Anthraquinone Concentration Research Articles

Influence of wood type on anthraquinone levels and quality properties of smoked chipotle pepper

This study aimed to assess the effects of pecan and mesquite wood, as well as smoking time, on anthraquinone (AQ) levels and quality properties of chipotle pepper (CHP) during the traditional smoking process. Changes in moisture content, microstructure, levels of total phenols (TPs), AQ, capsaicin (CAPS), dihydrocapsaicin (DHC), total polyphenols (TPPs), and total antioxidant activity (TAA), as well as color parameters, were measured. A wood mixture consisting of pecan, poplar, mesquite, and pine was used as the control. The CHP moisture content consistently decreased from 12 to 108 h of smoking, with long times exhibiting asymptotic trends across all treatments. Concurrently, structural changes, such as pericarp thinning and plant tissue collapse, were observed as the smoking process progressed. The wood type and processing time had a significant impact (P < 0.05) on TPs, AQ, CAPS, DHC, TAA levels, and color. TPs and AQ exhibited behavior opposite to that of the moisture content. CHP smoked in mesquite wood exhibited the highest TPs absorption rate and the lowest AQ levels. However, the AQ levels in CHP using any wood type exceeded permissible limits (0.02 mg·kg−1) at 12 h of processing, with the control exhibiting the highest AQ concentrations. The highest concentrations of CAPS and DHC were observed at 36 h in all treatments, with lower losses in mesquite wood CHP. The control exhibited the highest TAA values compared to fresh peppers. CHP color (a*, redness) decreased throughout the smoking process. The pecan and mesquite wood treatments resulted in the lowest loss of a* (P < 0.05). These results indicate that using mesquite wood for CHP production promotes higher TPs concentrations with lower AQ levels, followed by pecan wood, when compared to the control. These findings suggest the need to investigate the mechanisms of AQ formation to achieve CHP parameters within the regulatory limits with good quality.

Investigation of anthraquinone-producing Trichoderma reesei by highperformance liquid chromatography (HPLC)

Objective: To investigate the isolates of Trichoderma that produce anthraquinones by High-performance LiquidChromatography (HPLC).Methods: Trichoderma specimen were collected from Wassit Soil and identified dependent on morphological featuresand tested for production of anthraquinones by HPLC, Trichoderma isolate which produced a high concentration ofanthraquinones diagnosed for the species using PCR-ITS region.Results: Ten isolates were identified as Trichoderma according to morphological and microscopic features. Resultsthree Trichoderma isolates show differences between the concentrations of anthraquinones among the ten isolates.The total concentration of this compound in the extracts of specimens 1, 2 and 3 were (7.765ug/ml), (2.308ug/ml),and (4.977ug/ml) respectively. At the final concentration of Trichoderma isolates, genomic DNA have been extracted(400 to 600 ug) / (2 to 3g) fresh mycelium, and with a concentration of (1.6 to1.8), and the results of amplifyingTrichoderma DNA samples by using ITS-1 and ITS-4 showed a single unique band consistent with T. reesei F48-03, Whichwith other isolates of the Trichoderma were missing, were identified successfully.Conclusion: For identification and phylogenetic classification of Trichoderma, DNA-based methods that provide usefulclassification information are presently used. For several years, most T. spp. is regarded as a single species due to theirmorphological similarity. This research used ITS markers to distinguish genotypes within T. spp. because of amplifyinga distinct, naturally determined locus with a couple of T.reesei -specific oligonucleotide primers. This research wascarried out to provide supporting evidence for the long-standing antimicrobial use of anthraquinone.Keywords: DNA, Primers, Trichoderma, Phylogeny, Soil, Chromatography, Liquid, Polymerase, Reaction,Anthraquinones, Mycelium, Plant, Genomics.

Phytochemical Analysis of the Aerial Part of Golden Dock (&lt;i&gt;Rumex Maritimus&lt;/i&gt; L.)

