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1.
Int J Biol Macromol ; 280(Pt 1): 135691, 2024 Sep 14.
Artículo en Inglés | MEDLINE | ID: mdl-39284468

RESUMEN

Cancer remains a major global health concern, often challenging traditional treatments. Natural compounds like fungal polysaccharides have gained attention for their immune-modulatory properties. This study evaluates the phytochemical properties of the n-hexane fraction of Trichaptum biforme and explores its immune-enhancing effects. The study involved isolating three sterol derivatives using column chromatography and purifying polysaccharides from T. biforme (TBP) through hot aqueous extraction. TBP content was quantified via the phenol­sulfuric acid method, and antioxidant activity was assessed using DPPH and FRAP assays. Cytotoxicity of TBP on THP-1 cells and the impact on IL-1ß and TNF-α secretion were evaluated through the XTT assay. Flow cytometry and ELISA assessed cytotoxic activity and IFN-γ secretion in NK cells. The compound 9, 11-Dehydroergosterol peroxide was identified for the first time in T. biforme. The total polysaccharide content was 78.18 ± 0.81 %. The TBP significantly increased IL-1ß and TNF-α secretion from THP-1 cells at concentrations of 10 and 320 µg/mL (p < 0.01). Treatment of NK cells with the extract (320 µg/mL) and IL-2 (100 units/mL) significantly enhanced cytotoxic activity and IFN-γ secretion compared to the control group (p < 0.01). These findings suggest that TBP holds promise as a candidate for bolstering anticancer immune responses.

2.
Sci Rep ; 14(1): 18117, 2024 08 05.
Artículo en Inglés | MEDLINE | ID: mdl-39103444

RESUMEN

Diabetic nephropathy, characterized by inflammation and oxidative stress, poses a management challenge. This study investigates the effect of Polygonum hyrcanicum extract on diabetic nephropathy in alloxan-induced diabetic mice. In this experimental animal study, the P. hyrcanicum extract was prepared using continuous macerations. Thirty male Albino mice, divided into five groups, were induced with alloxan-induced diabetes. They received intraperitoneal injections of the plant extract (100 and 200 mg/kg) and metformin (300 mg/kg) for four weeks. Kidney and blood samples were collected to assess protein carbonyl, glutathione, lipid peroxidation, TNF-α and IL-6 levels. The amount of total flavonoid and phenolic content in the hydroalcoholic extract of P. hyrcanicum were 7.5 ± 0.3 mg of quercetin and 88.2 ± 1.3 mg gallic acid per gram of extract respectively. The antioxidant activity level of the hydroalcoholic extract was determined to be 1.78 ± 0.51 mM equivalent per gram of extract. Alloxan administration resulted in a significant reduction in glutathione levels and a significant increase in protein carbonyl, lipid peroxidation, TNF-α, and IL-6 levels. Hydroalcoholic extract of P. hyrcanicum effectively reduced oxidative stress markers and inflammatory cytokines (TNF-α, IL-6), indicating its potential in mitigating diabetic nephropathy. However, no significant difference in efficacy was observed between the 100 mg/kg and 200 mg/kg doses in terms of reducing these toxicities.


Asunto(s)
Antioxidantes , Diabetes Mellitus Experimental , Nefropatías Diabéticas , Estrés Oxidativo , Extractos Vegetales , Polygonum , Animales , Estrés Oxidativo/efectos de los fármacos , Extractos Vegetales/farmacología , Extractos Vegetales/química , Diabetes Mellitus Experimental/tratamiento farmacológico , Diabetes Mellitus Experimental/metabolismo , Nefropatías Diabéticas/tratamiento farmacológico , Nefropatías Diabéticas/metabolismo , Ratones , Masculino , Antioxidantes/farmacología , Polygonum/química , Aloxano , Peroxidación de Lípido/efectos de los fármacos , Factor de Necrosis Tumoral alfa/metabolismo , Glutatión/metabolismo , Riñón/efectos de los fármacos , Riñón/metabolismo , Riñón/patología , Interleucina-6/metabolismo , Interleucina-6/sangre
3.
Eur J Pharmacol ; 980: 176873, 2024 Oct 05.
Artículo en Inglés | MEDLINE | ID: mdl-39117264

RESUMEN

Huntington's disease (HD) is a progressive neurodegenerative disorder characterized by cognitive, motor, and psychiatric symptoms. Despite significant advances in understanding the underlying molecular mechanisms of HD, there is currently no cure or disease-modifying treatment available. Emerging pharmacological approaches offer promising strategies to alleviate symptoms and slow down disease progression. This comprehensive review aims to provide a critical appraisal of the latest developments in pharmacological interventions for HD. The review begins by discussing the pathogenesis of HD, focusing on the role of mutant huntingtin protein, mitochondrial dysfunction, excitotoxicity, and neuro-inflammation. It then explores emerging therapeutic targets, including the modulation of protein homeostasis, mitochondrial function, neuro-inflammation, and neurotransmitter systems. Pharmacological agents targeting these pathways are discussed, including small molecules, gene-based therapies, and neuroprotective agents. In recent years, several clinical trials have been conducted to evaluate the safety and efficiency of novel compounds for HD. This review presents an update on the outcomes of these trials, highlighting promising results and challenges encountered. Additionally, it discusses the potential of repurposing existing drugs approved for other indications as a cost-effective approach for HD treatment. The review concludes by summarizing the current state of pharmacological approaches for HD and outlining future directions in drug development. The integration of multiple therapeutic strategies, personalized medicine approaches, and combination therapies are highlighted as potential avenues to maximize treatment effectiveness.


