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I. Taxonomy, Fermentation and Isolation
JONG-GWAN KIM, HUNG-BAE CHANG, YOUNG-IN KWON, SEUNG-KEE MOON, HYOUNG-S ...
2002 Volume 55 Issue 5 Pages
457-461
Published: May 25, 2002
Released on J-STAGE: January 27, 2009
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New α-glucosidase inhibitors, CKD-711 and CKD-711a were produced from the fermentation broth of
Streptomyces sp. CK-4416 which was isolated from a forest soil of Jeju Island, South Korea. CKD-711 and CKD-711a were purified by Dowex 50W-2X and Sephadex G-10 column chromatography. In
in vitro studies, CKD-711 showed a potent inhibitory activity against α-glucosidase from mammalian, but less inhibition against α-amylase from microorganism and mammalian. CKD-711a showed a lower inhibitory activity than CKD-711.
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II. Biological Properties
YOUNG-IN KWON, HYEOG-JIN SON, KYOUNG SIK MOON, JOON KYUM KIM, JONG-GWA ...
2002 Volume 55 Issue 5 Pages
462-466
Published: May 25, 2002
Released on J-STAGE: January 27, 2009
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CKD-711 and CKD-711a are aminooligosaccharide α-glucosidase inhibitors discovered during the bioactive material screening for antibacterial agent. Their inhibitory activities were studied and compared with those of acarbose
in vitro and
in vivo with animals. In
in vitro study, CKD-711 showed similar effects to acarbose on porcine intestinal maltase and sucrase, IC
50s of 2.5 and 0.5μg/ml, respectively, whereas it had about 2 fold lower α-amylase inhibitory activity (IC
50, 78.0μg/ml) than acarbose (IC
50, 36μg/ml). CKD-711a showed less inhibitory activity than CKD-711 against all the enzymes tested. In rat fed on starch and sucrose meals, the dose of CKD-711 which reduced the postprandial blood glucose increment by 50 percent in comparison to control rats (ED
50) were 3.07 and 1.15mg/kg, respectively, and acarbose had ED
50s of 1.94 and 1.15mg/kg, respectively. CKD-711 and CKD-711a also showed antibacterial activity against
Comamonas terrigena.
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III. Physico-chemical Properties and Structure Elucidation
HUNG-BAE CHANG, SUN-HO KIM, YOUNG-IN KWON, DONG-HO CHOUNG, WON-KYU CHO ...
2002 Volume 55 Issue 5 Pages
467-471
Published: May 25, 2002
Released on J-STAGE: January 27, 2009
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We have isolated two novel α-glucosidase inhibitors,
O-[4-deoxy-4-(2, 3-epoxy-3-hydroxymethyl-4, 5, 6-trihydroxycyclohexane-1-yl-amino)-α-D-glucopyranosyl]-(1→4)-
O-α-D-glucopyranosyl-(1→4)-α-D-glucopyranose (named CKD-711) and its hexameric analog CKD-711a, from the fermentation broth of
Streptomyces sp. CK-4416. HRFAB-MS and NMR analyses reveal that molecular formulae of CKD-711 and CKD-711a are C
25H
43NO
20 and C
37H
63NO
30, respectively with the latter containing two more glucose moieties than the former. Detailed chemical structures of both compounds have been characterized by high-resolution two-dimensional NMR methods.
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I. Taxonomic Studies of the Producer Microorganism and Fermentation Results
J. WINK, F.-R. SCHMIDT, G. SEIBERT, W. ARETZ
2002 Volume 55 Issue 5 Pages
472-479
Published: May 25, 2002
Released on J-STAGE: January 27, 2009
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The cyclipostins are a group of hormone-sensitive lipase inhibitors produced by a
Streptomyces species. Having verticillate spore chains this strain exhibits significant differences to the known species of the former genus
Streptoverticillium. Taxonomic studies and fermentation results are presented.
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II. Isolation, Structure Elucidation and Biological Properties
LÁSZLÓ VÉRTESY, BERND BECK, MARK BRÖNSTRUP, ...
2002 Volume 55 Issue 5 Pages
480-494
Published: May 25, 2002
Released on J-STAGE: January 27, 2009
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Hormone-sensitive lipase (HSL) is a key enzyme of lipid metabolism and its control is therefore a target in the treatment of diabetes mellitus. Cultures of the
Streptomyces species DSM 13381 have been shown to potently inhibit HSL. Ten inhibitors of HSL, termed cyclipostins, have been isolated from the mycelium of this microorganism and a further nine related compounds detected. Their structures were characterized by 2-D NMR experiments and by mass spectrometry and were found to comprise neutral cyclic enol phosphate esters with an additional γ-lactone ring. On account of their ester-bound fatty alcohol side chain, the cyclipostins have physicochemical properties similar to those of triglycerides. The outstanding characteristic of the cyclipostins is their strong anti-HSL activity, with IC
50 values in the nanomolar range.
