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https://www.readbyqxmd.com/read/28816233/shikonin-induces-glioma-cell-necroptosis-in-vitro-by-ros-overproduction-and-promoting-rip1-rip3-necrosome-formation
#1
Bin Lu, Xu Gong, Zong-Qi Wang, Ye Ding, Chen Wang, Tian-Fei Luo, Mei-Hua Piao, Fan-Kai Meng, Guang-Fan Chi, Yi-Nan Luo, Peng-Fei Ge
Necroptosis is a type of programmed necrosis regulated by receptor interacting protein kinase 1 (RIP1) and RIP3. Necroptosis is found to be accompanied by an overproduction of reactive oxygen species (ROS), but the role of ROS in regulation of necroptosis remains elusive. In this study, we investigated how shikonin, a necroptosis inducer for cancer cells, regulated the signaling leading to necroptosis in glinoma cells in vitro. Treatment with shikonin (2-10 μmol/L) dose-dependently triggered necrosis and induced overproduction of intracellular ROS in rat C6 and human SHG-44, U87 and U251 glioma cell lines...
August 17, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28753907/shikonin-ameliorates-isoproterenol-iso-induced-myocardial-damage-through-suppressing-fibrosis-inflammation-apoptosis-and-er-stress
#2
Jun Yang, Zhao Wang, Dong-Lin Chen
Shikonin, isolated from the roots of herbal plant Lithospermum erythrorhizon, is a naphthoquinone. It has been reported to exert beneficial anti-inflammatory effects and anti-oxidant properties in various diseases. Isoproterenol (ISO) has been widely used to establish cardiac injury in vivo and in vitro. However, shikonin function in ISO-induced cardiac injury remains uncertain. In our study, we attempted to investigate the efficiency and possible molecular mechanism of shikonin in cardiac injury treatment induced by ISO...
September 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28753677/pyruvate-kinase-m2-is-a-poor-prognostic-marker-of-and-a-therapeutic-target-in-ovarian-cancer
#3
Tai-Kuang Chao, Tien-Shuo Huang, Yu-Ping Liao, Rui-Lan Huang, Po-Hsuan Su, Hueng-Yuan Shen, Hung-Cheng Lai, Yu-Chi Wang
Pyruvate kinase M2 (PKM2) regulates glycolysis and oxidative phosphorylation; however, the role of PKM2 in ovarian cancer remains largely unknown. We investigated whether ovarian cancer metabolism could provide insight into the development of therapeutic strategies. We performed immunohistochemical staining for PKM2 on a tissue microarray for multivariate analysis. It revealed that patients exhibiting higher PKM2 expression were significantly associated with malignancy groups (p < 0.001) and pathogenesis models (p < 0...
2017: PloS One
https://www.readbyqxmd.com/read/28714761/gamma-irradiation-of-medicinally-important-plants-and-the-enhancement-of-secondary-metabolite-production
#4
P Vivek Vardhan, Lata I Shukla
PURPOSE: The profitable production of some important plant-based secondary metabolites (ginsenosides, saponins, camptothecin, shikonins etc.) in vitro by gamma irradiation is a current area of interest. We reviewed different types of secondary metabolites, their mode of synthesis and effect of γ-radiation on their yield for different plants, organs and in vitro cultures (callus, suspension, hairy root). Special effort has been made to review the biochemical mechanisms underlying the increase in secondary metabolites...
July 17, 2017: International Journal of Radiation Biology
https://www.readbyqxmd.com/read/28713949/shikonin-suppresses-proliferation-and-induces-apoptosis-in-human-leukemia-nb4-cells-through-modulation-of-mapks-and-c%C3%A2-myc
#5
Zhi-Ling Shan, Liang Zhong, Chu-Lan Xiao, Liu-Gen Gan, Ting Xu, Hao Song, Rong Yang, Liu Li, Bei-Zhong Liu
Acute promyelocytic leukemia (APL) is a special subtype of acute myeloid leukemia that responds to treatment with all‑trans retinoic acid and arsenic trioxide. However, severe side effects and drug resistance limit the effectiveness of these treatments. Hence, new drugs for APL are required urgently. Shikonin, an active naphthoquinone derived from the Chinese medical herb Zi Cao exerts antitumor activity in several cancers. In the present study, the effects of shikonin on proliferation and apoptosis in NB4 cells, as well as related mechanisms were assessed...
