Tretinoin (Aberela) (Synonyms: Trans Retinoic Acid)

Tretinoin (Aberela) is a vitamin A-derived, non-peptidic, small lipophilic molecule that acts as ligand for nuclear RA receptors (RARs), converting them from transcriptional repressors to activators^[5].

In cultured human mesangial cells, Tretinoin (Aberela) increased the reduced glutathione content and the catalase activity in a dose- and time-dependent way, which then prevented the cytotoxicity of H2O2 ^[1].A549 cells were incubated with free Tretinoin (Aberela) (TTN), blank nanocapsules (LNC) and Tretinoin (Aberela) -loaded lipid-core nanocapsules (TTN-LNC). TTN-LNC induced apoptosis and cell cycle arrest at the G1-phase while TTN did not. TTN-LNC showed higher cytotoxic effects than TTN on A549 cells evaluated^[4].The combination of As-ODN-hTR and All-trans Tretinoin (Aberela) has a synergistic anti-tumor effect. This anti-tumor effect can be mainly attributed to apoptosis induced by a decrease in telomerase activity. Bcl-2 plays an important role in this process ^[7].

In male nmri mice, Tretinoin (Aberela) significantly inhibited cellular immunity and increased humoral immunity. Tretinoin (Aberela) decreased lymphocyte proliferation, decreased NBT, and interleukin-17 secretion, but increased interleukin-10 secretion ^[2]. In patients with facial acne, clindamycin phosphate Tretinoin (Aberela) Gel (CTG) (1.2% clindamycin phosphate, 0.025% Tretinoin (Aberela) in a gel base (Velac)) was significantly more effective than 0.025% Tretinoin (Aberela), which relayed on the anti-inflammatory efficacy of Tretinoin (Aberela) ^[3].The delivery of Tretinoin (Aberela) by polymeric micelles prolonged the blood circulation and enhanced the accumulation of Tretinoin (Aberela) in the tumor tissue compared with the administration of free Tretinoin (Aberela). Tumor growth was significantly delayed and the survival time of mice was prolonged following the treatment by Tretinoin (Aberela) polymeric micelles demonstrating the improved anticancer activity of Tretinoin (Aberela) ^[6].

References:
[1]: Manzano VM, Puyol MR, et,al. Tretinoin prevents age-related renal changes and stimulates antioxidant defenses in cultured renal mesangial cells. J Pharmacol Exp Ther. 1999 Apr;289(1):123-32. PMID: 10086995.
[2]: Froushani SM, Galeh HE. New insight into the immunomodulatory mechanisms of Tretinoin in NMRI mice. Iran J Basic Med Sci. 2014 Sep;17(9):632-7. PMID: 25691937; PMCID: PMC4322144.
[3]: Richter JR, FÖrstrÖm LR, et,al. Efficacy of the fixed 1.2% clindamycin phosphate, 0.025% tretinoin gel formulation (Velac) and a proprietary 0.025% tretinoin gel formulation (Aberela) in the topical control of facial acne. J Eur Acad Dermatol Venereol. 1998 Nov;11(3):227-33. PMID: 9883434.
[4]: Schultze E, Ourique A, et,al. Encapsulation in lipid-core nanocapsules overcomes lung cancer cell resistance to tretinoin. Eur J Pharm Biopharm. 2014 May;87(1):55-63. doi: 10.1016/j.ejpb.2014.02.003. Epub 2014 Feb 11. PMID: 24525073.
[5]: Rhinn M, DollÉ P. Retinoic acid signalling during development. Development. 2012 Mar;139(5):843-58. doi: 10.1242/dev.065938. PMID: 22318625.
[6]: Chansri N, Kawakami S, et,al. Anti-tumor effect of all-trans retinoic acid loaded polymeric micelles in solid tumor bearing mice. Pharm Res. 2008 Feb;25(2):428-34. doi: 10.1007/s11095-007-9398-x. Epub 2007 Jul 31. PMID: 17665288.
[7]: Xu Q, Zhang Z, et,al. Antisense oligonucleotides and all-trans retinoic acid have a synergistic anti-tumor effect on oral squamous cell carcinoma. BMC Cancer. 2008 Jun 3;8:159. doi: 10.1186/1471-2407-8-159. PMID: 18522733; PMCID: PMC2427037.