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184 result(s) for "isolated compounds"
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Pharmacological Update Properties of Aloe Vera and its Major Active Constituents
Aloe vera has been traditionally used to treat skin injuries (burns, cuts, insect bites, and eczemas) and digestive problems because its anti-inflammatory, antimicrobial, and wound healing properties. Research on this medicinal plant has been aimed at validating traditional uses and deepening the mechanism of action, identifying the compounds responsible for these activities. The most investigated active compounds are aloe-emodin, aloin, aloesin, emodin, and acemannan. Likewise, new actions have been investigated for Aloe vera and its active compounds. This review provides an overview of current pharmacological studies (in vitro, in vivo, and clinical trials), written in English during the last six years (2014–2019). In particular, new pharmacological data research has shown that most studies refer to anti-cancer action, skin and digestive protective activity, and antimicrobial properties. Most recent works are in vitro and in vivo. Clinical trials have been conducted just with Aloe vera, but not with isolated compounds; therefore, it would be interesting to study the clinical effect of relevant metabolites in different human conditions and pathologies. The promising results of these studies in basic research encourage a greater number of clinical trials to test the clinical application of Aloe vera and its main compounds, particularly on bone protection, cancer, and diabetes.
Anticancer Activity of Novel Plant Extracts and Compounds from Adenosma bracteosum (Bonati) in Human Lung and Liver Cancer Cells
Cancer is the second leading cause of death globally, and despite the advances in drug development, it is still necessary to develop new plant-derived medicines. Compared with using conventional chemical drugs to decrease the side effects induced by chemotherapy, natural herbal medicines have many advantages. The present study aimed to discover the potential cytotoxicity of ethanol extract and its derived fractions (chloroform, ethyl acetate, butanol, and aqueous) of Adenosma bracteosum Bonati. (A. bracteosum) on human large cell lung carcinoma (NCI-H460) and hepatocellular carcinoma (HepG2). Among these fractions, the chloroform showed significant activity in the inhibition of proliferation of both cancerous cells because of the presence of bioactive compounds including xanthomicrol, 5,4’-dihydroxy-6,7,8,3’-tetramethoxyflavone, and ursolic acid which were clearly revealed by nuclear magnetic resonance spectroscopy (1H-NMR, 13C-NMR, Heteronuclear Multiple Bond Coherence, and Heteronuclear Single Quantum Coherence Spectroscopy) analyses. According to the radical scavenging capacity, the 5,4’-dihydroxy-6,7,8,3’-tetramethoxyflavone compound (AB2) exhibited the highest anticancer activity on both NCI-H460 and HepG2 with IC50 values of 4.57 ± 0.32 and 5.67 ± 0.09 µg/mL respectively, followed by the ursolic acid with the lower percent inhibition at 13.05 ± 0.55 and 10.00 ± 0.16 µg/mL, respectively (p < 0.05). Remarkably, the AB2 compound induced to significant increase in the production of reactive oxygen species accompanied by attenuation of mitochondrial membrane potential, thus inducing the activation of caspase-3 activity in both human lung and liver cancer cells. These results suggest that A. bracteosum is a promising source of useful natural products and AB2 offers opportunities to develop the novel anticancer drugs.
Natural Products from Medicinal Plants against Phytopathogenic Fusarium Species: Current Research Endeavours, Challenges and Prospects
Many Fusarium species are pathogenic, causing crop diseases during crop production and spoilage of agricultural products in both commercial and smallholder farming. Fusarium attack often results into food contamination, yield loss and increases in food insecurity and food prices. Synthetic fungicides have been used as a control strategy for the management of crop diseases caused by Fusarium pathogens. The negative effects associated with application of many synthetic pesticides has necessitated the need to search for alternative control strategies that are affordable and environmentally safe. Research on medicinal plants as control agents for Fusarium pathogens has received attention since plants are readily available and they contain wide variety of secondary metabolites that are biodegradable. The activities of solvent extracts, essential oils and compounds from medicinal plants have been tested against Fusarium phytopathogenic species. A summary of recent information on antifungal activity of plants against Fusarium species is valuable for the development of biopesticides. This paper reviews the antifungal research conducted on medicinal plants against Fusarium pathogens, over a 10-year period, from January 2012 to May 2021. We also highlight the challenges and opportunities of using natural products from medicinal plants in crop protection. Several databases (Science Direct and Web of Science) were used to obtain information on botanical products used to control Fusarium diseases on crops. Keywords search used included natural products, antifungal, Fusarium, crops diseases, phytopathogenic, natural compounds and essential oil.
