Anti-leukemic effects of Vernonia amygdalina extract.

This study aimed to investigate the impact of Vernonia amygdalina leaf extract on FLT3 regulation. V. amygdalina was extracted with 96% ethanol (VAE-96), and its cytotoxicity against FLT3- cell lines (MOLM-13 and MV-4-11) was evaluated. The results indicated that VAE-96 induced apoptosis in these cells and inhibited the phosphorylation of AKT, MAPK, and FLT3. Additionally, VAE-96 substantially diminished the activity of the FLT3 promoter and the expression of FLT3 mRNA. The extract was found to contain alkaloids, saponin, reduced sugar compounds, and polyphenols, including tannins and flavonoids, as per the phytoconstituents analysis. The potential of alkaloid fractions on MOLM-13 cells was indicated by the robust cytotoxic effect of the alkaloid fractions, which resulted in over 50% cell mortality at 30 µg/ml. Our results suggest that VAE-96 may be a beneficial agent for the prevention and treatment of AML with FLT3-ITD mutation.

Effects of solvent extraction on the phytoconstituents and in vitro antioxidant activity properties of leaf extracts of the two selected medicinal plants from Malawi.

This study evaluated and compared the phytochemical and antioxidant properties of the solvent extracts of Azadirachta indica A. Juss and Vernonia amygdalina Del leaves. Methanolic and aqueous extracts showed high (P ≤ 0.05) extract yields (in %), compared to chloroform and ethyl acetate extracts from both V. amygdalina and A. indica leaves. The study exhibited high phytochemical content in methanol and aqueous extracts compared to chloroform and ethyl acetate extracts, confirming the potential for medicinal use. V. amygdalina methanol and aqueous extracts had higher (P ≤ 0.05) total phenolic content (TPC), in mg GAE/gDW, (158.810±0.846 and 217.883±0.265, respectively) than chloroform (37.574±0.118) and ethyl acetate (104.758±0.236) but higher ethyl acetate content in A. indica extracts. Low polar solvents extracted high (P ≤ 0.05) total flavonoids, in mgQE/gDW, (367.051±0.858 and 149.808±0.009) compared to high polar solvents (14.863±0.071 and 54.226±0.014 ) in V. amygdalina while as in A. indica leaf extracts, low polar solvents showed high TFC ( 658.469±3.451 and 275.288±10.490) compared to high polar solvents (26.312±0.063 and 48.858±0.063) respectively. In vitro total antioxidant capacity, in mg/g, was higher in polar solvents than in low-polar solvents, ranging from 34.300±1.784 to 121.015±6.839 for A. indica ethyl acetate and methanolic extracts. A strong correlation between TPC and tannic acid content was observed, except in A. indica methanolic extracts of A. indica. Ferric reducing power was high, except for V. amygdalina chloroform and methanol leaf extracts, which were lower (P≤ 0.05) than that of the standard ascorbic acid. The study revealed that high polar solvents, such as methanol and water, are more efficient in the extraction of antioxidants from A. indica but lower in V. amygdalina extracts. High phytochemical content and antioxidative capacity could be significant in treating various diseases in humans.

Effect of single and combination therapy on methanol extracts of Khaya senegalensis stem bark, Vernonia amygdalina leaves and Garcinia kola seed in Leptospira interrogans-infected mice.

