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https://www.readbyqxmd.com/read/28547157/shikonin-induces-necroptosis-by-reactive-oxygen-species-activation-in-nasopharyngeal-carcinoma-cell-line-cne-2z
#1
Zixuan Zhang, Zhirui Zhang, Qixiang Li, Hao Jiao, Dianlong Chong, Xiaojin Sun, Pei Zhang, Qiang Huo, Hao Liu
Shikonin, a natural small agent, has shown inhibitory effect in many kinds of cells, which increases intracellular reactive oxygen species (ROS) level and causes mitochondrial injury. In this study, shikonin showed good inhibitory effect on nasopharyngeal carcinoma CNE-2Z cells in vivo and vitro. The results presented here revealed that ROS levels increased markly after shikonin treated. The electron microscopy displays the change in ultrastructure of CNE-2Z cells after treatment for shikonin, which indicated that shikonin induced necroptosis...
May 25, 2017: Journal of Bioenergetics and Biomembranes
https://www.readbyqxmd.com/read/28521243/shikonin-alleviates-allergic-airway-remodeling-by-inhibiting-the-erk-nf-%C3%AE%C2%BAb-signaling-pathway
#2
Tian-Yue Wang, Qian-Lan Zhou, Miao Li, Yun-Xiao Shang
Shikonin is a naphthoquinone extracted from the root of Lithospermum erythrorhizon, and has been reported to suppress allergic airway inflammation in mice. However, the underlying mechanisms are unclear and need to be further elucidated. In this study, shikonin (0.5, 2 or 4mg/kg) was given intraperitoneally to ovalbumin (OVA)-challenged BALB/c mice. We found that the pathological airway remodeling of asthmatic mice was alleviated by shikonin, and the infiltrated inflammatory cells and collagen deposition in their lungs were reduced...
May 15, 2017: International Immunopharmacology
https://www.readbyqxmd.com/read/28485480/shikonin-inhibited-migration-and-invasion-of-human-lung-cancer-cells-via-suppression-of-c-met-mediated-epithelial-to-mesenchymal-transition
#3
Yei-San Hsieh, Chiung-Ho Liao, Wan-Shen Chen, Jih-Tung Pai, Meng-Shih Weng
Epithelial-to-mesenchymal transition (EMT) is a major process to regulate cell migration and invasion. Inhibition of epidermal growth factor receptor (EGFR)-mediated EMT by tyrosine kinase inhibitors (TKIs) is a strategy to prevent lung cancer invasion. However, drug resistance is emerged and accelerated invasion through other signaling bypassing EGFR after TKIs therapy. c-Met signaling pathway is highly activated in EGFR-mutated lung cancer cells. Targeting c-Met signaling pathway may be a strategy to suppress EGFR-independent migration and invasion for lung cancer therapy...
May 9, 2017: Journal of Cellular Biochemistry
https://www.readbyqxmd.com/read/28480438/preparation-and-properties-of-compound-arnebiae-radix-microemulsion-gel
#4
Jing Chen, Yanping He, Ting Gao, Licheng Zhang, Yuna Zhao
BACKGROUND: Compound Arnebiae radix oil has been clinically applied to treat burns and scalds for a long time. However, it is unstable and inconvenient to use. The aim of this study was to prepare a compound Arnebiae radix microemulsion gel for transdermal delivery system and evaluate its characteristics. MATERIALS AND METHODS: Based on the solubility of Shikonin, the active component of Arnebiae radix and the results of phase studies, adequate ratio of each component in microemulsion was determined...
2017: African Journal of Traditional, Complementary, and Alternative Medicines: AJTCAM
https://www.readbyqxmd.com/read/28401486/dual-treatment-with-shikonin-and-temozolomide-reduces-glioblastoma-tumor-growth-migration-and-glial-to-mesenchymal-transition
#5
Diana Matias, Joana Balça-Silva, Luiz Gustavo Dubois, Bruno Pontes, Valéria Pereira Ferrer, Luciane Rosário, Anália do Carmo, Juliana Echevarria-Lima, Ana Bela Sarmento-Ribeiro, Maria Celeste Lopes, Vivaldo Moura-Neto
PURPOSE: Glioblastomas (GBM) comprise 17% of all primary brain tumors. These tumors are extremely aggressive due to their infiltrative capacity and chemoresistance, with glial-to-mesenchymal transition (GMT) proteins playing a prominent role in tumor invasion. One compound that has recently been used to reduce the expression of these proteins is shikonin (SHK), a naphthoquinone with anti-tumor properties. Temozolomide (TMZ), the most commonly used chemotherapeutic agent in GBM treatment, has so far not been studied in combination with SHK...
