• Korean Journal of Food Science and Technology
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• v.39 no.6
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• pp.669-675
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• 2007

The present study was conducted to explore the anti-inflammatory action of $2-hydroxyethyl-{\beta}-undecenate$ (HPS) purified from Cumin (Cuminum cymium L.) seed against periodontitis. From the study in which human leukocyte was employed to detect the inhibiting effects of 5-lipokygenase and cyclooxygenase, enzymes generating carriers of infection like $LTB_4$ and PGs, as well as of collagenase and elastase, organ-destroying enzymes, following conclusions could be drawn: HPS was found to inhibit leukotrien $B_4$ biosynthesis by stimulating more than 97% of human polymorphonuclear leukocyte (PMNL) with addition of $5\;{\times}\;10^{-2}\;M$ when $IC_{50}$ was set at $2\;{\times}\;10^{-4}\;M$. Ninety-two percent of enzyme activation turned out to be inhibited when $5\;{\times}\;10^{-2}\;M$ was added in a test to prove inhibiting effects of HPS against activation of PMNL 5-lipoxygenase from homogeneous humans and purified 5-lipoxygenase on the market. Besides, $IC_{50}$ for enzyme activation was valued at $2.5\;{\times}\;10^{-4}\;M$, while the value of $IC_{50}$ for purified 5-lipoxygenase was $2.3\;{\times}\;10^{-4}\;M$. The $IC_{50}$ values of COX-activated leukocyte and purified collagenase were $5.1\;{\times}\;10^{-4}\;M$ and $2.3\;{\times}\;10^{-4}\;M$, respectively. Moreover, the value of $IC_{50}$ for activation of leukocyte collagenase was $2\;{\times}\;10^{-3}\;M$, whereas that for purified collagenase was $5\;{\times}\;10^{-2}\;M$. In case of leukocyte elastase, addition of $5\;{\times}\;10^{-2}\;M$ inhibited its activation by 66%. In case of purified one, however, activation of enzyme was inhibited by 25% with addition of $5\;{\times}\;10^{-2}\;M$. Furthermore, the $IC_{50}$ value for activation of leukocyte elastase was revealed to be $7.5\;{\times}\;10^{-3}\;M$. From the virulence test with human gingiva cell, it was shown that, on the second day of cultivation, 47.83% of the cell had been activated when HPS was added by $5\;{\times}\;10^{-2}\;M$. Even the addition of HPS by $1\;{\times}\;10^{-2}\;M$ featured 68.53% of cell activation, suggesting relatively strong toxicity of the substance against gingiva cell.

• Proceedings of the Korean Society of Applied Pharmacology
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• 1994.04a
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• pp.230-230
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• 1994

Human leukocyte elastase(HLE)는 폐와 피부, 혈관등의 Connective tissue의 주요 구성물인 elastin을 분해하는 효소로써, 백혈구의 식균작용에도 관여한다. 그러나 이효소가 과다하게 분비되면 pulmonary emphysema와 adult respiratory distress syndrome, rheumatoid arthritis를 유발한다고 알려지고 있다. 지금까지 HLE억제제로 시판되는 의약품은 없으나, 최근에 Cephalosporin유도체가 이 효소의 억제제로 우수한 효과가 있다는 보고가 있은 후, HLE억제제로써 이들의 유도체가 개발되고 있다. 연구자들은 다음일반식에서 2번과 3번위치에 치환기를 도입시킨 수종의 Cephalosporin Sulfone의 유도체들을 합성하고. 이들의 HLE억제 효과를 Spectrophotometerqkdtlr을 이용하여 측정하였다. 합성화합물증 몇가지는 우수한 HLE억제효과를 보여주었고, 2번위치에 diphenylcyclopropyl ring과 같은 부피가 큰 치환체를 도입하면 효소억제력이 증가되었다.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.23 no.2
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• pp.7-22
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• 1997

