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At least 253 records · Page 14Linked to original sources
PubMed2007

Simultaneous quantification of flavonoids and triterpenoids in licorice using HPLC.

Numerous bioactive compounds are present in licorice (Glycyrrhizae Radix), including flavonoids and triterpenoids. In this study, a reversed-phase high-performance liquid chromatography (HPLC) method for simultaneous quantification of three flavonoids (liquiritin, liquiritigenin and isoliquiritigenin) and four triterpenoids (glycyrrhizin, 18alpha-glycyrrhetinic acid, 18beta-glycyrrhetinic acid and 18beta-glycyrrhetinic acid methyl ester) from licorice was developed, and further, to quantify these 7 compounds from 20 different licorice samples. Specifically, the reverse-phase HPLC was performed with a gradient mobile phase composed of 25 mM phosphate buffer (pH 2.5)-acetonitrile featuring gradient elution steps as follows: 0 min, 100:0; 10 min, 80:20; 50 min, 70:30; 73 min, 50:50; 110 min, 50:50; 125 min, 20:80; 140 min, 20:80, and peaks were detected at 254 nm. By using our technique, a rather good specificity was obtained regarding to the separation of these seven compounds. The regression coefficient for the linear equations for the seven compounds lay between 0.9978 and 0.9992. The limits of detection and quantification lay in the range of 0.044-0.084 and 0.13-0.25 microg/ml, respectively. The relative recovery rates for the seven compounds lay between 96.63+/-2.43 and 103.55+/-2.77%. Coefficient variation for intra-day and inter-day precisions lay in the range of 0.20-1.84 and 0.28-1.86%, respectively. Based upon our validation results, this analytical technique is a convenient method to simultaneous quantify numerous bioactive compounds derived from licorice, featuring good quantification parameters, accuracy and precision.

Chromatography, High Pressure Liquid↗
PubMed2005

Inhibition of Naja naja venom hyaluronidase by plant-derived bioactive components and polysaccharides.

The inhibitory effect of several bioactive compounds on the activity of hyaluronidase enzyme purified from Naja naja venom was investigated in vitro. Compounds were found to inhibit the hyaluronidase activity dose dependently. Among glycosaminoglycans, heparin, heparan sulfate, and dermatan sulfate showed maximum inhibition compared to chondroitin sulfates. Different molecular forms of chitosan inhibit the enzyme, and inhibition appears to depend on the chain length. In addition, plant-derived bioactive compounds also inhibited the activity of hyaluronidase dose dependently. Among those tested, aristolochic acid, indomethacin, quercetin, curcumin, tannic acid, and flavone exhibited inhibition, with aristolochic acid and quercetin completely inhibiting the enzyme activity. It is concluded that the inhibitors of hyaluronidase could be used as potent first aid agents in snakebite therapy. Furthermore, these inhibitors not only reduce the local tissue damage but also retard the easy diffusion of systemic toxins and hence increase survival time.

Alkaloids↗
PubMed2003

Angiotherapeutics from natural products: from bench to clinics?

Angiogenesis offers an enormous potentials for therapeutic intervention of many disorders afflicting mankind at present. With the identification of the major molecular players involved in the sequence of events leading to the formation of new blood vessels from pre-existing capillaries, inhibition or induction of the process may now be regulated. Bioactive compounds from natural sources may be used as regulatory agents. Inhibition of angiogenesis can control diseases characterized with excessive blood vessel growth like cancer, arthritis, psoriasis and diabetes retinopathy. Stimulation of angiogenesis would be favorable in the treatment of ischemic disorders and tissue engineering. An increasing number of bioactive compounds from natural sources and whose chemical structures have already been elucidated are reported as either potential inhibitors or inducers of angiogenesis. Drug development from natural products is a fast-emerging field that needs to be supported to provide people with more readily available and affordable healthcare.

Angiogenesis Inducing Agents↗
PubMed2025

Biosynthesis and regulatory mechanism of tanshinones and phenolic acids in Salvia miltiorrhiza.

