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This mini review describes the research between 1962 and 2019 on ethnobotany, chemistry and pharmacology of Harungana madagascariensis (Hypericaceae), the unique plant species in the genus Harungana. The plant is mainly distributed in Africa and Europe, where it has been used in the traditional medicine to cure several diseases. The first chemical investigation of H. madagascariensis genus took place earlier in 1962 with the isolation of harunganin whose the structure was characterized by X-ray. Several works have been done over the last 57 years on leaves, bark, roots and branches of the plant and as result, 42 secondary metabolites belonging to numerous classes of compounds including anthranoids, anthraquinones, xanthones, triterpenoids, flavonoids, steroids and alkaloids have been isolated and are presented herein together with some derivatives obtained from chemical transformations including thermal rearrangement and allylation. The anthranoids reported from natural sources represent almost 49 % of the total secondary metabolites obtained from the genus and display the most potent biological activities. Along with anthraquinones, they constitute the chemo markers of Harungana. The extracts and compounds from the plant have been evaluated for their potencies in antimicrobial, anti-protozoan, anti-sickling, anti-inflammatory, antioxidant, enzyme inhibition or cytotoxic activities. The results support the uses of H. madagascariensis in folk medicine and provide further evidence in new drugs discovery.

BACKGROUND & AIMS: Oral iron absorption is hampered in obese and bariatric patients, especially after Roux-en-Y gastric bypass (RYGB). As a result, iron deficiency, which is common in both patient groups, can be difficult to treat by oral supplements, often necessitating a switch to parenteral administration. The aim of this study was to find possible predictors of the extent of absorption of an effervescent iron gluconate oral supplement, which enables to pre-emptively identify those patients in which oral supplementation is likely to fail. METHODS: The pharmacokinetic properties of 695 mg effervescent iron gluconate (80 mg Fe2+) were assessed in 13 obese patients (female = 10; mean age ± SD: 45.2 ± 12.5years) pre- and six months post-RYGB by measuring serum iron concentrations during 24 hours and by calculating the adjusted for baseline AUC0-24h, Cmax and Tmax. A multivariate regression analysis was performed to investigate the effect of hepcidin concentration, iron and hematologic indices, personal and anthropometric characteristics on iron absorption. Subsequently, Receiver Operating Characteristic (ROC) curves were used to propose the cut-off value for hepcidin concentrations above which obese patients are unlikely to benefit from oral iron supplementation. Data are expressed as mean ± SD. RESULTS: Low iron status persisted after surgery as there was no significant difference observed in TSAT (17.3 ± 5.2 vs. 20.2 ± 6.6%), ferritin (91.8 ± 68.6 vs. 136.2 ± 176.9 μg/L) and hepcidin concentration (32.0 ± 30.1 vs. 28.3 ± 21.3 ng/mL) after RYGB. The absorption of effervescent iron gluconate was similar pre- and post-RYGB [AUC0-24h,pre-RYGB: 28.6 ± 10.8 μg/dL*h; AUC0-24h,post-RYGB: 27.5 ± 9.11 μg/dL*h (P = 0.84)]. Post-RYGB, iron AUC0-24h showed a strong negative correlation with both hepcidin concentrations and TSAT (R=-0.51; P = 0.08 and R=-0.81; P = 0.001), respectively. Pre-RYGB, there was a clear trend for the same negative correlations for hepcidin concentrations and TSAT (R=-0.47; P = 0.11 ;R=-0.41; P = 0.16), respectively. Taking pre-and post-RYGB data together, the negative correlations were confirmed for hepcidin concentrations and TSAT (R=-0.54; P = 0.004; R=-0.60; P = 0.001), respectively. The AUCROC = 0.87 (95%CI 0.71; 1.00) showed an optimal sensitivity/specificity cut-off at hepcidin concentrations of 26.8 ng/mL. CONCLUSIONS: The iron AUC0-24h showed a negative correlation with the hepcidin concentration and TSAT of obese patients, in particular post-RYGB. Therefore, our data support the use of hepcidin concentration and TSAT to distinguish potential responders from non-responders for iron supplementation particularly post-RYGB. Additionally, this study showed that the pharmacokinetic properties of iron gluconate from an effervescent tablet were unaffected by RYGB-surgery. ispartof: JOURNAL OF TRACE ELEMENTS IN MEDICINE AND BIOLOGY vol:52 pages:68-73 ispartof: location:RUSSIA, St Petersburg status: published

Two alchornoic acid derivatives, deepoxyalchornoic acid ( 1 ) and bisalchornoicester ( 2 ), together with six known compounds, alchornoic acid ( 3 ), gallic acid, 4- O -methylgallic acid, shikimic acid, kaempferol-3- O -galactoside and 2,3-dihydroxypropyl octacosanoate were isolated from a dichloromethane/methanol-soluble extract of the ripe fruits of the Cameroonian medicinal plant Alchornea cordifolia . The structures of the new fatty acid derivatives were elucidated by interpretation of their HRESIMS, 1D and 2D NMR spectroscopic data and by comparison with those reported in the literature. Some of the isolated compounds demonstrated inhibition activity against the microbial strains Escherichia coli, Klebsiella pneumoniae and Citrobacter braakii .

