Your browser doesn't support javascript.
loading
Mostrar: 20 | 50 | 100
Resultados 1 - 20 de 39
Filtrar
1.
Molecules ; 28(1)2023 Jan 03.
Artigo em Inglês | MEDLINE | ID: mdl-36615596

RESUMO

To increase its operational stability and ongoing reusability, B. subtilis pectinase was immobilized on iron oxide nanocarrier. Through co-precipitation, magnetic iron oxide nanoparticles were synthesized. Scanning electron microscopy (SEM) and energy dispersive electron microscopy (EDEX) were used to analyze the nanoparticles. Pectinase was immobilized using glutaraldehyde as a crosslinking agent on iron oxide nanocarrier. In comparison to free pectinase, immobilized pectinase demonstrated higher enzymatic activity at a variety of temperatures and pH levels. Immobilization also boosted pectinase's catalytic stability. After 120 h of pre-incubation at 50 °C, immobilized pectinase maintained more than 90% of its initial activity due to the iron oxide nanocarrier, which improved the thermal stability of pectinase at various temperatures. Following 15 repetitions of enzymatic reactions, immobilized pectinase still exhibited 90% of its initial activity. According to the results, pectinase's catalytic capabilities were enhanced by its immobilization on iron oxide nanocarrier, making it economically suitable for industrial use.


Assuntos
Enzimas Imobilizadas , Nanopartículas de Magnetita , Enzimas Imobilizadas/metabolismo , Estabilidade Enzimática , Glutaral , Poligalacturonase/metabolismo , Concentração de Íons de Hidrogênio , Nanopartículas Magnéticas de Óxido de Ferro , Temperatura , Cinética
2.
Molecules ; 28(20)2023 Oct 18.
Artigo em Inglês | MEDLINE | ID: mdl-37894632

RESUMO

In this research, we focused on the production of amylose-lipid nanocomposite material (ALN) through a green synthesis technique utilizing high-speed homogenization. Our aim was to investigate this novel material's distinctive physicochemical features and its potential applications as a low-glycemic gelling and functional food ingredient. The study begins with the formulation of the amylose-lipid nanomaterial from starch and fatty acid complexes, including stearic, palmitic, and lauric acids. Structural analysis reveals the presence of ester carbonyl functionalities, solid matrix structures, partial crystallinities, and remarkable thermal stability within the ALN. Notably, the ALN exhibits a significantly low glycemic index (GI, 40%) and elevated resistance starch (RS) values. The research extends to the formulation of ALN into nanocomposite hydrogels, enabling the evaluation of its anthocyanin absorption capacity. This analysis provides valuable insights into the rheological properties and viscoelastic behavior of the resulting hydrogels. Furthermore, the study investigates anthocyanin encapsulation and retention by ALN-based hydrogels, with a particular focus on the influence of pH and physical cross-link networks on the uptake capacity presenting stearic-acid (SA) hydrogel with the best absorption capacity. In conclusion, the green-synthesized (ALN) shows remarkable functional and structural properties. The produced ALN-based hydrogels are promising materials for a variety of applications, such as medicine administration, food packaging, and other industrial purposes.


Assuntos
Amilose , Nanocompostos , Amilose/química , Hidrogéis/química , Antocianinas , Amido/química , Nanocompostos/química , Nanogéis
3.
Medicina (Kaunas) ; 59(10)2023 Oct 10.
Artigo em Inglês | MEDLINE | ID: mdl-37893523

RESUMO

Background and Objectives: We have recently reported that Fluvastatin, Atorvastatin, Simvastatin and Rosuvastatin have calcium channel antagonistic activities using rabbits' intestinal preparations. The current study is focused on the effects of Pitavastatin and Lovastatin for possible inhibition of vascular L-Type calcium channels, which may have vasorelaxant effect(s). Combined effects of Pitavastatin and Lovastatin in the presence of Amlodipine were also tested for vasorelaxation. Materials and Methods: Possible relaxing effects of Pitavastatin and Lovastatin on 80 mM Potassium chloride (KCL)-induced contractions and on 1 µM norepinephrine (N.E)-induced contractions were studied in isolated rabbit's aortic strips preparations. Relaxing effects on 80 mM KCL-induced vascular contractions were further verified by constructing Calcium Concentration Response Curves (CCRCs), in the absence and presence of three different concentrations of Pitavastatin and Lovastatin using CCRCs as negative control. Verapamil was used as a standard drug that has L-Type calcium channel binding activity. In other series of experiments, we studied drug interaction(s) among Pitavastatin, Lovastatin, and amlodipine. Results: The results of this study imply that Lovastatin is more potent than Pitavastatin for having comparatively lower EC50 (7.44 × 10-5 ± 0.16 M) in intact and (4.55 × 10-5 ± 0.10 M) in denuded aortae for KCL-induced contractions. Lovastatin amplitudes in intact and denuded aortae for KCL-induced contractions were, respectively, 24% and 35.5%; whereas amplitudes for Pitavastatin in intact and denuded aortae for KCL-induced contractions were 34% and 40%, respectively. A left shift in the EC50 values for the statins was seen when we added amlodipine in EC50 (Log Ca++ M). Right shift for CCRCs state that Pitavastatin and Lovastatin have calcium channel antagonistic effects. Lovastatin in test concentration (6.74 × 10-7 M) produced a right shift in relatively lower EC50 (-2.5 ± 0.10) Log Ca++ M as compared to Pitavastatin, which further confirms that lovastatin is relatively more potent. The right shift in EC50 resembles the right shift of Verapamil. Additive effect of Pitavastatin and Lovastatin was noted in presence of amlodipine (p < 0.05). Conclusions: KCL (80 mM)-induced vascular contractions were relaxed by Pitavastatin and Lovastatin via inhibitory effects on L-Type voltage-gated calcium channels. Lovastatin and Pitavastatin also relaxed Norepinephrine (1 µM)-induced contractions giving an insight for involvement of dual mode of action of Pitavastatin and Lovastatin.


