In vitro and in vivo evaluation of cnicin from blessed thistle (Centaurea benedicta) and its inclusion complexes with cyclodextrins against Schistosoma mansoni

Queiroz, Lucas Sales; Ferreira, Everton Allan; Mengarda, Ana C.; Almeida, Ayla das Chagas; Pinto, Priscila de Faria; Coimbra, Elaine Soares; Moraes, Josué de; Denadai, Ângelo Márcio Leite; Filho, Ademar Alves da Silva

doi:10.1007/s00436-020-06963-2

Cited by 15 publications

(12 citation statements)

References 59 publications

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“…The oogram consists of one of the most relevant parameters to demonstrate the efficacy of a schistosomicidal compound [8,23–25] . Additionally, the main lesions caused by S. mansoni to the organism are due to the presence of eggs in the tissues of the host, triggering inflammatory reactions and the formation of granulomas [5,8,23–25] .…”

Section: Resultsmentioning

confidence: 99%

Cardamonin Presents in Vivo Activity against Schistosoma mansoni and Inhibits Potato Apyrase

Carvalho

Silva

Souza

et al. 2021

Chemistry & Biodiversity

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Schistosomiasis, a neglected tropical disease caused by Schistosoma species, harms over 250 million people in several countries. The treatment is achieved with only one drug, praziquantel. Cardamonin, a natural chalcone with in vitro schistosomicidal activity, has not been in vivo evaluated against Schistosoma. In this work, we evaluated the in vivo schistosomicidal activities of cardamonin against Schistosoma mansoni worms and conducted enzymatic apyrase inhibition assay, as well as molecular docking analysis of cardamonin against potato apyrase, S. mansoni NTPDase 1 and S. mansoni NTPDase 2. In a mouse model of schistosomiasis, the oral treatment with cardamonin (400 mg/kg) showed efficacy against S. mansoni, decreasing the total worm load in 46.8 % and reducing in 54.5 % the number of eggs in mice. Cardamonin achieved a significant inhibition of the apyrase activity and the three‐dimensional structure of the potato apyrase, obtained by homology modeling, showed that cardamonin may interact mainly through hydrogen bonds. Molecular docking studies corroborate with the action of cardamonin in binding and inhibiting both potato apyrase and S. mansoni NTPDases.

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Section: Resultsmentioning

confidence: 99%

Cardamonin Presents in Vivo Activity against Schistosoma mansoni and Inhibits Potato Apyrase

Carvalho

Silva

Souza

et al. 2021

Chemistry & Biodiversity

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“…It has also exhibited antimicrobial and anti-inflammatory activities in previous in vitro and in vivo studies [ 14 ]. Cnicin is one of the major chemical constituents of Blessed thistle, and it was proven to exhibit a broad antimicrobial activity (e.g., antiparasitic toward Schistosoma mansoni and antibacterial) [ 47 , 48 ], but it is not an FDA-approved drug. C. benedictus is generally considered safe, and it is used as a component in Benedictine liqueur™ in the USA [ 14 ].…”

Section: Discussionmentioning

confidence: 99%

Cnicin as an Anti-SARS-CoV-2: An Integrated In Silico and In Vitro Approach for the Rapid Identification of Potential COVID-19 Therapeutics

et al. 2021

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Since the emergence of the SARS-CoV-2 pandemic in 2019, it has remained a significant global threat, especially with the newly evolved variants. Despite the presence of different COVID-19 vaccines, the discovery of proper antiviral therapeutics is an urgent necessity. Nature is considered as a historical trove for drug discovery, especially in global crises. During our efforts to discover potential anti-SARS CoV-2 natural therapeutics, screening our in-house natural products and plant crude extracts library led to the identification of C. benedictus extract as a promising candidate. To find out the main chemical constituents responsible for the extract’s antiviral activity, we utilized recently reported SARS CoV-2 structural information in comprehensive in silico investigations (e.g., ensemble docking and physics-based molecular modeling). As a result, we constructed protein–protein and protein–compound interaction networks that suggest cnicin as the most promising anti-SARS CoV-2 hit that might inhibit viral multi-targets. The subsequent in vitro validation confirmed that cnicin could impede the viral replication of SARS CoV-2 in a dose-dependent manner, with an IC50 value of 1.18 µg/mL. Furthermore, drug-like property calculations strongly recommended cnicin for further in vivo and clinical experiments. The present investigation highlighted natural products as crucial and readily available sources for developing antiviral therapeutics. Additionally, it revealed the key contributions of bioinformatics and computer-aided modeling tools in accelerating the discovery rate of potential therapeutics, particularly in emergency times like the current COVID-19 pandemic.

