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https://www.readbyqxmd.com/read/29140298/enhancement-of-bone-marrow-derived-mesenchymal-stem-cell-osteogenesis-and-new-bone-formation-in-rats-by-obtusilactone-a
#1
Yi-Hsiung Lin, Chung-Yi Chen, Liang-Yin Chou, Chung-Hwan Chen, Lin Kang, Chau-Zen Wang
The natural pure compound obtusilactone A (OA) was identified in Cinnamomum kotoense Kanehira & Sasaki, and shows effective anti-cancer activity. We studied the effect of OA on osteogenesis of bone marrow-derived mesenchymal stem cells (BMSCs). OA possesses biocompatibility, stimulates Alkaline Phosphatase (ALP) activity and facilitates mineralization of BMSCs. Expression of osteogenesis markers BMP2, Runx2, Collagen I, and Osteocalcin was enhanced in OA-treated BMSCs. An in vivo rat model with local administration of OA via needle implantation to bone marrow-residing BMSCs revealed that OA increased the new bone formation and trabecular bone volume in tibias...
November 15, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/29140270/the-oxepane-motif-in-marine-drugs
#2
REVIEW
Héctor Barbero, Carlos Díez-Poza, Asunción Barbero
Oceans have shown to be a remarkable source of natural products. The biological properties of many of these compounds have helped to produce great advances in medicinal chemistry. Within them, marine natural products containing an oxepanyl ring are present in a great variety of algae, sponges, fungus and corals and show very important biological activities, many of them possessing remarkable cytotoxic properties against a wide range of cancer cell lines. Their rich chemical structures have attracted the attention of many researchers who have reported interesting synthetic approaches to these targets...
November 15, 2017: Marine Drugs
https://www.readbyqxmd.com/read/29139598/preparation-and-comparative-evaluation-of-99m-tc-hynic-cngr-and-99m-tc-hynic-peg2-cngr-as-tumor-targeting-molecular-imaging-probes
#3
Kusum Vats, Drishty Satpati, Rohit Sharma, Chandan Kumar, Haladhar Dev Sarma, Sharmila Banerjee
The tripeptide sequence NGR (asparagine-glycine-arginine) specifically recognizes aminopeptidase N (APN or CD13) receptors highly expressed on tumor cells as well as tumor vasculature. Thus NGR peptides can precisely deliver therapeutic and diagnostic compounds to CD13 expressing cancer sites. In this regard two NGR peptide ligands, HYNIC-c(NGR) and HYNIC-PEG2 -c(NGR) were synthesized, radiolabeled with (99m) Tc and evaluated in CD13-positive human fibrosarcoma HT-1080 tumor xenografts. The radiotracers, (99m) Tc-HYNIC-c(NGR) and (99m) Tc-HYNIC-PEG2 -c(NGR) could be prepared in ~95% radiochemical purity (RCP) and exhibited excellent in vitro and in vivo stability...
November 15, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
https://www.readbyqxmd.com/read/29136951/chemopreventive-effect-of-myricetin-a-natural-occurring-compound-on-colonic-chronic-inflammation-and-inflammation-driven-tumorigenesis-in-mice
#4
Mei-Jia Zhang, Han Su, Jing-Yue Yan, Na Li, Zhi-Yu Song, Huai-Jie Wang, Lian-Guang Huo, Feng Wang, Wan-Sheng Ji, Xian-Jun Qu, Mei-Hua Qu
Myricetin is a flavonoids compound extracted from edible myrica rubra. We aimed to evaluate the efficacy of Myricetin on colonic chronic inflammation and inflammation-driven tumorigenesis in mice. Myricetin was administrated by gavage for 4 consecutive weeks. Mice were sacrificed and the number of colonic polyps was counted. Myricetin significantly inhibited AOM/DSS-induced colitis and colorectal tumorigenesis. Myricetin prevented the incidence of colorectal tumorigenesis and reduced the size of colorectal polyps...
November 9, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29136779/juglanin-ameliorates-lps-induced-neuroinflammation-in-animal-models-of-parkinson-s-disease-and-cell-culture-via-inactivating-tlr4-nf-%C3%AE%C2%BAb-pathway
#5
Fang-Xue Zhang, Ren-Shi Xu
Parkinson's disease (PD) is a common neuro-degenerative disorder, and novel therapeutic targets are required for the treatment of PD. Juglanin is a natural compound extracted from the crude Polygonum aviculare, exhibiting anti-inflammatory, anti-oxidant and anti-cancer activities. In our study, PD in mice was induced by systemic LPS treatment as evidenced by enhanced α-synuclein and reduced tyrosine hydroxylase (TH), which were reversed by juglanin treatment. Moreover, juglanin administration attenuated LPS-caused behavioral and memory impairments and reduced LPS-induced enhancement of neuro-degenerative markers, including amyloid β (Aβ) and p-Tau...
