Influence of different heat transfer models on therapeutic temperature prediction and heat-induced damage during magnetic hyperthermia.

Magnetic hyperthermia regulates the therapeutic temperature within a specific range to damage malignant cells after exposing the magnetic nanoparticles inside tumor tissue to an alternating magnetic field. The therapeutic temperature of living tissues can be generally predicted using Pennes' bio-heat equation after ignoring both the inhomogeneity of biological structure and the microstructural responses. Although various of the bio-heat transfer models proposed in literature fix these shortages, there is still a lack of a comprehensive report on investigating the discrepancy for different models when applied in the magnetic hyperthermia context. This study compares four different bio-heat equations in terms of the therapeutic temperature distribution and the heat-induced damage situation for a proposed geometric model, which is established based on computed tomography images of a tumor bearing mouse. The therapeutic temperature is also used as an index to evaluate the effect of two key relaxation times for the phase lag behavior on bio-heat transfer. Moreover, this work evaluates the effects of two blood perfusion rates on both the treatment temperature and the cumulative equivalent heating minutes at 43 °C. Numerical analysis results reveal that relaxation times for phase-lag behavior as well as the porosity for living tissues directly affect the therapeutic temperature variation and ultimately the thermal damage for the malignant tissue during magnetic hyperthermia. The dual-phase-lag equation can be converted into Pennes' equation and simple-phase-lag equation when relaxation times meet specific conditions during the process of heat transfer. In addition, different blood perfusion rates can result in an amplitude discrepancy for treatment temperature, but this parameter does not change the characteristics of thermal propagation during therapy.

Scrophularia ningpoensis Hemsl: a review of its phytochemistry, pharmacology, quality control and pharmacokinetics.

OBJECTIVES: Scrophularia ningpoensis Hemsl (SNH) is a commonly used medicinal plant in East Asia. Scrophulariae Radix (SR) is the dried roots of SNH, and is one of the most commonly used medicinal parts of SNH, and is an essential traditional medicine and widely used in East Asia for more than 2000 years. SR is used for clearing away heat and cooling blood, nourishing Yin and reducing fire, detoxicating and resolving a mass. The purpose of this paper is to systematically review the phytochemistry, pharmacology, quality control and pharmacokinetics of SNH based on the surveyed and summarized literature. KEY FINDINGS: Up to now, iridoids, phenolic glycosides, phenolic acids, alkaloids, flavonoids, triterpenes and other compounds have been isolated and identified from SNH. The extract and chemical components of SNH exerts multiple pharmacological effects, such as hepatoprotective effect, anti-inflammatory effect, neuroprotective effect, anti-ventricular remodeling effect and other activities. Various methods have been developed for the quality control of SNH, mainly for SR. Some bioactive compounds in SNH exhibited different pharmacokinetic behaviours and individual metabolic transformation profiles. SUMMARY: This review will contribute to understanding the correlation between the pharmacological activities and the traditional usage of SNH, and useful to rational use and drug development in the future.

Pillar-beam structures prevent layered cathode materials from destructive phase transitions.

Energy storage with high energy density and low cost has been the subject of a decades-long pursuit. Sodium-ion batteries are well expected because they utilize abundant resources. However, the lack of competent cathodes with both large capacities and long cycle lives prevents the commercialization of sodium-ion batteries. Conventional cathodes with hexagonal-P2-type structures suffer from structural degradations when the sodium content falls below 33%, or when the integral anions participate in gas evolution reactions. Here, we show a "pillar-beam" structure for sodium-ion battery cathodes where a few inert potassium ions uphold the layer-structured framework, while the working sodium ions could diffuse freely. The thus-created unorthodox orthogonal-P2 K0.4[Ni0.2Mn0.8]O2 cathode delivers a capacity of 194 mAh/g at 0.1 C, a rate capacity of 84% at 1 C, and an 86% capacity retention after 500 cycles at 1 C. The addition of the potassium ions boosts simultaneously the energy density and the cycle life.