Inhibitory effects of 200 medicinal plants on elastase activity were screened. Among the 200 plants, six plant extracts exhibited more than 65% of inhibition on elastase activity by their total methanol extracts at 1, 000$\mu\textrm{g}$/$m\ell$ as a final concentration. For six active plants including Areca catechu, Cinnamonum cassia, Myristica frograns, Curcumma longa, Alponia katsumadai, and Dryopteris crassirrhizoma, the inhibitory effects of their comsituents were examined on the activity of human leukocyte elastase, hyaluronidase and lipid peroxidation. In lipid peroxidation assay using TBA method, three of the 6 plants including Curcumma longa, Areca Catechu and Alponia katsumadai exhibited more than 70% of inhibition at the concentration of 1, 000$\mu\textrm{g}$/$m\ell$, but only one plant, Areca Ctechu showed high inhibitory effect on hyaluronidase activity. The results suggest that medicinal plants showing several biological activities may be potent inhibitors of anti-aging process on skin and that might be useful for application in cosmetics.

• Natural Product Sciences
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• v.9 no.4
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• pp.278-285
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• 2003

The serine proteases such as human leukocyte elastase (HLE) and porcine pancreatic elastase (PPE) are classified in the chymotrypsin family, and possibly the most destructive enzymes having the ability to degrade virtually all of the connective components in the body. In the present study, the extracts of water and methanol of Korean mistletoe (Viscum album var. coloratum) inhibited significantly the PPE activity. The fractions eluated on Amberlite XAD-2 from methanol extract were further purified on the repeated $SiO_2$ column chromatography and the fractions A, B and C were eluated. The fractions A, B and C at 3 mg/ml inhibited significantly the PPE activity up to 66%, 95% and 85%, respectively. In conclusion, the fraction A assumed as lignans or phenylpropanes, and fraction B and C assumed as triterpenoids showed the PPE inhibitory effects on the PPE and that these compounds in mistletoe may be used for treatment of pathological processes such as age-dependent tissue loss or inflammation.

• Proceedings of the PSK Conference
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• 2002.10a
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• pp.255.3-256
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• 2002

In the previous studies. we confirmed the anti-inflammatory components of Kalopanax pictus bark using activity-guided fractionation in vivo. For the elucidation of anti-inflammatory mechanism, we evaluated the effects of these components on the inhibition of NF-$\sub$K/B activity and human leukocyte elastase. A cell-based assay system developed in our laboratory was used in transfectant RAW 264.7 cells. (omitted)

• Journal of the Society of Cosmetic Scientists of Korea
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• v.24 no.3
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• pp.24-30
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• 1998

Inhibitory effects of the new material obtained from Areca catechu seed (CC-516) according to a special process, and its applicability to the skin as a cosmetic raw material in terms of its efficacy were presented. Areca catechu extract out of 150 medicinal plants, exhibited high inhibitory effect on the porcine pancreatic elastase ($IC_{50}$ : $40.8{\mu}$g/ml). It also had an inhibitory effect on the human leukocyte elastase ($IC_{50}$ : 48.1$\mu$g/ml), hyaluronidase ($IC_{50}$ : $416{\mu}$g/ml), antioxidative activity ($IC_{50}$ : $45.4\mu$g/ml) and free radical scavenging activity ($SC_{50}$ : $10.2{\mu}$g/ml). The cream contained 3％ of CC-516 improved skin hydration above 16.5％. Especially, the skin elasticity increases more than 35% and skin wrinkles decreased more than 23％. The CC-516 was designed to be utilized in cosmetology. The cream containing 3％ of this product has not only protecting effect on the skin mechanical properties provided by the collagen and the elastin in the derm but also restructuring effect of scarring or aging tissue.