November 7, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29135096/silibinin-promotes-the-apoptosis-of-gastric-cancer-bgc823-cells-through-caspase-pathway
#6
Runfang Li, Jianmin Yu, Chengjun Wang
PURPOSE: To investigate the effects of silibinin, a natural compound, on the proliferation and apoptosis of BGC-823 gastric cancer cell line and to figure out the relevant pathways. METHODS: BGC-823 gastric cancer cells were treated with silibinin at various concentrations (0,25,50,100,150 and 200μM). Zero μM was the control group and the other concentrations were defined as the experimental groups. The effects of silibinin on the proliferation of BGC-823 gastric cancer cells were explored through methylthiazolyldiphenyltetrazolium bromide (MTT)...
September 2017: Journal of B.U.ON.: Official Journal of the Balkan Union of Oncology
https://www.readbyqxmd.com/read/29134654/pten-loss-and-activation-of-k-ras-and-%C3%AE-catenin-cooperate-to-accelerate-prostate-tumourigenesis
#7
Matthew T Jefferies, Adam C Cox, Boris Y Shorning, Valerie Meniel, David Griffiths, Howard G Kynaston, Matthew J Smalley, Alan R Clarke
Aberrant phosphoinositide 3-kinase (PI3K), mitogen-activated protein kinase (MAPK) and WNT signalling are emerging as key events in the multistep nature of prostate tumourigenesis and progression. Here, we report a compound prostate cancer murine model in which these signalling pathways cooperate to produce a more aggressive prostate cancer phenotype. Using Cre-LoxP technology and the probasin promoter, we combined the loss of Pten (Pten(fl/fl) ), to activate the PI3K signalling pathway, with either dominant stabilized β-catenin [Catnb(+/lox(ex3)) ] or activated K-RAS (K-Ras(+/V12) ) to aberrantly activate WNT and MAPK signalling, respectively...
November 14, 2017: Journal of Pathology
https://www.readbyqxmd.com/read/29134467/diterpenoid-natural-compound-c4-crassin-exerts-cytostatic-effects-on-triple-negative-breast-cancer-cells-via-a-pathway-involving-reactive-oxygen-species
#8
Cathy E Richards, Sri H Vellanki, Yvonne E Smith, Ann M Hopkins
PURPOSE: Triple-negative breast cancers (TNBC) lack expression of three common cell surface receptors, i.e., estrogen receptor (ER), progesterone receptor (PR) and human epidermal growth factor receptor-2 (HER2). Accordingly, TNBCs are associated with fewer treatment options and a relatively poor prognosis. Having screened a National Cancer Institute natural compound library, the purpose of this study was to investigate the bioactivity of compound C4 (Crassin) in TNBC cells. METHODS: Cell viability assays were performed in two TNBC cell lines, MDA-MB-231 and 4T1, following C4 treatment in the presence or absence of the antioxidant N-acetyl-L-cysteine (NAC)...
November 13, 2017: Cellular Oncology (Dordrecht)
https://www.readbyqxmd.com/read/29133241/in-silico-comparisons-between-natural-inhibitors-of-abcb1-p-glycoprotein-to-overcome-doxorubicin-resistance-in-the-nci-adr-res-cell-line
#9
Mohamed A Morsy, Azza A K El-Sheikh, Ahmed R N Ibrahim, Mohammed A Khedr, Abdulla Y Al-Taher
To investigate compound-protein binding mode and molecular dynamic simulation of P-glycoprotein (P-gp), in silico studies were performed to compare 12 naturally occurring compounds using two softwares. The net results showed that piperine (PIP) had the best binding affinity. In vitro studies on DOX-resistant NCI/ADR-RES cells, known to express P-gp, showed that, dose-dependently, PIP significantly increased intracellular accumulation of rhodamine-123 and had cytotoxic effects accessed by MTT assay. In addition, PIP at 25 and 50μM significantly potentiated DOX-induced cytotoxicity on the same cell line...
November 10, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29133216/anti-cancer-effects-of-naturally-derived-compounds-targeting-histone-deacetylase-6-related-pathways
#10
REVIEW
Manon Lernoux, Michael Schnekenburger, Mario Dicato, Marc Diederich
Alterations of the epigenetic machinery, affecting multiple biological functions, represent a major hallmark enabling the development of tumors. Among epigenetic regulatory proteins, histone deacetylase (HDAC)6 has emerged as an interesting potential therapeutic target towards a variety of diseases including cancer. Accordingly, this isoenzyme regulates many vital cellular regulatory processes and pathways essential to physiological homeostasis, as well as tumor multistep transformation involving initiation, promotion, progression and metastasis...
