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1.
Chem Biodivers ; 21(6): e202400331, 2024 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-38578839

RESUMEN

Euphorbia antiquorum L. is a small plant in the Euphorbiaceae family that is found primarily in tropical and subtropical Asia. It has a long tradition of being utilized in Chinese, Ayurvedic, and other traditional systems for a variety of ailments. To date, More than 116 bioactive constituents were isolated from Euphorbia antiquorum, with diterpenoids being the most abundant. Extracts and isolated chemicals from various portions of the plant have demonstrated significant pharmacological activities such as anti-inflammatory, analgesic, antidiabetic, anticancer etc. It is necessary to conduct an in-depth investigation of the phytochemicals along with the pharmacological properties of E. antiquorum. This review summarised the knowledge of ethnobotany, phytochemistry and pharmacological activities of the plant which will provide a better understanding to clarify the traditional uses of the species and its relation to modern pharmacology which will ultimately pave the way for its clinical application.


Asunto(s)
Etnobotánica , Euphorbia , Fitoquímicos , Euphorbia/química , Humanos , Fitoquímicos/farmacología , Fitoquímicos/química , Fitoquímicos/aislamiento & purificación , Extractos Vegetales/química , Extractos Vegetales/farmacología , Extractos Vegetales/aislamiento & purificación , Animales , Antiinflamatorios/farmacología , Antiinflamatorios/química , Antiinflamatorios/aislamiento & purificación
2.
J Org Chem ; 80(8): 3891-901, 2015 Apr 17.
Artículo en Inglés | MEDLINE | ID: mdl-25807000

RESUMEN

A formal synthesis of the antiasthma drug montelukast sodium is described, wherein the key chiral diol intermediate was accessed with greater convergence of the C-C bond-forming steps as compared to previous routes. Improved synthetic efficiency was achieved by deploying homogeneous metal-based catalysis in two pivotal steps. In the first, a tandem Mizoroki-Heck reaction and double-bond isomerization between a previously known allyl alcohol intermediate and a hindered 2-(2-halophenyl)propan-2-ol secured direct access to the 3-(2-(2-hydroxypropan-2-yl)phenyl)-1-phenylpropan-1-one moiety in the product. In the second step, asymmetric hydrogenation of the ketone functionality in the Mizoroki-Heck reaction product provided a convenient method to introduce the benzylic alcohol chiral center and obtain the desired chiral diol precursor of montelukast sodium. A detailed catalyst screening led to the identification of ((R)-Xyl-BINAP)((R,R)-DPEN)RuCl2 as a catalyst that afforded an enantioselectivity of 99% ee in the hydrogenation step on a multigram lab scale at a molar substrate:catalyst loading of 5000:1.


Asunto(s)
Acetatos/síntesis química , Antiasmáticos/síntesis química , Complejos de Coordinación/química , Quinolinas/síntesis química , Acetatos/química , Antiasmáticos/química , Catálisis , Ciclopropanos , Hidrogenación , Estructura Molecular , Quinolinas/química , Rutenio/química , Sodio/química , Estereoisomerismo , Sulfuros
3.
Med Oncol ; 41(7): 164, 2024 May 30.
Artículo en Inglés | MEDLINE | ID: mdl-38816663

RESUMEN

The Wnt/ß-Catenin pathway (Wnt/ß-CatP) is implicated in accelerating carcinogenesis and cancer progression, contributing to increased morbidity and treatment resistance. Even though it holds promise as a focus for cancer treatment, its intricate nature and diverse physiological effects pose significant challenges. Recent years have witnessed significant advancements in this domain, with numerous natural products demonstrating promising preclinical anti-tumor effects and identified as inhibitors of the Wnt/ß-CatP through various upstream and downstream mechanisms. This study provides a comprehensive overview of the current landscape of Wnt/ß-Cat-targeted cancer therapy, examining the impact of natural products on Wnt/ß-Cat signaling in both cancer prevention and therapeutic contexts. A comprehensive search was conducted on scientific databases like SciFinder, PubMed, and Google Scholar to retrieve relevant literature on Wnt-signaling, natural products, ß-Catenin (ß-Cat), and cancer from 2020 to January 2024. As per the analysis of the relevant reference within the specified period, it has been noted that a total of 58 phytoconstituents, predominantly phenolics, followed by triterpenoids and several other classes, along with a limited number of plant extracts, have exhibited activity targeting the Wnt/ß-CatP. Most ß-Cat regulating modulators restrict cancer cell development by suppressing ß-Cat expression, facilitating proteasomal degradation, and inhibiting nuclear translocation. Multiple approaches have been devised to block the activity of ß-Cat in cancer therapy, a key factor in cancer progression, leading to the discovery of various Wnt/ß-CatP regulators. However, their exploration remains limited, necessitating further research using clinical models for potential clinical use in cancer prevention and therapeutics.