• Archives of Pharmacal Research
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• v.25 no.6
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• pp.801-806
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• 2002

Cyclicpeptides are important targets in peptide synthesis because of their interesting biological properties. Constraining highly flexible linear peptides by cyclization is one of the mostly widely used approaches to define the bioactive conformation of peptides. Cyclic peptides often have increased receptor affinity and metabolic stability over their linear counterparts. We carried out virtual screening experiment via docking in order to understand the interaction between HLE-Human Leukocyte Elastase and ligand peptide and to identify the sequence that can be a target in various ligand peptides. We made cyclic peptides as a target base on Metlle-Phe sequence having affinity for ligand and receptor active site docking. There are three ways to cyclize certain sequences of amino acids such as Met-lie-Phe-Gly-Ile. First is head-to-tail cyclization method, linking between N-terminal and C-terminal. Second method utilizes amino acid side chain such as thiol functional group in Cys, making a thioether bond. The last one includes an application of resin-substituted amino acids in solid phase reaction. Among the three methods, solid phase reaction showed the greatest yield. Macrocyclization of Fmoc-Met-Ile-Phe-Gly-Ile-OBn after cleavage of Fmoc protection in solution phase was carried out to give macrocyclic compound 5 in about 7% yield. In the contrast with solution phase reaction, solid phase reaction for macrocyclization of Met-Ile-Phe-Gly-Ile-Asp-Tentagel in normal concentrated condition gave macrocyclic compound 7 in more than 35% yield.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.25 no.1
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• pp.69-88
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• 1999

Several solvent extracts from Alpinia katsumudai were prepared and their various anti-inflammatory activities were evaluated. Alpinia katsumadai extract showed high various anti-inflammatory effects among the 8 medicinal plant extracts, Butanol extract from Alpinia katsumndai showed a potent anti-oxidative and free radical scavenging activities, Free radical scavenging effect of butanol fraction of Alpinia katsumadai($IC_{50}$/ : 50$\mu$g/m$\ell$) was higher than butylated hydroxytoluene($IC_{50}$/ : 50$\mu$g/m$\ell$) and ascorbic acid($IC_{50}$/ : 22$\mu$g/m$\ell$). Alpinia katsumadai butanol fraction exhibited relatively high antioxidative activity($IC_{50}$/ : 335$\mu$g/m$\ell$) compared to ascorbic acid. The inhibitory effect of Alpinia katsumadal ethanol extract on elastase exhibited 10 to 78% at 100 to 1000$\mu$g/m$\ell$ concentration , tile $IC_{50}$/ values with 465.7$\mu$g/m$\ell$ for porcine pancreatic elastase(PPE) and 481.9$\mu$g/m$\ell$ for human leukocyte elastase(HLE), respectively The Alpinta katsumadai extract inhibited effectively hyaluronidase activity($IC_{50}$/ 335$\mu$g/m$\ell$), and showed inhibition in vitro on delayed hypersensitivity when it was topically applied. These results suggest that Alpinia katsumadai extract may reduce inflammatory skin trouble. The Alpinia katsumadai extract also showed higher Inhibitory effect of melanin biosynthesis on cultured melanoma cell compared to arbutin and kojic acid.

• Journal of Yeungnam Medical Science
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• v.19 no.1
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• pp.55-62
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• 2002

Background: Interleukin-1(IL-1) and neutrophil appear to contribute to the pathogenesis of acute respiratory distress syndrome(ARDS). Elastase, as well as reactive oxygen species released from activated neutrophil, are thought to play pivotal roles in the experimental models of acute lung leak. This study investigated whether ICI 200,355, a synthetic elastase inhibitor, can attenuate acute lung injury induced by IL-1 in rats. Materials and Methods: We intratracheally instilled either saline or IL-1 with and without treatment of ICI 200,355 in rats. Lung lavage neutrophils, lung lavage cytokine-induced neutrophil chemoattractant(CINC) concentration, lung lavage protein concentration, lung myeloperoxidase(MPO) activity and lung leak index were measured at 5 hours of intratracheal treatment. Results: In rats given IL-1 intratracheally, lung lavage neutrophils, lung lavage CINC concentration, lung lavage protein concentration, lung MPO activity and lung leak index were higher. Intratracheal ICI 200,355 administration decreased lung lavage neutrophils, lung MFO activity and lung leak index, respectively, but did not decrease lung lavage CINC concentration. Conclusion: These results suggest that ICI 200,355 decreases lung inflammation and leak without decreasing lung lavage CINC concentration in rats given IL-1 intratracheally.