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Go, K.

Publications and source records attributed to Go, K..

7 recordsLinked to original sources

Reproductive history differentially shapes the neural response of middle-aged females to estradiol therapy after a metabolic challenge

BackgroundAdvancing age, the APOE{square}4 allele, and female sex are the top nonmodifiable risk factors for Alzheimers disease (AD). Female-specific experiences, such as parity and hormone therapy (HT) affect aging biomarkers such as metabolism and immune signaling and may even affect AD risk. Estradiol (E2), a common component of many HTs, affects cognition and brain health in aging females although this may vary depending on parity, genotype, and metabolic status. We hypothesized that prior parity influences brain and metabolic health, including response to E2, depending on APOE genotype. MethodsMiddle-aged female (10 month) wildtype (WT) or humanized (h) APOE{square}4 expressing rats, with different reproductive experience (nulliparous or primiparous) were fed a Western (WD) or standard diet (SD) for 2 months. In the second month, rats were given E2 or vehicle (oil) injections daily. Fear associative learning, plasma metabolic hormones, hippocampal inflammatory signalling, and neuroplasticity (neurogenesis, synaptic protein) were assessed. ResultsFemales fed a WD gained weight and displayed metabolic dysregulation, regardless of genotype. E2 treatment reduced WD-induced weight gain and reduced metabolic hormones, with stronger effects in WT rats. E2 treatment increased dorsal hippocampal inflammatory signalling selectively in primiparous hAPOE{square}4 females fed a WD. Previous parity increased neurogenesis and reduced certain cytokines in the hippocampus of middle-aged WT rats under a SD. Both E2 treatment and previous parity decreased dorsal neurogenesis in hippocampus of hAPOE{square}4 rats. In hAPOE{square}4 females, higher weight was associated with reduced contextual fear memory, an effect driven by primiparous females. In the cued fear conditioning task, hAPOE{square}4 females displayed better cued fear memory than WT, however, WD exposure reduced cued fear memory in this group. Together, this indicates that diet and weight gain may be more detrimental to associative memory in hAPOE{square}4 females and that E2 treatment has more favourable outcomes in WT rats. ConclusionsPrevious parity alters how females respond to E2 and metabolic stress in midlife. Primiparous hAPOE{square}4 females were especially vulnerable to the effects of WD and E2, exhibiting more inflammation, impaired memory, and reduced weight-loss. These findings highlight the importance of considering parity and genotype when evaluating midlife metabolic and cognitive risk. HighlightsO_LIEstradiol (E2) treatment reduced body weight gain under a Western diet (WD), with the most pronounced effects in wildtype primiparous rats. C_LIO_LIWD increased several metabolic hormones, and E2 treatment reduced several metabolic hormones after a WD in middle age, only in WT rats C_LIO_LIIncreased body weight impaired contextual associative memory in primiparous hAPOE{square}4 females. C_LIO_LIE2 treatment increased dorsal hippocampal inflammatory signalling in primiparous hAPOE{square}4 rats and the WD increased inflammatory signalling in primiparous WT rats. C_LIO_LIPrevious parity, but not E2 treatment, increased neurogenesis in WT rats only under standard diet conditions whereas a WD decreased neurogenesis based on genotype and previous parity C_LI Plain English SummaryAlzheimers disease (AD) causes general cognitive decline, and females are at higher risk than males, particularly those carrying the APOE{varepsilon}4 gene. Female-specific experiences, such as previous pregnancy (parity) and hormone therapy, as well as lifestyle factors like body weight and diet, may further influence AD risk. We examined how estradiol (E2), a hormone involved in the menstrual cycle, pregnancy, and some hormone therapies can affect memory, brain inflammation, synaptic plasticity (brain cell connectivity), and growth of new neurons (neurogenesis) in middle-aged female rats. We compared females with or without the APOE{varepsilon}4 gene and with or without prior parity, fed either a high-fat, high-sugar Western diet (WD) or a standard diet (SD). WD increased body weight and worsened metabolic health, but the strength of negative effects depended on genotype and pregnancy history. In females with the APOE{varepsilon}4 gene and prior parity, higher body weight was linked to poorer memory. hAPOE{varepsilon}4 females on SD showed better memory than non-carriers but this benefit disappeared on WD, suggesting WD and obesity are particularly detrimental for hAPOE{square}4 carriers with prior parity. WD-fed primiparous hAPOE{square}4 females treated with E2 also showed higher brain inflammation than other groups. Pregnancy history and E2 treatment were associated with more favourable outcomes in females without the genetic risk for AD and fed a standard diet. These findings highlight the importance of a personalized approach to hormone therapy and brain health in aging females. hAPOE{square}4 females with prior parity were most sensitive to the effects of diet. Together, this suggests genetic background, reproductive history, and diet interact to affect memory, inflammation, and neurogenesis, as well as the effects of E2 on these factors.

