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https://www.readbyqxmd.com/read/28214230/synthesis-and-cytotoxic-activities-of-goniothalamins-and-derivatives
#1
Anja Weber, Katja Döhl, Julia Sachs, Anja C M Nordschild, Dennis Schröder, Andrea Kulik, Thomas Fischer, Lutz Schmitt, Nicole Teusch, Jörg Pietruszka
Substituted goniothalamins containing cyclopropane-groups were efficiently prepared in high yields and good selectivity. Antiproliferative activity was measured on three human cancer cell lines (A549, MCF-7, HBL-100), to show which of the structural elements of goniothalamins is mandatory for cytotoxicity. We found that the configuration of the stereogenic centre of the δ-lactone plays an important role for cytotoxicity. In our studies only (R)-configured goniothalamins showed antiproliferative activity, whereby (R)-configuration accords to natural goniothalamin (R)-1...
February 6, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28213771/a-novel-spiroindoline-targets-cell-cycle-and-migration-via-modulation-of-microtubule-cytoskeleton
#2
Naveen Kumar, Santanu Hati, Parthapratim Munshi, Subhabrata Sen, Seema Sehrawat, Shailja Singh
Natural product-inspired libraries of molecules with diverse architectures have evolved as one of the most useful tools for discovering lead molecules for drug discovery. In comparison to conventional combinatorial libraries, these molecules have been inferred to perform better in phenotypic screening against complicated targets. Diversity-oriented synthesis (DOS) is a forward directional strategy to access such multifaceted library of molecules. From a successful DOS campaign of a natural product-inspired library, recently a small molecule with spiroindoline motif was identified as a potent anti-breast cancer compound...
February 17, 2017: Molecular and Cellular Biochemistry
https://www.readbyqxmd.com/read/28212843/natural-extranuclear-androgen-receptor-ligands-as-endocrine-disruptors-of-cancer-cell-growth
#3
Marilena Kampa, George Notas, Elias Castanas
Even though the term endocrine disruption primarily designates environmental chemicals that can interfere with the action of hormones, in recent years it has been extended to include also plant derived compounds that can reach the human body, naturally, or have been identified and studied as alternative pharmaceutical agents. In fact, for a large number of them, their antihormonal action was appreciated by different traditional herbal medicines. In the present review we report the majority of the plant derived compounds that exhibit an antiandrogenic effect and the known mechanisms of action...
February 14, 2017: Molecular and Cellular Endocrinology
https://www.readbyqxmd.com/read/28209987/targeting-phospholipase-d-in-cancer-infection-and-neurodegenerative-disorders
#4
REVIEW
H Alex Brown, Paul G Thomas, Craig W Lindsley
Lipid second messengers have essential roles in cellular function and contribute to the molecular mechanisms that underlie inflammation, malignant transformation, invasiveness, neurodegenerative disorders, and infectious and other pathophysiological processes. The phospholipase D (PLD) isoenzymes PLD1 and PLD2 are one of the major sources of signal-activated phosphatidic acid (PtdOH) generation downstream of a variety of cell-surface receptors, including G protein-coupled receptors (GPCRs), receptor tyrosine kinases (RTKs) and integrins...
February 17, 2017: Nature Reviews. Drug Discovery
https://www.readbyqxmd.com/read/28209094/attenuation-of-arsenic-trioxide-induced-cardiotoxicity-through-flaxseed-oil-in-experimental-rats
#5
Mathews V Varghese, M Abhilash, Manju Alex, M V Sauganth Paul, A Prathapan, K G Raghu, R Harikumaran Nair
OBJECTIVES: Arsenic trioxide (As2O3) is a potent drug for acute promyelocytic leukaemia, but its clinical trials are allied with some serious adverse events mainly cardiac functional abnormalities. So the objective of our investigation is to identify the cardioprotective action of flaxseed oil (FSO), a natural compound against As2O3 induced cardiotoxicity. METHODS: Male wistar rats were treated with As2O3 (4 mg/kg) to induce cardiotoxicity. FSO (250 and 500 mg/kg) was given in combination with As2O3 for evaluating its cardioprotective efficacy...
February 17, 2017: Redox Report: Communications in Free Radical Research
https://www.readbyqxmd.com/read/28208826/anticancer-activities-of-c18-c19-c20-and-bis-diterpenoid-alkaloids-derived-from-genus-aconitum
#6
REVIEW
Meng-Yue Ren, Qing-Tian Yu, Chun-Yu Shi, Jia-Bo Luo
Cancer is one of the most common lethal diseases, and natural products have been extensively studied as anticancer agents considering their availability, low toxicity, and economic affordability. Plants belonging to the genus Aconitum have been widely used medically in many Asian countries since ancient times. These plants have been proven effective for treating several types of cancer, such as lung, stomach, and liver cancers. The main effective components of Aconitum plants are diterpenoid alkaloids-which are divided into C18-, C19-, C20-, and bis-diterpenoid alkaloids-are reportedly some of the most promising, naturally abundant compounds for treating cancer...