Asunto(s)
Enfermedad de Huntington , Fármacos Neuroprotectores , Enfermedad de Huntington/tratamiento farmacológico , Humanos , Animales , Fármacos Neuroprotectores/uso terapéutico , Fármacos Neuroprotectores/farmacología , Proteína Huntingtina/genética , Proteína Huntingtina/antagonistas & inhibidores , Proteína Huntingtina/metabolismo , Mitocondrias/efectos de los fármacos , Mitocondrias/metabolismo , Terapia Genética/métodos
4.
J Clin Med ; 13(14)2024 Jul 18.
Artículo en Inglés | MEDLINE | ID: mdl-39064239

RESUMEN

Background/Objectives: Among various carbapenemases, New Delhi metallo-beta-lactamases (NDMs) are recognized as the most powerful type capable of hydrolyzing all beta-lactam antibiotics, often conferring multi-drug resistance to the microorganism. The objective of this review is to synthesize current scientific data on NDM inhibitors to facilitate the development of future therapeutics for challenging-to-treat pathogens. Methods: Following the Preferred Reporting Items for Systematic Reviews and Meta-Analyses (PRISMA) Extension for Scoping Reviews, we conducted a MEDLINE search for articles with relevant keywords from the beginning of 2009 to December 2022. We employed various generic terms to encompass all the literature ever published on potential NDM inhibitors. Results: Out of the 1760 articles identified through the database search, 91 met the eligibility criteria and were included in our analysis. The fractional inhibitory concentration index was assessed using the checkerboard assay for 47 compounds in 37 articles, which included 8 compounds already approved by the Food and Drug Administration (FDA) of the United States. Time-killing curve assays (14 studies, 25%), kinetic assays (15 studies, 40.5%), molecular investigations (25 studies, 67.6%), in vivo studies (14 studies, 37.8%), and toxicity assays (13 studies, 35.1%) were also conducted to strengthen the laboratory-level evidence of the potential inhibitors. None of them appeared to have been applied to human infections. Conclusions: Ongoing research efforts have identified several potential NDM inhibitors; however, there are currently no clinically applicable drugs. To address this, we must foster interdisciplinary and multifaceted collaborations by broadening our own horizons.

5.
JMIR Hum Factors ; 11: e48139, 2024 Jul 30.
Artículo en Inglés | MEDLINE | ID: mdl-39078685

RESUMEN

BACKGROUND: The enormous consequences of drugs include suicides, traffic accidents, and violence, affecting the individual, family, society, and country. Therefore, it is necessary to constantly identify and monitor the drug abuse rate among school-going youth. A geospatial dashboard is vital for the monitoring of drug abuse and related crime incidence in a decision support system. OBJECTIVE: This paper mainly focuses on developing MyAsriGeo, a geospatial drug abuse risk assessment and monitoring dashboard tailored for school students. It introduces innovative functionality, seamlessly orchestrating the assessment of drug abuse usage patterns and risks using multivariate student data. METHODS: A geospatial drug abuse dashboard for monitoring and analysis was designed and developed in this study based on agile methodology and prototyping. Using focus group and interviews, we first examined and gathered the requirements, feedback, and user approval of the MyAsriGeo dashboard. Experts and stakeholders such as the National Anti-Drugs Agency, police, the Federal Department of Town and Country Planning, school instructors, students, and researchers were among those who responded. A total of 20 specialists were involved in the requirement analysis and acceptance evaluation of the pilot and final version of the dashboard. The evaluation sought to identify various user acceptance aspects, such as ease of use and usefulness, for both the pilot and final versions, and 2 additional factors based on the Post-Study System Usability Questionnaire and Task-Technology Fit models were enlisted to assess the interface quality and dashboard sufficiency for the final version. RESULTS: The MyAsriGeo geospatial dashboard was designed to meet the needs of all user types, as identified through a requirement gathering process. It includes several key functions, such as a geospatial map that shows the locations of high-risk areas for drug abuse, data on drug abuse among students, tools for assessing the risk of drug abuse in different areas, demographic information, and a self-problem test. It also includes the Alcohol, Smoking, and Substance Involvement Screening Test and its risk assessment to help users understand and interpret the results of student risk. The initial prototype and final version of the dashboard were evaluated by 20 experts, which revealed a significant improvement in the ease of use (P=.047) and usefulness (P=.02) factors and showed a high acceptance mean scores for ease of use (4.2), usefulness (4.46), interface quality (4.29), and sufficiency (4.13). CONCLUSIONS: The MyAsriGeo geospatial dashboard is useful for monitoring and analyzing drug abuse among school-going youth in Malaysia. It was developed based on the needs of various stakeholders and includes a range of functions. The dashboard was evaluated by a group of experts. Overall, the MyAsriGeo geospatial dashboard is a valuable resource for helping stakeholders understand and respond to the issue of drug abuse among youth.


