Cactus Active Ingredients

Opuntia dillenii (KER-GAW.) HAW. is a cactus that grows mainly in the south of China and is called Xian Ren Zhang (仙人掌) in Chinese. The stem of this plant is used as a folk medicine for the treatment of diabetes, gastric ulcer, inflammatory and several other diseases, while its reddish fruit is commonly used as coloring agents for foods, drinks and drugs.In the course of our chemical studies on the bioactive constituents of O. dillenii, the 80% ethanolic extract of its stems was found to show potent anti-inflammatory and anti-diabetes effects. The 1-butanol soluble phase of the extract exhibited potenter anti-inflammatory activity than other phase. Scavenging effect on 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical and superoxide anion radical ( O2-) generated by the xanthing-xanthine oxidase system was also found in the 80% ethanolic extract.As for the chemical constituents of this plant, systemic studies lead to the isolation offorty-nine compounds from the extract, and forty-seven of them were identified by spectroscopic analysis. Nine new compounds were characterized, and they were: opuntioside I (11), 4-ethoxyl-6-hydroxymethyl-α-pyrone (14), (ethyl succinate)-(dimethyl malate)-ester (22), l-butoxyl-(L)-malate (24), ethyl α-L-rhamnopyranoside (26), opuntioside II (34), kaempferol 7-O-β-D-glucopyranosyl (1→4)-β-D-glucopyranoside (46), methyl α-D-glucopyranoside-6-(methyl 4-malate)-ester (47), and opuntioside III (48). Opuntioside I, II, III and 4-ethoxyl-6-hydroxymethyl-α-pyrone belong to the skelecton of α-pyrone. Twenty-eight known constituents were isolated from the genus of Opuntia for the first time, their names were listed as below: daucosterol (4), kaempferide (5), p-hydroxybenzoic acid (6), 3-O-methyl isorhamnetin (12), (E)-ferulic acid (13), 1-heptanecanol (15), vanillic acid (16), isorhamnetin-3-O-β-D-rutinoside (17), ethyl 3, 4-dihydroxybenzoate (19), 4-hydroxyaceophenone (20), l-(3-ethylphenyl)-l, 2-ethanediol (23), 5-(hydroxymethyl)-2- furaldehyde (25), (5)-3-hydroxy-3-methylglutarate (27), tetrahydro-5-oxo-2-furancaboxylic acid ethyl ester (28), guaiacylglycerol-β-ferulic acid ether (29), methyl p-hydroxy-(E)-cinnamate (30), methyl 4-hydroxybenzoate (31), ethyl α-D-arabinofuranoside (35), piceine (36), androsin (37), 3,4-dihydroxy benzoic acid (39), 3',5'-dimethoxy-4'-O-β-D-glucopyranosyl-cinnaniic acid (40), 9(5), 12(5), 13(S)-trihydroxyoctadeca 10(E), 15(Z)-dienoic acid (41), 9(5), 12(5), 13(5)-trihydroxy-10(E)-octadecenoic acid (42), 3-O-methyl quercetin 7-O-β-D-glucopyranoside (43), kaempferol7-O-β-D-glucopyranoside (44), manghaslin (45), and ethyl β-D-fructopyranoside (49). Eight compounds separated for the first time from the title plant were: aromadenerin (2), opuntiol (3), kaempferol (7), 3-O-methyl quercetin (8), quercetin (10), rutin (18), isorhamnetin (21), and benzoic acid (38).The compounds of α-pyrone type and flavonol type with large amount were subjected to bioactive studies. The scavenging effects on DPPH and "O2", inhibitory effects on nitric oxide generation, on aldose reductase, and on α-glucosidase were carried out. Flavonol type ingredients showed good activities on the aspects described above, expect for on a-glucosidase, while α-pyrone type compounds didn't show any activity. Flavonol type components maybe play an important role in 0. dillenii's pharmacological effects.On the base of chemical and pharmacological works, a study on. quality standardization of Yi-Jin-Jiang-Tang oral liquid consisted of O. dillenii was conducted. The methods for TLC identifications with 3-O-methyl quercetin and opuntiol as authentic samples, and quantitative determination were established. Base on the result of content tests, the contents of opuntiol in an ampoule of Yi-Jin-Jiang-Tang Oral Liquid (20 ml) should not lower than 20 mg.