Phytochemical Compositions and Antidiabetic Potentials of Salvia sclarea L. Essential Oils.

Salvia sclarea (SS) is characterized by its valuable essential oils (Eos) and potent biological activities. This study aimed at investigating the phytochemical composition of SS Eos collected in within the same week, from two different regions in Lebanon, Beirut (SS-Bt) and Taanayel (SS-Tl), utilizing GC-MS methods, and to explore their acute and subchronic antidiabetic potentials. Moreover, studying the phytochemical diversity of twenty SS Eos established on our work and literature descriptions in order to recognize the origin of the Lebanese active chemotype(s). The Eos have been obtained by hydro-distillation and identified via GC-MS analyses. Five chemotypes of SS Eos have been identified. The Lebanese Eos, SS-Bt and SS-Tl, studied here have shown evidence to belong to two different chemotypes 1 and 5, respectively. SS-Bt has shown to belong to chemotype 1, which is characterized by high linalool (LL) concentration (average 40.2%). On the other hand, SS-Tl has shown to belong to chemotype 5, which is characterized by high linalyl acetate (LA) concentration (average 50.4%). The acute and subchronic antidiabetic activities of these EOs have been monitored along with LL and LA, in order to find the most active chemotype. Chemotypes 1 (owned to high LL content), present at low altitude places of Lebanon and Poland, has shown significantly higher acute and subchronic antidiabetic activities than that of chemotype 5 (owned to high LA content). In conclusion, Salvia sclarea Eos have shown potential antidiabetic activities, and their Eos might be used in the future as a complementary or an alternative medicine in the management of diabetes and related complications.

Effects of methanol extracts from roots, leaves, and fruits of the Lebanese strawberry tree (Arbutus andrachne) on cardiac function together with their antioxidant activity.

CONTEXT: Several plant-derived natural products have been used in clinical phase for applications in neurological, cardiovascular, and inflammatory diseases. Arbutus andrachne L. (Ericacea) is an evergreen shrub native to the Mediterranean region. Traditionally, the fruits and leaves of Arbutus tree are well known and used as antiseptics, diuretics, blood tonic, and laxatives. OBJECTIVE: Data regarding the biological effects of compounds derived from the Lebanese Arbutus andrachne are not available. In the present work, we studied the antioxidant activity of methanol extracts of leaves, fruits, and roots of the plant against electrolysis; together with their effects on the cardiodynamics of isolated perfused rabbit hearts. MATERIALS AND METHODS: In vitro electrolysis of the different root, leaves, and fruits methanol extracts was evaluated by the amount of free radicals that has been reduced by increasing the concentration of root extracts ranging from 0.5 to 2 mg after 1, 2, 3, and 4 min. Left ventricular pressure (LVP), heart rate (HR), and coronary flow (CR) were investigated in isolated rabbit heart after administration of 0.5, 1, 2, and 2 mg of each methanol extracts plotted against time (0, 0.5, 1.5, 5, and 10 min), according to the Langendorff method. Lipid peroxidation study was performed by the colorimetric method on myocard tissue after incubation with 500 µl of the different methanol extracts. The amount of MDA was determined at 500 nm absorbance after 5 min incubation. RESULTS: Among the different methanol extracts, the roots showed the highest in vitro antioxidant activity, particularly observed at concentration of 2 mg which completely inhibits free radical generation after 4 min. LVP decreases by 32% at the dose of 2 mg of root extracts after 5 min. No significant effect was observed by the three tested extracts on the heart rate. The three methanol extracts did not show any significant effect on the coronary flow. Moreover, the roots show an increase in the coronary flow at a concentration of 1 and 2 mg/ml during 1 min. Electrolysis on heart tissue treated with the roots extracts shows a decrease in the MDA level from 70.51 ± 6.71 to 48.58 ± 4.15 nmole/g of tissue. DISCUSSION AND CONCLUSION: Methanol extracts of the roots possess antihypertensive effect that may result from its ability to decrease the LVP together with its protective role by inhibiting free radical generation and significantly decreasing the MDA level of heart tissue.

Antibacterial and antibiofilm activities of polysaccharides, essential oil, and fatty oil extracted from Laurus nobilis growing in Lebanon.