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YOSHIO HOSAKA, RYOICHI OKAMOTO, KAZUHIKO IRINODA, SATORU KAIEDA, WASAB ...
2002 Volume 55 Issue 5 Pages
495-498
Published: May 25, 2002
Released on J-STAGE: January 27, 2009
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Helicobacter pylori (H. pylori) is a Gram-negative curved rod-like or spiral bacterium that chronically infects the human gastric mucosa, and is a major risk factor for gastritis, gastric and duodenal ulcer and adenocarcinoma of the stomach. After partial gastrectomy, some patients may have persistent
H. pylori infection for five years or more. In this study, we detected three bacteria,
i.e., Klebsiella pneumoniae, Enterobacter aerogenes, and
Escherichia coli, in the gastric juice of patients with a remnant stomach. Some of these bacteria produced β-lactamase. These findings are potentially important since such bacteria could provide
H. pylori with the chance to acquire drug resistance and to transfer drug resistance genes. This could be one reason why
H. pylori is difficult to eradicate in the remnant stomach.
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II. The Combination of Amino Acid Residues in the Dipeptidic Moiety and its Effect on the Anti-Helicobacter pylori Activity
ATSUSHI HASUOKA, YUJI NISHIKIMI, YUTAKA NAKAYAMA, KEIJI KAMIYAMA, MASA ...
2002 Volume 55 Issue 5 Pages
499-507
Published: May 25, 2002
Released on J-STAGE: January 27, 2009
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The novel natural antibiotics pyloricidin A, B and C, consisting of a common (2
S, 3
R, 4
R, 5
S)-5-amino-2, 3, 4, 6-tetrahydroxyhexanoyl-β-D-phenylalanine moiety and a terminal peptidic moiety (pyloricidin A: L-valine-L-valine-L-leucine; pyloricidin B: L-valine-L-leucine; pyloricidin C: L-leucine), exhibit potent and highly selective anti-
Helicobacter pylori activity. In order to develop more potent compounds and to investigate structure activity relationships for the peptidic moiety with regard to the combination of amino acids, a series of derivatives with various dipeptidic moieties were prepared and evaluated for their anti-
H. pylori activity. The combination of the two amino acids in the moiety was found to have a significant effect on the activity; the compound with Nva-Abu showed excellent anti-
H pylori activity with an MIC value of 0.013μg/ml against
H. pylori TN2. In addition, this compound was found to show 60% clearance of
H. pylori from infected Mongolian gerbils upon repetitive oral administration (10mg/kg, b. i. d. for 7 days).
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HIRONOBU KATOH, KAZUO SHIN-YA, KAZUO FURIHATA, KEIKO FURIHATA, YOICHI ...
2002 Volume 55 Issue 5 Pages
508-510
Published: May 25, 2002
Released on J-STAGE: January 27, 2009
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WOON-HYUNG YEO, BONG-SIK YUN, YOUNG-SOOK KIM, SEUNG HUN YU, HWAN-MOOK ...
2002 Volume 55 Issue 5 Pages
511-515
Published: May 25, 2002
Released on J-STAGE: January 27, 2009
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YASUTAKA HOSHINO, VENETA BOJANOVA IVANOVA, KATSUKIYO YAZAWA, AKIKAZU A ...
2002 Volume 55 Issue 5 Pages
516-519
Published: May 25, 2002
Released on J-STAGE: January 27, 2009
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DEBORAH M. ROLL, MARK TISCHLER, R. THOMAS WILLIAMSON, GUY T. CARTER
2002 Volume 55 Issue 5 Pages
520-523
Published: May 25, 2002
Released on J-STAGE: January 27, 2009
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ATTILA AGÓCS, PÁL HERCZEGH, FERENC SZTARICSKAI, ZSUZSA G ...
2002 Volume 55 Issue 5 Pages
524-527
Published: May 25, 2002
Released on J-STAGE: January 27, 2009
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TOMOHISA HORIBE, HIROAKI NAGAI, HIROAKI MATSUI, YASUNARI HAGIWARA, MAS ...
2002 Volume 55 Issue 5 Pages
528-530
Published: May 25, 2002
Released on J-STAGE: January 27, 2009
JOURNAL
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