-
HAO H. SUN, COLIN J. BARROW, DAVID M. SEDLOCK, AMANDA M. GILLUM, RAYMO ...
1994 年 47 巻 5 号 p.
515-522
発行日: 1994/05/25
公開日: 2006/04/19
ジャーナル
フリー
In the course of screening microbial broths for neurokinin receptor antagonists, a series of new benzodiazepines, benzomalvins A (
1), B (
2) and C (
3), has been isolated from the culture broth of a fungus identified as a
Penicillium sp. Benzomalvin A (
1) showed inhibitory activity against substance P with
Ki values of 12, 42 and 43 fXM at the guinea pig, rat and human neurokinin NK1 receptors, respectively. Benzomalvins B (
2) and C (
3) were only weakly active. The structures of these compounds were determined by spectroscopic methods including MS measurements and NMR analysis.
抄録全体を表示
-
I. THE PRODUCING ORGANISM, FERMENTATION AND BIOLOGICAL ACTIVITY
MARIANNA JACKSON, NEAL S. BURRES, JAMES P. KARWOWSKI, LISA A. ALDER, P ...
1994 年 47 巻 5 号 p.
523-527
発行日: 1994/05/25
公開日: 2006/04/19
ジャーナル
フリー
A radioligand test to detect inhibitors of endothelin-1 binding to its receptors in bovine atrial and porcine cerebral membranes was used to screen fungal metabolites from stationary fermentations. Inhibitory activity, observed in culture extracts of two
Acremonium species, led to the discovery of aselacins A, B and C. Aselacin A inhibits binding to both membrane fractions with IC
50s of approximately 20 μg/ml.
抄録全体を表示
-
II. ISOLATION AND ELUCIDATION OF STRUCTURES
JILL E. HOCHLOWSKI, PRESTON HILL, DAVID N. WHITTERN, MICHAEL H. SCHERR ...
1994 年 47 巻 5 号 p.
528-535
発行日: 1994/05/25
公開日: 2006/04/19
ジャーナル
フリー
Three novel compounds, named the aselacins, which inhibit the binding of endothelin to its receptor have been isolated from two related
Acremonium species of fungi grown in stationary culture. These compounds are cyclic pentapeptolides with a ring formed by cyclo[Gly-D-Ser-D-Trp-β-Ala-L-Thr] and an additional exocyclic D-Gln to which is attached a functionalized long chain fatty acid. The aselacins differ in the functionalization of this acid. The structures of the aselacins were determined by amino acid analysis, mass spectrometry and evaluation of 1-D and 2-D homonuclear and heteronuclear
1H,
13C and
15N NMR spectra in protic and aprotic solvents. The stereochemistry of the amino acids present was elucidated by chiral HPLC of hydrolyzed compound.
抄録全体を表示
-
I. TAXONOMY, FERMENTATION, ISOLATION AND BIOLOGICAL ACTIVITIES
MASAHIDE AMEMIYA, MITSUHIRO UENO, MICHIYO OSONO, TOHRU MASUDA, NAOKO K ...
1994 年 47 巻 5 号 p.
536-540
発行日: 1994/05/25
公開日: 2006/04/19
ジャーナル
フリー
Cytostatin has been identified as a novel inhibitor of cell adhesion to components of extracellular matrix (ECM) in cultured broth of
Streptomyces sp. MJ654-NF4. Though cytostatin did not inhibit EL-4 cell adhesion to ECM components such as laminin and fibronectin, it inhibited the adhesion of B16 melanoma cells to laminin and collagen type IV but not to fibronectin. It exhibited antimetastatic activity on B16 melanoma cells in mice. The cytotoxicity of cytostatin are also reported.
抄録全体を表示
-
II. PHYSICO-CHEMICAL PROPERTIES AND STRUCTURE DETERMINATION
MASAHIDE AMEMIYA, TETSUYA SOMENO, RYUICHI SAWA, HIROSHI NAGANAWA, MASA ...
1994 年 47 巻 5 号 p.