Systematic exploration of Astragalus membranaceus and Panax ginseng as immune regulators: Insights from the comparative biological and computational analysis.

BACKGROUND: Immune system plays a decisive role for defending various pathogenic microorganisms. Astragalus membranaceus (AM) and Panax ginseng (PG) are two tonic herbs used in traditional Chinese medicine (TCM) as immune booster and help to control diseases with their healthy synergistic effect on immune system. PURPOSE: This study was aimed to investigate the promote effect and molecular mechanisms of AM and PG on immune system as booster and to control the target diseases using animal and computational systematic study. METHODS: Computational models including absorption, distribution, metabolism, and elimination (ADME) with weighted ensemble similarity (WES) algorithm-based models and ClueGo network analysis were used to find the potential bioactive compounds targets and pathways, which were responsible for immune regulation. Viscera index analysis, proliferation activity of splenic lymphocytes and cytotoxic activity of NK cells assays were performed to validate the effect of AM and PG on immune system of long-term administrated mice. Metabonomic study of mice plasma was conducted to investigate effect of AM and PG on the endogenous metabolic perturbations, together with correlation analysis. RESULTS: AM and PG simultaneously showed the ability to strengthen the immune system function including enhancement of spleen and thymus index, proliferation of splenic lymphocytes and cytotoxic activity of NK cells. Besides, the different molecular mechanisms of AM and PG on immune regulation were also investigated by analyzing the potential bioactive compounds, enzymes actions and pathways. Quercetin, formononetin and kaempferol were the main immune-related compounds in AM, while ginsenoside Ra1, ginsenoside Rh1 and kaempferol in PG. About 10 target proteins were found close to immune regulation, including acetylcholinesterase (ACHE, common target in AM and PG), sphingosine kinase 1(SPHK1), cytidine deaminase (CDA), and Choline O-acetyltransferase (CHAT). Glycerophospholipid metabolism was regulated in both AM and PG groups. Pyrimidine metabolism and sphingolipid metabolism were considered as the special pathway in AM groups. Energy metabolism and glycerolipid metabolism were the special pathways in PG groups. CONCLUSION: A novel comprehensive molecular mechanism analysis method was established and applied to clarify the scientific connotation of AM and PG as immune regulation, with similar herbal tonic effect provided in clinical practice of TCM, which can provide a new line of research for drug development (immune booster) using AM and PG.

The bioavailability and excretion of an antitussive compound IAsp-N-Glc in rats by validated UPLC-MS/MS methods.

IAsp-N-Glc is a potential antitussive agent that is first reported to be isolated from Ginkgo Semen, but the bioavailability and excretion of IAsp-N-Glc are unknown. Therefore, we carried out our study to obtain the bioavailability and excretion profiles of IAsp-N-Glc in rats. Rapid, specific, and reliable quantification methods for the measurement of IAsp-N-Glc in rat plasma and fecal samples by using ultra-high-performance liquid chromatography coupled with triple quadrupole mass spectrometry were developed and validated. A C18 column was used for the separation of IAsp-N-Glc and internal standards, and water (containing 0.1% formic acid) and acetonitrile were chosen as the mobile phase for the separation in the flow-gradient mode. In the ranges of 37.5-7500 ng/mL and 120-30000 ng/mL, the calibration curves of IAsp-N-Glc exhibited satisfactory linearity for plasma and fecal samples with each linear correlation coefficient higher than 0.99, respectively. The methods were reproducible and reliable. The analytes were stable, and no apparent matrix effects were observed. The bioanalytical methods were successfully used to study the pharmacokinetics and excretion of IAsp-N-Glc in rats. Oral administration of IAsp-N-Glc exhibited a low absolute oral bioavailability (1.83±0.09%), and 59.63±6.29% of IAsp-N-Glc was excreted in feces. This report is the first to describe the bioavailability and excretion of IAsp-N-Glc in rats and will lay the foundation for the in-depth study and drug development of IAsp-N-Glc.

