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1.
J Ethnopharmacol ; 301: 115170, 2023 Jan 30.
Artigo em Inglês | MEDLINE | ID: mdl-35358625

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Monsonia angustifolia is traditionally used to treat anthrax, heartburn, diarrhea, eye infections and hemorrhoids. Dodonaea angustifolia is frequently used as a treatment for dental pain, microbial infections and jungle fever. The two plant species were selected due to the presence of secondary metabolites such as coumarins, flavonoids, terpenoids, saponins and polyphenolics from the crude extracts, which exhibit pharmacological significance. The pure isolated compounds from the crude extracts are known for their diverse structures and interesting pharmacophores. AIM: To isolate and identify antibacterial and antifungal chemical constituents from Monsonia angustifolia and Dodonaea angustifolia plant extracts and evaluate the cytotoxicity of pure compounds from the crude extracts. MATERIALS AND METHODS: Extractives from M. angustifolia and D. angustifolia plants were isolated using chromatographic techniques and structures were elucidated based on NMR, IR and MS spectroscopic techniques. A microplate serial dilution method was used to evaluate the antibacterial activity of extracts and pure compounds against Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa and antifungal activity against Candida albicans and Cryptococcus neoformans. The cytotoxicity was determined using the 3-(4, 5-dimethylthiazol)-2, 5-diphenyl tetrazolium bromide (MTT) assay. RESULTS: The dichloromethane, ethyl acetate and methanol crude extracts from the plants exhibited significant inhibition of microbial growth. The phytochemical investigation of these active crude extracts led to the isolation of five pure active compounds, 5-methoxyjusticidin A (1), cis-phytyl diterpenoidal fatty acid ester (2), stigmasterol (3), ß-sitosterol (4) and 5-hydroxy-7,4'-dimethoxyflavone (5). Stigmasterol (3) showed good antifungal activity against Cryptococcus neoformans with a minimum inhibition concentration (MIC) of 25 µg/mL and Candida albicans (MIC = 50 µg/mL). CONCLUSION: Compounds (1-5) isolated from Monsonia angustifolia and Dodonaea angustifolia showed antibacterial and antifungal activities and were non-toxic against Madin-Darby canine kidney (MDCK) cells and VERO monkey kidney (VERO) cells.


Assuntos
Geraniaceae , Sapindaceae , Antifúngicos/toxicidade , Antifúngicos/química , Estigmasterol , Testes de Sensibilidade Microbiana , Extratos Vegetais/toxicidade , Extratos Vegetais/química , Antibacterianos/toxicidade , Antibacterianos/química
4.
J Ethnopharmacol ; 277: 114222, 2021 Sep 15.
Artigo em Inglês | MEDLINE | ID: mdl-34033901

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: There have been different methods proposed to prevent the sexual transmission of HIV-1 and many of them have centered on the use of anti-retrovirals as microbicides. Given that a large section of the African population still relies on herbal medicine, Lobostemon trigonus (L. trigonus), a traditionally used medicinal plant in South Africa to treat HIV-1 was further investigated for its potential as a natural microbicide to prevent the sexual transmission of HIV-1. METHODS: The aerial parts of L. trigonus were oven-dried at 80 °C, ground, extracted with boiling water for 30 min and then filtered. The aqueous extract produced was then bioassayed using different HIV-1 inhibition assays. The active components were purified and chemically profiled using ultra-performance liquid chromatography/quadrupole time-of flight mass spectrometry (UPLC-qTOF-MS). The mechanism of HIV-1 inhibition was determined by fusion arrest assay and time of addition assay. Molecular modelling and molecular dynamic simulations, using Schrödinger, were used to better understand the molecule's mechanism of entry inhibition by evaluating their docking affinity and stability against the gp120 of HIV-1. RESULTS: The aqueous extract of this plant had a broad spectrum of activity against different subtypes of the virus; neutralizing subtype A, B and C in the TZM-bl cells, with IC50 values ranging from 0.10 to 7.21 µg/mL. The extract was also inhibitory to the virus induced cytopathic effects in CEM-SS cells with an EC50 of 8.9 µg/mL. In addition, it inhibited infection in peripheral blood mononuclear cells (PBMC) and macrophages with IC50 values of 0.97 and 4.4 µg/mL, respectively. In the presence of vaginal and seminal simulants, and in human semen it retained its inhibitory activity albeit with a decrease in efficiency, by about 3-fold. Studies of the mode of action suggested that the extract blocked HIV-1 attachment to target cells. No toxicity was observed when the Lactobacilli strains, L. acidophilus, L. jensenii, and L. crispatus that populate the female genital tract were cultured in the presence of L. trigonus extract. UPLC-qTOF-MS analyses of the purified fraction of the extract, confirmed the presence of six compounds of which four were identified as rosmarinic acid, salvianolic acids B and C and lithospermic acid. The additional molecular dynamic simulations provided further insight into the entry inhibitory characteristics of salvianolic acid B against the HIV-1 gp120, with a stable pose being found within the CD4 binding site. CONCLUSION: The data suggests that the inhibitory effect of L. trigonus may be due to the presence of organic acids which are known to possess anti-HIV-1 properties. The molecules salvianolic acids B and C have been identified for the first time in L. trigonus species. Our study also showed that the L. trigonus extract blocked HIV-1 attachment to target cells, and that it has a broad spectrum of activity against different subtypes of the virus; thus, justifying further investigation as a HIV-1 microbicide.


