Giancarlo A. Statti

In vivo anti-inflammatory and in vitro antioxidant activities of Mediterranean dietary plants.

Five hydroalcoholic extracts of edible plants from Calabria region (Italy) used in local traditional medicine for the treatment of inflammatory diseases were evaluated for their in vivo topical anti-inflammatory activity (inhibition of croton oil-induced ear oedema in mice) and in vitro antioxidant and antiradical properties (inhibition of linoleic acid oxidation and bovine brain liposomes peroxidation, DPPH radical scavenging). All the extracts showed an anti-inflammatory effect: 300 microg/cm(2) provoked oedema reductions ranging from 21 to 27%. All the extracts exerted also radical scavenging and/or antioxidant properties, the most active plant being Mentha aquatica L. (Lamiaceae) which contained the highest amount of phenolics (337 mg/g) and of flavonoids (15.75 mg/g). Moreover, the content and the composition of sterols were assessed by GC-MS in the examined plants Borago officinalis L. (Boraginaceae) contained the highest number of sterols.

Biological and Pharmacological Activities of Iridoids: Recent Developments

Iridoids represent a large group of cyclopenta[c]pyran 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.

Estrogenic and antiproliferative activities of isoliquiritigenin in MCF7 breast cancer cells

Licorice root contains chemically diverse compounds that exhibit estrogenic effects in vitro and in vivo. The chalcone isoliquiritigenin (ISL) is a component of licorice extract exhibiting either antitumorigenic activity or estrogen receptor (ER) alpha-dependent growth promoting effects on breast cancer cells. In order to contribute to a better understanding of this apparent paradox, we synthesized and ascertained the estrogenic properties of ISL using, as model systems, the hormone-sensitive MCF7 breast cancer cells and the steroid-independent HeLa cells. Transfection experiments reveal that ISL is able to transactivate the endogenous ER alpha in MCF7 cells and this is supported by the capability to induce down-regulation of ER alpha protein levels and up-regulation of pS2 mRNA. Moreover, by using chimeric proteins consisting of the hormone binding domains of ER alpha and ER beta fused to the Gal4 DNA binding domain, we have determined that ISL is an estrogenic agonist of both ER isoforms. As a biological counterpart, low and intermediate ISL concentrations that induce substantial transcriptional activity stimulate the proliferation of MCF7 cells. However, high levels of ISL become cytotoxic even in steroid-receptor negative HeLa cells. Thus, the activity of ISL and the balance between risk or chemopreventive factor for estrogen-dependent breast cancer may depend on dietary intake.

Antioxidant activity of methanolic extract of Hypericum triquetrifolium Turra aerial part

The antioxidant activity of the methanol extract of Hypericum triquetrifolium Turra (Hypericaceae) aerial part and of flavonoids isolated therein, I3,II8-biapigenin, quercetin-3-O-galactoside, kaempferol-3-O-glycoside, (-)-epicatechin and hypericin, was evaluated. The IC(50) resulted between 0.062 and 1 mg/ml.

Antiproliferative effects of essential oils and their major constituents in human renal adenocarcinoma and amelanotic melanoma cells

Abstract.  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 IC50 value of 104.90 µg/mL against C32, followed by activity of P. orientalis and P. asperula on the renal adenocarcinoma cell line (IC50 of 121.93 and 139.17 µg/mL, respectively). P. orientalis essential oil was also active against amelanotic melanoma with an IC50 of 330.04 µg/mL. Three identified terpenes, linalool, β‐caryophyllene and α‐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 α‐cedrol. Interestingly, β‐caryophyllene and linalool exhibited comparable IC50 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.

In vitro inhibitory activities of plants used in Lebanon traditional medicine against angiotensin converting enzyme (ACE) and digestive enzymes related to diabetes

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.

Phytochemical Analysis and in vitro Antiviral Activities of the Essential Oils of Seven Lebanon Species

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 IC50 value of 120 μg/ml and a selectivity index (SI) of 4.16. This oil was characterized by the presence of β‐ocimene, 1,8‐cineole, α‐pinene, and β‐pinene as the main constituents. J. oxycedrus ssp. oxycedrus oil, in which α‐pinene and β‐myrcene were the major constituents, revealed antiviral activity against HSV‐1 with an IC50 value of 200 μg/ml and a SI of 5.

