Curaderm — or is it?

Coramsine is a novel chemotherapeutic agent isolated from Solanum linnaeanum (devil's apple). Topical treatment provides clinical benefit for skin tumors. To evaluate the potential broader applicability of the drug, its in vivo anticancer efficacy in a murine model of malignant mesothelioma and its mode of action were investigated. Systemic administration of coramsine slowed tumor growth and prolonged survival time. Importantly, the antitumor efficacy of coramsine was enhanced when treatment was combined with stimulation of innate immunity using unmethylated CpG-containing oligodeoxynucleotides (ODNs). Combination treatment further slowed tumor growth and provided a survival benefit. Coramsine seems to kill tumor cells by direct cell lysis. Using 2 different assays to detect apoptosis (caspase activation and DNA fragmentation), we found no evidence that coramsine induces any form of programmed cell death. The fact that the efficacy of coramsine is potentiated by CpG ODNs suggests that coramsine-induced cell death is an immunologic null event.

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Synthesis of solasodine glycoside derivatives and evaluation of their cytotoxic effects on human cancer cells

Cui

Wen

Cui

et al. 2012

Drug Discov Ther

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Solasodine glycosides, such as solamargine, have been proved to be very important anti-cancer agents. In order to discover more potent cytotoxic agents and explore the preliminary structure activity relationship, a new series of solasodine glycosides 2-9 were synthesized via a transglycosylation strategy, and their cytotoxic activity against a panel of human cancer cell lines (MCF-7, KB, K562, and PC3 cells) were evaluated by MTT assays. The results indicated that compounds 2, 8, and 9 with the substitute moiety of rhamnose, 2-hydroxyethoxymethyl, and 1,3-dihydroxypropan-2-yloxy-methyl, respectively, exhibited quite strong anticancer activity. The underlying mechanism tests demonstrated that these compounds could induce apoptosis detected by DAPI staining, and Annexin V and propidium iodide binding. Cell cycle analysis indicated that the cancer cells were predominantly arrested at the G2/M phase when exposure to these compounds was examined by flow cytometry. These compounds may serve as lead candidates in the development of novel chemotherapeutics for cancer treatment.

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Curaderm — or is it?

Cited by 3 publications

References 5 publications

Chemistry of Trisdecacyclic Pyrazine Antineoplastics: The Cephalostatins and Ritterazines † This review is dedicated to the community of isolation/identification natural product detectives, with special thanks to the groups of Bob Pettit and Nobuhiro Fusatani.

Chemistry of Trisdecacyclic Pyrazine Antineoplastics: The Cephalostatins and Ritterazines † This review is dedicated to the community of isolation/identification natural product detectives, with special thanks to the groups of Bob Pettit and Nobuhiro Fusatani.

Antitumor Efficacy of the Novel Chemotherapeutic Agent Coramsine Is Potentiated by Cotreatment With CpG-Containing Oligodeoxynucleotides

Synthesis of solasodine glycoside derivatives and evaluation of their cytotoxic effects on human cancer cells

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