Recent advances in cancer cell bionic nanoparticles for tumour therapy.

Nanoparticle-based drug delivery systems have found extensive use in delivering oncology therapeutics; however, some delivery vehicles still exhibit rapid immune clearance, lack of biocompatibility and insufficient targeting. In recent years, bionanoparticles constructed from tumour cell membranes have gained momentum as tumour-targeting therapeutic agents. Cancer cell membrane-coated nanoparticles (CCMCNPs) typically consist of a drug-loaded nanoparticle core coated with cancer cell membrane. CCMCNPs retain homologous tumour cell surface antigens, receptors and proteins, and it has been shown that the modified nanoparticles exhibit better homologous targeting, immune escape and biocompatibility. CCMCNPs are now widely used in a variety of cancer treatments, including photothermal, photodynamic and sonodynamic therapies, chemotherapy, immunotherapy, chemodynamical therapy or other combination therapies. This article presents different therapeutic approaches using multimodal antitumour therapy-combination of two or more therapies that treat tumours synergistically-based on tumour cell membrane systems. The advantages of CCMCNPs in different cancer treatments in recent years are summarised, thus, providing new strategies for cancer treatment research.

[Mechanism of Huangjing Qianshi Decoction in treatment of prediabetic mice based on transcriptome sequencing].

Based on transcriptome sequencing technology, the mouse model of prediabetes treated with Huangjing Qianshi Decoction was sequenced to explore the possible mechanism of treating prediabetes. First of all, transcriptome sequencing was performed on the normal BKS-DB mouse group, the prediabetic model group, and the Huangjing Qianshi Decoction treatment group(treatment group) to obtain differentially expressed genes in the skeletal muscle samples of mice. The serum biochemical indexes were detected in each group to screen out the core genes of Huangjing Qianshi Decoction in prediabetes. Gene Ontology(GO) database and Kyoto Encyclopedia of Genes and Genomes(KEGG) database were used to conduct signaling pathway enrichment analysis of differentially expressed genes, and real-time quantitative polymerase chain reaction(RT-qPCR) was used to verify them. The results showed that the levels of fasting blood glucose(FBG), fasting insulin(FINS), insulin resistance index(HOMA-IR), total cholesterol(TC), triglycerides(TG), and low-density lipoprotein cholesterol(LDL-C) in the mouse model were significantly decreased after treatment with Huangjing Qianshi Decoction. In the results of differential gene screening, there were 1 666 differentially expressed genes in the model group as compared with the normal group, and there were 971 differentially expressed genes in the treatment group as compared with the model group. Among them, interleukin-6(IL-6) and NR3C2 genes, which were closely related to the regulation of insulin resis-tance function, were significantly up-regulated between the model group and the normal group, and vascular endothelial growth factor A(VEGFA) genes were significantly down-regulated between the model group and the normal group. However, the expression results of IL-6, NR3C2, and VEGFA genes were adverse between the treatment group and the model group. GO functional enrichment analysis found that the biological process annotation mainly focused on cell synthesis, cycle, and metabolism; cell component annotation mainly focused on organelles and internal components; and molecular function annotation mainly focused on binding molecular functions. KEGG pathway enrichment analysis found that it involved the protein tyrosine kinase 6(PTK6) pathway, CD28-dependent phosphoinositide 3-kinase/protein kinase B(PI3K/AKT) pathway, p53 pathway, etc. Therefore, Huangjing Qianshi Decoction can improve the state of prediabetes, and the mechanism may be related to cell cycle and apoptosis, PI3K/AKT pathway, p53 pathway, and other biological pathways regulated by IL-6, NR3C2, and VEGFA.

Use of different ligand modification liposomes to evaluate the anti-liver tumor activity of cantharidin.

