• 생약학회지
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• 제29권1호
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• pp.22-27
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• 1998

This study was carried out to develop antitumor agents based on effects of the ethyl acetate soluble fraction of the methanolic extract of Lonicerae flos on human oral epitheloid carcinoma cells. Human oral epitheloid carcinoma cells were cultured in RPMI-1640 media containing 10% fetal bovine serum, antibiotic, and fungizone. After incubation for 24 hrs, the cells were treated with A, B, C, D, and E fractions for 48hrs under the same condition. MTT (3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazoliumbromide), NR (Neutral red) and SRB (Sulforhodamine B protein) assay were performed. The light microscopic findings were observed by inverted microscope. In MTT assay, fraction B was shown significant antitumor activity (P<0.001), fraction E was shown significant antitumor activities (P<0.05), but the other fractions were not shown. In NR assay, fraction B was shown significant antitumor activity (P<0.001). In SRB assay, fractions B was shown significant antitumor activities (P<0.01). fractions A and D were shown significant antitumor activities (P<0.05). but the other fractions were not shown. In light microscopy. the fraction B of the ethyl acetate soluble fraction of the methanolic extract of Lonicerae flos showed the highest antitumor activity. These finding suggested that fraction B possessed the most antitumorous agent.

• Bulletin of the Korean Chemical Society
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• 제30권11호
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• pp.2815-2818
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• 2009

• Biomolecules & Therapeutics
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• 제3권1호
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• pp.38-46
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• 1995

DA-125, a new anthracycline antitumor antibiotic, was administered at dose levels of 0, 0.04, 0.2 and 1.0 mg/kg/day intravenously to pregnant and subsequently delivered Sprague-Dawley rats from day 17 of gestation to day 21 of lactation. Effects of test agent on general toxicity of dams and growth, behaviour and mating performance of F1 offspring were examined. At 1 mg/kg, one out of the twentytwo dams showed difficult delivery, characterized by a stillbirth. Reduction in body weight, loss in food intake, and decrease in spleen weight were also observed in dams. In addition, the lower rates of successful performances in memory test (28.6%) and necrosis of tail end (9.5%) were seen in F1 offspring. At 0.04 and 0.2 mg/kg, no toxic effect on dams and F1 offspring was observed. There were no malformed Fl and F2 fetuses in all groups. The results indicate that the no effect dose levels(NOELs) of DA-125 are 0.2 mg/kg/day for dams and Fl offspring, and over 1 mg/kg/day for F2 fetuses.

• Biomolecules & Therapeutics
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• 제2권1호
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• pp.94-101
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• 1994

DA-125, a new anthracycline antitumor antibiotic, was at dose levels of 0, 0.03, 0.1 and 0.3 mg/kg/day administered intravenously to Sprague-Dawley male rats from premating to mating period and to females from premating to early gestation period. Effects of test agent on general findings and reproductive performance of parent animals and embryonic development were examined. No treatment-related changes in clinical signs, body weight, food consumption and necropsy findings were observed in all groups of both sexes. At 0.3 mg/kg, a decrease in the weight of spleen was found only in male rats. Mating performance and fertility of parent animals were not adversely affected by all doses tested. Fl fetuses showed no changes related to treatment of DA-125, except that at 0.3 mg/kg, an increase in the resorption rate was seen. The results show that the no effect dose levels (NOELS) for general toxicity of parent animals and fetal development are 0.1 mg/kg/day and NOELS for reproductive capability are over 0.3 mg/kg/day.

• Biomolecules & Therapeutics
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• 제2권1호
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• pp.82-93
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• 1994

DA-125, a new anthracycline antitumor antibiotic, was at dose levels of 0, 0.1, 0.3 and 1.0 mg/kg/day administered intravenously to pregnant Sprague-Dawley rats during the organogenetic period. Two-third of dams per group were subjected to caesarean section on day 20 of pregnancy and the remaining 10 dams per group were allowed to deliver. Effects of test substance on dams, embryonal development of Fl fetuses, as well as growth, behaviour and mating performance of Fl offspring were examined. 1. At 1 mg/kg, one out of the 10 dams showed difficult delivery. A decrease in food consumption, a loss in body weight and a decrease of spleen weight were found in this dose level group. At 0.3 mg/kg, difficult deliverys were observed in two out of the 10 dams. 2. At 1 mg/kg, an increased resorption rate and a decreased fetal weight were found. In addition, various types of external, visceral and skeletal malformations occurred at an incidence of 11.9, 41.8 and 14.5%, respectively. 3. At 1 mg/kg, body weight reduction, small eyeball, hydrocephalus and atrophy of sexual organs were observed in Fl offspring. One male pup receiving 0.3 mg/kg died on day 2 of lactation. The results show that the no-effect dose levels (NOELs) for dams and Fl offspring are 0.1 mg/kg/day and NOEL for Fl fetuses is 0.3 mg/kg/day.

