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1.
BMC Ecol ; 20(1): 45, 2020 08 03.
Artículo en Inglés | MEDLINE | ID: mdl-32746816

RESUMEN

BACKGROUND: In this multidisciplinary study we present soil chemical, phytochemical and GIS spatial patterning evidence that fairy circles studied in three separate locations of Namibia may be caused by Euphorbia species. RESULTS: We show that matrix sand coated with E. damarana latex resulted in faster water-infiltration rates. GC-MS analyses revealed that soil from fairy circles and from under decomposing E. damarana plants are very similar in phytochemistry. E. damarana and E. gummifera extracts have a detrimental effect on bacteria isolated from the rhizosphere of Stipagrostis uniplumis and inhibit grass seed germination. Several compounds previously identified with antimicrobial and phytotoxic activity were also identified in E. gummifera. GIS analyses showed that perimeter sizes and spatial characteristics (Voronoi tessellations, distance to nearest neighbour ratio, pair correlation function and L-function) of fairy circles are similar to those of fairy circles co-occurring with E. damarana (northern Namibia), and with E. gummifera (southern Namibia). Historical aerial imagery showed that in a population of 406 E. gummifera plants, 134 were replaced by fairy circles over a 50-year period. And finally, by integrating rainfall, altitude and landcover in a GIS-based site suitability model, we predict where fairy circles should occur. The model largely agreed with the distribution of three Euphorbia species and resulted in the discovery of new locations of fairy circles, in the far southeast of Namibia and part of the Kalahari Desert of South Africa. CONCLUSIONS: It is proposed that the allelopathic, adhesive, hydrophobic and toxic latex of E. damarana, E. gummifera, and possibly other species like E. gregaria, is the cause of the fairy circles of Namibia in the areas investigated and possibly in all other areas as well.


Asunto(s)
Euphorbia , Adhesivos , Látex , Namibia , Suelo
2.
Mol Plant Microbe Interact ; 30(9): 710-724, 2017 09.
Artículo en Inglés | MEDLINE | ID: mdl-28535078

RESUMEN

Gray leaf spot (GLS), caused by the sibling species Cercospora zeina or Cercospora zeae-maydis, is cited as one of the most important diseases threatening global maize production. C. zeina fails to produce cercosporin in vitro and, in most cases, causes large coalescing lesions during maize infection, a symptom generally absent from cercosporin-deficient mutants in other Cercospora spp. Here, we describe the C. zeina cercosporin toxin biosynthetic (CTB) gene cluster. The oxidoreductase gene CTB7 contained several insertions and deletions as compared with the C. zeae-maydis ortholog. We set out to determine whether complementing the defective CTB7 gene with the full-length gene from C. zeae-maydis could confer in vitro cercosporin production. C. zeina transformants containing C. zeae-maydis CTB7 were generated by Agrobacterium tumefaciens-mediated transformation and were evaluated for in vitro cercosporin production. When grown on nitrogen-limited medium in the light-conditions conducive to cercosporin production in other Cercospora spp.-one transformant accumulated a red pigment that was confirmed to be cercosporin by the KOH assay, thin-layer chromatography, and ultra performance liquid chromatography-quadrupole-time-of-flight mass spectrometry. Our results indicated that C. zeina has a defective CTB7, but all other necessary machinery required for synthesizing cercosporin-like molecules and, thus, C. zeina may produce a structural variant of cercosporin during maize infection.


Asunto(s)
Ascomicetos/genética , Proteínas Fúngicas/genética , Prueba de Complementación Genética , Perileno/análogos & derivados , Zea mays/microbiología , Empalme Alternativo/genética , Secuencia de Aminoácidos , Ascomicetos/aislamiento & purificación , Secuencia de Bases , Vías Biosintéticas/genética , Simulación por Computador , Secuencia Conservada/genética , ADN de Hongos/genética , Proteínas Fúngicas/química , Proteínas Fúngicas/metabolismo , Eliminación de Gen , Regulación Fúngica de la Expresión Génica , Genes Fúngicos , Intrones/genética , Espectrometría de Masas , Familia de Multigenes , Oxidorreductasas/metabolismo , Perileno/metabolismo , Transcripción Genética , Transformación Genética
3.
Bioorg Med Chem ; 22(17): 5013-9, 2014 Sep 01.
Artículo en Inglés | MEDLINE | ID: mdl-25059501

RESUMEN

In an effort to establish new candidates with enhanced anticancer activity of 5-hydroxy-7-methyl-1,4-naphthoquinone scaffold (7-methyljuglone) previously isolated from the root extract of Euclea natalensis, a series of 7-methyljuglone derivatives have been synthesized and assessed for cytotoxicity on selected human cancer lines. These compounds were screened in vitro for anticancer activity on MCF-7, HeLa, SNO and DU145 human cancer cell lines by MTT assay. Most of them exhibited significant toxicity on cancer cell lines with lower IC50 values. The most potent derivative (19) exhibited the toxicity on HeLa and DU145 cell lines with IC50 value of 5.3 and 6.8µM followed by compound (5) with IC50 value of 10.1 and 9.3µM, respectively. Structure-activity relationship reveals that the fluoro substituents at position C-8 while hydroxyl substituents at C-2 and C-5 positions played an important role in toxicity.


