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Hibiscus sabdariffa L. is a tropical plant belonging to the Malvaceae family. In Kurdistan, the Autonomous Region of Iraq, water infusion of H. sabdariffa calyces is recommended for the treatment of hypotension and the common cold. Three distillation techniques: hydrodistillation (HD), steam distillation (SD), and solvent-free microwave-assisted extraction (SFME) have been compared to obtain the essential oils from calyces. The composition of the extracts was investigated by GC-FID and GC-MS. A total of 62 compounds have been identified, from which 55 components were found in HD distillates (95.75%), 37 components in SFME (96.06%), and 29 in SD (99.63%). Chemometric tools were applied to optimise and evidence the relation between distillation techniques and composition of the obtained essential oils as an investigation for the essential oils commercialisation approach of Hibiscus sabdariffa L. that have been done from a long time using conventional hydrodistillation in the local Herbal and Tea markets in Kurdistan.

The characterization of monoclonal antibodies (mAbs) requires laborious and time-consuming sample preparation steps before the liquid chromatography-mass spectrometry (LC-MS) analysis. Middle-up approaches entailing the use of specific proteases (papain, IdeS, etc.) emerged as practical and informative methods for mAb characterization. This work reports the development of immobilized enzyme reactors (IMERs) based on papain able to support mAb analytical characterization. Two monolithic IMERs were prepared by the covalent immobilization of papain on different supports, both functionalized via epoxy groups: a Chromolith® WP 300 Epoxy silica column from Merck KGaA and a polymerized high internal phase emulsion (polyHIPE) material synthesized by our research group. The two bioreactors were included in an in-flow system and characterized in terms of immobilization yield, kinetics, activity, and stability using Nα-benzoyl-L-arginine ethyl ester (BAEE) as a standard substrate. Moreover, the two bioreactors were tested toward a standard mAb, namely, rituximab (RTX). An on-line platform for mAb sample preparation and analysis with minimal operator manipulation was developed with both IMERs, allowing to reduce enzyme consumption and to improve repeatability compared to in-batch reactions. The site-specificity of papain was maintained after its immobilization on silica and polyHIPE monolithic supports, and the two IMERs were successfully applied to RTX digestion for its structural characterization by LC-MS. The main pros and cons of the two supports for the present application were described., Competing Interests: BP was employed by the company Merck KGaA. The remaining authors declare that the research was conducted in the absence of any commercial or financial relationships that could be construed as a potential conflict of interest., (Copyright © 2021 Rinaldi, Tengattini, Brusotti, Tripodo, Peters, Temporini, Massolini and Calleri.)

A combination of flash chromatography, solid phase extraction, high-performance liquid chromatography, and in vitro bioassays was used to isolate phytocomponents endowed with anticholinesterase activity in extract from Phyllanthus muellarianus. Phytocomponents responsible for the anti-cholinesterase activity of subfractions PMF1 and PMF4 were identified and re-assayed to confirm their activity. Magnoflorine was identified as an active phytocomponent from PMF1 while nitidine was isolated from PMF4. Magnoflorine was shown to be a selective inhibitor of human butyrylcholinesterase-hBChE (IC 50 = 131 ± 9 μM and IC 50 = 1120 ± 83 μM, for hBuChE and human acetylcholinesterase-hAChE, respectively), while nitidine showed comparable inhibitory potencies against both enzymes (IC 50 = 6.68 ± 0.13 μM and IC 50 = 5.31 ± 0.50 μM, for hBChE and hAChE, respectively). When compared with the commercial anti-Alzheimer drug galanthamine, nitidine was as potent as galanthamine against hAChE and one order of magnitude more potent against hBuChE. Furthermore, nitidine also showed significant, although weak, antiaggregating activity towards amyloid-β self-aggregation.

Hovenia dulcis Thunberg is an herbal plant, belonging to the Rhamnaceae family, widespread in west Asia, USA, Australia and New Zealand, but still almost unknown in Western countries. H. dulcis has been described to possess several pharmacological properties, such as antidiabetic, anticancer, antioxidant, anti-inflammatory and hepatoprotective, especially in the hangover treatment, validating its use as an herbal remedy in the Chinese Traditional Medicine. These biological properties are related to a variety of secondary metabolites synthesized by the different plant parts. Root, bark and leaves are rich of dammarane-type triterpene saponins; dihydrokaempferol, quercetin, 3,3',5',5,7-pentahydroflavone and dihydromyricetin are flavonoids isolated from the seeds; fruits contain mainly dihydroflavonols, such as dihydromyricetin (or ampelopsin) and hovenodulinol, and flavonols such as myricetin and gallocatechin; alkaloids were found in root, barks (frangulanin) and seeds (perlolyrin), and organic acids (vanillic and ferulic) in hot water extract from seeds. Finally, peduncles have plenty of polysaccharides which justify the use as a food supplement. The aim of this work is to review the whole scientific production, with special focus on the last decade, in order to update phytochemistry, biological activities, nutritional properties, toxicological aspect and regulatory classification of H. dulcis extracts for its use in the European Union.

