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천연유래물질 펩타이드 유도체의 제조와 멜라닌 생성 저해 효과 탐색
신경훈 ( Kyong-hoon Shin ),이재호 ( Jae Ho Lee ),류근석 ( Geun Seok Ryu ),지경엽 ( Kyung Yup Jee ),박수남 ( Soo Nam Park ),김재일 ( Jae Il Kim ),조인식 ( In Shik Cho ),김한영 ( Han-young Kim ) 대한화장품학회 2010 대한화장품학회지 Vol.36 No.3
신규 미백 소재 개발을 위하여 tyrosinase의 활성을 억제하는 천연물과, alpha-melanocyte stimulating hormone (α-MSH)을 저해하는 펩타이드를 결합한 소재를 고체상 합성법으로 제조하였다[1,2]. Tyrosinase 활성 억제 효능이 있는 천연유래물질을 기존 연구를 바탕으로 선정하였으며, 이중에서 상업화 된 물질 17종에 대해 Mushroom Tyrosinase 활성 억제 효과를 측정하여, 그 중 caffeic acid, coumaric acid를 선별하였다. 펩타이드는 α-MSH 분비를 억제하며, tyrosinase활성을 억제하는 것으로 알려진 melanostatin을 선정하였으며[3-5], PLG-NH<sub>2</sub> (Proline-Leucine-Glycine-NH<sub>2</sub>) 중에서 유도체화 수율의 저하 원인으로 예상되는 Proline (Pro)의 서열을 다른 아미노산으로 변경하면서 선별된 천연물인 coumaric acid와 caffeic acid에 도입하였다. 또한 최종물질의 원가를 고려하여 acid-amide 형태를 acid형태로 전환한 유도체를 합성하였다. 이들 펩타이드 유도체들에 대해서 B16F1 melanoma cell에서의 멜라닌 생성 억제 효능을 평가하여 유도체화된 물질이 기존의 천연유래물질이나 펩타이드에 비하여 높은 저해효과를 가지는 것을 확인하였다. Derivatives of a novel natural compunds, melanostatin (PLG-NH<sub>2</sub>) were prepared by solid phase synthesis [1,2] and assayed to evaluate their melanogensis inhibitory activity. Also, a small library (natural compound- XLG-NH<sub>2</sub>, natural compound-X LG-OH) was prepared with same method for increasing synthetic yield and cost-reduction. PLG-NH<sub>2</sub> (Proline-Leucine-Glycine-NH<sub>2</sub>) was well-known tripeptide as its α-MSH release-inhibiting activity and tyrosinase inhibitory activity[3-5]. In order to choose best candidate for peptide derivatization, various natural compounds were screened by their tyrosinase inhibitory activity. As a result, caffeic acid and coumaric acid were selected. Most of these derivatives showed better activities than the parent natural compound, melanostatin.
김병훈 ( Byung-hoon Kim ),신경훈 ( Kyong-hoon Shin ),조자원 ( Ja-won Cho ),박지현 ( Ji-hyeon Park ) 대한예방치과·구강보건학회 2021 大韓口腔保健學會誌 Vol.45 No.4
Objectives: The study evaluated the effects of dentifrice with the proper amount of ginkgo biloba extract in the prevention of gum disease through clinical trials. Methods: Total sixty volunteers from the experimental group using experimental dentifrice (30 volunteers) and the control group using control dentifrice (30 volunteers) should use the experimental and control dentifrice for 8 weeks. Before the experiment, and 1, 2, 4, 6, and 8 weeks after the experiment, the papillary marginal attached gingival Index (the PMA index), Talbott’s gingival index, patient hygiene performance index (PHP index), and Tureski’s dental plaque index test were tested six times. Results: As a result of the PMA index measurement, the experimental and control groups showed statistically significant differences after 6 weeks, and the experimental group showed a significant decrease in the PMA index from 4 weeks after the experiment. The patient hygiene performance index measurement results showed a statistically significant difference between the experimental group and the control group after 4 weeks, and the experimental group showed a significant decrease in the PHP index 2 weeks after the experiment. Conclusions: The use of ginkgo-leaf-extract-containing-dentifrice confirmed that improved dental plaque removal, gingivitis relief, and periodontal disease prevention could be expected.
