Vernonia polyanthes Less. (Asteraceae Bercht. & Presl), a Natural Source of Bioactive Compounds with Antibiotic Effect against Multidrug-Resistant Staphylococcus aureus.

Vernonia polyanthes is a medicinal plant used to treat many disorders, including infectious diseases. This study investigated the chemical constituents and the antibacterial activity of V. polyanthes leaf rinse extract (Vp-LRE). The chemical characterization of Vp-LRE was established using ultra-high performance liquid chromatography coupled to quadrupole time-of-flight mass spectrometry (UHPLC/Q-TOF-MS), and glaucolide A was identified through 1H and 13C nuclear magnetic resonance (NMR) and mass fragmentation. The cytotoxicity was evaluated using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT). The antibacterial activity was assessed by minimal inhibitory concentration and minimal bactericidal concentration. Interactions between ligands and beta-lactamase were evaluated via molecular docking. UHPLC/Q-TOF-MS detected acacetin, apigenin, chrysoeriol, isorhamnetin, isorhamnetin isomer, kaempferide, 3',4'-dimethoxyluteolin, 3,7-dimethoxy-5,3',4'-trihydroxyflavone, piptocarphin A and glaucolide A. Vp-LRE (30 µg/mL) and glaucolide A (10 and 20 µg/mL) were cytotoxic against RAW 264.7 cells. Glaucolide A was not active, but Vp-LRE inhibited the Staphylococcus aureus, methicillin-resistant S. aureus (MRSA), Escherichia coli, Salmonella Choleraesuis and Typhimurium, with a bacteriostatic effect. The compounds (glaucolide A, 3',4'-dimethoxyluteolin, acacetin and apigenin) were able to interact with beta-lactamase, mainly through hydrogen bonding, with free energy between -6.2 to -7.5 kcal/mol. These results indicate that V. polyanthes is a potential natural source of phytochemicals with a significant antibiotic effect against MRSA strains.

In vitro hematotoxicity of Vernonanthura polyanthes leaf aqueous extract and its fractions.

Vernonanthura polyanthes, popularly known as 'assa-peixe', is widely used in Brazil for therapeutic purpose mainly to treat respiratory tract problems. However, few studies investigated its chemical safety. In this way, we first obtained the V. polyanthes leaf aqueous extract (VpLAE) and three fractions (aqueous; n-butanol, n-BF; and ethyl acetate), and we chemically characterized this material. Then, the cytogenotoxic potential of the VpLAE and its fractions was investigated against human erythrocytes and lymphocytes using Trypan blue exclusion test of cell viability and CometChip. The phytochemical screening of V. polyanthes leaf revealed the presence of total phenolic compounds, flavonoids, tannins, coumarins, terpenic compounds, and cardioactive heterosides. n-BF presented the highest total phenolic, flavonoids, and tannins contents and, consequently, the highest antioxidant activity, according to the DPPH free radical scavenging method. Although the VpLAE and its fractions did not cause death of erythrocytes, the cells acquired an echinocytic form. Regarding lymphocytes, VpLAE and its fractions presented cytotoxicity and genotoxicity. When VpLAE or its fractions were co-treated with doxorubicin (DXR), a recognized cytotoxic drug, we observed an enhancement of DXR cytotoxicity against lymphocytes, but the DXR genotoxicity decreased around 15%. Since the VpLAE and its fractions increased the DXR cytotoxicity and decreased its genotoxicity, further studies should be conducted for the development of an adjuvant drug from this extract to reduce the side effects of chemotherapy. Moreover, the indiscriminate use of 'assa-peixe' by local people should be discouraged.

Composition and leishmanicidal activity of the essential oil of Vernonia polyanthes Less (Asteraceae).

The composition of the essential oil (EO) from leaves of Vernonia polyanthes and the evaluation of its leishmanicidal potential are reported here for the first time. The oil obtained by hydrodistillation was analysed by combination of GC and GC/MS. Thirty-five compounds were identified, representing 91.8% of the oil composition. The oil consists primarily of monoterpenes (37.1%), sesquiterpenes (26.3%) and oxygenated sesquiterpenes (23.9%), myrcene (34.3%), zerumbone (15.8%), bicyclogermacrene (8.9%), α-humulene (4.8%) and germacrene D (4.3%) being the major constituents. Activity against Leishmania infantum was determined using the tetrazolium dye (MTT) colorimetric method. The oil, as well as zerumbone, one of its major constituents, showed significant leishmanicidal activity, with IC50 values of 19.4 and 9.0 µg/ml, respectively. Cytotoxicity in macrophages cells was evaluated using the MTT colorimetric assay. The EO showed the CC50 < 10 µg/ml to macrophages cells.

