Micro-Morphology characterization and HS-SPME-GC-MS Analysis of Floral parts of Quararibea funebris (La Llave) Vischer, traditionally known as Rosita de Cacao.

The flowers of Quararibea funebris are used to make a traditional drink called tejate, to which they add aroma, flavor and consistency. The study aims to profile the morphoanatomy of the floral parts of Q. funebris and analyze the changes in its volatile chemical composition during the drying process from 0 to 180 days by HS-SPME-GC-MS. The calyx, corolla, androecium, and gynoecium have distinct characteristics, such as non-glandular fused stellate trichomes, calcium oxalate crystals, and large secretory ducts. Histochemical localization reveals the presence of mucilage and total lipids in all parts of the flower. The chemical analysis of the essential oil, extracted from the flowers, showed that transfarnesol and geraniol were the most abundant compounds, with a yield of 0.04 %. HS-SPME analysis indicated that fresh flowers had a more complex composition than dried ones. In total, 31 components were identified. Nonanal and geranyl acetone were found to be distinctive components of dried flowers. Microscopic examination helps in identifying and authenticating raw materials and also reveals the presence of secretory ducts in all floral parts, which is a distinctive feature. The chemical profile of volatiles provides an important parameter for the evaluation of the quality of Rosita de Cacao raw materials.

Diligustilide releases H2S and stabilizes S-nitrosothiols in ethanol-induced lesions on rat gastric mucosa.

(Z,Z')-Diligustilide (DLG) or levistolide A is a dimeric phthalide isolated from Ligusticum porteri (Osha), the roots of which are used in the traditional treatment of many diseases including gastric aches. However, its action has not been completely elucidated. We analyzed the contributions of hydrogen sulfide and S-nitrosothiols to the action of DLG. Animals were pretreated with freshly formed in vitro nitrosothiol using Na2S and sodium nitroprusside to elucidate participation in the action of DLG. We also evaluated the production of H2S in vivo and in real time on the stomach via a specific electrode introduced into the stomachs of anaesthetized animals pretreated with DLG. Treatment with 10 mg/kg DLG increases gastric H2S production in vivo from 7.8 ± 0.81 ppm to 13.1 ± 3.01 ppm and prevents the decrease in gastric injury caused by absolute ethanol. In addition, it maintains endogenous concentrations of GSH and NO·. Exogenous S-nitrosothiols protect the gastric mucosa from damage, suggesting that the action of DLG might be associated with S-nitrosothiol and H2S formation.

Effect of N-Benzylpiperazine, Its Metabolite N-Benzylethylenediamine, and Its Disubstituted Analogue N,N'-Dibenzylpiperazine on the Acquisition, Formation, and Consolidation of Memory in Mice.

BACKGROUND: N-benzylpiperazine (BZP) belongs to a class of piperazine derivatives (PZDs) that have emerged as recreational drugs. These compounds increase the release of dopamine and serotonin. BZP mimics the psychoactive effects of 3,4-methylenedioxymethylamphetamine. BZP is metabolized to N-benzylethylenediamine (BEDA) and benzylamine. The compound N,N'-dibenzylpiperazine (DBZP) is obtained as a byproduct during the synthesis of BZP. Some PZDs have shown effects on memory; however, there are no previous reports on the activity of BZP, BEDA, and DBZP on memory or on a description of their neuropharmacological profile. We evaluated the effects of these compounds on acquisition, formation, and consolidation memory and explored their neuropharmacological profile in mice. METHODS: We used the passive avoidance test to evaluate the nootropic effect and for memory experiments. We also evaluated the sedative, myo-relaxant, motor coordination, anxiogenic, and locomotor activity of these compounds. RESULTS: We showed that BZP, its metabolite BEDA, and the disubstituted analogue DBZP enhance the memory and show anxiogenic effects. BZP, as well as DBZP but not BEDA, showed a strong myo-relaxant effect without impairing motor coordination. CONCLUSIONS: BZP and BEDA enhanced the acquisition and consolidation of memory, whereas DBZP only enhances the acquisition of the memory. BEDA and DBZP have an anxiogenic profile similar to that of BZP. BEDA and DBZP represent new psychoactive compounds with the potential to be new BZP-like recreational entities.

Anti-Hyperglycemic Activity of Major Compounds from Calea ternifolia.

