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https://www.readbyqxmd.com/read/28737925/lipid-bilayer-gated-mesoporous-silica-nanocarriers-for-tumor-targeted-delivery-of-zoledronic-acid-in-vivo
#1
Diti Desai, Jixi Zhang, Jouko Sandholm, Jaakko Lehtimäki, Tove Grönroos, Johanna Tuomela, Jessica M Rosenholm
Zoledronic acid (ZOL) is a nitrogen-containing bisphosphonate used for the treatment of bone diseases and calcium metabolism. Anticancer activity of ZOL has been established, but its extraskeletal effects are limited due to its rapid uptake and accumulation to bone hydroxyapatite. In this work, we report on the development of tethered lipid bilayer-gated mesoporous silica nanocarriers (MSNs) for the incorporation, retention and intracellular delivery of ZOL. The in vitro anticancer activity of ZOL-loaded nanocarriers was evaluated by cell viability assay and live-cell imaging...
July 24, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28737900/accumulation-of-charantin-and-expression-of-triterpenoid-biosynthesis-genes-in-bitter-melon-momordica-charantia
#2
Do Manh Cuong, Jin Jeon, Abubaker M A Morgan, Changsoo Kim, Jae Kwang Kim, Sook Young Lee, Sang Un Park
Charantin, a natural cucurbitane type triterpenoid, has been reported to have beneficial pharmacological functions such as anticancer, antidiabetic, and antibacterial activities. However, accumulation of charantin in bitter melon has been little studied. Here, we performed a transcriptome analysis to identify genes involved in the triterpenoid biosynthesis pathway in bitter melon seedlings. Total of 88,703 transcripts with an average length of 898 bp were identified in bitter melon seedlings. Based on a functional annotation, we identified 15 candidate genes encoding enzymes related to triterpenoid biosynthesis and analyzed their expression in different organs of mature plants...
July 24, 2017: Journal of Agricultural and Food Chemistry
https://www.readbyqxmd.com/read/28737849/antifungal-activity-of-alkaloids-against-candida-albicans
#3
Juliana Noguti, Mersedeh Rajinia, Bruna Raquel Zancope, Maria Carolina Salome Marquezin, Dalia Seleem, Vanessa Pardi, Ramiro M Murata
Candida albicans is a pathogen in the mouth responsible for opportunistic infections that are usually harmless. Natural products have been used to develop several drugs, mostly anticancer and anti-infective agents. Among these, alkaloids have been studied for their medicinal properties. In this study, we examined their antifungal activity against C. albicans in vitro. Among the alkaloids studied in this work, berberine hydrochloride showed the best activity against C. albicans.
August 2016: Journal—California Dental Association
https://www.readbyqxmd.com/read/28737832/self-assembled-polyprodrug-amphiphile-for-subcutaneous-xenograft-tumor-inhibition-with-prolonged-acting-time-in-vivo
#4
Dong Chen, Yu Huang, Shuting Xu, Huangyong Jiang, Jieli Wu, Xin Jin, Xinyuan Zhu
Polymeric drug delivery system termed as "polyprodrug amphiphile" poly(2-methylacryloyloxyethyl phosphorylcholine)-b-poly(10-hydroxy-camptothecin methacrylate (pMPC-b-pHCPT) is developed for the prolonged-acting cancer therapy. It is obtained by two-step reversible addition-fragmentation chain transfer polymerization of zwitterionic monomer MPC and an esterase-responsive polymerizable prodrug methacrylic anhydride-CPT, respectively. This diblock polymer is composed of both antifouling (pMPC) and bioactive (pHCPT) segments and the drug is designed as a building block to construct the polymer skeleton directly...
July 24, 2017: Macromolecular Bioscience
https://www.readbyqxmd.com/read/28737825/combination-of-rapamycin-and-garlic-derived-s-allylmercaptocysteine-induces-colon-cancer-cell-apoptosis-and-suppresses-tumor-growth-in-xenograft-nude-mice-through-autophagy-p62-nrf2-pathway
#5
Siying Li, Guang Yang, Xiaosong Zhu, Lin Cheng, Yueyue Sun, Zhongxi Zhao
The natural plant-derived product S-allylmercapto-cysteine (SAMC) has been studied in cancer therapy as a single and combination chemotherapeutic agent. The present study was employed to verify the combination use of SAMC and rapamycin that is the mTOR inhibitor with anticancer ability but has limited efficacy due to drug resistance, and to explore the underlying mechanisms. We combined rapamycin and SAMC for colorectal cancer treatment in the HCT‑116 cancer cells and a xenograft murine model. The in vivo study was established by xenografting HCT‑116 cells in BALB/c nude mice...
