11 results on '"Li, Xu-Wen"'
Search Results
2. Unusual polyoxygenated casbane diterpenoids from the South China Sea soft coral Sinularia erecta.
- Author
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Liu J, Wu MJ, Li H, Wang H, Tang W, Gu YC, Li XW, and Guo YW
- Subjects
- Animals, Anti-Inflammatory Agents chemistry, Anti-Inflammatory Agents isolation & purification, Diterpenes chemistry, Diterpenes isolation & purification, Mice, Peroxides chemistry, Peroxides isolation & purification, RAW 264.7 Cells, Stereoisomerism, Anthozoa chemistry, Anti-Inflammatory Agents pharmacology, Diterpenes pharmacology, Peroxides pharmacology
- Abstract
A further systematically chemical investigation of the South China Sea soft coral Sinularia erecta led to the discovery of two rare casbane diterpenoids with an uncommon 8,10-peroxide bridge, sinuereperoxides B (1) and C (2), five new casbanes with other oxygenated patterns (3-7), and seven known casbanes (8-14). The structures and absolute configurations of 1-7 were established by extensive spectroscopic data analyses, X-ray diffraction analysis, and/or quantum chemical calculations. In bioassay, compounds 2, 7, 11 and 12 exhibited considerable anti-inflammatory activity by the inhibition of TNF-α release, with IC
50 values of 33.8 μM, 5 μM, 9.9 μM and 8 μM., (Copyright © 2021 Elsevier Inc. All rights reserved.)- Published
- 2021
- Full Text
- View/download PDF
3. Sinusiaetone A, an Anti-inflammatory Norditerpenoid with a Bicyclo[11.3.0]hexadecane Nucleus from the Hainan Soft Coral Sinularia siaesensis .
- Author
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Chen ZH, Li WS, Zhang ZY, Luo H, Wang JR, Zhang HY, Zeng ZR, Chen B, Li XW, and Guo YW
- Subjects
- Alkanes, Animals, Anti-Inflammatory Agents chemistry, Bridged Bicyclo Compounds chemistry, Lipopolysaccharides chemistry, Molecular Structure, Anthozoa chemistry, Anti-Inflammatory Agents pharmacology, Bridged Bicyclo Compounds pharmacology, Diterpenes chemistry, Lipopolysaccharides pharmacology
- Abstract
A novel norditerpenoid, sinusiaetone A ( 1 ), featuring an uncommon bicyclo[11.3.0]hexadecane carbon skeleton, and four polyoxygenated cembranoids ( 2-5 ) were isolated from the Hainan soft coral Sinularia siaesensis . Their structures were established by spectroscopic analysis, X-ray diffraction, quantum chemical computational approaches, and/or a modified Mosher's method. A plausible biosynthetic pathway of 1 and its biogenetic relationship with 2-5 were proposed. New compounds 1-3 displayed an interesting inhibitory activity against lipopolysaccharide-induced inflammation in BV-2 microglial cells.
- Published
- 2021
- Full Text
- View/download PDF
4. Diversity-oriented synthesis of cembranoid derivatives as potential anti-inflammatory agents.
- Author
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Zhang C, Li H, Liu J, Liu M, Zhang H, Chen KX, Guo YW, Tang W, and Li XW
- Subjects
- Animals, Anti-Inflammatory Agents chemical synthesis, Anti-Inflammatory Agents chemistry, Cells, Cultured, Diterpenes chemical synthesis, Diterpenes chemistry, Dose-Response Relationship, Drug, Mice, Models, Molecular, Molecular Structure, RAW 264.7 Cells, Signal Transduction drug effects, Structure-Activity Relationship, Anti-Inflammatory Agents pharmacology, Diterpenes pharmacology, Transforming Growth Factor beta antagonists & inhibitors
- Abstract
Eleven novel cembranoid derivatives were designed, synthesized, and evaluated for their inflammation related activities on the basis of our isolated and previously reported anti-inflammatory marine cembranoids. In bioassay, compound 11 displayed the most promising inhibitory effects with IC
50 value of 1.1 μM for the TNF-α inhibitory activity. The further mechanism study of 11 on the inflammatory signaling transduction of RAW264.7 cells was also performed. This research may give an insight for the discovery of marine cembranoid derived anti-inflammatory drug leads., (Copyright © 2021 Elsevier Inc. All rights reserved.)- Published