Introduction. Golden dock (Rumex maritimus L., Polygonaceae) is used as a medicinal and food plant in Asian countries. The plant contains phytochemicals of various classes: flavonoids, tannins, anthraquinones etc. Plant extracts exhibit antibacterial, antioxidant, anti-inflammatory, astringent activity, and have antidiabetic potential. The plant is annual, and most of the biologically active substances accumulate in its aboveground organs. An important problem is the standardization of Rumex maritimus and the development of regulatory documentation for its the introduction to medical practice.Aim. To conduct phytochemical analysis of the aerial part of golden dock.Materials and methods. Air-dried aerial part of Rumex maritimus collected at flowering and beginning of fruiting stage, as well as individual above-ground organs (leaves, flowers, fruits, stems), were used for obtaining the extracts. Qualitative analysis of the extracts was carried out using reverse phase HPLC. The relative content of the components in the mixture was calculated by the method of simple normalization. Total content of free anthraquinones and anthraglycosides in terms of chrysophanic acid was determined using spectrophotometric method after acid hydrolysis. Total tannin content was calculated by titrimetric method.Results and discussion. Flavonoids isoquercetin and avicularin were first discovered in the aerial part of Rumex maritimus. The dominant component of the plant is rutin. Chrysophanol predominates among anthraquinones. The highest concentration of anthraquinones (2.80 ± 0.04 %) was found in flowers. Tannins accumulate mainly in leaves (9.97 ± 0.02 %). A significant amount of tannins (6.60 ± 0.03 %) and anthracene derivatives (1.96 ± 0.03 %) is contained in the whole aerial part.Conclusion. Phytochemical analysis of the aerial part of Rumex maritimus showed the presence of a significant amount of anthraquinones. As a plant raw material it is proposed to use the herb of Rumex maritimus. Standardization is recommended for anthraquinones in terms of chrysophanic acid (at least 1.5 %).

Dose-dependent Effects of Bio-AgNPs on Rubia tinctorum Callus and Root Biomass

Silver nanoparticles have frequently been used in many areas of biotechnology. These nanomaterials, especially biologically synthetized silver nanoparticles (bio-AgNPs), have some beneficial effects on plant biosystems because of their ethylene-inhibiting and auxin-stimulating effects which make them practical and cost-effective alternatives for synthetic plant growth regulators. The variety of the plants’ responses to bio-AgNPs is dose-dependent, and the effects show a wide variety for every plant, explant and culture types. In our study, bio-AgNPs derived from Syzygium aromaticum flowers were used in stem cultures of Rubia tinctorum. At 0–30 mg/L concentrations, their efficacies were evaluated on the basis of biomass and chemical accumulations. Bio-AgNPs affected the growth parameters and content of biomass depending on their concentrations. The highest biomass accumulations were detected at 10 mg/L concentration (up to 3.4 times higher compared to control). Callus and root regenerations were triggered at 5 and 10 mg/L concentrations. Total phenolic concentrations were detected at the highest level (16.54 and 18.86 mg GAE/g, respectively) at 15 mg/l concentration, whereas total flavonoid concentrations were the highest at 15 and 20 mg/L concentrations (5.63 and 5.42 mg QE/g, respectively). Total antioxidant capacity and radical scavenging activity enhanced in response to bio-AgNPs. The highest total antioxidant capacity was detected at 107.53 mg AAE/g at 1 mg/L concentration in root biomass (1.6 times higher than the control). Total anthraquinone concentrations reached their highest values at 30 mg/L bio-AgNP concentration in both callus and root tissues. The results revealed that bio-AgNPs acted as elicitors or/and biomass enhancers in response to their concentrations.