Quantification of 10 bioactive components of Yazhangsan in rat plasma by LC-MS/MS and its application.

Yazhangsan (YZS) is a common prescription for the treatment of cough and asthma caused by wind-cold. The purpose of this study was to investigate the pharmacokinetic profiles of 10 bioactive components in YZS. A simple, sensitive and reliable high-performance liquid chromatography coupled with a triple-quadruple mass spectrometry method (LC-MS/MS) was developed and fully validated in this study for the measurement of these 10 bioactive compounds in rat plasma. One-step protein precipitation method using methanol was applied to the treatment of rat plasma samples. Chromatographic separation was conducted on a C18 column by gradient elution, and water (containing 0.1% formic acid) and acetonitrile were chosen as the mobile phase. The analytes were quantified by using a mass spectrometer in multiple reaction monitoring scanning mode, and electrospray ionization was performed in positive and negative ion modes. The established method met the requirements for the quantification of these 10 bioactive compounds in biological samples, and it was successfully applied to the pharmacokinetic study of 10 components in rats after the intragastrical administration of YZS. This study will lay a foundation for the investigation of the mechanism of action of YZS and provide useful data for the rational use of YZS in clinical.

[Application of quality constant method in grade evaluation of Aurantii Fructus Immaturus pieces].

The grade classification of Chinese herbal medicines and their decoction pieces has always been a hot issue in the industry. In the trading history of Chinese herbal medicine,buyers and sellers often determine the price according to quality,so the naturally formed specifications and grades are changing with the change of technology and the increasing demand of the public for medical care.The planting,processing and circulation methods of Chinese medicinal materials have also changed greatly. Under the mode of pursuing yield and short-term benefit,the traditional rating evaluation method has been difficult to be used in the current quality status of prepared slices. Aurantii Fructus Immaturus is a genuine medicinal material of Jiangxi province,which is widely used,but has different quality levels on the market. In this paper,the quality levels were evaluated by the mass constant method. A set of grading method of Aurantii Fructus Immaturus slices was established,laying a foundation for " high quality and high price" Aurantii Fructus Immaturus slices. The grading method of Chinese herbal slices with quality constant was applied to 16 batches of Aurantii Fructus Immaturus slices collected form the market,and the final assessment results were as follows for different piece shapes( hemispherical type and thin type)respectively. The hemispherical Aurantii Fructus Immaturus pieces: quality constant ≥1. 11 for the first grade,< 1. 11 but ≥0. 69 for the second grade,and <0. 69 for the third grade. The thin type Aurantii Fructus Immaturus pieces: quality constant ≥0. 024 for the first grade,<0. 024 but ≥0. 015 for the second grade,and <0. 015 for the third grade. This work indicated that the quality constants grading method can be used to objectively classify the grades of traditional Chinese medicine,providing basis for standardizing market behavior and providing useful reference for grading of hemispherical or thin Aurantii Fructus Immaturus pieces.

[Research on quality standard of processed Cinnamomi Cortex decoction pieces containing volatile oil].

To build the quality standard of processed Cinnamomi Cortex standard decoction and provide quality reference for Cinnamomi Cortex formula granules. Fourteen batches of Cinnamomi Cortex standard decoction pieces were prepared according to the preparation requirements for standard decoction of Chinese herbal medicine containing volatile oil. With cinnamaldehyde as the quantitative index, the transfer rate and extraction rate were calculated; pH value was determined and HPLC fingerprint analysis method was established. By the measurement of 14 batches of standard decoction, the transfer rate ranged from 25.0% to 68.4%; the extraction rate was at a range of 3.7% to 10.1% and pH was 3.72 to 5.48. Then the Similarity Evaluation System for Chromatographic Fingerprint of Traditional Chinese Medicine (2012A) was used to analyze and compare the fingerprints. Four common peaks were determined and three were identified including coumarin (peak 1), cinnamic acid (peak 2) and cinnamaldehyde (peak 3). Moreover, the similarity was 1.0. This study established an HPLC fingerprint analysis method of processed Cinnamomi Cortex standard decoction. The method showed good precision, stability and repeatability in fingerprint analysis, with significance in identification.

