Boron neutron capture therapy(BNCT)has emerged as a promising treatment for cancers,offering a unique approach to selectively target tumor cells while sparing healthy tissues.Despite its clinical utility,the widesprea...Boron neutron capture therapy(BNCT)has emerged as a promising treatment for cancers,offering a unique approach to selectively target tumor cells while sparing healthy tissues.Despite its clinical utility,the widespread use of fructose-BPA(F-BPA)has been hampered by its limited ability to penetrate the blood-brain barrier(BBB)and potential risks for patients with certain complications such as diabetes,hyperuricemia,and gout,particularly with substantial dosages.Herein,a series of novel BPA derivatives were synthesized.After the primary screening,geniposide-BPA(G-BPA)and salidroside-BPA(S-BPA)exhibited high water solubility,low cytotoxicity and safe profiles for intravenous injection.Furthermore,both G-BPA and S-BPA had demonstrated superior efficacy in vitro against the 4T1 cell line compared with F-BPA.Notably,S-BPA displayed optimal BBB penetration capability,as evidenced by in vitro BBB models and glioblastoma models in vivo,surpassing all other BPA derivative candidates.Meanwhile,GBPA also exhibited enhanced performance relative to the clinical drug F-BPA.In brief,G-BPA and S-BPA,as novel BPA derivatives,demonstrated notable safety profiles and remarkable boron delivery capabilities,thereby offering promising therapeutic options for BNCT in the clinic.展开更多
本研究基于固相萃取-液相色谱-串联质谱(SPE-LC-MS/MS)技术,建立了一种高灵敏度分析方法,用于测定以鹌鹑为代表的禽类产品中痕量双酚A(BPA)和双酚F(BPF)的残留量。通过优化试验条件,采用Oasis PRiME HLB固相萃取柱净化,筛选色谱分离条件...本研究基于固相萃取-液相色谱-串联质谱(SPE-LC-MS/MS)技术,建立了一种高灵敏度分析方法,用于测定以鹌鹑为代表的禽类产品中痕量双酚A(BPA)和双酚F(BPF)的残留量。通过优化试验条件,采用Oasis PRiME HLB固相萃取柱净化,筛选色谱分离条件,结果表明:该分析方法在0.1~50 ng/g浓度范围内线性关系良好(R^(2)>0.999),检出限LOD(≤0.01 ng/g)和定量限LOQ(≤0.03 ng/g)均满足痕量分析要求,加标回收率(82.1%~96.8%)和精密度(RSD<8.0%)符合残留分析标准。该方法操作简便、灵敏度高、抗基质干扰性能优异,适用于禽产品中痕量BPA和BPF的确证检测,可为动物源性食品安全风险评估提供可靠技术支撑。展开更多
基金supported by Guangdong Basic and Applied Basic Research Foundation(No.2021B1515120065)National Natural Science Foundation of China(Nos.82202339,32271420,82202307)+3 种基金China Postdoctoral Science Foundation(Nos.2022M711527,2021M701640)Science Fund for Creative Research Groups of Nature Science Foundation of Hebei Province(No.B2021201038)National High-End Foreign Expert Recruitment Plan(No.G2022003007L)Natural Science Foundation of Hebei Province(No.B2023201108).
文摘Boron neutron capture therapy(BNCT)has emerged as a promising treatment for cancers,offering a unique approach to selectively target tumor cells while sparing healthy tissues.Despite its clinical utility,the widespread use of fructose-BPA(F-BPA)has been hampered by its limited ability to penetrate the blood-brain barrier(BBB)and potential risks for patients with certain complications such as diabetes,hyperuricemia,and gout,particularly with substantial dosages.Herein,a series of novel BPA derivatives were synthesized.After the primary screening,geniposide-BPA(G-BPA)and salidroside-BPA(S-BPA)exhibited high water solubility,low cytotoxicity and safe profiles for intravenous injection.Furthermore,both G-BPA and S-BPA had demonstrated superior efficacy in vitro against the 4T1 cell line compared with F-BPA.Notably,S-BPA displayed optimal BBB penetration capability,as evidenced by in vitro BBB models and glioblastoma models in vivo,surpassing all other BPA derivative candidates.Meanwhile,GBPA also exhibited enhanced performance relative to the clinical drug F-BPA.In brief,G-BPA and S-BPA,as novel BPA derivatives,demonstrated notable safety profiles and remarkable boron delivery capabilities,thereby offering promising therapeutic options for BNCT in the clinic.
