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Many Brassica species require vernalization (long-term winter-like cooling) for transition to the reproductive stage. In the past several decades, scientific efforts have been made to discern the molecular mechanisms underlying vernalization in many species. Thus, to identify the key regulators required for vernalization in Brassica rapa L., we constructed a linkage map composed of 7,833 single nucleotide polymorphism (SNP) markers using the late-flowering Chinese cabbage (B. rapa L. ssp. pekinensis) inbred line ‘Chiifu’ and the early-flowering yellow sarson (B. rapa L. ssp. trilocularis (Roxb.)) line ‘LP08’ and identified a single major QTL on the upper-arm of the chromosome A02. In addition, we compared the transcriptomes of the lines ‘Chiifu’ and ‘LP08’ at five vernalization time points, including both non-vernalized and post-vernalization conditions. We observed that BrFLC2 was significantly downregulated in the early flowering ‘LP08’ and had two deletion sites around the BrFLC2 genomic region compared with the BrFLC2 genomic region in ‘Chiifu.’ In the present study, we also demonstrate that early flowering in ‘LP08’ line is attributed to the low expression of BrFLC2, which is caused by nonsense-mediated mRNA decay (NMD). Therefore, this study provides a better understanding of the molecular mechanisms underlying floral transition in B. rapa.One sentence summaryNMD-mediated degradation of BrFLC2 mRNA transcripts is the main cause of rapid flowering of oilseed-type B. rapa ‘LP08’ plants.

The fastest aging society with the lowest fertility rate can be buffered by support for healthy pregnancies using sociocultural approaches. We aimed to address adult perceptions of a healthy pregnancy and explored their needs and concerns about childbirth across the lifespan. We conducted a qualitative study using content analysis to investigate general perceptions of a healthy pregnancy after focus-group interviews with adult men and women. We interviewed 60 participants in nine group sessions of 5 to 8 people per group. Three major themes emerged that affect healthy pregnancies: Taking responsibility for a prepared pregnancy, factors that interfere with a healthy pregnancy, and improving strategies for a healthy pregnancy. For the first theme, the two main concerns were financial and parenthood preparation. Factors interfering with a healthy pregnancy had direct and indirect causes, considering personal, social, and cultural changes. Strategies for a healthy pregnancy included family and workplace support, systematic education, and governmental support for financial preparation and health screening. Participants averred that various kinds of support (financial, healthcare, and career) are needed for a healthy pregnancy and childbirth. This public awareness could promote better decisions toward healthy pregnancy with more sociocultural approaches in the various settings of home, school, and the workplace.

To determine the degree to which nurses are aware of cervical cancer and to describe nurses' experiences of caring for patients with cervical cancer. To promote quality of nursing care of cervical cancer, we need to explore their perceptions and nursing experience in doing cervical-cancer care. This study was a qualitative descriptive design. Interviews were conducted with 14 registered nurses. The interviews were audiotaped, transcribed and analyzed. Content analysis was performed. Fourteen nurses who had been working at wards and cancer education centers were recruited in this study. Nine key themes emerged from three categories such as nurses’ awareness of cervical cancer, awareness of cervical cancer patient and caring experience. Nurses expressed fear of cervical cancer and helplessness in the face of a life-threatening prognosis. Nurses stated that they might have prejudice about cervical cancer, since it is caused by a sexually transmitted disease. They also recalled that patients with cervical cancer were more sensitive and demanding. Our findings provide a comprehensive and in-depth perspective in understanding the experience of caring for cervical cancer patients. Clinical nurses showed complex emotional reactions to cervical cancer, and expressed prejudice against the sex life of cervical-cancer patients. More education is required to ensure that clinical nurses can provide a nurse-led intervention with patients by managing nurses’ fear, prejudice, and the care burden.

Backgrounds As HPV is a sexually transmitted virus, men are crucial in the prevention of cervical cancer, but research about men’s awareness on cervical cancer is limited. Therefore, in this study, we investigated men’s awareness toward women’s cervical cancer, to thoroughly understand the viewpoints of men, and to emphasize the centrality of the role of men in the prevention of cervical cancer. Methods A qualitative descriptive design was chosen to explore men’s awareness of women’s cervical cancer. Twelve men aged 20–58 were interviewed. Snowball sampling was conducted to recruit participants. Results Most participants stated that they were not interested in women’s health, and that they did not have much knowledge about cause and prevention of cervical cancer. They acknowledged that cervical cancer was different from other cancers, based on cause and prognosis of disease. The recognition of cervical cancer in participants varied widely depending on their relationship with women. Respondents’ recognition of cervical cancer was classified into four types based on a Situational Awareness (SA) model including individual factors (knowledge about cervical cancer, interest in women’s health) and system/task factors (relationship with women, men’s responsibility). Conclusion This study is one of the few studies describing men’s awareness on cervical cancer. Korean men’s awareness level was low, and their concern and knowledge were not good. Some participants thought that cervical cancer can be treated, can be prevented, and is recognized as a disease of a female with men intervening. Our participants perceived that the role of men is necessary for the prevention of cervical cancer. Therefore, a strategy is needed to develop the awareness and knowledge of men on cervical cancer prevention. When planning cervical cancer education for men, phase and type-specific approaches are required, depending on perception level.

