Construction of oxime-functionalized PCN-222 based on the directed molecular structure design for recovering uranium from wastewater.

The directed construction of productive adsorbents is essential to avoid damaging human health from the harmful radioactive and toxic U(VI)-containing wastewater. Herein, a sort of Zr-based metal organic framework (MOF) called PCN-222 was synthesized and oxime functionalized based on directed molecular structure design to synthesize an efficient adsorbent with antimicrobial activity, named PCN-222-OM, for recovering U(VI) from wastewater. PCN-222-OM unfolded splendid adsorption capacity (403.4 mg·g-1) at pH = 6.0 because of abundant holey structure and mighty chelation for oxime groups with U(VI) ions. PCN-222-OM also exhibited outstanding selectivity and reusability during the adsorption. The XPS spectra authenticated the -NH and oxime groups which revealed a momentous function. Concurrently, PCN-222-OM also possessed good antimicrobial activity, antibiofouling activity, and environmental safety; adequately decreased detrimental repercussions about bacteria and Halamphora on adsorption capacity; and met non-toxic and non-hazardous requirements for the application. The splendid antimicrobial activity and antibiofouling activity perhaps arose from the Zr6(µ3-O)4(µ3-OH)4(H2O)4(OH)4 clusters and rich functional groups within PCN-222-OM. Originally proposed PCN-222-OM was one potentially propitious material to recover U(VI) in wastewater on account of outstanding adsorption capacity, antimicrobial activity, antibiofouling activity, and environmental safety, meanwhile providing a newfangled conception on the construction of peculiar efficient adsorbent.

Efficient removal of uranium (VI) from water by a hyper-cross-linked polymer adsorbent modified with polyethylenimine via phosphoramidate linkers.

Practical adsorbents with high efficiency are essential to effectively treating wastewater. Herein, a novel porous uranium adsorbent (PA-HCP) having a considerable amount of amine and phosphoryl groups was designed and synthesized by grafting polyethyleneimine (PEI) on a hyper-cross-linked fluorene-9-bisphenol skeleton via phosphoramidate linkers. Furthermore, it was used to treat uranium contamination in the environment. PA-HCP exhibited a large specific surface area (up to 124 m2/g) and a pore diameter of 2.5 nm. Batch uranium adsorptions on PA-HCP were investigated methodically. PA-HCP demonstrated a uranium sorption capacity of >300 mg/g in the pH range of 4-10 (C0 = 60 mg/L, T = 298.15 K), with its maximum capacity reaching 573.51 mg/g at pH = 7. The uranium sorption process obeyed the pseudo-second-order model and fitted well with the Langmuir isothermal. In the thermodynamic experiments, uranium sorption on PA-HCP was revealed to be an endothermic, spontaneous process. Even in the presence of competing metal ions, PA-HCP exhibited excellent sorption selectivity for uranium. Additionally, excellent recyclability can be achieved after six cycles. Based on FT-IR and XPS measurements, both the PO and -NH2 (and/or -NH-) groups on PA-HCP contributed to efficient uranium adsorption as a result of the strong coordination between these groups and uranium. Furthermore, the high hydrophilicity of the grafted PEI improved the dispersion of the adsorbents in water and facilitated uranium sorption. These findings suggest that PA-HCP can be used as an efficient and economical sorbent to remove U(VI) from wastewater.

Integrative analyses of transcriptome and metabolome reveal comprehensive mechanisms of Epigallocatechin-3-gallate (EGCG) biosynthesis in response to ecological factors in tea plant (Camellia sinensis).

