Xiaoli Ye

Southwest University in Chongqing, Pehpei, Chongqing Shi, China

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Publications (27)37.63 Total impact

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    ABSTRACT: Current work was conducted to evaluate the safety and antihypercholesterolemic activity of jatrorrhizine extracted from Rhizoma Coptidis (RC) and its potential mechanism on regulating cholesterol metabolism. It was found that the LD50 of jatrorrhizine in mice was more than 5500mg/kg and there were no influences on clinical signs, organ weight changes, urinalysis and hematological parameters, gross necropsy and histological alterations in jatrorrhizine-treated rats during the 3-month period, compared to the control group. Jatrorrhizine showed a strong lipid-lowering effect in a dose-dependent manner. Oral administration of 70.05mg/kg of jatrorrhizine on Mesocricetus auratus (Syrian golden hamsters) exhibited significant decrease in TC, TG, and LDL-c levels by 20%, 43%, and 19%, respectively, and increase in HDL-c and total bile acids (TBA) content in feces (p<0.01), compared to high-fat and high-cholesterol (HFHC) group. Besides, jatrorrhizine dose-dependently slowed the rate of weight gain. The results of qRT-PCR, western blotting and ELISA revealed that jatrorrhizine significantly up-regulated the mRNA and protein expression of LDLR and CYP7A1, but exhibited no significant effect on mRNA and protein expression of HMGR and ASBT in hamsters. In conclusion, jatrorrhizine was a safe and potential antihypercholesterolemic agent from RC which could improve the utilization and excretion of cholesterol by up-regulating the mRNA and protein expression of LDLR and CYP7A1.
    Phytomedicine: international journal of phytotherapy and phytopharmacology 05/2014; · 2.97 Impact Factor
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    ABSTRACT: Berberine (BBR), a major active component of natural plant product, has recently been demonstrated to be clinically effective in alleviating type 2 diabetes mellitus (T2DM). In this study, BBR and 8-alkylberberine were successively halogenated with bromine, iodine, chlorine under various conditions. HepG2 cell lines, phenotypically similar to human hepatocytes, were used to study the effect of the BBR derivatives on glucose consumption (GC) in vitro. The glucose-lowering effect of chloroberberine and bromoberberine was better than non-modified BBR under the concentrations studied (0.5, 1, 2, 4 μg/mL). Compared to the control, GC of HepG2 cells treated with chloroberberine at 1 μg/mL was increased by 90%. 8-Alkylberberine and 8-alkyl-13-bromoberberine did not exhibit any glucose-lowering effect. 8-Octylberberine caused the reduction of GC in a dose-dependent manner. The MTT assay was used to determine the cytotoxicity of BBR derivatives; the cytotoxicity of chloroberberine and iodoberberine was lower than that of the parent BBR. Meanwhile, the inhibition of HepG2 cell proliferation of 8-alkylberberine was stronger than that of 8-alkyl-13-bromoberberine. These observations suggest that chloroberberine could enhance the glucose-lowering activity and protect HepG2 cell lines as well. 8-Octylberberine showed the strongest HepG2 inhibition activity amongst all the synthesized compounds, which was over 36-fold higher than its parent BBR, and thus might be used as an anticancer agent. These results may open up new avenues for therapeutic applications of BBR in the treatment of T2DM.