Antiproliferative activity against human tumor cell lines and toxicity test on Mediterranean dietary plants.

Sixteen edible plants from Southern Italy were evaluated for their in vitro antiproliferative properties, using the sulforodamine B (SRB) assay, on four human cancer cell lines: breast cancer MCF-7, prostate cancer LNCaP, amelanotic melanoma C32 and renal adenocarcinoma ACHN. After 48 h of incubation the most antiproliferative plant extract was Cynara cardunculus ssp. cardunculus on C32 and ACHN cell lines with IC(50) of 21 and 18 microg/ml, respectively. Mentha aquatica showed a selective antiproliferative activity on breast cancer while significant activity was exerted by Cichorium intybus on melanoma. These species contained the highest amount of phenolics. The acute toxicity of the hydroalcohol extracts from all the plants were evaluated by using the Microtox acute toxicity test. This bacterial test measures the decrease in light emission from the marine luminescent Vibrio fischeri bacteria when exposed to organic extracts. This inhibition test was revealed to be highly sensitive, cost effective and easy to operate, requiring just 15 min to predict the sample toxicity. All the extracts analyzed resulted to give values very less than a limit of 20% value, demonstrating so an irrelevant toxicity for the human health. In contrast, Echium vulgare and Malva sylvestris showed bioluminescence inhibition values of 19.42% and 17.32%, respectively, just under the established limit.

Oldenlandia diffusa extracts exert antiproliferative and apoptotic effects on human breast cancer cells through ERα/Sp1-mediated p53 activation†‡

Breast cancer is the most frequent tumor and a major cause of death among women. Estrogens play a crucial role in breast tumor growth, which is the rationale for the use of hormonal antiestrogen therapies. Unfortunately, not all therapeutic modalities are efficacious and it is imperative to develop new effective antitumoral drugs. Oldenlandia diffusa (OD) is a well‐known medicinal plant used to prevent and treat many disorders, especially cancers. The aim of this study was to investigate the effects of OD extracts on breast cancer cell proliferation. We observed that OD extracts strongly inhibited anchorage‐dependent and ‐independent cell growth and induced apoptosis in estrogen receptor alpha (ERα)‐positive breast cancer cells, whereas proliferation and apoptotic responses of MCF‐10A normal breast epithelial cells were unaffected. Mechanistically, OD extracts enhance the tumor suppressor p53 expression as a result of an increased binding of ERα/Sp1 complex to the p53 promoter region. Finally, we isolated ursolic and oleanolic acids as the bioactive compounds able to upregulate p53 expression and inhibit breast cancer cell growth. These acids were greatly effective in reducing tamoxifen‐resistant growth of a derivative MCF‐7 breast cancer cell line resistant to the antiestrogen treatment. Our results evidence how OD, and its bioactive compounds, exert antiproliferative and apoptotic effects selectively in ERα‐positive breast cancer cells, highlighting the potential use of these herbal extracts as breast cancer preventive and/or therapeutic agents. J. Cell. Physiol. 227: 3363–3372, 2012.

Acetylcholinesterase and butyrylcholinesterase inhibition of ethanolic extract and monoterpenes from Pimpinella anisoides V Brig. (Apiaceae)

Ethanolic extract from the fruits of Pimpinella anisoides, an aromatic plant and a spice, exhibited activity against AChE and BChE, with IC(50) values of 227.5 and 362.1 microg/ml, respectively. The most abundant constituents of the extract were trans-anethole, (+)-limonene and (+)-sabinene. trans-Anethole exhibited the highest activity against AChE and BChE with IC(50) values of 134.7 and 209.6 microg/ml, respectively. The bicyclic monoterpene (+)-sabinene exhibited a promising activity against AChE (IC(50) of 176.5 microg/ml) and BChE (IC(50) of 218.6 microg/ml).