Nephroprotective Effect of Ethanol Extract of Carica Papaya Seed on Rats Induced Rifampicin and Isoniazid

Tuberculosis (TB) is an airborne, completely curable infection. The most common type is referred to as pulmonary TB. Rifampicin (RIF) is the first-line therapy for tuberculosis along with isoniazid (INH), ethambutol (ETB), and pyrazinamide (PZA). Papaya seeds are known to contain high concentrations of polyphenols, flavonoids, triterpenoids, tannins, saponins, alkaloids, glycosides, reducing sugars, steroids, proteins, lipids, anthraquinones, and anthocyanosides. The RIF is the most commonly prescribed anti-TB drug and most studies associate it with acute kidney injury. In this study, papaya seed ethanol extract was treated with different doses. For the test, eight groups of rats were used: normal, negative 1, negative 2, negative 3, positive, treatment I (100 mg/kg BW), treatment II (100 mg/kg BW), 300 mg/kg BW), and treatment III (500 mg/kg BW). After dissection of the mice, serum whey protein concentrations were measured. The results showed that compared to the negative control group, papaya seed ethanol extract significantly reduced urea, creatinine, uric acid, and creatinine clearance (<P0.05).

LARVICIDAL EFFICACY OF LEAF EXTRACTS FROM THREE ASTERACEOUS PLANT AGAINST MOSQUITO (Culex quinquefasciatus)

It is well known that the mosquito, Culex quinquefasciatus, badly affect individuals in endemic setting, causing filariasis. Intervention targeting the vector larva has not been given much priority. Therefore, the efficacy of ethanolic extract of Ageratum conyzoides, Bidens pilosa L. and Spilanthes filicaulis and a mixture of these plants in equal proportion was evaluated for larvicidal activities against filarial mosquito Culex quinquefasciantus. Phytochemical screening of the extracts was done by dissolving 5g each of plants in 30ml ethanol and water separately to obtain plant extracts. Samples were qualitatively screened following standard methodology for phytochemicals. Mortality of mosquito larva was examined after 12hrs, 24hr, 36hrs, and 48hrs treatment. Probit analysis for 50% Lethal Concentration was done using GraphPad Prism 9. Phytochemical screening of the plants revealed that Bidens pilos, Spilanthes filicaulis and Ageratum conyzoides contained moderated concentrations of Anthraquinones and Cardiac glycosids, Tannins, and Alkaloids respectively. Complete mortality was recorded with 0.60ml of Bidens pilosa, and Spilanthes filicaulis at 48hours and 36 hours respectively. More so, complete mortality was recorded with 0.40 and 0.60ml of the three plants in mixed proportion at 36 hours and 24 hours respectively. Larval mortality and time mortality were significantly (p&lt;0.05) different. 50%Lethal Concentration for Ageratum conyzoides L, Bidens pilosa L, Spilanthes filicaulis, and mixture of the three plants in equal proportion are 0.33ml, 0.25ml, 0.08ml, and 0.06ml respectively. Results showed that these plant materials exhibit significant activity and could be considered as potent natural larvicidal agent.

Development of a process for obtaining non-mutagenic madder root (Rubia tinctorum) extract for textile dyeing

Madder, used as a red dye, contains anthraquinones, and some of these can react with DNA possibly causing mutagenic effects. This is especially true for 1,3-dihydroxyanthraquinones with a hydroxymethyl (e.g., lucidin 6, ibericin 10) or methyl group (e.g., rubiadin 9) at C-2. In this research, a new process was developed through which the concentration of mutagenic compounds is minimized by adapting extraction and fractionation parameters. The process was tested on lab scale but also on 5000 L industrial scale. The first step is the key biotechnological step. Roots are stirred in water and the concentration of lucidin 6 is reduced to (near) zero by endogenous enzymes. When lucidin 6 is absent, the formation of mutagenic ibericin 10 by a reaction with ethanol as extraction solvent, is not possible. Mutagenicity can be further reduced by heat treatment, which is common in industrial downstream processing, e.g., in spray drying. Removal of rubiadin 9 is possible by flash chromatography. All madder root fractions were tested in the Salmonella microsome assay (Ames test, TA100) for mutagenicity, which was correlated with the anthraquinone concentration.

