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Chunzhi ZHANG, Hongshan YU, Yongming BAO, Lijia AN, Fengxie JIN
原稿種別: scientific monograph
2001 年 49 巻 7 号 p.
795-798
発行日: 2001年
公開日: 2002/05/31
ジャーナル
フリー
The ginsenoside-β-glucosidase that hydrolyzes the β-(1→2)-glucoside of the ginsenoside Rg3 sugar moiety to ginsenoside Rh2 was isolated from the ginseng root, and the enzyme was purified and characterized. The enzyme was purified to one spot in SDS polyacrylamide gel electrophoresis, and its molecular weight was about 59 kDa. The optimum temperature of the ginsenoside-β-glucosidase was 60 °C, and the optimum pH was 5.0. Ca
2+ ion had positive effect on ginsenoside-β-glucosidase, while Cu
2+ had negative effect on it. The ginsenoside-β-glucosidase may be a special β-glucosidase that is different from the original exocellulase such as β-glucosidase (EC 3.2.1.21).
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Kozo SAWADA, Satoshi OKADA, Akio KURODA, Shinya WATANABE, Yuki SAWADA, ...
原稿種別: scientific monograph
2001 年 49 巻 7 号 p.
799-813
発行日: 2001年
公開日: 2002/05/31
ジャーナル
フリー
A novel series of indolizinebutyric acids with various benzoyl substituents was synthesized to develop nonsteroidal inhibitors of steroid 5α-reductase, and the structure-activity relationships in this series were studied. We previously reported the structure-activity relationships in a series of indolebutyric acids as well as the discovery of the novel nonsteroidal 5α-reductase inhibitor, FK143. We have now made other modifications to this compound to improve in vivo inhibitory activity. By altering the heterocyclic nucleus and changing the benzoyl substituent we have succeeded in identifying the strongly active compound, FK687, (S)-4-[1-[4-[[1-(4-isobutylphenyl)butyl]oxy]benzoyl]indolizin-3-yl]butyric acid, which displays strong in vitro inhibitory activity against the human enzyme and in vivo inhibitory activity against the castrated young rat model. This compound should be a useful agent for the treatment of benign prostatic hyperplasia.
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Eleftherios KALPOUTZAKIS, Nektarios ALIGIANNIS, Sofia MITAKU, Ioanna C ...
原稿種別: scientific monograph
2001 年 49 巻 7 号 p.
814-817
発行日: 2001年
公開日: 2002/05/31
ジャーナル
フリー
The synthesis and antimicrobial activity of ten labdane-type diterpenes derived from ent-3-β-hydroxy-13-epi-manoyl oxide (ribenol) is reported. The chloroethyl carbamidic ester 9 showed the strongest antimicrobial activity against all the tested gram (+), gram (−) bacteria and pathogenic fungi. Moreover, the glycoside 11 exhibited an interesting activity against the three tested fungi.
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Chang-Sheng LU, Xiao-Ming REN, Chuan-Jiang HU, Hui-Zhen ZHU, Qing-Jin ...
原稿種別: scientific monograph
2001 年 49 巻 7 号 p.
818-821
発行日: 2001年
公開日: 2002/05/31
ジャーナル
フリー
A new β-cyclodextrin (β-CD) derivative, mono[6-deoxy-6-(2-butenedinitrile-2, 3-dimercapto sodium salt)]-β-CD (6-mnt-β-CD), and its inclusion compound with a ferrocenium drug, have been prepared and characterized by IR, UV,
13C-NMR spectroscopy, and mass spectrometry, elemental analysis, thermogravimetry, and cyclic voltammetry (CV). The interplay between the side-arm anion of β-CD and the ferrocenium (guest) in the inclusion compound 6-mnt-β-CD
-/Fc
+ has been investigated by
13C-NMR, UV, IR, and thermogravimetric methods. Charge transfer from the anion to the cation in 6-mnt-β-CD
-/Fc
+ was then experimentally identified. The interaction between the guest and the host with side-arm in 6-mnt-β-CD
-/Fc
+ resulted in smaller positive potential shifts compared to that in the inclusion compound [β-CD/Fc
+]BF
4-.
