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Copyright of Chinese Journal of Oil Crop Sciences is the property of Oil Crops Research Institute of Chinese Academy of Agricultural Sciences and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Xanthium strumarium is a traditional folk medicinal plant. The 50% ethanol eluting faction of X. mongolicum had significant activity to inhibit necroptosis. In order to investigate the active constituents, the active fraction of X. mongolicum were isolated and purified by various chromatographic methods such as repeated silica gel column chromatography, Sephadex LH-20 column chromatography, preparative high performance liquid chromatography and recrystallization. Their structures were established on the basis of NMR, MS spectraoscopic analyses and comparison with lirerature date. The results were as follows: A total of 14 compounds were isolated from the active part and identified as hydroxydihydrobovolide(1), raspberry ketone(2), salicyl alcohol(3), 4-hydroxyl-acetophenone(4), 4-hydroxybenzaldehyde(5), ethyl caffeate(6), ferulaldehyde(7), isoscopletin(8), 3,3′-bis(3,4-dihydro-4-hydroxy-6-methoxy-2H-1-benzopyran)(9), axillarin (10), quercetin (11), (+) pinoresinol(12), β-sitosterol(13) and palmatic acid(14). Compounds 1-4, 7-10 were all isolated from Xanthium mongolicum for the first time.

Objective　To investigate the active ingredients and components that inhibiting cathepsin K activity in Erzhi Wan, a classic kidney-tonifying formula. Methods　Then-butanol, dichloromethane, ethyl acetate and petroleum ether parts and 30 active components in Erzhi Wan were screened by established high throughput fluorescence methods of inhibit the binding activity of CTSK with Z-FR-MCA substrate, the formation of CTSK and chondroitin sulfate A (CSA) complex activity, and the activity of substrate type I collagen degradation by CTSK. Molecular docking and insoluble collagen substrate binding assays were applied to verify the potential CTSK inhibitors. Results　The n-butanol and petroleum ether parts of Erzhi Wan inhibited the formation of CTSK and CSA* complex by more than 90%, the petroleum ether part inhibited the binding of CTSK to substrate Z-FR-MCA by more than 90%, the collagen degradation inhibition rate of CTSK in n-butanol part was more than 95% and that in petroleum ether part was 58.6%. Among the 30 active components, 11 showed that the inhibition rate of CTSK and CSA* complex formation was more than 50%, and 5 components with the inhibition rate of Z-FR-MCA binding activity more than 50%. Finally, there were four components including eclalbasaponin Ⅸ, (-)-epicatechin gallate, nuezhenoside and wedelolactone. The inhibition rate of collagen degradation was more than 50%. Eclipta saponin IX inhibited the binding rate between collagen fibers and CTSK, up to 60%, but all of them failed to dock with CTSK active site. Conclusion　There are active components that inhibiting cathepsin K in Erzhi Wan, which mainly exists in the n-butanol ingredients, but the active components is not an active-site inhibitor. It might inhibit the binding of CTSK with oligosaccharides by binding to other sites of CTSK, and then reduce the collagen degradation activity of CTSK. [ABSTRACT FROM AUTHOR]

Xanthium strumarium is a traditional folk medicinal plant. The 50% ethanol eluting faction of X. mongolicum had significant activity to inhibit necroptosis. In order to investigate the active constituents, the active fraction of X. mongolicum were isolated and purified by various chromatographic methods such as repeated silica gel column chromatography, Sephadex LH-20 column chromatography, preparative high performance liquid chromatography and recrystallization. Their structures were established on the basis of NMR, MS spectraoscopic analyses and comparison with lirerature date. The results were as follows: A total of 14 compounds were isolated from the active part and identified as hydroxydihydrobovolide(1), raspberry ketone(2), salicyl alcohol(3), 4-hydroxyl-acetophenone(4), 4-hydroxybenzaldehyde(5), ethyl caffeate(6), ferulaldehyde(7), isoscopletin(8), 3, 3'-bis(3, 4-dihydro-4-hydroxy-6-methoxy-2H-1-benzopyran)(9), axillarin(10), quercetin(11), (+)pinoresinol(12), β-sitosterol(13)and palmatic acid(14). Compounds 1-4, 7-10 were all isolated from Xanthium mongolicum for the first time. [ABSTRACT FROM AUTHOR]

Extracts from sponge-associated fungus Trichoderma longibrachiatum have been studied and contain antibacterial compounds which can inhibit several pathogenic multidrug-resistant organisms. This study aims to determine the active fraction of the extract which is antibacterial against the gram-negative Multi Drug-Resistant Klebsiella. pneumoniae pathogen and gram-positive Methicillin-Resistant Staphylococcus aureus. In this study, the fungus was cultivated using solid media of malt extract agar (MEA) for 6-9 days (24 hours dark, static, pH 5.6, 60 ‰ salinity, and 27°C). The mycelia and media were macerated by methanol and then partitioned using ethyl acetate. Active fraction tracing was carried out using the bioautography method and then isolated by the open column chromatography method. Antibacterial activity testing was done using the Broth Dilution method to determine the Minimum Inhibitory Concentration (MIC). The results of the study showed that ethyl acetate extract contained one active fraction (Rf value = 0.14), which has reactive characteristics on vanillin reagent and absorbed ultraviolet light (λ 375.5 nm absorbance peak). The active fraction was able to inhibit the growth of MDR K. pneumoniae and MRSA bacteria at the same MIC value, i.e. 256 μg mL-1. In conclusion, an active fraction of T. longibrachiatum can be developed as an antibacterial against MDR K. pneumoniae and MRSA. [ABSTRACT FROM AUTHOR]