November 10, 2017: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
https://www.readbyqxmd.com/read/29133051/design-synthesis-and-preliminary-biological-evaluation-of-5-8-dihydropteridine-6-7-diones-that-induce-apoptosis-and-suppress-cell-migration
#11
Peng-Fei Geng, Cong-Cong Wang, Zhong-Hua Li, Xiao-Ning Hu, Tao-Qian Zhao, Dong-Jun Fu, Bing Zhao, Bin Yu, Hong-Min Liu
Pteridines are an important class of fused heterocycles found in natural products and drug molecules, and have shown diverse biological activities. A focused library of 5,8-dihydropteridine-6,7-dione derivatives were designed and evaluated for their antiproliferative activity against MGC-803, SGC-7901, A549 and PC-3 cancer cell lines. The SARs studies highlighted the importance of the piperazine substituted 5,8-dihydropteridine-6,7-dione frameworks for the activity and revealed essential structural elements...
November 5, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29133046/design-synthesis-and-biological-evaluation-of-novel-benzimidazole-amidines-as-potent-multi-target-inhibitors-for-the-treatment-of-non-small-cell-lung-cancer
#12
Andrea Bistrović, Luka Krstulović, Anja Harej, Petra Grbčić, Mirela Sedić, Sanja Koštrun, Sandra Kraljević Pavelić, Miroslav Bajić, Silvana Raić-Malić
A series of novel amidino 2-substituted benzimidazoles linked to 1,4-disubstituted 1,2,3-triazoles were synthesized by implementation of microwave and ultrasound irradiation in click reaction and subsequent condensation of thus obtained 4-(1,2,3-triazol-1-yl)benzaldehyde with o-phenylenediamines. In vitro antiproliferative screening of compounds performed on human cancer cell lines revealed that p-chlorophenyl-substituted 1,2,3-triazolyl N-isopropylamidine 10c and benzyl-substituted 1,2,3-triazolyl imidazoline 11f benzimidazoles had selective and potent cytostatic activities in the low nM range against non-small cell lung cancer cell line A549, which could be attributed to induction of apoptosis and primary necrosis...
November 10, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29131317/molecular-photoprotection-of-human-keratinocytes-in-vitro-by-the-naturally-occurring-mycosporine-like-amino-acid-maa-palythine
#13
K P Lawrence, R Gacesa, P F Long, A R Young
BACKGROUND: Solar ultraviolet radiation (UVR) induces molecular and genetic changes in the skin, which result in skin cancer, photoageing and photosensitivity disorders. The use of sunscreens is advocated to prevent such photodamage, however most formulations contain synthetic UVR filters that are non-biodegradable and can damage fragile marine ecosystems. Mycosporine-like amino acids (MAA) are natural UVR-absorbing compounds that have evolved in marine species for protection against chronic UVR exposure in shallow-water habitats...
November 13, 2017: British Journal of Dermatology
https://www.readbyqxmd.com/read/29130448/a-review-on-the-effects-of-current-chemotherapy-drugs-and-natural-agents-in-treating-non-small-cell-lung-cancer
#14
Chih-Yang Huang, Da-Tong Ju, Chih-Fen Chang, P Muralidhar Reddy, Bharath Kumar Velmurugan
Lung cancer is the leading cause of cancer deaths worldwide, and this makes it an attractive disease to review and possibly improve therapeutic treatment options. Surgery, radiation, chemotherapy, targeted treatments, and immunotherapy separate or in combination are commonly used to treat lung cancer. However, these treatment types may cause different side effects, and chemotherapy-based regimens appear to have reached a therapeutic plateau. Hence, effective, better-tolerated treatments are needed to address and hopefully overcome this conundrum...
December 2017: BioMedicine
https://www.readbyqxmd.com/read/29129699/deguelin-an-aurora-b-kinase-inhibitor-exhibits-potent-anti-tumor-effect-in-human-esophageal-squamous-cell-carcinoma
#15
Xinfang Yu, Qi Liang, Wenbin Liu, Li Zhou, Wei Li, Haidan Liu
Aurora B kinase has emerged as a key regulator of mitosis and deregulation of Aurora B activity is closely related to the development and progression of human cancers. In the present study, we found that Aurora B is overexpressed in human esophageal squamous cell carcinoma (ESCC), high levels of Aurora B protein were associated with a worse overall survival rate in ESCC patients. Depleting of Aurora B blunted the malignant phenotypes in ESCC cells. Importantly, we demonstrated that a natural compound, deguelin, has a profound anti-tumor effect on ESCC via inhibiting Aurora B activity...
