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15 pages, 2163 KiB

Open AccessArticle

Anti-Inflammatory Activity of Two Labdane Enantiomers from Gymnosperma glutinosum: An In Vivo, In Vitro, and In Silico Study

by Salud Pérez-Gutiérrez, Nimsi Campos-Xolalpa, Sofía A. Estrada-Barajas, Alan Carrasco-Carballo, Angel Mendoza and Ernesto Sánchez-Mendoza

Pharmaceuticals 2025, 18(4), 516; https://doi.org/10.3390/ph18040516 - 1 Apr 2025

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Abstract

Background/Objectives: Diseases associated with inflammatory processes continue to grow steadily throughout the world. Unfortunately, prolonged use of drugs induces adverse effects ranging from hypersensitivity reactions to damage to the digestive system. These negative effects open the possibility of continuing the search for [...] Read more.

Background/Objectives: Diseases associated with inflammatory processes continue to grow steadily throughout the world. Unfortunately, prolonged use of drugs induces adverse effects ranging from hypersensitivity reactions to damage to the digestive system. These negative effects open the possibility of continuing the search for anti-inflammatory compounds with less toxicity. The aim of this research was to isolate and evaluate the anti-inflammatory activity of a mixture of two enantiomeric labdanes isolated from Gymnosperma glutinosum by in vivo, in vitro, and in silico methods. Methods: A brief description of the main methods or treatments applied. This can include any relevant preregistration or specimen information. The structure of the labdanes enantiomers was elucidated by X-ray crystallography and spectroscopies methods. The anti-inflammatory effect was evaluated on a mouse model of ear edema induced with 12-O-tetradecanoyl phorbol-13-acetate; the pro-inflammatory mediators, nitric oxide (NO) and interleukin (IL-6), were quantified on macrophages stimulated with lipopolysaccharide, and the interaction between labdanes and diana was studied by molecular docking. Results: We identified the chemical structures of two new labdane enantiomers: a-gymglu acid and b-ent-gymglu acid. The enantiomer mixture, named gymglu acid, diminished ear edema at doses of 1 and 2 mg/ear by 36.07% and 41.99%, respectively. A concentration of 155.16 µM of gymglu acid inhibited the production of NO by 78.06% and IL-6 by 71.04%. The in silico results suggest two routes by which these labdanes reduce inflammation: partial agonism toward the corticosteroid receptors and inhibition of nitric oxide synthases. Conclusions: These results show that the gymglu acid enantiomers have promising anti-inflammatory activity. Full article

(This article belongs to the Special Issue Bioactive Compounds Derived from Plants and Their Medicinal Potential)

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26 pages, 11396 KiB

Open AccessArticle

Kaempferol Mitigates Pseudomonas aeruginosa-Induced Acute Lung Inflammation Through Suppressing GSK3β/JNK/c-Jun Signaling Pathway and NF-κB Activation

by Jue Wang, Linlin Zhang, Lu Fu and Zheng Pang

Pharmaceuticals 2025, 18(3), 322; https://doi.org/10.3390/ph18030322 - 25 Feb 2025

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Abstract

Background: Pseudomonas aeruginosa, one of the common bacterial pathogens causing nosocomial pneumonia, is characterized as highly pathogenic and multidrug-resistant. Kaempferol (KP), a natural flavonoid, has been shown to exhibit effectiveness in treating infection-induced lung injury. Methods: We applied network pharmacology to explore [...] Read more.

Background: Pseudomonas aeruginosa, one of the common bacterial pathogens causing nosocomial pneumonia, is characterized as highly pathogenic and multidrug-resistant. Kaempferol (KP), a natural flavonoid, has been shown to exhibit effectiveness in treating infection-induced lung injury. Methods: We applied network pharmacology to explore the underlying mechanisms of KP in treating P. aeruginosa pneumonia and further validated them through a mouse model of acute bacterial lung infection and an in vitro macrophage infection model. Results: The in vivo studies demonstrated that treatment with KP suppressed the production of proinflammatory cytokines, including TNF, IL-1β, IL-6, and MIP-2, and attenuated the neutrophil infiltration and lesions in lungs, leading to an increased survival rate of mice. Further studies revealed that KP treatment enhanced the phosphorylation of GSK3β at Ser9 and diminished the phosphorylation of JNK, c-Jun, and NF-κB p65 in lungs in comparison to the mice without drug treatment. Consistently, the in vitro studies showed that pretreatment with KP reduced the activation of GSK3β, JNK, c-Jun, and NF-κB p65 and decreased the levels of the proinflammatory cytokines in macrophages during P. aeruginosa infection. Conclusions: KP reduced the production of proinflammatory cytokines by inhibiting GSK3β/JNK/c-Jun signaling pathways and NF-κB activation, which effectively mitigated the P. aeruginosa-induced acute lung inflammation and injury, and elevated the survival rates of mice. Full article

(This article belongs to the Special Issue Bioactive Compounds Derived from Plants and Their Medicinal Potential)