Anthraquinone repellent seed treatment on corn reduces feeding by wild pigs

Wild pigs (Sus scrofa) are a destructive invasive species that cause extensive damage to agriculture throughout many regions of the world. In particular wild pigs damage corn more than any other crop, and most of that damage occurs immediately after planting when wild pigs excavate and consume planted seeds. We evaluated whether anthraquinone (AQ), a repellent, could be useful for protecting seed corn from consumption by wild pigs. Specifically, we conducted cafeteria-style tests at 16 bait sites for 6 nights using concentrations of: untreated, 0.5, 1.5, and 3.0% AQ by weight sprayed on whole-kernel corn in AL and TX, USA. We found that repellency for wild pigs was dependent on the AQ concentration, with the greatest repellencies of 95% (AL) and 59% (TX) observed using ~3% AQ. We also found that repellency decreased as the abundance of wild pigs increased at the bait sites. Raccoons (Procyon lotor) did not appear to be repelled by the AQ-coated corn, but white-tailed deer (Odocoileus virginianus) and mule deer (O. hemionus) were. Overall, our results show promise for the development of a repellent for treating seeds to protect them from wild pigs. We recommend the next steps of testing of the 3% concentration of AQ on corn seeds that are planted underground to optimize the best potential protection against damage from wild pigs.

The potential antitumor effect of chrysophanol in relation to cervical cancer cells.

Chrysophanol is an anthraquinone with proven antitumor activity against several tumor cell lines. However, its effect on cervical cancer cells is still unknown. Therefore, HeLa cells were exposed to various concentrations of chrysophanol and then subjected to biochemical, ultrastructural, and morphological analysis. It has been shown using flow cytometry and MTT reduction assay that chrysophanol has been shown to inhibit cell viability and arrest cells in the G2/M phase of the cell cycle. Using Annexin V/propidium iodide staining, a significant increase in apoptosis was found after chrysophanol treatment on HeLa cells, and this process was mediated by caspases 3/7 with a clear inactivation of the antiapoptotic Bcl-2 family protein. However, the demonstrated increased number of cells with double-stranded DNA breaks suggests that chrysophanol also causes DNA damage. By means of electron and fluorescence microscopy, a clear effect of chrysophanol on the intensification of degradation processes, on changes in the structure of the nucleus, endoplasmic reticulumand mitochondria was demonstrated. The changes visible in the mitochondria may be related to the increase in the level of free radicals induced by chrysophanol, which induces apoptosis, inter alia, by increasing the permeability of mitochondrial membranes. The range of observed changes depended on the concentration of anthraquinone was tested.

Inefficiency of anthraquinone-based avian repellents when applied to sunflower: the importance of crop vegetative and floral characteristics in field applications.

Blackbirds (Icteridae) cause significant damage to sunflower (Helianthus annuus L.) prompting the need for effective management tools. Anthraquinone-based repellents can reduce feeding by > 80% in laboratory settings, but require birds to learn the negative association through repellent ingestion. We evaluated an anthraquinone-based repellent applied directly to mature sunflower plants for its ability to reduce bird damage. We used captive male red-winged blackbirds (Agelaius phoeniceus) to evaluate efficacy of two anthraquinone-based formulations in varying concentrations and applied in a manner attainable by sunflower producers. We also assessed field application methods for repellent coverage and anthraquinone residues when using ground-rigs equipped with drop-nozzles situated below the crop canopy. The repellents failed to reduce feeding and birds did not exhibit a preference between untreated and treated sunflowers at concentrations 2.7× the suggested application rate (i.e. 9.35 L ha-1 of repellent). In the absence of disk flowers, which obstruct repellent from reaching the achenes, the repellents failed to reduce consumption. Anthraquinone concentrations in field applications were considerably less than those in the laboratory experiments and did not reduce bird damage. Efficacy is difficult to achieve in the field due to application issues where growth patterns and floral components of sunflower limit residues on achenes, thus contact with foraging birds. Although field residues could be improved by increasing anthraquinone concentrations in tank mixtures and decreasing droplet size, repellents optimized for loose achenes are inefficient in reducing avian consumption of sunflower when applied to intact plants in a manner representative of commercial agriculture. © 2020 Society of Chemical Industry.