February 13, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28208712/emerging-cytotoxic-alkaloids-in-the-battle-against-cancer-overview-of-molecular-mechanisms
#7
REVIEW
Zeina Habli, Georgio Toumieh, Maamoun Fatfat, Omar Nasser Rahal, Hala Gali-Muhtasib
Considered as the second deadliest disease globally, cancer has captured the attention of researchers who have been trying with perseverance to decode its hidden aspects, to find new prognosis methods, and to develop better and more effective treatments. Plants have continuously offered an excess of unique secondary metabolites with remarkable biological applications. Alkaloids, one of the most abundant metabolites, constitute a large conglomerate of basic heterocyclic nitrogen-containing natural compounds which are normally produced by plants as toxic substances...
February 8, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28207247/ortho-methoxyphenols-as-convenient-oxidative-bioconjugation-reagents-with-application-to-site-selective-heterobifunctional-crosslinkers
#8
Adel M ElSohly, James Irving MacDonald, Nina B Hentzen, Ioana Laura Aanei, Kareem M El Muslemany, Matthew B Francis
The synthesis of complex protein-based bioconjugates has been facilitated greatly by recent developments in chemoselective methods for biomolecular modification. The oxidative coupling of o-aminophenols or catechols with aniline functional groups is chemoselective, mild, and rapid; however, the oxidatively sensitive nature of the electron-rich aromatics and the paucity of commercial sources pose some obstacles to the general use of these reactive strategies. Herein, we identify o-methoxyphenols as air-stable, commercially available derivatives that undergo efficient oxidative couplings with anilines in the presence of periodate as oxidant...
February 16, 2017: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/28206955/grifolin-exhibits-anti-cancer-activity-by-inhibiting-the-development-and-invasion-of-gastric-tumor-cells
#9
Zijian Wu, Ying Li
Grifolin, a natural product isolated from the mushroom Albatrellus confluens, has been reported to be a potent anti-cancer agent in nasopharyngeal carcinoma and osteosarcoma. The data obtained in this study revealed that grifolin is capable of inhibiting the growth and invasion of gastric cancer cells by inducing apoptosis and suppressing the ERK1/2 pathway. Our results support the potent utility of grifolin as an anti-tumor lead compound against gastric cancer cells.
February 10, 2017: Oncotarget
https://www.readbyqxmd.com/read/28202364/fatty-acid-synthase-modern-tumor-cell-biology-insights-into-a-classical-oncology-target
#10
REVIEW
Douglas Buckley, Gregory Duke, Timothy S Heuer, Marie O'Farrell, Allan Wagman, William McCulloch, George Kemble
Decades of preclinical and natural history studies have highlighted the potential of fatty acid synthase (FASN) as a bona fide drug target for oncology. This review will highlight the foundational concepts upon which this perspective is built. Published studies have shown high levels of FASN in patient tumor tissues are present at later stages of disease and this overexpression predicts poor prognosis. Preclinical studies have shown that experimental overexpression of FASN in previously normal cells leads to changes that are critical for establishing a tumor phenotype...
February 12, 2017: Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/28199969/astragalin-induced-cell-death-is-caspase-dependent-and-enhances-the-susceptibility-of-lung-cancer-cells-to-tumor-necrosis-factor-by-inhibiting-the-nf-%C3%B0%C2%BAb-pathway
#11
Minghui Chen, Fangfang Cai, Daolong Zha, Xueshi Wang, Wenjing Zhang, Yan He, Qilai Huang, Hongqin Zhuang, Zi-Chun Hua
Flavonoids are naturally occurring polyphenolic compounds and are among the most promising anticancer agents. Here, we demonstrate that the flavonoid astragalin (AG), also known as kaempferol-3-O-β-D-glucoside, induces cell death. This was prevented by the caspase inhibitors z-DEVD-FMK and z-LEHD-FMK. AG-induced cell death was associated with an increase in the Bax:Bcl-2 ratio and amplified by the inhibition of extracellular signal-regulated kinase (ERK)-1/2 and Akt signaling. Meanwhile, AG suppressed LPS-induced NF-κB activation...