The Wnt/ β -catenin signaling is a conserved pathway that has a crucial role in embryonic and adult life. Dysregulation of the Wnt/ β -catenin pathway has been associated with diseases including cancer, and components of the signaling have been proposed as innovative therapeutic targets, mainly for cancer therapy. The attention of the worldwide researchers paid to this issue is increasing, also in view of the therapeutic potential of these agents in diseases, such as Parkinson's disease (PD), for which no cure is existing today. Much evidence indicates that abnormal Wnt/ β -catenin signaling is involved in tumor immunology and the targeting of Wnt/ β -catenin pathway has been also proposed as an attractive strategy to potentiate cancer immunotherapy. During the last decade, several products, including naturally occurring dietary agents as well as a wide variety of products from plant sources, including curcumin, quercetin, berberin, and ginsenosides, have been identified as potent modulators of the Wnt/ β -catenin signaling and have gained interest as promising candidates for the development of chemopreventive or therapeutic drugs for cancer. In this review we make an overview of the nature-derived compounds reported to have antitumor activity by modulating the Wnt/ β -catenin signaling, also focusing on extraction methods, chemical features, and bio-activity assays used for the screening of these compounds., (© 2020 Chinese Pharmaceutical Association and Institute of Materia Medica, Chinese Academy of Medical Sciences. Production and hosting by Elsevier B.V.)

Drypetes klainei Pierre ex Pax is used in Cameroon by Baka people in the wound healing process and for the treatment of burns. In a previous paper we demonstrated the ability of both water (WE) and defatted methanol (DME) extracts to accelerate scratch wound closure in fibroblast cultures, thus validating the traditional use of D. klainey stem bark in the treatment of skin lesions. In this work we carried out a bioassay-guided fractionation of the most active DME, which exhibited in vitro efficacy in accelerating wound healing process, in order to isolate and identify the compound/s responsible for the assessed biological activity. HPLC was used for the metabolite profiling of DME and fractions (analytical) and for the isolation of the bioactive compound (semi-preparative). MS analyses and NMR spectroscopy were used for identifying the isolated compound. The abilities of treatments in accelerating wound healing were studied on murine fibroblasts in terms of cell viability and cell migration (scratch wound-healing assay). The results obtained allowed to unambiguously identify the isolated bioactive compound as nigracin, a known phenolic glycoside firstly isolated and characterized from bark and leaves of Populus nigra in 1967. However, this is the first time that nigracin is identified in the Drypetes genus and that a wound healing activity is demonstrated for this molecule. Specifically, we demonstrated that nigracin significantly stimulates fibroblast growth and improves cell motility and wound closure of fibroblast monolayer in a dose-dependent manner, without any toxicity at the concentrations tested, and is still active at very low doses. This makes the molecule particularly attractive as a possible candidate for developing new therapeutic options for wound care., (Copyright © 2020 Sferrazza, Corti, Andreola, Giovannini, Nicotera, Zonfrillo, Serra, Tengattini, Calleri, Brusotti, Pierimarchi and Serafino.)

The paper focuses on the preparation of polyacrylate based biomaterials designed as patches for dermal/transdermal drug delivery using materials obtained by the high internal phase emulsion (HIPE) technique. In particular, butyl acrylate and glycidyl methacrylate were selected, respectively, as backbone and functional monomer while two different crosslinkers, bifunctional or trifunctional, were used to form the covalent network. The influence of PEG on the main properties of the materials was also investigated. The obtained materials show a characteristic and interconnected internal structure as confirmed by SEM studies. By an industrial point of view, an interesting feature of this system is that it can be shaped as needed, in any form and thickness. The physiochemically characterized materials showed a tailorable curcumin (model of hydrophobic drugs) drug release, effective mechanical properties and cell viability and resulted neither pro nor anti-angiogenic as demonstrated in vivo by the chick embryo choriallantoic membrane (CAM) assay. Based on these results, the obtained polyHIPEs could be proposed as devices for dermal/transdermal drug delivery and/or for the direct application on wounded skin., (Copyright © 2019 Elsevier B.V. All rights reserved.)

