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1.
PLoS Negl Trop Dis ; 16(4): e0010341, 2022 04.
Artigo em Inglês | MEDLINE | ID: mdl-35468134

RESUMO

Hyperreactive onchocerciasis (HO) is characterized by a severe skin inflammation with elevated Th17-Th2 combined responses. We previously demonstrated the anthelminthic activity of Aframomum melegueta (AM), Xylopia aethiopica (XA) and Khaya senegalensis (KS) used by traditional healers to treat helminthiasis in the endemic area of Togo. However, their effect on severe onchocerciasis is poorly investigated. The present study aimed to investigate the anti-Th17 and anti-Th2 effects of hydro-ethanolic extracts of AM, XA and KS during HO. Onchocerca volvulus-infected individuals were recruited in the Central region of Togo in 2018. Isolated peripheral blood mononuclear cells (PBMCs) from both generalized onchocerciasis (GEO) and HO forms were activated with anti-CD3 and anti-CD28 monoclonal antibodies in the presence or absence of the hydro-ethanolic extracts of AM, XA and KS as well as their delipidated, deproteinized and deglycosylated fractions. After 72 hours, cytokines were assayed from cell culture supernatants. Then, flow cytometry was used to investigate the effects of the extracts on cell activation, proliferation, intracellular cytokines and T cells transcription factors. The production of both Th17 and Th2 cytokines IL-17A and IL-5 were significantly inhibited upon T-cell receptor (TCR) activation in the presence of the hydro-ethanolic extracts of AM, XA and KS in HO individuals' PBMCs in vitro. AM and XA inhibited CD4+RORC2+IL-17A+ and CD4+GATA3+IL-4+ cell populations induction. This inhibition was not Th1 nor Treg-dependent since both IFN-γ and IL-10 were also inhibited by the extracts. AM and XA did not interfere with T cell activation and proliferation for their inhibitory pathways. Lipid and protein compounds from AM and XA were associated with the inhibition of IL-17A. This study showed that in addition to their anthelminthic effects, hydro-ethanolic extracts of Aframomum melegueta, Xylopia aethiopica and Khaya senegalensis could downregulate both Th17 and Th2 responses and prevent the severe skin disorder observed.


Assuntos
Meliaceae , Oncocercose , Xylopia , Zingiberaceae , Citocinas/metabolismo , Humanos , Interleucina-17/metabolismo , Leucócitos Mononucleares , Extratos Vegetais/farmacologia , Células Th1 , Células Th17
2.
Molecules ; 27(3)2022 Jan 28.
Artigo em Inglês | MEDLINE | ID: mdl-35164181

RESUMO

Compounds derived from plants have several anticancer properties. In the current study, one guaiane-type sesquiterpene dimer, vieloplain F, isolated from Xylopia vielana species, was tested against B-Raf kinase protein (PDB: 3OG7), a potent target for melanoma. A comprehensive in silico analysis was conducted in this research to understand the pharmacological properties of a compound encompassing absorption, distribution, metabolism, excretion, and toxicity (ADMET), bioactivity score predictions, and molecular docking. During ADMET estimations, the FDA-approved medicine vemurafenib was hepatotoxic, cytochrome-inhibiting, and non-cardiotoxic compared to the vieloplain F. The bioactivity scores of vieloplain F were active for nuclear receptor ligand and enzyme inhibitor. During molecular docking experiments, the compound vieloplain F has displayed a higher binding potential with -11.8 kcal/mol energy than control vemurafenib -10.2 kcal/mol. It was shown that intermolecular interaction with the B-Raf complex and the enzyme's active gorge through hydrogen bonding and hydrophobic contacts was very accurate for the compound vieloplain F, which was then examined for MD simulations. In addition, simulations using MM-GBSA showed that vieloplain F had the greatest propensity to bind to active site residues. The vieloplain F has predominantly represented a more robust profile compared to control vemurafenib, and these results opened the road for vieloplain F for its utilization as a plausible anti-melanoma agent and anticancer drug in the next era.


Assuntos
Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/farmacologia , Sesquiterpenos/química , Sesquiterpenos/farmacologia , Xylopia/química , Antineoplásicos Fitogênicos/isolamento & purificação , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Humanos , Melanoma/tratamento farmacológico , Melanoma/metabolismo , Simulação de Acoplamento Molecular , Proteínas Proto-Oncogênicas B-raf/antagonistas & inibidores , Proteínas Proto-Oncogênicas B-raf/metabolismo , Sesquiterpenos/isolamento & purificação
3.
J Biomol Struct Dyn ; 40(1): 484-498, 2022 01.
Artigo em Inglês | MEDLINE | ID: mdl-32876526

RESUMO

Natural products of herbal origin are prodigious to display diverse pharmacological activities. In the present study, five guaiane-type sesquiterpene dimers, xylopidimers A - E (1-5), isolated from Xylopia vielana species were tested against COX-2 protein target (PDB: 1CX2), a potent target for anti-inflammatory agents. To better understand the pharmacological properties of all these compounds, in this work, a systemic in silico study was performed on xylopidimers A-E using molecular docking, ADMET analysis and MD simulations. During ADMET predictions the two compounds xylopidimer C, D displayed best results as compared to others. The compound xylopidimer C was further evaluated for its MD simulations and its molecular interactions with COX2 complex showed clear interactions with active gorge of the enzyme through hydrogen bonding as well as hydrophobic contacts. The xylopidimer C has shown the best binding potential with -10.57Kcal/mol energy with 17.92 nano molar of predicted inhibition constant better than Ibuprofen and Felbinac. These findings provide enough significant information for designing and developing novel targeted base anti-inflammatory drugs from guaiane dimers.


