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Connor, M.

Publications and source records attributed to Connor, M..

17 recordsLinked to original sources

(+)-trans-Cannabidiol is a CB2 receptor agonist

3:(-)-trans-Cannabidiol ((-)-CBD) is a principal phytocannabinoid from Cannabis sativa. (-)-CBD has complex pharmacology but is a relatively weak inhibitor of CB1 and CB2 receptor signalling. Cannabidiol has two chiral centres and thus four stereoisomers. (+)-trans-CBD ((+)-CBD) has a higher affinity than (-)-CBD at CB1 and CB2, but its pharmacodynamic effects at these receptors are incompletely described. We examined the activity of (+)-CBD at human CB1 and CB2 receptors using a fluorescence-based assay of membrane potential in AtT20 cells stably expressing CB1 or CB2 receptors. (+)-CBD produced a rapid, concentration-dependent hyperpolarization in CB2-expressing cells (pEC50 6.63 {+/-} 0.08) with a maximal effect [~]90% of the response to CP55940. The CB2 response was blocked by pertussis toxin pretreatment and competitively inhibited by the CB2 antagonist AM630 (Schild slope 1.1 {+/-} 0.1). (+)-CBD was a low-efficacy, low-potency CB1 agonist and inhibited somatostatin-receptor effects at high concentrations (10-30 {micro}M). It had no effect on the membrane potential of AtT20 wild-type cells. In silico modelling of ligand interactions with CB2 indicated that (+)-CBD but not (-)-CBD formed an H-bond with Ser285, a residue crucial for agonist activation of CB2. Our data suggests (+)-CBD acted as a CB2 agonist via the orthosteric binding site on the receptor. Synthetic CBD, including (+)-CBD, has previously been administered in clinical trials, presumably without consideration of its potential CB2 agonist activity. Given the relative safety of (-)-CBD in people, (+)-CBD may be a useful drug to explore CB2-sensitive disease states, should it prove similarly safe.

pharmacology and toxicology↗

Tetracycline-Regulated Inducible CB2 Expression in AtT20 Cells: A Functional Assay for Quantifying Ligand Efficacy

IntroductionCannabinoid receptor-2 (CB2) is an emerging therapeutic target for chronic and inflammatory pain, cancer, and neurological disorders. Understanding the efficacy of CB2 ligands is crucial for future drug design and development. AimsWe aimed to establish a simple and robust system to control CB2 expression using a tetracycline-regulated mammalian expression system (T-REx), to enable application of the Black and Leff operational model to measure the operational efficacy ({tau}) of CB2 ligands. MethodsLigand-induced hyperpolarisation of AtT20 cells transfected with T-REx and human CB2 was measured by FLIPR membrane potential assay. Maximal and submaximal responses of the CB2 ligands were produced by regulating CB2 expression using tetracycline. Data were fitted to the operational model of receptor depletion to quantify the efficacy of seven ligands. Additionally, the maximal initial rate of signalling (IRmax), another putative measure of ligand efficacy, was determined. ResultsAK-F-064, CP55940 and 2-AG exhibited similar efficacy with a {tau} values of 11.4, 11 and 10.4 respectively, while anandamide (AEA) had the lowest efficacy ({tau}=1.07) among the tested agonists. The rank order of operational efficacy and IRmax was similar and was estimated as: AK-F-064 = CP55940 = 2-AG > 5F-AB-PICA = WIN55212-2 > HU-308 = AEA. ConclusionThis inducible expression system provides a reliable platform for quantifying and comparing CB2 ligand efficacy using the operational model. This approach may facilitate more precise CB2-targeted drug development and can be readily extended to other GPCR targets.

pharmacology and toxicology↗

New rice varieties with improved phosphorus-efficiency for low-input smallholder rice production in Africa