neuroscience↗

Heterogeneous Nuclear Ribonucleoprotein A1 as a Key Regulator in Pulmonary Arterial Hypertension Development

BackgroundAlthough plexiform lesion (PL) formation in severe pulmonary arterial hypertension (PAH) is a therapeutic target, the mechanisms underlying their formation have not been fully elucidated. This study aimed to identify candidate proteins involved in PL formation by examining differentially expressed proteins (DEPs) in PAH lesions. MethodsProteomic remodeling was assessed before and after the formation of PLs in a SU5416 combined with hypoxia (SuHx) rat model of severe PAH using laser-capture microdissection coupled with mass spectrometry. Unobstructed pulmonary arteries with medial hypertrophy (UMHPAs) and PLs from SuHx rats were subjected to qualitative and quantitative proteomics, revealing DEPs between these structures. ResultsWe identified 718 proteins with 58 DEPs, of which 31 were upregulated in UMHPAs and 27 were upregulated in PLs. Immunostaining confirmed that DEPs detected in our proteomic analysis were differentially expressed between UMHPAs and PLs. Among them, we focused on heterogeneous nuclear ribonucleoprotein A1 (hnRNPA1) as a candidate protein that may be strongly associated with PL formation because of its strong association with cell proliferation. siRNA knockdown of hnRNPA1 in hypoxia-treated pulmonary artery smooth muscle cells reduced pyruvate kinase M2 expression and significantly decreased proliferative capacity. Treatment of SuHx rats with hnRNPA1 inhibitors also suppressed pulmonary artery remodeling in PAH and PL formation. ConclusionsSeveral DEPs associated with PL formation but with unclear relevance to pulmonary artery remodeling in PAH were discovered. Among these, hnRNPA1, which was not detected in transcriptome analysis, may be important in PL formation. What are the Clinical Implications?The prognosis for pulmonary arterial hypertension (PAH) with plexiform lesions (PLs) is poor. Although PLs are therapeutic targets, the mechanisms of PL formation have not been fully elucidated, and there have been no direct examinations of proteomic remodeling before and after their formation. We identified several differentially expressed proteins (DEPs) that may be strongly associated with PL formation. Of these, heterogeneous nuclear ribonucleoprotein A1 (hnRNPA1) was examined as a candidate protein involved in PA remodeling in PAH and PLs. Inhibition of hnRNPA1 in a severe PAH model not only suppressed pulmonary artery remodeling in PAH but also reduced PL formation. Several DEPs involved in pulmonary artery remodeling in PAH may be of significant value in the search for new therapeutic targets.

cell biology↗

Conjugated GLP-1 and Estradiol Treatment as a Novel Treatment for Age-related Cognitive Decline in Males and Females

Middle age represents a critical window for metabolic and cognitive health, particularly in the context of rising obesity and diabetes rates. Glucagon-like peptide-1 (GLP-1)-based therapies, which regulate blood glucose and body weight, show sex-specific effects, with estradiol potentiating their metabolic benefits. However, research on GLP-1s cognitive and neuroprotective roles has largely been conducted in males. Here, we investigated the effects of GLP-1 conjugated to estradiol (GE2) on metabolism, cognition, cytokine levels and neurogenesis in the dentate gyrus of middle-aged male and female rats fed a standard (SD) or Western (WD) diet. In both sexes, WD increased body weight and plasma leptin levels, regardless of sex. GE2 treatment led to weight loss, enhanced cued and contextual fear memory, reduced cytokine levels in the hippocampus in SD rats, and increased neurogenesis in the dorsal dentate gyrus (DG), regardless of sex. Sex-specific differences were observed in fat distribution, glucose regulation, central cytokine levels, and neuroplasticity after WD and GE2 treatment. In females only, GE2 reduced visceral (gonadal) fat, reduced cytokines in the dorsal hippocampus, and improved basal blood glucose in response to a WD. In males only, GE2 restored neurogenesis in the DG after WD exposure, and reduced cytokine levels in the amygdala. These findings suggest that although WD increased body weight and GE2 improved associative learning in both sexes, both WD and GE2 had differential affects on metabolic hormones, insulin regulation, cytokine levels and neuroplasticity. Our findings underscore the importance of sex-specific approaches in metabolic and neuroprotective therapeutics in middle age.

neuroscience↗

Activity of estrogen receptor beta expressing neurons in the medial amygdala regulates preference towards receptive females in male mice.