Demethylisoencecalin (1) and caleins A (4) and C (5) (3.16-31.6 mg/kg, p.o.), the major components from an infusion of Calea ternifolia controlled postprandial glucose levels during an oral sucrose tolerance test (OSTT, 3 g/kg) in normal and nicotinamide/streptozotocin (NA/STZ, 40/100 mg/kg) hyperglicemic mice. The effects were comparable to those of acarbose (5 mg/kg). During the isolation of 1, 4, and 5, four additional metabolites not previously reported for the plant, were obtained, namely 6-acetyl-5-hydroxy-2-methyl-2-hydroxymethyl-2H-chromene (3), herniarin (6), scoparone (7), and 4',7-dimethylapigenin (8). In addition, the structure of calein C (5) was confirmed by X-ray analysis. Pharmacological evaluation of the essential oil of the species (31.6-316.2 mg/kg, p.o.) provoked also an important decrement of blood glucose levels during an OSTT. Gas chromatography coupled with mass spectrometry (GC-MS) analysis of the headspace solid phase microextraction (HS-SPME)-adsorbed compounds and active essential oil obtained by hydrodistillation revealed that chromene 1 was the major component (19.92%); sesquiterpenes represented the highest percentage of the essential oil content (55.67%) and included curcumene (7.10%), spathulenol (12.95%) and caryophyllene oxide (13.0%). A suitable High Performance Liquid Chromatography (HPLC) method for quantifying chromenes 1 and 6-hydroxyacetyl-5-hydroxy-2,2-dimethyl-2H-chromene (2) was developed and validated according to standard protocols.

Mechanism of action of relaxant effect of Agastache mexicana ssp.mexicana essential oil in guinea-pig trachea smooth muscle.

CONTEXT: Agastache mexicana ssp. mexicana (Kunth) Lint & Epling (Lamiaceae), popularly known as 'toronjil morado', is used in Mexican traditional medicine for the treatment of several diseases such as hypertension, anxiety and respiratory disorders. OBJECTIVE: This study investigates the relaxant action mechanism of A. mexicana ssp. mexicana essential oil (AMEO) in guinea-pig isolated trachea model. MATERIALS AND METHOD: AMEO was analyzed by GC/MS. The relaxant effect of AMEO (5-50 µg/mL) was tested in guinea-pig trachea pre-contracted with carbachol (3 × 10 - 6 M) or histamine (3 × 10 - 5 M) in the presence or absence of glibenclamide (10 - 5 M), propranolol (3 × 10 - 6 M) or 2',5'-dideoxyadenosine (10 - 5 M). The antagonist effect of AMEO (10-300 µg/mL) against contractions elicited by carbachol (10 - 15-10 - 3 M), histamine (10 - 15-10 - 3 M) or calcium (10-300 µg/mL) was evaluated. RESULTS: Essential oil composition was estragole, d-limonene and linalyl anthranilate. AMEO relaxed the carbachol (EC50 = 18.25 ± 1.03 µg/mL) and histamine (EC50 = 13.3 ± 1.02 µg/mL)-induced contractions. The relaxant effect of AMEO was not modified by the presence of propranolol, glibenclamide or 2',5'-dideoxyadenosine, suggesting that effect of AMEO is not related to ß2-adrenergic receptors, ATP-sensitive potassium channels or adenylate cyclase activation. AMEO was more potent to antagonize histamine (pA2' = -1.507 ± 0.122) than carbachol (pA2' = -2.180 ± 0.357). Also, AMEO antagonized the calcium chloride-induced contractions. CONCLUSION: The results suggest that relaxant effect of AMEO might be due to blockade of calcium influx in guinea-pig trachea smooth muscle. It is possible that estragole and d-limonene could contribute majority in the relaxant effect of AMEO.

Antineuropathic effect of 7-hydroxy-3,4-dihydrocadalin in streptozotocin-induced diabetic rodents.

