Boosting the Cell Performance of the SiO/Cu and SiO/PPy Anodes via In-Situ Reduction/Oxidation Coating Strategies.

Silicon monoxide (SiO) has attracted great attention due to its high theoretical specific capacity as an alternative material for conventional graphite anode, but its poor electrical conductivity and irreversible side reactions at the SiO/electrolyte interface seriously reduce its cycling stability. Here, to overcome the drawbacks, the dicharged SiO anode coated with Cu coating layer is elaborately designed by in-situ reduction method. Compared with the pristine SiO anode of lithium-ion battery (293 mAh g-1 at 0.5 A g-1 after 200 cycles), the obtained SiO/Cu composite presents superior cycling stability (1206 mAh g-1 at 0.5 A g-1 after 200 cycles). The tight combination of Cu particles and SiO significantly improves the conductivity of the composite, effectively inhibits the side-reaction between the active material and electrolyte. In addition, polypyrrole-coated SiO composites are further prepared by in-situ oxidation method, which delivers a high reversible specific capacity of 1311 mAh g-1 at 0.5 A g-1 after 200 cycles. The in-situ coating strategies in this work provide a new pathway for the development and practical application of high-performance silicon-based anode.

Emblica officinalis mitigates intestinal toxicity of mice by modulating gut microbiota in lead exposure.

Lead (Pb) contamination has been affecting public health for decades. As a plant-derived medicine, the safety and effectiveness of Emblica officinalis (E. officinalis) fruit extract has been emphasized. The current study focused on mitigating the adverse effects of lead (Pb) exposure in reducing its toxicity worldwide. According to our findings, E. officinalis significantly improved weight loss and colon length shortening (p < 0.05 or p < 0.01). The data of colon histopathology and serum levels of inflammatory cytokines indicated a positive impact to the colonic tissue and inflammatory cell infiltration in a dose-dependent manner. Moreover, we confirmed the expression level improvement of tight junction proteins (TJPs), including ZO-1, Claudin-1, and Occludin. Furthermore, we found that the abundance of some commensal species necessary for maintaining homeostasis and other beneficial function decreased in Pb exposure model, while a remarkable reversion impact was noticed on the intestinal microbiome composition in the treatment group. These findings were consistent with our speculations that E. officinalis could mitigate the adverse effects caused by Pb in alleviating intestinal tissue damage, intestinal barrier disruption, and inflammation. Meanwhile, the variations in gut microbiota might drive the fulfilling current impact. Hence, the present study could provide the theoretical basis for mitigating intestinal toxicity induced by Pb exposure with the help of E. officinalis.

Comprehensive characterization of the in vitro and in vivo metabolites of geniposide in rats using ultra-high-performance liquid chromatography coupled with linear ion trap-Orbitrap mass spectrometer.

1. Geniposide (genipin 1-O-glucose), one of the major bioactive constituents isolated from Fructus Gardeniae, possesses many biological activities. In this study, an efficient strategy was developed using ultra-high-performance liquid chromatography coupled with linear ion trap-Orbitrap mass spectrometer (UPLC-LTQ-Orbitrap) to profile the in vitro and in vivo metabolic patterns of geniposide in rat liver microsomes (RLMs), plasma, urine, and various tissues. And post-acquisition data-mining methods including extracted ion chromatogram (EIC), multiple mass defect filters (MMDF), fragment ion searching (FISh), and isotope pattern filtering (IPF) were adopted to characterize the known and unknown metabolites. 2. A total of 33 metabolites were detected and interpreted according to accurate mass measurement, diagnostic fragment ions, relevant drug biotransformation knowledge, and bibliography data. Among them, 17 metabolites were detected in the plasma, 31 metabolites were identified in the urine, six metabolites could be found in rat heart, 12 in liver, three in spleen, six in lung, 12 in kidney, six in brain, and four in RLMs. 3. A series of corresponding reactions such as hydrolysis, hydroxylation, taurine conjugation, hydrogenation, decarboxylation, demethylation, sulfate conjugation, cysteine S-conjugation, glucosylation, and their composite reactions were all discovered. 4. The results could provide comprehensive insights and guidance for elucidation of side effect mechanism and safety monitoring as well as for rational formulation design in drug delivery system. The newly discovered geniposide metabolites could be targets for future metabolism studies on the important chemical constituents from herbal medicines.

