Displaying publications 1 - 20 of 44 in total

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  1. Curcumin in a model skin lotion formulation
    Suhaimi H, Ahmad FB, Friberg SE
    J Pharm Sci, 1995 Mar;84(3):376-80.
    PMID: 7616381
    A lamellar liquid crystalline region was identified in a typical skin lotion formulation system composed of a mixture of isostearic acid and triethanolamine (TEA) at 65:35 (w/w), decane, and water (the temperature was controlled at 30 degrees C). The interlayer spacings were determined by a small-angle X-ray diffraction technique. Incorporation of a natural dye, curcumin, resulted in lower interlayer spacings and higher penetration of water into the layered structure. However, the higher penetration of water was not apparent at all compositions of isostearic acid:TEA, decane, and water.
    Matched MeSH terms: Curcumin/chemistry*
  2. Fulltext Rapid Green Synthesis and Characterization of Silver Nanoparticles Arbitrated by Curcumin in an Alkaline Medium
    Khan MJ, Shameli K, Sazili AQ, Selamat J, Kumari S
    Molecules, 2019 Feb 16;24(4).
    PMID: 30781541 DOI: 10.3390/molecules24040719
    Green synthesis of silver nanoparticles is desirable practice. It is not only the required technique for industrial and biomedical purposes but also a promising research area. The aim of this study was to synthesize green curcumin silver nanoparticles (C-Ag NPs). The synthesis of C-Ag NPs was achieved by reduction of the silver nitrate (AgNO₃) in an alkaline medium. The characterizations of the prepared samples were conducted by ultraviolet visible (UV-vis) spectroscopy, powder X-ray diffraction (PXRD), field emission scanning electron microscopy (FESEM), high-resolution transmission electron microscopy (HRTEM), selected area electron diffraction (SAED) and zeta potential (ZP) analyses. The formation of C-Ag NPs was evaluated by the dark color of the colloidal solutions and UV-vis spectra, with 445 nm as the maximum. The size of the crystalline nanoparticles, recorded as 12.6 ± 3.8nm, was confirmed by HRTEM, while the face-centered cubic (fcc) crystallographic structure was confirmed by PXRD and SAED. It is assumed that green synthesized curcumin silver nanoparticles (C-Ag NPs) can be efficiently utilized as a strong antimicrobial substance for food and meat preservation due to their homogeneous nature and small size.
    Matched MeSH terms: Curcumin/chemistry
  3. Hydrophobic kenaf nanocrystalline cellulose for the binding of curcumin
    Zainuddin N, Ahmad I, Kargarzadeh H, Ramli S
    Carbohydr Polym, 2017 May 01;163:261-269.
    PMID: 28267505 DOI: 10.1016/j.carbpol.2017.01.036
    Nanocrystalline cellulose (NCC) extracted from lignocellulosic materials has been actively investigated as a drug delivery excipients due to its large surface area, high aspect ratio, and biodegradability. In this study, the hydrophobically modified NCC was used as a drug delivery excipient of hydrophobic drug curcumin. The modification of NCC with a cationic surfactant, cetyl trimethylammonium bromide (CTAB) was used to modulate the loading of hydrophobic drugs that would not normally bind to NCC. The FTIR, Elemental analysis, XRD, TGA, and TEM were used to confirm the modification of NCC with CTAB. The effect of concentration of CTAB on the binding efficiency of hydrophobic drug curcumin was investigated. The amounts of curcumin bound onto the CTAB-NCC nanoparticles were analyzed by UV-vis Spectrophotometric. The result showed that the modified CTAB-NCC bound a significant amount of curcumin, in a range from 80% to 96% curcumin added. Nevertheless, at higher concentration of CTAB resulted in lower binding efficiency.
    Matched MeSH terms: Curcumin/chemistry*
  4. Solubility of core materials in aqueous polymeric solution effect on microencapsulation of curcumin
    Aziz HA, Peh KK, Tan YT
    Drug Dev Ind Pharm, 2007 Nov;33(11):1263-72.