Smallholder farmers in Sub-Saharan Africa frequently produce rice in marginal environments where low soil fertility and other biotic and abiotic stresses limit productivity. Rice varieties developed by centralized breeding under favorable conditions on research stations have often not been adopted by farmers in such marginal environments. Our objective was to develop modern rice varieties adapted to such low-input conditions through combining pre-breeding research with subsequent selection and variety testing directly in the target environment: smallholder farmers fields in Madagascar with phosphorus (P) fixing soils. Two breeding populations were developed for this purpose, one based on marker-assisted introgression of the Pup1 locus into IR64, the second using a donor (DJ123) for internal P utilization efficiency and external P acquisition efficiency. Selection within these populations was conducted in fields managed according to local farmers practice without mineral fertilizer addition. Selected breeding lines underwent government-supervised variety release testing including farmer participatory evaluations in four Malagasy regions between 18-1350 masl altitude, and two lines were released as varieties FyVary32 and VyVary85. Both had between 0.47-0.8 t ha-1 higher grain yield than parent IR64 and local check X265. Yield advantages were stable across a range from 2.1-5.5 t ha-1 (national average: 2.8 t ha-1). Higher yields were accompanied by superior root development and P uptake and by more efficient internal P utilization in FyVary85. Results show that decentralized breeding in marginal environments can produce varieties not only superior in lowest-yielding environments but across a broader range, clearly surpassing national average yields.

plant biology↗

Modeling viral and bacterial infections in human lung organotypic systems reveals strain specific host responses

In this study, we developed novel lung organoid-on-chip models that elucidate differential human tissue response to various strains of respiratory pathogens: Streptococcus pneumoniae and SARS-CoV-2. We show that human fetal-derived distal lung epithelial cells are readily expandable in 3D as organoids, thereby providing a highly sustainable source of lung progenitor cells. These 3D organoid progenitors can then be induced to produce airway and alveolar organoids on microfluidic devices. Upon challenge with Streptococcus pneumoniae, a bacterium known to cause pneumonia, a rapid and strain-dependent colonization was observed at the epithelial surface of alveolar chips. We also assessed SARS-CoV-2 infection in the alveoli-on-chip system and observed that the Delta variant exhibited greater infectivity as compared to the Omicron BA.5. Both SARS-CoV-2 variants induced potent interferon responses and triggered the expression of different interferon-stimulated genes. Our results demonstrate that strain-specific host defense mechanisms can be recapitulated in human-organoid-based microfluidic systems, paving the way for the use of such platforms for more targeted assessments of human response to novel emergent pathogen strains. HighlightsO_LIHuman fetal epithelial lung stem cells can be expanded as multipotent organoids and differentiated into both airway or alveolar organoids C_LIO_LIMultipotent lung organoids efficiently produce functional epithelia of small airway or alveoli when grown on-chip. C_LIO_LIStreptococcus pneumoniae inoculation in alveoli-on-chip mimics the early stages of bacterial colonization in lung epithelia C_LIO_LIAlveoli on-chip system recapitulates variant-specific interactions. SARS-CoV-2 Delta replicates but not Omicron BA.5. C_LIO_LIRobust interferon response upon SARS-CoV-2 infection shows Alveoli on-chip can model innate immune responses. C_LI

bioengineering↗

Polyunsaturated fatty acids and their endocannabinoid-related metabolites activity at human TRPV1 and TRPA1 ion channels expressed in HEK-293 cells.

BackgroundPolyunsaturated fatty acids (PUFAs), particularly Omega-3 ({omega}-3) and Omega-6 ({omega}-6) PUFAs, may exert neuroprotective effects via the endocannabinoid system (ECS) and are promoted as brain health supplements. However, despite their potential role in endocannabinoid biosynthesis, the impact of PUFAs on ion channels such as TRPV1 and TRPA1, which are modulated by endocannabinoids, remains incompletely understood. Furthermore, the potential in vitro actions of {omega}-6 to {omega}-3 PUFA combined in the ratios available in supplements remains uncertain. Therefore, the objective of this study is to evaluate the functional activity of individual PUFAs, their combination in a specific ratio, and their endocannabinoid-related derivatives on TRPV1 and TRPA1 ion channels. MethodologyWe employed a fluorescent Ca-sensitive dye in HEK-293 Flp-In T-REx cells expressing human TRPV1, TRPA1, or an empty vector to measure changes in intracellular calcium concentration ([Ca2+]i). ResultsCapsaicin and certain PUFA derivatives such as DHEA, {gamma}-LEA and AEA stimulate TRPV1 activity directly, whereas EPA, DHA, {gamma}-LA, and their 9:3:1 ratio triggered TRPV1 response via a mechanism dependent on prior exposure to phorbol ester. Similarly, cinnamaldehyde and selected PUFA derivatives such as EPEA, DHEA, {gamma}-LEA, 2-AG, 2-AG ether and AEA triggered TRPA1 response, with EPA, DHA, {gamma}-LA, and the 9:3:1 ratio showing significant effects at higher concentrations. ConclusionsPUFAs alone and their combined form in 9:3:1 ratio stimulate TRPA1 activity, whereas their metabolites trigger both TRPV1 and TRPA1 response. These findings suggest new avenues to explore for research into potential mechanisms underlying the neurological benefits of PUFAs and their metabolites.