This study aimed to explore active fraction of Smilacina japonica A.Gray with antifungal activity and its antifungal mechanisms.The rhizomes of Smilacina japonica A.Gray was extracted with 75% ethanol under reflux.Then the extract was partitioned with petroleum ether, ethyl acetate, n-butanol and water successively.Microdilution method, growth test, time-killing curve study, anti-biofilm formation assay and checkerboard microdilution assay were used to investigate the antifungal and antibiofilm activities of extracts of Smilacina japonica A.Gray.Spot assay and confocal laser scanning microscope were used to explore its antifungal mechanisms.n-butanol extract of Smilacina japonica A.Gray showed potent antifungal and antibiofilm activities with MICs ranged from 104 μg/mL to 832 μg/mL,and its MICs were lower than the concentration of its cytotoxicity.In addition, n-butanol extract of Smilacina japonica A.Gray dispalyed antifungal synergism with amphotericin B and anidulafungin.After treated with n-butanol extract of Smilacina japonica A.Gray, the sensitivities of fungi to cell wall inhibitors and amphotericin B were increased, and the chitin content was also augmented.Therefore, The n-butanol extract of Smilacina japonica A.Gray was its active fraction with antifungal activities, and its antifungal mechanism might be related to the effect on the cell wall and the increase of chitin content. [ABSTRACT FROM AUTHOR]

Elucidation of the inhibitory effects of humic substances (HSs) on phytopathogenic fungi and the underlying molecular mechanisms are highly important for improved biocontrol. In this study, we investigated the growth suppression, morphological characteristics, transcriptomic sequence, and radical signals of Rhizoctonia solani following HS addition (50 mg/L). Through mycelial cultured experiment, mycelia growth of R. solani had been suppressed with HS addition, and the inhibition rate was 24.88 ± 0.11% compared to the control. Field emission-scanning electron microscopy showed increased and superimposed branching mycelial growth, with a shriveled appearance. RNA samples of R. solani cultured with or without HSs were both extracted to examine the sequence on molecular level by Illumina HiSeq sequencing platform. RNA sequencing analysis revealed 175 differentially expressed genes (DEGs; 111 upregulated and 64 downregulated) between the HSs treatment and control. The upregulated unigenes were annotated and significantly enriched to three molecular processes: vitamin B6 metabolism, ABC transporters, and glutathione metabolism, while the downregulated unigenes were annotated to carbohydrate metabolism, but not significantly enriched. Real time-quantitative polymerase chain reaction analysis showed that the unigenes related to hexokinase, glucose-6-phosphate isomerase, glutathione synthase, and glutathione reductase were significantly decreased (by 60.03%, 70.70%, 60.33%, and 57.59%, respectively), while those related to glutathione S-transferase were significantly increased (2.66-fold). The electron paramagnetic resonance spectra showed that HSs induced increased the intensity of radical signals of R. solani in a cultured system increased by 59.56% compared to CK (without HSs addition). Network analysis based on DEGs expression and the chemical structure of HSs revealed that the carbonyl moiety in HSs formed the most links with nodes of the DEGs (sum of the links of positive and negative effects = 70), implicating this structure as the active fraction responsible for the inhibitory effect. This study provides molecular and chemical evidence of the biofungicidal activity of HSs with the potential for practical application.

The leaf decoction of Sesbania sesban var. bicolor is used traditionally by Santhal tribe of Assam, India, for the treatment of intestinal helminthic infections. This study was conducted to evaluate the in vitro and in vivo anthelmintic efficacy of methanolic extract of S. sesban var. bicolor leaves using Hymenolepis diminuta-rat (cestode) and Syphacia obvelata-mice (nematode) as test parasites and models. Praziquantel (PZQ) and albendazole (ABZ) were used as reference drugs. At the highest concentration of 30 mg/ml of the plant extract, H. diminuta and S. obvelata showed mortality at 0.81 ± 0.01 h and 15.17 ± 0.05 h, respectively. The in vivo results substantiated the in vitro findings, and the extract showed a better cestocidal efficacy in a dose-dependent manner, whereby treatment of rats with 400 mg/kg of the plant extract caused 65.10% reduction in eggs per gram (EPG) of faeces and 56% reduction in worm counts. S. obvelata-infected mice treated at the same dose showed 34.32% and 47.08% reduction in EPG and worm counts at necropsy, respectively. The methanolic extract was subjected to bioassay-guided fractionation using different solvents and the ethyl acetate fraction proved to be the most active. This active fraction was subjected to column chromatography using varying concentrations of hexane:ethyl acetate. Maximum efficacy was observed in 7:3 hexane:ethyl acetate, where H. diminuta and S. obvelata showed mortality at 3.56 ± 0.12 h and 9.21 ± 0.02 h, respectively. This indicates that the isolated fraction contained the active component responsible for its anthelmintic activity, which substantiates the medicinal usage in traditional practice. [ABSTRACT FROM AUTHOR]

Dayak Onion (Eleutherine palmifolia) is a widely available plant in Kalimantan which has never been optimally analyzed for its significant. The aim of this research was to determine the active fraction of Dayak Onion (Eleutherine palmifolia) which possesses antioxidant activity. Antioxidant testing was carried out quantitatively with 5 test preparations namely: total ethanol extract, n-hexane fraction, chloroform fraction, ethyl acetate fraction, and ethanol fraction, were carried out using UV-Visible spectrophotometry through DPPH reagent to obtain IC50 Inhibition concentration. The test data results were processed with descriptive analysis. Furthermore, active fraction selected Brine Shrimp Lethality Test (BSLT) was carried out to determine the value of lethal concentration LC50 on shrimp larvae to see the toxicity category. The results showed that the chloroform fraction was an active fraction which had an IC50 of 20.29 ppm (very high category) which was active fraction h. BSLT Test Chloroform fraction has an LC50 value of 527.229 (medium category). In conclusion, Dayak Onion (Eleutherinepalmifolia) which can be widely found in East Kalimantan, Indonesia, is a powerful plant to be an alternative of antioxidant sources. [ABSTRACT FROM AUTHOR]