Assuntos
Boraginaceae/química , HIV-1/efeitos dos fármacos , Extratos Vegetais/farmacologia , Fármacos Anti-HIV/isolamento & purificação , Fármacos Anti-HIV/farmacologia , Cromatografia Líquida de Alta Pressão , Feminino , Humanos , Leucócitos Mononucleares/efeitos dos fármacos , Leucócitos Mononucleares/virologia , Masculino , Modelos Moleculares , Simulação de Dinâmica Molecular , Componentes Aéreos da Planta , África do Sul
5.
Nat Prod Res ; 35(12): 1968-1976, 2021 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-31393174

RESUMO

A novel cycloartanol (1) and an acylated Sutherlandioside D (2) together with two known cycloartane derivatives, Sutherlandioside B (3) and Sutherlandioside A (4), were isolated from the aerial parts of Sutherlandia frutescens. The structures of these compounds were established by a combination of 1- and 2-D NMR techniques and further confirmed by high resolution ToF mass spectrometry (HRToFMS). Preliminary biological studies were also conducted to assess the activity of different plant extracts, fractions and compounds on cytokine expression. Compounds 1 and 2 prompted an increase in IL-6 expression while compound 4 showed a reduced IL-6 expression compared to the controls. Compound 1 is an effective suppressor of IL-10 expression. The plant compounds inhibited the expression of the two cytokines, IL-10 and TNFα. The results of the assays suggested that some components in the plant extract influence the immune system by suppressing the expression of IL-6, IL-10 and TNFα.


Assuntos
Citocinas/metabolismo , Fabaceae/química , Fatores Imunológicos/química , Fatores Imunológicos/farmacologia , Avaliação Pré-Clínica de Medicamentos , Fabaceae/metabolismo , Humanos , Espectroscopia de Ressonância Magnética , Espectrometria de Massas , Estrutura Molecular , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Plantas Medicinais/química , Triterpenos/química
6.
Onderstepoort J Vet Res ; 86(1): e1-e7, 2019 Jul 22.
Artigo em Inglês | MEDLINE | ID: mdl-31368326

RESUMO

Hot water and hydroethanolic (70:30) extracts were prepared from 15 plant species, which were investigated to discover eco-friendly and less expensive tick control methods as an alternative to synthetic acaricides. A contact bioassay was used to determine the acaricidal activity of these extracts against the cattle tick, Rhipicephalus turanicus (Acari: Ixodidae) at a concentration of 20% (200 mg/mL). The hydroethanolic extracts had better activity than the hot water extracts against R. turanicus. The hydroethanolic extract from Tabernaemontana elegans (leaves) had the best mortality (87.0%). This was followed by Calpurnia aurea (stems) with a mortality of 75.0%, Schkuhria pinnata (whole plant) with a mortality of 67.0% and Aloe rupestris (leaves) with a mortality of 66.6%. The toxicity of the plant extracts was also investigated and it was found that most of the hydroethanolic and hot water extracts were either safe or very safe on human Vero kidney and liver HepG2 cells. From this study, it was evident that botanicals have the potential to be developed as environmentally benign natural acaricides against R. turanicus.


