中国中药杂志2026，Vol.51Issue(3)：662-674,13.DOI:10.19540/j.cnki.cjcmm.20251111.302
基于酶抑制、转运体和纳米粒探究醋乳香多糖促进乳香酸类成分体内吸收的作用机制
Polysaccharides of frankincense processed with vinegar promote absorption of boswellic acids via enzyme inhibition,transporters,and nanoparticles
摘要
Abstract
This study aimed to investigate the promoting effects of polysaccharides from frankincense and vinegar-processed frankincense on the absorption of 3-O-acetyl-11-keto-β-boswellic acid(AKBA)and 11-keto-β-boswellic acid(KBA),and to explore their potential mechanisms through inhibition of carboxylesterase 2(CES2)and organic anion-transporting polypeptides(OATPs),as well as the formation of nanoparticles(NPs).The effects of polysaccharides from frankincense and vinegar-processed frankincense on the pharmacokinetic parameters of AKBA and KBA were analyzed by LC-MS/MS.The inhibitory effects of polysaccharides on CES2 were studied through in vitro human liver microsome metabolic experiments.The uptake of AKBA and KBA was analyzed via cells transfected with OATP1B1,OATP1B2,and the inhibitory effects of polysaccharides on expression of OATP1B1,OATP2B1 at the mRNA level were compared.Self-assembled polysaccharide-AKBA,KBA NPs were prepared and their physicochemical properties and in vitro release behaviors were characterized.The results showed that the polysaccharides,especially those from vinegar-processed frankincense,significantly enhanced the oral bioavailability of AKBA and KBA.Polysaccharides non-competitively inhibited CES2,thereby blocking the metabolism of AKBA.Moreover,they down-regulated the mRNA levels of OATP1B1,OATP2B1,reducing the cellular uptake of AKBA and KBA.Additionally,the 4 polysaccharides protected active ingredients from metabolism by forming NPs with AKBA and KBA.Overall,this study proved that vinegar-processed frankincense polysaccharides had the strongest promoting effects on the absorption of AKBA and KBA,and illustrated the roles of polysaccharides in the inhibition of CES2 and OATPs and formation of NPs for the first time.The findings offer a valuable clue for illustrating the principle underpinning the effect enhancement through vinegar processing from the view of polysaccharides.关键词
醋乳香/乙酰基-11-酮基-β-乳香酸/11-酮基-β-乳香酸/羧酸酯酶2/有机阴离子转运多肽/纳米粒Key words
frankincense processed with vinegar/3-O-acetyl-11-keto-β-boswellic acid/11-keto-β-boswellic acid/carboxylesterase 2/organic anion-transporting polypeptides/nanoparticles引用本文复制引用
郭静妍,孙永芳,王参政,华会明,王冬梅,潘英妮,任昆,任舒蒙,刘晓秋..基于酶抑制、转运体和纳米粒探究醋乳香多糖促进乳香酸类成分体内吸收的作用机制[J].中国中药杂志,2026,51(3):662-674,13.基金项目
国家自然科学基金项目(81973465) （81973465）
辽宁省教育厅高等学校基本科研项目青年项目(JYTQN2023329) （JYTQN2023329）
