Thangavel Ponrasu

Spontaneous ultra fast synthesis of gold nanoparticles using Punica granatum for cancer targeted drug delivery

Rapid synthesis of mono-dispersed gold nanoparticles through economically feasible green chemistry approach is highly desirable. In this study, we have developed a method to synthesize mono-dispersed gold nanoparticles (PAuNPs) by mixing gold solution with fruit peel extract of Punica granutum without using any surfactant or external energy. In this method, physiologically stable, biocompatible PAuNPs were formed within 60s. Casein, being a biocompatible polymer, is used to couple the prepared PAuNPs for functionalization of folic acid, which is highly expressed in cancer cells. These functionalized PAuNPs could be used for targeted drug delivery for cancer with enhanced therapeutic efficacy and minimal side effects. PAuNPs were characterized by UV, IR, TEM, Particle size analyzer and zeta potential measurement. In vitro stability of the PAuNPs was also analyzed. Hemocompatibility of PAuNPs was evaluated in human blood samples and found that the particles were hemocompatible. The toxicity of the PAuNPs, 5-Fu and 5Fu@PAuNPs was analyzed in zebrafish embryos. The in vitro cytotoxicity of free 5-Fu, 5Fu@PAuNPs-Fa was investigated against MCF-7 cells (breast cancer) and observed that the amount of 5-Fu required to achieve 50% of growth of inhibition (Ic50) was much lower when compared to free 5-Fu.

Green synthesis of pullulan stabilized gold nanoparticles for cancer targeted drug delivery

The aim of this study was to synthesize green chemistry based gold nanoparticles using liver specific biopolymer and to develop a liver cancer targeted drug delivery system with enhanced efficacy and minimal side effects. Pullulan stabilized gold nanoparticles (PAuNPs) were coupled with 5-Fluorouracil (5-Fu) and folic acid (Fa) which could be used as a tool for targeted drug delivery and imaging of cancer. The toxicity of 5-Fu, 5-Fu adsorbed gold nanoparticles (5-Fu@AuNPs), Fa-coupled 5-Fu adsorbed gold nanoparticles (5-Fu@AuNPs-Fa), was studied using zebrafish embryo as an in vivo model. The in vitro cytotoxicity of free 5-Fu, 5-Fu@AuNPs, 5-Fu@AuNPs-Fa against HepG2 cells was studied and found that the amount of 5-Fu required to achieve 50% of growth of inhibition (Ic50) was much lower in 5-Fu@AuNP-Fa than in free 5-Fu, 5-Fu@AuNPs. The in vivo biodistribution of PAuNPs showed that higher amount of gold had been accumulated in liver (54.42±5.96 μg) than in other organs.

Topical application of Acalypha indica accelerates rat cutaneous wound healing by up-regulating the expression of Type I and III collagen

ETHNOPHARMACOLOGICAL RELEVANCE Acalypha indica Linn. (Acalypha indica) vernacularly called Kuppaimeni in Tamil, has been used as a folklore medicine since ages for the treatment of wounds by tribal people of Tamil Nadu, Southern India. The present study investigates the biochemical and molecular rationale behind the healing potential of Acalypha indica on dermal wounds in rats. MATERIAL AND METHODS Acalypha indica extract (40 mg/kg body weight) was applied topically once a day on full-thickness excision wounds created on rats. The wound tissue was removed and used for estimation of various biochemical and biophysical analyses and to observe histopathological changes with and with-out extract treatment. The serum levels of pro-inflammatory cytokine tumor necrosis factor (TNF-α) was measured at 12 h, 24 h, 48 h and 72 h post-wounding using ELISA. Reverse transcription-polymerase chain reaction (RT-PCR) analysis was performed to study the expression pattern of transforming growth factor [TGF-β1], collagen 1 α (I) [Col 1 α (I)] and collagen 3 α (I) [Col 3 α (I)]. Likewise, linear incision wounds were created and treated with the extract and used for tensile strength measurements. RESULTS Wound healing in control rats was characterized by less inflammatory cell infiltration, lack of granulation tissue formation, deficit of collagen and significant decrease in biomechanical strength of wounds. Acalypha indica treatment mitigated the oxidative stress and decreased lipid peroxidation with concomitant increase in ascorbic acid levels. It also improved cellular proliferation, increased TNF-α levels during early stages of wound healing, up-regulated TGF-β1 and elevated collagen synthesis by markedly increasing the expression of Col 1 α (I) and Col 3 α (I). Increased rates of wound contraction, epithelialization, enhanced shrinkage temperature and high tensile strength were observed in the extract treated rats. CONCLUSION Acalypha indica extract was shown to augment the process of dermal wound healing by its ability to increase collagen synthesis through up-regulation of key players in different phases of wound healing and by its antioxidative potential.