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“…Rinsed leaves of C. benedicta L. (ECB) were extracted with dichloromethane:ethanol (9:1 v/v). Isolation and identification of CNI followed previously described methods (Queiroz et al 2021). The purity of cnicin was estimated to be greater than 95% by HPLC-DAD analysis (Queiroz et al 2021).…”

Section: Plant Materialsmentioning

confidence: 99%

“…1) is a sesquiterpene lactone identified from the genus Centaurea (Mizuno and Usuki 2018). This compound shows allelopathic, antibacterial, cytotoxic, anti-myeloma, schistosomicidal, and cytostatic potential (Al-Snafi 2016; Bach et al 2011;Queiroz et al 2021). Cnicin induced cytotoxicity in human macrophages (Bach et al 2011) and epithelial cells (LLC-PK1), human malignant melanoma (SK-MEL), and human ductal carcinoma (BT-549) (Erel et al 2011).…”

Section: Introductionmentioning

confidence: 99%

Cnicin from Centaurea benedicta L. is an active compound against skin inflammation in a mouse model

Sousa

Gonçalves

Queiroz

et al. 2021

Preprint

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Centaurea benedicta L., commonly known as “cardo santo,” is used as a tonic, antidepressant, anti-inflammatory, antibacterial, and antiseptic in traditional medicine. This study evaluated the topical anti-inflammatory potential of an extract (ECB) and cnicin (CNI) from C. benedicta leaves in a mouse model. Activity was assessed using the ear edema method with croton oil, phenol, capsaicin, and histamine as phlogistic agents. Myeloperoxidase (MPO), N-acetyl-β-D-glucosaminidase (NAG), nitric oxide (NO), t umor necrosis factor α (TNF-α), interleukin 6 (IL-6), and histopathology were assessed as markers of edema/inflammation. Interaction profiles between CNI and cyclooxygenase-1 and -2, induced nitric oxide synthase, and glucocorticoid receptor were examined with molecular docking. Twenty-four h after induction of inflammation, ECB and CNI treatments decreased the thickness and weight of ears by 39.59%– 94.72%. MPO, NAG, NO, TNF-α, and IL-6 levels were also reduced. Histopathological, treatments reduced edema thickness, leukocytes, and vasodilation. Inflammation induced by phenol and histamine was inhibited by ECB and CNI, and ECB suppressed capsaicin-induced inflammation. CNI interacts with cyclooxygenase-1 and nitric oxide synthase through conventional hydrogen bonds, indicating inhibition of these enzymes. ECB and its compound cnicin reduce chemically-induced inflammation in mice suggesting new possibilities for the treatment of diseases associated with dermal inflammatory processes.

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In vitro and in vivo evaluation of cnicin from blessed thistle (Centaurea benedicta) and its inclusion complexes with cyclodextrins against Schistosoma mansoni

Cited by 15 publications

References 59 publications

Cardamonin Presents in Vivo Activity against Schistosoma mansoni and Inhibits Potato Apyrase

Cardamonin Presents in Vivo Activity against Schistosoma mansoni and Inhibits Potato Apyrase

Cnicin as an Anti-SARS-CoV-2: An Integrated In Silico and In Vitro Approach for the Rapid Identification of Potential COVID-19 Therapeutics

Cnicin from Centaurea benedicta L. is an active compound against skin inflammation in a mouse model

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