April 11, 2017: Cellular Oncology (Dordrecht)
https://www.readbyqxmd.com/read/28385613/shikonin-alleviates-the-biotoxicity-produced-by-pneumococcal-pneumolysin
#6
Xiaoran Zhao, Yonglin Zhou, Laiying Wang, Meng Li, Dongxue Shi, Dan Li, Jianfeng Wang
AIMS: Streptococcus pneumoniae (S. pneumoniae) is a common pathogen that can cause severe infections in humans. Pneumolysin (PLY) is an important virulence trait of S. pneumoniae and has cytotoxicity, genotoxicity and pro-inflammatory activity; it is essential for the pathogenesis of S. pneumoniae pneumonia and is an anti-virulence target of small molecule drug development. The treatment options for this microbe were limit due to the ubiquitous antibiotic resistance; therefore, new drugs and treatment strategies are needed...
April 3, 2017: Life Sciences
https://www.readbyqxmd.com/read/28378811/inhibition-of-pyruvate-kinase-m2-markedly-reduces-chemoresistance-of-advanced-bladder-cancer-to-cisplatin
#7
Xing Wang, Fenglin Zhang, Xue-Ru Wu
Chemoresistance to cisplatin is a principal cause of treatment failure and mortality of advanced bladder cancer (BC). The underlying mechanisms remain unclear, which hinders the development of preventive strategies. Recent data indicate that pyruvate kinase M2 (PKM2), a glycolytic enzyme for Warburg effect, is strongly upregulated in BC. This study explores the role of PKM2 in chemoresistance and whether inhibiting PKM2 augments the chemosensitivity to cisplatin and reduces BC growth and progression. We found that Shikonin binds PKM2 and inhibits BC cell survival in a dose-dependent but pyruvate kinase activity-independent manner...
April 5, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28322323/anti-inflammatory-properties-of-shikonin-contribute-to-improved-early-stage-diabetic-retinopathy
#8
Po-Lin Liao, Cheng-Hui Lin, Ching-Hao Li, Chi-Hao Tsai, Jau-Der Ho, George C Y Chiou, Jaw-Jou Kang, Yu-Wen Cheng
Diabetic retinopathy (DR), a major microvascular complication of diabetes, leads to retinal vascular leakage, neuronal dysfunction, and apoptosis within the retina. In this study, we combined STZ with whole-body hypoxia (10% O2) for quicker induction of early-stage retinopathy in C57BL/6 mice. We also compared the effects of a high glucose condition combined with hypoxia (1% O2) to a low glucose condition by using retinal pigment epithelial (RPE) cells, which are a crucial component of the outer blood-retinal barrier and the damage is related to retinopathy...
March 21, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28322249/the-protective-effects-of-shikonin-on-hepatic-ischemia-reperfusion-injury-are-mediated-by-the-activation-of-the-pi3k-akt-pathway
#9
Tong Liu, QingHui Zhang, Wenhui Mo, Qiang Yu, Shizan Xu, Jingjing Li, Sainan Li, Jiao Feng, Liwei Wu, Xiya Lu, Rong Zhang, Linqiang Li, Keran Cheng, Yuqing Zhou, Shunfeng Zhou, Rui Kong, Fan Wang, Weiqi Dai, Kan Chen, Yujing Xia, Jie Lu, Yingqun Zhou, Yan Zhao, Chuanyong Guo
Hepatic ischemia/reperfusion (I/R) injury, which can result in severe liver injury and dysfunction, occurs in a variety of conditions such as liver transplantation, shock, and trauma. Cell death in hepatic I/R injury has been linked to apoptosis and autophagy. Shikonin plays a significant protective role in ischemia/reperfusion injury. The purpose of the present study was to investigate the protective effect of shikonin on hepatic I/R injury and explore the underlying mechanism. Mice were subjected to segmental (70%) hepatic warm ischemia to induce hepatic I/R injury...
March 21, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28303727/enhancement-of-nk-cells-proliferation-and-function-by-shikonin
#10
Yan Li, Hailin Lu, Yongchun Gu, Zhiqiang Ning, Tinghua Cao, Chao Chen, Chengru Hu, Min Tao
CONTEXT: Shikonin is a kind of naphthoquinone compound found mainly in Lithospermum erythrorhizon Sieb,et Zucc. Previous studies have shown that Shikonin has anti-tumor, anti-inflammatory and extensive pharmacological effects. According to new studies, Shikonin could also modulate the immune system function, but the effect to NK (nature killer) cells is yet unknown. OBJECTIVE: To investigate the effect and mechanism of Shikonin on NK cells proliferation and cytotoxicity to colon cancer cell line (Caco-2)...
