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https://www.readbyqxmd.com/read/30342308/synthesis-characterization-and-unravelling-the-molecular-interaction-of-new-bioactive-4-hydroxycoumarin-derivative-with-biopolymer-insights-from-spectroscopic-and-theoretical-aspect
#1
Abhijit Mukherjee, Suvranil Ghosh, Rudraditya Sarkar, Satyajit Samanta, Sudipta Ghosh, Mahadeb Pal, Adinath Majee, Sukanta Kumar Sen, Bula Singh
In the progress of small molecule as drug candidates, 4-hydroxycoumarin based compounds bearing a crucial place as potent antibiotic agents with appreciable safety in drug invention. Being synthetically and easily obtainable, 4-hydroxycoumarin related compounds with planar structure have been promoted predominantly as DNA targeting agent. Nevertheless, here we elucidate the synthesis, characterization and theoretical study of bio-active small molecule 4-hydroxy-3,4'-bichromenyl-2,2'-dione (4HBD). Then we have illuminated the binding interactions of 4HBD with calf thymus DNA (ctDNA), which is particularly designed for biological application...
October 13, 2018: Journal of Photochemistry and Photobiology. B, Biology
https://www.readbyqxmd.com/read/30342177/n-myristoyltransferases-inhibitory-activity-of-ellagitannins-from-terminalia-bentzo%C3%A3-l-l-f-subsp-bentzo%C3%A3
#2
Cécile Apel, Jérôme Bignon, Maria Conception García Alvarez, Sarah Ciccone, Patricia Clerc, Isabelle Grondin, Emmanuelle Girard-Valenciennes, Jacqueline Smadja, Philippe Lopes, Michel Frederich, Fanny Roussi, Thierry Meinnel, Carmela Giglione, Marc Litaudon
N-myristoylation (Myr) is an eukaryotic N-terminal co- or post-translational protein modification in which the enzyme N-myristoyltransferase (NMT) transfers a fatty acid (C14:0) to the N-terminal glycine residues of several cellular key proteins. Depending on the cellular context, NMT may serve as a molecular target in anticancer or anti-infectious therapy, and drugs that inhibit this enzyme may be useful in the treatment of cancer or infectious diseases. As part of an on-going project to identify natural Homo sapiens N-myristoyltransferase 1 inhibitors (HsNMT1), two ellagitannins, punicalagin (1) and isoterchebulin (2), along with eschweilenol C (3) and ellagic acid (4) were isolated from the bark of Terminalia bentzoë (L...
October 17, 2018: Fitoterapia
https://www.readbyqxmd.com/read/30342059/role-of-zip8-in-regulation-of-cisplatin-sensitivity-through-bcl-2
#3
Xiangrong Geng, Liu Liu, Kan-Jen Tsai, Zijuan Liu
ZIP8 is a membrane transporter that facilitates the uptake of divalent metals (e.g., Zn, Mn, Fe, Cd) and the mineral selenite in anionic form. ZIP8 functionality has been recently reported to regulate cell proliferation, migration and cytoskeleton arrangement, exhibiting an essential role for normal physiology. In this study, we report a ZIP8 role in chemotherapy response. We show ZIP8 regulates cell sensitivity to the anti-cancer drug cisplatin. Overexpression of ZIP8 in mouse embryonic fibroblast (MEF) cells induces cisplatin sensitivity, while knockout of ZIP8 in leukemia HAP1 cells leads to cisplatin resistance...
October 17, 2018: Toxicology and Applied Pharmacology
https://www.readbyqxmd.com/read/30342024/cxcr4-targeting-nanobodies-differentially-inhibit-cxcr4-function-and-hiv-entry
#4
Anneleen Van Hout, Alex Klarenbeek, Vladimir Bobkov, Jordi Doijen, Marta Arimont, Chunxia Zhao, Raimond Heukers, Rebecca Rimkunas, Chris de Graaf, Theo Verrips, Bas van der Woning, Hans de Haard, Joseph B Rucker, Kurt Vermeire, Tracy Handel, Tom Van Loy, Martine J Smit, Dominique Schols
The chemokine receptor CXCR4 and its ligand CXCL12 contribute to a variety of human diseases, such as cancer. CXCR4 is also a major co-receptor facilitating HIV entry. Accordingly, CXCR4 is considered as an attractive therapeutic target. Drug side effects and poor pharmacokinetic properties have been major hurdles that have prevented the implementation of CXCR4-directed inhibitors in treatment regimes. We evaluated the activity of a new and promising class of biologics, namely CXCR4-targeting nanobodies, with the purpose of identifying nanobodies that would preferentially inhibit HIV infection, while minimally disturbing other CXCR4-related functions...