[Standard decoction of Leonuri Herba].

To build an evaluation standard for quality of Leonuri Herba standard decoction. 13 batches of Leonuri Herba standard decoction with different quality were prepared. The contents of leonurine hydrochloride and stachydrine hydrochloride were determined; then the transfer rate and the extract rate were calculated and pH value was measured; and HPLC fingerprint method was established for analysis. The results of 13 batches of samples revealed that the transfer rate of leonurine hydrochloride and stachydrine hydrochloride was 30.0%-53.4% and 67.0%-82.6%, respectively; the extract rate was 12.1%-18.3% and the pH value was 5.87-6.22. Moreover, 12 common chromatographic peaks were determined based on fingerprint by using Similarity Evaluation System for Chromatographic fingerprint of Traditional Chinese Medicine (2012A). The similarity of 13 batches of samples was analyzed and compared, and the results showed that the similarity was higher than 0.9. In this study, the preparation method for Leonuri Herba decoction was standard, with high similarity in fingerprint, showing high precision, stability and repeatability in fingerprint analysis. Thus, this study can provide a reference for the quality control of Leonuri Herba dispensing granules.

[Grades evaluation of Scutellariae Radix slices based on quality constant].

By measuring the morphological indexes and the marker components content of 22 batches of Scutellariae Radix slices as well as calculating the quality constant, this research was aimed to establish a new method of evaluating the specifications and grades of Scutellariae Radix slices. The quality constants of these samples were in the range of 0.04-0.49, which can be divided into several grades based on the real requirement. If they were divided into three grades, the quality constant was ≥0.39 for the first grade, <0.39 but ≥0.24 for the second grade, and <0.24 for the third grade. This work indicated that the quality constants characterizing both apparent parameters and intrinsic quality can be used as a comprehensive evaluation index to classify the grades of traditional Chinese medicine quantitatively, clearly and objectively. The research results in this paper would provide new ideas and references for evaluating the specifications and grades of traditional Chinese medicines.

[Explore a method for formulation of limit standard of toxic components in traditional Chinese medicine:aristolochic acid as a case study].

It is urgent to establish the limit standard of toxic components of Chinese herbal medicine, since the safety of traditional Chinese medicine (TCM) has attracted more and more attention.This paper analyzes the present situation and problems in the study of the limit standard of toxic components of Chinese herbal medicine. In addition, the current methods for setting the limit standards of toxic ingredients of TCM are reviewed in this paper, and we also propose a theoretical calculation method for setting the limit standards of toxic ingredients of TCM. Employing aristolochic acid as a case study, we formulate the limit standard of toxic components of Chinese herbal medicine. We believe this paper would provide some useful suggesting for formulating limits standard of toxic components of TCM.

[Application of relative quality constant in grades evaluation of Glycyrrizae Radix et Rhizome pieces].

Quality constant evaluation is a comprehensive method for grades evaluation of traditional Chinese medicine pieces, but when it comes to Glycyrrizae Radix et Rhizome pieces, grades evaluation is diverged due to significant difference in contents of liquiritin and glycyrrhizic acid and unreasonable weight of index. To solve this problem, we have established a relative quality constant method in this paper to evaluate grades of Glycyrrizae Radix et Rhizome pieces. Twenty-nine batches of different quality samples were collected and tested, and finally, 17 batches of them were chosen as researcher objects. The results revealed that the range of the relative quality constant of these samples was from 1.78 to 11.49. When Glycyrrizae Radix et Rhizome pieces are divided into three grades: the relative quality constant of first grade is greater than or equal to 9.19; the second grade is greater than or equal to 5.75 but less than 9.19; while the third grade is less than 5.75. This research indicates that relative quality constant can divide the grades of herbal pieces in a scientific, reasonable, objective and specific way and remedy the shortage of quality constant perfectly. It provides a novel mode for grading pieces of Chinese medicine that contains multi-target ingredients.