Simultaneous Qualitation and Quantitation of Chlorogenic Acids in Kuding Tea Using Ultra-High-Performance Liquid Chromatography-Diode Array Detection Coupled with Linear Ion Trap-Orbitrap Mass Spectrometer.

Kuding tea, the leaves of Ilex Kudingcha C.J. Tseng, has been applied for treating obesity, hypertension, cardiovascular disease, hyperlipidemia, and so on. The chlorogenic acids (CGAs) in Kuding tea have shown excellent antioxidative, antiobesity, anti-atherosclerotic and anticancer activities. Nevertheless, the chemical profiles of CGAs in Kuding tea have not been comprehensively studied yet, which hinders further quality control. In the present study, a sensitive ultra-high-performance liquid chromatography-diode array detection coupled with a linear ion trap-Orbitrap (UHPLC-DAD-LTQ-Orbitrap) method was established to screen and identify CGAs in Kuding tea. Six CGA standards were first analyzed in negative ion mode with a CID-MS/MS experiment and then the diagnostic product ions (DPIs) were summarized. According to the retention behavior in the RP-ODS column, accurate mass measurement, DPIs and relevant bibliography data, a total of 68 CGA candidates attributed to 12 categories were unambiguously or preliminarily screened and characterized within 18 min of chromatographic time. This was the first systematic report on the distribution of CGAs in Kuding tea. Meanwhile, the contents of 6 major CGAs in Kuding tea were also determined by the UHPLC-DAD method. All the results indicated that the established analytical method could be employed as an effective technique for the comprehensive and systematic characterization of CGAs and quality control of the botanic extracts or Chinese medicinal formulas that contain various CGAs.

Identification of Metabolites of 6'-Hydroxy-3,4,5,2',4'-pentamethoxychalcone in Rats by a Combination of Ultra-High-Performance Liquid Chromatography with Linear Ion Trap-Orbitrap Mass Spectrometry Based on Multiple Data Processing Techniques.

In this study, an efficient strategy was established using ultra-high-performance liquid chromatography coupled with linear ion trap-Orbitrap mass spectrometry (UHPLC-LTQ-Orbitrap MS) to profile the in vivo metabolic fate of 6'-hydroxy-3,4,5,2',4'-pentamethoxychalcone (PTC) in rat urine and feces. The UHPLC-LTQ-Orbitrap method combines the high trapping capacity and MS(n) scanning function of the linear ion trap along with accurate mass measurements within 5 ppm and a resolving power of up to 30,000 over a wider dynamic range compared to many other mass spectrometers. In order to reduce the potential interferences of endogenous substances, the post-acquisition processing method including high-resolution extracted ion chromatogram (HREIC) and multiple mass defect filters (MMDF) were developed for metabolite detection. As a result, a total of 60 and 35 metabolites were detected in the urine and feces, respectively. The corresponding in vivo reactions such as methylation, hydroxylation, hydrogenation, decarbonylation, demethylation, dehydration, methylation, demethoxylation, sulfate conjugation, glucuronide conjugation, and their composite reactions were all detected in this study. The result on PTC metabolites significantly expanded the understanding of its pharmacological effects, and could be targets for future studies on the important chemical constituents from herbal medicines.

Transcriptome Profile Reveals that Pu-Erh Tea Represses the Expression of Vitellogenin Family to Reduce Fat Accumulation in Caenorhabditis elegans.

