Chemical composition, anticancer, antimicrobial activity of Aloysia citriodora Palau essential oils from four different locations in Palestine.

The primary aim of this investigation was to determine the anticancer and antimicrobial properties of essential oils (EOs) extracted from the leaves of Aloysia citriodora Palau, which were procured from four separate locations in Palestine, in addition to analyzing their chemical composition. These areas include Jericho, which has the distinction of being the lowest location on Earth, at 260 m below sea level. The EOs were acquired by hydrodistillation, and their chemical composition was examined utilizing gas chromatography-mass spectrometry (GC-MS). The minimum inhibitory concentration (MIC) of EOs was assessed against six bacterial strains and one fungal species using 96-well microtiter plates. The primary components found in these oils are geranial (26.32-37.22%), neral (18.38-29.00%), and α-curcumene (7.76-16.91%) in three regions. α-Curcumene (26.94%), spathulenol (13.69%), geranial (10.79%), caryophyllene oxide (8.66%), and neral (7.59%) were found to be the most common of the 32 chemical components in the EO from Jericho. The EOs exhibited bactericidal properties, particularly against Staphylococcus aureus, methicillin-resistant Staphylococcus aureus (MRSA), and showed highly effective fungicidal activity. Nevertheless, the antifungal efficacy of the EO was found to surpass its antibacterial activity when administered at lower dosages. The EOs exhibited anticancer activities against melanoma cancer cells, as indicated by their IC50 values, which ranged from 4.65 to 7.96 µg/mL. A. citriodora EO possesses substantial antifungal and anticancer characteristics, rendering it appropriate for utilization in food-related contexts, hence potentially enhancing the sustainability of the food sector.

Excito-repellent and Pesticide-Likeness Properties of Essential Oils on Carpophilus dimidiatus (Fabricius) (Nitidulidae) and Oryzaephilus mercator (L.) (Silvanidae).

Carpophilus dimidiatus (Fabricius) (Nitidulidae) and Oryzaephilus mercator (L.) (Silvanidae) are insect pests that cause severe damage in important walnut growing regions in the northwest of Argentina. The current management approaches for these pests involve the use of unsafe phosphorus pesticides whose overuse have led to farmworker poisoning, pest resistance issues, and environmental contamination. Plant extracts, particularly essential oils, are an alternative source of insect control agents. Excito-repellent essential oils can be used to develop ecofriendly tools for managing the pest population without affecting quality and visual appearance of the stored walnuts. Laboratory studies were conducted to assess the excito-repellent effects of C. dimidiatus and O. mercator of 12 essential oils derived from aromatic plants used as food additives and traditional medicine in Argentina: Aloysia citrodora (AC), Aloysia gratissima (AG), Aloysia gratissima var. Gratissima (AGG), Blepharocalyx salicipholius (BS), Hyptis mutabilis (HM), Lippia junelliana (LJ), Lippia turbinata (LT), Mentha x piperita (MP), Minthostachys mollis (MM), Minthostachys verticillata (MV), Origanum vulgare(OV), and Rosmarinus officinalis (RO). The most bioactive EOs (ERijk ≥ 70%) were Aloysia gratissima var. Gratissima (AGG), Minthostachys verticillata, and Lippia junelliana. Their bioactivity profile and chemical space, characterized from GC-MS measures, Generalized Estimating Equations, and Hierarchical Cluster Analysis, revealed that they are mixtures of very functionalized molecules with physicochemical properties similar to those of insecticides with low residual property that enter the insect body through the respiratory system by inhalation. The AGG, MV, and LJ oils are promising as protective agents of walnut products. In our laboratory, studies of their formulations for use in integrated pest management programs are still ongoing.

Water stress modulates terpene biosynthesis and morphophysiology at different ploidal levels in Lippia alba (Mill.) N. E. Brown (Verbenaceae).