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Akira IYOBE, Masahiko UCHIDA, Kouji KAMATA, Yukihiko HOTEI, Hiroshi KU ...
原稿種別: scientific monograph
2001 年 49 巻 7 号 p.
822-829
発行日: 2001年
公開日: 2002/05/31
ジャーナル
フリー
A series of 6-cyclic aliphatic amino-7-nitro-3, 4-dihydroquinoline-2(1H)-ones were prepared and tested for platelet aggregation inhibitory effect, cardiotonic activity and chronotropic activity. These compounds appeared to show selective inhibitory activity against platelet aggregation. Among them, 6-(4-ethoxycarbonylpiperidino)-7-nitro-3, 4-dihydroquinoline-2(1H)-one (22f) showed the most potent inhibitory activity and high selectivity. A divergent synthetic route to 6-cyclic aliphatic amino-7-nitro-3, 4-dihydroquinoline-2(1H)-one derivatives has also been investigated.
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Kenji OHISHI, Ritsuo AIYAMA, Hiroshi HATANO, Yasuto YOSHIDA, Yasue WAD ...
原稿種別: scientific monograph
2001 年 49 巻 7 号 p.
830-839
発行日: 2001年
公開日: 2002/05/31
ジャーナル
フリー
A novel series of acyl-CoA: cholesterol O-acyltransferase (ACAT) inhibitors were synthesized from a lead compound, 1-(4-hydroxy-3-methoxyphenyl)-7-phenylhept-1-en-3-one (1, Yakuchinone B) through a modification of three regions (A, B, C) in the molecule. In this study, the compounds prepared were tested for in vitro inhibitory activity on microsomal ACAT from the liver of rats and for in vivo hypocholesterolemic activity in rats given a high cholesterol diet. N-(3,5-Dimethoxy-4-n-octyloxycinnamoyl)-N'-(3,4-dimethylphenyl)piperazine (45), which belongs to the amide compounds, has finally been discovered. Compound 45 inhibited rat hepatic ACAT in a more striking manner than CI-976, an amide compound ACAT inhibitor, and it exhibited a high level of hypocholesterolemic activity in vivo. Since 45 strongly inhibited both microsomal ACAT prepared from HepG2 (a cell line derived from human hepatocarcinoma) and Caco2 (a cell line derived from human colon adenocarcinoma), there is speculation that 45 might have the ability to inhibit ACAT in both the human intestine and liver independent of the difference in the distribution of ACAT isozymes. On the other hand, 45 did not induce adrenotoxicity in subacute toxicity studies in rats. These results suggest that it has promise for development as a new therapeutic agent for hypercholesterolemia and atherosclerosis.
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Toru ISHIKAWA, Yukiko SEGA, Junichi KITAJIMA
原稿種別: scientific monograph
2001 年 49 巻 7 号 p.
840-844
発行日: 2001年
公開日: 2002/05/31
ジャーナル
フリー
From the water-soluble portion of the methanol extract of the fruit of Carum ajowan (ajowan), which has been used as a spice and medicine, 25 compounds, including five new monoterpenoid glucosides, a new monoterpenoid, two new aromatic compound glucosides, and two new glucides, were obtained. Their structures were clarified by spectral investigation.
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Toshiyuki MURAKAMI, Akinobu KISHI, Hisashi MATSUDA, Masao HATTORI, Mas ...
原稿種別: scientific monograph
2001 年 49 巻 7 号 p.
845-848
発行日: 2001年
公開日: 2002/05/31
ジャーナル
フリー
Two new ionone glucosides, named apocynosides I and II, were isolated from the roasted leaves of Apocynum venetum L. together with nine known compounds. The absolute stereostructures of apocynosides I and II were determined by chemical and physicochemical evidence, which included the application of a modified Mosher’s method and the circular dichroism helicity rule.
