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Parthasarathy K.,Siddha Central Research Institute | Parthasarathy K.,Orchid Chemicals & Pharmaceuticals Ltd. | Praveen C.,CSIR - Central Electrochemical Research Institute | Saranraj K.,CSIR - Central Leather Research Institute | And 2 more authors.
Medicinal Chemistry Research

Microwave-assisted tandem double condensation between isatins and 4-hydroxycoumarin under zinc triflate catalysis to afford spirooxindoles in excellent yield is reported. The synthesized compounds were screened for their in vitro antibacterial and antifungal activities. The compounds that showed promising antimicrobial activity (3a, 3j and 3m) were studied for their binding affinity towards AmpC-β-lactamase receptor, which revealed that compound 3a is highly stabilized by strong hydrogen bond interactions with in the binding pocket. The synthesized spirooxindoles were also evaluated for their cytotoxic potential against COLO320 adenocarcinoma colorectal cancer cells. Biological assay and in silico studies indicated compound 3n as the most active in terms of low IC50 value (50.7 μM) and least free energy of binding (−8.89 kcal/mol) respectively. © 2016 Springer Science+Business Media New York Source

Sanath Kumar T.S.S.P.N.S.,Osmania University | Sanath Kumar T.S.S.P.N.S.,Siddha Central Research Institute | Prasant A.,Osmania University | David Krupadanam G.L.,Osmania University | Akshaya Kumar K.,Osmania University
Indian Journal of Chemistry - Section B Organic and Medicinal Chemistry

2-Benzoyl-3-phenacyl-2.3-dihydrobenzofurans are synthesized by the reaction between 2-hydroxychalcones and 2-broinoaceto-phenones with potassium carbonate in boiling acetone in good yield. Source

Chitra B.,National Institute of Siddha | Ramaswamy R.S.,Central Council for Research in Siddha | Shakila R.,Siddha Central Research Institute
International Journal of Pharma and Bio Sciences

Siddha system of medicine is existing among the indian society since time immemorial. However, in spite of their efficacy, they have been widely criticized due to lack of standardization and their complex preparation methods. The present study was designed as a step towards standardization of the herbo-metallic formulation, Purna Cantirotaya Centuram (PCC). To assure the quality of PCC, the drug was subjected to physico-chemical parameters as mentioned in PLIM guidelines, X-Ray Diffraction (XRD) and Scanning Electron Microscopy (SEM) and Energy Dispersive analysis of Xray (EDAX). The SEM study revealed that the particles in the formulation are agglomerated. The particle size varied between 1 and 10 μm. EDAX study indicated that the drug contains mercury, sulphur, gold, sodium, potassium, calcium, carbon and oxygen in major percentage and magnesium, aluminium, silicon, iron and niobium in minor percentage. It is concluded that PCC is a complex compound, having very small particle size and essential elements that might be the reason for its wide ranging clinical efficacy. Source

Venkatasubbu G.D.,Anna University | Ramasamy S.,Anna University | Reddy G.P.,Siddha Central Research Institute | Kumar J.,Anna University
Biomedical Microdevices

Targeted drug delivery using nanocrystalline materials delivers the drug at the deseased site. This increases the efficacy of the drug in killing the cancer cells. Surface modifications were done to target the drug to a particular receptor on the cell surface. This paper reports synthesis of hydroxyapatite and titanium dioxide nanoparticles and modification of their surface with polyethylene glycol (PEG) followed by folic acid (FA). Paclitaxel, an anticancer drug, is attached to functionalized hydroxyapatite and titanium dioxide nanoparticles. The pure and functionalised nanoparticles are characterised with XRD, TEM and UV spectroscopy. Anticancer analysis was carried out in DEN induced hepatocarcinoma animals. Biochemical, hematological and histopathological analysis show that the surface modified paclitaxel attached nanoparticles have an higher anticancer activity than the pure paclitaxel and surface modified nanoparticles without paclitaxel. This is due to the targeting of the drug to the folate receptor in the cancer cells. © 2013 Springer Science+Business Media New York. Source

Venkatasubbu G.D.,University of Madras | Ramasamy S.,Anna University | Gaddam P.R.,Siddha Central Research Institute | Kumar J.,Anna University
International Journal of Nanomedicine

Nanoparticles are widely used for targeted drug delivery applications. Surface modification with appropriate polymer and ligands is carried out to target the drug to the affected area. Toxicity analysis is carried out to evaluate the safety of the surface modified nanoparticles. In this study, paclitaxel attached, folic acid functionalized, polyethylene glycol modified hydroxyapatite and titanium dioxide nanoparticles were used for targeted drug delivery system. The toxicological behavior of the system was studied in vivo in rats and mice. Acute and subchronic studies were carried out. Biochemical, hematological, and histopathological analysis was also done. There were no significant alterations in the biochemical parameters at a low dosage. There was a small change in alkaline phosphatase (ALP) level at a high dosage. The results indicate a safe toxicological profile. © 2015 Venkatasubbu et al. Source

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