Salvia miltiorrhiza, a perennial plant of the genus Salvia in the family Lamiaceae, is one of the most important traditional Chinese medicinal herbs, renowned for its significant economic and medicinal value. Its application in China dates back to 200 BC, where it has been utilized clinically either as a monotherapy or in combination with other herbal medicines for treating cardiovascular and cerebrovascular diseases, as well as various other ailments. The bioactive constituents of S. miltiorrhiza primarily include lipophilic tanshinones and hydrophilic phenolic acids. Over the past decades, the biosynthetic pathways of tanshinones and phenolic acids have been elucidated. Coupled with the sequencing of its genome, substantial progress has been made in deciphering the biosynthesis and regulatory mechanisms of bioactive compounds in S. miltiorrhiza, including tanshinones, phenolic acids, flavonoids, and prenylated quinones. This review summarizes recent advances in the regulatory mechanisms underlying the biosynthesis of phenolic acids and tanshinones in S. miltiorrhiza, focusing on transcriptional regulation, post-translational modifications, and epigenetic regulation. These insights provide a foundation for enhancing the production of bioactive compounds through biotechnological approaches and advancing pharmacological applications.

Salvia miltiorrhiza↗
PubMed2002

Characterization of synthetic adsorbents with fine particle sizes for preparative-scale chromatographic separation.

Synthetic adsorbents with fine particle sizes (15-30 microm) were manufactured. These adsorbents are made of poly(styrenedivinylbenzene) and polymethacrylate, and have the same chemical structure as analytical- (5-10 microm) or industrial- (200-600 microm) grade synthetic adsorbents. Both of them have very similar porous structure to those of analytical or industrial sizes, so that they can adsorb compounds of various molecular masses. Chromatographic separation characteristics of newly manufactured fine-particle grades of synthetic adsorbents were evaluated and compared to those of analytical or industrial adsorbents. Reasonable dependency of separation performance on particle size of synthetic adsorbents was obtained. Hydraulic properties of fine-grade adsorbents had also been measured in view of column operations. Furthermore, scalability and applicability of these adsorbents for preparative-scale chromatographic separation of bioactive compounds was evaluated. Separation of soybean isoflavones and tea catechin derivatives had revealed that fine-grade synthetic adsorbents could be well applied with scalability under the same elution conditions used for analytical use. Scalability up to a 22400-fold loading amount was achieved from a small column packed with analytical-grade adsorbent used for method development to a scale-up preparative column packed with fine-grade adsorbent used for preparative purification. These results showed the usefulness of the fine-grade synthetic adsorbents for more precise purification of bioactive compounds, including pharmaceuticals and functional food additives with higher recovery.

Adsorption↗
PubMed2005

Breeding and biotechnology for improving berry nutritional quality.

Breeding and biotechnological approaches are currently used to increase the content of specific bioactive components of plants, but the manipulation of plant metabolism is still not easy to address. There is an increasing awareness that multiple genetic and environmental factors affect production and accumulation of bioactive compounds, but these factors are rarely taken into account when fruit is marketed. Rigorous and unprejudiced evaluation of scientific evidence requires a defined set of criteria and methods of evaluation, particularly when breeding and biotech programs are aimed of producing new varieties with improved nutritional values combined with high plant production efficiency and fruit quality. In order to develop new genotypes and commercial cultivars the availability of new sources of Quality Attributes (QA) and Nutritional Attributes (NA) should be explored. In the strawberry, wild species such as F. virginiana glauca and F. vesca are good sources of bioactive compounds, but in raspberries the introduction of the wild germplasm (R. parvifolium) did not improve the nutritional quality of fruit. The methods available for detecting fruit TAC, combined with TPH and other quality parameters such as sugars, total acidity and fruit color, can be proposed as excellent tools for developing a fast and reliable program for screening large breeding populations for high nutritional quality genotypes. Furthermore, NA can represent a useful tool to facilitate analysis of "substantial equivalence" of transgenic and control derived fruit.

Antioxidants↗
PubMed2004

Clinically approved heterocyclics act on a mitochondrial target and reduce stroke-induced pathology.