Assuntos
Xylopia , Anti-Inflamatórios/farmacologia , Ciclo-Oxigenase 2 , Simulação de Acoplamento Molecular , Estrutura Molecular , Sesquiterpenos de Guaiano
4.
Nat Prod Res ; 36(5): 1288-1295, 2022 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-33487063

RESUMO

Two ent-kaurene diterpenoids, ent-15-ß-acetyloxy-kaur-16-en-19-oic acid (xylopic acid) 1 and ent-7-oxo-kaur-16-en-19-oic acid 2 were isolated from the fruits of Xylopia aethiopica. Chemical manipulation of xylopic acid yielded ent-kaurane derivatives 3, 4, 5, and 6. Their structures were elucidated by spectroscopic analysis, including 1 D- and 2 D-NMR spectroscopies. The antiproliferative activities of compounds 1, 2, 3, 4, and 6 were tested on breast MCF7 and SkBr3, endometrial Ishikawa, ovarian BG-1, mesothelioma IST-MES1 and hepatocellular HepG2 human tumor cells, and on mammalian MRC-10 fibroblast cells. Ketone 2 showed significant antiproliferative activity against MFC7 human breast cancer cells (IC50 = 3 ± 1 µM) and A549 pulmonary adenocarcinoma (8 ± 1 µM), that was higher than the well-known anti-cancer agent cisplatin (IC50 = 19 ± 3 and 15 ± 4 µM, respectively).[Formula: see text].


Assuntos
Diterpenos do Tipo Caurano , Diterpenos , Xylopia , Animais , Diterpenos do Tipo Caurano/química , Frutas , Células Hep G2 , Humanos
5.
Anticancer Agents Med Chem ; 22(4): 731-746, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-34645380

RESUMO

BACKGROUND: Natural products from herbs are abundant and display powerful anti-cancer activities. OBJECTIVES: In the current study, B-Raf kinase protein (PDB: 3OG7), a potent target for melanoma, was tested against two guaiane-type sesquiterpene dimers, xylopin E-F, obtained from Xylopia vielana. METHODS: In this work, a systematic in silico study using ADMET analysis, bioactivity score forecasts, and molecular docking along with its simulations was conducted to understand compounds' pharmacological properties. RESULTS: During ADMET predictions of both the compounds, xylopin E-F displayed a safer profile in hepatotoxicity and cytochrome inhibition, and only xylopin F was shown to be non-cardiotoxic compared to the FDA-approved drug vemurafenib. Both the compounds were proceeded to molecular docking experiments using Autodock docking software, and both the compounds, xylopin E-F, displayed higher binding potential with -11.5Kcal/mol energy compared to control vemurafenib (-10.2 Kcal/mol). All the compounds were further evaluated for their MD simulations, and their molecular interactions with the B-Raf kinase complex displayed precise interactions with the active gorge of the enzyme by hydrogen bonding. CONCLUSION: Overall, xylopin F had a better profile relative to xylopin E and vemurafenib, and these findings indicated that this bio-molecule could be used as an anti-melanoma agent and as a possible anti-cancer drug in the future. Therefore, this is a systematically optimized in silico approach for creating an anti-cancer pathway for guaiane dimers against the backdrop of its potential for future drug development.


Assuntos
Melanoma , Xylopia , Humanos , Informática , Melanoma/tratamento farmacológico , Simulação de Acoplamento Molecular , Simulação de Dinâmica Molecular , Estrutura Molecular , Proteínas Proto-Oncogênicas B-raf , Sesquiterpenos de Guaiano , Vemurafenib , Xylopia/química
6.
J Ethnopharmacol ; 280: 114406, 2021 Nov 15.
Artigo em Inglês | MEDLINE | ID: mdl-34245833