Monoterpenes are the main component in essential oils of Lippia alba. In this species, the chemical composition of essential oils varies with genome size: citral (geraniol and neral) is dominant in diploids and tetraploids, and linalool in triploids. Because environmental stress impacts various metabolic pathways, we hypothesized that stress responses in L. alba could alter the relationship between genome size and essential oil composition. Water stress affects the flowering, production, and reproduction of plants. Here, we evaluated the effect of water stress on morphophysiology, essential oil production, and the expression of genes related to monoterpene synthesis in diploid, triploid, and tetraploid accessions of L. alba cultivated in vitro for 40 days. First, using transcriptome data, we performed de novo gene assembly and identified orthologous genes using phylogenetic and clustering-based approaches. The expression of candidate genes related to terpene biosynthesis was estimated by real-time quantitative PCR. Next, we assessed the expression of these genes under water stress conditions, whereby 1% PEG-4000 was added to MS medium. Water stress modulated L. alba morphophysiology at all ploidal levels. Gene expression and essential oil production were affected in triploid accessions. Polyploid accessions showed greater growth and metabolic tolerance under stress compared to diploids. These results confirm the complex regulation of metabolic pathways such as the production of essential oils in polyploid genomes. In addition, they highlight aspects of genotype and environment interactions, which may be important for the conservation of tropical biodiversity.

Assessment of the in Vitro Antimelanoma Potential of Lippia microphylla Cham (Verbenaceae) Essential Oil.

Essential oils stand out among natural products for their complex composition, frequently described in the literature with a range of biological effects. This study evaluated the cytotoxic activity against several human cancer cell lines of essential oils extracted from the leaves of Lippia microphylla (EO-LM) Cham. (Verbenaceae). The melanoma cell line SK-MEL-28 was the most sensitive to the EO-LM, presenting an IC50 of 33.38±1.16 µg/mL. Afterward, the effects of EO-LM on the cell cycle, induction of apoptosis, and production of reactive oxygen species (ROS) were evaluated. We stated a significant increase in the sub-G1 population, indicating apoptosis, later confirmed by an increase of SK-MEL-28 cells labeled with Annexin V-FITC and by the formation of apoptotic bodies and membrane blebs, observed by confocal microscopy. Additionally, EO-LM reduced the production of ROS, indicating antioxidant activity. Therefore, EO-LM exhibits anti-melanoma activity in vitro, suggesting its potential as an anticancer agent.

Acute toxicity of essential oils of Aloysia triphylla (L'Hér.) Britton, Lippia gracilis Schauer, and Piper aduncum L. in Colossoma macropomum (Cuvier, 1818).

The aim of this study was to determine the acute toxicity of the essential oils (EOs) of Aloysia triphylla, Lippia gracilis and Piper aduncum in juvenile tambaqui (Colossoma macropomum), and evaluate the possible histopathological alterations in their gills. For the acute toxicity tests, juvenile tambaqui (n=24/treatment) were distributed in six treatments with three replicates, which comprised the control and five EO concentrations of A. triphylla (60, 80, 100, 120 and 140 mg L-1), L. gracilis (35, 40, 45, 50 and 55 mg L-1) and P. aduncum (42.5, 45, 47.5, 50 and 52.5 mg L-1), with an exposure period of 4 h. The mortality rate and severity of damage to the tambaqui gills were proportional to the increase in the concentration of the EO, with LC50-4 h values estimated at 109.57 mg L -1 for A. triphylla, 41.63 mg L -1 for L. gracilis and 48.17 mg L -1 for P. aduncum. The main morphological damages observed in the gills of the tambaqui exposed to the three EOs, were Grade I: hypertrophy and hyperplasia of lamellar epithelial cells, lamellar fusion, epithelial detachment, capillary dilation and constriction, proliferation of chloride cells and mucosal cells and edema; in low frequency Grade II damage as epithelial rupture and lamellar aneurysm. Necrosis (Grade III damage) was observed only in gill lamellae exposed to P. aduncum EO (47.5, 50.0 and 52.5 mg L-1). Concentrations of EOs below LC50-4 h can be used sparingly, for short periods of exposure for the treatment of diseases in tambaqui breeding.

Role of Polyphenols from the Aqueous Extract of Aloysia citrodora in the Inhibition of Aflatoxin B1 Synthesis in Aspergillus flavus.