Vernonia polyanthes (Spreng. ) Less.: uma visão geral da sua utilização como planta medicinal, composição química e atividades farmacológicas / Vernonia polyanthes (Spreng. ) Less.: an overview of its use as medicinal plant, chemical composition and pharmacological activities

As aplicações da biodiversidade brasileira em saúde são abrangentes, mas ainda não têm sido bem exploradas oficialmente, considerando o pequeno número de espécies vegetais listadas em compêndios oficiais para uso medicinal. Das espécies conhecidas como assa-peixe, empregadas comumente pela população há muitos anos para diversos fins, sobretudo nas afecções respiratórias, Vernonia polyanthes (Spreng.) Less. é a única regulamentada para utilização no Brasil, indicada como expectorante no Formulário de Fitoterápicos da Farmacopeia Brasileira. Seu cultivo é também praticado em Arranjos Produtivos Locais (APLs) de plantas medicinais, os quais possuem importante papel na conservação e sustentabilidade dos recursos naturais e na economia das famílias que dependem dessa parceria. Esta difusão de uso é característica de diversas espécies que compõem a Relação Nacional de Plantas Medicinais de Interesse ao SUS, mas ainda sem monografias que respaldem os critérios de qualidade para seu uso seguro, conforme o preconizado pela Organização Mundial de Saúde para plantas medicinais. O objetivo deste trabalho foi apresentar uma visão geral do conhecimento científico desta espécie, com foco em sua utilização na fitoterapia, identificação química e atividades farmacológicas, na expectativa de subsidiar a elaboração de monografias de Vernonia polyanthes, agregando valor e qualidade nas atividades dos APLs a longo prazo.(AU)

The applications of the Brazilian biodiversity in health are comprehensive, but still officially underused, since the number of medicinal plants listed in official compendia is minimal. Of several species popularly known as assa-peixe, which have been in common use by the population for many years with diverse pharmacological actions, particularly that related to respiratory affections, Vernonia polyanthes (Spreng.) Less. is the only one listed for use by Herbal Formulary of the Brazilian Pharmacopoeia, indicated as expectorant. It is also cultivated by Local Productive Arrangements (LPA) of medicinal plants, which have an important role in the conservation and sustainability of natural resources, as well as for the economic status of families that depend on this partnership. Several species widely used in folk medicine that compose the National List of Medicinal Plants of Interest to Unified Health System have no monograph that support the quality criteria for the safe use of medicinal plants, following the recommendations of World Health Organization. The present study aims at providing an overview of the scientific knowledge about this species, focusing on its use in herbal medicine, phytochemical identification, and pharmacological activities. This overview can help the elaboration of monographs of Vernonia polyanthes, adding value and quality in the LPA activities at long term.(AU)

Evidence of Bioactive Compounds from Vernonia polyanthes Leaves with Topical Anti-Inflammatory Potential.

Vernonia polyanthes Less. (Asteraceae), popularly known as "assa-peixe", is a plant species used in Brazilian traditional medicine for the treatment of cutaneous damage, cicatrization, inflammation, and rheumatism. Based on these ethnopharmacological findings, the current study evaluated the topical anti-inflammatory effects of the hexane (HEVP) and ethyl acetate (EAEVP) extracts from V. polyanthes leaves in experimental models of skin inflammation. Chemical characterization was carried out by HPLC-UV/DAD analysis. Anti-inflammatory activity was evaluated using Croton oil-, arachidonic acid (AA)-, phenol-, ethyl phenylpropiolate (EPP)-, and capsaicin-induced ear edema models in mice. Histopathological evaluation and measurements of myeloperoxidase (MPO) and N-acetyl-ß-d-glucosaminidase (NAG) enzymes were also performed. Rutin, luteolin, and apigenin were identified in EAEVP. Topically applied HEVP and EAEVP significantly (p < 0.05, p < 0.01 or p < 0.001) reduced edema induced by five different irritants at the doses tested (0.1, 0.5 and 1.0 mg/ear). Histopathological analysis revealed a reduction of edema, inflammatory cell infiltration, and vasodilation. In addition, the enzymes activity (MPO and NAG) in the ear tissues was reduced by the topical treatment of HEVP and EAEVP (p < 0.05, p < 0.01 or p < 0.001). The results suggest that V. polyanthes leaves are effective against cutaneous damage, which support its traditional use and open up new possibilities for the treatment of skin disorders.

