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1.
Molecules ; 29(9)2024 Apr 26.
Artigo em Inglês | MEDLINE | ID: mdl-38731493

RESUMO

The aim of this study was to investigate the potential of Amaranthus cruentus flavonoids (quercetin, kaempferol, catechin, hesperetin, naringenin, hesperidin, and naringin), cinnamic acid derivatives (p-coumaric acid, ferulic acid, and caffeic acid), and benzoic acids (vanillic acid and 4-hydroxybenzoic acid) as antioxidants, antidiabetic, and antihypertensive agents. An analytical method for simultaneous quantification of flavonoids, cinnamic acid derivatives, and benzoic acids for metabolomic analysis of leaves and inflorescences from A. cruentus was developed with HPLC-UV-DAD. Evaluation of linearity, limit of detection, limit of quantitation, precision, and recovery was used to validate the analytical method developed. Maximum total flavonoids contents (5.2 mg/g of lyophilized material) and cinnamic acid derivatives contents (0.6 mg/g of lyophilized material) were found in leaves. Using UV-Vis spectrophotometry, the maximum total betacyanin contents (74.4 mg/g of lyophilized material) and betaxanthin contents (31 mg/g of lyophilized material) were found in inflorescences. The leaf extract showed the highest activity in removing DPPH radicals. In vitro antidiabetic activity of extracts was performed with pancreatic α-glucosidase and intestinal α-amylase, and compared to acarbose. Both extracts exhibited a reduction in enzyme activity from 57 to 74%. Furthermore, the in vivo tests on normoglycemic murine models showed improved glucose homeostasis after sucrose load, which was significantly different from the control. In vitro antihypertensive activity of extracts was performed with angiotensin-converting enzyme and contrasted to captopril; both extracts exhibited a reduction of enzyme activity from 53 to 58%. The leaf extract induced a 45% relaxation in an ex vivo aorta model. In the molecular docking analysis, isoamaranthin and isogomphrenin-I showed predictive binding affinity for α-glucosidases (human maltase-glucoamylase and human sucrase-isomaltase), while catechin displayed binding affinity for human angiotensin-converting enzyme. The data from this study highlights the potential of A. cruentus as a functional food.


Assuntos
Amaranthus , Anti-Hipertensivos , Hipoglicemiantes , Metabolômica , Extratos Vegetais , Folhas de Planta , Amaranthus/química , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Folhas de Planta/química , Cromatografia Líquida de Alta Pressão , Hipoglicemiantes/farmacologia , Hipoglicemiantes/química , Anti-Hipertensivos/farmacologia , Anti-Hipertensivos/química , Metabolômica/métodos , Animais , Antioxidantes/farmacologia , Antioxidantes/química , Masculino , Ratos , Flavonoides/química , Flavonoides/farmacologia , Flavonoides/análise
2.
J Ethnopharmacol ; 301: 115840, 2023 Jan 30.
Artigo em Inglês | MEDLINE | ID: mdl-36257342

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Approximately 80% of people in developing countries depend on medicinal plants for their health care. Tridax procumbens (T. procumbens) and Allium sativum (A. sativum) have beneficial effects against parasitic and bacterial diseases. On the other side, the biological activity of the oxylipin (3S)-16,17-didehydrofalcarinol isolated from T. procumbens against the parasite Leishmania mexicana has been verified. AIM OF THE STUDY: To evaluate the acute oral toxicity of the methanolic extract of T. procumbens, the aqueous extract of A. sativum, their mixture, and pure oxylipin (3S)-16,17-didehydrofalcarinol in BALB/c mice. MATERIALS AND METHODS: Doses of 2000 and 5000 mg/kg of the methanolic extract of T. procumbens, the aqueous extract of A. sativum, and their mixture (1:1), and doses of 300 and 500 mg/kg of pure oxylipin were administered orally to female mice of the strain BALB/c, which were observed for 72 h in search of signs of toxicity. After 14 days, the animals were euthanized, blood was extracted for the measurement of transaminases, and the livers were recovered and stained with hematoxylin/eosin for histopathological analysis. RESULTS: No clinical signs of toxicity were observed in any of the animals dosed with T. procumbens and A. sativum extracts, while the majority of the animals dosed with pure oxylipin showed signs of toxicity and died. There was no difference in the weight index in most of the animals, except for the animals treated with T. procumbens at doses of 2000 mg/kg who presented an increase in the weight index, nor was there a correlation between the dose of A. sativum and the mixture and food consumption; however, a direct proportional correlation was observed between T. procumbens dose and food consumption. In none of the animals dosed with T. procumbens, A. sativum, and the mixture there was a difference in the levels of transaminases. In the histopathology study, slight lesions were observed in the hepatocytes of the mice treated with T. procumbens, A. sativum, and their mixture at doses of 2000 and 5000 mg/kg. On the other side, moderate injuries were observed in animals treated with pure oxylipin and it was considered as toxic due to almost all the animals died. CONCLUSION: The extracts of T. procumbens and A. sativum evaluated and applied orally did not cause signs of acute toxicity or severe liver damage, suggesting to evaluate their chronic toxicity including other biochemical parameters in the future. However, pure oxylipin caused signs of acute toxicity and death so it is recommended to work with lower doses.