Phytochemical and Antioxidant Evaluation of Varieties of Pepper Fruits in Akpan Andem Market in Uyo Akwa Ibom State, Nigeria

The results of this research showed significant difference in the phytochemical contents of Capsicum baccatum L. (Yellow), Capsicum baccatum L. (Red), Capsicum Chinese Jacq., Capsicum annuum L. (Cayenne), Capsicum annuum L. (Bell) in terms of total Saponin, Tanins and Cardiac glucosides. The concentrations of flavonoids, Alkaloids and Anthraquinones were similar in the five species of Capsicum studied and it could be attribute to cultivation, ripeness, storage and soil salinity, among other factors. Reducing power assay is one of established method for evaluation of antioxidant potential of a test sample which was employed in the course of this work. Basically, it involves reduction of Fe3+ into Fe2+ with the formation of Perl’s Prussian blue colour complex wherein absorbance is read at 700 nm. This reducing ability varies with respect to various concentrations of antioxidant present in the samples. The Different fruit composition of the five pepper species indicates that apart from the evident morphological differences in terms of fruit shape and appearance, they also differ in their content of phytochemicals.

Simultaneous Determination of Anthraquinone and Bisphenol A in Pulp and Paper Products by High Performance Liquid Chromatography‒Tandem Mass Spectrometry

A procedure for the rapid simultaneous determination of anthraquinone and bisphenol A in paper and cardboard is proposed based on a combination of extraction with subcritical methanol and subsequent analysis of the extracts by HPLC‒tandem mass spectrometry. The achieved limits of detection are 25 and 250 µg/kg for anthraquinone and bisphenol A, respectively, and fully meet present-day safety requirements for pulp and paper products. The total duration of the analysis, including sample preparation, is not more than 45 min. The sensitivity of anthraquinone determination is 1‒2 orders of magnitude higher than that of the known procedures, including those with the preconcentration of analytes. The results obtained were successfully used to study paper and cardboard samples, in most of which unacceptably high levels of the anthraquinone concentration were found.

Separation of Protein-Binding Anthraquinones from Semen Cassiae Using Two-Stage Foam Fractionation

Anthraquinones are compounds of high medicinal value in many plants. Based on their good protein binding affinity, foam fractionation was attempted to separate them using proteins in the aqueous extract of Semen Cassiae as collectors. Firstly, the interaction between anthraquinones and Semen Cassiae proteins has been analyzed by the Stem–Volmer equation with physcion as a standard. The results show that physcion had good interaction with the proteins via hydrophobic forces. More importantly, the proteins effectively assisted the foam fractionation of several anthraquinones including aurantio-obtusifolin, aloe-emodin, rhein, emodin, chrysophanol, and physcion. On this basis, a two-stage foam fractionation technology was developed for process intensification using a foam fractionation with vertical sieve trays (VSTs). VSTs, initial feed concentration of total anthraquinones, temperature, volumetric air flow rate and pore diameter of gas distributor had significant effects on enrichment ratio and recovery yield of anthraquinones. Under suitable conditions, the enrichment ratio of total anthraquinones reached 47.0 ± 4.5 with a concentration of 939 ± 94 mg/L in the foamate while their total recovery percentage reached more than 47.7%. In addition, foam fractionation also increased the purity and hydroxyl radical scavenging activity of total anthraquinones. The results had significant implications for the separation of anthraquinones from Semen Cassiae.

