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Volume 55, Issue 1
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Mohammad Abdul-Azim Mohammad, Nagwan Hamdy Zawilla, Fawzy Mohammad El- ...2007 Volume 55 Issue 1 Pages 1-6
Published: 2007
Released on J-STAGE: January 01, 2007
JOURNAL FREE ACCESSThree stability indicating assay methods are developed for the determination of norfloxacin (Nor) in the presence of its decarboxylated degradation product and in mixture with tinidazole (Tnd). The proposed methods are reversed phase ion pair liquid chromatography (LC), thin layer densitometry (TLC) and second derivative ratio spectra zero crossing spectrophotometry (2DD). Chromatographic separation was achieved on μ-Bondapack C18 column 5 μm (300 mm×3.9 mm, I.D.) and precoated silica gel TLC stationary phases for LC and TLC methods, respectively. Mobile phases consisting of phosphate buffer pH 3.2 : methanol (3 : 1, v/v) containing 0.005 M pentane sulfonic acid sodium salt and isopropanol : butanol : concentrated ammonia : water (25 : 50 : 5 : 25, v/v/v/v) were used for resolution of Nor and Tnd by both techniques, respectively. Detection was carried at 280 nm. In the ratio spectra method, detection of Nor was carried at 282 nm. Linearity, accuracy and precision were found to be acceptable over concentration ranges of 20—225 μg/ml, 0.8—4 μg/spot and 1—7 μg/ml for Nor by LC, TLC and 2DD methods and over concentration ranges of 37.5—375 μg/ml and 4.8—20 μg/spot for Tnd by LC and TLC methods respectively. The suggested methods were successfully applied for the determination of both drugs in bulk powder, laboratory prepared mixtures and in commercial samples. Statistical comparison between the results obtained by the proposed and the reference methods was carried out using Student t-test, F ratio and one way ANOVA.View full abstractDownload PDF (140K) -
Shigeki Kobayashi, Hidetaka Wakamatsu, Nahomi Atuchi, Rie Miyajima, Ay ...2007 Volume 55 Issue 1 Pages 7-14
Published: 2007
Released on J-STAGE: January 01, 2007
JOURNAL FREE ACCESSOur aim in this study is to elucidate the correlations between inhibition and chirality, especially, diastereomer, against cell proliferation of double-stranded peptides. In previous studies, we reported on the design, synthesis, and chemical properties on a series of novel double-stranded peptides, (y-AA–x-AA)2–spacer(S) (AA=amino acid, S=spacer, symbols x and y represent L- or D-forms, and (y-, x-) as represent of the symbol) conjugated with –y-AA–x-AA– and –z-AA–y-AA–x-AA– sequences to a spacer of carbon number n. The inhibition of A431 and srctsNRK cells growth by four diastereomers of the N1,N12-bis(y-Phe–x-Phe)dodecanediamines (n=12) increased in the following order: (L-, L-)<(D-, D-)<(L-, D-)<(D-, L-). A similar trend was seen in the order for the activity of (y-AA–x-AA)2–spacer(S) with a spacer of carbon number n=2, 3, 4, 5, 6, and 12 against the cell growth inhibition. To understand the mechanism of diasteromer selective cell growth inhibition, the correlations between chirality and cell growth inhibition were investigated from the measurement of the changes in cytosolic Ca2+ concentration (=[Ca2+]c) of A431 cells. Although less active N1,N12-bis(L-Phe–L-Phe)dodecanediamine increases cytosolic [Ca2+]c, more active diasteromers, N1,N12-bis(L-Phe–D-Phe)dodecanediamine and N1,N12-bis(D-Phe–L-Phe)dodecanediamine, decrease cytosolic [Ca2+]c in A431 cell. This study provides diastereomeric effected new insights—this controls the polarity of double-stranded peptides—into the control of tumor cell proliferation and design of the uptake by penetration through the cell membrane of drugs.View full abstractDownload PDF (1053K) -
Zhi-Gang Yang, He-Ran Li, Li-Yan Wang, Yong-Hai Li, Shun-Guang Lu, Xiu ...2007 Volume 55 Issue 1 Pages 15-18
Published: 2007
Released on J-STAGE: January 01, 2007
