26,713 results match your criteria Anti-Cancer Agents in Medicinal Chemistry[Journal]


CpG Island Methylator Phenotype May Predict Poor Overall Survival of Patients with Stage IV Colorectal Cancer.

Oncology 2018 Dec 12:1-8. Epub 2018 Dec 12.

Department of Oncology, National Taiwan University Hospital, Taipei City,

Objective: We aimed to study the prognostic role of CpG island methylator phenotype (CIMP) in patients with different stages of colorectal cancer (CRC).

Material And Methods: We analyzed CIMP in stage I-IV CRC specimens from patients who were diagnosed between 2005 and 2013. CIMP status was determined using a 5-gene MethyLight-based assay. Read More

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December 2018

Chemical Space and Biological Target Network of Anti-inflammatory Natural Products.

J Chem Inf Model 2018 Dec 12. Epub 2018 Dec 12.

Natural products (NPs) are a promising source of anti-inflammatory molecules for the development of drugs. Despite there being an abundance of reports of large numbers of NPs having bioactivity in preliminary cell-based assays of anti-inflammatory potential, their further optimization and exploration is limited by lack of a comprehensive understanding of their effective scaffold structure or biological targets. To facilitate target-based studies of anti-inflammatory NPs, the details of 665 NPs reported to have anti-inflammatory activity were extracted from the literature and compiled into a dataset we termed InflamNat. Read More

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December 2018

Tumor microenvironment remodeling by intratumoral oncolytic vaccinia virus enhances the efficacy of immune checkpoint blockade.

Clin Cancer Res 2018 Dec 11. Epub 2018 Dec 11.

Medical Oncology, CHA Bundang Medical Center

Purpose: Cancer immunotherapy is a potent treatment modality, but its clinical benefit depends on the tumor's immune profile. Here, we employed mJX-594 (JX), a targeted and GM-CSF-armed oncolytic vaccinia virus, as a strategy to remodel the tumor microenvironment (TME) and subsequently increase sensitivity to αPD-1 and/or αCTLA-4 immunotherapy.

Experimental Design: The remodeling of TME was determined using histologic, flow cytometric, and NanoString immune profiling analyses. Read More

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December 2018

Concise Syntheses of Δ12-Prostaglandin J Natural Products via Stereoretentive Metathesis.

J Am Chem Soc 2018 Dec 12. Epub 2018 Dec 12.

Δ12-Prostaglandin J family is recently dis-covered and has potent anti-cancer activity. Concise syntheses of four Δ12-prostaglandin J natural products (7-8 steps in the longest linear sequences) are reported, enabled by convergent stereoretentive cross-metathesis. Exceptional control of alkene geometry was achieved through stereoretention. Read More

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December 2018

BH3-Mimetic Drugs: Blazing the Trail for New Cancer Medicines.

Cancer Cell 2018 Dec;34(6):879-891

The Walter and Eliza Hall Institute of Medical Research, Parkville, VIC 3052, Australia; Department of Medical Biology, The University of Melbourne, Parkville, VIC 3010, Australia. Electronic address:

Defects in apoptotic cell death can promote cancer and impair responses of malignant cells to anti-cancer therapy. Pro-survival BCL-2 proteins prevent apoptosis by keeping the cell death effectors, BAX and BAK, in check. The BH3-only proteins initiate apoptosis by neutralizing the pro-survival BCL-2 proteins. Read More

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December 2018

microRNA-16-5p enhances radiosensitivity through modulating Cyclin D1/E1-pRb-E2F1 pathway in prostate cancer cells.

J Cell Physiol 2018 Dec 10. Epub 2018 Dec 10.

Institute of Modern Physics, Chinese Academy of Sciences, Lanzhou, People's Republic of China.

Prostate cancer (CaP) is the second most common cancer in men worldwide in 2012, and radiation therapy is one of the most common definitive treatment options for localized CaP. However, radioresistance is a major challenge for the current radiotherapy, accumulating evidences suggest microRNAs (miRNAs), as an important regulator in cellular ionizing radiation (IR) responses, are closely correlated with radiosensitivity in many cancers. Here, we identified microRNA-16-5p(miR-16-5p) is significantly upregulated in CaP LNCaP cells following IR and can enhance radiosensitivity through modulating Cyclin D1/E1-pRb-E2F1 pathway. Read More

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December 2018

7-hydroxyfrullanolide, isolated from Sphaeranthus indicus, inhibits colorectal cancer cell growth by p53 dependent and independent mechanism.

Carcinogenesis 2018 Dec 8. Epub 2018 Dec 8.

Biochemistry Division, CSIR-Central Drug Research Institute, Sector-10, Jankipuram Extension, Lucknow, India.

Sphaeranthus indicus Linn. is commonly used in Indian traditional medicine for management of multiple pathological conditions. However, there are limited studies on anti-cancer activity of this plant and its underlying molecular mechanisms. Read More

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December 2018
5.334 Impact Factor

Challenges and Opportunities of Nanotechnology as Delivery Platform for Tocotrienols in Cancer Therapy.