Assuntos
Inibidores de Hidroximetilglutaril-CoA Redutases , Vasodilatadores , Animais , Coelhos , Anlodipino/farmacologia , Inibidores de Hidroximetilglutaril-CoA Redutases/farmacologia , Inibidores de Hidroximetilglutaril-CoA Redutases/uso terapêutico , Lovastatina/farmacologia , Lovastatina/uso terapêutico , Bloqueadores dos Canais de Cálcio/farmacologia , Canais de Cálcio/metabolismo , Verapamil/farmacologia , Norepinefrina/farmacologia
4.
Medicina (Kaunas) ; 59(6)2023 May 25.
Artigo em Inglês | MEDLINE | ID: mdl-37374229

RESUMO

Background and Objectives: We have recently reported that stains have calcium channel blocking activity in isolated jejunal preparations. In this study, we examined the effects of atorvastatin and fluvastatin on blood vessels for a possible vasorelaxant effect. We also studied the possible additional vasorelaxant effect of atorvastatin and fluvastatin, in the presence of amlodipine, to quantify its effects on the systolic blood pressure of experimental animals. Materials and Methods: Atorvastatin and fluvastatin were tested in isolated rabbits' aortic strip preparations using 80mM Potassium Chloride (KCl) induced contractions and 1 micro molar Norepinephrine (NE) induced contractions. A positive relaxing effect on 80 mM KCl induced contractions were further confirmed in the absence and presence of atorvastatin and fluvastatin by constructing calcium concentration response curves (CCRCs) while using verapamil as a standard calcium channel blocker. In another series of experiments, hypertension was induced in Wistar rats and different test concentrations of atorvastatin and fluvastatin were administered in their respective EC50 values to the test animals. A fall in their systolic blood pressure was noted using amlodipine as a standard vasorelaxant drug. Results: The results show that fluvastatin is more potent than amlodipine as it relaxed NE induced contractions where the amplitude reached 10% of its control in denuded aortae. Atorvastatin relaxed KCL induced contractions with an amplitude reaching 34.4% of control response as compared to the amlodipine response, i.e., 39.1%. A right shift in the EC50 (Log Ca++ M) of Calcium Concentration Response Curves (CCRCs) implies that statins have calcium channel blocking activity. A right shift in the EC50 of fluvastatin with relatively less EC50 value (-2.8 Log Ca++ M) in the presence of test concentration (1.2 × 10-7 M) of fluvastatin implies that fluvastatin is more potent than atorvastatin. The shift in EC50 resembles the shift of Verapamil, a standard calcium channel blocker (-1.41 Log Ca++ M). Conclusions: Atorvastatin and fluvastatin relax the aortic strip preparations predominantly through the inhibition of voltage gated calcium channels in high molar KCL induced contractions. These statins also inhibit the effects of NE induced contractions. The study also confirms that atorvastatin and fluvastatin potentiate blood pressure lowering effects in hypertensive rats.