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Xylopia staudtii is a medicinal plant which fruits are traditionally used in western Cameroon as a spice in the preparation of soups known for their abdominal cramp relieving properties. Often identified as Xylopia africana, its bark is used in the treatment of dysentery in Mont Cameroun localities. This plant could therefore contain active ingredients against intestinal pathogens, including Shigella spp, which are responsible of the deathly dysenteric diarrhoea. AIM OF THE STUDY: This study aims to assess the efficacy of the hydroethanolic extract from Xylopia staudtii bark in immunodepressed mice infected with Shigella flexneri. MATERIALS AND METHODS: Qualitative detection of compounds in the crude extract was done using UPLC-DAD-(HR) ESI-MS analysis in an attempt to link the activity to the chemical composition. The MIC and the MBC of the extract was determined using broth dilution method. Shigellosis was induced by intraperitoneal administration of Shigella flexneri to immunodepressed mice pretreated with streptomycin. These infected mice were then treated with the extract (100, 200 and 400 mg/kg), and reference substances (ciprofloxacin and saline). During the 9 days of treatment, animal morphology, fecal pathology and deaths were recorded. At the end of the treatment period, blood and organs were collected from any surviving animals for hematological, biochemical and histopathological analyses. RESULTS: The extract was found to be significantly active, with a bactericidal effect against Shigella and a bacteriostatic effect against Escherichia coli. It was able to reduce and stop the faecal pathology caused by the infection in mice, as well as the rate of deaths which was brought to zero (0) in animal treated at 400 mg/kg. The bacteria load in faeces was reduced by 100% in animal treated at 400 mg/kg. Xylopia staudtii extract elicited anti-inflammatory properties by reducing MPO activity and Lcn2 intestinal level. It also prevents damages in the intestinal tissue and the shortening of colon which characterise Shigella infection. The serum level of ASAT, ALAT, bilirubin, urea and creatinine in animals treated with the extract was similar to those of normal animal used in the study. These activities of the plant may be due at least in part to the presence of ent-kauran type diterpens such as kaurenoic acid identified in the extract. CONCLUSION: These findings support the usage of Xylopia staudtii as an antimicrobial against bacillary dysentery, making this plant a potential candidate for the formulation of an improved standardized traditional medicine.


Assuntos
Antibacterianos/farmacologia , Extratos Vegetais/farmacologia , Shigella flexneri/efeitos dos fármacos , Xylopia/química , Animais , Antibacterianos/administração & dosagem , Antibacterianos/isolamento & purificação , Anti-Inflamatórios/administração & dosagem , Anti-Inflamatórios/isolamento & purificação , Anti-Inflamatórios/farmacologia , Camarões , Cromatografia Líquida de Alta Pressão , Ciprofloxacina/farmacologia , Relação Dose-Resposta a Droga , Disenteria Bacilar , Feminino , Masculino , Camundongos , Camundongos Endogâmicos BALB C , Extratos Vegetais/administração & dosagem , Espectrometria de Massas por Ionização por Electrospray
7.
Pak J Pharm Sci ; 34(2): 599-606, 2021 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-34275835

RESUMO

Annonacea species have been reported to possess antitumor properties. However, the in vitro and in vivo antitumor activities of Xylopia aromatica (Annonacea) have not yet been elucidated. This study aimed to investigate the effects of Xylopia aromatica leaves hexane fraction (XaHF) on Ehrlich ascites carcinoma cells lines (EAC), both in vitro and in vivo. In vitro assays revealed a significant cytotoxic effect with the two lower XaHF concentrations (62.5 and 32.3mg/mL). EAC (2.5x106 cells) were inoculated in the right flank of Swiss mice, and the animals were treated intraperitoneally with 32.3mg kg-1 of XaHF daily, for 20 days. Our findings indicate that XaHF suppressed the growth of EAC in vivo, with a significant decrease (46%) in tumor volume. There was also a decrease in the necrosis area (71%), inflammatory infiltrate, and MMP-2 expression. High-Performance Liquid Chromatography with Diode Array Detector (HPLC-DAD) identified secondary metabolites possibly related to phenolic acids, flavonoids, and alkaloids. Thus, the results confirmed the antitumoral activity that may be related to the presence of the identified metabolites in XaHF extract.


Assuntos
Carcinoma de Ehrlich/metabolismo , Proliferação de Células/efeitos dos fármacos , Metaloproteinase 2 da Matriz/efeitos dos fármacos , Extratos Vegetais/farmacologia , Folhas de Planta , Xylopia , Alcaloides/química , Animais , Aporfinas/química , Carcinoma de Ehrlich/patologia , Catequina/química , Linhagem Celular Tumoral , Ácido Clorogênico/química , Cromatografia Líquida de Alta Pressão , Regulação para Baixo , Flavonoides/química , Ácido Gálico/química , Linfócitos do Interstício Tumoral/efeitos dos fármacos , Metaloproteinase 2 da Matriz/metabolismo , Camundongos , Necrose , Fenóis/química , Extratos Vegetais/química , Quercetina/química , Rutina/química , Carga Tumoral/efeitos dos fármacos
8.
Food Res Int ; 141: 110121, 2021 03.
Artigo em Inglês | MEDLINE | ID: mdl-33641988