Front Pharmacol 2018 26;9:1358. Epub 2018 Nov 26.

Product Development and Advisory Services Division, Malaysian Palm Oil Board, Bandar Baru Bangi, Malaysia.

Plant-derived phytonutrients have emerged as health enhancers. Tocotrienols from the vitamin E family gained high attention in recent years due to their multi-targeted biological properties, including lipid-lowering, neuroprotection, anti-inflammatory, antioxidant, and anticancer effects. Despite well-defined mechanism of action as an anti-cancer agent, their clinical use is hampered by poor pharmacokinetic profile and low oral bioavailability. Read More

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November 2018

Steroidogenic effects of extract on the levels of steroidogenic enzymes in mouse Leydig cells.

Anim Cells Syst (Seoul) 2018 8;22(6):407-414. Epub 2018 Nov 8.

Department of Urology, Chung-Ang University College of Medicine, Seoul, Republic of Korea.

In this study, we investigated the steroidogenic effect of extract on mouse TM3 Leydig cells, which produce male hormones by increasing the levels of steroidogenic enzymes. Steroidogenic enzymes are involved in the production of testosterone in the testis. To date, the steroidogenic effect of has not been reported. Read More

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November 2018

Glutathione/pH-responsive nanosponges enhance strigolactone delivery to prostate cancer cells.

Oncotarget 2018 Nov 9;9(88):35813-35829. Epub 2018 Nov 9.

Department of Drug Science and Technology, University of Turin, Turin, Italy.

Strigolactones (SLs) are carotenoid-derived plant hormones that exhibit anti-cancer activities. We previously demonstrated that two SL analogues, MEB55 and ST362, inhibit the growth and survival of various cancer cell lines. However, these compounds have low aqueous solubility and stability at physiological pH. Read More

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November 2018
1 Read

Anagrelide for gastrointestinal stromal tumor.

Clin Cancer Res 2018 Dec 7. Epub 2018 Dec 7.

Department of Oncology, Helsinki University Hospital and University of Helsinki

Purpose: Gastrointestinal stromal tumor (GIST) is a common type of soft tissue sarcoma. Imatinib, an inhibitor of KIT, PDFGRA and a few other tyrosine kinases, is highly effective for GIST, but advanced GISTs frequently progress on imatinib and other approved tyrosine kinase inhibitors. We investigated phosphodiesterase 3 (PDE3) as a potential therapeutic target in GIST cell lines and xenograft models. Read More

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December 2018

The direct and indirect inhibition effects of resveratrol against tachyzoites .

Antimicrob Agents Chemother 2018 Dec 10. Epub 2018 Dec 10.

Department of Parasitology, West China School of Basic Medical Sciences and Forensic Medicine, Sichuan University, Chengdu, Sichuan, China

is one of the most widespread obligatory parasitic protozoa which infect nearly all the warm-blooded animals, leading to toxoplasmosis. Current administration of the therapeutic drugs like the combination of pyrimethamine and sulfadiazine shows high rates of toxic side effects and encounters drug resistance in some cases. Resveratrol is a natural plant extracts with multiple functions, such as anti-bacterial, anti-cancer and anti-parasite activities. Read More

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December 2018

Single crystal XRD, DFT investigations and molecular docking study of 2- ((1,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazol-4-yl)amino)naphthalene-1,4-dione as a potential anti- cancer lead molecule.

Comput Biol Chem 2018 Nov 30;78:153-164. Epub 2018 Nov 30.

Department of Chemistry, St. Berchmans College (Autonomous), Changanasserry, Kerala, India.

A derivative of naphthaquinone, 2-((1,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazol-4-yl)amino)naphthalene-1,4-dione (DPDHN) was synthesized from lawsone by ultrasound accelerated technique. The compound was characterized by elemental analysis, IR, UV-vis, NMR and mass spectral studies. Single crystal X-ray diffraction studies revealed that the compound crystallized in monoclinic space group P2/c. Read More

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November 2018

Phytochemicals: Current strategy to sensitize cancer cells to cisplatin.

Biomed Pharmacother 2018 Dec 7;110:518-527. Epub 2018 Dec 7.

Guangdong Provincial Hospital of Chinese Medicine, The Second Clinical College of Guangzhou University of Chinese Medicine, Guangzhou University of Chinese Medicine, Guangzhou, 510120, China. Electronic address:

Cisplatin-based chemotherapeutic regimens are the most frequently used adjuvant treatments for many types of cancer. However, the development of chemoresistance to cisplatin results in treatment failure. Despite the significant developments in understanding the mechanisms of cisplatin resistance, effective strategies to enhance the chemosensitivity of cisplatin are lacking. Read More

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December 2018

Fucoxanthin potentiates anoikis in colon mucosa and prevents carcinogenesis in AOM/DSS model mice.