In this study, cantharidin(CTD), a bioactive terpenoid in traditional Chinese medicine cantharidin, was selected as a model component to construct novel nano liposome delivery systems for hepatocellular carcinoma therapy. Previous studies have shown that although cantharidin has definite curative effects on primary liver cancer, it is associated with numerous toxic and side effects. Therefore, based on the glycyrrhetinic acid (GA) binding site and the asialoglycoprotein receptor (ASGPR) on the hepatocyte membrane, the surface of CTD liposomes was modified with stearyl alcohol galactoside (SA-Gal) or/and the newly synthesized 3-succinic-30-stearyl deoxyglycyrrhetinic acid (11-DGA-Suc) ligands, and the physicochemical properties, pharmacokinetics, in vivo and in vitro anti-liver tumor activity and its mechanism of modified liposomes were investigated. Compared to CTD-lip, SA-Gal-CTD-lip, and 11-DGA-Suc + SA-Gal-CTD-lip, 11-DGA-Suc-CTD-lip showed stronger cytotoxicity and increased inhibition of HepG2 cell migration had the highest apoptosis rate. The cell cycle results indicated that HepG2 cells was arrested mainly at G0/G1phase and G2/M phase. The results of in vivo pharmacokinetic experiments revealed that the distribution of modified liposomes in the liver was significantly increased compared with that of unmodified liposome. In vivo tumor inhibition experiment showed that 11-DGA-Suc-CTD-lip had excellent tumor inhibition, and the tumor inhibition rates was 80.96%. The 11-DGA-Suc-CTD-lip group also displayed the strongest proliferation inhibition with the lowest proliferation index of 7% in PCNA assay and the highest apoptotic index of 49% in TUNEL assay. Taken together, our findings provide a promising solution for improving the targeting of nano liposomes and further demonstrates the encouraging potential of poor solubility and high toxicity drugs applicable to tumor therapy.

Buyang Huanwu decoction affects gut microbiota and lipid metabolism in a ZDF rat model of co-morbid type 2 diabetes mellitus and obesity: An integrated metabolomics analysis.

Type 2 diabetes mellitus (T2DM) is a chronic disease associated with many severe complications such as blindness, amputation, renal failure, and cardiovascular disease. Currently, the prevention and treatment of T2DM is a major global challenge as the number of aging and obese people is increasing. Traditional Chinese medicine offers the advantages of multi-target holistic and individual treatment for obesity and type 2 diabetes. However, most of the TCMs for T2DM are not scientifically evaluated. Here, Buyang Huanwu decoction (BYHWD), a widely used TCM formula, was used to explore scientific pharmacological activity against T2DM in rat models. First, BYHWD exhibited excellent inhibitory actions against body fat accumulation and increased blood triglyceride levels, and a high-fat diet (HFD) induced blood glucose elevation in diabetic rats. Moreover, 16S rDNA sequencing of fecal samples identified the distinct changes in the community composition of gut flora following BYHWD treatment, displayed as significantly increased Bacteroidetes and dramatically decreased Firmicutes at the phyla level, and the remarkable increase in the abundance of Lactobacillus and Blautia. Additionally, lipid metabolomics based on liquid chromatography-mass spectrometry revealed a significant shift of lipid metabolites in the liver after BYHWD treatment. Notably, these differential lipid metabolites were particularly involved in biological processes such as cholesterol metabolism, linoleic acid metabolism, glycerolipid metabolism, glycerophospholipid metabolism, insulin resistance, arachidonic acid metabolism, and alpha-linoleic acid metabolism. Importantly, Spearman correlation analyses suggested an association between disturbed gut microbiota and altered lipid metabolites. Moreover, they were also closely associated with the bioactivities of BYHWD to reduce the blood lipid and blood glucose levels. Collectively, these results suggest that BYHWD could meliorate gut microbiota dysbiosis and lipid metabolite alterations induced by the HFD in diabetic rats. These results not only provide a novel perspective on understanding the mechanisms underlying BYHWD bioactivity against T2DM but also suggest the use of advanced systems biology methods to reveal some unknown scientific laws in TCM theories.

[Mechanism of Huangjing Qianshi Decoction in treatment of prediabetes based on network pharmacology and molecular docking].

