791 results match your criteria widr cells

Oxymestane, a cytostatic steroid derivative of exemestane with greater antitumor activity in non-estrogen-dependent cell lines.

J Steroid Biochem Mol Biol 2021 Jul 14;212:105950. Epub 2021 Jul 14.

University of Coimbra, CIEPQPF, FFUC, Laboratory of Pharmaceutical Chemistry, Azinhaga de Santa Comba, Pólo III - Pólo das Ciências da Saúde, Coimbra, 3000-548, Portugal. Electronic address:

A new promising steroid derivative of Exemestane (Exe), the drug used for the treatment of estrogen-dependent breast cancer, was synthesized and evaluated against a set of human cancer cell lines. The new compound (Oxymestane-D1, Oxy) was tested comparatively with Exe against colon (C2BBe1, WiDr), liver (HepG2, HuH-7), lung (A549, H1299) and prostate (LNCaP, PC3) human cancer cell lines. Likewise, its effect on human colon normal cells (CCD-841 CoN) and human normal fibroblast cells (HFF-1) was studied. Read More

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Inhibition of Heat-shock Protein 27 Reduces 5-Fluorouracil-acquired Resistance in Human Colon Cancer Cells.

Anticancer Res 2021 Mar;41(3):1283-1290

Department of Surgery, Keio University School of Medicine, Tokyo, Japan.

Background/aim: In previous work we showed that expression of heat-shock protein 27 (HSP27; encoded by HSPB1) was associated with inherent resistance to 5-fluorouracil (5-FU). However, the relationship between HSP27 and acquired resistance remains unknown.

Materials And Methods: We generated an acquired resistance model (WiDr-R) of a colon cancer cell line by exposing WiDr cells to 5-FU. Read More

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Biological Activities of Different Strains of the Genus Ganoderma spp. (Agaricomycetes) from Mexico.

Int J Med Mushrooms 2021 ;23(2):67-77

Centro de Investigación de Micología Aplicada, Universidad Veracruzana, 91010, Xalapa, Veracruz, Mexico.

Antiproliferative, antioxidant, and antibacterial activities were determined for 14 extracts obtained with a mixture of chloroform-methanol (1:1) from the mycelial cultures of 14 wild strains of the genus Ganoderma collected in the central-south part of Veracruz Province, Mexico. Identification of the strains collected was confirmed based on rDNA internal transcribed spacer phylogenetic analysis. The strains G. Read More

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January 2021

Evaluation of Combined CK2 Inhibition and Irradiation in Human WiDr Tumours.

In Vivo 2021 Jan-Feb;35(1):111-117

Department of Radiation Oncology, Heidelberg University Hospital, Heidelberg, Germany.

Background/aim: Casein kinase 2 (CK2) which sustains multiple pro-survival functions in cellular DNA-damage response, is strictly regulated in normal cells but elevated in cancer. CK2 is considered as a potential therapeutic target, and its inhibition has been associated with radiosensitization in mammalian cells in vitro. Here, we investigated potential radiosensitization by CK2 inhibition in vivo. Read More

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Enhancing antibody-dependent cellular phagocytosis by Re-education of tumor-associated macrophages with resiquimod-encapsulated liposomes.

Biomaterials 2021 01 13;268:120601. Epub 2020 Dec 13.

The Institute of Scientific and Industrial Research, Osaka University, Ibaraki 567-0047, Japan. Electronic address:

Tumor-associated macrophages (TAMs) exist in nearly all tumors, and form a major part of the tumor microenvironment. TAMs are divided into two groups: tumor-suppressing M1 type and tumor-promoting M2 type. Most TAMs are educated by the tumor cells to become M2 type, which support tumor growth and make immunotherapy ineffective. Read More

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January 2021

Gb3-cSrc complex in glycosphingolipid-enriched microdomains contributes to the expression of p53 mutant protein and cancer drug resistance via β-catenin-activated RNA methylation.

FASEB Bioadv 2020 Nov 2;2(11):653-667. Epub 2020 Sep 2.

School of Basic Pharmaceutical and Toxicological Sciences College of Pharmacy University of Louisiana at Monroe Monroe Louisiana USA.