    Journal of Functional Foods 03/2014; · 2.63 Impact Factor
  • Phytomedicine. 01/2014;
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    ABSTRACT: Herbal medicine, especially traditional Chinese medicine and Ayurvedic medicine have played and still play an important role in fighting against various diseases. Emerging clinical studies regarding traditional Chinese medicine have provided convincing evidence for the first time to gain credibility and reputation outside China. Although synergistic therapeutic actions of herbal ingredients have been frequently reported, few reports have offered clear underlying mechanisms. This might be the main reason for the conflicting views with respect to the therapeutic efficacy of medicinal herbs. Therefore,this paper reviews the herb synergisms reported in the recent literature and discusses thoroughly the mechanisms underlying synergistic actions of herbal ingredients. The authors conducted an electronic literature search to detect articles published mainly in the last five years. Articles were included if they pertained to synergy research of ethnomedicines or the active compounds derived from them, included verification of synergy effects using modern analytical tools and molecular - biological methods. Results have revealed that the multi-component nature of medicinal herbs makes them particularly suitable for treating complex diseases and offers great potential for exhibiting synergistic actions. The mechanisms underlying synergistic therapeutic actions of herb medicines are (1): different agents may regulate either the same or different target in various pathways, and therefore cooperate in an agonistic, synergistic way; (2): regulate the enzymes and transporters that involved in hepatic and intestinal metabolism to improve oral drug bioavailability ; (3): overcome the drug resistance mechanisms of microbial and cancer cells; (4): eliminate the adverse effects and enhance pharmacological potency of agents by "processing" or by drug-drug interaction. The exploration of synergistic mechanisms of herbal ingredients will not only help researchers to discover new phytomedicines or drug combinations but also help to avoid the possible negative synergy. Further clinical research is required for verifying these reported drug combinations and discovered synergistic mechanisms.
    Fitoterapia 10/2013; · 2.23 Impact Factor
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    ABSTRACT: ETHNOPHARMACOLOGICAL RELEVANCE: Rhizoma Coptidis (RC), a widely used traditional Chinese medicine, has been used for the treatment of heat-clearing and detoxifying, but there is very little information on its safety. AIM OF THE STUDY: To provide information on the safety of RC, we evaluated the toxicity of the crude RC and RC alkaloids (berberine, coptisine, palmatine and epiberberine) including cytotoxicity, acute toxicity in mice and sub-chronic toxicity in rats. MATERIALS AND METHODS: The cytotoxicity of RC alkaloids was tested in HepG2 and 3T3-L1 cells by the MTT assay. The acute toxicity of RC alkaloids was tested in mice and the mortality was calculated at the end of experiment. For sub-chronic toxicity study, the rats were treated with the RC alkaloids at a dose of 156mg/kg/day and RC at a dose of 521mg/kg/day for 90 days. Mortality, clinical signs, body weight changes, organ weights, urinalysis and hematological parameters, gross findings and histopathology were monitored during the study period. RESULTS: The cell assay indicates that the IC(50) values of berberine, coptisine, palmatine and epiberberine in HepG2 cells were 48.17, 64.81, 112.80 and 120.58µg/mL, which in 3T3-L1 cells were 41.76, 56.48, 84.32 and 104.18µg/mL, respectively. In the acute toxicity assay, the LD(50) values of four alkaloids were 713.57, 852.12, 1533.68 and 1360mg/kg, respectively. However, in the sub-chronic toxicity study, no mortality and morbidity were observed which could be related to RC alkaloids and RC treatment. Besides, there was no abnormality in clinical signs, body weights, organ weights, urinalysis, hematological parameters, gross necropsy and histopathology in any of the animals after the oral administration of RC alkaloids and RC. CONCLUSIONS: Taking these results together, we came to the conclusion that the toxicity of berberine is the maximum and palmatine is the minimal in four RC alkaloids. The currently recommended doses of RC alkaloids and RC consumed are relatively safe.
    Journal of ethnopharmacology 11/2012; · 2.32 Impact Factor
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    ABSTRACT: In this study, the bioactive component harpagoside and angroside C in the root of Scrophularia ningpoensis Hemsley was simultaneously separated by high-speed counter-current chromatography (HSCCC). A two-phase solvent system containing chloroform/n-butanol/methanol/water (4:1:3:2, v/v/v/v) was selected following consideration of the partition coefficient of the target compound. The crude extract (200 mg) was loaded onto a 280-mL HSCCC column and yielded 22 mg harpagoside and 31 mg angroside C with the purity of higher than 98 and 98.5%, respectively. It is feasible to isolate active compounds harpagoside and angroside C from S. ningpoensis using HSCCC.