This study analyzed the molecular mechanism of Huangjing Qianshi Decoction(HQD) in the treatment of prediabetes based on network pharmacology and molecular docking. The active components of HQD were identified and screened based on Traditional Chinese Medicine Systems Pharmacology Database and Analysis Platform(TCMSP, http://Lsp.nwu.edu.cn/tcmsp.php) and then the targets of the components and the genes related to prediabetes were retrieved, followed by identifying the common targets of the decoction and the disease. The medicinal component-target network was constructed by Cytoscape to screen key components. The protein-protein interaction(PPI) network was established by STRING and hub genes were identified by Cytoscape-CytoNCA, followed by Gene Ontology(GO) term enrichment and Kyoto Encyclopedia of Genes and Genomes(KEGG) of the hub genes with R-clusterProfi-ler. Thereby, the possible signaling pathways were predicted and the molecular mechanism was deduced. A total of 79 active components of HQD and 785 diabetes-related targets of the components were screened out. The hub genes mainly involved the GO terms of tricarboxylic acid cycle, peptide binding, amide binding, hydrolase activity, and kinase activity regulation, and the KEGG pathways of AGE-RAGE signaling pathway, TNF signaling pathway, AMPK signaling pathway, IL-17 signaling pathway, and insulin signaling pathway. Western blot result showed that HQD-containing serum significantly reduced the expression of AKT1, AGE, and RAGE proteins in insulin resistance model cells. HQD's treatment of prediabetes is characterized by multiple pathways, multiple targets, and multiple levels. The main mechanism is that the components zhonghualiaoine, baicalein, kaempferol, and luteolin act on AKT1 and inhibit the AGE-RAGE axis.

2,3,5,4'-Tetrahydroxystilbene-2-O-ß-D-glucoside, a major bioactive component from Polygoni multiflori Radix (Heshouwu) suppresses DSS induced acute colitis in BALb/c mice by modulating gut microbiota.

BACKGROUND: Inflammatory bowel disease (IBD) includes ulcerative colitis (UC) and Crohn's disease (CD), which is a common idiopathic digestive disease without a specific cure or treatment for improvement. Because Polygoni multiflori Radix has a traditional medicinal use to treat intestinal diseases, and the water extract of this herbal medicine had a positive influence on dextran sulfate sodium (DSS) induced UC model in our study. Meanwhile 2,3,5,4'-tetrahydroxystilbene-2-O-ß-D-glucoside (TSG) as the major component of the water extract of Polygoni multiflori Radix with yield of more than 10% exhibited the remarkable anti-inflammatory activity in vivo and in vitro, we predicted that TSG may contribute to benefit intestinal tract presented by the water extract of Polygoni multiflori Radix. Therefore, the present study aims to explore the pharmacological effect of this compound on UC model and its possible mechanism to regulate intestinal function through gut microbiota. METHODS: Ulcerative colitis model was established in BALb/c mice by continuously administrating 3% (w/v) DSS aqueous solution for one week. The disease activity index (DAI), colon length, histopathological examination by H&E and the levels of tight junction proteins (TJP) by immunofluorescence staining were performed in ulcerative colitis model following the protocol. Furthermore, the levels of main inflammatory factors like TNF-α, IL-ß, IL-6, and IL-10 were analyzed by the ELIZA kits for the further confirmation of anti-inflammatory activity of TSG on ulcerative colitis model. Finally, 16S rDNA sequencing technology was conducted to explore the composition and relative abundance of gut microbiota of different treatment groups. RESULTS: TSG treatments effectively increased body weight about 5% of those in DSS group (p < 0.001) as well remarkably reduced the DAI scores to the 50% of those in DSS group (p < 0.001) in the UC model. TSG treatments of either 25 mg/kg (TSG-25) or 100 mg/kg (TSG-100) dosage restored epithelial barrier structure and exhibited obviously intact colon histology with reduced signs of inflammatory cells infiltration, preserved epithelia barrier, restored crypt structure, and increased numbers of goblet cells. TSG treatments could markedly lessen the histopathologic score two or three times than those in DSS group (p < 0.001). Especially for TSG-100 treatment, the fluorescence intensity of ZO-1 and Occludin were nearly back to 80% of those in normal group, and were 1.5 times more than those in the DSS group (p < 0.001). Additionally, direct evidence pointed to TSG as a therapeutically active molecule in the prevention and treatment of UC by significantly reducing the production of these pro-inflammatory cytokines like TNF-α, IL-1ß, and IL-6 (p < 0.05-0.001) and increasing the levels of anti-inflammatory cytokine IL-10 (p < 0.05-0.001). Finally, it was found TSG treatments significantly raised the relative abundances of Firmicutes and Bacteroidetes with a dose-dependently and improved the homeostasis of the gut microbiota composition which disrupted by DSS through increasing genus level Lachnospiraceae_NK4A136 and decreasing genus level of Helicobacter, Bacteroides, Parabacteroides. CONCLUSION: The present results suggested that TSG treatments had a desirable pharmacological effect on acute colitis induced by DSS in the mice as well showed the possible mechanism relate to improve the intestinal function through balancing the gut microbiota of intestinal flora.

