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https://www.readbyqxmd.com/read/28814868/nano-sized-cytochrome-p450-3a4-inhibitors-to-block-hepatic-metabolism-of-docetaxel
#1
Marion Paolini, Laurence Poul, Céline Berjaud, Matthieu Germain, Audrey Darmon, Maxime Bergère, Agnès Pottier, Laurent Levy, Eric Vibert
Most drugs are metabolized by hepatic cytochrome P450 3A4 (CYP3A4), resulting in their reduced bioavailability. In this study, we present the design and evaluation of bio-compatible nanocarriers trapping a natural CYP3A4-inhibiting compound. Our aim in using nanocarriers was to target the natural CYP3A4-inhibiting agent to hepatic CYP3A4 and leave drug-metabolizing enzymes in other organs undisturbed. In the design of such nanocarriers, we took advantage of the nonspecific accumulation of small nanoparticles in the liver...
2017: International Journal of Nanomedicine
https://www.readbyqxmd.com/read/28813533/18%C3%A3-glycyrrhetinic-acid-derivative-promotes-proliferation-migration-and-aquaporin-3-expression-in-human-dermal-fibroblasts
#2
Chi-Feng Hung, Chien-Yu Hsiao, Wen-Hao Hsieh, Hsin-Ju Li, Yi-Ju Tsai, Chun-Nan Lin, Hsun-Hsien Chang, Nan-Lin Wu
Licorice (Glycyrrhiza) species have been widely used as a traditional medicine and a natural sweetener in foods. The 18β-glycyrrhetinic acid (18β-GA) is a bioactive compound in licorice that exhibits potential anti-cancer, anti-inflammatory, and anti-microbial activities. Many synthesized derivatives of 18β-GA have been reported to be cytotoxic and suggested for the treatment of malignant diseases. In this study, we explored the possible pharmacological roles of an 18β-GA derivative in skin biology using primary human dermal fibroblasts and HaCaT keratinocytes as cell models...
2017: PloS One
https://www.readbyqxmd.com/read/28812060/reolysin-and-histone-deacetylase-inhibition-in-the-treatment-of-head-and-neck-squamous-cell-carcinoma
#3
Alena C Jaime-Ramirez, Jun-Ge Yu, Enrico Caserta, Ji Young Yoo, Jianying Zhang, Tae Jin Lee, Craig Hofmeister, John H Lee, Bhavna Kumar, Quintin Pan, Pawan Kumar, Robert Baiocchi, Theodoros Teknos, Flavia Pichiorri, Balveen Kaur, Matthew Old
Oncolytic viruses (OVs) are emerging as powerful anti-cancer agents and are currently being tested for their safety and efficacy in patients. Reovirus (Reolysin), a naturally occurring non-pathogenic, double-stranded RNA virus, has natural oncolytic activity and is being tested in phase I-III clinical trials in a variety of tumor types. With its recent US Food and Drug Administration (FDA) orphan drug designation for several tumor types, Reolysin is a potential therapeutic agent for various cancers, including head and neck squamous cell carcinomas (HNSCCs), which have a 5-year survival of ∼55%...
June 16, 2017: Molecular Therapy Oncolytics
https://www.readbyqxmd.com/read/28808383/chemopreventive-potential-of-major-flavonoid-compound-of-methanolic-bark-extract-of-saraca-asoca-roxb-in-benzene-induced-toxicity-of-acute-myeloid-leukemia-mice
#4
Manas Kumar Mukhopadhyay, Mithun Shaw, Debjani Nath
BACKGROUND: Saraca asoca (SA) (Roxb.) is one of the folk medicinal plants found in India, Bangladesh, and Sri Lanka. Its major biological activity appears due to the presence of flavonoid group of compounds in its bark extract. OBJECTIVE: In this study, our research aims to analyze the chemopreventive effect of flavonoids, especially a natural phenol catechin present in the bark methanolic extract of SA on acute myeloid leukemia (AML) mice. MATERIALS AND METHODS: The total bark extract was partitioned and analyzed on thin-layer chromatography (TLC) plate...
