• 한국미생물·생명공학회지
• /
• 제23권3호
• /
• pp.329-336
• /
• 1995

For the development of new antitumor antibiotics produced by microorganisms, Streptomyces sp. YBE-316 was isolated from soil. The productivity of the antitumor antibiotic from Streptomyces sp. YBE-316 gradually increased after 60 hours, and was maximum after 100 hours after inoculation in growth medium (2.0% sucrose, 1.0% soybean meal, 0.1% K$_{2}$HPO$_{4}$, pH 7.0) at 30$\circ$C, 150 rpm, 5 NL/min by 30 l jar fermentor. This antitumor antibiotic was present only in mycelium, and stable in pH 5.0-10.0 for 20 minutes at 100$\circ$C. Antitumor and antibiotic activities were maintained at neutral pH, and heat stability was low. This antitumor antibiotic was soluble in methanol and ethanol, and insoluble in water, ethyl acetate, chloroform, and n-hexane. This antitumor antibiotic was sequentially purified by acetone extraction from mycelium, butanol extraction, and silica gel column chromatography. Antitumor activity was low against most tested cell lines, but antibiotic activity was high and low against yeasts and bacteria, respectivelv. The visualization test showed that this antitumor antibiotic had higher hydroxyl, ketone, amino, carboxyl groups, and sugar(s) in its structure. Instrumental analyses showed that this antitumor antibiotic was a pentaene in polyene class antibiotics. In pentaene class antibiotics, this was considered as an eurocidin or capacidin type antibiotics. The molecular weight of this antitumor antibiotic was higher than 683.0 daltons, and this antitumor antibiotic might be glycosylated by other sugar(s), instead of mycosamine or perosamine, an amino sugar.

• 한국미생물·생명공학회지
• /
• 제23권3호
• /
• pp.297-303
• /
• 1995

Antitumor antibiotic material was produced by Streptomyces sp. YBE-316 which was isolated from soil, and the optimal culture conditions for the antitumor antibiotic material production were as follows; 2.0% (w/v) sucrose, 0.8% (w/v) polypeptone, 0.4% (w/v) yeast extract, 0.2% (w/v) K$_{2}$HPO$_{4}$, pH 7.0, at 30$\circ$C, 150 rpm and for 100 hours culture. The antitumor antibiotic material had strong antitumor antibiotic activities against most testing tumor cell lines, gram positive and negative bacteria, yeasts, and, especially, Penicillium chrysogenum in fungi.

• Journal of Microbiology and Biotechnology
• /
• 제5권1호
• /
• pp.31-35
• /
• 1995

An antitumor antibiotic named YS-1649 was isolated from the culture filtrate of a newly isolated fungus identified as Penicillium sp.. The fermentation yield reached about 40 mg per liter of the broth. YS-1649, a $\gamma$-Iactone - structured antibiotic, has the molecular fomular of $C_7H_6O_4$, Its structure was determined to be patulin by spectral analysis. It is active against some bacteria and showed cytotoxic effect on the proliferation of human breast cancer cell line, MCF-7, at concentrations of more than 0.048 $mu g/ml$. This compound also showed strong cytotoxic effect on the proliferation of human cancer cell lines, A549 and ACHN.

• 한국미생물·생명공학회지
• /
• 제23권5호
• /
• pp.599-601
• /
• 1995

A cytotoxic compound, MCHS-4, was isolated from the mycelium of Streptomyces T70 and identified as manumycin A. The compound showed significant cytotoxicity against human gastric carcinoma cell line, SNU-1 and human hepatocellular cell line, SNU-354.

• BMB Reports
• /
• 제32권6호
• /
• pp.561-566
• /
• 1999

CA(1-8)-ME(1-12) [CA-ME], composed of cecropin A(1-8) and melittin(1-12), is a synthetic antimicrobial peptide having potent antibacterial and antitumor activities with minimal hemolytic activity. In order to investigate the effects of the flexible hinge sequence, Gly-Ile-Gly, of CA-ME on antibiotic activity, CA-ME and three analogues, CA-ME1, CA-ME2, and CA-ME3, were synthesized. The Gly-Ile-Gly sequence of Ca-ME was deleted in CA-ME1 and replaced with Pro and Gly-Pro-Gly in CA-ME2 and CA-ME3, respectively. CA-ME1 and CA-ME3 showed a significant decrease in antitumor activity and phospholipid vesicle-disrupting ability. However, CA-ME2 showed similar antitumor and vesicle-disrupting activities, as compared with CA-ME. These results suggest that the flexibility or ${\beta}$-turn induced by Gly-Ile-Gly or Pro in the central part of CA-ME may be important in the electrostatic interaction of the N-terminus cationic ${\alpha}$-helical region with the cell membrane surface and the hydrophobic interaction of the C-terminus amphipathic ${\alpha}$-helical region with the hydrophobic acyl chains in the cell membrane. CA-ME3 exhibited lower antitumor and vesicle-disrupting activities than CA-ME and CA-ME2. This result suggests that the excessive ${\beta}$-turn structure caused by the Gly-Pro-Gly sequence in CA-ME3 seems to interrupt ion channel/pore formation in the lipid bilayer. We concluded that the appropriate flexibility or bilayer. We concluded that the appropriate flexibility or ${\beta}$-turn structure provided by the central hinge is responsible for the effective antibiotic activity of the antimicrobial peptides with the helix-hinge-helix structure.

