Posted by admin on Dec 31, 2020 in |
Nicotinic acetylcholine receptor α3β4 is considered as a potential target for anti-smoking drug discovery. In this study, in-silico approaches, including molecular docking and molecular dynamics simulation were applied to investigate binding affinities of 300 alkaloids into the α3β4 (Pdb id: 6PV8). The docking results showed that most of the alkaloids fitted well into the binding pocket of α3β4. The top hit compounds were A122 (indole alkaloid) and A128 (tropane alkaloid) with their binding affinities of less than -8.0 kcal.mol-1 and the interactions with key residue, Trp149. Structures and binding affinities relationships between the indole and tropane compounds with the α3β4 emphasized the important roles of indole backbone and the benzyl substituent at C3 of tropane scaffold in forming the hydrophobic interactions making good binding affinities. Molecular dynamics simulations revealed the potential of A128 to binding stably with the α3β4 during 20 ns. Binding free energy of the complex A128 – α3β4 was calculated based on Molecular Mechanics – Poisson Boltzmann Surface Area (MM-PBSA) method, which also emphasized the importance...
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Posted by admin on Dec 31, 2020 in |
This study is aimed to evaluate the effects of different concentrations of cyclodextrin, an auxin stabilizing agent, on callus growth from the stem explants of Tinospora cordifolia and to assess the antioxidant properties of the bioactive hydrolysates of callus tissue using chymotrypsin, trypsin, pepsin, and papain. Cyclodextrin exerted a dose- and time-dependent effect on the callus growth. α-chymotrypsin hydrolysate showed the strongest 1,1-diphenyl-2-picrylhydrazyl (DPPH•) radical scavenging, while trypsin hydrolysate exhibited the highest 2,2’-azinobis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS•+) activity. Protein profiling of callus tissue revealed a few tissue-specific bands at 41, 30, 20, and 9 kDa with varying intensities. A growth medium containing sucrose has a specific impact on the expression of these polypeptides. Purification of 30 kDa polypeptide by Sephadex-G50 revealed distinct quantitative differences to different concentrations of cyclodextrin. This study suggested that T.cordifolia callus tissue protein hydrolysates exhibited antioxidant efficacy, leading to the development of a nutraceutical agent in promoting...
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Posted by admin on Dec 31, 2020 in |
A Simple, accurate, and precise spectrophotometric method (1st order derivative method) was developed and validated for the estimation of Anagliptin and Metformin HCl in synthetic mixture. In this method, Anagliptin was estimated at 244 nm where Metformin HCl showed zero absorbance. Metformin HCl is estimated at 234 nm at which Anagliptin showed zero absorbance. The method was linear over the concentration ranges 2-12 µg/mL for Anagliptin and 5-30 µg/mL for Metformin HCl. The LOD was found to be 0.127 µg/mL for Anagliptin and 0.599 µg/mL for Metformin HCl. The LOQ was found to be 0.387 µg/mL for Anagliptin and 1.817µg/mL for Metformin HCl. In the recovery study, % recovery was 99.55 – 101.65% of Anagliptin and 100.25-100.57% of Metformin HCl. The method was found to be precise as %RSD was less than 2.00 in repeatability, Interday, and intraday precision for Anagliptin and Metformin HCl. The % assay of analyte drugs was found to be 101.42% of Anagliptin and 99.61% of Metformin HCl, which showed good applicability of the developed...
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Posted by admin on Dec 31, 2020 in |
The present study deals with the PHB made cast film with different plant and algal formulations. Its biocompatibility was tested in-vitro and in-vivo. The anti-inflammatory activity was higher in F4 and F5, close to the standard Diclofenac. The F7 and F8 exhibited moderate cytotoxicity, and formulation F2 exhibited low cytotoxicity. The maximum zone of inhibition was exhibited in F5 followed by F4 against skin pathogens. The overall results of antioxidant activity indicated that F4, F5, and F8 have good antioxidant properties. Percentage (%) of wound contraction at the 10th day of control was 16.9% and PHB alone was 21.3%. F5 and F3 showed higher activity with 51.7 and 49.7%, respectively. The self-healing potential was found to be 35.6%, but PHB was able to cure additional 5% (40.5) on 16th day. F5, F3, and F4 showed high activity of 81.5, 80.1, and 79.9, respectively. The in-vitro and in-vivo studies showed that the Centella asiatica and Padina tetrastromatica with PHB has an effective activity towards antimicrobial, antioxidant, and wound healing activity....
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Posted by admin on Dec 31, 2020 in |
Astaxanthin (3,3′-dihydroxy-β, β′-carotene-4,4′-dione) is a xanthophyll carotenoid, which is found in Haematococcus pluvialis, Chlorella zofingiensis, Chlorococcum, and Phaffiarhodozyma. Astaxanthin play major role as a nutritional supplement, antioxidant and anticancer agent, anti-diabetes, cardiovascular diseases, and neurodegenerative disorders. In our previous study, astaxanthin was first encapsulated by different agents and characterized using SEM, FT-IR, and in-vitro drug release. The present study aimed to explore the anticancer activity of encapsulated and non-encapsulated astaxanthin on the African green monkey normal kidney Vero cell line and HepG2 cell line. From the in-vitro study, the IC50 of HepG2 cells was found to be 500 μg/ml compared to the normal Vero cell line with IC50 of 600 μg/ml of which was confirmed by MTT assay. Further, the fluorescence microscope and DNA fragmentation were carried to analyze the apoptosis in HepG2 treated cells. Thus, our results suggested that liposomal encapsulated astaxanthin (ME1) exhibits good anticancer activity when compared amongst other test samples and positive drug...
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