• Microbiology and Biotechnology Letters
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• v.24 no.3
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• pp.380-383
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• 1996

Adenosine deaminase inhibitor was extracted from culture broth of Streptomyces sp. strain V-8 with ethylacetate. The ethylacetate extract showed the characteristic UV absorption spectrum of actinomycins at 440-450 nm. The ethylacetate extract was compared with respect to inhibitory behavior against adenosine deaminase from calf intestinal mucosa with actinomycin D, -C complex and actinomycin V. The Ki values for actnomycin D, -C complex, and actinomycin V against adenosine deaminase were determined to be 9.9 $\times$ 10$^{-6}$ M, 9.6 $\times$ 10$^{-6}$ M and 9.3 $\times$ 10$^{-6}$ M, respectively. The Ki value for the ethylacetate extract of culture broth against adenosine deaminase was determined to be 5.7 $\times$ 10$^{-6}$ M. The kinetic parameters of actinomycin D, -C complex, -V and ethylacetate extract of culture broth for adenosine deaminase were as follows:I$_{50}$ = 1.5 $\times$ 10$^{-5}$ M (actinomycin D), 2.7 $\times$ 10$^{-5}$ M (actinomycin C complex), 3.5 $\times$ 10$^{-5}$ M (actinomycin V), 8.9 $\times$ 10$^{-6}$ M (ethylacetate extract of culture broth). The adenosine deaminase was inhibited noncompetitively by ethylacetate extract of culture broth as well as by actinomycin D, -C complex and actinomycin V.

• Journal of Life Science
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• v.21 no.1
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• pp.141-145
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• 2011

Actinomycin D is a natural antibiotic that is used in anti-cancer chemotherapy and is known as a transcription inhibitor. Interestingly, actinomycin D induces phosphorylation of signal transducers and activators of transcription 3 (STAT3) in renal cancer Caki cells. In this study, we examined the molecular mechanism of actinomycin D-induced STAT3 phosphorylation. Treatment with actinomycin D induced phosphorylation of STAT3 (Tyr705) in a dose- and time-dependent manner. However, actinomycin D did not induce phosphorylation of STAT3 (Ser727), STAT1 (Tyr701) and STAT1 (Ser727). Moreover, actinomycin D-induced STAT3 phosphorylation was caused by decreased protein and mRNA levels of SOCS3, but not by JAK2 and SHP-1. In addition, other transcription inhibitor (5,6-dichloro-1-b-D-ribofuranosyl benzimidazole; DRB) also induced phosphorylation of STAT3 (Tyr705). Taken together, the present study demonstrates that transcriptional inhibitors (actinomycin D and DRB) induce phosphorylation of STAT3 (Tyr705) in Caki cells by down-regulation of SOCS3.

• Microbiology and Biotechnology Letters
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• v.22 no.2
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• pp.164-168
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• 1994

Identification of the Actinomycetes isolate strain No. 1372, a producer of Actinomycin X$_{2}$ was performed by using ISP method.l The strain, designated as No. 1372, was identified as Streptomyces floridae based on its morphological, physiological and biochemical characteristics. The highest production of the antibiotics by the strain was achieved in a fermentation medium containing soluble starch, yeast extract, (NH$_{4}$)SO$_{4}$, K$_{2}$HPO$_{4}$, NaCl$_{2}$, CaCO$_{3}$, and trace element.

• The Korean Journal of Zoology
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• v.26 no.4
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• pp.225-233
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• 1983

In order to know the mode of the action of gondotrophic hormone on the expansion of cumuli oophori, oocyte-cumulus complexes isolated from Graafian follicles of mice were stimulated to expand in vitro with human chorionic gonadotrophin (HCG), and the effects of puromycin and actinomycin D on the expansion were examined. THe complexes were cultured in medium TC 199 containing 10% bovine serum in the presence or absence of HCG and the inhibitors. Puromycin in the medium (0.5-4 $\\mu$g/ml) suppresseed the HCG-induced cumulus expansion dose-dependently. This effect of puromycin was reversible. Puromycin affected the complexes throughout the HCG-stimulating stage (3 hours) and hyaluronic acid synthesis stage (3-18 hours). Actinomycin D also inhibited the expansion of the cumulus from the concentration of 0.025 $\\mu$g/ml. But the effect of actinomycin D was not completely reversible and the drug appeared to give an irreversible damage to the complexes at 0.1 $\\mu$g/ml. From the above results, it is suggested that RNA or protein synthesis is involved in the process in which HCG stimulates the cumulus cells to expand therefore cAMP elevated by te gonadotrophin may control expansion at the transcriptional or translational level.