    PMID: 18058323
    Curcumin, the main active constituent of turmeric herb (Curcuma longa L.) have been reported to possess many medicinal values. The application of curcumin in dermatological preparations is limited by their intense yellow color property, which stains the fabric and skin. The objectives of this study were to reduce the color staining effect and enhance the stability of curcumin via microencapsulation using gelatin simple coacervation method. As for curcumin, ethanol and acetone were used as coacervating solvents. Curcumin was dispersed in ethanol while dissolved in acetone. Irrespective of the types of coacervating solvents used, microencapsulation resolved the color-staining problem and enhanced the flow properties and photo-stability of curcumin. Nevertheless, it was found that more spherical curcumin microcapsules with higher yield, higher curcumin loading, and higher entrapment efficiency were obtained with acetone than ethanol. The in vitro release of curcumin after microencapsulation was slightly prolonged. Further evaluation of the effects of solubility of core materials in coacervating solvent or polymeric aqueous solution using six different drug compounds, namely, ketoconazole, ketoprofen, magnesium stearate, pseudoephedrine HCl, diclofenac sodium, and paracetamol, suggested that the solubility of core materials in aqueous polymeric solution determined the successful formation of microcapsules. Microcapsules could only be formed if the core materials were not dissolved in the aqueous polymeric solution while the core materials could either be dissolved or dispersed in the coacervating solvent. In summary, microencapsulation not only circumvents the color-staining problem but also improved the stability and flowability of curcumin. The solubility of core material in aqueous polymeric solution plays a pivotal role in determining the successful formation of microcapsules.
    Matched MeSH terms: Curcumin/chemistry*
  5. Current prospects of synthetic curcumin analogs and chalcone derivatives against mycobacterium tuberculosis
    Bukhari SN, Franzblau SG, Jantan I, Jasamai M
    Med Chem, 2013 Nov;9(7):897-903.
    PMID: 23305394
    Tuberculosis, caused by Mycobacterium tuberculosis, is amongst the foremost infectious diseases. Treatment of tuberculosis is a complex process due to various factors including a patient's inability to persevere with a combined treatment regimen, the difficulty in eradicating the infection in immune-suppressed patients, and multidrug resistance (MDR). Extensive research circumscribing molecules to counteract this disease has led to the identification of many inhibitory small molecules. Among these are chalcone derivatives along with curcumin analogs. In this review article, we summarize the reported literature regarding anti tubercular activity of chalcone derivatives and synthetic curcumin analogs. Our goal is to provide an analysis of research to date in order to facilitate the synthesis of superior antitubercular chalcone derivatives and curcumin analogs.
    Matched MeSH terms: Curcumin/chemistry
  6. An Evaluation of Curcumin-Encapsulated Chitosan Nanoparticles for Transdermal Delivery
    Nair RS, Morris A, Billa N, Leong CO
    AAPS PharmSciTech, 2019 Jan 10;20(2):69.
    PMID: 30631984 DOI: 10.1208/s12249-018-1279-6
    Curcumin-loaded chitosan nanoparticles were synthesised and evaluated in vitro for enhanced transdermal delivery. Zetasizer® characterisation of three different formulations of curcumin nanoparticles (Cu-NPs) showed the size ranged from 167.3 ± 3.8 nm to 251.5 ± 5.8 nm, the polydispersity index (PDI) values were between 0.26 and 0.46 and the zeta potential values were positive (+ 18.1 to + 20.2 mV). Scanning electron microscopy (SEM) images supported this size data and confirmed the spherical shape of the nanoparticles. All the formulations showed excellent entrapment efficiency above 80%. FTIR results demonstrate the interaction between chitosan and sodium tripolyphosphate (TPP) and confirm the presence of curcumin in the nanoparticle. Differential scanning calorimetry (DSC) studies of Cu-NPs indicate the presence of curcumin in a disordered crystalline or amorphous state, suggesting the interaction between the drug and the polymer. Drug release studies showed an improved drug release at pH 5.0 than in pH 7.4 and followed a zero order kinetics. The in vitro permeation studies through Strat-M® membrane demonstrated an enhanced permeation of Cu-NPs compared to aqueous curcumin solution (p ˂ 0.05) having a flux of 0.54 ± 0.03 μg cm-2 h-1 and 0.44 ± 0.03 μg cm-2 h-1 corresponding to formulations 5:1 and 3:1, respectively. The cytotoxicity assay on human keratinocyte (HaCat) cells showed enhanced percentage cell viability of Cu-NPs compared to curcumin solution. Cu-NPs developed in this study exhibit superior drug release and enhanced transdermal permeation of curcumin and superior percentage cell viability. Further ex vivo and in vivo evaluations will be conducted to support these findings.