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16 pages, 2361 KiB

Open AccessArticle

Potential of Newly Synthesized Sea Buckthorn Phytocarriers as Anti-Inflammatory Active Agents

by Ionela Daniela Popescu, Elena Codrici, Sevinci Pop, Tudor Emanuel Fertig, Maria Dudău, Iliuta Laurentiu Anghelache, Nicoleta Constantin, Radu Marian Marinescu, Vlad Mihai Voiculescu, Georgiana Ileana Badea, Mirela Diaconu, Monica Elisabeta Maxim, Mihaela Scurtu, Kliment Zanov, Ana-Maria Enciu, Simona Carmen Litescu and Cristiana Tanase

Pharmaceuticals 2025, 18(2), 212; https://doi.org/10.3390/ph18020212 - 5 Feb 2025

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Abstract

Background: Phytocarriers are advanced drug delivery systems that use biocompatible and biodegradable materials to enhance the efficacy, stability, and bioavailability of natural products. The sea buckthorn (Hippophae rhamnoides L.) berry extract is rich in essential fatty acids and antioxidants, including vitamin C, [...] Read more.

Background: Phytocarriers are advanced drug delivery systems that use biocompatible and biodegradable materials to enhance the efficacy, stability, and bioavailability of natural products. The sea buckthorn (Hippophae rhamnoides L.) berry extract is rich in essential fatty acids and antioxidants, including vitamin C, vitamin E, and anthocyanins, which contribute to its wide-ranging health benefits. In this study, we assessed the morphology, intracellular delivery, and anti-inflammatory effect of sodium cholate (NaC) and sodium deoxycholate (NaDC)-based phytocarriers loaded with ethanolic extract from sea buckthorn berries (sea buckthorn carrier nanostructures, further defined as phytocarriers). Methods: Negative and electron cryo-microscopy were used to analyze hollow and loaded nanocarriers. The cyto-compatibility of nanocarriers was assessed by endpoint (LDH and MTS) and real-time cell assays, on both human fibroblasts (HS27) and human normal monocytes (SC). The anti-inflammatory effect of hollow and loaded nanocarriers was tested by multiplexing. Results: The negative and electron cryo-microscopy analyses showed that NaC-based phytocarriers were spherical, whilst NaDC-based phytocarriers were predominantly polymorphic. Moreover, the NaDC-based phytocarriers frequently formed large lipid networks or “plaques”. Although 24 h cytotoxicity testing showed both types of nanocarriers are biocompatible with human fibroblasts and monocytes, based on a long-term real-time assay, NaDC delayed fibroblast proliferation. NaC sea buckthorn phytocarriers did not impair fibroblast proliferation in the long term and they were uptaken by cells, as shown by hyperspectral microscopy. NaC nanocarriers and NaC sea buckthorn phytocarriers induced an anti-inflammatory effect, lowering IL-8 cytokine production in normal human monocytes as soon as 4 h of treatment lapsed. Conclusions: NaC-derived phytocarriers loaded with sea buckthorn alcoholic extract are a cell-compatible delivery system with anti-inflammatory properties. Full article

(This article belongs to the Special Issue Bioactive Compounds Derived from Plants and Their Medicinal Potential)

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19 pages, 1274 KiB

Open AccessArticle

Protective Effects of Phycobiliproteins from Arthrospira maxima (Spirulina) Against Cyclophosphamide-Induced Embryotoxicity and Genotoxicity in Pregnant CD1 Mice

by Yuliana García-Martínez, Amparo Celene Razo-Estrada, Ricardo Pérez-Pastén-Borja, Candelaria Galván-Colorado, Germán Chamorro-Cevallos, José Jorge Chanona-Pérez, Oscar Alberto López-Canales, Hariz Islas-Flores, Salud Pérez-Gutiérrez, Joaquín Cordero-Martínez and José Melesio Cristóbal-Luna

Pharmaceuticals 2025, 18(1), 101; https://doi.org/10.3390/ph18010101 - 15 Jan 2025

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Abstract

Background/Objectives: In recent years the global incidence of cancer during pregnancy is rising, occurring in 1 out of every 1000 pregnancies. In this regard, the most used chemotherapy drugs to treat cancer are alkylating agents such as cyclophosphamide (Cp). Despite its great [...] Read more.

Background/Objectives: In recent years the global incidence of cancer during pregnancy is rising, occurring in 1 out of every 1000 pregnancies. In this regard, the most used chemotherapy drugs to treat cancer are alkylating agents such as cyclophosphamide (Cp). Despite its great efficacy, has been associated with the production of oxidative stress and DNA damage, leading to embryotoxicity, genotoxicity, and teratogenicity in the developing conceptus. Therefore, this study aimed to investigate the protective role of phycobiliproteins (PBP) derived from Arthrospira maxima (spirulina) in reducing Cp-induced embryotoxicity and genotoxicity in pregnant CD1 mice. Methods: Pregnant CD1 mice were divided into five groups: control, Cp 20 mg/kg, and three doses of PBP (50, 100, and 200 mg/kg) + Cp co-treatment. PBP were administered orally from day 6 to 10.5 dpc, followed by a single intraperitoneal dose of Cp on 10.5 dpc. Embryos were collected at 12.5 dpc to assess morphological development and vascular alterations, while maternal DNA damage was evaluated using micronucleus assays and antioxidant enzyme activity in maternal plasma. Results: PBP exhibited a dose-dependent protective effect against Cp-induced damage. The 200 mg/kg PBP dose significantly reduced developmental abnormalities, micronucleated polychromatic erythrocytes, and oxidative stress, (as evidenced by increased SOD and GPx activity). Conclusions: Phycobiliproteins from Arthrospira maxima (spirulina) effectively reduced Cp-induced morphological and vascular alterations in embryos and genotoxicity in pregnant mice. These findings highlight their potential as a complementary therapy to mitigate teratogenic risks during chemotherapy. Further research is needed to optimize dosing and explore clinical applications. Full article

