Abstract:
BACKGROUND:Drug design and discovery studies still remain of great importance in the search for more convenient chemotherapeutic to avoid the drug resistance, systemic toxicity or the longterm side effects. OBJECTIVE:A series of mononuclear gold (III) and platinum (II) complexes based on 4-dihydroxyboryl- DL-phenylalanine (BPA) was designed and synthesized, for the first time, by using 2, 2'-dipyridyl (L1) and 4, 4'-diaminobibenzyl (L2) ligands. Characterization of the synthesized complexes was achieved by using 1H-NMR, IR, MS and elemental analyses. METHOD:MTT cell viability, endothelial tube formation, cancer cell colony formation and TRITCphalloidin cytoskeleton staining assays were performed on human umbilical vein endothelial (HUVEC) and human lung adenocarcinoma (A549) cells to establish the anticancer and anti-angiogenic activities of the complexes. It was determined that the organometallic complexes that include 2, 2'-dipyridyl ligand have higher antiproliferative activity than L2-based complexes in the micromolar range. Colony formation experiments showed that the anchorage-independent growth ability of A549s was significantly affected by the complexes in a concentration-dependent manner though L1-based complexes were more effective than L2-based ones. RESULTS:It was also clearly observed that the complexes have significant anti-angiogenic and cytoskeleton alterative activities. Consequently, the phenylalanine-based organometallic complexes seem to have anti-lung cancer and anti-angiogenic activities depending on the ligand type and a great potential in oncology drug development because phenylalanine amino acid has an ability to cross the cell membrane by using L-amino acid transport system. CONCLUSION:Design, synthesis and activity studies with amino acid analogs should be therefore increased to discover more efficient drugs to cure cancer diseases.
journal_name
Curr Drug Delivjournal_title
Current drug deliveryauthors
Varol M,Koparal AT,Benkli K,Bostancioglu RBdoi
10.2174/1567201815666180727145724subject
Has Abstractpub_date
2018-01-01 00:00:00pages
1417-1425issue
10eissn
1567-2018issn
1875-5704pii
CDD-EPUB-91996journal_volume
15pub_type
杂志文章abstract:OBJECTIVE:The label free ultrasmall fluorescent ferrite clusters have been engineered in a controlled fashion which was stabilized by serum protein and functionalized by folic acid for the application of targeted multimodal optical and Magnetic Resonance (MR) cancer imaging. METHODS:The ultra-small manganese ferrite n...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/1567201816666181119112410
更新日期:2019-01-01 00:00:00
abstract:BACKGROUND:Hesperetin (HSP) is a low water-soluble flavanone aglycone with low bioavailability. OBJECTIVES:This study aimed at enhancing the hepatoprotective effects of HSP by a combinatory technique based on solid dispersions of co-crystals of HSP. METHODS:Co-crystals were prepared using citric acid, tartaric acid, ...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/1567201815666180730141556
更新日期:2018-01-01 00:00:00
abstract:BACKGROUND:The present work aimed to develop an ethosomal gel of naproxen sodium for the amelioration of rheumatoid arthritis. OBJECTIVE:In the present work, we have explored the potential of ethosomes to deliver naproxen into deeper skin strata. Further, the anti-inflammatory efficacy of naproxen ethosomal formulatio...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/1567201817666200724170203
更新日期:2020-01-01 00:00:00
abstract::The research presented in this paper discusses the potential of iontophoresis facilitated transdermal delivery of glycine. Iontophoresis has been widely investigated as a noninvasive transdermal drug delivery system. Iontophoresis is the use of a low electric current to carry ionized as well as unionized drug molecule...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/156720109787846207
更新日期:2009-04-01 00:00:00
abstract:BACKGROUND:PnPP-19 is a 19-amino-acid synthetic peptide previously described as a novel drug for the treatment of erectile dysfunction. OBJECTIVE:The aim of this work was to evaluate the physicochemical properties of cationic transfersomes containing PnPP-19 and the skin permeation of free PnPP-19 and PnPP-19-loaded t...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/1567201815666180108170206
更新日期:2018-01-01 00:00:00
abstract::The mucosal administration of vaccines is an area currently receiving a high level of interest due to potential advantages offered by this technique. These advantages include the ability to administer vaccines without need for needles, thus improving patient compliance with vaccination schedules, and the capacity to i...
journal_title:Current drug delivery
pub_type: 杂志文章,评审
doi:10.2174/1567201043334588
更新日期:2004-10-01 00:00:00
abstract::The aim of the present study was to prepare and evaluate hydrogels containing 0.1% isosorbide mononitrate (ISMN) for topical treatment of anal fissure. The hydrogels were prepared on the base of Carbopol 940, Poloxamer 407 or their combination. The highest viscosity and significant thyxotropy were observed for the com...
