Research Progress on G2/M Arrest in Breast Cancer Cells by Active Compounds of Traditional Chinese Medicine / 中国实验方剂学杂志

The global incidence of breast cancer has increased year by year. Breast cancer has the highest mortality rate in female patients with malignant tumors. Traditional Chinese medicine（TCM） has made great contribution to health of human being， improving the overall curative effect， reducing the patients' pain， improving the quality of life and alleviating adverse reactions in patients. TCM and its active compounds can inhibit the proliferation of breast cancer cells by inducing cell cycle arrest， invasion， metastasis and reversing multidrug resistance. The effect of the compounds in TCM is obvious on inducing the arrest of the breast cancer cells cycle. It′s a novel method to fight against breast cancer by influencing the progress of the breast cancer cell cycle and inducing the cell cycle arrest in breast cancer cells. Lots of studies have shown that the G2/M phase checkpoint which transition from gap-phase （G2 phase） to mitotic phase （M phase） in the cell cycle is the key point for cell survival or death. Many antitumor drugs can inhibit the proliferation of tumor cells through the cell cycle arrest. We summarized the domestic and foreign literatures in recent years， and comprehensively explained the research progress on the related regulatory molecules in G2/M arrest. In addition， we summarized and sorted out the researches on the methods and ways of alkaloids， polysaccharides， terpenes， flavonoids， saponins and other active compounds of TCM in inducing the G2/M arrest of human breast cancer cells. By summarizing the active compounds of various Chinese medicines in inducing G2/M arrest of breast cancer cells， and reviewing the research progress on mechanism of active TCM compounds for inhibiting the proliferation of breast cancer cells， we will， in this paper， investigate the mechanism of active TCM compounds for inhibiting the proliferation of breast cancer cells through inducing G2/M arrest of human breast cancer cells， so as to provide a scientific basis for in-depth research on the anti-breast cancer mechanism of the active compounds in TCM.

Distribución bioclimática de plantas medicinales y sus principios activos en el Departamento de Cajamarca (Perú) / Bioclimatic distribution of medicinal plants and its active substances in the Department of Cajamarca (Peru)

This work presents a distribution of medicinal plants and active substances from Cajamarca Department (Peru) under a bioclimatic criterion. The results show that 108 medicinal plants are spread among five bioclimatic belts: infratropical, thermotropical, mesotropical, supratropical and orotropical. As a statistical analysis shows (non-metric multidimensional scaling, MDS), most of them are concentrated in the mesotropical belt and a subhumid precipitation range. In addition a canonical correspondence analysis (CCA), using the altitude (m), the thermicity index (It) and annual precipitation (P) as environmental variables, indicates how active substances are also distributed with tendencies of them, showing phenolic substances and essential oils as mesotropical products, and complex alkaloids to the highest It values, while simple alkaloids to the lowest It values. Most of these molecular compounds are generated under the highest values of the subhumid and humid precipitation intervals. This bioclimatic method can led us to find new medicinal plants and active molecules.

Este trabajo presenta una distribución de plantas medicinales y principios activos en el departamento de Cajamarca (Perú) bajo un criterio bioclimático. Los resultados muestran que 108 plantas medicinales están repartidas entre cinco pisos bioclimáticos: infratropical, termotropical, mesotropical, supratropical y orotropical. Como muestra el análisis estadístico realizado MDS (non-metric multidimensional scaling), la mayoría de plantas se concentra en el piso mesotropical y en el intervalo subhúmedo de precipitaciones. Además, un análisis canónico de correspondencias (CCA), donde intervienen la altitud (h), el índice de termicidad (It) y las precipitaciones anuales (P) como variables ambientales, indica cómo los principios activos también se distribuyen según tendencias de estas, mostrando a los compuestos fenólicos y aceites esenciales como productos mesotropicales, los alcaloides complejos hacia los valores más elevados de It, mientras que los alcaloides simples hacia los más bajos. Asimismo, la mayoría de estos compuestos tienen su óptimo en los valores más elevados del intervalo subhúmedo y el intervalo húmedo de precipitaciones. Este método bioclimático nos puede llevar a encontrar nuevas plantas medicinales y principios activos.

