• Title/Summary/Keyword: 약학

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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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    • v.21 no.4
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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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Evaluation of the Congenital Hypothyroidism for Newborn Screening Program in Korea: A 14-year Retrospective Cohort Study (한국인 선천성 갑상선기능저하증에 대한 신생아선별검사의 14년간의 후향적 연구; 발생빈도와 유효성)

  • Yoon, Hye-Ran;Ahn, Sunhyun;Lee, Hyangja
    • Journal of The Korean Society of Inherited Metabolic disease
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    • v.19 no.1
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    • pp.1-11
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    • 2019
  • Purpose: Congenital hypothyroidism (CH) is the most common congenital endocrine disorder. The purpose of the present study was to determine the incidence of CH in South Korea during the period from January 1991 to March 2004. Methods: Central data from each city branch of SCL (Seoul Clinical Reference Laboratories) in Yongin, South Korea, was gathered and collectively analyzed. Newborn screening (NBS) for CH was based on measuring the levels of neonatal thyroid stimulating hormone (TSH) and free T4 (a cut-off of 20 mIU/L and less than 0.8 ng/dL, respectively). Results: During the study period, 671,805 live births were screened for CH based on TSH and free T4 ELISA assays. A total of 159 newborns were deemed positive for CH out of 671,805, with a corresponding incidence of 1 in 4,225. When a cut-off of 20 mIU/L was used in TSH assays, the associated sensitivity, specificity, and positive predictive values (PPV) were 100.0%, 99.7%, and 10.8%, respectively. When a cut-off of 0.8 ng/dL in free T4 assays was used, the associated sensitivity, specificity, and PPV were 100.0%, 98.5%, and 3.9%, respectively. Conclusion: CH incidence in South Korea as evidenced by the results of NBS was compared with its incidence and comparable to the other countries prior to 2004.

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Korean Ginseng in "The Veritable Records of King Sejong" (『세종실록』을 통해 본 고려인삼)

  • Joo, Seungjae
    • Journal of Ginseng Culture
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    • v.3
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    • pp.11-37
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    • 2021
  • Korean ginseng is the one of the most famous medicinal herbs globally and has long been a representative item of East Asian trade, including across China and Japan. Since Joseon (1392-1910) ginseng trade was entirely controlled by the state, The Veritable Records of the Joseon Dynasty are a valuable resource that can shed light on the history of the ginseng industry at that time. By studying the subsection "The Veritable Records of King Sejong" (世宗實錄), when ginseng was used even more widely, we assess the purpose and scale of its trade in the 15th century, identify its original listing in the geographical appendix, develop a distribution map, and explore similarities to current ginseng cultivation areas. During the reign of King Sejong (1418-1450), ginseng was sent to China as a tribute 101 times, with a combined weight of 7,060 kilograms, with less than one-third of that amount given to Japan and Okinawa. It was used to cover the travel expenses of foreign envoys and servants, but this can be seen to gradually decrease after the regnal mid-term, primarily due to a decrease in the amount of ginseng being collected. At the time, there were 113 areas of naturally growing ginseng as listed in the records' geographical appendix, including 12 recorded in the 'tributes' category: Yeongdeok-gun, Yeongju, and Cheongsong-gun in Gyeongsangbuk-do; Ulju-gun and Ulsan in Gyeongsangnam-do; Jeongeup, Wanju-gun, and Jangsu-gun in Jeollabuk-do; Hwasun-gun in Jeollanam-do; Goksan-gun and Sinpyeong-gun in Hwanghaebuk-do; Jeongju and Taecheon-gun in Pyeonganbuk-do; and Jaseong-gun and Junggang-gun in Jagang-do. A total of 101 places are recorded in the 'medicinal herbs' category, located throughout the mountains of the eight Joseon provinces, except the islands. In comparison with current ginseng cultivation sites, many of these historical areas are either consistent with or adjacent to contemporary locations. The geographical appendix to "The Veritable Records of King Sejong" was compiled in the early days of the king's reign (1432) when there was a lot of wild ginseng. The appendix is a valuable resource that indicates the possibility of growing ginseng on the Korean Peninsula in the future. The apparently natural habitats in the south, where ginseng is not currently cultivated, could be candidates for the future. Moreover, areas in the north where ginseng has not been grown, except Kaesǒng, could be a good alternative under sustainable inter-Korean exchange should cultivation sites move north due to climate warming.

