Analysis of the permeable and retainable components of Cayratia japonica ointment through intact or broken skin after topical application by UPLC-Q-TOF-MS/MS combined with in vitro transdermal assay

Cayratia japonica ointment has been used for many years to promote wound healing after perianal abscess surgery. This study aimed to determine the skin-permeable and skin-retainable components of Cayratia japonica ointment after topical application to intact or broken skin via UPLC-Q-TOF-MS/MS analysis and in vitro transdermal assay. Moreover, a combination of semi-quantitative and molecular docking analyses was performed to identify the main active components of the Cayratia japonica ointment and the probable phases of the wound healing process that they act on. Modified vertical Franz diffusion cells and abdominal skin of rats were selected for the in vitro transdermal study. Mass spectrometry data were collected in both positive and negative ion modes. A total of 7 flavonoids (schaftoside, luteolin-7-O-glucuronide, luteolin-7-O-glucoside, apigenin-7-O-glucuronide, luteolin, apigenin, and chrysin) and 1 coumarin (esculetin), were found to permeate and/or retained by intact or broken skin. Among them, the flavonoids were more permeable through intact/broken skin and exhibited stronger binding affinities for targets related to the inflammatory and proliferative phases of wound healing. This study suggests that the flavonoids in Cayratia japonica ointment are most likely the main active components and are crucial at the inflammatory and proliferative phases of wound healing.