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Chikako SAOTOME, Machiko ONO, Hiroyuki AKITA
原稿種別: scientific monograph
2001 年 49 巻 7 号 p.
849-853
発行日: 2001年
公開日: 2002/05/31
ジャーナル
フリー
A reaction of methyl (4R, 5R)-4, 5-epoxy-2(E)-hexenoate 1 with N-benzylmethylamine gave a diastereomerically pure methyl (4R, 5R)-4, 5-epoxy-(3S)-N-benzylmethylamino hexanoate 6 and methyl (4S, 5R)-4-N-benzylmethylamino-5-hydroxy-2(E)-hexenoate 7. The former was chemoenzymatically converted to (−)-osmundalactone 11, which is an aglycone of osmundalin. On the other hand, the directly conjugated addition of dimethylamine to methyl (4S, 5S)-4, 5-epoxy-2(E)-hexenoate 1 followed by treatment with MeOH at 40 °C exclusively provided methyl (4R, 5S)-4-dimethylamino-5-hydroxy-2(E)-hexenoate 16, which was converted into L-(−)-forosamine 18.
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Pittaya TUNTIWACHWUTTIKUL, Walter Charles TAYLOR
原稿種別: scientific monograph
2001 年 49 巻 7 号 p.
854-857
発行日: 2001年
公開日: 2002/05/31
ジャーナル
フリー
Baenzigeroside B, a new rearranged clerodane diterpene glucoside, was isolated from the stems of Tinospora baenzigeri. The aglycone of baenzigeroside B, baenzigeride B (isolated as its acetate), was found together with baenzigeride A, baenzigerosides A and B in the leaves of the same plant. Baenzigeride B and baenzigeroside B are the first examples of a new class of rearranged clerodane diterpenes. The possible biogenesis of the compounds is discussed.
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Toshiyuki TANAKA, Ibrahim ILIYA, Tetsuro ITO, Miyuki FURUSAWA, Ken-ich ...
原稿種別: scientific monograph
2001 年 49 巻 7 号 p.
858-862
発行日: 2001年
公開日: 2002/05/31
ジャーナル
フリー
Five new stilbene dimers were isolated from the lianas of Gnetum parvifolium in addition to known stilbenoids. The structures of the compounds were established on the basis of spectroscopic evidence, including long-range coupling and nuclear Overhauser effect experiments, in NMR spectrum. Among the isolates, 2b-hydroxyampelopsin F showed potent inhibitory activity in the Maillard reaction.
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Masayuki YOSHIKAWA, Toshiyuki MURAKAMI, Akinobu KISHI, Tadashi KAGEURA ...
原稿種別: scientific monograph
2001 年 49 巻 7 号 p.
863-870
発行日: 2001年
公開日: 2002/05/31
ジャーナル
フリー
The methanolic extract and its 1-butanol-soluble fraction from the flowers of Calendula officinalis were found to show a hypoglycemic effect, inhibitory activity of gastric emptying, and gastroprotective effect. From the 1-butanol-soluble fraction, four new triterpene oligoglycosides, calendasaponins A, B, C, and D, were isolated, together with eight known saponins, seven known flavonol glycosides, and a known sesquiterpene glucoside. Their structures were elucidated on the basis of chemical and physicochemical evidence. The principal saponin constituents, glycosides A, B, C, D, and F, exhibited potent inhibitory effects on an increase in serum glucose levels in glucose-loaded rats, gastric emptying in mice, and ethanol- and indomethacin-induced gastric lesions in rats. Some structure-activity relationships are discussed.
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Mei-Lin GO, Si-Shen FENG
原稿種別: scientific monograph
2001 年 49 巻 7 号 p.