    Matched MeSH terms: Curcumin/chemistry
  7. Biological evaluation of curcumin and related diarylheptanoids
    Abas F, Hui LS, Ahmad S, Stanslas J, Israf DA, Shaari K, et al.
    Z Naturforsch C J Biosci, 2006 12 2;61(9-10):625-31.
    PMID: 17137104
    Nine derivatives of three natural diarylheptanoids, curcumin, demethoxycurcumin and bisdemethoxycurcumin, were prepared. Their antioxidant, free radical scavenging, nitric oxide (NO) inhibitory and cytotoxic activities were evaluated and compared with those of the respective natural compounds. Curcumin (1), demethoxycurcumin (2), demethyldemethoxy-curcumin (C3), diacetyldemethoxycurcumin (AC2) and triacetyldemethylcurcumin (AC5) exhibited higher antioxidant activity than quercetin while products from demethylation of 1 and 2 exhibited higher free radical scavenging activity. Compounds AC2 and AC5 were found to be most active in inhibiting breast cancer cells (MCF-7) proliferation with IC50 values of 6.7 and 3.6 microM, respectively. The activity of AC2 is almost doubled and of AC5 almost tripled as compared to curcumin. Their selectivity towards different cell lines is also more noticeable. Compounds AC2 and AC5 also showed increased activity against a human prostate cancer cell line (DU-145) and non-small lung cancer cell line (NCI-H460) with IC50 values of 20.4, 16.3 and 18.3, 10.7 microM, respectively.
    Matched MeSH terms: Curcumin/chemistry
  8. Fulltext Curcuma longa ethanol extract and Curcumin inhibit the growth of Acanthamoeba triangularis trophozoites and cysts isolated from water reservoirs at Walailak University, Thailand
    Mitsuwan W, Bunsuwansakul C, Leonard TE, Laohaprapanon S, Hounkong K, Bunluepuech K, et al.
    Pathog Glob Health, 2020 05 18;114(4):194-204.
    PMID: 32315247 DOI: 10.1080/20477724.2020.1755551
    CURCUMA LONGA: (C. longa) rhizome extract has been traditionally used to treat many infections. Curcumin, a pure compound isolated from the plant, has been documented to possess a wide spectrum of pharmacological effects. The present study aimed to investigate the effects of Thai medicinal plant extracts including C. longa extract and Curcumin on Acanthamoeba triangularis, a causative agent of human Acanthamoeba keratitis. The parasite was isolated from the recreational reservoir at Walailak University, Thailand. The organism was identified as A. triangularis using morphology and 18S rDNA nucleotide sequences. The pathogen was tested for their susceptibility to ethanol extracts of Thai medicinal plants based on eye infection treatment. The ethanol C. longa extract showed the strongest anti-Acanthamoeba activity against both the trophozoites and cysts, followed by Coscinium fenestratum, Coccinia grandis, and Acmella oleracea extracts, respectively. After 24 h, 95% reduction of trophozoite viability was significantly decreased following the treatment with C. longa extract at 125 µg/mL, compared with the control (P Curcumin against the trophozoites were 125 and 62.5 µg/mL, respectively. While the MICs of the extract and curcumin against the cysts were 500 and 1,000 µg/mL, respectively. The results suggested the potential medicinal benefits of C. longa extract and Curcumin as the alternative treatment of Acanthamoeba infections.