Asunto(s)
Estudiantes , Trastornos Relacionados con Sustancias , Humanos , Trastornos Relacionados con Sustancias/epidemiología , Trastornos Relacionados con Sustancias/diagnóstico , Medición de Riesgo/métodos , Adolescente , Instituciones Académicas , Grupos Focales , Masculino , Femenino , Interfaz Usuario-Computador
6.
Phytochem Anal ; 35(5): 927-989, 2024 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-38837522

RESUMEN

INTRODUCTION: Organic molecules that bind to cannabinoid receptors are known as cannabinoids. These molecules possess pharmacological properties similar to those produced by Cannabis sativa L. High-performance liquid chromatography (HPLC) and ultra-performance liquid chromatography (UPLC, also known as ultra-high-performance liquid chromatography, UHPLC) have become the most widely used analytical tools for detection and quantification of phytocannabinoids in various matrices. HPLC and UPLC (or UHPLC) are usually coupled to an ultraviolet (UV), photodiode array (PDA), or mass spectrometric (MS) detector. OBJECTIVE: To critically appraise the literature on the application of HPLC and UPLC (or UHPLC) methods for the analysis of phytocannabinoids published from January 2020 to December 2023. METHODOLOGY: An extensive literature search was conducted using Web of Science, PubMed, and Google Scholar and published materials including relevant books. In various combinations, using cannabinoid in all combinations, cannabis, hemp, hashish, C. sativa, marijuana, analysis, HPLC, UHPLC, UPLC, and quantitative, qualitative, and quality control were used as the keywords for the literature search. RESULTS: Several HPLC- and UPLC (or UHPLC)-based methods for the analysis of phytocannabinoids were reported. While simple HPLC-UV or HPLC-PDA-based methods were common, the use of HPLC-MS, HPLC-MS/MS, UPLC (or UHPLC)-PDA, UPLC (or UHPLC)-MS, and UPLC (or UHPLC)-MS/MS was also reported. Applications of mathematical and computational models for optimization of protocols were noted. Pre-analyses included various environmentally friendly extraction protocols. CONCLUSION: During the last 4 years, HPLC and UPLC (or UHPLC) remained the main analytical tools for phytocannabinoid analysis in different matrices.


Asunto(s)
Cannabinoides , Cromatografía Líquida de Alta Presión/métodos , Cannabinoides/análisis , Cannabis/química
7.
Fitoterapia ; 176: 106026, 2024 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-38768794

RESUMEN

Rydingia michauxii and R. persica, respectively, known as Kase Gol and Goldar in Persian, belong to the family Lamiaceae and they are well known herbal medicine in Iran for the treatment of various diseases, particularly diabetes. This review aims to appraise the phytochemistry, ethnopharmacology, and pharmacological activities of Rydingia species growing in Iran and assess their potential in clinical applications. Besides, it critically evaluates existing literature and looks into the perspective for further research and utilization. All available scientific literature was consulted using the database searches involving Google Scholar, PubMed, and Web of Science applying the keyword Rydingia and its Syn; Otostegia. Only the search results that are associated with the Iranian species R. michauxii and R. persica are included in this review. α-pinene, carvacrol, caryophyllene oxide, diisooctyl phthalate, dillapiole, eugenol, hexadecanoic acid, and pentacosane are the major constituents of the essential oils of the Rydingia species. Additionally, these species produce bioactive flavonoids, phenolic acids, steroids, and terpenoids. Extracts and active compounds from Rydingia species have been reported to possess various pharmacological activities including antidiabetic, anti-inflammatory, antimalarial, antimicrobial, antioxidant, cytotoxic, and lipid-lowering properties. Based on the information available to date on the Iranian Rydingia species, it will be worth subjecting these species to further developmental work involving preclinical and clinical trials.


