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The inhibitory activity of alpha-amylase and the phytochemical composition of Cedrus libani essential oils obtained from wood, leaves and cones were investigated. The C. libani woods oil exhibit an IC(50) value of 0.14 mg/ml, whereas the leaves and cones oils were devoid of any significant activity. [ABSTRACT FROM AUTHOR]

Consultation for liver disease during pregnancy is challenging for both the hepatologist and gynecologist, as normal physiologic changes during pregnancy can mimic chronic liver disease. Pregnancy-specific liver disorders are leading causes of abnormal liver function tests during pregnancy. Moreover, up to 3% of all pregnant women in developed countries experience liver diseases nonspecific to pregnancy. When severe, pregnancy-specific liver disorders are associated with significant morbidity and mortality for both the mother and the fetus. The main factors that determine maternal prognosis are the type of liver disease; degree of impaired synthetic, metabolic, and excretory liver function; and timing of delivery. This article focuses on a systematic approach to diagnosing and managing pregnancy-specific liver disorders, which includes understanding normal findings in pregnancy, excluding liver diseases nonspecific to pregnancy, factoring in trimester status, and using clinical clues to make a diagnosis and provide treatment in a timely fashion., Competing Interests: Disclosures: The authors have no relevant conflicts of interest to disclose., (Copyright © 2021, Gastro-Hep Communications, Inc.)

Natural products frequently exert pharmacological activities. The present review gives an overview of the ethnobotany, phytochemistry and pharmacology of the Cedrus genus, e.g. cytotoxic, spasmolytic immunomodulatory, antiallergic, anti-inflammatory and analgesic activities. Cancer patients frequently seek remedies from traditional medicinal plants that are believed to exert less side effects than conventional therapy with synthetic drugs. A long-lasting goal of anti-cancer and anti-microbial therapy research is to find compounds with reduced side effects compared to currently approved drugs. In this respect, Cedrus species might be of interest. The essential oil isolated from Cedrus libani leaves may bear potential for drug development due to its high concentrations of germacrene D and β-caryophyllene. The essential oils from Cedrus species also show bioactivity against bacteria and viruses. More preclinical analyses (e.g. in vivo experiments) as well as clinical trials are required to evaluate the potential of essential oils from Cedrus species for drug development.

The frequent failure of standard cancer chemotherapy requires the development of novel drugs capable of killing otherwise drug-resistant tumors. Here, we have investigated a chloroform extract of Laurus nobilis seeds. Fatty acids and 23 constituents of the volatile fraction were identified by gas chromotography/flame ionization detection (GC/FID) and gas chromatography/mass spectrometry (GC/MS), in good agreement with (1)H NMR (nuclear magnetic resonance) spectrum. Multidrug-resistant P-glycoprotein-expressing CEM/ADR5000 leukemia cells were hypersensitive (collaterally sensitive) toward this extract compared to drug-sensitive CCRF-CEM cells, whereas CEM/ADR5000 cells were 2586-fold resistant to doxorubicin as control drug. Collateral sensitivity was verified by measurement of apoptotic cells by flow cytometry. The log10IC50 values of 3 compounds in the extract (limonene, eucalyptol, oleic acid) did not correlate with mRNA expression of the P-glycoprotein-coding ABCB1/MDR1 gene and accumulation of the P-glycoprotein substrate rhodamine in the NCI panel of tumor cell lines. A microarray-based profile of 20 genes predicted resistance to doxorubicin and 7 other anticancer drugs involved in the multidrug resistance phenotype but not to limonene, eucalyptol and oleic acid. In conclusion, our results show that Laurus nobilis seed extract is suitable to kill multidrug-resistant P-glycoprotein expressing tumor cells.

A set of 6-substituted quinolone nucleosides linked to aniline or phenol via N or O heteroatom-bridges presenting new compounds were synthesized by palladium-catalyzed Buchwald-Hartwig cross-coupling reactions. 6-Bromoquinolone nucleoside precursors, being protected by either benzoyl or TBDMS protecting groups on the ribose moiety, were subjected to different Buchwald-Hartwig conditions as the key step. Defined deprotection steps led, in good yields, to the final target compounds that carry, in position 3, either ester, acid, or amide functions. Thus, a series of novel quinolone nucleoside derivatives was obtained via a convergent synthesis route. Biological tests in human chronic myelogenous leukemia K562 cells exerted an efficient antiproliferative activity for two of them without induction of differentiation. These novel nucleosides deserve further experiments to determine their antiproliferative effects on other CML cell lines., (© 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.)

