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1.
Food Res Int ; 195: 114970, 2024 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-39277267

RESUMEN

Lupins, and other legumes, have attained international interest due to their reported remarkable health benefits. Currently, the seed coats are discarded as waste or animal feed. The research presented here summarizes the potential for incorporating the seed coats into 'whole grain' foods. We aimed to identify metabolites found in the seed coats of nine commercial Australian cultivars of lupin (Lupinus angustifolius and L. albus species), and to evaluate and compare their functional, nutritional, antioxidant, and antidiabetic properties, along with in silico exploration of mechanisms of action for selected identified secondary metabolites. The seed coats were found to contain 79 to 90% dietary fibers and substantial quantity of essential macrometals. LC-QTOF MS-based, untargeted bioactive metabolite profiling explored a total of 673 chemical entities, and identified 63 bioactive secondary metabolites including: biophenols, unsaturated fatty acids, triterpenoids, alkaloids, and dietary prebiotics (insoluble fibers). The seed coats from these nine cultivars show substantial antioxidant activity. The cultivars of L. angustifolius inhibit α-amylase and α-glucosidase significantly in vitro. Moreover, in silico docking and dynamic simulation along with ADME/T analysis suggest that quercetin 3-methyl ether and 8-C-methylquercetin 3-methyl ether as molecules, novel in lupin seed coats, are responsible for the α-amylase and α-glucosidase inhibition. The findings indicated that lupin seed coats might be beneficial food components, rather than be discarded as 'mill waste'.


Asunto(s)
Antioxidantes , Hipoglucemiantes , Lupinus , Semillas , Antioxidantes/análisis , Semillas/química , Lupinus/química , Hipoglucemiantes/análisis , Simulación por Computador , Fibras de la Dieta/análisis , Valor Nutritivo , Australia , alfa-Amilasas/metabolismo , alfa-Amilasas/antagonistas & inhibidores , Cromatografía Liquida/métodos , Extractos Vegetales/química , Extractos Vegetales/farmacología , Simulación del Acoplamiento Molecular , Inhibidores de Glicósido Hidrolasas/farmacología , Espectrometría de Masas/métodos
2.
Clin Dermatol ; 2024 Sep 09.
Artículo en Inglés | MEDLINE | ID: mdl-39260457

RESUMEN

Mentorship is a critical aspect of personal and professional development throughout anyone's life. Unlike many other fields, a medical career is a long multistep process that can begin in high school and continue throughout a physician's career. When considering competitive specialties such as dermatology, mentors are increasingly crucial in helping students successfully match to programs of their choice, but the variability and extent of mentorship can raise ethical concerns. We discuss the evolution of mentorship in dermatology and the potential ethical issues involved. We propose possible solutions to the ethical conflict between mentor and mentee.

5.
Clin Dermatol ; 42(4): 343-350, 2024.
Artículo en Inglés | MEDLINE | ID: mdl-38281689

RESUMEN

Benign tumors of the eye and eyelid are common in children and adults, and they rarely undergo malignant transformation. Their workup and management have evolved over the years with increasing advancements in surgical and laser therapies. This contribution focuses on describing the following benign eye and eyelid tumors and their diagnostic and treatment approaches: congenital and acquired melanocytic nevi; nevus of Ota (Hori nevus); conjunctival papilloma; seborrheic keratosis; epidermoid cyst; dermoid cyst; milium; xanthelasma; hemangioma (cherry angioma and pyogenic granuloma); neurofibroma; neurilemmoma (schwannoma); and fibroepithelial polyp. Surgical removal is the primary treatment approach for many of these benign tumors. With advancements in laser technologies, there are now several laser types that can be used in the treatment of these benign eye and eyelid tumors. Other treatment modalities include cryosurgery, electrosurgery, and topical or intralesional medications. We hope this review will provide a reference to dermatologists and ophthalmologists in their approach to evaluation and management of benign eye and eyelid tumors.