Bellevalia saviczii is a medicinal plant used as anti-rheumatic and anti-inflammatory herbal remedy in Iraqi-Kurdistan. The aim of this study was to evaluate the anti-inflammatory activity of its extract and the isolated homoisoflavonoid ( Dracol ) by studying the Ca 2+ -dependent NF-kB pathway. Nuclear translocation of p65 NF-kB subunit, as parameter of NF-kB activation, was visualized in human leukemic monocytes by immunofluorescence and Western blot analyses, after cell treatment with B. saviczii root extract or Dracol followed by Lipopolysaccharide stimulation. In parallel, Ca 2+ signals responsible for NF-kB activation and levels of inflammatory cytokines were investigated. LPS-induced p65 translocation was evident in monocytes and both treatments, in particular that with Dracol , were able to counteract this activation. Intracellular Ca 2+ oscillations were halted and the cytokine release reduced. These results confirm the traditional anti-inflammatory efficacy of B. saviczii and identify one of the molecules in the extract which appears to be responsible of this action.

Affinity-based methods using immobilized proteins are important approaches for understanding the interactions between small molecules and biological targets. This review is intended to provide an overview of different affinity based separation methods that have been applied to the study of peroxisome proliferator activated receptors (PPARs). The screening of compound to increase screening rates for synthetic and natural ligands of PPAR are reported. Pros and cons of the approaches in ligand discovery initiatives are discussed., (Copyright © 2018 Elsevier Inc. All rights reserved.)

PPAR antagonists are ligands that bind their receptor with high affinity without transactivation activity. Recently, they have been demonstrated to maintain insulin-sensitizing and antidiabetic properties, and they serve as an alternative treatment for metabolic diseases. In this work, an affinity-based bioassay was found to be effective for selecting PPAR ligands from the dried extract of an African plant (Diospyros bipindensis). Among the ligands, we identified betulinic acid (BA), a compound already known for its anti-inflammatory, anti-tumour and antidiabetic properties, as a PPARγ and PPARα antagonist. Cell differentiation assays showed that BA inhibits adipogenesis and promotes osteogenesis; either down-regulates or does not affect the expression of a series of adipogenic markers; and up-regulates the expression of osteogenic markers. Moreover, BA increases basal glucose uptake in 3T3-L1 adipocytes. The crystal structure of the complex of BA with PPARγ sheds light, at the molecular level, on the mechanism by which BA antagonizes PPARγ, and indicates a unique binding mode of this antagonist type. The results of this study show that the natural compound BA could be an interesting and safe candidate for the treatment of type 2 diabetes and bone diseases.

Ethnopharmacological Relevance: Allanblackia floribunda Oliv. is one of the most commonly used medicinal plant in Cameroon. The stem bark of the plant is traditionally used for its aphrodisiac and antihypertensive properties., Aim of the Study: To validate the traditional uses of Allanblackia floribunda stem bark ethanol extract through the evaluation of their aphrodisiac and vasorelaxant properties., Materials and Methods: The extract's ability to increase sexual desire and the frequencies of erection (mount), intromission and prolonged latency of ejaculation were studied on adult male rats. The vasodilator effect was investigated using isolated rat aorta rings. Tests were conducted using fractions obtained by reverse phase column-chromatography (CC), after the acquisition of the HPLC fingerprint of the ethanol extract, resulted the most active in previous studies., Results: The CC allowed the isolation of five fractions whose aphrodisiac and vasodilator activities were tested and compared with those of the whole extract. Four compounds were identified and characterized, three of them, Fukugiside, Morelloflavone and Volkensiflavone, are secondary metabolites known to be in Allanblackia floribunda; the fourth, Spicataside, is a biflavonoid glycoside known to be present in the genus Garcinia but never found neither in Allanblackia floribunda nor in Allanblackia genus. The crude ethanolic extract (CEE) induced a relaxation on aorta rings with EC 50 =11±2μg/mL and Morelloflavone displayed a similar activity with EC 50 =42±6μg/mL; for all the other compounds only the vasodilation % at the maximum concentration assessable (90μg/mL) was determined: 30±8 (Fukugiside), 24±6 (Spicataside), 33±4 (Morelloflavone+Volkensiflavone), 47±1 (Volkensiflavone). Regarding the activity on male sexual behaviour, only CEE and Fukugiside showed activity in the 9 parameters evaluated., Conclusions: These results may support the traditional uses of Allanblackia floribunda as aphrodisiac plant with antihypertensive properties suggesting the phytocomplex as responsible for the claimed activity., (Copyright © 2016 Elsevier Ireland Ltd. All rights reserved.)