September 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/28709426/xue-fu-zhu-yu-decoction-protects-rats-against-retinal-ischemia-by-downregulation-of-hif-1%C3%AE-and-vegf-via-inhibition-of-rbp2-and-pkm2
#6
Shu-Qiu Tan, Xue Geng, Jorn-Hon Liu, Wynn Hwai-Tzong Pan, Li-Xiang Wang, Hui-Kang Liu, Lei Hu, Hsiao-Ming Chao
BACKGROUND: Retinal ischemia-related eye diseases result in visual dysfunction. This study investigates the protective effects and mechanisms of Xue-Fu-Zhu-Yu decoction (XFZYD) with respect to retinal ischemia. METHODS: Retinal ischemia (I) was induced in Wistar rats by a high intraocular pressure (HIOP) of 120 mmHg for 1 h, which was followed by reperfusion of the ischemic eye; the fellow untreated eye acted as a control. Electroretinogram (ERG), biochemistry and histopathology investigations were performed...
July 14, 2017: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/28699129/shikonin-changes-the-lipopolysaccharide-induced-expression-of-inflammation-related-genes-in-macrophages
#7
Lucia Satiko Yoshida, Tomohito Kakegawa, Yasukatsu Yuda, Hiromi Takano-Ohmuro
We aimed to find candidate molecules possibly involved in the anti-inflammatory activity of shikonin (active compound of "Shikon") by analyzing its effects on gene expression of lipopolysaccharide (LPS)-treated THP-1 macrophages. Polysome-associated mRNAs (those expected to be under translation: translatome) from cells treated with LPS alone (LPS: 5 µg/mL), shikonin alone (S: 100 nM), or LPS plus shikonin (LPS&S) for 3 h were analyzed by DNA microarray followed by detection of enriched pathways/gene ontologies using the tools of the STRING database...
July 11, 2017: Journal of Natural Medicines
https://www.readbyqxmd.com/read/28688289/antiviral-activity-of-a-synthesized-shikonin-ester-against-influenza-a-h1n1-virus-and-insights-into-its-mechanism
#8
Yahan Zhang, Hongwei Han, Hanyue Qiu, Hongyan Lin, Lugang Yu, Wanzhan Zhu, Jinliang Qi, Rongwu Yang, Yanjun Pang, Xiaoming Wang, Guihua Lu, Yonghua Yang
This study aimed to examine the antiviral effects of shikonin ester ((R)-1-(5, 8-dihydroxy-1,4-dioxo-1,4-dihydronaphthalen-2-yl)-4-methylpent-3-en-1-yl3-(1H- indol-3-yl) propanoate (PMM-034) against influenza A (H1N1) virus. We investigated PMM-034 anti-H1N1 activity and its effect on caspase 3 gene expression during cellular apoptosis after influenza virus infection in vitro. Neuraminidase (NA) inhibition was assessed in comparison with oseltamivir in the influenza virus standard strains A/PR/8/34 to understand the viral mechanism...
September 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28688274/discovery-of-novel-naphthoquinone-derivatives-as-inhibitors-of-the-tumor-cell-specific-m2-isoform-of-pyruvate-kinase
#9
Xianling Ning, Hailong Qi, Ridong Li, Yunqiao Li, Yan Jin, Michael A McNutt, Junyi Liu, Yuxin Yin
Pyruvate kinase M2 (PKM2) is a rate-limiting enzyme of the glycolytic pathway which is highly expressed in cancer cells. Cancer cells rely heavily on PKM2 for anabolic and energy requirements, and specific targeting of PKM2 therefore has potential as strategy for cancer therapy. Here, we report the synthesis and biologic evaluation of novel naphthoquinone derivatives as selective small molecule inhibitors of PKM2. Some target compounds, such as compound 3k, displayed more potent PKM2 inhibitory activity than the reported optimal PKM2 inhibitor shikonin...
June 29, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28684144/shikonin-suppresses-proliferation-and-induces-cell-cycle-arrest-through-the-inhibition-of-hypoxia-inducible-factor-1%C3%AE-signaling
#10
Ming Yue Li, Chunliu Mi, Ke Si Wang, Zhe Wang, Hong Xiang Zuo, Lian Xun Piao, Guang Hua Xu, Xuezheng Li, Juan Ma, Xuejun Jin
Hypoxia enhances the development of solid tumors. Hypoxia-inducible factor-1α (HIF-1α) is a transcription factor that is dominantly expressed under hypoxia in solid tumor cells and is a key factor of tumor regulation. HIF-1α regulates several target genes involved in many aspects of cancer progression, including angiogenesis, metastasis, and cell proliferation, as well as imparting resistance to cancer treatment. In this study, we assessed shikonin, which derives from the traditional medical herb Lithospermum erythrorhizon, for its anti-cancer effects in hypoxia-induced human colon cancer cell lines...