Assuntos
Asteraceae , Alho , Camundongos , Animais , Camundongos Endogâmicos BALB C , Oxilipinas , Extratos Vegetais/toxicidade , Antioxidantes , Transaminases
3.
Molecules ; 27(23)2022 Nov 26.
Artigo em Inglês | MEDLINE | ID: mdl-36500355

RESUMO

Leukemia is one of the most frequent types of cancer. No effective treatment currently exists, driving a search for new compounds. Simple structural modifications were made to novel triterpenes isolated from Phoradendron wattii. Of the three resulting derivatives, 3α-methoxy-24-hydroxylup-20(29)-en-28-oic acid (T1m) caused a decrease in the median inhibitory concentration (IC50) on the K562 cell line. Its mode of action was apparently apoptosis, ROS generation, and loss of mitochondrial membrane potential (MMP). Molecular docking analysis showed T1m to produce lower binding energies than its precursor for the Bcl-2 and EGFR proteins. Small, simple, and viable modifications to triterpenes can improve their activity against leukemia cell lines. T1m is a potentially promising element for future research. Clarifying the targets in its mode of action will improve its applicability.


Assuntos
Leucemia , Triterpenos , Humanos , Triterpenos/química , Lupanos , Simulação de Acoplamento Molecular , Apoptose , Leucemia/tratamento farmacológico , Linhagem Celular Tumoral
4.
Molecules ; 27(17)2022 Aug 31.
Artigo em Inglês | MEDLINE | ID: mdl-36080390

RESUMO

Current antineoplastic agents present multiple disadvantages, driving an ongoing search for new and better compounds. Four lupane-type triterpenes, 3α,24-dihydroxylup-20(29)-en-28-oic acid (1), 3α,23-dihydroxy-30-oxo-lup-20(29)-en-28-oic acid (2), 3α,23-O-isopropylidenyl-3α,23-dihydroxylup-20(29)-en-28-oic acid (3), and 3α,23-dihydroxylup-20(29)-en-28-oic acid (4), previously isolated from Phoradendron wattii, were evaluated on two cell lines of chronic (K562) and acute (HL60) myeloid leukemia. Compounds 1, 2, and 4 decreased cell viability and inhibit proliferation, mainly in K562, and exhibited an apoptotic effect from 24 h of treatment. Of particular interest is compound 2, which caused arrest in active phases (G2/M) of the cell cycle, as shown by in silico study of the CDK1/Cyclin B/Csk2 complex by molecular docking. This compound [3α,23-dihydroxy-30-oxo-lup-20(29)-en-28-oic acid] s a promising candidate for incorporation into cancer treatments and deserves further study.


Assuntos
Leucemia , Phoradendron , Triterpenos , Ciclo Celular , Linhagem Celular , Humanos , Leucemia/tratamento farmacológico , Simulação de Acoplamento Molecular , Estrutura Molecular , Phoradendron/metabolismo , Folhas de Planta/metabolismo
5.
Nat Prod Res ; 36(17): 4466-4469, 2022 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-34613838

RESUMO

Plant-derived secondary metabolites are a source of promising bioactive molecules in the search for safer more selective cancer drugs. Mexico's flora is extremely diverse and many species, such as Phoradendron wattii, form part of traditional medicine. Compounds with notable cytotoxic activity have been isolated from P. wattii, but their concentrations may vary seasonally. The aim was to identify any variation in active metabolite concentrations in Phoradendron wattii methanol extracts in response to season. Betulin exhibited the most evident seasonal variations, being most abundant during the midsummer drought. Cytotoxic activity was highest (29 ± 1 µg/mL) in the rainy season methanol extract. Though not the most abundant metabolite in the extracts, 3α,24-dihydroxylup-20(29)-en-28-oic acid is apparently one of the most active among them and is a promising chemotaxonomic biomarker for this species. In summary, secondary metabolite concentrations in P. wattii methanol extracts varied in response to season, and these variations influenced cytotoxic activity.