Quantitative analysis of multicomponents by single marker combined with HPLC fingerprint qualitative analyses for comprehensive evaluation of Aurantii Fructus.

The present study aimed to develop a strategy involving quantitative analysis of multicomponents by single marker in combination with high-performance liquid chromatography fingerprint qualitative analysis for performing the quality control of Aurantii Fructus. The content of 12 components (eriocitrin, neoeriocitrin, narirutin, naringin, hesperidin, neohesperidin, meranzin, poncirin, naringenin, nobiletin, tangeretin, and auraptene) in samples was determined using reliable relative correction factors that were obtained using naringin as an internal reference standard. The new method demonstrated good applicability, and no significant differences were observed between the external standard method and the new method as determined by calculating standard method difference. Qualitative evaluation of samples was conducted using similarity analysis, hierarchical cluster analysis, and quality fluctuation analysis. Chromatographic fingerprint data were divided into three groups by similarity and hierarchical cluster analyses, and seven components may have a more significant impact on the quality of Aurantii Fructus in quality fluctuation analysis. Overall, the study suggests that the qualitative and quantitative analyses of multicomponents using quantitative analysis of multicomponents by single marker combined with chromatographic fingerprinting can be considered good quality criteria for performing quality control and providing technical support for the further pharmacological and pharmaceutical research of Aurantii Fructus.

Quality Evaluation of Ilex asprella Based on Simultaneous Determination of Five Bioactive Components, Chlorogenic Acid, Luteoloside, Quercitrin, Quercetin, and Kaempferol, Using UPLC-Q-TOF MS Study.

Background: Ilex asprella (Hook. Et Arn.) Champ. Ex Benth. is one of the representative medicinal plants that naturally grows in South China. It serves as a major component of herbal tea as an aid for sore throat, toothache, and acne, and it is a folk medicine for treating upper respiratory tract inflammation resulting from fever, infectious hepatitis, and enteritis. Objective: To evaluate the quality of Ilex asprella, the bioactive components were identified comprehensively using quadruple time-of-flight (Q-TOF) MS, and the HPLC method for quality evaluation was established for the first time. Methods: Detection was conducted under the positive electrospray ionization mode with the 110 V fragment voltage and 4.0 kV capillary voltage for the ultra-performance LC-Q-TOF MS study. A Thermo Fisher C18 column (4.6 × 150 mm, 5 µm) associated with the 0.10% formic acid and acetonitrile as mobile phase and gradient elution was carried out for separation process, and the HPLC quality evaluation was detected at a wavelength of 340 nm. Results: The method was validated according to the International Conference on Harmonization regulation including LOQ, LOD, recovery, replication, precision, and linearity. The contents of five components were important for quality evaluation of Ilex asprella. Moreover, luteoloside and quercitrin had more significant impact than others. Conclusions: A specific accurate method has been proposed for the identification of the bioactive components and applied to simultaneous quantification analysis of five components in Ilex asprella. Highlights: The quality evaluation of Ilex asprella established based on its bioactive components can provide a solid promotion for applications of Ilex asprella in food and drug fields.

