Studies On Active Constituents Of Smooth Muscle Relaxation And Antibioses From Lappula Echinata Gilib

Objective: To investigate the active constituents of anti-diarrhea from Lappula echinata and research its possible pharmacological activity. Methods: Extracts and parts from Lappula echinata were screened by the degree of inhibiting the motility of smooth muscle firstly. These active extracts and parts were further isolated by silica gel column chromatography, gel column chromatography, silica gel flash column chromatography, PTLC and HPLC. Chemical structures of the compounds were identified by ¹H-NMR, ¹³C-NMR, 2D-NMR, EI-MS, HR-MS, IR and UV. Finally activity of smooth muscle relaxation of these compounds was determined, and antibacterial activity was determined by KB method.Results: LEGO 118, LEG0119 from EtOAC extracts and n-BuOH extracts were found to have obvious activity of inhibiting the contraction of isolated ileum of rabbit. Among six compounds isolated from the above three active parts and extracts, LEG 1402 was identified as a new quinolone alkloid named 8-methoxy-4-quinolone-2-caboxylic acid; LEG4801 is Rosmarinic acid; LEG3902 is a glucoside whose aglycon is the same as LEG1402; chemical structures of other compounds is under analysis. LEG4801 and LEG3902 showed evident activity of inhibiting the motility of smooth muscle, and P < 0.01 comparing with blank control. LEG1402 was not observed to have this activity. According to the results of antibacterial experiment in vitro, LEG1402 was found to have antibacterial activity on pseudomonas pyocyanea ATCC27853, EPEC O111, pneumobacillus and staphylococcus epidermidis. Conclusion: Active constituents with activity of smooth muscle relaxation were...