Two new prenylated 2-arylbenzofurans from roots of Artocarpus heterophyllus and their anti-respiratory burst activities / 中国中药杂志

Two prenylated 2-arylbenzofurans were isolated from roots of Artocarpus heterophyllus, with a combination of various chromatographic approaches, including ODS, MCI, Sephadex LH-20, and semipreparative high performance liquid chromatography(HPLC). They were identified as 5-[6-hydroxy-4-methoxy-5,7-bis(3-methylbut-2-enyl)benzofuran-2-yl]-1,3-benzenediol(1) and 5-[2H,9H-2,2,9,9-tetramethyl-furo[2,3-f]pyrano[2,3-h][1]benzopyran-6-yl]-1,3-benzenediol(2) with spectroscopic methods, such as HR-ESI-MS, IR, 1D NMR, and 2D NMR, and named artoheterins B(1) and C(2), respectively. The anti-respiratory burst activities of the two compounds were evaluated with rat polymorphonuclear neutrophils(PMNs) stimulated by phorbol 12-myristate 13-acetate(PMA). The results showed that 1 and 2 exhibited significant inhibitory effect on respiratory burst of PMNs with IC_(50) values of 0.27 and 1.53 μmol·L~(-1), respectively.

Pueraria lobate advances in molecular pharmacognosy / 中国中药杂志

Molecular pharmacognosy is a science of classification and identification, cultivation and protection, and production of active ingredients of graduated drugs at the molecular level. The proposal of molecular pharmacognosy allows the research of crude drugs to advance from the microscopic level to the genetic level. Pueraria lobata root, as a medicinal and edible plant, has high application value and economic value. There are many varieties that are easy to cause confusion, and it is not easy to distinguish and identify according to traditional identification methods. Moreover, the research of P. lobate root at the genetic level is still relatively shallow. the study received extensive attention of scholars. This article reviews recent research on molecular identification of P. lobate, transcriptome sequencing, cloning and synthesis of functional genes of P. lobate root in recent years in order to provide references for further promoting the development and utilization of P. lobate root and its active ingredients.

Difference Analysis of Chemical Constituents in Different Varieties of Puerariae Flos by UPLC-Q-TOF-MS / 中国实验方剂学杂志

Objective:To compare the chemical constituents of Puerariae Flos from three different varieties of <italic>Pueraria montana</italic> var. <italic>lobata</italic>， <italic>P. montana</italic> var. <italic>thomsonii</italic> and <italic>P</italic>. <italic>montana</italic> var<italic>. montana</italic>. Method:Ultra-performance liquid chromatography-quadrupole-time-of-flight mass spectrometry （UPLC-Q-TOF-MS） was used with the mobile phase of 0.1% formic acid aqueous solution （A）-acetonitrile （B） for gradient elution （0-20 min， 10%-30%B； 20-30 min， 30%-55%B； 30-35 min， 55%-95%B； 35-37 min， 95%B； 37-40 min， 95%-10%B）， the flow rate was 0.25 mL·min^-1. Electrospray ionization （ESI） was used to scan and collect MS data in positive and negative ion modes with scanning range of <italic>m</italic>/<italic>z</italic> 50-1 500. The chemical components from different sources of Puerariae Flos were identified in combination with the chemical composition database and literature information. After the obtained data were normalized by MarkerView^TM 1.2.1， they were imported into SICMA-P 14.1 software for principal component analysis （PCA） and orthogonal partial least squares discriminant analysis （OPLS-DA） to select the main differentiated components among the three different varieties. Result:A total of 35 compounds were identified from three different varieties of Puerariae Flos， including 22 isoflavones， 6 flavonoids and 7 saponins. The flowers of <italic>P</italic>. <italic>lobata</italic>， <italic>P. montana</italic> var. <italic>thomsonii</italic> and <italic>P</italic>. <italic>montana</italic> var<italic>. montana</italic> contained 32， 35， 33 compounds， respectively. And 18 differential compounds were screened under the positive and negative ion modes， including kakkalide， tectoridin， 6″-<italic>O</italic>-xylosyl-tectoridin， 4'-methyltectorigenin-7-glucoside， glycitin， 6″-<italic>O</italic>-xylosyl-glycitin， irisolidone， kaikasaponin Ⅲ， 6″-<italic>O</italic>-malonylglycitin， kakkalidone， tectorigenin， rutin， soyasaponin BB， vitexin， biochanin A， genistin， kakkatin， azukisaponin Ⅱ. Conclusion:This research is the first to systematically study the chemical constituents of the flower of <italic>P</italic>. <italic>montana</italic> var<italic>. montana</italic>， although the flower of <italic>P</italic>. <italic>montana</italic> var<italic>. montana</italic> is used as adulterants， it has high contents of tectoridin and 6″-<italic>O</italic>-xylosyl-tectoridin， which has great potential for development. The efficacy components such as kakkalide and tectoridin in Puerariae Flos from the three sources of varieties are obviously different， and it is necessary to carefully consider the application of these three varieties as Puerariae Flos.