BACKGROUND: Painful neuropathy is the most common and debilitating complication of diabetes and results in hyperalgesia and allodynia. Hyperglycemia clearly plays a key role in the development and progression of diabetic neuropathy. Current therapeutic approaches are only partially successful and they are only thought to reduce the pain associated with peripheral neuropathy. Some natural products offer combined antioxidant, anti-inflammatory and antinociceptive properties that may help to treat in a more integrative manner this condition. In this regard, the purpose of this study was to investigate the antineuropathic effect of 7-hydroxy-3,4-dihydrocadalin in streptozotocin-induced diabetic rats and mice without glucose control as well as the possible mechanism of action involved in this effect. METHODS: Rats and mice were injected with 50 or 200 mg/kg streptozotocin, respectively, to produce hyperglycemia. The formalin test and von Frey filaments were used to assess the nociceptive activity. Rota-rod was utilized to measure motor activity and malondialdehyde assay to determine anti-oxidative properties. RESULTS: After 3 weeks of diabetes induction, chemical hyperalgesia was observed in streptozotocin-injected rats. Oral acute administration of 7-hydroxy-3,4-dihydrocadalin (0.3-30 mg/kg) decreased in a dose-dependent manner formalin-evoked hyperalgesia in diabetic rats. In addition, methiothepin (non-selective 5-HT receptor antagonist, 1 mg/kg, i.p.) and ODQ (guanylyl cyclase inhibitor, 2 mg/kg, i.p.), but not naltrexone (opioid receptor antagonist, 1 mg/kg, s.c.), prevented 7-hydroxy-3,4-dihydrocadalin-induced antihyperalgesic effect. The anti-hyperalgesic effect of 7-hydroxy-3,4-dihydrocadalin was similar to that produced by pregabalin (10 mg/kg, p.o.). Furthermore, oral acute administration of 7-hydroxy-3,4-dihydrocadalin (30 mg/kg) reduced streptozotocin-induced changes in malondialdehyde concentration from plasma samples. Unlike pregabalin, 7-hydroxy-3,4-dihydrocadalin did not affect motor activity. Six weeks after diabetes induction, tactile allodynia was observed in the streptozotocin-injected rats. At this time, oral administration of 7-hydroxy-3,4-dihydrocadalin (30 mg/kg) or pregabalin (10 mg/kg) reduced in a similar way tactile allodynia in diabetic rats. Finally, chronic oral administration of 7-hydroxy-3,4-dihydrocadalin (30-300 mg/kg, 3 times/week, during 6 weeks), significantly prevented the development of mechanical hyperalgesia and allodynia in streptozotocin-induced diabetic mice. CONCLUSIONS: Data suggests that 7-hydroxy-3,4-dihydrocadalin has acute and chronic effects in painful diabetic neuropathy. This effect seems to involve antioxidant properties as well as activation of 5-HT receptors and inhibition of guanylyl cyclase enzyme.

Study on action mechanism of 1-(4-methoxy-2-methylphenyl)piperazine (MMPP) in acquisition, formation, and consolidation of memory in mice.

In the present study, the mechanism of action of MMPP (1-(4-methoxy-2-methylphenyl) piperazine) in the acquisition (pretraining administration), formation (posttraining administration), and consolidation (pretest administration) of memory was assessed in the passive avoidance test using a short- and long-term memory protocol in mice. MMPP modified avoidance in the acquisition and formation of memory protocols but not in the consolidation protocol. Scopolamine (0.1 mg/kg i.p.), dizocilpine (0.003 mg/kg i.p.), and buspirone (0.1 mg/kg i.p.) completely inhibited MMPP-induced effects on memory acquisition and partially inhibited memory formation in the short-term but not long-term paradigm. This suggested that cholinergic, N-methyl-D-aspartate (NMDA) and 5-hydroxytryptamine-1A (5-HT1A ) receptors were implicated in the MMPP-induced improvements in memory. The sedative, anxiolytic, motor impairment, myorelaxant, and anticonvulsive (pentylenetetrazole-induced seizures) properties of MMPP were also assessed with the compound only showing a nondose-dependent myorelaxation. These results suggest that MMPP can enhance acquisition and formation, but not consolidation, of memory in short-term and long-term protocol via cholinergic, NMDA-glutamatergic, and 5-HT1A receptors.

Chemical profiling and quantification of flavones in several Pseudognaphalium and Gnaphalium species of Mexican gordolobo using UHPLC/PDA/MS.

