• 한방안이비인후피부과학회지
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• 제23권1호
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• pp.135-148
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• 2010

Recently, the demands for the effective and safe depigmentating and anti-aging agents of the skin have increased due to the medical, pharmaceutical and cosmetic reasons. The aim of this study is to search Galla Rhois (GR) inhibitory activity against aging process of skin in vitro. GR was screened for their inhibitory activity against elastase. GR (final concentration 1 mg/ml) appeared over 40% of inhibition of elastase activity. So we investigated anti wrinkle effects of GR look through MMP-1 inhibition activity. Also Extracts of GR showed higher anti-tyrosinase activity than arbutin (final concentration 1 mg/ml). These results suggest that GR could be potential sources of anti-aging and whitening effects for the skin. Objective : Galla Rhois extracts, Elastase (pancreatic from porcine pancreas), N-Succinyl-(Ala)3-p-nitroanilide, Ursolic acid, mushroom tyrosinase, L-tyrosine, arbutin, Amicon Ultra, Hand Hold UV lamp, MMP-1 primary antibody, MMP-1 secondary antibody Result : 1. GR appeared over 40% of elastase inhibitory activity. 2. GR had MMP-1 inhibition activity. 3. GR showed higher anti-tyrosinase activity than arbutin. Conclusion : According to above results, it is supposed that Galla Rhois could be strong potential sources of anti-aging and whitening effects for the skin.

• International Journal of Oral Biology
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• 제46권1호
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• pp.51-59
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• 2021

Periodontal disease is an inflammatory disease that affects the destruction of the bone supporting the tooth and connective tissues surrounding it. Periodontal ligament fibroblasts (PDLFs) induce overexpression of matrix metalloproteinase (MMP) involved in periodontal disease's inflammatory destruction. Osteoclasts take part in physiological bone remodeling, but they are also involved in bone destruction in many kinds of bone diseases, including osteoporosis and periodontal disease. This study examined the effect of baicalin on proteolytic enzymes' production and secretion of inflammatory cytokines in PDLFs and RAW 264.7 cells under the lipopolysaccharide (LPS)-induced inflammatory conditions. Baicalin inhibited the expression of the protein, MMP-1 and MMP-2, without affecting PDLFs' cell viability, suggesting its possibility because of the inhibition of phosphorylation activation of mitogen-activated protein kinase's p38, and the signal transduction process of nuclear factor κB (NFκB)-related protein. Also, baicalin reduced the expression of MMP-8 and MMP-9 in RAW 264.7 cells. This reduction is thought to be due to the inhibition of the signal transduction process of NFκB-related proteins affected by inhibiting p65RelA phosphorylation. Also, baicalin inhibited the secretion of nitric oxide and interleukin-6 induced by LPS in RAW 264.7 cells. These results suggest that baicalin inhibits connective tissue destruction in periodontal disease. The inhibition of periodontal tissue destruction may be a therapeutic strategy for treating inflammatory periodontal-diseased patients.

• 한국식물생명공학회:학술대회논문집
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• 한국식물생명공학회 2004년도 생명공학 실용화를 위한 비젼
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• pp.81-90
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• 2004

