Phenylethanoid glycosides from Scutellaria galericulata

From the aerial parts of Scutellaria galericulata L., four phenylethanoid glycosides, 2-(4-hydroxyphenyl)-ethyl-(6-O-caffeoyl)-\beta -D-glucopyranoside (1), calceolarioside B (2), osmanthuside E (3) and martynoside (4), were isolated. The structure elucidations of the isolated compounds were performed by spectroscopic (UV, IR, ESI-MS, 1D- and 2D-NMR) methods. Compounds 1-4 demonstrated scavenging properties toward the 1,1-diphenyl-1-picrylhydrazyl (DPPH) radical in TLC autographic assays

Evaluation of biological activity of Turkish plants. Rapid screening for the antimicrobial, antioxidant, and acetylcholinesterase inhibitory potential by TLC bioautographic methods

Using thin-layer chromatography (TLC) bioautography, a total of 58 extracts from various organs (aerial parts, leaves, flowers, fruits, roots) of 16 Turkish plants were tested for their antibacterial, antifungal, acetylcholinesterase inhibitory, antioxidant, and radical scavenging activities. The hexane, CHCl3/CH2Cl2, water, and total MeOH extracts were used. No activity was observed against two Gram-negative bacteria (Escherichia coli and Pseudomonas aureginosa) and the yeast Candida albicans. However, 23 plant extracts, mostly the CHCl3/CH2Cl2 and H2O-solubles, inhibited the growth of all five Gram-positive bacteria tested, Micrococcus luteus, Bacillus subtilis, Bacillus cereus, Staphylococcus aureus, and Staphylococcus epidermidis. Of the active extracts, the CHCl3-soluble of the roots of Putoria calabrica (L. fil) DC (Rubiaceae) displayed the highest antibacterial potential. The majority of the CHCl3/CH2Cl2 crude extracts also appeared to inhibit acetylcholinesterase on TLC plates at 100 µg/spot concentration. Particularly active samples were the middle polarity extracts (CHCl3/CH2Cl2) of the leaves of Rhododendron smirnovii Trautv., R. ponticum L., and R. ungernii Trautv. (Ericaceae). β-Carotene, β-carotene/linoleic acid mixture, and 2,2-diphenyl-l-pieryhydrazyl (DPPH) solutions sprayed onto TLC plates were used for detecting antioxidant and radical scavenging properties of the crude extracts. Antioxidant and radical scavenging activities were found to be predominant in highly polar extracts. The water-solubles of all Rhododendron (Ericaceae) and Phlomis (Lamiaceae) species presented the most significant activity

Population modelling of Varroa jacobsoni Oud

To understand population dynamics of the mite Varrroa jacobsoni and to enable computer simulations, Fries et al. [Bee World 75 (1994) 5-28] incorporated available knowledge into a mite population model. In this paper, we update and extend this model by incorporating more recent data, in particular on mite invasion from bees into brood cells. By predicting invasion into and emergence from brood cells, the model proves to be useful to evaluate the effects of changes in model parameters on the mite population when the distribution of mites over bees and brood are important. The model predicts that a longer brood rearing period dramatically increases the mite population size and that a relatively larger number of drone brood cells leads to an increased population growth. As mite control treatments often only affect mites either in brood cells or on adult bees, the model can be used to evaluate their effectiveness and timing. The model indicates that changes in parameters that affect the reproductive success of the mites in brood cells have a large impact on the mite population. © Inra/DIB/AGIB/Elsevier, Pari

A Comparative Characterization of the HPA-MCM-48 Type Catalysts Produced by the Direct Hydrothermal and Room Temperature Synthesis Methods

MCM-48 type support materials synthesized by the direct hydrothermal synthesis (HTS) and room temperature synthesis (RTS) methods were incorporated with tungstophosphoric acid (TPA) in the range of 10–40 wt% by using a wet impregnation technique in methanol solutions. Resulting HPA-MCM-48 catalysts were characterized by the XRD, Nitrogen Physisorption, SEM, TEM, EDS, and FT-IR methods in order to determine the effects of different initial synthesis conditions on the catalyst properties. RTS samples were found to have better crystalline structures, higher BET surface areas, and higher BJH pore volumes than HTS samples. They also had slightly higher TPA incorporation, except for the 40 wt% samples, as evidenced by the EDS results. Keggin ion structure was preserved, for both methods, even at the highest acid loading of 40 wt%. It was concluded that the simpler and more economical RTS method was more successful than the HTS method for heteropoly acid incorporation into MCM-48 type materials

