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https://www.readbyqxmd.com/read/28441013/cytotoxicity-of-pyrazine-based-cyclometalated-c-n-pz-c-au-iii-carbene-complexes-impact-of-the-nature-of-the-ancillary-ligand-on-the-biological-properties
#1
Benoît Bertrand, Julio Fernandez-Cestau, Jesus Angulo, Marco M D Cominetti, Zoë A E Waller, Mark Searcey, Maria A O'Connell, Manfred Bochmann
The synthesis of a series of cyclometalated gold(III) complexes supported by pyrazine-based (C^N^C)-type pincer ligands is reported, including the crystal structure of a cationic example. The compounds provide a new platform for the study of antiproliferative properties of gold(III) complexes. Seven complexes were tested: the neutral series (C^N(pz)^C)AuX [X = Cl (1), 6-thioguanine (4), C≡CPh (5), SPh (6)] and an ionic series that included the N-methyl complex [(C^N(pzMe)^C)AuCl]BF4 (7) and the N-heterocyclic carbene complexes [(C^N(pz)^C)AuL](+) with L = 1,3-dimethylbenzimidazol-2-ylidene (2) or 1,3,7,9-tetramethylxanthin-8-ylidene (3)...
April 25, 2017: Inorganic Chemistry
https://www.readbyqxmd.com/read/28440433/effective-cytotoxic-activity-of-osw-1-on-colon-cancer-by-inducing-apoptosis-in%C3%A2-vitro-and-in%C3%A2-vivo
#2
Yanhong Zhang, Fengqi Fang, Kai Fan, Yanli Zhang, Jie Zhang, Huishu Guo, Peiyao Yu, Jianmei Ma
As a natural compound, Ornithogalum caudatum Ait is primarily used as an anti-inflammatory and antitumor agent in Chinese folk medicine. In 1992, OSW-1 was isolated from this compound, which is a new member of cholestane saponin family. In numerous recent studies, OSW-1 has been shown to have powerful cytotoxic anticancer effects against various malignant cells. However, the therapeutic efficacy of OSW-1 on colon cancer and the underlying mechanism are not understood. To explore the mechanism underlying OSW-1 in antitumor therapy, a therapeutic function analysis of OSW-1 on colon cancer was performed in vitro and in vivo...
April 19, 2017: Oncology Reports
https://www.readbyqxmd.com/read/28440207/epithelial-mesenchymal-transition-in-cancer-progression-preventive-phytochemicals
#3
Soorya Parathodi Illam, Arunaksharan Narayanankutty, Shaji Edappilly Mathew, Remya Valsalakumari, Rosemol M Jacob, Achuthan Chathrattil Raghavamenon
BACKGROUND: Epithelial-Mesenchymal Transition (EMT) is the conversion of epithelial cells into mesenchymal phenotype generally observed during embryogenesis and wound healing as well as in malignant transformation. Several signaling pathways and transcription factors associated with EMT have been explored. Dietary phytochemicals are multi-targeted agents that interfere with these pathways, assume preventive potential against pathologic EMT. OBJECTIVE: Present review aims to provide a detailed description on the nature, characteristics of EMT in physiological and pathophysiological conditions and the scope of phytochemicals in its prevention...
April 24, 2017: Recent Patents on Anti-cancer Drug Discovery
https://www.readbyqxmd.com/read/28439316/epigenetic-assays-for-chemical-biology-and-drug-discovery
#4
REVIEW
Sheraz Gul
The implication of epigenetic abnormalities in many diseases and the approval of a number of compounds that modulate specific epigenetic targets in a therapeutically relevant manner in cancer specifically confirms that some of these targets are druggable by small molecules. Furthermore, a number of compounds are currently in clinical trials for other diseases including cardiovascular, neurological and metabolic disorders. Despite these advances, the approved treatments for cancer only extend progression-free survival for a relatively short time and being associated with significant side effects...
2017: Clinical Epigenetics
https://www.readbyqxmd.com/read/28439094/selective-targeting-of-cancer-cells-by-oxidative-vulnerabilities-with-novel-curcumin-analogs
#5
Christopher Pignanelli, Dennis Ma, Megan Noel, Jesse Ropat, Fadi Mansour, Colin Curran, Simon Pupulin, Kristen Larocque, Jianzhang Wu, Guang Liang, Yi Wang, Siyaram Pandey
Recently, research has focused on targeting the oxidative and metabolic vulnerabilities in cancer cells. Natural compounds like curcumin that target such susceptibilities have failed further clinical advancements due to the poor stability and bioavailability as well as the need of high effective doses. We have synthesized and evaluated the anti-cancer activity of several monocarbonyl analogs of curcumin. Interestingly, two novel analogs (Compound A and I) in comparison to curcumin, have increased chemical stability and have greater anti-cancer activity in a variety of human cancer cells, including triple-negative, inflammatory breast cancer cells...