Optimization of Alkaline Pulp Extraction from Napier Grass Using Response Surface Methodology

Napier grass which has several types of them has been studied by researchers for few applications such as biofuel, sugar and pulp production. This research focused on specific type of Napier grass which is the Dwarf Napier due to high cellulose content to produce pulp. Delignification of Dwarf Napier grass was carried out by soda anthraquinone pulping under varying conditions selected according to experimental design software with three factors. The influence of these three factors including concentration of sodium hydroxide (15%, 17.5% and 20%), concentration of anthraquinone (0.05% and 0.1%) and duration of cooking time (30, 60 and 90 min) on pulp yield was studied. 18 runs of experiment were conducted and the result obtained was used to analyse the optimized condition for pulp extraction by using RSM. Results indicated that the optimized response obtained while Napier grass stem is treated with 17.5% sodium hydroxide and 0.05% AQ with 66 mins of cooking time meanwhile the predicted yield is 34.87 %. However, the actual pulp yield obtained (36.38%) is higher than the predicted yield. The pulp which extracted with optimized condition is then bleached with hydroxide peroxide. Fourier transform infrared spectroscopy (FTIR) was used to characterize the raw grass fiber and pulp obtained. Napier grass is successfully demonstrated to be an effective alternative source for producing paper pulp. In the this study Dwarf Napier grass fibres were successfully pulped applying soda AQ process although the obtained pulp is not as high as the studied done before due to the limitations. FTIR analysis also confirmed the removal of lignin as well as most of the hemicellulose during the pulping process. Therefore, the abundance and fast growth of Napier grass are an added advantage as an alternative non-wood source for papermaking

Predicting the content of anthraquinone bioactive in Rhei rhizome (Rheum officinale Baill.) with the concentration addition model

Rhei rhizome (Rheum officinale Baill.) (RR) contains a large number of anthraquinone bioactive, yet little is known of the combined effect of these anthraquinones in a mixture. The goals of this study were: to determine the inhibitory potencies of individual anthraquinones and whole RR extract against human liver microsomal CYP1A2/3A4 activity, to predict the content of anthraquinones in RR using the concentration addition (CA) model, and to compare predicted and empirical contents in the same RR sample. Anthraquinone concentrations in the RR extract were determined using HPLC. The inhibitory potencies of individual anthraquinones were determined in incubations containing human liver microsomes. The study results were used to predict an effect-based dose measure of the anthraquinones in RR using the CA model. An empirical dose measure also was determined in the whole RR extract using the CYP1A2/3A4-based bioassay. For the CYP1A2-based studies, the predicted and empirical dose measures of anthraquinones were identical; they were 12.0 ± 1.80 and 12.20 ± 0.81 mg aloe-emodin equivalents/g RR, respectively. For the CYP3A4-based studies, the predicted and empirical dose measures were different; they were 2.80 ± 0.10 and 19.04 ± 0.41 mg aloe-emodin equivalents/g RR, respectively. Only the CYP1A2-based CA model which assumed additive effects of RR anthraquinones predicted an effect-based dose measure that was verifiable by empirical data. The CA model provides an alternative approach to the CYP1A2/3A4-based bioassay or empirical method to screen for the anthraquinones in RR. The CA model as described in this study is applicable to other botanical drugs, plant-based foods and dietary supplements.

Efficacy of repellent-treated structural barriers for Richardson’s ground squirrels (Urocitellus richardsonii (Sabine)) and house mice (Mus musculus L.)

