TY - JOUR
T1 - New derivatives of 11-keto-β-boswellic acid (KBA) induce apoptosis in breast and prostate cancers cells
AU - Bini Araba, Asma
AU - Ur Rehman, Najeeb
AU - Al-Araimi, Amna
AU - Al-Hashmi, Sulaiman
AU - Al-Shidhani, Sulaiman
AU - Csuk, Rene
AU - Hussain, Hidayat
AU - Al-Harrasi, Ahmed
AU - Zadjali, Fahad
N1 - Publisher Copyright:
© 2019 Informa UK Limited, trading as Taylor & Francis Group.
PY - 2019
Y1 - 2019
N2 - 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.
AB - 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.
KW - 11-keto-β-boswellic acid
KW - 3-acetyl-11-Keto-β-boswellic acid
KW - Boswellia sacra
KW - breast cancer cell lines
KW - normal cell lines
KW - prostate cancer cell lines
UR - http://www.scopus.com/inward/record.url?scp=85063775309&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=85063775309&partnerID=8YFLogxK
U2 - 10.1080/14786419.2019.1593165
DO - 10.1080/14786419.2019.1593165
M3 - Article
C2 - 30931626
AN - SCOPUS:85063775309
SN - 1478-6419
VL - 35
SP - 707
EP - 716
JO - Natural Product Research
JF - Natural Product Research
IS - 5
ER -