    Journal of Separation Science 10/2012; 35(19):2659-64. · 2.59 Impact Factor
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    ABSTRACT: This paper reports a physiologically relevant and rapid mitochondria-based assay for assessing antioxidant properties of pure compounds and herb extracts. The principle of this method is antioxidants can scavenge peroxyl radicals generated in mitochondria thus to inhibit 2′,7′-dichlorofluorescin diacetate oxidation. Ascorbic acid, chlorogenic acid and berberine showed a dose-dependent antioxidative capacity; interestingly, lutein, Rehmannia glutinosa and Scrophularia ningpoensi exhibited pro-antioxidant properties. The antioxidant properties of herb extracts obtained by this method are in good agreement with the results measured by cell-based assay (r = 0.931, p < 0.001). This novel assay has acceptable accuracy, precision, reproducibility and the mitochondria-based assay may be more useful than conventional assay for detecting antioxidant capacity in a variety of foods.
    Food Research International. 10/2012; 48(2):454–461.
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    ABSTRACT: An effective and rapid method for the separation of scopoletin from Lycium barbarum L. by high-speed counter-current chromatography (HSCCC) was established. The ethyl alcohol extract of the Lycium barbarum L. was initially separated using D-101 macroporous resins and further purified by HSCCC. The thin layer chromatography coupling with fluorometric spectrophotometry (TLC-F) method was used to determine the partitioning coefficient of scopoletin in different solvent systems. The results showed the solvent system of chloroformmethanol-water (10:7:3, v/v/v) was the best one for the HSCCC separation. A total of 10.2 mg of scopoletin with high purity (98. 3%, analyzed by high performance liquid chromatography (HPLC)) was obtained in one step by the following separation procedures: the upper phase as the stationary phase, the lower phase as the mobile phase, with a flow rate of 1.5 mL/min, with the apparatus rotated at 850 r/min, and detected at 365 nm. The structure of the obtained compound was identified by 'H-nuclear magnetic resonance and 13C-nuclear magnetic resonance. The sample could be injected into HSCCC twice successively and the whole separation was achieved with satisfactory peak resolution. These results suggested that the TLC-F method is useful in measuring the partitioning coefficients of the target compound in HSCCC solvent systems and HSCCC is a fast and convenient method for the separation of scopoletin.
    Se pu = Chinese journal of chromatography / Zhongguo hua xue hui 09/2012; 30(9):971-4.
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    ABSTRACT: This study was carried out to evaluate the effect of cigarette smoke (CS) on the activity of oral peroxidase (OPO) after berberine was added to the cigarette filter. Activated carbon fiber (ACF) was chosen to load berberine as a part of the cellulose acetate (CA) filter to obtain the modified B-ACF cigarette filter. Then the effects of CS from the testing cigarettes on the activity of OPO were investigated in vitro by the 2-nitrobenzoic acid assay, and the smoke chemistry was also analyzed, especially the content of hydrogen cyanide (HCN) in the CS. The results indicated that the loss of activity of OPO in B-ACF filter cigarette group decreased by 20% and 25%, compared with those of ACF and CA filter cigarette groups, respectively. The relative residual activity of OPO in B-ACF filter group was increased with the increase of berberine in the filter compared with the CA filter group. It could be observed that the reduction in HCN might be related to the berberine in the cigarette filter, reducing the inhibition of CS on the activity of OPO.
