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https://www.readbyqxmd.com/read/29223927/biochemical-characterization-of-the-ybpci-miniprotein-the-first-carboxypeptidase-inhibitor-isolated-from-yellow-bell-pepper-capsicum-annuum-l-a-novel-contribution-to-the-knowledge-of-miniproteins-stability
#1
Juliana Cotabarren, Mariana Edith Tellechea, Francesc Xavier Avilés, Julia Lorenzo, Walter David Obregón
The cystine-knot metallocarboxypeptidase inhibitors (MCPIs) are peptides that contribute to control proteolytic activity, involved in storage, growth and maintenance of plants. Lately studies reported several MCPIs with potential use in biomedical applications; as anti-cancer, anti-thrombotic, anti-malaric and anti-angiogenic agents. We report the isolation, purification, chemical stability and biochemical characterization of a novel carboxypeptidase A inhibitor (YBPCI) isolated from Capsicum annuum L. var...
December 6, 2017: Protein Expression and Purification
https://www.readbyqxmd.com/read/29223554/oral-administration-of-nigella-sativa-oil-and-thymoquinone-attenuates-long-term-cisplatin-treatment-induced-toxicity-and-oxidative-damage-in-rat-kidney
#2
Zeba Farooqui, Faaiza Shahid, Aijaz Ahmed Khan, Farah Khan
Cisplatin (CP) is an effective anti-cancer drug which causes remarkable toxicity to the kidney, particularly to proximal tubules, by generating reactive oxygen species. Nigella sativa (NS), commonly known as "black cumin" reduces the progression of various kidney disorders. Thymoquinone (TQ), the major bioactive constituent of NS seeds, has been credited for various pharmacological effects of NS. Since, a typical clinical CP dosing regimen involves CP administration in multiple cycles over a long time duration, hence the present study aimed to evaluate the renoprotective efficacy of NS oil and TQ against multiple dose CP treatment induced deleterious biochemical and histological alterations in rat kidney...
December 6, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29223538/curcumin-induces-osteoblast-differentiation-through-mild-endoplasmic-reticulum-stress-mediated-such-as-bmp2-on-osteoblast-cells
#3
Hyo-Eun Son, Eun-Jung Kim, Won-Gu Jang
AIMS: Curcumin (diferuloylmethane or [1E,6E]-1,7-bis[4-hydroxy-3-methoxyphenyl]-1,6heptadiene-3,5-dione) is a phenolic natural product derived from the rhizomes of the turmeric plant, Curcuma longa. It is reported to have various biological actions such as anti-oxidative, anti-inflammatory, and anti-cancer effects. However, the molecular mechanism of osteoblast differentiation by curcumin has not yet been reported. MAIN METHODS: The cytotoxicity of curcumin was identified using the 3-(4,5-dimethylthiazol-2yl)-2,5-diphenyltetrazolium bromide (MTT) assay...
December 6, 2017: Life Sciences
https://www.readbyqxmd.com/read/29222980/bonding-of-doxorubicin-to-nanosilica-and-human-serum-albumin-in-various-media
#4
V M Gun'ko, T V Krupska, L S Andriyko, N Yu Klymenko, I V Siora, O A Novikova, A I Marynin, A I Ukrainets, B Charmas, S B Shekhunova, V V Turov
Interaction of doxorubicin hydrochloride (DOX) (anti-cancer drug) with hydro-compacted nanosilica A-300 (cA-300) alone or cA-300/human serum albumin (HSA) at a small content of water (h = 0.4 g per gram of dry silica) in different dispersion media (air, chloroform, and chloroform/trifluoroacetic acid) was analyzed using low-temperature 1H NMR spectroscopy, NMR cryoporometry and quantum chemistry to elucidate specific changes in the interfacial layers. Initial (bulk density ρb ≈ 0.046 g/cm3) and hydro-compacted (ρb ≈ 0...
December 5, 2017: Journal of Colloid and Interface Science
https://www.readbyqxmd.com/read/29222400/nkg2d-based-car-t-cells-and-radiotherapy-exert-synergistic-efficacy-in-glioblastoma
#5
Tobias Weiss, Michael Weller, Matthias Guckenberger, Charles L Sentman, Patrick Roth
Chimeric antigen receptor (CAR) T cell therapy is an emerging immunotherapy against several malignancies including glioblastoma, the most common and most aggressive malignant primary brain tumor in adults. The challenges in solid tumor immunotherapy comprise heterogenously expressed tumor target antigens and restricted trafficking of CAR T cells to and impaired long-term persistence at the tumor site, as well as the unaddressed integration of CAR T cell therapy into conventional anti-cancer treatments. We addressed these questions using a NKG2D-based chimeric antigen receptor construct (chNKG2D) in fully immunocompetent orthotopic glioblastoma mouse models...
