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https://www.readbyqxmd.com/read/28211616/design-synthesis-and-biological-evaluation-of-chalcone-containing-shikonin-derivatives-as-inhibitors-of-tubulin-polymerization
#1
Han-Yue Qiu, Fang Wang, Xue Wang, Wen-Xue Sun, Jin-Liang Qi, Yan-Jun Pang, Rong-Wu Yang, Gui-Hua Lu, Xiao-Ming Wang, Yong-Hua Yang
The biological importance of microtubules in mitosis makes them an interesting target for the development of anticancer agents. In this study, a series of novel chalcone-containing shikonin derivatives was designed, synthesized, and evaluated for biological activities. Among them, derivative PMMB-259 [(R)-1-(5,8-dihydroxy-1,4-dioxo-1,4-dihydronaphthalen-2-yl)-4-methylpent-3-en-1-yl (E)-2-(4-(3-oxo-3-(3-(trifluoromethoxy)phenyl)prop-1-en-1-yl)phenoxy)acetate] was identified as a potent inhibitor of tubulin polymerization...
February 17, 2017: ChemMedChem
https://www.readbyqxmd.com/read/28140740/comparison-of-some-secondary-metabolite-content-in-the-seventeen-species-of-the-boraginaceae-family
#2
Sławomir Dresler, Grażyna Szymczak, Małgorzata Wójcik
CONTEXT: The Boraginaceae family comprises plants that have important therapeutic and cosmetic applications. Their pharmacological effect is related to the presence of naphthaquinones, flavonoids, terpenoids, phenols, or purine derivative - allantoin. OBJECTIVE: In the present study, comparison of some secondary metabolite content and phytochemical relationship between 17 species of the Boraginaceae family were analyzed. MATERIALS AND METHODS: High performance capillary electrophoresis (HPCE) was used to perform a chemometric analysis in the following Boraginaceae species: Anchusa azurea Mill...
December 2017: Pharmaceutical Biology
https://www.readbyqxmd.com/read/28108311/rip1-and-rip3-contribute-to-shikonin-induced-dna-double-strand-breaks-in-glioma-cells-via-increase-of-intracellular-reactive-oxygen-species
#3
Zijian Zhou, Bin Lu, Chen Wang, Zongqi Wang, Tianfei Luo, Meihua Piao, Fankai Meng, Guangfan Chi, Yinan Luo, Pengfei Ge
Shikonin has been reported to induce glioma cell death via necroptosis, a type of programmed necrosis primarily mediated by RIP1 and RIP3. Although RIP1 and RIP3 are found to regulate some features of necrosis such as energy depletion and cellular membrane disruption, it remains unclear whether RIP1 and RIP3 could modulate DNA double strand breaks (DSBs), which is a crucial event leading to chromatinolysis. In this study, we used glioma cell lines and mice model of xenograft glioma to investigate the roles of RIP1 and RIP3 in shikonin-induced DNA DSBs...
April 1, 2017: Cancer Letters
https://www.readbyqxmd.com/read/28088387/sirt2-mediated-antitumor-effects-of-shikonin-on-metastatic-colorectal-cancer
#4
Li-Li Zhang, Lin Zhan, Yong-Dong Jin, Zhen-Li Min, Can Wei, Qiang Wang, Ya-Jun Chen, Qing-Ming Wu, Xia-Min Hu, Qiong Yuan
SIRT2 is involved in the development of a variety of cancers. Shikonin is a natural compound that is known to have antitumor effects. This study aims to assess the effects of shikonin on the development and metastatic progression of colorectal cancer (CRC) through regulation of SIRT2 expression and whether this effect is related to the phosphorylation of extracellular signal-regulated kinases (ERKs). The results demonstrated that SIRT2 is downregulated in CRC biopsy samples (n=31) compared with the adjacent non-cancerous tissues (ANCT, n=26)...
January 12, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28069896/anti-tumor-effects-of-shikonin-derivatives-on-human-medullary-thyroid-carcinoma-cells
#5
Carina Hasenoehrl, Gert Schwach, Nassim Ghaffari-Tabrizi-Wizsy, Robert Fuchs, Nadine Kretschmer, Rudolf Bauer, Roswitha Pfragner
New treatment options are needed for medullary thyroid carcinoma (MTC), a highly metastasizing neuroendocrine tumor that is resistant to standard radio- and chemotherapy. We show that the following shikonin derivatives inhibit cell proliferation and cell viability of the MTC cell line TT: acetylshikonin, β,β-dimethylacrylshikonin, shikonin and a petroleum ether extract of the roots of Onosma paniculata containing several shikonin derivatives. The unsubstituted shikonin derivative was found to be the most effective compound with an IC50 of 1...