• Biomolecules & Therapeutics
• /
• 제3권1호
• /
• pp.47-53
• /
• 1995

DA-125, a new anthracycline antitumor antibiotic, was administered at dose levels of 0, 0.2, 0.6 and 1.8 mg/kg/day intravenously to pregnant New Zealand White rabbits from day 6 through 18 of gestation. The does were subjected to the caesarean section on day 28 of gestation. Effects of test agent on general toxicity of does and embryonic development of F1 fetuses were examined. At 1.8 mg/kg, the organ weight for ovary of does was significantly decreased. The decrease in the number of corpus lutea, implantations and litter size, and the increase in the rate of resorptions were also observed. In addition, various types of external, visceral and skeletal malformations occurred in fetuses at an incidence of 7.7, 7.7 and 20.6%, respectively. The results show that the no effect dose levels (NOELs) of DA-125 are 0.6 mg/kg/day for does and F1 fetuses.

• 한국미생물·생명공학회지
• /
• 제18권4호
• /
• pp.331-337
• /
• 1990

토양에서 새로히 분리한 곰팡이를 배양하고 그의 배양액 중에 함암활성을 갖는 물질을 screening한 결과 시험균 B.subtilis에 대해 항균활성을 갖고 glutathoine에 의해 항균활성이 길항되는 물질을 생산하는 B-1123 균주를 얻었다. 생산균주의 형태학적, 배양학적 성상의 관찰 결과 B-1123 균주는 Aspergillus terreus로 동정되었다. 대두분을 질소원으로 한 배지에서 $30^{\circ}C$, 5일간 진탕배양하고 배양여액 중의 활성물질을 ethyl acetate로추출하고 silica gel column chromatography에 의해 정제 하여 연황색 판상결정을 얻었으며 B-1123 물질이라 명명했다.

• BMB Reports
• /
• 제33권1호
• /
• pp.49-53
• /
• 2000

PMAP-23 is a 23-residue antimicrobial peptide derived from porcine myloid cells. In order to investigate the effects of two Pro residues at positions 12 and 15 of PMAP-23 on antibiotic activity, two analogues in which Ala was substituted for Pro residue at position 12 or 15 were synthesized. $Pro^{12}{\rightarrow}Ala$ (PMAPl) or $Pro^{15}{\rightarrow}Ala$(PMAP2) substitution in PMAP-23 caused a significant reduction on antitumor and phospholipid vesicle-disrupting activities, but did not cause a significant effect on antibacterial activity. PMAP-23 displayed the type I ${\beta}-turn$ structure with a negative ellipticity at near 205 om in SDS micelle, whereas PMAP1 and PMAP2 had a somewhat ${\alpha}-helical$ propensity in TFE solution, as compared to PMAP-23. These results suggest that two Pro residues of positions 12 and 15 in PMAP-23 play important roles in the formation of ${\beta}-turn$ structure on lipid membrane and its ${\beta}-turn$ structure may be essential for antibiotic activity including phospholipid vesicle-disrupting property.

• 한국식품영양과학회:학술대회논문집
• /
• 한국식품영양과학회 2001년도 International Symposium on Food,Nutrition and Health for 21st Century
• /
• pp.161-169
• /
• 2001

Lactic acid producing bacteria were isolated from baby feces and characterized to be used as a probiotic with anti Helicobacter pylori functions. The selected bacteria had inhibition activity on the adherance and growth of H. pylori. These bacteria had additional beneficial characteristics for the probiotic such as antibacterial activity, antitumor activity, immunostimulation activity, resistance to antibiotic and bile salt, ability to bind to the intestinal cells, and safe for the human use.

• 한국미생물·생명공학회지
• /
• 제22권2호
• /
• pp.169-174
• /
• 1994

Antitumor antibiotic HS-1 was purified from the culture broth of a streptomyces floridae SHS-1372 which had been isolated from soil, by solvent extraction, silica gel column chromatography and gel filtration. It was confirmed that HS-1 was active against gram positive bacteria and cancer cells(K562, P388, MCF-7, HT-29). Through the analysis of UV spectrum, melting point, IR spectrum, FAB-MS, $_{1}$H-NMR, $_{13}$C-NMR, 2D-NMR spectra, HS-1 could be identified sa the actinomycin X$_{2}$ antibiotics containing actinocine chromophore and peptides consisted of threonine, proline, methylvaline, sarcosine, D-valine and 4-ketoproline.