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https://www.readbyqxmd.com/read/29678463/design-synthesis-and-antineoplastic-activity-of-novel-hybrids-of-podophyllotoxin-and-indirubin-against-human-leukaemia-cancer-cells-as-multifunctional-anti-mdr-agents
#1
Jing Wang, Li Long, Yongzheng Chen, Yingshu Xu, Lei Zhang
To overcome cancer drug resistance, in present study, a series of podophyllotoxin-indirubin hybrids were designed, synthesized, and evaluated for anticancer efficacy against two human chronic myeloid leukemia cell cultures. Among them, compound Da-1 was the most potent in resistent K562/VCR cells with an IC50 value of 0.076 ± 0.008 μM. Preliminary mechanism studies showed that Da-1 significantly induced apoptosis and cell cycle arrest at the G2 phase. Decrease in mitochondrial membrane potential, accompanied by activated PARP cleavage, was observed in K562/VCR cells after incubation with Da-1...
April 10, 2018: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/29678389/vascular-smooth-muscle-cell-proliferation-as-a-therapeutic-target-part-2-natural-products-inhibiting-proliferation
#2
REVIEW
Pavel Uhrin, Dongdong Wang, Andrei Mocan, Birgit Waltenberger, Johannes M Breuss, Devesh Tewari, Judit Mihaly-Bison, Łukasz Huminiecki, Rafał R Starzyński, Nikolay T Tzvetkov, Jarosław Horbańczuk, Atanas G Atanasov
Many natural products have been so far tested regarding their potency to inhibit vascular smooth muscle cell proliferation, a process involved in atherosclerosis, pulmonary hypertension and restenosis. Compounds studied in vitro and in vivo as VSMC proliferation inhibitors include, for example indirubin-3'-monoxime, resveratrol, hyperoside, plumericin, pelargonidin, zerumbone and apamin. Moreover, taxol and rapamycin, the most prominent compounds applied in drug-eluting stents to counteract restenosis, are natural products...
April 17, 2018: Biotechnology Advances
https://www.readbyqxmd.com/read/29671340/the-combination-of-indirubin-and-isatin-attenuates-dextran-sodium-sulfate-induced-ulcerative-colitis-in-mice
#3
Wenyan Gao, Luding Zhang, Xiaoqian Wang, Li Yu, Changhong Wang, Yang Gong
Indirubin and isatin have been used in the treatment of inflammatory diseases due to their anti-inflammatory properties. The present study aimed to evaluate the combined effect of indirubin and isatin on dextran sulfate sodium (DSS)-induced ulcerative colitis (UC). UC was induced by administration of 3% (w/v) DSS solution and then the model mice were administered indirubin (10 mg/kg) or/and isatin (10 mg/kg) by gavage once daily for a week. The results showed that indirubin or/and isatin significantly inhibited weight loss, lowered disease activity index (DAI), ameliorated pathological changes, decreased the levels of pro-inflammatory mediators and myeloperoxidase (MPO) activity, increased anti-inflammatory cytokine and Foxp3 expression, suppressed CD4+ T cell infiltration, and inhibited oxidative stress and epithelial cell apoptosis...
April 19, 2018: Biochemistry and Cell Biology, Biochimie et Biologie Cellulaire
https://www.readbyqxmd.com/read/29603199/indirubin-and-nad-prevent-mitochondrial-ischemia-reperfusion-damage-in-fatty-livers
#4
João Soeiro Teodoro, Ana Teresa Varela, Filipe Valente Duarte, Ana Patrícia Gomes, Carlos Marques Palmeira, Anabela Pinto Rolo
BACKGROUND: Fatty livers are considerably more susceptible to acute stressors, such as ischemia/reperfusion (I/R). Since the incidence of I/R is high due to surgical events and some pathologies, there is an urgent need to find strategies against I/R injury (I/RI) in fatty livers. We postulate that an acute pre-treatment with Indirubin-3'-oxime (Ind) or NAD+ prevents mitochondrial dysfunction associated with warm I/RI in fatty livers. MATERIALS AND METHODS: Zucker fatty rats were subjected to warm ischemia and 12 hrs of reperfusion...
