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https://www.readbyqxmd.com/read/28057719/structure-and-inhibitor-specificity-of-the-pctaire-family-kinase-cdk16
#1
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 protein 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 an unique consensus substrate phosphorylation motif compared to 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...
January 5, 2017: Biochemical Journal
https://www.readbyqxmd.com/read/27981893/meisoindigo-but-not-its-core-chemical-structure-indirubin-inhibits-zebrafish-interstitial-leukocyte-chemotactic-migration
#2
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
#3
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
#4
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
#5
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
#6
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 11, 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
#7
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)...
October 7, 2016: 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
#8
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...
July 13, 2016: 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
#9
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
https://www.readbyqxmd.com/read/27363197/-biosynthesis-of-indigo-and-indirubin-by-whole-cell-catalyst-designed-by-combination-of-protein-engineering-and-metabolic-engineering
#10
Yang Li, Junge Zhu, Jianjun Wang, Huanzhang Xia, Sheng Wu
The phenylacetone monooxygenase, isolated from Thermobifida fusca, mainly catalyzes Baeyer-Villiger oxidation reaction towards aromatic compounds. Met446 plays a vital role in catalytic promiscuity, based on the structure and function of phenylacetone monooxygenase. Mutation in Met446 locus can offer enzyme new catalytic feature to activate C-H bond, oxidizing indole to finally generate indigo and indirubin, but the yield was only 1.89 mg/L. In order to further improve the biosynthesis efficiency of the whole-cell catalyst, metabolic engineering was applied to change glucose metabolism pathway of Escherichia coli...
January 2016: Sheng Wu Gong Cheng Xue Bao, Chinese Journal of Biotechnology
https://www.readbyqxmd.com/read/27347027/genotoxicity-testing-of-persicariae-rhizoma-persicaria-tinctoria-h-gross-aqueous-extracts
#11
Won Ho Lee, Seong Hun Choi, Su Jin Kang, Chang Hyun Song, Soo Jin Park, Young Joon Lee, Sae Kwang Ku
Persicariae Rhizoma (PR) has been used as an anti-inflammatory and detoxification agent in Korea, and contains the biologically active dyes purple indirubin and blue indigo. Despite synthetic indigo showing genotoxic potential, thorough studies have not been carried out on the genotoxicity of PR. The potential genotoxicity of an aqueous extract of PR containing indigo (0.043%) and indirubin (0.009%) was evaluated using a standard battery of tests for safety assessment. The PR extract did not induce any genotoxic effects under the conditions of this study...
July 2016: Experimental and Therapeutic Medicine
https://www.readbyqxmd.com/read/27281580/development-and-full-validation-of-an-uplc-ms-ms-method-for-the-quantification-of-the-plant-derived-alkaloid-indirubin-in-rat-plasma
#12
Evelyn A Jähne, Chethan Sampath, Veronika Butterweck, Matthias Hamburger, Mouhssin Oufir
An UPLC-MS/MS method for the quantification of indirubin in lithium heparinized rat plasma was developed and validated according to current international guidelines. Indirubin was extracted from rat plasma by using Waters Ostro™ pass-through sample preparation plates. The method was validated with a LLOQ of 5.00ng/mL and an ULOQ of 500ng/mL. The calibration curve was fitted by least-square quadratic regression, and a weighting factor of 1/X was applied. Recoveries of indirubin and I.S. were consistent and ≥75...
September 5, 2016: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/27251501/indirubin-3-epoxide-induces-caspase-independent-cell-death-in-human-neuroblastoma
#13
Masahiro Kurita, Satoshi Hanada, Yoshimi Ichimaru, Hiroaki Saito, Keiichi Tabata, Satoru Asami, Shinichi Miyairi, Takashi Suzuki
Indirubin inhibits cyclin-dependent kinases by binding to their ATP-binding site, thereby exerting potent cytotoxicity on some tumor cells. We examined the anti-tumor effect of indirubin 3'-epoxide on human neuroblastoma cell lines (IMR-32, SK-N-SH, and NB-39). The results revealed potent cytotoxicity of indirubin 3'-epoxide against the IMR-32 (IC50: 0.16 µM) and SK-N-SH (IC50: 0.07 µM) cells. Furthermore, it also induced an increase of the sub-G1 population in the IMR-32 cells. Examination by Hoechst 33342 staining revealed apoptosis characterized by cell shrinkage, nuclear condensation and nuclear fragmentation in a concentration-dependent manner...
2016: Biological & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/27211013/embryonic-cardiotoxicity-of-weak-aryl-hydrocarbon-receptor-agonists-and-cyp1a-inhibitor-fluoranthene-in-the-atlantic-killifish-fundulus-heteroclitus
#14
D R Brown, B W Clark, L V T Garner, R T Di Giulio
High affinity aryl hydrocarbon receptor (AHR) ligands, such as certain polychlorinated biphenyls and 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD), cause severe cardiac teratogenesis in fish embryos. Moderately strong AHR agonists, for example benzo[a]pyrene and β-naphthoflavone, are capable of causing similar cardiotoxic effects, particularly when coupled with cytochrome P450 1A (CYP1A) inhibitors (e.g., fluoranthene (FL). Additionally, some weaker AHR agonists (carbaryl, 2-methylindole, 3-methylindole, and phenanthrene) are known to also cause cardiotoxicity in zebrafish (Danio rerio) embryos when coupled with FL; however, the cardiotoxic effects were not mediated specifically by AHR stimulation...