Asunto(s)
Neoplasias de los Párpados , Humanos , Neoplasias de los Párpados/terapia , Neoplasias del Ojo/terapia , Neoplasias del Ojo/diagnóstico , Quiste Dermoide/terapia , Neurofibroma/terapia , Neurofibroma/cirugía , Hemangioma/terapia , Quiste Epidérmico/terapia , Quiste Epidérmico/diagnóstico , Quiste Epidérmico/cirugía , Nevo Pigmentado/terapia , Queratosis Seborreica/terapia , Queratosis Seborreica/diagnóstico , Neurilemoma/terapia , Terapia por Láser , Xantomatosis/terapia
6.
Pharmaceuticals (Basel) ; 16(12)2023 Dec 18.
Artículo en Inglés | MEDLINE | ID: mdl-38139868

RESUMEN

BACKGROUND: Advancements in nanoscience have led to a profound paradigm shift in the therapeutic applications of medicinally important natural drugs. The goal of this research is to develop a nano-natural product for efficient cancer treatment. METHODS AND RESULTS: For this purpose, mesoporous silica nanoparticles (MSNPs) were formulated, characterized, and loaded with caffeine to develop a targeted drug delivery system, i.e., caffeine-coated nanoparticles (CcNPs). In silico docking studies were conducted to examine the binding efficiency of the CcNPs with different apoptotic targets followed by in vitro and in vivo bioassays in respective animal models. Caffeine, administered both as a free drug and in nanomedicine form, along with doxorubicin, was delivered intravenously to a benzene-induced AML model. The anti-leukemic potential was assessed through hematological profiling, enzymatic biomarker analysis, and RT-PCR examination of genetic alterations in leukemia markers. Docking studies show strong inter-molecular interactions between CcNPs and apoptotic markers. In vitro analysis exhibits statistically significant antioxidant activity, whereas in vivo analysis exhibits normalization of the genetic expression of leukemia biomarkers STMN1 and S1009A, accompanied by the restoration of the hematological and morphological traits of leukemic blood cells in nanomedicine-treated rats. Likewise, a substantial improvement in hepatic and renal biomarkers is also observed. In addition to these findings, the nanomedicine successfully normalizes the elevated expression of GAPDH and mTOR induced by exposure to benzene. Further, the nanomedicine downregulates pro-survival components of the NF-kappa B pathway and upregulated P53 expression. Additionally, in the TRAIL pathway, it enhances the expression of pro-apoptotic players TRAIL and DR5 and downregulates the anti-apoptotic protein cFLIP. CONCLUSIONS: Our data suggest that MSNPs loaded with caffeine, i.e., CcNP/nanomedicine, can potentially inhibit transformed cell proliferation and induce pro-apoptotic TRAIL machinery to counter benzene-induced leukemia. These results render our nanomedicine as a potentially excellent therapeutic agent against AML.

7.
Cells ; 12(21)2023 10 31.
Artículo en Inglés | MEDLINE | ID: mdl-37947635

RESUMEN

As Australian lupin cultivars are rich sources of polyphenols, dietary fibers, high-quality proteins, and abundant bioactive compounds with significant antioxidant, antidiabetic, and anticancer activities, this research work is aimed at investigating the colon cancer alleviation activity of nine cultivars of lupin seeds on HCT116 and HT29 colon carcinoma cell lines through anti-proliferation assay, measurement of apoptosis, and identification of the mechanism of apoptosis. Nine cultivars were pre-screened for anti-proliferation of HCT116 and HT29 cells along with consideration of the impact of heat processing on cancer cell viability. Mandelup and Jurien showed significant inhibition of HCT116 cells, whereas the highest inhibition of HT29 cell proliferation was attained by Jurien and Mandelup. Processing decreased the anti-proliferation activity drastically. Lupin cultivars Mandelup, Barlock, and Jurien (dose: 300 µg/mL) induced early and late apoptosis of colon cancer cells in Annexin V-FITC assay. The mechanism of apoptosis was explored, which involves boosting of caspases-3/7 activation and intracellular reactive oxygen species (ROS) generation in HCT116 cells (Mandelup and Barlock) and HT29 cells (Jurien and Mandelup). Thus, the findings showed that lupin cultivars arrest cell cycles by inducing apoptosis of colorectal carcinoma cells triggered by elevated ROS generation and caspases-3/7 activation.


