Rendimiento de la PET/TC con 11C-colina en el seguimiento del cáncer de próstata / Effectiveness of 11C-choline PET/CT in prostate cancer surveillance

Objetivo Analizar el rendimiento diagnóstico de la PET/TC con 11C-colina en el seguimiento del cáncer de próstata (CaP), especialmente en pacientes con antígeno prostático específico (PSA)>1ng/ml. Material y métodos Se evaluaron retrospectivamente 329 exploraciones PET/TC con 11C-colina de 191 pacientes (68,2±7,2 años) con CaP con recaída bioquímica o en seguimiento (PSA en el momento de la PET/TC: 13,0±84,2ng/ml). El tratamiento inicial fue prostatectomía radical en 81 pacientes y otros tratamientos (radioterapia, quimioterapia, hormonoterapia) en 110. La PET/TC se adquirió 20min después de la inyección de 555-740MBq de 11C-colina. El seguimiento mínimo fue superior a 12 meses. Resultados Doscientas diecinueve (66,6%) de las 329 exploraciones PET/TC fueron positivas. El porcentaje de positivos fue significativamente mayor en los pacientes con otro tratamiento inicial diferente a la prostatectomía radical (85,6 frente a 43,6%, respectivamente). Ciento treinta PET/TC (59,4%) mostraron recidiva local, 48 (21,9%) a distancia y 41 (18,7%) local más a distancia. El abordaje terapéutico inicial se modificó en 139 casos (63,5%). De las 81 PET/TC con 11C-colina realizadas con PSA<1ng/ml, 23 (28,4%) fueron positivas. El abordaje terapéutico inicial se modificó en 9 (11,1%). Tres de 63 pacientes (4,8%) fallecieron por CaP. Conclusiones La PET/TC con 11C-colina demostró su eficacia en el seguimiento y la reestadificación del CaP, incluso en pacientes con PSA sérico<1ng/ml. El rendimiento diagnóstico fue diferente según el tratamiento inicial al que fueron sometidos los pacientes, siendo mayor en aquellos tratados inicialmente con otros tratamientos distintos de la PR prostatectomía radical (AU)

Aim Our aim was to analyse the performance of 11C-choline PET/CT in prostate cancer (PCa) surveillance, especially in patients with prostate specific antigen (PSA)<1ng/ml. Material and methods Three hundred and twenty-nine 11C-choline PET/CT examinations from 191 patients (68.2±7.2 years) submitted for PCa surveillance or biochemical recurrence were retrospectively evaluated (PSA at study was 13.0±84.2ng/ml). Main initial treatment was radical prostatectomy in 81 patients, and other treatments (radiotherapy, chemotherapy, hormonotherapy) in 110. PET/CT was acquired 20min after injection of 555-740MBq of 11C-choline. Minimum follow-up was 12 months. Results Two hundred and nineteen (66.6%) out of the 329 PET/CT examinations were positive. The percentage of positive examinations was significantly higher in patients with other initial treatment than radical prostatectomy compared to patients with radical prostatectomy (85.6 vs. 43.6%, respectively). One hundred and thirty PET/CT (59.4%) showed local recurrence, 48 (21.9%) distant recurrence, and 41 (18.7%) local plus distant recurrence. Initial therapeutic approach was changed in 139 cases (63.5%). In the subgroup of 81 11C-choline PET/CT scans performed with PSA<1ng/ml, 23 (28.4%) showed a positive result. Initial therapeutic approach was changed in 9 (11.1%). Three (4.8%) out of 63 patients died as per PCa. Conclusions 11C-choline PET/CT demonstrated its effectiveness in PCa surveillance and restaging, even in patients with serum PSA<1ng/ml. The diagnostic performance was different depending on the initial treatment, been higher in patients with non-surgical treatment (AU)

Guiding Principles for Implementing Stepped Care in Mental Health: Alignment on the Bigger Picture.

