A new generation of star polymer: magnetic aromatic polyamides with unique microscopic flower morphology and in vitro hyperthermia of cancer therapy

Drugs targeting heat shock protein 90 (Hsp90) have been extensively explored for their anticancer potential in advanced clinical trials. Nanoformulations have been an important drug delivery platform for the anticancer molecules like Hsp90 inhibitors. It has been reported that bovine serum albumin (BSA) nanoparticles (NPs) serve as carriers for anticancer drugs, which have been extensively explored for their therapeutic efficacy against cancers. Luminespib (also known as NVP-AUY922) is a new generation Hsp90 inhibitor that was introduced recently. It is one of the most studied Hsp90 inhibitors for a variety of cancers in Phase I and II clinical trials and is similar to its predecessors such as the ansamycin class of molecules. To our knowledge, nanoformulations for luminespib remain unexplored for their anticancer potential. In the present study, we developed aqueous dispensable BSA NPs for controlled delivery of luminespib. The luminespib-loaded BSA NPs were characterized by SEM, TEM, FTIR, XPS, UV-visible spectroscopy and fluorescence spectroscopy. The results suggest that luminespib interacts by non-covalent reversible interactions with BSA to form drug-loaded BSA NPs (DNPs). Our in vitro evaluations suggest that DNP-based aqueous nanoformulations can be used in both pancreatic (MIA PaCa-2) and breast (MCF-7) cancer therapy.

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Investigation of Star Polymer Nanoshells for Use in Diagnostic Imaging and Photothermal Cancer Therapy Applications

10.31979/etd.2smx-jmu5 ◽

2012 ◽

Author(s):

Lizabeth Gomez

Keyword(s):

Cancer Therapy ◽

Diagnostic Imaging ◽

Star Polymer

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Flavonoids as P-gp Inhibitors: A Systematic Review of SARs

Current Medicinal Chemistry ◽

10.2174/0929867325666181001115225 ◽

2019 ◽

Vol 26 (25) ◽

pp. 4799-4831 ◽

Cited By ~ 4

Author(s):

Jiahua Cui ◽

Xiaoyang Liu ◽

Larry M.C. Chow

Keyword(s):

Molecular Mechanisms ◽

Metastatic Cancer ◽

Drug Candidates ◽

Chemical Structures ◽

Transporter Family ◽

Promising Area ◽

New Generation ◽

Nontoxic Inhibitors

P-glycoprotein, also known as ABCB1 in the ABC transporter family, confers the simultaneous resistance of metastatic cancer cells towards various anticancer drugs with different targets and diverse chemical structures. The exploration of safe and specific inhibitors of this pump has always been the pursuit of scientists for the past four decades. Naturally occurring flavonoids as benzopyrone derivatives were recognized as a class of nontoxic inhibitors of P-gp. The recent advent of synthetic flavonoid dimer FD18, as a potent P-gp modulator in reversing multidrug resistance both in vitro and in vivo, specifically targeted the pseudodimeric structure of the drug transporter and represented a new generation of inhibitors with high transporter binding affinity and low toxicity. This review concerned the recent updates on the structure-activity relationships of flavonoids as P-gp inhibitors, the molecular mechanisms of their action and their ability to overcome P-gp-mediated MDR in preclinical studies. It had crucial implications on the discovery of new drug candidates that modulated the efflux of ABC transporters and also provided some clues for the future development in this promising area.

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Synthesis and Anti-Tumor Activity Evaluation of Novel 7-Fluoro-4-(1- Piperazinyl) Quinolines

Letters in Drug Design & Discovery ◽

10.2174/1570180815666180820131036 ◽

2019 ◽

Vol 16 (6) ◽

pp. 663-669

Author(s):

Dan Liu ◽

Aiqi Xue ◽

Zhixin Liu ◽

Yi Zhang ◽

Penghui Peng ◽

...

Keyword(s):

Spectral Analysis ◽

Cancer Therapy ◽

Carcinoma Cell ◽

A549 Cells ◽

Quinoline Derivatives ◽

Human Carcinoma ◽

Carcinoma Cell Lines ◽

Human Carcinoma Cell ◽

Anti Tumor Activity

Background: Three series of new 7-fluoro-4-(1-piperazinyl) quinolines (I1~I6, II1~II2 and IV1~IV4) were synthesized. Their anti-tumor activity was evaluated in vitro against three human carcinoma cell lines, namely SGC-7901 cells, BEL-7402 cells and A549 cells expressing high levels of EGFR by Methyl Thiazolyl Terazolium (MTT) assay. Methods: Three series of quinoline derivatives were synthesized, characterized and evaluated for their in vitro anti-tumor activities. Results and Discussion: Structures of the newly synthesized compounds were confirmed by spectral analysis. The preliminary bioassay indicated that compounds I1, I10 and II1 exhibited better anti-tumor activity than the rest of the target compounds and gefitinib against A549 cell based assay, which demonstrated that compounds I1, I10 and II1 are potential agents for cancer therapy. Results suggested that the substitutes on piperazinyl influenced anti-tumor activities remarkably. Conclusion: These results are useful for discovering more potent novel anti-tumor compounds and further studies are ongoing.