Impact of parameter fluctuations on the performance of ethanol precipitation in production of Re Du Ning Injections, based on HPLC fingerprints and principal component analysis.

The present study was designed to determine the relationships between the performance of ethanol precipitation and seven process parameters in the ethanol precipitation process of Re Du Ning Injections, including concentrate density, concentrate temperature, ethanol content, flow rate and stir rate in the addition of ethanol, precipitation time, and precipitation temperature. Under the experimental and simulated production conditions, a series of precipitated resultants were prepared by changing these variables one by one, and then examined by HPLC fingerprint analyses. Different from the traditional evaluation model based on single or a few constituents, the fingerprint data of every parameter fluctuation test was processed with Principal Component Analysis (PCA) to comprehensively assess the performance of ethanol precipitation. Our results showed that concentrate density, ethanol content, and precipitation time were the most important parameters that influence the recovery of active compounds in precipitation resultants. The present study would provide some reference for pharmaceutical scientists engaged in research on pharmaceutical process optimization and help pharmaceutical enterprises adapt a scientific and reasonable cost-effective approach to ensure the batch-to-batch quality consistency of the final products.

[Application of high performance liquid-ion trap mass spectrometry in analyzing saponins in sodium aescinate].

Sodium aescinate, which is produced from saponins of Chinese Buckeye Seed, is a prescription drug for treatment of brain edema and all kinds of swellings caused by surgery. In this article, high-performance liquid chromatography/ion trap (HPLC-IT) mass spectrometry was applied to study the characteristic ions of ten reference substances, namely escin Ⅰa, escin Ⅰb, isoescin Ⅰa, isoescin Ⅰb, aesculiside A, aesculiside B, aesculuside A, escin Ⅳc, escinⅡa and escin Ⅴ, which were isolated from aescinate. Furthermore, 19 saponin compounds were predicted in sodium aescinate, besides the above mentioned reference substances. The study showed that sapogenins in sodium aescinate had two structural types, namely protoaescigenin and barringenol C, and the substituent acetyl, tigloyl or angeloyl was usually located at C-21, C-22 or C-28 position. Among these predicted saponins, their sugar chains were all located at C-3 position consisting of glucose and glucuronide. This study provides experimental data for chemical constituents in sodium aescinate and scientific basis for quality and safety evaluation.

[Research on Chinese medicine pairs effects of Panax notoginseng and Bletilla striata before and after compatibility on contents of notoginsenosides].

To discuss the synergistic mechanism of compatible use of two medicinal herbs,Panax notoginseng and Bletilla striata, an HPLC was established to determine two ginseng saponins (20S)-ginseng saponin Rg3 and ginseng saponin Rh4 contained in single decoction of Panax notoginseng as well as in compound decoction of Panax notoginseng and Bletillastriata in different compatibility ratio (1∶0.5, 1∶1, 1∶2), followed by analyzing the impact of amount of notoginsenosides after compatibility. As a result, compared with the single decoction of Panax notoginseng, the contents of ginseng saponin Rg3 and ginseng saponin Rh4 in the compound decoction of Panax notoginseng and Bletillastriata were on the rise as the increasement of the amount of Bletillastriata. The contents of the notoginsengsaponin R1, ginseng saponin Rg1 and ginseng saponin Rb1 of Panax notoginseng single decoction were significantly decreased after compatibility. Therefore, after compatibility, it was more easy to produce (20S)-ginseng saponin Rg3 and ginseng saponin Rh4.This study can extend to a method of preparation of (20S)-ginseng saponin Rg3 and ginseng saponin Rh4. Furthermore, after compatibility, two ginseng saponins which had lipase inhibitory effect were both increased significantly, indicating that the compatibility of these two herb medicines may have effect on losing weight.

