Abstract:
:Several Pt(IV) and Pt(II) complexes containing 1R,2R-cyclohexanediamine (1R,2R-dach) as a carrier ligand were synthesized. The cytotoxicities and the uptake of the platinum complexes by leukemia L1210 cells were compared in order to study the correlation between their structures and cytotoxicities. [Pt(II)Cl2(1R,2R-dach)], [(Pt(II)(oxalato)(1R,2R-dach)], and [Pt(II)(malonato)(1R,2R-dach)], which have excellent anticancer properties, exhibited very high cytotoxicities and were easily taken up by leukemia L1210 cells. [Pt(IV)Cl4(1R,2R-dach)], trans(Cl)-[Pt(IV)Cl2(oxalato)(1R,2R-dach)], and trans(Cl)-[Pt(IV)Cl2(malonato)(1R,2R-dach)] also had high cytotoxicities. After a short incubation time, the uptake of [Pt(II)Cl2(1R,2R-dach)], [Pt(II)(oxalato)(1R,2R-dach)], and [Pt(II)(malonato)(1R,2R-dach)] by leukemia L1210 cells were respectively very similar to those of [Pt(IV)Cl4(1R,2R-dach)], trans(Cl)-[Pt(IV)Cl2(oxalato)(1R,2R-dach)], and trans(Cl)-[Pt(IV)Cl2(malonato)(1R,2R-dach)]. In addition, trans(OH)-[Pt(IV)(OH)2Y2(1R,2R-dach)] (Y2: oxalato or malonato) did not exhibit cytotoxicity towards leukemia L1210 cells, whereas trans(Cl)-[Pt(IV)Cl2Y2(1R,2R-dach)] (Y2: oxalato or malonato) were highly cytotoxic. The accumulation of trans(OH)-[Pt(IV)(OH)2Y2(1R,2R-dach)] in leukemia L1210 cells was much lower than that of trans(Cl)-[Pt(IV)Cl2Y2(1R,2R-dach)]. Platinum(IV) complexes, in which leaving groups are replaced by hydroxide groups, have decreased cytotoxic activity, because the hydroxide groups of the platinum(IV) complex reduce the uptake of platinum by the cells. trans(OH),cis(Cl)-[Pt(IV)(OH)2Cl2(1R,2R-dach)], which has hydroxide and chloride groups, was easily incorporated into the cells and exhibited the high cytotoxic activity. This behavior indicates that the chloride group apparently overcomes the ameliorating effect of the hydroxide group.
journal_name
Biol Pharm Bulljournal_title
Biological & pharmaceutical bulletinauthors
Yamashita T,Hirose J,Noji M,Saito R,Tomida H,Kidani Ydoi
10.1248/bpb.16.1014subject
Has Abstractpub_date
1993-10-01 00:00:00pages
1014-8issue
10eissn
0918-6158issn
1347-5215journal_volume
16pub_type
杂志文章abstract::A liposomal formulation of UCN-01 was studied to prevent binding of drug to human alpha1-acid glycoprotein (hAGP). The release of drug from liposomes added to various media was investigated by monitoring the concentration of UCN-01 in different fractions. Protein bound UCN-01 was separated from liposomal UCN-01 and fr...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.28.1259
更新日期:2005-07-01 00:00:00
abstract::To elucidate molecular mechanisms of adipocyte differentiation, we previously isolated TC10-like/TC10betaLong (TCL/TC10betaL), regulators of G protein signaling 2 (RGS2), factor for adipocyte differentiation (fad) 104 and fad158, which were transiently expressed in the early phase of adipogenesis. These four genes see...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.33.404
更新日期:2010-01-01 00:00:00
abstract::A conditioned medium (CM) was prepared by culturing human sperm at 3.0 x 10(6) sperm/ml for 12 h. The fusion index increased significantly when the sperm penetration assay (SPA) was performed with CM (0.6 without CM to 2.0 with CM). The conditioned medium was also effective on the sperm from 11 patients who showed a l...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.18.5
更新日期:1995-01-01 00:00:00
abstract::The potential usefulness of oil in water (O/W) lipid emulsions as parenteral drug delivery system for lipophilic drugs was examined in tumor-bearing rats. A model lipophilic drug, sudan II (PCoct = 226000), was formulated in five lipid emulsions consisting of soybean oil and various surfactants. Compared with HCO-60 m...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.17.1490
更新日期:1994-11-01 00:00:00
abstract::Only a few biosynthetic pathways in fungal cells have been used as antifungal targets. Therefore, the number of antifungals has been limited, and a cross-drug resistance among them has emerged in the therapy of mycoses. Under such circumstances, the identification of an antifungal with a new mode of action is highly d...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.18.1267
更新日期:1995-09-01 00:00:00
abstract::The oligopeptide transporter PEPT1 (SLC15A1) is responsible for absorption of peptidic nutrients in the small intestine. Although the L-diastereomer of the beta-lactam antibiotic cephalexin (L-cephalexin) is likely to be transported by PEPT1, there has been no direct demonstration of PEPT1-mediated L-cephalexin transp...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.32.1459
更新日期:2009-08-01 00:00:00
abstract::The mature form of rat adrenodoxin (Ad) was purified from a heterologous direct expression system in Escherichia coli with a yield of 56 mg/l culture. The purified Ad showed a A414/A280 ratio of 0.91 and the sequence of 10 amino terminal residues was identical with that of authentic rat Ad. By Time of Flight/Mass spec...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.21.1106