An Analysis of Ginseng Advertisements in 1920-1930s Newspapers During Japanese Colonial Period (일제강점기 중 1920-1930년대 신문에 실린 인삼 광고 분석)

  • Oh, Hoon-Il
    • Journal of Ginseng Culture
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    • v.4
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    • pp.103-127
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    • 2022
  • The influx of modern culture in the early 20th century in Korea led to numerous changes in the country's ginseng industry. With the development of ginseng cultivation technology and commerce, the production and consumption of ginseng increased, and various ginseng products were developed using modern manufacturing technology. Consequently, competition for the sales of these products became fierce. At that time, newspaper advertisements showed detailed trends in the development and sales competition of ginseng products. Before 1920, however, there were few advertisements of ginseng in newspapers. This is thought to be because newspapers had not yet been generalized, and the ginseng industry had not developed that much. Ginseng advertisements started to revitalize in the early 1920s after the launch of the Korean daily newspapers Dong-A Ilbo and Chosun Ilbo. Such advertisements in this period focused on emphasizing the traditional efficacy of Oriental medicine and the mysterious effects of ginseng. There were many advertisements for products that prescribed the combination of ginseng and deer antler, indicating the great popularity of this prescription at the time. Furthermore, advertisements showed many personal experience stories about taking such products. Mail order and telemarketing sales were already widely used in the 1920s . In 1925, there were advertisements that ginseng products were delivered every day. The advertisements revealed that ginseng roots were classified more elaborately than they are now according to size and quality. Ginseng products in the 1920s did not deviate significantly from the scope of traditional Oriental medicine formulations such as liquid medicine, pill, and concentrated extract. In the 1930s, ginseng advertisements became more active. At this time, experts such as university professors and doctors in medicine or in pharmacy appeared in the advertisements. They recommended ginseng products or explained the ingredients and medicinal effects of the products. Even their experimental notes based on scientific research results appeared in the advertisements to enhance the reliability of the ginseng products. In 1931, modern tablet advertisements appeared. Ginseng products supplemented with vitamins and other specific ingredients as well as ginseng thin rice gruel for the sick appeared at this time. In 1938, ginseng advertisements became more popular, and advertisements using talents as models, such as dancer Choi Seunghee or famous movie stars, models appeared. Ginseng advertisements in the 1920s and 1930s clearly show a side of our rapidly changing society at the time.

Increase in Neurogenesis of Neural Stem Cells Cultured from Postnatal Mouse Subventricular Zone by Nifedipine (L-type 칼슘 채널을 저해하는 저해제, nifedipine에 의한 쥐 뇌실하 영역 신경줄기세포의 신경세포로의 분화 촉진)

  • Park, Ki-Youb;Kim, Man Su
    • Journal of Life Science
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    • v.32 no.2
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    • pp.108-118
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    • 2022
  • The subventricular zone (SVZ) in the brain contains neural stem cells (NSCs) that generate new neurons throughout one's lifetime. Many extracellular and intracellular factors that affect cell proliferation and neuronal differentiation of NSCs are already well-known. Recently, L-type calcium channels have been reported to regulate neural development and are present in NSCs, differentiating neuroblasts, and mature neurons in the SVZ. Nifedipine, a blocker of L-type calcium channels, has been long used as a therapeutic drug for hypertension. However, studies on the use of nifedipine to inhibit L-type calcium channels of NSCs are lacking. Herein, we treated NSCs cultured from mouse postnatal SVZ with nifedipine during neuronal differentiation. Nifedipine increased the number of Tuj1-positive neurons but did not significantly change the number of Olig2-positive oligodendrocytes. Nifedipine increased cell division during early differentiation, which was detected using the 5-ethynyl-2'-deoxyuridine incorporation assay and immunocytochemistry assessment by staining the cells with phosphorylated histone H3, a mitosis marker. Nifedipine increased the transcription of Dlx2, a neurogenic transcription factor, and the level of Mash1, a marker for early neurogenesis. In addition to nifedipine, verapamil, which is also an L-type calcium channel blocker, showed a slight increase in neurogenesis, but its statistical significance was very low. In contrast, pimozide, a T-type calcium channel blocker, did not affect neurogenesis, although T-type calcium channel genes Cav3.1, Cav3.2, and Cav3.3 were expressed. In summary, nifedipine might promote the neuronal fate of NSCs during early differentiation and calcium signaling through L-type calcium channels might be involved in neuronal differentiation, especially during the early stages of differentiation.