Asunto(s)
Productos Biológicos , Neoplasias , Vía de Señalización Wnt , Humanos , Productos Biológicos/uso terapéutico , Productos Biológicos/farmacología , Neoplasias/tratamiento farmacológico , Neoplasias/prevención & control , Neoplasias/metabolismo , Vía de Señalización Wnt/efectos de los fármacos , beta Catenina/metabolismo , Animales
4.
Artículo en Inglés | MEDLINE | ID: mdl-38549520

RESUMEN

Overproduction of reactive nitrogen and oxygen species (RNS and ROS) has been linked to the pathogenesis of diabetes, hypertension, hyperlipidemia, stroke, angina, and other cardiovascular diseases. These species are produced in part by the mitochondrial respiratory chain, NADPH oxidase, and xanthine oxidase. RNS and ROS both contribute to oxidative stress, which is necessary for the development of cardiovascular disorders. In addition to ROS species like hydroxyl ion, hydrogen peroxide, and superoxide anion, RNS species like nitric oxide, peroxynitrous acid, peroxynitrite, and nitrogen dioxide radicals have also been linked to a number of cardiovascular conditions. They promote endothelial dysfunction, vascular inflammation, lipid peroxidation, and oxidative damage, all of which contribute to the development of cardiovascular pathologies. It's crucial to understand the mechanisms that result in the production of RNS and ROS in order to identify potential therapeutic targets. Redox biomarkers serve as indicators of oxidative stress, making them crucial tools for diagnosing and predicting cardiovascular states. The advancements in proteomics, metabolomics, genomics, and transcriptomics have made the identification and detection of these small molecules possible. The following redox biomarkers are notable examples: 3-nitrotyrosine, 4-hydroxy-2-nonenal, 8- iso-prostaglandin F2, 8-hydroxy-2-deoxyguanosine, malondialdehyde, Diacron reactive oxygen metabolites, total thiol, and specific microRNAs (e.g. miRNA199, miRNA21, miRNA1254, miRNA1306-5p, miRNA26b-5p, and miRNA660-5p) are examples. Although redox biomarkers have great potential, their clinical applicability faces challenges. Redox biomarkers frequently have a short half-life and exist in small quantities in the blood, making them challenging to identify and measure. The interpretation of biomarker data may also be influenced by confounding factors and the complex interplay of various oxidative stress pathways. Therefore, in-depth validation studies and the development of sensitive and precise detection methods are needed to address these problems. In the search for redox biomarkers, cutting-edge techniques like mass spectrometry, immunoassays, and molecular diagnostics are applied. New platforms and technologies have made it possible to accurately detect and monitor redox biomarkers, which facilitates their use in clinical settings. Our expanding knowledge of RNS and ROS involvement in cardiovascular disorders has made it possible to develop redox biomarkers as diagnostic and prognostic tools. Overcoming the challenges associated with their utility and utilizing advanced detection techniques, which will improve their clinical applicability, will ultimately benefit the management and treatment of cardiovascular conditions.

5.
CrystEngComm ; 2013(21): 4221-4224, 2013 Jun 07.
Artículo en Inglés | MEDLINE | ID: mdl-24701132

RESUMEN

The first synthesis and structural elucidation of Ag(I) ternary complexes with 1,2-diazines and chelating heteroarenes have been described. Conserved modes of inter-cation Ag+⋯π and π⋯π stacking interactions result in near identical patterns of cation self-assembly in these ternary complexes.