Development of a Method for Simultaneous Determination of Two Stilbenes and Four Anthraquinones from Polygonum Cuspidatum by RP-HPLC.

Background: Polygonum cuspidatum Sieb. et Zucc. (named Huzhang in China) is a traditional and popular Chinese medicinal herb used in removing jaundice, clearing heat-toxin, improving blood circulation, expelling stasis, dispelling wind and dampness, repelling phlegm, and suppressing cough. It is widely used in drug and functional food fields and distributed throughout the world, including in China, Japan, and North America. Objective: To control the quality of Polygonum cuspidatum, an effective, reliable, and simple method for simultaneous determination of two stilbenes (polydatin, resveratrol) and four anthraquinones (emodin, physcion, rhein, and anthraglycoside B) was developed and validated for the first time in this study by reversed-phase HPLC (RP-HPLC). Methods: Separation was carried out on Agilent C18 column (250 × 4.6 mm I.D., 5 µm) with acetonitrile and 0.10% aqueous phosphoric acid as mobile phase and gradient elution at a flow rate of 0.8 mL/min. Detection was conducted with mobile wavelength at 30°C. Results: Good validation of the method including linearity, precision, repeatability, and recovery was performed. The contents of the studied analytes are significantly different, and resveratrol and rhein in particular existed in greater fluctuation among the samples. Conclusion: A simple, reliable, and sensitive method has been successfully established and applied to the analysis for simultaneous determination of the target compounds in 11 batches of samples. Highlights: Separation and quantitative analysis of two stilbenes and four anthraquinones from P. cuspidatum were developed by RP-HPLC. This method is convenient, sensitive, and accurate and can provide a reliable basis for further applications of P. cuspidatum in drug or food fields.

Discovery of potent and selective acetylcholinesterase (AChE) inhibitors: acacetin 7-O-methyl ether Mannich base derivatives synthesised from easy access natural product naringin.

Naringin, as a component universal existing in the peel of some fruits or medicinal plants, was usually selected as the material to synthesise bioactive derivates since it was easy to gain with low cost. In present investigation, eight new acacetin-7-O-methyl ether Mannich base derivatives (1-8) were synthesised from naringin. The bioactivity evaluation revealed that most of them exhibited moderate or potent acetylcholinesterase (AChE) inhibitory activity. Among them, compound 7 (IC50 for AChE = 0.82 ± 0.08 µmol•L-1, IC50 for BuChE = 46.30 ± 3.26 µmol•L-1) showed a potent activity and high selectivity compared with the positive control Rivastigmine (IC50 for AChE = 10.54 ± 0.86 µmol•L-1, IC50 for BuChE = 0.26 ± 0.08 µmol•L-1). The kinetic study suggested that compound 7 bind to AChE with mix-type inhibitory profile. Molecular docking study revealed that compound 7 could combine both catalytic active site (CAS) and peripheral active site (PAS) of AChE with four points (Trp84, Trp279, Tyr70 and Phe330), while it could bind with BuChE via only His 20.

The assessment of the chronic hepatotoxicity induced by Polygoni Multiflori Radix in rats: A pilot study by using untargeted metabolomics method.

