In response to the urgent need to control Coronavirus disease 19 (COVID-19), this study aims to explore potential anti-SARS-CoV-2 agents from natural sources. Moreover, cytokine immunological responses to the viral infection could lead to acute respiratory distress which is considered a critical and life-threatening complication associated with the infection. Therefore, the anti-viral and anti-inflammatory agents can be key to the management of patients with COVID-19. Four bioactive compounds, namely ferulic acid 1, rutin 2, gallic acid 3, and chlorogenic acid 4 were isolated from the leaves of Pimenta dioica (L.) Merr (ethyl acetate extract) and identified using spectroscopic evidence. Furthermore, molecular docking and dynamics simulations were performed for the isolated and identified compounds (1–4) against SARS-CoV-2 main protease (Mpro) as a proposed mechanism of action. Furthermore, all compounds were tested for their half-maximal cytotoxicity (CC50) and SARS-CoV-2 inhibitory concentrations (IC50). Additionally, lung toxicity was induced in rats by mercuric chloride and the effects of treatment with P. dioca aqueous extract, ferulic acid 1, rutin 2, gallic acid 3, and chlorogenic acid 4 were recorded through measuring TNF-α, IL-1β, IL-2, IL-10, G-CSF, and genetic expression of miRNA 21-3P and miRNA-155 levels to assess their anti-inflammatory effects essential for COVID-19 patients. Interestingly, rutin 2, gallic acid 3, and chlorogenic acid 4 showed remarkable anti-SARS-CoV-2 activities with IC50 values of 31 µg/mL, 108 μg/mL, and 360 µg/mL, respectively. Moreover, the anti-inflammatory effects were found to be better in ferulic acid 1 and rutin 2 treatments. Our results could be promising for more advanced preclinical and clinical studies especially on rutin 2 either alone or in combination with other isolates for COVID-19 management.
Parkia roxburghii belongs to the family Mimosaceae; it has been used since ancient times as a cure for different health complications; such as inflammatory and gynecological diseases and hemiplegia. In this investigation, a reversed-phase-high-performance liquid chromatography (RP-HPLC) profile was carried out for P. roxburghii; also, the isolated bioactive compounds including quercetin, catechin, and biochaninA were individually and/or in combination investigated for their inhibitory effects on scopolamine-induced memory impairments in mice, implying that they have the ability to reduce the neurodegenerative effects of scopolamine and thus could be employed as a more effective therapeutic agent in the treatment of Alzheimer's disease (AD) in humans. The possible interactions of Parkia flavonoids with acetylcholinesterase (AChE), γ-aminobutyric acid A receptor, alpha5 (GABA A α5), glycogen synthase kinase-3 (GSK-3), p38 mitogen-activated protein kinase (p38MAP-kinase), signal-regulated kinase (ERK), and protein-serine/threonine kinase (Akt) were then determined using molecular docking.
These results suggested that mechanistic-based evidence substantiating the traditional claims of cucurbitacin E glucoside (1) and its derivatives (2 and 3) to be applied for the treatment of inflammation-related disorders, such as oxidative liver damage and inflammation diseases.
Context: Genus Verbascum (Scrophulariaceae) comprises about 360 species of flowering plants. Verbascum has been used in traditional medicine as an astringent, antitussive, analgesic and anti-inflammatory. Objective: Nothing was found in the available literature concerning Verbascum nubicum Murb; therefore, the study evaluates the biological activities, isolated compounds and HPLC profile. Materials and methods: Methanol extract (VME) and butanol fraction (VBF) of air-dried powdered V. nubicum were obtained. Four compounds were isolated from VBE and identified by 1 H- and 13 C-NMR. High-performance liquid chromatography (HPLC) profile was determined for (VME). LD 50 , in vitro antioxidant, in vivo antiulcerogenic and anti-inflammatory activities as well as hepatoprotective activity were assessed. Anti-ulcerogenic and hepatoprotective activities were supported by histopathological examinations. Results: HPLC analysis of VME revealed the presence of luteolin 7-glucoside (2215.43 mg/100 g), hesperidin (954.51 mg/100 g) and apigenin (233.15 mg/100 g) as major compounds. Four compounds were isolated and confirmed by NMR data, were identified as gentiopicroside, luteolin, aucubin and gallic acid. The LD 50 of VME and VBF extracts were calculated to be 8200 and 4225 mg/kg b.w., respectively. IC 50 values of VBE and VMF as measured by DPPH·method were 43.6 and 50 µg/mL, respectively. Also, anti-inflammatory effect of VME (400 mg/kg b.w.) and VBF (200 mg/kg b.w.) induced edema model after 120 min were 61.93 and 56.13%, respectively. Antiulcerogenic activity of VME (400 mg/kg b.w.) and VBF (200 mg/kg b.w.) in albino rats were 65.14 and 84.57%, respectively. Conclusions: The V. nubicum extracts displayed safe and promising antioxidant, anti-inflammatory and hepatoprotective properties. It can be also applied in the pharmacy industry, food industry and healthcare.