A fast and selective capillary electrophoresis method has been developed for the simultaneous determination of the antihypertensive drugs captopril and hydrochlorothiazide and their related impurities in a combined dosage form. Method development was carried out implementing each step of Quality by Design workflow, the new paradigm of quality outlined in International Conference on Harmonisation Guidelines. Captopril is characterized by the lack of a strong chromophore and contains a proline-similar moiety, which gives rise to the presence of interconverting cis-trans isomers and leads to the possible interference between electrophoretic migration and reaction of isomerization. The scouting phase was dedicated to the investigation of several operative modes in order to overcome detection and isomerization issues. The best performances were obtained with sodium cholate-based micellar electrokinetic chromatography with the addition of n-butanol and γ-cyclodextrin. Critical quality attributes were represented by the critical resolution values and by analysis time. Critical process parameters were defined as temperature, voltage, concentration and pH of borate buffer, concentration of sodium cholate, n-butanol and γ-cyclodextrin. Screening experimental design was applied for investigating knowledge space. Response surface methodology pointed out several significant interaction effects, and with Monte-Carlo simulations led to map out the design space at a selected probability level. Robustness testing was carried out and a control strategy based on system suitability tests was defined. The selected working conditions gave a complete separation of the analytes in less than three minutes. The method was validated and applied to the analysis of a real sample of coformulation tablets., (Copyright © 2016 Elsevier B.V. All rights reserved.)

Ethnopharmacological Relevance: Drypetes klainei Pierre ex Pax is used in Cameroon by Baka Pygmies in the wound healing process and for the treatment of burns., Aim of the Study: To validate the traditional use of D. klainei Pierre ex Pax stem bark extracts through the evaluation of their antimicrobial properties and their ability to improve wound healing process in fibroblast cell cultures., Materials and Methods: The antimicrobial properties of D. klainei extracts were evaluated against Staphylococcus aureus ATCC 6538, Streptococcus pyogenes ATCC 19615, Escherichia coli ATCC 10536, Candida albicans ATCC 10231, on the basis of the minimum inhibitory concentration (MIC) and the minimum bactericidal-fungicidal concentration (MBC-MFC) by the macrodilution method. The extracts abilities to accelerate wound healing were studied on murine and human fibroblasts in terms of cell viability and migration (scratch wound-healing assay)., Results: All the extracts were non-toxic against the selected microorganisms at the tested concentrations, and significantly improve wound healing process in vitro, compared to untreated controls. However, the defatted methanol extract was active at lower concentrations, compared to the water extract., Conclusions: The ability of both water and defatted methanol extracts to accelerate scratch wound closure in fibroblast cultures may support the traditional use of D. klainei stem bark in the treatment of skin lesions (such as burns) even if no antimicrobial activity was evidenced., (Copyright © 2015 Elsevier Ireland Ltd. All rights reserved.)

Phyllanthus muellerianus (Kuntze) Excell (family Euphorbiaceae) stem bark methanol extract inhibited the growth of Clostridium sporogenes and Streptococcus pyogenes, responsible for gas gangrene and suppurative and non suppurative diseases, respectively. After the HPLC fingerprint acquisition a bioguided fractionation of the defatted methanol extract allowed the isolation of six fractions whose activity was evaluated against the two pathogen bacteria. A further purification of the most active fraction afforded a pure compound responsible for the very interesting inhibitory activity against C. sporogenes and S. pyogenes (MIC 0.91 μM, MIC 3.64 μM). (1)H NMR and MS analytical techniques allowed the identification of the bioactive as Nitidine; this quaternary ammonium alkaloid was observed in the genus Phyllanthus for the first time. A study on Nitidine counter ion, performed using energy dispersive spectroscopy (EDS) coupled with scanning electron microscopy (SEM) was also carried out., (Copyright © 2014 Elsevier B.V. All rights reserved.)