July 2017: Pharmacognosy Magazine
https://www.readbyqxmd.com/read/28803233/comprehensive-analysis-of-the-chemical-composition-and-in-vitro-cytotoxic-mechanisms-of-pallines-spinosa-flower-and-leaf-essential-oils-against-breast-cancer-cells
#5
Ayman M Saleh, Mahmoud A Al-Qudah, Amre Nasr, Sayed A Rizvi, Anwar Borai, Mustafa Daghistani
BACKGROUND/AIMS: In our quest for new natural anticancer agents, we studied the cytotoxicity of the essential oils extracted from flowers and leaves of Pallines spinosa. METHODS: The essential oils were extracted by hydrodistillation and solid phase microextraction (SPME) from flowers and leaves of the plant and their composition was determined by GC/GC-MS. The cytotoxicity of the oils was evaluated against MCF-7 and MDA-MB-231 breast adenocarcinomas, and the non-cancerous MCF-10-2A cells, using a flow cytometry-based assay Apoptosis was evaluated by flow cytometry, nuclear staining, caspases activation, and Western blotting techniques, and cell cycle by measuring DNA contents...
August 11, 2017: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/28803136/anti-inflammatory-activity-of-natural-stilbenoids-a-review
#6
REVIEW
Marcela Dvorakova, Premysl Landa
Resveratrol and other natural stilbenoids, including piceatannol, pterostilbene, and gnetol, are well-known anti-inflammatory compounds with indisputable activity in vitro as well as in vivo. Their molecular targets include inducible nitric oxide synthase, cyclooxygenases, leukotrienes, nuclear factor kappa B, tumor necrosis factor α, interleukins and many more. This anti-inflammatory activity together with their antioxidant activity is believed to stand behind their other positive health effects against cancer, cardiovascular and neurodegenerative diseases or diabetes...
August 9, 2017: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
https://www.readbyqxmd.com/read/28802670/chemoselective-fluorination-and-chemoinformatic-analysis-of-griseofulvin-natural-vs-fluorinated-fungal-metabolites
#7
Noemi D Paguigan, Mohammed H Al-Huniti, Huzefa A Raja, Austin Czarnecki, Joanna E Burdette, Mariana González-Medina, José L Medina-Franco, Stephen J Polyak, Cedric J Pearce, Mitchell P Croatt, Nicholas H Oberlies
Griseofulvin is a fungal metabolite and antifungal drug used for the treatment of dermatophytosis in both humans and animals. Recently, griseofulvin and its analogues have attracted renewed attention due to reports of their potential anticancer effects. In this study griseofulvin (1) and related analogues (2-6, with 4 being new to literature) were isolated from Xylaria cubensis. Six fluorinated analogues (7-12) were synthesized, each in a single step using the isolated natural products and Selectflour, so as to examine the effects of fluorine incorporation on the bioactivities of this structural class...
July 28, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28801140/the-therapeutic-effects-of-longikaurin-a-a-natural-ent-kauranoid-in-esophageal-squamous-cell-carcinoma-depend-on-ros-accumulation-and-jnk-p38-mapk-activation
#8
Yun Che, Jingnan Wang, Zuyang Yuan, Yuan Li, Zhiliang Lu, Zhirong Zhang, Jinyao Zhang, Jun Wan, Handong Sun, Zhaoli Chen, Jianxin Pu, Jie He
Effective treatments for esophageal squamous cell carcinoma (ESCC), one of the most common cancers in China, are lacking. Longikaurin A (LK-A), an ent-kauranoid diterpenoid isolated from Isodon ternifolius, has been shown to have potent cytotoxic effects on ESCC cells both in vivo and in vitro, mainly by inducing apoptosis. In this study, LK-A inhibited ESCC cells viability and induced G2/M cell cycle arrest. Moreover, LK-A was also highly effective in a KYSE-30 xenograft nude mouse model. Treatment with Z-VAD(OMe)-FMK partially attenuated LK-A-induced apoptosis...