March 30, 2018: European Journal of Clinical Investigation
https://www.readbyqxmd.com/read/29439254/inhibition-of-suicidal-erythrocyte-death-by-indirubin-3-monoxime
#5
Chunqiu Liu, Peipei Jiang, Yuanhong Xu, Meijuan Zheng, Jinpin Qiao, Xueyong Zhou, Dake Huang, Maohong Bian
BACKGROUND/AIMS: Qing Dai is a prized traditional Chinese medicine whose major component, indirubin, and its derivative, indirubin-3'-monoxime (IDM), have inhibitory effects on the growth of many human tumor cells and pronounced anti-leukemic activities. However, the effects of IDM on mature human erythrocytes are unclear. This study aimed to evaluate the potential impact of IDM on erythrocytes and the mechanisms underlying that impact. METHODS: Utilizing flow cytometry and confocal laser scanning microscopy, phosphatidylserine exposure at the cell surface was estimated by annexin V-fluorescein isothiocyanate (FITC)...
February 7, 2018: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/29416667/discovery-of-a-flt3-inhibitor-ldd1937-as-an-anti-leukemic-agent-for-acute-myeloid-leukemia
#6
Hyo Jeong Lee, Jungeun Lee, Pyeonghwa Jeong, Jungil Choi, Juhwa Baek, Su Jin Ahn, Yeongyu Moon, Jeong Doo Heo, Young Hee Choi, Young-Won Chin, Yong-Chul Kim, Sun-Young Han
FMS-like receptor tyrosine kinase-3 (FLT3) belongs to the family of receptor tyrosine kinase (RTK), and the FLT3 mutation is observed in 1/3 of all acute myeloid leukemia (AML) patients. Potential FLT3 inhibitors have been investigated as potential therapeutic agents of AML. In this study, we identified a potent FLT3 inhibitor LDD1937 containing an indirubin skeleton. The potent inhibitory activity of LDD1937 against FLT3 was shown with an in vitro kinase assay (IC 50 = 3 nM). The LDD1937 compound selectively inhibited the growth of MV-4-11 cells (GI 50 = 1 nM) and induced apoptotic cell death...
January 2, 2018: Oncotarget
https://www.readbyqxmd.com/read/29357584/indirubin-a-novel-topical-agent-in-the-treatment-of-psoriasis
#7
S Sekhon, J Koo
No abstract text is available yet for this article.
January 2018: British Journal of Dermatology
https://www.readbyqxmd.com/read/29331686/quercetin-decrease-somatic-cells-count-in-mastitis-of-dairy-cows
#8
Artur Burmańczuk, Piotr Hola, Andrzej Milczak, Tomasz Piech, Cezary Kowalski, Beata Wojciechowska, Tomasz Grabowski
Quercetin is a dietary flavonoid which has an effect on inflammation, angiogenesis and vascular inflammation. In several other flavonoids (e.g. kaempferol, astragalin, alpinetin, baicalein, indirubin), anti-inflammatory mechanism was proven by using mice mastitis model. The aim of the current study was pilot analysis of quercetin tolerability and its impact on somatic cells count (SCC) after multiple intramammary treatment on dairy cows with clinical mastitis. Based on SCC and clinical investigation, 9 dairy cows with clinical mastitis of one quarter were selected for the pilot study...
April 2018: Research in Veterinary Science
https://www.readbyqxmd.com/read/29301095/metabolic-engineering-of-escherichia-coli-for-the-production-of-indirubin-from-glucose
#9
Jikun Du, Dongsoo Yang, Zi Wei Luo, Sang Yup Lee
Indirubin is an indole alkaloid that can be used to treat various diseases including granulocytic leukemia, cancer, and Alzheimer's disease. Microbial production of indirubin has so far been achieved by supplementation of rather expensive substrates such as indole or tryptophan. Here, we report the development of metabolically engineered Escherichia coli strain capable of producing indirubin directly from glucose. First, the Methylophaga aminisulfidivorans flavin-containing monooxygenase (FMO) and E. coli tryptophanase (TnaA) were introduced into E...