Using enrichment culture, Sphingobacterium multivorum GIN723 (KCCM80060) was isolated as having activity for deglycosylation of compound K and ginsenoside F1 to produce ginsenoside aglycons such as S-protopanaxadiol (PPD(S)) and S-protopanaxatriol (PPT(S)). Through BLAST search, purified enzyme from S. multivorum GIN723 was revealed to be the outer membrane protein. The purified enzyme from S. multivorum GIN723 has unique specificity for the glucose moiety. However, it has activity with PPD and PPT group ginsenosides such as ginsenosides Rb1, Rb2, Rb3, Rc, F2, CK, Rh2, Re, and F1. From these results, it was predicted that the enzyme has activity on several ginsenosides. Therefore, the biotransformation pathway from Rb1, which is a major, highly glycosylated compound of ginseng, was analyzed using high-performance liquid chromatography and electrospray ionization mass spectrometry/mass spectrometry. The dominant biotransformation pathway from Rb1 to PPD(S) was determined to be Rb1 → Gp-XVII → Gp-LXXV → CK → PPD(S). S. multivorum GIN723 can be used as a whole cell biocatalyst because its activity as whole cells is nine times higher than its activity as cell extracts. The specific activity of whole cells is 2.89 nmol/mg/min in the production of PPD(S). On the other hand, the specific activity of cell extracts is 0.32 nmol/mg/min. The productivity of this enzyme in whole cell form is 500 mg/1 l of cultured cell. Its optimum reaction condition is 10 mM of calcium ions added to a phosphate buffer with a pH of 8.5.

Nocardia pseudobrasiliensis is predominantly associated with invasive infections in immunocompromised patients. We report a case of disseminated mycetoma caused by N. pseudobrasiliensis in a 57-yr-old woman with microscopic polyangiitis, who was treated for 3 months with corticosteroids. The same organism was isolated from mycetoma cultures on the patient's scalp, right arm, and right leg. The phenotypic characteristics of the isolate were consistent with both Nocardia brasiliensis and N. pseudobrasiliensis, i.e., catalase and urease positivity, hydrolysis of esculin, gelatin, casein, hypoxanthine, and tyrosine, but no hydrolysis of xanthine. The isolate was identified as N. pseudobrasiliensis based on 16S rRNA and hsp65 gene sequencing. The patient was treated for 5 days with intravenous ampicillin/sulbactam, at which time both the mycetomas and fever had subsided and discharged on amoxicillin/clavulanate. This case highlights a very rare presentation of mainly cutaneous mycetoma caused by N. pseudobrasiliensis. This is the first reported case of N. pseudobrasiliensis infection in Korea.

Objective To explore and understand how patients with knee osteoarthritis (OA) experience moxibustion. Method This qualitative research was conducted as part of a larger clinical trial of the effectiveness of moxibustion for the treatment of knee OA by qualitative content analysis. Sixteen patients with mild knee OA who participated in a 12-week moxibustion treatment as part of the trial were interviewed using open-ended questions. Results The participants recognised knee OA as a normal ageing process that caused physical and emotional discomfort in daily life. Regardless of any adverse effects of moxibustion, most of the participants were interested in continuous moxibustion treatment as a long-term management strategy and for general health. Conclusions This study suggests that moxibustion can be helpful in managing symptoms related to knee OA. Patients’ attitudes towards moxibustion can affect the treatment result and those who prefer it want to continue the treatment for a long time because they understand that knee OA is a chronic condition which needs continuous care. However, practitioners need to pay more attention to those who are very enthusiastic because they tend to endure treatment-related adverse events in their desire for better effects.

Purpose: The purpose of this study was to develop a Simulation-based Integrated Clinical Practice Program (SICPP) for nursing students and to identify the effect of this program. Methods: A non-equivalent pre-post test of quasi-experimental design was used. One hundred thirty-one nursing students participated in the study with 69 in the experimental group and 62 in the control group. We developed a SICPP taking 3 hours per session, once per week for 10 weeks. Data were analyzed using the SPSS 19.0 program with descriptive statistics, -test, independent t-test. Results: There were significant increases in nursing clinical competence (t