- 2021
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- View/download PDF
5. Chemical Constituents from Citrus changshan-huyou and Their Anti-Inflammatory Activities.
- Author
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Hu YH, Liu J, Li H, Tang W, Li XW, and Guo YW
- Subjects
- Animals, Anti-Inflammatory Agents isolation & purification, Anti-Inflammatory Agents pharmacology, Citrus metabolism, Fruit chemistry, Fruit metabolism, Limonins chemistry, Limonins isolation & purification, Limonins pharmacology, Lipopolysaccharides pharmacology, Macrophages cytology, Macrophages drug effects, Macrophages metabolism, Magnetic Resonance Spectroscopy, Medicine, Chinese Traditional, Mice, Molecular Conformation, Plant Extracts chemistry, RAW 264.7 Cells, Structure-Activity Relationship, Tumor Necrosis Factor-alpha metabolism, Anti-Inflammatory Agents chemistry, Citrus chemistry
- Abstract
A systematically chemical investigation of Citrus changshan-huyou Y.B.Chang resulted in the isolation and structure determination of twelve known natural products, including limonoid, nootkatone, scoparone, β-sitosterol, 3,3',4',5,6,7,8,-heptamethoxyflavone, nobiletin, tangeretin, naringin, hesperidin, neohesperidin, 3,5-dihydroxyphenyl β-D-glucoside, β-sitosterol-D-glucoside. The structure modification of the most abundant compound limonin further led to eight limonoid derivatives, including epi-limonol, epi-limonyl acetate, and six new compounds epi-limonol A, limonol A, limonol B, epi-limonol B, epi-limonol C, epi-limonol D, which enlarged the chemical diversity of limonin related limonoids. The structures of the new limonoid derivatives were identified by extensive spectroscopic analysis. In bioassay, all the isolates, the semi-synthetic derivatives and the previously isolated limonoids in our natural product library were subjected for anti-inflammatory activities evaluation, and several limonoids exhibited the inhibition of TNF-α release., (© 2020 Wiley-VHCA AG, Zurich, Switzerland.)
- Published
- 2020
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6. Synthesis and Target Identification of Benzoxepane Derivatives as Potential Anti-Neuroinflammatory Agents for Ischemic Stroke.
- Author
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Gao CL, Hou GG, Liu J, Ru T, Xu YZ, Zhao SY, Ye H, Zhang LY, Chen KX, Guo YW, Pang T, and Li XW
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- Animals, Anti-Inflammatory Agents pharmacology, Anti-Inflammatory Agents therapeutic use, Dibenzoxepins pharmacology, Dibenzoxepins therapeutic use, Disease Models, Animal, Infarction, Middle Cerebral Artery complications, Infarction, Middle Cerebral Artery pathology, Interleukin-1beta genetics, Interleukin-1beta metabolism, Ischemic Stroke drug therapy, Ischemic Stroke etiology, Lipopolysaccharides toxicity, Macrophages cytology, Macrophages drug effects, Macrophages metabolism, Mice, Microglia cytology, Microglia drug effects, Microglia metabolism, NLR Family, Pyrin Domain-Containing 3 Protein metabolism, Naphthoquinones therapeutic use, Pyruvate Kinase antagonists & inhibitors, Pyruvate Kinase metabolism, RAW 264.7 Cells, Rats, Structure-Activity Relationship, Tumor Necrosis Factor-alpha genetics, Tumor Necrosis Factor-alpha metabolism, Anti-Inflammatory Agents chemical synthesis, Dibenzoxepins chemistry
- Abstract
Benzoxepane derivatives were designed and synthesized, and one hit compound emerged as being effective in vitro with low toxicity. In vivo, this hit compound ameliorated both sickness behavior through anti-inflammation in LPS-induced neuroinflammatory mice model and cerebral ischemic injury through anti-neuroinflammation in rats subjected to transient middle cerebral artery occlusion. Target fishing for the hit compound using photoaffinity probes led to identification of PKM2 as the target protein responsible for anti-inflammatory effect of the hit compound. Furthermore, the hit exhibited an anti-neuroinflammatory effect in vitro and in vivo by inhibiting PKM2-mediated glycolysis and NLRP3 activation, indicating PKM2 as a novel target for neuroinflammation and its related brain disorders. This hit compound has a better safety profile compared to shikonin, a reported PKM2 inhibitor, identifying it as a lead compound in targeting PKM2 for the treatment of inflammation-related diseases., (© 2019 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim.)
