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https://www.readbyqxmd.com/read/28238876/ar-12-suppresses-dengue-virus-replication-by-down-regulation-of-pi3k-akt-and-grp78
#1
Hsin-Hsin Chen, Chien-Chin Chen, Yee-Shin Lin, Chiou-Feng Lin, Chia-Ling Chen, Chih-Peng Chang
Dengue virus (DENV) infection has become a public health issue of worldwide concern and is a serious health problem in Taiwan, yet there are no approved effective antiviral drugs to treat DENV. The replication of DENV requires both viral and cellular factors. Owing to the rapid mutation rate of viral factors, targeting host factors may serve as a more promising antiviral strategy. It has been known that up-regulation of PI3K/AKT signaling and GRP78 by DENV infection supports its replication. AR-12, a phase I trial completed anticancer drug, shows potent inhibitory activities on both PI3K/AKT signaling and GRP78 expression levels, and recently has been found to block the replication of several hemorrhagic fever viruses...
February 23, 2017: Antiviral Research
https://www.readbyqxmd.com/read/28238138/dual-wavelength-triggered-gold-nanorods-for-anticancer-treatment
#2
Dennis B Pacardo, Frances S Ligler, Zhen Gu
Gold nanomaterials with light-responsive properties can be exploited as light-triggered delivery vehicles to enhance the therapeutic efficacy of anticancer drugs. Additionally, different wavelengths of light can be utilized to achieve the combined effects of light-triggered release of therapeutics and light-induced localized heating, which results in improved anticancer efficacy. Herein, we describe methods to develop gold nanorod (AuNR) complexes that provide drug delivery or photothermal therapy when activated by ultraviolet (UV) or near-infrared (NIR) wavelengths of light, respectively...
2017: Methods in Molecular Biology
https://www.readbyqxmd.com/read/28237662/the-derivatives-of-pulsatilla-saponin-a-a-bioactive-compound-from-pulsatilla-chinensis-their-synthesis-cytotoxicity-haemolytic-toxicity-and-mechanism-of-action
#3
Xiaohang Tong, Li Han, Huaqing Duan, Yaru Cui, Yulin Feng, Yongming Zhu, Zhong Chen, Shilin Yang
The strong haemolytic toxicity of Pulsatilla saponin A (PSA) has hampered its clinical development as an injectable anticancer agent. To circumvent this challenge, twenty PSA derivatives with C ring or C-28 or C-3 modifications were synthesized and evaluated for cytotoxicity against seven selected human tumor lines, as well as for haemolytic toxicity. Structure-activity relationship (SAR) and structure-toxicity relationship (STR) correlations were also elucidated. Compared with PSA, compound 22 showed a better balance between haemolytic toxicity (HD50 > 500 μM) and cytotoxicity toward lung cancer cells A549 (IC50 = 4...
February 15, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28236767/triggering-autophagic-cell-death-with-a-di-manganese-ii-developmental-therapeutic
#4
Creina Slator, Zara Molphy, Vickie McKee, Andrew Kellett
There is an unmet need for novel metal-based chemotherapeutics with alternative modes of action compared to clinical agents such as cisplatin and metallo-bleomycin. Recent attention in this field has focused on designing intracellular ROS-mediators as powerful cytotoxins of human cancers and identifying potentially unique toxic mechanisms underpinning their utility. Herein, we report the developmental di-manganese(II) therapeutic [Mn2(μ-oda)(phen)4(H2O)2][Mn2(μ-oda)(phen)4(oda)2]·4H2O (Mn-Oda) induces autophagy-promoted apoptosis in human ovarian cancer cells (SKOV3)...
February 4, 2017: Redox Biology
https://www.readbyqxmd.com/read/28236692/synthesis-and-characterization-of-folate-decorated-albumin-bio-conjugate-nanoparticles-loaded-with-a-synthetic-curcumin-difluorinated-analogue
#5
Kaustubh A Gawde, Prashant Kesharwani, Samaresh Sau, Fazlul H Sarkar, Subhash Padhye, Sushil K Kashaw, Arun K Iyer
Albumin-bound paclitaxel colloidal nanoparticle (Abraxane®) is an FDA approved anticancer formulation available in the market. It is a suspension which is currently used therapeutically for treating cancers of the breast, lung, and pancreas among others. CDF is a novel new and potent synthetic curcumin analogue that is widely used for breast and ovarian cancer. The aim of this study was to use biocompatible albumin as well as folate decorated albumin to formulate colloidal nanoparticles encapsulating curcumin difluorinated (CDF)...