The phytochemical research based on ethnopharmacology is considered an effective approach in the discovery of novel chemicals entities with potential as drug leads. Plants/plant extracts/decoctions, used by folklore traditions for treating several diseases, represent a source of chemical entities but no information are available on their nature. Starting from this viewpoint, the aim of this review is to address natural-products chemists to the choice of the best methodologies, which include the combination of extraction/sample preparation tools and analytical techniques, for isolating and characterizing bioactive secondary metabolites from plants, as potential lead compounds in the drug discovery process. The work is distributed according to the different steps involved in the ethnopharmacological approach (extraction, sample preparation, biological screening, etc.), discussing the analytical techniques employed for the isolation and identification of compound/s responsible for the biological activity claimed in the traditional use (separation, spectroscopic, hyphenated techniques, etc.). Particular emphasis will be on herbal medicines applications and developments achieved from 2010 up to date., (Copyright © 2013 Elsevier B.V. All rights reserved.)

The water maceration and methanolic extract of the stem barks of Diospyros bipindensis, which is a medicinal plant used in Cameroon by Baka pygmies, revealed a complex high-performance liquid chromatography (HPLC) profile primarily composed of coumarin and naphthoquinone glycosides. The methanolic and apolar extracts also exhibited significant antifungal activity on a TLC bioautography assay against Candida albicans. HPLC-microfractionation in 96-well plates combined with bioautography enabled the rapid localization of the antifungal compound that was identified by HPLC-PDA and HPLC-MS analysis as plumbagin. These on-line structural information were also used to dereplicate four known compounds. The isolation of the polar constituents from the methanolic extract enabled the identification of eleven other compounds also present in the traditional preparation, nine of which are reported for the first time. The structures of those compounds were elucidated by UV, NMR and HR-MS analysis., (Copyright © 2013 Elsevier Ltd. All rights reserved.)

Ethnopharmacological Relevance: Diospyros bipindensis (Gürke) stem bark is used in Cameroon by Baka Pygmies for the treatment of respiratory disorders., Aim of the Study: To assess the anti-inflammatory, antibacterial and antioxidant properties of constituents from the bark extracts through bioassay-guided fractionation., Materials and Methods: The anti-inflammatory activity of extracts, fractions and pure compounds was assessed through the inhibition of the pro-inflammatory mediator nuclear factor-kappa B (NF-κB) transcriptional activity and nitric oxide (NO) production. DPPH, ABTS and ORAC assays were used for determining the antioxidant properties. The activity against Streptococcus pneumoniae, Staphylococcus aureus, Streptococcus pyogenes, Escherichia coli and Klebsiella pneumoniae, was evaluated on the basis of the minimum inhibitory concentration (MIC) and the minimum bactericidal concentration (MBC) by the macrodilution method., Results: The water extract showed antimicrobial activity against S. pneumoniae (MIC: 300 μg/ml) and S. pyogenes (MIC: 300 μg/ml). The dichloromethane extract efficiently inhibited NF-κB transcriptional activity and NO production and exhibited significant antioxidant activity in the ORAC assay. An interesting activity was also found against S. pneumoniae (MIC: 200 μg/ml), S. aureus (MIC: 400 μg/ml) and S. pyogenes (MIC: 200 μg/ml). The phytochemical investigation of the dichloromethane extract afforded plumbagin, canaliculatin, ismailin, betulinic acid and 4-hydroxy-5-methyl-coumarin as the main constituents. Plumbagin and ismailin were found to be responsible for the main biological activities observed., Conclusions: These results may provide a rational support for the traditional use of Diospyros bipindensis stem bark in the treatment of respiratory disorders, since the anti-inflammatory, antimicrobial and antioxidant compounds isolated from the dichloromethane extract were also present in the traditional water extract., (Copyright © 2013 Elsevier Ireland Ltd. All rights reserved.)

The volatile fractions isolated from Prangos peucedanifolia FENZL leaves and flowers were investigated for their phytochemical composition and biological properties. Flower and leaf hydrodistillation afforded 3.14 and 0.49 g of yellowish oils in 1.25 and 0.41% yields, respectively, from dry vegetable materials. According to the GC-FID and GC/MS analyses, 36 (99.35% of the total oil composition) and 26 compounds (89.12%) were identified in the two oils, respectively. The major constituents in the flower volatile fraction were β-pinene (35.58%), α-pinene (22.13%), and β-phellandrene (12.54%), while m-cresol (50.38%) was the main constituent of the leaf volatile fraction. The antimicrobial activity was evaluated against several bacterial and fungal strains, on the basis of the minimum inhibitory concentration (MIC) by the micro- and macrodilution methods. The two volatile fractions showed moderate antifungal and antibacterial activities, especially against Trichophyton rubrum (MIC of 2×10(3) μg/ml), Streptococcus mutans, Streptococcus pyogenes, and Staphylococcus aureus (MIC≤1.9×10(3) μg/ml for all)., (Copyright © 2013 Verlag Helvetica Chimica Acta AG, Zürich.)