Aflatoxin B1 (AFB1) is a mycotoxin considered a potent carcinogen for humans that contaminates a wide range of crops. Various strategies have been established to reduce or block the synthesis of AFB1 in food and feed. The use of aqueous extracts derived from plants with high antioxidant activity has been a subject of study in recent years due to their efficacy in inhibiting AFB1. In this study, we assessed the effect of Aloysia citrodora aqueous extract on Aspergillus flavus growth and on AFB1 production. A bio-guided fractionation followed by High Performance Liquid Chromatography (HPLC) and Mass spectrometry analysis of the active fraction were applied to identify the candidate molecules responsible for the dose-effect inhibition of AFB1 synthesis. Our results revealed that polyphenols are the molecules implicated in AFB1 inhibition, achieving almost a total inhibition of the toxin production (99%). We identified luteolin-7-diglucuronide as one of the main constituents in A. citrodora extract, and demonstrated that it is able to inhibit, by itself, AFB1 production by 57%. This is the first study demonstrating the anti-Aflatoxin B1 effect of this molecule, while other polyphenols surely intervene in A. citrodora anti-AFB1 activity.

Comparison of bacterial diversity in Bactrocera cucurbitae (Coquillett) ovaries and eggs based on 16S rRNA sequencing.

Next-generation sequencing allows for fine-scale studies of microbial communities. Herein, 16S ribosomal RNA high-throughput sequencing was used to identify, classify, and predict the functions of the bacterial communities in the eggs and ovaries of Bactrocera cucurbitae (Coquillett) (Diptera: Tephritidae), which is a pest that infests a variety of cucurbit fruits at different developmental stages. Taxonomic analyses indicate that bacteria associated with B. cucurbitae represent 19 phyla, which were spread across different developmental stages. Specifically, the egg microbiota had a higher alpha diversity than those of microbiota in the primary and mature ovaries. Significant differences were not observed between the primary and mature ovaries in terms of their microbiota's alpha diversities. Pseudomonadota, Deinococcota, Bacteroidota, Bacillota, and Actinomycetota were the dominant phyla in all three developmental stages of B. cucurbitae, and Pseudomonadaceae and Enterobacteriaceae were the most abundant families. Owing to the unique physiological environment of the ovaries, the diversity of their bacterial community was significantly lower than that in the eggs. This study provides new insights into the structure and abundance of the microbiota in B. cucurbitae at different developmental stages and contributes to forming management strategies for this pest.

Long-term fungal inoculation of Ficus sycomorus and Tectona grandis woods with Aspergillus flavus and Penicillium chrysogenum.

In the current study, two molds, Aspergillus flavus (ACC# LC325160) and Penicillium chrysogenum (ACC# LC325162) were inoculated into two types of wood to be examined using scanning electron microscopy-energy dispersive X-ray (SEM-EDX) and computerized tomography (CT) scanning. Ficus sycomorus, a non-durable wood, and Tectona grandis, a durable wood, were the two wood blocks chosen, and they were inoculated with the two molds and incubated for 36 months at an ambient temperature of 27 ± 2 °C and 70 ± 5% relative humidity (RH). The surface and a 5-mm depth of inoculated wood blocks were histologically evaluated using SEM and CT images. The results showed that A. flavus and P. chrysogenum grew enormously on and inside of F. sycomorus wood blocks, but T. grandis wood displayed resistance to mold growth. The atomic percentages of C declined from 61.69% (control) to 59.33% in F. sycomorus wood samples inoculated with A. flavus while O increased from 37.81 to 39.59%. P. chrysogenum caused the C and O atomic percentages in F. sycomorus wood to drop to 58.43%, and 26.34%, respectively. C with atomic percentages in Teak wood's C content fell from 70.85 to 54.16%, and 40.89%, after being inoculated with A. flavus and P. chrysogenum. The O atomic percentage rose from 28.78 to 45.19% and 52.43%, when inoculated with A. flavus and P. chrysogenum, respectively. Depending on how durable each wood was, The examined fungi were able to attack the two distinct types of wood in various deterioration patterns. T. grandis wood overtaken by the two molds under study appears to be a useful material for a variety of uses.

Prenylated-coumarins from Gmelina arborea and evaluation for neurotrophic activity.

