Anti-inflammatory Ingenane Diterpenoids from the Roots of Euphorbia kansui

Zhang, Jun‐Sheng; Weng, Han-Zhuang; Huang, Jia-Luo; Yin, Sheng

doi:10.1055/a-0646-4306

Cited by 21 publications

(9 citation statements)

References 28 publications

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“…Additionally, 50% ethanolic extract of persimmon leaves potently inhibited the production of NO • , PGE 2 and IL-6 in LPS-induced RAW264.7 cells [32]. Likewise, the ethanolic extract of the Euphorbia kansui root containing ingenane diterpenoids (euphorkans A and B), together with 16 known analogues, exerted an anti-inflammatory activity that was consistent with Q by inhibiting the effects of certain inflammation mediators, such as TNF-α and IL-6, in a concentration-dependent manner through the inhibition of NF-κB activity [33]. Moreover, the ethanolic extract of the QingX-iaoWuWei decoction, containing quercetin and other ingredients, exhibited synergistic anti-inflammatory activity in the LPS-induced RAW264.7 cell culture via JUN, MAPK1 and AKT1 targets and the mitogen-activated protein kinases (MAPK)/phosphatidylinositol-3 kinase (PI3K)/Akt serine/threonine kinases pathways [34].…”

Section: Discussionmentioning

confidence: 86%

Quercetin-Rich Ethanolic Extract of Polygonum odoratum var Pakphai Leaves Decreased Gene Expression and Secretion of Pro-Inflammatory Mediators in Lipopolysaccharide-Induced Murine RAW264.7 Macrophages

et al. 2022

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Polygonum odoratum var. Pakphai has been used in traditional Thai medicine for the treatment of flatulence and constipation and to relieve the inflammation caused by insect bites. Quercetin (Q), which is abundant in plant-based foods, has been found to exert anti-inflammatory properties. This study evaluated the anti-inflammatory activity of P. odoratum ethanolic extract in RAW264.7 macrophage cells. Leaves were extracted with 50% ethanol, phenolics and flavonoids were then analyzed using UHPLC-QTOF-MS and HPLC-DAD. RAW264.7 cells were induced with lipopolysaccharides (LPSs). They were then treated with the extract and prostaglandin E2 (PGE2), and interleukin-6 (IL-6) and tumor necrotic factor-alpha (TNF-α) concentrations were determined. Levels of cyclooxygenase-2 (COX-2), inducible nitric oxide synthase (iNOS), IL-6 and TNF-α mRNAs were analyzed using qRT-PCR. Chemical analysis demonstrated that the extract was abundant with Q while also containing catechin, gallic acid, epicatechin gallate and coumarin. The extract increased the viability of RAW264.7 cells and dose-dependently decreased nitric oxide production, PGE2, IL-6 and TNF-α levels in the medium from the LPS-induced RAW264.7 cell culture. Consistently, COX-2, iNOS, IL-6 and TNF-α mRNA levels were decreased in a concentration-dependent manner (p < 0.05). Thus, the quercetin-rich ethanolic extract derived from P. odoratum var Pakphai leaves can exert anti-inflammatory activity in LPS-induced RAW264.7 cells through a reduction of the pro-inflammatory mediator response.

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Section: Discussionmentioning

confidence: 86%

Quercetin-Rich Ethanolic Extract of Polygonum odoratum var Pakphai Leaves Decreased Gene Expression and Secretion of Pro-Inflammatory Mediators in Lipopolysaccharide-Induced Murine RAW264.7 Macrophages

et al. 2022

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“…Therein, 11 compounds are ingenane-type and jastrophane-type diterpenoids and triterpenoids. Modern pharmacological study showed that kansuiphorin B and kansuinin A that belong to the ingenane-type and jastrophane-type diterpenoids, respectively, could inhibit NF-kB activity to exert anti-inflammatory activity in RAW264.7 macrophage cells based on a bioassay-guided separation [64].…”

Section: Resultsmentioning

confidence: 99%

Interpretation of Euphorbia Kansui Stir-Fried with Vinegar Treating Malignant Ascites by a UPLC-Q-TOF/MS Based Rat Serum and Urine Metabolomics Strategy Coupled with Network Pharmacology