pharmacology and toxicology↗

Activation of cannabinoid CB2 receptors by (-)-cannabichromene but not (+)-cannabichromene

IntroductionCannabichromene (CBC) is a minor constituent of Cannabis that is a selective cannabinoid CB2 receptor agonist and activator of TRPA1. To date, it has not been shown whether (-)-CBC, (+)-CBC (or both) can mediate these effects. In this study we investigate the activity of the CBC enantiomers at CB1, CB2 and TRPA1 in vitro. Materials and MethodsCBC enantiomers were purified from synthetic CBC by chiral chromatography, and their optical activity was confirmed by spectroscopy. Human CB1 and CB2 receptor activity was measured using a fluorescent assay of membrane potential in stably transfected AtT20 cells. TRPA1 activation was measured using a fluorescent assay of intracellular calcium in stably transfected HEK293 cells. Results(-)-CBC activated CB2 with an EC50 of 1.5 {micro}M, to a maximum of 60 % of CP55940. (+)-CBC did not activate CB2 at concentrations up to 30 {micro}M. Only 30 {micro}M (-)- CBC produced detectable activation of CB1, (+)-CBC was inactive. Both (-)-CBC and (+)- CBC activated TRPA1; at 30 {micro}M (-)-CBC produced an activation 50% of that of the reference agonist cinnamaldehyde (300 {micro}M), 30 {micro}M (+)-CBC activated TRPA1 to 38% of the cinnamaldehyde maximum. DiscussionIt is unclear whether (-)-CBC is the sole or even the predominant enantiomer of CBC enzymatically synthesized in Cannabis. This study shows that (-)-CBC is the active isomer at CB2 receptors, while both isomers activate TRPA1. The results suggest that medicinal preparations of CBC that target cannabinoid receptors would be most effective when (-)-CBC is the dominant isomer.

pharmacology and toxicology↗

Impact of Streptococcus pneumoniae biosynthesis gene mutations on epithelial microinvasion and cellular responses