Assuntos
Acaricidas/farmacologia , Acaricidas/toxicidade , Extratos Vegetais/farmacologia , Extratos Vegetais/toxicidade , Rhipicephalus/efeitos dos fármacos , Animais , Chlorocebus aethiops , Feminino , Células Hep G2 , Humanos , Rim/efeitos dos fármacos , Fígado/efeitos dos fármacos , Magnoliopsida/química , Masculino , Especificidade da Espécie
7.
Nat Prod Res ; 33(22): 3240-3247, 2019 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-29741101

RESUMO

The stem bark extract of Suregada zanzibariensis afforded a previously undescribed ent-abietane diterpenoid trivially named mangiolide (1) and a known jolkinolide B (2) via anticancer bioassay-guided fractionation. The CH2Cl2:MeOH extract of S. zanzibariensis was initially analysed for its anticancer properties against three cancer cell lines, renal (TK10), melanoma (UACC62), and breast (MCF7) and was found to be potent at low µg/mL ranges. Compound 1, 6α-acetoxy-14-keto-ent-abieta-7(8),13(15)-diene-16,12-olide (mangiolide) inhibited the growth of renal (TK10) with a GI50 of 0.02 µg/mL; a GI50 of 0.03 µg/mL for melanoma (UACC62) and a GI50 of 0.05 µg/mL for breast (MCF7) cancer cell lines. Compound 2, 8,13-diepoxy-13,15-ent-abietene-16,12-olide (jolkinolide B) inhibited the growth (GI50) of the cell lines at 3.31 µg/mL for renal (TK10), 0.94 µg/mL for melanoma (UACC62) and 2.99 µg/mL for the breast (MCF7). The structures were established on the basis of their spectroscopic analysis and the absolute stereostructures assigned using electronic circular dichroism (ECD).


Assuntos
Abietanos/farmacologia , Suregada/química , Abietanos/química , Abietanos/isolamento & purificação , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Diterpenos/isolamento & purificação , Diterpenos/farmacologia , Ensaios de Seleção de Medicamentos Antitumorais , Euphorbiaceae/química , Humanos , Estrutura Molecular , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Análise Espectral , Estereoisomerismo
8.
BMC Complement Altern Med ; 18(1): 137, 2018 May 02.
Artigo em Inglês | MEDLINE | ID: mdl-29720141

RESUMO

BACKGROUND: Solanum aculeastrum fruits are used by some cancer sufferers as a form of alternative treatment. Scientific literature is scarce concerning its anticancer activity, and thus the aim of the study was to assess the in vitro anticancer and P-glycoprotein inhibitory potential of extracts of S. aculeastrum fruits. Furthermore, assessment of the combinational effect with doxorubicin was also done. METHODS: The crude extract was prepared by ultrasonic maceration. Liquid-liquid extraction yielded one aqueous and two organic fractions. Bioactive constituents were isolated from the aqueous fraction by means of column chromatography, solid phase extraction and preparative thin-layer chromatography. Confirmation of bioactive constituent identity was done by nuclear magnetic resonance and ultra-performance liquid chromatography mass spectrometry. The crude extract and fractions were assessed for cytotoxicity and P-glycoprotein inhibition in both cancerous and non-cancerous cell lines using the sulforhodamine B and rhodamine-123 assays, respectively. RESULTS: Both the crude extract and aqueous fraction was cytotoxic to all cell lines, with the SH-SY5Y neuroblastoma cell line being most susceptible to exposure (IC50 = 10.72 µg/mL [crude], 17.21 µg/mL [aqueous]). Dose-dependent P-glycoprotein inhibition was observed for the crude extract (5.9 to 18.9-fold at 100 µg/mL) and aqueous fraction (2.9 to 21.2 at 100 µg/mL). The steroidal alkaloids solamargine and solanine were identified. While solanine was not bioactive, solamargine displayed an IC50 of 15.62 µg/mL, and 9.1-fold P-glycoprotein inhibition at 100 µg/mL against the SH-SY5Y cell line. Additive effects were noted for combinations of doxorubicin against the SH-SY5Y cell line. CONCLUSIONS: The crude extract and aqueous fraction displayed potent non-selective cytotoxicity and noteworthy P-glycoprotein inhibition. These effects were attributed to solamargine. P-glycoprotein inhibitory activity was only present at concentrations higher than those inducing cytotoxicity, and thus does not appear to be the likely mechanism for the enhancement of doxorubicin's cytotoxicity. Preliminary results suggest that non-selective cytotoxicity may hinder drug development, however, further assessment of the mode of cell death is necessary to determine the route forward.