Ethnopharmacological Relevance: Phyllanthus muellerianus (Kuntze) Excel (family Euphorbiaceae) stem bark is used in Cameroon by Baka pygmies as a remedy for wound healing and tetanus., Aim of the Study: To characterize the chemical composition and to evaluate the antimicrobial properties of the essential oil of the plant., Materials and Methods: The essential oil was extracted from the stem bark by dynamic head space and by hydrodistillation and characterized by GC and GC-MS analyses. The antimicrobial activity was evaluated on the basis of the minimum inhibitory concentration (MIC) and the minimum bactericidal-fungicidal concentration (MBC-MFC) by the micro and macrodilution methods. The following bacteria and fungi were used: Clostridium sporogenes ATCC 3584, Staphylococcus aureus ATCC 6538, Streptococcus mutans ATCC 25175, Streptococcus pyogenes ATCC 19615, Escherichia coli ATCC 10536, Candida albicans ATCC 10231, Candida albicans LM 450, Trichophyton mentagrophytes LM 230, Trichophyton rubrum LM 237, Microsporum canis LM 324., Results: The hydrodistillation afforded 0.06% (dry weight basis) of pale yellow oil. Thirty-eight compounds representing 90.69% were identified. The major component (36.40%) was found to be (E)-isoelemicin, identified by comparison of its (1)H-NMR experimental data, with literature data. The oil showed good antibacterial activity against Clostridium Sporogenes, Streptococcus mutans and Streptococcus pyogenes with MIC ranging from 13.5 to 126 μg/ml. A weak antifungal activity (MIC 250 μg/ml) was found against Trichophyton rubrum, only., Conclusions: The antimicrobial activity and the chemical composition of Phyllanthus muellerianus stem bark essential oil are reported for the first time., (Copyright © 2012 Elsevier Ireland Ltd. All rights reserved.)

Introduction and Objectives: The Dizziness Handicap Inventory is a useful tool for quantifying self-perceived handicap in patients with vertigo, dizziness or unsteadiness and its impact on daily living activities. The Dizziness Handicap Inventory identifies functional, physical and emotional disorders related to balance disturbance. Our objective was to cross-culturally adapt the Peninsular Spanish version of the Dizziness Handicap Inventory for use in Argentina and validate the adapted Argentinian version., Methods: We included both healthy subjects and patients with vertigo, dizziness or unsteadiness, aged 18 to 85 years, native Spanish-speaking Argentinians. We introduced linguistic and cultural modifications to the Peninsular Spanish version to obtain the Argentinian one. This version was given twice to 108 patients, 24 to 72 h apart. Internal consistency, test-retest reliability and construct validity were assessed using a visual analogue scale, the Romberg test, the tandem Romberg test and the tandem gait test., Results: We found high internal consistency (α=0.87) and very high test-retest reliability for the total Dizziness Handicap Inventory score (intraclass correlation coefficient: 0.98) and its subscales. The total Dizziness Handicap Inventory and the functional subscale were found to correlate significantly with the Romberg and tandem Romberg tests. The emotional subscale showed a significant correlation with the Romberg test and the eyes-open tandem Romberg test (P<.05), Conclusions: The Argentinian version of the Dizziness Handicap Inventory proved to be a reliable and valid tool to quantify self-perceived handicap resulting from vertigo, dizziness or unsteadiness., (Copyright © 2011 Elsevier España, S.L. All rights reserved.)