Atopic dermatitis (AD) is a chronic and relapsing inflammatory skin disease affecting > 10% of children and 1-3% of adults, and can cause significant morbidity. The incidence of AD seems to be increasing. Omalizumab, a monoclonal antibody, has recently been suggested as a potential new systemic treatment for patients with recalcitrant AD with elevated IgE levels, based on its efficacy in treating asthma and allergic rhinitis. We report a study of 10 patients with AD (aged 19-35 years) who received anti-IgE treatment for persistent asthma. All patients, regardless of IgE value, were treated with a fixed schedule of eight cycles of omalizumab 300 mg administered subcutaneously at intervals of 2 weeks. Eczema symptoms were scored at baseline and after 2, 4 and 6 months of treatment. There was a steady improvement in the objective SCORAD (SCORing Atopic Dermatitis), with significantly lower scores observed at the 6-month evaluation. At 2 months after the end of treatment, two patients had a very good result (SCORAD reduction of > 50%), five patients had a satisfactory result (reduction of 25-50%), and three patients had no clinically relevant result (reduction of 25-50%). No patient had worsening of the AD (increase of > 25% in SCORAD), and once a clinical improvement occurred, none of the patients experienced worsening of their eczema symptoms while on omalizumab. With the caveats of the financial expense and unknown long-term risks of malignancy associated with omalizumab, this drug should be considered for treatment-resistant patients with AD, particularly patients with high IgE level whose symptoms are not controlled by routine therapies. Omalizumab has proven useful in treating asthma, but it may also prove valuable for other conditions, such as allergic rhinitis, food allergies, chronic urticaria, and AD, as shown by the present study.

To assess the current level of acceptance in the United States of complementary and alternative medicine, recent research into the prevalence, acceptance, accessibility, and recognition of complementary and alternative therapies were reviewed. Several signs point to an increasing acceptance of complementary and alternative medicine in the United States; the use of complementary and alternative medicine is significantly increasing, many aspects of Chinese medicine and Ayurveda are becoming mainstream, practitioners in the United States are beginning to be licensed, and insurance companies are beginning to cover some complementary and alternative therapies. Remaining challenges to true acceptance include the restrictive Western mindset, the absence of published studies, a lack of consistent manufacturing processes and quality standards, and a fear of adulteration. Although the field still faces many challenges, alternative and complementary medicine, including Chinese medicine and Ayurvedic medicine, is becoming more accepted and accessible in the United States.

Astragalin (kaempferol-3-O-β-D-glucopyranoside, Ast) glucosides were synthesized by the acceptor reaction of a dextransucrase produced by Leuconostoc mesenteroides B-512FMCM with astragalin and sucrose. Each glucoside was purified and their structures were assigned as kaempferol-3-O-β-D-glucopyranosyl-(1→3)-O-α-D-glucopyranoside (or kaempferol-3-O-β-D-nigeroside, Ast-G1') and kaempferol-3-O-β-D-glucopyranosyl-(1→6)-O-α-D-glucopyranoside (or kaempferol-3-O-β-D-isomaltoside, Ast-G1) for one glucose transferred, and kaempferol-3-O-β-D-isomaltooligosacharide (Ast-IMO or Ast-Gn; n=2-8). The astragalin glucosides exhibited 8.3-60.6% higher inhibitory effects on matrix metalloproteinase-1 expression, 18.8-20.3% increased antioxidant effects, and 3.8-18.8% increased inhibition activity of melanin synthesis compared to control (without the addition of compound), depending on the number of glucosyl residues linked to astragalin. These novel compounds could be used to further expand the industrial applications of astragalin glucosides, in particular in the cosmetics industry.

Using enrichment culture, Rhizobium sp. strain GIN611 was isolated as having activity for deglycosylation of a ginsenoside, compound K (CK). The purified heterodimeric protein complex from Rhizobium sp. GIN611 consisted of two subunits with molecular masses of 63.5 kDa and 17.5 kDa. In the genome, the coding sequence for the small subunit was located right after the sequence for the large subunit, with one nucleotide overlapping. The large subunit showed CK oxidation activity, and the deglycosylation of compound K was performed via oxidation of ginsenoside glucose by glycoside oxidoreductase. Coexpression of the small subunit helped soluble expression of the large subunit in recombinant Escherichia coli . The purified large subunit also showed oxidation activity against other ginsenoside compounds, such as Rb1, Rb2, Rb3, Rc, F2, CK, Rh2, Re, F1, and the isoflavone daidzin, but at a much lower rate. When oxidized CK was extracted and incubated in phosphate buffer with or without enzyme, ( S )-protopanaxadiol [PPD(S)] was detected in both cases, which suggests that deglycosylation of oxidized glucose is spontaneous.

The medicinal herb Oldenlandia diffusa is known as a folk medicine for the treatment of hepatitis, sore throat, appendicitis, malignant tumors and urethral infection in Southern China and Korea. Another species O. corymbosa, is also used for the therapy of the similar conditions, however, only O. diffusa is referred to the medicinal herb by Chinese Pharmacopoeia. Due to their similar morphology, O. diffusa and O. corymbosa are often misidentified. To easily identify O. diffusa from O. corymbosa, the phylogenetic utility of nuclear ribosomal DNA (nrDNA) internal transcribed spacers (ITS) were investigated among different O. diffusa and O. corymbosa populations in Korea. The nrDNA ITS sequence of O. diffusa contained 791 bp, with GenBank accession number of JF837601-JF837602. The nrDNA ITS sequence of O. corymbosa was 785-786 bp, with GenBank accession number of JF837603-JF837611. The results showed that there are some certain divergences in the ITS region sequence between both species, even among different populations of the same species. Particularly, O. corymbosa ST-4 population showed the highest dissimilarity of the ITS region sequence with other nine populations of O. corymbosa and two populations of O. diffusa. This consequence makes us further understand the molecular diversification between O. corymbosa and O. diffusa, and help to promote the correct use and safety.