February 14, 2017: Journal of Colloid and Interface Science
https://www.readbyqxmd.com/read/28236621/proapoptotic-and-growth-inhibitory-effects-of-plumbagin-on-human-gastric-cancer-cells-via-suppression-of-signal-transducer-and-activator-of-transcription-3-and-protein-kinase-b
#6
Jing Li, Jia Li, Guowei Cai, Lin Shen, Furong Lu
Context • Gastric cancer (GC) is the fourth most common cancer and the second leading cause of cancer-related deaths in the world. The current treatments include surgery and chemotherapy, either alone or in combination with radiotherapy, but the prognosis for patients with GC is usually poor. A safe and effective chemopreventive treatment for this malignant disease is urgently needed. Objective • The study intended to investigate the effects and underlying mechanisms of plumbagin, a quinonoid constituent that is derived from the roots of the medicinal plant Plumbago zeylanica, which exhibits potent anticancer properties against a number of cancers...
February 27, 2017: Alternative Therapies in Health and Medicine
https://www.readbyqxmd.com/read/28236592/novel-conjugates-of-endoperoxide-and-4-anilinoquinazoline-as-potential-anticancer-agents
#7
Jing Yang, Zhengchao Tu, Xin Xu, Jinfeng Luo, Xing Yan, Chongzhao Ran, Xinliang Mao, Ke Ding, Chunhua Qiao
In the present study, endoperoxide and 4-anilinoqnazoline were conjugated to obtain a series of compounds. These conjugates exhibited high antiproliferative potency against a number of cancer cell lines, including the epidermal growth factor receptor (EGFR) L858R/T790M mutant cell. Compound 5 was selected as a representative for mechanistic study. Further experiments revealed the conjugate's reactive oxygen species (ROS) generating ability, apoptosis inducing activity and involvement in EGFR downstream signaling pathways...
February 13, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28236409/new-arbutin-derivatives-from-the-leaves-of-heliciopsis-lobata-with-cytotoxicity
#8
Wei-Yan Qi, Na Ou, Xiao-Dong Wu, Han-Mei Xu
Heliciopsis lobata is a medicinal plant, which is exclusively used to treat tumor in Li folk region. Two new arbutin derivatives, 6'-((E)2-methoxy-5-hydroxycinnamoyl) arbutin (1) and 2'-((E)2, 5-dihydroxycinnamoyl) arbutin (2) along with five known compounds (3-7), were isolated from the leaves of Heliciopsis lobata. Their structures were elucidated on the basis of extensive spectroscopic interpretations. They were evaluated for their potential anticancer activity. Compounds 6 and 7 exhibited cytotoxicity against MGC-803 cells with IC50 values being 44...
October 2016: Chinese Journal of Natural Medicines
https://www.readbyqxmd.com/read/28236195/induction-of-apoptosis-in-human-cancer-cells-through-extrinsic-and-intrinsic-pathways-by-balanites-aegyptiaca-furostanol-saponins-and-saponin-coated-silvernanoparticles
#9
Abdelrahman M Yassin, Nehal M El-Deeb, Ahmed M Metwaly, Gomaa F El Fawal, Mohamed M Radwan, Elsayed E Hafez
The aim of this investigation is to examine the anticancer activities of Balanites aegyptiaca fruit extract with its biogenic silver nanoparticles (AgNPs) against colon and liver cancer cells. B. aegyptiaca aqueous extract was fractionated according to polarity and by biosynthesized AgNP. The cytotoxicity of the extract, semi-purified fractions, and the AgNPs was examined on noncancerous cell lines. The safer fraction was subjected to ultra-performance liquid chromatography-MS to identify the major active constituents...
February 24, 2017: Applied Biochemistry and Biotechnology
https://www.readbyqxmd.com/read/28235989/bacillus-thuringiensis-a-successful-insecticide-with-new-environmental-features-and-tidings
#10
REVIEW
Gholamreza Salehi Jouzani, Elena Valijanian, Reza Sharafi
Bacillus thuringiensis (Bt) is known as the most successful microbial insecticide against different orders of insect pests in agriculture and medicine. Moreover, Bt toxin genes also have been efficiently used to enhance resistance to insect pests in genetically modified crops. In light of the scientific advantages of new molecular biology technologies, recently, some other new potentials of Bt have been explored. These new environmental features include the toxicity against nematodes, mites, and ticks, antagonistic effects against plant and animal pathogenic bacteria and fungi, plant growth-promoting activities (PGPR), bioremediation of different heavy metals and other pollutants, biosynthesis of metal nanoparticles, production of polyhydroxyalkanoate biopolymer, and anticancer activities (due to parasporins)...