6.
Ren Fail ; 35(10): 1412-7, 2013.
Artículo en Inglés | MEDLINE | ID: mdl-24001301

RESUMEN

Cisplatin is a popular anticancer drug, but its side effects like nephrotoxicity and hepatotoxicity due to oxidative stress limited its clinical use. In tis study, nephoprotective effect of fractions of Leea asiatica (Leeaceae) leaves was assessed against cisplatin induced toxicity in rats. Leaves of L. asiatica extracted with methanol, ethyl acetate, petroleum ether, and evaluated for in vitro and ex vivo antioxidant activity using several assay models. Methanol extract showed better antioxidant effects, and contain higher amount of phenolic (77.75 ± 0.87 mg GAE/g of dry material) and flavonoid compound (60.98 ± 0.58 mg QE/g of dry material) compared with other extracts. Hance methanol extract was selected for further investigation and fractionated with methanol, ethyl acetate, petroleum ether. Protective effect of methanol extract and its fractions was evaluated against cisplatin (20 mg/kg, i.p.) induced nephrotoxicity. Pretreatment with methanol extract (150 and 300 mg/kg), and its fractions especially methanol, ethyl acetate fraction (75 and 150 mg/kg) significantly reduced blood urea nitrogen, serum creatinine, uric acid levels, and decreased malondialdehyde level and increase total protein and albumin level (p < 0.05, 0.01). Ethyl acetate fraction produced highest nephroprotective, possibly by inhibiting lipid peroxidation process. Result suggested that ethyl acetate fraction possesses potent nephroprotective activity and can be used an adjunct therapy aiming to improve the effectiveness of several nephrotoxic drugs.


Asunto(s)
Antineoplásicos/toxicidad , Cisplatino/toxicidad , Enfermedades Renales/prevención & control , Fitoterapia , Extractos Vegetales/uso terapéutico , Vitaceae/química , Animales , Antioxidantes/análisis , Evaluación Preclínica de Medicamentos , Flavonoides/análisis , Enfermedades Renales/inducido químicamente , Ratones , Fenoles/análisis , Hojas de la Planta/química , Ratas , Vitaceae/toxicidad
7.
Artículo en Inglés | MEDLINE | ID: mdl-24098200

RESUMEN

The title compound, C11H8O5, features a 'skipped' diene, an anti-bis-(epoxide) and a cyclic carbonate, all embedded in a densely functionalized [4.4.3]propellane scaffold. The crystal packing of this diepoxide is effected primarily by C-H⋯O hydrogen bonds, which link the mol-ecules into tapes along the b axis. Inter-tape connectivity is brought about by centrosymmetrically disposed pairs of C⋯O contacts [3.183 (4) Å] between the C(δ+)=O(δ-) dipoles of neighbouring carbonate moieties.

8.
Pharm Biol ; 51(4): 426-32, 2013 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-23336600

RESUMEN

CONTEXT: Pisonia aculeata leaves (Nyctagenaceae), a Folk medicinal plant used in the treatment of several inflammation, pain, and oxidative stress associated diseases. OBJECTIVE: To evaluate anti-inflammatory, analgesic, and antioxidant potential of crude methanol extract of P. aculeata leaves (MEPA). MATERIALS AND METHODS: Analgesic and anti-inflammatory activities of MEPA (250 and 500 mg/kg) were evaluated using writhing, formalin, hot plate, tail flick, carrageenan-induced paw edema test, and membrane stabilizing activity. Free radical scavenging activity, total phenolic and flavonoid contents of MEPA were also determined using standard methods. RESULTS: Oral administration of MEPA showed significant (p < 0.001) inhibition of paw edema, pronounced at 4 h and 5 h after carrageenan injection, and at 200 µg/mL exerts 77.67 and 38.51% protective effect against hypotonic solution and heat induced hemolysis, respectively. MEPA (250 and 500 mg/kg) produced 35.21 and 79.14% inhibition of acetic acid-induced writhing. Furthermore, MEPA (500 mg/kg) inhibited 49.19% early and 73.14% late phase of formalin-induced hypernociception. In contrast, a lower dose of MEPA did not prevent hot plate induced nociception, while in the tail immersion method, pronounced analgesic activity was observed between 1 and 4 h postdosing. The extract possesses significant in vitro antioxidant activity and a lipid peroxidation inhibition effect. Total phenolic and total flavonoid content in MEPA were 87.99 ± 0.87 mg GAE/g and 58.98 ± 0.01 mg QE/g, respectively. DISCUSSION AND CONCLUSION: Our findings confirmed the analgesic, anti-inflammatory and antioxidant activities of Pisonia aculeata leaves. Contents of flavonoids and phenolic compounds in extract could be correlated with its observed biological activities.