Vernonanthura polyanthes leaves aqueous extract enhances doxorubicin genotoxicity in somatic cells of Drosophila melanogaster and presents no antifungal activity against Candida spp / O extrato aquoso das folhas de Vernonanthura polyanthes potencializa a genotoxicidade da doxorrubicina em células somáticas de Drosophila melanogaster e não apresenta atividade antifúngica contra Candida spp

Abstract Vernonanthura polyanthes (Spreng.) A.J. Vega & Dematt. (Asteraceae), known as “assa-peixe”, has been used in ethnomedicine for the treatment of various diseases such as bronchitis, pneumonia, hemoptysis, persistent cough, internal abscesses, gastric and kidney stone pain. Moreover, some studies demonstrated that species of Genus Vernonia present antifungal activity. Due to the biological relevance of this species, the aim of this study was to investigate the toxic, genotoxic, antigenotoxic and antifungal potential of V. polyanthes leaves aqueous extract in somatic cells of Drosophila melanogaster or against Candida spp. The aqueous extract of the plant showed no toxic, genotoxic and antigenotoxic activity in the experimental conditions tested using the wing somatic mutation and recombination test (SMART/wing). However, when the extract was associated with doxorubicin, used in this work as a positive control, the mutagenic potential of doxorubicin was enhanced, increasing the number of mutations in D. melanogaster somatic cells. In the other hand, no inhibitory activity against Candida spp. was observed for V. polyanthes leaves aqueous extract using agar-well diffusion assay. More studies are necessary to reveal the components present in the V. polyanthes leaves aqueous extract that could contribute to potentiate the doxorubicin genotoxicity.

Resumo Vernonanthura polyanthes (Spreng.) A.J. Vega & Dematt. (Asteraceae), conhecida como “assa-peixe”, tem sido utilizada na medicina popular para o tratamento de várias doenças, como bronquite, pneumonia, hemoptise, tosse persistente, abcessos internos, afecções gástricas e cálculo renal. Além disso, alguns estudos já demonstraram que espécies do Gênero Vernonia apresentam atividade antifúngica. Devido à relevância biológica dessa espécie, o objetivo deste estudo foi investigar os efeitos citotóxico, genotóxico, antigenotóxico e antifúngico do extrato aquoso das folhas de V. polyanthes em células somáticas de Drosophila melanogaster ou contra Candida spp. O extrato aquoso da planta não apresentou atividade citotóxica, genotóxica e antigenotóxica nas condições experimentais testadas usando o teste de recombinação e mutação somática em asa (SMART-asa). No entanto, quando o extrato foi associado com a doxorrubicina, utilizada neste trabalho como controle positivo, o potencial mutagênico da doxorrubicina foi potencializado, aumentando o número de mutações em células somáticas de D. melanogaster. Por outro lado, nenhuma atividade inibitória contra Candida spp. foi observada utilizando o extrato aquoso das folhas de V. polyanthes por meio do método de difusão em ágar. Mais estudos são necessários para desvendar os componentes presentes no extrato aquoso das folhas de V. polyanthes que possam contribuir para potencializar a genotoxicidade da doxorrubicina.

Antileishmanial activity of compounds produced by endophytic fungi derived from medicinal plant Vernonia polyanthes and their potential as source of bioactive substances.

The purpose of this work was to evaluate the antileishmanial activity of endophytic fungi isolated from leaves of Vernonia polyanthes plant and their prospective use in the discovery of bioactive compounds. Sixteen endophytes were isolated by using potato dextrose agar medium and submitted to cultivation in rice medium. The fungal cultures were extracted with ethanol and used as crude extracts for testing their antileishmanial activity. The most active ethanol extract was obtained from P2-F3 strain, which was identified as Cochliobolus sativus by ITS rRNA gene sequence data. Followed by a bioassay-guided fractionation, the cochlioquinone A, isocochlioquinone A and anhydrocochlioquinone A compounds were isolated from the crude extracts and demonstrated to inhibit the parasites. From the present work, it is possible to conclude that endophytic fungi derived from medicinal plant V. polyanthes may be considered promising source for the discovery of bioactive compounds.

Antinociceptive and anti-inflammatory effects of ethanol extract from Vernonia polyanthes leaves in Rodents.

The ethanol extract from Vernonia polyanthes leaves (EEVP) was investigated for antinociceptive and anti-inflammatory effects at the doses (p.o.) of 100, 200 and 400 mg/kg in animal models. The extract reduced the number of abdominal contortions by 16.75% and 31.44% at a dose of 200 and 400 mg/kg, respectively. The results obtained showed that EEVP exerted a significant antinociceptive effect in the two phases of formalin. The EEVP increased the reaction time on a hot plate at the doses of 100, 200 and 400 mg/kg after 90 min of treatment. The paw edema was reduced by EEVP at the doses of 100, 200 and 400 mg/kg after 4 h of application of carrageenan. Doses of 200 and 400 mg/kg, administered 4 h before the carrageenan injection, significantly reduced the exudate volume (29.25 and 45.74%, respectively) and leukocyte migration (18.19 and 27.95%, respectively). These results suggest that V. polyanthes can be an active source of substances with antinociceptive and anti-inflammatory activities.