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SATOSHI NAKANISHI, KATSUHIKO ANDO, ISAO KAWAMOTO, YUZURU MATSUDA
1993 Volume 46 Issue 12 Pages
1775-1781
Published: December 25, 1993
Released on J-STAGE: April 19, 2006
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MS-347a was isolated from the culture broths of
Aspergillus sp. KY52178 as an inhibitor of smooth muscle myosin light chain kinase (MLCK). MS-347a inhibited the activity of chicken gizzard MLCK with an IC
50 value of 9.2 μM. The inhibition was dependent on time of preincubation of MS-347a with the enzyme, suggesting irreversible inhibition. It is likely that the inhibitor binds to the catalytic domain of MLCK, since the compound inhibited not only calmodulin-dependent but also calmodulin-independent activity of MLCK. Calmodulin-dependent cyclic nucleotide phosphodiesterase, cAMP-dependent protein kinase and cGMP-dependent protein kinase were not inhibited by 150μM MS-347a at all, although the compound inhibited protein kinase C with an IC
50 value of 16μM. MS-347b, a minor component was also isolated from the same culture broths. This minor component at 150μM did not inhibit the activity of MLCK.
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KEIJI HASUMI, CHIKARA SHINOHARA, TAKASHI IWANAGA, AKIRA ENDO
1993 Volume 46 Issue 12 Pages
1782-1787
Published: December 25, 1993
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A new inhibitor of acyl-Co A:cholesterol acyltransferase (ACAT), designated lateritin, was isolated from the mycelial cake of
Gibberella lateritium IFO 7188 by successive purification procedure of solvent extraction, silica gel column chromatography and reverse phase HPLC. Spectroscopic analyses of the compound yielded 4-methyl-6-(1-methylethyl)-3-phenylmethyl-1, 4-perhydrooxazine2, 5-dione as the proposed structure. Lateritin inhibited rat liver ACAT activity by 50% at a concentration of 5.7μM. This inhibition was time-dependent and irreversible.
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TAXONOMY OF THE PRODUCING ORGANISM, FERMENTATION, ISOLATION, PHYSICO-CHEMICAL PROPERTIES AND BIOLOGICAL ACTIVITIES
KAZUTOSHI SAKAMOTO, EISAKU TSUJII, MICHIYO MIYAUCHI, TOMOKO NAKANISHI, ...
1993 Volume 46 Issue 12 Pages
1788-1798
Published: December 25, 1993
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FR901459, a novel immunosuppressant, has been isolated from the fermentation broth of
Stachybotrys chartarum No. 19392. The molecular formula of FR901459 was determined as C
62H
111N
11O
13. FR901459 was found to be a member of the cyclosporin family. However, it is structurally distinct from any other cyclosporins discovered so far, in that Leu is present at position 5 instead of Val. FR901459 was capable of prolonging the survival time of skin allografts in rats with one third the potency of cyclosporin A.
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I. FERMENTATION, ISOLATION, PHYSICO-CHEMICAL AND BIOLOGICAL PROPERTIES
KATSUHISA KOJIRI, SHIGERU NAKAJIMA, HAJIME SUZUKI, AKIRA OKURA, HIROYU ...
1993 Volume 46 Issue 12 Pages
1799-1803
Published: December 25, 1993
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New antitumor substance, designated BE-18591, was isolated from the culture broth of a streptomycete, strain BA18591. The active principle was extracted from mycelium by methanol and purified by silica gel chromatography. BE-18591 inhibited the growth of MKN-45 human stomach cancer cell line as well as P388 cell line. In
in vivo experiments, BE-18591 inhibited the growth of Ehrlich ascites tumor.BE-18591 showed antimicrobial activity against Gram-positive and some Gram-negative bacteria.
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I. TAXONOMY, PRODUCTION, ISOLATION, PHYSICO-CHEMICAL PROPERTIES AND BIOLOGICAL ACTIVITIES
NOBUAKI NARUSE, OSAMU TENMYO, SEIKICHI KOBARU, MASAMI HATORI, KOJI TOM ...