The chemical investigation of the whole plant of Indigofera spicata Forsk (Fabaceae), a medicinal plant from Cameroon, resulted in the isolation of a new benzofuran, named spibenzofuran (1a), together with ten known secondary metabolites including one benzofuran (2), one flavonoid (3), one saponin (6), two triterpenes (4 and 5), two steroids (8 and 11), one phthalate (7) and two fatty acids (9 and 10). All these compounds have been isolated for the first time from this plant. The structures of the isolated compounds were established by spectroscopic analysis including HR-ESI-MS, 1D and 2D NMR and by comparison of our data with the reported data. The isolated compounds might be considered as the chemophenetic markers of this species, and antibacterial and urease inhibitory activities of some isolated compounds were assessed.

Conducting polymer nanoparticles (CPNPs), composed of the conducting polymer poly[2-methoxy-5-(2-ethylhexyl-oxy)-p-phenylenevinylene] (MEH-PPV) were studied for applications in biophotonics and therapeutics. The extent of cellular uptake, cytotoxicity, and effectiveness of these nanoparticles in photodynamic therapy (PDT) was investigated for four cell lines, namely TE-71, MDA-MB-231, A549 and OVCAR3. Confocal fluorescence imaging and flow cytometry show that CPNPs are taken up only in limited quantities by TE-71, while they are taken up extensively by the cancer cell lines. The uptake among the cancer cell lines was observed to vary with cell line, with CPNPs uptake increasing from MDA-MB-231 to A549 to OVCAR3. Fluorescence imaging experiments show that the CPNPs have high brightness and appear stable in the intracellular environment. No cytotoxicity of non-photoactivated CPNPs (in dark) was observed from MTT assay. After completion of PDT, the quantitative data on cell viability suggest that cell death scales across the cell lines with CPNP uptake, is light dose dependent, and is complete for OVCAR3. In addition, for OVCAR3 apoptotic cell death is observed after PDT. The reported work illustrates the potential of the intrinsically fluorescent and photoactivateable CPNPs for application in biophotonics and therapeutics.

This article is part of a Special Issue “Puberty and Adolescence”. The onset of reproduction is preceded by a host of organismal adjustments and transformations, involving morphological, physiological, and behavioral changes. In highly social mammals, including humans and most nonhuman primates, the timing and nature of maturational processes are affected by the animal's social milieu as well as its ecology. Here, we review a diverse set of findings on how maturation unfolds in wild baboons in the Amboseli basin of southern Kenya, and we place these findings in the context of other reports of maturational processes in primates and other mammals. First, we describe the series of events and processes that signal maturation in female and male baboons. Sex differences in age at both sexual maturity and first reproduction documented for this species are consistent with expectations of life history theory; males mature later than females and exhibit an adolescent growth spurt that is absent or minimal in females. Second, we summarize what we know about sources of variance in the timing of maturational processes including natal dispersal. In Amboseli, individuals in a food-enhanced group mature earlier than their wild-feeding counterparts, and offspring of high-ranking females mature earlier than offspring of low-ranking females. We also report on how genetic admixture, which occurs in Amboseli between two closely related baboon taxa, affects individual maturation schedules.

In mammals, maternal care is essential for offspring survival, yet individual differences in this care can dramatically affect offspring growth and development. Few studies have, however, investigated the sources, magnitude and consequences of naturally occurring interindividual variation in maternal care during the neonatal period. In this study, we examine several hormonal and nonhormonal predictors of naturally occurring variation in the mothereneonate relationship during the first 8 weeks of infancy in 34 wild baboon (Papio cynocephalus) mothereinfant dyads in Amboseli, Kenya. We use data on physical contact and suckling patterns to assess the quality of the mothereneonate relationship and to evaluate the extent to which variation in this relationship is predictable from perinatal ovarian steroids (i.e. faecal oestrogen and progesterone metabolites), previous infant care experience, maternal dominance rank and offspring sex. We found that newborn infants of more experienced mothers initiated higher rates of changes in mothereinfant contact than newborns of less experienced mothers. However, at each level of maternal experience, newborn males initiated higher rates of changes in mothereinfant contact than newborn females. Moreover, we found evidence suggesting that variation in suckling activity among daughters (but not sons) was predictable from maternal dominance rank and faecal oestrogen (fE) concentrations before birth. To our knowledge, our study provides the first evidence of (1) the influence of cumulative maternal experience on the mothereinfant relationship and (2) the emergence of sex differences in the mothereinfant relationship during the neonatal period in wild primates. Our results suggest that the well-documented sex differences in life history, behaviour and ecology in primates (and other social mammals) may originate very early in life. 2012 The Association for the Study of Animal Behaviour. Published by Elsevier Ltd. All rights reserved. For vertebrates, mammalian newborns are unusually dependent on their mothers for nourishment, transport, protection and support (Clutton-Brock 1991). Although offspring eventually transition from complete reliance on their mothers to nutritional, locomotor and social independence, the timing of these events can vary widely across individuals of the same species (Clutton-Brock 1991). Despite the critical importance of the neonatal period in the life of each individual, few studies have investigated the sources, magnitude and consequences of interindividual variation in the mothereoffspring relationship during the neonatal period in wild mammals (Altmann 1980; Bales et al. 2002). In this study, we

