Alzheimers disease (AD) is the most common form of neurodegenerative disorders. If more effective therapies than the ones currently available are not developed that either prevent AD or other ...neurodegenerative or block progression of the diseases in its very early stages, the economic and societal cost of caring for AD patients will be devastating. Besides the neuropathologic hallmarks of the diseases, namely neurofibrillary tangles and AD neuritic plaques, the disease is characterized neurochemically by a consistent deficit in cholinergic neurotransmission, particularly affecting cholinergic neurons in basal forebrain. AD and other forms of dementia could be treated by the use of agents which restore the level of acetylcholine through inhibition of both two major forms of cholinesterase: acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). Moreover, the inhibition of AChE holds a key role not only to enhance cholinergic transmission in the brain but also to reduce the aggregation of β-amyloid and the formation of the neurotoxic fibrils in AD. Following this view, in recent years, an increased interest has emerged directed to finding drugs able to inhibit both of these events. This review summarizes and highlights recent advances in current knowdlege on natural products as cholinesterase inhibitors and how these compounds have also served as the starting points for semi-synthetic analogs with improved properties.
Iridoids represent a large group of cyclopentacpyran monoterpenoids that occur wide-spread in nature, mainly in dicotyledonous plant families like Apocynaceae, Scrophulariaceae, Diervillaceae, ...Lamiaceae, Loganiaceae and Rubiaceae. Recently, more extensive studies revealed that iridoids exhibit a wide range of bioactivity, such as neuroprotective, antinflammatory and immunomodulator, hepatoprotective and cardioprotective effects. Anticancer, antioxidant, antimicrobic, hypoglycaemic, hypolipidemic, choleretic, antispasmodic and purgative properties were also reported. The aim of the present review is to discuss the recent developments on biological and pharmacological activities of iridoids, supporting the new therapeutic possibilities for the use of these compounds.
The essential oils of four
Teucrium species were studied and 150 components, in all, were identified. All oils were rich in sesquiterpenes (50.1–55.8%). Spathulenol and δ-cadinene were the main ...compounds of
Teucrium brevifolium oil; caryophyllene and 4-vinyl guaiacol predominated in
Teucrium flavum. Carvacrol and caryophyllene oxide predominated in
Teucrium montbretii ssp.
heliotropiifolium, while carvacrol and caryophyllene were the most abundant components in
Teucrium polium ssp.
capitatum. The oil which most effectively inhibited LPS-induced NO production in macrophage cell line RAW 264.7 was that from
T. brevifolium (IC
50
=
7.1
μg/ml), followed by
T. montbretii ssp.
heliotropiifolium and
T. polium ssp.
capitatum (IC
50
=
16.5 and 29.4
μg/ml, respectively). The
in vitro cytotoxic assay on three human cancer cell lines showed that the most antiproliferative oils were those from
T. polium ssp.
capitatum and
T. montbretii ssp.
heliotropiifolium on CACO-2 cell lines (IC
50
=
52.7 and 92.2
μg/ml, respectively). The
T. brevifolium oil showed a selective cytotoxicity on COR-L23 while significant activity was exerted by
T. polium oil on C32.
The essential oils of
Origanum ehrenbergii and
O. syriacum collected in Lebanon were analysed by GC and GC–MS and evaluated for their anticholinesterase, NO production inhibitory activities, and ...antioxidant properties.
O.
ehrenbergi essential oil was characterised by the presence of 37 components, representing 94.9% of the total oil of which thymol (19%) and
p-cymene (16.1%) were the main abundant compounds. Thirty-six compounds characterised the
O.
syriacum essential oil, representing 90.6% of the total oil. The most abundant components were thymol (24.7%) and carvacrol (17.6%).
O. ehrenbergii demonstrated interesting scavenging effects on DPPH with an IC
50 value of 0.99
μg/ml. In addition, both
O. ehrenbergii and
O. syriacum oils inhibited oxidation of linoleic acid after 30
min of incubation, as well as after 60
min of incubation with IC
50 values of 42.1 and 33.6
μg/ml, and 46.9 and 58.9
μg/ml, respectively. Interestingly,
O. ehrenbergii oil inhibited NO production in the murine monocytic macrophage cell line RAW 264.7 with an IC
50 value of 66.4
μg/ml. Acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibition was assessed by modifications of the Ellman’s method.
O. ehrenbergii exhibited a strong activity against both cholinesterases with IC
50 values of 0.3
μg/ml. The data suggest that
O. ehrenbergii and
O. syriacum oils could be used as a valuable new flavour with functional properties for food or nutriceutical products with particular relevance to supplements for the elderly.
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 IC 50 values on C32 and ACHN of 75.45 and 78.24 μg/ml, respectively. The activity of S. perfoliata oil on both cell lines (IC 50 of 100.90 mg/ml for C32 and 98.58 μg/ml for ACHN, respectively) was also interesting. Among the tested constituents the highest
activity was found when α-humulene was applied to LNCaP cells (IC 50 of 11.24 μg/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.
Objectives
This study involves for the first time the evaluation of Berberis aetnensis C. Presl. and Berberis libanotica Ehrenb. ex C.K. Schneid. roots for anticholinesterase and antioxidant ...properties, with the aim to search compounds possibly useful for the treatment of Alzheimer's disease (AD).