Glucosylceramide synthase (GCS) is a key enzyme catalyzing ceramide glycosylation to generate glucosylceramide (GlcCer), which in turn serves as the precursor for cells to produce glycosphingolipids (GSLs). In cell membranes, GSLs serve as essential components of GSL-enriched microdomains (GEMs) and mediate membrane functions and cell behaviors. Previous studies showed that ceramide glycosylation correlates with upregulated expression of p53 hotspot mutant R273H and cancer drug resistance. Read More

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November 2020

Epithelial Transfer of the Tyrosine Kinase Inhibitors Erlotinib, Gefitinib, Afatinib, Crizotinib, Sorafenib, Sunitinib, and Dasatinib: Implications for Clinical Resistance.

Cancers (Basel) 2020 Nov 10;12(11). Epub 2020 Nov 10.

Department of Medical Oncology, Amsterdam UMC, VU University Medical Center, PO Box 7057, 1007 MB Amsterdam, The Netherlands.

tyrosine kinase inhibitors (TKIs) inhibit phosphorylation of signaling proteins. TKIs often show large variations in the clinic due to poor pharmacology, possibly leading to resistance. We compared gut absorption of inhibitors of epidermal growth factor receptor (erlotinib, gefitinib, and afatinib), ALK-cMET (crizotinib), PDGFR/BCR-Abl (dasatinib), and multikinase inhibitors (sunitinib and sorafenib). Read More

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November 2020

Optimizing the Profile of [Tc]Tc-NT(7-13) Tracers in Pancreatic Cancer Models by Means of Protease Inhibitors.

Int J Mol Sci 2020 Oct 26;21(21). Epub 2020 Oct 26.

Molecular Radiopharmacy, INRASTES, NCSR "Demokritos", 15341 Athens, Greece.

Background: The overexpression of neurotensin subtype 1 receptors (NTS1Rs) in human tumors may be elegantly exploited for directing neurotensin (NT)-based radionuclide carriers specifically to cancer sites for theranostic purposes. We have recently shown that [Tc]Tc-DT1 ([Tc]Tc-[N-Gly]NT(7-13)) and [Tc]Tc-DT5 ([Tc]Tc-[N-Ala,Dab]NT(7-13)) show notably improved uptake in human colon adenocarcinoma WiDr xenografts in mice treated with neprilysin (NEP) inhibitors and/or angiotensin-converting enzyme (ACE) inhibitors compared with untreated controls. Aiming toward translation of this promising approach in NTS1R-positive pancreatic ductal adenocarcinoma (PDAC) patients, we now report on the impact of registered NEP/ACE inhibitors on the performance of [Tc]Tc-DT1 and [Tc]Tc-DT5 in pancreatic cancer models. Read More

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October 2020

Synthesis, in vitro, and in vivo evaluation of novel N-phenylindazolyl diarylureas as potential anti-cancer agents.

Sci Rep 2020 10 21;10(1):17969. Epub 2020 Oct 21.

Integrated Biosciences Graduate Program, University of Minnesota, Duluth, MN, 55812, USA.

Novel N-phenylindazole based diarylureas have been designed, synthesized and evaluated as potential anticancer agents. In vitro cell viability studies of these derivatives illustrate good potency with IC values in the range of 0.4-50 μM in several cancer cell lines including murine metastatic breast cancer 4T1, murine glioblastoma GL261, human triple negative breast cancer MDA-MB-231, human pancreatic cancer MIAPaCa-2, and human colorectal cancer cell line WiDr. Read More

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October 2020

Two new 2-arylbenzofurans from L. and their cytotoxicity towards cancer cell.

Nat Prod Res 2020 Sep 18:1-6. Epub 2020 Sep 18.

Natural Products Chemistry Research Group, Organic Chemistry Division, Department of Chemistry, Faculty of Science and Technology, Universitas Airlangga, Surabaya, Indonesia.