Polygoni Multiflori Radix is the dried root of Polygonum multiflorum Thunb officially recorded in the Chinese Pharmacopoeia as HeShouWu (HSW) in Chinese pinyin. The processed HSW are commonly used in TCM to treat liver disease and Chinese Pharmacopoeia has described the actions of it to tonify liver-kidney, replenish essence and blood, blacken beard and hair, strengthen sinew and bone, and resolve turbidity and lower lipid hence making it use not only as a herbal medicine in TCM but also as supplementary food in health care. AIM OF THE STUDY: Concerns about the hepatotoxicity in association with Polygoni Multiflori Radix and its processed products have been reported in some countries. In the present study, we aim to investigate the potential hepatotoxicity of HSW in rats with oral administration of 95% ethanol-extracts of Polygoni Multiflori Radix by using metabolomics method. MATERIALS AND METHODS: Here, male rats with 150-180g body weight were received vehicle control or Polygoni Multiflori Radix extracts (HSW-Ex) orally at 19.2 (low dose), 192 (medium dose), or 1920mg/kg/day (high dose), respectively, for 28 consecutive days. Signs of HSW-induced toxicity were monitored by traditional toxicity assessments (e.g., clinical pathology and histopathology). Metabolomics investigation of serum was performed to identify potential endogenous metabolites which may be relevant to liver injury. RESULTS: Rats received High and Medium dose of HSW-Ex showed greater sign of liver injury with increased levels of ASP, ALT, and AST, as well as reduced SOD activity when compared to vehicle control. In contrast, there are no significant changes relevant to liver injury observed in rats by receiving the low dose of HSW-Ex. Metabolomics analyses have identified ten potential endogenous metabolites varied significantly among the treatment groups with varying doses of HSW-Ex, of which might be related to liver injury. CONCLUSION: Our data has further suggested that liver damage resulting from HSW-Ex consumption is dosage dependent in rats. It is possible that disruption in amino acid and energy metabolism might lead to subsequent oxidative damage in the liver of rats. Because the clinic practice often use low dose in a short time, therefore HSW usage in TCM still keep safe currently, but we present a warning to the clinical doctors and make them has some concern about high dose of HSW usage in a long term that has potential danger to damage liver.

[Tissue distribution of galactosyl daphnoretin liposomes in rats].

To study the tissue distribution of galactosyl daphnoretin liposomes in rats. At the dose of 10 mg•kg⁻¹, daphnoretin solution, daphnoretin liposomes, and galactosyl daphnoretin liposomes were administered to healthy SD rats via tail vein injection. The blood and tissue of heart, liver, spleen, lung, kidney, stomach, small intestine, brain and thymus were collected at 5, 15, 30, 45, 60, 120, 240, 360 min after administration. The concentrations of daphnoretin in plasma and tissue samples were determined by HPLC. The results showed that galactosyl daphnoretin liposomes group had the highest concentration of daphnoretin in liver of unit weight at different time points; and at all of the time points, the target index DTI values of galactosyl daphnoretin liposomes to liver were greater than that of daphnoretin liposomes. Compared with daphnoretin solution, the AUC0-6 and Cmax of galactosyl daphnoretin liposomes in liver were 2.23, 5.22 times, respectively. This indicated that galactosyl daphnoretin liposomes can be concentrated at liver, with a significant liver targeting effect.

Neuroprotective effect of a formula, moschus combined with borneolum synthcticum, from traditional chinese medicine on ischemia stroke in rats.

Moschus compatible with borneolum synthcticum is a well-known herb pair in Traditional Chinese Medicine and the present study aims to assess the neuroprotective effect of a formula composed of this herb pair on ischemia stroke in rats. The middle cerebral artery occlusion model of focal cerebral ischemia in rat was performed by using intraluminal suture method. The behavioral scores, infarct volume, and neuron ultrastructure of model and formula-treated rats were investigated after the 2 h of ischemia and 24 h of reperfusion. Meanwhile the expression levels of caspase-3, caspase-9, Bcl-2, and Bax were measured by western blot analysis. The formula treatment showed obvious neuroprotective effect according to significant decrease of the neurological scores (P < 0.01) and the infarct volumes (P < 0.05) when compared to the MCAO group. We also observed that this formula had antiapoptosis activity on neuron cell under electron microscope. Furthermore, our result supported the idea that pro- and postadministration of this formula had an antiapoptosis effect by decreasing remarkably the expression of caspase-3 and caspase-9 (P < 0.05) as well as increasing significantly the ratio of Bcl-2 to Bax (P < 0.01). All evidences demonstrated the neuroprotective effect of this formula on ischemia stroke due to decrease of brain infract volume and modulation of the expression of apoptosis-related proteins.