RESUMO

While the fruits of Xylopia aethiopica (Dunal) A. Rich. are important in African countries as a local trade product, their composition remains scarcely investigated. Phenolic fingerprint is herein delivered through HPLC-DAD-ESI(Ion Trap)-MSn and UPLC-ESI-QTOF-MS2 analysis, six cinnamoylquinic acid derivatives and twenty-four flavonoid glycosides being determined, chrysoeriol-7-O-glycosides being the main constituents. A cytotoxicity screening of twenty-eight hydroethanol extracts, obtained from a collection of Guinea-Bissauan plants, against A549 and AGS carcinoma cells, revealed the selective and potent effect towards AGS cells (IC50 = 151 × 10-3 g L-1), upon exposure to the extract from X. aethiopica fruits. Additional experiments demonstrated insignificant effect on LDH release at 151 × 10-3 g L-1, morphological analysis further suggesting induction of apoptosis. Pro-apoptotic effects were confirmed, as the extract enabled the activation of the effector caspase-3, broadening the knowledge on the anticancer mechanisms elicited by the fruits of X. aethiopica. Phenolic constituents might contribute to the cytotoxic effects, particularly via caspase-3 activation. Considering that X. aethiopica fruit is very often referred as an anticancer ingredient in Africa, but mainly the potent cytotoxicity herein recorded, our results call for additional research aiming to identify non-phenolic constituents contributing to the effects and also to further detail the anticancer mechanisms.


Assuntos
Adenocarcinoma , Xylopia , África , Caspase 3 , Cromatografia Líquida de Alta Pressão , Frutas , Extratos Vegetais/farmacologia , Neoplasias Gástricas
9.
Bioorg Chem ; 108: 104646, 2021 03.
Artigo em Inglês | MEDLINE | ID: mdl-33484941

RESUMO

The transcriptional repressor Snail trriggers epithelial-mesenchymal transition (EMT), the process allowing cancer cells with invasive and metastasis properties. In this study, we screened medicinal plants for the Snail inhibitory active components by high content screen (HCS) and found that the crude extract of Xylopia vielana leaves showed potential activity. Subsequently, bioassay-guided isolation of the extract of Xylopia vielana was performed to obtain twenty-four dimeric guaianes (1-24), including 16 new analogues (1-5, 8-11, 13-15, 17, 18, 21, and 22). Their structures were elucidated by the comprehensive application of multiple spectroscopic methods. Compounds 1, 11, 12, and 16 were initially identified as the active compounds. Wound healing assay, transwell migration assay and western blot experiments verified that compounds 1 and 12 inhibited the expression of Snail in a concentration-dependent manner, and compound 12 was verified as a potent tumor migration inhibitory agent. This work showed a practical strategy for the discovery of new Snail inhibitors from natural products and provided potential insights for dimeric guaianes as anticancer lead compounds specifically targeting Snail protein.


Assuntos
Plantas Medicinais/química , Sesquiterpenos de Guaiano/farmacologia , Fatores de Transcrição da Família Snail/antagonistas & inibidores , Xylopia/química , Relação Dose-Resposta a Droga , Humanos , Estrutura Molecular , Folhas de Planta/química , Sesquiterpenos de Guaiano/química , Sesquiterpenos de Guaiano/isolamento & purificação , Relação Estrutura-Atividade , Células Tumorais Cultivadas
10.
JBRA Assist Reprod ; 25(2): 252-256, 2021 04 27.
Artigo em Inglês | MEDLINE | ID: mdl-33507724

RESUMO

OBJECTIVE: Xylopia aethiopica is a common plant in West Africa, with wide applications in trado-medical management of several diseases. Thus, our study aimed to analyze the histology and hormonal effects of ethanol extracts of Xylopia aethiopica seeds on cadmium chloride-induced reproductive dysfunction in female Wistar rats. METHODS: We used twenty-five rats weighing 120-150g for this study. The rats were divided into five groups (n=5). Group 1: received only distilled water orally; Group 2: received 2 mg/kg cadmium chloride orally; Group 3: received 2 mg/kg cadmium chloride plus 50 mg/kg Xylopia aethiopica seeds orally; Group 4: received 2 mg/kg cadmium chloride plus 100 mg/kg Xylopia aethiopica seeds orally, and Group 5: received 100 mg/kg Xylopia aethiopica seeds only, orally. We administered the extracts for 14 days, after which we slaughtered the animals following chloroform anesthesia. We took the blood samples by cardiac puncture for hormonal assay. The ovaries and uterus were harvested for histology. We analyzed the data using ANOVA, and the differences in mean values were considered significant at p<0.05. RESULTS: The body weight of the rats showed a dose-dependent reduction (p<0.05), compared with the controls. Xylopia aethiopica seeds significantly (p<0.05) reversed the detrimental effects of Cadmium on LH and FSH. The histological analysis of the ovary showed significant improvement upon treatment with Xylopia aethiopica extract in a dose-dependent manner. CONCLUSIONS: The ameliorative effects of Xylopia aethiopica against cadmium chloride-induced reproductive toxicity in female Wistar rats may be attributed to its antioxidant properties.


