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1.
J Ayurveda Integr Med ; 12(3): 489-499, 2021.
Artículo en Inglés | MEDLINE | ID: mdl-34353694

RESUMEN

BACKGROUND: Nayopayam kwatha (NK) is a well-known polyherbal formulation widely used to cure respiratory ailments, heart problems, and postnatal difficulties. Literature suggests that so far no standardization protocol was developed for NK to validate its quality and purity. OBJECTIVE(S): To develop a standardization protocol for NK based on the marker phytoconstituents present in the individual herbs of the formulation. MATERIALS AND METHODS: The roots of bala [Sida cordifolia (B1) and Sida retusa (B2)], seeds of jeeraka (Cuminum cyminum), and rhizomes of nagara (Zingiber officinale) were the ingredients of NK. Since there were two source plants for bala, two sets of NK (NKB1 and NKB2) were prepared in the ratio 3:2:1 as per Vaidya Manorama and 10:1:1 as per Arogyaraksha Kalpadruma along with 1:1:1 as per the general way of Ayurvedic polyherbal decoctions. Both the individual herbs and the kwatha (decoction) prepared were analyzed in terms of pharmacognostical, organoleptic, and physcicochemical parameters as per the standard methods. Phytochemical analysis of the individual herbs resulted in the isolation of major phytoconstituents and the kwatha was quantified in terms of marker compounds with the aid of HPLC. RESULTS: HPLC quantification suggests that appreciable amount of marker phytoconstituents of individual herbs are present in the kwatha. Thus, the isolated compounds luteolin (C. cyminum), 6-gingerol (Z. officinale), ß-sitosterol (S. retusa), and ecdysterone (S.cordifolia) can be used as markers to standardize NK. CONCLUSION: Characteristics of NK, as well as its individual drugs, were well-established. The present study of NK with respect to its phytochemistry revealed that the classical drug ratios of the polyherbal formulation are of utmost importance rather than the ingredients in equal proportion. The characterization parameters of individual herbs and kwatha described in this study may serve as a standard reference for quality control analysis of NK and the method developed in this study can be used as a reliable technique for standardization of NK to ensure the purity and quality of raw drugs used.

2.
Nat Prod Res ; 35(5): 867-872, 2021 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-31104493

RESUMEN

Promalabaricone B (PMB), an acylphenol was isolated from dichloromethane-soluble extract of the seeds of Myrisitica fatua Houtt. PMB exhibited significant inhibitory activity on α-glucosidase enzyme. The molecular docking and dynamics studies of PMB with human maltase-glucoamylase were performed. PMB exhibited an enhanced glucose uptake in L6 myotubes with 46.3% in 2.5 µM. Encouraged with these results; we investigated the molecular mechanism of PMB through the upregulation of AMPK. The results revealed that PMB promoted the glucose uptake in myocytes by stimulating the translocation and expression of GLUT4. From this, it is clear that PMB can acts as a potential therapeutic option for diabetes treatment, and its hypoglycaemic effect may be mediated by AMPK upregulation and induction of GLUT4 translocation.


Asunto(s)
Proteínas Quinasas Activadas por AMP/metabolismo , Glucosa/metabolismo , Hipoglucemiantes/farmacología , Fibras Musculares Esqueléticas/metabolismo , Myristica/química , Fenoles/farmacología , Semillas/química , Regulación hacia Arriba/efectos de los fármacos , Animales , Transporte Biológico/efectos de los fármacos , Transportador de Glucosa de Tipo 4/metabolismo , Glicosilación/efectos de los fármacos , Humanos , Simulación del Acoplamiento Molecular , Fibras Musculares Esqueléticas/efectos de los fármacos , Fenoles/química , Fenoles/aislamiento & purificación , Saccharomyces cerevisiae/enzimología , Transducción de Señal/efectos de los fármacos , Porcinos , alfa-Amilasas/metabolismo , alfa-Glucosidasas/metabolismo
3.
Trans Indian Natl Acad Eng ; 5(2): 289-294, 2020.
Artículo en Inglés | MEDLINE | ID: mdl-38624417