February 10, 2018: Journal of Biotechnology
https://www.readbyqxmd.com/read/29285277/indirubin-a-bisindole-alkaloid-from-isatis-indigotica-reduces-h1n1-susceptibility-in-stressed-mice-by-regulating-mavs-signaling
#10
Chong Jie, Zhuo Luo, Huan Chen, Min Wang, Chang Yan, Zhong-Fu Mao, Gao-Keng Xiao, Hiroshi Kurihara, Yi-Fang Li, Rong-Rong He
Isatis indigotica has a long history in treating virus infection and related symptoms in China. Nevertheless, its antivirus evidence in animal studies is not satisfactory, which might be due to the lack of appropriate animal model. Previously, we had utilized restraint stress to establish mouse H1N1 susceptibility model which was helpful in evaluating the anti-virus effect of medicines targeting host factors, such as type I interferon production. In this study, this model was employed to investigate the effect and mechanism of indirubin, a natural bisindole alkaloid from Isatis indigotica , on influenza A virus susceptibility...
December 1, 2017: Oncotarget
https://www.readbyqxmd.com/read/29274785/indirubin-3-oxime-inhibits-anticancer-agent-induced-yb-1-nuclear-translocation-in-hepg2-human-hepatocellular-carcinoma-cells
#11
Toru Tanaka, Sachiyo Ohashi, Hiroaki Saito, Taira Wada, Tadashi Aoyama, Yoshimi Ichimaru, Shinichi Miyairi, Shunsuke Kobayashi
Hepatocellular carcinoma (HCC) is a disease with poor prognosis. Nuclear accumulation of YB-1 is closely related to the malignancy of HCC. Treatment with anticancer agents often induces translocation of YB-1 from cytoplasm to nucleus and activates the expression of multidrug resistance gene 1 (MDR1). Therefore, any effective inhibitor of this phenomenon would be useful for cancer treatment. Here we examined various indirubin derivatives and found that indirubin 3'-oxime inhibits actinomycin D-induced nuclear transport of YB-1 and suppresses the activation of MDR1 gene expression in the human hepatocellular carcinoma cell line HepG2...
January 29, 2018: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/29234273/indirubin-derivative-7-bromoindirubin-3-oxime-7bio-attenuates-a%C3%AE-oligomer-induced-cognitive-impairments-in-mice
#12
Liping Chen, Chunhui Huang, Jieyi Shentu, Minjun Wang, Sicheng Yan, Fei Zhou, Zaijun Zhang, Chuang Wang, Yifan Han, Qinwen Wang, Wei Cui
Indirubins are natural occurring alkaloids extracted from indigo dye-containing plants. Indirubins could inhibit various kinases, and might be used to treat chronic myelocytic leukemia, cancer and neurodegenerative disorders. 7-bromoindirubin-3-oxime (7Bio), an indirubin derivative derived from indirubin-3-oxime, possesses inhibitory effects against cyclin-dependent kinase-5 (CDK5) and glycogen synthase kinase-3β (GSK3β), two pharmacological targets of Alzheimer's disease (AD). In this study, we have discovered that 2...
