Search

The relationship between diet and health has drawn ever-growing interest. Bioactive peptides are involved in various biological activities, including control of cell proliferation, antimicrobial, antihypertensive, antioxidant, anticholesterolemic, and opioid activity. However, the peptide potential activity is quenched by some factors such as peptide digestion by proteases, cell membrane permeability, and clearance by kidney function. These obstacles to peptide bioavailability are increased for the nutraceutical use of peptides. The aim of this paper is to review the biochemical peculiarities that can improve the nutraceutical use of peptides. The involvement of amino acid sequence, N- and C-terminal groups, and internal chemical modifications of peptide are reported and discussed. In particular, the block of N-terminal group (N-acetylation, or presence of pyroGlu) or/and of C-terminal group (C-amidation), as well as the Ser/Thr/Tyr phosphorylation, prevent the peptide hydrolysis by digestive proteases and give them a better chance to enhance penetration of biological barriers. [ABSTRACT FROM AUTHOR]

Background: NeemAzal® (NA) is a quantified extract from seed kernels of neem, Azadirachta indica A.Juss. (Meliaceae), with a wide spectrum of biological properties, classically ascribed to its limonoid content. NA contains several azadirachtins (A to L), azadirachtin A (AzaA) being its main constituent. AzaA has been shown to inhibit microgamete formation of the rodent malaria parasite Plasmodium berghei, and NA was found to completely inhibit the transmission of Plasmodium berghei to Anopheles stephensi mosquitoes when administered to gametocytemic mice at a corresponding AzaA dose of 50mg/kg before exposure to mosquitoes.Purpose: The present study was aimed at i) assessing the pharmacodynamics and duration of action of NA and AzaA against P. berghei exflagellation in systemic circulation in mice and ii) elucidating the transmission blocking activity (TBA) of the main NA constituents.Study Design: The NA and AzaA pharmacodynamics on exflagellation were assessed through ex vivo exflagellation assays, while TBA of NA constituents was evaluated through in vitro ookinete development assay.Methods: Pharmacodynamics experiments: Peripheral blood from P. berghei infected BALB/c mice with circulating mature gametocytes, were treated i.p. with 50mg/kg and 100mg/kg pure AzaA and with NeemAzal® (Trifolio-M GmbH) at the corresponding AzaA concentrations. The effect magnitude and duration of action of compounds was estimated by counting exflagellation centers, formed by microgametocytes in process of releasing flagellated gametes, at various time points after treatment in ex vivo exflagellation tests. Ookinete Development Assay: The direct effects of NeemAzal® and AzaA on ookinete development were measured by fluorescence microscopy after incubation of gametocytemic blood with various concentrations of test substances in microplates for 24h.Results: The exflagellation tests revealed an half-life of NA anti-plasmodial compounds of up to 7h at a NA dose corresponding to 100mg/kg equivalent dose of AzaA. The ookinete development assay showed an increased activity of NA against early sporogonic stages compared to that of AzaA. The IC50 value determined for NA was 6.8µg/ml (CI95: 5.95-7.86), about half of the AzaA IC50 (12.4µg/ml; CI95: 11.0-14.04).Conclusion: The stronger activity of NA, when compared to AzaA, could not be explained by an additive or synergistic effect by other azadirachtins (B, D and I) present in NA. In fact, the addition of these compounds at 50µM concentration to AzaA did not evidence any decrease of the IC50 against early sporogonic stages to that obtained with AzaA alone. It is likely that other non-limonoid compounds present in NA may contribute to AzaA activity and enhanced pharmacodynamics against exflagellation both in vitro and in vivo. [ABSTRACT FROM AUTHOR]