cAMP 신호전달과정을 통한 신규 천연유래물질 펩타이드 유도체의 미백 효능 연구
이혜숙 ( Hye Suk Lee ),신경훈 ( Kyong Hoon Shin ),류근석 ( Geun Seok Ryu ),지경엽 ( Kyung Yup Jee ),조인식 ( In Shik Cho ),김한영 ( Han Young Kim ) 대한화장품학회 2011 대한화장품학회지 Vol.37 No.3
MC1R의 길항제 역할을 하는 펩타이드와 tyrosinase를 저해하는 효능을 가지는 천연유래 물질을 유도체화하여 신규 미백소재를 개발하였다. 또한 이러한 새로운 기작에 의한 미백 효능을 평가할 수 있는 방법을 cAMP 신호전달 과정을 활용하여 제시하였다. 총 24종의 유도체를 합성하였고, cAMP assay의 결과를 통해 11종의 유도체를 선별하였으며, 선별된 유도체에 대하여 멜라닌 형성 억제 효능을 평가하여 본 평가 방법의 유효성을 확인하였다. 이 과정에서 RW를 서열에 포함하는 펩타이드 유도체가 특별히 멜라닌 형성 억제 효능이 높은 것을 알 수 있었다. 또한, cAMP assay는 MC1R의 antagonist라는 특정 타겟 물질을 디자인한 소재의 스크리닝 방법에는 활용할 수 있음을 알 수 있었다. 하지만, 미백소재로서의 가능성을 확인하기 위해서는 멜라닌 생성저해 시험과 병행하여야 할 것으로 판단된다. Novel whitening agents were prepared using peptide-Natural origin compound derivatives. The peptide could be an antagonist of MC1R and Natural origin compound were well-known material as a Tyrosinase inhibitor. We also suggest the new assay method which could evaluate the Antagonistic effectiveness to MC1R using cAMP signaling pathway. 24 candidates were synthesized and 11 peptide derivatives were selected by cAMP assay method. To evaluate cAMP assay, the selected peptide derivatives were assayed to evaluate their melanogensis inhibitory activity. At this work, we could know that the sequences which include -RW- have a melanogensis inhibitory activity, and cAMP assy could use as a evaluating method of MC1R antagonist. But, to evaluate the whitening activity of some material, cross-checking with melanin inhibitory assay method was recommended.
덴탈타입실리카, 토코페롤아세테이트, 불화나트륨 및 피로인산나트륨 배합 세치제가 치아표면 탈회 및 치아밀도 감소 억제에 미치는 영향
정호기 ( Ho-ki Jung ),정선영 ( Sun-young Chung ),안용수 ( Yong-su Ahn ),신경훈 ( Kyong-hoon Shin ),조자원 ( Ja-won Cho ) 대한예방치과·구강보건학회 2020 大韓口腔保健學會誌 Vol.44 No.4
Objectives: In this study, we aimed to investigate the preventive and protective effects of new dentifrice containing dental type silica, tocopheryl acetate, fluorides, and sodium pyrophosphate on the mineral density of teeth and demineralization of tooth surfaces. Methods: A total of 119 bovine teeth pre-treated with the new dentifrice at three different concentrations for the experiment were randomly allocated into two control (DW and PW) and one experimental (EC) groups. The enamel surface of all bovine teeth were demineralized using an artificial demineralization solution. The dentifrice was diluted with distilled water (DW) at 1:1, 1:2, and 1:3 ratios. The samples were treated with the demineralization solution for 4 h after treatment with the supernatants of each diluted dentifrice for 30 min, and this procedure was repeated 3 times over a period of 24 h. The samples were examined using micro-CT to determine the amount of reduced bone mineral density (BMD) comparing the control and experimental dentifrices. The surface changes of the samples were also examined using the scanning electron microscope (SEM). Results: The average BMD of the bovine enamel surface between the treated and non-treated area with the dimineralization solution was significantly different in the control, DW, PW 1:1, PW 1:2, and PW 1:3 groups. However, there was no significant difference observed in the experimental groups, including EC 1:1, EC 1:2, and EC 1:3. The average BMD of the dimineralized surfaces based on the results of the 7 groups was significantly higher in every EC group when compared to the DW and three PW groups. Conclusions: The new dentifrice containing dental type silica, tocopheryl acetate, fluorides, and sodium pyrophosphate is effective in inhibiting the decrease in BMD and demineralization of enamel surface, which was observed when the new dentifrice and demineralization solution was repeatedly applied to the samples for 24 h.
치아우식증 유발 세균에 대한 CPC 함유 구강청정제의 항균효과
조원호 ( Won-ho Cho ),조자원 ( Ja-won Cho ),유현준 ( Hyun-jun Yoo ),신경훈 ( Kyong-hoon Shin ),신기해 ( Gi-hae Shin ),전열매 ( Yeol-mae Jeon ),이종천 ( Jong-cheon Lee ) 대한예방치과·구강보건학회 2021 大韓口腔保健學會誌 Vol.45 No.2
Objectives: The purpose of this study was to evaluate and report the antibacterial efficacy in relation to oral disease-causing bacteria using a mouthwash containing 0.05% CPC in an in vitro test. Methods: The sterilization test and susceptibility assay of mouthwash containing 0.05% CPC were investigated against Streptococcus mutans, Streptococcus sobrinus, and Lactobacillus acidophilus; Streptococcus sanguinis as oral bacteria related to dental caries; Enterococcus faecalis as apical periodontitis-related bacteria; and Actinomyces israelii, Aggregatibacter actinomycetemcomitans, Fusobacterium nucleatum, Prevotella intermedia, Prevotella nigrescence, Porphyromonas gingivalis, Tannerella forsythia, Treponema denticola, and Filifactor alocis as periodontal disease-related bacteria. Results: In the sterilization test, most of the bacteria had more than 99.99% sterilizing power for all samples but compared to other bacteria, the sterilizing power of these samples was not successful for L. acidophilus and E. faecalis bacteria. When comparing the sterilization power between the samples, sample 3 (0.05% CPC+20% ethanol) was the strongest. Conclusions: In the antimicrobial activity test, sample 3 inhibited growth at the lowest concentration overall.