Stepped care models are a mental healthcare delivery framework in which a continuum of support allows selection of a range of interventions to match a client's evolving needs and preferences. Currently in use in multiple settings worldwide, stepped care has the potential to provide a needed advance for the development of comprehensive mental health systems. However, definitions of stepped care lack consistency, resulting in differing interpretations reflected in variable implementation, ultimately limiting its replicability, utility and potential for impact. To help foster greater alignment in research and practice, we propose a set of principles for stepped care which can provide guidance on how to bridge multiple mental health services together, reduce fragmentation, and respond to the full breadth of mental health needs along a continuum of care in diverse settings. We hope that articulating these principles will foster discussion and spur mental health stakeholders to translate them into actionable standards.

Effectiveness of 11C-choline PET/CT in prostate cancer surveillance.

AIM: Our aim was to analyse the performance of [11C]choline PET/CT in prostate cancer (PCa) surveillance, especially in patients with prostate specific antigen (PSA) < 1 ng/mL. MATERIAL AND METHODS: Three hundred and twenty-nine [11C]choline PET/CT examinations from 191 patients (68.2 ±â€¯7.2 years) submitted for PCa surveillance or biochemical recurrence were retrospectively evaluated. PSA at study was 13.0 ±â€¯84.2 ng/mL. Main initial treatment was radical prostatectomy (RP) in 81 patients, and other treatments (radiotherapy, chemotherapy, hormonotherapy) in 110. PET/CT was acquired 20' after injection of 555-740 MBq of [11C]choline. Minimum follow-up was 12 months. RESULTS: Two hundred and nineteen (66.6%) out of the 329 PET/CT examinations were positive. The percentage of positive examinations was significantly higher in patients with other initial treatment than RP compared to patients with RP (85.6% vs. 43.6%, respectively). One hundred and thirty PET/CT (59.4%) showed local recurrence, 48 (21.9%) distant recurrence, and 41 (18.7%) local plus distant recurrence. Initial therapeutic approach was changed in 139 cases (63.5%). In the subgroup of 81 [11C]choline PET/CT scans performed with PSA < 1 ng/mL, 23 (28.4%) showed a positive result. Initial therapeutic approach was changed in 9 (11.1%). Three (4.8%) out of 63 patients died as per PCa. CONCLUSION: [11C]choline PET/CT demonstrated its effectiveness in PCa surveillance and restaging, even in patients with serum PSA < 1 ng/mL. The diagnostic performance was different depending on the initial treatment, been higher in patients with non-surgical treatment.

Efficacy of Hexetidine, Thymol and Hydrogen Peroxide-Containing Oral Antiseptics in Reducing Sars-Cov-2 Virus in the Oral Cavity: A Pilot Study.

BACKGROUND: Studies have demonstrated the role of sputum as a site of severe acute respiratory syndrome-coronavirus-2 (SARSCoV-2) transmission. However, there is limited literature on the virucidal efficacy of oral antiseptics against SARS-CoV-2 virus. This study investigated the virucidal efficacy of three oral-antiseptics compared to a placebo-control in the sputum of SARS-CoV-2 infected individuals. METHODOLOGY: A pilot study of adults with SARS-CoV-2 positive results, as determined by reverse transcription-polymerase chain reaction (RT-PCR) of <7 days. The oral antiseptics investigated were: Hexetidine (0.1% w/v); Thymol (0.063% w/v) and H2O2(1.5%) compared to de-mineralized sterile water (Placebo-control). The primary outcome measure was the proportion of negative RT-PCR results at 15-mins, 30-mins, 1-hour, 2-hours and 4-hours After Oral antiseptics Interventions (AOI) compared to the placebo-control. Statistical analysis was done using STATA 15.0 software with p-values of <0.05 considered statistically significant. RESULTS: Data from a total of 66 participants that were RT-PCR SARS-CoV-2 positive at baseline (0-min) was analysed. At 15-mins AOI, the highest proportion of negativation from sputum samples was observed in the Hexedine group, with 69.2% of the baseline PCR positive cases converting to negative compared to 46.7% in the placebo-control group. In addition, H2O2 demonstrated efficacy at 2-hours AOI compared to placebo-control (62.5% vs 37.5% respectively) and other oral-antiseptics. Across all time-points, the oral-antiseptic groups compared to the placebo-control group, there was no statistically significant difference in the proportion of sputum samples which converted to a negative status (p>0.05). CONCLUSION: The findings in this study suggest there was no significant difference in the proportion of participants who converted to a negative sputum status across the treatment groups at various time points. Future studies could compare the cycle threshold (ct) viral titre values of sputum samples to determine quantitative differences.