    Matched MeSH terms: Curcumin/chemistry*
  9. Fulltext Nanotechnology in drug delivery gaining new perspectives in respiratory diseases
    Dua K, Madan JR, Chellappan DK, Gupta G
    Panminerva Med, 2018 09;60(3):135-136.
    PMID: 30176702 DOI: 10.23736/S0031-0808.18.03442-0
    Matched MeSH terms: Curcumin/chemistry
  10. Thermoresponsive curcumin/DsiRNA nanoparticle gels for the treatment of diabetic wounds: synthesis and drug release
    Katas H, Wen CY, Siddique MI, Hussain Z, Mohd Fadhil FH
    Ther Deliv, 2017 01;8(3):137-150.
    PMID: 28145827 DOI: 10.4155/tde-2016-0075
    AIM: Chitosan (CS) has been extensively studied as drug delivery systems for wound healing. Results/methodology: CS nanoparticles were loaded with curcumin (Cur) and DsiRNA against prostaglandin transporter gene and they were incorporated into 20 and 25% w/v Pluronic F-127. The gels were later analyzed for their rheology, gelation temperature (Tgel), morphology, drug incorporation and in vitro drug release. The particle size was in the range of 231 ± 17-320 ± 20 nm, depending on CS concentration. The gels had Tgel of 23-28°C and exhibited sustained drug release with high accumulated amount of drugs over 48 h.

    CONCLUSION: A thermo-sensitive gel containing Cur/DsiRNA CS nanoparticles was successfully developed and has a great potential to be further developed.

    Matched MeSH terms: Curcumin/chemistry*
  11. Fulltext Modeling the Effect of Composition on Formation of Aerosolized Nanoemulsion System Encapsulating Docetaxel and Curcumin Using D-Optimal Mixture Experimental Design
    Asmawi AA, Salim N, Abdulmalek E, Abdul Rahman MB
    Int J Mol Sci, 2020 Jun 19;21(12).
    PMID: 32575390 DOI: 10.3390/ijms21124357
    The synergistic anticancer effect of docetaxel (DTX) and curcumin (CCM) has emerged as an attractive therapeutic candidate for lung cancer treatment. However, the lack of optimal bioavailability because of high toxicity, low stability, and poor solubility has limited their clinical success. Given this, an aerosolized nanoemulsion system for pulmonary delivery is recommended to mitigate these drawbacks. In this study, DTX- and CCM-loaded nanoemulsions were optimized using the D-optimal mixture experimental design (MED). The effect of nanoemulsion compositions towards two response variables, namely, particle size and aerosol size, was studied. The optimized formulations for both DTX- and CCM-loaded nanoemulsions were determined, and their physicochemical and aerodynamic properties were evaluated as well. The MED models achieved the optimum formulation for DTX- and CCM-loaded nanoemulsions containing a 6.0 wt% mixture of palm kernel oil ester (PKOE) and safflower seed oils (1:1), 2.5 wt% of lecithin, 2.0 wt% mixture of Tween 85 and Span 85 (9:1), and 2.5 wt% of glycerol in the aqueous phase. The actual values of the optimized formulations were in line with the predicted values obtained from the MED, and they exhibited desirable attributes of physicochemical and aerodynamic properties for inhalation therapy. Thus, the optimized formulations have potential use as a drug delivery system for a pulmonary application.
    Matched MeSH terms: Curcumin/chemistry
  12. Fulltext Adsorption and in vitro release study of curcumin form polyethyleneglycol functionalized multi walled carbon nanotube: kinetic and isotherm study
    Koupaei Malek S, Gabris MA, Hadi Jume B, Baradaran R, Aziz M, Karim KJBA, et al.