Epigallocatechin-3-gallate (EGCG), a flavoured and healthy compounds in tea, is affected by the ecological factors. However, the biosynthetic mechanisms of EGCG in response to the ecological factors remian unclear. In this study, a response surface method with a Box-Behnken design was used to investigate the relationship between EGCG accumulation and ecological factors; further, integrative transcriptome and metabolome analyses were performed to explore the mechanism underlying EGCG biosynthesis in response to environmental factors. The optimal environmental conditions obtained for EGCG biosynthesis were as follows: 28℃, 70 % relative humidity of the substrate, and 280 µmol·m-2·s-1 light intensity; the EGCG content was increased by 86.83 % compared to the control (CK1). Meanwhile, the order of EGCG content in response to the interaction of ecological factors was as follows: interaction of temperature and light intensity > interaction of temperature and relative humidity of the substrate > interaction of light intensity and relative humidity of the substrate, indicating that temperature was the dominant ecological factors. EGCG biosynthesis in tea plants was found to be comprehensively regulated by a series of structural genes (CsANS, CsF3H, CsCHI, CsCHS, and CsaroDE), miRNAs (miR164, miR396d, miR5264, miR166a, miR171d, miR529, miR396a, miR169, miR7814, miR3444b, and miR5240), and transcription factors (MYB93, NAC2, NAC6, NAC43, WRK24, bHLH30, and WRK70); further, the metabolic flux was regulated and converted from phenolic acid to the flavonoid biosynthesis pathway based on accelerated consumption of phosphoenolpyruvic acid, d-erythrose-4-phosphate, and l-phenylalanine in response to ambient changes in temperature and light intensity. Overall, the results of this study reveal the effect of ecological factors on EGCG biosynthesis in tea plants, providing novel insights for improving tea quality.

Efficient uranium adsorbent with antimicrobial function constructed by grafting amidoxime groups on ZIF-90 via malononitrile intermediate.

Herein, a dual-function Zeolitic Imidazole Frameworks (ZIFs) ZIF-90 grafted with malononitrile by Knoevenagel reaction and following with an amidoximation reaction to form an efficient U (VI) adsorbent (ZIF-90-AO). The strong chelation power of amidoxime groups (AO) with uranium and ZIF-90's mesoporous structure afforded ZIF-90-AO high maximum uranium adsorption capacity of 468.3 mg/g (pH = 5). In addition, the factors affecting uranium adsorption process were investigated by a batch of adsorption tests under different adsorption conditions. ZIF-90-AO displayed good selectivity to UO22+ in the solution containing multiple co-existing ions and good regeneration property. More importantly, ZIF-90-AO showed excellent antimicrobial property against both E. coli and S. aureus. Therefore, ZIF-90-AO is a U-adsorbent with great application value for removing U (VI) from wastewater due to the high U (VI) adsorption capacity in weak acid condition and good anti-biofouling properties.

The antiviral mechanism of the crude extract from the flowers of Trollius chinensis based on TLR 3 signaling pathway.

The effects of crude extract from the flowers of Trollius chinensis on expressions of mRNA and proteins related to vital genes (TLR 3, TBK 1, IRF 3 and IFN ß) in TLR 3 signaling pathway were investigated in the presence/absence of Polyinosinic acid-polycytidylic acid (PolyI: C) to ascertain the antiviral mechanism of these flowers. Real-time PCR and western blot were applied to determine the expressions of mRNA and proteins, respectively, and immunofluorescence assay was employed to study the effect on IRF 3 distribution between nuclei and cytoplasma. In the absence of PolyI:C, the crude extract reduced the mRNA expression of TLR 3, IRF 3 and IFN ß and the protein expression of TLR 3, and increased the protein expression of IRF 3 and the distribution of IRF 3 in nuclei. In the presence of PolyI:C, the extract reduced the mRNA and protein expressions of TLR 3 and the mRNA expression of IFN ß, meanwhile inhibited the translocation of IRF 3 into nuclei. The antiviral mechanism of the crude extract from the flowers of T. chinensis is to protect the host from inflammatory damage through intervening the TLR 3 signaling pathway and reducing the secretion of inflammatory factors.

Synthesis of phosphorylated hyper-cross-linked polymers and their efficient uranium adsorption in water.

