Chemical Constituents From Calotropis Gigantea And Their Antitumor Activity In Vitro

Objective:To study the chemical composition in Calotropis gigantea, and the anti-tumor activities of some compounds isolated in vitro. Methods:The powdered whole plants of Calotropis gigantean. Calotropis gigantea were extracted with 95% industrial alcohol.After removal of the solvent,the residue was extracted with petroleum ether,then the aqueous layer was extracted with chloroform to obtain crude alkaloids.Column chromatograghies on silica gel,RP-18,Sephadex LH-20 were applied for the isolation and purification of the compounds.The structures were elucidated by their physicochemical properties and spectral data.Using solid phase micro extraction (SPME) and simultaneous distillation extraction (SDE) to extract the volatile components of horn melon, combining with mass spectrometry technique for analysis. The main compound isolated and 95% ethanol extract assaied by the MTT in vitro evaluation of anti-tumor activity.Results:Sixteen compounds were isolated from Calotropis gigantea by repeated column chromatography on silica gel, ODS and Sephadex LH-20 and their structures were characterized as Frugoside (AFF-1), Uzarigenone(AFF-2),Arjunolicacid(AFF-3),3ξ-(1ξ-Hydroxyethyl)-7-hydroxy-1-isobe nzofuranone (AFF-4), Daucosterol (AFF-5), Syringaresinol (AFF-6), Myristate (AFF-7),12-O-Benzoyldeacylmetaplexignin-3-O-p-D-oleandropyranosyl-(1�'4)-β-D-cymaropyranosyl-(1�'4)-β-D-cymaropyranoside(AFF-8),12-O-Benzoyldeacylme-t aplexigenin (AFF-9), Benzoic acid (AFF-10), AFF-11, ursolic acid (AFF-12), β-sitosterd (AFF-13), Methyl 1-naphthaleneacetate (AFF-14), butylparaben (AFF-15), 4-O-acetyloleandrose (AFF-16). Conclusion:Compounds uzarigenone (AFF-2), Arjunolicacid(AFF-3) were isolated from Calotropis gigantean for the first time, 3ξ-(1ξ-Hydroxyethyl)-7-hydroxy-l-isobenzofuranone(AFF-4),Syringaresinol(AFF-6), myristic(AFF-7),12-O-Benzoyldeacylmetaplexignin-3-O-β-D-oleandropyranosyl-(1 �'4)-β-D-cymaropyranosyl-(1�'4)-β-D-cymaropyranoside(AFF-8),12-O-Benzoyldea cylmetaplexignin(AFF-9),Benzoic acid(AFF-10),3-hydroxy-4-methoxybenzoic acid (AFF-11), Methyl 1-naphthaleneacetate (AFF-14), butylparaben (AFF-15),4-0-acetyloleandrose (AFF-16) were isolated from Calotropis R. Br for the first time; The GC-MS analysis showed that 163 compisitions of the chemical compounds were identified by two extraction methods,81 compounds were obtained of SPME and 82 compounds were obtained of SDE; The results of the antitumor activity screening showed that,Compounds AFF-1,AFF-2 show cytotoxicity against HLE、K562、 RPMI8226、MCF7、MDA、WM9 cells,with K562 and RPM8226 being the most sentitive cell lines.