J Nutr Biochem 2018 Oct 25;64:198-205. Epub 2018 Oct 25.

Epidemiology and Preventions Group, Center for Public Health Sciences, National Cancer Center, 5-1-1 Tsukiji, Chuo-ku, Tokyo 104-0045, Japan.

Fucoxanthin (Fx) and its biotransformed fucoxanthinol (FxOH) present strong anti-cancer effects in vitro and in vivo, however, the underlying mechanisms are not well known. We recently demonstrated that FxOH could induce anoikis-like cells in human colorectal cancer (CRC) cells. Thus, we developed molecular hallmarks for anoikis in vitro, and to confirm induction of such molecular hallmarks in an azoxymethane/ dextran sodium sulfate carcinogenic model by Fx ingestion. Read More

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October 2018

Synthesis of 8-hydroxyquinoline glycoconjugates and preliminary assay of their β1,4-GalT inhibitory and anti-cancer properties.

Bioorg Chem 2018 Nov 24;84:326-338. Epub 2018 Nov 24.

Institute of Chemistry, University of Silesia, Szkolna 9, 40-006 Katowice, Poland.

8-Hydroxyquinoline scaffold is a privileged structure used in designing a new active agents with therapeutic potential. Its connections with the sugar unit is formed to improve the pharmacokinetic properties. The broad spectrum of activity of quinoline derivatives, especially glycoconjugates, is often associated with the ability to chelate metal ions or with the ability to intercalate into DNA. Read More

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November 2018

Glycyrrhetinic acid-conjugated polymeric prodrug micelles co-delivered with doxorubicin as combination therapy treatment for liver cancer.

Colloids Surf B Biointerfaces 2018 Nov 30;175:106-115. Epub 2018 Nov 30.

Department of Pharmaceutics, School of Pharmacy, Ningxia Medical University, No. 1160, Shengli Street, Yinchuan, 750004, China; Key Laboratory of Hui Ethnic Medicine Modernization, Ministry of Education, Ningxia Medical University, Yinchuan, 750004, China. Electronic address:

Significant synergy of doxorubicin (DOX) and glycyrrhizic acid (GA) in inhibiting the proliferation of cancer cells was demonstrated in the human hepatocellular carcinoma cell line, HepG2. A novel polymeric prodrug micellar carrier based on polyethylene glycol-derivatized GA (PEG-Fmoc-GA), was developed for co-delivery of DOX as a combined anti-cancer treatment. The PEG-Fmoc-GA polymeric prodrug micelles achieved a more effective synergistic action on cell proliferation inhibition and apoptosis induction, when co-delivered with DOX, which can be attributed to the dual effect of the cleaved GA and loaded DOX. Read More

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November 2018

A multifunctional drug nanocarrier for efficient anticancer therapy.

J Control Release 2018 Dec 7. Epub 2018 Dec 7.

Department of Pharmacy and Pharmaceutical Technology, Center for Research in Molecular Medicine and Chronic Diseases (CIMUS), Universidade de Santiago de Compostela, Santiago de Compostela, Spain. Electronic address:

So far, the success of anticancer nanomedicines has been moderate due to their lack of adequate targeting properties and/or to their difficulties penetrating tumors. Here we report a multifunctional drug nanocarrier consisting of hyaluronic acid nanocapsules conjugated with the tumor homing peptide tLyp1, which exhibits both, dual targeting properties (to the tumor and to the lymphatics), and enhanced tumor penetration. Data from a 3D co-culture in vitro model showed the capacity of these nanocapsules to interact with the NRP1 receptors over-expressed in cancer cells. Read More

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December 2018

Development of posaconazole-based analogues as hedgehog signaling pathway inhibitors.

Eur J Med Chem 2018 Nov 23;163:320-332. Epub 2018 Nov 23.

Department of Pharmaceutical Sciences, University of Connecticut, 69 N Eagleville Rd, Unit 3092, Storrs, CT, 06269, USA. Electronic address:

Inhibition of the hedgehog (Hh) signaling pathway has been validated as a therapeutic strategy to treat basal cell carcinoma and holds potential for several other forms of human cancer. Itraconazole and posaconazole are clinically useful triazole anti-fungals that are being repurposed as anti-cancer agents based on their ability to inhibit the Hh pathway. We have previously demonstrated that removal of the triazole from itraconazole does not affect its ability to inhibit the Hh pathway while abolishing its primary side effect, potent inhibition of Cyp3A4. Read More

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November 2018

Rational design of 5-((1H-imidazol-1-yl)methyl)quinolin-8-ol derivatives as novel bromodomain-containing protein 4 inhibitors.

Eur J Med Chem 2018 Nov 16;163:281-294. Epub 2018 Nov 16.