    Daru, 2019 Jun;27(1):9-20.
    PMID: 30554368 DOI: 10.1007/s40199-018-0232-2
    Polyethylene glycol functionalized with oxygenated multi-walled carbon nanotubes (O-PEG-MWCNTs) as an efficient nanomaterial for the in vitro adsorption/release of curcumin (CUR) anticancer agent. The synthesized material was morphologically characterized using scanning electron microscopy, Fourier transform infrared spectroscopy and transmission electron microscopy. In addition, the CUR adsorption process was assessed with kinetic and isotherm models fitting well with pseudo-second order and Langmuir isotherms. The results showed that the proposed O-PEG-MWCNTs has a high adsorption capacity for CUR (2.0 × 103 mg/g) based on the Langmuir model. The in vitro release of CUR from O-PEG-MWCNTs was studied in simulating human body fluids with different pHs (ABS pH 5, intestinal fluid pH 6.6 and body fluid pH 7.4). Lastly, to confirm the success compliance of the O-PEG-MWCNT nanocomposite as a drug delivery system, the parameters affecting the CUR release such as temperature and PEG content were investigated. As a result, the proposed nanocomposite could be used as an efficient carrier for CUR delivery with an enhanced prolonged release property. Graphical Abstract ᅟ.
    Matched MeSH terms: Curcumin/chemistry*
  13. Effects of novel diarylpentanoid analogues of curcumin on secretory phospholipase A2 , cyclooxygenases, lipo-oxygenase, and microsomal prostaglandin E synthase-1
    Ahmad W, Kumolosasi E, Jantan I, Bukhari SN, Jasamai M
    Chem Biol Drug Des, 2014 Jun;83(6):670-81.
    PMID: 24406103 DOI: 10.1111/cbdd.12280
    Arachidonic acid and its metabolites have generated a heightened interest due to their significant role in inflammation. Inhibiting the enzymes involved in arachidonic acid metabolism has been considered as the synergistic anti-inflammatory effect. A series of novel curcumin diarylpentanoid analogues were synthesized and evaluated for their inhibitory effects on activity of secretory phospholipase A2 , cyclooxygenases, soybean lipo-oxygenase as well as microsomal prostaglandin E synthase-1. Among the curcumin analogues, compounds 3, 6, 9, 12, and 17 exhibited strong inhibition of secretory phospholipase A2 activity, with IC50 values ranging from 5.89 to 11.02 μm. Seven curcumin analogues 1, 3, 6, 7, 9, 11, and 12 showed inhibition of cyclooxygenases-2 with IC50 values in the range of 46.11 to 94.86 μm, which were lower than that of curcumin. Compounds 3, 6, 7, 12, and 17 showed strong inhibition of lipo-oxygenase enzyme activity. Preliminary screening of diarylpentanoid curcumin analogues for microsomal prostaglandin E synthase-1 activity revealed that four diarylpentanoid curcumin analogues 5, 6, 7, and 13 demonstrated higher inhibition of microsomal prostaglandin E synthase-1 activity with IC50 ranging from 2.41 to 4.48 μm, which was less than that of curcumin. The present results suggest that some of these diarylpentanoid analogues were able to inhibit the activity of these enzymes. This raises the possibility that diarylpentanoid analogues of curcumin might serve as useful starting point for the design of improved anti-inflammatory agents.
    Matched MeSH terms: Curcumin/chemistry
  14. Antioxidative constituents of Etlingera elatior
    Mohamad H, Lajis NH, Abas F, Ali AM, Sukari MA, Kikuzaki H, et al.
    J Nat Prod, 2005 Feb;68(2):285-8.