January 9, 2017: Endocrine Connections
https://www.readbyqxmd.com/read/28040409/antifungal-effects-of-phytocompounds-on-candida-species-alone-and-in-combination-with-fluconazole
#6
REVIEW
Mengjiao Lu, Tao Li, Jianjian Wan, Xiuyun Li, Lei Yuan, Shujuan Sun
Invasive fungal infections caused by Candida spp. remain the most predominant nosocomial fungal infections. Owing to the increased use of antifungal agents, resistance of Candida spp. to antimycotics has emerged frequently, especially to fluconazole (FLC). To cope with this issue, new efforts have been dedicated to discovering novel antimycotics or new agents that can enhance the susceptibility of Candida spp. to existing antimycotics. The secondary metabolites of plants represent a large library of compounds that are important sources for new drugs or compounds suitable for further modification...
December 15, 2016: International Journal of Antimicrobial Agents
https://www.readbyqxmd.com/read/28006752/regulation-of-mirnas-by-herbal-medicine-an-emerging-field-in-cancer-therapies
#7
REVIEW
Ali Mohammadi, Behzad Mansoori, Behzad Baradaran
MicroRNAs' expression profiles have recently gained major attention as far as cancer research is concerned. MicroRNAs are able to inhibit target gene expression via binding to the 3' UTR of target mRNA, resulting in target mRNA cleavage or translation inhibition. MicroRNAs play significant parts in a myriad of biological processes; studies have proven, on the other hand, that aberrant microRNA expression is, more often than not, associated with the growth and progression of cancers. MicroRNAs could act as oncogenes (oncomir) or tumor suppressors and can also be utilized as biomarkers for diagnosis, prognosis, and cancer therapy...
February 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/27990691/synthesis-and-evaluation-of-new-naphthalene-and-naphthoquinone-derivatives-as-anticancer-agents
#8
Giovanni L Beretta, Giovanni Ribaudo, Ileana Menegazzo, Rosanna Supino, Giovanni Capranico, Franco Zunino, Giuseppe Zagotto
DNA topoisomerase I inhibitors, both synthetic and of natural origin, are receiving increasing consideration primarily as drugs against refractory tumors. Alkannin and shikonin, two enantiomeric dyes from Alkanna tinctoria and Lithospermum erythrorhizon, have been known over many centuries as dyestuff, wound healing, anti-inflammatory, antibacterial and antitumor substances. Although multiple mechanisms appear to be implicated, their potency is associated with the inhibition of topoisomerase I and with the redox properties of the naphthazarin scaffold...
December 19, 2016: Archiv der Pharmazie
https://www.readbyqxmd.com/read/27976094/shikonin-reduces-the-tumour-formation-and-il-17-in-a-model-of-colorectal-cancer-associated-to-chronic-colitis-in-c57bl-6-mice
#9
J L Ríos, E Giner, R M Giner, S Máñez, M C Recio
No abstract text is available yet for this article.
December 2016: Planta Medica
https://www.readbyqxmd.com/read/27975397/metabolic-profiling-study-of-shikonin-s-inhibitory-effect-on-cancer-cell-lines
#10
E D Spyrelli, C Virgiliou, A E Koletti, H Gika, G Mossialos, V P Papageorgiou, A N Assimopoulou
No abstract text is available yet for this article.
December 2016: Planta Medica
https://www.readbyqxmd.com/read/27943122/shikonin-inhibits-tnf-%C3%AE-production-through-suppressing-pkc-nf-%C3%AE%C2%BAb-dependent-decrease-of-il-10-in-rheumatoid-arthritis-like-cell-model
#11
Wen-Xiao Sun, Yan Liu, Wei Zhou, He-Wei Li, Jian Yang, Zhen-Bing Chen
Shikonin, a major effective component in the Chinese herbal medicine Lithospermum erythrorhizon Sieb., exhibits an anti-inflammatory property towards rheumatoid arthritis (RA), but the potential mechanism is unclear. Our aim was to investigate the mechanism of shikonin on the lipopolysaccharide (LPS)-induced fibroblast-like synoviocyte (LiFLS) inflammation model. Fibroblast-like synoviocytes (FLSs) were treated with 200 μg/ml of LPS for 24 h to establish the RA-like model, LiFLS. FLSs were pretreated with shikonin (0...