Asunto(s)
Apoptosis , Neoplasias del Colon , Humanos , Especies Reactivas de Oxígeno/metabolismo , Australia , Neoplasias del Colon/patología , Células HCT116 , Caspasas/metabolismo
8.
J Clin Aesthet Dermatol ; 15(8): 38-40, 2022 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-36061484

RESUMEN

Objective: Dermatopathology training is incorporated into dermatology residency programs, yet some individuals choose to pursue additional fellowship training in dermatopathology. We sought to characterize the impact of dermatopathology training on practice patterns of dermatologists performing pathology exams in the Medicare population. Methods: We conducted a cross-sectional review of the 2017 Medicare Public Use File to identify all residency-trained dermatologists performing microscopic pathology exams in 2017. Formal dermatopathology fellowship training was identified through the American Board of Medical Specialties website. Results: There were 2,150 dermatologists performing pathology examinations in 2017; of these, 592 (27.5%) had formal dermatopathology fellowship training. Fellowship training was associated with a higher mean annual pathology exam volume. Those without fellowship training were more likely to practice in the West, in non-academic settings, and in non-metropolitan counties. Limitations: Residency-trained pathologists are not included in the sample. Additionally, some dermatopathology labs may submit claims as an entire organization, rather than at the level of each physician. Conclusion: Fellowship-trained dermatopathologists perform pathology exams at a higher rate than their non-fellowship-trained colleagues and are concentrated in academic practice settings. The findings support the important role of fellowship-trained dermatopathologists in evaluating a wide array of skin pathologies.

9.
Biol Futur ; 73(2): 219-227, 2022 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-35318616

RESUMEN

Different gentian preparations are used as traditional remedies for internal pain control in: Persian traditional medicine (PTM), Chinese traditional medicine (CTM) and Ancient Greek medicine (AGM) from the time of the Roman Empire. Objective: To present a survey of the ethnopharmacological applications of gentians recorded as being used in Eastern and Western traditional medical systems (PTM, CTM and AGM) and their pharmacological effects, chemical composition as well as an in silico investigation of the possible active component/s for the alleviation of internal pain via molecular docking studies. Major traditional medicine literature (PTM, CTM and AGM, 50 AD- 1770) and ethnobotanical studies for the application of gentians were reviewed. Nine European species representing 5 of the 13 sections currently attributed to Gentiana were selected. Chemical compounds and pharmacological activity data of these species were gathered from different databases including Google Scholar, PubChem, PubMed and Web of Science (between 1972 and 2020). The possible active constituents of gentians on visceral pain receptors were investigated, in silico. In all investigated literature, traditional uses of gentian were indicated to have anti-nociceptive effects on visceral pain and possess diuretic action. According to our computational study, acylated flavonoid glycosides, viz. trans-feruloyl-2"-isovitexin (33), trans-feruloyl-2"-isovitexin-4'-O-ß-D-glucoside (34), iso-orientin-4'-O-glucoside (38), trans-caffeoyl-2"-iso-orientin-4'-O-ß-D-glucoside (39), iso-orientin-2"-O-ß-D-glucoside (40) and isoscoparin (41), might be responsible for visceral pain reduction by interacting with the purinergic receptor (P2X3) and vanilloid receptor 1 (TrpV1). This finding shows a good correlation with different traditional gentian uses in Persian, Chinese and European ethnomedicine for visceral pain control.