Biomimetic hybrid porous scaffolds immobilized with platelet derived growth factor-BB promote cellularization and vascularization in tissue engineering.

Development of hybrid scaffolds with synergistic combination of growth factor is a promising approach to promote early in vivo wound repair and tissue regeneration. Here, we show the rapid wound healing in Wistar albino rats using biomimetic collagen-poly(dialdehyde) guar gum based hybrid porous scaffolds covalently immobilized with platelet derived growth factor-BB. The immobilized platelet derived growth factor in the hybrid scaffolds not only enhance the total protein, collagen, hexosamine, and uronic acid contents in the granulation tissue but also provide stronger tissues. The wound closure analysis reveal that the complete epithelialization period is 15.4 ± 0.9 days for collagen-poly(dialdehyde) guar gum-platelet derived growth factor hybrid scaffolds, whereas it is significantly higher for control, collagen, collagen- poly(dialdehyde) guar gum and povidine-iodine treated groups. Further, the histological evaluation shows that the immobilized platelet derived growth factor in the hybrid scaffolds induced a more robust cellular and vascular response in the implanted site. Hence, we demonstrate that the collagen-poly(dialdehyde) guar gum hybrid scaffolds loaded with platelet derived growth factor stimulates chemotactic effects in the implanted site to promote rapid tissue regeneration and wound repair without the assistance of antibacterial agents.

Angiotensin-converting enzyme inhibitory and antioxidant activities of enzymatically synthesized phenolic and vitamin glycosides

Amyloglucosidase from Rhizopus mould and β‐glucosidase from sweet almond were employed for the preparation of phenolic and vitamin glycosides of vanillin, N‐vanillylnonanamide, DL‐dopa, dopamine, curcumin, α‐tocopherol (vitamin E), pyridoxine (vitamin B6), ergocalciferol (vitamin D2), thiamin (vitamin B1) and riboflavin (vitamin B2). Approx. 20 enzymatically prepared phenolic and vitamin glycosides were subjected to ACE (angiotensin‐converting enzyme) inhibition activity measurements, and 14 glycosides were tested for antioxidant activities. Both phenolic and vitamin glycosides exhibited IC50 values for ACE inhibition in the 0.52±0.03–3.33±0.17 mM range and antioxidant activities ranging from 0.8±0.04 to 1.18±0.06 mM. Comparable ACE inhibition values were observed between free phenols and vitamin glycosides. However, antioxidant activities of glycosides were, in general, lesser than those of free phenols. Best IC50 value for ACE inhibition were observed for 11‐O‐(D‐fructofuranosyl)thiamin (0.52±0.03 mM), 3‐hydroxy‐4‐O‐(6‐D‐sorbitol)phenylalanine (0.56±0.03 mM), 4‐O‐(β‐D‐glucopyranosyl)vanillin (0.61±0.03 mM), 4‐O‐(D‐galactopyranosyl)vanillin (0.61±0.03 mM) and pyridoxine‐D‐glucoside (0.84±0.04 mM). Similarly, best IC50 values for antioxidant activity were observed for 1,7‐O‐(bis‐β‐D‐glucopyranosyl)curcumin (0.8±0.04 mM), 4‐O‐(β‐D‐glucopyranosyl)vanillin (0.9±0.05 mM), 3‐hydroxy‐4‐O‐(β‐D‐galactopyranosyl‐(1′→4)β‐D‐glucopyranosyl)phenylalanine (0.9±0.05 mM), 20‐O‐(D‐glucopyranosyl)ergocalciferol (0.9±0.05 mM) and dopamine‐D‐galactoside (0.93±0.05 mM).