October 17, 2018: Biochemical Pharmacology
https://www.readbyqxmd.com/read/30341733/low-doses-of-widely-consumed-cannabinoids-cannabidiol-and-cannabidivarin-cause-dna-damage-and-chromosomal-aberrations-in-human-derived-cells
#5
Chiara Russo, Franziska Ferk, Miroslav Mišík, Nathalie Ropek, Armen Nersesyan, Doris Mejri, Klaus Holzmann, Margherita Lavorgna, Marina Isidori, Siegfried Knasmüller
Cannabidiol (CBD) and cannabidivarin (CBDV) are natural cannabinoids which are consumed in increasing amounts worldwide in cannabis extracts, as they prevent epilepsy, anxiety, and seizures. It was claimed that they may be useful in cancer therapy and have anti-inflammatory properties. Adverse long-term effects of these drugs (induction of cancer and infertility) which are related to damage of the genetic material have not been investigated. Therefore, we studied their DNA-damaging properties in human-derived cell lines under conditions which reflect the exposure of consumers...
October 19, 2018: Archives of Toxicology
https://www.readbyqxmd.com/read/30340007/yulangsan-polysaccharide-inhibits-4t1-breast-cancer-cell-proliferation-and-induces-apoptosis-in-vitro-and-in-vivo
#6
Ni Qin, Shiyin Lu, Ning Chen, Chunxia Chen, Qiuqiao Xie, Xiaojie Wei, Fangxing Ye, Junhui He, Yuchun Li, Lixiu Chen, Luhui Jiang, Xiaoqi Lu, Yuchan Yuan, Jian Li, Yang Jiao, Renbin Huang
Yulangsan polysaccharide (YLSPS) is derived from the root of Millettia pulchra (Benth.) Kurz var. Recent studies have postulated YLSPS as a regimen for cancer treatment. However, the underlying mechanism anti-breast cancer is still poorly unknown. The aim of this study was to examine the suppressive and apoptosis effect of YLSPS on the growth of breast cancer cell 4T1 and its possible underlying mechanism. In this study, breast cancer cell 4T1 viability and apoptosis were assessed by CCK-8 and flow cytometry, relative quantitative real-time PCR and western blot after treated with drug-serum of YLSPS...
October 16, 2018: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/30339990/synthesis-theoretical-spectroscopic-and-electrochemical-dna-binding-investigations-of-1-3-4-thiadiazole-derivatives-of-ibuprofen-and-ciprofloxacin-cancer-cell-line-studies
#7
Shahid Iqbal Farooqi, Nasima Arshad, Pervaiz Ali Channar, Fouzia Perveen, Aamer Saeed, Fayaz Ali Larik, Aneela Javeed
Two new 1,3,4-thiadiazole derivatives of ibuprofen and ciprofloxacin namely {(5-(1-(4-isobutylphenyl)ethyl)-1,3,4-thiadiazol-2-amine)} 1 and {(3-(5-amino-1,3,4-thiadiazol-2-yl)-1-cyclopropyl-6-fluoro-7-(piperazin-1-yl)quinolin-4(1H)-one)} 2 were synthesized and characterized by spectroscopic and elemental analysis. DFT and molecular docking were done initially for theoretical binding possibilities of the investigated compounds. In vitro DNA binding investigations were carried out with UV-visible spectroscopic, fluorescence spectroscopic, cyclic voltammetric (CV) experiments under physiological conditions of the stomach (4...