The inflorescences of the Mexican gordolobo are used as a folk medicine to treat various respiratory diseases. Currently, the botanical species that bear the name Mexican gordolobo belong to the genera Gnaphalium and Pseudognaphalium. Despite a long history of traditional use, most Mexican gordolobo species have never been fully chemically characterized, and the range of constituents in the species has not been comprehensively reported. To establish a quality control and chemical characterization method, a total of 49 samples belonging to 18 species of Pseudognaphalium and four species of Gnaphalium were studied. Nine flavones were quantified using a UPLC-PDA method. The method was validated in terms of linearity (R2 > 0.99), precision (intra- and inter-day: 0.1-3.9%), accuracy (96-103%), detection limit (10 ng/mL), limit of quantification (25 ng/mL) and robustness. 3-Methylquercetin, luteolin, quercetin, 3,5-dihydroxy-6,7,8-trimethoxyflavone, apigenin and gnaphaliin A were present at relatively high levels in most of the samples analyzed. The samples of P. oxyphyllum and P. liebmannii showed the highest content of the 9 compounds analyzed. Whereas the samples of the 5 species of Gnaphalium showed the lowest levels, including non-detectable, of the 9 compounds quantified. This marks an important difference with Pseudognaphalium species. Furthermore, using UHPLC-ESI-QToF data with targeted and non-targeted approaches, 57 compounds, were identified in Mexican gordolobo samples. Flavonoids were the main group of compounds found in Mexican gordolobo.

Synergistic Assembly of 1DZnO and Anti-CYFRA 21-1: A Physicochemical Approach to Optical Biosensing.

Objective: We conducted a comprehensive physicochemical analysis of one-dimensional ZnO nanowires (1DZnO), incorporating anti-CYFRA 21-1 immobilization to promote fast optical biomarker detection up to 10 ng ml-1. Impact Statement: This study highlights the effectiveness of proof-of-concept 1DZnO nanoplatforms for rapid cancer biomarker detection by examining the nanoscale integration of 1DZnO with these bioreceptors to deliver reliable photoluminescent output signals. Introduction: The urgent need for swift and accurate prognoses in healthcare settings drives the rise of sensitive biosensing nanoplatforms for cancer detection, which has benefited from biomarker identification. CYFRA 21-1 is a reliable target for the early prediction of cancer formation that can be perceptible in blood, saliva, and serum. However, 1DZnO nanostructures have been barely applied for CYFRA 21-1 detection. Methods: We assessed the nanoscale interaction between 1DZnO and anti-CYFRA 21-1 antibodies to develop rapid CYFRA 21-1 detection in two distinct matrices: PhosphateBuffered Saline (PBS) buffer and artificial saliva. The chemical modifications were tracked utilizing Fourier transform infrared spectroscopy, while transmission electron microscopy and energy dispersive spectroscopy confirmed antigen-antibody interplay over nanostructures. Results: Our results show high antibody immobilization efficiencies, affirming the effectiveness of 1DZnO nanoplatforms for rapid CYFRA 21-1 testing within a 5-min detection window in both PBS and artificial saliva. Photoluminescence measurements also revealed distinct optical responses across biomarker concentrations ranging from 10 to 1,000 ng ml-1. Conclusion: Discernible PL signal responses obtained after 5 min affirm the potential of 1DZnO nanoplatforms for further advancement in optical biomarker detection for application in early cancer prognosis.

Evaluation of Mechanical Properties of Composite Material with a Thermoplastic Matrix Reinforced with Cellulose Acetate Microfibers.

Low-density polyethylene (LDPE) has been widely used in various applications due to its flexibility, lightness, and low production cost. However, its massive use in disposable products has raised environmental concerns, prompting the search for more sustainable alternatives. This study aims to investigate the mechanical properties achievable in a composite material utilizing low-density polyethylene (LDPE), potato starch (PS), and cellulose microfibrils (MFCA) at loadings of 0.05%, 0.15%, and 0.30%. Initially, the cellulose acetate microfibrils (MFCA) were produced via an electrospinning process. Subsequently, a dispersive mixture of the aforementioned materials was created through the extrusion and pelletizing process to form pellets. These pellets were then molded by injection molding to produce test specimens in accordance with ASTM D 638, the standard for tensile strength testing. The evaluation of the properties was conducted through mechanical tensile tests (ASTM D638), hardness tests (ASTM D 2240), melt flow index (ASTM D1238), and scanning electron microscopy (SEM). This study determined the influence of cellulose acetate microfibril loadings below 0.3% as reinforcement within a thermoplastic LDPE matrix. It was demonstrated that these microfibrils, due to their length-to-diameter ratio, contribute to an enhancement in the mechanical properties.

Brain Evaluation by Dual PET/CT with [18F] FDOPA and [18F] FDG in Differential Diagnosis of Parkinsonian Syndromes.

