Browsing by Author "Adya Prasad Chaturvedi"

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3D-QSAR and insilico study: Modeling parameters for designing new selective 12-LO enzymes inhibitors
(2011) Hemendra Pratap Singh; Adya Prasad Chaturvedi; Chandra Shekhar Sharma
Selective 5-LO and 12-LO enzyme inhibitors have attracted much attention in recent times in the design of novel anthracenone derivatives, which may be used in cancer and psoriasis. However, not much computational studies has been done to examine specific type of parameters beneficial for anthracenone derivatives against 12-LO inhibitions. In our preliminary study we have done 2D QSAR studies by include a series of 2-arylalkyl substituted anthracenone derivatives having inhibitory action on 12-LO isoforms in epidermal homogenate of mice, bovine platelets and porcine leukocyte. These studies produced good predictive models and give statistically significant correlations with selective 12-LO enzyme inhibition. So these structural activity relationship studies were extended to 3DQSAR model studies utilizing theoretical molecular descriptors that can be calculated directly from molecular structures. All the descriptors were selected by genetic algorithm and multiple linear regression (MLRA) methods. All the QSAR models were validated by leave one out (LOO) method. In addition, insilico toxicity studies were also done. These all studies helps in designing some novel anthracenone derivatives with selective 12-LO enzyme inhibition activity with less toxicity.
Comparative analysis of phenolic and flavonoid content of Jatropha Curcas Linn.
(2012) Amit Kumar Sharma; Mayank Gangwar; Adya Prasad Chaturvedi; A.S.K. Sinha; Yamini B. Tripathi
Jatropha species belong to the family Euphorbiaceae commonly called physic nut, purging nut or pig nut. Based on their economic and pharmaceutical importance, we investigated the total phenolic and flavonoid content of different parts of whole plant. The dried plant powder was subjected to Soxhlet extraction with methanol. Phenolic content was estimated using Folin ciocalteau reagent, flavonoid using aluminium chloride (2%) reagent as quercetin equivalent and TLC analysis using chloroform, benzene, hexane and ethyl acetate for the analysis of number of constituent in different extract. Methanolic extract of J. curcas leaf contain higher phenolic content (38.8±2.14) followed by latex (29.12±4.52) and root (26.15±3.84). Flavonoid contents was found to be maximum in cake (26.15±3.84) followed by latex (18.14±2.54). TLC analysis shows four to six spots in different extract showing varying number of components using hexane, chloroform and benzene solvent. The study revealed that the extracts of J. curcas showed presence of high amount of phenolic and flavonoid compounds especially presscake along with secondary metabolites suggesting its use for treatment of various infections.
Methanolic extract of leaves of Jasminum grandiflorum Linn modulates oxidative stress and inflammatory mediators
(2011) Adya Prasad Chaturvedi; Yamini Bhusan Tripathi
The leaves of Jasminum grandiflorum (JG) are in clinical use in Ayurveda for wound management. Since, oxidative stress and inflammation are the primary causes in delayed wound healing, so here its antioxidant and anti-inflammatory activities have been investigated using in vitro as well as in vivo models. The solvent-free methanolic extract of dried leaves of JG were tested for its trapping capacity toward pre-generated ABTS •+ radicals, instantly generated superoxide and hydroxyl radicals, along with metal chelation property, reducing power and total phenolic content. Further, it was tested on LPS-induced nitric oxide and cell viability, on primary culture of rat peritoneal macrophages. Its anti-inflammatory property was also tested on carrageenan-induced paw edema in rats. This extract significantly inhibited iron-induced lipid peroxidation and trapped ABTS •+, superoxide and OH radicals. It significantly inhibited nitric oxide (NO) release, without affecting the cell viability at 800 μg/ml concentration and reduced the formation of paw edema in rats. Thus, it could be suggested that the aforesaid anti-inflammatory properties of JG leaves are associated to its high phenolic content (2.25 ± 0.105 mg/l of gallic acid equivalent), reducing power and its free radical-scavenging property. © 2011 Springer Basel AG.
Microspheres based on mannosylated lysine-co-sodium alginate for macrophage-specific delivery of isoniazid
(2012) Sanjay Tiwari; Adya Prasad Chaturvedi; Yamini Bhusan Tripathi; Brahmeshwar Mishra
The present investigation reports coupling of ε- and α-amino groups of lysine (LS) with mannose (m-LS) and sodium alginate (SA), respectively, to reduce its toxicity. Prepared conjugate, m-LS-co-SA, was characterized through infra-red spectroscopy and differential scanning calorimetry. Cell viability studies were undertaken to assess the safety profile of the prepared conjugate. Microspheres, based on the conjugate, were prepared using spray drying technique and studied for targeting of isoniazid to alveolar macrophages (AMs). Pharmacokinetic studies of the optimized formulation batch were performed in Charles Foster rats. Infra-red spectral data of the synthesized conjugate were in agreement to the presumptive sequence of the conjugation process. Dispersibility, thermal stability and safety of the conjugate were conducive to its biomedical application. Microspheres, formulated from the conjugate, were of uniform size and offered satisfactory drug loading efficiency and in vitro release characteristics. X-ray diffraction studies established that drug was entrapped within the microspheres rather than being adsorbed on to the surface. Pharmacokinetic studies revealed that the conjugate could be a potential vehicle towards both active targeting of isoniazid to AMs and controlling its release rate. © 2011 Elsevier Ltd. All rights reserved.