In vitro activity of Sorghum bicolor extracts, 3-deoxyanthocyanidins, against Toxoplasma gondii (original) (raw)
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Molecules, 2015
Rhododendron formosanum is an endemic species distributed in the central mountains of Taiwan. In this study, the biological activities of major procyanidins isolated from the leaf extract of R. formosanum were investigated. Four compounds, including two procyanidin dimers, procyanidin A1 (1) and B3 (2), and two procyanidin trimmers, procyanidin C4 (4) and cinnamtannin D1 (5), were isolated and identified on the basis of spectroscopic data. The structure of a new procyanidin dimer, rhodonidin A (3), was elucidated by 2D-NMR, CD spectrum and MS. The procyanidin trimmers and rhodonidin A are reported for the first time in Ericaceae. The biological activities of these procyanidins were evaluated using anti-bacterial and anti-oxidative assays. Only the new compound 3 demonstrated strong anti-bacterial activity against Staphylococcus aureus at an MIC value of 4 μg/mL. All compounds showed pronounced antioxidant activities and the activities are enhanced as the amount of OH groups in procyanidins increased. In conclusion, the pleiotropic effects of procyanidins isolated from the leaves of R. formosanum can be a source of promising compounds for the development of future pharmacological applications.
Parasitology Research, 2017
Toxoplasma gondii is a ubiquitous intracellular zoonotic parasite estimated to affect about 30-90% of the world's human population. The most affected are immunocompromised individuals such as HIV-AIDS and cancer patients, organ and tissue transplant recipients, and congenitally infected children. No effective and safe drugs and vaccines are available against all forms of the parasite. We report here the antagonistic and indifferent activity of the combination of five different formulations of pure synthetic 3-deoxyanthocyaninidin (3-DA) chloride compounds against T. gondii tachyzoites and the synergistic and additive interaction against a human foreskin fibroblast (HFF) cell line in vitro using fluorescence microscopy, trypan blue assay, and fractional inhibitory concentration index. The individual and the combined pure 3-DA compounds were observed to have effective inhibition against T. gondii parasites with less cytotoxic effect in a ratio of 1:1. The IC 50 values for parasite inhibition ranged from 1.88 μg/mL (1. 5 1-2. 3 2 μ g / m L) f o r l u t e o l i n i n d i n p l u s 7methoxyapigeninindin (LU/7-MAP) and 2.23 μg/mL (1.66-2.97 μg/mL) for apigeninindin plus 7-methoxyapigeninindin (AP/7-MAP) combinations at 95% confidence interval (CI) after 48 h of culture. We found LU/7-MAP to be antagonistic and AP/7-MAP to be indifferent in interaction against T. gondii growth. Both individual and combination 3-DA compounds not only depicted very strong inhibitory activity against T. gondii, but also had synergistic and additive cytotoxic effects against HFF cells. These synthetic 3-DAs have potential as antiparasitic agents for the treatment of human toxoplasmosis.
Phytochemistry, 2010
Phytochemical investigation of the ethyl acetate fraction of the methanol extract of the leaves of Ixora coccinea led to the isolation and identification of an A-type trimeric proanthocyanidin epicatechin-(2b ? O ? 7, 4b ? 8)-epicatechin-(5 ? O ? 2b, 6 ? 4b)-epicatechin named ixoratannin A-2 along with seven known compounds, epicatechin, procyanidin A2, cinnamtannin B-1, and four flavon-3-ol rhamnosides viz: kaempferol-7-O-a-L-rhamnnoside, kaempferol-3-O-a-L-rhamnoside, quercetin-3-O-a-Lrhamnopyranoside, and kaempferol-3,7-O-a-L-dirhamnoside. The structures were elucidated by the application of IR, UV, MS, 1D-, and 2D-NMR spectroscopic analyses and by comparison with literature data. Antioxidant evaluation of isolated compounds revealed that ixoratannin A-2 and cinnamtannin B-1 were the most active compounds in DPPH, inhibition of lipid peroxidation and nitric oxide radical scavenging assays. Antibacterial activities were assessed by means of agar-diffusion assays using Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa and Bacillus subtilis. All tested compounds inhibited the growth of B. subtilis, while only epicatechin and quercetin-3-O-a-L-rhamnopyranoside inhibited the growth of E. coli.