April 24, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28436164/synthesis-and-sar-study-of-novel-anticancer-protoflavone-derivatives-investigation-of-cytotoxicity-and-interaction-with-the-abcb1-and-abcg2-multidrug-efflux-transporters
#6
Balázs Dankó, Szilárd Tóth, Ana Martins, Vágvölgyi Máté, Norbert Kúsz, Joseph Molnár, Fang-Rong Chang, Yang-Chang Wu, Gergely Szakács, Attila Hunyadi
There is a constant need for new therapies against multidrug resistant (MDR) cancer. Natural compounds represent a promising class of novel anticancer agents. Recently, we have shown that protoflavones display activity in multidrug resistant cancer cell lines overexpressing the drug efflux pump P-glycoprotein. In the present study, 52 protoflavones, including 22 new derivatives were synthesized and tested against a panel of sensitive parental cells and their MDR derivatives obtained by transfection with the human ABCB1 or ABCG2 genes, or by adaptation to chemotherapeutics...
April 23, 2017: ChemMedChem
https://www.readbyqxmd.com/read/28435333/new-insights-into-therapeutic-activity-and-anticancer-properties-of-curcumin
#7
REVIEW
Abir Kumar Panda, Dwaipayan Chakraborty, Irene Sarkar, Tila Khan, Gaurisankar Sa
Natural compounds obtained from plants are capable of garnering considerable attention from the scientific community, primarily due to their ability to check and prevent the onset and progress of cancer. These natural compounds are primarily used due to their nontoxic nature and the fewer side effects they cause compared to chemotherapeutic drugs. Furthermore, such natural products perform even better when given as an adjuvant along with traditional chemotherapeutic drugs, thereby enhancing the potential of chemotherapeutics and simultaneously reducing their undesired side effects...
2017: Journal of Experimental Pharmacology
https://www.readbyqxmd.com/read/28435252/polyphenol-nanoformulations-for-cancer-therapy-experimental-evidence-and-clinical-perspective
#8
REVIEW
Yasamin Davatgaran-Taghipour, Salar Masoomzadeh, Mohammad Hosein Farzaei, Roodabeh Bahramsoltani, Zahra Karimi-Soureh, Roja Rahimi, Mohammad Abdollahi
Cancer is defined as the abnormal cell growth that can cause life-threatening malignancies with high financial costs for patients as well as the health care system. Natural polyphenols have long been used for the prevention and treatment of several disorders due to their antioxidant, anti-inflammatory, cytotoxic, antineoplastic, and immunomodulatory effects discussed in the literature; thus, these phytochemicals are potentially able to act as chemopreventive and chemotherapeutic agents in different types of cancer...
2017: International Journal of Nanomedicine
https://www.readbyqxmd.com/read/28434764/novel-non-trimethoxylphenyl-piperlongumine-derivatives-selectively-kill-cancer-cells
#9
Youjun Zhang, Hao Ma, Yuelin Wu, Zhongli Wu, Zhengguang Yao, Wannian Zhang, Chunlin Zhuang, Zhenyuan Miao
Piperlongumine (PL) is a natural alkaloid with broad biological activities. Twelve analogues have been designed and synthesized with non-substituted benzyl rings or heterocycles in this work. Most of the compounds showed better anticancer activities than the parent PL without apparent toxicity in normal cells. Elevation of cellular ROS levels was one of the main anticancer mechanisms of these compounds. Cell apoptosis and cell cycle arrest for the best compound ZM90 were evaluated and similar mechanism of action with PL was demonstrated...
April 13, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28427809/picrasidine-g-decreases-viability-of-mda-mb-468-egfr-overexpressing-triple-negative-breast-cancer-cells-through-inhibition-of-egfr-stat3-signaling-pathway
#10
Naoya Yamashita, Manami Kondo, Shuai Zhao, Wei Li, Kazuo Koike, Kiyomitsu Nemoto, Yuichiro Kanno
Targeted therapy is unavailable for treating patients with triple-negative breast cancer (TNBC), which accounts for approximately 15% of all breast cancers. Overexpression of epidermal growth factor receptor (EGFR) is observed in approximately 30-60% of TNBCs. Therefore, developing novel strategies for inhibiting EGFR signaling is required. In the present study, a natural compound library was screened to identify molecules that target TNBCs that overexpress EGFR. Picrasidine G (PG), a naturally occurring dimeric alkaloid produced by Picrasma quassioides, decreased the viability of the MDA-MB 468 cell line (TNBC(EGFR+)) compared with other breast cancer cell lines...