The action and mechanism of ethanol extract of Cichorium glandulosum on type 2 diabetes mellitus accompanied with nonalcoholic fatty liver disease based on systems pharmacology / 药学学报

italic>Cichorium glandulosum has been used to treat non-alcoholic fatty liver disease (NAFLD) and type 2 diabetes mellitus (T2DM) in Uyghur folk medicine. The mechanism of Cichorium glandulosum (CG)on type 2 diabetes mellitus accompanied with non-alcoholic fatty liver disease (T2DM-NAFLD) remains unclear. The effect of CGextraction on T2DM-NAFLD was determined in animal experiments here (all the experiments here were approved by the Animal Care Committee of the First Affiliated Hospital of the Medical College, Shihezi University). The mechanism of CG for treatment of T2DM-NAFLD was predicted and verified based on systems pharmacology. Based on the active compounds of CGon T2DM-NAFLD, T2DM and NAFLD-related targets, pathways and diseases were screened and predicted. Active compounds-targets, compounds-targets-pathways and compounds-targets-diseases were constructed and analyzed. The results of animal experiments showed that CGextractioncan reduce the levels of blood glucose and blood lipid in T2DM-NAFLD rats. In addition, it can improve the glucose tolerance and relieve liver injury. Total 29 active compounds and 198 targets were screened by systems pharmacology, of which 106 targets were involved in T2DM, 88 were involved in NAFLD, and 56 targets were common between T2DM and NAFLD, mainly related to insulin resistance and inflammation. These 198 targets include those in metabolic pathways, calcium pathway, PI3K/Akt pathway, cAMP pathway, and MAPK pathway. Our study confirmed that CG can be potential phytomedicine for treatment of T2DM-NAFLD. This work provides a reference for studying the treatment of multiple diseases using multiple-targets phytomedicine in systems pharmacology.

Study on Intestinal Absorption Characteristics of 5 Active Components in Ethanol Extract from Bletilla striata / 中国药房

OBJECTIVE： To investigate absorption kinetic characteristics of main active components as 4-（glucoseoxy）- glucoseoxybenzyl cinnamate （A1）， 2-isobutyl malic acid （A2）， 1，4-bis [4-（glucoxy） benzyl]-2-isobutyl malic acid ester （A3）， dihydrophenanthrenes 1 （A4） and 1，4-bis [4-（glucosoxy） benzyl]-2-isobutyl malic acid ester-2-（4-O-cinnamoyl-6-O-acetyl） glucoside （A5） from ethanol extract of Bletilla striata in the intestines of rats. METHODS： Using puerarin as internal standard， UPLC-MS/MS was used to determined the concentration of A1-A5 in intestinal circulation fluid. The determination was performed on Acquity UPLC BEH C18 column with mobile phase consisted of acetonitrile （containing 0.1％ formic acid）-water （containing 0.1％ formic acid） （gradient elution） at the flow rate of 0.35 mL/min. The column temperature was 45 ℃， and sample size was 3 μL. The positive ion and negative ion scanning were carried out in the multiple reaction monitoring mode by electrospray ion source. The ion pairs for quantitative analysis were m/z 593.2→431.1 （A1）， m/z 189.0→129.0 （A2）， m/z 725.3→457.2 （A3）， m/z 347.1→332.1 （A4）， m/z 1 059.3→793.1 （A5）， m/z 417.0→267.0 （internal standard）. In the in vivo intestinal circulation perfusion model， using accumulative absorption transfer rate （A） and absorption and transformation rate constant （Ka） as indexes， the effects of different doses of ethanol extract from B. striata （low-， medium-， high-dose were 166， 333，667 μg/mL，respectively）， bile， P-glycoprotein （P-gp） inhibitors （verapamil） and different intestinal segments on the absorption of above 5 components were investigated. RESULTS： The linear range of A1， A2， A3， A4 and A5 were 0.22-14.00， 0.34-21.75， 1.99-127.16， 0.15-9.75， 0.16-10.00 μg/mL（r＞0.99）. The limits of quantitation were 0.22， 0.34， 1.99， 0.15， 0.16 μg/mL， respectively. The lowest detection limits were 0.028， 0.085， 0.251， 0.035 and 0.010 μg/mL. RSDs of inter-day and intra-day were all lower than 10％. The recoveries ranged 83.60％-106.91％. Matrix effect did not affect the determination of the substance to be measured. A and Ka values of A1 in B. striata ethanol extract low-dose and medium-dose groups were significantly higher than high-dose group； A value of A3 in low-dose group was significantly higher than medium-dose and high-dose groups （P＜0.05 or P＜0.01）. A and Ka values of A1 and A3 in non-ligation group were significantly lower than control group， while A and Ka values of A4 were significantly higher than control group （P＜0.05 or P＜0.01）. A and Ka values of A1 and A3 in P-gp inhibitor group were significantly lower than control group （P＜0.05 or P＜0.01）. A values of A1 in jejunum group， ileum group and colon group， Ka value of A1 in colon group， A and Ka values of A2 in colon group， A value of A3 in ileum group， A and Ka values of A4 in ileum group and colon group， A values of A5 in jejunum group and ileum group as well as Ka value of A5 in jejunum group were all significantly lower than duodenum group. Ka values of A3 in jejunum group， ileum group and colon group were significantly higher than duodenum group （P＜0.05 or P＜0.01）. CONCLUSIONS： Established UPLC-MS/MS method is specific， sensitive and simple， and it can be used for quantitative analysis and pharmacokinetic study of A1-A5. The 5 active components in B. striata ethanol extract are absorbed by the whole intestine， and the intestinal segments are different. A1 and A3 are absorbed more in intestinal tract and may be saturated. Bile can inhibit intestinal absorption of A1 and A2， but promoted intestinal absorption of A4. A1-A5 may not be the substrate of P-gp.