ETHNOPHARMACOLOGICAL RELEVANCE: Pastoralists in Nigeria mix Garcinia kola seed (GK), Khaya senegalensis stem bark (KS), and Vernonia amygdalina leaves (VA) to treat leptospirosis. AIM: To determine the in vitro and in vivo effect on single and combination therapy on Leptospira interrogans-infected mice. MATERIALS AND METHODS: Evaluation of in vitro assay for anti-leptospiral motility of the extracts was carried out in triplicates. For the in vivo assessment, 40 adult male mice inoculated with Leptospira were randomly allocated into 8 groups of 5 mice each. Groups IV-IX were treated with 800 mg/kg b.w. of KS, GK, VA, KS + GK, KS + VA, GK + VA for 5 days. Group I was negative control, II was model control, and III was treated with penicillin (3.7 mg/kg b.w.) intramuscularly. RESULTS: In vitro, at 90 min, all the extracts at 800, 400, and 200 mg/ml showed complete cessation of motility which was significantly (p < 0.05) different when compared to the negative control. A significant (p < 0.05) IC50 of 0.18 mg/ml was recorded with GK when compared to KS (0.40 mg/ml), VA (0.25 mg/ml), and procaine penicillin (0.31 mg/ml). Mean packed cell volume, haemoglobin concentration, and mean corpuscular haemoglobin concentration decreased significantly (p < 0.05) in all infected groups and returned to almost pre-infection values. However, significant leucocytosis (p < 0.05) was observed in group II. AST and ALP showed a significant increase (p < 0.001). Histopathological evaluation showed the extracts to prevent the distortion of normal architecture of the selected organs. CONCLUSION: This study demonstrates the significant potential of Garcinia kola, Khaya senegalensis, and Vernonia amygdalina extracts singly and in combination to combat leptospirosis.

Exploring the inhibitory potential of phytochemicals from Vernonia glaberrima leaves against snake venom toxins through computational simulation and experimental validation.

Phospholipase A2 (PLA2) is an enzyme present in appreciable quantity in snake venoms which catalyze the hydrolysis of glycerophospholipids at sn-2 position and promote the release of lysophospholipids and fatty acids. 5-methylcoumarin-4-ß-glucoside (5MC4BG) and lupeol were previously isolated from the leaves of V. glaberrima. The aim of this research was to evaluate effect of these compounds as potential inhibitors of snake venom toxins of Naja nigricollis using an in vitro and in silico studies. Antisnake venom studies was conducted using acidimetry while the molecular docking analysis against PLA2 enzyme from N. nigricollis was performed using Auto Dock Vina and ADME-Tox analysis was evaluated using swissADME and ProTox-II online servers. The two compounds (5MC4BG and Lupeol) were able to inhibit the hydrolytic actions of PLA2 enzyme with percentage inhibition ranging from 23.99 to 72.36 % and 21.97-24.82 % at 0.0625-1.00 mg/mL respectively while the standard ASV had 82.63 % at 1.00 mg/mL after 10 min incubation at 37 °C. Similar effects were observed after 30 min incubation, although there was significant increase in percentage inhibition of 5MC4BG and lupeol ranging from 66.51 to 83.73 % and 54.87-59.60 % at similar concentrations. Furthermore, the compounds were able to bind to the active site of PLA2 enzyme with high affinity (-7.7 to -6.3 kcal/mol); the standard ligand, Varespladib had a docking score of -6.9 kcal/mol and they exhibited favorable drug-likeness and pharmacokinetic properties and according to toxicity predictions, the two compounds are toxic. In conclusion, the leaf of V. glaberrima contains phytoconstituents with antisnake activity and thus, validates the hypothesis that, the phytoconstituents of V. glaberrima leaves has antisnake venom activity against N. nigricollis venom and thus, should be studied further for the development as antisnake venom agents.

Anti-inflammatory germacrane-type sesquiterpene lactones from Vernonia sylvatica.

Nine new germacranolides, sylvaticalides A-H (1-9), and three known analogues (10-12) were isolated from the aerial part of Vernonia sylvatica. Their structures were established using comprehensive spectroscopic analysis, including high-resolution electrospray ionization mass spectroscopy (HR-ESI-MS) and 1D and 2D nuclear magnetic resonance (NMR) spectra. Their absolute configurations were determined by X-ray diffraction experiments. The anti-inflammatory activities of all isolated compounds were assessed by evaluating their inhibitory effects on the nuclear factor kappa B (NF-κB) pathway, which was activated by lipopolysaccharide (LPS)-stimulated human THP1-Dual cells, and the interferon-stimulated gene (ISG) pathway, activated by STING agonist MSA-2 in the same cell model. Compounds 1, 2 and 6 showed inhibitory effects on the NF-κB and ISG signaling pathways, with IC50 values ranging from 4.12 to 10.57 µmol·L-1.

