Dammarane-type triterpene oligoglycosides from the leaves and stems of Panax notoginseng and their antiinflammatory activities

Li, Juan,Wang, Ru-Feng,Zhou, Yue,Hu, Hai-Jun,Yang, Ying-Bo,Yang, Li,Wang, Zheng-Tao The Korean Society of Ginseng 2019 Journal of Ginseng Research Vol.43 No.3

Background: Inflammation is widespread in the clinical pathology and closely associated to the progress of many diseases. Triterpenoid saponins as a key group of active ingredients in Panax notoginseng (Burk.) F.H. Chen were demonstrated to show antiinflammatory effects. However, the chemical structures of saponins in the leaves and stems of Panax notoginseng (PNLS) are still not fully clear. Herein, the isolation, purification and further evaluation of the antiinflammatory activity of dammarane-type triterpenoid saponins from PNLS were conducted. Methods: Silica gel and reversed-phase C8 column chromatography were used. Furthermore, preparative HPLC was used as a final purification technique to obtain minor saponins with high purities. MS, NMR experiments, and chemical methods were used in the structural identifications. The antiinflammatory activities of the isolated saponins were assessed by measuring the nitric oxide production in RAW 264.7 cells stimulated by lipopolysaccharides. Real-time reverse transcription polymerase chain reaction was used to measure the gene expressions of inflammation-related gene. Results: Eight new minor dammarane-type triterpene oligoglycosides, namely notoginsenosides LK1-LK8 (1-8) were obtained from PNLS, along with seven known ones. Among the isolated saponins, gypenoside IX significantly suppressed the nitric oxide production and inflammatory cytokines including tumor necrosis $factor-{\alpha}$, interleukin 10, interferon-inducible protein 10 and $interleukin-1{\beta}$. Conclusion: The eight saponins may enrich and expand the chemical library of saponins in Panax genus. Moreover, it is reported for the first time that gypenoside IX showed moderate antiinflammatory activity.

Preparation and In Vitro Release of Ramose Chitosan-Based-5-Fluorouracil Microspheres

Li, He-Ping,Li, Hui,Wang, Zhou-Dong,Zhang, Juan-Juan,Deng, Man-Feng,Chen, San-Long Korean Chemical Society 2013 대한화학회지 Vol.57 No.1

In order to construct a controlled release system of drugs and to reduce toxic side effects of 5-fluorouracil, the novel ramose chitosan-based-5-fluorouracil microspheres (CS-FU-MS) were prepared. Firstly, using chitosan (CS) as carriers and 5-fluorouracil (5-FU) as a model drug, ramose chitosan-based-5-fluorouracil (CS-FU) was efciently synthesized by chemical crosslinking method through microwave irradiation, drug loading was 10.6%; Secondly, CS-FU-MS were prepared by CS-FU self-assembled under the dialysis conditions and the free 5-FU was encapsulated further at the same time. The size dispersivity of particles is uniform, and the average diameter of the CS-FU-MS was $4{\mu}m$. The drug encapsulation efficiency was 76.1%, and the drug loading was increased to 26.22%. CS-FU-MS maintain the zero-order release time in PBS (pH = 7.4) and HCl/KCl (pH = 1.2) dialysis medium was 40h and 34h respectively, and the cumulative release were 58.89% and 79.33% in 182 h. The results showed that CS-FU-MS have excellent sustained release properties.