Nasopharyngeal colonisation by Streptococcus pneumoniae is characterised by bacterial adherence to epithelial cells, microinvasion and innate immune activation. Previously, we have shown two serotype 6B S. pneumoniae mutant strains affecting bacterial metabolism ({Delta}proABC/pia and{Delta} fhs/pia) colonise humans and mice, but in a murine disease model do not cause invasive infection. Here, we explore whether S. pneumoniae epithelial microinvasion and the induction of innate immune responses persist despite disease attenuation. We show that under serum stress, these biosynthesis gene mutations had a broad but different impact on pneumococcal virulence gene expression, oxidative stress regulation, and purine and carbohydrate metabolism genes. However, although these mutations did not attenuate microinvasion in human challenge and epithelial models, there was less transmigration of Detroit 562 nasopharyngeal epithelial cells by the mutants compared to WT. Cellular reorganisation of primary human airway epithelium varied considerably between strains. Compared to WT, infection of Detroit 562 epithelial cells by the{Delta} fhs/piaA strain, but not the{Delta} proABC/piaA strain was less pro-inflammatory, induced less caspase 8 production, and were associated with increased pneumococcal hydrogen peroxide and reduced pneumolysin secretion. These findings suggest that the observed differences in microinvasion and the epithelial response were driven by the differential expression of multiple bacterial virulence and metabolic pathways, rather than single genes or pathways of genes. These data highlight the complex impact of single gene mutations on bacterial virulence and suggest that the virulence determinants of pneumococcal epithelial colonisation, microinvasion and innate immunity are not necessarily directly linked to disease. Author SummaryStreptococcus pneumoniae (the pneumococcus) commonly colonises the back of the human nose, and is a leading cause of pneumonia, meningitis, and sepsis. During colonisation, the pneumococcus adheres to the cells in the nose, invades these cells (so-called microinvasion), and activates them. Colonisation is a pre-requisite for disease, however, since disease is largely a dead end for S. pneumoniae, it remains unclear whether these processes are directly linked to disease progression. We have previously shown that if we introduce gene mutations into S. pneumoniae that affect key metabolic pathways, these bacteria retain their ability to colonize human and animal models without causing disease. We now show that these mutants retain their ability to microinvade epithelial cells in human and mouse models, and some may still cause inflammation, but are less able to pass through the epithelial barrier. However, although the attenuation of disease may be explained by the broad-ranging impact of these mutations on pneumococcal virulence, oxidative stress, and metabolism, they are not driven by a single determinant. Our findings suggest that pneumococcal microinvasion and immune activation are not necessarily pre-cursors to disease progression. This supports the idea that S. pneumoniae adapts and evolves to promote colonisation and ultimately transmission rather than cause disease. Graphical AbstractS. pneumoniae colonisation is characterised by mucus association, epithelial adherence, microcolony formation and microinvasion - where the pneumococcus invades the epithelial barrier without causing disease. Although mutations in S. pneumoniae biosynthesis genes ({Delta}proABC and{Delta} fhs) attenuate disease in a murine model, they do not attenuate microinvasion in either experimental human pneumococcal challenge (EHPC), ex vivo or in vitro epithelial cells. Transmigration of the epithelial barrier is attenuated. These mutations show strain-dependent effects on both the epithelial and bacterial responses to infection. Factors such as epithelial cellular reorganisation, inflammation and caspase 8 activity alongside pneumococcal metabolic adaptation, virulence factor expression and response to stress are important components of these processes. O_FIG O_LINKSMALLFIG WIDTH=200 HEIGHT=86 SRC="FIGDIR/small/545009v8_ufig1.gif" ALT="Figure 1"> View larger version (24K): org.highwire.dtl.DTLVardef@11a17aeorg.highwire.dtl.DTLVardef@8c707org.highwire.dtl.DTLVardef@42abf8org.highwire.dtl.DTLVardef@12850f9_HPS_FORMAT_FIGEXP M_FIG C_FIG

microbiology↗

Modulation of Recombinant Human T-type calcium channels by Δ9-tetrahydrocannabinolic acid in vitro

IntroductionLow voltage-activated T-type calcium channels (T-type ICa), CaV3.1, CaV3.2, and CaV3.3 are opened by small depolarizations from the resting membrane potential in many cells and have been associated with neurological disorders including absence epilepsy and pain. {Delta}9-tetrahydrocannabinol (THC) is the principal psychoactive compound in Cannabis and also directly modulates T-type ICa, however, there is no information about functional activity of most phytocannabinoids on T-type calcium channels, including {Delta}9-tetrahydrocannabinol acid (THCA), the natural non-psychoactive precursor of THC. The aim of this work was to characterize THCA effects on T-type calcium channels. Materials and MethodsWe used HEK293 Flp-In-TREx cells stably expressing CaV3.1, 3.2 or 3.3. Whole-cell patch clamp recordings were made to investigate cannabinoid modulation of ICa. ResultsTHCA and THC inhibited the peak current amplitude CaV3.1 with a pEC50s of 6.0 {+/-} 0.7 and 5.6 {+/-} 0.4, respectively. 1M THCA or THC produced a significant negative shift in half activation and inactivation of CaV3.1 and both drugs prolonged CaV3.1 deactivation kinetics. THCA (10 M) inhibited CaV3.2 by 53% {+/-} 4 and both THCA and THC produced a substantial negative shift in the voltage for half inactivation and modest negative shift in half activation of CaV3.2. THC prolonged the deactivation time of CaV3.2 while THCA did not. THCA inhibited the peak current of CaV3.3 by 43% {+/-} 2 (10M) but did not notably affect CaV3.3 channel activation or inactivation, however, THC caused significant hyperpolarizing shift in CaV3.3 steady state inactivation. DiscussionTHCA modulated T-type ICa currents in vitro, with significant modulation of kinetics and voltage dependence at low M concentrations. This study suggests that THCA may have potential for therapeutic use in pain and epilepsy via T-type channel modulation without the unwanted psychoactive effects associated with THC.