Copyright of Acta Edulis Fungi is the property of Acta Edulis Fungi and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Lysimachia ramosa (Primulaceae) is a traditionally used medicinal plant, leaves extract of which is being widely used by the Jaintia tribes of Meghalaya, India for controlling helminthiasis. Preliminary investigation carried out on helminth parasites revealed that the crude extract of the plant causes deformity in the surface topography leading to death of the parasites. Therefore, the present study was conducted to identify the specific fraction of the crude leaf extract of the plant responsible for cestocidal efficacy, through biochemical and ultrastructural studies in Raillietina echinobothrida exposed to crude extract and its different fractions namely hexane, chloroform, ethyl acetate and n-butanol. A dose dependent efficacy, with highest rate of mortality among n-butanol exposed parasites was recorded. The treated parasites exhibited complete erosion of microtriches from the tegument, disintegration of muscle bundles, cellular organelles, plasma membrane, nuclear membrane, nucleolus and vacuolization of mitochondria was also observed. Observations on histochemical distribution of some important tegumental enzymes like adenosine triphosphatase (ATPase), alkaline phosphatase (AlkPase), acid phosphatase (AcPase) and 5′Nucleotidase (5′-Nu) revealed a marked diminished stain intensity in the tegument of R. echinobothrida exposed to the crude extract and n-butanol fraction of the crude extract compared to the control. Highest reduction (77.93%) in the activity of ATPase was observed when the parasites exposed to 6 mg n-butanol fraction/ml of PBS. The results suggest that these enzymes act as target for anthelmintic stress caused by the phytochemicals present in the plant. [ABSTRACT FROM AUTHOR]

Copyright of Journal of Zhejiang University: Science B is the property of Springer Nature and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Primarily using cropped systems, previous studies have reported a positive linear relationship between microbial biomass carbon (MBC) and soil organic carbon (SOC). We conducted a meta-analysis to explore this relationship separately for grasslands and croplands using available literature. Studies were limited to those using fumigation-extraction for MBC for field samples. Trials were noted separately where records were distinct in space or time. Grasslands were naturally occurring, restored, or seeded. Cropping systems were typical of the temperate zone. MBC had a positive linear response to increasing SOC that was significant in both grasslands (p < 0.001; r 2 = 0.76) and croplands (p < 0.001; r 2 = 0.48). However, MBC increased 2.5-fold more steeply per unit of increasing SOC for grassland soils, as compared to the corresponding response in cropland soils. Expressing MBC as a proportion of SOC across the regression overall, slopes corresponded to 2.7% for grasslands and 1.1% for croplands. The slope of the linear relationship for grasslands was significantly (p = 0.0013) steeper than for croplands. The difference between the two systems is possibly caused by a greater proportion of SOC in grasslands being active rather than passive, relative to that in croplands, with that active fraction promoting the formation of MBC. [ABSTRACT FROM AUTHOR]

Ethnopharmacological relevance In traditional Chinese medicines, osteoporosis was considered to be induced by the deficiency of kidney's function. The Rhizoma of Dioscorea spongiosa was one of the kidney tonifying and bone strengthening agent in the traditional usage and previous study had shown that its 90% ethanol fraction was effective on anti-osteoporosis using the ovariectomized (OVX) rats. However, for the secondary osteoporosis, like glucocorticoid-induced osteoporosis (GIO), its effect was still unknown. Materials and methods The GIO model was established by injecting dexamethasone into the muscles of rats. The 90% ethanol extraction of Dioscorea spongiosa (DSE) were administrated to rats in three different dosages, 125, 250 and 500 mg/Kg/d, respectively. After the administration, the rats were sacrificed to measure different kinds of indicators, including the biochemical indexes in urine and serum, the bone tissue metrology, BMC and BMD, biomechanical indicators and histological changes. Results DSE could significantly reduce the content of BGP, ALT, TRAcP, HOP/Cr and Ca/Cr, increase the content of P/Cr compared with the control group, suggesting that DSE is effective on controlling the excessive transition of bones and inhibiting the bone resorption. By the administration of DSE, the dry bone weight/volume, ash weight/volume, the content of Ca, BMD and BMC were also obviously increased, suggesting that DSE could increase the bone mass by increasing its Ca content. Besides, the flexure strength and maximum bending force could be improved by DSE, suggesting that it could strengthen the hardness and strength of bones. In the histological investigation, DSE could repair the broken of cancellous bones and bone trabecular with the similar activity with XLGB. Conclusions The results showed that DSE is effective on inhibiting GIO in rats by improving the bone tissue metrology, BMC and BMD as well as biomechanical indicators, and also repairing the microscopic changes of cancellous bones and trabecular bones. The mechanism was related to the inhibition of excessive bone transition and bone resorption according to the changes of biochemical indexes. [ABSTRACT FROM AUTHOR]

[Objective] to screen the anti-inflammatory fraction from HERBA COMMELINAE. [Methods] Anti-inflammatory fraction was screened by using mice auricle swelling model induced by xylene, mice abdominal capillary permeability model induced by glacial acetic acid, rats pedal swelling model induced by carrageenan, and effects on PGE2 in inflammatory tissue of rats pedal edema induced by carrageenan. [Results] Compared with 5% Tween-80 group, the high- and middle dosage groups (30, 15 g/kg) of water fraction had significantly inhibitory effects on mice auricle swelling induced by xylene, mice abdominal capillary permeability induced by glacial acetic acid, rats pedal swelling induced by carrageenan, and PGE2 in inflammatory tissue of rats pedal edema induced by carrageenan (P <0. 05, 0. 01) . Other fractions had weak or basically no activities. [Conclusions] Water fraction was the anti-inflammatory active fraction of HERBA COMMELINAE. [ABSTRACT FROM AUTHOR]