July 24, 2017: Oncology Reports
https://www.readbyqxmd.com/read/28737785/how-to-obtain-pt-iv-complexes-suitable-for-conjugation-to-nanovectors-from-the-oxidation-of-ptcl-terpyridine
#6
E Gabano, E Perin, C Fielden, J A Platts, A Gallina, B Rangone, M Ravera
Oxidation of [Pt((II))Cl(terpy)](+) (terpy = 2,2':6',2''-terpyridine) has been attempted with several oxidizing agents and under different experimental conditions in order to obtain a Pt(iv) complex suitable for the conjugation to nanovectors to be used in drug delivery targeting for anticancer therapy. The best compromise in terms of yield and purity of the final complex was obtained by microwave-assisted reaction at 70 °C in 50% aqueous H2O2 for 2 h. Under these conditions the quantitative formation of [Pt((IV))Cl(OH)2(terpy)](+) was observed...
July 24, 2017: Dalton Transactions: An International Journal of Inorganic Chemistry
https://www.readbyqxmd.com/read/28737782/ferrocene-cinchona-hybrids-with-triazolyl-chalcone-linkers-act-as-pro-oxidants-and-sensitize-human-cancer-cell-lines-to-paclitaxel
#7
Ana Podolski-Renić, Szilvia Bősze, Jelena Dinić, László Kocsis, Ferenc Hudecz, Antal Csámpai, Milica Pešić
Recently, we demonstrated that ferrocene-containing compounds with a cinchona moiety displayed marked anticancer activity. Here we report on the effects of the most promising isomers encompassing quinine- (compounds 4 and 5) and quinidine-epimers (compounds 6 and 7) - synthesized using improved methods providing controlled diastereoselectivity - in three different human multidrug resistant (MDR) cancer cell lines and their sensitive counterparts (non-small cell lung carcinoma NCI-H460/R/NCI-H460, colorectal carcinoma DLD1-TxR/DLD1 and glioblastoma U87-TxR/U87)...
July 24, 2017: Metallomics: Integrated Biometal Science
https://www.readbyqxmd.com/read/28737386/telomerase-inhibition-and-human-telomeric-g-quadruplex-dna-stabilization-by-a-%C3%AE-carboline-benzimidazole-derivative-at-low-concentration
#8
Kranthikumar Yadav, Penchala Narasimha Rao Meka, Sudeshna Sadhu, Sravanthi Devi Guggilapu, Jeshma Kovvuri, Ahmed Kamal, Ragampeta Srinivas, Panuganti Devayani, Bathini Nagendra Babu, Narayana Nagesh
Guanine rich regions in DNA, which can form highly stable secondary structures, namely, G-quadruplex or G4 DNA structures, affects DNA replication and transcription. Molecules that stabilize G4 DNA have attained importance in recent years. In the present study, G4 DNA stabilization, inhibition of telomerase and anticancer activity of synthetic β-carboline-benzimidazoles (5a, 5d, 5h and 5r), were studied. Among them, derivatives containing a 4-methoxyphenyl ring at C1 and 6-methoxy substituted benzimidazole at C3 (5a) was found to stabilize telomeric G-quadruplex DNA efficiently...
July 24, 2017: Biochemistry
https://www.readbyqxmd.com/read/28736788/characterisation-of-anticancer-peptides-at-the-single-cell-level
#9
L Armbrecht, G Gabernet, F Kurth, J A Hiss, G Schneider, P S Dittrich
The development of efficacious anticancer therapeutics is difficult due to the heterogeneity of the cellular response to chemotherapy. Anticancer peptides (ACPs) are promising drug candidates that have been shown to be active against a range of cancer cells. However, few ACP studies focus on tumour single-cell heterogeneities. In order to address this need, we developed a microfluidic device and an imaging procedure that enable the capture, monitoring, and analysis of several hundred single cells for the study of drug response...
July 24, 2017: Lab on a Chip
https://www.readbyqxmd.com/read/28734965/enhanced-immunostimulatory-activity-of-in-silico-discovered-agonists-of-toll-like-receptor-2-tlr2
#10
M S Murgueitio, S Ebner, P Hörtnagl, C Rakers, R Bruckner, P Henneke, G Wolber, S Santos-Sierra
BACKGROUND: Emergent therapies in anticancer vaccination use Toll-like receptors (TLRs) agonists as dendritic cell (DC) vaccine adjuvants. DCs from the patient are isolated, stimulated with TLR agonists and tumor antigens ex vivo and then infused back into the patient. Although some TLR ligands have been tested in clinical trials, novel TLR agonists with improved immunomodulatory properties are essential to optimize treatment success. We report on the discovery of small-molecule TLR2 agonists, with favorable properties as synthetic adjuvants...