December 8, 2017: Cancer Research
https://www.readbyqxmd.com/read/29222039/the-role-of-stat3-in-leading-the-crosstalk-between-human-cancers-and-the-immune-system
#6
Yu Wang, Yicheng Shen, Sinan Wang, Qiang Shen, Xuan Zhou
The development and progression of human cancers are continuously and dynamically regulated by intrinsic and extrinsic factors. As a converging point of multiple oncogenic pathways, signal transducer and activator of transcription 3 (STAT3) is constitutively activated both in tumor cells and tumor-infiltrated immune cells. Activated STAT3 persistently triggers tumor progression through direct regulation of oncogenic gene expression. Apart from its oncogenic role in regulating gene expression in tumor cells, STAT3 also paves the way for human cancer growth through immunosuppression...
December 5, 2017: Cancer Letters
https://www.readbyqxmd.com/read/29221949/anti-cancer-activity-of-a-new-dihydropyridine-derivative-vdie-2n-in-head-and-neck-squamous-cell-carcinoma
#7
Renata Nishida Goto, Lays Martin Sobral, Lucas Oliveira Sousa, Cristiana Bernadelli Garcia, Norberto Peporine Lopes, Javier Marín-Prida, Estael Ochoa-Rodríguez, Yamila Verdecia-Reyes, Gilberto Lázaro Pardo-Andreu, Carlos Curti, Andréia Machado Leopoldino
This study aims to examine the effects of a new 1,4-dihydropyridine derivative, VdiE-2N, on cell signaling pathways and mitochondrial events in head and neck squamous cell carcinoma (HNSCC) cells, and on a mice model of xenograft tumor growth/cell proliferation. Four HNSCC cell lines (HN13, HN12, HN6, and CAL27), HEK293 cells (human embryonic kidney 293 cells), and human oral healthy mucosa fibroblasts (OHMF) were used for in vitro assessment of cell viability (resazurin assay) and invasion capacity (modified Boyden chamber assay), and mitochondrial membrane potential (JC-1 fluorescence assay), morphology (transmission electron microscopy), and number of mitochondria (MitoTracker® imaging)...
December 5, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/29221287/anti-cancer-activity-of-dose-fractioned-mpe-bevacizumab-regimen-is-paralleled-by-immune-modulation-in-advanced-squamous-nslc-patients
#8
Pierpaolo Pastina, Valerio Nardone, Stefania Croci, Giuseppe Battaglia, Francesca Vanni, Cristiana Bellan, Marcella Barbarino, Veronica Ricci, Susan Costantini, Francesca Capone, Cirino Botta, Mayra Rachele Zarone, Gabriella Misso, Mariarosaria Boccellino, Michele Caraglia, Antonio Giordano, Piero Paladini, Pierfrancesco Tassone, Pierosandro Tagliaferri, Maria Grazia Cusi, Luigi Pirtoli, Pierpaolo Correale
Background: Results from the BEVA2007 trial, suggest that the metronomic chemotherapy regimen with dose-fractioned cisplatin and oral etoposide (mPE) +/- bevacizumab, a monoclonal antibody to the vascular endothelial growth factor (VEGF), shows anti-angiogenic and immunological effects and is a safe and active treatment for metastatic non-small cell lung cancer (mNSCLC) patients. We carried out a retrospective analysis aimed to evaluate the antitumor effects of this treatment in a subset of patients with squamous histology...
September 2017: Journal of Thoracic Disease
https://www.readbyqxmd.com/read/29221189/novel-direct-ampk-activator-suppresses-non-small-cell-lung-cancer-through-inhibition-of-lipid-metabolism
#9
Xi Chen, Chun Xie, Xing-Xing Fan, Ze-Bo Jiang, Vincent Kam-Wai Wong, Jia-Hui Xu, Xiao-Jun Yao, Liang Liu, Elaine Lai-Han Leung
Drug resistance is becoming an obstacle in anti-cancer therapies. For target-based therapy of lung cancer, gefitinib, as the first generation of tyrosine kinase inhibitors (TKIs), demonstrated good initial response to the non-small cell lung cancer (NSCLC) patients whom harbors epidermal growth factor receptor (EGFR) mutation. However, within one year, additional EGFR mutation occurred, leading to eventual gefitinib-resistance. Therefore, it is urgently to discover novel effective small molecule inhibitors for those patients...
November 10, 2017: Oncotarget
https://www.readbyqxmd.com/read/29221182/differential-modulation-of-bax-bcl-2-ratio-and-onset-of-caspase-3-7-activation-induced-by-derivatives-of-justicidin-b-in-human-melanoma-cells-a375
#10
Aljawharah Al-Qathama, Simon Gibbons, Jose M Prieto
Diphyllin and its derivatives are well known cytotoxic natural products structurally related to the anti-cancer drug podophyllotoxin. We here study their structure-activity relationship upon human melanoma cells for first time. To this end, human melanoma A375 cells were incubated with Justicidin B and its 4-methoxylated or 4-glycosylated derivatives to evaluate their selective cytotoxicity and study their effects on cell cycle distribution, caspase activation, apoptosis induction using Annexin V-FITC/PI staining, cell morphology and western blot analysis...