Assuntos
Membro 1 da Subfamília B de Cassetes de Ligação de ATP/antagonistas & inibidores , Sobrevivência Celular/efeitos dos fármacos , Alcaloides de Solanáceas/farmacologia , Solanum/química , Antineoplásicos/farmacologia , Morte Celular/efeitos dos fármacos , Linhagem Celular Tumoral , Doxorrubicina/farmacologia , Sinergismo Farmacológico , Humanos
9.
Onderstepoort J Vet Res ; 84(1): e1-e6, 2017 Nov 23.
Artigo em Inglês | MEDLINE | ID: mdl-29227130

RESUMO

The acaricidal activity of acetone and ethanol extracts of 12 plant species was evaluated using the contact method on Rhipicephalus turanicus (Acari: Ixodidae) ticks at an initial concentration of 20% (200 mg/mL). Eight of the 12 plants had mortality greater than 50% and the acetone extracts had better acaricidal activity than the ethanol extracts. The acetone extract of Calpurnia aurea (leaves and flowers) had the highest corrected mortality (CM) of 92.2% followed by Schkuhria pinnata (whole plant) with a CM of 88.9%, Ficus sycomorus (bark and stems) 86.7% and Senna italica subsp. arachoides (roots, leaves and fruits) 83.3%. Selected extracts were tested at five different concentrations using the adult immersion test. From dose-response assays, EC50 values of 61.82 mg/mL, 115.21 mg/mL and 161.02 mg/mL were obtained for the acetone extracts of S. pinnata (whole plant), S. italica subsp. arachoides (roots, leaves and fruits) and C. aurea (leaves and flowers) respectively. The ethanol extract of Monsonia angustifolia (whole plant) had the highest CM of 97.8% followed by S. pinnata (whole plant) with a CM of 86.7%, C. aurea (leaves and flowers) 81.1% and Cleome gynandra (leaves) 77.8%. There is potential for the development of environmentally benign botanicals as natural acaricides against R. turanicus.


Assuntos
Acaricidas/farmacologia , Doenças dos Bovinos/prevenção & controle , Extratos Vegetais/farmacologia , Rhipicephalus/efeitos dos fármacos , Doenças Transmitidas por Carrapatos/veterinária , Animais , Bovinos , Concentração Inibidora 50 , Fitoterapia , Doenças Transmitidas por Carrapatos/prevenção & controle
10.
J Agric Food Chem ; 65(15): 3133-3140, 2017 Apr 19.
Artigo em Inglês | MEDLINE | ID: mdl-28378593

RESUMO

Alzheimer's disease (AD), a progressive neurodegenerative disorder, is characterized by the accumulation of neurotoxic ß-amyloid (Aß) peptides, which consequently affects cognitive decline and memory impairment. Current research on AD treatment is actively focusing on the prevention of neurotoxic Aß peptide accumulation. Monsonia angustifolia is reported to be consumed as an indigenous vegetable in Tanzania. In this study, we investigated the effect of the ethanol (EtOH) extract of M. angustifolia dried ground material on Aß production and spatial learning ability as protection against AD. The formation of Aß peptides was significantly reduced in HeLa cells stably transfected with the Swedish mutant form of ß-amyloid precursor protein (APPsw) after treatment with a 60% EtOH extract of M. angustifolia. We next examined the cognitive-improving effects of the EtOH extract in vivo. Tg2576 mice were treated with extract for 6 months and subjected to Morris water maze and novel object recognition tests. The results showed that the 60% EtOH extract of M. angustifolia significantly ameliorated behavioral deficits of the AD transgenic mice and reduced the level of insoluble Aß42 in the cerebral cortex and hippocampus. We further found that the 60% EtOH extract was effective for memory function recovery after shorter treatment (4 months). In addition, we isolated and identified several single compounds, justicidin A, 5-methoxyjusticidin A, chinensinaphthol, retrochinensinaphthol methyl ether, and suchilactone, from M. angustifolia and tested these compounds. Among them, justicidin A potently decreased the formation of Aß in APPsw-transfected cells. These data suggest that the 60% EtOH extract of M. angustifolia has the potential to be developed as a treatment of AD. Furthermore, justicidin A may contribute, at least partially, to the Aß alteration observed with the extract treatment.