In this study we investigated the inhibitory effects and possible mechanisms of action of 8'-hydroxydaidzein and 3'-hydroxydaidzein, two ortho-dihydroxyisoflavone derivatives from Korean fermented soybean paste, on melanogenesis in B16 murine melanoma cells. The two hydroxydaidzeins reduced melanin synthesis comparably to treatment with kojic acid, a proven whitening agent, in B16 melanoma cells. Furthermore, when in vitro human skin equivalents were treated with the hydroxydaidzeins, the levels of melanogenesis were significantly reduced relative to a kojic acid control. The RT-PCR results demonstrated that depigmentation was due to transcriptional repression of several melanogenesis genes, including microphthalmia-associated transcription factor (MITF), by the hydroxydaidzeins. The immunoblotting results confirmed that diminution of MITF expression subsequently decreased expression of tyrosinase, and tyrosinase-related proteins 1 and 2. Cumulatively, these results suggest that hydroxydaidzeins would be potent attenuators of melanin synthesis as well as effective inhibitors of hyperpigmentation in human skin. Copyright © 2011 John Wiley & Sons, Ltd.

Ginsenoside (G)-F1 is an enzymatic metabolite generated from G-Rg1. Although this metabolite has been reported to suppress platelet aggregation and to reduce gap junction-mediated intercellular communication, the modulatory activity of G-F1 on the functional role of skin-derived cells has not yet been elucidated. In this study, we evaluated the regulatory role of G-F1 on the cellular responses of B16 melanoma cells. G-F1 strongly suppressed the proliferation of B16 cells up to 60% at 200 μg/mL, while only diminishing the viability of HEK293 cells up to 30%. Furthermore, G-F1 remarkably induced morphological change and clustering of B16 melanoma cells. The melanin production of B16 cells was also significantly blocked by G-F1 up to 70%. Interestingly, intracellular signaling events involved in cell proliferation, migration, and morphological change were up-regulated at 1 h incubation but down-regulated at 12 h. Therefore, our results suggest that G-F1 can be applied as a novel anti?skin cancer drug with anti-proliferative and anti-migration features.

Purpose: The survey was performed to explore nurses` attitudes toward migrant wives in Korean society. Method: Four hundred thirty-eight respondents were recruited from 2 acute hospitals from 2 different geological areas. The attitude inventory to measure attitude toward migrant wives was utilized, which includes 6 factors such as prejudice, reliability, offensiveness, interests, acceptance, and influence. Result: The overall attitude was slightly positive (3.23) and reliability was the only non-positive scoring factor. Among the general characteristics education level showed a significant difference in 5 factors consistently compared to other characteristics. Conclusion: It can be concluded that Korean nurses tend to take a neutral to slightly positive attitude toward migrant wives. Therefore, any influence from nurses` attitudes related to migrant wives can be ignored. Obstacles or barriers which could hamper nursing care for migrant wives need to be identified and studies of strategies to overcome any existing barriers are called for.

Purpose: The present study was performed to identify the perception, attitude, and knowledge regarding the use of physical restraints among nursing personnel working at long-term care facilities. Method: 289 nurses, nurse aids and private caregivers working at 13 wards from 7 facilities participated in the survey. Perception, attitude and knowledge regarding the use of physical restraints were evaluated using the Perceptions of Restraints Use Questionnaire developed by Evans and Strumpf(1993) and Physical Restraint Questionnaire suggested by Janelli, et al(2006). Results: Wrist restraints were used the most frequently. The perception score regarding the use of physical restraints was 3.35, which is a moderate value. Study respondents considered `safety measure` and `safe use of a medical device` as the most important aspects when applying physical restraints to elderly. The respondents reported physical restraints were therapeutic at least to some degree but knowledge level about physical restraints of the respondents was rather low. Conclusion: Perception and attitude toward physical restraints were identified. The lack in knowledge about physical restraints needs to be addressed for more efficient use of them.

is bifunctional enzyme, which catalyzes the hydroxylation of L-tyrosine to L-dopa and enhances the oxidation of L-dopa to dopaquinone. There-fore, inhibitors of tyrosinase should be useful as therapeutic agents for the treatment of melanin hyperpigmentation. Many metal ion chelators, for example, kojic acid