Background: Sophora belongs to the family of Fabaceae and the species in this genus are currently used as a folklore medicine for preventing a variety of ailments including cancer. Our aim was to identify and validate an anticancer compound from Sophora interrupta using multi-spectroscopic, anticancer screening, and molecular docking approach. Methods: The cytotoxicity of the various solvent extracts, petroleum ether, n-butanol, and ethyl acetate (EtOAc) of the S. interrupta root powder was evaluated in a breast cancer cell lines (MCF-7). The extract that had anticancer activity was subjected to column chromatography based on the polarity of the solvents. The anticancer activity of the elution fractions was validated using a 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. The isolated metabolite fraction with anticancer activity was run through a C18 column isocratic and gradient high-performance liquid chromatography (HPLC). The structure of the isolated compound was characterized using ¹H nuclear magnetic resonance (NMR), 13C-NMR, Fourier transform infrared spectroscopy, and liquid chromatography-mass spectrometer methods. Results: The crude EtAOc extract effectively inhibited the proliferation of MCF-7 cells. The column eluted chloroform and EtOAc (4:6) fraction of the EtOAc extract showed significant anticancer activity in the MCF-7 cells compared with normal mesenchymal stem cells. This fraction showed three major peaks in the HPLC chromatogram and the first major peak with a retention time (RT) of 7.153 was purified using preparative-HPLC. The structure of the compound is a piceatannol, which is a metabolic product of resveratrol. Piceatannol formed direct two hydrogen bond interactions between Cys912 (2H), and Glu878 of vascular endothelial growth factor receptor 1 (VEGFR1) with a glide-score (G-score) of -10.193, and two hydrogen bond interactions between Cys919, and Asp1046 of VEGFR2, with a G-score of -8.359. The structure is similar to that of the crystallized protein for VEGFR1 and R2. Conclusions: Piceatannol is a secondary metabolite of S. interrupta that has anticancer activity. Moreover, piceatannol has been isolated for the first time from S. interrupta. [ABSTRACT FROM AUTHOR]

Primarily using cropped systems, previous studies have reported a positive linear relationship between microbial biomass carbon (MBC) and soil organic carbon (SOC). We conducted a meta-analysis to explore this relationship separately for grasslands and croplands using available literature. Studies were limited to those using fumigation–extraction for MBC for field samples. Trials were noted separately where records were distinct in space or time. Grasslands were naturally occurring, restored, or seeded. Cropping systems were typical of the temperate zone. MBC had a positive linear response to increasing SOC that was significant in both grasslands (p < 0.001; r2 = 0.76) and croplands (p < 0.001; r2 = 0.48). However, MBC increased 2.5-fold more steeply per unit of increasing SOC for grassland soils, as compared to the corresponding response in cropland soils. Expressing MBC as a proportion of SOC across the regression overall, slopes corresponded to 2.7% for grasslands and 1.1% for croplands. The slope of the linear relationship for grasslands was significantly (p = 0.0013) steeper than for croplands. The difference between the two systems is possibly caused by a greater proportion of SOC in grasslands being active rather than passive, relative to that in croplands, with that active fraction promoting the formation of MBC.

[Objective] To screen the anti-inflammatory active fractions from RADIX ET RHIZOMA GENTIANAE. [Methods] Anti-inflammatory activity screening was carried out based on mice auricle swelling model induced by xylene, capillary permeability model in mice abdominal cavity induced by glacial acetic acid, rats footpad swelling model induced by carrageenan and PGE2 model in inflammatory tissues of rats swelling foot induced by carrageenan. [Results] Compared with Tween-80 group, high-and middle-dosage groups of water fractions (6, 3 g/kg) had significant inhibitory effects on mice auricle swelling induced by xylene, capillary permeability in mice abdominal cavity induced by glacial acetic acid, rats footpad swelling induced by carrageenan, and PGE2 in inflammatory tissues of rats swelling foot induced by carrageenan (P <0. 05, 0. 01). Other fractions showed weak or basically no activities. [Conclusions] Water fraction was the anti-inflammatory active fraction of RADIX ET RHIZOMA GENTIANAE. [ABSTRACT FROM AUTHOR]

The total saponin from the stem bark of Albizia julibrissin (AJS t ) has previously showed the adjuvant potentials in mice. In this study, AJS t was subjected to resin column chromatography to afford four fractions (AJS 30 , AJS 50 , AJS 75 and AJS 95 ), and these fractions were further compared for the hemolytic activities and adjuvant potentials on the immune response to ovalbumin (OVA) and recombinant fowl pox virus vector-based avian influenza vaccine (rFPV). AJS t , AJS 50 , AJS 75 and AJS 95 showed a slight hemolytic effect. AJS t , AJS 50 and AJS 75 significantly enhanced not only the concanavalin A (Con A)-, lipopolysaccharide (LPS)- and antigen-stimulated splenocyte proliferation, but also serum antigen-specific IgG, IgG1, IgG2a and IgG2b antibody titers in the mice immunized with OVA and rFPV. AJS t , AJS 50 and AJS 75 also significantly promoted the NK cell activity and delayed-type hypersensitivity (DTH) in the OVA-immunized mice. Furthermore, the mechanisms of adjuvant action were explored by determining the effects of AJS 75 on cytokines and chemokines at the site of injection using antibody array. AJS75 induced or up-regulated the protein expression of 12 cytokines (IL-12p40, IL-12p40/p70, IFN-γ, IL-13, IL-1β, IL-6, IL-10, TNF-α, sTNFR I, sTNFR III, IL-3 and IL-9) and 10 chemokines (Eotaxin, I-TAC, MIG, MIP-1α, RANTES, TECK, Fracatlkine, FasL, M-CSF and GM-CSF) in the injected muscles. The results suggested that AJS 75 , the most adjuvant-active fraction of AJS t , could improve antigen-specific both cellular and humoral immune responses and simultaneously elicit a Th1/Th2 response by inducing cytokine and chemokine at the site of injection. [ABSTRACT FROM AUTHOR]