Uranium (U) is hazardous and radioactive, wastewater containing U(VI) should be treated before being discharged. Here, two novel uranium adsorbents, phosphorylated hyper-cross-linked bisphenol A (PHCP-1) and fluorene-9-bisphenol (PHCP-2) were separately synthesized via Friedel-Crafts reaction followed by phosphorylation using phosphorus oxychloride. PHCPs had a BET surface area (up to 564 m2/g) with pore sizes of 2.2-2.8 nm. These adsorbents were used for the first time for uranium adsorption from water and demonstrated outstanding adsorption performance. PHCP-2 had a great uranium adsorption capacity (297.14 mg/g) and a very fast sorption rate (85% removal rate within 5 min). The adsorption data were well fitted with Freundlich isotherm and the pseudo-second-order kinetic model. PHCPs displayed selective adsorption capacity for U(VI) from solution that including a variety of competing metal ions. The reusability was confirmed through three regeneration cycles. Based on a series of spectroscopic analyses, the mechanism of action between PHCPs and U(VI) is primarily derived from the complex between phosphate functional groups and U (VI). The sorption performance of PHCPs is attributed to their huge specific surface area and the strong complex between phosphate groups and U(VI). These findings suggest that PHCPs could be useful in the effective adsorption of uranium from water.

Exploring the In Vivo Existence Forms (23 Original Constituents and 147 Metabolites) of Astragali Radix Total Flavonoids and Their Distributions in Rats Using HPLC-DAD-ESI-IT-TOF-MSn.

Astragali Radix total flavonoids (ARTF) is one of the main bioactive components of Astragali Radix (AR), and has many pharmacological effects. However, its metabolism and effective forms remains unclear. The HPLC-DAD-ESI-IT-TOF-MSn technique was used to screen and tentatively identify the in vivo original constituents and metabolites of ARTF and to clarify their distribution in rats after oral administration. In addition, modern chromatographic methods were used to isolate the main metabolites from rat urine and NMR spectroscopy was used to elucidate their structures. As a result, 170 compounds (23 original constituents and 147 metabolites) were tentatively identified as forms existing in vivo, 13 of which have the same pharmacological effect with ARTF. Among 170 compounds, three were newly detected original constituents in vivo and 89 were new metabolites of ARTF, from which 12 metabolites were regarded as new compounds. Nineteen original constituents and 65 metabolites were detected in 10 organs. Four metabolites were isolated and identified from rat urine, including a new compound (calycoisn-3'-O-glucuronide methyl ester), a firstly-isolated metabolite (astraisoflavan-7-O-glucoside-2'-O-glucuronide), and two known metabolites (daidzein-7-O-sulfate and calycosin-3'-O-glucuronide). The original constituents and metabolites existing in vivo may be material basis for ARTF efficacy, and these findings are helpful for further clarifying the effective forms of ARTF.

Global Profiling and Structural Characterization of Metabolites of Ononin Using HPLC-ESI-IT-TOF-MSn After Oral Administration to Rats.

Ononin is a bioactive isoflavone of legumes. To explore the "effective forms" of ononin, its metabolites were characterized using HPLC-ESI-IT-TOF-MSn after oral administration to rats. Metabolites (106), including 94 new metabolites, were characterized, which contained 17 phase I, 23 hydroxylated and methylated, 54 sulfated, 10 glucuronidated, and 2 sulfated and glucuronidated metabolites. Six hydroxylated metabolites of formononetin (aglycone of ononin) were simultaneously detected for the first time. Twenty-three hydroxylated and methylated metabolites were the new metabolites of ononin, and the number of hydroxylation and methylation was 1-3 and 1-2. Twenty metabolites have ononin-related bioactivities, and many metabolites have the same bioactivities. Their probable mechanisms of action may be additive and/or synergistic effects, especially because of the addition of the blood concentrations of these compounds. The results provide a foundation for a better understanding of the "effective forms" of ononin.