October 9, 2018: Journal of Photochemistry and Photobiology. B, Biology
https://www.readbyqxmd.com/read/30339356/cascade-amplifiers-of-intracellular-ros-based-on-mitochondria-targeted-core-shell-zno-tpp-d-h-nanorods-for-breast-cancer-therapy
#8
Xiao Liang, Shu-Mao Xu, Jun Zhang, Jing Li, Qi Shen
Tumor cells are vulnerable to reactive oxygen species (ROS). However, it is still a challenge to induce ROS efficiently in tumor cells. In this study, cascade amplifiers of intracellular ROS based on charge-reversible mitochondria-targeted ZnO-TPP@D/H nanorods were firstly developed for breast cancer therapy. The core-shell ZnO-TPP@D/H nanorod with particle size of 179.60 ± 5.67 nm was composed of a core of ZnO nanorod, an inner shell of triphenyl phosphonium (TPP), and an outer shell of heparin. DOX was loaded on ZnO-TPP@D/H nanorods with high drug loading efficiency of 22...
October 19, 2018: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/30337872/antidiabetic-biguanides-radiosensitize-hypoxic-colorectal-cancer-cells-through-a-decrease-in-oxygen-consumption
#9
Sven de Mey, Heng Jiang, Cyril Corbet, Hui Wang, Inès Dufait, Kalun Law, Estelle Bastien, Valeri Verovski, Thierry Gevaert, Olivier Feron, Mark De Ridder
Background and Purpose: The anti-diabetic biguanide drugs metformin and phenformin exhibit antitumor activity in various models. However, their radiomodulatory effect under hypoxic conditions, particularly for phenformin, is largely unknown. This study therefore examines whether metformin and phenformin as mitochondrial complex I blockades could overcome hypoxic radioresistance through inhibition of oxygen consumption. Materials and Methods: A panel of colorectal cancer cells (HCT116, DLD-1, HT29, SW480, and CT26) was exposed to metformin or phenformin for 16 h at indicated concentrations...
2018: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/30337535/a-discrete-organoplatinum-ii-metallacage-as-a-multimodality-theranostic-platform-for-cancer-photochemotherapy
#10
Guocan Yu, Shan Yu, Manik Lal Saha, Jiong Zhou, Timothy R Cook, Bryant C Yung, Jin Chen, Zhengwei Mao, Fuwu Zhang, Zijian Zhou, Yijing Liu, Li Shao, Sheng Wang, Changyou Gao, Feihe Huang, Peter J Stang, Xiaoyuan Chen
Photodynamic therapy is an effective alternative to traditional treatments due to its minimally invasive nature, negligible systemic toxicity, fewer side effects, and avoidance of drug resistance. However, it is still challenging to design photosensitizers with high singlet oxygen (1 O2 ) quantum yields (QY) due to severe aggregation of the hydrophobic photosensitizers. Herein, we developed a discrete organoplatinum(II) metallacage using therapeutic cis-(PEt3 )2 Pt(OTf)2 as the building block to improve the 1 O2 QY, thus achieving synergistic anticancer efficacy...
October 18, 2018: Nature Communications
https://www.readbyqxmd.com/read/30336366/restoring-guardianship-of-the-genome-anticancer-drug-strategies-to-reverse-oncogenic-mutant-p53-misfolding
#11
REVIEW
Husam A Babikir, Rayhaneh Afjei, Ramasamy Paulmurugan, Tarik F Massoud
p53 is a transcription factor that activates numerous genes involved in essential maintenance of genetic stability. P53 is the most frequently mutated gene in human cancer. One third of these mutations are structural, resulting in mutant p53 with a disrupted protein conformation. Here we review current progress in a relatively underexplored aspect of p53-targeted drug development, that is, strategies to reactivate wild-type function of misfolded mutant p53. Unfortunately, most p53-targeted drugs are still at early stages of development and many of them are progressing slowly toward clinical implementation...
September 20, 2018: Cancer Treatment Reviews
https://www.readbyqxmd.com/read/30336364/a-designer-bow-tie-combination-therapeutic-platform-an-approach-to-resistant-cancer-treatment-by-simultaneous-delivery-of-cytotoxic-and-anti-inflammatory-agents-and-radiation
#12
Rakesh K Pathak, Uttara Basu, Anis Ahmad, Shrita Sarkar, Anil Kumar, Bapurao Surnar, Saba Ansari, Katarzyna Wilczek, Michael E Ivan, Brian Marples, Nagesh Kolishetti, Shanta Dhar
Multimodal therapies are used to treat advanced cancers including castration-resistant prostate cancer to manage the biological characteristics of the tumors like inflammation, bone metastases, and participation of metabolically altered cancer stem cells (CSCs) that have integral roles in disease dissemination and progression. We developed a multifunctional polymer-based self-assembled technology to deliver a predefined stoichiometric combination of a chemotherapy and an anti-inflammatory agent in a stimuli responsive manner, to complement and improve the currently established treatment methods of prostate cancer...