pharmacology and toxicology↗

Modulation of Human T-type Calcium Channels by Synthetic Cannabinoid Receptor Agonists in vitro

BACKGROUND AND PURPOSEConsumption of Synthetic Cannabinoid Receptor agonists (SCRAs) is associated with severe adverse reactions including seizures, arrhythmias and death, but the molecular mechanisms surrounding SCRA toxicity are not yet established. These disease-like symptoms are also synonymous with altered T-type calcium channel activity which controls rhythmicity in the heart and brain. This study examined whether SCRAs alter T-type activity and whether this represents a possible mechanism of toxicity. EXPERIMENTAL APPROACHFluorescence-based and electrophysiology assays were used to screen 16 structurally related synthetic cannabinoids for their ability to inhibit human T-type calcium channels expressed in HEK293 cells. The most potent compounds were then further examined using patch clamp electrophysiology. KEY RESULTSMDMB-CHMICA and AMB-CHMINACA potently blocked Cav3.2 with IC50 values of 1.5 and 0.74 M respectively. Current inhibition increased from 47 to 80% and 45 to 87% respectively when the channel was in slow-inactivated state. Both SCRAs had little effect on steady state inactivation, however MDMB-CHMICA significantly shifted the half activation potential by -7mV. Neither drug produced frequency dependent block, in contrast to the phytocannabinoid {Delta}9-THC. CONCLUSIONS and IMPLICATIONSSCRAs are potent agonists of CB1 receptors and can be extremely toxic, but observed toxicity also resembles symptoms associated with altered Cav3.2 activity. Many SCRAs tested were potent modulators of Cav3.2, raising the possibility that SC toxicity may be due in part to Cav3.2 modulation. This potent T-type channel modulation suggests the possibility of SCRAs as a new drug class with potential to treat diseases associated with altered T-type channel activity.

pharmacology and toxicology↗

Streptococcus pneumoniae infection promotes histone H3 dephosphorylation by modulating host PP1 phosphatase

Pathogenic bacteria can alter host gene expression through post-translational modifications of histones. We show for the first time that a natural colonizer, Streptococcus pneumoniae, also induces specific histone modifications, including robust dephosphorylation of histone H3 on serine 10, during infection of respiratory epithelial cells. Two bacterial factors are important for the induction of this modification: the bacterial toxin PLY, a pore-forming toxin, and the pyruvate oxidase SpxB, an enzyme responsible for H2O2 production. The combined effects of PLY and H2O2 lead to host signaling which culminates in H3S10 dephosphorylation, mediated by the host cell phosphatase PP1. Strikingly, S. pneumoniae infection induces dephosphorylation and associated activation of PP1 catalytic activity. Colonization of cells, which lacked active PP1, resulted in the impairment of intracellular S. pneumoniae survival. Interestingly, PP1 activation mediating H3S10 dephosphorylation is not restricted to S. pneumoniae and appears to be a general epigenomic mechanism favoring intracellular survival.

microbiology↗

Differential activation of G protein-mediated signalling by synthetic cannabinoid receptor agonists

Synthetic cannabinoid receptor agonists (SCRAs) are new psychoactive substances associated with acute intoxication and even death. However, the molecular mechanisms through which SCRAs may exert their toxic effects remain unclear - including the potential differential activation of G protein subtypes by CB1, a major target of SCRA. We measured CB1-mediated activation of Gs and Gi/o proteins by SCRAs by examining stimulation (PTX-treated) as well as inhibition (non-PTX treated) of forskolin-induced cAMP accumulation in HEK cells stably expressing CB1. Real-time measurements of stimulation and inhibition of cAMP levels were made using a BRET biosensor. We found that the maximum concentration of SCRAs tested (10 M), increased cAMP levels 12 to 45% above that produced by forskolin alone, while the phytocannabinoid THC did not significantly alter cAMP levels in PTX-treated HEK-CB1 cells. All SCRAs had greater potency to inhibit of forskolin-induced cAMP levels than to stimulate cAMP levels. The rank order of potencies for SCRA stimulation of cAMP (Gs) was PB-22 > 5F-MDMB-PICA > JWH-018 > AB-FUBINACA > XLR-11. By contrast, the potency of SCRAs for inhibition of cAMP (Gi/o) was 5F-MDMB-PICA > AB-FUBINACA > PB-22 > JWH-018 > XLR-11. The different rank order of potency of the SCRAs to stimulate Gs-like signalling compared to Gi/o signalling suggests differences in G protein preference between SCRAs. Understanding the apparent differences among these drugs may contribute to unravelling their complex effects in humans.

