Microsome-SQ20 was 134.8 nm to obtain a bluish emulsified phase. The antioxidant effects of F-SQ and MF-SQ by DPPH radicals were 80.72% and 81.5%, respectively, showing superior effects compared to L-ascorbic acid. The cell viability of squalene (SQ), fermented squalene (F-SQ) and microsome squalene (MF-SQ) was at 10 ppm, respectively, showing 121.2%, 150.3%, and 129.9% cell viability. It was found that SQ, F-SQ, and MF-SQ had an elastase inhibitory ability of 8.7%, 10.33% and 8.7% at 10 ppm, respectively. In addition, the inhibitory ability of MMP-1 was 1.55%, 41.44%, 31.79% at 10 ppm for SQ, F-SQ, and MF-SQ, respectively, indicating that F-SQ significantly reduced the MMP-1 expression.

Evaluation of Physiological Activities of Cnidium officinale Makino Extracts with Different Solvents (추출용매에 따른 천궁(Cnidium officinale Makino) 추출물의 생리활성 평가)

  • Hur, Sang-Sun
    • Journal of the Korean Applied Science and Technology
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    • v.32 no.1
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    • pp.170-179
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    • 2015
  • The objective of this study was to investigate the physiological activities of Cnidium officinale Makino extracts on extraction solvents. The yield of ethanol extract, 87.54%, was higher than that of the hot water extract(83.06%) and of the methanol extract(78.32%). In the inhibitory activity of xanthine oxidase, the ethanol extracts and methanol from Cnidium officinale Makino appeared to show significantly higher activity than hot water extract at $1,000{\mu}g/mL$. The DPPH radical scavenging activities of the ethanol and the methanol extracts at $50-2,000{\mu}g/mL$ were 19.96-89.01% and 19.41-88.21%, respectively. The SOD-like activities of all the extracts improved with an increase in the treatment concentration. Both collagenase and elastase inhibitory activities were shown higher from the ethanol and methanol extract compared to that of hot water extract. The tyrosinase inhibitory activity of ethanol extract, 12.04-73.85%($50-2,000{\mu}g/mL$), was higher than that of the other extracts. Taken together, these data suggest that Cnidium officinale Makino extract is effective in whitening and anti-wrinkle effect, thus it might strongly be considered as potential functional cosmetic components.

Variation in bioactive principles and bioactive compounds of Rosa rugosa fruit during ripening (해당화 열매 성숙단계에 따른 생리활성 및 기능성 물질 변화 분석)

  • Kwak, Minjeong;Eom, Seung Hee;Gil, Jinsu;Kim, Ju-Sung;Hyun, Tae Kyung
    • Journal of Plant Biotechnology
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    • v.46 no.3
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    • pp.236-245
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    • 2019
  • Fruit ripening is a genetically programmed process involving a number of biochemical and physiological processes assisted by variations in gene expression and enzyme activities. This process generally affects the phytochemical profile and the bioactive principles in fruits and vegetables. To appraise the variation in bioactive principles of fruits from Rosa rugosa during its ripening process, we analyzed the changes in antioxidant and anti-elastase activities and polyphenolic compounds during the four ripening stages of fruits. Overall, an extract of unripe fruits contained the highest levels of total phenolic and flavonoid contents, radical scavenging activity, reducing power, oxygen radical antioxidant capacity, and elastase inhibitory activity, compared with the extracts of fruits at other stages of ripening. Additionally, we found that the reduction of flavonoid content occurs because of decreased transcriptional levels of genes involved in flavonoid biosynthesis pathway during the ripening process. Based on HPLC analysis, we found that the extract of unripe fruits contained the highest amount of myricetin, caffeic acid, chlorogenic acid, syringic acid, and p-coumaric acid and suggested that the antioxidant and anti-elastase activities of the extract obtained from stage 1, should be mediated by the presence of these compounds. Additionally, we analyzed the interaction sites and patterns between these compounds and elastase using the structure-based molecular docking approach, and suggested that chlorogenic acid strongly interacted with elastase. Together, these findings suggest that the maturity of fruits has profound effects on the pharmaceutical value of R. rugosa.

Synthesis of New 4-Oxo-2-Thioxo-1,2,3,4-Tetrahydropyrimidine Derivatives with an Incorporated Thiazolidinone Moiety and Testing Their Possible Serine Protease and Cercarial Elastase Inhibitory Effects with a Possible Prospective to Block Penetration of Schistosoma mansoni Cercariae into the Mice Skin

