Oxyresveratrol (OXY) is a small molecule phytochemical which has been reported to have important biological function. The aim of this study was to elucidate the gene expression and biological pathways altered in MCF-7, breast cancer cells following exposure to OXY. The cytotoxicity to different cancer cell lines was screened using MTT assay and then whole gene expression was elucidated using microarray. The pathways selected were also validated by quantitative PCR analysis, fluorometric and western blot assay. A total of 686 genes were found to have altered mRNA expression levels of two-fold or more in the 50 μM OXY-treated group, while 2,338 genes were differentially expressed in the 100 µM-treated group. The relevant visualized global expression patterns of genes and pathways were generated. Apoptosis was activated through mitochondria-lost membrane potential, caspase-3 expression and chromatin condensation without DNA damage. G0/G1 and S phases of the cell cycle control were inhibited dose-dependently by the compound. Rad51 gene (DNA repair pathway) was significantly down-regulated (p < 0.0001). These results indicate that OXY moderates key genes and pathways in MCF-7 cells and that it could be developed as a chemotherapy or chemo-sensitizing agent.
Artocarpus lakoocha Wall. ex Roxb. (family: Moraceae) has been used as a traditional Thai medicine for the treatment of various parasitic diseases. This species has been reported to be the source of phytochemicals, which show potent biological activities. The objective of this study was to investigate the phytochemical profile of the extracts of the heartwood of A. lakoocha and their pro-oxidant activity in vitro. The heartwood was ground, extracted, and then chromatographic and spectroscopic analyses were carried out; oxyresveratrol was identified as the major component in the extracts. The pro-oxidant activity was investigated using DNA-nick, reactive oxygen species and reducing assays. The results showed that oxyresveratrol induced DNA damage dose-dependently in the presence of copper (II) ions. It was also found to generate reactive oxygen species (ROS) in a dose-dependent manner and reduce copper (II) to copper (I). It is concluded that oxyresveratrol is the most abundant stilbenoid in A. lakoocha heartwood. The compound exhibited pro-oxidant activity in the presence of copper (II) ions, which may be associated with its ability to act as an anticancer compound.
1 January 2008 in American Journal of Agricultural and Biological Sciences
Scales of shed king cobra (Ophiophagus hannah) skin from the dorsal portions, (SSS) and human breast epidermis (HE) were used as barrier membranes for comparison in an in vitro drug permeation study of nine active compounds (MW range 150-300 g mol-1, pKa 3-10). Each compound, saturated in a donor solution at pH 4.0 or 5.6, permeated through the barrier membrane, fully hydrated. A receptor solution at pH 7.4 was sampled for quantification at its λmax by UV-Visible spectrophotometry and/or HPLC. The permeability coefficients of nine compounds were correlated to the n-octanol/water partition coefficients of these compounds. The permeability coefficient of these compounds using HE and SSS was correlated. Scales of shed skin from the dorsal portions of king cobras were shown to be well correlated to the human breast epidermis in this in vitro aqueous permeation study of these compounds.
1 March 2007 in American Journal of Agricultural and Biological Sciences
Cancer remains a global health challenge due to the limitations of conventional therapies, including severe side effects and drug resistance. While Cordyceps militaris (L.) Fr. is well-regarded in traditional medicine for its antitumor effects, research has primarily focused on small molecules like cordycepin. The anticancer potential of its total protein-rich isolate remains less characterized. This study aimed to extract, characterize, and evaluate the in vitro cytotoxic activities of the protein-rich isolate from C. militaris fruiting bodies against various human cancer cell lines. Proteins were extracted from dried fruiting bodies using an alkaline extraction method (pH 12.0) followed by isoelectric precipitation (pH 7.0) and lyophilization. The isolate was analyzed for yield, protein content, water activity, and moisture. Bioactive markers (cordycepin and adenosine) were quantified using UHPLC. Cytotoxicity was assessed via MTT assay against MCF-7 (breast), HT-29 and Caco-2 (colorectal), and HepG2 (liver) cancer cells, with HDFn (normal fibroblasts) used to determine selectivity. Results showed that the extraction process achieved a high yield of 72.61% with a protein content of 41.90 ± 0.19%. The isolate demonstrated excellent stability with a low water activity (aw) of 0.22 ± 0.01. Notably, cordycepin was significantly enriched in the isolate, increasing tenfold to 1048 mg/100 g compared to the raw powder. The protein-rich isolate showed dose-dependent cytotoxicity, with the highest potency against MCF-7 cells (IC50 = 8.68 µg/mL). Crucially, the isolate exhibited promising selectivity in this model, being nearly 55 times less toxic to normal HDFn cells (IC50 = 475.56 µg/mL). It is concluded that C. militaris protein-rich isolate is a stable, bioactive-rich fraction with potent and selective anticancer activity. The significant enrichment of cordycepin and the wide therapeutic window suggest its potential as a safe candidate for functional foods or adjuvant cancer therapies.