541-544
発行日: 1994/05/25
公開日: 2006/04/19
ジャーナル
フリー
The structure of cytostatin was determined to be 5, 6-dihydro-5-methyl-6-(6-hydroxy-1, 5-dimethyl-4-phosphonooxy-7, 9, 11-tridecatrienyl)-2
H-pyran-2-one sodium salt on the basis of physico-chemical properties and NMR studies.
抄録全体を表示
-
TAKASHI HORIGUCHI, Kozo HAYASHI, SHIGETOSHI TSUBOTANI, SHIGEMI IINUMA, ...
1994 年 47 巻 5 号 p.
545-556
発行日: 1994/05/25
公開日: 2006/04/19
ジャーナル
フリー
New naphthacenecarboxamide antibiotics, TAN-1518 A and B, were isolated from a culture broth of
Streptomyces sp. AL-16012. Their structures were elucidated from their reactions and from spectroscopic analyses. The relaxation of supercoiled pBR322 DNA by calf thymus DNA topoisomerase I was inhibited by these metabolites as potently as by camptothecin. However, the decatenation of kinetoplast DNA by calf thymus DNA topoisomerase II was little affected by these agents. The major metabolite, TAN-1518 A, strongly suppressed the growth of various murine and human tumor cells, inducing apoptosis. Unlike camptothecin, TAN-1518 A did not stimulate cleavable complex formation in the nuclei of CHO-K1 cells and had weak activity in intercalating into DNA strands. This metabolite arrested the growth of human tumor cell lines in Gl phase of the cell cycle. These results suggest that TAN-1518 A and B are novel antitumor agents targeting topoisomerase I.
抄録全体を表示
-
TSUNEO ASANO, KUNIO MATSUOKA, TSUNEAKI HIDA, MAKOTO KOBAYASHI, YUMIKO ...
1994 年 47 巻 5 号 p.
557-565
発行日: 1994/05/25
公開日: 2006/04/19
ジャーナル
フリー
Four kinds of retrovirus protease inhibitors (RPI-856 A, B, C and D) were isolated as white powder from the culture filtrate of a soil isolate,
Streptomyces sp. AL-322 by column chroma-tography using Diaion HP-20, Sephadex LH-20, ODS reversed phase HPLC and SP-2SW ion exchange HPLC. The structures of these inhibitors were elucidated by physico-chemical properties, chemical reactions and spectral analyses, as valyl-ADPAA-leucyl-AOPBA-valyl-valyl-aspartic acid (RPI-856 A and B) and valyl-ADPAA-leucyl-AOPBA-valyl-valine (RPI-856 C and D) [ADPAA = 2-amino-2-(3, 5-dihydroxyphenyl)acetic acid, AOPBA = 3-amino-2-oxo-4-phenylbutyric acid]. RPI-856 A and B, and RPI-856 C and D were both determined to be diastereomers each other on the asymmetric carbon in AOPBA. These four inhibitors strongly inhibited
in vitro HIV-1 protease and HTLV-I protease both derived from recombinant
Escherichia coli with IC
50 ofl0-
7-
10-8M.
抄録全体を表示
-
TSUTOMU SATO, KOJI NAGAI, MITSUYOSHI SHIBAZAKI, KENJI ABE, YUKIHIRO TA ...
1994 年 47 巻 5 号 p.
566-570
発行日: 1994/05/25
公開日: 2006/04/19
ジャーナル
フリー
Novel pepstatin A-sensitive
Candida albicans aspartyl protease inhibitors, named YF-0200R-A and B, were isolated by column chromatography and preparative HPLC from the fermentation broth of
Streptomyces sp. YF-0200R. The structures of YF-0200R-A and B were elucidated by spectroscopic analysis as α, β and γ, δ unsaturated fatty acids with two or three hydroxyl groups. YF-0200R-A and B inhibit aspartyl protease from
Candida albicans with IC
50 values of 6.5×10
-4M and 6.2×10
-4M, respectively.
