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SYUNZ-16, a newly synthesized alkannin derivative, induces tumor cells apoptosis and suppresses tumor growth through inhibition of PKB/AKT kinase activity and blockade of AKT/FOXO signal pathway.
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Alkannin is the major bioactive compound of Arnebia euchroma roots, which is used in many therapeutic remedies in Chinese traditional medicine. SYUNZ-16 is a new derivative of alkannin. In this study, anticancer effects of SYUNZ-16 on human lung adenocarcinoma cell line GLC-82 and human
Alkannin represses growth of pancreatic cancer cells based on the down regulation of miR-199a.
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Alkannin displays tumor suppressive activity by initiating apoptosis. Here, we corroborated its role in pancreatic carcinoma (PANC-1) cells and addressed the molecular mechanism in which microRNA-199a (miR-199a) and Klotho might be implicated. PANC-1 and MIN6 cells were treated by alkannin and its
Advance in Anti-tumor Mechanisms of Shikonin, Alkannin and Their Derivatives.
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Shikonin, alkannin and their derivatives, the main ingredient of Lithospermum erythrorhizon and Arnebia euchroma (Royle) Johnst native to Inner Mongolian and Northwest of China respectively, hold promising potentials for antitumor effects via multiple-target mechanisms. This review will emphasize
Thermosensitive hydrogels as a controlled release system for alkannin to improve localized treatment of Candida vaginitis after external beam radiotherapy in vitro and in vivo.
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External beam radiotherapy increases the risk of Candida vaginitis in cervical cancer patients, which brings a lot of insufferable influence to their life. Here, we explored the efficacy of alkannin in the treatment of Candida vaginitis after external beam radiotherapy. We exploit thermosensitive
Shikonin and its analogs inhibit cancer cell glycolysis by targeting tumor pyruvate kinase-M2.
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We recently reported that shikonin and its analogs were a class of necroptotic inducers that could bypass cancer drug resistance. However, the molecular targets of shikonin are not known. Here, we showed that shikonin and its analogs are inhibitors of tumor-specific pyruvate kinase-M2 (PKM2), among
Alkannin induces cytotoxic autophagy and apoptosis by promoting ROS-mediated mitochondrial dysfunction and activation of JNK pathway
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Naphthoquinone derivatives and metabolites are widely dispersed molecules in nature. Alkannin, a natural naphthoquinone compound, induces excellent cytotoxicity in cancer cells. However, the detailed mechanism by which alkannin inhibits cancer cell survival remains unclear. In the present study, we
DMAKO-20 as a new multi-target anticancer prodrug activated by the tumor specific CYP1B1 enzyme.
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In order to reduce the pervasive toxicity of natural shikonin, alkannin and their synthetic analogues and to enhance the selectivity of these chemotherapeutics towards cancer cells, a novel 5,8-dimethyl alkannin oxime derivative (DMAKO-20) was designed, synthesized and evaluated for its strong
Synthesis and evaluation of novel alkannin and shikonin oxime derivatives as potent antitumor agents.
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A set of forty alkannin and shikonin oxime derivatives were firstly designed and synthesized. Their cytotoxicities against three kinds of tumor cells and a normal cell line were tested and compared with alkannin and shikonin. The cell-based investigation demonstrated that some oxime derivatives were
Design, synthesis, and biological evaluation of shikonin and alkannin derivatives as potential anticancer agents via a prodrug approach.
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To minimize the cytotoxicity of shikonin and alkannin that arises through the generation of reactive oxygen species (ROS) and alkylation of the naphthazarin ring, two series of novel core-scaffold-modified shikonin and alkannin derivatives were designed. These derivatives, which differ in their
Alkannin restrains oral squamous carcinoma cell growth, migration and invasion by regulating microRNA-9/RECK axis.
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Alkannin (ALK) has anti-inflammatory and anti-tumour activities. We tried to probe the underlying functions of ALK in oral squamous carcinoma (OSCC) cells growth, migration and invasion. OSCC cells viability was investigated after treatment with ALK. Then, BrdU, flow cytometry, Western blot and
Naphthoquinone components from Alkanna tinctoria (L.) Tausch show significant antiproliferative effects on human colorectal cancer cells.
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Our research to seek active compounds against human colorectal cancer from the root of Alkanna tinctoria (L.) Tausch led to the isolation of two naphthoquinones, alkannin (1) and angelylalkannin (2). The antiproliferative effects of the two compounds on human colon cancer cells HCT-116 and SW-480
Suppressive effect of β, β-dimethylacryloyl alkannin on activated dendritic cells in an imiquimod-induced psoriasis mouse model.
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OBJECTIVE
To investigate the effect of β, β-dimethylacryloyl alkannin, a main component of Lithospermum erythrorhizon, on activated dendritic cells (DCs) in a psoriasis mouse model.
METHODS
BALB/c mice were used to establish the animal model for psoriasis-like skin lesion; alkannin at 10 mg/kg
Alkannin inhibits proliferation, migration and invasion of hepatocellular carcinoma cells via regulation of miR-92a.
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Effect of Onosma echioides on DMBA/croton oil mediated carcinogenic response, hyperproliferation and oxidative damage in murine skin.
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The current study unveils the effect of O. echioides extract on two-stage skin carcinogenesis and on tumor promoter induced markers and oxidative stress in Swiss mice. Treatment of dorsal shaven cutaneous portions of the mice with single topical application of benzoyl peroxide (BPO) followed by
Sterically stabilized liposomes as a potent carrier for shikonin.
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The ability of pegylated liposomes (sterically stabilized liposomes-SSL) to localize in solid tumors via the enhanced permeability and retention (EPR) effect, partly depends on their long circulating properties which can be achieved by grafting polyethylene glycol (PEG) to the liposomes' surface.
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