November 10, 2017: Oncotarget
https://www.readbyqxmd.com/read/29221173/farnesyl-phenolic-enantiomers-as-natural-mth1-inhibitors-from-ganoderma-sinense
#11
Ya Gao, Lihan Zhu, Jing Guo, Ting Yuan, Liqing Wang, Hua Li, Lixia Chen
Cancer cells are more addictive to MTH1 than normal cells because of their dysfunctional redox regulations. MTH1 plays an important role to maintain tumor cell survival, while it is not indispensable for the growth of normal cells. Farnesyl phenols having a coumaroyl substitution are rather uncommon in nature. Eight farnesyl phenolic compounds with such substituent moiety (1-8), including six new ones, ganosinensols E-J (1-6) were isolated from the 95% EtOH extract of the fruiting bodies of Ganoderma sinense...
November 10, 2017: Oncotarget
https://www.readbyqxmd.com/read/29220692/plag-alleviates-chemotherapy-induced-thrombocytopenia-via-promotion-of-megakaryocyte-erythrocyte-progenitor-differentiation-in-mice
#12
Ha-Reum Lee, Nina Yoo, Jinseon Jeong, Ki-Young Sohn, Sun Young Yoon, Jae Wha Kim
Previously, PLAG (1-palmitoyl-2-linoleoyl-3-acetyl-rac-glycerol, acetylated diglyceride) was reported to have an effect on the proliferation of hematopoietic stem cells (HSCs) or to contribute to the prevention of chemotherapy-induced neutropenia. In this study, we examined the role of PLAG in the differentiation of bone marrow cells from HSCs into progenitor cells in mice. After 15days, the lineage-negative cells, especially megakaryocyte/erythrocyte progenitors (MEP), were significantly increased in mice that received daily PLAG administration compared to those in the untreated mice...
October 10, 2017: Thrombosis Research
https://www.readbyqxmd.com/read/29220397/desethylamiodarone-a-metabolite-of-amiodarone-induces-apoptosis-on-t24-human-bladder-cancer-cells-via-multiple-pathways
#13
Zita Bognar, Katalin Fekete, Csenge Antus, Eniko Hocsak, Rita Bognar, Antal Tapodi, Arpad Boronkai, Nelli Farkas, Ferenc Gallyas, Balazs Sumegi, Arpad Szanto
Bladder cancer (BC) is a common malignancy of the urinary tract that has a higher frequency in men than in women. Cytostatic resistance and metastasis formation are significant risk factors in BC therapy; therefore, there is great interest in overcoming drug resistance and in initiating research for novel chemotherapeutic approaches. Here, we suggest that desethylamiodarone (DEA)-a metabolite of amiodarone-may have cytostatic potential. DEA activates the collapse of mitochondrial membrane potential (detected by JC-1 fluorescence), and induces cell death in T24 human transitional-cell bladder carcinoma cell line at physiologically achievable concentrations...
2017: PloS One
https://www.readbyqxmd.com/read/29220106/chemoprevention-by-resveratrol-and-pterostilbene-targeting-on-epigenetic-regulation
#14
REVIEW
Pei-Sheng Lee, Yi-Shiou Chiou, Chi-Tang Ho, Min-Hsiung Pan
Epigenetic mechanisms are essential in regulating normal cellular functions and play an important role during the disease developmental stages. However, aberrant epigenetic mechanisms may lead to pathological consequences such as cancer, neurological disorders, bone and skeletal diseases, cardiovascular dysfunction, and metabolic syndrome. The molecular mechanisms of epigenetic modification include DNA methylation, histone modification (acetylation, methylation and phosphorylation), and microRNAs (miRNAs). Unlike genetic modifications, epigenetic states of genes are reversible and can be altered by certain intrinsic and extrinsic factors...
December 8, 2017: BioFactors
https://www.readbyqxmd.com/read/29219656/modulating-secreted-components-of-tumor-microenvironment-a-masterstroke-in-tumor-therapeutics
#15
Himadri Patel, Pritish Nilendu, Devashree Jahagirdar, Jayanta K Pal, Nilesh Kumar Sharma
The microenvironment in which cancer resides plays an important role in regulating cancer survival, progression, malignancy and drug resistance. Tumor microenvironment (TME) consists of heterogeneous number and types of cellular and non-cellular components that vary in relation to tumor phenotype and genotype. In recent, non-cellular secreted components of microenvironmental heterogeneity have been suggested to contain various growth factors, cytokines, RNA, DNA, metabolites, structural matrix and matricellular proteins...
