Antitumor Activity of Ethanolic Extract from Thymbra Spicata L. aerial Parts: Effects on Cell Viability and Proliferation, Apoptosis Induction, STAT3, and NF-kB Signaling.

Thyme-like plants including Thymbra spicata L. are widely used as food and folk medicinal remedies in the Mediterranean area. This study aimed to explore the in vitro antitumor potential of polyphenol-enriched extracts from aerial parts of T. spicata. The ethanolic extract significantly inhibited proliferation of different human tumor cell lines, without significant effects on non-neoplastic cells. A deeper investigation of the molecular mechanism sustaining the in vitro antitumor activity of the extract was carried on the human breast cancer cells MCF-7 in comparison with the normal breast cells MCF-10A. The effects on MCF-7 cells were associated with the following: (i) production of reactive oxygen species (ROS) and release of nitric oxide; (ii) apoptosis induction; and (iii) reduction in STAT3 and NF-kB phosphorylation. The ethanolic extract from T. spicata leaves might represent a novel therapeutic tool in combination with conventional chemotherapy to reduce the adverse side effects and drug resistance.

Repressive effect of Rhus coriaria L. fruit extracts on microglial cells-mediated inflammatory and oxidative stress responses.

ETHNOPHARMACOLOGICAL RELEVANCE: Rhus coriaria L. represents a herbal shrub that is used widely in traditional medicine in the Middle East region to treat different diseases including inflammation-related disorders. R. coriaria extracts have been well characterized in terms of their biological activities, pharmacological potential and phytochemical components. However, the effect of R. coriaria on neuro-inflammation has not been studied previously in detail. AIM OF THE STUDY: In the present study, we performed a qualitative phytochemical analysis and investigated the antioxidant and anti-neuro-inflammatory potential of R. coriaria extracts on BV-2 microglial cells. MATERIALS AND METHODS: R. coriaria extracts were prepared using two different solvents: distilled water and ethanol. Phytochemical screening was performed to determine the principal bioactive components. The radical scavenging activity was assessed by DPPH method (2,2-diphenyl-1-picrylhydrazyl). The effect of R. coriaria on neuro-inflammation was studied upon measuring the production of oxidative stress and inflammatory factors using DCF (2',7'-dichlorofluorescein) and Nitric oxide (NO) assays respectively, and by analyzing the mRNA (TNFα, IL-10, iNOS and COX-2) and protein (NFκß) levels of genes involved BV-2 microglia cells-mediated inflammation using quantitative Real Time PCR and Western blot, respectively. RESULTS: We found that R. coriaria extracts contain high phenolic and flavonoid contents. Interestingly, the ethanolic extract exerted a potent anti-inflammatory potential on insulted BV-2 cells manifested by: i) inhibition of Reactive Oxygen species (ROS) production and nitric oxide (NO) release; ii) suppressing TNFα, iNOS and COX-2 mRNA levels; iii) reducing NFκß activation; and iiii) enhancing IL-10 transcription levels. CONCLUSION: Our results indicate that the neuro-inflammation inhibitory activity of R. coriaria extracts involves the inhibition of NF-κB signaling pathway. These findings suggest that R. coriaria might carry therapeutic potential against neurodegenerative diseases.

Protective effects of extracts from Ephedra foeminea Forssk fruits against oxidative injury in human endothelial cells.

ETHNOPHARMACOLOGICAL RELEVANCE: Ephedra foeminea is a member of the Ephedraceae family which is widespread in the eastern Mediterranean area. In Lebanon, Ephedra is a popular remedy in traditional medicine to prevent and/or counteract many stress oxidative-related diseases like inflammation and bacterial infections. AIM OF THE STUDY: Oxidative stress leads to endothelial cell dysfunction, and is a major factor contributing to etiology of atherosclerosis and related diseases. This study aims to investigate the antioxidant and cytoprotective potential of extracts from E. foeminea fruits on human endothelial cells exposed to hydrogen peroxide (H2O2) to mimic in vitro vascular endothelium dysfunction. MATERIALS AND METHODS: Different extracts of E. foeminea fruits were prepared using pure ethanol (EE), methanol/water (EMW), pure hexane (Ehex) or ethyl acetate/water (Epoly) as extraction solvents. The phenolome profile of each extract was characterized using high-performance liquid chromatography coupled with mass spectrometry (HPLC-MS/MS). Total phenolic and flavonoid content, and radical scavenging properties of the extracts were assessed spectrophotometrically. Then, the effects on human endothelial cells HECV were evaluated. RESULTS: Epoly extract showed the highest phenol and flavonoid content, and the highest radical scavenging capacity. On H2O2-insulted HECV cells Epoly was able: (i) to counteract the ROS/RNS production and lipid peroxidation; (ii) to rescue the ROS-dependent decrease in the mitochondrial membrane potential; (iii) to counteract the apoptosis induction; (iv) to restore endothelial cell viability and migration. CONCLUSIONS: The findings indicated that the polyphenol-enriched extract Epoly from E. foeminea fruits is endowed with in vitro anti-oxidant and anti-apoptotic effects and might be used as nutraceutical for treating ROS-related endothelium dysfunction and inflammation.