A new triterpenoid saponin named bafouoside C 3- O - β - d -glucopyranosyl-(1 → 4)-[ β - d -galactopyranosyl-(1 → 2)]- β - d -glucuronopyranosyloleanolic acid 28- O - β - d -glucopyranosyl ester; (1), together with five known compounds 3- O - β - d -galactopyranosyl-(1 → 2)- β - d -glucuronopyranosyloleanolic acid (2), 23-hydroxyursolic acid (3), 28- O - α - l -rhamnopyranosyl-(1 → 4)- O - β - d -glucopyranosyl-(1 → 6)- O - β - d -glucopyranosyl-23-hydroxyursolic acid (4), 3- O - β - d -glucopyranosyl-23-hydroxyursolic acid (5), and 3- O - α - l -arabinopyranosyl-23-hydroxyursolic acid (6), were isolated from the roots of Cussonia bancoensis Aubrev. & Pellegr. Their structures were established on the basis of 1D- and 2D NMR data, mass spectrometry and chemical methods. The NMR data of the known compounds, as far as we know, are herein reported for the first time in CD 3 OD. Compound 3 exhibited a weak cytotoxic activity against MDA-MB 231 human breast adenocarcinoma, A375 human malignant melanoma, and HCT116 human colon carcinoma cell lines. [ABSTRACT FROM AUTHOR]

Highlights: [•] Three new steroidal saponins were isolated from the leaves of Cordyline fruticosa. [•] The new compounds were tested for cytotoxic and antimicrobial activity. [•] Two of the compounds showed cytotoxicity against three human tumour cell lines. [•] One compound showed a moderate antibacterial activity against Enterococcus faecalis. [Copyright &y& Elsevier]

Highlights: [•] The protozoan toxin climacostol exerts prooxidant activity in the presence of Cu(II) ions. [•] Climacostol binds to DNA. [•] The prooxidant activity can damage plasmid and eukaryotic DNA. [Copyright &y& Elsevier]

Abstract: Smyrnium olusatrum, better known as Alexanders or wild celery, is a biennal herb used in cuisine for many centuries by Romans in many dishes, where it has now been replaced by celery. In order to provide additional evidences so that this forgotten vegetable can be reconsidered in the human diet, as well as in pharmaceutics, the essential oils obtained from different parts and its main isolated furanosesquiterpenes were in vitro biologically assayed for antiproliferative activity on human tumor cell lines by MTT assay, for antioxidant potential by DPPH, ABTS and FRAP assays, and for antimicrobial activity by the agar disc diffusion method. The essential oils showed cytotoxic effects on tested human tumor cell lines, related to the furanosesquiterpenoid content; the IC50 values on colon carcinoma, glioblastoma, and breast adenocarcinoma cells were 8.51, 13.35, and 14.81μg/ml, respectively. Isofuranodiene and 1β-acetoxyfuranoeudesm-4(15)-ene resulted the most active constituents. The essential oils possessed also radical scavenging activity. [Copyright &y& Elsevier]

Abstract: Climacostol (5-(Z)-non-2-enyl-benzene-1,3-diol) is a natural toxin isolated from the freshwater ciliated protozoan Climacostomum virens and belongs to the group of resorcinolic lipids, compounds that show antimicrobial, antiparasitic and antitumor activities. We investigated the cytotoxic activity of the chemically synthesized toxin on: (1) human tumor squamous carcinoma A431 cells, (2) human promyelocytic leukaemia HL60 cells, and (3) human non-tumor endothelial EA.hy926 cells. The results showed that climacostol effectively inhibited the growth of tumor cell lines in a dose-dependent manner by inducing programmed cell death, with non-tumor cells proving significantly more resistant to the toxin. [Copyright &y& Elsevier]

Abstract: Angiotensin converting enzyme (ACE) is the dipeptidyl-carboxypeptidase of the renin–angiotensin system involved in the control of blood pressure and hydromineral metabolism. It converts angiotensin I to angiotensin II, the biologically active octapeptide. Angiotensin converting enzyme-like activity has been demonstrated in a wide range of vertebrates. The presence of ACE was investigated in tissues of two amphibian species, the frog Rana esculenta and the toad Xenopus laevis. ACE activities were determined by specific substrate hydrolysis in gut, gonads, lung, kidney, heart, liver, skin, erythrocytes, and muscle homogenates and plasma by means of high performance liquid chromatography. Significant ACE activity was found in gut, gonads, lung and kidney, while that in heart, liver, skin, erythrocytes, muscle, and plasma was very low. Testis of toad contained the highest ACE activity, while that in erythrocytes of male and female frogs was notable. [Copyright &y& Elsevier]

