Separation and structural elucidation of a novel vardenafil analogue as an adulterant in a natural health care dietary supplement

Chunzheng Li; Xinzheng Wang; Shengming Wu; Junqing Zhao; Junjian Fang; Hui Li; Yingjie Zhu; Kang Zhang; Jing Peng; Jie Mao; Weihua Li; Kun He; Na Wang; Fangting Dong

doi:10.1016/j.heliyon.2023.e15418

Separation and structural elucidation of a novel vardenafil analogue as an adulterant in a natural health care dietary supplement

Heliyon. 2023 Apr 12;9(4):e15418. doi: 10.1016/j.heliyon.2023.e15418. eCollection 2023 Apr.

Authors

Chunzheng Li¹, Xinzheng Wang¹, Shengming Wu¹, Junqing Zhao¹, Junjian Fang¹, Hui Li¹, Yingjie Zhu¹, Kang Zhang¹, Jing Peng¹, Jie Mao¹, Weihua Li¹, Kun He¹, Na Wang¹, Fangting Dong¹

Affiliation

¹ National Center of Biomedical Analysis, Beijing, 100039, China.

Abstract

A novel vardenafil analogue was identified in dietary supplement as an adulterant in herbal formulations. The structure of this analogue was elucidated using HRMS, NMR after extraction from the pulverized powder. It was named morphardenafil as a morpholine ring has replaced the N-ethyl piperazine ring in vardenafil. A tablet of this dietary supplement contained about 50 mg of unspecified morphardenafil, which is 2.5 - 20-times the prescriptive dosage of Levetra, the commercial formulation of the vardenafil monohydrochloride salt in the market and probably places unwary consumers at risk for potentially serious adverse effects or drug-drug interaction (DDI).

Keywords: Adulterants; Dietary supplement; HRMS; Morpholine ring; NMR; PDE-5 inhibitor; Vardenafil analogue.