Due to misbalanced energy surplus and expenditure, obesity has become a common chronic disorder that is highly associated with many metabolic diseases. Pu-erh tea, a traditional Chinese beverage, has been believed to have numerous health benefits, such as anti-obesity. However, the underlying mechanisms of its anti-obesity effect are yet to be understood. Here, we take the advantages of transcriptional profile by RNA sequencing (RNA-Seq) to view the global gene expression of Pu-erh tea. The model organism Caenorhabditis elegans was treated with different concentrations of Pu-erh tea water extract (PTE, 0 g/mL, 0.025 g/mL, and 0.05 g/mL). Compared with the control, PTE indeed decreases lipid droplets size and fat accumulation. The high-throughput RNA-Sequence technique detected 18073 and 18105 genes expressed in 0.025 g/mL and 0.05 g/mL PTE treated groups, respectively. Interestingly, the expression of the vitellogenin family (vit-1, vit-2, vit-3, vit-4 and vit-5) was significantly decreased by PTE, which was validated by qPCR analysis. Furthermore, vit-1(ok2616), vit-3(ok2348) and vit-5(ok3239) mutants are insensitive to PTE triggered fat reduction. In conclusion, our transcriptional profile by RNA-Sequence suggests that Pu-erh tea lowers the fat accumulation primarily through repression of the expression of vit(vitellogenin) family, in addition to our previously reported (sterol regulatory element binding protein) SREBP-SCD (stearoyl-CoA desaturase) axis.

[Studies on chemical constituents from seeds of Euryale ferox].

OBJECTIVE: To study the chemical constituents from the seeds of Euryale ferox. METHODS: The chemical constituents were isolated by silica gel column, Sephadex LH-20 and their structures were identified by physico-chemical and spectral analysis. RESULTS: Seven compounds were purified from the 95% ethanol extract. These constituents were elucidated as protocatechuic acid (1), gallic acid (2), gallic acid ethyl ester(3),5 ,7-dihydroxychromone(4), ß-sitosterol(5), daucosterol(6), and 5,7-dihydroxy-6,4'-dimethoxyflavone(7), respectively. CONCLUSION: All compounds are isolated from this plant for the first time.

Cytotoxic glutarimide-containing polyketides isolated from Streptomyces sp. JCM 4793.

Glutarimide-containing polyketides usually exhibit anti-fungi activity, which was well exampled by cycloheximide. In our work, three new polyketide structures, 12-amidestreptimidone (1), 12-carboxylstreptimidone (2) and 3-(5S,8R)-(2-amino-2-oxoethyl-2'-methoxy-2'-oxoethyl)-8,10-dimethyl-7-oxododeca-5-hydroxy-9E,11-diolefin (3) were isolated from Streptomyces sp. JCM 4793. 3 without the glutarimide moiety is not active against fungi as expected, while 1 bearing the amide moiety is much more active than its carboxylic form 2. Here we report the isolation, structural elucidation, antifungal activity, and proposed biosynthesis pathway of 1-3.

Analyses of m6A regulatory genes and subtype classification in atrial fibrillation.

Objective: To explore the role of m6A regulatory genes in atrial fibrillation (AF), we classified atrial fibrillation patients into subtypes by two genotyping methods associated with m6A regulatory genes and explored their clinical significance. Methods: We downloaded datasets from the Gene Expression Omnibus (GEO) database. The m6A regulatory gene expression levels were extracted. We constructed and compared random forest (RF) and support vector machine (SVM) models. Feature genes were selected to develop a nomogram model with the superior model. We identified m6A subtypes based on significantly differentially expressed m6A regulatory genes and identified m6A gene subtypes based on m6A-related differentially expressed genes (DEGs). Comprehensive evaluation of the two m6A modification patterns was performed. Results: The data of 107 samples from three datasets, GSE115574, GSE14975 and GSE41177, were acquired from the GEO database for training models, comprising 65 AF samples and 42 sinus rhythm (SR) samples. The data of 26 samples from dataset GSE79768 comprising 14 AF samples and 12 SR samples were acquired from the GEO database for external validation. The expression levels of 23 regulatory genes of m6A were extracted. There were correlations among the m6A readers, erasers, and writers. Five feature m6A regulatory genes, ZC3H13, YTHDF1, HNRNPA2B1, IGFBP2, and IGFBP3, were determined (p < 0.05) to establish a nomogram model that can predict the incidence of atrial fibrillation with the RF model. We identified two m6A subtypes based on the five significant m6A regulatory genes (p < 0.05). Cluster B had a lower immune infiltration of immature dendritic cells than cluster A (p < 0.05). On the basis of six m6A-related DEGs between m6A subtypes (p < 0.05), two m6A gene subtypes were identified. Both cluster A and gene cluster A scored higher than the other clusters in terms of m6A score computed by principal component analysis (PCA) algorithms (p < 0.05). The m6A subtypes and m6A gene subtypes were highly consistent. Conclusion: The m6A regulatory genes play non-negligible roles in atrial fibrillation. A nomogram model developed by five feature m6A regulatory genes could be used to predict the incidence of atrial fibrillation. Two m6A modification patterns were identified and evaluated comprehensively, which may provide insights into the classification of atrial fibrillation patients and guide treatment.