March 23, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28427230/deguelin-inhibits-non-small-cell-lung-cancer-via-down-regulating-hexokinases-ii-mediated-glycolysis
#11
Wei Li, Feng Gao, Xiaoqian Ma, Ruike Wang, Xin Dong, Wei Wang
Hexokinases II (HK2) is a hub in the regulation of cancer cell glycolysis. Here we reported deguelin, a natural compound which has been studied in various tumor types, has a profound anti-tumor effect on human non-small cell lung cancer (NSCLC) via directly down-regulating of glycolysis. In NSCLC cell lines and primary NSCLC tissue, we found HK2 is overexpressed. Deguelin treatment markedly inhibited anchorage-dependent and independent growth of NSCLC cell lines. We revealed that deguelin exposure impaired glucose metabolism by inhibiting Akt-mediated Hexokinase II expression, overexpression of constitutively activated Akt1 substantially rescued deguelin-induced glycolysis suppression...
March 6, 2017: Oncotarget
https://www.readbyqxmd.com/read/28425857/antioxidant-properties-of-fractions-for-unripe-fruits-of-capsicum-annuum-l-var-conoides
#12
Chung-Yi Chen, Ching-Yu Yen, Gao-Mai Shen, Tzu-Jung Yu, Yi-Shin Liao, Ru-In Jian, Sheng-Chieh Wang, Jen-Yang Tang, H-W Chang
BACKGROUND: Capsicum plant, especially for C. annuum, is an abundant resource for bioactive antioxidants, but few studies have examined the unripe fruit part of the Capsicum plant. OBJECTIVE: MeOH extract of unripe fruits of C. annuum L. var. conoides (UFCA) was chromatographed over a silica gel column using a gradient of CH2Cl2/MeOH as eluent to produce 9 fractions. Antioxidant activities are evaluated along with cell viabilities of 9 fractions of UFCA. METHOD: The antioxidant properties were analyzed in terms of total phenol content (TPC), total flavonoid content (TFC), 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging, 2,2-azinobis (3-ethyl-benzothiazoline-6-sulfonic acid) (ABTS) radical scavenging, ferric reducing, and ferrous ion-chelating ability...
April 19, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28423064/biochemical-evaluation-of-the-anticancer-potential-of-the-polyamine-based-nanocarrier-nano11047
#13
Tracy Murray-Stewart, Elena Ferrari, Ying Xie, Fei Yu, Laurence J Marton, David Oupicky, Robert A Casero
Synthesizing polycationic polymers directly from existing drugs overcomes the drug-loading limitations often associated with pharmacologically inert nanocarriers. We recently described nanocarriers formed from a first-generation polyamine analogue, bis(ethyl)norspermine (BENSpm), that could simultaneously target polyamine metabolism while delivering therapeutic nucleic acids. In the current study, we describe the synthesis and evaluation of self-immolative nanocarriers derived from the second-generation polyamine analogue PG-11047...
2017: PloS One
https://www.readbyqxmd.com/read/28422286/isorhapontigenin-induced-cell-growth-inhibition-and-apoptosis-by-targeting-egfr-related-pathways-in-prostate-cancer
#14
Cuicui Zhu, Qingyi Zhu, Zhaomeng Wu, Yingying Yin, Dan Kang, Shan Lu, Ping Liu
Isorhapontigenin (ISO), a naturally phytopolyphenol compound existing in Chinese herb, apples and various vegetables, has attracted extensive interest in recent years for its diverse pharmacological characteristics. Increasing evidences reveal that ISO can inhibit cancer cell growth by induced apoptosis, however the molecular mechanisms is not fully understood. In this study, we found for the first time that ISO apparently induced cell growth inhibition and apoptosis by targeting EGFR and its downstream signal pathways in prostate cancer (PCa) cells both in vitro and in vivo, whereas no obviously effect on normal prostate cells...
April 19, 2017: Journal of Cellular Physiology
https://www.readbyqxmd.com/read/28419927/synthesis-and-evaluation-of-anti-plasmodial-and-cytotoxic-activities-of-epoxyazadiradione-derivatives
#15
P Ashok Yadav, Ch Pavan Kumar, Bandi Siva, K Suresh Babu, Aparna Devi Allanki, Puran Singh Sijwali, Nishant Jain, A Veerabhadra Rao
Epoxyazadiradione (1), a major compound derived from Neem oil, showed modest anti-plasmodial activity against CQ-resistant and CQ-sensitive strains of the most virulent human malaria parasite P. falciparum. A series of analogues were synthesized by modification of the key structural moieties of this high yield natural product. Out of the library of all compounds tested, compounds 3c and 3g have showed modest anti-plasmodial activity against CQ-sensitive (IC50 2.8 ± 0.29 μM and 1.5 ± 0.01 μM) and CQ-resistant strains (IC50 1...