Parkinsonian syndromes are considered clinicopathological conditions that are challenging to diagnose. Molecular imaging with [18F]-FDOPA and [18F]-FDG contributes to a more accurate clinical diagnosis by evaluating presynaptic dopaminergic pathways and glucose metabolism, respectively. The aim of this study was to correlate diagnoses made from dual PET/CT with the initial clinical diagnoses, as well as during follow-ups in patients with Parkinsonian syndromes. A secondary objective was to describe the imaging findings. Methods: A total of 150 patients with a clinical diagnosis of neurodegenerative Parkinsonism were evaluated using dual PET/CT. Clinically, 82% were diagnosed with PD, while the remaining 18% had an atypical Parkinsonism. Results: Using dual PET/CT, the most frequent diagnosis was PD in 67% of the patients, with the rest being diagnosed with an atypical Parkinsonism. In an agreement analysis between the initial clinical diagnosis and the imaging diagnosis by dual PET/CT, a concordance of 94.1% (n = 95) was observed for PD. In the remaining patients, the clinical diagnosis differed from that suggested by dual PET/CT, with atypical Parkinsonian syndromes being diagnosed as DLB in 40% (n = 4), PSP in 46.7% (n = 7), MSA-C in 75% (n = 6), MSA-P in 70% (n = 7), and CBD in 66.7% (n = 4). A total of 38.66% (n = 58) of patients were followed up (median follow-up of 27 months), with a Kappa coefficient of 0.591 (p < 0.001), suggesting substantial agreement. Conclusions: Dual FDOPA-FDG PET/CT demonstrated moderate agreement with the initial clinical diagnosis of Parkinsonism and moderate to substantial agreement during follow-up. This dual technique, therefore, stands out in differentiating between types of Parkinsonisms.

Flavones isolated from Pseudognaphalium liebmannii with tracheal smooth muscle relaxant properties.

The inflorescences of Pseudognaphalium liebmannii are used as folk medicine to treat various respiratory diseases. In this work, we report the isolation of seven known flavones: 5-hydroxy-3,7-dimethoxyflavone 1, 5,8-dihydroxy-3,7-dimethoxyflavone 2, 5,7-dihydroxy-3,8-dimethoxyflavone 3 (gnaphaliin A), 3,5-dihydroxy-7,8-dimethoxyflavone 4 (gnaphaliin B), 3,5-dihydroxy-6,7,8-trimethoxyflavone 5, 3,5,7-trimethoxyflavone 6 and 3-O-methylquercetin 7. All these flavones except 1 and 6 showed a relaxant effect on guinea pig tracheal preparation with EC50 between 69.91 ± 15.32 and 118.72 ± 7.06 µM. Aminophylline (EC50 = 122.03 ± 7.05 µM) was used as a relaxant reference drug. The active flavones shifted the concentration-response curves of forskolin and nitroprusside leftward, and significantly reduced the EC50 values of these drugs. Furthermore, these flavones dose-dependently inhibited phosphodiesterase (PDE) in an in vitro assay. This reveals that the inflorescences of P. liebmannii contain several flavones with relaxant effect on airway smooth muscle and with PDEs inhibition that contribute to supporting the anti-asthmatic traditional use.

Synthesis, docking study and relaxant effect of 2-alkyl and 2-naphthylchromones on rat aorta and guinea-pig trachea through phosphodiesterase inhibition.

Chromone (4), which form the base structure of various flavonoids isolated as natural products, is capable of relaxing smooth muscle. This is relevant to the treatment of high blood pressure, asthma and chronic obstructive pulmonary disease. The former disorder involves the contraction of vascular smooth muscle (VSM), and the latter two bronchoconstriction of airway smooth muscle (ASM). One of the principal mechanisms by which flavonoids relax muscle tissue is the inhibition of phosphodiesterases (PDEs), present in both VSM and ASM. Therefore, a study was designed to analyze the structure-activity relationship of chromone derivatives in vaso- and bronchorelaxation through the inhibition of PDE. Docking studies showed that these chromones bind at the catalytic site of PDEs. Consequently, we synthesized analogs of chromones substituted at position C-2 with alkyl and naphthyl groups. These compounds were synthesized from 2-hydroxyacetophenone and acyl chlorides in the presence of DBU and pyridine, modifying the methodology reported for the synthesis of 3-acylchromones by changing the reaction temperature from 80 to 30°C and using methylene chloride as solvent, yielding the corresponding phenolic esters 10a-10h. These compounds were cyclized with an equivalent of DBU, pyridine as solvent, and heated at reflux temperature, yielding the chromones 11a-11h. Evaluation of the vasorelaxant effect of 4, 11a-11h on rat aorta demonstrated that potency decreases with branched alkyl groups. Whereas the EC50 of compound 11d (substituted by an n-hexyl group) was 8.64±0.39 µM, that of 11f (substituted by an isobutyl group) was 14.58±0.64 µM. Contrarily, the effectiveness of the compound is directly proportional to the length of the alkyl chain, as evidenced by the increase in maximal effect of compound 11c versus 11d (66% versus 100%) and 11e versus 11f (60% versus 96%). With an aromatic group like naphthyl as the C-2 substituent, the effectiveness was only 43%. All compounds tested on guinea pig trachea showed less than 55% effectiveness. Compounds 4, 11a-11h were evaluated as PDE inhibitors in vitro, with 11d showing the greatest effect (73%), corroborating the importance of a long alkyl chain, which inhibits the decomposition of cGMP. Docking studies showed that the compound 11d was selective for the inhibition of PDE-5.

