保健食品中違法摻加Sildenafil類緣物之分離與鑑定   全文下載

Isolation and Identification of a Novel Sildenafil Analogue Adulterated in Dietary Supplements

本報告係報導一宣稱具有壯陽效果之保健食品，以薄層層析及紫外光分光光度法檢驗，檢出摻加一種首次發現之新成分，該成分之紫外光圖譜類似於acetildenafil（sildenafil 類緣物）。為鑑定該成分，進行分離、純化及經測試核磁共振光譜、質譜及紅外線光譜，所得數據加以分析，確認其化學結構，此新化合物1 其結構為acetyl 基取代sildenafil 之 sulfonyl-Nmethylpiperazine基團。其化學名稱為5-[2-ethoxy-5-acetyl-phenyl]-1-methyl-3-n-propyl-7H-pyrazolo[4,3-d]pyrimidin-7-one（分子式為C19H22N4O3, 分子量354）。雖然此成分尚無相關文獻報導其藥理作用與安全評估，但由本研究結果推測該成分係違法摻加於保健食品中，為維護國民健康，本局已將該成分列入日常檢驗分析項目中。"

A suspected sildenafil analogue (1) was firstly detected from dietary supplements, which claimed for energy enforcement, by TLC and UV method. The UV spectrum of this suspected compound showed close similar pattern to that of acetildenafil (2, sildenafil analogue). In order to identify this compound, separation and purification were carried out as well as structure determination was conducted by various NMR techniques, mass spectrum and IR. This new compound 1 had an acetyl group instead of sulfonyl- N-methylpiperazine moiety in sildenafil (3), and its structure was determined as 5-[2-ethoxy-5-acetyl-phenyl]-1-methyl-3-n-propyl- 1,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one (molecular formula C19H22N4O3, molecular weight 354). So far no related report and literature to describe its pharmacological action and to provide related safety evaluation of this compound was published. The above results revealed that this compound was illegally adulterated into the dietary supplements, and has thus been included in our routine analysis list for public health.