A MeOH extract of the stem of Gmelina arborea Roxb. ex Sm. (Lamiaceae) exhibited neurite outgrowth-promoting activity in NGF-mediated PC12 cells. Bioassay-guided fractionation resulted in the isolation of eight previously undescribed prenylated coumarin compounds along with nine known compounds. Structural elucidation of these compounds was accomplished by analysis of extensive spectroscopic data, comparison with the literature, and chemical reactions. It was the first time to find prenylated coumarin compounds from G. arborea. Among the isolated compounds, N-methylflindersine and artanin showed neurite outgrowth-promoting activity in NGF-mediated PC12 cells.

Volatile Compounds and Biological Activity of the Essential Oil of Aloysia citrodora Paláu: Comparison of Hydrodistillation and Microwave-Assisted Hydrodistillation.

Aromatic plants are a remarkable source of natural products. Aloysia citrodora Paláu (Verbenaceae), commonly known as lemon verbena, is a relevant source of essential oils with potential applications due to its lemony scent and bioactive properties. Studies carried out on this species have focused on the volatile composition of the essential oil obtained by Clevenger hydrodistillation (CHD), with little information available on alternative extraction methodologies or the biological properties of the oil. Therefore, this work aimed to compare the volatile composition, antioxidant activity, cytotoxicity, anti-inflammatory and antibacterial activities of the essential oil extracted by conventional hydrodistillation by Clevenger (CHD) and Microwave-Assisted Hydrodistillation (MAHD). Significant differences (p < 0.05) were observed for some compounds, including the two major ones, geranial (18.7-21.1%) and neral (15.3-16.2%). Better antioxidant activity was exhibited by the MAHD essential oil in DPPH radical scavenging and reducing power assays, while no differences were observed in the cellular antioxidant assay. The MADH essential oil also presented higher inhibition against four tumoral cell lines and exhibited lower cytotoxicity in non-tumoral cells as compared with Clevenger-extracted essential oil. In contrast, the latter showed higher anti-inflammatory activity. Both essential oils were able to inhibit the growth of eleven out of the fifteen bacterial strains tested.

The characteristics of the intestinal bacterial community from Oreochromis mossambicus and its interaction with microbiota from artificial fishery habitats.

BACKGROUND: Artificial habitats can allow many fish to flock together and interact and have been widely used to restore and protect fishery resources. The piece of research intends to elucidate the relationship of microbial communities between tilapia (Oreochromis mossambicus) intestines and artificial fishery habitats (water and sediments). Hence, 16 S rDNA sequencing technology was used to study the bacterial communities from intestines, water, and sediments. RESULTS: The results showed that the tilapia intestines had the lowest richness of Operational Taxonomic Units (OTUs) and the lowest diversity of the bacterial community compared to water and sediments. The intestine, water, and sediment microbial communities shared many OTUs. Overall, 663 shared OTUs were identified from the tilapia intestines (76.20%), the surrounding water (71.14%), and sediment (56.86%) in artificial habitats. However, there were unique OTUs that were detected in different sample types. There were 81, 77 and 112 unique OTUs observed in tilapia intestines, the surrounding water and sediment, respectively. Proteobacteria, Cyanobacteria, Actinobacteria, Firmicutes, Fusobacteria, and Bacteroidetes were the most common and dominant bacterial phyla between the tilapia intestines and habitats. In the two groups, the microbial communities were similar in the taxonomic composition but different in the abundance of bacterial phyla. Interestingly, Firmicutes increased, while Fusobacteria decreased in artificial habitats. These findings indicated that the artificial habitats had fewer effects on the water environment and indicated that the mode of artificial habitats could have an effect on the enriched bacteria in the tilapia intestines. CONCLUSIONS: This study analysed the bacterial communities of artificial habitats from the intestines, water, and sediments, which can explain the relationship between the tilapia intestines and habitats and strengthen the value of ecological services provided by artificial habitats.

Evaluation of the susceptibility of Tritrichomonas foetus to extracts of Lantana camara (Verbenaceae) by flow cytometry.