Asunto(s)
Analgésicos/farmacología , Antiinflamatorios/farmacología , Antioxidantes/farmacología , Inflamación/prevención & control , Nyctaginaceae , Estrés Oxidativo/efectos de los fármacos , Dolor/prevención & control , Ácido Acético , Administración Oral , Analgésicos/administración & dosificación , Analgésicos/química , Analgésicos/aislamiento & purificación , Animales , Antiinflamatorios/administración & dosificación , Antiinflamatorios/química , Antiinflamatorios/aislamiento & purificación , Antioxidantes/administración & dosificación , Antioxidantes/química , Antioxidantes/aislamiento & purificación , Carragenina , Modelos Animales de Enfermedad , Relación Dosis-Respuesta a Droga , Flavonoides/aislamiento & purificación , Formaldehído , Calor , Inflamación/inducido químicamente , Peroxidación de Lípido/efectos de los fármacos , Medicina Tradicional , Metanol/química , Ratones , Nyctaginaceae/química , Dolor/etiología , Fenoles/aislamiento & purificación , Hojas de la Planta , Plantas Medicinales , Solventes/química , Factores de Tiempo
9.
Curr Top Med Chem ; 23(24): 2277-2299, 2023.
Artículo en Inglés | MEDLINE | ID: mdl-37649298

RESUMEN

BACKGROUND: Dibru-Saikhowa National Park and Biosphere Reserve (DSNPBR), Assam, India, is a part of biodiversity hotspots and a store house of many orchid species. This systematic review was conducted to document the medicinal importante of orchids available in DSNPBR and to analyse their importance in drug discovery. METHODS: This systematic review was conducted using the Preferred Reporting Items for Systematic Review and Meta-Analysis (PRISMA) guidelines. Scientific databases were used to search relevant literature to document ethnomedicinal uses, pharmacological activity and phytochemistry of orchid species available in DSNPBR. RESULTS: We have analysed 84 articles to document relevant information on 52 orchid species available in DSNPBR. Dendrobium (n = 13) is the top genus. Different orchid species available in DSNPBR were used traditionally in India, Nepal, Bangladesh, and China to cure gastrointestinal disorders, disease-associated pain and inflammation, skin diseases, wound, arthritis, menstrual pain, tuberculosis etc. The pre-clinical investigations confirmed that extract/fraction/isolated compounds of orchids possess antirheumatic, anticancer, antitumor, anti-inflammatory, antidiabetic, antimicrobial, nephroprotective and neuroprotective activities through different mechanisms. Biomolecules isolated from orchid species like Dendrobium nobile alkaloids, polysaccharides have shown a potential to be developed as future drug molecules. Many phytochemicals isolated have demonstrated in vitro anticancer activities. The lack of clinical data in support of the therapeutic effectiveness of orchids is a major limitation. CONCLUSION: Orchids found in DSNPBR hold great significance in traditional culture for their medicinal properties and have been effectively studied for their bioactivities. Nevertheless, to confirm their effectiveness as therapeutics, conducting methodical research, examining their molecular mechanisms, and performing toxicity tests are necessary.

10.
Curr Top Med Chem ; 23(24): 2332-2341, 2023.
Artículo en Inglés | MEDLINE | ID: mdl-37469158

RESUMEN

BACKGROUND: Food grains' ability to promote health is widely recognized as a result of their rich nutritional profile and presence of antioxidants. AIM: The present study aimed to investigate the antioxidant, antidyslipidemic, and cardiac risk preventive effects of unpolished whole rice extracts of Keteki and Kola Joha of Assam, India, and to profile the polyphenolic compounds present. METHODS: Whole unpolished rice samples were extracted with ethanol and the efficacy of the extract of both rice cultivars was evaluated against high-fat and high-sugar induced hyperlipidemia in rats. The effects of extracts on lipid profile, hepatic enzyme, endogenous antioxidants, lipid peroxidation, creatine kinase-NAC, lactate dehydrogenase, C-reactive protein and lipoprotein(s) were evaluated. Atherogenic indices were calculated to find the effect of the extract on cardiac risk. HPLC analysis of whole unpolished rice samples was also carried out to profile the polyphenolics present. RESULTS: HPLC analysis revealed the presence of gallic acid, vanillic acid, caffeic acid, sinapic acid, o-coumaric acid, t-coumaric acid, rosamarinic acid, chlorogenic acid, phytic acid in both rice samples. Protocatechuic acid, syringic acid, and p-coumaric acid were detected in keteki joha, and ferulic acid was detected in kola joha only. Ethanol extracts (200 and 400 mg/kg) of both rice varieties for 30 days significantly averted dyslipidemia, preserved the level of endogenous antioxidants, and prevented lipid peroxidation. Levels of creatine kinase-NAC, lactate dehydrogenase, Creactive protein, and lipoprotein (a) were significantly (P < 0.01) less in the extract-treated group compared to the disease-control group. Extract treatment enhanced ApoA1 level while the reduced level of ApoB. ApoB/ApoA1 ratio was found more in the disease control group, which was significantly reduced in the extract-treated group. The atherogenic index, atherogenic coefficient, and cardiac risk ratio were reduced, while the cardioprotective index was enhanced in treatment groups. CONCLUSION: This paper profiled polyphenolic compounds for the first time. Keteki joha exhibited better results than Kola joha. Observations offer novel insights into the hypothesis for the first time that unpolished Keteki and Kola Joha rice can be beneficial in averting hyperlipidemia and its associated coronary events.

