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β-cyclodextrin 및 그 유도체의 포접체 형성에 의한 LG 106W의 유용성 및 안정성 개선에 관한 연구
정성훈 ( Seong-hoon Jeong ),이천구 ( Cheon-koo Lee ),조완구 ( Wan-goo Cho ),강세훈 ( Seh-hoon Kang ) 대한화장품학회 1999 대한화장품학회지 Vol.25 No.1
A newly synthesized polyhydroxy aromatic compound(LG 106W) has good skin lightening effect. Inclusion complexation of LG 106W with β -cyclodextrin and its hydroxypropyl and dimethyl derivatives was studied by the solubility method, scanning electron microscopy and differential thermal analysis. A relationship between host and guest was clearly reflected in the magnitude of the stability constant(DM- β > HP- β >β -cyclodextrin). Formulation problems, which resulted from its very low solubility in aqueous solution, were resolved by the inclusion formation. LG 106W from inclusions is much more water-soluble than pure one. The improvement of pH and temperature stability correlated with the increased solubility was also observed. Inclusion complex of LG 106W had similar activity to pure LG 106W on the inhibition of melanin synthesis in B-16 melanoma cell but showed lower irritation on cultured cell test in vitro. According to the results, cyclodextrins might be one of the reliable candidates for improving the availability of LG 106W.
송영숙 ( Young-sook Song ),정봉열 ( Bong-yul Chung ),조완구 ( Wan-goo Cho ),강세훈 ( Seh-hoon Kang ) 대한화장품학회 2000 대한화장품학회지 Vol.26 No.1
A series of novel ascorbic acid derivatives, polyethoxylated ascorbic acid (PEAA) were synthesized by coupling ascorbic acid with polyethylene glycol (PEG) of two molecular weights (MW: 350 and 550) at the C-2 or C-3 hydroxyl group (2PEAA350, 3PEAA350, 2PEAA550, 3PEAA550) to increase the stability and retain the activity, as a skin whitening agent. Their stability, scavenging activity against free radical, inhibitoiy activity against tyrosinase and inhibitory activity of melanin synthesis in B16 melanoma cell of PEAAs were evaluated in vitro and compared with those of ascorbic acid and 3-O-ethyl ascorbic acid (30EAA), a known stable vitamin C derivative. Among PEAAs, 2PEAA350 and 2PEAA550 liad high scavenging activity against free radical, inhibitoiy activity against tyrosinase and inhibitoiy activity of melanogenesis but low stability. 3PEAA350 had high stability and moderate scavenging activity against free radical, inhibitoiy activity against tyrosinase and inhibitoiy activity of melanogenesis. The stability, scavenging activity against free radical and inhibitoiy activity of melanogenesis of 3PEAA350 were higher than those of 30EAA. The most stable 3PEAA350 among PEAAs was nontoxic in various toxicological tests. These results suggest that PEAA would be a good whitening agent for enhancing stability and bioavailability.
흰쥐 다형핵백혈구의 fMLP로 유도한 유주현상에 대한 신나믹산 유사체의 억제효과
민경락(Kyung Rak Min),김진준(Jin Jun Kim),박선규(Sun Gyoo Park),이정래(Jeong Rai Lee),강세훈(Seh Hoon Kang),김영수(Young Soo Kim) 대한약학회 1998 약학회지 Vol.42 No.2
Inhibitory effects of 16 cinnamic acid analogs on formyl-Met-Leu-Phe(fMLP)-induced chemotaxis of rat polymorphonuclear leukocytes were determined by using a microchemotaxis apparatus. 3,4-Dlhydrocinnamic acid called as caffeic acid exhibited the highest inhibitory effect on the chemotaxis among cinnamic acid analogs tested in this study. Hydroxycinnamic acids exhibited stronger inhibitory effects on the chemotaxis than cinnnamic acid. Hydroxycinnamic acids with one hydroxy group at ortho, meta or para position exhibited similar inhibitory effects on the chemotaxis with corresponding methoxy cinnamic acids, but 3,4-dihydroxycinnamic acid did stronger inhibitory effects than 3,4-dimethoxycinnamic acid. 3,4-Dimethoxycinnamic acid exhibited weaker inhibitory effects on the chemotaxis than 1,2-dimethoxy-4-propenylbenzene and 3,4-dimethoxy cinnamonitrile with -CH=CHCN or -CH=CHCH3, group instead of -CH=CHCOOH group. 4-Hydroxy cinnamic acid and 3,4-dihydroxycinnamic acid exhibited stronger exhibitory effects on the chemotaxis than 3-(4-hydroxyphenyl) propionic acid and 3,4-dihydroxyhydrocinnamic acid with -CH2CH2COOH group instead of -CH=CHCOOH group.