Bovine Trichomonosis (BT), a sexually transmitted disease endemic in countries with extensive cattle farming and natural service, is one of the most common causes of reproductive failure. 5-nitroimidazoles and their derivatives are used for its treatment, mainly metronidazole. The emergence of drug resistance mechanisms and treatment failures raise the need to investigate the effectiveness of new active compounds that contribute to parasite control. In this regard, extracts of Lantana camara (Verbenacea) have shown high biocidal potential against isolates of Trypanosoma cruzi and Leishmania braziliensis in vitro assays, although their effect on Tritrichomonas foetus has not been demonstrated yet. The available information on in vitro susceptibility of trichomonicidal drugs comes from the use of a diversity of methodologies and criteria, especially the observation of parasite motility under the optical microscope to assess their viability. Recently, in our laboratory, the use of flow cytometry has been described for the first time as a rapid and efficient method to evaluate the viability of T. foetus against metronidazole. The present study aimed to evaluate the cytostatic effect of L. camara extracts against T. foetus isolates by flow cytometry. Under aerobic conditions, IC50 values of 22.60 µg/mL were obtained on average. Under anaerobic conditions, the IC50 oscilated around 29.04 µg/mL. The results obtained allowed describing the susceptibility exhibited by these protozoa, being a valuable information for the development of potential BT treatments.

Antibacterial Activity and Antibacterial Mechanism of Lemon Verbena Essential Oil.

The destructive effect and mode of action of lemon verbena essential oil on cells were investigated, taking the isolated Pseudosciaena D4 as the research object. The extracellular absorbance of the Pseudosciaena D4 increased at OD260 and OD280 after being treated with lemon verbena essential oil, which destroyed the integrity of Pseudosciaena D4 cells, showing a significant effect on preventing biomembrane formation and destroying the formed biomembrane. With an increased concentration of lemon verbena essential oil, extracellular polysaccharide showed a significant decrease in content and a significant increase in inhibition rate, indicating that the secretion of extracellular polysaccharide by Pseudosciaena D4 cells could be inhibited by lemon verbena essential oil during the process of biomembrane formation. Cell introcession and shrinkage appeared after the treatment with essential oil, and a transparent cavity was formed by the out-flowed cell content. Lemon verbena essential oil destroyed the cell wall, resulting in an enhanced permeability of the cell membrane and leakage of the contents, thereby causing cell death.

Chromosome-scale assembly of the Verbenaceae species Queen's Wreath (Petrea volubilis L.).

OBJECTIVES: Petrea volubilis, a member of the Order Lamiales and the Verbenaceae family, is an important horticultural species that has been used in traditional folk medicine. To provide a genome sequence for comparative studies within the Order Lamiales that includes important families such as Lamiaceae (mints), we generated a long-read, chromosome-scale genome assembly of this species. DATA DESCRIPTION: Using a total of 45.5 Gb of Pacific Biosciences long read sequence, we generated a 480.2 Mb assembly of P. volubilis, of which, 93% is chromosome anchored. Representation of genic regions was robust with 96.6% of the Benchmarking of Universal Single Copy Orthologs present in the genome assembly. A total of 57.8% of the genome was annotated as a repetitive sequence. Using a gene annotation pipeline that included refinement of gene models using transcript evidence, 30,982 high confidence genes were annotated. Access to the P. volubilis genome will facilitate evolutionary studies in the Lamiales, a key order of Asterids that includes significant crop and medicinal plant species.

Deleterious liver-adipose crosstalk in obesity: Hydroethanolic extract of Lampaya medicinalis Phil. (Verbenaceae) counteracts fatty acid-induced fibrotic marker expression in human hepatocytes.