11.
Int J Biol Macromol ; 227: 424-436, 2023 Feb 01.
Artículo en Inglés | MEDLINE | ID: mdl-36549610

RESUMEN

The current work was designed to study the starch's physicochemical attributes, tablet disintegration and dissolution efficiency and its derivatives obtained from the glutinous Assam bora rice (G-ABR) variety of Assam, Northeast India. Starch was isolated by a simple protein denaturation method, and a starch derivative was prepared through citric acid modification. G-ABRS and citrated G-ABRS were characterized through FTIR, DSC, XRD and SEM. The rate of consolidation, consolidation index, angle of internal friction, packing rearrangement and cohesive properties were determined to investigate their applications as functional excipients in pharmaceutical industries. G-ABRS and citrated G-ABRS exhibited better packing rearrangement and cohesive properties than standard corn starch. Furthermore, immediate release of API from the tablet compact was observed when the starch concentration increased from 1 to 5 %, indicating facilitation of the tablet compact disintegration. Therefore, G-ABRS and citrated G-ABRS are potentially functional and sustainable materials for pharmaceutical industries.


Asunto(s)
Oryza , Oryza/química , Solubilidad , Ácido Cítrico , Almidón/química , Comprimidos/química
12.
Int J Biol Macromol ; 240: 124475, 2023 Jun 15.
Artículo en Inglés | MEDLINE | ID: mdl-37076065

RESUMEN

Assam soft rice starch (ASRS) and Citric acid-esterified Assam soft rice starch (c-ASRS) were studied extensively. FTIR, CHN, DSC, XRD, SEM, TEM and optical microscope studies were performed for native and modified starches. Powder rearrangements, cohesiveness and flowability were studied by the Kawakita plot. Moisture and ash content was around 9 % and 0.5 %. In vitro digestibility of ASRS and c-ASRS produced functional RS. Paracetamol tablets were prepared using ASRS and c-ASRS as granulating-disintegrating agents through wet granulation methods. The prepared tablets' physical properties, disintegrant properties, in vitro dissolution and dissolution efficiency (DE) were performed. The average particle size was obtained at 6.59 ± 0.355 µm and 8.15 ± 0.168 µm for ASRS and c-ASRS, respectively. All the results were statistically significant at p < 0.05, p < 0.01 and p < 0.001. The amylose content was 6.78 %, classifying it as a low amylose type of starch. The disintegration time was reduced with the increasing concentration of ASRS and c-ASRS and facilitated the immediate release of the model drug from the tablet compact to improve its bioavailability. Therefore, the current investigation concludes that ASRS and c-ASRS can be used as novel and functional materials in pharmaceutical industries due to their unique physicochemical attributes. HYPOTHESIS: The central hypothesis of the current work was to develop citrated starch through a one-step reactive extrusion method and investigate its disintegrants property for pharmaceutical tablets. Extrusion is a continuous, simple, high-speed, low-cost, producing very limited wastewater and gas. Characterization was done through different instrumental techniques to confirm successful esterification. The flow properties were evaluated, and tablets were prepared at a different level of ASRS and c-ASRS (disintegrating agent), followed by the evaluation of tablets to confirm the model drug's dissolution and disintegration efficiency. Finally, in vitro digestibility of both ASRS and c-ASRS was analyzed to establish their potential nutritional benefits.