Antisteatotic and antioxidant activities of Thymbra spicata L. extracts in hepatic and endothelial cells as in vitro models of non-alcoholic fatty liver disease.

ETHNOPHARMACOLOGICAL RELEVANCE: Thymbra spicata, a member of the Lamiaceae family, is native to eastern Mediterranean area. Leaves of this plant are rich in phenolic compounds and are a popular remedy of traditional medicine in Lebanon to prevent and/or counteract hyperlipidemia and hyperglycemia. AIM OF THE STUDY: To evaluate the antisteatotic and antioxidant activities of extracts from leaves of Thymbra spicata L. using in vitro models of non-alcoholic fatty liver disease (NAFLD), a leading cause of liver-related morbidity and mortality worldwide, for whom no effective treatments are still available. MATERIALS AND METHODS: Two different extracts from Thymbra spicata L. aerial parts were prepared using water (TW) or ethanol (TE) as solvent. Their chemical composition was characterized by gas and liquid chromatography coupled with mass spectrometry. Both extracts were tested on cultured hepatic and endothelial cells treated to mimic in vitro a multisistemic pathology such as NAFLD. We assayed the effects on lipid accumulation, free radical production, lipid peroxidation, cell migration. RESULTS: Both the total phenolic and the total flavonoid contents were higher in the ethanolic extract. Rosmarinic acid was the most abundant polyphenol in TW, while TE was richer in carvacrol. Our findings demonstrated that both extracts ameliorated lipid accumulation, oxidative stress and inflammation in the NAFLD cellular models. However, the aqueous extract was more effective to reduce hepatic steatosis, and the ethanolic extract had higheranti-oxidant potential and wound healing activity. CONCLUSIONS: T. spicata extracts could be promising bioactive products to develop natural therapeutic agents or dietary supplements to treat NAFLD and obesity-related metabolic disease. Our findings suggest that while the ethanolic extract might be used in preventing endothelium dysfunction, the aqueous extract would act better as lipid-lowering agent.

Chemical composition, in vitro cytotoxicity and anti-free radical properties of six extracts from Lebanese Trigonella berythea Boiss.

This study represents an original work aimed to recognize the main constitution of Trigonella berythea. The total phenolic content and total flavonoid content of leaves and stems of T. berythea have been estimated. An extraction and purification of phenolic mixture compounds from the leaves and stems of this plant have been performed and their antioxidant potential using the DPPH, H2O2 and chelating of ferrous ions tests has been evaluated. Then, their cytotoxicity on the MCF7 breast cancer cell line by the XTT Cell Viability technique has been studied. Our results demonstrated that leaves of T. berythea had higher total phenolic content and total flavonoid content than stems. On the other hand, the six extract from leaves and stems of this plant demonstrated a high antioxidant potential reaches more than 80%. Also, extracts from leaves of T. berythea had the highest inhibitory effect on MCF7 and U937 cell growth than that of stems. This inhibition was more than 60% for all extracts. These results provide new insight into the health functions of leaves and stems and demonstrate that T. berythea extracts can potentially have health benefits.

Chemical composition and antioxidant activity of a Lebanese plant Euphorbia macroclada schyzoceras.

OBJECTIVE: To determine the chemical composition, total phenolic and total flavonoid contents of the crude extracts from leaves and stems of a Lebanese plant Euphorbia macroclada schyzoceras (E. macroclada), and to evaluate their antioxidant potential using DPPH, H2O2, and chelating of ferrous ions tests. METHODS: Quantification of the total phenolic and total flavonoid contents of the crude extracts from leaves and stems and the antioxidant activities were evaluated using spectrophotometric analyses. The chemical composition has been estimated using different techniques such as IR, LC/MS and NMR. RESULTS: Ethanolic extract from leaves of E. macroclada was better than aqueous extract and showed higher content in total phenolic and total flavonoid than found in the stems. On the other hand, using DPPH and H2O2 tests, this extract from leaves showed higher antioxidant capacity than aqueous extract. However, using the chelating of ferrous ions test, the antioxidant activity of the aqueous extract of both stems and leaves was stronger than that of ethanolic once. The chemical composition of the whole plant showed the presence of some aromatic compounds and fatty acids. CONCLUSIONS: Both ethanolic and water extracts from both parts of this plant are effective and have good antioxidant power. So, this plant can be used in the prevention of a number of diseases related to oxidative stress.