Elevated circulating fatty acids in obesity may induce hepatic steatosis, leading to liver inflammation, fibrosis and nonalcoholic fatty liver disease (NAFLD). On the other hand, impaired communication between hepatocytes and adipose tissue (AT) in obesity influences adipose lipolysis and fibrosis, negatively affecting metabolic function. Infusions of Lampaya medicinalis Phil. (Verbenaceae) are used in Chilean folk medicine to treat inflammatory diseases. Hydroethanolic extract of lampaya (HEL) contains flavonoids that may explain its anti-inflammatory effect, but it is unknown whether HEL modulates fibrogenic processes in hepatocytes. We studied lipolysis and expression of fibrosis markers after exposure of visceral AT explants from subjects with obesity to HepG2-secreted factors. In addition, we evaluated the effect of HEL on palmitic acid (PA, C16:0) and oleic acid (OA; C18:1)-induced fibrotic marker expression in HepG2 hepatocytes. Results: Exposure to HepG2-secreted factors increased visceral AT lipolysis and expression of CTGF and collagen I. Exposure to OA/PA elevated collagen I, CTGF, fibronectin, α-smooth muscle actin, MMP-2 and MMP-9 expression in HepG2 cells, and these effects were prevented by HEL co-treatment. Conclusion: HEL effect counteracting OA/PA-induced fibrotic marker expression in HepG2 hepatocytes may represent a preventive approach against hepatic fibrosis and deleterious liver-adipose crosstalk in obesity.

Chemical composition and biological activities of the essential oils from Lippia alba and Lippia origanoides.

There is an increasing interest in essential oils extracted from Verbenaceae plant species as potential sources of biologically active compounds that could provide a starting point for designing novel phyto-pharmaceuticals in aquaculture. The present study was aimed to investigate the chemical composition, antioxidant activity, acute toxicity and antimicrobial effects against Vibrio parahaemolyticus of essential oils extracted from Lippia alba and L. origanoides. Approximately 23 components were identified and quantified by gas chromatography-mass spectrometry and flame ionization detection in each species' essential oil. The most predominant compounds were geranial (23.0%), limonene (17.0%) and neral (15.5%) in L. alba, and thymol (47.2%), p-cymene (16.0%) and E-caryophyllene (11.3%) in L. origanoides. The essential oils have antibacterial activity against Vibrio parahaemolyticus presenting Minimum Inhibitory Concentration (MIC) and Bactericidal Concentration (MBC) values between 156-625 µg mL-1. The essential oils also show antioxidant potential estimated by 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging assays, presenting IC50 of 60.16 mg mL-1 and 0.22 mg mL-1 for L. alba and L. origanoides EO, respectively. Both oils were classified as toxic to Artemia salina nauplii. Therefore, these essential oils may be useful for controlling pathogenic bacteria important to the aquaculture industry.

Evidence of the Cardioprotective Effects of Aloysia polystachya in Isoproterenol-Induced Myocardial Infarction in Rats.

Aloysia polystachya is a plant species that is widely used in Brazilian folk medicine for the treatment of different disorders that affect the cardiovascular system. The aim of the study was to investigate the cardioprotective effects of an ethanol-soluble fraction of A. polystachya (ESAP) on isoproterenol-induced myocardial infarction in rats. Different groups of rats (n = 8) were orally treated with ESAP (30, 100, and 300 mg/kg), carvedilol (10 mg/kg), or vehicle (filtered water; 1 mL/100 g) for 7 days. Naive rats received no treatment. On the morning of day 6, acute myocardial infarction was induced by the acute oral administration of isoproterenol (100 mg/kg). On the morning of day 8, all rats underwent electrocardiography and transthoracic echocardiography. Blood samples were then collected, and serum levels of creatine kinase-MB fraction (CK-MB) and cardiac troponin T (cTNT) were quantified. ESAP significantly reduced electrocardiographic changes, improved the ventricular ejection fraction, and reduced serum levels of CK-MB and cTNT in infarcted rats. The cardioprotective effects of ESAP could be exploited as an effective tool against isoproterenol-induced myocardial infarction in rats.

Inhibition of α-Glycosidase by Lippia dulcis Trevir. (Verbenaceae) Preparations, Quantification of Verbascoside, and Study of Its Molecular Docking.