JOURNAL FREE ACCESSIn our investigation on the chemical constituents of Hippophae rhamnoides L., the chloroform-soluble fraction of the 80% acetone extract of branch bark was observed to inhibit nitric oxide (NO) production in a lipopolysaccharide and recombinant mouse interferon-γ-activated murine macrophage-like cell line, RAW 264.7 cells. Two new triterpenoids, 2-O-trans-p-coumaroyl maslinic acid (1) and 2-O-caffeoyl maslinic acid (2), and three known triterpenoids, oleanolic acid (3), 3-O-trans-p-coumaroyl oleanolic acid (4), and 3-O-caffeoyl oleanolic acid (5), and 6-methoxy-2H-1-benzopyran (6) and β-sitosterol (7) were isolated from the branch bark extract. Their inhibitory activities on the production of NO in RAW 264.7 cells and radical-scavenging activities were examined.View full abstractDownload PDF (91K) -
Naonobu Tanaka, Yoshihisa Takaishi2007 Volume 55 Issue 1 Pages 19-21
Published: 2007
Released on J-STAGE: January 01, 2007
JOURNAL FREE ACCESSSix new xanthones, 4,6-dihydroxy-2,3-dimethoxyxanthone (1), 2,6-dihydroxy-3,4-dimethoxyxanthone (2), 6-hydroxy-2,3,4-trimethoxyxanthone (3), 3,6-dihydroxy-1,2-dimethoxyxanthone (4), 4,7-dihydroxy-2,3-dimethoxyxanthone (5), and 3,7-dihydroxy-2,4-dimethoxyxanthone (6) were isolated from the stems of Hypericum chinense, together with four known xanthones. Their structures were established based on spectroscopic studies.View full abstractDownload PDF (87K) -
Elena Cartagena, Olga Álvarez Colom, Adriana Neske, Juan Carlos ...2007 Volume 55 Issue 1 Pages 22-25
Published: 2007
Released on J-STAGE: January 01, 2007
JOURNAL FREE ACCESSSixteen plant sesquiterpene lactones, thirteen from four species of the Family Asteraceae, and three from a species of Hepaticae, as well as seven annonaceous acetogenins isolated from the seeds of the tropical tree Annona cherimolia (Family Annonaceae), were evaluated for their ability to inhibit or stimulate the production of biofilm by a strain of Pseudomonas aeruginosa. The tested compounds carry a γ-lactone moiety in their structures. This structural feature is similar to the lactone moiety present in N-acyl homoserine lactones, compounds that play the important role of “quorum sensors” in the mechanisms of biofilm formation observed in many gram-negative bacteria. A special assay was employed to evaluate the influence of the tested plant compounds to inhibit or stimulate the production of biofilm in a P. aeruginosa wild strain. Most of the tested compounds affected the biofilm formation mechanism. Six sesquiterpene lactones isolated from Acanthospermum hispidum and one from Enydra anagallis as well as an acetogenin from Annona cherimolia strongly inhibited (69—77%) the biofilm formation when incorporated to a bacterial culture at a concentration of 2.5 μg/ml. However, one of the acetogenins, squamocin, stimulated the biofilm formation even at a concentration of 0.25 μg/ml. The study of substances affecting the biofilm formation can lead to the design of new strategies to control P. aeruginosa infections.View full abstractDownload PDF (154K) -
Tian-Rong Li, Zheng-Yin Yang, Bao-Dui Wang2007 Volume 55 Issue 1 Pages 26-28
Published: 2007
Released on J-STAGE: January 01, 2007
JOURNAL FREE ACCESSA new ligand, naringenin-2-hydroxy benzoyl hydrazone (H5L), was prepared by condensation of naringenin with 2-hydroxy benzoyl hydrazine. Its Cu(II), Ni(II), Zn(II) complexes have also been synthesized and characterized on the basis of 1H-NMR, IR, UV–Vis spectra, elemental analyses, molar conductivity and thermal analyses. The general formula of these complexes was M(H3L) [M=Cu(II), Ni(II) and Zn(II)]. In addition, the antioxidant activities (superoxide and hydroxyl radical) of the free ligand and its complexes were determined in vitro. These compounds were found to possess potent antioxidant activity and be better than standard antioxidants like vitamin C and mannitol. In particular, the Cu(II) complex displayed excellent activity on the superoxide radical.View full abstractDownload PDF (102K) -
Helena Nicklasson, Fridrun Podczeckb2007 Volume 55 Issue 1 Pages 29-33
Published: 2007
Released on J-STAGE: January 01, 2007