Asunto(s)
Antineoplásicos/síntesis química , Antineoplásicos/farmacología , Naftoquinonas/química , Naftoquinonas/farmacología , Antineoplásicos/química , Ciclo Celular/efectos de los fármacos , Proliferación Celular/efectos de los fármacos , Relación Dosis-Respuesta a Droga , Ensayos de Selección de Medicamentos Antitumorales , Células HeLa , Humanos , Células MCF-7 , Estructura Molecular , Naftoquinonas/síntesis química , Relación Estructura-Actividad , Células Tumorales Cultivadas , Células U937
4.
Bioelectron Med ; 6(1): 22, 2020 Nov 24.
Artículo en Inglés | MEDLINE | ID: mdl-33292846

RESUMEN

COVID-19 has left mankind desperately seeking how to manage dramatically rising infection rates associated with severe disease progressions. COVID-19 courses range from mild symptoms up to multiple organ failure and death, triggered by excessively high serum cytokine levels (IL 1ß, IL 6, TNF α, IL 8). The vagally driven cholinergic anti-inflammatory pathway (CAP) stops the action of nuclear factor κB (NF-κB), the transcriptional factor of pro-inflammatory cytokines. Thus, well-balanced cytokine release depends on adequate vagal signaling. Coronaviruses replicate using NF-κB transcriptional factor as well. By degrading the cytoplasmatic inhibitor of NF-κB subunits (IκB), coronaviruses induce unrestricted NF-κB expression accelerating both, virus replication and cytokine transcription.We hypothesize that CAP detriment due to depressed vagal tone critically determines the severity of COVID-19.

5.
Ann Trop Med Parasitol ; 103(5): 427-39, 2009 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-19583913

RESUMEN

In a recent study, various extracts of Pterocarpus angolensis were prepared and tested against bacteria. The acetone extract was found to be the most active against all the bacteria investigated, with minimum inhibitory concentrations varying from 0.0156 mg/ml against Staphylococcus aureus to 2 mg/ml against Enterobacter cloacae. Seven pure compounds were subsequently isolated from the ethanol extract of P. angolensis. Using several chromatographic and spectroscopic methods, the structures of five of these compounds - phthalate and four derivatives of epicatechin [(-)-epicatechin, epicatechin-3-O-galate, epicatechin (4beta-8)-epicatechin (B2), and a hexamer of epicatechin] - were successfully determined. The seven purified compounds were then further tested, in vitro, against Staphylococcus aureus and Entamoeba histolytica, and for their in-vitro cytotoxic activity. Although all seven were active against S. aureus, just one of the purified compounds from P. angolensis and piperitenone, a pure compound isolated from Lippia javanica essential oil, were found to have marked activity against Entamoeba histolytica, with median inhibitory concentrations (IC(50)) of 25 and 100 microg/ml, respectively. The other P. angolensis compounds were either weakly active or showed no activity against the amoebae when tested at concentrations up to 400 microg/ml. All seven compounds isolated from P. angolensis showed less toxicity against cultures of human (HCT-8) cells than piperitenone, with IC(50) of 175-375 microg/ml. The presence of epichatechin and derivatives (with strong antibacterial activities but generally weak activities against Entamoeba histolytica) in the stem bark of P. angolensis has thus been demonstrated. Further investigation of the activities of these compounds and their potential use in the treatment of bacterial diseases appears justified.


Asunto(s)
Antibacterianos/farmacología , Bacterias/efectos de los fármacos , Entamoeba histolytica/efectos de los fármacos , Lippia/química , Extractos Vegetales/farmacología , Pterocarpus/química , Catequina/análogos & derivados , Catequina/química , Humanos , Concentración 50 Inhibidora , Pruebas de Sensibilidad Microbiana , Aceites Volátiles/química , Aceites Volátiles/farmacología , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación
6.
Z Naturforsch C J Biosci ; 64(11-12): 831-9, 2009.
Artículo en Inglés | MEDLINE | ID: mdl-20158154

