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https://www.readbyqxmd.com/read/28643772/cryptic-indole-hydroxylation-by-a-non-canonical-terpenoid-cyclase-parallels-bacterial-xenobiotic-detoxification
#1
Susann Kugel, Martin Baunach, Philipp Baer, Mie Ishida-Ito, Srividhya Sundaram, Zhongli Xu, Michael Groll, Christian Hertweck
Terpenoid natural products comprise a wide range of molecular architectures that typically result from C-C bond formations catalysed by classical type I/II terpene cyclases. However, the molecular diversity of biologically active terpenoids is substantially increased by fully unrelated, non-canonical terpenoid cyclases. Their evolutionary origin has remained enigmatic. Here we report the in vitro reconstitution of an unusual flavin-dependent bacterial indoloterpenoid cyclase, XiaF, together with a designated flavoenzyme-reductase (XiaP) that mediates a key step in xiamycin biosynthesis...
June 15, 2017: Nature Communications
https://www.readbyqxmd.com/read/28625363/design-synthesis-and-biological-evaluation-of-novel-indolin-2-ones-as-potent-anticancer-compounds
#2
Andong Zhou, Lei Yan, Fangfang Lai, Xiaoguang Chen, Masuo Goto, Kuo-Hsiung Lee, Zhiyan Xiao
The indolin-2-one core is a privileged structure for antitumor agents, especially kinase inhibitors. Twenty-three novel indolin-2-ones were designed by molecular dissection of the anticancer drug indirubin. Seventeen of them exhibited significant inhibition against the tested cell lines, and two of them (1c and 1h) showed IC50 values at the submicromolar level against HCT-116 cells. Compounds 1c and 2c were also potent inhibitors of the triple-negative breast cancer (TNBC) cell line MDA-MB-231. Flow cytometry was utilized to explore the antitumor mechanism of 1c and 2c with MDA-MB-231 cells, and distinct effects were observed on 2c...
June 7, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28557430/identification-of-a-water-soluble-indirubin-derivative-as-potent-inhibitor-of-insulin-like-growth-factor-1-receptor-through-structural-modification-of-the-parent-natural-molecule
#3
Xinlai Cheng, Karl-Heinz Merz, Sandra Vatter, Jochen Zeller, Stephan Muehlbeyer, Andrea Thommet, Jochen Christ, Stefan Wölfl, Gerhard Eisenbrand
Indirubins have been identified as potent ATP-competitive protein kinase inhibitors. Structural modifications in the 5- and 3'-position have been extensively investigated, but the impact of substituents in 5'-position is not equally well-studied. Here, we report the synthesis of new indirubin 3'- and 5'-derivatives in the search of water-soluble indirubins by introducing basic centers. Antiproliferative activity of all compounds in tumor cells was evaluated along with kinase inhibition of selected compounds...
June 6, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28525368/indirubin-improves-antioxidant-and-anti-inflammatory-functions-in-lipopolysaccharide-challenged-mice
#4
Tianjie Qi, Haitao Li, Shuai Li
Indirubin, a traditional Chinese medicine formulation from the Muricidae family, has been reported to exhibit abroad anti-cancer and anti-inflammation activities and mediate nuclear factor-κB (NF-κB) signal. Thus, this study aimed to investigate the protective effects of indirubin on LPS-induced acute lung injury and the potential mechanism in mice. The results showed that LPS treatment caused oxidative stress and inflammation in mice. Indirubin alleviated LPS-caused oxidative stress and inflammation via reducing MDA abundance and IL-1β and TNF-α expressions in mice...
May 30, 2017: Oncotarget
https://www.readbyqxmd.com/read/28508966/recurrent-purple-urine-bag-syndrome-presenting-with-full-spectrum-of-disease-severity-case-report-and-review-of-literature
#5
Junzhi Lin, Martha Hlafka, Omar Vargas, Mukul Bhattarai
Purple urine bag syndrome (PUBS) is a unique phenomenon characterized by purple discoloration of the urinary catheter bag and tubing following urinary catheterization lasting for hours to days. The purple discoloration is a mixture of indirubin dissolved in plastic with indigo on its surface. PUBS is most commonly associated with urinary tract infection (UTI) caused by bacteria with indoxyl phosphatase/sulfatase activity. It occurs predominantly in chronically catheterized, constipated elderly female patients...
