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한약단미제 및 탕제의 항 Herpes Simplex Virus Type-1 활성탐색 (Screening of Antiviral Activities of Korean Medicinal Herbs and Traditional Prescriptions Against Herpes Simplex Virus Type-1)

  • 강봉주;양기상;김명희;박갑주
    • 대한바이러스학회지
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    • 제27권2호
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    • pp.227-237
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    • 1997
  • 향약집성방 및 동의보감등 한의학 서적을 기초로 하여 선택한 탕제 45종과 단미제 80종의 메탄올과 열수추출물을 가지고 MTT assay를 실시하여 항Herpes simplex virus-1 (HSV-1)에 대한 활성을 조사하였다. 열수추출 탕제 45종 중 백사전방, 현람방I, 현람방II, 반천청방 4종에서 항 HSV-1 활성을 나타냈고, 이들의 SI (selective index)값은 $2.1{\pm}0.5$에서 $11.8{\pm}2.2$ 범위의 값을 가졌으며 메탄올추출 탕제 45종 중에서는 단치시호탕III, 반천청방, 정향울금방, 대황오배자고, 홍인락삼등방, 호장해독탕에서 활성을 보였고 이들의 SI값은 $1.7{\pm}0.2$에서 $10.5{\pm}3.1$ 범위의 값을 나타냈다. 열수추출 단미제 중계지, 관중, 구인분, 대황, 자화지정, 포공영, 호장근, 황백등 8종에서 항 HSV-1 활성이 나타났고, 이들의 SI값은 $1.6{\pm}0.1$에서 $10.2{\pm}0.7$ 범위의 값을 가졌으며 메탄올추출 탕제 중에서는 계지, 목방기, 상지, 호장근에서 활성을 보였고 이들의 SI 값은 $2.9{\pm}1.5$에서 $9.3{\pm}0.5$ 범위의 값을 나타내었다. 처방제 중 반천청방은 열수추출물과 메탄올 추출물 모두에서 항바이러스 활성을 나타냈고, 단미제 중 계지와 호장근도 열수와 메탄올 추출물 모두에서 항바이러스 활성을 보였다. 이들 탕제 및 단미제는 분획 및 분석실험을 실시하여 활성성분을 추적하고 있다.

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Potential Antitumor $\alpha$-Methylene-$\gamma$-butyrolactone-Bearing Nucleic Acid Base. 3. Synthesis of $5^1$-Methyl-$5^1$-[(6-substituted-9H-purin-9-yl)methyl]-$2^1$-oxo-$3^1$-methylenetetrahydrofurans

  • Kim, Jack-C.;Kim, Si-Hwan;Kim, Ji-A;Choi, Soon-Kyu;Park, Won-Woo
    • Archives of Pharmacal Research
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    • 제21권4호
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    • pp.458-464
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    • 1998
  • Search for a new $\alpha$-methylene-$\gamma$-butyrolactone-bearing 6-substituted purine as a potental antitumor agent has led to synthesize seven, hitherto unreported, $5^1$-Methyl-$5^1$-[(6-substituted-9H-purin-9-yl)methyl]-$2^1$-oxo-$3^1$- methylenetetrahydrofurans (H, Cl, l, $CH_3$, $NH_2$, SH, >C=O) (6a-g). These include $5^1$-Methyl-$5^1$-[(9H-purin-9-yl)methyll-$2^1$-oxo-$3^1$ -methylenetetrahydrofurans (6a), $5^1$-Methyl-$5^1$-[(6-chloro-9H-purin-9-yl)methyl]-$2^1$-oxo-$3^1$-methylenetetrahydr ofurans (6b), $5^1$-Methyl-$5^1$-[(6-chloro-9H-purin-9-yl) methyl]-$2^1$-oxo-$3^1$-methylenetetrahydrofurans (6c), $5^1$-Methyl-$5^1$-[(6-methyl-9H-purin-9-yl) methyl]-$2^1$-oxo-$3^1$-methylenetetrahydrofurans (6d), $5^1$-Methyl-$5^1$-[(9H-adenin-9-yl)methyll-$2^1$-oxo-$3^1$-methylenetetrahydrofurans (6e), $5^1$-Methyl-$5^1$-[(6-mercapto-9H-purin-9-yl) methyl]-$2^1$-oxo-$3^1$-methylenetetrahydrofurans (6f) and $5^1$-Methyl-$5^1$-[(9H-hypoxanthin-9-yl)methyll-$2^1$-oxo-$3^1$-methylenetetrahydrof urans (6g) which were made by the Reformatsky-type reaction of ethyl $\alpha$-(bromomethyl) acrylate with the corresponding (6-substituted-9H-purin-9-yl)-2-propanone intermediates (5a-g). These ketone intermediates 5a-g, 1-(9H-purin-9-yl)-2-propanone (5a), 1-(6-chloro-9H-purin-9-yl)-2-propanone (5b), 1-(6-iodo-9H-purin-9-yi)-2-propanone (5c), 1-(6-methyl-9H-purin-9-yl)-2-propanone (5d), 1-(9H-adenin-9-yl)-2-propanone (Se), 1-(6-mercapto-9H-purin-9-yl)-2-propanone (5f), and 1-(9H-hypoxanthin-9-yl)-2-propanone (5g) were directly obtained by the alkylation of the 6-substituted purine bases with the chloroacetone in the presence of $K_2$$CO_3$ (or NaH) under DMF (or DMSO). The preliminary in vitro cytotoxcity assay for the synthetic .alpha.-methylene-y-butyro-lactone compounds (6a-g) were determined against three cell lines (PM-3A, P-388, and K-562) and showed the moderate antitumor activity ($IC_50$ ranged from 1.4 to 4.3 $\mu\textrm{g}$/ml) with the compound $5^1$-methyl-$5^1$ -[(9H-hypoxanthin-9-yl)methyl]-$2^1$-oxo-$3^1$-methylenetetrahydrofuran (6g) showing the least antitumor activity.