JOURNAL FREE ACCESSThe purpose of this study was to investigate the role of pores in the fracture of circular compacts and to predict compact properties and critical crack lengths. Four different particle size fractions of sucrose, ranging from 20 to 500 μm, were compressed into circular discs (i.e. flat tablets) and rectangular beam specimens of porosity between 30 and 14%. Modelling of the relationship between the tensile strength of the circular discs and the compact porosity indicated extensive fragmentation during compaction for particles in the size range of 250—500 μm, accompanied by a change in densification mechanism for very coarse particles (355—500 μm). When determining the critical stress intensity factor from rectangular single edge notched beam specimens by 3-point bending, an apparent influence of particle size on the values could be seen, whereby here the results indicated that the critical particle size for fragmentation to occur is about 20—40 μm. It was possible to predict the critical stress intensity factor of the compacts from the median pore size and the tensile strength of the circular disc specimens by interpolation of the critical crack length for propagation to occur. The results indicated that for sucrose compacts regardless of their porosity, the pores themselves acted as stress concentrators, not as sharp cracks. For sucrose compacts, crack propagation hence proceeds most likely along grain boundaries.View full abstractDownload PDF (88K) -
Naoko Kiyota, Kazushi Shingu, Koki Yamaguchi, Yasuyuki Yoshitake, Kazu ...2007 Volume 55 Issue 1 Pages 34-36
Published: 2007
Released on J-STAGE: January 01, 2007
JOURNAL FREE ACCESSThree new C28 steroidal glycosides, isotubocaposides A (1), B (2), and C (3), were isolated from the fruits of Tubocapsicum anomalum MAKINO. Their chemical structures were elucidated on the basis of spectroscopic and X-ray diffraction analysis of p-bromobenzoyl derivative (5) of isotubocaposigenin (4), the sapogenol derivative of these three glycosides. Isotubocaposides have the structural peculiarity of an unusual side chain carrying a C-21 bound to C-24 on the lactone ring.View full abstractDownload PDF (188K) -
Kazunari Sakagami, Toshihito Kumagai, Takeo Taguchi, Atsuro Nakazato2007 Volume 55 Issue 1 Pages 37-43
Published: 2007
Released on J-STAGE: January 01, 2007
JOURNAL FREE ACCESSWe successfully synthesized the potent and selective group II mGluR agonist (+)-1 (MGS0008) via a process incorporating the key step of efficient fluorination of epoxide (±)-5c. This method would be adaptable to large-scale synthesis to produce (+)-1 in multi-gram quantities.View full abstractDownload PDF (240K) -
Ponnurengam Malliappan Sivakumar, Sethu Kailasam Geetha Babu, Doble Mu ...2007 Volume 55 Issue 1 Pages 44-49
Published: 2007
Released on J-STAGE: January 01, 2007
JOURNAL FREE ACCESSDesign of compounds having good anti-tubercular activity is gaining much importance in the field of tuberculosis research due to reemergence of antibiotic resistance strains. In this paper quantitative structure activity relationships (QSAR) were developed on chalcones, chalcone-like compounds, flavones and flavanones to understand the relationship between biological activity and structural features. Genetic function approximation (GFA) method was used to identify the descriptors that would lead to good regression equations. The best molecular descriptors identified were Jurs descriptors (Jurs charged partial surface area), hydrogen bond donor, principal moment of inertia, molecular energy, dipole magnetic, molecular area, absorption, distribution, metabolism and excretion (ADME) properties and Chi indices (Kier & Hall chi connectivity indices). Excellent statistically significant models were developed by this approach (r2=0.8—0.97) for the four groups of compounds. The cross validated r2 (XV r2) which is an indication of the predictive capability of the model for all the cases was also very good (=0.79—0.94).View full abstractDownload PDF (117K) -
Kun-Teng Wang, Lih-Geeng Chen, Ling-Ling Yang, Wei-Ming Ke, Hsing-Chan ...2007 Volume 55 Issue 1 Pages 50-56
Published: 2007
Released on J-STAGE: January 01, 2007
