Chemical and Pharmaceutical Bulletin
Online ISSN : 1347-5223
Print ISSN : 0009-2363
ISSN-L : 0009-2363
53 巻, 6 号
選択された号の論文の29件中1~29を表示しています
Regular Articles
  • Xun Sun, You-Rong Duan, Qin He, Jiao Lu, Zhi-Rong Zhang
    2005 年 53 巻 6 号 p. 599-603
    発行日: 2005年
    公開日: 2005/06/01
    ジャーナル フリー
    Biodegradable monomethoxy(polyethyleneglycol)–poly(lactide-co-glycolide)–monomethoxy(poly-ethyleneglycol) (PELGE) copolymers were synthesized by ring-opening polymerization to formulate plasmid DNA loaded nanoparticles. A double emusion method with polyvinyl alcohol as the emulsifier in the external aqueous phase was employed to prepare nanoparticles. The effects of monomethoxypoly(ethyleneglycol) (mPEG) segments in the polymer on particle size, zeta potential, encapsulation efficiency and in vitro release were investigated. It was found that the introduction of a certain amount of hydrophilic mPEG segments in the copolymer chains could improve the affinity of copolymer with plasmid DNA and enhance the emulsification ability of the copolymer. Thus DNA loaded nanoparticles with smaller particle sizes and higher encapsulation efficiencies were obtained by using PELGE copolymer as the matrix.
  • Mohammad Sohel Rana, Keietsu Tamagake
    2005 年 53 巻 6 号 p. 604-606
    発行日: 2005年
    公開日: 2005/06/01
    ジャーナル フリー
    Electrochemical formation of ferryl porphyrin was examined by electrocatalytic oxidation of alkene by measuring luminol chemiluminescence using a flow-injection method. Emission was observed both below the reduction potential of FeIIITMPyP (−0.08 V at pH 11, −0.02 V at pH 7 and 0.15 V at pH 3) and above the oxidation potential (0.6 V at pH 11, 0.75 V at pH 7 and 1.1 V at pH 3). However, both anodic and cathodic emissions were inhibited significantly by the addition of alkene (cyclopent-2-ene-1-acetic acid) solutions downstream of the working electrode. Further, the spectra at both anodic and cathodic sides shifted to the longer wavelength (>424 nm) compared to the original spectrum of FeIIITMPyP (422 nm), which was not observed with the addition of alkene solution. Therefore, the results suggest that the electrochemically generated oxo-ferryl species have been engaged in catalytic oxidation of alkene before the flow reaches the observation cell.
  • Xiaodong Wang, Wenyuan Gao, Zhi Yao, Shaoyu Zhang, Yanwen Zhang, Yoshi ...
    2005 年 53 巻 6 号 p. 607-610
    発行日: 2005年
    公開日: 2005/06/01
    ジャーナル フリー
    Five new sesquiterpenes, 1β-furanoyl-2β,3α,7α,8β,11-pentaacetoxy-4α,5α-dihydroxy-dihydroagarofuran (1), 1β,2β,3α,5α,7β,8β,11-heptaacetoxy-dihydroagarofuran (2), 1β-furanoyl-2β,3α,7α,8β,11-pentaacetoxy-5α-hydroxy-dihydroagarofuran (3), 1β,7β,8α-triacetoxy-2β-furanoyl-4α-hydroxy-11-isobutyryloxy-dihydroagarofuran (4), and 1β-nicotinoyl-2β,5α,7β-triacetoxy-4α-hydroxy-11-isobutyryloxy-8α-furanoyl-dihydroagarofuran (5), were isolated from the xylem of Tripterygium wilfordii, together with a known compound (6). Their structures were elucidated on the basis of spectroscopic studies. Compounds 2—5 showed significant immunosuppressive activities.
  • Sanjay Bajaj, Surinder Singh Sambi, Anil Kumar Madan
    2005 年 53 巻 6 号 p. 611-615
    発行日: 2005年
    公開日: 2005/06/01
    ジャーナル フリー
    Relationship between topochemical indices and inhibition of CDK2/cyclin A by 3-aminopyrazoles was investigated using a data set comprising of 42 3-aminopyrazoles. Three topochemical indices—the Wiener's topochemical index – a distance based topochemical index, atomic molecular connectivity index – an adjacency based topochemical index and superadjacency topochemical index – an adjacency-cum-distance based topochemical index were used for the present investigations. The values of Wiener's topochemical index, atomic molecular connectivity index and superadjacency topochemical index for each of the 42 compounds comprising the data set were computed using an in-house computer program. Resultant data was subsequently analyzed and suitable models were developed after identification of the active ranges. Subsequently, a biological activity was assigned to each of the compounds using these models, which was then compared with the reported CDK2/cyclin A inhibitory activity. High accuracy of prediction ranging from 86 to 89% was observed using these models.