(This article belongs to the Special Issue Bioactive Compounds Derived from Plants and Their Medicinal Potential)

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24 pages, 5776 KiB

Open AccessArticle

Garcinia brasiliensis Leaves Extracts Inhibit the Development of Ascitic and Solid Ehrlich Tumors

by Lucas Sylvestre Silva, Eduardo Cavallini, Rafael André da Silva, Monielle Sant’Ana, Ariane Harumi Yoshikawa, Thiago Salomão, Bianca Huang, Paula Craice, Luiz Philipe de Souza Ferreira, Heitor Pedro Della Matta, Cristiane Damas Gil, Maria de Lourdes Gomes Pereira and Ana Paula Girol

Pharmaceuticals 2025, 18(1), 24; https://doi.org/10.3390/ph18010024 - 28 Dec 2024

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Abstract

Background: Garcinia brasiliensis is traditionally known for its medicinal properties. Objectives: Here, we investigated the effects of crude extract (CE) and ethyl acetate fraction (EAF) obtained from G. brasiliensis leaves on the ascitic (EA) and solid (ES) forms of Ehrlich tumors. Methods [...] Read more.

Background: Garcinia brasiliensis is traditionally known for its medicinal properties. Objectives: Here, we investigated the effects of crude extract (CE) and ethyl acetate fraction (EAF) obtained from G. brasiliensis leaves on the ascitic (EA) and solid (ES) forms of Ehrlich tumors. Methods: Induced and uninduced BALB/c mice were treated intramuscularly, for 7 or 14 days, with saline solution or CE and EAF, both at a 10% concentration, based on in vitro cytotoxicity assessment. Biochemical analyses were also performed to evaluate in vivo cytotoxicity. In relation to tumor-induced animals, morphological changes, plasma enzymes, inflammatory mediators and the induction of apoptosis were analyzed, in addition to histopathological studies, to evaluate the inhibition of tumor growth. Results: Alanine aminotransferase (ALT), aspartate aminotransferase (AST) and gamma glutamyl transferase (GGT) were regulated by CE and EAF administration. Furthermore, both treatments were effective in inhibiting tumor growth in EA and ES by modulating the levels of interleukin (IL)-6 and tumor necrosis factor (TNF)-α, decreasing mast cells numbers and inducing apoptosis. Conclusions: This research indicates that both CE and EAF from G. brasiliensis leaves have potential antitumor effects with low cytotoxicity. Full article

(This article belongs to the Special Issue Bioactive Compounds Derived from Plants and Their Medicinal Potential)

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28 pages, 12654 KiB

Open AccessArticle

Investigating the Antibacterial, Antioxidant, and Anti-Inflammatory Properties of a Lycopene Selenium Nano-Formulation: An In Vitro and In Vivo Study

by Reem Binsuwaidan, Thanaa A. El-Masry, Maysa M. F. El-Nagar, Enas I. El Zahaby, Mohamed M. S. Gaballa and Maisra M. El-Bouseary

Pharmaceuticals 2024, 17(12), 1600; https://doi.org/10.3390/ph17121600 - 27 Nov 2024

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Abstract

Background: The potent antioxidant lycopene has attracted a large amount of research attention given its potential health benefits. We aimed to assess the antimicrobial, anti-inflammatory, and antioxidant properties of lycopene (Lyc), selenium nanoparticles (Se-NPs), and lycopene selenium nanoparticles (Lyc-Se-NPs). Methods: FTIR, polydispersity index, [...] Read more.

Background: The potent antioxidant lycopene has attracted a large amount of research attention given its potential health benefits. We aimed to assess the antimicrobial, anti-inflammatory, and antioxidant properties of lycopene (Lyc), selenium nanoparticles (Se-NPs), and lycopene selenium nanoparticles (Lyc-Se-NPs). Methods: FTIR, polydispersity index, and zeta potential evaluations provided a complete characterization of the synthesized Lyc-Se-NPs. The broth dilution method and a crystal violet microtiter plate assay were employed to assess the antibacterial and antibiofilm activity, respectively. The rat wound infection model was performed to study the anti-inflammatory effect. Findings: The Lyc-Se-NPs had a zeta potential range of −16.93 to −31.04 mV and a mean particle size of 126.6 ± 3.12 nm. All peaks’ percentage transmittance decreased, according to the FTIR analysis of the Lyc-Se-NPs, with the exception of one peak at 2924.22 cm⁻¹, which is suggestive of C-H stretching. The mean scavenging concentrations for Lyc-Se-NPs in the DPPH and ABTS radical scavenging experiments were 3.85 ± 0.65 and 4.26 ± 0.7 µg/mL, respectively. For S. aureus, the Lyc-Se-NPs’ MIC values varied from 64 to 1024 µg/mL. CLSM verified that S. aureus treated with sub-MICs of Lyc-Se-NPs showed a significant reduction in biofilm formation. Furthermore, the group treated with 50 mg of Lyc-Se-NPs showed the quickest rate of wound healing. They demonstrated a notable elevation of the HO⁻¹ content in skin tissues, together with the greatest downregulation of TNF-α, IL-1β, and COX-2. Conclusions: The distinguishing features of Lyc-Se-NPs reveal that this unique compound is a promising antibacterial, antioxidant, and anti-inflammatory agent. Full article