Sialic acid containing glycosphingolipids (gangliosides) have been implicated in the regulation of various biological phenomena such as atherosclerosis. Recent report suggeststhat exogenously supplied disialoganglioside (GD3) serves a dual role in vascular smooth muscle cells (VSMC) proliferation and apoptosis. However, the role of the GD3 synthase gene in VSMC responses has not yet been elucidated. To determine whether a ganglioside is able to modulate VSMC growth. the effect of overexpression of the GD3 synthase gene on DNA synthesis was examined. The results show that the overexpression of this gene has a potent inhibitory effect on DNA synthesis and ERK phosphorylation in cultured VSMC in the presence of PDGF. The suppression of the GD3 synthase gene was correlated with the down-regulation of cyclinE/CDK2. the up-regulation of the CDK inhibitor p21 and blocking of the p27 inhibition,whereas up-regulation of p53 as the result of GD3 synthase gene expression was not observed. Consistently, blockade of GD3 function with anti-GD3 antibody reversed VSMC proliferation and cell cycle proteins. The expression of the CD3 synthase gene also led to the inhibition of TNF--induced matrix metalloproteinase-9 (MMP-9) expression in VSMC as determined by zymography and immunoblot. Furthermore, GD3 synthase gene expression strongly decreased MMP-9 promoteractivlty in response to TNF-. This inhibition was characterized by the down-regulation of MMP-9,which was Iranscriptionally regulated at NF-B and activation protein-1 (AP-1) sites in the MMP-9promoter Finally, the overexpression of MMP-9 in GD3 synthase transfectant cells rescued VSMC proliferation. However MMP-2 overexpression was not affected the cell proliferation. These findings suggest that the fl13 synthase gene represents a physiological modulator of VSMC responses that may contribute to plaque instability in atherosclerosis.

• 치위생과학회지
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• 제10권1호
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• pp.25-29
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• 2010

치주질환의 예방 및 치료 효과를 연구하기 위해 수 종의 천연물을 이용하여 P. gingivalis에 대한 항균력과 IL-$1{\alpha}$ 생성 억제율을 평가하여 1차 선별한 후 MMP-1 활성 억제율 평가와 SOD 활성평가를 수행한 결과 다음과 같은 결론을 얻었다. 1. P. gingivalis에 대한 항균력 평가 결과 은행엽, 육두구, 대황, 후박, 구절초, 용아초, 목향, 세신, 산초, 회향 추출물에서 우수한 항균효과가 나타났다. 2. 인터루킨-$1{\alpha}$ (IL-$1{\alpha}$) 생성 억제율 평가 결과 은행엽, 작약, 육두구, 하고초, 후박, 과루, 산약 추출물이 우수한 IL-$1{\alpha}$ 생성 억제율을 나타내었다. 3. 매트릭스 메탈로프로테나제-1(MMP-1)의 활성 억제평가 결과, 육두구, 은행엽 추출물이 우수한 MMP-1 활성 억제율을 나타내었다. 4. 슈퍼록사이드 디스뮤타제 (Superoxide dismutase, SOD) 활성 평가 결과 은행엽, 산약, 육두구 추출물서 우수한 SOD 활성을 나타내었다. 5. 구강용 제품에 적용 시 은행엽 추출물은 우수한 잇몸질환 예방 및 치료 효능을 나타낼 수 있다.

• BMB Reports
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• 제32권1호
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• pp.60-66
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• 1999

Matrix metalloproteinase-2 (MMP-2; 72-kDa gelatinase; 72-kDa type IV collagenase; gelatinase A) plays an important role in normal physiological processes and in many pathologic processes such as arthritis and metastasis of cancer. Tissue inhibitor of metalloproteinases-2 (TIMP-2) binds to proMMP-2 or mature MMP-2 at a 1:1 ratio and inhibits the catalytic activity of MMP-2. We demonstrated that the baculovirus/insect cell system does not have TIMP-2 activity. The human proMMP-2 free of TIMP-2 was expressed in the expression system and purified by one-step affinity chromatography using gelatin-Sepharose. The free proMMP-2 was autoactivated to the mature MMP-2 and autodegraded into smaller molecular weight forms in the absence of external activator. The activation and autodegradation of the proMMP-2 was much more rapid in the presence of 4-aminophenylmercuric acetate (APMA). Addition of TIMP-2 inhibits both APMA-induced activation and autodegradation of the free proMMP-2. However, an increasing concentration of TIMP-2 more readily inhibited activation of the free proMMP-2 than autodegradation. These results demonstrate that TIMP-2 plays roles in inhibition of both activation and autodegradation of the free proMMP-2 in addition to inhibition of the catalytic activity of MMP-2.