Stereoselective separation, configuration determination, and quantification of flavanone glycosides in Citrus using chiral HPLC-UV in combination with CD spectra.

Flavanone glucosides, such as naringin and neohesperidin, are present in specific Citrus species and manifest a chiral center at the C-2 position of their flavanone moiety. This study successfully achieved the simultaneous stereoselective separation of the C-2 diastereomers of naringin, neohesperidin and hesperidin, as well as the partial separation of narirutin using a chiral high performance liquid chromatography with ultraviolet detection method with cellulose tris(3,5-dichlorophenylcarbamate) as the stationary phase under normal-phase mode. The mobile phase comprised n-hexane and ethanol (containing 0.25% formic acid) at a proportion of 65 : 35 (v/v) with a flow rate of 0.6 mL min-1. Each single epimer of chiral flavanone glycosides was prepared using chiral semi-preparative chromatography, and the absolute configuration was then characterized by combining the experimental electronic circular dichroism detection and time-dependent density functional theory calculations. The epimer composition of each chiral flavonoid glycoside in Fructus aurantii (Zhiqiao) and Fructus aurantii immaturus (Zhishi) was determined revealing variations among herbs collected from different production regions. Additionally, the epimer composition was found to be related to the harvesting time of the herbs. Considering the safety and efficacy, the existence of epimers of different stereo-configurations should be given more attention in the quality evaluation of natural drugs.

Corilagin ameliorates macrophages inflammation in atherosclerosis through TLR4-NFκB/MAPK pathway.

Corilagin, a polyphenolic tannic acid compound, showed significant anti-inflammatory activity in atherosclerotic mice. The present study aimed to evaluate the effect and mechanism of corilagin in atherosclerosis by in vivo, in vitro and in molecular docking strategies analysis. An atherosclerotic model was established by feeding ApoE-/- mice a high-fat diet. Murine RAW264.7 macrophages were cultured and induced with lipopolysaccharide (LPS). Treatment with corilagin had a marked inhibitory effect on the plaque area and lipid accumulation in atherosclerotic mice. Corilagin decreased the expression of iNOS and promoted the expression of CD206 in aortic plaque, as well as inhibited the production of proinflammatory factors in HFD-fed ApoE-/- mice and LPS-induced RAW264.6 cell. Corilagin also obviously inhibited the expression of TLR4, reduced the phosphorylation of the JNK, the protein expressions of p38 and NF-κB pathway. In addition, corilagin markedly diminished the nuclear translocation of NF-κBp65. Similarly, molecular docking study suggested that hydrogen bonds were detected between the corilagin and the five proteins (TLR4, Myd88, p65, P38, and JNK) with a significant "CDOCKER energy". These results showed that the antiatherosclerotic effect of corilagin against M1 macrophage polarization and inflammation via suppression the activation of TLR4-NFκB/MAPK signaling pathway. Therefore, corilagin could be a promising lead compound to develop drugs for the treatment of atherosclerosis.

Protective effects of Emblica officinalis polysaccharide against lead induced liver injury in mice model.

