Pharmacodynamic evaluation of phenanthridine derivatives in
c57bl/6 mice
According to the aforementioned in vitro assays, HCJA121 and HCJA404
effectively stimulated melanin production through a new mode of action
that involved targeting of the axin protein. Subsequently, in vivo
pharmacodynamic assays were conducted to evaluate the therapeutic
effects of HCJA121 and HCJA404 on vitiligo. We used a total of 108
C57BL/6 mice (half male and half female), weighing between 18 and 22 g.
We coated 99 mice with 5% HQ for 50 consecutive days to establish a
mouse model of vitiligo. The mice were randomly divided into 8 groups: a
negative control group, a positive control group (8-MOP), and six groups
that were treated with low (0.0425 mg/kg), medium (0.425 mg/kg), or high
(4. 25 mg/kg) doses of the compounds. The remaining eight mice were not
treated with 5% HQ, and they served as a blank control group.
Phenanthridine was administered once daily for 30 days. During the
modelling process, the skin of each group of mice was pale, and hair
growth was slow. With prolonged modelling, white spots appeared, and the
new hair turned white. As shown in Fig. 4a and Table S1, the skin and
colour of the newly generated hair in the test area of the vitiligo mice
exhibited varying degrees of restoration to black in the groups treated
with 8-MOP and the phenanthridine derivatives. Particularly, the skin
and hair of vitiligo mice recovered very well after the administration
of HCJA121 and HCJA404, even at a low dose, indicating that the clinical
symptoms of vitiligo mice were significantly improved, implying that 1
and 2 produce strong curative effects for vitiligo.