pharmacology and toxicology↗

Brodifacoum does not modulate human cannabinoid receptor-mediated hyperpolarization of AtT20 cells or inhibition of adenylyl cyclase in HEK 293 cells

BackgroundSynthetic cannabinoids are a commonly used class of recreational drugs that can have significant adverse effects. There have been sporadic reports of co-consumption of illicit drugs with rodenticides such as warfarin and brodifacoum (BFC) over the past 20 years but recently, hundreds of people have been reported to have been poisoned with a mixture of synthetic cannabinoids and BFC. We have sought to establish whether BFC directly affects cannabinoid receptors, or their activation by the synthetic cannabinoid CP55940 or the phytocannabinoid {Delta}9-tetrahydrocannabinol ({Delta}9-THC).\n\nMethodsThe effects of BFC on the hyperpolarization of wild type AtT20 cells, or AtT20 cells stably expressing human CB1- and CB2-mediated receptors, were studied using a fluorescent assay of membrane potential. The effects of BFC on CB1 and CB2 mediated inhibition of forskolin-stimulated adenylyl cyclase (AC) activation was measured using a BRET assay of cAMP levels in HEK 293 cells stably expressing human CB1 and CB2.\n\nResultsBFC did not activate CB1 or CB2 receptors, or affect the hyperpolarization of wild type AtT20 cells produced by somatostatin. BFC (10 {micro}M) did not affect the hyperpolarization of AtT20-CB1 or AtT20-CB2 cells produced by CP55940 or {Delta}9-THC. BFC (1 {micro}M) did not affect the inhibition of forskolin-stimulated AC activity by CP55940 in HEK 293 cells expressing CB1 or CB2. BFC (1 {micro}M) also failed to affect the desensitization of CB1 and CB2 signalling produced by prolonged (30 min) application of CP55940 or {Delta}9-THC to AtT20 cells.\n\nDiscussionBFC is not a cannabinoid receptor agonist, and appeared not to affect cannabinoid receptor activation. Our data suggests there is no pharmacodynamic rationale for mixing BFC with synthetic cannabinoids, however, it does not speak to whether BFC may affect synthetic cannabinoid metabolism or biodistribution. The reasons underlying the mixing of BFC with synthetic cannabinoids are unknown, and it remains to be established whether the \"contamination\" was deliberate or accidental. However, the consequences for people who ingested the mixture were often serious, and sometimes fatal, but this seems unlikely to be due to BFC action at cannabinoid receptors.

pharmacology and toxicology↗

Absence of entourage: Terpenoids commonly found in Cannabis sativa do not modulate the functional activity of Δ9-THC at human CB1 and CB2 receptors