December 9, 2016: Journal of Natural Medicines
https://www.readbyqxmd.com/read/27905569/shikonin-induces-mitochondria-mediated-apoptosis-and-enhances-chemotherapeutic-sensitivity-of-gastric-cancer-through-reactive-oxygen-species
#12
Wenquan Liang, Aizhen Cai, Guozhu Chen, Hongqing Xi, Xiaosong Wu, Jianxin Cui, Kecheng Zhang, Xudong Zhao, Jiyun Yu, Bo Wei, Lin Chen
The prognosis of gastric cancer remains poor due to clinical drug resistance. Novel drugs are urgently needed. Shikonin (SHK), a natural naphthoquinone, has been reported to trigger cell death and overcome drug resistance in anti-tumour therapy. In this study, we investigated the effectiveness and molecular mechanisms of SHK in treatment with gastric cancer. In vitro, SHK suppresses proliferation and triggers cell death of gastric cancer cells but leads minor damage to gastric epithelial cells. SHK induces the generation of intracellular reactive oxygen species (ROS), depolarizes the mitochondrial membrane potential (MMP) and ultimately triggers mitochondria-mediated apoptosis...
December 1, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27903739/homocysteine-activates-b-cells-via-regulating-pkm2-dependent-metabolic-reprogramming
#13
Jiacheng Deng, Silin Lü, Huiying Liu, Bo Liu, Changtao Jiang, Qingbo Xu, Juan Feng, Xian Wang
The overactivation of immune cells plays an important role in the pathogenesis of hyperhomocysteinemia (HHcy)-accelerated atherosclerosis. Homocysteine (Hcy) activates B cell proliferation and Ab secretion; however, the underlying mechanisms for these effects remain largely unknown. Metabolic reprogramming is critical for lymphocyte activation and effector function. In this study, we showed that Hcy-activated B cells displayed an increase in both oxidative phosphorylation and glycolysis, with a tendency to shift toward the latter, as well as an accumulation of intermediates in the pentose phosphate pathway, to provide energy and biosynthetic substrates for cell growth and function...
January 1, 2017: Journal of Immunology: Official Journal of the American Association of Immunologists
https://www.readbyqxmd.com/read/27864022/shikonin-inhibits-gefitinib-resistant-non-small-cell-lung-cancer-by-inhibiting-trxr-and-activating-the-egfr-proteasomal-degradation-pathway
#14
Xia Li, Xing-Xing Fan, Ze-Bo Jiang, Wings Ty Loo, Xiao-Jun Yao, Elaine Lai-Han Leung, Louis Wc Chow, Liang Liu
Non-small cell lung cancer (NSCLC) is the dominant type of lung cancer. Molecular targeting has highly improved the treatment efficacy of lung cancer, but new challenges have emerged, such as gefitinib-resistance and cancer recurrence. Therefore, new chemotherapeutic agents and treatment strategies are urgently needed. Shikonin is the main active component of a Chinese medicinal plant 'Zi Cao', which has been shown to exhibit powerful anti-cancer activity in certain types of cancer; however, its activity in gefitinib-resistant lung cancer has never been addressed...
January 2017: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
https://www.readbyqxmd.com/read/27855956/selected-secondary-metabolites-in-echium-vulgare-l-populations-from-nonmetalliferous-and-metalliferous-areas
#15
Sławomir Dresler, Ewelina Rutkowska, Wiesław Bednarek, Grzegorz Stanisławski, Tomasz Kubrak, Anna Bogucka-Kocka, Małgorzata Wójcik
The aim of this study was to evaluate the effect of severe environmental conditions prevailing on metalliferous waste heaps and heavy metal-contaminated growth substrates on accumulation of selected secondary metabolites, antioxidant capacity, and heavy metal concentration in two metallicolous (MC, MZ) and one nonmetallicolous (NM) populations of Echium vulgare L. The shoots and the roots of the three studied populations were collected from their natural habitats. Additionally, the plants were cultivated on different growth substrates, i...