March 17, 2017: Immunopharmacology and Immunotoxicology
https://www.readbyqxmd.com/read/28265634/metabolic-profiling-study-of-shikonin-s-cytotoxic-activity-in-the-huh7-human-hepatoma-cell-line
#11
E D Spyrelli, A V Kyriazou, C Virgiliou, A Nakas, O Deda, V P Papageorgiou, A N Assimopoulou, H G Gika
Shikonin and its enantiomer alkannin, which are natural products, have been extensively studied in vitro and in vivo for, among others, their antitumor activity. The investigation of the molecular pathways involved in their action is of interest, since they are not yet clearly defined. Metabolic profiling in cells can provide a picture of a cell's phenotype upon intervention, assisting in the elucidation of the mechanism of action. In this study, the cytotoxic effect of shikonin on a human hepatocarcinoma cell line was studied...
May 2, 2017: Molecular BioSystems
https://www.readbyqxmd.com/read/28245783/advance-in-anti-tumor-mechanisms-of-shikonin-alkannin-and-their-derivatives
#12
Xu Zhang, Jia-Hua Cui, Qing-Qing Meng, Shao-Shun Li, Wen Zhou, Sui Xiao
Shikonin, alkannin and their derivatives, the main ingredient of Lithospermum erythrorhizon native to Inner Mongolian and Northwest of China, displayed good antitumor effects via multiple-target mechanisms. This review focus on their antitumor mechanisms from the direct reaction and the indirect reaction aspects, and expounded the death of tumor cells caused by shkionin, akannin and derivatives, which are involved in the ROS-mediated mechanisms and direct interaction with DNA and protein.
February 28, 2017: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28230806/metabolic-profiling-and-identification-of-shikonins-in-root-periderm-of-two-invasive-echium-spp-weeds-in-australia
#13
Dominik Skoneczny, Paul A Weston, Xiaocheng Zhu, Geoff M Gurr, Ragan M Callaway, Russel A Barrow, Leslie A Weston
Metabolic profiling can be successfully implemented to analyse a living system's response to environmental conditions by providing critical information on an organism's physiological state at a particular point in time and allowing for both quantitative and qualitative assessment of a specific subset(s) of key metabolites. Shikonins are highly reactive chemicals that affect various cell signalling pathways and possess antifungal, antibacterial and allelopathic activity. Based on previous bioassay results, bioactive shikonins, are likely to play important roles in the regulation of rhizosphere interactions with neighbouring plants, microbes and herbivores...
February 21, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28228400/inhibiting-aerobic-glycolysis-suppresses-renal-interstitial-fibroblasts-activation-and-renal-fibrosis
#14
Hao Ding, Lei Jiang, Jing Xu, Feng Bai, Yang Zhou, Qi Yuan, Jing Luo, Ke Zen, Junwei Yang
Chronic kidney diseases (CKD) generally lead to renal fibrosis. Despite great progresses have been made in identifying molecular mediators of fibrosis, the mechanism that governs renal fibrosis remains unclear and so far no effective therapeutic anti-fibrosis strategy is available. Here we demonstrated that a switch of metabolism from oxidative phosphorylation to aerobic glycolysis (Warburg effect) in renal fibroblasts was the primary feature of fibroblast activation during renal fibrosis, and that suppressing renal fibroblast aerobic glycolysis could significantly reduce renal fibrosis...
February 22, 2017: American Journal of Physiology. Renal Physiology
https://www.readbyqxmd.com/read/28211616/design-synthesis-and-biological-evaluation-of-chalcone-containing-shikonin-derivatives-as-inhibitors-of-tubulin-polymerization
#15
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
#16
COMPARATIVE STUDY
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
#17
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
#18
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)...
February 15, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28069896/anti-tumor-effects-of-shikonin-derivatives-on-human-medullary-thyroid-carcinoma-cells
#19
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 radiotherapy 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...
February 2017: Endocrine Connections
https://www.readbyqxmd.com/read/28040409/antifungal-effects-of-phytocompounds-on-candida-species-alone-and-in-combination-with-fluconazole
#20
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...
February 2017: International Journal of Antimicrobial Agents
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