Drug Discovery and Design Center, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zuchongzhi Road, Shanghai, 201203, China. Electronic address:

Bromodomain-containing protein 4 (BRD4), an epigenetic reader of acetyl lysine, has emerged as a promising therapeutic target for many diseases including cancer, inflammation and heart failure. Our previous study reported that nitroxoline, an FDA approved antibiotic, showed potential BRD4 inhibitory activity and antiproliferation activity against leukemia cell lines. In this study, we further explored the structure-activity relationship (SAR) around nitroxoline and employed our previously developed machine learning based activity scoring function BRD4LGR for further analysis. Read More

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November 2018
2 Reads

Diadzein ameliorates 5-fluorouracil-induced intestinal mucositis by suppressing oxidative stress and inflammatory mediators in rodents.

Eur J Pharmacol 2018 Dec 7. Epub 2018 Dec 7.

Department of Pharmacy, Faculty of Biological Sciences, Quaid-i-Azam University, Islamabad, 45320, Pakistan. Electronic address:

5-Fluorouracil (5-FU) is one of the most commonly prescribed anti-cancer agent however, its use is associated with several debilitating adverse effects such as intestinal mucositis (IM) and myelosuppression. Oxidative stress and inflammation are major contributors in the development of mucositis. Diadzein is known for its potent anti-inflammatory and anti-oxidative activities from decades. Read More

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December 2018

Antrodia salmonea suppresses invasion and metastasis in triple-negative breast cancer cells by reversing EMT through the NF-κB and Wnt/β-catenin signaling pathway.

Food Chem Toxicol 2018 Dec 7. Epub 2018 Dec 7.

Institute of Nutrition, College of Biopharmaceutical and Food Sciences, China Medical University, Taichung, 40402, Taiwan. Electronic address:

Antrodia salmonea (AS), a fungus that is indigenous to Taiwan has been well known for its anti-cancer properties. We investigated the anti-metastatic and anti-epithelial-mesenchymal transition (EMT) properties of AS in TNBC cells. To determine their EMT and metastasis levels, in vitro wound healing, wound invasion, Western blotting, RT-PCR, luciferase activity and immunofluorescence assays were performed, while the in vivo anti-metastatic efficacy of AS was evaluated in BALB/c-nu mice through bioluminescence imaging, HE staining, and immunohistochemical staining. Read More

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December 2018

The evolution of antiviral nucleoside analogues: A review for chemists and non-chemists. Part II: Complex modifications to the nucleoside scaffold.

Antiviral Res 2018 Dec 7. Epub 2018 Dec 7.

Department of Chemistry & Biochemistry, University of Maryland, Baltimore County, Baltimore, MD, USA. Electronic address:

This is the second of two invited articles reviewing the development of nucleoside analogue antiviral drugs, written for a target audience of virologists and other non-chemists, as well as chemists who may not be familiar with the field. As with the first paper, rather than providing a chronological account, we have chosen to examine particular examples of structural modifications made to nucleoside analogues that have proven fruitful as various antiviral, anticancer, and other therapeutics. The first review covered the more common, and in most cases, single modifications to the sugar and base moieties of the nucleoside scaffold. Read More

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December 2018

A homologous series of apoptosis-inducing N‑acylserinols: Thermotropic phase behavior, interaction with cholesterol and characterization of cationic N‑myristoylserinol-cholesterol-CTAB niosomes.

Biochim Biophys Acta Biomembr 2018 Dec 6. Epub 2018 Dec 6.

School of Chemistry, University of Hyderabad, Hyderabad 500 046, India. Electronic address:

N‑Acylserinols (NASOHs) exhibit anti-cancer activity by elevating ceramide levels, and/or by activating proapoptotic effectors. In the present work we investigated the thermotropic phase behavior and supramolecular organization of a homologous series of NASOHs (number of C-atoms in the acyl chain, n = 8-18), and the interaction of N-myristoylserinol (NMSOH) with cholesterol, and characterized cationic niosomes made up of NMSOH, cholesterol and cetyltrimethylammonium bromide (CTAB). Differential scanning calorimetric studies revealed that NASOHs exhibit a major chain-melting phase transition under both dry and hydrated states. Read More

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December 2018

An emerging role for nanomaterials in increasing immunogenicity of cancer cell death.

Biochim Biophys Acta Rev Cancer 2018 Dec 5. Epub 2018 Dec 5.

Institute of Biology and Biomedicine, National Research Lobachevsky State University of Nizhni Novgorod, Nizhny Novgorod, Russian Federation; Cell Death Investigation and Therapy Laboratory, Department of Human Structure and Repair, Ghent University, Ghent, Belgium,; Cancer Research Institute Ghent, Ghent, Belgium. Electronic address:

In the last decade, it has become clear that anti-cancer therapy is more successful when it can also induce an immunogenic form of cancer cell death (ICD). ICD is an umbrella term covering several cell death modalities, including apoptosis and necroptosis. In general, ICD is characterized by the emission of damage-associated molecular patterns (DAMPs) and/or cytokines/chemokines, leading to the induction of strong anti-tumor immune responses. Read More

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December 2018
1 Read

Synthesis and SAR of novel capsazepine analogs with significant anti-cancer effects in multiple cancer types.