We report the fabrication and characterization of composite nanoparticles consisting of a conducting polymer, poly-3-hexylthiophene (P3HT), doped with varying amounts of [6,6]-phenyl C61-butyric acid methyl ester (PCBM), a material blend that is commonly applied in bulk heterojunction organic photovoltaic devices (OPVs). Single particle spectroscopy (SPS) studies, where nanoparticles are studied one particle at a time, reveal that these nanoparticles have spectroscopic characteristics consistent with the existence of two types of crystalline nanodomains, one with a higher energy emission at 660 nm and one with a lower energy emission at 720 nm. In addition, the occurrence of emission at lower peak energy increases with increasing PCBM doping levels, and the intensity of the lower energy peak emission increases with respect to the higher energy peak emission as well. These data reveal a PCBM concentration dependent formation of two types of P3HT crystalline nanodomains in P3HT/PCBM composite nanoparticles, where the lower energy crystal structure becomes more favored with higher PCBM concentration. This work provides a molecular scale insight in the correlation between changes in morphology of conjugated polymer materials with different weight percentages of fullerene dopants.

We report the study of the photoluminescence properties of composite conjugated polymer (MEH-PPV)/fullerene (PCBM) nanoparticles as a function of PCBM doping level. The emission properties of individual nanoparticles were studied by Single Particle Spectroscopy (SPS), and distinct changes in vibronic structure with nanoparticle composition were observed. These changes are found to be due to the presence of domains in the nanoparticles with two distinct types of optical signatures, one with molecular and one with aggregate character, for which the abundance and morphology is found to change with PCBM doping levels. Interestingly, highly delocalized structures with a large extent of exciton migration are formed at low PCBM doping levels, while at high PCBM doping levels the exciton collapses into highly localized structures. Furthermore, at very high doping levels phase separation within the MEH-PPV/PCBM nanoparticles is found, even though the reported nanoparticles are only a few tens of nanometers in diameter.

Minor changes in processing conditions and composition of blended conjugated polymer materials have led to sometimes unpredictable properties of resulting plastic optoelectronic devices due to the complex morphology of conjugated polymer materials. We report a Single Particle Spectroscopy study of composite poly-(3-hexylthiophene) (P3HT)/1-(3-Methoxycarbonylpropyl)-1-phenyl-[6.6]C 61 (PCBM) nanoparticles fabricated with varying doping levels of PCBM to investigate changes in morphology of P3HT with respect to blend composition. We find that this material system consists of crystalline nanodomains with two distinct morphologies that have characteristic optical signatures, and that exhibit a change in their relative abundance with changing PCBM dopant concentration in favor of the more densely packed crystal structure with higher PCBM concentrations.

The preparation and characterization of composite MEH-PPV/PCBM nanoparticles with doping levels up to 75 wt% PCBM is reported. These nanoparticles represent structures in between single molecules and bulk that allow for a detailed investigation of the role of nanostructure on the properties of the corresponding functional materials. Combining this material system with single particle spectroscopy studies reveals molecular scale information on the extent to which variations in polymer chain folding and interactions between polymer chains and fullerenes affect material morphology and photophysical properties. Key observations are that the single particle ensemble spectra shift with respect to each other depending on PCBM doping levels, and that the vibronic structure of the single particle ensemble spectra changes with PCBM doping levels. These observations are indicative of a reduction in conducting polymer conjugation length and interchain interactions due to steric effects caused by the presence of PCBM that result in reduced exciton transport.

