@article {1064, title = {In vitro Screening for Antioxidant and Antimicrobial Properties of 3,5-Bis(E-thienylmethylene) piperidin-4-one, a Curcumin Analogue}, journal = {Pharmacognosy Research}, volume = {14}, year = {2022}, month = {July 2022}, pages = {276-283}, type = {Original Article}, chapter = {276}, abstract = {

Background: Curcumin is a naturally occurring bis-chalcone derivative in the commonly used Indian spice turmeric and is well-known for its potent chemopreventive, anti-angiogenic, anti-cancer properties. 3,5-bis[(E)-thienylmethylene] piperidin-4-one (BTMP) is the newly synthesised synthetic analogue of curcumin that is tested for its antioxidant and antimicrobial properties in vitro. Objectives: This study was to determine the antioxidant activity and antibacterial potentials of newly synthesised analogues of curcumin viz., 3,5-bis[(E)- thienylmethylene] piperidin-4-one (BTMP), was examined in vitro. Materials and Methods: BTMP was evaluated for its antioxidant and antimicrobial using 1,1-diphenyl-2-picryl hydroxyl (DPPH{\textbullet}) radical scavenging assay, 2,2{\textquoteright}-azinobis3-ethyl benzothiazoline-6-sulfonic acid (ABTS{\textbullet}+), ferric reducing antioxidant power (FRAP), nitric oxide scavenging assay, superoxide anion radical scavenging assay (O2{\textbullet}-), hydrogen peroxide scavenging, reducing ability assay, metal ion chelating and phosphomolybdenum assays. Results: 40μg/ml of BTMP showed higher antioxidant activity than the other three doses due to its highest free radical scavenging ability at this particular dose. All doses of BTMP showed antimicrobial activity against E. coli and S. aureus. 40μg/ml of BTMP showed the highest zone of inhibition against both tested pathogens. Conclusion: The introduction of basic functionality and the presence of exocyclic double bonds of BTMP has significantly contributed to the antioxidant activity and antimicrobial activity against both gram-positive and gram-negative bacteria.

}, keywords = {Antibacterial, Antioxidant, Curcumin, DPPH, Reducing ability}, doi = {10.5530/pres.14.3.40}, author = {Jayaseelan Nivedha and Kaliyamoorthi Kanimozhi and Subashchandrabose Olikkavi and T. Vidhyasagar and Natesan Vijayakumar and Chinnaiyan Uma and K. Rajeswari and Lakshmanan Vennila} } @article {191, title = {Targeted Delivery of Curcumin Using MgONPs and Solid Lipid Nanoparticles: Attenuates Aluminum-Induced Neurotoxicity in Albino Rats}, journal = {Pharmacognosy Research}, volume = {12}, year = {2020}, month = {January 2021}, pages = {380-386}, type = {Original Article}, chapter = {380}, keywords = {Acetylcholine and acetylcholine esterase, Curcumin, Curcumin loaded magnesium oxide nanoparticles, Curcumin loaded solid lipid nanoparticles, Histological analyses}, doi = {10.4103/pr.pr_18_20}, author = {Swathi Ganna and Rajasekhara Reddy Gutturu and Rajesh Megala and Rasajna Nadella and Deva Prasad Raju Borelli and John Sushma Nannepaga} } @article {131, title = {Design and Development of Microparticulate Delivery System for Curcumin}, journal = {Pharmacognosy Research}, volume = {11}, year = {2019}, month = {August 2019}, pages = {321-328}, type = {Original Article}, chapter = {321}, abstract = {

Background: Curcumin has been associated with remarkable beneficial effects; despite having a broad spectrum of activities, curcumin is characterized by poor water solubility and low bioavailability. Objective: The objective of this study is to enhance the solubility of curcumin using polyethylene glycol 400 (PEG400) and establish a microparticulate drug delivery system in a sodium alginate polymer matrix (microspheres containing curcumin triturated with PEG400 [Cur-PEGMS]) to improve the bioavailability of curcumin. Materials and Methods: The microspheres were formulated using the ionic gelation technique. Nine batches (F1 to F9) were prepared using 32 factorial design. The amount of sodium alginate and calcium chloride was selected as a formulation variable. The prepared Cur-PEGMS were characterized by Fourier-transform infrared spectroscopy, scanning electron microscope, differential scanning calorimeter, ultraviolet spectrophotometer, and high-performance thin-layer chromatography (HPTLC). The pharmacokinetics of curcumin was characterized in rats using high-performance liquid chromatography, and calculations were performed using WinNonlin standard edition version 1.1 software. Results: We found that solubility was affected by the use of cosolvent. All F1{\textendash}F9 batches were investigated for entrapment efficiency, and batch F5 was found to be optimum batch which was further evaluated. HPTLC chromatogram of Cur-PEGMS shows peak retention for curcumin. The particle size of microspheres was found to be in the range of 384{\textendash}468 μm. Remarkable improvement in maximum plasma concentration and bioavailability was observed. Maximum the time after administration of a drug when maximum plasma concentration is reached (Tmax) was found to be 0.5 h, and AUC0{\textendash}24 was found to be 374.75 ng/ml and 622 ng/ml for curcumin suspension and curcumin microspheres, respectively. Conclusion: The developed formulation enhances the bioavailability of the drug. This enhanced oral absorption of Cur-PEGMS may provide a practical formulation to conduct a correlative pharmacodynamic study.