Two new 2-arylbenzofurans, sesbagrandiflorain D () and E () along with two known 2-arylbenzofurans, spinosan A () and spinosan B () were isolated from the stem bark of L. The structure of two new compounds established by HRESIMS, 1 D NMR (H, C) and 2 D NMR (HMQC, HMBC) spectra. Compounds (-) assayed for their cytotoxicity towards three human cancer cells (MCF-7, HeLa, and WiDr). Read More

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September 2020

γ-H2AX as a potential indicator of radiosensitivity in colorectal cancer cells.

Oncol Lett 2020 Sep 26;20(3):2331-2337. Epub 2020 Jun 26.

Department of General and Gastroenterological Surgery, Osaka Medical College, Osaka 569-8686, Japan.

Preoperative radiotherapy improves local disease control and disease-free survival in patients with advanced rectal cancer; however, a reliable predictive biomarker for the effectiveness of irradiation has yet to be elucidated. Phosphorylation of H2A histone family member X (H2AX) to γ-H2AX is induced by DNA double-strand breaks and is associated with the development of colorectal cancer (CRC). The current study aimed to clarify the relationship between γ-H2AX expression and CRC radiosensitivity and . Read More

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September 2020

Placenta-specific protein 1 enhances liver metastatic potential and is associated with the PI3K/AKT/NF-κB signaling pathway in colorectal cancer.

Eur J Cancer Prev 2021 May;30(3):220-231

Department of Oncological Surgery, The First Affiliated Hospital of Bengbu Medical College, Bengbu, Anhui, P.R. China.

To better explore the underlying mechanism of liver metastatic formation by placenta-specific protein 1 (PLAC1) in human colorectal cancer, we investigated the proliferation, invasion and angiogenic capabilities of human colorectal cancer cells with different liver metastatic potentials as well as the mechanism of action of PLAC1 in the metastatic process. The expression of PLAC1 was detected by reverse transcriptase PCR, western blot, and real-time PCR. The effect of PLAC1 on metastatic potential was determined by proliferation, invasion, and angiogenesis assays, including an in-vitro coculture system consisting of cancer cells and vascular endothelial cells that were used to detect the relationship between cancer cells and angiogenesis. Read More

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Anticancer Activity of Polyisoprenoids from Blume. in WiDr Cells.

Iran J Pharm Res 2019 ;18(3):1477-1487

Department of Forestry, Faculty of Forestry, University of Sumatera Utara, Medan, Indonesia.

Colorectal cancer is the third most common cancer world wide and has been occurred more in developing regions. The use of conventional chemotherapy agents may lead to various adverse effects. Therefore, it is required to find the potential drug for anticancer from alternative source of natural product including mangrove plants. Read More

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January 2019

Synthesis and biological evaluation of arylphosphonium-benzoxaborole conjugates as novel anticancer agents.

Bioorg Med Chem Lett 2020 07 12;30(14):127259. Epub 2020 May 12.

Integrated Biosciences Graduate Program, University of Minnesota, Duluth, MN 55812, USA; Department of Chemistry and Biochemistry, University of Minnesota Duluth, Duluth, MN 55812, USA; Department of Pharmacy Practice Pharmaceutical Sciences, University of Minnesota, Duluth, MN 55812, USA. Electronic address:

Arylphosphonium-benzoxaborole conjugates have been synthesized as potential mitochondria targeting anticancer agents. The synthesized compounds have been tested for their effects on cell viability in various solid tumor cell lines including breast cancer 4T1 and MCF-7, pancreatic cancer MIAPaCa-2 and colorectal adenocarcinoma WiDr. Compound 6c is designated as a lead compound for further studies due to its enhanced effects on cell viability in the above-mentioned cell lines. Read More

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Key-Protease Inhibition Regimens Promote Tumor Targeting of Neurotensin Radioligands.

Pharmaceutics 2020 Jun 9;12(6). Epub 2020 Jun 9.

Molecular Radiopharmacy, INRASTES, NCSR "Demokritos", 15341 Athens, Greece.