Determination of biflavonoids in four Mexican species of Selaginella by HPLC.

The genus Selaginella comprises several species, some of which grow on the American continent. Among these species, S. nothohybrida Valdespino, S. lepidophylla Hook et Grev, S. pallescens (Presl) Spring, and S. reflexa Underw. are found in several states of the Mexican Republic. The aforementioned three species are used medicinally, typically to treat renal disorders. This paper describes the development of an HPLC-UV method for the determination of amentoflavone (1), robustaflavone (2), and (2S)-2,3-dihydrorobustaflavone (3) as major components of the above-mentioned species of Selaginella. Components 1, 2, and 3 were quantitatively determined using an XBridge Waters C18 5 microm column, with a gradient system consisting of mixtures of acetonitrile and water with 0.4% acetic acid. The flow rate was 0.4 mL/min, with UV detection at 367 nm. LOD and LOQ values were in the range of 0.025 to 0.216 microg/mL. Compounds 1, 2, and 3 showed good linearity in the 1.2 to 18 microg/mL range; recovery was within 98.2 and 101.9% for all three cases. Compounds 1 and 2 were detected in all eight samples; their concentration ranged from 0.35 to 1.79 mg/g of plant. Thus, compounds 1 and 2 could be used as markers for S. nothohybrida, S. lepidophylla, S. pallescens, and S. reflexa. In addition, trehalose was detected in all samples as two peaks at 1.5 and 2.0 min. The HPLC method described here was shown to be reliable, reproducible, and accurate and can be used for QC of Selaginella medicinal materials.

Toxic rather than neuropharmacological effect of Ternstroemia sylvatica fruits and identification of 28-O-[ß-l-6-rhamnopyranosyl]-R1-barrigenol as a new compound with toxic effects in mice.

CONTEXT: Fruits of Ternstroemia sylvatica Schltdl. and Cham. (Theaceae) are used in Mexican traditional medicine to alleviate anxiety, sleep disorders and seizures; however, the active principles have not been identified. OBJECTIVE: To identify the neuroactive principles of T. sylvatica fruits using neuropharmacological tests on mice. MATERIALS AND METHODS: The methanol and aqueous extracts of pericarp or seeds of T. sylvatica fruits were intraperitoneally administered (1-562 mg/kg, single doses) to mice. The exploratory cylinder, hole board, open field, Rota-rod and sodium pentobarbital-induced hypnosis tests were used to evaluate the CNS depressant effect after 30 min single administration of extracts. From aqueous seeds extract, triterpene glycoside 28-O-[ß-l-6-rhamnopyranosyl]-R1-barrigenol was isolated an active compound. RESULTS: Crude extracts of T. sylvatica fruits, separated from seed and pericarp, showed sedative effect in mice. The aqueous (ED50 = 4.9 ± 0.8 mg/kg) seed extracts is the most active among them. This extract also decrease locomotor activity and disrupt motor coordination of mice. This extract was also the most toxic extract (LD50 = 5.0 ± 1.4 mg/kg; i.p.). The triterpene glycoside 28-O-[ß-l-6-rhamnopyranosyl]-R1-barrigenol was identified in this extract as one of the active sedative compounds (ED50 = 0.12 ± 0.01 mg/kg) also with toxic effect (LD50 = 1.11 ± 0.23 mg/kg). CONCLUSION: The results suggest that T. sylvatica fruits has toxic activity rather than CNS depressant activity in mice and that this effect might be related to the presence of 28-O-[ß-l-6-rhamnopyranosyl]-R1-barrigenol, one of the active principles of T. sylvatica fruits with sedative and toxic effect.