Molecules
It has now been proven that many pathogens that cause infections and inflammation gradually mutate and become resistant to antibiotics. Chemically synthesized drugs treating inflammation most often only affect symptoms, but side effects could lead to the failure of human organs’ functionality. On the other hand, plant-derived natural compounds have a long-term healing effect. It was shown that sea buckthorn (SBT) twigs are a rich source of biologically active compounds, including oligomeric proanthocyanidins (PACs). This study aimed to assess the anti-pathogenic and anti-inflammatory activity of water/ethanol extracts and PACs obtained from the lignocellulosic biomass of eight SBT cultivars. The anti-pathogenic activity of extracts and PACs was studied against pathogenic bacteria Pseudomonas aeruginosa, Staphylococcus aureus, Escherichia coli, Bacillus cereus and fungus Candida albicans in 96-well plates by the two-fold serial broth microdilution method. The anti-bacterial activity ...
Antioxidants, 2017
In a previous study, the detailed low-molecular weight polyphenolic profile of the different plant parts (leaves, stem, bark and wood) of Uncaria tomentosa was reported, the leaves being the plant part with the highest phenolic content and presenting the most heterogenous proanthocyanidin composition. Further, cytotoxicity of leaves extracts in two cancer cell lines was also found to be higher than in the remaining parts of the plant. In the present study, fractioning of U. tomentosa leaves polyphenolic extracts was performed using Diaion ® HP-20 resin and a detailed characterization and quantification of fractions (n = 5) was achieved using advanced analytical techniques such as Ultra-Performance Liquid Chromatography coupled with Electrospray Ionization and Triple Quadrupole (TQD) Tandem Mass Spectrometry (UPLC/TQ-ESI-MS) and 13 C-NMR. Oxygen Radical Absorbance Capacity (ORAC) and cytotoxicity on gastric adenocarcinoma AGS and colon adenocarcinoma SW20 cell lines were also determined in the different fractions. Results showed selective distribution of 32 non-flavonoid and flavonoid phenolics among the different fractions. ORAC varied between 3.2 and 11.8 µmol TE/mg in the different fractions, whereas IC 50 of cytotoxicity on gastric adenocarcinoma AGS and colon adenocarcinoma SW20 cell lines best values were between 71.4 and 75.6 µg/mL. Fractions rich in proanthocyanidins also showed the highest bioactivity. In fact, significant positive correlation was found between total proanthocyanidins (TP) quantified by UPLC-DAD and ORAC (R 2 = 0.970), whereas significant negative correlation was found between TP and cytotoxicity towards AGS (R 2 = 0.820) and SW620 (R 2 = 0.843) adenocarcinoma cell lines. Among proanthocyanidins, propelargonidin dimers were of particular interest, showing significant correlation with cytotoxic selectivity on both gastric AGS (R 2 = 0.848) and colon SW620 (R 2 = 0.883) adenocarcinoma cell lines. These results show further evidence of the bioactivity of U. tomentosa proanthocyanidin extracts and their potential health effects.
The aim of this work was to evaluate the antimicrobial activity of synthesized heterocyclic compound (SHCs) like as (furan derivate(Fd) (1-furan-2-yl-thioxo-propenon) , thiophene derivate (Thd) (2-cyano-2-sc-thiophene-2-yl-[1,2]dithiol-3ylidene thioactamide)) and herbal extracts (HEs) like as (Cocklebur and Colocynth) against plant pathogens: three fungal strains (Fusarium oxysporum , Rhizopus stolonifer and Aspergillius niger), two bacteria strains (Pseudomonas solanacearum and Erwinia cartovora) and one actinomycetes strains (Streptomyces scabies). The synthesized heterocyclic compounds were subjected to antimicrobial activity against various plant pathogenic microorganisms. Investigation of antimicrobial activity of the derivatives demonstrated the ability to inhibit Gram-negative microorganisms with zone of inhibition ranging from 10-14 mm, fungal inhibition zone ranging from 9-22 mm. All extracts (synthesizes and herbal) had strong antimicrobial activity against the evaluated p...