    PMID: 15730265
    Phytochemical studies on the rhizomes of Etlingera elatior have resulted in the isolation of 1,7-bis(4-hydroxyphenyl)-2,4,6-heptatrienone (1), demethoxycurcumin (2), 1,7-bis(4-hydroxyphenyl)-1,4,6-heptatrien-3-one (3), 16-hydroxylabda-8(17),11,13-trien-15,16-olide (4), stigmast-4-en-3-one, stigmast-4-ene-3,6-dione, stigmast-4-en-6beta-ol-3-one, and 5alpha,8alpha-epidioxyergosta-6,22-dien-3beta-ol. Compounds 1 and 4 are new, and their structures were elucidated by analysis of spectroscopic data. Diarylheptanoids 1-3 were found to inhibit lipid peroxidation in a more potent manner than alpha-tocopherol.
    Matched MeSH terms: Curcumin/chemistry
  15. Fulltext Fluorine-19 Magnetic Resonance Imaging for Detection of Amyloid β Oligomers Using a Keto Form of Curcumin Derivative in a Mouse Model of Alzheimer's Disease
    Yanagisawa D, Ibrahim NF, Taguchi H, Morikawa S, Tomiyama T, Tooyama I
    Molecules, 2021 Mar 04;26(5).
    PMID: 33806326 DOI: 10.3390/molecules26051362
    Recent evidence suggests that the formation of soluble amyloid β (Aβ) aggregates with high toxicity, such as oligomers and protofibrils, is a key event that causes Alzheimer's disease (AD). However, understanding the pathophysiological role of such soluble Aβ aggregates in the brain in vivo could be difficult due to the lack of a clinically available method to detect, visualize, and quantify soluble Aβ aggregates in the brain. We had synthesized a novel fluorinated curcumin derivative with a fixed keto form, named as Shiga-Y51, which exhibited high selectivity to Aβ oligomers in vitro. In this study, we investigated the in vivo detection of Aβ oligomers by fluorine-19 (19F) magnetic resonance imaging (MRI) using Shiga-Y51 in an APP/PS1 double transgenic mouse model of AD. Significantly high levels of 19F signals were detected in the upper forebrain region of APP/PS1 mice compared with wild-type mice. Moreover, the highest levels of Aβ oligomers were detected in the upper forebrain region of APP/PS1 mice in enzyme-linked immunosorbent assay. These findings suggested that 19F-MRI using Shiga-Y51 detected Aβ oligomers in the in vivo brain. Therefore, 19F-MRI using Shiga-Y51 with a 7 T MR scanner could be a powerful tool for imaging Aβ oligomers in the brain.
    Matched MeSH terms: Curcumin/chemistry
  16. Preparation and photodynamic bactericidal effects of curcumin-β-cyclodextrin complex
    Lai D, Zhou A, Tan BK, Tang Y, Sarah Hamzah S, Zhang Z, et al.
    Food Chem, 2021 Nov 01;361:130117.
    PMID: 34058659 DOI: 10.1016/j.foodchem.2021.130117
    To overcome the poor water solubility of curcumin, a curcumin-β-cyclodextrin (Cur-β-CD) complex was prepared as a novel photosensitizer. Fourier-transform infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC), and X-ray diffraction (XRD) were used to verify the formation of Cur-β-CD. Furthermore, the ROS generation capacity and photodynamic bactericidal effect were measured to confirm this Cur-β-CD complex kept photodynamic activity of curcumin. The result showed Cur-β-CD could effectively generate ROS upon blue-light irradiation. The plate count assay demonstrated Cur-β-CD complex possess desirable photodynamic antibacterial effect against food-borne pathogens including Staphylococcus aureus, Listeria monocytogenes and Escherichia coli. The cell morphology determined by scanning electron microscope (SEM) and transmission electron microscope (TEM) showed Cur-β-CD could cause cell deformation, surface collapse and cell structure damage of the bacteria, resulting in the leakage of cytoplasmic; while agarose gel electrophoresis and SDS-PAGE further illustrated the inactivation mechanisms by Cur-β-CD involve bacterial DNA damage and protein degradation.