Variations in the contents of gingerols and chromatographic fingerprints of ginger root extracts prepared by different preparation methods.

In the present study, an HPLC-DAD method was optimized for the quantitative determination of 6-gingerol, 6-shogaol, 8-gingerol, and 10-gingerol in ginger extracts. A chromatographic fingerprinting method was also established to differentiate and evaluate the ginger extracts for bioactivity. Twenty-one extracts were prepared by methods differing in ginger type (fresh versus dried), solvent, and extraction methods. The ANOVA analysis showed the methods' influence on the mean extraction yields of gingerols increased in the order of: high pressure-high temperature (HP)>blender (BD)>low pressure (LP). The optimal solvent to extract gingerols was found to be 95% ethanol. The type of ginger used had significant effects on the content of gingerols, but its overall influence depended on the solvent used. In order to maximize the extraction efficiency of gingerols, a combination of dry ginger, 95% ethanol, and the HP extraction method should be employed. The chromatographic fingerprints were obtained to differentiate the unknown components from all ginger extracts. The similarity of the chromatographic fingerprints was used to evaluate the differences among all extracts. It can be concluded that the chromatographic fingerprints are able to ensure the stability of each extract and have some correlation with the observed bioactivity.

[Study on the rule of influence of two purification methods on the chemical compositions in aqueous solution of paeoniae radix alba].

OBJECTIVE: To explore the rule of influence of chitosan flocculation clarification and alcohol precipitation on the chemical compositions in aqueous extract of Paeoniae Radix Alba. METHODS: The fingerprints of aqueous extracts of Radix Paeoniae Alba were established by HPLC method, and the influences of the two purification methods on the chemical compositions in aqueous extract of Paeoniae Radix Alba were compared with the apparent content and relative apparent content of the composition as evaluation indexes. RESULTS: The chitosan flocculation clarification was superior to alcohol precipitation for keeping the polar compositions in aqueous extract, close to alcohol precipitation for keeping the medium polar compositions, and inferior to alcohol precipitation for keeping the lower polar compositions. CONCLUSION: The experiment result provides evidence for reasonably selecting above two purification methods to purify aqueous extract of Chinese medicinal herbs.

Combining Oxymatrine or Matrine with Lamivudine Increased Its Antireplication Effect against the Hepatitis B Virus In Vitro.

Some recent clinical reports have shown that the combination of oxymatrine, a phyto-derived drug, with lamivudine (3TC) could improve its curative effect against hepatitis B virus (HBV) infection. However, the experimental data in support of this combination strategy are lacking. In this study, we investigated the anti-HBV activity of the combination of 3TC and either oxymatrine or matrine on HepG2 2.2.15 in vitro. The activities of the combination and the solo compound, each in different concentrations, were compared on the 3rd, 6th, and 9th experimental days. The cytotoxicity results showed that the nontoxic concentrations of both oxymatrine and matrine to HepG2 2.2.15 cells were 800 µg/mL. We found that the single use of oxymatrine below 100 µg/ml, matrine below 200 µg/ml, and 3TC below 30 µg/ml showed weak inhibitory effects on the secretion of hepatitis B surface antigen (HBsAg), hepatitis B e antigen (HBeAg), and HBV-DNA in culture media; the combination of 3TC (30 µg/ml) with oxymatrine (100 µg/ml) or matrine (100 µg/ml) showed significant inhibitory effects that were higher than or equivalent to the single use of 3TC at 100 µg/ml. The results provide a new impetus to develop novel, multicomponent anti-HBV drugs through the combination of natural products with nucleoside analogs to enhance their activity.

