| Literature DB >> 30931626 |
Asma Bini Araba1, Najeeb Ur Rehman2, Amna Al-Araimi1, Sulaiman Al-Hashmi2, Sulaiman Al-Shidhani2, Rene Csuk3, Hidayat Hussain2,4, Ahmed Al-Harrasi2, Fahad Zadjali1.
Abstract
A series of new 11-keto-β-boswellic acid were partially-synthesized by modifying the hydroxyl and carboxylic acid functional groups of ring A. The structures of the new analogs were confirmed by detailed spectral data analysis. Compounds 4, 5 and 9 exhibited potent anti-cancer results against two human tumor cancer cell lines having IC50 value of MCF-7 (breast) and LNCaP (prostate): 123.6, 9.6 and 88.94 μM and 9.6, 44.12 and 12.03 μM, respectively. Additionally, a maximum nuclear fragmentation was observed for 4 (78.44%) in AKBA treated cells after 24 hr followed by 5 and 9 with (74.25 and 66.9% respectively). This study suggests that the presence of hydrazone functionality (4 and 9) has effectively improved the potency of AKBA. Interestingly, compound 5 with a lost carboxylic acid group of ring A showed comparable potent activity. Highly selective AKBA requires further modification to improve its bioavailability and solubility inside the cancer cells.Entities:
Keywords: 11-keto-β-boswellic acid; 3-acetyl-11-Keto-β-boswellic acid; Boswellia sacra; breast cancer cell lines; normal cell lines; prostate cancer cell lines
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Year: 2019 PMID: 30931626 DOI: 10.1080/14786419.2019.1593165
Source DB: PubMed Journal: Nat Prod Res ISSN: 1478-6419 Impact factor: 2.861