Syntheses of Retinol Glycosides Using β-glucosidase in SCCO2 Media

Abstractβ-Glucosidase isolated from sweet almond catalyzed syntheses of water soluble retinol glycosides were carried out in SCCO2 media with carbohydrates—D-glucose 2, D-galactose 3, D-mannose 4, D-fructose 5, and D-sorbitol 6. Retinol glycosides yields were in the 9–34% range. Reaction with D-fructose 5 gave a highest yield of 34%. Excellent regioselectivity was observed with D-mannose 4 and D-sorbitol 6 which gave exclusively C1β-mannoside and C1-D-sorbitolide.

An eco-friendly method for short term preservation of skins/hides using Semecarpus anacardium nut extract

Preservation or curing of hides and skins is performed as the primary step of leather processing. Common salt is employed as the conventional agent for curing purpose. Use of salt enhances the pollution load of tannery effluent which becomes highly contaminated with increased total dissolved solids and chlorides. To overcome this hurdle, researchers are in constant search of alternative preservation techniques which are either totally void of salt or use only a meager amount of salt. In the present study, we had explored the possibility of using Semecarpus anacardium nut extract as an alternative to salt for the curing process by assessing different parameters like hair slip, putrefaction odor, volatile nitrogen content, moisture content, bacterial count, and shrinkage temperature in comparison to the salt curing method. The antibacterial property of the plant extract was also investigated. The results obtained substantiated that the nut extract of S. anacardium effectively could preserve the skins for more than a month, by its antibacterial activity along with the dehydrating property of acetone.

Curcumin loaded on pullulan acetate nanoparticles protects the liver from damage induced by DEN

In recent years, nanoparticle based drug delivery has been used to treat liver diseases. Even though curcumin is a potent antioxidant, reactive oxygen species (ROS) scavenger and anti-inflammatory agent, its use at a clinical level is very limited due to its poor bioavailability rendered by its physiochemical properties. In this study, biodegradable liver specific pullulan acetate nanoparticles (PA) loaded with curcumin were developed for the first time. These curcumin loaded PA nanoparticles were found to improve the encapsulation efficiency and stability of curcumin with sustained release, under physiological conditions. Thus, curcumin loaded pullulan acetate nanoparticles (PAC) could solve the physicochemical defects of curcumin like solubility, pH stability, photo-stability, and be used as an effective hepato-protective agent against diethyl nitrosamine (DEN) induced liver damage.

Efficacy of Acorus calamus on collagen maturation on full thickness cutaneous wounds in rats

Background: The rhizomes of Acorus calamus and their essential oil are widely used in the flavoring industry and production of alcoholic beverages in Europe. Recent reports have confirmed the presence of several pharmacological components in the rhizomes of A. calamus. Objective: The objective of this study was to find out the efficacy of topical administration of ethanolic extract of A. calamus on dermal wound healing in rats. Wound healing is a natural process occurring in living organisms, which results in a complete or partial remodeling of injured tissue and ultimately progresses to the formation of a fibrous scar. Several natural products have been reported to augment the wound healing process. Materials and Methods: An ethanolic extract of A. calamus was prepared and its wound-healing efficacy was studied. An excision wound was made on the back of the rat and 200 μL (40 mg/kg body weight) of the A. calamus extract was applied topically once daily for the treated wounds. The control wounds were treated with 200 μL of phosphate buffered saline. Results: The granulation tissues formed were removed at 4, 8 and 12 days and biochemical parameters such as deoxyribonucleic acid, total protein, total collagen, hexosamine and uronic acids were measured. The amount of type I/III collagen formed in control and treated wound tissues was evaluated by sodium dodecyl sulfate-polyacrylamide gel electrophoresis. The epithelialization time, tensile strength and histological examination of the wounds were also studied. Biochemical analyses of the granulation tissues revealed a significant increase in collagen, hexosamine and uronic acid when compared with the control. The tensile strength of extract treated wounds was found to increase by 112%. A significant reduction in lipid peroxide levels suggested that A. calamus possesses antioxidant components. Conclusions: The results strongly confirm the beneficial effects of A. calamus in augmenting the wound healing process.