871-876
発行日: 2001年
公開日: 2002/05/31
ジャーナル
フリー
The antimalarial agent halofantrine penetrates dipalmitolylphosphatidylcholine (DPPC) monolayers resulting in an increase in surface pressure and an expansion in area occupied by the lipid components of the monolayer. This phenomenon is observed at concentrations (0.05-0.2 μM) of halofantrine that have no surface activity. Penetration increases with drug concentration and is greatest at low initial surface pressures of the monolayer. A critical surface pressure of the DPPC monolayer has been determined from constant area and constant pressure conditions. The magnitude of these values support the hypothesis that halofantrine readily penetrates the DPPC monolayers. The presence of cholesterol in the DPPC monolayer hampers penetration and a lower critical surface pressure is obtained under such conditions. Even then, a slower rate of penetration is observed only in monolayers maintained at high initial surface pressures (10, 15 mN/m), corresponding to the liquid condensed phase of the monolayer, and not at low surface pressures (2.5, 5.0 mN/m). These results help to give a better understanding of the dynamics of the halofantrine-phospholipid interaction as well as the pharmacodynamic character of the drug.
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Yasuhiro SHIKISHIMA, Yoshihisa TAKAISHI, Gisho HONDA, Michiho ITO, Yos ...
原稿種別: scientific monograph
2001 年 49 巻 7 号 p.
877-880
発行日: 2001年
公開日: 2002/05/31
ジャーナル
フリー
The methanol extract of the dried aerial parts of Prangos tschimganica gave three new coumarin derivatives and 30 known coumarin derivatives. Their structures were established on the basis of chemical and spectroscopic evidence. Absolute configuration of the isolated compounds were determined by using a modified Mosher’s method. Some of the isolated compounds showed anti-HIV activity.
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Hitomi HAGIWARA, Tominari CHOSHI, Junko NOBUHIRO, Hiroyuki FUJIMOTO, S ...
原稿種別: scientific monograph
2001 年 49 巻 7 号 p.
881-886
発行日: 2001年
公開日: 2002/05/31
ジャーナル
フリー
The formal total synthesis of murrayaquinone A (1) and the total synthesis of furostifoline (5) were completed by the construction of 4-oxygenated 3-methylcarbazoles 7 based on a new type of electrocyclic reaction through 2-alkenyl-3-allenylindole intermediates 8 derived from the 2-alkenyl-3-propargylindoles 9, starting from 2-chloroindole-3-carbaldehyde (11). The N, O-bisbenzyloxymethyl group of 16c and 22 underwent a Birch reduction followed by treatment with Triton B to produce the known 4-hydroxy-3-methylcarbazole (7a) and 4-hydroxy-3-methylfuro[3, 2-a]carbazole (7b) as precursors of murrayaquinone A (1) and furostifoline (5), respectively. The trifluoromethanesulfonyloxy-3-methylfuro[3, 2-a]carbazole (24), prepared from 7b, was subjected to reductive cleavage to provide furostifoline (5).
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Zhi-Hong JIANG, Yoko HIROSE, Hiromi IWATA, Saori SAKAMOTO, Takashi TAN ...
原稿種別: scientific monograph
2001 年 49 巻 7 号 p.
887-892
発行日: 2001年
公開日: 2002/05/31
ジャーナル
フリー
Eighteen new and sixteen known acyl glucoses having caffeoyl, coumaroyl, galloyl, and hexahydroxydiphenoyl groups were isolated from a medicinal parasitic plant, Balanophora japonica. Their structures were determined by spectroscopic and chemical methods. Caffeoyl ellagitannins, which have been rarely found in nature, were major phenolic constituents of this plant, and this is the first report of the isolation of ellagitannins from Balanophoraceae.
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Reiko FUJITA, Kazuhiro WATANABE, Toshiteru YOSHISUJI, Chizuko KABUTO, ...
原稿種別: scientific monograph
2001 年 49 巻 7 号 p.