Asunto(s)
Gentiana , Dolor Visceral , Glucósidos , Simulación del Acoplamiento Molecular , Fitoterapia
10.
Chemosphere ; 293: 133515, 2022 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-34990716

RESUMEN

Endocrine-disrupting compounds (EDCs), as well as microplastics, have drawn global attention due to their presence in the aquatic ecosystem and persistence in wastewater treatment plants (WWTPs). In the present study, for simultaneous bio-removal of two EDCs, 17α-ethinylestradiol (EE2), bisphenol A (BPA), and a microplastic, polypropylene (PP) four kinds of periphytic biofilms were employed. Additionally, the effect of humic acid (HA) on the removal efficacy of these biofilms was evaluated. It was observed that EE2 and BPA (0.2 mg L-1 each) were completely (∼100%) removed within 36 days of treatment; and the biodegradation of EE2, BPA, and PP was significantly enhanced in the presence of HA. Biodegradation of EE2 and BPA was evaluated through Ultra-high performance liquid chromatography (UHPLC), and Gas chromatography coupled with tandem mass spectrometry (GC-MS/MS) was used to determine the mechanism of degradation. Gel permeation chromatography (GPC) and SEM had validated the biodegradation of PP (5.2-14.7%). MiSeqsequencing showed that the community structure of natural biofilm changed after the addition of HA, as well as after the addition of EDCs and PP. This change in community structure might be a key factor regarding variable biodegradation percentages. The present study revealed the potential of periphytic biofilms for the simultaneous removal of pollutants of different chemical natures, thus provides a promising new method for wastewater treatment applications.


Asunto(s)
Disruptores Endocrinos , Microbiota , Perifiton , Contaminantes Químicos del Agua , Disruptores Endocrinos/análisis , Etinilestradiol/análisis , Cromatografía de Gases y Espectrometría de Masas , Sustancias Húmicas/análisis , Microplásticos , Plásticos , Espectrometría de Masas en Tándem , Contaminantes Químicos del Agua/análisis
11.
J Nat Med ; 76(2): 490-503, 2022 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-35032247

RESUMEN

In diabetes, interactions between AGEs (advanced glycation end products) and RAGEs (receptors of AGEs) are responsible for chronic complications and the current work reports the potential of ursolic acid as a RAGE inhibitor. The three-dimensional crystal structure of RAGE was first docked with target molecules by 'AutodockVina' using GROMOS 96 4381 parameters. Druggability and pharmacokinetic properties were calculated from the SwissADME server. In vitro bovine serum albumin (BSA)-glucose fluorescence and BSA-methylglyoxal fluorescence assays were also performed. Finally, alloxan-induced diabetic mice were administered ursolic acid and metformin standards (at 1, 50, 100 mg/kg) for 50 days. Blood glucose levels, several blood parameters, blood lipid profiles, supernatants of homogenized kidney and plasma of mice were examined. In the computational study, ursolic acid showed greater binding affinity (-7.5 kcal/mol) for RAGE with an ADMET profiles and lead-likeness compared to metformin as a standard antidiabetic. In the in vitro fluorescence assays, the IC50 value for ursolic acid was much less than that of metformin standard. During the in vivo study, significant reduction in the levels of blood glucose, HbA1C (glycated hemoglobin), creatinine, uric acid, BUN (blood urea nitrogen), AST (aspartate aminotransferase), ALT (alanine aminotransferase), ALP (alkaline phosphatase) were observed in the ursolic acid and metformin-treated mice. Substantial inhibition of AGEs' formation in the plasma and kidney were also detected. Finally, the histopathological examinations of the kidney revealed reversal of cellular necrosis. Hence, ursolic acid is proved to be a potent AGE inhibitory agent in managing the diabetic complications.


Asunto(s)
Complicaciones de la Diabetes , Diabetes Mellitus Experimental , Triterpenos , Animales , Complicaciones de la Diabetes/tratamiento farmacológico , Diabetes Mellitus Experimental/inducido químicamente , Productos Finales de Glicación Avanzada/metabolismo , Ratones , Receptor para Productos Finales de Glicación Avanzada , Triterpenos/farmacología , Triterpenos/uso terapéutico , Ácido Ursólico
12.
J Am Acad Dermatol ; 86(3): 515-524, 2022 03.
Artículo en Inglés | MEDLINE | ID: mdl-34915056

RESUMEN

Despite advances in early detection as described in part 1 of this continuing medical education series, melanoma continues to be a large contributor to cutaneous cancer-related mortality. In a subset of patients with unresectable or metastatic disease, surgical clearance is often not possible; therefore, systemic and local therapies are considered. The second article in this series provides dermatologists with an up-to-date working knowledge of the treatment options that may be prescribed by oncologists for patients with unresectable stage III, stage IV, and recurrent melanoma.


