Abstract：
:The surface topology of ligands on liposomes is an important factor in active targeting in drug delivery systems. Accurately evaluating the density of anchors and bioactive functional ligands on a liposomal surface is critical for ensuring the efficient delivery of liposomes. For evaluating surface ligand density, it is necessary to clarify that on the ligand-modified liposomal surfaces, some anchors are attached to ligands but some are not. To distinguish between these situations, a key parameter, surface anchor density, was introduced to specify amount of total anchors on the liposomal surface. Second, the parameter reaction yield was introduced to identify the amount of ligand-attached anchors among total anchors, since the conjugation efficiency is not always the same nor 100%. Combining these independent parameters, we derived: incorporation ratio=surface anchor density×reaction yield. The term incorporation ratio defines the surface ligand density. Since the surface anchor density represents the density of polyethylene glycol (PEG) on the surfaces in most cases, it also determines liposomal function. It is possible to accurately characterize various PEG and ligand densities and to define the surface topologies. In conclusion, this quantitative methodology can standardize the liposome preparation process and qualify the modified liposomal surfaces.
journal_name
Biol Pharm Bulljournal_title
Biological & pharmaceutical bulletinauthors
Lee SH,Sato Y,Hyodo M,Harashima Hdoi
10.1248/bpb.b16-00462subject
Has Abstractpub_date
2016-01-01 00:00:00pages
1983-1994issue
12eissn
0918-6158issn
1347-5215journal_volume
39pub_type
杂志文章abstract：:To search for possible anti-tumor-promoters, we carried out a primary screening of 21 cucurbitane triterpenoids using an in vitro assay system. Of these triterpenoids, scandenoside R6 (6), 23,24-dihydrocucurbitacin F (14), 25-acetyl-23,24-dihydrocucurbitacin F (15), 2-O-beta-D-glucopyranosyl-23,24-dihydrocucurbitacin ...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.17.668
更新日期：1994-05-01 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 role of leukotriene B4 (LTB4) in leukocyte infiltration in zymosan-induced rat pleurisy was investigated by studying the effects of 5-lipoxygenase inhibitors, T-0757 and AA-861, and a cyclooxygenase inhibitor, indomethacin, on leukocyte infiltration and LTB4 levels in the inflammatory exudate of rat pleurisy induc...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.18.1302
更新日期：1995-09-01 00:00:00
abstract：:The effects of gamma-oryzanol, a drug mainly used for the treatment of hyperlipidaemia, on several cytochrome P450 (CYP) specific reactions in human liver microsomes were investigated to predict drug interactions with gamma-oryzanol in vivo from in vitro data. The following eight CYP catalytic reactions were used in t...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.27.1151
更新日期：2004-07-01 00:00:00
abstract：:The effect of the Dynorphin A analog, E2078, on the physicochemical properties of lipid membranes was investigated. E2078 induces the leakage of calcein, especially out of negatively-charged vesicles. The peptide binds to dipalmitoylphosphatidylglycerol sonicated vesicles according to the Lamgmuir isotherm, with a bin...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.22.543
更新日期：1999-05-01 00:00:00
abstract：:There exist limitations in the detection of exogenous oligosaccharides due to their polydisperse and diversiform nature, and particularly the interference of endogenous glycosaminoglycans (GAGs). Herein, a surface plasmon resonance (SPR) assay for detecting acidic oligosaccharide sugar chain (AOSC), an anti-Alzheimer'...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.29.60
更新日期：2006-01-01 00:00:00
abstract：:The total iron-binding capacity (TIBC) and iron contents of diabetic rat serum, as well as the iron-binding capacity of glycated transferrin and oxygen radical production by the glycated proteins were examined. The TIBC and iron content of diabetic rat sera were found to be much lower than those of control rat sera. I...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.18.396
更新日期：1995-03-01 00:00:00
abstract：:Cytochrome P450 monooxygenases (P450s) catalyze a wide variety of monooxygenation reactions in primary and secondary metabolism in plants. The share of P450 genes in each plant genome is estimated to be up to 1%. This implies that the diversification of P450 has made a significant contribution to the ability to acquir...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章,评审
doi：10.1248/bpb.35.824
更新日期：2012-01-01 00:00:00