- Published
- 2020
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7. Klyflaccilides A and B, Diterpenoids with 6/5/8/3 Fused Tetracyclic Carbon Skeleton from the Hainan Soft Coral Klyxum flaccidum .
- Author
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Li G, Li H, Tang W, Guo YW, and Li XW
- Subjects
- Animals, Models, Molecular, Molecular Conformation, Quantum Theory, Anthozoa chemistry, Anti-Inflammatory Agents chemistry, Diterpenes chemistry
- Abstract
Two novel polyoxygenated diterpenoids, klyflaccilides A ( 1 ) and B ( 2 ), featuring an uncommon 6/5/8/3 tetracyclic ring system, were isolated from the Hainan soft coral Klyxum flaccidum . Their structures were established by extensive spectroscopic analysis, X-ray diffraction analysis, and/or a quantum chemical computation method. A plausible biosynthetic relationship of 1 and 2 with their potential precursor 3 was further proposed. Compounds 1 and 3 exhibited moderate anti-inflammatory activity by the inhibition of LPS-induced TNF-α protein release.
- Published
- 2019
- Full Text
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8. Diversity-oriented synthesis of marine sponge derived hyrtioreticulins and their anti-inflammatory activities
- Author
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LI Xu-wen, Guo Yue-Wei, Pang Tao, Liu Jin, Chen Bo-Ru, Gao Cheng-Long, and Jiang Jian-Lan
- Subjects
Drug ,medicine.drug_class ,media_common.quotation_subject ,medicine.medical_treatment ,Anti-Inflammatory Agents ,Anti-inflammatory ,Indole Alkaloids ,Structure-Activity Relationship ,Drug Discovery ,medicine ,Animals ,media_common ,Indole test ,Biological Products ,Pictet–Spengler reaction ,Indole alkaloid ,biology ,Chemistry ,Biological activity ,General Medicine ,biology.organism_classification ,Porifera ,Sponge ,Cytokine ,Complementary and alternative medicine ,Biochemistry - Abstract
Diversity-oriented synthesis is aiming to increase the chemical diversity of the target natural products for extensive biological activity evaluation. Indole ring is an important functional group in a large number of drugs and other biologically active agents, and indole-containing natural products have been frequently isolated from marine sources in recent years. In this paper, a series of indole-containing marine natural hyrtioreticulin derivatives, including 19 new ones, were designed, synthesized via a key Pictet-Spengler reaction, and evaluated for their inflammation related activity. Compound 13b displayed the most promising activity by inhibiting TNF-α cytokine release with inhibitory rate of 92% at a concentration of 20 μM. A preliminary structure-activity relationship analysis was also discussed. This research may give an insight for the discovery of marine indole alkaloid derived anti-inflammatory drug leads.