The worldwide presence of vertebrate pests such as rodents has created a need for non-lethal control methods that can be applied to integrated pest management plans. Chemical repellents are often a useful wildlife management tool as they can be directly applied to a commodity or structure to prevent infringement and damage. We assessed the efficacy of an anthraquinone (AQ)-based repellent in a structural barrier model against Richardson’s ground squirrels (Urocitellus richardsonii (Sabine)) (RGS) and house mice (Mus musculus L.). The AQ-based repellent was applied to pieces of burlap which were secured over each end of a small section of PVC pipe. Unadulterated enrichment food was then offered within the enclosed PVC pipe to motivate interactions with repellent-treated and untreated burlap barriers. Defeat of the barrier was defined as a physical breach by means of chewing the burlap or burlap/repellent barrier such that the test animal was able to gain entry to the hide and the enrichment food. RGS defeated 55% (±7.9) of untreated barriers, 25% (±6.8) of barriers treated with 50% dilution AQ-based repellent, and 27.5% (±5.6) of barriers treated with 0% dilution AQ-based repellent. House mice defeated 100% (±0.0) of untreated barriers, 20.5% (±6.4) of barriers treated with 50% dilution AQ-based repellent, and 45.5% (±7.8) of barriers treated with 0% dilution AQ-based repellent. Relative to untreated barriers, AQ treatments reduced defeat of the barrier by 50–55% for RGS and 55–80% for house mice. RGS showed a marked decrease in consumption of enrichment food after exposure to AQ. The 0% dilution of AQ-treated structural barrier had more individuals of both RGS and house mice chew through the structural barrier than the 50% dilution despite the increased concentration of AQ. We hypothesized that the additional water in the 50% dilution may have allowed for greater absorption of the repellent throughout the burlap fibers, thus enabling greater interaction with the AQ-treated barriers. Our results indicate that AQ-based repellents show promise as structural barriers for RGS and house mice.

Transcriptional regulation effect of THSG and anthraquinones in tubers of Polygonum multiflorum based on human progesterone X receptor (PXR) mediated CYP3A4 rapid screening system

The rapid screening technology was used to investigate the transcriptional regulation effect of main chemical constituents in tubers of Polygonum multiflorum, including 2,3,5,4'-tetrahydroxystilbene-2-O-β-D-glucopyranoside(THSG) and anthraquinones (such as rhein, chrysophanol, aloe-emodin, emodin) on CYP3A4 drug inducers induced by human pregnancy X receptor (PXR).The effect of chemical composition on the cell activity was detected by MTS cell viability assay. IC₅₀ was calculated. The expression vector and the reporter vector were co-transfected into HepG2 cells, with 10 μmol•L⁻¹ rifampicin (RIF) as a positive control, and 10 μmol•L⁻¹ ketoconazole (TKZ) as a negative control. After treated with different concentrations of anthraquinones (2.5, 5, 10 μmol•L⁻¹) for 24 h, the cells were tested for dual luciferase activity. The results show that the inhibitory effect of THSG, chrysophanol, emodin, rhein and aloe-emodin on CYP3A4 was inhibited by co-transfection of pcDNA3.1 and pGL4.17-CYP3A4. The expressions of pcDNA3.14-PXR and pGL4.17-CYP3A4 were induced by the four compounds. Besides, emodin had a direct inducing effect. In conclusion, the four anthraquinone compounds have an inducing effect on CYP3A4 by PXR, but emodin can directly induce CYP3A4. THSG can inhibit CYP3A4, but plasmid can induce CYP3A4 after intervened with PXR.These results suggest that we should pay attention to the liver function and avoid liver damage in the combined administration of drugs.

The Influence of Compatibility of Rhubarb and Radix Scutellariae on the Pharmacokinetics of Anthraquinones and Flavonoids in Rat Plasma.

Rhubarb-Radix scutellariae is a classic herb pair, which is commonly used to clear away heat and toxin in clinic. The aim of this study was to investigate the influence of compatibility of Rhubarb and Radix scutellariae on the pharmacokinetic behaviors of anthraquinones and flavonoids in rat plasma. Eighteen rats were randomly divided into three groups, and were orally administered Rhubarb and/or Radix scutellariae extracts. A sensitive and rapid UPLC-MS/MS method was developed and validated to determine the concentrations of baicalin, baicalein, wogonside, wogonin, rhein, and emodin in rat plasma. The concentrations of phase II conjugates of flavonoid aglycones and anthraquinone aglycones were also determined after hydrolyzing the plasma with sulfatase. Compared with administration of Radix scutellariae alone, co-administration of Rhubarb significantly decreased the first maximum plasma concentration (C max1) of baicalin, wogonside, and the phase II conjugates of baicalein, wogonin to 46.40, 61.27, 41.49, and 20.50%, respectively. The area under the plasma concentration-time curve from time zero to infinity (AUC0-∞) was significantly decreased from 82.60±20.22 to 51.91±7.46μM·h for rhein and 276.83±98.02 to 175.42±86.82μM·h for the phase II conjugates of wogonin after compatibility. The time to reach the first maximum plasma concentration (T max1) of anthraquinones was shortened and the second peak of anthraquinones disappeared after compatibility. Compatibility of Rhubarb and Radix scutellariae can significantly affect the pharmacokinetic behaviors of characteristic constituents of the two herbs. The cause of these pharmacokinetic differences was further discussed combined with the in vivo ADME (absorption, disposition, metabolism, and excretion) processes of anthraquinones and flavonoids.