Assuntos
Doença de Alzheimer/prevenção & controle , Geraniaceae/química , Extratos Vegetais/administração & dosagem , Doença de Alzheimer/metabolismo , Doença de Alzheimer/psicologia , Peptídeos beta-Amiloides/metabolismo , Precursor de Proteína beta-Amiloide/metabolismo , Animais , Cognição/efeitos dos fármacos , Modelos Animais de Doenças , Humanos , Masculino , Memória/efeitos dos fármacos , Camundongos , Camundongos Transgênicos , Extratos Vegetais/química
11.
Vet Parasitol ; 234: 10-12, 2017 Jan 30.
Artigo em Inglês | MEDLINE | ID: mdl-28115176

RESUMO

The goal of our research is to develop a lower cost eco-friendly tick control method because acaricides that are commonly used to control ticks are often toxic, harmful to the environment or too expensive for resource-limited farmers. Acetone and ethanol extracts were prepared and their acaricidal activities determined against the southern cattle tick, Rhipicephalus (Boophilus) microplus. A 1% solution of each of the plant extracts was prepared for efficacy testing using the adapted Shaw Larval Immersion Test (SLIT). The acetone stem extract from Cissus quadrangularis (Vitaceae) and the ethanol leaf and flower extract from Calpurnia aurea (Fabaceae) had potent activity like that of the commercial acaricide, chlorfenvinphos [corrected mortality (CM)=100.0%]. The ethanol extracts of the stem of C. quadrangularis (CM=98.9%) and that of the roots, leaves and fruit of Senna italica subsp arachoides (CM=96.7%) also had good acaricidal activity. There is potential for the development of botanicals as natural acaricides against R. (B.) microplus that can be used commercially to protect animals against tick infestation. Further studies to isolate the acaricidal active compounds and to determine the environmental fate, species toxicity and skin toxicity of these plants species are, however, required before they can be considered as a treatment against ticks.


Assuntos
Acaricidas , Cissus/química , Fabaceae/química , Extratos Vegetais/farmacologia , Rhipicephalus/efeitos dos fármacos , Controle de Ácaros e Carrapatos , Acetona/química , Animais , Clorfenvinfos/farmacologia , Etanol/química , Larva/efeitos dos fármacos , África do Sul
12.
Artigo em Inglês | MEDLINE | ID: mdl-27672399

RESUMO

The acute and subacute toxicity profile of the aerial extract of Monsonia angustifolia in Wistar rats was evaluated. The Organization for Economic Cooperation and Development (OECD) 420 guideline was adopted in the acute toxicity testing with a single oral dose of 5000 mg/kg (b.w.). For the 28-day daily oral dosing, the extract was administered at 75, 150, and 300 mg/kg b.w.; 1% ethanol in sterile distilled water was used as control. Clinical toxicity signs were subsequently evaluated. At a single dose of 5000 mg/kg b.w. the extract elicited no treatment-related signs of toxicity in the animals during the 14 days of experimental period. In the subacute toxicity, there was no significant difference in hematological, renal, and liver function indices. However, dose-dependent significant increases were observed on the plasma concentrations of white blood cell and platelet counts of the treated animals compared to the control group. While cage observations revealed no treatment-facilitated signs of toxicity, histopathological examinations of the kidneys and liver also showed no obvious lesions and morphological changes. These results suggest that the extract may be labelled and classified as safe and practically nontoxic within the doses and period of investigation in this study.

13.
Onderstepoort J Vet Res ; 83(1): e1-7, 2016 07 29.
Artigo em Inglês | MEDLINE | ID: mdl-27543148

RESUMO

The nematode, Haemonchus contortus, is responsible for major economic losses in the livestock industry. The management of parasites such as H. contortus has been through the use of synthetic parasiticides. This has resulted in the presence of residues in meat and milk, which affects food safety. The development of resistance to available anthelmintics coupled with their high cost has further complicated matters. This has led to the investigation of alternative methods to manage nematodes, including the use of plants and plant extracts as a potential source of novel anthelmintics. Acetone extracts were prepared from 15 South African plant species and their anthelmintic activity determined using the egg hatch assay (EHA). The leaf extract of Cleome gynandra had the best inhibitory activity (68% ± 3%) at a concentration of 2.5 mg/mL, followed by the stem extract of Maerua angolensis (65% ± 5%). The extracts had a relatively low toxicity on Vero cells determined by the MTT (3-(4,5-dimethylthiazol-2-yl)-2,5- diphenyltetrazolium bromide) cellular assay.