Ethnopharmacological Relevance: The plants of the genus Phyllanthus (Euphorbiaceae) are widely distributed in most tropical and subtropical countries, and have long been used in folk medicine to treat several diseases. Particularly, Phyllanthus muellerianus (Kuntze) Excell, commonly called "mbolongo" in Cameroon, is used by pygmies baka as a remedy for tetanus and wound infections., Aim of the Study: To investigate the antimicrobial properties of Phyllanthus muellerianus (Kuntze) Excell (family Euphorbiaceae) stem bark used in Cameroon by baka pygmies as a remedy for wound healing and tetanus., Materials and Methods: Aqueous and methanol extracts with and without defatting treatment, were prepared and their activity against Clostridium sporogenes ATCC 3584, Staphylococcus aureus ATCC 6538, Streptococcus mutans ATCC 25175, Streptococcus pyogenes ATCC 19615, Escherichia coli ATCC 10536, Candida albicans ATCC 10231, was evaluated on the basis of the minimum inhibitory concentration (MIC) and the minimum bactericidal-fungicidal concentration (MBC-MFC) by the macrodilution method., Results: Water extract showed a weak activity against Clostridium sporogenes (MIC 900 μg/mL) and resulted inactive at the tested concentrations against all the other microorganisms. The defatted methanol extract, inactive against Staphylococcus aureus, Escherichia coli, Candida albicans, exhibited a very interesting activity against Clostridium sporogenes and Streptococcus pyogenes (MIC 100 μg/mL and 300 μg/mL, respectively), which seems to validate the use of this plant in pygmies traditional medicine for the treatment of tetanus and wound infections. The activity found against Streptococcus mutans (300 μg/mL), aetiological agent of caries, may suggest a possible use of this plant as natural remedy to prevent dental diseases., Conclusions: The activity against streptococci and Clostridium sporogenes ATCC 3584, showed by stem bark extracts of Phyllanthus muellerianus, traditionally used by baka pygmies to treat wound infections and tetanus, is reported for the first time., (Copyright © 2011 Elsevier Ireland Ltd. All rights reserved.)

Euphorbiaceae barks are known to contain an appreciable amount of polyphenolic compounds responsible for several biological activities. Preliminary extraction from Bridelia grandis stem bark afforded high content of polyphenols, determined by spectrophotometric methods such as Folin-Ciocalteu (for total phenols, TP) and n-butanol-HCl (for condensed tannins, CT). A preliminary Plackett-Burman screening design was used to identify the key factors that influence the TP and CT extraction. Between all the variables known to influence the extraction from vegetable matrixes, six were selected; maceration was chosen as traditional extraction methodology. To investigate the effect of solvents and extraction method, methanol, acetone 70% (v/v in water), centrifugation and ultrasound were chosen. A full factorial design 2(3) was applied to optimize the extraction procedure. The responses were obtained analyzing the extracts for their TP and CT contents determined by the above-mentioned spectrophotometric methods. The results confirm that, within the explored domain, the optimum solvent is methanol and the optimum method is one-cycle centrifugation. Finally, it was also compared with the effect of maceration on the considered responses. It has never given results better than centrifugation, whereas in the case of CT it represents an advantage to employ a three-cycle centrifugation instead of one.

Approximately 60 species of Bridelia, (Phyllanthaceae) are found throughout tropical and subtropical regions of the world, mainly in Africa and Asia. Several Bridelia species are used in popular medicines as antiamebic, antianemic, antibacterial, anticonvulsant, anti-diabetic, antidiarrhoeal, antihelmintic, anti-inflammatory, antimalarial, antinociceptive, antiviral, hypoglycemic and for abdominal pain, cardiovascular, gynecological and sexual diseases. The present paper reviews the traditional usage, the biological activities and the correlated chemical compounds of Bridelia species with emphasis on the validation of the ethnopharmacological uses. The findings in some Bridelia species of, for example, gallocatechin-(4'-O-7)-epigallocatechin (1), quercetin (2), myricetin glycosides (5-6), bridelone (11), bridelonine (12), isoflavone may justify the uses of these species against pains in African and Asian traditional medicines.

Aim of the Study: Bridelia grandis (Pierre ex Hutch) (Euphorbiaceae) is a medicinal plant traditionally used in Cameroon by pygmies Baka as a remedy for oral cavity affection. Bioassay-guided stem bark extracts were investigated for their in vitro antimicrobial properties as well as their phytochemical constituents., Materials and Methods: The first extraction was carried out according to the traditional use. Further extractions were carried out with solvents of different polarity such as methanol (MeOH), ethyl acetate (EtOAc) and mixtures of MeOH-H2O. The antimicrobial activity of the extracts against oral Streptococci was evaluated on the basis of the minimum inhibitory concentration (MIC) and the minimum bactericidal concentration (MBC) by the macrodilution method; the bacterial surface hydrophobicity was also evaluated., Results: Water, methanol and mixtures methanol-water extracts, exhibited antibacterial activity with MIC between 0.5 and 2mg/ml justifying the traditional use of Bridelia grandis stem bark for oral cavity affection. Preliminary phytochemical analysis was performed on the most active extract (methanol) using appropriate tests and well established analytical screening methods, such as TLC and RP-HPLC/DAD., Conclusions: The data obtained indicate that tannins constitute the chemical family responsible for the biological activity.

