• Biomolecules & Therapeutics
• /
• 제5권1호
• /
• pp.74-81
• /
• 1997

DA-5018(N-(3-(3, 4-dimethylphenyl)propyl)-4-(2-aminoethoxy)-3-methoxyphenylacetamide) is a new capsaicin derivative under development as topical analgesic agent. The general pharmacological properties of DA-5018 on central nervous, cardiovascular, gastrointestinal and other organ systems were studied in experimental animals. DA-5018 cream (0.3%) had no effects on behavior, hexobarbital-induced sleeping time, body temperature, spontaneous activity, blood pressure, heart rate, intestinal charcoal propulsion, urine volume and electrolyte excretion even at a high dose of 2000 mg/kg in rats. In addition, DA-5Ol8 cream had little skin irritation compared to Zostrix-HP (capsaicin, 0.075%) cream in rabbits. In isolated guinea pig tissue studies, DA-5018 increased the contractility of trachea and ileum and also increased sinus rate of atrium in a range of 10^{-8}-10^{-5}$$ M, but its efficacy as a agonist was weak. These results suggest that DA-5018 cream might be used topically without serious side effects.

• 대한약학회:학술대회논문집
• /
• 대한약학회 2000년도 춘계총회 및 학술대회
• /
• pp.129.3-130
• /
• 2000

• 한국독성학회:학술대회논문집
• /
• 한국독성학회 2001년도 International Symposium on Dietary and Medicinal Antimutgens and Anticarcinogens
• /
• pp.194-194
• /
• 2001

Preclinical test methods for allergenic potential chemicals has been widely used to assess human risks and has been developed. Recently, the murine local lymph node assay (LLNA) has been proposed as a prospective method to identify contact allergens and to replace conventional the guinea pig maximization test (GPMT). The objective of this study was to establish LLNA and to evaluate allergenicity of chemicals by LLNA. (omitted)

• 대한화장품학회지
• /
• 제23권3호
• /
• pp.134-146
• /
• 1997

Consumers have recently preferred to purchase extensive UV intercepting products, which are waterproof and free from side effects on skin. Testing Cytoroxicity in SR method, cell survivial ratio of UV-B interceptors decreased above 0.08W/V%, and so did that of UV-A interceptors above 0.06W/V%. Also, Patch-test of inorganic UV interceptors resulted in no skin irritation even below 10.0 and 11.25. UV interceptors in the sunlight showed yellowish discoloration in 5 to 14 days. In absorption curves, UV-B was most suitable for Octyl methoxycinnamate and UV-A for Butyl methoxy dibenzoylmethane. Fro this reason, Nylonpoly UVA/UVB the material of OMC and BMDM coated with Nylon & polyethylene, was used as the organic UV interceptor. And zinc oxide and titanium dioxide was used as inorganic UV ibterceptors. The appropriate mixture ratio of ZnO and TiO2 was 6 to 4.6% of ZnO, 4% of TiO2 and 5% of Nylonpoly UVA/UVB were all combined with our sunscreen cream. The SPF value of in-vivo applied to a guinea pig was 34.9 and that of in-vivo was 38.5. Cyclomerhicone and dimerthicone were used in water-in-Silicone system. Ceryl diverhicone and sorbitan sesquioleate were used as emulsifiers and MgSO4, 7H2O, Mg-stearate/Mg-Al-stearate copolymer as emulsification stabilizers. In practical application, each SPF duration of O/W type and W/S type containing sunscreen cream of the same content showed that W/S type of sunscreen cream was 5 times as durable as the other. This product is fit for using in swimming, climbing or skiing. This research is to minimize skin trouble used by UV interceptors and to make one with proper softness, skin safety and UV intercepting efficiency.

• 대한화장품학회지
• /
• 제27권1호
• /
• pp.119-131
• /
• 2001

Exposure of the human skin to UV-light can cause sun-tanning, photoaging and even photo-carcinogenesis. Melanin is important in protecting the skin against UV damage, but excessive or uneven melanin production can lead to the formation of freckles and aged spot. Control of hyperpigmentation is becoming even more important as aged population continues to grow. These needs led us to develop effective and safe depigmenting-agent, kojyl 3-aminopropyl phosphate (kojyl-APPA), called Whitegen. The development of whitegen was based on the fact that phosphate group of 3-aminopropyl phosphate can make kojic acid more compatible to the skin membrane and more stable. Instability of kojic acid has been a problem in cosmetic use. The insertion of phosphoester group has been recognized as a powerful tool to improve such physical properties as solubility and stability, because the phosphodiester residue is well characterized as a non-toxic moiety, having a high affinity for cell membranes. Kojyl-APPA showed no tyrosinase inhibition effect compared to kojic acid in vitro, but showed tyrosinase inhibition effect in situ. It means that kojyl-APPA is converted to kojic acid enzymatically in cells. Kojyl-APPA showed the inhibitory activity on melanin synthesis in mouse melanoma and normal humal melnaocytes and also showed long-lasting stability in comparison with its original form (kojic acid). Kojyl-APPA showed depigmenting effects when applied to UVB-induced hyperpigmentated region of guinea pig skin. Based on these results, kojyl 3-aminopropyl phosphate can be used as a safe and effective ingredient for the brightness and cleanness of skin.