更新日期:1998-10-01 00:00:00
abstract::The effects of aged garlic extract (AGE) on longevity and learning and memory performances were studied in the senescence accelerated mouse (SAM). A solid diet containing 2% (w/w) AGE was given to SAM from 2 months of age. The survival ratio of SAM P8, senescence accelerated animals, treated with AGE was significantly...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.17.1589
更新日期:1994-12-01 00:00:00
abstract::We have studied lysosomal proteases capable of degrading a major form of cytochrome P450 (CYP2B1) which was purified from the liver microsomes of phenobarbital-treated rats. After incubation of CYP2B1 with extracts of triton-filled lysosomes (tritosomes), its proteolysis was measured by a quantitative immunoblot proce...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.17.568
更新日期:1994-05-01 00:00:00
abstract::Tetrandrine (TET), a bis-benzylisoquinoline alkaloid isolated from the dried root of hang-fang-chi (Stephania tetrandra S. Moore), is traditionally used in China for treating inflammation, hypertension and silicosis. In this study, our aim was to examine the anti-inflammatory mechanism of TET through measuring the ind...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.30.59
更新日期:2007-01-01 00:00:00
abstract::Costunolide, isolated from the stem bark of Magnolia sieboldii, is a sesquiterpene lactone that exhibits various biological and immunological actions. We investigated the induction mechanism of apoptosis by costunolide in a human B cell leukemia NALM-6 cell culture system. Costunolide (10 microM)-induced apoptosis tim...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.31.1024
更新日期:2008-05-01 00:00:00
abstract::CC chemokine receptor 4 (CCR4) is generally recognized as a preferential marker for T helper 2 cells, and we have previously reported morpholine-derivative CCR4 antagonists, RS-1154 and RS-1269. Here, we investigate the pharmacological profiles of a novel pyrimidine-derivative CCR4 antagonist, 2-{4-[2-(diethylamino)et...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.33.1067
更新日期:2010-01-01 00:00:00
abstract::In the present study, we evaluated the effect of the novel acid pump antagonist 7-(4-fluorobenzyloxy)-2,3-dimethyl-1-{[(1S,2S)-2-methylcyclopropyl]methyl}-1H-pyrrolo[2,3-d]pyridazine (CS-526) on the intragastric acidity of cynomolgus monkeys. The study was performed in a crossover manner with five male animals. CS-526...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.32.2010
更新日期:2009-12-01 00:00:00
abstract::The effects of a liquid nutritive and tonic drug (NTD) selected from a modification of the "Kai-xin-shou-yu-shen-qi-wan" prescription, on scopolamine-induced amnesia in mice were investigated using the passive avoidance and water-maze tasks. A popular NTD in Japan that contains 17 crude (natural) drug extracts togethe...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.28.1886
更新日期:2005-10-01 00:00:00
abstract::Coagulase-negative Staphylococcus (CNS) strains are frequently associated with bacteremia and hospital-acquired infections. 293 CNS strains were isolated from 744 samples from a dialysis center in S. M. de Tucumán, Argentina, from hemocultures, catheters and urine and identified as S. epidermidis, S. haemolyticus, S. ...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.29.1592
更新日期:2006-08-01 00:00:00
abstract::Cerebral ischemia causes the depletion of oxygen and nutrition from brain tissues, and when persistent, results in irreversible damage to the cell function and survival. The cellular response to ischemic conditions and its mechanisms have been investigated widely in in vivo and in vitro experimental models, yet no stu...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.34.764
更新日期:2011-01-01 00:00:00
abstract::We investigated the cytotoxicity of eight vitamin K3 (VK3) analogs against neuroblastoma cell lines (IMR-32, LA-N-1, NB-39, and SK-N-SH) and normal cell lines (human umbilical vein endothelial cells (HUVEC) and human dermal fibroblasts (HDF)) using a 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide (MTT) a...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.35.617
更新日期:2012-01-01 00:00:00
abstract::Coenzyme Q10 (Co-Q10) is a vitamin-like supplement which appears to be safe, with minimal side effects and low drug interaction potential. Co-Q10 is used in the treatment of a variety of disorders related primarily to suboptimal cellular energy metabolism and oxidative injury. Studies supporting the efficacy of Co-Q10...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.b16-00124
更新日期:2016-01-01 00:00:00