JOURNAL FREE ACCESSIn Asia, processed Atractylodis Rhizoma, the dried rhizome of Atractylodes ovata DE CANDOLLE (Compositae), is widely used as a tonic agent in herbal diets; stir-frying with soil is the most common processing method. In this study, we focused on determining variations in the function and concentrations of sesquiterpenoids in processed Atractylodis Rhizoma. Raw Atractylodis Rhizoma was processed by stir-frying it with different assistant substrates (i.e., red soil and burnt clay). The results indicated that there was less atractylon in stir-fried materials than in raw materials. However, there were higher levels of atractylenolides II and III in stir-fried materials than in raw materials. We also found that the heavy-metal content in burnt clay exceeded regulations set by the Taiwanese government. Moreover, commercial Atractylodis Rhizoma in Taiwan exhibited great differences in concentrations of the active components. In addition, atractylon showed stronger cytotoxicity than atractylenolides II and III in various cell lines. Therefore, we suggest that the toxic effects of atractylon are reduced following atractylon degradation to atractylenolides II and III. In conclusion, the toxicity of Atractylodis Rhizoma is reduced through processing.View full abstractDownload PDF (143K) -
Masayuki Yoshikawa, Toshio Morikawa, Seikou Nakamura, Ning Li, Xian Li ...2007 Volume 55 Issue 1 Pages 57-63
Published: 2007
Released on J-STAGE: January 01, 2007
JOURNAL FREE ACCESSSeven new acylated oleanane-type triterpene oligoglycosides, theasaponins A4 (1), A5 (2), C1 (3), E8 (4), E9 (5), G1 (6), and H1 (7), were isolated from the seeds of Japanese tea plant (Camellia sinensis). The structures of 1—7 were elucidated on the basis of chemical and physicochemical evidence.View full abstractDownload PDF (159K) -
Norbert Handler, Walter Jaeger, Helmut Puschacher, Klaus Leisser, Thom ...2007 Volume 55 Issue 1 Pages 64-71
Published: 2007
Released on J-STAGE: January 01, 2007
JOURNAL FREE ACCESSCurcumin, a major yellow pigment and active component of turmeric, has been shown to possess anti-inflammatory and anti-cancer activities. Recent studies have indicated that cyclooxygenase-1 (COX-1) plays an important role in inflammation and carcinogenesis. In order to find more selective COX-1 inhibitors a series of novel curcumin derivatives was synthesized and evaluated for their ability to inhibit this enzyme using in vitro inhibition assays for COX-1 and COX-2 by measuring PGE2 production. All curcumin analogues showed a higher rate of COX-1 inhibition. The most potent curcumin compounds were (1E,6E)-1,7-di-(2,3,4-trimethoxyphenyl)-1,6-heptadien-3,5-dione (4) (COX-1: IC50=0.06 μM, COX-2: IC50>100 μM, selectivity index>1666) and (1E,6E)-methyl 4-[7-(4-methoxycarbonyl)phenyl]-3,5-dioxo-1,6-heptadienyl]benzoate (6) (COX-1: IC50=0.05 μM, COX-2: IC50>100 μM, selectivity index>2000). Curcumin analogues therefore represent a novel class of highly selective COX-1 inhibitors and promising candidates for in vivo studies.View full abstractDownload PDF (948K) -
Love Kumar Soni, Satish Gopalrao Kaskhedikar2007 Volume 55 Issue 1 Pages 72-75
Published: 2007
Released on J-STAGE: January 01, 2007
JOURNAL FREE ACCESSDesigning of a highly selective, potent and safe inhibitor of aldose reductase (ALR) capable of potentially blocking the excess glucose flux through the polyol pathway that prevails under diabetic condition has been a long standing challenge. In our study, we did quantitative structure–activity relationship (QSAR) analysis, based on Fujita–Ban and classical Hansch approach, on 5-[[2-(ω-carboxyalkoxy)aryl]methylene]-4-oxo-2-thioxothiazolidine derivatives. Study gave structural insight into the binding mode of the molecules to the aldose reductase enzyme. The Fujita–Ban approach revealed that benzylidene thiazolidine nucleus is more potent as compare to naphthyl-methylene thiazolidine analogs. The bulkierness of naphthyl-methylene might be inquisitive with receptor. Hansch approach suggested that electron-withdrawing groups are conducive to aldose reductase inhibitory activity.View full abstractDownload PDF (79K) -
Veerachamy Alagarsamy, Sankaranarayanan Murugesan2007 Volume 55 Issue 1 Pages 76-80
Published: 2007
Released on J-STAGE: January 01, 2007
JOURNAL FREE ACCESSA variety of novel 3-(4-methoxyphenyl)-2-substitutedamino-quinazolin-4(3H)-ones were synthesized by reacting the amino group of 2-hydrazino-3-(4-methoxyphenyl)-quinazolin-4(3H)-one with a variety of alkyl and aryl ketones. The starting material 2-hydrazino-3-(4-methoxyphenyl)-quinazolin-4(3H)-one was synthesized from 4-methoxyaniline. The title compounds were investigated for analgesic, anti-inflammatory and ulcerogenic index activities. While the test compounds exhibited significant activity, compounds 2-(1-methylpropylidene)-hydrazino-3-(4-methoxyphenyl)-quinazolin-4(3H)-one (A1), 2-(1-ethylpropylidene)-hydrazino-3-(4-methoxyphenyl)-quinazolin-4(3H)-one (A2) and 2-(1-methylbutylidene)-hydrazino-3-(4-methoxyphenyl)-quinazolin-4(3H)-one (A3) showed moderately more potent analgesic activity and the compound 2-(1-methylbutylidene)-hydrazino-3-(4-methoxyphenyl)-quinazolin-4(3H)-one (A3) showed moderately more potent anti-inflammatory activity when compared to the reference standard diclofenac sodium. Interestingly the test compounds showed only mild ulcerogenic potential when compared to aspirin.View full abstractDownload PDF (120K) -