Assuntos
Xylopia , Animais , Cloreto de Cádmio/toxicidade , Etanol/toxicidade , Frutas , Gonadotropinas , Ovário , Extratos Vegetais , Ratos , Ratos Wistar
11.
Nat Prod Res ; 35(5): 788-791, 2021 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-30990061

RESUMO

The present study was designed to conduct the bioassay-guided isolation of possible bioactive compound(s) responsible for the antidiabetic action of Xylopia aethiopica (Dunal) A. Rich. fruit. The isolation of compound was guided by α-glycosidase and α-amylase inhibitory activities. Molecular docking with Autodock Vina was used to decipher the mode of interaction and binding affinity of the possible compound(s) with the selected enzymes. A pentacyclic triterpene, oleanolic acid (OA) was isolated from fruit and exhibited significantly (p < 0.05) lower IC50 values (α-amylase: 89.02 ± 1.12 µM, α-glucosidase: 46.05 ± 0.25 µM) than other fractions and the acarbose. Interestingly, OA was found to bind to the α-amylase and α-glucosidase with minimum binding energy values of -0.9 and -1.2 kcal/mol respectively and none of the interactions involved hydrogen bond formation. Data of this study suggest that OA is responsible for the antidiabetic action of X. aethiopica fruit through the inhibition of α-amylase and α-glucosidase enzyme activities.


Assuntos
Bioensaio , Frutas/química , Hipoglicemiantes/farmacologia , Simulação de Acoplamento Molecular , Ácido Oleanólico/isolamento & purificação , Ácido Oleanólico/farmacologia , Xylopia/química , Acarbose/farmacologia , Espectroscopia de Ressonância Magnética Nuclear de Carbono-13 , Inibidores Enzimáticos/farmacologia , Concentração Inibidora 50 , Extratos Vegetais/farmacologia , Espectroscopia de Prótons por Ressonância Magnética , alfa-Amilases/antagonistas & inibidores , alfa-Glucosidases/metabolismo
12.
Nat Prod Res ; 35(10): 1682-1685, 2021 May.
Artigo em Inglês | MEDLINE | ID: mdl-31198053

RESUMO

Hydro-distilled essential oil from leaves of Xylopia laevigata was characterized by GC-MS. Twenty-seven components were identified and the oil's major constituents comprised germacrene D, bicyclogermacrene, (E)-caryophyllene and germacrene B. The cytotoxicity of the essential oil of X. laevigata (EOXL), determined by MTT and mitotic index methods in cultured human lymphocytes was observed in all tested concentrations. Cultures treated with EOXL demonstrated significant increase in the frequencies of micronuclei in the cytokinesis-block micronucleus assay (CBMN) and reduction of the cytokinesis-block proliferation index (CBPI) rates. Results demonstrated the cytostatic and mutagenic effects of EOXL, the latter for the first time.


Assuntos
Citostáticos/farmacologia , Linfócitos/efeitos dos fármacos , Mutagênicos/farmacologia , Óleos Voláteis/farmacologia , Xylopia/química , Células Cultivadas , Citostáticos/química , Cromatografia Gasosa-Espectrometria de Massas , Humanos , Linfócitos/fisiologia , Testes para Micronúcleos , Mutagênicos/química , Óleos Voláteis/química , Óleos Voláteis/toxicidade , Folhas de Planta/química , Plantas Medicinais/química , Sesquiterpenos Policíclicos/análise , Sesquiterpenos de Germacrano/análise
13.
Z Naturforsch C J Biosci ; 75(11-12): 479-484, 2020 Nov 26.
Artigo em Inglês | MEDLINE | ID: mdl-32960782

RESUMO

The rich and diversified Malaysian flora represents an excellent resource of new chemical structures with biological activities. The genus Xylopia L. includes aromatic plants that have both nutritional and medicinal uses. This study aims to contribute with information about the volatile components of three Xylopia species essential oils: Xylopia frutescens, Xylopia ferruginea, and Xylopia magna. In this study, essential oils were extracted from the leaves by a hydrodistillation process. The identification of the essential oil components was performed by gas chromatography (GC-FID) and gas chromatography-coupled mass spectrometry (GC-MS). The major components of the essential oils from X. frutescens were bicyclogermacrene (22.8%), germacrene D (14.2%), elemol (12.8%), and guaiol (12.8%), whereas components of the essential oils from X. magna were germacrene D (35.9%), bicyclogermacrene (22.8%), and spathulenol (11.1%). The X. ferruginea oil was dominated by bicyclogermacrene (23.6%), elemol (13.7%), guaiol (13.4%), and germacrene D (12.3%).


Assuntos
Óleos Voláteis/química , Folhas de Planta/química , Xylopia/química , Cicloexanonas/química , Cicloexanonas/isolamento & purificação , Cromatografia Gasosa-Espectrometria de Massas , Plantas Medicinais/química , Sesquiterpenos/química , Sesquiterpenos/isolamento & purificação , Sesquiterpenos de Germacrano/química , Sesquiterpenos de Germacrano/isolamento & purificação , Sesquiterpenos de Guaiano/química , Sesquiterpenos de Guaiano/isolamento & purificação
14.
BMC Complement Med Ther ; 20(1): 212, 2020 Jul 07.
Artigo em Inglês | MEDLINE | ID: mdl-32635909