Gonad, lung, kidney and serum angiotensin converting enzyme (ACE) activities were determined by specific substrate hydrolysis in male and female Rana esculenta over 1 year. Ovary ACE activity showed the highest values among the different tissues, with a significant peak (223±52 nmol min−1 mg protein−1) in late winter-early spring. Testis ACE activity followed a significant seasonal cycle, increasing from September to peak in April (2.5±0.8 nmol min−1 mg protein−1) and then decreased in the post-reproductive period. Lung and kidney ACE activities were not correlated with the annual reproductive cycle phases. In serum a peak of activity was present in the post-reproductive period both in male and female frogs. The present data show a correlation between ACE and the annual reproductive cycle of R. esculenta. [Copyright &y& Elsevier]

The objectives of this study were to evaluate in horse testes the expression of kisspeptin (KiSS) and GnRH1 neuropeptides and their cognate receptors, KiSS1R and GnRH1R, as well as their action on testosterone, GnRH1, prostaglandin F2α (PGF2α), and PGE2 synthesis and cyclooxygenase 1 (COX1) and COX2 activity by Leydig cells in vitro. Testes were obtained from 9 sexually mature horses by surgical castration. Immunohistochemistry, evidenced the presence of KiSS, KiSS1R, GnRH, and GnRH1R in Leydig cells, whereas germinal and Sertoli cells were positive only for GnRH1. Transcripts for both neuropeptides and their cognate receptors were revealed in isolated Leydig cells by RT-PCR. Isolated and purified Leydig cells were in vitro cultured with agonists and antagonists of KiSS (KiSS-10 and KiSS-234, respectively) and GnRH1 (buserelin and antide, respectively). KiSS-10 and buserelin increased (P < 0.01) COX1 activity and testosterone and PGF2α basal secretion, while decreased (P < 0.01) that of PGE2. KiSS-10 and buserelin did not affect COX2 activity. GnRH1 basal production was increased (P < 0.01) by KiSS-10, but not by buserelin. Antide counteracted the KiSS and GnRH1 effects, whereas KiSS-234 influence only those of KiSS. Summarizing, the KiSS/GnRH1 system is present in horse Leydig cells and modulates their endocrine activity. In particular, the endocrine effects of KiSS are mediated by GnRH1, so suggesting that hypothalamic-like interaction between KiSS and GnRH1 occurs also in Leydig cells. • Kisspeptin/KISS1R and GnRH/GnRH1R systems are present in horse Leydig cells. • Kisspeptin (KiSS-10) and GnRH (buserelin) agonists stimulate Leydig cell testosterone production. • KiSS-10 stimulates Leydig cell GnRH1 production. • GnRH antagonist (antide) counteracts both KiSS-10 and buserelin effects, whereas KiSS antagonist counteracts only KiSS ones. • KiSS/KiSS1R and GnRH1/GnRH1R systems interact as a single system to affect the Leydig cell endocrine activity. [ABSTRACT FROM AUTHOR]

A new sulfated steroidal derivative (fruticogenin A: 1-sulfo-australigenin-3-sodium sulphate, 1) and three new steroidal saponins named fruticoside K (3-sulfo-spirostan-25(27)-ene-1 β ,3 β -diol-1- O -[α-L-rhamnopyranosyl-(1 → 4)- β -D-fucopyranoside], 2), fruticoside L (3-sulfo-spirostan-25(27)-ene-1 β ,3 β ,6α-triol-1- O -[ α -L-rhamnopyranosyl-(1 → 4)- β -D-fucopyranoside], 3) and fruticoside M (spirostan-25(27)-ene-1 β ,3α-diol-1- O -[ α -L-rhamnopyranosyl-(1 → 2)- α -L-rhamnopyranoside], 4) were isolated from the aerial parts of Cordyline fruticosa L. var. strawberries. Their structures were established on the basis of 1D and 2D NMR data, mass spectrometry and chemical methods. Compounds 2 and 4 exhibited weak cytotoxicity against melanoma (A375), breast adenocarcinoma (MDA-MB-231), and colon carcinoma (HCT116) human tumor cell lines. Unlabelled Image [ABSTRACT FROM AUTHOR]