CONTEXTE: Des études ont démontré le rôle des expectorations comme un site de transmission du syndrome respiratoire aigu sévère-coronavirus- 2 (SRAS-CoV-2). Cependant, il existe peu de documentation sur l'efficacité virucide des antiseptiques oraux contre le virus du SRASCoV-2. Cette étude a examiné l'efficacité virucide de trois antiseptiques oraux par rapport à un contrôle placebo dans les expectorations de personnes infectées par le SRAS-CoV-2. MÉTHODOLOGIE: Une étude pilote menée auprès d'adultes dont les résultats sont positifs pour le SRAS-CoV-2, tels que déterminés par la réaction en chaîne de la polymérase par transcription inverse (RT-PCR) pendant 7 jours. Les antiseptiques oraux étudiés étaient : Hexetidine (0,1% p/v) ; Thymol (0,063% p/v) et H2O2 (1,5%) par rapport à l'eau stérile déminéralisée (Placebo-contrôle). Le principal critère d'évaluation était la proportion de résultats RT-PCR négatifs 15 minutes, 30 minutes, 1 heure, 2 heures et 4 heures après les interventions antiseptiques orales (AOI) par rapport au contrôle placebo. L'analyse statistique a été réalisée à l'aide du logiciel STATA 15.0, les valeurs p de <0,05 étant considérées comme statistiquement significatives. RÉSULTATS: Les données d'un total de 66 participants qui étaient positifs à la RT-PCR SARS-CoV-2 au départ (0 minute) ont été analysées. Au bout de 15 minutes, la plus forte proportion de négativation des échantillons d'expectoration a été observée dans le groupe Hexedine, 69,2 % des cas positifs au départ par PCR devenant négatifs, contre 46,7 % dans le groupe témoin placebo. En outre, l'H2O2 a démontré son efficacité à 2 heures après l'apparition de la maladie par rapport au groupe placebo (62,5 % contre 37,5 % respectivement) et aux autres antiseptiques oraux. Pour tous les points temporels, les groupes d'antiseptiques oraux comparés au groupe placebo n'ont pas présenté de différence statistiquement significative dans la proportion d'échantillons d'expectoration qui sont devenus négatifs (p>0,05). CONCLUSION: Les résultats de cette étude suggèrent qu'il n'y a pas de différence significative dans la proportion de participants qui sont passés à un statut négatif d'expectoration dans les groupes de traitement à différents moments. Les études futures pourraient comparer les valeurs du titre viral au seuil de cycle (ct) des échantillons d'expectoration afin de déterminer les différences quantitatives. MOTS CLÉS: SRAS-CoV-2, antiseptiques oraux, hexétidine, peroxyde d'hydrogène.

Theoretical versus empirical measures of retinal magnification for scaling AOSLO images.

The adaptive optics scanning light ophthalmoscope (AOSLO) allows cellular resolution imaging of the living retina. The accuracy of many quantitative measurements made from these images requires accurate estimates of the lateral scale of the images. Here, we used trial lenses, which are known to affect the relative magnification of the retinal image, to compare empirical measures of image scale with theoretical estimates from a four-surface optical model. The theoretical optical model overestimated the empirically determined change in image scale in 70% of the subjects examined, albeit to varying degrees. While the origin for the differences between subjects is not known, residual accommodation during imaging likely contributes to this variability in retinal magnification. These data provide an opportunity to derive improved lateral scaling error estimates for structural metrics extracted from AOSLO retinal images.

Rapid prototyping of flexible terahertz metasurfaces using a microplotter.

Additive manufacturing is a promising tool for the rapid prototyping of terahertz metamaterials at low-cost. In this letter, a terahertz metamaterial is fabricated using a microplotter system on a flexible polyimide film. The limits of the rapid prototyping technique is investigated both experimentally and numerically in order to determine the spectral range accessible by the fabricated metamaterials. Here, the metamaterial is composed of four arrays of metal-insulator-metal (MIM) antennas exhibiting a Fabry Perot resonance at frequencies from 0.25 to 0.8 THz. From a structural analysis of the printed antennas, we determined that the printing resolution is limited to about 5 µm. The arrays are analyzed by terahertz time-domain spectroscopy (THz-TDS). The good agreement between THz-TDS measurements and numerical simulations showed that the microplotter system can be used for rapid prototyping by adjusting a limited number of fabrication parameters.