Anti-influenza A virus mechanism of three representative compounds from Flos Trollii via TLRs signaling pathways.

ETHNOPHARMACOLOGICAL RELEVANCE: Flos Trollii is the dried flowers of Trollius chinensis. It has been used as a traditional herbal medicine for the treatment of upper respiratory tract infection, tonsillitis and pharyngitis in China for a long history. Veratric acid, vitexin, and trolline are the representative compounds of phenolic acids, flavonoids and alkaloids in this herbal medicine. All of these three compounds show antiviral activity which is related to the efficacy of Flos Trollii. AIM OF THE STUDY: To investigate the anti-influenza A virus mechanism of the three representative compounds from the perspective of regulating TLRs signaling pathways, so as to understand the relevant efficacy of Flos Trollii. MATERIALS AND METHODS: Influenza A virus A/FM/1/47 (H1N1) and mouse peritoneal macrophages (RAW264.7) were used in the whole process of investigation. MTT assay was conducted to select the appropriate experimental concentrations of the three compounds on RAW264.7 cells. Western blot, RT-PCR, and ELISA assays were performed to determine the protein and mRNA expression of key factors and related inflammatory factors of TLRs signaling pathways. Griess method was employed to detect the production of NO. RESULTS: The three representative compounds reduced the inflammatory factors including NO, IL-6, and TNF-α and enhanced the production of IFN-ß through dynamically regulating the TLRs 3, 4 and 7 pathways. Veratric acid significantly down-regulated the protein expression of TLR3 and IRF3 as well as the mRNA expression of TBK1 and TRIF. Vitexin significantly down-regulated the protein expression of TBK1 and IRF3 as well as the mRNA expression of TLR3, TBK1, TRIF and IRF3 while up-regulated the protein expression of TLR4 and IKKα. Trolline significantly down-regulated the protein expression of TLR7 whereas significantly up-regulated the protein expression of TLR4, IKKα and TAK1. CONCLUSIONS: The three representative compounds from Flos Trollii play their parts in anti-H1N1 viral effect through partially down-regulating TLRs 3 and 7 pathways and up-regulating TLR4 pathway. They counteract the inflammatory injury caused by excessive production of NO, IL-1, IL-6, and TNF-α induced by virus infection and enhance the production of IFN-ß so as to eliminate the virus.

Investigation of the In Vivo Metabolism of Sibirioside A and Angoroside C in Rats by HPLC-ESI-IT-TOF-MSn.

Sibirioside A and angoroside C are two important phenylpropanoid glycosides of the traditional Chinese medicine Scrophulariae Radix. High performance liquid chromatography, coupled with an ion trap time-of-flight multistage mass spectrometry equipped with electrospray ionization source (HPLC-ESI-IT-TOF-MSn), was applied to the profile and we identified the metabolites of sibirioside A and angoroside C in vivo in rats. A total of four metabolites of sibirioside A were identified: SM1, SM2 and SM3 which were known as new compounds. A total of 25 metabolites were detected for angoroside C: AM4, AM5, AM6, AM7, AM16, AM17, AM20, AM21, AM22, AM23 and AM25 which were identified to be new compounds. The main metabolic reactions were hydrolysis, reduction, hydroxylation, methylation, sulfation, and gluconylation. The prototype of sibirioside A was widely distributed in tissues found in the heart, liver, spleen, lung, kidney, stomach and small intestine of rats, and mainly distributed in the stomach, small intestine, kidney and liver. But for angoroside C, nothing was found in the viscera except the stomach and small intestine. The metabolites of sibirioside A were mainly eliminated from feces, while it was urine for the metabolites of angoroside C. Furthermore, 19 metabolites were likely to have bioactivities based on the 'PharmMapper' analysis, which roughly matched the known pharmacological activities of Scrophulariae Radix (SR) and the prototypes. One of the main pharmacological activities of SR in traditional Chinese medicine is anti-diabetes, and the predicted results showed that SM1, SM2, SM3, AM2, AM4, AM5, AM6, AM9, AM10, AM11, AM12, AM13, AM15, AM18, AM19, AM24, and AM25 might be used to cure diabetes. These findings provide a reference for studying the metabolism, distribution and pharmacological actions of phenylpropanoid glycosides in vivo.