The industrial extraction and further applications of isofuranodiene are limited because at room temperature it spontaneously converts to curzerene, a structurally less active isomer. This work definitively identified the structure of isofuranodiene in the solid state, showing the two methyl groups in syn position. In addition, two bioactive metal cations, namely, silver(I) and copper(II) ions, were used in the attempt to obtain the chemical stability of isofuranodiene: in the case of silver(I), a labile adduct was formed, while in the case of copper(II), a more stable 1:1 adduct was achieved. In the former, the presence of silver did not significantly affect the biological activities of isofuranodiene, while in the latter, the copper(II) coordination suppressed them. The biological activities of the isofuranodiene adducts were then evaluated as antiproliferative agents against human tumor cell lines (HCT116, MDA-MB 231, and T98G). In addition, for the first time, isofuranodiene was tested as an inhibitor of DHFR (DiHydroFolateReductase) from Escherichia coli . Anticancer activity was observed in the isofuranodiene with the AgCF 3 SO 3 adduct, in the tested cell lines, with IC 50 values ranging from 4.89 μM to 13.06 μM, while inhibition assays highlighted a Ki of 6.22 μM for isofuranodiene and of 0.17 μM for the related silver adduct. Docking studies indicated a binding mode score of − 6.83 Kcal/mol for isofuranodiene, and an energy value of − 11.82 Kcal/mol for methotrexate (a classic DHFR inhibitor). [ABSTRACT FROM AUTHOR]

Rosmarinus eriocalyx is an aromatic evergreen bush endemic to Algeria where it is used as a condiment to flavour soups and meat and as a traditional remedy. In the present work we have analyzed for the first time the phenolic composition of polar extracts obtained from stems, leaves and flowers of R. eriocalyx by HPLC, and determined the antioxidant and antimicrobial effects by DPPH, ABTS, FRAP, ORAC and agar disc diffusion methods, respectively. Results showed that ethanolic extracts of leaves and flowers are a rich source of phenolic compounds, mainly rosmarinic acid, carnosic acid and carnosol that are the main responsible for the noteworthy antioxidant activity observed in the assays. This study showed that R. eriocalyx might be a spice to be included in the European food additive list and used as a preservative agent besides R. officinalis . [ABSTRACT FROM AUTHOR]

Atractyloside, carboxyatractyloside, their aglycon atractyligenin, and several synthetic derivatives were tested and found to be active against a panel of human tumor cell lines. Atractyligenin was subjected to oxidation, bromination, and elimination reactions, obtaining several compounds. A singular skeleton was synthesized by chemical rearrangement starting from 3 β -bromo-2,15-diketoatractyligenin methyl ester. The synthesized compounds resulted active against all cell lines tested. In particular, 15-ketoatractyligenin methyl ester and 3 β -bromo-2,15-diketoatractyligenin methyl ester resulted the most active with IC 50 values of 0.427 and 0.723 μM against A375 melanoma cell line. Excellent results were also obtained against the colon cancer cell line CaCo2, with slightly lower antiproliferative activity. An interesting extension of the study should be to analyze the atractyligenin derivatives also as target for human melanoma and human colon cancer cells. [Display omitted] • Chemical modification of aglycon atractyligenin. • Favorskii-like rearrangement of the six membered ring to a five membered. • Atractyligenin derivatives were evaluated, in vitro , for antiproliferative activity. • Some IC 50 values were very similar to those of cisplatin. [ABSTRACT FROM AUTHOR]