Bioorg Med Chem 2018 Nov 29. Epub 2018 Nov 29.

Department of Comprehensive Dentistry, University of Texas Health Science Center at San Antonio School of Dentistry, San Antonio, Texas 78229, USA; Mays Cancer Center, University of Texas Health Science Center at San Antonio, San Antonio, Texas 78229, USA. Electronic address:

We previously demonstrated that capsazepine (CPZ), a synthetic transient receptor potential Vanilloid subtype 1 (TRPV1) antagonist, has significant anti-cancer effects in vivo. The purpose of this study was to develop more potent analogs based upon CPZ pharmacophore and structure-activity relationships (SAR) across analogs. We generated 30 novel compounds and screened for their anti-proliferative effects in cultured HeLa cervical cancer cells. Read More

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November 2018
1 Read

A new gold(I) complex-Au(PPh)PT is a deubiquitinase inhibitor and inhibits tumor growth.

EBioMedicine 2018 Dec 5. Epub 2018 Dec 5.

Affiliated Cancer Hospital & Institute of Guangzhou Medical University, Guangzhou, Guangdong 510095, China; Protein Modification and Degradation Lab, State Key Lab of Respiratory Disease, Guangzhou Medical University, Guangdong, China. Electronic address:

Background: Ubiquitin-proteasome system (UPS) is integral to cell survival by maintaining protein homeostasis, and its dysfunction has been linked to cancer and several other human diseases. Through counteracting ubiquitination, deubiquitinases (DUBs) can either positively or negatively regulate UPS function, thereby representing attractive targets of cancer therapies. Previous studies have shown that metal complexes can inhibit tumor growth through targeting the UPS; however, novel metal complexes with higher specificity for cancer therapy are still lacking. Read More

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December 2018

Cryoprotectant toxicity in Caenorhabditis elegans.

Cryobiology 2018 Dec 4. Epub 2018 Dec 4.

Institute for Behavioral Genetics, University of Colorado, Boulder, USA; Department of Integrative Physiology, University of Colorado, Boulder, USA. Electronic address:

We have looked at the effects of the cryoprotectant M22 upon viability in the model organism C. elegans. M22 is a well-known vitrification solution which has been successfully used in the laboratory to preserve organs destined for transplantation. Read More

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December 2018

Mesenchymal stem cells in preclinical cancer cytotherapy: a systematic review.

Stem Cell Res Ther 2018 Dec 7;9(1):336. Epub 2018 Dec 7.

Institute of Biological Research and Biotechnology, National Hellenic Research Foundation (NHRF), Konstantinou 48 Av., 116 35, Athens, Greece.

Mesenchymal stem cells (MSC) comprise a heterogeneous population of rapidly proliferating cells that can be isolated from adult (e.g., bone marrow, adipose tissue) as well as fetal (e. Read More

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December 2018

Deletion of the murine ortholog of the 8q24 gene desert has anti-cancer effects in transgenic mammary cancer models.

BMC Cancer 2018 Dec 10;18(1):1233. Epub 2018 Dec 10.

Department of Pathology and Laboratory Medicine, Medical University of South Carolina, 68 President Street, Charleston, SC, 29425, USA.

Background: The gene desert on human chromosomal band 8q24 harbors multiple genetic variants associated with common cancers, including breast cancer. The locus, including the gene desert and its flanking genes, MYC, PVT1 and FAM84B, is also frequently amplified in human breast cancer. We generated a megadeletion (MD) mouse model lacking 430-Kb of sequence orthologous to the breast cancer-associated region in the gene desert. Read More

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December 2018
3.362 Impact Factor

Berberine Effects on NFκB, HIF1A and NFE2L2/AP-1 Pathways in HeLa Cells.

Anticancer Agents Med Chem 2018 Dec 11. Epub 2018 Dec 11.

Biomedical Innovations LLC, 112 Mechnikova st., 344013, Rostov-on-Don. Russian Federation.

Background: Berberine has multitudinous anti-cancer stem cells effects making it a highly promising candidate substance for the next-generation cancer therapy. However, berberine modes of action predispose it to significant side-effects that probably limit its clinical testing and application.

Materials And Method: HeLa cells were treated with two concentrations of berberine (30 and 100 μM) for 24 hours to asses the functioning of the NFE2L2/AP-1, NFκB and HIF1A pathways using 22 RNAs expression qPCR-based analysis. Read More

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December 2018

Molecular dynamic simulations on an inhibitor of anti-apoptotic Bcl-2 proteins for insights into its interaction mechanism for anti-cancer activity.

J Biomol Struct Dyn 2018 Dec 10:1-13. Epub 2018 Dec 10.

b Dr. Bhanuben Nanavati College of Pharmacy , Mumbai , India.