(This article belongs to the Special Issue Bioactive Compounds Derived from Plants and Their Medicinal Potential)

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17 pages, 2032 KiB

Open AccessArticle

Analgesic and Anti-Arthritic Potential of Methanolic Extract and Palmatine Obtained from Annona squamosa Leaves

by Caren Naomi Aguero Ito, Elisangela dos Santos Procopio, Natália de Matos Balsalobre, Lucas Luiz Machado, Saulo Euclides Silva-Filho, Taíse Fonseca Pedroso, Caroline Caramano de Lourenço, Rodrigo Juliano Oliveira, Arielle Cristina Arena, Marcos José Salvador and Cândida Aparecida Leite Kassuya

Pharmaceuticals 2024, 17(10), 1331; https://doi.org/10.3390/ph17101331 - 5 Oct 2024

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Abstract

Background/Objectives: Annona squamosa is used in folk medicine to treat pain and arthritis. Palmatine is an alkaloid isolated from several plants, including A. squamosa leaves. The aim of the present study was to investigate the analgesic, anti-arthritic, and anti-inflammatory potential of the [...] Read more.

Background/Objectives: Annona squamosa is used in folk medicine to treat pain and arthritis. Palmatine is an alkaloid isolated from several plants, including A. squamosa leaves. The aim of the present study was to investigate the analgesic, anti-arthritic, and anti-inflammatory potential of the methanolic extract of A. squamosa (EMAS) and palmatine. Methods: The chemical profile of EMAS was evaluated by ultra high-performance liquid chromatography with electrospray ionization coupled to mass spectrometry (UHPLC-ESI/MS). EMAS and palmatine were evaluated in carrageenan-induced pleurisy, zymosan-induced joint inflammation, formalin-induced nociception, and tumor necrosis factor (TNF)-induced mechanical hyperalgesia in experimental models in mice. A cytotoxicity test of EMAS and palmatine was performed using a methylthiazolidiphenyl-tetrazolium (MTT) bromide assay. Results: The analysis of the chemical profile of the extract showed the presence of palmatine, liriodenine, and anonaine. Oral administration of EMAS and palmatine significantly reduced leukocyte migration and oxide nitric production in the carrageenan-induced pleurisy model. EMAS and palmatine reduced mechanical hyperalgesia, leukocyte migration, and edema formation in the joint inflammation induced by zymosan. In the formalin test, palmatine was effective against the second-phase nociceptive response, mechanical hyperalgesia, and cold allodynia. In addition, palmatine reduced mechanical hyperalgesia induced by TNF. EMAS and palmatine did not demonstrate cytotoxicity. Conclusions: The present study showed that A. squamosa and palmatine are analgesic and anti-inflammatory agents, and that the anti-hyperalgesic properties of palmatine may involve the TNF pathway. Palmatine may be one of the compounds responsible for the anti-hyperalgesic and/or anti-arthritic properties of this medicinal plant. Full article

(This article belongs to the Special Issue Bioactive Compounds Derived from Plants and Their Medicinal Potential)

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13 pages, 1878 KiB

Open AccessArticle

The Anti-Arthritic Potential of the Ethanolic Extract of Salvia Lachnostachys Benth. Leaves and Icetexane Dinor-Diterpenoid Fruticuline B

by Natália de M. Balsalobre, Elisangela dos Santos-Procopio, Cristhian S. Oliveira, Silvia C. Neves, Maria H. Verdan, Saulo E. Silva-Filho, Rodrigo J. Oliveira, Maria É. A. Stefanello and Cândida A. L. Kassuya

Pharmaceuticals 2024, 17(9), 1226; https://doi.org/10.3390/ph17091226 - 18 Sep 2024

Cited by 1 | Viewed by 1251

Abstract

The decoction of Salvia lachnostachys Benth. leaves is used in Brazilian folk medicine for anti-spasmodic, antipyretic, and anxiolytic purposes. Some of the biological effects of an S. lachnostachys extract have been shown to be anti-inflammatory, anti-cancer, and antidepressant effects. In addition, this medicinal [...] Read more.