  • Bahgat Mahmoud Mohamed;Maghraby Amany Sayed;Heiba Mogeda Emam;Ruppel Andreas;Fathalla Omar Abd-elfattah Mohamed
    • Archives of Pharmacal Research
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    • v.28 no.9
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    • pp.1002-1012
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    • 2005
  • 5-Substituted 4-oxo-2-thioxo-1,,2,3,4-tetrahydropyrimidine were synthesized by interaction of 4­oxo-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-sulfonylhydrazide with some aldehydes to give the corresponding Schiff-bases, which after cyclization gave corresponding thiazolidinones. For some of the thiazolidinones, Mannich bases reaction was carried out. All the derivatives were tested for their possible inhibitory effect on Schistosoma mansoni cercarial elastase (CE). Only, N'-(4-methylbenzyledine)-4-oxo-2-thioxo-1,2 ,3,4-tetrahydropyrimidine-5-sulfonylhydrazide was found to have potent inhibitory effect on the CE activity with $IC_{50} = 264{\mu}M.$ Upon its use as a paint for mice tails before infection with S. mansoni cercariae, the compound formulated in jojoba oil caused a significant reduction ($93\%$; P-value = 0.0002) in the worm burden. IgG & IgM in mice sera were measured by using several S. mansoni antigens by ELISA. Sera from treated infected mice (TIM) 2, 4, and 6 weeks (W) post infection (PI) showed 1.2 folds lower, 1.2 folds higher, 1.7 folds lower IgM reactivity against soluble cercarial antigenic preparation (CAP), respectively, when compared with sera collected from infected untreated mice (IUM). Sera from TIM 2, 4, and 6WPI showed 1.3, 1.6, and 1.7 folds higher IgG reactivity, respectively against CAP than the IgG reactivity from IUM. Sera from TIM 2, 4 and 6WPI showed 1.5, 1.2 folds lower and 1.4 folds higher IgM reactivity, respectively against soluble worm antigenic preparation (SWAP) when compared with sera collected from IUM. Sera from TIM 2, 4, and 6WPI showed 1.4, 1 folds lower and 1 fold higher IgG reactivity, respectivley to SWAP when compared with sera from IUM. Sera from TIM 2, 4, and 6WPI had generaly lower IgM and IgG reactivities against soluble egg antigen (SEA) when compared with sera from IUM.

In vitro anti-skin-aging effects of dried pomegranate concentrated powder

  • Lee, Dae-Geon;Choi, Beom-Rak;Ku, Sae-Kwang;Kang, Su-Jin;Park, Hye-Rim;Sung, Mi-Sun;Lee, Young-Joon;Park, Ki-Moon
    • Journal of Society of Preventive Korean Medicine
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    • v.22 no.2
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    • pp.109-123
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    • 2018
  • Purpose : In this study, we intended to observe the anti-wrinkle and moisturizing effects of dried pomegranate juice concentration powder (PCP) using in vitro test. Materials and methods : Antioxidant effects of PCP were determined by free radical scavenging capacity (DPPH assay) and the cytotoxicity of PCP was examined in human keratinocyte (HaCaT) and human primary dermal fibroblast-neonatal (HDF) cells. To investigate the moisturizing effect of PCP, hyaluronan synthesis was examined in HaCaT cells. Activity of procollagen production were assessed in HDF cells and elastase inhibition properties of PCP were evaluated in cell free condition, to determine their anti-wrinkle effects. Metalloproteinase 1 (MMP-1) activity was also assessed following UVB irradiation, in the current in vitro experiment. Results : No PCP treatment related significant cytotoxic effects were demonstrated against to the both HDF and HaCaT cells. PCP showed favorable free radical scavenging activities in dose-dependent manner. In PCP-treated HaCaT cells, hyaluronan synthesis was non-significantly but markedly increased, and pro-collagen productions were significantly increased in HDF cells, at all three different concentrations (0.25, 0.75 and 1 mg/ml), and elastase inhibitory activities were observed by PCP treatment. A significant decrease in UVB-induced MMP-1 activity was also observed in 1 mg/ml PCP-treated HDF cells as compared to those of UVB-exposed cells. Conclusions : Taken together, these results suggest that PCP has favorable antioxidant, anti-wrinkle and moisturizing effects without meaningful cytotoxicity on HDF and HaCaT cell lines.

Verification of anti-oxidative activity of Aruncus dioicus, a native plant of Ulleungdo (울릉도 자생식물 삼나물(Aruncusdioicus)의 항산화 활성 검증)

  • Kim, Dong-Hee;Moon, Yong-Sun;Son, Jun-Ho
    • Journal of Plant Biotechnology
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    • v.42 no.1
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    • pp.55-59
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    • 2015
  • The extracts of Aruncus dioicus were investigated for anti-oxidant and biological activities in order to verify its potential as functional ingredients of cosmetic products. The ethyl acetate (EtOAc) extract of A. dioicus showed excellent scavenging activity using DPPH and ABTS anti-oxidant analysis at the $1,000{\mu}g/mL$ concentration. While tyrosinase inhibitory effect was measure for whitening assay and showed 59.2%, the suppression levels of elastase and collagenase were 56% and 90% respectively for anti-wrinkle activity. Therefore, it is plausible to conclude that A. dioicus extract, especially EtOAc fraction which has outstanding whitening, anti-oxidant, and anti-wrinkle activities, could be used as a new functional materials for cosmetics.