Lingyi Kong

China Pharmaceutical University

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Papers

Citation

H-Index

i-10 index

Research Trends

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Document Type

Co-Authors

Jian‐Guang Luo

China Pharmaceutical University

115

Jun Luo

China Pharmaceutical University

103

Xiaobing Wang

Jiuquan Iron & Steel (China)

Junsong Wang

Nanjing University of Science and Technology

Ming‐Hua Yang

Kunming Medical University

Wen‐Jun Xu

China Pharmaceutical University

Fucheng Yin

State Key Laboratory of Natural Medicine

Shang Li

Shandong University

Dongrong Zhu

Tianjin University of Technology

Chao Han

Zhejiang Chinese Medical University

Cooperative Institutions

China Pharmaceutical University

489

State Key Laboratory of Natural Medicine

350

Chinese Academy of Sciences

137

Chinese Academy of Medical Sciences & Peking Union Medical College

Sichuan University

State Council of the People's Republic of China

Huazhong University of Science and Technology

Shanghai Jiao Tong University

Sun Yat-sen University

University of Chinese Academy of Sciences

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Semi-Synthesis of Harringtonolide Derivatives and Their Antiproliferative Activity

Molecules (2021)

Xiu-Tao Wu Lijie Gong Chen Chen Tao Ye Wu-Xi Zhou

Harringtonolide (HO), a natural product isolated from Cephalotaxus harringtonia, exhibits potent antiproliferative activity. However, little information has been reported on the systematic structure−activity relationship (SAR) of HO derivatives. Modifications on tropone, lactone, and allyl positions of HO (1) were carried out to provide 17 derivatives (2–13, 11a–11f). The in vitro antiproliferative activity against four cancer cell lines (HCT-116, A375, A549, and Huh-7) and one normal cell line (L-02) was tested. Amongst these novel derivatives, compound 6 exhibited comparable cell growth inhibitory activity to HO and displayed better selectivity index (SI = 56.5) between Huh-7 and L-02 cells. The SAR results revealed that the tropone and lactone moieties are essential for the cytotoxic activities, which provided useful suggestions for further structural optimization of HO.

Tropone

Natural product

Cancer cell lines

Structure–activity relationship

10.3390/molecules26051380

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Citations (8)

Iso-seco-tanapartholide from Artemisia argyi inhibits the PFKFB3-mediated glycolytic pathway to attenuate airway inflammation in lipopolysaccharide-induced acute lung injury mice

Journal of Ethnopharmacology (2022)

Min Kong Dongrong Zhu Junyi Dong Lingyi Kong Jian‐Guang Luo

10.1016/j.jep.2022.115781

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Citations (8)

Glycyrrhetinic Acid Functionalized Graphene Oxide for Mitochondria Targeting and Cancer Treatment In Vivo

Small (2017)

Chao Zhang Zunfeng Liu Ying Zheng Yadi Geng Chao Han

Abstract Mitochondria‐mediated apoptosis (MMA) is a preferential option for cancer therapy due to the presence of cell‐suicide factors in mitochondria, however, low permeability of mitochondria is a bottleneck for targeting drug delivery. In this paper, glycyrrhetinic acid (GA), a natural product from Glycyrrhiza glabra , is found to be a novel mitochondria targeting ligand, which can improve mitochondrial permeability and enhance the drug uptake of mitochondria. GA‐functionalized graphene oxide (GO) is prepared and used as an effective carrier for targeted delivery of doxorubicin into mitochondria. The detailed in vitro and in vivo mechanism study shows that GA‐functionalized GO causes a decrease in mitochondrial membrane potential and activates the MMA pathway. The GA‐functionalized drug delivery system demonstrates highly improved apoptosis induction ability and anticancer efficacy compared to the non‐GA‐functionalized nanocarrier delivery system. The GA‐functionalized nanocarrier also shows low toxicity, suggesting that it can be a useful tool for drug delivery.

Nanocarriers

10.1002/smll.201703306

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Citations (114)

Polypharmacological Drug Design Guided by Integrating Phenotypic and Restricted Fragment Docking Strategies

Journal of Medicinal Chemistry (2024)

Shang Li Xinxin Li Liangliang Ma Zhongwen Luo Fucheng Yin

Polypharmacological drugs are of great value for treating complex human diseases by the combinative modulation of several biological targets. However, multitarget drug design with more than two targets is challenging and generally discovered by serendipity. Herein, a restricted fragment docking (RFD) computational method combined with a phenotypic discovery approach was developed for rational polypharmacological drug design. Via genetic and drug combination studies in a microglial phenotype, we first identified novel synergistic effects by triple target modulation toward RIPK1, MAP4K4, and ALK. Drawing on the RFD method to explore virtual chemical spaces in three target pockets, we identified a lead compound,

Docking (animal)

Fragment (logic)

10.1021/acs.jmedchem.4c01731

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Citations (0)

CCDC 698929: Experimental Crystal Structure Determination

The Cambridge Structural Database (2009)

Jun Luo Junsong Wang Xiaobing Wang X. R. Huang Jian-Guang Luo

An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available from the CCDC and typically includes 3D coordinates, cell parameters, space group, experimental conditions and quality measures.