MediminA 를 함유한 O/W 에멀전의 주름 개선 효과
박선규 ( Sun-gyoo Park ),장민열 ( Min-youl Chang ),김영득 ( Young-deuk Kim ),정봉열 ( Bong-youl Chung ),원영호 ( Young-ho Won ),김진준 ( Jin-jun Kim ),강세훈 ( Seh-hoon Kang ) 대한화장품학회 1999 대한화장품학회지 Vol.25 No.1
Medimin A 는 경피 흡수성과 안정 성을 높이 기 위해 retinoic acid 와 poiyethiylene giycol(PEG)를 결합시켜 개발한 비타민 A 유도체이다. Medimin A 의 주름 완화 효과를 확인하기 위하여 콜라겐 합성능 및 임상 평가를 실시하였다. In vitro 콜라겐 합성능은 섬유아세포를 배양하여 생산되는 단백질 중에서, collagenase 에만 특이적으로 분해되는 단백질에 함유된 [3H]-proline 의 양을 측정하여 평가하였으며, 임상 평가는 피부주형(replica)의 영상분석, 주름의 육안적 관찰, 피시험자의 자가판단에 의하여 평가하였다. Medimin A를 섬유아세포에 처리한 결과 10-6% 농도에서 약 40%의 콜라겐 합성 증진을 보였다. Medimin A 가 0.2%함유된 O/W 에멀 젼을 10주간 피시험자에 도포한 결과, 피부 주형에서 가장 깊은 주름이 약 38.4% 가 감소되었으며, 육안적 관찰에 의한 눈가 주름은 25.5% - 44.1%가 감소되었다. 또한 피시험자의 자가 진단에 의하면 전체 피시험자 중 93%가 10주간 도포 후 주름이 호전되었다고 응답하였다. 이상과 같은 결과에서, Medimin A 는 객관적 평가법(invitro 콜라겐 합성능, 피부 주형의 영상분석) 및 주관적 평가법(육안적 관찰, 피시험자의 자가진단)에서 모두 유의하게 주름을 완화시키는 물질임이 확인 되었다. Medimin A is a derivative of vitamin A which has been developed by coupling retinoic acid with polyethylene glycol(PEG) to enhance skin permeability and stability. We carried out the collagen synthesis and clinical test to examine the reducing effect of wrinkles by Medimin In vitro collagen synthesis was evaluated by quantitative assay of [<sup>3</sup>H]-proline incorporation into collagenase sensitive protein in fibroblast cultures. Clinical test was evaluated by image analysis of skin replica, visual observation and self-estimated response of volunteers for 10 weeks. Medimin A stimulated about 40% in collagen synthesis. The area of main deep wrinkle on the skin replica was reduced 38.4% with topical application of O/W emulsion containing 0.2% Medimin A, The wrinkles on the eye region was also reduced 25.4%-44.1% by the visual observation and 93% of all volunteers responded that topical application of the O/W emulsion was showed some reducing effect of wrinkles after 10weeks. From these results, we suggest that Medimin A is a potent anti-wrinkle agent by objective evaluation methods(m vitro collagen synthesis and image analysis of skin replica) and subjective evaluation methods(visual observation and self-estimated response of volunteers).
한국인에서 8 % Homomenthyl Salicylate 로숀의 광원에 따른 광방어지수의 비교
윤재일 ( Jai Il Youn ),김병국 ( Byoung Kook Kim ),서대헌 ( Dae Hun Suh ),오선진 ( Sun Jin Oh ),김진준 ( Jin Jun Kim ),강세훈 ( Seh Hoon Kang ) 대한피부과학회 1996 대한피부과학회지 Vol.34 No.1
Background: The need for using sunscreen is increasing today, but we know little about the effect of sunscreens on the skin of Korean people. Objective : We tried to estimate and compare the SPF of 8% homomenthyl salicylate lotion, which was recommended as the control in SPF experiments by the FDA, USA, in Koreans according to different light sources Methods : After application of 8% homomenthyl salicylate lotion to the back, 33 men of the third decade were irradiated by xenon arc solar simulator or by fluorescent sunlamp, We estimated the SPF of them 24 hours later. Results : The SPF of 8% homomenthyl salicylate lotion was 4.8+0.8 with the solar simulator, 2.7+0.6 with the fluorescent sunlamp. Conclusion : We confimed that the SPF of 8% homomenthyl salicylate lotion with xenon arc solar simulator can be used as a control value in Koreans, and found out that the SPF with the fluorescent sunlamp was significantly lower than that with the xenon arc lamp. So it should be taken into consideration that differences of SPF according to light sources exists in studying sunscreens. (Kor J Dermatol 1996;34(1): 46-51)
한국 청년층의 UVB에 의한 최소홍반량에 따른 광피부형의 분류
윤재일 ( Jai Il Youn ),오준규 ( Jun Gyu Oh ),김병국 ( Byoung Kook Kim ),정진호 ( Jin Ho Chung ),오선진 ( Sun Jin Oh ),김진준 ( Jin Jun Kim ),강세훈 ( Seh Hoon Kang ) 대한피부과학회 1996 대한피부과학회지 Vol.34 No.6