December 2018: Biomaterials
https://www.readbyqxmd.com/read/30336249/the-involvement-of-autophagic-flux-in-the-development-and-recovery-of-doxorubicin-induced-neurotoxicity
#13
Xueyuan Zhou, Pengfei Xu, Ruili Dang, Yujin Guo, Gongying Li, Yi Qiao, Ruining Xie, Yuanyuan Liu, Pei Jiang
Doxorubicin (Dox) is an effective anti-cancer agent, whose clinical use is limited by the cytotoxicity in non-target tissues, especially the heart and brain. The drug-induced neuronal damage is primarily mediated by oxidative stress, in which autophagy plays a central role. Although numerous studies indicate the involvement of autophagy in neurodegenerative diseases and brain injury, the evidence concerning autophagic process in Dox-induced neuronal death is limited. We found that repeated Dox administration induced the protein expression of LC3II and P62 and impaired autophagic flux with enhanced autophagasome accumulation in rat hippocampus, whereas two weeks after the cessation of Dox treatment, the autophagic process was restored, even stimulated, with normalized protein levels of LC3II and P62 and enhanced expression of Becline-1, indicating a compensatory response in the recovery state...
October 15, 2018: Free Radical Biology & Medicine
https://www.readbyqxmd.com/read/30336060/cordycepin-augments-the-chemosensitivity-of-human-glioma-cells-to-temozolomide-by-activating-ampk-and-inhibiting-the-akt-signaling-pathway
#14
Yiming Bi, Han Li, Dazhuang Yi, Yuxue Sun, Yang Bai, Sheng Zhong, Yang Song, Gang Zhao, Yong Chen
Glioblastoma multiforme (GBM) is the most commonly encountered subtype of deadly brain cancer in human adults. It has a high recurrence rate and shows aggressive proliferation. The novel cytotoxic agent temozolomide (TMZ) is now frequently applied as the first-line chemotherapeutic treatment for GBM; however, a considerable number of patients treated with TMZ turn out to be refractory to this drug. Hence, a more effective therapeutic approach is urgently required to overcome this critical issue. Accumulating evidence has shown that both AMPK and AKT are activated by TMZ, while only AMPK contributes to apoptosis via mammalian target of rapamycin (mTOR) inhibition...
October 17, 2018: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/30336012/single-site-labeling-of-native-proteins-enabled-by-a-chemoselective-and-site-selective-chemical-technology
#15
Srinivasa Rao Adusumalli, Dattatraya Gautam Rawale, Usha Singh, Prabhanshu Tripathi, Rajesh Paul, Neetu Kalra, Ram Kumar Mishra, Sanjeev Shukla, Vishal Rai
Chemical biology research often requires precise covalent attachment of labels to the native proteins. Such methods are sought after to probe, design, and regulate the properties of proteins. At present, this demand is largely unmet due to the lack of empowering chemical technology. Here, we report a chemical platform that enables site-selective labeling of native proteins. Initially, a reversible intermolecular reaction places the "chemical linchpins" globally on all the accessible Lys residues. These linchpins have the capability to drive site-selective covalent labeling of proteins...
October 17, 2018: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/30335192/assessment-of-oatp-transporter-mediated-drug-drug-interaction-using-physiologically-based-pharmacokinetic-pbpk-modeling-a-case-example
#16
Yuan Chen, Rui Zhu, Fang Ma, Jialin Mao, Eugene C Chen, Edna Choo, Srikumar Sahasranaman, Lichuan Liu
GDC-0810 was under development as an oral anti-cancer drug for the treatment of estrogen receptor-positive breast cancer as a single agent or in combination. In vitro data indicated that GDC-0810 is a potent inhibitor of OATP1B1/1B3. To assess clinical risk, PBPK model was developed to predict the transporter drug-drug interaction (tDDI) between GDC-0810 and pravastatin in human. The PBPK model was constructed in Simcyp® by integrating in vitro and in vivo data for GDC-0810. The prediction of human pharmacokinetics (PK) was verified using GDC-0810 phase I clinical PK data...