August 8, 2017: Toxicology Letters
https://www.readbyqxmd.com/read/28800931/molecular-signatures-of-longevity-insights-from-cross-species-comparative-studies
#9
REVIEW
Siming Ma, Vadim N Gladyshev
Much of the current research on longevity focuses on the aging process within a single species. Several molecular players (e.g. IGF1 and MTOR), pharmacological compounds (e.g. rapamycin and metformin), and dietary approaches (e.g. calorie restriction and methionine restriction) have been shown to be important in regulating and modestly extending lifespan in model organisms. On the other hand, natural lifespan varies much more significantly across species. Within mammals alone, maximum lifespan differs more than 100 fold, but the underlying regulatory mechanisms remain poorly understood...
August 8, 2017: Seminars in Cell & Developmental Biology
https://www.readbyqxmd.com/read/28800701/a-new-indole-derivative-decreased-sall4-gene-expression-in-acute-promyelocytic-leukemia-cell-line-nb4
#10
Zahra Sheikhrezaei, Parisa Heydari, Alireza Farsinezhad, Ahmad Fatemi, Soudeh Khanamani Falahati-Pour, Shokoofeh Darakhshan, Mojgan Noroozi Karimabad, Ali Darekordi, Hossein Khorramdelazad, Gholamhossein Hassanshahi
Background: Acute myeloblastic leukemia (AML) is a clonal disorder due to bone marrow failure and uncontrolled proliferation of myeloid lineage. Acute promyelocytic leukemia (APL) is a subtype of AML. Heterocyclic compounds, such as indole, are considered as attractive candidates for cancer therapy, due to their abundance in nature and known biological activity. Sal-like protein (SALL4) is a zinc finger transcription factor involving in the multi-potency of stem cells, in the NB4 cell line...
August 12, 2017: Iranian Biomedical Journal
https://www.readbyqxmd.com/read/28799796/immune-modulation-by-curcumin-the-role-of-interleukin-10
#11
Hamid Mollazadeh, Arrigo F G Cicero, Christopher N Blesso, Matteo Pirro, Muhammed Majeed, Amirhossein Sahebkar
Cytokines are small secreted proteins released by different types of cells with specific effects on cellular signaling and communication via binding to their receptors on the cell surface. IL-10 is known to be a pleiotropic and potent anti-inflammatory and immunosuppressive cytokine that is produced by both innate and adaptive immunity cells including dendritic cells, macrophages, mast cells, natural killer cells, eosinophils, neutrophils, B cells, CD8(+) T cells, and TH1, TH2, and TH17 and regulatory T cells...
August 11, 2017: Critical Reviews in Food Science and Nutrition
https://www.readbyqxmd.com/read/28798007/industrial-pollutants-and-nasopharyngeal-cancer-an-open-question
#12
Roberto Menicagli, Gianni Bolla, Laura Menicagli, Anastassia Esseiridou
INTRODUCTION AND OBJECTIVES: Nasopharyngeal Carcinoma represents 0.7% of the total cancer cases in the world with an ASR index of 1.7 and is widely associated with Epstein-Barr virus. It is not common in Italy (ASR index of 0.5) while in China (ASR 1.9), one third of the clinical cases are observed in Guangdong (ASR index 11.3). It is also quite common in Malaysia and Indonesia. The activation of the cancerogenesis process happens after the exposure to some environmental parameters that epidemiological studies have indicated with various dietary habits, mainly for salted fish consumption...
