Studies On Bioactive Constituents With Myogenesis And Angiogenesis Activity From Geum Japonicum Thunb.Vax.Chinense F.Bolle

Geum Japonicum Thunb.vax. chinense F. Bolle belongs to genus of Geum. Recent studies revealed that its methanol extracts showed strong bioactivity of inducing myogenesis and angiogenesis, and two PCT patents based on the above discovery were applied. Using the method of bioactivity-guided isolation to search bioactive compounds possessing myogenesis and/or angiogenesis activity from Geum Japonicum Thunb.Vax.Chinense F.Bolle. 10 compounds were obtained by using various chromatography methods, and their structures were elucidated on the basis of physicochemical and spectral methods. In this paper, we described the bioactivity-guided isolation, structure determination, and evaluation of myogenesis and angiogenesis effects in vitro and in vivo.The 10 compounds obtained were established as: Gemin A(l) , Casuarinin(2) , Pedunculagin(3), Potentillin(4),Tellimagrandin 11(5), Niga-ichigoside F1(6), Kaji-ichigoside F1(7), Tormentic acid(8), Euscaphic acid(9) and β -Sitosterol(10).The angiogenesis and/or myogenesis effects of tannin Gemin A(1) and triterpenoid saponin Niga-ichigoside F1(6) was researched by in vitro cell proliferation assay, muscle injury and myocardium infarction animal models. Gemin A(l) stimulated the growth proliferation of HCAECs cell, and Niga-ichigoside F1(6) showed potential activity in inducing proliferation of C2Cl2 cells within the range of 1-10μg/mL in vitro. In rat muscle injury experiment, Gemin A(1) mainly induced significant revascularization within 24 hours post muscle injury, but was less effective for myogenesis. Niga-ichigoside F1 (6) can also enhance significant myotube regeneration within 48 hours, but may be only moderate effective for early angiogenesis. In rat myocardium infarction experiment, it was found that the infarct size in the mixture of 1 and 6(1:1) treated hearts was on average approximately 1/3-1/2 times smaller than that in the control as measured by the volume of infarction in the left ventricular free wall associated with many newly formed vessels in the infarcted area on day 2 after ligation. On day 7 many newly formed blood vessels filled with blood cells and newly regenerated myocardium remained in the infarction area including the central areas and the border regions of the infarct in agents treated animals.