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Melanogenesis regulatory constituents from Premna serratifolia wood collected in Myanmar

  • WOO, SO-YEUN
    • 한국자원식물학회:학술대회논문집
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    • 한국자원식물학회 2019년도 춘계학술대회
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    • pp.21-22
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    • 2019
  • Melanin is a mixture of pigmented biopolymers synthesized by epidermal melanocytes that determine the skin, eye, and hair colors. Melanocytes produce two different kinds of melanin, eumelanin (dark brown/black insoluble pigments found in dark skin and dark hair and pheomelanin (lighter red/yellow). The biological role of melanin is to prevent skin damage by ultraviolet (UV) radiation. However, the overproduction or deficiency of melanin synthesis could lead to serious dermatological problems, which include melasma, melanoderma, lentigo, and vitiligo. Therefore, regulating melanin production is important to prevent the pigmentation disorders. Myanmar has a rich in natural resources. However, the chemical constituents of these natural resources in Myanmar have not been fully investigated. In the effort to search for compounds with anti-melanin deposition activity from Myanmar natural resources, five plants were collected in Myanmar. Extracts of these collected five plants were tested for anti-melanin deposition activity against a mouse melanoma cell line (B16-F10) induced with ${\alpha}$-melanocyte-stimulating hormone (${\alpha}$-MSH) and 3-isobutyl-1-methylxanthine (IBMX), and their anti-melanin deposition activities were compared with the positive control, arbutin. Among the tested extracts, the CHCl3 extracts of the Premna serratifolia (syn: P. integrifolia) wood showed anti-melanin deposition activities with IC50 values of $81.3{\mu}g/mL$. Hence, this study aims to identify secondary metabolites with anti-melanin deposition activity from P. serratifolia wood of Myanmar. P. serratifolia belongs to the Verbenaceae family and is widely distributed in near western sea coast from South Asia to South East Asia, which include India, Malaysia, Vietnam, Cambodia, and Sri Lanka. People in Tanintharyi region located in the southern part of Myanmar utilize the P. serratifolia, Sperethusa crenulata, Naringi crenulata, and Limonia acidissima as Thanaka, traditional cosmetics in Myanmar. Thanaka is applied in the form of paste onto skins to make it smooth and clear, as well as to prevent wrinkles, skin aging, excessive facial oil, pimples, blackheads, and whiteheads. However, the chemical constituents responsible for their cosmetic properties are yet to be identified. Moreover, the chemical constituents of P. serratifolia was almost uncharacterized. Investigation of the P. serratifolia chemical constituents is thus an attractive endeavor to discover new anti-melanin deposition active compounds. The investigation of the chemical constituents of the active CHCl3 extract of P. serratifolia led to isolation of four new lignoids, premnan A (1), premnan B (2), taungtangyiol C (3), and 7,9-dihydroxydolichanthin B (4), together with premnan C (5) (assumed to be an artifact), one natural newlignoid,(3R,4S)-4-(1,3-benzodioxol-5-ylcarbonyl)-3-[(R)-1-(1,3-benzo dioxol-5-yl)-1-hydroxy methyl]tetrahydro-2-furanone (6), and five known compounds (7-11)1,2). The structures of all isolated compounds were determined on the basis of their spectroscopic data and by comparison with the reported literatures. The absolute configurations of 1-3 and 5 were also determined by optical rotation and circular dichroism (CD) data analyses1). The anti-melanin deposition activities of all the isolated compounds were evaluated against B16-F10 cell line. 7,9-Dihydroxydolichanthin B (4) and ($2{\alpha},3{\alpha}$)-olean-12-en-28-oic acid (11) showed strong anti-melanin deposition activities with IC50 values of 18.4 and $11.2{\mu}M$, respectively, without cytotoxicity2). On the other hand, compounds 1-3, 5, and 7 showed melanogenesis enhancing activities1). To better understand their anti-melanin deposition mechanism, the effects of 4 and 11 on tyrosinase activities were investigated. The assay indicated that compounds 4 and 11 did not inhibit tyrosinase. Furthermore, we also examined the mRNA expression of microphthalmia-associated transcription factor (MITF), tyrosinase (TYR), tyrosinase-related protein-1 (TRP-1), and tyrosinase-related protein-2 (TRP-2). Compounds 4 and 11 down-regulated the expression of Tyr and Mitf mRNAs, respectively. Although the P. serratifolia wood has been used as traditional cosmetics in Myanmar for centuries, there are no scientific evidences to support its effectiveness as cosmetics. Investigation of the anti-melanin deposition activity of the chemical constituents of P. serratifolia thus provided insight into the effectiveness of the P. serratifolia wood as a cosmetic agent.

