Comparison of Anticancer, Antioxidant, Enzyme Inhibitory Effects and Phytochemical Contents between Edible Lettuce (Lactuca sativa) and A New Wild Species (Lactuca anatolica).

In this study, the bioactive components, enzyme inhibitory, antioxidant and anticancer potentials of edible (L. sativa) and a new species (L. anatolica) of Lactuca were evaluated and compared. The quantitative analyzes of the bioactive components of L. sativa (LS) and L. anatolica (LA) were analyzed quantitatively by GC-MS and Orbitrab HPLC-HRMS. Antioxidant, enzyme inhibitory and anticancer properties were analyzed by various assays. In general, LA exhibited more stronger antioxidant properties compared to LS. The extracts showed similar inhibitory effects on these enzymes. It was determined that LS was dominant in terms of linoleic acid (23.71%), while LA contained a high level of α-linolenic acid (31.70%). LA and LS inhibited the viability of A549 and MCF-7 cells in a dose-dependent manner. IC50 values for LA, LS and cisplatin were determined as 120.3, 197.5, 4.3 µg/mL in A549 cell line and 286.2, 472.8, 7.2 µg/mL in MCF-7 cell line, respectively. It was revealed that LA and LS treatment at 50 µg/mL concentrations in A549 cells completely suppressed the colony forming capacity, and treatment with IC50 doses inhibited cell migration, and triggered apoptosis by regulating caspase-3, cPARP, p53 and p21. The findings of this study suggested that these species have significant pharmacological potential.

Quercetin and Luteolin Improve the Anticancer Effects of 5-Fluorouracil in Human Colorectal Adenocarcinoma In Vitro Model: A Mechanistic Insight.

The aim of this study was to investigate the antitumor effects of quercetin and luteolin combined with 5-Fluorouracil (5-FU) in HT-29 human colorectal cancer cells. Cell viability induced by quercetin, luteolin and combination of these compounds with 5-FU were determined by MTT assay, also Cell death detection Elisa assay and fluorescence microscopy were performed to investigate apoptotic effects. Hu-VEGF Elisa assay was employed to determine the effects of treatments on angiogenesis. Western blot and qRT-PCR analysis were performed to investigate effects on p53, Bax, Bcl-2, p38 MAPK, mTOR, PTEN, and Akt proteins and genes. The results indicated that quercetin, luteolin and combinations of these compounds with 5-FU inhibited the growth of HT 29 cells. Compared to the control, apoptosis were triggered 8.1 and 10.1 fold in HT-29 cells, that treated with quercetin + 5-FU and luteolin + 5-FU, respectively. VEGF amount significantly decreased by combined treatments. qRT-PCR and western blot results demonstrated that quercetin, luteolin and the combinations of these flavonoids with 5-FU, modulate the apoptotic pathways in HT-29 cells. The increase in p53, Bax, p38 MAPK, and PTEN gene expression levels compared to the control group was 1.71, 1.42, 3.26, and 3.29-fold with 5-FU + L treatment, respectively, while this increase was 8.43, 1.65, 3.55, and 3.54-fold with 5-FU + Q treatment, respectively. In addition, when the anti-apoptotic Bcl-2, mTOR, and Akt gene expression levels were normalized as 1 in the control group, they were 0.28, 0.41, and 0.22 with 5-FU + L treatment, and 0.32, 0.46, and 0.39, respectively, with 5-FU + Q treatment. These findings suggested that quercetin and luteolin synergistically enhanced the anticancer effect of 5-FU in HT 29 cells and may therefore minimize the toxic effects of 5-FU in the clinical treatment of colorectal cancer.

In vitro anticancer, antioxidant and enzyme inhibitory potentials of endemic Cephalaria elazigensis var. purpurea with in silico studies.

In this study, the therapeutic potential and phytochemical composition of ethanolic extract of Cephalaria elazigensis var. purpurea (CE), an endemic species, were investigated. For this purpose, the antiproliferative effect of CE on the MCF-7 human breast cancer cell line was evaluated by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay, and its effectiveness on colony formation and cell migration was analyzed with clonogenic assay and wound healing assay, respectively. In addition, the cell death detection ELISA (CDDE) assay was conducted to determine the pro-apoptotic capacity of CE. The IC50 value of the CE was determined as 324.2 ± 14.7 µg/mL. Furthermore, upon 1000 µg/mL CE treatment, there was 4.96-fold increase in the population of cells undergoing apoptosis compared to the untreated control cells. The antioxidant activity tests were performed by DPPH free radical, ABTS cation radical, ferric-ion reducing power (FRAP) and ferrous-ion chelating power (FCAP) assays. Antioxidant activity values for the DPPH, ABTS and FRAP assays were found to be 125.6 ± 6.3, 34.09 ± 0.1 and 123.4 ± 4.2 µmol TE/mg DE, respectively. We further determined the effect of CE ethanolic extract against acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) enzymes. CE plays an effective inhibitory role in AChE and BuChE (AChE: IC50: 10.54 µg/mL, BuChE: IC50: 6.84 µg/mL) respectively. Further, molecular docking stuy was conducted to understand the nature of the all compound against AChE an BChE. It is revealed that α-Linolenic acid shows lowest binding energy (-7.90 kcal/mol) towards AChE, on the other side, Linoleic acid shows good binding affinity (-7.40 kcal/mol) for BChE.Communicated by Ramaswamy H. Sarma.