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Anti-tumor activity of new artemisinin-chalcone hybrids.

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In an attempt to develop potent and selective anti-tumor agents, three new series of artemisinin-chalcone hybrids 10a-10g, 11a-11g and 12a-12h were designed, synthesized and screened for their anti-tumor activity against five cell lines (HT-29, A549, MDA-MB-231, HeLa and H460) in vitro. Among

Synthesis and anti-cancer activity of covalent conjugates of artemisinin and a transferrin-receptor targeting peptide.

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Artemisinin, a natural product isolated from Artemisia annua L., shows a unique anti-cancer activity by an iron dependent mechanism. Artemisinin was covalently conjugated to a transferrin-receptor targeting peptide, HAIYPRH that binds to a cavity on the surface of transferrin receptor. This enables

Comparative cytotoxicity of artemisinin and cisplatin and their interactions with chlorogenic acids in MCF7 breast cancer cells.

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In parts of Africa and Asia, self-medication with a hot water infusion of Artemisia annua (Artemisia tea) is a common practice for a number of ailments including malaria and cancer. In our earlier work, such an extract showed better potency than artemisinin alone against both chloroquine-sensitive

Design and synthesis of novel artemisinin derivatives with potent activities against colorectal cancer in vitro and in vivo.

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A series of novel derivatives of artemisinin-4-(arylamino)quinazoline have been designed and synthesized, and most of them showing potent in vitro cytotoxic activity against HCT116 and WM-266-4 cell lines. Compound 32 was the most active derivative against HCT116 cell line with an IC₅₀ of

Preclinical Efficacy and Safety Assessment of Artemisinin-Chemotherapeutic Agent Conjugates for Ovarian Cancer.

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Artemisinin (ARS) and its derivatives, which are clinically used antimalarial agents, have shown antitumor activities. Their therapeutic potencies, however, are limited by their low solubility and poor bioavailability. Here, through a pharmacophore hybridization strategy, we synthesized ARS-drug

Artemisinin selectively decreases functional levels of estrogen receptor-alpha and ablates estrogen-induced proliferation in human breast cancer cells.

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MCF7 cells are an estrogen-responsive human breast cancer cell line that expresses both estrogen receptor (ER) alpha and ERbeta. Treatment of MCF7 cells with artemisinin, an antimalarial phytochemical from the sweet wormwood plant, effectively blocked estrogen-stimulated cell cycle progression

Artemisinin disrupts androgen responsiveness of human prostate cancer cells by stimulating the 26S proteasome-mediated degradation of the androgen receptor protein.

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Androgen receptor (AR) expression and activity is highly linked to the development and progression of prostate cancer and is a target of therapeutic strategies for this disease. We investigated whether the antimalarial drug artemisinin, which is a sesquiterpene lactone isolated from the sweet

Recent Progresses in Cancer Nanotherapeutics Design Using Artemisinins as Free Radical Precursors

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Artemisinin and its derivatives (ARTs) are sort of important antimalarials, which exhibit a wide range of biological activities including anticancer effect. To solve the issues regarding poor solubility and limited bioavailability of ARTs, nanoformulation of ARTs has thus emerged as a promising

Artemisinin-transferrin conjugate retards growth of breast tumors in the rat.

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BACKGROUND Artemisinin is a compound isolated from the wormwood Artemisia annua L. It reacts with iron and forms cytotoxic free radicals. It is selectively more toxic to cancer than normal cells because cancer cells contain significantly more intracellular free iron. Previously, we found that

Oral artemisinin prevents and delays the development of 7,12-dimethylbenz[a]anthracene (DMBA)-induced breast cancer in the rat.

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Artemisinin, a compound isolated from the sweet wormwood Artemisia annua L., has previously been shown to have selective toxicity towards cancer cells in vitro. In the present experiment, we studied the potential of artemisinin to prevent breast cancer development in rats treated with a single oral

Synthesis of Tamoxifen-Artemisinin and Estrogen-Artemisinin Hybrids Highly Potent Against Breast and Prostate Cancer.

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In search for new and effective treatments of breast and prostate cancer, a series of hybrid compounds based on tamoxifen, estrogens and artemisinin were successfully synthesized and analyzed towards their in vitro activities against human prostate (PC-3) and breast cancer (MCF-7) cell lines. Most

Bioinformatic and experimental fishing for artemisinin-interacting proteins from human nasopharyngeal cancer cells.

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Determining interacting cellular partners of drugs by chemical proteomic techniques is complex and tedious. Most approaches rely on activity-based probe profiling and compound-centric chemical proteomics. The anti-malarial artemisinin also exerts profound anti-cancer activity, but the mechanisms of

A survey on anticancer effects of artemisinin, iron, miconazole, and butyric acid on 5637 (bladder cancer) and 4T1 (Breast cancer) cell lines.

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BACKGROUND Anticancer properties of artemisinin and its derivatives have been shown in many experiments. OBJECTIVE Addition of butyric acid, miconazole, and iron to this traditional drug has been done in order to enhance its anticancer potency. METHODS Cell lines 5637 and 4T1, were cultivated and

Artemisinin sensitizes tumor cells to NK cell-mediated cytolysis.

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The antimalarial drug Artemisinin has been reported to possess direct anti-tumor effects on various types of tumor cells. However, its anti-tumor potential has not been fully revealed, and its effects on tumor susceptibility to immune surveillance by the host are still unknown. Natural killer (NK)

Artemisinin enhances the anti-tumor immune response in 4T1 breast cancer cells in vitro and in vivo.

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Breast cancer is a prominent cause of death among women worldwide. Recent studies have demonstrated that artemisinin (ART) displays anti-tumor activity. Using a mouse breast cancer model, we investigated the effects of ART in vitro and in vivo to determine how it influences the

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