Verification of Anti-Inflammatory Efficacy of Apple Mango (Mangifera indica L.) Peel in LPS-Activated Macrophage (LPS에 의해 활성화된 대식세포에서 애플망고 껍질(Mangifera indica L. Peel)의 항염증 효능 검증)

  • Hyo-Min Kim;Dan-Hee Yoo;In-Chul Lee
    • Microbiology and Biotechnology Letters
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    • v.50 no.3
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    • pp.337-346
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    • 2022
  • The purpose of this study was to investigate the antioxidant and anti-inflammatory activities of hot water (AMPW) and 70% ethanol (AMPE) extracts of apple mango (Mangifera indica L.) peel. The antioxidant activities were measured using a total polyphenol, electron-donating, 2,2'-azinobis [3-ethylbenzothiazoline6-sulfonic acid] (ABTS) radical scavenging assay. The total polyphenol content of AMPW and AMPE was 66.08 ± 0.62 mg TAE/100 g and 100.13 ± 0.23 mg TAE/100 g, respectively. As a result of measuring the electrondonating ability, at a concentration of 1,000 ㎍/ml, AMPW and AMPE showed an effectiveness of 86% and 94%, respectively. The ABTS assay showed 80% and 98% respective radical scavenging activity for AMPW and AMPE, at a concentration of 1,000 ㎍/ml. The cell viability on macrophage cells was performed using a 3-[4,5-dimethyl-thiazol-2-yl]-2,5-diphenyl-tetrazoliumbromide (MTT) assay, and the results showed more than 90% cell viability at a 100 ㎍/ml concentration. Anti-inflammatory activity was verified by confirming nitric oxide (NO) production inhibitory activity, inducible nitric oxide synthase (iNOS), and cyclooxygenase-2 (COX-2) protein and mRNA expression inhibitory activity from lipopolysaccharide (LPS)-treated RAW 264.7 cells. The NO production inhibitory effects were measured using the Griess assay, which confirmed 45% and 40% inhibition after treatment with AMPW and AMPE, respectively. Moreover, the protein and mRNA expression of inflammatory-related factors iNOS and COX-2, decreased in a concentrationdependent manner. In conclusion, this study showed antioxidant and anti-inflammatory effects of Mangifera indica L. peel and revealed its promising potential for application as an antioxidant and anti-inflammatory agent.

Analysis of research trends in mushroom science in North Korean journals (1978-2023) (북한 학술지에 게재된 버섯과학 연구동향 분석(1978~2023))

  • Woo-Sik Jo
    • Journal of Mushroom
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    • v.21 no.3
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    • pp.93-100
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    • 2023
  • In this study, research trends in mushroom science were examined using North Korean journal articles published in 1978-2023. Researchers in each field reviewed 450 papers and finally selected 429 papers, excluding 21 papers classified in different fields. The number of researchers was 872, and the number of authors per paper was 2.03. Kim Cheol-Hak published the most academic papers in the field of mushroom science in North Korea, with 12 papers. The number of research articles increased annually, from 7 in 1985, 12 in 1998, 11 in 2008, and 27 in 2020, and has especially increased rapidly since the mid-2010s. The study by mushroom type was as follows: 42 pine mushrooms (17.8 %), 25 oyster mushrooms (10.6 %), 23 Ganoderma sp. (9.8 %), 19 shiitake mushrooms (8.1 %), 17 button mushrooms (7.2 %), and 16 manna lichens (6.8 %). This study is considered meaningful in reviewing the research status and technology level in North Korea through analyzing North Korean academic journals in the field of mushroom science for the first time.