Inhibition of normal cellular apoptosis or programed cell death is the hallmark of all cancers. Apoptotic dysregulation can result in numerous pathological conditions, such as cancers, autoimmune disorders, and neurodegeneration. Members of the BCL-2 family of proteins regulate the process of apoptosis by its promotion or inhibition and overexpression of the pro-survival anti-apoptotic proteins (Bcl-2, Bcl-xL, and Mcl-1) has been associated with tumor maintenance, growth and progression Small molecules and peptides which bind the BH3 binding groove of these proteins have been explored in the recent times for their anticancer potential. Read More

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December 2018
1 Read

Sarcopenia associated with chemotherapy and targeted agents for cancer therapy.

Ann Palliat Med 2018 Sep 7. Epub 2018 Sep 7.

Cancer Center, Geisinger Medical Center, Danville, PA, USA.

Clinicians often believe that cachexia is caused by cancer and anorexia as a toxicity of chemotherapy or targeted anti-cancer agents. It is now recognized that chemotherapy and certain targeted agents cause sarcopenia which reduce physical function and quality of life. Pre-treatment sarcopenia predicts chemotherapy toxicity, reduced response, increased disability, poor anti-tumor response and survival. Read More

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September 2018

Genus Psoralea A review of the traditional and modern uses, phytochemistry and pharmacology.

J Ethnopharmacol 2018 Dec 3. Epub 2018 Dec 3.

CSIR-National Botanical Research Institute, Plant Transgenic Laboratory, P.O. Box 436, Rana Pratap Marg,Lucknow-226 001, U.P., India. Electronic address:

Ethnopharmacological Relevance: The genus Psoralea (Fabaceae) harbours 105 accepted species that are extensively used by local peoples and medicinal practitioners of China, India, and other countries for treatment of tooth decay, psoriasis, leucoderma, leprosy, kidney problems, tuberculosis, indigestion, constipation and impotence. Presently, pharmacological research reports are available on only few species namely Bituminaria bituminosa (Syn: P. bituminosa), P. Read More

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December 2018
8 Reads

Preparation and optimization of poly (lactic acid) nanoparticles loaded with fisetin to improve anti-cancer therapy.

Int J Biol Macromol 2018 Dec 3. Epub 2018 Dec 3.

Department of Pharmaceutics, School of Pharmacy, Jiangsu University, Zhenjiang 212013, PR China. Electronic address:

Fisetin is a natural flavonoid with promising antitumor activity, whereas its clinical application is limited by its hydrophobic property. In this study, we aimed to load fisetin into poly(lactic acid) (PLA) nanoparticles to increase fisetin's solubility and therapeutic efficacy. Based on spontaneous emulsification solvent diffusion (SESD) method, the formulation of PLA nanoparticles was optimized by two successive experimental designs. Read More

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December 2018
2 Reads

Glucuronorhamnoxylan from Capsosiphon fulvescens inhibits the growth of HT-29 human colon cancer cells in vitro and in vivo via induction of apoptotic cell death.

Int J Biol Macromol 2018 Dec 3;124:1060-1068. Epub 2018 Dec 3.

Department of Biotechnology, The Catholic University of Korea, Bucheon, Gyeonggi-do 14662, Republic of Korea. Electronic address:

Colorectal cancer is the third most diagnosed cancer and a leading cause of cancer death. Dissatisfaction with currently available anti-colorectal cancer drugs caused by unwanted side effects and low efficacy necessitates new therapeutic agents. In the present study, a sulfated glucuronorhamnoxylan polysaccharide (named SPS-CF) purified from a green alga Capsosiphon fulvescens was evaluated for its anti-cancer activity in vitro and in vivo against colorectal cancer. Read More

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December 2018
1 Read

Cytochrome P450 epoxygenases and cancer: A genetic and a molecular perspective.

Pharmacol Ther 2018 Dec 3. Epub 2018 Dec 3.

Division of Nephrology and Hypertension, Department of Medicine, Vanderbilt University Medical Center, Nashville, Tennessee;; Department of Veterans Affairs, Nashville, TN, USA. Electronic address:

Cytochrome CYP450 epoxygenases catalyze the epoxidation of polyunsaturated fatty acids including arachidonic acid, eicosapentaenoic acid, and docosahexaenoic acid. The arachidonic acid-derived products are potent pro-angiogenic lipids and promote tumor development and growth. On the other hand, eicosapentaenoic acid- and docosahexaenoic acid-derived products inhibit angiogenesis and play a protective role in certain pathological conditions including cancer. Read More

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December 2018
3 Reads

Design, synthesis and anti-tumor evaluation of novel steroidal glycoconjugate with furoxan derivatives.

Steroids 2018 Dec 3;141:81-95. Epub 2018 Dec 3.