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주민 의식 조사를 통한 지자체 기후변화 대응 강화 방안에 관한 연구 - 강남구를 중심으로 - (A Study on the Reinforcement Plan for the Local Government to Respond to the Climate Change through the Survey of Residents Consciousness - Focused on the Gangnam-gu -)

  • 최봉석;박경은;전의찬
    • 한국기후변화학회지
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    • 제5권1호
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    • pp.83-94
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    • 2014
  • 본 연구에 활용된 강남구는 광양과 울산, 포항 등 일부 산업지역을 제외한 단위 면적당 에너지소비량과 온실가스 배출량이 가장 많은 지역이다. 강남구의 온실가스 배출량은 4,863,765 $tCO_2$로, 서울시 50,330,356 $tCO_2$의 약 10%를 차지하고 있으며, 상업부문의 온실가스 배출량 1위, 가정부문 배출량 2위를 차지하고 있다. 지구온난화 현상에 관한 5가지 항목의 평균 인지도는 83.58%로 나타났으며, 온실가스 감축의 주체에 대한 설문에서는 20대를 제외한 모든 연령대에서 강남구 주민이 해야 한다고 응답하였다. 지자체의 기후 변화 대응(완화)을 위한 지자체의 역할부문에서는 걷기 자전거 타기에 좋은 도시 기반 구축이 필요한 것으로 나타났으며, 기후변화 대응을 위한 교육시설 항목에서는 중 고등학교에서 교육이 이루어져야 한다고 나타났다. 생활 속 기후변화 대응을 위한 실천행동에 대해서는 생활 속에서의 에너지 및 자원 절약은 대체적으로 잘 실천되고 있었지만, 에코마일리지(구 탄소마일리지)에 대해서는 실천하지 않는다는 응답이 높았다. 또한, 생활 속 실천을 해도 혜택이 없다는 응답이 많아, 지자체의 기후변화 대응 정책이 구체적이고 실효성이 있으려면 인센티브가 필요함을 알 수 있었다. 본 연구는 기후변화 대응 의식조사를 통해 의식이 낮은 항목에 지자체의 정책적 노력을 통해 주민의식을 향상시킬 수 있는 정책적 방안을 모색하는 데 있다.