• 대한화장품학회지
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• 제30권3호
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• pp.393-397
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• 2004

L-Carnitine $({\beta}-hydroxy-\gamma-trimethyl-ammoniumbutyric{\;}acid)$은 분자량이 적은 수용성 분자로서 세포 내 지방 대사에서 중요한 역할을 수행한다. 지방산의 운반 분자인 아실-코에이(acyl-CoA)가 미토콘드리아의 세포막을 투과하지 못하기 때문에 지방산은 CoA로부터 카르니틴으로 운반되어 미토콘드리아에서 작용한다. 노화와 연관된 L-carnitine의 기능을 확인하기 위하여 MMP inhibition assay와 자외선 조사에 의해 유도된 MMP 발현에 대한 영향을 확인하였다. MMP inhibition assay는 콜라겐을 이용한 형광분석법을 실시하였고 자외선 조사에 의해 유도된 MMP 발현양은 ELISA로 정량하였으며 그 활성은 젤라틴 기질 zymography로 확인하였고 MMP mRNA 발현양은 RT-PCR ELISA로 확인하였다. 또한, 사람을 이용한 임상 실험을 통하여 주름 개선 효과를 평가하였다. L-carnitine은 농도 의존적으로 MMP 저해 활성을 나타났으며 $IC_{50}$값은 2.45 mM이었으며 자외선 조사에 의해 발현된 MMP 활성을 강하게 저해하였다. 자외선 조사에 의해 발현되는 MMP에 대해 단백질의 양적인 변화는 $40\%$ 정도 감소되었으며 L-carnitine 처리에 의해 농도 의존적으로 MMP mRNA의 발현양은 감소되었다. 이러한 실험결과를 통하여 L-carnitine은 MMP 효소의 저해능 뿐만 아니라 자외선 조사에 의해 유도되는 MMP 단백질 발현과 mRNA 유전자 수준에서의 조절이 가능함을 확인하였다. 사람을 이용한 임상 실험에서는 $1\%$ 카르니틴을 함유하는 화장품을 약 3개월간 사용 후에는 유의적으로 주름 개선 효과를 확인하였다. 결론적으로 L-Carnitine은 광노화에 관여하는 MMP 활성과 발현 조절 메커니즘을 통하여 광손상에 대응하는 항노화 소재로서의 화장품에 매우 효과적이었음을 확인하였다.

• 동의생리병리학회지
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• 제21권1호
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• pp.243-249
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• 2007

The French paradox has been attributed to the antioxidant properties of flavonoids present in the red wine. Amentoflavone(AF) is a bi-flavonoid compound with anti-fungal and anti-inflammatory activities. We isolated AF from Selaginella tamariscina, and studied its effects on nuclear factor-B(NF-B)-mediated MMP-9 gene expression in RAW264.7 cells. AF blocked the lipopolysaccharide(LPS)-induced expression of MMP-9. Zymographic and immunoblot analyses showed that AF suppressed LPS-induced MMP-9 expression in a dose-dependent manner. To clarify the mechanistic basis for its inhibition of MMP-9 induction, we examined the effect of AF on the transactivation of MMP-9 gene by luciferase reporter activity using -1.59 kb flanking region. AF potently suppressed the reporter gene activity. This inhibition was characterized by down-regulation of MMP-9, which was transcriptionally regulated at NF-B site and activation protein-1 (AP-1) site in the MMP-9 promoter, two important nuclear transcription factors that are involved in MMP-9 expression. These findings indicate the efficacy of AF in inhibiting MMP-9 expression through the transcription factors NF-B and AP-1 on LPS-induced RAW264.7 cells.