Assuntos
Bloqueadores dos Canais de Cálcio , Inibidores de Hidroximetilglutaril-CoA Redutases , Ratos , Coelhos , Animais , Bloqueadores dos Canais de Cálcio/farmacologia , Bloqueadores dos Canais de Cálcio/uso terapêutico , Atorvastatina/farmacologia , Atorvastatina/uso terapêutico , Fluvastatina/farmacologia , Fluvastatina/uso terapêutico , Vasodilatadores/farmacologia , Inibidores de Hidroximetilglutaril-CoA Redutases/farmacologia , Inibidores de Hidroximetilglutaril-CoA Redutases/uso terapêutico , Anlodipino/farmacologia , Anlodipino/uso terapêutico , Cálcio , Pressão Sanguínea , Ratos Wistar , Verapamil/farmacologia , Canais de Cálcio/farmacologia , Cloreto de Potássio/farmacologia
5.
Pak J Pharm Sci ; 36(3(Special)): 953-961, 2023 May.
Artigo em Inglês | MEDLINE | ID: mdl-37587704

RESUMO

This study is carried out to assess the effects of rosuvastatin and simvastatin on blood vessels for possible vasorelaxant effect. The study is also translating the possible vasorelaxant effect in Wistar rats for a subsequent fall in systolic blood pressure. It is evident from the EC50, that rosuvastatin is more effective on relaxing N.E induced contractions, while simvastatin is more effective on relaxing KCL induced contractions. Simvastatin is equipotent when compared to effects of amlodipine on KCl induced contractions in denuded aortae. Simvastatin produced significant right shift in test concentration 1.1× 10-6M with its respective EC50 -1.85logCa++M as compared to its respective control EC50 -3logCa++M. Rosuvastatin also produced significant right shift in the EC50. In conclusion, it is stated that rosuvastatin and simvastatin relax the aortic strips preparations through inhibition of voltage gated calcium channels and inhibition of N.E induced contractions. Rosuvastatin and simvastatin have additive effects when used in the presence of a standard vaso-relaxant drug like amlodipine, which further confirms its additive effect on decreasing the systolic blood pressure of hypertensive rats (P<0.05).


Assuntos
Anlodipino , Anti-Hipertensivos , Animais , Ratos , Ratos Wistar , Anti-Hipertensivos/farmacologia , Anlodipino/farmacologia , Rosuvastatina Cálcica/farmacologia , Sinvastatina/farmacologia , Vasodilatação , Vasodilatadores/farmacologia
6.
Molecules ; 27(14)2022 Jul 07.
Artigo em Inglês | MEDLINE | ID: mdl-35889221

RESUMO

This study reports the isolation of three new C20 diterpenoid alkaloids, Chitralinine A-C (1-3) from the aerial parts of Delphinium chitralense. Their structures were established on the basis of latest spectral techniques and single crystal X-rays crystallographic studies of chitralinine A described basic skeleton of these compounds. All the isolated Compounds (1-3) showed strong, competitive type inhibition against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) in comparison to standard allanzanthane and galanthamine however, chitralinine-C remained the most potent with IC50 value of 11.64 ± 0.08 µM against AChE, and 24.31 ± 0.33 µM against BChE, respectively. The molecular docking reflected a binding free energy of -16.400 K Cal-mol-1 for chitralinine-C, having strong interactions with active site residues, TYR334, ASP72, SER122, and SER200. The overall findings suggest that these new diterpenoid alkaloids could serve as lead drugs against dementia-related diseases including Alzheimer's disease.


Assuntos
Alcaloides , Delphinium , Diterpenos , Acetilcolinesterase/metabolismo , Alcaloides/química , Butirilcolinesterase/metabolismo , Inibidores da Colinesterase/química , Delphinium/química , Diterpenos/química , Simulação de Acoplamento Molecular
7.
Molecules ; 27(11)2022 Jun 06.
Artigo em Inglês | MEDLINE | ID: mdl-35684582

RESUMO

This study was designed to evaluate the emulsifying and rheological properties of acorn protein isolate (API) in different pH mediums (pH 3, 7 and 9) and in the presence of ionic salts (1 M NaCl and 1 M CaCl2). API shows higher solubility in distilled water at pH 7, while at the same pH, a decrease in solubility was observed for API in the presence of CaCl2 (61.30%). A lower emulsifying activity index (EAI), lower stability index (ESI), larger droplet sizes and slight flocculation were observed for API in the presence of salts at different pHs. Importantly, CaCl2 treated samples showed relevantly higher EAI (252.67 m2/g) and ESI (152.67 min) values at all pH as compared to NaCl (221.76 m2/g), (111.82 min), respectively. A significant increase in interfacial protein concentration (4.61 mg/m2) was observed for emulsion at pH 9 with CaCl2, while the major fractions of API were observed in an interfacial layer after SDS-PAGE analysis. All of the emulsion shows shear thinning behavior (τc > 0 and n < 1), while the highest viscosity was observed for emulsion prepared with CaCl2 at pH 3 (11.03 ± 1.62). In conclusion, API, in the presence of ionic salts at acidic, neutral and basic pH, can produce natural emulsions, which could be substitutes for synthetic surfactants for such formulations.


