The antipyretic, analgesic, and anti-inflammatory activities of dehydroandrographolide succinate (DAS), an andrographolide derivative, are superior to its parent compound. However, its instability and poor water solubility have restricted its clinical use. To solve these problems, a series of DAS conjugates with functional amino acids or peptides coupled to methoxypolyethylene glycol (mPEG) were designed and synthesized. Conjugation of DAS directly to mPEG improved the compound solubility in aqueous solution, but the thermostability of the conjugate was reduced compared with the parent compound. Introduction of methionine (Met) or oligomethionyl peptides, DAS-Metn-mPEG (n = 1, 2, or 3), protected the DAS skeleton from ring opening and double bond oxidation, thus improving the anti-inflammatory properties of these derivatives compared with DAS.
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