Dammarane-type triterpene oligoglycosides from the leaves and stems of Panax notoginseng and their antiinflammatory activities

Juan Li,Ru-Feng Wang,Yue Zhou,Hai-Jun Hu,Ying-Bo Yang,Li Yang,Zheng-Tao Wang 고려인삼학회 2019 Journal of Ginseng Research Vol.43 No.3

Background: Inflammation is widespread in the clinical pathology and closely associated to the progressof many diseases. Triterpenoid saponins as a key group of active ingredients in Panax notoginseng (Burk.)F.H. Chen were demonstrated to show antiinflammatory effects. However, the chemical structures ofsaponins in the leaves and stems of Panax notoginseng (PNLS) are still not fully clear. Herein, the isolation,purification and further evaluation of the antiinflammatory activity of dammarane-type triterpenoidsaponins from PNLS were conducted. Methods: Silica gel and reversed-phase C8 column chromatography were used. Furthermore, preparativeHPLC was used as a final purification technique to obtain minor saponins with high purities. MS, NMRexperiments, and chemical methods were used in the structural identifications. The antiinflammatoryactivities of the isolated saponins were assessed by measuring the nitric oxide production in RAW 264.7cells stimulated by lipopolysaccharides. Real-time reverse transcription polymerase chain reaction wasused to measure the gene expressions of inflammation-related gene. Results: Eight new minor dammarane-type triterpene oligoglycosides, namely notoginsenosides LK1-LK8 (1e8) were obtained from PNLS, along with seven known ones. Among the isolated saponins,gypenoside IX significantly suppressed the nitric oxide production and inflammatory cytokines includingtumor necrosis factor-a, interleukin 10, interferon-inducible protein 10 and interleukin-1b. Conclusion: The eight saponins may enrich and expand the chemical library of saponins in Panax genus. Moreover, it is reported for the first time that gypenoside IX showed moderate antiinflammatory activity.

Chemical transformation and target preparation of saponins in stems and leaves of Panax notoginseng

Wang, Ru-Feng,Li, Juan,Hu, Hai-Jun,Li, Jia,Yang, Ying-Bo,Yang, Li,Wang, Zheng-Tao The Korean Society of Ginseng 2018 Journal of Ginseng Research Vol.42 No.3

Background: Notoginsenoside Ft1 is a promising potential candidate for cardiovascular and cancer disease therapy owing to its positive pharmacological activities. However, the yield of Ft1 is ultralow utilizing reported methods. Herein, an acid hydrolyzing strategy was implemented in the acquirement of rare notoginsenoside Ft1. Methods: Chemical profiles were identified by ultraperformance liquid chromatography coupled with quadruple-time-of-flight and electrospray ionization mass spectrometry (UPLC-Q/TOF-ESI-MS). The acid hydrolyzing dynamic changes of chemical compositions and the possible transformation pathways of saponins were monitored by ultrahigh-performance LC coupled with tandem MS (UHPLC-MS/ MS). Results and conclusion: Notoginsenoside Ft1 was epimerized from notoginsenoside ST4, which was generated through cleaving the carbohydrate side chains at C-20 of notoginsenosides Fa and Fc, and vinaginsenoside R7, and further converted to other compounds via hydroxylation at C-25 or hydrolysis of the carbohydrate side chains at C-3 under the acid conditions. High temperature contributed to the hydroxylation reaction at C-25 and 25% acetic acid concentration was conducive to the preparation of notoginsenoside Ft1. C-20 epimers of notoginsenoside Ft1 and ST4 were successfully separated utilizing solvent method of acetic acid solution. The theoretical preparation yield rate of notoginsenoside Ft1 was about 1.8%, which would be beneficial to further study on its bioactivities and clinical application.

SSR and SCAR mapping of a multiple-allele male-sterile gene in Chinese cabbage (Brassica rapa L.)

Feng, Hui,Wei, Peng,Piao, Zhong-Yun,Liu, Zhi-Yong,Li, Cheng-Yu,Wang, Yu-Gang,Ji, Rui-Qin,Ji, Shu-Juan,Zou, Ting,Choi, Su-Ryun,Lim, Yong-Pyo Springer-Verlag 2009 TAG. Theoretical and applied genetics. Theoretisch Vol.119 No.2

Apoptosis induction by alantolactone in breast cancer MDA-MB- 231 cells through reactive oxygen species-mediated mitochondrion-dependent pathway