Assuntos
Anti-Helmínticos/farmacologia , Hemoncose/veterinária , Haemonchus/efeitos dos fármacos , Extratos Vegetais/farmacologia , Animais , Hemoncose/prevenção & controle , Larva/efeitos dos fármacos , Dose Letal Mediana , Gado , Óvulo/efeitos dos fármacos , Fitoterapia , Componentes Aéreos da Planta , Raízes de Plantas
14.
Vet Parasitol ; 224: 39-43, 2016 Jul 15.
Artigo em Inglês | MEDLINE | ID: mdl-27270388

RESUMO

The African blue tick, Rhipicephalus (Boophilus) decoloratus, is a common tick species found in South Africa and affects cattle production as well as vectoring pathogens in regions of Africa and Asia. In an attempt to develop a non-toxic, lower cost and environmentally friendly tick control method, twenty-six plant extracts were prepared from thirteen plant species using 99.5% acetone and 99% ethanol. The adapted Shaw Larval Immersion Test (SLIT) was used to test the efficacy of the extracts. A 1% solution of each of the plant extracts was prepared for efficacy testing and the ethanol extracts were found to have better acaricidal activity than the acetone extracts. The ethanol extract from the leaves and flowers of Calpurnia aurea had the best activity [corrected mortality (CM)=82.9%] which was followed by the stem extract of Cissus quadrangularis (CM=80.4%). The plant species were screened against Vero cells and were found to have low toxicity. From this study it is apparent that there is potential for the development of botanicals as natural acaricides against R. (B.) decoloratus.


Assuntos
Acaricidas , Extratos Vegetais , Plantas/química , Rhipicephalus , Acaricidas/toxicidade , Acetona/química , Animais , Sobrevivência Celular/efeitos dos fármacos , Chlorocebus aethiops , Etanol/química , Flores/química , Extratos Vegetais/toxicidade , Folhas de Planta/química , Caules de Planta/química , África do Sul , Células Vero
15.
BMC Complement Altern Med ; 15: 343, 2015 Oct 02.
Artigo em Inglês | MEDLINE | ID: mdl-26432276

RESUMO

BACKGROUND: Monsonia angustifolia (Geraniaceae) is a medicinal plant traditionally used in South Africa to increase libido and to treat erectile dysfunction. METHODS: In-vivo aphrodisiac activities of the crude extracts of the plant prepared in water at 3, 30 and 300 mg/kg body weight were evaluated for 7 days using sildenafil citrate (Viagra) and 1% ethanol in distilled water as positive and negative controls respectively. Male rats were selected and monitored in each group for sexual behaviour by exposing them to sexually receptive females on days 1, 3 and 7 for 60 minutes each between 7:00 pm and 3:00 am. The following male sexual parameters were observed: Mount Frequency (MF), Intromission Frequency (IF), Mount Latency (ML), Intromission Latency (IL), Ejaculation Frequency (EF), Ejaculatory Latency (EL) and Post-Ejaculatory Interval (PEI). RESULTS: The administration of the extract resulted in significant increase (p < 0.05) in mount frequency, intromission frequency, ejaculation frequency, ejaculation latency and serum hormone concentrations. The computed indices of sexual behaviour such as erection, quick flips, long flips and total penile reflexes were also increased. However, the mount latency, intromission latency and post ejaculation interval were significantly decreased throughout the experimental period. The administration of 300 mg/kg body weight of the aqueous extract produced the best effects in all the parameters. CONCLUSION: Generally, the extract of Monsonia angustifolia produced pro-sexual stimulatory effects in the male rats especially when administered at 300 mg/kg body weight. The results validate the use of the plant by the indigenous people to increase libido and treat premature ejaculation and erectile dysfunction in males.


