通过表型筛选鉴定用于治疗骨关节炎的双功能桦木酸类似物。 - Suppr

Identification of a dual functional betulinic acid analog for the treatment of osteoarthritis by phenotypic screening.

作者信息

Lin Ze-Min, Xiang Mai, Wei Wen-Hui, Fan Shu-Hui, Chen Li, Wang Jie, Yang Xiao-Qian, Yang Chun-Hao, He Shi-Jun, Zuo Jian-Ping

机构信息

Laboratory of Immunopharmacology, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, 201203, China.

School of Pharmacy, University of Chinese Academy of Sciences, Beijing, 100049, China.

出版信息

Sci China Life Sci. 2025 Jan;68(1):300-302. doi: 10.1007/s11427-023-2587-2. Epub 2024 Oct 25.

DOI:10.1007/s11427-023-2587-2

PMID:39465461

Abstract

摘要

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Identification of a dual functional betulinic acid analog for the treatment of osteoarthritis by phenotypic screening.通过表型筛选鉴定用于治疗骨关节炎的双功能桦木酸类似物。

Sci China Life Sci. 2025 Jan;68(1):300-302. doi: 10.1007/s11427-023-2587-2. Epub 2024 Oct 25.

Betulinic acid-induced Mcl-1 expression in human melanoma--mode of action and functional significance.桦木酸诱导人黑色素瘤中Mcl-1表达的作用机制及功能意义

Mol Med. 2002 Dec;8(12):877-84.

Betulinic acid derivative BA5, a dual NF-kB/calcineurin inhibitor, alleviates experimental shock and delayed hypersensitivity.桦木酸衍生物BA5，一种双重NF-κB/钙调神经磷酸酶抑制剂，可减轻实验性休克和迟发型超敏反应。

Eur J Pharmacol. 2017 Nov 15;815:156-165. doi: 10.1016/j.ejphar.2017.09.008. Epub 2017 Sep 9.

Betulinic acid, a potent inhibitor of eukaryotic topoisomerase I: identification of the inhibitory step, the major functional group responsible and development of more potent derivatives.桦木酸，一种有效的真核生物拓扑异构酶I抑制剂：抑制步骤的鉴定、主要功能基团的确定以及更有效衍生物的开发。

Med Sci Monit. 2002 Jul;8(7):BR254-65.

Betulinic acid analogs inhibit N- and T-type voltage-gated calcium channels to attenuate nerve-injury associated neuropathic and formalin models of pain.桦木酸类似物可抑制N型和T型电压门控钙通道，以减轻与神经损伤相关的神经性疼痛和福尔马林疼痛模型。

Neurobiol Pain. 2023 Jan 14;13:100116. doi: 10.1016/j.ynpai.2023.100116. eCollection 2023 Jan-Jul.

Betulinic acid inhibits IL-1β-induced inflammation by activating PPAR-γ in human osteoarthritis chondrocytes.桦木酸通过激活人骨关节炎软骨细胞中的过氧化物酶体增殖物激活受体-γ抑制白细胞介素-1β诱导的炎症。

Int Immunopharmacol. 2015 Dec;29(2):687-692. doi: 10.1016/j.intimp.2015.09.009. Epub 2015 Sep 29.

Synthesis and Biological Evaluation of C-17-Amino-Substituted Pyrazole-Fused Betulinic Acid Derivatives as Novel Agents for Osteoarthritis Treatment.C-17-氨基取代的吡唑并白桦脂酸衍生物的合成及生物评价作为骨关节炎治疗的新型药物。

J Med Chem. 2021 Sep 23;64(18):13676-13692. doi: 10.1021/acs.jmedchem.1c01019. Epub 2021 Sep 7.

Boosting the biosynthesis of betulinic acid and related triterpenoids in Yarrowia lipolytica via multimodular metabolic engineering.通过多模块代谢工程提高解脂耶氏酵母中白桦脂酸和相关三萜类化合物的生物合成。

Microb Cell Fact. 2019 May 3;18(1):77. doi: 10.1186/s12934-019-1127-8.

Synthesis and cytotoxicity of triterpenoids derived from betulin and betulinic acid via click chemistry.通过点击化学法由桦木醇和桦木酸衍生的三萜类化合物的合成及其细胞毒性

J Asian Nat Prod Res. 2015;17(2):159-69. doi: 10.1080/10286020.2014.979164. Epub 2014 Nov 7.

Proteomic investigation into betulinic acid-induced apoptosis of human cervical cancer HeLa cells.桦木酸诱导人宫颈癌HeLa细胞凋亡的蛋白质组学研究

PLoS One. 2014 Aug 22;9(8):e105768. doi: 10.1371/journal.pone.0105768. eCollection 2014.

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Bioactive silica nanoparticles target autophagy, NF-κB, and MAPK pathways to inhibit osteoclastogenesis.生物活性硅纳米颗粒靶向自噬、NF-κB 和 MAPK 通路抑制破骨细胞生成。

Biomaterials. 2023 Oct;301:122238. doi: 10.1016/j.biomaterials.2023.122238. Epub 2023 Jul 5.

Phenotypic drug discovery: recent successes, lessons learned and new directions.表型药物发现：近期的成功、经验教训和新方向。

Nat Rev Drug Discov. 2022 Dec;21(12):899-914. doi: 10.1038/s41573-022-00472-w. Epub 2022 May 30.

Diagnosis and Treatment of Hip and Knee Osteoarthritis: A Review.髋关节和膝关节骨关节炎的诊断与治疗：综述

JAMA. 2021 Feb 9;325(6):568-578. doi: 10.1001/jama.2020.22171.

Melatonin alleviates intervertebral disc degeneration by disrupting the IL-1β/NF-κB-NLRP3 inflammasome positive feedback loop.褪黑素通过破坏白细胞介素-1β/核因子κB-NLRP3炎性小体正反馈环来减轻椎间盘退变。

Bone Res. 2020 Feb 18;8:10. doi: 10.1038/s41413-020-0087-2. eCollection 2020.

Improved betulinic acid biosynthesis using synthetic yeast chromosome recombination and semi-automated rapid LC-MS screening.利用合成酵母染色体重组和半自动化快速 LC-MS 筛选提高白桦脂酸生物合成。

Nat Commun. 2020 Feb 13;11(1):868. doi: 10.1038/s41467-020-14708-z.

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Identification of a dual functional betulinic acid analog for the treatment of osteoarthritis by phenotypic screening.

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