Ethnomedicinal uses, biological activities, phytochemistry and conservation of African ginger (Siphonochilus aethiopicus): A commercially important and endangered medicinal plant.

ETHNOPHARMACOLOGICAL RELEVANCE: In sub-Saharan Africa, African ginger (Siphonochilus aethiopicus) is used for treating common illnesses including colds, coughs, inflammation and related symptoms. The available literature survey on this plant provided scarce anecdotal information, particularly in western and eastern Africa, with a few reports on its bioactivity. In addition, the indigenous knowledge and conservation strategies of this economically important and critically endangered species are currently fragmented. AIM OF THE REVIEW: This review entails a critical appraisal of existing literature on the ethnomedicinal uses, biological activities, phytochemicals, research opportunities and prospects for the sustainable use of S. aethiopicus. MATERIALS AND METHODS: This review was conducted using a comprehensive literature search on the ethnomedicinal uses, biological activities and phytochemistry of S. aethiopicus throughout its distributional range. The conservation status and associated bio-economy potential of African ginger were also assessed. We searched different online databases (e.g. Google Scholar, ScienceDirect, PubMed and Scopus) for peer-reviewed journals, conference outputs, international, regional and national organizational reports, published books and theses. RESULTS: We established that S. aethiopicus is used to treat a wide variety of ailments such as respiratory problems (including cough, influenza), pain, inflammation and malaria. Extracts of African ginger are used as an ingredient in some commercialised products for nutraceutical, cosmeceutical and pharmaceutical purposes. The rhizome extract demonstrated anti-asthmatic, anti-inflammatory, and antiplasmodial activities, which led to the development of a patented novel extract for treating asthma and allergies. Phytochemical analysis of leaf, root and rhizome extracts of African ginger revealed the presence of flavonoids, phenolic acids, volatile and essential oils as the major constituents. These phytochemicals are known to possess bioactivities such as antimicrobial and anti-inflammatory activities. Particularly, the bioactive compounds, siphonochilone and eucalyptol, found in the roots and rhizomes have demonstrated potential to be used in remedies for treating asthma and allergic reactions. Furthermore, extracts of S. aethiopicus contained natural anti-inflammatory mediators with potential to combat and manage chronic inflammation. This plant is classified on the Red List of South African Plants as a critically endangered plant. Its high risk of extinction due to its unsustainable harvesting and exploitation necessitates its rapid propagation and cultivation to meet its increasing demand. CONCLUSIONS: The review highlights the therapeutic potential of S. aethiopicus and rational prioritization of this plant species with the potential for isolating new bioactive compounds. In the light of the use of this plant extract in traditional medicine and many commercial products, there is a heightened need to explore the mechanism(s) of action of the identified extracts and bioactive compounds in order to fully understand their pharmacokinetics and probably elucidate the pathways of their activities.

Grewia mollis Leaf Extracts and Fractions Demonstrated Good Inhibitory Activity on Pro-Inflammatory Enzymes and with Lower Cytotoxicity in vitro.