Asunto(s)
Etnofarmacología , Lamiaceae , Aceites Volátiles , Fitoquímicos , Fitoquímicos/farmacología , Fitoquímicos/aislamiento & purificación , Irán , Lamiaceae/química , Humanos , Aceites Volátiles/farmacología , Aceites Volátiles/química , Animales , Extractos Vegetales/farmacología , Extractos Vegetales/química , Fitoterapia
8.
Fitoterapia ; 176: 105979, 2024 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-38692415

RESUMEN

Anogeissus leiocarpus (DC.) Guill. & Perr. belongs to the family Combretaceae and is used both by African traditional medical practitioners and livestock rearers to treat diseases such as African trypanosomiasis, animal diarrhoea, asthma, cancer, cough, diabetes, dysentery, erectile dysfunction, fever, giardiasis, helminthiases, meningitis, menstrual disorders, monkeypox, oral infections, poliomyelitis, sickle cell anaemia, snake bites, toothache, urinary schistosomiasis, and yellow fever. Some of these activities have been associated with the presence of polyphenols in the plant which include ellagic acid derivatives, flavonoids, stilbenes, tannins, and triterpenes. Several bioactive molecules have been identified from A. leiocarpus. These include the main active constituents, ellagitannins, ellagic acid derivates, flavonoids and triterpenes. Pharmacological studies have confirmed its antibacterial, antifungal, antihyperglycemic, antihypertensive, antimalarial, antioxidative, antiparasitic, antitumour and anti-ulcer effects. The stem bark has been investigated mainly for biological activities and phytochemistry, and it is the most mentioned plant part highlighted by the traditional users in ethnomedicinal surveys. In vitro and in vivo models, which revealed a wide range of pharmacological actions against parasites causing helminthiasis, leishmaniasis, malaria and trypanosomiasis, have been used to study compounds from A. leiocarpus. Because of its uses in African traditional medicine and veterinary practices, A. leiocarpus has received considerable attention from researchers. The current review provides a comprehensive overview and critical appraisal of scientific reports on A. leiocarpus, covering its traditional uses, pharmacological activities and phytochemistry.


Asunto(s)
Combretaceae , Medicinas Tradicionales Africanas , Fitoquímicos , Fitoquímicos/farmacología , Fitoquímicos/aislamiento & purificación , Combretaceae/química , Humanos , Extractos Vegetales/farmacología , Extractos Vegetales/química , Animales , Corteza de la Planta/química
9.
J Exp Bot ; 75(16): 5037-5053, 2024 Aug 28.
Artículo en Inglés | MEDLINE | ID: mdl-38727615

RESUMEN

Transgenerational plasticity in plants enables rapid adaptation to environmental changes, allowing organisms and their offspring to adapt to the environment without altering their underlying DNA. In this study, we investigated the transgenerational plasticity in salinity tolerance of rice plants using a reciprocal transplant experimental strategy. Our aim was to assess whether non-genetic environment-induced phenotypic modifications and transgenerational salinity affect the salinity tolerance of progeny while excluding nuclear genomic factors for two generations. Using salt-tolerant and salt-sensitive rice genotypes, we observed that the parentally salt-stressed salt-sensitive genotype displayed greater growth performance, photosynthetic activity, yield performance, and transcriptional responses than the parentally non-stressed salt-sensitive plants under salt stress conditions. Surprisingly, salt stress-exposed salt-tolerant progeny did not exhibit as much salinity tolerance as salt stress-exposed salt-sensitive progeny under salt stress. Our findings indicate that the phenotypes of offspring plants differed based on the environment experienced by their ancestors, resulting in heritable transgenerational phenotypic modifications in salt-sensitive genotypes via maternal effects. These results elucidated the mechanisms underlying transgenerational plasticity in salinity tolerance, providing valuable insights into how plants respond to changing environmental conditions.


Asunto(s)
Oryza , Fenotipo , Tolerancia a la Sal , Oryza/genética , Oryza/fisiología , Oryza/crecimiento & desarrollo , Tolerancia a la Sal/genética , Genotipo , Adaptación Fisiológica/genética , Salinidad , Ambiente
10.
Toxicon ; 238: 107603, 2024 Feb 01.
Artículo en Inglés | MEDLINE | ID: mdl-38184283

RESUMEN

Arsenic toxicity is a major problem across the world due to geogenic activity and has been supposed to generate free radicals and genotoxicity among the arsenic-poisoned population. There is a need to find suitable free radical quenching compounds for the arsenic-induced free radical-affected population. In the present study, Na3AsO3- induced oxidative stress and genotoxicity were evaluated in Oryctolagus cuniculus L, and quenching competency of Ocimum species was examined by applying enzymatic and non-enzymatic in vitro tests, comet assay, and Random Amplified Polymorphic Deoxyribonucleic acid - Polymerase Chain Reaction (RAPD-PCR) methods. In the present study, oxidative damage due to Na3AsO3 intoxication in O. cuniculus L has been confirmed followed by substantive genotoxicity, and in a further study, it has also been reported that the extract of O. gratissimum L lowers the oxidative stress in experimental animals confirmed by a decrease in Malondialdehyde (MDA) 4.78 ± 0.05 (nmol/mg protein), and an increase in Glutathione (GSH) 2.87 ± 0.50 (µmoles/mg proteins), Superoxide Dismutase (SOD) 1.78 ± 0.03(Units/mg protein), Catalase (CAT) 2.72 ± 0.02 (µmoles of H2O2 consumed/min/mg proteins) and Glutathione peroxidase (GPX) 7.43 ± 0.01 (µg of glutathione utilized/min/mg protein). A positive impact of extract of O. gratissimum L on protection of genotoxicity has been also confirmed by Random Amplified Polymorphic DNA (RAPD) based reduction in polymorphic bands of Deoxyribonucleic acid (DNA) from 6.5 to 3.16 and comet assay-based increase in head DNA % (87.86 ± 1.58), tail moment (1.07 ± 0.27) and decrease in tail DNA % (12.13 ± 1.58) & tail length (8.2 ± 1.46) at 5% P in lymphocytes. A significant level reduction in free radicals and reduction in DNA polymorphism has proved the competency of test material for the development of suitable antidotes against arsenicosis.