RESUMEN

Chitra Disinfection Gateway is meant for the decontamination of personnel entering a cleaner private space from a public space. This is equipped with an arrangement for generating hydrogen peroxide mist and ultraviolet rays. Hydrogen peroxide mist will decontaminate clothes, hands and the bags a person carries. The ultraviolet system will decontaminate the chamber once the person has moved out. The system is controlled electronically by sensors and actuators. The sensors fixed in the chamber detect the entry of a person and initiates the hydrogen peroxide atomization process. The person is required to walk through the chamber. When the person exits the chamber, the system will put off the hydrogen peroxide atomization system and will turn on the UV lamp inside the chamber to decontaminate it. The ultraviolet system will be ON for a predefined time and after the process, the next person can enter the walkway. The whole process takes a maximum of 40 s. The safety and efficacy of the system have been validated experimentally through both in vivo and in vitro studies.

4.
Bioorg Med Chem ; 26(12): 3461-3467, 2018 07 23.
Artículo en Inglés | MEDLINE | ID: mdl-29789207

RESUMEN

Phytochemical investigation of the stem bark of Myristica fatua Houtt. led to the isolation of a new compound 1 (3-tridecanoylbenzoic acid), along with six known acylphenols (2-7). All the compounds displayed moderate inhibitory activity on α-amylase and significant activity on α-glucosidase; however malabaricone B (6) and C (7) were identified as potent α-glucosidase inhibitors with IC50 values of 63.70 ±â€¯0.546, and 43.61 ±â€¯0.620 µM respectively. Acylphenols (compounds 3-7) also showed significant antiglycation property. The molecular docking and dynamics simulation studies confirmed the efficient binding of malabaricone C with C-terminus of human maltase-glucoamylase (2QMJ). Malabaricone B also enhanced the 2-NBDG [2-(N-(7-nitrobenz-2-oxa-1,3-diazol-4-yl)amino)-2-deoxy glucose] uptake in L6 myotubes. These findings demonstrate that acylphenols isolated from Myristica fatua Houtt. can be considered as a lead scaffold for the treatment of type II diabetes mellitus.


Asunto(s)
Inhibidores de Glicósido Hidrolasas/química , Hipoglucemiantes/química , Myristicaceae/química , Fitoquímicos/química , Sitios de Unión , Línea Celular , Supervivencia Celular/efectos de los fármacos , Diabetes Mellitus Tipo 2/tratamiento farmacológico , Diabetes Mellitus Tipo 2/patología , Inhibidores de Glicósido Hidrolasas/metabolismo , Inhibidores de Glicósido Hidrolasas/farmacología , Humanos , Hipoglucemiantes/metabolismo , Hipoglucemiantes/farmacología , Hipoglucemiantes/uso terapéutico , Simulación de Dinámica Molecular , Células Musculares/citología , Células Musculares/efectos de los fármacos , Células Musculares/metabolismo , Myristicaceae/metabolismo , Fitoquímicos/metabolismo , Fitoquímicos/farmacología , Corteza de la Planta/química , Corteza de la Planta/metabolismo , Extractos Vegetales/química , Tallos de la Planta/química , Tallos de la Planta/metabolismo , Estructura Terciaria de Proteína , Resorcinoles/química , Resorcinoles/metabolismo , Resorcinoles/farmacología , alfa-Glucosidasas/química , alfa-Glucosidasas/metabolismo
5.
Life Sci ; 152: 220-30, 2016 May 01.
Artículo en Inglés | MEDLINE | ID: mdl-27049116

