Department of Pharmaceutical Chemistry, College of Pharmacy, University of Hail, Hail, Saudi Arabia.
Department of Analytical Chemistry, Faculty of Pharmacy, Cairo University, Cairo, Egypt.
Nat Prod Res. 2022 Sep;36(18):4645-4650. doi: 10.1080/14786419.2021.2010074. Epub 2021 Nov 30.
This study was done to evaluate the anticancer potential of (Forssk.) Sch.Bip. leaves methanolic extract in detail for the first time, in addition to investigating its antimicrobial activity. The antimicrobial assay revealed that the extract exerted high activity against (MIC = 156.25 µg/ml) and (MIC = 625 µg/ml), while moderate activity was observed against other microbes. The extract was also screened against HepG2, A549, HCT116 and MCF7 cancer cells and was found to be active across all cells with highest selectivity and cytotoxic activity being observed for A549 cells (IC = 1.21 µg/ml). Further mechanistic studies on A549 cells showed that the extract resulted in S-phase arrest and induced apoptosis activation of caspase-3, p53 and Bax, in addition to downregulation of Bcl-2. HR-LCMS analysis indicated the presence of 3-hydroxycoumarin, quercetin 3,3'-dimethyl ether and skullcapflavone II which might be responsible for the extract's bioactivity.
本研究首次详细评估了 （Forssk.）Sch.Bip.叶甲醇提取物的抗癌潜力，并研究了其抗菌活性。抗菌测定表明，该提取物对 （MIC = 156.25μg/ml）和 （MIC = 625μg/ml）具有高活性，而对其他微生物则表现出中等活性。该提取物还针对 HepG2、A549、HCT116 和 MCF7 癌细胞进行了筛选，结果表明它对所有细胞均具有活性，对 A549 细胞的选择性和细胞毒性最高（IC = 1.21μg/ml）。对 A549 细胞的进一步机制研究表明，该提取物导致 S 期停滞，并诱导细胞凋亡，激活 caspase-3、p53 和 Bax，同时下调 Bcl-2。HR-LCMS 分析表明，提取物中存在 3-羟基香豆素、槲皮素 3,3'-二甲醚和黄芩素 II，它们可能是提取物生物活性的原因。