Neurotensin subtype 1 receptors (NTS1R) represent attractive molecular targets for directing radiolabeled neurotensin (NT) analogs to tumor lesions for diagnostic and therapeutic purposes. This approach has been largely undermined by the rapid in vivo degradation of linear NT-based radioligands. Herein, we aim to increase the tumor targeting of three Tc-labeled NT analogs by the in-situ inhibition of two key proteases involved in their catabolism. Read More

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GC-MS metabolomics revealed protocatechuic acid as a cytotoxic and apoptosis-inducing compound from black rice brans.

Food Sci Biotechnol 2020 Jun 7;29(6):825-835. Epub 2020 Feb 7.

Department of Food Science and Technology, Faculty of Agricultural Technology, Bogor Agricultural University (IPB University), PO BOX 220, IPB Darmaga Campus, Bogor, 16002 Indonesia.

GC-MS metabolomics was used to discriminate the phytochemicals profile of Indonesian white, red, and black rice brans, and Japanese white rice brans. This technique was used for the first time to identify compounds in rice brans having cytotoxic activity against WiDr colon cancer cells. Orthogonal Projection to the Latent Structure (OPLS) analysis showed that protocatechuic acid (PA) was a discriminating factor found in black rice brans which strongly correlated with its cytotoxicity (IC 8. Read More

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An Animal Model of Colorectal Cancer Liver Metastasis With a High Metastasis Rate and Clonal Dynamics.

Anticancer Res 2020 Jun;40(6):3297-3306

Department of Pharmacology, Busan Paik Hospital, Inje University College of Medicine, Busan, Republic of Korea.

Background: Various animal models have been introduced into the study of liver metastasis of colorectal cancer, but they have not been compared under the same conditions. The aim of this study was to identify an optimized mouse model that showed a high rate of hepatic metastasis and expression of clonal dynamics.

Materials And Methods: Athymic nude mice (n=30) were divided into two equal groups for the creation of a splenic injection model (SIM) and surgically orthotopic implantation model (SOIM) of liver metastasis of colorectal cancer using HCT116 cells. Read More

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Amphiphilic Rhenium-Oxo Corroles as a New Class of Sensitizers for Photodynamic Therapy.

ACS Omega 2020 May 27;5(18):10596-10601. Epub 2020 Apr 27.

Department of Clinical and Molecular Medicine and Department of Physics, Norwegian University of Science and Technology, NTNU, N-7491 Trondheim, Norway.

A set of rhenium(V)-oxo -triarylcorroles bearing ester and carboxylic acid functionalities were synthesized with a view to determining their potential for photodynamic therapy. Toward this end, we measured their near-IR phosphorescence and their ability to sensitize singlet oxygen formation. The two esters studied, ReO 5,10,15-tris(-carbomethoxyphenyl)corrole and ReO 5,10,15-tris(-carbomethoxyphenyl)corrole, were found to exhibit phosphorescence quantum yields of around 1% and fairly long phosphorescence lifetimes of about 60 μs in toluene. Read More

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New in vitro highly cytotoxic platinum and palladium cyanoximates with minimal side effects in vivo.

J Inorg Biochem 2020 07 6;208:111082. Epub 2020 May 6.

Department of Chemistry, Temple Hall 431, Missouri State University, 901 S. National, Springfield, MO 65897, USA. Electronic address:

Several biologically active bivalent Pd and Pt complexes with two structurally similar cyanoxime ligands abbreviated as H(DECO): 2-oximino-2-cyano-N,N'-diethylacetamide, and H(PyrCO): 2-oximino-2-cyan-N-pyrrolidine acetamide were synthesized and characterized using spectroscopic methods, thermal analysis and X-ray crystallography. Structures revealed planar cis-geometry of studied complexes. Freshly obtained Pt(DECO), Pd(DECO), Pt(PyrCO) and Pd(PyrCO) complexes were used in for in vitro cytotoxicity assays using two different etiology human cancer cell lines HeLa and WiDr cells. Read More

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Methanol Extract of (Lour) Exhibited Antiproliferative Activity and Induced Programmed Cell Death in Colon Cancer Cell WiDr.

Int J Food Sci 2020 24;2020:9068326. Epub 2020 Jan 24.

Primate Research Center, Bogor Agricultural University, Jalan Lodaya II/5, Bogor 16151, Indonesia.