OBJECTIVE: To evaluate the antibacterial activity of the extracts of Laurus nobilis against three Gram-positive bacteria (Staphylococcus aureus ATCC 25923, Enterococcus faecalis ATCC 29212 and Staphylococcus epidermidis CIP 444) and two Gram-negative bacteria (Escherichia coli ATCC 35218 and Pseudomonas aeruginosa ATCC 27853). Also, the antibiofilm activity has been investigated against the biofilm produced by Staphylococcus epidermidis CIP 444. MATERIALS: The polysaccharides, essential oil, and fatty oils extracted from the plant were used in broth microdilution methods to study the minimal inhibitory concentration, and then the minimal bactericidal concentration was determined. RESULTS: The results showed that alginate, fucoidan, fatty oils and essential oil have good antibacterial activities against the 5 bacterial strains, and a negligible biofilm eradication activity of fucoidan, laminaran, fatty oil, and essential oil was observed, but a promising biofilm eradication activity was obtained with alginate, which showed a reduced biofilm mass even at low concentration. CONCLUSIONS: The extracts obtained have promising antibacterial capacities which need further investigation for them to be incorporated in medical or nutritional applications.

In vitro cytotoxic and anticlastogenic activities of saxifragifolin B and cyclamin isolated from Cyclamen persicum and Cyclamen libanoticum.

CONTEXT: The genus Cyclamen L. (Primulaceae) is rich in saponins known to have interesting biological activities. OBJECTIVE: To isolate saxifragifolin B and cyclamin, two triterpene saponins, from Cyclamen libanoticum Hildebr and Cyclamen persicum Mill, and to assess their cytotoxic, clastogenic/aneugenic, and anticlastogenic effects, as well as antioxidant potential. MATERIALS AND METHODS: Saxifragifolin B and cyclamin were tested for their cytotoxicity against SK-BR-3, HT-29, HepG2/3A, NCI-H1299, BXPC-3, 22RV1, and normal DMEM cell lines using WST-1 assay. Their clastogenic/aneugenic activities and anticlastogenic effects against the anticancer drug mitomycin C were assessed by the in vitro micronucleus assay in CHO cells. Their antioxidant capacities were determined using Fe(2+)-chelating and 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging assays. RESULTS: Both saponins were described for the first time in Cyclamen libanoticum. They showed strong cytotoxic activities against the tested cancer cell lines. Saxifragifolin B was found to be 56- and 37-times more active than mitomycin C against breast adenocarcinoma (SK-BR-3) and lung carcinoma (NCI-H1299), respectively. Also, saxifragifolin B did not induce micronuclei formation and prevented cells from mitomycin C clastogenic effect. Cyclamin induced a significant increase of micronucleated cells after metabolic activation with S9 mix, and did not possess any anticlastogenic activity. Both molecules exhibited low antioxidant activities as compared to reference compounds. DISCUSSION AND CONCLUSIONS: This study showed the remarkable cytotoxic activity of saxifragifolin B, especially against breast adenocarcinoma and lung carcinoma and its chemoprotective activity against mitomycin C. Thus, saxifragifolin B could be suggested as a potential cytotoxic drug with a preventive effect against possible exposures to genotoxic agents.

Electron beam and gamma radiolysis of solid-state metoclopramide.

PURPOSE: Study the radiolysis of solid-state metoclopramide hydrochloride at various absorbed doses. Elucidate the structure of the degradation products to gain information on the radiolysis mechanisms. METHODS: Solid-state metoclopramide samples were irradiated at several doses with gamma rays and high-energy electrons to evaluate the influence of the dose rate. High-performance liquid chromatography with a diode array detector was used to measure the chemical potency as a function of the absorbed dose and to quantify the degradation products. The characterization of degradation products was performed by liquid chromatography/atmospheric pressure chemical ionization/tandem mass spectrometry. RESULTS: The degradation of solid-state metoclopramide after irradiation was negligible. No qualitative or quantitative differences were observed between gamma and electron beam irradiations (no dose rate effect). Four degradation products that were similar to metoclopramide were detected in trace levels (below 0.1% of the drug concentration) and were not unique to irradiation because they were found in lower amounts in unirradiated metoclopramide. The major degradation product formed after radiation was due to the loss of the chlorine atom from the metoclopramide molecule. CONCLUSION: Solid-state metoclopramide is radioresistant from a chemical point of view and therefore could be a suitable candidate for radiosterilization studies by either gamma rays or high-energy electrons.