10.5517/ccrg93l

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Citations (0)

New lignans and acetophenone derivatives with α-glucosidase inhibitory activity from the leaves of Melicope patulinervia

Fitoterapia (2020)

Van‐Tuan Vu Manh-Tuyen Nguyen Nguyen-Minh Khoi Xiaojuan Xu Lingyi Kong

Acetophenone

IC50

10.1016/j.fitote.2020.104805

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Citations (7)

Red-Emitting Fluorescent Probe for Detection of γ-Glutamyltranspeptidase and Its Application of Real-Time Imaging under Oxidative Stress in Cells and in Vivo

Analytical Chemistry (2018)

Feiyan Liu Zhen Wang Wenli Wang Jian‐Guang Luo Lingyi Kong

γ-Glutamyltranspeptidase (GGT) plays critical roles in regulating various physiological/pathophysiological processes including the intracellular redox homeostasis. However, an effective fluorescent probe for dissecting the relationships between GGT and oxidative stress in vivo remains largely unexplored. Herein, we present a light-up fluorescent probe (DCDHF-Glu) with long wavelength emission (613 nm) for the highly sensitive and selective detection of GGT using dicyanomethylenedihydrofuran derivative as the fluorescent reporter and γ-glutamyl group as the enzyme-active trigger. DCDHF-Glu is competent to real-time image endogenous GGT in live cells and mice. In particular, DCDHF-Glu enables the direct real-time visualization of the upregulation of GGT under drug-induced oxidative stress in the HepG2 cells and the LO2 cells, as well as in vivo, vividly implying its excellent capacity in elucidation of GGT function in GGT-related biological events.

Homeostasis

10.1021/acs.analchem.8b00994

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Citations (50)

Discovery of First-in-Class Dual PARP and EZH2 Inhibitors for Triple-Negative Breast Cancer with Wild-Type BRCA

Journal of Medicinal Chemistry (2021)

Chéng Wáng Lailiang Qu Shang Li Fucheng Yin Limei Ji

PARP inhibitors have highly significant effects on BRCA mutant cells, allowing targeted therapy of triple-negative breast cancer (TNBC). However, some TBNC patients lack BRCA mutations. Recent studies have shown that EZH2 inhibitors can increase the sensitivity of wild-type BRCA cells to PARP inhibitors. We designed a series of dual PARP and EZH2 inhibitors, and the most promising compound, 5a, showed good inhibitory activity against PARP-1 and EZH2 and good inhibitory effects on MDA-MB-231 (IC50 = 2.63 μM) and MDA-MB-468 (IC50 = 0.41 μM) cells with wild-type BRCA. Compared with that of olaparib, the growth inhibitory activities against these two cell types increased by approximately 15- and 80-fold, respectively, which was even more effective than the combination of olaparib and tazemetostat/GSK126. 5a can induce autophagy death of tumor cells and cause less damage to normal cells. Therefore, 5a, as a first-in-class dual PARP and EZH2 inhibitor, is a potential anticancer drug candidate for the treatment of TNBC.

Olaparib

PARP inhibitor

Triple-negative breast cancer

10.1021/acs.jmedchem.1c00567

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Citations (49)

Coumarin-naphthol conjugated Schiff base as a “turn-on” fluorescent probe for Cu2+ via selective hydrolysis of imine and its application in live cell imaging

Journal of Photochemistry and Photobiology A Chemistry (2016)

Sisi Wang Zhen Wang Yong Yin Jian‐Guang Luo Lingyi Kong

Imine

Fluorescence-lifetime imaging microscopy

Turn (biochemistry)

HEPES

10.1016/j.jphotochem.2016.10.030

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Citations (45)

Anti-inflammatory diterpene dimers from the root barks of Aphanamixis grandifolia

Organic & Biomolecular Chemistry (2015)

Hongjian Zhang Yang‐Mei Zhang Jian‐Guang Luo Jun Luo Lingyi Kong

A total of 14 new diterpene dimers, aphanamenes C-P ()1-14, with four known homologous compounds were isolated from the root barks of Aphanamixis grandifolia Bl. The structures of these compounds were elucidated by spectroscopic analyses, and their absolute configurations were determined using the CD exciton chirality method. In addition, all the compounds exhibited significant inhibition of lipopolysaccharide-induced nitric oxide production in RAW264.7 macrophages, with IC50 values between 7.75 and 38.23 μM.

Chirality

10.1039/c5ob00674k

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Citations (17)