Kornvika Charupant, Khanit Suwanborirux, Surattana Amnuoypol, Emi Sait ...2007 Volume 55 Issue 1 Pages 81-86
Published: 2007
Released on J-STAGE: January 01, 2007
JOURNAL FREE ACCESSJorunnamycins A—C (1a—c), three stabilized renieramycin-type bistetrahydroisoquinolines, were isolated from the mantles, the visceral organs, and the egg ribbons of the Thai nudibranch Jorunna funebris that was pretreated with potassium cyanide (KCN), along with five known compounds, renieramycins M (2m), N (2n), O (2o), and Q (2q) and mimosamycin (3). The structures of 1a—c were elucidated from spectroscopic data and by chemical conversion of renieramycin M (2m) into 1c via 1a. The chemical stability and the oxidative degradation generating simple isoquinoline alkaloids of a carbinolamine analog 1d, which was easily prepared by reacting 1c with silver nitrate in aqueous acetonitrile, are discussed. The results of cytotoxicity studies are also presented.View full abstractDownload PDF (168K) -
Yan Shi, Xiancheng Zhan, Lie Ma, Bing Lin, Linli Li, Chengrong Li, Nin ...2007 Volume 55 Issue 1 Pages 87-91
Published: 2007
Released on J-STAGE: January 01, 2007
JOURNAL FREE ACCESSA drug stability experiment accelerated by compressed oxygen was established. The stability of 10% ascorbic acid solution as a model was studied and the kinetic parameters were obtained with the newly established experimental method. Because ascorbic acid degrades under both anaerobic and aerobic conditions, the total rate constant ktotal can be expressed as: ktotal=kanaerobic+kaerobic, where kanaerobic and kaerobic are the rate con-stants of anaerobic and aerobic degradations, respectively. The kanaerobic can be expressed as kanaerobic=Aanaerobic·exp(−Ea,anaerobic/RT) according to Arrhenius equation, and the kaerobic was found to be kaerobic=Aaerobic·exp(−Ea,aerobic/RT)·pO2 in our study.View full abstractDownload PDF (236K) -
Takafumi Nakatani, Katsuaki Jinpo, Naoki Noda2007 Volume 55 Issue 1 Pages 92-94
Published: 2007
Released on J-STAGE: January 01, 2007
JOURNAL FREE ACCESSFive cantharidin-related compounds were isolated from the Chinese blister beetle, Mylabris phalerate PALLAS (Meloidae). Their structures were determined based on spectroscopic and chemical evidence. Three of them were identified as cantharimide dimers, which consist of two units of cantharimide combined with a tri-, tetra-, or penta-methylene group.View full abstractDownload PDF (94K) -
Akikazu Kakehi, Hiroyuki Suga, Hirohide Isogai2007 Volume 55 Issue 1 Pages 95-101
Published: 2007
Released on J-STAGE: January 01, 2007
JOURNAL FREE ACCESSVarious thieno[3,4-b]indolizine derivatives having an acylmethylthio or (3-ethoxycarbonyl-2-propenyl)thio group at the 3-position which could not be obtained by a conventional method were prepared by a new procedure using cyanoethyl group as a protecting group and their intramolecular arene–π interactions were investigated. In the 1H-NMR spectra of these thieno[3,4-b]indolizines, the low-field shifts (δ 0.10—0.33 ppm) for the 5-protons were observed in comparison with those of 3-(methylthio)thieno[3,4-b]indolizines as a standard. The UV spectra also exhibited a characteristic absorption band at 425—445 nm attributable to the arene–π interaction but their intensities were generally lower than those of 3-(arylmethylthio)thieno[3,4-b]indolizines. In their X-ray analyses, the anti conformation for 3-(acylmethylthio)thieno[3,4-b]indolizines and the gauche one for the 3-(3-ethoxycarbonyl-2-propenyl)thio derivatives were exhibited.View full abstractDownload PDF (331K)
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Nino Tabatadze, Riad Elias, Robert Faure, Pascal Gerkens, Marie Claire ...2007 Volume 55 Issue 1 Pages 102-105
