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Triterpene saponins with XOD inhibitory activity from the roots of Ilex pubescens

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Chinese Chemical Letters 2011年第6期22卷 697-700页

作者： li ping lin Wei Qu Jing Yu liang Department of Natural Medicinal Chemistry China Pharmaceutical University Nanjing 210009 China

A new triterpene saponin with 28-nor-urs-12（13）,18（17）-dien-3β-ol as aglycone,named ilexsaponin C（1） was isolated from the roots of Ilex pubescens,together with three known saponins 2,3 and *** structure of 1 was elucidated on the basis of spectral analysis including 1D and 2D NMR and *** 1 and 4 exhibited significant XOD inhibitory activity in the test.

关键词： Triterpene saponin Ilex pubescens Ilexsaponin C Xanthine oxidase

The first examples of ilexgenin A hybrids as a new class of multi-potent,anti-platelet agents

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Chinese Chemical Letters 2013年第8期24卷 723-726页

作者： li-ping lin Fei-Hua Wu Jing-Yu liang School of Traditional Chinese Pharmacy China Pharmaceutical University Jiangsu Center for Research & Development of Medicinal Plants Institute of BotanyJiangsu Province and Chinese Academy of Sciences

Seventeen novel ilexgenin A hybrids（lA-aspirin） and（IA-NO）,as donor hybrids（IA-NO will release NO in vivo and function as NO donor）,were designed and synthesized in order to develop new multi-targeting agents for the treatment of platelet *** in vitro activities against ADP,AA and thrombin were *** a result,IA hybrids achieved substantial increases in the three tested pathways compared with ***,the most potent hybrid compounds 6d and 14d displayed about 8-fold higher potency than aspirin,and 3-fold higher potency than the simultaneous administration of aspirin and IA in inhibiting ADP-induced aggregation with IC_（50） values of 0.15 mmol/L and 0.14 mmol/L,respectively. The results suggest these IA hybrids are good candidates for multi-target therapies,and especially,may be considered as promising ADP agonists.

关键词： Ilexgenin A Hybrids Multi-potent anti-platelet activity ADP agonists

Post-ingestion conversion of dietary indoles into anticancer agents

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National Science Review 2022年第4期9卷 128-138页

作者： li ping lin Dan liu Jia Cheng Qian liang Wu Quan Zhao Ren Xiang Tan State Key Laboratory of Pharmaceutical Biotechnology Institute of Functional BiomoleculesNanjing University State Key Laboratory Cultivation Base for TCM Quality and Efficacy Nanjing University of Chinese Medicine

There are health benefits from consuming cruciferous vegetables that release indole-3-carbinol(I3 C), but the in vivo transformation of I3 C-related indoles remains underinvestigated. Here we detail the post-ingestion conversion of I3 C into antitumor agents, 2-(indol-3-ylmethyl)-3,3′-diindolylmethane(LTr1) and 3,3′-diindolylmethane(DIM), by conceptualizing and materializing the reaction flux derailing(RFD) approach as a means of unraveling these stepwise transformations to be non-enzymatic but p H-dependent and gut microbe-sensitive. In the upper(or acidic) gastrointestinal tract, LTr1 is generated through Michael addition of 3-methyleneindolium(3 MI, derived in situ from I3 C) to DIM produced from I3 C via the formaldehyde-releasing(major) and CO-liberating(minor) pathways. In the large intestine,‘endogenous’ I3 C and DIM can form, respectively, from couplings of formaldehyde with one and two molecules of indole(a tryptophan catabolite). Acid-producing gut bacteria such as Lactobacillus acidophilus facilitate the H+-promotable steps. This work updates our understanding of the merits of I3 C consumption and identifies LTr1 as a drug candidate.

关键词： indole-3-carbinol reaction flux derailing (RFD) approach 2-(indol-3-ylmethyl)-3,3′-diindolylmethane (LTr1) anticancer Lactobacillus acidophilus

Bacterial spectrum and resistance patterns in corneal infections at a Tertiary Eye Care Center in South China

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International Journal of Ophthalmology(English edition) 2016年第3期9卷 384-389页

作者： Nan Wang Qiang Huang Yi-Wei Tan li-ping lin Kai-li Wu Zhongshan Ophthalmic Center State Key Laboratory of OphthalmologySun Yat-sen University