One new ortho-dihydroxyisoflavone, 7,3',4'-trihydroxyisoflavone (2), and two known ortho-dihydroxyisoflavone derivatives were isolated from 5-year-old Doenjang (Korean fermented soypaste), and evaluated as potent antioxidant by comparing with other known isoflavones. 7,8,4'-Trihydroxyisoflavone (1), 7,3',4'-trihydroxyisoflavone (2), and 6,7,4'-trihydroxyisoflavone (3) inhibited DPPH (Diphenyl-1-picryl hydrazyl) formation by 50% at a concentration of 21.5+/-0.2, 28.7+/-0.4 and 32.6+/-0.6 (IC(50)), respectively, whereas three isoflavones showed weak DPPH radical scavenging activity. In xanthine oxidase (XO) system, in which both inhibition of xanthine oxidase and superoxide scavenging effect were measured in one assay. Compound 1 (IC(50)= 6.6+/-0.4 microM) and 2 (IC(50)=16.8+/-1.2 microM) show significant inhibitory activity and greater effect than allopurinol. But, compound 3 and other isoflavones showed lower inhibition activity. This study shows that the position of hydroxyl substituent at the aromatic ring of isoflavone plays an important role in radical scavenging effect.

Data were obtained as meanvalue of 1/[V], inverse of the increase of optical density at 450 nm per min. (OD450/min), of three independent tests with differentconcentrations of L-tyrosine as a substrate. (A) with 100 μM (rectangle), 50 μM (triangle), 25 μM (circle), or no kojic acid (B) with 40 μM(rectangle), 20 μM (triangle), 10 μM (circle), or no compound

To improve lipase activity and make the particulate carrier for practical application, lipase was conjugated to chitosan(Mwavg=80,000) by immine reaction. The lipase activity of conjugate was 93% of its initial activity at room temperature for 7 months, whereas the intact lipase activity decreased to 40%. And then, lipase-chitosan conjugate was intercalated within porous silica. The composite was characterized by X-ray diffraction, scanning electron microscopy, thermo gravimetric analysis. The Pore size was regulated in the range of 5~15nm. The maximum enzyme activity of lipase-chitosan conjugate needs the structure with 15nm pore of mesoporous silica. The resultant composite was found to have the free flowing property and keep up inner lipase activity.

Objectives Korean adolescent girls are unprepared for cervical cancer prevention due to the lack of a mandatory policy regarding human papilloma virus (HPV) vaccination and school health education regarding cervical cancer. The aim of this study was to determine how aware mothers are about cervical cancer prevention in their adolescent daughters, with a view to developing strategies for expanding primary cervical cancer prevention for adolescent girls through the mothers’ involvement. Design A qualitative design was employed. Nine mothers with adolescent daughters participated in this study and were interviewed using open-ended questions. The themes were extracted by content analysis. Setting A general living area in Seoul, South Korea. Participants The snowball method was used to select mothers. Results Five themes emerged. In general, the mothers’ awareness of cervical cancer was not clear, and they exhibited a lack of awareness of the importance of having a regular Papanicolaou screening test. The mothers recognised that they were role models for their daughters, and realised and accepted the necessity of educating their daughters regarding cervical cancer; however, they perceived barriers related to the prevention of cervical cancer in their daughters. The mothers recommended enforcing sex education in schools and the provision of financial support for HPV vaccination. Conclusions The mothers’ awareness and preparedness with respect to the prevention of cervical cancer in their adolescent daughters were low and inadequate. Mothers should be informed and motivated to play a role in the education of their daughters regarding cervical cancer prevention. Strategies for disseminating information regarding early cervical cancer prevention for adolescent girls are recommended by communicating with both the girls and their mothers and providing them with education regarding cervical cancer prevention.

There is an increasing reliability concern of thermal stress-induced failures in multilevel coatings in recent years. This work reports investigations of cracking of NiCr coatings due to thermal cycling. The temperature cycling in accelerated testing was performed in three temperature range of 150, 175 and 200°C. The NiCr coatings were considered to have failed when the sheet resistance changed by 30% relative to an initial value. As the cyclic repetition of thermal shock increased, the sheet resistance of NiCr coatings increased. The Coffin-Manson equation was applied to the failure mechanism of cracking of NiCr coatings and the SEM observation of cracks and delamination in NiCr coatings due to thermal cycling agreed well with the failure mechanism.

