EM2487, a novel anti-HIV-1 antibiotic, produced by Streptomyces sp. Mer-2487: taxonomy, fermentation, biological properties, isolation and structure elucidation.

作者: HITOSHI TAKEUCHI , NAOKI ASAI , KAZUNORI TANABE , TERUYA KOZAKI , MASANORI FUJITA

DOI: 10.7164/ANTIBIOTICS.52.971

关键词:

摘要: For the purpose of discovering novel agents that inhibit HIV-1 replication at transcriptional level, we have established cell lines reflecting long terminal repeat-driven gene expression. Using these lines, screened approximately 10,000 microorganism products and found culture supernatant Streptomyces sp. Mer-2487 suppresses Tat-induced expression without affecting basal or tumor necrosis factor-alpha-induced transcription. The purified active component has a unique structure, as shown in Fig. 1. This compound an inhibitory effect on chronically infected cells well acutely cells, suggesting inhibition occurs postintegration step proviral DNA cycle.

参考文章(18)
Masanori Baba, Cellular factors as alternative targets for inhibition of HIV-1 Antiviral Research. ,vol. 33, pp. 141- 152 ,(1997) , 10.1016/S0166-3542(96)01010-8
K T Jeang, B Berkhout, B Dropulic, Effects of integration and replication on transcription of the HIV-1 long terminal repeat. Journal of Biological Chemistry. ,vol. 268, pp. 24940- 24949 ,(1993) , 10.1016/S0021-9258(19)74555-4
T. G. Pridham, David Gottlieb, The Utilization of Carbon Compounds by Some Actinomycetales as an Aid for Species Determination Journal of Bacteriology. ,vol. 56, pp. 107- 114 ,(1948) , 10.1128/JB.56.1.107-114.1948
W A O'Brien, M Sumner-Smith, S H Mao, S Sadeghi, J Q Zhao, I S Chen, Anti-Human Immunodeficiency Virus Type 1 Activity of an Oligocationic Compound Mediated via gp120 V3 Interactions Journal of Virology. ,vol. 70, pp. 2825- 2831 ,(1996) , 10.1128/JVI.70.5.2825-2831.1996
KIYOSHI ISONO, MASAKAZU URAMOTO, HIROO KUSAKABE, KEN-ICHI KIMURA, KAZUO IZAKI, CHAD C. NELSON, JAMES A. MCCLOSKEY, Liposidomycins: novel nucleoside antibiotics which inhibit bacterial peptidoglycan synthesis. The Journal of Antibiotics. ,vol. 38, pp. 1617- 1621 ,(1985) , 10.7164/ANTIBIOTICS.38.1617
M Witvrouw, R Pauwels, A M Vandamme, D Schols, D Reymen, N Yamamoto, J Desmyter, E De Clercq, Cell type-specific anti-human immunodeficiency virus type 1 activity of the transactivation inhibitor Ro5-3335. Antimicrobial Agents and Chemotherapy. ,vol. 36, pp. 2628- 2633 ,(1992) , 10.1128/AAC.36.12.2628
KIYOSHI ISONO, Nucleoside antibiotics: structure, biological activity, and biosynthesis The Journal of Antibiotics. ,vol. 41, pp. 1711- 1739 ,(1988) , 10.7164/ANTIBIOTICS.41.1711
Rudi Pauwels, Jan Balzarini, Masanori Baba, Robert Snoeck, Dominique Schols, Piet Herdewijn, Jan Desmyter, Erik De Clercq, Rapid and automated tetrazolium-based colorimetric assay for the detection of anti-HIV compounds Journal of Virological Methods. ,vol. 20, pp. 309- 321 ,(1988) , 10.1016/0166-0934(88)90134-6
Makoto. Ubukata, Kiyoshi. Isono, Kenichi. Kimura, Chad C. Nelson, James A. McCloskey, The structure of liposidomycin B, an inhibitor of bacterial peptidoglycan synthesis Journal of the American Chemical Society. ,vol. 110, pp. 4416- 4417 ,(1988) , 10.1021/JA00221A052