INTRODUCTION: Plant extracts are used to treat illnesses, promote health, and maintain general well-being in traditional medicine. Grewia mollis Juss (Malvaceae) is one of the medicinal herbs that is used traditionally to treat chronic diseases and related pain because currently used anti-inflammatory drugs may cause severe side effects, and naturally occurring compounds with reduced cytotoxicity could be explored for therapeutic goals. MATERIALS AND METHODS: Dried leaf of G. mollis was extracted with aqueous and organic solvents and partitioned based on polarity using solvent-solvent methods. The extracts were tested in anti-inflammatory assays against cyclooxygenases and lipoxygenase, and the safety profile was determined in a cell-based in-vitro assay. RESULTS: The n-hexane fraction of G. mollis leaf extracts had significant activity against both COX-1 (IC50 =0.97±1.9 µg/mL) and COX-2 (IC50 =1.13±0.2 µg/mL) better than the indomethacin positive control (IC50 =1.3±0.6 and 1.52±0.2 µg/mL), respectively (p≤ 0.05). Also, all the extracts and fractions of G. mollis tested inhibited the activity of 15-LOX (IC50 =12.48±2.9 to 29.43±9.9 µg/mL) better than the quercetin reference control (IC50 =61.82±5.5 µg/mL), with the butanol fraction demonstrating the best anti-15 LOX action (IC50 =12.48±2.9 µg/mL). Furthermore, all the extracts and fractions of G. mollis had relatively lower cytotoxicity on vero monkey kidney cells (LD50 =30.56-479±0.07 µg/mL) compared to the doxorubicin positive control (LD50 =2.59 µg/mL), but the selectivity index (SI=1.04-1.89) determination suggested that some of the extracts may contain toxic constituents. CONCLUSION: Organic extracts of the leaves of Grewia mollis contained bioactive molecules with potent action on COX-2 and 15-LOX. Targeted high-resolution high-performance liquid chromatographic (HPLC) methods have streamlined and enhanced bioactive compound isolation and purification process. This allows for the separation of undesirable compounds that could cause metabolic cytotoxicity in the plant extract mixtures. The method could be used to develop an alternative therapeutic strategy to manage pain associated with chronic inflammation where the use of NSAID is problematic.

[Paraneoplastic Syndromes in Ophthalmology (French version of the article)]. / Syndromes paranéoplasiques en ophtalmologie.

Paraneoplastic syndromes involving the visual system are a heterogeneous group of disorders occurring in the setting of systemic malignancy. Although these syndromes are rare, the clinical manifestations can herald an unsuspected, underlying malignancy. The associated antibodies and histopathology of each syndrome are presented to help in the understanding of these autoimmune phenomena. Outlined in this review article are diagnostic features useful in differentiating cancer-associated retinopathy, melanoma-associated retinopathy, paraneoplastic polymorphous vitelliform maculopathy, bilateral diffuse uveal melanocytic proliferation and paraneoplastic neurologic syndromes such as optic neuropathy, opsoclonus-myoclonus, Lambert-Eaton myasthenia and paraneoplastic cerebellar degeneration.

Paraneoplastic syndromes in ophthalmology.

Paraneoplastic syndromes involving the visual system are a heterogeneous group of disorders occurring in the setting of systemic malignancy. They are unrelated to local tumor invasion or metastasis and unexplained by nutritional, metabolic, infectious or iatrogenic causes. The presence of antibodies may aid in the diagnosis of a paraneoplastic syndrome, although this is not an absolute requirement. Chorioretinal involvement is seen in CAR (cancer-associated retinopathy) syndrome, MAR (melanoma-associated retinopathy) syndrome, paraneoplastic vitelliform maculopathy, and bilateral diffuse uveal melanocytic proliferation. Paraneoplastic neurological syndromes with ophthalmologic involvement include optic neuropathy, opsoclonus-myoclonus, Eaton-Lambert myasthenic syndrome, paraneoplastic cerebellar degeneration (PCD) and rhombencephalitis.

[Lyme disease or not ?] / Maladie de Lyme ou pas ?

Lyme disease is a complex pathology due to an infection by a spirochaete from the genus Borrelia. This infection results from a tick bite lasting more than 24 hours. Signs and symptoms are numerous and are usually classified in three stages: early localized disease, early disseminated disease and late disease. The skin, the heart, the nervous system and the joints are mostly concerned. It is important to distinguish the clinical manifestations of the disease from those that are sometimes associated with it but with no scientific evidence. The purpose of this article is to insist on which signs and symptoms can be related to the disease and on those that usually are not. Diagnostic methods and treatments are also discussed.

La maladie de Lyme est une pathologie complexe, qui résulte d'une infection par un spirochète du genre Borrelia. Cette infection est transmise par une morsure de tique, devant perdurer plus de 24 heures. Les manifestations cliniques de la maladie de Lyme sont nombreuses et classiquement divisées en 3 phases : primaire, secondaire et tertiaire. Elle touche principalement les systèmes cutané, cardiaque, neurologique et articulaire. Il est important de distinguer les manifestations cliniques pouvant être rapportées à cette maladie et celles pour lesquelles aucune évidence scientifique n'a pu être apportée. En effet, il est de plus en plus fréquent que certaines pathologies, dont l'étiologie est incertaine à l'heure actuelle, soient considérées comme provoquées ou secondaires à la borréliose. Cet article vise à faire la lumière sur les symptômes et signes pouvant être attribués à cette affection et ceux qui ne le sont pas. Les méthodes diagnostiques et thérapeutiques seront aussi discutées.