February 24, 2017: Applied Microbiology and Biotechnology
https://www.readbyqxmd.com/read/28235701/design-synthesis-and-biological-evaluation-of-imidazo-1-2-b-pyridazine-derivatives-as-mtor-inhibitors
#11
Beibei Mao, Shanyun Gao, Yiran Weng, Liangren Zhang, Lihe Zhang
ATP-competitive mTOR inhibitors have been studied as potential antitumor agents. Based on the structure-activity relationship of known mTOR inhibitors, a series of novel imidazo[1,2-b]pyridazine derivatives were synthesized and characterized. The anti-proliferative activities of these compounds were evaluated by SRB assay against six human cancer cell lines. Imidazo[1,2-b]pyridazine diaryl urea derivatives A15-A24 exhibited significant anti-proliferative activity especially against non-small cell lung cancer A549 and H460 with IC50 values ranging from 0...
February 9, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28235687/immodin-and-its-immune-system-supportive-role-in-paclitaxel-therapy-of-4t1-mouse-breast-cancer
#12
Vlasta Demečková, Peter Solár, Gabriela Hrčková, Dagmar Mudroňová, Bianka Bojková, Monika Kassayová, Soňa Gancarčiková
It is evident that standard chemotherapy agents may have an impact on both tumor and host immune system. Paclitaxel (PTX), a very potent anticancer drug from a taxane family, has achieved prominence in clinical oncology for its efficacy against a wide range of tumors including breast cancer. However, significant toxicity, such as myelosuppression, limit the effectiveness of Paclitaxel-based treatment regimens. Immodin (IM) is low molecular dialysate fraction of homogenate made from human leukocytes. It contains a mixture of substances from which so far have been described e...
February 21, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28235427/efficient-t3p-%C3%A2-mediated-synthesis-differential-cytotoxicity-and-apoptosis-induction-by-indolo-triazolo-thiadiazoles-in-human-breast-adenocarcinoma-cells
#13
Pooja R Kamath, Dhanya Sunil, Shubhankar Das, Abdul A Ajees, B S Satish Rao
The limited efficacy of marketed anticancer agents demands the design of novel target-specific hybrid molecules incorporating multiple bioactive pharmacores to combat cancer. In the present study, a one-pot simple and efficient T3P(®) mediated procedure for the preparation of twelve new 3-(substituted- [1,2,4]triazolo[3,4-b] [1,3,4]thiadiazolo)-1H-indoles with short reaction times, easy workup procedure, good yields, and purity of products is described. Cytotoxicity assay (MTT), flow-cytometric univariate cell cycle analysis, Annexin V-FITC staining and DNA fragmentation for cell death mechanism suggested that compound 3d with chloro-substituted phenyl ring induced enhanced cytotoxicity by an apoptotic pathway with high differential toxicity to breast adenocarcinoma cells (MCF-7) when compared with normal human dermal fibroblast cells...
February 21, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/28231533/synthesis-characterization-and-dna-binding-cleavage-protein-binding-and-cytotoxicity-studies-of-co-ii-ni-ii-cu-ii-and-zn-ii-complexes-of-aminonaphthoquinone
#14
A Kosiha, C Parthiban, Kuppanagounder P Elango
The Co(II), Ni(II), Cu(II) and Zn(II) complexes of an aminonaphthoquinone ligand (L) have been prepared and characterized using analytical and spectral techniques. The structures of L and its Zn(II) complex are confirmed by single crystal X-ray diffraction study. The results indicate that Co(II), Ni(II) and Zn(II) complexes possess tetrahedral geometry while Cu(II) complex exhibits square planar structure. The interaction of L and its complexes with CT-DNA reveal that they could interact with CT-DNA through intercalation...
February 16, 2017: Journal of Photochemistry and Photobiology. B, Biology
https://www.readbyqxmd.com/read/28231500/silver-nanoparticle-embedded-graphene-oxide-methotrexate-for-targeted-cancer-treatment
#15
Raj Kumar Thapa, Jae Hee Kim, Jee-Heon Jeong, Beom Soo Shin, Han-Gon Choi, Chul Soon Yong, Jong Oh Kim
Combination therapies are widely investigated cancer treatment modalities. Carbon based systems such as graphene oxide (GO), plasmonic nanoparticles such as silver nanoparticles (AgNPs), and the folate analog, methotrexate (MTX), have been separately studied for their potential anticancer effects. In this study, we combined these systems to develop AgNPs-embedded GO with conjugated MTX (MTX-GO/AgNPs) and studied their folate receptor-targeted anticancer effects. Results revealed successful formation of AgNPs on GO along with MTX conjugation as suggested by UV/visible, TEM, AFM, FTIR, and XRD analysis...