Five piperazine derivatives (S)-4-benzyl-1-(4-bromo-3-methylphenyl)-2 methylpiperazine (A), (S)-1-benzyl-3-isobutylpiperazine-2,5-dione (B), (S)-1-benzyl-3 methylpiperazine-2,5-dione (C), (S)-1,3-dibenzylpiperazine-2,5-dione (D), (E)-1-(3-methyl 4-((E)-3-(2-methylpropylidene) piperazin-1-yl) phenyl)-2-(2 methylpropylidene) piperazine (E) and triphenyl derivative ammonium 2-((2,3',3''-trimethyl-[1,1':4',1''-terphenyl]-4 yl)oxy)acetate (F) were tested for inhibition of K-562 cell proliferation and for induction of erythroid differentiation. Among them, two piperazine and one triphenyl derivatives, compounds A, E, and F inhibited the proliferation of the K562 cell lines exhibiting inhibition concentration 50 (IC50) (IC50) of values 30.10±1.6, 4.60±0.4 and 25.70±1.10 μg ml(-1), respectively. If compound A and F were added to suboptimal concentrations of the established anticancer drugs cytosine arabinoside or mithramycin, pronounced synergic effects were observed.

The antioxidant and antiproliferative activities of the essential oils from Laurus nobilis leaves and seeds in relation to their composition were analysed. The most abundant components of the leaf essential oil were 1,8-cineole, 1-p-menthen-8-ethyl acetate, linalool and sabinene, while the seed oil was characterised by β-ocimene, 1,8-cineole, α-pinene and β-pinene as main constituents. Both seed and leaf essential oils exhibited a scavenging effect on the DPPH radical, with IC₅₀ values of 66.1 and 53.5 µg mL⁻¹, respectively. The leaf essential oil showed the strongest antioxidant activity in the β-carotene/linoleic acid system, with an IC₅₀ value of 35.6 µg mL⁻¹ after 30 min of incubation. Both leaf and seed oils inhibited proliferation of the K562 tumour cell line with IC₅₀ values of 95 and 75 µg mL⁻¹, respectively. The L. nobilis leaf oil showed a percentage of erythroide differentiation of 15% at a concentration of 10 µg mL⁻¹. A value of 12% was found for the seed essential oil at a concentration of 50 µg mL⁻¹. When the oils were added to a suboptimal concentration of the commercial drug, cytosine arabinoside, a clear synergic effect was observed.

There are four kinds of Cedar: Cedrus libani naturally occurring in Lebanon, Syria and Turkey, Cedrus atlantica in Morocco and Algeria, Cedrus brevefolia in Cyprus Island and Cedrus deodara which is distributed in Himalayan Mountains. Wood essential oils obtained from C. libani, C. atlantica and C. deodara were tested for the inhibition of K562 cell proliferation and for the induction of erythroid differentiation. The wood essential oils of C. libani, C. atlantica and C. deodara inhibited the proliferation of the K562 cell line exhibiting IC(50) values 23.38 ± 1.7, 59.37 ± 2.6 and 37.09 ± 1.4 µg mL(-1), respectively. Meanwhile, C. libani wood oils induced a percentage of erythroid differentiation of 15 ± 2% at concentration 5 µg mL(-1). Cedrus deodara wood oil indicated a percentage of erythroid differentiation of 20 ± 2% at concentration 25 µg mL(-1) and C. atlantica wood oils showed a percentage of erythroid differentiation of 12 ± 1.8% at concentration 10 µg mL(-1).

The Morris water maze is a commonly employed method to investigate learning and memory. The task demands experimental subjects use distal spatial cues in navigating to a hidden escape platform while swimming in a pool of opaque water. Since its primary description thirty years ago, several modifications have emerged. For example, part-way through the experiment, the target platform can be re-located, thus requiring subjects re-learn spatial aspects of the task. This procedure demands sequential memory encoding of highly similar events and can be selectively impaired by genetic and pharmacological methods affecting cognitive flexibility. While the primary reasons for employing re-locating platform tasks are to study aspects of cognitive flexibility, the paradigms also demonstrate a potential for reducing within-treatment group variation by enabling within-subject analysis. We tested this hypothesis using the C57BL/6 mouse line, a commonly chosen subject for behavioral experiments, and demonstrate that a within-subject comparison approach is both valid and effective in reducing variability. Interestingly, the within-subject statistical advantage is most pronounced for performance measures of short-term memory. In addition, we find that subject naivety, but not experimental inter-phase interval or subcutaneous saline injections, has a significant effect on variation in performance. We also found repeated training in the Morris water maze improved short-term memory without enhancing long-term memory. Together, the data suggest platform re-location tasks can help alleviate within-group variability, a major conundrum in behavioral neuroscience, and provide valuable insight into the general sources of variability underlying performance in cognitive tasks., (Copyright © 2011 Elsevier B.V. All rights reserved.)

Objectives: The purpose of this study was to evaluate cytotoxic activity of Platycladus orientalis, Prangos asperula and Cupressus sempervirens ssp. pyramidalis essential oils and to identify active components involved in inhibition of population growth of human cancer cell lines., Materials and Methods: Essential oils were obtained by hydrodistillation and were analysed by gas chromatography and gas chromatography coupled to mass spectrometry. Antiproliferative activity was tested on amelanotic melanoma C32 cells and on renal cell adenocarcinoma cells, using the sulphorhodamine B assay., Results: Cupressus sempervirens ssp. pyramidalis leaf oil exerted the highest cytotoxic activity with an IC(50)value of 104.90 microg/mL against C32, followed by activity of P. orientalis and P. asperula on the renal adenocarcinoma cell line (IC(50) of 121.93 and 139.17 microg/mL, respectively). P. orientalis essential oil was also active against amelanotic melanoma with an IC(50) of 330.04 microg/mL. Three identified terpenes, linalool, beta-caryophyllene and alpha-cedrol, were found to be active on both cell lines tested., Conclusions: Our findings provide novel insights into the field of cytotoxic properties of essential oils. This study provided evidence on how cytotoxic activity of the oils is not always related to their major constituents, except for lower activity found in both cell lines for alpha-cedrol. Interestingly, beta-caryophyllene and linalool exhibited comparable IC(50) values to the commercial drug vinblastine on the ACHN cell line. This opens a new field of investigation to discover mechanisms responsible for the observed activity.

