Abstract:
:Folic acid-conjugated albumin nanospheres (FA-AN) have been developed to provide an actively targetable drug delivery system for improved drug targeting of cancer cells with reduced side effects. The nanospheres were prepared by conjugating folic acid onto the surface of albumin nanospheres using 1-ethyl-3-(3-dimethylaminopropyl) carbodiimide (EDAC) as a catalyst. To test the efficacy of these nanospheres as a potential delivery platform, doxorubicin-loaded albumin nanospheres (DOX-AN) and doxorubicin-loaded FA-AN (FA-DOX-AN) were prepared by entrapping DOX (an anthracycline, antibiotic drug widely used in cancer chemotherapy that works by intercalating DNA) into AN and FA-AN nanoparticles. Cell uptake of the DOX was then measured. The results show that FA-AN was incorporated into HeLa cells (tumor cells) only after 2.0h incubation, whereas HeLa cells failed to incorporate albumin nanospheres without conjugated folic acid after 4.0h incubation. When HeLa cells were treated with the DOX-AN, FA-DOX-AN nanoparticles or free DOX, cell viability decreased with increasing culture time (i.e. cell death increases with time) over a 70h period. Cell viability was always the lowest for free DOX followed by FA-DOX-AN4 and then DOX-AN. In a second set of experiments, HeLa cells washed to remove excess DOX after an initial incubation for 2h were incubated for 70h. The corresponding cell viability was slightly higher when the cells were treated with FA-DOX-AN or free DOX whilst cells treated with DOX-AN nanoparticles remained viable. The above experiments were repeated for non-cancerous, aortic smooth muscle cells (AoSMC). As expected, cell viability of the HeLa cells (with FA receptor alpha, FRα) and AoSMC cells (without FRα) decreased rapidly with time in the presence of free DOX, but treatment with FA-DOX-AN resulted in selective killing of the tumor cells. These results indicated that FA-AN may be used as a promising actively targetable drug delivery system to improve drug targeting to cancer cells.
journal_name
Pharmacol Resjournal_title
Pharmacological researchauthors
Shen Z,Li Y,Kohama K,Oneill B,Bi Jdoi
10.1016/j.phrs.2010.10.012subject
Has Abstractpub_date
2011-01-01 00:00:00pages
51-8issue
1eissn
1043-6618issn
1096-1186pii
S1043-6618(10)00204-5journal_volume
63pub_type
杂志文章abstract::The altered vascular responses to various vasopressors and relaxants have been well reported in various animal models of hypertension, insulin resistance and diabetes. Though the role of oxidative stress (increased superoxide levels) associated with these altered vascular responses in hyperglycemic/diabetic state is w...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2005.11.002
更新日期:2006-03-01 00:00:00
abstract::The effects of the P(2)-purinoceptor antagonist pyridoxal-phosphate-6-azophenyl- 2('),4(')- disulphonic acid (PPADS), the nitric oxide (NO) synthase inhibitor N(G)-nitro- l -arginine (l -NOARG), the K(+)-channel blocker apamin, the pituitary adenylate cyclase activating peptide (PACAP) antagonist PACAP(6-38) and the s...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1006/phrs.2000.0742
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更新日期:2020-11-01 00:00:00
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journal_title:Pharmacological research
pub_type: 杂志文章
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更新日期:2013-12-01 00:00:00
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更新日期:2020-08-01 00:00:00
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journal_title:Pharmacological research
pub_type: 杂志文章,评审
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更新日期:1998-11-01 00:00:00
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journal_title:Pharmacological research
pub_type: 杂志文章,评审
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更新日期:1995-02-01 00:00:00
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journal_title:Pharmacological research
pub_type: 杂志文章
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更新日期:2002-07-01 00:00:00
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pub_type: 杂志文章
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更新日期:2020-09-01 00:00:00
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journal_title:Pharmacological research
pub_type: 杂志文章,评审
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更新日期:2017-10-01 00:00:00
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journal_title:Pharmacological research
pub_type: 杂志文章,评审
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更新日期:2018-10-01 00:00:00
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journal_title:Pharmacological research
pub_type: 杂志文章,评审
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更新日期:2016-12-01 00:00:00
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journal_title:Pharmacological research
pub_type: 杂志文章,评审
doi:10.1016/j.phrs.2015.08.008
更新日期:2015-10-01 00:00:00
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journal_title:Pharmacological research
pub_type: 杂志文章,评审
doi:10.1016/j.phrs.2020.105311
更新日期:2021-01-01 00:00:00
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journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2011.04.006
更新日期:2011-09-01 00:00:00
abstract::A traditional Chinese medicine (TCM) formula (SL) comprising Sophorae Flos and Lonicerae Japonicae Flos was used for treating melanoma in ancient China. We have previously shown that an ethanolic extract of SL (SLE) possesses anti-melanoma effects and suppresses STAT3 signaling in vitro and in vivo. STAT3 has been lin...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2019.02.020
更新日期:2019-04-01 00:00:00
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journal_title:Pharmacological research
pub_type: 杂志文章
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journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2016.07.018
更新日期:2016-09-01 00:00:00
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journal_title:Pharmacological research
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journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1006/phrs.1997.0200
更新日期:1997-08-01 00:00:00
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journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1006/phrs.2000.0730
更新日期:2000-11-01 00:00:00
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journal_title:Pharmacological research
pub_type: 杂志文章,随机对照试验
doi:10.1016/j.phrs.2016.08.010
更新日期:2016-09-01 00:00:00
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journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2018.02.012
更新日期:2018-05-01 00:00:00
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journal_title:Pharmacological research
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.1006/phrs.1997.0144
更新日期:1997-04-01 00:00:00
abstract::The insulinotropic action of several new esters of succinic acid was assessed in isolated rat islets incubated in the presence of 7 mM D-glucose. An efficient secretory response was observed with the monobenzyl, monoisopropyl, monoallyl, monopropyl, monoethyl, monobutyl, dibutyl, dipropyl and diallyl esters of succini...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1006/phrs.1996.0038
更新日期:1996-04-01 00:00:00
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journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2011.10.001
更新日期:2012-03-01 00:00:00
abstract::The uridin-diphosphoglucuronyl-transferase (UDP-GT) is a membrane-bound enzyme responsible for glucuronidation of endogenous and exogenous compounds. This work established the UDP-GT activity and its lipid membrane microenvironment in two experimental models: acute paracetamol intoxication, and cholestasis followed by...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1006/phrs.1999.0530
更新日期:1999-10-01 00:00:00
abstract::Coronavirus Disease 2019 (COVID-19) caused by the emerging severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) is associated with a crude case fatality rate of about 0.5-10 % depending on locality. A few clinically approved drugs, such as remdesivir, chloroquine, hydroxychloroquine, nafamostat, camostat, and ...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2020.104960
更新日期:2020-09-01 00:00:00
abstract::The modification in the composition of bile acids in hamster by the administration of high dose of ursodeoxycholic acid (UDCA) was investigated. Male Golden Syrian hamsters were divided into five groups: a control group, two groups that received 0.5 g of UDCA per 100 g of standard diet during 30 and 60 days and anothe...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/1043-6618(90)90727-u
更新日期:1990-05-01 00:00:00
abstract::The understanding of signaling cascades involved in the induction, promotion, and progression of cancer, although advanced in recent years, is still incomplete. Tracing the imbalance of the impaired, physiologically-essential cellular signaling that drives the neoplastic process is a complex issue. This review discuss...
journal_title:Pharmacological research
pub_type: 杂志文章,评审
doi:10.1016/j.phrs.2012.03.014
更新日期:2012-07-01 00:00:00