abstract：:The aim of this study was to determine the stimulatory effects of Maillard reaction, a non-enzymatic browning reaction on the expression of pro-inflammatory cytokines and phagocytic activity induced by whey protein concentrate (WPC). Glycated WPC (G-WPC) was prepared by a reaction between WPC and the lactose it contai...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.b15-00596
更新日期：2016-01-01 00:00:00
abstract：:The number of patients with colitis has been increasing year by year. Recently, intestinal inflammation, as one of the factors for its onset, has been demonstrated to be induced by P2X7 receptor-mediated activation of colonic immune cells such as mast cells. Activation of P2X7 receptor (P2X7R) is known to be inhibited...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.b17-00143
更新日期：2017-01-01 00:00:00
abstract：:We investigated whether peripherally administered aconitine increases spontaneous acetylcholine (ACh) release from the frontal cerebral cortex in freely moving rats using in vivo microdialysis, as it relates to aconitine-induced bradycardia estimated by a tail-artery cuff technique in unilateral anterior hypothalamus ...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.19.1440
更新日期：1996-11-01 00:00:00
abstract：:We previously reported the isolation of a novel cerebroside (1-O-(beta-D-glucopyranosyl)-(2S,3R,4E,8Z)-2-N-palmityloc tadecasphinga-4,8-diene; LCC) from the fruits of Lycium chinense MILL. (Solanaceae) which protected primary cultured rat hepatocytes from the toxicity induced by carbon tetrachloride (CCl4). The presen...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.22.873
更新日期：1999-08-01 00:00:00
abstract：:The purpose of this study was to evaluate the essential oils from sweet basil (Ocimum basilicum, OB) as skin permeation enhancers to promote the percutaneous absorption of drugs. The in vitro and in vivo irritancy of the essential oils was also examined. Terpenes with various carbon numbers (mono-, sesqui-, di-, and t...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.27.1819
更新日期：2004-11-01 00:00:00
abstract：:We aimed to identify a novel flavonoid from the in-house natural products to suppress matrix metalloproteases (MMPs), which is responsible for degradation of collagen and other extracellular matrix proteins. Total eight natural products were screened for identification of a novel MMP-9 suppressor using MMP-9 reporter ...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.b13-00534
更新日期：2014-01-01 00:00:00
abstract：:The tissue distribution and disposition of carnitine, which plays an important role in the transport of long-chain fatty acids across the mitochondrial inner membrane for beta-oxidation, are well controlled by carnitine transporter organic cation/carnitine transporter 2 (OCTN2). Since little information is available o...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.31.1230
更新日期：2008-06-01 00:00:00
abstract：:A homology-based cloning strategy yielded Sdga, a cDNA clone presumably encoding alpha-subunit of heterotrimeric guanosine 5'-triphosphate-binding protein complex, from leaf tissues of Scoparia dulcis. Phylogenetic tree analysis of G-protein alpha-subunits from various biological sources suggested that, unlike in anim...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.31.2150
更新日期：2008-11-01 00:00:00
abstract：:A rat model of early sepsis induced by lipopolysaccharide (LPS) combined with interleukin-2 (IL-2) was developed. The primary aim was to assess the pharmacokinetics of gentamicin and sepsis-induced pathophysiological changes. Moreover, the effects on the glomerular filtration rate and tubular function were studied in ...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.b12-00205
更新日期：2012-01-01 00:00:00
abstract：:The antiemetic effect of a potent and selective neurokinin-1 (NK1) receptor antagonist, FK886 ([3,5-bis(trifluoromethyl)phenyl][(2R)-2-(3-hydroxy-4-methylbenzyl)-4-{2-[(2S)-2-(methoxymethyl)morpholin-4-yl]ethyl}piperazin-1-yl]methanone dihydrochloride), on cisplatin-induced acute and delayed emesis in ferrets was stud...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.b13-00521
更新日期：2014-01-01 00:00:00
abstract：:Silymarin is a polyphenolic flavonoid from milk thistle (Silybum marianum), which has anti-inflammatory, cytoprotective, and anticarcinogenic effects. In this study, we assessed the effect of silibinin (Fig. 1), the major active compound in silymarin, on ultraviolet light (UV)-induced cell apoptosis in HaCaT cells, a ...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.29.1096
更新日期：2006-06-01 00:00:00