This study aimed to quantify verbascoside (VEB), perform molecular docking studies of VEB with the α-glucosidase (GL) of Bacillus stearothermophilus, and evaluate the inhibition of the enzyme by L. dulcis preparations. The substrate concentration and presence of reduced glutathione were evaluated for their effect on the in vitro inhibition of the GL enzyme. Assays were also performed in the presence and absence of simulated gastric fluid. The antidiabetic fractions 2 and 3 were the most inhibited GL, but their activity were significantly decreased in the presence of gastric fluid. Chromatographic analyses confirmed the predominant presence of VEB in the samples. The samples had VEB concentrations between 49.9 and 243.5 mg/g. Simulation of the molecular docking of VEB were consistent with its GL-inhibitory activity. It can conclude that the crude ethanol extract and fractions show inhibitory activity against the GL enzyme.

A new flavone and a newly synthesized alkaloid from Lippia rugosa A. Chev (Verbenaceae).

The chemical investigation of the leaf extract of a Cameroonian medicinal plant, Lippia rugosa A Chev (Verbenaceae) led to the isolation of a new flavonoid derivative flavolippia (1), alongside eleven known compounds: 2,4-dimethylpyridin-3,5-diol (2), 5-hydroxy-6,7,4'-trimethoxylflavone (3), 5-hydroxy-3,7,4'-trimethoxyflavone (4), 7-hydroxy-5,6,4'-trimethoxyflavone (5), 3ß-hydroxy-urs-12-en-3-ol (α-amyrin) (6), lupeol acetate (7), lup-20(29)-en-3ß-ol (lupeol) (8), lup-20(29)-en-3ß,28-diol (betulin) (9), fridelan-3-one (fridelan) (10), saccharose (11), cosanol (12). In addition, a new semi-synthetic alkaloid derivative named lippiamicin (13) was prepared from 2,4-dimethylpyridin-3,5-diol (2). Their structures were established on the basis of their spectroscopic data, as well as 1 D and 2 D NMR. Compounds 1-13 were evaluated for their antioxidant activities. The results obtained showed that compounds 2 and 12 were the most active with IC50 values of 0.145 ± 0.011 and 0.195 ± 0.017 µM/mL respectively (for DPPH•) and 0.241 ± 0.027 and 0.223 ± 0.024 µM/mL respectively (for FRAP) compared to butylated hydroxyltoluene used as positive control.

Anti-asthmatic activity of standardized hydro-ethanolic and aqueous extracts of Stachytarpheta cayennensis (Rich.) Vahl in a murine model.

ETHNOPHARMACOLOGICAL RELEVANCE: Stachytarpheta cayennensis (Verbenaceae) has been used in Brazilian traditional medicine to treat asthma and other respiratory diseases. AIMS OF THE STUDY: To investigate the effects of different doses of standardized hydro-ethanolic (SCH) and aqueous (SCA) extracts of aerial parts of S. cayennensis using a murine ovalbumin (OVA)-induced asthma model. MATERIALS AND METHODS: The major constituents of the plant extracts were identified and standardized by ultra-performance liquid chromatography coupled with mass spectrometry. Balb/c mice were challenged with OVA solution and treated concomitantly by intraperitoneal injection of standardized SCH or SCA extracts at 50, 100, and 200 mg/kg concentrations. OVA-challenged control animals were treated with either dexamethasone (OVA-DEX) or saline solution (OVA-SAL). After challenge, we assessed in vivo bronchial hyperresponsiveness, airway inflammation (number of cells), peribronchial inflammation (histological analysis) and production of OVA-specific IgE and interleukin (IL)-4, IL-5, and IL-13 (ELISA). RESULTS: Acteoside, isoacteoside, and ipolamiide were the major constituents of SCH and SCA. The respective concentrations of acteoside in SCH and SCA were 78 and 98 µg/mL, while those of ipolamiide were 30 and 19 µg/mL. Treatment with 200 mg/kg of SCH or SCA decreased IL-4, IL-5, and IL-13 in lung homogenates. These reductions were accompanied by a lower influx of inflammatory cells (eosinophils, lymphocytes, and macrophages) to the airways and lungs. In addition to the anti-inflammatory effects, administration of SCA, but not SCH, ameliorated the parameters of bronchial hyperresponsiveness and decreased levels of circulating OVA-specific IgE. CONCLUSION: The results presented herein demonstrate for the first time the anti-asthmatic activity of S. cayennensis extracts in a murine model, thereby supporting the ethnopharmacological uses of the plant.