Screening of Components with Potential Regulation Effect in Lagotis brevituba Based on Target Cell and Molecular Docking / 中国实验方剂学杂志

Objective:To study the components with urate anion transporter 1（URAT1） regulation effect and their combination mechanisms of Lagotis brevituba by integrating techniques of HK-2 cell capture，UPLC-Q-TOF-MS and molecular docking，so as to provide material and theory bases for the development of new hypouricemic medicines based on L. brevituba. Method:The HK-2 cells were applied to capture the components of L. brevituba. UPLC-Q-TOF-MS was used to identify those components. The molecular docking technique was adopted to study the interaction mechanism between the compounds and URAT1. Result:Eight components were successfully screened and identified as hyperoside，plantamajoside，kaempferol-3-O-glucoside，lugrandoside，nepitrin，isolugrandoside，homoplantaginin，luteolin，respectively. Those components could combine with URAT1 mainly through hydrogen bond，van der Waals force and hydrophobic action，which were closely related to structure and compound types. Furthermore，the LibDock score of phenylethanoids was higher than that of flavonoids. Conclusion:The integration of target cell capture，UPLC-Q-TOF-MS and molecular docking techniques could be successfully used to identify captured compounds of L. brevituba with URAT1 regulation effects and illustrate their potential combination mechanisms as well as the structure-activity relationships. The findings may provide material and theory bases for the development of new hypouricemic medicines based on L. brevituba.

Methodology for Screening Effective Substances of Chinese Herbal Medicine for Reducing Serum Uric Acid Level / 中国实验方剂学杂志

Gout is caused by the nucleation and growth of monosodium rate crystals in tissues and around joints, which is followed by long-standing hyperuricemia and serum urate of above the saturation threshold. It could cause a series of complications, such as cardiovascular, hypertension, and renal complications. Over the past two decades, the incidences of hyperuricemia and gout have been increasing due to the continuous improvement of living standards and the changes in dietary structure. The prime and most important therapy for hyperuricemia and gout is to reduce serum uric acid levels, but the western medicine for reducing uric acid in clinical application has serious toxic and side effects. With the rapid development of modern science and technology, the application and development of different screening methods for effective ingredients with a low toxicity and side effects from Chinese herbal medicines for reducing serum uric acid levels has attracted much attention in the research and development of drugs for the prevention and treatment of hyperuricemia and gout. In this study, the screening methods for extracts, fractions, active monomer components and other effective substances were reviewed and analyzed. According to the findings, the screening methods had a considerable progress both in vivo and in vitro. The results showed that the in vivo methods were mainly applied for studying the urate lowing effect and mechanisms of herbal extracts, while the studies for xanthine oxidase(XOD) inhibitors mainly depended on the in vitro methods. Molecular docking homology modeling and liquid chromatography-mass spectrometry have become a new trend for screening effective substances with XOD inhibitory activities and uric acid excretion activities, while cell model will open up a new way for screening effective substances for uric acid excretion. The review provides certain reference for effective components screening of hyperuricemia and gout.

Comparison of chemical constituents in different parts of Gardenia jasminoides based on multiple wavelength HPLC-DAD / 中国中药杂志

Seven compounds(deacetylasperulasidic acid methyl ester, gardenoside, chlorogenic acid, geniposide, crocin-Ⅰ, crocin-Ⅱ, chikusetsu saponin Ⅳa)were determined simultaneously by multiple wavelength HPLC with diode array detector(DAD) in different parts of Gardenia jasminoides. The results showed that these components in different parts of G. jasminoides had a different distribution, and there was a large difference in content of each component. Geniposide was mainly distributed in fruits and leaves; chikusetsu saponin Ⅳa was mainly distributed in roots and stems; crocus glycosides existed mainly in fruits; chlorogenic acid had a higher distribution in leaves and stems; gardenoside had a higher distribution in leaves and roots, while ceacetylasperulasidic acid methyl ester had a higher distribution in roots and stems. Based on the analysis of the chemical composition and content difference in different parts of G. jasminoides, the basis for the comprehensive utilization and quality evaluation of resources of G. jasminoides was provided.

Dynamic analysis on endo phylohormone during bolting time of roots in Saponikovia cata / 中草药

Objective: Through determining the contents of growth hormone (IAA), gibberellic acid (GA), and abscisic acid (ABA) to make the content changes of IAA, GA, and ABA clear before and after bolting time in the roots of Saponikovia cata, so as to provide the theoretical basis for studying the early bolting mechanism in the roots of S. cata. Methods: The contents of IAA, GA, and ABA before and after the bolting time were determined by HPLC. The chromatographic conditions were as follows: C18 ODS RP column, temperature: 35°C, detection wavelength: 254 nm, volumn flow: 0.7 mL/min, mobile phase: methanol-acetonitrile -0.7% acetic acid (40:15:45). Results: The content variation trend of IAA and GA in the roots, stems, and leaves of S. cata was almost the same during the bolting time. The contents of IAA and GA in the roots of S. cata revealed the downgrade tendency sharply after bolting; The contents of IAA and GA in the roots of S. cata before bolting were obviously higher than those after bolting. The content variation trends of ABA in the roots, stems, and leaves of S. cata were the same during the bolting time, but far more different from IAA and GA. Although there was the little fluctuation of ABA before bolting, the contents of ABA after bolting were sharply upgraded and were obviously higher than those before bolting. Conclusion: The phenomenon of early bolting in the roots of S. cata directly relates to the endo phylohormone level, so we may extrapolate that the levels of endo phylohormone could straightly cause the bolting in the roots of S. cata or not.