OBJECTIVE: Previous work has found that the Traditional Chinese Medicine (TCM) form aggregates in the aqueous solution, and the activities of two Chinese herbal formulae against three cardiovascular targets were aggregates-related. This paper further studied the molecular morphology composed of aggregation and single active molecule in TCM. METHODS: We take Pueraria lobata (Willd.) Ohwi (PUE) as an example. By means of dynamic light scattering (DLS), transmission electron microscopy (TEM), and high performance liquid chromatography-mass spectrometry (HPLC-MS), the mechanism and active components of the aggregates in PUE have been studies. Besides the relationship between aggregation and therapeutic activities in the vivo level has been studied by hemorheological method. RESULTS: Puerarin, daidzein, daidzin, genistein, these cardiovascular bioactive compounds existed in the aggregates. Three kinds of aggregation processes by the bioactive molecules in the solution were elucidated: (1) the aggregation of single molecule oneself; (2) the aggregation between different single molecules; (3) the aggregation between different single molecules and the primary metabolites. Furthermore, the therapeutic activity of PUE solution was aggregates-related in vivo level. CONCLUSIONS: The aggregation morphology of molecules in TCM might be a promising way to study the mechanism of TCM, even to develop an approach of new nanomedicine of TCM.
OBJECTIVE: Previous work has found that the Traditional Chinese Medicine (TCM) form aggregates in the aqueous solution, and the activities of two Chinese herbal formulae against three cardiovascular targets were aggregates-related. This paper further studied the molecular morphology composed of aggregation and single active molecule in TCM. METHODS: We take Pueraria lobata (Willd.) Ohwi (PUE) as an example. By means of dynamic light scattering (DLS), transmission electron microscopy (TEM), and high performance liquid chromatography-mass spectrometry (HPLC-MS), the mechanism and active components of the aggregates in PUE have been studies. Besides the relationship between aggregation and therapeutic activities in the vivo level has been studied by hemorheological method. RESULTS:Puerarin, daidzein, daidzin, genistein, these cardiovascular bioactive compounds existed in the aggregates. Three kinds of aggregation processes by the bioactive molecules in the solution were elucidated: (1) the aggregation of single molecule oneself; (2) the aggregation between different single molecules; (3) the aggregation between different single molecules and the primary metabolites. Furthermore, the therapeutic activity of PUE solution was aggregates-related in vivo level. CONCLUSIONS: The aggregation morphology of molecules in TCM might be a promising way to study the mechanism of TCM, even to develop an approach of new nanomedicine of TCM.