2017: Frontiers in Molecular Neuroscience
https://www.readbyqxmd.com/read/29122482/indirubin-derivatives-protect-against-endoplasmic-reticulum-stress-induced-cytotoxicity-and-down-regulate-chop-levels-in-ht22-cells
#13
Yasuhiro Kosuge, Hiroaki Saito, Tatsuki Haraguchi, Yoshimi Ichimaru, Sachiyo Ohashi, Hiroko Miyagishi, Shunsuke Kobayashi, Kumiko Ishige, Shinichi Miyairi, Yoshihisa Ito
Indirubin and its derivatives have been reported to exhibit anti-cancer and anti-inflammatory activities. Recently, some of its derived analogs have been shown to have neuroprotective potential. Endoplasmic reticulum (ER) stress has been demonstrated to contribute to the pathogenesis of various neurodegenerative diseases, whereas the effects of indirubin derivatives on ER stress-induced cell death have not been addressed. In the present study, a series of 44 derivatives of indirubin was prepared to search for a novel class of neuroprotective agents against ER stress-induced neuronal death...
December 1, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/29039496/gsk-3%C3%AE-inhibitor-6-bromo-indirubin-3-oxime-promotes-both-adhesive-activity-and-drug-resistance-in-colorectal-cancer-cells
#14
Kunping Liu, Jinbang Li, Xuefang Wu, Meixiang Chen, Feng Luo, Jun Li
Multi-targets inhibitor 6-bromo-indirubin-3'-oxime (BIO) has diverse biological effects on cancer cells. The key component of the β-catenin destruction complex glycogen synthase kinase 3β (GSK-3β), one of the major target for BIO, polyubiquitination and degradation of the main oncoprotein β-catenin in colorectal cancer (CRC). In the present study, we evaluated the effect of BIO on drug resistance and biological properties of CRC cells. Whole-genome transcriptional profiling revealed that differentially expressed genes were mainly centered on well-characterized signaling pathways including stem cell, cell adhesion and cell growth in BIO-treated CRC cells...
October 16, 2017: International Journal of Oncology
https://www.readbyqxmd.com/read/28916781/6-bromo-indirubin-3-oxime-6bio-a-glycogen-synthase-kinase-3%C3%AE-inhibitor-activates-cytoprotective-cellular-modules-and-suppresses-cellular-senescence-mediated-biomolecular-damage-in-human-fibroblasts
#15
Aimilia D Sklirou, Nicolas Gaboriaud-Kolar, Issidora Papassideri, Alexios-Leandros Skaltsounis, Ioannis P Trougakos
As genetic interventions or extended caloric restriction cannot be applied in humans, many studies have been devoted to the identification of natural products that can prolong healthspan. 6-bromoindirubin-3'-oxime (6BIO), a hemi-synthetic derivative of indirubins found in edible mollusks and plants, is a potent inhibitor of Glycogen synthase kinase 3β (Gsk-3β). This pleiotropic kinase has been implicated in various age-related diseases including tumorigenesis, neurodegeneration and diabetes. Accordingly, 6BIO has shown anti-tumor and anti-neurodegenerative activities; nevertheless, the potential role of 6BIO in normal human cells senescence remains largely unknown...
September 15, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28817720/targeting-of-cdk9-with-indirubin-3-monoxime-safely-and-durably-reduces-hiv-viremia-in-chronically-infected-humanized-mice
#16
Sandra Medina-Moreno, Thomas C Dowling, Juan C Zapata, Nhut M Le, Edward Sausville, Joseph Bryant, Robert R Redfield, Alonso Heredia
Successful propagation of HIV in the human host requires entry into a permissive cell, reverse transcription of viral RNA, integration into the human genome, transcription of the integrated provirus, and assembly/release of new virus particles. Currently, there are antiretrovirals against each of these viral steps, except for provirus transcription. An inhibitor of HIV transcription could both increase potency of treatment and suppress drug-resistant strains. Cellular cyclin-dependent kinase 9 (CDK9) serves as a cofactor for the HIV Tat protein and is required for effective transcription of the provirus...