The chiral recognition mechanism of Penicillin G Acylase (PGA) was investigated with a set of 18 new chiral acidic compounds. A series of 2-aryloxyalkyl- and 2-arylalkyl-2-aryloxyacetic acids in which the absolute configuration has been reported to exert a strong influence on pharmacological activity, were synthesized and analysed on PGA-based chiral stationary phase (CSP) and 11 racemates were completely resolved with a mobile phase composed of 50 mM phosphate buffer (pH 7.0). The influence of structural variations of analytes on retention and enantioselectivity was investigated by application of molecular modelling studies. Docking experiments were also carried out to rationalize the observed enantioselective behaviour. The computation approach revealed to be helpful in elucidating the molecular basis of the enantioselectivity observed on PGA-CSP.

The development and characterization of an anti-aflatoxin B1 (anti-AFB1) immunoaffinity monolithic disk is reported. Polyclonal anti-AFB1 was covalently immobilized in batch on an epoxy-activated monolithic Convective Interaction Media (CIM) disk (12 mm x 3 mm i.d.) by a one-step reaction via epoxy groups of the polymer surface. 0.96 mg of antibody were immobilized and the binding capacity of the CIM disk was determined by frontal analysis. The CIM disk was coupled through a switching valve to a reversed-phase column, namely Chromolith Performance RP-18e. A fully automated HPLC method with fluorescence detection for the determination of aflatoxin B1 in aqueous solution was developed. The total analysis time with the integrated system is 46 min and the retention time of AFB1 is approximately 29 min. The binding capacity of the immunoaffinity disk was evaluated in terms of linearity, precision and accuracy of the extraction procedure. The immunoaffinity support was stable after repeated runs.

S-phenylmercapturic acid (PMA) is one specific urinary biomarker of low-level benzene exposure. It is used for biological monitoring of benzene-exposed workers in the petrochemical industry and normally ranges from non-measurable to 10 microg/l levels in non-exposed non-smoking subjects. Benzene-exposure caused by workplace or lifestyle sources is frequently accompanied by toluene exposure, which can cause the occurrence of high levels (from 10 mg/l to more than 2000 mg/l) of hippuric acid (HA) in urine. Both solvents are toxic, and benzene is classified as a human carcinogen. The biological monitoring of benzene and toluene is therefore required for preventive care of exposed workers health. In this study a GC-MS method was adopted for measuring urinary PMA, which involved liquid-liquid extraction (LLE) with ethyl acetate from acidified urine and esterification with 0.5 N hydrochloric acid in methanol. The method evidenced a GC effect in a conventional HP-5 (30 m x 0.25 mm i.d., 0.25 microm film-thickness) methyl-phenylsilicone capillary column produced by HA on PMA. The results demonstrate that HA at concentrations as low as 250 mg/l can delay the elution of PMA and labelled internal standard from the column. The recognition and discussion of this particular GC phase soaking effect may be of help for those who are occupied in the determination of PMA and of urinary acidic metabolites by GC.

In the present paper, we report on the synthesis and antinociceptive activity of a new series of N-methyl-arylpyrrolidinols that we designed for a rational structure-activity relationship (SAR) study. The antinociceptive properties were investigated in vivo by the hot plate and formalin tests in mice and control on the locomotory activity was also monitored by the rota rod test. With this aim, the evaluation of the lipophilicity of all compounds was performed by the Daylight computational method in order to better understand the SAR. Interesting properties were proven for the compounds of the entire series.

Since the early days of combinatorial chemistry solid-phase organic synthesis has been the method of choice for the production of large libraries. Solution-phase synthesis is again gaining importance especially for the synthesis of parallel arrays of smaller, focussed libraries containing single compounds with high degrees of purity. In the field of solution-phase library generation, the use of solid-supported reagents, catalysts and scavengers is emerging as a leading strategy, combining the advantages of both solid-phase organic synthesis (e.g. allowing the employment of an excess of reagent without the need for additional purification steps) and solution-phase chemistry (e.g. the ease of monitoring the progress of the reactions by applying LC-MS, TLC or standard NMR techniques). An account of some of the most recent advances in this area of research will be presented.