November 2016: CEN Case Reports
https://www.readbyqxmd.com/read/28458622/characterization-of-the-indirubin-derivative-ldd970-as-a-small-molecule-aurora-kinase-a-inhibitor-in-human-colorectal-cancer-cells
#6
Karyn Muzinga Ndolo, Kyeong Ryang Park, Hyo Jeong Lee, Kyoung Bin Yoon, Yong-Chul Kim, Sun-Young Han
Aurora kinase A plays an essential role in mitosis including chromosome separation and cytokinesis. Aberrant expression and activity of Aurora kinase A is associated with numerous malignancies including colorectal cancer followed by poor prognosis. The aim of this study is to determine the inhibitory effects of LDD970, an indirubin derivative, on Aurora kinase A in HT29 colorectal cancer cells. In vitro kinase assay revealed that, LDD970 inhibited levels of activated Aurora kinase A (IC50=0.37 mM). The inhibitory effects of LDD970 on Aurora kinase A, autophosphorylation and phosphorylation of histone H3 (Ser10), were confirmed by immunoblot analysis...
April 2017: Immune Network
https://www.readbyqxmd.com/read/28347789/induction-of-cell-death-in-pancreatic-ductal-adenocarcinoma-by-indirubin-3-oxime-and-5-methoxyindirubin-3-oxime-in%C3%A2-vitro-and-in%C3%A2-vivo
#7
Makoto Sano, Yoshimi Ichimaru, Masahiro Kurita, Emiko Hayashi, Taku Homma, Hiroaki Saito, Shinobu Masuda, Norimichi Nemoto, Akihiro Hemmi, Takashi Suzuki, Shinichi Miyairi, Hiroyuki Hao
Pancreatic ductal adenocarcinoma (PDAC) is an aggressive cancer with a poor prognosis. To identify potential effective therapeutic drugs for PDAC, we established a screening system based on spheroid formation using 170#3 mouse PDAC cells with or without fibroblasts. We found that indirubin 3'-oxime (Indox) and 5-methoxyindirubin 3'-oxime (5MeOIndox) inhibited PDAC cell proliferation. Furthermore, PDAC xenograft growth was also inhibited in BALB/c nu/nu mice after administration of Indox and 5MeOIndox. Both phosphorylated CDK1 and cyclin B1 levels in 170#3 cells were significantly reduced by treatment with Indox and 5MeOIndox in vitro and in vivo...
March 24, 2017: Cancer Letters
https://www.readbyqxmd.com/read/28265680/indirubin-inhibits-the-migration-invasion-and-activation-of-fibroblast-like-synoviocytes-from-rheumatoid-arthritis-patients
#8
Mingcheng Huang, Lihui Wang, Shan Zeng, Qian Qiu, Yaoyao Zou, Maohua Shi, Hanshi Xu, Liuqin Liang
OBJECTIVES: To evaluate the inhibition of indirubin in FLSs migration, invasion, activation, and proliferation in RA FLSs. METHODS: The levels of IL-6 and IL-8 in cultural supernatants were measured by ELISA. RA FLS migration and invasion in vitro were measured by the Boyden chamber method and the scratch assay. Signal transduction protein expression was measured by western blot. FLS proliferation was detected by Edu incorporation. F-actin was measured by immunofluorescence staining...
March 6, 2017: Inflammation Research: Official Journal of the European Histamine Research Society ... [et Al.]
https://www.readbyqxmd.com/read/28255203/indirubin-treatment-of-lipopolysaccharide-induced-mastitis-in-a-mouse-model-and-activity-in-mouse-mammary-epithelial-cells
#9
Jin-Lun Lai, Yu-Hui Liu, Yong-Chong Peng, Pan Ge, Chen-Fei He, Chang Liu, Ying-Yu Chen, Ai-Zhen Guo, Chang-Min Hu
Indirubin is a Chinese medicine extracted from indigo and known to be effective for treating chronic myelogenous leukemia, neoplasia, and inflammatory disease. This study evaluated the in vivo anti-inflammatory activity of indirubin in a lipopolysaccharide- (LPS-) induced mouse mastitis model. The indirubin mechanism and targets were evaluated in vitro in mouse mammary epithelial cells. In the mouse model, indirubin significantly attenuated the severity of inflammatory lesions, edema, inflammatory hyperemia, milk stasis and local tissue necrosis, and neutrophil infiltration...
2017: Mediators of Inflammation
https://www.readbyqxmd.com/read/28253732/the-indirubin-derivative-6-bromoindirubin-3-oxime-activates-proteostatic-modules-reprograms-cellular-bioenergetic-pathways-and-exerts-antiaging-effects
#10
Eleni N Tsakiri, Nicolas Gaboriaud-Kolar, Kalliopi K Iliaki, Job Tchoumtchoua, Eleni-Dimitra Papanagnou, Sofia Chatzigeorgiou, Konstantinos D Tallas, Emmanuel Mikros, Maria Halabalaki, Alexios-Leandros Skaltsounis, Ioannis P Trougakos
AIMS: Organismal aging can be delayed by mutations that either activate stress responses or reduce the nutrient-sensing pathway signaling; thus, by using Drosophila melanogaster as an in vivo experimental screening platform, we searched for compounds that modulate these pathways. RESULTS: We noted that oral administration of the glycogen synthase kinase 3 (Gsk-3) inhibitor 6-bromoindirubin-3'-oxime (6BIO) in Drosophila flies extended healthy life span. 6BIO is not metabolized in fly tissues, modulated bioenergetic pathways, decreased lipid and glucose tissue load, activated antioxidant and proteostatic modules, and enhanced resistance to stressors...