RNA sequencing and analysis of three Lupinus nodulomes provide new insights into specific host-symbiont relationships with compatible and incompatible Bradyrhizobium strains.

Nitrogen fixation in the legume root-nodule symbiosis has a critical importance in natural and agricultural ecosystems and depends on the proper choice of the symbiotic partners. However, the genetic determinism of symbiotic specificity remains unclear. To study this process, we inoculated three Lupinus species (L. albus, L. luteus, L. mariae-josephae), belonging to the under-investigated tribe of Genistoids, with two Bradyrhizobium strains (B. japonicum, B. valentinum) presenting contrasted degrees of symbiotic specificity depending on the host. We produced the first transcriptomes (RNA-Seq) from lupine nodules in a context of symbiotic specificity. For each lupine species, we compared gene expression between functional and non-functional interactions and determined differentially expressed (DE) genes. This revealed that L. luteus and L. mariae-josephae (nodulated by only one of the Bradyrhizobium strains) specific nodulomes were richest in DE genes than L. albus (nodulation with both microsymbionts, but non-functional with B. valentinum) and share a higher number of these genes between them than with L. albus. In addition, a functional analysis of DE genes highlighted the central role of the genetic pathways controlling infection and nodule organogenesis, hormones, secondary, carbon and nitrogen metabolisms, as well as the implication of plant defence in response to compatible or incompatible Bradyrhizobium strains.

Investigation of the Mechanism of Anti-Inflammatory Action and Cytotoxicity of a Semipurified Fraction and Isolated Compounds From the Leaf of Peltophorum africanum (Fabaceae).

Peltophorum africanum extracts have been shown to possess many important medicinal benefits, including anti-inflammatory and antiviral activities. However, the mechanism of action is poorly understood. The mechanism of anti-inflammatory action was determined by measuring the synthesis of cytokines in lipopolysaccharide (LPS) stimulated RAW 264.7 macrophage cells in vitro. Compound 1 (CP1), compound 2 (CP2), and fraction F3.3.0 (F3.3.0) significantly reduced the synthesis of interleukin 1ß (IL-1ß) from RAW 264.7 cells (1.18, 1.32, and 0.92 ng/mL), respectively. Similarly, CP1, CP2, and F3.3.0 inhibited the production of IL-2 and tumor necrosis factor-α (TNF-α) by RAW 264.7 cells (0.41, 0.60, 0.74 and 0.11, 0.27, 0.24 ng/mL, respectively. In addition, CP1 and CP2 had lower cytotoxicity toward RAW 264.7 cells, with CP2 indicating the lowest cytotoxicity (LD50 = 207.88 µg/mL). The mechanism of action was found to be via the inhibition of pro-inflammation cytokines (IL-1 ß and TNF-α). This observation may support the use of P africanum to treat pain-related conditions.

The evolutionary fate of the chloroplast and nuclear rps16 genes as revealed through the sequencing and comparative analyses of four novel legume chloroplast genomes from Lupinus.

The Fabaceae family is considered as a model system for understanding chloroplast genome evolution due to the presence of extensive structural rearrangements, gene losses and localized hypermutable regions. Here, we provide sequences of four chloroplast genomes from the Lupinus genus, belonging to the underinvestigated Genistoid clade. Notably, we found in Lupinus species the functional loss of the essential rps16 gene, which was most likely replaced by the nuclear rps16 gene that encodes chloroplast and mitochondrion targeted RPS16 proteins. To study the evolutionary fate of the rps16 gene, we explored all available plant chloroplast, mitochondrial and nuclear genomes. Whereas no plant mitochondrial genomes carry an rps16 gene, many plants still have a functional nuclear and chloroplast rps16 gene. Ka/Ks ratios revealed that both chloroplast and nuclear rps16 copies were under purifying selection. However, due to the dual targeting of the nuclear rps16 gene product and the absence of a mitochondrial copy, the chloroplast gene may be lost. We also performed comparative analyses of lupine plastomes (SNPs, indels and repeat elements), identified the most variable regions and examined their phylogenetic utility. The markers identified here will help to reveal the evolutionary history of lupines, Genistoids and closely related clades.