(Lour) (CA) has been reported to possess many pharmacological activities. In this study, evaluation of cytotoxicity using brine shrimp lethality bioassay and MTT assay using WiDr cell lines was carried out. The expression of several genes responsible for programmed cell death of the methanol extract of CA was also investigated. Read More

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January 2020

Bioassay-Guided Isolation and HPLC Quantification of Antiproliferative Metabolites from .

Molecules 2020 Jan 28;25(3). Epub 2020 Jan 28.

Division of Chinese Materia Medica Development, National Research Institute of Chinese Medicine, Taipei 11221, Taiwan.

In folk medicine, Gagnep. has been used to treat diseases related to inflammation, ulcers, and cancer. There are no reports concerning the chemical components and bioactivities of ; thus, this study aims to explore the phytochemicals, quantify the main compounds, and test the anticancer activity of isolates from Dried rhizomes were extracted with 95% ethanol and, then, partitioned, fractionated, and isolated. Read More

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January 2020

Urotensin-II-Targeted Liposomes as a New Drug Delivery System towards Prostate and Colon Cancer Cells.

J Oncol 2019 17;2019:9293560. Epub 2019 Dec 17.

Department of Precision Medicine, University of Campania "L. Vanvitelli", Via L. de Crecchio, 7, 80138 Naples, Italy.

Urotensin-II (UT-II) and its receptor (UTR) are involved in the occurrence of different epithelial cancers. In particular, UTR was found overexpressed on colon, bladder, and prostate cancer cells. The conjugation of ligands, able to specifically bind receptors that are overexpressed on cancer cells, to liposome surface represents an efficient active targeting strategy to enhance selectivity and efficiency of drug delivery systems. Read More

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December 2019

Novel Efficient Bioprocessing of Marine Chitins into Active Anticancer Prodigiosin.

Mar Drugs 2019 Dec 23;18(1). Epub 2019 Dec 23.

Department of Chemistry, Tamkang University, New Taipei City 25137, Taiwan.

Marine chitins (MC) have been utilized for the production of vast array of bioactive products, including chitooligomers, chitinase, chitosanase, antioxidants, anti-NO, and antidiabetic compounds. The aim of this study is the bioprocessing of MC into a potent anticancer compound, prodigiosin (PG), via microbial fermentation. This bioactive compound was produced by TKU011 with the highest yield of 4. Read More

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December 2019

Carcinoembryonic antigen-targeted photodynamic therapy in colorectal cancer models.

EJNMMI Res 2019 Dec 11;9(1):108. Epub 2019 Dec 11.

Department of Radiology and Nuclear Medicine, Radboud University Medical Center, PO Box 9101, 6500 HB, Nijmegen, The Netherlands.

Background: In colorectal cancer, survival of patients is drastically reduced when complete resection is hampered by involvement of critical structures. Targeted photodynamic therapy (tPDT) is a local and targeted therapy which could play a role in eradicating residual tumor cells after incomplete resection. Since carcinoembryonic antigen (CEA; CEACAM5) is abundantly overexpressed in colorectal cancer, it is a potential target for tPDT of colorectal cancer. Read More

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December 2019

Development of Novel Silyl Cyanocinnamic Acid Derivatives as Metabolic Plasticity Inhibitors for Cancer Treatment.

Sci Rep 2019 12 4;9(1):18266. Epub 2019 Dec 4.

Integrated Biosciences Graduate Program, University of Minnesota, Duluth, MN, 55812, USA.

Novel silyl cyanocinnamic acid derivatives have been synthesized and evaluated as potential anticancer agents. In vitro studies reveal that lead derivatives 2a and 2b have enhanced cancer cell proliferation inhibition properties when compared to the parent monocarboxylate transporter (MCT) inhibitor cyano-hydroxycinnamic acid (CHC). Further, candidate compounds exhibit several-fold more potent MCT1 inhibition properties as determined by lactate-uptake studies, and these studies are supported by MCT homology modeling and computational inhibitor-docking studies. Read More

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December 2019

anticancer activity extract nanoparticle on WiDr cells.

