Background: Cancer is one of the leading causes of illness and death worldwide. Only palliative therapeutic options are available for many types of cancers, and most anticancer drugs in clinical use exhibit significant side effects. It is therefore important to develop new anticancer drugs that are more effective and less toxic. In this study, we evaluate the bioactivity of a Philippine endemic plant, "katmon" or Dillenia philippinensis, and its potential use in cancer therapy. Methods: The cytotoxicity of the crude leaf extract, partitions, and isocratic column chromatography fractions of Dillenia philippinensis was determined in vitro by MTT assay against drug-sensitive cancer cell lines MCF7 (human breast adenocarcinoma) and HCT 116 (human colorectal carcinoma), as well as against moderately multidrug resistant (MDR) cancer cell line HCT-15 (human colorectal carcinoma) and its highly MDR subline HCT-15/Dox. The selectivity of the extract to cancer cells was determined by computing for the selectivity index (SI) with respect to normal mouse embryonic fibroblasts (NIH/3T3) cell line. To check for a possible mechanism for overcoming cancer multiple drug resistance, Calcein-AM assay was performed to assess the activity of the extract against P-glycoprotein-activated efflux pump. Results: Dillenia philippinensis (DP1) fraction from the hexane partition exhibited cytotoxicity (IC 50 < 30 µg/ml) against MCF7, HCT 116, HCT-15, and HCT-15/Dox cells. DP1 also exhibited a moderate level of selectivity against cancer cells over normal cells as supported by the SI computed from the IC 50 value obtained for the normal cell line. DP1 was able to inhibit P-glycoprotein (P-gp) activity in a dose-dependent manner, suggesting its possible role in targeting cancer cells with overexpressed P-gp. Conclusion: The present findings thus demonstrate the potential chemotherapeutic properties of D. philippinensis which can be promising for future drug development against cancer.
Ultrashort cationic lipopeptides (USCLs) are amphiphiles that exhibit antimicrobial and anticancer activity. They are composed of an aliphatic chain attached to a positively charged peptide group consisting of a few amino acid residues. Here, we report the activity of a series of l‐2,4‐diaminobutyric acid (Dab)‐rich USCLs with varying N‐acyl chain length and charge against Escherichia coli, Staphylococcus aureus, Candida albicans, colon, breast, and lung epithelial cancer cell lines. USCLs with chain lengths of 14–18 carbons showed significant antimicrobial activity with C16‐conjugated peptides being the most active against E. coli and S. aureus, and C18‐conjugated peptides being the most active against C. albicans. Doubly charged USCLs with aliphatic tails that are 14 carbon atoms and longer showed more potent anticancer activity compared to their triply charged counterparts. C14‐Dab2‐NH2 displayed little toxicity to normal cells, and selectivity to microbial and cancer cells over normal cells. Its structural simplicity, bioactivity, nontoxicity, and selectivity make it a promising therapeutic agent.
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