Anti-inflammatory effect of the compounds from the flowers of Trollius chinensis.

In order to investigate the anti-inflammatory activity of flavonoids, phenolic acids, and alkaloids from the flowers of Trollius chinensis, some representative compounds, namely, orientin, 2"-O-ß-L-galactopyranosylorientin, vitexin, quercetin, isoquercetin, luteolin, veratric acid, proglobeflowery acid, trollioside, and trolline were selected to study their inhibitory effects against LPS-induced NO, IL-6, and TNF-ß release in RAW264.7 cells. At the higher concentration, both phenolic acids and flavonoids inhibited the production of NO, whereas only phenolic acids showed this effect at the lower concentration. Although trolline had stronger cytotoxicity, it exhibited a potential effect of decreasing NO production induced by LPS in the non-toxic concentration range. In addition, all tested compounds decreased the production of IL-6 and TNF-a by almost 50% at both the higher and lower concentrations. It is concluded that the anti-inflammatory activity of the phenolic acids is stronger than that of the flavonoids.

Lignans and diterpenes isolated from Tirpitzia ovoidea and their biological activities.

A new lignan, tirpitzin A (17) together with 20 known compounds (1-16, and 18-21) were isolated from the ethyl acetate soluble fraction of ethanol extract of the aerial parts of Tirpitzia ovoidea. The structure of new compound was elucidated by means of spectroscopic analysis. Of the known compounds, 7-21 were isolated from Linaceae family for the first time. The pharmacological activity of the crude extracts was tested using a mouse inflammation model induced by dimethyl benzene. The results demonstrated that the ethyl acetate soluble fraction had anti-inflammatory activity. Moreover, the cytotoxic and anti-inflammatory activities of some compounds were studied. The new compound 17 showed moderate cytotoxic effect against BxPC-3 cell line (IC50 = 19.51µmol·L-1) and Compound 10 showed significant cytotoxicity against HepG2, HL-60, U87 and BxPC-3 cell lines with IC50 values in the range 4.2-8.3µmol·L-1. Additionally, Compounds 2, 10, 11, and 13 exhibited potent inhibitory effects on LPS-induced nitric oxide production in RAW 264.7 macrophages at the concentration of 50µmol·L-1.

Antitumoral Activity of (20R)- and (20S)-Ginsenoside Rh2 on Transplanted Hepatocellular Carcinoma in Mice.

Hepatocellular carcinoma is one of the leading causes of malignancy-related death in China. Its therapy in clinics is a big challenge. Ginsenoside Rh2 is one of the most notable cancer-preventing components from red ginseng and it has been reported that ginsenoside Rh2 exhibited potent cytotoxicity against human hepatoma cells. Rh2 exists as two different stereoisomeric forms, (20S)-ginsenoside Rh2 and (20R)-ginsenoside Rh2. Previous reports showed that the Rh2 epimers demonstrated different pharmacological activities and only (20S)-ginsenoside Rh2 showed potent proliferation inhibition on cancer cells in vitro. However, the in vivo anti-hepatoma activity of (20R)-ginsenoside Rh2 and (20S)-ginsenoside Rh2 has not been reported yet. This work assessed and compared the anti-hepatoma activities of (20S)-ginsenoside Rh2 and (20R)-ginsenoside Rh2 using H22 a hepatoma-bearing mouse model in vivo. In addition, hematoxylin and eosin staining, the deoxynucleotidyl transferase dUTP nick-end labeling assay, and the semiquantitative reverse transcriptase polymerase chain reaction method were used to further study the apoptosis of the tumors. The results showed that both (20S)-ginsenoside Rh2 and (20R)-ginsenoside Rh2 suppressed the growth of H22 transplanted tumors in vivo, and the highest inhibition rate could be up to 42.2 and 46.8 %, respectively (p < 0.05). Further, hematoxylin/eosin staining and the deoxynucleotidyl transferase dUTP nick-end labeling assay indicated that both (20R)-ginsenoside Rh2 and (20S)-ginsenoside Rh2 could induce H22 hepatoma tumor cell apoptosis, with apoptosis indexes of 3.87 %, and 3.80 %, respectively (p < 0.05). Moreover, this effect was accompanied by downregulating the level of Bcl-2 mRNA. In conclusion, both (20S)-ginsenoside Rh2 and (20R)-ginsenoside Rh2 can suppress the growth of H22 hepatomas without causing severe side effects, and this effect is associated with the induction of apoptosis.