Assuntos
Quercus , Sais , Cloreto de Cálcio , Emulsificantes/química , Emulsões/química , Concentração de Íons de Hidrogênio , Proteínas , Reologia , Cloreto de Sódio
8.
Molecules ; 27(8)2022 Apr 11.
Artigo em Inglês | MEDLINE | ID: mdl-35458662

RESUMO

Alzheimer's disease is an emerging health disorder associated with cognitive decline and memory loss. In this study, six curcumin analogs (1a−1f) were synthesized and screened for in vitro cholinesterase inhibitory potential. On the basis of promising results, they were further investigated for in vivo analysis using elevated plus maze (EPM), Y-maze, and novel object recognition (NOR) behavioral models. The binding mode of the synthesized compounds with the active sites of cholinesterases, and the involvement of the cholinergic system in brain hippocampus was determined. The synthesized curcumin analog 1d (p < 0.001, n = 6), and 1c (p < 0.01, n = 6) showed promising results by decreasing retention time in EPM, significantly increasing % SAP in Y-maze, while significantly (p < 0.001) enhancing the % discrimination index (DI) and the time exploring the novel objects in NORT mice behavioral models. A molecular docking study using MOE software was used for validation of the inhibition of cholinesterase(s). It has been indicated from the current research work that the synthesized curcumin analogs enhanced memory functions in mice models and could be used as valuable therapeutic molecules against neurodegenerative disorders. To determine their exact mechanism of action, further studies are suggested.


Assuntos
Curcumina , Escopolamina , Acetilcolinesterase/metabolismo , Amnésia/induzido quimicamente , Amnésia/tratamento farmacológico , Animais , Colinérgicos , Inibidores da Colinesterase/farmacologia , Inibidores da Colinesterase/uso terapêutico , Colinesterases , Modelos Animais de Doenças , Aprendizagem em Labirinto , Camundongos , Simulação de Acoplamento Molecular , Escopolamina/efeitos adversos
9.
Molecules ; 26(23)2021 Nov 26.
Artigo em Inglês | MEDLINE | ID: mdl-34885751

RESUMO

Cognitive decline in dementia is associated with deficiency of the cholinergic system. In this study, five mono-carbonyl curcumin analogs were synthesized, and on the basis of their promising in vitro anticholinesterase activities, they were further investigated for in vivo neuroprotective and memory enhancing effects in scopolamine-induced amnesia using elevated plus maze (EPM) and novel object recognition (NOR) behavioral mice models. The effects of the synthesized compounds on the cholinergic system involvement in the brain hippocampus and their binding mode in the active site of cholinesterases were also determined. Compound h2 (p < 0.001) and h3 (p < 0.001) significantly inhibited the cholinesterases and reversed the effects of scopolamine by significantly reducing TLT (p < 0.001) in EPM, while (p < 0.001) increased the time exploring the novel object. The % discrimination index (DI) was significantly increased (p < 0.001) in the novel object recognition test. The mechanism of cholinesterase inhibition was further validated through molecular docking study using MOE software. The results obtained from the in vitro, in vivo and ex vivo studies showed that the synthesized curcumin analogs exhibited significantly higher memory-enhancing potential, and h3 could be an effective neuroprotective agent. However, more study is suggested to explore its exact mechanism of action.


Assuntos
Amnésia/tratamento farmacológico , Colinesterases/efeitos dos fármacos , Disfunção Cognitiva/tratamento farmacológico , Curcumina/farmacologia , Demência/tratamento farmacológico , Amnésia/induzido quimicamente , Amnésia/diagnóstico por imagem , Amnésia/patologia , Animais , Domínio Catalítico/efeitos dos fármacos , Colinérgicos/síntese química , Colinérgicos/química , Colinérgicos/farmacologia , Inibidores da Colinesterase/síntese química , Inibidores da Colinesterase/química , Inibidores da Colinesterase/farmacologia , Disfunção Cognitiva/induzido quimicamente , Disfunção Cognitiva/diagnóstico por imagem , Disfunção Cognitiva/patologia , Curcumina/análogos & derivados , Curcumina/síntese química , Curcumina/química , Demência/induzido quimicamente , Demência/diagnóstico por imagem , Demência/patologia , Hipocampo/diagnóstico por imagem , Hipocampo/efeitos dos fármacos , Hipocampo/patologia , Humanos , Aprendizagem em Labirinto/efeitos dos fármacos , Memória/efeitos dos fármacos , Camundongos , Simulação de Acoplamento Molecular , Fármacos Neuroprotetores/síntese química , Fármacos Neuroprotetores/química , Fármacos Neuroprotetores/farmacologia , Estresse Oxidativo/efeitos dos fármacos , Escopolamina/toxicidade
10.
Pak J Pharm Sci ; 34(5(Supplementary)): 1983-1988, 2021 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-34836870