Assuntos
Afrodisíacos/farmacologia , Disfunção Erétil/tratamento farmacológico , Magnoliopsida/química , Extratos Vegetais/farmacologia , Animais , Ejaculação/efeitos dos fármacos , Feminino , Humanos , Masculino , Ereção Peniana/efeitos dos fármacos , Componentes Aéreos da Planta , Ratos , Ratos Wistar , Comportamento Sexual , Comportamento Sexual Animal/efeitos dos fármacos , Testosterona/sangue
16.
Fitoterapia ; 93: 81-7, 2014 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-24382449

RESUMO

Human African trypanosomiasis is a neglected tropical disease in sub Saharan Africa that is fatal if left untreated. In a search for new natural products with antitrypanosomal activity, we recently identified abruquinones B and I from Abrus precatorius as potent in vitro trypanocidal compounds with high selectivity indices. To obtain sufficient compound for in vivo efficacy tests in mice, a second batch of plant material was re-collected and extracted. However, the chemical profiles of the two batches differed, and additional abruquinones were isolated and identified by HR-ESI-MS, and 1D and 2D NMR ((1)H, (13)C, COSY, HMBC, HSQC, and NOESY) spectroscopy. Abruquinones J (1), K (2), and L (3) were new, while abruquinones A (4) and D (5) were known from the first batch of plant material. The absolute configuration of compounds 1 to 3 was determined by comparison of electronic circular dichroism (ECD) spectra with calculated ECD data. Compounds 2 to 5 showed high in vitro activity against T. b. rhodesiense (IC50 of 0.01, 0.02, 0.02 and 0.01 µM, respectively), and remarkable SIs of 508, 374, 1379, and 668, respectively.


Assuntos
Abrus/química , Tripanossomicidas/isolamento & purificação , Animais , Benzopiranos/isolamento & purificação , Benzopiranos/toxicidade , Benzoquinonas/isolamento & purificação , Benzoquinonas/toxicidade , Testes de Sensibilidade Microbiana , Ratos
17.
BMC Complement Altern Med ; 13: 356, 2013 Dec 13.
Artigo em Inglês | MEDLINE | ID: mdl-24330447

RESUMO

BACKGROUND: Athrixia phylicoides DC. (Asteraceae) is used medicinally in South Africa to treat a plethora of ailments, including heart problems, diabetes, diarrhoea, sores and infected wounds. It is also prepared in the form of a tea (hot decoction) taken as a refreshing, pleasant-tasting beverage with commercialization potential. METHODS: Extracts of the dried ground aerial parts were prepared using organic solvents (diethyl ether, dichloromethane/methanol, ethyl acetate and ethanol) and water. These extracts were subjected to HPLC, TLC and bioautography analysis with the aim of linking a range of peaks visualized in HPLC chromatography profiles to antibacterial and antifungal activity of the same extracts. RESULTS: HPLC revealed a group of compounds extracted by more than one solvent. Compounds identified include inositol, caffeic acid, quercetin, kaempferol, apigenin, hymenoxin and oleanolic acid. The organic extracts displayed similar TLC profiles, and bioautography indicated approximately five antibacterial compounds, but only two antifungal compounds in these extracts. Bioautography indicated that cold water extracted the least antimicrobial compounds. CONCLUSIONS: Several previously unknown compounds were identified in Athrixia phylicoides extracts, and bioautography indicated a number of antibacterial and antifungal compounds. There were notable differences in chemical composition and bioactivity between the organic and aqueous extracts. Further research is necessary to fully characterize the active components of the extracts.


Assuntos
Antibacterianos/química , Antibacterianos/farmacologia , Antifúngicos/química , Antifúngicos/farmacologia , Asteraceae/química , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Bactérias/efeitos dos fármacos , Cromatografia Líquida de Alta Pressão/métodos , Cromatografia em Camada Fina , Fungos/efeitos dos fármacos , Interações Hidrofóbicas e Hidrofílicas , Testes de Sensibilidade Microbiana , Componentes Aéreos da Planta/química
18.
Nat Prod Commun ; 8(9): 1213-6, 2013 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-24273848

RESUMO

Boophone disticha (Amaryllidaceae) is widely used in traditional medicine in southern Africa. Several alkaloids, volatile oils and fatty acids have been isolated from the plant. However, there has been no literature report of a triterpene from B. disticha. Cycloeucalenol, a cycloartane triterpene, together with its regio-isomer, was isolated from the ethyl acetate extract of the bulbs using column chromatography and preparative thin layer chromatography. Structural elucidation was carried out using 1D and 2D NMR and mass spectroscopy. The MTT and neutral red assays were used to assess the cytotoxicity of the compound in human neuroblastoma (SH-SY5Y) cells. The compound was obtained as a mixture of two regio-isomers, which were separated for the first time by chromatographic optimization. Integration of the 1H NMR spectrum showed that cycloeucalenol and its regio-isomer were present in a ratio of 1.04:1. A dose-dependent decrease in cell viability was observed using both cytotoxicity assays. IC51 values of 173.0 +/- 5.1 microM and 223.0 +/- 6.4 microM were obtained for the MTT and neutral red assays, respectively, indicative of the low toxicity of the compound. This work describes for the first time, the presence of triterpene compounds from the genus Boophone.