Heavy metal contamination especially lead (Pb) causes a serious threat to global public health. In the current study, we explored the protective and regulating effects of Emblica officinalis polysaccharide (EOP) in the liver against Pb-induced toxicity. According to our findings, EOP decreased the Pb-induced pathological lesions of liver and overall weight index in mice (p < 0.05). Following treatment with EOP, the levels of biological biomarkers for liver hepatic function (i.e., ALT and AST) were significantly decreased (p < 0.01) in a dose-dependent manner, consisted with histopathological changes. The key proteins involved in hepatic oxidative stress and apoptosis, including Nrf2, HO-1, Bcl-2, and Bax were quantified, which indicated EOP as an effective approach in protecting against the liver injury. Moreover, EOP treatment ameliorated the negative changes of liver metabolic profile (i.e., metabolites concentrations and metabolic patterns). In conclusion, EOP could protect the liver against oxidative stress and apoptosis induced by Pb poisoning, associated with the efficacy of ameliorating the negative changes in liver metabolic profile. Hence, the current findings recommend EOP as an efficient way for alleviating liver injury in lead poisoning.

Effects of Glycyrrhiza Polysaccharides on Chickens' Intestinal Health and Homeostasis.

The overuse of antibiotics in poultry farming causes the accumulation of drug residue in animals' bodies and the occurrence of antibiotic-resistant bacteria, which not only compromise animals' health but ultimately endanger human health. Thus, there is an urgent need for a novel poultry feed additive to substitute for excessive antibiotics. Glycyrrhiza polysaccharides (GPS) derived from Chinese licorice have shown promising immunomodulatory effects in previous studies. The present study investigated the pharmacological effects of GPS on poultry intestines to assess whether it can be used as a feed additive. The results show that GPS can increase production of sIgA, promote the secretion activity of goblet cells, alter the gut microbial composition and lead to changes in short-chain fatty acids. GPS also elevated both Th1 and Th2 immune responses by facilitating the expression of IL-2, IL-4, IL-1ß, and IFN-γ while increasing the proportion of both CD4+ and CD8+ cells in the intestine. Moreover, the results of 16S rRNA gene sequencing showed that GPS could significantly change intestinal microbiota composition in the intestine, evidenced by the increased proportion of Bacteroides, Butyricicoccus and Eisenbergiella, as well as a decreased portion of Erysipelatoclostridium, leading to a healthier intestinal microbiota composition for the host. Taken together, it can be concluded that GPS is safe to use as a novel feed additive that can be used as an alternative to prophylactic antibiotics in poultry feeding.

Glycyrrhiza polysaccharides can improve and prolong the response of chickens to the Newcastle disease vaccine.

Licorice is a medicinal and food plant widely used to treat diseases and produce food additives, because of its unique chemical constituents like polysaccharides, flavones, and saponins. Glycyrrhiza Polysaccharides (GPS-1) are water-soluble neutral polysaccharides extracted from licorice. Currently, GPS-1 is administrated to chickens by gavage every d for 14 d to observe the impact of GPS-1 on the Newcastle disease vaccine. To determine the immunity of these chickens to NDV, blood serum levels of hemagglutinin-inhibition (HI) antibody, and immunoglobulins IgA and IgG were measured. Meanwhile, the expression levels of cytokines IL-2, IL-4, IL-17, and IFN-γ were measured to evaluate the degree of immune booster activity. The chickens' spleen and peripheral blood lymphocytes displayed a significant increase in the proportion of CD4+ and CD8+ T cells after booster treatments with GPS-1. The results indicated that GPS-1 had a significant, dose-dependent, immune-boosting effect which could enhance NDV vaccine immunity in chickens.

Immunomodulatory and antioxidant effects of Glycyrrhiza uralensis polysaccharide in Lohmann Brown chickens.