RESUMO

Moxifloxacin and gemifloxacin were tested on isolated rabbits' jejunal preparations as little is known about its effects on gastrointestinal tissues. Moxifloxacin and gemifloxacin were tested in concentrations 0.01-10µg/mL for possible effect(s) on isolated rabbits' jejunal preparations. The drugs were applied on spontaneous, on low K+ (20mM)-induced contractions and on high K+ (80mM)-induced contractions. Response was plotted as % of its respective controls. EC50 for Moxifloxacin and Gemifloxacin on spontaneous (without Glibenclamide) contractions are 2.83±0.5µg/mL and 1.11±0.2µg/mL, respectively. Moxifloxacin and Gemifloxacin relaxed the low K+ (20mM) -induced contractions, which were inhibited in presence of Glibenclamide (3µM). Our result indicates that the relaxant activity of Moxifloxacin and Gemifloxacin is mediated possibly through activation of ATP-sensitive potassium channels (KATP). The relaxant effect of Moxifloxacin and Gemifloxacin is predominantly mediated by activation of ATP-Sensitive potassium channels (KATP), which could be cause of one of relaxing mechanisms.


Assuntos
Gemifloxacina/farmacologia , Canais KATP/efeitos dos fármacos , Moxifloxacina/farmacologia , Parassimpatolíticos/farmacologia , Animais , Bioensaio , Feminino , Glibureto/farmacologia , Jejuno/efeitos dos fármacos , Masculino , Contração Muscular/efeitos dos fármacos , Relaxantes Musculares Centrais/farmacologia , Relaxamento Muscular/efeitos dos fármacos , Coelhos
11.
Pak J Pharm Sci ; 33(2(Supplementary)): 765-770, 2020 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-32863250

RESUMO

Indomethacin is potent and effective drug belongs to NSAID group having low bioavailability. To address this issue the novel method is Nanosuspensions which can be achieved through bottom up and top down methods. The drug concentration, batch size and crystallinity retention are the problems associated with bottom up method consequently top down method was applied. In current project batch size of 350 ml was prepared by mixing 3.5% of Indomethacin with polymer solution. Then it was introduced into Dena⌖ having 0.2µm yttrium reinforced zirconium beads. The effect of milling time was observed for sixty minutes. Stable nanocrystals with particle size of 161nm ±1.90 with PDI of 0.229 ±0.06 were produced. The DSC and PXRD confirmed the crystallinity of created nanocrystals. The pattern of particle size reduction was initially abrupt and then gradual. The two months Stability studies at 4°C and at 25°C revealed that polymers combination (PVP-K30, HPMC-6cps, SDS) were effective in marinating the stability. The SEM and TEM studies unfastened that nanocrystals were homogenously distributed with discrete crystalline morphology. The fabricated nanocrystals demonstrated marked dissolution rate compared to the raw and marketed formulations. It is demonstrated that it is useful for industry due to high drug concentration, large batch size and retention of distinct characteristics.


Assuntos
Indometacina/química , Nanopartículas/química , Disponibilidade Biológica , Química Farmacêutica/métodos , Composição de Medicamentos/métodos , Tamanho da Partícula , Polímeros/química , Solubilidade , Difração de Raios X/métodos
12.
Pak J Pharm Sci ; 32(2): 661-667, 2019 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-31081780

RESUMO

The work presented in this paper illustrates the isolation and structure elucidation of secondary metabolites of Hyoscyamus albus. Two new natural source and three known compounds were isolated from the Hyoscyamus albus. Among the isolated compounds, grivilloside H (1) and betulaplatoside (2) were isolated for the first time while scopolamine (3), ß-sitosterol (4) and stigmasterol (5) have been reported previously from the same plant. The structures of all the isolated compounds were established by using modern spectroscopic technique (UV, IR, NMR, and EI-MS) and by comparing with those available in literature.


Assuntos
Hyoscyamus/metabolismo , Compostos Fitoquímicos/química , Plantas Medicinais/metabolismo , Glucosídeos/química , Glucosídeos/isolamento & purificação , Glucosídeos/metabolismo , Hyoscyamus/química , Espectroscopia de Ressonância Magnética , Estrutura Molecular , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/metabolismo , Plantas Medicinais/química , Escopolamina/química , Escopolamina/isolamento & purificação , Escopolamina/metabolismo , Metabolismo Secundário , Sitosteroides/química , Sitosteroides/isolamento & purificação , Sitosteroides/metabolismo , Espectrofotometria Infravermelho , Espectrofotometria Ultravioleta , Estigmasterol/química , Estigmasterol/isolamento & purificação , Estigmasterol/metabolismo
13.
Bioorg Chem ; 78: 427-435, 2018 08.
Artigo em Inglês | MEDLINE | ID: mdl-29698893