Traditional Uses, Phytochemistry, and Pharmacological Activities of Vernonia cinerea (L.) Less.: An Updated Review.

Vernonia cinerea (L.) Less. is a perennial herbaceous plant found mainly in tropical areas, particularly in Southeast Asia, South America, and India. Various parts of V. cinerea have traditionally been used in folk medicine to treat several diseases, such as malaria, fever, and liver diseases. V. cinerea has so far yielded about 92 secondary metabolites. The majority of these are sesquiterpene lactones, but triterpenes, flavonoids, steroids, phenolics, and other compounds are present as well. V. cinerea crude extracts reportedly exhibit anti-inflammatory, antiprotozoal, antidiabetic, anticancer, antimicrobial, antioxidant, and renoprotective activities. This study aims to provide the latest up-to-date information on the botanical characterization, distribution, traditional uses, phytochemistry, and pharmacological activity of V. cinerea. Information on V. cinerea was thoroughly reviewed. The literature published between 1950 and 2024 was compiled through online bibliographic databases, including SciFinder, Web of Science, Google Scholar, PubMed, ScienceDirect, Springer Link, Wiley, and the MDPI online library. The keywords used for the literature search included Vernonia cinerea (L.) Less. and the synonyms Cyanthillium cinereum (L.) H.Rob., Conyza cinerea L., and various others.

Identification of Vernonia patula Merr. and Its Similar Varieties Based on a Combination of HPLC Fingerprinting and Chemical Pattern Recognition.

Vernonia patula Merr. (VP) is a traditional medicine used by the Zhuang and Yao people, known for its therapeutic properties in treating anemopyretic cold and other diseases. Distinguishing VP from similar varieties such as Praxelis clematidea (PC), Ageratum conyzoides L. (AC) and Ageratum houstonianum Mill (AH) was challenging due to their similar traits and plant morphology. The HPLC fingerprints of 40 batches of VP and three similar varieties were established. SPSS 20.0 and SIMCA-P 13.0 were used to statistically analyze the chromatographic peak areas of 37 components. The results showed that the similarity of the HPLC fingerprints for each of the four varieties was >0.9, while the similarity between the control chromatogram of VP and its similar varieties was <0.678. Cluster analysis and partial least squares discriminant analysis provided consistent results, indicating that all four varieties could be individually clustered together. Through further analysis, we found isochlorogenic acid A and isochlorogenic acid C were present only in the original VP, while preconene II was present in the three similar varieties of VP. These three components are expected to be identification points for accurately distinguishing VP from PC, AC and AH.

Highly efficient catalytic degradation of organic dyes using iron nanoparticles synthesized with Vernonia Amygdalina leaf extract.

Today, nanoscience explores the potential of nanoparticles due to their extraordinary properties compared to bulk materials. The synthesis of metal nanoparticles using plant extracts is a very promising method for environmental remediation, which gets global attention due to pollution-led global warming. In the present study, iron nanoparticles (FeNPs) were successfully synthesized by the green method using Vernonia amygdalina plant leaf extract as a natural reducing and capping agent. Biosynthesized FeNPs were characterized with different analytical techniques such as UV-visible, FT-IR, XRD, and SEM. The analysis revealed the formation of amorphous FeNPs with an irregular morphology and non-uniform distribution in size and shape. The average particle size was approximately 2.31 µm. According to the catalytic degradation investigation, the FeNPs produced via the green approach are highly effective in breaking down both CV and MB into non-toxic products, with a maximum degradation efficiency of 97.47% and 94.22%, respectively, when the right conditions are met. The kinetics study exhibited a high correlation coefficient close to unity (0.999) and (0.995) for the degradation of MB and CV, respectively, for the zero-order pseudo-kinetics model, which describes the model as highly suitable for the degradation of both dyes by FeNPs compared to other models. The reusability and stability of biosynthesized nano-catalysts were studied and successfully used as efficient catalysts with a slight decrease in the degradation rate more than four times. The results from this study illustrate that green synthesized FeNPs offer a cost-effective, environmentally friendly, and efficient means for the catalytic degradation of organic dyes.