December 8, 2017: Cancer Biology & Therapy
https://www.readbyqxmd.com/read/29218506/in-silico-discovery-of-novel-ligands-for-antimicrobial-lipopeptides-for-computer-aided-drug-design
#16
REVIEW
Satya Eswari Jujjavarapu, Swasti Dhagat
The increase in antibiotic-resistant strains of pathogens has created havoc worldwide. These antibiotic-resistant pathogens require potent drugs for their inhibition. Lipopeptides, which are produced as secondary metabolites by many microorganisms, have the ability to act as potent safe drugs. Lipopeptides are amphiphilic molecules containing a lipid chain bound to the peptide. They exhibit broad-spectrum activities against both bacteria and fungi. Other than their antimicrobial properties, they have displayed anti-cancer properties as well, but their mechanism of action is not understood...
December 7, 2017: Probiotics and Antimicrobial Proteins
https://www.readbyqxmd.com/read/29218107/scutellarin-suppresses-human-colorectal-cancer-metastasis-and-angiogenesis-by-targeting-ephrinb2
#17
Ping Ting Zhu, Ming Mao, Zhao Guo Liu, Li Tao, Bing Chun Yan
Tumor induced angiogenesis is an attractive target for anti-cancer drug treatment. Scutellarin, which is a native compound derived from scutellaria altissima leaves, has already been proved to possess anti-tumor activities. Nevertheless, their effects in colorectal cancer metastasis and angiogenesis have not been evaluated. In order to reveal the anti-angiogenic and anti-metastasis capacity of scutellarin, wound healing and Transwell chamber inserts invasion were done in colorectal cancer cells, and cell proliferation as wells colony formation were conducted to identify the proliferation inhibition of colorectal cancer in vitro...
2017: American Journal of Translational Research
https://www.readbyqxmd.com/read/29217339/standardization-chemical-profiling-in%C3%A2-vitro-cytotoxic-effects-in%C3%A2-vivo-anti-carcinogenic-potential-and-biosafety-profile-of-indian-propolis
#18
Harshad Kapare, Sathiyanarayanan Lohidasan, Arulmozhi Sinnathambi, Kakasaheb Mahadik
BACKGROUND: Propolis from apiculture is known for wide range of medicinal properties owing to its vast chemical constituents including polyphenols, flavonoids and anticancer agent Caffeic acid phenethyl ester (CAPE). OBJECTIVES: The objective of the study was to extract and standardize Indian propolis (IP) with respect to selected markers by newly developed High performance liquid chromatography (HPLC) method, to evaluate in vitro and in vivo anticancer activity and biosafety of Indian propolis...
December 4, 2017: Journal of Ayurveda and Integrative Medicine
https://www.readbyqxmd.com/read/29216717/assembly-of-high-potency-photosensitiser-antibody-conjugates-through-application-of-dendron-multiplier-technology
#19
Vijay Chudasama, Francesca Bryden, Huguette Savoie, Antoine Maruani, Miffy Cheng, Andrew Beeby, Joao Rodrigues, Ross W Boyle
Exploitation of photosensitisers as payloads for antibody-based anti-cancer therapeutics offers a novel alternative to the small pool of commonly-utilised cytotoxins. However, existing bioconjugation methodologies are incompatible with the requirement of increased antibody loading without compromising antibody function, stability or homogeneity. Herein, we describe the first application of dendritic multiplier groups to allow the loading of more than 4 porphyrins to a full IgG antibody in a site-specific and highly homogeneous manner...
December 7, 2017: Bioconjugate Chemistry
https://www.readbyqxmd.com/read/29216716/cyclodipeptide-c-orn-pro-conjugate-with-4-ethylpiperic-acid-epa-abrogates-cancer-cells-metastasis-through-modulating-mdm2
#20
Sudha Shankar, Mir Mohd Faheem, Debasis Nayak, Naiem Ahmad Wani, Saleem Farooq, Surrinder Koul, Anindya Goswami, Rajkishor Rai
The present work describes the synthesis, characterization and anticancer properties of c(Lys-Pro), P1; c(Orn-Pro), P2 and conjugates PA-c(Lys-Pro), C1; PA-c(Orn-Pro), C2; EPA-c(Lys-Pro), C3 and EPA-c(Orn-Pro), C4. Among all, conjugate C4 displays potent anti-cancer activity with IC50 1.3μM in MDA-MB-231, 3.5 µM in PC-3, 8.9μM in MCF-7 and 9.6 μM in Miapaca-2 cancer cells. In addition, C4 down regulates the expression of MDM2 and abrogates the cancer cell invasion/metastasis. Through knock-down MDM2, we demonstrate that this abrogation of metastasis by C4 is primarily MDM2 dependent...
December 7, 2017: Bioconjugate Chemistry
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