July 3, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/28674499/phytochemicals-approach-for-developing-cancer-immunotherapeutics
#11
REVIEW
Shu-Yi Yin, Ning-Sun Yang, Tien-Jen Lin
Phytochemicals or their derived compounds are being increasingly recognized as potentially potent complementary treatments for cancer. Among them, some phytochemicals are being actively evaluated for use as adjuvants in anticancer therapies. For instance, shikonin and hypericin were found to induce immunogenic cell death of specific cancer cells, and this effect was able to further activate the recognition activity of tumor cells by the host immune system. On the other hand, some derivatives of phytochemicals, such as dihydrobenzofuran lignan (Q2-3) have been found to induce the secretion of an endogenous anticancer factor, namely IL-25, from non-malignant cells...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28667265/transcriptome-analysis-explores-genes-related-to-shikonin-biosynthesis-in-lithospermeae-plants-and-provides-insights-into-boraginales-evolutionary-history
#12
Feng-Yao Wu, Cheng-Yi Tang, Yu-Min Guo, Zhuo-Wu Bian, Jiang-Yan Fu, Gui-Hua Lu, Jin-Liang Qi, Yan-Jun Pang, Yong-Hua Yang
Shikonin and its derivatives extracted from Lithospermeae plants' red roots have current applications in food and pharmaceutical industries. Previous studies have cloned some genes related to shikonin biosynthesis. However, most genes related to shikonin biosynthesis remain unclear, because the lack of the genome/transcriptome of the Lithospermeae plants. Therefore, in order to provide a new understanding of shikonin biosynthesis, we obtained transcriptome data and unigenes expression profiles in three shikonin-producing Lithospermeae plants, i...
June 30, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28662515/trail-enhances-shikonin-induced-apoptosis-through-ros-jnk-signaling-in-cholangiocarcinoma-cells
#13
Guangyao Zhou, Zuqin Yang, Xiaodong Wang, Ran Tao, Yuanping Zhou
BACKGROUND/AIMS: Cholangiocarcinoma (CCA), arising from varying locations within the biliary tree, is the second most common primary liver malignancy worldwide. Shikonin, an active compound extracted from the Chinese herb Zicao, holds anti-bacterial, anti-inflammatory, and anti-tumor activities. However, the effect of shikonin on human cholangiocarcinoma and detailed mechanisms of TRAIL enhancement remains to be elucidated. The purpose of the study was to investigate the protective functions of TRAIL enhancement for shikonin induced apoptosis in cholangiocarcinoma cells...
June 29, 2017: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/28644383/use-of-ultrasonication-technology-for-the-increased-production-of-plant-secondary-metabolites
#14
REVIEW
Md Mohidul Hasan, Tufail Bashir, Hanhong Bae
Plant secondary metabolites (PSMs) provide taste, color, odor, and resistance to plants, and they are also used to treat cancer and cardiovascular diseases. Synthesis of PSMs in plants is stimulated in response to different forms of external stress. Use of ultrasonication (US) to clean or decontaminate fruits and vegetables leads to physical stress that finally results in the accumulation of PSMs. US can stimulate accumulation of taxol, ginsenoside saponins, shikonin, and resveratrol, e.g., up to 319-fold increase of resveratrol synthesis has been observed in grape due to US...
June 23, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28633108/bioactivity-and-quantitative-analysis-of-isohexenylnaphthazarins-in-root-periderm-of-two-echium-spp-e-%C3%A2-plantagineum-and-e-%C3%A2-gaditanum
#15
Alexandra G Durán, M Teresa Gutiérrez, Carlos Rial, Ascensión Torres, Rosa M Varela, Manuel M Valdivia, José M G Molinillo, Dominik Skoneczny, Leslie A Weston, Francisco A Macías
Isohexenylnaphthazarins are commonly found in the root periderm of several Boraginaceous plants and are known for their broad range of biological activities. The work described herein concerns the biological activity of compounds from the roots of Echium plantagineum L. and Echium gaditanum Boiss (Boraginaceae) collected from field sites in southern Spain and Australia. Bioactivity was assessed using etiolated wheat coleoptile bioassay and in vitro growth inhibitory activity in HeLa and IGROV-1 cells. The quantification of four isohexenylnaphthazarins (shikonin/alkannin, deoxyshikonin/deoxyalkannin, acetylshikonin/acetylalkannin and dimethylacrylshikonin/dimethylacrylalkannin) was performed by LC-MS/MS using juglone as internal standard...