Background: We predicted that t.he self reporting questionnaire proposed by Fitzpatrick might not be appropriate for classifyin~v; the skin phoiotype in Korean people. Objective : We classified the skin phototypes in Korean people by measuring the minimal erythema dose (MED) of UVB on t.he basis of MEDs of skin type proposed by Pathak and Fitzpatrick. Methods : Two hundred and eighty-four male Korean rnedical students participated in this study. We irradiated UVB with Waldmann UV 800 and measured MEDs after 24 hours. Results : The mean MED was 70.1+21.3 mJ/cm2. Most of the MEDs were 70, 60, 50 mJ/cm in the order of frequency. On the basis of the skin type proposed by Pathak and Fitzpatrick, the most frequent phototype was the skin type V(56.3%) by MED. 20.8% and 13.8% of the subjects eorresponded to the skin types UV and III, respectively. 9.1% of the subjects fell into the UV sensitive group, skin type l and II. Conclusion : Using these results as groundwork, simple and precisely applicable classification of skin phototype in Korean people needs to be established. (Kor J Dermatol 1996;34(6): 893-897)
Min, Kyung Rak,Kim, Youngki,Kang, Seh-Hoon,Mar, Woongchon,Lee, Kyong Soon,Ro, Jae Seup,Lee, Seung Ho,Kim, Youngsoo 영남대학교 약품개발연구소 1997 영남대학교 약품개발연구소 연구업적집 Vol.7 No.-
Prostaglandin H₂synthase is the pharmacological target site of nonsteroidal antiinflammatory drugs. Inhibitory effects on cyclooxygenase activity of the synthase by extracts prepared from herbal medicines and wild plants in Korea have been estimated. Sixteen species out of 612 species exhibited more than 50% of inhibition on the enzyme activity. The active extracts prepared from Carex humilis, Celastrus orbiculatus, Eugenia caryophyllata, Gleditsia japonica var. koraiensis, Glycyrrhiza grabra, Glycyrrhiza uralensis, Gyrophora exculenta, lespedeza maximowiczii, Morus alba, Persicaria conspicua, Prunus salicina, Pterocarya stenoptera, Rheum undulatum, Vitis amurensis, and Vitis coignetiae have been sequentially washed with methylene chloride, ethyl acetate, n-butanol. Among the solvent fractions of the active herbal extracts, ethyl acetate fraction of Carex humilis exhibited the highest inhibitory effect on the cyclooxygenase activity of prostaglandin H₂ synthase.
α-Viniferin : A Prostaglandin H₂ Synthase Inhibitor from Root of Carex humilis
Lee, Seung-Ho,Shin, Nam-Ho,Kang, Seh-Hoon,Park, Ji Soo,Chung, See Ryun,Min, Kyung Rak,Kim, Youngsoo 영남대학교 약품개발연구소 1998 영남대학교 약품개발연구소 연구업적집 Vol.8 No.-
An inhibitor on cyclooxygenase activity of prostaglandin H₂ synthase was purified from the root of Carex humilis Leyss (Cyperaceae) by a variety of column chromatographic methods. As a result of the structure analysis by FAB-mass, ¹H-NMR, and ^(13)C-NMR spectral data, the active compound was identified as (+)-α-viniferin, an oligomeric stilbene characterized originally from Corogono chomlogu Lamaeck (Leguminosae). (+)-α-Viniferin exhibited a dose-dependent inhibition on cyclooxygenase activity, where 50% of inhibition (IC_(50)) was shown at a final concentration of about 7 μM. Resveratrol, a putative building block of oligomeric stilbenes, also inhibited the cyclooxygenase activity. The inhibitory potency of (+)-α-viniferin was about 3-to 4-fold stronger than that of resveratrol on cyclooxygenase activity of prostaglandin H₂ synthase partially purified from sheep seminal vesicles.
Min, Kyung Rak,Kim, Youngki,Kang, Seh-Hoon,Mar, Woongchon,Lee, Kyong Soon,Ro, Jai Seup,Lee, Seung Ho,Kim, Youngsoo 영남대학교 약품개발연구소 1996 영남대학교 약품개발연구소 연구업적집 Vol.6 No.-
Prostaglandin H₂ synthase is the pharmacological target site of nonsteroidal antiinflammatory drugs. Inhibitory effects on cyclooxygenase activity of the synthase by extracts prepared from herbal medicines and wild plants in Korea have been estimated. Sixteen species out of 61s species exhibited more than 50% of inhibition on the enzyme activity. The active extracts prepared from Carex humikus, Celastrus orbiculatus, Eugenia caryophyllata, Gleditsia japonica var. koraieosis, Glycyrrhiza grabra, Glycyrrhiza uralensis, Gyrophora exculenta, Lespedeza maximowiczii, Morus alba, Persicaria conspicua, Prunus salicina, Pterocarya stnoptera, Rheum undulatum, Vitis amurensis, and Vitis coignetiae have been sequentially washed with methylene chloride, ethyl acetate, n-butanol. Among the solvent fractions of the active herbal extracts, ethyl acetate fraction of Carex humilis exhibited the highest inhibitory effect on the cyclooxygenase activity of prostaglandin H₂ synthase.