RESUMO

BACKGROUND: Traditional medicines are the main source of treatment of helminthiasis in endemic areas of Togo. The present study aimed to investigate the plants used by Traditional healers (THs) to treat helminth infections in endemic communities within the Central and Kara regions of Togo and to evaluate the anthelmintic activity of the three most cited plants. METHODS: An ethnobotanical survey was conducted from 19 to 24 June 2017 among traditional healers in the Central and Kara regions of Togo. The anthelmintic activity of the most cited plants namely Aframomum melegueta K. Schum, Khaya senegalensis A. Juss and Xylopia aethiopica A. Rich, was evaluated using microfilariae (Mf) of Litomosoides sigmodontis. The plants were evaluated for cytotoxicity according to the recommendation of NF EN ISO 10993-5 standard using the propidium iodide (PI) dye by flow cytometry on human peripheral blood mononuclear cells. RESULTS: A total of 197 THs were interviewed and 41 plant species were recorded. Leguminosae (14.6%) and Annonaceae (9.7%) families constitute the highest number of species cited for treatment of helminth infections. Afromomum melegueta was the most cited by the THs for the treatment of onchocerciasis (UV = 0.036) while X. aethiopica was associated with the treatment of schistosomiasis (UV = 0.061) and lymphatic filariasis (UV = 0.061). There was a great agreement among the THs regarding ethnomedicinal uses of plants to treat helminthiasis with ICF values ranging from 0.57 to 0.67. The anthelmintic assay yielded lethal doses values of 233 µg/mL, 265 µg/mL and 550 µg/mL, respectively for X. aethiopica, A. melegueta and K. senegalensis. Afromomum melegueta and X. aethiopica presented no cytotoxicity, less than 20% death, whereas K. senegalensis induced moderate toxicity, 24 ± 8% death. CONCLUSION: This study demonstrated the scientific rationale for the use of plants to treat helminthiasis in the Togolese traditional medicine. However, the use of K. senegalensis requires more caution since the plant is fairly toxic. TRIAL REGISTRATION: NA.


Assuntos
Anti-Helmínticos/farmacologia , Anti-Helmínticos/uso terapêutico , Helmintíase/tratamento farmacológico , Medicina Tradicional Africana/métodos , Adulto , Etnobotânica , Feminino , Humanos , Masculino , Meliaceae , Inquéritos e Questionários , Togo , Xylopia , Zingiberaceae
15.
Phytochem Anal ; 31(3): 349-354, 2020 May.
Artigo em Inglês | MEDLINE | ID: mdl-31875345

RESUMO

INTRODUCTION: Kaurane diterpenes, notably xylopic acid, have demonstrated important biological activities including analgesia, anti-oxidant, antimicrobial and cytotoxicity. The fruits of Xylopia aethiopica have been reported to be a rich source of kaurane diterpenes. OBJECTIVE: An analytical approach for detailed imaging and characterisation of selected kaurane diterpenes was developed using matrix-assisted laser desorption/ionisation high-resolution mass spectrometry (MALDI-HRMS) imaging techniques and high-performance liquid chromatography-high resolution electrospray ionisation-tandem mass spectrometry (HPLC-HRESI-MSn ) studies, respectively. METHODS: The images of the compounds were constructed based on selected ions from their HRESI-MS spectra. The matrix employed comprised a solution of α-cyano-4-hydroxycinnamic acid (HCCA) in acetonitrile-water with trifluoroacetic acid (TFA). HPLC-HRESI-MSn measurements were conducted on an LTQ-Orbitrap spectrometer equipped with a heated electrospray ionisation (HESI)-II source. RESULTS: The analytical strategy adopted showed the spatial distribution of the compounds in the fruits of X. aethiopica based on the dominant ions at m/z 301.2163 [M + H - HOCOCH3 ]+ and m/z 399.1932 [M + K]+ for xylopic acid, m/z 317.2111 [M + H]+ and m/z 355.1670 [M + K]+ for 15-oxo-ent-kaur-16-en-19-oic acid and m/z 303.2319 [M + H]+ for ent-kaur-16-en-19-oic acid. The fragmentation patterns of the compounds were proposed based on the HRESI-MSn measurements. CONCLUSIONS: The study revealed the spatial variability, differential behaviours and specificity of the selected kaurane diterpenes in the fruit, seed and pericarp. The compounds under study were predominantly restricted to the pericarp of the fruit with trace amounts in the seed.


Assuntos
Annonaceae , Diterpenos do Tipo Caurano , Diterpenos , Xylopia , Cromatografia Líquida de Alta Pressão , Frutas , Espectrometria de Massas por Ionização e Dessorção a Laser Assistida por Matriz
16.
J Ethnopharmacol ; 248: 112312, 2020 Feb 10.
Artigo em Inglês | MEDLINE | ID: mdl-31629028