The decoction of Salvia lachnostachys Benth. leaves is used in Brazilian folk medicine for anti-spasmodic, antipyretic, and anxiolytic purposes. Some of the biological effects of an S. lachnostachys extract have been shown to be anti-inflammatory, anti-cancer, and antidepressant effects. In addition, this medicinal plant produces several compounds including icetexane diterpenoids, such as fruticuline A and fruticuline B. The aim of the present work was to evaluate the anti-hyperalgesic and anti-inflammatory properties of fruticuline B (FRUT B) and the ethanolic extract obtained from the leaves of S. lachnostachys (EESL) in experimental mouse models. EESL (30, 100, and 300 mg/kg) and FRUT B (1 mg/kg) were evaluated in articular inflammation-induced models in Swiss mice. In articular inflammation induced by Zymosan, EESL (300 mg/kg) and FRUT B (1 mg/kg) significantly reduced mechanical hyperalgesia (83.17% inhibition for EESL and 81.19% for FRUT B); edema (68.75% reduction for EESL and 33.66% for FRUT B); leukocyte migration (81.3% for EESSL and 92.2% for FRUT B), and nitric oxide production (88.3% for EESL and 74.4% for FRUT B). The exposure to fruticuline B significantly inhibited the edema (51.5%), mechanical (88.12%) and cold hyperalgesia (80.8%), and myeloperoxidase (MPO) (63.4%) activity 24 h after CFA injection. In the pleurisy model, FRUT B reduced 89.1% of leukocyte migration and 50.3% in nitric oxide production. Four hours after carrageenan injection, FRUT B (1 mg/kg) diminished 89.11% of mechanical hyperalgesia, 65.8% of paw edema, and 82.12% of the response to cold hyperalgesia. In the MTT test, EESL and fruticuline B caused no cytotoxicity. The present study revealed, for the first time, the anti-arthritic and anti-nociceptive effects of FRUT B, pointing out the therapeutic potential of the species to control inflammation and nociception. Future studies are needed to evaluate other biological properties of fruticuline B and to better understand its mechanism of action. Full article

(This article belongs to the Special Issue Bioactive Compounds Derived from Plants and Their Medicinal Potential)

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19 pages, 4126 KiB

Open AccessArticle

Thymol Protects against 5-Fluorouracil-Induced Hepatotoxicity via the Regulation of the Akt/GSK-3β Pathway in In Vivo and In Silico Experimental Models

by Yasmen F. Mahran, Amira M. Badr, Layla A. Al-Kharashi, Hanaa N. Alajami, Nouf T. Aldamry, Nervana Moustafa Bayoumy, Elshaymaa I. Elmongy and Sahar Soliman

Pharmaceuticals 2024, 17(8), 1094; https://doi.org/10.3390/ph17081094 - 21 Aug 2024

Cited by 1 | Viewed by 1746

Abstract

Background: 5-fluorouracil (5-FU) is a widely used, highly effective chemotherapeutic agent. However, its therapeutic efficacy is often limited by associated adverse effects, with hepatotoxicity being frequently reported with 5-FU therapy. Thymol is a monoterpene found in thyme (Thymus vulgaris L., Lamiaceae) and [...] Read more.

Background: 5-fluorouracil (5-FU) is a widely used, highly effective chemotherapeutic agent. However, its therapeutic efficacy is often limited by associated adverse effects, with hepatotoxicity being frequently reported with 5-FU therapy. Thymol is a monoterpene found in thyme (Thymus vulgaris L., Lamiaceae) and is known for its antioxidant, anti-apoptotic, and anticancer activities. This study aimed to explore the hepatoprotective activity of thymol against 5-FU-induced liver injury. Methods: Rats received two intraperitoneal doses of 5-FU (150 mg/kg) either alone or in combination with thymol at doses of 60 mg/kg or 120 mg/kg. Liver enzymes, oxidative stress, and apoptotic markers, in addition to histopathological changes, were assessed. Results: 5-FU induced marked liver injuries as evidenced by elevated liver enzymes and histopathological changes, in addition to abnormalities of oxidative and apoptotic markers. The administration of thymol ameliorated the 5-FU-induced oxidative damage through increasing hepatic antioxidants and lowering lipid peroxidation. Apoptotic response markers such as Bax, Bcl-2, Bax/Bcl-2 ratio, and PARP were also improved. Furthermore, Western blotting analysis showed that thymol modulated the 5-FU-induced changes in the expression of Akt/GSK-3β and p44/42 MAPK (ERK1/2) signaling pathways. Conclusions: Our research is the first to shed light on thymol’s potential protective effect against 5-FU- induced hepatotoxicity by inhibiting oxidative and apoptotic pathways and modulating the Akt/ GSK-3β as well as p44/42 MAPK (ERK1/2) signaling pathways. Full article

(This article belongs to the Special Issue Bioactive Compounds Derived from Plants and Their Medicinal Potential)

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22 pages, 3434 KiB

Open AccessArticle

Antinociceptive and Anti-Inflammatory Activities of Acetonic Extract from Bougainvillea x buttiana (var. Rose)

by Gabriela Castañeda-Corral, Mayra Cedillo-Cortezano, Magdalena Aviles-Flores, Misael López-Castillo, Juan José Acevedo-Fernández and Vera L. Petricevich

Pharmaceuticals 2024, 17(8), 1037; https://doi.org/10.3390/ph17081037 - 6 Aug 2024

Cited by 1 | Viewed by 1717

Abstract

Background:Bougainvillea x buttiana is an ornamental plant with antioxidant, anti-inflammatory, and cytotoxic activities, which has been traditionally used to treat respiratory diseases. This study aimed to investigate whether the acetonic extract of Bougainvillea x buttiana var. Rose (BxbRAE-100%) has analgesic and anti-inflammatory [...] Read more.