Asunto(s)
Melanoma/terapia , Recurrencia Local de Neoplasia/terapia , Neoplasias Cutáneas/terapia , Educación Médica Continua , Humanos , Inmunoterapia , Melanoma/patología , Recurrencia Local de Neoplasia/patología , Neoplasias Cutáneas/patología
13.
J Am Acad Dermatol ; 86(3): 503-512, 2022 03.
Artículo en Inglés | MEDLINE | ID: mdl-34915058

RESUMEN

In response to rising rates of melanoma worldwide, novel noninvasive melanoma detection techniques are emerging to facilitate the early detection of melanoma and decrease unnecessary biopsies of benign pigmented lesions. Because they often report similar study findings, it may be difficult to determine how best to incorporate these technologies into clinical practice based on their supporting studies alone. The first article in this continuing medical education series provides practical advice on how and when to use various noninvasive melanoma detection techniques in clinical practice.


Asunto(s)
Melanoma , Neoplasias Cutáneas , Biopsia , Dermoscopía/métodos , Humanos , Melanoma/diagnóstico , Melanoma/patología , Microscopía Confocal/métodos , Sensibilidad y Especificidad , Neoplasias Cutáneas/diagnóstico , Neoplasias Cutáneas/patología
14.
Bioresour Technol ; 347: 126421, 2022 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-34838961

RESUMEN

This study presents an approach for developing periphytic biofilm with N-acyl-homoserine-lactones (AHLs) stimulation and lanthanum (La, a rare earth element) loading, to achieve highly efficient and stable phosphorus (P) recovery from wastewater. AHLs stimulated biofilm growth and formation, also improved stable P entrapment by enhancing extracellular polymeric substance (EPS) production and optimizing P-entrapment bacterial communities. Periphytic biofilms loading La is based on ligand exchanges, and La loading achieved initial rapid P entrapment by surface adsorption. The combination of AHLs stimulation and La loading achieved 99.0% P entrapment. Interestingly, the enhanced EPS production stimulated by AHLs protected biofilms against La. Moreover, a method for P and La separately recovery from biofilms was developed, achieving 89-96% of P and 88-93% of La recovery. This study offers a promising biotechnology to reuse La from La-rich wastewater and recover P by biofilm doped with La, which results in a win-win situation for resource sustainability.


Asunto(s)
Acil-Butirolactonas , Homoserina , Biopelículas , Biotecnología , Matriz Extracelular de Sustancias Poliméricas , Lantano , Fósforo , Percepción de Quorum
15.
Sci Rep ; 11(1): 21515, 2021 11 02.
Artículo en Inglés | MEDLINE | ID: mdl-34728683

RESUMEN

Lupin holds an important place among the legumes and the utilization of lupin as a dietary protein source is an excellent environmentally friendly alternative to animal-based products for human nutrition. In the present study, nutritional, thermal, rheological and functional properties of nine Australian lupin cultivars have been assayed in order to find the most valuable one, both nutritiously and industrially. The set comprised six Lupinus angustifolius L. viz., Barlock, Gunyadi, Jenabillup, Jindalee, Jurien, Mandelup and three Lupinus albus L. viz., Luxor, Rosetta, WK388 cultivars. The tests included analysis of color, macronutrient and micronutrient composition, pasting, textural and thermal properties, electrophoretic profile of protein isolates, swelling power, water and oil absorption capacity, emulsifying capacity, emulsion stability, creaming stability, foaming capacity and stability of the cultivars' dehulled seed flours. The results indicated substantial variation in macro and micro-nutritional value as well as satisfactory swelling ability, solubility, surface hydrophobicity, foaming ability, emulsifying capacity and gelation property of lupin flours. Superior nutritional, thermal, rheological and functional potential was demonstrated by the L. albus cultivars compared to the L. angustifolius cultivars with the exception of Mandelup.


