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Identification of new shikonin derivatives as STAT3 inhibitors

Biochemical Pharmacology, 2017
The signal transducer and activator of transcription 3 is a constitutively activated oncogenic protein in various human tumors and represents a valid target for anticancer drug design. In this study, we have achieved a new type of STAT3 inhibitors based on structural modifications on shikonin scaffold, guided by computational modelling.
Han-Yue, Qiu   +12 more
openaire   +2 more sources

Structure determination of oligomeric alkannin and shikonin derivatives

Biomedical Chromatography, 2005
AbstractMonomeric alkannin and shikonin (A/S) are potent pharmaceutical substances with a wide spectrum of biological activity and comprise the active ingredients for several pharmaceutical preparations. Therefore, the determination of the impurities, degradation products or byproducts in alkannin and shikonin samples is of great importance. Oligomeric
Apostolos, Spyros   +2 more
openaire   +2 more sources

Addition of β-Lactoglobulin Produces Water-Soluble Shikonin

Journal of Agricultural and Food Chemistry, 2012
Shikonin and its ester derivatives belong to a group of secondary metabolites with a wide array of beneficial effects on human health. However, shikonin is principally used in oil-based preparations due to the low solubility of the pigment in aqueous media, and the positive properties of shikonin are not exploited to their full potential.
Alen, Albreht   +2 more
openaire   +2 more sources

Functional and mechanistic investigation of Shikonin in scarring

Chemico-Biological Interactions, 2015
Scarring is a significant medical burden; financially to the health care system and physically and psychologically for patients. Importantly, there have been numerous case reports describing the occurrence of cancer in burn scars. Currently available therapies are not satisfactory due to their undesirable side-effects, complex delivery routes ...
Yan Xie   +8 more
openaire   +3 more sources

Shikonin ameliorates cerulein-induced acute pancreatitis in mice

Journal of Ethnopharmacology, 2013
Shikonin, a highly liposoluble naphthoquinone pigment isolated from the traditional medical herbs Lithospermum erythrorhizon (LE), was considered to exhibit an anti-inflammatory property. While the potential of shikonin to ameliorate acute pancreatitis (AP) is unknown.
Jie, Xiong   +13 more
openaire   +2 more sources

Shikonin alleviates the biotoxicity produced by pneumococcal pneumolysin

Life Sciences, 2017
Streptococcus pneumoniae (S. pneumoniae) is a common pathogen that can cause severe infections in humans. Pneumolysin (PLY) is an important virulence trait of S. pneumoniae and has cytotoxicity, genotoxicity and pro-inflammatory activity; it is essential for the pathogenesis of S.
Xiaoran, Zhao   +6 more
openaire   +2 more sources

Necrostatin-1 reverts shikonin-induced necroptosis to apoptosis

Apoptosis, 2009
Degterev et al. previously demonstrated that death receptor mediated apoptosis could be diverted to necroptosis when apoptosis signaling was blocked, suggesting that necroptosis may function as a backup mechanism to insure the elimination of damaged cells under certain conditions when apoptosis was inhibited.
Weidong, Han   +4 more
openaire   +2 more sources

Novel Shikonin Derivatives Targeting Tubulin as Anticancer Agents

Chemical Biology & Drug Design, 2014
In this study, we report the identification of a new shikonin‐phenoxyacetic acid derivative, as an inhibitor of tubulin. A series of compounds were prepared; among them, compound 16 [(R) ‐1 ‐ (5, 8‐ dihydroxy‐1, 4‐ dioxo‐1, 4‐ dihydronaphthalen‐2‐yl)‐4‐methylpent‐3‐enyl 2‐ (4‐ phenoxyphenyl) acetate] potently inhibited the function of microtubules ...
Jing, Guo   +12 more
openaire   +2 more sources

Synthesis and antitumor activity of new shikonin glycosides

European Journal of Medicinal Chemistry, 2010
Eleven shikonin glycosides were synthesized and evaluated for their antitumor activity in vitro. Some of them were found to exhibit cytotoxic activities against both drug sensitive cell lines (K562, MCF-7 and HL60) and their drug resistant cell sublines (K562/ADR, MCF-7/ADR and HL60/ADR).
Yehua, Su   +4 more
openaire   +2 more sources

Photochemical decomposition of alkannin/shikonin enantiomers

International Journal of Pharmaceutics, 1995
Abstract Alkannin/shikonin ((±)-5,8-dihydroxy-2-(1-hydroxy-4-methyl-3-pentenyl)-1,4-naphthoquinone), isolated from Macrotomia euchroma , is sensitive to light exposure. A chloroform solution of alkannin/shikonin was exposed to sunlight for 1 month. The major photolytic product, a newly discovered naphthoquinone derivative, was isolated by adsorption
openaire   +1 more source

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