• Asian Pacific Journal of Cancer Prevention
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• v.16 no.8
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• pp.3351-3354
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• 2015

Background: Rhabdomyosarcoma (RMS) is the most common soft tissue sarcoma in the pediatric age group. All patients with RMS regardless of their initial stage or group receive combination chemotherapy as 'standard therapy' consisting of vincristine, actinomycin-D and cyclophosphamide. Actinomycin-D was not readily available in Turkey at one time. Carboplatin was used instead in order to prevent delays in treatment. The aim of this report is to present the results of patients with rhabdomyosarcoma receiving carboplatin or actinomycin-D therapy. Materials and Methods: Twenty four patients with rhabdomyosarcoma treated between December 2000 and June 2011 were included in this retrospective study. The patients were treated according to International Rhabdomyosarcoma Study Group guidelines. Eleven patients were treated with actinomycin-D and 13 with carboplatin ($250mg/m^2/dose$ for 2 days). The two groups were then compared in terms of 2- and 5-year overall survival (OS) and hematological and non-hematological toxicities. Results: Age, sex, stage and the mean duration of follow-up were similar in both groups (p>0.05). Two- and five-year OS levels were 68.2% in the carboplatin group and 78.0% and 40.0%, respectively, in the actinomycin-D group. There was no statistical difference in the number of febrile episodes (p=0.86) and no other hematological and non-hematological adverse effects were recorded in both groups. Conclusions: The findings show that carboplatin can be used as an alternative drug in the primary treatment of rhabdomyosarcoma in the event that actinomycin-D is unavailable or not tolerated.

• BMB Reports
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• v.36 no.3
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• pp.305-311
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• 2003

A modified actinomycin D was prepared with a hydroxyl group that replaced the amino group at the chromophore 2-position, a substitution known to strongly reduce affinity for double-stranded DNA. Interactions of the modified drug on single-stranded DNAs of the defined sequence were investigated. Competition assays showed that 2-hydroxyactinomycin D has low affinity for two oligonucleotides that have high affinities ($K_a\;=\;5-10{\times}10^6\;M^{-1}$ oligomer) for 7-aminoactinomycin D and actinomycin D. Primer extension inhibition assays performed on several single-stranded DNA templates totaling around 1000 nt in length detected a single high affinity site for 2-hydroxyactinomycin D, while many high affinity binding sites of unmodified actinomycin D were found on the same templates. The sequence selectivity of 2-hydroxyactinomycin D binding is unusually high and approximates the selectivity of restriction endonucleases. Binding appears to require a complex structure, including residues well removed from the polymerase pause site.

• Korean Journal Plant Pathology
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• v.12 no.1
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• pp.80-84
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• 1996

토양에서 분리한 방선균류(actinomycetes) GT103 균주의 배양여액 및 균체추출물은 담배의 주요 병원균인 담배 줄기속마름병균(Erwinia carotovora subsp. carotovora), 담배 탄저병균(Colletotrichum tabacum), 담배역병균(Phytophthora nicotianae var. nicotianae)등에 강한 항균활성을 보였다. 항균활성물질은 용매 추출, silica gel chromatography, HPLC 등을 실시하여 분리.정제하였으며 UV, IR, FAB-MS, \ulcornerH-NMR, \ulcornerC-NMR 분석결과 actinomycin group의 펩타이드계 항생 물질인 actinomycin C\ulcorner로 동정되었다. 이 활성물질의 담배 탄저병에 대한 방제효과는 50$\mu\textrm{g}$/ml 농도에서 100%, 10$\mu\textrm{g}$/ml 농도에서 90%의 방제효과를 보였다.