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The Role of Herbal Bioactive Components in Mitochondria Function and Cancer Therapy

Evidence-based Complementary and Alternative Medicine ◽

10.1155/2019/3868354 ◽

2019 ◽

Vol 2019 ◽

pp. 1-12 ◽

Cited By ~ 1

Author(s):

Fangfang Tao ◽

Yanrong Zhang ◽

Zhiqian Zhang

Keyword(s):

Cancer Therapy ◽

Cancer Cell ◽

Apoptotic Cell ◽

Redox Status ◽

Cancer Therapies ◽

Bioactive Components ◽

Atp Production

Mitochondria are highly dynamic double-membrane organelles which play a well-recognized role in ATP production, calcium homeostasis, oxidation-reduction (redox) status, apoptotic cell death, and inflammation. Dysfunction of mitochondria has long been observed in a number of human diseases, including cancer. Targeting mitochondria metabolism in tumors as a cancer therapeutic strategy has attracted much attention for researchers in recent years due to the essential role of mitochondria in cancer cell growth, apoptosis, and progression. On the other hand, a series of studies have indicated that traditional medicinal herbs, including traditional Chinese medicines (TCM), exert their potential anticancer effects as an effective adjunct treatment for alleviating the systemic side effects of conventional cancer therapies, for reducing the risk of recurrence and cancer mortality and for improving the quality of patients’ life. An amazing feature of these structurally diverse bioactive components is that majority of them target mitochondria to provoke cancer cell-specific death program. The aim of this review is to summarize the in vitro and in vivo studies about the role of these herbs, especially their bioactive compounds in the modulation of the disturbed mitochondrial function for cancer therapy.

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Doxorubicin-conjugated bacteriophages carrying anti-MHC class I chain-related A for targeted cancer therapy in vitro

OncoTargets and Therapy ◽

10.2147/ott.s69315 ◽

2014 ◽

pp. 2183

Author(s):

Chanvit Leelayuwat ◽

Achara Phumyen ◽

Siriporn Chantasorn ◽

Amonrat Jumnainsong

Keyword(s):

Cancer Therapy ◽

Mhc Class I ◽

Class I ◽

Targeted Cancer Therapy

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Carrier Design: New Generation of Polycationic Branched Polypeptides Containing OH Groups with Prolonged Blood Survival and Diminished in Vitro Cytotoxicity

Bioconjugate Chemistry ◽

10.1021/bc990015q ◽

1999 ◽

Vol 10 (5) ◽

pp. 781-790 ◽

Cited By ~ 23

Author(s):

Ferenc Hudecz ◽

Malcolm V. Pimm ◽

Éva Rajnavölgyi ◽

G´bor Mezo ◽

Angels Fabra ◽

...

Keyword(s):

In Vitro Cytotoxicity ◽

Oh Groups ◽

New Generation

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Cationic Amphiphiles, a New Generation of Antimicrobials Inspired by the Natural Antimicrobial Peptide Scaffold

Antimicrobial Agents and Chemotherapy ◽

10.1128/aac.00530-10 ◽

2010 ◽

Vol 54 (10) ◽

pp. 4049-4058 ◽

Cited By ~ 193

Author(s):

Brandon Findlay ◽

George G. Zhanel ◽

Frank Schweizer

Keyword(s):

Cytoplasmic Membrane ◽

Resistant Bacteria ◽

Clinical Settings ◽

Specific Amino Acid ◽

Cationic Amphiphiles ◽

Naturally Occurring ◽

Pharmacokinetic Properties ◽

To Come ◽

New Generation

ABSTRACT Naturally occurring cationic antimicrobial peptides (AMPs) and their mimics form a diverse class of antibacterial agents currently validated in preclinical and clinical settings for the treatment of infections caused by antimicrobial-resistant bacteria. Numerous studies with linear, cyclic, and diastereomeric AMPs have strongly supported the hypothesis that their physicochemical properties, rather than any specific amino acid sequence, are responsible for their microbiological activities. It is generally believed that the amphiphilic topology is essential for insertion into and disruption of the cytoplasmic membrane. In particular, the ability to rapidly kill bacteria and the relative difficulty with which bacteria develop resistance make AMPs and their mimics attractive targets for drug development. However, the therapeutic use of naturally occurring AMPs is hampered by the high manufacturing costs, poor pharmacokinetic properties, and low bacteriological efficacy in animal models. In order to overcome these problems, a variety of novel and structurally diverse cationic amphiphiles that mimic the amphiphilic topology of AMPs have recently appeared. Many of these compounds exhibit superior pharmacokinetic properties and reduced in vitro toxicity while retaining potent antibacterial activity against resistant and nonresistant bacteria. In summary, cationic amphiphiles promise to provide a new and rich source of diverse antibacterial lead structures in the years to come.

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