Synthesis and biological evaluation of novel sinomenine derivatives as anti-inflammatory and analgesic agent

Gao, Feng; Dai, Ziqi; Zhang, Tong; Gu, Yuhao; Cai, Desheng; Lu, Mingjun; Zhang, Zijie; Zeng, Qi; Shang, Bingxian; Xu, Bing; Lei, Haimin

doi:10.1039/d2ra05558a

Cited by 5 publications

(1 citation statement)

References 47 publications

(54 reference statements)

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“…Zhou et al found that N-demethyl SIN (30) attenuated neuropathic and inflammatory pain in mice, which was more effective than that of SIN [148]. F. Gao et al reported that SIN derivative 17 (31) significantly inhibited the secretion of the pro-inflammatory factor µnitric oxide in Mouse mononuclear macrophage leukemia cells Raw264.7, with an IC 50 value of 30.28 µM and no cytotoxic effects at concentrations up to 100 µM [149]. E.E.…”

Section: Anti-inflammatory Activity and Analgesic Activity Of Compoun...mentioning

confidence: 99%

Bioactivities and Mechanisms of Action of Sinomenine and Its Derivatives: A Comprehensive Review

Hou,

Huang,

Huang

et al. 2024

Molecules

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Sinomenine, an isoquinoline alkaloid extracted from the roots and stems of Sinomenium acutum, has been extensively studied for its derivatives as bioactive agents. This review concentrates on the research advancements in the biological activities and action mechanisms of sinomenine-related compounds until November 2023. The findings indicate a broad spectrum of pharmacological effects, including antitumor, anti-inflammation, neuroprotection, and immunosuppressive properties. These compounds are notably effective against breast, lung, liver, and prostate cancers, exhibiting IC50 values of approximately 121.4 nM against PC-3 and DU-145 cells, primarily through the PI3K/Akt/mTOR, NF-κB, MAPK, and JAK/STAT signaling pathways. Additionally, they manifest anti-inflammatory and analgesic effects predominantly via the NF-κB, MAPK, and Nrf2 signaling pathways. Utilized in treating rheumatic arthritis, these alkaloids also play a significant role in cardiovascular and cerebrovascular protection, as well as organ protection through the NF-κB, Nrf2, MAPK, and PI3K/Akt/mTOR signaling pathways. This review concludes with perspectives and insights on this topic, highlighting the potential of sinomenine-related compounds in clinical applications and the development of medications derived from natural products.

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Section: Anti-inflammatory Activity and Analgesic Activity Of Compoun...mentioning

confidence: 99%

Bioactivities and Mechanisms of Action of Sinomenine and Its Derivatives: A Comprehensive Review

Hou,

Huang,

Huang

et al. 2024

Molecules

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show abstract

Proposal for the classification of sinomenine alkaloids

Chen,

Xie,

Chen

et al. 2024

Fitoterapia

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A straightforward trifluoromethylation at the C6 position of morphinane alkaloids, their modification and evaluation of inhibition of the SARS-CoV-2 main protease

Finke,

Krasnov,

Rybalova

et al. 2023

Journal of Fluorine Chemistry

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Synthesis and biological evaluation of novel sinomenine derivatives as anti-inflammatory and analgesic agent

Abstract: A series of novel sinomenine derivatives were designed and synthesized. Among them, compound 17 showed strong anti-inflammatory and analgesic activities.

Cited by 5 publications

References 47 publications

Bioactivities and Mechanisms of Action of Sinomenine and Its Derivatives: A Comprehensive Review

Bioactivities and Mechanisms of Action of Sinomenine and Its Derivatives: A Comprehensive Review

Proposal for the classification of sinomenine alkaloids

A straightforward trifluoromethylation at the C6 position of morphinane alkaloids, their modification and evaluation of inhibition of the SARS-CoV-2 main protease

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