Asunto(s)
Intoxicación por Arsénico , Arsénico , Ocimum , Animales , Conejos , Antioxidantes/farmacología , Arsénico/toxicidad , Ocimum/metabolismo , Peróxido de Hidrógeno , Técnica del ADN Polimorfo Amplificado Aleatorio , Estrés Oxidativo , Glutatión/metabolismo , Daño del ADN , ADN/metabolismo , Superóxido Dismutasa/metabolismo
11.
Phytochem Anal ; 34(8): 903-924, 2023 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-37963411

RESUMEN

INTRODUCTION: Cannabinoids are a group of compounds that bind to cannabinoid receptors. They possess pharmacological properties like that of the plant Cannabis sativa. Gas chromatography (GC) is one of the popular chromatographic techniques that has been routinely used in the analysis of cannabinoids in different matrices. OBJECTIVE: The article aims to review the literature on the application of GC-based analytical methods for the analysis of phytocannabinoids published during the period from January 2020 to August 2023. METHODOLOGY: A thorough literature search was conducted using different databases, like Web of Knowledge, PubMed, Google Scholar, and other relevant published materials including published books. The keywords used, in various combinations, with cannabinoids being present in all combinations, in the search were cannabinoids, Cannabis sativa, marijuana, analysis, GC, quantitative, qualitative, and quality control. From the search results, only the publications that incorporate the GC analysis of phytocannabinoids were reviewed, and papers on synthetic cannabinoids were excluded. RESULTS: Since the publication of the review article on GC analysis of phytocannabinoids in early 2020, several GC-based methods for the analysis of phytocannabinoids have appeared in the literature. While simple 1D GC-mass spectrometry (MS) and GC-flame ionisation detector (FID) methods are still quite common in phytocannabinoids analysis, 2D GC-MS and GC-MS/MS are increasingly becoming popular, as these techniques offer more useful data for identification and quantification of phytocannabinoids in various matrices. The use of automation in sample preparation and the utilisation of mathematical and computational models for optimisation of different protocols have become a norm in phytocannabinoids analysis. Pre-analyses have been found to incorporate different derivatisation techniques and environmentally friendly extraction protocols. CONCLUSIONS: GC-based analysis of phytocannabinoids, especially using GC-MS, remains one of the most preferred methods for the analysis of these compounds. New derivatisation methods, ionisation techniques, mathematical models, and computational approaches for method optimisation have been introduced.


Asunto(s)
Cannabinoides , Cannabis , Alucinógenos , Espectrometría de Masas en Tándem/métodos , Cromatografía de Gases y Espectrometría de Masas/métodos , Cannabinoides/análisis , Cannabis/química
12.
Phytochemistry ; 215: 113853, 2023 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-37689382

RESUMEN

Bioactivity-guided phytochemical fractionation of the methanol extract of Olax subscorpioidea root has led to the isolation of six triterpenes. Three of these compounds are previously undescribed triterpenoid saponins: oleanolic acid 3-O-[α-L-rhamnopyranosyl-(1→3)-ß-D-glucopyranosyl-(1 â†’ 2)-6-O-methyl-ß-D-glucuronopyranoside]-28-O-ß-D-glucopyranosyl ester (2), oleanolic acid 3-O-[ß-D-glucopyranosyl-(1 â†’ 4)-ß-D-glucopyranosyl-(1 â†’ 3)-ß-D-glucopyranoside] (3), and oleanolic acid 3-O-[ß-D-glucopyranosyl-(1 â†’ 4)-6-O-methyl-ß-D-glucuronopyranoside] ester (5). Other reported known compounds include two triterpene glycosides: oleanolic acid 3-O-[ß-D-glucopyranosyl-(1 â†’ 4)-6-O-methyl-ß-D-glucuronopyranoside]-28-O-ß-D-glucopyranosyl ester (1) and oleanolic acid 3-O-[ß-D-glucopyranosyl-(1 â†’ 4)-ß-D-glucuronopyranoside] (4); and a triterpene acid, oleanolic acid (6). The structures of these compounds were elucidated by spectroscopic means. The isolated compounds were tested against human cervical cancer (HeLa), colorectal cancer (Caco-2) and breast cancer (MCF-7) cell lines using the in vitro 3-[4,5-dimethylthiazole-2-yl] 3,5-diphenyltetrazolium bromide (MTT) assay, with vincristine as positive control. The cytotoxicity assay showed that compounds 3 and 5 exhibited significant inhibitory effects on the HeLa cell line, with IC50 values of 7.42 ± 0.34 µM and 10.27 ± 1.26 µM; and moderate effects on MCF-7 (IC50 values, 36.67 ± 1.23 µM and 43.83 ± 0.65 µM) and Caco-2 (IC50 values, 35.83 ± 0.55 µM and 39.03 ± 4.38 µM, respectively) cell lines. They were also more selectively cytotoxic than vincristine against the cancer cell lines, when compared with cytotoxicity against the normal lung cell line MRC5.