抄録全体を表示
-
SHUICHI GOMI, KEI-ICHI IMAMURA, TAKASHI YAGUCHI, Yosmo KODAMA, NOBUTO ...
1994 年 47 巻 5 号 p.
571-580
発行日: 1994/05/25
公開日: 2006/04/19
ジャーナル
フリー
A new insecticidal compound PF1018 was isolated from the culture broth of
Humicola sp. It exhibited insecticidal activity against a wide range of critical pest species. The structure of PF1018 was determined to be (7a
S)-2-((2
E)-l-hydroxy-3-((1
S, 3a
R, 4
R, 5
R, 7a
R)-3a, 4, 5, 7a-tetrahydro-1, 3, 5, 7-tetramethyl-5, 1-((3
S)-(
Z)-2, 3-dimethylpropeno)-1
H-inden-4-yl)-2-propenylidene)pyrrolizidine1, 3-dione, by NMR spectral analyses coupled with X-ray crystallographic analysis and chemical degradation study.
抄録全体を表示
-
AMALIA NARANDJA, BOZIDAR ŠUŠKOVIC, ZELJKO KELNERIC, SLOB ...
1994 年 47 巻 5 号 p.
581-587
発行日: 1994/05/25
公開日: 2006/04/19
ジャーナル
フリー
Tetra-, hexa-and octahydro derivatives of tylosin were prepared by the reduction of the conjugated double bond and carbonyl groups. Hydrogenation of the diene did not change the
in vitro antimicrobial activity of compounds, while reduction of carbonyls causes small or complete loss of activity.
抄録全体を表示
-
TSUTOMU SATO, MITSUYOSHI SHIBAZAKI, HIROSHI YAMAGUCHI, KENJI ABE, HISA ...
1994 年 47 巻 5 号 p.
588-590
発行日: 1994/05/25
公開日: 2006/04/19
ジャーナル
フリー
-
KAZUYA SAKAI, HIROYUKI CHIBA, REI KANETO, MICHIKO SAKAMOTO, KAZUHIKO O ...
1994 年 47 巻 5 号 p.
591-594
発行日: 1994/05/25
公開日: 2006/04/19
ジャーナル
フリー
-
SUGATA CHATTERJEE, S. R. NADKARNI, E. K. S. VIJAYAKUMAR, M. V. PATEL, ...
1994 年 47 巻 5 号 p.
595-598
発行日: 1994/05/25
公開日: 2006/04/19
ジャーナル
フリー
-
HAO H. SUN, STEPHEN J. BYARD, RAYMOND COOPER
1994 年 47 巻 5 号 p.
599-601
発行日: 1994/05/25
公開日: 2006/04/19
ジャーナル
フリー
-
KUNIAKI TATSUTA, MANABU ITOH
1994 年 47 巻 5 号 p.
602-605
発行日: 1994/05/25
公開日: 2006/04/19
ジャーナル
フリー
-
HOKOON PARK, JAE YEOL LEE, YONG SUP LEE, JONG OK PARK, SUNG BO KOH, WO ...
1994 年 47 巻 5 号 p.
606-608
発行日: 1994/05/25
公開日: 2006/04/19
ジャーナル
フリー
-
YONG SUP LEE, JAE YEOL LEE, SUN HO JUNG, EUN-RHAN WOO, DAE HWAN SUK, S ...
1994 年 47 巻 5 号 p.
609-612
発行日: 1994/05/25
公開日: 2006/04/19
ジャーナル
フリー
-
NAN-JIN WANG, BAO-LING HAN, NORIYUKI YAMASHITA, MASAYA SATO
1994 年 47 巻 5 号 p.
613-615
発行日: 1994/05/25
公開日: 2006/04/19
ジャーナル
フリー
-
MARIKO NAKAMURA, HITOSHI HONMA, MINORI KAMADA, TSUNEYA OHNO, SETSUKO K ...
1994 年 47 巻 5 号 p.
616-618
発行日: 1994/05/25
公開日: 2006/04/19
ジャーナル
フリー