Asunto(s)
Oryza , Almidón Resistente , Amilosa , Ácido Cítrico , Química Farmacéutica , Solubilidad , Almidón/química , Excipientes/química , Comprimidos/química
13.
Curr Top Med Chem ; 23(8): 690-710, 2023.
Artículo en Inglés | MEDLINE | ID: mdl-37114791

RESUMEN

Flavonoids are important bioactive phenolic compounds abundant in plants and exhibit different therapeutic potentials. A wound is a significant problem in diabetic individuals. A hyperglycaemic environment alters the normal wound-healing process and increases the risk of microbial infection, leading to hospitalization, morbidity, and amputation. Flavonoids are an important class of phytochemicals with excellent antioxidant, anti-inflammatory, antimicrobial, antidiabetic, antitumor, and wound healing property. Quercetin, hesperidin, curcumin, kaempferol, apigenin, luteolin, morin, etc. have shown their wound healing potential. Flavonoids effectively exhibit antimicrobial activity, scavenge reactive oxygen species, augment endogenous antioxidants, reduce the expression and synthesis of inflammatory cytokines (i.e. IL-1ß, IL-6, TNF-α, NF-κB), inhibit inflammatory enzymes, enhance anti-inflammatory cytokine (IL-10), enhance insulin section, reduce insulin resistance, and control blood glucose level. Several flavonoids like hesperidin, curcumin, quercetin, rutin, naringin, and luteolin have shown their potential in managing diabetic wounds. Natural products that maintain glucose haemostatic, exert anti-inflammatory activity, suppress/inhibit microbial growth, modulate cytokines, inhibit matrix metalloproteinase (MMP), stimulate angiogenesis and extracellular matrix, and modulate growth factor can be considered as a potential therapeutic lead to treat diabetic wound. Flavonoids were found to play a positive role in management of diabetic wounds by regulating MMP-2, MMP-8, MMP-9, MMP-13, Ras/Raf/ MEK/ERK, PI3K/Akt, and nitric oxide pathways. Therefore, it can be assumed that flavonoids could be potential therapeutics to prevent devastating effects of diabetic wounds. This paper focused on the potential role of flavonoids in managing diabetic wounds and discussed their possible mechanism of action.


Asunto(s)
Curcumina , Diabetes Mellitus , Hesperidina , Humanos , Flavonoides/farmacología , Flavonoides/uso terapéutico , Quercetina , Luteolina , Fosfatidilinositol 3-Quinasas , Citocinas , Antiinflamatorios/farmacología , Antiinflamatorios/uso terapéutico , Diabetes Mellitus/tratamiento farmacológico
14.
World J Clin Cases ; 11(6): 1275-1286, 2023 Feb 26.
Artículo en Inglés | MEDLINE | ID: mdl-36926128

RESUMEN

Metabolic associated fatty liver disorder (MAFLD) characterizes the contributing etiologies (i.e., type 2 diabetes mellitus, metabolic syndrome, overweight) of individuals with fatty liver disease that affects 1/3rd of the world population. In 2020, the coronavirus disease 2019 (COVID-19) crisis was unprecedented, and people with different comorbidities became more susceptible to the infection caused by severe acute respiratory syndrome coronavirus 2. MAFLD patients are frequently obese with added metabolic menace like diabetes, hypertension, and dyslipidemia leading to greater jeopardy of COVID-19. MAFLD patients are 4 to 6-fold more prone towards infections. COVID-19 induces liver injury with elevated levels of aspartate aminotransferase and alanine aminotransferase and insignificantly elevated bilirubin. Hence, MAFLD in COVID-19 patients worsens the condition significantly. The evidence highlighting the interaction between MAFLD and altered liver functioning in COVID-19 suggested that COVID-19 patients with pre-existing MAFLD are at greater risk of morbidity or intensive care unit admission. Direct hepatic injury, enhanced levels of inflammatory cytokines, declined hepatic mitochondrial activity, and compromised immunity are considered as some underlying mechanisms. The main focus of this review is to discuss the implications of metabolic dysfunction associated with fatty liver disease in COVID-19 patients. The review systematically analyzes the effect of striking two worldwide pandemics (MAFLD and COVID-19) together in the present era.

15.
Nat Prod Res ; : 1-6, 2023 Aug 10.
Artículo en Inglés | MEDLINE | ID: mdl-37585696

RESUMEN

Amomum dealbatum Roxb. parts have been traditionally used as remedies for joint pain, diabetes, muscular rheumatism, antiseptic, and abscesses in Arunachal Pradesh, Assam, and Tripura. Ethyl acetate sub-fraction E3 had significantly inhibited the α-glucosidase (IC50 5.385 µg/mL). The molecular docking revealed quercetin-3-O-galactoside to be the most potent α-glucosidase inhibitor (binding energy -43.214 kcal/mol). Using the QSAR model, the pIC50 values of myricetin, gallic acid, quercetin-3-O-galactoside, and acarbose were predicted to be 5.65235, 4.39858, 5.65235, and 6.03058, respectively. For the first time, quercetin-3-O-galactoside, myricetin, and gallic acid have been isolated from the flowers of A. dealbatum (ADF). E3 decreased blood glucose level to a near-normal concentration (100.60 ± 2.94 mg/dL) in comparison to diabetic control rats (575.20 ± 24.80 mg/dL). The results have strongly suggested the potential of ADF in treating diabetes. This lesser-known plant has the potential to uncover its full medicinal properties through further in-depth research.

