Discovery of novel danshensu derivatives bearing pyrazolone moiety as potential anti-ischemic stroke agents with antioxidant activity

Li, Yi; Luo, Yunchun; Wang, Jing; Sheng, Hao; Liao, Jun; Wang, Yan; Chen, Zhe‐Sheng; Xiong, Liangshan; Zhang, Chuan; Wang, Tingfang

doi:10.1016/j.bioorg.2022.106283

Cited by 8 publications

(4 citation statements)

References 48 publications

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“…Tanshinol is the main water‐soluble component of Salviae Miltiorrhizae Radix et Rhizoma . Tanshinol mainly has pharmacological effects such as anti‐coagulation, anti‐platelet aggregation, improvement of cerebral nerve damage, scavenging of free radicals, and anti‐inflammation (Li, Luo, et al, 2023; Seetapun et al, 2013). Ligustrazine Hydrochloride is the characteristic alkaloid of Chuanxiong Rhizoma and can be used as an indicator component to evaluate the alkaloid content of Chuanxiong Rhizoma .…”

Section: Ameliorative Effect Of Tcm Formulas On Ismentioning

confidence: 99%

Traditional Chinese medicines treat ischemic stroke and their main bioactive constituents and mechanisms

Fan,

Liu,

Liu

et al. 2023

Phytotherapy Research

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Ischemic stroke (IS) remains one of the leading causes of death and disability in humans. Unfortunately, none of the treatments effectively provide functional benefits to patients with IS, although many do so by targeting different aspects of the ischemic cascade response. The advantages of traditional Chinese medicine (TCM) in preventing and treating IS are obvious in terms of early treatment and global coordination. The efficacy of TCM and its bioactive constituents has been scientifically proven over the past decades. Based on clinical trials, this article provides a review of commonly used TCM patent medicines and herbal decoctions indicated for IS. In addition, this paper also reviews the mechanisms of bioactive constituents in TCM for the treatment of IS in recent years, both domestically and internationally. A comprehensive review of preclinical and clinical studies will hopefully provide new ideas to address the threat of IS.

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Section: Ameliorative Effect Of Tcm Formulas On Ismentioning

confidence: 99%

Traditional Chinese medicines treat ischemic stroke and their main bioactive constituents and mechanisms

Fan,

Liu,

Liu

et al. 2023

Phytotherapy Research

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“…However, because of low lipid solubility, the ability of Salvianic acid A to penetrate the BBB alone is limited. Therefore, most existing studies use a synthetic Salvianic acid A carrier system or derivatives to improve the BBB penetration rate of Salvianic acid A and increase the effective concentration of the drug to promote the therapeutic effects of the drug ( Li et al, 2023 ) 18.…”

Section: Protective Effects Of Salvianic Acid a Against Cerebral I/r ...mentioning

confidence: 99%

Protective effects of Salvianic acid A against multiple-organ ischemia-reperfusion injury: a review

Yang,

Chen,

et al. 2023

Front. Pharmacol.

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Ischemia-reperfusion (I/R) injury refers to a new injury caused by reperfusion after the restoration of ischemic tissue or organ blood supply. Salvianic acid A (danshensu) is a primary active ingredient extracted from Salvia miltiorrhiza. It has a protective function against I/R injury in the cardiovascular system, brain, liver, kidney, gastrointestinal tract, and other organs. This article reviews evidence of the protective effects of Salvianic acid A and its potential mechanisms of action in organ I/R injury protection. The aim of this review is to investigate the role of Salvianic acid A in the treatment of I/R injury, providing a reference resource that could facilitate subsequent studies.

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“…Since 2011, salvianolic acid injection was approved by the Chinese Food and Drug Administration for treating ischemic stroke in clinics . Danshensu (DSS) is one of the main components of salvianolic acid injection; DSS has attracted significant attention owing to its excellent ROS clearance and inflammation-regulation functions. , However, the strong water solubility and inherent small-molecule properties of DSS considerably hinder it from entering the brain. Therefore, nanodelivery technology must be chosen to effectively target and deliver DSS to the brain.…”

Section: Introductionmentioning

confidence: 99%

Nanocarriers Loaded with Danshensu for Treating Ischemic Stroke by Reducing Oxidative Stress and Glial Overactivation

Wang,

Xiao,

Fan

et al. 2024

ACS Omega

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Ischemic stroke is a complex health condition that can cause ischemia and necrosis of brain tissue. Subsequently, the excessive activation of glial cells can result in various inflammatory and oxidative stress reactions that exacerbate ischemic brain injury. In this paper, we propose the targeted selfassembly of a three-dimensional nanoparticle network containing Danshensu to rescue ischemic penumbra by reducing oxidative stress and glial overactivation. The network comprises nanoparticles composed of chitosan, thiol ketone, and carboxymethyl-β-cyclodextrin as the core wrapped by the Pro−His−Ser−Arg− Asn (PHSRN) peptide sequence as the outer layer and loaded with Danshensu. The PHSRN-peptide-modified nanoparticles bind to integrin α5β1 overexpressed on the damaged blood−brain barrier and accumulate in the damaged brain in a rat model of ischemia/reperfusion. When stimulated by reactive oxygen species, thiol ketone bonded to the nanoparticles was hydrolyzed, facilitating responsive drug release while consuming the reactive oxygen species. Subsequently, the released Danshensu scavenged the reactive oxygen species to prevent oxidative stress and inhibited the activation of astrocytes, thereby suppressing proinflammatory cytokine secretion, improving the inflammatory brain microenvironment and reducing neuronal apoptosis.

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Discovery of novel danshensu derivatives bearing pyrazolone moiety as potential anti-ischemic stroke agents with antioxidant activity

Cited by 8 publications

References 48 publications

Traditional Chinese medicines treat ischemic stroke and their main bioactive constituents and mechanisms

Traditional Chinese medicines treat ischemic stroke and their main bioactive constituents and mechanisms

Protective effects of Salvianic acid A against multiple-organ ischemia-reperfusion injury: a review

Nanocarriers Loaded with Danshensu for Treating Ischemic Stroke by Reducing Oxidative Stress and Glial Overactivation

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