Super-molecular Extract Of Andrographis Paniculata And Andrographolide Derivatives Synthesis And Activity Of Research

Andrographis panniculata(Burm. f. )Nees was found in India and planted in east, middlesouth and southwest China. It is used extensively as an antipyretic, anti-inflammtory and antivirus medicine for a long time.Re-cently, it's newly pharmacological activities were found, such as immune activity, antitumor effect, hepatoprotective activity, inhibitory effect on platelet aggregation, antihypotensive effect, antifertility activity and antih-yperglycemic effect. It's main component is diterpene lactams which is represented by andrographolide.In this article, the active ingredients of Andrographis panniculata Nees EtOH extract was increased greatly by supramolecule technology in the first time.This method is better than supereritical CO₂ fluid and macroporous adsorptive resins for it's higher content of active ingredients and feasible operation. At the same time, 16 andrographolide derivatives were synthesized from andrographolide, 10 of them have been already reported, 6 of them are new. The new compounds are andrographolidic acid(53), trifloroacetyl andrographolide(55), andrographolide trimaleic acid monoes-ter(56),isoandrographolide disuccinic acid monoester(62), isoandrographolide dioxalochlolide monoester(63)and isoandrographolide dioxalic acid monoester(64), the others are triacetyl andrographolide(54),dehydroandrog-rapholide(4), diacetyl dehydroandrographolide(57), dehydroandrographoli-de disuccinic acid monoester(24),dehydroandrographolide-3,19-cyclophos-phate(58), adduct of andrographolide and NaHSO3(36),14-deoxyandrogra-pholide(2),diacetyl-14-deoxyandrographolide(59),isoandrographolide(60) and diacetyl isoandrographolide (61).We also studied the antipyretic effect, the anti-inflammtory effect,the immune activity, antitumor activity of them and the SAR of the andrographolide derivatives.