AIM： To investigate the spectrum and antibiotic susceptibility of bacteria isolated from patients with suspected corneal infections in Zhongshan Ophthalmic Center in South China over the past four years retrospectively. METHODS： Totally 1943 corneal scrapes from patients with corneal infections from 2010 to 2013 were cultured and processed using standard microbiological procedures to identify bacterial isolates. Simultaneously, the bacterial isolates were tested for antibiotic susceptibility to 8 antibiotics （ceftazidime, cefuroxim, cefazolin, levofloxacin, ofloxacin, neomycin, tobramycin, chloramphenicol） using the Kirby-Bauer disc diffusion technique. RESULTS： Of the total 1943 scrapes, 397 （20.43%） were culture-positive, of which 294 （74.06%） were gram- positive （GP） and 103 （25.94%） were gram-negative （GN） bacteria. Of the GP organisms, the most prevalent genera were Staphylococcus spp. （56.17%, n=223）, Kocuria spp. （5.29%, n=21） and Micrococcus spp. （1.26%, n=5）. On the other hand, the most prevalent genera were Pseudomonas spp. （12.85%, n=51）, Burkholderia spp. （2.02%, n=8） and Acinetobacter spp. （1.51%, n =6） for the GN organisms. Among five antibiotics that have eye drop products, the resistant to neomycin of GP （7.82%, 95% Ch 4.72%-10.92%） and GN isolates （9.71%, 95% Ch 4.01%-15.41% ） was lowest, while the resistant to chloramphenicol was highest （GP： 34.35%, 95% Ch 28.92%-39.78%; GN： 60.19%, 95% Ch 50.74%-69.64%）. CONCLUSION： Staphylococcus spp. was the most common bacterial pathogens isolated from patients with corneal infections in this setting. High percentages of GP and GN bacteria were mostly susceptible to neomycin and highly resistant to chloramphenicol.

关键词： antibiotic susceptibility epidemiology corneal infections bacterial spectrum

Four new polyhydroxylated steroids from the South Sea sponge Plakortis sp.

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Chinese Journal of Natural Medicines 2020年第11期18卷 844-849页

作者： WANG Kun-Ya li ping-lin SUN Jing-Fan de Voogd Nicole J TANG Xu-li li Guo-Qiang Key Laboratory of Marine Drugs Chinese Ministry of EducationSchool of Medicine and PharmacyOcean University of ChinaQingdao 266003China Laboratory of Marine Drugs and Biological Products National Laboratory of Marine Science and TechnologyQingdao 266235China National Museum of Natural History PO Box 95172300 RA Leidenthe Netherlands Collge of Chemistry and Chemical Engineering Ocean Universiy of ChinaQingdao 266100China

Four new polyhydroxylated steroids plaksterols A–D(1–4), together with two known related steroids ergost-7,9(11),22-trien-3β,5α,6α-triol(5) and ergosta-6β-methoxy-7,22-diene-3β,5α-diol(6), were isolated from methanol extract of the South China Sea marine sponge Plakortis sp. Their structures were identified by spectroscopic analysis, including NMR, MS, and IR. The cytotoxicity of the polyhydroxylated steroids were evaluated, and compound 6 showed moderate inhibitory activities against K562, HL-60 and BEL-7402 cells.

关键词： Polyhydroxylated steroids Plakortis sp. Cytotoxic activity

Electrolytic reduction of Nantong coal and model compounds with oxygenic functional groups in an aqueous NaCl solution

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Journal of China University of Mining and Technology 2008年第1期18卷 112-115页

作者： ZHAO Wei YAO li-ping lin Juan ZONG Zhi-min School of Chemical Engineering China University of Mining ＆ Technology Xuzhou Jiangsu 221008 China

Electrolytic reductions of oxygenic functional groups （OFGs） on coal surface and coal model compounds with OFGs in an aqueous NaCl solution are studied by electrochemical methods combined with GC/MS, GC and FFIR analyses. Different electrode reactions, their corresponding potentials and dynamic equations during the processes are investigated. The results show that benzoic acid, benzaldehyde, benzalcohol and hypnone are reduced to benzaldehyde and benzalcohol, methoxybenzene and benzal- cohol, toluene and styrene, respectively, at the cathode. The corresponding electrode potentials and dynamic equations are deter- mined. *** reduction also leads to an increase in the contents of hydroxyl groups and aliphatic moieties and a corresponding decrease in those of carboxyl and carbonyl groups in Nantong coal, a high-sulfur coal, an enhancement in the flotation desulfurization of the coal. ER also reduces organic sulfur and FeS2 in the coal.