• Applied Microscopy
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• v.14 no.2
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• pp.1-14
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• 1984

Chick embryos received a single injection of actinomycin D($0.1{\mu}g,\;0.05{\mu}g\;or\;0.1{\mu}g$) or puromycin($10.0{\mu}g,\;30.0{\mu}g\;or\;50.0{\mu}g$) into the yolk sac of Arbor acres chick embryos either prior to incubation or at certain periods of time (48, 96 and 144 hours) after incubation. After 10days of incubation, surviving embryos were investigated morphologically and biochemically. Embryos treated with actinomycin D or puromycin showed a high mortality when they were exposed prior to incubation and at 48 hours after incubation. Electron micrographs of chondrocytes in tarso-metatarsal of antibiotics (actinomycin D or puromycin) treated embryos showed the destruction of cytoplasm and nuclei when they were exposed prior to incubation. Endoplasmic reticulum was expanded and mitochondria were damaged in chondrocytes of surving embryos treated with low doses at 48 hours, 96 hours or 144 hours after incubation. The activities of enzymes such as lactate dehydrogenase, malate dehydrogenase and succinate dehydrogenase in embryos treated with actinomycin D or puromycin were much less than those of the saline treated group. Also, the amounts of DNA, RNA and protein were greatly decreased.

• Applied Microscopy
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• v.15 no.1
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• pp.1-12
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• 1985

In this study, the pathway and date of migrating Primordial germ cells (PGCs) were observed light microscopically and ultrastructural changes of them during migration were observed by electron microscopic examination. For these purpose, alkaline phosphatase reactions were used for identifying the PGCs and acid phosphatase reactions were used for observing their degenerating activities. Also, effects of actinomycin D on the migration of PGCs were examined. According to these results, at the 9th gestation day, PGCs were observed in the endodermal cells of yolk sac, at the 11th gestation day, they were seen in the hindgut and then entered into the dorsal mesentery by the 13th gestation day. At the 14th gestation day, they were located in the genital ridges. When PGCs were located in the hindgut and genital ridges, the positive reactions of alkaline phosphatase were dominated, but acid phosphatase reactions were limited in all stage except they were in dorsal mesentery. However, these reactions were lessened in case of actinomycin D treatment. By electron microscopic examination, PGCs had pseudopodia, tail process, trailing cytoplasm and nuage as the ultrastructural characteristics. In addition, these morphological features were damaged by actinomycin D treatment.

• Proceedings of the Korean Society of Applied Pharmacology
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• 1994.04a
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• pp.268-268
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• 1994

포자의 전자현미경사진과 mycelium의 광학현미경사진을 찍어 strain V-8 균주의 형태학적인 특성을 조사하였을 때 방선균 계열인 streptomyces로 확인되었다. 이 균주의 배양액은 노란색을 띠고 있고 이 노란색은 430 nm에서 특징적인 흡광을 보였다. 이 물질은 유기 용매로 추출되었다. 이 물질의 자외선 흡광스펙트럼의 특징을 기존에 보고된 화합물과 비교하여 이 물질이 actinomycin계열에 속함을 발견하였다. 이 물질의 FAB mass spectrum에서 각 분획들의 주성분들의 분자의 질량 + H 이온이 1290과 1292에서 각각 관찰되었다. 이 화합물들은 분자량이 1258인 actinomycin D와는 상이한 구조를 소유하고 있는 것으로 확인되었다. 각 분획 성분들의 proton 및 carbon HIR spectra를 얻어 기존에 알려진 화합물의 자료와 비교하였을 때 actinomycin계열에 속하는 신물질로 생각되었다. 지금까지 actinomycin 계열의 항생물질이 adenosine deaminase의 효소 활성을 저해한다는 사실은 보고된바 없다. 본 연구자는 분리한 2개의 화합물에 대하여 구조 연구를 계속하고 있다.