Substantial evidence indicates that mitochondria are a major checkpoint in several pathways leading to neuronal cell death, but discerning critical propagation stages from downstream consequences has been difficult. The mitochondrial permeability transition (mPT) may be critical in stroke-related injury. To address this hypothesis, identify potential therapeutics, and screen for new uses for established drugs with known toxicity, 1,040 FDA-approved drugs and other bioactive compounds were tested as potential mPT inhibitors. We report the identification of 28 structurally related drugs, including tricyclic antidepressants and antipsychotics, capable of delaying the mPT. Clinically achievable doses of one drug in this general structural class that inhibits mPT, promethazine, were protective in both in vitro and mouse models of stroke. Specifically, promethazine protected primary neuronal cultures subjected to oxygen-glucose deprivation and reduced infarct size and neurological impairment in mice subjected to middle cerebral artery occlusion/reperfusion. These results, in conjunction with new insights provided to older studies, (a) suggest a class of safe, tolerable drugs for stroke and neurodegeneration; (b) provide new tools for understanding mitochondrial roles in neuronal cell death; (c) demonstrate the clinical/experimental value of screening collections of bioactive compounds enriched in clinically available agents; and (d) provide discovery-based evidence that mPT is an essential, causative event in stroke-related injury.

Animals↗
PubMed2003

Cultivation of primmorphs from the marine sponge Suberites domuncula: morphogenetic potential of silicon and iron.

Marine demosponges (phylum Porifera) are rich sources for potent bioactive compounds. With the establishment of the primmorph system from sponges, especially from Suberites domuncula, the technology to cultivate sponge cells in vitro improved considerably. This progress was possible after the elucidation that sponges are provided with characteristic metazoan cell adhesion receptors and extracellular matrix molecules which allow their cells a positioning in a complex organization pattern. This review summarizes recent data on the cultivation of sponges in aquaria and--with main emphasis--of primmorphs in vitro. It is outlined that silicon and Fe(+++) contribute substantially to the formation of larger primmorphs (size of 10 mm) as well as of a canal system in primmorphs; canals are probably required for an improved oxygen and food supply. We conclude that the primmorph system will facilitate a sustainable use of sponges in the production of bioactive compounds; it may furthermore allow new and hitherto not feasible insights into basic questions on the origin of Metazoa.

Animals↗
PubMed2007

Expression of plant flavor genes in Lactococcus lactis.

Lactic acid bacteria, such as Lactococcus lactis, are attractive hosts for the production of plant-bioactive compounds because of their food grade status, efficient expression, and metabolic engineering tools. Two genes from strawberry (Fragaria x ananassa), encoding an alcohol acyltransferase (SAAT) and a linalool/nerolidol synthase (FaNES), were cloned in L. lactis and actively expressed using the nisin-induced expression system. The specific activity of SAAT could be improved threefold (up to 564 pmol octyl acetate h-1 mg protein-1) by increasing the concentration of tRNA1Arg, which is a rare tRNA molecule in L. lactis. Fermentation tests with GM17 medium and milk with recombinant L. lactis strains expressing SAAT or FaNES resulted in the production of octyl acetate (1.9 microM) and linalool (85 nM) to levels above their odor thresholds in water. The results illustrate the potential of the application of L. lactis as a food grade expression platform for the recombinant production of proteins and bioactive compounds from plants.

Acyltransferases↗
PubMed2005

A microfluidic-based enzymatic assay for bioactivity screening combined with capillary liquid chromatography and mass spectrometry.

The design and implementation of a continuous-flow microfluidic assay for the screening of (complex) mixtures for bioactive compounds is described. The microfluidic chip featured two microreactors (1.6 and 2.4 microL) in which an enzyme inhibition and a substrate conversion reaction were performed, respectively. Enzyme inhibition was detected by continuously monitoring the products formed in the enzyme-substrate reaction by electrospray ionization mass spectrometry (ESI-MS). In order to enable the screening of mixtures of compounds, the chip-based assay was coupled on-line to capillary reversed-phase high-performance liquid chromatography (HPLC) with the HPLC column being operated either in isocratic or gradient elution mode. In order to improve the detection limits of the current method, sample preconcentration based on a micro on-line solid-phase extraction column was employed. The use of electrospray MS allowed the simultaneous detection of chemical (MS spectra) and biological parameters (enzyme inhibition) of ligands eluting from the HPLC column. The present system was optimized and validated using the protease cathepsin B as enzyme of choice. Inhibition of cathepsin B is detected by monitoring three product traces, obtained by cleavage of the substrate. The two microreactors provided 32 and 36 s reaction time, respectively, which resulted in sufficient assay dynamics to enable the screening of bioactive compounds. The total flow rate was 4 microL min-1, which a 25-fold decrease was compared with a macro-scale system described earlier. Detection limits of 0.17-2.6 micromol L-1 were obtained for the screening of inhibitors, which is comparable to either microtiter plate assays or continuous-flow assays described in the literature.