May 2017: Gulf Journal of Oncology
https://www.readbyqxmd.com/read/28795757/ph-driven-preparation-of-two-related-platinum-ii-complexes-exhibiting-distinct-cytotoxic-properties
#13
Jordi Molas Saborit, Amparo Caubet, Rosa F Brissos, Luís Korrodi-Gregório, Ricardo Pérez-Tomás, Manuel Martínez, Patrick Gamez
Reaction of cis-[PtCl2(DMSO)2] with the ligand 4-methyl-2-N-(2-pyridylmethylene)aminophenol (Hpyrimol, LH) in methanol at room temperature produces the complexes [PtCl2LH] or [PtClL], under acidic or basic conditions, respectively. The two platinum compounds exhibit distinct DNA-interacting properties, [PtCl2LH] showing a higher affinity for the biomolecules. Furthermore, [PtClL] is clearly more cytotoxic than [PtCl2LH] in three different cancer cell lines. Solution studies reveal the occurrence of intricate solvation processes generating different aquated/hydroxido species, whose nature depends on the starting metal complex and the pH of the medium...
August 10, 2017: Dalton Transactions: An International Journal of Inorganic Chemistry
https://www.readbyqxmd.com/read/28795217/animals-living-in-polluted-environments-are-a-potential-source-of-anti-tumor-molecule-s
#14
REVIEW
Shareni Jeyamogan, Naveed Ahmed Khan, Ruqaiyyah Siddiqui
Despite advances in therapeutic interventions and supportive care, the morbidity and mortality associated with cancer have remained significant. Thus, there is a need for newer and more powerful anti-tumor agents. The search for new anti-tumor compounds originating from natural resources is a promising research area. Animals living in polluted environments are a potent source of anti-tumor agents. Under polluted milieus, species such as crocodiles, feed on rotten meat, are exposed to heavy metals, endure high levels of radiation, and are among the very few species to survive the catastrophic Cretaceous-Tertiary extinction event with a prolonged lifespan...
August 9, 2017: Cancer Chemotherapy and Pharmacology
https://www.readbyqxmd.com/read/28794411/dextran-catechin-inhibits-angiogenesis-by-disrupting-copper-homeostasis-in-endothelial-cells
#15
Eugene M H Yee, Miriam B Brandl, Eddy Pasquier, Giuseppe Cirillo, Kathleen Kimpton, Maria Kavallaris, Naresh Kumar, Orazio Vittorio
Formation of blood vessels, or angiogenesis, is crucial to cancer progression. Thus, inhibiting angiogenesis can limit the growth and spread of tumors. The natural polyphenol catechin has moderate anti-tumor activity and interacts with copper, which is essential for angiogenesis. Catechin is easily metabolized in the body and this limits its clinical application. We have recently shown that conjugation of catechin with dextran (Dextran-Catechin) improves its serum stability, and exhibits potent anti-tumor activity against neuroblastoma by targeting copper homeostasis...
August 9, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28791369/cepharanthine-hydrochloride-reverses-p%C3%A2-glycoprotein-mediated-multidrug-resistance-in-human-ovarian-carcinoma-a2780-taxol-cells-by-inhibiting-the-pi3k-akt-signaling-pathway
#16
Chen-Zheng Huang, Ya-Feng Wang, Yan Zhang, You-Mei Peng, Yi-Xian Liu, Fang Ma, Jin-Hua Jiang, Qing-Duan Wang
Ovarian cancer has the highest mortality rate among gynecologic malignant tumors. The major obstacle to treatment success is multidrug resistance (MDR) to chemotherapy drugs. Cepharanthine hydrochloride (CH), a natural alkaloid-derived compound, has shown MDR reversal potency in several tumor cell lines; however, the molecular mechanism is not entirely known. In the present study, we assessed whether CH sensitized malignant cells to chemotherapy drugs in ovarian cancer and explored the relevant mechanism. We found that CH reduced the IC50 value of paclitaxel and increased intracellular rhodamine-123 accumulation in human ovarian cancer A2780/Taxol cells in a concentration-dependent manner...