Background: Acacia farnesiana is a medicinal plant that grows throughout tropical parts of Indian subcontinent, particularly in sandy soils of river beds in Northern India. The objective of the present study was to evaluate the anti-hyperglycemic activity of the extracts using glucose tolerance test. Isolation of an active fraction (AF) from the active extract (water extract) using alcohol precipitation and to get insight to the mechanism of action of the AF of A. farnesiana. Materials and Methods: Glucose uptake by isolated rat diaphragm of the AF was performed. Further the effect of release of Insulin from isolated and cultured pancreatic β-cell was determined. Besides, effect of oral administration of the AF was compared with that of intraperitonial administration. The effect of AF on serum glucose levels in orally glucose loaded rats was compared with that of intraperitoneal glucose loaded rats. Results: The water extract significantly lowered the blood glucose level. When precipitated with alcohol, the activity was found in the soluble fraction. Glucose uptake in the isolated rat hemidiaphragm, was increased by the AF at 40 μg/ml concentration, the AF did not significantly influence insulin release from cultured islets. The AF was found to be effective in orally glucose loaded in contrast to intraperitonial route. Conclusion: Our findings suggest that this plant is promising for further studies leading to the development of valuable medicine for diabetes. [ABSTRACT FROM AUTHOR]

Background: Sophora belongs to the family of Fabaceae and the species in this genus are currently used as a folklore medicine for preventing a variety of ailments including cancer. Our aim was to identify and validate an anticancer compound from Sophora interrupta using multi-spectroscopic, anticancer screening, and molecular docking approach. Methods: The cytotoxicity of the various solvent extracts, petroleum ether, n-butanol, and ethyl acetate (EtOAc) of the S. interrupta root powder was evaluated in a breast cancer cell lines (MCF-7). The extract that had anticancer activity was subjected to column chromatography based on the polarity of the solvents. The anticancer activity of the elution fractions was validated using a 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. The isolated metabolite fraction with anticancer activity was run through a C18 column isocratic and gradient high-performance liquid chromatography (HPLC). The structure of the isolated compound was characterized using 1 H nuclear magnetic resonance (NMR), 13 C-NMR, Fourier transform infrared spectroscopy, and liquid chromatography-mass spectrometer methods. Results: The crude EtAOc extract effectively inhibited the proliferation of MCF-7 cells. The column eluted chloroform and EtOAc (4:6) fraction of the EtOAc extract showed significant anticancer activity in the MCF-7 cells compared with normal mesenchymal stem cells. This fraction showed three major peaks in the HPLC chromatogram and the first major peak with a retention time (RT) of 7.153 was purified using preparative-HPLC. The structure of the compound is a piceatannol, which is a metabolic product of resveratrol. Piceatannol formed direct two hydrogen bond interactions between Cys912 (2H), and Glu878 of vascular endothelial growth factor receptor 1 (VEGFR1) with a glide-score (G-score) of −10.193, and two hydrogen bond interactions between Cys919, and Asp1046 of VEGFR2, with a G-score of −8.359. The structure is similar to that of the crystallized protein for VEGFR1 and R2. Conclusions: Piceatannol is a secondary metabolite of S. interrupta that has anticancer activity. Moreover, piceatannol has been isolated for the first time from S. interrupta.

In our previous report (J Pharmaceut Biomed 56 (2011) 443-447), a support vector machine (SVM)-based pharmacodynamic model was established for predicting active fractions of herbal medicines (HMs), where information contents embedded in the chromatograms of the fractions were represented with the peak areas. However, in this representation the global characteristics of the chromatograms were completely missed, which is definitely contrary to the global and holistic views in theories of HMs and undoubtedly reduce the success rate of this model. To deal with the challenge, two chemometrics methods, that is, minimum redundancy maximum relevance ( mRMR) and particle swarm optimizer (PSO), were applied in this article for feature selection of the whole chromatograms, and the PSO was also used to tune the SVM parameters. As a case, a sample HM, that is, Xiangdan injection, was investigated. The predictive accuracy was fully evaluated and compared with those by other popular and reported methods. Furthermore, the confirmation on the independent predicting set exhibited that the predicted bioactivities were well consistent with the experimental values. The important potential application of the present model is to be extended to help search active fractions of other HMs. [ABSTRACT FROM AUTHOR]

Abstract: Ethnopharmacological relevance: Xiaoyaosan (XYS), a well-known formula for relieving depression, was originated from the book of “Taiping Huimin Heji Jufang” in Song Dynasty (960–1127 AD), composed of Radix Bupleuri, Radix Angelicae Sinensis, Radix Paeoniae Alba, Rhizoma Atractylodis Macrocephalae, Poria, Herba Menthae, Rhizoma Zingiberis Recens and Radix Glycyrrhizae with dose proportion of 6:6:6:6:6:3:2:2. It is commonly used for the treatment of depression-related syndromes in China. In the formula, Radix Bupleuri usually serves as the principal drug, Radix Angelicae Sinensis and Radix Paeoniae Alba serve as the ministerial drugs, Rhizoma Atractylodis Macrocephalae, Poria, Herba Menthae and Rhizoma Zingiberis Recens serve as adjunctive drugs, Radix Glycyrrhizae serves as messenger drug, they coordinate with each other and enhance the effect of the formula. In our previous experiments, the antidepressant effect of XYS was revealed. However, the antidepressant part (or component) of this prescription was still obscure. Materials and methods: An experimental despair animal model: the mice tail suspension test (TST) was used to evaluate the antidepressant activity of XYS and its fractions. GC–MS method was developed to identify the volatile components and determine 4 major volatile components in active fraction. Results: In the TST test, the effect of a low polar fraction (XY-EA) was superior to other fractions of XYS. 13 volatile compounds in the XY-EA were identified on the basis of standards, isolation and structural determination in our laboratory, NIST 05 database and literature data. The content of 4 major volatile compounds in XY-EA which is 6.703%. Conclusions: The petroleum ether fraction (XY-EA) appears to be the active fraction of XYS. 4 major components Z-ligustilide, palmitic acid, atractylenolide I, and atractylenolide II may be the antidepressant active compounds. [Copyright &y& Elsevier]