Published: 2007
Released on J-STAGE: January 01, 2007
JOURNAL FREE ACCESSThree new oleanane-type saponins, giganteosides L (1), M (2) and N (3) along with eight known ones were isolated from the roots of Cephalaria gigantea. Their structures were established as 3-O-[β-D-galactopyranosyl-(1→2)-β-D-glucuronopyranosyl]-28-O-[β-D-glucopyranosyl-(1→6)-β-D-glucopyranosyl]-oleanolic acid, 3-O-[β-D-galactopyranosyl-(1→2)-β-D-glucuronopyranosyl]-28-O-[β-D-glucopyranosyl-(1→6)-β-D-glucopyranosyl]-hederagenin, 3-O-[α-L-rhamnopyranosyl-(1→2)-β-D-glucuronopyranosyl]-28-O-[β-D-glucopyranosyl-(1→6)-β-D-glucopyranosyl]-hederagenin, respectively, by means of spectroscopic methods (1D and 2D NMR, HR-ESI-MS). Cytotoxic activity of monodesmosides was investigated in vitro using three cancer cell lines, namely, human non pigmented melanoma MEL-5 and human leukemia HL-60. Giganteosides D (4) and E (5) showed antiproliferative effect on human cell lines with IC50 values in the range 3.15—7.5 μM.View full abstractDownload PDF (88K) -
Hisashi Matsuda, Sachiko Sugimoto, Toshio Morikawa, Koudai Matsuhira, ...2007 Volume 55 Issue 1 Pages 106-110
Published: 2007
Released on J-STAGE: January 01, 2007
JOURNAL FREE ACCESSThe ethyl acetate-soluble fraction of the methanolic extract from the seeds of Psoralea corylifolia was found to inhibit the release of β-hexosaminidase, as a marker of antigen-IgE-induced degranulation in RBL-2H3 cells. Sixteen constituents were isolated from the ethyl acetate-soluble fraction and several constituents, Δ1,3-hydroxybakuchiol (IC50=49 μM), Δ3,2-hydroxybakuchiol (69 μM, bavachin (58 μM), and psoralidin (ca. 100 μM), showed inhibitory activities against the antigen-induced degranulation.View full abstractDownload PDF (155K) -
Nobuko Mibu, Kazumi Yokomizo, Nobuhiro Kashige, Fumio Miake, Takeshi M ...2007 Volume 55 Issue 1 Pages 111-114
Published: 2007
Released on J-STAGE: January 01, 2007
JOURNAL FREE ACCESSN-Monoacyl-2,6-diaminopyridines (2a—c) and N,N′-diacyl-2,6-diaminopyridines (3a—c) were synthesized from 2,6-diaminopyridine by acylation with the corresponding acyl halide or by dehydration with the corresponding carboxylic acid using 1,3-dicyclohexylcarbodiimide (DCC). The antiviral activities of N-monoacyl- and N,N′-diacyl-2,6-diaminopyridines (2a—c and 3a—c) were estimated using plaque reduction assay with HSV-1. All N-monoacyl derivatives (2a—c) showed significant anti-herpes simplex virus (HSV)-1 activity (EC50=15.3—18.5 μg/ml). The CC50 values of 2a—c measured using Vero cells ranged at 37.5—50.0 μg/ml. These compounds showed no significant antibacterial activities with Escherichia coli or Staphylococcus aureus even at a concentration of 1 mg/ml. The N,N′-diacyl derivatives (3a—c) showed no significant anti-HSV-1 activity.View full abstractDownload PDF (76K) -
Raghvendra Dubey, Narayana Subbiah Hari Narayana Moorthy2007 Volume 55 Issue 1 Pages 115-117
Published: 2007
Released on J-STAGE: January 01, 2007
JOURNAL FREE ACCESSBenzimidazole and their derivative were reported to have wide biological activities and were synthesized by using different solvents and ring closing agents. The present work deals with the comparative synthesis of 2-alkyl and aryl substituted benzimidazole derivative in the presence of polyphosphoric acid through microwave and conventional methods and also studied the effect of salt form of reactant for completion of the reaction. The 2-substituted aryl and alkyl benzimidazole derivative were synthesized via microwave and was observed to be more beneficial, in respect of yield (increases up to 10 to 50%) and time (96 to 98% was reduced) than conventional method of synthesis. This study was concluded that the salt form of reactant (o-phenylenediamine dihydrochloride) gave reduced colour impurities, homogenous mixing and reduced time for completion of reaction.View full abstractDownload PDF (70K) -
Athar Ata, Leigha J. Conci, Jordan Betteridge, Ilkay Orhan, Bilge Sene ...2007 Volume 55 Issue 1 Pages 118-123
Published: 2007
Released on J-STAGE: January 01, 2007