Transformation of trollioside and isoquercetin by human intestinal flora in vitro.

The present study was designed to determine the intestinal bacterial metabolites of trollioside and isoquercetin and their antibacterial activities. A systematic in vitro biotransformation investigation on trollioside and isoquercetin, including metabolite identification, metabolic pathway deduction, and time course, was accomplished using a human intestinal bacterial model. The metabolites were analyzed and identified by HPLC and HPLC-MS. The antibacterial activities of trollioside, isoquercetin, and their metabolites were evaluated using the broth microdilution method with berberine as a positive control, and their potency was measured as minimal inhibitory concentration (MIC). Our results indicated that trollioside and isoquercetin were metabolized by human intestinal flora through O-deglycosylation, yielding aglycones proglobeflowery acid and quercetin, respectively The antibacterial activities of both metabolites were more potent than that of their parent compounds. In conclusion, trollioside and isoquercetin are totally and rapidly transformed by human intestinal bacteria in vitro and the transformation favors the improvement of the antibacterial activities of the parent compounds.

Pharmacokinetics and tissue distributions of veratric acid after intravenous administration in rats.

The present study was designed to investigate the pharmacokinetics and tissue distributions of veratric acid following intravenous administration in rats. The concentrations of veratric acid in rat plasma at various times after administrated at doses of 2.5, 5, and 10 mg·kg(-1) were quantified by HPLC. The tissue distributions of veratric acid at various times after a single intravenous dose of 2.5 mg·kg(-1) were also analyzed. The plasma pharmacokinetic parameters at the three doses were as follows: t(1/2), (86.23 ± 6.83), (72.66 ± 4.10) and (71.20 ± 2.90) min; C0, (11.10 ± 1.47), (23.67 ± 1.24) and (39.17 ± 3.90) µg·mL(-1); and AUC(0→∞), (1 240.90 ± 129.14), (2 273.84 ± 132.47) and (3 516.4 ± 403.37) min·µg·mL(-1), respectively. The compound was distributed into tissues rapidly and extensively after intravenous administration and was mainly distributed into the liver, heart and kidneys.

Characterization of the intestinal absorption of seven flavonoids from the flowers of Trollius chinensis using the Caco-2 cell monolayer model.