The processing of information regarding the sex and reproductive state of conspecific individuals is critical for successful reproduction and survival in males. Generally, male mice exhibit a preference towards sexually receptive (RF) over non-receptive females (XF) or gonadally intact males (IM). Previous studies suggested the involvement of estrogen receptor beta (ER{beta}) expressed in the medial amygdala (MeA) in male preference towards RF. To further delineate the role played by ER{beta} in the MeA in the neuronal network regulating male preference, we developed a new ER{beta}-iCre mouse line using the CRISPR-Cas9 system. Fiber-photometry Ca2+ imaging revealed that ER{beta} expressing neurons in the postero-dorsal part of the MeA (MeApd-ER{beta}+ neurons) were more active during social investigation towards RF compared to copresented XF or IM mice in a preference test. Chemogenetic inhibition of MeApd-ER{beta}+ neuronal activity abolished a preference to RF in "RF vs. XF", but not "RF vs. IM", tests. Analysis with cre-dependent retrograde tracing viral vectors identified the principal part of the bed nucleus of stria terminalis (BNSTp) as a primary projection site of MeApd-ER{beta}+ neurons. Fiber-photometry recording in the BNSTp during a preference test revealed that chemogenetic inhibition of MeApd-ER{beta}+ neurons abolished differential neuronal activity of BNSTp cells as well as a preference to RF against XF but not against IM mice. Collectively, these findings demonstrate for the first time that MeApd-ER{beta}+ neuronal activity is required for expression of receptivity-based preference (i.e., RF vs XF) but not sex-based preference (i.e., RF vs IM) in male mice. Significance StatementIn this study, by introducing a new Cre mice line for ER{beta}+ cells, we described the function of MeApd-ER{beta}+ neurons and characteristics of their neuronal activity during preference tests. Using fiber photometry and DREADD techniques we have found MeApd-ER{beta}+ neurons have a specific role in receptivity-based (receptive female vs. non-receptive female) preference but not in sexbased (receptive female vs. intact male) preference in male mice. We have also described this specific role of MeApd-ER{beta}+ neurons is achieved by regulating the neuronal activity of downstream BNSTp neurons during receptivity-based, but not sex-based, preference tests. Our findings contribute to a better understating of the function of estrogen receptor expressing neurons in the neuronal network for the male-typical reproductive behaviors.

neuroscience↗

Identification of an inhibitory pocket in falcilysin bound by chloroquine provides a new avenue for malaria drug development

Despite their widespread use, our understanding of how many antiparasitic drugs work remains limited. We used mass-spectrometry based cellular thermal shift assay (MS-CETSA) to identify possible protein targets of several malaria drugs and drug candidates. We found that falcilysin (FLN) is a common target for several quinoline drugs including chloroquine and mefloquine, as well as drug candidates MK-4815, MMV000848 and MMV665806. At pH 7.5, these compounds all inhibit FLN proteolytic activity with IC50 values ranging from 1.6 to 67.9 {micro}M. Their interaction with FLN was systematically probed by isothermal titration calorimetry and X-ray crystallography, revealing a shared hydrophobic pocket in the catalytic chamber of the enzyme. Characterization of transgenic cell lines with depleted FLN expression demonstrated statistically significant increases in susceptibility towards chloroquine, mefloquine, MK-4815 and MMV000848. Taken together, our findings point to a multimodal mechanism of action for several commonly used anti-malaria drugs. Importantly, a common allosteric pocket of FLN appears amenable to inhibition, providing a structural basis to guide the development of novel drugs against malaria.

microbiology↗

Postpartum corticosterone and fluoxetine shift the tryptophan-kynurenine pathway in dams