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Ethnopharmacological surveys on Guinea-Bissauan flora reveal that several species are used to treat or ameliorate the symptomatology of conditions with an inflammatory background. As such, extracts obtained from a series of plants recorded in those surveys were screened for their anti-inflammatory properties, a hydroethanolic extract obtained from the leaves of Xylopia aethiopica (Dunal) A. Rich, (Annonaceae), used on the treatment of headache, muscular pain and rheumatic pain, scoring positively and being further investigated. AIM OF THE STUDY: In order to identify species with anti-inflammatory properties, extracts were screened for their ability to interfere with LPS-induced TNF-α levels. Since significant effects were recorded upon treatment with the extract of the leaves obtained from X. aethiopica, further assays were conducted to elucidate additional mechanisms underlying its anti-inflammatory potential. Since little is known on the chemical composition of the plant, we also aimed to characterise its phenolic profile. MATERIALS AND METHODS: Interference with cytokines was evaluated by ELISA assay, through the quantification of TNF-α and IL-6 levels in the culture medium collected from LPS-activated THP-1-derived-macrophages. Inhibition of 5-lipoxygenase was assessed based on the oxidation of linoleic acid to 13-hydroperoxylinoleic acid. Characterization of the phenolic profile was attained by HPLC-DAD. RESULTS: Evaluation of TNF-α levels in LPS-challenged THP-1 macrophages evidenced a significant inhibition (>90%) upon treatment with the hydroethanolic extract obtained from X. aethiopica leaves at a concentration of 500 µg/mL. Additional anti-inflammatory effects were recorded, including a significant decrease on IL-6 levels at 250 and 500 µg/mL. The extract proved to be active towards 5-LOX, leading to significant inhibition at concentrations ranging from 16 to 250 µg/mL (IC50 = 85 µg/mL). Phenolic profiling allowed the identification and quantitation of eight constituents, including caffeoylquinic acids (1-3), mono-O-glycosylated flavonols (5-8), and the mono-O-glycosyl flavone luteolin-7-O-glucoside (4). The main phenolic constituent, kaempferol-3-O-rutinoside (8), was found to significantly contribute to the anti-inflammatory effects, namely through the inhibition of 5-LOX. However, no effects on the decrease of TNF-α and IL-6 levels caused by this phenolic compound were found. CONCLUSION: The anti-inflammatory effects of X. aethiopica leaves are demonstrated experimentally, thus substantiating its use in folk Medicine. Relevantly, the observed anti-inflammatory properties can stimulate further studies in order to fully unveil the therapeutic potential of the plant, namely as a source of phenolic compounds with a significant ability to interfere with conventional inflammatory targets.


Assuntos
Anti-Inflamatórios/farmacologia , Flavonoides/farmacologia , Mediadores da Inflamação/metabolismo , Interleucina-6/metabolismo , Macrófagos/efeitos dos fármacos , Extratos Vegetais/farmacologia , Folhas de Planta , Fator de Necrose Tumoral alfa/metabolismo , Xylopia , Anti-Inflamatórios/isolamento & purificação , Araquidonato 5-Lipoxigenase/metabolismo , Flavonoides/isolamento & purificação , Humanos , Lipopolissacarídeos/toxicidade , Macrófagos/metabolismo , Extratos Vegetais/isolamento & purificação , Folhas de Planta/química , Células THP-1 , Xylopia/química
17.
Nat Prod Res ; 34(24): 3526-3530, 2020 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-30810362

RESUMO

Aiming to investigate the antiplasmodial activity and the phytochemical composition of Xylopia sericea leaves, the essential oil and dichloromethane extract were analyzed by gas and liquid chromatography, respectively, both of them coupled to mass spectrometry, and were evaluated against the chloroquine-resistant Plasmodium falciparum strain (W2) and for cytotoxicity to HepG2 cells. Low growth inhibition of P. falciparum as well as low cytotoxicity to HepG2 cells were observed for the essential oil. The leaves dichloromethane extract showed moderate growth inhibition of P. falciparum and low cytotoxicity to HepG2 cells. Bioguided chromatographic fractionation of this extract led to fractions with increased antiplasmodial activity from which liriodenine (IC50 6.1 ± 0.1 µg/mL, CC50 > 1000.0 µg/mL, SI > 164), an aporphine alkaloid, and an acetogenin-rich fraction containing mainly isomers of annomontacin and 4-deoxy-annomontacin (IC50 22.7 ± 1.9 µg/mL, CC50 336.1 ± 15.5 µg/mL, SI = 15) might be highlighted for their antiplasmodial activity.


Assuntos
Antimaláricos/farmacologia , Plasmodium falciparum/efeitos dos fármacos , Xylopia/química , Animais , Antimaláricos/química , Antimaláricos/toxicidade , Aporfinas/química , Aporfinas/farmacologia , Cloroquina/farmacologia , Cromatografia Gasosa , Cromatografia Líquida , Avaliação Pré-Clínica de Medicamentos , Resistência Microbiana a Medicamentos , Furanos/farmacologia , Células Hep G2 , Humanos , Lactonas/farmacologia , Óleos Voláteis/química , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Folhas de Planta/química
18.
J Pharm Pharmacol ; 71(10): 1544-1552, 2019 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-31380566