Aim of the Study: In recent years the use of medicinal plants has been growing worldwide and this is particularly true in Lebanon. In the present investigation we report the inhibitory activity against digestive enzymes related to diabetes and angiotensin converting enzyme (ACE) of extracts of nine plant species collected in Lebanon, where they have a traditional use against diabetes., Materials and Methods: In order to evaluate if the extraction procedure could influence the activity we decided to perform different extractions with methanol, n-hexane and chloroform of Calamintha origanifolia, Satureja thymbra, Prangos asperula, Sideritis perfoliata, Asperula glomerata, Hyssopus officinalis, Erythraea centaurium, Marrubium radiatum and Salvia acetabulosa and test each of them., Results and Conclusions: Marrubium radiatum and Salvia acetabulosa methanol extracts exerted the highest activity against alpha-amylase (IC(50) 61.1 and 91.2 microg/ml, respectively) and alpha-glucosidase (IC(50) 68.8 and 76.9 microg/ml, respectively). The same extracts exhibited a strong inhibitory activity against ACE with IC(50) of 72.7 and 52.7 microg/ml, respectively. The results support the traditional use of some the species examined.

The chemical composition of the essential oils of Laurus nobilis, Juniperus oxycedrus ssp. oxycedrus, Thuja orientalis, Cupressus sempervirens ssp. pyramidalis, Pistacia palaestina, Salvia officinalis, and Satureja thymbra was determined by GC/MS analysis. Essential oils have been evaluated for their inhibitory activity against SARS-CoV and HSV-1 replication in vitro by visually scoring of the virus-induced cytopathogenic effect post-infection. L. nobilis oil exerted an interesting activity against SARS-CoV with an IC(50) value of 120 microg/ml and a selectivity index (SI) of 4.16. This oil was characterized by the presence of beta-ocimene, 1,8-cineole, alpha-pinene, and beta-pinene as the main constituents. J. oxycedrus ssp. oxycedrus oil, in which alpha-pinene and beta-myrcene were the major constituents, revealed antiviral activity against HSV-1 with an IC(50) value of 200 microg/ml and a SI of 5.

Background: The aim of this work was to study the cytotoxicity of essential oils and their identified constituents from Sideritis perfoliata, Satureia thymbra, Salvia officinalis, Laurus nobilis and Pistacia palestina., Materials and Methods: Essential oils were obtained by hydrodistillation and were analysed by gas chromatography (GC) and GC/mass spectrometry (MS). The cytotoxic activity was evaluated in amelanotic melanoma C32, renal cell adenocarcinoma ACHN, hormone-dependent prostate carcinoma LNCaP, and MCF-7 breast cancer cell lines by the sulforhodamine B (SRB) assay., Results: L. nobilis fruit oil exerted the highest activity with IC50 values on C32 and ACHN of 75.45 and 78.24 microg/ml, respectively. The activity of S. perfoliata oil on both cell lines (IC50 of 100.90 mg/ml for C32 and 98.58 microg/ml for ACHN, respectively) was also interesting. Among the tested constituents the highest activity was found when a-humulene was applied to LNCaP cells (IC50 of 11.24 microg/ml)., Conclusion: This study suggests for the first time the ability of S. perfoliata, S. thymbra, S. officinalis, L. nobilis and P. palestina essential oils and some identified terpenes to inhibit human tumor cell growth.

The essential oils obtained from different officinal plants of Lebanon, belonging to the Magnoliophyta division, have been tested for their antiproliferative activity on human erythroleukemic K562 cells. Satureja montana showed the most interesting biological activity in inhibiting the cell growth and inducing erythroid differentiation of K562 cells. The essential oil of Satureja montana was therefore analyzed using a GC/MS (gas chromatography/mass spectrometry) system in order to identify the major constituents and compare them with analysis performed on Satureja hortensis. We demonstrated that the essential oil composition varied with the species, the major constituent of Satureja hortensis being carvacrol (50.61%) and that of Satureja montana being alpha-terpineol (12.66%). In order to identify molecules possibly responsible for the biological activity, commercially available derivatives have been assayed on the K562 cell line. Satureja montana essential oil displayed different natural derivatives characterized by higher activity than those present in Satureja hortensis. The common active principles are alpha-pinene, gamma-terpinene, 4-terpineol, alpha-terpineol, tau-cadinene, tau-cadinol and caryophyllene. Both caryophyllene and alpha-terpineol showed important antiproliferative effects on K562 cells.