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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 2, 2017: Oncotarget
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
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
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
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.]
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
Eleni Tsakiri, Nicolas Gaboriaud-Kolar, Kalliopi Iliaki, Job Tchoumtchoua, Eleni-Dimitra Papanagnou, Sofia Chatzigeorgiou, Konstantinos 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 nutrients sensing pathways 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 lifespan. 6BIO is not metabolized in flies' tissues; modulated bioenergetic pathways, decreased lipid and glucose tissues' load, activated antioxidant and proteostatic modules and enhanced resistance to stressors...
March 2, 2017: Antioxidants & Redox Signaling
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
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
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
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
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
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
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
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
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
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
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
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
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
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