May 16, 2017: Antioxidants & Redox Signaling
https://www.readbyqxmd.com/read/28129131/6bio-enhances-oligonucleotide-activity-in-cells-a-potential-combinatorial-anti-androgen-receptor-therapy-in-prostate-cancer-cells
#11
Xiaowei Zhang, Daniela Castanotto, Sangkil Nam, David Horne, Cy Stein
Approximately 15%-25% of men diagnosed with prostate cancer do not survive their disease. The American Cancer Society estimated that for the year 2016 the number of prostate cancer deaths will be 26,120. Thus, there is a critical need for novel approaches to treat this deadly disease. Using high-throughput small-molecule screening, we found that the small molecule 6-bromo-indirubin-3'-oxime (6BIO) significantly improves the targeting of antisense oligonucleotides (ASOs) delivered by gymnosis (i.e., in the absence of any transfection reagents) in both the cell cytoplasm and the nucleus...
January 4, 2017: Molecular Therapy: the Journal of the American Society of Gene Therapy
https://www.readbyqxmd.com/read/28057719/structure-and-inhibitor-specificity-of-the-pctaire-family-kinase-cdk16
#12
Sarah E Dixon-Clarke, Saifeldin N Shehata, Tobias Krojer, Timothy D Sharpe, Frank von Delft, Kei Sakamoto, Alex N Bullock
CDK16 (also known as PCTAIRE1 or PCTK1) is an atypical member of the cyclin-dependent kinase (CDK) family that has emerged as a key regulator of neurite outgrowth, vesicle trafficking and cancer cell proliferation. CDK16 is activated through binding to cyclin Y via a phosphorylation-dependent 14-3-3 interaction and has a unique consensus substrate phosphorylation motif compared with conventional CDKs. To elucidate the structure and inhibitor-binding properties of this atypical CDK, we screened the CDK16 kinase domain against different inhibitor libraries and determined the co-structures of identified hits...
February 20, 2017: Biochemical Journal
https://www.readbyqxmd.com/read/27981893/meisoindigo-but-not-its-core-chemical-structure-indirubin-inhibits-zebrafish-interstitial-leukocyte-chemotactic-migration
#13
Baixin Ye, Xiaoxing Xiong, Xu Deng, Lijuan Gu, Qiongyu Wang, Zhi Zeng, Xiang Gao, Qingping Gao, Yueying Wang
CONTEXT: Inflammatory disease is a big threat to human health. Leukocyte chemotactic migration is required for efficient inflammatory response. Inhibition of leukocyte chemotactic migration to the inflammatory site has been shown to provide therapeutic targets for treating inflammatory diseases. OBJECTIVE: Our study was designed to discover effective and safe compounds that can inhibit leukocyte chemotactic migration, thus providing possible novel therapeutic strategy for treating inflammatory diseases...
December 2017: Pharmaceutical Biology
https://www.readbyqxmd.com/read/27976145/toxicological-study-of-the-indirubin-derivative-7bio
#14
J Tchoumtchoua, S Theocharis, M Halabalaki, A Efstathiou, N Gaboriaud-Kolar, D Smirlis, A E Konstantinidou, E S Patsouris, A L Skaltsounis
No abstract text is available yet for this article.
December 2016: Planta Medica
https://www.readbyqxmd.com/read/27845365/computational-drug-target-screening-through-protein-interaction-profiles
#15
Santiago Vilar, Elías Quezada, Eugenio Uriarte, Stefano Costanzi, Fernanda Borges, Dolores Viña, George Hripcsak
The development of computational methods to discover novel drug-target interactions on a large scale is of great interest. We propose a new method for virtual screening based on protein interaction profile similarity to discover new targets for molecules, including existing drugs. We calculated Target Interaction Profile Fingerprints (TIPFs) based on ChEMBL database to evaluate drug similarity and generated new putative compound-target candidates from the non-intersecting targets in each pair of compounds. A set of drugs was further studied in monoamine oxidase B (MAO-B) and cyclooxygenase-1 (COX-1) enzyme through molecular docking and experimental assays...