16.
Chimia (Aarau) ; 66(12): 892-8, 2012.
Artículo en Inglés | MEDLINE | ID: mdl-23394272

RESUMEN

This brief account highlights the notable findings of our investigation into the supramolecular chemistry of conformationally locked polycyclitols in the solid state. The study was aimed at analyzing the crystal packing and unraveling the modalities of non-covalent interactions (particularly, intramolecular vis-à-vis intermolecular O-H˙˙˙O hydrogen bonds) in polyols. The know-how obtained thereof, was successfully utilized to engineer self-assemblies of designer polycyclitols, having hydrogen bond donors and acceptors fettered onto a trans-decalin scaffold. The results seek to draw particular attention to the intrinsic attribute of this rigid carbocyclic framework to lock functional groups into spatially invariant positions and bring potential intramolecular hydrogen bonding partners into favorable interaction geometry to engender predictability in the self-assembly patterns.


Asunto(s)
Polímeros/química , Polímeros/síntesis química , Enlace de Hidrógeno , Sustancias Macromoleculares/síntesis química , Sustancias Macromoleculares/química , Modelos Moleculares , Conformación Molecular
17.
Acta Crystallogr Sect E Struct Rep Online ; 68(Pt 12): o3392-3, 2012 Dec 01.
Artículo en Inglés | MEDLINE | ID: mdl-23476221

RESUMEN

The title compound, C17H24O5, featuring a 2-carbeth-oxy-3-oxepanone unit in its intra-molecularly O-H⋯O hydrogen-bonded enol form, was obtained via [(CF3CO2)2Rh]2-catal-ysed intra-molecular O-H bond insertion in the α-diazo-ω-hy-droxy-ß-ketoester, ethyl 4-[(1S,3aS,6R,6aS)-6-hy-droxy-2,2,3a-trimethyl-3-oxo-octa-hydro-penta-len-1-yl]-2-diazo-3-oxobutano-ate. The seven-membered oxacyclic ring, thus constructed on a cis-fused diquinane platform, was found to adopt a distorted boat-sofa conformation.

18.
Pharm Biol ; 50(2): 247-53, 2012 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-22103691

RESUMEN

CONTEXT: Nephrotoxicity induced by several synthetic drugs is a major problem of modern age. Medicinal plants and phytomedicine are the prime choice of research as they possess better activity and lesser side effects. OBJECTIVE: To investigate the protective effect of Cardiospermum halicacabum Linn. (Sapindaceae), methanol and petroleum ether extracts against acetaminophen-induced nephrotoxicity in rats. MATERIALS AND METHODS: Nephrotoxicity was induced by the administration of acetaminophen suspension (750 mg/kg, p.o.) after the pretreatment with methanol extract (MECF) and petroleum ether extract (PEECF) of Cardiospermum halicacabum for 7 days. Forty-eight h after the acetaminophen administration estimations of serum alkaline phosphate, creatinine, blood urea nitrogen, uric acid, total proteins, cholesterol, albumin level and histological analysis of kidney injuries were determined. RESULTS: In nephrotoxic animals, a significant (P < 0.01) elevation of serum alkaline phosphate, creatinine, blood urea nitrogen, uric acid, cholesterol and depletion of total proteins and albumin were observed. Pretreatment with MECF and PEECF (400 mg/kg) significantly (P < 0.01, P < 0.05) decreased serum alkaline phosphate, creatinine, blood urea nitrogen, uric acid, cholesterol level and causes elevation of total protein and albumin level, though MECF produces better effect than PEECF in rats. Histopathological studies also confirm the protective effect of extracts. The protective effect of Cardiospermum halicacabum was associated with restoration of serum alkaline phosphate, creatinine, blood urea nitrogen, uric acid, cholesterol, total protein and albumin level. DISCUSSION AND CONCLUSIONS: Methanol and petroleum ether extracts of Cardiospermum halicacabum had a significant nephroprotective activity against acetaminophen-induced nephrotoxicity in rats.