Abstract: Herbal medicine has been successfully applied in clinical therapeutics throughout the world. In this paper, various information contents in addition to a best-first search strategy are proposed for improving prediction quality of quantitative profile–efficacy relationship (QPER). As a demonstration, a QPER model was constructed to predict the blood-clotting time increasing effect of Naodesheng prescription, a widely used herbal medicine in China. Evaluated by both the self-consistency test and the rigorous jackknife test, the predictive accuracy was increased by feeding the model with the merged information contents compared to only with the common chromatographic peak areas. The confirmation experiment exhibited that the predicted blood-clotting time were well consistent with the observed values. Furthermore, it has not escaped from our notice that the important potential application of the current QPER model is to be extended to help search active fractions, which has attracted more and more attention in the re-developments of herbal medicines based on the active compounds. [Copyright &y& Elsevier]

Achyranthes bidentata Blume is a commonly prescribed Chinese medicinal herb. Our previous studies have proved the neuroprotective function of Achyranthes bidentata polypeptides (ABPP), a major constituent from aqueous extracts of the herb. Now we have separated an active fraction, referred to as ABPP-E4, from ABPP by HPLC methods. This study aimed to investigate the possible therapeutic potential of ABPP-E4. Assessments of cell viability and apoptosis indicated that ABPP-E4 pretreatment, in a concentration-dependent manner, antagonized the cell viability loss and cell apoptosis of cultured SH-SY5Y cells deprived of serum. ABPP-E4 pretreatment also resulted in increase of Bcl-2/Bax ratio and inhibition of caspase-3 activation in the cells on exposure to serum deprivation. Signaling pathway analysis indicated that ABPP-E4 treatment stimulated the activation of Akt/Gsk3β signaling in cultured SH-SY5Y cells, and anti-apoptotic effects of ABPP-E4 could be blocked by chemical inhibition of PI3K. Taken together, all the results suggest that ABPP-E4 might exert protective effects against serum deprivation-induced neuronal apoptosis through modulation of PI3K/Akt/Gsk3β pathways. [ABSTRACT FROM AUTHOR]

Abstract: The complex chemical composition of herbal medicine leads to the lack of appropriate method for identifying active compounds and optimizing the formulation of herbal medicine. One of the most commonly used method is bioassay-guided fractionation. However, if the herbal medicine was divided into many fractions, it would cost much money and time in carrying out such a full bioassay. So, can we just perform the bioassay of a few fractions, and then develop a method to predict the bioactivities of other fractions? This study is designed to try to answer the question. In this work, a support vector machine (SVM) pharmacodynamic prediction model was introduced to search active fraction and ingredients of Naodesheng prescription. The prescription was first divided into five extracts, yielding a total of 25 =32 combinations. Anti-platelet aggregation experiment with SD rats was just carried out on 16 combinations. The effects of the remained 32−16=16 combinations were then predicted by the SVM model. The prediction quality was evaluated by both the rigorous jackknife test and the independent dataset validation test. Furthermore, the present method was compared with the frequently used MLR, PCR and PLSR. The present method outperforms the other 3 methods, yielding: RMSECV=2.40, R =0.895 by the jackknife test and RMSEP=7.41, R =0.910 by the independent dataset test. It indicates that the SVM prediction model has good accuracy and generalization ability. The active fraction and ingredients of Naodesheng prescription were then predicted by the model. It is believed that the present model can be extended to help search the active fraction and ingredients of other herbal medicines. [Copyright &y& Elsevier]

Abstract: Ethnopharmacological relevance: Xiaoyaosan (XYS), composed of Radix Bupleuri, Radix Angelicae Sinensis, Radix Paeoniae Alba, Rhizoma Atractylodis Macrocephalae, Poria, Herba Menthae, Rhizoma Zingiberis Recens and Radix Glycyrrhizae, is a valuable traditional Chinese medicine (TCM) which is used for the treatment of depression in China. In the formula, Radix Bupleuri usually serves as the principal drug, Radix Angelicae Sinensis and Radix Paeoniae Alba serve as the ministerial drugs, Rhizoma Atractylodis Macrocephalae, Poria, Herba Menthae and Rhizoma Zingiberis Recens serve as adjunctive drugs, Radix Glycyrrhizae serves as messenger drug, they coordinate with each other and enhance the effect of the formula. In our previous experiments, the antidepressant effect of XYS was revealed. However, the antidepressant part (or component) of this prescription was still obscure. We divided the XYS into five different polar fractions, and explored the antidepressant activity of five different polar fractions to identify the active fraction. Materials and methods: Behavior research and metabonomics method based on 1H NMR were used for efficacy study of different fractions in chronic unpredictable mild stress (CUMS) model of depression. Rats were divided into 8 groups and drugs were administered during the 21 days model building period. The urine samples of rats were collected overnight (12h) on 21 day and the metabolic profiling of the urine was measured using NMR. Multivariate analysis was also utilized to evaluate the active fraction of XYS. Results: In the behavior research, there were significant difference between the lipophilic fraction group (XY-A) and the model group. In addition, with pattern recognition analysis of urinary metabolites, the results showed a clear separation of the model group and control group, while XY-A group was much closer to the control group in the OSC-PLS score plot. Seven endogenous metabolites contributing to the separation of the model group and control group were detected, while XY-A group regulated the 5 perturbed metabolites showing a tendency of recovering to control group. Conclusions: The present work suggested that petroleum ether fraction was the most effective fraction, implying that lipophilic components contribute to the antidepressant effect of XYS. [Copyright &y& Elsevier]

Abstract: Ethanolic extract prepared from the seeds of Vernonia anthelmintica was evaluated for its antihyperglycemic activity in STZ (Streptozotocin) induced diabetic rats. Administration of ethanolic extract at a dosage of 0.50g/kgbw produced the maximum fall (82%) in the blood glucose levels in diabetic rats after 6h of treatment. Bioassay-directed fractionation using silica gel column chromatography was performed. Among the five fractions (A1, B1, C1, A2 and B2) obtained, of an initial chromatographic separation of the ethanolic extract, fraction A2 (100mg/kgbw) showed the maximum antihyperglycemic activity which is significantly higher than that of the reference drug glibenclamide (20mg/kgbw). Administration of the active fraction (100mg/kgbw) for 45days resulted in significant reduction in plasma glucose, HbA1C, cholesterol, triglycerides, LDL, VLDL, free fatty acids, phospholipids and HMG-CoA reductase in STZ diabetic rats. In addition to that, significant decrease in plasma insulin, protein, HDL and hepatic glycogen observed in STZ diabetic rats, was normalized after 45days of treatment with the active fraction of V. anthelmintica seeds. From the present study, it is evident that, the seeds of V. anthelmintica possess significant antidiabetic and antihyperlipidemic property without evident toxic effects. [Copyright &y& Elsevier]