    Toxicology and Industrial Health 03/2012; · 1.56 Impact Factor
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    ABSTRACT: The root of Polygonatum odoratum (YuZhu), also a medicinal food has long been used for the treatment of diabetes. The objective of the study was to characterize the anti-diabetic active fractions or compounds in this herb. Fractions with a different polarity were prepared by solvent extraction and macroporous absorptive resin (D101) column and their anti-diabetic potentials were evaluated by glucose uptake in HepG2 cells and STZ-induced diabetic rats. In addition, α-glycosidase inhibitory activities of active fractions were measured in vitro and chemical compositions including saponin, total flavonoids and total sugar in the fractions were determined. The n-buthanol fraction, a saponin-rich fraction obtained by partitioning the ethanol extract with n-buthanol after petroleum ether and acetic ether showed the highest anti-diabetic potential in glucose uptake in HepG2 cells followed by acetic ether fraction which was rich in flavonoids. Further fractionation the saponin-rich fraction using macroporous resin column (D101), polysaccharide, flavonoid and saponin rich fractions were obtained by elution with water, 40% and 60% ethanol, respectively and their anti-diabetic potentials proved by glucose uptake test in HepG2 cells and STZ-induced diabetic rats were in the order of saponin rich fraction>flavonoid rich fraction>polysaccharide rich fraction. Long-term therapy test (60d) in severe diabetic rats indicated that saponin-rich fraction significantly ameliorated clinical symptoms of diabetes including the elevated blood glucose, body weight loss as well as the increased food and water intake while flavonoid-rich fraction was more potential than saponin-rich fraction to increase superoxide dismutase (SOD) activity and decrease malondialdehyde (MDA) level in rat plasma. Additionally, saponin-rich fraction and flavonoid-rich fraction showed α-glycosidase inhibitory activity with IC(50) value of 2.05±0.32 and 3.92±0.65mg/ml, respectively. The results suggested that saponin in this herb was more important than flavonoid in exhibiting anti-diabetic activity and flavonoid contributed more to anti-oxidant activity in vivo.
    Journal of ethnopharmacology 02/2012; 141(1):228-33. · 2.32 Impact Factor
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    ABSTRACT: A four-step microwave-assisted procedure was used to synthesize 7-alkoxyl-rhein derivatives 5a–e starting from emodin and 1-bromoalkanes. These compounds exhibited hypoglycemic activity by inhibiting α-glucosaccharase, which were influenced by the aliphatic chain length. Results showed that 5c displayed remarkable activity in vitro and in vivo.
    Medicinal Chemistry Research 01/2012; · 1.61 Impact Factor
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    ABSTRACT: To increase the bioavailability of berberine, three new 9-O-glycosyl-berberine derivatives, 9-O-glucosyl-(4a), 9-O-arabinosyl-(4b), and 9-O-erythrol-(4c) were obtained and confirmed by UV, 1HNMR, 13CNMR, and MS. The pharmacokinetic profiles of these synthetic compounds have been evaluated compared with berberine (1) and 9-O-alkyl-berberine (5) derivatives, which showed that maximum concentration (C max) and area under concentration–time curve (AUC) of 9-O-glycosyl-berberine increased dramatically. The results indicated that hydrophilic modification could significantly improve the bioavailability of berberine; 9-O-glycosyl-berberine might be a promising prodrug.
    Medicinal Chemistry Research 01/2012; · 1.61 Impact Factor
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    ABSTRACT: It is known that the choice of solvent system for high speed counter-current chromatography separation is of utmost importance. In this study, a simple and rapid thin layer chromatograph coupling with fluorometric (TLC-F) method has been used to determine the partition coefficient of target compounds in HSCCC solvent system. Two components, 6,7-dimethoxycoumarin and 5-hydroxymethyl-2-furfural were successfully separated from purple sweet potato extracts by successive sample injection for the first time, using n-hexane-ethyl acetate-methanol-water (1:2:1:1, v/v/v/v) as the solvent system. Additionally, statistical analysis showed that there was no significant difference in partition coefficient obtained by the TLC-F method and by HPLC, which demonstrated the usefulness of TLC-F method.