Li Cui,Weiquan Bu,Jie Song,Liang Feng,Tingting Xu,Dan Liu,Wenbo Ding,Jianhua Wang,Changyang Li,Binge Ma,Yi Luo,Ziyu Jiang,Chengcheng Wang,Juan Chen,Jian Hou,Hong-mei Yan,Lei Yang,Xiao-bin Jia 대한약학회 2018 Archives of Pharmacal Research Vol.41 No.3

Alantolactone is a sesquiterpene lactone isolatedfrom Inula helenium L. Although alantolactone possessesanti-inflammation and apoptosis-induction activities, theunderlying mechanism of anti-cancer effect on humanbreast cancer cells remains largely unknown. In this study,we explored the possibility of alantolactone as an apoptosis-inducing cytotoxic agent using MDA-MB-231 cells asin vitro model. Alantolactone significantly induced itsapoptosis, demonstrated by cell cycle analysis, annexinV-APC/7-AAD double staining and dUTP nick end labeling. Additionally, alantolactone triggered the mitochondrial-mediated caspase cascade apoptotic pathway, whichwas confirmed by increased Bax/Bcl-2 ratio, loss of MMP,release of cytc from mitochondria to cytoplasm, activationof caspase 9/3, and subsequent cleavage of PARP. Z-VADFMKpartially prevented apoptosis induced by alantolactone. Alantolactone provoked the production of ROS, whileNAC (a scavenger of ROS) reversed alantolactone-mediateddepolarization of MMP and apoptosis. Alantolactonemodulated the activities of MAPKs. As expected, cotreatmentwith SB203580, SP600125 or U0126 could reducedthe apoptotic rate. Furthermore, alantolactone decreasedthe protein expressions of p-NF-kB p65 and p-STAT3,increased p-c-Jun level in a dose-dependent manner. Thesefindings suggested that alantolactone possessed anticanceractivity via ROS-mediated mitochondrial dysfunctioninvolving MAPK pathway, and had an effect on the transcriptionfactors of NF-kB, AP-1 and STAT3.

An Improved Method for Extracting Bacteria from Soil for High Molecular Weight DNA Recovery and BAC Library Construction

Juan Liu,Jingquan Li,Li Feng,Hui Cao,Zhongli Cui 한국미생물학회 2010 The journal of microbiology Vol.48 No.6

Separation of bacterial cells from soil is a key step in the construction of metagenomic BAC libraries with large DNA inserts. Our results showed that when combined with sodium pyro-phosphate and homogenization for soil dispersion, sucrose density gradient centrifugation (SDGC) was more effective at separating bacteria from soil than was low speed centrifugation (LSC). More than 70% of the cells, along with some soil colloids,were recovered with one round of centrifugation. A solution of 0.8% NaCl was used to resuspend these cell and soil pellets for purification with nycodenz density gradient centrifugation (NDGC). After purification,more than 30% of the bacterial cells in the primary soil were extracted. This procedure effectively removed soil contamination and yielded sufficient cells for high molecular weight (HMW) DNA isolation. Ribosomal intergenic spacer analysis (RISA) showed that the microbial community structure of the extracted cells was similar to that of the primary soil, suggesting that this extraction procedure did not significantly change the the soil bacteria community structure. HMW DNA was isolated from bacterial cells extracted from red soil for metagenomic BAC library construction. This library contained DNA inserts of more than 200 Mb with an average size of 75 kb.

A New Practical System for Evaluating the Pharmacological Properties of Uricase as a Potential Drug for Hyperuricemia

Juan Feng,Xiang Li,Xiaolan Yang,Chun Zhang,Yonghua Yuan,Jun Pu,Yunsheng Zhao,Yanling Xie,Huidong Yuan,Youquan Bu,Fei Liao 대한약학회 2010 Archives of Pharmacal Research Vol.33 No.11