RESUMEN

Phytochemical studies of an ethanolic extract of the aerial parts of Salvia disermas resulted in the isolation of seven known compounds, rosmarinic (1) and caffeic (2) acids, salvigenin (3), luteolin (4), luteolin 7-O-beta-arabinoside (5), luteolin 7-O-beta-glucoside (6), and ocotillol II (7). The initiation stage of carcinogenesis is triggered by activation of procarcinogens by phase I enzymes, such as cytochrome P-450 1A, and oxidative stress that leads to DNA damage. The initiation stage is countered by phase II detoxification enzymes such as glutathione S-transferases (GST), quinine reductase (QR), epoxide hydrolase (mEH) besides conjugation with thiols. We aimed to investigate the cancer chemopreventive and tumour anti-initiating activity of the ethanolic extract of the aerial parts of Salvia disermas and its constituents. The S. disermas extract was a promising inhibitor of CYP1A activity, inducer of GST, QR, and mEH activities, enhancer of thiol content, radical scavenger, and inhibitor of DNA damage. On the other hand, 3 was an enhancer of thiol content and QR activity, while 4 was an inhibitor of CYP1A activity, inducer of QR activity, and radical scavenger of ROO*, and 5 was an inducer of GST activity and inhibitor of DNA damage. The present study indicated that the ethanolic extract of S. disermas and 4 are promising anti-initiating and multipotent blocking agents.


Asunto(s)
Anticarcinógenos/farmacología , Antioxidantes/farmacología , Medicamentos Herbarios Chinos/aislamiento & purificación , Medicamentos Herbarios Chinos/farmacología , Animales , Anticarcinógenos/aislamiento & purificación , Canfanos , Carcinoma Hepatocelular/enzimología , Línea Celular Tumoral , Citocromo P-450 CYP1A1/antagonistas & inhibidores , Inhibidores del Citocromo P-450 CYP1A2 , Daño del ADN/efectos de los fármacos , Inhibidores Enzimáticos/aislamiento & purificación , Inhibidores Enzimáticos/farmacología , Glutatión Transferasa/efectos de los fármacos , Glutatión Transferasa/metabolismo , Ratones , Panax notoginseng , Salvia/química , Salvia miltiorrhiza
7.
J Ethnopharmacol ; 228: 148-155, 2019 Jan 10.
Artículo en Inglés | MEDLINE | ID: mdl-30048730

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: The Vha-Venda people living in rural areas of Limpopo Province of South Africa regularly use traditional plant-based medicines to treat malaria. In our earlier publication, twenty indigenous plant species used to treat malaria or its symptoms by Vha-Venda people were evaluated for antiplasmodial activity. The main objective of the current study was to assess the robustness of NMR-based metabolomics in discriminating classes of secondary compounds that are responsible for the observed antimalarial activity and the isolation of antiplasmodial compounds. MATERIALS AND METHODS: Twenty dichloromethane extracts were reconstituted in CDCl3, subjected to 1H NMR-based metabolomic analysis on a Varian 600 MHz spectrometer and the acquired 1H NMR spectra were then evaluated collectively using multivariate data analysis (MDA). Principal Component Analysis (PCA) and Orthogonal Projections to Latent Structures-Discriminant Analysis (OPLS-DA) were used to 'globally' discern antiplasmodial profiles. A contribution plot was then generated from the OPLS-DA scoring plot in an attempt to determine the classes of compounds that are responsible for the observed grouping. Further phytochemical analyses were conducted on the lipophilic extracts of Tabernaemontana elegans and Vangueria infausta subsp. infausta. These best candidates were fractionated, purified and their isolated compounds identified based on conventional chromatographic and spectroscopic techniques. RESULTS: The PCA did not separate the acquired profiles according to the detected antiplasmodial bioactivity. Application of a supervised OPLS-DA on the 1H NMR profiles resulted in a discrimination pattern that could be correlated to the observed antimalarial bioactivity. A contribution plot generated from the OPLS-DA scoring plot illustrated the classes of compounds responsible for the observed grouping. Prominent peaks were observed in the aromatic, sugar-based/N-containing and aliphatic spectral regions of the contribution plot. Two known indole alkaloids were isolated from T. elegans, and identified as tabernaemontanine (IC50 = 12.0 ±â€¯0.8 µM) and dregamine (IC50 = 62.0 ±â€¯2.4 µM). Friedelin (IC50 = 7.20 ±â€¯0.5 µM) and morindolide (IC50 = 107.1 ±â€¯0.6 µM) were isolated from V. infausta subsp. infausta. This is the first report of the rare iridoid lactone, morindolide's antimalarial activity. While these two compounds have been previously identified, this is the first account of their occurrence in the genus Vangueria. CONCLUSION: The study illustrated the potential of NMR-based metabolomics in discriminating classes of compounds that may be attributed to antiplasmodial activity. Additionally, the study demonstrated the potential of discovering novel antiplasmodial scaffolds from medicinal plants and the rationale for the bioprospecting antimalarial plant species used by Vha-Venda people.


