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Exploring the potential of Inula viscosa extracts for antioxidant, antiproliferative and apoptotic effects on human liver cancer cells and a molecular docking study.

ABSTRACT: In folk medicine, Inula viscosa (Asteraceae) has been traditionally utilized for treating various ailments, including diabetes, bronchitis, diarrhea, rheumatism, and injuries. In this study, we aimed to investigate the chemical composition, antioxidant, antiproliferative, and apoptotic properties of I. viscosa leaf extracts. Extraction was performed using solvents of varying polarities. Antioxidant activity was determined using Ferric reducing antioxidant power (FRAP) and 2,2-azinobis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) assays. The results revealed that aqueous ethanol (70%) and aqueous ethyl acetate (70%) extracts contained high levels of phenols (645.58 ± 8.77 mg CE/g) and flavonoids (180.69 ± 1.54 mg QE/g), respectively. Aqueous ethanol (70%) extract exhibited the highest antioxidant activity with IC50 of 572.74 μmol TE/g DW (μmol Trolox equivalent in 1g of dry extract) in the ABTS assay and 76862.06 μM TE/g DW in the FRAP test. All extracts showed a considerable dose-dependent cytotoxic effect on cancerous HepG2 cells (P < 0.05). The aqueous ethanol extract demonstrated the highest inhibitory effect (IC50 = 1.67 mg/ml). Treatment with aqueous ethanol (70%) and pure ethyl acetate extracts significantly increased the number of apoptotic cells to 8 and 6%, respectively, in HepG2 cells (P < 0.05). Additionally, the aqueous ethanol extract significantly elevatedreactive oxygen species (ROS) levels (53%) in HepG2 cells. The molecular docking study identified paxanthone and banaxanthone E as the compounds that exhibited the highest binding affinities with BCL-2. This study demonstrated the potent antioxidant, antiproliferation, and intracellular ROS production of I. viscosa leaf extracts. Further studies should be conducted to identify the active compounds involved.

SUBMITTER: Kheyar-Kraouche N

PROVIDER: S-EPMC10323743 | biostudies-literature | 2023

REPOSITORIES: biostudies-literature

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Exploring the potential of Inula viscosa extracts for antioxidant, antiproliferative and apoptotic effects on human liver cancer cells and a molecular docking study.

Kheyar-Kraouche Naoual N Boucheffa Saliha S Bellik Yuva Y Farida Kheyar K Brahmi-Chendouh Nabila N

Biotechnologia 20230626 2

In folk medicine, Inula viscosa (Asteraceae) has been traditionally utilized for treating various ailments, including diabetes, bronchitis, diarrhea, rheumatism, and injuries. In this study, we aimed to investigate the chemical composition, antioxidant, antiproliferative, and apoptotic properties of I. viscosa leaf extracts. Extraction was performed using solvents of varying polarities. Antioxidant activity was determined using Ferric reducing antioxidant power (FRAP) and 2,2-azino ...[more]

PMID: 37427027

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Project description:Inula viscosa is a widely used plant in traditional Mediterranean and Middle Eastern medicine for various illnesses. I. viscosa has been shown to have anticancer effects against various cancers, but its effects against lung cancer have been under limited investigation. At the same time, I. viscosa is rich in terpenoids whose anti-lung cancer effects have been poorly investigated. This study aimed to examine the potential anticancer properties of methanolic and aqueous extracts of stems and leaves of I. viscosa and its terpenoid-rich fraction against human lung cancer A549 cells. Results showed that the methanolic extracts of I. viscosa had significantly higher polyphenol and flavonoid content and radical scavenging capacity than the aqueous extracts. In addition, leaves methanolic extracts (IVLM) caused the highest reduction in viability of A549 cells among all the extracts. IVLM also reduced the viability of human ovarian SK-OV-3, breast MCF-7, liver HepG2, and colorectal HCT116 cancer cells. A terpenoid-rich I. viscosa fraction (IVL DCM), prepared by liquid-liquid separation of IVLM in dichloromethane (DCM), displayed a substantial reduction in the viability of A549 cells (IC50 = 27.8 ± 1.5 µg/mL at 48 h) and the panel of tested cancerous cell lines but was not cytotoxic to normal human embryonic fibroblasts (HDFn). The assessment of IVL DCM phytochemical constituents using GC-MS analysis revealed 21 metabolites, highlighting an enrichment in terpenoids, such as lupeol and its derivatives, caryophyllene oxide, betulin, and isopulegol, known to exhibit proapoptotic and antimetastatic functions. IVL DCM also showed robust antioxidant capacity and decent polyphenol and flavonoid contents. Furthermore, Western blotting analysis indicated that IVL DCM reduced proliferation (reduction of proliferation marker Ki67 and induction of proliferation inhibitor proteins P21 and P27), contaminant with P38 MAP kinase activation, and induced the intrinsic apoptotic pathway (P53/BCL2/BAX/Caspase3/PARP) in A549 cells. IVL DCM also reduced the migration of A549 cells, potentially by reducing FAK activation. Future identification of anticancer metabolites of IVL DCM, especially terpenoids, is recommended. These data place I. viscosa as a new resource of herbal anticancer agents.

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Exploring the potential of Inula viscosa extracts for antioxidant, antiproliferative and apoptotic effects on human liver cancer cells and a molecular docking study.

Publications

Exploring the potential of <i>Inula viscosa</i> extracts for antioxidant, antiproliferative and apoptotic effects on human liver cancer cells and a molecular docking study.

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