Abstract: Ethnopharmacological relevance: The herbal formula Xiangdan injection and its modifications have been used in traditional Chinese medicine for about hundreds years to alleviate pain and promoting blood. Aim: To investigate the anti-hypoxia active fraction of Xiangdan injection. Materials and methods: Xiangdan injection was extracted by ligarine, chloroform, acetic ether, n-butanol and water, represented respectively by A, B, C, D and E. Five extractions were group on the L12(25) orthogonal designed table. NIH mices anti-hypoxia experiment under normal pressure with rats was adopted on the basis of orthogonal design, prediction pharmacodynamics model of TCM prescriptions was established, and the simulation bias was evaluated by combining two scatterplots. The anti-hypoxia active fraction of Xiangdan injection was determined by experiments. Results: The prediction model of TCM prescriptions established in this study can predict the drug actions for different formulas, and PE%≤25% was observed in 112 mice (93.3%). Conclusion: As indicated in model prediction and experimental confirmation, the pharmacodynamic actions of the 5 formulas are all superior to that of the original formula, and ADE has the best effect. [Copyright &y& Elsevier]

A rapid and specific high-performance liquid chromatographic method coupled with electrospray ionization mass spectrometric detection has been developed and validated for identification and quantification of wogonin and oroxylin A in rat plasma. Wogonin, oroxylin A, and diazepam (internal standard) were extracted from plasma samples by liquid–liquid extraction with ethyl acetate. Chromatographic separation was achieved on a C18 column with acetonitrile–0.6% aqueous formic acid 35:65 ( v/ v) as mobile phase at a flow rate of 0.2 mL min−1. Detection was performed with a single-quadrupole mass spectrometer in selected-ion-monitoring (SIM) mode. Linearity was good within the concentration range 14.4–360 ng mL−1 for wogonin and 10.8–271 ng mL−1 for oroxylin A; the correlation coefficients ( r 2) were 0.9999. The intra-day and inter-day precision, as RSD, was below 12.4%, and accuracy ranged from 81.1 to 111.9%. The lower limit of quantification was 14.4 ng mL−1 for wogonin and 10.8 ng mL−1 for oroxylin A. This method was successfully used in the first pharmacokinetic study of wogonin and oroxylin A in rat plasma after oral administration of the active fraction from Xiao-xu-ming decoction. [ABSTRACT FROM AUTHOR]

The active fraction extracted from dragon’s blood displayed an inhibitory effect on alpha-glucosidase activity with an IC50 of 0.152 μg/mL, which is nearly half of the crude material. Its inhibition on alpha-glucosidase was noncompetitive. In addition, when this fraction was orally administered to mice dosed with Acarbose (20 mg/kg), the active fraction (100, 300, 500 mg/kg) significantly suppressed increase of blood glucose levels after sucrose loading in a dose-dependent manner. These results suggest that this extract from dragon’s blood exerts an anti-diabetic effect by suppressing intestinal carbohydrate absorption and thereby reducing the postprandial increase of blood glucose. [ABSTRACT FROM AUTHOR]

Abstract: This study examined the antioxidant and cytotoxic activities of various fractions (prepared by using solvents of varying polarity) of ethanol extract of Dianthus superbus (DS). The antioxidant activities of various fractions were evaluated in terms of their free radical-scavenging activity. The total phenolics and reducing powers of the fractions were measured. The cytotoxic activities of the fractions on three human malignant cell lines were also investigated. Among all fractions, the ethyl acetate fraction (EE-DS), which had the highest phenolic content and the strongest reducing power, exhibited the strongest antioxidant and cytotoxic activities. [Copyright &y& Elsevier]

In order to better understand the effects of ice nucleation on deep convective clouds, two parameterizations that represent the high active fraction (H-AF case) and low active fraction (L-AF case) of ice nuclei (IN) are implemented into the Weather Research and Forecasting (WRF) model to investigate an extreme real precipitation case. The results indicate that the maximum value of 24-h surface precipitation for the H-AF case is closer to the observation measurement than that for the L-AF case. In early stage of precipitation, increasing IN leads to stronger competition for water vapor in homogeneous regime (above the −40 °C level) and a delay in the growth of ice particles for the H-AF case. With the development of convective system, a large number of ice particles are generated and there are more supercooled droplets occurring above the −20 °C level in H-AF case, resulting in significantly increased mass of snow and graupel and heavier precipitation than that in L-AF case mainly through the processes of R_RCW and R_SML • The maximum value of 24-h surface precipitation for H-AF case is closer to the observation measurement than L-AF case, suggesting that the higher active fractions of IN are responsible for the extreme precipitation. • The increasing IN numbers in H-AF case lead to the stronger competition for water vapor in homogeneous regime (above the −40 °C level) and a delay in the growth of ice particles in the early stage. • With the development of convective system, there are more supercooled droplets and ice particles in H-AF case, resulting in the significantly increased mass of snow and graupel and heavier precipitation. [ABSTRACT FROM AUTHOR]

Amomi Fructus is the dried ripe fruit of Amomum villosum Lour. ( A. villosum ). It is a well-known traditional Chinese medicine widely used to treat gastrointestinal diseases, while the efficacy or mechanism of main components in Amomi Fructus on cancer treatment remains unknown. In this study, volatile oil of A. villosum (VOAV), total flavonoids of A. villosum (FNAV) and the other residue of A. villosum (RFAV) were distilled, extracted and separated as different active fractions of A. villosum . The cell toxicity test results indicated that VOAV and FNAV can effectively inhibit the cell growth of MFC cells. Flow cytometry test results confirmed that MFC cells were caused apoptosis after being treated with VOAV, FNAV or RFAV. VOAV, FNAV or RFAV induced MFC cells apoptosis through reactive oxygen species (ROS)-mediated mitochondrial pathway, evident by the increase of endogenous ROS and mitochondrial membrane potential collapse. In addition, FNAV exhibited robust inhibitory effects on MFC tumor growth, and could improve the health status of mice compared to that of mice in 5-FU treated group. To sum up, all the above results suggest that FNAV may be a good candidate for the development of new drugs for the treatment of gastric cancer., Competing Interests: Competing Interests: The authors have declared that no competing interest exists., (© The author(s).)