Asunto(s)
Antineoplásicos , Olacaceae , Ácido Oleanólico , Saponinas , Triterpenos , Humanos , Células HeLa , Vincristina , Células CACO-2 , Saponinas/farmacología , Saponinas/química , Triterpenos/farmacología , Triterpenos/química
13.
Fitoterapia ; 170: 105647, 2023 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-37562490

RESUMEN

Oliveria decumbens Vent., an annual herb resistant to harsh environmental conditions, is an aromatic medicinal plant of the Apiaceae family. O. decumbens has numerous pharmacological, food and feed, and cosmetic applications. This species is endemic to Iran, Iraq, and Turkey. Published literature, available until 30 November 2022 on the morphology, phytochemistry, and bioactivity of O. decumbens, has been reviewed, and appraised for the potential therapeutic potential of this species, utilizing the databases, Web of Science, Google Scholar, PubMed, and Dictionary of Natural Products. The search term used was O. decumbens. Some manuscripts were issued on the chemical components of O. decumbens essential oil (EO) and various extracts. The EO of O. decumbens was evaluated for its chemical composition and medicinal potential against various diseases. Thymol and carvacrol constituted the primary oxygenated monoterpenes detected in substantial amounts within the EO. Additionally, diverse metabolites of O. decumbens were examined for their bactericidal, antioxidant, larvicidal, and immunomodulatory effects. This review article discusses morphology, phenology, and geographical distribution of O. decumbens and presents a critical appraisal of its phytochemistry and therapeutic potential as documented in the published literature.


Asunto(s)
Apiaceae , Aceites Volátiles , Plantas Medicinales , Apiaceae/química , Estructura Molecular , Aceites Volátiles/farmacología , Aceites Volátiles/química , Timol , Plantas Medicinales/química , Extractos Vegetales/farmacología , Extractos Vegetales/química , Fitoquímicos/farmacología , Etnofarmacología
14.
Phytochem Anal ; 34(7): 709-728, 2023 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-37392081

RESUMEN

INTRODUCTION: In recent decades, quantitative structure-activity relationship (QSAR) analysis has become an important method for drug design and natural product research. With the availability of bioinformatic and cheminformatic tools, a vast number of descriptors have been generated, making it challenging to select potential independent variables that are accurately related to the dependent response variable. OBJECTIVE: The objective of this study is to demonstrate various descriptor selection procedures, such as the Boruta approach, all subsets regression, the ANOVA approach, the AIC method, stepwise regression, and genetic algorithm, that can be used in QSAR studies. Additionally, we performed regression diagnostics using R software to test parameters such as normality, linearity, residual histograms, PP plots, multicollinearity, and homoscedasticity. RESULTS: The workflow designed in this study highlights the different descriptor selection procedures and regression diagnostics that can be used in QSAR studies. The results showed that the Boruta approach and genetic algorithm performed better than other methods in selecting potential independent variables. The regression diagnostics parameters tested using R software, such as normality, linearity, residual histograms, PP plots, multicollinearity, and homoscedasticity, helped in identifying and diagnosing model errors, ensuring the reliability of the QSAR model. CONCLUSION: QSAR analysis is vital in drug design and natural product research. To develop a reliable QSAR model, it is essential to choose suitable descriptors and perform regression diagnostics. This study offers an accessible, customizable approach for researchers to select appropriate descriptors and diagnose errors in QSAR studies.