Anti-inflammatory effect in macrophages according to the mixing ratio of acemannan and aloesin (Acemannan과 aloesin의 혼합 비율에 따른 대식세포에서의 항염증 효과)

  • Hyo-Min Kim;Jeong-Hwan Kim;Dan-Hee Yoo;Se-Yeong Jeon;Hyun-Jin Kim;Seon-Gil Do;In-Chul Lee;Jung-Wook Kang
    • Food Science and Preservation
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    • v.31 no.2
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    • pp.315-323
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    • 2024
  • This study aims to confirm the anti-inflammatory activities of acemannan and aloesin, which have been studied for various efficacies at various mixed sample ratios. The mixed samples were mixed at a ratio of 1:1 (AA-1), 1:2 (AA-2), 1:3 (AA-3), 2:1 (AA-4), and 3:1 (AA-5). Seven samples were evaluated for their cytotoxic ability on macrophages, and the results showed that all cell viability was over 90% at a concentration of 100 ㎍/mL. First, due to the NO production inhibitory activity, a better inhibitory effect was achieved when using a mixed sample rather than a single material. Afterward, the activity of inhibiting the production of PGE2, TNF-α, and IL-6 was confirmed using a mixed sample. It was confirmed that AA-2 had the best inhibitory activity on producing PGE2, TNF-α, and IL-6 rather than AA-1, AA-3, AA-4, and AA-5. For this reason, experiments were conducted using AA-2 to determine the protein expression levels of iNOS and COX-2, which are inflammation-related proteins. It was confirmed that AA-2 inhibited iNOS and COX-2 protein expression by 25.01% and 27.27%, respectively, compared to the LPS-alone treatment group. In conclusion, the mixed sample of acemannan and aloesin is judged to have anti-inflammatory activity and can potentially to be used as a functional material.

Anti-wrinkle effects of solvent fractions from Jubak on CCD-986sk (CCD-986sk 세포 내 주박 분획물의 항주름 효능)

  • Young-Ah Jang;Hyejeong Lee
    • Journal of the Korean Applied Science and Technology
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    • v.41 no.2
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    • pp.508-519
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    • 2024
  • In this study, in order to evaluate the possibility of using Jubak as a functional cosmetic material, evaluation of antioxidant activity according to fractions and anti-wrinkle efficacy in CCD-986sk cells, a human fibroblast, were conducted. As a result of confirming the antioxidant activity by measuring ABTS+ radical scavenging ability, Jubak's Ethyl Acetate fractions was found to be 75.5% at a concentration of 1,000 ㎍/ml, showing the highest antioxidant activity among the extraction solvents. The wrinkle improvement effect was confirmed by measuring the inhibitory activity of elastase and collagenase, and in both test results, Jubak's Ethyl Acetate fractions showed the highest efficacy at a concentration of 1,000 ㎍/ml. As a result of measuring the synthesis rate of pro-collagen type I in CCD-986sk cells induced by UVB, Jubak showed the highest efficacy in the order of Ethyl Acetate, Water, Acetonitrile, and Hexan fractions at the same concentration of 20 ㎍/ml. As a result of measuring the inhibition rate of MMP-1, a collagen degrading enzyme, all four solvent fractions showed an efficacy of more than 70% at 20 ㎍/ml. As a result of measuring the mRNA expression levels of pro-collagen type I, MMP-1, and MMP-3 in a real-time PCR experiment, the protein expression level of pro-collagen type I increased when treated with Jubak fractions compared to the UVB group alone. The mRNA expression levels of MMP-1 and MMP-3 were confirmed to be decreased, and Ethyl Acetate fractions was the most effective in improving wrinkles after the control group (EGCG). As a result, it was confirmed that the Ethyl Acetate fractions among Jubak's solvent fractions has an anti-wrinkle effect against photoaging caused by UVB stimulation, and is expected to be used as a natural material for cosmetics.