• 대한화학회지
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• 제32권6호
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• pp.575-580
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• 1988

항암항생제 Rhodomycin(2)의 합성단계 최종물질인 (${\pm}$)-${\gamma}$-Rhodomycinone(4) 과 10-Deoxy-${\gamma}$-rhodomycinone(5)이 9-ethyl-9,10-epoxy-4,6, 11-trihydroxy-7,8,9,10-tetrahydronaphthacene-5,12-dione(10)의 epoxide ring 쪼개짐으로부터 만들어졌고, epoxide 10은 Hauser-Rhee가 개발한 고리접합법을 이용해서 만든 9-acetyl-4,5,6,11,12-pentamethoxy-7,8-dihydronaphthacene(6)으로 부터 얻었다.

• 대한화학회지
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• 제30권1호
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• pp.109-117
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• 1986

항암항생제 Daunorubicin(2a)합성단계의 최종물질인 7,9-Dideoxydaunomycinone (32)를 3-methoxybenzoic acid(5)로 부터 합성하였다. 3-methoxybenzoic acid를 4-methoxy-3-(phenylsulfonyl)-1(3H)-isobenzofuranone(11)으로 변형시킨 뒤 Hauser와 Rhee가 개발한 고리접합법을 이용하여 trimethoxynaphthoate 16을 얻은 후에 phenylsulfonylnaphthofuranone 22로 변화시킨 뒤 이 물질을 7-(ethylenedioxy)-2-octenoate(23)과 Michael형태의 반응을 전개시켜 anthracenoate 24를 얻었다. Anthracenoate을 tetracyclic 화합물 28로 바꾼뒤 ring B와 C에 붙은 methyl기들을 제거하여 7,9-Dideoxydaunomycinone(32)를 만들었다.

• Bulletin of the Korean Chemical Society
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• 제20권9호
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• pp.1078-1084
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• 1999

A synthetic cecropin A(1-13)-melittin(1-13) [CA-ME] hybrid peptide was known to be an antimicrobial peptide having strong antibacterial, antifungal and antitumor activity with minimal cytotoxic effect against human erythrocyte. Analogues were synthesized to investigate the influences of the flexible hinge region of CA-ME on the antibiotic activity. Antibiotic activity of the peptides was measured by the growth inhibition against bac-terial, fungal and tumor cells and vesicle-aggregating or disrupting activity. The deletion of Gln-Gly-Ile (P1) or Gly-Gln-Gly-Ile-Gly (P3) from CA-ME brought about a significant decrease on the antibiotic activities. In contrast, Gly-Ile-Gly deletion (P2) from CA-ME or Pro insertion (P5) instead of Gly-Gln-Gly-Ile-Gly of CA-ME retained antibiotic activity. This result indicated that the flexible hinge or β-bend structure provided by Gly-Gln-Gly-Ile-Gly, Gln-Gly, or Pro in the central region of the peptides is requisite for its effective antibiotic activity and may facilitate easily the hydrophobic C-terminal region of the peptide to penetrate the lipid bilayers of the target cell membrane. In contrast, P4 and P6 with Gly-Gln-Gly-Pro-Gly or Gly-Gln-Pro in the central region of the peptide caused a drastic reduction on the antibiotic activities. This result suggested that the con-secutive β-bend structure provided by Gly-Gln-Gly-Pro-Gly or Gly-Gln-Pro in the central hinge region of the peptide seems to interrupt the ion channel/pore formation on the target cell membranes.

• 한국생물물리학회:학술대회논문집
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• 한국생물물리학회 1999년도 학술발표회 진행표 및 논문초록
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• pp.32-32
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• 1999

Cecropin A(1-8)-magainin 2(1-12) and cecropm A(1-8)-melittin(1-12) hybrid peptides were known to have potent antitumor and antibacterial activity. In particular, cecropm A(l-8)-magainin 2(1-12) has powerful antibacterial and antitumor activity with no hemolytic effect.(omitted)

• Biomolecules & Therapeutics
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• 제1권2호
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• pp.226-235
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• 1993

DA-125, a new anthracycline antitumor antibiotic, was administered to Sprague-Dawley rats intravenously for 4 weeks to investigate the repeated dose toxicity Focal alopecia was noted in three female rats receiving 1.0mg/kg/day. In rats receiving 1.0 mg/kg/day, weight gain decreased in both sexes after first or second week. Hematological examination revealed lower counts of total leukocyte and increased numbers of platelet after second week. At terminal necropsy, atrophy of thymus and spleen was observed. Lymphocytic depletion of thymus and atrophy of white pulp in spleen were observed microscopically. A decrease in the number of hematopoietic cells in the bone marrow and degeneration of germinal epithelia in testes were also observed. These treatment-related effects were mainly confined to rats receiving 1.0 mg/kg/day. And toxic effects with microscopic changes were not observed in rats receiving 0.2 mg/kg/day or 0.04 mg/kg/day.