Assuntos
Antineoplásicos , Phoradendron , Antineoplásicos/farmacologia , Metanol , Extratos Vegetais/farmacologia , Estações do Ano
6.
Nat Prod Res ; 35(5): 826-828, 2021 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-30990072

RESUMO

Secundiflorol G (SG) is an isoflavan isolated from the root bark of Aeschynomene fascicularis, a Mayan medicinal plant used to treat cancer-like symptoms. SG has been shown to have cytotoxic effects on cervical cancer cells (HeLa). Assays were done to identify the mechanisms of SG's cytotoxic effect.HeLa cells treated with SG exhibited early and late apoptosis, and caspase-9, -8 and -3 activities. It also induces generation of reactive oxygen species and disrupted mitochondrial membrane potential.SG isolated from A. fascicularis induces apoptosis through extrinsic and intrinsic pathways on HeLa cells. SG could be a candidate for in vivo studies and a promising natural compound in cervical cancer treatment.


Assuntos
Apoptose/efeitos dos fármacos , Benzopiranos/isolamento & purificação , Benzopiranos/farmacologia , Fabaceae/química , Isoflavonas/isolamento & purificação , Isoflavonas/farmacologia , Plantas Medicinais/química , Neoplasias do Colo do Útero/patologia , Antineoplásicos/farmacologia , Benzopiranos/química , Caspases/metabolismo , Inibidor de Quinase Dependente de Ciclina p21/metabolismo , Ativação Enzimática/efeitos dos fármacos , Feminino , Células HeLa , Humanos , Isoflavonas/química , Potencial da Membrana Mitocondrial/efeitos dos fármacos , Extratos Vegetais/farmacologia , Espécies Reativas de Oxigênio/metabolismo , Neoplasias do Colo do Útero/tratamento farmacológico , Neoplasias do Colo do Útero/enzimologia , Proteína X Associada a bcl-2/metabolismo
7.
Phytochem Anal ; 31(2): 183-190, 2020 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-31343078

RESUMO

INTRODUCTION: (3S)-16,17-Didehydrofalcarinol (1) has been isolated from Tridax procumbens and has proved to have notorious bioactivity against Leishmania mexicana. In this study, hexane fractions obtained from the methanol extract of each plant part (roots, stems, leaves, flowers, and fruits) of T. procumbens collected monthly during a year were analysed in order to determine the quantity of 1 associated with biotic variables. OBJECTIVE: The aim of this study was to find the season of the year in which the bioactive metabolite 1 is at the highest concentration and to correlate it with temperature, length of day light, and rainfall. METHODS: Hexane fractions were obtained by liquid-liquid extraction and an accurate quantitation of 1 was performed using gas chromatography with a flame ionisation detector (GC-FID) employing pelargonic acid vanillyl amide (2) as internal standard. Partial validation was based on linearity and precision. RESULTS: Our results indicated that the total content of 1 has significant variation (P ≤ 0.05) during the different collecting months. The total content of the metabolite reached its highest level in the roots of the plant during June in the rainfall season (0.0358 ± 0.001 mg/g), and its lowest values in February and March during the drought season (0.0015 ± 0.000 and 0.0008 ± 0.000 mg/g, respectively). CONCLUSION: Our study provided evidence that the content of 1 in roots is strongly influenced by the variables of the harvesting season, also indicating that the biosynthesis of the active metabolite is enhanced during the warm and rainy months.