journal_title:Current drug delivery
pub_type: 杂志文章,随机对照试验
doi:10.2174/156720112802650635
更新日期:2012-09-01 00:00:00
abstract::Paclitaxel (taxol, 1a) and docetaxel (taxotere, 1b) have established themselves as an important class of antitumor drugs currently available to the oncologist. While the great contribution of these drugs to the management of the disease and their effect on the improvement of the patient quality of life could not be ov...
journal_title:Current drug delivery
pub_type: 杂志文章,评审
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更新日期:2008-01-01 00:00:00
abstract:OBJECTIVE:A new tumor targeted polymer-coated gold/graphene hybrid has been developed for achieving simultaneously thermoablation and chemoterapy of folate receptor-positive cancer cells. METHODS:The gold/graphene hybrid was prepared by depositing gold nanospheres onto graphene oxide and coating it with an inulin-fola...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/1567201813666160520113804
更新日期:2017-01-01 00:00:00
abstract::The objective of this investigation was to prepare mucoadhesive microspheres of ketorolac for nasal delivery to avoid gastrointestinal side effects of conventional dosage form. Mucoadhesive microspheres were prepared using carbopol, polycarbophil and chitosan as polymer by spray drying method. The process and formulat...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/156720112800234503
更新日期:2012-03-01 00:00:00
abstract::The stratum corneum (SC) is a primary rate limiting barrier to permeation of drug molecules through the skin. Small molecular weight lipophilic drugs that are effective at low doses can be effectively delivered by passive transdermal delivery. The SC does not permit passage of polar/hydrophilic and macromolecules. Pas...
journal_title:Current drug delivery
pub_type: 杂志文章,评审
doi:10.2174/156720110791011765
更新日期:2010-04-01 00:00:00
abstract::Curcumin as an antioxidative agent which has been widely used medicinally in India and China. However, rapid metabolism coupled with the instability of curcumin under physiological conditions has greatly limited its applications in vivo. In the present study, a thermosensitive hydrogel with high payload of curcumin wa...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/1567201813666151109102532
更新日期:2016-01-01 00:00:00
abstract:BACKGROUND:The purpose of this study was to investigate Quality by Design (QbD) principle for the preparation of hydrogel products to prove both practicability and utility of executing QbD concept to hydrogel based controlled release systems. Product and process understanding will help in decreasing the variability of ...
journal_title:Current drug delivery
pub_type: 杂志文章,评审
doi:10.2174/1567201812666150817122506
更新日期:2016-01-01 00:00:00
abstract::Percutaneous coronary intervention (PCI) has become a highly effective alternative for the treatment of coronary artery disease. The use of stents has reduced the rates of restenosis by preventing elastic recoil and negative remodeling, however neointima formation still remains an issue. Local drug delivery is an attr...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/156720111796642282
更新日期:2011-09-01 00:00:00
abstract:BACKGROUND:Gemcitabine (GEM) is found effective in the treatment of many solid tumors. However, its use is restricted due to its small circulation half-life, fast metabolism and low capacity for selective tumor uptake. Folate receptors (FRs) have been recognized as cellular surface markers, which can be used for cancer...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/1567201815666181024112252
更新日期:2019-01-01 00:00:00
abstract::In this study we developed and evaluated a prototype of an effective occlusive mucoadhesive system for prophylaxis and/or treatment of oral mucositis based on chitosan and gelatine models together with nystatin as a prophylactic agent incorporated into the formulation and investigated drug release in-vitro. Results of...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/1567201811310010020
更新日期:2013-02-01 00:00:00
abstract::The objective of this investigation was aimed to explore the cancer targeting potential of folate conjugated dendrimer (polypropylene imine, PPI) under strategic influence of folate receptor up-regulators (all trans Retinoic acid, ATRA and Dexamethasone, DEXA). The folate conjugated dendrimer nanoconjugate (FPPI) was ...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/1567201811310040012
更新日期:2013-08-01 00:00:00
abstract::Camptothecins are a family of alkaloids originally extracted from the Chinese tree Camptotheca acuminata, Nyssaceae, exhibiting a strong activity against colorectal cancer (CRC). CRC is a common malignancy worlwide. Despite significant developments in the treatment of this disease, it still causes considerable morbidi...