July 19, 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/28734931/piperlongumine-inhibits-tgf-%C3%AE-induced-epithelial-to-mesenchymal-transition-by-modulating-the-expression-of-e-cadherin-snail1-and-twist1
#11
Min-Ju Park, Da-Eun Lee, Man Kyu Shim, Eun Hyang Jang, Jong Kil Lee, Seo Young Jeong, Jong-Ho Kim
Cancer is a life-threatening disease, and the occurrence of metastasis, which increases the lethality of primary tumors, is increasing. The epithelial-to-mesenchymal transition (EMT) is a biological process by which epithelial cells lose cell-cell adhesion properties and acquire mesenchymal properties, including motility and invasiveness. EMT is considered an early stage of metastasis; therefore, inhibiting EMT may be an effective anticancer therapy. In the present study, the antimetastatic effect of piperlongumine (PL) was assessed in human cancer cells...
July 19, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28734664/ph-responsive-biodegradable-nanogels-for-sustained-release-of-bleomycin
#12
Prashant Sahu, Sushil K Kashaw, Varun Kushwah, Samaresh Sau, Sanyog Jain, Arun K Iyer
Site specific drug delivery with desired therapeutic effect still remains challenging task due to suboptimal release, tissue toxicity, low selectivity and meager therapeutic efficacy in skin cancers. The aim of the current study was to fabricate pH responsive, self-assembled, chemically cross-linked biodegradable chitosan nanogel loaded with bleomycin to target the dermal area of the skin. The nanogel synthesized by ion gelation technique and was characterized for drug loading, swelling and thermal stability followed by in vitro analysis...
June 27, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28734206/theoretical-investigation-of-the-conformational-space-of-baicalin
#13
Juan J Martínez Medina, Evelina G Ferrer, Patricia A M Williams, Nora B Okulik
Flavonoids are a large group of polyphenolic compounds ubiquitously present in plants. They are important components of human diet. They are recognized as potential drug candidates to be used in the treatment and prevention of a lot of pathological disorders, due to their protective effects. Baicalin (7-glucuronic acid 5, 6-dihydroxyflavone) is one of the main single active constituents isolated from the dried roots of Scutellaria baicalensis Georgi. The great interest on this flavonoid is due to its various pharmacological properties, such as antioxidant, antimicrobial, anti-inflammatory, anticancer and so on, and its high accumulation in the roots of S...
July 11, 2017: Journal of Molecular Graphics & Modelling
https://www.readbyqxmd.com/read/28734166/naturally-occurring-immunomodulators-with-antitumor-activity-an-insight-on-their-mechanisms-of-action
#14
REVIEW
Shimaa Ibrahim Abdelmonym Mohamed, Ibrahim Jantan, Md Areeful Haque
Natural products with immunomodulatory activity are widely used in treatment of many diseases including autoimmune diseases, inflammatory disorders in addition to cancer. They gained a great interest in the last decades as therapeutic agents since they provide inexpensive and less toxic products than the synthetic chemotherapeutic agents. Immunomodulators are the agents that have the ability to boost or suppress the host defense response that can be used as a prophylaxis as well as in combination with other therapeutic modalities...
July 19, 2017: International Immunopharmacology
https://www.readbyqxmd.com/read/28734085/novel-menadione-hybrids-synthesis-anticancer-activity-and-cell-based-studies
#15
Chakka Vara Prasad, Vadithe Lakshma Nayak, Sistla Ramakrishna, Uppuluri Venkata Mallavadhani
A series of novel menadione based triazole hybrids were designed and synthesized by employing copper catalyzed azide-alkyne cycloaddition (CuAAC). All the synthesized hybrids were characterized by their spectral data ((1) H NMR, (13) C NMR, IR and HRMS). The synthesized compounds were evaluated for their anticancer activity against five selected cancer cell lines including lung (A549), prostate (DU-145), cervical (Hela), breast (MCF-7) and mouse melanoma (B-16) by using MTT assay. The screening results showed that majority of the synthesized compounds displayed significant anticancer activity...