Glycyrrhiza polysaccharide extract 1 (GPS-1) is a bioactive component isolated from Glycyrrhiza uralensis, also known as Chinese licorice. It appears to be pharmacologically active as an antibacterial, antiviral, and anti-tumor agent. GPS-1 has also been shown to buffer liver health and regulate the immune system. Moreover, GPS-1 is low cost and easy to extract. More study was needed to elucidate the biochemical pathways underlying the immunomodulatory and antioxidant benefits observed in Glycyrrhiza polysaccharide extract 1 (GPS-1). in vitro experiments on chicken lymphocytes and dendritic cells (DCs) show that GPS-1 significantly promotes the proliferation of immune cells and is linked to lymphocytes' secretion of IL-12, IFN-γ, and TNF-α by. DC secretion of NO, IL-2, IL-1ß, IFN-γ, TNF-α, and IL-12p70 was also increased significantly. Additionally, GPS-1 also displayed a significant antioxidant effect in vitro, able to scavenge DPPH, hydrogen peroxide, ABTS, and other free radicals like superoxide anions. Separately, GPS-1 was tested in vivo in combination with the Newcastle disease virus (NDV) - attenuated vaccine. 120 Lohmann Brown chickens were vaccinated, while another 30 became the unvaccinated blank control (BC) group. For three consecutive days 1 mL of GPS-1 was administered at doses of 19.53 µg/mL, 9.77 µg/mL, or 4.88 µg/mL to the ND-vaccinated birds, except for the vaccine control (VC), where n = 30 per group. In vivo results show that GPS-1 combined with Newcastle disease (ND) vaccine had the best efficacy at significantly increasing chickens' body weight and ND serum antibody titer, enhancing their secretion of IL-2 and IFN- γ, and promoting the development of immune organs. The results also indicate that GPS-1 was able increase the proliferation of in vitro immune cells and elevate their cytokine secretion, which enhances the body's immune response. GPS-1 also clearly has the potential to be used as an immune adjuvant alongside ND vaccination.

Structure of a new glycyrrhiza polysaccharide and its immunomodulatory activity.

A component of licorice polysaccharide (GPS-1) was extracted from licorice, its primary structure was identified and characterized for the first time, and its immunomodulatory activity was studied. Crude licorice polysaccharide was isolated and purified by DEAE sepharose FF ion-exchange column chromatography and Chromdex 200 PG gel filtration column chromatography to obtain a purified Glycyrrhiza polysaccharide named GPS-1. NMR and methylation analysis revealed that GPS-1 is composed of homogalacturonan (HG)-type pectin with 4)-D-GalpA-(1 as the backbone. This study of GPS-1 also examined its significant role in regulating immune activity in vitro and in vivo. As a result, GPS-1 promoted the secretion of IFN-γ and IL-4 in mice and increased the proportion of CD3+CD4+ and CD3+CD8+ T lymphocytes in their spleens. Dendritic cells (DCs) treated with GPS-1 showed promotion of DC maturation, antigen presentation, and phagocytic capacity. The results suggest that GPS-1 is a potential immunomodulator that stimulates the immune system by regulating multiple signaling pathways. Combined with our characterization of the primary structure of GPS-1, the present investigation provides the basis for future study of the form-function relationship of polysaccharides.

Polysaccharides from Polygonatum kingianum improve glucose and lipid metabolism in rats fed a high fat diet.

OBJECTIVE: Polygonatum kingianum is a traditional Chinese medicine commonly used to treat diabetes and hyperlipidemia. Polysaccharides from Polygonatum kingianum could regulate glucose and lipid metabolism in high-fat diet (HFD) rats. METHODS: The gel permeation chromatography (GPC), liquid chromatography (HPLC) and chemical analysis were used to determine the molecular weight, monosaccharide composition, protein, polysaccharide and uronic acid content of the polysaccharide from Polygonatum kingianum, respectively. Total (PS) and high molecular weight (PSF) polysaccharides (> 100 KDa) were isolated and treated HFD rats for a 14-week period. TC, TG contents in blood samples were measured every two weeks, and HDL-C, LDL-C was measured at 12 and 14 weeks evaluating of blood lipids regulation activity of polysaccharide. The stool samples were used for 16S rDNA V4 highly variable region measurement method to regulate the role of polysaccharide in the intestinal microflora. The content of short chain fatty acid (SCFAs) in faeces was determined by gas chromatography (GC) to investigate the effect of polysaccharides on the content of SCFAs in the intestinal tract of rats. The expression of tight junction protein ZO-1 and occludin of intestinal tissue, and detection of the key protein expression in the LPS-TLR4/NFκB signaling pathway were detected by Western blot technique. RESULTS: We found that PS and PSF improved both diabetic symptoms and lipid metabolism. PS and PSF also modulated the gut microbiota composition, abundance and diversity of HFD rats, increased the relative abundance of short chain fatty acid (SCFA) producing bacteria and increased SCFA production, reduced intestinal permeability, relieved gastrointestinal inflammation, and improved lipid metabolism. CONCLUSION: Polygonatum kingianum polysaccharides regulated the abundance and diversity of the intestinal microbial community through increasing the relative abundance of SCFA-producing bacteria. This promotes recovery of the intestinal permeability barrier, inhibits LPS entry into the circulation, alleviates inflammation, and prevents glucose and lipid metabolic disorders.