J Adv Pharm Technol Res 2019 Oct-Dec;10(4):149-154

Department of Pharmacology, Faculty of Veterinary Medicine, Airlangga University, Surabaya, Indonesia.

This study aimed to prepare leaf extract-loaded chitosan nanoparticles (nano-ASLE) against human colon cancer (WiDr) cells. Nano-ASLE was made with ionic gelation method. Four concentrations of the nano-ASLE (50, 100, 200, and 400 μg/mL) in dimethyl sulfoxide were prepared on WiDr cells to determine the IC value using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. Read More

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November 2019

α-Aminoisobutyric Acid-Containing Amphipathic Helical Peptide-Cyclic RGD Conjugation as a Potential Drug Delivery System for MicroRNA Replacement Therapy in Vitro.

Mol Pharm 2019 11 25;16(11):4542-4550. Epub 2019 Oct 25.

Department of Bioorganic Chemistry , Osaka University of Pharmaceutical Sciences , 4-20-1 Nasahara , Takatsuki , Osaka 569-1094 , Japan.

Replacement therapy with tumor suppressive microRNA (TS-miRNA) might be the next-generation oligonucleotide therapy; however, a novel drug delivery system (DDS) is required. Recently, we developed the cell-penetrating peptide, model amphipathic peptide with α-aminoisobutyric acid (MAP(Aib)), as a carrier for oligonucleotide delivery to cells. In this study, we examined whether a modified MAP(Aib) analogue, MAP(Aib)-cRGD, could be a DDS for TS-miRNA replacement therapy. Read More

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November 2019

A new steroid glycoside from : cytotoxic activity and docking studies.

Nat Prod Res 2021 Jul 26;35(13):2224-2231. Epub 2019 Sep 26.

Faculty of Science, Department of Pharmacy, Tadulako University, Palu, Indonesia.

Chemical investigation on the ethyl acetate extract of the aerial parts of afforded a new steroid glycoside, 9(11)α,16(17)α-dioxirane-20,25-dihydroxy-β-sitosterol-3--β-glucopyranoside () along with a known steroidal glycoside, β-sitosterol-3--β-D-glucopyranoside (). The Chemical structures were elucidated by 1D and 2D NMR and mass spectroscopic analysis. Cytotoxicity against four different cancer cell lines (HeLa, T47D, WiDr and Vero) was assessed. Read More

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Overcoming radioresistance in WiDr cells with heavy ion irradiation and radiosensitization by 2-deoxyglucose with photon irradiation.

Clin Transl Radiat Oncol 2019 Nov 20;19:52-58. Epub 2019 Aug 20.

Department of Radiation Oncology, University Hospital Heidelberg, Im Neuenheimer Feld 400, 69120 Heidelberg, Germany.

Background And Purpose: Radiosensitizers and heavy ion irradiation could improve therapy for female patients with malignant tumors located in the pelvic region through dose reduction. Aim of the study was to investigate the radiosensitizing potential of 2-deoxy-d-glucose (2-DG) in combination with carbon ion-irradiation (C) in representative cell lines of cancer in the female pelvic region.

Materials And Methods: The human cervix carcinoma cell line CaSki and the colorectal carcinoma cell line WiDr were used. Read More

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November 2019

Whole Transcriptome Analysis Identifies TNS4 as a Key Effector of Cetuximab and a Regulator of the Oncogenic Activity of KRAS Mutant Colorectal Cancer Cell Lines.

Cells 2019 08 12;8(8). Epub 2019 Aug 12.

Department of Nanobiomedical Science, Dankook University, Cheonan 31116, Korea.

The targeting of activated epidermal growth factor receptor (EGFR) with therapeutic anti-EGFR monoclonal antibodies (mAbs) such as cetuximab and panitumumab has been used as an effective strategy in the treatment of colorectal cancer (CRC). However, its clinical efficacy occurs only in a limited number of patients. Here, we performed whole-transcriptome analysis in xenograft mouse tumors induced by mutation-bearing LS174T CRC cells following treatment with either cetuximab or PBS. Read More

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