1993 Volume 46 Issue 12 Pages
1804-1811
Published: December 25, 1993
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A new strain of
Microtetraspora parvosata subsp.
kistnae subsp. nov. (ATCC 55076) was found to produce new antiviral antibiotics, designated kistamicins A and B. These antibiotics exhibited activity against influenza virus type A and moderate activity against Gram-positive bacteria.
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II. STRUCTURE DETERMINATION
NOBUAKI NARUSE, MASAHISA OKA, MASATAKA KONISHI, TOSHIKAZU OKI
1993 Volume 46 Issue 12 Pages
1812-1818
Published: December 25, 1993
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The structures of antiviral antibiotics kistamicins A and B have been determined by a combination of chemical degradation and spectral analysis. They are commonly composed of D-tyrosine, 3, 5-dihydrophenylglycine, a biphenyl ether bis-amino acid, and a diphenyl substituted indole tris-amino acid, forming a tricyclic ring structure. Kistamicin B possessed a phenethylamide at the amino terminal of kistamicin A. They are structurally related to the nuclei of the vancornycin group antibiotics particularly to antibiotic complestatin.
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YIN-MEI CHIUNG, TOMOYUKI FUJITA, MASAHIRA NAKAGAWA, HIROSHI NOZAKI, GU ...
1993 Volume 46 Issue 12 Pages
1819-1826
Published: December 25, 1993
Released on J-STAGE: April 19, 2006
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A novel quinone antibiotic named malbranicin was isolated from the culture filtrate and mycelium of
Malbranchea cinnamomea TAIM 13T54, a thermophilic fungus. The antibiotic was elucidated to be 6-(1-acetylethyl)-2-methoxy-2, 5-cyclohexadiene-1, 4-dione by spectral analysis. Malbranicin exhibited antimicrobial and cytotoxic activities against Gram-positive bacteria and mammalian cell lines, respectively.
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AKIRA URAKAWA, TOSHIO OTANI, KEN-ICHIRO YOSHIDA, MITSURU NAKAYAMA, KAY ...
1993 Volume 46 Issue 12 Pages
1827-1833
Published: December 25, 1993
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A new antifungal antibiotic, S-632-C, was extracted with ethyl acetate from the culture filtrate of
Streptomyces hygroscopicus S-632 and isolated through a combination of column and preparative thin-layer chromatographies on silica gel. The structure of S-632-C was determined by analysis of
1H and
13C-NMR, MS, UV and IR spectra in comparison with those of S-632-A
2 (9-methylstreptimidone). The signals were assigned on the basis of 2D NMR experiments, which involved
1H-
1H DQF COSY, HMQC and HMBC spectral analysis. From these results, the chemical structure of S-632-C was elucidated as 6-(3, 5-dimethyl-2-oxo-4, 6-octadienyl)-4-carbamoylmethyl3, 4, 5, 6-tetrahydro-2-pyrone. The antibiotic exhibited exclusively weak
in vitro antifungal activity against
Saccharomyces spp. and similar cytotoxic activity against KB carcinoma cells, as compared with the glutarimide antibiotic S-632-A
2. In addition, this antibiotic had the ability to change the morphology of
rasts-transformed NRK cells to that of normal cells, also a characteristic S-632-A
2 and B
1.
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FERMENTATION, ISOLATION, STRUCTURE, AND ANTIMICROBIAL ACTIVITY
HIDEYUKI SHIOZAWA, TAKESHI KAGASAKI, TAKESHI KINOSHITA, HIDEYUKI HARUY ...
1993 Volume 46 Issue 12 Pages
1834-1842
Published: December 25, 1993
Released on J-STAGE: April 19, 2006
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Thiomarinol, an antimicrobial antibiotic, was isolated from the culture broth of a marine bacterium,
Alteromonas rava sp. nov. SANK 73390. Its structure was deduced as a hybrid composed of a pseudomonic acid analogue and holothin by NMR spectral analysis and chemical degradation. Antimicrobial activity against Gram-positive and Gram-negative bacteria of thiomarinol was stronger than both of pseudomonic acids and pyrrothine antibiotics.
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MASAYUKI IGARASHI, YASUYUKI TETSUKA, YAYOI MIMURA, ATSUSHI TAKAHASHI, ...