abstract::A possible evaluation technique was devised for examing timely cholesterol synthetic activity in the rat liver. The principle of the technique is to measure the incorporation rate of 14C atoms into a few target metabolites excreted in bile with time after an intraportal injection of [1,2-14C] acetate to the conscious ...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.18.1467
更新日期:1995-11-01 00:00:00
abstract::We showed previously that transdifferentiation of skin epidermis to mucous epithelium can be induced by treatment with 20 µM retinol for 1 d followed by culture for 4 d without retinol in chick embryonic tarsometatarsal skin. In mouse epidermal cells, 3 µM retinoic acid (an active metabolite of retinol) inhibits epide...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.34.1227
更新日期:2011-01-01 00:00:00
abstract::Ferulic acid (FA), a naturally occurring polyphenol abundant in vegetables and rice bran, is known to possess a potent antioxidant activity, thereby protecting cells from oxidative stress. In the present study, we show that in addition to its known anti-oxidant activity, ferulic acid exerts substantial inhibitory acti...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.b12-00695
更新日期:2013-01-01 00:00:00
abstract::The phylogenetic relationship of Cistanche deserticola, C. salsa and C. tubulosa was analyzed by comparing the nucleotide sequences of the plastid rps2 gene and the intergenic spacer region between rpl16 and rpl14. By comparison of sequence data, the Cistanche samples were distinguishable from each other. The results ...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.25.218
更新日期:2002-02-01 00:00:00
abstract::Possible involvement of the peripheral-type benzodiazepine receptor (PBR) in hemin/protoporphyrin-induced erythroid differentiation of human leukemia K562 cells was investigated by the use of the ligands, diazepam and PK11195. Diazepam itself exhibited differentiation-inducing activity on K562 cells. The PBR-specific ...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.18.903
更新日期:1995-06-01 00:00:00
abstract::Vesicular glutamate transporter (VGLUT) is responsible for the active transport of L-glutamate into synaptic vesicles and, thus, plays an essential role in the glutamatergic chemical transmission in the central and peripheral nervous systems. Recent studies indicated that VGLUT is also expressed and localized in vario...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章,评审
doi:10.1248/bpb.31.1844
更新日期:2008-10-01 00:00:00
abstract::Electrets are polymeric discs that carry semi permanent electrostatic charge. These provide electrostatic potentials in the range of 500 to 3,000 V. In the current work, the effect of electret exposure on the skin permeability was investigated. Transdermal transport studies were carried out across porcine epidermis in...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.31.99
更新日期:2008-01-01 00:00:00
abstract::In most species, solar light is both a DNA-damaging agent and the key entraining stimulus for the endogenous circadian clock. The zebrafish is an attractive vertebrate system in which to study the influence of light on gene expression because the DNA repair proteins and circadian oscillators in this species are light-...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.34.1343
更新日期:2011-01-01 00:00:00
abstract::Defining a quantitative and reliable relationship between in vitro drug release and in vivo absorption is highly desired for rational development, optimization, and evaluation of controlled-release dosage forms and manufacturing process. During the development of once daily extended-release (ER) tablet of glipizide, a...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.31.1946
更新日期:2008-10-01 00:00:00
abstract::Transport mechanisms of p-aminohippurate (PAH) were investigated in rat renal brush-border membrane vesicles. The uptake of PAH was stimulated by an inside-positive membrane potential created by K+ and valinomycin. This potential-stimulated uptake of PAH was inhibited by various anion transport inhibitors and was satu...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.16.395
更新日期:1993-04-01 00:00:00
abstract::The aim of the present study was to determine the effect of sulfaphenazole (SP) on the pharmacokinetics of ampiroxicam (AM) which is metabolized by cytochrome P-450 (CYP) 2C9, since SP is a potent inhibitor of CYP 2C9, and so a dramatic pharmacokinetic drug interaction between both drugs is assumed after dosing. Singl...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.22.191
更新日期:1999-02-01 00:00:00
abstract::A novel tricyclic 21-amino-acid peptide, FR901724, was isolated from the cultured broth of Streptomyces sp. No. 73264. This peptide appears to possess potent anti-human immunodeficiency virus (HIV) activity in vitro and might represent a lead to a new class of anti-HIV agents; it qualifies as an HIV-cell fusion inhibi...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.19.405
更新日期:1996-03-01 00:00:00