In the present work we carried out a phytochemical and biological investigation on three Hypericum species, i.e. Hypericum reflexum , Hypericum canariense and Hypericum grandifolium , from the Canary Islands where they are traditionally used as diuretic, wound healing, vermifuge, sedative and antidepressive agents. The polar extracts of the top flowering aerial parts, prepared by Soxhlet apparatus using a methanol–acetone (1:1) extracting mixture, were analyzed by HPLC-DAD and HPLC-MS for the content of eight biomarkers such as hypericin, hyperforin, chlorogenic acid, rutin, hyperoside, isoquercitrin, quercitrin and quercetin, whereas the hydrodistilled essential oils were analyzed by GC-FID and GC-MS. The three Hypericum species had different results in both polar and volatile constituents, H . reflexum being the only one endowed with a small amount of naphtodianthrones (hypericin and pseudohypericin), and containing high levels of chlorogenic acid, rutin and volatile mono- and sesquiterpenes. After chemical characterization, all products were in vitro biologically assayed for antiproliferative activity on human tumor cell lines by MTT assay, for antioxidant potential by DPPH, ABTS and FRAP assays, and for antimicrobial activity by the agar disc diffusion and microdilution methods. Results revealed interesting bioactivities and differences between polar extracts and essential oils, with the former being endowed with significant antioxidant activity and the latter with comparable inhibition effects on the tumor cells (A375, MDA-MB 231 and HCT 116) to that of cisplatin. [ABSTRACT FROM AUTHOR]

Highlights: [•] Fruits of Xylopia parviflora are used to make traditional Cameroonian soups. [•] The essential oil composition was dominated by monoterpene hydrocarbons. [•] The oil strongly inhibited the growth of tumour cells MDA-MB 231 and HCT116. [•] The oil exhibited important anti-inflammatory activity on RAW 264.7 macrophages. [ABSTRACT FROM AUTHOR]

Abstract: Stachys alopecuros subsp. divulsa (Lamiaceae), a perennial herb endemic to central Italy growing on mountain pastures, was investigated for the first time for the content of secondary metabolites, for the micromorphology and histochemistry of glandular trichomes, and for the biological activity of the volatile oil, namely cytotoxic, antioxidant and antimicrobial. The plant showed the molecular pattern of iridoids, among which a new iridoid diglycoside (4′-O-β-d-galactopyranosyl-teuhircoside) was detected, together with a sterol glucoside and a phenylethanoid glycoside. The essential oil from the flowering aerial parts was characterized by a high proportion of sesquiterpene hydrocarbons (65.1%), with (E)-caryophyllene (33.2%) as the most abundant, while other main components were germacrene D (7.6%), α-humulene (6.4%) and the oxygenated cis-sesquisabinene hydrate (10.2%). Taken together, polar and apolar chemical profiles support the classification of the species within the section Betonica of the genus Stachys. Micromorphological study revealed three types of glandular hairs secreting different classes of compounds, with type A peltate hairs producing the bulk of the essential oil. MTT assay revealed the potential of the volatile oil in inhibiting A375, HCT116 and MDA-MB 231 tumor cells (IC50 values below 20μg/ml). [Copyright &y& Elsevier]

Abstract: The antineoplastic potential of a new stable mixed phosphine gold(I) complex containing tris(tert-butyl)phosphine (tBu3P) and bis(diphenylphosphino)ethene (dppet), namely [Au(tBu3P)(dppet)Cl], has been investigated in the human colon cancer HCT-116 cell line. The 31P NMR solution study, confirms the structural features observed in the solid state and, in addition, indicates partial formation of dinuclear cationic [Au(tBu3P)2]+ and [Au(dppet)2]+ species. The ionic character and strong Au–P bonds of this gold(I) species are similar to those of the most active antitumor gold compounds so far studied. The title compound was found to exhibit strong cytotoxicity, showing 85 fold greater toxicity than cisplatin (IC50 =0.45μM vs IC50 =39.16 for cisplatin at 24h) on the HCT-116 line. The cytotoxic effects were, at least partly, mediated by the induction of apoptotic cell death as evidenced by the sub-G1 cell accumulation, oligonucleosomal DNA fragmentation, caspase-3 activation and the release of cytochrome c from the mitochondria. The gold(I) compound showed little interaction with DNA measured through fluorescence quenching studies with calf thymus DNA. The inhibitory effect of the gold(I) compound on intracellular redox proteins has been also observed in pretreated HCT-116 cells. The compound was particularly effective in inhibiting thioredoxin reductase, that is likely responsible for the increased ROS production, and subsequent apoptosis induction via the mitochondrial pathway. [Copyright &y& Elsevier]