1993 Volume 46 Issue 12 Pages
1843-1848
Published: December 25, 1993
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Novel chlorosis-inducing substances, AB5046A and B, were isolated from the culture broth of a fungal strain. The producing organism, designated AB5046, was identified as a member of
Nodulisporium.
AB5046A and B were purified by extraction with EtOAc and silica gel chromatography. The structure of AB5046A and B were determined to be 2-butyryl-3, 5-dihydroxy-cyclohex-2-ene-1-one and 2-acetyl-3, 5-dihydroxy-cyclohex-2-ene-1-one, respectively, by spectroscopic analyses.
AB5046A and B induced chlorosis against Japanese barnyard millet
in vitro. The chlorosis activity of these compounds was stronger against monocotyledons than dicotyledons.
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I. PRODUCTION, ISOLATION AND PHYSICO-CHEMICAL AND BIOLOGICAL PROPERTIES
NORIKO TABATA, HIROSHI TOMODA, ROKURO MASUMA, KATSUJI HANEDA, YUZURU I ...
1993 Volume 46 Issue 12 Pages
1849-1853
Published: December 25, 1993
Released on J-STAGE: April 19, 2006
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Penicillium sp. FO-1611, a soil isolate, was found to produce a series of new anticoccidial compounds. Three active compounds, designated hynapenes A, B and C, were isolated from the fermetation broth of the producing strain by solvent extraction, silica gel column chromatography, gel filtration on Sephadex LH-20 and preparative HPLC. Hynapenes inhibited the growth of
Eimeria tenella in an
in vitro assay using BHK-21 cells as a host. No schizont in the cells was observed at concentrations ranging above 123μM, 34.7μM and 34.7μM for hynapenes A, B and C, respectively.
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II. STRUCTURE ELUCIDATION
NORIKO TABATA, HIROSHI TOMODA, YUZURU IWAI, SATOSHI OMURA
1993 Volume 46 Issue 12 Pages
1854-1858
Published: December 25, 1993
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The structures of hynapenes A, B and C, novel anticoccidial agents, were determined by spectroscopic analyses. Hynapenes A, B and C were deduced to be (2
E, 4
E)-5-(1, 3, 4-trihydroxy-2, 6, 8-trimethyldecalin)-2, 4-pentadienoic acid, (2
E, 4
E)-5-(1-ene-3-oxo-2, 6, 8-trimethyldecalin)-2, 4-pentadienoic acid and (2
E, 4
E)-5-(3-ene-1-oxo-2, 6, 8-trimethyldecalin)-2, 2, 4-pentadienoic acid, respectively.
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SHINICHIRO KATO, TOMIKO KAWASAKI, TETSURO URATA, JUNICHIRO MOCHIZUKI
1993 Volume 46 Issue 12 Pages
1859-1865
Published: December 25, 1993
Released on J-STAGE: April 19, 2006
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Free radical scavenging activities of various carbazole compounds, carazostatin, carbazomycin B and their chemically modified derivatives were studied
in vitro and
ex vivo. Among these compounds, carazostatin, which was isolated as a free radical scavenger from the culture of
Streptomyces chromofuscus, showed the most potent inhibitory activity against lipid peroxidation of rat brain homogenate
in vitro. Carbazomycin B, a known antimicrobial antibiotic, also exhibited strong activity in this system. Although
O-modified derivatives of carazostatin and carbazomycin B retained considerable activity,
N,
O-dimethyl derivatives did not suppress the peroxidation. On the other hand, the results from the
ex vivo evaluation of these carbazoles in the lipid peroxidation system of mouse blood plasma showed that the original compounds as well as their
O-modified derivatives had a strong inhibitory activity upon oral administration to mice. These findings suggest that these natural carbazoles and their effective derivatives can protect tissues from the peroxidative damage due to generation of free radicals.
