Metabolomic profiling of the effects of Curcumae rhizoma and Sparganii rhizome on stress-led blood stasis.

Blood stasis (BS) is a complex syndrome with blood flow retardation or cessation. The Traditional Chinese Medicine, Curcumae rhizome (CR) and Sparganii rhizome (SR), showed promising effects on this disease, and especially effective when used in combination. However, the detailed influence of the TCMs on the BSS disturbed metabolic pathways was still unclear. In this study, a BS model was constructed in SD rat and the TCMs were used individually or in combination to assess the effects. As a result, combination of CR and SR led to the improvement in hemorheology parameters of up to 80% in the BS model. Further analyzing using metabolomics showed several metabolic pathways, including center carbon metabolism, amino acid metabolism, etc., recovered to the normal levels after treatment. Informatively, tyrosine and thymidine exhibited potential importance in the BSS and its treatment process. From these results, the metabolic profiles of BS and the SR-CR treatment were provided, which may helpful for better understanding the BSS mechanism and the development of more effective therapies.

Selective estrogen receptor modulator: A novel polysaccharide from Sparganii Rhizoma induces apoptosis in breast cancer cells.

A polysaccharide named SpaTA, as novel selective estrogen receptor modulator, was isolated from water extraction of traditional Chinese herbal medicine Sparganii Rhizoma. SpaTA had a backbone consisting of 2-O-grailsine-ß-xylose (4→6)-α-glucose (1→4) -ß-mannose osamine. There is an aluminium element combined with nitrogen on both grailsine and mannose osamine in repeating unit of SpaTA. The anticancer effect of SpaTA was assessed using ZR-75-1 human breast cancer cells. The results showed that SpaTA induced sequential increases in proliferation and apoptosis through a time- and concentration-dependent manner. Further studies revealed that SpaTA regulated the expression and nuclear translocation of ERα, then modulated the downstream estrogen signaling pathway. Moreover, knock-down ERα in ZR-75-1 cells and overexpress ERα in MDA-MB-231 cells also provided evidences that SpaTA activated the apoptosis-related caspase -3, -8, -9 and PARP in an ERα-dependent manner. Taken together, these results indicated that SpaTA can induce the apoptosis of breast cancer cells through regulating ERα. Therefore, SpaTA may be considered as an effective agent against human breast cancer.

Inhibition of polycystin-L channel by the Chinese herb Sparganum stoloniferum Buch.-Ham.

The Chinese herb Sparganum stoloniferum Buch.-Ham. (SBH) is frequently used to improve blood circulation and to rehabilitate vascular obstruction in traditional Chinese medicine. It was recently reported that SBH reduces the proliferation of renal epithelial cells stimulated by epidermal growth factor (EGF), and inhibits the phosphorylation of the EGF receptor. SBH has also been used as a trial drug to treat polycystic kidney disease (PKD) patients in China. The potential molecular actions of SBH on PKD remain unknown. Autosomal dominant PKD (ADPKD) is associated with mutations in polycystin-1 or polycystin-2 (PC2). PC2 and its homologue, polycystin-L (PCL), are nonselective cation channels permeable to potassium, sodium, and calcium. Here, we examine the effects of SBH on the human PCL channel expressed in Xenopus oocytes, using 2-microelectrode voltage-clamp electrophysiology and radiotracer uptake measurements. In PCL-expressing oocytes, with or without preincubation with SBH, the PCL channel was inhibited by SBH in a dose-dependent and reversible manner; a concentration of 2% SBH completely abolished the channel activation. The IC50 value for SBH was 0.48% +/- 0.03%, with a 10-min preincubation period. SBH was also found to inhibit the PCL-mediated 45Ca tracer uptake in oocytes. Our study suggests that SBH contains 1 or more yet-to-be determined components that are inhibitors of PCL channel. The therapeutic potential of SBH for ADPKD and its chemical composition remain to be investigated.