Department of Medicinal Chemistry, School of Pharmacy, Fudan University, Shanghai 201203, China. Electronic address:

In this study, eighteen novel steroidal-furoxan derivatives with 3-glycosyl or 3-methoxy moiety (12a-c, 13a-c, 17a-c, 26a-c, 27a-c and 28a-c) were synthesized and their anti-proliferative activity was evaluated against eight drug-sensitive and three drug-resistant cancer cell lines HeLa, A2780, LNCaP, PC-3, MDA-MB-231, MCF-7, SW480, A549, MCF-7/ADR, A2780/CDDP and A2780/T. Most of them displayed significant anti-cancer potency in vitro with IC values at the nanomole level. Among them, 3-methoxy steroidal-furoxan hybrids expressed much better activity than that of 3-glycosyl substitute ones, while estrane and 5α-H-androstane scaffold were slightly more favorable to the improvement of anti-proliferative activity. Read More

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December 2018
3 Reads

Oligomerization of equilibrative nucleoside transporters: a novel regulatory and functional mechanism involving PKC and PP1.

FASEB J 2018 Dec 6:fj201800440RR. Epub 2018 Dec 6.

Department of Chemistry and Biology, Ryerson University, Toronto, Ontario, Canada.

Equilibrative nucleoside transporters (ENTs) translocate nucleosides and nucleobases across plasma membranes, as well as a variety of anti-cancer, -viral, and -parasite nucleoside analogs. They are also key members of the purinome complex and regulate the protective and anti-inflammatory effects of adenosine. Despite their important role, little is known about the mechanisms involved in their regulation. Read More

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December 2018
2 Reads

Chinese Expert Consensus Workshop Report: Guideline for permanent iodine-125 seed implantation of primary and metastatic lung tumors.

Thorac Cancer 2018 Dec 6. Epub 2018 Dec 6.

Department of Interventional Medicine, The Second Hospital of Shandong University, Jinan, China.

Surgery remains the first choice of cure for early stage lung cancer. However, many patients are diagnosed at advanced stage, and thus miss the opportunity to undergo surgery. As such patients derive limited benefits from chemotherapy or radiotherapy, alternatives focusing on local control have emerged, including iodine-125 seed implantation. Read More

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December 2018
1 Read

Mesoporous silica nanoparticles as a prospective and promising approach for drug delivery and biomedical applications.

Curr Cancer Drug Targets 2018 Dec 5. Epub 2018 Dec 5.

Institute of Materia Medica, School of Pharmacy, Henan University, Jinming Road, Kaifeng, 475004. China.

Background: With the development of nanotechnology, nanocarrier has widely applied in such fields as drug delivery, diagnostic and medical imaging and engineering in recent years. Among all of the available nanocarrier, mesoporous silica nanoparticles (MSNs) have become a hot issue because of their unique properties, such as large surface area and voidage, tunable drug loading capacity and release kinetics, good biosafety and easily modified surface.

Objectives: We described the most recent progress in silica-assisted drug delivery and biomedical applications according to different types of Cargo in order to allow researchers to quickly learn about of the advance in this field. Read More

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December 2018

Doxorubicin effects on leukemia and breast cancer cells in culture on the TK1 protein levels using AroCell TK 210 ELISA: a tool for drug development.

Nucleosides Nucleotides Nucleic Acids 2018 Dec 6:1-8. Epub 2018 Dec 6.

a Department of Anatomy, Physiology and Biochemistry , Swedish University of Agricultural Sciences , VHC , Uppsala , Sweden.

In this study changes in thymidine kinase 1 (TK1) levels after 24 hours of Doxorubicin (Dox) exposure of CEM and MDA MB-231 cells were determined using the commercially available AroCell TK 210 ELISA test. In cell extracts, TK1 levels increased twofold with 1 µM Dox in both cell lines, while the TK1 levels in the culture media increased with 5 and 10 µM of Dox only in case of CEM cells. In conclusion, this study reveals that the TK 210 ELISA can measure changes in intra- and extracellular TK1 levels apparently related to the mechanism of cytotoxicity of anti-cancer agents. Read More

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December 2018

Alantolactone sensitizes human pancreatic cancer cells to EGFR inhibitors through the inhibition of STAT3 signaling.

Mol Carcinog 2018 Dec 5. Epub 2018 Dec 5.

Chemical Biology Research Center, School of Pharmaceutical Sciences, Wenzhou Medical University, Wenzhou, Zhejiang 325035, China.

Several studies have implicated the feedback activation of signal transducer and activator of transcription 3 (STAT3) as a new cancer drug-resistance mechanism and linked it to the failure of epidermal growth factor receptor (EGFR)-targeted therapies. In this study we discovered that Alantolactone, a natural sesquiterpene lactone, potently inhibited human pancreatic cancer cells and suppressed constitutively activated STAT3. In contrast, Alantolactone had little effect on the EGFR pathway. Read More

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December 2018

Focused ultrasound for the treatment of bone metastases: effectiveness and feasibility.

J Ther Ultrasound 2018 30;6. Epub 2018 Nov 30.

Department of Oncology, Centre de Lutte anti-Cancer Antoine Lacassagne, 33 Avenue de Valombrose, 06100 NICE, France.