JOURNAL FREE ACCESSFungal catalysis of sclareolide (1) using Mucor plumbeus (ATCC 4740), Cunninghamella blakesleeana (ATCC 9245), Cunninghamella echinulata (ATCC 9244), Curvularia lunata (ATCC 12017) and Aspergillus niger (ATCC 1004), was performed. Cunninghamella blakesleeana (ATCC 9245) metabolized compound 1 to afford O6-sclareolide (2), 3β,6α-dihydroxysclareolide (3), 9-hydroxysclareolide (4), along with three known metabolites, 1β,3β-dihydroxysclareolide (5), 3-oxosclareolide (6) and 3β-hydroxysclareolide (7). Biotransformation experiments of compound 1 with Cunninghamella echinulata (ATCC 9244) also yielded two new compounds, 5-hydroxysclareolide (8), and 7β-hydroxysclareolide (9) along with two known compounds 5 and 7. Spectroscopic methods were used to establish the structures of compounds 2—9. Compounds 2—9 exhibited modest acetylcholinesterase inhibitory activity.View full abstractDownload PDF (148K) -
Fumiko Fujisaki, Marumi Oishi, Kunihiro Sumoto2007 Volume 55 Issue 1 Pages 124-127
Published: 2007
Released on J-STAGE: January 01, 2007
JOURNAL FREE ACCESSThe preparation of amide derivatives (4) by N-acylation of unprotected α-amino acids is easily achieved via readily available benzotriazolyl carboxylates (2a—d) or succinimidyl carboxylates (2e—f). These intermediates (2) are prepared from reaction of carboxylic acids (1) with 1-hydroxybenzotriazole (HO-Bt) or N-hydroxysuccinimide (HO-Su) in the presence of equimolar amounts of 1-ethyl-3-(3′-dimethylaminopropyl)carbodiimide hydrochloride (WSCI). The overall yields of the target compounds (4) were excellent, and this two-stage procedure could be applicable as an alternative procedure for one-pot reaction.View full abstractDownload PDF (121K) -
Shi-Kai Yan, Yan-Wen Wu, Run-Hui Liu, Wei-Dong Zhang2007 Volume 55 Issue 1 Pages 128-132
Published: 2007
Released on J-STAGE: January 01, 2007
JOURNAL FREE ACCESSMajor bioactive components in various Calculus Bovis, including natural, artificial and in-vitro cultured Calculus Bovis, were comparatively studied. An approach of high-performance liquid chromatography coupled with ultraviolet and evaporative light scattering detections (HPLC/UV/ELSD) was established to simultaneously determinate six bioactive components thereof, including five bile acids (cholic acid, deoxycholic acid, ursodeoxycholic, chenodeoxycholic acid, hyodeoxycholic acid) and bilirubin. ELSD and UV detector were applied to detect bile acids and bilirubin respectively. The assay was performed on a C18 column with water–acetonitrile gradient elution and the investigated constituents were authenticated by comparing retention times and mass spectra with those of reference compounds. The proposed method was applied to analyze twenty-one Calculus Bovis extraction samples, and produced data with acceptable linearity, precision, repeatability and accuracy. The result indicated the variations among Calculus Bovis samples under different developmental conditions. Artificial and in-vitro cultured Calculus Bovis, especially in-vitro cultured ones, which contain total bioactive constituents no less than natural products and have the best batch-to-batch uniformity, suffice to be used as substitutes of natural Calculus Bovis.View full abstractDownload PDF (358K) -
Hisahiro Kai, Masaki Baba, Toru Okuyama2007 Volume 55 Issue 1 Pages 133-136
Published: 2007
Released on J-STAGE: January 01, 2007
JOURNAL FREE ACCESSTwo new megastigmane, cucumegastigmanes I (1) and II (2), together with a known megastigmane, (+)-dehydrovomifoliol (3), and five other known compounds were isolated from the leaves of Cucumis sativus. The structures of the new compounds were elucidated from spectroscopic analysis and their absolute stereochemistries were determined in detail using the chemical conversion and a modified Mosher's method.View full abstractDownload PDF (128K) -
Jun Lee, Dongho Lee, Dae Sik Jang, Joo-Won Nam, Jong-Pyung Kim, Ki Hun ...2007 Volume 55 Issue 1 Pages 137-139
Published: 2007
Released on J-STAGE: January 01, 2007