Assuntos
Extratos Vegetais , Polímero Poliacetilênico , Di-Inos , Álcoois Graxos , Estações do Ano , Distribuição Tecidual
8.
J Nat Med ; 73(3): 672-678, 2019 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-30778894

RESUMO

Neurological disorders are a public health problem worldwide for which there is currently no direct treatment of the cause of the disorder. The goal of this study was to investigate the potential in vitro neuroprotective property of plants used in Mayan traditional medicine. Plant ethanolic extracts were prepared and tested on models in which neuronal damage was induced by glutamate, i.e., a human neuroblastoma cell line (SH-SY5Y) and rat cortical neurons. HPLC profiles from active extracts were also obtained. A total of 51 plant species were identified in the literature as plant species used in Mayan traditional medicine for the treatment of symptoms suggestive of neurological disorders, and we studied 34 of these in our analysis. Six extracts had a neuroprotective effect on SH-SY5Y cells, with the most active extract being that from Schwenckia americana roots (half maximal effective concentration [EC50] 11.3 ± 2.9 µg/mL), and three extracts exhibited a neuroprotective effect in the rat neuron cortical model, with the most active extract being that from Elytraria imbricata aerial parts (EC50 6.8 ± 3.1 µg/mL). These results suggest that the active extracts from such plants have the potential to be a great resource. Future studies should be performed that are more extensive and which isolate the active constituents.


Assuntos
Ácido Glutâmico/toxicidade , Fármacos Neuroprotetores/uso terapêutico , Extratos Vegetais/química , Plantas Medicinais/química , Animais , Humanos , Fármacos Neuroprotetores/farmacologia , Ratos , Ratos Wistar
9.
J Nat Prod ; 80(11): 3038-3042, 2017 11 22.
Artigo em Inglês | MEDLINE | ID: mdl-29120172

RESUMO

Three new lupane-type triterpenes, 3α,24-dihydroxylup-20(29)-en-28-oic acid (1), 3α,23-dihydroxy-30-oxolup-20(29)-en-28-oic acid (2), and 3α,23-O-isopropylidenyl-3α,23-dihydroxylup-20(29)-en-28-oic acid (3), together with eight known compounds (4-11) were isolated from a methanol extract of Phoradendron vernicosum aerial parts. The chemical structures of 1-3 were determined on the basis of spectroscopic data interpretation. The isolated compounds were tested against seven human cancer cell lines and two normal cell lines.


Assuntos
Antineoplásicos Fitogênicos/isolamento & purificação , Phoradendron/química , Componentes Aéreos da Planta/química , Triterpenos/isolamento & purificação , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/farmacologia , Ensaios de Seleção de Medicamentos Antitumorais , Células HeLa , Humanos , Células KB , Células MCF-7 , México , Estrutura Molecular , Ressonância Magnética Nuclear Biomolecular , Extratos Vegetais/química , Folhas de Planta/química , Triterpenos/química , Triterpenos/farmacologia
10.
Rev Argent Microbiol ; 49(1): 83-92, 2017.
Artigo em Inglês | MEDLINE | ID: mdl-28258772

RESUMO

Fungal metabolites are promising alternatives for the development of biorational pesticides. In this sense, microfungi from tropical regions are valuable sources of natural compounds for pest management. With the aim of broadening the search for new eco-friendly products to manage plant pests, this study was carried out to evaluate the biological activity of 23 tropical fungal extracts on three species of phytophagous insects and a plant parasitic nematode. In addition, the active principles of the most effective extract were identified. The insect deterrent activity of fungal extracts was evaluated on the settling of aphids Myzus persicae and Rhopalosiphum padi, and on the feeding of lepidoptera larva Spodoptera littoralis; the nematostatic activity was evaluated on the mobility of Meloidogyne javanica. Active metabolites from Gliomastix masseei were identified by GC-MS techniques and by comparison with commercial standards. Results showed seven extracts with strong effect on the settling of M. persicae and R. padi (settling inhibition >80%). The calculated median of effective concentration (EC50) values ranged from 8 to 38µg/cm2 for the extracts of Clonostachys rosea and G. masseei, respectively. Bioassay-guided separation of the ethyl acetate extract of G. masseei revealed the presence of fatty acids and their derivatives, where methyl 9-octadecenoate was the most active compound with EC50 values of 16µg and 35µg/cm2 for M. persicae and R. padi, respectively. Extracts of C. rosea and G. masseei could be a promising option in the control of pest aphids in agriculture.