Inhibiting activities of the secondary metabolites of Phlomis brunneogaleata against parasitic protozoa and plasmodial enoyl-ACP reductase, a crucial enzyme in fatty acid biosynthesis

Anti-plasmodial activity-guided fractionation of Phlomis brunneogaleata (Lamiaceae) led to the isolation of two new metabolites, the iridoid glycoside, brunneogaleatoside and a new pyrrolidinium derivative (2S,4R)-2-carboxy-4-(E)-p-coumaroyloxy-1,1-dimethylpyrrolidinium inner salt [(2S,4R)-1,1-dimethyl-4-(E)-p-coumaroyloxyproline inner salt]. Moreover, a known iridoid glycoside, ipolamiide, six known phenylethanoid glycosides, verbascoside, isoverbascoside, forsythoside B, echinacoside, glucopyranosyl-(1→Gi-6)-martynoside and integrifolioside B, two flavone glycosides, luteolin 7-O-β-D-glucopyranoside (10) and chrysoeriol 7-O-β-D-glucopyranoside (11), a lignan glycoside liriodendrin, an acetophenone glycoside 4-hydroxyacetophenone 4-O-(6′-O-β-D-apiofuranosyl)-β-D-glucopyranoside and three caffeic acid esters, chlorogenic acid, 3-O-caffeoylquinic acid methyl ester and 5-O-caffeoylshikimic acid were isolated. The structures of the pure compounds were elucidated by means of spectroscopic methods (UV, IR, MS, 1D and 2D NMR, [α]D) and X-ray crystallography. Compounds 10 and 11 were determined to be the major anti-malarial principles of the crude extract (IC50 values of 2.4 and 5.9 μg/mL, respectively). They also exhibited significant leishmanicidal activity (IC50 = 1.1 and 4.1 μg/mL, respectively). The inhibitory potential of the pure metabolites against plasmodial enoyl-ACP reductase (FabI), which is the key regulator of type II fatty acid synthases (FAS-II) in P. falciparum, was also assessed. Compound 10 showed promising FabI inhibiting effect (IC50 = 10 μg/mL) and appears to be the first anti-malarial natural product targeting FabI of P. falciparum

New cut-off values for ferritin and soluble transferrin receptor for the assessment of iron deficiency in children in a high infection pressure area

Background: Due to the potential risk of iron supplementation in iron replete children, it is important to properly identify children who may require iron supplementation. However, assessment of the iron status has proven to be difficult, especially in children living in areas with high infection pressure (including malaria). Aims and Methods: Biochemical iron markers were compared to bone marrow iron findings in 381 Malawian children with severe anaemia. Results: Soluble transferrin receptor/log ferritin (TfR-F index), using a cut-off of 5.6, best predicted bone marrow iron stores deficiency (sensitivity 74%, specificity 73%, accuracy 73%). In order to improve the diagnostic accuracy of ferritin or sTfR as a stand-alone marker, the normal cut-off value needed to be increased by 810% and 83% respectively. Mean cell haemoglobin concentration (MCHC), using a cut-off of 32.1 g/dl, had a sensitivity of 67% and specificity of 64% for detecting iron stores deficiency. Conclusion: TfR-F index incorporated the high sensitivity of sTfR, a proxy for cellular iron need, and the high specificity of ferritin, a proxy for iron stores. In areas with a high infection pressure, the TfR-F index best predicted iron deficiency. However, in settings where diagnostic tests are limited, MCHC may be an acceptable alternative screening test

Liver cancer cells are sensitive to Lanatoside C induced cell death independent of their PTEN status