JOURNAL FREE ACCESSTwo new stereoisomers of tetrahydrofuranoid lignans, 7S,8R,7′S,8′R- (1) and 7R,8S,7′S,8′R-3,4,3′,4′-tetramethoxy-9,7′-dihydroxy-8.8′,7.O.9′-lignan (2) along with nine known lignans including tetrahydrofuranoids (3, 4) and tetrahydrofurofuranoids (5—11) were isolated from a CHCl3-soluble fraction of the flower buds of Magnolia fargesii. Two tetrahydrofuranoids, magnostellin A (3) and lariciresinol dimethyl ether (4) were isolated from this species for the first time. The structures of these compounds (1—11) were identified by spectroscopic methods as well as by comparison with published values. Absolute configurations of new stereoisomers (1, 2) were determined by the Mosher's esterification method and Circular Dichroism (CD) studies. All the isolates (1—11) were evaluated for their antioxidant activities using modified superoxide radical-scavenging assay. Compounds 5—8 showed the potent superoxide radical-scavenging activities with the ED50 values of 19.2, 19.2, 16.5, and 27.7 μM, respectively, as compared with standard antioxidants (BHA: 22.8 μM; Trolox: 940 μM).View full abstractDownload PDF (114K) -
Song-Lin Li, Ru Yan, Yun-Kau Tam, Ge Lin2007 Volume 55 Issue 1 Pages 140-144
Published: 2007
Released on J-STAGE: January 01, 2007
JOURNAL FREE ACCESSRhizoma Chuanxiong (Ligusticum chuanxiong HORT.) is a commonly used traditional Chinese medicinal herb for the treatment of cardiovascular disorders. Significant variations of the main components in this herb were observed in commercial samples. The present study investigated effects of post-harvest drying and processing methods on nine main components in the herb. Results showed that drying at 60 °C or under the sun the contents of three major constituents, namely senkyunolide A (4), coniferylferulate (5) and Z-ligustilide (6), decreased significantly, while the contents of ferulic acid (1), riligustilide (8) and levistolide A (9) increased significantly. Senkyunolide I (2) and senkyunolide H (3), which were not detected in fresh herbs, appeared in dried samples. Similar chemical alterations, such as decrease in the contents of three major ingredients and increase in the contents of compounds 1, 2, 3, 8 and 9, were also observed in differently processed herbal samples. The possible converting mechanisms of these components were clarified by employing pure major components treated under the same conditions.View full abstractDownload PDF (461K) -
Akihito Yokosuka, Yoshihiro Mimaki2007 Volume 55 Issue 1 Pages 145-149
Published: 2007
Released on J-STAGE: January 01, 2007
JOURNAL FREE ACCESSThree new spirostanol glycosides (1—3) and a new furostanol glycoside (4), together with two known spirostanol glycosides (5 and 6) were isolated from the whole plants of Agave utahensis (Agavaceae). The structures of the new compounds were determined by spectroscopic analysis and the results of hydrolytic cleavage.View full abstractDownload PDF (114K) -
So Young Park, Seong Su Hong, Xiang Hua Han, Ji Sang Hwang, Dongho Lee ...2007 Volume 55 Issue 1 Pages 150-152
Published: 2007
Released on J-STAGE: January 01, 2007
JOURNAL FREE ACCESSA new butyrolactone sesquilignan, isolappaol C (1), together with four known lignans, lappaol C (2), lappaol D (3), lappaol F (4), and diarctigenin (5), were isolated from the methanolic extract of the seeds from the Arctium lappa plant. The structure of isolappaol C (1) was determined by spectral analysis including 1D- and 2D-NMR. All the isolates were evaluated for their inhibitory effects on the LPS-induced nitric oxide production using murine macrophage RAW264.7 cells. Lappaol F (4) and diarctigenin (5) strongly inhibited NO production in the LPS-stimulated RAW264.7 cells with IC50 values of 9.5 and 9.6 μM, respectively.View full abstractDownload PDF (101K) -
Ryuichiro Suzuki, Miki Iijima, Yoshihito Okada, Toru Okuyama2007 Volume 55 Issue 1 Pages 153-155
Published: 2007
Released on J-STAGE: January 01, 2007
JOURNAL FREE ACCESSA new sesquiterpene along with 15 known compounds were isolated from the style of Zea mays L. These structures were elucidated on the basis of spectroscopic analysis. The ability of these compounds to inhibit glycation in vitro was analyzed. This allowed determination of chemical functional groups required for the inhibition of glycation.View full abstractDownload PDF (100K) -
Shin-ichi Hirashima, Akichika Itoh2007 Volume 55 Issue 1 Pages 156-158
Published: 2007
Released on J-STAGE: January 01, 2007
JOURNAL FREE ACCESSAldehydes were found to be oxidized with molecular oxygen to the corresponding carboxylic acid in the presence of catalytic hydrobromic acid or bromine under photo-irradiation.View full abstractDownload PDF (124K)
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