Methods
Samples were evaluated for their ability to inhibit acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). The antioxidant activity was assayed by 2,2‐diphenyl‐1‐picrylhydrazyl radical and β‐carotene bleaching tests. Berberine and palmatine were isolated by flash chromatography and identified by spectrometric methods as main constituents. Non‐polar compounds were analysed by gas chromatography and gas chromatography‐mass spectrometry.
Key findings
Extracts, fractions and isolated compounds inhibited AChE and BChE to varying degrees. The methanol fractions exhibited the strongest AChE inhibitory activity with inhibitory concentration 50% (IC50) of 7.6 and 16.9 μg/ml for B. aetnensis and B. libanotica, respectively. The alkaloid fraction of B. aetnensis inhibited AChE (IC50 of 24.5 μg/ml) and possessed the highest antioxidant activity (IC50 value of 2.2 μg/ml in β‐carotene‐bleaching test after 30 min of incubation). Berberine was more potent of palmatine against AChE (IC50 of 2.2 and 7.4 μg/ml, respectively).
Conclusions
These findings raise the possibility of developing B. aetnensis and B. libanotica as a promising candidate for the treatment of AD.
In this study the chemical composition, cholinesterase inhibitory property and anti-inflammatory activity of S. leriifolia Benth. essential oil was evaluated for the first time. GC and GC-MS analysis ...revealed the presence of camphor (10.5%), 1,8-cineole (8.6%), camphene (6.2%) and α-pinene (4.7%) as main constituents. S. leriifolia oil exhibited a promising antioxidant activity by DPPH assay with an IC50 2.26 μL/mL. Interesting cholinesterase inhibitory activity was also found with IC50 values of 0.32 and 0.29 μL/mL for acetylcholinesterase (AChE) and butyrrylcholinesterase (BChE), respectively. Moreover, this oil inhibited LPS-induced NO production with an IC50 value of 165 μg/mL. The absence of cytotoxicity at 1000 μg/mL was evaluated by MTT assay in 142BR cells.
ABSTRACT In the present study the in vitro hypoglycemic and anti-acetylcholinesterase activities of hot pepper fruits (Capsicum annuum var. acuminatum L.) at different ripening stages were ...investigated. The mature, green-stage fruits had the highest activity against alpha-amylase and alpha-glucosidase with 50% inhibitory concentration (IC(50)) values of 55.88 and 76.11 microg/mL, respectively, while C. annuum var. acuminatum in the prematurity green stage exhibited the highest acetylcholinesterase inhibition property (IC(50) = 84.30 microg/mL), using the Ellman method. This study highlights the biochemical rationale for chemopreventive significance in health benefits when consuming this variety of pepper.
The aim of this work was to examine the chemical composition and antiproliferative activity of Salvia leriifolia Benth. and Salvia acetabulosa L. oils. S. leriifolia oil was characterized by 50 ...components, whereas 19 components were identified in S. acetabulosa. S. leriifolia oil was characterized by camphor (10.5%), 1,8-cineole (8.6%), camphene (6.2%), and alpha-pinene (4.7%). alpha-Pinene (52.3%), 1,8-cineole (27.7%), and camphor (6.7%) were the major components in S. acetabulosa oil. Both oils exerted a strong antiproliferative activity comparing with vinblastine against COR-L23 with 50% inhibitory concentration (IC(50)) values of 7.5 and 6.5 microg/mL for S. leriifolia and S. acetabulosa, respectively. Salvia oils showed an interesting activity also on C32 (IC(50) = 6.3 and 9.1 microg/mL for S. acetabulosa and S. leriifolia, respectively). S. acetabulosa was also found to possess cytotoxic activity against renal adenocarcinoma (IC(50) = 6.8 microg/mL). The results clearly showed that for both Salvia species the antiproliferative activity could not be related to the major abundant compounds. Consequently, the minor components may be involved in some type of synergism with the other active compounds.
: The interest in medicinal plant research and in the aroma‐therapeutic effects of essential oils in humans has increased in recent years, especially for the treatment of pathologies of relevant ...social impact such as Alzheimer's disease. The present study was taken up to evaluate the antioxidant capacity and the acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activity of the peel essential oils from three Citrus species, C. aurantifolia Swingle, C. aurantium L., and C. bergamia Risso & Poit. Essential oils were analyzed by GC and GC‐MS and they contain mainly limonene, α‐pinene, β‐pinene, γ‐terpinene, and linalyl acetate. C. aurantifolia oil showed the highest radical scavenging activity on ABTS assay (IC50 value of 19.6 μg/mL), while C. bergamia exhibited a good antioxidant activity evaluated by the β‐carotene bleaching test (IC50= 42.6 μg/mL after 60 min of incubation). C. aurantifolia inhibited more selectively AChE. Obtained data suggest a potential use of Citrus oils as a valuable new flavor with functional properties for food or nutraceutical products with particular relevance to supplements for the elderly.
Practical Application: The demonstrated antioxidant activity and procholinesterase properties of Citrus essential oils suggested their use as a new potential source of natural antioxidant to added as extra‐nutrient for using in food industries as a valuable new flavor with functional properties for food or nutraceutical products with particular relevance to supplements for the elderly.
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