November 15, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27771929/the-role-of-indirubins-in-inflammation-and-associated-tumorigenesis
#16
Xinlai Cheng, Karl-Heinz Merz
Indirubin is the major active component of an herbal recipe 'Dangui Luhui Wan' () in traditional Chinese medicine (TCM). It is widely used in China for the treatment of inflammation, cancer, and other chronic diseases and is known for good efficiency and very low side effects. Primary studies on the mechanism of action revealed that indirubin and derivatives are potent ATP-competitive inhibitors of CDKs and GSK3ß achieving IC50 values down to the low nanomolar range. However, the clinical application of indirubins is limited by the extremely poor water solubility (<1 mg/L in general) and consequently the insufficient bioavailability originating from strong binding forces in the crystal lattice...
2016: Advances in Experimental Medicine and Biology
https://www.readbyqxmd.com/read/27726390/natural-based-indirubins-display-potent-cytotoxicity-toward-wild-type-and-t315i-resistant-leukemia-cell-lines
#17
Nicolas Gaboriaud-Kolar, Vasillios Myrianthopoulos, Konstantina Vougogiannopoulou, Panagiotis Gerolymatos, David A Horne, Richard Jove, Emmanuel Mikros, Sangkil Nam, Alexios-Leandros Skaltsounis
Drug resistance in chronic myelogenous leukemia (CML) requires the development of new CML chemotherapeutic drugs. Indirubin, a well-known mutikinase inhibitor, is the major active component of "Danggui Longhui Wan", a Chinese traditional medicine used for the treatment of CML symptoms. An in-house collection of indirubin derivatives was screened at 1 μM on wild-type and imatinib-resistant T315I mutant CML cells. Herein are reported that only 15 analogues of the natural 6-bromoindirubin displayed potent cytotoxicity in the submicromolar range...
October 28, 2016: Journal of Natural Products
https://www.readbyqxmd.com/read/27718095/indirubin-inhibits-lps-induced-inflammation-via-tlr4-abrogation-mediated-by-the-nf-kb-and-mapk-signaling-pathways
#18
Jin-Lun Lai, Yu-Hui Liu, Chang Liu, Ming-Pu Qi, Rui-Ning Liu, Xi-Fang Zhu, Qiu-Ge Zhou, Ying-Yu Chen, Ai-Zhen Guo, Chang-Min Hu
Indirubin plays an important role in the treatment of many chronic diseases and exhibits strong anti-inflammatory activity. However, the molecular mode of action during mastitis prophylaxis remains poorly understood. In this study, a lipopolysaccharide (LPS)-induced mastitis mouse model showed that indirubin attenuated histopathological changes in the mammary gland, local tissue necrosis, and neutrophil infiltration. Moreover, indirubin significantly downregulated the production of interleukin (IL)-1β, IL-6, and tumor necrosis factor-α (TNF-α)...
February 2017: Inflammation
https://www.readbyqxmd.com/read/27412761/indirubin-3-oxime-prevents-h2o2-induced-neuronal-apoptosis-via-concurrently-inhibiting-gsk3%C3%AE-and-the-erk-pathway
#19
Jie Yu, Jiacheng Zheng, Jiajia Lin, Linlu Jin, Rui Yu, Shinghung Mak, Shengquan Hu, Hongya Sun, Xiang Wu, Zaijun Zhang, Mingyuen Lee, Wahkeung Tsim, Wei Su, Wenhua Zhou, Wei Cui, Yifan Han, Qinwen Wang
Oxidative stress-induced neuronal apoptosis plays an important role in many neurodegenerative disorders. In this study, we have shown that indirubin-3-oxime, a derivative of indirubin originally designed for leukemia therapy, could prevent hydrogen peroxide (H2O2)-induced apoptosis in both SH-SY5Y cells and primary cerebellar granule neurons. H2O2 exposure led to the increased activities of glycogen synthase kinase 3β (GSK3β) and extracellular signal-regulated kinase (ERK) in SH-SY5Y cells. Indirubin-3-oxime treatment significantly reversed the altered activity of both the PI3-K/Akt/GSK3β cascade and the ERK pathway induced by H2O2...
May 2017: Cellular and Molecular Neurobiology
https://www.readbyqxmd.com/read/27396532/indirubin-ameliorates-dextran-sulfate-sodium-induced-ulcerative-colitis-in-mice-through-the-inhibition-of-inflammation-and-the-induction-of-foxp3-expressing-regulatory-t-cells
#20
Wenyan Gao, Yufang Guo, Changhong Wang, Yifan Lin, Li Yu, Tianjiao Sheng, Zhuolin Wu, Yang Gong
Indirubin, an active ingredient of a traditional Chinese medicine prescription named Danggui Longhui Wan, has been reported to exhibit abroad anti-cancer and anti-inflammation activities. However, the effect of indirubin on ulcerative colitis (UC) has not been addressed. Here, we investigated the therapeutic efficacy of indirubin on dextran sulfate sodium (DSS)-induced UC in mice and explored its underlying mechanisms. UC model was induced in BALB/c mice by administrating with 3% DSS in drinking water for 7days...
July 2016: Acta Histochemica
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