• 대한화장품학회지
• /
• 제33권1호
• /
• pp.1-6
• /
• 2007

일반적으로 cyclodextrin (CD)은 liposome의 구조를 불안정하게 만드는 것으로 알려져 있다. 본 연구에서는 양친매성 고분자전해질을 리포좀에 도입하여 CD에 대한 리포좀의 안정도를 증진시키는 연구를 수행하였다. Transmission electron microscopy와 photocorrelation spectroscopy 결과들로부터 ${\beta}-CD$ (${\beta}CD$)와 hydroxypropyl-${\beta}CD$ ($HP{\beta}CD$)를 함유하는 리포좀에 고분자가 도입되었을 때 CD를 함유하는 phosphatidylcholine (PC)-cholesterol (Chol) 리포좀보다 우수한 구조적 안정성을 나타내었다. 또한, rhaponticin (Rh)을 $HP{\beta}CD$에 포접시키고 이를 함유하는 PC-Chol 리포좀과 고분자가 도입된 리포좀의 안정도를 비교해 보았을 경우도 마찬가지로 고분자가 도입된 리포좀이 월등히 향상된 구조적인 안정성을 나타내는 것을 확인하였다. 이와 더불어 guinea pig의 피부조직을 사용하고 franz-cell을 통한 in vitro 피부흡수실험을 수행한 결과, $HP{\beta}CD$에 의해 가용화된 Rh의 피부흡수가 고분자가 도입된 리포좀에 의해 증진됨을 확인할 수 있었다. 상기 결과들은 양친매성 고분자 전해질의 도입에 따라 CD에 의해 가용화된 특정한 활성성분을 함유하는 리포좀의 구조적인 안정성을 효과적으로 증진시킬 수 있음을 확인시켜 주었으며, 이렇게 향상된 리포좀의 구조적인 안정성을 통해 약물전달시스템 측면에서 많은 응용이 가능할 것으로 생각된다.

• Toxicological Research
• /
• 제18권2호
• /
• pp.175-181
• /
• 2002

Allergic contact dermatitis (skin sensitization) may be caused by a wide variety of chemicals. A murine local lymph node assay (LLNA) has been developed as an alternative to guinea pig models for assessing the contact sensitization potential of chemical. This study was carried out to evaluate the skin sensitization potential for chemicals in Balb/c mice by LLNA. Contact allergen, dinitrochlorobenzene (DNCB), respiratory allergen, toluene diisocyanate (TDI) and a weak allergen, $\alpha$-hexlycinnamaldehyde (HCA) were wed as positive chemicals and irritant, sodium lauryl sulfate(SLS) also wed as a reference chemical in this study. The weights of lymph node in the mice treated with DNCB, TDI, and HCA were increased compared to vehicle control. There was a significant increase in lymph node weight of mice treated with high concentration of SLS compared to vehicle control. The stimulation index (SI) of Lymph node cell in the mice treated with DNCB, TDI, and HCA revealed over three-fold increase compared to vehicle control by $3^H$-thymidine uptake. All allergens correctly identified in this LLNA study wing Balb/c mice. These results suggest that LLNA wing Balb/c mice could be a useful method for screening the allergenic potential of chemicals. The expression of IL-2 mRNA was slightly increased in draining auricular lymph node cell of the mice treated with TDI and HCA by RT-PCR. However the IL-2 levels in DNCB and SLS of treated animals were not significantly changed.