}, keywords = {Curcumin, Factorial design, Fharmacokinetics, Microspheres, Polyethylene glycol 400., Sodium alginate}, doi = {10.4103/pr.pr_24_19}, author = {Aditi Shrinivas Kulkarni and Santosh S. Bhujbal} } @article {391, title = {Ameliorative Effect of Curcumin on Olanzapine-induced Obesity in Sprague-Dawley Rats}, journal = {Pharmacognosy Research}, volume = {9}, year = {2017}, month = {July 2017}, pages = {247-252}, type = {Original Article}, chapter = {247}, abstract = {

Objective: To evaluate the effect of curcumin on olanzapine-induced obesity in rats. Materials and Methods: Sprague-Dawley (SD) rats were used for experiments. The animals were divided into six groups, namely, normal control, olanzapine control, betahistine (10 mg/kg), and curcumin 50, 100, and 200 mg/kg treated groups. Except the normal control group, all other animals were administered with olanzapine 4 mg/kg intraperitoneally to induce obesity. The drugs were administered once daily, per oral for 28 days. During the experiment, body weight changes and behavior alterations were monitored at regular intervals. At the end of the experiment, blood sample was collected from all the experimental animals for biochemical analysis. Part of the liver and kidney tissues was harvested from the sacrificed animals and preserved in neutral formalin for histopathological studies. Results: Curcumin showed a significant reduction in olanzapine-induced body weight gain on the rats and improved the locomotor effects. The effect of curcumin on olanzapine-induced body weight gain is not comparable with that of betahistine. Conclusion: This study has shown metabolic alteration effect of curcumin on olanzapine, an antipsychotic drug, treated SD rats.

}, keywords = {Betahistine, Curcumin, Obesity, Olanzapine}, doi = {10.4103/pr.pr_8_17}, author = {Subramani Parasuraman and Khor Ming Zhen and Urmila Banik and Parayil Varghese Christapher} } @article {544, title = {Curcumin and Natural Derivatives Inhibit Ebola Viral Proteins: An In silico Approach}, journal = {Pharmacognosy Research}, volume = {9}, year = {2017}, month = {December 2017}, pages = {s15-s22}, type = {Original Article}, chapter = {s15}, abstract = {

Background: Ebola viral disease is a severe and mostly fatal disease in humans caused by Ebola virus. This virus belongs to family Filoviridae and is a single-stranded negative-sense virus. There is no single treatment for this disease which puts forth the need to identify new therapy to control and treat this fatal condition. Curcumin, one of the bioactives of turmeric, has proven antiviral property. Objective: The current study evaluates the inhibitory activity of curcumin, bisdemethoxycurcumin, demethoxycurcumin, and tetrahydrocurcumin against Zaire Ebola viral proteins (VPs). Materials and Methods: Molecular simulation of the Ebola VPs followed by docking studies with ligands comprising curcumin and related compounds was performed. Results: The highest binding activity for VP40 is -6.3 kcal/mol, VP35 is -8.3 kcal/mol, VP30 is -8.0 kcal/mol, VP24 is -7.7 kcal/mol, glycoprotein is -7.1 kcal/mol, and nucleoprotein is 6.8 kcal/mol. Conclusion: Bisdemethoxycurcumin shows better binding affinity than curcumin for most VPs. Metabolite tetrahydrocurcumin also shows binding affinity comparable to curcumin. These results indicate that curcumin, curcuminoids, and metabolite tetrahydrocurcumin can be potential lead compounds for developing a new therapy for Ebola viral disease.

}, keywords = {Bisdemethoxycurcumin, Curcumin, Demethoxycurcumin, Docking, Ebola virus, Tetrahydrocurcumin}, doi = {10.4103/pr.pr_30_17}, author = {Shruti Baikerikar} } @article {962, title = {Inhibitory Effect of Rutin and Curcumin on Experimentally-induced Calcium Oxalate Urolithiasis in Rats}, journal = {Pharmacognosy Research}, volume = {2}, year = {2010}, month = {January 2011}, pages = {388-392}, type = {Short Communication}, chapter = {388}, abstract = {

Background: Renal epithelial cell injury by reactive oxygen species is pre-requisite step in the pathogenesis of urolithiasis. Rutin and curcumin are polyphenolic compounds known to have antioxidant and anti-inflammatory activities, but their effect on urolithiasis is yet to be elucidated. In the present study, we have investigated the inhibitory effect of rutin and curcumin on calcium oxalate urolithiasis in Wistar albino rats. Methods: Calcium oxalate urolithiasis was induced experimentally by administration of 0.75\% v/v ethylene glycol with 1\% w/v ammonium chloride in drinking water for three days followed by only 0.75\% v/v ethylene glycol for 25 days. Rutin (20 mg/kg body weight) and curcumin (60 mg/kg body weight) were given once daily for 28 days by oral route. After treatment period, calcium and oxalate levels in urine and kidney tissue homogenate were measured. Kidney was also used for histopathological examination. Results: Stone-induction with ethylene glycol and ammonium chloride resulted in elevated levels of calcium and oxalate in the urine and kidney sample, whereas supplementation of rutin and curcumin restored it near to normal. Histopathological study revealed minimum tissue damage and less number of calcium oxalate deposits in kidney of animal treated with rutin and curcumin as compared to calculi-induced animal. Conclusion: The data suggest that the rutin and curcumin inhibits calcium oxalate urolithiasis. This effect is mediated possibly through a lowering of urinary concentration of stone forming constituents, anti-inflammatory and antioxidant effects.

}, keywords = {Calcium oxalate, Curcumin, Ethylene glycol, Rutin, Urolithiasis}, doi = {10.4103/0974-8490.75462}, author = {Jaydip Ghodasara and Anil Pawar and Chinmay Deshmukh and Bhanudas Kuchekar} }