[Study on the extraction technology of its flavonoids parts from Tricyrtis maculata growing in Shaanxi Province].

OBJECTIVE: To optimize the extraction technology of total flavonoids from Tricyrtis maculata. METHODS: With UV spectrophotometry as detection method and the content of total flavonoids as index,using single factor experiment and L9 (3(4)) orthogonal test, the optimal condition was deterined. RESULTS: The best extraction technology was as follows:soaked the medicinal materials for 15 minutes, water-decoted for 3 times, the solid-water ratio was 1:45, 1:40, 1:40 and the decotion time was 1, 0.5, 0.5 h respectively. CONCLUSION: The optimal extraction technology is reasonable and provides a basis for its further study.

[Research on good usage practice for Chinese Materia Medica (I): chemical equivalence of different prepare procedures and optimal conditions for good clinical usage of rhubarb].

OBJECTIVE: To probe into the influences of different granule sizes and to prepare procedures on rational clinical usage of rhubarb based on chemical equivalence. METHOD: The effects of particle size, extract solvent, extract time and repeat times, and pre-extract or pro-extract of rhubarb on the extract amounts of the anthraquinones (AQs) were compared. RESULT: The different prepare procedures investigated in the paper revealed significant influence on the extract amounts of the AQs and those extracts were not chemical equivalent. Ethanol extracted more AQs than water did, when other conditions were same. When extracted with water, the rhubarb of piece size 0.8-1.2 cm could extract relatively high amount of AQs nearly equal to superfine grinded powders, and the former was cheap. The water extraction of AQs showed an increasing trend with the extraction time extended. And pro-extract manner with water could extract more AQs than pre-extract manner with a extraction time of 30, 60 min. The water extraction of AQs repeated two times exceeded half of the amount of totally six times. When extracted with ethanol, the rhubarb of fine powders could extract relatively high amount of AQs nearly equal to superfine grinded powders. And pre-extract manner with ethanol could extract more AQs than pro-extract manner. The ethanol extraction of AQs increased in 30 min and then increased slower. The ethanol extraction of AQs repeated two times exceeded 70% of the amount of totally six times. So, the optimal conditions for water extraction rhubarb were pro-extract, two times repeated and 30 min per time; and the optimal conditions for ethanol extract were pre-extract, two times repeated and 30 min per time. CONCLUSION: The different prepare procedures showed significant influence on the extraction of rhubarb AQs. There is great need to establish a good usage practice (GUP) for Chinese Materia Medica to maintain rational clinical usage.

Investigation of the differences between the "Cold" and "Hot" nature of Coptis chinensis Franch and its processed materials based on animal's temperature tropism.

The description and differentiation of the so-called "Cold" and "Hot" natures, the primary "Drug Naure" of Chinese medicine, is the focus of theoretical research. In this study, the divergency between the "Cold" and the "Hot" natures was investigated through examining the temperature tropism of mice affected by Coptis chinensis Franch and its processed materials by using a cold/hot plate differentiating technology. After exposure to C. chinensis Franch, the macroscopic behavioral index of the remaining rate (RR) on a warm pad (40 degrees C) significantly increased (P<0.05), suggesting the enhancement of Hot tropism. The internal indexes of adenosine triphosphatase (ATPase) activity and oxygen consuming volume decreased significantly (P<0.05), suggesting the decapability of energy metabolism. This external behavior of Hot tropism might reflect the internal Cold nature of C. chinensis Franch. However, the processed materials of C. chinensis Franch exhibited a different Cold nature in temperature tropism compared with crude C. chinensis Franch (CC): the Cold nature of bile-processed C. chinensis Franch (BC) enhanced while the ginger-processed C. chinensis Franch (GC) changed inversely. The changing sequence was consistent with the theoretical prognostication. It is indicated that the external Cold & Hot natures of Chinese medicine may possibly reflect in an ethological way for the changes of animal's temperature tropism which might be internally regulated by the body's energy metabolism.