February 10, 2017: Oncotarget
https://www.readbyqxmd.com/read/28198103/synthesis-of-5%C3%AE-8%C3%AE-ergosterol-peroxide-3-carbamate-derivatives-and-fluorescent-mitochondria-targeting-conjugate-for-enhanced-anticancer-activities
#12
Ming Bu, Tingting Cao, Hongxia Li, Mingzhou Guo, Burton B Yang, Chengchu Zeng, Liming Hu
By inspiration of significant anticancer activity of our previously screened natural ergosterol peroxide (1), a series of novel ergosterol peroxide 3-carbamate derivatives were synthesized and characterized. The anti-proliferative activity of synthesized compounds against human hepatocellular carcinoma cells (HepG2, SK-Hep1) and human breast cancer cells (MCF-7, MDA-MB231) were investigated. Compound 3d, 3f and their hydrochloride exhibited significant in vitro anti-proliferative activity against the tested tumor cell lines, with IC50 values ranging from 0...
February 15, 2017: ChemMedChem
https://www.readbyqxmd.com/read/28198062/curcumin-suppresses-lung-cancer-stem-cells-via-inhibiting-wnt-%C3%AE-catenin-and-sonic-hedgehog-pathways
#13
Jian-Yun Zhu, Xue Yang, Yue Chen, Ye Jiang, Shi-Jia Wang, Yuan Li, Xiao-Qian Wang, Yu Meng, Ming-Ming Zhu, Xiao Ma, Cong Huang, Rui Wu, Chun-Feng Xie, Xiao-Ting Li, Shan-Shan Geng, Jie-Shu Wu, Cai-Yun Zhong, Hong-Yu Han
Cancer stem cells (CSCs) are highly implicated in the progression of human cancers. Thus, targeting CSCs may be a promising strategy for cancer therapy. Wnt/β-catenin and Sonic Hedgehog pathways play an important regulatory role in maintaining CSC characteristics. Natural compounds, such as curcumin, possess chemopreventive properties. However, the interventional effect of curcumin on lung CSCs has not been clarified. In the present study, tumorsphere formation assay was used to enrich lung CSCs from A549 and H1299 cells...
February 15, 2017: Phytotherapy Research: PTR
https://www.readbyqxmd.com/read/28197319/structure-based-design-of-non-natural-peptidic-macrocyclic-mcl-1-inhibitors
#14
Jeffrey W Johannes, Stephanie Bates, Carl Beigie, Matthew A Belmonte, John Breen, Shenggen Cao, Paolo A Centrella, Matthew A Clark, John W Cuozzo, Christoph E Dumelin, Andrew D Ferguson, Sevan Habeshian, David Hargreaves, Camil Joubran, Steven Kazmirski, Anthony D Keefe, Michelle L Lamb, Haiye Lan, Yunxia Li, Hao Ma, Scott Mlynarski, Martin J Packer, Philip B Rawlins, Daniel W Robbins, Haidong Shen, Eric A Sigel, Holly H Soutter, Nancy Su, Dawn M Troast, Haiyun Wang, Kate F Wickson, Chengyan Wu, Ying Zhang, Qiuying Zhao, Xiaolan Zheng, Alexander W Hird
Mcl-1 is a pro-apoptotic BH3 protein family member similar to Bcl-2 and Bcl-xL. Overexpression of Mcl-1 is often seen in various tumors and allows cancer cells to evade apoptosis. Here we report the discovery and optimization of a series of non-natural peptide Mcl-1 inhibitors. Screening of DNA-encoded libraries resulted in hit compound 1, a 1.5 μM Mcl-1 inhibitor. A subsequent crystal structure demonstrated that compound 1 bound to Mcl-1 in a β-turn conformation, such that the two ends of the peptide were close together...
February 9, 2017: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28197098/in-vitro-antiproliferative-and-apoptosis-inducing-effect-of-allium-atroviolaceum-bulb-extract-on-breast-cervical-and-liver-cancer-cells
#15
Somayeh Khazaei, Norhaizan M Esa, Vasudevan Ramachandran, Roslida A Hamid, Ashok K Pandurangan, Ali Etemad, Patimah Ismail
Natural products are considered potent sources for novel drug discovery and development. The multiple therapeutic effects of natural compounds in traditional medicine motivate us to evaluate the cytotoxic activity of bulb of Allium atroviolaceum in MCF7 and MDA-MB-231, HeLa and HepG2 cell lines. The bulb methanol extract of A. atroviolaceum was found to be an active cell proliferation inhibitor at the time and dose dependent manner. Determination of DNA content by flow cytometry demonstrated S and G2/M phase arrest of MCF-7 cell, correlated to Cdk1 downregulation, S phase arrest in MDA-MB-231 which is p53 and Cdk1-dependent, sub-G0 cell cycle arrest in HeLa aligned with Cdk1 downregulation, G0/G1, S, G2/M phase arrest in HepG2 which is p53-dependent...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28196522/xpo1-in-b-cell-hematological-malignancies-from-recurrent-somatic-mutations-to-targeted-therapy
#16
REVIEW
Vincent Camus, Hadjer Miloudi, Antoine Taly, Brigitte Sola, Fabrice Jardin
Many recent publications highlight the large role of the pivotal eukaryotic nuclear export protein exportin-1 (XPO1) in the oncogenesis of several malignancies, and there is emerging evidence that XPO1 inhibition is a key target against cancer. The clinical validation of the pharmacological inhibition of XPO1 was recently achieved with the development of the selective inhibitor of nuclear export compounds, displaying an interesting anti-tumor activity in patients with massive pre-treated hematological malignancies...