November 3, 2017: EBioMedicine
https://www.readbyqxmd.com/read/29129653/targeting-ncrnas-by-plant-secondary-metabolites-the-ncrnas-game-in-the-balance-towards-malignancy-inhibition
#16
REVIEW
Diana Gulei, Nikolay Mehterov, Seyed Mohammad Nabavi, Atanas Georgiev Atanasov, Ioana Berindan-Neagoe
The current trend of combining state of the art technologies with quondam treatments in order to overcome existing gaps in clinics determined an increased interest into polyphenols, common dietary phytochemicals, for the prevention and treatment of chronic diseases, especially cancer. The reemergence of polyphenols in the cancer field is sustained by transcriptomics technologies able to identify coding and non-coding genes and their related signaling pathways modulated by natural compounds. Identification of the structural correspondence between interacting molecules will allow the development of more targeted and informed therapeutic strategies for cancer management...
November 9, 2017: Biotechnology Advances
https://www.readbyqxmd.com/read/29129629/phenolic-compounds-based-conjugates-from-dextran-aldehyde-and-bsa-preparation-characterization-and-evaluation-of-their-anti-cancer-efficacy-for-therapeutic-applications
#17
Sudheer Rai, Amit Kumar Kureel, P K Dutta, G K Mehrotra
Here, we have synthesized phenolic compounds (pc) based on conjugates from dextran aldehyde (dex-ald) and bovine serum albumin (BSA) and screening their potential activity as therapeutic agents in cancer disease. The synthesized conjugates were analyzed by UV-vis, FT-IR, XRD and SEM analysis. UV-vis spectra of conjugates showed the shifting of spectral peak at UV to visible region revealed the enhanced conjugation due to formation of linkage. The XRD peaks of conjugates found broader and indicating the amorphous phase of conjugating materials in compared to free components...
November 9, 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/29127724/safety-aspects-of-the-use-of-quercetin-as-a-dietary-supplement
#18
REVIEW
Susanne Andres, Sophie Pevny, Rainer Ziegenhagen, Nadiya Bakhiya, Bernd Schäfer, Karen Ildico Hirsch-Ernst, Alfonso Lampen
The flavonoid quercetin is frequently found in low amounts as a secondary plant metabolite in fruits and vegetables. Isolated quercetin is also marketed as a dietary supplement, mostly as the free quercetin aglycone, and frequently in daily doses of up to 1000 mg per day exceeding usual dietary intake levels. The present review is dedicated to safety aspects of isolated quercetin used as single compound in dietary supplements. Among the numerous published human intervention studies, adverse effects following supplemental quercetin intake have been rarely reported and any such effects were mild in nature...
November 11, 2017: Molecular Nutrition & Food Research
https://www.readbyqxmd.com/read/29126025/metallurgical-residues-reused-as-filler-after-35years-and-their-natural-weathering-implications-in-a-mountain-area
#19
Leticia Gómez-Nubla, Julene Aramendia, Silvia Fdez-Ortiz de Vallejuelo, Juan Manuel Madariaga
The natural weathering of EAF (Electric Arc Furnace) and LF (Ladle Furnace) steel slag was evaluated through changes in the mineralogical and elemental composition. For that purpose, black steel slag and mixture of black and white steel slag were collected from two forest tracks, where they had been used as filler 19 and 35years ago respectively in a protected mountain area. Primary/original and secondary/degradation compounds were identified by spectroscopic techniques (Raman Spectroscopy, X-Ray Diffraction (XRD) and Scanning Electron Microscopy/Energy Dispersive X-Ray Spectroscopy (SEM/EDS))...
November 7, 2017: Science of the Total Environment
https://www.readbyqxmd.com/read/29125580/structural-diversity-biological-properties-and-applications-of-natural-products-from-cyanobacteria-a-review
#20
REVIEW
Sayed Asmat Ali Shah, Najeeb Akhter, Bibi Nazia Auckloo, Ishrat Khan, Yanbin Lu, Kuiwu Wang, Bin Wu, Yue-Wei Guo
Nowadays, various drugs on the market are becoming more and more resistant to numerous diseases, thus declining their efficacy for treatment purposes in human beings. Antibiotic resistance is one among the top listed threat around the world which eventually urged the discovery of new potent drugs followed by an increase in the number of deaths caused by cancer due to chemotherapy resistance as well. Accordingly, marine cyanobacteria, being the oldest prokaryotic microorganisms belonging to a monophyletic group, have proven themselves as being able to generate pharmaceutically important natural products...
November 10, 2017: Marine Drugs
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