Background: To evaluate the effectiveness and feasibility of high-intensity focused ultrasound (HIFU) for the treatment of bone metastases.

Methods: A single-center prospective study was made involving 17 consecutive patients with symptomatic bone metastases. Patients were treated by Focused Ultrasound (FUs) performed with magnetic resonance (MR) guidance. Read More

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November 2018
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Oxymatrine Synergistically Potentiates the Antitumor Effects of Cisplatin in Human Gastric Cancer Cells.

J Cancer 2018 31;9(23):4527-4535. Epub 2018 Oct 31.

Department of General Surgery, Wujiang No.1 People's Hospital affiliated to Nantong University, Suzhou, Jiangsu 215200, PR China.

Cisplatin (CDDP) has been extensively used for gastric cancer (GC) treatment but limited by drug resistance and severe toxicity. The chemo-sensitizers that enhance its efficiency and overcome its limitation are urgently needed. Oxymatrine (OMT), a primary active ingredient from the dry roots of Sophora favescens, has shown powerful anti-cancer property with little side-effect. Read More

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October 2018

ALS-Associated E478G Mutation in Human OPTN (Optineurin) Promotes Inflammation and Induces Neuronal Cell Death.

Front Immunol 2018 14;9:2647. Epub 2018 Nov 14.

State Key Laboratory of Molecular Biology, CAS Center for Excellence in Molecular Cell Science, Innovation Center for Cell Signaling Network, Shanghai Institute of Biochemistry and Cell Biology, University of Chinese Academy of Sciences, Shanghai, China.

Amyotrophic Lateral Sclerosis (ALS) is a group of neurodegenerative disorders that featured with the death of motor neurons, which leads to loss of voluntary control on muscles. The etiologies vary among different subtypes of ALS, and no effective management or medication could be provided to the patients, with the underlying mechanisms incompletely understood yet. Mutations in human (Optineurin), particularly E478G, have been found in many ALS patients. Read More

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November 2018
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DHS (trans-4,4'-dihydroxystilbene) suppresses DNA replication and tumor growth by inhibiting RRM2 (ribonucleotide reductase regulatory subunit M2).

Oncogene 2018 Dec 5. Epub 2018 Dec 5.

Department of Biochemistry and Molecular Medicine, The George Washington University School of Medicine and Health Sciences, Washington, DC, USA.

DNA replication machinery is responsible for accurate and efficient duplication of the chromosome. Since inhibition of DNA replication can lead to replication fork stalling, resulting in DNA damage and apoptotic death, inhibitors of DNA replication are commonly used in cancer chemotherapy. Ribonucleotide reductase (RNR) is the rate-limiting enzyme in the biosynthesis of deoxyribonucleoside triphosphates (dNTPs) that are essential for DNA replication and DNA damage repair. Read More

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December 2018

5-Fluorouracil inhibits neural differentiation via Mfn1/2 reduction in human induced pluripotent stem cells.

J Toxicol Sci 2018 ;43(12):727-734

Division of Pharmacology, National Institute of Health Sciences, Japan.

5-fluorouracil (5-FU) has been widely used for the treatment of tumors. Regardless of its widespread use as an anti-cancer drug, 5-FU therapy can cause several side effects, including developmental toxicity and neurotoxicity. However, the potential action of 5-FU at the early fetal stage has not yet been completely elucidated. Read More

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January 2018

The natural polyphenol curcumin induces apoptosis by suppressing STAT3 signaling in esophageal squamous cell carcinoma.

J Exp Clin Cancer Res 2018 Dec 5;37(1):303. Epub 2018 Dec 5.

Department of Pathophysiology, School of Basic Medical Sciences, Zhengzhou University, Zhengzhou, Henan, 450001, People's Republic of China.

Background: We and others have previously shown that the STAT3 signaling pathway is activated in some esophageal squamous cell carcinoma (ESCC) cells and is required for the survival and growth of these primary ESCC-derived xenografts. It has also been shown that the natural polyphenol curcumin is an effective anti-tumor agent.

Methods: Luciferase assay and immunoblotting were performed to examine whether curcumin suppressed STAT3 signaling. Read More

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December 2018

A Promising Biocompatible Platform: Lipid-Based and Bio-Inspired Smart Drug Delivery Systems for Cancer Therapy.

Int J Mol Sci 2018 Dec 4;19(12). Epub 2018 Dec 4.

International Research Organization for Advanced Science and Technology (IROAST), Kumamoto University, Kumamoto 860-8555, Japan.

Designing new drug delivery systems (DDSs) for safer cancer therapy during pre-clinical and clinical applications still constitutes a considerable challenge, despite advances made in related fields. Lipid-based drug delivery systems (LBDDSs) have emerged as biocompatible candidates that overcome many biological obstacles. In particular, a combination of the merits of lipid carriers and functional polymers has maximized drug delivery efficiency. Read More

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December 2018