January 2017: Phytochemistry
https://www.readbyqxmd.com/read/27793648/shikonin-regulates-c-myc-and-glut1-expression-through-the-mst1-yap1-tead1-axis
#16
Karel Vališ, Pavel Talacko, Valéria Grobárová, Jan Černý, Petr Novák
The general mechanism underlying the tumor suppressor activity of the Hippo signaling pathway remains unclear. In this study, we explore the molecular mechanisms connecting the Hippo signaling pathway with glucose metabolism. We have found that two key regulators of glycolysis, C-MYC and GLUT1, are targets of the Hippo signaling pathway in human leukemia cells. Our results revealed that activation of MST1 by the natural compound shikonin inhibited the expression of GLUT1 and C-MYC. Furthermore, RNAi experiments confirmed the regulation of GLUT1 and C-MYC expression via the MST1-YAP1-TEAD1 axis...
October 25, 2016: Experimental Cell Research
https://www.readbyqxmd.com/read/27746419/the-serum-pdgf-dependent-melanogenic-role-of-the-minute-level-of-the-oncogenic-kinase-pak1-in-melanoma-cells-proven-by-the-highly-sensitive-kinase-assay
#17
Pham Thi Be Tu, Binh Cao Quan Nguyen, Shinkichi Tawata, Cheong-Yong Yun, Eung Gook Kim, Hiroshi Maruta
We previously demonstrated that the oncogenic kinase PAK4, which both melanomas and normal melanocytes express at a very high level, is essential for their melanogenesis. In the present study, using the highly sensitive "Macaroni-Western" (IP-ATP-Glo) kinase assay, we investigated the melanogenic potential of another oncogenic kinase PAK1, which melanoma (B16F10) cells express only at a very minute level. After transfecting melanoma cells with PAK1-shRNA for silencing PAK1 gene, melanin content, tyrosinase activity, and kinase activity of PAK1 were compared between the wild-type and transfectants...
October 17, 2016: Drug Discoveries & Therapeutics
https://www.readbyqxmd.com/read/27703516/shikonin-inhibits-inflammation-and-chondrocyte-apoptosis-by-regulation-of-the-pi3k-akt-signaling-pathway-in-a-rat-model-of-osteoarthritis
#18
Daijie Fu, Xifu Shang, Zhe Ni, Guoguang Shi
Shikonin has previously been shown to have antitumor, anti-inflammatory, antiviral and extensive pharmacological effects. The aim of the present study was to explore whether the protective effect of shikonin is mediated via the inhibition of inflammation and chondrocyte apoptosis, and to elucidate the potential molecular mechanisms in a rat model of osteoarthritis. A model of osteoarthritis was established in healthy male Sprague-Dawley rats and 10 mg/kg/day shikonin was administered intraperitoneally for 4 days...
October 2016: Experimental and Therapeutic Medicine
https://www.readbyqxmd.com/read/27601995/shikonin-inhibits-intestinal-calcium-activated-chloride-channels-and-prevents-rotaviral-diarrhea
#19
Yu Jiang, Bo Yu, Hong Yang, Tonghui Ma
Secretory diarrhea remains a global health burden and causes major mortality in children. There have been some focuses on antidiarrheal therapies that may reduce fluid losses and intestinal motility in diarrheal diseases. In the present study, we identified shikonin as an inhibitor of TMEM16A chloride channel activity using cell-based fluorescent-quenching assay. The IC50 value of shikonin was 6.5 μM. Short-circuit current measurements demonstrated that shikonin inhibited Eact-induced Cl(-) current in a dose-dependent manner, with IC50 value of 1...
2016: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/27556106/n-end-rule-pathway-inhibition-assists-colon-tumor-regression-via-necroptosis
#20
Pritha Agarwalla, Rajkumar Banerjee
Recent study has shown that N-end rule pathway, an ubiquitin dependent proteolytic system, counteracts cell death by degrading many antisurvival protein fragments like BCLxL, BRCA1, RIPK1, etc. Inhibition of the N-end rule pathway can lead to metabolic stabilization of proapoptotic protein fragments like RIPK1, thereby sensitizing cells to programmed cell death. Receptor interacting serine-threonine protein kinase-1 (RIPK1) is one of the upstream regulators of programmed necrosis known as necroptosis. Necroptosis is particularly gaining attention of cancer biologists as it provides an alternate therapeutic modality to kill cancer cells, which often evolve multiple strategies to circumvent growth inhibition by apoptosis...
2016: Molecular Therapy Oncolytics
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