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KENNETH J. WILDONGER, RONALD W. RATCLIFFE
1993 Volume 46 Issue 12 Pages
1866-1882
Published: December 25, 1993
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The syntheses of five thiols, including three dihydropyrrolotriazoliumthiol salts, 1, 4-dimethyl5-mercaptomethyl-1, 2, 4-triazolium trifluoromethanesulfonate, and 6-mercapto-6, 7-dihydro-5
H-pyrazolo[1, 2-
a][1, 2, 4]triazolium chloride; and the addition of these thiols to 4-nitrobenzyl (1
R, 5
R, 6
S)-2-(diphenylphosphono)oxy-6-[1(
R)-hydroxyethyl]-1-methylcarbapen-2-em-3-carboxylate and the subsequent hydrogenolysis of the addition products is described. The latter thiol provides a new route towards the preparation of L-627 (LJC 10, 627). The compounds were evaluated
in vitro against a panel of Gram-positive and Gram-negative bacteria and their antibacterial activities compared with imipenem. The compounds were measured for their hydrolytic stability to dehydropeptidase I (DHP-I) relative to imipenem. The five compounds generally had poorer Gram-positive and
Pseudomonas activity than imipenem, although their Gram-negative activity was variably improved. The monocyclic triazolium analog was nearly comparable in overall activity to the four bicyclic heterarylium analogs evaluated, including L-627 (LJC 10, 627). All compounds were more stable to DHP-I than imipenem, although minor differences existed among them.
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YOSHIO NISHIMURA, YOJI UMEZAWA, SHINICHI KONDO, TOMIO TAKEUCHI, KEIJI ...
1993 Volume 46 Issue 12 Pages
1883-1889
Published: December 25, 1993
Released on J-STAGE: April 19, 2006
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Two epimers of siastatin B, 3-episiastatin B (
3) and 3, 4-diepisiastatin B (
4), were obtained by the chemical modification of siastatin B. Compound
3 showed marked inhibitory activity against influenza virus neuraminidases and significant inhibition of influenza virus infection
in vitro.
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YASUHIRO HORI, YUKIKO ABE, NOBUHARU SHIGEMATSU, TOSHIO GOTO, MASAKUNI ...
1993 Volume 46 Issue 12 Pages
1890-1893
Published: December 25, 1993
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II. STRUCTURE DETERMINATION
SHIGERU NAKAJIMA, KATSUHISA KOJIRI, HIROYUKI SUDA
1993 Volume 46 Issue 12 Pages
1894-1896
Published: December 25, 1993
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ROBERT J. TERNANSKY, CHRISTOPHER L. JORDAN, F. WILLIAM BELL, THERESEA ...
1993 Volume 46 Issue 12 Pages
1897-1900
Published: December 25, 1993
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YASUHIRO HORI, YUKIKO ABE, HIDENORI NAKAJIMA, NOBUHARU SHIGEMATSU, SHI ...
1993 Volume 46 Issue 12 Pages
1901-1903
Published: December 25, 1993
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KEN-ICHIRO HAYASHI, MASAHIRA NAKAGAWA, OMOYUKI FUJITA, SHINJI TANIMORI ...
1993 Volume 46 Issue 12 Pages
1904-1907
Published: December 25, 1993
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SATOSHI OMURA, HARUO TANAKA, KEIICHI MATSUZAKI, HODAKA IKEDA, ROKURO M ...
1993 Volume 46 Issue 12 Pages
1908-1911
Published: December 25, 1993
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KIMIE KOBINATA, HIROYUKI KOSHINO, HIROO KUSAKABE, YUMIKO KOBAYASHI, IS ...
1993 Volume 46 Issue 12 Pages
1912-1915
Published: December 25, 1993
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IV. A CLUE TO THE SIMILARITY OF 2-DEOXY-SCFLLO-INOSOSE SYNTHASE TO DEHYDROQUINATE SYNTHASE
NORIAKI YAMAUCHI, KATSUMI KAKINUMA
1993 Volume 46 Issue 12 Pages
1916-1918
Published: December 25, 1993
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MASAYA NAKATA, CHU CHONG, YOSHIHISA NIWATA, KAZUNOBU TOSHIMA, KUNIAKI ...
1993 Volume 46 Issue 12 Pages
1919-1922
Published: December 25, 1993
Released on J-STAGE: April 19, 2006
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