September 2017: Phytochemistry
https://www.readbyqxmd.com/read/28627658/shikonin-promotes-adriamycin%C3%A2-induced-apoptosis-by-upregulating-caspase%C3%A2-3-and-caspase%C3%A2-8-in-osteosarcoma
#16
Qing Yang, Suoyuan Li, Zeze Fu, Binhui Lin, Zifei Zhou, Zhuoying Wang, Yingqi Hua, Zhengdong Cai
Osteosarcoma is the most common primary malignant bone tumor. Cancer cells employ a host of mechanisms to develop resistance to adriamycin (ADM) or other chemotherapeutic drugs. Shikonin (SK), an active constituent extracted from a Chinese medicinal herb, has been shown to cooperate with ADM in the treatment of osteosarcoma and certain other types of cancer by contributing to the response rate of chemotherapy and the side effects. The aim of the present study was to investigate the role and underlying mechanism of SK in chemotherapy for osteosarcoma...
August 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/28621748/identification-of-onosma-visianii-roots-extract-and-purified-shikonin-derivatives-as-potential-acaricidal-agents-against-tetranychus-urticae
#17
Stefania Sut, Roman Pavela, Vladislav Kolarčik, Loredana Cappellacci, Riccardo Petrelli, Filippo Maggi, Stefano Dall'Acqua, Giovanni Benelli
There is an increasing need for the discovery of reliable and eco-friendly pesticides and natural plant-derived products may play a crucial role as source of new active compounds. In this research, a lipophilic extract of Onosma visianii roots extract containing 12% of shikonin derivatives demonstrated significant toxicity and inhibition of oviposition against Tetranychus urticae mites. Extensive chromatographic separation allowed the isolation of 11 naphthoquinone derivatives that were identified by spectral techniques and were tested against Tetranychus urticae...
June 16, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28603416/successful-in-vivo-hyperthermal-therapy-toward-breast-cancer-by-chinese-medicine-shikonin-loaded-thermosensitive-micelle
#18
Yonghua Su, Nian Huang, Di Chen, Li Zhang, Xia Dong, Yun Sun, Xiandi Zhu, Fulei Zhang, Jie Gao, Ying Wang, Kexing Fan, Puichi Lo, Wei Li, Changquan Ling
The Chinese traditional medicine Shikonin is an ideal drug due to its multiple targets to tumor cells. But in clinics, improving its aqueous solubility and tumor accumulation is still a challenge. Herein, a copolymer with tunable poly(N-isopropylacrymaide) and polylactic acid block lengths is designed, synthesized, and characterized in nuclear magnetic resonance. The corresponding thermosensitive nanomicelle (TN) with well-defined core-shell structure is then assembled in an aqueous solution. For promoting the therapeutic index, the physical-chemistry properties of TNs including narrow size, low critical micellar concentration, high serum stability, tunable volume phase transition temperature (VPTT), high drug-loading capacity, and temperature-controlled drug release are systematically investigated and regulated through the fine self-assembly...
2017: International Journal of Nanomedicine
https://www.readbyqxmd.com/read/28588262/identification-of-new-shikonin-derivatives-as-antitumor-agents-targeting-stat3-sh2-domain
#19
Han-Yue Qiu, Xiang Zhu, Yue-Lin Luo, Hong-Yan Lin, Cheng-Yi Tang, Jin-Liang Qi, Yan-Jun Pang, Rong-Wu Yang, Gui-Hua Lu, Xiao-Ming Wang, Yong-Hua Yang
Signal transducer and activator of transcription 3 (STAT3) is hyper-activated in diversiform human tumors and has been validated as an attractive therapeutic target. Current research showed that a natural product, shikonin, along with its synthetic analogues, is able to inhibit the activity of STAT3 potently. The potential space of shikonin in developing novel anti-cancer agents encouraged us to carry out the investigation of the probable binding mode with STAT3. From this foundation, we have designed new types of STAT3 SH2 inhibitors...
June 6, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28569199/shikonin-induced-necroptosis-is-enhanced-by-the-inhibition-of-autophagy-in-non-small-cell-lung-cancer-cells
#20
Hyo-Jin Kim, Ki-Eun Hwang, Do-Sim Park, Seon-Hee Oh, Hong Young Jun, Kwon-Ha Yoon, Eun-Taik Jeong, Hak-Ryul Kim, Young-Suk Kim
BACKGROUND: Shikonin, a natural naphthoquinone pigment purified from Lithospermum erythrorhizon, induces necroptosis in various cancer types, but the mechanisms underlying the anticancer activity of shikonin in lung cancer are not fully understood. This study was designed to clarify whether shikonin causes necroptosis in non-small cell lung cancer (NSCLC) cells and to investigate the mechanism of action. METHODS: Multiplex and caspase 8 assays were used to analyze effect of shikonin on A549 cells...
May 31, 2017: Journal of Translational Medicine
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