    Matched MeSH terms: Curcumin/chemistry*
  17. Docking Studies of Curcumin and Analogues with Various Phosphodiesterase 4 Subtypes
    Yi YX, Gaurav A, Akowuah GA
    Curr Drug Discov Technol, 2020;17(2):248-260.
    PMID: 30332967 DOI: 10.2174/1570163815666181017091655
    INTRODUCTION: The primary aim of this study is to understand the binding of curcumin and its analogues to different PDE4 subtypes and identify the role of PDE4 subtype inhibition in the anti-inflammatory property of curcumin. Docking analysis has been used to acquire the above mentioned structural information and this has been further used for designing of curcumin derivatives with better anti-inflammatory activity.

    MATERIALS AND METHODS: Curcumin and its analogues were subjected to docking using PDE4A, PDE4B, PDE4C and PDE4D as the targets. A data set comprising 18 analogues of curcumin, was used as ligands for docking of PDE4 subtypes. Curcumin was used as the standard for comparison. Docking was performed using AutoDock Vina 1.1.2 software integrated in LigandScout 4.1. During this process water molecules were removed from proteins, charges were added and receptor structures were minimised by applying suitable force fields. The docking scores were compared, and the selectivity of compounds for PDE4B over PDE4D was calculated as well.

    RESULTS: All curcumin analogues used in the study showed good binding affinity with all PDE4 subtypes, with evident selectivity towards PDE4B subtype. Analogue A11 provides the highest binding affinity among all ligands.

    CONCLUSION: Curcumin and analogues have moderate to strong affinity towards all PDE4 subtypes and have evident selectivity towards PDE4B. The Oxygen atom of the methoxy group plays a key role in PDE4B binding and any alterations could interfere with the binding. Tetrahydropyran side chain and heterocyclic rings are also suggested to be helpful in PDE4B binding.

    Matched MeSH terms: Curcumin/chemistry
  18. An overview of structure-activity relationship studies of curcumin analogs as antioxidant and anti-inflammatory agents
    Arshad L, Haque MA, Abbas Bukhari SN, Jantan I
    Future Med Chem, 2017 04;9(6):605-626.
    PMID: 28394628 DOI: 10.4155/fmc-2016-0223
    Curcumin, extracted mainly from Curcuma longa rhizomes, has been reported to possess potent anti-inflammatory and anti-oxidant activities. Although safe at higher doses and exhibiting multiple biological activities, curcumin still has the problem of poor bioavailability which has been an attractive area of research over the last few years. A number of efforts have been made by modifying structural features of curcumin. This review highlights the structurally modified and more stable newly synthesized curcumin analogs that have been screened against antioxidant and anti-inflammatory activities. Also the structure-activity relationship to gain insight into future guidelines for scheming new compounds has been discussed, and further these analogs being more stable may serve as promising agents for use in different pathological conditions.
    Matched MeSH terms: Curcumin/chemistry
  19. Fulltext DK1 Induces Apoptosis via Mitochondria-Dependent Signaling Pathway in Human Colon Carcinoma Cell Lines In Vitro
    Hussin Y, Aziz MNM, Che Rahim NF, Yeap SK, Mohamad NE, Masarudin MJ, et al.
    Int J Mol Sci, 2018 Apr 11;19(4).