Asunto(s)
Antimaláricos , Metabolómica , Fitoquímicos , Plantas Medicinales , Animales , Antimaláricos/aislamiento & purificación , Antimaláricos/farmacología , Línea Celular , Medicinas Tradicionales Africanas , Fitoquímicos/aislamiento & purificación , Fitoquímicos/farmacología , Plasmodium falciparum/efectos de los fármacos , Espectroscopía de Protones por Resonancia Magnética , Ratas , Sudáfrica
8.
J Nat Prod ; 71(11): 1919-22, 2008 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-18855442

RESUMEN

A new indanone derivative (1) and two new diterpenoids (2 and 3), together with three known flavonoids, have been isolated from an ethanol extract of the leaves of Croton steenkampianus. The structure of 2 was solved by single-crystal X-ray diffraction analysis, whereas those of 1 and 3 were established mainly by 1D and 2D NMR spectroscopic methods. The isolated compounds were tested for their antiplasmodial activity and cytotoxicity. Antiplasmodial assays against chloroquine-susceptible strains (D10 and D6) and the chloroquine-resistant strains (Dd2 and W2) of Plasmodium falciparum showed that compound 2 gave moderate activities at 9.1-15.8 µM, while none of the compounds were cytotoxic against Vero cells.


Asunto(s)
Antimaláricos/aislamiento & purificación , Antimaláricos/farmacología , Croton/química , Diterpenos/aislamiento & purificación , Diterpenos/farmacología , Indanos/aislamiento & purificación , Indanos/farmacología , Plasmodium falciparum/efectos de los fármacos , Animales , Antimaláricos/química , Chlorocebus aethiops , Cloroquina/farmacología , Diterpenos/química , Resistencia a Medicamentos/efectos de los fármacos , Indanos/química , Conformación Molecular , Estructura Molecular , Resonancia Magnética Nuclear Biomolecular , Sudáfrica , Células Vero , Difracción de Rayos X
9.
J Ethnopharmacol ; 119(3): 473-7, 2008 Oct 28.
Artículo en Inglés | MEDLINE | ID: mdl-18672045

RESUMEN

Ethanol extracts of eight plant species used traditionally in South Africa for the treatment of oral diseases were investigated for in vitro antimicrobial activity against oral pathogens namely Actinobacillus actinomycetemcomitans, Actinomyces naeslundii, Actinomyces israelii, Candida albicans, Porphyromonus gingivalis, Privotella intermedia and Streptococcus mutans using the disk diffusion method. Minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) of ethanol extracts were determined against these microorganisms using micro dilution. The cytotoxicity and therapeutic index (TI) of selected active extracts were also determined. Out of eight plants, six (Annona senegalensis, Englerophytum magalismontanum, Dicerocarym senecioides, Euclea divinorum, Euclea natalensis, Solanum panduriforme and Parinari curatellifolia) exhibited MIC values ranging from 25.0 mg/ml to 0.8 mg/ml. Gram negative bacteria were found to be more resistant to the plant extracts than Gram positive bacteria, except for Euclea natalensis which inhibited all three Gram negative bacteria tested in this study. All plant extracts showed moderate cytotoxicity on the Vero cell line. The fifty percent inhibitory concentration (IC(50)) of all plants tested range from 92.3 to 285.1 microg/ml.


Asunto(s)
Antiinfecciosos/farmacología , Boca/microbiología , Plantas Medicinales/química , Animales , Antiinfecciosos/aislamiento & purificación , Antiinfecciosos Locales/farmacología , Supervivencia Celular/efectos de los fármacos , Clorhexidina/farmacología , Chlorocebus aethiops , Caries Dental/microbiología , Gingivitis/microbiología , Humanos , Medicinas Tradicionales Africanas , Pruebas de Sensibilidad Microbiana , Periodontitis/microbiología , Extractos Vegetales/química , Extractos Vegetales/farmacología , Sudáfrica , Células Vero
10.
J Ethnopharmacol ; 119(3): 482-500, 2008 Oct 28.
Artículo en Inglés | MEDLINE | ID: mdl-18805475

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: In South Africa, tuberculosis (TB) caused by Mycobacterium tuberculosis is the most commonly notified disease and the fifth largest cause of mortality, with one in ten cases of TB resistant to treatment in some areas. Many plants are used locally in traditional medicine to treat TB-related symptoms. AIM OF THE STUDY: The aim was to summarize currently available knowledge on South African plants used to treat TB symptoms, and antimycobacterial efficacy of plant-derived extracts and compounds. MATERIALS AND METHODS: The traditional uses of plants for respiratory ailments and TB were collated and tabulated. The antimycobacterial activity tests of extracts and chemical constituents of several of these plants and others using different methods and target organisms were summarized. RESULTS: Almost 180 plants used for TB-related symptoms in South African traditional medicine were documented. About 30% of these have been tested for antimycobacterial efficacy, mostly against fast-growing, non-pathogenic Mycobacterium species. CONCLUSIONS: Many plant species are used in traditional South African medicine to alleviate symptoms of TB, and several interesting leads have originated for further inquiry following in vitro antimycobacterial activity evaluation. However, much work remains to be done on the systematic assessment of anti-TB efficacy of local plants against pathogenic Mycobacterium species, both in vitro and in vivo.