IntroductionCompounds present in Cannabis sativa such as phytocannabinoids and terpenoids, may act in concert to elicit therapeutic effects. Cannabinoids such as {Delta}9-tetrahydrocannabinol ({Delta}9-THC) directly activate cannabinoid receptor 1 (CB1) and cannabinoid receptor 2 (CB2), however, it is not known if terpenoids present in Cannabis also affect cannabinoid receptor signalling. Therefore, we examined 6 common terpenoids alone, and in combination with cannabinoid receptor agonists, on CB1 and CB2 signalling in vitro.\n\nMaterials and MethodsPotassium channel activity in AtT20 FlpIn cells transfected with human CB1 or CB2 receptors was measured in real-time using FLIPR(R) membrane potential dye in a FlexStation 3 plate reader. Terpenoids were tested individually and in combination for periods up to 30 minutes. Endogenous somatostatin receptors served as a control for direct effects of drugs on potassium channels.\n\nResults-Pinene, {beta}-pinene, {beta}-caryophyllene, linalool, limonene and {beta}-myrcene (up to 30-100 {micro}M) did not change membrane potential in AtT20 cells expressing CB1 or CB2, or affect the response to a maximally effective concentration of the synthetic cannabinoid CP55,940. The presence of individual or a combination of terpenoids did not affect the hyperpolarization produced by {Delta}9-THC (10{micro}M): (CB1: control, 59{+/-}7%; with terpenoids (10 {micro}M each) 55{+/-}4%; CB2: {Delta}9-THC 16{+/-}5%, with terpenoids (10 {micro}M each) 17{+/-}4%). To investigate possible effect on desensitization of CB1 responses, all six terpenoids were added together with {Delta}9-THC and signalling measured continuously over 30 min. Terpenoids did not affect desensitization, after 30 minutes the control hyperpolarization recovered by 63{+/-}6%, in the presence of the terpenoids recovery was 61{+/-}5%.\n\nDiscussionNone of the six of the most common terpenoids in Cannabis directly activated CB1 or CB2, or modulated the signalling of the phytocannabinoid agonist {Delta}9-THC. These results suggest that if a phytocannabinoid-terpenoid entourage effect exists, it is not at the CB1 or CB2 receptor level. It remains possible that terpenoids activate CB1 and CB2 signalling pathways that do not involve potassium channels, however, it seems more likely that they may act at different molecular target(s) in the neuronal circuits important for the behavioural effect of Cannabis.

pharmacology and toxicology↗

Cannabichromene is a cannabinoid CB2 receptor agonist

BACKGROUNDCannabichromene (CBC) is one of the most abundant phytocannabinoids in Cannabis spp. It has modest anti-nociceptive and anti-inflammatory effects and potentiates some effects of {Delta}9-tetrahydrocannabinol (THC) in vivo. How CBC exerts these effects is poorly defined and there is little information about its efficacy at cannabinoid receptors. We sought to determine the functional activity of CBC at CB1 and CB2 receptors.\n\nEXPERIMENTAL APPROACHAtT20 cells stably expressing HA-tagged human CB1 and CB2 receptors were used. Assays of cellular membrane potential and loss of cell surface receptors were performed.\n\nKEY RESULTSCBC activated CB2 but not CB1 receptors to produce a hyperpolarization of AtT20 cells. Activation of CB2 receptors was antagonised by the CB2 antagonist AM630 and sensitive to pertussis toxin. Co-application of CBC reduced activation of CB2 receptors CP55,940, a potent CB1 and CB2 agonist. Continuous CBC application induced loss of cell surface CB2 receptors and desensitisation of the CB2-induced hyperpolarization.\n\nCONCLUSIONS AND IMPLICATIONSCannabichromene is a selective CB2 receptor agonist displaying higher efficacy than THC in hyperpolarising AtT20 cells. CBC may contribute to the potential therapeutic effectiveness of some cannabis preparations, potentially through CB2-mediated modulation of inflammation.

pharmacology and toxicology↗

The chemistry and pharmacology of putative synthetic cannabinoid receptor agonist (SCRA) new psychoactive substances (NPS) 5F-PY-PICA, 5F-PY-PINACA, and their analogues

The structural diversity of synthetic cannabinoid receptor agonist (SCRA) new psychoactive substances (NPS) has increased since the first examples were reported a decade ago. 5F-PY-PICA and 5F-PY-PINACA were identified in 2015 as putative SCRA NPS, although nothing is known of their pharmacology. 5F-PY-PICA, 5F-PY-PINACA, and analogues intended to explore structure-activity relationships within this class of SCRAs were synthesized and characterized by nuclear magnetic resonance spectroscopy and liquid chromatography-quadrupole time-of-flight-mass spectrometry. Using competitive binding experiments and fluorescence-based plate reader membrane potential assays, the affinities and activities of all analogues at cannabinoid type 1 and type 2 receptors (CB1 and CB2) were evaluated. All ligands showed minimal affinity for CB1 (pKi < 5), although several demonstrated moderate CB2 binding (pKi = 5.45-6.99). At 10 M none of the compounds produced an effect > 50% of CP55,950 at CB1, while several compounds showed a slightly higher relative efficacy at CB2. Unlike other SCRA NPS, 5F-PYPICA and 5F-PY-PINACA did not produce cannabimimetic effects in mice at doses up to 10 mg/kg.