15.
Phytochem Anal ; 34(7): 855-868, 2023 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-37337376

RESUMEN

INTRODUCTION: Azadirachta indica A. Juss. is a well-known medicinal plant that has been used traditionally to cure various ailments in every corner of the globe. There are many in vitro and in vivo experimental evidences in connection with the bioactivity of the extracts of this plant. Lung cancer is the deadliest form of cancer and contributes to the most cancer related deaths. The mode of action of anticancer components of this plant is still to be established explicitly. OBJECTIVE: The objective of this study is to identify druggable targets of active constituents of A. indica A. Juss. for non-small cell lung cancer (NSCLC) using network pharmacology and validation of activity through molecular docking analysis. METHODOLOGY: Targets of all the active phytochemicals from A. indica were predicted and genes related to NSCLC were retrieved. A protein-protein interaction (PPI) network of the overlapping genes were prepared. Various databases and servers were employed to analyse the disease pathway enrichment analysis of the clustered genes. Validation of the gene/protein activity was achieved by performing molecular docking, and ADMET profiling of selected phytocompounds was performed. RESULT: Gene networking revealed three key target genes as EGFR, BRAF and PIK3CA against NSCLC by the active components of A. indica. Molecular docking and ADMET analysis further validated that desacetylnimbin, nimbandiol, nimbin, nimbinene, nimbolide, salannin and vepinin are the best suited anti- NSCLC among all the phytocompounds present in this plant. CONCLUSION: The present study has provided a better understanding of the pharmacological effects of active components from A. indica and its potential therapeutic effect on NSCLC.


Asunto(s)
Azadirachta , Carcinoma de Pulmón de Células no Pequeñas , Neoplasias Pulmonares , Simulación del Acoplamiento Molecular , Carcinoma de Pulmón de Células no Pequeñas/tratamiento farmacológico , Carcinoma de Pulmón de Células no Pequeñas/genética , Azadirachta/química , Farmacología en Red , Neoplasias Pulmonares/tratamiento farmacológico , Neoplasias Pulmonares/genética
16.
Plants (Basel) ; 12(9)2023 May 08.
Artículo en Inglés | MEDLINE | ID: mdl-37176968

RESUMEN

The yield-reduction effect of abiotic stressors such as salinity and heat stresses with the growing world population threatens food security. Although adverse effects of salinity and heat stress on plant growth and production parameters have been documented, in nature, abiotic stresses occur sequentially or simultaneously. In this study, the stress tolerance and yield capacity of Yukinkomai, YNU31-2-4, and YNU SL rice genotypes tested under control (26 °C, 0 mM NaCl), salinity (26 °C, 75 mM NaCl), heat (31 °C, 0 mM NaCl), and heat and salinity (31 °C, 75 mM NaCl) stress combinations at vegetative and reproductive stages with six different scenarios. The results show that salinity and the heat and salinity combination stresses highly reduce plant growth performance and yield capacity. Heat stress during reproduction does not affect the yield but reduces the grain quality. The YNU31-2-4 genotype performs better under heavy salt and heat and salinity stress then the Yukinkomai and YNU SL genotypes. YNU31-2-4 genotypes accumulate less Na+ and more K+ under salt and multiple stresses. In the YNU31-2-4 genotype, low Na+ ion accumulation increases photosynthetic activity and pigment deposition, boosting the yield. Stress lowers the glucose accumulation in dry seeds, but the YNU31-2-4 genotype has a higher glucose accumulation.

17.
Food Sci Nutr ; 11(3): 1553-1562, 2023 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-36911838

RESUMEN

Phoenix sylvestris Roxb. (Arecaceae) seeds are used in the treatment of diabetes in the traditional system of medicine. The present study evaluated antihyperglycemic and antioxidant activities as well as the total phenolic and flavonoid content of the methanol extract of P. sylvestris seeds (MEPS). The constituents of the extract were identified by GC-MS analysis. MEPS demonstrated strong antioxidant activity against 2,2-diphenyl-1-picrylhydrazyl (DPPH) (IC50 = 162.70 ± 14.99 µg) and nitric oxide (NO) (IC50 = 101.56 ± 9.46 µg/ml) free radicals. It also possesses a substantial amount of phenolics and flavonoids. It significantly (p < .05) reduced blood glucose levels in glucose-loaded and alloxan-induced diabetic mice at the doses of 150 and 300 mg/kg b.w., respectively. A total of 46 compounds were detected and identified by gas chromatography-mass spectroscopy (GC-MS) analysis, among which 8-methylisoquinoline N-oxide (32.82%) was predominant. The phytochemical study by GC-MS revealed that the MEPS possesses compounds which could be related to its antidiabetic and antioxidant activities. To recapitulate, P. sylvestris seeds can be a very good option for antidiabetic and antioxidant activity though further studies are still recommended to figure out the responsible phytochemicals and establish their exact mechanism of action.