Asunto(s)
Proteínas en la Dieta/metabolismo , Harina/análisis , Lupinus/metabolismo , Valor Nutritivo , Proteínas de Plantas/metabolismo , Reología , Semillas/metabolismo , Australia , Humanos , Lupinus/química , Semillas/química
16.
Clin Dermatol ; 39(5): 840-846, 2021.
Artículo en Inglés | MEDLINE | ID: mdl-34785011

RESUMEN

Vitamin D is a steroid hormone of importance to the field of dermatology. Skin is unique in that it is the site of vitamin D synthesis upon sun exposure and a target organ for its activity. We explore the physiology and metabolic mechanism of action of vitamin D, as well as its effects on the skin. We also discuss the current evidence of the efficacy and safety of oral and topical vitamin D analogues on skin conditions such as psoriasis, atopic dermatitis, vitiligo, sunburn, actinic keratosis, and fibrosing skin disorders. Based on currently available scientific evidence, the National Academy of Medicine's recommended dietary allowance for vitamin D ranges from 400 IU to 800 IU daily based on age categories.


Asunto(s)
Psoriasis , Quemadura Solar , Humanos , Psoriasis/tratamiento farmacológico , Piel , Vitamina D , Vitaminas/uso terapéutico
17.
Sci Total Environ ; 801: 149708, 2021 Dec 20.
Artículo en Inglés | MEDLINE | ID: mdl-34438149

RESUMEN

Dissolved organic matter (DOM) plays vital roles in carbon and other nutrient transformation at soil-water interfaces (SWI) in paddy fields. It is associated with the growth and withering of periphytic biofilms. However, the interactions between DOM and periphytic biofilms remain largely unknown. In this study, a microcosm experiment with different initial DOM contents elucidated that the biomass, and biomass nitrogen and phosphorus contents were greatly influenced by humic-like substances (C2 and C3), while the growth of periphytic biofilms increased the contents of humic-like (C1 and C2) and tryptophan-like substances (C5) in soil. Moreover, the decomposition of periphytic biofilms significantly increased soil pH, DOM, C2, C3 and C5 contents, but caused decrease in Eh, with consequent reduce in water soluble phosphorus (WSP) and release of algal available phosphorus (AAP). Results from this study revealed how DOM interacts with periphytic biofilms and the consequent effects on changes of bioactive phosphorus fractions, and provide practical information for designing periphytic biofilm based biofertilizer from the perspective of soil DOM.


Asunto(s)
Fósforo , Suelo , Biopelículas , Sustancias Húmicas/análisis , Nitrógeno/análisis , Espectrometría de Fluorescencia , Agua
18.
J Am Acad Dermatol ; 85(4): 841-846, 2021 10.
Artículo en Inglés | MEDLINE | ID: mdl-34116095

RESUMEN

BACKGROUND: Melanoma is one of the most commonly diagnosed malignancies in the United States and is responsible for the majority of deaths from skin cancer. OBJECTIVE: Since the 1970s, the incidence of melanoma has risen appreciably while melanoma-specific mortality has remained stable. This has raised a debate about potential overdiagnosis of melanoma. Herein, we review temporal trends in melanoma incidence and mortality and explore factors that may contribute to observed trends, including an aging population in the United States, ultraviolet exposure, increased numbers of biopsies by dermatologists and physician extenders, skin cancer screenings, histopathology criteria, and historic underdiagnosis. Additionally, we discuss melanoma overdiagnosis and the extent to which it may contribute to current trends. METHODS: The literature was reviewed. RESULTS: Several factors may contribute to an increased incidence of melanoma, including an aging population, ultraviolet exposure, increased skin biopsies, skin cancer screenings, histopathologic criteria, historic underdiagnosis, and current overdiagnosis. LIMITATIONS: Further studies are required to determine exactly which tumors are being overdiagnosed, and how to improve patient outcomes with adjustment to physician's practice. CONCLUSION: The rise in the incidence of melanoma observed since the 1970s is likely multifactorial.