Background Hepatocellular carcinoma is the second deadliest cancer with limited treatment options. Loss of PTEN causes the P13K/Akt pathway to be hyperactive which contributes to cell survival and resistance to therapeutics in various cancers, including the liver cancer. Hence molecules targeting this pathway present good therapeutic strategies for liver cancer. Hypothesis It was previously reported that Cardiac glycosides possessed antitumor activity by inducing apoptosis of multiple cancer cells through oxidative stress. However, whether Cardiac glycoside Lanatoside C can induce oxidative stress in liver cancer cells and induce cell death both in vitro and in vivo remains unknown. Methods Cell viability was measured by SRB assay. Cell death analysis was investigated by propidium iodide staining with flow cytometry and PARP cleavage. DCFH-DA staining and cytometry were used for intracellular ROS measurement. Protein levels were analyzed by western blot analysis. Antitumor activity was investigated on mice xenografts in vivo. Results In this study, we found that Cardiac glycosides, particularly Lanatoside C from Digitalis ferruginea could significantly inhibit PTEN protein adequate Huh7 and PTEN deficient Mahlavu human liver cancer cell proliferation by the induction of apoptosis and G2/M arrest in the cells. Lanatoside C was further shown to induce oxidative stress and alter ERK and Akt pathways. Consequently, JNK1 activation resulted in extrinsic apoptotic pathway stimulation in both cells while JNK2 activation involved in the inhibition of cell survival only in PTEN deficient cells. Furthermore, nude mice xenografts followed by MRI showed that Lanatoside C caused a significant decrease in the tumor size. In this study apoptosis induction by Lanatoside C was characterized through ROS altered ERK and Akt pathways in both PTEN adequate epithelial and deficient mesenchymal liver cancer cells. Conclusion The results indicated that Lanatoside C could be contemplated in liver cancer therapeutics, particularly in PTEN deficient tumors. This is due to Lanatoside C's stress inducing action on ERK and Akt pathways through differential activation of JNK1 and JNK2 by GSK3β. © 2015 Elsevier GmbH. © 2016 Elsevier GmbH. All rights reserved

Secondary metabolites of Phlomis viscosa and their biological activities

Further phytochemical studies on the aerial parts of Phlomis viscosa (Lamiaceae) led to the isolation of 24 compounds: 3 iridoid glycosides, 10 phenylethanoid glycosides, a megastigmane glycoside and a hydroquinone glycoside, as well as 2 lignan glucosides and 7 neolignan glucosides, 1 of which is new (17b). Compound 17b was obtained as a minor component of an inseparable mixture (2:1) of 2 neolignan glucosides (17a/b), and characterized as 3',4-O-dimethylcedrusin 9-O-b -glucopyranoside. Full NMR data of the known 8-O-4' neolignan glucoside, erythro-1-(4-O-b-glucopyranosyl-3-methoxyphenyl)- 2-{2-methoxyl-4-[1-(E)-propene-3-ol]-phenoxyl}-propane-1,3-diol (18) are also reported. All isolated compounds were screened for cell growth inhibition versus 3 tumor cell lines (MCF7, NCI-H460, and SF-268) and several phenylethanoid glycosides were found to possess weak antitumoral activity. The phenylethanoid glycosides were also evaluated for their free radical (DPPH) scavenging, antibacterial and antifungal activities. The free radical (DPPH) scavenging activities of verbascoside (4), isoacteoside (5), forsythoside B (10), myricoside (13) and samioside (14) were found to be comparable to that of dl-a -tocopherol. Compounds 4, 5, 10 and 14 (MIC: 500 m g/mL) as well as Leucosceptoside A (8) and 13 (MIC:1000 m g/mL) showed very weak activity against Gram (+) bacteria

Improved method for assessing iron stores in the bone marrow

Background: Bone marrow iron microscopy has been the "gold standard'' method of assessing iron deficiency. However, the commonly used method of grading marrow iron remains highly subjective. Aim: To improve the bone marrow grading method by developing a detailed protocol that assesses iron in fragments, in macrophages around fragments and in erythroblasts. Methods: A descriptive study of marrow aspirates of 303 children (aged 6-60 months) with severe anaemia and 22 controls (children undergoing elective surgery) was conducted at hospitals in southern Malawi (2002-04). Results: Using an intensive marrow iron grading method, 22% and 39% of cases and controls had deficient iron stores, and 40% and 46% had functional iron deficiency, respectively. Further evaluation of the iron status classification by the intensive method showed that functional iron deficiency was associated with significantly increased C-reactive protein concentrations (126.7 (85.6) mg/l), and iron stores deficiency with significantly increased soluble transferrin receptor concentrations (21.7 (12.5) mg/ml). Conclusions: Iron assessment can be greatly improved by a more intense marrow examination. This provides a useful iron status classification which is of particular importance in areas where there is a high rate of inflammatory conditions