Asunto(s)
Antibacterianos/farmacología , Antituberculosos/farmacología , Infecciones por Mycobacterium/tratamiento farmacológico , Plantas Medicinales/química , Animales , Antibacterianos/química , Antibacterianos/aislamiento & purificación , Antituberculosos/química , Antituberculosos/aislamiento & purificación , Etnobotánica , Humanos , Medicinas Tradicionales Africanas , Mycobacterium/efectos de los fármacos , Infecciones por Mycobacterium/microbiología , Sudáfrica , Tuberculosis/tratamiento farmacológico , Tuberculosis/microbiología
11.
J Ethnopharmacol ; 119(3): 599-603, 2008 Oct 28.
Artículo en Inglés | MEDLINE | ID: mdl-18638534

RESUMEN

AIM OF STUDY: Securidaca longepedunculata is used in the treatment of erectile dysfunction in South Africa. The aim of the study was to isolate and identify the active constituents and to determine their activity in the relaxation of corpus cavernosal smooth muscle. MATERIALS AND METHODS: Bioassay guided isolation of the bioactive compounds using a smooth muscle relaxation bioassay and structural elucidation was carried out using different spectroscopic techniques including 2D NMR. RESULTS: Two new xanthones were isolated; one of them showed potent activity to relax the corpus cavernosal smooth muscle by 97 % in comparison to sildenafil (Viagra) at 1.8 x 10(-5) mg/ml. CONCLUSIONS: S. longepedunculata's xanthones stimulate the relaxation of corpus cavenosum smooth muscle, which supports the traditional use of its root bark.


Asunto(s)
Disfunción Eréctil/tratamiento farmacológico , Fitoterapia , Securidaca/química , Xantonas/farmacología , Animales , Espectroscopía de Resonancia Magnética , Masculino , Medicinas Tradicionales Africanas , Relajación Muscular/efectos de los fármacos , Músculo Liso/efectos de los fármacos , Pene/efectos de los fármacos , Corteza de la Planta/química , Conejos , Sudáfrica , Espectrofotometría Ultravioleta , Xantonas/aislamiento & purificación
12.
J Ethnopharmacol ; 116(1): 194-7, 2008 Feb 28.
Artículo en Inglés | MEDLINE | ID: mdl-18191928

RESUMEN

Spirostachys africana Sond. stem bark is used traditionally for the treatment of diarrhoea and dysentery in Limpopo Province of South Africa. Bioassay-guided fractionation of ethanolic extract from bark of Spirostachys africana led to the isolation of four known compounds, two triterpenoids, compound 1 [d-Friedoolean-14-en-oic acid (3-acetyl aleuritolic acid)] and compound 2 (Lupeol), and two diterpenes, compound 3 [ent-2,6alpha-dihydroxy-norbeyer-1,4,15-trien-3-one (diosphenol 2)] and compound 4 (ent-3beta-hydroxy-beyer-15-ene-2-one). Isolated compounds were tested for antibacterial activity using micro-dilution method. Compound 1, exhibited minimum inhibitory concentration (MIC) of 50 microg/ml against Staphylococcus aureus, Salmonella typhy, Vibrio cholera, Escherichia coli and Shigella dysentery. Compound 2 was not active against all tested microorganisms at 200 microg/ml, which was the highest concentration tested. At this concentration, all four compounds were not active against Shigella sonnei. Cytotoxicity of ethanol crude extracts and isolated compounds from Spirostachys africana was determined using the sodium-2,3-bis-[2-methoxy-4-nitro-5-sulfophenyl]-2H-tetrazolium-5-carboxanilide (XTT) assay on Vero cells. Compounds 2 and 3, isolated from Spirostachys africana, had up to three times higher [50% inhibitory concentration (IC(50) values; 300.9 and 308.9 microg/ml)] than the ethanol crude extracts (102.8 microg/ml) suggesting higher toxicity of the crude extract as compared to these two compounds. In contrast, compounds 1 and 4 were not cytotoxic to Vero cell lines (African green monkey) in vitro at the concentrations tested (IC(50)>400 microg/ml). This is the first report on the antibacterial activity and cytotoxicity of purified compounds from Spirostachys africana.


Asunto(s)
Antibacterianos/farmacología , Euphorbiaceae/química , Medicinas Tradicionales Africanas , Terpenos/farmacología , Animales , Supervivencia Celular/efectos de los fármacos , Chlorocebus aethiops , Células Vero
13.
J Ethnopharmacol ; 119(3): 478-81, 2008 Oct 28.
Artículo en Inglés | MEDLINE | ID: mdl-18809485