RESUMO

OBJECTIVES: This study sought to determine the quality of essential oil from Xylopia aethiopica fruits of different geographical origins using GC-MS-based metabolomics, bacterial quorum sensing and anti-inflammation assessment. METHODS: Essential oil was obtained from eight batches of X. aethiopica fruits from Ghana and Nigeria by hydrodistillation, characterized using gas chromatography-mass spectrometry and differences therein found using metabolomics. The respective antibacterial activity of the oils was tested against four bacterial strains: two Gram-positive strains, Staphylococcus aureus (ATCC 25923) and Bacillus licheniformis (ATCC12759), and two Gram-negative strains, Escherichia coli (ATCC25922) and Klebsiella pneumoniae (ATCC 13883). Anti-inflammation was tested using RAW 264.7 macrophage cells. KEY FINDINGS: The outcome of the study revealed that the oil of the Ghana-sourced samples exhibited superior antibacterial, cytotoxic and anti-inflammatory effects than those from Nigeria. This could be attributed to the higher levels of the bioactive compounds present in those samples. This distinction between the samples from the two countries was clearly established using the metabolomics approach, and 14 differential metabolites were found to be potential chemical markers. CONCLUSIONS: The study lends credence to the traditional uses of the essential oil of X. aethiopica as an antimicrobial and anti-inflammatory agent.


Assuntos
Antibacterianos/química , Antibacterianos/farmacologia , Anti-Inflamatórios/química , Anti-Inflamatórios/farmacologia , Óleos Voláteis/química , Óleos Voláteis/farmacologia , Xylopia/química , Antioxidantes/química , Antioxidantes/farmacologia , Frutas/química , Cromatografia Gasosa-Espectrometria de Massas/métodos , Gana , Metabolômica/métodos , Testes de Sensibilidade Microbiana/métodos , Nigéria , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Óleos Vegetais/química , Óleos Vegetais/farmacologia
19.
Chem Biodivers ; 16(7): e1900141, 2019 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-31087758

RESUMO

Bioguided fractionation of Xylopia sericea antiplasmodial dichloromethane leaves extract led to the isolation of (-)-7-oxo-ent-kaur-16-en-19-oic acid (C20 H28 O3 ) that was identified by a combination of 1D and 2D NMR experiments (COSY, HMBC, HSQC, HSQC-TOCSY, HSQC-NOESY and NOESY) and by X-ray crystallography. A feature to be pointed out is its (4R) configuration that was inferred from the NOE experiments (HSQC-NOESY and NOESY) and X-ray crystallography. In vitro evaluation of this rare diterpene acid against the chloroquine-resistant strain Plasmodium falciparum W2 by the PfLDH method showed it disclosed a low antiplasmodial activity and was not cytotoxic to HepG2 cells (CC50 862.6±6.7 µm) by the MTT assay. The unequivocal NMR signals assignments, the X-ray crystallographic structure, the assessment to the bioactivities and the occurrence this diterpene in X. sericea are reported here for the first time.


Assuntos
Antimaláricos/farmacologia , Antineoplásicos Fitogênicos/farmacologia , Diterpenos do Tipo Caurano/farmacologia , Diterpenos/farmacologia , Extratos Vegetais/farmacologia , Folhas de Planta/química , Plasmodium falciparum/efeitos dos fármacos , Xylopia/química , Antimaláricos/química , Antimaláricos/isolamento & purificação , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/isolamento & purificação , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Cristalografia por Raios X , Diterpenos/química , Diterpenos/isolamento & purificação , Diterpenos do Tipo Caurano/química , Diterpenos do Tipo Caurano/isolamento & purificação , Relação Dose-Resposta a Droga , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Espectroscopia de Ressonância Magnética , Modelos Moleculares , Conformação Molecular , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Relação Estrutura-Atividade
20.
Molecules ; 24(10)2019 May 23.
Artigo em Inglês | MEDLINE | ID: mdl-31126018

RESUMO

Aside from its multiple medicinal uses, the fruit of Xylopia aethiopica is widely used in Africa as food. Herein, we characterize the protein profiles, mineral content and bioactive phytochemical composition of the seeds of this plant sourced in Ghana and Nigeria. Using label-free proteomics, a total of 677 proteins were identified, with 260 found in the Ghana-sourced samples while 608 proteins were detected in the samples from Nigeria. However, 114 proteins were common between the samples from the two countries, among which 48 were significantly changed. Bioinformatics and functional analyses revealed that the differential levels of the proteins were mainly linked to pathways involved amino acids metabolism and biosynthesis. The significantly changed proteins related mainly to catalytic activity and carbon metabolism. The samples from Nigeria also exhibited superior qualities in terms of their antioxidant effects, and total phenolic and flavonoid content. Finally, only the content of Na varied to a statistically significant level. This study lends support to its culinary use and hints towards the impact of location of cultivation on the quality of the seeds. There is however need for further mechanistic investigations to unravel the underlying reasons for the observed differences.


Assuntos
Minerais/análise , Compostos Fitoquímicos/análise , Proteínas de Plantas/metabolismo , Proteômica/métodos , Xylopia/classificação , Antioxidantes/análise , Flavonoides/análise , Regulação da Expressão Gênica de Plantas , Gana , Nigéria , Fenóis/análise , Extratos Vegetais/análise , Sementes/química , Sementes/metabolismo , Especificidade da Espécie , Xylopia/química , Xylopia/metabolismo
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