  • Kenneth Oben Eyong, Karsten Krohn, Hidayat Hussain, Gabriel Ngosong Fo ...
    2005 年 53 巻 6 号 p. 616-619
    発行日: 2005年
    公開日: 2005/06/01
    ジャーナル フリー
    Newbouldiaquinone (1), a new naphthoquinone–anthraquinone coupled pigment and a new ceramide named newbouldiamide (2), have been isolated from Newbouldia laevis, besides the known compounds lapachol (3), canthic acid, oleanolic acid, 2-methyl-9,10-anthracenedione, 2-acetylfuro-1,4-naphthoquinone, 2,3-dimethoxy-1,4-benzoquinone, 2-(4-hydroxyphenyl)ethyl triacontanoate, β-sitosterol and β-sitosterol glucopyranoside. The structure elucidations of the isolated new compounds were performed on the basis of spectroscopic and chemical evidence. Preliminary studies showed that 1 is moderately antibacterial against Gram-positive Bacillus megaterium and that 3 has moderate herbicidal and antibacterial activities.
  • Mei-Ying Ning, Ying-Zhi Guo, Huai-Zhong Pan, He-Ming Yu, Zhong-Wei Gu
    2005 年 53 巻 6 号 p. 620-624
    発行日: 2005年
    公開日: 2005/06/01
    ジャーナル フリー
    Clotrimazole (CT)-containing proliposomes were prepared by penetrating an ethanol solution of CT and Egg phosphatidylcholine (PC) into microporous sorbitol particles, followed by vacuum evaporation of the solvent. As a result, CT proliposomes with free-flowing flowability were obtained. On contact with water, the proliposomes were rapidly converted into a liposomal dispersion, in which a certain amount of CT was entrapped by the liposomes. The result in scanning electronic micrograph confirmed the formation of liposomes structures from proliposomes, and the particles revealed round or ellipse. The ratio of drug to total lipid, ratio of PC to cholesterol and ratio of lipid to sorbitol affected the entrapment efficiency (EE%). The EE% of optimized formulation (CT 10 mg, 0.1 g total lipid, PC/CH ratio is 60 : 40 and 1 g sorbitol) in this investigation was 96.2±1.5%. The proliposomes system can provide sustaining release in simulated vaginal fluid at 37±1 °C for 24 h. In-vivo performance of blank proliposomes, a physical mixture of sorbitol and drug, clotrimazole proliposomes and commercial ointment formulation were evaluated using antifungal activity test. At 7 d post-dose, the c.f.u. of C. albicans decreased in proliposomes-treated groups than ointment and the physical mixture (t-Student, p<0.05). The results indicated that CT-containing vaginal proliposomes prolonged drug release and may increase amount of drug retention into the mucosa to result in more antifungal efficacy. In addition, CT-proliposomes did not affect the morphology of vaginal tissues. Therefore, the dosage form might be further developed for safe, convenient, and effective treatment of vaginal candidasis with reduced dosing interval.
  • Toshio Morikawa, Shin Ando, Hisashi Matsuda, Shinya Kataoka, Osamu Mur ...
    2005 年 53 巻 6 号 p. 625-630
    発行日: 2005年
    公開日: 2005/06/01
    ジャーナル フリー
    The 80% aqueous acetone extract from the rhizomes of Alpinia galanga showed nitric oxide (NO) production inhibitory activities in mouse peritoneal macrophages. From the aqueous acetone extract, three new 8–9′ linked neolignans, galanganal, galanganols A and B, and a sesquineolignan, galanganol C, were isolated together with nine known phenylpropanoids and p-hydroxybenzaldehyde. The structures of new neolignans were determined on the basis of physicochemical and chemical evidence. In addition, the inhibitory effects of the constituents from the rhizomes of A. galanga on NO production induced by lipopolysaccharide in mouse peritoneal macrophages were examined. Among them, galanganal (IC50=68 μM), galanganols B (88 μM) and C (33 μM), 1′S-1′-acetoxychavicol acetate (2.3 μM), 1′S-1′-acetoxyeugenol acetate (11 μM), trans-p-hydroxycinnamaldehyde (ca. 20 μM), trans-p-coumaryl alcohol (72 μM), and trans-p-coumaryl diacetate (19 μM) were found to show inhibitory activity.
  • Hongfei Liu, Shu Zhang, Shufang Nie, Xin Zhao, Xiyang Sun, Xingang Yan ...
    2005 年 53 巻 6 号 p. 631-633
    発行日: 2005年
    公開日: 2005/06/01
    ジャーナル フリー
    Methylacrylic acid/styrene cross-linked with divinylbenzene is a novel pH-sensitive ion exchange resin. Microspheres of this resin were characterized by Fourier transform infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC). The microspheres showed a pulsatile swelling behavior when the pH of the media changed. The pH-sensitive microspheres were loaded with salbutamol sulfate and the drug-release characteristics were studied under both simulated gastric and intestinal pH conditions. The results obtained showed that the drug release also depended on the pH of the release media.