Activity of Compounds from Temperate Propolis against Trypanosoma brucei and Leishmania mexicana
Ethanolic extracts of samples of temperate zone propolis, four from the UK and one from Poland, were tested against three Trypanosoma brucei strains and displayed EC50 values < 20 µg/mL. The extracts were fractionated, from which 12 compounds and one two-component mixture were isolated, and characterized by NMR and high-resolution mass spectrometry, as 3-acetoxypinobanksin, tectochrysin, kaempferol, pinocembrin, 4′-methoxykaempferol, galangin, chrysin, apigenin, pinostrobin, cinnamic acid, coumaric acid, cinnamyl ester/coumaric acid benzyl ester (mixture), 4′,7-dimethoxykaempferol, and naringenin 4′,7-dimethyl ether. The isolated compounds were tested against drug-sensitive and drug-resistant strains of T. brucei and Leishmania mexicana, with the highest activities ≤ 15 µM. The most active compounds against T. brucei were naringenin 4′,7 dimethyl ether and 4′methoxy kaempferol with activity of 15–20 µM against the three T. brucei strains. The most active compounds against L. mexicana were 4′,7-dimethoxykaempferol and the coumaric acid ester mixture, with EC50 values of 12.9 ± 3.7 µM and 13.1 ± 1.0 µM. No loss of activity was found with the diamidine- and arsenical-resistant or phenanthridine-resistant T. brucei strains, or the miltefosine-resistant L. mexicana strain; no clear structure activity relationship was observed for the isolated compounds. Temperate propolis yields multiple compounds with anti-kinetoplastid activity.
A Comprehensive Review of the Pharmacological Properties and Bioactive Components of Retama monosperma
Retama monosperma L. (Boiss.) or Genista monosperma L. (Lam.), known locally as “R’tam”, is a spontaneous and annual herb that belongs to the Fabaceae family. It is native to the Mediterranean regions, specifically in the desert areas and across the Middle Atlas in Morocco. This plant has been extensively used in folk medicine and it is rich in bioactive compounds, including polyphenols, flavonoids, and alkaloids. Current research efforts are focusing on the development of novel natural drugs as alternatives to various organic and non-organic chemical products from Retama monosperma. In addition, extract, and isolated compounds obtained from different parts of the chosen plant have been described to exhibit multiple biological and pharmacological properties such as antioxidant, anti-aging, anti-inflammatory, antihypertensive, anti-helminthic, disinfectant, diuretic, and hypoglycemic effects. The plant-derived extract also acts as an antimicrobial agent, which is highly efficient in the treatment of bacterial, viral, and fungal infections. Its antiproliferative effects are associated with some mechanisms, such as the inhibition of cell cycle arrest and apoptosis. In light of these assessments, we critically highlight the beneficial effects of the flowers, stems, seeds extracts, and isolated compounds from R. monosperma (L.) Boiss in human health care, industrial, and other applications, as well as the possible ways to be employed as a potential natural source for future drug discovery.
Chemical Constituents from Osmanthus fragrans var. aurantiacus Makino with Their In Vitro and In Silico Studies Target Anti-Inflammation by Suppressing ERK 1/2 MAPK Signaling
Osmanthus fragrans var. aurantiacus Makino is a traditional medicine for treating various diseases, including inflammation. In this study, we discovered the biological features of this plant by assessing antioxidative and anti-inflammatory activities. The GNPS-FBMN approach and in vitro assays guided the identification of active ingredients. As a result, one new compound and 17 other compounds were separated and identified. The structure of the new compound was established by CD spectrum and hydrolysis, followed by HPLC analysis. These compounds demonstrated antioxidative and anti-inflammatory activities. Western blotting clarified the active compound by inhibiting inflammation through COX-2 and iNOS enzymes and blocking the ERK 1/2 MAPK signaling. In silico approaches supported the binding affinity and dynamic features of the established complexes’ target inflammation. Our finding supports evidence from both experimental and in silico approaches that O. fragrans fractions and its constituents may be employed as potential therapeutic phytochemicals for treating inflammatory bowel diseases.
Potent in Vitro α-Glucosidase Inhibition of Secondary Metabolites Derived from Dryopteris cycadina
α-glucosidase is responsible for the hydrolysis of complex carbohydrates into simple absorbable glucose and causes postprandial hyperglycemia. α-glucosidase inhibition is thus the ideal target to prevent postprandial hyperglycemia. The present study was therefore designed to analyze the effects of various compounds isolated from Dryopteris cycadina against α-glucosidase including β-Sitosterol 1, β-Sitosterol3-O-β-d-glucopyranoside 2, 3, 5, 7-trihydroxy-2-(p-tolyl) chorman-4-one 3, Quercetin-3-0-β-d-glucopyranoside (3/→0-3///)- β-d- Quercetin -3-0- β –d-galactopyranoside 4 and 5, 7, 4/-Trihydroxyflavon-3-glucopyranoid 5. The in vitro spectrophotometric method was used for the analysis of test compounds against possible inhibition. Similarly, molecular docking studies were performed using the MOE software. These compounds showed concentration-dependent inhibition on α-glucosidase, and compounds 1 (IC50: 143 ± 0.47 µM), 3 (IC50:133 ± 6.90 µM) and 5 (IC50: 146 ± 1.93 µM) were more potent than the standard drug, acarbose (IC50: 290 ± 0.54 µM). Computational studies of these compounds strongly supported the in vitro studies and showed strong binding receptor sensitivity. In short, the secondary metabolites isolated from D. cycadina demonstrated potent α-glucosidase inhibition that were supported by molecular docking with a high docking score.