February 14, 2017: Journal of Hematology & Oncology
https://www.readbyqxmd.com/read/28195671/trachycladines-and-analogues-synthesis-and-anti-cancer-activity-evaluation
#17
Zisis V Peitsinis, Achilleas G Mitrakas, Eirini A Nakiou, Dafni A Melidou, Dimitra Kalamida, Christos Kakouratos, Michael I Koukourakis, Alexandros E Koumbis
The synthesis of four new analogues of marine nucleoside trachycladine A was accomplished via direct regio- and stereoselective Vorbrüggen glycosylations of 2,6-dichloropurine and 2-chloropurine with a D-ribose derived chiron. Naturally occurring trachycladines (A and B) and a series of analogues were examined for their cytotoxic activity against a number of cancer cell lines (glioblastoma, lung and cervical cancer). Parent trachycladine A and two analogues (the diacetate of 2,6-dichloropurine derivative and N-cyclopropyl trachycladine A) were found to result in a significant reduction of cell viability, with the latter exhibiting a stronger effect...
February 14, 2017: ChemMedChem
https://www.readbyqxmd.com/read/28192510/downregulation-of-sp1-by-minnelide-leads-to-decrease-in-hsp70-and-decrease-in-tumor-burden-of-gastric-cancer
#18
Nivedita Arora, Osama Alsaied, Patricia Dauer, Kaustav Majumder, Shrey Modi, Bhuwan Giri, Vikas Dudeja, Sulagna Banerjee, Daniel Von Hoff, Ashok Saluja
BACKGROUND: Gastric cancer is the third leading cause of cancer related mortality worldwide with poor survival rates. Even though a number of chemotherapeutic compounds have been used against this disease, stomach cancer has not been particularly sensitive to these drugs. In this study we have evaluated the effect of triptolide, a naturally derived diterpene triepoxide and its water soluble pro-drug Minnelide on several gastric adenocarcinoma cell lines both as monotherapy and in combination with CPT-11...
2017: PloS One
https://www.readbyqxmd.com/read/28191652/goniothalamin-and-celecoxib-effects-during-aging-targeting-pro-inflammatory-mediators-in-chemoprevention-of-prostatic-disorders
#19
Larissa Akemi Kido, Fabio Montico, Débora Barbosa Vendramini-Costa, Ronaldo Aloise Pilli, Valeria Helena Alves Cagnon
BACKGROUND: Prostate is highly affected by aging, which lead to inflammatory disorders that can predispose to cancer development. Chemoprevention has emerged as a new therapeutic approach, intensifying studies evaluating the biological properties of new compounds. The aim of this study was to characterize the inflammatory responses in the prostate ventral lobe from senile mice treated with Goniothalamin (GTN), a promising natural compound with anti-inflammatory and antiproliferative properties...
February 13, 2017: Prostate
https://www.readbyqxmd.com/read/28188066/synthesis-and-in-vitro-evaluation-of-sg3227-a-pyrrolobenzodiazepine-dimer-antibody-drug-conjugate-payload-based-on-sibiromycin
#20
Gary C Kemp, Arnaud C Tiberghien, Neki V Patel, Francois D'Hooge, Sanjay M Nilapwar, Lauren R Adams, Simon Corbett, David G Williams, John A Hartley, Philip W Howard
A novel pyrrolobenzodiazepine dimer payload, SG3227, was rationally designed based on the naturally occurring antitumour compound sibiromycin. SG3227 was synthesized from a dimeric core in an efficient fashion. An unexpected room temperature Diels-Alder reaction occurred during the final step of the synthesis and was circumvented by use of an iodoacetamide conjugation moiety in place of a maleimide. The payload was successfully conjugated to trastuzumab and the resulting ADC exhibited potent activity against a HER2-expressing human cancer cell line in vitro...
January 30, 2017: Bioorganic & Medicinal Chemistry Letters
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