    PMID: 29641445 DOI: 10.3390/ijms19041151
    Extensive research has been done in the search for innovative treatments against colon adenocarcinomas; however, the incidence rate of patients remains a major cause of cancer-related deaths in Malaysia. Natural bioactive compounds such as curcumin have been substantially studied as an alternative to anticancer drug therapies and have been surmised as a potent agent but, nevertheless, remain deficient due to its poor cellular uptake. Therefore, efforts now have shifted toward mimicking curcumin to synthesize novel compounds sharing similar effects. A synthetic analog, (Z)-3-hydroxy-1-(2-hydroxyphenyl)-3-phenylprop-2-ene-1-one (DK1), was recently synthesized and reported to confer improved bioavailability and selectivity toward human breast cancer cells. This study, therefore, aims to assess the anticancer mechanism of DK1 in relation to the induction of in vitro cell death in selected human colon cancer cell lines. Using the3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide(MTT) assay, the cytotoxicity of DK1 towards HT29 and SW620 cell lines were investigated. Acridine orange/propidium iodide (AO/PI) dual-staining assay and flow cytometry analyses (cell cycle analysis, Annexin/V-FITC and JC-1 assays) were incorporated to determine the mode of cell death. To further determine the mechanism of cell death, quantitative real-time polymerase chain reaction (qRT-PCR) and proteome profiling were conducted. Results from this study suggest that DK1 induced changes in cell morphology, leading to a decrease in cell viability and subsequent induction of apoptosis. DK1 treatment inhibited cell viability and proliferation 48 h post treatment with IC50 values of 7.5 ± 1.6 µM for HT29 cells and 14.5 ± 4.3 µM for SW620 cells, causing cell cycle arrest with increased accumulation of cell populations at the sub-G₀/G₁phaseof 74% and 23%, respectively. Flow cytometry analyses showed that DK1 treatment in cancer cells induced apoptosis, as indicated by DNA fragmentation and depolarization of the mitochondrial membrane. qRT-PCR results show significant upregulation in the expression of caspase-9 in both HT29 and SW620 cell lines, further supporting that cell death induction by DK1 is via an intrinsic pathway. These outcomes, therefore, demonstrate DK1 as a potential anticancer agent for colon adenocarcinoma due to its anti-apoptotic attributes.
    Matched MeSH terms: Curcumin/chemistry
  20. 3,5-Bis[4-(diethoxymethyl)benzylidene]-1-methyl-piperidin-4-one, a Novel Curcumin Analogue, Inhibits Cellular and Humoral Immune Responses in Male Balb/c Mice
    Arshad L, Jantan I, Bukhari SNA, Fauzi MB
    Curr Pharm Biotechnol, 2018;19(6):468-482.
    PMID: 29968535 DOI: 10.2174/1389201019666180703092723
    BACKGROUND: 3,5-Bis[4-(diethoxymethyl)benzylidene]-1-methyl-piperidin-4-one (BBP), a novel synthetic curcumin analogue has previously been shown to manifest potent immunosuppressive effects on the in vitro phagocytosis process of human neutrophils.

    OBJECTIVE: In the present study, BBP was investigated for it's in vivo innate and adaptive immune responses mediated by different humoral and cellular immune factors.

    METHODS: Male Balb/c mice were orally fed with BBP (5, 10 and 20 mg/kg) for a period of 14 days and immunized with sheep red blood cells (sRBC) on day 0 for the determination of adaptive responses. The effects of BBP on phagocytosis process of neutrophils isolated from blood of treated/untreated animals were determined. The ceruloplasmin and lysozyme serum levels and myeloperoxidase (MPO) plasma level were also monitored. The mechanism was further explored by assessing its effects on the proliferation of T and B lymphocytes, T-lymphocytes subsets CD4+ and CD8+ and on the secretion of Th1/Th2 cytokines as well as serum immunoglobulins (IgG, IgM) and delayed type hypersensitivity (DTH) reaction.

    RESULTS: BBP showed a significant dose-dependent reduction on the migration of neutrophils, Mac-1 expression, phagocytic activity and reactive oxygen species (ROS) production. In comparison to the sensitized control group, a dose-dependent inhibition was observed on lymphocyte proliferation along with the downregulation of effector cells expression and release of cytokines. Moreover, a statistically significant decrease was perceived in serum levels of ceruloplasmin, lysozyme and immunoglobulins and MPO plasma level of BBP-treated mice. BBP also dose-dependently inhibited sheep red blood cells (sRBC)-induced swelling rate of mice paw in DTH.

    CONCLUSION: These findings suggest the potential of BBP as a potent immunosuppressive agent.

    Matched MeSH terms: Curcumin/chemistry
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