abstract |
The present invention relates to an andrographolide derivative of the formula (I), wherein R 1 , R 2 and R 3 are same or different substituents selected from hydrogen, substituted or unsubstituted organic acid radicals, inorganic acid radicals, alkyl, aryl or heteroaryl, and at least one of R 1 , R 2 and R 3 is R-lipoic acid, S-lipoic acid or a mixture thereof, or corresponding dihydrolipoic acids thereof, or N-acetylcysteine radical. The derivative has good antitumor effect, can induce apoptosis of tumor cells, can directly kill Gram-positive bacteria ( staphylococcus aureus ) and drug resistance bacteria (MRSA5676 and MRSA5677), can inhibit the QS-system of Gram-negative bacteria ( Pseudomonas aeruginosa ), can inhibit and destroy the formation of biofilm of Pseudomonas aeruginosa; and exhibits significant hypoglycemic effect, so that it can be used in manufacture of medicaments for treatment of cancers, inflammation, diabetes, and bacterial and viral infections. |