Tectorigenin 7-O-xylosylglucoside

Comparative pharmacokinetic profiles of tectorigenin in rat plasma by UPLC-MS/MS after oral administration of Iris tectorum Maxim extract and pure tectoridin.[Pubmed:26004225]

J Pharm Biomed Anal. 2015 Oct 10;114:34-41.

Iris tectorum Maxim, a well-known herb medicine, is commonly used for treatment of inflammation, cough, and pharyngitis for a long time in China. Tectoridin, main active ingredient of Iris tectorum Maxim, is often used for its quality control. This study was aimed to analyze the pharmacokinetic profile of tectorigenin (the metabolite of tectoridin) after oral administration of I. tectorum Maxim extract, and to compare the pharmacokinetic characterization of tectorigenin after oral administration of I. tectorum Maxim extract (ITME) and pure tectoridin (PT) in rats. In addition, a simple, reliable and sensitive UPLC-MS/MS method was developed for determination of tectorigenin in rat plasma, using kaempferol as internal standard. The processed samples were separated on a Poroshell 120 SB-C(1)(8) column and detected by positive electrospray ionization in multiple reaction monitoring (MRM) mode. The method validation results indicated that the established method was simple, specific and reliable. The pharmacokinetic results showed that the plasma concentration of tectorigenin in ITME group was much higher than that of the PT group (p<0.01). Moreover, compared to PT group, t(1)/(2) value and AUC(0-infinity) value were also notably increased in ITME group (p<0.01). In conclusion, potential interaction exists between those chemical components in ITME, and the co-existing components in ITME could notably promote the absorption of tectoridin in rats, however, the exact compound(s) which enhance the absorption of tectoridin should be investigated in future study.

Characterization and evaluation of a self-microemulsifying drug delivery system containing tectorigenin, an isoflavone with low aqueous solubility and poor permeability.[Pubmed:28283000]

Drug Deliv. 2017 Nov;24(1):632-640.

The purpose of this study was to characterize and evaluate tectorigenin-loaded self-microemulsifying drug delivery system (TG-SMEDDS), a previously studied preparation, and further confirm the improvement of TG in solubility and bioavailability. The appearance of TG-SMEDDS was clear and transparent, with good mobility. The microemulsion formed by TG-SMEDDS was globular, edge smooth, clear-cut, and distribution homogeneous under transmission electron microscope. The stability studies revealed that TG-SMEDDS remained stable at room temperature for at least 3 months. TG-SMEDDS showed excellent dissolution behavior that more than 90% of TG was released in only 5 min. The in situ intestinal perfusion studies indicated enhancement of absorption in four tested intestinal segments, and the main absorption site of TG was changed to duodenum. In addition, TG-SMEDDS showed significantly higher Cmax and AUC values (11-fold and 5-fold higher values, respectively; P < 0.05) than TG, and the absolute oral bioavailability of TG-SMEDDS was 56.33% (5-fold higher than that of crude TG). What's more, the AUC0-t of crude TG and TG-SMEDDS in bile duct non-ligation rats were 6.05 and 2.80 times, respectively, than that in bile duct ligation rats, indicating the existence of enterohepatic circulation and the secretion of bile could significantly affect the absorption of TG. Further studies showed that even the bile duct was ligation, TG-SMEDDS can still keep a better oral bioavailability (179.67%, compared with crude TG in the bile duct non-ligation rats). Therefore, our study implies that SMEDDS containing TG could be an effective strategy for the oral administration of TG.

Tectorigenin inhibits osteosarcoma cell migration through downregulation of matrix metalloproteinases in vitro.[Pubmed:26991068]

Anticancer Drugs. 2016 Jul;27(6):540-6.

Tectorigenin (Tec) is an effective component of the traditional Chinese medicine Belamcanda chinensis, which has been reported to exert beneficial effects in various types of cancer. However, the activity and mechanism of Tec in osteosarcoma (OS) have not been investigated to date. The aim of the present study was to examine the inhibitory effect of Tec on OS and its underlying mechanism of action. OS cells (Saos2 and U2OS) were treated with various concentrations of Tec for 24, 48, and 72 h. Cell proliferation was evaluated using an CCK-8 assay. Cell migration and invasion ability were measured using the Transwell assay. The expressions of MMP1, MMP2, MMP9, and cleaved caspase3 were measured using real-time PCR and/or western blot analysis. We found that Tec inhibited the proliferation of OS cells (Saos2 and U2OS) in a dose-dependent and time-dependent manner. In addition, Tec significantly inhibited migration and invasion in OS cells (P<0.05). Tec upregulated the expression of cleaved caspase3, while downregulating the expression of MMP1, MMP2, and MMP9. Taken together, the present study provided fundamental evidence for the application of Tec in chemotherapy against OS.