abstract：:This study examined the osteoblast-like MC3T3-E1 cell responses to poly(DL-lactide) (PDLLA) and poly(L-lactide) (PLLA) with different weight average molecular weight (M.W.). Colony formation of MC3T3-E1 cells on the PLLA with M.W. 270000 or 1370000 was slightly lower than that on glass. The protein, DNA and hydroxypro...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.23.1470
更新日期：2000-12-01 00:00:00
abstract：:An accumulating body of evidence indicates that inflammation plays a crucial role in the pathophysiology of myocardial infarction (MI). Nucleotide-binding oligomerization domain-like receptor (NLR) family pyrin domain containing 3 (NLRP3) inflammasome is an intracellular multiprotein complex that regulates caspase-1 a...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章,评审
doi：10.1248/bpb.b18-00369
更新日期：2019-01-01 00:00:00
abstract：:The pharmacological profiles of antigen-induced immediate airway response (IAR) in rats are not fully understood. In this study, we established an ovalbumin (OVA)-induced IAR model using noninvasive measurement in rats, and evaluated the effects of commonly used and effective antiasthmatic drugs, i.e. ketotifen (antih...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.31.2260
更新日期：2008-12-01 00:00:00
abstract：:To develop a piroxicam-loaded gelatin microcapsule with enhanced bioavailability, a gelatin microcapsule encapsulated ethanol and piroxicam has been formulated by using gelatin as a water-soluble polymer shell. The aqueous solubility and bioavailability of piroxicam in piroxicam-loaded microcapsule in rats were then e...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.31.1284
更新日期：2008-06-01 00:00:00
abstract：:Stevens-Johnson syndrome (SJS) was diagnosed in a 39-year-old woman, treated with ampicillin (4000-8000 mg daily), phenytoin (250 mg daily), and furosemide (20-40 mg daily) for 25, 21, and 20 d, respectively, before the appearance of the eruption. The lymphocyte stimulation test with the MTT [3-(4,5-dimethyl thiazol-2...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.27.929
更新日期：2004-06-01 00:00:00
abstract：:Berberine is one of the main alkaloids of Rhizoma coptidis which has been used as a folk medicine to treat diabetes mellitus for more than 1400 years in China. To investigate the chronic effect of berberine on diabetic hyperlipidemic rats, fasted rats were intraperitoneally injected 35 mg/kg streptozotocin. Diabetic r...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.31.1169
更新日期：2008-06-01 00:00:00
abstract：:The total alkaloid fractions of the methanolic extracts of the leaves, ripe fruits, roots, seeds and stem of Solanum pseudocapsicum were subjected to in-vitro cytotoxicity, short-term toxicity and long-term survival studies. All the five fractions exhibited potent activity. The total alkaloid fraction of leaves was fo...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.27.528
更新日期：2004-04-01 00:00:00
abstract：:The purpose of this study was to evaluate the accuracy of the recommended theophylline therapeutic range in the treatment of acute airway obstruction. Twenty seven patients (20 to 64 years) with acute asthma attack were given aminophylline intravenously to obtain a theophylline concentration between 10 and 20 microgra...
journal_title：Biological & pharmaceutical bulletin
pub_type： 临床试验,杂志文章
doi：10.1248/bpb.19.710
更新日期：1996-05-01 00:00:00
abstract：:Diosgenyl saponins are the most abundant steroid saponins, and exert a large variety of biological functions. In a previous report, we showed that dioscin was able to induce cytotoxicity and apoptosis in human myeloblast leukemia HL-60 cells. This study further investigated the action mechanisms underlying this effect...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.27.1059
更新日期：2004-07-01 00:00:00
abstract：:The extracellular matrix (ECM), which contributes to structural homeostasis as well as to the regulation of cellular function, is enzymatically cleaved by proteases, such as matrix metalloproteinases and cathepsins, in the normal and diseased heart. During the past two decades, matricryptins have been defined as fragm...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章,评审
doi：10.1248/bpb.b17-00308
更新日期：2017-01-01 00:00:00
abstract：:Escherichia coli BM2506 produced macrolide 2'-phosphotransferase II [MPH (2') II]. A gene for MPH (2') II, designated mphB, is located on plasmids pTZ3721 and pTZ3723 in E. coli BM2506. In the present study, we determined the nucleotide sequence of the 6.5-kb EcoRI-PstI fragment containing mphB on pTZ3721. The DNA reg...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.22.227
更新日期：1999-02-01 00:00:00
