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Abstract4-Methylsulfinyl-3-butenyl isothiocyanate (MTBITC) found in the radish (Raphanus sativus L.), is a wellknown anticancer agent. In this study, the mechanisms of the MTBITC induction of cell apoptosis in human A549 lung cancer cells were investigated. Our PI staining results showed that MTBITC treatment significantly increased the apoptotic sub-G1 fraction in a dose-dependent manner. The mechanism of apoptosis induced by MTBITC was investigated by testing the change of mitochondrial membrane potential (ΔΨm), the expression of mRNAs of apoptosis-related genes by RT-PCR, and the activities of caspase-3 and -9 by caspase colorimetric assay. MTBITC treatment decreased mitochondrial membrane potential by down-regulating the rate of Bcl-2/ Bax and Bcl-xL/Bax, and activation of caspase-3 and -9. Therefore, mitochondrial pathway and Bcl-2 gene family could be involved in the mechanisms of A549 cell apoptosis induced by MTBITC.

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Benzyl isothiocyanate (BITC) and phenylethyl isothiocyanate (PEITC) are two poorly water-soluble plant components that can form inclusion complexes with β-cyclodextrin (β-CD), namely, β-cyclodextrin−BITC and β-cyclodextrin−PEITC, that are two water-soluble complexes. The inclusion complexes were prepared by two independent processes: physical mixing and coprecipitation. The content of guest molecules in the complexes was measured by UV spectrophotometry. Response surface design (RSD) was applied to optimize the preparation conditions of said complexes. The results showed that the embedding ratios for β-CD−BITC and β-CD−PEITC were 94.9% and 94.1%, respectively. Variance analysis revealed that the mass ratio and the inclusion temperature were two important factors in terms of inclusion action. The optimum conditions for the inclusion of β-CD−BITC were a mass ratio of 0.17 and an inclusion temperature of 57.99 °C, and those for β-CD−PEITC were a mass ratio of 0.0057 and an inclusion temperature of 64.87 °C. The inclusion complexes prepared were qualified by thermal methods [thermogravimetry (TG) and differential scanning calorimetry (DSC)], Fourier transform infrared (FTIR) spectroscopy, and X-ray powder diffraction (XRD). The thermal analysis of β-CD and the two complexes indicated that an interaction between the guest and host molecules did occur. BITC and PEITC could be partially embedded in the hydrophobic cavity of β-CD, so the formation of the said complexes was established. The X-ray and FTIR results support this indication of inclusion behavior.