The human Caco-2 cell monolayer model was used to investigate the absorption property, mechanism, and structure-property relationship of seven representative flavonoids, namely, orientin, vitexin, 2"-O-ß-L-galactopyranosylorientin, 2"-O-ß-L-galactopyranosylvitexin, isoswertisin, isoswertiajaponin, and 2"-O-(2"'-methylbutanoyl)isoswertisin from the flowers of Trollius chinensis. The results showed that these flavonoids were hardly transported through the Caco-2 cell monolayer. The compounds with 7-OCH3 including isoswertisin, isoswertiajaponin and 2"-O-(2"'-methylbutanoyl)isoswertisin were absorbed in a passive diffusion manner, and their absorbability was increased in the same order as their polarity. The absorption of the remaining compounds with 7-OH including orientin, vitexin, 2"-O-ß-L-galactopyranosylorientin, and 2"-O-ß-L-galactopyranosylvitexin involved transporter mediated efflux in addition to passive diffusion. Among the four compounds with 7-OH, those with a free hydroxyl group at C-2" such as orientin and vitexin were the substrates of P-glycoprotein (P-gp) and that with a free hydroxyl group at C-2' such as 2"-O-ß-L-galactopyranosylorientin was the substrate of multidrug resistance protein 2 (MRP2). The results of this study also implied that the absorbability of the flavonoids should be taken into account when estimating the effective components of T. chinensis.

[Study on Stability of Human Intestinal Bacterial Biotransformation Model].

UNLABELLED: Objective: To investigate the stability of human intestinal bacterial biotransformation model using isoquercetin as the substrate of transformation. METHODs: The in vitro transformation model was established using the intestinal bacteria form different volunteers, or different passages of the same volunteer in accordance with the "biotransformation model of human intestinal bacteria and its standard operating procedures" to transform isoquercetin. RESULTS: Within 24 hours, all models established with the intestinal bacteria from different volunteers could transform isoquercetin to quercetin and the transformation efficiency was inclined to increase with the increase of the number of culture passages. CONCLUSION: The intestinal bacterial model established in accordance with the "standard operating procedures" is stable and the results obtained with this model are reproducible, which demonstrats the suitability of this model for the investigation of the chemical constituents of Chinese medicinal materials.

Chromatographic fingerprint analysis of the floral parts of Trollius chinensis.

This study provided a practical procedure, for the first time, to compare the component difference of the floral parts of Trollius chinensis and identify the characteristic peaks of each floral part using the high-performance liquid chromatographic fingerprint technique followed by similarity analysis. The results showed that the constituents of different floral parts exhibited lower similarity than those of the same part. It can be concluded that the procedure established herein is useful for analysis of variability in constituent distribution of herbal drugs, and the components are unevenly distributed in the floral parts of T. chinensis.

Absorption properties and mechanism of trolline and veratric acid and their implication to an evaluation of the effective components of the flowers of Trollius chinensis.

AIM: To study the absorption properties and mechanism of two important components, trolline and veratric acid, from the flowers of Trollius chinensis, in order to better understand the contribution of these two compounds to the effectiveness of these flowers. METHOD: The human Caco-2 cell monolayer model was employed to study the transport of trolline and veratric acid from apical side (AP) to basal side (BL), and from BL to AP by determining the transport rates as the function of time and concentration and calculating apparent permeability coefficients (Papp). RESULTS: Trolline and veratric acid were transported across Caco-2 cell monolayer through different mechanisms in a concentration dependent manner. Trolline was transported at a Papp level of 10(-6) cm·s(-1) with a Papp AP→BL/Papp BL→AP ratio of more than 1.8 or less than 0.8, while veratric acid was transported at a Papp level of 10(-5)cm·s(-1) with a Papp AP→BL/Papp BL→AP ratio of close to 1.0. CONCLUSION: Trolline is moderately absorbed through an associative mechanism involving active and passive transport, and veratric acid is well-absorbed mainly through passive diffusion. These factors should be taken into account when chemically assessing the pharmacodynamic material basis of the flowers of T. chinensis.

Activity directed investigation on anti-inflammatory fractions and compounds from flowers of Trollius chinensis.

The flower of Trollius chinensis Bunge is used as an anti-inflammatory drug to treat upper respiratory tract infection, pharyngitis, tonsillitis, and bronchitis. In order to identify the active components, the activity-screen directed compound isolation was carried out, leading to the identification of the major active fraction and 4 compounds thereof. As a result, flavonoids and phenolics were demonstrated to be the major anti-inflammatory components.