"Eritadenine as a regulator of anxiety Disorders: An experimental and docking Approach".

Uncertainty persists regarding the specific chemical causal factors and their corresponding behavioral effects in anxiety disorders. Commonly employed first-line treatments for anxiety target G protein-coupled receptors (GPCRs), including inhibitors of monoaminergic systems. Alternatively, emerging natural bioactive strategies offer potential for mitigating adverse effects. Recent investigations have implicated adenosine in anxiety-triggering mechanisms, while eritadenine, an adenosine analog derived from Shiitake mushroom, has displayed promising attributes. This study explores eritadenine's potential as a bioactive substance for anxiety disorders in mice, employing behavioral tests, pentobarbital-sleep induction, and molecular docking. Behavioral test results reveal a pronounced anxiolytic and sedative-hypnotic pharmacological effect of eritadenine. Our findings suggest that eritadenine may modulate locomotor functions mediated by adenosine receptors, with a stronger affinity for binding to A2AAR over A1AR, thus eliciting these effects.

Gastroprotective effect methanol extract of Caesalpinia coriaria pods against indomethacin- and ethanol-induced gastric lesions in Wistar rats.

ETHNOPHARMACOLOGICAL RELEVANCE: Caesalpinia coriaria (Jacq.) Willd is widely used as a traditional medinal plant in Mexico for protective and healing purposes and the treatment of gastrointestinal diseases. AIM OF THE STUDY: To investigate the gastroprotective effect of extract of Caesalpinia coriaria pods against ethanol-induced and indomethacin-induced gastric lesion models, its anti-inflammatory and antioxidative activities, and its main compounds through LC-MS analysis. MATERIALS AND METHODS: Male Wistar rats were orally administered a methanol extract obtained from the pods of C. coriaria at doses of 10, 30, 100, and 300 mg/kg prior to inducing gastric lesions with ethanol or indomethacin. Gastric mucosal lesions were evaluated by macroscopic and histopathological alterations. Determination of prostaglandin E2 (PGE2), alpha tumor necrosis factor (TNF-α), leukotriene B4 (LTB4), nitrites/nitrates, superoxide dismutase (SOD), and H2S gastric levels were investigated. Its main compounds of the active extract through LC-MS analysis. RESULTS: Phenolic compounds were identified as major components of methanol extract. LC-MS analysis identified 15 constituents, and the significant compounds were gallic acid, 3-O-galloylquinic acid, digalloylglucose, tetragalloylglucose, valoneic acid dilactone, pentagalloylglucose, digalloylshikimic acid, and ellagic acid. Pretreatment with the extract at doses of 100 and 300 mg/kg significantly reduced gastric ulcer lesions in both models. Compared with the reference drugs (omeprazole or ranitidine, respectively), no significant difference was found (p < 0.05). The extract's gastroprotective effect was accompanied by significant decreases in leukocyte recruitment, and gastric levels of TNF-α and LTB4 by two to fourfold (p < 0.05). Also, gastric levels of PGE2 gastric levels were maintained and the antioxidant enzyme activities of SOD and nitrate/nitrite in the gastric tissue were improved (p < 0.05). The LC-MS analysis indicated the presence of hydrolyzable tannins (mainly gallic acid derivatives). CONCLUSION: The results suggest that the gastroprotective effect of the methanol extract of C. coriaria pods occurs through anti-inflammatory, antioxidant, and NO modulation properties, and gallic acid derivatives may be the main possible compounds responsible for its actions.

UV Radiation Effect in New Materials Developed for the Construction of Beehives.