Asunto(s)
Melanoma , Neoplasias Cutáneas , Anciano , Humanos , Incidencia , Melanoma/diagnóstico , Melanoma/epidemiología , Sobrediagnóstico , Piel , Neoplasias Cutáneas/diagnóstico , Neoplasias Cutáneas/epidemiología , Estados Unidos/epidemiología
19.
J Ethnopharmacol ; 273: 113975, 2021 Jun 12.
Artículo en Inglés | MEDLINE | ID: mdl-33652111

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: Functional disability associated with rheumatoid arthritis (RA), a chronic inflammatory autoimmune disease is a challenging concern in healthcare systems. Along with environmental factors and epigenetic disorders, multiple pathways are reported as prominent mechanism for the progression of RA symptoms including; pain, swelling and stiffness of joints. Elaeocarpus floribundus Blume has been used as a folklore medicine for RA from ancient times. This plant harbours a suite of endophytic fungi that produce a range of metabolites of potential interest. Thus, for the establishment of a scientific basis for this folklore use, it is essential to find out the involvement, if any, of the endophytic fungi living in this plant and the metabolites they elaborate, for the management of RA. AIM OF THE STUDY: This study was designed to isolate, identify and evaluate the in vitro anti-inflammatory and in vivo antinociceptive and antiarthritic activities of the compounds produced by the endophytic fungi living in different parts of Elaeocarpus floribundus Blume. MATERIALS AND METHODS: Endophytic fungi from different parts of the plant were isolated and cultured for the production of secondary metabolites. Chromatographically fractionated fungal extracts were assessed for anti-inflammatory and antinociceptive activities. For the evaluation of anti-inflammatory activity, in vitro cyclooxygenase (COX1/COX2) and 5-lipoxygenase (5-LOX) inhibitory assays were performed. For the evaluation of in vivo antinociceptive activity, hot plate acetic acid induced writhing, and formalin induced paw licking methods were adopted, whereas complete Freund's adjuvant (CFA) induced poly-arthritic method was adopted for the evaluation of antiarthritic activity. The most effective fraction was analyzed by liquid chromatography-mass spectroscopy (LC-MS) in search of the bioactive extracellular metabolites. RESULTS: Five endophytic fungi viz. Aspergillus fumigatus, Aspergillus niger, Rhizoctonia oryzae, Rhizopus oryzae, and Syncephalastrum racemosum were isolated. COX1/COX2 and 5-LOX inhibitory assays state that the Aspergillus niger fraction possesses the greatest activity against these enzymes of inflammatory process. In vivo antinociceptive showed significant (***P<0.001) reduction of pain in a dose dependent manner. As well, significant (***P<0.001) reduction of paw volume was observed in CFA induce poly-arthritic test. LC/MS analysis of the Aspergillus niger fraction revealed the presence of bioactive compounds including tensyuic acid, hexylitaconic acid, chlorogenic acid, nigragillin, TMC-256C1, asnipyrone B, asperenone, fumaric acid and fusarubin, all having reported pharmacological activities. CONCLUSION: The present study demonstrates that secondary metabolites produced by endophytic fungi living in various parts of Elaeocarpus floribundus Blume had potential to relief pain and inflammation. The endophytes were found to contain multiple biomolecules effective in rheumatoid arthritis. These findings provide a rationale for the folklore use of the plant in the management of rheumatoid arthritis.