Asunto(s)
Acetaminofén/toxicidad , Enfermedades Renales/prevención & control , Extractos Vegetales/farmacología , Sapindaceae/química , Alcanos/química , Analgésicos no Narcóticos/toxicidad , Animales , Nitrógeno de la Urea Sanguínea , Enfermedades Renales/inducido químicamente , Pruebas de Función Renal , Metanol/química , Ratas , Ratas Wistar , Solventes/química
19.
Int J Biol Macromol ; 206: 681-698, 2022 May 01.
Artículo en Inglés | MEDLINE | ID: mdl-35247430

RESUMEN

Currently, research on natural products is facing challenging future in various aspects. A large group of natural polysaccharides such as ß-glucan, cellulose, hemicellulose, chitin, pectin, agaropectin, heteroglycans, lignins, hydrocolloids, homopolysaccharides, heteropolysaccharides were studied extensively for their various therapeutical potential. Several research works have already demonstrated those polysaccharides has tremendous health benefits, and found to exhibit anticancer, antiviral, immunomodulatory, antimicrobial, anticoagulant, anti-inflammatory, antidiabetic, antioxidant and antitumor activities. Different mushroom, plant, fungus, algae, vegetables, microalgae etc. are some important source of several polysaccharide macromolecules such as glucans, ulvan A, ulvan B, fucoidan, rhamnan sulfate, laminarin sulfate, agar, alginate, heteroglycans. Earlier research work demonstrated that natural polysaccharides have the highest ability to carry biological properties along with some biopolymers like as proteins and nucleic acids due to their structural variability. The preventive effect of these biomacromolecules was extensively studied, especially their beneficial effect on chronic metabolic conditions like dyslipidemia and related disorders. Dyslipidemia is a serious metabolic disorder associated with coronary heart disease, coronary artery diseases, hypercholesterolemia, atherosclerosis, etc. Dietary natural polysaccharides could play an important role in the management and prevention of dyslipidemia. Polysaccharides from natural sources mainly sulfated polysaccharides exhibited predominant lipid-lowering and cholesterol-lowering activities through different mechanisms. Polysaccharides isolated from different edible plants, vegetables, plant, algae, mushroom with higher biological activities, particularly hypolipidemic activity were highlighted in this paper, in a way for their futuristic therapeutic application. This review aims to comprehensively discuss overall advances in hypolipidemic activity of polysaccharides, including their sources, structural characteristic and chemistry, biological activity and their probable mode of action.


Asunto(s)
Agaricales , Hiperlipidemias , Glucanos/química , Humanos , Polisacáridos/química , Polisacáridos/farmacología , Polisacáridos/uso terapéutico , Sulfatos/química
20.
World J Diabetes ; 13(9): 696-716, 2022 Sep 15.
Artículo en Inglés | MEDLINE | ID: mdl-36188143

RESUMEN

Diabetes mellitus is a chronic metabolic disorder resulting in an increased blood glucose level and prolonged hyperglycemia, causes long term health conse-quences. Chronic wound is frequently occurring in diabetes patients due to compromised wound healing capability. Management of wounds in diabetic patients remains a clinical challenge despite many advancements in the field of science and technology. Increasing evidence indicates that alteration of the biochemical milieu resulting from alteration in inflammatory cytokines and matrix metalloproteinase, decrease in fibroblast and keratinocyte functioning, neuropathy, altered leukocyte functioning, infection, etc., plays a significant role in impaired wound healing in diabetic people. Apart from the current pharmacotherapy, different other approaches like the use of conventional drugs, antidiabetic medication, antibiotics, debridement, offloading, platelet-rich plasma, growth factor, oxygen therapy, negative pressure wound therapy, low-level laser, extracorporeal shock wave bioengineered substitute can be considered in the management of diabetic wounds. Drugs/therapeutic strategy that induce angiogenesis and collagen synthesis, inhibition of MMPs, reduction of oxidative stress, controlling hyperglycemia, increase growth factors, regulate inflammatory cytokines, cause NO induction, induce fibroblast and keratinocyte proliferation, control microbial infections are considered important in controlling diabetic wound. Further, medicinal plants and/or phytoconstituents also offer a viable alternative in the treatment of diabetic wound. The focus of the present review is to highlight the molecular and cellular mechanisms, and discuss the drug targets and treatment strategies involved in the diabetic wound.

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