18.
Acta Med Okayama ; 77(1): 1-9, 2023 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-36849140

RESUMEN

Inducible resistance to the macrolide, lincosamide, and streptogramin B (iMLSB) antibiotic family is a latent mechanism for antimicrobial resistance in Staphylococcus aureus. We here investigated the frequency and genotypic profiles of iMLSB resistance in clindamycin (CLDM)-susceptible S. aureus isolated in Okayama University Hospital from June 2020 to June 2021. We phenotypically screened the iMLSB resistance via D-zone test and performed PCR testing for the erythromycin ribosomal methylase (erm) genes: ermA and ermC. Among 432 CLDM-susceptible S. aureus isolates, 138 (31.9%) exhibited an iMLSB-resistance phenotype, with methicillinresistant S. aureus isolates (MRSA; 61 isolates: 58.6%) exhibiting higher positivity than methicillin-sensitive S. aureus isolates (MSSA; 77 isolates: 23.5%) (p<0.001). Male patients had a higher frequency of iMLSB resistance than females (OR [95%CI]: 1.8 [1.2-2.8]; p=0.007). Genotypically, ermA predominated in both MSSA (70.1%) and MRSA (86.9%) compared to ermC (14.3% in MSSA and 11.5% in MRSA). A single strain of MRSA possessed both ermA and ermC, while 12 (15.6%) MSSA isolates were negative for both ermA and ermC, suggesting the presence of other genetic mechanisms. Collectively, these results show that approximately 33% of CLDM-susceptible S. aureus isolates at our university hospital exhibited iMLSB resistance, predominantly caused by ermA in both MSSA and MRSA.


Asunto(s)
Clindamicina , Infecciones Estafilocócicas , Femenino , Humanos , Masculino , Antibacterianos/farmacología , Clindamicina/farmacología , Hospitales Universitarios , Lincosamidas/farmacología , Macrólidos/farmacología , Prevalencia , Infecciones Estafilocócicas/tratamiento farmacológico , Infecciones Estafilocócicas/epidemiología , Staphylococcus aureus/genética , Estreptogramina B/farmacología , Japón/epidemiología
19.
Plant Physiol Biochem ; 196: 542-555, 2023 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-36774910

RESUMEN

Salinity is a serious environmental problem that limits plant yield in almost half of the agricultural fields. The hitomebore salt tolerant 1(hst1) is a mutant B-type response regulator gene that was reported to improve salinity tolerance in the 'YNU31-2-4' (YNU) genotype. The sister line (SL) is salt-sensitive, and the nearest genomic relative of the YNU plant has the OsRR22 gene, which is the non-mutant form of the hst1 gene. Biochemical and comprehensive transcriptome analysis of SL and YNU plants was performed to clarify the salinity tolerance mechanism(s) mediated by the hst1 gene. The hst1 gene reduced Na+ ions, lipid peroxidation, and H2O2 content, and improve proline and antioxidant enzymes activities under salt stress. Various transporter and gene-specific transcriptional regulator genes up-regulated in presence of the hst1 gene under saline conditions, identifying that post-stress transcription factors (OsbHLH056, OsH43, OsGRAS29, and OsMADS1) contributed to improved salinity tolerance in YNU plants. Specifically, OsSalT, miR156, and OsLPT1.16 genes were up-regulated, while upstream (OsHKs and OsHPs) and downstream regulators of the OsRR22 gene were down-regulated in YNU plants under saline conditions. Notably, the transcription factors reprogramming, upstream and downstream genes, indicate that these pathways are transcriptionally regulated by the hst1 gene. The findings of the regulatory role of the hst1 gene on plant transcriptome provide a greater understanding of hst1-mediated salt tolerance in rice plants. This knowledge will contribute to understanding the salinity tolerance mechanisms in rice and the evolution of salt-tolerant crops with the ability to withstand higher salinity to ensure food security during climate change.


Asunto(s)
Oryza , Tolerancia a la Sal , Tolerancia a la Sal/genética , Oryza/metabolismo , Factores de Transcripción/genética , Factores de Transcripción/metabolismo , Antioxidantes/metabolismo , Peróxido de Hidrógeno/metabolismo , Salinidad , Estrés Fisiológico/genética , Regulación de la Expresión Génica de las Plantas
20.
Molecules ; 27(24)2022 Dec 11.
Artículo en Inglés | MEDLINE | ID: mdl-36557918

RESUMEN

Arbutin, a hydroquinone glucoside, has been detected in ca. 50 plant families, especially in the plants of the Asteraceae, Ericaceae, Proteaceae and Rosaceae families. It is one of the most widely used natural skin-whitening agents. In addition to its skin whitening property, arbutin possesses other therapeutically relevant biological properties, e.g., antioxidant, antimicrobial and anti-inflammatory, as well as anticancer potential. This review presents, for the first time, a comprehensive overview of the distribution of arbutin in the plant kingdom and critically appraises its therapeutic potential as an anticancer agent based on the literature published until the end of August 2022, accessed via several databases, e.g., Web of Science, Science Direct, Dictionary of Natural Products, PubMed and Google Scholar. The keywords used in the search were arbutin, cancer, anticancer, distribution and hydroquinone. Published outputs suggest that arbutin has potential anticancer properties against bladder, bone, brain, breast, cervix, colon, liver, prostate and skin cancers and a low level of acute or chronic toxicity.


Asunto(s)
Antineoplásicos , Arbutina , Femenino , Humanos , Arbutina/farmacología , Arbutina/uso terapéutico , Hidroquinonas , Glucósidos , Antineoplásicos/farmacología , Antineoplásicos/uso terapéutico
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