Cathepsin B↗
PubMed2006

The effect of short-term lyophilized beer consumption on established hypertension in rats.

Effects of short-term lyophilized beer (LB) consumption on normotensive (WKY) and hypertensive (SHR) rats are reported. It was found that LB contains high quantities of bioactive compounds and has a high antioxidant potential. The WKY and SHR rats were divided into four groups of 8, two experimental and two controls, which were named LBWKY and LBSHR and ControlWKY and ControlSHR, respectively. LB was given to the rats of the LBWKY and LBSHR groups intragastrically at a dose of 2.72 g/kg in a volume of 10 ml/kg for 10 days. The rats of the control groups received saline solution. The following indices were determined: body weight gain, heart rate, systolic blood pressure, using a tail cuff method and GABA accumulation in the hypothalamus and the pons-medulla as measured by GABA-T inhibition. It was found that the treatment of rats with LB had no effect on the blood pressure and heart rate values. In both rat strains, LB decreased GABA accumulation in the hypothalamus and the pons-medulla. A significant reduction of body weight gain was observed in both LB-treated groups when compared with the corresponding controls. In conclusion, LB contains high quantities of bioactive compounds and possesses a high antioxidant potential. Diet supplemented with LB causes significant reduction of the central GABAergic activity in WKY and SHR rats without any effect on cardiovascular function. In addition, in both animal strains there was an apparent inverse association between LB intake and body weight gains.

Animals↗
PubMed2026

Assessment the Effects of Roasted and Non-Roasted Coffee Extracts on Colon Cancer Cells.

Coffee extracts contain numerous bioactive compounds. Given the dietary link between coffee consumption and colorectal cancer, this study compared the effects of roasted and green (unroasted) coffee extracts on human colorectal cancer cells (HCT116) and non-cancerous fibroblasts (BJ-5ta) to evaluate how processing influences proliferation and molecular signaling. Real-time cell analysis (RTCA), qRT-PCR, and label-free quantitative proteomic analysis were performed to assess cellular responses. MTS and RTCA showed that in BJ-5Ta fibroblasts, coffee extracts increased proliferation in the order CNR < CAR < CAU < CNU, whereas the trend was reversed in HCT116 cancer cells. Proteomic analysis revealed that in BJ-5Ta cells, unroasted coffee extract caused downregulation of the ribosome pathway, and natural coffee extract caused downregulation of the gap junction pathway, indicating reduced protein synthesis and cell-cell communication as a potential stress-adaptive response. In contrast, in HCT116 cells, unroasted coffee extract upregulated the ribosome pathway. Also, natural coffee extract upregulated the pentose phosphate pathway in HCT116 cells, which may enhance NADPH production and reduce oxidative stress. Current evidence suggests coffee's bioactive compounds may have different effects varying by coffee extract type and their preparation.

Humans↗
PubMed2005

Some essential phytochemicals and the antioxidant potential in fresh and dried persimmon.

Fresh persimmon contains high quantities of bioactive compounds, but is only available in the autumn and winter months. The aim of this investigation was to compare fresh and dried persimmon in order to determine whether the latter could be a substitute for fresh fruit. It was found that the contents of dietary fibers and trace elements in fresh and equivalent quantities of dried fruits were comparable. The content of total polyphenols in fresh persimmon was higher than in dried fruit, but not significantly (P > 0.05). Also the antioxidant potential in fresh persimmon as determined by all three used tests was higher than in dried fruit, but not significantly (P > 0.05). The methanol extracts of fresh and dried persimmon using the ss-carotene-linoleate model system have shown 91% and 88% of antioxidant activity at 50?microl, respectively. Radical scavenging activity with the 1,1-diphenyl-2-picrylhydrazyl (DPPH) method has shown 88% and 84% for the same extracts and the nitric oxide test showed similar results. The best correlation was found between polyphenols, ss-carotene, DPPH and nitric oxide values (R(2) ranges between 0.9535 and 0.9934). In conclusion, both fresh and dried persimmon possess high contents of bioactive compounds and have a high antioxidant potential. When fresh fruits are not available, proper dried persimmon can be successfully used.

Antioxidants↗
PubMed2005

Anti-inflammatory effects of extracts from some traditional Mediterranean diet plants.