Assuntos
Agentes de Controle Biológico , Fungos , Insetos , Animais , Afídeos , Fungos/química , Larva , México , Plantas
11.
Rev. argent. microbiol ; 49(1): 83-92, mar. 2017. tab
Artigo em Inglês | LILACS | ID: biblio-843187

RESUMO

Fungal metabolites are promising alternatives for the development of biorational pesticides. In this sense, microfungi from tropical regions are valuable sources of natural compounds for pest management. With the aim of broadening the search for new eco-friendly products to manage plant pests, this study was carried out to evaluate the biological activity of 23 tropical fungal extracts on three species of phytophagous insects and a plant parasitic nematode. In addition, the active principles of the most effective extract were identified. The insect deterrent activity of fungal extracts was evaluated on the settling of aphids Myzus persicae and Rhopalosiphum padi, and on the feeding of lepidoptera larva Spodoptera littoralis; the nematostatic activity was evaluated on the mobility of Meloidogyne javanica. Active metabolites from Gliomastix masseei were identified by GC-MS techniques and by comparison with commercial standards. Results showed seven extracts with strong effect on the settling of M. persicae and R. padi (settling inhibition >80%). The calculated median of effective concentration (EC50) values ranged from 8 to 38 µg/cm² for the extracts of Clonostachys rosea and G. masseei, respectively. Bioassay-guided separation of the ethyl acetate extract of G. masseei revealed the presence of fatty acids and their derivatives, where methyl 9-octadecenoate was the most active compound with EC50 values of 16 µg and 35 µg/cm² for M. persicae and R. padi, respectively. Extracts of C. rosea and G. masseei could be a promising option in the control of pest aphids in agriculture.


Los metabolitos fúngicos son agentes prometedores para el desarrollo de plaguicidas biorracionales. En este sentido, los hongos microscópicos de zonas tropicales representan una valiosa fuente de compuestos naturales para el manejo de plagas. Con la finalidad de ampliar la investigación en productos amigables con el medio ambiente, en este estudio se evaluó la actividad biológica de 23 extractos de hongos sobre 3 especies de insectos fitófagos y un nematodo fitoparásito; además se identificaron los componentes del extracto más activo. El efecto disuasivo de los extractos fúngicos se evaluó en el asentamiento de Myzus persicae y Rhopalosiphum padi, así como en la alimentación de Spodoptera littoralis; la actividad nematostática se evaluó sobre la movilidad de Meloidogyne javanica. Los metabolitos activos de Gliomastix masseei se identificaron por cromatografía de gases-espectrometría de masas y por comparación con muestras comerciales. Los resultados mostraron 7 extractos con fuerte efecto en la inhibición del asentamiento (> 80%) de M. persicae y R. padi. Los valores de la concentración efectiva media (CE50) estuvieron en el rango de 8 a 38 µg/cm² para los extractos de Clonostachys rosea y G. masseei, respectivamente. El extracto de acetato de etilo de G. masseei se fraccionó por un proceso biodirigido y reveló la presencia de ácidos grasos y sus derivados, donde el 9-octadecenoato de metilo fue el más activo, con una CE50 de 16 µg/cm² para M. persicae y 35 µg/cm² para R. padi. Los extractos fúngicos de C. rosea y G. masseei pueden ser una alternativa promisoria en el control de áfidos que son plaga en la agricultura.


Assuntos
Animais , Agentes de Controle Biológico , Fungos , Insetos , Afídeos , Plantas , Fungos/química , Larva , México
12.
Biomed Res Int ; 2015: 847457, 2015.
Artigo em Inglês | MEDLINE | ID: mdl-26557704

RESUMO

The purpose of this study was to investigate antiproliferative activity of bonediol, an alkyl catechol isolated from the Mayan medicinal plant Bonellia macrocarpa. Bonediol was assessed for growth inhibition of androgen-sensitive (LNCaP), androgen-insensitive (PC-3), and metastatic androgen-insensitive (PC-3M) human prostate tumor cells; toxicity on normal cell line (HEK 293) was also evaluated. Hedgehog pathway was evaluated and competitive 3H-estradiol ligand binding assay was performed. Additionally, antioxidant activity on Nrf2-ARE pathway was evaluated. Bonediol induced a growth inhibition on prostate cancer cell lines (IC50 from 8.5 to 20.6 µM). Interestingly, bonediol binds to both estrogen receptors (ERα (2.5 µM) and ERß (2.1 µM)) and displaces the native ligand E2 (17ß-estradiol). No significant activity was found in the Hedgehog pathway. Additionally, activity of bonediol on Nrf2-ARE pathway suggested that bonediol could induce oxidative stress and activation of detoxification enzymes at 1 µM (3.8-fold). We propose that the compound bonediol may serve as a potential chemopreventive treatment with therapeutic potential against prostate cancer.


