R1128 SUBSTANCES, NOVEL NONSTEROIDAL ESTROGEN-RECEPTOR ANTAGONISTS PRODUCED BY A STREPTOMYCES .1. TAXONOMY, FERMENTATION, ISOLATION AND BIOLOGICAL PROPERTIES

被引：21

作者：

HORI, Y

ABE, Y

EZAKI, M

GOTO, T

OKUHARA, M

KOHSAKA, M

机构：

[1] Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd., Ibaraki,300-26, 5-2-3 Tokodai, Tsukuba

来源：

JOURNAL OF ANTIBIOTICS | 1993年 / 46卷 / 07期

关键词：

D O I：

10.7164/antibiotics.46.1055

中图分类号：

Q81 [生物工程学（生物技术）]; Q93 [微生物学];

学科分类号：

071005 ; 0836 ; 090102 ; 100705 ;

摘要：

New non-steroidal estrogen-receptor antagonists, R1128 A, B, C and D, were isolated from the cultured broth of Streptomyces sp. No. 11 28 by solvent extraction, silica gel chromatography, reverse phase chromatography and preparative HPLC. These compounds inhibited estrogen binding to its receptor. The IC50 values of R1128 A, B, C and D for partially purified rat uterine cytosol receptor were 1.1 x 10(-7)m, 1.2 x 10(-7)m, 2.6 x 10(-7)m and 2.7 x 10(-7)m, respectively.

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页码：1055 / 1062

页数：8

相关论文

共 19 条

[1] CHEMICAL COMPOSITION OF CELL-WALL PREPARATIONS FROM STRAINS OF VARIOUS FORM-GENERA OF AEROBIC ACTINOMYCETES [J].

BECKER, B ;

LECHEVALIER, MP ;

LECHEVALIER, HA .

APPLIED MICROBIOLOGY, 1965, 13 (02) :236-+

[2] NOVEL CHOLECYSTOKININ ANTAGONISTS FROM ASPERGILLUS-ALLIACEUS .1. FERMENTATION, ISOLATION, AND BIOLOGICAL PROPERTIES [J].

GOETZ, MA ;

MONAGHAN, RL ;

CHANG, RSL ;

ONDEYKA, J ;

CHEN, TB ;

LOTTI, VJ .

JOURNAL OF ANTIBIOTICS, 1988, 41 (07) :875-877

[3] WS9326A, A NOVEL TACHYKININ ANTAGONIST ISOLATED FROM STREPTOMYCES-VIOLACEUSNIGER NO-9326 [J].

HAYASHI, K ;

HASHIMOTO, M ;

SHIGEMATSU, N ;

NISHIKAWA, M ;

EZAKI, M ;

YAMASHITA, M ;

KIYOTO, S ;

OKUHARA, M ;

KOHSAKA, M ;

IMANAKA, H .

JOURNAL OF ANTIBIOTICS, 1992, 45 (07) :1055-1063

[4] R1128 SUBSTANCES, NOVEL NONSTEROIDAL ESTROGEN-RECEPTOR ANTAGONISTS PRODUCED BY A STREPTOMYCES .2. PHYSICOCHEMICAL PROPERTIES AND STRUCTURE DETERMINATION [J].

HORI, Y ;

TAKASE, S ;

SHIGEMATSU, N ;

GOTO, T ;

OKUHARA, M ;

KOHSAKA, M .

JOURNAL OF ANTIBIOTICS, 1993, 46 (07) :1063-1068

[5] R1128 SUBSTANCES, NOVEL NONSTEROIDAL ESTROGEN-RECEPTOR ANTAGONISTS PRODUCED BY A STREPTOMYCES .3. PHARMACOLOGICAL PROPERTIES AND ANTITUMOR ACTIVITIES [J].

HORI, Y ;

ABE, Y ;

NISHIMURA, M ;

GOTO, T ;

OKUHARA, M ;

KOHSAKA, M .

JOURNAL OF ANTIBIOTICS, 1993, 46 (07) :1069-1075

[6] ENDOTHELIN-BINDING INHIBITORS, BE-18257A AND BE-18257B .1. TAXONOMY, FERMENTATION, ISOLATION AND CHARACTERIZATION [J].

KOJIRI, K ;

IHARA, M ;

NAKAJIMA, S ;

KAWAMURA, K ;

FUNAISHI, K ;

YANO, M ;

SUDA, H .

JOURNAL OF ANTIBIOTICS, 1991, 44 (12) :1342-1347

[7] BE-14348 SUBSTANCES, NEW SPECIFIC ESTROGEN-RECEPTOR BINDING INHIBITORS - PRODUCTION, ISOLATION, STRUCTURE DETERMINATION AND BIOLOGICAL PROPERTIES [J].

KONDO, H ;

NAKAJIMA, S ;

YAMAMOTO, N ;

OKURA, A ;

SATOH, F ;

SUDA, H ;

OKANISHI, M ;

TANAKA, N .

JOURNAL OF ANTIBIOTICS, 1990, 43 (12) :1533-1542

[8]

Kornerup A., 1978, METHUEN HDB COLOUR, V3rd

[9]

LECHEVALIER M P, 1970, International Journal of Systematic Bacteriology, V20, P435

[10]

Lechevalier MP, 1980, ACTINOMYCETE TAXONOM, V6, P227