893-899
発行日: 2001年
公開日: 2002/05/31
ジャーナル
フリー
Diels-Alder cycloadditions of 2(1H)-quinolones having an electron-withdrawing group at the 3-position with alkyl- and silyloxy-1, 3-butadienes (2a, b) were carried out to give phenanthridones richly functionalized regio- or stereoselectively under conditions of atmospheric and high pressure. Furthermore, regioselectivity and chemoselectivity of 3-substituted 2(1H)-quinolones to 2a, b were examined using MO calculation.
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Reiko FUJITA, Kazuhiro WATANABE, Toshiteru YOSHISUJI, Hiroshi HONGO, H ...
原稿種別: scientific monograph
2001 年 49 巻 7 号 p.
900-904
発行日: 2001年
公開日: 2002/05/31
ジャーナル
フリー
Diels-Alder reactions of 1-methyl-2(1H)-quinolones having an electron-withdrawing group at the 4-position with isoprene, butadiene sulfone, and cyclohexadiene were performed to yield functionalized phenanthridones stereoselectively at atmospheric and at high pressure. Regioselectivity and stereochemistry of a methoxycarbonyl group were studied using the semi-empirical and ab initio MO methods, respectively.
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Naotaka KURODA, Daisuke SATO, Kaname OHYAMA, Mitsuhiro WADA, Yuji NAKA ...
原稿種別: scientific monograph
2001 年 49 巻 7 号 p.
905-908
発行日: 2001年
公開日: 2002/05/31
ジャーナル
フリー
Separation of twelve sympathomimetic amines and related compounds by micellar electrokinetic chromatography (MEKC) with UV absorbance detection is described. These amines were well separated within 25 min using 50 mM sodium tetraborate solution containing 15 mM sodium dodecylsulfate (SDS) of pH 9.3 as a running solution and detected at 210 nm. MEKC was performed with an applied voltage of 13 kV at 25 °C using a fused-silica capillary (50 cm×75 mm i.d.) with effective length of 37.5 cm. The detection limits of these compounds were in the range from 4 to 97 fmol/injection at a signal-to-noise ratio (S/N) of 3. The reproducibility of the method expressed as relative standard deviation (RSD) for within-day (n=6) and between-day (n=5) assays was less than 4.8 and 8.8%, respectively. The proposed method could be applied to the determination of an anorectic drug, phentermine, in Chinese tea with a detection limit of 99 μg/g (105 fmol/injection, S/N=3).
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Hiroyuki ITOH, Harukazu TANAKA, Hiroshi OHTA, Hideo TAKESHIBA
原稿種別: scientific monograph
2001 年 49 巻 7 号 p.
909-911
発行日: 2001年
公開日: 2002/05/31
ジャーナル
フリー
A new series of silicon-containing derivatives of 2-aryl-3-(1H-1, 2, 4-triazol-1-yl)propanenitriles were synthesized and evaluated for fungicidal activities against rice sheath blight and powdery mildew on cucumber. These derivatives exhibited higher efficacy than reference fungicides.
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Chil Mann JUNG, Hak Cheol KWON, Jung Ju SEO, Yasushi OHIZUMI, Kimihiro ...
原稿種別: scientific monograph
2001 年 49 巻 7 号 p.
912-914
発行日: 2001年
公開日: 2002/05/31
ジャーナル
フリー
The aerial part of Aster scaber THUNB. (Asteraceae) yielded two new monoterpene peroxide glycosides, (3S)-3-O-(3',4'-diangeloyl-β-D-glucopyranosyloxy)-7-hydroperoxy-3,7-dimethylocta-1,5-diene (1) and (3S)-3-O-(3',4'-diangeloyl-β-D-glucopyranosyloxy)-6-hydroperoxy-3,7-dimethylocta-1,7-diene (2), and five known compounds, α-spinasterol (3), germacra-4(15),5,10(14)-triene-1β-ol (4), 7-methoxy-4(15)-oppositen-1β-ol (5), 6α-methoxy-4(15)-eudesmane-1β-ol (6) and α-spinasterol 3-O-β-D-glucopyranoside (7). The structures were established by chemical and spectroscopic methods.