Abstract: Three new triterpenoid saponins, elucidated as 3-O-β-d-glucopyranosyloleanolic acid 28-O-β-d-xylopyranosyl-(1→4)-α-l-rhamnopyranosyl-(1→2)-β-d-xylopyranoside (parkioside A, 1), 3-O-[β-d-apifuranosyl-(1→3)-β-d-glucopyranosyl]oleanolic acid 28-O-[β-d-apifuranosyl-(1→3)-β-d-xylopyranosyl-(1→4)-[α-l-rhamnopyranosyl-(1→3)]-α-l-rhamnopyranosyl-(1→2)β-d-xylopyranoside (parkioside B, 2) and 3-O-β-d-glucuronopyranosyl-16α-hydroxyprotobassic acid 28-O-α-l-rhamnopyranosyl-(1→3)-β-d-xylopyranosyl-(1→4)-α-l-rhamnopyranosyl-(1→2)-β-d-xylopyranoside (parkioside C, 3), were isolated from the n-BuOH extract of the root bark of Butyrospermum parkii, along with the known 3-O-β-d-glucopyranosyloleanolic acid (androseptoside A). The structures of the isolated compounds were established on the basis of chemical and spectroscopic methods, mainly 1D and 2D NMR data and mass spectrometry. The new compounds were tested for both radical scavenging and cytotoxic activities. Compound 2 showed cytotoxic activity against A375 and T98G cell lines, with IC50 values of 2.74 and 2.93μM, respectively. Furthermore, it showed an antioxidant activity comparable to that of Trolox or butylated hydroxytoluene (BHT), used as controls, against 2,2-diphenyl-1-picryl hydrazyl (DPPH), 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS), oxygen and nitric oxide radicals. [Copyright &y& Elsevier]

Three saponins, including two dimeric triterpenoid glucosides possessing an unusual skeleton, ivorenosides A and B, and a monomeric triterpenoid saponin (ivorenoside C), together with the known sericoside, were isolated from the bark of Terminalia ivorensis. Their structures were established on the basis of 1D and 2D NMR data, chemical methods and tandem MS–MS spectrometry as a dimer of β-ᴅ-glucopyranosyl-18,19-seco-2α,3β,19,19,24-pentahydroxyolean-12-en-28-oate and β-ᴅ-glucopyranosyl-2α,3β,19α,24-tetrahydroxyolean-12-en-28-oate (ivorenoside A, 1), a dimer of β-ᴅ-glucopyranosyl-18,19-seco-24-carboxyl-2α,3β,19,19-tetrahydroxyolean-12-en-28-oate and β-ᴅ-glucopyranosyl-2α,3β,19α,24-tetrahydroxyolean-12-en-28-oate (ivorenoside B, 2) and β-ᴅ-glucopyranosyl-2α,3β,19β,24-tetrahydroxyolean-11-oxo-olean-12-en-28-oate (ivorenoside C, 3). Ivorenosides A and B are the first examples in nature of dimeric triterpenoid saponins with a 18,19-seco E ring of one of the two units. These isolated compounds were evaluated for their antioxidant properties and further for their cytotoxic activity against four human cancer cell lines. Ivorenoside B and C exhibited scavenging activity against DPPH and ABTS+ radicals with IC50 values comparable with that of the standard drug Trolox and ivorenoside A showed antiproliferative activity against MDA-MB-231 and HCT116 human cancer cell lines with IC50 values of 3.96 and 3.43 μM, respectively. [ABSTRACT FROM AUTHOR]

