Phytoconstituents from < em > Piliostigma foveolatum < /em > (Dalzell) Thoth. leaves induce antiproliferative effect, apoptosis, and cell cycle arrest in Hop-62 cells

Nat Prod Res. 2023 Apr 4:1-5. doi: 10.1080/14786419.2023.2197228. Online ahead of print.ABSTRACTThe study evaluated the therapeutic potential of ethanolic leaf extract of Piliostigma foveolatum (Dalzell) Thoth. (EEBF), its toluene, ethylacetate, methanol soluble fractions (viz. TFBF, EFBF, MFBF), and isolated phytoconstituents against lung cancer. Four compounds were isolated from MFBF by column chromatography and preparative HPLC. Structures were elucidated by IR, 13C-NMR, 1H-NMR, mass spectroscopy and identified as Quercetin, Kaempferol, Isorhamnetin, and ß-glucogallin. EEBF and its biofractions exhibited remarkable antiproliferative activity with GI50<85µg/mL, while isolated Quercetin, Kaempferol, Isorhamnetin, and ß-Glucogallin displayed GI50 values of 56.15 ± 1.16 μM, 68.41 ± 3.98 μM, 55.08 ± 0.57 μM and 58.99 ± 12.39 μM respectively. MFBF demonstrated significant apoptotic activity with 42.24 ± 0.57% cells in early and 4.61 ± 0.88% cells in late apoptosis comparable to standard Doxorubicin. Kaempferol exhibited 23.03 ± 0.37% cells in early and 2.11 ± 0.55% cells in late apoptosis, arresting Hop-62 cells in S-phase. In silico molecular docking, revealed that isolated constituents effectively bound to the same binding site of caspase-3 as Doxorubicin, highlighting their apoptotic mode of action.PMID:37013695 | DOI:10.1080/14786419.2023.2197228
Source: Natural Product Research - Category: Biochemistry Authors: Source Type: research