Pharmacokinetics of Maxing Shigan decoction in normal rats and RSV pneumonia model rats by HPLC-MS/MS.

To establish a LC-MS/MS method to determine the concentrations of liquiritin, glycyrrhizin, glycyrrhetinic acid, amygdalin, amygdalin prunasin, ephedrine, pseudoephedrine and methylephedrine of Maxing Shigan decoction in rat plasma, and study the differences on their pharmacokinetic process in normal rats and RSV pneumonia model rats. After normal rats and RSV pneumonia model rats were orally administered with Maxing Shigan decoction, the blood was collected from retinal vein plexus of different time points. Specifically, tetrahydropalmatine was taken as internal standard for determining ephedrine, while chloramphenicol was taken as internal standard for determining other components. After plasma samples were pre-treated as the above, the supernatant was dried with nitrogen blowing concentrator and then redissolved with methylalcohol. The chromatography was eluted with mobile phase consisted of acetonitrile and 0.1% formic acid solution in a gradient manner. ESI sources were adopted to scan ingredients in ephedra in a positive ion scanning mode and other ingredientsin a negative ion scanning mode. The multiple-reaction monitoring (MRM) method was developed the plasma concentration of each active component. The pharmacokinetic parameters of each group were calculated by using Win-Nonlin 4.1 software and put into the statistical analysis. The result showed the plasma concentration of the eight active ingredients, i.e., liquiritin, glycyrrhizin, glycyrrhetinic acid, amygdalin, amygdalin prunasin, ephedrine, pseudoephedrine and methylephedrine within the ranges of 1.04-1040, 1.04-1040, 0.89-445, 1.05-4200, 1.25-2490, 0.3-480, 0.3-480, 0.3-480 microg x L(-1), with a good linearity and satisfactory precision, recovery and stability in the above ingredients. After modeling, except for glycyrrhetinic acid whose pharmacokinetic parameters were lacked due to the data missing, all of the rest components showed significant higher Cmax, AUC(0-1) and lower clearance rate (CL) than that of the normal group, indicating the increase in absorption in rats in the pathological state by reducing the clearance rate. The method is accurate and sensitive and so can be used to determine the plasma concentrations of the eight active ingredients in Maxing Shigan decoction. RSV pneumonia-infected rats absorbed more ingredients in Maxing Shigan decoction.

[Traditional Chinese medicine pairs (III)--effect of extract of Ginseng Radix et Rhizoma and Puerariae Lobatae Radix on intestinal absorption in rats].

This study focused on the intestinal absorption of traditional Chinese medicines (TCM) to reveal the scientific connotation of the compatibility of TCM pairs. The single pass intestinal perfusion (SPIP) was used in rats to compare the absorption of single extracts from Puerariae Lobatae Radix, single extracts from Ginseng Radix et Rhizoma, combined extracts from Puerariae Lobatae Radix and Ginseng Radix et Rhizoma and Puerariae Lobatae Radix and Ginseng Radix et Rhizoma mixture in rats. The content of puerarin, ginsenoside Rg1, ginsenoside Re and ginsenoside Rb1 in liquid were tested by HPLC. The speed constant (Ka) and apparent permeability coefficients (Papp) were calculated and compared. Specifically, the order of puerarin Ka and Papp values from high to low was Ginseng Radix et Rhizoma and Puerariae Lobatae Radix mixture > single extracts from Puerariae Lobatae Radix > combined extracts from Ginseng Radix et Rhizoma and Puerariae Lobatae Radix; the order of ginsenosides Ka and Papp values from high to low was Ginseng Radix et Rhizoma and Puerariae Lobatae Radix mixture > single extracts from Ginseng Radix et Rhizoma > combined extracts from Ginseng Radix et Rhizoma and Puerariae Lobatae Radix. The combined administration of Ginseng Radix et Rhizoma and Puerariae Lobatae Radix may improve the absorption in the intestinal tract.