The use of uricase-deficient mammals to screen formulations of engineered uricases as potential drugs for hyperuricemia involves heavy costs and presents a technical bottleneck. Herein, a new practical system was investigated to evaluate the pharmacological significance of a bacterial uricase based on its ability to eliminate uric acid in plasma in vitro, its pharmacokinetics in vivo in healthy rats, and the modeled pharmacodynamics in vivo. This uricase, before and after modification with the monomethyl ether of poly(ethylene glycol)-5000, effectively eliminated uric acid in vitro in rabbit plasma, but its action was susceptible to xanthine inhibition. After intravenous injection of the modified uricase without purification, a bi-exponential model fit well to uricase activities in vivo in the plasma of healthy rats; the half-life of the modified uricase was estimated without interference from the unmodified uricase leftover in the sample and was nearly 100-fold longer than that of the unmodified uricase. Using a model of the elimination of uric acid in vivo taking into account of uricase pharmacokinetics and xanthine inhibition, modeled pharmacodynamics supported that the half-life of uricase and its susceptibility to xanthine are crucial for the pharmacological significance of uricase. Hence,this practical system is desirable for doing preliminary screening of formulations of engineered uricases as potential drugs for hyperuricemia.

Edge-Controlled Growth and Etching of Two-Dimensional GaSe Monolayers

Li, Xufan,Dong, Jichen,Idrobo, Juan C.,Puretzky, Alexander A.,Rouleau, Christopher M.,Geohegan, David B.,Ding, Feng,Xiao, Kai American Chemical Society 2017 JOURNAL OF THE AMERICAN CHEMICAL SOCIETY - Vol.139 No.1

<P>Understanding the atomistic mechanisms governing the growth of two-dimensional (2D) materials is of great importance in guiding the synthesis of wafer-sized, single-crystalline, high-quality 2D crystals and heterostructures. Etching, in many cases regarded as the reverse process of material growth, has been used to study the growth kinetics of graphene. In this work, we explore a growth-etching-regrowth process of monolayer GaSe crystals, including single-crystalline triangles and irregularly shaped domains formed by merged triangles. We show that the etching begins at a slow rate, creating triangular, truncated triangular, or hexagonally shaped holes that eventually evolve to exclusively triangles that are rotated 60 degrees with respect to the crystalline orientation of the monolayer triangular crystals. The regrowth occurs much faster than etching, reversibly filling the etched holes and then enlarging the size of the monolayer crystals. A theoretical model developed based on kinetic Wulff construction (KWC) theory and density functional theory (DFT) calculations accurately describe the observed morphology evolution of the monolayer GaSe crystals and etched holes during the growth and etching processes, showing that they are governed by the probability of atom attachment/detachment to/from different types of edges with different formation energies of nucleus/dents mediated by chemical potential difference Ait between Ga and Se. Our growth-etching-regrowth study provides not only guidance to understand the growth mechanisms of 2D binary crystals but also a potential method for the synthesis of large, shape-controllable, high-quality single-crystalline 2D crystals and their lateral heterostructures.</P>

Initial selection of groove location combination for multi-groove casing treatments

Juan Du,Lipeng Gao,Jichao Li,Feng Lin,Jingyi Chen 대한기계학회 2016 JOURNAL OF MECHANICAL SCIENCE AND TECHNOLOGY Vol.30 No.2

Stall margin improvement (SMI) curve is a function of a single groove location for a low-speed axial compressor and is investigated numerically and experimentally in this paper. SMI curve illustrates that good grooves are located in a fairly wide region approximately from 30% C ax to 80% C ax aft of the rotor leading edge. The narrow region that contains bad grooves is near 20% C ax aft of the rotor leading edge. The initial selection of groove location combination for multi-groove casing treatments is proposed based on the SMI and efficiency improvement data generated by a series of single-groove and multi-groove casing treatments. The grooves should be set in the “wide region” of the SMI curve. The grooves located near the “narrow region” and the rotor trailing edge should be avoided. The “narrow region” can be identified by the axial momentum distribution of the tip leakage flow or the circumferentially averaged axial shear stress on the casing using the simulation results of the smooth casing at the near-stall point.