Assuntos
Antineoplásicos/farmacologia , Catecóis/farmacologia , Moduladores de Receptor Estrogênico/farmacologia , Extratos Vegetais/farmacologia , Primulaceae/química , Animais , Antineoplásicos/química , Catecóis/química , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Moduladores de Receptor Estrogênico/química , Células HEK293 , Humanos , Camundongos , Células NIH 3T3 , Extratos Vegetais/química , Ensaio Radioligante , Receptores de Estrogênio/efeitos dos fármacos , Receptores de Estrogênio/metabolismo
13.
Nat Prod Commun ; 10(9): 1513-6, 2015 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-26594746

RESUMO

Serjania goniocarpa is a plant used in Mayan traditional medicine as a remedy for the treatment of cancer-like symptoms. Bio-guided fractionation of the methanol extract of the leaves led to the isolation of an α- and ß-amyrin mixture, palmitic acid, phytol and the new sesterterpene goniocarpic acid whose structure was elucidated by IR, GC-MS, and NMR spectroscopic analyses. Goniocarpic acid exhibited cytotoxic and antiproliferative activity against several cancer cell lines.


Assuntos
Ácido Oleanólico/análogos & derivados , Sapindaceae/química , Sesquiterpenos/química , Sesquiterpenos/isolamento & purificação , Sesterterpenos/química , Sesterterpenos/isolamento & purificação , Linhagem Celular Tumoral , Humanos , Medicina Tradicional , Estrutura Molecular , Ácido Oleanólico/química , Ácido Oleanólico/isolamento & purificação , Extratos Vegetais/química , Folhas de Planta/química
14.
Molecules ; 20(8): 13563-74, 2015 Jul 24.
Artigo em Inglês | MEDLINE | ID: mdl-26213910

RESUMO

The plant Aeschynomene fascicularis (Fabaceae) has been used in Mayan traditional medicine in the Yucatan peninsula. However, the compounds present in the plant responsible for its curative properties have not yet been investigated. Aeschynomene fascicularis root bark was extracted with 100% methanol to obtain a crude extract. The methanol extract was partitioned successively with solvents with increasing polarity to obtain the corresponding hexane (Hx), dichloromethane (DCM) and ethyl acetate fractions (EtOAc), as well as a residual water-alcoholic fraction. These fractions were tested for their cytotoxic activities using an MTT assay against Hep-2 cancer cell lines. The Hx fraction led to the isolation of spinochalcone C (1), spinochalcone A (2), isocordoin (3) and secundiflorol G (4). Their structures were identified based on spectroscopic evidence and chemical properties. All compounds were subjected to cytotoxicity and antiproliferative assays against a panel of seven cell lines, including one normal-type cell line. Spinochalcone A (2) exhibited cytotoxic activity against DU-145 cell line and antiproliferative activity against the KB cell line. Secundiflorol G (4) showed strong cytotoxic activity towards KB and Hep-2 cell lines. In addition, isocordoin (3) showed moderate activity on KB, Hep-2 and DU-145 cell lines. The active Compounds 2, 3 and 4 are potential therapeutic entities against cancer.


Assuntos
Antineoplásicos , Citotoxinas , Fabaceae/química , Casca de Planta/química , Raízes de Plantas/química , Plantas Medicinais/química , Antineoplásicos/química , Antineoplásicos/isolamento & purificação , Antineoplásicos/farmacologia , Proliferação de Células/efeitos dos fármacos , Citotoxinas/química , Citotoxinas/isolamento & purificação , Citotoxinas/farmacologia , Ensaios de Seleção de Medicamentos Antitumorais , Células HeLa , Células Hep G2 , Humanos
15.
Parasite ; 21: 15, 2014.
Artigo em Inglês | MEDLINE | ID: mdl-24717526