Maternal care is the most significant measure of successful adaptation among female mammals. Understanding the predictors of individual differences in offspring care is a major objective of mammalian reproductive biology. Recent studies suggest that differences in caregiving motivation may be associated with variation in glucocorticoid (GC) hormones in new mothers. Despite these intriguing reports, questions remain about the stability of this association during a period of rapid change in both behaviour and physiology, about whether this relationship is dependent on other nonhormonal variables and about the generality of this pattern across species and in wild populations. Glucocorticoids modulate animals’ responses to ongoing stressors and may also prepare animals for predictable future challenges. We evaluated evidence for both actions of GCs on maternal responsiveness towards infant cries during the first 2 months of infancy in 34 wild baboon mothereinfant dyads in Amboseli, Kenya. We found that stable individual differences in faecal GCs during late pregnancy predicted stable individual differences in maternal responsiveness after birth, even after controlling for maternal rank and parity, and infant sex and distress rate. This study is among the first to provide evidence of preparative actions of GCs in wild animals and to show stability of behavioural and hormonal traits during a period of rapid changes in both hormones and behaviour. Because elevations in GCs during late pregnancy are probably primarily of fetal rather than maternal origin, our results raise the intriguing possibility that parenteoffspring conflict may underlie the preparative actions of GCs on maternal responsiveness to infant distress.

Biphenyltetrazoles are recognized privileged structures. Among them, the therapeutically important class of sartans displays antagonistic activity on AT1 receptors. We have developed a method for anchoring tetrazole derivatives via the heterocycle on a hydroxylated resin using zinc triflate. New Suzuki–Miyaura cross-coupling conditions are developed for the quantitative formation of the phenyl–phenyl bond. Our straightforward synthesis scheme, starting from the conserved phenyltetrazole moiety and ending with the appending of the structurally variable moiety, is well suited to the preparation of sartans and their analogues at a laboratory scale. We thus describe here the first solid phase synthesis of irbesartan, a marketed AT1 antagonist.

An investigation of the effect of an applied electric field on the photoluminescence (PL) intensity of single CdSe nanocrystals has revealed a measurable field induced PL modulation for a large fraction of the nanocrystals studied. The field induced intensity modulation characteristics (i.e. modulation sign and depth) were observed to vary from particle to particle, and even for different time periods for the same particle in many cases. Simultaneous intensity and frequency resolved PL measurement show that the PL intensity modulation is in fact due to an electric field effect on the PL quantum yield. The results are consistent with a model in which the energies of surface charge trapping sites are modulated by the applied electric field, causing in turn a modulation of the rates of exciton quenching by these sites. The complex observed field effects can be explained by the superposition of the applied and internal electric fields due to deeply trapped charges on the surface of the nanoparticle.

We describe a novel strategy for the synthesis of N-substituted nortropinone derivatives starting from tropinone. The key step of our synthesis is a reactivity umpolung of tropinone, which yields 8,8-dimethyl-3-oxo-8-azonia-bicyclo[3.2.1]octane iodide (IDABO) as a stable and convenient synthetic equivalent of cycloheptadienone.

Using a new Ullmann–Finkelstein tandem reaction, N-(iodophenyl)-amides were synthesized from the corresponding amides and iodo-bromobenzenes. The catalyst/ligand couple CuI/N,N′-dimethyl-cyclohexane-1,2-diamine was used for this reaction in dioxane with K3PO4 as base.

This paper describes a preliminary experimental study on charge injection in MEH-PPV polymer nanoparticles incorporated in an OLED type device. The nanoparticles have been investigated with single molecule fluorescence spectroscopy recorded simultaneously with charging and discharging of the particles. Structure and dynamics of an anion/MEH-PPV complex, proposed to be responsible for discrete photobleaching in conjugated polymers, have been investigated with this technique. Device physics and kinetics have been elucidated by using the fluorescent conjugated polymer nanoparticles as probes for detecting the presence of hole polarons, and have been related to the electrically induced oxidation and reduction of the anion/MEH-PPV complex.

A two-step sequence involving an Ugi four-component reaction was developed for the preparation of 4-aminopiperidine-4-carboxylic acid derivatives. This strategy has led to the successful preparation of two drugs carfentanil and remifentanil in shorter times and better yields than previously described methods.

Homophthalic anhydride reacts with benzaldehyde in the presence of boron trifluoride-diethyl ether complex to give the cycloadduct 3-phenyl-3,4-dihydroisocoumarin-4-carboxylic acid in good to excellent yield. Under these conditions we did not observe the formation of Perkin-type products. The reaction can be extended to a wide variety of aldehydes and to some ketones in synthetically useful yields. Amides can be obtained in good yields after activation of the carboxylic function with DCC at O°C.

Cycloaddition of imines with homophthalic anhydride in the presence of BF 3 leads to the trans isomers of isoquinolonic acids with a high stereoselectivity and avoids the formation of homophtalic amides. This catalyst extends the scope of the reaction to imines which did not react under previously described conditions.

The 2,4-dinitrophenyl group used for histidine side chain protection is not stable during aminolytic removal of Fmoc protecting groups. In the presence