RESUMO

Three new norditerpenoids alkaloids, 1ß-hydroxy,14ß-acetyl condelphine (1), jadwarine-A (2), jadwarine-B (3) along with two known alkaloids isotalatizidine hydrate (4) and dihydropentagynine (5) were isolated from medicinal plant Delphinium denudatum. The structures of natural products 1-5 were established on the basis of HR-EIMS, 1H and 13C NMR (1D & 2D) spectroscopic data as well as by comparison from literature data. The structures of compound 1 and 4 were also confirmed by single crystal X-ray diffraction studies. In-vitro AChE and BChE enzyme inhibitory activities of compounds 1-5 and molecular docking studies were performed to investigate the possible molecular inhibitory mechanism of the isolated natural products. Compound 2, 4 and 5 showed competitive inhibitory effects by inhibiting AChE and BChE, respectively, while 1 and 3 showed non-competitive inhibition. This work is the first report that provides a supporting evidence about the use of constituents of Delphinium denudatum in cerebral dementia and Alzheimer diseases.


Assuntos
Acetilcolinesterase/metabolismo , Alcaloides/farmacologia , Butirilcolinesterase/metabolismo , Inibidores da Colinesterase/farmacologia , Delphinium/química , Diterpenos/farmacologia , Alcaloides/química , Alcaloides/isolamento & purificação , Animais , Inibidores da Colinesterase/química , Inibidores da Colinesterase/isolamento & purificação , Diterpenos/química , Diterpenos/isolamento & purificação , Relação Dose-Resposta a Droga , Electrophorus , Cavalos , Conformação Molecular , Simulação de Acoplamento Molecular , Relação Estrutura-Atividade
14.
J Asian Nat Prod Res ; 20(2): 172-181, 2018 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-28463565

RESUMO

New lycoctonine-type dual cholinesterase inhibitor, swatinine-C (1), along with three known norditerpenoid alkaloids, hohenackerine (2), aconorine (5) and lappaconitine (6) and two synthetically known but phytochemically new benzene derivatives, methyl 2-acetamidobenzoate (3) and methyl 4-[2-(methoxycarbonyl)anilino]-4-oxobutanoate (4), was isolated from the roots of A. laeve. Structures of new and known compounds (1-6) were established on the basis of latest spectroscopic techniques and by close comparison with the data available in literature. In vitro, compounds (1-6) were tested against AChE and BChE inhibitory activities. Compounds 1 and 2 showed competitive inhibition against AChE (IC50 = 3.7 µM, 4.53 µM) and BChE (IC50 = 12.23 µM, 9.94 µM), respectively. Compounds 5 and 6 showed promising noncompetitive type of inhibitory profile against AChE (IC50 = 2.51 and 6.13 µM) only. Compounds 3 and 4 showed weak inhibitory profile against both AChE and BChE.


Assuntos
Aconitum/química , Inibidores da Colinesterase/isolamento & purificação , Inibidores da Colinesterase/farmacologia , Aconitina/análogos & derivados , Aconitina/química , Aconitina/isolamento & purificação , Aconitina/farmacologia , Alcaloides/química , Alcaloides/isolamento & purificação , Butirilcolinesterase/metabolismo , Inibidores da Colinesterase/química , Estrutura Molecular , Raízes de Plantas/química
15.
Bioorg Med Chem ; 25(13): 3368-3376, 2017 07 01.
Artigo em Inglês | MEDLINE | ID: mdl-28457693

RESUMO

Extensive chromatographic separations performed on the basic (pH=8-10) chloroform soluble fraction of Aconitum heterophyllum resulted in the isolation of three new diterpenoid alkaloids, 6ß-Methoxy, 9ß-dihydroxylheteratisine (1), 1α,11,13ß-trihydroxylhetisine (2), 6,15ß-dihydroxylhetisine (3), and the known compounds iso-atisine (4), heteratisine (5), hetisinone (6), 19-epi-isoatisine (7), and atidine (8). Structures of the isolated compounds were established by means of mass and NMR spectroscopy as well as single crystal X-ray crystallography. Compounds 1-8 were screened for their antioxidant and enzyme inhibition activities followed by in silico studies to find out the possible inhibitory mechanism of the tested compounds. This work is the first report demonstrating significant antioxidant and anticholinesterase potentials of diterpenoid alkaloids isolated from a natural source.