April 13, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28418619/determination-of-lipoic-acid-in-human-urine-by-capillary-zone-electrophoresis
#16
Paweł Kubalczyk, Rafał Głowacki
Fast, simple and accurate CE method enabling determination of lipoic acid (LA) in human urine has been developed and validated. LA is a disulfide-containing natural compound absorbed from the organism's diet. Due to powerful antioxidant activity, LA has been used for prevention and treatment of various diseases and disorders, e.g. cardiovascular diseases, neurodegenerative disorders and cancer. The proposed analytical procedure consists of liquid-liquid sample extraction, reduction of LA with tris(2-carboxyethyl)phosphine, derivatization with 1-benzyl-2-chloropyridinium bromide (BCPB) followed by field amplified sample injection stacking, capillary zone electrophoresis separation and ultraviolet-absorbance detection of LA-BCPB derivative at 322 nm...
April 18, 2017: Electrophoresis
https://www.readbyqxmd.com/read/28418248/total-synthesis-configuration-assignment-and-cytotoxic-activity-evaluation-of-protulactone-a
#17
Martin Markovič, Peter Koóš, Tomáš Čarný, Saskia Sokoliová, Nikola Boháčiková, Ján Moncol, Tibor Gracza
The first total synthesis and absolute configuration assignment of protulactone A (1) has been achieved. Four stereoisomers, 1a, ent-1a, 1b, and ent-1b, of this natural polyketide were prepared by chiral pool synthesis starting from l- and d-arabinose, respectively. The absolute and relative configurations of all isomers were assigned by single-crystal X-ray analysis. Target compounds were screened for their in vitro cytotoxicity toward certain human tumor cells (NCI60 cancer cell line panel).
April 18, 2017: Journal of Natural Products
https://www.readbyqxmd.com/read/28416754/unique-synergistic-formulation-of-curcumin-epicatechin-gallate-and-resveratrol-tricurin-suppresses-hpv-e6-eliminates-hpv-cancer-cells-and-inhibits-tumor-progression
#18
Sumit Mukherjee, Priya Ranjan Debata, Rahman Hussaini, Kaushiki Chatterjee, Juliet N E Baidoo, Samay Sampat, Anita Szerszen, Joseph P Navarra, Jimmie Fata, Elena Severinova, Probal Banerjee, Mario R Castellanos
Curcumin (from curry) (C) is highly potent against cervical cancer cells (CCC), but poor bioavailability has limited its clinical use. Similar natural polyphenols resveratrol (from grapes) (R), and epicatechin gallate (from green tea) (E) also display activity against CCC. By treating CCC (HeLa) with C, E, or R, or combinations of these compounds, we computed combination indices and observed a strong synergism among C, E, and R at the unique molar ratio 4:1:12.5. This combination, named as TriCurin, rapidly down regulated HPV18 E6 and NF-kB expression while concomitantly inducing the tumor suppressor protein p53 in HeLa cells...
March 29, 2017: Oncotarget
https://www.readbyqxmd.com/read/28414793/radiosensitizing-effect-of-diosmetin-on-radioresistant-lung-cancer-cells-via-akt-signaling-pathway
#19
Zhijie Xu, Yuanliang Yan, Lingfang Xiao, Shuang Dai, Shuangshuang Zeng, Long Qian, Lin Wang, Xue Yang, Yi Xiao, Zhicheng Gong
Radiotherapy is a powerful tool in the treatment of cancer that has the advantage of preserving normal tissues. However, tumor radioresistance currently remains a major impediment to effective RT. Thus, exploring effective radiation sensitizers is urgently needed. In this study, we have shown that diosmetin, the aglycone of the lavonoid glycoside from olive leaves, citrus fruits and some medicinal herbs, has a promising effect on radiotherapy sensitization. In our results, DIO could induce G1 phase arrest and thus enhance the radiosensitivity of radioresistant A549/IR lung cancer cells...
2017: PloS One
https://www.readbyqxmd.com/read/28414767/the-fungal-natural-product-azaphilone-9-binds-to-hur-and-inhibits-hur-rna-interaction-in-vitro
#20
Kawaljit Kaur, Xiaoqing Wu, James K Fields, David K Johnson, Lan Lan, Miranda Pratt, Amber D Somoza, Clay C C Wang, John Karanicolas, Berl R Oakley, Liang Xu, Roberto N De Guzman
The RNA-binding protein Hu antigen R (HuR) binds to AU-rich elements (ARE) in the 3'-untranslated region (UTR) of target mRNAs. The HuR-ARE interactions stabilize many oncogenic mRNAs that play important roles in tumorigenesis. Thus, small molecules that interfere with the HuR-ARE interaction could potentially inhibit cancer cell growth and progression. Using a fluorescence polarization (FP) competition assay, we identified the compound azaphilone-9 (AZA-9) derived from the fungal natural product asperbenzaldehyde, binds to HuR and inhibits HuR-ARE interaction (IC50 ~1...
2017: PloS One
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