• 대한화장품학회지
• /
• 제25권4호
• /
• pp.1-5
• /
• 1999

The purpose of this study was to determine the effect of IPBC(3-lodo-2-propynylbutylcarbamate) on dandruff caused by the anthropophilic fungus Malassezia furfur. The effects of IPBC on dandruff were examined by evaluating (a) the MIC value of IPBC using broth dilution method; (b) the remnant antimicrobial activity of IPBC containing shampoo on skin disc; (c) the antidandruff efficacy of 1.0 % IPBC containing shampoo in double blind clinical trial. To investigate the remnant antimicrobial activity of IPBC against Malassezia furfur, guinea pig-skin disc was washed with antidandruff shampoo and then the diameter of inhibition zone per disc was measured. For clinical trial, thirty healthy volunteers, aged 25-35, participated in 4 week study. At 0, 2, 4 weeks, examinations of scaling, itching on scalp were carried out. The MIC(Minimun Inhibition Concentration) values of IPBC range from 0.10 to 1.00${\mu}g/ml$ and it seems that IPBC is more effective in the MIC values than zinc pyrithione, selenium disulphide, piroctone olamine and comparable to ketoconazole, climbazole. When the remnant antimicrobial activity of IPBC shampoo on skin disc was determined, 0.5% IPBC shampoo and 2.0% Ketoconazole shampoo resulted in similar antimicrobial effect. In addition, 1.0%, 2.0% IPBC shampoo was more effective than 2.0% ketoconazole shampoo. After two and four-weeks of 1.0% IPBC shampoo treatment, there was significant reduction of scaling, itching in test group compared to control group. On the basis of these results, it can be concluded that 1.0% IPBC is more effective than 2.0% Ketoconazole in reducing dandruff. It seems that strong capacity of drug binding to the stratum corneum plays a role in its antidandruff effect since adsorption of active ingredients on scalp is very important factor in reducing dandruff.

• 대한화장품학회:학술대회논문집
• /
• 대한화장품학회 1999년도 IFSCC . ASCS 학술대회 발표 논문
• /
• pp.1-5
• /
• 1999

The purpose of this study was to determine the effect of IPBC(3-lodo-2-propynylbutyl carbamate) on dandruff caused by the anthropophilic fungus Maiassezia furfur. The effects of IPBC on dandruff were examined by evaluating (a) the MIC value of IPBC using broth dilution method : (b) the remnant antimicrobial activity of IPBC containing shampoo on skin disc ; (c) the antidandruff efficacy of 1.0 % IPBC containing shampoo in double blind clinical trial. To investigate the remnant antimicrobial activity of IPBC against Maiassezia furfur, guinea pig-skin disc was washed with antidandruff shampoo and then the diameter of inhibition zone per disc was measured. For clinical trial, thirty healthy volunteers, aged 25-35, participated in 4 week study. At 0,2,4 weeks, examinations of scaling, itching on scalp were carried out. The MIC(Minimun Inhibition Concentration) values of IPBC range from 0.10 to 1.00$\mu$ g/ml and it seems that IPBC is more effective in the MIC values than zinc pyrithione, selenium disulphide, piroctone olamine and comparable to ketoconazole, climbazole. When the rimnant antimicrobial activity of IPBC shampoo on skin disc was determined, 0.5% IPBC shampoo and 2.0% Ketoconazole shampoo resulted in similar antimicrobial effect. In addition, 1.0%,2.0% IPBC shampoo was more effective than 2.0% ketoconazole shampoo. After two and four-weeks of 1.0% IPBC shampoo treatment, there was significant reduction of scaling, itching in test group compared to control group. On the basis of these results, it can be concluded that 1.0% IPBC is more effective than 2.0% Ketoconazole in reducing dandruff. It seems that strong capacity of drug binding to the stratum corneum plays a role in its antidandruff effect since adsorption of active ingredients on scalp is very important factor in reducing dandruff.

• Journal of Photoscience
• /
• 제2권1호
• /
• pp.37-45
• /
• 1995

INTRODUCTION : Psoralens are planar tricyclic furocoumarins present in numerous plants and fungi found throughout the world.' Naturally occurring and synthesized psoralen derivatives(see Figure 1) are photosensitizers of UVA especially from 320 nm to 400 nm, a range at which cellular nucleic acids and proteins are weakly absorbing if any at all. Because of their skinphotosensitizing properties, these compounds have been used in the photochemotherapy of psoriasis and vitiligo. However, undesirable side effects such as carcinoma development in hairless mice as well as possible liver damage from the use of 8-methoxypsoralen(8-MOP) have been reported. The other photobiological effects include inactivation of DNA viruses, killing and mutagenesis of bacteria, inhibition of tumor transmitting capacity of various cells, and hyperpigmentation on human and guinea pig skin. PUVA(psoralen+UVA) photochemotherapy is in fact thousands of years old, having been used in Egypt and India since B.C. 1200-2000. Photochemotherapy for a common disfiguring disease, vitiligo, was practiced in the ancient world by physicians and herbalists who used boiled extracts of the fruits of certain umbelliferous plants, e.g. Ammi majus Linnaeus in Egypt or the leguminous plants, Psoralea corylifolia L. in India. It was first described by Kuske in 19388 that photosensitization of skin by plants was related to the presence of psoralen. He identified natural psoralens in plants as photosensitizers and isolated bergapten(5methoxypsoralen) from the oil of bergamot. The scientific interest in photosensitizing psoralens, however, has grown considerably after the introduction into clinics of the psoralen photochemotherapy for the treatment of psoriasis and of other skin (abbreviation)