Lipid peroxidation has been suggested to play a key role in damaging biological processes resulting from excessive exposure to UV light. Aging of skin has been associated with increased peroxidation of skin lipid. In particular, squalene, which is a main component of skin surface polyunsaturated lipids, is easily peroxidized. Squalene-monohydroperoxide (Sq-OOH), the initial product of peroxidized squalene, is produced at the human skin by natural exposure to sunlight during day time activities. Recently, a few researchers reported on the damages of hairless mice skin by the topical application of Sq-OOH. Repeated application of Sq-OOH to the hairless mice induced its the skin wrinkles with clear and fine appearance. Histologically were seen, more keratinocyte hypertrophy with Sq-OOH treated skin than with chronic UVB irradiated group in epidermis. In dermis, characteristics, found in UVB irradiated skin, such as the loss of polarity, fractured collagen bundle and elastosis, were not observed severely. The alteration of epidermal layer might be the main factor for the formation of wrinkle caused by Sq-OOH. From the previous works, Sq-OOH is considered as an important source of damage in the early stage of aging process to result in epidermal wrinkle. Thus, it is very important to minimize such damage that would be induced mainly by Sq-OOH against healthy skin condition. Therefore, we tried to develop new anti-aging materials for protecting skin damage by Sq-OOH. Hydroxamic acids, the naturally occurring products exhibit low toxicities in general, and are of interest for many therapeutic applications. Recently, hydroxamic acids and derivatives were reported largely as effective antibacterial and antifungal agents. Their activities originate from their ability to coordinate on metal ions. That is, hydroxamic acid group is regarded as an one electron donor. Hydroxamic acid moiety has also drawn much attention as a reactive oxygen species (ROS) scavenger. In this study, a new skin protecting compound, (4-(Nhydroxycarbamoyl)phenyl)-N-adamantanylcarboxamide (1) is synthesized to show inhibitory activities of lipid peroxidation both in vitro and in vivo. The targeted compound 1 is a hydroxamic acid derivative which possesses an amide linker between hydroxamic acid and adamantane moiety. Adamantane group was adopted as a hydrophobic moiety to optimize antioxidant activity of hydroxamic acid in animal test. Compound 1 is believed to be adequate in skin permeation because of its balance in hydrophilic and hydrophobic character.

Two kaempferol glycosides were isolated from green tea seed extract (GTSE). After conducting a structure analysis, these two compounds were identified as kaempferol-3-O-[2-O-beta-D-galactopyranosyl-6-O-alpha-L-rhamnopyranosyl]-beta-D-glucopyranoside (compound 1) and kaempferol-3-O-[2-O-beta-D-xylopyranosyl-6-O-alpha-L-rhanmopyranosyl]-beta-D-glucopyranoside (compound 2). These two compounds were hydrolysed by o-glycolytic enzymes for the production of kaempferol. After performing several reactions, we found the optimum enzyme combination, a reaction with beta-galactosidase and hesperidinase. Finally, we produced kaempferol of above 95% purity. The 5alpha-reductase inhibition activities of GTSE hydrolysate (GTSE-H) containing kaempferol were evaluated by the contact cell-based metabolic method using a stable HEK 293 cell line. GTSE-H showed a good inhibition effect on HEK 293 cell lines both type 1 and type 2 on 5alpha-reductase. Especially, GTSE-H inhibited type 2 with kaempferol content dependency. The results indicate that the inhibition activity of hydrolysate on 5alpha-reductase type 2 increases in accordance with kaempferol content.

Background Although retinoids have potential efficacy in aged skin, their side effect (skin irritation) remains a clinical problem. We designed a novel synthetic retinoid, seletinoid G, by using computer-aided molecular modeling, and investigated its effects on the expression of extracellular matrix proteins in human skin in vivo. Methods Twenty-three subjects were tested on the buttocks using 4-day occlusive application of seletinoid G and all- trans retinoic acid ( t RA). Skin irritation after topical application was quantified by the degree of erythema and cutaneous blood flow. The expression of extracellular matrix proteins and interstitial collagenase (MMP-1) in skin biopsies was investigated by immunohistochemical staining and Western blotting. Results The topical application of seletinoid G under occlusion induced no skin irritation in contrast to t RA, which caused severe erythema. The topical treatment with seletinoid G increased the expressions of type I procollagen, tropoelastin, and fibrillin-1, and reduced MMP-1 in old skin in vivo. Seletinoid G was found to inhibit not only the UV-induced decrease of type I procollagen but the UV-induced increase of MMP-1 and c-Jun protein in young skin in vivo. Conclusions Seletinoid G is a novel synthetic retinoid, which has little the side effect of skin irritation after topical application. Seletinoid G can repair altered connective tissue in old skin and inhibit UV-induced collagen deficiency in young skin.

A stable derivative of kojic acid, 5-[(3-aminopropyl)phosphinooxy]-2-(hydroxymethyl)-4H-pyran-4-one (Kojyl-APPA), was synthesized in good yield. The effects of Kojyl-APPA on tyrosinase activity and melanin synthesis were investigated. Kojyl-APPA showed tyrosinase inhibition effect (30%) in situ, but not in vitro. Kojyl-APPA inhibited tyrosinase activity significantly at 24 h after treatment in normal human melanocytes. It means that Kojyl-APPA is not a direct inhibitor of tyrosinase itself, but it is converted to a potential inhibitor kojic acid enzymatically in cells. In addition, Kojyl-APPA decreased melanin content to 75% of control in melanoma cells and decreased neomelanin synthesis to 43% of control in normal human melanocytes. Its permeation through skin increased by about 8 times as compared with kojic acid.