Spectrum-effect relationship between ultra-performance liquid chromatography fingerprints and melanogenic effect of Vernonia anthelmintica effective part.

The fingerprint of Vernonia anthelmintica effective part (VAEP) from 15 different producing areas was established, followed by cluster analysis and principal component analysis. The relationship between the fingerprint and the melanogenesis-promoting activity of VAEP was then analyzed using the grey correlation degree and the orthogonal partial least square method. The characteristic peaks reflecting the pharmacodynamic effect of VAEP were identified as vernodalin, 3,5-O-dicaffeoyl quinic acid (3,5-diCQA), and butin. Based on the distribution characteristics of these components in plants from different habitats and the verification of results from the spectrum-effect relationship, vernodalin and 3,5-diCQA can be used as characteristic components for quality control and pharmacodynamic assessment of V. anthelmintica products. This research establishes a theoretical foundation for planting areas and provides a scientific evaluation of the melanogenesis-promoting effect of V. anthelmintica.

Pyrroloquinolones B-F: Five unusual alkaloids from Vernonia glabra (Steetz) Vatke (Asteraceae).

Five unusual alkaloids featuring a pyrrolo[1,2-a]quinolone skeleton (pyrroloquinolones B-F, 1-5) were isolated from the ethanol extract of the whole plant of Vernonia glabra (Steetz) Vatke, along with sixteen known compounds. Their structures were established by means of spectroscopic (1D and 2D NMR, UV, IR, and ECD) and high resolution mass spectrometric techniques as well as by comparison of their spectroscopic data with those reported in the literature. The ethanol extract and some isolated compounds were assessed for their antibacterial activity against four bacterial strains. The extract was significantly active against Staphylococcus aureus ATCC1026 and S. epidermidis ATCC35984 (MIC = 64 µg/mL). All the tested compounds showed moderate activity against S. epidermidis (16 ≤ MIC ≤ 64 µg/mL). Furthermore, this is the first report on tricyclic pyrrolo[1,2-a]quinolone alkaloids from a plant source. A biosynthetic pathway for the formation of these compounds is also proposed.

Anti-bacterial and anti-inflammatory properties of Vernonia arborea accelerate the healing of infected wounds in adult Zebrafish.

BACKGROUND: Management of wounds and healing under impaired conditions are the major challenges faced globally by healthcare workers. Phytocompounds which are anti-microbial and capable of modulating inflammation contribute to overall wound healing and regain of the lost structure and function especially in wounds impaired with polymicrobial infection. METHODS: An acute cutaneous impaired wound model using adult zebrafish was validated to simulate mammalian wound pathophysiology. This model was used to evaluate phytofractions of Vernonia arborea in the present study, for reduction of infection; myeloperoxidase (MPO) as a marker of infection; neutrophil infiltration and resolution; kinetics of inflammatory cytokines; and wound repair kinetics (viz., nitrite levels and iNoS expression; reepithelisation). RESULTS: Four fractions which were active in-vitro against five selected wound microbes were shown to reduce ex-vivo microbial bioburden upto 96% in the infected wound tissue. The reduction in CFU correlated with the neutrophil kinetics and MPO enzyme levels in the treated, wound infected zebrafish. Expression of pro-inflammatory cytokines (IL-6 and TNF-α) was downregulated while upregulating anti-inflammatory cytokine (IL-10), and nitric oxide signalling with fourfold increase in iNOS expression. The adult zebrafish wound model could well serve as a standard tool for assessing phytoextracts such as V. arborea for wound healing with anti-microbial properties.

Aqueous distillate of mature leaves of Vernonia zeylanica (L.) Less. and Mallotus repandus (Rottler) Müll. Arg. cued from traditional medicine exhibits rapid wound healing properties.