pharmacology and toxicology↗

A highly conserved complete accessory Escherichia coli type III secretion system 2 is widespread in bloodstream isolates of the ST69 lineage

Bacterial type III secretion systems (T3SS) play an important role in pathogenesis of Gram-negative infections. Enteropathogenic and enterohemorrhagic Escherichia coli contain a well-defined T3SS but in addition a second T3SS termed E. coli T3SS 2 (ETT2) has been described in a number of strains of E. coli. The majority of E. coli contain elements of a genetic locus encoding ETT2, but which has undergone significant mutational attrition rendering it without predicted function. Only a very few strains have been reported to contain an intact ETT2 locus. To investigate the occurrence of the ETT2 locus in strains of human pathogenic E. coli, we carried out genomic sequencing of 162 isolates obtained from patient blood cultures in Scotland. We found that all 26 ST69 isolates from this collection contained an intact ETT2 together with an associated eip locus which encodes putative secreted ETT2 effectors as well as eilA, a gene encoding a putative transcriptional regulator of ETT2 associated genes. Using a reporter gene for eilA activation, we defined conditions under which this gene was differentially activated. However, comparison of secreted proteins from ST69 strains under high and low eilA activation failed to identify any ETT2 secreted substrates. The conservation of the genes encoding ETT2 in human pathogenic ST69 strains strongly suggests it has functional importance in infection, although its exact functional role remains obscure.\n\nImportanceOne of the commonest bacteria causing bloodstream infections in humans is Escherichia coli, which has a significant morbidity and mortality. Better understating of the mechanisms by which this microbe can invade blood could lead to more effective prevention and treatment. One mechanism by which some strains cause disease is by elaboration of a specialized secretion system, the type III secretion system (T3SS), encoded by the locus of enterocyte effacement (LEE). In addition to this well-defined T3SS, a second T3SS has been found in some E. coli strains termed E. coli type III secretion system 2 (ETT2). Most strains carry elements of the ETT2 locus, but with significant mutational attrition rendering it functionless. The significance of our work is that we have discovered that human bloodstream isolates of E. coli of sequence type 69 contain a fully intact ETT2 and associated genes, strongly suggesting its functional importance in human infection.

microbiology↗

In vitro determination of the CB1 efficacy of illicit synthetic cannabinoids

BACKGROUND AND PURPOSEThe morbidity and mortality associated with recreational use of synthetic cannabinoid receptor agonists (SCRAs) is a major health concern, and may involve over-activation of CB1 receptors. Thus, we sought to determine the efficacy of 13 SCRAs at CB1 using receptor depletion with the irreversible CB1 antagonist AM6544 followed by fitting the curve with the Black and Leff operational model to calculate efficacy.\n\nEXPERIMENTAL APPROACHReceptor depletion in mouse AtT-20 neuroblastoma cells stably expressing human CB1 was achieved by pre-treatment of cells with AM6544 (10 {micro}M, 60 mins). The CB1-mediated hyperpolarisation of AtT20 cells was measured using membrane potential dye. From data fit to the operational model, the efficacy (tau) and affinity (KA) parameters were obtained for each drug.\n\nKEY RESULTSAM6544 did not affect the potency or maximal effect of native somatostatin receptor-induced hyperpolarisation (Control, pEC50 9.13 {+/-} 0.05, Emax 38 {+/-} 1%; AM6544 treated pEC50 9.18 {+/-} 0.04, Emax 39 {+/-} 0.7%). The tau value of {triangleup}9-THC was 70-fold less than the reference CB-agonist CP55940, and 240-fold less than the highest efficacy SCRA, 5F-MDMB-PICA. Most of the SCRAs had about 50% of the efficacy of CP55940. There was no correlation between the tau and KA values for any SCRA.\n\nCONCLUSION AND IMPLICATIONSAll the SCRA tested showed substantially higher agonist activity at CB1 than {triangleup}9-THC, which may contribute to the adverse effects seen with these drugs but not {triangleup}9-THC, although the mechanisms underlying SCRA toxicity are still poorly defined.

pharmacology and toxicology↗