October 18, 2018: Biopharmaceutics & Drug Disposition
https://www.readbyqxmd.com/read/30334765/identification-of-novel-scaffolds-with-dual-role-as-antiepileptic-and-anti-breast-cancer
#17
Shailima Rampogu, Ayoung Baek, Rohit S Bavi, Minky Son, Guang Ping Cao, Raj Kumar, Chanin Park, Amir Zeb, Rabia Mukthar Rana, Seok Ju Park, Keun Woo Lee
Aromatase inhibitors with an IC50 value ranging from 1.4 to 49.7uM are known to act as antiepileptic drugs besides being potential breast cancer inhibitors. The aim of the present study is to identify novel antiepileptic aromatase inhibitors with higher activity exploiting the ligand-based pharmacophore approach utilizing the experimentally known inhibitors. The resultant Hypo1 consists of four features and was further validated by using three different strategies. Hypo1 was allowed to screen different databases to identify lead molecules and were further subjected to Lipinski' Rule of Five and ADMET to establish their drug-like properties...
October 12, 2018: IEEE/ACM Transactions on Computational Biology and Bioinformatics
https://www.readbyqxmd.com/read/30334571/combination-therapy-for-the-treatment-of-pancreatic-cancer-through-hyaluronic-acid-decorated-nanoparticles-loaded-with-quercetin-and-gemcitabine-a-preliminary-in-vitro-study
#18
Carla Serri, Vincenzo Quagliariello, Rosario Vincenzo Iaffaioli, Sabato Fusco, Gerardo Botti, Laura Mayol, Marco Biondi
Combination chemotherapy by means of two or more drugs is prone to suppressing or discouraging the inception of multidrug resistance, exploiting the fact that diverse drugs act in different points of the cellular cycle of amplifying tumor cells. For example, the combination of gemcitabine (GMC) with quercetin (QCT) showed a synergistic effect in inhibiting the migration of pancreatic cancer cells. Consequently, herein GMC and QCT have been loaded within biodegradable nanoparticles (NPs) based on poly(lactic-co-glycolic acid), externally decorated with hyaluronic acid (HA; viz...
October 18, 2018: Journal of Cellular Physiology
https://www.readbyqxmd.com/read/30334060/synthesis-chemical-characterization-and-cancer-cell-growth-inhibitory-activities-of-cu-ii-and-ru-iii-aliphatic-and-aromatic-dithiocarbamato-complexes
#19
L Brustolin, C Nardon, N Pettenuzzo, N Zuin Fantoni, S Quarta, F Chiara, A Gambalunga, A Trevisan, L Marchiò, P Pontisso, D Fregona
In this paper, we focused on the analysis of the effects mediated by different cyclic dithiocarbamic ligands (DTC) on three classes of antiproliferative coordination compounds, namely, Ru(iii) complexes with the general formulae [Ru(DTC)3] and [Ru2(DTC)5]Cl, and the neutral Cu(ii) derivatives of the type [Cu(DTC)2]. In particular, we present the synthesis and characterization of a library of total 23 coordination compounds containing Ru(iii) or Cu(ii) as the biologically-active metal center and two or more dithiocarbamato (DTC) ligands derived from cyclic amines (aliphatic or aromatic)...
October 18, 2018: Dalton Transactions: An International Journal of Inorganic Chemistry
https://www.readbyqxmd.com/read/30334018/bh3-dependent-and-independent-activation-of-bax-and-bak-in-mitochondrial-apoptosis
#20
Paul S Jeng, Akane Inoue-Yamauchi, James J Hsieh, Emily H Cheng
Mitochondria play key roles in mammalian apoptosis, a highly regulated genetic program of cell suicide. Multiple apoptotic signals culminate in mitochondrial outer membrane permeabilization (MOMP), which not only couples the mitochondria to the activation of caspases but also initiates caspase-independent mitochondrial dysfunction. The BCL-2 family proteins are central regulators of MOMP. Multidomain pro-apoptotic BAX and BAK are essential effectors responsible for MOMP, whereas anti-apoptotic BCL-2, BCL-XL , and MCL-1 preserve mitochondrial integrity...
June 2018: Current Opinion in Physiology
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