October 2016: Comparative Biochemistry and Physiology. Toxicology & Pharmacology: CBP
https://www.readbyqxmd.com/read/27185663/increased-aerobic-glycolysis-is-important-for-the-motility-of-activated-vsmc-and-inhibited-by-indirubin-3-monoxime
#15
Elke H Heiss, Daniel Schachner, Maddalena Donati, Christoph S Grojer, Verena M Dirsch
Increased aerobic glycolysis is a recognized feature of multiple cellular phenotypes and offers a potential point for drug interference, as pursued by anti-tumor agents targeting the Warburg effect. This study aimed at examining the role of aerobic glycolysis for migration of vascular smooth muscle cells (VSMC) and its susceptibility to the small molecule indirubin-3'-monoxime (I3MO). Activation of VSMC with platelet-derived growth factor (PDGF) resulted in migration and increased glycolytic activity which was accompanied by an increased glucose uptake and hexokinase (HK) 2 expression...
August 2016: Vascular Pharmacology
https://www.readbyqxmd.com/read/27160749/indole-compounds-may-be-promising-medicines-for-ulcerative-colitis
#16
REVIEW
Shinya Sugimoto, Makoto Naganuma, Takanori Kanai
Indole compounds are extracted from indigo plants and have been used as blue or purple dyes for hundreds of years. In traditional Chinese medicine, herbal agents in combination with Qing-Dai (also known as indigo naturalis) have been used to treat patients with ulcerative colitis (UC) and to remedy inflammatory conditions. Recent studies have noted that indole compounds can be biosynthesized from tryptophan metabolites produced by various enzymes derived from intestinal microbiota. In addition to their action on indole compounds, the intestinal microbiota produce various tryptophan metabolites that mediate critical functions through distinct pathways and enzymes...
September 2016: Journal of Gastroenterology
https://www.readbyqxmd.com/read/27150638/characterization-of-anti-leukemia-components-from-indigo-naturalis-using-comprehensive-two-dimensional-k562-cell-membrane-chromatography-and-in-silico-target-identification
#17
Xunxun Wu, Xiaofei Chen, Jia Dan, Yan Cao, Shouhong Gao, Zhiying Guo, Philipp Zerbe, Yifeng Chai, Yong Diao, Lei Zhang
Traditional Chinese Medicine (TCM) has been developed for thousands of years and has formed an integrated theoretical system based on a large amount of clinical practice. However, essential ingredients in TCM herbs have not been fully identified, and their precise mechanisms and targets are not elucidated. In this study, a new strategy combining comprehensive two-dimensional K562/cell membrane chromatographic system and in silico target identification was established to characterize active components from Indigo naturalis, a famous TCM herb that has been widely used for the treatment of leukemia in China, and their targets...
2016: Scientific Reports
https://www.readbyqxmd.com/read/27125189/determination-of-tyrian-purple-by-high-performance-liquid-chromatography-with-diode-array-detection
#18
Athina Vasileiadou, Ioannis Karapanagiotis, Anastasia Zotou
Indigotin, indirubin, 6-bromoindigotin, 6'-bromoindirubin, 6-bromoindirubin, 6,6'-dibromoindigotin and 6,6'-dibromoindirubin, the colouring components of Tyrian purple, are quantified by an efficient HPLC method coupled to a diode array detector. The compounds were separated using gradient elution, on a RP-column (Alltima C18, 250mm×3.0mm i.d., 5μm), thermostated at 35°C, with a mobile phase consisting of solvents (Α) H2O+0.1% (v/v) trifluoroacetic acid and (Β) acetonitrile+0.1% (v/v) trifluoroacetic acid, at a flow rate of 0...
May 27, 2016: Journal of Chromatography. A
https://www.readbyqxmd.com/read/27106709/discovery-of-indirubin-derivatives-as-new-class-of-drak2-inhibitors-from-high-throughput-screening
#19
Myoung Eun Jung, Byung Jin Byun, Hye-Mi Kim, Joo Yun Lee, Jin-Hee Park, Nari Lee, You Hwa Son, Sang Un Choi, Kyung-Min Yang, Seong-Jin Kim, Kwangho Lee, Yong-Chul Kim, Gildon Choi
DRAK2 is a serine/threonine kinase belonging to the death-associated protein kinase (DAPK) family and has emerged as a promising drug target for the treatment of autoimmune diseases and cancers. To identify small molecule inhibitors for DRAK2, we performed a high throughput screening campaign using in-house chemical library and identified indirubin-3'-monoximes as novel class of DRAK2 inhibitors. Among the compounds tested, compound 16 exhibited the most potent inhibitory activity against DRAK2 (IC50=0.003μM)...
June 1, 2016: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/26987505/indirubin-a-component-of-ban-lan-gen-activates-cyp3a4-gene-transcription-through-the-human-pregnane-x-receptor
#20
Takeshi Kumagai, Yusuke Aratsu, Ryosuke Sugawara, Takamitsu Sasaki, Shinichi Miyairi, Kiyoshi Nagata
Ban-Lan-Gen is the common name for the dried roots of indigo plants, including Polygonum tinctorium, Isatis indigotica, Isatis tinctoria, and Strobilanthes cusia. Ban-Lan-Gen is frequently used as an anti-inflammatory and an anti-viral for the treatment of hepatitis, influenza, and various types of inflammation. One of the cytochrome P450 (CYP) enzymes, CYP3A4, is responsible for the metabolism of a wide variety of xenobiotics, including an estimated 60% of all clinically used drugs. In this study, we investigated the effect of Ban-Lan-Gen on the transcriptional activation of the CYP3A4 gene...
April 2016: Drug Metabolism and Pharmacokinetics
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