天然倍半萜内酯小白菊内酯对人血清白蛋白的共价修饰。
Covalent modification of human serum albumin by the natural sesquiterpene lactone parthenolide.
作者信息
Plöger Michael, Sendker Jandirk, Langer Klaus, Schmidt Thomas J
机构信息
Institute of Pharmaceutical Technology and Biopharmacy, University of Münster, PharmaCampus, Corrensstr. 48, D-48149 Münster, Germany.
Institute of Pharmaceutical Biology and Phytochemistry, University of Münster, PharmaCampus, Corrensstr. 48, D-48149 Münster, Germany.
出版信息
Molecules. 2015 Apr 9;20(4):6211-23. doi: 10.3390/molecules20046211.
The reactivity of parthenolide (PRT), a natural sesquiterpene lactone from Tanacetum parthenium (Asteraceae), with human serum albumin (HSA) was studied by UHPLC/+ESI-QqTOF MS analysis after tryptic digestion of albumin samples after incubation with this compound. It was found that the single free cysteine residue, C34, of HSA (0.6 mM) reacted readily with PRT when incubated at approximately 13-fold excess of PRT (8 mM). Time-course studies with PRT and its 11β,13-dihydro derivative at equimolar ratios of the reactants revealed that PRT under the chosen conditions reacts preferably with C34 and does so exclusively via its α-methylene-γ-lactone moiety, while the epoxide structure is not involved in the reaction.
通过对与人参二醇（PRT）孵育后的白蛋白样品进行胰蛋白酶消化，再采用超高效液相色谱/电喷雾串联四极杆飞行时间质谱（UHPLC/+ESI-QqTOF MS）分析，研究了源自小白菊（菊科）的天然倍半萜内酯——小白菊内酯（PRT）与人血清白蛋白（HSA）的反应活性。结果发现，当HSA（0.6 mM）与PRT以大约13倍过量（8 mM）孵育时，HSA的单个游离半胱氨酸残基C34能迅速与PRT发生反应。对反应物等摩尔比的PRT及其11β,13-二氢衍生物进行的时间进程研究表明，在选定条件下，PRT优先与C34反应，且仅通过其α-亚甲基-γ-内酯部分进行反应，而环氧化物结构不参与该反应。
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