Asunto(s)
Analgésicos/farmacología , Antiinflamatorios/farmacología , Elaeocarpaceae/microbiología , Endófitos/química , Hongos/química , Analgésicos/química , Animales , Antiinflamatorios/química , Araquidonato 5-Lipooxigenasa/metabolismo , Inhibidores de la Ciclooxigenasa/química , Inhibidores de la Ciclooxigenasa/farmacología , Femenino , Inhibidores de la Lipooxigenasa , Masculino , Ratones , Estructura Molecular , Dolor/tratamiento farmacológico
20.
J Ethnopharmacol ; 270: 113781, 2021 Apr 24.
Artículo en Inglés | MEDLINE | ID: mdl-33421602

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: Phragmites karka (Retz.) of family Poaceae is a pristine tropical plant that is well known to the local healers for ailments of diabetes, fever, diarrhea and CNS depression but lacks the scientific evidence behind its traditional usage. Hence, we explicated this plant to find the scientific basis of its traditional utilization. AIM OF THE STUDY: The current study aims to find out the antidiabetic potential, toxicity after oral administration and in vitro cytotoxic activity of aerial parts of the plant on HeLa cells. METHODS: The plant was extracted with methanol by maceration and the crude extract was then subjected to solvent partitioning with modified Kupchan method for preparing several fractions. Phytochemical screening and total phenolic content of the plant was first determined through established procedures. Acute toxicity of the plant was studied by orally administering a single high dose (5000 mg/kg) of drug. Cytotoxicity of the methanolic plant extract was determined by measuring the percentage of cell viability on human cervical cancer cell lines, HeLa. In vitro antidiabetic activity was determined through iodine starch and DNSA (3,5-dinitrosalicylic acid) method of α-amylase inhibition. Finally, in vivo oral glucose tolerance test and alloxan induced antidiabetic activity test was performed at 150 and 300 mg/kg body weight doses of plant extract to confirm the in vivo antidiabetic activity. RESULTS: No mortality was demonstrated by Phragmites karka in the acute toxicity test. However, signs of cellular toxicity was observed and histopathological studies on major organs exhibited necrosis in liver and kidney. In vitro cytotoxicity assay revealed the death of HeLa cells by DCM (dichloromethane) and n-hexane fractions of plant extract at 100 and 10 µg/mL concentrations. The IC50 value of the fractions were later evaluated by MTT assay (316.1 and 96.7 µg/mL for n-hexane and DCM fractions, respectively). In the iodine starch and DNSA method of α-amylase enzyme inhibitory activity test, substantial inhibition of enzyme was observed with the IC50 values of 2.05 and 2.08 mg/mL, respectively. In the in vivo antidiabetic activity test, considerable reduction in blood glucose level of diabetic mice was detected in both oral glucose tolerance test and alloxan induced antidiabetic activity test. In addition, the microscopic examination of pancreas showed noticeable recovery of pancreatic ß cells and the blood lipid profile analysis represented a significant (p < 0.05) reduction of total cholesterol, LDL (low density lipoprotein) and triglyceride level in plant extract treated mice. CONCLUSION: Results of this study reveals that the Phragmites karka extract is toxic at cellular level after oral administration and cytotoxic when tested on HeLa cells. The plant also evidenced hypoglycemic property, possibly through the inhibition of α-amylase enzyme and recovered the pancreatic beta cells along with the improvement of lipid profile of diabetic mice. However, robust studies on this plant is required to isolate the bioactive compounds, elucidate structures and evaluate their mechanism of actions in support of our findings. CLASSIFICATION: Toxicology and Safety, Quality Traditional Medicine.


Asunto(s)
Citotoxinas/farmacología , Diabetes Mellitus Experimental/tratamiento farmacológico , Hipoglucemiantes/farmacología , Componentes Aéreos de las Plantas/química , Extractos Vegetales/farmacología , Poaceae/química , Animales , Bangladesh , Glucemia/efectos de los fármacos , Citotoxinas/uso terapéutico , Femenino , Células HeLa , Humanos , Hipoglucemiantes/uso terapéutico , Concentración 50 Inhibidora , Lípidos/sangre , Masculino , Medicina Tradicional , Ratones , Páncreas/efectos de los fármacos , Páncreas/patología , Fenol/análisis , Fitoquímicos/análisis , Extractos Vegetales/uso terapéutico , Ratas Wistar , alfa-Amilasas/antagonistas & inhibidores
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