journal_title:Current drug delivery
pub_type: 杂志文章,评审
doi:10.2174/156720112800234558
更新日期:2012-03-01 00:00:00
abstract:BACKGROUND:Subarachnoid hemorrhage (SAH) is considered as a violent disease with high rate of morbidity and mortality. Early brain injury (EBI) and delayed vasospasm are the two aspects of this disease that are becoming research hotspots. OBJECTIVE:We aim to update the role of oxidative stress in the development of EB...
journal_title:Current drug delivery
pub_type: 杂志文章,评审
doi:10.2174/1567201813666161025115531
更新日期:2017-09-06 00:00:00
abstract::Conventional dosage forms such as tablets, capsules and syrups are prescribed in the normal course of practice. However, concerns about patient preferences and market demands have given rise to the exploration of novel unconventional dosage forms. Among these, confectionery-based dose forms have strong potential to ov...
journal_title:Current drug delivery
pub_type: 杂志文章,评审
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更新日期:2015-01-01 00:00:00
abstract::The objective of the present study was to fabricate and evaluate a multiparticulate oral gastroretentive dosage form of baclofen characterized by a central large cavity (hollow core) promoting unmitigated floatation with practical applications to alleviate the signs and symptoms of spasticity and muscular rigidity. So...
journal_title:Current drug delivery
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doi:10.2174/1567201811666140414113838
更新日期:2014-01-01 00:00:00
abstract:BACKGROUND:The aim of this research was to engineer solid dispersion lipid particles (SDSLs) in which a solid dispersion (SD) was encapsulated to form the core of solid lipid particles (SLs), thereby achieving an efficient enhancement in the dissolution of a poorly water-soluble drug. METHODS:Ultrasonication was intro...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/1567201814666170606101138
更新日期:2018-01-01 00:00:00
abstract::Fast-dissolving drug delivery systems have been developed as an alternative to conventional dosage form as an oral means of drug delivery in case of chronic conditions. Now a day's fast dissolving films are preferred over conventional tablets and capsules for masking the taste of bitter drugs to increase the patient c...
journal_title:Current drug delivery
pub_type: 杂志文章,评审
doi:10.2174/156720111795768022
更新日期:2011-07-01 00:00:00
abstract:BACKGROUND:The scope of nanotechnology has been extended to almost every sphere of our daily life. As a result of this, nanocarriers like Carbon Nanotubes (CNTs) are gaining considerable attention for their use in various therapeutic and diagnostic applications. OBJECTIVE:The objective of the current article is to rev...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/1567201817999200508092821
更新日期:2020-01-01 00:00:00
abstract:OBJECTIVES:In this study, central composite factorial design was used for the preparation and optimization of chitosan/Na-alginate hydrogel films containing metformin via solvent evaporation technique. METHODS:Low and high molecular weight (MW) chitosan was used as a polymer in different concentrations while genipin w...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/1567201815666180409102459
更新日期:2018-01-01 00:00:00
abstract::Gene therapy has the potential to treat both acquired and inherited genetic diseases. Generally, two types of gene delivery vectors are used - viral vectors and non-viral vectors. Non-viral gene delivery systems have attracted significant interest (e.g. 115 gene therapies approved for clinical trials in 2018; clinical...
journal_title:Current drug delivery
pub_type: 杂志文章,评审
doi:10.2174/1567201816666190529072914
更新日期:2019-01-01 00:00:00
abstract::The gastroretentive drug delivery system is site-specific and allows the drug to remain in the stomach for a prolonged period of time so that it can be released in a controlled manner in gastrointestinal tract. The present study was carried out to develop a gastroretentive drug delivery system using isabgol as an exci...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/15672018113106660065
更新日期:2014-01-01 00:00:00
abstract::Nowadays, cancer is one of the deadliest diseases affecting an annually enormous number of people. Around 9.6 million people had died from different cancer types in 2018. Chemotherapy is considered to be a mainline treatment, and systemic administration of a single anticancer agent is also considered as vital clinical...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/1567201818999210120203904
更新日期:2021-01-20 00:00:00
abstract:BACKGROUND:The management of TB is difficult due to the resistance developed by Mycobacterium tuberculosis against anti-tubercular drugs causes the new challenges for treating and managing the disease. OBJECTIVE:The objective of the study was to combat multiple drug resistance (MDR) exhibited by mycobacterium species ...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/1567201813666160502124811
更新日期:2016-01-01 00:00:00
abstract::Biphenyl Dimethyl Dicarboxylate (BDD) is insoluble in aqueous solution and the bioavailability after oral administration is low. Self-nanoemulsifying drug delivery system (SNEDDS) containing BDD has been successfully prepared using carefully selected ingredients which are less affected by pH and ionic strength changes...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/156720108784911695
更新日期:2008-07-01 00:00:00