Assuntos
Aconitum/química , Alcaloides/farmacologia , Antioxidantes/farmacologia , Inibidores da Colinesterase/farmacologia , Colinesterases/metabolismo , Diterpenos/farmacologia , Alcaloides/química , Alcaloides/isolamento & purificação , Animais , Antioxidantes/química , Antioxidantes/isolamento & purificação , Inibidores da Colinesterase/química , Inibidores da Colinesterase/isolamento & purificação , Cristalografia por Raios X , Diterpenos/química , Diterpenos/isolamento & purificação , Relação Dose-Resposta a Droga , Electrophorus , Modelos Moleculares , Estrutura Molecular , Teoria Quântica , Relação Estrutura-Atividade
16.
Pharm Biol ; 55(1): 680-686, 2017 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-28033733

RESUMO

CONTEXT: Delphinium denudatum Wall (Ranunculaceae) is a rich source of diterpenoid alkaloids and is widely used for the treatment of various neurological disorders such as epilepsy, sciatica and Alzheimer's disease. OBJECTIVE: The present study describes crystal structure determination and cholinesterase inhibitory potential of isotalatazidine hydrate isolated from the aerial part of Delphinium denudatum. MATERIALS AND METHODS: Phytochemical investigation of Delphinium denudatum resulted in the isolation of isotalatazidine hydrate in crystalline form. The molecular structure of the isolated compound was established by X-ray diffraction. The structural data (bond length and angles) of the compound were calculated by Density Functional Theory (DFT) using B3LYP/6-31 + G (p) basis set. The cholinesterase inhibitory potential of the isolated natural product was determined at various concentrations (62.5, 125, 250, 500 and 1000 µg/mL) followed by molecular docking to investigate the possible inhibitory mechanism of isotalatazidine hydrate. RESULTS: The compound crystallized in hexagonal unit cell with space group P65. Some other electronic properties such as energies associated with HOMO-LUMO, band gaps, global hardness, global electrophilicity, electron affinity and ionization potential were also calculated by means of B3LYP/6-31 + G (p) basis set. The compound showed competitive type inhibition of both acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) with IC50 values of 12.13 µM and 21.41 µM, respectively. DISCUSSION AND CONCLUSION: These results suggest that isotalatazidine hydrate is a potent dual cholinesterase inhibitor and can be used as a target drug in Alzheimer diseases. This is first report indicating isotalatazidine hydrate with anticholinesterase potential.


Assuntos
Aconitina/análogos & derivados , Inibidores da Colinesterase/isolamento & purificação , Delphinium/química , Aconitina/química , Aconitina/isolamento & purificação , Aconitina/farmacologia , Inibidores da Colinesterase/química , Inibidores da Colinesterase/farmacologia , Cristalografia por Raios X , Simulação de Acoplamento Molecular , Estrutura Molecular
17.
Int J Nanomedicine ; 19: 3187-3215, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-38590511

RESUMO

Green synthesis of silver (Ag) and gold (Au) nanoparticles (NPs) has acquired huge popularity owing to their potential applications in various fields. A large number of research articles exist in the literature describing the green synthesis of Ag and Au NPs for biomedical applications. However, these findings are scattered, making it time-consuming for researchers to locate promising advancements in Ag and Au NPs synthesis and their unexplored biomedical applications. Unlike other review articles, this systematic study not only highlights recent advancements in the green synthesis of Ag and Au NPs but also explores their potential unexplored biomedical applications. The article discusses the various synthesis approaches for the green synthesis of Ag and Au NPs highlighting the emerging developments and novel strategies. Then, the article reviews the important biomedical applications of green synthesized Ag and Au NPs by critically evaluating the expected advantages. To expose future research direction in the field, the article describes the unexplored biomedical applications of the NPs. Finally, the articles discuss the challenges and limitations in the green synthesis of Ag and Au NPs and their biomedical applications. This article will serve as a valuable reference for researchers, working on green synthesis of Ag and Au NPs for biomedical applications.


Assuntos
Nanopartículas Metálicas , Prata , Ouro
18.
ACS Omega ; 9(8): 9813-9822, 2024 Feb 27.
Artigo em Inglês | MEDLINE | ID: mdl-38434828