2017: PloS One
https://www.readbyqxmd.com/read/28815560/comparison-of-indirubin-concentrations-in-indigo-naturalis-ointment-for-psoriasis-treatment-a-randomized-double-blind-dosage-controlled-trial
#17
Y K Lin, L C See, Y H Huang, C C Chi, R C Y Hui
BACKGROUND: Indigo naturalis and its refined formulation, Lindioil, are effective in treating psoriatic symptoms topically. Indirubin is the active ingredient in indigo naturalis. OBJECTIVES: To determine the efficacy and safety of different concentrations of indirubin in Lindioil ointment for treating psoriasis. METHODS: In this randomized, double-blind trial, adult patients presenting with chronic plaque psoriasis for >1 year and with <20% of the body surface area (BSA) affected were randomized to apply Lindioil ointment containing 200 μg/g, 100 μg/g, 50 μg/g, or 10 μg/g of indirubin twice daily for 8 weeks followed by an additional 12-week safety/extension period...
August 17, 2017: British Journal of Dermatology
https://www.readbyqxmd.com/read/28743492/5-bromoindirubin-3-o-oxiran-2-ylmethyl-oxime-a-long-acting-anticancer-agent-and-a-suicide-inhibitor-for-epoxide-hydrolase
#18
Yoshimi Ichimaru, Takeshi Fujii, Hiroaki Saito, Makoto Sano, Taketo Uchiyama, Shinichi Miyairi
Indirubin 3'-oxime (Indox (1b)) suppresses cancer cell growth (IC50 : 15μM towards HepG2 cells) and inhibits cell cycle-related kinases such as cyclin-dependent kinases and glycogen synthase kinase-3β. We have previously reported that the conjugation of 1b with oxirane, a protein-reactive component, enhanced the cytotoxic activity of Indox as determined from the IC50 value (1.7μM) of indirubin 3'-(O-oxiran-2-ylmethyl)oxime (Epox/Ind (1c)). Here we prepared Epox/Ind derivatives with one or two halogen atoms or a methoxy group on the aromatic ring(s) of an Indox moiety and studied the structure-activity relationships of the substituent(s)...
September 1, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28738722/effects-of-indirubin-and-isatin-on-cell-viability-mutagenicity-genotoxicity-and-bax-ercc1-gene-expression
#19
Manoela Viar Fogaça, Priscila de Matos Cândido-Bacani, Lucas Milanez Benicio, Lara Martinelli Zapata, Priscilla de Freitas Cardoso, Marcelo Tempesta de Oliveira, Tamara Regina Calvo, Eliana Aparecida Varanda, Wagner Vilegas, Ilce Mara de Syllos Cólus
CONTEXT: Indigofera suffruticosa Miller (Fabaceae) and I. truxillensis Kunth produce compounds, such as isatin (ISA) and indirubin (IRN), which possess antitumour properties. Their effects in mammalian cells are still not very well understood. OBJECTIVE: We evaluated the activities of ISA and/or IRN on cell viability and apoptosis in vitro, their genotoxic potentials in vitro and in vivo, and the IRN- and ISA-induced expression of ERCC1 or BAX genes. MATERIALS AND METHODS: HeLa and/or CHO-K1 cell lines were tested (3 or 24 h) in the MTT, Trypan blue exclusion, acridine orange/ethidium bromide, cytokinesis-blocked micronucleus (CBMN) and comet (36, 24 and 72 h) tests after treatment with IRN (0...
December 2017: Pharmaceutical Biology
https://www.readbyqxmd.com/read/28700696/small-molecule-inhibition-of-pyruvate-phosphate-dikinase-targeting-the-nucleotide-binding-site
#20
Alexander Minges, Georg Groth
Pyruvate phosphate dikinase (PPDK) is an essential enzyme of C4 photosynthesis in plants, catalyzing the ATP-driven conversion of pyruvate to phosphoenolpyruvate (PEP). It is further used by some bacteria and unicellular protists in the reverse, ATP-forming direction. Many weed species use C4 photosynthesis in contrast to world's major crops, which are C3 plants. Hence inhibitors of PPDK may be used as C4-specific herbicides. By screening a library of 80 commercially available kinase inhibitors, we identified compounds derived from bisindolylmaleimide (bisindolylmaleimide IV, IC50 = 0...
2017: PloS One
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