February 13, 2017: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/28231175/mushroom-polysaccharides-chemistry-and-antiobesity-antidiabetes-anticancer-and-antibiotic-properties-in-cells-rodents-and-humans
#16
REVIEW
Mendel Friedman
More than 2000 species of edible and/or medicinal mushrooms have been identified to date, many of which are widely consumed, stimulating much research on their health-promoting properties. These properties are associated with bioactive compounds produced by the mushrooms, including polysaccharides. Although β-glucans (homopolysaccharides) are believed to be the major bioactive polysaccharides of mushrooms, other types of mushroom polysaccharides (heteropolysaccharides) also possess biological properties. Here we survey the chemistry of such health-promoting polysaccharides and their reported antiobesity and antidiabetic properties as well as selected anticarcinogenic, antimicrobial, and antiviral effects that demonstrate their multiple health-promoting potential...
November 29, 2016: Foods (Basel, Switzerland)
https://www.readbyqxmd.com/read/28230972/paclitaxel-biosynthesis-adenylation-and-thiolation-domains-of-an-nrps-tyca-pheat-module-produce-various-arylisoserine-coa-thioesters
#17
Ruth Muchiri, Kevin D Walker
Structure-activity relationship studies show that the phenylisoserinyl moiety of paclitaxel is largely necessary for the effective anticancer activity. Several paclitaxel analogs with a variant isoserinyl sides chain have improved pharmaceutical properties over the parent drug. To produce the isoserinyl CoAs as intermediates needed for enzyme catalysis on a semibiosynthetic pathway to paclitaxel analogs, we repurposed the adenylation and thiolation domains of a non-ribosomal peptide synthetase (Phe-AT) to function as a CoA ligase...
February 23, 2017: Biochemistry
https://www.readbyqxmd.com/read/28230866/oridonin-induces-autophagy-via-inhibition-of-glucose-metabolism-in-p53-mutated-colorectal-cancer-cells
#18
Zhuo Yao, Fuhua Xie, Min Li, Zirui Liang, Wenli Xu, Jianhua Yang, Chang Liu, Hongwangwang Li, Hui Zhou, Liang-Hu Qu
The Warburg effect is an important characteristic of tumor cells, making it an attractive therapeutic target. Current anticancer drug development strategies predominantly focus on inhibitors of the specific molecular effectors involved in tumor cell proliferation. These drugs or natural compounds, many of which target the Warburg effect and the underlying mechanisms, still need to be characterized. To elucidate the anticancer effects of a natural diterpenoid, oridonin, we first demonstrated the anticancer activity of oridonin both in vitro and in vivo in colorectal cancer (CRC) cells...
February 23, 2017: Cell Death & Disease
https://www.readbyqxmd.com/read/28230855/simvastatin-induced-cell-cycle-arrest-through-inhibition-of-stat3-skp2-axis-and-activation-of-ampk-to-promote-p27-and-p21-accumulation-in-hepatocellular-carcinoma-cells
#19
Sin-Ting Wang, Hsiu J Ho, Jaw-Town Lin, Jeng-Jer Shieh, Chun-Ying Wu
Hepatocellular carcinoma (HCC) is characterized by a poor prognosis and is one of the leading causes of cancer-related death worldwide. Simvastatin, an HMG-CoA reductase inhibitor, which decreases cholesterol synthesis by inhibiting mevalonate pathways and is widely used to treat cardiovascular diseases. Simvastatin exhibits anticancer effects against several malignancies. However, the molecular mechanisms underlying the anticancer effects of simvastatin on HCC are still not well understood. In this study, we demonstrated simvastatin-induced G0/G1 arrest by inducing p21 and p27 accumulation in HepG2 and Hep3B cells...
February 23, 2017: Cell Death & Disease
https://www.readbyqxmd.com/read/28229436/purification-and-characterization-of-a-novel-ubiquitin-like-antitumour-protein-with-hemagglutinating-and-deoxyribonuclease-activities-from-the-edible-mushroom-ramaria-botrytis
#20
Rong Zhou, Ya-Jie Han, Min-Hui Zhang, Ke-Ren Zhang, Tzi Bun Ng, Fang Liu
A novel ubiquitin-like antitumour protein (RBUP) was isolated from fruiting bodies of the edible mushroom Ramaria botrytis. The protein was isolated with a purification protocol involving ion exchange chromatography on DEAE-Sepharose fast flow and gel filtration on Sephadex G-75. SDS-PAGE, Native-PAGE and ultracentrifugation analysis disclosed that RBUP was a monomeric protein with a molecular weight of 18.5 kDa. ESI-MS/MS demonstrated that it shared 69% amino acid sequence similarity with Coprinellus congregates ubiquitin (gi|136667)...
December 2017: AMB Express
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