It is believed that bioactive compounds from plant foods may have health beneficial effects and reduce the risk of chronic inflammatory diseases. In this study extracts of 121 plants typical for the traditional Mediterranean diet have been screened for their potential anti-inflammatory activities. The ability of the extracts to inhibit cytokine-stimulated, iNOS-dependent synthesis of nitric oxide in murine endothelial cells, without affecting cell viability, was the primary indicator of their anti-inflammatory properties. Based on these experiments we selected eight plant extracts for further analysis: Chrysanthemum coronarium L., Scandix pecten-veneris L., Urospermum picroides (L.) Scop. Ex F. W. Smith, Amaranthus cf. graecizans L., Onopordum macracanthum Schousboe, Eryngium campestre L., Artemisia alba Turra and Merendera pyrenaica (Pourret) Fourn. Only the effects of Onopordum macracanthum could be non-specific since the extract strongly inhibited total protein synthesis. All remaining 7 extracts decreased nitric oxide and TNFalpha synthesis in the cells of monocyte origin activated with LPS, and 4 of them significantly reduced surface expression of VCAM1 on TNFalpha-stimulated endothelial cells. All seven plant extracts decreased cytokine or LPS-stimulated iNOS mRNA levels in both cell types. Further research to identify bioactive compounds influencing intracellular signaling pathways activated by cytokines and LPS will consequently be needed in order to better understand these in vitro effects.

Animals↗
PubMed2025

Logical Exploration of Cinnamoyl-Containing Nonribosomal Peptides via Metabologenomic Targeting and Regulator Overexpression.

A targeted method for discovering cinnamoyl-containing nonribosomal peptides (CCNPs), a unique class of bioactive compounds, was devised by using cinnamoyl isomerase, a key enzyme in the biosynthesis of the cinnamoyl moiety, as a genome mining probe. A total of 39 hit strains were obtained, including 35 from polymerase chain reaction-based screening of the in-house bacterial library (2.5% of 1400 strains) targeting the cinnamoyl isomerase-encoding gene and 4 from the genome mining of online databases. Sequence similarity networking and phylogenetic analyses of the isomerase amplicons (&#x223c;530 bp) classified the CCNPs into three major substructure-based groups (Z-, E-, and M-type CCNPs) and revealed distinct clade-structure relationships (13 clades). To overcome the challenge of silent biosynthetic gene clusters, we activated these clusters by overexpressing conserved cluster-situated LuxR regulators combined with extensive culture optimization. CCNP production was metabolomically detected in the bacterial extracts by using the characteristic UV absorption and MS/MS fragments of cinnamoyl moieties. CCNP production was observed in 20 of the 39 hit strains, resulting in the isolation of 6 new CCNPs, including oxy-skyllamycin B (2), gwanacinnamycin (3), and luxocinnamycins A-D (4-7), with high structural novelty. Their structures were elucidated using comprehensive spectroscopic analyses and multiple-step chemical derivatizations, and the putative biosynthetic pathways were bioinformatically proposed. Gwanacinnamycin (3) exhibited significant antimycobacterial activity, whereas luxocinnamycin A (4) displayed moderate antiproliferative activity against stomach cancer cells. Our findings highlight a targeted metabologenomic approach combined with transcriptional regulator overexpression as a logical and efficient platform for the discovery of bioactive compounds from nature.

Peptides↗
PubMed2005

Bioactive phenolic compounds from a medicinal lichen, Usnea longissima.

Natural products, longissiminone A (1) and longissiminone B (2), were isolated along with a known compound, glutinol (3), from a medicinal lichen, Usnea longissima. The structures of compounds 1 and 2 were determined with the help of spectroscopic studies. Compound 1 was found to possess potent anti-inflammatory activity in a cell-based contemporary assay. Cytotoxicity activity measured by cell viability assay showed 100% viability in the presence of 200 microg/mL conc. of these compounds.

Anti-Inflammatory Agents, Non-Steroidal↗
PubMed2000

New bioactive aromatic compounds from Vismia guianensis.

Five benzophenones, vismiaguianones A-E, and two benzocoumarins, vismiaguianins A and B were isolated from the CHCl3 extract of the roots of Vismia guianensis by bioassay-directed fractionation using the DNA strand-scission assay and KB cell line. Of the isolates obtained, vismiaguianone B exhibited DNA strand-scission activity, whereas vismiaguianones D and E and vismiaguianin A were found to be significantly cytotoxic.

Antineoplastic Agents, Phytogenic↗