RESUMO

Diabetes, also known as diabetes mellitus (DM), is a metabolic disorder characterized by an abnormal rise in blood sugar (glucose) levels brought on by a complete or partial lack of insulin secretion along with corresponding changes in the metabolism of lipids, proteins, and carbohydrates. It has been reported that medicinal plants play a pivotal role in the treatment of various ailments such as diabetes mellitus, dyslipidemia, and hypertension. The current study involved exploring the acute toxicity and in vivo antidiabetic activity of berberine (WA1), palmatine (WA2), and 8-trichloromethyl dihydroberberine (WA3) previously isolated from Berberis glaucocarpa Stapf using a streptozotocin (STZ)-induced diabetic rat model. Body weight and blood glucose level were assessed on a day interval for 4 weeks. Biochemical parameters, antioxidant enzymes, and oxidative stress markers were also determined. In an acute toxicity profile, the WA1, WA2, and WA3 were determined to be nontoxic up to 500 mg/kg (b.w). After the second and third weeks of treatment (14 and 21 days), the blood glucose levels in the WA1-, WA2-, and WA3-treated groups were significantly lower than those in the diabetic control group (476.81 ± 8.65 mg/dL, n = 8, P < 0.001). On the 21st day, there was a decrease in the blood glucose level and the results obtained were 176.33 ± 4.69, 197.21 ± 4.80, and 161.99 ± 4.75 mg/dL (n = 8, P < 0.001) for WA1, WA2, and WA3 at 12 mg/kg, respectively, as opposed to the diabetic control group (482.87 ± 7.11 mg/dL, n = 8, P < 0.001). Upon comparison with the diabetic group at the end of the study (28 days), a substantial drop in the glucose level of WA3 at 12 mg/kg (110.56 ± 4.11 mg/dL, n = 8, P < 0.001) was observed that was almost near the values of the normal control group. The treated groups (WA1, WA2, and WA3) treated with the samples displayed a significant decline in the levels of HbA1c. Treatment of the samples dramatically lowered the lipid level profile. In groups treated with samples, plasma levels of triglycerides, total cholesterol, and LDL were significantly lowered [F (5, 42) = 100.6, n = 8, P < 0.001]; these levels were also significantly decreased [F (5, 42) = 129.6 and 91.17, n = 8, P < 0.001]. In contrast to the diabetes group, all treated groups had significantly higher HDL levels [F (5, 42) = 15.46, n = 8, P < 0.001]. As a result, hypolipidemic activity was anticipated in the samples. In addition to that, the activity of the antioxidant enzymes superoxide dismutase (SOD) and catalase (CAT) was considerably elevated in the groups treated with the sample compared to the diabetic control group (n = 8, P < 0.001).

19.
Heliyon ; 10(1): e23549, 2024 Jan 15.
Artigo em Inglês | MEDLINE | ID: mdl-38169865

RESUMO

Pectinolytic enzymes are among the important group of industrial enzymes that have wide applications in different food industries. In this study, pectinase-based silica nanocarriers were synthesized using co-precipitation and cross-linking techniques. The resulting silica nanoparticles were investigated using scanning electron microscopy (SEM), energy-dispersive electron microscopy (EDEX), and X-ray diffraction (XRD) for determination of its morphology, elemental composition, and crystalline pattern. Under the optimal immobilization conditions like 1.5 % glutaraldehyde, 3000 IU/mg pectinase concentration, 90 min immobilization time and 40 °C immobilization temperature, pectinase showed maximum immobilization yield. The immobilization of pectinase onto the silica nanocarriers led to enhanced catalytic characteristics, displaying higher enzymatic activity across various temperature and pH levels compared to soluble pectinase. Moreover, the immobilization substantially improved the temperature stability of pectinase, exhibiting 100 % of its initial activity even after 120 h of pre-incubation at 50 °C. Additionally, the silica nanocarrier pectinase retained 100 % of its original activity even after being reused 10 times in a single batch of reactions. These findings indicate that the immobilization of silica nanocarriers effectively enhances pectinase's industrial capabilities, making it economically feasible for industrial use and an efficient system for various biotechnological applications.

20.
Front Bioeng Biotechnol ; 11: 1320739, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-38268939

RESUMO

Green synthesis of metal nanoparticles (NPs) has received extensive attention over other conventional approaches due to their non-toxic nature and more biocompatibility. Herein we report gold and silver NPs (AuNPs@AV and AgNPs@AV) prepared by employing a green approach using crude extract of Aconitum violaceum Jacquem. ex Stapf. The synthesized NPs were characterized using Scanning Electron Microscopy (SEM), Transmission Electron Microscopy (TEM), Energy Dispersive X-ray (EDX), X-ray Diffraction (XRD), UV/Visible spectroscopy, Fourier Transform Infrared (FTIR), X-ray Photoelectron Spectroscopy (XPS), and Zeta Potential. Morphological analysis showed spherical and triangular shapes of the NPs with average size of <100 nm. The AuNPs@AV and AgNPs@AV exhibited effective antibacterial activities, with minimum inhibitory concentrations (MICs) of 95 and 70 µg/mL against Lactobacillus acidophilus (L. acidophilus) and 90 and 65 µg/mL against Escherichia coli (E. coli), respectively. Strong antioxidant effect of AuNPs@AV and AgNPs@AV were reported against DPPH radical and PTIO within range of IC50 values; 161-80 µg/ml as compared to the standard (23-11 µg/mL) respectively. Moreover, the AuNPs@AV and AgNPs@AV showed efficient photocatalytic activity and degraded 89.88% and 93.7% methylene blue (MB) dye under UV light, respectively.

SELEÇÃO DE REFERÊNCIAS
DETALHE DA PESQUISA