    Journal of chromatography. B, Analytical technologies in the biomedical and life sciences 12/2011; 881-882:49-54. · 2.78 Impact Factor
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    ABSTRACT: Traditional Chinese medicine (TCM) has been used for treating complex chronic diseases owing to their fewer side-effects, better patient tolerance and relatively less cost. The present work was carried out to study the anti-diabetic efficacy and mechanisms of 34 TCMs. Streptozotocin (STZ)-diabetic mice were orally administrated with corresponding herbal solution once a day for 4 weeks. At the end of experiment, the level of plasma glucose, malondialdehyde (MDA), the activity of superoxide dismutase (SOD) and the serum aldose reductase (AR) were determined, the effects of TCM extract on α-glucosidase and angiotensin-converting enzyme (ACE) in vitro were also evaluated. 13 out of the 34 herbs showed a statistically significant plasma glucose lowering action compared with the diabetic control group. Biochemical analysis revealed that Atractylodes macrocephala, Codonopsis pilosula, Dioscorea opposite, Flos lonicerae and Pueraria lobata may retard the progression of diabetes via reduce the blood glucose level and prevent the increase of AR activity. Other tested herbs, such as Ramulus cinnamomi, Cinnamomum cassia, and Eucommia ulmoides, showed the antidiabetic ability by either prevent the decrease in SOD activity or suppress the increase of MDA. Zymologic assay reveals that Pueraria lobata and Anemarrhena asphodeloides showed the highest inhibition against α-glucosidase and ACE respectively. Interestingly, the post-treatment glucose levels and AR activity were positively correlated with kidney/body weight of 34 herbs treated diabetic mice (p = 0.02, 0.04 respectively). Several potential antidiabetic herbs derived from Chinese traditional pharmacopeia such as Dioscorea opposite, Pueraria lobata, Codonopsis pilosula and Ramulus cinnamomi, have been found to exert a beneficial action on diabetes and diabetic complications via multi-mechanisms.
    Journal of ethnopharmacology 07/2011; 137(3):1135-42. · 2.32 Impact Factor
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    ABSTRACT: Some new 7-alkoxyhesperetin derivatives, 7-methoxy-(c), 7-butoxy-(d), 7-octyloxy-(e), 7-decyloxy-(f), and 7-dodecyloxyhesperetin(g), were synthesized and confirmed by UV, IR, 1H NMR, and MS spectra data. The series of the synthesized compounds has been screened for their antibacterial activity in vitro and evaluated their structure–activity relationships. Substitution of the H with alkyl groups at C-7-OH led to significant change of their antibacterial activity. The antibacterial activity of 7-alkoxyhesperetin derivatives increased with the elongating of the length of aliphatic chain, and the maximum activity was reached at twelve carbon atoms. Compound f showed the highest antibacterial activity among all the compounds. KeywordsSynthesis–7-alkoxyhesperetin derivatives–Hesperetin–Antibacterial activity
    Medicinal Chemistry Research 01/2011; 20(8):1200-1205. · 1.61 Impact Factor
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    ABSTRACT: To study the hypolipidemic active compounds from Crataegus pinnatifida and mechanism of action of those. Guided by the inhibitory activity to HMG-CoA reductase, the active compounds were separated and purified with macroporous resin and silica gel. Four active compounds were obtained, which were quercetin, hyperoside, rutin and chlorogenic acid, the sum of their inhibitory rate was 50.01%, and the total inhibitory rate of the mixture of four active compounds matched was 79.48%. Quercetin and hyperoside were the principle active components inhibiting HMG-CoA reductase in Hawthorn fruit, and there were synergistic action among them.
    Zhongguo Zhong yao za zhi = Zhongguo zhongyao zazhi = China journal of Chinese materia medica 09/2010; 35(18):2428-31.
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    ABSTRACT: To determine the pharmacokinetics, distribution and mutual transformation of the total alkaloids, jatrorrhizine, coptisine, berberine and palmatine from Coptis chinensis in rats. After the total alkaloids and berberine were fed into rats, their contents in plasma, tissues and gastrointestinal tract were determined by reversed-phase HPLC. The peak times of berberine in blood were 2.0 h (Cmax 3.7 mg x L(-1)) and 5.0 h Cmax 2.8 mg x L(-1)), respectively. Berberine in rat blood can be transformed into jatrorrhizine. After the rats were fed with the total alkaloids by gavage, the content of berberine was decreased monotonously, while coptisine, palmatine and jatrorrhizine contents were increased gradually in the stomach, it speculated that berberine may be transformed into jatrorrhizine in the stomach. Animal experiments showed that berberine and palmatine were mainly distributed in the lungs of animals, followed by the distribution in the liver, while jatrorrhizine and coptisine was mainly in the liver, then in the lungs. Berberine could transform into jatrorrhizine. The mechanism on the appearance of two maximum blood concentration of berberine in blood could be explained with the propulsion of the gastrointestinal tract partly.