Π-A isotherms and phase behaviors of ‘tocomide’, a newly synthesized 1,3-bis(N-(2-hydroxyethyl)-tocopherol succinylamino)-2-hydroxypropane, mixed with cholesterol and linoleic acid, was studied for its monolayer miscibility and a stable delivery formulation for antioxidant applications. The monolayer of tocomide and cholesterol was formed in a homogeneously mixed state at air–water interface. The ternary mixtures with linoleic acid showed various bulk structures, including a stable and transparent solution of thermodynamically stable lamellar phase. The lamellar structure was confirmed by the X-ray diffraction (XRD) patterns and polarized microscopy such that pure tocomide formed a liquid crystal at room temperature with a lamellar periodicity of 36.7 A (2θ=2.41°)

Tyrosinase is a copper-containing enzyme, which catalyzes two distinct reactions of melanin synthesis, the hydroxylation of L-tyrosine to L-dopa and the oxidation of L-dopa to dopaquinone. These processes are involved in local hyperpigmentation such as melasma and lentigo. Therefore, the inhibition of tyrosinase to treat the pigmentation disorders has been a recent subject of many studies. Kojic acid (1) is well known as one of the most popular tyrosinase inhibitors and it has been widely used as a skin-whitening agent. However, the inhibitory activity of kojic acid is not potent enough. To overcome this drawback, many semi-synthetic kojic acid derivatives were synthesized usually by the modification of C-2 hydroxyl group into ester, hydroxyphenyl ether, and glycoside. Recently, two molecules of kojic acid were connected by ester and ethylene. Their inhibitory activities were dramatically enhanced. Thus we became interested in new kojic acid derivatives containing two molecules of kojic acid. In this study, we connected two molecules of kojic acid by various chemical bonds such as ester, amide, and thioether. Anti-melanogenic activities of compounds (4a-4f) were compared with that of kojic acid (Figure 1).

genous supplementation of antioxidants may be an effective strategy to counteract the deleterious effects of the ROS generated from the excessive exposure to UV irradiation. Resveratrol (trans-3,4',5-trihydroxystilbene), a naturally occurring hydroxyl stilbene, is considered an essential antioxidative constituent of red wine. 4 It showed broad antioxidative activities such as scavenging of the free radicals, 5 inhibition of lipid peroxidation, 6 inhibition of the platelet aggregation 7 and anti-cancer activity. 8 However, because of its unfavorable photo stability, the application of transresveratrol has been limited. Various UV irradiation conditions showed that trans-resveratrol was easily transformed into cis-resveratrol. 9 Therefore, an attempt to search for photo stable alternative material of trans-resveratrol is desirable. In this study, a mimic compound of trans-resveratrol, 3,5-dihydroxy-N-(4-hydroxyphenyl)benzamide (2), containing an amide linker between two hydroxyl phenyl groups, is synthesized. We evaluated various biological activities of compound 2 compared with trans-resveratrol (Fig. 1).

Green chemistry has attracted much attention in organic chemistry. Major goal in this area is to maximize the efficient use of raw materials and simultaneously to minimize waste. In this context, conversion of conventional organic processes into the highly atom-efficient protocol with good selectivity is the most desirable. The carboxylation of epoxides shows an interesting application in the utilization of carbon dioxide to produce cyclic carbonates. These compounds are useful as monomers, polar aprotic solvents, and intermediates for the synthesis of pharmaceuticals and fine chemicals. Recently, we have studied the coupling of CO2 with styrene oxide as a model reaction as the carboxylation of epoxides and have noticed the processes using quaternary onium salts such as tetraalkylammonium and phosphonium halides are of full-atom-economy-type to convert styrene oxide into styrene carbonate: efficient, clean and by-productfree under solvent-free reaction conditions. We found the detailed information on the use of onium salts for this reaction under solvent-free conditions is surprisingly limited except a few examples. The patent by McMullen et al. described the coupling reaction of ethylene oxide with CO2 to produce ethylene carbonate in up to 99% yield when catalyzed by several ammonium salts such as tetraethylammonium chloride and a few other ammonium halides. However, the detailed studies of the reaction profile and the catalytic efficiency of quaternary salts in the coupling of CO2 with epoxides are still lacking so far. Historically, quaternary ammonium halides have been often used as complexed with transition metal catalysts or as the reaction ionic medium to promote the reactions of the coupling of CO2 with epoxides rather than used alone. Recent mechanistic studies suggest on the role of these catalytic systems that an epoxide is coordinated to the halogenated metal anion, generated from the interaction of the metal halide with the halide ion, and the resulting coordinated epoxide ring is opened by the halide ion to form an haloalkoxy species. Nucleophilic attack of the haloalkoxy species on CO2 leads to a linear halocarbonate that is transformed into a cyclic carbonate by the intramolecular substitution of the halide. Herein, we report on the detailed reaction profile of carboxylation of styrene oxide catalyzed by various onium salts, particularly such as quartenary ammonium and phosphonium halides under various temperatures and CO2 pressures as shown in Scheme 1. Quatenary ammonium salts-catalyzed reaction. Table 1 shows the results of the experiments performed to optimize the conditions for the carboxylation of styrene oxide in the Scheme 1