August 4, 2017: Oncology Reports
https://www.readbyqxmd.com/read/28783331/discovery-and-synthesis-of-caracolamide-a-an-ion-channel-modulating-dichlorovinylidene-containing-phenethylamide-from-a-panamanian-marine-cyanobacterium-cf-symploca-species
#17
C Benjamin Naman, Jehad Almaliti, Lorene Armstrong, Eduardo J Caro-Díaz, Marsha L Pierce, Evgenia Glukhov, Amanda Fenner, Carmenza Spadafora, Hosana M Debonsi, Pieter C Dorrestein, Thomas F Murray, William H Gerwick
A recent untargeted metabolomics investigation into the chemical profile of 10 organic extracts from cf. Symploca spp. revealed several interesting chemical leads for further natural product drug discovery. Subsequent target-directed isolation efforts with one of these, a Panamanian marine cyanobacterium cf. Symploca sp., yielded a phenethylamide metabolite that terminates in a relatively rare gem-dichlorovinylidene moiety, caracolamide A (1), along with a known isotactic polymethoxy-1-alkene (2). Detailed NMR and HRESIMS analyses were used to determine the structures of these molecules, and compound 1 was confirmed by a three-step synthesis...
August 7, 2017: Journal of Natural Products
https://www.readbyqxmd.com/read/28782773/triptolide-and-celastrol-loaded-silk-fibroin-nanoparticles-show-synergistic-effect-against-human-pancreatic-cancer-cells
#18
Baoyue Ding, Md Arif Wahid, Zhijun Wang, Chen Xie, Arvind Thakkar, Sunil Prabhu, Jeffrey Wang
Pancreatic cancer is a lethal disease with a dreadful 5-year survival rate of only 5%. In spite of several treatment options, the prognosis still remains extremely poor. Therefore, novel therapy strategies with combinations of drugs are urgently required to combat this fatal disease. Triptolide (TPL) and celastrol (CL), two main compounds in traditional Chinese medicine isolated from Thunder God Vine, have a broad range of bioactivities including anticancer activity. Silk fibroin (SF), a naturally occurring protein with several unique properties, is an ideal carrier material...
August 7, 2017: Nanoscale
https://www.readbyqxmd.com/read/28780757/quinoxaline-dopamine-and-amino-acid-derived-metabolites-from-the-edible-insect-protaetia-brevitarsis-seulensis
#19
JungIn Lee, In Hyun Hwang, Jang Hoon Kim, Mi-Ae Kim, Jae Sam Hwang, Young Ho Kim, MinKyun Na
Edible insects have been reported to produce metabolites showing various pharmacological activities, recently emerging as rich sources of health functional food. In particular, the larvae of Protaetia brevitarsis seulensis (Kolbe) have been used as traditional Korean medicines for treating diverse diseases, such as breast cancer, inflammatory disease, hepatic cancer, liver cirrhosis, and hepatitis. However, only few chemical investigations were reported on the insect larvae. Therefore, the aim of this study was to discover and identify biologically active chemical components of the larvae of P...
August 5, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/28780322/reduction-of-oxidative-damages-induced-by-titanium-dioxide-nanoparticles-correlates-with-induction-of-the-nrf2-pathway-by-gspe-supplementation-in-mice
#20
Linpeng Niu, Mengjiao Shao, Yuan Liu, Jinfeng Hu, Ruofan Li, Heran Xie, Lixiao Zhou, Lei Shi, Rong Zhang, Yujie Niu
Titanium dioxide nanoparticles (TiO2 NPs) are widely used to additives in cosmetics, pharmaceuticals, paints and foods. Recent studies have demonstrated that TiO2 NPs increased the risk of cancer and the mechanism might relate with oxidative stress. Grape seed procyanidin extract (GSPE) is a natural compound which has been demonstrated to possess a wide array of pharmacological and biochemical actions, including anti-inflammatory, anti-carcinogenic, and antioxidant properties. Our data show that GSPE prevents the changes of histopathology and biomarkers in heart, liver and kidney that occur in mice exposed to TiO2 NPs...
August 2, 2017: Chemico-biological Interactions
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