Identification and Integrative Discovery of Anti-Inflammatory Compounds Isolated from Eclipta prostrata (L.) L. by Network Pharmacology, Molecular Docking, and In Vitro Evaluation
Background/Objective: Eclipta prostrata (L.) L. is a traditional medicinal herb utilized throughout Asia that is widely used for hepatoprotective activity, wound healing, and blood cooling/bleeding disorders. This work aimed to identify bioactive constituents from E. prostrata collected in Vietnam, and clarify their anti-inflammatory capacity of the extract and active fraction. Method: Extraction and isolation of compounds from the extract of E. prostrata were performed. The extract, fractions, and isolated compounds were evaluated for inflammatory cytokines in LPS-stimulated RAW264.7 cells. Isolates showed inflammatory potential by in silico approaches. Results: Thirteen compounds, comprising a first isolated compound (diosmin), flavonoids, and phenolic derivatives, were separated and identified. The protein–protein interaction (PPI) network demonstrated TNF, IL6, AKT1, NFKB1, EGFR, and PTGS2 as central targets, highlighting their significance in inflammatory signaling. Gene Ontology and KEGG pathway enrichment underscored substantial participation in TNF and IL-17 cytokine signaling pathways. Molecular docking demonstrated robust interactions between several flavonoids and core targets, indicating their function as essential regulators. Experimental validation in LPS-stimulated RAW264.7 macrophages revealed that wedelolactone, luteolin, apigenin, and quercetin significantly inhibited TNF-α and IL-6 production. Conclusions: The results proposed that E. prostrata demonstrates its anti-inflammatory efficacy via a multi-target, poly-pharmacological strategy that encompasses central cytokine pathways and upstream receptor-mediated signaling. Our findings offer new mechanistic evidence that supports the ethnomedicinal application of E. prostrata and indicates its potential as a valuable natural resource for treating anti-inflammatory diseases.
Evaluation of Antioxidant-Rich Mexican Oregano (Lippia graveolens) Infusion and Carvacrol: Impact on Metabolic Activity and Cytotoxicity in Breast Cancer Cell Lines
Background/Objectives: The search for natural alternatives in breast cancer (BC) management has spurred interest in plant-derived extracts, particularly oregano variants and their bioactive compound carvacrol (Cv). However, Mexican oregano (Lippia graveolens) infusion (MoI) remains unexplored. This study aimed to chemically characterize MoI and compare its anticancer effects with Cv across BC cell lines, including aggressive triple-negative (TN) subtypes. Methods: MoI was analyzed for composition, antioxidant capacity (ABTS, DPPH, FRAP, total phenols/flavonoids), and phytochemical profile (FTIR, HPLC). Anticancer activity was assessed via MTT and LDH assays. Results: MoI exhibits strong antioxidant capacity and concentration-dependent antiproliferative effects, with IC50 values ranging from 0.08 to 0.18 mg/mL across BC lines, significantly higher (i.e., less cytotoxic) than Cv IC50 of 121–211 µM. Importantly, MoI displayed markedly lower cytotoxicity toward non-cancerous cells (IC50 0.18 mg/mL) compared to Cv (IC50 110 µM). Conclusions: While both agents reduced metabolic activity, Cv induced a more acute suppression. These findings position MoI as a promising, selective candidate for BC therapy, particularly for poor-prognosis subtypes like TN BC, warranting further mechanistic investigation.
Evaluation of the Antifungal and Antiproliferative Properties of the Lichen Roccella tinctoria DC. Extracts and Main Components
In this work, phytochemical analysis on different extracts of Roccella tinctoria DC. was reported using different techniques with respect to the past. Twenty volatile and three non-volatile compounds were identified, some of which were found in this species for the first time. The methanolic extracts and their non-volatile components were then evaluated for their antitumor effects in cancerous A549 and Mz-ChA-1 cells and for their tolerability in non-cancerous BEAS-2B and H69 cells, showing IC50 values from 94.6 µg/mL to 416.4 µg/mL, in general. The same extracts and compounds were also tested for their antifungal effects in Candida albicans, with only compound 2 being active, with an MIC50 value of 87 µg/mL. In addition, they were tested for their anti-Candida adhesion activity, anti-Candida biofilm formation, and anti-Candida mature biofilm inhibition, with efficacy percentages generally above 50% but not for all of them. Lastly, the DF3 extract and compounds 1–2 were tested in vivo according to the Galleria mellonella survival assay, showing positive mortality rates above 50% at different concentrations. All these biological assays were conducted on this species for the first time. Comparisons with other lichens and compounds were also presented and discussed.