Elucidation of the inhibitory effects of humic substances (HSs) on phytopathogenic fungi and the underlying molecular mechanisms are highly important for improved biocontrol. In this study, we investigated the growth suppression, morphological characteristics, transcriptomic sequence, and radical signals of Rhizoctonia solani following HS addition (50 mg/L). Through mycelial cultured experiment, mycelia growth of R. solani had been suppressed with HS addition, and the inhibition rate was 24.88 ± 0.11% compared to the control. Field emission-scanning electron microscopy showed increased and superimposed branching mycelial growth, with a shriveled appearance. RNA samples of R. solani cultured with or without HSs were both extracted to examine the sequence on molecular level by Illumina HiSeq sequencing platform. RNA sequencing analysis revealed 175 differentially expressed genes (DEGs; 111 upregulated and 64 downregulated) between the HSs treatment and control. The upregulated unigenes were annotated and significantly enriched to three molecular processes: vitamin B6 metabolism, ABC transporters, and glutathione metabolism, while the downregulated unigenes were annotated to carbohydrate metabolism, but not significantly enriched. Real time-quantitative polymerase chain reaction analysis showed that the unigenes related to hexokinase, glucose-6-phosphate isomerase, glutathione synthase, and glutathione reductase were significantly decreased (by 60.03%, 70.70%, 60.33%, and 57.59%, respectively), while those related to glutathione S-transferase were significantly increased (2.66-fold). The electron paramagnetic resonance spectra showed that HSs induced increased the intensity of radical signals of R. solani in a cultured system increased by 59.56% compared to CK (without HSs addition). Network analysis based on DEGs expression and the chemical structure of HSs revealed that the carbonyl moiety in HSs formed the most links with nodes of the DEGs (sum of the links of positive and negative effects = 70), implicating this structure as the active fraction responsible for the inhibitory effect. This study provides molecular and chemical evidence of the biofungicidal activity of HSs with the potential for practical application. ga1 • Humic Substances suppressed the activity of Rhizoctonia solani. • Unigenes associated with glutathione production were upregulated. • Unigenes associated with glutathione consumption were downregulated. • HSs increased the intensity of radical signals of cultured R. solani. • C˭O in HSs was implicated as the active fraction responsible for inhibition. [ABSTRACT FROM AUTHOR]

Objectives: The finding of alternative medicine for malarial treatment still has become a substantial demand. The plant is one of the potential sources of drugs, among other natural sources. Artocarpus species showed great potential as the antimalarial source. This study aims to obtain active antimalarial fractions from Artocarpus sericicarpus stem bark., Methods: Stem bark of A. sericicarpus was extracted by ultrasonic-assisted extraction method using n-hexane, dichloromethane, and methanol as solvents. Fractionation of dichloromethane extract was conducted by open column chromatography using octadecyl silica as a stationary phase and gradient acetonitrile-water as a mobile phase. The antimalarial activity was determined by lactate dehydrogenase (LDH) assay against Plasmodium falciparum 3D7 strain., Results: A. sericicarpus n-hexane, dichloromethane, and methanol extracts were showed antimalarial activity with an IC 50 value of >4, 2.11, and >4 μg/mL, respectively. Fractionation of dichloromethane extract was obtained 13 fractions. Seven of the 13 fractions tested showed antimalarial activity. Fraction-6 performed the highest inhibition with an IC 50 value of 1.53 ± 0.04 μg/mL. Phytochemistry screening revealed that Fraction-6 contains flavonoid, polyphenol, and terpenoid compounds that can take a role in its antimalarial activity., Conclusions: A. sericicarpus contains antimalarial substances mainly in Fraction-6, which strongly inhibited the growth of P. falciparum . The flavonoid, polyphenol, and terpenoid compounds were identified in Fraction-6, which need to be further isolated to obtain and elucidate the active antimalarial compounds., (© 2021 Walter de Gruyter GmbH, Berlin/Boston.)

Artemisia lavandulaefolia, a traditional herbal medicine, has been utilized as anti-inflammatory and analgesia agent in clinic. Bioassay-guided fractionation resulted in a fraction (ALDF) with anti-inflammatory effect obtained from A. lavandulaefolia. Its main constituents were analyzed and identified by UPLC-ESI-Q-TOF-MS technology. ALDF showed the strong inhibitory activity on the nitrogen oxide (NO) production in LPS-induced RAW 264.7 macrophages with an IC 50 value of 1.64±0.41 μg/mL. Further results displayed that ALDF also significantly suppressed the secretion of key pro-inflammatory mediators, including tumor necrosis factor-α (TNF-α), prostaglandin E 2 (PGE 2 ) and interleukin-1β (IL-1β), and the increase of the inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) protein expression induced by LPS stimulation. Mechanism study indicated that ALDF was able to block NF-κB signaling pathway through inhibiting IκB and p65 phosphorylation, as well as NF-κB p65 nuclear translocation. Furthermore, in vivo results in mice revealed that treatments with ALDF evoked significant inhibition on ear edema induced by xylene and on the writhing responses induced by acetic acid. These results suggest that ALDF holds great potential in the prevention and treatment of inflammatory disorders., (© 2021 Wiley-VHCA AG, Zurich, Switzerland.)