RESUMO

We tested a mixture of Tridax procumbens, known for its direct action against Leishmania mexicana, and Allium sativum, known for its immunomodulatory effect, as an alternative to treat cutaneous leishmaniasis. Acute oral toxicity was tested with the Up-and-Down Procedure (UDP) using a group of healthy mice administered with either T. procumbens or A. sativum extracts and compared with a control group. Liver injury and other parameters of toxicity were determined in mice at day 14. The in vivo assay was performed with mice infected with L. mexicana promastigotes and treated with either a mixture of T. procumbens and A. sativum or each extract separately. The thickness of the mice's footpads was measured weekly. After the 12-week period of infection, blood samples were obtained by cardiac puncture to determine the total IgG, IgG1 and IgG2a immunoglobulins by a noncommercial indirect ELISA. We showed that the mixture of T. procumbens and A. sativum extracts was better at controlling L. mexicana infection while not being toxic when tested in the acute oral toxicity assay in mice. An increase in the ratio of IgG2a/IgG1 indicated a tendency to raise a Th1-type immune response in mice treated with the mixture. The mixture of T. procumbens and A. sativum extracts is a promising natural treatment for cutaneous leishmaniasis and its healing effects make it a good candidate for a possible new phytomedicine.


Assuntos
Antiprotozoários/uso terapêutico , Asteraceae , Alho , Fatores Imunológicos/uso terapêutico , Leishmania mexicana/efeitos dos fármacos , Leishmaniose Cutânea/tratamento farmacológico , Fitoterapia , Extratos Vegetais/uso terapêutico , Administração Oral , Animais , Anticorpos Antiprotozoários/sangue , Anticorpos Antiprotozoários/imunologia , Antiprotozoários/administração & dosagem , Antiprotozoários/isolamento & purificação , Antiprotozoários/toxicidade , Peso Corporal/efeitos dos fármacos , Doença Hepática Induzida por Substâncias e Drogas/etiologia , Avaliação Pré-Clínica de Medicamentos , Feminino , Imunoglobulina G/sangue , Imunoglobulina G/imunologia , Fatores Imunológicos/administração & dosagem , Fatores Imunológicos/isolamento & purificação , Fatores Imunológicos/toxicidade , Leishmania mexicana/imunologia , Leishmaniose Cutânea/parasitologia , Fígado/efeitos dos fármacos , Fígado/patologia , Camundongos , Camundongos Endogâmicos BALB C , Tamanho do Órgão/efeitos dos fármacos , Fitoterapia/efeitos adversos , Extratos Vegetais/administração & dosagem , Extratos Vegetais/toxicidade , Baço/efeitos dos fármacos , Baço/patologia
16.
Nat Prod Commun ; 8(10): 1421-2, 2013 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-24354191

RESUMO

A new pterocarpan, aeschynocarpin (1), and the known pterocarpan 2-methoxymedicarpin (2) were isolated for the first time from Aeschynomene fascicularis (Fabaceae) and their structures elucidated by means of spectroscopic {UV/Vis, IR, and NMR (1H, 13C, COSY, HMQC,and HMBC)} andmass spectrometric (EI-MS and HRCIMS) techniques. Both compounds were tested in vitro for their cytotoxic and antiproliferative activities against a panel of cancer cell lines. This is the first report on the presence of pterocarpans in the genus Aeschynomene.


Assuntos
Antineoplásicos Fitogênicos/isolamento & purificação , Fabaceae/química , Pterocarpanos/isolamento & purificação , Antineoplásicos Fitogênicos/química , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Células KB , Estrutura Molecular , Casca de Planta/química , Raízes de Plantas/química , Plantas Medicinais/química , Pterocarpanos/química
17.
Nat Prod Commun ; 8(9): 1245-6, 2013 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-24273857

RESUMO

The new flavone glycoside 6-O-(6"-O-E-p-coumaroyl)-beta-D-galactoscutellarein (triumfettalarein, 1), along with indol-3-carboxylic acid (2), beta-sitosterol glycoside, and squalene were isolated from the methanol extract of leaves of Triumfetta semitriloba. The structure of the new isolate was established by spectral methods.


Assuntos
Flavonas/isolamento & purificação , Glicosídeos/isolamento & purificação , Triumfetta/química , Flavonas/química , Glicosídeos/química , Estrutura Molecular , Folhas de Planta/química
18.
Parasitol Res ; 112(2): 559-66, 2013 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-23086442

