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1.
Chem Biodivers ; 21(9): e202400552, 2024 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-38958194

RESUMO

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.


Assuntos
Antineoplásicos Fitogênicos , Antioxidantes , Proliferação de Células , Sobrevivência Celular , Ensaios de Seleção de Medicamentos Antitumorais , Lactuca , Humanos , Antioxidantes/farmacologia , Antioxidantes/química , Antioxidantes/isolamento & purificação , Lactuca/efeitos dos fármacos , Lactuca/química , Antineoplásicos Fitogênicos/farmacologia , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/isolamento & purificação , Proliferação de Células/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/química , Compostos Fitoquímicos/isolamento & purificação , Células A549 , Apoptose/efeitos dos fármacos , Relação Dose-Resposta a Droga , Inibidores Enzimáticos/farmacologia , Inibidores Enzimáticos/química , Inibidores Enzimáticos/isolamento & purificação , Células MCF-7 , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Antineoplásicos/farmacologia , Antineoplásicos/química , Antineoplásicos/isolamento & purificação , Linhagem Celular Tumoral
2.
J Biomol Struct Dyn ; 41(21): 11832-11844, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-36637391

RESUMO

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.


Assuntos
Antioxidantes , Dipsacaceae , Humanos , Antioxidantes/farmacologia , Antioxidantes/química , Butirilcolinesterase/metabolismo , Acetilcolinesterase/metabolismo , Inibidores da Colinesterase/farmacologia , Inibidores da Colinesterase/química , Dipsacaceae/metabolismo , Simulação de Acoplamento Molecular , Extratos Vegetais/farmacologia , Extratos Vegetais/química
3.
Bioorg Chem ; 113: 105032, 2021 08.
Artigo em Inglês | MEDLINE | ID: mdl-34089947

RESUMO

This study attempts to evaluate the antioxidant, enzyme inhibitory, and anticancer properties as well as fatty acid compositions of endemic Saponaria prostrata WILLD. subsp. anatolica HEDGE. The gas chromatography-mass spectrometry (GC-MS) was used to determine the fatty acid content of methanol: dichloromethane extract from S. prostrata subsp. anatolica (SPA). Enzymatic activity was measured against acetylcholinesterase, butyrylcholinesterase and α-glucosidase. DPPH (2,2-diphenyl-1-picrylhydrazyl) free radical scavenging activity and Ferric reducing antioxidant power assay (FRAP) were conducted to antioxidant properties. The anticancer effect of SPA on human MCF-7 breast cancer and human HCT116 colorectal cancer cell line was evaluated by WST-1 cell viability assay, colony formation assay and wound healing assay. In addition, human VEGF Elisa method was used to determine the anti-angiogenic effect, and the quantitative real-time PCR (qRT-PCR) method on p53, Bax and Bcl-2 mRNA levels were used to evaluate apoptosis. While high amounts of palmitic acid (40.8%), linoleic acid (17.75%) and α-linolenic acid (16.84%) were detected in the SPA, the total amount of unsaturated fatty acid (51.34%) was higher than the total amount of saturated fatty acid (48.66%). SPA displayed the most promising acetylcholinesterase (AChE), butyrylcholinesterase (BuChE) and α-glycosidase (AG) inhibitory activities (AChE: IC50: 18.03 µg/mL, BuChE: IC50: 44.24 µg/mL and AG: IC50: 210.85 µg/mL). The half maximum inhibitory concentration (IC50) of SPA in MCF-7 and HCT116 cells was determined as 259.79 µg/mL and 97.24 µg/mL, respectively. In addition, it was determined that SPA suppresses colony formation and wound closure, and suppresses angiogenesis as well as triggering apoptosis at a significant level. It is true that endemic S. prostrata subsp. anatolica is a potential source of functional food ingredients, but more analytical and in vivo experiments are needed to explore further secondary metabolite diversity and pharmacological properties.


Assuntos
Antineoplásicos Fitogênicos/química , Antioxidantes/química , Ácidos Graxos/análise , Extratos Vegetais/química , Saponaria/química , Acetilcolinesterase/química , Acetilcolinesterase/metabolismo , Inibidores da Angiogênese/química , Inibidores da Angiogênese/metabolismo , Inibidores da Angiogênese/farmacologia , Antineoplásicos Fitogênicos/metabolismo , Antineoplásicos Fitogênicos/farmacologia , Apoptose/efeitos dos fármacos , Butirilcolinesterase/química , Butirilcolinesterase/metabolismo , Linhagem Celular Tumoral , Movimento Celular/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Inibidores da Colinesterase/química , Inibidores da Colinesterase/metabolismo , Inibidores de Glicosídeo Hidrolases/química , Inibidores de Glicosídeo Hidrolases/metabolismo , Humanos , Saponaria/metabolismo , alfa-Glucosidases/química , alfa-Glucosidases/metabolismo
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