Background:Bougainvillea x buttiana is an ornamental plant with antioxidant, anti-inflammatory, and cytotoxic activities, which has been traditionally used to treat respiratory diseases. This study aimed to investigate whether the acetonic extract of Bougainvillea x buttiana var. Rose (BxbRAE-100%) has analgesic and anti-inflammatory properties and its potential action mechanisms. Methods: Analgesic and anti-inflammatory activities were evaluated using three murine pain models and two acute inflammation models. In vitro, the ability of the extract to inhibit proteolytic activity and the activities of the enzymes phospholipase A2 (PLA2) and cyclooxygenase (COX) were evaluated. In silico analysis was performed to predict the physicochemical and Absorption, distribution, metabolism, and excretion (ADME) profiles of the compounds previously identified in BxbRAE-100%. Results: In vivo BxbRAE-100% decreased the nociceptive behaviors in the writhing model, the tail immersion, and the formalin test, suggesting that the extract has the potential to relieve pain at peripheral and central levels. Additionally, topical or oral BxbRAE-100% treatment reduced dose-dependent 12-O-Tetradecanoylphorbol-13-acetate (TPA)-induced ear inflammation and carrageenan-induced paw edema, respectively. In vitro, BxbRAE-100% significantly inhibited proteolytic activity and PLA2, COX-1 and COX-2 activities. In silico, the compounds previously identified in BxbRAE-100% met Lipinski’s rule of five and showed adequate ADME properties. Conclusions: These results support the use of B. x buttiana in Traditional Mexican Medicine and highlight its potential for the development of new treatments for pain and inflammation. Full article

(This article belongs to the Special Issue Bioactive Compounds Derived from Plants and Their Medicinal Potential)

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19 pages, 11500 KiB

Open AccessArticle

Ethanolic Extracts of Cupressaceae Species Conifers Provide Rapid Protection against Barium Chloride-Induced Cardiac Arrhythmia

by Meng-Ting Zeng, Li-Yue Huang, Xiao-Hui Zheng, Yan-Qi Fu and Ching-Feng Weng

Pharmaceuticals 2024, 17(8), 1003; https://doi.org/10.3390/ph17081003 - 29 Jul 2024

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Abstract

Sudden cardiac death (SCD) is responsible for a high percentage of cardiovascular fatalities, with ventricular arrhythmias being the most common cause. Despite numerous clinically available antiarrhythmic drugs (AADs), AADs retain some undesirable arrhythmic effects, and their inappropriate use can lead to severe adverse [...] Read more.

Sudden cardiac death (SCD) is responsible for a high percentage of cardiovascular fatalities, with ventricular arrhythmias being the most common cause. Despite numerous clinically available antiarrhythmic drugs (AADs), AADs retain some undesirable arrhythmic effects, and their inappropriate use can lead to severe adverse reactions. The exploration of new therapeutic options against arrhythmias with fewer unreceptive effects is of utmost importance. The ethanolic extracts of seven Cupressaceae species, namely, Chamaecyparis obtusa, Juniperus chinensis (L.) Ant., Sabina chinensis (L.) Ant. cv. Kaizuca, Platycladus orientalis (L.) Franco, Juniperus sabina L., Fokienia hodginsii, and Juniperus chinensis ‘Pyramidalis’ were investigated for their pharmacological effects on barium chloride (BaCl₂)-induced arrhythmia using normal II lead electrocardiogram (ECG) measurements in a mouse model. According to the ECG profiles, pretreatment with C. obtusa, P. orientalis, and J. sabina extracts provoked dose-dependent protection against BaCl₂-induced arrhythmia, while pretreatment with the other four species and amiodarone did not exert cardioprotective effects. The treatment effects were confirmed using a rat model. The therapeutic effects of C. obtusa, P. orientalis, and J. sabina extracts on the M2 and M3 receptors but not the M1 receptor were mediated by the inhibition of the M2 receptor blocker (methoctramine tetrahydrochloride), M3 antagonist (4-DAMP), or M1 receptor blocker (pirenzepine dihydrochloride). This first-line evidence illustrates that certain Cupressaceae species possess active antiarrhythmic components. The first line of key findings revealed that active components of certain Cupressaceae species have cardioprotective effects, suggesting that these innovative phytochemicals have promising potential for preventing the occurrence of cardiac arrhythmia and reducing sudden cardiac death. Full article

(This article belongs to the Special Issue Bioactive Compounds Derived from Plants and Their Medicinal Potential)

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22 pages, 7552 KiB

Open AccessArticle

Evaluation of Crocetin as a Protective Agent in High Altitude Hypoxia-Induced Organ Damage

by Jun Yang, Kai Luo, Ziliang Guo, Renjie Wang, Qingyuan Qian, Shuhe Ma, Maoxing Li and Yue Gao

Pharmaceuticals 2024, 17(8), 985; https://doi.org/10.3390/ph17080985 - 25 Jul 2024

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Abstract

Crocetin is an aglycone of crocin naturally occurring in saffron and has been proved to have antioxidant, anti-inflammatory, and antibacterial activities. In this experiment, the protective effect of crocetin on vital organs in high-altitude hypoxia rats was studied. Crocetin was prepared from gardenia [...] Read more.