ETHNOPHARMACOLOGICAL RELEVANCE: Sri Lankan traditional medicine uses Vernonia zeylanica and Mallotus repandus broadly for the treatment of a multitude of disease conditions, including wound healing. AIM OF THE STUDY: We aimed to scientifically validate the safety and efficacy of wound healing of an aqueous distillate of Vernonia zeylanica and Mallotus repandus (ADVM) mature leaves, tested on primary human dermal fibroblasts. MATERIALS AND METHODS: Human dermal fibroblasts isolated from clinical waste from circumcision surgery were characterized by flowcytometry and trilineage differentiation. The MTT dye reduction assay, and the ex vivo wound healing scratch assay established wound healing properties of ADVM using the primary human dermal fibroblast cell line. Upregulation of genes associated with wound healing (MMP3, COL3A1, TGFB1, FGF2) were confirmed by RT qPCR. GC-MS chromatography evaluated the phytochemical composition of ADVM. RESULTS: Compared to the synthetic stimulant, ß fibroblast growth factor, ADVM at 0.25% concentration on the primary dermal fibroblast cell line exhibited significant ex vivo, (i) 1.7-fold % cell viability (178.7% vs 304.3 %, p < 0.001), (ii) twofold greater % wound closure (%WC) potential (47.74% vs 80.11%, p < 0.001), and (iii) higher rate of % WC (3.251 vs 3.456 % WC/h, p < 0.05), sans cyto-genotoxicity. Up regulated expression of FGF2, TGFB1, COL3A1 and MMP3, genes associated with wound healing, confirmed effective stimulation of pathways of the three overlapping phases of wound healing (P < 0.05). GC-MS profile of ADVM characterized four methyl esters, which may be posited as wound healing phytochemicals. CONCLUSIONS: Exceeding traditional medicine claims, the exvivo demonstration of rapid skin regeneration, reiterated by upregulated expression of genes related to wound healing pathways, sans cytotoxicity, propounds ADVM, cued from traditional medicine, as a potential safe and effective natural stimulant for rapid wound-healing. Additionally, it may serve as an effective proliferative stimulant of dermal fibroblasts for cell therapy, with potential in reparative and regenerative therapy of skin disorders.

Stigmastane-type steroid saponins from the leaves of Vernonia amygdalina and their α-glucosidase and xanthine oxidase inhibitory activities.

Two new vernonioside K (1) and vernonioside L (2) and four known Δ7,9(11) stigmastane-type steroidal saponins-vernonioside B2 (3), vernoniacum B (4), vernonioside B1 (5), and vernoamyoside A (6)-were isolated from the leaves of Vernonia amygdalina. Their structures were determined by comprehensive spectroscopic analysis with one-dimensional nuclear magnetic resonance, two-dimensional nuclear magnetic resonance, and high-resolution mass spectrometry. All isolated compounds (1-6) were evaluated to determine their inhibitory effects on α-glucosidase and xanthine oxidase. Among them, two new compounds 1 and 2 showed significant inhibition of α-glucosidase with IC50 values of 78.56 ± 7.28 and 14.74 ± 1.57 (µM), respectively, comparable with acarbose as a positive control (127.53 ± 1.73 µM); none of these compounds inhibited xanthine oxidase activity. Compounds 1 and 2 are promising candidates for the development of antidiabetic agents from natural sources.

Therapeutic Benefit of Vernonia amygdalina in the Treatment of Diabetes and Its Associated Complications in Preclinical Studies.

Diabetes mellitus (DM), a complex heterogeneous metabolic disorder characterized by a defect in the function of insulin, is on the rapid rise globally. Sustained hyperglycemia which is a major sign of DM is linked to the generation of reactive oxygen species which promotes adverse complications of the disorder. Traditional herbal treatment of DM is a common practice in Africa and other tropical parts of the world. Vernonia amygdalina (VA), one of the highly researched species in the Asteraceae family, has proven to possess potent antidiabetic properties. Several phytochemicals identified in multiple extracts from VA are purported to be responsible for the antidiabetic potential of the plant. In this review, we discuss the therapeutic potential of VA in diabetes and its associated complications. We appraise the current evidence and further suggest potential areas that could be effectively exploited in future VA research on diabetes.