    Zhongguo Zhong yao za zhi = Zhongguo zhongyao zazhi = China journal of Chinese materia medica 08/2010; 35(15):2017-20.
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    ABSTRACT: The binding reaction of sodium houttuyfonate analogues (SHAs) to bovine serum albumin (BSA) was studied by fluorescence quenching. Both dynamic and static interactions are involved in the quenching process. SHAs with shorter carbon chains are more likely to undergo a predominantly dynamic quench over a static quench. In contrast, SHAs with longer carbon chains act as static quenchers. Quench efficiency is in the order SHA-C8>SHA-C10>SHA-C12≈SHA-C14>SHA-C6. It was also observed that the two tryptophan residues of BSA are accessible to SHAs. Most of the SHAs have two binding sites, except SHA-C12, which has one. Binding of SHAs to BSA is as a result of spontaneous intermolecular interaction at the experimental temperature. We concluded that SHAs bind to and may be transported by BSA. KeywordsBovine serum albumin-Sodium houttuyfonate analogues-Fluorescence quench-Binding affinity
    Medicinal Chemistry Research 01/2010; 19(9):1287-1295. · 1.61 Impact Factor
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    ABSTRACT: In this study the effects of houttuyfonate homologues (HOU-Cn) on the surface and shape, the lipid fluidity and the protein conformation, the fatty acid compositions and fatty acid synthase II (FAS II) of B. subtilis were studied to elucidate the antibacterial mechanism of HOU-Cn against Bacillus subtilis. The scanning electronic microscope (SEM) results showed that the glycocalyx on the surface of B. subtilis disappeared and the cell became smaller after being treated with HOU-Cn. During the co-incubation of HOU-Cn and B. subtilis, HOU-Cn was decomposed into alkyl acyl aldehyde and sodium sulfite rapidly. Then alkyl acyl aldehyde was congregated onto cell membrane and inserted into lipid bilayer, further increased the fluidity of membrane and changed the conformation of membrane protein by hydrophobic binding. Subsequently, HOU-Cn inhibited the FAS II activity, and decreased the synthesis of fatty acids, especially increased the percentage of saturated fatty acid. HOU-Cn showed a strong antibacterial activity against G+-bacteria by a multi-target antibacterial mechanism.
    Colloids and Surfaces A Physicochemical and Engineering Aspects 10/2009; 350(1):130-135. · 2.11 Impact Factor
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    ABSTRACT: To evaluate the effect of additives on absorption of Coptis chinensis total alkaloid and their pharmacokinetics in mice. The mice were fed with the mixture of C. chinensis total alkaloids and additives (1:1). And then the feces and orbital blood were taken to detect the content of total alkaloids by HPLC and their pharmacokinetics. Glutin could make the absorption of jatrorrhizine, coptisine, berberine and total alkaloids increased by 30%. Tween 80 and arabic gum did not affect the absorption of berberine, but inhibit that of other alkaloids. There had no influence of lecithin on the absorption of alkaloids. The peak time of total alkaloids in blood were 2 h (Cmax 1=5.9 mg x L(-1)) and 5.0 h (Cmax 2=3.4 mg x L(-1)), respectively, AUC was 17.6 mg x h x L(-1), the elimination of Half-life t1/2 was 5.2 h. After addition of glutin, the peak time of total alkaloids in blood were 1.5 h (Cmax 1=7.6 mg x L(-1)) and 4.8 h (Cmax 2=8.5 mg x L(-1)), AUC was up to 31.1 mg x h(-1) x L(-1), the elimination of Half-life t1/2 was 6.2 h. Glutin could accelerate the mice on the absorption of C. chinensis total alkaloids, to extend the elimination half-life, increase the blood concentration and bioavailability.
    Zhongguo Zhong yao za zhi = Zhongguo zhongyao zazhi = China journal of Chinese materia medica 03/2009; 34(3):344-8.