Abstract: Two triterpenoid saponins have been isolated from the seed kernels of Entada rheedii. Their structures have been established using 1D- and 2D-NMR and mass spectrometry as 3-O-β-d-xylopyranosyl-(1→3)-O-α-l-arabinopyranosyl-(1→6)-2-acetylamino-2-deoxy-β-d-glucopyranosylentagenic acid 28-O-β-apiofuranosyl-(1→3)-β-d-xylopyranosyl-(1→2)-β-d-glucopyranoside (Rheediinoside A, 1) and 3-O-β-d-glucopyranosyl-(1→3)-O-[β-d-xylopyranosyl-(1→3)-α-l-arabinopyranosyl-(1→6)]-2-acetylamino-2-deoxy-β-d-glucopyranosylentagenic acid 28-O-β-apiofuranosyl-(1→3)-β-d-xylopyranosyl-(1→2)-β-d-glucopyranoside (Rheediinoside B, 2). Compounds 1 and 2 were tested for their antiproliferative activity against T98G, A431, PC3 and B16-F1 cell lines, and further for their antioxidant properties. Moderate cytotoxic potency and antioxidant properties were found for these compounds whereas Rheediinoside B was in all assays more active than Rheediinoside A. [Copyright &y& Elsevier]

Abstract: Essential oil from flowers (FL) and vegetative parts (VP) of Achillea ligustica (Asteraceae), naturalized after cultivation in central Italy, was investigated by GC–FID and GC–MS. The most abundant components were linalool, viridiflorol, β-pinene, 1,8-cineole and terpinen-4-ol. The antioxidant assays (DPPH and ABTS radical scavenging assays, and β-carotene bleaching test) demonstrated a moderate activity of essential oils. The antimicrobial activity was evaluated by the broth micro-dilution method on 6 microbial strains and showed to be quite strong against the cariogenic Gram-positive Streptococcus mutans, suggesting that this essential oil could be a valid candidate for anti-cariogenic formulations. Moderate cytotoxic activity was observed in assays on four tumour cell lines by MTT assay. [Copyright &y& Elsevier]

Since time immemorial, the oleo-gum-resins of Ferula assa-foetida and F. gummosa are used in the traditional medical systems as well as in foodstuffs, perfumery and cosmetics. In the present study, we explored the insecticidal efficacy of the essential oils obtained from these oleo-gum-resins to widen their fields of industrial applications. The two essential oils were mainly composed of sulfides [sec-butyl (Z)-propenyl disulfide, sec-butyl (E)-propenyl disulfide, sec-butyl (Z)-propenyl trisulfide and sec-butyl (E)-propenyl trisulfide)] and monoterpenes (α-pinene, β-pinene and β-phellandrene), respectively, as determined by GC-MS analysis. The two essential oils were assayed for toxicity on a panel of insects, represented by species of public health relevance (Culex quinquefasciatus and Musca domestica), agricultural (Spodoptera littoralis) and stored-product pests (Prostephanus truncatus and Trogoderma granarium). The ecotoxicological effects of the essential oils were assessed on the aquatic microcrustacean Daphnia magna and the earthworm Eisenia fetida, as well as on human cells. Overall, the two essential oils were effective against important insect pests and vectors. On the other hand, they resulted cytotoxic to fibroblasts and non-target aquatic microcrustaceans. Thus, further insights are needed to determine the full spectrum of their eco-toxicological effects. Image 1 • The volatile oils from the oleo-gum-resins of Ferula assa-foetida and F. gummosa were studied. • Their efficacy against arthropod vectors, and agricultural and stored-product pests was evaluated. • The eco-toxicological effects on non-target organisms were measured. • The cytotoxicity on non-target vertebrate cells and on tumor cells was determined. [ABSTRACT FROM AUTHOR]