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Chao-Mei MA, Norio NAKAMURA, Masao HATTORI
原稿種別: scientific monograph
2001 年 49 巻 7 号 p.
915-917
発行日: 2001年
公開日: 2002/05/31
ジャーナル
フリー
From a methanol extract of Artemisia caruifolia, which showed a moderate inhibitory activity on HIV-1 protease in a preliminary screening, N
1, N
5, N
10-tri-p-coumaroylspermidine and three dicaffeoylquinic acids were isolated. The former compound was found to appreciably inhibit HIV-1 protease. Of related amides which were chemically synthesized, N
1, N
5, N
10, N
14-tetra-p-coumaroylspermine and N
1, N
4, N
7, N
10, N
13-penta-p-coumaroyltetraethylenepentamine inhibited HIV-1 protease more potently than N
1, N
5, N
10-tri-p-coumaroylspermidine.
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Atef A. ABDEL-HAFEZ, Meselhy R. MESELHY, Norio NAKAMURA, Masao HATTORI ...
原稿種別: scientific monograph
2001 年 49 巻 7 号 p.
918-920
発行日: 2001年
公開日: 2002/05/31
ジャーナル
フリー
During the course of preparing anticonvulsant paeonimetabolin-I adducts, new paeonilactone-A adducts: 9-phenylthiopaeonilactone-A, 9-(o-tolylthio)paeonilactone-A, 9-(m-tolylthio)paeonilactone-A. 9-(p-tolylthio)-paeonilactone-A and 9-(2-naphthylthio)paeonilactone-A, were obtained along with expected paeonimetabolin-I adducts by anaerobic incubation of paeoniflorin from peony roots with Lactobacillus brevis in the presence of the aromatic thiols, phenylthiol, o-tolylthiol, m-tolylthiol, p-tolylthiol and 2-naphthylthiol. The structures of these compounds were determined by spectroscopic methods including two dimensional (2D) NMR.
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Hhideaki OTSUKA, Eiji HIRATA, Takakazu SHINZATO, Yoshio TAKEDA
原稿種別: scientific monograph
2001 年 49 巻 7 号 p.
921-923
発行日: 2001年
公開日: 2002/05/31
ジャーナル
フリー
From the leaves of Glochidion zeylanicum collected in Okinawa, four flavanol glucosides, named as glochiflavanosides A-D were isolated along with known flavone C-glucosides, vitexin and isoorientin. Their structures were elucidated by spectroscopic analyses.
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Masao TOYOTA, Ikuko OMATSU, Yoshinori ASAKAWA
原稿種別: scientific monograph
2001 年 49 巻 7 号 p.
924-926
発行日: 2001年
公開日: 2002/05/31
ジャーナル
フリー
The diethyl ether extract of the Japanese liverwort Metacalypogeia cordifolia yielded five new chroman type derivatives in addition to known sesquiterpenoids. One of the new chroman derivatives was also isolated from the ether extract of another liverwort, Cephalozia otaruensis. Their structures were established by extensive two dimensional (2D) NMR techniques and chemical evidence. They were shown to be 2, 2-dimethyl-7-(3-methyl-2-butenyl)-chroman derivatives. This was the first example of the isolation of the chroman-type compounds, although various types of aromatic compounds have been isolated from liverworts.
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Consolacion Y. RAGASA, Vilma F. TEMPLORA, John A. RIDEOUT
原稿種別: scientific monograph
2001 年 49 巻 7 号 p.
927-929
発行日: 2001年
公開日: 2002/05/31
ジャーナル
フリー
The chloroform extract of the air-dried leaves of Coleus blumei afforded a mixture of diastereomers of a new abietane type diterpene whose structures were elucidated by extensive one and two dimensional (1D, 2D) NMR and mass spectrometry. Acetylation of the mixture afforded a single compound. Antimicrobial tests on the diterpene indicate that it is active against Bacillus subtilis, Pseudomonas aeruginosa and Candida albicans.
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