Coompo Research Chemicals

Solamargine possessed a potent cytotoxicity to human hepatocyte (Hep3B) and normal skin fibroblast. The inhibition curves of solamargine to the both cells were essentially overlapped, suggesting a parallel effect for the cell death. To define mechanism of cytotoxicity of solamargine, the changes of morphology and DNA content in cells were studied. A sub-G1 cell stage was drastically increased after 3-h incubation with solamargine. The results evidence that solamargine arises cell death by apoptosis. In addition, the gene expression of TNFR I were up-regulated within 30 min of solamargine treatment. Since TNF Receptor I has been involved in apoptosis, the overexpression of TNF receptor I may be related with the mechanism of cytotoxicity of solamargine. This communication is the first report that a component of Chinese herbs triggers gene expression of human TNFR I which may lead to cell apoptosis.

SM (solamargine) triggered apoptosis of breast cancer cells (MCF-7 and SK-BR-3 cells) and non-cancerous breast epithelial cells (HBL-100 cells) within 3 h. To extend the application of trastuzumab in breast cancer patients, the regulation of HER2/neu expression by SM was investigated. SM significantly up-regulates HER2/neu expression in breast cancer cells with low and high expression levels of HER2/neu, and synergistically enhanced the effect of trastuzumab in inhibiting cell proliferation. Additionally, HER2/neu and TOP2A [TopoII (topoisomerase II) alpha] genes share the same amplicon on an identical chromosome. Notably, SM co-regulates HER2/neu and TopoIIalpha expression markedly, and enhances TopoII inhibitor-EPI (epirubicin)-induced cytotoxicity to breast cancer cells.

Solamargine could modulate the expressions of TNFRs and Bcl-2, and might be a potential anticancer agent for TNFs and Bcl-2 related resistance of human lung cancer cells.

Solamargine display antifungical, schistosomicidal, antiprotozoal, molluscicidal, antiviral, antimutagenic, and antineoplasic activities against a variety of neoplastic cell lines, as well as hypoglycemic and gastric emptying inhibitory activities.

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