Antimicrobial Agents and Chemotherapy, 2006
Trypanosomiasis and leishmaniasis are important parasitic diseases affecting millions of people in Africa, Asia, and South America. In a previous study, we identified several flavonoid glycosides as antiprotozoal principles from a Turkish plant. Here we surveyed a large set of flavonoid aglycones and glycosides, as well as a panel of other related compounds of phenolic and phenylpropanoid nature, for their in vitro activities against Trypanosoma brucei rhodesiense, Trypanosoma cruzi, and Leishmania donovani. The cytotoxicities of more than 100 compounds for mammalian L6 cells were also assessed and compared to their antiparasitic activities. Several compounds were investigated in vivo for their antileishmanial and antitrypanosomal efficacies in mouse models. Overall, the best in vitro trypanocidal activity for T. brucei rhodesiense was exerted by 7,8dihydroxyflavone (50% inhibitory concentration [IC 50 ], 68 ng/ml), followed by 3-hydroxyflavone, rhamnetin, and 7,8,3,4-tetrahydroxyflavone (IC 50 s, 0.5 g/ml) and catechol (IC 50 , 0.8 g/ml). The activity against T. cruzi was moderate, and only chrysin dimethylether and 3-hydroxydaidzein had IC 50 s less than 5.0 g/ml. The majority of the metabolites tested possessed remarkable leishmanicidal potential. Fisetin, 3-hydroxyflavone, luteolin, and quercetin were the most potent, giving IC 50 s of 0.6, 0.7, 0.8, and 1.0 g/ml, respectively. 7,8-Dihydroxyflavone and quercetin appeared to ameliorate parasitic infections in mouse models. Generally, the test compounds lacked cytotoxicity in vitro and in vivo. By screening a large number of flavonoids and analogues, we were able to establish some general trends with respect to the structure-activity relationship, but it was not possible to draw clear and detailed quantitative structure-activity relationships for any of the bioactivities by two different approaches. However, our results can help in directing the rational design of 7,8-dihydroxyflavone and quercetin derivatives as potent and effective antiprotozoal agents.
Phytochemistry 65 (2004) 2987–2994
Infection of leaves of tea (Camellia sinensis (Kuntze) L, cv TRI 2025) which was susceptible to blister blight (Exobasidium vexans Massee), resulted in a shift of the proanthocyanidin stereochemistry away from 2,3-trans (e.g. catechin and gallocatechin) and towards 2,3-cis (e.g. epicatechin and epigallocatechin). Infection also resulted in increased gallic acid esterification of the initiating subunits of proanthocyanidins. This was shown by both mass spectroscopy and phloroglucinolysis.
Control of Toxigenic Fungi and Mycotoxins with Phytochemicals: Potentials and Challenges
InTech eBooks, 2013
Control of Toxigenic Fungi and Mycotoxins with Phytochemicals: Potentials and Challenges 183 Antifungal action of plant extracts has great potential as they are easy to prepare and apply. Further, these are safe and effective in view of their systemic action and lack residual effect, easily biodegradable and exhibit stimulating effect on plant metabolism. Also, large number of earlier workers has reported antifungal properties of several plant species (Naganawa et al., 1996; Kubo et al., 1995). Efficacy of some plant phytochemicals against mycotoxin producing fungi suggests its possible use in minimizing the risk of mycotoxins as well as fungicides exposure. Varieties of secondary metabolites in plants are tannins, terpenoids, alkaloids, and flavonoids, which have been found in vitro to have fungitoxic properties (Table 1). Common name Scientific name Compound Class Activity Apple Malus sylvestris Phloretin Flavonoid derivative General a Betel pepper Piper betel Catechols, eugenol Essential oils General Bacteria, fungi Ceylon cinnamon Cinnamomum verum Essential oils, others Terpenoids, tannins General Garlic Allium sativum Allicin, ajoene Sulfoxide General Grapefruit peel Citrus paradise Terpenoid Fungi Green tea Camellia sinensis Catechin Flavonoid General Lantana Lantana camara 6,7dimethylesculetin alkaloid General Mesquite Prosopis juliflora Phenethylamine alkaloid General Olive oil Olea europaea Hexanal Aldehyde General Orange peel Citrus sinensis d-limonene Terpenoid Fungi Peppermint Mentha piperita Menthol Terpenoid General Periwinkle Vinca minor Reserpine Alkaloid General Potato Solanum tuberosum Solanine Bacteria, fungi Snakeplant Rivea corymbosa