Java Ginger Bangle / 日本補完代替医療学会誌

The review reveals latest studies of Bangle that has unique ingredients, safety, healthy effect and especially neurotrophin activity. Banglenes have some neurotrophin activity such as neuritogenesis without NGF in vitro, property that enhances hippocampal neurogenesis and crosses the blood-brain barrier (BBB) in vivo. On the other hand, Java ginger bangle (Extract) improves spatial learning in Senescence-Accelerated Mouse. Moreover the human clinical trial for MCI (Mild Cognitive Impairment) have been just started.

Pharmacognostic and HPTLC Fingerprint Profile of the Root of Aristolochia indica Linn. and Quantification of the Marker Compound.

Introduction: Root of Aristolochia indica Linn. has long been used as an oxytoxic agent to aid women in child birth and as abortifacient in Indian folk medicine. It is also one of the ingredients in some traditional Ayurveda medicinal preparations. Aims: The present work has been designed to delineate the pharmacognostic profile of the root of Aristolochia indica Linn and the High-performance thin-layer chromatographic (HPTLC) identification of the active compound and its quantitative estimation in the herbal sample. Materials and Methods: Macroscopic, microscopic evaluation, powder analysis, fluorescence standards of the root of Aristolochia indica Linn and its HPTLC fingerprint profile. Results: Pharmacognostic profile of the root investigated revealed the transverse section possessing somewhat circular outline with tissue organization as outer thin walled cork layers, narrow cortex, and inner cortical cells with groups of stone cells. Secondary xylem tissues were fissured to form narrow strips, wide medullary rays with greater quantities of parenchyma, ray cells with rich deposition of starch. Vessels were solitary and occluded with tyloses and starch grains with 'Maltese cross' were the characteristic features of the taxon. HPTLC method was developed for the estimation of the marker constituent, Aristolochic Acid I (AAI) in dried root sample. Chloroform: Methanol (6:2v/v), was used as mobile phase to separate the analyte. The Rf value for Aristolochic Acid I (C17H11NO7) was found to be 0.53. Calibration plot was established showing the dependence of response on the amount chromatographed. Linearity was found to be in the concentration range of 100 to 500ng/spot for AAI with the correlation coefficient value r=0.998. The result showed that the content of marker compound (AAI) in dried root of Aristochia india Linn was 0.082%. Conclusions: The results of the present study suggest that, the documented morphological descriptors, delineated anatomical markers and developed HPTLC methods are complementary characteristics, which could be effectively used for the identification and authentication of the root of Aristolochia indica Linn.

Diversity, Utility, Analytical Methods and Use Implications of Aroma-active Compounds from Select Angiosperm Familie.