- Published
- 2021
9. Bioactive polyoxygenated cembranoids from a novel Hainan chemotype of the soft coral Sinularia flexibilis.
- Author
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Wu, Qihao, Li, Xu-Wen, Li, Heng, Yao, Li-Gong, Tang, Wei, Miao, Ze-Hong, Wang, Hong, and Guo, Yue-Wei
- Subjects
- *
ALCYONACEA , *BIOACTIVE compounds , *ANTI-inflammatory agents , *CELL-mediated cytotoxicity , *X-ray diffraction - Abstract
Graphical abstract Highlights • Three novel structures were isolated and identified from soft coral Sinularia flexibilis. • The cembranoids from S. flexibilis in South China Sea showed great chemical diversity. • Several cembranoids exhibited strong anti-inflammatory effect and cytotoxicity. Abstract Different chemotypes of Sinularia flexibilis exist in the Hainan island. Thus, a collection of this soft coral from a location different from the one of our previous study afforded three novel cembranoid esters featuring a n -butyl alcohol moiety, a structural element rare in natural products of both terrestrial and marine origin. The structures of the new compounds were elucidated by detailed spectroscopic analysis and by the comparison of their spectroscopic data with those reported in the literature. In addition, the absolute stereochemistry of the previously reported diepoxycembrene (9) was first time determined by the X-ray diffraction analysis. In bioassays, compounds 6 – 8 exhibited strong anti-inflammatory effect with IC 50 values of 2.7, 4.7, and 4.2 μM, respectively, whereas compound 5 displayed cytotoxicity against several cancer cells with IC 50 values ranging from 8.9 to 27.4 μM. A preliminary structural-activity relationship (SAR) was also described. [ABSTRACT FROM AUTHOR]
- Published
- 2019
- Full Text
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10. Design, synthesis and in vitro biological evaluation of marine phidianidine derivatives as potential anti-inflammatory agents.
- Author
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Xu, Quan, Zhao, Ning, Liu, Jin, Song, Jin-Qian, Huang, Li-Hua, Wang, Hong, Li, Xu-Wen, Pang, Tao, and Guo, Yue-Wei
- Subjects
- *
BIOSYNTHESIS , *INDOLE alkaloids , *ANTI-inflammatory agents , *T helper cells , *MOLECULAR docking , *PHORBOL esters - Abstract
[Display omitted] • A series of phidianidine derivatives were synthesized to study anti-inflammatory activity. • Compounds 9a and 22c exhibited excellent anti-inflammatory activity and low toxicity on IL-17A production in PMA and ionomycin-stimulated EL4 cells. • Compound 9a could decrease the STAT3 phosphorylation at Y705 to inhibit IL-17A production in EL-4 cells. • Molecular docking analysis explained our SAR study. Phidianidines A and B are novel marine indole alkaloids with various biological activities. Based on their potential anti-inflammatory properties, a series of phidianidine derivatives were designed, synthesized, and tested for their effects on IL-17A production in PMA/ionomycin-stimulated T -cell-lymphoma EL-4 cells. Compounds 9a and 22c exhibited excellent anti-inflammatory activity and low toxicity, with IC 50 values of 7.7 μM and 5.3 μM for IL-17A production in PMA/ionomycin-stimulated EL-4 cells, respectively. Further mechanistic study showed that 9a could decrease the STAT3 phosphorylation at Y705 to inhibit IL-17A production in EL-4 cells, indicating its ability of preventing the differentiation of Th17 cells and their possible function. This research may give an insight for the discovery of marine indole alkaloid derived anti-inflammatory drug leads for the treatment of T cell-mediated diseases. [ABSTRACT FROM AUTHOR]
- Published
- 2022
- Full Text
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11. Synthesis of rabdokunmin C analogues and their inhibitory effect on NF-κB activation
- Author
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Aoyagi, Yutaka, Adachi, Yoshiyuki, Ozawa, Kei, Yokomizo, Chihiro, Gui, Ming-Yu, Jin, Yong-Ri, Li, Xu-Wen, Ohno, Naohito, and Takeya, Koichi
- Subjects
- *
DRUG development , *ANTI-inflammatory agents , *NF-kappa B , *B cells , *ENZYMES , *ABSORPTION , *CHEMICAL inhibitors , *BIOLOGICAL assay - Abstract
Abstract: A series of rabdokunmin C analogues were prepared and their inhibitory effect on NF-κB activation was assayed. One of them, 18-acetyl-12-deoxy-11,12-dehydrorabdokunmin C (16) was found to be a promising candidate for an anti-inflammatory agent. [Copyright &y& Elsevier]
- Published
- 2011
- Full Text
- View/download PDF
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