The acrid raphides in tuberous root of Pinellia ternata have lipophilic character and are specifically denatured by ginger extract.

Unprocessed dried tuberous root of Pinellia ternata (Pinellia Tuber) has been used as a component of traditional Japanese Kampo medicine, while this crude drug is usually used after processing with Ginger in traditional Chinese medicine (TCM). It is known that the raphides contained in unprocessed Pinellia Tuber can induce severe acrid irritation of the oral and laryngopharynx mucosa when it is boiled insufficiently. However, the mechanism of the inducing irritation by the raphides nor that of the detoxification by heat or processing with Ginger have been left unclear, mainly because of the difficulties in the extraction and the purification of the raphides and in the assays of acridity. In this study, we developed an easy protocol that can be used to collect raphides from unprocessed Pinellia Tuber and an assay protocol that can be used to evaluate the acridity of the raphides in vitro. The raphides of Pinellia Tuber were discovered to have a lipophilic character and to be collected easily by the extraction using petroleum ether. It was also found that the denaturation of the raphides could be assayed by the dispersity of them in petroleum ether layer of the water/petroleum ether partition, and the acridity of the raphides was found to be in correlation with the assayed denaturation. The raphides were denatured by heat, methanol, or Ginger extract and the denaturing activity of Ginger on raphides was found to be attributable to its lipophilic and thermostable components, which may explain the meaning of the processing of Pinellia Tuber with Ginger in TCM, and may lead to the development of an easier and safer protocol to administer Pinellia Tuber. In addition, it was found that rinsing the mouth with salad oil can effectively relieve irritation of the oral mucosa caused by unprocessed Pinellia Tuber, probably due to the lipophilicity of the raphides.

Comparative genomic hybridization study of genetic changes associated with vindesine resistance in esophageal carcinoma.

The acquisition of drug-resistance is a major problem for cancer patients undergoing chemotherapy. To clarify genetic alterations in cancer cells that develop drug-resistance, comparative genomic hybridization (CGH) was applied to esophageal squamous cell carcinoma cell lines (SH-1V1, SH-1V2, SH-1V4 and SH-1V8) and chemoresistance-related genes in altered chromosomal regions were evaluated. These cell lines were derived from the parental SH-1 cell line, after multiple steps of selection by an increasing exposure to vindesine. SH-1V8 cells were strongly resistant to vindesine. DNA copy number at 16p which includes the MRP (multidrug resistance related protein) gene was markedly increased in all cell lines examined. Increased DNA copy numbers were found at the regions of 5q31-32, 10q11.1-23, and 14q32-qter in SH-1V8 cells that acquired resistance to other drugs as well. Both SH-1V4 and SH-1V8 showed increased DNA copy numbers at 7q11.1-22, 16q12.1-qter, 19p13.2-13.3, 19q11-13.2 and 20q13.1-qter. The chromosomal region of 7q11.1-22 including MDR-1 (multidrug resistance-1) gene was highly amplified in SH-1V4 and SH-1V8. Amplification of the MRP region suggests the prerequisite of developing resistance to vindesine, and further amplification of MDR-1 may play a critical role in acquiring drug-resistance. Several unknown genes related to the induction of chemoresistance might be concealed in other altered chromosomal regions.