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: [corrected The plants selected in this study are used traditionally in the treatment of sexually transmitted diseases and traditional healers interviewed claimed these plants can also help AIDS patients. AIM: To evaluating the in vitro anti-HIV properties of selected plants in various bioassays. MATERIALS AND METHODS: The extracts were evaluated for their inhibition against alpha-glycohydrolase, reverse transcriptase and viral proteins (NF-kappaB and Tat) which play a significant role in the HIV life cycle. RESULTS: Terminalia sericea extract (IC(50)=92mg/ml) exhibited a considerable alpha-glucosidase inhibitory activity which was better than acarbose (IC(50)=131mg/ml) under our assay conditions. In the reverse transcriptase assay, T. sericea also showed good inhibitory activity (IC(50)=43mg/ml), which was higher than that of the reference drug, Adriamycin (IC(50)=100mg/ml). The ethyl acetate extract of Elaeodendron transvaalense exhibited the most potent inhibitory activity in both the NF-kappaB and Tat assays with inhibitory activity of 76% and 75% respectively at a concentration of 15mg/ml. The acetone and chloroform extracts of E. transvaalense and Zanthoxylum davyi also showed good activity in the NF-kappaB and Tat assays.


Asunto(s)
Fármacos Anti-VIH/farmacología , Plantas Medicinales/química , Enfermedades de Transmisión Sexual/tratamiento farmacológico , Bioensayo , Muerte Celular/efectos de los fármacos , Línea Celular , Etnobotánica , Glicósido Hidrolasas/metabolismo , Células HeLa , Humanos , FN-kappa B/antagonistas & inhibidores , Corteza de la Planta/química , Extractos Vegetales/química , Extractos Vegetales/farmacología , Raíces de Plantas/química , Inhibidores de la Transcriptasa Inversa/farmacología , Sudáfrica , Productos del Gen tat del Virus de la Inmunodeficiencia Humana/antagonistas & inhibidores
14.
J Ethnopharmacol ; 120(1): 17-24, 2008 Oct 30.
Artículo en Inglés | MEDLINE | ID: mdl-18718518

RESUMEN

The aim of this study was to evaluate the antimicrobial activity of the methanol extracts from Ficus chlamydocarpa (FCR), Ficus cordata (FCB), mixture of the two plants (FCM), as well as that of the isolated flavonoids Alpinumisoflavone (2), Genistein (3), Laburnetin (4), Luteolin (5) (isolated from FCR), Catechin (7) and Epiafzelechin (8) (isolated from FCB). Mycobacteria, fungi, Gram-positive and Gram-negative bacterial species were tested for their susceptibility to the above samples. The microplate dilution and radiometric respiratory methods were used to determine the susceptibility testing of the samples against Mycobacterium smegmatis and Mycobacterium tuberculosis, respectively. The disc diffusion assay was used to determine the sensitivity of the samples, whilst the micro-dilution method was used for the determination of the minimal inhibition concentration (MIC) and the minimal microbicidal concentration (MMC) against fungi, Gram-positive and Gram-negative bacterial species. All the samples except compound 7 were found to be active to Mycobacterium smegmatis and the MIC ranged from 0.61 to 312.50microg/ml. Compound 4 showed the best activity against Mycobacterium tuberculosis exhibiting an MIC of 4.88microg/ml. The results of the diffusion test indicated that the crude extract from FCB, FCM as well as compounds 5 and 8 were able to prevent the growth of all tested (fungi, Gram-positive and Gram-negative bacteria) organisms. The inhibition effect of the crude extract from Ficus chlamydocarpa was observed on 10 (62.5%) of the 16 tested microorganisms (excluding mycobacteria) whereas that of compounds 4, 2 and 3 was respectively noted on 14 (87.5%), 8 (50.0%) and 7 (39.9%) of the tested microbial species. FCB was found to be more active than FCR on most of the tested organisms. The results provided evidence that the studied plants extract, as well as some of the isolated compounds might be potential sources of new antimicrobial drug.


Asunto(s)
Antiinfecciosos/farmacología , Ficus/química , Flavonoides/farmacología , Extractos Vegetales/farmacología , Antiinfecciosos/aislamiento & purificación , Candida/efectos de los fármacos , Flavonoides/aislamiento & purificación , Bacterias Gramnegativas/efectos de los fármacos , Bacterias Grampositivas/efectos de los fármacos , Pruebas de Sensibilidad Microbiana , Mycobacterium/efectos de los fármacos
15.
J Ethnopharmacol ; 115(3): 494-501, 2008 Feb 12.
Artículo en Inglés | MEDLINE | ID: mdl-18063329