Crocetin is an aglycone of crocin naturally occurring in saffron and has been proved to have antioxidant, anti-inflammatory, and antibacterial activities. In this experiment, the protective effect of crocetin on vital organs in high-altitude hypoxia rats was studied. Crocetin was prepared from gardenia by the alkaline hydrolysis method, and its reducing ability and free radical scavenging ability were tested. The in vitro anti-hypoxia vitality was studied on PC₁₂ cells. The anti-hypoxic survival time of mice was determined in several models. The acute hypoxic injury rat model was established by simulating the hypoxic environment of 8000 m-high altitude for 24 h, and the anti-hypoxia effect of crocetin was evaluated by intraperitoneal injection with the doses of 10, 20, and 40 mg/kg. The water contents of the brain and lung were determined, and the pathological sections in the brain, lung, heart, liver, and kidney were observed by HE staining. The levels of oxidative stress (SOD, CAT, H₂O₂, GSH, GSH-Px, MDA) and inflammatory factors (IL-1β, IL-6, TNF-α, VEGF) in rat brain, lung, heart, liver, and kidney tissues were detected by ELISA. The results indicated that crocetin exhibited strong reducing ability and free radical scavenging ability and could improve the activity of PC₁₂ cells under hypoxia. After intraperitoneal injection with crocetin, the survival time of mice was prolonged, and the pathological damage, oxidative stress, and inflammation in rats’ tissue were ameliorated. The protective activity of crocetin on vital organs in high-altitude hypoxia rats may be related to reducing oxidative stress and inhibiting inflammatory response. Full article

(This article belongs to the Special Issue Bioactive Compounds Derived from Plants and Their Medicinal Potential)

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Review

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30 pages, 3053 KiB

Open AccessReview

The Dynamic Role of Curcumin in Mitigating Human Illnesses: Recent Advances in Therapeutic Applications

by Md Shamshir Alam, Md Jamir Anwar, Manish Kumar Maity, Faizul Azam, Mariusz Jaremko and Abdul-Hamid Emwas

Pharmaceuticals 2024, 17(12), 1674; https://doi.org/10.3390/ph17121674 - 11 Dec 2024

Cited by 1 | Viewed by 2939

Abstract

Herbal medicine, particularly in developing regions, remains highly popular due to its cost-effectiveness, accessibility, and minimal risk of adverse effects. Curcuma longa L., commonly known as turmeric, exemplifies such herbal remedies with its extensive history of culinary and medicinal applications across Asia for [...] Read more.

Herbal medicine, particularly in developing regions, remains highly popular due to its cost-effectiveness, accessibility, and minimal risk of adverse effects. Curcuma longa L., commonly known as turmeric, exemplifies such herbal remedies with its extensive history of culinary and medicinal applications across Asia for thousands of years. Traditionally utilized as a dye, flavoring, and in cultural rituals, turmeric has also been employed to treat a spectrum of medical conditions, including inflammatory, bacterial, and fungal infections, jaundice, tumors, and ulcers. Building on this longstanding use, contemporary biochemical and clinical research has identified curcumin—the primary active compound in turmeric—as possessing significant therapeutic potential. This review hypothesizes that curcumin’s antioxidant properties are pivotal in preventing and treating chronic inflammatory diseases, which are often precursors to more severe conditions, such as cancer, and neurological disorders, like Parkinson’s and Alzheimer’s disease. Additionally, while curcumin demonstrates a favorable safety profile, its anticoagulant effects warrant cautious application. This article synthesizes recent studies to elucidate the molecular mechanisms underlying curcumin’s actions and evaluates its therapeutic efficacy in various human illnesses, including cancer, inflammatory bowel disease, osteoarthritis, atherosclerosis, peptic ulcers, COVID-19, psoriasis, vitiligo, and depression. By integrating diverse research findings, this review aims to provide a comprehensive perspective on curcumin’s role in modern medicine and its potential as a multifaceted therapeutic agent. Full article

(This article belongs to the Special Issue Bioactive Compounds Derived from Plants and Their Medicinal Potential)

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21 pages, 1438 KiB

Open AccessReview

Exploring the Comprehensive Neuroprotective and Anticancer Potential of Afzelin

by Mateusz Kciuk, Nitika Garg, Sanchit Dhankhar, Monika Saini, Somdutt Mujwar, Sushma Devi, Samrat Chauhan, Thakur Gurjeet Singh, Randhir Singh, Beata Marciniak, Adrianna Gielecińska and Renata Kontek

Pharmaceuticals 2024, 17(6), 701; https://doi.org/10.3390/ph17060701 - 28 May 2024

Cited by 5 | Viewed by 1811

Abstract

Neurodegenerative diseases (Alzheimer’s disease, Parkinson’s disease, Huntington’s disease, and others) and cancer, seemingly disparate in their etiology and manifestation, exhibit intriguing associations in certain cellular and molecular processes. Both cancer and neurodegenerative diseases involve the deregulation of cellular processes such as apoptosis, proliferation, [...] Read more.