Long chain alkanolamides have attracted considerable interest because of their intrinsic amphiphilic properties. They are frequently used as a surfactant for cosmetics and pharmaceutical use. In the course of the synthesis of alkanolamides, control of chemoselective amide formation over competing O-acylation of neighboring hydroxyl groups plays a key step. Several methods have been developed which include a few enzymatic synthesis and the reaction of carboxylic acid with amino alcohols by the aid of N-ethoxy1-ethoxy-dihydroquinone (EEDQ) in ethanol reflux condition. However, these known methods have drawbacks for example narrow application scope in enzymatic reaction, longer reaction time and harsh reaction condition. Recently, we have reported that chemoselective N-acylation of amino alcohols promoted by magnesium oxide in aqueous organic solution. Although the use of this method was successful in many cases, preparation of acid chloride is not always easy so there is still a strong need for more convenient amidation method of amino alcohols. Now we report a useful procedure for the efficient and chemoselective amidation of hydrophilic amino alcohols with mixed anhydride generated from carboxylic acid and ethylchloroformate (Scheme 1). Treatment of benzoic acid 1a with ethylchloroformate (1.1 equiv) in the presence of N-methylmorpholine (1.1 equiv) in THF gave mixed anhydride, which subsequently reacted with tris(hydroxymethyl)aminomethane 3a in DMF and TEA (1.1 equiv) to give alkanolamide 4a in 85% yield (entry 1 in Table 1). The formation of by-products such as O-acylated and N, O-diacylated derivatives have not been observed in HPLC analysis. After the disappearance of mixed anhydride checked by TLC analysis, DMF was evaporated in vacuo. The residue of reaction mixture was extracted with ethyl acetate, washed with water. The organic layer was analyzed by HPLC. As shown in Figure 1, small amount of benzoic acid were detected without by-products. Benzoic acid was easily separated by flash chromatography. As an additive for the synthesis of mixed anhydride, TEA as well as N-methylmorpholine was effective. Of solvents tested, THF and ether were suitable. Using aliphatic carboxylic acid 2b, alkanolamide 4b was also obtained in high yield (entry 2). Further, this method was successfully extended to other acids containing acid or base-sensitive groups such as cyclic disulfide, ester and acetate (entry 3, 4 and 5). In all cases, byproducts that are usually formed in the reaction of acid chlorides with amino alcohols were not detected. Preferential amine selectivity can be explained by assuming low electrophilicity of mixed anhydride comparing with acid chloride. Because of its low electrophilicity, more nucleophilic amino groups may only react with mixed anhydride. The reaction also worked well for the other hydrophilic amine such as ethanolamine, DL-serine methyl ester and diethanolamine. The desired alkanolamides 4f, 4g and 4h

The reaction of hydrophilic amino alcohols with sulfonyl chlorides in the presence of metal oxide (MgO, CuO, Ag2O) in aqueous organic solution cleanly provided alkanolsulfonamide. Advantages of this method were mild, neutral reaction conditions, chemoselectivity and easy isolation of the final product.

Meanwhile, in many of the designed supramolecularsystems, obtaining a specific convergent orientation of parti-cular ligating functions toward active site is highly desirablefor selective and strong binding of targeted guests. For thesepurpose, U-shaped structural motif of Kemp’s triacid isknown to be very useful and resulted in the developments ofmany sophisticated supramolecular systems.

The reaction of hydrophilic amino alcohols with acid chlorides in the presence of magnesium oxide in aqueous organic solution (THF/H2O=4:1) cleanly provided alkanolamides.

Summary Background. Melasma is a common pigmentary disorder that poses therapeutic challenges. Mixed-type melasma usually does not respond to conventional monotherapy. Objective. To evaluate the effectiveness and safety of 1064-nm Q-switched neodymium-doped yttrium–aluminium–garnet laser (1064 QNYL) and 30% glycolic acid (GA) peel in the treatment of melasma. Methods. This was a split-face study, in which 16 patients were treated with 1064 QNYL (6-mm spot size, 2.0–2.3 J/cm2 fluence) for six sessions at 1-week intervals to the entire face, and with GA for three sessions at 2-week intervals to the experimental side of the face. Clinical evaluations, measurements on a pigment measuring device (Mexameter), and assessment of patient satisfaction and adverse events were performed at baseline and every visit. Results. After treatment, significant improvements from baseline were seen in Mexameter and modified Melasma Area and Severity Index (mMASI) on both sides of the face. The combined therapy side achieved an average 32.6% improvement in Mexameter readings and 37.4% improvement in mMASI, compared with 22% and 16.7%, respectively, on the side treated with laser only (P ≤ 0.05). Both the physician and patient assessments correlated with the Mexameter results and mMASI. Conclusion. Combined 1064 QNYL and GA seems to be superior to 1064 QNYL alone in the treatment of mixed-type melasma.