[Simultaneous determination of 9 major components of dachengqi tang in rat plasma by UPLC-MS/MS].

The study established a UPLC-MS/MS method that is used for simultaneous determination nine major bioactive compounds of Dachengqi Tang in rat plasma. Using Aglient C18 column (2.1 mm x 50 mm,1.7 microm) was chromatographed, using methanol-5 mmol x L(-1) ammonium formate mobile phase gradient, elution 0.3 mL x min(-1). In the plasma pre-treatment process, not only the method of methanol and acetonitrile protein precipitation was investigated, and different factors extraction solvent, the type of the scroll time, the number and the type of extraction solvent, the extraction volume of the extraction solution of liquid-liquid extraction is investigated. Finally, with ibuprofen as an internal standard, using ethyl acetate liquid-liquid extraction method pretreatment blood, N2 dry reconstituted supernatant after centrifugation UPLC-MS/MS analysis, in electrospray ionization (ESI) negative mode, using multiple reaction monitoring mode for testing. The linear range of emodin, rhein, aloe-emodin, chrysophanol, magnolol, honokiol, hesperidin and hesperitin is 0.33-660, 0.40-792, 0.41-827, 0.34-680, 0.45-907, 0.46-927, 0.43-867, 0.34-683, 0.39-787 microg x L(-1) respectively, good linear relationship; and extraction recovery were greater than 69.39%, days after the day of the RSD is less than 15%. This method can be used to study the rat gastric large bearing gas after Dachengqi Tang, the simultaneous determination of nine components in plasma for its pharmacokinetics and efficacy material base to provide a theoretical basis.

Interaction of baicalin with berberine for glucose uptake in 3T3-L1 adipocytes and HepG2 hepatocytes.

ETHNOPHARMACOLOGICAL RELEVANCE: Baicalin and berberine are important coexisting constituents of the combination of Radix Scutellariae and Rhizoma Coptidis, known as scutellaria-coptis herb couple (SC), which has heat clearing and detoxifying effects. The aims of the present study were to investigate the effects of the combination of baicalin+berberine on glucose uptake in 3T3-L1 adipocytes or HepG2 cells. MATERIALS AND METHODS: Insulin-resistant adipocytes and hepatocytes models were established. Glucose consumption was assayed to evaluate the effects of berberine, baicalin, and berberine+baicalin on glucose uptake, and the interaction of baicalin with berberine for glucose uptake was evaluated in 3T3-L1 adipocytes or HepG2 cells. Moreover, the effects of baicalin on the dose-effect relationship of berberine for glucose uptake was also evaluated in 3T3-L1 adipocytes. RESULTS: The results of the present study demonstrated that berberine increased glucose consumption in 3T3-L1 adipocytes and HepG2 hepatocytes in a dose-dependent manner. In contrast, statistical analyses indicated that baicalin (in doses up to 100µmol/L) produced no obvious effect. The effect of berberine+baicalin on glucose uptake was better than that of berberine or baicalin alone, which indicated that berberine and baicalin had the trend of synergetic effect on glucose uptake. Furthermore, these results showed that the synergistic effect occurred in a specific dose range, while the antagonistic effect was present in another dose range in the presence of 10µmol/L baicalin. Interestingly, the entire dose-response curves of berberine shifted down in the presence of 100µmol/L baicalin, and baicalin antagonised the effect of berberine on glucose uptake in 3T3-L1 adipocytes. CONCLUSIONS: The results of the present study showed that berberine dose-dependently increased glucose consumption in 3T3-L1 adipocytes and HepG2 hepatocytes. Furthermore, interaction of baicalin with berberine was additive at low doses of baicalin and antagonistic at higher baicalin doses. Thus, it is possible that baicalin is a partial agonist. These results provided a basis for the study of the TCM compatibility mechanism and a new insight into the application for Gegen Qinlian Decoction (GGQLD) or SC in the clinic.