RESUMEN

The aim of this study was to evaluate the antitumor, antioxidant and antimicrobial activities as well as the phytochemical composition and the acute toxicity of the methanolic extracts from the roots (BER), stem bark (BEB), leaves (BEL) and wood (BEW) of Bersama engleriana. The crown gall tumor and DPPH radical scavenging assays were used to detect respectively the antitumoral and oxidant activities. Agar diffusion and liquid dilution were used for antimicrobial tests and the phytochemical assays were conducted according to Harbone methods. The single-dose oral toxicity test was performed in accordance with the OPPTS 870.1100 and OECD 401 guidelines. The phytochemical tests indicated the presence of flavonoids, phenols, triterpenes and anthraquinones in all extracts. Pronounced tumor reducing activity was observed with the extracts from the roots (69.32%) and leaves (65.42%). The DPPH scavenging activity showed that the extract from the leaves was the most active with 93.71% inhibition rate at the 1000 microg/ml. The results of antimicrobial activity showed that all tested extracts were active against all tested microbial species, including Gram-positive, and negative bacteria, the two Candida species and mycobacteria. The MIC values obtained ranged from 9.76 to 156.25 microg/ml. Under the conditions of the studied toxicity, all extracts were found to be non-toxic. The overall results of this study indicates that the extracts from the roots, stem bark, leaves and wood have interesting antioxidant properties and represent a potential source of medicine for the treatment of infectious diseases and cancer.


Asunto(s)
Antiinfecciosos/farmacología , Antineoplásicos Fitogénicos/farmacología , Antioxidantes/farmacología , Extractos Vegetales/farmacología , Animales , Antiinfecciosos/aislamiento & purificación , Antineoplásicos Fitogénicos/aislamiento & purificación , Antioxidantes/aislamiento & purificación , Camerún , Candida/efectos de los fármacos , Ensayos de Selección de Medicamentos Antitumorales , Radicales Libres/metabolismo , Bacterias Gramnegativas/efectos de los fármacos , Bacterias Grampositivas/efectos de los fármacos , Pruebas de Sensibilidad Microbiana , Mycobacterium/efectos de los fármacos , Extractos Vegetales/química , Extractos Vegetales/toxicidad , Ratas , Ratas Wistar , Pruebas de Toxicidad Aguda
16.
J Ethnopharmacol ; 116(3): 483-9, 2008 Mar 28.
Artículo en Inglés | MEDLINE | ID: mdl-18280679

RESUMEN

The aim of this study was to evaluate the antimicrobial activity of the crude extract of the twigs of Dorstenia barteri (DBT) as well as that of four of the five flavonoids isolated from this extract. Gram-positive bacteria (six species), Gram-negative bacteria (12 species) and fungi (four species) were used. The agar disc diffusion test was used to determine the sensitivity of the tested samples while the well micro-dilution was used to determine the minimal inhibition concentrations (MIC) and the minimal microbicidal concentration (MMC) of the active samples. The results of the disc diffusion assay showed that DBT, isobavachalcone (1), and kanzonol C (4) prevented the growth of all the 22 tested microbial species. Other compounds showed selective activity. The inhibitory activity of the most active compounds namely compounds 1 and 4 was noted on 86.4% of the tested microorganisms and that of 4-hydroxylonchocarpin (3) was observed on 72.7%. This lowest MIC value of 19.06microg/ml was observed with the crude extract on seven microorganisms namely Citrobacter freundii, Enterobacter aerogens, Proteus mirabilis, Proteus vulgaris, Bacillus megaterium, Bacillus stearothermophilus and Candida albicans. For the tested compounds, the lowest MIC value of 0.3microg/ml (on six of the 22 organisms tested) was obtained only with compound 1, which appeared as the most active compound. This lowest MIC value (0.3microg/ml) is about 4-fold lower than that of the RA, indicating the powerful and very interesting antimicrobial potential of isobavachalcone (1). The antimicrobial activities of DBT, as well as that of compounds 1, 3, 4, amentoflavone (5) are being reported for the first time. The overall results provide promising baseline information for the potential use of the crude extracts from DBT as well as some of the isolated compounds in the treatment of bacterial and fungal infections.


Asunto(s)
Antiinfecciosos/farmacología , Bacterias/efectos de los fármacos , Flavonoides/farmacología , Hongos Mitospóricos/efectos de los fármacos , Moraceae/química , Extractos Vegetales/farmacología , Antiinfecciosos/química , Flavonoides/química , Pruebas de Sensibilidad Microbiana , Extractos Vegetales/química , Tallos de la Planta/química
17.
Bioorg Med Chem ; 15(24): 7638-46, 2007 Dec 15.
Artículo en Inglés | MEDLINE | ID: mdl-17888665

RESUMEN

The naphthoquinone 7-methyljuglone (5-hydroxy-7-methyl-1,4-naphthoquinone) has previously been isolated and identified as an active component of root extracts of Euclea natalensis which displays antitubercular activity. Herein, a series of synthetic and plant-derived naphthoquinone derivates of the 7-methyljuglone scaffold have been prepared and evaluated for antibacterial activity against Mycobacterium tuberculosis. Several of these compounds have been shown to operate as subversive substrates with mycothiol disulfide reductase. The absence of a direct correlation between antitubercular activity and subversive substrate efficiency with mycothiol disulfide reductase, might be a consequence of their non-specific reactivity with multiple biological targets (e.g. other disulfide reductases).


