ABSTRACT
A new compound and twelve known compounds were isolated from the ethyl acetate extract of the roots of Homonoia riparia Lour, which are used in folk medicine for treatment of hepatitis, bellyache and scald, by the method of silica gel column chromatography repeatedly with a gradient of PE-EtOAc, PE-Me2CO, CHCl3-Me2CO, CHCl3-MeOH. Their structures were identified as a new compound 1-oxo-aleuritolic acid (1), and twelve known compounds aleuritolic acid (2), 3-acetoxy-aleuritolic acid (3), taraxerone (4), taraxerol (5), methyl 3-acetoxy-12-oleanen-28-oate (6), 3-acetoxy-12-oleanen-28-ol (7), ursolic acid (8), lupenol (9), 3beta-acetoxy-lupenol (10), cleomiscosin A (11), chrysophanol (12), and gallic acid (13), which were obtained from this plant for the first time, by the spectroscopic techniques of NMR, HMBC, IR and MS, separately. Among the cytotoxicities evaluation of compounds 1 -3 towards AGZY 83-a (human lung cancer cells) and SMMC-7721 (human liver cancer cells) tumor cells was assayed by MTT methods with cis-dichlorodiamminoplatinum (DDP) used as positive control. Compound 2 exerted weak activity against AGZY 83-a with the IC50 value of 33.055 microg x mL(-1), while 1 and 3 showed no activity to these two cell lines.
Subject(s)
Humans , Antineoplastic Agents, Phytogenic , Chemistry , Pharmacology , Cell Line, Tumor , Cell Survival , Coumarins , Dioxanes , Chemistry , Pharmacology , Euphorbiaceae , Chemistry , Inhibitory Concentration 50 , Molecular Structure , Oleanolic Acid , Chemistry , Pharmacology , Palmitic Acids , Chemistry , Pharmacology , Plant Roots , Chemistry , Plants, Medicinal , Chemistry , Triterpenes , Chemistry , PharmacologyABSTRACT
<p><b>AIM</b>The anti-gastric ulcer constituents from the roots of Crepis napifera (Franch) Babc (Compositae) were studied.</p><p><b>METHODS</b>Solvent partition, Si gel and Rp-18 column chromatography, crystallization and spectral methods were used to extract, isolate and identify two compounds. The activity of compound 1 was tested on the rat stomach by determining the effect on aspirin-induced gastric lesions and on histamine-stimulated gastric acid secretion.</p><p><b>RESULTS</b>Two sesquiterpene lactone glycosides, taraxinic acid-1'-O-beta-D-glucopyranoside (1) and 11,13-dihydro-taraxinic acid-1'-O-beta-D-glucopyranoside (2) were obtained. Compound 1 at the dose of 80 mg.kg-1 p.o. inhibited significantly the development of aspirin-induced gastric lesions in the rat and at an i.v. dose of 70 mg.kg-1 did not affect histamine-stimulated gastric acid secretion in the lumen-perfused rat stomach.</p><p><b>CONCLUSION</b>Compound 1 is the active component of the plant which protects gastric mucosa and exhibits anti-gastric ulcer action.</p>