1. 천연물 분획 library 및 화합물 library 제작 및 활용 : 천연물과 화합물을 PPAR 조절제 검색에 적합한 96-well plate 형태로 제작 후 활용. 2. PPARgamma antagonist 발굴 및 원료화 연구 : 검색을 위한 FRET법과 루시퍼래이즈법을 확립하고, 스크리닝 실시하여, 1차 후보 선정. 1차 후보물질을 대상으로 지방세포 분화 저해 활성을 평가하여, 천연물 1종과 화합물 1종을 선정. 선정된 천연물은 유효성분을 규명하고, 원료화 연구를 실시하여 최종 후보 2종을 도출 후 공정연
1. 천연물 분획 library 및 화합물 library 제작 및 활용 : 천연물과 화합물을 PPAR 조절제 검색에 적합한 96-well plate 형태로 제작 후 활용. 2. PPARgamma antagonist 발굴 및 원료화 연구 : 검색을 위한 FRET법과 루시퍼래이즈법을 확립하고, 스크리닝 실시하여, 1차 후보 선정. 1차 후보물질을 대상으로 지방세포 분화 저해 활성을 평가하여, 천연물 1종과 화합물 1종을 선정. 선정된 천연물은 유효성분을 규명하고, 원료화 연구를 실시하여 최종 후보 2종을 도출 후 공정연구 완료. 화합물 1종에 대해서는 원료화 연구 진행중. 3. PPARs agonist 발굴 및 원료화 연구 : 검색을 위한 ELISA법과 루시퍼래이즈법을 확립하고, 스크리닝 실시하여, PPARalpha agonist 천연물 3종과 화합물 3종, PPARgamma agonist 천연물 2종과 화합물 2종을 1차 선정. 1차 후보를 대상으로 각질세포 분화에 대한 활성 평가. 천초목의 경우, 1,3-BG 추출물의 적용 용이성을 고려해 추출상태로 효능 연구를 실시하여 항염 및 장벽생성 촉진을 확인하고 원료화 연구 실시하여 원료화 후보로 도출함. 천선자의 경우 분획을 통한 성분 연구로 유효물질 규명 후, 원료화 연구 진행중
Abstract▼
I. Aims of development : Due to extension of concept of cosmetics field, development of cosmeceuticals with physiological effects is very active and the consumers` needs for cosmeceuticals targeting slimming, acne or atopic dermatitis are increasing now. Therefore, development of newly functional
I. Aims of development : Due to extension of concept of cosmetics field, development of cosmeceuticals with physiological effects is very active and the consumers` needs for cosmeceuticals targeting slimming, acne or atopic dermatitis are increasing now. Therefore, development of newly functional materials helpful for skin is urgent in cosmetics market to strength the competitiveness. PPARs are known that they have major role in formation of subcutaneous fat or skin homeostasis. However, there is few available cosmetics materials regulate PPAR. Therefore, development of exclusive and new cosmetics materials can be possible through the development of PPAR regulators. II. Contents and Scopes 1. Development of PPARgamma antagonist as slimming materials : PPARgamma is a key regulator in differentiation of preadipocytes into adipocytes in white fat tissue and known that it regulates lipogensis in subcutaneous fat tissue. Therefore, PPARgamma antagonist is different from other slimming materials which increase lipolysis or prevent fat deposition in adipocytes and also can make synergy with them. Thus, we intend to develop PPARgamma antagonist as a simming agent through establishing screening methods, screening candidates from natural and chemical library, evaluating the selected candidates and then developing them as cosmetics materials. 2. Development of PPAR agonist as skin barrier recovery materials : PPARs which are activated by their own agonists accelerate keratinocyte differentiaion, show anti-inflammation effects and function in regulating skin homeostasis. Therefore, development of PPARs agonist can make very effective and exclusive materials which are different from other products for symptom relief or barrier supplement. Thus, we intend to develop PPARs agonist as skin barrier recovery materials through establishing screening methods, screening candidates from natural and chemical library, evaluating the selected candidates and then developing them as cosmetics materials. III. Results 1. Establishment of natural library(2000 samples) and chemical library(400 samples) as 96 well plate form for screening 2. Development of PPARgamma antagonist and study of materialization : Establishment of FRET and luciferase assay, screening and selection of the first candidates. Selection of one natural candidate and one chemical candidate by test of its anti-adipogenetic effect. Purification and identification of active ingredient from the natural candidate by activity-guided fractionation. Final selection of two natural extract-derived ingredients as cosmetic materials by materialization study and study of process. 3. Development of PPAR agonist and study of materialization : Establishment of ELISA and luciferase assay, screening and selection of the first candidates. Selection of 3 natural candidates and 3 chemical candidates as a PPARalpha agonist, and 2 natural candidates and 2 chemical candidates as a PPARgamma agonist by test of its pro-differentiation effect. IV. Plans of application 1. Launching of slimming cosmetics which contain tanshinone derivatives which have PPARgamma antagonist activity. 2. Development of anti-acne proudcts using tanshinone derivatives which have PPARgamma antagonist activity. 3. Launching of cosmetics for skin barrier recovery using Zanthoxylum bungeanum extract, a PPARalpha agonist.
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