Perinatal depression (PND) affects 15% of mothers. Selective serotonin reuptake inhibitors (SSRIs) are currently the first-line of treatment for PND but are not always efficacious. Previously, we found significant reductions in plasma tryptophan concentrations and higher hippocampal proinflammatory cytokine, IL-1b levels, due to maternal SSRI treatment. Both inflammation and tryptophan-kynurenine metabolic pathway (TKP) are associated with SSRI efficacy in individuals with major depressive disorder (MDD). TKP is divided into neuroprotective and neurotoxic pathways. Higher metabolite concentrations of the neurotoxic pathway are associated with depression onset and implicated in SSRI efficacy. Metabolites in TKP were investigated in a rodent model of de novo postpartum depression (PPD) given treatment with the SSRI, fluoxetine (FLX). Dams were administered corticosterone (CORT) (40mg/kg, s.c.), and treated with the SSRI, fluoxetine (FLX) (10mg/kg, s.c.), during the postpartum for 22 days after parturition. Plasma TKP metabolite concentrations were quantified on the last day of treatment. Maternal postpartum CORT increased neurotoxic metabolites and co-enzyme/cofactors in dams (3-hydroxykynurenine, 3-hydroxyanthranilic acid, vitamin B2, flavin adenine dinucleotide). The combination of both CORT and FLX shifted the neuroprotective-to-neurotoxic ratio towards neurotoxicity. Postpartum FLX decreased plasma xanthurenic acid concentrations. Together, our data indicate higher neurotoxic TKP expression due to maternal postpartum CORT treatment, similar to clinical presentation of MDD. Moreover, maternal FLX treatment showed limited efficacy to influence TKP metabolites, which may correspond to its limited efficacy to treat depressive-like endophenotypes. Overall suggesting changes in TKP may be used as a biomarker of de novo PPD and antidepressant efficacy and targeting this pathway may serve as a potential therapeutic target. HighlightsO_LITryptophan-kynurenine pathway (TKP) is altered by postpartum corticosterone (CORT) C_LIO_LIPostpartum CORT upregulated neurotoxic more metabolites (3HK, 3HAA) C_LIO_LIPostpartum fluoxetine (FLX) increased xanthurenic acid concentrations C_LIO_LIPostpartum CORT and FLX together shifted the TKP balance towards neurotoxicity C_LI

neuroscience↗

Postpartum fluoxetine increased maternal hippocampal IL-1β and decreased plasma tryptophan: clues for efficacy

Perinatal depression (PND) affects approximately 15% of women, and de novo postpartum depression affects approximately 40% of PND cases. Selective serotonin reuptake inhibitors (SSRIs) are a common class of antidepressants prescribed to treat PND. However, the safety and efficacy of SSRIs have been questioned in both clinical and preclinical research. Here, using a preclinical rodent model of postpartum depression, we aim to better understand neuroinflammatory cytokines and tryptophan mechanisms that may be related to SSRIs efficacy. Rodent dams were treated with high corticosterone (CORT; 40mg/kg, s.c.) for 21 days in the postpartum period to simulate depressive-like behaviors in the late postpartum period. Concurrently, a subset of dams was treated with the SSRI, fluoxetine (FLX; 10mg/kg, s.c.), in the postpartum period. We showed, consistent with previous studies, that although maternal FLX treatment prevented CORT-induced disturbances in maternal care behavior during the early postpartum, it failed to prevent the expression of CORT-induced depressive-like behavior in the late postpartum. Furthermore, FLX treatment, regardless of CORT treatment, increased maternal hippocampal IL-1{beta} and decreased maternal plasma tryptophan levels, plasma tryptophan, 4-pyridoxic acid, and pyridoxal concentrations. Maternal CORT treatment reduced maternal hippocampal TNF- and IFN-{gamma} levels. Our work suggests that the limited efficacy of FLX in the late postpartum may be associated with elevated levels of the proinflammatory cytokine IL-1{beta} in the maternal hippocampus, decreased plasma tryptophan concentration, and changes in vitamin B6 dependent tryptophan-kynurenine pathway. These findings suggest novel pathways for improving SSRI efficacy in alleviating perinatal depression. HIGHLIGHTSO_LIPostpartum fluoxetine (FLX) increased interleukin-1{beta} levels in hippocampus C_LIO_LIPostpartum corticosterone (CORT) decreased TNF- and IFN-{gamma} in the hippocampus C_LIO_LIPostpartum FLX did not prevent CORT-induced depressive-like behavior C_LIO_LIPostpartum FLX prevented CORT-induced changes in maternal behavior C_LIO_LIPostpartum FLX decreased plasma tryptophan, 4-pyridoxic acid, and pyridoxal levels C_LI

neuroscience↗