Assuntos
Antineoplásicos Fitogênicos/isolamento & purificação , Liliaceae/química , Fitosteróis/isolamento & purificação , Linhagem Celular Tumoral , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Isomerismo , Plantas Medicinais/química
19.
BMC Complement Altern Med ; 13: 304, 2013 Nov 05.
Artigo em Inglês | MEDLINE | ID: mdl-24188320

RESUMO

BACKGROUND: Aging is an inevitable process for all living organisms. During this process reactive oxygen species generation is increased which leads to the activation of hyaluronidase, collagenase and elastase, which can further contribute to skin aging. Four southern African medicinal plants; Clerodendrum glabrum, Schotia brachypetala, Psychotria capensis and Peltophorum africanum, were investigated to assess their anti-aging properties. METHODS: Anti-elastase, anti-collagenase and anti-hyaluronidase activities of twenty-eight samples, consisting of methanol and ethyl acetate extracts of the four plants, were determined using spectrophotometric methods. Radical scavenging activity was determined by the ability of the plant extracts to scavenge the ABTS•+ radical. RESULTS: The majority of the samples in the anti-elastase assay and nine in the anti-collagenase assay showed more than 80% inhibition. The ethyl acetate extract of S. brachypetala bark and leaves of P. capensis inhibited elastase activity by more than 90%. The methanol extract of S. brachypetala bark contained the highest anti-hyaluronidase activity (75.13 ± 7.49%) whilst the ethyl acetate extract of P. africanum bark exhibited the highest antioxidant activity (IC50: 1.99 ± 0.23 µg/ml). CONCLUSION: The free radical scavenging activity and enzyme inhibitory activity of the plant extracts investigated suggests that they can help restore skin elasticity and thereby slow the wrinkling process. P. africanum was the plant with the most promising activity and will be subjected to further testing and isolation of the active compound/s.


Assuntos
Envelhecimento/efeitos dos fármacos , Inibidores Enzimáticos/análise , Extratos Vegetais/análise , Plantas Medicinais/química , Inibidores Enzimáticos/isolamento & purificação , Inibidores Enzimáticos/farmacologia , Humanos , Hialuronoglucosaminidase/antagonistas & inibidores , Oxirredução , Elastase Pancreática/antagonistas & inibidores , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/farmacologia , África do Sul
20.
Artigo em Inglês | MEDLINE | ID: mdl-24146494

RESUMO

Amyloid-beta peptide (Aß) is implicated in the pathogenesis of Alzheimer's disease (AD), a neurodegenerative disorder. This study was designed to determine the effect of four medicinal plants used to treat neurodegenerative diseases on Aß-induced cell death. Cytotoxicity of the ethanol extracts of the plants was determined against SH-SY5Y (human neuroblastoma) cells which were untreated, as well as toxically induced with Aß, using the MTT and neutral red uptake assays. Cell viability was reduced to 16% when exposed to 20 µM Aß25-35 for 72 h. The methanol extract of the roots of Ziziphus mucronata Willd., Lannea schweinfurthii (Engl.) Engl. and Terminalia sericea Burch. ex DC., were the least toxic to the SH-SY5Ycells at the highest concentration tested (100 µg/ml). All four plants tested were observed to reduce the effects of Aß-induced neuronal cell death, indicating that they may contain compounds which may be relevant in the prevention of AD progression.


Assuntos
Doença de Alzheimer/metabolismo , Peptídeos beta-Amiloides/metabolismo , Anacardiaceae , Crinum , Fragmentos de Peptídeos/metabolismo , Extratos Vegetais/farmacologia , Terminalia , Ziziphus , Doença de Alzheimer/tratamento farmacológico , Peptídeos beta-Amiloides/efeitos adversos , Morte Celular/efeitos dos fármacos , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Humanos , Neuroblastoma , Neurônios/efeitos dos fármacos , Fragmentos de Peptídeos/efeitos adversos , Extratos Vegetais/uso terapêutico , Plantas Medicinais
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