RESUMO

A total of 82 fungal extracts were selected and screened against Mycobacterium tuberculosis and promastigotes of Leishmania mexicana strains. Results showed inhibitory activity in 29 % of the fungal strains against at least one of the targets tested. The most significant antituberculosis (antiTB) effects were presented by Cylindrocarpon sp. XH9B, Fusarium sp. TA54, Fusarium XH1Ga, Gliocladium penicillioides TH04 and TH21, Gliocladium sp. TH16, Kutilakesa sp. MR46, and Verticillium sp. TH28 strains (minimal inhibition concentration (MIC) = 1.56-25 µg/ml). Mortality of L. mexicana promastigotes was displayed by only four strains, Fusarium sp. TA50, Fusarium sp. TA54, Verticillium sp. TH28, and the unidentified 2TA2 strain (IC(50) = 14.23-100 µg/ml and IC(100) = 50-100 µg/ml). Seven of these most active strains were defatted and their corresponding fractions evaluated again. The results showed the best antiTB activity in Gliocladium sp. TH16 (MIC = 1.56 µg/ml) and the highest leishmanicidal potential in Fusarium sp. TA54 (IC(50) = 6.36 µg/ml). These results show that fungi living in the tropical regions of México have the ability to produce bioactive metabolites that could be used in the near future as natural products to control neglected tropical diseases.


Assuntos
Antiprotozoários/farmacologia , Antituberculosos/farmacologia , Fungos/química , Leishmania mexicana/efeitos dos fármacos , Mycobacterium tuberculosis/efeitos dos fármacos , Antiprotozoários/isolamento & purificação , Antituberculosos/isolamento & purificação , Sobrevivência Celular/efeitos dos fármacos , Humanos , Concentração Inibidora 50 , México , Testes de Sensibilidade Microbiana , Clima Tropical
19.
Nat Prod Res ; 27(3): 286-9, 2013.
Artigo em Inglês | MEDLINE | ID: mdl-22456000

RESUMO

Diphysidione (1), a new p-hydroxyphenyl anhydride, and vitexin (2) were isolated from the leaves of Diphysa carthagenensis. The structure of the new metabolite was characterised as 4-(4-hydroxy-phenyl)-3H-pyran-2,6-dione using 1D and 2D NMR spectroscopy.


Assuntos
Anidridos/química , Fabaceae/química , Folhas de Planta/química , Estrutura Molecular
20.
J Ethnopharmacol ; 135(3): 719-24, 2011 Jun 01.
Artigo em Inglês | MEDLINE | ID: mdl-21501677

RESUMO

AIM OF THE STUDY: To investigate the potential of plants used in Mayan traditional medicine to treat cancer-like symptoms using the Mayan ethnobotany literature, and evaluate their organic extracts for in vitro cytotoxic activity on cancer cell lines. MATERIALS AND METHODS: The selection of the plants studied in this investigation was based on the Mayan ethnobotanical information provided by different literature sources. Extracts were obtained by maceration with methanol for 72 h of each plant part used and evaporated in vacuo to give the corresponding dried extract. Each methanol extract was tested for its cytotoxicity using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay performed in 96-well tissue plates on seven cancer cell lines, lung carcinoma (A549), cervix adenocarcinoma (HeLa), laryngeal carcinoma (Hep-2), nasopharynx carcinoma (KB), breast adenocarcinoma (MCF-7), prostate adenocarcinoma (PC-3), and cervix squamous carcinoma cells (SiHa), as well as normal human embryonic kidney cell line (HEK-293). Cell proliferation/viability was spectrophotometrically assessed at 540 nm after addition of MTT. RESULTS: 51 plants were found in the literature to be used for the treatment of symptoms suggestive of cancer, 21 were chosen to evaluate the cytotoxic activity. Aeschynomene fascicularis root bark extract showed a pronounced cytotoxic activity on Hela and KB cell lines and Bonellia macrocarpa stem and root bark extracts showed similar prominent activities on KB cells. CONCLUSION: 21 plants were selected according to their use in the treatment of cancer-like symptoms recorded in the ethnobotanical literature. Plant extracts prepared from Aeschynomene fascicularis root bark and Bonellia macrocarpa stem and root bark have been selected for extensive studies leading to the isolation of the active constituents.


Assuntos
Antineoplásicos Fitogênicos/uso terapêutico , Etnobotânica , Medicina Tradicional , Neoplasias/tratamento farmacológico , Fitoterapia , Extratos Vegetais/uso terapêutico , Plantas Medicinais , Indígena Americano ou Nativo do Alasca , Antineoplásicos Fitogênicos/farmacologia , Células HeLa , Humanos , Magnoliopsida , Neoplasias/complicações , Casca de Planta , Extratos Vegetais/farmacologia , Raízes de Plantas
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