RESUMEN

AIMS: The present study investigates the protective effect of partially characterized Tribulus terrestris L. fruit methanol extract against mitochondrial dysfunction in cell based (H9c2) myocardial ischemia model. MAIN METHODS: To induce ischemia, the cells were maintained in an ischemic buffer (composition in mM -137 NaCl, 12 KCl, 0.5 MgCl2, 0.9 CaCl2, 20 HEPES, 20 2-deoxy-d-glucose, pH-6.2) at 37°C with 0.1% O2, 5% CO2, and 95% N2 in a hypoxia incubator for 1h. Cells were pretreated with various concentrations of T. terrestris L. fruit methanol extract (10 and 25µg/ml) and Cyclosporin A (1µM) for 24h prior to the induction of ischemia. KEY FINDINGS: Different parameters like lactate dehydrogenase release, total antioxidant capacity, glutathione content and antioxidant enzymes were investigated. Studies were conducted on mitochondria by analyzing alterations in mitochondrial membrane potential, integrity, and dynamics (fission and fusion proteins - Mfn1, Mfn2, OPA1, Drp1 and Fis1). Various biochemical processes in mitochondria like activity of electron transport chain (ETC) complexes, oxygen consumption and ATP production was measured. Ischemia for 1h caused a significant (p≤0.05) increase in LDH leakage, decrease in antioxidant activity and caused mitochondrial dysfunction. T. terrestris L. fruit methanol extract pretreatment was found effective in safeguarding mitochondria via its antioxidant potential, mediated through various bioactives. HPLC of T. terrestris L. fruit methanol extract revealed the presence of ferulic acid, phloridzin and diosgenin. SIGNIFICANCE: T. terrestris L. fruit ameliorate ischemic insult in H9c2 cells by safeguarding mitochondrial function. This validates the use of T. terrestris L. against heart disorders.


Asunto(s)
Enfermedades Mitocondriales/tratamiento farmacológico , Enfermedades Mitocondriales/metabolismo , Isquemia Miocárdica/tratamiento farmacológico , Isquemia Miocárdica/metabolismo , Extractos Vegetales/uso terapéutico , Tribulus/química , Antioxidantes/metabolismo , Línea Celular , Ácidos Cumáricos/análisis , Ácidos Cumáricos/farmacología , Ciclosporina/farmacología , Diosgenina/análisis , Diosgenina/farmacología , Transporte de Electrón/efectos de los fármacos , Frutas/química , Glutatión/metabolismo , Humanos , L-Lactato Deshidrogenasa/metabolismo , Potencial de la Membrana Mitocondrial/efectos de los fármacos , Isquemia Miocárdica/enzimología , Florizina/análisis , Florizina/farmacología
6.
J Biomed Mater Res B Appl Biomater ; 89(2): 282-292, 2009 May.
Artículo en Inglés | MEDLINE | ID: mdl-18837453

RESUMEN

High molecular weight chitosan (CS) was depolymerized by oxidative degradation with NaNO(2) at room temperature to get 11 samples of CS derivatives of varying molecular weights with a view to assessing their effective molecular weight range for gene delivery applications. Viscosity studies indicated that the molecular weight of the depolymerized CS was proportional to the CS/NaNO(2) ratio. The condensation behavior of DNA/CS complexes at various charge ratios was studied using UV spectroscopy, FTIR, CD, SEM, and AFM. The results indicated that CSs having very low molecular weights and high charge density exhibited strong binding affinity to DNA compared to high molecular weight CSs. However, the very low molecular weight (1.9-7.7 kDa) CSs were found to form aggregates easily even at very low charge ratios. On the other hand, CSs having medium molecular weight (49-51 kDa) and high degree of deacetylation (DD) gave stable uniform-sized nanoparticles. Biological studies carried out with the spherical nano-sized polyplexes formed between CS of 50 kDa (DD of 94%) and pEGFP plasmid DNA at N/P ratio of 5.0 showed excellent gene transfection efficiency at pH 6.5 in HeLa cells without cytotoxicity indicating their potential as gene delivery carriers.


Asunto(s)
Quitosano/química , ADN/química , Técnicas de Transferencia de Gen , Nanopartículas/química , Animales , Conformación de Carbohidratos , Secuencia de Carbohidratos , Bovinos , Quitosano/metabolismo , Portadores de Fármacos/química , Terapia Genética , Células HeLa , Humanos , Sustancias Macromoleculares/química , Ensayo de Materiales , Microscopía de Fuerza Atómica , Datos de Secuencia Molecular , Peso Molecular , Tamaño de la Partícula , Viscosidad
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