Danshen: a phytochemical and pharmacological overview.

Danshen, the dried root or rhizome of Salvia miltiorrhiza Bge., is a traditional and folk medicine in Asian countries, especially in China and Japan. In this review, we summarized the recent researches of Danshen in traditional uses and preparations, chemical constituents, pharmacological activities and side effects. A total of 201 compounds from Danshen have been reported, including lipophilic diterpenoids, water-soluble phenolic acids, and other constituents, which have showed various pharmacological activities, such as anti-inflammation, anti-oxidation, anti-tumor, anti-atherogenesis, and anti-diabetes. This article intends to provide novel insight information for further development of Danshen, which could be of great value to its improvement of utilization.

Kudinoside-D, a triterpenoid saponin derived from Ilex kudingcha suppresses adipogenesis through modulation of the AMPK pathway in 3T3-L1 adipocytes.

The leaves of Ilex Kudingcha, locally named "Kudingcha" in China, has been traditionally applied for treating obesity. Studies have demonstrated that the ethanol extract of Ilex kudingcha have anti-adipogenic effects. However, the constituent which was responsible for its anti-obesity and its underlying molecular mechanism has not yet been elucidated. This research explored the anti-obesity effect of kudinoside-D which was a main natural component of triterpenoid saponin from the ethanol extract of Ilex kudingcha, on lipid accumulation and the potential mechanism of action of adipogenesis in 3T3-L1 adipocytes. The adipocytes were treated with various concentrations of kudinoside D (0 to 40µM) during differentiation. The image-based Oil Red O staining analyses revealed that KD-D, dose dependently reduced cytoplasmic lipid droplet in 3T3-L1 adipocytes with the IC50 is 59.49µM. Meanwhile, major adipogenic transcription factor peroxisome proliferator-activated receptor γ (PPARγ), CCAAT/enhancer binding protein-α (C/EBPα) and sterol regulatory element-binding protein 1c (SREBP-1c) were significantly repressed as well as their target genes. The phosphorylation of AMP-activated protein kinase (AMPK) and its downstream target phosphorylated-acetyl CoA carboxylase (ACC) expression were also increased. In addition, the inhibitory effects of KD-D on the expressions of PPARγ and C/EBPα were weakened when cells were cotreated with AMPK inhibitor Compound C. These results indicated KD-D exerts anti-adipogenic effects through modulation of adipogenic transcription factors via AMPK signaling pathway. And the current findings demonstrated that KD-D was a potential therapeutic candidate for alleviating obesity and hyperlipidemia.

Cytotoxic steroidal saponins from Ophiopogon japonicus.

Four new steroidal saponins, named ophiopogonin P-S (1-4), together with eleven known ones (5-15) were isolated from the tuberous roots of Ophiopogon japonicus. Their structures were elucidated by spectroscopic and chemical analysis. Compounds 2-15 were evaluated for their cytotoxic activity against five human tumor cell lines (HepG2, HLE, BEL7402, BEL7403 and Hela). Compounds 2, 5, 6, 8 and 9 were cytotoxic for all cell lines tested. Compounds 7, 11 and 15 showed selective cytotoxicity against some of the cell lines. The structure-activity relationship of these compounds was discussed.