Neurodegenerative diseases (Alzheimer’s disease, Parkinson’s disease, Huntington’s disease, and others) and cancer, seemingly disparate in their etiology and manifestation, exhibit intriguing associations in certain cellular and molecular processes. Both cancer and neurodegenerative diseases involve the deregulation of cellular processes such as apoptosis, proliferation, and DNA repair and pose a significant global health challenge. Afzelin (kaempferol 3-O-rhamnoside) is a flavonoid compound abundant in various plant sources. Afzelin exhibits a diverse range of biological activities, offering promising prospects for the treatment of diseases hallmarked by oxidative stress and deregulation of cell death pathways. Its protective potential against oxidative stress is also promising for alleviating the side effects of chemotherapy. This review explores the potential therapeutic implications of afzelin, including its capacity to mitigate oxidative stress, modulate inflammation, and promote cellular regeneration in neurodegenerative and cancer diseases. Full article

(This article belongs to the Special Issue Bioactive Compounds Derived from Plants and Their Medicinal Potential)

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15 pages, 2548 KiB

Open AccessSystematic Review

Unveiling the Neuroprotective Potential of Date Palm (Phoenix dactylifera): A Systematic Review

by Syed Mohammed Basheeruddin Asdaq, Abdulaziz Ali Almutiri, Abdullah Alenzi, Maheen Shaikh, Mujeeb Ahmed Shaik, Sultan Alshehri and Syed Imam Rabbani

Pharmaceuticals 2024, 17(9), 1221; https://doi.org/10.3390/ph17091221 - 17 Sep 2024

Viewed by 1882

Abstract

Background: Neurodegenerative diseases primarily afflict the elderly and are characterized by a progressive loss of neurons. Oxidative stress is intricately linked to the advancement of these conditions. This study focuses on Phoenix dactylifera (P. dactylifera; Family: Arecaceae), commonly known as “Ajwa,” [...] Read more.

Background: Neurodegenerative diseases primarily afflict the elderly and are characterized by a progressive loss of neurons. Oxidative stress is intricately linked to the advancement of these conditions. This study focuses on Phoenix dactylifera (P. dactylifera; Family: Arecaceae), commonly known as “Ajwa,” a globally cultivated herbal plant renowned for its potent antioxidant properties and reported neuroprotective effects in pharmacological studies. Method: This comprehensive systematic review delves into the antioxidant properties of plant extracts and their phytochemical components, with a particular emphasis on P. dactylifera and its potential neuroprotective benefits. Preferred reporting items for systemic reviews and meta-analysis (PRISMA) were employed to review the articles. Results: The study includes 269 articles published in the literature and 17 were selected after qualitative analysis. The growing body of research underscores the critical role of polyphenolic compounds found in P. dactylifera, which significantly contribute to its neuroprotective effects through antioxidant mechanisms. Despite emerging insights into the antioxidant actions of P. dactylifera, further investigation is essential to fully elucidate the specific pathways through which it confers neuroprotection. Conclusions: Like many other plant-based supplements, P. dactylifera’s antioxidant effects are likely mediated by synergistic interactions among its diverse bioactive compounds, rather than by any single constituent alone. Therefore, additional preclinical and clinical studies are necessary to explore P. dactylifera’s therapeutic potential comprehensively, especially in terms of its targeted antioxidant activities aimed at mitigating neurodegenerative processes. Such research holds promise for advancing our understanding and potentially harnessing the therapeutic benefits of P. dactylifera in neuroprotection. Full article

(This article belongs to the Special Issue Bioactive Compounds Derived from Plants and Their Medicinal Potential)

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8 pages, 648 KiB

Open AccessBrief Report

In Vitro Evaluation of the Combinatorial Effect of Naringenin and Miltefosine against Leishmania amazonensis

by Vinícius Lopes Lessa, Gustavo Gonçalves, Beatriz Santos, Victoria Cruz Cavalari, Rafael Felipe da Costa Vieira and Fabiano Borges Figueiredo

Pharmaceuticals 2024, 17(8), 1014; https://doi.org/10.3390/ph17081014 - 1 Aug 2024

Viewed by 967

Abstract

Leishmania amazonensis causes a clinical form called diffuse cutaneous leishmaniasis (DCL) with challenges to treatment, like low efficiency and drug toxicity. Therefore, it is necessary to investigate new therapies using less toxic leishmanicidal compounds, such as flavonoids like naringenin, and their combination with [...] Read more.

Leishmania amazonensis causes a clinical form called diffuse cutaneous leishmaniasis (DCL) with challenges to treatment, like low efficiency and drug toxicity. Therefore, it is necessary to investigate new therapies using less toxic leishmanicidal compounds, such as flavonoids like naringenin, and their combination with conventional drugs, such as miltefosine. Antileishmanial dose/response activity, isobologram, calculation of dose reduction index (DRI), and fractional inhibitory concentration index (FICI) tests were performed on in vitro assays using reference promastigote forms of L. amazonensis (IFLA/BR/67/PH8) to assess the combinatorial effect between naringenin and miltefosine. The in vitro results of isobologram, DRI, and FICI calculations showed that the combination of the compounds had an additive effect and was able to reduce the half maximal inhibitory concentration (IC₅₀) of miltefosine in the promastigote forms of the parasite compared to the treatment of the drug alone. This study demonstrated in vitro the viability of a combination action of the flavonoid with the treatment with miltefosine, opening space for further investigations on the association of natural compounds with the drugs used for the treatment of L. amazonensis. Full article

(This article belongs to the Special Issue Bioactive Compounds Derived from Plants and Their Medicinal Potential)

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