Zhang

Wang

et al. 2018

Molecules

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Euphorbia kansui stir-fried with vinegar (V-kansui) has promising biological activities toward treating malignant ascites with reduced toxicity compared to crude kansui. But the mechanism concerning promoting the excretion of ascites has not been systematically studied. The purpose of this paper was to investigate the possible mechanism of V-kansui in treating malignant ascites, including metabolic pathways and molecular mechanism using an integrated serum and urine metabolomics coupled with network pharmacology. Serum and urine samples of rats were collected and analyzed by ultra-high-performance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry (UPLC-Q-TOF/MS). A comparison with crude kansui was also made to demonstrate the feasibility of processing. Principle component analysis (PCA) and orthogonal partial least square discriminate analysis (OPLS-DA) were conducted to discriminate the groups, search important variables and reveal the possible pathways. A compound-target-metabolite network was finally constructed to identify the crucial targets to further understand the molecular mechanism. Sixteen significant metabolites contributing to the discrimination of model and control groups were tentatively screened out. They were mainly involved in the arachidonic acid metabolism, steroid hormone biosynthesis and primary bile acid to possibly reduce inflammatory and modulate the renin-angiotensin-aldosterone system to achieve treating malignant ascites. A bio-network starting from the compounds and ending in the metabolites was constructed to elucidate the molecular mechanism. HSP90AA1, ANXA2, PRDX6, PCNA, SOD2 and ALB were identified as the potential key targets that were responsible for the treatment of malignant ascites by the parameter combining the average shortest path length and betweenness centrality. The correlated 17 compounds were considered as the potential active ingredients in V-kansui. In addition, the metabolomics showed that the effect of V-kansui was almost in accordance with crude kansui. These results systematically revealed the mechanism of V-kansui against malignant ascites for the first time using metabolomics coupled with network pharmacology. V-kansui could be a promising safe and therapeutic medicine for the excretion of ascites.

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“…It can relieve pleural effusion, ascites and urine retention. 1 Besides, modern pharmacology experiments have indicated that Kansui also has attractive pharmacological usage, such as anticancer, 2,3 antivirus, 4 anti-inflammatory, 5 antiallergic 6 and antiasthma 7 activities.…”

Section: Introductionmentioning

confidence: 99%

Detoxification mechanism of vinegar‐processed Kansui revealed by systematic phytochemical analysis using ultrahigh‐performance liquid chromatography diode array detection tandem mass spectrometry, ultrahigh‐performance liquid chromatography high‐resolution mass spectrometry and in silico drug target identification

Lian

Lv³

et al. 2022

Rapid Comm Mass Spectrometry

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Rationale The dried roots of Euphorbia kansui L., known as Kansui, are used to treat ascites and edema in traditional Chinese medicine. However, the toxicity of this herb has seriously restricted its clinical application. A unique vinegar‐processing method has been used to reduce its toxicity since the time of ancient China. However, the detoxification mechanism underlying such vinegar processing has not been fully revealed. To find the answer, the process‐induced changes in components should be carefully investigated. Methods We performed a systematic analysis of chemical components in raw and vinegar‐processed Kansui using ultrahigh‐performance liquid chromatography (UHPLC) diode array detection tandem mass spectrometry and UHPLC high‐resolution mass spectrometry. Thirty‐one chemical components in raw and vinegar‐processed Kansui were found, the chemical structures of 28 components among them were proposed and the process‐induced changes in components were then investigated. Results A comprehensive conclusion about the process‐induced chemical change was drawn. It was found that jatrophane‐type diterpenoids decreased markedly after vinegar processing, while ingenane‐type diterpenoids were retained during vinegar processing. In silico drug target identification gave hints that jatrophane‐type diterpenoids, which decreased markedly during vinegar processing, may have more intense toxicity involving cholinesterase and mitogen‐activated protein kinases, while ingenane‐type diterpenoids, which were retained during vinegar processing, may have a more intense therapeutic effect involving carbonic anhydrase. Conclusions The possible detoxification mechanism of vinegar‐processed Kansui is presented. The research has significance for the therapeutic/toxic chemical basis of Kansui. Also, it has significance for drug discovery from terpenoids within the herb.

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Anti-inflammatory Ingenane Diterpenoids from the Roots of Euphorbia kansui

Cited by 21 publications

References 28 publications

Quercetin-Rich Ethanolic Extract of Polygonum odoratum var Pakphai Leaves Decreased Gene Expression and Secretion of Pro-Inflammatory Mediators in Lipopolysaccharide-Induced Murine RAW264.7 Macrophages

Quercetin-Rich Ethanolic Extract of Polygonum odoratum var Pakphai Leaves Decreased Gene Expression and Secretion of Pro-Inflammatory Mediators in Lipopolysaccharide-Induced Murine RAW264.7 Macrophages

Interpretation of Euphorbia Kansui Stir-Fried with Vinegar Treating Malignant Ascites by a UPLC-Q-TOF/MS Based Rat Serum and Urine Metabolomics Strategy Coupled with Network Pharmacology

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