First isolation of glutinol and a bioactive fraction with good anti-inflammatory activity from n-hexane fraction of Peltophorum africanum leaf.

OBJECTIVE: To investigate the anti-inflammatory activity of different fractions and glutinol (isolated compound), using nitric oxide synthase and cyclooxygenase (COX) inhibition as an indication of anti-inflammatory activity. METHODS: Anti-inflammatory activity was evaluated using an in vitro assay determining the inhibition of the activity of pro-inflammatory enzyme model. Cyclooxygenases and inducible nitric oxide synthase are crucial enzymes involved in the pathogenesis of many chronic inflammatory conditions. RESULTS: Sub-fraction F3.3 that was derived from n-hexane fraction of PA leaves significantly inhibited (P = 0.01) the catalytic activity of COX-2 (IC50 = 0.67 µg/mL) better than isolated compound, glutinol (IC50 = 1.22 µg/mL), compound 2 (CP2) (IC50 = 1.71 µg/mL) and sub-fraction F3.3.0 (IC50 = 1.30 µg/mL). A similar trend was observed in investigation of the inhibition of nitric oxide synthesis in RAW 264.7 cells by F3.3, glutinol, CP2 and F3.3.0. Inducible COX-2 and inducible nitric oxide synthase are among potent signalling enzymes that exacerbate inflammation. CONCLUSIONS: Bioactive sub-fractions (F3.3 and F3.3.0) derived from the n-hexane fraction of PA had good anti-inflammatory activity, and the isolated compound, and glutinol may be useful as a template for the development of new anti-inflammatory drugs.

First isolation of glutinol and a bioactive fraction with good anti-inflammatory activity from n-hexane fraction of Peltophorum africanum leaf

OBJECTIVE@#To investigate the anti-inflammatory activity of different fractions and glutinol (isolated compound), using nitric oxide synthase and cyclooxygenase (COX) inhibition as an indication of anti-inflammatory activity.@*METHODS@#Anti-inflammatory activity was evaluated using an in vitro assay determining the inhibition of the activity of pro-inflammatory enzyme model. Cyclooxygenases and inducible nitric oxide synthase are crucial enzymes involved in the pathogenesis of many chronic inflammatory conditions.@*RESULTS@#Sub-fraction F3.3 that was derived from n-hexane fraction of PA leaves significantly inhibited (P = 0.01) the catalytic activity of COX-2 (IC = 0.67 μg/mL) better than isolated compound, glutinol (IC = 1.22 μg/mL), compound 2 (CP2) (IC = 1.71 μg/mL) and sub-fraction F3.3.0 (IC = 1.30 μg/mL). A similar trend was observed in investigation of the inhibition of nitric oxide synthesis in RAW 264.7 cells by F3.3, glutinol, CP2 and F3.3.0. Inducible COX-2 and inducible nitric oxide synthase are among potent signalling enzymes that exacerbate inflammation.@*CONCLUSIONS@#Bioactive sub-fractions (F3.3 and F3.3.0) derived from the n-hexane fraction of PA had good anti-inflammatory activity, and the isolated compound, and glutinol may be useful as a template for the development of new anti-inflammatory drugs.

First isolation of glutinol and a bioactive fraction with good anti-inflammatory activity from n-hexane fraction of Peltophorum africanum leaf

Objective To investigate the anti-inflammatory activity of different fractions and glutinol (isolated compound), using nitric oxide synthase and cyclooxygenase (COX) inhibition as an indication of anti-inflammatory activity. Methods Anti-inflammatory activity was evaluated using an in vitro assay determining the inhibition of the activity of pro-inflammatory enzyme model. Cyclooxygenases and inducible nitric oxide synthase are crucial enzymes involved in the pathogenesis of many chronic inflammatory conditions. Results Sub-fraction F3.3 that was derived from n-hexane fraction of PA leaves significantly inhibited (P = 0.01) the catalytic activity of COX-2 (IC