Asunto(s)
Antibacterianos/síntesis química , Ebenaceae/química , Mycobacterium tuberculosis/efectos de los fármacos , NADH NADPH Oxidorreductasas/química , Naftoquinonas/química , Raíces de Plantas/química , Antibacterianos/química , Antibacterianos/farmacología , Relación Dosis-Respuesta a Droga , Pruebas de Sensibilidad Microbiana , Estructura Molecular , Mycobacterium tuberculosis/enzimología , NADH NADPH Oxidorreductasas/metabolismo , Naftoquinonas/farmacología
18.
J Ethnopharmacol ; 114(1): 54-60, 2007 Oct 08.
Artículo en Inglés | MEDLINE | ID: mdl-17766070

RESUMEN

The antimicrobial activity of the methanolic extract from the stem bark of Irvingia gabonensis (IGM), fractions and compounds isolated from IGM [3-friedelanone (1), betulinic acid (2), oleanolic acid (3), 3,3',4'-tri-O-methylellagic acid (4), 3,4-di-O-methylellagic acid (5) and hardwickiic acid (6)] was evaluated against Gram-positive bacteria (6 species), Gram-negative bacteria (13 species) and three Candida species using dilution methods for the determination of the minimal inhibition concentration (MIC) and the minimal microbicidal concentration (MMC). From the obtained results, IGM prevented the growth of all the species of microorganisms tested at a concentration limit of 312.50 microg/ml. Compounds 4-6 also inhibited the growth of all the tested microbial species while compounds 1-3 showed selective activities. The lowest MIC values (78.12 microg/ml) were obtained with IGM on 13 of the 22 microorganisms tested. The corresponding value of 1.22 microg/ml (4.26 microM) for compounds was recorded with compound 6 on Neisseria gonorrhoeae. The obtained results confirmed the use of Irvingia gabonensis in the treatment of bacterial and fungal infections.


Asunto(s)
Antiinfecciosos/farmacología , Celulosa/química , Extractos Vegetales/farmacología , Antiinfecciosos/aislamiento & purificación , Camerún , Candida/efectos de los fármacos , Diterpenos/aislamiento & purificación , Diterpenos/farmacología , Ácido Elágico/análogos & derivados , Ácido Elágico/aislamiento & purificación , Ácido Elágico/farmacología , Bacterias Gramnegativas/efectos de los fármacos , Bacterias Grampositivas/efectos de los fármacos , Pruebas de Sensibilidad Microbiana , Ácido Oleanólico/aislamiento & purificación , Ácido Oleanólico/farmacología , Triterpenos Pentacíclicos , Corteza de la Planta , Extractos Vegetales/aislamiento & purificación , Triterpenos/aislamiento & purificación , Triterpenos/farmacología , Ácido Betulínico
19.
J Ethnopharmacol ; 105(1-2): 84-8, 2006 Apr 21.
Artículo en Inglés | MEDLINE | ID: mdl-16309865

RESUMEN

Chloroform and ethanol extracts of root bark of Securidaca longepedunculata, Wrightia natalensis and Rhoicissus tridentata were investigated for their in vitro activity on the contraction of corpus cavernosal smooth muscle of white New Zealand rabbits. Some of the extracts of these plants relaxed the corpus cavernosal smooth muscle at low concentrations. The highest activity was obtained from Securidaca longepedunculata chloroform extracts at a concentration of 13.0 mg/ml, which induced 66.6% relaxation. Viagra was used as a positive control in this study. Extracts of Securidaca longepedunculata added to human spermatozoa affected certain sperm parameters negatively at 6.5 mg/ml and higher whilst there was no effect at 1.0 mg/ml.


Asunto(s)
Disfunción Eréctil/terapia , Plantas Medicinales , Espermatozoides/fisiología , Animales , Humanos , Técnicas In Vitro , Masculino , Relajación Muscular , Músculo Liso/fisiopatología , Conejos
20.
Fitoterapia ; 77(3): 230-2, 2006 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-16529879

RESUMEN

Bioassay guided fractionation of the acetonic extract of Helichrysum melanacme using human Influenza virus type A and a drug-sensitive strain of Mycobacterium tuberculosis in vitro resulted in the isolation of 2 4',6'-trihydroxy-3'-prenylchalcone (1) and 4',6',5''-trihydroxy-6'',6''-dimethyldihydropyrano[2'',3''-2',3'] chalcone (2) as active constituents. 3-O-methylquercetin and quercetin were also isolated but were inactive against the microorganisms tested in this study.


Asunto(s)
Antituberculosos/farmacología , Antivirales/farmacología , Chalconas/farmacología , Helichrysum/química , Virus de la Influenza A/efectos de los fármacos , Mycobacterium tuberculosis/efectos de los fármacos , Piranos/farmacología , Acetona/química , Chalconas/química , Chalconas/aislamiento & purificación , Pruebas de Sensibilidad Microbiana , Brotes de la Planta/química , Piranos/química , Piranos/aislamiento & purificación
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