Spontaneous photosensitization by Heterophyllaea pustulata Hook. f. (Rubiaceae), in sheep from Northwestern Argentina.

Heterophyllaea pustulata Hook. f. (Rubiaceae) is a phototoxic plant. It grows in the Andean area of northwest of Argentina, and it causes significant economic losses in the livestock. This plant induces dermal lesions by photosensitization probably due to its content of photosensitizing anthraquinones. This paper describes an outbreak of poisoning in Corriedale sheepfold, which had an incidence of 49%. Ear skin biopsies and blood samples were collected of six affected animals. Liver enzymes remained within the reference limits. Histopathologically, a deep necrotizing dermatitis was identified in all samples. H. pustulata was identified in the areas of grazing. Anthraquinone concentration in leaves was 0.84% p/p, expressed as rubiadin. All findings allow us to conclude that the diagnosis is a primary photosensitization. Huge regional economic losses could be attributed to H. pustulata poisoning, although its toxicity has been little studied.

Pharmacokinetics and pharmacodynamics of rhubarb anthraquinones extract in normal and disease rats

BackgroundAnthraquinones extract from Rheum palmatum L. (rhubarb) including rhein, emodin, aloe-emodin, chrysophanol, physcion and sennoside A, has been widely used in China to treat various diseases. ObjectiveThis study was designed to explore the pharmacokinetic and pharmacodynamic properties of rhubarb anthraquinones extract in diabetic nephropathy and acute liver injury rats. MethodsThe diabetic nephropathy and acute liver injury rats were induced by intraperitoneal injection with streptozotocin (STZ) and carbon tetrachloride (CCL4), respectively. The rats were treated with different doses of rhubarb anthraquinones extract (37.5, 75 and 150mg/kg) as administration groups. For pharmacokinetics, the drug concentrations of rhubarb anthraquinones consisting of rhein, emodin, aloe-emodin, chrysophanol, physcion and sennoside A were determined. For pharmacodynamics, the anti-diabetic nephropathy and hepatoprotective effects were assessed under different dosage regimens. ResultsThe rhein, emodin, aloe-emodin, chrysophanol were considered as pharmacokinetic markers at three doses of rhubarb anthraquinones extract. In diabetic nephropathy rats, no obvious pharmacokinetic change of the four ingredients was observed compared with control rats. However, the plasma exposures of the four ingredients increased in acute liver injury rats compared with control rats. The serum creatinine (SCr), blood urea nitrogen (BUN) and urine protein (UP) values in diabetic nephropathy rats decreased compared with those in the model group, which suggested that rhubarb anthraquinones extract displayed certain therapeutic and preventive effects against the diabetic nephropathy. However, rhubarb anthraquinones extract cannot ameliorate the CCL4-induced liver injury under the three different dosage regimens. ConclusionThere was no significant pharmacokinetic difference after a single oral administration of rhubarb anthraquinones extract between control and diabetic nephropathy rats. However, apparent pharmacokinetic differences were observed between control and liver injury rats. Also, rhubarb anthraquinones extract had beneficial effects on diabetic nephropathy rats, while no marked effect on liver injury rats under the same dosage regimens.