关键词： coal model compounds electrolytic reduction dynamic equations

Carbon-nitrogen bond formation to construct novel polyketide-indole hybrids from the indole-3-carbinol exposed culture of Daldinia eschscholzii

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Synthetic and Systems Biotechnology 2022年第2期7卷 750-755页

作者： li ping lin Min Wu Nan Jiang Wei Wang Ren Xiang Tan State Key Laboratory Cultivation Base for TCM Quality and Efficacy Nanjing University of Chinese MedicineNanjing210023China State Key Laboratory of Pharmaceutical Biotechnology Institute of Functional BiomoleculesNanjing UniversityNanjing210023China Key Laboratory of Cardiovascular&Cerebrovascular Medicine School of PharmacyNanjing Medical UniversityNanjing211166China Key Laboratory of Marine Drugs Ministry of EducationOcean University of ChinaQingdao266003China

A plenty of cytochrome P450s have been annotated in the Daldinia eschosholzii *** by the fact that some P450s have been reported to catalyze the carbon-nitrogen(C-N)bond formation,we were curious about whether hybrids through C-N bond formation could be generated in the indole-3-carbinol(I3C)exposed culture of *** expected,two skeletally undescribed polyketide-indole hybrids,designated as indolpolyketone A and B(1 and 2),were isolated and assigned to be constructed through C-N bond *** structures were elucidated by 1D and 2D NMR *** absolute configurations of 1 and 2 were determined by comparing the recorded and calculated electronic circular dichroism(ECD)***,the plausible biosynthetic pathways for 1 and 2 were *** 1 and 2 exhibited significant antiviral activity against H1N1 with IC_(50) values of 45.2 and 31.4μM,*** brief,compounds 1 and 2 were reported here for the first time and were the first example of polyketide-indole hybrids pieced together through C-N bond formation in the I3C-exposed culture of ***,this study expands the knowledge about the chemical production of *** through precursor-directed biosynthesis(PDB).

关键词： Polyketide-indole hybrids Daldinia eschosholzii Indole-3-carbinol C-N bond formation P450 Precursor-directed biosynthesis

Modification Method of lightning Shielding Angle Calculation for Transmission lines in Mountain Areas

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高电压技术 2013年第10期39卷 2445-2451页

作者： WANG ping li lin GENG Jianghai State Key Laboratory of Alternate Electrical Power System with Renewable Energy Sources North China Electric Power University Beijing 102206 China

Shielding angle is one of the main factors influencing lightning performance of transmission lines,which always stays in the focus of the design and the evaluation of lightning protection.A formula for the improved shielding angle is proposed for evaluating the lightning performance in different *** digital elevation model(DEM) is used to obtain the micro-topography data,such as the slope gradient,slope aspect,*** following results are obtained by analyzing the influence of topography factors on the improved shielding angle:(1) improved shielding angle non-linearly increases with the increase of the slope gradient and the slope aspect,(2) improved shielding angle is more sensitive to the slope gradient than to the slope aspect,(3) the improved shielding angle in the mountain terrains is much greater than the designed shielding *** may be the reason why the designed shielding angle is limited into the rational range,while the shielding faults occur frequently.

关键词：雷电屏蔽输电线路修改方法角度计算山区防雷性能地形数据数字高程模型

Synthesis and antitumor activity of novel salvicine analogues

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Chinese Chemical Letters 2011年第1期22卷 25-28页

作者： Fei Deng Jin Jian Lu Hong Ying liu li ping lin Jian Ding Jin Sheng Zhang State Key Laboratory of Drug Research Shanghai Institute of Materia Medica Chinese Academy of Sciences Shanghai 201203 China College of life Sciences Northwest A & F University Yangling 712100 China

Systematic structure modification of the side train of the lead compound saprothoquinone provides a series of salvicine analogues, fifteen of them were first reported. Some compounds were demonstrated potent cytotoxicity against tumor cells with the 50% inhibition concentration in the micromolar range. Furthermore some compounds showed potent topoisomerase II inhibitory effects. The preliminary structure-activity relationship of saprorthoquinone analogues was discussed according to their cytotoxicity against three tumor cells.

关键词： Saprorthoquinone Salvicine Antitumor Structural modification