  • Abolghasem Jouyban, Nora Yat Knork Chew, Hak-Kim Chan, Mohammad Sabour ...
    2005 年 53 巻 6 号 p. 634-637
    発行日: 2005年
    公開日: 2005/06/01
    ジャーナル フリー
    Organic solvents are amongst the most powerful solubilization agents for a large number of water-insoluble drugs. A number of equations has been reported for mathematical representation of solute solubility in mixed solvents. The question is then posed—is there a mathematical difference between these models? To address this point, it has been demonstrated that all cosolvency models could be made equivalent by using algebraic manipulations. In order to familiarize the readers with the available cosolvency models, they are briefly reviewed. The models can be divided into two mathematical categories, i.e. linear and non-linear models. The linear models include: the log-linear, extended Hildebrand solubility approach, excess free energy equations, combined nearly ideal binary solvent/Redlich-Kister equation and Margule equations which can be converted to a general single model which expresses the logarithm of mole fraction solubility of a solute as a power series of volume fraction of the cosolvent. The non-linear models include the mixture response surface methods, two step solvation model and modified Wilson model which can be converted to a non-linear general form. Also, it has been shown that both the general single model and a non-linear general model are mathematically identical. To show the applicability of the models on real experimental data, 35 data sets have been collected from the literature. Both linear and nonlinear models produced comparable accuracies when an equal number of constant terms was employed in numerical analyses.
  • Ichiro Hayakawa, Rieko Shioya, Toshinori Agatsuma, Yuichi Sugano
    2005 年 53 巻 6 号 p. 638-640
    発行日: 2005年
    公開日: 2005/06/01
    ジャーナル フリー
    For the construction of new combinatorial libraries, a lead compound was created by replacing the core structure of a hit compound discovered by screening for cytotoxic agents against a tumorigenic cell line. The newly designed compound maintained biological activity and allowed alternative library construction for antitumor drugs.
  • Tae Hoon Kim, Hideyuki Ito, Kikuyo Hayashi, Toshio Hasegawa, Takahisa ...
    2005 年 53 巻 6 号 p. 641-644
    発行日: 2005年
    公開日: 2005/06/01
    ジャーナル フリー
    A phytochemical investigation of the polar constituents in the heartwood of Indian Santalum album L. resulted in the isolation of three new neolignans (1—3) and a new aromatic ester (4), along with 14 known components. The structures of the new compounds (1—4) were established using spectroscopic methods.
  • Yue Wang, Nobuo Okabe
    2005 年 53 巻 6 号 p. 645-652
    発行日: 2005年
    公開日: 2005/06/01
    ジャーナル フリー
    The crystal structures of the three Zn(II) complexes, [Zn(bpy)(o-AB)2] (1) (bpy=2,2′-bipyridine, o-AB=o-aminobenzoic acid=Vitamin L), [Zn(bpy)(m-AB)Cl]2 (2) (m-AB=m-aminobenzoic acid), [Zn(bpy)(p-AB)Cl]·p-AB·H2O (3) (p-AB=p-aminobenzoic acid=Vitamin H′), have been determined and the basic coordination geometries and architectures organized by hydrogen-bonds and π–π interactions also characterized. The substitute amine group at ortho-, meta-, and para-position of AB plays an important role to produce completely different coordination motif of these complexes, further, in all complexes, aromatic amines are not coordinated to Zn(II) atom. While two different types of coordination modes of the carboxylate O atoms are present in these complexes: one mode consists of the usual Zn–O bond lengths (2.009(2)—2.251(2) Å) in complex 1, 2 and 3; another consists of a very long Zn–O bond lengths (2.422(2) Å) in complex 1. Each of the complexes has the characteristic UV absorption bands around 250—310 nm region, and the intense fluorescence band at near 325 nm.
  • Kiyosei Takasu, Tsubasa Shimogama, Chalerm Saiin, Hye-Sook Kim, Yusuke ...
    2005 年 53 巻 6 号 p. 653-661
    発行日: 2005年
    公開日: 2005/06/01
    ジャーナル フリー
    Several β-carbolines including naturally occurring substances and their corresponding cationic derivatives were synthesized and evaluated for antimalarial (antiplasmodial) activity in vitro and in vivo. A tetracyclic carbolinium salt was elucidated for antileishmanial and antitrypanosomal activities in vitro as well as antiplasmodial activity. Quarternary carbolinium cations showed much higher potencies in vitro than electronically neutral β-carbolines and a good correlation was observed between π-delocalized lipophilic cationic (DLC) structure and antimalarial efficacy. β-Carbolinium compounds exhibit medium suppressive activity in vivo against rodent malaria.
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