• 약학회지
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• 제48권2호
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• pp.165-170
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• 2004

The production of matrix metalloproteinases (MMPs) by the UV irradiated skin fibroblast and the degradation of extracellular matrix (ECM) by these enzymes is known as one of the main reasons of photoaging. In this paper, to investigate the relationship between aging and Selaginella tamariscina extract (STE), we investigated the effects of antioxidant and expression of UVA-induced MMP-1 in human dermal fibroblasts. STE was found to show scavenging activities of radicals and reactive oxygen species (ROS) with the $IC_{50}$/ values of 65.1 $\mu\textrm{g}$/$m\ell$ against 1,1-diphenyl-2-picrylhydrazyl(DPPH) radical and 40.9 $\mu\textrm{g}$/$m\ell$ against superoxide radicals in the xanthine/xanthine oxidase system, respectively. UVA induced MMP expression was reduced 75.5% by treatment with STE, and MMP-1 mRNA expression was reduced in a dose-dependent manner. Therefore STE was able to significantly inhibition of MMP expression in protein and mRNA level. All these results suggested that STE may act as an anti-aging agent by antioxidation and reducing UVA-induced MMP-1 production.

• 대한본초학회지
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• 제31권4호
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• pp.53-60
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• 2016

Objective : The purpose of this study was to investigate anti-aging and antioxidant effects of extracts of Nelumbo nucifera leaves (NN-L) using ethanol on skin .Methods : Each part of leaves(NN-L), flowers(NN-F) and stem(NN-S) was extracted with 70% ethanol. We performed radical scavenging assay(DPPH, ABTS+, Superoxide anion radical), elastase inhibition assay, collagenase inhibition assay. NN-L extracts were tested for cell viability(MTT assay), MMP-1 inhibition and MMP-1 protein expression on CCD-986sk cells (human fibroblast line).Results : Recently, many studies have reported that elastin is also involved in inhibiting or repairing wrinkle formation, although collagen is a major factor in the skin wrinkle formation. We measured its free radical scavenging activity, elastase inhibitory activity and expression of MMP-1 (matrix metalloprotease-1) in human fibroblast cells. Among the parts of Nelumbo nucifera, NN-L showed the highest antioxidant activities and in radical scavenging. DPPH, ABTS+ and Superoxide anion radical scavenging activity of NN-L at concentration of 1,000 μg/mL were 91.43%, 99.31% and 73.7% respectively. In vitro elastase and collagenase inhibition effects of NN-L at concentration of 1,000 μg/mL was 42.8% and 55.3% respectively. The ethanol extract of NN-L showed cell viability of 95.4% in 50 μg/mL concentration. In addition, The results from Western blot assay showed that NN-L decreased the expression of MMP-1 protein in a dose-dependent manner (by up to 35.0% at 50 μM).Conclusion : The findings suggest that the NN-L great potential as a cosmeceutical ingredient with antioxidant and anti-wrinkling effects.

• Advances in Traditional Medicine
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• 제5권4호
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• pp.283-293
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• 2005

Our previous study showed that a novel synthetic shikonin derivative, 6-(1-hydroxyimino-4-methylpentyl)5,8-dimethyoxy 1,4-naphthoquinone S-52 (DMNQ S-52) induced apoptosis. In the present study, we investigated its anti-metastatic activities as compared with shikonin because DMNQ S-52 was synthesized for overcoming weak points of shikonin such as high toxicity, low solubility and deleterious effects. DMNQ S-52 showed the weaker cytotoxicity $(IC_{50};\;12.3{\pm}1.6\;{\mu}M)$ against Lewis lung carcinoma (LLC) cells than that of shikonin $(IC_{50};\;4.2{\pm}1.1\;{\mu}M)$. DMNQ S-52, at non-toxic concentrations $(less\;than\;10\;{\mu}M)$, significantly inhibited the invasion and migration of LLC cells. DMNQ S-52 also significantly inhibited the production of MMP-9, MTl-MMP and uPAR. Moreover, daily i.p. administration of DMNQ S-52 at dose of 5 mg/kg in mice resulted in a potent inhibition of the primary tumor size of LLC in the lung as well as the metastasis of lymph nodes. These findings suggest that the DMNQ S-52 has therapeutic potential to inhibit metastasis via inhibition of MMP family and uPA/plasminogen system.