Objective: The present study deals with isolation, structure elucidation of ferulic and coumaric acids from Fortunella japonica Swingle leaves and their structure antioxidant activity relationship. Structural analysis was conducted using UV, IR, mass and Nuclear Magentic Resonance (NMR) spectroscopy. Methodology: In particular, completely assigned
Saussurea costus is a plant traditionally used for the treatment of several ailments. Our study accomplished the UPLC/T-TOF–MS/MS analysis of a methanol extract of Saussurea costus roots (MESC), in addition to lipoidal matter determination and assessment of its in vivo hepatoprotective activity. In this study, we were able to identify the major metabolites in MESC rather than the previously known isolated compounds, improving our knowledge of its chemical constituents. The flavones apigenin, acacetin, baicalein, luteolin, and diosmetin, and the flavonol aglycones quercetin, kaempferol, isorhamnetin, gossypetin, and myricetin and/or their glycosides and glucuronic derivatives were the major identified compounds. The hepatoprotective activity of MESC was evaluated by measuring catalase activity using UV spectrophotometry, inflammatory cytokines and apoptotic markers using ELISA techniques, and genetic markers using PCR. Paracetamol toxicity caused a significant increase in plasma caspase 2, cytokeratin 18 (CK18), liver tumor necrosis factor-α (TNF-α), interleukin 6 (IL-6), miRNA-34a, and miRNA-223, as well as a significant decrease in liver catalase (CAT) activity and in the levels of liver nuclear factor 1α (HNF-1α), sirtuin-1, and C/ebpα. Oral pretreatment with MESC (200 mg/kg) showed a significant decrease in caspase 2, CK18, TNF-α, IL-6 and a significant increase in liver CAT activity. MESC decreased the levels of liver miRNA-34a and miRNA-223 and induced HNF-1α, sirtuin-1, and C/ebpα gene expression. The histological examination showed a significant normalization in rats pretreated with MESC. Our findings showed that Saussurea costus may exert a potent hepatoprotective activity through the modulation of the expression of cellular cytokines, miRNA-34a, and miRNA-223.
Background: Delonix regia (Hook.) Raf. (Fabaceae) is an ornamental tree with flamboyant flowers. Objective: to carry out pharmacognostical studies to evaluate the features of different D. regia organs, quantification and HPLC profiling of phenolics and flavonoids of leaf extract, also to evaluate possible hepatoprotective activities of the leaf hydroalcoholic extract and its fractions. Materials and Methods: Total phenolic content (TPC) as gallic acid equivalent /100 g dried extract (GAE/100 g DE), and total flavonoid content (TFC) as catechin equivalent /100 g (CE/100 g DE) of the leaves were carried out using Folin-Ciocalteu's and aluminum chloride assays, respectively. Hepatoprotective activity was determined against CCl 4 induced hepatotoxicity in rats. Results: TPC and TFC were 5.5 g GAE/100 g DE and 53.3 g CE/100 g DE respectively, with identification of 13 flavonoids, and 17 phenolics. Hesperidin was present as the highest flavonoid content (48622.5 mg/100 g DE), followed by quercetrin (711.5 mg/100 g DE), whilst hydroxytyrosol was the major identified phenolic compound (1111.2 mg/100g DE) followed by catechin (1026.1 mg/100 g DE). The ethyl acetate fraction showed significant protection against the elevation in the levels of serum biochemical parameters, normal hepatocytes with minimum fatty changes, portal vain congestion and mild inflammatory cell infiltration around the portal vain comparable to CCl 4 group (P< 0.001). The potent and significant hepatoprotective activity of the ethyl acetate fraction may be attributed to its high content of antioxidant phenolic compounds. Thus, the present study may be the first to test the hepatoprotective effect of Delonix regia fractions. INTRODUCTIONThe Caesalpinioideae (Fabaceae) represent approximately 11% of all legume taxa with more than 2250 species of mostly tropical and subtropical trees and shrubs.1 Delonix is a genus of Caesalpinioideae that is widely used in folk medicine. Delonix regia (Hook.) Raf. (Poinciana regia Boj. ex Hook, Gul mohar) is an ornamental tree (10-18 m) with fern-like bipinnately compound leaves and attractive red peacock flowers. It is native to Madagascar and widely grown in Egypt (especially in Cairo and Sinai), lining the streets and gardens for its beauty.2 Delonix regia, with an impressive range of medicinal and biological properties, has been used in folk medicine for the treatment of constipation, inflammation, arthritis, hemiplagia, gynecological disorders, and rheumatism. The leaves were reported to have antidiabetic, 4 anti-inflammatory, 5 antimicrobial and antioxidant activities.6 A methanolic extract of aerial parts possesses hepatoprotective activity against CCl 4 -induced hepatotoxicity in rats.7 Chemically, the leaves are reported to contain lupeol, epilupeol, β-sitosterol 8 and phenolic acids (gallic, protocatechuic and salicylic acids).9 It is well established that phenolic antioxidants, including flavonoids and phenolic acids, are commonly distributed in plant leaves. Natural flavonoids and phenolic acids ha...
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