Introduction: An “aroma-active compound” (AAC) has a “flavor”- ie: a “distinct taste and odor”. An example is menthol. All aromatic plants (APs), including some medicinal plants, such as Mentha×piperita (Family Lamiaceae), produce a group of fat-soluble secondary metabolites called “essential oils” (EOs) for various ecophysiological reasons. An EO has a “flavor” because it contains one or more AACs. A typical EO is a complex mixture of several AACs, with wide ranging, dose-dependent pharmacological/ toxic effects. Owing to their complexity and variability, many EOs need to be standardized to ISO’s criteria. Professional use of EOs/ AAPs in food and drugs is controlled by good manufacturing practice (GMP). Aim: Given the immense diversities in sources, chemical structures, and bioactivities of EOs/ AACs, which are greatly patronized in foods and drugs, this review focused on their: i) sources in plants, beneficial attributes and liabilities; and ii) chemistry and analytical methods, in order to gain a better insight into their regulation in foods and drugs. Methodology: Using the 2009 Angiosperm Phylogenic Grouping (APG) of plants as a guide, pertinent literature was perused to ascertain: i) the taxa of APs; ii) their EOs/ AAPs; and iii) the methods for analyzing EOs/ AACs in raw materials (RMs) and finished products (FPs). Results: The literature revealed scores of AACs with varying health implications. But their levels in samples are usually unknown, or extremely hard to ascertain, owing to costs and complexities of the methods used. Conclusions: Given the wide ranging effects of EOs/ AAPs vis-à-vis the dearth of data on their levels in samples, it is recommended that their regulation in FPs should focus on: i) controlling the wholesomeness of RMs; and ii) on enforcing strict GMP in using such RMs. Meanwhile relevant agencies should sponsor research into more cost-effective methods.

Effect of active compound components of SQ on MMP-1,TIMP-1,VEGF,t-PA and PAI-1 of in? ammatory endometrial cell / 中华中医药杂志

Objective :To study the effect of MMP-1,TIMP-1,VEGF and t-PA,PAI-1 in the inflammatory process of endometrium cell and the active components of SQ.Methods: ICC,ISH and WB was used to test the level of protein of MMP-1,TIMP-1,VEGF and t-PA,PAI-1 and mRNA of MMP-1,TIMP-1 and VEGF of endometrium cell in regular group,pattern group,GongXueNing group and SQ group.Result: In contrast with model group,the level of MMP-1protein and mRNA expression obviously decreased,but the level of TIMP-1 and VEGF increased in SQ group,there were signifi cant differences(P

Screening and isolation of fibrinolytic active compound from marine microorganism / 中国海洋药物

Objective To isolate bioactive compound of enhancing fibrinolysis from secondary metabolites of marine microorganism.Methods The separation of microorganism from seawater samples,screening of producing fibrinolytic compound's strain,selection of the active strain's optimum fermentation medium and refining of active compound were done by the method of selective cultivation,measuring of compound's fibrinolytic activity and semipreparative HPLC,respectively.Results Nine hundred and thirty-six single strains from 31 samples were collected 100 meters off the coast,and cultures of the fungus(FG216) contained enhancing fibrinolytic compound.Compounds from modified Czapek medium as the fermentation medium of FG216 showed significant fibrinolytic effect.Finally,active fraction were isolated and refined from cultures of FG216.Conclusion In this paper,active compound of enhancing fibrinolysis were gained from secondary metabolites of isolated single microorganism from seawater.

SFE-CO_2 constituents of simplified formula of Danggui Shaoyao Powder in the prevention and treatment of vascular dementia / 中成药

AIM: To isolate,identify and screen active compounds of simplitied formula of Danggui Shaoyao Power(poria,Rhizoma Atracty-lodis Macrocephalae,and Radix Angeliae Sinensis). METHODS: Compounds in the fraction of CO_2 supercritical fluid extraction(SFE-CO_2) were isolated by silica gel chromatography and detected the protective effect on KCl-induced PC12 cell damage. RESULTS: Twelve compounds were obtained,and nine of them were identified as atractylenolide Ⅰ,Ⅱ,Ⅲ,biatractylenolide,levistolid A,pachymic acid,ferulic acid,?-sitosterol and ?-daucosterol,of which only atractylenolide Ⅲ can improve the cell viability significantly. CONCLUSION: Atractylenolide Ⅲ may be one of the active compounds of FBD in curing vascular dementia.