Blood pressure lowering effects of Vernonia amygdalina Del. Aqueous fraction on hypertensive Wistar Kyoto rats.

OBJECTIVES: Vernonia amygdalina (VA) is a plant that consumed as vegetable by Indonesians contained numerous secondary metabolites. VA's pharmacological action, including its antioxidant properties, anticancer, antidiabetic, and hepatoprotective. The purpose of this research is to reveal the activity of Vernonia amygdalina. leafs aqueous fraction (VALAF) as a blood pressure-lowering agent in hypertensive model. METHODS: Combination of prednisone and NaCl were used as hypertensive inducer. The animals were split into five different groups, normal control group treated with distilled water, treatment VALAF groups with dose of 10; 20 and 40 mg/kg BW respectively, while the last group was treated with captopril at dose of 2.25 mg/kg BW. All animals were given an oral treatment for 15 days. On days 5, 10, and 15, systolic and diastolic blood pressure, heart rate (HR), mean arterial pressure (MAP), and blood flow (BF) were all measured. On days 0 and 15, NO level were assessed. All data were analyzed using two-way ANOVA, and Duncan Multiple Range Test. RESULTS: The V. amygdalina leaf aqueous fraction has blood pressure lowering activity. The blood pressure parameter of the rats treated with VALAF were lower as compared to the normal control group (p<0.05). NO levels in the VALAF group were not significantly higher than in the normal control group (p>0.05). The VALAF 20 give the greatest percentage of decrease in blood pressure, heart rate and blood volume on the 15th day of examination. CONCLUSIONS: These study indicated that V. amygdalina leaf aqueous fraction has the potential to be an alternative therapy for managing blood pressure in hypertensive animal models.

Insight on Vernonia Plant for its Pharmacological Properties: A Review.

Vernonia is a woody shrub of the family Asteraceae. Over 1500 species are distributed in tropical and subtropical regions of Africa and Asia. There are more than 54 species known to possess similar morphological features with the characteristic bitter taste. The pharmacological properties of different parts like seeds, leaves, and roots are well documented in folk medicine. They are rich in biologically active constituents such as alkaloids, phenolics, flavonoids, terpenoids, steroid tannins, and carotenoids having broad therapeutic activities like antiinflammatory, hypoglycemic, hyperlipidemia, antimicrobial, antitumor, antioxidative, antiproliferative, antihypertensive, hepatoprotective, etc. The present study summarizes and discusses the phytochemical profile, pharmacological properties, and toxicological effects of the Vernonia plant.

Polyoxygenated Stigmastane-Type Steroids from Vernonia kotschyana Sch. Bip. ex Walp. and Their Chemophenetic Significance.

Four polyoxygenated stigmastanes (1-4) alongside known analogues (7-8) and flavonoids (5-6) were isolated from a dichloromethane/methanol (1:1, v/v) extract of the whole plant of Vernonia kotschyana Sch. Bip. ex Walp. (Asteraceae). Their structures were determined by means of spectroscopic and spectrometric analysis. The relative stereochemistry of the new compounds was established and confirmed via biosynthesis evidence and cyclization of 1 under acidic conditions. A plausible biosynthetic pathway to the new compounds and the chemophenetic significance of the isolated constituents were also discussed. The crude extract, fractions, and compounds (1-3) were assessed for their antibacterial activity against five highly prevalent bacterial strains. The fractions and compounds showed low to moderate activity with minimal inhibitory concentrations (MICs) > 125 µg/mL.

Genetic diversity and population structure of Vernonia amygdalina Del. in Uganda based on genome wide markers.

