Synthesis and cytotoxicity of the boron carrier pentagamaboronon-0-ol for boron neutron capture therapy against breast cancer
Penulis/Author
Dr. Sci. apt. Rohmad Yudi Utomo, M.Sc. (1); FEBRI WULANDARI (2); DHANIA NOVITASARI (3); Prof. Dr. apt. Ratna Asmah Susidarti, MS. (4); Mitsunori Kirihata (5); Prof. Dr.rer.nat. apt. Adam Hermawan, S.Farm., M.Sc. (6); Prof. Dr. apt. Edy Meiyanto, M.Si. (7)
Tanggal/Date
21 2022
Kata Kunci/Keyword
Abstrak/Abstract
Boronic acid‑containing curcumin analog, pentagamaboronon‑0 (PGB‑0), acts
as a potential boron‑carrier agent but has limited water solubility. Thus, a new
compound (PGB‑0‑ol) with better chemical and pharmacological properties than PGB‑0
has been synthesized. Molecular docking was performed using a molecular operating
environment. Prediction of PGB‑0‑ol absorption, distribution, metabolism, and excretion
(ADME) was performed using pkCSM software. PGB‑0‑ol was synthesized by adding
NaBH4
to PGB‑0 and stirring for 1 h. The crude PGB‑0‑ol was purified using preparative
layer chromatography. Cell viability was evaluated using the trypan blue exclusion assay.
In comparison to PGB‑0 based on molecular docking study, PGB‑0‑ol could interact in
with several cancer biomarkers, such as human epidermal growth factor2 epidermal
growth factor receptor, IκB kinase, folate receptor‑α, and integrin αv
β3
. PGB‑0‑ol also
showed an improved ADME profile because of its higher water solubility than PGB‑0.
PGB‑0‑ol was synthesized by selective ketone reduction of PGB‑0 into primary alcohol by
sodium borohydrate producing 30% yield. The cytotoxicity of PGB‑0‑ol against several
breast cancer cells was lower than that of PGB‑0. The novel compound PGB‑0‑ol was
synthesized using simple steps. PGB‑0‑ol has low cytotoxicity against breast cancer
cells and could be applied in boron neutron capture therapy as a boron carrier.