July 22, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28734001/control-of-reversible-activation-dynamics-of-ru-%C3%AE-%C3%A2-%C3%AE%C2%BA%C3%A2-c%C3%A2-h%C3%A2-c%C3%A2-h%C3%A2-nh%C3%A2-xy-n-and-the-effect-of-chelate-ligand-variation
#16
Francisco Martínez-Peña, Ana M Pizarro
The potential use of organometallic ruthenium complexes as anticancer drugs is well known. Here we show a family of activatable tethered ruthenium(II) arene complexes of general formula [Ru(η⁶:κ¹-C₆H₅(C₆H₄)NH₂)(XY)]n+ (closed tether-ring) bearing different chelating XY ligands (XY = aliphatic diamine, phenylenediamine, oxalato, bis(phosphino)ethane). The activation of these complexes (closed-to-open tether conversion) occurs in methanol and dimethylsulfoxide at different rates, and to different reaction extents at equilibrium...
July 22, 2017: Chemistry: a European Journal
https://www.readbyqxmd.com/read/28733879/anticancer-activity-of-salicin-and-fenofibrate
#17
Marwa Sabaa, Hassan M ELFayoumi, Shimaa Elshazly, Mahmoud Youns, Waleed Barakat
Cancer refers to a disorder of cell proliferation that leads to tumor production. Cancer is usually treated by surgery, chemotherapeutic drugs, and radiation. Despite the presence of many anticancer drugs, cancer is still an uncontrolled disease and is a major cause of death worldwide. In addition, most anticancer drugs have severe side effects that can limit their use in some patients. This study aims to investigate the possible anticancer activity of two clinically used drugs: a natural antioxidant agent (salicin) and an antihyperlipidemic agent (fenofibrate) against two breast cancer models (in vivo EAC and in vitro MCF7) and the pancreatic cancer cell line (Panc-1)...
July 21, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28733703/induction-of-accelerated-senescence-by-the-microtubule-stabilizing-agent-peloruside-a
#18
Ariane Chan, Connie Gilfillan, Nikki Templeton, Ian Paterson, Peter T Northcote, John H Miller
Chemotherapeutic agents can induce accelerated senescence in tumor cells, an irreversible state of cell cycle arrest. Paclitaxel, a microtubule-stabilizing agent used to treat solid tumors of the breast, ovary, and lung and discodermolide, another stabilizing agent from a marine sponge, induce senescence in cultured cancer cells. The aim of this study was to determine if the microtubule-stabilizing agent peloruside A, a polyketide natural product from a marine sponge, can induce accelerated senescence in a breast cancer cell line MCF7...
July 22, 2017: Investigational New Drugs
https://www.readbyqxmd.com/read/28733545/a-small-molecule-inhibitor-targeting-the-aurkc-i%C3%AE%C2%BAb%C3%AE-interaction-decreases-transformed-growth-of-mda-mb-231-breast-cancer-cells
#19
Eun Hee Han, Jin-Young Min, Shin-Ae Yoo, Sung-Joon Park, Yun-Jeong Choe, Hee Sub Yun, Zee-Won Lee, Sun Woo Jin, Hyung Gyun Kim, Hye Gwang Jeong, Hyun Kyoung Kim, Nam Doo Kim, Young-Ho Chung
The Aurora kinases, Aurora A (AURKA), Aurora B (AURKB), and Aurora C (AURKC), are serine/threonine kinases required for the control of mitosis (AURKA and AURKB) or meiosis (AURKC). Several Aurora kinase inhibitors are being investigated as novel anticancer therapeutics. Recent studies demonstrated that AURKC activation contributes to breast cancer cell transformation. Therefore, AURKC is both a promising marker and therapeutic target for breast cancer; however, its signaling network has not been fully characterized...
June 29, 2017: Oncotarget
https://www.readbyqxmd.com/read/28733542/use-of-a-genome-wide-haploid-genetic-screen-to-identify-treatment-predicting-factors-a-proof-of-principle-study-in-pancreatic-cancer
#20
Yuk Ting Ma, Sarah M Leonard, Naheema Gordon, Jennifer Anderton, Claire James, David Huen, Ciaran B Woodman, Daniel H Palmer
The ability to develop a comprehensive panel of treatment predicting factors would significantly improve our ability to stratify patients for cytotoxic or targeted therapies, and prevent patients receiving ineffective treatments. We have investigated if a recently developed genome-wide haploid genetic screen can be used to reveal the critical mediators of response to anticancer therapy. Pancreatic cancer is known to be highly resistant to systemic therapy. Recently epigenetic changes have been shown to be a key determinant in the maintenance of subpopulations of cancer cells with high-level resistance to cytotoxic therapy...
June 29, 2017: Oncotarget
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