Determining the extent and distribution of genetic diversity is an essential component of plant breeding. In the present study, we explored the genetic diversity and population structure of Vernonia amygdalina, a fodder, vegetable and medicinal species of Africa and some parts of Yemen. Most empirical studies demonstrate that populations that are separated by geographic or ecological factors may experience genetic differentiation resulting from restricted gene flow between populations. A total of 238 individuals were sampled from two populations: i) Lake Victoria crescent (LVC) and ii) Southern and Eastern Lake Kyoga basin (SEK) agroecological zones of Uganda and genotyped using DArT platform. Of the two populations, the overall mean observed heterozygosity (Ho) was low to medium (Ho = 0.07[silicoDArTs] and 0.2[SNPs]). Inbreeding levels were also very low (-0.04 to -0.08) suggesting the presence of random mating. Partitioning of genetic structure in the two populations indicated that SEK exhibited a higher genetic diversity than LVC. The principal coordinates analysis (PCA) showed no geographical structuring, consistent with the low genetic differentiation (Fst = 0.00) and the low Euclidean genetic distance (1.38-1.39) between the LVC and SEK populations. However, STRUCTURE analysis with admixture models revealed weak possible genetic clusters with very small genetic distance among them. Overall, the results suggest low genetic diversity and weak genetic differentiation between the two populations. One possible explanation of the results could be the presence of human assisted gene flow over long distances.

Evaluation of the Antibacterial and Antibiofilm Effects of Ethyl Acetate Root Extracts from Vernonia adoensis (Asteraceae) against Pseudomonas aeruginosa.

There is an increase in mortality and morbidity in the health facilities due to nosocomial infections caused by multidrug-resistant nosocomial bacteria; hence, there is a need for new antibacterial agents. Vernonia adoensis has been found to possess medicinal value. Plant phytochemicals may have antimicrobial activity against some resistant pathogens. The antibacterial efficacy of root extracts against Staphylococcus aureus and Pseudomonas aeruginosa was investigated using the microbroth dilution method. All extracts from the roots had an inhibitory effect on the growth of both bacteria, with the most susceptible being P. aeruginosa. The most potent extract was the ethyl acetate extract which caused a percentage inhibition of 86% against P. aeruginosa. The toxicity of the extract was determined on sheep erythrocytes, and its effect on membrane integrity was determined by quantifying the amount of protein and nucleic acid leakage from the bacteria. The lowest concentration of extract used, which was 100 µg/ml, did not cause haemolysis of the erythrocytes, while at 1 mg/ml of the extract, 21% haemolysis was observed. The ethyl acetate extract caused membrane impairment of P. aeruginosa, leading to protein leakage. The effect of the extract on the biofilms of P. aeruginosa was determined in 96-microwell plates using crystal violet. In the concentration range of 0-100 µg/ml, the extract inhibited the formation of biofilms and decreased the attachment efficiency. The phytochemical constituents of the extract were determined using gas chromatography-mass spectrometry. Results of analysis showed the presence of 3-methylene-15-methoxy pentadecanol, 2-acetyl-6-(t-butyl)-4-methylphenol, 2-(2,2,3,3-tetrafluoropropanoyl) cyclohexane-1,4-dione, E,E,Z-1,3,12-nonadecatriene-5,14-diol, and stigmasta-5,22-dien-3-ol. Fractionation and purification will elucidate the potential antimicrobial compounds which are present in the roots of V. adoensis.

Bisabolane-Type Sesquiterpenoids with a Tetrahydrofuran or Tetrahydropyran Ring from Vernonia solanifolia.

Phytochemical investigation of the aerial parts of Vernonia solanifolia resulted in the isolation of 23 new highly oxidized bisabolane-type sesquiterpenoids (1-23). Structures were determined by interpretation of spectroscopic data, single-crystal X-ray diffraction analysis, and time-dependent density functional theory electronic circular dichroism calculations. Most compounds possess a rare tetrahydrofuran (1-17) or tetrahydropyran ring (18-21). Compounds 1/2 and 11/12 are pairs of epimers isomerized at C-10, while compounds 9/10 and 15/16 are isomerized at C-11 and C-2, respectively. The anti-inflammatory effect in lipopolysaccharide (LPS)-stimulated RAW264.7 macrophages was evaluated for pure compounds. Compound 9 inhibited LPS-stimulated NO production at the concentration of 80 µM. It showed an anti-inflammatory effect by suppressing the activation of the NF-κB signaling pathway.