In recent decades, there has been an increasing focus on the alarming decline in global bee populations, given their critical ecological contributions to natural pollination and biodiversity. This decline, marked by a substantial reduction in bee colonies in forested areas, has serious implications for sustainable beekeeping practices and poses a broader risk to ecological well-being. Addressing these pressing issues requires innovative solutions, one of which involves the development and fabrication of beehives crafted from composite materials that are ecologically compatible with bee biology. Importantly, these materials should also exhibit a high resistance to environmental factors, such as ultraviolet (UV) radiation, in order to maintain their mechanical integrity and longevity. To investigate this, we conducted accelerated UV degradation tests on a variety of composite materials to rapidly assess their susceptibility to UV-induced changes. High-density polyethylene (HDPE) served as the matrix material and was reinforced with natural fibers, specifically fique fibers (Furcraea bedinghausii), banana fibers, and goose feathers. Our findings indicate that UV radiation exposure results in a noticeable reduction in the tensile strength of these materials. For example, wood composites experienced a 48% decline in tensile strength over a 60-day period, a rate of deterioration notably higher than that of other tested composite materials. Conversely, HDPE composites fortified with banana fibers initially demonstrated tensile strengths exceeding 9 MPa and 10 MPa. Although these values gradually decreased over the observation period, the composites still displayed favorable stress-strain characteristics. This research underscores the substantial influence of UV radiation on the longevity and efficacy of beehive materials, which in turn affects the durability of natural wood hives exposed to these environmental factors. The resultant increased maintenance and replacement costs for beekeepers further emphasize the need for judicious material selection in beehive construction and point to the viability of the composite materials examined in this study.

Are neurologic symptoms associated with worse QoL in non-CNS cancer patients?

BACKGROUND: The burden of having neurologic symptoms (NS) in cancer patients has scantly been studied; therefore, we performed a study whose purpose was to measure the impact of having clinically active (NS) on the quality of life (QoL) of non-primary CNS cancer patients. METHODS: Patients with systemic cancer (non-primary CNS cancer) sent for neurological evaluation at a single cancer center (INCAN) were prospectively invited to respond the EORTC-QLQ-C30 and BN20 questionnaires. Associations of the questionnairés items were blindly measured for the following groups: NS+ or not (NS-) and having active cancer (AC+) or not (AC-). RESULTS: Of 205 patients aged 55.4 ± 15.4 years, 122 (60%) had NS+ and 107 (52%) AC +. The NS+ group (compared with the NS-) showed a significant worse perception in the following scales/items of the EORTC QLQ-C30: physical functioning (median 86 vs. 92, P = 0.012), role functioning (66 vs. 100, P < 0.001), emotional functioning (75 vs. 83, P = 0.005), cognitive functioning (66 vs. 83, P < 0.001), fatigue (33 vs. 22, P < 0.001), nausea and vomiting (P = 0.021), pain (33 vs. 16, P < 0.001), insomnia (33 vs. 0, P = 0.011), appetite loss (P = 0.021), and global health (66 vs. 75, P = 0.001). CONCLUSION: In patients with systemic (non-CNS) cancer, the QoL is significantly worse for patients with active neurologic symptoms.

α-glucosidase inhibitors from Brickellia cavanillesii.

An aqueous extract from the aerial parts of Brickellia cavanillesii attenuated postprandial hyperglycemia in diabetic mice during oral glucose and sucrose tolerance tests. Experimental type-II DM was achieved by treating mice with streptozotocin (100 mg/kg) and ß-nicotinamide adenine dinucleotide (40 mg/kg). These pharmacological results demonstrated that B. cavanillesii is effective for controlling fasting and postprandial blood glucose levels in animal models. The same aqueous extract also showed potent inhibitory activity (IC(50) = 0.169 vs 1.12 mg/mL for acarbose) against yeast α-glucosidase. Bioassay-guided fractionation of the active extract using the α-glucosidase inhibitory assay led to the isolation of several compounds including two chromenes [6-acetyl-5-hydroxy-2,2-dimethyl-2H-chromene (1) and 6-hydroxyacetyl-5-hydroxy-2,2-dimethyl-2H-chromene (2)], two sesquiterpene lactones [caleins B (3) and C (4)], several flavonoids [acacetin (5), genkwanin (6), isorhamnetin (7), kaempferol (8), and quercetin (9)], and 3,5-di-O-caffeoylquinic acid (10). Chromene 2 is a new chemical entity. Compounds 2, 4, 7, and 9 inhibited the activity of yeast α-glucosidase with IC(50) 0.42, 0.28, 0.16, and 0.53 mM, respectively, vs 1.7 mM for acarbose. Kinetic analysis revealed that compounds 4 and 7 behaved as mixed-type inhibitors with K(i) values of 1.91 and 0.41 mM, respectively, while 2 was noncompetititive, with a K(i) of 0.13 mM. Docking analysis predicted that these compounds, except 2, bind to the enzyme at the catalytic site.